Page last updated: 2024-10-15

rifampin

Description

Rifampin: A semisynthetic antibiotic produced from Streptomyces mediterranei. It has a broad antibacterial spectrum, including activity against several forms of Mycobacterium. In susceptible organisms it inhibits DNA-dependent RNA polymerase activity by forming a stable complex with the enzyme. It thus suppresses the initiation of RNA synthesis. Rifampin is bactericidal, and acts on both intracellular and extracellular organisms. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p1160) [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID136122621
SCHEMBL ID23491
MeSH IDM0019110
PubMed CID135398735
CHEMBL ID374478
CHEBI ID28077
SCHEMBL ID23490
MeSH IDM0019110

Synonyms (210)

Synonym
NCGC00094777-01
tox21_300550
NCGC00254537-01
tox21_201385
NCGC00258936-01
cas-13292-46-1
tox21_111329
BRD-K01507359-001-12-0
SCHEMBL23491
NCGC00179536-02
tox21_111329_1
AS-13687
AKOS034819783
BRD-K01507359-001-22-9
2094025-69-9
EN300-26868961
(7s,11s,12r,13s,14r,15r,16r,17s,18s,19z,21z)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-[(e)-[(4-methylpiperazin-1-yl)imino]methyl]-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1^{4,7}.0^{5,28}]triaconta-1,3,5(28),9,19,21,25(
Z1515376764
rifampicin & eep
rifampicin & propolis
rifamcin
CHEBI:28077 ,
rifampicina
(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-{(e)-[(4-methylpiperazin-1-yl)imino]methyl}-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.1(4,7).0(5,28)]triaconta-1(28),1(29),2,4,9,19
(2s,12z,14e,16s,17s,18r,19r,20r,21s,22r,23s,24e)-5,6,9,17,19-pentahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-{(e)-[(4-methylpiperazin-1-yl)imino]methyl}-1,11-dioxo-1,2-dihydro-2,7-(epoxypentadeca[1,11,13]trienoimino)naphtho[2,1-b]furan-21-yl ac
(2s,12z,14e,16s,17s,18r,19r,20r,21s,22r,23s,24e)-5,6,9,17,19-pentahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-{(e)-[(4-methylpiperazin-1-yl)imino]methyl}-1,11-dioxo-1,2-dihydro-2,7-(epoxypentadeca[1,11,13]trienoimino)naphtho[2,1-b]furan-21-yl acet
rifampin [usan]
5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-(n-(4-methyl-1-piperazinyl)formimidoyl)-2,7-(epoxypentadeca(1,11,13)trienimino)naphtho(2,1-b)furan-1,11(2h)-dione 21-acetate
einecs 236-312-0
2,7-(epoxypentadeca(1,11,13)trienimino)naphtho(2,1-b)furan-1,11(2h)-dione, 5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-(n-(4-methyl-1-piperazinyl)formimidoyl)-, 21-acetate
nsc 113926
rifampicin [inn:ban:jan]
l-5103 ,
rifamsolin
ba-41166e
rifampin (usp)
rifampicin (jp17/inn)
D00211
rimactane (tn)
rifadin (tn)
PRESTWICK_833
BSPBIO_000509
PRESTWICK2_000525
BPBIO1_000561
SPECTRUM5_002018
PRESTWICK3_000525
RFP ,
RIF ,
rimactizid
[pentahydroxy-methoxy-heptamethyl-[(e)-(4-methylpiperazin-1-yl)iminomethyl]-dioxo-[?]yl] acetate
rifampicin sv
rifaldin
l-5103 lepetit
rifaldazine
rifampin
riforal
2,11,13]trienimino)naphtho[2,1-b]furan-1,11(2h)-dione, 5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-[n-(4-methyl-1-piperazinyl)formimidoyl]-, 21-acetate
8-[[(4-methyl-1-piperazinyl)imino]methyl]rifamycin sv
rimazid
rifa
stereoisomer of 5,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-he@ptamethyl-8-[n-(4-methyl-1-piperazinyl)formimidoyl]-2,7-(epoxypentadeca[1,11,13]trienimino)naphtho[2,1-b]furan-1,11(2h)-dione 21-acetate
3-([(4-methyl-1-piperazinyl)imino]methyl)rifamycin sv
ba 41166
13292-46-1
rimactane
rifaprodin
wln: v1 wq a&1 e&1 e1un- at6n dntj d1
8-[[(4-methylpiperazinyl)imino]methyl]rifamycin sv
ba 41166/e
rimactan
archidyn
rifoldin
rifamycin, 3-[[(4-methyl-1-piperazinyl)imino]methyl]-
3-[(4-methyl-1-piperazinyl)iminomethyl]rifamycin sv
tubocin
RIFAMPICIN ,
nsc113926 ,
r/amp
rifadine
rifamycin amp
rifomycin sv, 8-[n-(4-methyl-1-piperazinyl)formidoyl]-
rifampicine
rifadin
nsc-113926
rifoldine
rifagen
3-(4-methylpiperazinyliminomethyl)-rifamycin sv
8ci)
5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-(n-(4-methyl-1-piperazinyl)formimidoyl)-2,7-(epoxypentadeca(1,11,13)trienimino)naphtho(2,1-beta)furan-1,11(2h)-dione 21-acetate
rifaldazin
3-[[(4-methyl-1-piperazinyl)imino]-methyl]rifamycin
doloresum
rifinah
rifcin
rifomycin sv, 8-(n-(4-methyl-1-piperazinyl)formidoyl)-
8-(4-methylpiperazinyliminomethyl) rifamycin sv
rifampicina [inn-spanish]
rifamycin, 3-(((4-methyl-1-piperazinyl)imino)methyl)-
2,7-(epoxy[1,11,13]pentadecatrienoimino)naphtho[2,1-b]furan-1,11(2h)-dione, 21-(acetyloxy)-5,6,9,17,19-pentahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-[(e)-[(4-methyl-1-piperazinyl)imino]meth
rifobac
drg-0109
rifamor
ccris 551
rifampicinum [inn-latin]
hsdb 3181
rifampicinum
arficin
3-(((4-methyl-1-piperazinyl)imino)methyl)rifamycin sv
8-(((4-methyl-1-piperazinyl)imino)methyl)rifamycin sv
rimactazid
abrifam
5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-[n-(4-methyl-1-piperazinyl)formimidoyl]-, 21-acetate
rifadin i.v.
sinerdol
dione 21-acetate
rifam
rifampicine [french]
fenampicin
yl]-, (2s,12z,14e,16s,17s,18r,19r,20r,21s,22r,23s,24e)-
benemicin
2,7-(epoxypentadeca(1,11,13)trienimino)naphtho(2,1-b)furan-1,11(2h)-dione, 5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-(n-(4-methyl-1-piperazinyl)formimidoyl)-, 21-acetate (
8-[[(4-methyl-1-piperazinyl)imino[methyl]rifamycin
r-cin
eremfat
arzide
famcin
NCGC00022678-03
C06688
rifampicin, plant cell culture tested, bioreagent, >=97% (hplc), crystalline
DB01045
3-(4-methylpiperazinyliminomethyl)rifamycin sv
NCGC00022678-05
NCGC00022678-04
azt + rifampin
rifampicin, >=97% (hplc), powder
rifampicin, >=97.0% (hplc)
reserpine & rifampicin
piperine & rifampicin
(2s,14e,16s,17s,18r,19r,20r,21s,22r,23s,24e)-5,6,9,17,19-pentahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-{[(4-methylpiperazin-1-yl)imino]methyl}-1,11-dioxo-1,2-dihydro-2,7-(epoxypentadeca[1,11,13]trienoimino)naphtho[2,1-b]furan-21-yl acetate
HMS2089F12
HMS1569J11
NCGC00022678-06
HMS2096J11
rifampin [usan:usp]
vjt6j7r4tr ,
unii-vjt6j7r4tr
dtxcid301244
dtxsid6021244 ,
AKOS015951372
bdbm50370232
rifadin iv
rifapiam
ba 411661e
nih-10782
l-5103-lepetit
CHEMBL374478
rifampicinum [who-ip latin]
rifampicin [inn]
rifampicin [iarc]
rifampin [usp monograph]
rifampicin [who-dd]
rifampicin [mart.]
rifampin component of rifamate
rifamate component rifampin
rifampin component of rifater
rifampicin [ep impurity]
rifater component rifampin
rifampin [hsdb]
rifampin [orange book]
3-(((4-methyl-1-piperazinyl)imino)methyl)rifamycin
rifampicin [who-ip]
rifampin [mi]
5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-[n-(4-methyl-1-piperazinyl)formimidoyl]-2,7-(epoxypentadeca[1,11,13]trienimino)naphtho[2,1-b]furan-1,11(2h)-dione 21-acetate
ba-41166/e
rifampin [vandf]
rifamycin amp [mi]
rifampicin [ep monograph]
rifampicin [jan]
CCG-208267
GR-306
SCHEMBL23490
AB00383022_07
rifampin, united states pharmacopeia (usp) reference standard
rifampicin, vetranal(tm), analytical standard
SR-05000002118-3
sr-05000002118
rifampin, pharmaceutical secondary standard; certified reference material
rifampicin, european pharmacopoeia (ep) reference standard
rifampicin, powder, gamma-irradiated
HMS3713J11
[(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-[(e)-(4-methylpiperazin-1-yl)iminomethyl]-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.14,7.05,28]triaconta-1(29),2,4,9,19,21,25,27-o
(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,27,29-pentahydroxy-11- methoxy-3,7,12,14,16,18,22-heptamethyl-26-{(e)-[(4-methylpiperazin-1-yl)imino] methyl}-6,23-dioxo-8,30-dioxa-24-azatetracyclo[23.3.1.14,7.05,28]triaconta-1 (28),2,4,9,19,21,25(
rifampicin - cas 13292-46-1
rifampicin in combination with actinonin, bb-3497, hydroxylamine hydrochloride, and 1,10-phenanthroline
3-((4-methylpiperazin-1-yl)iminomethyl)rifamycin
rifampicinum (inn-latin)
rifampin (rifampicin)
(7s,9e,11s,12r,13s,14r,15r,16r,17s,18s,19e,21z)-2,15,17,27,29-pentahydroxy-11-methoxy-3,7,12,14,16,18,22-heptamethyl-26-((e)-((4-methylpiperazin-1-yl)imino)methyl)-6,23-dioxo-8,30-dioxa-24-azatetracyclo(23.3.1.1(4,7).0(5,28))triaconta-1(28),1(29),2,4,9,19
2,7-(epoxypentadeca(1,11,13)trienimino)naphtho(2,1-b)furan-1,11(2-h)-dione, 5,6,9,17,19,21-hexahydroxy-23-methoxy-2,4,12,1///
rifampicin (ep monograph)
rifampicin (mart.)
j04ab02
(2s,12z,14e,16s,17s,18r,19r,20r,21s,22r,23s,24e)-5,6,9,17,19-pentahydroxy-23-methoxy-2,4,12,16,18,20,22-heptamethyl-8-(4-methylpiperazin-1-yliminomethyl)-1,11-dioxo-1,2-dihydro-2,7-(epoxypentadeca(1,11,13)trienimino)naphtho(2,1-b)furan-21-yl acetate
rifampin (usan:usp)
rifampicin (ep impurity)
rifampicina (inn-spanish)
rifadin iv novaplus
rifampin (usp monograph)
rifampicin (iarc)
3-((4-methyl-1-piperazinyl)iminomethyl)rifamycin sv

Research Excerpts

Overview

Rifampin is a semisynthetic antibiotic which is known to alter hepatic cytochrome P-450 mediated drug metabolizing enzymes. It is an antibiotic with the ability to penetrate bacterial biofilms, and has been considered as a potentially important adjunct in the prevention and treatment of PJI.

ExcerptReference
"Rifampin is a semisynthetic antibiotic which is known to alter hepatic cytochrome P-450 mediated drug metabolizing enzymes. "( Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
Stohs, SJ; Wu, CL, 1983
)
"Rifampin is a key drug for tuberculosis (TB) treatment. "( Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
Aarnoutse, RE; Alisjahbana, B; Nijland, HM; Parwati, I; Ruslami, R; van Crevel, R, 2007
)
"Rifampin is a cornerstone of modern antituberculosis therapy. "( Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
Deziel, MR; Drusano, GL; Gumbo, T; Liu, W; Louie, A; Parsons, LM; Salfinger, M, 2007
)
"Rifampin is an antibiotic with the ability to penetrate bacterial biofilms, and thus has been considered as a potentially important adjunct in the prevention and treatment of PJI."( The Use of Rifampin in Total Joint Arthroplasty: A Systematic Review and Meta-Analysis of Comparative Studies.
Chaudhry, H; Ekhtiari, S; Kandel, CE; Kruse, CC; Mundi, R; Oral, I; Pincus, D; Selznick, A; Wolfstadt, J, 2022
)
"Rifampin is an antituberculosis drug that is a potent inducer of cytochrome P450 3 subfamily A member 4, which is involved in an alternative catabolic pathway of vitamin D."( Long-term Efficacy and Safety of Rifampin in the Treatment of a Patient Carrying a CYP24A1 Loss-of-Function Variant.
Baldinotti, F; Borsari, S; Brancatella, A; Caligo, MA; Cappellani, D; Cetani, F; Jones, G; Kaufmann, M; Marcocci, C; Sardella, C; Semeraro, A, 2022
)
"Rifampin (RIF) is a first-line antimicrobial agent with potent bactericidal action."( Angiopep-2 Modified Exosomes Load Rifampicin with Potential for Treating Central Nervous System Tuberculosis.
An, Y; Chen, R; Chen, W; Ding, Y; Hu, C; Huang, J; Li, H; Tang, Q; Zhao, Y, 2023
)
"Rifampin is a known strong CYP3A4 inducer and is recommended by the FDA as a positive control in the CYP3A4 induction assay."( Alflutinib (AST2818), primarily metabolized by CYP3A4, is a potent CYP3A4 inducer.
Chen, ZD; Diao, XX; Guo, ZT; Jiang, Y; Liu, XY; Zhang, YF; Zhao, QY; Zhong, DF; Zhou, JL, 2020
)
"Rifampin (RIF) is an important first-line anti-TB drug, and rifampin resistance (RIF-R) is a key factor in formulating treatment regimen and evaluating the prognosis of TB."( Mechanisms and detection methods of Mycobacterium tuberculosis rifampicin resistance: The phenomenon of drug resistance is complex.
Jia, X; Liu, H; Wang, X; Xu, G; Xu, P, 2021
)
"Rifampin is a strong inducer of several drug-metabolizing enzymes, including CYP3A."( Oxycodone Resistance Due to Rifampin Use in an Osteosarcoma Patient with Tuberculosis.
Hori, Y; Matsuda, S; Okamoto, T; Sakamoto, A; Shimizu, A; Yamashita, M, 2017
)
"Rifampin (RIF) is a bactericidal antibiotic drug and potent inducer of hepatic and intestinal cytochrome P-450 (CYP-450) enzyme systems. "( Encapsulation of rifampin in a polymeric layer-by-layer structure for drug delivery.
Esmaeili, A; Khodaei, M, 2018
)
"Rifampin is a pleiotropic inducer of multiple drug metabolizing enzymes and transporters. "( Rifampin modulation of xeno- and endobiotic conjugating enzyme mRNA expression and associated microRNAs in human hepatocytes.
Desta, Z; Eadon, MT; Gao, H; Gufford, BT; Lin, H; Liu, Y; Robarge, JD; Skaar, TC, 2018
)
"Rifampin is an effective eradicator of Staphylococcal biofilms."( Topical rifampin powder for orthopedic trauma part I: Rifampin powder reduces recalcitrant infection in a delayed treatment musculoskeletal trauma model.
Shiels, SM; Tennent, DJ; Wenke, JC, 2018
)
"Rifampin is a powerful antibiotic used in the treatment of biofilm-forming bacteria with studies supporting its use in PMMA cement. "( Rifampin and tobramycin combination with PMMA antibiotic cement.
Likine, EF; Seligson, D, 2019
)
"Rifampin resistance is a critical concern for tuberculosis treatment."( Evolution of Rifampin Resistance in Escherichia coli and Mycobacterium smegmatis Due to Substandard Drugs.
Weinstein, ZB; Zaman, MH, 2019
)
"Rifampin is a bactericidal antibiotic drug of the rifamycin group. "( Stability of rifampin in SyrSpend SF.
Sorenson, B; Whaley, P,
)
"Rifampin is a potent inducer of cytochrome P450 (CYP) enzymes and transporters. "( Induction of influx and efflux transporters and cytochrome P450 3A4 in primary human hepatocytes by rifampin, rifabutin, and rifapentine.
Back, DJ; Dooley, KE; Owen, A; Williamson, B; Zhang, Y, 2013
)
"Rifampin is an important drug used in the treatment of tuberculosis, and it increases the drug metabolism in human hepatocytes. "( Integrative network analysis of rifampin-regulated miRNAs and their functions in human hepatocytes.
Cong, W; Feng, W; Li, J; Liang, H; Liu, Y; Meng, X; Wang, L; Wang, Y, 2015
)
"Rifampin is a key sterilizing drug in the treatment of tuberculosis (TB). "( Model-Based Evaluation of Higher Doses of Rifampin Using a Semimechanistic Model Incorporating Autoinduction and Saturation of Hepatic Extraction.
Chirehwa, MT; Denti, P; McIlleron, H; Mthiyane, T; Onyebujoh, P; Rustomjee, R; Smith, P, 2016
)
"Rifampin (RIF) is a first-line drug used for the treatment of tuberculosis and other bacterial infections. "( Structural basis of rifampin inactivation by rifampin phosphotransferase.
Gao, J; He, N; He, Y; Lin, W; Ma, M; Qi, X; Wang, C; Wang, Y; Xiao, Y; Zhang, P; Zhou, H, 2016
)
"Rifampin resistance is a key prognostic marker for treatment success in tuberculosis patients. "( Rifampin resistance, Beijing-W clade-single nucleotide polymorphism cluster group 2 phylogeny, and the Rv2629 191-C allele in Mycobacterium tuberculosis strains.
Aladegbami, B; Alland, D; Brimacombe, M; Chakravorty, S; Dai, Y; Helb, D; Motiwala, AS; Safi, H, 2008
)
"Rifampin is a first line antituberculosis drug active against bacilli in logarithmic and stationary phase, which interferes with RNA synthesis by binding to bacterial RNA polymerase. "( Genetic evaluation of relationship between mutations in rpoB and resistance of Mycobacterium tuberculosis to rifampin.
Augustynowicz-Kopec, E; Brzostek, A; Dziadek, J; Zaczek, A; Zwolska, Z, 2009
)
"Rifampin is a key drug in antituberculosis chemotherapy because it rapidly kills the majority of bacilli in tuberculosis lesions, prevents relapse and thus enables 6-month short-course chemotherapy. "( Rifampin pharmacokinetics in children, with and without human immunodeficiency virus infection, hospitalized for the management of severe forms of tuberculosis.
Cilliers, K; Donald, PR; Hussey, GD; Labadarios, D; Maritz, JS; McIlleron, H; Schaaf, HS; Smith, P; Willemse, M, 2009
)
"Rifampin is a strong inducer of several drug-metabolizing enzymes."( Rifampin greatly reduces the plasma concentrations of intravenous and oral oxycodone.
Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Nieminen, TH; Olkkola, KT; Pertovaara, A; Saari, TI, 2009
)
"Rifampin is a key component of standard short-course first-line therapy against Mycobacterium tuberculosis (MTB). "( A mutation in Mycobacterium tuberculosis rpoB gene confers rifampin resistance in three HIV-TB cases.
Cook, VJ; Elwood, K; Malhotra, S; Sharma, MK; Tang, P; Wolfe, JN, 2010
)
"Rifampin is a potent inhibitor of RNA polymerase (RNAP) in vivo but has been shown to be less effective against stationary-phase bacteria."( Sigma factor F does not prevent rifampin inhibition of RNA polymerase or cause rifampin tolerance in Mycobacterium tuberculosis.
Chen, JM; Cole, ST; Hartkoorn, RC; Magnet, SJ; Pojer, F; Sala, C, 2010
)
"Rifampin is a mainstay of therapy."( The combination of rifampin plus moxifloxacin is synergistic for suppression of resistance but antagonistic for cell kill of Mycobacterium tuberculosis as determined in a hollow-fiber infection model.
Brown, DL; Drusano, GL; Eichas, A; Kulawy, R; Louie, A; Sgambati, N, 2010
)
"Rifampin is a more potent inducer of buprenorphine metabolism than rifabutin with pharmacokinetic and pharmacodynamic adverse consequences. "( Rifampin, but not rifabutin, may produce opiate withdrawal in buprenorphine-maintained patients.
Friedland, G; McCance-Katz, EF; Moody, DE; Prathikanti, S; Rainey, PM, 2011
)
"Rifampin is a substrate of P-glycoprotein (coded for by the ABCB1 gene) and organic anion-transporting polypeptide 1B1 (coded for by SLCO1B1)."( The SLCO1B1 rs4149032 polymorphism is highly prevalent in South Africans and is associated with reduced rifampin concentrations: dosing implications.
Chigutsa, E; Denti, P; Egan, D; Holford, NH; Maartens, G; McIlleron, H; Owen, A; Pushpakom, S; Smith, PJ; Swart, EC; Visser, ME, 2011
)
"Rifampin is a potent inducer of CYP3A4 in vitro and precipitates numerous drug-drug interactions (DDIs) when coadministered with CYP3A4 substrates. "( Predictive utility of in vitro rifampin induction data generated in fresh and cryopreserved human hepatocytes, Fa2N-4, and HepaRG cells.
Galetin, A; Houston, JB; Templeton, IE, 2011
)
"Rifampin is a major drug used to treat leprosy and tuberculosis. "( Mutation analysis of mycobacterial rpoB genes and rifampin resistance using recombinant Mycobacterium smegmatis.
Kai, M; Makino, M; Nakata, N, 2012
)
"Rifampin (RIF) is a standard part of TB treatment but is a potent inducer of drug metabolizing enzymes."( Safety, tolerability, and pharmacokinetics of the HIV integrase inhibitor dolutegravir given twice daily with rifampin or once daily with rifabutin: results of a phase 1 study among healthy subjects.
Borland, J; Chen, S; Dooley, KE; Everts, S; Flexner, C; Peppercorn, A; Piscitelli, S; Purdy, E; Sayre, P; Song, I, 2013
)
"Rifampin is a potent inducer of both cytochrome P-450 oxidative enzymes and the P-glycoprotein transport system. "( Update on rifampin, rifabutin, and rifapentine drug interactions.
Baciewicz, AM; Chrisman, CR; Finch, CK; Self, TH, 2013
)
"Rifampin is a key component of standard short-course first-line therapy against Mycobacterium tuberculosis, and rifampin resistance of this pathogen has been reported to be related to rpoB gene mutations. "( Characterization of rifampin-resistant isolates of Mycobacterium tuberculosis from Sichuan in China.
Feng, Q; Guo, J; He, Y; Li, Y; Luo, M; Sun, H; Sun, Q; Tang, K; Zhang, C; Zhao, Y, 2013
)
"Rifampin is a cornerstone of the treatment of staphylococcal osteoarticular infections, particularly those of implanted material."( Optimizing combination rifampin therapy for staphylococcal osteoarticular infections.
Albert, JD; Arvieux, C; Coiffier, G; Guggenbuhl, P, 2013
)
"Rifampin is a front-line antibiotic for the treatment of tuberculosis. "( A rifampin-hypersensitive mutant reveals differences between strains of Mycobacterium smegmatis and presence of a novel transposon, IS1623.
Alexander, DC; Jones, JR; Liu, J, 2003
)
"Rifampin is an important drug in the treatment of tuberculosis, but administration of rifampin in combination with protease inhibitors is complicated because of drug-drug interactions. "( Pharmacokinetic interaction between rifampin and the combination of indinavir and low-dose ritonavir in HIV-infected patients.
Andersen, AB; Brøsen, K; Gerstoft, J; Justesen, US; Klitgaard, NA; Pedersen, C, 2004
)
"Rifampin is a more effective therapy in combination with other antibiotics for treatment of this kind of infections."( [Effectiveness of the antibiotics chloramphenicol and rifampin in the treatment of Streptococcus pneumoniae-induced meningitis and systemic infections].
Hernández, M; Mejía, GI; Robledo, J; Trujillo, H, 2003
)
"Rifampin is a major drug used in the treatment of tuberculosis infections, and increasing rifampin resistance represents a worldwide clinical problem. "( Effect of rpoB mutations conferring rifampin resistance on fitness of Mycobacterium tuberculosis.
Andersson, DI; Hoffner, SE; Mariam, DH; Mengistu, Y, 2004
)
"Rifampin is a bactericidal antibiotic that acts both on extra- and intracellular bacilli. "( Activity of rifampin against Mycobacterium tuberculosis in a reference center.
Casal, M; Gutierrez, J; Rodríguez-Cano, F; Ruiz, P; Zerolo, FJ, 2004
)
"Rifampin appears to be an agent for preventing peri-implant capsule formation."( Influence of rifampin on capsule formation around silicone implants in a rat model.
Can, B; Orbay, H; Sensoz, O; Tekdemir, I; Unlu, RE; Yilmaz, AD,
)
"Rifampin is a potent inducer of cytochrome P-450 oxidative enzymes as well as the P-glycoprotein transport system. "( Update on rifampin and rifabutin drug interactions.
Baciewicz, AM; Chrisman, CR; Finch, CK; Self, TH, 2008
)
"Rifampin has proved to be a valuable antibiotic with relatively few major adverse effects. "( Adverse effects of rifampin.
Grosset, J; Leventis, S,
)
"Rifampin appears to be a uniquely effective antibiotic for the treatment of certain infections. "( The antimicrobial activity of rifampin: emphasis on the relation to phagocytes.
Mandell, GL,
)
"Rifampin is a potentially useful anti-staphylococcal agent, but resistance develops frequently when the drug is used alone. "( Treatment of experimental staphylococcal infections: effect of rifampin alone and in combination on development of rifampin resistance.
Mandell, GL; Moorman, DR, 1980
)
"Rifampin is an enzymatic inducer known to increase steroid metabolism. "( Rifampin-induced nonresponsiveness of giant cell arteritis to prednisone treatment.
Becq-Giraudon, B; Bouquet, S; Carrie, F; Delon, A; Roblot, F; Roblot, P, 1994
)
"Rifampin is a potent enzyme inducer that may seriously interact with some substrates of CYP3A4."( Rifampin drastically reduces plasma concentrations and effects of oral midazolam.
Backman, JT; Neuvonen, PJ; Olkkola, KT, 1996
)
"Rifampin (rifampicin) is a potent inducer of CYP3A4 and it is known to markedly reduce plasma concentrations and effects of drugs such as midazolam."( Triazolam is ineffective in patients taking rifampin.
Backman, JT; Kivistö, KT; Neuvonen, PJ; Olkkola, KT; Villikka, K, 1997
)
"Rifampin is a drug able to induce adverse reactions involving both the kidney and the hematological system. "( Adverse drug reaction to rifampin: a case with long lasting antiplatelet antibodies.
Addario, C; Bartoloni, C; Gentiloni Silveri, N; Guidi, L; Magalini, S; Tricerri, A; Vangeli, M, 1997
)
"Rifampin therapy is an infrequently reported cause of pseudomembranous colitis. "( Delayed onset of pseudomembranous colitis after rifampin therapy.
Byrd, RP; Fields, CL; Ossorio, MA; Roy, TM, 1997
)
"Rifampin is a potent inducer of cytochrome P-450 oxidative enzymes. "( Update on rifampin drug interactions, III.
Baciewicz, AM; Self, TH; Strayhorn, VA, 1997
)
"Rifampin is a potent inducer of losartan and E3174 elimination. "( Effects of erythromycin or rifampin on losartan pharmacokinetics in healthy volunteers.
Adams, KF; McQueen, RH; Patterson, JH; Pieper, JA; Williamson, KM, 1998
)
"Rifampin is a useful drug for several types of bacterial infections because of its broad spectrum of activity, excellent tissue penetration, and low side effect profile."( Rifampin, a useful drug for nonmycobacterial infections.
Pien, BC; Pien, FD; Vesely, JJ,
)
"Rifampin is a key component of therapeutic regimens for tuberculosis control, and a marker for multidrug resistance of Mycobacterium tuberculosis. "( Dideoxy fingerprinting for rapid screening of rpoB gene mutations in clinical isolates of Mycobacterium tuberculosis.
Chen, CS; Huang, TS; Huang, WK; Liu, YC; Tu, HZ, 1998
)
"Rifampin is a first-line drug useful in the treatment of tuberculosis. "( Efficacy of microencapsulated rifampin in Mycobacterium tuberculosis-infected mice.
Barrow, EL; Barrow, WW; Quenelle, DC; Staas, JK; Winchester, GA, 1999
)
"Rifampin is a potent inducer of hepatic enzymes and is well documented to cause many clinically significant drug interactions. "( Interaction between rifampin and levothyroxine.
Nolan, SR; Norwood, JM; Self, TH, 1999
)
"Rifampin (rifampicin) is a potent inducer of several cytochrome P450 (CYP) enzymes, including CYP3A4. "( Rifampin greatly reduces plasma simvastatin and simvastatin acid concentrations.
Backman, JT; Kivistö, KT; Kyrklund, C; Laitila, J; Neuvonen, M; Neuvonen, PJ, 2000
)
"Rifampin is a potent inducer of cytochrome P-450 oxidative enzymes. "( Rifampin and rifabutin drug interactions: an update.
Baciewicz, AM; Chrisman, CR; Finch, CK; Self, TH, 2002
)
"Rifampin is a drug used in the treatment of tuberculosis. "( Rifampin, oral contraceptives, and pregnancy.
Anderson, WH; Katz, DB; Skolnick, JL; Stoler, BS, 1976
)
"Rifampin is a new drug that is well tolerated and efficacious, although expensive."( An evaluation of the current therapeutic regimen for renal tuberculosis.
Lattimer, JK; Wechsler, M, 1975
)
"Rifampin is a potent inducer of hepatic P450 oxidative enzymes. "( Update on rifampin drug interactions. II.
Baciewicz, AM; Borcherding, SM; Self, TH, 1992
)
"Rifampin appears to be a safe drug in the management of the pruritus of primary biliary cirrhosis."( Treatment of pruritus of primary biliary cirrhosis with rifampin.
Companc, JP; Flores, D; Lopez, P; Mastai, R; Podesta, A; Terg, R; Udaondo, CB; Villamil, F, 1991
)
"Rifampin is an antimicrobial agent recently found to exhibit immunosuppressive activity in both animal and human studies."( Rifampin therapy in rheumatoid arthritis.
Conn, DL; Gabriel, SE; Luthra, H, 1990
)
"Rifampin is known to be an important stimulus to drug-metabolizing enzymes and can also induce the production of alpha 1-acid glycoprotein (AGP). "( The kinetics of induction by rifampin of alpha 1-acid glycoprotein and antipyrine clearance in the dog.
Abramson, FP; Lutz, MP,
)
"Rifampin is a widely used antimicrobial agent, most commonly administered in the treatment of tuberculosis. "( Acute interstitial nephritis associated with intermittent rifampin use.
Katz, MD; Lor, E, 1986
)
"Rifampin is a potent antituberculous drug. "( Rifampin.
Dorken, E; Grzybowski, S; Schonell, M, 1972
)
"Rifampin is a newer semi-synthetic derivative of rifamycin. "( Rifampin in the treatment of pulmonary tuberculosis.
Hyde, L, 1972
)

Effects

Rifampin has a higher affinity for TL (Kd=128 microM) than albumin. It reduces the serum concentrations of immunosuppressive agents.

Rifampin (RIF) has been widely used for the treatment of bacterial infections, including tuberculosis (TB) It has been shown to eradicate mature Staphylococcal biofilms and its use proven for treating musculoskeletal infections.

ExcerptReference
"Rifampin has a higher affinity for TL (Kd=128 microM) than albumin."( Tear lipocalin: potential for selective delivery of rifampin.
Abduragimov, AR; Dooley, AN; Gasimov, EO; Gasymov, OK; Glasgow, BJ; Yusifov, TN, 2004
)
"Rifampin has a potent sterilizing activity, but it reduces the serum concentrations of the immunosuppressive agents."( Clinical outcomes of tuberculosis in renal transplant recipients.
Chang, KH; Cho, CH; Choi, JY; Kim, JM; Kim, YS; Park, YS; Song, YG, 2004
)
"Rifampin has a broad antibacterial spectrum. "( Rifampin therapy for brucellosis, flavobacterium meningitis, and cutaneous leishmaniasis.
Conti, R; Parenti, F,
)
"Rifampin, which has an incomplete action in a neutral control environment, was used as a sensitive indicator of possible synergistic or antagonistic interaction of the biofilm bacteria with the dialysis environments."( Impact of dialysis fluid on the susceptibility of Staphylococcus epidermidis biofilms to rifampin.
Gagnon, RF; Kostiner, GB; Morcos, R; Richards, GK, 1993
)
"Rifampin (RIF) has been reported to cause haemolysis due to the production of drug-dependent antibodies, and haemolysis results in an increased level of free haem, which affects the function of hepatocytes."( Association of ABO blood group and antituberculosis drug-induced liver injury: A case-control study from a Chinese Han population.
Chen, H; Liu, W; Pan, H; Tang, S; Tao, B; Yang, M; Yi, H, 2020
)
"Rifampin has been shown to eradicate mature Staphylococcal biofilms and its use proven for treating musculoskeletal infections."( Topical rifampin powder for orthopaedic trauma part II: Topical rifampin allows for spontaneous bone healing in sterile and contaminated wounds.
Lofgren, AL; Shiels, SM; Tennent, DJ; Wenke, JC, 2018
)
"Rifampin has been used as an agent in combination therapy in orthopedic device-related infections (ODRI) for almost three decades. "( Role of Rifampin against Staphylococcal Biofilm Infections
Sendi, P; Zimmerli, W, 2019
)
"Rifampin (RIF) has been widely used for the treatment of bacterial infections, including tuberculosis (TB). "( Rifampin Induces Expression of P-glycoprotein on the THP1 Cell-Derived Macrophages, Causing Decrease Intramacrophage Concentration of Prothionamide.
Cho, M; Hasanuzzaman, M; Lee, SJ; Parvez, MM; Shin, JG; Yi, M, 2019
)
"Rifampin has been used for the treatment of bacterial infections for many years. "( Rifampin inhibits Toll-like receptor 4 signaling by targeting myeloid differentiation protein 2 and attenuates neuropathic pain.
Cheng, K; Grace, PM; Li, J; Pham, MN; Smith, C; Strand, KA; Wang, X; Watkins, LR; Yin, H, 2013
)
"Rifampin has been shown to be one of the most active antimicrobial agents in the eradication of the staphylococcal biofilm."( Antimicrobial activity of tigecycline alone or in combination with rifampin against Staphylococcus epidermidis in biofilm.
Kaznowski, A; Szczuka, E, 2014
)
"Rifampin has been a cornerstone of tuberculosis (TB) treatment since its introduction. "( Novel Chemical Scaffolds for Inhibition of Rifamycin-Resistant RNA Polymerase Discovered from High-Throughput Screening.
Garcia, GA; Kontos, A; Molodtsov, V; Murakami, KS; Scharf, NT, 2017
)
"Rifampin has been shown to impair both humoral and cell-mediated immune responses in animal models. "( Immunological responsiveness of tuberculosis patients receiving rifampin.
Fotiadis, IG; Ruben, FL; Winkelstein, A, 1974
)
"Rifampin has been studied as prophylaxis against Staphylococcus aureus-related infections in patients on dialysis."( Oral rifampin for prevention of S. aureus carriage-related infections in patients with renal failure--a meta-analysis of randomized controlled trials.
Bliziotis, IA; Falagas, ME; Fragoulis, KN, 2006
)
"Rifampin has been used for the eradication of Staphylococcus aureus (S. "( Oral rifampin for eradication of Staphylococcus aureus carriage from healthy and sick populations: a systematic review of the evidence from comparative trials.
Bliziotis, IA; Falagas, ME; Fragoulis, KN, 2007
)
"Rifampin has been used against bacterial and occasionally protozoal infections."( Rifampin therapy for brucellosis, flavobacterium meningitis, and cutaneous leishmaniasis.
Conti, R; Parenti, F,
)
"Rifampin has been effective in combination therapy for serious staphylococcal and enterococcal infections."( Activity of rifampin against viridans streptococci.
Phillips, EK; Stamm, AM, 1983
)
"Rifampin has been reported to cause acute pancreatitis in up to 2.7% of patients."( Pancreatic insufficiency due to antituberculous therapy.
Cohen, LB; Knowles, SR; Liu, BA; Shear, NH; Werb, MR, 1997
)
"Rifampin has been proposed to reduce pruritus in children and adults with chronic cholestasis; however, there is a paucity of published data regarding the use of rifampin in children."( Use of rifampin for severe pruritus in children with chronic cholestasis.
Karrer, FM; Narkewicz, MR; Smith, D; Sokol, RJ; Yerushalmi, B, 1999
)
"Rifampin has been reported to increase the warfarin requirements in human subjects ingesting these agents simultaneously."( Rifampin and warfarin: a drug interaction.
Ehrman, M; Romankiewicz, JA, 1975
)
"Rifampin has been noted to exhibit exceptional antimicrobial activity against Staphylococcus epidermidis biofilms as compared to commonly used antibiotics. "( The activity of rifampin and analogs against Staphylococcus epidermidis biofilms in a CAPD environment model.
Gagnon, RF; Harris, A; Obst, G; Prentis, J; Richards, GK, 1989
)
"New rifampin interactions have been described for cyclosporine, ketoconazole, chloramphenicol, beta-blockers, verapamil, and phenytoin."( Update on rifampin drug interactions.
Baciewicz, AM; Bekemeyer, WB; Self, TH, 1987
)
"Rifampin has been shown to induce the immunosuppressive effect in animal models due to the inhibition of protein synthesis by cells involved in the immune process."( Rifampin therapy in Henoch-Schönlein purpura nephritis accompanied by nephrotic syndrome.
Choi, IJ; Jeong, HJ; Kim, KS; Kim, PK; Lee, JK; Lee, JS,
)
"Rifampin has been advocated as a concurrent second antibiotic because of its extraordinary potent bactericidal activity for Staphylococcus aureus."( Rifampin resistance. Development during the therapy of methicillin-resistant Staphylococcus aureus infection.
Cherubin, C; Eng, RH; Smith, SM; Tillem, M, 1985
)
"Rifampin has been studied in 68 patients and results can be summarized as follows:* There has been no evidence of significant toxicity.* In a randomized study of active tuberculosis patients who had not received prior chemotherapy, isoniazid-rifampin and isoniazid-aminosalicylic acid regiments were equally effective.* In retreatment patients with active, positive tuberculosis, the regimen of isoniazid, rifampin, and ethambutol proved to be very effective, especially when the two latter drugs had not been used previously.* In patients with pulmonary infections caused by atypical acid-fast bacilli, results varied with the organism isolated and the extent of disease."( Rifampin in the treatment of pulmonary tuberculosis.
Hyde, L, 1972
)

Actions

Rifampin can cause rapid metabolization and reduction in plasma levels of both prednisone and doxycycline and should be avoided with combined therapy. Rifampsin showed an increase in the biofilm density and number of viable bacteria at 24 h.

ExcerptReference
"Rifampin can cause rapid metabolization and reduction in plasma levels of both prednisone and doxycycline and should be avoided with combined therapy."( Case Report: Treatment of Severe Neuroretinitis and other Sequelae Associated with Cat Scratch Disease.
Whorff, J, 2022
)
"Rifampin showed an increase in the biofilm density and the number of viable bacteria at 24 h."( Antibacterial effect of antibiotic-loaded SBA-15 on biofilm formation by Staphylococcus aureus and Staphylococcus epidermidis.
Aguilar-Colomer, A; Doadrio, JC; Esteban, J; Manzano, M; Pérez-Jorge, C; Vallet-Regí, M, 2017
)
"Rifampin did not increase the formation of DNA adducts induced by isoniazid."( Effects of rifampin on CYP2E1-dependent hepatotoxicity of isoniazid in rats.
Chen, J; Dong, G; Liu, Y; Peng, R; Yue, J, 2009
)
"Rifampin was found to increase the values of clearance/bioavailability (CL/F) and volume of distribution/ bioavailability (V/F) by approximately 70%."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
"Oral rifampin may cause esophagitis. "( Pill-induced esophagitis caused by oral rifampin.
Chow, AW; Lee, AJ; Maddix, DS; Smith, SJ, 1999
)
"Rifampin is known to lower plasma warfarin concentrations by increasing the rate of warfarin clearance. "( Complex interaction of rifampin and warfarin.
Almog, S; Bank, HZ; Farfel, Z; Halkin, H; Martinowitz, U, 1988
)
"Rifampin produced lower concentrations in both prostatic interstitial fluid and prostatic secretion than in plasma, while trimethoprim concentrations were much higher in prostatic secretion and prostatic interstitial fluid than in plasma."( Rifampin and trimethoprim distribution in normal and hydronephrotic kidney and in prostate: an experimental study in dogs.
Frimodt-Møller, N; Maigaard, S, 1987
)
"Rifampin appears to produce some inhibition of acetylation of the metabolite acetylhydrazine to diacetylhydrazine."( Effect of rifampin, phenobarbital pretreatment, and acetylator phenotype on acetylisoniazid metabolism in the rabbit.
Thomas, BH; Whitehouse, LW; Zeitz, W, 1987
)
"Rifampin does not inhibit phage release from mutant cells possessing a rifampin-resistant deoxyribonucleic acid-dependent RNA polymerase."( Ribonucleic acid bacteriophage release: requirement for host-controlled protein synthesis.
Engelberg, H; Soudry, E, 1971
)
"Rifampin inhibits the increase in content of this coat antigen."( Development of a quantitative immunological assay for the study of spore coat synthesis and morphogenesis.
Aronson, AI; Golub, ES; Horn, D, 1973
)
"Rifampin failed to inhibit adenovirus replication in tissue culture. "( Failure of rifampin to inhibit adenovirus replication.
Beam, WE; McCormick, DP; Smith, EP; Wenzel, RP, 1972
)

Treatment

Treatment with rifampin resulted in a 70% increase (p = 0.008) of the serum concentration of the bile acid precursor 7alpha-hydroxy-4-cholesten-3-one. Treatment with streptomycin for 4 weeks or more inhibited growth of M. ulcerans.

ExcerptReference
"Rifampin treatment increased intestinal P-gp content 3.5 +/- 2.1-fold, which correlated with the AUC after oral digoxin but not after intravenous digoxin."( The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin.
Eichelbaum, M; Fritz, P; Greiner, B; Kreichgauer, HP; Kroemer, HK; von Richter, O; Zundler, J, 1999
)
"Rifampin treatment also affected the transcription factors that regulate iNOS mRNA: there was an increased and prolonged degradation of the inhibitory subunit of NF-kappaB, a corresponding increase in the level of cytokine-induced DNA binding of NF-kappaB (2.1 +/- 0.2-fold), and a decrease in the level of expression of peroxisome proliferator-activated receptor gamma (PPARgamma)."( Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
Ashkenazi, S; Berent, E; Cohen, R; Yuhas, Y, 2009
)
"Rifampin pretreatment was employed to increase persister formation, and the resulting cells were exposed to a high concentration of ampicillin (10× MIC) to remove nonpersisters."( Specific Enrichment and Proteomics Analysis of Escherichia coli Persisters from Rifampin Pretreatment.
Hao, C; Lam, H; Sulaiman, JE, 2018
)
"Rifampin-based treatment was less likely to be used in patients with prior rejection (P= .04)."( Tuberculosis in solid-organ transplant recipients: disease characteristics and outcomes in the current era.
Aguado, JM; Bouza, E; Bruno, D; Garcia-Reyne, A; John, GT; Lara, R; Lattes, R; Montejo, M; Munoz, P; Singh, N; Sun, HY; Torre-Cisneros, J; Valerio, M; Wagener, MM, 2014
)
"Rifampin treatment induced systemic CYP3A metabolism of (11)C-verapamil; however, it reduced the ER by 6%."( Modulation of P-glycoprotein at the Human Blood-Brain Barrier by Quinidine or Rifampin Treatment: A Positron Emission Tomography Imaging Study.
Collier, AC; Deo, AK; Domino, KB; Eary, JF; Hsiao, P; Link, JM; Liu, L; Mankoff, DA; Spiekerman, CF; Unadkat, JD, 2015
)
"Rifampin treatment was defined as 3 or more days of rifampin postoperatively."( Rifampin for Surgically Treated Staphylococcal Infective Endocarditis: A Propensity Score-Adjusted Cohort Study.
Gordon, SM; Hussain, ST; Nowacki, AS; Pettersson, GB; Shah, SY; Shrestha, NK; Wang, H, 2016
)
"Rifampin treatment substantially increased the Cmax and AUC0-12h of 8-hydroxyefavirenz and 8,14-dihydroxyefavirenz, metabolic ratio (AUC0-72h of metabolites to AUC0-72h efavirenz) and the amount of metabolites excreted in urine (Ae0-12hr) (all, p < 0.01)."( Rifampin enhances cytochrome P450 (CYP) 2B6-mediated efavirenz 8-hydroxylation in healthy volunteers.
Blievernicht, J; Cho, DY; Desta, Z; Flockhart, DA; Kim, KB; Lemler, SM; Li, L; Shen, JH; Shin, JG; Skaar, TC; Zanger, UM, 2016
)
"The rifampin-treated group also had reduced morbidity and neurologic sequelae; however, these were not statistically significant."( Role of Rifampin in Reducing Inflammation and Neuronal Damage in Childhood Bacterial Meningitis: A Pilot Randomized Controlled Trial.
Aggarwal, R; Singhi, P; Singhi, S; Uppal, L, 2017
)
"Oral rifampin-cotrimoxazole treatment showed outcomes comparable to those for intravenous cloxacillin treatment."( Long-term follow-up trial of oral rifampin-cotrimoxazole combination versus intravenous cloxacillin in treatment of chronic staphylococcal osteomyelitis.
Ariza, J; Cabo, J; Euba, G; Fernández-Sabé, N; Gudiol, F; Mascaró, J; Murillo, O; Pérez, A; Tubau, F; Verdaguer, R, 2009
)
"Rifampin-treated BALB/c mice remained culture positive at 3 months."( Treatment of tuberculosis with rifamycin-containing regimens in immune-deficient mice.
Ahmad, Z; Almeida, DV; Converse, PJ; Grosset, JH; Li, SY; Nuermberger, EL; Peloquin, CA; Rosenthal, IM; Zhang, M, 2011
)
"Rifampin-pretreated A549 cells demonstrated decreases in apoptosis and cell death induced by A. "( Rifampin protects human lung epithelial cells against cytotoxicity induced by clinical multi and pandrug-resistant Acinetobacter baumannii.
Domínguez-Herrera, J; Pachón, J; Smani, Y, 2011
)
"rifampin. She was treated with a total of 36 days of intraventricular colistin, 40 days of intraventricular tobramycin, 51 days of i.v."( Prolonged triple therapy for persistent multidrug-resistant Acinetobacter baumannii ventriculitis.
Pacheco, SM; Patel, JA; Postelnick, M; Sutton, S, 2011
)
"With rifampin treatment, the median ERMBT(IV) result and CL/F increased 2-fold (P < or =.01), but the median ERMBT(oral) result was unchanged (P =.30)."( Cytochrome P450 3A4 and P-glycoprotein mediate the interaction between an oral erythromycin breath test and rifampin.
Hoffmaster, KA; Paine, MF; Wagner, DA; Watkins, PB, 2002
)
"Rifampin pretreatment markedly increased the systemic (two-fold) and oral clearance (16-fold) of midazolam, and the ERBT (two-fold) but the variabilities were unchanged."( Genotype-phenotype associations for common CYP3A4 and CYP3A5 variants in the basal and induced metabolism of midazolam in European- and African-American men and women.
Bhat, K; Floyd, MD; George, AL; Gervasini, G; Kim, RB; Masica, AL; Mayo, G; Wilkinson, GR, 2003
)
"Rifampin treatment increased the apparent clearance of bupropion in Chinese subjects and white subjects combined (n = 16) from 2.6 L x h(-1) x kg(-1) (95% confidence interval [CI], 2.3-3.0 L x h(-1) x kg(-1)) after bupropion alone to 7.9 L x h(-1) x kg(-1) (95% CI, 6.8-10.1 L x h(-1) x kg(-1)) during rifampin treatment. "( Cytochrome P450 2B6 activity as measured by bupropion hydroxylation: effect of induction by rifampin and ethnicity.
Blievernicht, JK; Day, RO; Gross, AS; Liauw, WS; Loboz, KK; McLachlan, AJ; Williams, KM; Zanger, UM, 2006
)
"Rifampin treatment markedly increased pregnane X receptor protein in the wild-type pregnane X receptor-transfected cells as shown by coimmunoprecipitation but not in Q158K pregnane X receptor-transfected cells."( Pregnane X receptor polymorphism affects CYP3A4 induction via a ligand-dependent interaction with steroid receptor coactivator-1.
Huang, JD; Lim, YP, 2007
)
"Rifampin pretreatment produced only one significant change in the parameters studied and that was a reduction in AcINH excreted in urine."( Isoniazid metabolism in the rabbit, and the effect of rifampin pretreatment.
Solomonraj, G; Thomas, BH; Wong, LT; Zeitz, W, 1981
)
"When rifampin-prednisone treatment must be used in giant cell arteritis, we propose increasing the prednisone dosage to 2 mg/kg per day."( Rifampin-induced nonresponsiveness of giant cell arteritis to prednisone treatment.
Becq-Giraudon, B; Bouquet, S; Carrie, F; Delon, A; Roblot, F; Roblot, P, 1994
)
"Rifampin treatment significantly increased the oral clearance of each drug from 1.4-fold (valproic acid) to 3.4-fold (quinidine)."( Use of single sample clearance estimates of cytochrome P450 substrates to characterize human hepatic CYP status in vivo.
Bachmann, KA; Jauregui, L, 1993
)
"Rifampin pretreatment decreased the area under the plasma midazolam concentration-time curve by 96% (i.e., from 10.2 +/- 0.8 to 0.42 +/- 0.05 micrograms.min/ml [mean +/- SEM; p < 0.001]) and the maximum concentration by 94% (i.e., from 55 +/- 4 to 3.5 +/- 0.7 ng/ml [p < 0.001]). "( Rifampin drastically reduces plasma concentrations and effects of oral midazolam.
Backman, JT; Neuvonen, PJ; Olkkola, KT, 1996
)
"Rifampin pretreatment decreased the maximum plasma concentration of triazolam to 12.4% of the control value (i.e., from 2.9 +/- 0.2 to 0.36 +/- 0.06 ng/ml [p < 0.001]) and the elimination half-life from 2.8 +/- 0.1 to 1.3 +/- 0.1 hours (p < 0.001)."( Triazolam is ineffective in patients taking rifampin.
Backman, JT; Kivistö, KT; Neuvonen, PJ; Olkkola, KT; Villikka, K, 1997
)
"Rifampin treatment for four days utilized as a single agent after completion of parenteral therapy failed to reliably eradicate GBS colonization in infants."( Failure of rifampin to eradicate group B streptococcal colonization in infants.
Albanyan, EA; Baker, CJ; Edwards, MS; Fernandez, M; Rench, MA, 2001
)
"In rifampin-treated immunosuppressed animals the survival half-life of solid bacilli, in the absence of host immunity, was 12-13 days."( Effect of rifampin, clofazimine, and B1912 on the viability of Mycobacterium leprae in established mouse footpad infection.
Banerjee, DK; Hilson, GR; Holmes, IB, 1976
)
"Rifampin treatment resulted in a five- or eightfold mean increase (P < 0.05) in the biopsy concentration of P450IIIA4 mRNA when normalized for content of sucrase isomaltase or intestinal fatty acid binding protein mRNAs, respectively."( Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes.
Fang, C; Kolars, JC; Schmiedlin-Ren, P; Schuetz, JD; Watkins, PB, 1992
)
"The rifampin-treated patients had a significant delay in time to first catheter-related infection (P less than 0.015) and significantly fewer catheter-related infections overall (P less than 0.001)."( Randomized controlled trial of prophylactic rifampin for peritoneal dialysis-related infections.
Ahrens, E; Craig, W; Engeseth, S; Johnson, CA; Leggett, J; O'Brien, M; Oxton, L; Roecker, EB; Zimmerman, SW, 1991
)
"Rifampin pretreatment led to a significant decrease in average serum free fraction of lidocaine, from 0.24 +/- 0.08 to 0.080 +/- 0.030 (P less than 0.001)."( Effect of serum protein binding on the entry of lidocaine into brain and cerebrospinal fluid in dogs.
Artru, AA; Bowdle, TA; Marathe, PH; Shen, DD, 1991
)
"The rifampin treatment, on the other hand, did significantly lower the relapse rate and only a single case of dapsone resistance was detected."( Relapse rate and incidence of dapsone resistance in lepromatous leprosy patients in Addis Ababa: risk factors and effect of short-term supplementary treatment.
Mengistu, G; Warndorff van Diepen, T, 1985
)
"Rifampin pretreatment in healthy humans induced the ABT by 27%, but did not induce the PBT."( Comparison of the phenacetin and aminopyrine breath tests: effect of liver disease, inducers and cobaltous chloride.
Baker, AL; Kotake, AN; Krager, PS; Lambert, GH; Schoeller, DA,
)
"Rifampin pretreatment in the rabbit caused a selective induction of hepatic parameters resembling in some respects phenobarbital induction. "( Effects of rifampin pretreatment on hepatic parameters in the rabbit.
Iverson, F; Whitehouse, LW; Wong, LT,
)
"Rifampin treatment also resulted in the uncondensing of isolated nucleoids and in an axial appearance of the nucleoids in ultrathin sections."( Effect of rifampin on the structure and membrane attachment of the nucleoid of Escherichia coli.
Dworsky, P; Schaechter, M, 1973
)
"Treatment of rifampin-monoresistant/multidrug-resistant Tuberculosis (RR/MDR-TB) requires long treatment courses, complicated by frequent adverse events and low success rates. "( Rifampin-resistant/multidrug-resistant Tuberculosis in Alberta, Canada: Epidemiology and treatment outcomes in a low-incidence setting.
Cooper, R; Edwards, BD; Edwards, J; Fisher, D; Kunimoto, D; Somayaji, R, 2021
)
"Treatment with rifampin and pyrazinamide was more effective than treatment with rifampin, isoniazid, and pyrazinamide at reducing the lung CFU count, consistent with past evidence of isoniazid's antagonism in this model."( Enhanced bactericidal activity of rifampin and/or pyrazinamide when combined with PA-824 in a murine model of tuberculosis.
Grosset, J; Nuermberger, E; Tasneen, R; Tyagi, S; Williams, K, 2008
)
"Treatment was rifampin, isoniazide, and pyrazinamide or ethambutol."( Tuberculous orchiepididymitis during 1978-2003 period: review of 34 cases and role of 16S rRNA amplification.
Baquero, F; Buitrago, LA; Burgos Revilla, J; Gómez García, I; Gómez Mampaso, E; Gómez Rodríguez, A; Molina, MR; Sampietro Crespo, A, 2010
)
"Pretreatment with rifampin, a potent CYP3A4 inducer, decreased ruxolitinib AUC(0-∞) by 71% while resulting in only a 10% decrease in the overall PD activity."( The effect of CYP3A4 inhibition or induction on the pharmacokinetics and pharmacodynamics of orally administered ruxolitinib (INCB018424 phosphate) in healthy volunteers.
Chen, X; Emm, T; Landman, RR; Lo, Y; McGee, RF; McKeever, EG; Punwani, NG; Scherle, PA; Shi, JG; Williams, WV; Yeleswaram, S, 2012
)
"Pretreatment with rifampin significantly decreased serum alanine transaminase (ALT) activities, aspartate transaminase (AST) activities and prevented severe liver necrosis following acetaminophen overdose."( Effects and mechanisms of rifampin on hepatotoxicity of acetaminophen in mice.
Chen, C; Chen, Z; He, M; Huang, J; Huang, R; Jiao, Y; Lin, X; Zhang, S, 2012
)
"Treatment with rifampin, tobramycin, and ciprofloxacin was started 7 days after subcutaneous implantation of catheters precolonized with 10(4) CFU of S."( Rapid direct method for monitoring antibiotics in a mouse model of bacterial biofilm infection.
Contag, PR; Francis, KP; Kadurugamuwa, JL; Kimura, R; Purchio, T; Sin, LV; Yu, J, 2003
)
"Treatment with rifampin resulted in a 70% increase (p = 0.008) of the serum concentration of the bile acid precursor 7alpha-hydroxy-4-cholesten-3-one, which is a marker for bile acid production. "( Influence of rifampin on serum markers of cholesterol and bile acid synthesis in men.
Axelson, M; Hahn, C; Lütjohann, D; Prange, W; Reichel, C; Sauerbruch, T; Sudhop, T; von Bergmann, K, 2004
)
"Treatment with rifampin and streptomycin for 4 weeks or more inhibited growth of M."( Efficacy of the combination rifampin-streptomycin in preventing growth of Mycobacterium ulcerans in early lesions of Buruli ulcer in humans.
Amedofu, GK; Amofah, G; Ampadu, E; Asiedu, K; Awuah, P; Carbonnelle, B; Etuaful, S; Evans, M; Grosset, J; Horsfield, C; Klustse, E; Lucas, S; Ofori-Adjei, D; Owusu-Boateng, J; Phillips, R; Wansbrough-Jones, M, 2005
)
"Treatment with rifampin led to complete or partial resolution of pruritus in 47 (77%) patients as compared with 12(20%) treated with placebo or alternative (OR 15.2, 95% confidence interval 5.2-45.6, P=0.001)."( Rifampin is safe for treatment of pruritus due to chronic cholestasis: a meta-analysis of prospective randomized-controlled trials.
Khurana, S; Singh, P, 2006
)
"Treatment with rifampin-clarithromycin or moxifloxacin-clarithromycin for 8 weeks displayed promising bactericidal activity against Mycobacterium ulcerans in mice; none of the mice treated with rifampin-clarithromycin relapsed, whereas 59% of those treated with moxifloxacin-clarithromycin relapsed after treatment was stopped. "( Bactericidal and sterilizing activities of several orally administered combined regimens against Mycobacterium ulcerans in mice.
Chauffour, A; Jarlier, V; Ji, B; Robert, J, 2008
)
"Treatment with rifampin alone or with rifampin plus cloxacillin eradicated the original strain from 80% of the men for 12 weeks after treatment; 15%-20% of the 80 subjects acquired a strain of a different phage type."( Long-term studies of the effect of rifampin on nasal carriage of coagulase-positive staphylococci.
Kohler, RB; Luft, FC; Wheat, LJ; White, A,
)
"Pretreatment with rifampin (50 microM) resulted in a 5.5- to 9-fold higher rate of midazolam metabolism when compared with control cultures."( Induction of the metabolism of midazolam by rifampin in cultured porcine hepatocytes: preliminary evidence for CYP3A isoforms in pigs.
Hansen, LK; Hosagrahara, VP; Remmel, RP, 1999
)
"Treatment with rifampin resulted in a significantly increased expression of duodenal P-glycoprotein content 4.2-fold (2.9, 6.51) (Western blot) and messenger RNA was increased in six of the eight volunteers."( Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction.
Franke, G; Fritz, P; Hachenberg, T; Kauffmann, HM; Knoke, M; Kroemer, HK; Oertel, R; Schrenk, D; Siegmund, W; Terhaag, B; von Richter, O; Warzok, R; Weinbrenner, A; Westphal, K; Zschiesche, M, 2000
)
"Treatment with rifampin-loaded microspheres alone resulted in significant reductions in the numbers of CFU in the lungs and spleens by day 26."( Treatment of tuberculosis using a combination of sustained-release rifampin-loaded microspheres and oral dosing with isoniazid.
Barrow, EL; Barrow, WW; Quenelle, DC; Staas, JK; Winchester, GA, 2001
)
"Treatment with rifampin, even for one or two weeks, drastically reduced the number of infections by all of these criteris, and treatment for three weeks cured nearly all mice; the incidences of primary and residual infections in rifampin-treated mice after three weeks were 0 and 8.5%, respectively, as compared with 70.3% and 73.5%, respectively, in tetracycline-treated mice."( Rifampin in the treatment of experimental brucellosis in mice and guinea pigs.
Kazmierczak, A; Marly, JL; Nevot, PA; Philippon, AM; Plommet, MG, 1977
)
"Treatment with rifampin and ethambutol resulted in progressive clinical and roentgenographic resolution with an apparent cure after 18 months of therapy."( Pulmonary disease caused by Mycobacterium terrae complex.
Hammond, MD; Tonner, JA, 1989
)
"Treatment with rifampin significantly (p less than 0.01) decreased the number of MRSA per gram of bone compared with the number in control animals."( Treatment of methicillin-resistant Staphylococcus aureus experimental osteomyelitis with ciprofloxacin or vancomycin alone or in combination with rifampin.
Henry, NK; McConnell, ME; Rouse, MS; Whitesell, AL; Wilson, WR, 1987
)
"Treatment with rifampin also increased co-transformation by linked heterospecific markers."( Relation of macromolecular synthesis in streptococci to efficiency of transformation by markers of homospecific and heterospecific origin.
Deddish, PA; Ravin, AW, 1974
)

Toxicity

Diosmin may be used along with anti-tubercular drugs (isoniazid and rifampin) in tuberculosis patients to overcome their hepatotoxic adverse effect.

ExcerptReference
"Observations with the light and electron microscopes showed that a reverse transcriptase inhibitor, AF/ABDP cis which is a rifampicin derivative, had a toxic effect on ovaries of young Xenopus laevis."( Cytotoxic effect of a reverse transcriptase inhibitor, AF/ABDP cis, on ovaries of young Xenopus laevis--ultrastructural and autoradiographic study.
Steens, M, 1977
)
" Thus, the adverse effects of rifampin on renal transplant function might be overcome by increasing the dose of glucocorticoid drug."( Interaction of rifampin and glucocorticoids. Adverse effect on renal allograft function.
Buffington, GA; Dominguez, JH; Hebert, LA; Kauffman, HM; Lemann, J; Piering, WF, 1976
)
" An additive toxic effect was obvious in patients receiving streptomycin; when the treatment was withdrawn the urinary NAG activity stabilized within 15-21 days."( Detection of rifampicin-induced nephrotoxicity by N-acetyl-3-D-glucosaminidase activity.
Krishnaswamy, K; Kumar, BD; Prasad, CE, 1992
)
"It was established on isolated rat hearts that adaptation of the organism to stress exposure effectively limits toxic effect of chronic rifampicin administration (7 mg/kg/day for 8 days) and does not affect the depression of contractile function induced by chronic polymyxin B administration (0."( [Adaptation of the body to stressors prevents the cardiotoxic effect of rifampicin but not polymyxin B].
Malyshev, IIu; Meerson, FZ, 1991
)
" The hypothesis that this toxic effect might have resulted from abnormal metabolism of cyclosporin by liver cytochrome P-450 IIIA was investigated with the [14C]erythromycin breath test, which is a measure of this enzyme's activity."( Cyclosporin toxicity at therapeutic blood levels and cytochrome P-450 IIIA.
Aldrich, M; Campbell, DA; Kolars, JC; Lucey, MR; Merion, RM; Watkins, PB, 1990
)
"7%]); had similar rates of adverse drug reactions (7."( USPHS Tuberculosis Short-Course Chemotherapy Trial 21: effectiveness, toxicity, and acceptability. The report of final results.
Combs, DL; Geiter, LJ; O'Brien, RJ, 1990
)
" Because of the high frequency of adverse effects and more than adequate rifampin concentrations achieved in the cerebrospinal fluid, rifampin doses lower than that used in this study may be evaluated in future studies."( Pharmacokinetics, cerebrospinal fluid concentration, and safety of intravenous rifampin in pediatric patients undergoing shunt placements.
Barson, WJ; Bartkowski, HM; Fan-Havard, P; Kosnik, EJ; Nahata, MC, 1990
)
"An analysis of the adverse effects appearing in 101 patients during at least 4 months of chemotherapy for newly detected pulmonary tuberculosis between September, 1985 and July, 1987 was performed."( Adverse effects of antitubercular drugs and significance of measurement of the drug-stimulating lymphocyte transformation rate.
Umeki, S,
)
" This association of toxic reactions with antibodies is highly significant (P<0."( Potentially serious side effects of high-dose twice-weekly rifampicin.
Poole, G; Stradling, P; Worlledge, S, 1971
)
"Possible toxic side-effects of antituberculous chemotherapy are studied in 718 children affected with pulmonary tuberculosis."( [Toxicity in the current treatment of pulmonary tuberculosis in children].
Alcáide Megías, J; Altet Gómez, MN; Boque Genovard, MA, 1984
)
"Rifampin has proved to be a valuable antibiotic with relatively few major adverse effects."( Adverse effects of rifampin.
Grosset, J; Leventis, S,
)
" It is concluded that the combination RMP + ETH is the toxic component."( Hepatotoxicity of the combination of rifampin-ethionamide in the treatment of multibacillary leprosy.
Bourland, J; Davies, EM; Feracci, C; Grillone, S; Janssens, L; Pattyn, SR; Saylan, T, 1984
)
"Pyrazinamide, an antituberculous drug discovered in 1952, was first considered as a toxic drug."( [Toxicity of pyrazinamide in antituberculous treatments (author's transl)].
Perdrizet, S; Pretet, S, 1980
)
" Major toxic effects occurred in 22 patients; in 14 during the daily phase and in 8 during the twice-weekly phase."( Undesirable side effects of isoniazid and rifampin in largely twice-weekly short-course chemotherapy for tuberculosis.
Dutt, AK; Moers, D; Stead, WW, 1983
)
"The adverse effects of drugs which caused changes in therapeutic regimens have been studied in 511 patients with pulmonary tuberculosis, at the Pavilion Koch of Buenos Aires University."( Adverse effects of antituberculosis drugs causing changes in treatment.
Dambrosi, A; Dambrosi, VM; Gonzalez Montaner, LJ; Manassero, M, 1982
)
" These cases plus similar reports in the literature suggest that isoniazid or rifampin, or both, may potentiate the hepatotoxicity of acetaminophen, perhaps by induction of cytochrome P450 isozymes that oxidize acetaminophen to its toxic metabolites."( Hepatotoxicity associated with acetaminophen usage in patients receiving multiple drug therapy for tuberculosis.
Nelson, SD; Nolan, CM; Sandblom, RE; Slattery, JT; Thummel, KE, 1994
)
" Although these could have been engendered by dapsone toxicity, it was thought that a concommitant adverse reaction to rifampicin, which is known to be hepatotoxic, nephrotoxic and possibly capable of predisposing to the dapsone syndrome, could not be excluded."( A fatal case of drug-induced multi-organ damage in a patient with Hansen's disease: dapsone syndrome or rifampicin toxicity?
Lau, G, 1995
)
" Adverse events were reported by four patients (five events) in the RMP group and six patients (six events) in the RBT group."( Efficacy and safety of rifabutin in the treatment of patients with newly diagnosed pulmonary tuberculosis.
Bredell, M; Felten, MK; Fourie, PB; Mabuza, B; McGregor, MM; Olliaro, P; Wolmarans, L, 1996
)
" Isoniazid and rifampicin encapsulated in liposomes were less toxic to peritoneal macrophages as compared to free drugs."( Lung specific stealth liposomes: stability, biodistribution and toxicity of liposomal antitubercular drugs in mice.
Deol, P; Khuller, GK, 1997
)
" We examined retrospectively adverse events occurring during a 6-month period of antituberculosis treatment."( [Adverse effects related to the use of antitubercular drugs in psychiatric centers: retrospective study at the Philippe Pinel CH in Amiens 1994].
Andréjak, M; Compagnon, M; Decocq, G; Doutrellot, C; Guedj, B,
)
" Rifampicin analogues also inhibited the toxicity of pre-aggregated amyloid beta1-42 peptides, suggesting a common toxic mechanism of different amyloid peptides and their therapeutic potential for several amyloidoses."( Rifampicin inhibits the toxicity of pre-aggregated amyloid peptides by binding to peptide fibrils and preventing amyloid-cell interaction.
Asano, S; Endo, N; Kaneko, H; Kataoka, Ki; Tomiyama, T, 1997
)
"We realized a comparative study of the epidemiologic and clinical characteristics, and the incidence of adverse reactions to rifampin (between 1986-1993), comparing the seropositive patients treated with rifampin, during more than 3 months, with one control group, of equal number of patients, without evidence of HIV infection, taken at random, with epidemiologic characteristics (age and sex) similar to the first group and also treated with rifampin during a similar period."( [Rifampicin toxicity in HIV-infected patients: A study of its incidence and the risk factors].
Falguera, M; Gort, A; Schoenenberger, JA, 1997
)
" Safety was carefully monitored by regular biochemical and haematological testing and recording of adverse events."( Efficacy and safety of teicoplanin plus rifampicin in the treatment of bacteraemic infections caused by Staphylococcus aureus.
Boelens, HA; Verbrugh, HA; Vogel, M; Yzerman, EP, 1998
)
" Although toxic effects of most individual therapies are known, the toxic potential of most combination therapies has not been established."( Subchronic toxicity of human immunodeficiency virus and tuberculosis combination therapies in B6C3F1 mice.
Farnell, DR; Giles, HD; Heath, JE; Lindamood, C; Rao, GN, 1998
)
"The usefulness of the lymphocyte transformation test (LTT) for the analysis of adverse reactions to antituberculous drugs was evaluated."( Lymphocyte transformation test for the evaluation of adverse effects of antituberculous drugs.
Greinert, U; Müller-Quernheim, J; Schlaak, M; Schreiber, J; Zissel, G, 1999
)
" RMF and PN plus RMF did not show any adverse effects at this in vivo experimental condition."( Effect of pyridoxine on rifampicin toxicity.
Chung, JH; Kim, HS; Kim, KH; Yun, YP, 1991
)
"2% developed adverse hepatic reaction within the first month of INH + RMP treatment."( Slow N-acetyltransferase 2 genotype affects the incidence of isoniazid and rifampicin-induced hepatotoxicity.
Azuma, J; Fukuda, T; Igarashi, T; Ito, M; Komuta, K; Maeda, K; Maekura, R; Ogura, T; Ohno, M; Yamaguchi, I; Yamamoto, I; Yamamoto, Y; Yokota, S, 2000
)
"To determine whether foals with pneumonia that were treated with erythromycin, alone or in combination with rifampin or gentamicin, had a higher risk of developing adverse effects, compared with foals treated with trimethoprim-sulfamethoxazole (TMS), penicillin G procaine (PGP), or a combination of TMS and PGP (control foals)."( Risk of adverse effects in pneumonic foals treated with erythromycin versus other antibiotics: 143 cases (1986-1996).
Gardner, IA; Stratton-Phelps, M; Wilson, WD, 2000
)
" Relative risk (RR) and attributable risk (AR) were calculated to compare risk of adverse reactions between foals treated with erythromycin and control foals."( Risk of adverse effects in pneumonic foals treated with erythromycin versus other antibiotics: 143 cases (1986-1996).
Gardner, IA; Stratton-Phelps, M; Wilson, WD, 2000
)
" Adverse effects were more likely to occur in MB cases and were more frequent during the first 6 doses of intermittent regimens."( Serious side effects of rifampin on the course of WHO/MDT: a case report.
Namisato, M; Ogawa, H, 2000
)
" We conclude that CFZ is a generally well tolerated and safe drug when given as a daily dose of 50mg, which is currently used in leprosy patients."( Biochemical and hematological side effects of clofazimine in leprosy patients.
Costa Queiroz, RH; de Souza, AM; Melchior, E; Sampaio, SV, 2002
)
"Major adverse reactions to antituberculosis drugs can cause significant morbidity, and compromise treatment regimens for tuberculosis (TB)."( Incidence of serious side effects from first-line antituberculosis drugs among patients treated for active tuberculosis.
Menzies, D; Parisien, I; Pelletier, M; Rocher, I; Valiquette, C; Yee, D, 2003
)
"The introduction of multidrug therapy (WHO/MDT)-composed by the drugs dapsone, clofazimine and rifampicin has enabled the cure of Hansen's disease, however, the adverse effects of these drugs were not given priority by the health team."( [Adverse effects of multidrug therapy in leprosy patients: a five-year survey at a Health Center of the Federal University of Uberlândia].
Arbex, GL; Carneiro, MH; Gadia, R; Goulart, IM; Rodrigues, MS,
)
" Group II also registered; the maximum cost and highest incidence of adverse effects."( Comparative evaluation of efficacy and safety profile of three anti-tuberculous regimens in Mangalore.
Beena, S; Pai, MR; Rao, KN, 2002
)
" In all five studies, most adverse events were related to hypoglycemia, as expected in a normal population given a blood glucose regulator."( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide.
Hansen, KT; Hatorp, V; Thomsen, MS, 2003
)
" Patients in both groups tolerated the therapy well; the adverse effects profile was comparable except that group A patients had a higher incidence of hepatitis than group B patients (13."( Safety and antiretroviral effectiveness of concomitant use of rifampicin and efavirenz for antiretroviral-naive patients in India who are coinfected with tuberculosis and HIV-1.
Patel, A; Patel, B; Patel, J; Patel, K; Rani, S; Shah, N, 2004
)
" Severe adverse reactions included rash (two), toxic hepatitis (six), Immune Reconstitution Syndrome (seven), and four deaths."( Efficacy and safety of Efavirenz in HIV patients on Rifampin for tuberculosis.
Alves, CR; Badaro, R; Brites, C; Netto, EM; Oliveira, AS; Pedral-Sampaio, DB, 2004
)
"Types and frequency of drug-related adverse events and outcomes of treatment."( Adverse events and treatment completion for latent tuberculosis in jail inmates and homeless persons.
Bock, NN; Grabau, JC; Jasmer, RM; Lobato, MN; Reves, RR; Shang, N, 2005
)
"4%) who had a drug-related adverse event."( Adverse events and treatment completion for latent tuberculosis in jail inmates and homeless persons.
Bock, NN; Grabau, JC; Jasmer, RM; Lobato, MN; Reves, RR; Shang, N, 2005
)
" On some occasions, it cannot be used due to severe adverse effects."( [Use of rifabutin in cases of toxicity to rifampicin].
Moreno González, B; Noguerado Asensio, A; Rodríguez Barrientos, R; Rodríguez Blanco, A; Vidal Pérez, JL, 2005
)
"5 million adverse drug reaction (ADR) reports for 8620 drugs/biologics that are listed for 1191 Coding Symbols for Thesaurus of Adverse Reaction (COSTAR) terms of adverse effects."( Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
Benz, RD; Contrera, JF; Kruhlak, NL; Matthews, EJ; Weaver, JL, 2004
)
"This meta-analysis suggests that rifampin is safe and effective for treatment of pruritus due to chronic cholestasis."( Rifampin is safe for treatment of pruritus due to chronic cholestasis: a meta-analysis of prospective randomized-controlled trials.
Khurana, S; Singh, P, 2006
)
" In this study, we compared treatment completion and clinically recognized adverse drug reactions in patients prescribed 9 months of isoniazid therapy or 4 months of rifampin therapy for LTBI."( Improved adherence and less toxicity with rifampin vs isoniazid for treatment of latent tuberculosis: a retrospective study.
Adelakun, A; Baruch, N; Bur, S; Cronin, WA; Doherty, MC; Dorman, SE; Federline, L; Karney, W; Milman, J; Montes de Oca, R; Page, KR; Sifakis, F; Walsh, T, 2006
)
"Compared with a 9-month isoniazid regimen, a 4-month rifampin regimen was associated with a higher percentage of patients completing treatment and a lower percentage of patients with clinically recognized adverse reactions."( Improved adherence and less toxicity with rifampin vs isoniazid for treatment of latent tuberculosis: a retrospective study.
Adelakun, A; Baruch, N; Bur, S; Cronin, WA; Doherty, MC; Dorman, SE; Federline, L; Karney, W; Milman, J; Montes de Oca, R; Page, KR; Sifakis, F; Walsh, T, 2006
)
" Secondary endpoints were presence of grade 3 and serious adverse events, clinical improvement, CD4 count and genotypic resistance to ritonavir/saquinavir."( Safety, efficacy and pharmacokinetics of ritonavir 400mg/saquinavir 400mg twice daily plus rifampicin combined therapy in HIV patients with tuberculosis.
da Silva Vieira, MA; de Jesus, Cda S; Ferreira Filho, M; Gonçalves Morgado, M; Lourenço, MC; Pereira Pinto, D; Rolla, VC; Werneck-Barroso, E, 2006
)
" During the antiretroviral therapy, 15 patients dropped out, 14 because of adverse events."( Safety, efficacy and pharmacokinetics of ritonavir 400mg/saquinavir 400mg twice daily plus rifampicin combined therapy in HIV patients with tuberculosis.
da Silva Vieira, MA; de Jesus, Cda S; Ferreira Filho, M; Gonçalves Morgado, M; Lourenço, MC; Pereira Pinto, D; Rolla, VC; Werneck-Barroso, E, 2006
)
"Therapeutic concentrations of the studied drugs and reduction of viral load were achieved; adverse events are the main limitation of use of a ritonavir/saquinavir regimen in treatment-naive patients, but its clinical benefits were evident."( Safety, efficacy and pharmacokinetics of ritonavir 400mg/saquinavir 400mg twice daily plus rifampicin combined therapy in HIV patients with tuberculosis.
da Silva Vieira, MA; de Jesus, Cda S; Ferreira Filho, M; Gonçalves Morgado, M; Lourenço, MC; Pereira Pinto, D; Rolla, VC; Werneck-Barroso, E, 2006
)
"Rifampicin in a dose of 10-20 mg/Kg/day is safe and effective in ameliorating uncontrollable pruritus in children with persistent cholestasis."( Safety and efficacy of rifampicin in children with cholestatic pruritus.
El-Karaksy, H; El-Koofy, N; El-Raziky, M; El-Sayed, R; Mansour, S; Taha, G, 2007
)
" A longer well-designed randomized controlled trial is needed to confirm the efficacy of bile acid binding agents and accurately assess adverse events."( The efficacy and safety of bile Acid binding agents, opioid antagonists, or rifampin in the treatment of cholestasis-associated pruritus.
Bain, VG; Rowe, BH; Tandon, P; Vandermeer, B, 2007
)
" The aim of this study was to evaluate the influences of pyridoxine, rifampin, and renal function on hematological adverse events."( Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
Bové, A; García, S; Marcos, M; Martínez, JA; Martínez, JC; Mensa, J; Ortega, M; Peñarroja, G; Soriano, A, 2007
)
" Although safe and generally well tolerated, 300 mg or 400 mg atazanavir administered every 12 h did not maintain adequate plasma exposure when coadministered with rifampin."( Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
Acosta, EP; Agarwala, S; Alston-Smith, B; Bertz, R; Child, M; Gerber, JG; Haas, DW; Hosey, L; Kendall, MA; Koletar, SL; Zolopa, AR, 2007
)
"Liver transplant candidates with latent tuberculosis infection by positive tuberculin skin test (>5 mm) were prospectively enrolled and treated with 9 months of INH or 4 months of RIF, and were monitored monthly for their liver enzyme profiles, adverse effects, compliance, and completion rate."( Safety of treatment of latent tuberculosis infection in compensated cirrhotic patients during transplant candidacy period.
Bui, L; Jahng, AW; Joyner, JL; Tran, T, 2007
)
"Treatment of latent tuberculosis in liver transplant patients during their candidacy with INH or RIF appears to be a safe, viable option, if carefully monitored for adverse effects and liver enzymes."( Safety of treatment of latent tuberculosis infection in compensated cirrhotic patients during transplant candidacy period.
Bui, L; Jahng, AW; Joyner, JL; Tran, T, 2007
)
" Adverse effects often negatively affect the compliance, because they frequently require a change of treatment, which may have negative consequences for treatment outcome."( Antituberculosis drug-induced hepatotoxicity: concise up-to-date review.
Aarnoutse, RE; Boeree, MJ; de Lange, WC; Dekhuijzen, R; Tostmann, A; van der Ven, AJ, 2008
)
" Metabolism and the formation of toxic metabolites of the TB drugs may play an important role in the development of ATDH."( Isoniazid and its toxic metabolite hydrazine induce in vitro pyrazinamide toxicity.
Aarnoutse, RE; Boeree, MJ; Dekhuijzen, PN; Peters, WH; Roelofs, HM; Tostmann, A; van der Ven, AJ, 2008
)
" The occurrence of adverse effects was also monitored."( Clinical evaluation and monitoring of adverse effects for fixed multidose combination against single drug therapy in pulmonary tuberculosis patients.
Chaudhry, A; Jamshaid, M; Zaka-Ur-Rehman, Z, 2008
)
"The study showed a high incidence of adverse events when a higher than standard dose of the new lopinavir/ritonavir tablets was combined with rifampicin."( High incidence of adverse events in healthy volunteers receiving rifampicin and adjusted doses of lopinavir/ritonavir tablets.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Koopmans, PP; L'homme, RF; Nijland, HM; Rongen, GA; van Crevel, R; van Uden, P, 2008
)
" However, it is undetectable in cultured hepatocyte monolayers in vitro at the equivalent toxic concentration in vivo."( Investigation of rifampicin-induced hepatotoxicity in rat hepatocytes maintained in gel entrapment culture.
Cheng, X; Li, D; Meng, Q; Shen, C, 2009
)
"To compare the frequency of adverse events and treatment completion in 2 treatment regimens for latent tuberculosis infection."( Adverse events with 4 months of rifampin therapy or 9 months of isoniazid therapy for latent tuberculosis infection: a randomized trial.
Al Jahdali, H; Benedetti, A; Dion, MJ; Gardam, M; Hoeppner, V; Khan, K; Long, R; Memish, Z; Menzies, D; Schwartzman, K; Trajman, A; Yang, J, 2008
)
"Grade 3 to 4 drug-related adverse events resulting in drug discontinuation (primary outcome), and on-time treatment completion, grade 1 to 2 drug-related adverse events, and changes in liver enzymes and hematologic variables (secondary outcomes)."( Adverse events with 4 months of rifampin therapy or 9 months of isoniazid therapy for latent tuberculosis infection: a randomized trial.
Al Jahdali, H; Benedetti, A; Dion, MJ; Gardam, M; Hoeppner, V; Khan, K; Long, R; Memish, Z; Menzies, D; Schwartzman, K; Trajman, A; Yang, J, 2008
)
"Seventeen of 422 participants who started isoniazid therapy developed grade 3 to 4 adverse events compared with 7 of 418 who started rifampin therapy (risk difference [rifampin minus isoniazid], -2."( Adverse events with 4 months of rifampin therapy or 9 months of isoniazid therapy for latent tuberculosis infection: a randomized trial.
Al Jahdali, H; Benedetti, A; Dion, MJ; Gardam, M; Hoeppner, V; Khan, K; Long, R; Memish, Z; Menzies, D; Schwartzman, K; Trajman, A; Yang, J, 2008
)
"The study did not measure efficacy, and the open-label design may increase the chance of bias in ascertainment of adverse events."( Adverse events with 4 months of rifampin therapy or 9 months of isoniazid therapy for latent tuberculosis infection: a randomized trial.
Al Jahdali, H; Benedetti, A; Dion, MJ; Gardam, M; Hoeppner, V; Khan, K; Long, R; Memish, Z; Menzies, D; Schwartzman, K; Trajman, A; Yang, J, 2008
)
"Treatment of latent tuberculosis with 4 months of rifampin leads to fewer serious adverse events and better adherence than 9 months of isoniazid."( Adverse events with 4 months of rifampin therapy or 9 months of isoniazid therapy for latent tuberculosis infection: a randomized trial.
Al Jahdali, H; Benedetti, A; Dion, MJ; Gardam, M; Hoeppner, V; Khan, K; Long, R; Memish, Z; Menzies, D; Schwartzman, K; Trajman, A; Yang, J, 2008
)
" Two moderate-grade adverse events were observed."( Continuous cefazolin infusion to treat bone and joint infections: clinical efficacy, feasibility, safety, and serum and bone concentrations.
Desplaces, N; Durand, F; Kitzis, MD; Lhotellier, L; Mamoudy, P; Zeller, V; Ziza, JM, 2009
)
" DHS and other adverse effects of dapsone lead to withdrawal of the drug."( A retrospective study of the effect of modified multi-drug therapy in Nepali leprosy patients following the development of adverse effects due to dapsone.
Pandey, B; Sapkota, BR; Shrestha, K; Walker, SL, 2008
)
"We reviewed the notes of patients who had dapsone withdrawn from their multi-drug therapy (MDT) following an adverse reaction to the drug between 1990 and 2007."( A retrospective study of the effect of modified multi-drug therapy in Nepali leprosy patients following the development of adverse effects due to dapsone.
Pandey, B; Sapkota, BR; Shrestha, K; Walker, SL, 2008
)
"Rifampicin and clofazimine appear to be satisfactory treatment for both paucibacillary and multibacillary patients who have to have dapsone stopped because of severe adverse effects."( A retrospective study of the effect of modified multi-drug therapy in Nepali leprosy patients following the development of adverse effects due to dapsone.
Pandey, B; Sapkota, BR; Shrestha, K; Walker, SL, 2008
)
"Acetaminophen (APAP) is safe at therapeutic levels but causes hepatotoxicity via N-acetyl-p-benzoquinone imine-induced oxidative stress upon overdose."( Rifampicin-activated human pregnane X receptor and CYP3A4 induction enhance acetaminophen-induced toxicity.
Cheng, J; Gonzalez, FJ; Idle, JR; Krausz, KW; Ma, X, 2009
)
"Completion rates, total cost, and adverse effects were compared for patients in central Massachusetts treated for latent tuberculosis infection with 9 months of isoniazid or 4 months of rifampin."( A retrospective evaluation of completion rates, total cost, and adverse effects for treatment of latent tuberculosis infection in a public health clinic in central massachusetts.
Daly, JS; Ellis, J; Kaminski, M; Wessolossky, M; Young, H, 2009
)
" Efficacy of short-term treatment was analyzed by per-protocol analysis (PP analysis) and intention-to-treat analysis (ITT analysis) while drug adverse reactions was also observed."( [Study on the efficacy and safety of short-term treatment including fluoroquinolones anti-tuberculosis drugs for rifampicin resistant pulmonary tuberculosis].
Chu, NH; Duanmu, HJ; Kang, WL; Li, L; Miao, ZP; Tan, WG; Wang, XM; Xie, YG; Yan, XL; Yang, YZ; You, YH, 2009
)
" (3) Three patients withdrew in each of the two groups because of adverse effects to the drugs."( [Study on the efficacy and safety of short-term treatment including fluoroquinolones anti-tuberculosis drugs for rifampicin resistant pulmonary tuberculosis].
Chu, NH; Duanmu, HJ; Kang, WL; Li, L; Miao, ZP; Tan, WG; Wang, XM; Xie, YG; Yan, XL; Yang, YZ; You, YH, 2009
)
"Drug-induced hepatotoxicity (DIH) is the most common adverse drug reaction leading to interruption of antituberculosis treatment."( Safety of 3 different reintroduction regimens of antituberculosis drugs after development of antituberculosis treatment-induced hepatotoxicity.
Jayaswal, A; Makharia, G; Mohan, A; Sarda, P; Sharma, SK; Singh, S; Singla, R; Sreenivas, V, 2010
)
" Even though rifampicin is an effective drug in the management of tuberculosis, it has been documented to have some toxic effects in humans."( Modulatory activity of antioxidants against the toxicity of Rifampicin in vivo.
Akintonwa, A; Awodele, O; Coker, HA; Osunkalu, VO,
)
"Among the adverse events related to tuberculosis treatment, hepatotoxicity is the most serious, and recognition of risk factors for it is essential to achieve successful therapy."( Hepatotoxicity due to rifampicin, isoniazid and pyrazinamide in patients with tuberculosis: is anti-HCV a risk factor?
Bassanesi, SL; de Mattos, AA; De Mattos, AZ; Nader, LA; Picon, PD; Pineiro Rodriguez, M,
)
" An understanding of structure-activity relationships (SARs) of chemicals can make a significant contribution to the identification of potential toxic effects early in the drug development process and aid in avoiding such problems."( Developing structure-activity relationships for the prediction of hepatotoxicity.
Fisk, L; Greene, N; Naven, RT; Note, RR; Patel, ML; Pelletier, DJ, 2010
)
"Treatment for latent tuberculosis infection with isoniazid for 9 months (9INH) has poor completion and serious adverse events, while treatment for 4 months with daily rifampin (4RIF) has significantly higher completion and fewer adverse events."( Impact of treatment completion, intolerance and adverse events on health system costs in a randomised trial of 4 months rifampin or 9 months isoniazid for latent TB.
Aspler, A; Dion, MJ; Khan, K; Long, R; Menzies, D; Schwartzman, K; Trajman, A, 2010
)
" Costs were modestly increased in patients with minor intolerance and substantially increased if the treating physician stopped treatment because of possible adverse events."( Impact of treatment completion, intolerance and adverse events on health system costs in a randomised trial of 4 months rifampin or 9 months isoniazid for latent TB.
Aspler, A; Dion, MJ; Khan, K; Long, R; Menzies, D; Schwartzman, K; Trajman, A, 2010
)
"The 4RIF regimen was significantly cheaper per patient completing treatment because of better completion and fewer adverse events."( Impact of treatment completion, intolerance and adverse events on health system costs in a randomised trial of 4 months rifampin or 9 months isoniazid for latent TB.
Aspler, A; Dion, MJ; Khan, K; Long, R; Menzies, D; Schwartzman, K; Trajman, A, 2010
)
" Adverse events (AEs), ECG recordings, vital signs and clinical laboratory parameters were monitored throughout the study and at follow-up."( Effects of rifampicin (rifampin) on the pharmacokinetics and safety of ambrisentan in healthy subjects: a single-sequence, open-label study.
Boinpally, R; Dufton, C; Harrison, B; Henderson, LS; Magee, MH; Mandagere, A; Walker, G, 2010
)
" The use of INH for the treatment of LTBI is safe in older patients with clinical or biochemical monitoring."( Age-related risk of hepatotoxicity in the treatment of latent tuberculosis infection: a systematic review.
Khan, KS; Kunst, H, 2010
)
" Studies investigating the association of therapy with serious adverse events have not included the entire treated population nor accounted for comorbidities or occurrence of similar events in the untreated general population."( Adverse events associated with treatment of latent tuberculosis in the general population.
Bartlett, G; Menzies, D; Schwartzman, K; Smith, BM, 2011
)
" The primary outcome was hospital admission for therapy-associated adverse events."( Adverse events associated with treatment of latent tuberculosis in the general population.
Bartlett, G; Menzies, D; Schwartzman, K; Smith, BM, 2011
)
"The risk of adverse events requiring hospital admission increased significantly among patients over 65 years receiving treatment for latent tuberculosis infection."( Adverse events associated with treatment of latent tuberculosis in the general population.
Bartlett, G; Menzies, D; Schwartzman, K; Smith, BM, 2011
)
" Noninferiority was dependent on consistent results from a per-protocol and modified intention-to-treat analysis, using 2 different models for the latter, classifying all changes of treatment or refusal to continue treatment (eg, bacteriological failure/relapse, adverse event, default, drug resistance) as unfavorable (model 1) and classifying changes of treatment for reasons other than therapeutic outcomes according to their 18-month bacteriological outcome if available (post hoc model 2)."( Efficacy and safety of a 4-drug fixed-dose combination regimen compared with separate drugs for treatment of pulmonary tuberculosis: the Study C randomized controlled trial.
Anyo, G; Burgos, M; Cook, SV; Enarson, DA; Jindani, A; Kim, SJ; Lienhardt, C; Nunn, AJ; Rigouts, L; Yorke-Edwards, V, 2011
)
" Adverse events related to trial drugs were similarly distributed among treatment groups."( Efficacy and safety of a 4-drug fixed-dose combination regimen compared with separate drugs for treatment of pulmonary tuberculosis: the Study C randomized controlled trial.
Anyo, G; Burgos, M; Cook, SV; Enarson, DA; Jindani, A; Kim, SJ; Lienhardt, C; Nunn, AJ; Rigouts, L; Yorke-Edwards, V, 2011
)
"To assess the adverse effects of multi drug therapy (MDT) in leprosy patients."( Adverse effects of multi-drug therapy in leprosy, a two years' experience (2006-2008) in tertiary health care centre in the tribal region of Chhattisgarh State (Bastar, Jagdalpur).
Dey, V; Dulhani, N; Nel, B; Singh, H; Tiwari, P, 2011
)
" The adverse effects were recorded on the personal record of every individual patient, filled during the course of treatment."( Adverse effects of multi-drug therapy in leprosy, a two years' experience (2006-2008) in tertiary health care centre in the tribal region of Chhattisgarh State (Bastar, Jagdalpur).
Dey, V; Dulhani, N; Nel, B; Singh, H; Tiwari, P, 2011
)
"176 patient's records were analysed, looking for adverse effects."( Adverse effects of multi-drug therapy in leprosy, a two years' experience (2006-2008) in tertiary health care centre in the tribal region of Chhattisgarh State (Bastar, Jagdalpur).
Dey, V; Dulhani, N; Nel, B; Singh, H; Tiwari, P, 2011
)
" We evaluated adverse events and TB incidence in all persons screened after rifampicin (RFP) prophylaxis, and specifically assessed the new TB cases in relation to initial TST and IGRA results."( Adverse events and development of tuberculosis after 4 months of rifampicin prophylaxis in a tuberculosis outbreak.
Cho, YS; Kim, HJ; Lee, EJ; Lee, HK; Lee, SH; Lee, YM; Lew, WJ; Seo, HS; Shim, TS; Yim, JJ, 2012
)
" The cytotoxic effects against mouse fibroblasts (NIH 3T3) in vitro were evaluated for 5c and 5d, which displayed no toxic effects (IC(50) > 1000 μM) against the mouse fibroblast cell line NIH 3T3."( Synthesis of 3-heteroarylthioquinoline derivatives and their in vitro antituberculosis and cytotoxicity studies.
Chitra, S; Manisankar, P; Muthusubramanian, S; Paul, N; Sriram, D; Yogeeswari, P, 2011
)
" Four patients did not complete the 1-year treatment because of adverse events."( The clinical efficacy and safety of a fluoroquinolone-containing regimen for pulmonary MAC disease.
Fujita, M; Harada, E; Ikegame, S; Kajiki, A; Matsumoto, T; Miyazaki, M; Nakanishi, Y; Ouchi, H; Tao, Y; Uchino, J; Watanabe, K, 2012
)
" This case illustrates a unique side effect of INH that caused exudative EPEs and drug-induced lupus with positive anti-dsDNA."( Isoniazid (INH)-induced eosinophilic exudative pleural effusion and lupus erythematosus. A clinical reminder of drug side effects.
Dahal, K; Khattri, S; Kushawaha, A; Lee, M; Mobarakai, N, 2011
)
"PVP-CD was proved safe and demonstrated excellent biocompatibility, healing and degradation properties."( Safety, healing, and efficacy of vascular prostheses coated with hydroxypropyl-β-cyclodextrin polymer: experimental in vitro and animal studies.
Blanchemain, N; Haulon, S; Hildebrand, HF; Jean-Baptiste, E; Martel, B; Neut, C, 2012
)
"Tuberculosis (TB) treatment can cause serious sequelae including adverse effects such as anti-TB drug-induced hepatotoxicity (ATDH)."( Genetic variants in antioxidant pathway: risk factors for hepatotoxicity in tuberculosis patients.
Fukushima, K; Higuchi, N; Inamine, T; Kohno, S; Kondo, S; Mawatari, T; Nakaura, A; Nanashima, K; Suyama, N; Tahara, N; Tsukamoto, K; Yanagihara, K, 2012
)
" With careful monitoring rifampin is a safe and less toxic regimen and appears to be a reasonable alternative because of its shorter duration, allowing more people to complete treatment behind bars."( Isoniazid vs. rifampin for latent tuberculosis infection in jail inmates: toxicity and adherence.
Chen, L; Goldenson, J; Kawamura, LM; Lee, JR; Spetz, J; Tulsky, JP; White, MC, 2012
)
"Rifampicin together with rifampicin and metabolites of isoniazid produce cellular toxic effects and hydrazine may be the most toxiferous metabolite."( Cellular toxicity of isoniazid together with rifampicin and the metabolites of isoniazid on QSG-7701 hepatocytes.
Hou, YN; Tang, JH; Wu, HH; Zhan, ZL; Zhang, XL; Zhang, ZH, 2012
)
" In addition, it was found that the microsomal Ca(2+)-ATPase activity was not directly related to acetaminophen toxic species generated in the P450 enzyme system in vitro."( Effects and mechanisms of rifampin on hepatotoxicity of acetaminophen in mice.
Chen, C; Chen, Z; He, M; Huang, J; Huang, R; Jiao, Y; Lin, X; Zhang, S, 2012
)
"Hepatotoxicity is one of the most frequent adverse events occurring during tuberculosis treatment that may negatively affect treatment compliance, clinical outcome."( Management of and risk factors related to hepatotoxicity during tuberculosis treatment.
Ağca, S; Arda, H; Babalık, A; Bakırcı, N; Calışır, HC; Cetintaş, G; Kızıltaş, S; Oruç, K, 2012
)
" Adverse events were mostly mild and no serious adverse events or drug discontinuations were reported."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
"This study sought to verify the correlation between leprosy types and the adverse effects of treatment drugs."( Brazilian clinical trial of uniform multidrug therapy for leprosy patients: the correlation between clinical disease types and adverse effects.
Almeida, PC; Bührer-Sékula, S; Cruz, R; Gonçalves, Hde S; Moraes, ME; Penna, GO; Pontes, MA, 2012
)
" Cytochrome P450 2E1 (CYP2E1) metabolizes many toxic substrates, including ethanol, carbon tetrachloride, and INH, which ultimately results in liver injury."( Protective effects of kaempferol on isoniazid- and rifampicin-induced hepatotoxicity.
Hsieh, CB; Hu, OY; Lee, HS; Shih, TY; Young, TH, 2013
)
"55), and non-serious adverse event incidence (p = 0."( Efficacy and safety of thrice weekly DOTS in tuberculosis patients with and without HIV co-infection: an observational study.
Devarapu, SK; Gupta, D; Mohan, K; Ranjan, S; Sharma, SK; Singh, B; Sinha, S; Sreenivas, V; Vashishtha, R, 2013
)
" There is limited documented information regarding adverse effects and recommendations for serum biochemistry monitoring."( Adverse effects of rifampicin in dogs and serum alanine aminotransferase monitoring recommendations based on a retrospective study of 344 dogs.
Bajwa, J; Charach, M; Duclos, D, 2013
)
"The aims of this retrospective study were as follows: (i) to document the occurrence of adverse events in dogs receiving oral rifampicin; (ii) to determine the relationship between adverse events and the dosage/duration of therapy and concurrent medications; and (iii) to report findings associated with changes on serum alanine aminotransferase (ALT)."( Adverse effects of rifampicin in dogs and serum alanine aminotransferase monitoring recommendations based on a retrospective study of 344 dogs.
Bajwa, J; Charach, M; Duclos, D, 2013
)
" Serum ALT concentrations and adverse effects were recorded and analysed."( Adverse effects of rifampicin in dogs and serum alanine aminotransferase monitoring recommendations based on a retrospective study of 344 dogs.
Bajwa, J; Charach, M; Duclos, D, 2013
)
" Adverse events occurred in 16."( Adverse effects of rifampicin in dogs and serum alanine aminotransferase monitoring recommendations based on a retrospective study of 344 dogs.
Bajwa, J; Charach, M; Duclos, D, 2013
)
"Significant adverse events were noted in association with concurrent drug administration and with serum ALT elevations."( Adverse effects of rifampicin in dogs and serum alanine aminotransferase monitoring recommendations based on a retrospective study of 344 dogs.
Bajwa, J; Charach, M; Duclos, D, 2013
)
" NO production was also significantly higher but less than toxic level."( Microparticles of rifampicin: comparison of pulmonary route with oral route for drug uptake by alveolar macrophages, phagocytosis activity and toxicity study in albino rats.
Dalwadi, S; Parikh, R; Patel, L, 2014
)
"The safety of rifabutin replacing rifampicin among adults having rifampicin-related adverse reactions (ARs) during the treatment of tuberculosis remains unknown."( Safety of rifabutin replacing rifampicin in the treatment of tuberculosis: a single-centre retrospective cohort study.
Chien, JY; Chien, ST; Huang, SY; Yu, CJ, 2014
)
"Prolonged antimicrobial therapy is recommended for methicillin-susceptible Staphylococcus aureus (MSSA) bone and joint infections (BJI), but its safety profile and risk factors for severe adverse events (SAE) in clinical practice are unknown."( Antimicrobial-related severe adverse events during treatment of bone and joint infection due to methicillin-susceptible Staphylococcus aureus.
Ader, F; Bouaziz, A; Chidiac, C; Ecochard, R; Ferry, T; Karsenty, J; Laurent, F; Lustig, S; Tod, M; Valour, F, 2014
)
" Three (6%) of 50 participants in the rifampicin group and 12 (24%) of 50 in the placebo group had one or more serious adverse events; none was thought to be related to treatment."( Efficacy and safety of rifampicin for multiple system atrophy: a randomised, double-blind, placebo-controlled trial.
Biaggioni, I; Chelimsky, T; Cheshire, W; Dupont, WD; Freeman, R; Galpern, WR; Gilman, S; Hauser, RA; Kaufmann, H; Lessig, S; Low, PA; Mandrekar, J; Perlman, S; Robertson, D; Singer, W; Vernino, S, 2014
)
" The primary outcome was death and secondary outcome measures were 6 month disability, repeat MRI changes and serious adverse events (SAEs)."( Safety and efficacy of levofloxacin versus rifampicin in tuberculous meningitis: an open-label randomized controlled trial.
Bhoi, SK; Kalita, J; Misra, UK; Prasad, S, 2014
)
"There is an urgent need for new antituberculosis (anti-TB) drugs, including agents that are safe and effective with concomitant antiretrovirals (ARV) and first-line TB drugs."( Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.
Allen, R; Aweeka, F; Bao, J; Cramer, Y; Dooley, KE; Haas, DW; Koletar, SL; Luetkemeyer, AF; Marzan, F; Murray, S; Park, JG; Savic, R; Sutherland, D, 2014
)
" Adverse events were rare: 20 (6%) in the 9INH group and 2 (3%) in the 4RMP group, and none was serious."( Safety and completion of a 4-month course of rifampicin for latent tuberculous infection in children.
Cruz, AT; Starke, JR, 2014
)
"Observational study of clinical and laboratory adverse events among infants exposed to rifampin from 348 neonatal intensive care units managed by the Pediatrix Medical Group between 1997 and 2012."( Rifampin use and safety in hospitalized infants.
Arnold, CJ; Benjamin, DK; Chu, VH; Clark, RH; Corey, KL; Ericson, J; Hornik, CP; Kohman, J; Oh, M; Onabanjo, J; Smith, PB, 2015
)
" Thrombocytopenia (121/1,000 infant days) and conjugated hyperbilirubinemia (25/1,000 infant days) were the most common laboratory adverse events."( Rifampin use and safety in hospitalized infants.
Arnold, CJ; Benjamin, DK; Chu, VH; Clark, RH; Corey, KL; Ericson, J; Hornik, CP; Kohman, J; Oh, M; Onabanjo, J; Smith, PB, 2015
)
"The overall incidence of adverse events among infants receiving rifampin appears low; however, additional studies to further evaluate safety and dosing of rifampin in this population are needed."( Rifampin use and safety in hospitalized infants.
Arnold, CJ; Benjamin, DK; Chu, VH; Clark, RH; Corey, KL; Ericson, J; Hornik, CP; Kohman, J; Oh, M; Onabanjo, J; Smith, PB, 2015
)
" Similar LD50 (1570 mg/kg) and absence (or reversal in satellite group) of adverse events in repeat dose (three doses; highest dose was up to 50 times the human therapeutic dose) toxicity studies confirmed safety of RIF-SLNs."( Nano-formulation of rifampicin with enhanced bioavailability: development, characterization and in-vivo safety.
Jindal, S; Kaur, IP; Sharma, G; Singh, H; Singh, M, 2015
)
" We also assessed safety and tolerability by monitoring adverse events."( Efficiency and safety of the combination of moxifloxacin, pretomanid (PA-824), and pyrazinamide during the first 8 weeks of antituberculosis treatment: a phase 2b, open-label, partly randomised trial in patients with drug-susceptible or drug-resistant pul
Burger, DA; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Eisenach, K; Everitt, D; Ive, P; Mendel, CM; Ntinginya, NE; Page-Shipp, L; Pym, A; Reither, K; Schall, R; Spigelman, M; van Niekerk, C; Variava, E; Venter, A; von Groote-Bidlingmaier, F, 2015
)
" Frequencies of adverse events were similar to standard treatment in all groups."( Efficiency and safety of the combination of moxifloxacin, pretomanid (PA-824), and pyrazinamide during the first 8 weeks of antituberculosis treatment: a phase 2b, open-label, partly randomised trial in patients with drug-susceptible or drug-resistant pul
Burger, DA; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Eisenach, K; Everitt, D; Ive, P; Mendel, CM; Ntinginya, NE; Page-Shipp, L; Pym, A; Reither, K; Schall, R; Spigelman, M; van Niekerk, C; Variava, E; Venter, A; von Groote-Bidlingmaier, F, 2015
)
"3%] in the RPT 450 mg, RPT 600 mg and RMP groups), as were ⩾grade 3 adverse events (0/54 [0%], 1/51 [2."( Two-stage activity-safety study of daily rifapentine during intensive phase treatment of pulmonary tuberculosis.
Barnes, GL; Carman, D; Chaisson, RE; Dawson, R; Dorman, SE; Efron, A; Gupte, N; Hoffman, J; McIlleron, H; Narunsky, K; Whitelaw, A, 2015
)
" Daily RPT was safe and well-tolerated."( Two-stage activity-safety study of daily rifapentine during intensive phase treatment of pulmonary tuberculosis.
Barnes, GL; Carman, D; Chaisson, RE; Dawson, R; Dorman, SE; Efron, A; Gupte, N; Hoffman, J; McIlleron, H; Narunsky, K; Whitelaw, A, 2015
)
" Whereas free thioridazine was highly toxic in both cells and zebrafish embryos, after encapsulation in nanoparticles no toxicity was detected."( Thioridazine in PLGA nanoparticles reduces toxicity and improves rifampicin therapy against mycobacterial infection in zebrafish.
Anes, E; Bogoeva, V; Fenaroli, F; Griffiths, G; Hildahl, J; Kalluru, R; Pires, D; Speth, M; Vibe, CB; Wilson, SR, 2016
)
" The combination of anti-TB drugs (4-Tabs)- isoniazid (INH), rifampicin (RIF), pyrazinamide (PZA) and ethambutol (ETB) are effective in the management of the disease, however, their toxic effect is a major concern."( Ameliorative Effects of Kolaviron, a Biflavonoid Fraction from Garcinia Kola Seed, on Hepato-renal Toxicity of Anti-tuberculosis Drugs in Wistar Rats.
Adaramoye, OA; Adefisan, A; Adeyemi, O; Akanni, OO; Kehinde, AO; Oyinlola, I, 2016
)
"These findings suggest that anti-TB drugs elicit oxidative damage in liver and kidney of rats while KV protects against the adverse effects via antioxidative mechanism."( Ameliorative Effects of Kolaviron, a Biflavonoid Fraction from Garcinia Kola Seed, on Hepato-renal Toxicity of Anti-tuberculosis Drugs in Wistar Rats.
Adaramoye, OA; Adefisan, A; Adeyemi, O; Akanni, OO; Kehinde, AO; Oyinlola, I, 2016
)
" Eighty children with TBI received a 12-dose once-weekly isoniazid/rifapentine regimen; 79 (99%) completed therapy, 94% reported no adverse events, 1 child had mildly elevated transaminases but 1 adolescent later developed pulmonary TB."( Safety and Adherence for 12 Weekly Doses of Isoniazid and Rifapentine for Pediatric Tuberculosis Infection.
Cruz, AT; Starke, JR, 2016
)
"To assess whether increasing the dose of rifampicin (RMP) from 10 mg/kg to 15 or 20 mg/kg results in an increase in grade 3 or 4 hepatic adverse events and/or serious adverse events (SAE)."( A randomised Phase II trial to evaluate the toxicity of high-dose rifampicin to treat pulmonary tuberculosis.
Atwine, D; Bonnet, M; Borgulya, G; Burgos, M; Checkley, AM; de Fernandes, RA; de Patiño, IW; Dubash, F; Gonzales, T; Harrison, TS; Jindani, A; Mitchison, D; Patel, N; Shrestha, B, 2016
)
"No significant increase in adverse events occurred when the RMP dose was increased from 10 mg/kg to 15 mg/kg or 20 mg/kg."( A randomised Phase II trial to evaluate the toxicity of high-dose rifampicin to treat pulmonary tuberculosis.
Atwine, D; Bonnet, M; Borgulya, G; Burgos, M; Checkley, AM; de Fernandes, RA; de Patiño, IW; Dubash, F; Gonzales, T; Harrison, TS; Jindani, A; Mitchison, D; Patel, N; Shrestha, B, 2016
)
" Primary outcome was death and secondary outcomes were disability as assess by Barthel Index score and adverse events."( Safety and efficacy of additional levofloxacin in tuberculous meningitis: A randomized controlled pilot study.
Betai, S; Bhoi, SK; Kalita, J; Misra, UK, 2016
)
"The bacteriophage lambda replication initiation protein P exhibits a toxic effect on its Escherichia coli (E."( Lambda gpP-DnaB Helicase Sequestration and gpP-RpoB Associated Effects: On Screens for Auxotrophs, Selection for Rif(R), Toxicity, Mutagenicity, Plasmid Curing.
Banerjee, A; Chu, A; Hayes, C; Hayes, S; Rajamanickam, K; Wang, W, 2016
)
"Many adverse drug reactions are caused by the cytochrome P450 (CYP)-dependent activation of drugs into reactive metabolites."( Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
Jones, LH; Nadanaciva, S; Rana, P; Will, Y, 2016
)
"Anti-tuberculosis drug-induced hepatotoxicity (ATDH) is a serious adverse reaction to anti-tuberculosis (TB) treatment."( Association between TXNRD1 polymorphisms and anti-tuberculosis drug-induced hepatotoxicity in a prospective study.
He, JQ; Ji, GY; Liu, QQ; Sandford, AJ; Wang, Y; Wu, JC; Wu, SQ; Zhang, MM, 2016
)
" DR-TB treatment is complicated to administer and relies on the use of multiple toxic drugs, with potential for severe adverse drug reactions."( Severe adverse events during second-line tuberculosis treatment in the context of high HIV Co-infection in South Africa: a retrospective cohort study.
Berhanu, RH; Black, A; Evans, D; Firnhaber, C; Maitisa, N; Schnippel, K; Sinanovic, E, 2016
)
"Although modes of action (MOAs) play a key role in the understanding of the toxic mechanism of chemicals, the MOAs have not been investigated for antibiotics to green algae."( Toxicity of 13 different antibiotics towards freshwater green algae Pseudokirchneriella subcapitata and their modes of action.
Fu, L; Huang, T; Li, C; Su, L; Wang, S; Wang, X; Zhao, Y, 2017
)
" Safety was monitored by measuring the pro-inflammatory cytokines in their sputum, lung function test, blood chemistry and adverse events."( Evaluation of Proinflammatory Cytokines and Adverse Events in Healthy Volunteers upon Inhalation of Antituberculosis Drugs.
Juthong, S; Laohapojanart, N; Padmavathi, AR; Pungrassami, P; Ratanajamit, C; Srichana, T; Suwandecha, T, 2016
)
" Three patients could not conclude the 3HR treatment (13%), but only two had adverse effects (8."( Efficacy and safety of short-term treatment with isoniazid and rifampicin for latent tuberculosis infection in lung transplant candidates.
Guirao-Arrabal, E; Redel, J; Santos, F; Torre-Cisneros, J; Vaquero, JM, 2017
)
"Treatment of LTBI in lung transplant candidates using a short course of 3HR appears to be effective and safe in preventing posttransplant TB in lung transplant recipients."( Efficacy and safety of short-term treatment with isoniazid and rifampicin for latent tuberculosis infection in lung transplant candidates.
Guirao-Arrabal, E; Redel, J; Santos, F; Torre-Cisneros, J; Vaquero, JM, 2017
)
" These results were attributed to the combined toxic action of the released iron, silver ions and antibiotics."( Release and cytotoxicity studies of magnetite/Ag/antibiotic nanoparticles: An interdependent relationship.
Coy, E; Gapinski, J; Ivashchenko, O; Jurga, S; Peplinska, B; Woźniak, A, 2017
)
"First line antiTB drugs have several physical and toxic manifestations which limit their applications."( Conjugated and Entrapped HPMA-PLA Nano-Polymeric Micelles Based Dual Delivery of First Line Anti TB Drugs: Improved and Safe Drug Delivery against Sensitive and Resistant Mycobacterium Tuberculosis.
Bhaskar, N; Chauhan, DS; Gothwal, A; Gupta, U; Gupta, UD; Khan, I; Pachouri, PK; Upadhyay, S, 2017
)
" These data demonstrate that OA inhibited the transactivation of PXR and CAR, reduced the expression and function of CYP3A4 and CYP2B6, and may therefore serve as an effective agent for reducing probability adverse interactions between transcriptional inducers of CYP450 and therapeutic drugs."( Oleanolic Acid-Mediated Inhibition of Pregnane X Receptor and Constitutive Androstane Receptor Attenuates Rifampin-Isoniazid Cytotoxicity.
Chang, HY; Chen, CJ; Chen, JJ; Cheng, WK; Lee, YR; Lim, YP; Lin, YN, 2017
)
" The characteristics of RMR-TB were compared with those with adverse events to rifampin (RAE-TB)."( Treatment outcomes of rifampin-sparing treatment in patients with pulmonary tuberculosis with rifampin-mono-resistance or rifampin adverse events: A retrospective cohort analysis.
Jo, KW; Kim, WS; Lee, SD; Park, S; Shim, TS, 2017
)
" Nanotechnology and microbiology researchers are looking for new and safe nano drugs for eliminating Mycobacterium tuberculosis, the causative agent of tuberculosis."( Toxicity effects of AgZnO nanoparticles and rifampicin on Mycobacterium tuberculosis into the macrophage.
Dehghanpour, M; Fathizadeh, S; Jafari Nodooshan, S; Jafari, A; Kamalzadeh, M; Majidpour, A; Mosavari, N; Movahedzadeh, F; Novin Kashani, A; Rasouli Koohi, S; Safarkar, R, 2018
)
"The traditional treatment of tuberculosis (TB) infection (9 months of daily isoniazid [9H]) is safe but completion rates of <50% are reported."( Completion Rate and Safety of Tuberculosis Infection Treatment With Shorter Regimens.
Cruz, AT; Starke, JR, 2018
)
" We compared the frequency of completion and adverse events (AEs) in children receiving 3HP, 4R, and 9H; the latter 2 regimens could be administered by families (termed self-administered therapy [SAT]) or as directly observed preventive therapy (DOPT); 3HP was always administered under DOPT."( Completion Rate and Safety of Tuberculosis Infection Treatment With Shorter Regimens.
Cruz, AT; Starke, JR, 2018
)
" The anti-TB drugs of first choice were developed more than 4 decades ago and present several adverse effects, making the treatment of TB even more complicated and the development of new chemotherapeutics for this disease imperative."( New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity.
Aiub, CAF; Araujo-Lima, CF; Boechat, N; Castelo-Branco, FS; Costa, TEMM; Costa-Lima, MM; de Lima, EC; Domingos, JLO; Felzenszwalb, I; Gomes, KM; Henriques, MG; Lourenço, MCS; Penido, C; Pinto, AC, 2018
)
" We aimed to determine whether the INH/RPT-3 regimen had similar or lesser rates of adverse events compared to other LTBI regimens, namely INH for 9 months, INH for 6 months, rifampin for 3 to 4 months, and rifampin plus INH for 3 to 4 months."( A systematic review of adverse events of rifapentine and isoniazid compared to other treatments for latent tuberculosis infection.
Alvarez, GG; Barbeau, P; Hamel, C; Hutton, B; Pease, C; Skidmore, B; Wolfe, D; Yazdi, F, 2018
)
"gov, and Canadian Agency for Drugs and Technologies in Health's Gray Matters Light for randomized, postmarketing, and comparative nonrandomized studies of patients with confirmed LTBI that reported the frequency of at least 1 adverse event of relevance for a regimen of interest."( A systematic review of adverse events of rifapentine and isoniazid compared to other treatments for latent tuberculosis infection.
Alvarez, GG; Barbeau, P; Hamel, C; Hutton, B; Pease, C; Skidmore, B; Wolfe, D; Yazdi, F, 2018
)
" Although inconsistent event reporting and high heterogeneity limited comparisons, the adverse event profile of INH/RPT-3 appeared generally favorable."( A systematic review of adverse events of rifapentine and isoniazid compared to other treatments for latent tuberculosis infection.
Alvarez, GG; Barbeau, P; Hamel, C; Hutton, B; Pease, C; Skidmore, B; Wolfe, D; Yazdi, F, 2018
)
"While INH/RPT-3 had an overall low frequency of adverse events compared to INH monotherapy, reporting of adverse events for many regimens was limited meaning results should be interpreted cautiously."( A systematic review of adverse events of rifapentine and isoniazid compared to other treatments for latent tuberculosis infection.
Alvarez, GG; Barbeau, P; Hamel, C; Hutton, B; Pease, C; Skidmore, B; Wolfe, D; Yazdi, F, 2018
)
"The Clinical Trial for Uniform Multidrug Therapy for Leprosy Patients in Brazil (U-MDT/CT-BR), designed to evaluate the effectiveness of a six-months regimen, assessed the adverse effects caused by the drugs."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
"Describe adverse effects due to MDT in U-MDT/CT-BR, comparing the uniform regimen (U-MDT) to the current WHO regimen (R-MDT)."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
"2%) stopped dapsone intake due to adverse effects, of whom 16."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
"There was no statistical difference regarding adverse effects in the R-MDT and U-MDT groups but anemia was greater in patients from R-MDT/MB group, therefore adverse effects do not represent a constraint to recommend the six-month uniform regimen of treatment for all leprosy patients."( Clinical trial for uniform multidrug therapy for leprosy patients in Brazil (U-MDT/CT-BR): adverse effects approach.
Bührer-Sékula, S; Cruz, RCDS; Gonçalves, HS; Moraes, MEA; Penna, GO; Penna, MLF; Pontes, MAA; Stefani, MMA; Talhari, S, 2018
)
" The current standard treatment - 9 months of isoniazid - has been associated with poor adherence and toxic effects, which have hampered the effectiveness of the drug."( Safety and Side Effects of Rifampin versus Isoniazid in Children.
Adjobimey, M; Apriani, L; Benedetti, A; Diallo, T; Elwood, K; Fregonese, F; Gninafon, M; Hill, PC; Hornby, K; Li, PZ; Long, R; Marks, GB; Menzies, D; Obeng Baah, J; Ruslami, R; Schwartzman, K; Sow, O; Trajman, A; Valiquette, C; Wulandari, DA; Zielinski, D, 2018
)
" The primary outcome was adverse events of grade 1 to 5 that resulted in the permanent discontinuation of a trial drug."( Safety and Side Effects of Rifampin versus Isoniazid in Children.
Adjobimey, M; Apriani, L; Benedetti, A; Diallo, T; Elwood, K; Fregonese, F; Gninafon, M; Hill, PC; Hornby, K; Li, PZ; Long, R; Marks, GB; Menzies, D; Obeng Baah, J; Ruslami, R; Schwartzman, K; Sow, O; Trajman, A; Valiquette, C; Wulandari, DA; Zielinski, D, 2018
)
" There were no significant between-group differences in the rates of adverse events, with fewer than 5% of the children in the combined groups with grade 1 or 2 adverse events that were deemed to be possibly related to a trial drug."( Safety and Side Effects of Rifampin versus Isoniazid in Children.
Adjobimey, M; Apriani, L; Benedetti, A; Diallo, T; Elwood, K; Fregonese, F; Gninafon, M; Hill, PC; Hornby, K; Li, PZ; Long, R; Marks, GB; Menzies, D; Obeng Baah, J; Ruslami, R; Schwartzman, K; Sow, O; Trajman, A; Valiquette, C; Wulandari, DA; Zielinski, D, 2018
)
" 501 (98·0%) of 511 patients had at least one treatment-emergent adverse event."( Efficacy and safety of delamanid in combination with an optimised background regimen for treatment of multidrug-resistant tuberculosis: a multicentre, randomised, double-blind, placebo-controlled, parallel group phase 3 trial.
Balanag, V; Bielskiene, V; Cadena, E; Caoili, J; Cirule, A; Danilovits, M; Davidaviciene, E; Domente, L; Geiter, LJ; Gupta, R; Hafkin, J; Hittel, N; Lizarbe, V; Patientia, R; Petersen, C; Sanchez, E; Segura, P; Staples, S; Ticona, E; Variava, E; von Groote-Bidlingmaier, F; Wells, C; Yu, C, 2019
)
" Therefore, this side effect is thought to be unrecognized by most physicians."( Acute tubulointerstitial nephritis caused by rifampicin: An increasing and often overlooked side effect in elderly patients
.
Iwata, K; Nagata, M; Ohji, G, 2019
)
" Incidence rate of adverse effects was 19."( Efficacy and safety of cholecalciferol-augmented anti-tuberculosis therapy for treatment of naïve patients with pulmonary tuberculosis: A randomized, controlled, clinical study.
Abd-Ellatief, RB; Hasanain, AFA; Nafee, AMA; Zayed, AAH, 2019
)
" In addition, adding vitamin D3 to ATT provides extra protection against the hepatic and muscular adverse effects of ATT."( Efficacy and safety of cholecalciferol-augmented anti-tuberculosis therapy for treatment of naïve patients with pulmonary tuberculosis: A randomized, controlled, clinical study.
Abd-Ellatief, RB; Hasanain, AFA; Nafee, AMA; Zayed, AAH, 2019
)
" There were no adverse events related to rifampin."( Rifampin Pharmacokinetics and Safety in Preterm and Term Infants.
Anand, R; Benjamin, DK; Boakye-Agyeman, F; Cohen-Wolkowiez, M; Cotten, CM; Hudak, ML; Laughon, MM; Lewandowski, A; Poindexter, BB; Smith, PB; Sullivan, JE, 2019
)
" In conclusion, regimen including PZA seems to be safe for late elderly patients with pulmonary TB."( Safety of pyrazinamide-including regimen in late elderly patients with pulmonary tuberculosis: A prospective randomized open-label study.
Asaoka, M; Baba, T; Hagiwara, E; Katano, T; Kitamura, H; Komatsu, S; Ogura, T; Okuda, R; Sekine, A; Suido, Y, 2019
)
" We investigated the incidence of adverse events and cure rates according to HIV status for patients receiving standard TB therapy in the trial."( Toxicity related to standard TB therapy for pulmonary tuberculosis and treatment outcomes in the REMoxTB study according to HIV status.
Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; McHugh, TD; Mendel, CM; Meredith, SK; Mohapi, L; Murphy, ME; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD, 2019
)
" Grade 3 and 4 adverse events (AEs) were summarised by MedDRA System Organ Class."( Toxicity related to standard TB therapy for pulmonary tuberculosis and treatment outcomes in the REMoxTB study according to HIV status.
Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; McHugh, TD; Mendel, CM; Meredith, SK; Mohapi, L; Murphy, ME; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD, 2019
)
"HIV-positive patients receiving standard TB therapy in the REMoxTB study were at greater risk of adverse events during treatment but cure rates were similar when compared to a matched sample of HIV-negative patients."( Toxicity related to standard TB therapy for pulmonary tuberculosis and treatment outcomes in the REMoxTB study according to HIV status.
Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; McHugh, TD; Mendel, CM; Meredith, SK; Mohapi, L; Murphy, ME; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD, 2019
)
"An important problem limiting treatment of latent tuberculosis infection is the occurrence of adverse events with isoniazid."( Adverse events in adults with latent tuberculosis infection receiving daily rifampicin or isoniazid: post-hoc safety analysis of two randomised controlled trials.
Adjobimey, M; Benedetti, A; Campbell, JR; Cook, VJ; Eisenbeis, L; Fregonese, F; Johnston, JC; Menzies, D; Ruslami, R; Trajman, A; Valiquette, C, 2020
)
" The primary outcome evaluated was adverse events (including grade 1-2 rash and all events of grade 3-5) resulting in permanent discontinuation of study medication and judged possibly or probably related to study drug by a masked, independent, three-member adjudication panel (trial registration: NCT00170209; NCT00931736)."( Adverse events in adults with latent tuberculosis infection receiving daily rifampicin or isoniazid: post-hoc safety analysis of two randomised controlled trials.
Adjobimey, M; Benedetti, A; Campbell, JR; Cook, VJ; Eisenbeis, L; Fregonese, F; Johnston, JC; Menzies, D; Ruslami, R; Trajman, A; Valiquette, C, 2020
)
" Among those receiving isoniazid, 86 (2·7%) of 3205 had grade 1-2 rash or any grade 3-5 adverse events, more than the 50 (1·5%) of 3280 who had these events with rifampicin (risk difference -1·2%, 95% CI -1·9 to -0·5)."( Adverse events in adults with latent tuberculosis infection receiving daily rifampicin or isoniazid: post-hoc safety analysis of two randomised controlled trials.
Adjobimey, M; Benedetti, A; Campbell, JR; Cook, VJ; Eisenbeis, L; Fregonese, F; Johnston, JC; Menzies, D; Ruslami, R; Trajman, A; Valiquette, C, 2020
)
" With more widespread use of rifampicin, rare, but serious adverse events might be seen."( Adverse events in adults with latent tuberculosis infection receiving daily rifampicin or isoniazid: post-hoc safety analysis of two randomised controlled trials.
Adjobimey, M; Benedetti, A; Campbell, JR; Cook, VJ; Eisenbeis, L; Fregonese, F; Johnston, JC; Menzies, D; Ruslami, R; Trajman, A; Valiquette, C, 2020
)
" The ingestion of these first-line TB drugs are, however, not free of side effects, and are toxic to the liver, kidney, and central nervous system."( Metabolomics describes previously unknown toxicity mechanisms of isoniazid and rifampicin.
Combrink, M; du Preez, I; Loots, DT, 2020
)
" The main toxic effect of the substances was related to inhibition of mitochondrial dehydrogenases (succinate dehydrogenase and α-glycerol phosphate dehydrogenase) usually followed by suppression of activity of hydrolytic enzymes (acid phosphatase and non-specific esterase)."( Cytochemical Evaluation of the Toxic Effects of Combined Antituberculosis Substances on Metabolic State of Blood Lymphocytes.
Dolgushin, MV, 2020
)
" Incidents of systemic adverse reactions (SARs) and treatment interruption rates in an elderly group (≥60 years old) and a young group (<60 years old) were analyzed."( Safety and treatment completion of latent tuberculosis infection treatment in the elderly population-A prospective observational study in Taiwan.
Chen, CY; Feng, JY; Huang, WC; Lee, SS; Li, CP; Lin, CB; Lin, SM; Pan, SW; Shu, CC; Su, WJ; Tung, CL; Wang, TY; Wei, YF, 2020
)
" Owing to an unexpected high frequency of adverse events (70."( Efficacy and safety of weekly rifapentine and isoniazid for tuberculosis prevention in Chinese silicosis patients: a randomized controlled trial.
Cai, LM; Hong, JJ; Huang, XT; Jiang, T; Lin, MY; Ling, Q; Liu, XF; Ma, CL; Mao, JC; Pan, KC; Peng, GQ; Ruan, QL; Shao, LY; Shen, YJ; Wang, XD; Wang, XZ; Wu, J; Wu, TZ; Yang, QL; Zhang, WH, 2021
)
" The regimen must be used with caution because of the high rates of adverse effects."( Efficacy and safety of weekly rifapentine and isoniazid for tuberculosis prevention in Chinese silicosis patients: a randomized controlled trial.
Cai, LM; Hong, JJ; Huang, XT; Jiang, T; Lin, MY; Ling, Q; Liu, XF; Ma, CL; Mao, JC; Pan, KC; Peng, GQ; Ruan, QL; Shao, LY; Shen, YJ; Wang, XD; Wang, XZ; Wu, J; Wu, TZ; Yang, QL; Zhang, WH, 2021
)
" We report completion, drug-related adverse events (AE), and active tuberculosis incidence among people living with HIV; with renal failure or receiving immunosuppressants; using drugs or with hepatitis; with diabetes mellitus; consuming >1 alcoholic drink per week or current/former smokers; and with no health condition."( Safety and Efficacy of Rifampin or Isoniazid Among People With Mycobacterium tuberculosis Infection and Living With Human Immunodeficiency Virus or Other Health Conditions: Post Hoc Analysis of 2 Randomized Trials.
Al-Jahdali, H; Bah, B; Belo, M; Campbell, JR; Cook, VJ; Long, R; Menzies, D; Schwartzman, K; Trajman, A, 2021
)
"Rifampin appears to be safe and as effective as isoniazid across many populations with health conditions, including HIV."( Safety and Efficacy of Rifampin or Isoniazid Among People With Mycobacterium tuberculosis Infection and Living With Human Immunodeficiency Virus or Other Health Conditions: Post Hoc Analysis of 2 Randomized Trials.
Al-Jahdali, H; Bah, B; Belo, M; Campbell, JR; Cook, VJ; Long, R; Menzies, D; Schwartzman, K; Trajman, A, 2021
)
" Anemia was the most frequent severe adverse event (AE)."( Safety and Effectiveness of an All-Oral, Bedaquiline-Based, Shorter Treatment Regimen for Rifampicin-Resistant Tuberculosis in High Human Immunodeficiency Virus (HIV) Burden Rural South Africa: A Retrospective Cohort Analysis.
Bulti, AB; Dumicho, A; Furin, J; Isaakidis, P; Mbatha, M; Ohler, L; Shigayeva, A; Tack, I; White, K, 2021
)
" Since the introduction of new and repurposed anti-TB medications, the implementation of active TB Drug Safety Monitoring (aDSM) was a critical program component to help establish safety and manage all treatment related Serious Adverse Events (SAEs)."( Incidence rate and time to serious adverse events among rifampicin resistant tuberculosis patients in Georgia treated with new and repurposed anti-tuberculosis drugs, 2016-2018.
Buziashvili, M; Davtyan, H; Denisiuk, O; Gozalov, O; Hovhannesyan, A; Lomtadze, N; Sereda, Y, 2021
)
" Inhaled delivery of high-dose rifampicin was safe to rat lungs and liver suggesting its potential for localized as well as systemic drug delivery without toxicity concerns."( Studies on the safety and the tissue distribution of inhaled high-dose amorphous and crystalline rifampicin in a rat model.
Das, SC; Dummer, J; Hill, PC; Katare, R; Khadka, P; Sinha, S; Tucker, IG, 2021
)
" The aim was to describe the adverse effects of polychemotherapy, as well the most prevalent and most vulnerable populations."( Adverse effects of polychemotherapy for leprosy in 13 years of follow-up at a university hospital.
Brotas, AM; Carneiro, S; Daxbacher, EL; Tortelly, VD,
)
" No other adverse events were observed."( Safety and feasibility of 1 month of daily rifapentine plus isoniazid to prevent tuberculosis in children and adolescents: a prospective cohort study.
Amanullah, F; Becerra, MC; Fareed, U; Farooq, S; Hussain, H; Jaswal, M; Keshavjee, S; Khan, AJ; Khan, H; Malik, AA; Nasir, K; Safdar, N; Shahbaz, S, 2021
)
" We assessed effectiveness and predictors of drug adverse events (DAE) among patients treated with STR."( Effectiveness and Safety of a Shorter Treatment Regimen in a Setting with a High Burden of Multidrug-Resistant Tuberculosis.
Akopyan, K; Ciobanu, A; Gadoev, J; Hovhannesyan, A; Kalandarova, L; Parpieva, N; Sadirova, D; Trubnikov, A, 2021
)
"Effective yet safe treatment of latent tuberculosis is important for preventing the spread of tuberculosis and the progression to active disease in pediatric patients."( Adverse events associated with weekly short course isoniazid and rifapentine therapy in pediatric patients with latent tuberculosis: A chart and literature review.
Boyce, C; Huang, FS; Khalil, N; Kohlrieser, CM; Peck, GM; Schlaudecker, EP; Staat, MA, 2021
)
"In this retrospective chart review, pediatric patients ages 2-20 years receiving 3HP with DOT for latent tuberculosis experienced frequent adverse events, more severe adverse events such as anaphylaxis, and higher treatment discontinuation than that which has been previously reported in the literature."( Adverse events associated with weekly short course isoniazid and rifapentine therapy in pediatric patients with latent tuberculosis: A chart and literature review.
Boyce, C; Huang, FS; Khalil, N; Kohlrieser, CM; Peck, GM; Schlaudecker, EP; Staat, MA, 2021
)
"Our data suggests that the short course combination regimen for pediatric latent tuberculosis patients may have a higher adverse event rate than previously established."( Adverse events associated with weekly short course isoniazid and rifapentine therapy in pediatric patients with latent tuberculosis: A chart and literature review.
Boyce, C; Huang, FS; Khalil, N; Kohlrieser, CM; Peck, GM; Schlaudecker, EP; Staat, MA, 2021
)
" Secondary outcomes were clinical signs and symptoms of pulmonary TB and adverse drug reactions (ADRs) related to anti-TB agents."( Efficacy and safety of combined isoniazid-rifampicin-pyrazinamide-levofloxacin dry powder inhaler in treatment of pulmonary tuberculosis: A randomized controlled trial.
Kawkitinarong, K; Laohapojanart, N; Ratanajamit, C; Srichana, T, 2021
)
" Adverse events (AEs) related to oral anti-TB agents, (e."( Efficacy and safety of combined isoniazid-rifampicin-pyrazinamide-levofloxacin dry powder inhaler in treatment of pulmonary tuberculosis: A randomized controlled trial.
Kawkitinarong, K; Laohapojanart, N; Ratanajamit, C; Srichana, T, 2021
)
" Except for one patient with transient drug-induced hepatitis, no other serious adverse events were observed."( Efficacy and safety of rifampicin in patients with persistent hepatocellular secretory failure.
Lian, M; Ma, X; Miao, Q; Sheng, L; Shi, M; Wang, Q; Xiao, X, 2021
)
" A 3-month regimen of weekly isoniazid and rifapentine (3HP) is safe and effective for tuberculosis prevention in adults and children, including those with HIV, but 3HP has not been evaluated in pregnancy."( Pharmacokinetics and Safety of 3 Months of Weekly Rifapentine and Isoniazid for Tuberculosis Prevention in Pregnant Women.
Bradford, S; Britto, P; Chakhtoura, N; Chalermchockcharoentkit, A; Chipato, T; Dooley, KE; Gupta, A; Jayachandran, P; Kamthunzi, P; Langat, D; Mathad, JS; Montepiedra, G; Norman, J; Patil, S; Popson, S; Rouzier, V; Savic, R; Townley, E; Wiesner, L; Zhang, N, 2022
)
" There were no drug-related serious adverse events, treatment discontinuations, or tuberculosis cases in women or infants."( Pharmacokinetics and Safety of 3 Months of Weekly Rifapentine and Isoniazid for Tuberculosis Prevention in Pregnant Women.
Bradford, S; Britto, P; Chakhtoura, N; Chalermchockcharoentkit, A; Chipato, T; Dooley, KE; Gupta, A; Jayachandran, P; Kamthunzi, P; Langat, D; Mathad, JS; Montepiedra, G; Norman, J; Patil, S; Popson, S; Rouzier, V; Savic, R; Townley, E; Wiesner, L; Zhang, N, 2022
)
"It can be concluded from this meta-analysis that there is no significant relation of high-dose rifampicin with adverse events and the reduction of mortality in TBM patients."( Safety and efficacy of high-dose rifampicin in the management of tuberculosis meningitis: Systematic review and meta-analysis.
Abay, SM; Charlie, L; Goretti, M; Mlera, RN; Mwango, S; Tesfaye, A,
)
"Rifampicin doses of 40 mg/kg in adults are safe and well tolerated, may shorten anti-TB treatment and improve outcomes, but have not been evaluated in children."( Pharmacokinetics and safety of high-dose rifampicin in children with TB: the Opti-Rif trial.
Aarnoutse, RE; Denti, P; Draper, HR; Fairlie, L; Garcia-Prats, AJ; Hesseling, AC; Karlsson, MO; Masenya, M; Norman, J; Schaaf, HS; Svensson, EM; van der Laan, LE; Wiesner, L; Winckler, J, 2021
)
" Approximately half of participants had an adverse event related to study rifampicin; none was grade 3 or higher."( Pharmacokinetics and safety of high-dose rifampicin in children with TB: the Opti-Rif trial.
Aarnoutse, RE; Denti, P; Draper, HR; Fairlie, L; Garcia-Prats, AJ; Hesseling, AC; Karlsson, MO; Masenya, M; Norman, J; Schaaf, HS; Svensson, EM; van der Laan, LE; Wiesner, L; Winckler, J, 2021
)
"High rifampicin doses in children achieved target exposures and the doses evaluated were safe over 2 weeks."( Pharmacokinetics and safety of high-dose rifampicin in children with TB: the Opti-Rif trial.
Aarnoutse, RE; Denti, P; Draper, HR; Fairlie, L; Garcia-Prats, AJ; Hesseling, AC; Karlsson, MO; Masenya, M; Norman, J; Schaaf, HS; Svensson, EM; van der Laan, LE; Wiesner, L; Winckler, J, 2021
)
" Adverse drug events were more frequent in the older age group (22."( Safety of latent tuberculosis infection treatment in older patients with immune-mediated inflammatory diseases.
Chung, C; Jo, KW; Kim, YJ; Shim, TS, 2022
)
"LTBI treatment is generally safe in older patients with IMIDs, especially with respect to hepatotoxicity."( Safety of latent tuberculosis infection treatment in older patients with immune-mediated inflammatory diseases.
Chung, C; Jo, KW; Kim, YJ; Shim, TS, 2022
)
" All serious adverse events and adverse events of special interest (AESI), leading to a treatment change, or judged significant by a clinician, were systematically monitored and documented."( Safety and Effectiveness Outcomes From a 14-Country Cohort of Patients With Multi-Drug Resistant Tuberculosis Treated Concomitantly With Bedaquiline, Delamanid, and Other Second-Line Drugs.
Ahmed, S; Bastard, M; Franke, MF; Grium Tefera, D; Hewison, C; Holtzman, D; Huerga, H; Islam, S; Jacques Leblanc, G; Khan, PY; Khan, U; Kumsa, A; Lachenal, N; Leonovich, O; Mamsa, S; Manzur-Ul-Alam, M; Melikyan, N; Mitnick, CD; Myint, Z; Osso, E; Padayachee, S; Rafi Siddiqui, M; Rashitov, M; Rich, ML; Salahuddin, N; Salia, G; Sánchez, E; Serobyan, A; Seung, KJ; Varaine, F; Vetushko, D; Yeghiazaryan, L, 2022
)
"Concomitant use of Bdq and Dlm, along with linezolid and clofazimine, is safe and effective for MDR/RR-TB patients with extensive disease."( Safety and Effectiveness Outcomes From a 14-Country Cohort of Patients With Multi-Drug Resistant Tuberculosis Treated Concomitantly With Bedaquiline, Delamanid, and Other Second-Line Drugs.
Ahmed, S; Bastard, M; Franke, MF; Grium Tefera, D; Hewison, C; Holtzman, D; Huerga, H; Islam, S; Jacques Leblanc, G; Khan, PY; Khan, U; Kumsa, A; Lachenal, N; Leonovich, O; Mamsa, S; Manzur-Ul-Alam, M; Melikyan, N; Mitnick, CD; Myint, Z; Osso, E; Padayachee, S; Rafi Siddiqui, M; Rashitov, M; Rich, ML; Salahuddin, N; Salia, G; Sánchez, E; Serobyan, A; Seung, KJ; Varaine, F; Vetushko, D; Yeghiazaryan, L, 2022
)
" RFB and RFM are both effective and safe to use in LDLT recipients with active TB."( Comparative analysis of the drug-drug interaction between immunosuppressants, safety and efficacy of rifabutin from rifampicin-based Anti-TB treatment in living donor liver transplant recipients with active tuberculosis.
Chan, YC; Chen, CL; Co, JS; Encarnacion, DD; Lee, WF; Lin, CC; Lin, TL; Salvador, NG; Wang, YC; Wu, CC, 2021
)
"Hepatotoxicity is a well-known adverse effect of many substances, with toxicity often resulting from interactions of drugs with other drug-like substances."( Implications for herbal polypharmacy: coumarin-induced hepatotoxicity increased through common herbal phytochemicals astragaloside IV and atractylenolide I.
Britza, SM; Byard, RW; Musgrave, IF, 2022
)
" The outcomes of interest were culture conversion and incidence of adverse events."( Efficacy and safety of daily treatments for drug-susceptible pulmonary tuberculosis: a systematic review and network meta-analysis.
Beraldi-Magalhães, F; Fernandez-Llimos, F; Imazu, P; Pontarolo, R; Santos, JM; Tonin, FS, 2022
)
" The use of rifapentine 450 mg instead of rifampicin in the standard regimen demonstrated to be statistically safer than all other options for serious adverse events (e."( Efficacy and safety of daily treatments for drug-susceptible pulmonary tuberculosis: a systematic review and network meta-analysis.
Beraldi-Magalhães, F; Fernandez-Llimos, F; Imazu, P; Pontarolo, R; Santos, JM; Tonin, FS, 2022
)
"The WHO standard regimen remains an overall effective and safe alternative for DS-TB."( Efficacy and safety of daily treatments for drug-susceptible pulmonary tuberculosis: a systematic review and network meta-analysis.
Beraldi-Magalhães, F; Fernandez-Llimos, F; Imazu, P; Pontarolo, R; Santos, JM; Tonin, FS, 2022
)
" Ten children experienced 27 adverse events at least possibly related to bedaquiline; no adverse events led to bedaquiline withdrawal."( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022
)
"The evaluated doses of bedaquiline in children ≥ 6 years of age were safe but achieved slightly lower plasma concentrations compared to adults receiving the recommended dose, possibly due to delayed food intake relative to bedaquiline administration."( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022
)
"We used the Korea Adverse Event Reporting System (KAERS) database (2009-2018)."( Analysis of Adverse Drug Reactions to First-Line Anti-Tuberculosis Drugs Using the Korea Adverse Event Reporting System.
Byeon, SJ; Choi, JH; Chung, SJ, 2022
)
" A shorter, less toxic and more efficacious regimen would improve outcomes for people with rifampicin-resistant tuberculosis."( TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tubercul
Berry, C; du Cros, P; Fielding, K; Gajewski, S; Kazounis, E; McHugh, TD; Merle, C; Moore, DAJ; Motta, I; Nyang'wa, BT, 2022
)
"TB-PRACTECAL is an ambitious trial using adaptive design to accelerate regimen assessment and bring novel treatments that are effective and safe to patients quicker."( TB-PRACTECAL: study protocol for a randomised, controlled, open-label, phase II-III trial to evaluate the safety and efficacy of regimens containing bedaquiline and pretomanid for the treatment of adult patients with pulmonary multidrug-resistant tubercul
Berry, C; du Cros, P; Fielding, K; Gajewski, S; Kazounis, E; McHugh, TD; Merle, C; Moore, DAJ; Motta, I; Nyang'wa, BT, 2022
)
"We investigated adverse events in patients with prosthetic joint infections receiving combination therapy with linezolid, rifampicin, and clindamycin for ≥ 7 days."( Safety of linezolid, rifampicin, and clindamycin combination therapy in patients with prosthetic joint infection.
Kitaoka, A; Kobayashi, S; Ogura, T; Tagawa, S; Yasu, T, 2022
)
"Refractory rifampicin-resistant/multidrug resistant/extensively-drug resistant tuberculosis (RR/MDR/XDR-TB) were defined as patients infected with Mycobacterium tuberculosis (MTB) resistant to rifampicin(RR-TB), or at least resistant to rifampicin and isoniazid (MDR-TB) or added resistant to fluoroquinolones (FQs) and one of second line injectable agents (XDR-TB), a patient for whom an effective regimen (fewer than 4 effective agents due to adverse events (AEs) or multiple drug resistances) cannot be developed."( Effectiveness and safety of bedaquiline-containing regimens for treatment on patients with refractory RR/MDR/XDR-tuberculosis: a retrospective cohort study in East China.
Fan, L; Li, YP; Sun, WW; Xiao, HP; Yang, Y; Zhang, SJ; Zhang, ZM; Zhang, ZS, 2022
)
" Meanwhile, the types and incidence of adverse effects associated with LZD were evaluated."( Linezolid-related adverse effects in the treatment of rifampicin resistant tuberculosis: a retrospective study.
Chen, G; Cui, D; Hu, X; Shi, L; Wang, D, 2023
)
" Of 106 evaluated, 95 (90%) were successfully treated, six (6%) were lost-to-follow-up, one (1%) died, and four (4%) had treatment failure, including three with permanent regimen change owing to adverse events (AE) and one with culture reversion."( Effectiveness and safety of bedaquiline-based, modified all-oral 9-11-month treatment regimen for rifampicin-resistant tuberculosis in Vietnam.
Decroo, T; Hoang, TTT; Le, THM; Merle, CSC; Nguyen, BH; Nguyen, NL; Nguyen, TMP; Nguyen, VN; Pedrazzoli, D, 2023
)
"4:1:1) to 3 treatment arms (1, standard of care [SOC]; 2, SOC + additional rifampicin [up to 35 mg/kg/d] + linezolid 1200 mg/d reducing after 28 days to 600 mg/d; 3, as per arm 2 + aspirin 1000 mg/d) for 56 days, when the primary outcome of adverse events of special interest (AESI) or death was assessed."( A Phase 2A Trial of the Safety and Tolerability of Increased Dose Rifampicin and Adjunctive Linezolid, With or Without Aspirin, for Human Immunodeficiency Virus-Associated Tuberculous Meningitis: The LASER-TBM Trial.
Aziz, S; Banderker, IA; Black, J; Bremer, M; Candy, S; Crede, T; Daroowala, R; Davis, AG; Denti, P; Goliath, R; Jackson, A; Jason Liang, C; Kadernani, Y; Koekemoer, S; Lai Sai, L; Lai, RPJ; Maartens, G; Maxebengula, M; Meintjes, G; Moosa, MS; Naude, J; Offiah, C; Raubenheimer, P; Sihoyiya, T; Stegmann, S; Stek, C; Szymanski, P; Vallie, Y; Vorster, I; Wahl, G; Wasserman, S; Wilkinson, RJ, 2023
)
"Rifampicin-resistant tuberculosis (RR-TB) treatment requires combination treatment, which frequently causes serious adverse events and globally results in not much more than 60% treatment success."( Safety, effectiveness, and adherence of a short and all-oral treatment regimen for the treatment of rifampicin-resistant tuberculosis in Niger: a study protocol of a pragmatic randomised clinical trial with stratified block randomisation.
Adehossi, E; Decroo, T; Gagara-Issoufou, A; Halidou-Moussa, S; Mamadou, S; Maman Lawan, I; Ortuño-Gutiérrez, N; Piubello, A; Souleymane, MB; Soumana, A; Van Deun, A, 2022
)
" Thus, we conclude that diosmin may be used along with anti-tubercular drugs (isoniazid and rifampin) in tuberculosis patients to overcome their hepatotoxic adverse effect."( Hepatoprotective potential of diosmin against hepatotoxic effect of isoniazid and rifampin in wistar rats.
Ahmed, RA; Alam, MF; Alqahtani, SS; Alruwaili, MN; Alshahrani, S; Anwer, T; Jali, A; Moni, SS,
)
"Within a randomized clinical trial, clinical response and adverse events of high-dose rifampicin (900-1200 mg/day) plus doxycycline 100 mg twice daily were compared with standard-dose rifampicin (600 mg/day) plus doxycycline 100 mg twice daily in 120 patients with brucellosis."( Comparing efficacy and safety of high-dose and standard-dose rifampicin in the treatment of brucellosis: a randomized clinical trial.
Abbasi, A; Farbod, F; Jafari, S; Khalili, H; Rahmani, H; Salehi, M, 2023
)
" The most common adverse events of the treatment were nausea (37."( Comparing efficacy and safety of high-dose and standard-dose rifampicin in the treatment of brucellosis: a randomized clinical trial.
Abbasi, A; Farbod, F; Jafari, S; Khalili, H; Rahmani, H; Salehi, M, 2023
)
"The rate of clinical response in patients with brucellosis who were treated with high-dose rifampicin plus standard-dose doxycycline was significantly higher than in the patients who received the standard doses of rifampicin and doxycycline, without further adverse events."( Comparing efficacy and safety of high-dose and standard-dose rifampicin in the treatment of brucellosis: a randomized clinical trial.
Abbasi, A; Farbod, F; Jafari, S; Khalili, H; Rahmani, H; Salehi, M, 2023
)
" Eligible studies compared 3HP or 4R to 6 months or 9 months of isoniazid and reported treatment completion, adverse events, or incidence of tuberculosis disease."( Completion, safety, and efficacy of tuberculosis preventive treatment regimens containing rifampicin or rifapentine: an individual patient data network meta-analysis.
Belknap, R; Benedetti, A; Borisov, A; Campbell, JR; Chaisson, RE; Chan, PC; Martinson, N; Menzies, D; Nahid, P; Scott, NA; Sizemore, E; Sterling, TR; Villarino, ME; Wang, JY; Winters, N, 2023
)
" For treatment-related adverse events leading to drug discontinuation, risks were higher for 3HP than for 4R for adverse events of any severity (aRR 2·86 [2·12-4·21]; aRD 0·03 [0·02-0·05]) and for grade 3-4 adverse events (aRR 3·46 [2·09-6·17]; aRD 0·02 [0·01-0·03])."( Completion, safety, and efficacy of tuberculosis preventive treatment regimens containing rifampicin or rifapentine: an individual patient data network meta-analysis.
Belknap, R; Benedetti, A; Borisov, A; Campbell, JR; Chaisson, RE; Chan, PC; Martinson, N; Menzies, D; Nahid, P; Scott, NA; Sizemore, E; Sterling, TR; Villarino, ME; Wang, JY; Winters, N, 2023
)
"In the absence of RCTs, our individual patient data network meta-analysis indicates that 3HP provided an increase in treatment completion over 4R, but was associated with a higher risk of adverse events."( Completion, safety, and efficacy of tuberculosis preventive treatment regimens containing rifampicin or rifapentine: an individual patient data network meta-analysis.
Belknap, R; Benedetti, A; Borisov, A; Campbell, JR; Chaisson, RE; Chan, PC; Martinson, N; Menzies, D; Nahid, P; Scott, NA; Sizemore, E; Sterling, TR; Villarino, ME; Wang, JY; Winters, N, 2023
)

Pharmacokinetics

Study was to determine if there is a pharmacokinetic interaction when amprenavir is given with rifabutin or rifampin and to determine the effects of these drugs on the ERMBT.

ExcerptReference
"Two-stage pharmacokinetic studies were conducted in patients suffering from pulmonary tuberculosis treated with rifampicin (RMP)."( Studies on pharmacokinetics of rifampicin in the body of patients with pulmonary tuberculosis.
Pawlowska, I; Pniewski, T, 1979
)
" The average elimination half-life of hexobarbital had decreased from 624 to 262 min and that of tolbutamide from 292 to 160 min following rifampicin treatment."( Stimulation of drug metabolism by rifampicin in patients with cirrhosis or cholestasis measured by increased hexobarbital and tolbutamide clearance.
Breimer, DD; Richter, E; Zilly, W, 1977
)
" The average elimination half-life of hexobarbital had decreased from 325 to 122 min and of tolbutamide from 418 to 183 min following rifampicin treatment."( Induction of drug metabolism in man after rifampicin treatment measured by increased hexobarbital and tolbutamide clearance.
Breimer, DD; Richter, E; Zilly, W, 1975
)
" On average, the Cmax then is approximately 300 ng/ml, which is achieved rapidly within 30 min after drug intake."( Pharmacokinetic profile of nicorandil in humans: an overview.
Frydman, A, 1992
)
" The absorption rate constant was found to be lower and the time to reach peak concentration was longer after drug administration at 24."( Chronopharmacokinetics of rifampicin.
Avachat, MK; Rambhau, D; Rao, BR; Rao, JV; Rao, VV, 1992
)
" The results suggested that the pharmacokinetic behavior of Iso in rats belonged to a 2-compartment model."( Effects of rifampicin on pharmacokinetics of isoniazid and its metabolite acetylhydrazine in rats.
Cheng, WB; Li, D; Wang, ZY; Zhang, RL, 1992
)
" Mean peak ciprofloxacin concentrations and other pharmacokinetic parameters were not altered significantly by coadministration of either rifampin or clindamycin."( Crossover assessment of serum bactericidal activity and pharmacokinetics of ciprofloxacin alone and in combination in healthy elderly volunteers.
Deeter, RG; Gross, JS; Swanson, KA; Weinstein, MP, 1991
)
"The here described investigations show correspondingly that the administration of isoniazid, rifampicin and pyrazinamide in a fixed combination of the administration of the individual substances is bioequivalent under pharmacokinetic aspects."( [Pharmacokinetic aspects of tuberculosis therapy with a fixed combination of rifampicin, isoniazide and pyrazinamide].
Lode, H; Schaberg, T, 1991
)
"The purpose of this clinical study was to investigate the influence of concomitant drug therapy with ciprofloxacin and rifampin on the individual pharmacokinetic profile of each agent in elderly patients."( Multiple-dose pharmacokinetics of concurrent oral ciprofloxacin and rifampin therapy in elderly patients.
Chandler, MH; Korvick, JA; Muder, RR; Rapp, RP; Toler, SM, 1990
)
" In order to determine the endoplasmatic reticulum enzyme function, 6-beta-hydroxycortisol excretion and antipyrine pharmacokinetic parameters were evaluated."( Comparative effects of rifampin and/or probenecid on the pharmacokinetics of temazepam and nitrazepam.
Brockmeyer, NH; Goos, M; Klimek, K; Mertins, L; Ohnhaus, EE, 1990
)
"We investigated the pharmacokinetic interaction of RMP (administered from the first day of treatment onwards), PZA (given from the second day onwards), and INH (day 17 onwards) in ten, previously untreated patients with pulmonary tuberculosis (five slow acetylators and five fast acetylators)."( [Clinico-pharmacokinetic interactions of rifampicin, pyrazinamide and isoniazide].
Loos, U; Musch, E; Schwabe, HK, 1990
)
"0748 hr-1), elimination half-life (average reduction, 13."( Influence of rifampin on tocainide pharmacokinetics in humans.
Celestin, C; Foster, JR; Patterson, JH; Powell, JR; Rice, TL, 1989
)
" Numerous pharmacokinetic drug interactions of potential clinical significance exist because other drugs may induce or inhibit the metabolism of CyA."( Cyclosporine pharmacokinetic drug interactions.
Baciewicz, AM; Baciewicz, FA, 1989
)
" To show distribution profiles of antituberculous drugs in patients in organs and tissues of experimental animals after their administration alone or in combination, pharmacokinetic parameters of isoniazid and rifampicin were studied."( [Pharmacokinetics of isoniazid and rifampicin in an experiment and in clinical practice].
Anisimova, NB; Karkishchenko, NN; Khoron'ko, VV; Lavrushko, AN; Vorob'ev, VS, 1988
)
" So, the main pharmacokinetic parameters of doxycycline (200 mg/day orally) in seven patients before and after rifampicin association (10 mg/kg/day)."( [Effects of rifampicin on the pharmacokinetics of doxycycline].
Bernard, E; Beziau, H; Chichmanian, RM; Dellamonica, P; Fournier, JP; Garraffo, R; Lapalus, P, 1987
)
" Three days after rifampicin the elimination half-life of dapsone was reduced from 40."( Influence of once-monthly rifampicin and daily clofazimine on the pharmacokinetics of dapsone in leprosy patients in Nigeria.
Pieters, FA; Woonink, F; Zuidema, J, 1988
)
"This study assessed the potential pharmacokinetic interaction between rifampicin and ketoconazole, two drugs used to treat the increasingly common combination of Mycobacterium tuberculosis and Candida albicans infection in AIDS patients."( Pharmacokinetic study of the interaction between rifampicin and ketoconazole.
Doble, N; Keal, EE; Lush, M; Rowland-Hill, C; Shaw, R; Warnock, DW, 1988
)
" The pharmacokinetic analysis of oral rifampicin was performed using a one-compartment open model with absorption."( The effects of peptidoglycan, a pyrogenic constituent of gram-positive microorganisms, on the pharmacokinetics of rifampicin.
Lavický, J; Rasková, H; Rotta, J; Urbanová, Z; Vanĕcek, J, 1988
)
" The metabolic clearance rate (MCR) and plasma half-life of this material were measured before and after 6 days of rifampicin treatment (600 mg/day) in seven patients with Addison's disease due to tuberculosis."( Pharmacokinetics of aldosterone in patients with Addison's disease: effect of rifampicin treatment on glucocorticoid and mineralocorticoid metabolism.
Benker, G; Mönig, H; Ohnhaus, EE; Pagel, H; Reinwein, D; Schulte, HM, 1987
)
" The plasma elimination half-life of lidocaine was markedly shortened after rifampicin treatment, due to a diminished volume of distribution."( Influence of enhanced alpha-1-acid glycoprotein concentration on protein binding, pharmacokinetics and antiarrhythmic effect of lidocaine in the dog.
Belpaire, FM; Bogaert, MG; De Rick, AF; Dello, C, 1987
)
"02 micrograms kg-1 given intravenously 1 h prior to the oral administration of RFP (20 mg kg-1) induced considerable pharmacokinetic changes."( Bacterial pyrogens of different origin and pharmacokinetics of rifampicin.
Celeda, L; Krecek, J; Kvĕtina, J; Lavický, J; Rasková, H; Urbanová, Z; Vanĕcek, J, 1987
)
" However, the pharmacokinetic data relevant to the antibiotic administration in the above doses were satisfactorily described by the biexponential equation."( [Modelling of rifampicin pharmacokinetics in experimental animals administered the drug intravenously and internally].
Firsov, AA; Fomina, IP; Stepanov, VM; Umnova, LV, 1986
)
" The elimination half-life was 17."( Pharmacokinetics of rifampin given as a single oral dose in foals.
Brown, MP; Castro, LA; Gronwall, R; Houston, AE; Miles, N, 1986
)
" In spite of this minimal portion the course of pharmacokinetic processes can distinctly be learned from its alterations."( [The pharmacokinetics of rifampicin in the intermittent treatment of patients with pulmonary tuberculosis. 1. Excretion of rifampicin in the urine].
Eule, H; Iwainsky, H; Werner, E; Winsel, K, 1985
)
"A comparative pharmacokinetic study of Lositril (rifampicin) was carried out in six multibacillary and twelve paucibacillary leprosy cases."( Effect of clofazimine and dapsone on rifampicin (Lositril) pharmacokinetics in multibacillary and paucibacillary leprosy cases.
Gandhi, IS; Mehta, J; Sane, SB; Wamburkar, MN,
)
"The unique pharmacokinetic properties of rifampin in humans are discussed in this review."( Pharmacokinetics and metabolism of rifampin in humans.
Acocella, G,
)
" By an iteration process, based on non-linear regression analysis, the following pharmacokinetic parameters were calculated: Vd, Ka, Ke, T0."( Pharmacokinetics of antituberculosis drugs after oral isolated and simultaneous administration in triple combination.
Janků, I; Papezová, E; Stastná, J; Tousek, J; Zítková, L, 1983
)
"The good results gotten employing short-term (6 months) medication regimes with rifampin, isoniazid and an initial supplement (2 months) of streptomycin and pyrazinamide, gave an impulse to pharmacodynamic research."( [Pharmacokinetics of antitubercular agents in man].
Acocella, G, 1984
)
"A pharmacokinetic study was carried out in 18 male patients in order to assess the blood concentrations of rifampicin after intravenous administration of 3 different doses (600, 900 and 1200 mg) over 3 different periods of infusion (1, 2 and 3 hours)."( Pharmacokinetic study on intravenous rifampicin in man.
Acocella, G; Conti, R; Pagani, V; Pallanza, R; Perna, G; Segre, G; Simone, P, 1984
)
" Terminal plasma half-life ranged between 14 and 18 hours; the compound is eliminated mainly via the bile with the feces (92% of dose)."( Pharmacokinetics of rifapentine, a new long lasting rifamycin, in the rat, the mouse and the rabbit.
Assandri, A; Cristina, T; Ratti, B, 1984
)
" After rifampicin treatment the elimination half-life of antipyrine had decreased in all patients from 12."( Influence of rifampicin treatment on antipyrine clearance and metabolite formation in patients with tuberculosis.
Bakker, W; Breimer, DD; Meerburg-Van der Torren, JE; Teunissen, MW, 1984
)
" The comparative pharmacokinetic properties of rifampicin and clindamycin demonstrated that the peak serum and abscess levels reached with rifampicin were significantly higher than those of clindamycin."( Therapeutic efficacy and pharmacokinetic properties of rifampicin in a Bacteroides fragilis intra-abdominal abscess.
Fu, KP; Kimble, EF; Konopka, EA; Lasinski, ER; Zoganas, HC, 1984
)
" The same applies to the Cmax value (1."( Pharmacokinetic studies of rifampicin in the elderly.
Advenier, C; Bidet, D; Gobert, C; Houin, G; Richelet, S; Tillement, JP, 1983
)
" The reduction in area under the time concentration curve of free, non-protein bound prednisolone was 56."( Changes in prednisolone pharmacokinetics and protein binding during treatment with rifampicin.
Bergrem, H; Refvem, OK, 1983
)
"The pharmacodynamic properties of levofloxacin (an optically active isomer of ofloxacin), ofloxacin, and ciprofloxacin, alone and in combination with rifampin, were evaluated over 24 to 48 h against clinical isolates of methicillin-susceptible and -resistant Staphylococcus aureus (MSSA 1199 and MRSA 494, respectively) in an in vitro infection model."( Pharmacodynamics of levofloxacin, ofloxacin, and ciprofloxacin, alone and in combination with rifampin, against methicillin-susceptible and -resistant Staphylococcus aureus in an in vitro infection model.
Kaatz, GW; Kang, SL; McGrath, BJ; Rybak, MJ; Seo, SM, 1994
)
" There were significant changes in caffeine plasma half-life (6."( The influence of rifampin treatment on caffeine clearance in healthy man.
Generet, K; Marschall, HU; Matern, S; Wietholtz, H; Zysset, T, 1995
)
" Pharmacokinetic parameters (mean +/- SEM) were: Cmax 13."( Determination of oral rifampin pharmacokinetic parameters in Mexicans and comparison with other populations: absence of evidence for interethnic variability.
Castañeda-Hernández, G; Flores-Murrieta, FJ; Herrera, JE; Hong, E, 1994
)
" The calculated CLH values were then compared to literature values of clearance (CL) to the same metabolite obtained during pharmacokinetic studies in humans."( Predicting the hepatic clearance of xenobiotics in humans from in vitro data.
Hoener, BA, 1994
)
"h/liter) and the terminal half-life of fleroxacin (11."( Influence of rifampin on fleroxacin pharmacokinetics.
Dayer, P; Leemann, T; Lew, DP; Portmann, R; Schrenzel, J; Weidekamm, E, 1993
)
" Serial IV pharmacokinetic studies of prednisolone (1 mg/kg) in groups of 3 patients over a 1 month period of rifampin co-treatment or after its withdrawal, revealed significant changes in the area under the curve, the total clearance, the non-renal clearance and the half-life."( Time course of the changes in prednisolone pharmacokinetics after co-administration or discontinuation of rifampin.
Chong, WS; Jang, IJ; Kim, S; Lee, JS; Lee, KH; Shin, JG; Shin, SG, 1993
)
" Pharmacokinetic variables for rifampin determined using the HPLC method were comparable to variables reported from earlier studies utilizing a microbiological assay."( Pharmacokinetics of single intravenous and single and multiple dose oral administration of rifampin in mares.
Kohn, CW; Kowalski, JJ; Powers, J; Sams, R; Wallace, S, 1993
)
"A potential pharmacokinetic interaction between rifampin (Rimactan, Rifadin) and zidovudine (AZT, Retrovir) was investigated in the population of human immunodeficiency virus-infected patients at our hospital."( Pharmacokinetic interaction between rifampin and zidovudine.
Beijnen, JH; Burger, DM; Koks, CH; Meenhorst, PL, 1993
)
" For the above penicillins pharmacokinetic data are scarce, and clinical experience is limited."( Pharmacokinetics and pharmacodynamics of antistaphylococcal antibiotics in continuous ambulatory peritoneal dialysis patients.
Keller, E, 1993
)
" Plasma levodopa and levodopa metabolite pharmacokinetic profiles were determined using standard techniques."( A clinical and pharmacokinetic case study of an interaction of levodopa and antituberculous therapy in Parkinson's disease.
O'Connell, MT; Patsalos, PN; Quinn, NP; Wenning, GK, 1995
)
" The coadministration of rifampin resulted in a 18 fold decrease of the Cmax of itraconazole [from 113."( [Pharmacokinetic interaction between itraconazole and rifampin in Yucatan miniature pigs].
Cavalier, A; Elkhaili, H; Jehl, F; Kaltenbach, G; Levêque, D; Monteil, H; Peter, JD; Salmon, J; Salmon, Y, 1996
)
"To compare the pharmacokinetic parameters and the clinical efficacy of isoniazid, administered in 10 mg/kg or 5 mg/kg to children suffering from pulmonary tuberculosis."( Pharmacokinetics of isoniazid in pulmonary tuberculosis--a comparative study at two dose levels.
Chopra, K; Roy, V; Tekur, U, 1996
)
"Rifabutin is structurally similar to rifampin, but there are important pharmacokinetic differences between the two drugs."( The clinical pharmacokinetics of rifabutin.
Blaschke, TF; Skinner, MH, 1996
)
" Theophylline concentrations were determined for 46 h after each dose, and pharmacokinetic parameters were determined."( Induction of theophylline clearance by rifampin and rifabutin in healthy male volunteers.
Bruzzese, VL; Gillum, JG; Israel, DS; Polk, RE; Sesler, JM, 1996
)
"We compared the pharmacodynamic activities of levofloxacin versus vancomycin, with or without rifampin, in an in vitro model with infected platelet-fibrin clots simulating vegetations."( Pharmacodynamics of once- or twice-daily levofloxacin versus vancomycin, with or without rifampin, against Staphylococcus aureus in an in vitro model with infected platelet-fibrin clots.
Palmer, SM; Rybak, MJ, 1996
)
"The aim of this study was to assess the pharmacokinetics and subsequent pharmacodynamic interaction of MPC-1304, a dihydropyridine Ca2+ antagonist, with other drugs in animal experiments."( Interaction of some drugs on the pharmacokinetics or pharmacodynamics of MPC-1304, a dihydropyridine Ca2+ antagonist.
Miyake, H; Miyoshi, K; Nakano, M; Nishizaki, J; Umeno, Y; Yoshida, K,
)
"In the bioavailability studies with drugs biotransformed to biologically active metabolities only the concentrations of the parent drug (PD) are usually taken into account even when the pharmacokinetic data on the metabolite(s) (M) are available."( [Correlation between pharmacokinetic parameters of rifampicin and its biologically active metabolite as related to estimation of the relative bioavailability of the antibiotic].
Dombrovskiĭ, VS; Firsov, AA; Gagaeva, EV; Kadenatsi, IB; Strachunskiĭ, LS, 1996
)
"The pharmacodynamic effects of amikacin, imipenem, ofloxacin, rifampin, and vancomycin were studied on the slime-producing, oxacillin-resistant strain Staphylococcus epidermidis ATCC 35984 growing in Mueller Hinton broth or, in order to inhibit growth, incubated in phosphate-buffered saline."( Pharmacodynamic effects of antibiotics and antibiotic combinations on growing and nongrowing Staphylococcus epidermidis cells.
Hanberger, H; Nilsson, LE; Svensson, E, 1997
)
" A one-compartment open model with first-order absorption and elimination was used as the structural pharmacokinetic model."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
"The pharmacokinetic interaction of oral rifampicin (1200 mg) and oral nifedipine (10 mg capsules), given as single doses, was investigated in six healthy volunteers (mean age 28."( The effect of single does of rifampicin on the pharmacokinetics of oral nifedipine.
Abdu-Aguye, I; Mustapha, A; Ndanusa, BU, 1997
)
" time curve (AUC), the maximum concentration, or the terminal half-life (t1/2) of isoniazid, rifampin, and pyrazinamide."( Pharmacokinetics of antimycobacterial drugs in patients with tuberculosis, AIDS, and diarrhea.
Aoki, FY; Choudhri, SH; Gathua, S; Hawken, M; Long, R; Minyiri, GO; Sahai, J; Sitar, DS; Watkins, W, 1997
)
" The pharmacokinetic behaviors of INH, RIF, and PZA were well described by the three methods used."( Population pharmacokinetic modeling of isoniazid, rifampin, and pyrazinamide.
Bulpitt, AE; Jaresko, GS; Jelliffe, RW; Keung, AC; Peloquin, CA; Yong, CL, 1997
)
" Maximum plasma concentration of rifapentine was lower, time to maximum plasma concentration (tmax) was greater, and elimination half-life (t 1/2) was longer in the patients with moderate-to-severe hepatic dysfunction than in those with mild-to-moderate dysfunction."( Pharmacokinetics of rifapentine in patients with varying degrees of hepatic dysfunction.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
"This study was undertaken to characterize the pharmacokinetic profiles of rifapentine and its active metabolite, 25-desacetlyl rifapentine, in elderly men."( Single-dose pharmacokinetics of rifapentine in elderly men.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" The control group consisted of 20 healthy, young (18-45 years) males volunteers from a previous, single-dose (600 mg) rifapentine pharmacokinetic study."( Single-dose pharmacokinetics of rifapentine in elderly men.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" Disposition of rifapentine was monophasic with a mean terminal half-life of 19."( Single-dose pharmacokinetics of rifapentine in elderly men.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
"Because the aged-related changes in the pharmacokinetic profile of rifapentine observed in this study were modest and unlikely to be associated with toxicity, no dosage adjustments for this antibiotic are recommended in elderly patients."( Single-dose pharmacokinetics of rifapentine in elderly men.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" Plasma samples were obtained at frequent intervals for up to 72 hr after the dose to determine the pharmacokinetic (PK) parameters of rifapentine and its active metabolite, 25-desacetyl-rifapentine."( Single-dose pharmacokinetics of rifapentine in women.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" Small differences were found in mean tmax (0."( Pharmacokinetics of dolasetron with coadministration of cimetidine or rifampin in healthy subjects.
Arumugham, T; Cramer, MB; Dimmitt, DC; Keung, A; Weir, SJ, 1999
)
"Based on the small changes in the pharmacokinetic parameters of dolasetron and its active metabolites, as well as the favorable safety results, no dosage adjustments for dolasetron mesylate are recommended with concomitant administration of cimetidine or rifampin."( Pharmacokinetics of dolasetron with coadministration of cimetidine or rifampin in healthy subjects.
Arumugham, T; Cramer, MB; Dimmitt, DC; Keung, A; Weir, SJ, 1999
)
" A pharmacokinetic interaction with rifampin, an antituberculosis agent and potent inducer of CYP3A4 and P-glycoprotein, and tacrolimus was evaluated in six healthy male volunteers."( Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers.
Bekersky, I; Dressler, D; Fisher, RM; Hebert, MF; Marsh, CL, 1999
)
"05) and the Cmax by 57% (P<0."( Interactions of buspirone with itraconazole and rifampicin: effects on the pharmacokinetics of the active 1-(2-pyrimidinyl)-piperazine metabolite of buspirone.
Kivistö, KT; Lamberg, TS; Neuvonen, PJ, 1999
)
"001]) and the elimination half-life (t1/2) by 38% (P < ."( The effect of rifampin on the pharmacokinetics of oral and intravenous ondansetron.
Kivistö, KT; Neuvonen, PJ; Villikka, K, 1999
)
" Pharmacokinetic data from a previously published healthy volunteer study were used for comparison."( Pharmacokinetics of rifapentine in subjects seropositive for the human immunodeficiency virus: a phase I study.
Eller, MG; Keung, AC; Nicolau, DP; Nightingale, CH; Owens, RC; Weir, SJ, 1999
)
"An open randomized cross-over study was conducted in 8 healthy male volunteers to study the pharmacokinetic pattern and the safety of a 300-mg single oral dose of a new 3-azinomethyl-rifamycin (USAN rifametane, SPA-S-565) compared with 300 mg of conventional rifampicin."( Phase I pharmacokinetic study of a new 3-azinomethyl-rifamycin (rifametane) as compared to rifampicin.
Ajay, S; Bruzzese, T; Cooverji, ND; Gogtay, N; Gokhale, P; Kshirsagar, NA; Potkar, C,
)
" Multiple doses of trikatu also reduced the Cmax and delayed the Tmax of rifampicin although not to a statistically significant level."( Effect of trikatu, an Ayurvedic prescription, on the pharmacokinetic profile of rifampicin in rabbits.
Bhargava, VK; Garg, SK; Karan, RS, 1999
)
"In the present study, Diabecon (D-400), a herbomineral anti-diabetic preparation, was studied for its pharmacokinetic interaction with the commonly used drugs rifampicin and nifedipine."( Pharmacokinetic interaction of Diabecon (D-400) with rifampicin and nifedipine.
Gopumadhavan, S; Mitra, SK; Sundaram, R; Venkataranganna, MV,
)
" Subsequently model-independent methods were used to determine the pharmacokinetic profiles for each subject."( Rifapentine pharmacokinetics in adolescents.
Abdel-Rahman, S; Johnson, K; Kauffman, RE; Kearns, GL; Marshall, JD, 1999
)
" The Cmax and the elimination half life were reduced 3 times."( Rifampicin treatment greatly increases the apparent oral clearance of quinidine.
Brøsen, K; Damkier, P; Hansen, LL, 1999
)
" These data provide a pharmacokinetic rationale for extended-interval dosing."( Single-dose intrapulmonary pharmacokinetics of rifapentine in normal subjects.
Conte, JE; Golden, JA; Kipps, J; Lin, ET; McQuitty, M; Zurlinden, E, 2000
)
"The objective of this study was to determine if there is a pharmacokinetic interaction when amprenavir is given with rifabutin or rifampin and to determine the effects of these drugs on the erythromycin breath test (ERMBT)."( Pharmacokinetic Interaction between amprenavir and rifabutin or rifampin in healthy males.
Brophy, DF; Chittick, GE; Israel, DS; Kristoff, D; Lou, Y; Patron, R; Polk, RE; Sadler, BM; Stein, DS; Symonds, WT, 2001
)
" Rifampicin pharmacokinetic studies were carried out on day 1 and day 15."( Effect of indinavir on the pharmacokinetics of rifampicin in HIV-infected patients.
Jaruratanasirikul, S; Sriwiriyajan, S, 2001
)
" Treatment with ciprofloxacin significantly increased the half-life and also significantly decreased the maximum peak concentration of rifampicin."( Rifampicin pharmacokinetics with and without ciprofloxacin.
Afonne, OJ; Agbasi, PU; Obi, E; Ofoefule, SI; Orisakwe, OE; Orish, CN,
)
" However, cytochrome P-450 content and the pharmacokinetic parameters of diazepam were not changed in the RFP + INH group."( [Effects of rifampin and isoniazid on the pharmacokinetics of diazepam in rabbits].
Long, CF; Lou, YC; Zhang, Y, 1997
)
" Pharmacokinetic parameters were calculated with noncompartmental methods, and t tests were used for comparisons between the phases and between the smokers and nonsmokers."( Effect of rifampin and tobacco smoking on the pharmacokinetics of ropivacaine.
Ahonen, J; Jokinen, MJ; Neuvonen, PJ; Olkkola, KT, 2001
)
"There were no statistically significant differences in the area under the plasma concentration-time curve (AUC), plasma clearance (CL), or half-life (t(1/2)) of ropivacaine between the smokers and nonsmokers."( Effect of rifampin and tobacco smoking on the pharmacokinetics of ropivacaine.
Ahonen, J; Jokinen, MJ; Neuvonen, PJ; Olkkola, KT, 2001
)
" Everolimus half-life was reduced significantly, from an average of 32 hours to 24 hours."( Effect of rifampin on apparent clearance of everolimus.
Figueiredo, J; Hartmann, S; Kovarik, JM; Port, A; Rordorf, C; Rouilly, M, 2002
)
" The pharmacokinetic profile of repaglinide and the improvements in post-prandial hyperglycaemia and overall glycaemic control make repaglinide suitable for administration preprandially, with the opportunity for flexible meal arrangements, including skipped meals, without the risk of hypoglycaemia."( Clinical pharmacokinetics and pharmacodynamics of repaglinide.
Hatorp, V, 2002
)
"To evaluate the pharmacokinetic interactions between efavirenz and rifampicin (rifampin) in patients with HIV infection and tuberculosis."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
"Nonblind, randomised, pharmacokinetic study."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
"Plasma concentrations of efavirenz and rifampicin were quantified by using validated high performance liquid chromatography assays, and pharmacokinetic parameter values were determined by noncompartmental methods."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
"There was a correlation between the pharmacokinetic parameters of efavirenz and the dose/kg administered."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
" We present detailed pharmacokinetic (PK) data for amikacin (AMK), ethambutol (EMB), INH, pyrazinamide (PZA), RIF, and levofloxacin in four female bongos."( Population pharmacokinetics of antituberculous drugs and treatment of Mycobacterium bovis infection in bongo antelope (Tragelaphus eurycerus isaaci).
Aguilar, R; Auclair, B; Maslow, JN; Mikota, SK; Peloquin, CA, 2002
)
" Data from controlled release experiments in vitro were used, and the concentration time courses of the antimicrobials in serum were calculated by pharmacokinetic simulations."( Pharmacokinetics of the antimicrobial agents rifampicin and miconazole released from a loaded central venous catheter.
Güttler, K; König, DP; Korenkov, M; Rump, AF; Schierholz, JM; Yücel, N, 2003
)
" Peak plasma concentration (Cmax), Tmax, elimination half-life (t1/2e) and AUC0- infinity of alginate drugs were significantly higher than those of free drugs."( Alginate-based oral drug delivery system for tuberculosis: pharmacokinetics and therapeutic effects.
Garg, SK; Khuller, GK; Sharma, S, 2003
)
" Intensive steady-state pharmacokinetic sampling from baseline to 8 hours revealed very low plasma concentrations of nelfinavir: area under the plasma concentration-time curve (AUC(0-24)) <10% of adult population values for 750 mg every 8 hours and nonquantifiable concentrations of nelfinavir's principal metabolite (M8)."( Ritonavir-enhanced pharmacokinetics of nelfinavir/M8 during rifampin use.
Bergshoeff, AS; Burger, DM; Geelen, SP; Wolfs, TF, 2003
)
" Ritonavir resolved the pharmacokinetic interaction between rifampin and nelfinavir by boosting nelfinavir and, especially, M8 concentrations."( Ritonavir-enhanced pharmacokinetics of nelfinavir/M8 during rifampin use.
Bergshoeff, AS; Burger, DM; Geelen, SP; Wolfs, TF, 2003
)
" The results have shown that the pattern of absorption, plasma concentrations and pharmacokinetic parameters were found to be very similar after administration of the drugs in free and fixed combinations."( The pharmacokinetic factors and bioavailability of rifampicin, isoniazid and pyrazinamid fixed in one dose capsule.
Augustynowicz-Kopeć, E; Niemirowska-Mikulska, H; Zwolska, Z,
)
"5 mg/kg) administration of MDZ, and pharmacokinetic parameters were estimated by fitting to a noncompartmental model."( Expression of the human CYP3A4 gene in the small intestine of transgenic mice: in vitro metabolism and pharmacokinetics of midazolam.
Akiyama, TE; Cheung, C; Elizondo, G; Feigenbaum, L; Gonzalez, FJ; Granvil, CP; Krausz, KW; Yu, AM, 2003
)
"Potential alternatives, including linezolid, adjunctive rifampin, and moxifloxacin, were evaluated against vancomycin-tolerant (P9802-020) and vancomycin-susceptible clinical isolates of Streptococcus pneumoniae in an in vitro pharmacodynamic model."( Linezolid and vancomycin, alone and in combination with rifampin, compared with moxifloxacin against a multidrug-resistant and a vancomycin-tolerant Streptococcus pneumoniae strain in an in vitro pharmacodynamic model.
Cha, R; Rybak, MJ, 2003
)
"The concentration and half-life of theophylline was decreased and its clearance was increased significantly at days 5-7 after administration of antituberculosis agents compared to before the therapy was started."( The clearance of theophylline is increased during the initial period of tuberculosis treatment.
Ahn, HC; Lee, YC, 2003
)
" Compared to administration of repaglinide alone, concomitant ketoconazole increased mean AUC0-infinity for repaglinide by 15% and mean Cmax by 7%."( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide.
Hansen, KT; Hatorp, V; Thomsen, MS, 2003
)
"Limited information exists on the pharmacokinetic (PK)-pharmacodynamic (PD) relationships of drugs against Mycobacterium tuberculosis."( Pharmacokinetics-pharmacodynamics of rifampin in an aerosol infection model of tuberculosis.
Balasubramanian, V; Bharat, S; Gaonkar, S; Jayaram, R; Jayashree, R; Kantharaj, E; Kaur, P; Mahesh, BN; Nandi, V; Shandil, RK; Suresh, BL, 2003
)
"The relationships between the pharmacokinetic properties of quinine during a 7-day treatment course and the therapeutic response were studied in 30 adult patients with uncomplicated falciparum malaria monitored for > or = 28 days."( Quinine pharmacokinetic-pharmacodynamic relationships in uncomplicated falciparum malaria.
Huyakorn, S; Jantra, A; Looareesuwan, S; Pukrittayakamee, S; Stepniewska, K; Wanwimolruk, S; White, NJ, 2003
)
" The ratios of least squares means (LSM) and 90% confidence intervals for enfuvirtide and enfuvirtide metabolite pharmacokinetic parameters (AUC12h, Cmax, Ctrough) were estimated in the presence and absence of rifampicin."( Lack of enzyme-inducing effect of rifampicin on the pharmacokinetics of enfuvirtide.
Boyd, MA; Buss, N; Dorr, A; Kinchelow, T; Kolis, S; Nieforth, K; Patel, IH; Ruxrungtham, K; Zhang, X, 2003
)
" Pharmacokinetic evaluations of steady-state concentrations of indinavir and ritonavir were performed before and after administration of rifampin (300 mg every day for 4 days)."( Pharmacokinetic interaction between rifampin and the combination of indinavir and low-dose ritonavir in HIV-infected patients.
Andersen, AB; Brøsen, K; Gerstoft, J; Justesen, US; Klitgaard, NA; Pedersen, C, 2004
)
" Rifampicin had no significant effect on the peak concentration, elimination half-life or renal clearance of pravastatin."( Effect of rifampicin on pravastatin pharmacokinetics in healthy subjects.
Backman, JT; Kyrklund, C; Neuvonen, M; Neuvonen, PJ, 2004
)
" Pharmacokinetic parameters were determined based on non-compartmental model analysis using the computer program KINETICA."( Influence of rifampicin pretreatment on the pharmacokinetics of celecoxib in healthy male volunteers.
Chandrasekhar, K; Jayasagar, G; Krishna Kumar, M; Madhusudan Rao, Y, 2003
)
" The present pharmacokinetic study supports further trials to determine the optimal rifapentine dose for treatment of tuberculosis."( Pharmacokinetics of rifapentine at 600, 900, and 1,200 mg during once-weekly tuberculosis therapy.
Bock, N; Burman, WJ; Goldberg, S; Hayden, K; Khan, A; Peloquin, CA; Sterling, TR; Vernon, A; Weiner, M; Weis, S; Zhao, Z, 2004
)
"Prospective nonblinded pharmacokinetic study."( Effect of sex and AIDS status on the plasma and intrapulmonary pharmacokinetics of rifampicin.
Conte, JE; Golden, JA; Kipps, JE; Lin, ET; Zurlinden, E, 2004
)
"Coadministration of lopinavir-ritonavir, an antiretroviral protease inhibitor, at the standard dose (400/100 mg twice a day [BID]) with the antituberculous agent rifampin is contraindicated because of a significant pharmacokinetic interaction due to induction of cytochrome P450 3A by rifampin."( Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers.
Bertz, R; Boeree, MJ; Burger, DM; Colbers, EP; Hekster, YA; Koopmans, PP; la Porte, CJ; Voncken, DS; Wikstrom, K, 2004
)
" The pharmacokinetic profile of intravenous midazolam was characterized before and after itraconazole administration (200 mg once daily for 4 days) and also after rifampin (INN, rifampicin) pretreatment (600 mg once daily for 10 days), with a washout period of 2 weeks in between."( Effect of the CYP3A5 genotype on the pharmacokinetics of intravenous midazolam during inhibited and induced metabolic states.
Cho, JY; Chung, JY; Hong, KS; Jang, IJ; Kim, JR; Lim, HS; Liu, KH; Oh, DS; Shin, JG; Shin, SG; Yi, SY; Yu, KS, 2004
)
"The pharmacokinetic profiles of midazolam and of its hydroxy metabolites did not show differences between the genotype groups under basal and induced metabolic conditions."( Effect of the CYP3A5 genotype on the pharmacokinetics of intravenous midazolam during inhibited and induced metabolic states.
Cho, JY; Chung, JY; Hong, KS; Jang, IJ; Kim, JR; Lim, HS; Liu, KH; Oh, DS; Shin, JG; Shin, SG; Yi, SY; Yu, KS, 2004
)
" Blood samples were collected from the first 12 patients in each group and pharmacokinetic parameters for fluconazole were calculated."( Effect of rifampicin on the pharmacokinetics of fluconazole in patients with AIDS.
Panomvana Na Ayudhya, D; Tansuphaswadikul, S; Thanompuangseree, N, 2004
)
"Coadministration of rifampicin with fluconazole caused significant changes in the pharmacokinetic parameters of fluconazole."( Effect of rifampicin on the pharmacokinetics of fluconazole in patients with AIDS.
Panomvana Na Ayudhya, D; Tansuphaswadikul, S; Thanompuangseree, N, 2004
)
" Pharmacokinetic data for 23 subjects were thus evaluable."( Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers.
Buffels, R; Burger, DM; Droste, JA; Hekster, YA; Kearney, BP; Vanhorssen, PJ; Verweij-van Wissen, CP, 2005
)
" The pharmacokinetic and pharmacodynamic profiles of intravenous lorazepam were characterized before and after inhibition with 600 mg valproate once daily for 4 days and after induction with rifampin (INN, rifampicin) pretreatment (600 mg once daily for 10 days), with a washout period of 10 days between."( Effect of the UGT2B15 genotype on the pharmacokinetics, pharmacodynamics, and drug interactions of intravenous lorazepam in healthy volunteers.
Cho, JY; Chung, JY; Jang, IJ; Jung, HR; Kim, JR; Lim, KS; Shin, SG; Yu, KS, 2005
)
" In this investigation, physico-chemical characterization, single dose pharmacokinetic studies and the permeability of rifampicin under physiological conditions in the rat were studied to trace the possible reasons for its variable absorption."( Implication of biopharmaceutics and pharmacokinetics of rifampicin in variable bioavailability from solid oral dosage forms.
Agrawal, S; Panchagnula, R, 2005
)
" Based on these findings, three clinical studies were carried out to investigate pharmacokinetic drug interactions in vivo with gefitinib."( Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol.
Laight, A; Leadbetter, J; McKillop, D; Ranson, M; Smith, RP; Swaisland, HC; Wild, MJ, 2005
)
" Comparisons of area under the serum concentration time curves from 0 to 3 h (AUC(0-3)), AUC(0-24), Cmax, apparent oral clearance of digoxin (CL/F), and elimination half-life were used to assess the effects of milk thistle, black cohosh, rifampin, and clarithromycin on digoxin pharmacokinetics."( Effect of milk thistle (Silybum marianum) and black cohosh (Cimicifuga racemosa) supplementation on digoxin pharmacokinetics in humans.
Barone, GW; Breen, P; Carrier, J; Cheboyina, S; Gurley, BJ; Hubbard, MA; Song, PF; Tong, Y; Williams, DK; Yates, CR, 2006
)
" Special reference was made to studying the influence of previous exposure to rifampin (RIF) and the variability in pharmacokinetic parameters between patients and between occasions and the influence of different covariates."( Population pharmacokinetics of rifapentine and its primary desacetyl metabolite in South African tuberculosis patients.
Langdon, G; McFadyen, L; McIlleron, H; Simonsson, US; Smith, P; Wilkins, J, 2005
)
"Evaluation of sources of pharmacokinetic variation can facilitate optimization of tuberculosis treatment regimens by identification of avoidable sources of variation and of risk factors for low or high drug concentrations in patients."( Determinants of rifampin, isoniazid, pyrazinamide, and ethambutol pharmacokinetics in a cohort of tuberculosis patients.
Burger, A; Folb, PI; McIlleron, H; Norman, J; Smith, P; Wash, P, 2006
)
" ATV was administered orally (10 mg/kg) and intravenously (2 mg/kg) to rats in the absence and presence of a single intravenous dose of RIF (20 mg/kg), and pharmacokinetic parameters were compared between control and RIF-treatment groups."( Pharmacokinetics of atorvastatin and its hydroxy metabolites in rats and the effects of concomitant rifampicin single doses: relevance of first-pass effect from hepatic uptake transporters, and intestinal and hepatic metabolism.
Benet, LZ; Huang, Y; Lau, YY; Okochi, H, 2006
)
" Pharmacokinetic parameters were determined using a model-independent approach."( Pharmacokinetics of rifapentine in children.
Abdel-Rahman, SM; Blake, MJ; Jacobs, RF; Kearns, GL; Lowery, NK; Sterling, TR, 2006
)
"To study the effect of oral administration of crude aqueous extract of garlic for 14 days on pharmacokinetic parameters of isoniazid and rifampicin."( Effect of oral administration of crude aqueous extract of garlic on pharmacokinetic parameters of isoniazid and rifampicin in rabbits.
Dhamija, P; Malhotra, S; Pandhi, P, 2006
)
" Baseline pharmacokinetic parameters for single-dose isoniazid and rifampicin were calculated from plasma drug concentrations obtained at various time intervals after dosing."( Effect of oral administration of crude aqueous extract of garlic on pharmacokinetic parameters of isoniazid and rifampicin in rabbits.
Dhamija, P; Malhotra, S; Pandhi, P, 2006
)
"Administration of crude aqueous extract of garlic significantly altered the pharmacokinetic parameters for isoniazid."( Effect of oral administration of crude aqueous extract of garlic on pharmacokinetic parameters of isoniazid and rifampicin in rabbits.
Dhamija, P; Malhotra, S; Pandhi, P, 2006
)
" Comparisons of area under the curve (AUC)((0-3)), AUC((0-24)), C(max,) CL/F, and elimination half-life were used to assess the effects of goldenseal, kava kava, rifampin, and clarithromycin on digoxin pharmacokinetics."( Effect of goldenseal (Hydrastis canadensis) and kava kava (Piper methysticum) supplementation on digoxin pharmacokinetics in humans.
Barone, GW; Breen, P; Cheboyina, S; Gurley, BJ; Hubbard, MA; Stuart, LB; Swain, A; Tong, Y; Williams, DK; Yates, CR, 2007
)
" A randomized, placebo controlled crossover oral pharmacokinetic study was conducted in 12 healthy male human volunteers and in vitro (everted sac) and in situ (intestinal loop) studies were conducted in rats to study the role of P-gp."( Effect of ketoconazole and rifampicin on the pharmacokinetics of ranitidine in healthy human volunteers: a possible role of P-glycoprotein.
Gundu, J; Machavaram, KK; Yamsani, MR, 2006
)
" This study demonstrates the intracellular and extracellular killing activity of antimycobacterial drugs in a pharmacokinetic intracellular in vitro model."( Evaluation of an intracellular pharmacokinetic in vitro infection model as a tool to assess tuberculosis therapy.
Cappelletty, DM, 2007
)
" A complete pharmacokinetic evaluation of the steady-state concentrations of atazanavir and ritonavir was performed."( Pharmacokinetic interaction between rifampicin and ritonavir-boosted atazanavir in HIV-infected patients.
Blanco, JL; Gatell, JM; López-Púa, Y; Mallolas, J; Martínez, E; Nomdedeu, M; Sarasa, M; Soriano, A, 2007
)
"In all three cases, more than 50% of the time the atazanavir level was below the minimum recommended trough plasma level (150 ng/mL according to current pharmacokinetic guidelines) to inhibit HIV wild-type replication."( Pharmacokinetic interaction between rifampicin and ritonavir-boosted atazanavir in HIV-infected patients.
Blanco, JL; Gatell, JM; López-Púa, Y; Mallolas, J; Martínez, E; Nomdedeu, M; Sarasa, M; Soriano, A, 2007
)
" On average, rifampin increased atrasentan peak plasma concentrations by 150% and reduced its terminal half-life by 77% (P<."( Dual effects of rifampin on the pharmacokinetics of atrasentan.
Achari, R; Carr, RA; Doan, TT; Jankowski, JR; Katz, DA; Locke, CS; Sleep, DJ; Wang, P; Xiong, H, 2007
)
" A full pharmacokinetic curve for rifampin, pyrazinamide, and ethambutol was recorded after 6 weeks of daily TB treatment."( Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
Aarnoutse, RE; Alisjahbana, B; Nijland, HM; Parwati, I; Ruslami, R; van Crevel, R, 2007
)
" EFV levels in plasma were assayed by high-performance liquid chromatography (HLPC) predose (C(trough)) and at 1, 2, 3, 4, 5, 6, 8, 10, 11, 12, 13, 14, 16, 18, 22 and 24 hours post-dose, and pharmacokinetic parameters were determined by non-compartmental methods."( Multiple-dose pharmacokinetics of efavirenz with and without the use of rifampicin in HIV-positive patients.
Caligaris, S; Capone, S; Carosi, G; Carvalho, AC; Cusato, M; De Iaco, G; Manfrin, M; Matteelli, A; Regazzi, M; Tomasoni, L; Villani, P, 2007
)
" We performed an open-label, single-arm study to assess the safety and pharmacokinetic interactions of the HIV protease inhibitor atazanavir coadministered with rifampin."( Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
Acosta, EP; Agarwala, S; Alston-Smith, B; Bertz, R; Child, M; Gerber, JG; Haas, DW; Hosey, L; Kendall, MA; Koletar, SL; Zolopa, AR, 2007
)
" The present work investigated the influence of RMP and PYR on the pharmacokinetic parameters of INH when groups of rats were pre-treated for 21 days with INH alone or in combination with RMP and/or PYR, in the following amounts per kg body weight: INH 100 mg; INH 100 mg+RMP 100 mg; INH 100 mg+PYR 350 mg; INH 100 mg+PYR 350 mg+RMP 100 mg."( The effect of rifampicin and pyrazinamide on isoniazid pharmacokinetics in rats.
Baldan, HM; Brunetti, IL; De Rosa, HJ; Machado, RG; Ximenes, VF, 2007
)
" Lopinavir pharmacokinetic measures (median [interquartile range]) for children with and without rifampicin, respectively, were maximum concentration (Cmax) of 10."( Effect of rifampicin on lopinavir pharmacokinetics in HIV-infected children with tuberculosis.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2008
)
" Although the median Cmax and AUC0-12 were lowered by 26% and 31%."( Effect of rifampicin on lopinavir pharmacokinetics in HIV-infected children with tuberculosis.
Egbers, C; Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2008
)
" A compartmental pharmacokinetic model was developed using nonlinear mixed-effects modeling."( Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
Karlsson, MO; Langdon, G; McIlleron, H; Pillai, G; Savic, RM; Simonsson, US; Smith, PJ; Wilkins, JJ, 2008
)
" pharmacokinetic data on 670 drugs representing, to our knowledge, the largest publicly available set of human clinical pharmacokinetic data."( Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
Lombardo, F; Obach, RS; Waters, NJ, 2008
)
" Pharmacokinetic sampling was performed on day 7 of TMC207 administration up to 24 h postdose."( Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
Allen, J; De Beule, K; De Marez, T; Diacon, AH; Donald, PR; Kerstens, R; Koul, A; McNeeley, DF; Mthiyane, TC; Patientia, RF; Reddy, C; Rustomjee, R; van Heeswijk, R; Venter, A, 2008
)
"Free drug serum concentrations of minocycline associated with the doses given to humans (100 mg every 12 hours for 24 hours) were simulated in an in vitro hollow-fiber pharmacokinetic model."( Pharmacodynamics of minocycline against Staphylococcus aureus in an in vitro pharmacokinetic model.
Bowker, KE; Macgowan, AP; Noel, AR, 2008
)
" Compound (S)-33a was advanced into a pharmacodynamic model in cynomolgus monkeys, where it inhibited adipose 11beta-HSD1 activity after being orally administered."( Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
Bartberger, MD; Bercot, EA; Chen, M; Cupples, R; Emery, M; Fotsch, C; Fretland, J; Guram, A; Hale, C; Han, N; Hayashi, M; Hickman, D; Hungate, RW; Komorowski, R; Liu, Q; Matsumoto, G; St Jean, DJ; Tu, H; Ursu, S; Véniant, M; Wang, M; Xu, G; Ye, Q; Yuan, C; Zhang, J; Zhang, X, 2008
)
" A complete pharmacokinetic study was conducted with 19 HIV-TB patients on two occasions (with and without RMP)."( CYP2B6 G516T polymorphism but not rifampin coadministration influences steady-state pharmacokinetics of efavirenz in human immunodeficiency virus-infected patients in South India.
Anitha, S; Gomathi, C; Hemanth Kumar, AK; Kumar, P; Menon, P; Narendran, G; Rajasekaran, S; Ramachandran, G; Ramesh, K; Swaminathan, S, 2009
)
" Efavirenz Cmin was not significantly different during vs."( Effect of rifampicin on efavirenz pharmacokinetics in HIV-infected children with tuberculosis.
Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2009
)
" The substantial proportion of participants with estimated Cmin <1 mg/L could result in the rapid emergence of efavirenz-resistant mutations and treatment failure."( Effect of rifampicin on efavirenz pharmacokinetics in HIV-infected children with tuberculosis.
Eley, BS; Maartens, G; McIlleron, HM; Meyers, TM; Nuttall, JJ; Ren, Y; Smith, PJ, 2009
)
" We used population pharmacokinetic modeling and Monte Carlo simulation to describe and explore the pulmonary pharmacokinetics and pharmacodynamics of rifampin (RIF; rifampicin)."( Population modeling and Monte Carlo simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of rifampin in lungs.
Bourguignon, L; Conte, JE; Goutelle, S; Jelliffe, RW; Maire, PH; Van Guilder, M, 2009
)
" Pharmacokinetic studies of higher dosages of rifampin are urgently needed in children to assist in placing the dosage of rifampin used in childhood on a more scientific foundation."( Rifampin pharmacokinetics in children, with and without human immunodeficiency virus infection, hospitalized for the management of severe forms of tuberculosis.
Cilliers, K; Donald, PR; Hussey, GD; Labadarios, D; Maritz, JS; McIlleron, H; Schaaf, HS; Smith, P; Willemse, M, 2009
)
" Pharmacokinetic studies were performed with formulations delivered to guinea pigs by intratracheal insufflation and compared to oral and intravenous delivery of rifampicin."( Formulation and pharmacokinetics of self-assembled rifampicin nanoparticle systems for pulmonary delivery.
Durbin, D; Edwards, DA; Elbert, KJ; Garcia-Contreras, L; Hickey, AJ; Padilla, DJ; Peloquin, CA; Sung, JC; Verberkmoes, JL, 2009
)
" Two pharmacokinetic studies were performed in healthy subjects: study 1 examined the effect of administration of 600-mg rifampin once daily on the pharmacokinetics of a single dose of 400-mg raltegravir, and study 2 examined the effect of 600-mg rifampin once daily on the pharmacokinetics of 800-mg raltegravir twice daily compared to 400-mg raltegravir twice daily without rifampin."( Effect of rifampin, a potent inducer of drug-metabolizing enzymes, on the pharmacokinetics of raltegravir.
Berg, JK; Brainard, DM; Chodakewitz, JA; Ghosh, K; Gottesdiener, KM; Hanley, WD; Iwamoto, M; Jin, B; Mangin, E; Marbury, TC; Petry, AS; Stone, JA; Wagner, JA; Wenning, LA, 2009
)
" A population pharmacokinetic (PopPK) model was developed using trough blood CsA concentration data from 106 patients with NS."( Population pharmacokinetic study of cyclosporine in patients with nephrotic syndrome.
Qiang, F; Xiaoli, D, 2009
)
" Therefore, pharmacokinetic and drug metabolism studies were conducted in animals to support its clinical development."( Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.
Anderson, JJ; Barten, DM; Boulton, DW; Felsenstein, KM; Flint, OP; Hansel, SB; Krishna, R; Lubinski, J; Pursley, JM; Santone, KS; Thakur, A; Wang, J; Yao, M; Zheng, M, 2009
)
" Since cytochrome P450 enzymes CYP3A4 and CYP2B6 play a major role in prasugrel's active metabolite formation, the effect of potent CYP induction by rifampin on the pharmacokinetics of prasugrel and on the pharmacodynamic response to prasugrel was evaluated in healthy male subjects."( Effect of rifampin on the pharmacokinetics and pharmacodynamics of prasugrel in healthy male subjects.
Brandt, JT; Ernest II, CS; Farid, NA; Jakubowski, JA; Jin, Y; Li, YG; Payne, CD; Salazar, DE; Small, DS; Winters, KJ, 2009
)
" Blood collection for pharmacokinetic and pharmacodynamic analyses occurred after the LD and fifth MD of prasugrel in both periods."( Effect of rifampin on the pharmacokinetics and pharmacodynamics of prasugrel in healthy male subjects.
Brandt, JT; Ernest II, CS; Farid, NA; Jakubowski, JA; Jin, Y; Li, YG; Payne, CD; Salazar, DE; Small, DS; Winters, KJ, 2009
)
" A limitation of this study is that while results of the in vitro post hoc study indicate a pharmacodynamic interaction with rifampin, the mechanism underlying this interaction has not been elucidated."( Effect of rifampin on the pharmacokinetics and pharmacodynamics of prasugrel in healthy male subjects.
Brandt, JT; Ernest II, CS; Farid, NA; Jakubowski, JA; Jin, Y; Li, YG; Payne, CD; Salazar, DE; Small, DS; Winters, KJ, 2009
)
"Rifampin expectedly decreased AUCinf and Cmax of axitinib (geometric mean reduced by 79 and 71%, respectively)."( Effect of rifampin on the pharmacokinetics of Axitinib (AG-013736) in Japanese and Caucasian healthy volunteers.
Garrett, M; Hee, B; Klamerus, KJ; Kuruganti, U; Ni, G; Pithavala, YK; Toh, M; Tortorici, M, 2010
)
" The mean pharmacokinetic parameters for pravastatin that changed significantly were as follows (rifampicin and placebo groups, respectively): C(max) (315."( Effects of a concomitant single oral dose of rifampicin on the pharmacokinetics of pravastatin in a two-phase, randomized, single-blind, placebo-controlled, crossover study in healthy Chinese male subjects.
Cao, D; Chen, XP; Dai, ZY; Deng, S; Li, YJ; Luo, J; Tang, L; Yin, T, 2009
)
" These results show that the cynomolgus monkey can be a predictive in vivo animal model of PXR-mediated induction of human CYP3A4 and can provide a useful assessment of the resulting pharmacokinetic changes of affected drugs."( Evaluation of cynomolgus monkey pregnane X receptor, primary hepatocyte, and in vivo pharmacokinetic changes in predicting human CYP3A4 induction.
Anthony, MN; Dinchuk, JE; Dulac, HA; Grace, JE; Kim, S; Mosure, KW; Orcutt, T; Pizzano, J; Sauer, MB; Simmermacher, J; Sinz, M; Vuppugalla, R; Zoeckler, ME, 2010
)
" This validated method was successfully applied to a pharmacokinetic study involving intravenous administration of 14mgkg(-1) DPT and 30mgkg(-1) RFM to rabbits."( Simultaneous quantification of daptomycin and rifampicin in plasma by ultra performance liquid chromatography: Application to a pharmacokinetic study.
Bazoti, FN; Fanourgiakis, P; Gikas, E; Perivolioti, E; Roussidis, A; Skoutelis, A; Tsarbopoulos, A, 2010
)
"Modulation of P-glycoprotein (Pgp)-mediated transport has significant pharmacokinetic implications for Pgp substrates."( Pharmacokinetic and pharmacodynamic implications of P-glycoprotein modulation.
Padowski, JM; Pollack, GM, 2010
)
" Intensive pharmacokinetic sampling was performed for rifampin, pyrazinamide, and ethambutol at steady state."( Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
Aarnoutse, RE; Adhiarta, IG; Alisjahbana, B; Kariadi, SH; Nijland, HM; Ruslami, R; van Crevel, R, 2010
)
" Population pharmacokinetic parameters and their variability encountered in tuberculosis patients were utilized in Monte Carlo simulations to determine the probability that particular daily doses of the drugs would achieve or exceed the EC(90) in the epithelial lining fluid of 10,000 tuberculosis patients."( New susceptibility breakpoints for first-line antituberculosis drugs based on antimicrobial pharmacokinetic/pharmacodynamic science and population pharmacokinetic variability.
Gumbo, T, 2010
)
" Serial blood samples were collected for pharmacokinetic analysis after the administration of mirodenafil in each study period."( The effects of ketoconazole and rifampicin on the pharmacokinetics of mirodenafil in healthy Korean male volunteers: an open-label, one-sequence, three-period, three-treatment crossover study.
Cho, JY; Jang, IJ; Kim, BH; Kim, JW; Kim, TE; Shin, KH; Shin, SG; Yi, S; Yoon, SH; Yu, KS, 2009
)
" The mean half-life and apparent oral clearance were decreased for the combination treatment compared with linezolid alone."( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism.
Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011
)
" Pharmacokinetic data were analyzed by nonlinear mixed-effect modeling using NONMEM."( Effects of four different meal types on the population pharmacokinetics of single-dose rifapentine in healthy male volunteers.
Fourie, PB; McIlleron, HM; Mitchison, D; Roscigno, G; Simonsson, US; Smith, PJ; Van Der Walt, JS; Zvada, SP, 2010
)
" Subjects underwent 12 h intensive pharmacokinetic sampling on Days 7, 14 and 21 of nevirapine treatment."( Nevirapine pharmacokinetics when initiated at 200 mg or 400 mg daily in HIV-1 and tuberculosis co-infected Ugandan adults on rifampicin.
Back, D; Boffito, M; Byakika-Kibwika, P; Coakley, P; Colebunders, R; Kalemeera, F; Khoo, S; Lamorde, M; Merry, C; Namakula, R; Okaba-Kayom, V; Ryan, M, 2011
)
" Finally, the pharmacodynamic interaction index (PDI) was computed as the ratio of the volumes under the observed and simulated surfaces."( Pharmacodynamic assessment of vancomycin-rifampicin combination against methicillin resistant Staphylococcus aureus biofilm: a parametric response surface analysis.
Elkhatib, WF; Noreddin, AM; Salem, AH, 2011
)
" There were no significant differences between group CON and the other pretreatment groups in pharmacokinetic parameters taking both sexes into account."( The influence of modulation of P-glycoprotein and /or cytochrome P450 3A on the pharmacokinetics and pharmacodynamics of orally administered morphine in dogs.
Croubels, S; Gadeyne, C; Gasthuys, F; Polis, I; Schauvliege, S; Van der Heyden, S, 2011
)
" The pharmacokinetic parameters were: plasma drug concentration-time profile from 0 to 72 h (AUC0-72), plasma drug concentration-time profile from 0 h to infinity (AUC0-inf), maximal drug concentration (Cmax), time to reach maximal drug concentration (tmax), and time to reach half the initial drug concentration in elimination phase (t1/2)."( Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers.
Djoerban, Z; Setiabudy, R, 2011
)
" An in vitro pharmacodynamic model was used to simulate adult steady-state epithelial lining fluid concentrations of tigecycline (50 mg every 12 h) given alone and in combination with either meropenem (2 g by 3-hour infusion every 8 h) or rifampin (600 mg every 12 h)."( In vitro pharmacodynamics of simulated pulmonary exposures of tigecycline alone and in combination against Klebsiella pneumoniae isolates producing a KPC carbapenemase.
Koomanachai, P; Kuti, JL; Nicasio, AM; Nicolau, DP; Wiskirchen, DE, 2011
)
" Pharmacokinetic parameters were determined using non-compartmental methods."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
" However, current pharmacokinetic data are insufficient to guide optimized concurrent dosing."( Modest but variable effect of rifampin on steady-state plasma pharmacokinetics of efavirenz in healthy African-American and Caucasian volunteers.
Court, MH; Dumond, JB; Greenblatt, DJ; Kashuba, AD; Kurpewski, J; Kwara, A; Poethke, P; Tashima, KT, 2011
)
" There were no significant differences in the LPV area under the plasma concentration-time curve from 0 to 12 h (AUC(0-12)), C(0), C(12), maximum concentration of drug in serum (C(max)), or half-life (t(1/2)) between the baseline and double-dose LPV/r time points."( Pharmacokinetics of lopinavir in HIV-infected adults receiving rifampin with adjusted doses of lopinavir-ritonavir tablets.
Decloedt, EH; Maartens, G; McIlleron, H; Merry, C; Orrell, C; Smith, P, 2011
)
" These results suggested that pretreatment with rifampicin prior to SAB administration could decrease significantly the total and bile elimination of SAB and alter its pharmacokinetic profiles."( Influence of rifampicin on the pharmacokinetics of salvianolic acid B may involve inhibition of organic anion transporting polypeptide (Oatp) mediated influx.
Chen, XJ; Gao, ZD; Han, DE; Li, N; Li, TT; Lu, Y; Zhang, YJ; Zhao, D, 2012
)
" Since moxifloxacin has a longer half-life than rifampin, rifampin concentrations are <1% of the maximum concentration in serum (C(max)) on day 6 and nondetectable on day 7, while concentrations of moxifloxacin remain and are able to induce error-prone replication."( Effect of administration of moxifloxacin plus rifampin against Mycobacterium tuberculosis for 7 of 7 days versus 5 of 7 days in an in vitro pharmacodynamic system.
Brown, D; Drusano, GL; Eichas, A; Kulawy, R; Louie, A; Sgambati, N, 2011
)
" The aim of this study was to determine the pharmacokinetic parameters for ETH in children on antituberculosis treatment including ETH."( Pharmacokinetics of ethionamide in children.
Donald, PR; Hesseling, AC; Magdorf, K; Rosenkranz, B; Schaaf, HS; Seifart, HI; Thee, S, 2011
)
" One of the major mechanisms proposed to lead to the emergence of drug resistance is pharmacokinetic mismatch."( Pharmacokinetic mismatch does not lead to emergence of isoniazid- or rifampin-resistant Mycobacterium tuberculosis but to better antimicrobial effect: a new paradigm for antituberculosis drug scheduling.
Gumbo, T; Leff, R; Meek, C; Sherman, C; Srivastava, S, 2011
)
" No pharmacokinetic studies for these revised dosages are available for children <2 years."( Pharmacokinetics of isoniazid, rifampin, and pyrazinamide in children younger than two years of age with tuberculosis: evidence for implementation of revised World Health Organization recommendations.
Donald, PR; Hesseling, AC; Magdorf, K; Roll, S; Rosenkranz, B; Schaaf, HS; Seddon, JA; Seifart, HI; Thee, S; Werely, CJ, 2011
)
" This is despite the availability of antibiotics that have good activity against Mycobacterium tuberculosis in vitro and favorable pharmacokinetic profiles in plasma."( Pharmacokinetic evaluation of the penetration of antituberculosis agents in rabbit pulmonary lesions.
Barry, CE; Dartois, V; Goh, A; Kern, S; Kjellsson, MC; Low, KM; Pillai, G; Via, LE; Weiner, D, 2012
)
" Due to the saturable nature of tolvaptan's effect on urine excretion rate, changes in the pharmacokinetic profile of tolvaptan do not produce proportional changes in urine output."( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012
)
" We also explored the effect of pharmacokinetic variability on MDR-tuberculosis emergence using computer-aided clinical trial simulations of 10 000 Cape Town, South Africa, tuberculosis patients."( Multidrug-resistant tuberculosis not due to noncompliance but to between-patient pharmacokinetic variability.
Gumbo, T; Leff, R; Meek, C; Pasipanodya, JG; Srivastava, S, 2011
)
" However, clinical trial simulations demonstrated that approximately 1% of tuberculosis patients with perfect adherence would still develop MDR-tuberculosis due to pharmacokinetic variability alone."( Multidrug-resistant tuberculosis not due to noncompliance but to between-patient pharmacokinetic variability.
Gumbo, T; Leff, R; Meek, C; Pasipanodya, JG; Srivastava, S, 2011
)
" This study evaluated the effects of co-administration of a potent CYP3A4 inducer (rifampicin [rifampin]) and a weak CYP3A4 inducer (dexamethasone) on the pharmacokinetic, pharmacodynamic and safety profiles of bortezomib."( Effect of cytochrome P450 3A4 inducers on the pharmacokinetic, pharmacodynamic and safety profiles of bortezomib in patients with multiple myeloma or non-Hodgkin's lymphoma.
Feng, H; Girgis, S; Hellmann, A; Louw, VJ; Patel, H; Rule, S; Shpilberg, O; Skee, DM; van de Velde, H; Walewski, J, 2011
)
" Blood samples were collected on days 11 through 14 of cycles 2 and 3 before and after bortezomib administration, at prespecified time points, for pharmacokinetic and pharmacodynamic (proteasome inhibition) assessments."( Effect of cytochrome P450 3A4 inducers on the pharmacokinetic, pharmacodynamic and safety profiles of bortezomib in patients with multiple myeloma or non-Hodgkin's lymphoma.
Feng, H; Girgis, S; Hellmann, A; Louw, VJ; Patel, H; Rule, S; Shpilberg, O; Skee, DM; van de Velde, H; Walewski, J, 2011
)
" These results showed that Labrasol and Pluronic F68 might inhibit the function of P-gp in the intestine, thereby increasing intestinal absorption and changing the pharmacokinetic parameters of rifampicin."( Effects of Pluronic F68 and Labrasol on the intestinal absorption and pharmacokinetics of rifampicin in rats.
Ma, L; Ma, X; Wei, Y; Wu, X; Zhou, Y, 2011
)
" We performed a prospective case-control association study to identify the incidence, pharmacogenetic, pharmacokinetic and biochemical predictors for anti-tubercular and antiretroviral drugs induced liver injury (DILI) in HIV and tuberculosis (TB) co-infected patients."( Pharmacogenetic & pharmacokinetic biomarker for efavirenz based ARV and rifampicin based anti-TB drug induced liver injury in TB-HIV infected patients.
Aderaye, G; Aklillu, E; Amogne, W; Burhenne, J; Habtewold, A; Lindquist, L; Makonnen, E; Riedel, KD; Suda, A; Ueda, N; Yimer, G, 2011
)
" Blood sampling for pharmacokinetic assessment of RMP was done after at least 14 days of regular daily treatment to ensure steady state."( Pharmacokinetics of standard dose regimens of rifampicin in patients with pulmonary tuberculosis in Pakistan.
Farooqi, ZU; Najmi, MH; Saeed, W; Shaheen, A, 2012
)
" The turnover of the inducible process was estimated to have a half-life of approximately 8 days in a typical patient."( A semimechanistic pharmacokinetic-enzyme turnover model for rifampin autoinduction in adult tuberculosis patients.
Bocar Lo, M; Gninafon, M; Horton, J; Khandelwal, A; Lienhardt, C; McIlleron, H; Merle, C; Olliaro, PL; Rustomjee, R; Simonsson, US; Smith, P; Smythe, W; Sow, OB, 2012
)
" Both time to Cmax (Tmax) and apparent halflife (t₁/₂) were similar."( The effect of multiple doses of rifampin and ketoconazole on the single-dose pharmacokinetics of ridaforolimus.
Agrawal, N; Breidinger, S; Iwamoto, M; Johnson-Levonas, A; Kraft, WK; Marsilio, S; McCrea, J; Murphy, G; Orford, K; Palcza, J; Panebianco, D; Stroh, M; Trucksis, M; Wagner, JA, 2012
)
"2 mg/liter, respectively, and the time to the peak concentration was 6 h (slow absorber) instead of 2 h (fast absorber) for 61 patients (62."( Pharmacokinetics of rifampin in Peruvian tuberculosis patients with and without comorbid diabetes or HIV.
Ardrey, A; Davies, G; Jave, O; López-Romero, SL; Moore, DA; Requena-Méndez, A; Ward, SA, 2012
)
" A population pharmacokinetic model was developed with MONOLIX 4 software."( Population pharmacokinetics of clindamycin orally and intravenously administered in patients with osteomyelitis.
Bouazza, N; Curis, E; Jullien, V; Pestre, V; Salmon, D; Tréluyer, JM; Urien, S, 2012
)
"The effects of multiple oral doses of ketoconazole (a potent CYP3A4 inhibitor) and multiple oral doses of rifampicin (a potent CYP3A4 inducer) on the pharmacokinetic properties of a single oral dose of gemigliptin were evaluated in fasting healthy male Korean volunteers."( Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers.
Bae, KS; Choi, HY; Jin, SJ; Kim, MJ; Kim, YH; Lim, HS; Noh, YH; Sung, HR, 2012
)
" Pharmacokinetic parameters were estimated via noncompartmental methods."( Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers.
Bae, KS; Choi, HY; Jin, SJ; Kim, MJ; Kim, YH; Lim, HS; Noh, YH; Sung, HR, 2012
)
"Twenty-two children received antituberculosis and antiretroviral therapy (ART) concurrently for 4 weeks before pharmacokinetic sampling."( Pharmacokinetics of nevirapine in HIV-infected children under 3 years on rifampicin-based antituberculosis treatment.
Burger, DM; Chintu, C; Cook, A; Gibb, DM; McIlleron, H; Merry, C; Mulenga, V; Oudijk, JM; Walker, AS, 2012
)
" aureus (MRSA) strain and the antibiotic pharmacodynamic profile against extracellular (broth) and intracellular (human THP-1 monocytes) bacteria."( Pharmacodynamic evaluation of the activity of antibiotics against hemin- and menadione-dependent small-colony variants of Staphylococcus aureus in models of extracellular (broth) and intracellular (THP-1 monocytes) infections.
Becker, K; Denis, O; Garcia, LG; Kahl, BC; Lemaire, S; Proctor, RA; Tulkens, PM; Van Bambeke, F, 2012
)
"001), but shortened only moderately the elimination half-life of intravenous and oral S-ketamine."( Rifampicin has a profound effect on the pharmacokinetics of oral S-ketamine and less on intravenous S-ketamine.
Hagelberg, NM; Kurkinen, KJ; Laine, K; Neuvonen, PJ; Olkkola, KT; Peltoniemi, MA; Saari, TI, 2012
)
" The PK-PD parameter calculated was Cmax free/MIC."( Rifampin breakpoint for Acinetobacter baumannii based on pharmacokinetic-pharmacodynamic models with Monte Carlo simulation.
Aznar, J; García-Cabrera, E; Gil-Navarro, MV; Lepe, JA, 2012
)
"We retrospectively collected pharmacokinetic data of all patients treated for MAC lung disease in the Adult Care Unit at National Jewish Health, Denver, Colorado, in the January 2006 to January 2010 period; we retrospectively calculated areas under the time-concentration curve (AUC)."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
"We included 531 pharmacokinetic analyses, performed for 481 patients (84% females; mean age, 63 yr; mean body mass index, 21."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
" Pharmacodynamic indices for rifampicin, clarithromycin, amikacin, and moxifloxacin are seldom met."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
"We describe a rapid screening methodology for performing pharmacokinetic (PK) studies in mice called Fast PK."( Fast mouse PK (Fast PK): a rapid screening method to increase pharmacokinetic throughput in pre-clinical drug discovery.
Madishetti, S; Reddy, J; Vachaspati, PR, 2012
)
" Pharmacokinetic sampling for determination of eribulin plasma concentrations was performed up to 144 h following administration."( Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin.
Beijnen, JH; Copalu, W; Devriese, LA; Edwards, G; Huitema, AD; Law, K; Marchetti, S; Peng, F; Reyderman, L; Schellens, JH; Voest, EE; Wanders, J; Witteveen, PE, 2013
)
"Fourteen patients were included and 11 patients were evaluable for pharmacokinetic analysis."( Pharmacokinetics of eribulin mesylate in patients with solid tumours receiving repeated oral rifampicin.
Beijnen, JH; Copalu, W; Devriese, LA; Edwards, G; Huitema, AD; Law, K; Marchetti, S; Peng, F; Reyderman, L; Schellens, JH; Voest, EE; Wanders, J; Witteveen, PE, 2013
)
"We studied the pharmacokinetic and pharmacodynamic parameters of levofloxacin and rifampicin in bone and joint infections."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
" We then computed the 6 hours post dose area under the concentration-time curve (AUC(0-6h)), the peak plasma concentration (Cmax), the area under the inhibitory concentration curve (AUIC), and the peak-to-minimum-inhibitory-concentration ratio (Cmax/MIC)."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
"h/l, the average Cmax 10."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
"The optimal thresholds of pharmacodynamic effectiveness were obtained for most patients with levofloxacin at 500 mg bid."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
" For pharmacokinetic analysis, serial blood samples were collected over 24 h on day 7 of treatment."( Pharmacokinetic and safety evaluation of the use of ciprofloxacin on an isoniazid-rifampicin regimen in rabbits.
Baldan, HM; Brunetti, IL; Campos, ML; Davanço, MG; de Pontes Machado, DV; Filho, MA; Padilha, EC; Peccinini, RG; Pires, RV, 2012
)
"This was a Phase II open-label multiple dose pharmacokinetic and safety study."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
"A total of 25 patients (56% male) completed the study; 21 had evaluable pharmacokinetic profiles."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
"Coadministration of efavirenz, tenofovir and emtricitabine with a standard first-line TB treatment regimen did not significantly alter the pharmacokinetic parameters of these drugs and was tolerated well by Tanzanian TB patients who are coinfected with HIV."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
"Phase I pharmacokinetic drug interaction study."( Safety, tolerability, and pharmacokinetics of the HIV integrase inhibitor dolutegravir given twice daily with rifampin or once daily with rifabutin: results of a phase 1 study among healthy subjects.
Borland, J; Chen, S; Dooley, KE; Everts, S; Flexner, C; Peppercorn, A; Piscitelli, S; Purdy, E; Sayre, P; Song, I, 2013
)
" Ticagrelor and AR-C124910XX plasma concentrations were quantified for pharmacokinetic analysis (n = 14); inhibition of platelet aggregation (IPA) was also assessed (n = 14)."( Effect of rifampicin on the pharmacokinetics and pharmacodynamics of ticagrelor in healthy subjects.
Butler, K; Mitchell, P; Teng, R, 2013
)
" No pharmacokinetic data are available from South American children."( Pharmacokinetics of anti-tuberculosis drugs in Venezuelan children younger than 16 years of age: supportive evidence for the implementation of revised WHO dosing recommendations.
Aarnoutse, RE; de Groot, R; de Waard, JH; García, JF; Hermans, PW; López, D; Verhagen, LM; Warris, A, 2012
)
"25 patients (83%) had an isoniazid Cmax below 3 mg/l and 23 patients (77%) had a rifampicin Cmax below 8 mg/l."( Pharmacokinetics of anti-tuberculosis drugs in Venezuelan children younger than 16 years of age: supportive evidence for the implementation of revised WHO dosing recommendations.
Aarnoutse, RE; de Groot, R; de Waard, JH; García, JF; Hermans, PW; López, D; Verhagen, LM; Warris, A, 2012
)
" A pharmacokinetic model was applied to model systemic RIF concentrations and to predict the RIF concentrations in the lung epithelial lining fluid (ELF)."( A preclinical pharmacokinetic modeling approach to the biopharmaceutical characterization of immediate and microsphere-based sustained release pulmonary formulations of rifampicin.
Couet, W; Doan, TV; Gobin, P; Grégoire, N; Lamarche, I; Marchand, S; Olivier, JC, 2013
)
" The purpose of this study was to develop and validate a population pharmacokinetic model to characterize the inter- and intra-individual variability in pharmacokinetic parameters of RIF in Mexican patients."( Population pharmacokinetics of rifampicin in Mexican patients with tuberculosis.
Brundage, RC; Domínguez Ramírez, AM; Jung Cook, H; Magaña Aquino, M; Milán Segovia, RC; Romano Moreno, S; Vigna Pérez, M, 2013
)
" In vitro hollow-fiber infection model (HFIM) is employed to simulate human in vivo drug clearance and investigate pharmacodynamic synergism of antibiotics."( Optimizing hollow-fiber-based pharmacokinetic assay via chemical stability study to account for inaccurate simulated drug clearance of rifampicin.
Chan, EC; Cheah, GJ; Kwa, AL; Lim, TP; New, LS; Oh, JW, 2013
)
" In order to gain insight into these discrepant findings, we conducted a steady-state pharmacokinetic (PK) study in healthy guinea pigs to study the metabolism and autoinduction of RIF and RFP."( Preliminary pharmacokinetic study of repeated doses of rifampin and rifapentine in guinea pigs.
Alsultan, A; Dutta, NK; Karakousis, PC; Peloquin, CA, 2013
)
" In vitro/in vivo assays were performed to evaluate the pharmacokinetic (PK) and pharmacodynamic (PD) performance of these nanoparticles following nanoencapsulation of the anti-tuberculosis drugs rifampicin (RIF) and isoniazid (INH)."( In vivo/in vitro pharmacokinetic and pharmacodynamic study of spray-dried poly-(dl-lactic-co-glycolic) acid nanoparticles encapsulating rifampicin and isoniazid.
Booysen, LL; Brooks, E; du Plessis, LH; Gilliland, J; Gruppo, V; Hansen, R; Kalombo, L; Kotze, AF; Lenaerts, A; Lungenhofer, P; Semete-Makokotlela, B; Swai, HS, 2013
)
" In order to increase the available mathematical tools needed to support such a model for preclinical anti-TB drug development, we constructed a preliminary whole-body physiologically based pharmacokinetic (PBPK) model of rifampin in mice, using data from the literature."( A physiologically based pharmacokinetic model of rifampin in mice.
Lenaerts, AJ; Lyons, MA; Reisfeld, B; Yang, RS, 2013
)
"A baseline pharmacokinetic study of MFX (400 mg once daily) was conducted in 36 healthy adults and repeated after one week of daily MFX with either RMP (450/600 mg) (n = 18) or INH (300 mg) (n = 18)."( Effect of rifampicin & isoniazid on the steady state pharmacokinetics of moxifloxacin.
Geetharani, A; Hemanth Kumar, AK; Nandhakumar, B; Nandini, R; Ramachandran, G; Srinivasan, R; Sugirda, P; Tharani, CB, 2012
)
"Plasma peak concentration and exposure of MFX was significantly lower and plasma clearance significantly higher when combined with RMP (P<0."( Effect of rifampicin & isoniazid on the steady state pharmacokinetics of moxifloxacin.
Geetharani, A; Hemanth Kumar, AK; Nandhakumar, B; Nandini, R; Ramachandran, G; Srinivasan, R; Sugirda, P; Tharani, CB, 2012
)
" The objective of this study was to develop a population pharmacokinetic model describing the pharmacokinetic differences of lopinavir and ritonavir, with and without rifampicin, between children and adults."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
"An integrated population pharmacokinetic model developed in nonmem 7 was used to describe the pharmacokinetics of lopinavir and ritonavir in 21 HIV infected adults, 39 HIV infected children and 35 HIV infected children with tuberculosis, who were established on lopinavir/ritonavir-based antiretroviral therapy with and without rifampicin-containing antituberculosis therapy."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
" In children, the absorption half-life of lopinavir and the mean transit time of ritonavir were lengthened, compared with those in adults."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
" We therefore determined the pharmacokinetic characteristics of first-line TB drugs in Tanzanian patients using intensive pharmacokinetic sampling."( Pharmacokinetics of first-line tuberculosis drugs in Tanzanian patients.
Aarnoutse, RE; Boeree, MJ; Kibiki, GS; Mtabho, CM; Semvua, HH; Tostmann, A; van den Boogaard, J, 2013
)
" Log-transformed anacetrapib AUC0-∞ and Cmax were analyzed by a linear mixed effects model."( Effects of Rifampin, a potent inducer of drug-metabolizing enzymes and an inhibitor of OATP1B1/3 transport, on the single dose pharmacokinetics of anacetrapib.
Anderson, MS; Auger, P; Cote, J; Gutstein, DE; Hohnstein, A; Johnson-Levonas, AO; Liu, Y; Rasmussen, S; Stypinski, D, 2013
)
"The currently recommended dosages of rifampicin (RMP), isoniazid (INH), pyrazinamide (PZA) and ethambutol in children are extrapolated from adult pharmacokinetic studies, and have not been adequately evaluated in children."( Age, nutritional status and INH acetylator status affect pharmacokinetics of anti-tuberculosis drugs in children.
Banu Rekha, VV; Bhavani, PK; Hemanth Kumar, AK; Mathevan, G; Poorana Gangadevi, N; Ramachandran, G; Ramesh Kumar, S; Ravichandran, N; Sekar, L; Swaminathan, S; Vijayasekaran, D, 2013
)
" During the intensive phase of anti-tuberculosis treatment, a complete pharmacokinetic study was performed after directly observed administration of drugs."( Age, nutritional status and INH acetylator status affect pharmacokinetics of anti-tuberculosis drugs in children.
Banu Rekha, VV; Bhavani, PK; Hemanth Kumar, AK; Mathevan, G; Poorana Gangadevi, N; Ramachandran, G; Ramesh Kumar, S; Ravichandran, N; Sekar, L; Swaminathan, S; Vijayasekaran, D, 2013
)
"Children aged <3 years had significantly lower RMP, INH and PZA concentrations than older children, and 90% of all children had sub-therapeutic RMP Cmax (<8 μg/ml)."( Age, nutritional status and INH acetylator status affect pharmacokinetics of anti-tuberculosis drugs in children.
Banu Rekha, VV; Bhavani, PK; Hemanth Kumar, AK; Mathevan, G; Poorana Gangadevi, N; Ramachandran, G; Ramesh Kumar, S; Ravichandran, N; Sekar, L; Swaminathan, S; Vijayasekaran, D, 2013
)
" Systolic and diastolic blood pressures and pulse rate were periodically recorded after nadolol administration as pharmacodynamic parameters."( Pharmacokinetic and pharmacodynamic interaction of nadolol with itraconazole, rifampicin and grapefruit juice in healthy volunteers.
Fukushima, T; Kimura, J; Misaka, S; Miyazaki, N; Ono, T; Shikama, Y; Yatabe, MS, 2013
)
" Therefore, a physiologically-based pharmacokinetic (PBPK) model for verapamil and its primary metabolite was developed and validated through the recovery of observed clinical plasma concentration data for both moieties and the reported interaction with midazolam, albeit a cytochrome P450 3A4-mediated DDI."( Application of permeability-limited physiologically-based pharmacokinetic models: part II - prediction of P-glycoprotein mediated drug-drug interactions with digoxin.
Barter, Z; Jamei, M; Neuhoff, S; Rostami-Hodjegan, A; Turner, DB; Yeo, KR, 2013
)
"There were no significant pharmacokinetic interactions between netupitant and palonosetron."( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives.
Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013
)
"We studied if the clinical pharmacokinetics and drug-drug interactions (DDIs) of the sulfonylurea-derivative glibenclamide can be simulated via a physiologically-based pharmacokinetic modeling approach."( Semi-mechanistic physiologically-based pharmacokinetic modeling of clinical glibenclamide pharmacokinetics and drug-drug-interactions.
Benne, MS; Greupink, R; Huisman, MT; Russel, FG; Schreurs, M, 2013
)
" Various pharmacokinetic parameters of RIF significantly differ when administered alone or in combination with OXC and NXC."( Effect of ofloxacin and norfloxacin on rifampicin pharmacokinetics in man.
Barikpoar, E; Brown, S; Ezejiofor, NA; Orisakwe, OE,
)
"A single dose of rifampin significantly increased the mean area under the plasma concentration-time curve(AUC)(0-48 h) and Cmax of pitavastatin by 573."( Effect of a single-dose rifampin on the pharmacokinetics of pitavastatin in healthy volunteers.
Chen, Y; Huang, WH; Huang, X; Tan, ZR; Wang, YC; Zhang, W; Zhou, HH, 2013
)
"The clinical pharmacokinetic findings and in vitro data suggest that CYP3A4 is important for ospemifene metabolism, but other CYP isoforms and metabolic pathways also contribute."( Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene.
Lammintausta, R; Lehtinen, T; Pelkonen, O; Scheinin, M; Tolonen, A; Turpeinen, M; Uusitalo, J; Vuorinen, J, 2013
)
" Clinical studies in healthy subjects were performed to evaluate potential pharmacokinetic interactions between vortioxetine (Lu AA21004) and co-administered agents, including fluconazole (cytochrome P450 [CYP] 2C9, CYP2C19 and CYP3A inhibitor), ketoconazole (CYP3A and P-glycoprotein inhibitor), rifampicin (CYP inducer), bupropion (CYP2D6 inhibitor and CYP2B6 substrate), ethinyl estradiol/levonorgestrel (CYP3A substrates) and omeprazole (CYP2C19 substrate and inhibitor)."( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant.
Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013
)
", area under the plasma concentration-time curve [AUC] and maximum plasma concentration [C max]) was used to assess pharmacokinetic interactions."( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant.
Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013
)
" Serum concentration-time profiles, maximum serum concentrations, time to achieve maximum serum concentrations, the half-life and the areas under the serum concentration-time curve for each of the four drugs were determined."( Pharmacokinetics and serum concentrations of antimycobacterial drugs in adult Turkish patients.
Arpag, H; Babalık, A; Bakirci, N; Çarpaner, E; Dagyildiz, L; Kuyucu, T; Ulus, IH, 2013
)
"Wide variations in pharmacokinetic parameters were observed among patients."( Pharmacokinetics and serum concentrations of antimycobacterial drugs in adult Turkish patients.
Arpag, H; Babalık, A; Bakirci, N; Çarpaner, E; Dagyildiz, L; Kuyucu, T; Ulus, IH, 2013
)
" We evaluated the effect of rifapentine on the pharmacokinetic properties of raltegravir."( Pharmacokinetic interaction of rifapentine and raltegravir in healthy volunteers.
Egelund, EF; Engle, M; Gelfond, JA; Kiser, M; Mac Kenzie, W; Peloquin, CA; Prihoda, TJ; Weiner, M, 2014
)
"In 16 subjects who completed the study, coadministration of raltegravir with rifapentine (900 mg once weekly; Period 2) compared with raltegravir alone resulted in the geometric mean of the raltegravir AUC from 0 to 12 h (AUC0-12) being increased by 71%; the peak concentration increased by 89% and the trough concentration decreased by 12%."( Pharmacokinetic interaction of rifapentine and raltegravir in healthy volunteers.
Egelund, EF; Engle, M; Gelfond, JA; Kiser, M; Mac Kenzie, W; Peloquin, CA; Prihoda, TJ; Weiner, M, 2014
)
" Samples were obtained for pharmacokinetic assessment on day 8 of each study cycle."( Factors associated with variability in rifampin plasma pharmacokinetics and the relationship between rifampin concentrations and induction of efavirenz clearance.
Cao, L; Court, MH; Kurpewski, J; Kwara, A; Mahjoub, BD; Peloquin, CA; Poethke, P; Tashima, KT; Yang, H, 2014
)
" A physiologically based pharmacokinetic (PBPK) model was developed to project the dynamics and magnitude of CYP3A4 induction in vivo from in vitro data generated with primary human hepatocytes."( Physiologically based pharmacokinetic modeling of CYP3A4 induction by rifampicin in human: influence of time between substrate and inducer administration.
Baneyx, G; Iliadis, A; Lavé, T; Meille, C; Parrott, N, 2014
)
" Ten pharmacokinetic studies and three efficacy/safety studies in overactive bladder (OAB) patients were pooled for the population pharmacokinetic analysis."( Population pharmacokinetics of the 5-hydroxymethyl metabolite of tolterodine after administration of fesoterodine sustained release tablet in Western and East Asian populations.
Malhotra, B; Oishi, M; Tomono, Y; Yamagami, H, 2014
)
" Rectal isoniazid produced an earlier Tmax compared with oral administration."( The pharmacokinetics of a single oral or rectal dose of concurrently administered isoniazid, rifampin, pyrazinamide, and ethambutol in Asian elephants (Elephas maximus).
Egelund, EF; Hunter, RP; Isaza, R; P Brock, A; Peloquin, CA, 2014
)
"The present study reports the comparative pharmacokinetic evaluation and biodistribution of rifampicin (RIF) following oral administration of nanoparticles of a bioadhesive polymer, Gantrez and a hydrophobic polymer poly(ethylene sebacate) (PES)."( Comparative evaluation of polymeric nanoparticles of rifampicin comprising Gantrez and poly(ethylene sebacate) on pharmacokinetics, biodistribution and lung uptake following oral administration.
Date, PV; Devarajan, PV; Gaikwad, RV; Malshe, VC; Patel, MD; Samad, A, 2014
)
" The lag time (tlag) and the time before reach Cmax (Tmax) were longer for female TB patients (P < 0."( Pharmacokinetics of rifampicin in Mexican patients with tuberculosis and healthy volunteers.
Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, Rdel C; Portales-Pérez, DP; Romano-Moreno, S, 2014
)
" Pharmacokinetic sampling occurred at the end of each dosing period."( Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.
Allen, R; Aweeka, F; Bao, J; Cramer, Y; Dooley, KE; Haas, DW; Koletar, SL; Luetkemeyer, AF; Marzan, F; Murray, S; Park, JG; Savic, R; Sutherland, D, 2014
)
"4) and Cmax (from 290 vs."( The impact of co-administration of ketoconazole and rifampicin on the pharmacokinetics of apremilast in healthy volunteers.
Liu, Y; Palmisano, M; Wan, Y; Wu, A; Zhou, S, 2014
)
" The aim of the current work was to develop a novel physiologically based pharmacokinetic (PBPK) model to quantitatively assess the magnitude of CYP3A4 mediated drug-drug interactions with alisporivir as the substrate or victim drug."( Physiologically based pharmacokinetic modeling for assessing the clinical drug-drug interaction of alisporivir.
Alexander, N; Barve, A; Einolf, H; Gu, H; Hanna, I; He, H; Heimbach, T; Ke, J; Mangold, JB; Sunkara, G; Wang, L; Xia, B; Zhang, T, 2014
)
" This study evaluated the effects of co-administration of a potent CYP3A4 inducer rifampin on the pharmacokinetic and safety profiles of navitoclax."( Effect of rifampin on the pharmacokinetics, safety and tolerability of navitoclax (ABT-263), a dual inhibitor of Bcl-2 and Bcl-XL , in patients with cancer.
Graham, AM; Holen, KD; Pradhan, RS; Rosen, LS; Xiong, H; Yang, J, 2014
)
" Rifampin did not affect the half-life of navitoclax."( Effect of rifampin on the pharmacokinetics, safety and tolerability of navitoclax (ABT-263), a dual inhibitor of Bcl-2 and Bcl-XL , in patients with cancer.
Graham, AM; Holen, KD; Pradhan, RS; Rosen, LS; Xiong, H; Yang, J, 2014
)
" After 7 days of exposure to 200 mg of ketoconazole once daily, the AUC0-t and Cmax of the parent drug were not affected significantly."( Effects of rifampin and ketoconazole on pharmacokinetics of morinidazole in healthy chinese subjects.
Chen, X; Gao, R; Pang, X; Zhang, Y; Zhong, D; Zhong, K, 2014
)
" This on-line RAM-HPLC method was successfully applied to the pharmacokinetic study of RIP in rat plasma."( Determination of rifampicin in rat plasma by modified large-volume direct injection RAM-HPLC and its application to a pharmcokinetic study.
Jia, Z; Li, W; Wang, R; Wang, Y; Xie, H; Zhang, J; Zhang, X, 2015
)
" This study aimed to characterize the pharmacokinetics of posaconazole in adults and investigate factors that influence posaconazole pharmacokinetics byusing a population pharmacokinetic approach."( Understanding variability in posaconazole exposure using an integrated population pharmacokinetic analysis.
Brüggemann, RJ; Burger, DM; Dolton, MJ; McLachlan, AJ, 2014
)
" The objective of this work was to build a physiologically based pharmacokinetic (PBPK) model to assess MMAE-drug interactions for vc-MMAE ADCs."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
" The model was developed using in silico and in vitro data and in vivo pharmacokinetic data from anti-CD22-vc-MMAE ADC."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
"The pharmacokinetic profile of acMMAE and unconjugated MMAE following administration of anti-CD22-vc-MMAE was well described by simulations using the developed PBPK model."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
" Pharmacokinetic (PK) parameters can be affected by several factors, such as comorbidities or the interaction of TB drugs with food."( Effects of dosage, comorbidities, and food on isoniazid pharmacokinetics in Peruvian tuberculosis patients.
Ardrey, A; Davies, G; Jave, O; López-Romero, SL; Moore, DA; Requena-Méndez, A; Ward, SA; Waterhouse, D, 2014
)
"The objective of this study was to develop a population pharmacokinetic model for rifampin in elephants."( Population pharmacokinetics of rifampin in the treatment of Mycobacterium tuberculosis in Asian elephants.
Alsultan, A; An, G; Brock, AP; Egelund, EF; Isaza, R; Peloquin, CA, 2015
)
" Pharmacokinetic sampling was performed on days 5, 33 and 38."( Effect of intermittent rifampicin on the pharmacokinetics and safety of raltegravir.
Back, DJ; Chaponda, M; Chiong, J; Chrdle, A; Egan, D; Else, L; Khoo, SH; Reynolds, HE, 2015
)
" Raltegravir Cmax and AUC0-12 were both significantly higher in the presence of rifampicin when dosed at 800 mg twice daily (76% and 84%, respectively), but this dose was well tolerated."( Effect of intermittent rifampicin on the pharmacokinetics and safety of raltegravir.
Back, DJ; Chaponda, M; Chiong, J; Chrdle, A; Egan, D; Else, L; Khoo, SH; Reynolds, HE, 2015
)
" The pharmacokinetic parameters of rifampin, isoniazid, ethambutol, and pyrazinamide were determined for each patient."( Impact of nonlinear interactions of pharmacokinetics and MICs on sputum bacillary kill rates as a marker of sterilizing effect in tuberculosis.
Chigutsa, E; Gumbo, T; McIlleron, H; Pasipanodya, JG; Sirgel, FA; Smith, PJ; van Helden, PD; Visser, ME, 2015
)
" Probenecid increased the Cmax by 13% and the AUC by 21%."( Effects of rifampin, cyclosporine A, and probenecid on the pharmacokinetic profile of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in healthy participants.
Ariyawansa, J; Curtin, C; Devineni, D; Di Prospero, NA; Mamidi, RN; Murphy, J; Rothenberg, P; Stieltjes, H; Vaccaro, N; Wajs, E; Wang, SS; Weiner, S, 2015
)
"In pharmacokinetic evaluation of mice, using serial sampling methods rather than a terminal blood sampling method could reduce the number of animals needed and lead to more reliable data by excluding individual differences."( Using improved serial blood sampling method of mice to study pharmacokinetics and drug-drug interaction.
Nezasa, K; Ogawa, K; Shimizu, R; Takai, N; Tanaka, Y; Watanabe, A; Watari, R; Yamaguchi, Y, 2015
)
" During the intensive phase of TB treatment with directly observed administration of the drugs, a complete pharmacokinetic study was performed."( Pharmacokinetics of first-line antituberculosis drugs in HIV-infected children with tuberculosis treated with intermittent regimens in India.
Banurekha, VV; Bhavani, PK; Dayal, R; Gangadevi, NP; Kannan, T; Kumar, AK; Kumar, SR; Mathevan, G; Ramachandran, G; Ravichandran, N; Sanjeeva, GN; Sekar, L; Swaminathan, S, 2015
)
" The pharmacokinetic profiles of bedaquiline and M2 were compared over 336 h after the administration of bedaquiline alone and in combination with steady-state rifapentine or rifampin."( Evaluation of the pharmacokinetic interaction between repeated doses of rifapentine or rifampin and a single dose of bedaquiline in healthy adult subjects.
Egizi, E; Erondu, N; Ginsberg, A; Murray, S; Pauli, E; Rouse, DJ; Severynse-Stevens, D; Winter, H, 2015
)
"Physiologically based pharmacokinetic modeling was applied to characterize the potential drug-drug interactions for ruxolitinib."( Predicting drug-drug interactions involving multiple mechanisms using physiologically based pharmacokinetic modeling: a case study with ruxolitinib.
Fraczkiewicz, G; Shi, JG; Williams, WV; Yeleswaram, S, 2015
)
" Pharmacokinetic sampling was performed once in every patient during the first three critical days."( Pharmacokinetic/pharmacodynamic analysis of an intensified regimen containing rifampicin and moxifloxacin for tuberculous meningitis.
Aarnoutse, R; Burger, D; Dian, S; Donders, R; Ganiem, AR; Ruesen, C; Ruslami, R; Te Brake, L; van Crevel, R, 2015
)
"Thirty children aged 6 months to 15 years underwent intensive pharmacokinetic sampling for first-line anti-TB drugs at Queen Elizabeth Central Hospital, Blantyre, Malawi."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
"These data support recently revised WHO recommendations for dosing of anti-TB drugs in children, but dosing of ethambutol in children also appears inadequate by comparison with adult pharmacokinetic data."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
" Median time to C(max) and mean half-life were shorter for bosutinib plus rifampin vs."( Effect of rifampin on the pharmacokinetics of bosutinib, a dual Src/Abl tyrosine kinase inhibitor, when administered concomitantly to healthy subjects.
Abbas, R; Boni, J; Sonnichsen, D, 2015
)
" This study was carried out to identify the contribution percentage of CYP450 to icotinib and use the results to develop a physiologically based pharmacokinetic (PBPK) model, which can help to predict drug-drug interaction (DDI)."( Relative contributions of the major human CYP450 to the metabolism of icotinib and its implication in prediction of drug-drug interaction between icotinib and CYP3A4 inhibitors/inducers using physiologically based pharmacokinetic modeling.
Chen, J; Hu, P; Jiang, J; Liu, D; Zhao, Q; Zheng, X, 2015
)
" Pharmacokinetic (PK) drug-drug interactions (DDIs) were evaluated clinically between cabozantinib and (1) a CYP3A inducer (rifampin) in healthy volunteers, (2) a CYP3A inhibitor (ketoconazole) in healthy volunteers, and (3) a CYP2C8 substrate (rosiglitazone) in patients with solid tumors."( Pharmacokinetic (PK) drug interaction studies of cabozantinib: Effect of CYP3A inducer rifampin and inhibitor ketoconazole on cabozantinib plasma PK and effect of cabozantinib on CYP2C8 probe substrate rosiglitazone plasma PK.
Benrimoh, N; Engel, C; Holland, J; Lacy, S; Miles, D; Nguyen, L; O'Reilly, T, 2015
)
" Peak RMP levels appear to be lower and the single dose elimination half-life shorter in children than in adults."( Rifampicin pharmacokinetics in children under the Revised National Tuberculosis Control Programme, India, 2009.
Arya, A; Kapoor, S; Khanna, A; Lomash, A; Rangari, G; Roy, V, 2015
)
"The available pharmacokinetic data on anti-tubercular drugs in children raises the concern of suboptimal plasma concentrations attained when doses extrapolated from adult studies are used."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
" A pharmacokinetic model was built in a forward and reverse procedure using nonlinear mixed effect modeling in NONMEM VI followed by model-based simulations for optimal doses."( CYP2B6*6, CYP2B6*18, Body weight and sex are predictors of efavirenz pharmacokinetics and treatment response: population pharmacokinetic modeling in an HIV/AIDS and TB cohort in Zimbabwe.
Chonzi, P; Dhoro, M; Kadzirange, G; Masimirembwa, C; Ngara, B; Nhachi, C; Zvada, S, 2015
)
" Notably, similar AUC (when corrected by dose), similar CL, λ, and half-life were obtained after oral administration of RIF at 40 mg/kg and pulmonary administration of RIF at 20 mg/kg."( Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs.
Edwards, D; Elbert, K; Garcia Contreras, L; Hickey, A; Ibrahim, M; Sung, J, 2015
)
" A one-compartmental pharmacokinetic population model with first-order absorption and lag time was developed using observed rifampin plasma concentrations from 55 patients."( Pharmacokinetic Modeling and Optimal Sampling Strategies for Therapeutic Drug Monitoring of Rifampin in Patients with Tuberculosis.
Aarnoutse, RE; Alffenaar, JW; de Jager, A; de Lange, WC; Kosterink, JG; Mulder, LW; Proost, JH; Sturkenboom, MG; van Altena, R; van der Werf, TS, 2015
)
" Plasma concentrations of edoxaban and its metabolites M4 and M6 were measured, and limited assessments of pharmacodynamic markers of coagulation were performed."( The effect of rifampin on the pharmacokinetics of edoxaban in healthy adults.
Chen, S; Desai, M; He, L; Mendell, J; Parasramupria, DA, 2015
)
"Participants receiving daily rifapentine and isoniazid with efavirenz had pharmacokinetic evaluations at baseline and weeks 2 and 4 of concomitant therapy."( Efavirenz Pharmacokinetics and Pharmacodynamics in HIV-Infected Persons Receiving Rifapentine and Isoniazid for Tuberculosis Prevention.
Andersen, JW; Bao, Y; Benson, CA; Chaisson, RE; Fletcher, CV; Gupta, A; Kim, P; Mohapi, L; Mwelase, T; Podany, AT; Supparatpinyo, K; Swindells, S, 2015
)
" Pharmacokinetic sampling was performed over 12-hour periods, 4 weeks after initiation of RAL together with RIF (period 1), 4 weeks after RIF discontinuation (period 2), and after the RAL dose reduction in arm 2 (period 3)."( Pharmacokinetics of Raltegravir in HIV-Infected Patients on Rifampicin-Based Antitubercular Therapy.
Assuied, A; De Castro, N; Fagard, C; Grinsztejn, B; Grondin, C; Molina, JM; Pilotto, JH; Sauvageon, H; Taburet, AM; Veloso, V, 2015
)
" The purpose of the present study is to develop a physiologically based pharmacokinetic (PBPK) model for atorvastatin and its two primary metabolites, 2-hydroxy-atorvastatin acid and atorvastatin lactone, using in vitro and in vivo data."( Physiologically based pharmacokinetic modeling of disposition and drug-drug interactions for atorvastatin and its metabolites.
Zhang, T, 2015
)
" The main objectives of the present study were to: 1) develop and refine a physiologically based pharmacokinetic (PBPK) model of crizotinib on the basis of clinical single- and multiple-dose results, 2) verify the crizotinib PBPK model from crizotinib single-dose drug-drug interaction (DDI) results with multiple-dose coadministration of ketoconazole or rifampin, and 3) apply the crizotinib PBPK model to predict crizotinib multiple-dose DDI outcomes."( Prediction of Drug-Drug Interactions with Crizotinib as the CYP3A Substrate Using a Physiologically Based Pharmacokinetic Model.
Johnson, TR; Smith, BJ; Yamazaki, S, 2015
)
" Administration of piragliatin (100-mg single dose) resulted in a 32% Cmax and 44% area under the curve (AUC∞ ) increase in piragliatin exposure without affecting glucose AUC0-6h following ketoconazole (400 mg QD × 5 days); 30% Cmax and 72% AUC∞ decrease in piragliatin exposure with a 13% increase in glucose AUC0-6h following rifampicin (600 mg QD × 5 days); and, unexpectedly, a 32% Cmax and 23% AUC0-6h decrease (no change in AUC∞ ) in piragliatin exposure with a 13% increase in glucose AUC0-6h following alcohol (40-g single dose)."( Exploratory effects of a strong CYP3A inhibitor (ketoconazole), a strong CYP3A inducer (rifampicin), and concomitant ethanol on piragliatin pharmacokinetics and pharmacodynamics in type 2 diabetic patients.
Boldrin, M; Georgy, A; Liang, Z; Zhai, S; Zhi, J, 2016
)
" Plasma concentration-time data were analysed using NONMEM to estimate population pharmacokinetic parameters and evaluate relationships between parameters and demographic factors, and metabolic enzyme, transporter and transcriptional regulator genotypes."( Population pharmacokinetics of rifampicin and 25-deacetyl-rifampicin in healthy Asian adults.
Chew, N; Hee, KH; Khoo, SH; Lee, LS; Seng, KY; Soon, GH, 2015
)
" 25-Deacetyl-rifampicin pharmacokinetic data were best described by a two-compartment model linked to the rifampicin model."( Population pharmacokinetics of rifampicin and 25-deacetyl-rifampicin in healthy Asian adults.
Chew, N; Hee, KH; Khoo, SH; Lee, LS; Seng, KY; Soon, GH, 2015
)
"We recently published analyses regarding the predictive performance of physiologically based pharmacokinetic (PBPK) models, submitted to the US Food and Drug Administration (FDA), for the effect of cytochrome P450 (CYP) inhibitors on the pharmacokinetics of substrate drugs."( Predicting the Effect of CYP3A Inducers on the Pharmacokinetics of Substrate Drugs Using Physiologically Based Pharmacokinetic (PBPK) Modeling: An Analysis of PBPK Submissions to the US FDA.
Hsu, V; Pan, Y; Sinha, V; Wagner, C; Zhao, P, 2016
)
" Relevant pharmacokinetic (PK) parameters for crizotinib and PF096269182 were estimated by standard non-compartmental analysis (NCA) method."( The effects of ketoconazole and rifampin on the single-dose pharmacokinetics of crizotinib in healthy subjects.
Bello, A; Brega, N; O'Gorman, M; Tan, W; Xu, H, 2015
)
"A physiological-based pharmacokinetic (PBPK) model was developed by combining observations from clinical studies and physicochemical parameters as well as absorption, distribution, metabolism and excretion parameters determined in vitro."( Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug-Drug Interactions.
Buchmann, S; de Kanter, R; Delahaye, S; Gnerre, C; Kohl, C; Segrestaa, J; Sidharta, PN; Treiber, A, 2016
)
"Rifampicin (RIF) induces cytochrome P450, which in turn catalyzes drug metabolism; however, pharmacokinetic studies on this phenomenon in the Chinese population, especially in the context of disease, are limited."( Population Pharmacokinetics of Rifampicin in Chinese Patients With Pulmonary Tuberculosis.
Huang, SP; Jing, Y; Wang, Q; Yang, JW; Zhang, J; Zhu, LQ, 2016
)
" The biochemical and immunological parameters were assessed on the same day that the pharmacokinetic evaluation of RIF was performed."( Clinical Pharmacokinetics of Rifampin in Patients with Tuberculosis and Type 2 Diabetes Mellitus: Association with Biochemical and Immunological Parameters.
Cortez-Espinosa, N; González-Amaro, R; Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Portales-Pérez, DP; Romano-Moreno, S; Vargas-Morales, JM, 2015
)
" A population pharmacokinetic model was developed to investigate the effects of pregnancy on rifampin pharmacokinetics."( Population Pharmacokinetics of Rifampin in Pregnant Women with Tuberculosis and HIV Coinfection in Soweto, South Africa.
Castel, S; Chaisson, RE; Cohn, S; Denti, P; Dooley, KE; Hoffmann, J; Martinson, N; Mashabela, F; McIlleron, H; Msandiwa, R; Wiesner, L, 2015
)
" Population pharmacokinetic modelling was applied to investigate the interaction and generate alternative doses to inform clinical trial design."( Simulation of the impact of rifampicin on once-daily darunavir/ritonavir pharmacokinetics and dose adjustment strategies: a population pharmacokinetic approach.
Back, D; Boffito, M; Dickinson, L; Khoo, S; Siccardi, M; Winston, A, 2016
)
"1 M phosphate buffer (10% dissolved) produced approximately 25% lower Cmax and AUC0-24 values, as compared with those achieved by RFP in ultrapure water in fasted rats."( Influence of Food on Rifampicin Pharmacokinetics in Rats.
Aoyama, T; Nogami, R; Shigeno, A; Shimada, S; Shimomura, H, 2016
)
" Standard pharmacokinetic parameters were calculated in all studies."( Effects of CYP3A4 Inhibitors Ketoconazole and Verapamil and the CYP3A4 Inducer Rifampicin on the Pharmacokinetic Parameters of Fostamatinib: Results from In Vitro and Phase I Clinical Studies.
Baluom, M; Brealey, C; Craven, K; Gillen, M; Grossbard, EB; Lau, D; Mant, T; Martin, P; Millson, D; Oliver, S; Sweeny, D, 2016
)
"Drug interactions often result from multiple pharmacokinetic changes, such as after rifampicin (RIF) and clarithromycin (CLA) in the treatment of abscessing lung diseases."( Pharmacokinetics and Pulmonary Distribution of Clarithromycin and Rifampicin after Concomitant and Consecutive Administration in Foals.
Berlin, S; Grube, M; Hasan, M; Keiser, M; Lumpe, S; Oswald, S; Siegmund, W; Spieckermann, L; Ullrich, A; Venner, M, 2016
)
"There are limited pharmacokinetic data for use of the first-line antituberculosis drugs during infancy (<12 months of age), when drug disposition may differ."( Pharmacokinetics of Rifampin, Isoniazid, Pyrazinamide, and Ethambutol in Infants Dosed According to Revised WHO-Recommended Treatment Guidelines.
Bekker, A; Donald, PR; Draper, HR; Hesseling, AC; McIlleron, HM; Murray, S; Schaaf, HS; van der Laan, L; Wiesner, L, 2016
)
" Plasma concentrations of moxifloxacin and rifampicin were determined using LC-MS at the designated time points after drug administration, and the main pharmacokinetic parameters were calculated."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
" A naïve-pooled non-compartmental data analysis was used to describe the pharmacokinetic properties of drugs in the two-age groups of children ≤ 4 years or > 4 years of age."( Naïve-pooled pharmacokinetic analysis of pyrazinamide, isoniazid and rifampicin in plasma and cerebrospinal fluid of Vietnamese children with tuberculous meningitis.
Bang, ND; Caws, M; Day, JN; Dung, NH; Duong, TN; Phuong, PN; Pouplin, T; Tarning, J; Thwaites, GE; Toi, PV, 2016
)
" In light of this dilemma in the interpretation of the pharmacokinetic data with rifampicin, several questions require further consideration."( Pharmacokinetic Interaction of Rifampicin with Oral Versus Intravenous Anticancer Drugs: Challenges, Dilemmas and Paradoxical Effects Due to Multiple Mechanisms.
Srinivas, NR, 2016
)
" Coadministration of rifampicin significantly changed the pharmacokinetic behavior of enrofloxacin orally administered by showing clearly lower AUC0-∞, AUC0-t, and Cmax as well as longer Tmax."( Potential pharmacokinetic effect of rifampicin on enrofloxacin in broilers: Roles of P-glycoprotein and BCRP induction by rifampicin.
Dai, X; Guo, M; Hu, D; Ren, W; Sun, Y; Wang, L; Zhang, Y, 2016
)
"We compared the pharmacokinetic (PK) exposure parameters of efavirenz (EFV) and its major inactive metabolite, 8-hydroxy-efavirenz (8-OH-EFV), in an open-label, single-sequence, and parallel design of HIV-infected and tuberculosis (TB)-HIV-coinfected Ethiopian patients in the HIV-TB Pharmagene study with 20 and 33 patients, respectively."( Long-Term Effect of Rifampicin-Based Anti-TB Regimen Coadministration on the Pharmacokinetic Parameters of Efavirenz and 8-Hydroxy-Efavirenz in Ethiopian Patients.
Aderaye, G; Aklillu, E; Amogne, W; Bertilsson, L; Burhenne, J; Habtewold, A; Makonnen, E; Owen, JS; Yimer, G, 2016
)
" Co-administration with ketoconazole (a strong CYP3A4 inhibitor) increased the Cmax , AUC and terminal elimination half-life of alisporivir by approximately two-, eight- ,and threefold, respectively."( The effects of CYP3A4 induction and inhibition on the pharmacokinetics of alisporivir in humans.
Barve, A; Crabbe, R; Dabovic, K; Dole, K; Grosgurin, P; Ke, J; Kovacs, SJ; Menetrey, A; Nicolas-Métral, V; Praestgaard, J; Stein, D; Sunkara, G; Zhang, J, 2015
)
"We evaluated the impact of a strong CYP3A4 inhibitor, ketoconazole, and a strong inducer, rifampicin, on the pharmacokinetic (PK) exposure of abiraterone in two studies in healthy men."( Impact on abiraterone pharmacokinetics and safety: Open-label drug-drug interaction studies with ketoconazole and rifampicin.
Acharya, M; Bernard, A; Chien, C; De Vries, R; Jiao, J; Monbaliu, J; Stieltjes, H; Tran, N; Vaccaro, N; Yu, M, 2015
)
" Rifampin decreased maximum plasma concentration (Cmax ) and area under the plasma concentration-time curve (AUC) from time zero to time of last measurable concentration (AUC0-t ) and from time zero to infinity (AUC0-∞ ) of ponatinib by 42%, 59%, and 63%, respectively, with no effect on time to Cmax ."( Evaluation of the effect of multiple doses of rifampin on the pharmacokinetics and safety of ponatinib in healthy subjects.
Davis, J; Dorer, DJ; Narasimhan, NI; Sonnichsen, D; Turner, CD, 2015
)
"A physiologically based pharmacokinetic (PBPK) model was developed for cobimetinib using in vitro data."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
"The PBPK model described cobimetinib pharmacokinetic profiles after both intravenous and oral administration of cobimetinib well and accurately simulated the itraconazole-cobimetinib DDI."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
" To help inform such an optimization, a physiologically based pharmacokinetic (PBPK) model was developed to predict time course, tissue-specific concentrations of RPT and its active metabolite, 25-desacetyl rifapentine (dRPT), in humans after specified administration schedules for RPT."( Physiologically Based Pharmacokinetic Model of Rifapentine and 25-Desacetyl Rifapentine Disposition in Humans.
Eppers, GJ; Reisfeld, B; Zurlinden, TJ, 2016
)
" After the completion of chemical synthesis, all the compounds were evaluated through in vitro antibacterial activity assay, some of which were further subject to in vivo rat pharmacokinetic assessment."( New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
Chen, C; Hu, W; Lv, F; Tang, Y; Wei, J; Zhu, T, 2016
)
"Based on ibrutinib pharmacokinetics and potential sensitivity towards CYP3A4-mediated drug-drug interactions (DDIs), a physiologically based pharmacokinetic approach was developed to mechanistically describe DDI with various CYP3A4 perpetrators in healthy men under fasting conditions."( Ibrutinib Dosing Strategies Based on Interaction Potential of CYP3A4 Perpetrators Using Physiologically Based Pharmacokinetic Modeling.
De Jong, J; de Zwart, L; Mannaert, E; Monshouwer, M; Snoeys, J; Sukbuntherng, J, 2016
)
" The relative bias and relative imprecision of each pharmacokinetic parameter for each drug were derived and assessed to choose the final designs."( Population pharmacokinetics, optimised design and sample size determination for rifampicin, isoniazid, ethambutol and pyrazinamide in the mouse.
Alameda, L; Chen, C; Ferrer, S; Ortega, F; Simonsson, US, 2016
)
" The AZM Cmax was measured in patients receiving daily therapy (250 mg of AZM daily, n = 77) or intermittent therapy (500 mg of AZM three times weekly, n = 89) for MAC-LD and daily therapy for Mycobacterium abscessus complex LD (MABC-LD) (250 mg of AZM daily, n = 55)."( Peak Plasma Concentration of Azithromycin and Treatment Responses in Mycobacterium avium Complex Lung Disease.
Daley, CL; Jeon, K; Jeong, BH; Kim, SY; Koh, WJ; Lee, SY; Moon, SM; Park, HY; Shin, SJ, 2016
)
"RMP peak concentration (Cmax) was sub-therapeutic (<8 μg/ml) in 88% of the patients."( Pharmacokinetics of thrice-weekly rifampicin, isoniazid and pyrazinamide in adult tuberculosis patients in India.
Chandrasekaran, V; Hemanth Kumar, AK; Kannan, T; Lavanya, J; Ramachandran, G; Ramesh, K; Sudha, V; Swaminathan, S; Vijayakumar, A, 2016
)
" A high proportion of TB patients had RMP Cmax below the expected range, which is a matter of concern."( Pharmacokinetics of thrice-weekly rifampicin, isoniazid and pyrazinamide in adult tuberculosis patients in India.
Chandrasekaran, V; Hemanth Kumar, AK; Kannan, T; Lavanya, J; Ramachandran, G; Ramesh, K; Sudha, V; Swaminathan, S; Vijayakumar, A, 2016
)
"2) mg⋅h/L, respectively; Cmax values were 14."( Pharmacokinetics and safety/tolerability of higher oral and intravenous doses of rifampicin in adult tuberculous meningitis patients.
Aarnoutse, R; Dian, S; Ganiem, AR; Hanggono Achmad, T; Hayati, E; Meijerhof-Jager, P; Purnama Dewi, A; Ruslami, R; Teulen, M; van Crevel, R; Yunivita, V, 2016
)
" As important signaling molecules, the alternations of BAs might favour the regulatory effect on enzymes and transporters involved in BAs physiological homeostasis at the transcriptional level, which could lead to pharmacokinetic changes of drugs."( Effect of cholecystectomy on bile acids as well as relevant enzymes and transporters in mice: Implication for pharmacokinetic changes of rifampicin.
Duan, Y; Ma, Y; Qin, H; Rao, Z; Wei, Y; Wu, X; Xi, L; Zhang, F; Zhang, J; Zhao, Y, 2017
)
"Parameters of BAs in different specimens, mRNA and protein expression of enzymes, transporters and nuclear receptors that relate to BAs homeostasis in liver and ileum, and the pharmacokinetic character of rifampicin were measured in sham-operated and cholecystectomized mice."( Effect of cholecystectomy on bile acids as well as relevant enzymes and transporters in mice: Implication for pharmacokinetic changes of rifampicin.
Duan, Y; Ma, Y; Qin, H; Rao, Z; Wei, Y; Wu, X; Xi, L; Zhang, F; Zhang, J; Zhao, Y, 2017
)
" Especially, the down-regulation of hepatic Cyp3a11 suggests that undesirable pharmacokinetic alternations of drugs especially Cyp3a11 substrates like rifampicin might occur in phase with cholecystectomy."( Effect of cholecystectomy on bile acids as well as relevant enzymes and transporters in mice: Implication for pharmacokinetic changes of rifampicin.
Duan, Y; Ma, Y; Qin, H; Rao, Z; Wei, Y; Wu, X; Xi, L; Zhang, F; Zhang, J; Zhao, Y, 2017
)
" Clinical DDIs of montelukast were evaluated using physiologically based pharmacokinetic modeling; and simulation of the interactions with gemfibrozil-CYP2C8 and OATP1B1/1B3 inhibitor, clarithromycin-CYP3A and OATP1B1/1B3 inhibitor, and itraconazole-CYP3A inhibitor, implicated OATPs-CYP2C8-CYP2C8 interplay as the primary determinant of montelukast pharmacokinetics."( Transporter-Mediated Hepatic Uptake Plays an Important Role in the Pharmacokinetics and Drug-Drug Interactions of Montelukast.
Bi, Y; El-Kattan, AF; Eng, H; Kalgutkar, AS; Kimoto, E; Lin, J; Rodrigues, AD; Scialis, R; Tremaine, LM; Varma, MV, 2017
)
"This report describes the pharmacokinetic profiles of chronically administered oral isoniazid and rifampin in one adult male and one adult female Asian elephant ( Elephas maximus ) that were asymptomatically infected with Mycobacterium tuberculosis ."( ISONIAZID AND RIFAMPIN PHARMACOKINETICS IN TWO ASIAN ELEPHANTS (ELEPHAS MAXIMUS) INFECTED WITH MYCOBACTERIUM TUBERCULOSIS.
Alsultan, A; Egelund, EF; Isaza, R; Peloquin, CA, 2016
)
" There are no studies describing the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
" The main objectives of this study were to 1) develop physiologically based pharmacokinetic (PBPK) models of bosutinib; 2) verify and refine the PBPK models based on clinical study results of bosutinib single-dose drug-drug interaction (DDI) with ketoconazole and rifampin, as well as single-dose drug-disease interaction (DDZI) in patients with renal and hepatic impairment; 3) apply the PBPK models to predict DDI outcomes in patients with weak and moderate CYP3A inhibitors; and 4) apply the PBPK models to predict DDZI outcomes in renally and hepatically impaired patients after multiple-dose administration."( Application of Physiologically Based Pharmacokinetic Modeling to the Understanding of Bosutinib Pharmacokinetics: Prediction of Drug-Drug and Drug-Disease Interactions.
Abbas, R; Hsyu, PH; Loi, CM; Ono, C; Yamazaki, S, 2017
)
"A population pharmacokinetic (PK) model was developed for cediranib to simulate cediranib exposure for different doses, including comedication with strong uridine glucuronosyl transferase/P-glycoprotein inducers such as rifampicin, in cancer patients."( Population pharmacokinetic and exposure simulation analysis for cediranib (AZD2171) in pooled Phase I/II studies in patients with cancer.
Al-Huniti, N; Henningsson, A; Li, J; Masson, E; Tang, W, 2017
)
" This report describes the development of a physiologically based pharmacokinetic (PBPK) model of rosuvastatin for prediction of pharmacokinetic (PK) DDIs."( Investigating Transporter-Mediated Drug-Drug Interactions Using a Physiologically Based Pharmacokinetic Model of Rosuvastatin.
Leil, T; Wang, Q; Zheng, M, 2017
)
"52), and apparent terminal half-life were observed when co-administered with multiple-dose rifampin vs."( The Effect of Single and Multiple Doses of Rifampin on the Pharmacokinetics of Doravirine in Healthy Subjects.
Anderson, MS; Brejda, J; Butterton, JR; Judge, T; Khalilieh, SG; Liu, R; Manthos, H; Sanchez, RI; Yee, KL, 2017
)
" Pyrazinamide pharmacokinetic (PK) data from 61 HIV/TB-coinfected patients in South Africa were used in the analysis."( Pharmacokinetics of Pyrazinamide and Optimal Dosing Regimens for Drug-Sensitive and -Resistant Tuberculosis.
Chirehwa, MT; Denti, P; McIlleron, H; Mthiyane, T; Onyebujoh, P; Rustomjee, R; Smith, P, 2017
)
" The final population pharmacokinetic model included an enzyme turnover model accounting for time-dependent elimination due to autoinduction, concentration-dependent clearance, and dose-dependent bioavailability."( A Population Pharmacokinetic Model Incorporating Saturable Pharmacokinetics and Autoinduction for High Rifampicin Doses.
Aarnoutse, RE; Boeree, MJ; Dawson, R; Diacon, AH; Gillespie, SH; Simonsson, USH; Svensson, RJ, 2018
)
" The mean hepatic clearances determined by in silico fitting for individual pharmacokinetic models of warfarin and midazolam in the aged group were, respectively, 23% and 56% smaller than those for the young group."( Effects of aging and rifampicin pretreatment on the pharmacokinetics of human cytochrome P450 probes caffeine, warfarin, omeprazole, metoprolol and midazolam in common marmosets genotyped for cytochrome P450 2C19.
Inoue, T; Kusama, T; Mogi, M; Sasaki, E; Shimizu, M; Toda, A; Uehara, S; Uno, Y; Utoh, M; Yamazaki, H, 2018
)
" The present study evaluated the possible pharmacokinetic interactions of selexipag with gemfibrozil, a strong CYP2C8 inhibitor, and rifampicin, an inducer of CYP2C8."( Effect of gemfibrozil and rifampicin on the pharmacokinetics of selexipag and its active metabolite in healthy subjects.
Boehler, M; Bruderer, S; Dingemanse, J; Halabi, A; Petersen-Sylla, M; Remeňová, T, 2017
)
" Subjects received a second dose of 30 mg cabotegravir on day 21 followed by pharmacokinetic sampling on days 21 to 28."( Effect of Rifampin on the Single-Dose Pharmacokinetics of Oral Cabotegravir in Healthy Subjects.
Ford, SL; Lou, Y; Patel, P; Spreen, W; Sutton, K; Tenorio, A; Trezza, C; Zhang, Z, 2017
)
" The clinical drug-drug interaction study results were reconciled well by a physiologically based pharmacokinetic model that incorporated a minor contribution of CYP3A to overall ixazomib clearance and quantitatively considered the strength of induction of CYP3A and intestinal P-glycoprotein by rifampin."( Effects of Strong CYP3A Inhibition and Induction on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor: Results of Drug-Drug Interaction Studies in Patients With Advanced Solid Tumors or Lymphoma and a Physiologically Based Pharmacokinetic Ana
Bessudo, A; Esseltine, DL; Gupta, N; Hanley, MJ; Ke, A; Liu, G; Nemunaitis, J; O'Neil, BH; Patel, C; Rasco, DW; Rowland Yeo, K; Sharma, S; Venkatakrishnan, K; Wang, B; Xia, C; Zhang, X, 2018
)
" Intensive pharmacokinetic sampling occurred in 63 patients after 6 weeks of treatment, and safety/tolerability was assessed."( Pharmacokinetics, Tolerability, and Bacteriological Response of Rifampin Administered at 600, 900, and 1,200 Milligrams Daily in Patients with Pulmonary Tuberculosis.
Aarnoutse, RE; Boeree, MJ; Colbers, A; Gillespie, SH; Haraka, F; Hoelscher, M; Kibiki, GS; Logger, JGM; Magis-Escurra, C; Mpagama, SG; Mtabho, CM; Phillips, PPJ; Plemper van Balen, G; Reither, K; Semvua, HH; Sumari-de Boer, IM; Te Brake, LHM; van den Boogaard, J; Wattenberg, M, 2017
)
"In recent years, physiologically based PharmacoKinetic (PBPK) modeling has received growing interest as a useful tool for the assessment of drug pharmacokinetics."( Prediction of drug-drug interactions using physiologically-based pharmacokinetic models of CYP450 modulators included in Simcyp software.
Daali, Y; Desmeules, JA; Marsousi, N; Rudaz, S, 2018
)
" This dose of ceftaroline was adequate to achieve the pharmacodynamic endpoint associated with efficacy for methicillin-resistant Staphyloccocus aureus."( Pharmacokinetics of Ceftaroline in a Preterm Infant With Methicillin-Resistant Staphylococcus Aureus Pneumonia.
Bernhardt, J; Gonzalez, D; Jhaveri, R; Laughon, M; Massaro, M; Salerno, SN, 2018
)
" The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physiologically based pharmacokinetic (PBPK) modeling."( A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4.
Gobburu, JVS; Liu, T, 2018
)
" A simultaneous pharmacokinetic model of parent and active metabolites was initially developed by incorporating data from in vitro, preclinical, and clinical pharmacokinetic studies in healthy volunteers and in patients with AML or advSM."( Simultaneous Physiologically Based Pharmacokinetic (PBPK) Modeling of Parent and Active Metabolites to Investigate Complex CYP3A4 Drug-Drug Interaction Potential: A Case Example of Midostaurin.
Chun, DY; Dutreix, C; Einolf, HJ; Gu, H; He, H; Ouatas, T; Rebello, S; Wang, L, 2018
)
" A combined population pharmacokinetic model was developed to jointly describe the pharmacokinetics of lopinavir and ritonavir in 32 HIV-infected children (16 with MDR-TB receiving treatment with combinations of high-dose isoniazid, pyrazinamide, ethambutol, ethionamide, terizidone, a fluoroquinolone, and amikacin and 16 without TB) who were established on a lopinavir-ritonavir-containing antiretroviral regimen."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
" Pharmacokinetic and pharmacogenetic studies are increasingly performed and might confirm their potential role in optimizing treatment outcome in specific settings and populations."( Pharmacokinetics and pharmacogenetics of anti-tubercular drugs: a tool for treatment optimization?
Bonora, S; Calcagno, A; Motta, I, 2018
)
" The combination of rifampicin with the new, poorly metabolised gamithromycin, a long-acting analogue of azithromycin and tulathromycin with lower pharmacokinetic interaction potential, might be a suitable alternative."( Intestinal and hepatic contributions to the pharmacokinetic interaction between gamithromycin and rifampicin after single-dose and multiple-dose administration in healthy foals.
Berlin, S; Grube, M; Hasan, M; Oswald, S; Scheuch, E; Siegmund, W; Ullrich, A; Venner, M; Wallstabe, S; Wegner, D, 2018
)
"To evaluate the pharmacokinetic interactions and pulmonary distribution of rifampicin and gamithromycin in healthy foals, and to investigate the cellular uptake of gamithromycin in vitro."( Intestinal and hepatic contributions to the pharmacokinetic interaction between gamithromycin and rifampicin after single-dose and multiple-dose administration in healthy foals.
Berlin, S; Grube, M; Hasan, M; Oswald, S; Scheuch, E; Siegmund, W; Ullrich, A; Venner, M; Wallstabe, S; Wegner, D, 2018
)
"16-fold increase of AUC of avatrombopag, prolonged terminal elimination phase half-life (from 19."( Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs.
Aluri, J; Boyd, P; Chang, MK; Ferry, J; Lai, WG; Nomoto, M; Rege, B; Schuck, E; Siu, YA; Yasuda, S; Zamora, CA, 2018
)
" A pharmacokinetic model was developed to describe uptake, and modelling was performed using ADAPT 5 software."( Functionalization of PLGA Nanoparticles with 1,3-β-glucan Enhances the Intracellular Pharmacokinetics of Rifampicin in Macrophages.
Dube, A; Gouveia, L; Hayeshi, R; Naicker, B; Paixao, P; Tukulula, M, 2018
)
" Data describing the Cmax and AUC were extracted."( Pharmacokinetics of rifampicin in adult TB patients and healthy volunteers: a systematic review and meta-analysis.
Aarnoutse, R; Alffenaar, JWC; Boeree, MJ; Davies, G; Koegelenberg, CFN; McIlleron, H; Peloquin, C; Pertinez, H; Ramachandran, G; Requena-Méndez, A; Ruslami, R; Stott, KE; Sturkenboom, MGG; Swaminathan, S; Tostmann, A, 2018
)
" These findings led us to investigate the factors influencing the underlying pharmacokinetic mechanisms of bosutinib with physiologically based pharmacokinetic (PBPK) models."( Application of Physiologically Based Pharmacokinetic Modeling in Understanding Bosutinib Drug-Drug Interactions: Importance of Intestinal P-Glycoprotein.
Costales, C; Kimoto, E; Loi, CM; Varma, MV; Yamazaki, S, 2018
)
"Dried blood spot (DBS) sampling for pharmacokinetic (PK) studies and therapeutic drug monitoring have unique advantages over venous sampling."( Evaluation of dried blood spot sampling for pharmacokinetic research and therapeutic drug monitoring of anti-tuberculosis drugs in children.
Aarnoutse, RE; Aguirre, S; Alffenaar, JW; Chaparro, G; Coronel, R; Gomez, R; Gonzalez, F; Huisman, J; Jongedijk, E; Kerkhoff, J; Magis-Escurra, C; Martial, LC; Martinez, N; Molinas, G; Pérez, D; Rodríguez, M; Roman, M; Touw, DJ, 2018
)
" Genetic polymorphisms and pharmacokinetic (PK) parameters of EFV400 without (PK1) and with INH/RIF following 4 (PK2) and 12 (PK3) weeks of coadministration were evaluated."( Pharmacokinetics of Efavirenz 400 mg Once Daily Coadministered With Isoniazid and Rifampicin in Human Immunodeficiency Virus-Infected Individuals.
Boffito, M; Cerrone, M; Day-Weber, I; Fedele, S; Hill, A; McClure, M; Neary, M; Owen, A; Wang, X; Weaver, C, 2019
)
" Because concurrent induction of these enzymes could affect ertugliflozin exposure, this study assessed the effect of multiple doses of rifampin on the pharmacokinetic properties of single-dose ertugliflozin."( Effect of Rifampin on the Pharmacokinetics of Ertugliflozin in Healthy Subjects.
Cutler, DL; Dawra, VK; Hickman, A; Liang, Y; Matschke, K; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG, 2018
)
" Plasma samples for ertugliflozin pharmacokinetic analysis were collected during 72hours after dosing on day 1 of period 1 and day 8 of period 2 and analyzed using a validated HPLC-MS/MS method."( Effect of Rifampin on the Pharmacokinetics of Ertugliflozin in Healthy Subjects.
Cutler, DL; Dawra, VK; Hickman, A; Liang, Y; Matschke, K; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG, 2018
)
"To predict the optimal chemoprophylactic dose of mefloquine in infants of 5-10 kg using physiologically based pharmacokinetic (PBPK) and clinical effectiveness models."( Development of a physiologically based pharmacokinetic model for mefloquine and its application alongside a clinical effectiveness model to select an optimal dose for prevention of malaria in young Caucasian children.
Cleary, Y; Johnson, TN; Parrott, N; Reigner, B; Smith, JR; Toovey, S, 2019
)
"1 and verified against clinical pharmacokinetic data in adults; the final model, accounting for developmental physiology and enzyme ontogeny was then applied in the paediatric population."( Development of a physiologically based pharmacokinetic model for mefloquine and its application alongside a clinical effectiveness model to select an optimal dose for prevention of malaria in young Caucasian children.
Cleary, Y; Johnson, TN; Parrott, N; Reigner, B; Smith, JR; Toovey, S, 2019
)
"To describe the pharmacokinetics of isoniazid and acetyl-isoniazid in TB/HIV-coinfected patients, and assess the effects of efavirenz co-administration and a 50% increase in the dose of rifampicin on the pharmacokinetic parameters of isoniazid and acetyl-isoniazid."( Effect of efavirenz-based antiretroviral therapy and high-dose rifampicin on the pharmacokinetics of isoniazid and acetyl-isoniazid.
Affolabi, D; Bah-Sow, O; Chirehwa, MT; Denti, P; McIlleron, H; Merle, C; Wiesner, L, 2019
)
"Dosing recommendations for treating childhood tuberculosis (TB) were revised by the World Health Organization, yet so far, pharmacokinetic studies that have evaluated these changes are relatively limited."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
" Pharmacokinetic samplings were done 16 weeks after initiation of efavirenz-based anti-retroviral therapy and eight weeks after completion of rifampicin-based anti-tuberculosis treatment."( Long-term efavirenz pharmacokinetics is comparable between Tanzanian HIV and HIV/Tuberculosis patients with the same CYP2B6*6 genotype.
Aklillu, E; Bertilsson, L; Burhenne, J; Janabi, M; Kitabi, EN; Minzi, OMS; Mugusi, F; Mugusi, S; Sasi, P, 2018
)
" Pharmacokinetic parameters can be affected by comorbidities or the interaction of drugs with food."( Intra-individual effects of food upon the pharmacokinetics of rifampicin and isoniazid.
Ardrey, A; Davies, G; Jave, O; López-Romero, SL; Moore, DAJ; Requena-Méndez, A; Ward, SA; Waterhouse, D, 2019
)
" Three phase 1, open-label, drug-drug interaction studies were conducted to examine the pharmacokinetic interactions of orally administered rolapitant with midazolam, rolapitant with ketoconazole, and rolapitant with rifampin."( Pharmacokinetic Interactions of Rolapitant With Cytochrome P450 3A Substrates in Healthy Subjects.
Arora, S; Christensen, J; Hughes, L; Lu, S; Wang, J; Wang, X; Zhang, ZY, 2019
)
" The aim of this study was to simulate and predict drug-drug interactions (DDIs) between these LA antiretroviral agents and rifampicin using physiologically based pharmacokinetic (PBPK) modeling."( Predicting Drug-Drug Interactions Between Rifampicin and Long-Acting Cabotegravir and Rilpivirine Using Physiologically Based Pharmacokinetic Modeling.
Back, D; Chiong, J; Curley, P; Flexner, C; Owen, A; Rajoli, RKR; Siccardi, M, 2019
)
" Qualified PBPK models were utilized for pharmacokinetic prediction of DDIs."( Predicting Drug-Drug Interactions Between Rifampicin and Long-Acting Cabotegravir and Rilpivirine Using Physiologically Based Pharmacokinetic Modeling.
Back, D; Chiong, J; Curley, P; Flexner, C; Owen, A; Rajoli, RKR; Siccardi, M, 2019
)
" In the experiment in vivo, the process of rifampicin was studied after intragastric administration of rifampicin and rifampicin+ tannins in Galla Chinensis, and then the pharmacokinetic parameters were calculated."( [Effects of tannins in Galla Chinensis on pharmacokinetics of rifampicin in vivo and in vitro].
Chen, J; Dong, ZY; Huang, JM; Jin, R; Liu, YL; Tang, H; Wang, MS; Wang, Q; Ye, JC, 2018
)
" While concomitant food intake and HIV infection explain part of the pharmacokinetic variability associated with rifapentine, few studies have evaluated the contribution of genetic polymorphisms."( A Population Pharmacokinetic Analysis Shows that Arylacetamide Deacetylase (AADAC) Gene Polymorphism and HIV Infection Affect the Exposure of Rifapentine.
Charalambous, S; Dawson, R; Denti, P; Dorman, S; Egan, D; Francis, J; Gupte, N; Harrison, TS; Hatherill, M; Jindani, A; McIlleron, HM; Mungofa, S; Olagunju, A; Owen, A; Wiesner, L; Zvada, SP, 2019
)
"An in vitro dynamic pharmacokinetic (PK) cell culture system was developed to more precisely simulate physiologic nanoparticle/drug exposure."( In vitro Pharmacokinetic Cell Culture System that Simulates Physiologic Drug and Nanoparticle Exposure to Macrophages.
Kutscher, HL; Morse, GD; Prasad, PN; Reynolds, JL, 2019
)
"The dynamic PK cell culture system mimics a one-compartment elimination pharmacokinetic profile to properly mimic in vivo extracellular exposure."( In vitro Pharmacokinetic Cell Culture System that Simulates Physiologic Drug and Nanoparticle Exposure to Macrophages.
Kutscher, HL; Morse, GD; Prasad, PN; Reynolds, JL, 2019
)
"We report the prevalence and effect of genetic variability on pharmacokinetic parameters of isoniazid and rifampicin."( Effects of genetic variability on rifampicin and isoniazid pharmacokinetics in South African patients with recurrent tuberculosis.
Adamson, J; Chirehwa, M; Denti, P; Govender, K; McIlleron, H; Naidoo, A; Naidoo, K; Ncgapu, S; Padayatchi, N; Ramsuran, V; Singh, R; Yende-Zuma, N, 2019
)
" Olanzapine and samidorphan pharmacokinetic parameters were determined after OLZ/SAM dosing on days 1 and 22."( A Phase I Open-Label Study to Evaluate the Effects of Rifampin on the Pharmacokinetics of Olanzapine and Samidorphan Administered in Combination in Healthy Human Subjects.
Kumar, V; McDonnell, D; Sun, L; von Moltke, L; Yu, M, 2019
)
" Pharmacokinetic analyses of the CYP2C19 probe drug, omeprazole, were performed before and after rifampicin or fluvoxamine administration."( Effect of co-administered inducer or inhibitor on omeprazole pharmacokinetics based on CYP2C19 genotype.
Hakamata, A; Inui, N; Kamiya, C; Miyakawa, S; Namiki, N; Odagiri, K; Tanaka, S; Uchida, S; Watanabe, H, 2019
)
" We performed a multicenter, prospective pharmacokinetic (PK) and safety study of intravenous rifampin in infants of <121 days postnatal age (PNA)."( Rifampin Pharmacokinetics and Safety in Preterm and Term Infants.
Anand, R; Benjamin, DK; Boakye-Agyeman, F; Cohen-Wolkowiez, M; Cotten, CM; Hudak, ML; Laughon, MM; Lewandowski, A; Poindexter, BB; Smith, PB; Sullivan, JE, 2019
)
" Inter-individual pharmacokinetic variability and the effect of age, nutritional status, Human immunodeficiency virus (HIV) infection, acetylator genotype may need to be accounted for in striving for the dosages best suited for an individual."( Pharmacokinetics of First-Line Anti-Tubercular Drugs.
Kabra, SK; Lodha, R; Mukherjee, A, 2019
)
"The population pharmacokinetics and lysophosphatidic acid C18:2 response of GLPG1690 were adequately described by a combined population pharmacokinetic and pharmacokinetic/pharmacodynamic model."( Population Pharmacokinetic and Pharmacodynamic Analysis of GLPG1690, an Autotaxin Inhibitor, in Healthy Volunteers and Patients with Idiopathic Pulmonary Fibrosis.
Allamasey, L; Blanqué, R; Desrivot, J; Diderichsen, PM; Fagard, L; Fieuw, A; Namour, F; Taneja, A; Van der Aar, E, 2019
)
" Elimination half-life was not affected."( Influence of Rifampin-Mediated Organic Anion-Transporting Polypeptide 1B1/1B3 Inhibition on the Pharmacokinetics of Clazosentan.
Dingemanse, J; Dogterom, P; Juif, PE; Ufer, M; Voors-Pette, C, 2019
)
" To exploit the full potential of PET, quantitative pharmacokinetic models are required."( Towards Improved Pharmacokinetic Models for the Analysis of Transporter-Mediated Hepatic Disposition of Drug Molecules with Positron Emission Tomography.
Bauer, M; Blaickner, M; Hacker, M; Hernández Lozano, I; Karch, R; Langer, O; Matsuda, A; Wulkersdorfer, B; Zeitlinger, M, 2019
)
" We aimed to establish a semi-physiologically based pharmacokinetic (semi-PBPK) model involving both enzyme and transporter turnover to simultaneously predict pharmacokinetic interaction of rifampicin with oral versus intravenous substrates of cytochrome P450 (CYP) 3A4/P‑glycoprotein (P-GP) in human."( Simultaneously predict pharmacokinetic interaction of rifampicin with oral versus intravenous substrates of cytochrome P450 3A/P‑glycoprotein to healthy human using a semi-physiologically based pharmacokinetic model involving both enzyme and transporter t
Chen, Y; Liu, L; Liu, XD; Qian, CQ; Zhao, KJ, 2019
)
"To evaluate the proportion of children with lopinavir Cmin ≥1 mg/L when receiving a novel 8-hourly lopinavir/ritonavir dosing strategy during rifampicin co-treatment."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
"HIV-infected children on lopinavir/ritonavir and rifampicin were enrolled in a prospective pharmacokinetic study."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
" Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies."( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron.
Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019
)
"This study applied pharmacokinetic modelling using virtual clinical trials, to pharmacokinetically quantify the extent and impact of rifampicin-mediated drug-drug interactions (DDI) on methadone plasma concentrations."( The optimization of methadone dosing whilst treating with rifampicin: A pharmacokinetic modeling study.
Al Zabit, D; Badhan, RKS; Gittins, R, 2019
)
" A physiologically based pharmacokinetic (PBPK) model was established to evaluate the changes in the ruxolitinib systemic exposures with co-administration of CYP3A4 and CYP2C9 perpetrators."( Drug-drug interaction (DDI) assessments of ruxolitinib, a dual substrate of CYP3A4 and CYP2C9, using a verified physiologically based pharmacokinetic (PBPK) model to support regulatory submissions.
Aslanis, V; He, H; Heimbach, T; Huth, F; Jin, Y; Schiller, H; Umehara, K, 2019
)
"We predicted the drug-drug interaction (DDI) potential of siponimod in presence of cytochrome P450 (CYP)2C9/CYP3A4 inhibitors/inducers in subjects with different CYP2C9 genotypes by physiologically-based pharmacokinetic (PK) modeling."( Prediction of the Impact of Cytochrome P450 2C9 Genotypes on the Drug-Drug Interaction Potential of Siponimod With Physiologically-Based Pharmacokinetic Modeling: A Comprehensive Approach for Drug Label Recommendations.
Gardin, A; He, H; Huth, F; Umehara, K, 2019
)
"A population pharmacokinetic (PopPK) model for pretomanid was developed using data from 14 studies in the pretomanid development program: six phase 1 studies, six phase 2 studies, and two phase 3 studies."( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid.
Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 2019
)
" We previously constructed a physiologically-based pharmacokinetic (PBPK) model of rifampicin accounting for the components for the induction of cytochrome P450 (CYP) 3A/CYP2C9 and the inhibition of organic anion transporting polypeptide 1B (OATP1B)."( Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for Predicting Interactions With Drugs and an Endogenous Biomarker via Complex Mechanisms Including Organic Anion Transporting Polypeptide 1B Induction.
Asaumi, R; Imawaka, H; Kusuhara, H; Lee, W; Menzel, K; Nunoya, KI; Sugiyama, Y, 2019
)
"Physiologically-based pharmacokinetic (PBPK) modeling is a powerful tool to quantitatively describe drug disposition profiles in vivo, thereby providing an alternative to predict drug-drug interactions (DDIs) that have not been tested clinically."( Physiologically-Based Pharmacokinetic Modeling Approach to Predict Rifampin-Mediated Intestinal P-Glycoprotein Induction.
Costales, C; Eatemadpour, S; Kimoto, E; Lazzaro, S; Varma, MV; Yamazaki, S, 2019
)
" Intensive RAL pharmacokinetic sampling was conducted 5 to 8 days after antiretroviral therapy was initiated; a fourth antiretroviral agent was then added."( Pharmacokinetics and safety of a raltegravir-containing regimen in HIV-infected children aged 2-12 years on rifampicin for tuberculosis.
Acosta, EP; Bradford, S; Cotton, MF; Denson, K; Hesseling, A; Hovind, L; Krogstad, P; Marillo, L; Masenya, M; Mathiba, SR; Meyers, T; Moye, J; Samson, P; Sise, T; Teppler, H; Townley, E, 2019
)
"Giving 12 mg/kg twice daily of the chewable RAL formulation achieved pharmacokinetic targets safely in HIV-infected children receiving RIF for TB."( Pharmacokinetics and safety of a raltegravir-containing regimen in HIV-infected children aged 2-12 years on rifampicin for tuberculosis.
Acosta, EP; Bradford, S; Cotton, MF; Denson, K; Hesseling, A; Hovind, L; Krogstad, P; Marillo, L; Masenya, M; Mathiba, SR; Meyers, T; Moye, J; Samson, P; Sise, T; Teppler, H; Townley, E, 2019
)
" Median (IQR) Cmax and Tmax were 10."( Role of pharmacogenetics in rifampicin pharmacokinetics and the potential effect on TB-rifampicin sensitivity among Ugandan patients.
Aklillu, E; Kengo, A; Kutesa, B; McHugh, TD; Mukonzo, JK; Nanzigu, S; Pohanka, A; Zumla, A, 2020
)
"To evaluate the safety and pharmacokinetic profile of adjusted doses of darunavir/ritonavir with rifampicin."( Pharmacokinetic profile and safety of adjusted doses of darunavir/ritonavir with rifampicin in people living with HIV.
Ebrahim, I; Maartens, G; McIlleron, H; Orrell, C; Smythe, W; Wiesner, L, 2020
)
" A physiologically based pharmacokinetic (PBPK) model incorporating the metabolites was developed to predict the effect of other strong and moderate CYP3A4 inhibitors and inducers."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
" Thereby, population pharmacokinetic parameters were estimated followed by elucidating relations between the parameters and statistical factors."( The Population Pharmacokinetics of Rifampicin in Japanese Pulmonary Tuberculosis Patients.
Atsuda, K; Kobayashi, M; Kohno, H; Koike, Y; Maruoka, D; Nagai, H; Nishimura, T, 2020
)
" Pharmacokinetic parameters were calculated using noncompartmental analysis, and safety was assessed."( Effects of itraconazole and rifampicin on the single-dose pharmacokinetics of the nonsteroidal mineralocorticoid receptor blocker esaxerenone in healthy Japanese subjects.
Irie, S; Ishizuka, H; Ishizuka, T; Kato, M; Kirigaya, Y; Nakatsu, T; Nishikawa, Y; Shimizu, T; Shiramoto, M; Uchimaru, H, 2020
)
" This study illustrates the importance of incorporating target biology, drug-target interactions and in vitro clearance parameters into mechanistic PBPK/PD models and the utility of such models for pharmacokinetic, pharmacodynamic and DDI predictions."( A Translational Physiologically Based Pharmacokinetics/Pharmacodynamics Framework of Target-Mediated Disposition, Target Inhibition and Drug-Drug Interactions of Bortezomib.
Hanley, M; Iwasaki, S; Venkatakrishnan, K; Xia, C; Zhu, A, 2020
)
"This study was aimed at the evaluation of rifampicin's enzyme induction effect on the pharmacokinetic parameters of orally administered metoclopramide."( Influence of Rifampicin Pre-treatment on the In vivo Pharmacokinetics of Metoclopramide in Pakistani Healthy Volunteers Following Concurrent Oral Administration.
Abrar, MA; Anwer, N; Kaukab, I; Murtaza, G; Shah, SNH, 2020
)
"This randomized, single-blind, two-phase cross-over pharmacokinetic study separated by a 4-week washout period was conducted at a single center in Pakistan."( Influence of Rifampicin Pre-treatment on the In vivo Pharmacokinetics of Metoclopramide in Pakistani Healthy Volunteers Following Concurrent Oral Administration.
Abrar, MA; Anwer, N; Kaukab, I; Murtaza, G; Shah, SNH, 2020
)
" We found that 12 mg/kg twice daily raltegravir chewable tablets (administered after crushing) safely achieved pharmacokinetic targets in children living with HIV aged 4 weeks to <2 years receiving concurrent rifampin to treat TB."( Pharmacokinetics and Safety of a Raltegravir-Containing Regimen in Children Aged 4 Weeks to 2 Years Living With Human Immunodeficiency Virus and Receiving Rifampin for Tuberculosis.
Acosta, EP; Bradford, S; Brown, E; Denson, K; Fairlie, L; Graham, B; Hovind, L; Krogstad, P; Mathiba, SR; Meyers, T; Moye, J; Samson, P; Sise, T; Slade, G; Teppler, H; Townley, E; Winckler, JL, 2021
)
"Despite a recent expansion in the recognition of the potential utility of coproporphyrin (CP) as an endogenous biomarker of organic anion-transporting polypeptide (OATP) 1B activity, there have been few detailed studies of CP's pharmacokinetic behavior and an overall poor understanding of its pharmacokinetic fate from tissues and excretion."( Absorption and Disposition of Coproporphyrin I (CPI) in Cynomolgus Monkeys and Mice: Pharmacokinetic Evidence to Support the Use of CPI to Inform the Potential for Organic Anion-Transporting Polypeptide Inhibition.
Fancher, RM; Gan, J; Gu, X; Hong, Y; Lai, Y; Shen, H; Sinz, M; Tian, Y; Wang, L, 2020
)
" A physiologically-based pharmacokinetic (PBPK) model was developed integrating in vitro, preclinical, and clinical data of HVs and patients with cancer."( Ribociclib Drug-Drug Interactions: Clinical Evaluations and Physiologically-Based Pharmacokinetic Modeling to Guide Drug Labeling.
Chakraborty, A; Dhuria, SV; Elmeliegy, M; He, H; Heimbach, T; Huth, F; Ji, Y; Miller, M; Samant, TS; Schiller, H; Umehara, K, 2020
)
" To enable administering safe doses of molibresib to healthy volunteers, this 2-part randomized, open-label, crossover drug-drug interaction trial was conducted as an adaptive design study using physiologically based pharmacokinetic (PBPK) modeling and simulation to predict the lowest doses of molibresib that could be safely administered alone (10 mg) or with itraconazole and rifampicin (strong inhibitors and inducers of CYP3A and P-gp, respectively)."( An Adaptive Physiologically Based Pharmacokinetic-Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers.
Collins, G; Ferron-Brady, G; Kremer, BE; Patel, A; Riddell, K; Schramek, D; Zhou, Y, 2021
)
"Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)."( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia.
Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020
)
" As M9 concentrations have not been quantified in previous clinical studies, a physiologically based pharmacokinetic model was developed to investigate the change in M9 exposure when doravirine is coadministered with CYP3A inducers."( Physiologically Based Pharmacokinetic Modeling of Doravirine and Its Major Metabolite to Support Dose Adjustment With Rifabutin.
Cabalu, TD; Dreyer, D; Fillgrove, KL; Iwamoto, M; Khalilieh, SG; Kuo, Y; Liu, Y; McClain, S; Sanchez, RI; Stoch, SA; Triantafyllou, I; Wenning, L; Yee, KL, 2021
)
"The aim of this review is to summarize the pharmacokinetic drug-drug interaction (DDI) of 45 antibiotics commonly used in sepsis care in China."( Pharmacokinetic Drug-drug Interaction of Antibiotics Used in Sepsis Care in China.
Cheng, C; Chu, Z; He, R; Li, J; Wang, Y; Yu, X, 2021
)
" Physiologically-based pharmacokinetic models for apixaban and rivaroxaban were developed to estimate the net effect of CYP3A induction, P-gp inhibition, and P-gp induction by rifampicin."( Physiologically-Based Pharmacokinetic Modeling for the Prediction of a Drug-Drug Interaction of Combined Effects on P-glycoprotein and Cytochrome P450 3A.
Bonate, PL; Choules, MP; Komatsu, K; Otsuka, Y, 2020
)
" Measuring the pharmacodynamic (PD) efficacy of FIR on DNL provides a unique opportunity to determine optimal dosing strategies for liver-targeted OATP substrates in settings of altered OATP function."( Organic Anion Transporting Polypeptide Inhibition Dramatically Increases Plasma Exposure but not Pharmacodynamic Effect nor Inferred Hepatic Intracellular Exposure of Firsocostat.
Ampaw, L; Beysen, C; Garrison, KL; Kearney, BP; Kirby, BJ; Lutz, JD; Mathias, A; Myers, RP; Qin, AR; Yue, MS, 2021
)
" For the first time, we developed a physiologically based pharmacokinetic (PBPK) model-based approach to assess CYP3A-mediated drug-drug interaction (DDI) risk for polatuzumab vedotin (Polivy), an anti-CD79b-vc-monomethyl auristatin E (MMAE) antibody-drug conjugate (ADC)."( Physiologically Based Pharmacokinetic Model-Informed Drug Development for Polatuzumab Vedotin: Label for Drug-Drug Interactions Without Dedicated Clinical Trials.
Chen, Y; Ding, H; Girish, S; Jin, J; Li, C; Lu, D; Ma, F; Mao, J; Miles, D; Samineni, D; Shi, R; Wright, M, 2020
)
"To provide whole-body physiologically based pharmacokinetic (PBPK) models of the potent clinical organic anion transporter (OAT) inhibitor probenecid and the clinical OAT victim drug furosemide for their application in transporter-based drug-drug interaction (DDI) modeling."( Physiologically Based Pharmacokinetic Models of Probenecid and Furosemide to Predict Transporter Mediated Drug-Drug Interactions.
Britz, H; Fernandez, É; Hanke, N; Lehr, T; Nock, V; Prasad, B; Stopfer, P; Taub, ME; Wang, T, 2020
)
" Participants provided sparse pharmacokinetic (PK) sampling at baseline and weeks 2 and 4 for trough nevirapine determination."( Nevirapine pharmacokinetics in HIV-infected persons receiving rifapentine and isoniazid for TB prevention.
Benson, CA; Chaisson, RE; Fletcher, CV; Gupta, A; Hakim, J; Kanyama, C; Langat, D; Leon-Cruz, J; Mwelase, N; Omoz-Oarhe, A; Podany, AT; Supparatpinyo, K; Swindells, S, 2021
)
" Physiologically based pharmacokinetic models built upon two independent bottom-up approaches predicted elevation of E7766 plasma exposure when administered with Rifampicin, a clinical OATP inhibitor."( Prediction of Transporter-Mediated Drug-Drug Interactions and Phenotyping of Hepatobiliary Transporters Involved in the Clearance of E7766, a Novel Macrocycle-Bridged Dinucleotide.
Burgess, L; Dixit, V; Hart, A; Jiang, R; Kim, DS; Lai, WG, 2021
)
" In addition, rifampicin exists either as amorphous or crystalline particles, which may show different pharmacokinetic behaviour."( Pharmacokinetics of rifampicin after repeated intra-tracheal administration of amorphous and crystalline powder formulations to Sprague Dawley rats.
Das, SC; Dummer, J; Hill, PC; Katare, R; Khadka, P; Sinha, S; Tucker, IG, 2021
)
" We investigated whether the single-dose pharmacokinetic (PK) profile of pamiparib is altered by coadministration of a strong CYP3A inducer (rifampin) or a strong CYP3A inhibitor (itraconazole) in patients with solid tumors."( The pharmacokinetics of pamiparib in the presence of a strong CYP3A inhibitor (itraconazole) and strong CYP3A inducer (rifampin) in patients with solid tumors: an open-label, parallel-group phase 1 study.
Andreu-Vieyra, C; Bulat, I; Lin, C; Maglakelidze, M; Mu, S; Sahasranaman, S; Skarbova, V; Skrzypczyk-Ostaszewicz, A, 2021
)
"The objective of this study was to determine the effects of the OATP inhibitor rifampin on pharmacokinetic of Biopharmaceutics Drug Disposition Classification System Class 1 compound fluvastatin."( Effects of Single Dose Rifampin on the Pharmacokinetics of Fluvastatin in Healthy Volunteers.
Benet, LZ; Frassetto, LA; Kozachenko, I; Okochi, H; Sodhi, JK; Xiang, Y, 2021
)
"An important clindamycin-rifampicin pharmacokinetic (PK) interaction has been reported, but the potential influence of the clindamycin administration route on that interaction is unknown."( Influence of the clindamycin administration route on the magnitude of clindamycin-rifampicin interaction: a prospective pharmacokinetic study.
Billaud, E; Heym, B; Jannot, AS; Jullien, V; Kitzis, MD; Magreault, S; Marmor, S; Salmon, D; Salomon, L; Zeller, V, 2021
)
"Tetracyclines are widely used as oral therapy of MRSA infection, however, the pharmacodynamic underpinning is absent."( The pharmacodynamics of minocycline alone and in combination with rifampicin against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
Attwood, M; Bowker, KE; MacGowan, AP; Noel, AR, 2021
)
"We employed an in vitro pharmacokinetic model to study the pharmacodynamics of minocycline alone and in combination with rifampicin."( The pharmacodynamics of minocycline alone and in combination with rifampicin against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
Attwood, M; Bowker, KE; MacGowan, AP; Noel, AR, 2021
)
" Population pharmacokinetic models for olanzapine and samidorphan were developed using data from 11 clinical studies in healthy subjects or patients with schizophrenia."( Population Pharmacokinetics of Olanzapine and Samidorphan When Administered in Combination in Healthy Subjects and Patients With Schizophrenia.
Mills, R; Rege, B; Sadler, BM; Sun, L, 2021
)
" A pooled population pharmacokinetic analysis with 744 plasma medroxyprogesterone acetate concentrations from 138 women treated with depot medroxyprogesterone and antiretroviral/antituberculosis treatment across three clinical trials was performed."( A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug-Drug Interactions With Antiretroviral and Antituberculosis Treatment.
Cohn, SE; Denti, P; Dooley, KE; Firnhaber, C; Francis, J; Godfrey, C; Kendall, MA; McIlleron, H; Mngqibisa, R; Wu, X, 2021
)
" A physiologically based pharmacokinetic (PBPK) model was constructed to predict plasma concentration-time profiles of selumetinib, and to evaluate the impact of coadministering moderate cytochrome P450 (CYP) 3A4/2C19 inhibitors/inducers."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
"Physiologically based pharmacokinetic (PBPK) models are increasingly used in drug development to simulate changes in both systemic and tissue exposures that arise as a result of changes in enzyme and/or transporter activity."( Physiologically Based Pharmacokinetic Modeling of Transporter-Mediated Hepatic Disposition of Imaging Biomarker Gadoxetate in Rats.
Darwich, AS; Galetin, A; Melillo, N; Ogungbenro, K; Schütz, G; Scotcher, D; Sourbron, S; Tadimalla, S; Ziemian, S, 2021
)
"Moxifloxacin is a recommended drug for rifampin-resistant tuberculosis (RR-TB) treatment, but there is limited pediatric pharmacokinetic and safety data, especially in young children."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
" Pharmacokinetic simulations were performed to predict expected exposure and optimal weight-banded dosing."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
" Pharmacokinetic sampling was performed with the first (second/third trimester) and twelfth (third trimester/postpartum) doses."( Pharmacokinetics and Safety of 3 Months of Weekly Rifapentine and Isoniazid for Tuberculosis Prevention in Pregnant Women.
Bradford, S; Britto, P; Chakhtoura, N; Chalermchockcharoentkit, A; Chipato, T; Dooley, KE; Gupta, A; Jayachandran, P; Kamthunzi, P; Langat, D; Mathad, JS; Montepiedra, G; Norman, J; Patil, S; Popson, S; Rouzier, V; Savic, R; Townley, E; Wiesner, L; Zhang, N, 2022
)
" Very few pharmacokinetic data are available in this population."( Ciprofloxacin population pharmacokinetics during long-term treatment of osteoarticular infections.
Aubry, A; Bleibtreu, A; Chauvin, C; Comets, E; Fourniols, E; Funck-Brentano, C; Jaureguiberry, S; Llopis, B; Noe, G; Tissot, N; Urien, S; Zahr, N, 2021
)
" Pooled LPV AUC12 (157 203 hours × ng/mL) and Ctrough (9876 ng/mL) were similar to historical controls; RBT AUC24 (7374 hours × ng/mL) and Ctrough (208 ng/mL) were higher, although 3 participants in arm C had RBT Cmax <250 ng/mL."( Safety and Pharmacokinetics of Double-Dose Lopinavir/Ritonavir + Rifampin Versus Lopinavir/Ritonavir + Daily Rifabutin for Treatment of Human Immunodeficiency Virus-Tuberculosis Coinfection.
Benson, CA; Cardoso, SW; Fletcher, CV; Ive, P; Kendall, MA; Lalloo, U; Podany, AT; Wu, X, 2021
)
" Faster RBT clearance and low Cmax in 3 participants on RBT+RAL requires further study."( Safety and Pharmacokinetics of Double-Dose Lopinavir/Ritonavir + Rifampin Versus Lopinavir/Ritonavir + Daily Rifabutin for Treatment of Human Immunodeficiency Virus-Tuberculosis Coinfection.
Benson, CA; Cardoso, SW; Fletcher, CV; Ive, P; Kendall, MA; Lalloo, U; Podany, AT; Wu, X, 2021
)
" Physiologically based pharmacokinetic (PBPK) modelling was performed to predict the drug-drug interaction (DDI) effect of cytochrome P450 (CYP)3A modulators on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment."( Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment.
Igawa, Y; Ishizuka, H; Ishizuka, T; Shimizu, T; Watanabe, A; Yamada, M, 2022
)
" We report the first pharmacokinetic data for these FDC tablets in Zambian and South African children in the treatment-shortening SHINE trial."( Pharmacokinetics of First-Line Drugs in Children With Tuberculosis, Using World Health Organization-Recommended Weight Band Doses and Formulations.
Aarnoutse, R; Chabala, C; Chirehwa, M; Choo, L; Gibb, D; Hesseling, AC; Hissar, S; Kapasa, M; Kinikar, A; LeBeau, K; Mave, V; McIlleron, H; Mulenga, V; Palmer, M; Turkova, A; van der Zalm, M; Wiesner, L; Wobudeya, E; Zimba, KM, 2022
)
" Pharmacokinetic data from days 14 and 15 were analysed using population modelling and safety data reviewed."( Pharmacokinetics and safety of high-dose rifampicin in children with TB: the Opti-Rif trial.
Aarnoutse, RE; Denti, P; Draper, HR; Fairlie, L; Garcia-Prats, AJ; Hesseling, AC; Karlsson, MO; Masenya, M; Norman, J; Schaaf, HS; Svensson, EM; van der Laan, LE; Wiesner, L; Winckler, J, 2021
)
" We developed a physiologically based pharmacokinetic model in Simcyp version 19, with available and newly generated in vitro and in vivo data, to estimate pharmacokinetic parameters of moxifloxacin alone and when administered with rifampicin."( Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling.
Aarnoutse, RE; Boeree, MJ; Bolwerk, C; Burger, DM; Greupink, R; Hoefsloot, W; Koenderink, JB; Kuipers, S; Litjens, CHC; Magis-Escurra, C; Ruslami, R; Russel, FGM; Svensson, EM; Te Brake, LHM; van Crevel, R; van den Broek, PHH; van den Heuvel, JJMW; van Ingen, J; van Laarhoven, A; Verscheijden, LFM, 2022
)
"Children with drug-susceptible tuberculosis in Malawi and South Africa underwent pharmacokinetic sampling while receiving first-line tuberculosis drugs as single formulations according the 2010 WHO recommended doses."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
" Serum CAM, 14-OH CAM, EB, and RFP concentrations were measured before and at 2, 4, 6, and 12 or 24 h after administration on days 14, 28, and 42, and pharmacokinetic parameters were calculated."( Impact of rifampicin on the pharmacokinetics of clarithromycin and 14-hydroxy clarithromycin in patients with multidrug combination therapy for pulmonary Mycobacterium avium complex infection.
Enoki, Y; Hasegawa, N; Iketani, O; Kizu, J; Komeya, A; Matsumoto, K; Taguchi, K; Uno, S; Uwamino, Y, 2022
)
" Although physiologically based pharmacokinetic (PBPK) modeling has become a widely accepted approach to assess DDIs and is able to reasonably predict DDIs caused by CYP3A4 induction and P-gp induction individually, the predictability of PBPK models for the effect of simultaneous P-gp and CYP3A4 induction on P-gp-CYP3A4 dual substrates remains to be systematically evaluated."( Unraveling pleiotropic effects of rifampicin by using physiologically based pharmacokinetic modeling: Assessing the induction magnitude of P-glycoprotein-cytochrome P450 3A4 dual substrates.
Neuhoff, S; Pan, X; Pilla Reddy, V; Yamazaki, S; Zhang, M, 2021
)
" The DTG pharmacokinetic profiles in different groups were assessed."( Pharmacokinetic features of dolutegravir with rifampicin and rifabutin among patients coinfected with human immunodeficiency virus and tuberculosis/mycobacterium avium complex.
Chen, J; Guo, X; Le, X; Liu, L; Qi, T; Shen, Y; Song, W; Sun, J; Tang, Y; Wang, J; Wang, Z; Yin, L; Zhang, L; Zhang, R, 2022
)
"We explored the Web of Science, Cochrane Library, PubMed, and Scopus databases for articles that reported the pharmacokinetic parameters of rifampicin in diabetic and nondiabetic patients with tuberculosis published until September 2020."( The impact of diabetes mellitus on the pharmacokinetics of rifampicin among tuberculosis patients: A systematic review and meta-analysis study.
El-Sheikh, SMA; Galal, AAA; Metwally, AS, 2022
)
"Diabetes mellitus increased the Tmax of rifampicin without further impact on other rifampicin pharmacokinetic parameters such as Cmax, AUC0-24, Vd, CL and MRT."( The impact of diabetes mellitus on the pharmacokinetics of rifampicin among tuberculosis patients: A systematic review and meta-analysis study.
El-Sheikh, SMA; Galal, AAA; Metwally, AS, 2022
)
" Several population pharmacokinetic (PK) studies on rifampicin in adult and child populations have been studied previously, therefore the aims of the systematic review were (i) to summarize the relevant published studies and significant covariates that influence the PK of rifampicin across different populations, and (ii) to identify any knowledge gap that requires additional research in the future."( Population pharmacokinetics analyses of rifampicin in adult and children populations: A systematic review.
Harun, SN; Muda, MR; Sheikh Ghadzi, SM; Syed Sulaiman, SA, 2022
)
" Population pharmacokinetic models used plasma and intrapulmonary drug levels at 8 and 16 weeks."( High Intrapulmonary Rifampicin and Isoniazid Concentrations Are Associated With Rapid Sputum Bacillary Clearance in Patients With Pulmonary Tuberculosis.
Chasweka, M; Chirambo, AP; Chitani, A; Corbett, EL; Davies, GR; Ghany, JF; Gordon, SB; Khoo, SH; Malamba, R; Mallewa, JE; McCallum, AD; Meghji, JZ; Mwandumba, HC; Pertinez, HE; Shani, D; Sheha, I; Sloan, DJ, 2022
)
"In this observational cohort study, children aged 6-17 years receiving bedaquiline at recommended doses as part of MDR/RR-TB treatment underwent semi-intensive pharmacokinetic sampling."( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022
)
" A bedaquiline pharmacokinetic model was adapted to be allometrically scaled in clearance and volume, centered in the median child population weight."( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022
)
" A population pharmacokinetic model was developed describing PAS pharmacokinetics in children receiving routine RR-TB treatment."( Pharmacokinetics and Dose Optimization Strategies of Para-Aminosalicylic Acid in Children with Rifampicin-Resistant Tuberculosis.
Chirehwa, M; Denti, P; Donald, PR; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Mao, J; McIlleron, H; Norman, J; Schaaf, HS; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
" This study aimed to establish a physiologically based pharmacokinetic (PBPK) model of rifampicin to predict the P-gp-mediated drug-drug interactions (DDIs) and assess the DDI impact in the intestine, liver, and kidney."( Robust physiologically based pharmacokinetic model of rifampicin for predicting drug-drug interactions via P-glycoprotein induction and inhibition in the intestine, liver, and kidney.
Asaumi, R; Nunoya, KI; Sugiyama, Y; Taskar, KS; Yamaura, Y, 2022
)
"58 children were assessed for eligibilty and enrolled between June 25, 2016, and Feb 6, 2018; 44 had complete stool testing and serum pharmacokinetic data, and they were included in the analyses."( Enteropathogen spectrum and effect on antimycobacterial pharmacokinetics among children with tuberculosis in rural Tanzania: a prospective cohort study.
Alshaer, MH; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kosek, M; Liu, J; Maro, A; Mduma, E; Mpagama, SG; Mujaga, B; Peloquin, CA; Rogawski McQuade, ET; Thomas, TA; Van Aartsen, D, 2022
)
"Tanzanian children undergoing tuberculosis treatment rarely attained pharmacokinetic targets; enteropathogen carriage was common and enteropathogen burden was associated with significant reductions in the concentrations of some antimycobacterial drugs."( Enteropathogen spectrum and effect on antimycobacterial pharmacokinetics among children with tuberculosis in rural Tanzania: a prospective cohort study.
Alshaer, MH; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kosek, M; Liu, J; Maro, A; Mduma, E; Mpagama, SG; Mujaga, B; Peloquin, CA; Rogawski McQuade, ET; Thomas, TA; Van Aartsen, D, 2022
)
" This study utilized physiologically based pharmacokinetic (PBPK) modeling to explore the pharmacokinetics of BRV and drug interactions between BRV and rifampin (RIF), a CYP2C19 inducer, based on CYP2C19 genetic polymorphisms."( Physiologically based pharmacokinetic modeling of brivaracetam and its interactions with rifampin based on CYP2C19 phenotypes.
Jiang, X; Wang, L; Yang, H; Yang, L; Zheng, L; Zhong, X, 2022
)
" Here, we investigate the pharmacokinetic drug-drug interaction potential of trilaciclib."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
" Population pharmacokinetic modeling showed no significant effect of trilaciclib on topotecan clearance."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
"Physiologically based pharmacokinetic (PBPK) models have gained in popularity in the last decade in both drug development and regulatory science."( A Comparative Analysis of Physiologically Based Pharmacokinetic Models for Human Immunodeficiency Virus and Tuberculosis Infections.
Jacobs, BA; Mtshali, S, 2022
)
"This study aimed to investigate the drug-drug interactions of ponatinib with strong, moderate, or weak CYP3A4 inhibitors/inducers by developing physiologically based pharmacokinetic (PBPK) models."( Physiologically based pharmacokinetic modeling of ponatinib to describe drug-drug interactions in patients with cancer.
Hanada, K; Morita, TO, 2022
)
" Nonlinear mixed-effects models were developed to describe the pharmacokinetic data."( Effects of Enzyme Induction and Polymorphism on the Pharmacokinetics of Isoniazid and Rifampin in Tuberculosis/HIV Patients.
Äbelö, A; Ashton, M; Bienvenu, E; Birgersson, S; Sundell, J, 2022
)
"Although rifampicin (RIF) is used as a synergistic agent for multidrug-resistant Acinetobacter baumannii (MDR-AB) infection, the optimal pharmacokinetic (PK) indices of this medication have not been studied in the intensive care unit (ICU) settings."( Pharmacokinetic study of high-dose oral rifampicin in critically Ill patients with multidrug-resistant Acinetobacter baumannii infection.
Ahmadi, A; Karballaei-Mirzahosseini, H; Kaveh-Ahangaran, R; Mojtahedzadeh, A; Mojtahedzadeh, M; Najafi, A; Najmeddin, F; Rouini, MR; Sadrai, S; Shahrami, B, 2022
)
" Pharmacokinetic parameters were calculated using noncompartmental analysis and safety was assessed."( The effect of rifampin on the pharmacokinetics of famitinib in healthy subjects.
Cao, Y; Fu, Y; Gao, X; Jiang, X; Li, T; Li, X; Lin, P; Liu, Y; Shi, P; Sun, F; Wang, C; Zhang, Y, 2022
)
"We systematically searched MEDLINE, Embase and Web of Science (1990-2021) for pharmacokinetic studies of first-line anti-TB drugs in children and adolescents."( Global estimates and determinants of antituberculosis drug pharmacokinetics in children and adolescents: a systematic review and individual patient data meta-analysis.
Aarnoutse, RE; Agarwal, D; Alffenaar, JC; Antwi, S; Bang, ND; Bekker, A; Bell, DJ; Chabala, C; Choo, L; Davies, GR; Day, JN; Dayal, R; Denti, P; Donald, PR; Engidawork, E; Gafar, F; Garcia-Prats, AJ; Gibb, D; Graham, SM; Hesseling, AC; Heysell, SK; Idris, MI; Kabra, SK; Kinikar, A; Kumar, AKH; Kwara, A; Lodha, R; Magis-Escurra, C; Marais, BJ; Martinez, N; Mathew, BS; Mave, V; McIlleron, HM; Mduma, E; Mlotha-Mitole, R; Mpagama, SG; Mukherjee, A; Nataprawira, HM; Peloquin, CA; Pouplin, T; Ramachandran, G; Ranjalkar, J; Roy, V; Ruslami, R; Schaaf, HS; Shah, I; Singh, Y; Stevens, J; Sturkenboom, MGG; Svensson, EM; Swaminathan, S; Taxis, K; Thatte, U; Thee, S; Thomas, TA; Tikiso, T; Touw, DJ; Turkova, A; Velpandian, T; Verhagen, LM; Wasmann, RE; Winckler, JL; Yang, H; Yunivita, V, 2023
)
" This study aimed to develop a population pharmacokinetic model of LPV/r and provide dosage optimization in Thai PLWH."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
"The population pharmacokinetic model was developed by integrating the interaction between LPV and RTV."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
"A phase I open-label study assessed the effect of multiple oral doses of a potent CYP3A4 inhibitor (itraconazole) and inducer (rifampicin) on the pharmacokinetic profile of a single oral dose of senaparib, a novel, highly potent poly-(ADP-ribose) polymerase 1/2 inhibitor and CYP3A4 substrate, in Chinese healthy male volunteers (HMV)."( Effect of a strong CYP3A4 inhibitor and inducer on the pharmacokinetics of senaparib (IMP4297) in healthy volunteers: A drug-drug interaction study.
Cai, SX; Hsieh, CY; Hu, X; Li, X; Liu, L; Liu, P; Liu, W; Shi, H; Xu, P; Xu, S; Zhang, H; Zhang, M; Zhang, Y, 2023
)
" Third, a physiologically-based pharmacokinetic model analysis was conducted with 10 substrate drugs following estimation of relative OATP1B functional activity in virtual disease population models using coproporphyrin-I data and verification of substrate models with rifampin drug-drug interaction data."( Effect of Hepatic Impairment on OATP1B Activity: Quantitative Pharmacokinetic Analysis of Endogenous Biomarker and Substrate Drugs.
Bergman, A; Costales, C; Kimoto, E; Li, R; Lin, J; Rodrigues, AD; Varma, MVS; Vourvahis, M; Yamazaki, S, 2023
)
" To consider an adult physiologically-based pharmacokinetic (PBPK) model for pediatric scaling, we assessed in vitro-derived cytochrome P450 (CYP) and uridine 5'-diphospho-glucuronosyltransferase (UGT) enzyme contributions to CBD clearance in human."( Verifying in vitro-determined enzyme contributions to cannabidiol clearance for exposure predictions in human through physiologically-based pharmacokinetic modeling.
Beers, JL; Edginton, AN; Jackson, KD; Yeung, CHT, 2023
)
" Reference baseline pharmacokinetic samples were collected on day 1 after the subjects were administered a single dose of 5 mg evogliptin."( Effect of Rifampicin on the Pharmacokinetics of Evogliptin in Healthy Volunteers.
Choi, C; Kim, CO; Oh, ES; Park, K; Park, MS; Shin, Y, 2022
)
" The findings showed that the CYP3A4 inhibitor itraconazole had no apparent pharmacokinetic drug interaction with chiglitazar, whereas rifampicin did."( Pharmacokinetic Interaction of Chiglitazar with CYP3A4 Inducer or Inhibitor: An Open-Label, Sequential Crossover, Self-Control, 3-Period Study in Healthy Chinese Volunteers.
Chen, H; Chen, W; Li, H; Li, J; Li, X; Liu, C; Sheng, L; Wu, Y; Xu, H; Yang, M; Yuan, F, 2023
)
" This review describes our work on (1) the establishment of a standard framework for determining physiologically based pharmacokinetic (PBPK) model structures and parameters useful for quantitatively analyzing DDIs via hepatic organic anion transporting polypeptides (OATPs)."( [Development of Prediction Methods for Drug-Drug Interactions Based on the Construction of Physiologically Based Pharmacokinetic Models for Hepatic OATP Substrate Drugs and Endogenous Substrates].
Yoshikado, T, 2023
)
" We aimed to determine whether children treated using World Health Organization-recommended or higher doses of first-line drugs achieve successful outcomes and sufficient pharmacokinetic (PK) exposures."( Effectiveness and Pharmacokinetic Exposures of First-Line Drugs Used to Treat Drug-Susceptible Tuberculosis in Children: A Systematic Review and Meta-Analysis.
Béranger, A; Gegia, M; Linh, NN; Mirzayev, F; Mohamed, A; Nahid, P; Radtke, K; Savic, RM; Schumacher, SG; Solans, BP, 2023
)
" Levonorgestrel pharmacokinetic parameters were compared between groups using geometric mean ratios (GMR) with 90% confidence intervals."( Pharmacokinetics of dose-adjusted levonorgestrel emergency contraception combined with efavirenz-based antiretroviral therapy or rifampicin-containing tuberculosis regimens.
Badal-Faesen, S; Barr, E; Belaunzaran-Zamudio, PF; Cohn, SE; Gadama, L; Gatechompol, S; Godfrey, C; Jalil, EM; Mawlana, S; Mngqibisa, R; Olefsky, M; Pham, M; Podany, AT; Scarsi, KK; Smeaton, LM; Supparatpinyo, K; Woolley, E, 2023
)
"5 mg to 3 mg improves levonorgestrel pharmacokinetic exposure in participants receiving either efavirenz-based antiretroviral regimens or rifampicin-containing tuberculosis therapy."( Pharmacokinetics of dose-adjusted levonorgestrel emergency contraception combined with efavirenz-based antiretroviral therapy or rifampicin-containing tuberculosis regimens.
Badal-Faesen, S; Barr, E; Belaunzaran-Zamudio, PF; Cohn, SE; Gadama, L; Gatechompol, S; Godfrey, C; Jalil, EM; Mawlana, S; Mngqibisa, R; Olefsky, M; Pham, M; Podany, AT; Scarsi, KK; Smeaton, LM; Supparatpinyo, K; Woolley, E, 2023
)
" Children with TBM were included in this pharmacokinetic analysis."( Population Pharmacokinetic Analysis of Rifampicin in Plasma, Cerebrospinal Fluid, and Brain Extracellular Fluid in South African Children with Tuberculous Meningitis.
Abdelgawad, N; Abdelwahab, MT; Castel, S; Denti, P; Enslin, JN; Figaji, A; McIlleron, H; Rohlwink, U; Steele, C; Thango, NS; Tshavhungwe, MP; Wiesner, L, 2023
)
"The aim of the present study is to develop physiologically based pharmacokinetic (PBPK) models for saxagliptin and its active metabolite, 5-hydroxy saxagliptin, and to predict the effect of coadministration of rifampicin, a strong inducer of cytochrome P450 3A4 enzymes, on the pharmacokinetics of saxagliptin and 5-hydroxy saxagliptin in patients with renal impairment."( Physiologically Based Pharmacokinetic Modeling Characterizes the Drug-Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment.
Ke, M; Lin, C; Lin, R; Wu, W; Ye, L, 2023
)
" We aimed to evaluate the pharmacokinetic and pharmacodynamic effects of a short course (2 weeks) of rifampin on serum etonogestrel (ENG) concentrations and serologic measures of ovarian activity (endogenous estradiol [E2] and progesterone [P4]) among ENG implant users."( The effect of rifampin on serum etonogestrel concentrations and biomarkers of ovulation among contraceptive implant users: A pharmacokinetic and pharmacodynamic study.
Lazorwitz, A; Sheeder, J; Teal, S, 2023
)
" Pharmacokinetic parameters were calculated using non-compartmental analysis."( Effect of CYP3A4 induction and inhibition on the pharmacokinetics of SHR0302 in healthy subjects.
Feng, S; Fu, M; Gao, X; Li, X; Li, Y; Lin, H; Shen, K; Yu, G; Zhang, P; Zhang, Z, 2023
)
" Treatment efficacy is extrapolated by assessing respective pharmacodynamic (PD) indices, as well as parameters associated with the emergence of resistance."( Physiologically-based pharmacokinetic modeling to inform dosing regimens and routes of administration of rifampicin and colistin combination against Acinetobacter baumannii.
Lv, Z; Oo, C; Schlender, JF; Song, C; Sy, SKB; Wu, M; Yu, M; Yue, J; Zhang, J; Zhu, P; Zhu, S; Zhu, Y, 2023
)
"Physiologically-based pharmacokinetic models of rifampicin and colistin were utilized to predict tissue exposures."( Physiologically-based pharmacokinetic modeling to inform dosing regimens and routes of administration of rifampicin and colistin combination against Acinetobacter baumannii.
Lv, Z; Oo, C; Schlender, JF; Song, C; Sy, SKB; Wu, M; Yu, M; Yue, J; Zhang, J; Zhu, P; Zhu, S; Zhu, Y, 2023
)
" We find that the observation on the slow phase's dependence on pharmacokinetic measures, specifically peak concentrations are only compatible with models of heteroresistance and incompatible with models of persistence."( High rifampicin peak plasma concentrations accelerate the slow phase of bacterial decline in tuberculosis patients: Evidence for heteroresistance.
Aarnoutse, RE; Abel Zur Wiesch, P; Boeree, MJ; Dawson, R; Diacon, AH; Hemez, C; Martinecz, A, 2023
)
" Clinical pharmacokinetic drug-drug interaction (DDI) of ocedurenone with CYP3A inhibitor and inducer were investigated in healthy volunteers."( Pharmacokinetics and Drug-Drug Interaction of Ocedurenone (KBP-5074) in vitro and in vivo.
Liu, J; McCabe, J; Tan, X; Wang, P; Yang, F; Zhang, J, 2023
)
" To address this gap, we formulate a whole-body physiologically-based pharmacokinetic (PBPK) model for EPTB that for the first time includes the ability to simulate drug concentrations in the pleura and lymph node, the most commonly affected sites of EPTB."( A physiologically-based pharmacokinetic model for tuberculosis drug disposition at extrapulmonary sites.
Gadgil, CJ; Ramachandran, A, 2023
)
" The present study aims to utilize physiologically based pharmacokinetic (PBPK) modeling to predict CYP3A4-based drug interactions of pyrotinib."( Physiologically Based Pharmacokinetic Modeling to Simulate CYP3A4-Mediated Drug-Drug Interactions for Pyrotinib.
Chen, X; Hu, W; Liu, Y; Ni, L; Wang, L; Xu, W; Zhang, Q; Zhao, Y; Zheng, L, 2023
)
"We conducted a crossover pharmacokinetic trial in children aged ≤5 years receiving levofloxacin RR-TB preventive therapy."( Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children.
Denti, P; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Palmer, M; Schaaf, HS; van der Laan, LE; Wiesner, L, 2023
)
" Based on the detailed stability study of the analyzed compounds at various storage conditions, we proposed recommendations for handling the plasma and serum samples in TDM and other pharmacokinetic studies."( New approach to rifampicin stability and first-line anti-tubercular drug pharmacokinetics by UPLC-MS/MS.
Heysell, SK; Kagan, L; Karaźniewicz-Łada, M; Kosicka-Noworzyń, K; Modi, N; Rao, P; Xie, YL, 2023
)

Compound-Compound Interactions

The study demonstrated for the first time that fosfomycin (FOS) combined with rifampin (RIF) showed strong synergistic effects against CRPA and carbapenem-susceptible PA. The knowledge about efficacy of linezolid alone or in combination with r ifampin in device infections is limited.

ExcerptReference
"Suboptimal doses of amphotericin B in combination with either rifampin or 5-fluorocytosine were better than single-drug therapy in the treatment of disseminated Aspergillus fumigatus infection in mice."( Therapy of murine aspergillosis with amphotericin B in combination with rifampin of 5-fluorocytosine.
Arroyo, J; Kobayashi, GS; Medoff, G, 1977
)
" The binding of digitoxin and cardioactive metabolites to serum proteins was studied using equilibrium dialysis (an in vitro chemical assay) alone and in combination with a modified 86Rb method."( Studies on digitalis. V. The influence of impaired renal function, hemodialysis, and drug interaction on serum protein binding of digitoxin and digoxin.
Storstein, L, 1976
)
"The effect of amphotericin B combined with rifampicin or doxycycline on growth, oxygen consumption and ATP levels in cultures of Candida albicans, was studied."( In-vitro effects of Candida albicans of amphotericin B combined with other antibiotics. Preliminary observations.
Akesson, E; Anséhn, S; Granström, S; Höjer, H; Lundin, A; Nilsson, L; Thore, A, 1976
)
"14C-Isoniazid (20 mg/kg po or iv) was administered alone or in combination with aspirin (100 mg/kg po), rifampin (30 mg/kg po), ethambutol (100 mg/kg po), or ethanol (3 g/kg po) to rats."( Drug interactions with isoniazid metabolism in rats.
Solomonraj, G; Thomas, BH, 1977
)
" Staphylococci isolated from the bones of therapeutic failures that had received rifampin alone or in combination with other antibiotics were highly resistant to rifampin (minimal inhibitory concentration, greater than 250 mug/ml), whereas the organisms recovered from animals not receiving rifampin remained sensitive."( Experimental osteomyelitis. IV. Therapeutic trials with rifampin alone and in combination with gentamicin, sisomicin, and cephalothin.
Norden, CW, 1975
)
"The activity of TLC G-65 (a liposomal gentamicin preparation), alone and in combination with rifapentine, clarithromycin, clofazimine and ethambutol, was evaluated in the beige mouse (C57BL/6J--bgj/bgj) model of disseminated Mycobacterium avium infection."( TLC G-65 in combination with other agents in the therapy of Mycobacterium avium infection in beige mice.
Cynamon, MH; Klemens, SP; Swenson, CE, 1992
)
" It is concluded that rifampicin treatment of protein-sealed Dacron grafts combined with intravenous cefoxitin provides more protection from contaminating Staphylococcus aureus than intravenous cefoxitin alone in this animal model."( Prevention of prosthetic vascular graft infection by rifampicin impregnation of a protein-sealed Dacron graft in combination with parenteral cephalosporin.
Avramovic, J; Fletcher, JP,
)
"The activity of clarithromycin in combination with ethambutol and rifampicin was tested at concentrations achievable in serum against 20 strains of Mycobacterium avium complex."( In vitro testing of clarithromycin in combination with ethambutol and rifampicin against Mycobacterium avium complex.
Dörtbudak, O; Lahonik, E; Stauffer, F,
)
" Most women are more likely to use antibiotics, analgesics, and antihistamines, which have also been shown to interact with OCs."( Oral contraceptive drug interactions: important considerations.
Fazio, A, 1991
)
"The in-vitro activity of cefpirome and ceftazidime when combined with aminoglycosides (gentamicin, amikacin, and tobramycin) in the presence and in the absence of rifampicin was evaluated against 32 isolates of Pseudomonas aeruginosa by two methods."( The effect of rifampicin on the in-vitro activity of cefpirome or ceftazidime in combination with aminoglycosides against Pseudomonas aeruginosa.
Baltch, AL; Hammer, MC; Ritz, WJ; Smith, RP; Valdes, JM, 1990
)
"Treatment of disseminated Pseudomonas aeruginosa infection in leukopenic mice was evaluated using cefpirome alone and in combination with gentamicin and/or rifampin."( Comparative therapy with cefpirome alone and in combination with rifampin and/or gentamicin against a disseminated Pseudomonas aeruginosa infection in leukopenic mice.
Baltch, AL; Franke, M; Michelsen, P; Ritz, WJ; Singh, J; Smith, RP; Valdes, JM; Williams, S, 1990
)
"The bactericidal activities of teicoplanin and vancomycin, as single agents or combined with fosfomycin, fusidic acid or rifampicin, were investigated in an in vitro study involving 20 strains of Staphylococcus epidermidis isolated from infected vein catheters."( Antibacterial activity of teicoplanin and vancomycin in combination with rifampicin, fusidic acid or fosfomycin against staphylococci on vein catheters.
Simon, M; Simon, VC, 1990
)
"The efficacies of the quinolones ciprofloxacin and pefloxacin alone and in combination with rifampin were compared with those of vancomycin alone and in combination with rifampin in a rat model of chronic osteomyelitis caused by methicillin-resistant Staphylococcus aureus."( Comparative efficacies of ciprofloxacin, pefloxacin, and vancomycin in combination with rifampin in a rat model of methicillin-resistant Staphylococcus aureus chronic osteomyelitis.
Dworkin, R; Kunz, S; Modin, G; Rich, R; Sande, M; Zak, O, 1990
)
"Early investigational trials with new quinolone antibiotics revealed two important drug-drug interactions: decreased fluoroquinolone absorption when co-administered with magnesium-aluminum antacids and inhibition of theophylline metabolism."( Drug-drug interactions with ciprofloxacin and other fluoroquinolones.
Polk, RE, 1989
)
"Killing kinetic experiments were performed with ciprofloxacin, fusidic acid and rifampicin alone and with ciprofloxacin combined with either fusidic acid or rifampicin against ten strains of Staphylococcus aureus."( In-vitro activity of ciprofloxacin combined with either fusidic acid or rifampicin against Staphylococcus aureus.
Gutschik, E; Røder, BL, 1989
)
"Oral contraceptives (OCs) should be used with additional caution in combination with other drugs in certain disease states."( Drug interactions with oral contraceptive preparations.
Shenfield, GM, 1986
)
"Rifampin, a potent inducer of the hepatic microsomal system, has been shown to cause clinically important interactions when combined with other drugs, including oral anticoagulants, oral contraceptives, digitoxin, methadone hydrochloride, sulfonylureas, and barbiturates."( Update on rifampin drug interactions.
Baciewicz, AM; Bekemeyer, WB; Self, TH, 1987
)
"The bactericidal interactions in vitro of two antibiotics active at the cell wall (teicoplanin and vancomycin) or two inhibitors of DNA gyrase (coumermycin and ciprofloxacin) combined with two inhibitors of protein synthesis (rifampicin and LM 427) were assessed against five Staphylococcus aureus strains."( Comparative in-vitro activities of teicoplanin, vancomycin, coumermycin and ciprofloxacin, alone and in combination with rifampicin or LM 427, against Staphylococcus aureus.
Joly, P; Van der Auwera, P, 1987
)
"The in vitro susceptibility of Mycobacterium tuberculosis to new quinolones, ofloxacin and ciprofloxacin, alone and in combination with rifampin or isoniazid, was studied by the agar dilution method."( In vitro susceptibility of Mycobacterium tuberculosis to ofloxacin and ciprofloxacin in combination with rifampin and isoniazid.
Casal, M; González, J; Gutierrez, J; Ruiz, P, 1987
)
" Intracavernous instillation and rapid intravenous administration (RIA) of the drug in combination with 10 per cent solution of isoniazid and intramuscular administration of streptomycin were used."( [Effectiveness of soluble rifampicin in combination with other antibacterial preparations in treating disseminated destructive pulmonary tuberculosis in an experiment].
Bondarev, IM; Ivanov, VL; Kovaleva, LA; Mozhokina, GN; Novoselova, VP, 1987
)
"The in vitro activity of fosfomycin alone and in combination with rifampin, pefloxacin and imipenem was studied by the time-kill method against staphylococci."( In vitro activity of fosfomycin combined with rifampin, pefloxacin and imipenem against staphylococci: a study by the time-kill curve method.
Bebear, C; Lafferriere, C; Noury, P; Quentin, C; Saivin, S, 1987
)
" Fosfomycin combined with pefloxacin was found to be additive or moderately synergistic."( [In vitro action of fosfomycin combined with rifampicin, pefloxacin and imipenem on staphylococci (checkerboard method in a liquid medium)].
Bebear, C; Laurent, C; Noury, P; Quentin, C; Saivin, S, 1987
)
" We tested rifampin in combination with nafcillin, vancomycin, clindamycin, pefloxacin, ciprofloxacin, trimethoprim, teicoplanin, or erythromycin."( Serum bactericidal activity of rifampin in combination with other antimicrobial agents against Staphylococcus aureus.
Chambers, HF; Hackbarth, CJ; Sande, MA, 1986
)
" tuberculosis were treated in the initial phase as inpatients for 2-3 months at random with either pyrazinamide (Z) or ethambutol (E) in combination with isoniazid (H) and rifampicin (R)."( [Which is the best drug combination for the short-term therapy of tuberculosis? A prospective randomized study with 190 patients].
Bezel, R; Brändli, O; Häcki, M; Karrer, W; Röthlisberger, K; Rubin, S, 1985
)
"189 bacterial strains were investigated for their in vitro sensitivity against ceftazidime (alone and in combination with another antibiotic)."( In vitro activity of ceftazidime in combination with other antibiotics.
Littschwager, G; Simon, C,
)
" Diphenyl hydantoin is often combined with barbiturates to treat epilepsy."( [Drug interactions in the use of steroid hormones, especially oral contraceptives].
Bolt, HM, 1985
)
" Synergistic studies also demonstrated that teichomycin A2 combined with rifampin is more active than vancomycin combined with rifampin against Staphylococcus aureus and Staphylococcus epidermidis isolates."( Comparative in vitro activities of teichomycin and vancomycin alone and in combination with rifampin and aminoglycosides against staphylococci and enterococci.
Miller, H; Tuazon, CU, 1984
)
"A total of 440 fresh clinical isolates of yeasts from cancer patients were tested by an agar dilution technique against miconazole, miconazole nitrate, and ketoconazole individually and combined with 5 micrograms of rifampin per ml."( In vitro activities of miconazole, miconazole nitrate, and ketoconazole alone and combined with rifampin against Candida spp. and Torulopsis glabrata recovered from cancer patients.
Moody, MR; Morris, MJ; Schimpff, SC; Young, VM, 1980
)
" Flucytosine combined with amphotericin B produced little or no reduction of the MICs at which 90% of the strains were inhibited compared with amphotericin B alone."( In vitro activities of amphotericin B in combination with four antifungal agents and rifampin against Aspergillus spp.
Gerding, DN; Harris, C; Hughes, CE; Moody, JA; Peterson, LR, 1984
)
"The efficacy of rifampin alone and in combination with sisomicin, cephalothin, sisomicin and cephalothin, or trimethoprim was measured in an experimental model of chronic osteomyelitis due to Staphylococcus aureus in rabbits."( Experimental chronic staphylococcal osteomyelitis in rabbits: treatment with rifampin alone and in combination with other antimicrobial agents.
Norden, CW,
)
" Based on previous studies, antipyrine given with phenobarbitone produced slightly more induction than phenobarbitone given alone."( Enzyme-inducing drug combinations and their effects on liver microsomal enzyme activity in man.
Gerber-Taras, E; Ohnhaus, EE; Park, BK, 1983
)
" The therapeutic advantage of using these two drugs in combination should be more readily appreciated."( A comparative evaluation of drug combinations used in the treatment of pulmonary tuberculosis.
Miller, SD, 1983
)
"The in vitro activity of rifampin alone and in combination with oxacillin was determined for 75 Staphylococcus aureus strains (64 susceptible and 11 resistant to oxacillin)."( In vitro activity of rifampin in combination with oxacillin against Staphylococcus aureus.
Goldmann, DA; Maduri Traczewski, M; Murphy, P, 1983
)
"A review of the published literature has allowed the identification of a number of non-tubercular indications where rifampicin (trade mark Ciba-Geigy: Rimactane) has been successfully used in combination with other chemotherapeutic agents."( Rifampicin in free combination with other antimicrobial drugs in non-Tb infections. Clinical data on 650 patients (a review).
Bergamini, N; Kissling, M, 1981
)
"The pharmacodynamic properties of levofloxacin (an optically active isomer of ofloxacin), ofloxacin, and ciprofloxacin, alone and in combination with rifampin, were evaluated over 24 to 48 h against clinical isolates of methicillin-susceptible and -resistant Staphylococcus aureus (MSSA 1199 and MRSA 494, respectively) in an in vitro infection model."( Pharmacodynamics of levofloxacin, ofloxacin, and ciprofloxacin, alone and in combination with rifampin, against methicillin-susceptible and -resistant Staphylococcus aureus in an in vitro infection model.
Kaatz, GW; Kang, SL; McGrath, BJ; Rybak, MJ; Seo, SM, 1994
)
"The activity of fusidic acid alone and in combination with gentamicin, oxacillin, rifampicin, fosfomycin and ciprofloxacin was investigated against 36 strains of Staphylococcus aureus."( In-vitro antibacterial activity of fusidic acid alone and in combination with other antibiotics against methicillin-sensitive and -resistant Staphylococcus aureus.
Caillon, J; Drugeon, HB; Juvin, ME, 1994
)
" Unfortunately, the emergence of multiple drug-resistant tuberculosis in many parts of the world is leading to a diversification of drug regimens and to the use of drugs that are more toxic per se and more likely to interact with others."( Clinically significant drug interactions with antituberculosis agents.
Davies, PD; Grange, JM; Winstanley, PA, 1994
)
"The in vitro activity of vancomycin and teicoplanin (fourfold the MBC), alone and in combination with amikacin (16 mg/l) or rifampin (1 mg/l), against Staphylococcus epidermidis (slime-producing and non slime-producing strains) biofilms on different plastic catheters was evaluated."( Activity of glycopeptides in combination with amikacin or rifampin against Staphylococcus epidermidis biofilms on plastic catheters.
Pascual, A; Perea, EJ; Ramirez de Arellano, E, 1994
)
"The antimicrobial effects of ofloxacin against Mycobacterium leprae, either alone or in combination with rifampicin and rifabutin, were studied using mouse foot pad assay technique."( In vivo susceptibility of Mycobacterium leprae to ofloxacin either singly or in combination with rifampicin and rifabutin. Anti-leprosy activity of ofloxacin and ansamycins in mice.
Dhople, AM; Ibanez, MA, 1994
)
" melitensis intraperitoneally on day 0 and were randomized to receive, starting on day 7, STR alone at 75, 150, or 300 mg/kg of body weight per day intraperitoneally or DOX at 6 mg/kg/day orally, RIF at 3 mg/kg/day orally, or CIP at 200 mg/kg/day orally, each of the last three drugs alone or in combination with STR at 75, 150, or 300 mg/kg/day, for 14 days."( Therapy of experimental murine brucellosis with streptomycin alone and in combination with ciprofloxacin, doxycycline, and rifampin.
Lang, R; Rubinstein, E; Shasha, B, 1993
)
" malmoense isolates to a number of antibacterial drugs as well as their possible synergistic interactions when each of them was combined with ethambutol."( Susceptibility of Mycobacterium malmoense to antibacterial drugs and drug combinations.
Hjelm, U; Hoffner, SE; Källenius, G, 1993
)
" The pharmacokinetic literature on racemic drugs contains a vast amount of information on drug-drug interactions derived from the measurement of total drug concentrations in plasma and urine."( Stereoselective and isozyme-selective drug interactions.
Gibaldi, M, 1993
)
"The activity of KRM-1648, alone and in combination with isoniazid, was compared with those of isoniazid, rifampin, and the combination of rifampin plus isoniazid in a murine model of tuberculosis."( Activity of KRM-1648 in combination with isoniazid against Mycobacterium tuberculosis in a murine model.
Cynamon, MH; Klemens, SP, 1996
)
"The in vivo activities of KRM-1648 alone or in combination with both ethambutol (EB) and kanamycin (KM) or clarithromycin (CAM) were tested against Mycobacterium intracellulare infections in beige mice."( Activity of KRM-1648 alone or in combination with both ethambutol and kanamycin or clarithromycin against Mycobacterium intracellulare infections in beige mice.
Amitani, R; Kuze, F; Murayama, T; Suzuki, K; Tanaka, E; Yamamoto, T, 1996
)
"The in vitro activity of DU-6859a (DU) alone and in combination with various antimicrobials was evaluated against multiresistant enterococci including some isolates with defined gyrA mutations."( Bactericidal activity of the fluoroquinolone DU-6859a alone and in combination with other antimicrobial agents against multiresistant enterococci.
Erdem, I; Korten, V; Murray, BE, 1996
)
" Usually, indifference was seen when RPR 106972 was tested in combination with rifampicin or ciprofloxacin."( In-vitro activity of a new oral streptogramin, RPR 106972, alone and in combination with rifampicin or ciprofloxacin against Legionella spp.
Killian, AD; Pendland, SL; Rodvold, KA; Woodward, JG, 1997
)
"The utility of primary human hepatocytes in the evaluation of drug-drug interactions is being investigated in our laboratories."( Applications of primary human hepatocytes in the evaluation of pharmacokinetic drug-drug interactions: evaluation of model drugs terfenadine and rifampin.
Jurima-Romet, M; Li, AP, 1997
)
" These findings suggest that metronidazole, given with bactericidal drugs such as rifampicin and isoniazid may be of value in eliminating persisting tubercle bacilli, but further studies are warranted."( Action of metronidazole in combination with isoniazid & rifampicin on persisting organisms in experimental murine tuberculosis.
Herbert, D; Kubendiran, G; Paramasivan, CN, 1998
)
" The combination beta-lactam-ciprofloxacin-tobramycin was the combination with the most consistently synergistic effect."( Comparative in vitro activities of meropenem, imipenem, temocillin, piperacillin, and ceftazidime in combination with tobramycin, rifampin, or ciprofloxacin against Burkholderia cepacia isolates from patients with cystic fibrosis.
Bingen, E; Bonacorsi, S; Fitoussi, F; Lhopital, S, 1999
)
"This in vitro study evaluated the activities of vancomycin, LY333328, and teicoplanin alone and in combination with gentamicin, rifampin, and RP59500 against Staphylococcus aureus isolates with intermediate susceptibilities to vancomycin."( Evaluation of bactericidal activities of LY333328, vancomycin, teicoplanin, ampicillin-sulbactam, trovafloxacin, and RP59500 alone or in combination with rifampin or gentamicin against different strains of vancomycin-intermediate Staphylococcus aureus by
Aeschlimann, JR; Hershberger, E; Moldovan, T; Rybak, MJ, 1999
)
"The effect of rifampicin in combination with dicloxacillin or fusidic acid on the extracellular and intracellular killing of Staphylococcus aureus in human neutrophil granulocytes in the presence of serum was studied."( Extracellular and intracellular killing in neutrophil granulocytes of Staphylococcus aureus with rifampicin in combination with dicloxacillin or fusidic acid.
Black, FT; Nielsen, SL, 1999
)
"The killing activities of trovafloxacin alone and in combination with beta-lactam agents (extended-spectrum cephalosporins, meropenem), rifampin, or vancomycin were evaluated against 20 genotypically characterized Streptococcus pneumoniae isolates for which amoxicillin MICs were >/=4 microg/ml (cefotaxime MICs, >/=4 microg/ml for six strains) at concentrations clinically achievable in cerebrospinal fluid."( Killing activities of trovafloxacin alone and in combination with beta-lactam agents, rifampin, or vancomycin against Streptococcus pneumoniae isolates with various susceptibilities to extended-spectrum cephalosporins at concentrations clinically achievab
Bingen, E; Doit, C; Fitoussi, F; Geslin, P, 1999
)
"There was a significant difference in the Cmax between free and RIF combined with INH (6."( Bioavailability of rifampicin in a separate formulation and fixed dose combination with isoniazid NIH: a case for a fixed dose combination (FDC) for the treatment of tuberculosis.
Chitemerere, C; Gumbo, J; Ndudzo, P; Nyazema, NZ; Rabvukwa, P, 1999
)
"To evaluate the activity of vancomycin and levofloxacin alone and combined with rifampin against planktonic and sessile cells."( Comparative in vitro activity of vancomycin and levofloxacin in combination with rifampin against planktonic versus sessile cells of Staphylococcus epidermidis.
Kang-Birken, SL, 2000
)
"Killing kinetic experiments were performed with moxifloxacin, a novel fluoroquinolone, vancomycin, clarithromycin, cotrimoxazole, gentamicin, rifampicin and with moxifloxacin in combination with each of the above drugs against six methicillin-resistant Staphylococcus aureus clinical isolates."( In-vitro activity of moxifloxacin combined with other antibacterials against methicillin-resistant Staphylococcus aureus.
Bottura, P; Capra, R; Maggiolo, F; Migliorino, M; Pravettoni, G; Suter, F, 2000
)
"The activities of clarithromycin or roxithromicin used in combination with other antimicrobial drugs were tested in human macrophages experimentally infected with 23 strains of Mycobacterium avium."( Efficacy of macrolides used in combination with ethambutol, with or without other drugs, against Mycobacterium avium within human macrophages.
Brandi, G; Celeste, AG; Salvaggio, L; Schiavano, GF; Sisti, M, 2001
)
"The antimicrobial effect of sitafloxacin (DU-6859a), used either singly or in combination with rifampicin, was evaluated in vitro against Mycobacterium ulcerans."( In vitro activity of sitafloxacin (DU-6859a) alone, or in combination with rifampicin, against Mycobacterium ulcerans.
Dhople, AM; Namba, K, 2002
)
"The antimicrobial effects of sitafloxacin (DU-6859a) against Mycobacterium leprae, either singly or in combination with either rifampicin, rifabutin or KRM-1648, were studied using a mouse footpad assay technique and the results were compared with those obtained with ofloxacin."( In vivo susceptibility of Mycobacterium leprae to sitafloxacin (DU-6859a), either singly or in combination with rifampicin analogues.
Dhople, AM; Namba, K, 2003
)
"The in vitro activity of the oxazolidinone linezolid was studied alone and in combination with three antibiotics acting on different cellular targets."( In vitro activity of linezolid alone and in combination with gentamicin, vancomycin or rifampicin against methicillin-resistant Staphylococcus aureus by time-kill curve methods.
Bugnon, D; Caillon, J; Donnio, PY; Jacqueline, C; Le Mabecque, V; Miegeville, AF; Potel, G, 2003
)
" Similar to ofloxacin and levofloxacin, sitafloxacin also exhibited synergistic activity when combined with either rifabutin or KRM-1648, but not with rifampin."( In-vitro activity of sitafloxacin (DU-6859a), either singly or in combination with rifampin analogs, against Mycobacterium leprae.
Dhople, AM; Namba, K, 2003
)
" Either used singly or in combination with rifampin, the effects of sitafloxacin were bactericidal."( Activities of sitafloxacin (DU-6859a), either singly or in combination with rifampin, against Mycobacterium ulcerans infection in mice.
Dhople, AM; Namba, K, 2003
)
"The efficacy of levofloxacin and dirithromycin, alone and in combination with rifampicin in the treatment of experimental brucellosis was investigated."( Efficacy of oral levofloxacin and dirithromycin alone and in combination with rifampicin in the treatment of experimental murine Brucella abortus infection.
Arda, B; Gökengin, D; Gürel, O; Tunçel, M; Yaimazhan, T, 2004
)
" In the present study, two adjusted-dose regimens of lopinavir-ritonavir were tested in combination with rifampin."( Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers.
Bertz, R; Boeree, MJ; Burger, DM; Colbers, EP; Hekster, YA; Koopmans, PP; la Porte, CJ; Voncken, DS; Wikstrom, K, 2004
)
"Disposition of uric acid upon administration of ofloxacin (O) alone and in combination with other anti-tuberculosis drugs, rifampicin (R), isoniazid (H) and pyrazinamide (Z) was studied."( Disposition of uric acid upon administration of ofloxacin alone and in combination with other anti-tuberculosis drugs.
Gurumurthy, P; Kumar, AK, 2004
)
"To estimate the rate of potential drug-drug interactions in outpatients of a typical Thai university hospital, and to identify risk factors for such interactions in Thai patients."( Pharmacoepidemiologic study of potential drug interactions in outpatients of a university hospital in Thailand.
Chongsuvivatwong, V; Janchawee, B; Owatranporn, T; Wongpoowarak, W, 2005
)
"Tenofovir disoproxil fumarate (tenofovir DF) was studied in combination with rifampin in 24 healthy subjects in a multiple-dose, open-label, single-group, two-period study."( Pharmacokinetic study of tenofovir disoproxil fumarate combined with rifampin in healthy volunteers.
Buffels, R; Burger, DM; Droste, JA; Hekster, YA; Kearney, BP; Vanhorssen, PJ; Verweij-van Wissen, CP, 2005
)
"The purpose of this study was to carry out drug-drug compatibility studies on pure first line anti-tuberculosis drugs, viz."( Drug-drug interaction studies on first-line anti-tuberculosis drugs.
Bhutani, H; Jindal, KC; Singh, S, 2005
)
"Rifampicin, an important drug in the treatment of tuberculosis, is used extensively despite its broad effects on drug-drug interactions, creating serious problems."( Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor.
Chen, J; Raymond, K, 2006
)
" In-vitro studies have reported that polymyxins combined with carbapenems, rifampicin or azithromycin are synergistic against these strains despite in-vitro resistance to these agents alone."( In-vitro activity of polymyxin B in combination with imipenem, rifampicin and azithromycin versus multidrug resistant strains of Acinetobacter baumannii producing OXA-23 carbapenemases.
Bean, DC; Wareham, DW, 2006
)
" Marked synergy was not seen with polymyxin in combination with imipenem, rifampicin or azithromycin against any of the strains."( In-vitro activity of polymyxin B in combination with imipenem, rifampicin and azithromycin versus multidrug resistant strains of Acinetobacter baumannii producing OXA-23 carbapenemases.
Bean, DC; Wareham, DW, 2006
)
"In-vitro synergy with polymxyin in combination with imipenem, rifampicin or azithromycin is highly strain and method dependent."( In-vitro activity of polymyxin B in combination with imipenem, rifampicin and azithromycin versus multidrug resistant strains of Acinetobacter baumannii producing OXA-23 carbapenemases.
Bean, DC; Wareham, DW, 2006
)
" Drug-drug interactions (DDIs) caused by induction of CYP3A4 can result in decreased exposure to coadministered drugs, with potential loss of efficacy."( Use of immortalized human hepatocytes to predict the magnitude of clinical drug-drug interactions caused by CYP3A4 induction.
de Morais, SM; Fahmi, OA; Liras, JL; Maurer, TS; Mills, JB; Ripp, SL; Trevena, KA, 2006
)
" These data suggest that colistin, in combination with rifampin and imipenem, is safe and effective, in promoting healing in DFI due to MDR P aeruginosa and suggest the need for controlled clinical studies."( Clinical and microbiological efficacy of colistin therapy in combination with rifampin and imipenem in multidrug-resistant Pseudomonas aeruginosa diabetic foot infection with osteomyelitis.
Gemignani, G; Leonildi, A; Menichetti, F; Palumbo, F; Piaggesi, A; Tascini, C; Tedeschi, A, 2006
)
"The objective of this paper was to investigate the in vitro effects of linezolid combined with five antistaphylococcal antibiotics--doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin--upon methicillin-susceptible Staphylococcus aureus (MSSA)."( In vitro activity of linezolid in combination with doxycycline, fosfomycin, levofloxacin, rifampicin and vancomycin against methicillin-susceptible Staphylococcus aureus.
Cantón, E; Colombo Gainza, E; Gil Brusola, A; Gobernado, M; Ortiz Estévez, R; Sahuquillo Arce, JM, 2006
)
" This review focuses on the influence of transporters on the pharmacokinetics of beta-lactam antibiotics, new quinolones, and other antimicrobial agents, as well as focusing on the drug-drug interactions associated with transporter-mediated uptake from the small intestine and transporter-mediated elimination from the kidney and liver."( Impact of transporter-mediated drug absorption, distribution, elimination and drug interactions in antimicrobial chemotherapy.
Tsuji, A, 2006
)
"In previous studies, the diarylquinoline R207910 (also known as TMC207) was demonstrated to have high bactericidal activity when combined with first- or second-line antituberculous drugs."( Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
Andries, K; Chauffour, A; Ibrahim, M; Jarlier, V; Lounis, N; Truffot-Pernot, C; Veziris, N, 2007
)
" Daptomycin sub-MICs combined with gentamicin concentrations lower than the MIC yielded synergy in 34 (68%) of the 50 strains."( Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
Appelbaum, PC; Credito, K; Lin, G, 2007
)
"Pharmacokinetic drug-drug interactions (DDIs) are a major concern in drug development."( New strategies to address drug-drug interactions involving OATPs.
Funk, C; Lavé, T; Noé, J; Poirier, A, 2007
)
" The objective of this study was also to determine the effects of the interaction of linezolid when it was combined with rifampicin and test this effect against strains of methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis."( Linezolid alone and in combination with rifampicin prevents experimental vascular graft infection due to methicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis.
Baltalarli, A; Duver, H; Goksin, I; Kaan Inan, B; Kaleli, I; Onem, G; Ozcan, V; Sacar, M; Sacar, S; Turgut, H, 2007
)
"The activities of tigecycline alone and in combination with other antimicrobials are not well defined for carbapenem-intermediate or -resistant Acinetobacter baumannii (CIRA)."( In vitro activities of various antimicrobials alone and in combination with tigecycline against carbapenem-intermediate or -resistant Acinetobacter baumannii.
Noskin, GA; Obias, A; Postelnick, MJ; Qi, C; Scheetz, MH; Warren, JR; Zembower, T, 2007
)
" Several regimens of gatifloxacin in combination with rifampicin were compared with isoniazid plus rifampicin in a mouse tuberculosis model."( Gatifloxacin in combination with rifampicin in a murine tuberculosis model.
Cynamon, M; Shoen, C; Sklaney, MR, 2007
)
"Gatifloxacin in combination with rifampicin is a promising combination for potential evaluation in human clinical trials."( Gatifloxacin in combination with rifampicin in a murine tuberculosis model.
Cynamon, M; Shoen, C; Sklaney, MR, 2007
)
"We compared the efficacy of quinupristin/dalfopristin versus vancomycin, alone or in combination with rifampicin, in a rabbit model of methicillin-resistant Staphylococcus aureus-induced arthritis."( Efficacy of quinupristin/dalfopristin versus vancomycin, alone or in combination with rifampicin, against methicillin-resistant Staphylococcus aureus in a rabbit arthritis model.
Batard, E; Caillon, J; Hamel, A; Jacqueline, C; Potel, G, 2008
)
" In this study, the effects of Ag85A DNA or ESAT6/Ag85A chimeric DNA vaccines alone or in combination with rifampin (RFP) were studied for the treatment of mice with MDR-TB."( The treatment of mice infected with multi-drug-resistant Mycobacterium tuberculosis using DNA vaccines or in combination with rifampin.
Bai, X; Li, N; Li, Z; Liang, Y; Liu, C; Liu, Q; Shi, Y; Wu, X; Yang, Y; Yu, Q; Zhang, J; Zhang, P, 2008
)
" This study describes the synergistic activity of oritavancin in combination with gentamicin, linezolid, moxifloxacin, or rifampin in time-kill studies against methicillin-susceptible, vancomycin-intermediate, and vancomycin-resistant Staphylococcus aureus."( Assessment by time-kill methodology of the synergistic effects of oritavancin in combination with other antimicrobial agents against Staphylococcus aureus.
Arhin, FF; Belley, A; McKay, GA; Moeck, G; Neesham-Grenon, E; Parr, TR, 2008
)
"Rifampicin (rifampin) has been reported to have drug-drug interaction with several 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors due to its ability to influence the function of cytochrome P450 enzymes or transporters."( Pharmacokinetics of rosuvastatin when coadministered with rifampicin in healthy males: a randomized, single-blind, placebo-controlled, crossover study.
Cao, D; Chen, XP; Deng, S; He, FY; Li, YJ; Xie, HT; Zhang, W; Zhou, G; Zhou, HH, 2008
)
" Rifabutin, another rifamycin used less frequently than rifampicin, can also interact with drugs metabolized through the hepatic cytochromes."( Pharmacokinetics and pharmacodynamics of drug interactions involving rifampicin, rifabutin and antimalarial drugs.
Boffito, M; Pozniak, A; Sousa, M, 2008
)
"The knowledge about efficacy of linezolid alone or in combination with rifampin in device infections is limited."( Efficacy of linezolid alone and in combination with rifampin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Domenech, A; Euba, G; Gudiol, F; Murillo, O; Tubau, F; Verdaguer, R, 2008
)
"Linezolid alone showed moderate efficacy, whereas its combination with rifampin prevented the emergence of rifampin resistance."( Efficacy of linezolid alone and in combination with rifampin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Domenech, A; Euba, G; Gudiol, F; Murillo, O; Tubau, F; Verdaguer, R, 2008
)
"Resectional lung surgery combined with isoniazid- and rifampin-based anti-tuberculous chemotherapy can be an effective treatment strategy for patients with well-localized, cavitary pulmonary MDR-TB and XDR-TB."( Pulmonary resection combined with isoniazid- and rifampin-based drug therapy for patients with multidrug-resistant and extensively drug-resistant tuberculosis.
Cho, JS; Kang, H; Kim, JH; Park, SK; Smego, RA, 2009
)
"We investigated the activity of linezolid, alone and in combination with rifampin (rifampicin), against a methicillin-resistant Staphylococcus aureus (MRSA) strain in vitro and in a guinea pig model of foreign-body infection."( Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
Baldoni, D; Haschke, M; Rajacic, Z; Trampuz, A; Zimmerli, W, 2009
)
"This study evaluated vancomycin susceptibility and activity alone and in combination with rifampicin and tigecycline against low-biofilm- and high-biofilm-producing methicillin-resistant Staphylococcus aureus (MRSA) clinical isolates."( Impact of biofilm on the in vitro activity of vancomycin alone and in combination with tigecycline and rifampicin against Staphylococcus aureus.
Poppens, PT; Rose, WE, 2009
)
" Time-kill analysis was performed on six low- and six high-biofilm-producing isolates with 15 mg/L vancomycin alone and in combination with rifampicin or tigecycline at 4x MIC."( Impact of biofilm on the in vitro activity of vancomycin alone and in combination with tigecycline and rifampicin against Staphylococcus aureus.
Poppens, PT; Rose, WE, 2009
)
" The aims of this study was to determine the efficacies of meropenem alone and combined with rifampin against two Streptococcus pneumoniae strains with different susceptibility to beta-lactams using the guinea pig meningitis model and compare them with the standard ceftriaxone plus vancomycin therapy."( Evaluation of meropenem alone and combined with rifampin in the guinea pig model of pneumococcal meningitis.
Cabellos, C; Doménech, A; Force, E; Gudiol, F; Ribes, S; Taberner, F; Tubau, F; Viladrich, PF, 2009
)
" In this study we aimed to determine the in vitro activity of hydrogen peroxide (H2O2; reactive oxygen intermediate) and acidified sodium nitrite (ASN; reactive nitrogen intermediate) alone and in combination with rifampicin (RIF) and tetracycline (TET) against four clinical isolates of Brucella melitensis."( [In vitro effect of reactive nitrogen and oxygen intermediates alone and in combination with some antibiotics against Brucella melitensis clinical isolates].
Coban, AY; Durupinar, B; Tanyel, E; Taşdelen Fişgin, N; Tülek, N, 2009
)
"3 log(10) CFU/ml, whereas in combination with rifampin, a reduction in the counts of >6 log(10) CFU/ml was observed."( Efficacy of daptomycin in implant-associated infection due to methicillin-resistant Staphylococcus aureus: importance of combination with rifampin.
Baldoni, D; Haschke, M; John, AK; Rentsch, K; Schaerli, P; Trampuz, A; Zimmerli, W, 2009
)
" The purpose of the present study was to quantify the biofilm formation of methicillin (meticillin)-resistant Staphylococcus aureus (MRSA) isolates obtained from patients with IE and to evaluate the in vitro activities of daptomycin and vancomycin alone and in combination with rifampin (rifampicin) or gentamicin while monitoring the isolates for the development of resistance."( Activities of daptomycin and vancomycin alone and in combination with rifampin and gentamicin against biofilm-forming methicillin-resistant Staphylococcus aureus isolates in an experimental model of endocarditis.
LaPlante, KL; Woodmansee, S, 2009
)
"Vancomycin is often combined with a second antibiotic, most often rifampin or gentamicin, for the treatment of serious methicillin-resistant Staphylococcus aureus infections."( Vancomycin in combination with other antibiotics for the treatment of serious methicillin-resistant Staphylococcus aureus infections.
Deresinski, S, 2009
)
"To review all currently published drug-drug interaction studies with the HIV-integrase inhibitor raltegravir."( Drug-drug interactions with raltegravir.
Burger, DM, 2009
)
"A total of 14 drug-drug interaction studies were found."( Drug-drug interactions with raltegravir.
Burger, DM, 2009
)
"Raltegravir is not without drug-drug interactions but due to the lack of an effect on CYP450 or UGT by raltegravir and the broad therapeutic range of raltegravir itself, this agent can safely combined with almost all tested agents."( Drug-drug interactions with raltegravir.
Burger, DM, 2009
)
" As a result, OATP1B1 and OATP1B3 represent sites for potential drug-drug interactions."( Fluorescence-based assays for the assessment of drug interaction with the human transporters OATP1B1 and OATP1B3.
Bednarczyk, D, 2010
)
"Increasing the ritonavir dose to achieve a lopinavir/ritonavir ratio of 1:1 when given in combination with rifampicin-based TB treatment did not completely compensate for the enhancement of lopinavir CL/F caused by rifampicin."( Population pharmacokinetics of lopinavir in combination with rifampicin-based antitubercular treatment in HIV-infected South African children.
Elsherbiny, D; Maartens, G; McIlleron, H; Ren, Y; Simonsson, US, 2010
)
" Simulated regimens included vancomycin (VAN) plus rifampin (RIF), moxifloxacin (MOX), and high doses (10 mg/kg of body weight/day) of daptomycin (DAP) alone or combined with RIF or clarithromycin (CLA)."( Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
Parra-Ruiz, J; Rose, WE; Rybak, MJ; Vidaillac, C, 2010
)
" Daptomycin in combination with rifampicin needs to be assessed in bone infection."( Efficacy of daptomycin combined with rifampicin for the treatment of experimental meticillin-resistant Staphylococcus aureus (MRSA) acute osteomyelitis.
Amador, G; Asseray, N; Caillon, J; Jacqueline, C; Le Mabecque, V; Lefebvre, M; Miegeville, A; Potel, G, 2010
)
" The aim of this study was to evaluate the efficacies of daptomycin at usual and high doses (equivalent to 6 and 10 mg/kg of body weight/day, respectively, in humans) and in combination with rifampin and to compare the activities to those of conventional anti-MRSA therapies."( Efficacy of usual and high doses of daptomycin in combination with rifampin versus alternative therapies in experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
Ariza, J; Cabellos, C; Cabo, J; Euba, G; Garrigós, C; Murillo, O; Tubau, F; Verdaguer, R, 2010
)
" These results suggest modifications to drug-drug interaction (DDI) trial designs."( Rifampin's acute inhibitory and chronic inductive drug interactions: experimental and model-based approaches to drug-drug interaction trial design.
Cai, X; Chu, X; Ding, Y; Evers, R; Gibson, C; Reitman, ML; Roupe, K; Stoch, A; Stone, JA; Venkatasubramanian, R; Wagner, JA; Witter, R; Yabut, J; Zajic, S, 2011
)
" We studied the effects of Ag85A DNA vaccine alone or in combination with rifampin (RFP) or pyrazinamide (PZA) for the treatment of MDR-TB in mice."( Treatment of multi-drug-resistant tuberculosis in mice with DNA vaccines alone or in combination with chemotherapeutic drugs.
Bai, X; Li, N; Li, Z; Liang, Y; Wang, L; Wu, X; Yang, Y; Yu, Q; Zhang, J, 2011
)
"Conflicting drug-drug interaction (DDI) studies with the HIV protease inhibitors (PIs) suggest net induction or inhibition of intestinal or hepatic CYP3A."( Complex drug interactions of HIV protease inhibitors 1: inactivation, induction, and inhibition of cytochrome P450 3A by ritonavir or nelfinavir.
Collier, AC; Kharasch, ED; Kirby, BJ; Thummel, KE; Unadkat, JD; Whittington, D, 2011
)
"Exposure to vandetanib, as assessed by AUC(504) in healthy subjects, was reduced by around 40% when a single dose was given in combination with the potent CYP3A4 inducer rifampicin."( Pharmacokinetic drug interactions with vandetanib during coadministration with rifampicin or itraconazole.
Duvauchelle, T; Kennedy, SJ; Martin, P; Oliver, S; Read, J; Robertson, J, 2011
)
" Food and Drug Administration draft drug interaction guidance as CYP3A4 inducers for clinical drug-drug interaction (DDI) studies."( Simulation of clinical drug-drug interactions from hepatocyte CYP3A4 induction data and its potential utility in trial designs.
Hayashi, M; Shou, M; Skiles, GL; Xu, Y; Zhou, Y, 2011
)
"Ketoconazole and rifampin are the most widely used compounds examined in recent drug-drug interaction (DDI) studies, and they have multiple roles in modulating drug metabolizing enzymes and transporters."( Inhibitory effects of ketoconazole and rifampin on OAT1 and OATP1B1 transport activities: considerations on drug-drug interactions.
Ahn, SH; Bae, MA; Choi, MK; Choi, YL; Jin, QR; Song, IS, 2011
)
"Information regarding the utility of adjunct diagnostic tests in combination with Xpert MTB/RIF (Cepheid, Sunnyvale, CA, USA) is limited."( Do adjunct tuberculosis tests, when combined with Xpert MTB/RIF, improve accuracy and the cost of diagnosis in a resource-poor setting?
Allwood, B; Calligaro, G; Dawson, R; Dheda, K; Kumar Mishra, H; Meldau, R; Peter, J; Pooran, A; Sharma, SK; Theron, G; van Zyl-Smit, R, 2012
)
"Effectiveness of amphotericin B alone or in combination with rifampicin or clarithromycin on the killing of Candida species biofilms was investigated in vitro."( Effect of amphotericin B alone or in combination with rifampicin or clarithromycin against Candida species biofilms.
Alonso, M; Del Pozo, JL; Francés, ML; Hernáez, S; Rubio, MF; Serrera, A, 2011
)
" When combined with 8 mg/L rifampicin, MBECs for ciprofloxacin and linezolid dropped to 16-32 mg/L for the four isolates tested."( Effectiveness of ciprofloxacin or linezolid in combination with rifampicin against Enterococcus faecalis in biofilms.
Holmberg, A; Mörgelin, M; Rasmussen, M, 2012
)
" The aim of this study was to develop an integrated population pharmacokinetic model accounting for the drug-drug interactions between lopinavir, ritonavir and rifampicin, and to evaluate optimal doses of lopinavir/ritonavir when co-administered with rifampicin."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
"The model describes the drug-drug interactions between lopinavir, ritonavir and rifampicin in adults."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
"The induction of cytochrome P450 (P450) enzymes is one of the risk factors for drug-drug interactions (DDIs)."( Investigation of drug-drug interactions caused by human pregnane X receptor-mediated induction of CYP3A4 and CYP2C subfamilies in chimeric mice with a humanized liver.
Hasegawa, M; Inoue, R; Kakuni, M; Tahara, H; Tateno, C; Ushiki, J, 2012
)
" In conclusion, our results suggested a strong activity of tigecycline alone and in combination with other antimicrobial agents against multi-resistant Gram-positive organisms isolated from wound infections."( In vitro activity and in vivo efficacy of tigecycline alone and in combination with daptomycin and rifampin against Gram-positive cocci isolated from surgical wound infection.
Arzeni, D; Brescini, L; Cirioni, O; Ganzetti, G; Ghiselli, R; Giacometti, A; Guerrieri, M; Offidani, A; Orlando, F; Provinciali, M; Silvestri, C; Simonetti, O; Staffolani, S, 2012
)
"As part of a larger clinical drug-drug interaction (DDI) study aimed at in vitro to in vivo prediction of HIV protease inhibitor metabolic and transporter-based DDIs, we measured the inductive (staggered administration) and inductive plus inhibitory (simultaneously administered) effect of multiple dose ritonavir (RTV), nelfinavir (NFV), or rifampin (RIF) on the pharmacokinetics of the P-glycoprotein probe, digoxin (DIG), when administered simultaneously or staggered with the protease inhibitors or RIF."( Complex drug interactions of the HIV protease inhibitors 3: effect of simultaneous or staggered dosing of digoxin and ritonavir, nelfinavir, rifampin, or bupropion.
Collier, AC; Kharasch, ED; Kirby, BJ; Thummel, KE; Unadkat, JD; Whittington, D, 2012
)
" Drug therapy either alone or in combination with BCG, was more effective at lessening clinical disease and lesion severity compared to control animals or those receiving BCG alone."( Drug treatment combined with BCG vaccination reduces disease reactivation in guinea pigs infected with Mycobacterium tuberculosis.
Ackart, D; Basaraba, RJ; Caraway, ML; Hascall-Dove, L; Henao-Tamayo, M; Ordway, DJ; Orme, EA; Orme, IM; Shang, S; Shanley, CA, 2012
)
"Antibiotics combined with surgery may significantly increase treatment success for Mycobacterium ulcerans infections, and fluoroquinolone combined with rifampicin-containing antibiotic regimens can provide an effective and safe oral treatment option."( Successful outcomes with oral fluoroquinolones combined with rifampicin in the treatment of Mycobacterium ulcerans: an observational cohort study.
Athan, E; Callan, P; Friedman, ND; Holten, I; Hughes, A; McDonald, A; O'Brien, DP; Robson, M; Walton, A, 2012
)
"We report a case of postsurgical meningitis caused by multiresistant Acinetobacter baumannii successfully treated with high doses of ampicillin/sulbactam combined with rifampicin and fosfomycin."( Postsurgical meningitis due to multiresistant Acinetobacter baumannii successfully treated with high doses of ampicillin/sulbactam combined with rifampicin and fosfomycin.
Clec'h, C; Cohen, Y; Jauréguy, F; Mellon, G; Picard, B, 2012
)
"In this open-label, 2-part, 3-treatment, 1-sequence, 2-period crossover drug-drug interaction study, 1 group of subjects received a single 50-mg oral dose of gemigliptin on 2 separate occasions-once as monotherapy and again after pretreatment with 400 mg of oral ketoconazole once daily for 7 days."( Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers.
Bae, KS; Choi, HY; Jin, SJ; Kim, MJ; Kim, YH; Lim, HS; Noh, YH; Sung, HR, 2012
)
" These findings suggest that gemigliptin may require a dose adjustment when concurrently administered with drugs that alter CYP3A4 activity."( Effects of ketoconazole and rifampicin on the pharmacokinetics of gemigliptin, a dipeptidyl peptidase-IV inhibitor: a crossover drug-drug interaction study in healthy male Korean volunteers.
Bae, KS; Choi, HY; Jin, SJ; Kim, MJ; Kim, YH; Lim, HS; Noh, YH; Sung, HR, 2012
)
"The hepatic organic anion transporting polypeptides (OATPs) influence the pharmacokinetics of several drug classes and are involved in many clinical drug-drug interactions."( Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
Artursson, P; Haglund, U; Karlgren, M; Kimoto, E; Lai, Y; Norinder, U; Vildhede, A; Wisniewski, JR, 2012
)
"To develop physiologically based pharmacokinetic (PBPK) model to predict the pharmacokinetics and drug-drug interactions (DDI) of pravastatin, using the in vitro transport parameters."( Physiologically based modeling of pravastatin transporter-mediated hepatobiliary disposition and drug-drug interactions.
Bergman, A; Feng, B; Goosen, TC; Lai, Y; Litchfield, J; Varma, MV, 2012
)
" For TB drugs, equivalence was suggested for peak plasma concentrations when administered with and without efavirenz/tenofovir/emtricitabine."( Efavirenz, tenofovir and emtricitabine combined with first-line tuberculosis treatment in tuberculosis-HIV-coinfected Tanzanian patients: a pharmacokinetic and safety study.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Fillekes, Q; Kibiki, GS; Kisanga, ER; Kisonga, RM; Mleoh, L; Mtabho, CM; Ndaro, A; Semvua, HH; van den Boogaard, J; van der Ven, A, 2013
)
" We used a panel of stably and transiently transfected cell lines to elucidate the carrier-mediated transport processes that are involved in linagliptin disposition in vivo and to assess the potential for drug-drug interactions (DDIs)."( Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods.
Ebner, T; Ishiguro, N; Kishimoto, W; Schaefer, O; Shimizu, H, 2013
)
"Comprehensive information on the effects of cytochrome P450 2B6 (CYP2B6) polymorphisms, clinical factors, and drug-drug interactions on efavirenz concentrations in HIV/tuberculosis-coinfected (HIV/TB) patients is unavailable."( Impact of pharmacogenetic markers of CYP2B6, clinical factors, and drug-drug interaction on efavirenz concentrations in HIV/tuberculosis-coinfected patients.
Lueangniyomkul, A; Mankatitham, W; Manosuthi, S; Manosuthi, W; Nilkamhang, S; Sukasem, C; Sungkanuparph, S; Thongyen, S, 2013
)
"Organic anion-transporting polypeptides (OATP) 1B1, 1B3, and 2B1 can serve as the loci of drug-drug interactions (DDIs)."( Cynomolgus monkey as a potential model to assess drug interactions involving hepatic organic anion transporting polypeptides: in vitro, in vivo, and in vitro-to-in vivo extrapolation.
Balimane, P; Chen, C; Han, YH; Jemal, M; Kallipatti, S; Krishnamurthy, P; Marathe, P; Mintier, G; Rodrigues, AD; Selvam, S; Shen, H; Sukrutharaj, S; Yang, Z; Zhang, R; Zhao, W, 2013
)
"Rodent models are less suitable for predicting drug-drug interactions at the level of the human intestinal mucosa, especially when nuclear receptors such as pregnane X receptor (PXR) are involved."( PXR/CYP3A4-humanized mice for studying drug-drug interactions involving intestinal P-glycoprotein.
Annaert, P; Augustijns, P; Baes, M; Gonzalez, FJ; Holmstock, N, 2013
)
" As adult studies cannot reliably predict their magnitude in children, drug-drug interactions should be evaluated in paediatric patient populations."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
"Treatment of Gram-positive osteoarticular infections requires an adequate surgical approach combined with intensive antimicrobial therapy."( The safety and efficacy of high-dose daptomycin combined with rifampicin for the treatment of Gram-positive osteoarticular infections.
Garbino, J; Hoffmeyer, P; Jugun, K; Lew, D; Pagani, L; Uçkay, I; Vaudaux, P, 2013
)
"Digoxin is the recommended substrate for assessment of P-glycoprotein (P-gp)-mediated drug-drug interactions (DDIs) in vivo."( Application of permeability-limited physiologically-based pharmacokinetic models: part II - prediction of P-glycoprotein mediated drug-drug interactions with digoxin.
Barter, Z; Jamei, M; Neuhoff, S; Rostami-Hodjegan, A; Turner, DB; Yeo, KR, 2013
)
" Simultaneous drug-drug interactions through uptake and efflux transport systems in hepatocytes according to the cellular concentrations of competing drugs were never investigated."( Evidence of drug-drug interactions through uptake and efflux transport systems in rat hepatocytes: implications for cellular concentrations of competing drugs.
Daali, Y; Dayer, P; Millet, P; Pastor, CM, 2013
)
" Three studies were designed to evaluate the potential drug-drug interaction of netupitant with palonosetron and of the fixed dose combination of netupitant and palonosetron, NEPA, with an inhibitor (ketoconazole), an inducer (rifampicin) and a substrate (oral contraceptives) of CYP3A4."( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives.
Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013
)
" In study 2, 36 subjects received NEPA alone (day 1) and in combination with ketoconazole or rifampicin."( Effect of netupitant, a highly selective NK₁ receptor antagonist, on the pharmacokinetics of palonosetron and impact of the fixed dose combination of netupitant and palonosetron when coadministered with ketoconazole, rifampicin, and oral contraceptives.
Calcagnile, S; Henriksson, A; Kammerer, KP; Lanzarotti, C; Rossi, G; Timmer, W, 2013
)
" This study evaluated the CYP3A-mediated drug-drug interaction potential of brentuximab vedotin and the excretion of MMAE."( CYP3A-mediated drug-drug interaction potential and excretion of brentuximab vedotin, an antibody-drug conjugate, in patients with CD30-positive hematologic malignancies.
Alley, SC; Chen, R; Cooper, M; Gopal, AK; Goy, A; Grove, LE; Han, TH; Lynch, CM; Matous, JV; O'Connor, OA; Ramchandren, R, 2013
)
"We studied if the clinical pharmacokinetics and drug-drug interactions (DDIs) of the sulfonylurea-derivative glibenclamide can be simulated via a physiologically-based pharmacokinetic modeling approach."( Semi-mechanistic physiologically-based pharmacokinetic modeling of clinical glibenclamide pharmacokinetics and drug-drug-interactions.
Benne, MS; Greupink, R; Huisman, MT; Russel, FG; Schreurs, M, 2013
)
"The activity of dalbavancin, a representative of the lipoglycopeptide antibiotics, alone and in combination with rifampicin, was investigated against meticillin-resistant Staphylococcus aureus (MRSA) in a foreign-body infection model in guinea pigs."( Activity of dalbavancin, alone and in combination with rifampicin, against meticillin-resistant Staphylococcus aureus in a foreign-body infection model.
Aeppli, S; Angevaare, E; Baldoni, D; Furustrand Tafin, U; Haschke, M; Oliva, A; Trampuz, A; Zimmerli, W, 2013
)
"The identification and quantification of potential drug-drug interactions is important for avoiding or minimizing the interaction-induced adverse events associated with specific drug combinations."( Pharmacokinetic drug interactions involving vortioxetine (Lu AA21004), a multimodal antidepressant.
Buchbjerg, JK; Chen, G; Højer, AM; Lee, R; Serenko, M; Zhao, Z, 2013
)
" The fractional inhibition concentration indices (FICI) for vancomycin combined with rifampicin, levofloxacin or fosfomycin were ≥1."( Comparative study of the mutant prevention concentrations of vancomycin alone and in combination with levofloxacin, rifampicin and fosfomycin against methicillin-resistant Staphylococcus epidermidis.
Cheng, J; Hu, LF; Li, JB; Liu, LG; Ye, Y; Zhu, YL, 2013
)
"5% of the strains for meropenem combination with tigecycline."( Activity of Tigecycline in combination with Colistin, Meropenem, Rifampin, or Gentamicin against KPC-producing Enterobacteriaceae in a murine thigh infection model.
Labrou, M; Manousaka, S; Michail, G; Pitiriga, V; Pournaras, S; Sakellaridis, N; Tsakris, A, 2013
)
" Here, we address the clinical relevance of CYP3A4-related drug-drug interactions with midostaurin as either a "victim" or "perpetrator."( Investigation into CYP3A4-mediated drug-drug interactions on midostaurin in healthy volunteers.
Dutreix, C; Lorenzo, S; Munarini, F; Roesel, J; Wang, Y, 2013
)
"Induction of cytochrome P450 3A4 (CYP3A4) expression is often implicated in clinically relevant drug-drug interactions (DDI), as metabolism catalyzed by this enzyme is the dominant route of elimination for many drugs."( Modeling of rifampicin-induced CYP3A4 activation dynamics for the prediction of clinical drug-drug interactions from in vitro data.
Asai, Y; Hashida, M; Hisaka, A; Kitano, H; Sasa, Y; Suzuki, H; Yamashita, F; Yoshida, S, 2013
)
"The aim of this study was to investigate the in vitro activities of polymyxin B (PB) and rifampin (RIF) in combination with ampicillin/sulbactam (AS) or cefoperazone/sulbactam (CS) against 20 multidrug-resistant Acinetobacter baumannii (MDR-AB) isolates by the checkerboard and E-test methods."( Determination of in vitro activities of polymyxin B and rifampin in combination with ampicillin/sulbactam or cefoperazone/sulbactam against multidrug-resistant Acinetobacter baumannii by the E-test and checkerboard methods.
Aridogan, BC; Cetin, ES; Ozseven, AG; Tekeli, A; Us, E, 2013
)
" Tigecycline in combination with rifampin demonstrated higher activity against bacteria embedded in biofilms than tigecycline alone."( Antimicrobial activity of tigecycline alone or in combination with rifampin against Staphylococcus epidermidis in biofilm.
Kaznowski, A; Szczuka, E, 2014
)
" As afatinib is not a relevant modulator or substrate of cytochrome P450 enzymes, the drug-drug interaction potential is considered to be low."( Pharmacokinetic drug interactions of afatinib with rifampicin and ritonavir.
Bertulis, J; Brand, T; Gansser, D; Giessmann, T; Hocke, J; Jungnik, A; Marzin, K; Stopfer, P; Wind, S, 2014
)
" We compared the synergistic activity and post-antibiotic effect (PAE) of colistin in combination with other antimicrobials against colistin-susceptible and -resistant KPC-Kp bloodstream isolates."( In vitro activity and post-antibiotic effects of colistin in combination with other antimicrobials against colistin-resistant KPC-producing Klebsiella pneumoniae bloodstream isolates.
Ambretti, S; Bonora, S; Gaibani, P; Landini, MP; Lewis, RE; Lombardo, D; Mercuri, M, 2014
)
" Evaluation of a drug-drug interaction (DDI) study and supportive semi-mechanistic population pharmacokinetic (PK) analyses were undertaken to help delineate this issue."( Why did the FDA approve efavirenz 800 mg when co-administered with rifampin?
Arya, V; Chan-Tack, KM; Jadhav, P; Kraft, J; Liu, J; Robertson, SM; Seo, S; Singer, ME; Struble, KA, 2014
)
" Simulations compared EFV exposure at various doses in combination with RIF to EFV exposures at 600 mg once daily (QD)."( Why did the FDA approve efavirenz 800 mg when co-administered with rifampin?
Arya, V; Chan-Tack, KM; Jadhav, P; Kraft, J; Liu, J; Robertson, SM; Seo, S; Singer, ME; Struble, KA, 2014
)
" In time-kill assays, COL combined with either RIF or TGC was superior to single agents, but only the COL/RIF regimen was reliably bactericidal."( Activity of colistin in combination with tigecycline or rifampicin against multidrug-resistant Stenotrophomonas maltophilia.
Betts, JW; Phee, LM; Wareham, DW; Woodford, N, 2014
)
"To evaluate potential drug-drug interactions with the atypical antipsychotic lurasidone."( Lurasidone drug-drug interaction studies: a comprehensive review.
Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014
)
" No dose adjustment for lurasidone is needed when administered with lithium or valproate."( Lurasidone drug-drug interaction studies: a comprehensive review.
Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014
)
" This midostaurin drug-drug interaction study assessed the dynamic response and clinical usefulness of urinary 6β-hydroxycortisol to cortisol ratio (6βCR) and plasma 4β-hydroxycholesterol (4βHC) for monitoring CYP3A4 activity in the presence or absence of rifampicin, a strong CYP3A4 inducer."( Comparison of two endogenous biomarkers of CYP3A4 activity in a drug-drug interaction study between midostaurin and rifampicin.
Dutreix, C; Lorenzo, S; Wang, Y, 2014
)
"New verapamil analogues were synthesized and their inhibitory activities against Mycobacterium tuberculosis H37Rv determined in vitro alone and in combination with rifampicin (RIF)."( Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
Chibale, K; Kumar, M; Naran, K; Pavadai, E; Ruminski, PG; Singh, K; Warner, DF, 2014
)
" In this study, we sought to investigate the sterilizing activity of human-equivalent doses of thioridazine when given in combination with the "Denver regimen" against acute murine tuberculosis."( Sterilizing activity of thioridazine in combination with the first-line regimen against acute murine tuberculosis.
Dutta, NK; Karakousis, PC; Pinn, ML, 2014
)
" The aim of the current work was to develop a novel physiologically based pharmacokinetic (PBPK) model to quantitatively assess the magnitude of CYP3A4 mediated drug-drug interactions with alisporivir as the substrate or victim drug."( Physiologically based pharmacokinetic modeling for assessing the clinical drug-drug interaction of alisporivir.
Alexander, N; Barve, A; Einolf, H; Gu, H; Hanna, I; He, H; Heimbach, T; Ke, J; Mangold, JB; Sunkara, G; Wang, L; Xia, B; Zhang, T, 2014
)
"The prediction of drug-drug interactions mediated by the induction or inhibition of cytochrome P450 enzymes is of great relevance in the development of new drugs."( HepaRG cell line as an in vitro model for screening drug-drug interactions mediated by metabolic induction: amiodarone used as a model substance.
Alves, G; Falcão, A; Ferreira, A; Rodrigues, M; Silvestre, S, 2014
)
" Therefore, evaluating the drug-drug interaction (DDI) potential associated with MMAE is important in the clinical development of ADCs."( Physiologically based pharmacokinetic modeling as a tool to predict drug interactions for antibody-drug conjugates.
Chen, Y; Girish, S; Hop, C; Jin, JY; Li, C; Lu, D; Mukadam, S; Samineni, D; Shen, BQ; Wong, H, 2015
)
"The risk assessment of organic anion transporting polypeptide (OATP) 1B1-mediated drug-drug interactions (DDIs) is an indispensable part of drug development."( Investigation of the impact of substrate selection on in vitro organic anion transporting polypeptide 1B1 inhibition profiles for the prediction of drug-drug interactions.
Izumi, S; Komori, T; Kusuhara, H; Maeda, K; Nozaki, Y; Sugiyama, Y; Takenaka, O, 2015
)
" In addition, using serial sampling methods can be valuable for evaluation of the drug-drug interaction (DDI) potential of drug candidates."( Using improved serial blood sampling method of mice to study pharmacokinetics and drug-drug interaction.
Nezasa, K; Ogawa, K; Shimizu, R; Takai, N; Tanaka, Y; Watanabe, A; Watari, R; Yamaguchi, Y, 2015
)
"Colistin, tigecycline, levofloxacin, tobramycin, and rifampin alone and in combination with doripenem were investigated for their in vitro activities and postantibiotic effects (PAEs) on Klebsiella pneumoniae."( Effects of various antibiotics alone or in combination with doripenem against Klebsiella pneumoniae strains isolated in an intensive care unit.
Mataraci-Kara, E; Ozbek Celik, B; Yilmaz, M, 2014
)
" This first study in patients was done to determine safety, tolerability, pharmacokinetics and bacteriological effect of different doses of SQ109 alone and in combination with rifampicin when administered over 14 days."( Early phase evaluation of SQ109 alone and in combination with rifampicin in pulmonary TB patients.
Aarnoutse, RE; Boeree, MJ; Dawson, R; Diacon, AH; du Bois, J; Gillespie, SH; Heinrich, N; Henne, S; Hoelscher, M; Horwith, G; Nacy, CA; Narunsky, K; Phillips, PP; Phipps, AJ; Rachow, A; Venter, A, 2015
)
"Physiologically based pharmacokinetic modeling was applied to characterize the potential drug-drug interactions for ruxolitinib."( Predicting drug-drug interactions involving multiple mechanisms using physiologically based pharmacokinetic modeling: a case study with ruxolitinib.
Fraczkiewicz, G; Shi, JG; Williams, WV; Yeleswaram, S, 2015
)
" This study was carried out to identify the contribution percentage of CYP450 to icotinib and use the results to develop a physiologically based pharmacokinetic (PBPK) model, which can help to predict drug-drug interaction (DDI)."( Relative contributions of the major human CYP450 to the metabolism of icotinib and its implication in prediction of drug-drug interaction between icotinib and CYP3A4 inhibitors/inducers using physiologically based pharmacokinetic modeling.
Chen, J; Hu, P; Jiang, J; Liu, D; Zhao, Q; Zheng, X, 2015
)
" Tasimelteon is rapidly absorbed, with a mean absolute bioavailability of approximately 38%, and is extensively metabolized primarily by oxidation at multiple sites, mainly by cytochrome P450 (CYP) 1A2 and CYP3A4/5, as initially demonstrated by in vitro studies and confirmed by the results of clinical drug-drug interactions presented here."( Clinical assessment of drug-drug interactions of tasimelteon, a novel dual melatonin receptor agonist.
Baroldi, P; Dressman, MA; Kramer, WG; Ogilvie, BW; Torres, R, 2015
)
" Pharmacokinetic (PK) drug-drug interactions (DDIs) were evaluated clinically between cabozantinib and (1) a CYP3A inducer (rifampin) in healthy volunteers, (2) a CYP3A inhibitor (ketoconazole) in healthy volunteers, and (3) a CYP2C8 substrate (rosiglitazone) in patients with solid tumors."( Pharmacokinetic (PK) drug interaction studies of cabozantinib: Effect of CYP3A inducer rifampin and inhibitor ketoconazole on cabozantinib plasma PK and effect of cabozantinib on CYP2C8 probe substrate rosiglitazone plasma PK.
Benrimoh, N; Engel, C; Holland, J; Lacy, S; Miles, D; Nguyen, L; O'Reilly, T, 2015
)
" haemolyticus strains isolated from bloodstream infections and assess in vitro the activity of rifampicin combined with daptomycin or tigecycline against bacteria growing in a biofilm."( In Vitro Activity of Rifampicin Combined with Daptomycin or Tigecycline on Staphylococcus haemolyticus Biofilms.
Grabska, K; Kaznowski, A; Szczuka, E, 2015
)
" This study systematically evaluated by in vitro time-kill studies the effect of daptomycin in combination with ampicillin, cefazolin, ceftriaxone, ceftaroline, ertapenem, gentamicin, tigecycline, and rifampin, for a collection of 9 daptomycin-NS enterococci that exhibited a broad range of MICs and different resistance-conferring mutations."( In vitro activity of daptomycin in combination with β-lactams, gentamicin, rifampin, and tigecycline against daptomycin-nonsusceptible enterococci.
Carvalho, M; Charlton, CL; Hindler, JA; Humphries, R; Kelesidis, T; Miller, SA; Nizet, V; Nonejuie, P; Pogliano, J; Sakoulas, G; Wong-Beringer, A, 2015
)
"Since drug-drug interaction (DDI) can affect organic anion-transporting polypeptide (OATP) and cause clinical events, prediction of such DDI is important in early clinical development."( Dehydroepiandrosterone sulfate, a useful endogenous probe for evaluation of drug-drug interaction on hepatic organic anion transporting polypeptide (OATP) in cynomolgus monkeys.
Tamai, I; Watanabe, M; Watanabe, T; Yabuki, M, 2015
)
" Overall, the safety profile of romidepsin was not altered by coadministration with ketoconazole or rifampin, except that a higher incidence and greater severity of thrombocytopenia was observed when romidepsin was given with rifampin."( Evaluation of CYP3A-mediated drug-drug interactions with romidepsin in patients with advanced cancer.
Arkenau, HT; Burris, HA; Infante, J; Jones, SF; Laille, E; Lemech, C; Liu, L; Patel, M, 2015
)
" The model was used to predict the pharmacokinetic profiles and drug-drug interaction (DDI) effect for atorvastatin and its metabolites in different DDI scenarios."( Physiologically based pharmacokinetic modeling of disposition and drug-drug interactions for atorvastatin and its metabolites.
Zhang, T, 2015
)
" These predictions were in good agreement with clinical single dose drug-drug interaction studies, but not with reports of imatinib interactions at steady-state."( Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation.
Beumer, JH; Christner, SM; Kiesel, BF; Parise, RA; Pillai, VC; Rudek, MA; Venkataramanan, R, 2015
)
" The main objectives of the present study were to: 1) develop and refine a physiologically based pharmacokinetic (PBPK) model of crizotinib on the basis of clinical single- and multiple-dose results, 2) verify the crizotinib PBPK model from crizotinib single-dose drug-drug interaction (DDI) results with multiple-dose coadministration of ketoconazole or rifampin, and 3) apply the crizotinib PBPK model to predict crizotinib multiple-dose DDI outcomes."( Prediction of Drug-Drug Interactions with Crizotinib as the CYP3A Substrate Using a Physiologically Based Pharmacokinetic Model.
Johnson, TR; Smith, BJ; Yamazaki, S, 2015
)
"This example of the application of PBPK modeling to predict drug-drug interactions was used to support the labeling of macitentan (Opsumit)."( Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug-Drug Interactions.
Buchmann, S; de Kanter, R; Delahaye, S; Gnerre, C; Kohl, C; Segrestaa, J; Sidharta, PN; Treiber, A, 2016
)
"New compounds with antituberculosis activity and their combination with classic drugs have been evaluated to determine possible interactions and antagonism."( Potential of Casiopeínas® Copper Complexes and Antituberculosis Drug Combination against Mycobacterium tuberculosis.
Barbosa, AR; Caleffi-Ferracioli, KR; Cardoso, RF; García-Ramos, JC; Leite, CQ; Pavan, FR; Ruiz-Azuara, L; Siqueira, VL; Toledano-Magaña, Y, 2016
)
" However, the potential drug-drug interactions between moxifloxacin and rifampicin were unknown."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
" Preclinical studies of GTx-024 supported the evaluation of several potential drug-drug interactions in a clinical setting."( Pharmacokinetic drug interactions of the selective androgen receptor modulator GTx-024(Enobosarm) with itraconazole, rifampin, probenecid, celecoxib and rosuvastatin.
Coss, CC; Dalton, JT; Jones, A, 2016
)
" Study A: When given with ketoconazole, abiraterone exposure increased by 9% for maximum plasma concentration (Cmax ) and 15% for area under the plasma concentration-time curve from 0 to time of the last quantifiable concentration (AUClast ) and AUC from time 0 to infinity (AUC∞ ) compared to abiraterone acetate alone."( Impact on abiraterone pharmacokinetics and safety: Open-label drug-drug interaction studies with ketoconazole and rifampicin.
Acharya, M; Bernard, A; Chien, C; De Vries, R; Jiao, J; Monbaliu, J; Stieltjes, H; Tran, N; Vaccaro, N; Yu, M, 2015
)
" A clinical drug-drug interaction (DDI) study with the potent CYP3A4 inhibitor itraconazole resulted in an approximately sevenfold increase in cobimetinib exposure."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
" Using a murine thigh-infection model, we examined the in vivo efficacy of colistin in combination with meropenem, tigecycline, fosfomycin, fusidic acid, rifampin, or sulbactam against 12 XDR-AB strains."( Activity of Colistin in Combination with Meropenem, Tigecycline, Fosfomycin, Fusidic Acid, Rifampin or Sulbactam against Extensively Drug-Resistant Acinetobacter baumannii in a Murine Thigh-Infection Model.
Cong, Y; Fan, B; Guan, J; Wang, X, 2016
)
" Collectively, we conclude that CP-I and CP-III in plasma and urine can be appropriate endogenous biomarkers specifically and reliably reflecting OATP inhibition, and thus the measurement of these molecules can serve as a useful tool to assess OATP drug-drug interaction liabilities in early clinical studies."( Coproporphyrins in Plasma and Urine Can Be Appropriate Clinical Biomarkers to Recapitulate Drug-Drug Interactions Mediated by Organic Anion Transporting Polypeptide Inhibition.
Cheng, Y; Dai, J; Date, O; Gaud, N; Holenarsipur, VK; Humphreys, WG; Lai, Y; Langish, R; Mandlekar, S; Marathe, P; Murugesan, S; Rajanna, P; Selvam, S; Shen, H; Shipkova, P, 2016
)
" The objective of the present study was to identify the mechanism of clopidogrel-mediated drug-drug interactions (DDIs) on the pharmacokinetics of OATP1B1 and/or CYP2C8 substrates in vivo."( Clarification of the Mechanism of Clopidogrel-Mediated Drug-Drug Interaction in a Clinical Cassette Small-dose Study and Its Prediction Based on In Vitro Information.
Ieiri, I; Irie, S; Kim, SJ; Kimura, M; Kusuhara, H; Maeda, K; Sugiyama, Y; Yoshikado, T, 2016
)
" Three studies were conducted to evaluate the potential drug-drug interactions between delamanid and antiretroviral drugs, including ritonavir, a strong inhibitor of CYP3A4, and selected anti-TB drugs, including rifampin, a strong inducer of cytochrome P450 (CYP) isozymes."( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects.
Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016
)
" We present results from 3 fixed-sequence studies evaluating drug-drug interactions for alectinib through CYP3A."( Clinical Drug-Drug Interactions Through Cytochrome P450 3A (CYP3A) for the Selective ALK Inhibitor Alectinib.
Bogman, K; Bordogna, W; Cleary, Y; Dall, G; De Petris, L; Guerini, E; Martin-Facklam, M; Morcos, PN; Phipps, A; Viteri, S; Yu, L, 2017
)
" Imipenem, meropenem and doripenem were significantly more effective (reduced fold-change of MICs) when combined with rifampicin in bla VIM-negative isolates, especially in isolates with porin frameshift mutation."( In vitro antibacterial activity of rifampicin in combination with imipenem, meropenem and doripenem against multidrug-resistant clinical isolates of Pseudomonas aeruginosa.
Hu, YF; Liu, CP; Shih, SC; Wang, NY, 2016
)
" We evaluated the quantitative role of hepatic uptake transport in its pharmacokinetics and drug-drug interactions (DDIs)."( Transporter-Mediated Hepatic Uptake Plays an Important Role in the Pharmacokinetics and Drug-Drug Interactions of Montelukast.
Bi, Y; El-Kattan, AF; Eng, H; Kalgutkar, AS; Kimoto, E; Lin, J; Rodrigues, AD; Scialis, R; Tremaine, LM; Varma, MV, 2017
)
" Fusidic acid (FA) has been used for decades for bone infection, including prosthetic joint infection (PJI), often in combination with rifampin (RIF)."( A Randomized Study Evaluating Oral Fusidic Acid (CEM-102) in Combination With Oral Rifampin Compared With Standard-of-Care Antibiotics for Treatment of Prosthetic Joint Infections: A Newly Identified Drug-Drug Interaction.
Berkowitz, R; Darouiche, R; Fernandes, P; Iglesias-Ussel, MD; Keedy, K; Kreuzer, S; MacLauchlin, C; Mould, DR; Oldach, D; Pushkin, R, 2016
)
" The sponsor elected to terminate this study due to a clearly illustrated drug-drug interaction between FA and RIF, which lowered FA levels to a degree that could influence subject outcomes."( A Randomized Study Evaluating Oral Fusidic Acid (CEM-102) in Combination With Oral Rifampin Compared With Standard-of-Care Antibiotics for Treatment of Prosthetic Joint Infections: A Newly Identified Drug-Drug Interaction.
Berkowitz, R; Darouiche, R; Fernandes, P; Iglesias-Ussel, MD; Keedy, K; Kreuzer, S; MacLauchlin, C; Mould, DR; Oldach, D; Pushkin, R, 2016
)
" Ultimately, the good permeability, moderate rates of metabolism and low risk of drug-drug interactions displayed by some of the synthesized compounds indicate that 2-(quinolin-4-yloxy)acetamides may yield candidates to use in the development of novel alternative therapeutics for tuberculosis treatment."( New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
Abbadi, BL; Back, DF; Basso, LA; Campos, MM; Giacobbo, BC; Grams, ES; Machado, P; Pissinate, K; Rodrigues-Junior, V; Santos, DS; Sperotto, N; Subtil, FT; Trindade, RV; Villela, AD, 2017
)
" The main objectives of this study were to 1) develop physiologically based pharmacokinetic (PBPK) models of bosutinib; 2) verify and refine the PBPK models based on clinical study results of bosutinib single-dose drug-drug interaction (DDI) with ketoconazole and rifampin, as well as single-dose drug-disease interaction (DDZI) in patients with renal and hepatic impairment; 3) apply the PBPK models to predict DDI outcomes in patients with weak and moderate CYP3A inhibitors; and 4) apply the PBPK models to predict DDZI outcomes in renally and hepatically impaired patients after multiple-dose administration."( Application of Physiologically Based Pharmacokinetic Modeling to the Understanding of Bosutinib Pharmacokinetics: Prediction of Drug-Drug and Drug-Disease Interactions.
Abbas, R; Hsyu, PH; Loi, CM; Ono, C; Yamazaki, S, 2017
)
"Rosuvastatin is a frequently used probe in transporter-mediated drug-drug interaction (DDI) studies."( Investigating Transporter-Mediated Drug-Drug Interactions Using a Physiologically Based Pharmacokinetic Model of Rosuvastatin.
Leil, T; Wang, Q; Zheng, M, 2017
)
"A microdose drug-drug interaction (DDI) study may be a valuable tool for anticipating drug interaction at therapeutic doses."( Drug-drug interaction of microdose and regular-dose omeprazole with a CYP2C19 inhibitor and inducer.
Bae, SH; Han, S; Park, GJ; Park, MH; Park, WS; Shin, SH; Shin, YG; Yim, DS, 2017
)
"This study aims to investigate the drug-drug interactions (DDIs) between orally administered atorvastatin (ATV) and rifampicin (RIF) in rats."( Quantitative Analysis of the Transporter-Mediated Drug-Drug Interaction Between Atorvastatin and Rifampicin Using a Stable Isotope-IV Method.
Hasegawa, T; Higashino, H; Kataoka, M; Minami, K; Mutaguchi, K; Tachihara, M; Togashi, K; Yamashita, S, 2017
)
" Eighty-eight patients were enrolled across the 3 drug-drug interaction studies; the ixazomib toxicity profile was consistent with previous studies."( Effects of Strong CYP3A Inhibition and Induction on the Pharmacokinetics of Ixazomib, an Oral Proteasome Inhibitor: Results of Drug-Drug Interaction Studies in Patients With Advanced Solid Tumors or Lymphoma and a Physiologically Based Pharmacokinetic Ana
Bessudo, A; Esseltine, DL; Gupta, N; Hanley, MJ; Ke, A; Liu, G; Nemunaitis, J; O'Neil, BH; Patel, C; Rasco, DW; Rowland Yeo, K; Sharma, S; Venkatakrishnan, K; Wang, B; Xia, C; Zhang, X, 2018
)
" Based on a previous clinical drug-drug interaction study with ketoconazole (KTZ), the contribution of CYP3A4 in vivo was estimated to be ∼40%."( Physiologically Based Pharmacokinetic Model Predictions of Panobinostat (LBH589) as a Victim and Perpetrator of Drug-Drug Interactions.
Chun, DY; Einolf, HJ; Gu, H; He, H; Lin, W; Mangold, JB; Wang, L; Won, CS, 2017
)
" It has been demonstrated to be informative and helpful to quantify the modification in drug exposure due to specific physio-pathological conditions, age, genetic polymorphisms, ethnicity and particularly drug-drug interactions (DDIs)."( Prediction of drug-drug interactions using physiologically-based pharmacokinetic models of CYP450 modulators included in Simcyp software.
Daali, Y; Desmeules, JA; Marsousi, N; Rudaz, S, 2018
)
" Rifampicin (RIF) and isoniazid (ISO) are first line combination drugs for treatment of tuberculosis (TB) that negatively interact with each other upon simultaneous release in acidic environment."( Anti-tuberculosis drug combination for controlled oral delivery using 3D printed compartmental dosage forms: From drug product design to in vivo testing.
Boetker, JP; Bohr, A; Colombo, S; Genina, N; Harmankaya, N; Rantanen, J, 2017
)
" The purpose of this research was to predict the magnitude of drug-drug interaction (DDI) after coadministration of a strong CYP3A4 inducer or inhibitor using physiologically based pharmacokinetic (PBPK) modeling."( A Physiologically Based Pharmacokinetic Modeling Approach to Predict Drug-Drug Interactions of Buprenorphine After Subcutaneous Administration of CAM2038 With Perpetrators of CYP3A4.
Gobburu, JVS; Liu, T, 2018
)
" In vitro and clinical drug-drug interaction (DDI) studies indicated that midostaurin and its metabolites are substrates, reversible and time-dependent inhibitors, and inducers of CYP3A4."( Simultaneous Physiologically Based Pharmacokinetic (PBPK) Modeling of Parent and Active Metabolites to Investigate Complex CYP3A4 Drug-Drug Interaction Potential: A Case Example of Midostaurin.
Chun, DY; Dutreix, C; Einolf, HJ; Gu, H; He, H; Ouatas, T; Rebello, S; Wang, L, 2018
)
" We describe the pharmacokinetics of and potential drug-drug interactions between lopinavir-ritonavir and drugs routinely used for MDR-TB treatment in HIV-infected children."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
" Treatments of colistin alone or combined with rifampicin or meropenem were started 1 h after infection."( Activity of colistin alone or in combination with rifampicin or meropenem in a carbapenem-resistant bioluminescent Pseudomonas aeruginosa intraperitoneal murine infection model.
Cai, Y; Wang, J; Wang, R; Yang, D, 2018
)
"In vivo imaging showed that both low- and high-dose colistin combined with rifampicin resulted in a significant decrease in bioluminescence signals compared with monotherapy of colistin or rifampicin alone, whereas colistin and meropenem combination therapy did not show a greater bactericidal effect compared with monotherapy."( Activity of colistin alone or in combination with rifampicin or meropenem in a carbapenem-resistant bioluminescent Pseudomonas aeruginosa intraperitoneal murine infection model.
Cai, Y; Wang, J; Wang, R; Yang, D, 2018
)
"This study evaluated coproporphyrin I (CPI) as a selective endogenous biomarker of OATP1B-mediated drug-drug interactions (DDIs) relative to clinical probe rosuvastatin using nonlinear mixed-effect modeling."( Gaining Mechanistic Insight Into Coproporphyrin I as Endogenous Biomarker for OATP1B-Mediated Drug-Drug Interactions Using Population Pharmacokinetic Modeling and Simulation.
Barnett, S; Galetin, A; Humphreys, WG; Lai, Y; Ménochet, K; Ogungbenro, K; Shen, H, 2018
)
" We assessed three drug-drug interactions of avatrombopag as a victim with dual or selective CYP2C9/3A inhibitors and inducers."( Pharmacokinetic/pharmacodynamic drug-drug interactions of avatrombopag when coadministered with dual or selective CYP2C9 and CYP3A interacting drugs.
Aluri, J; Boyd, P; Chang, MK; Ferry, J; Lai, WG; Nomoto, M; Rege, B; Schuck, E; Siu, YA; Yasuda, S; Zamora, CA, 2018
)
"This study aimed to construct a physiologically based pharmacokinetic (PBPK) model of rifampicin that can accurately and quantitatively predict complex drug-drug interactions (DDIs) involving its saturable hepatic uptake and auto-induction."( Comprehensive PBPK Model of Rifampicin for Quantitative Prediction of Complex Drug-Drug Interactions: CYP3A/2C9 Induction and OATP Inhibition Effects.
Asaumi, R; Hashizume, K; Imawaka, H; Lee, W; Nunoya, KI; Sugiyama, Y; Tobe, Y; Toshimoto, K, 2018
)
" This study aimed to examine pharmacokinetic drug-drug interactions between this regimen and dolutegravir, a first-line antiretroviral medication."( Cytokine-Mediated Systemic Adverse Drug Reactions in a Drug-Drug Interaction Study of Dolutegravir With Once-Weekly Isoniazid and Rifapentine.
Alfaro, RM; Brooks, KM; De, P; Dobos, KM; George, JM; Hadigan, C; Kellogg, A; Kovacs, JA; Kumar, P; McLaughlin, M; McManus, M; Mehaffy, C; Pau, AK; Rupert, A, 2018
)
"This was a single-center, open-label, fixed-sequence, drug-drug interaction study in healthy volunteers."( Cytokine-Mediated Systemic Adverse Drug Reactions in a Drug-Drug Interaction Study of Dolutegravir With Once-Weekly Isoniazid and Rifapentine.
Alfaro, RM; Brooks, KM; De, P; Dobos, KM; George, JM; Hadigan, C; Kellogg, A; Kovacs, JA; Kumar, P; McLaughlin, M; McManus, M; Mehaffy, C; Pau, AK; Rupert, A, 2018
)
" A combination of in vitro data, clinical pharmacokinetic data, and drug-drug interaction (DDI) data of osimertinib in oncology patients were used to develop the physiologically based pharmacokinetic (PBPK) model and verify the DDI data of osimertinib."( Development, Verification, and Prediction of Osimertinib Drug-Drug Interactions Using PBPK Modeling Approach to Inform Drug Label.
Ballard, P; Pilla Reddy, V; Sharma, P; Vishwanathan, K; Walker, M, 2018
)
" This combination involves a pharmacokinetic drug-drug interaction leading to subtherapeutic drug concentrations of amiodarone and its active metabolite."( Amiodarone Rifampicin Drug-Drug Interaction Management With Therapeutic Drug Monitoring.
Demmer, A; Movig, KLL; Oude Munnink, TH; Slenter, RHJ, 2018
)
" Because it is a substrate of the cytochrome P450 system, specifically CYP3A4/5, ivacaftor is subject to significant drug-drug interactions, including due to commonly used antimicrobials such as rifampin."( Sensitivity of ivacaftor to drug-drug interactions with rifampin, a cytochrome P450 3A4 inducer.
Acosta, EP; Guimbellot, JS; Rowe, SM, 2018
)
" Our primary objectives were to: 1) refine the previously developed bosutinib PBPK model on the basis of the latest oral bioavailability data and 2) verify the refined PBPK model with P-glycoprotein kinetics on the basis of the bosutinib drug-drug interaction (DDI) results with ketoconazole and rifampin."( Application of Physiologically Based Pharmacokinetic Modeling in Understanding Bosutinib Drug-Drug Interactions: Importance of Intestinal P-Glycoprotein.
Costales, C; Kimoto, E; Loi, CM; Varma, MV; Yamazaki, S, 2018
)
"A robust UHPLC-MS/MS assay was developed and validated for CP-I and CP-III in plasma, and is currently applied to clinical studies to confirm suitability of Coproporphyrins as a potential substitute for drug-drug interaction study."( UHPLC-MS/MS bioanalysis of human plasma coproporphyrins as potential biomarkers for organic anion-transporting polypeptide-mediated drug interactions.
Burrrell, R; Easter, J; Kadiyala, P; Kandoussi, H; Lai, Y; Langish, R; Marathe, P; Mariannino, T; Paterson, P; Pillutla, R; Santockyte, R; Shah, K; Shen, H; Shipkova, P; Zeng, J; Zhang, Y, 2018
)
" Pharmacokinetic profiles in plasma and epithelial lining fluid (ELF) as well as the therapeutic efficacy of linezolid alone and in combination with rifampicin were investigated in a murine pneumonia model."( Increased activity of linezolid in combination with rifampicin in a murine pneumonia model due to MRSA.
Bu, MX; Li, L; Liao, XP; Liu, YH; Sun, J; Tao, MT; Xiong, YQ; Zhou, YF, 2018
)
" The aim of this study was to evaluate the anti-Mycobacterium tuberculosis activity of nine naphthoimidazoles, alone and combined with isoniazid (INH) and rifampicin (RIF)."( Anti-Mycobacterium tuberculosis activity of naphthoimidazoles combined with isoniazid and rifampicin.
Carvalho, TDSC; Corrêa Barros, LP; da Silva, PEA; de Moura, KCG; Del Rio, KP; Halicki, PCB; Pinto, MDCFR; Ramos, DF, 2018
)
" The 4200 patients who have been treated for hepatitis B combined with pulmonary TB in 8 different hospitals from Feb 2014 to Feb 2016 were selected as research objects."( Clinical effect of lamivudine in treating liver function lesion caused by hepatitis B combined with Anti-TB drugs.
Han, Y; Xia, S; Zhou, J, 2018
)
"Rifampin (RIF) plus clarithromycin (CLR) for 8 weeks is now the standard of care for Buruli ulcer (BU) treatment, but CLR may not be an ideal companion for rifamycins due to bidirectional drug-drug interactions."( Oxazolidinones Can Replace Clarithromycin in Combination with Rifampin in a Mouse Model of Buruli Ulcer.
Almeida, DV; Converse, PJ; Grosset, JH; Lee, J; Li, SY; Nuermberger, EL; Omansen, TF, 2019
)
" The aim of this study was to simulate and predict drug-drug interactions (DDIs) between these LA antiretroviral agents and rifampicin using physiologically based pharmacokinetic (PBPK) modeling."( Predicting Drug-Drug Interactions Between Rifampicin and Long-Acting Cabotegravir and Rilpivirine Using Physiologically Based Pharmacokinetic Modeling.
Back, D; Chiong, J; Curley, P; Flexner, C; Owen, A; Rajoli, RKR; Siccardi, M, 2019
)
" We enrolled eligible adults (>18 years) with pulmonary multidrug-resistant tuberculosis to receive, in combination with an optimised background regimen developed according to WHO and national guidelines, either oral delamanid (100 mg twice daily) for 2 months followed by 200 mg once daily for 4 months or placebo (same regimen)."( Efficacy and safety of delamanid in combination with an optimised background regimen for treatment of multidrug-resistant tuberculosis: a multicentre, randomised, double-blind, placebo-controlled, parallel group phase 3 trial.
Balanag, V; Bielskiene, V; Cadena, E; Caoili, J; Cirule, A; Danilovits, M; Davidaviciene, E; Domente, L; Geiter, LJ; Gupta, R; Hafkin, J; Hittel, N; Lizarbe, V; Patientia, R; Petersen, C; Sanchez, E; Segura, P; Staples, S; Ticona, E; Variava, E; von Groote-Bidlingmaier, F; Wells, C; Yu, C, 2019
)
" Four concentrations of fresh pomegranate juice (FPJ) (5%, 10%, 15%, and 20%) were evaluated in combination with R and INH at a dose range of (1."( Evaluation of Polyphenolic Profile and Antibacterial Activity of Pomegranate Juice in Combination with Rifampin (R) against MDR-TB Clinical Isolates.
AlMatar, M; Eker, E; Kafkas, E; Kayar, B; Köksal, F; Var, I; Zarifikhosroshahi, M, 2019
)
"This study aimed to explore daptomycin combined with fosfomycin or rifampin against the planktonic and adherent linezolid-resistant isolates of Enterococcus faecalis."( In vitro activities of daptomycin combined with fosfomycin or rifampin on planktonic and adherent linezolid-resistant isolates of Enterococcus faecalis.
Chen, Z; Deng, QW; Jiang, SB; Lin, ZW; Qi, GB; Qu, D; Sun, X; Tu, HP; Wu, Y; Yu, ZJ; Zheng, JX, 2019
)
" Potential drug-drug interactions (DDIs) following coadministration of these 2 overactive bladder treatments were estimated using physiologically based pharmacokinetic models, developed and verified by comparing predicted and observed pharmacokinetic profiles from clinical studies."( Physiologically Based Pharmacokinetic Modeling Suggests Limited Drug-Drug Interaction for Fesoterodine When Coadministered With Mirabegron.
Goosen, TC; Lin, J; Malhotra, B; Tse, S; Yamagami, H, 2019
)
"We predicted the drug-drug interaction (DDI) potential of siponimod in presence of cytochrome P450 (CYP)2C9/CYP3A4 inhibitors/inducers in subjects with different CYP2C9 genotypes by physiologically-based pharmacokinetic (PK) modeling."( Prediction of the Impact of Cytochrome P450 2C9 Genotypes on the Drug-Drug Interaction Potential of Siponimod With Physiologically-Based Pharmacokinetic Modeling: A Comprehensive Approach for Drug Label Recommendations.
Gardin, A; He, H; Huth, F; Umehara, K, 2019
)
" Accordingly, the drug-drug interaction (DDI) potential of darolutamide was investigated in both nonclinical and clinical studies."( Drug-Drug Interaction Potential of Darolutamide: In Vitro and Clinical Studies.
Bairlein, M; Denner, K; Fricke, R; Gieschen, H; Graudenz, K; Korjamo, T; Koskinen, M; Prien, O; von Bühler, CJ; Wilkinson, G; Zurth, C, 2019
)
"Open-label Phase 2 drug-drug interaction randomized trial."( Effect of high-dose rifampicin on efavirenz pharmacokinetics: drug-drug interaction randomized trial.
Atwine, D; Barrail-Tran, A; Baudin, E; Bonnet, M; Furlan, V; Gelé, T; K T Nanjebe, D; Kananura, K; Kyohairwe, R; Muyindike, W; Mworozi, K; Nyehangane, D; Orikiriza, P; Taburet, AM; Verstuyft, C, 2020
)
" In this work, we developed a translational approach which can allow for forward translation to predict efficacy of drug combination in EBA studies using the Multistate Tuberculosis Pharmacometric (MTP) and the General Pharmacodynamic Interaction (GPDI) models informed by in vitro static time-kill data."( Translational Model-Informed Approach for Selection of Tuberculosis Drug Combination Regimens in Early Clinical Development.
Coates, ARM; Hu, Y; Simonsson, USH; Susanto, BO; Wicha, SG, 2020
)
" Despite the extensive clinical use of bortezomib, the mechanism of the complex time-dependent pharmacokinetics of bortezomib has not been fully investigated in context of its pharmacodynamics (PD) and drug-drug interaction (DDI) profiles."( A Translational Physiologically Based Pharmacokinetics/Pharmacodynamics Framework of Target-Mediated Disposition, Target Inhibition and Drug-Drug Interactions of Bortezomib.
Hanley, M; Iwasaki, S; Venkatakrishnan, K; Xia, C; Zhu, A, 2020
)
"53 mg/kg combined with MEM 8 g using a 3-hr prolonged infusion every 8 hr and RIF 600 mg every 24 hr resulted in bacterial counts below the quantitative limit within 24 hr and remained undetectable throughout the 10-day experiment."( In pursuit of the triple crown: mechanism-based pharmacodynamic modelling for the optimization of three-drug combinations against KPC-producing Klebsiella pneumoniae.
Bulitta, JB; Bulman, ZP; Forrest, A; Holden, PN; Li, J; Nation, RL; Onufrak, NJ; Satlin, MJ; Smith, NM; Tan, X; Tsuji, BT, 2020
)
"Ribociclib is approved in combination with endocrine therapy as initial endocrine-based therapy for HR-positive and HER2-negative advanced breast cancer."( Ribociclib Drug-Drug Interactions: Clinical Evaluations and Physiologically-Based Pharmacokinetic Modeling to Guide Drug Labeling.
Chakraborty, A; Dhuria, SV; Elmeliegy, M; He, H; Heimbach, T; Huth, F; Ji, Y; Miller, M; Samant, TS; Schiller, H; Umehara, K, 2020
)
"Age-related comorbidities and consequently polypharmacy are highly prevalent in the elderly, resulting in an increased risk for drug-drug interactions (DDIs)."( Clinical Data Combined With Modeling and Simulation Indicate Unchanged Drug-Drug Interaction Magnitudes in the Elderly.
Battegay, M; Courlet, P; Decosterd, LA; Kinvig, H; Marzolini, C; Penny, MA; Siccardi, M; Stader, F, 2021
)
" In addition, AA-INH was combined with a RIF-carboxymethylcellulose very fast release complex (CMC-RIF) obtained previously and subjected to acid dissolution assays to evaluate RIF acid stability and determine RIF and INH dissolution efficiencies."( Anti-tuberculosis site-specific oral delivery system that enhances rifampicin bioavailability in a fixed-dose combination with isoniazid.
Litterio, NJ; Lorenzutti, AM; Luciani-Giacobbe, LC; Olivera, ME; Ramírez-Rigo, MV, 2021
)
" Consequently, the potential of iberdomide as a victim of drug-drug interactions (DDI) was evaluated in a clinical study with healthy subjects."( Evaluation of iberdomide and cytochrome p450 drug-drug interaction potential in vitro and in a phase 1 study in healthy subjects.
Atsriku, C; Gaudy, A; Liu, L; MacGorman, K; Palmisano, M; Surapaneni, S; Xue, Y; Ye, Y, 2021
)
"6 mg) and when administered with the CYP3A and P-gp inhibitor itraconazole (200 mg twice daily on day 1 and 200 once daily on days 2 through 9)."( Evaluation of iberdomide and cytochrome p450 drug-drug interaction potential in vitro and in a phase 1 study in healthy subjects.
Atsriku, C; Gaudy, A; Liu, L; MacGorman, K; Palmisano, M; Surapaneni, S; Xue, Y; Ye, Y, 2021
)
"Develop a physiologically based pharmacokinetic (PBPK) model of ivosidenib using in vitro and clinical PK data from healthy participants (HPs), refine it with clinical data on ivosidenib co-administered with itraconazole, and develop a model for patients with acute myeloid leukemia (AML) and apply it to predict ivosidenib drug-drug interactions (DDI)."( Physiologically based pharmacokinetic modeling and simulation to predict drug-drug interactions of ivosidenib with CYP3A perpetrators in patients with acute myeloid leukemia.
Fan, B; Ke, A; Le, K; Prakash, C; Yang, H, 2020
)
"The aim of this review is to summarize the pharmacokinetic drug-drug interaction (DDI) of 45 antibiotics commonly used in sepsis care in China."( Pharmacokinetic Drug-drug Interaction of Antibiotics Used in Sepsis Care in China.
Cheng, C; Chu, Z; He, R; Li, J; Wang, Y; Yu, X, 2021
)
" The models were verified with observed clinical drug-drug interactions with CYP3A and P-gp inhibitors."( Physiologically-Based Pharmacokinetic Modeling for the Prediction of a Drug-Drug Interaction of Combined Effects on P-glycoprotein and Cytochrome P450 3A.
Bonate, PL; Choules, MP; Komatsu, K; Otsuka, Y, 2020
)
" Here, we developed a PBPK model of PMF to capture drug-drug interactions (DDI) incurred by cyclosporine (CsA) and rifampicin (RIF), the two OATP1B inhibitors."( Improved Prediction of the Drug-Drug Interactions of Pemafibrate Caused by Cyclosporine A and Rifampicin via PBPK Modeling: Consideration of the Albumin-Mediated Hepatic Uptake of Pemafibrate and Inhibition Constants With Preincubation Against OATP1B.
Lee, W; Morita, S; Park, JE; Sahi, J; Shitara, Y; Sugiyama, Y; Toshimoto, K, 2021
)
" For the first time, we developed a physiologically based pharmacokinetic (PBPK) model-based approach to assess CYP3A-mediated drug-drug interaction (DDI) risk for polatuzumab vedotin (Polivy), an anti-CD79b-vc-monomethyl auristatin E (MMAE) antibody-drug conjugate (ADC)."( Physiologically Based Pharmacokinetic Model-Informed Drug Development for Polatuzumab Vedotin: Label for Drug-Drug Interactions Without Dedicated Clinical Trials.
Chen, Y; Ding, H; Girish, S; Jin, J; Li, C; Lu, D; Ma, F; Mao, J; Miles, D; Samineni, D; Shi, R; Wright, M, 2020
)
" Due to its widespread use and CYP3A4-mediated metabolism, there is concern regarding drug-drug interactions (DDIs), particularly a suboptimal LNG exposure when co-administered with CYP3A4 inducers, potentially leading to unintended pregnancies."( Quantitative Assessment of Levonorgestrel Binding Partner Interplay and Drug-Drug Interactions Using Physiologically Based Pharmacokinetic Modeling.
Chaturvedula, A; Cicali, B; Cristofoletti, R; Hoechel, J; Lingineni, K; Schmidt, S; Vozmediano, V; Wendl, T; Wiesinger, H, 2021
)
"To provide whole-body physiologically based pharmacokinetic (PBPK) models of the potent clinical organic anion transporter (OAT) inhibitor probenecid and the clinical OAT victim drug furosemide for their application in transporter-based drug-drug interaction (DDI) modeling."( Physiologically Based Pharmacokinetic Models of Probenecid and Furosemide to Predict Transporter Mediated Drug-Drug Interactions.
Britz, H; Fernandez, É; Hanke, N; Lehr, T; Nock, V; Prasad, B; Stopfer, P; Taub, ME; Wang, T, 2020
)
" The patient started with a febrile headache that progressed to impaired consciousness after 20 days, and she finally died after treatment with vancomycin combined with rifampicin."( A case report of the differential diagnosis of Cellulosimicrobium cellulans-infected endocarditis combined with intracranial infection by conventional blood culture and second-generation sequencing.
He, C; Tian, R; Wang, R; Zhang, H, 2020
)
" Physiologically based pharmacokinetic models built upon two independent bottom-up approaches predicted elevation of E7766 plasma exposure when administered with Rifampicin, a clinical OATP inhibitor."( Prediction of Transporter-Mediated Drug-Drug Interactions and Phenotyping of Hepatobiliary Transporters Involved in the Clearance of E7766, a Novel Macrocycle-Bridged Dinucleotide.
Burgess, L; Dixit, V; Hart, A; Jiang, R; Kim, DS; Lai, WG, 2021
)
"We employed an in vitro pharmacokinetic model to study the pharmacodynamics of minocycline alone and in combination with rifampicin."( The pharmacodynamics of minocycline alone and in combination with rifampicin against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
Attwood, M; Bowker, KE; MacGowan, AP; Noel, AR, 2021
)
"An exposure-ranging design was used to establish fAUC/MIC targets for static, -1 log drop and -2 log drop effects against Staphylococcus aureus for minocycline and in combination with rifampicin."( The pharmacodynamics of minocycline alone and in combination with rifampicin against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
Attwood, M; Bowker, KE; MacGowan, AP; Noel, AR, 2021
)
" As medroxyprogesterone acetate is a cytochrome P450 (CYP3A4) substrate, drug-drug interactions (DDIs) with antiretroviral or antituberculosis treatment may lead to subtherapeutic medroxyprogesterone acetate concentrations (< 0."( A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug-Drug Interactions With Antiretroviral and Antituberculosis Treatment.
Cohn, SE; Denti, P; Dooley, KE; Firnhaber, C; Francis, J; Godfrey, C; Kendall, MA; McIlleron, H; Mngqibisa, R; Wu, X, 2021
)
" This model was built based on physiochemical data and clinical in vivo drug-drug interaction (DDI) studies with itraconazole and fluconazole, and verified against data from an in vivo rifampicin DDI study and an absolute bioavailability study."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
" Drug-drug interactions (DDI) caused by rifampicin (RIF) are a major issue."( Model-Based Comparative Analysis of Rifampicin and Rifabutin Drug-Drug Interaction Profile.
Bleyzac, N; Bourguignon, L; France, M; Garreau, R; Goutelle, S; Tod, M; Tuloup, V, 2021
)
"We investigated savolitinib pharmacokinetics (PK) when administered alone or in combination with rifampicin, itraconazole or famotidine, and investigated midazolam PK when administered with or without savolitinib in healthy males."( Clinical evaluation of the potential drug-drug interactions of savolitinib: Interaction with rifampicin, itraconazole, famotidine or midazolam.
Burke, W; Cantarini, M; Frewer, P; Goldwater, R; Han, D; Hara, I; Li, Y; Ren, S; Scarfe, G; Schalkwijk, S; Vishwanathan, K, 2022
)
"The aim of this study was to simulate the drug-drug interaction (DDI) between ritonavir-boosted atazanavir (ATV/r) and rifampicin (RIF) using physiologically based pharmacokinetic (PBPK) modelling, and to predict suitable dose adjustments for ATV/r for the treatment of people living with HIV (PLWH) co-infected with tuberculosis."( Predicting Drug-Drug Interactions between Rifampicin and Ritonavir-Boosted Atazanavir Using PBPK Modelling.
Bunglawala, F; Cottura, N; Denti, P; Fabrega, F; Howarth, A; Kinvig, H; Lloyd, A; Montanha, MC; Siccardi, M; Waitt, C, 2022
)
"When RFP is combined with CAM in the treatment of pulmonary MAC infection, the blood concentration of CAM significantly decreased and that of the active metabolite 14-OH CAM increased, but not significantly."( Impact of rifampicin on the pharmacokinetics of clarithromycin and 14-hydroxy clarithromycin in patients with multidrug combination therapy for pulmonary Mycobacterium avium complex infection.
Enoki, Y; Hasegawa, N; Iketani, O; Kizu, J; Komeya, A; Matsumoto, K; Taguchi, K; Uno, S; Uwamino, Y, 2022
)
" In this study, we aimed to explore the antibiofilm activity of melittin, either alone or in combination with vancomycin and rifampin, against biofilm-producing MRSE strains."( Prevention, inhibition, and degradation effects of melittin alone and in combination with vancomycin and rifampin against strong biofilm producer strains of methicillin-resistant Staphylococcus epidermidis.
Alikhani, MY; Arciola, CR; Bagheri, KP; Mirzaei, R; Sedighi, I; Yousefimashouf, R, 2022
)
" The 29 studies identified examined warfarin (n = 17), direct oral anticoagulants (DOACs) (n = 8), and antiplatelet agents (n = 4) combined with rifampin (n = 28) or rifabutin (n = 1)."( Systematic review of drug-drug interactions between rifamycins and anticoagulant and antiplatelet agents and considerations for management.
Canonica, T; Keh, C; Louie, J; MacDougall, C; P Phan, BA, 2022
)
" As such, this 2-part clinical drug-drug interaction study was conducted to assess the effect of itraconazole (a strong CYP3A4 inhibitor), rifampicin (a strong CYP3A4 inducer), rabeprazole, and omeprazole (both proton pump inhibitors) on the pharmacokinetics of belumosudil."( A Phase 1 Pharmacokinetic Drug Interaction Study of Belumosudil Coadministered With CYP3A4 Inhibitors and Inducers and Proton Pump Inhibitors.
Alabanza, A; Lohmer, L; Patel, J; Schueller, O; Singh, N; Willson, A, 2022
)
" Clofazimine (CFZ) has showed benefit in shortening DS-TB treatment in vivo from six to four months when used in combination with this regimen in murine models of experimental infection."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
"In the current in vitro study, the inhibitory and bactericidal activities of CFZ in combination with the primary anti-TB drugs, RMP, INH and EMB against the AR and SR organisms in planktonic and biofilm-forming cultures, respectively, were evaluated by fractional inhibitory concentration index (FICI) and fractional bactericidal concentration index (FBCI) determinations, using the Loewe Additivity Model."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
"In planktonic cultures, CFZ demonstrated synergistic growth inhibitory activity in combination with RMP and INH individually and collectively."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
"Clofazimine exhibited synergistic effects in combination with primary anti-TB drugs against both planktonic and biofilm-forming cultures, showing potential benefit in augmenting treatment outcome when used during standard TB chemotherapy."( Assessment of the efficacy of clofazimine alone and in combination with primary agents against Mycobacterium tuberculosis in vitro.
Anderson, R; Cholo, MC; Mashele, SA; Matjokotja, MT; Rasehlo, SSM; Steel, HC, 2022
)
"Although rifampin drug-drug interaction (DDI) studies are routinely conducted, there have been instances of liver function test (LFT) elevations, warranting further evaluation."( A literature review of liver function test elevations in rifampin drug-drug interaction studies.
Chen, J; Ibrahim, SM; Pithavala, YK; Vourvahis, M, 2022
)
" This study aimed to establish a physiologically based pharmacokinetic (PBPK) model of rifampicin to predict the P-gp-mediated drug-drug interactions (DDIs) and assess the DDI impact in the intestine, liver, and kidney."( Robust physiologically based pharmacokinetic model of rifampicin for predicting drug-drug interactions via P-glycoprotein induction and inhibition in the intestine, liver, and kidney.
Asaumi, R; Nunoya, KI; Sugiyama, Y; Taskar, KS; Yamaura, Y, 2022
)
"Clinical development of new drugs may require dedicated drug-drug interaction (DDI) studies, such as to evaluate the effect of cytochrome P450 3A induction on the pharmacokinetics of investigational drugs."( Rifampin Drug-Drug-Interaction Studies: Reflections on the Nitrosamine Impurities Issue.
Benrimoh, N; Garvin, C; Paglialunga, S; Smith, S; van Haarst, A, 2023
)
" Hence, their metabolic stability and potential involvement in relevant drug-drug interactions (DDI) are of great clinical interest, being HepaRG cells herein used as an in vitro human model."( Study of the metabolic stability profiles of perampanel, rufinamide and stiripentol and prediction of drug interactions using HepaRG cells as an in vitro human model.
Alves, G; Falcão, A; Fortuna, A; Meirinho, S; Rodrigues, M, 2022
)
"Evaluation of the organic anion transporting polypeptide (OATP) 1B-mediated drug-drug interaction (DDI) potential is important for drug development."( Quantitative prediction of OATP1B-mediated drug-drug interactions using endogenous biomarker coproporphyrin I.
Bessho, K; Shigemi, R; Takubo, H; Watari, R, 2022
)
" Hence, rifampicin is used extensively in clinical studies to assess drug-drug interactions (DDIs)."( Alternatives to rifampicin: A review and perspectives on the choice of strong CYP3A inducers for clinical drug-drug interaction studies.
Bolleddula, J; Dong, J; Gopalakrishnan, S; Hu, P; Venkatakrishnan, K, 2022
)
" Here, we investigate the pharmacokinetic drug-drug interaction potential of trilaciclib."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
"Overall, the drug-drug interaction and safety profiles of trilaciclib in these studies support its continued use in patients with extensive-stage small-cell lung cancer."( Pharmacokinetic Drug-Drug Interaction Studies Between Trilaciclib and Midazolam, Metformin, Rifampin, Itraconazole, and Topotecan in Healthy Volunteers and Patients with Extensive-Stage Small-Cell Lung Cancer.
Beelen, A; Curd, L; Goti, V; Horton, JK; Li, C; Sale, M; Tao, W, 2022
)
" Understanding potential drug-drug interactions (DDIs) informs proper dosing when co-administering tucatinib with other therapies."( Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers.
Abdulrasool, LI; Endres, CJ; Lee, A; Mayor, JG; Rustia, EL; Sun, H; Topletz-Erickson, A; Walker, L, 2022
)
" Here, we report the results from 2 drug-drug interaction studies."( Drug-Drug Interaction Studies to Evaluate the Effect of Inhibition of UGT1A1 and CYP3A4 and Induction of CYP3A4 on the Pharmacokinetics of Tropifexor in Healthy Subjects.
Chen, J; Gu, J; Hackling, M; Prince, W; Shah, B; Stringer, R; Woessner, R; Zhang, Y, 2022
)
"This study aimed to investigate the drug-drug interactions of ponatinib with strong, moderate, or weak CYP3A4 inhibitors/inducers by developing physiologically based pharmacokinetic (PBPK) models."( Physiologically based pharmacokinetic modeling of ponatinib to describe drug-drug interactions in patients with cancer.
Hanada, K; Morita, TO, 2022
)
" It also reasonably predicted its pharmacokinetics when combined with ketoconazole and rifampicin."( Physiologically based pharmacokinetic modeling of ponatinib to describe drug-drug interactions in patients with cancer.
Hanada, K; Morita, TO, 2022
)
"The PBPK model predicted a significant drug interaction when ponatinib was combined with a strong CYP3A4 inducer."( Physiologically based pharmacokinetic modeling of ponatinib to describe drug-drug interactions in patients with cancer.
Hanada, K; Morita, TO, 2022
)
" This study demonstrated for the first time that fosfomycin (FOS) combined with rifampin (RIF) showed strong synergistic effects against CRPA and carbapenem-susceptible PA, with 100% synergistic rates."( Antibacterial and antibiofilm activities of fosfomycin combined with rifampin against carbapenem-resistant Pseudomonas aeruginosa.
Li, M; Liu, Y; Ma, W; Sun, L; Sun, S; Wu, J; Zhao, W, 2022
)
" The delay in the lag phase of growth curve observed when used in combination with AlEW, especially at 50 MPa or less, and was prolonged by about 4 to 6 hours."( Effect of High Hydrostatic Pressure Treatment Combined with Alkaline Electrolyzed Water on the Injury and Growth Characteristics of Bacterial Spores.
Hamanaka, D; Morita, K, 2022
)
"Long-acting (LA) intramuscular cabotegravir and rilpivirine are prone to drug-drug interactions (DDI)."( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
" Cabotegravir and rilpivirine were given alone and in combination with rifampicin or rifabutin."( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
"The US Food and Drug Administration (FDA) guidance has recommended several model-based predictions to determine potential drug-drug interactions (DDIs) mediated by cytochrome P450 (CYP) induction."( Beyond the Michaelis-Menten: Accurate Prediction of Drug Interactions Through Cytochrome P450 3A4 Induction.
Chae, JW; Kim, JK; Kim, SK; Song, YM; Tran, QT; Vu, NT; Yun, HY, 2023
)
"Quantitative prediction of the potential for drug-drug interaction (DDI) is essential to guarantee the safety and efficacy of drugs."( [Development of Prediction Methods for Drug-Drug Interactions Based on the Construction of Physiologically Based Pharmacokinetic Models for Hepatic OATP Substrate Drugs and Endogenous Substrates].
Yoshikado, T, 2023
)
"To determine if double-dose levonorgestrel emergency contraception (EC) in combination with efavirenz or rifampicin, 2 drugs known to decrease levonorgestrel exposure, resulted in similar pharmacokinetics compared to standard-dose levonorgestrel EC without drug-drug interactions."( Pharmacokinetics of dose-adjusted levonorgestrel emergency contraception combined with efavirenz-based antiretroviral therapy or rifampicin-containing tuberculosis regimens.
Badal-Faesen, S; Barr, E; Belaunzaran-Zamudio, PF; Cohn, SE; Gadama, L; Gatechompol, S; Godfrey, C; Jalil, EM; Mawlana, S; Mngqibisa, R; Olefsky, M; Pham, M; Podany, AT; Scarsi, KK; Smeaton, LM; Supparatpinyo, K; Woolley, E, 2023
)
" Based on nonclinical in vitro characterization of gepotidacin metabolism, two phase I studies were conducted in healthy participants to investigate clinical drug-drug interactions (DDIs)."( Clinical assessment of gepotidacin (GSK2140944) as a victim and perpetrator of drug-drug interactions via CYP3A metabolism and transporters.
Barth, A; Brimhall, DB; Dumont, EF; Nguyen, D; Perry, CR; Shabbir, S; Srinivasan, M; Swift, B; Thomas, S; Zamek-Gliszczynski, MJ, 2023
)
" Then, the effect of renal impairment combined with drug-drug interaction on saxagliptin and 5-hydroxy saxagliptin pharmacokinetics was investigated."( Physiologically Based Pharmacokinetic Modeling Characterizes the Drug-Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment.
Ke, M; Lin, C; Lin, R; Wu, W; Ye, L, 2023
)
" Our objective was to evaluate potential drug-drug interactions of cilofexor as a victim and as a perpetrator."( Evaluation of the Potential for Cytochrome P450 and Transporter-Mediated Drug-Drug Interactions for Cilofexor, a Selective Nonsteroidal Farnesoid X Receptor (FXR) Agonist.
Kirby, BJ; Nelson, C; Othman, AA; Shen, G; Watkins, TR; Weber, E; Xiao, D; Younis, I, 2023
)
"In this Phase 1 study, healthy adult participants (n = 18-24 per each of the 6 cohorts) were administered cilofexor in combination with either perpetrators or substrates of cytochrome P-450 (CYP) enzymes and drug transporters."( Evaluation of the Potential for Cytochrome P450 and Transporter-Mediated Drug-Drug Interactions for Cilofexor, a Selective Nonsteroidal Farnesoid X Receptor (FXR) Agonist.
Kirby, BJ; Nelson, C; Othman, AA; Shen, G; Watkins, TR; Weber, E; Xiao, D; Younis, I, 2023
)
" A limited fraction of potential drug-drug interactions (DDIs) have been or can ethically be studied in clinical trials, leaving the vast majority unexplored."( General Framework to Quantitatively Predict Pharmacokinetic Induction Drug-Drug Interactions Using In Vitro Data.
Akpan, A; Bearon, R; Grañana-Castillo, S; Hodge, D; Khoo, S; Pham, T; Siccardi, M; Williams, A, 2023
)
" Considering the possibility of combination therapy in patients with NSCLC, we investigated the drug-drug interaction (DDI) potential of SH-1028 both in vitro and in clinical trials."( Drug-drug interaction potential of SH-1028, a third-generation EGFR-TKI: in vitro and clinical trials.
Ding, J; Ding, Y; He, C; Li, X; Liu, B; Liu, Y; Shan, R; Wang, Y; Wang, Z; Xie, J; Xu, Y; Zhou, H; Zhu, M, 2023
)
" Phase I studies investigated the drug-drug interactions of futibatinib with itraconazole (a dual P-gp and strong CYP3A inhibitor), rifampin (a dual P-gp and strong CYP3A inducer), or midazolam (a sensitive CYP3A substrate) in healthy adult participants."( Evaluation of the Cytochrome P450 3A and P-glycoprotein Drug-Drug Interaction Potential of Futibatinib.
Benhadji, KA; Gao, L; He, Y; Hunt, A; Mina, M; Sonnichsen, D; Takenaka, T; Yamamiya, I, 2023
)
" Previous drug-drug interaction (DDI) studies have demonstrated that co-administration of zanubrutinib with rifampin, a strong CYP3A inducer, reduces zanubrutinib plasma concentrations, potentially impacting activity."( A Phase 1, Open-Label, Fixed-Sequence, Drug-Drug Interaction Study of Zanubrutinib with Rifabutin in Healthy Volunteers.
Cohen, A; Conto, S; Ou, YC; Sahasranaman, S; Tariq, B, 2023
)
"The predictive performance of the PBPK model to simulate dolutegravir and raltegravir pharmacokinetics and to reproduce the strength of induction was verified using clinical drug-drug interaction studies (steady-state induction) and switch studies (residual induction)."( Management of Drug Interactions with Inducers: Onset and Disappearance of Induction on Cytochrome P450 3A4 and Uridine Diphosphate Glucuronosyltransferase 1A1 Substrates.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
"Compared to rifampicin (600 mg/day), standard doses of rifabutin (300 mg/day) have a lower risk of drug-drug interactions due to induction of cytochrome P450 3A4 (CYP3A4) or P-glycoprotein (Pgp/ABCB1) mediated by the pregnane X receptor (PXR)."( Comprehensive in vitro analysis evaluating the variable drug-drug interaction risk of rifampicin compared to rifabutin.
Haefeli, WE; Nilles, J; Ruez, S; Sauter, M; Theile, D; Weiss, J, 2023
)
" Clinical pharmacokinetic drug-drug interaction (DDI) of ocedurenone with CYP3A inhibitor and inducer were investigated in healthy volunteers."( Pharmacokinetics and Drug-Drug Interaction of Ocedurenone (KBP-5074) in vitro and in vivo.
Liu, J; McCabe, J; Tan, X; Wang, P; Yang, F; Zhang, J, 2023
)
" ROC curve analysis showed that Xpert MTB/RIF combined with TBseq Ultra showed the highest area under the curve (0."( Value analysis of next-generation sequencing combined with Xpert in early precise diagnosis of pulmonary tuberculosis.
Chen, Y; Fei, F; Lang, Y; Qin, Y; Wang, P; Zhou, L; Zhu, Y; Zou, X, 2023
)
" However, there is little data regarding the impact of this drug-drug Interaction in PLWH, which makes health care providers reluctant to prescribe them together."( The clinical impact of rifampicin-based anti-TB therapy and tenofovir alafenamide-containing ARV regimen drug Interaction in people living with HIV: Case series report.
Alamer, A; Almulhim, A; Alrashed, A; Alwafai, S; Cahusac, P; Damfu, N; Mohzari, YA; Musawa, MA; Zaeri, B, 2023
)
" The objective of this study was to report the clinical impact of this drug-drug interaction (rifampicin + TAF-containing antiretroviral (ARV) regimen) on HIV viral load control in PLWH."( The clinical impact of rifampicin-based anti-TB therapy and tenofovir alafenamide-containing ARV regimen drug Interaction in people living with HIV: Case series report.
Alamer, A; Almulhim, A; Alrashed, A; Alwafai, S; Cahusac, P; Damfu, N; Mohzari, YA; Musawa, MA; Zaeri, B, 2023
)

Bioavailability

Rifaximin is a rifamycin analogue with a broad spectrum of activity similar to that of rifampin. Because it is poorly absorbed in the gastrointestinal tract, the focus of its development has been on intestinal infections and diseases.

ExcerptReference
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
" A kinetic model study on the transfer constants between various body compartments has indicated that rifampicin is rapidly absorbed from the intestine and that the absorption rate increases with time."( Clinical pharmacokinetics of rifampicin.
Acocella, G,
)
" The renal elimination of apparent rifampicin can be used as a parameter for assessment of relative bioavailability of rifampicin from oral dosage forms of the same nominal strength if an appropriate number of volunteers is involved in the test."( The renal elimination of rifampicin as a function of the oral dose. A convenient way to assess relative bioavailability.
Brechbühler, S; Fluehler, H; Riess, W; Theobald, W, 1978
)
" The studies on the pharmacokinetics of rifampicin showed that the drug was well absorbed from the gastro-intestinal tract."( [Pharmacokinetics of rifampicin in single and repeated administration to patients with inflammatory processes in the lungs of nontuberculotic etiology].
Kopeiko, IP; Makarenkova, RV, 1977
)
"The bioavailability of rifampicin and isoniazid from formulations containing these drugs in combination has been compared to that from formulations containing either drug alone."( Serum concentrations and bioavailability of rifampicin and isoniazid in combination.
Chasseaud, LF; Garnham, JC; Taylor, T; Turner, P, 1976
)
"The bioavailability (plasma concentrations, AUC and urinary excretion) of an oral solution of rifampicin was investigated in six healthy volunteers."( Mechanism of the inhibitory effect of PAS granules on the absorption of rifampicin: adsorption of rifampicin by an excipient, bentonite.
Boman, G; Lundgren, P; Stjernström, G, 1975
)
" Thus, it easily enters the systemic blood flow, resulting in almost complete bioavailability (75-100%)."( Pharmacokinetic profile of nicorandil in humans: an overview.
Frydman, A, 1992
)
" The absorption rate constant was found to be lower and the time to reach peak concentration was longer after drug administration at 24."( Chronopharmacokinetics of rifampicin.
Avachat, MK; Rambhau, D; Rao, BR; Rao, JV; Rao, VV, 1992
)
" Rifampin not only induces the hepatic metabolism of cyclosporine but also decreases its bioavailability to a greater extent than would be predicted by the increased metabolism."( Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction.
Benet, LZ; Hebert, MF; Prueksaritanont, T; Roberts, JP, 1992
)
"Due to the unstable nature of rifampicin, a rapid automated high-performance liquid chromatographic method had to be developed for the analysis of a large number of plasma samples generated during a bioavailability trial."( Automated high-performance liquid chromatographic method for the determination of rifampicin in plasma.
Papgis, M; Swart, KJ, 1992
)
"25 mg/kg RPE, suggesting that FCE would be a better drug than RPE if its bioavailability could be improved, and that the levels following 16 mg/kg RPE were similar to those found in man after 8 mg/kg RPE taken with a fat-rich meal, suggesting good prospects for effective once-fortnightly human treatment."( Activity of two long-acting rifamycins, rifapentine and FCE 22807, in experimental murine tuberculosis.
Dhillon, J; Dickinson, JM; Guy, JA; Mitchison, DA; Ng, TK, 1992
)
" Serial plasma samples taken under controlled conditions suggested that a decreased rate of absorption was responsible for low one-hour concentrations in one of the subjects."( Ciprofloxacin in patients with mycobacterial infections: experience in 15 patients.
Kahana, LM; Spino, M, 1991
)
"Pharmacokinetics and bioavailability of rifampin in adult sheep were investigated by use of high-performance liquid chromatography for determination of serum concentrations."( Pharmacokinetics of rifampin in adult sheep.
Jernigan, AD; Rings, DM; Sams, RA; St Jean, GD, 1991
)
"Oral contraceptive steroids (OCS) are well absorbed from the gastrointestinal tract in humans."( Oral contraceptive steroids--pharmacological issues of interest to the prescribing physician.
Back, DJ; Orme, M, 1991
)
" The investigations--in most cases estimations of the nonbiotransformated part of antituberculotic drugs and theophylline had following purposes: security of the necessary dose especially in the case of INH (hereditary INH-polymorphismus), proof of a sufficient permeation of INH and RMP in the tuberculous kidney, control of the usefulness or uselessness of the INH-depot-preparations, relations between the concentration in the serum and dose respectively of the appearance of side effects, estimation of bioavailability and pharmacokinetic parameters during the development of an useful retard-preparation of theophylline."( [Clinical pharmacology in optimization of therapy of lung diseases].
Iwainsky, H; Wiesner, B; Winsel, K, 1991
)
"A comparative bioavailability study was undertaken between a new formulation of rifampicin 'Famcin' and a standard formulation of rifampicin 'R-cin' in eight healthy male volunteers at two dose levels: 300 mg and 450 mg given orally under both single dose and steady state conditions."( Comparative bioavailability and in-vitro antimicrobial activity of two different brands of rifampicin.
Chakrabarti, A; Garg, SK; Kumar, N; Panigrahi, D; Sharma, M; Sharma, PL; Talwar, P,
)
"In a pilot study involving 62 patients with open pulmonary tuberculosis, we established that slow acetyators and patients receiving intravenous rifampicin treatment showed a tendency towards a more rapid negativisation of the sputum culture than did fast acetyators (lower levels of isoniazid) or patients receiving oral rifampicin therapy (decreasing bioavailability of the rifampicin during treatment)."( [Significance of the acetylator phenotype and initial oral/intravenous rifampicin administration in the treatment of tuberculosis].
Loos, U; Musch, E; Schwabe, HK, 1990
)
" The resultant decreased bioavailability of cyclosporine may precipitate graft rejection."( Interactions of cyclosporine with antimicrobial agents.
Brown, RB; Sands, M,
)
" Among the drugs that can decrease digoxin bioavailability are cholestyramine, antacid gels, kaolin-pectate, certain antimicrobial drugs and cancer chemotherapeutic agents."( Pharmacokinetic interactions between digoxin and other drugs.
Marcus, FI, 1985
)
"A comparative bioavailability study of the antituberculosis drugs isoniazid, rifampin, and pyrazinamide was carried out in a group of 10 healthy volunteers after administration of the three compounds, once in individual association and once in a combined, fixed preparation."( Comparative bioavailability of isoniazid, rifampin, and pyrazinamide administered in free combination and in a fixed triple formulation designed for daily use in antituberculosis chemotherapy. I. Single-dose study.
Acocella, G; Gialdroni-Grassi, G; Grassi, C; Nonis, A, 1988
)
"The pharmacokinetics and bioavailability of rifampin were determined after IV (10 mg/kg of body weight) and intragastric (20 mg/kg of body weight) administration to 6 healthy, adult horses."( Pharmacokinetics, bioavailability, and in vitro antibacterial activity of rifampin in the horse.
Baggot, JD; Hietala, SK; Spensley, MS; Wilson, WD, 1988
)
" Elevated temperature alone was not responsible for observed pharmacokinetic changes leading to the increase of bioavailability of oral rifampicin since another pyrogenic substance (endotoxin) had an opposite effect on pharmacokinetics of previously tested drugs."( The effects of peptidoglycan, a pyrogenic constituent of gram-positive microorganisms, on the pharmacokinetics of rifampicin.
Lavický, J; Rasková, H; Rotta, J; Urbanová, Z; Vanĕcek, J, 1988
)
" After the toxin administration the bioavailability of oral RFP was 4-fold lower."( Bacterial pyrogens of different origin and pharmacokinetics of rifampicin.
Celeda, L; Krecek, J; Kvĕtina, J; Lavický, J; Rasková, H; Urbanová, Z; Vanĕcek, J, 1987
)
"The bioavailability of isoniazid, rifampin, and pyrazinamide in 2 combined formulations of the 3 drugs (Rifater) for use primarily in the short-course chemotherapy of tuberculosis has been studied in Chinese patients in Singapore and Hong Kong."( The bioavailability of isoniazid, rifampin, and pyrazinamide in two commercially available combined formulations designed for use in the short-course treatment of tuberculosis.
Allen, BW; Chan, SL; Ellard, DR; Ellard, GA; Girling, DJ; Ng, HK; Nunn, AJ; Tan, TH; Teo, SK, 1986
)
"A bioavailability study of rifampicin 450 mg caplets and rifampicin 600 mg caplets was carried out in 20 healthy male subjects."( Bioavailability of rifampicin caplets (600 mg and 450 mg) in healthy Indonesian subjects.
Ganiswarna, SG; Ringoringo, VS; Setiabudy, R; Wilmana, PF, 1986
)
"The absolute bioavailability of oral rifampin was determined in 20 pediatric patients."( Pharmacokinetics of rifampin in children. II. Oral bioavailability.
Koup, JR; Smith, AL; Viswanathan, CT; Weber, A; Williams-Warren, J, 1986
)
" The apparent bioavailability was moderate to low for IM and oral administrations (59."( Rifampin in the horse: comparison of intravenous, intramuscular, and oral administrations.
Beckstrom, DA; Burrows, GE; MacAllister, CG; Nick, JT, 1985
)
" These compounds are zwitterionic in nature and are poorly absorbed through the gastroenteric tract but maintain the ability to cross the bacterial cell wall."( 4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
Brufani, M; Cellai, L; Marchi, E; Mascellani, G; Montecchi, L; Venturini, AP, 1985
)
" Considering these multiform processes, the determination of the bioavailability of RMP preparations by means of the RMP secretion in urine is taken to be manipulatable and uncertainly."( [The pharmacokinetics of rifampicin in the intermittent treatment of patients with pulmonary tuberculosis. 1. Excretion of rifampicin in the urine].
Eule, H; Iwainsky, H; Werner, E; Winsel, K, 1985
)
" The bioavailability of the active, orally administered rifampicin decreased from 93% after the first single oral dose to 68% after 3 weeks of oral and intravenous rifampicin therapy."( Pharmacokinetics of oral and intravenous rifampicin during chronic administration.
Eichelbaum, M; Jensen, JC; Loos, U; Mikus, G; Musch, E; Schwabe, HK, 1985
)
" Total area under the concentration-time curve from 0 to 8 hours and the rate of absorption were also significantly reduced when rifampicin was administered with food."( Effect of food on bioavailability of rifampicin.
Krishnaswamy, K; Polasa, K, 1983
)
" On their bioavailability parameters, the DI product showed higher C max and AUC value than CB, in both healthy subjects and tubercular patients, but did not show a statistically significant difference."( The dissolution and bioavailability of rifampicin products in healthy subjects and tubercular patients.
Araki, Y; Shinozawa, S; Yoshimura, A, 1983
)
"In a 3-year bioavailability program 14 studies in 45 healthy volunteers were carried out to differentiate between experimental lots of rifampicin (RMP) capsules and marketed preparations of other manufacturers with lower bioavailability than Rifadin (RFD), used as standard reference drug."( Bioavailability of rifampicin capsules.
Buniva, G; Carozzi, A; Pagani, V, 1983
)
" Because of the marked reduction in the extent of bioavailability of total, and especially free, prednisolone, dosage adjustments should be made accordingly if prednisolone and rifampicin are prescribed concomitantly."( Changes in prednisolone pharmacokinetics and protein binding during treatment with rifampicin.
Bergrem, H; Refvem, OK, 1983
)
" The bioavailability of norethisterone and ethinyl estradiol (EE) is incomplete when drugs are given orally as opposed to intravenously."( The third S.K. & F. Prize lecture, University of London, December 1981. The clinical pharmacology of oral contraceptive steroids.
Orme, ML, 1982
)
"The triple combination studied could replace the separate drugs in the initial treatment phase in countries where the bioavailability of the drugs used has been proven."( [Clinical trial of a combination of three drugs in fixed proportions in the treatment of tuberculosis. Groupe de Travail sur la Chimiothérapie de la Tuberculose].
Boulahbal, F; Chaulet, P, 1995
)
"The low and variable bioavailability of cyclosporine has been attributed to poor absorption."( Differentiation of absorption and first-pass gut and hepatic metabolism in humans: studies with cyclosporine.
Benet, LZ; Gomez, DY; Gupta, SK; Hebert, MF; Rowland, M; Wacher, VJ; Wu, CY, 1995
)
" Food may however decrease the oral bioavailability of rifampicin and isoniazid."( Study of the effect of concomitant food on the bioavailability of rifampicin, isoniazid and pyrazinamide.
Smith, P; Zent, C, 1995
)
"A triple-crossover pharmacokinetic study in 27 patients with tuberculosis (15 males and 12 females) compared the bioavailability of rifampicin, isoniazid and pyrazinamide without food (control) with that when taken with a high carbohydrate (CHO) or high lipid (LIPID) diet."( Study of the effect of concomitant food on the bioavailability of rifampicin, isoniazid and pyrazinamide.
Smith, P; Zent, C, 1995
)
" Individual patient bioavailability on each meal was compared to the no-food control."( Study of the effect of concomitant food on the bioavailability of rifampicin, isoniazid and pyrazinamide.
Smith, P; Zent, C, 1995
)
"The relative bioavailability of a capsule formulation and the effects of food on the pharmacokinetics of a hypolipidemic agent (CGP 43371) in 12 healthy subjects were examined."( Effect of food on the relative bioavailability of a hypolipidemic agent (CGP 43371) in healthy subjects.
Chan, K; Cipriano, A; John, VA; Klibaner, M; Sun, JX, 1994
)
" The results of fecal analysis indicated that transit of the two compounds in the gastrointestinal tract were similar, and bioavailability of CGP 43371 was calculated to be 9% based on the difference between the cumulative amounts of the nonabsorbable radioactive marker and CGP 43371 found in the feces."( Explaining variable absorption of a hypolipidemic agent (CGP 43371) in healthy subjects by gamma scintigraphy and pharmacokinetics.
Chan, K; Cipriano, A; Digenis, GA; Maniara, WM; Page, RC; Powell, ML; Ryo, UY; Sandefer, EP; Sun, JX; Walter, B, 1996
)
" The oral bioavailability of rifabutin is low."( The clinical pharmacokinetics of rifabutin.
Blaschke, TF; Skinner, MH, 1996
)
" Systemic clearance and bioavailability of the verapamil enantiomers were determined by coadministering deuterated verapamil intravenously on day 4, on day 16, and on day 24."( Differential induction of prehepatic and hepatic metabolism of verapamil by rifampin.
Busse, D; Eichelbaum, M; Fromm, MF; Kroemer, HK, 1996
)
"01) and bioavailability decreased from 41."( The nifedipine-rifampin interaction. Evidence for induction of gut wall metabolism.
Fromm, MF; Heidemann, H; Holtbecker, N; Kroemer, HK; Ohnhaus, EE, 1996
)
"Twenty male volunteers who were slow metabolisers of isoniazid, completed this single-blind, single-dose, randomised, cross-over study to compare the bioavailability of rifampicin (CAS 13292-46-1), isoniazid (CAS 54-85-3) and ethambutol (CAS 1070-11-7) from Myrin tablets (test preparation) with the bioavailability of these drugs from a combination of capsules containing rifampicin and tablets containing isoniazid and ethambutol (reference)."( Relative bioavailability of rifampicin, isoniazid and ethambutol from a combination tablet vs. concomitant administration of a capsule containing rifampicin and a tablet containing isoniazid and ethambutol.
Duursema, L; Groenewoud, G; Hundt, HK; Middle, MV; Mogilnicka, EM; Müller, FO; Schall, R; Swart, KJ, 1995
)
"In the bioavailability studies with drugs biotransformed to biologically active metabolities only the concentrations of the parent drug (PD) are usually taken into account even when the pharmacokinetic data on the metabolite(s) (M) are available."( [Correlation between pharmacokinetic parameters of rifampicin and its biologically active metabolite as related to estimation of the relative bioavailability of the antibiotic].
Dombrovskiĭ, VS; Firsov, AA; Gagaeva, EV; Kadenatsi, IB; Strachunskiĭ, LS, 1996
)
"In this study the bioavailability of a new pharmaceutical form of rifampicin, Rifampicine Generic (300 mg capsules), was compared to a reference form Rimactan (300 mg capsules)."( Bioequivalence study of two pharmaceutical forms of rifampicin capsules in man.
Barre, J; Benakis, A; Chouchane, N; Tillement, JP; Toumi, A,
)
" Rifampin was found to increase the values of clearance/bioavailability (CL/F) and volume of distribution/ bioavailability (V/F) by approximately 70%."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
" The mean relative bioavailability of nifedipine following pre-treatment with rifampicin 1200 mg was 35."( The effect of single does of rifampicin on the pharmacokinetics of oral nifedipine.
Abdu-Aguye, I; Mustapha, A; Ndanusa, BU, 1997
)
"Assessment of the bioavailability of the Chinese rifapentine used in the trial."( Bioavailability of Chinese rifapentine during a clinical trial in Hong Kong.
Chan, SL; Dickinson, JM; Lam, CW; Mitchison, DA; Tam, CM, 1997
)
"An initial comparison of areas under curve obtained in a random allocation to 40 patients of rifapentine either of Western or Chinese origin indicated that the bioavailability of the Chinese drug was 74% of the Western drug."( Bioavailability of Chinese rifapentine during a clinical trial in Hong Kong.
Chan, SL; Dickinson, JM; Lam, CW; Mitchison, DA; Tam, CM, 1997
)
" Because of poor bioavailability of the rifapentine used (produced in China), its dose size was increased from 600 mg initially to about 750 mg in the last third of patients to obtain serum concentrations similar to those with rifapentine of Western origin; all doses were given after a meal promoting absorption."( Rifapentine and isoniazid in the continuation phase of treating pulmonary tuberculosis. Initial report.
Chan, SL; Kam, KM; Lam, CW; Leung, CC; Mitchison, DA; Morris, JS; Tam, CM, 1998
)
"To test whether the bioavailability of antituberculosis drugs is altered in HIV-infected patients with tuberculosis."( Does AIDS impair the absorption of antituberculosis agents?
Smith, PJ; Taylor, B, 1998
)
"To examine the relative bioavailability of rifampicin, isoniazid and pyrazinamide after oral administration of the drugs given alone in comparison to that of the same drugs after administration of Trifazid."( Bioavailability of rifampicin, isoniazid and pyrazinamide from fixed-dose combination capsules.
Augustynowicz-Kopec, E; Grubek-Jaworska, H; Niemirowska-Mikulska, H; Safianowska, A; Stambrowska, H; Walkiewicz, R; Zwolska, Z, 1998
)
"This study was carried out to elucidate the possible mechanism(s) responsible for reduced oral rifampicin bioavailability after multiple dosing."( Assessment of presystemic factors on the oral bioavailability of rifampicin following multiple dosing.
Chiu, FC; Li, RC; Liu, XG; Zhang, JN; Zhu, M, 1998
)
"Purpose of the study was the examination of the relative bioavailability of rifampicin and isoniazid from Rifamazid (fixed-dose combination) and bioavailability of each drug in free simultaneous combination."( [Results of examination in healthy volunteers of rifampicin and isoniazid bioavailability from Polish two-drug combination capsules of rifamazid used for tuberculosis treatment].
Augustynowicz-Kopeć, E; Niemirowska-Mikulska, H; Stambrowska, A; Zofia, Z, 1998
)
"03) and decreased tacrolimus bioavailability (14."( Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers.
Bekersky, I; Dressler, D; Fisher, RM; Hebert, MF; Marsh, CL, 1999
)
"The present study assesses bioavailability indices for rifampicin, isoniazid and pyrazinamide when administered to healthy volunteers separately or in a fixed triple-drug formulation, Rifater 125 SCT."( Bioavailability of rifampicin, isoniazid and pyrazinamide in a triple drug formulation: comparison of plasma and urine kinetics.
Chandrasekaran, V; Gurumurthy, P; Kumar, AK; Kumaraswami, V; Prabhakar, R; Ramachandran, G; Venkatesan, P; Vijayalakshmi, S; Vjayasekaran, V, 1999
)
"To compare the pharmacokinetics of rifampicin, isoniazid and pyrazinamide based on their blood concentrations up to 12 hours with the proportions of the doses of the drugs and their metabolites excreted in urine up to 12 hours, and to assess the bioavailability indices for the free and fixed triple drug formulations."( Bioavailability of rifampicin, isoniazid and pyrazinamide in a triple drug formulation: comparison of plasma and urine kinetics.
Chandrasekaran, V; Gurumurthy, P; Kumar, AK; Kumaraswami, V; Prabhakar, R; Ramachandran, G; Venkatesan, P; Vijayalakshmi, S; Vjayasekaran, V, 1999
)
"Human bioavailability studies provide direct straightforward information, particularly when studying compounds such as rifampicin and other major anti-tuberculosis drugs."( Bioavailability of rifampicin, isoniazid and pyrazinamide in a triple drug formulation: comparison of plasma and urine kinetics.
Chandrasekaran, V; Gurumurthy, P; Kumar, AK; Kumaraswami, V; Prabhakar, R; Ramachandran, G; Venkatesan, P; Vijayalakshmi, S; Vjayasekaran, V, 1999
)
" The bioavailability of oral ondansetron was reduced from 60% to 40% (P < ."( The effect of rifampin on the pharmacokinetics of oral and intravenous ondansetron.
Kivistö, KT; Neuvonen, PJ; Villikka, K, 1999
)
"The effect of single and multiple doses of a herbal preparation trikatu, an Ayurvedic prescription, on the bioavailability and pharmacokinetics of rifampicin was studied in rabbits."( Effect of trikatu, an Ayurvedic prescription, on the pharmacokinetic profile of rifampicin in rabbits.
Bhargava, VK; Garg, SK; Karan, RS, 1999
)
"To assess the bioavailability of rifampicin (RMP) in three brands of combination formulations of anti-tuberculosis drugs."( Comparative bioequivalence study of rifampicin and isoniazid combinations in healthy volunteers.
Bhatt, AD; D'Sa, S; Desai, ND; Gandewar, K; Padgaonkar, KA; Revankar, SN; Shah, V; Vaz, JA, 1999
)
"A three-way double-blind, cross-over bioavailability study of RMP and isoniazid (INH), consisting of a comparison of a two-drug combination of tablets of RMP and INH each separately (reference brand R) and a tablet of RMP + INH (brand N), and a capsule of RMP + INH (brand L) was carried out in 12 healthy male volunteers."( Comparative bioequivalence study of rifampicin and isoniazid combinations in healthy volunteers.
Bhatt, AD; D'Sa, S; Desai, ND; Gandewar, K; Padgaonkar, KA; Revankar, SN; Shah, V; Vaz, JA, 1999
)
" In vitro dissolution profiles of the same drugs were determined and compared with human bioavailability study results."( Comparative bioavailability of three different preparations of rifampicin.
Ansko, P; Davies, PD; Kiivet, RA; Lambert, J; Pähkla, R; Winstanley, P, 1999
)
"No statistically significant difference was found in main bioavailability parameters between Rimactane and generic preparations studied."( Comparative bioavailability of three different preparations of rifampicin.
Ansko, P; Davies, PD; Kiivet, RA; Lambert, J; Pähkla, R; Winstanley, P, 1999
)
"Rifampicin (RIF) hydrolyzes in acidic medium to form insoluble and poorly absorbed 3-Formyl rifamycin SV (3-FRSV)."( Stability of rifampicin in dissolution medium in presence of isoniazid.
Kotecha, JS; Rathod, IS; Savale, SS; Shah, PB; Shah, SA; Shishoo, CJ, 1999
)
"Compared with an oral solution, the relative bioavailability of rifapentine is 70% following oral admninistration of tablets."( Rifapentine: its role in the treatment of tuberculosis.
Nahata, MC; Temple, ME, 1999
)
" By contrast, published information concerning the absorption of rifampicin from currently marketed combined formulations and on laboratory methods for precisely assessing their bioavailability is very sparse."( Rifampicin bioavailability: a review of its pharmacology and the chemotherapeutic necessity for ensuring optimal absorption.
Ellard, GA; Fourie, PB, 1999
)
"Concern has been expressed about the bioavailability of rifampicin in some fixed-dose combination (FDC) anti-tuberculosis formulations."( Recent bioequivalence studies on fixed-dose combination anti-tuberculosis drug formulations available on the global market.
Fourie, PB; Gabriels, G; McIlleron, H; Onyebujoh, PC; Padayatchi, N; Pillai, G; Smith, PJ, 1999
)
"To evaluate the relative bioavailability of rifampicin in various FDC formulations currently in use in tuberculosis control programmes in the global market."( Recent bioequivalence studies on fixed-dose combination anti-tuberculosis drug formulations available on the global market.
Fourie, PB; Gabriels, G; McIlleron, H; Onyebujoh, PC; Padayatchi, N; Pillai, G; Smith, PJ, 1999
)
"The poor relative bioavailability of rifampicin from some FDCs has been documented."( Recent bioequivalence studies on fixed-dose combination anti-tuberculosis drug formulations available on the global market.
Fourie, PB; Gabriels, G; McIlleron, H; Onyebujoh, PC; Padayatchi, N; Pillai, G; Smith, PJ, 1999
)
"The perceived need to demonstrate whether or not the rifampicin bioavailability of commercially manufactured fixed-dose combinations is satisfactory."( The evaluation of rifampicin bioavailabilities of fixed-dose combinations of anti-tuberculosis drugs: procedures for ensuring laboratory proficiency.
Ellard, GA, 1999
)
" Due to difficulties in producing effective combined formulations of these three drugs, the bioavailability of new combination formulations needs to be assessed prior to registration."( Determination of rifampicin, isoniazid and pyrazinamide by high performance liquid chromatography after their simultaneous extraction from plasma.
Fredericks, A; Smith, PJ; van Dyk, J, 1999
)
"To develop a rapid, simple and sensitive high performance liquid chromatography (HPLC) assay method suitable for assaying RIF, INH and PZA in large numbers of plasma samples generated in bioavailability studies."( Determination of rifampicin, isoniazid and pyrazinamide by high performance liquid chromatography after their simultaneous extraction from plasma.
Fredericks, A; Smith, PJ; van Dyk, J, 1999
)
"The prerequisite for in vivo bioavailability testing of rifampicin in fixed-dose combination (FDC) formulations is widely accepted."( The development of a standardised screening protocol for the in vivo assessment of rifampicin bioavailability.
Ellard, GA; Fourie, PB; Gabriels, G; McIlleron, H; Smith, PJ, 1999
)
"The results of three bioavailability and bioequivalence studies of different rifampicin-containing FDCs were analysed."( The development of a standardised screening protocol for the in vivo assessment of rifampicin bioavailability.
Ellard, GA; Fourie, PB; Gabriels, G; McIlleron, H; Smith, PJ, 1999
)
"Estimates of relative bioavailability calculated using the contracted blood sampling protocol were closely similar to those derived using the extended sampling schedules."( The development of a standardised screening protocol for the in vivo assessment of rifampicin bioavailability.
Ellard, GA; Fourie, PB; Gabriels, G; McIlleron, H; Smith, PJ, 1999
)
"To evaluate the comparative bioavailability of antituberculosis drugs in FDC formulations and the same doses in separate formulations of antituberculosis drugs, using a simplified protocol developed by the World Health Organization (WHO)."( The WHO simplified study protocol in practice: investigation of combined formulations supplied by the WHO.
Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 1999
)
" This is predominantly necessitated by the fact that rifampicin bioavailability can be adversely affected when put in combination with isoniazid and pyrazinamide, and by the need for standardisation of the formulations to only a few essential combinations in order to better control quality."( Proposed minimum registration requirements for fixed-dose combination anti-tuberculosis drugs.
Fourie, PB, 1999
)
"Combining rifampicin in the same tablet with isoniazid, with or without pyrazinamide, is known to affect the bioavailability of the drug."( Structures required, roles and responsibilities in maintaining laboratories for quality assurance of anti-tuberculosis fixed-dose combinations in accordance with the IUATLD/WHO statement.
Fourie, PB; Spinaci, S, 1999
)
"To study and compare the bioavailability of rifampicin (RIF), in two locally manufactured formulations; an FDC and a separate formulation and an imported FDC formulation."( Bioavailability of rifampicin in a separate formulation and fixed dose combination with isoniazid NIH: a case for a fixed dose combination (FDC) for the treatment of tuberculosis.
Chitemerere, C; Gumbo, J; Ndudzo, P; Nyazema, NZ; Rabvukwa, P, 1999
)
" However, bioavailability of propafenone dropped from 30% +/- 24% to 4% +/- 3% (P < ."( Enzyme induction in the elderly: effect of rifampin on the pharmacokinetics and pharmacodynamics of propafenone.
Dilger, K; Hofmann, U; Klotz, U, 2000
)
" The data indicate that these inhibitors can be used to determine the in vivo relevance of Oatp1 and Oatp2 for the overall bioavailability and disposition of drugs and other Oatp1/2 substrates."( Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2.
Cattori, V; Fattinger, K; Hagenbuch, B; Meier, PJ; Stieger, B, 2000
)
" A five-fold increase in the area under plasma rifampicin concentration-time curve for niosomal rifampicin as compared to free drug indicated better bioavailability of encapsulated drug."( Prolonged release biodegradable vesicular carriers for rifampicin--formulation and kinetics of release.
Kamath, MP; Karki, R; Kotian, M; Shenoy, BD; Tiwari, SB; Udupa, N, 2000
)
" We conclude that the cause of the increased oral clearance of fexofenadine is a reduced bioavailability caused by induction of intestinal P-glycoprotein."( The effect of rifampin administration on the disposition of fexofenadine.
Bruce, MA; Haehner-Daniels, BD; Hall, SD; Hamman, MA, 2001
)
"The perceived need for simple, non-invasive methods of assessing the relative bioavailability of rifampicin in fixed-dose combination (FDC) anti-tuberculosis formulations."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
"To compare the performance of methods based on urinary excretion data with those utilising plasma concentration-time profiles to assess the relative bioavailability of rifampicin in combined and single-drug formulations."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
"There was good agreement between the relative bioavailability of the formulations using plasma and urinary excretion data, although the precision of the urinary-based estimates was slightly less than those derived from the plasma findings."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
"The problem of poor/variable bioavailability of rifampicin, which is shown in particular when the drugs are present in anti-tubercular fixed-dose combination (FDC) products, is a matter of serious concern."( A critical review of the probable reasons for the poor variable bioavailability of rifampicin from anti-tubercular fixed-dose combination (FDC) products, and the likely solutions to the problem.
Mariappan, TT; Sarda, N; Shankar, R; Singh, B; Singh, S, 2001
)
"The present study describes comparative bioavailability of rifampicin (RIF) after administration of a single component RIF (450 mg) capsule and rifampicin-isoniazid (RIF-INH) (450+300 mg) fixed dose combination (FDC) capsule formulations."( Impaired bioavailability of rifampicin in presence of isoniazid from fixed dose combination (FDC) formulation.
Rathod, IS; Savale, SS; Shah, SA; Shishoo, CJ; Vora, MJ, 2001
)
"The effects of hepatic and presystemic enzyme induction on the bioavailability (F) and disposition of antipyrine after repeated rifampicin (RFM) and rifabutin (RBT) exposure were studied in mice."( Induction of hepatic and presystemic metabolism of antipyrine in the mice: rifampicin versus rifabutin.
Li, RC; Liu, XG; Narang, PK,
)
"Because rifampicin may greatly decrease the oral bioavailability of nilvadipine, caution is needed when these two drugs are to be coadministered."( The effects of rifampicin on the pharmacokinetics and pharmacodynamics of orally administered nilvadipine to healthy subjects.
Echizen, H; Fukuda, J; Furuie, K; Hayashi, T; Saima, S; Yoshimoto, H, 2002
)
" The relative bioavailability of rifampicin (RIF), isoniazid (INH) and pyrazinamide (PYZ) was assessed on a group of 13 healthy male subjects from a four drug FDC versus separate formulations at the same dose levels."( Assessment of bioequivalence of rifampicin, isoniazid and pyrazinamide in a four drug fixed dose combination with separate formulations at the same dose levels.
Agrawal, S; Bhade, SR; Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 2002
)
" The national drug regulatory authority subsequently withdrew the batches in question, as sufficient bioavailability data had not been submitted after what the manufacturer had considered to be a minor formulation change."( Widespread distribution of a single drug rifampicin formulation of inferior bioavailability in South Africa.
Burger, A; Folb, P; McIlleron, H; Smith, P; Wash, P, 2002
)
"Although rifampicin is a key drug in tuberculosis treatment, little is known about its quality and bioavailability in countries endemic for tuberculosis."( Low plasma concentrations of rifampicin in tuberculosis patients in Indonesia.
Alisjahbana, B; Borst, F; Burger, D; Danusantoso, H; de Lange, WC; Nelwan, RH; van Crevel, R; van der Meer, JW, 2002
)
"To investigate possible variations in the bioavailability of plasma rifampicin in tuberculosis patients in Indonesia."( Low plasma concentrations of rifampicin in tuberculosis patients in Indonesia.
Alisjahbana, B; Borst, F; Burger, D; Danusantoso, H; de Lange, WC; Nelwan, RH; van Crevel, R; van der Meer, JW, 2002
)
"The unexpectedly low plasma concentrations of rifampicin in this setting are most likely due to reduced bioavailability of local drug preparations, as the rifampicin content of the drug preparations was found to be normal."( Low plasma concentrations of rifampicin in tuberculosis patients in Indonesia.
Alisjahbana, B; Borst, F; Burger, D; Danusantoso, H; de Lange, WC; Nelwan, RH; van Crevel, R; van der Meer, JW, 2002
)
" In this study, the relative bioavailability of rifampicin, isoniazid and pyrazinamide was assessed in a group of 14 healthy male subjects using the FDC tablet containing 4 drugs versus separate formulations at the same dose levels."( Bioequivalence assessment of rifampicin, isoniazid and pyrazinamide in a fixed dose combination of rifampicin, isoniazid, pyrazinamide and ethambutol vs. separate formulations.
Agrawal, S; Bhade, SR; Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 2002
)
" The encapsulation of drug in alginate microparticles resulted in up to a nine-fold increase in relative bioavailability compared with free drugs."( Alginate-based oral drug delivery system for tuberculosis: pharmacokinetics and therapeutic effects.
Garg, SK; Khuller, GK; Sharma, S, 2003
)
" The main target of the mentioned study was a comparison of the bioavailability of rifampicin."( The pharmacokinetic factors and bioavailability of rifampicin, isoniazid and pyrazinamid fixed in one dose capsule.
Augustynowicz-Kopeć, E; Niemirowska-Mikulska, H; Zwolska, Z,
)
" The objective of this investigation was to evaluate whether the World Health Organization (WHO) simplified screening protocol for the bioequivalence assessment of rifampicin can be used for the evaluation of other components of FDC so as to ensure the bioavailability of all drugs at tissue site."( Evaluation of bioequivalence of isoniazid and pyrazinamide in three and four drugs fixed dose combinations using WHO simplified protocol.
Agrawal, S; Kaul, CL; Panchagnula, R; Rungta, S; Sancheti, P, 2003
)
"RMP was well absorbed from the stomach due to its solubility, which was maximum between pH 1-2."( Regional gastrointestinal permeability of rifampicin and isoniazid (alone and their combination) in the rat.
Mariappan, TT; Singh, S, 2003
)
" Relative bioavailability of encapsulated drugs was greater than that of free drugs."( Chemotherapeutic potential of orally administered poly(lactide-co-glycolide) microparticles containing isoniazid, rifampin, and pyrazinamide against experimental tuberculosis.
Khuller, GK; Sharma, S; Ul-Ain, Q, 2003
)
" The chances of reduced bioavailability of rifampicin from FDCs necessitated its evaluation against standard formulations of individual drugs in bioequivalence studies."( Plasma pooling methodology as a faster and cheaper tool to evaluate bioequivalence of rifampicin component of FDCs of antitubercular drugs.
Agrawal, S; Panchagnula, R; Sharma, A, 2003
)
" In literature, there are conflicting reports regarding effect of food on the bioavailability of rifampicin."( In vitro evaluation of food effect on the bioavailability of rifampicin from antituberculosis fixed dose combination formulations.
Agrawal, S; Kaul, CL; Panchagnula, R; Rungta, S; Sancheti, P, 2003
)
" The elimination half-life and mean residence time of the drugs were significantly prolonged compared to when the parent drugs were administered orally, resulting in an enhanced relative bioavailability (compared to oral administration) for encapsulated drugs (12."( Poly (DL-lactide-co-glycolide) nanoparticle-based inhalable sustained drug delivery system for experimental tuberculosis.
Khuller, GK; Pandey, R; Prasad, B; Sharma, A; Sharma, S; Zahoor, A, 2003
)
"Nebulization of nanoparticles-based ATDs forms a sound basis for improving drug bioavailability and reducing the dosing frequency for better management of pulmonary tuberculosis."( Poly (DL-lactide-co-glycolide) nanoparticle-based inhalable sustained drug delivery system for experimental tuberculosis.
Khuller, GK; Pandey, R; Prasad, B; Sharma, A; Sharma, S; Zahoor, A, 2003
)
"Poor bioavailability of rifampicin (R) in combination with other anti-tuberculosis drugs such as isoniazid (H), pyrazinamide (Z), and ethambutol (E) is a subject of much concern for the last few decades."( Bioavailability of rifampicin following concomitant administration of ethambutol or isoniazid or pyrazinamide or a combination of the three drugs.
Chandrasekaran, V; Gurumurthy, P; Immanuel, C; Prabhakar, R; Ramachandran, G; Venkatesan, P, 2003
)
" Bioavailability was expressed as an index (BI) of area under time concentration curve (AUC) calculated from the plasma concentrations or proportion of dose of R excreted as R plus DR in urine with the combinations to that with R alone."( Bioavailability of rifampicin following concomitant administration of ethambutol or isoniazid or pyrazinamide or a combination of the three drugs.
Chandrasekaran, V; Gurumurthy, P; Immanuel, C; Prabhakar, R; Ramachandran, G; Venkatesan, P, 2003
)
" Hence, bioequivalence study of four drug FDC tablet was conducted using 22 healthy male volunteers according to WHO recommended protocol to determine bioavailability of rifampicin, isoniazid and pyrazinamide compared to standard separate combination at the same dose level."( Comparative bioavailability of rifampicin, isoniazid and pyrazinamide from a four drug fixed dose combination with separate formulations at the same dose levels.
Agrawal, S; Bhade, SR; Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 2004
)
" The mean residence time and absolute bioavailability were increased several-fold as compared with unencapsulated drugs."( Subcutaneous nanoparticle-based antitubercular chemotherapy in an experimental model.
Khuller, GK; Pandey, R, 2004
)
"Even today the treatment outcome of tuberculosis is questionable due to variable bioavailability of rifampicin, which was discovered four decades back."( Biopharmaceutic and pharmacokinetic aspects of variable bioavailability of rifampicin.
Agrawal, S; Panchagnula, R, 2004
)
"To examine the bioavailability of rifampicin formulations produced in Indonesia, we conducted a single-dose, double-blind, cross-over bioavailability study."( Bioavailability of rifampicin in Indonesian subjects: a comparison of different local drug manufacturers.
Alisjahbana, B; Borst, F; Burger, D; Cox, J; de Graaff, M; de Lange, WC; Nelwan, RH; Sahiratmadja, E; van Crevel, R; van der Meij, W, 2004
)
"Polymorphism of rifampicin has been postulated to be responsible for its variable bioavailability from solid oral dosage forms."( Solid-state characterization of rifampicin samples and its biopharmaceutic relevance.
Agrawal, S; Ashokraj, Y; Bharatam, PV; Panchagnula, R; Pillai, O, 2004
)
"Rifampicin shows variable bioavailability from solid oral dosage forms and the reasons for this variable absorption reported in literature varies from extrinsic formulations factors to intrinsic variability in rifampicin absorption."( Bioequivalence trials of rifampicin containing formulations: extrinsic and intrinsic factors in the absorption of rifampicin.
Agrawal, S; Bhade, S; Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 2004
)
"A 15 mg/kg dose of RPT was well absorbed and well tolerated."( Consecutive-dose pharmacokinetics of rifapentine in patients diagnosed with pulmonary tuberculosis.
Langdon, G; McIlleron, H; Smith, PJ; Wilkins, JJ, 2004
)
" HIV and HIV-tuberculosis patients who have diarrhea and cryptosporidial infection exhibit decreased bioavailability of antituberculosis drugs."( Decreased bioavailability of rifampin and other antituberculosis drugs in patients with advanced human immunodeficiency virus disease.
Bhagavathy, S; Gurumurthy, P; Hemanth Kumar, AK; Mahilmaran, A; Padmapriyadarsini, C; Paramesh, P; Rajasekaran, S; Ramachandran, G; Ravichandran, N; Sekar, L; Swaminathan, S; Venkatesan, P, 2004
)
" This investigation characterized the bioavailability and first-pass metabolism of oral ALF and tested the hypotheses that (1) first-pass ALF clearance reflects first-pass CYP3A activity, (2) miosis after oral ALF will reflect intestinal and hepatic CYP3A activity, and (3) miosis can approximate plasma concentration-based pharmacokinetic measures for IV and oral ALF as a noninvasive in vivo probe for hepatic and first-pass CYP3A activity and drug interactions."( Intravenous and oral alfentanil as in vivo probes for hepatic and first-pass cytochrome P450 3A activity: noninvasive assessment by use of pupillary miosis.
Hoffer, C; Kharasch, ED; Sheffels, P; Walker, A, 2004
)
"Rifaximin is a rifamycin analogue with a broad spectrum of activity similar to that of rifampin; however, because it is poorly absorbed in the gastrointestinal tract, the focus of its development has been on intestinal infections and diseases."( Rifaximin: a nonabsorbed oral antibiotic.
Baker, DE, 2005
)
" The mean residence time and drug bioavailability were improved several-fold in the case of drug-loaded SLPs."( Solid lipid particle-based inhalable sustained drug delivery system against experimental tuberculosis.
Khuller, GK; Pandey, R, 2005
)
" As Pgp varies from person to person to an extent of 2-8-fold, it can be one direct reason for the interindividual variable bioavailability shown by rifampicin."( Evidence of efflux-mediated and saturable absorption of rifampicin in rat intestine using the ligated loop and everted gut sac techniques.
Mariappan, TT; Singh, S,
)
"Rifampicin is one of the oldest and most effective chemotherapeutic agents available for the treatment of tuberculosis but exhibits variable bioavailability from separate and fixed dose combination formulations, which has been identified as a major bottleneck in the effective treatment of tuberculosis."( Implication of biopharmaceutics and pharmacokinetics of rifampicin in variable bioavailability from solid oral dosage forms.
Agrawal, S; Panchagnula, R, 2005
)
" Rifampicin has been found one of the most important anti-tubercular drugs, however variable bioavailability of rifampicin in some FDCs as well as separate formulations has been reported in the literature, and led to the development of WHO model protocol for evaluation of FDCs for bioequivalence trials."( Statistical evaluation of physiological variability of rifampicin in fixed dose combinations.
Ashokraj, Y; Bade, SR; Kaur, K; Panchagnula, R; Parmar, J; Singh, I, 2006
)
" Both hepatic and intestinal metabolism contribute to the low oral bioavailability of ATV in rats."( Pharmacokinetics of atorvastatin and its hydroxy metabolites in rats and the effects of concomitant rifampicin single doses: relevance of first-pass effect from hepatic uptake transporters, and intestinal and hepatic metabolism.
Benet, LZ; Huang, Y; Lau, YY; Okochi, H, 2006
)
" Our findings suggest that decreased bioavailability of nevirapine because of rifampicin coadministration could be overcome by increasing the dose of nevirapine from 200 to 300 mg twice daily without short-term adverse events."( Increasing nevirapine dose can overcome reduced bioavailability due to rifampicin coadministration.
Hemanthkumar, AK; Kumaraswami, V; Narendran, G; Padmapriyadarsini, C; Raja, K; Rajasekaran, S; Ramachandran, G; Sathishnarayan, S; Sukumar, B; Swaminathan, S, 2006
)
"Oral administration of garlic extract decreased the bioavailability of isoniazid significantly with no change in rate of elimination."( Effect of oral administration of crude aqueous extract of garlic on pharmacokinetic parameters of isoniazid and rifampicin in rabbits.
Dhamija, P; Malhotra, S; Pandhi, P, 2006
)
" The relative/absolute bioavailability of the 4 antituberculosis drugs was enhanced several fold."( Chemotherapeutic efficacy of nanoparticle encapsulated antitubercular drugs.
Khuller, GK; Pandey, R; Sharma, S,
)
"Rifampicin has been found to be one of the most important antitubercular drugs; however, variable bioavailability of rifampicin in some fixed dose combinations (FDCs) as well as separate formulations has been reported in the literature."( Plasma pooling to expedite bioequivalence estimation of rifampicin in fixed dose combinations.
Bhade, SR; Kaur, JK; Panchagnula, R; Parmar, J; Singh, I, 2006
)
"The bioavailability of rifampicin (RIF) in a fixed dose combination (FDC) used for the treatment of tuberculosis remains an area of clinical concern and several pharmaceutical alternatives are being explored to overcome this problem."( Herbal modulation of drug bioavailability: enhancement of rifampicin levels in plasma by herbal products and a flavonoid glycoside derived from Cuminum cyminum.
Gupta, BD; Johri, RK; Qazi, GN; Sachin, BS; Satti, NK; Sethi, S; Sharma, SC; Suri, KA; Tasduq, SA; Tikoo, AK; Tikoo, MK, 2007
)
" Ranitidine was shown to be a P-gp substrate in vivo in human volunteers and it was found that oral bioavailability of ranitidine was influenced at the intestinal absorption phase."( Effect of ketoconazole and rifampicin on the pharmacokinetics of ranitidine in healthy human volunteers: a possible role of P-glycoprotein.
Gundu, J; Machavaram, KK; Yamsani, MR, 2006
)
" Its function is to limit the bioavailability of orally administered compounds."( Venlafaxine induces P-glycoprotein in human Caco-2 cells.
Ehret, MJ; Levin, GM; Narasimhan, M; Rathinavelu, A, 2007
)
" The studies determined the bioavailability and bioequivalence of RMP-containing FDCs, and conformed with the requirements of the South African national drug regulatory authority for each of the active constituents."( Modification to improve efficiency of sampling schedules for BA/BE testing of FDC anti-tuberculosis drugs.
Folb, PI; Fourie, PB; Gabriels, GA; McIlleron, H; Smith, PJ, 2007
)
" The objective of this research was to study intestinal absorptive function and bioavailability of rifampin and isoniazid in TB patients."( Intestinal permeability and malabsorption of rifampin and isoniazid in active pulmonary tuberculosis.
Barroso, EC; Bushen, OY; Façanha, MC; Guerrant, RL; Lima, AA; Monteiro, HS; Peloquin, CA; Pinheiro, VG; Ramos, LM, 2006
)
" Human oral bioavailability is an important pharmacokinetic property, which is directly related to the amount of drug available in the systemic circulation to exert pharmacological and therapeutic effects."( Hologram QSAR model for the prediction of human oral bioavailability.
Andricopulo, AD; Moda, TL; Montanari, CA, 2007
)
"The crux of this research was the pragmatic investigation into the formulation of a reconstitutable multiparticulate anti-tuberculosis drug delivery system for facilitated administration for the attainment of segregated gastrointestinal (GI) delivery of rifampicin (RIF) and isoniazid (INH) in order to address issues of unacceptable RIF bioavailability on coadministration with INH."( Formulation and statistical optimization of a novel crosslinked polymeric anti-tuberculosis drug delivery system.
Danckwerts, MP; du Toit, LC; Penny, C; Pillay, V, 2008
)
" Thus, rifampin reduced the exposure to risperidone, probably because of a decrease in its bioavailability through the induction of CYP3A and probably P-glycoprotein."( Effect of rifampin, an inducer of CYP3A and P-glycoprotein, on the pharmacokinetics of risperidone.
Kim, KA; Kim, KB; Lee, HJ; Liu, KH; Park, JY; Park, PW; Shin, JG, 2008
)
" The variant ABCC2 1249G>A (V417I), however, was associated with lower oral bioavailability (P=0."( Influence of genetic polymorphisms on intestinal expression and rifampicin-type induction of ABCC2 and on bioavailability of talinolol.
Caliebe, A; Cascorbi, I; Haenisch, S; May, K; Siegmund, W; Wegner, D, 2008
)
" Variability in the shape of the absorption curve was described using a flexible transit compartment model, in which a delay in the onset of absorption and a gradually changing absorption rate were modeled as the passage of drug through a chain of hypothetical compartments, ultimately reaching the absorption compartment."( Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
Karlsson, MO; Langdon, G; McIlleron, H; Pillai, G; Savic, RM; Simonsson, US; Smith, PJ; Wilkins, JJ, 2008
)
"Rifaximin, a poorly absorbed rifamycin derivative, is a promising alternative for the treatment of Clostridium difficile infections."( Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
Galang, MA; Gerding, DN; Hecht, DW; Johnson, S; O'Connor, JR; Sambol, SP; Vedantam, G, 2008
)
"Rifampicin, one of the main first line anti-TB drugs, shows variable bioavailability in different marketed preparations and reasons cited include physiological, degradation, manufacturing/ processing, solid state, and bioavailability assessment procedure."( Effect of amorphous content on dissolution characteristics of rifampicin.
Bhardwaj, V; Panchagnula, R, 2008
)
"5 h of free drug) and a systemic bioavailability similar to that of free drug."( Slow release formulations of inhaled rifampin.
Arya, V; Coowanitwong, I; Hochhaus, G; Kulvanich, P, 2008
)
" In comparison to free drugs (which were cleared from plasma/organs within 12-24 h), there was a significant enhancement in the relative bioavailability of encapsulated drugs."( Alginate nanoparticles as antituberculosis drug carriers: formulation development, pharmacokinetics and therapeutic potential.
Ahmad, Z; Khuller, GK; Pandey, R; Sharma, S,
)
"4% and reduced the absorption rate constant (k(a)) by almost sixfold."( Population pharmacokinetics of nevirapine in combination with rifampicin-based short course chemotherapy in HIV- and tuberculosis-infected South African patients.
Cohen, K; Elsherbiny, D; Jansson, B; McIlleron, H; Simonsson, US; Smith, P, 2009
)
" The compound appeared to have low to intermediate total body clearance and was orally bioavailable (24-100%)."( Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.
Anderson, JJ; Barten, DM; Boulton, DW; Felsenstein, KM; Flint, OP; Hansel, SB; Krishna, R; Lubinski, J; Pursley, JM; Santone, KS; Thakur, A; Wang, J; Yao, M; Zheng, M, 2009
)
" CC-1a, chemically standardized butanolic fraction, enhanced the plasma levels of rifampicin, pyrazinamide, and isoniazid in Wistar rat, resulting in increased bioavailability indices (C(max) and AUC) of the drugs."( Pharmacokinetic interaction of some antitubercular drugs with caraway: implications in the enhancement of drug bioavailability.
Gupta, BD; Johri, RK; Monica, P; Sachin, BS; Satti, NK; Sharma, SC; Suri, KA; Tikoo, AK; Tikoo, MK, 2009
)
"001), with an enormous reduction in the oral bioavailability of ebastine and significantly reduced histamine-induced skin reactions."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
"Rifaximin is a poorly absorbed semisynthetic antibiotic derivative of rifampin licensed for use in the treatment of traveler's diarrhea."( Pretreatment of epithelial cells with rifaximin alters bacterial attachment and internalization profiles.
Brown, EL; Dupont, HL; Jiang, ZD; Xu, Y; Xue, Q, 2010
)
" Regressional analysis of UV spectrophotometric data for simultaneous RIF and INH prediction thus provides a simplified methodology for use in diverse research settings for the assurance of RIF bioavailability from FDC formulations, specifically modified-release forms."( A mathematical approach for the simultaneous in vitro spectrophotometric analysis of rifampicin and isoniazid from modified-release anti-TB drug delivery systems.
Choonara, Y; du Toit, L; Pillay, V, 2010
)
" SCY-635 was shown to be orally bioavailable in multiple animal species and produced blood and liver concentrations of parent drug that exceeded the 50% effective dose determined in the bicistronic con1b-derived replicon assay."( SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro.
Erdmann, F; Fischer, G; Harris, R; Hopkins, S; Huang, Z; Murray, MG; Ribeill, Y; Scorneaux, B; Smitley, C; Wring, S, 2010
)
" The bioavailability of rifampin was determined by comparing rifampin exposure after oral versus intravenous administration."( Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
Aarnoutse, RE; Adhiarta, IG; Alisjahbana, B; Kariadi, SH; Nijland, HM; Ruslami, R; van Crevel, R, 2010
)
"Oral bioavailability (F) is a product of fraction absorbed (Fa), fraction escaping gut-wall elimination (Fg), and fraction escaping hepatic elimination (Fh)."( Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
Chang, G; El-Kattan, A; Miller, HR; Obach, RS; Rotter, C; Steyn, SJ; Troutman, MD; Varma, MV, 2010
)
"The front line antitubercular drugs rifampicin (RMP) and isoniazid (INH), when co-administered, face the problem of reduced bioavailability of RMP."( Tailored release drug delivery system for rifampicin and isoniazid for enhanced bioavailability of rifampicin.
Avachat, AM; Bhise, SB, 2011
)
" This model also has application for the screening of drug candidates for effects on oral bioavailability via effects on the subcellular distribution and trafficking of P-gp."( Characterization of PXR mediated P-glycoprotein regulation in intestinal LS174T cells.
Allen, J; Bebawy, M; Kota, BP; Roufogalis, BD; Tran, VH, 2010
)
"Nilotinib (Tasigna), an orally bioavailable second-generation BCR-ABL tyrosine kinase inhibitor, is approved for use in patients with chronic myeloid leukemia in chronic phase and accelerated phase who are resistant or intolerant to prior therapy, including imatinib."( Effects of rifampin and ketoconazole on the pharmacokinetics of nilotinib in healthy participants.
Galitz, L; Grouss, K; Harrell, R; Schran, H; Sethuraman, V; Smith, T; Tanaka, C; Yin, OQ, 2011
)
" This led us to investigate the bioavailability of the product."( Relative bioavailability of rifampicin in a three-drug fixed-dose combination formulation.
Domínguez-Ramírez, AM; Jung-Cook, H; Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Romano-Moreno, S; Romero-Méndez, MC; Vigna-Pérez, M, 2010
)
"To investigate the relative bioavailability of RMP from a generic 3FDC formulation used in the Mexican health care system, in comparison to the reference product, in healthy volunteers."( Relative bioavailability of rifampicin in a three-drug fixed-dose combination formulation.
Domínguez-Ramírez, AM; Jung-Cook, H; Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Romano-Moreno, S; Romero-Méndez, MC; Vigna-Pérez, M, 2010
)
"The test product displayed delayed absorption and markedly inferior RMP bioavailability in comparison to the reference product."( Relative bioavailability of rifampicin in a three-drug fixed-dose combination formulation.
Domínguez-Ramírez, AM; Jung-Cook, H; Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Romano-Moreno, S; Romero-Méndez, MC; Vigna-Pérez, M, 2010
)
"Rifaximin is a poorly absorbed non-systemic antimicrobial agent used in various gastrointestinal disorders."( Rifaximin intake leads to emergence of rifampin-resistant staphylococci.
Hoenigl, M; Krause, R; Leitner, E; Rohn, A; Salzer, HJ; Valentin, T; Zollner-Schwetz, I, 2011
)
" Other factors also play important role in the development of MDR-TB such as poor administrative control on purchase and distribution of the drugs with no proper mechanism on quality control and bioavailability tests."( Multi-drug resistant tuberculosis burden and risk factors: an update.
Marahatta, SB,
)
" This study evaluated efavirenz bioavailability after rifampicin administration to healthy volunteers."( Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers.
Djoerban, Z; Setiabudy, R, 2011
)
"Co-administration of a single dose of efavirenz 600 mg/day with 1-week rifampicin 450 mg/day significantly reduced efavirenz bioavailability in healthy volunteers."( Pharmacokinetic interaction between efavirenz and rifampicin in healthy volunteers.
Djoerban, Z; Setiabudy, R, 2011
)
"Gastroretentive floating microspheres have a potential for enhancing the bioavailability and controlled delivery of drugs."( Development and characterization of rifampicin loaded floating microspheres.
Gill, S; Goyal, AK; Goyal, P; Gupta, UD; Narang, RK; Rath, G, 2011
)
" After RIF comedication, relative bioavailability of CLR decreased by more than 90%."( Oral absorption of clarithromycin is nearly abolished by chronic comedication of rifampicin in foals.
Block, W; Freyer, J; Grube, M; Kroemer, HK; Lämmer, M; Lütjohann, D; Oswald, S; Peters, J; Siegmund, W; Venner, M, 2011
)
" Patients heterozygous and homozygous for this polymorphism had reductions in the bioavailability (and, thus, the area under the curve [AUC]) of rifampin of 18% and 28%, respectively."( The SLCO1B1 rs4149032 polymorphism is highly prevalent in South Africans and is associated with reduced rifampin concentrations: dosing implications.
Chigutsa, E; Denti, P; Egan, D; Holford, NH; Maartens, G; McIlleron, H; Owen, A; Pushpakom, S; Smith, PJ; Swart, EC; Visser, ME, 2011
)
" Rifampicin reduced the oral bioavailability of lopinavir and ritonavir by 20% and 45% respectively, and it increased their clearance by 71% and 36% respectively."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
" The higher trough concentrations observed in the morning were explained by both higher bioavailability with the evening meal and lower clearance overnight."( Model-based approach to dose optimization of lopinavir/ritonavir when co-administered with rifampicin.
Decloedt, E; Denti, P; Karlsson, MO; Maartens, G; McIlleron, H; Simonsson, US; Zhang, C, 2012
)
" Antitubercular treatment reduced the oral bioavailability of lopinavir by 77% in children receiving twice usual lopinavir/ritonavir doses and increased ritonavir clearance by 50%."( Population pharmacokinetics of lopinavir and ritonavir in combination with rifampicin-based antitubercular treatment in HIV-infected children.
Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Simonsson, US; van der Walt, JS; Zhang, C, 2012
)
"In order to improve the bioavailability of rifampicin (RIF) from rifampicin and isoniazid (INH) combination formulations, the physicochemical characteristics of RIF, stability of RIF in different pH buffers in the presence of INH, as well as the effect of particle size of RIF materials on the dissolution rate were investigated."( Design and evaluation of enteric-coated tablets for rifampicin and isoniazid combinations.
He, Z; Liu, H; Liu, K; Sun, J; Wang, Y,
)
"Administration of rifampicin for 7 days resulted in a significant reduction in the bioavailability of dabigatran, which returned almost to baseline after 7 days washout."( Decrease in the oral bioavailability of dabigatran etexilate after co-medication with rifampicin.
Härtter, S; Koenen-Bergmann, M; Lemke, U; Nehmiz, G; Reilly, PA; Sharma, A; Timmer, W, 2012
)
" The typical population estimates (interindividual variability) for clearance, volume of distribution and absorption rate constant were 16."( Population pharmacokinetics of clindamycin orally and intravenously administered in patients with osteomyelitis.
Bouazza, N; Curis, E; Jullien, V; Pestre, V; Salmon, D; Tréluyer, JM; Urien, S, 2012
)
"Posaconazole has an important role in the prophylaxis and salvage treatment of invasive fungal infections (IFIs), although poor and variable bioavailability remains an important clinical concern."( Multicenter study of posaconazole therapeutic drug monitoring: exposure-response relationship and factors affecting concentration.
Chen, SC; Dolton, MJ; McLachlan, AJ; Ng, K; Pont, L; Ray, JE, 2012
)
"2-(4-(4-(tert-Butylcarbamoyl)-2-(2-chloro-4-cyclopropylphenylsulfonamido)phenoxy)-5-chloro-2-fluorophenyl)acetic acid (AMG 853) is an orally bioavailable and potent dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors."( Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
Amore, BM; Banfield, C; Boudreaux, MD; Davis, JA; Emery, MG; Foti, RS; Pearson, JT; Prokop, SP; Rock, DA; Wahlstrom, JL; Wienkers, LC; Wong, SL; Zalikowski, JA, 2012
)
" Bioavailability of oral tramadol was reduced by rifampicin from 66 to 49 % (P = 0."( Rifampicin markedly decreases the exposure to oral and intravenous tramadol.
Hagelberg, NM; Laine, K; Neuvonen, M; Neuvonen, PJ; Olkkola, KT; Saari, TI; Saarikoski, T; Scheinin, M, 2013
)
" Rifampin was chosen due to its promising activity against planktonic and biofilm Propionibacterium, its favourable minimal inhibitory concentrations, its excellent oral bioavailability and tissue penetration."( Prosthetic valve endocarditis caused by Propionibacterium species successfully treated with coadministered rifampin: report of two cases.
Braun, DL; Fehr, JS; Hasse, BK; Stricker, J, 2013
)
" Those with the best potency and oral bioavailability were progressed to evaluations of efficacy against acute murine TB."( Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents.
Cho, SN; Franzblau, SG; Hwang, JM; Kaneko, T; Kim, P; Ma, Z; Oh, T; Upton, AM, 2013
)
" However, the quality of FDCs with respect to variable bioavailability is a major issue."( Oral bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide in a 4-drug fixed-dose combination compared with the separate formulations in healthy Chinese male volunteers.
Chen, M; Fu, L; Jin, H; Liu, C; Lu, Y; Wang, B; Xu, J; Zhao, W; Zheng, M; Zhou, L; Zhu, H, 2013
)
"This study was conducted in healthy Chinese subjects to compare the bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide from a 4-drug FDC formulation versus that of the separate formulations."( Oral bioavailability of rifampicin, isoniazid, ethambutol, and pyrazinamide in a 4-drug fixed-dose combination compared with the separate formulations in healthy Chinese male volunteers.
Chen, M; Fu, L; Jin, H; Liu, C; Lu, Y; Wang, B; Xu, J; Zhao, W; Zheng, M; Zhou, L; Zhu, H, 2013
)
"The bioavailability of lopinavir was reduced by 25% in adults whereas children on antituberculosis treatment experienced a 59% reduction, an effect that was moderated by the dose of ritonavir."( Model-based evaluation of the pharmacokinetic differences between adults and children for lopinavir and ritonavir in combination with rifampicin.
Decloedt, EH; Denti, P; Karlsson, MO; McIlleron, H; Ren, Y; Zhang, C, 2013
)
" NXC reduced the extent and rate of absorption of RIF."( Effect of ofloxacin and norfloxacin on rifampicin pharmacokinetics in man.
Barikpoar, E; Brown, S; Ezejiofor, NA; Orisakwe, OE,
)
" The metabolism and bioavailability of cyclosporin can be significantly and persistently influenced through induction of CYP3A4 caused by the concomitant use of rifampicin."( [Low cyclosporin levels induced by the brief use of rifampicin; immunosuppression may fail for several weeks].
Alidjan, F; Bakker, R; Rommers, MK; Swen, JJ; Valk-Swinkels, CG; van 't Veer, NE, 2013
)
"Macrocycles are ideal in efforts to tackle "difficult" targets, but our understanding of what makes them cell permeable and orally bioavailable is limited."( Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?
Giordanetto, F; Kihlberg, J, 2014
)
"To enhance the oral bioavailability of rifampicin (RMP), the newly emerging phospholipid complexation technique was employed."( Novel rifampicin-phospholipid complex for tubercular therapy: synthesis, physicochemical characterization and in-vivo evaluation.
Bhatt, TD; Gill, MS; Singh, C; Suresh, S, 2014
)
" Further studies will be required to determine whether rifampin reduces oxytetracycline bioavailability in this system, as suggested by human studies using other tetracycline-rifampin combinations."( Efficacy of three-week oxytetracycline or rifampin monotherapy compared with a combination regimen against the filarial nematode Onchocerca ochengi.
Bah, GS; Makepeace, BL; Srivastava, A; Tanya, VN; Trees, AJ; Ward, EL, 2014
)
"Subtherapeutic plasma isoniazid (INH) concentrations and the development of bacterial resistance may be attributed to poor quality and reduced bioavailability of fixed-dose combination (FDC) formulations."( Relative bioavailability of isoniazid in a fixed-dose combination product in healthy Mexican subjects.
Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Romano-Moreno, S; Romero-Méndez, MC; Vargas-Morales, JM; Vigna-Pérez, M, 2014
)
"To evaluate the bioequivalence of a generic three-drug FDC formulation (3FDC) in comparison with a 3FDC reference with doses of 300 mg INH in 20 healthy Mexican adults, and to generate data regarding the oral relative bioavailability of the drug in this population."( Relative bioavailability of isoniazid in a fixed-dose combination product in healthy Mexican subjects.
Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Romano-Moreno, S; Romero-Méndez, MC; Vargas-Morales, JM; Vigna-Pérez, M, 2014
)
" The average relative bioavailability calculated for maximum serum concentration area under the concentration-time curve (AUC), AUC(0-24h) and AUC(0-∞) of the test 3FDC formulation vs."( Relative bioavailability of isoniazid in a fixed-dose combination product in healthy Mexican subjects.
Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RC; Romano-Moreno, S; Romero-Méndez, MC; Vargas-Morales, JM; Vigna-Pérez, M, 2014
)
" Under gastric conditions, RIF undergoes fast hydrolysis (a pathway hastened by INH) and oral bioavailability loss."( Rifampicin-loaded 'flower-like' polymeric micelles for enhanced oral bioavailability in an extemporaneous liquid fixed-dose combination with isoniazid.
Hocht, C; Moretton, MA; Sosnik, A; Taira, C, 2014
)
"Low bioavailability of rifampicin, one of the main antituberculous drug, stimulates searches of its new optimized formulations."( [Drug delivery system on the base of phospholipid nanoparticles for rifampicin].
Ipatova, OM; Medvedeva, NV; Prozorovskiĭ, VN; Sanzhakov, MA; Tarkhovskaia, TI; Tikhonova, EG,
)
" Higher oral clearance values in intermediate and fast acetylators also resulted from 23% lower bioavailability compared with slow acetylators."( Population pharmacokinetics of rifampicin, pyrazinamide and isoniazid in children with tuberculosis: in silico evaluation of currently recommended doses.
Denti, P; Donald, PR; McIlleron, HM; Schaaf, HS; Seddon, JA; Seifart, HI; Simonsson, US; Smith, PJ; Thee, S; Zvada, SP, 2014
)
" A previous rifapentine dose escalation study with daily dosing indicated a possible decrease in bioavailability as the dose increased and an increase in clearance over time for rifapentine and its active metabolite, desacetyl rifapentine."( Population pharmacokinetics of rifapentine and desacetyl rifapentine in healthy volunteers: nonlinearities in clearance and bioavailability.
Bliven-Sizemore, E; Burman, W; Dooley, KE; Dorman, SE; Lu, Y; Nuermberger, E; Savic, RM; Weiner, M, 2014
)
" Oral rifampin and oral ethambutol were well absorbed while rectal rifampin was not."( The pharmacokinetics of a single oral or rectal dose of concurrently administered isoniazid, rifampin, pyrazinamide, and ethambutol in Asian elephants (Elephas maximus).
Egelund, EF; Hunter, RP; Isaza, R; P Brock, A; Peloquin, CA, 2014
)
" The model adjusted for body size via allometric scaling, accounted for clearance autoinduction, and detected an increase in bioavailability (+14%) for the patients in the continuation phase."( Nutritional supplementation increases rifampin exposure among tuberculosis patients coinfected with HIV.
Andersen, AB; Castel, S; Changalucha, J; Chigutsa, E; Christiansen, M; Denti, P; Faurholt-Jepsen, D; Friis, H; Hagen, CM; Jeremiah, K; McIlleron, H; PrayGod, G; Range, N; Wiesner, L, 2014
)
" The significantly higher bioavailability and lung accumulation with Gantrez nanoparticle over PES nanoparticles was attributed mucoadhesion and high affinity of Gantrez to the Peyer's patches."( Comparative evaluation of polymeric nanoparticles of rifampicin comprising Gantrez and poly(ethylene sebacate) on pharmacokinetics, biodistribution and lung uptake following oral administration.
Date, PV; Devarajan, PV; Gaikwad, RV; Malshe, VC; Patel, MD; Samad, A, 2014
)
" Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability."( Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Achar, V; Arora, U; Awasthy, D; Bharath, S; Bheemarao, U; Chinnapattu, M; Coulson, M; de Sousa, SM; Ganguly, S; Gaonkar, S; Ghosh, A; Hameed P, S; Hoffner, S; Humnabadkar, V; Kaur, P; Kumar K N, M; Kumar, CN; Madhavapeddi, P; Manjrekar, P; Menasinakai, S; Mukherjee, K; Nandishaiah, R; Narayan, C; Panduga, V; Patil, V; Puttur, J; Raichurkar, A; Ramya, VK; Reddy, J; Rudrapatana, S; Sambandamurthy, VK; Shanbhag, G; Sharma, S; Sharma, U; Shinde, V; Solapure, S; Waterson, D; Werngren, J, 2014
)
" The absorption rate was slower in TB patients and the volume of distribution normalized by total body weight (Vd/kg) was greater than healthy volunteers (P < 0."( Pharmacokinetics of rifampicin in Mexican patients with tuberculosis and healthy volunteers.
Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, Rdel C; Portales-Pérez, DP; Romano-Moreno, S, 2014
)
" The optimized IPAs 49 and 50 showed not only excellent oral bioavailability (80."( Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.
Ahn, S; Choi, I; Jang, J; Kang, H; Kang, S; Kim, HJ; Kim, J; Kim, RY; Kim, YM; Ko, Y; Lee, S; Nam, J; Nam, K; No, Z; Park, S; Pethe, K; Seo, JJ; Seo, M; Seo, MJ, 2014
)
" However the role of ASC on the interaction between dissolution stability and in vivo bioavailability of RIF in the presence of INH has not been explored and therefore examined in the present study."( Ascorbic acid improves stability and pharmacokinetics of rifampicin in the presence of isoniazid.
Natham, R; Rajaram, S; Vemuri, VD, 2014
)
" Bioavailability of Rifampicin is taken care of by conjugating this drug through a acylhydrazine linker to the polymeric backbone."( Increased bioavailability of rifampicin from stimuli-responsive smart nano carrier.
Das Sarma, J; Dinda, H; Mane, SR; Sathyan, A; Shunmugam, R, 2014
)
" Posaconazole relative bioavailability was 55% lower in patients who received posaconazole than in healthy volunteers."( Understanding variability in posaconazole exposure using an integrated population pharmacokinetic analysis.
Brüggemann, RJ; Burger, DM; Dolton, MJ; McLachlan, AJ, 2014
)
" Based on the final model, DM affected the absorption rate constant (ka) and the volume of distribution (Vd) of rifampin."( Effects of type 2 diabetes mellitus on the population pharmacokinetics of rifampin in tuberculosis patients.
Chae, JW; Chang, MJ; Cho, YJ; Choi, HD; Kim, J; Lee, CT; Lee, JH; Lee, JI; Park, JS; Shin, WG; Yoon, HI; Yun, HY, 2015
)
"The bioavailability of rifampicin (RMP) decreases by ∼30% on interaction with isoniazid (INH) in stomach acid conditions, which can result in the development of drug resistance and treatment failure."( Comparative bioavailability of rifampicin and isoniazid in fixed-dose combinations and single-drug formulations.
Chen, MT; Chi, JY; Fu, L; Guo, SC; Hao, LH; Liu, CC; Lu, Y; Nie, WJ; Wang, B; Yang, W; Zhou, L; Zhu, H, 2014
)
"To compare the bioavailability in healthy volunteers of five anti-tuberculosis fixed-drug combinations (FDCs) used in China (formulations A-E) containing RMP and INH against single-drug formulations taken as reference."( Comparative bioavailability of rifampicin and isoniazid in fixed-dose combinations and single-drug formulations.
Chen, MT; Chi, JY; Fu, L; Guo, SC; Hao, LH; Liu, CC; Lu, Y; Nie, WJ; Wang, B; Yang, W; Zhou, L; Zhu, H, 2014
)
" This antibiotic is bactericidal and is orally bioavailable in mice."( Structure-activity relationship for the oxadiazole class of antibiotics.
Antunes, NT; Boudreau, MA; Chang, M; Ding, D; Lastochkin, E; Leemans, E; Lichtenwalter, K; Mobashery, S; O'Daniel, PI; Peng, Z; Pi, H; Schroeder, VA; Song, W; Spink, E; Suckow, MA; Testero, SA; Vakulenko, S; Wolter, WR, 2015
)
"2h) and low absolute bioavailability (1."( Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis.
Chaturvedi, V; Dasgupta, A; Gupta, AD; Jaiswal, S; Kashyap, VK; Khan, SR; Krishnan, MY; Lal, J; Roy, KK; Saxena, AK; Sharma, A; Sharma, SK; Singh, S; Sinha, S; Srivastava, R, 2015
)
"Decreases in the bioavailability of rifampicin (RFP) can lead to the development of drug resistance and treatment failure."( Relative bioavailability of rifampicin in four Chinese fixed-dose combinations compared with rifampicin in free combinations.
Chen, MT; Chi, JY; Fu, L; Guo, SC; Hao, LH; Liu, CC; Lu, Y; Nie, WJ; Wang, B; Yang, W; Zhou, L; Zhu, H, 2015
)
" The three two-drug FDCs (formulations B, C and D) displayed inferior RFP bioavailability compared with the reference (Chinese Clinical Trials registration number: ChiCTR-TTRCC-12002451)."( Relative bioavailability of rifampicin in four Chinese fixed-dose combinations compared with rifampicin in free combinations.
Chen, MT; Chi, JY; Fu, L; Guo, SC; Hao, LH; Liu, CC; Lu, Y; Nie, WJ; Wang, B; Yang, W; Zhou, L; Zhu, H, 2015
)
"An early prediction of solubility in physiological media (PBS, SGF and SIF) is useful to predict qualitatively bioavailability and absorption of lead candidates."( Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
Bharate, SS; Vishwakarma, RA, 2015
)
"14 times higher (in comparison to free RIF) plasma bioavailability with sustained levels for 5 days."( Nano-formulation of rifampicin with enhanced bioavailability: development, characterization and in-vivo safety.
Jindal, S; Kaur, IP; Sharma, G; Singh, H; Singh, M, 2015
)
" For PK studies, it was found that relative bioavailability (RB) was decreased to 22."( Combined effect of rifampicin-induced P-glycoprotein expression and lipopolysaccharide-induced intestinal sepsis on the effective permeability and pharmacokinetics of an anti-malarial candidate CDRI 97/78 in rats.
Hidau, MK; Krishna, J; Singh, SK; Singh, Y, 2015
)
"Bosutinib is an orally bioavailable dual Src/Abl tyrosine kinase inhibitor and a CYP3A4 enzyme substrate."( Effect of rifampin on the pharmacokinetics of bosutinib, a dual Src/Abl tyrosine kinase inhibitor, when administered concomitantly to healthy subjects.
Abbas, R; Boni, J; Sonnichsen, D, 2015
)
" Bioavailability decreases with increasing dose, yet high daily exposures are likely needed to improve efficacy and shorten the tuberculosis treatment duration."( Novel dosing strategies increase exposures of the potent antituberculosis drug rifapentine but are poorly tolerated in healthy volunteers.
Benson, CA; Cramer, Y; Dooley, KE; Dorman, SE; Haas, DW; Hafner, R; Hogg, E; Hovind, L; Janik, J; Marzinke, MA; Park, JG; Patterson, K; Savic, RM, 2015
)
" Tasimelteon is rapidly absorbed, with a mean absolute bioavailability of approximately 38%, and is extensively metabolized primarily by oxidation at multiple sites, mainly by cytochrome P450 (CYP) 1A2 and CYP3A4/5, as initially demonstrated by in vitro studies and confirmed by the results of clinical drug-drug interactions presented here."( Clinical assessment of drug-drug interactions of tasimelteon, a novel dual melatonin receptor agonist.
Baroldi, P; Dressman, MA; Kramer, WG; Ogilvie, BW; Torres, R, 2015
)
"Rifampicin is one of the frontline drugs for tuberculosis therapy but poor bioavailability of Rifampicin in combination with other anti-tuberculosis drugs is a subject of concern."( In vitro controlled release of Rifampicin through liquid-crystalline folate nanoparticles.
Misra, R; Mohanty, S; Parmar, R, 2015
)
" Thus, the results presented herein strongly indicate the potential of this scaffold for its use as multi-drug resistance reversal agent or bioavailability enhancer."( Discovery of 4-acetyl-3-(4-fluorophenyl)-1-(p-tolyl)-5-methylpyrrole as a dual inhibitor of human P-glycoprotein and Staphylococcus aureus Nor A efflux pump.
Bharate, JB; Bharate, SB; Joshi, P; Khan, IA; Kumar, A; Sharma, S; Singh, S; Vishwakarma, RA; Wani, A, 2015
)
" However, RIF in the IRPP group had a shorter Tmax and higher bioavailability than orally dosed groups."( Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs.
Edwards, D; Elbert, K; Garcia Contreras, L; Hickey, A; Ibrahim, M; Sung, J, 2015
)
" Using several drugs substances as an example, increased bioavailability and specific activity were demonstrated for the formulations equipped with such transport nanosystem."( [Pharmacological agents and transport nanosystems based on plant phospholipids].
Druzilovskaya, OS; Ignatov, DV; Ipatova, OM; Kasatkina, EO; Kudinov, VA; Medvedeva, NV; Prosorovskiy, VN; Tikhonova, EG,
)
"Many active substances are poorly water-soluble and pose a great challenge when orally administered because drug bioavailability is largely dependent on its solubility."( Impact of HPMC on the physical properties of spray-congealed PEG microparticles and its swelling effect on rifampicin dissolution.
Chan, LW; Heng, PW; Oh, CM; Ru Shan Siow, C, 2016
)
" These compounds have excellent oral bioavailability in preclinical species and exhibit pharmacodynamic effects of S1P1 antagonism in several in vivo models following oral dosing."( Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
Adam, A; Byth, K; Castriotta, L; Grewal, G; Hamilton, GA; Hennessy, EJ; Kamhi, VM; Lewis, P; Li, D; Lyne, P; Öster, L; Oza, V; Rooney, MT; Saeh, JC; Sha, L; Su, Q; Wen, S; Xue, Y; Yang, B, 2015
)
" Nonlinear mixed-effects modeling found that influential covariates for the pharmacokinetics were weight, sex, and a 30% increased bioavailability among heterozygous carriers of SLCO1B1 rs1104581 (previously associated with low rifampin concentrations)."( Effect of SLCO1B1 Polymorphisms on Rifabutin Pharmacokinetics in African HIV-Infected Patients with Tuberculosis.
Egan, D; Hennig, S; Kellerman, T; McIlleron, H; Naiker, S; Owen, A; Pym, A; Reddy, T; Wiesner, L, 2016
)
" Relative bioavailability in children was estimated at 49% lower compared to adults (100% relative bioavailability)."( A simultaneous population pharmacokinetic analysis of rifampicin in Malawian adults and children.
Davies, G; Dzinjalamala, FK; Khoo, S; Lopez, N; Mlota, R; Molyneux, E; Pertinez, H; Schipani, A; van Oosterhout, JJ; Ward, SA, 2016
)
" Simulations with apparent oral clearance increased by 71% and 36% and relative bioavailability decreased by 20% and 45% for darunavir and ritonavir, respectively, were performed for +rifampicin, 600 mg once daily (n = 1000)."( Simulation of the impact of rifampicin on once-daily darunavir/ritonavir pharmacokinetics and dose adjustment strategies: a population pharmacokinetic approach.
Back, D; Boffito, M; Dickinson, L; Khoo, S; Siccardi, M; Winston, A, 2016
)
" Apixaban absolute oral bioavailability was 49 % when administered alone and 39 % following induction by rifampin."( Effect of Rifampin on the Pharmacokinetics of Apixaban, an Oral Direct Inhibitor of Factor Xa.
Boyd, RA; Byon, W; Dias, C; Frost, C; LaCreta, F; Shenker, A; Vakkalagadda, B; Wang, J; Yu, Z; Zhang, D, 2016
)
"Co-administration of apixaban with rifampin reduced apixaban exposure via both decreased bioavailability and increased systemic clearance."( Effect of Rifampin on the Pharmacokinetics of Apixaban, an Oral Direct Inhibitor of Factor Xa.
Boyd, RA; Byon, W; Dias, C; Frost, C; LaCreta, F; Shenker, A; Vakkalagadda, B; Wang, J; Yu, Z; Zhang, D, 2016
)
" Absolute bioavailability of CLA was reduced from ∼40% to below 5% after comedication of RIF in both schedules of administration, and Tmax occurred ∼2-3 h earlier."( Pharmacokinetics and Pulmonary Distribution of Clarithromycin and Rifampicin after Concomitant and Consecutive Administration in Foals.
Berlin, S; Grube, M; Hasan, M; Keiser, M; Lumpe, S; Oswald, S; Siegmund, W; Spieckermann, L; Ullrich, A; Venner, M, 2016
)
" However, the Caco-2 cell transwell experiment showed that moxifloxacin could not affect the absorption rate of rifampicin."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
"P-glycoprotein ( P-GP: , encoding gene Abcb1) and Breast Cancer Resistance Protein ( BCRP: , encoding gene Abcg2) are transport proteins that play a major role in modulating the bioavailability of oral drugs in humans and rodents."( Potential pharmacokinetic effect of rifampicin on enrofloxacin in broilers: Roles of P-glycoprotein and BCRP induction by rifampicin.
Dai, X; Guo, M; Hu, D; Ren, W; Sun, Y; Wang, L; Zhang, Y, 2016
)
" Its bioavailability at an oral dose of 2 mg/kg was 15%."( Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
Beuerman, RW; Cao, D; Corkran, HM; Dick, T; Koh, JJ; Lakshminarayanan, R; Lim, F; Lin, S; Liu, S; Mukherjee, D; Stocker, BL; Tan, DTH; Tan, DZ; Tan, JK; Timmer, MSM; Zou, H, 2016
)
" Eventually, the rifampicin bioavailability was improved with depressed clearance in mice without gallbladders."( Effect of cholecystectomy on bile acids as well as relevant enzymes and transporters in mice: Implication for pharmacokinetic changes of rifampicin.
Duan, Y; Ma, Y; Qin, H; Rao, Z; Wei, Y; Wu, X; Xi, L; Zhang, F; Zhang, J; Zhao, Y, 2017
)
"One of the main obstacles to the successful treatment of tuberculosis is the poor and variable oral bioavailability of rifampicin (RIF), which is mainly due to its low hydrophilicity and dissolution rate."( Very fast dissolving acid carboxymethylcellulose-rifampicin matrix: Development and solid-state characterization.
Garro-Linck, Y; Luciani-Giacobbe, LC; Manzo, RH; Monti, GA; Olivera, ME; Ramírez-Rigo, MV, 2017
)
" Several factors like age, weight, gender, doses and formulations, gastro-intestinal disorders, ethnicity etc alter the absorption and bioavailability of rifampicin thus altering the drug levels."( Importance of Therapeutic Drug Monitoring of Rifampicin.
Amale, RA; Ashavaid, TF; Chawla, PK; Dherai, AJ; Lokhande, RV; Mahashur, AA; Naik, PR; Soman, R; Udwadia, ZF, 2016
)
" Compound 10a also displayed good pharmacokinetic profiles with oral bioavailability (F) of 41."( Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis.
Ding, K; Li, M; Liu, Z; Lu, X; Tang, J; Zhang, T; Zhang, X, 2016
)
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
" The addition of other orally bioavailable anti-staphylococcal agents to tedizolid may be unlikely to improve killing but further research is warranted to assess the impact of these combinations on resistance prevention, or against biofilm-embedded organisms."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
"Cavosonstat (N91115), an orally bioavailable inhibitor of S-nitrosoglutathione reductase, promotes cystic fibrosis transmembrane conductance regulator (CFTR) maturation and plasma membrane stability, with a mechanism of action complementary to CFTR correctors and potentiators."( Pharmacokinetics and safety of cavosonstat (N91115) in healthy and cystic fibrosis adults homozygous for F508DEL-CFTR.
Casey, A; Chmiel, JF; Donaldson, SH; Flume, PA; Mandagere, A; McCoy, K; Shoemaker, SA; Solomon, GM; Taylor-Cousar, JL; Troha, JM; Zeitlin, PL; Zemanick, ET, 2017
)
" We sought to test the hypothesis that markers of intestinal damage, bacterial translocation and systemic immune activation would relate to rifampicin bioavailability among HIV/TB patients."( Markers of gut dysfunction do not explain low rifampicin bioavailability in HIV-associated TB.
Bisson, GP; Gumbo, T; Modongo, C; Pasipanodya, J; Ravimohan, S; Srivastava, S; Tamuhla, N; Vinnard, C; Weissman, D; Zetola, NM, 2017
)
" Non-linear mixed-effects modelling was performed to determine whether variability in markers of gut damage, microbial translocation or systemic immune activation contributed to variability in rifampicin bioavailability before and after the initiation of ART."( Markers of gut dysfunction do not explain low rifampicin bioavailability in HIV-associated TB.
Bisson, GP; Gumbo, T; Modongo, C; Pasipanodya, J; Ravimohan, S; Srivastava, S; Tamuhla, N; Vinnard, C; Weissman, D; Zetola, NM, 2017
)
" In the non-linear mixed-effects model, we did not observe significant covariate effects of markers of gut damage, microbial translocation or immune activation on rifampicin bioavailability before and after ART initiation."( Markers of gut dysfunction do not explain low rifampicin bioavailability in HIV-associated TB.
Bisson, GP; Gumbo, T; Modongo, C; Pasipanodya, J; Ravimohan, S; Srivastava, S; Tamuhla, N; Vinnard, C; Weissman, D; Zetola, NM, 2017
)
"Rifaximin, a poorly absorbed antibiotics, has gut-specific therapeutic effects."( Emergence of rifampin-resistant staphylococci after rifaximin administration in cirrhotic patients.
Chang, JY; Joo, YH; Jung, HK; Jung, SA; Kim, SE; Kim, TH; Lee, J; Lee, KE; Lee, KH; Moon, CM; Ryu, MS; Shim, KN; Woo, SY, 2017
)
" MDR-TB treatment did not have a significant effect on the bioavailability, clearance, or absorption rate constants of lopinavir or ritonavir."( Pharmacokinetics and Drug-Drug Interactions of Lopinavir-Ritonavir Administered with First- and Second-Line Antituberculosis Drugs in HIV-Infected Children Treated for Multidrug-Resistant Tuberculosis.
de Kock, M; Denti, P; Garcia-Prats, AJ; Hesseling, AC; McIlleron, H; Norman, J; Schaaf, HS; Tikiso, T; van der Laan, LE; Wiesner, L; Winckler, J, 2018
)
"The nanosized rifampicin (RIF) has been prepared to increase the solubility in aqueous solution, which leads to remarkable enhancement of its bioavailability and their convenient delivery system studied by newly produced nontoxic, biodegradable magnetic iron oxide nanoparticles (MIONs) cross-linked polyethylene glycol hybrid chitosan (mCS-PEG) gel beads."( Magnetic iron oxide nanoparticles (MIONs) cross-linked natural polymer-based hybrid gel beads: Controlled nano anti-TB drug delivery application.
Annaraj, J; Ayyanaar, S; Dhaveethu Raja, J; Kesavan, MP; Rajesh, J; Sakthipandi, K; Vijayakumar, V, 2018
)
" These results suggest that rifapentine delivery via ASD with these cellulosic polymers may improve bioavailability in vivo."( Cellulose-based amorphous solid dispersions enhance rifapentine delivery characteristics in vitro.
Edgar, KJ; Mosquera-Giraldo, LI; Neilson, AP; Nichols, BLB; Novo, DC; Taylor, LS; Winslow, CJ, 2018
)
" Rifampicin, which is very effective against Mycobacterium tuberculosis, in both the phases of treatment, has certain concerns, which includes, decreased bioavailability with chronic use and hepatotoxicity."( A Randomized, Controlled, Phase III Clinical Trial to Evaluate the Efficacy and Tolerability of Risorine with Conventional Rifampicin in the Treatment of Newly Diagnosed Pulmonary Tuberculosis Patients.
Jagannath, K; Patel, A; Patel, M; Patel, N; Vora, A, 2017
)
"Exposure to nintedanib is increased by co-administration of ketoconazole and decreased by co-administration of rifampicin, likely due to effects on bioavailability of the absorbed fraction."( Effects of Ketoconazole and Rifampicin on the Pharmacokinetics of Nintedanib in Healthy Subjects.
Dallinger, C; Jungnik, A; Luedtke, D; Marzin, K; von Wangenheim, U, 2018
)
"We performed an open-label, three-way cross-over study of three licensed RMP-containing formulations widely used in South Africa to evaluate the bioavailability of RMP in a two-drug fixed-dose combination tablet (2FDC) and a four-drug FDC (4FDC) against a single-drug reference."( Quality assurance of rifampicin-containing fixed-drug combinations in South Africa: dosing implications.
Chirehwa, MT; Court, R; Kramer, N; McIlleron, H; Smythe, W; Wiesner, L; Wright, B, 2018
)
" The AUC0-12 of the 4FDC/reference (geometric mean ratio [GMR] 78%, 90%CI 69-89) indicated an average 20% reduction in RMP bioavailability in the 4FDC."( Quality assurance of rifampicin-containing fixed-drug combinations in South Africa: dosing implications.
Chirehwa, MT; Court, R; Kramer, N; McIlleron, H; Smythe, W; Wiesner, L; Wright, B, 2018
)
"Post-marketing surveillance of in vivo bioavailability of RMP and improved weight band-based dosing are recommended."( Quality assurance of rifampicin-containing fixed-drug combinations in South Africa: dosing implications.
Chirehwa, MT; Court, R; Kramer, N; McIlleron, H; Smythe, W; Wiesner, L; Wright, B, 2018
)
" Multidrug-resistance TB developed due to error in TB management in the past such as initiation of an inadequat regimen using first line anti-TB drugs, the addition of single drug to a failing regimen, the failure to identify pre-existing resistance and variations in bioavailability of anti-TB drugs that predispose the patient to the development of MDR-TB."( Risk Factors for Multidrug-resistant Tuberculosis.
Rumende, CM, 2018
)
" Our primary objectives were to: 1) refine the previously developed bosutinib PBPK model on the basis of the latest oral bioavailability data and 2) verify the refined PBPK model with P-glycoprotein kinetics on the basis of the bosutinib drug-drug interaction (DDI) results with ketoconazole and rifampin."( Application of Physiologically Based Pharmacokinetic Modeling in Understanding Bosutinib Drug-Drug Interactions: Importance of Intestinal P-Glycoprotein.
Costales, C; Kimoto, E; Loi, CM; Varma, MV; Yamazaki, S, 2018
)
" The low bioavailability of rifampicin (RIF), one of the vital constituent of antitubercular therapy, instigates an urge to develop nanocarrier, which can prevent its degradation in the acidic pH of the stomach."( Formulation, optimization, and characterization of rifampicin-loaded solid lipid nanoparticles for the treatment of tuberculosis.
Chokshi, NV; Khatri, HN; Patel, MM, 2018
)
" Pharmacokinetic studies indicate that 1 has an oral bioavailability with an average F-value of 27."( An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
Eslamimehr, S; Franzblau, SG; Kong, Y; Kurosu, M; Lemieux, MR; Mitachi, K; Park, F; Pressly, JD; Siricilla, S; Wang, Y; Yang, D, 2018
)
" Monotherapy with an orally bioavailable MptpB inhibitor reduces infection burden in acute and chronic guinea pig models and improves the overall pathology."( Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosis Survival and Infection Burden in Vivo.
Cavet, JS; Chakraborty, A; Fernandez, P; Gutierrez, MG; Kreiswith, BN; Kurepina, N; Naranjo, Y; Park, S; Perlin, DS; Pons, M; Saville, C; Schnettger, LS; Silva, APG; Tabernero, L; Thomas, EJ; Vickers, CF, 2018
)
" These compounds were found to be orally bioavailable and highly effective."( Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
Eswaran, S; Narayanan, S; Shivarudraiah, P; Shruthi, TG; Subramanian, S, 2019
)
"Tuberculosis (TB) chemotherapy witnesses some major challenges such as poor water-solubility and bioavailability of drugs that frequently delay the treatment."( HPMA-PLGA Based Nanoparticles for Effective In Vitro Delivery of Rifampicin.
Chauhan, DS; Gothwal, A; Gupta, U; Gupta, UD; Pachouri, PK; Pandey, PK; Rani, S, 2018
)
" It may be concluded that HPR-NPs holds promising potential for increasing solubility and bioavailability of RMP."( HPMA-PLGA Based Nanoparticles for Effective In Vitro Delivery of Rifampicin.
Chauhan, DS; Gothwal, A; Gupta, U; Gupta, UD; Pachouri, PK; Pandey, PK; Rani, S, 2018
)
"Tetrazole, a bioisostere of the carboxylic acid group, can replace the carboxyl group in drugs to increase the lipophilicity, bioavailability and reduce side effects."( Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
Chang, L; Ding, C; Feng, LS; Gao, C; Wu, X; Xu, Z; Yan, XF; Zhao, F, 2019
)
"0 h and the bioavailability was only 31."( [Effects of tannins in Galla Chinensis on pharmacokinetics of rifampicin in vivo and in vitro].
Chen, J; Dong, ZY; Huang, JM; Jin, R; Liu, YL; Tang, H; Wang, MS; Wang, Q; Ye, JC, 2018
)
"The formulation of the antituberculosis drug rifampicin embedded into 20-30 nm nanoparticles from soy phosphatidylcholine and sodium oleate, is characterized by greater bioavailability as compared with free drug substance."( [Increase of antituberculosis efficiency of rifampicin embedded into phospholipid nanoparticles with sodium oleate].
Ipatova, OM; Medvedeva, NV; Prozorovskiy, VN; Sanzhakov, MA; Tikhonova, EG; Torkhovskaya, TI; Zakharova, TS, 2018
)
"Anti-tuberculosis drug delivery has remained a challenge due to inconsistent bioavailability and inadequate sustained-release properties leading to treatment failure."( Lipopolysaccharide Polyelectrolyte Complex for Oral Delivery of an Anti-tubercular Drug.
Choonara, YE; Kumar, P; Pillay, V; Ramburrun, P; Sumaila, M, 2019
)
"One of the most effective strategies to enhance the bioavailability and the therapeutic effect of hydrophobic drugs is the use of nanocarriers."( Enhanced effects of curcumin encapsulated in polycaprolactone-grafted oligocarrageenan nanomicelles, a novel nanoparticle drug delivery system.
Bénard, S; Bhaw-Luximon, A; Casale, S; Catan, A; Couprie, J; Diotel, N; Gimié, F; Giraud, P; Jhurry, D; Koshel, D; Lallemand, L; Lefebvre D'Hellencourt, C; Meilhac, O; Meneyrol, V; Youssouf, L, 2019
)
" Thus, our modified drug delivery nanocomposites afforded higher drug bioavailability with large potential for fabrication as long-acting drug delivery nanocomposites, especially with hydrophobic drugs inducing the growth of osteoblastic bone cells."( Fabrication of bioactive rifampicin loaded κ-Car-MA-INH/Nano hydroxyapatite composite for tuberculosis osteomyelitis infected tissue regeneration.
Amarnath Praphakar, R; Rajan, M; Sam Ebenezer, R; Shakila, H; Sumathra, M; Vignesh, S, 2019
)
" Pretomanid pharmacokinetic behavior was described by a one-compartment model that at a given dose was linear in its absorption and clearance processes but where the rate of absorption and extent of bioavailability changed with dose."( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid.
Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 2019
)
"The therapeutic success of peptidic GLP-1 receptor agonists for treatment of type 2 diabetes mellitus (T2DM) motivated our search for orally bioavailable small molecules that can activate the GLP-1 receptor (GLP-1R) as a well-validated target for T2DM."( Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R).
Breitschopf, K; Defossa, E; Kurz, M; Lebreton, S; Li, Z; Lohmann, M; Löhn, M; Matter, H; Méndez, M; Mors, H; Podeschwa, M; Rackelmann, N; Riedel, J; Safar, P; Schäfer, M; Thorpe, DS; Weitz, D, 2020
)
" This strategy can enable efficient distribution of rifampicin within the lungs, localizing its action, enhancing its bioavailability and reducing its systemic exposure consequently side effects."( Rifampicin-Carbohydrate Spray-Dried Nanocomposite: A Futuristic Multiparticulate Platform For Pulmonary Delivery.
Elgindy, NA; Mehanna, MM; Mohyeldin, SM, 2019
)
"Presently, we provide a proof of the fact that the simultaneous oral administration of rifampicin (RIF), upon incorporation into solid lipid nanoparticles (RIF-SLNs), with isoniazid (INH) overcomes its INH-induced degradation and improves its oral bioavailability in rats."( Encapsulating Rifampicin into SLNs: A Viable Option for Managing its Bioavailability Issues Upon Co-Delivery with Isoniazid.
Bambal, R; Bhatnagar, PK; Chaira, T; Kaur, IP; Khanna, A; Singh, H; Singh, M; Sood, R; Upadhaya, DJ, 2020
)
"The results confirm the scope of combining RIF-SLNs with INH to overcome the bioavailability of free RIF when combined with INH, especially in fixed dose combinations."( Encapsulating Rifampicin into SLNs: A Viable Option for Managing its Bioavailability Issues Upon Co-Delivery with Isoniazid.
Bambal, R; Bhatnagar, PK; Chaira, T; Kaur, IP; Khanna, A; Singh, H; Singh, M; Sood, R; Upadhaya, DJ, 2020
)
" An absolute bioavailability study informed the hepatic and gastric availability."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
" The analyses demonstrate that meal affected the bioavailability, primary absorption rate constant, and zero order absorption time in the constructed model."( The Population Pharmacokinetics of Rifampicin in Japanese Pulmonary Tuberculosis Patients.
Atsuda, K; Kobayashi, M; Kohno, H; Koike, Y; Maruoka, D; Nagai, H; Nishimura, T, 2020
)
" This strategy allows for increasing the dissolution rate and improving the bioavailability of this BCS class II drug."( Rifampicin nanocrystals: Towards an innovative approach to treat tuberculosis.
Bou-Chacra, NA; Henostroza, MAB; Löbenberg, R; Melo, KJC, 2020
)
"Molibresib (GSK525762), an orally bioavailable small molecule with 2 major equipotent active metabolites, is being developed for the treatment of cancers."( An Adaptive Physiologically Based Pharmacokinetic-Driven Design to Investigate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of Molibresib (GSK525762) in Healthy Female Volunteers.
Collins, G; Ferron-Brady, G; Kremer, BE; Patel, A; Riddell, K; Schramek, D; Zhou, Y, 2021
)
"The in vivo release segregation of rifampicin (RIF) and isoniazid (INH) has been proposed as a strategy to avoid RIF acid degradation, which is known as one of the main factors for reduced RIF bioavailability and can result in drug-resistant tuberculosis."( Anti-tuberculosis site-specific oral delivery system that enhances rifampicin bioavailability in a fixed-dose combination with isoniazid.
Litterio, NJ; Lorenzutti, AM; Luciani-Giacobbe, LC; Olivera, ME; Ramírez-Rigo, MV, 2021
)
"Nadolol is a hydrophilic and nonselective β-adrenoceptor blocker with a bioavailability of 30%, relatively longer half-life, negligible metabolism, and predominant renal excretion."( Urinary Excretion of Nadolol as a Possible In Vivo Probe for Drug Interactions Involving P-Glycoprotein.
Kuroda, J; Misaka, S; Shimazaki, S; Shimomura, K, 2021
)
" The in vivo pharmacokinetic studies in sprague-dawley rats were performed and Mn-RIF-SLNs showed remarkable enhancement in terms of relative bioavailability (~17-folds) as compared to its drug solution via oral administration."( Fabrication and Characterization of Surface Engineered Rifampicin Loaded Lipid Nanoparticulate Systems for the Potential Treatment of Tuberculosis: An In Vitro and In Vivo Evaluation.
Bora, V; Chokshi, NV; Gajjar, S; Patel, BM; Patel, MM; Rawal, S; Solanki, D, 2021
)
" For both formulations, the intra-tracheal delivery led to significantly higher AUC compared to the oral delivery at the same dose suggesting higher rifampicin bioavailability from the inhaled route."( Pharmacokinetics of rifampicin after repeated intra-tracheal administration of amorphous and crystalline powder formulations to Sprague Dawley rats.
Das, SC; Dummer, J; Hill, PC; Katare, R; Khadka, P; Sinha, S; Tucker, IG, 2021
)
" This model was built based on physiochemical data and clinical in vivo drug-drug interaction (DDI) studies with itraconazole and fluconazole, and verified against data from an in vivo rifampicin DDI study and an absolute bioavailability study."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
" Following oral administration in mice, drug loaded StM exhibited highest distribution in macrophage rich organs, longer half-life, AUC, AUMC and MRT in comparison to isotactic nanomicelles indicating maximum bioavailability and efficacy of StM."( Polyethylene imine conjugated supramolecular stereocomplexed nanomicelles for intracellular delivery of rifampicin against Mycobacterium bovis.
Ali, S; Arshad, R; Aslam, A; Kiani, MH; Qadry, A; Shahnaz, G, 2021
)
" Rifampicin bioavailability was also lower in patients on concomitant ART."( Effect of efavirenz-based ART on the pharmacokinetics of rifampicin and its primary metabolite in patients coinfected with TB and HIV.
Äbelö, A; Ashton, M; Bienvenu, E; Sundell, J, 2021
)
" Most antibiotics active against Gram-positive cocci (GPC) exhibit both high oral bioavailability and bone diffusion."( Fully oral targeted antibiotic therapy for Gram-positive cocci-related periprosthetic joint infections: a real-life before and after study.
Beltrand, E; Blondiaux, N; Coehlo, A; Dezeque, H; Loiez, C; Migaud, H; Patoz, P; Putman, S; Robineau, O; Senneville, E; Titecat, M, 2021
)
" Antibiotics prescribed to our patients had high oral bioavailability and bone diffusion with rifampicin/fluoroquinolone combinations being the most frequent antibiotic regimens."( Fully oral targeted antibiotic therapy for Gram-positive cocci-related periprosthetic joint infections: a real-life before and after study.
Beltrand, E; Blondiaux, N; Coehlo, A; Dezeque, H; Loiez, C; Migaud, H; Patoz, P; Putman, S; Robineau, O; Senneville, E; Titecat, M, 2021
)
"Full oral targeted antibiotic therapy using a drug regimen with high oral bioavailability and good bone diffusion is an option for the treatment of patients with GPC-related PJIs."( Fully oral targeted antibiotic therapy for Gram-positive cocci-related periprosthetic joint infections: a real-life before and after study.
Beltrand, E; Blondiaux, N; Coehlo, A; Dezeque, H; Loiez, C; Migaud, H; Patoz, P; Putman, S; Robineau, O; Senneville, E; Titecat, M, 2021
)
" Bedaquiline bioavailability was 57% of that in adults."( Pharmacokinetics and Safety of Bedaquiline in Human Immunodeficiency Virus (HIV)-Positive and Negative Older Children and Adolescents With Rifampicin-Resistant Tuberculosis.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Hughes, JA; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; van der Laan, L; Wiesner, L; Winckler, JL, 2022
)
"Rifampicin is one of the most commonly used antibiotics for treating tuberculosis, but shows low bioavailability and requires long-term administration, and hence its use may result in severe side effects."( Optimization of rifampicin encapsulation in PLGA polymeric reservoirs.
Castañeda-Fernandez, C; Chávez-Santos, RM; Espitia-Pinzón, C; Kozina, A; Martínez, R; Silva-Miranda, M, 2022
)
"To assess the impact of diabetes mellitus on plasma concentration and bioavailability of rifampicin."( Impact of diabetes mellitus on rifampicin's plasma concentration and bioavailability in patients with tuberculosis: A systematic review and meta-analysis study.
El-Sheikh, SMA; Galal, AAA; Metwally, AS,
)
"Web of Science, Cochrane Library, PubMed and Scopus databases were screened until September 2020 on studies reported rifampicin's plasma concentration, bioavailability among diabetic tuberculosis patients and non-diabetic tuberculosis patients."( Impact of diabetes mellitus on rifampicin's plasma concentration and bioavailability in patients with tuberculosis: A systematic review and meta-analysis study.
El-Sheikh, SMA; Galal, AAA; Metwally, AS,
)
" There were no significant difference in rifampicin's maximum plasma concentration, event of low maximum plasma concentration, bioavailability and half-life between both groups."( Impact of diabetes mellitus on rifampicin's plasma concentration and bioavailability in patients with tuberculosis: A systematic review and meta-analysis study.
El-Sheikh, SMA; Galal, AAA; Metwally, AS,
)
"Diabetes mellitus attributed with 37% of low rifampicin's plasma concentration 2-h after administration but not influenced rifampicin's maximum plasma concentration, bioavailability and half-life."( Impact of diabetes mellitus on rifampicin's plasma concentration and bioavailability in patients with tuberculosis: A systematic review and meta-analysis study.
El-Sheikh, SMA; Galal, AAA; Metwally, AS,
)
" The model estimated an autoinduction of both rifampin bioavailability (0."( Effects of Enzyme Induction and Polymorphism on the Pharmacokinetics of Isoniazid and Rifampin in Tuberculosis/HIV Patients.
Äbelö, A; Ashton, M; Bienvenu, E; Birgersson, S; Sundell, J, 2022
)
"In order to clarify the effect of rifampicin on the bioavailability of the P-glycoprotein substrate talinolol, its absorption kinetics was modeled after multiple-dose oral administration of talinolol in healthy subjects."( Analysis of Complex Absorption After Multiple Dosing: Application to the Interaction Between the P-glycoprotein Substrate Talinolol and Rifampicin.
D'Argenio, DZ; Siegmund, W; Weiss, M, 2022
)
"Rifampicin changes the time course of absorption rate but not the fraction absorbed of talinolol."( Analysis of Complex Absorption After Multiple Dosing: Application to the Interaction Between the P-glycoprotein Substrate Talinolol and Rifampicin.
D'Argenio, DZ; Siegmund, W; Weiss, M, 2022
)
" To address this issue, we utilized a murine model of antibiotic-induced dysbiosis to assay the bioavailability of rifampicin, moxifloxacin, pyrazinamide, and isoniazid in mouse plasma over a period of 12 h following individual oral administration."( The Dysbiosis Triggered by First-Line Tuberculosis Antibiotics Fails to Reduce Their Bioavailability.
Dartois, V; Mittereder, LR; Namasivayam, S; Oland, S; Sher, A; Wang, H; Zimmerman, M, 2023
)
"We measured antibiotic penetration and bioavailability in staphylococcus biofilms using simulated humanized concentrations of fluorescent vancomycin plus or minus rifampin."( Staphylococcal biofilm: penetration and bioavailability of vancomycin with or without rifampin.
Antoci, V; Bleick, CR; Daffinee, KE; Garcia, D; LaPlante, KL; O'Neill, ET; Williams, G, 2023
)
"5% reduced bioavailability compared with the dispersible formulation, with no significant differences in other absorption parameters."( Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children.
Denti, P; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Palmer, M; Schaaf, HS; van der Laan, LE; Wiesner, L, 2023
)
"The dispersible paediatric levofloxacin formulation has improved bioavailability compared with the crushed non-dispersible adult formulation, but exposures remain below those in adults."( Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children.
Denti, P; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Palmer, M; Schaaf, HS; van der Laan, LE; Wiesner, L, 2023
)
"Esaxerenone was estimated to have high bioavailability (85."( Population pharmacokinetics of esaxerenone, a novel non-steroidal mineralocorticoid receptor blocker, in patients with essential hypertension, patients with diabetic nephropathy, and healthy volunteers.
Fukae, M; Ishizuka, H; Kastrissios, H; Shimizu, T; Wada, R; Yoshihara, K, 2023
)
" Age affected the bioavailability of rifampicin and isoniazid; at birth, children had 48."( Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis.
Aarnoutse, R; Chabala, C; Cotton, MF; Denti, P; Galileya, LT; Gibb, D; Hesseling, A; Lee, J; McIlleron, H; Njahira Mukui, I; Rabie, H; Turkova, A; Wasmann, RE; Zar, H, 2023
)

Dosage Studied

The efficacy at the currently approved dosage of 600 mg may be slightly lower than that of rifampin. Therapeutic simulations were performed with the full model to study the antibacterial effect of various dosage regimens of r ifampin in lungs.

ExcerptReference
" 48 h after dosage of [3H]rifampicin (33 mg/kg) to rats, 29-2 +/- 4-1 (S."( Implication of rifampicin-quinone in the irreversible binding of rifampicin to macromolecules.
Bolt, HM; Remmer, H, 1976
)
" Hence probenecid should not be used to reduce rifampicin dosage in antituberculosis therapy."( Probenecid and rifampicin serum levels.
Allan, GW; Fallon, RJ; Lees, AW; Smith, J; Tyrrell, WF, 1975
)
" But this effect is small and does not justify a change in the usual dosage of rifampicin."( [The use of mycobacteria in the estimation of the concentration of antibiotics, antimycotics and antituberculotics (author's transl)].
Iwainsky, H; Reutgen, H; Sesser, I, 1978
)
" Basing their comment on the published literature, they analyze the properties, pharmacology, toxicity, and side-effects of each medication, and define their dosage and modes of administration."( [Principles underlying the use of antituberculosis medication in children (author's transl)].
Besson-Leaud, M; Ollivier, A,
)
" The PZA dosage in blood and urine and pyrazinoic acid in urine were performed in a sample of 80 patients divided into 4 groups."( [Absorption and urinary elimination of pyrazinamid administered alone or in combination with isoniazid and rifampicin].
Bouhassen, H; Boulahbal, F; Khaled, S; Larbaoui, D,
)
"5% rifampin according to two dosage schedules."( Corneal penetration of rifampin.
Feldman, MF; Moses, RA, 1977
)
" The accumulation of a nontoxic drug in the eye is not necessarily of clinical significance, but ocular damage can occur in patients on long-term tricyclic agents when the amount, duration, and frequency of dosage are sufficiently high."( Ocular accumulation and toxicity of certain systemically administered drugs.
Mason, CG, 1977
)
" The 350 children were treated with 2 drugs, during the early years isoniazid and PAS and in the past 3 years isoniazid and rifampicin in standard dosage for either 12 or 18 months."( Occult tuberculous infection in children.
Fox, TG, 1977
)
" Both drugs given together have unchanged cinetics and with adapted dosing of isoniazide the hepatic accidents seem to disappear."( [New information on the metabolism of isoniazide and rifampicin. Their therapeutical consequences (author's transl)].
Canavate, A; Sainte-Laudy, J; Sauvaget, J, 1979
)
" It rests on an optimum dosage in connection with a best suited combination, taking into consideration the relations of sensitiveness and side effects as well as consequent long-term treatment."( [Modern therapy and after-care in urogenital tuberculosis].
Kalweit, H; Lenk, S; Rothkopf, M, 1978
)
" The renal elimination of apparent rifampicin can be used as a parameter for assessment of relative bioavailability of rifampicin from oral dosage forms of the same nominal strength if an appropriate number of volunteers is involved in the test."( The renal elimination of rifampicin as a function of the oral dose. A convenient way to assess relative bioavailability.
Brechbühler, S; Fluehler, H; Riess, W; Theobald, W, 1978
)
" The patient's cooperation during a systematic triple drug therapy in adequate dosage is important."( [Present status and treatment of urogenital tuberculosis].
Haubensak, K; Osterhage, HR, 1975
)
" With both 600 and 1200 mg rifampicin dosage the bacteriological results at the end of a year were similar (5% bacteriologically unfavourable in each group)."( A comparative study of daily followed by twice- or once-weekly regimens of ethambutol and rifampicin in the retreatment of patients with pulmonary tuberculosis: second report.
, 1976
)
" In the treatements with PAS Na and PRA the analysis of the frequencies of the cell carring chromosomal aberrations and of the chromosomal lesion types indicated a dose-response correlation."( Cytogenetic effect of some anti-tuberculosis drugs in vitro.
Georgian, L; Roman, IC, 1977
)
" Administration of this drug to two healthy subjects in a dosage of 600 mg daily for 28 days was associated with suppression of T-lymphocyte rosettes."( Suppression of T-lymphocyte rosettes by rifampin. Studies in normals and patients with tuberculosis.
Grieco, MH; Gupta, S; Siegel, I, 1975
)
" During this period, the prothrombin time (PT) rose remarkably little as the dosage of warfarin was increased."( Interaction of rifampin and warfarin.
Mann, RB; Self, TH, 1975
)
" This indicated that the dosage form of the granules and not PAS itself was responsible for the interaction, and that the dissolution of RMP was not involved."( Mechanism of the inhibitory effect of PAS granules on the absorption of rifampicin: adsorption of rifampicin by an excipient, bentonite.
Boman, G; Lundgren, P; Stjernström, G, 1975
)
"00 hr than at other dosing times."( Chronopharmacokinetics of rifampicin.
Avachat, MK; Rambhau, D; Rao, BR; Rao, JV; Rao, VV, 1992
)
" A dose-response experiment was performed with clarithromycin at 50, 100, 200, or 300 mg/kg of body weight administered daily by gavage to mice infected with approximately 10(7) viable MAC."( Activity of clarithromycin against Mycobacterium avium complex infection in beige mice.
Cynamon, MH; DeStefano, MS; Klemens, SP, 1992
)
" Both these antimicrobials seem appropriate for the treatment of meningitis caused by penicillin G-resistant pneumococci provided their dosage is adjusted to achieve adequate drug levels in the cerebrospinal fluid."( [Bacteriostatic activity and killing curves of eight antibiotics against seven strains of penicillin G-resistant pneumococci].
Barakett, V; Burghoffer, B; Delisle, F; Guidet, B; Lesage, D; Offenstadt, G; Petit, JC; Richard, G; Vergez, P, 1992
)
"We present a patient acutely ill from severe tuberculous meningo-encephalitis, in whom acute hepatic and renal failure, due to intercurrent septic shock, precluded the administration of full systemic dosage of antituberculous drugs."( Intraventricular rifampicin in severe tuberculous meningo-encephalitis.
D'Haens, J; Lauwers, S; Meysman, M; Verbeelen, D; Vincken, W, 1992
)
" Oral administration of rifampin at three times the intra-articular dosage was devoid of any therapeutic activity."( Clinical improvement in ankylosing spondylitis with rifamycin SV infiltrations of peripheral joints.
Caruso, I; Cazzola, M; Santandrea, S, 1992
)
" Monitoring of clinical response and blood drug concentrations is essential to adjust the drug dosage during rifampicin therapy."( Pharmacokinetic drug interactions with rifampicin.
Venkatesan, K, 1992
)
" A dose-response experiment was performed with a daily rifapentine dose of 10, 20 or 40 mg/kg administered intraperitoneally."( Activity of rifapentine against Mycobacterium avium infection in beige mice.
Cynamon, MH; Klemens, SP, 1992
)
" In order to solve this, we have been using antibiotic therapy with Rifampicin (Rifampin) for the last 2 years; the dosage is 20 mg/kg per day 1 h before surgery and then for 48 h after the surgical procedure."( Valvular infections in patients with hydrocephalus: preventive aspects.
Casagnas, M; Suárez, JC; Tregnaghi, M; Viano, JC, 1990
)
" On the basis of pharmacokinetic values, serum concentrations measured in this study, and published minimal inhibitory concentrations, the dosage of 20 mg of rifampin/kg, PO, every 24 hours should provide adequate serum concentrations for treatment of rifampin-susceptible bacterial infections in sheep."( Pharmacokinetics of rifampin in adult sheep.
Jernigan, AD; Rings, DM; Sams, RA; St Jean, GD, 1991
)
"By use of the mouse footpad technique, the susceptibility testing of 13 strains of Mycobacterium leprae to rifampicin (RFP) and the determination of minimal effective dosage (MED) were carried out."( The susceptibility testing of 13 strains of Mycobacterium leprae to rifampicin and the determination of minimal effective dosage.
Li, WZ; Shi, MQ; Wang, HY; Ye, GY; Yu, LC, 1991
)
" At a dosage of 25 mg/kg, minocycline was more active than clarithromycin at a dosage of 50 mg/kg."( Effectiveness of clarithromycin and minocycline alone and in combination against experimental Mycobacterium leprae infection in mice.
Grosset, JH; Ji, B; Perani, EG, 1991
)
" Dose-response relations and kinetics of killing of intracellular bacteria by antibiotics in the free and encapsulated form were studied under different conditions using J 774 mouse macrophages, because phagocytes from CGD patients are not available in great amounts."( Staphylococci surviving intracellularly in phagocytes from patients suffering from chronic granulomatous disease are killed in vitro by antibiotics encapsulated in liposomes.
Hockertz, S; Lohmann-Matthes, ML; Roesler, J; Vogt, B, 1991
)
"Comparative efficacy of the use of injection and oral dosage forms of rifampicin in the subtherapeutic doses in combination with peptidoglycan , an immunomodulator of microbial origin, was studied in respect to experimental anthracic infection with application of multifactorial analysis."( [Comparative multifactorial analysis of combined administration of injection and peroral forms of an antibiotic with a microbial immunomodulator in experimental anthrax].
Bodunkova, LE; Buravtseva, NP; Fomina, IP; Ivanitskaia, LP; Kogotkova, OI; Nikitin, AV, 1991
)
" Elderly patients are more sensitive to antituberculous (anti-TB) drugs; therefore, a modification in the dosage for this patient group should be considered."( The disposition of antituberculous drugs in plasma of elderly patients. II. Isoniazid, rifampicin and pyrazinamide.
Chan, HS; Chan, K; Walubo, A; Wong, CL; Woo, J, 1991
)
" drug abusers on levomethadon maintenance programs, adjustment of the levomethadon dosage may be necessary when specific therapy for HIV infection and associated diseases requires the use of drugs known to be potent inducers of the liver microsomal enzyme system."( Pharmacokinetic interaction of antimicrobial agents with levomethadon in drug-addicted AIDS patients.
Brockmeyer, NH; Goos, M; Mertins, L, 1991
)
" The peak concentration of rifampin produced by gavage was approximately 11/2 times higher than the maximum plasma concentration of the corresponding dosage in fresh diet."( Rifampin in drug-incorporated diet: effect of duration and temperature of storage. Relevance to drug-susceptibility testing in mice inoculated with M. leprae.
Abraham, B; Cariappa, A; Chacko, CJ, 1991
)
" A drug is likely to be particularly effective in widely spaced intermittent dosage if it has a long half-life and high bactericidal activity."( In vitro activities against mycobacteria of two long-acting rifamycins, FCE22807 and CGP40/469A (SPA-S-565).
Dickinson, JM; Mitchison, DA, 1990
)
" These data suggest that ciprofloxacin and rifampin may be given concomitantly in standard clinical dosing regimens."( Multiple-dose pharmacokinetics of concurrent oral ciprofloxacin and rifampin therapy in elderly patients.
Chandler, MH; Korvick, JA; Muder, RR; Rapp, RP; Toler, SM, 1990
)
" Daily dosing with 600 mg rifampicin for 22 days caused a three to eightfold increase in the 0-8 h urinary R/S ratio of mephenytoin following oral administration (100 mg) of racemic drug to extensive metabolizers of the anticonvulsant."( Induction of polymorphic 4'-hydroxylation of S-mephenytoin by rifampicin.
Anthony, LB; Wilkinson, GR; Wood, AJ; Zhou, HH, 1990
)
" The patient was able to maintain once-a-day dosing without incident even with steroid taper."( Rapid oral desensitization to isoniazid and rifampin.
Bielory, L; Holland, CL; Malasky, C; Ogunkoya, A, 1990
)
" These preliminary results indicate that MDT is effective in treatment of paucibacillary leprosy, and also that clinical cure can be achieved in much shorter duration, particularly with higher dosage of rifampicin."( Multidrug therapy for treatment of paucibacillary leprosy in western Kenya--preliminary communications.
Makokha, S; Nyawalo, J; Obura, M; Okelo, C; Okuku, P; Orege, PA, 1990
)
" The treatment schemes included daily intra-tonsillar++ injections of the dosage forms for 5 days."( [Evaluation of liposomal forms of rifampicin and prodigiozan in the treatment of experimental chronic tonsillitis].
Bazavluk, AD; Dikiĭ, IL; Filatov, VF; Iakovenko, VD; Tsyganenko, AIa; Vasil'chenko, VN, 1990
)
" The dosage of each drug was very similar whether it was given combined or separately."( Acceptability, compliance, and adverse reactions when isoniazid, rifampin, and pyrazinamide are given as a combined formulation or separately during three-times-weekly antituberculosis chemotherapy.
, 1989
)
" The main factors increasing the risk of hepatic toxicity was a high dosage of INH and overall malnutrition."( [Hepatotoxicity of the combination of isoniazid-rifampicin in African children. Role of malnutrition and HB virus].
Boguikouma, JB; Gahouma, D; Gendrel, D; Mouba, JF; Moussavou, A; Nardou, M, 1989
)
" Rifampin kinetics were measured at the end of the 22-day dosing period."( The kinetics of induction by rifampin of alpha 1-acid glycoprotein and antipyrine clearance in the dog.
Abramson, FP; Lutz, MP,
)
" In contrast, clindamycin was highly effective over a broad dosing range (8."( Comparison of clindamycin, rifampin, tetracycline, metronidazole, and penicillin for efficacy in prevention of experimental gas gangrene due to Clostridium perfringens.
Laine, BM; Maier, KA; Mitten, JE; Stevens, DL, 1987
)
" In the same subjects, rifabutin in the proposed therapeutic dosage (300 mg daily) for 7 days also enhanced the metabolic elimination of antipyrine, with preferential stimulation of the demethylation pathway, and increased the excretion of 6-beta-hydroxycortisol, but the magnitude of the effects was significantly less than after rifampicin."( Comparative effects of rifabutin and rifampicin on hepatic microsomal enzyme activity in normal subjects.
Frigo, GM; Grimaldi, R; Mönig, H; Ohnhaus, EE; Perucca, E; Sardi, A, 1988
)
" This difference should be taken into account when parameters of in-vitro efficacy are applied to establish dosage schedules."( The efficacy of rifampicin against Staphylococcus aureus in vitro and in an experimental infection in normal and granulocytopenic mice.
Hoogeterp, JJ; Krul, AM; Mattie, H; van Furth, R, 1988
)
" Based on these findings, pirmenol dosage adjustment will be required when pirmenol is given to patients concurrently receiving rifampin."( Enhanced pirmenol elimination by rifampin.
Cetnarowski, AB; Chang, T; Goldfarb, A; Lebsack, ME; Sedman, AJ; Stringer, KA, 1988
)
" A freshly made-up solution of this labile antibiotic in a daily dosage of 20 mg/kg iv did not affect mean graft survival time in a heterotopic heart transplant model."( Rifampicin quinone is an immunosuppressant, but not rifampicin itself.
Konrad, P; Stenberg, P, 1988
)
"Efficacy of a new rifampicin dosage form developed at the All-Union Research Institute of Antibiotics was studied on dogs with extensive destructive tuberculosis of the lungs."( [Effectiveness of soluble rifampicin in combination with other antibacterial preparations in treating disseminated destructive pulmonary tuberculosis in an experiment].
Bondarev, IM; Ivanov, VL; Kovaleva, LA; Mozhokina, GN; Novoselova, VP, 1987
)
" These findings were confirmed by dose-response curves calculated from fungal dry weight determinations of Rhizopus spp."( Synergistic action of amphotericin B and rifampin against Rhizopus species.
Christenson, JC; Guruswamy, A; Marks, MI; Shalit, I; Welch, DF, 1987
)
" Rifampin in a daily dose of 20 mg/kg (maximum 600 mg) for 4 days eradicated the carrier state in 86% of cases, as did the combination of rifampin at the same dosage and trimethoprim in a daily dose of 5 mg/kg (maximum 160 mg) for 4 days."( Rifampin alone or with trimethoprim for contacts of children with Haemophilus influenzae type b infections.
Bannatyne, RM; Cheung, R; Jadavji, T; Prober, CG, 1986
)
" Therapeutic activities of R-76-1 versus RMP and DL 473 versus RMP were compared, respectively, in the experimental infection of mice with Mycobacterium lepraemurium by different treatment schedules (immediate and delayed) and dosage regimens."( Antimycobacterial activities of two newer ansamycins, R-76-1 and DL 473.
Chen, JK; Hou, YH; Ji, BH; Lu, XZ; Ni, GX; Tang, QK; Wang, SY; Zhou, DH, 1986
)
"The bactericidal activity of the aminoglycoside antibiotics streptomycin and kanamycin for Mycobacterium leprae in mice was assessed, both alone and in combination with rifampin, utilizing various dosage schedules."( Further studies of the killing of M. leprae by aminoglycosides: reduced dosage and frequency of administration.
Gelber, RH, 1987
)
"A spectrophotometric method for the simultaneous determination of rifampin and isoniazid in dosage form is described."( Spectrophotometric estimation of rifampin-isoniazid mixture in dosage form.
Das, S; Sharma, SC; Talwar, SK,
)
" Self-induction of rifampin clearance by chronic dosing with the drug may lead to subtherapeutic levels of rifampin."( Pharmacokinetics of antituberculosis drugs in patients.
el-Attar, H; Israili, ZH; Rogers, CM, 1987
)
" In the first study, when isoniazid was prescribed daily in a dosage of 20 mg/kg, 39% of the patients developed jaundice; however, when the dosage was reduced to 12 mg/kg, the incidence fell to 16%."( Three chemotherapy studies of tuberculous meningitis in children.
Duraipandian, M; Nagarajan, M; Prabhakar, R; Ramachandran, P; Ramakrishnan, CV; Tripathy, SP, 1986
)
" ENL was also more frequent in regimens C and D and was not prevented by CLO in the dosage used."( Prospective study on the relationship between intensive bactericidal therapy and leprosy reactions.
Coussens, L; Groenen, G; Janssens, L; Kayembe, T; Nollet, E; Pattyn, SR, 1986
)
"An analysis carried out on the dosage schemes adopted in several controlled clinical trials in tuberculosis has indicated that preestablishing the daily doses of isoniazid, rifampicin, and pyrazinamide in the initial intensive phase results in large deviations of the doses administered from those considered appropriate in mg/kg body weight."( Short-course chemotherapy of pulmonary tuberculosis: a new approach to drug dosage in the initial intensive phase.
Acocella, G; Angel, JH, 1986
)
"Six foals from 6 to 8 weeks of age were given a single oral dose of rifampin at a dosage of 10 mg/kg of body weight."( Pharmacokinetics of rifampin given as a single oral dose in foals.
Brown, MP; Castro, LA; Gronwall, R; Houston, AE; Miles, N, 1986
)
" Of course, overall expense for the hospitalized patient includes costs of tests for monitoring for toxicity as well as administration costs, which are affected by the dosing frequency."( Choosing antimicrobials. Factors to consider, available agents.
Pankey, GA; Valainis, GT, 1985
)
" Minor adverse reactions occurred with similar frequencies during daily (5%) and intermittent (5%) treatment but in no case was modification of rifampicin dosage required."( Safety of thrice-weekly rifampicin for tuberculosis in South-East Asian refugees.
McKenzie, DK; Mukerjee, CM, 1985
)
" It would appear that dosage intervals may need to be shortened from 12 to 8 h during continuous therapy, and that periodic measurement of rifampin concentration may be required."( Pharmacokinetics of rifampin in children. I. Multiple dose intravenous infusion.
Koup, JR; Smith, AL; Weber, A; Williams-Warren, J, 1986
)
" This two-fold effect of rifampin offers an explanation for the discrepancy surrounding the dosage and species differences in hepatic induction reported in the literature."( Effects of rifampin pretreatment on hepatic parameters in the rabbit.
Iverson, F; Whitehouse, LW; Wong, LT,
)
" Despite the reduced dosage of thioamide, a 16."( Hepatotoxicity of the daily combination of 5 mg/kg prothionamide + 10 mg/kg rifampin.
Artus, JC; Cartel, JL; Grosset, JH; Naudillon, Y, 1985
)
" In patients receiving theophylline, blood levels should be monitored closely and dosage adjusted if rifampicin therapy is introduced or withdrawn."( Effect of rifampicin administration on theophylline pharmacokinetics in humans.
Gray, BJ; Jamieson, AP; Moxham, J; Powell-Jackson, PR; Williams, R, 1985
)
" Current dosage recommendations are based on total body weight (TBW); drug toxicity might result in obese patients receiving TBW doses."( Dosage of antituberculous drugs in obese patients.
Geiseler, PJ; Maddux, MS; Manis, RD, 1985
)
"A patient with Addison's disease required increased corticosteroid dosage whilst receiving rifampicin."( Changes in cortisol metabolism following rifampicin therapy.
Courtenay-Evans, RJ; Edwards, OM; Galley, JM; Hunter, J; Tait, AD, 1974
)
" The others received the same dosage of ethambutol and 450 mg."( Treatment of chronic drug-resistant pulmonary tuberculosis with rifampin and ethambutol.
Eidus, L; Jeanes, CW; Jessamine, AG, 1972
)
" An alteration in the dosage schedule is usually only necessary for drugs with a small therapeutic ratio."( Clinical implications of enzyme induction and enzyme inhibition.
Breckenridge, AM; Park, BK,
)
" The results suggest that the dosage of mexiletine should be adjusted when enzyme inducing drugs are started or stopped during therapy with it."( Effect of rifampicin treatment on the kinetics of mexiletine.
Hiltunen, HA; Koivula, IH; Pentikäinen, PJ, 1982
)
" The reduction in steady-state beta-adrenergic receptor drug concentration following enzyme induction is sufficiently large that an altered pharmacodynamic response would be expected if no dosage modification is made."( Enzyme induction and beta-adrenergic receptor blocking drugs.
Branch, RA; Herman, RJ, 1984
)
" Rifampin was given as sole therapy in a daily dosage of 600 to 1 200 mg."( [Treatment of human brucellosis with rifampicin].
Cabane, J; Fuchs, G; Godeau, P; Guillevin, L; Herson, S; Philippon, A; Tucat, G, 1984
)
" Additional pediatric pharmacokinetic studies are necessary to confirm the current dosage recommendation and use of these agents in the pediatric patient."( Clinical pharmacology of antitubercular drugs.
Blumer, JL; Reed, MD, 1983
)
" Prescribed at a daily dosage of 30 to 35 mg/kg (1,5 to 2 g daily), it gives no major side effects."( [Toxicity of pyrazinamide in antituberculous treatments (author's transl)].
Perdrizet, S; Pretet, S, 1980
)
" The most effective dosage was 20 mg of rifampin/kg given once daily for four days."( Rifampin alone and in combination with trimethoprim in chemoprophylaxis for infections due to Haemophilus influenzae type b.
Ambrosino, D; Boies, E; Daum, RS; Glode, MP; Goldmann, DA; Granoff, DM; Halsey, NA; Johansen, TL,
)
" Five different dosage combinations of the beta-lactam agent and rifampin were administered for a three-day period, and an attempt was made to correlate peak serum bactericidal titers with results of quantitative cultures of vegetations after therapy."( Rifampin in experimental endocarditis due to Staphylococcus aureus in rabbits.
Sande, MA; Scheld, WM; Zak, O,
)
" After an initial 2 week dosing period, all individuals additionally received 600 mg rifampicin daily for 3 weeks followed by a 4 week period during which again only the propranolol was given."( Induction of propranolol metabolism by rifampicin.
Herman, RJ; Nakamura, K; Wilkinson, GR; Wood, AJ, 1983
)
" In a controlled study of culture-positive advanced pulmonary tuberculosis we have compared treatment regimens with PZA in a dosage of less than 2 g and with ethambutol (EMB)."( [Pyrazinamide versus ethambutol in short-term therapy of lung tuberculosis. A randomized study].
Brändli, O; Fiala, W; Häcki, MA, 1983
)
" Therefore alteration in dosage regimes are not necessary in the undernourished."( Rifampicin kinetics in undernutrition.
Krishnaswamy, K; Murthy, KJ; Polasa, K, 1984
)
" When recommended dosage regiments are followed, the incidence of adverse reactions is low with short-course therapy, and in only 5% or less of patients is it necessary to withdraw one or more drugs."( Short-course therapy for tuberculosis.
Aquinas, M, 1982
)
" The cases were divided into 7 groups depending on the dosage and frequency of administration of RFP."( Rifampicin (RFP) trial in lepromatous leprosy.
Chulawala, RG; Juwatkar, PS; Koticha, KK; Pade, SS, 1982
)
" Simulation of plasma concentrations after different dosage regimens shows that a double rate of infusion--20 mg min-1 during 1 h and then 200 mg h-1--allows plasma concentrations to be quickly reached and maintained at a 20 mg L-1 level, far higher than the minimum inhibitory concentrations of most germs."( Pharmacokinetics of rifampicin and desacetylrifampicin in tuberculous patients after different rates of infusion.
Beucler, A; Brioude, R; Houin, G; Lafaix, C; Richelet, S; Tillement, JP, 1983
)
" Because of the marked reduction in the extent of bioavailability of total, and especially free, prednisolone, dosage adjustments should be made accordingly if prednisolone and rifampicin are prescribed concomitantly."( Changes in prednisolone pharmacokinetics and protein binding during treatment with rifampicin.
Bergrem, H; Refvem, OK, 1983
)
" Because of the marked reduction in total and especially free prednisolone, the dosage should be adjusted accordingly if prednisolone and rifampicin are prescribed concomitantly."( Altered prednisolone pharmacokinetics in patients treated with rifampicin.
Bergrem, H; Refvem, OK, 1983
)
"When dosing isoniazid in patients' serum after ingestion, the authors find a difference in the isoniazid levels when isoniazid is used alone, then, when isoniazid is used simultaneously with rifampicin."( [Antibacterian activity modifications of serum isoniazid when using it with rifampicin (author's transl)].
Bergogne-Berezin, E; Lafaix, C; Nouhouayi, A, 1982
)
" The PAE phenomenon may be of clinical importance with regard to dosage regimens in antimicrobial chemotherapy."( [Experimental study of optimal dose interval in antibiotic therapy].
Craig, WA; Gerber, AU, 1982
)
" At the end of treatment 6 of 11 patients given the lower dosage were cured clinically and bacteriologically compared to 8 of 9 given the higher dosage."( A study of the effectiveness of rifaprim in chronic prostatitis caused mainly by Staphylococcus aureus.
Daikos, GK; Giamarellou, H; Kosmidis, J; Leonidas, M; Papadakis, M, 1982
)
" Dosage of diazepam may require adjustment in patients with tuberculosis on chemotherapy."( Diazepam interaction with antituberculosis drugs.
Dengler, HJ; Greenblatt, DJ; Ochs, HR; Roberts, GM, 1981
)
"Ten healthy volunteers were given 'Rifaprim' in the dosage recommended for the treatment of urinary infections in man (rifampicin 300 mg + trimethoprim 80 mg in the morning and double these amounts at night, for 7 days)."( Rifaprim (rifampicin plus trimethoprim): pharmacokinetics and effects on the normal flora of man.
Brumfitt, W; Hamilton-Miller, JM,
)
" The normal dosage was 300 mg twice a day."( Intravenous use of rifampicin.
Boman, G; Nilsson, BS, 1981
)
"A 62-year-old man who had been taking 250 mg of chlorpropamide daily for several years received rifampin concomitantly and had a subsequent increased dosing requirement of chlorpropamide."( Interaction of rifampin and chlorpropamide.
Morris, T; Self, TH, 1980
)
" No major adverse events requiring dosage reduction or withdrawal of any study medication were seen in either treatment group."( A pilot study of antituberculosis combinations comparing rifabutin with rifampicin in the treatment of HIV-1 associated tuberculosis. A single-blind randomized evaluation in Ugandan patients with HIV-1 infection and pulmonary tuberculosis.
Kityo, C; Lutalo, T; Mateega, A; Mugerwa, R; Mugyenyi, P; Okwera, A; Rubaramira, R; Rüsch-Gerdes, S; Schwander, S; Tugume, S, 1995
)
" Analysis of data from previous studies in our laboratories shows that in the absence of intestinal metabolism, cyclosporine absorption from its presently available dosage form averages at least 65% +/- 12% in healthy volunteers and 77% +/- 19% in kidney transplant patients."( Differentiation of absorption and first-pass gut and hepatic metabolism in humans: studies with cyclosporine.
Benet, LZ; Gomez, DY; Gupta, SK; Hebert, MF; Rowland, M; Wacher, VJ; Wu, CY, 1995
)
" An intravenous dosage of 1g every 6 hours as initial therapy will be effective in most cases."( Treatment of Legionnaires' disease. Current recommendations.
Carreres, A; Domingo, C; Roig, J, 1993
)
" The fluoroquinolones were administered to simulate dosage regimens of 200 mg, 400 mg given intravenously (i."( Pharmacodynamics of levofloxacin, ofloxacin, and ciprofloxacin, alone and in combination with rifampin, against methicillin-susceptible and -resistant Staphylococcus aureus in an in vitro infection model.
Kaatz, GW; Kang, SL; McGrath, BJ; Rybak, MJ; Seo, SM, 1994
)
" Mouse hepatic microsomal mixed-function oxidase activity is markedly increased by repeated dosing with rifampicin, whereas administration of rifabutin may be ineffective."( Induction and autoinduction properties of rifamycin derivatives: a review of animal and human studies.
Dostert, P; Strolin Benedetti, M, 1994
)
" Pharmacokinetics of selected anti-infective agents are altered in hepatic disease, necessitating careful monitoring and dosage titration to avoid enhanced drug concentrations and risk of toxicity."( Anti-infective agents and hepatic disease.
Tschida, SJ; Vance-Bryan, K; Zaske, DE, 1995
)
" Therefore, dosing regimens designed for Caucasians can be extrapolated for other populations."( Determination of oral rifampin pharmacokinetic parameters in Mexicans and comparison with other populations: absence of evidence for interethnic variability.
Castañeda-Hernández, G; Flores-Murrieta, FJ; Herrera, JE; Hong, E, 1994
)
" Amphotericin B is often considered as the gold standard treatment despite its high toxicity particularly with high dosage (1-1."( [Curative treatment of invasive aspergillosis].
Dupont, B, 1994
)
" The activity of RPT was significantly enhanced when INH was added at the same dosing frequency."( Preventive therapy of tuberculosis with rifapentine in immunocompetent and nude mice.
Chapuis, L; Grosset, JH; Ji, B; O'Brien, RJ; Raviglione, MC; Truffot-Pernot, C, 1994
)
" When rifampin-prednisone treatment must be used in giant cell arteritis, we propose increasing the prednisone dosage to 2 mg/kg per day."( Rifampin-induced nonresponsiveness of giant cell arteritis to prednisone treatment.
Becq-Giraudon, B; Bouquet, S; Carrie, F; Delon, A; Roblot, F; Roblot, P, 1994
)
" The findings of this study suggest that prolonging the dosing interval by taking the PAE into account may not only lower the cost of antimicrobial therapy and the risk of toxicity, but also ensure the efficacy of subsequent doses."( Loss of bactericidal activities of quinolones during the post-antibiotic effect induced by rifampicin.
Meng, X; Nightingale, CH; Quintiliani, R; Sweeney, KR, 1994
)
" Increasing the wild-type mutS gene dosage resulted in a reversal of the mutator phenotype in about 60% of the mutant strains, indicating that the mutant and wild-type proteins compete."( Dominant negative mutator mutations in the mutS gene of Escherichia coli.
Marinus, MG; Wu, TH, 1994
)
" An adaptation of the rapid oral desensitization protocol for penicillin was used, with the dosing intervals increased to account for the different kinetics of these drugs."( Oral desensitization to rifampin and ethambutol in mycobacterial disease.
Borish, LC; Matz, J; Rosenwasser, LJ; Routes, JM, 1994
)
"The dose-response activity of rifabutin and the comparative activities of rifabutin and rifapentine were evaluated in the beige mouse model of disseminated Mycobacterium avium complex (MAC) infection."( Comparative in vivo activities of rifabutin and rifapentine against Mycobacterium avium complex.
Cynamon, MH; Grossi, MA; Klemens, SP, 1994
)
"310 patients with pulmonary tuberculosis disseminating bacteria received isoniazid, rifampicin, streptomycin (ethambutol) and pirazinamid in different regimens and dosage forms."( [Combined chemotherapy of patients with tuberculosis - new regimens and dosage forms].
Elistratova, NA; Khalbaeva, IV; Koriakin, VA; Sokolova, GB; Ziia, AV, 1993
)
" administration, we concur with the current dosage recommendation of 10 mg/kg twice a day by mouth."( Pharmacokinetics of single intravenous and single and multiple dose oral administration of rifampin in mares.
Kohn, CW; Kowalski, JJ; Powers, J; Sams, R; Wallace, S, 1993
)
" The formulation employed contained 125 mg of isoniazid (H), 100 mg of rifampicin (R) and 375 mg of pyrazinamide (Z) per tablet; six tablets were administered to every subject, giving a total dosage of 750 mg of isoniazid, 600 mg of rifampicin and 2,250 mg of pyrazinamide."( Bioavailability of isoniazid, rifampicin and pyrazinamide (in free combination or fixed-triple formulation) in intermittent antituberculous chemotherapy.
Acocella, G; Grassi, C; Grassi, GG; Luisetti, M; Peona, V; Pozzi, E, 1993
)
" The pharmacokinetics of vancomycin and clinical cure rates of peritonitis with different dosing guidelines have been studied extensively."( Pharmacokinetics and pharmacodynamics of antistaphylococcal antibiotics in continuous ambulatory peritoneal dialysis patients.
Keller, E, 1993
)
" Antibiotic dosing was adjusted for renal dysfunction."( Oral antibiotic treatment of right-sided staphylococcal endocarditis in injection drug users: prospective randomized comparison with parenteral therapy.
Daoud, EG; Flexner, C; Goodman, SN; Hartert, TV; Heldman, AW; Kowalski, TE; Lietman, PS; Petty, BG; Pompili, VJ; Ray, SC; Sisson, SD; Tidmore, WC; vom Eigen, KA, 1996
)
" The pits received daily during three weeks oral itraconazole at a dosage of 200 mg at the beginning of the meal, then during the next two weeks oral itraconazole combined with an intravenous administration of rifampin at a dosage of 10 mg/kg/day."( [Pharmacokinetic interaction between itraconazole and rifampin in Yucatan miniature pigs].
Cavalier, A; Elkhaili, H; Jehl, F; Kaltenbach, G; Levêque, D; Monteil, H; Peter, JD; Salmon, J; Salmon, Y, 1996
)
" In this study, we have been able to demonstrate the usefulness of a reproducible long-time antimicrobial dosage regime from the internal phase of the implant as compared to surface coated polymers."( Drug delivery concepts for the efficacious prevention of foreign-body infections.
Pulverer, G; Rump, A; Schierholz, JM, 1996
)
" However, the dosage and combinations to be used require further study."( Treatment of endocarditis with teicoplanin: a retrospective analysis of 104 cases.
Gaya, H; Wilson, AP, 1996
)
" We conclude that the efficacy and tolerability of RBT is equivalent to that of RMP in the treatment of newly diagnosed uncomplicated tuberculosis, and that RBT can be effectively administered in a part-daily, part-intermittent dosage schedule."( Efficacy and safety of rifabutin in the treatment of patients with newly diagnosed pulmonary tuberculosis.
Bredell, M; Felten, MK; Fourie, PB; Mabuza, B; McGregor, MM; Olliaro, P; Wolmarans, L, 1996
)
" These results suggest that rifampicin dosage adjustment may not be necessary when this drug is coadministered with fluconazole."( Lack of effect of fluconazole on the pharmacokinetics of rifampicin in AIDS patients.
Jaruratanasirikul, S; Kleepkaew, A, 1996
)
" The world's literature describing warfarin-rifampin interactions for the past 32 years was reviewed to suggest guidelines for warfarin dosage when rifampin is given simultaneously."( Inability to attain oral anticoagulation: warfarin-rifampin interaction revisited.
Casner, PR, 1996
)
" Each dosage form was administered, one after the other, to each subject in the morning after a fasted night period."( Bioequivalence study of two pharmaceutical forms of rifampicin capsules in man.
Barre, J; Benakis, A; Chouchane, N; Tillement, JP; Toumi, A,
)
"The population pharmacokinetics of dapsone were examined in human immunodeficiency virus-infected patients receiving dapsone at a dosage of 100 mg twice weekly for the prevention of Pneumocystis carinii pneumonia."( Population pharmacokinetics of dapsone administered biweekly to human immunodeficiency virus-infected patients.
Bassetti, D; Casazza, R; Cruciani, M; Gatti, G; Hossein, J; Karlsson, M; Merighi, M; Travaini, S, 1996
)
" Harvested plasma from serial blood samples collected after dosing on days 15, 16, and 30 was assayed for delavirdine and its N-desalkyl metabolite concentrations with a reversed-phase HPLC method."( Pharmacokinetic study of the interaction between rifampin and delavirdine mesylate.
Borin, MT; Carel, BJ; Chambers, JH; Freimuth, WW; Gagnon, S, 1997
)
"09 mumol/L) steady-state through drug concentrations in all patients after 2 weeks of concurrent dosing of delavirdine mesylate and rifampin."( Pharmacokinetic study of the interaction between rifampin and delavirdine mesylate.
Borin, MT; Carel, BJ; Chambers, JH; Freimuth, WW; Gagnon, S, 1997
)
" The pharmacokinetics of all three drugs in the plasma of 24 healthy males were studied as part of a randomized cross-over phase I study of two dosage forms."( Population pharmacokinetic modeling of isoniazid, rifampin, and pyrazinamide.
Bulpitt, AE; Jaresko, GS; Jelliffe, RW; Keung, AC; Peloquin, CA; Yong, CL, 1997
)
"Interest in determining plasma levels of rifampin for adjustment of dosage regimens has increased, but conflicting results exist concerning rifampin stability."( Stability of rifampin in plasma: consequences for therapeutic monitoring and pharmacokinetic studies.
Breteau, M; Gaudet, ML; Lamanetre, S; Le Guellec, C, 1997
)
" Therefore, rifampicin dosage adjustment for Thai patients may not be necessary."( The pharmacokinetics of oral rifampicin in AIDS patients.
Jaruratanasirikul, S, 1998
)
" We conclude that, at the dosage regimen used, CYP3A and Pgp responses to CYP3A inducers are regulated independently in rat liver."( Modulation of P-glycoprotein expression by cytochrome P450 3A inducers in male and female rat livers.
Benet, LZ; Salphati, L, 1998
)
" bovis Ravenel infection, three rifamycin derivatives gave "distinctive dose-response curves" in the correlation of dose sizes with the mean survival times or "log10CFU/lungs reductions"."( [Therapeutic efficacy of benzoxazinorifamycin KRM-1648 against experimental murine tuberculosis: (1). A study on the efficacy of short course treatment with the intratracheal and intravenous infection model].
Doi, N, 1998
)
" In mouse experiments, the activity of a single dose of the combination OFLO-MINO was dosage related; the higher dosage of the combination displayed bactericidal activity which was significantly inferior to that of a single dose of RMP, whereas the lower dosage did not exhibit a bactericidal effect."( Bactericidal activity of a single-dose combination of ofloxacin plus minocycline, with or without rifampin, against Mycobacterium leprae in mice and in lepromatous patients.
Diderot, V; Grosset, J; Ji, B; Lienhardt, C; Perani, E; Sow, S, 1998
)
" These safety and pharmacokinetic results suggest that no dosage adjustments for rifapentine are needed in patients with hepatic impairment."( Pharmacokinetics of rifapentine in patients with varying degrees of hepatic dysfunction.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" Biliary excretion was the major route of elimination of radioactivity in bile duct-cannulated rats dosed either po or IV."( Disposition and metabolism of rifapentine, a rifamycin antibiotic, in mice, rats, and monkeys.
Emary, WB; Huh, K; Mathews, B; Toren, PC, 1998
)
"Because the aged-related changes in the pharmacokinetic profile of rifapentine observed in this study were modest and unlikely to be associated with toxicity, no dosage adjustments for this antibiotic are recommended in elderly patients."( Single-dose pharmacokinetics of rifapentine in elderly men.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" Rifampicin therapy was administered orally, without any concomitant drug, with an effective dosage of 5-17 mg/kg/day."( Unexpected clinical remission of cholestasis after rifampicin therapy in patients with normal or slightly increased levels of gamma-glutamyl transpeptidase.
Cançado, EL; Carrilho, FJ; Laudanna, AA; Leitão, RM, 1998
)
" Undergoing therapy with a suitable dosage of rifampicin, none of the patients had a cholestatic crisis even during a period for as long as 12 months."( Unexpected clinical remission of cholestasis after rifampicin therapy in patients with normal or slightly increased levels of gamma-glutamyl transpeptidase.
Cançado, EL; Carrilho, FJ; Laudanna, AA; Leitão, RM, 1998
)
"A prospective, observational study of isoniazid (INH), rifampicin (RMP) and ethionamide (ETH) in a dosage of 20 mg/kg, and pyrazinamide (PZA) 40 mg/kg, all given once daily in hospital for 6 months."( Intensive short course chemotherapy in the management of tuberculous meningitis.
De Villiers, JN; Donald, PR; Pretorius, M; Schoeman, JF; Springer, P; Van Zyl, LE, 1998
)
" Based on these PK and safety data, no dosage adjustments for rifapentine based on gender are recommended."( Single-dose pharmacokinetics of rifapentine in women.
Eller, MG; Keung, AC; Weir, SJ, 1998
)
" To estimate the possible involvement of microbial degradation, rifampicin kinetics were also assessed in rats on day 8 after receiving multiple oral dosing and concurrent administration of nonabsorbable triple antibiotics for gut sterilization 3 days prior to the study day."( Assessment of presystemic factors on the oral bioavailability of rifampicin following multiple dosing.
Chiu, FC; Li, RC; Liu, XG; Zhang, JN; Zhu, M, 1998
)
"Based on the small changes in the pharmacokinetic parameters of dolasetron and its active metabolites, as well as the favorable safety results, no dosage adjustments for dolasetron mesylate are recommended with concomitant administration of cimetidine or rifampin."( Pharmacokinetics of dolasetron with coadministration of cimetidine or rifampin in healthy subjects.
Arumugham, T; Cramer, MB; Dimmitt, DC; Keung, A; Weir, SJ, 1999
)
" The pharmacokinetics of tacrolimus were obtained from serial blood samples collected over 96 hours, after single oral and intravenous administration prior to and during an 18-day concomitant rifampin dosing phase."( Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers.
Bekersky, I; Dressler, D; Fisher, RM; Hebert, MF; Marsh, CL, 1999
)
" Increases in amiodarone and desethylamiodarone concentrations were observed after an increase in the amiodarone dosage and discontinuation of rifampin."( Impact of rifampin on serum amiodarone concentrations in a patient with congenital heart disease.
Costanzo, MR; Fischer, SA; Porter, MT; Santucci, PA; Trohman, RG; Zarembski, DG, 1999
)
" Transfected cells were dosed with several known inducers of CYP3A4 and the levels of SPAP were measured."( A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human CYP3A4 gene in vitro.
Gibson, GG; Goldfarb, PS; Gray, TJ; Ogg, MS; Tarbit, M; Williams, JM, 1999
)
" Thus the microsphere formulations, administered in one or two doses, were able to achieve results in mice similar to those obtained with a daily drug regimen within the range of the highest clinically tolerated dosage in humans."( Efficacy of microencapsulated rifampin in Mycobacterium tuberculosis-infected mice.
Barrow, EL; Barrow, WW; Quenelle, DC; Staas, JK; Winchester, GA, 1999
)
" Although food increased the exposure of these patients to rifapentine, the infrequent dosing schedule for the treatment of tuberculosis (e."( Pharmacokinetics of rifapentine in subjects seropositive for the human immunodeficiency virus: a phase I study.
Eller, MG; Keung, AC; Nicolau, DP; Nightingale, CH; Owens, RC; Weir, SJ, 1999
)
" PZA is significantly dialyzed and should be dosed after hemodialysis."( The effect of hemodialysis on isoniazid, rifampin, pyrazinamide, and ethambutol.
Childs, JM; Fish, DN; Malone, RS; Peloquin, CA; Spiegel, DM, 1999
)
" The per cent increase in the ratio of 6beta-hydroxycortisol:cortisol following daily doses (+357%) was much higher compared with every 72-hour dosing (+236%)."( Enzyme induction observed in healthy volunteers after repeated administration of rifapentine and its lack of effect on steady-state rifapentine pharmacokinetics: part I.
Cheng, L; Eller, MG; Keung, A; McKenzie, KA; Reith, K; Weir, SJ, 1999
)
" In addition, the extended t(1/2) of rifapentine and its active metabolite support clinical investigation of once or twice-weekly rifapentine dosage regimens of rifapentine for the management of tuberculosis."( Single and multiple dose pharmacokinetics of rifapentine in man: part II.
Eller, MG; Keung, A; McKenzie, KA; Weir, SJ, 1999
)
" Our results demonstrate the use of human hepatocyte cultures to investigate the induction of cytochrome P-450 by xenobiotics in intact cells and stress the importance of large dose-response studies as well as the need to assess toxicity in these investigations."( The use of human hepatocyte cultures to study the induction of cytochrome P-450.
Dorko, K; Esplen, JE; Kostrubsky, VE; Ramachandran, V; Sinclair, JF; Strom, SC; Venkataramanan, R; Wrighton, SA; Zhang, S, 1999
)
" The results indicated elevations in the 6beta-OHF/F ratios that were dependent on both the dosing period and dose levels adopted."( Increase in urinary excretion of 6beta-hydroxycortisol in common marmosets as a marker of hepatic CYP3A induction.
Koyanagi, F; Manabe, S; Tanaka, K; Totsuka, S; Watanabe, T; Yasuda, M,
)
" Thus, lower concentration of RIF may be available for absorption leading to poor bioavailability of RIF from combination dosage forms (RIF+INH) as compared to formulations containing only RIF."( Stability of rifampicin in dissolution medium in presence of isoniazid.
Kotecha, JS; Rathod, IS; Savale, SS; Shah, PB; Shah, SA; Shishoo, CJ, 1999
)
" Its efficacy at the currently approved dosage of 600 mg may be slightly lower than that of rifampin."( Rifapentine: its role in the treatment of tuberculosis.
Nahata, MC; Temple, ME, 1999
)
" The optimum dosing regimen for rifapentine will have to be determined by controlled clinical trials."( Single-dose intrapulmonary pharmacokinetics of rifapentine in normal subjects.
Conte, JE; Golden, JA; Kipps, J; Lin, ET; McQuitty, M; Zurlinden, E, 2000
)
" Treatment had to be given up to three times a week for up to nine months, with any initial daily dosing period not more than one month, and was compared to daily dosing throughout for the same period."( Fully intermittent dosing with drugs for tuberculosis.
Mwandumba, HC; Squire, SB, 2000
)
" The most common dosage and duration for our patients were 20 mg/[kg x d] every 12 hours and 14 days, respectively."( Hepatosplenic cat-scratch disease in children: selected clinical features and treatment.
Arisoy, ES; Correa, AG; Kaplan, SL; Wagner, ML, 1999
)
" Treatment had to be given up to three times a week for up to nine months, with any initial daily dosing period not more than one month, and was compared to daily dosing throughout for the same period."( Fully intermittent dosing with drugs for tuberculosis.
Mwandumba, HC; Squire, SB, 2000
)
" Administered as single doses, MXFX in a dosage of 150 mg per kg was more active than OFLO in the same dosage, and displayed the same level of activity as RMP in a dosage of 10 mg per kg; the combination MXFX-minocycline (MINO) (MM) was more bactericidal than the combination OFLO-MINO (OM); RPT in a dosage of 10 mg per kg was more bactericidal than RMP administered in the same dosage, and even more active than the combination RMP-OFLO-MINO (ROM); the combination RPT-MXFX-MINO (PMM) killed 99."( Combination of rifapentine-moxifloxacin-minocycline (PMM) for the treatment of leprosy.
Grosset, J; Ji, B, 2000
)
" Rifater, which consists of rifampin, isoniazid, and pyrazinamide, was developed to assist patients in complying with their dosage schedules."( Three-in-one TB drug approved.
,
)
" Results show that RIF/PZA, dosed either daily or twice weekly, is as effective in preventing tuberculosis in dually-infected adults, as INH/pyridoxine given for 6-12 months."( Short course preventive therapy for tuberculosis is successful in HIV-infected patients.
Chaisson, RE, 1998
)
" The rifampicin and desacetylrifampicin content of complete urinary collections made from 0-4 and 4-8 hours after dosage were determined using both the HPLC and a much simpler colorimetric procedure."( The potential use of urinary excretion data for assessing the relative bioavailability of rifampicin in fixed dose combination anti-tuberculosis formulations.
Ellard, GA; Fourie, PB; Pillai, G; Smith, PJ, 2001
)
" A 233% increase in warfarin dosage over 4 months proved insufficient to attain a therapeutic INR during long-term rifampin therapy More aggressive titration of the warfarin dosage was needed."( Difficulties in anticoagulation management during coadministration of warfarin and rifampin.
Lee, CR; Thrasher, KA, 2001
)
" Treatment had to be given up to three times a week for up to nine months, with any initial daily dosing period not more than one month, and was compared to daily dosing throughout for the same period."( Fully intermittent dosing with drugs for treating tuberculosis in adults.
Mwandumba, HC; Squire, SB, 2001
)
" Rifampin dosage was increased again if blood levels were still subtherapeutic."( Utility of rifampin blood levels in the treatment and follow-up of active pulmonary tuberculosis in patients who were slow to respond to routine directly observed therapy.
Byrd, RP; Fountain, F; Mehta, JB; Morton, SE; Roy, TM; Shantaveerapa, H, 2001
)
" All six patients responded clinically, radiographically, and mycobacteriologically after an increase in rifampin dosage to reach target drug blood level."( Utility of rifampin blood levels in the treatment and follow-up of active pulmonary tuberculosis in patients who were slow to respond to routine directly observed therapy.
Byrd, RP; Fountain, F; Mehta, JB; Morton, SE; Roy, TM; Shantaveerapa, H, 2001
)
"Standard dosing with rifampin resulted in a poor clinical response and subtherapeutic serum levels in six patients."( Utility of rifampin blood levels in the treatment and follow-up of active pulmonary tuberculosis in patients who were slow to respond to routine directly observed therapy.
Byrd, RP; Fountain, F; Mehta, JB; Morton, SE; Roy, TM; Shantaveerapa, H, 2001
)
" Given that the lowest trough serum concentration of nevirapine exceeded by more than 40 times the protein binding adjusted median infective dose (IC(50)) of wild-type HIV in all patients, we suggest that there is no need to increase nevirapine dosage when it is given with rifampicin."( Pharmacokinetic interaction between nevirapine and rifampicin in HIV-infected patients with tuberculosis.
Crespo, M; Falco, V; Lopez, RM; Ocaña, I; Pahissa, A; Pou, L; Ribera, E; Ruiz, I, 2001
)
" These changes depended on drug dosage and duration, especially the severe influence on coagulation were detected when the RFP were reused after the ALT normalized in seventh to tenth months."( [Changes in blood coagulation affected by rifampicin administration].
Bu, R; Fang, X; Zhang, H, 1999
)
" ICR mice were divided to receive 4 daily oral dosing of either the dosing vehicle or 50 mg/kg of REM or RBT."( Induction of hepatic and presystemic metabolism of antipyrine in the mice: rifampicin versus rifabutin.
Li, RC; Liu, XG; Narang, PK,
)
" Further studies with increased rifapentine dosage are necessary."( Rifapentine and isoniazid in the continuation phase of a 6-month regimen. Final report at 5 years: prognostic value of various measures.
Chan, SL; Goodall, RL; Kam, KM; Mitchison, DA; Tam, CM, 2002
)
" Rifapentine 900-mg, once-weekly dosing appears to be safe and well tolerated and is being evaluated in Phase III efficacy trials of treatment of latent tuberculosis."( A prospective, randomized, double-blind study of the tolerability of rifapentine 600, 900, and 1,200 mg plus isoniazid in the continuation phase of tuberculosis treatment.
Bock, NN; Conwell, DS; Hamilton, CD; Mosher, A; Pachucki, C; Samuels, M; Sterling, TR; Vernon, A; Wang, YC, 2002
)
"A simple and accurate liquid chromatographic method was developed and validated for estimation of isoniazid (ISN), pyrazinamide (PYR) and rifampicin (RIF) in combined dosage forms."( Validation of a RP-LC method for the simultaneous determination of isoniazid, pyrazinamide and rifampicin in a pharmaceutical formulation.
Caccialanza, G; Calleri, E; De Lorenzi, E; Furlanetto, S; Massolini, G, 2002
)
" Overall, our results demonstrate that there is no gene dosage effect in the chloroplast and that transcript abundance is not limiting in the expression of chloroplast-encoded protein."( Searching limiting steps in the expression of chloroplast-encoded proteins: relations between gene copy number, transcription, transcript abundance and translation rate in the chloroplast of Chlamydomonas reinhardtii.
Drapier, D; Eberhard, S; Wollman, FA, 2002
)
"Although the minimal effective efavirenz plasma concentration that assures virological success is not currently known, it may be advisable to increase the dosage of efavirenz to 800 mg once daily when it is coadministered with rifampicin."( Pharmacokinetic interactions between efavirenz and rifampicin in HIV-infected patients with tuberculosis.
Alarcón-González, A; Gómez-Mateos, J; León-Jimenez, E; López-Cortés, LF; López-Pua, Y; Pachón, J; Ruiz-Valderas, R; Sarasanacenta, M; Viciana, P, 2002
)
" Treatment of transformants with various concentrations of rifampicin produced a dose-response curve with maximal induction at 10 microM (5."( A cell-based reporter gene assay for determining induction of CYP3A4 in a high-volume system.
Allen, SW; Raucy, J; Warfe, L; Yueh, MF, 2002
)
" The potential for alternative day or thrice weekly dosing with teicoplanin may offer further cost advantages whilst maintaining equivalent clinical effectiveness."( Cost-minimization analysis and audit of antibiotic management of bone and joint infections with ambulatory teicoplanin, in-patient care or outpatient oral linezolid therapy.
Ajdukiewicz, K; Barlow, GD; Clift, B; Davey, P; France, AJ; Gray, K; Morrison, J; Nathwani, D, 2003
)
" The dissolution characteristics of the extemporaneous powder for suspension were also compared to the dissolution profiles of commercially available anti-tuberculosis tablet dosage forms."( Pharmaceutical formulation of a fixed-dose anti-tuberculosis combination.
Danckwerts, MP; Ebrahim, S; Pillay, V, 2003
)
"The powder for suspension for rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride all compared favourably to the dissolution rate from the commercially available tablet dosage forms."( Pharmaceutical formulation of a fixed-dose anti-tuberculosis combination.
Danckwerts, MP; Ebrahim, S; Pillay, V, 2003
)
" Profiles of blood glucose concentration following repaglinide dosing were altered by less than 8% by both ketoconazole and rifampicin."( Influence of drugs interacting with CYP3A4 on the pharmacokinetics, pharmacodynamics, and safety of the prandial glucose regulator repaglinide.
Hansen, KT; Hatorp, V; Thomsen, MS, 2003
)
"05 mg/kg over a 30-minute period) and oral doses of midazolam (3-8 mg of a stable isotope, (15)N(3)-midazolam) before and after 7 days of rifampin dosing (600 mg once daily in the evening)."( The effect of age, sex, and rifampin administration on intestinal and hepatic cytochrome P450 3A activity.
Ambrosius, WT; Bruce, MA; Gorski, JC; Haehner-Daniels, B; Hall, SD; Hamman, MA; Vannaprasaht, S, 2003
)
" Further, effect of food on the rifampicin release was a function of dosage form characteristics such as disintegration time and dissolution rate, which will subsequently affect the release behavior of a formulation in presence of food."( In vitro evaluation of food effect on the bioavailability of rifampicin from antituberculosis fixed dose combination formulations.
Agrawal, S; Kaul, CL; Panchagnula, R; Rungta, S; Sancheti, P, 2003
)
" Imatinib pharmacokinetics were determined up to 96 h after dosing on day 1 (no induction) and on days 15-18 (during concomitant rifampicin)."( Effect of rifampicin on the pharmacokinetics of imatinib mesylate (Gleevec, STI571) in healthy subjects.
Bolton, AE; Capdeville, R; Hubert, M; Keller, U; Krebs-Brown, A; Peng, B; Seiberling, M, 2004
)
"Nebulization of nanoparticles-based ATDs forms a sound basis for improving drug bioavailability and reducing the dosing frequency for better management of pulmonary tuberculosis."( Poly (DL-lactide-co-glycolide) nanoparticle-based inhalable sustained drug delivery system for experimental tuberculosis.
Khuller, GK; Pandey, R; Prasad, B; Sharma, A; Sharma, S; Zahoor, A, 2003
)
"Patient non-compliance is the major drawback associated with the long-duration chemotherapy of tuberculosis (TB); hence, reduction in dosing frequency forms an important therapeutic strategy."( Nanoparticle encapsulated antitubercular drugs as a potential oral drug delivery system against murine tuberculosis.
Khuller, GK; Pandey, R; Sharma, S; Zahoor, A, 2003
)
" After re-starting treatment with EB and INH on Aug 24, RFP was added in small dosage (0."( [Agranulocytosis due to anti-tuberculosis drugs including isoniazid (INH) and rifampicin (RFP)--a report of four cases and review of the literature].
Akagawa, S; Baba, M; Kawabe, Y; Komatsu, H; Kurashima, A; Machida, K; Masuda, K; Nagai, H; Nagayama, N; Shishido, Y; Tamura, A; Yotsumoto, H, 2003
)
" There was no significant difference in the pharmacokinetic parameters of rifampicin as a component of Mairin-P and in combination with antitubercuous agents as free dosage forms."( [Assessment of the use of a multicomponent drug in the treatment of new cases of pulmonary tuberculosis].
Semenova, OV, 2003
)
" This interaction has a significant clinical relevance and may warrant dosage adjustment when celecoxib is co-administered with rifampicin in chronic treatment conditions, such as tuberculosis, leprosy and other infections of joints, bones, etc."( Influence of rifampicin pretreatment on the pharmacokinetics of celecoxib in healthy male volunteers.
Chandrasekhar, K; Jayasagar, G; Krishna Kumar, M; Madhusudan Rao, Y, 2003
)
" Hence, injectable PLG nanoparticles hold promise for increasing drug bioavailability and reducing dosing frequency for better management of tuberculosis."( Subcutaneous nanoparticle-based antitubercular chemotherapy in an experimental model.
Khuller, GK; Pandey, R, 2004
)
"Polymorphism of rifampicin has been postulated to be responsible for its variable bioavailability from solid oral dosage forms."( Solid-state characterization of rifampicin samples and its biopharmaceutic relevance.
Agrawal, S; Ashokraj, Y; Bharatam, PV; Panchagnula, R; Pillai, O, 2004
)
"Rifampicin shows variable bioavailability from solid oral dosage forms and the reasons for this variable absorption reported in literature varies from extrinsic formulations factors to intrinsic variability in rifampicin absorption."( Bioequivalence trials of rifampicin containing formulations: extrinsic and intrinsic factors in the absorption of rifampicin.
Agrawal, S; Bhade, S; Kaul, CL; Kaur, KJ; Panchagnula, R; Singh, I, 2004
)
"The problem of patient non-compliance in the management of tuberculosis (TB) can be overcome by reducing the dosing frequency of antitubercular drugs (ATD) employing drug carriers."( Lung specific stealth liposomes as antitubercular drug carriers in guinea pigs.
Khuller, GK; Pandey, R; Sharma, S, 2004
)
" Clostridium difficile was also isolated from the faeces of a third horse given an even lower dosage of erythromycin in combination with rifampicin."( The association of erythromycin ethylsuccinate with acute colitis in horses in Sweden.
Båverud, V; Franklin, A; Gunnarsson, A; Gustafsson, A; Lindholm, A; Rantzien, MH, 1997
)
" The impact of these variables should not be overlooked when clinical dosing regimens are optimized."( Post-antibiotic effect induced by an antibiotic combination: influence of mode, sequence and interval of exposure.
Li, RC; Tang, MC, 2004
)
" The effective therapeutic dosage of drugs could be reduced to half by supplementing HNP-1 in the therapeutic schedule."( Role of human neutrophil peptide-1 as a possible adjunct to antituberculosis chemotherapy.
Kalita, A; Khuller, GK; Verma, I, 2004
)
" Liver involvement of tuberculosis can have many facets and may be treated by gradual dosing of standard drugs."( Enlarged cervical lymph nodes and elevated liver chemistry tests: a therapeutic dilemma.
Dietrich, CG; Gartung, C; Geier, A; Lammert, F; Lorenzen, J; Matern, S; Wasmuth, HE,
)
" The results of the study therefore reveal that patients undergoing therapy had significantly greater DNA damage than untreated patients, indicating bacterial infection and drug therapy as the causal factors, since lepromatous-type disease is the more severe form with the patients having lower resistance to Mycobacterium leprae and requiring heavier and prolonged dosage of antibiotics."( DNA damage studies in untreated and treated leprosy patients.
Gandhi, G; Singh, B, 2004
)
" According to clinical and histopathological findings a diagnosis of tufted hair folliculitis was made and a treatment with oral rifampicin was started at the dosage of 450 mg twice per day."( Tufted hair folliculitis: complete enduring response after treatment with rifampicin.
Bottoni, U; Di Napoli, A; Grimaldi, M; Palese, E; Pranteda, G, 2004
)
" [3H]-verapamil was administered either nasally or via in situ brain perfusion, and dose-response profiles were constructed for P-gp inhibition."( Functional evidence for P-glycoprotein at the nose-brain barrier.
Graff, CL; Pollack, GM, 2005
)
" This is especially important, however, for a drug that is pivotal to a patient's well-being; its therapeutic effect should be carefully monitored when any new drug is added or a change in the dosage of a concurrent drug is made."( Exacerbation of panic disorder with rifampin therapy in a patient receiving citalopram.
Argo, TR; Carnahan, RM; Kukoyi, O, 2005
)
" Thus, nebulization of SLP-based antitubercular drugs forms a sound basis for improving drug bioavailability and reducing the dosing frequency for better management of pulmonary tuberculosis."( Solid lipid particle-based inhalable sustained drug delivery system against experimental tuberculosis.
Khuller, GK; Pandey, R, 2005
)
"The risk for ARR among HIV-infected persons with TB did not depend on the rifamycin used but, rather, on the rifampin dosing schedule in the intensive phase of treatment."( Relapse and acquired rifampin resistance in HIV-infected patients with tuberculosis treated with rifampin- or rifabutin-based regimens in New York City, 1997-2000.
Driver, CR; Li, J; Munsiff, SS; Sackoff, J, 2005
)
" However, it was found that the rate of dissolution in association with pH and the concentration-dependent absorption of rifampicin affects the in vivo performance of the dosage forms."( Implication of biopharmaceutics and pharmacokinetics of rifampicin in variable bioavailability from solid oral dosage forms.
Agrawal, S; Panchagnula, R, 2005
)
" It is advisable to increase the dosage of atorvastatin and preferable to administer it in the evening to guarantee adequate concentrations during the nighttime rapid cholesterol synthesis when rifampin or other potent inducers of cytochrome P450 3A4 are coadministered."( Rifampin markedly decreases and gemfibrozil increases the plasma concentrations of atorvastatin and its metabolites.
Backman, JT; Luurila, H; Neuvonen, M; Neuvonen, PJ, 2005
)
" Plasma efavirenz levels can be reduced by rifampicin, but the appropriate daily dosage of efavirenz is unclear."( Efavirenz levels and 24-week efficacy in HIV-infected patients with tuberculosis receiving highly active antiretroviral therapy and rifampicin.
Kiertiburanakul, S; Mahanontharit, A; Manosuthi, W; Prasithsirikul, W; Rattanasiri, S; Ruxrungtham, K; Sankote, J; Sungkanuparph, S; Thakkinstian, A; Vibhagool, A, 2005
)
" Plasma efavirenz levels were measured (at 12 h after dosing and on day 14) by high-performance liquid chromatography."( Efavirenz levels and 24-week efficacy in HIV-infected patients with tuberculosis receiving highly active antiretroviral therapy and rifampicin.
Kiertiburanakul, S; Mahanontharit, A; Manosuthi, W; Prasithsirikul, W; Rattanasiri, S; Ruxrungtham, K; Sankote, J; Sungkanuparph, S; Thakkinstian, A; Vibhagool, A, 2005
)
" Exposure to gefitinib is increased by coadministration with CYP3A4 inhibitors, but since gefitinib is known to have a good tolerability profile, a dosage reduction is not recommended."( Pharmacokinetic drug interactions of gefitinib with rifampicin, itraconazole and metoprolol.
Laight, A; Leadbetter, J; McKillop, D; Ranson, M; Smith, RP; Swaisland, HC; Wild, MJ, 2005
)
" We evaluated with the same model similar regimens in which we increased the dosing of rifapentine from 10 to 15 mg/kg of body weight and of moxifloxacin from 100 to 400 mg/kg."( Efficient intermittent rifapentine-moxifloxacin-containing short-course regimen for treatment of tuberculosis in mice.
Chauffour, A; Jarlier, V; Lounis, N; Truffot-Pernot, C; Veziris, N, 2005
)
" Patients were included in the study if they had been receiving first-line antimycobacterial therapy (rifampin, isoniazid, pyrazinamide, and ethambutol) for not less than 4 weeks and not more than 6 weeks and were divided into three RFP dosage groups based on weight: 600 mg, <45 kg; 750 mg, 46 to 55 kg; and 900 mg, >55 kg."( Population pharmacokinetics of rifapentine and its primary desacetyl metabolite in South African tuberculosis patients.
Langdon, G; McFadyen, L; McIlleron, H; Simonsson, US; Smith, P; Wilkins, J, 2005
)
" Thus, SLN based antitubercular drug therapy forms a sound basis for reducing dosing frequency and improving patient compliance for better management of tuberculosis."( Oral solid lipid nanoparticle-based antitubercular chemotherapy.
Khuller, GK; Pandey, R; Sharma, S,
)
"Serum drug concentrations were determined 2, 6, and 10 h after dosing in 36 HIV-infected patients with TB who were taking rifampin and in 49 who were taking ethambutol."( The clinical pharmacokinetics of rifampin and ethambutol in HIV-infected persons with tuberculosis.
Hafner, R; Peloquin, CA; Perlman, DC; Rainey, PM; Remmel, RP; Rosenkranz, S; Salomon, N; Segal, Y, 2005
)
"With daily dosing of rifampin (600 mg), 26 (77%) of 34 patients (95% confidence interval [CI], 59%-89%]) had a low maximum concentration of rifampin (<8 microg/mL), and 12 (35%; 95% CI, 20%-54%) had a very low maximum concentration (<4 microg/mL)."( The clinical pharmacokinetics of rifampin and ethambutol in HIV-infected persons with tuberculosis.
Hafner, R; Peloquin, CA; Perlman, DC; Rainey, PM; Remmel, RP; Rosenkranz, S; Salomon, N; Segal, Y, 2005
)
" The optimal efavirenz dosage is still unclear."( Efavirenz 600 mg/day versus efavirenz 800 mg/day in HIV-infected patients with tuberculosis receiving rifampicin: 48 weeks results.
Kiertiburanakul, S; Manosuthi, W; Rattanasiri, S; Ruxrungtham, K; Sungkanuparph, S; Thakkinstian, A; Vibhagool, A, 2006
)
" Rifampicin was administered orally in a 600 mg daily dosage for at least 60 days."( Old drug--new indication. Rifampicin in psoriasis.
Grozdev, I; Kkzandjieva, J; Tsankov, N, 2006
)
" Further studies are required to assess the implications of variations in antituberculosis drug concentrations for efficacy and safety before decisions are made to change the dosing strategy in patients at risk."( Determinants of rifampin, isoniazid, pyrazinamide, and ethambutol pharmacokinetics in a cohort of tuberculosis patients.
Burger, A; Folb, PI; McIlleron, H; Norman, J; Smith, P; Wash, P, 2006
)
" Hence, the study suggests that co-administration of Rp and H should be avoided, like in case of R and H, and the two drugs should not be formulated directly into a single dosage form."( Study of the interaction between rifapentine and isoniazid under acid conditions.
Bhutani, H; Prasad, B; Singh, S, 2006
)
" Alginate nanoparticles hold great potential in reducing dosing frequency of antitubercular drugs."( Pharmacokinetic and pharmacodynamic behaviour of antitubercular drugs encapsulated in alginate nanoparticles at two doses.
Ahmad, Z; Khuller, GK; Pandey, R; Sharma, S, 2006
)
" The area under the plasma concentration-time curve (AUC(0-infinity)) for ATV also increased significantly after intravenous dosing of ATV with RIF, but the extent was much less than that observed for oral ATV dosing."( Pharmacokinetics of atorvastatin and its hydroxy metabolites in rats and the effects of concomitant rifampicin single doses: relevance of first-pass effect from hepatic uptake transporters, and intestinal and hepatic metabolism.
Benet, LZ; Huang, Y; Lau, YY; Okochi, H, 2006
)
"A significant difference in dose-normalized area under the curves (AUC0-n and AUC0-infinity) was observed between children receiving the 150 and 300 mg doses, which was accounted for by differences in age between the dosing arms."( Pharmacokinetics of rifapentine in children.
Abdel-Rahman, SM; Blake, MJ; Jacobs, RF; Kearns, GL; Lowery, NK; Sterling, TR, 2006
)
" We concluded that polymeric nanoparticle based oral 4-drug combination bears significant potential to shorten the duration of TB chemotherapy, besides reducing the dosing frequency."( Chemotherapeutic efficacy of nanoparticle encapsulated antitubercular drugs.
Khuller, GK; Pandey, R; Sharma, S,
)
" Pyridoxine is preventative in low dosage and curative in high dosage."( [Isoniazid induced neuropathy: consider prevention].
De Broucker, T; Martinez-Almoyna, L; Steichen, O, 2006
)
" P-glycoprotein expression and transport activity in brain capillaries from transgenic mice was significantly increased when capillaries were exposed to the hPXR ligands, rifampin and hyperforin, in vitro and when the mice were dosed with rifampin in vivo."( In vivo activation of human pregnane X receptor tightens the blood-brain barrier to methadone through P-glycoprotein up-regulation.
Bauer, B; Hartz, AM; Kalvass, JC; Miller, DS; Olson, ER; Pollack, GM; Yang, X; Zhao, R, 2006
)
"Because rifampin (RIF) induces hepatic enzymes and inhibits uptake transporters, dosing a drug that is a dual substrate of enzymes and uptake transporters on the final day of an inducing regimen should exhibit less inductive effect than dosing on the following day in the absence of RIF, since RIF decreases drug uptake into liver."( Elucidating the effect of final-day dosing of rifampin in induction studies on hepatic drug disposition and metabolism.
Benet, LZ; Lam, JL; Okochi, H; Shugarts, SB, 2006
)
" Atazanavir (ATV) has clinical efficacy comparable to a standard of care regimen in naive patients and, when dosed with low-dose ritonavir (RTV), also in treatment-experienced patients."( Effect of rifampin on steady-state pharmacokinetics of atazanavir with ritonavir in healthy volunteers.
Agarwala, S; Been-Tiktak, A; Bertz, R; Burger, DM; Child, M; Wang, Y, 2006
)
" More research is needed to determine well-founded dosing guidelines."( Pharmacokinetics of intravenous rifampicin (rifampin) in neonates.
Degraeuwe, PL; Neef, C; Pullen, J; Stolk, LM; van Tiel, FH; Zimmermann, LJ, 2006
)
"Currently recommended compendial dissolution methods for quality control of orally administered solid dosage forms of rifampicin containing formulations are not found to be able to forecast the in vivo performance."( Dissolution testing of marketed rifampicin containing fixed dose combination formulations using a new discriminative media: a post marketing retrospective study.
Agrawal, S; Ashokraj, Y; Kumar Bajpai, A; Panchagnula, R, 2006
)
" Twice-daily dosing or higher saquinavir doses in once-daily administration should be tested to obtain more appropriate plasma levels."( Pharmacokinetic interaction between rifampicin and the once-daily combination of saquinavir and low-dose ritonavir in HIV-infected patients with tuberculosis.
Azuaje, C; Colomer, J; Crespo, M; Curran, A; Domingo, P; Falcó, V; Feijoo, M; Lopez, RM; Lopez-Colomes, JL; Ocaña, I; Pahissa, A; Pou, L; Ribera, E; Sambeat, MA; Sánchez, P, 2007
)
" We determined peak concentration ranges for each drug and acetylisoniazid/isoniazid and 25-desacetylrifampicin/rifampicin ratios by analyzing 2-h post-dose samples in patients treated with standard dosing as a first-line treatment."( Simultaneous determination of first-line anti-tuberculosis drugs and their major metabolic ratios by liquid chromatography/tandem mass spectrometry.
Jun, SH; Kim, JQ; Lee, JH; Park, KU; Song, J; Song, SH; Yoon, Y, 2007
)
" Depending on the intended indication and dosing regimen, PPL can delay or stop development of a compound in the drug discovery process."( Evaluation of a published in silico model and construction of a novel Bayesian model for predicting phospholipidosis inducing potential.
Gehlhaar, D; Greene, N; Johnson, TO; Pelletier, DJ; Tilloy-Ellul, A,
)
" Although the advantage of aminoglycosides is easily achieved high blood concentration, if aminoglycoside dosage is exceed 15 mg/kg, the possibility of auditory disturbance increase."( [Perspective of pulmonary MAC infection treatment].
Kurashima, A, 2007
)
"Patients were treated in a controlled clinical trial with 2HRZE3/6HE with thrice-weekly direct dosing in the intensive phase and once-weekly with six doses self-administered in the continuation phase."( Evaluation of a non-rifampicin continuation phase (6HE) following thrice-weekly intensive phase for the treatment of new sputum positive pulmonary tuberculosis.
, 2007
)
" The ability to measure rifampicin drug concentrations in both plasma and in cells may be useful in evaluating the suitability of dosage regimens for populations and individuals."( A rapid and sensitive HPLC-MS method for the detection of plasma and cellular rifampicin.
Ardrey, A; Ashleigh, S; Back, DJ; Chaponda, M; Davies, G; Hartkoorn, RC; Khoo, S; Tjia, JF; Waitt, CJ; Ward, SA, 2007
)
"In the treatment of tuberculosis with rifampicin in patients treated with prednisolone and cyclosporine, we have to increase the dosage of these drugs."( [Examination of administrative dosage of cyclosporine during anti-tuberculosis chemotherapy including rifampicin].
Akagawa, S; Kawabe, Y; Kawashima, M; Kurashima, A; Machida, K; Masuda, K; Matsui, Y; Nagai, H; Nagayama, N; Suzuki, J; Tamura, A; Yotsumoto, H, 2007
)
" Prednisolone had been also administrated in all patients and the dosage was doubled from the beginning of the treatment."( [Examination of administrative dosage of cyclosporine during anti-tuberculosis chemotherapy including rifampicin].
Akagawa, S; Kawabe, Y; Kawashima, M; Kurashima, A; Machida, K; Masuda, K; Matsui, Y; Nagai, H; Nagayama, N; Suzuki, J; Tamura, A; Yotsumoto, H, 2007
)
"The appropriate dosage of cyclosporine was found to be approximately 3 times that of the initial dosage in all patients, but it required a long-term and frequent measurements of trough levels before reaching this goal."( [Examination of administrative dosage of cyclosporine during anti-tuberculosis chemotherapy including rifampicin].
Akagawa, S; Kawabe, Y; Kawashima, M; Kurashima, A; Machida, K; Masuda, K; Matsui, Y; Nagai, H; Nagayama, N; Suzuki, J; Tamura, A; Yotsumoto, H, 2007
)
" This system was used to modulate dosage during combined therapy with RFP and CAM."( [Measurement of rifampicin and clarithromycin in serum by high-performance liquid chromatography with electrochemical detection].
Nakagawa, T; Nikai, T; Ogawa, K; Taki, H, 2007
)
" In current recommendations the dosage of EMB is calculated per kg body weight."( Ethambutol in paediatric tuberculosis: aspects of ethambutol serum concentration, efficacy and toxicity in children.
Detjen, A; Magdorf, K; Quarcoo, D; Thee, S; Wahn, U, 2007
)
"To present two studies investigating an appropriate EMB dosage in children, and observational data on its toxicity and efficacy."( Ethambutol in paediatric tuberculosis: aspects of ethambutol serum concentration, efficacy and toxicity in children.
Detjen, A; Magdorf, K; Quarcoo, D; Thee, S; Wahn, U, 2007
)
" It appears to be more valid to calculate the EMB dosage on the basis of body surface rather than body weight, leading to higher dosages especially in younger children."( Ethambutol in paediatric tuberculosis: aspects of ethambutol serum concentration, efficacy and toxicity in children.
Detjen, A; Magdorf, K; Quarcoo, D; Thee, S; Wahn, U, 2007
)
"The aim of the present investigation was to develop a novel dosage form of rifampicin and isoniazid to minimize degradation of rifampicin in acidic medium and to modulate the release of rifampicin in the stomach and isoniazid in the intestine."( A novel solid dosage form of rifampicin and isoniazid with improved functionality.
Gohel, MC; Sarvaiya, KG, 2007
)
" In addition, applying the pharmacodynamic approach and dose-response analysis, we aimed to describe the nature of potential interactions of tested azole antimycotics coadministered with a prototypical PXR ligand rifampicin in transactivation of CYP3A4 gene."( Azole antimycotics differentially affect rifampicin-induced pregnane X receptor-mediated CYP3A4 gene expression.
Anzenbacher, P; Anzenbacherova, E; Burysek, L; Cerveny, L; Dvorak, Z; Grim, J; Kunes, J; Pavek, P; Pour, M; Staud, F; Svecova, L; Trejtnar, F; Vrzal, R, 2008
)
" Sometimes literature references are submitted to the FDA to support dosing recommendations."( Are literature references sufficient for dose recommendations? An FDA case study of efavirenz and rifampin.
Chan-Tack, KM; DiGiacinto, JL; Reynolds, KS; Robertson, SM; Struble, KA, 2008
)
" From days 6-15, volunteers were randomized to receive lopinavir/ritonavir tablets dosed as either 600/150 or 800/200 mg twice daily, both in addition to 600 mg rifampicin once daily."( High incidence of adverse events in healthy volunteers receiving rifampicin and adjusted doses of lopinavir/ritonavir tablets.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Koopmans, PP; L'homme, RF; Nijland, HM; Rongen, GA; van Crevel, R; van Uden, P, 2008
)
" In contrast, fractionation of the dose at a free AUC associated with a static effect indicated that once daily dosing was superior."( Pharmacodynamics of minocycline against Staphylococcus aureus in an in vitro pharmacokinetic model.
Bowker, KE; Macgowan, AP; Noel, AR, 2008
)
"The need to investigate novel dosing regimens and combinations is essential in combating poor treatment outcomes for Staphylococcus aureus bacteremia and endocarditis."( Evaluation of daptomycin pharmacodynamics and resistance at various dosage regimens against Staphylococcus aureus isolates with reduced susceptibilities to daptomycin in an in vitro pharmacodynamic model with simulated endocardial vegetations.
Leonard, SN; Rose, WE; Rybak, MJ, 2008
)
"Oral controlled release microspheres of rifampicin (RIF) were prepared in order to circumvent the required regular high dose of the conventional dosage forms for the treatment of tuberculosis."( Gelatin microspheres of rifampicin cross-linked with sucrose using thermal gelation method for the treatment of tuberculosis.
Chuttani, K; Khar, RK; Mishra, AK; Samad, A; Sultana, Y, 2009
)
"Reduction in the dosing frequency of antituberculosis drugs (ATDs) by applying drug delivery technology has the potential to improve the patient compliance in tuberculosis (TB)."( Alginate nanoparticles as antituberculosis drug carriers: formulation development, pharmacokinetics and therapeutic potential.
Ahmad, Z; Khuller, GK; Pandey, R; Sharma, S,
)
" The efficacy of the rifampin-levofloxacin combination is not significantly improved by the dosage of levofloxacin."( Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
Ariza, J; Cabellos, C; Cabo, J; Euba, G; Gudiol, F; Murillo, O; Pachón, ME; Tubau, F; Verdaguer, R, 2008
)
" With a dosage of 30 mg/kg PZA, efficient serum levels were reached."( Pyrazinamide serum levels in childhood tuberculosis.
Detjen, A; Magdorf, K; Thee, S; Wahn, U, 2008
)
" Blood glucose levels were significantly lower than those observed after dosing with glyburide alone."( Elucidating rifampin's inducing and inhibiting effects on glyburide pharmacokinetics and blood glucose in healthy volunteers: unmasking the differential effects of enzyme induction and transporter inhibition for a drug and its primary metabolite.
Benet, LZ; Frassetto, LA; Huang, Y; Zheng, HX, 2009
)
"Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of new multisource and reformulated immediate release (IR) solid oral dosage forms containing rifampicin as the only Active Pharmaceutical Ingredient (API) are reviewed."( Biowaiver monographs for immediate release solid oral dosage forms: rifampicin.
Barends, DM; Becker, C; Dressman, JB; Junginger, HE; Kopp, S; Midha, KK; Shah, VP; Stavchansky, S, 2009
)
" Mild hepatotoxicity to the rat, treated with RFP of higher dosage (100 mg/kg) and longer duration (14 days), was revealed by the traditional histopathological method."( [Metabonomic profile of urine from rats administrated with different treatment period of rifampin].
Chen, HB; Liao, Y; Peng, SQ; Yan, XZ; Zhang, LS, 2008
)
" Therapy was performed according to regimens 3 and 1, by using individual dosage regimens depending on the extent and severity of a specific process, the presence of complications, and age-related features."( [Optimization of chemotherapy regimens in children with primary pulmonary tuberculosis].
Dovgaliuk, IF; Ovchinnikova, IuE; Starshinova, AA, 2009
)
" The objective of this experiment is to assess the impacts of various dosing frequencies of the combination on its bactericidal and sterilizing activities against Mycobacterium ulcerans in mice."( Impacts of dosing frequency of the combination rifampin-streptomycin on its bactericidal and sterilizing activities against Mycobacterium ulcerans in mice.
Aubry, A; Chauffour, A; Ibrahim, M; Jarlier, V; Ji, B; Robert, J, 2009
)
" Pharmacokinetic studies of higher dosages of rifampin are urgently needed in children to assist in placing the dosage of rifampin used in childhood on a more scientific foundation."( Rifampin pharmacokinetics in children, with and without human immunodeficiency virus infection, hospitalized for the management of severe forms of tuberculosis.
Cilliers, K; Donald, PR; Hussey, GD; Labadarios, D; Maritz, JS; McIlleron, H; Schaaf, HS; Smith, P; Willemse, M, 2009
)
" The median number of dosage adjustments to attain normal concentrations was 1 (range 0-4 adjustments)."( Therapeutic drug monitoring of antimycobacterial drugs in patients with both tuberculosis and advanced human immunodeficiency virus infection.
Engemann, JJ; Fortenberry, ER; Hamilton, CD; Holland, DP; Peloquin, CA; Stout, JE; Weintrob, AC, 2009
)
" Efavirenz and nevirapine concentrations at 12 h after dosing (C12) were monitored at weeks 6 and 12."( A randomized trial comparing plasma drug concentrations and efficacies between 2 nonnucleoside reverse-transcriptase inhibitor-based regimens in HIV-infected patients receiving rifampicin: the N2R Study.
Burapatarawong, S; Likanonsakul, S; Lueangniyomkul, A; Mankatitham, W; Manosuthi, W; Prasithsirskul, W; Prommool, V; Ruxrungtham, K; Sungkanuparph, S; Tantanathip, P; Thawornwa, U; Thongyen, S, 2009
)
" The oral absorption of BMS-299897 from solid dosage forms appeared to be dissolution rate-limited."( Studies on the pharmacokinetics and metabolism of a gamma-secretase inhibitor BMS-299897, and exploratory investigation of CYP enzyme induction.
Anderson, JJ; Barten, DM; Boulton, DW; Felsenstein, KM; Flint, OP; Hansel, SB; Krishna, R; Lubinski, J; Pursley, JM; Santone, KS; Thakur, A; Wang, J; Yao, M; Zheng, M, 2009
)
" So more attention should be paid to reducing the frequency, times and dosage of antimicrobials, especially third or fourth cephalosporins."( Transconjugation and genotyping of the plasmid-mediated AmpC beta-lactamase and extended-spectrum beta-lactamase genes in Klebsiella pneumoniae.
Qin, JP; Shi, WF; Zhou, J, 2009
)
" The following three regimens were administered: regimen A (n = 9) consisted of CAM (400 mg/d), ethambutol (EB) [750 mg/d], and rifampicin (RFP) [450 mg/d]; regimen B (n = 12) consisted of CAM (800 mg/d), EB (750 mg/d), and RFP (450 mg/d); and regimen C (n = 13) consisted of CAM (800 mg/d), EB (1,000 mg/d), and RFP (600 mg/d) during the first 2 months followed by a reduction of the dosage of EB from 1,000 to 750 mg/d."( Therapeutic effects of various initial combinations of chemotherapy including clarithromycin against Mycobacterium avium complex pulmonary disease.
Fukunaga, K; Hasegawa, N; Ishii, K; Ishizaka, A; Miyairi, M; Nishimura, T; Ohtani, S; Takeshita, K; Tasaka, S; Urano, T, 2009
)
"6%), which included a daily dosage of 400 mg of CAM (9."( Therapeutic effects of various initial combinations of chemotherapy including clarithromycin against Mycobacterium avium complex pulmonary disease.
Fukunaga, K; Hasegawa, N; Ishii, K; Ishizaka, A; Miyairi, M; Nishimura, T; Ohtani, S; Takeshita, K; Tasaka, S; Urano, T, 2009
)
" The length and the dosage of treatment are not yet firmly established."( The effect of combined treatment with oral clindamycin and oral rifampicin in patients with hidradenitis suppurativa.
Boer, J; Jemec, GB; Prens, EP; van der Zee, HH, 2009
)
" This case highlights the importance of the correct administration and dosing of BCG vaccine and suggests a management option that may prevent the severe local and systemic complications that are frequently associated with BCG overdose."( Too much of a good thing: management of BCG vaccine overdose.
Curtis, N; Ritz, N; Streeton, J; Tebruegge, M, 2009
)
" Fasting efavirenz concentrations at 12 h after dosing (C12) were monitored."( Body weight cutoff for daily dosage of efavirenz and 60-week efficacy of efavirenz-based regimen in human immunodeficiency virus and tuberculosis coinfected patients receiving rifampin.
Eampokarap, B; Kaewsaard, S; Lueangniyomkul, A; Mankatitham, W; Manosuthi, W; Ruxrungtham, K; Sungkanuparph, S; Suwanvattana, P; Tantanathip, P; Thongyen, S; Uttayamakul, S, 2009
)
" The current World Health Organization (WHO) guidelines recommend an oral dosage of 10 (8-12) mg per kg body weight."( Rifampicin serum levels in childhood tuberculosis.
Detjen, A; Magdorf, K; Thee, S; Wahn, U, 2009
)
" In children, it appears to be more valid to calculate RMP dosage on the basis of body surface area rather than body weight, leading to higher dosages especially in younger children."( Rifampicin serum levels in childhood tuberculosis.
Detjen, A; Magdorf, K; Thee, S; Wahn, U, 2009
)
" Hence, GPs hold promising potential for increasing drug targetability vis a vis reducing dosing frequency with the interception of minimal side effects, for efficient management of tuberculosis."( Gelatin nanocarriers as potential vectors for effective management of tuberculosis.
Agrawal, GP; Gupta, P; Gupta, UD; Jain, NK; Saraogi, GK, 2010
)
" The antihistamine response after ebastine dosing would be decreased following rifampin pretreatments."( Itraconazole and rifampin alter significantly the disposition and antihistamine effect of ebastine and its metabolites in healthy participants.
Cha, IJ; Lee, SS; Liu, KH; Shin, JG; Shon, JH; Yeo, CW, 2010
)
" For the first 2 weeks of therapy, the dosing frequency was 5 days/week, and for the remaining period, twice weekly."( Comparison of the 'Denver regimen' against acute tuberculosis in the mouse and guinea pig.
Ahmad, Z; Grosset, JH; Karakousis, PC; Nuermberger, EL; Peloquin, CA; Pinn, ML; Tasneen, R; Williams, KN, 2010
)
" According to the findings of the present study, all 3 of the potentially hepatotoxic drugs (isoniazid, rifampicin, and pyrazinamide) can be reintroduced simultaneously at full dosage safely from day 1, especially for patients with bilateral extensive pulmonary tuberculosis, to halt disease transmission or to treat patients with life-threatening tuberculosis."( Safety of 3 different reintroduction regimens of antituberculosis drugs after development of antituberculosis treatment-induced hepatotoxicity.
Jayaswal, A; Makharia, G; Mohan, A; Sarda, P; Sharma, SK; Singh, S; Singla, R; Sreenivas, V, 2010
)
" On the other hand, simulations indicated that at least 2 weeks of dosing would be needed to detect the potent inhibition of CYP3A (maximal ~40% decrease in 4βHC plasma levels)."( Does the long plasma half-life of 4beta-hydroxycholesterol impact its utility as a cytochrome P450 3A (CYP3A) metric?
Rodrigues, AD; Yang, Z, 2010
)
"Therapeutic drug monitoring allows to determine the best dosage regimen adapted to each patient optimizing the therapeutic benefits, while minimizing the risk for side effects."( Determination of antituberculosis drug concentration in human plasma by MALDI-TOF/TOF.
Ascenzi, P; Bevilacqua, N; Gullotta, F; Lauria, FN; Mancone, C; Notari, S; Pucillo, LP; Sergi, M; Tempestilli, M; Tripodi, M; Urso, R, 2010
)
"A systematic review and meta-analysis of randomized, controlled trials and cohort studies was conducted to evaluate the impact of duration and dosing schedule of rifamycin and use of antiretroviral therapy in the treatment of active tuberculosis in HIV-positive patients."( Treatment of active tuberculosis in HIV-coinfected patients: a systematic review and meta-analysis.
Burman, W; Harries, AD; Khan, FA; Menzies, D; Minion, J; Pai, M; Royce, S, 2010
)
" When coadministered with rifampin, area under the plasma concentration-time curve over the dosing interval and maximum concentration values for linezolid were reduced approximately 32% and 21%, respectively."( Unexpected effect of rifampin on the pharmacokinetics of linezolid: in silico and in vitro approaches to explain its mechanism.
Damle, B; Fahmi, OA; Gandelman, K; Glue, P; Lian, K; Obach, RS; Zhu, T, 2011
)
" The rifamycin activity could be improved by increasing the dose size of rifampicin or by daily dosing with long acting rifapentine."( The near future: improving the activity of rifamycins and pyrazinamide.
Fourie, PB; Mitchison, DA, 2010
)
"A questionnaire regarding what antitubercular drugs, their dosage and for how long was asked to attending faculty in an International Conference on musculoskeletal infections."( A survey of prescribing pattern for osteoarticular tuberculosis: orthopaedic surgeons' and infectious disease experts' perspective.
Agarwal, A; Arora, A; Kumar, S, 2009
)
" As meal behavior has a substantial impact on rifapentine exposure, it should be considered in the evaluation of optimal dosing approaches."( Effects of four different meal types on the population pharmacokinetics of single-dose rifapentine in healthy male volunteers.
Fourie, PB; McIlleron, HM; Mitchison, D; Roscigno, G; Simonsson, US; Smith, PJ; Van Der Walt, JS; Zvada, SP, 2010
)
" Of 506 patients prescribed a three-drug fixed-dose combination (FDC), the dosage was adequate in 374 (73."( Inconsistent dosing of anti-tuberculosis drugs in Taipei, Taiwan.
Bai, KJ; Chiang, CY; Enarson, DA; Lee, CN; Luh, KT; Suo, J, 2010
)
" Lopinavir CL/F increased linearly during the dosing interval."( Population pharmacokinetics of lopinavir in combination with rifampicin-based antitubercular treatment in HIV-infected South African children.
Elsherbiny, D; Maartens, G; McIlleron, H; Ren, Y; Simonsson, US, 2010
)
" The time-dependent lopinavir CL/F might be due to a time-dependent recovery from ritonavir inhibition of lopinavir metabolism during the dosing interval."( Population pharmacokinetics of lopinavir in combination with rifampicin-based antitubercular treatment in HIV-infected South African children.
Elsherbiny, D; Maartens, G; McIlleron, H; Ren, Y; Simonsson, US, 2010
)
" However, in multivariable analyses, the rifampin AUC(0-24) was significantly affected by rifampin dosage (in mg/kg of body weight), polymorphisms in the SLCO1B1 gene, and the presence of tuberculosis by geographic region."( Effects of tuberculosis, race, and human gene SLCO1B1 polymorphisms on rifampin concentrations.
Bliven-Sizemore, E; Burman, W; Engle, M; Johnson, JL; Luo, CC; Mac Kenzie, WR; Peloquin, C; Prihoda, TJ; Vernon, A; Weiner, M, 2010
)
" These results indicate that concurrent use of strong CYP3A4 inducers or inhibitors may necessitate dosage adjustments of nilotinib and should be avoided when possible."( Effects of rifampin and ketoconazole on the pharmacokinetics of nilotinib in healthy participants.
Galitz, L; Grouss, K; Harrell, R; Schran, H; Sethuraman, V; Smith, T; Tanaka, C; Yin, OQ, 2011
)
" Our results demonstrated that the dosage of dapsone in leprosy treatment does not promote a significant methemoglobinemia."( Methemoglobinemia and dapsone levels in patients with leprosy.
Martins, Ade N; Riveira, JG; Salgado, CG; Silva, JP; Vieira, JL,
)
" In conclusion, the result of this study suggested that the bioavailability-enhancing property of MoAF may help to lower the dosage level and shorten the treatment course of rifampicin."( Influence of Moringa oleifera on pharmacokinetic disposition of rifampicin using HPLC-PDA method: a pre-clinical study.
Arya, JS; Bawankule, DU; Darokar, MP; Gupta, MM; Gupta, SC; Pal, A; Shanker, K; Singh Khanuja, SP; Yadav, NP, 2011
)
" A dosage adjustment of bisoprolol is necessary if the clinical status of the patient requires treatment with the antituberculosis drug rifampicin."( [Urinary bladder tuberculosis and Bacillus Calmette-Guérin instillation: reduced efficacy of bisoprolol in hypertension].
Drechsler, A; Kirch, W, 2010
)
" The main outcome measure was the analysis of ambrisentan pharmacokinetics (area under the plasma concentration-time curve during a dosage interval [AUC(τ)], maximum plasma drug concentration [C(max)] and minimum plasma drug concentration [C(min)]) for steady-state ambrisentan alone (day 5) as compared with steady-state ambrisentan plus steady-state rifampicin (day 13)."( Effects of rifampicin (rifampin) on the pharmacokinetics and safety of ambrisentan in healthy subjects: a single-sequence, open-label study.
Boinpally, R; Dufton, C; Harrison, B; Henderson, LS; Magee, MH; Mandagere, A; Walker, G, 2010
)
" A minimum effective concentration (MEC) of 3000 ng/mL was used to interpret nevirapine concentrations 12 h after dosing (C(12))."( Nevirapine pharmacokinetics when initiated at 200 mg or 400 mg daily in HIV-1 and tuberculosis co-infected Ugandan adults on rifampicin.
Back, D; Boffito, M; Byakika-Kibwika, P; Coakley, P; Colebunders, R; Kalemeera, F; Khoo, S; Lamorde, M; Merry, C; Namakula, R; Okaba-Kayom, V; Ryan, M, 2011
)
" A dosage adjustment of bisoprolol is necessary if the clinical status of the patient requires treatment with the antituberculosis drug rifampicin."( [Urinary bladder tuberculosis and bacillus calmette-guérin instillation: reduced efficacy of bisoprolol in hypertension].
Drechsler, A; Kirch, W, 2010
)
" PubMed, Ovid MEDLINE and EMBASE were systematically searched for publications in English to evaluate the evidence about dosing schedules and treatment efficacy."( Treatment of tuberculosis and optimal dosing schedules.
Chang, KC; Grosset, J; Leung, CC; Yew, WW, 2011
)
" Rifampin's effect on the AUC(0-3 h) of digoxin was biphasic: the AUC(0-3 h) increased with concomitant dosing of the two drugs but decreased when digoxin was administered after rifampin."( Rifampin's acute inhibitory and chronic inductive drug interactions: experimental and model-based approaches to drug-drug interaction trial design.
Cai, X; Chu, X; Ding, Y; Evers, R; Gibson, C; Reitman, ML; Roupe, K; Stoch, A; Stone, JA; Venkatasubramanian, R; Wagner, JA; Witter, R; Yabut, J; Zajic, S, 2011
)
"The objective of this study was to compare, under fasting conditions in healthy volunteers, the rate and extent of absorption of a generic rifampicin capsule in oral dosage form versus the proprietary equivalent formulation for the purpose of registration approval of the test formulation."( A bioequivalence comparison of two formulations of rifampicin (300- vs 150-mg capsules): An open-label, randomized, two-treatment, two-way crossover study in healthy volunteers.
Basu, RC; Chik, Z; Lee, TC; Mohamed, Z; Pendek, R, 2010
)
" The dosage of sirolimus had to be increased, in one case up to six-fold and in the second case up to five-fold, to maintain serum levels after starting the rifampicin."( Drug interaction between rifampicin and sirolimus in transplant patients.
Khan, D; Ngo, BT; Pascoe, M, 2011
)
" This trial is based on the hypothesis that current anti-mycobacterial treatment schedules for TBM are not potent enough and that outcomes will be improved by increasing the CSF penetrating power of this regimen by optimising dosage and using additional drugs with better CSF penetration."( Intensified treatment with high dose rifampicin and levofloxacin compared to standard treatment for adult patients with tuberculous meningitis (TBM-IT): protocol for a randomized controlled trial.
Bang, ND; Caws, M; Chau, TT; Day, J; Dung, NH; Farrar, J; Heemskerk, D; Merson, L; Olliaro, P; Pouplin, T; Wolbers, M; Yen, NT, 2011
)
"Historical trials suggest that higher than standard RMP dosing results in improved culture conversion rates."( Higher-dose rifampin for the treatment of pulmonary tuberculosis: a systematic review.
Deck, D; Hopewell, PC; Huang, D; Jotblad, S; Nahid, P; Robsky, K; Steingart, KR, 2011
)
" Using plasma ALF concentrations and area under the curve (AUC), clearance, or single-point concentrations, both simultaneous and sequential dosing provided equivalent results and detected hepatic and intestinal CYP3A induction and inhibition."( Concurrent assessment of hepatic and intestinal cytochrome P450 3A activities using deuterated alfentanil.
Blood, J; Buck, N; Kharasch, ED; Kim, T; London, A; Mach, RH; Vangveravong, S, 2011
)
"This study aimed to test whether a pharmacokinetic simulation model could extrapolate nonclinical drug data to predict human efavirenz exposure after single and continuous dosing as well as the effects of concomitant rifampicin and further to evaluate the weight-based dosage recommendations used to counteract the rifampicin-efavirenz interaction."( In silico prediction of efavirenz and rifampicin drug-drug interaction considering weight and CYP2B6 phenotype.
Ashton, M; Mukonzo, J; Rekić, D; Röshammar, D, 2011
)
" These results indicate that for equivalent RMP dosages adult patients reach a lower C(max) than adult volunteers and that adults, both volunteers and patients established on RMP reach higher C(max) values than children; children established on RMP require approximately twice the mg/kg body weight dosage of RMP to reach serum concentrations equivalent to those of adults."( The pharmacokinetics and pharmacodynamics of rifampicin in adults and children in relation to the dosage recommended for children.
Diacon, AH; Donald, PR; Maritz, JS, 2011
)
" To optimize the dose regimens of these inducers for use in DDI studies, their effect at various doses and dosing durations on the area under the curve (AUC) of multiple probe substrates was simulated using a population-based simulator."( Simulation of clinical drug-drug interactions from hepatocyte CYP3A4 induction data and its potential utility in trial designs.
Hayashi, M; Shou, M; Skiles, GL; Xu, Y; Zhou, Y, 2011
)
" The transit profiles demonstrated that the dosage form was retained in the stomach for more than 320 min."( Gastroretentive delivery of rifampicin: in vitro mucoadhesion and in vivo gamma scintigraphy.
Joshi, A; Nivsarkar, M; Pund, S; Shishoo, C; Vasu, K, 2011
)
" Recent in vitro, animal, and early bactericidal activity studies suggest that the 600-mg once daily dose is at the lower end of the dose-response curve, refuting the pharmacokinetic argument."( Why Do We Use 600 mg of Rifampicin in Tuberculosis Treatment?
Aarnoutse, RE; Boeree, MJ; Dawson, R; Diacon, AH; Donald, PR; Gillespie, SH; Plemper van Balen, G; van Ingen, J, 2011
)
" Body weight and genetic factors will be important covariates in dosing algorithms."( Modest but variable effect of rifampin on steady-state plasma pharmacokinetics of efavirenz in healthy African-American and Caucasian volunteers.
Court, MH; Dumond, JB; Greenblatt, DJ; Kashuba, AD; Kurpewski, J; Kwara, A; Poethke, P; Tashima, KT, 2011
)
" Therapeutic simulations were performed with the full model to study the antibacterial effect of various dosage regimens of rifampin in lungs."( Mathematical modeling of pulmonary tuberculosis therapy: Insights from a prototype model with rifampin.
Bourguignon, L; Conte, JE; Goutelle, S; Jelliffe, RW; Maire, P, 2011
)
" We proposed a systematic classification scheme using FDA-approved drug labeling to assess the DILI potential of drugs, which yielded a benchmark dataset with 287 drugs representing a wide range of therapeutic categories and daily dosage amounts."( FDA-approved drug labeling for the study of drug-induced liver injury.
Chen, M; Fang, H; Liu, Z; Shi, Q; Tong, W; Vijay, V, 2011
)
"Individuals from the CIPRA-South Africa cohort taking EFV-based antiretroviral therapy with concomitant tuberculosis (TB) were dosed with either increased (800 mg) or standard (600 mg) dose EFV during TB treatment."( Efavirenz and rifampicin in the South African context: is there a need to dose-increase efavirenz with concurrent rifampicin therapy?
Cohen, K; Conradie, F; Ive, P; Orrell, C; Sanne, I; Wood, R; Zeinecker, J, 2011
)
"Mycophenolate mofetil (MMF) is now commonly used in pediatric liver transplant recipients, but no clear recommendations about the dosing regimen have been made for this population."( Optimization of the dosing regimen of mycophenolate mofetil in pediatric liver transplant recipients.
Barau, C; Barrail-Tran, A; Debray, D; Furlan, V; Habes, D; Hemerziu, B; Taburet, AM, 2011
)
" For dose-response studies, LS-180 cells were treated with different concentrations of the selected drugs followed by P-gp protein and gene expressions analyses."( Exposure of LS-180 cells to drugs of diverse physicochemical and therapeutic properties up-regulates P-glycoprotein expression and activity.
Abuznait, AH; Kaddoumi, A; Patrick, SG, 2011
)
" The patient reported complete compliance with using amiodarone daily, with no recent changes in dosage or formulation."( A significant drug-drug interaction detected through corneal examination: resolution of cornea verticillata while using amiodarone.
Bunya, VY; Dunaief, JL; Mehta, S; Orlin, SE; Sulewski, ME, 2012
)
"The World Health Organization (WHO) recently issued revised first-line antituberculosis (anti-TB) drug dosage recommendations for children."( Pharmacokinetics of isoniazid, rifampin, and pyrazinamide in children younger than two years of age with tuberculosis: evidence for implementation of revised World Health Organization recommendations.
Donald, PR; Hesseling, AC; Magdorf, K; Roll, S; Rosenkranz, B; Schaaf, HS; Seddon, JA; Seifart, HI; Thee, S; Werely, CJ, 2011
)
" Once-daily dosing of aerosolized pentamidine resulted in higher concentrations in BAL fluid than after intravenous administration."( Penetration of anti-infective agents into pulmonary epithelial lining fluid: focus on antifungal, antitubercular and miscellaneous anti-infective agents.
George, JM; Rodvold, KA; Yoo, L, 2011
)
" As tolvaptan is a CYP3A4 substrate, knowing the effects of inhibition and induction on CYP3A4-mediated metabolism was important for dosing recommendations."( Effects of CYP3A4 inhibition and induction on the pharmacokinetics and pharmacodynamics of tolvaptan, a non-peptide AVP antagonist in healthy subjects.
Bricmont, P; Mallikaarjun, S; Shoaf, SE, 2012
)
" Rifampicin concentrations during the dosing interval were determined by HPLC at three different timepoints: (i) after 2 weeks of TB therapy and before starting HIV therapy (T0); (ii) after 4 weeks of combined therapy (T1); and (iii) after 10 weeks of combined therapy (T2)."( Systemic exposure to rifampicin in patients with tuberculosis and advanced HIV disease during highly active antiretroviral therapy in Burkina Faso.
Bonkoungou, V; Carvalho, AC; Comelli, M; Cusato, M; Dembélé, SM; Kouanda, S; Matteelli, A; Nacanabo, R; Regazzi, M; Saleri, N; Villani, P, 2012
)
"Therapeutic drug monitoring (TDM) is used to optimize dosing that maximizes therapeutic benefit while minimizing toxicity."( Therapeutic drug monitoring in the treatment of active tuberculosis.
Babalik, A; Francis, D; Mannix, S; Menzies, D,
)
" We evaluated the inductive effect of rifampicin (RIF), a typical human PXR ligand, on the plasma exposure to the four P450 substrate drugs (triazolam/CYP3A4, pioglitazone/CYP2C8, (S)-warfarin/CYP2C9, and (S)-(-)-mephenytoin/CYP2C19) by cassette dosing in PXB mice."( Investigation of drug-drug interactions caused by human pregnane X receptor-mediated induction of CYP3A4 and CYP2C subfamilies in chimeric mice with a humanized liver.
Hasegawa, M; Inoue, R; Kakuni, M; Tahara, H; Tateno, C; Ushiki, J, 2012
)
" In this article, a case series is presented to illustrate the value of individualized TB drug dosing in four patients with low TB drug concentrations."( Therapeutic drug monitoring in the treatment of tuberculosis patients.
Aarnoutse, R; Boeree, M; Ijdema, D; Magis-Escurra, C; van den Boogaard, J, 2012
)
" Average CAM dosage was increased from the early (517 mg/day) to the later (800 mg/day) period."( Relationship between clinical efficacy for pulmonary MAC and drug-sensitivity test for isolated MAC in a recent 6-year period.
Abe, M; Kato, S; Kobashi, Y; Mouri, K; Obase, Y; Oka, M, 2012
)
"The currently recommended doses of rifampin are believed to be at the lower end of the dose-response curve."( A semimechanistic pharmacokinetic-enzyme turnover model for rifampin autoinduction in adult tuberculosis patients.
Bocar Lo, M; Gninafon, M; Horton, J; Khandelwal, A; Lienhardt, C; McIlleron, H; Merle, C; Olliaro, PL; Rustomjee, R; Simonsson, US; Smith, P; Smythe, W; Sow, OB, 2012
)
" Daily dosing of rifapentine (P), a potent rifamycin with high intracellular accumulation, in place of rifampin (R) in the standard antitubercular regimen significantly shortens the duration of treatment needed to prevent relapse in a murine model of active TB."( Rifapentine is not more active than rifampin against chronic tuberculosis in guinea pigs.
Dutta, NK; Grosset, JH; Illei, PB; Karakousis, PC; Mdluli, KE; Nuermberger, EL; Peloquin, CA; Pinn, ML, 2012
)
" Dosage adjustments were performed when C(min) ≥10 mg/L and/or AUC₂₄ ≥400 mg/L · h."( Therapeutic drug monitoring may improve safety outcomes of long-term treatment with linezolid in adult patients.
Cojutti, P; Del Pin, B; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2012
)
" Dosage adjustments were needed in 40% versus 0% of patients in the linezolid group (n = 35) versus the linezolid + rifampicin group (n = 10), respectively."( Therapeutic drug monitoring may improve safety outcomes of long-term treatment with linezolid in adult patients.
Cojutti, P; Del Pin, B; Furlanut, M; Pea, F; Viale, P; Zamparini, E, 2012
)
" Trials of new drugs and new dosing strategies are needed."( The pharmacokinetics and pharmacodynamics of pulmonary Mycobacterium avium complex disease treatment.
Aarnoutse, RE; Boeree, MJ; Daley, CL; Egelund, EF; Heifets, LB; Levin, A; Mouton, JW; Peloquin, CA; Totten, SE; van Ingen, J, 2012
)
"Historically, dosing regimens for the treatment of tuberculosis (TB) have been proposed in an empirical manner."( Feasibility of a fixed-dose regimen of pyrazinamide and its impact on systemic drug exposure and liver safety in patients with tuberculosis.
Della Pasqua, O; Sahota, T, 2012
)
" All anti-tuberculosis drugs was continued at full dosage after the normalization of liver enzyme in 76."( Management of and risk factors related to hepatotoxicity during tuberculosis treatment.
Ağca, S; Arda, H; Babalık, A; Bakırcı, N; Calışır, HC; Cetintaş, G; Kızıltaş, S; Oruç, K, 2012
)
" Noncompliance treatment, simulated by a reduced duration and dosing frequency, resulted in a relapse of infection."( Consequences of noncompliance for therapy efficacy and emergence of resistance in murine tuberculosis caused by the Beijing genotype of Mycobacterium tuberculosis.
Aarnoutse, RE; Bakker-Woudenberg, IA; Boeree, MJ; de Knegt, GJ; de Steenwinkel, JE; den Bakker, MA; ten Kate, MT; van Soolingen, D; Verbrugh, HA, 2012
)
" Post hoc meta-regression restricted to arms with ART demonstrated no associations between rifamycin duration, dosing schedule, and outcomes."( An updated systematic review and meta-analysis on the treatment of active tuberculosis in patients with HIV infection.
Ahmad Khan, F; Al-Motairi, A; Benedetti, A; Harries, AD; Menzies, D; Minion, J, 2012
)
" Use of rifamycins for ≥8 months and daily dosing in the intensive phase also improve TB treatment outcomes; however, a paucity of evidence makes their importance less clear for patients on ART."( An updated systematic review and meta-analysis on the treatment of active tuberculosis in patients with HIV infection.
Ahmad Khan, F; Al-Motairi, A; Benedetti, A; Harries, AD; Menzies, D; Minion, J, 2012
)
" This suggests that conventional antituberculous dosing may be too low and consideration should be given to increase the maximum initial weight-based doses in HIV-infected patients."( Factors associated with reduced antituberculous serum drug concentrations in patients with HIV-TB coinfection.
Ahmed, R; Cooper, R; Der, E; Foisy, M; Kunimoto, D,
)
"We performed plasma dosage for each antibiotic in patients with a bone and joint infection requiring treatment with a levofloxacin and rifampicin combination."( Pharmacokinetic and dynamic study of levofloxacin and rifampicin in bone and joint infections.
Bensalem, M; Bland, S; Bru, JP; Gaillat, J; Garraffo, R; Guillaume, M; Janssen, C, 2012
)
"5% of tuberculosis (TB) cases reported in 2003 in Taipei City had no recorded pre-treatment body weight and that among those who had, inconsistent dosing of anti-TB drugs was frequent."( Improved consistency in dosing anti-tuberculosis drugs in Taipei, Taiwan.
Bai, KJ; Chiang, CY; Hsu, YL; Lin, TP; Shih, HC; Yang, SL; Yen, MY; Yu, MC, 2012
)
" The proportion of patients treated with consistent dosing of a 3-drug fixed-dose combination (FDC) increased from 73."( Improved consistency in dosing anti-tuberculosis drugs in Taipei, Taiwan.
Bai, KJ; Chiang, CY; Hsu, YL; Lin, TP; Shih, HC; Yang, SL; Yen, MY; Yu, MC, 2012
)
"The phase behavior of rifampicin in cholesteryl-based carbonate esters (CCEs), cholesterol and polyethylene glycol4000 (PEG4000) was determined to evaluate their potential in the formulation of dry powder inhalation dosage forms."( Phase behavior of rifampicin in cholesterol-based liquid crystals and polyethylene glycol.
Buatong, W; Changsan, V; Gangadhar, KN; Srichana, T, 2012
)
"In HIV-infected patients receiving rifampicin-based treatment for tuberculosis (TB), the dosage of lopinavir/ritonavir (LPV/r) is adjusted to prevent sub-therapeutic lopinavir concentrations."( Coadministration of lopinavir/ritonavir and rifampicin in HIV and tuberculosis co-infected adults in South Africa.
Gandhi, RT; Kuritzkes, DR; Marconi, VC; Murphy, RA; Sunpath, H, 2012
)
" The durability of coadministered treatment was significantly shorter in patients who received super-boosted lopinavir/ritonavir with TB treatment compared to patients who received standard lopinavir/ritonavir dosing (log rank, P = 0."( Coadministration of lopinavir/ritonavir and rifampicin in HIV and tuberculosis co-infected adults in South Africa.
Gandhi, RT; Kuritzkes, DR; Marconi, VC; Murphy, RA; Sunpath, H, 2012
)
" We review the literature with regard to the dosing regimen and therapeutic drug levels of RMP and INH in premature infants and discuss issues of management."( Rifampicin pharmacokinetics in extreme prematurity to treat congenital tuberculosis.
Barber, N; Doerholt, K; Le Doare, K; Sharland, M, 2013
)
" The purpose of this study is to predict the dosing time-dependent pharmacokinetic interactions of repaglinide with rifampicin, using mechanistic models."( Quantitative prediction of repaglinide-rifampicin complex drug interactions using dynamic and static mechanistic models: delineating differential CYP3A4 induction and OATP1B1 inhibition potential of rifampicin.
Bi, YA; El-Kattan, AF; Fahmi, OA; Goosen, TC; Lai, Y; Lam, JL; Lin, J; Rotter, CJ; Varma, MV, 2013
)
"The discovery of novel therapeutics for the treatment of tuberculosis involves routine testing in a mouse model over four weeks of daily dosing with test compounds."( Effect of repeated dosing on rifampin exposure in BALB/c mice.
Ahuja, V; Ganguly, S; Giridhar, J; Hosagrahara, V; Panduga, V; Parab, M; Reddy, J, 2013
)
" Although clinicians are aware of the interaction with two widely used antituberculosis agents, rifampin and isoniazid, few reports have described the implications for managing phenytoin dosing in this situation."( Phenytoin-rifampin drug interaction in a hypoalbuminemic, renal failure patient: a complex clinical case.
Hurdle, AC; Twilla, JD; Van Berkel, MA, 2013
)
"The dosage of 10 mg/kg/d rifampin, as currently used in the treatment of tuberculosis (TB), is not an optimal dose."( Optimization of the rifampin dosage to improve the therapeutic efficacy in tuberculosis treatment using a murine model.
Aarnoutse, RE; Bakker-Woudenberg, IA; Boeree, MJ; de Knegt, GJ; de Steenwinkel, JE; ten Kate, MT; Teulen, M; van Soolingen, D; Verbrugh, HA, 2013
)
"Determination of optimal rifampin dosage in mice, resulting in maximum therapeutic effect and without adverse effects."( Optimization of the rifampin dosage to improve the therapeutic efficacy in tuberculosis treatment using a murine model.
Aarnoutse, RE; Bakker-Woudenberg, IA; Boeree, MJ; de Knegt, GJ; de Steenwinkel, JE; ten Kate, MT; Teulen, M; van Soolingen, D; Verbrugh, HA, 2013
)
"Maximum tolerated dosage of rifampin in the murine TB was 160 mg/kg/d."( Optimization of the rifampin dosage to improve the therapeutic efficacy in tuberculosis treatment using a murine model.
Aarnoutse, RE; Bakker-Woudenberg, IA; Boeree, MJ; de Knegt, GJ; de Steenwinkel, JE; ten Kate, MT; Teulen, M; van Soolingen, D; Verbrugh, HA, 2013
)
"Our findings indicate that the currently used rifampin dosage in the therapy of TB is too low."( Optimization of the rifampin dosage to improve the therapeutic efficacy in tuberculosis treatment using a murine model.
Aarnoutse, RE; Bakker-Woudenberg, IA; Boeree, MJ; de Knegt, GJ; de Steenwinkel, JE; ten Kate, MT; Teulen, M; van Soolingen, D; Verbrugh, HA, 2013
)
" These data do not support weight-based dosing of EFV with RIF."( Relationship between weight, efavirenz exposure, and virologic suppression in HIV-infected patients on rifampin-based tuberculosis treatment in the AIDS Clinical Trials Group A5221 STRIDE Study.
Aweeka, F; Benson, CA; Grinsztejn, B; Havlir, DV; Hogg, E; Ive, P; Lu, D; Luetkemeyer, AF; Marzan, F; Rosenkranz, SL; Sanne, IM; Swindells, S, 2013
)
" In response to this issue, our laboratory has conducted a proof-of-concept study to investigate the potential utility of juvenile pigs to serve as surrogates for children during preclinical PK testing of selected rifampin dosage forms."( Assessment of juvenile pigs to serve as human pediatric surrogates for preclinical formulation pharmacokinetic testing.
Cooper, BR; Hannou, S; Kissinger, CB; Knipp, GT; Marchant-Forde, JN; McCain, RR; Roth, WJ; Vreeman, RC, 2013
)
" Steady-state mirabegron pharmacokinetic parameters (50 and 100 mg mirabegron OCAS) were similar in 13 CYP2D6 poor, 40 intermediate, and 99 extensive metabolizers, whereas C max and AUC under the dosing interval τ of 24 h (AUCτ) were 30-47 % lower in 10 ultrarapid metabolizers."( Role of cytochrome p450 isoenzymes 3A and 2D6 in the in vivo metabolism of mirabegron, a β3-adrenoceptor agonist.
Keirns, J; Kerbusch, V; Kowalski, D; Krauwinkel, W; Lee, J; Marion, A; Meijer, J; Moy, S; Roy, M; Sawamoto, T; Takusagawa, S; van Gelderen, M, 2013
)
" Three months of sequential increases in the warfarin dosage were necessary to reach a therapeutic INR, and frequent visits to the anticoagulation clinic were needed to educate the patient about her pharmacotherapy and to perform the warfarin dosage adjustments."( Rifampicin-warfarin interaction leading to macroscopic hematuria: a case report and review of the literature.
Martins, MA; Nobre, V; Reis, AM; Ribeiro, AL; Ribeiro, DD; Rocha, MO; Sales, MF, 2013
)
"The present case exemplifies the influence of rifampicin therapy on warfarin dosage requirements and the increased risk of bleeding after rifampicin discontinuation."( Rifampicin-warfarin interaction leading to macroscopic hematuria: a case report and review of the literature.
Martins, MA; Nobre, V; Reis, AM; Ribeiro, AL; Ribeiro, DD; Rocha, MO; Sales, MF, 2013
)
" We measured total plasma thyroxine (T4) concentrations over a 6-hour period after dosing using liquid chromatography-tandem mass spectrometry."( Ciprofloxacin and rifampin have opposite effects on levothyroxine absorption.
Asher, LJ; Goldberg, AS; Kim, RB; Tirona, RG; Van Uum, SH, 2013
)
" New dosing strategies for rifampicin and ethambutol should be studied to increase the exposure to these drugs and thus maximise their impact."( Synergistic activity of rifampicin and ethambutol against slow-growing nontuberculous mycobacteria is currently of questionable clinical significance.
Boeree, MJ; Hoefsloot, W; Mouton, JW; van Ingen, J; van Soolingen, D, 2013
)
" This open-label, fixed-sequence, 3-period study was intended to evaluate the potential of anacetrapib to be a victim of OATP1B1/3 inhibition and strong CYP3A induction using acute and chronic dosing of rifampin, respectively, as a probe."( Effects of Rifampin, a potent inducer of drug-metabolizing enzymes and an inhibitor of OATP1B1/3 transport, on the single dose pharmacokinetics of anacetrapib.
Anderson, MS; Auger, P; Cote, J; Gutstein, DE; Hohnstein, A; Johnson-Levonas, AO; Liu, Y; Rasmussen, S; Stypinski, D, 2013
)
" Rifampin is commonly manufactured in capsule, tablet, and syrup dosage solutions containing alcohol or sorbitol."( Stability of rifampin in SyrSpend SF.
Sorenson, B; Whaley, P,
)
"We describe a patient treated with caspofungin and rifampin; after increasing the dosage of the former (70 mg/day) we observed an unexpectedly lower plasma exposure (AUC0-24 79."( Pharmacokinetics of caspofungin increased dosage in a patient on rifampin-containing anti-tubercular treatment.
Baietto, L; Bertucci, R; Calcagno, A; D'Avolio, A; De Rosa, FG; Di Perri, G; Pagani, N; Rostagno, R, 2013
)
" Only clarithromycin and the combination clarithromycin-rifampin were predicted to achieve concentrations in bronchoalveolar cells and pulmonary epithelial lining fluid above the MPC for the entire dosing interval."( Mutant prevention concentration and mutant selection window for 10 antimicrobial agents against Rhodococcus equi.
Berghaus, LJ; Giguère, S; Guldbech, K, 2013
)
" The case series will provide details on commonly encountered scenarios and the dosage adjustments required to maintain a therapeutic INR."( Describing the profile of patients on concurrent rifampin and warfarin therapy in western Kenya: a case series.
Karwa, R; Kirui, N; Kirwa, C; Maina, MW; Manji, I; Pastakia, SD, 2013
)
"Patients on concurrent therapy should be rigorously monitored with regular INR checks and warfarin dosage adjustments."( Describing the profile of patients on concurrent rifampin and warfarin therapy in western Kenya: a case series.
Karwa, R; Kirui, N; Kirwa, C; Maina, MW; Manji, I; Pastakia, SD, 2013
)
" A 6-month regimen of oxytetracycline with monthly dosing was strongly adulticidal, while 3-week and 6-week regimens exhibited weaker adulticidal effects."( Efficacy of three-week oxytetracycline or rifampin monotherapy compared with a combination regimen against the filarial nematode Onchocerca ochengi.
Bah, GS; Makepeace, BL; Srivastava, A; Tanya, VN; Trees, AJ; Ward, EL, 2014
)
" Rifapentine, a rifamycin antibiotic, is currently approved for intermittent dosing in the treatment of TB."( An update on the use of rifapentine for tuberculosis therapy.
Bai, X; Chan, JG; Traini, D, 2014
)
"Erlotinib exposure (AUC0-∞ and C max) was reduced after pre- or concomitant dosing with rifampicin."( The effect of rifampicin, a prototypical CYP3A4 inducer, on erlotinib pharmacokinetics in healthy subjects.
Drolet, DW; Fettner, SH; Hamilton, M; Lum, BL; Rakhit, AK; Witt, K; Wolf, JL, 2014
)
"Simulations based on our models suggest that with the new WHO dosing guidelines and utilizing available paediatric fixed-dose combinations, children will receive adequate rifampicin exposures when compared with adults, but with a larger degree of variability."( Population pharmacokinetics of rifampicin, pyrazinamide and isoniazid in children with tuberculosis: in silico evaluation of currently recommended doses.
Denti, P; Donald, PR; McIlleron, HM; Schaaf, HS; Seddon, JA; Seifart, HI; Simonsson, US; Smith, PJ; Thee, S; Zvada, SP, 2014
)
"6 for the three dosing groups (10, 20 and 100 mg)."( Quinine compared to 4β-hydroxycholesterol and midazolam as markers for CYP3A induction by rifampicin.
Andersson, TB; Bäckström, T; Bertilsson, L; Björkhem-Bergman, L; Bredberg, E; Diczfalusy, U; Nylén, H; Rönquist-Nii, Y, 2014
)
" The administration of tacrolimus (1 mg) was started as the dosage of oral glucocorticoids was tapered."( Paradoxical response to disseminated non-tuberculosis mycobacteriosis treatment in a patient receiving tumor necrosis factor-α inhibitor: a case report.
Imamura, Y; Izumikawa, K; Kakeya, H; Kohno, S; Miyazaki, T; Nakamura, S; Takazono, T; Yanagihara, K, 2014
)
"Recent murine studies found that rifapentine, dosed daily, at least halved tuberculosis treatment times compared with standard rifampicin and isoniazid-containing regimens."( A novel inhalable form of rifapentine.
Britton, WJ; Chan, HK; Chan, JC; Chan, JG; Duke, CC; Ong, HX; Traini, D; Tyne, AS; Young, PM, 2014
)
" A previous rifapentine dose escalation study with daily dosing indicated a possible decrease in bioavailability as the dose increased and an increase in clearance over time for rifapentine and its active metabolite, desacetyl rifapentine."( Population pharmacokinetics of rifapentine and desacetyl rifapentine in healthy volunteers: nonlinearities in clearance and bioavailability.
Bliven-Sizemore, E; Burman, W; Dooley, KE; Dorman, SE; Lu, Y; Nuermberger, E; Savic, RM; Weiner, M, 2014
)
" This study demonstrates notable individual variability, indicating that dosing of these medications requires individual monitoring and provides additional information to guide the clinician when treating elephants."( The pharmacokinetics of a single oral or rectal dose of concurrently administered isoniazid, rifampin, pyrazinamide, and ethambutol in Asian elephants (Elephas maximus).
Egelund, EF; Hunter, RP; Isaza, R; P Brock, A; Peloquin, CA, 2014
)
" The risk of joint-related AVN as a side effect of adjunctive steroid therapy should be taken into consideration when evaluating the dosage and treatment duration in tuberculous encephalitis."( Joint failure after steroid therapy in tuberculous encephalitis.
Kircher, J; Krauspe, R; Patzer, T; Richter, J; Ziskoven, C, 2014
)
"Seven phase I studies were conducted to investigate the effects of repeated dosing of ketoconazole, diltiazem, rifampin, or lithium on the pharmacokinetics (PK) of single oral doses of lurasidone, or the effects of repeated dosing of lurasidone on the PK of digoxin, midazolam, or the oral contraceptive norgestimate/ethinyl estradiol."( Lurasidone drug-drug interaction studies: a comprehensive review.
Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014
)
" Steady-state dosing with lurasidone increased Cmax and AUC0-24 (AUC from time 0 to 24 h postdose) of digoxin by 9% and 13%, respectively, and of midazolam by 21% and 44%, respectively."( Lurasidone drug-drug interaction studies: a comprehensive review.
Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014
)
"Lurasidone PK is altered by strong cytochrome P450 (CYP) 3A4 inhibitors or inducers, and coadministration is contraindicated; whereas moderate CYP3A4 inhibitors have less effect, and lurasidone dosage restrictions are recommended."( Lurasidone drug-drug interaction studies: a comprehensive review.
Chiu, YY; Ereshefsky, L; Loebel, A; Poola, N; Preskorn, SH, 2014
)
" In addition, differences in PK parameters observed by sex should be considered for further dosing recommendations."( Pharmacokinetics of rifampicin in Mexican patients with tuberculosis and healthy volunteers.
Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, Rdel C; Portales-Pérez, DP; Romano-Moreno, S, 2014
)
" However, further studies to identify the optimal statin and dosing are required."( Simvastatin increases the in vivo activity of the first-line tuberculosis regimen.
Bruiners, N; Gennaro, ML; Karakousis, PC; Pine, R; Pinn, ML; Skerry, C, 2014
)
"13 log10 reduction at 10 mg/kg dosing level, respectively) in mouse lung."( Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.
Ahn, S; Choi, I; Jang, J; Kang, H; Kang, S; Kim, HJ; Kim, J; Kim, RY; Kim, YM; Ko, Y; Lee, S; Nam, J; Nam, K; No, Z; Park, S; Pethe, K; Seo, JJ; Seo, M; Seo, MJ, 2014
)
"Patients were enrolled in a single-arm clinical trial to receive intermittent dosing after at least 14 initial daily doses of RMP+PZA+EMB."( Intermittent tuberculosis treatment for patients with isoniazid intolerance or drug resistance.
Bock, N; Bozeman, L; Goldberg, SV; Hamilton, CD; Heilig, CM; Hershfield, E; Kyle, RP; Narita, M; Reves, R; Tapy, JM; Wing, D, 2014
)
" BIW dosing was used in 77 and TIW in 21."( Intermittent tuberculosis treatment for patients with isoniazid intolerance or drug resistance.
Bock, N; Bozeman, L; Goldberg, SV; Hamilton, CD; Heilig, CM; Hershfield, E; Kyle, RP; Narita, M; Reves, R; Tapy, JM; Wing, D, 2014
)
" In South Africa, clinicians are advised to use 'double-dose' LPV/r dosed at 800 mg/200 mg twice daily during anti-tuberculosis treatment."( Double-dose lopinavir-ritonavir in combination with rifampicin-based anti-tuberculosis treatment in South Africa.
Chelin, N; Cohen, S; Gandhi, RT; Murphy, RA; Sunpath, H; Tennant, I; Winternheimer, P, 2014
)
" Major progress has been made to evaluate the interactions between TB drugs and antiretroviral therapy; however, burning questions remain concerning nevirapine and efavirenz effectiveness during rifampicin-based TB treatment, treatment options for TB-HIV-coinfected patients with nonnucleoside reverse transcriptase inhibitor resistance or intolerance, and exact treatment or dosing schedules for vulnerable patients including children and pregnant women."( Pharmacological interactions between rifampicin and antiretroviral drugs: challenges and research priorities for resource-limited settings.
Aarnoutse, R; Boeree, MJ; Burger, DM; Kibiki, GS; Kisanga, ER; Semvua, HH, 2015
)
" Pharmacokinetic sampling occurred at the end of each dosing period."( Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin.
Allen, R; Aweeka, F; Bao, J; Cramer, Y; Dooley, KE; Haas, DW; Koletar, SL; Luetkemeyer, AF; Marzan, F; Murray, S; Park, JG; Savic, R; Sutherland, D, 2014
)
" Increased rifampicin dosage may be warranted in African, HIV- TB co-infected patients."( Low rifampicin concentrations in tuberculosis patients with HIV infection.
Abdool Karim, SS; Botha, JH; Gengiah, TN; Naidoo, K; Soowamber, D, 2014
)
" Here, we combine pharmacokinetic/pharmacodynamic (PK/PD) modeling with multiobjective optimization to quantitatively explore trade-offs between therapeutic and adverse effects of optimal dosing for the example of rifampin in TB-infected mice."( Computational pharmacology of rifampin in mice: an application to dose optimization with conflicting objectives in tuberculosis treatment.
Lyons, MA, 2014
)
" Twice-weekly weight-adjusted dosing of INH appears to be quite robust with respect to important potentially influential patient factors under program conditions."( Effects of dosage, comorbidities, and food on isoniazid pharmacokinetics in Peruvian tuberculosis patients.
Ardrey, A; Davies, G; Jave, O; López-Romero, SL; Moore, DA; Requena-Méndez, A; Ward, SA; Waterhouse, D, 2014
)
" We further optimized the dosing of rifampin based upon simulations using the population pharmacokinetic model."( Population pharmacokinetics of rifampin in the treatment of Mycobacterium tuberculosis in Asian elephants.
Alsultan, A; An, G; Brock, AP; Egelund, EF; Isaza, R; Peloquin, CA, 2015
)
"Previous studies of raltegravir and rifampicin have not studied the interaction when rifampicin is dosed intermittently."( Effect of intermittent rifampicin on the pharmacokinetics and safety of raltegravir.
Back, DJ; Chaponda, M; Chiong, J; Chrdle, A; Egan, D; Else, L; Khoo, SH; Reynolds, HE, 2015
)
" Raltegravir trough plasma concentration (C12) was significantly lower in the presence of rifampicin when dosed at 400 mg twice daily (40%), which was not observed with 800 mg twice daily dosing."( Effect of intermittent rifampicin on the pharmacokinetics and safety of raltegravir.
Back, DJ; Chaponda, M; Chiong, J; Chrdle, A; Egan, D; Else, L; Khoo, SH; Reynolds, HE, 2015
)
" Therefore, no efavirenz dosage adjustment during rifampicin cotreatment is required in Ugandans."( CYP2B6 genotype, but not rifampicin-based anti-TB cotreatments, explains variability in long-term efavirenz plasma exposure.
Aklillu, E; Gustafson, LL; Mukonzo, JK; Nanzigu, S; Ogwal-Okeng, J; Waako, P, 2014
)
" Simulations indicated that increasing the bedaquiline dosage to mitigate the interaction would yield elevated M2 concentrations during the first treatment weeks."( Rifampicin and rifapentine significantly reduce concentrations of bedaquiline, a new anti-TB drug.
Dooley, KE; Karlsson, MO; Murray, S; Svensson, EM, 2015
)
"We conclude that anti-MRSA antibiotics are utilized via various dosage regimens by a majority of CF Foundation accredited care programs for the treatment of chronic MRSA in PEx, and there is no consensus on the best treatment approach."( Utilization of antibiotics for methicillin-resistant Staphylococcus aureus infection in cystic fibrosis.
Ampofo, K; Chin, MJ; Dasenbrook, E; Epps, KL; Marshall, BC; Montague, M; Olson, J; Young, DC; Zobell, JT, 2015
)
" Adequacy of SDC was based on the maximum concentration (Cmax) achieved in serum, with rifampicin (RMP) values <8 μg/ml and isoniazid (INH) values <3 μg/ml for daily dosing and <9 μg/ml for intermittent dosing considered inadequate."( Serum drug concentrations of INH and RMP predict 2-month sputum culture results in tuberculosis patients.
Ahmed, R; Cooper, R; Der, E; Gao, Z; Hansen, E; Kharrat, H; Kunimoto, D; Long, R; Mah, A, 2015
)
"The overall incidence of adverse events among infants receiving rifampin appears low; however, additional studies to further evaluate safety and dosing of rifampin in this population are needed."( Rifampin use and safety in hospitalized infants.
Arnold, CJ; Benjamin, DK; Chu, VH; Clark, RH; Corey, KL; Ericson, J; Hornik, CP; Kohman, J; Oh, M; Onabanjo, J; Smith, PB, 2015
)
" There was a nonlinear increase in exposure to rifampin without an apparent ceiling effect and a greater estimated fall in bacterial load in the higher dosing groups."( A dose-ranging trial to optimize the dose of rifampin in the treatment of tuberculosis.
Aarnoutse, RE; Boeree, MJ; Burger, D; Dawson, R; Diacon, AH; du Bois, J; Gillespie, SH; Heinrich, N; Hoelscher, M; Magis-Escurra, C; McHugh, TD; Narunsky, K; Phillips, PP; Plemper van Balen, G; Rehal, S; van Ingen, J; van Soolingen, D; Venter, A, 2015
)
"Current guidelines for dosing of anti-TB drugs in children advocate higher doses for rifampicin and isoniazid despite limited availability of paediatric data on the pharmacokinetics of these drugs, especially from Africa, where the burden of childhood disease remains high."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
" Rifampicin, isoniazid, pyrazinamide and ethambutol were dosed at 10, 5, 25 and 20 mg/kg, respectively."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
" Predicted AUC0 -∞ for rifampicin dosed at 15 mg/kg was comparable to that of adults while the dose required to achieve ethambutol exposure similar to that in adults was 55 mg/kg or higher."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
"These data support recently revised WHO recommendations for dosing of anti-TB drugs in children, but dosing of ethambutol in children also appears inadequate by comparison with adult pharmacokinetic data."( Pharmacokinetics of anti-TB drugs in Malawian children: reconsidering the role of ethambutol.
Ardrey, A; Davies, GR; Dzinjalamala, F; Mlotha, R; Molyneux, E; Ward, S; Waterhouse, D, 2015
)
" Improved pharmacokinetic profile of RIF-SLNs can be translated to a reduced dose and dosage frequency of RIF, thus resulting in lower or no hepatotoxicity commonly associated with its use."( Nano-formulation of rifampicin with enhanced bioavailability: development, characterization and in-vivo safety.
Jindal, S; Kaur, IP; Sharma, G; Singh, H; Singh, M, 2015
)
"Tuberculosis (TB) remains a major global health concern, and new therapies are needed to overcome the problems associated with dosing frequency, patient compliance, and drug resistance."( Antitubercular Nanocarrier Combination Therapy: Formulation Strategies and in Vitro Efficacy for Rifampicin and SQ641.
D'Addio, SM; Einck, L; Liu, Y; Prud'homme, RK; Reddy, VM; Sinko, PJ, 2015
)
" In arm 1, rifapentine was administered at 10 mg/kg of body weight twice daily and 20 mg/kg once daily, each for 14 days, separated by a 28-day washout; the dosing sequence was randomized."( Novel dosing strategies increase exposures of the potent antituberculosis drug rifapentine but are poorly tolerated in healthy volunteers.
Benson, CA; Cramer, Y; Dooley, KE; Dorman, SE; Haas, DW; Hafner, R; Hogg, E; Hovind, L; Janik, J; Marzinke, MA; Park, JG; Patterson, K; Savic, RM, 2015
)
" We conducted this study with the aims of determining the plasma concentrations of isoniazid, rifampicin, pyrazinamide and ethambutol achieved with different dosage of the anti-tubercular drugs so as to provide supportive evidence to the revised dosages and to evaluate the effects of malnutrition on the pharmacokinetics of these drugs in children."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
"Prospective drug estimation study was conducted in two groups of children, age 6 months to 15 years, with tuberculosis, with or without severe malnutrition, receiving different dosage of daily anti- tubercular therapy."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
"7%) children in the two dosing regimen, respectively."( Pharmacokinetics of isoniazid, rifampicin, pyrazinamide and ethambutol in Indian children.
Kabra, SK; Kanhiya, K; Lodha, R; Mukherjee, A; Singla, M; Velpandian, T, 2015
)
" This study used population pharmacokinetics modeling to explore the influence of demographic and pharmacogenetic factors including efavirenz-rifampicin interaction on EFV pharmacokinetics, towards safer dosing of EFV."( CYP2B6*6, CYP2B6*18, Body weight and sex are predictors of efavirenz pharmacokinetics and treatment response: population pharmacokinetic modeling in an HIV/AIDS and TB cohort in Zimbabwe.
Chonzi, P; Dhoro, M; Kadzirange, G; Masimirembwa, C; Ngara, B; Nhachi, C; Zvada, S, 2015
)
" However, RIF in the IRPP group had a shorter Tmax and higher bioavailability than orally dosed groups."( Pharmacokinetics of Inhaled Rifampicin Porous Particles for Tuberculosis Treatment: Insight into Rifampicin Absorption from the Lungs of Guinea Pigs.
Edwards, D; Elbert, K; Garcia Contreras, L; Hickey, A; Ibrahim, M; Sung, J, 2015
)
"Data on the tolerance and effectiveness of rifampicin-levofloxacin combination therapy (RLCT) in patients treated for prosthetic joint infections (PJIs) according to daily dosage are lacking."( Influence of daily dosage and frequency of administration of rifampicin-levofloxacin therapy on tolerance and effectiveness in 154 patients treated for prosthetic joint infections.
Beltrand, E; Blondiaux, N; Loiez, C; Migaud, H; Nguyen, S; Robineau, O; Senneville, E; Titecat, M; Valette, M, 2015
)
" While such pharmacokinetic/pharmacodynamic (PK/PD) studies are useful for the identification of optimal clinical dosing regimens, they are resource intensive and are not routinely performed."( Computational pharmacokinetics/pharmacodynamics of rifampin in a mouse tuberculosis infection model.
Lenaerts, AJ; Lyons, MA, 2015
)
"Information about intralesional pharmacokinetics (PK) and spatial distribution of tuberculosis (TB) drugs is limited and has not been used to optimize dosing recommendations for new or existing drugs."( Determination of [11C]rifampin pharmacokinetics within Mycobacterium tuberculosis-infected mice by using dynamic positron emission tomography bioimaging.
Dannals, RF; Dartois, V; DeMarco, VP; Dooley, KE; Holt, DP; Jain, SK; Klunk, M; Lee, CK; Ordonez, AA; Prideaux, B; Tonge, PJ; Wang, H; Weinstein, EA; Zhuo, Z, 2015
)
" The impact of HAART on imatinib may depend on whether it is being initiated or has already been dosed chronically in patients."( Human hepatocyte assessment of imatinib drug-drug interactions - complexities in clinical translation.
Beumer, JH; Christner, SM; Kiesel, BF; Parise, RA; Pillai, VC; Rudek, MA; Venkataramanan, R, 2015
)
" Further investigation is needed to determine the optimal dosage for loading rifapentine."( Treatment of Staphylococcus aureus-induced chronic osteomyelitis with bone-like hydroxyapatite/poly amino acid loaded with rifapentine microspheres.
Cao, ZD; Jiang, DM; Li, YJ; Wang, X; Wang, ZL; Wu, J; Yan, L; Yi, YF, 2015
)
"The HFS-TB model is highly accurate at identifying optimal drug exposures, doses, and dosing schedules for use in the clinic."( Correlations Between the Hollow Fiber Model of Tuberculosis and Therapeutic Events in Tuberculosis Patients: Learn and Confirm.
Gumbo, T; Hanna, D; Nuermberger, E; Pasipanodya, JG; Romero, K, 2015
)
" One of the reasons (carba)penems are seldom used for treatment of TB is the high dosage levels required, often at the therapeutic limits."( Carbapenems and Rifampin Exhibit Synergy against Mycobacterium tuberculosis and Mycobacterium abscessus.
Kaushik, A; Lamichhane, G; Makkar, N; Pandey, P; Parrish, N; Singh, U, 2015
)
" difficile infection after TB medication was not low considering the relatively low TB medication dosage compared to other antibiotics."( Incidence and Clinical Outcomes of Clostridium difficile Infection after Treatment with Tuberculosis Medication.
Huh, KC; Jang, BI; Jung, Y; Kim, SH; Koo, HS; Lee, SW; Lee, YM; Moon, HS; Shin, JE; Yoon, SM, 2016
)
" Current rifampin dosing achieves low cerebrospinal fluid (CSF) concentrations, and CSF penetration of ethambutol is poor."( Pediatric tuberculous meningitis: Model-based approach to determining optimal doses of the anti-tuberculosis drugs rifampin and levofloxacin for children.
Aarnoutse, R; Dooley, KE; Ganiem, AR; Gupta, A; Hesseling, A; Hibma, JE; McIlleron, H; Ramachandran, G; Ruslami, R; Savic, RM; Swaminathan, S; Thakur, K; van Crevel, R, 2015
)
" The model was robust enough to allow prospective predictions of macitentan-drug combinations not studied, including an alternative dosing regimen of ketoconazole and nine other CYP3A4-interacting drugs."( Physiologically-Based Pharmacokinetic Modeling of Macitentan: Prediction of Drug-Drug Interactions.
Buchmann, S; de Kanter, R; Delahaye, S; Gnerre, C; Kohl, C; Segrestaa, J; Sidharta, PN; Treiber, A, 2016
)
" Further, this PMAA/INH/RMP nanogel exhibited lower cytotoxicity than did INH or RMP alone, suggesting that this PMAA/INH/RMP nanogel could be a more useful dosage form than separate doses of INH and RMP for intestinal MTB."( Lower cytotoxicity, high stability, and long-term antibacterial activity of a poly(methacrylic acid)/isoniazid/rifampin nanogel against multidrug-resistant intestinal Mycobacterium tuberculosis.
Chen, L; Chen, T; Chen, X; Guo, H; Guo, L; Li, H; Li, Q; Li, Z; Wu, T; Yu, L; Zhao, M; Zhong, Q; Zhou, L, 2016
)
"The dosing of drugs in critically ill patients undergoing renal replacement therapy is based on limited data."( Single- and multiple-dose pharmacokinetics of ethambutol and rifampicin in a tuberculosis patient with acute respiratory distress syndrome undergoing extended daily dialysis and ECMO treatment.
Ciesek, S; Hoeper, MM; Kielstein, JT; Kühn, C; Schmidt, JJ; Strunk, AK; Welte, T, 2016
)
"Encapsulating antibiotics such as rifampicin in biodegradable nanoparticles provides several advantages compared to free drug administration, including reduced dosing due to localized targeting and sustained release."( Thioridazine in PLGA nanoparticles reduces toxicity and improves rifampicin therapy against mycobacterial infection in zebrafish.
Anes, E; Bogoeva, V; Fenaroli, F; Griffiths, G; Hildahl, J; Kalluru, R; Pires, D; Speth, M; Vibe, CB; Wilson, SR, 2016
)
"Improvement in tuberculosis treatment regimens requires selection of antibiotics and dosing schedules from a large design space of possibilities."( In silico evaluation and exploration of antibiotic tuberculosis treatment regimens.
Dartois, V; Kirschner, DE; Linderman, JJ; Pienaar, E, 2015
)
" The objectives of this study were to characterize the population pharmacokinetics (popPK) of rifampicin in Malawian children and adults with tuberculosis, simulate exposures under revised WHO dosing guidelines that aim to reduce the risk of low exposures of rifampicin and examine predicted exposures using weight- and age-based dosing bands under new dosing recommendations."( A simultaneous population pharmacokinetic analysis of rifampicin in Malawian adults and children.
Davies, G; Dzinjalamala, FK; Khoo, S; Lopez, N; Mlota, R; Molyneux, E; Pertinez, H; Schipani, A; van Oosterhout, JJ; Ward, SA, 2016
)
" Using age as a surrogate for weight in dosing bands gave similar results compared with the weight bands."( A simultaneous population pharmacokinetic analysis of rifampicin in Malawian adults and children.
Davies, G; Dzinjalamala, FK; Khoo, S; Lopez, N; Mlota, R; Molyneux, E; Pertinez, H; Schipani, A; van Oosterhout, JJ; Ward, SA, 2016
)
"The popPK model developed can be used to optimize rifampicin exposures through dosing simulations."( A simultaneous population pharmacokinetic analysis of rifampicin in Malawian adults and children.
Davies, G; Dzinjalamala, FK; Khoo, S; Lopez, N; Mlota, R; Molyneux, E; Pertinez, H; Schipani, A; van Oosterhout, JJ; Ward, SA, 2016
)
"To supplement previous state-of-art reviews on anti-tuberculosis treatment and to pave the way forward with reference to the current status, we systematically reviewed published literature on clinical research on tuberculosis (TB) over the past decade in the treatment of drug-susceptible and multidrug-resistant TB (MDR-TB), with a focus on drugs, dosing factors and regimens."( Clinical research in the treatment of tuberculosis: current status and future prospects.
Chang, KC; Sotgiu, G; Yew, WW, 2015
)
" equi pneumonia, but nephrotoxicity indicates that an alternative dosing interval or route (such as nebulization) will be needed before LG is adequately safe for clinical use."( Use of Liposomal Gentamicin for Treatment of 5 Foals with Experimentally Induced Rhodococcus equi Pneumonia.
Berghaus, LJ; Bordin, AI; Brake, CN; Burton, AJ; Cohen, ND; Coleman, MC; Giguère, S; Rocha, JN,
)
" Reports of resistance have led to combination use of fusidic acid with rifampin, which is superseded by the development of a new dosing regimen for fusidic acid that can be used in monotherapy."( Fusidic Acid: A Bacterial Elongation Factor Inhibitor for the Oral Treatment of Acute and Chronic Staphylococcal Infections.
Fernandes, P, 2016
)
" Although linezolid therapy is known to result in thrombocytopenia, dosage adjustment or therapeutic drug monitoring of linezolid is not generally necessary."( Successful treatment of methicillin-resistant Staphylococcus aureus osteomyelitis with combination therapy using linezolid and rifampicin under therapeutic drug monitoring.
Ashizawa, N; Gejo, R; Higashi, Y; Kawago, K; Kimura, T; Narukawa, M; Nogami, M; Tashiro, M; Tsuji, Y; Yamamoto, Y, 2016
)
" Quantitative IMS experiments were performed on liver tissue from an animal dosed in vivo."( Absolute Quantitative MALDI Imaging Mass Spectrometry: A Case of Rifampicin in Liver Tissues.
Allen, JL; Barry, CE; Caprioli, RM; Chumbley, CW; Marriner, GA; Reyzer, ML; Via, LE, 2016
)
" These changes could enhance the drug efficacy, but they could also cause drug accumulation, which might induce adverse effect, so it was suggested that the drug dosage should be adjusted and the drug concentration in plasma should be monitored if moxifloxacin and rifampicin are co-administered."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
" A maximum effect model was used to determine the PK/PD index that best described the dose-response data."( Investigation on rifampicin administration from the standpoint of pharmacokinetics/pharmacodynamics in a neutropenic murine thigh infection model.
Hagihara, M; Hanaki, H; Hirai, J; Kato, H; Koizumi, Y; Mikamo, H; Nishiyama, N; Sakanashi, D; Suematsu, H; Yamagishi, Y, 2016
)
"Around 450 and 250 mg daily doses might meet EFV dosing needs of HIV-TB infected Ugandans in general and CYP2B6*6/*6 genotypes, respectively."( CYP2B6 genotype-based efavirenz dose recommendations during rifampicin-based antituberculosis cotreatment for a sub-Saharan Africa population.
Aklillu, E; Bisaso, RK; Gustafsson, LL; Mukonzo, JK; Ogwal-Okeng, J; Owen, JS, 2016
)
" She had acute kidney injury, requiring daptomycin dosage adjustment."( Successful Use of High-dose Daptomycin in a Child With Staphylococcus aureus Endocarditis.
Gnanasambandam, S; Kanjani, A; Nambi, PS; Prabhudesai, S; Ramachandran, B, 2016
)
" Steady-state ketoconazole did not cause a clinically significant change in the pharmacokinetics of a single dose of tivozanib; therefore, dosing of tivozanib with a CYP3A4 pathway inhibitor should not cause a clinically significant change in serum tivozanib levels."( Effects of ketoconazole or rifampin on the pharmacokinetics of tivozanib hydrochloride, a vascular endothelial growth factor receptor tyrosine kinase inhibitor.
Cotreau, MM; Miller, J; Siebers, NM; Slichenmyer, W; Strahs, AL, 2015
)
" The UA-Lipo may be used as a dosage form to improve the antimycobacterial activity of RIF, a first-line drug for the treatment of infections caused by Mtb."( Effects of the encapsulation of usnic acid into liposomes and interactions with antituberculous agents against multidrug-resistant tuberculosis clinical isolates.
Cavalcanti, IM; Ferraz-Carvalho, RS; Linhares, LA; Lira-Nogueira, MC; Montenegro, LM; Pereira, MA; Santos-Magalhães, NS, 2016
)
" We pooled data by study quality, design, region, dosing modality and patient characteristics."( Therapeutic drug monitoring in anti-tuberculosis treatment: a systematic review and meta-analysis.
Al-Efraij, K; Campbell, JR; Cook, VJ; Johnston, J; Marra, F; Mota, L, 2016
)
" These findings point to a discrepancy between accepted 2 h TDM thresholds and TB drug dosing recommendations."( Therapeutic drug monitoring in anti-tuberculosis treatment: a systematic review and meta-analysis.
Al-Efraij, K; Campbell, JR; Cook, VJ; Johnston, J; Marra, F; Mota, L, 2016
)
" Median rifapentine area under the concentration-time curve (AUC0-24) was 313 mcg*h/mL, similar to recent studies of rifapentine dosed at 450-600 mg daily."( A Phase 2 Randomized Trial of a Rifapentine plus Moxifloxacin-Based Regimen for Treatment of Pulmonary Tuberculosis.
Armstrong, DT; Barnes, GL; Cavalcante, SC; Chaisson, RE; Cohn, S; Conde, MB; Dalcolmo, M; Dooley, KE; Dorman, SE; Duarte, RS; Durovni, B; Efron, A; Loredo, C; Marzinke, MA; Mello, FC; Moulton, LH; Rolla, V; Savic, RM, 2016
)
" The DDI risk for cobimetinib with other CYP3A4 inhibitors and inducers needs to be assessed in order to provide dosing instructions."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
"This study demonstrates the value of using PBPK simulation to assess the clinical DDI risk inorder to provide dosing instructions with other CYP3A4 perpetrators."( Evaluation of Cytochrome P450 3A4-Mediated Drug-Drug Interaction Potential for Cobimetinib Using Physiologically Based Pharmacokinetic Modeling and Simulation.
Budha, NR; Chen, Y; Dresser, M; Eppler, S; Ji, T; Jin, JY; Musib, L, 2016
)
") dosage extrapolated from dose that is used in human for 28 d once daily."( Deleterious effects of 28-day oral co-administration of first-line anti-TB drugs on spleen, blood and bone marrow chromosomes in normal rat.
Sharma, R; Sharma, VL, 2017
)
" Based on these results, it is anticipated that the PBPK model developed in this study will be useful in evaluating dosing regimens for RPT and for characterizing tissue-level doses that could be predictors of problems related to efficacy or safety."( Physiologically Based Pharmacokinetic Model of Rifapentine and 25-Desacetyl Rifapentine Disposition in Humans.
Eppers, GJ; Reisfeld, B; Zurlinden, TJ, 2016
)
"Accurate prediction of drug target activity and rational dosing regimen design require knowledge of drug concentrations at the target."( Intracellular Unbound Atorvastatin Concentrations in the Presence of Metabolism and Transport.
Korzekwa, K; Kulkarni, P; Nagar, S, 2016
)
" Coadministration of Kaletra (lopinavir/ritonavir) with delamanid resulted in an approximately 25% higher delamanid area under the concentration-time curve from time 0 to the end of the dosing interval (AUCτ)."( Delamanid Coadministered with Antiretroviral Drugs or Antituberculosis Drugs Shows No Clinically Relevant Drug-Drug Interactions in Healthy Subjects.
Geiter, L; Mallikaarjun, S; Paccaly, A; Patil, S; Petersen, C; Shoaf, SE; Wells, C, 2016
)
" One hundred patients with pulmonary tuberculosis (65% coinfected with HIV-1) were intensively sampled to determine rifampin, isoniazid, and pyrazinamide plasma concentrations after 7 to 8 weeks of a daily quadruple-therapy regimen dosed according to World Health Organization (WHO) weight bands."( HIV-1 Coinfection Does Not Reduce Exposure to Rifampin, Isoniazid, and Pyrazinamide in South African Tuberculosis Outpatients.
Chirehwa, M; Denti, P; McIlleron, H; Meintjes, G; Rockwood, N; Wiesner, L; Wilkinson, RJ, 2016
)
" Early studies that explored this potential using intermittent, higher dosing were derailed by toxicity."( Evaluation of high-dose rifampin in patients with new, smear-positive tuberculosis (HIRIF): study protocol for a randomized controlled trial.
Calderon, R; Coit, J; Coleman, D; Contreras, C; Davies, G; Lecca, L; Milstein, M; Mitchison, D; Mitnick, CD; Osso, E; Pagano, M; Peloquin, C; Sanchez Garavito, E; Seung, K; Vargas Vasquez, DE, 2016
)
" The aim of this work was to obtain a hydrophilic new material that allows a very fast dissolution rate of RIF and therefore is potentially useful in the development of oral solid dosage forms."( Very fast dissolving acid carboxymethylcellulose-rifampicin matrix: Development and solid-state characterization.
Garro-Linck, Y; Luciani-Giacobbe, LC; Manzo, RH; Monti, GA; Olivera, ME; Ramírez-Rigo, MV, 2017
)
" However, there is always concern about the safety of the dosage form by inhalation as it may induce inflammation."( Evaluation of Proinflammatory Cytokines and Adverse Events in Healthy Volunteers upon Inhalation of Antituberculosis Drugs.
Juthong, S; Laohapojanart, N; Padmavathi, AR; Pungrassami, P; Ratanajamit, C; Srichana, T; Suwandecha, T, 2016
)
"Animal infection models in the pharmacokinetic/pharmacodynamic (PK/PD) evaluation of antimicrobial therapy serve an important role in preclinical assessments of new antibiotics, dosing optimization for those that are clinically approved, and setting or confirming susceptibility breakpoints."( Animal models in the pharmacokinetic/pharmacodynamic evaluation of antimicrobial agents.
Andes, DR; Lepak, AJ; Zhao, M, 2016
)
" The effectiveness of weekly dosing with inhalable rifapentine will be assessed in murine Mycobacterium tuberculosis infection."( Inhalation of Respirable Crystalline Rifapentine Particles Induces Pulmonary Inflammation.
Ashhurst, AS; Britton, WJ; Chan, HK; Nagalingam, G; Parumasivam, T, 2017
)
" Designing rational dosage regimens for patients to maximize the antimicrobial activity and minimize the emergence and prevalence of resistance is recommended."( Systematic Review of Antimicrobial Resistance of Clinical Acinetobacter baumannii Isolates in Iran: An Update.
Ardebili, A; Mardaneh, J; Razavi Nikoo, H, 2017
)
" The results obtained indicate that adsorption of rifampicin on the copper nanoparticles surface might provide the reduction of antibiotic dosage and prevent its adverse side effects."( Green synthesis of rifampicin-loaded copper nanoparticles with enhanced antimicrobial activity.
Jarek, M; Jurga, S; Langer, K; Nowaczyk, G; Peplińska, B; Przysiecka, Ł; Wiesner, M; Woźniak-Budych, MJ, 2017
)
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
"We compared the pharmacokinetics of moxifloxacin during rifampicin co-treatment or when dosed alone in African patients with drug-susceptible recurrent TB."( Effect of rifampicin and efavirenz on moxifloxacin concentrations when co-administered in patients with drug-susceptible TB.
Adamson, J; Chirehwa, M; Denti, P; Essack, S; Govender, K; Kimba-Phongi, E; McIlleron, H; Naidoo, A; Naidoo, K; Padayatchi, N; Yende-Zuma, N, 2017
)
" Only 4 cases received rifampicin on a daily basis for pulmonary tuberculosis treatment and the others were on intermittent dosing schedule for pulmonary tuberculosis or leprosy treatment."( Rifampicin-induced disseminated intravascular coagulation in pulmonary tuberculosis treatment: A case report and literature review.
Chen, G; He, JQ, 2017
)
" The dose-response sensorgrams of BSA upon increasing concentration of refampicin were attained in SPR analysis."( Kinetic and thermodynamic study of bovine serum albumin interaction with rifampicin using surface plasmon resonance and molecular docking methods.
Dolatabadi, JE; Fathi, F; Jafari, B; Rashidi, M; Rashidi, MR; Sharifi, M; Tajalli, H, 2017
)
"" This could be due to the incomplete selection pressure by an inadequate RIF exposure caused by various factors including a low-RIF dosage being used widely and poor Directly observed treatment."( Are WHO approved nucleic acid amplification tests causing large-scale "false identification" of rifampicin-resistant tuberculosis?: Programmatic experience from south india.
Ambika, AP; Balakrishnan, R; Kottuthodi, RP; Moosan, H; Mrithunjayan, SK; Sanker, P; Santhosh, VT,
)
" The aim of this analysis was to characterize factors contributing to the variability in exposure and to evaluate drug exposures using alternative doses, thus providing evidence to support revised dosing recommendations for drug-susceptible and multidrug-resistant tuberculosis (MDR-TB)."( Pharmacokinetics of Pyrazinamide and Optimal Dosing Regimens for Drug-Sensitive and -Resistant Tuberculosis.
Chirehwa, MT; Denti, P; McIlleron, H; Mthiyane, T; Onyebujoh, P; Rustomjee, R; Smith, P, 2017
)
" The developed approach can lead to improved patient compliance and reduced dosing in future, offering improved treatment of tuberculosis."( Conjugated and Entrapped HPMA-PLA Nano-Polymeric Micelles Based Dual Delivery of First Line Anti TB Drugs: Improved and Safe Drug Delivery against Sensitive and Resistant Mycobacterium Tuberculosis.
Bhaskar, N; Chauhan, DS; Gothwal, A; Gupta, U; Gupta, UD; Khan, I; Pachouri, PK; Upadhyay, S, 2017
)
" Factors associated with low Cmax were NAT2 metabolizer phenotype status for isoniazid; height, dosage and HIV coinfection status for rifampin; height for pyrazinamide; and age, dosage and HIV coinfection status for ethambutol."( Evaluation of the Adequacy of the 2010 Revised World Health Organization Recommended Dosages of the First-line Antituberculosis Drugs for Children: Adequacy of Revised Dosages of TB Drugs for Children.
Adu Awhireng, E; Antwi, S; Dompreh, A; Enimil, A; Gillani, FS; Kwara, A; Ortsin, A; Owusu, M; Peloquin, CA; Wiesner, L; Yang, H, 2018
)
" There is a need for more research on optimization of dosing to maximize efficacy and safety of currently used drugs."( Food significantly reduces plasma concentrations of first-line anti-tuberculosis drugs.
Chandrasekaran, V; Kawaskar, M; Kumar, AK; Kumar, AKH; Lavanya, J; Ramachandran, G; Swaminathan, S, 2017
)
" The results from these studies were incorporated into the Food and Drug Administration-approved product label, providing guidance for panobinostat dosing recommendations when it is combined with other drugs."( Physiologically Based Pharmacokinetic Model Predictions of Panobinostat (LBH589) as a Victim and Perpetrator of Drug-Drug Interactions.
Chun, DY; Einolf, HJ; Gu, H; He, H; Lin, W; Mangold, JB; Wang, L; Won, CS, 2017
)
"Treatment with standardized antituberculosis regimens dosed daily throughout, high uptake of antiretroviral therapy, and low prevalence of isoniazid monoresistance were associated with a low frequency of ADR."( Low Frequency of Acquired Isoniazid and Rifampicin Resistance in Rifampicin-Susceptible Pulmonary Tuberculosis in a Setting of High HIV-1 Infection and Tuberculosis Coprevalence.
Meintjes, G; Rockwood, N; Sirgel, F; Streicher, E; Warren, R; Wilkinson, RJ, 2017
)
"The design and production of an oral dual-compartmental dosage unit (dcDU) was examined in vitro and in vivo with the purpose of physically isolating and modulating the release profile of an anti-tuberculosis drug combination."( Anti-tuberculosis drug combination for controlled oral delivery using 3D printed compartmental dosage forms: From drug product design to in vivo testing.
Boetker, JP; Bohr, A; Colombo, S; Genina, N; Harmankaya, N; Rantanen, J, 2017
)
" As irrational use and inadequate dosing of anti-TB drugs may contribute to the epidemic of drug-resistant TB, we assessed the drug types and dosages prescribed in the treatment of TB cases in a representative sample of health care facilities in Yunnan."( Prescription practice of anti-tuberculosis drugs in Yunnan, China: A clinical audit.
Chen, J; Chiang, CY; Innes, AL; Li, L; Xu, L, 2017
)
" Outcomes of interest included the regimen used in the treatment of new and retreatment TB patients; and the proportion of patients treated with adequate dosing of anti-TB drugs."( Prescription practice of anti-tuberculosis drugs in Yunnan, China: A clinical audit.
Chen, J; Chiang, CY; Innes, AL; Li, L; Xu, L, 2017
)
"2 observed ratio) after daily dosing of midostaurin for 4 days."( Simultaneous Physiologically Based Pharmacokinetic (PBPK) Modeling of Parent and Active Metabolites to Investigate Complex CYP3A4 Drug-Drug Interaction Potential: A Case Example of Midostaurin.
Chun, DY; Dutreix, C; Einolf, HJ; Gu, H; He, H; Ouatas, T; Rebello, S; Wang, L, 2018
)
" Isoniazid, rifampin, and pyrazinamide concentration-time profiles and treatment outcome were obtained from 161 Indian children with drug-sensitive tuberculosis undergoing thrice-weekly dosing as per previous Indian pediatric guidelines."( Suboptimal Antituberculosis Drug Concentrations and Outcomes in Small and HIV-Coinfected Children in India: Recommendations for Dose Modifications.
Bhavani, PK; Dooley, KE; Gangadevi, NP; Guiastrennec, B; Gupta, A; Karlsson, MO; Kumar, AKH; Ramachandran, G; Savic, RM; Swaminathan, S, 2018
)
"The dosage of INH and RIF is minimal in the combination form with the NOR nanoparticles compared to the plain INH and RIF."( Enhancing antimycobacterial activity of isoniazid and rifampicin incorporated norbornene nanoparticles.
Kumarasingam, K; Mane, SR; Shunmugam, R; Sivakumar, S; Uma Devi, KR; Vincent, M,
)
"Low dosage of INH and RIF along with NOR nanocarrier has similar activity to that of INH and RIF; thus this is expected to reduce adverse effects and NOR did not alter the functional activity of INH and RIF, thus becoming eligible for the newer drug carrier in TB treatment."( Enhancing antimycobacterial activity of isoniazid and rifampicin incorporated norbornene nanoparticles.
Kumarasingam, K; Mane, SR; Shunmugam, R; Sivakumar, S; Uma Devi, KR; Vincent, M,
)
" This supports the current 600 mg EFV dosing when coadministered with anti-TB drugs."( Pharmacokinetics of efavirenz in patients on antituberculosis treatment in high human immunodeficiency virus and tuberculosis burden countries: A systematic review.
Atwine, D; Bonnet, M; Taburet, AM, 2018
)
" RMP dosed at 600 mg was administered 2 weeks apart in random sequence."( Quality assurance of rifampicin-containing fixed-drug combinations in South Africa: dosing implications.
Chirehwa, MT; Court, R; Kramer, N; McIlleron, H; Smythe, W; Wiesner, L; Wright, B, 2018
)
"Post-marketing surveillance of in vivo bioavailability of RMP and improved weight band-based dosing are recommended."( Quality assurance of rifampicin-containing fixed-drug combinations in South Africa: dosing implications.
Chirehwa, MT; Court, R; Kramer, N; McIlleron, H; Smythe, W; Wiesner, L; Wright, B, 2018
)
" Many new cases of MDR-TB are created by physician's errors related to drugs regimen, dosing interval and duration of treatment."( Risk Factors for Multidrug-resistant Tuberculosis.
Rumende, CM, 2018
)
" The recommended dosage of rifampicin should be increased to improve efficacy."( Pharmacokinetics of rifampicin in adult TB patients and healthy volunteers: a systematic review and meta-analysis.
Aarnoutse, R; Alffenaar, JWC; Boeree, MJ; Davies, G; Koegelenberg, CFN; McIlleron, H; Peloquin, C; Pertinez, H; Ramachandran, G; Requena-Méndez, A; Ruslami, R; Stott, KE; Sturkenboom, MGG; Swaminathan, S; Tostmann, A, 2018
)
"Subjects were randomly assigned to receive two single 400 mg doses of bedaquiline, alone, and, after a 4 week washout period, in combination with steady-state daily dosing of either rifabutin 300 mg or rifampin 600 mg."( Mycobactericidal activity of bedaquiline plus rifabutin or rifampin in ex vivo whole blood cultures of healthy volunteers: A randomized controlled trial.
Blumer, JL; Good, CE; Griffiss, JM; Healan, A; Jacobs, MR; O'Riordan, MA; Salata, RA; Wallis, RS, 2018
)
" Combined dosing with rifampin or rifabutin produced maximal effects of -0."( Mycobactericidal activity of bedaquiline plus rifabutin or rifampin in ex vivo whole blood cultures of healthy volunteers: A randomized controlled trial.
Blumer, JL; Good, CE; Griffiss, JM; Healan, A; Jacobs, MR; O'Riordan, MA; Salata, RA; Wallis, RS, 2018
)
"Paraguayan children were treated according to the revised paediatric dosing scheme of the World Health Organization."( Evaluation of dried blood spot sampling for pharmacokinetic research and therapeutic drug monitoring of anti-tuberculosis drugs in children.
Aarnoutse, RE; Aguirre, S; Alffenaar, JW; Chaparro, G; Coronel, R; Gomez, R; Gonzalez, F; Huisman, J; Jongedijk, E; Kerkhoff, J; Magis-Escurra, C; Martial, LC; Martinez, N; Molinas, G; Pérez, D; Rodríguez, M; Roman, M; Touw, DJ, 2018
)
"Anti-tuberculosis chemotherapy with a long duration and adequate dosing is the mainstay for treatment of osteoarticular tuberculosis (TB)."( A bioactive implant in situ and long-term releases combined drugs for treatment of osteoarticular tuberculosis.
Cui, X; Li, BN; Li, G; Li, L; Ma, YG; Shi, F; Wang, F; Wang, H; Wang, L; Weng, J; Zhang, C; Zhou, CX; Zhou, Z, 2018
)
" The Emax Hill equation was used to model the dose-response relationship."( Increased activity of linezolid in combination with rifampicin in a murine pneumonia model due to MRSA.
Bu, MX; Li, L; Liao, XP; Liu, YH; Sun, J; Tao, MT; Xiong, YQ; Zhou, YF, 2018
)
" Higher rifampicin doses have been associated with better bactericidal activity, but optimal dosing is uncertain."( The Potential for Treatment Shortening With Higher Rifampicin Doses: Relating Drug Exposure to Treatment Response in Patients With Pulmonary Tuberculosis.
Aarnoutse, R; Boeree, MJ; Churchyard, G; Dawson, R; Diacon, AH; Gillespie, SH; Heinrich, N; Hoelscher, M; Kibiki, GS; Konsten, S; Minja, LT; Ntingiya, NE; Phillips, PPJ; Sanne, I; Simonsson, USH; Svensson, EM; Svensson, RJ; Te Brake, LHM, 2018
)
" Optimizing rifampicin dosage while preventing toxicity is a clinical priority."( The Potential for Treatment Shortening With Higher Rifampicin Doses: Relating Drug Exposure to Treatment Response in Patients With Pulmonary Tuberculosis.
Aarnoutse, R; Boeree, MJ; Churchyard, G; Dawson, R; Diacon, AH; Gillespie, SH; Heinrich, N; Hoelscher, M; Kibiki, GS; Konsten, S; Minja, LT; Ntingiya, NE; Phillips, PPJ; Sanne, I; Simonsson, USH; Svensson, EM; Svensson, RJ; Te Brake, LHM, 2018
)
" Combinations of optimal dose and release rates were simulated such that plasma concentrations were maintained over the epidemiological cut-off or minimum inhibitory concentration for the dosing interval."( Modelling the long-acting administration of anti-tuberculosis agents using PBPK: a proof of concept study.
Flexner, C; Moss, DM; Owen, A; Podany, AT; Rajoli, RKR; Siccardi, M; Swindells, S, 2018
)
" These results suggested that this GEN-CS/INH/RMP NGPs inhalation powder would be a more useful dosage form than separate dose of INH or RMP for MTB."( Genipin-crosslinked carboxymethyl chitosan nanogel for lung-targeted delivery of isoniazid and rifampin.
Cai, X; Chen, T; Guo, L; Liao, W; Ma, D; Tan, W; Wang, W; Wu, T; Xiang, W; Yu, W; Zhang, J; Zhou, J, 2018
)
" Plasma samples for ertugliflozin pharmacokinetic analysis were collected during 72hours after dosing on day 1 of period 1 and day 8 of period 2 and analyzed using a validated HPLC-MS/MS method."( Effect of Rifampin on the Pharmacokinetics of Ertugliflozin in Healthy Subjects.
Cutler, DL; Dawra, VK; Hickman, A; Liang, Y; Matschke, K; Sahasrabudhe, V; Saur, D; Shi, H; Terra, SG, 2018
)
" Trials were heterogenous in terms of dosing of interventions and outcome measures."( Antibiotics for treating scrub typhus.
El Sayed, I; Hine, P; Liu, Q; Wee, I, 2018
)
" We evaluated plasma drug concentrations of rifampicin (RIF), isoniazid (INH), pyrazinamide (PZA), and ethambutol (EMB) among children undergoing TB treatment in Tanzania when these dosing recommendations were being implemented."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
" Differences in median drug concentrations were compared on the basis of the weight-based dosing strategy using the Mann-Whitney U test."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
"Among this cohort of human immunodeficiency virus-negative Tanzanian children, use of the revised dosing strategy for treating childhood TB did not result in the target drug concentration for RIF, INH, or EMB being reached."( Pharmacokinetics of First-Line Drugs Among Children With Tuberculosis in Rural Tanzania.
Augustino, D; Gratz, J; Heysell, SK; Houpt, ER; Justine, M; Kibiki, GS; Kivuyo, S; Mduma, E; Mfinanga, S; Mmbaga, B; Nicodemu, I; Peloquin, CA; Thomas, TA; Yeconia, A; Zagurski, T, 2020
)
" CYP2B6 genotyping but not anti-tuberculosis co-treatment should guide efavirenz dosing to optimize treatment outcomes."( Long-term efavirenz pharmacokinetics is comparable between Tanzanian HIV and HIV/Tuberculosis patients with the same CYP2B6*6 genotype.
Aklillu, E; Bertilsson, L; Burhenne, J; Janabi, M; Kitabi, EN; Minzi, OMS; Mugusi, F; Mugusi, S; Sasi, P, 2018
)
" In treating the patients with NTM, we were able to maintain an adequate blood concentration of CNI by decreasing the dosage from one-half to one-quarter."( Management of De Novo Mycobacterial Infection After Lung Transplantation Without Rifampicin: Case Series of a Single Institution.
Matsuda, Y; Noda, M; Oishi, H; Okada, Y; Sado, T; Suzuki, H; Tamada, T; Watanabe, T; Yamada, M, 2018
)
"Revised WHO dosing does not increase incidence of hepatitis compared to old dosing in HIV negative children."( Revised Antituberculosis Drug Doses and Hepatotoxicity in HIV Negative Children.
Indumathi, CK; Jain, S; Krishnamurthy, S; Sethuraman, A, 2019
)
"Pharmacokinetic studies in the past have shown inadequate antituberculosis drug levels in children with the currently available dosing regimens."( Optimization of dosing regimens of isoniazid and rifampicin in children with tuberculosis in India.
Aruldhas, BW; Bose, A; Hoglund, RM; Mathew, BS; Mathew, SK; Ranjalkar, J; Tarning, J; Verghese, VP, 2019
)
" For rifampicin, a novel dosing regimen was developed to ensure adequate drug concentrations in children."( Optimization of dosing regimens of isoniazid and rifampicin in children with tuberculosis in India.
Aruldhas, BW; Bose, A; Hoglund, RM; Mathew, BS; Mathew, SK; Ranjalkar, J; Tarning, J; Verghese, VP, 2019
)
" Although no studies have been performed, anti-tuberculosis treatment may also have to be prolonged or intensified in terms of regimen or drug dosage if DM is present."( Clinical management of combined tuberculosis and diabetes.
Harries, AD; Hill, PC; Koesoemadinata, R; van Crevel, R, 2018
)
", drug dosing and drug elimination curves) based on previously obtained PK parameters."( In vitro Pharmacokinetic Cell Culture System that Simulates Physiologic Drug and Nanoparticle Exposure to Macrophages.
Kutscher, HL; Morse, GD; Prasad, PN; Reynolds, JL, 2019
)
"Pharmacokinetics studies recommend increasing efavirenz dosage in tuberculosis/HIV patients using rifampicin."( Daily 800 mg versus 600 mg Efavirenz for HIV Patients Treating Tuberculosis with a Rifampicin-Based Regimen: An Open Label Randomized Controlled Trial.
do Brasil, PEAA; Hadad, DJ; Maia, IR; Rolla, V; Sant'anna, FM; Schmaltz, CAS; Trajman, A; Xavier, MS, 2018
)
" To show clinical relevance, we use quantitative systems pharmacology computational models for in vitro-in vivo translation of the experimental results and to identify favorable dosing regimens for one of the tested drugs."( Translational Assessment of Drug-Induced Proximal Tubule Injury Using a Kidney Microphysiological System.
Cirit, M; Himmelfarb, J; Kelly, EJ; Maass, C; Sorensen, NB; Stokes, CL, 2019
)
" Patients with severe illness received high-dose rifampicin immediately, the others had a higher dosage guided by therapeutic drug monitoring."( High-dose rifampicin in tuberculosis: Experiences from a Dutch tuberculosis centre.
Aarnoutse, R; Bergsma-de Guchteneire, I; Boeree, M; Hoefsloot, W; Kuipers, S; Magis-Escurra, C; Seijger, C; Te Brake, L; van Crevel, R; van Ingen, J, 2019
)
" Measurement of drug exposures could be used as a tool/guide to increase rifampicin dosage if a reduced medication absorption or a poor treatment outcome is suspected."( High-dose rifampicin in tuberculosis: Experiences from a Dutch tuberculosis centre.
Aarnoutse, R; Bergsma-de Guchteneire, I; Boeree, M; Hoefsloot, W; Kuipers, S; Magis-Escurra, C; Seijger, C; Te Brake, L; van Crevel, R; van Ingen, J, 2019
)
" Olanzapine and samidorphan pharmacokinetic parameters were determined after OLZ/SAM dosing on days 1 and 22."( A Phase I Open-Label Study to Evaluate the Effects of Rifampin on the Pharmacokinetics of Olanzapine and Samidorphan Administered in Combination in Healthy Human Subjects.
Kumar, V; McDonnell, D; Sun, L; von Moltke, L; Yu, M, 2019
)
" Simulated weight and PNA-based intravenous dosing regimens administered once daily (<14 days PNA, 8 mg/kg; ≥14 days PNA, 15 mg/kg) in infants resulted in comparable exposures to adults receiving therapeutic doses of rifampin against staphylococcal infections and TB."( Rifampin Pharmacokinetics and Safety in Preterm and Term Infants.
Anand, R; Benjamin, DK; Boakye-Agyeman, F; Cohen-Wolkowiez, M; Cotten, CM; Hudak, ML; Laughon, MM; Lewandowski, A; Poindexter, BB; Smith, PB; Sullivan, JE, 2019
)
" Stochastic PK/pharmacodynamic (PD) simulations were carried out to evaluate current regimen combinations and dosing guidelines in distinct patient strata."( Tuberculosis drugs' distribution and emergence of resistance in patient's lung lesions: A mechanistic model and tool for regimen and dose optimization.
Bang, H; Barry, CE; Dartois, V; Eum, S; Fox, WS; Gupta, SV; Lee, M; Savic, RM; Shim, T; Strydom, N; Via, LE; Zimmerman, M, 2019
)
"Anthropometric, genetic, and dosage characteristics of Mexican patients with TB are an important source of risk for subtherapeutic plasma concentrations of anti-TB drugs."( Anthropometric and Genetic Factors Associated With the Exposure of Rifampicin and Isoniazid in Mexican Patients With Tuberculosis.
Huerta-García, AP; Magaña-Aquino, M; Medellín-Garibay, SE; Milán-Segovia, RDC; Ortiz-Álvarez, A; Portales-Pérez, DP; Rodríguez-Pinal, CJ; Romano-Moreno, S; Salazar-González, RA, 2019
)
" Higher or more frequent dosing is needed to improve TB treatment outcomes in India."( Subtherapeutic Rifampicin Concentration Is Associated With Unfavorable Tuberculosis Treatment Outcomes.
Agibothu Kupparam, HK; Balasubramanian, U; Chandrasekaran, P; Dhanasekaran, K; Dooley, KE; Gaikwad, S; Golub, J; Gupta, A; Gupte, A; Gupte, N; Hanna, LE; Kadam, D; Kagal, A; Kulkarni, V; Mave, V; Murali, L; Paradkar, M; Pradhan, N; Ramachandran, G; Shivakumar, SVBY; Sivaramakrishnan, GN; Swaminathan, S; Thiruvengadam, K; Thomas, B, 2020
)
"To evaluate the proportion of children with lopinavir Cmin ≥1 mg/L when receiving a novel 8-hourly lopinavir/ritonavir dosing strategy during rifampicin co-treatment."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
" Rifampicin was dosed at 10-20 mg/kg/day."( Pharmacokinetics of adjusted-dose 8-hourly lopinavir/ritonavir in HIV-infected children co-treated with rifampicin.
McIlleron, H; Rabie, H; Rawizza, H; Van Rie, A; Wiesner, L; Winckler, J; Zar, H; Zuidewind, P, 2019
)
" Midazolam, caffeine, and TMU concentrations were assessed at baseline and following dosing of rifampicin (300 mg daily) for 7 days."( Identification of the caffeine to trimethyluric acid ratio as a dietary biomarker to characterise variability in cytochrome P450 3A activity.
Hopkins, A; Marshall, JC; Miners, JO; Rowland, A; Sorich, MJ; van Dyk, M; Wood, LS, 2019
)
" To assess maximal hepatic CYP3A4 induction, oral rifampin (600 mg daily) should be dosed for > 10 days."( Guidance for Rifampin and Midazolam Dosing Protocols To Study Intestinal and Hepatic Cytochrome P450 (CYP) 3A4 Induction and De-induction.
Kapetas, AJ; Rodrigues, AD; Rowland, A; Sorich, MJ, 2019
)
" WHO dosing guidelines for drugs for tuberculosis treatment are based only on weight, which might lead to systematic underdosing and poor outcomes in these children."( Alternative dosing guidelines to improve outcomes in childhood tuberculosis: a mathematical modelling study.
Dodd, PJ; Dooley, KE; Garcia-Prats, AJ; Hesseling, AC; McKenna, L; Radtke, KK; Savic, RM, 2019
)
" We estimated tuberculosis treatment outcomes in children younger than 5 years following WHO guidelines (children are dosed by weight bands corresponding to the number of fixed-dose combination tablets [75 mg rifampicin, 50 mg isoniazid, 150 mg pyrazinamide]) and two alternative dosing strategies: one based on a proposed algorithm that uses age, weight, and available formulations, in which underweight children would receive the same drug doses as would normal weight children of the same age; and another based on an individualised algorithm without dose limitations, in which derived doses results in target exposure attainment for the typical child."( Alternative dosing guidelines to improve outcomes in childhood tuberculosis: a mathematical modelling study.
Dodd, PJ; Dooley, KE; Garcia-Prats, AJ; Hesseling, AC; McKenna, L; Radtke, KK; Savic, RM, 2019
)
"We estimated that 57 234 (43%) of 133 302 children younger than 5 years who were treated for tuberculosis in 2017 were underdosed with WHO dosing and only 47% of children would reach the rifampicin exposure target."( Alternative dosing guidelines to improve outcomes in childhood tuberculosis: a mathematical modelling study.
Dodd, PJ; Dooley, KE; Garcia-Prats, AJ; Hesseling, AC; McKenna, L; Radtke, KK; Savic, RM, 2019
)
"This work shows that a simple change in dosing procedure to include age and nutritional status, requiring no additional measurements or new drug formulations, is one approach to improve tuberculosis treatment outcomes in children, especially malnourished children who are at high risk of mortality."( Alternative dosing guidelines to improve outcomes in childhood tuberculosis: a mathematical modelling study.
Dodd, PJ; Dooley, KE; Garcia-Prats, AJ; Hesseling, AC; McKenna, L; Radtke, KK; Savic, RM, 2019
)
"We aim to optimize the paediatric dosing regimen of isoniazid, rifampicin and pyrazinamide for the first-line treatment of tuberculosis, based on a fixed dose combination (FDC) mini-tablet using simulations."( Optimization of a paediatric fixed dose combination mini-tablet and dosing regimen for the first line treatment of tuberculosis.
Dokoumetzidis, A; Nalda-Molina, R; Sfouni, M; Tsiligiannis, A, 2019
)
" The final analysis data set contained 17,725 observations from 1,054 subjects, including healthy subjects and subjects with drug-sensitive, multidrug-resistant, or extensively drug-resistant pulmonary tuberculosis dosed pretomanid in monotherapy or combination therapy for up to 6 months."( Population Pharmacokinetics of the Antituberculosis Agent Pretomanid.
Everitt, D; Nedelman, JR; Salinger, DH; Subramoney, V, 2019
)
" The established PBPK model was capable of accurately predicting complex rifampicin-induced alterations in the profiles of glibenclamide, repaglinide, and coproporphyrin I (an endogenous biomarker of OATP1B activities) with various dosing regimens."( Expanded Physiologically-Based Pharmacokinetic Model of Rifampicin for Predicting Interactions With Drugs and an Endogenous Biomarker via Complex Mechanisms Including Organic Anion Transporting Polypeptide 1B Induction.
Asaumi, R; Imawaka, H; Kusuhara, H; Lee, W; Menzel, K; Nunoya, KI; Sugiyama, Y, 2019
)
" To investigate in vivo OATP induction, RIF (18 mg/kg per day) was orally dosed to cynomolgus monkeys for 7 days."( Organic Anion-Transporting Polypeptide Genes Are Not Induced by the Pregnane X Receptor Activator Rifampin: Studies in Hepatocytes In Vitro and in Monkeys In Vivo.
Lai, Y; Murakami, E; Niu, C; Smith, B; Subramanian, R; Tep, S; Wang, Y; Zhao, X, 2019
)
"There is a need for individualized dosing of isoniazid and rifampicin based on plasma concentration measurements (therapeutic drug monitoring) and for clinical trials on higher doses of these TB drugs in patients with TB and DM."( Effect of diabetes mellitus on TB drug concentrations in Tanzanian patients.
Aarnoutse, RE; Boeree, MJ; Burger, DM; Colbers, A; Irongo, CF; Kibiki, GS; Mtabho, CM; Semvua, HH; Tostmann, A; van Crevel, R; van den Boogaard, J; van der Ven, AJAM, 2019
)
" By combining parallel experimental evolution with high-throughput dose-response measurements, we measure phenotypic profiles of collateral sensitivity and resistance for a total of 900 mutant-drug combinations."( Pervasive and diverse collateral sensitivity profiles inform optimal strategies to limit antibiotic resistance.
Maltas, J; Wood, KB, 2019
)
" Our objective was to characterize the relationship between rifampicin exposures and mortality in order to identify optimal dosing for tuberculous meningitis."( Model-Based Meta-analysis of Rifampicin Exposure and Mortality in Indonesian Tuberculous Meningitis Trials.
Aarnoutse, RE; Dian, S; Ganiem, AR; Ruslami, R; Svensson, EM; Te Brake, L; Van Crevel, R; van Laarhoven, A; Yunivita, V, 2020
)
" Further studies are needed to identify appropriate regimens with adequate dosing of ATT for the management of paediatric TBM to improve treatment outcomes."( Tuberculous meningitis in children: Clinical management & outcome.
Daniel, BD; Grace, GA; Natrajan, M, 2019
)
"The addition of a single dose of lorlatinib to daily dosing with rifampin significantly reduced lorlatinib plasma exposure relative to a single dose of lorlatinib administered alone and was associated with severe but self-limiting transaminase elevations in all healthy participants."( The Effect of Rifampin on the Pharmacokinetics and Safety of Lorlatinib: Results of a Phase One, Open-Label, Crossover Study in Healthy Participants.
Bergeron, M; Chen, J; Ginman, K; James, LP; Lee, K; Pawlak, S; Peltz, G; Pithavala, YK; Xu, H, 2020
)
"The weight-band dosing in tuberculosis treatment regimen has been implemented in clinical practice for decades."( Rifampicin Can Be Given as Flat-Dosing Instead of Weight-Band Dosing.
Aarnoutse, R; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Svensson, RJ, 2020
)
"Rifampicin exposure were simulated using previously published population pharmacokinetics model at dose 10-40 mg/kg for weight-band dosing and dose 600-2400 mg for flat-dosing."( Rifampicin Can Be Given as Flat-Dosing Instead of Weight-Band Dosing.
Aarnoutse, R; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Svensson, RJ, 2020
)
"The difference of median AUC0-24 h of all dose groups between flat-dosing and weight-band dosing were considered low (< 20%) except for the lowest dose."( Rifampicin Can Be Given as Flat-Dosing Instead of Weight-Band Dosing.
Aarnoutse, R; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Svensson, RJ, 2020
)
"Weight-band dosing yields a small and non-clinically relevant decrease in variability of AUC0-24h."( Rifampicin Can Be Given as Flat-Dosing Instead of Weight-Band Dosing.
Aarnoutse, R; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Svensson, RJ, 2020
)
"Linezolid is increasingly used for the treatment of tuberculosis resistant to first-line agents, but the most effective dosing strategy is yet unknown."( Fourteen-Day Bactericidal Activity, Safety, and Pharmacokinetics of Linezolid in Adults with Drug-Sensitive Pulmonary Tuberculosis.
Burger, DA; Dawson, R; De Jager, VR; Diacon, AH; Everitt, D; Mendel, CM; Narunsky, K; Nedelman, J; Pappas, F; Vanker, N, 2020
)
" We discuss the epidemiology, pathophysiology and management of rifampicin induced shock, concluding that clinicians should be aware of this rare, but potential adverse effect, and be aware that adverse reactions to rifampicin are more frequent during re-exposure or longer dosing interval regimes."( Rifampicin induced shock during re-exposure for treatment of latent tuberculosis.
Harlow, CF; Harris, T; Kon, OM; Martin, L; Meghji, J, 2020
)
" The current PBPK model, which considers changes in unbound potency-adjusted active species, can be used to inform dosing recommendations when abemaciclib is coadministered with CYP3A4 perpetrators."( Predicting Clinical Effects of CYP3A4 Modulators on Abemaciclib and Active Metabolites Exposure Using Physiologically Based Pharmacokinetic Modeling.
Dickinson, GL; Hall, SD; Kulanthaivel, P; Morse, BL; Posada, MM; Turner, PK, 2020
)
" Urine rifampin absorbance (Abs) was then determined from timed specimens from children treated for TB in Tanzania, and compared to serum pharmacokinetic measurements collected throughout the dosing interval."( Determination of Rifampin Concentrations by Urine Colorimetry and Mobile Phone Readout for Personalized Dosing in Tuberculosis Treatment.
Al-Shaer, MH; Criddle, S; Heysell, SK; Justine, M; Mduma, E; Mpagama, S; Peloquin, C; Rao, P; Szipszky, C; Thomas, TA; Van Aartsen, D; Vinnard, C; Zentner, I, 2021
)
" The objectives of this study are to (1) identify covariate(s) that may explain the variation of rifampicin, which is the key antitubercular agent, under the steady-state by evaluating its population pharmacokinetics and (2) to propose an appropriate dosing method of rifampicin to Japanese patients."( The Population Pharmacokinetics of Rifampicin in Japanese Pulmonary Tuberculosis Patients.
Atsuda, K; Kobayashi, M; Kohno, H; Koike, Y; Maruoka, D; Nagai, H; Nishimura, T, 2020
)
" New data on optimal drug selection and dosing are emerging with the inclusion of children in clinical trials and ongoing research on age-related pharmacokinetics and pharmacodynamics."( Tuberculosis treatment in children: The changing landscape.
Huynh, J; Marais, BJ; Schaaf, HS; Thwaites, G, 2020
)
" We aimed to evaluate the actual rifampicin dosing regimens using a population pharmacokinetic model of rifampicin in patients with osteoarticular infections."( Evaluation of current dosing guidance for oral rifampicin treatment in adult patients with osteoarticular infections.
Allanioux, L; Blin, O; Dupouey, J; Guilhaumou, R; Marsot, A; Ménard, A, 2020
)
"A 10-day HFIM was utilized to simulate human pharmacokinetics (PK) of various PMB, MEM and RIF dosing regimens against a clinical KPC-Kp isolate, with total and resistant subpopulations quantified to capture PD response."( In pursuit of the triple crown: mechanism-based pharmacodynamic modelling for the optimization of three-drug combinations against KPC-producing Klebsiella pneumoniae.
Bulitta, JB; Bulman, ZP; Forrest, A; Holden, PN; Li, J; Nation, RL; Onufrak, NJ; Satlin, MJ; Smith, NM; Tan, X; Tsuji, BT, 2020
)
" Based on pharmacokinetics, safety, and efficacy data, and PBPK modeling, dosing modifications for ribociclib recommend avoiding concurrent use of strong CYP3A inhibitors/inducers, and caution regarding using CYP3A substrates with narrow therapeutic indices."( Ribociclib Drug-Drug Interactions: Clinical Evaluations and Physiologically-Based Pharmacokinetic Modeling to Guide Drug Labeling.
Chakraborty, A; Dhuria, SV; Elmeliegy, M; He, H; Heimbach, T; Huth, F; Ji, Y; Miller, M; Samant, TS; Schiller, H; Umehara, K, 2020
)
" Since 25% of the drug resistance was attributable to sanctuary EPTB sites notorious for poor rifampin penetration, we hypothesize that poor anti-tuberculosis drug dosing might have a role in the development of resistance."( Machine learning reveals that Mycobacterium tuberculosis genotypes and anatomic disease site impacts drug resistance and disease transmission among patients with proven extra-pulmonary tuberculosis.
Magazi, BT; Malinga, LA; Maningi, NE; Mbelle, NN; Pasipanodya, JG; Shey, BA; Sibandze, DB, 2020
)
" Side effects of rifampicin are rare with the once-a-month dosage regimen of anti-leprosy multidrug therapy."( Case Report: Rifampicin-Induced Thrombocytopenia in a Patient with Borderline Lepromatous Leprosy.
Jing, Z; Shi, C; Shui, T; Yang, D; Zhu, J, 2020
)
" In conclusion, CMC-RIF and AA-INH may be useful for the formulation of a site-specific solid dosage form to overcome some of the main obstacles in tuberculosis treatment."( Anti-tuberculosis site-specific oral delivery system that enhances rifampicin bioavailability in a fixed-dose combination with isoniazid.
Litterio, NJ; Lorenzutti, AM; Luciani-Giacobbe, LC; Olivera, ME; Ramírez-Rigo, MV, 2021
)
" The aim of this work was to develop and characterise rifapentine (RPT)-loaded PLGA-based nanoparticles (NPs) for reducing dosing frequency."( Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice.
Chen, J; Li, X; Liang, Q; Luo, C; Ma, X; Song, X; Tian, Z; Xiang, H; Zhao, W, 2020
)
"The application of PLGA-based NPs as sustained-release delivery vehicles for RPT could prolong drug release, modify pharmacokinetics, increase antitubercular activity and diminish toxicity, thereby allowing low dosage and frequency."( Development of Rifapentine-Loaded PLGA-Based Nanoparticles: In vitro Characterisation and in vivo Study in Mice.
Chen, J; Li, X; Liang, Q; Luo, C; Ma, X; Song, X; Tian, Z; Xiang, H; Zhao, W, 2020
)
" Blood sampling was also performed 120  minutes after dosing for the detection of Cmax purpose."( Effect of interval between food intake and drug administration at fasting condition on the plasma concentrations of first-line anti-tuberculosis drugs in Chinese population.
Chu, N; Du, Y; Guo, R; Han, X; Pang, Y; Wang, J; Wang, Q, 2020
)
" Measuring the pharmacodynamic (PD) efficacy of FIR on DNL provides a unique opportunity to determine optimal dosing strategies for liver-targeted OATP substrates in settings of altered OATP function."( Organic Anion Transporting Polypeptide Inhibition Dramatically Increases Plasma Exposure but not Pharmacodynamic Effect nor Inferred Hepatic Intracellular Exposure of Firsocostat.
Ampaw, L; Beysen, C; Garrison, KL; Kearney, BP; Kirby, BJ; Lutz, JD; Mathias, A; Myers, RP; Qin, AR; Yue, MS, 2021
)
"Overuse or abuse of antibiotics has undoubtedly accelerated the increasing prevalence of global antibiotic resistance crisis, and thus, people have been trying to explore approaches to decrease dosage of antibiotics or find new antibacterial agents for many years."( The Synergistic Effect of Mud Crab Antimicrobial Peptides Sphistin and Sph
Chen, F; Liu, J; Peng, H; Wang, KJ; Wang, X; Zhang, H, 2020
)
" Meanwhile, reducing the dosing of SLIDs to thrice weekly from Day 1, and their replacement for any degree of audiometry abnormalities before or during treatment will largely avoid serious ototoxicity."( Second-line injectable drugs for rifampicin-resistant tuberculosis: better the devil we know?
de Jong, BC; Decroo, T; Tahseen, S; Van Deun, A, 2021
)
" As a guide to determining dosing regimens in pediatric studies, the verified PBPK model, along with UGT enzyme ontogeny maturation understanding, was used for predictions of dapagliflozin monotherapy exposures in pediatric subjects aged 1 month to 18 years that best matched exposure in adult patients with a 10-mg single dose of dapagliflozin."( Model-Informed Pediatric Dose Selection for Dapagliflozin by Incorporating Developmental Changes.
Boulton, DW; Jo, H; Parkinson, J; Pilla Reddy, V; Tang, W, 2021
)
"Daptomycin is increasingly used in the treatment of bone and joint infection (BJI), but its pharmacokinetics (PK) and dosage requirements have not been thoroughly investigated in this indication."( Population pharmacokinetics of daptomycin in patients with bone and joint infection: minimal effect of rifampicin co-administration and confirmation of a sex difference.
Bourguignon, L; Bricca, R; Conrad, A; Ferry, T; Gagnieu, MC; Garreau, R; Goutelle, S; Roux, S, 2021
)
"To investigate the population PK and dosage requirements of daptomycin in patients with BJI, and examine the influence of rifampicin co-administration."( Population pharmacokinetics of daptomycin in patients with bone and joint infection: minimal effect of rifampicin co-administration and confirmation of a sex difference.
Bourguignon, L; Bricca, R; Conrad, A; Ferry, T; Gagnieu, MC; Garreau, R; Goutelle, S; Roux, S, 2021
)
"A daptomycin dosage of 8 mg/kg/24 h in women and 10 mg/kg/24 h in men should optimize efficacy but may lead to excessive trough concentrations in many patients, especially in women."( Population pharmacokinetics of daptomycin in patients with bone and joint infection: minimal effect of rifampicin co-administration and confirmation of a sex difference.
Bourguignon, L; Bricca, R; Conrad, A; Ferry, T; Gagnieu, MC; Garreau, R; Goutelle, S; Roux, S, 2021
)
" Use for triage to other investigation or personalized dosing strategy should be tested in a randomized study."( Levofloxacin pharmacokinetics in saliva as measured by a mobile microvolume UV spectrophotometer among people treated for rifampicin-resistant TB in Tanzania.
Alffenaar, JC; Heysell, SK; Jongedijk, EM; Mbelele, P; Mohamed, S; Mpagama, S; Mvungi, HC; Rao, P; Sariko, M; Stroup, S; Touw, DJ; van Winkel, CAJ, 2021
)
" Dosing was according to participant bodyweight."( Safety and feasibility of 1 month of daily rifapentine plus isoniazid to prevent tuberculosis in children and adolescents: a prospective cohort study.
Amanullah, F; Becerra, MC; Fareed, U; Farooq, S; Hussain, H; Jaswal, M; Keshavjee, S; Khan, AJ; Khan, H; Malik, AA; Nasir, K; Safdar, N; Shahbaz, S, 2021
)
"A growing amount of evidence suggests that the rifampicin dosing currently recommended for tuberculosis treatment could be associated with inadequate exposure and unfavourable outcomes."( Standard versus high dose of rifampicin in the treatment of pulmonary tuberculosis: a systematic review and meta-analysis.
Alessio, L; Chiodini, P; Coppola, N; Di Caprio, G; Gentile, V; Onorato, L; Russo, A, 2021
)
"To determine an optimal RFP dosing for MDR-MRSP treatment without induction of RFP resistance and identify causal mutations for antimicrobial resistance."( Genomic and in vitro pharmacodynamic analysis of rifampicin resistance in multidrug-resistant canine Staphylococcus pseudintermedius isolates.
Boothe, D; Cao, W; Hathcock, T; Hicks, K; Kennis, R; Tan, Y; Wang, X; White, A; Zhang, D, 2021
)
" The dosing of rifampin had no effect on outcome."( If, When, and How to Use Rifampin in Acute Staphylococcal Periprosthetic Joint Infections, a Multicentre Observational Study.
Albiach, L; Belden, KA; Beldman, M; Carvalho, A; Goswami, K; Jutte, P; Knobben, BAS; Löwik, C; Parvizi, J; Soriano, A; Sousa, R; Wouthuyzen-Bakker, M; Zijlstra, WP, 2021
)
" We then simulated 7-10 day human dosing of minocycline and the combination."( The pharmacodynamics of minocycline alone and in combination with rifampicin against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
Attwood, M; Bowker, KE; MacGowan, AP; Noel, AR, 2021
)
" The addition of simulated free rifampicin associated with dosing 300 mg q12h reduced the 24 h minocycline fAUC/MICs."( The pharmacodynamics of minocycline alone and in combination with rifampicin against Staphylococcus aureus studied in an in vitro pharmacokinetic model of infection.
Attwood, M; Bowker, KE; MacGowan, AP; Noel, AR, 2021
)
"1 ng/mL), resulting in contraception failure, when depot medroxyprogesterone is dosed at 12-week intervals."( A Semimechanistic Pharmacokinetic Model for Depot Medroxyprogesterone Acetate and Drug-Drug Interactions With Antiretroviral and Antituberculosis Treatment.
Cohn, SE; Denti, P; Dooley, KE; Firnhaber, C; Francis, J; Godfrey, C; Kendall, MA; McIlleron, H; Mngqibisa, R; Wu, X, 2021
)
" The model was also used to extrapolate pharmacokinetic exposures from older children with different body surface area to guide dosing in younger children."( Physiologically Based Pharmacokinetic Modeling for Selumetinib to Evaluate Drug-Drug Interactions and Pediatric Dose Regimens.
Cohen-Rabbie, S; Freshwater, T; Jain, L; Schalkwijk, S; Tomkinson, H; Vishwanathan, K; Wild, M; Xu, S; Zhou, D; Zhou, L, 2021
)
" bovis CFU at reduced dosing frequency by drug loaded StM in comparison to control group."( Polyethylene imine conjugated supramolecular stereocomplexed nanomicelles for intracellular delivery of rifampicin against Mycobacterium bovis.
Ali, S; Arshad, R; Aslam, A; Kiani, MH; Qadry, A; Shahnaz, G, 2021
)
" We characterize moxifloxacin population pharmacokinetics and QT interval prolongation and evaluate optimal dosing in children with RR-TB."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
" Model-based simulations of moxifloxacin pharmacokinetics predicted that current dosing recommendations are too low in children."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
" When patients are co-treated with rifampicin, ciprofloxacin dosage should be increased by 50% to 60%."( Ciprofloxacin population pharmacokinetics during long-term treatment of osteoarticular infections.
Aubry, A; Bleibtreu, A; Chauvin, C; Comets, E; Fourniols, E; Funck-Brentano, C; Jaureguiberry, S; Llopis, B; Noe, G; Tissot, N; Urien, S; Zahr, N, 2021
)
"Study A5338 suggested that more frequent depot MPA dosing may be appropriate for women receiving rifampicin, isoniazid, and efavirenz."( Pharmacogenetics of interaction between depot medroxyprogesterone acetate and efavirenz, rifampicin, and isoniazid during treatment of HIV and tuberculosis.
Angira, F; Badal-Faesen, S; Baker, P; Cohn, SE; Denti, P; Francis, J; Haas, DW; Kendall, MA; Mawlana, S; McIlleron, H; Mngqibisa, R; Omoz-Oarhe, A; Robinson, JA; Samaneka, WP, 2022
)
"We conclude that despite availability of clinical evidence, double dosing LPV/r in patients receiving rifampicin-based TB treatment is low in Uganda's public HIV clinics but this does not seem to affect patient survival and viral suppression."( Adoption of evidence-informed guidelines in prescribing protease inhibitors for HIV-Tuberculosis co-infected patients on rifampicin and effects on HIV treatment outcomes in Uganda.
Castelnuovo, B; Haguma, P; Kalibbala, D; Kirenga, B; Muddu, M; Mulindwa, F; Semitala, FC, 2021
)
" We proposed the use of reconstructed granules as a suitable, flexible dosage form and developed an on-site granulation method using a compounding mixer."( Extemporaneous preparation of rifampicin granules from capsules to improve usability.
Kagawa, Y; Miyazaki, Y; Uchino, T, 2023
)
" Furthermore, the weight loss of the granules during the dosing process was significantly lower than that of the capsule powder content."( Extemporaneous preparation of rifampicin granules from capsules to improve usability.
Kagawa, Y; Miyazaki, Y; Uchino, T, 2023
)
" The model was also verified by the observed pharmacokinetics after multiple oral dosing and by the effect of hepatic impairment on esaxerenone pharmacokinetics."( Physiologically based pharmacokinetic modelling to predict the clinical effect of CYP3A inhibitors/inducers on esaxerenone pharmacokinetics in healthy subjects and subjects with hepatic impairment.
Igawa, Y; Ishizuka, H; Ishizuka, T; Shimizu, T; Watanabe, A; Yamada, M, 2022
)
"The Opti-Rif trial enrolled dosing cohorts of 20 children aged 0-12 years, with incremental dose escalation with each subsequent cohort, until achievement of target exposures or safety concerns."( Pharmacokinetics and safety of high-dose rifampicin in children with TB: the Opti-Rif trial.
Aarnoutse, RE; Denti, P; Draper, HR; Fairlie, L; Garcia-Prats, AJ; Hesseling, AC; Karlsson, MO; Masenya, M; Norman, J; Schaaf, HS; Svensson, EM; van der Laan, LE; Wiesner, L; Winckler, J, 2021
)
"All rabbits in group A were treated by INH-RFP-BSA-NPs's injection and in group B were treated with classic dosage form of INH and RFP, while in group C normal saline was given as the blank control."( Treatment of spinal tuberculosis in rabbits using bovine serum albumin nanoparticles loaded with isoniazid and rifampicin.
Chen, Z; Ge, Z; Liang, S; Liu, X; Ma, H; Ma, R; Wu, P; Zhang, J, 2022
)
"In 2010, the World Health Organization (WHO) revised dosing guidelines for treatment of childhood tuberculosis."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
" Nonlinear mixed-effects modeling and simulation was used to design the optimal FDC and weight-band dosing strategy for achieving the pharmacokinetic targets based on literature-derived adult AUC0-24h for rifampicin (38."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
" Optimal dosing of all drugs cannot be achieved with the current FDCs."( Optimizing Dosing and Fixed-Dose Combinations of Rifampicin, Isoniazid, and Pyrazinamide in Pediatric Patients With Tuberculosis: A Prospective Population Pharmacokinetic Study.
Bekker, A; Davies, G; Denti, P; Gonzalez-Martinez, C; Hesseling, AC; McIlleron, HM; Rabie, H; Svensson, EM; van der Laan, LE; van Rie, A; Wasmann, RE; Wiesner, L; Winckler, J; Zar, HJ, 2022
)
" Although ethambutol has been demonstrated to inhibit macrolide resistance, the ethambutol dosage is sometimes decreased due to concerns about optic neuropathy."( Low-dosage ethambutol, less than 12.5 mg/kg/day, does not worsen the clinical outcomes of pulmonary Mycobacterium avium and Mycobacterium intracellulare disease: a retrospective cohort study.
Fujiwara, K; Furuuchi, K; Hanada, K; Kaburaki, S; Kurashima, A; Morimoto, K; Ohta, K; Shiraishi, Y; Tanaka, Y; Uesugi, F; Watanabe, F; Yoshiyama, T, 2022
)
" Daily ethambutol dosage was not identified as a prognostic factor for any of the outcomes."( Low-dosage ethambutol, less than 12.5 mg/kg/day, does not worsen the clinical outcomes of pulmonary Mycobacterium avium and Mycobacterium intracellulare disease: a retrospective cohort study.
Fujiwara, K; Furuuchi, K; Hanada, K; Kaburaki, S; Kurashima, A; Morimoto, K; Ohta, K; Shiraishi, Y; Tanaka, Y; Uesugi, F; Watanabe, F; Yoshiyama, T, 2022
)
"An ethambutol dosage of 12."( Low-dosage ethambutol, less than 12.5 mg/kg/day, does not worsen the clinical outcomes of pulmonary Mycobacterium avium and Mycobacterium intracellulare disease: a retrospective cohort study.
Fujiwara, K; Furuuchi, K; Hanada, K; Kaburaki, S; Kurashima, A; Morimoto, K; Ohta, K; Shiraishi, Y; Tanaka, Y; Uesugi, F; Watanabe, F; Yoshiyama, T, 2022
)
" Among 834 patients initially eligible for the shorter regimen, 385 (46%) may have benefited from reduced drug dosage or removing ineffective drugs when WGS data were considered."( Whole-Genome Sequencing Has the Potential To Improve Treatment for Rifampicin-Resistant Tuberculosis in High-Burden Settings: a Retrospective Cohort Study.
Beisel, C; Borrell, S; Cox, H; Cudahy, PGT; Daniels, J; Dippenaar, A; Doetsch, A; Furin, J; Gagneux, S; Goig, GA; Mohr-Holland, E; Nicol, MP; Reinhard, M; Reuter, A; Salaam-Dreyer, Z; Warren, RM, 2022
)
"It is important to consider the effects of DDIs on the abrocitinib active moiety when making dosing recommendations."( Assessment of the Effects of Inhibition or Induction of CYP2C19 and CYP2C9 Enzymes, or Inhibition of OAT3, on the Pharmacokinetics of Abrocitinib and Its Metabolites in Healthy Individuals.
Connell, CA; Dowty, ME; Le, VH; Malhotra, BK; O'Gorman, MT; Tatulych, S; Tripathy, S; Valdez, H; Wang, X; Winton, JA; Wouters, A; Yin, N, 2022
)
" When a 200-mg single oral dose of belumosudil was coadministered with both rabeprazole and omeprazole, parent and metabolite exposures were largely reduced, suggesting that belumosudil dosage should be increased when given with PPIs."( A Phase 1 Pharmacokinetic Drug Interaction Study of Belumosudil Coadministered With CYP3A4 Inhibitors and Inducers and Proton Pump Inhibitors.
Alabanza, A; Lohmer, L; Patel, J; Schueller, O; Singh, N; Willson, A, 2022
)
"Increased dosing of rifampicin and pyrazinamide seems a viable strategy to shorten treatment and prevent relapse of drug-susceptible tuberculosis (TB), but safety and efficacy remains to be confirmed."( Safety and pharmacokinetics-pharmacodynamics of a shorter tuberculosis treatment with high-dose pyrazinamide and rifampicin: a study protocol of a phase II clinical trial (HighShort-RP).
Alffenaar, JC; Augustinsson, D; Bornefall, A; Carlsson, B; Ekqvist, D; Fredrikson, M; Niward, K; Nordvall, MJ; Paues, J; Sandstedt, M; Simonsson, USH; Sönnerbrandt, M, 2022
)
" The optimal dosing of PAS in children is uncertain, specifically for delayed-release granule preparations, which are the most used."( Pharmacokinetics and Dose Optimization Strategies of Para-Aminosalicylic Acid in Children with Rifampicin-Resistant Tuberculosis.
Chirehwa, M; Denti, P; Donald, PR; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Mao, J; McIlleron, H; Norman, J; Schaaf, HS; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
" Based on the established PBPK model, following repeated dosing of 600 mg rifampicin, the deduced net effect was an approximately threefold induction in P-gp activities in the intestine, liver, and kidney."( Robust physiologically based pharmacokinetic model of rifampicin for predicting drug-drug interactions via P-glycoprotein induction and inhibition in the intestine, liver, and kidney.
Asaumi, R; Nunoya, KI; Sugiyama, Y; Taskar, KS; Yamaura, Y, 2022
)
"In the survey, 86 of 90 (96%) HIV clinics in 18 countries reported prescribing dolutegravir to patients who were receiving rifampicin as part of tuberculosis treatment, with 77 (90%) reporting that they use twice-daily dosing of dolutegravir, of which 74 (96%) reported having 50 mg tablets available to accommodate twice-daily dosing."( Real-world use and outcomes of dolutegravir-containing antiretroviral therapy in HIV and tuberculosis co-infection: a site survey and cohort study in sub-Saharan Africa.
Brazier, E; Chimbetete, C; De Waal, R; Diero, L; Dzudie, A; Ezechi, OC; Fenner, L; Kunzekwenyika, C; Lelo, P; Mahambou-Nsondé, D; Muhairwe, JA; Murenzi, G; Muyindike, WR; Nash, D; Rafael, I; Romo, ML; Sekaggya-Wiltshire, C; Shah, NS; Tiendrebeogo, T; Twizere, C; Wools-Kaloustian, KK; Yotebieng, M, 2022
)
" Understanding potential drug-drug interactions (DDIs) informs proper dosing when co-administering tucatinib with other therapies."( Evaluation of Safety and Clinically Relevant Drug-Drug Interactions with Tucatinib in Healthy Volunteers.
Abdulrasool, LI; Endres, CJ; Lee, A; Mayor, JG; Rustia, EL; Sun, H; Topletz-Erickson, A; Walker, L, 2022
)
" Dosage regimens simulated the human PK of DAL (1500 mg, single dose), vancomycin (VAN) (1000 mg/12 h) and linezolid (LZD) (600 mg/12 h), alone and with RIF (600 mg/24 h)."( Comparative efficacy of dalbavancin alone and with rifampicin against in vitro biofilms in a pharmacodynamic model with methicillin-resistant Staphylococcus aureus.
Benavent, E; El Haj, C; Gomez-Junyent, J; Murillo, O; Rigo-Bonnin, R; Rosselló, I; Sierra, Y; Soldevila, L; Torrejón, B, 2022
)
" This study aimed to develop a population pharmacokinetic model of LPV/r and provide dosage optimization in Thai PLWH."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
" The reduced LPV/r dosage offers sufficient LPV exposure for Thai PLWH."( Dose optimization with population pharmacokinetics of ritonavir-boosted lopinavir for Thai people living with HIV with and without active tuberculosis.
Avihingsanon, A; Chaivichacharn, P; Gatechompol, S; Punyawudho, B; Ubolyam, S, 2022
)
" The potential for genotype-guided dosing during TBM treatment should be further explored in prospective clinical studies."( Pharmacogenetic variability and the probability of site of action target attainment during tuberculosis meningitis treatment: A physiologically based pharmacokinetic modeling and simulations study.
Bisson, GP; Heysell, SK; Kreiswirth, BN; Kurepina, N; Mehta, K; Narayanan, N; Subbian, S; Vinnard, C, 2022
)
" However, given the long dosing interval, the conduct of clinical DDIs studies with LA antiretrovirals is challenging."( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
" An increase in the dosing frequency did not overcome the DDI with rifampicin."( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
"LA cabotegravir/rilpivirine should be avoided with strong inducers but coadministration with moderate inducers is possible by adding oral rilpivirine daily dosing to the monthly injection."( Management of Drug-Drug Interactions Between Long-Acting Cabotegravir and Rilpivirine and Comedications With Inducing Properties: A Modeling Study.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
" They require dosage adjustments, detailed in public and private HIV guidelines."( Training, guideline access and knowledge of antiretroviral interactions: Is the South African private sector being left behind?
Blockman, M; Chisholm, BS; Swart, AM, 2022
)
" Private sector knowledge of dosing changes was lower for all interacting drugs, with the difference only significant for calcium and iron."( Training, guideline access and knowledge of antiretroviral interactions: Is the South African private sector being left behind?
Blockman, M; Chisholm, BS; Swart, AM, 2022
)
" In a high-burden HIV setting such as SA, it is vital that healthcare workers across all professions, in both the public and private sector, know how to adjust antiretroviral dosing due to clinically significant interactions."( Training, guideline access and knowledge of antiretroviral interactions: Is the South African private sector being left behind?
Blockman, M; Chisholm, BS; Swart, AM, 2022
)
" We utilized a randomized, crossover, open (blinded laboratory) and placebo-controlled trial with 600-mg rifampicin or placebo dosed for a week to investigate the effects of PXR activation on erythrocyte, plasma, faecal and urine porphyrins."( Effects of rifampicin on porphyrin metabolism in healthy volunteers.
Hämäläinen, E; Hukkanen, J; Kauppinen, R; Ranta, S; Tolonen, H, 2023
)
" A single-center, open-label, sequential crossover, and self-control study was carried out in 24 healthy subjects to determine the pharmacokinetics of chiglitazar dosed with and without CYP3A4 inhibitors and inducers."( Pharmacokinetic Interaction of Chiglitazar with CYP3A4 Inducer or Inhibitor: An Open-Label, Sequential Crossover, Self-Control, 3-Period Study in Healthy Chinese Volunteers.
Chen, H; Chen, W; Li, H; Li, J; Li, X; Liu, C; Sheng, L; Wu, Y; Xu, H; Yang, M; Yuan, F, 2023
)
" However, daily dosing of diosmin significantly reduced these markers of liver dysfunction, inflammatory cytokines and apoptosis to near normal levels."( Hepatoprotective potential of diosmin against hepatotoxic effect of isoniazid and rifampin in wistar rats.
Ahmed, RA; Alam, MF; Alqahtani, SS; Alruwaili, MN; Alshahrani, S; Anwer, T; Jali, A; Moni, SS,
)
"Although super-boosted lopinavir/ritonavir (LPV/r; ratio 4:4 instead of 4:1) is recommended for infants living with HIV and receiving concomitant rifampicin, in clinical practice, many different LPV/r dosing strategies are applied due to poor availability of pediatric separate ritonavir formulations needed to superboost."( Brief Report: Suboptimal Lopinavir Exposure in Infants on Rifampicin Treatment Receiving Double-dosed or Semisuperboosted Lopinavir/Ritonavir: Time for a Change.
Ballesteros, A; Buck, WC; Burger, DM; Chabala, C; Chitsamatanga, M; Colbers, A; Domínguez-Rodríguez, S; Jacobs, TG; Madrid, L; Moraleda, C; Mujuru, HA; Mumbiro, V; Namuziya, N; Nathoo, KJ; Nduna, B; Passanduca, A; Rojo, P; Tagarro, A, 2023
)
" He was diagnosed with meningitis and the dosage of vancomycin was increased."( Nosocomial meningitis caused by Staphylococcus haemolyticus in a child with neutropenia in the absence of intracranial devices: a case report.
Fujikawa, T; Hasegawa, D; Kasai, M; Kosaka, Y; Mizuno, S; Uemura, S, 2023
)
" Concomitant use with the potent CYP2C9 inducer, rifampin, requires close monitoring and dosage adjustments."( Warfarin-Rifampin-Gene (WARIF-G) Interaction: A Retrospective, Genetic, Case-Control Study.
Abdalazim, W; Bader, L; El-Bardissy, A; Elawady, MI; Elewa, H; Elshafei, MN; Fahmi, AM; Howady, F; Kasem, M; Khalil, A; Mahmoud, H; Salem, M; Sherbash, M, 2023
)
" Our comparative analysis suggests DOAC plasma concentration monitoring as a possible strategy to guide dosing owing to the predictable correlation between DOACs' plasma concentration and effect."( Interactions Between Direct Oral Anticoagulants (DOACs) and Antiseizure Medications: Potential Implications on DOAC Treatment.
Bialer, M; Goldstein, R; Gronich, N; Jacobs, AR; Muszkat, M; Zighan, L, 2023
)
" For patients with the same degree of renal impairment, rifampicin would have a slightly synergistic effect on the increase of 5-hydroxy saxagliptin exposure compared with dosed alone."( Physiologically Based Pharmacokinetic Modeling Characterizes the Drug-Drug Interaction Between Saxagliptin and Rifampicin in Patients With Renal Impairment.
Ke, M; Lin, C; Lin, R; Wu, W; Ye, L, 2023
)
" During the first 2 months of treatment, participants received weight-based dosing of first-line anti-TBdrugs (rifampicin, isoniazid, pyrazinamide and ethambutol), and had plasma drug concentrations measured at 2 and 6 hours after drugadministration during the 8th week of treatment."( Clinical impact of plasma concentrations of first-line antituberculosis drugs.
Naidoo, A; Naidoo, K; Padayatchi, N; Perumal, R, 2023
)
" These present studies provided valuable information that helps inform SHR0302 dosing instructions and concomitant medication precautions."( Effect of CYP3A4 induction and inhibition on the pharmacokinetics of SHR0302 in healthy subjects.
Feng, S; Fu, M; Gao, X; Li, X; Li, Y; Lin, H; Shen, K; Yu, G; Zhang, P; Zhang, Z, 2023
)
" To support dose optimisation of rifampicin, this study investigated new and innovative staggered dosing of rifampicin using clinical trial simulations to minimise tolerability problems and still achieve good efficacy."( Model-based analysis of bactericidal activity and a new dosing strategy for optimised-dose rifampicin.
Aarnoutse, RE; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Te Brake, L, 2023
)
" Furthermore, clinical trial simulations of rifampicin exposure were performed following four different staggered dosing scenarios."( Model-based analysis of bactericidal activity and a new dosing strategy for optimised-dose rifampicin.
Aarnoutse, RE; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Te Brake, L, 2023
)
" Clinical trial simulations of a staggered dosing strategy starting the treatment at a lower dose (20 mg/kg) for 7 days followed by a higher dose (40 mg/kg) predicted a lower initial exposure with lower probability of tolerability problems and better EBA compared with a regimen of 35 mg/kg daily."( Model-based analysis of bactericidal activity and a new dosing strategy for optimised-dose rifampicin.
Aarnoutse, RE; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Te Brake, L, 2023
)
"Staggered dosing of 20 mg/kg for 7 days followed by 40 mg/kg is predicted to reduce tolerability while maintaining exposure levels associated with better efficacy."( Model-based analysis of bactericidal activity and a new dosing strategy for optimised-dose rifampicin.
Aarnoutse, RE; Boeree, MJ; Simonsson, USH; Susanto, BO; Svensson, EM; Te Brake, L, 2023
)
"This in silico extrapolation provides valuable information on dosing regimens and routes of administration against CRAB infections in specific tissues."( Physiologically-based pharmacokinetic modeling to inform dosing regimens and routes of administration of rifampicin and colistin combination against Acinetobacter baumannii.
Lv, Z; Oo, C; Schlender, JF; Song, C; Sy, SKB; Wu, M; Yu, M; Yue, J; Zhang, J; Zhu, P; Zhu, S; Zhu, Y, 2023
)
" This study aimed to identify risk factors for adverse drug reactions (ADRs) or death in very elderly patients with pulmonary tuberculosis and to assess the association between the dosage of antituberculosis drugs and outcomes."( Factors associated with adverse drug reactions or death in very elderly hospitalized patients with pulmonary tuberculosis.
Emoto, R; Kobayashi, H; Matsui, S; Matsuura, A; Mutoh, Y; Nakagawa, T; Ogawa, K; Sakakibara, T; Sano, M; Shindo, Y; Yagi, M, 2023
)
"Pharmacokinetic variability drives tuberculosis (TB) treatment outcomes but measurement of serum drug concentrations for personalised dosing is inaccessible for children in TB-endemic settings."( Rifampin urinary excretion to predict serum targets in children with tuberculosis: a prospective diagnostic accuracy study.
Augustino, D; Handler, D; Heysell, SK; Kagan, L; Lukumay, S; Mduma, E; Mejan, P; Mmbaga, B; Mosha, R; Peloquin, CA; Petros de Guex, K; Pfaeffle, H; Rao, P; Reiss, R; Siemiątkowska, A; Thomas, TA; Vinnard, C; Xie, YL; Yu, S, 2023
)
"Urine spectrophotometry correlated with a clinically relevant serum target for rifampin, representing a step toward personalised dosing for children in TB-endemic settings."( Rifampin urinary excretion to predict serum targets in children with tuberculosis: a prospective diagnostic accuracy study.
Augustino, D; Handler, D; Heysell, SK; Kagan, L; Lukumay, S; Mduma, E; Mejan, P; Mmbaga, B; Mosha, R; Peloquin, CA; Petros de Guex, K; Pfaeffle, H; Rao, P; Reiss, R; Siemiątkowska, A; Thomas, TA; Vinnard, C; Xie, YL; Yu, S, 2023
)
" Linezolid dosing and clinical management was provider driven, and most patients had linezolid adjusted by therapeutic drug monitoring."( Implementation of Bedaquiline, Pretomanid, and Linezolid in the United States: Experience Using a Novel All-Oral Treatment Regimen for Treatment of Rifampin-Resistant or Rifampin-Intolerant Tuberculosis Disease.
Andrino, BB; Ashkin, D; Burgos, M; Caloia, LA; Chen, L; Colon-Semidey, A; DeSilva, MB; Dhanireddy, S; Dorman, SE; Dworkin, FF; Easton, AV; Gaensbauer, JT; Ghassemieh, B; Gomez, ME; Goswami, ND; Haley, CA; Hammond-Epstein, H; Horne, D; Jasuja, S; Jones, BA; Kaplan, LJ; Khan, AE; Kracen, E; Labuda, S; Landers, KM; Lardizabal, AA; Lasley, MT; Letzer, DM; Lopes, VK; Lubelchek, RJ; Mihalyov, A; Misch, EA; Murray, JA; Narita, M; Nilsen, DM; Ninneman, MJ; Ogawa, L; Oladele, A; Overman, M; Patricia Macias, C; Peloquin, CA; Peter Cegielski, J; Ray, SM; Ritger, KA; Rowlinson, MC; Sabuwala, N; Schechter, MC; Schiller, TM; Schwartz, LE; Spitters, C; Thomson, DB; Tresgallo, RR; Valois, P, 2023
)
" Use of individualized linezolid dosing and monitoring likely enhanced safety and treatment completion."( Implementation of Bedaquiline, Pretomanid, and Linezolid in the United States: Experience Using a Novel All-Oral Treatment Regimen for Treatment of Rifampin-Resistant or Rifampin-Intolerant Tuberculosis Disease.
Andrino, BB; Ashkin, D; Burgos, M; Caloia, LA; Chen, L; Colon-Semidey, A; DeSilva, MB; Dhanireddy, S; Dorman, SE; Dworkin, FF; Easton, AV; Gaensbauer, JT; Ghassemieh, B; Gomez, ME; Goswami, ND; Haley, CA; Hammond-Epstein, H; Horne, D; Jasuja, S; Jones, BA; Kaplan, LJ; Khan, AE; Kracen, E; Labuda, S; Landers, KM; Lardizabal, AA; Lasley, MT; Letzer, DM; Lopes, VK; Lubelchek, RJ; Mihalyov, A; Misch, EA; Murray, JA; Narita, M; Nilsen, DM; Ninneman, MJ; Ogawa, L; Oladele, A; Overman, M; Patricia Macias, C; Peloquin, CA; Peter Cegielski, J; Ray, SM; Ritger, KA; Rowlinson, MC; Sabuwala, N; Schechter, MC; Schiller, TM; Schwartz, LE; Spitters, C; Thomson, DB; Tresgallo, RR; Valois, P, 2023
)
"Our simulations support the common practice of maintaining the adjusted dosage of a drug for another 2 weeks after stopping an inducer."( Management of Drug Interactions with Inducers: Onset and Disappearance of Induction on Cytochrome P450 3A4 and Uridine Diphosphate Glucuronosyltransferase 1A1 Substrates.
Battegay, M; Berton, M; Bettonte, S; Marzolini, C; Stader, F, 2023
)
" We used a validated paucibacillary mouse model of TPT in combination with dynamic oral dosing of both drugs to simulate and understand exposure-activity relationships to inform posology for future LAI formulations."( Using Dynamic Oral Dosing of Rifapentine and Rifabutin to Simulate Exposure Profiles of Long-Acting Formulations in a Mouse Model of Tuberculosis Preventive Therapy.
Ammerman, NC; Betoudji, F; Chang, YS; Lee, J; Li, SY; Nuermberger, EL; Owen, A; Pertinez, H; Rannard, SP, 2023
)
" Simulations with clinically utilised dosing regimens confirmed the therapeutic potential of this combination, particularly in the prevention of bacterial regrowth."( Model-informed dose optimisation of polymyxin-rifampicin combination therapy against multidrug-resistant Acinetobacter baumannii.
Bergen, P; Han, ML; Li, J; Lin, YW; Lu, J; Rao, G; Velkov, T; Wickremasinghe, H; Yu, HH; Zhao, J; Zhou, QT; Zhu, Y, 2023
)
" As plasma CP-I's sensitivity, specificity, and selectivity have been validated in humans, monitoring CP-I levels in single and multiple clinical phase I dose escalation studies is recommended for early assessment of DDI risks and understanding the full dose-response of an investigational drug to OATP inhibitions."( The Role of Coproporphyrins As Endogenous Biomarkers for Organic Anion Transporting Polypeptide 1B Inhibition-Progress from 2016 to 2023.
Lai, Y, 2023
)
" We evaluated whether increased daily dosing with modified 8-hourly lopinavir/ritonavir 4:1 would maintain therapeutic plasma concentrations of lopinavir in children living with HIV receiving rifampicin-based antituberculosis treatment."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
"9 kg, on rifampicin-based antituberculosis treatment were commenced or switched to 8-hourly liquid lopinavir/ritonavir 4:1 with increased daily dosing using weight-band dosing approach."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
"7 mg/L]) were lower than on standard dosing without rifampicin (n = 12; area under the curve 24 121."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
"Modified 8-hourly dosing of lopinavir/ritonavir failed to achieve adequate lopinavir concentrations with concurrent antituberculosis treatment."( Inadequate Lopinavir Concentrations With Modified 8-Hourly Lopinavir/Ritonavir 4:1 Dosing During Rifampicin-based Tuberculosis Treatment in Children Living With HIV.
Chabala, C; Choo, L; Chungu, C; Crook, A; Gibb, D; Kapasa, M; LeBeau, K; Lungu, J; McIlleron, H; Mulenga, V; Tembo, CH; Turkova, A; Weisner, L; Zimba, K; Zyambo, K, 2023
)
" The simultaneous release of antibiotics and potentiators can be promoted and inhibited in response to the severity of bacterial-induced hypoxia, leading to antimicrobial dosing in a precision manner."( Precision Dosing of Antibiotics and Potentiators by Hypoxia-Responsive Nanoparticles for Overcoming Antibiotic Resistance in Gram-Negative Bacteria.
Bai, W; Ge, C; Hu, Y; Rao, J; Shi, L; Zhao, J; Zhu, Z, 2023
)
" Recent data showed higher exposures with 100 mg dispersible compared with non-dispersible tablet formulations with potentially important dosing implications in children."( Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children.
Denti, P; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Palmer, M; Schaaf, HS; van der Laan, LE; Wiesner, L, 2023
)
"Dosing simulations showed that current recommended dosing for both formulations result in median exposures below adult-equivalent exposures at a 750 mg daily dose, mainly in children >6 months."( Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children.
Denti, P; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Palmer, M; Schaaf, HS; van der Laan, LE; Wiesner, L, 2023
)
" We propose optimized age- and weight-based dosing for levofloxacin, which require further evaluation."( Pharmacokinetics and optimized dosing of dispersible and non-dispersible levofloxacin formulations in young children.
Denti, P; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; Palmer, M; Schaaf, HS; van der Laan, LE; Wiesner, L, 2023
)
" We provide suggested dolutegravir dosing considerations with concomitant rifapentine use, not currently addressed in recommended guidelines."( Alternative dolutegravir dosing strategies with concurrent rifapentine utilized for latent tuberculosis treatment.
Pecora Fulco, P; Taylor, A; Winthrop, E, 2023
)
" In addition, the possibility of compensation by dosage adjustments was evaluated."( Rifampicin reduces plasma concentration of linezolid in patients with infective endocarditis.
Bock, M; Bruun, NE; Bundgaard, H; Christensen, JJ; Christiansen, U; Elming, H; Fosbøl, EL; Fuursted, K; Gill, S; Helweg-Larsen, J; Høfsten, DE; Høiby, N; Ihlemann, N; Iversen, K; Køber, L; Moser, C; Povlsen, JA; Pries-Heje, MM; Rosenvinge, FS; Schwartz, F; Torp-Pedersen, C; Tønder, N; Van Hasselt, JGC; Wang, H, 2023
)
" Model-based dosing simulations showed that rifampicin cotreatment decreased the PTA of linezolid from 94."( Rifampicin reduces plasma concentration of linezolid in patients with infective endocarditis.
Bock, M; Bruun, NE; Bundgaard, H; Christensen, JJ; Christiansen, U; Elming, H; Fosbøl, EL; Fuursted, K; Gill, S; Helweg-Larsen, J; Høfsten, DE; Høiby, N; Ihlemann, N; Iversen, K; Køber, L; Moser, C; Povlsen, JA; Pries-Heje, MM; Rosenvinge, FS; Schwartz, F; Torp-Pedersen, C; Tønder, N; Van Hasselt, JGC; Wang, H, 2023
)
"The current World Health Organization (WHO) pediatric tuberculosis dosing guidelines lead to suboptimal drug exposures."( Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis.
Aarnoutse, R; Chabala, C; Cotton, MF; Denti, P; Galileya, LT; Gibb, D; Hesseling, A; Lee, J; McIlleron, H; Njahira Mukui, I; Rabie, H; Turkova, A; Wasmann, RE; Zar, H, 2023
)
" The importance of the drug-drug interactions with lopinavir/ritonavir and efavirenz should be evaluated further and considered in future dosing guidance."( Evaluating pediatric tuberculosis dosing guidelines: A model-based individual data pooled analysis.
Aarnoutse, R; Chabala, C; Cotton, MF; Denti, P; Galileya, LT; Gibb, D; Hesseling, A; Lee, J; McIlleron, H; Njahira Mukui, I; Rabie, H; Turkova, A; Wasmann, RE; Zar, H, 2023
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (12)

RoleDescription
EC 2.7.7.6 (RNA polymerase) inhibitorAn EC 2.7.7.* (nucleotidyltransferase) inhibitor that interferes with the action of RNA polymerase (EC 2.7.7.6).
DNA synthesis inhibitorAny substance that inhibits the synthesis of DNA.
antitubercular agentA substance that kills or slows the growth of Mycobacterium tuberculosis and is used in the treatment of tuberculosis.
leprostatic drugA substance that suppresses Mycobacterium leprae, ameliorates the clinical manifestations of leprosy, and/or reduces the incidence and severity of leprous reactions.
Escherichia coli metaboliteAny bacterial metabolite produced during a metabolic reaction in Escherichia coli.
protein synthesis inhibitorA compound, usually an anti-bacterial agent or a toxin, which inhibits the synthesis of a protein.
neuroprotective agentAny compound that can be used for the treatment of neurodegenerative disorders.
angiogenesis inhibitorAn agent and endogenous substances that antagonize or inhibit the development of new blood vessels.
pregnane X receptor agonistAn agonist that selectively binds to and activates a pregnane X receptor.
antineoplastic agentA substance that inhibits or prevents the proliferation of neoplasms.
antiamoebic agentAn antiparasitic agent which is effective against amoeba, a genus of single-celled amoeboids in the family Amoebidae.
geroprotectorAny compound that supports healthy aging, slows the biological aging process, or extends lifespan.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (7)

ClassDescription
rifamycins
N-iminopiperazine
N-methylpiperazine
hydrazoneCompounds having the structure R2C=NNR2, formally derived from aldehydes or ketones by replacing =O by =NNH2 (or substituted analogues).
cyclic ketalA ketal in the molecule of which the ketal carbon and one or both oxygen atoms thereon are members of a ring.
semisynthetic derivativeAny organic molecular entity derived from a natural product by partial chemical synthesis.
zwitterionA neutral compound having formal unit electrical charges of opposite sign on non-adjacent atoms. Sometimes referred to as inner salts, dipolar ions (a misnomer).
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Pathways (10)

PathwayProteinsCompounds
Metabolism of proteins1058144
Post-translational protein modification666112
SUMOylation1676
SUMO E3 ligases SUMOylate target proteins1643
SUMOylation of intracellular receptors303
Disease1278231
Infectious disease89579
Infection with Mycobacterium tuberculosis7442
Antimicrobial action and antimicrobial resistance in Mtb42
Bacterial Infection Pathways12347

Protein Targets (77)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
LuciferasePhotinus pyralis (common eastern firefly)Potency80.09570.007215.758889.3584AID1224835
acetylcholinesteraseHomo sapiens (human)Potency89.86890.002541.796015,848.9004AID1347398
RAR-related orphan receptor gammaMus musculus (house mouse)Potency44.90720.006038.004119,952.5996AID1159521; AID1159523
SMAD family member 2Homo sapiens (human)Potency55.26380.173734.304761.8120AID1346859
GALC proteinHomo sapiens (human)Potency0.631028.183828.183828.1838AID1159614
SMAD family member 3Homo sapiens (human)Potency55.26380.173734.304761.8120AID1346859
TDP1 proteinHomo sapiens (human)Potency21.27620.000811.382244.6684AID686978; AID686979
GLI family zinc finger 3Homo sapiens (human)Potency24.62260.000714.592883.7951AID1259369; AID1259392
AR proteinHomo sapiens (human)Potency36.79550.000221.22318,912.5098AID1259243; AID1259247; AID743035; AID743042; AID743054; AID743063
nuclear receptor subfamily 1, group I, member 3Homo sapiens (human)Potency33.61750.001022.650876.6163AID1224838; AID1224893
progesterone receptorHomo sapiens (human)Potency61.44150.000417.946075.1148AID1346795
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency7.25540.01237.983543.2770AID1346984; AID1645841
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency21.31380.000214.376460.0339AID720692
estrogen-related nuclear receptor alphaHomo sapiens (human)Potency31.23570.001530.607315,848.9004AID1224841; AID1224842; AID1224848; AID1224849; AID1259401; AID1259403
farnesoid X nuclear receptorHomo sapiens (human)Potency6.68190.375827.485161.6524AID743217
pregnane X nuclear receptorHomo sapiens (human)Potency15.34780.005428.02631,258.9301AID1346982; AID1346985
estrogen nuclear receptor alphaHomo sapiens (human)Potency31.16600.000229.305416,493.5996AID1259244; AID1259248; AID743069; AID743075; AID743079
GVesicular stomatitis virusPotency30.90080.01238.964839.8107AID1645842
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency41.04820.001019.414170.9645AID743140
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency25.15470.023723.228263.5986AID743222; AID743241
cytochrome P450, family 19, subfamily A, polypeptide 1, isoform CRA_aHomo sapiens (human)Potency44.12570.001723.839378.1014AID743083
thyroid stimulating hormone receptorHomo sapiens (human)Potency68.93850.001628.015177.1139AID1259385
activating transcription factor 6Homo sapiens (human)Potency0.02480.143427.612159.8106AID1159516
nuclear factor of kappa light polypeptide gene enhancer in B-cells 1 (p105), isoform CRA_aHomo sapiens (human)Potency0.197219.739145.978464.9432AID1159509
Histone H2A.xCricetulus griseus (Chinese hamster)Potency42.89570.039147.5451146.8240AID1224845; AID1224896
thyroid hormone receptor beta isoform 2Rattus norvegicus (Norway rat)Potency33.65470.000323.4451159.6830AID743065; AID743067
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency8.05800.000627.21521,122.0200AID743202; AID743219
Voltage-dependent calcium channel gamma-2 subunitMus musculus (house mouse)Potency38.76700.001557.789015,848.9004AID1259244
Interferon betaHomo sapiens (human)Potency30.90080.00339.158239.8107AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency30.90080.01238.964839.8107AID1645842
Cellular tumor antigen p53Homo sapiens (human)Potency15.43340.002319.595674.0614AID651631
Glutamate receptor 2Rattus norvegicus (Norway rat)Potency38.76700.001551.739315,848.9004AID1259244
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency30.90080.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency30.90080.01238.964839.8107AID1645842
Chain A, CruzipainTrypanosoma cruziPotency12.58930.002014.677939.8107AID1476
interleukin 8Homo sapiens (human)Potency66.82420.047349.480674.9780AID651758
15-lipoxygenase, partialHomo sapiens (human)Potency31.62280.012610.691788.5700AID887
Microtubule-associated protein tauHomo sapiens (human)Potency31.62280.180013.557439.8107AID1460
AR proteinHomo sapiens (human)Potency31.09890.000221.22318,912.5098AID588515; AID588516
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency39.81070.011212.4002100.0000AID1030
thyroid stimulating hormone receptorHomo sapiens (human)Potency25.11890.001318.074339.8107AID926; AID938
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency26.63210.000214.376460.0339AID588533
retinoid X nuclear receptor alphaHomo sapiens (human)Potency2.23870.000817.505159.3239AID588544
pregnane X nuclear receptorHomo sapiens (human)Potency11.70310.005428.02631,258.9301AID720659
estrogen nuclear receptor alphaHomo sapiens (human)Potency39.81070.000229.305416,493.5996AID588513
peroxisome proliferator-activated receptor deltaHomo sapiens (human)Potency44.66840.001024.504861.6448AID588534
peroxisome proliferator activated receptor gammaHomo sapiens (human)Potency50.11870.001019.414170.9645AID588536
vitamin D (1,25- dihydroxyvitamin D3) receptorHomo sapiens (human)Potency22.38720.023723.228263.5986AID588543
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency19.95260.035520.977089.1251AID504332
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency64.73030.000627.21521,122.0200AID651741
Polyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)Potency31.62280.316212.765731.6228AID881
Histamine H2 receptorCavia porcellus (domestic guinea pig)Potency31.62280.00638.235039.8107AID881
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
ATP-binding cassette sub-family C member 3Homo sapiens (human)IC50 (µMol)69.00000.63154.45319.3000AID1473740
Multidrug resistance-associated protein 4Homo sapiens (human)IC50 (µMol)41.90000.20005.677410.0000AID1473741
Solute carrier organic anion transporter family member 1A4Rattus norvegicus (Norway rat)Ki1.43000.03702.34107.3000AID680348; AID681846
Bile salt export pumpRattus norvegicus (Norway rat)IC50 (µMol)34.70000.40002.75008.6000AID1209456
Bile salt export pumpRattus norvegicus (Norway rat)Ki11.90000.30003.10006.1000AID679145
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)IC50 (µMol)65.00000.55003.70836.1000AID699544
Solute carrier organic anion transporter family member 2B1 Homo sapiens (human)Ki63.00000.53004.11578.4800AID699544
Bile salt export pumpHomo sapiens (human)IC50 (µMol)20.15000.11007.190310.0000AID1209455; AID1443980; AID1443986; AID1473738
60 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50 (µMol)100.00000.17004.559010.0000AID1423480
Polyunsaturated fatty acid lipoxygenase ALOX15Oryctolagus cuniculus (rabbit)IC50 (µMol)2.94900.11003.26419.0330AID625146
Caspase-1Homo sapiens (human)IC50 (µMol)8.31900.00201.70138.8000AID625174
Alpha-synucleinHomo sapiens (human)IC50 (µMol)26.65000.19003.82049.8000AID1695729; AID1695730
Solute carrier organic anion transporter family member 1A1Rattus norvegicus (Norway rat)Ki18.20001.10004.51259.8000AID680469
10 kDa heat shock protein, mitochondrialHomo sapiens (human)IC50 (µMol)100.00000.17004.559010.0000AID1423480
Glutathione S-transferase omega-1Homo sapiens (human)IC50 (µMol)75.00000.02801.60404.6000AID1384565
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC50 (µMol)50.00000.01502.467610.0000AID1272956
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50 (µMol)50.00000.01503.477310.0000AID1272956
Enoyl-[acyl-carrier-protein] reductase [NADH]Mycobacterium tuberculosis H37RvIC50 (µMol)0.03000.03002.286410.0000AID1181177
DNA-directed RNA polymerase subunit betaMycobacterium tuberculosis H37RvIC50 (µMol)0.01000.01000.01000.0100AID626869
Thiosulfate sulfurtransferaseHomo sapiens (human)IC50 (µMol)100.00000.06003.96319.7000AID1423472
Lanosterol 14-alpha demethylaseHomo sapiens (human)IC50 (µMol)30.00000.05001.43904.0000AID322753
60 kDa chaperonin Escherichia coliIC50 (µMol)100.00000.03903.55529.8000AID1423469; AID1423470
10 kDa chaperonin Escherichia coliIC50 (µMol)100.00000.03903.55529.8000AID1423469; AID1423470
Canalicular multispecific organic anion transporter 1Homo sapiens (human)IC50 (µMol)53.00002.41006.343310.0000AID1473739
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)IC50 (µMol)1.50000.10472.71957.0795AID699543
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Ki3.20000.08002.46889.8000AID679646; AID699543
Broad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)IC50 (µMol)56.00000.00401.966610.0000AID1873198
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)IC50 (µMol)1.50000.05002.37979.7000AID1218863; AID1218864; AID1218865; AID699542
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Ki9.05000.04401.36305.0000AID679507; AID699542
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Activation Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Nuclear receptor subfamily 1 group I member 2Homo sapiens (human)EC50 (µMol)2.16560.00203.519610.0000AID1215086; AID1215087; AID1215094; AID1287454; AID1310890; AID1398739; AID1775048; AID626877; AID669188
AlbuminHomo sapiens (human)Kd12.00000.08933.31358.0000AID557095
Cytochrome P450 2B6Homo sapiens (human)EC50 (µMol)1.30001.30001.30001.3000AID1210066
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Arylacetamide deacetylaseHomo sapiens (human)Km200.00000.00182.35094.7000AID1210916
Solute carrier organic anion transporter family member 1B3Homo sapiens (human)Km2.30000.03912.93886.4000AID680208
Solute carrier organic anion transporter family member 1B1Homo sapiens (human)Km7.25000.00763.201810.0000AID680552; AID680558
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (390)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycle G2/M phase transitionCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
ER overload responseCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
mitophagyCellular tumor antigen p53Homo sapiens (human)
in utero embryonic developmentCellular tumor antigen p53Homo sapiens (human)
somitogenesisCellular tumor antigen p53Homo sapiens (human)
release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
hematopoietic progenitor cell differentiationCellular tumor antigen p53Homo sapiens (human)
T cell proliferation involved in immune responseCellular tumor antigen p53Homo sapiens (human)
B cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
T cell lineage commitmentCellular tumor antigen p53Homo sapiens (human)
response to ischemiaCellular tumor antigen p53Homo sapiens (human)
nucleotide-excision repairCellular tumor antigen p53Homo sapiens (human)
double-strand break repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
protein import into nucleusCellular tumor antigen p53Homo sapiens (human)
autophagyCellular tumor antigen p53Homo sapiens (human)
DNA damage responseCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in cell cycle arrestCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediator resulting in transcription of p21 class mediatorCellular tumor antigen p53Homo sapiens (human)
transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
Ras protein signal transductionCellular tumor antigen p53Homo sapiens (human)
gastrulationCellular tumor antigen p53Homo sapiens (human)
neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of neuroblast proliferationCellular tumor antigen p53Homo sapiens (human)
protein localizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA replicationCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell population proliferationCellular tumor antigen p53Homo sapiens (human)
determination of adult lifespanCellular tumor antigen p53Homo sapiens (human)
mRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
rRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
response to salt stressCellular tumor antigen p53Homo sapiens (human)
response to inorganic substanceCellular tumor antigen p53Homo sapiens (human)
response to X-rayCellular tumor antigen p53Homo sapiens (human)
response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
positive regulation of gene expressionCellular tumor antigen p53Homo sapiens (human)
cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of cardiac muscle cell apoptotic processCellular tumor antigen p53Homo sapiens (human)
glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
viral processCellular tumor antigen p53Homo sapiens (human)
glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
cerebellum developmentCellular tumor antigen p53Homo sapiens (human)
negative regulation of cell growthCellular tumor antigen p53Homo sapiens (human)
DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
negative regulation of transforming growth factor beta receptor signaling pathwayCellular tumor antigen p53Homo sapiens (human)
mitotic G1 DNA damage checkpoint signalingCellular tumor antigen p53Homo sapiens (human)
negative regulation of telomere maintenance via telomeraseCellular tumor antigen p53Homo sapiens (human)
T cell differentiation in thymusCellular tumor antigen p53Homo sapiens (human)
tumor necrosis factor-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
regulation of tissue remodelingCellular tumor antigen p53Homo sapiens (human)
cellular response to UVCellular tumor antigen p53Homo sapiens (human)
multicellular organism growthCellular tumor antigen p53Homo sapiens (human)
positive regulation of mitochondrial membrane permeabilityCellular tumor antigen p53Homo sapiens (human)
cellular response to glucose starvationCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to DNA damage by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of apoptotic processCellular tumor antigen p53Homo sapiens (human)
entrainment of circadian clock by photoperiodCellular tumor antigen p53Homo sapiens (human)
mitochondrial DNA repairCellular tumor antigen p53Homo sapiens (human)
regulation of DNA damage response, signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
transcription initiation-coupled chromatin remodelingCellular tumor antigen p53Homo sapiens (human)
negative regulation of proteolysisCellular tumor antigen p53Homo sapiens (human)
negative regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of DNA-templated transcriptionCellular tumor antigen p53Homo sapiens (human)
positive regulation of RNA polymerase II transcription preinitiation complex assemblyCellular tumor antigen p53Homo sapiens (human)
positive regulation of transcription by RNA polymerase IICellular tumor antigen p53Homo sapiens (human)
response to antibioticCellular tumor antigen p53Homo sapiens (human)
fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
negative regulation of fibroblast proliferationCellular tumor antigen p53Homo sapiens (human)
circadian behaviorCellular tumor antigen p53Homo sapiens (human)
bone marrow developmentCellular tumor antigen p53Homo sapiens (human)
embryonic organ developmentCellular tumor antigen p53Homo sapiens (human)
positive regulation of peptidyl-tyrosine phosphorylationCellular tumor antigen p53Homo sapiens (human)
protein stabilizationCellular tumor antigen p53Homo sapiens (human)
negative regulation of helicase activityCellular tumor antigen p53Homo sapiens (human)
protein tetramerizationCellular tumor antigen p53Homo sapiens (human)
chromosome organizationCellular tumor antigen p53Homo sapiens (human)
neuron apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of cell cycleCellular tumor antigen p53Homo sapiens (human)
hematopoietic stem cell differentiationCellular tumor antigen p53Homo sapiens (human)
negative regulation of glial cell proliferationCellular tumor antigen p53Homo sapiens (human)
type II interferon-mediated signaling pathwayCellular tumor antigen p53Homo sapiens (human)
cardiac septum morphogenesisCellular tumor antigen p53Homo sapiens (human)
positive regulation of programmed necrotic cell deathCellular tumor antigen p53Homo sapiens (human)
protein-containing complex assemblyCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to endoplasmic reticulum stressCellular tumor antigen p53Homo sapiens (human)
thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of thymocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
necroptotic processCellular tumor antigen p53Homo sapiens (human)
cellular response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
cellular response to xenobiotic stimulusCellular tumor antigen p53Homo sapiens (human)
cellular response to ionizing radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to gamma radiationCellular tumor antigen p53Homo sapiens (human)
cellular response to UV-CCellular tumor antigen p53Homo sapiens (human)
stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
signal transduction by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
cellular response to actinomycin DCellular tumor antigen p53Homo sapiens (human)
positive regulation of release of cytochrome c from mitochondriaCellular tumor antigen p53Homo sapiens (human)
cellular senescenceCellular tumor antigen p53Homo sapiens (human)
replicative senescenceCellular tumor antigen p53Homo sapiens (human)
oxidative stress-induced premature senescenceCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
oligodendrocyte apoptotic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of execution phase of apoptosisCellular tumor antigen p53Homo sapiens (human)
negative regulation of mitophagyCellular tumor antigen p53Homo sapiens (human)
regulation of mitochondrial membrane permeability involved in apoptotic processCellular tumor antigen p53Homo sapiens (human)
regulation of intrinsic apoptotic signaling pathway by p53 class mediatorCellular tumor antigen p53Homo sapiens (human)
positive regulation of miRNA transcriptionCellular tumor antigen p53Homo sapiens (human)
negative regulation of G1 to G0 transitionCellular tumor antigen p53Homo sapiens (human)
negative regulation of miRNA processingCellular tumor antigen p53Homo sapiens (human)
negative regulation of glucose catabolic process to lactate via pyruvateCellular tumor antigen p53Homo sapiens (human)
negative regulation of pentose-phosphate shuntCellular tumor antigen p53Homo sapiens (human)
intrinsic apoptotic signaling pathway in response to hypoxiaCellular tumor antigen p53Homo sapiens (human)
regulation of fibroblast apoptotic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
positive regulation of reactive oxygen species metabolic processCellular tumor antigen p53Homo sapiens (human)
negative regulation of stem cell proliferationCellular tumor antigen p53Homo sapiens (human)
positive regulation of cellular senescenceCellular tumor antigen p53Homo sapiens (human)
positive regulation of intrinsic apoptotic signaling pathwayCellular tumor antigen p53Homo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
lipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
phospholipid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
apoptotic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell population proliferationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of macrophage derived foam cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell migrationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
prostate gland developmentPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
regulation of epithelial cell differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of chemokine productionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of peroxisome proliferator activated receptor signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
positive regulation of keratinocyte differentiationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of cell cyclePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
negative regulation of growthPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
hepoxilin biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
endocannabinoid signaling pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cannabinoid biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxin A4 biosynthetic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleic acid metabolic processPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid oxidationPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipoxygenase pathwayPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
xenobiotic metabolic processATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
bile acid and bile salt transportATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transportATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
leukotriene transportATP-binding cassette sub-family C member 3Homo sapiens (human)
monoatomic anion transmembrane transportATP-binding cassette sub-family C member 3Homo sapiens (human)
transport across blood-brain barrierATP-binding cassette sub-family C member 3Homo sapiens (human)
prostaglandin secretionMultidrug resistance-associated protein 4Homo sapiens (human)
cilium assemblyMultidrug resistance-associated protein 4Homo sapiens (human)
platelet degranulationMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic metabolic processMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
bile acid and bile salt transportMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transportMultidrug resistance-associated protein 4Homo sapiens (human)
urate transportMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
cAMP transportMultidrug resistance-associated protein 4Homo sapiens (human)
leukotriene transportMultidrug resistance-associated protein 4Homo sapiens (human)
monoatomic anion transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
export across plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
transport across blood-brain barrierMultidrug resistance-associated protein 4Homo sapiens (human)
guanine nucleotide transmembrane transportMultidrug resistance-associated protein 4Homo sapiens (human)
negative regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
signal transductionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
steroid metabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of gene expressionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intracellular receptor signaling pathwayNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic catabolic processNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic transportNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
positive regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
cell differentiationNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
negative regulation of transcription by RNA polymerase IINuclear receptor subfamily 1 group I member 2Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transport across blood-brain barrierSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
cellular response to starvationAlbuminHomo sapiens (human)
negative regulation of mitochondrial depolarizationAlbuminHomo sapiens (human)
cellular response to calcium ion starvationAlbuminHomo sapiens (human)
cellular oxidant detoxificationAlbuminHomo sapiens (human)
transportAlbuminHomo sapiens (human)
adhesion of symbiont to host60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of type II interferon production60 kDa heat shock protein, mitochondrialHomo sapiens (human)
T cell activation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
MyD88-dependent toll-like receptor signaling pathway60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of T cell mediated immune response to tumor cell60 kDa heat shock protein, mitochondrialHomo sapiens (human)
'de novo' protein folding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process60 kDa heat shock protein, mitochondrialHomo sapiens (human)
response to unfolded protein60 kDa heat shock protein, mitochondrialHomo sapiens (human)
response to cold60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of interferon-alpha production60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of type II interferon production60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of interleukin-10 production60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of interleukin-12 production60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of interleukin-6 production60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein refolding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
B cell proliferation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
B cell activation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of macrophage activation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of apoptotic process60 kDa heat shock protein, mitochondrialHomo sapiens (human)
negative regulation of apoptotic process60 kDa heat shock protein, mitochondrialHomo sapiens (human)
isotype switching to IgG isotypes60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein stabilization60 kDa heat shock protein, mitochondrialHomo sapiens (human)
positive regulation of T cell activation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
chaperone-mediated protein complex assembly60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein maturation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
biological process involved in interaction with symbiont60 kDa heat shock protein, mitochondrialHomo sapiens (human)
cellular response to interleukin-760 kDa heat shock protein, mitochondrialHomo sapiens (human)
T cell activation60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein import into mitochondrial intermembrane space60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein folding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
mitochondrial unfolded protein response60 kDa heat shock protein, mitochondrialHomo sapiens (human)
apoptotic mitochondrial changes60 kDa heat shock protein, mitochondrialHomo sapiens (human)
xenobiotic metabolic processCytochrome P450 2B6Homo sapiens (human)
steroid metabolic processCytochrome P450 2B6Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 2B6Homo sapiens (human)
cellular ketone metabolic processCytochrome P450 2B6Homo sapiens (human)
epoxygenase P450 pathwayCytochrome P450 2B6Homo sapiens (human)
lipid metabolic processArylacetamide deacetylaseHomo sapiens (human)
xenobiotic metabolic processArylacetamide deacetylaseHomo sapiens (human)
positive regulation of triglyceride catabolic processArylacetamide deacetylaseHomo sapiens (human)
cellular response to organic substanceCaspase-1Homo sapiens (human)
pattern recognition receptor signaling pathwayCaspase-1Homo sapiens (human)
proteolysisCaspase-1Homo sapiens (human)
apoptotic processCaspase-1Homo sapiens (human)
signal transductionCaspase-1Homo sapiens (human)
osmosensory signaling pathwayCaspase-1Homo sapiens (human)
protein autoprocessingCaspase-1Homo sapiens (human)
positive regulation of interleukin-1 beta productionCaspase-1Homo sapiens (human)
positive regulation of interleukin-18 productionCaspase-1Homo sapiens (human)
defense response to bacteriumCaspase-1Homo sapiens (human)
regulation of apoptotic processCaspase-1Homo sapiens (human)
positive regulation of canonical NF-kappaB signal transductionCaspase-1Homo sapiens (human)
positive regulation of cysteine-type endopeptidase activity involved in apoptotic processCaspase-1Homo sapiens (human)
icosanoid biosynthetic processCaspase-1Homo sapiens (human)
regulation of inflammatory responseCaspase-1Homo sapiens (human)
positive regulation of inflammatory responseCaspase-1Homo sapiens (human)
protein maturationCaspase-1Homo sapiens (human)
defense response to virusCaspase-1Homo sapiens (human)
pyroptosisCaspase-1Homo sapiens (human)
cellular response to lipopolysaccharideCaspase-1Homo sapiens (human)
cellular response to mechanical stimulusCaspase-1Homo sapiens (human)
cellular response to type II interferonCaspase-1Homo sapiens (human)
cytokine precursor processingCaspase-1Homo sapiens (human)
signaling receptor ligand precursor processingCaspase-1Homo sapiens (human)
AIM2 inflammasome complex assemblyCaspase-1Homo sapiens (human)
positive regulation of tumor necrosis factor-mediated signaling pathwayCaspase-1Homo sapiens (human)
calcium ion homeostasisAlpha-synucleinHomo sapiens (human)
negative regulation of transcription by RNA polymerase IIAlpha-synucleinHomo sapiens (human)
microglial cell activationAlpha-synucleinHomo sapiens (human)
positive regulation of receptor recyclingAlpha-synucleinHomo sapiens (human)
positive regulation of neurotransmitter secretionAlpha-synucleinHomo sapiens (human)
negative regulation of protein kinase activityAlpha-synucleinHomo sapiens (human)
fatty acid metabolic processAlpha-synucleinHomo sapiens (human)
neutral lipid metabolic processAlpha-synucleinHomo sapiens (human)
phospholipid metabolic processAlpha-synucleinHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
mitochondrial membrane organizationAlpha-synucleinHomo sapiens (human)
adult locomotory behaviorAlpha-synucleinHomo sapiens (human)
response to xenobiotic stimulusAlpha-synucleinHomo sapiens (human)
response to iron(II) ionAlpha-synucleinHomo sapiens (human)
regulation of phospholipase activityAlpha-synucleinHomo sapiens (human)
negative regulation of platelet-derived growth factor receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
regulation of glutamate secretionAlpha-synucleinHomo sapiens (human)
regulation of dopamine secretionAlpha-synucleinHomo sapiens (human)
synaptic vesicle exocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle primingAlpha-synucleinHomo sapiens (human)
regulation of transmembrane transporter activityAlpha-synucleinHomo sapiens (human)
negative regulation of microtubule polymerizationAlpha-synucleinHomo sapiens (human)
receptor internalizationAlpha-synucleinHomo sapiens (human)
protein destabilizationAlpha-synucleinHomo sapiens (human)
response to magnesium ionAlpha-synucleinHomo sapiens (human)
negative regulation of transporter activityAlpha-synucleinHomo sapiens (human)
response to lipopolysaccharideAlpha-synucleinHomo sapiens (human)
negative regulation of monooxygenase activityAlpha-synucleinHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylationAlpha-synucleinHomo sapiens (human)
response to type II interferonAlpha-synucleinHomo sapiens (human)
cellular response to oxidative stressAlpha-synucleinHomo sapiens (human)
SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
positive regulation of SNARE complex assemblyAlpha-synucleinHomo sapiens (human)
regulation of locomotionAlpha-synucleinHomo sapiens (human)
dopamine biosynthetic processAlpha-synucleinHomo sapiens (human)
mitochondrial ATP synthesis coupled electron transportAlpha-synucleinHomo sapiens (human)
regulation of macrophage activationAlpha-synucleinHomo sapiens (human)
positive regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of cysteine-type endopeptidase activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
negative regulation of neuron apoptotic processAlpha-synucleinHomo sapiens (human)
positive regulation of endocytosisAlpha-synucleinHomo sapiens (human)
negative regulation of exocytosisAlpha-synucleinHomo sapiens (human)
positive regulation of exocytosisAlpha-synucleinHomo sapiens (human)
regulation of long-term neuronal synaptic plasticityAlpha-synucleinHomo sapiens (human)
synaptic vesicle endocytosisAlpha-synucleinHomo sapiens (human)
synaptic vesicle transportAlpha-synucleinHomo sapiens (human)
positive regulation of inflammatory responseAlpha-synucleinHomo sapiens (human)
regulation of acyl-CoA biosynthetic processAlpha-synucleinHomo sapiens (human)
protein tetramerizationAlpha-synucleinHomo sapiens (human)
positive regulation of release of sequestered calcium ion into cytosolAlpha-synucleinHomo sapiens (human)
neuron apoptotic processAlpha-synucleinHomo sapiens (human)
dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of dopamine uptake involved in synaptic transmissionAlpha-synucleinHomo sapiens (human)
negative regulation of serotonin uptakeAlpha-synucleinHomo sapiens (human)
regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
negative regulation of norepinephrine uptakeAlpha-synucleinHomo sapiens (human)
excitatory postsynaptic potentialAlpha-synucleinHomo sapiens (human)
long-term synaptic potentiationAlpha-synucleinHomo sapiens (human)
positive regulation of inositol phosphate biosynthetic processAlpha-synucleinHomo sapiens (human)
negative regulation of thrombin-activated receptor signaling pathwayAlpha-synucleinHomo sapiens (human)
response to interleukin-1Alpha-synucleinHomo sapiens (human)
cellular response to copper ionAlpha-synucleinHomo sapiens (human)
cellular response to epinephrine stimulusAlpha-synucleinHomo sapiens (human)
positive regulation of protein serine/threonine kinase activityAlpha-synucleinHomo sapiens (human)
supramolecular fiber organizationAlpha-synucleinHomo sapiens (human)
negative regulation of mitochondrial electron transport, NADH to ubiquinoneAlpha-synucleinHomo sapiens (human)
positive regulation of glutathione peroxidase activityAlpha-synucleinHomo sapiens (human)
positive regulation of hydrogen peroxide catabolic processAlpha-synucleinHomo sapiens (human)
regulation of synaptic vesicle recyclingAlpha-synucleinHomo sapiens (human)
regulation of reactive oxygen species biosynthetic processAlpha-synucleinHomo sapiens (human)
positive regulation of protein localization to cell peripheryAlpha-synucleinHomo sapiens (human)
negative regulation of chaperone-mediated autophagyAlpha-synucleinHomo sapiens (human)
regulation of presynapse assemblyAlpha-synucleinHomo sapiens (human)
amyloid fibril formationAlpha-synucleinHomo sapiens (human)
synapse organizationAlpha-synucleinHomo sapiens (human)
chemical synaptic transmissionAlpha-synucleinHomo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
organic cation transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
osteoblast differentiation10 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein folding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
activation of cysteine-type endopeptidase activity involved in apoptotic process10 kDa heat shock protein, mitochondrialHomo sapiens (human)
response to unfolded protein10 kDa heat shock protein, mitochondrialHomo sapiens (human)
chaperone cofactor-dependent protein refolding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
regulation of release of sequestered calcium ion into cytosol by sarcoplasmic reticulumGlutathione S-transferase omega-1Homo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionGlutathione S-transferase omega-1Homo sapiens (human)
positive regulation of skeletal muscle contraction by regulation of release of sequestered calcium ionGlutathione S-transferase omega-1Homo sapiens (human)
L-ascorbic acid metabolic processGlutathione S-transferase omega-1Homo sapiens (human)
xenobiotic catabolic processGlutathione S-transferase omega-1Homo sapiens (human)
negative regulation of ryanodine-sensitive calcium-release channel activityGlutathione S-transferase omega-1Homo sapiens (human)
positive regulation of ryanodine-sensitive calcium-release channel activityGlutathione S-transferase omega-1Homo sapiens (human)
cellular response to arsenic-containing substanceGlutathione S-transferase omega-1Homo sapiens (human)
cellular oxidant detoxificationGlutathione S-transferase omega-1Homo sapiens (human)
glutathione metabolic processGlutathione S-transferase omega-1Homo sapiens (human)
sulfur amino acid catabolic processThiosulfate sulfurtransferaseHomo sapiens (human)
cyanate catabolic processThiosulfate sulfurtransferaseHomo sapiens (human)
epithelial cell differentiationThiosulfate sulfurtransferaseHomo sapiens (human)
rRNA import into mitochondrionThiosulfate sulfurtransferaseHomo sapiens (human)
rRNA transportThiosulfate sulfurtransferaseHomo sapiens (human)
steroid biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
cholesterol biosynthetic processLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol metabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein catabolic processLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of protein secretionLanosterol 14-alpha demethylaseHomo sapiens (human)
negative regulation of amyloid-beta clearanceLanosterol 14-alpha demethylaseHomo sapiens (human)
xenobiotic metabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
negative regulation of gene expressionCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bile acid and bile salt transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
heme catabolic processCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic export from cellCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transepithelial transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
leukotriene transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
monoatomic anion transmembrane transportCanalicular multispecific organic anion transporter 1Homo sapiens (human)
transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transport across blood-brain barrierCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
lipid transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid biosynthetic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate metabolic processBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transmembrane transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transepithelial transportBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
renal urate salt excretionBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
export across plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
cellular detoxificationBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transport across blood-brain barrierBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic metabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
monoatomic ion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid and bile salt transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
heme catabolic processSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
transmembrane transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transportSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (159)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
transcription cis-regulatory region bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
cis-regulatory region sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
core promoter sequence-specific DNA bindingCellular tumor antigen p53Homo sapiens (human)
TFIID-class transcription factor complex bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription repressor activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificCellular tumor antigen p53Homo sapiens (human)
protease bindingCellular tumor antigen p53Homo sapiens (human)
p53 bindingCellular tumor antigen p53Homo sapiens (human)
DNA bindingCellular tumor antigen p53Homo sapiens (human)
chromatin bindingCellular tumor antigen p53Homo sapiens (human)
DNA-binding transcription factor activityCellular tumor antigen p53Homo sapiens (human)
mRNA 3'-UTR bindingCellular tumor antigen p53Homo sapiens (human)
copper ion bindingCellular tumor antigen p53Homo sapiens (human)
protein bindingCellular tumor antigen p53Homo sapiens (human)
zinc ion bindingCellular tumor antigen p53Homo sapiens (human)
enzyme bindingCellular tumor antigen p53Homo sapiens (human)
receptor tyrosine kinase bindingCellular tumor antigen p53Homo sapiens (human)
ubiquitin protein ligase bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase regulator activityCellular tumor antigen p53Homo sapiens (human)
ATP-dependent DNA/DNA annealing activityCellular tumor antigen p53Homo sapiens (human)
identical protein bindingCellular tumor antigen p53Homo sapiens (human)
histone deacetylase bindingCellular tumor antigen p53Homo sapiens (human)
protein heterodimerization activityCellular tumor antigen p53Homo sapiens (human)
protein-folding chaperone bindingCellular tumor antigen p53Homo sapiens (human)
protein phosphatase 2A bindingCellular tumor antigen p53Homo sapiens (human)
RNA polymerase II-specific DNA-binding transcription factor bindingCellular tumor antigen p53Homo sapiens (human)
14-3-3 protein bindingCellular tumor antigen p53Homo sapiens (human)
MDM2/MDM4 family protein bindingCellular tumor antigen p53Homo sapiens (human)
disordered domain specific bindingCellular tumor antigen p53Homo sapiens (human)
general transcription initiation factor bindingCellular tumor antigen p53Homo sapiens (human)
molecular function activator activityCellular tumor antigen p53Homo sapiens (human)
promoter-specific chromatin bindingCellular tumor antigen p53Homo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
iron ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
calcium ion bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
protein bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
lipid bindingPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 13S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 8(S)-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
arachidonate 15-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
linoleate 9S-lipoxygenase activityPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
ATP bindingATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type xenobiotic transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
glucuronoside transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type bile acid transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATP hydrolysis activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
xenobiotic transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
icosanoid transmembrane transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
ABC-type transporter activityATP-binding cassette sub-family C member 3Homo sapiens (human)
guanine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
protein bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ATP bindingMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type xenobiotic transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
prostaglandin transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
urate transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
purine nucleotide transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type bile acid transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
efflux transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
15-hydroxyprostaglandin dehydrogenase (NAD+) activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATP hydrolysis activityMultidrug resistance-associated protein 4Homo sapiens (human)
glutathione transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
xenobiotic transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
ABC-type transporter activityMultidrug resistance-associated protein 4Homo sapiens (human)
RNA polymerase II transcription regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription factor activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
DNA-binding transcription activator activity, RNA polymerase II-specificNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor activityNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
protein bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
zinc ion bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear receptor bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
sequence-specific double-stranded DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
RNA polymerase II cis-regulatory region sequence-specific DNA bindingNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
oxygen bindingAlbuminHomo sapiens (human)
DNA bindingAlbuminHomo sapiens (human)
fatty acid bindingAlbuminHomo sapiens (human)
copper ion bindingAlbuminHomo sapiens (human)
protein bindingAlbuminHomo sapiens (human)
toxic substance bindingAlbuminHomo sapiens (human)
antioxidant activityAlbuminHomo sapiens (human)
pyridoxal phosphate bindingAlbuminHomo sapiens (human)
identical protein bindingAlbuminHomo sapiens (human)
protein-folding chaperone bindingAlbuminHomo sapiens (human)
exogenous protein bindingAlbuminHomo sapiens (human)
enterobactin bindingAlbuminHomo sapiens (human)
lipopolysaccharide binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
p53 binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
DNA replication origin binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
single-stranded DNA binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
RNA binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
double-stranded RNA binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
ATP binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
high-density lipoprotein particle binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
isomerase activity60 kDa heat shock protein, mitochondrialHomo sapiens (human)
ATP hydrolysis activity60 kDa heat shock protein, mitochondrialHomo sapiens (human)
enzyme binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
ubiquitin protein ligase binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
apolipoprotein binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
apolipoprotein A-I binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
unfolded protein binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein-folding chaperone binding60 kDa heat shock protein, mitochondrialHomo sapiens (human)
ATP-dependent protein folding chaperone60 kDa heat shock protein, mitochondrialHomo sapiens (human)
monooxygenase activityCytochrome P450 2B6Homo sapiens (human)
iron ion bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-alpha-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
heme bindingCytochrome P450 2B6Homo sapiens (human)
testosterone 16-beta-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 2B6Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 2B6Homo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenCytochrome P450 2B6Homo sapiens (human)
arachidonic acid epoxygenase activityCytochrome P450 2B6Homo sapiens (human)
catalytic activityArylacetamide deacetylaseHomo sapiens (human)
triglyceride lipase activityArylacetamide deacetylaseHomo sapiens (human)
protein bindingArylacetamide deacetylaseHomo sapiens (human)
lipase activityArylacetamide deacetylaseHomo sapiens (human)
serine hydrolase activityArylacetamide deacetylaseHomo sapiens (human)
deacetylase activityArylacetamide deacetylaseHomo sapiens (human)
endopeptidase activityCaspase-1Homo sapiens (human)
cysteine-type endopeptidase activityCaspase-1Homo sapiens (human)
protein bindingCaspase-1Homo sapiens (human)
cysteine-type endopeptidase activator activity involved in apoptotic processCaspase-1Homo sapiens (human)
kinase bindingCaspase-1Homo sapiens (human)
cytokine bindingCaspase-1Homo sapiens (human)
identical protein bindingCaspase-1Homo sapiens (human)
CARD domain bindingCaspase-1Homo sapiens (human)
caspase bindingCaspase-1Homo sapiens (human)
fatty acid bindingAlpha-synucleinHomo sapiens (human)
phospholipase D inhibitor activityAlpha-synucleinHomo sapiens (human)
SNARE bindingAlpha-synucleinHomo sapiens (human)
magnesium ion bindingAlpha-synucleinHomo sapiens (human)
transcription cis-regulatory region bindingAlpha-synucleinHomo sapiens (human)
actin bindingAlpha-synucleinHomo sapiens (human)
protein kinase inhibitor activityAlpha-synucleinHomo sapiens (human)
copper ion bindingAlpha-synucleinHomo sapiens (human)
calcium ion bindingAlpha-synucleinHomo sapiens (human)
protein bindingAlpha-synucleinHomo sapiens (human)
phospholipid bindingAlpha-synucleinHomo sapiens (human)
ferrous iron bindingAlpha-synucleinHomo sapiens (human)
zinc ion bindingAlpha-synucleinHomo sapiens (human)
lipid bindingAlpha-synucleinHomo sapiens (human)
oxidoreductase activityAlpha-synucleinHomo sapiens (human)
kinesin bindingAlpha-synucleinHomo sapiens (human)
Hsp70 protein bindingAlpha-synucleinHomo sapiens (human)
histone bindingAlpha-synucleinHomo sapiens (human)
identical protein bindingAlpha-synucleinHomo sapiens (human)
alpha-tubulin bindingAlpha-synucleinHomo sapiens (human)
cysteine-type endopeptidase inhibitor activity involved in apoptotic processAlpha-synucleinHomo sapiens (human)
tau protein bindingAlpha-synucleinHomo sapiens (human)
phosphoprotein bindingAlpha-synucleinHomo sapiens (human)
molecular adaptor activityAlpha-synucleinHomo sapiens (human)
dynein complex bindingAlpha-synucleinHomo sapiens (human)
cuprous ion bindingAlpha-synucleinHomo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
organic cation transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1A2Homo sapiens (human)
RNA binding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein binding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
ATP binding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein folding chaperone10 kDa heat shock protein, mitochondrialHomo sapiens (human)
unfolded protein binding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein-folding chaperone binding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
metal ion binding10 kDa heat shock protein, mitochondrialHomo sapiens (human)
glutathione transferase activityGlutathione S-transferase omega-1Homo sapiens (human)
protein bindingGlutathione S-transferase omega-1Homo sapiens (human)
oxidoreductase activityGlutathione S-transferase omega-1Homo sapiens (human)
glutathione dehydrogenase (ascorbate) activityGlutathione S-transferase omega-1Homo sapiens (human)
methylarsonate reductase activityGlutathione S-transferase omega-1Homo sapiens (human)
thiosulfate sulfurtransferase activityThiosulfate sulfurtransferaseHomo sapiens (human)
5S rRNA bindingThiosulfate sulfurtransferaseHomo sapiens (human)
3-mercaptopyruvate sulfurtransferase activityThiosulfate sulfurtransferaseHomo sapiens (human)
iron ion bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
sterol 14-demethylase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
heme bindingLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activityLanosterol 14-alpha demethylaseHomo sapiens (human)
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygenLanosterol 14-alpha demethylaseHomo sapiens (human)
protein bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP bindingCanalicular multispecific organic anion transporter 1Homo sapiens (human)
organic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type xenobiotic transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
bilirubin transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type glutathione S-conjugate transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATP hydrolysis activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
xenobiotic transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ATPase-coupled inorganic anion transmembrane transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
ABC-type transporter activityCanalicular multispecific organic anion transporter 1Homo sapiens (human)
serine-type endopeptidase inhibitor activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B3Homo sapiens (human)
protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ABC-type xenobiotic transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
urate transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
biotin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
efflux transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATP hydrolysis activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
riboflavin transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
ATPase-coupled transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
identical protein bindingBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
protein homodimerization activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
xenobiotic transmembrane transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
sphingolipid transporter activityBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
bile acid transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
prostaglandin transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
sodium-independent organic anion transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
thyroid hormone transmembrane transporter activitySolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (86)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nuclear bodyCellular tumor antigen p53Homo sapiens (human)
nucleusCellular tumor antigen p53Homo sapiens (human)
nucleoplasmCellular tumor antigen p53Homo sapiens (human)
replication forkCellular tumor antigen p53Homo sapiens (human)
nucleolusCellular tumor antigen p53Homo sapiens (human)
cytoplasmCellular tumor antigen p53Homo sapiens (human)
mitochondrionCellular tumor antigen p53Homo sapiens (human)
mitochondrial matrixCellular tumor antigen p53Homo sapiens (human)
endoplasmic reticulumCellular tumor antigen p53Homo sapiens (human)
centrosomeCellular tumor antigen p53Homo sapiens (human)
cytosolCellular tumor antigen p53Homo sapiens (human)
nuclear matrixCellular tumor antigen p53Homo sapiens (human)
PML bodyCellular tumor antigen p53Homo sapiens (human)
transcription repressor complexCellular tumor antigen p53Homo sapiens (human)
site of double-strand breakCellular tumor antigen p53Homo sapiens (human)
germ cell nucleusCellular tumor antigen p53Homo sapiens (human)
chromatinCellular tumor antigen p53Homo sapiens (human)
transcription regulator complexCellular tumor antigen p53Homo sapiens (human)
protein-containing complexCellular tumor antigen p53Homo sapiens (human)
plasma membraneGlutamate receptor 2Rattus norvegicus (Norway rat)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytosolPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
cytoskeletonPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
adherens junctionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
focal adhesionPolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
membranePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
extracellular exosomePolyunsaturated fatty acid lipoxygenase ALOX15BHomo sapiens (human)
plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basal plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
basolateral plasma membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
membraneATP-binding cassette sub-family C member 3Homo sapiens (human)
nucleolusMultidrug resistance-associated protein 4Homo sapiens (human)
Golgi apparatusMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
membraneMultidrug resistance-associated protein 4Homo sapiens (human)
basolateral plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
platelet dense granule membraneMultidrug resistance-associated protein 4Homo sapiens (human)
external side of apical plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
plasma membraneMultidrug resistance-associated protein 4Homo sapiens (human)
nucleoplasmNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
transcription regulator complexNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nuclear bodyNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
intermediate filament cytoskeletonNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
chromatinNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
nucleusNuclear receptor subfamily 1 group I member 2Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 2B1 Homo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
extracellular regionAlbuminHomo sapiens (human)
extracellular spaceAlbuminHomo sapiens (human)
nucleusAlbuminHomo sapiens (human)
endoplasmic reticulumAlbuminHomo sapiens (human)
endoplasmic reticulum lumenAlbuminHomo sapiens (human)
Golgi apparatusAlbuminHomo sapiens (human)
platelet alpha granule lumenAlbuminHomo sapiens (human)
extracellular exosomeAlbuminHomo sapiens (human)
blood microparticleAlbuminHomo sapiens (human)
protein-containing complexAlbuminHomo sapiens (human)
cytoplasmAlbuminHomo sapiens (human)
mitochondrial matrix60 kDa heat shock protein, mitochondrialHomo sapiens (human)
extracellular space60 kDa heat shock protein, mitochondrialHomo sapiens (human)
cytoplasm60 kDa heat shock protein, mitochondrialHomo sapiens (human)
mitochondrion60 kDa heat shock protein, mitochondrialHomo sapiens (human)
mitochondrial inner membrane60 kDa heat shock protein, mitochondrialHomo sapiens (human)
mitochondrial matrix60 kDa heat shock protein, mitochondrialHomo sapiens (human)
early endosome60 kDa heat shock protein, mitochondrialHomo sapiens (human)
cytosol60 kDa heat shock protein, mitochondrialHomo sapiens (human)
plasma membrane60 kDa heat shock protein, mitochondrialHomo sapiens (human)
clathrin-coated pit60 kDa heat shock protein, mitochondrialHomo sapiens (human)
cell surface60 kDa heat shock protein, mitochondrialHomo sapiens (human)
membrane60 kDa heat shock protein, mitochondrialHomo sapiens (human)
coated vesicle60 kDa heat shock protein, mitochondrialHomo sapiens (human)
secretory granule60 kDa heat shock protein, mitochondrialHomo sapiens (human)
extracellular exosome60 kDa heat shock protein, mitochondrialHomo sapiens (human)
sperm midpiece60 kDa heat shock protein, mitochondrialHomo sapiens (human)
sperm plasma membrane60 kDa heat shock protein, mitochondrialHomo sapiens (human)
migrasome60 kDa heat shock protein, mitochondrialHomo sapiens (human)
protein-containing complex60 kDa heat shock protein, mitochondrialHomo sapiens (human)
lipopolysaccharide receptor complex60 kDa heat shock protein, mitochondrialHomo sapiens (human)
mitochondrial inner membrane60 kDa heat shock protein, mitochondrialHomo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 2B6Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 2B6Homo sapiens (human)
cytoplasmCytochrome P450 2B6Homo sapiens (human)
endoplasmic reticulum membraneArylacetamide deacetylaseHomo sapiens (human)
endoplasmic reticulum membraneArylacetamide deacetylaseHomo sapiens (human)
cytoplasmCaspase-1Homo sapiens (human)
cytosolCaspase-1Homo sapiens (human)
nucleolusCaspase-1Homo sapiens (human)
cytoplasmCaspase-1Homo sapiens (human)
cytosolCaspase-1Homo sapiens (human)
microtubuleCaspase-1Homo sapiens (human)
plasma membraneCaspase-1Homo sapiens (human)
canonical inflammasome complexCaspase-1Homo sapiens (human)
NLRP1 inflammasome complexCaspase-1Homo sapiens (human)
NLRP3 inflammasome complexCaspase-1Homo sapiens (human)
AIM2 inflammasome complexCaspase-1Homo sapiens (human)
protein-containing complexCaspase-1Homo sapiens (human)
IPAF inflammasome complexCaspase-1Homo sapiens (human)
protease inhibitor complexCaspase-1Homo sapiens (human)
platelet alpha granule membraneAlpha-synucleinHomo sapiens (human)
extracellular regionAlpha-synucleinHomo sapiens (human)
extracellular spaceAlpha-synucleinHomo sapiens (human)
nucleusAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
mitochondrionAlpha-synucleinHomo sapiens (human)
lysosomeAlpha-synucleinHomo sapiens (human)
cytosolAlpha-synucleinHomo sapiens (human)
plasma membraneAlpha-synucleinHomo sapiens (human)
cell cortexAlpha-synucleinHomo sapiens (human)
actin cytoskeletonAlpha-synucleinHomo sapiens (human)
membraneAlpha-synucleinHomo sapiens (human)
inclusion bodyAlpha-synucleinHomo sapiens (human)
axonAlpha-synucleinHomo sapiens (human)
growth coneAlpha-synucleinHomo sapiens (human)
synaptic vesicle membraneAlpha-synucleinHomo sapiens (human)
perinuclear region of cytoplasmAlpha-synucleinHomo sapiens (human)
postsynapseAlpha-synucleinHomo sapiens (human)
supramolecular fiberAlpha-synucleinHomo sapiens (human)
protein-containing complexAlpha-synucleinHomo sapiens (human)
cytoplasmAlpha-synucleinHomo sapiens (human)
axon terminusAlpha-synucleinHomo sapiens (human)
neuronal cell bodyAlpha-synucleinHomo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
apical plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1A2Homo sapiens (human)
mitochondrion10 kDa heat shock protein, mitochondrialHomo sapiens (human)
membrane10 kDa heat shock protein, mitochondrialHomo sapiens (human)
extracellular exosome10 kDa heat shock protein, mitochondrialHomo sapiens (human)
mitochondrial matrix10 kDa heat shock protein, mitochondrialHomo sapiens (human)
cytoplasmGlutathione S-transferase omega-1Homo sapiens (human)
cytosolGlutathione S-transferase omega-1Homo sapiens (human)
extracellular exosomeGlutathione S-transferase omega-1Homo sapiens (human)
cytoplasmGlutathione S-transferase omega-1Homo sapiens (human)
cytosolDNA-directed RNA polymerase subunit betaMycobacterium tuberculosis H37Rv
extracellular spaceThiosulfate sulfurtransferaseHomo sapiens (human)
mitochondrionThiosulfate sulfurtransferaseHomo sapiens (human)
mitochondrial matrixThiosulfate sulfurtransferaseHomo sapiens (human)
mitochondrionThiosulfate sulfurtransferaseHomo sapiens (human)
endoplasmic reticulum membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
membraneLanosterol 14-alpha demethylaseHomo sapiens (human)
plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
cell surfaceCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
intercellular canaliculusCanalicular multispecific organic anion transporter 1Homo sapiens (human)
apical plasma membraneCanalicular multispecific organic anion transporter 1Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B3Homo sapiens (human)
nucleoplasmBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
brush border membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
mitochondrial membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
membrane raftBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
external side of apical plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneBroad substrate specificity ATP-binding cassette transporter ABCG2Homo sapiens (human)
plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basal plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
basolateral plasma membraneSolute carrier organic anion transporter family member 1B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (5086)

Assay IDTitleYearJournalArticle
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1871137Antitubercular activity against Multidrug-resistant Mycobacterium tuberculosis clinical isolate PT20 assessed as bacterial growth inhibition incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties.
AID373981Drug uptake in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID278680Antibacterial activity against Enterococcus faecium isolate 57512007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1223013Activation of mouse PXR expressed in human HepG2 cells at 50 uM after 24 hrs by firefly luciferase DR3 reporter gene assay2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1173786Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 100 uM after 72 hrs by MTT assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID373037Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate DL34 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID276760Antimycobacterial activity against Mycobacterium kansasii measured as susceptibility at 1 ug/mL2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1476410Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through carboxymethylcellulose vehicle as single oral dose per gavage after 4 hrs by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID442392Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification of benzofuro[2,3-b]quinoline derivatives as a new class of antituberculosis agents.
AID489577Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 21 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID534421Antibacterial activity against Mycobacterium bovis BCG-Denmark2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID564131Antimicrobial activity against methicillin-resistant Staphylococcus aureus HUSA 304 infected in Wistar rat assessed as decrease in bacterial load in tissue cage fluid at 35 mg/kg, ip administered every 12 hrs for 7 days measured on day 11 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID1304522Antibacterial activity against Staphylococcus aureus XEN36 incubated overnight by microbroth-dilution method2016Journal of natural products, Mar-25, Volume: 79, Issue:3
Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.
AID572060Antibacterial activity against abeS-deficient Acinetobacter baumannii AC0037 by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID456897Inhibition of Mycobacterium membrane bound ATP synthase2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents.
AID671454Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth at 2 ug/ml by radiometric-BACTEC assay2012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors.
AID1210918Activity of AADAC in human jejunum microsome2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID1293906Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1423470Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding after 45 mins by spectrometric analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID283170Increase in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID425596Antibacterial activity against extracellular Escherichia coli isolate HM605 isolated from colonic mucosal biopsies of patient with Crohn's disease at 0.01 to 10 ug/ml after 3 hrs2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID530673Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1427050Selectivity index, ratio of GI50 for human A549 cells to MIC for dormant stage of Mycobacterium tuberculosis H37Ra ATCC 251772017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID537117Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774A1 cells assessed as reduction of bacterial growth at 1 ug/ml after 6 days relative to untreated control2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1597874Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis ATCC 35822 after 7 days by resazurin microtiter assay
AID103648In vitro activity of compound against rapidly growing Mycobacterium fortuitum 12871990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID373936Half life in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 2100 mg, po administered twice a week2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID571437Antibacterial activity against Escherichia coli IH3080 by Etest method in presence of 1 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1337868Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID372538Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 0-24 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID669186Antitubercular activity against Mycobacterium tuberculosis H37Rv in aerobic conditions after 7 days by microplate-based alamar blue assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1191013Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 7 days under 7H12 medium by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1514453Antitubercular activity against moxifloxacin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1765357Antimycobacterial activity against Streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 35820 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID373966Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as rate constant for maximal bacterial kill2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID626870Inhibition of Mycobacterium tuberculosis expressing RNA polymerase RpoB S450L mutant after 10 mins using ribo green by rolling circle transcription assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID1832325Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis HN878 harboring RpoBH455D mutant assessed as bacterial growth inhibition measured after 5 days by serial dilution method2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel C-3-(N-alkyl-aryl)-aminomethyl rifamycin SV derivatives exhibit activity against rifampicin-resistant Mycobacterium tuberculosis RpoB
AID732683Cytotoxicity against human HEK293 cells assessed as inhibition of cell viability after 24 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Syntheses of lipophilic chalcones and their conformationally restricted analogues as antitubercular agents.
AID1244813Antibacterial activity against Staphylococcus aureus ATCC 4163 after 18 hrs by serial microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID569258Antimycobacterial activity against Mycobacterium avium subsp. hominissuis 1042011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1070197Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis UT544 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1196885Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID1364759Antibacterial activity against replicative stage Mycobacterium tuberculosis H37Rv after 7 days by MABA2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID530996Antimicrobial activity against Clostridium difficile isolate 43 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID425628Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as effect on average time to detection of growth at >10'2 CFU of inoculum by MGIT 960 susceptibility test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID645552Antimicrobial activity against Mycobacterium abscessus by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1262037Antitubercular activity against Mycobacterium tuberculosis H37Rv measured on day 4 by microplate Alamar blue assay2015European journal of medicinal chemistry, Nov-13, Volume: 105Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents.
AID534106Antibacterial activity against Pasteurella multocida AL435 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1297732Octanol-water partition coefficient, logP of the compound after 1 hr by UV-vis spectrophotometric analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID380453Antibacterial activity against Mycobacterium tuberculosis by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID1296399Cytotoxicity against MDCK2-MDR1 cells assessed as cell viability after 24 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID373794fAUC (0 to infinity) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 600 mg/day, po2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1890843Antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC empty vector assessed as inhibition of mycobacterial growth incubated for 3 to 5 days by resazurin microtiter assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID572531Absorption rate constant in pulmonary tuberculosis patient in first order model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID560501Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gz06040 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1427042Antitubercular activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells after 8 days by nitrate reductase assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID294765Antibacterial activity against methicillin-resistant Staphylococcus aureus 910 after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID1311233Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1577325Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1471053Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium bovis BCG ATCC 35743 dormant stage2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID634271Antimycobacterial activity against Mycobacterium tuberculosis isolate MA03 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1291988Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of mycobacterial replication after 6 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Investigation of 4-amino-5-alkynylpyrimidine-2(1H)-ones as anti-mycobacterial agents.
AID1278195Cytotoxicity against mouse J774 cells assessed as cell viability at 80 ug/ml by MTT assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
AID1625575Bactericidal activity against wild-type non-replicating Mycobacterium tuberculosis H37Rv at 1 to 100 ug/ml incubated for 7 days measured at OD580 = 0.1 in presence of up to 0.5 mM NaNO22016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID530796Antimicrobial activity against Clostridium difficile isolate 27 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID325118Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 2 ug/ml after 3 weeks at by BACTED460 method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis.
AID1471025Growth inhibition of Mycobacterium tuberculosis H37Ra ATCC 25177 at 30 ug/ml by XTT dye based two-fold dilution method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1654158Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth after 7 days by alamar blue assay2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID1244179Antitubercular activity against fluorescent reporter strain of Mycobacterium tuberculosis H37Rv after 5 days by fluorescence assay2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
AID1365704Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv RIF-R1 harboring rpoB S522L mutant after 5 days2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID251784Antimycobacterial activity of compound against Mycobacterium tuberculosis H37Rv at 0.125 ug/mL2004Bioorganic & medicinal chemistry letters, Aug-02, Volume: 14, Issue:15
Antituberculous activity of some aryl semicarbazone derivatives.
AID545936Ratio of MIC for Escherichia coli IH3080 to MIC for Escherichia coli IH3080 in presence of 4 ug/ml of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1071081Cytotoxicity against mouse J774A1 cells assessed as cell viability at 1 ug/ml after 7 days by MTT assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID531271Antimicrobial activity against Clostridium difficile isolate 43 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1765358Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID341064AUC (0 to 24 hrs) in human at 600 mg, po once daily after 14 days coadministered with moxifloxacin at 400 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID1827056Antibacterial activity against Vibrio cholerae A1552 El Tor assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1856916Antibacterial activity against Escherichia coli ATCC 25922 assessed as fold increase in MIC measured after 15 passages by resistance development assay relative to control2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1423478Antibacterial activity against Pseudomonas aeruginosa ATCC 10145 after 24 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID373962Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as sigmoidicity constant for drug effect on microbial grow2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID495511Antibacterial activity against multidrug-resistant Acinetobacter baumannii BM4665 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID332360Inhibition of RNA synthesis in Bacillus subtilis assessed as [3H]uridine uptake at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2003Journal of natural products, Feb, Volume: 66, Issue:2
Antibacterial diterpenes from Calceolaria pinifolia.
AID373034Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate BJ3-9 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID531260Antimicrobial activity against Clostridium difficile isolate 32 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1244176Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
AID1400043Bactericidal activity against Staphylococcus aureus BAA 1683 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1291987Antimycobacterial activity against Mycobacterium bovis BCG assessed as inhibition of mycobacterial replication after 6 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Investigation of 4-amino-5-alkynylpyrimidine-2(1H)-ones as anti-mycobacterial agents.
AID1296397Cytotoxicity against human HeLa cells assessed as cell viability after 24 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID555304Antibacterial activity against methicillin-resistant Staphylococcus aureus 507 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID594787Antituberculosis activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry letters, May-15, Volume: 21, Issue:10
A green expedient synthesis of pyridopyrimidine-2-thiones and their antitubercular activity.
AID325116Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 2 ug/ml after 1 week by BACTED460 method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis.
AID748176Inhibition of wild type Mycobacterium tuberculosis RNA polymerase after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID145298Antibacterial activity against Mycobacterium tuberculosis H37Rv.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID574554Decrease in PSMbeta1 levels in Staphylococcus aureus USA300 at subinhibitory concentration after 24 hrs by RP-HPLC/ESI-MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID1264490Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin microtiter assay2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents.
AID611488Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 116 isolated from patient knee abscess after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID545813Antimicrobial activity against vancomycin-resistant Staphylococcus aureus isolate VRS5 assessed as inhibition of biofilm formation after 24 hrs by by serial dilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID580618Inhibition of protein synthesis in Bacillus subtilis BD54 at 5 X MIC by L-[4,5-3H]leucine incorporation assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.
AID1055956Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1060900Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as parasite growth inhibition after 28 days by agar dilution method2014European journal of medicinal chemistry, Jan, Volume: 71Rational design and synthesis of novel dibenzo[b,d]furan-1,2,3-triazole conjugates as potent inhibitors of Mycobacterium tuberculosis.
AID571651Ratio of the MIC for Escherichia coli in the absence of NAB7061 to MIC for Escherichia coli in the presence of 4 ug/ml of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID562798Antimicrobial activity against Chlamydia muridarum MoPn/tetR14 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1079933Acute liver toxicity defined via clinical observations and clear clinical-chemistry results: serum ALT or AST activity > 6 N or serum alkaline phosphatases activity > 1.7 N. This category includes cytolytic, choleostatic and mixed liver toxicity. Value is
AID326295Antibacterial activity against methicillin-resistant Staphylococcus aureus 859 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID530652Inhibition of DNA synthesis in rifamycin-resistant Staphylococcus aureus CB370 harboring rpoB H481Y mutant gene assessed as [methyl-3H]thymidine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1335284Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling activity using relaxed pBR322 as substrate incubated for 30 mins by ethidium bromide staining based agarose gel electrophoresis2016European journal of medicinal chemistry, Nov-29, Volume: 124Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
AID297113Antibacterial activity against Mycobacterium bovis BCG Tokyo after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID400493Inhibition of AAH in Sprague-Dawley rat intestine microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 0.50 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1070195Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis MTB985 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID564974Antimicrobial activity against Mycobacterium bovis BCG by resazurine microtiter assay in presence of 1 mg/liter CCCP2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1476350Antitubercular activity against isoniazid resistant Mycobacterium tuberculosis H37Rv ATCC 35822 after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1612597Antibacterial activity against Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Feb-01, Volume: 163Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
AID510516AUC (0 to 24 hrs) in tuberculosis patient at 10 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID562782Antimicrobial activity against Chlamydia trachomatis L2/oflR harboring ompA gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1143684Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in lung at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 3 w2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
AID1167605Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold agar dilution method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.
AID1444294Antimycobacterial activity against Mycobacterium tuberculosis H37Rv CNCTC My 331/88 after 14 days by micromethod2017European journal of medicinal chemistry, Apr-21, Volume: 130Structure-activity relationship studies on 3,5-dinitrophenyl tetrazoles as antitubercular agents.
AID278857Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID533661Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid CU12008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID1294367Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774 cells assessed as log reduction in bacterial burden at 10 times lower MIC measured 7 days postinfection relative to control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID529530Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-GTG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID562788Antimicrobial activity against Chlamydia muridarum MoPn/rifRoflR harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1209531Activation of rat PXR expressed in human HepG2 cells coexpressing CYP3A4 at 0.1 to 10 uM after 24 hrs by dual luciferase reporter gene assay relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID1497850Antibacterial activity against Staphylococcus aureus ATCC 29737 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID445334Selectivity for Mycobacterium tuberculosis H37Rv over human MRC5 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1879552Antibacterial activity against Bacteroides vulgatus MMX 83482022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID531035Antimicrobial activity against Clostridium difficile isolate 2 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID604201Antimycobacterial activity against mid-log phase of Mycobacterium tuberculosis Erdman ATCC 35801 after 7 days by 96 well plate assay2011Bioorganic & medicinal chemistry, Jul-01, Volume: 19, Issue:13
Evaluation of NTF1836 as an inhibitor of the mycothiol biosynthetic enzyme MshC in growing and non-replicating Mycobacterium tuberculosis.
AID535541Antimicrobial activity against glycopeptide-intermediate Staphylococcus epidermidis NRS6 by broth microdilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Daptomycin is effective for treatment of experimental endocarditis due to methicillin-resistant and glycopeptide-intermediate Staphylococcus epidermidis.
AID1209456Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1602928Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1482267Antibacterial activity against Escherichia coli MG1655 measured every 15 mins for 12 hrs2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Prediction of Antibiotic Interactions Using Descriptors Derived from Molecular Structure.
AID1597871Cytotoxicity against mouse J774.A1 cells measured after 24 hrs by resazurin based assay
AID1856899Induction of cytoplasmic membrane depolarization in Escherichia coli ATCC 25922 assessed as increase in fluorescence intensity measured within 1 min by DiSC3-5 dye based fluorescence method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID425583Antibacterial activity against Escherichia coli isolate HM605 isolated from colonic mucosal biopsies of patient with Crohn's disease2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1311273Antimycobacterial activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 measured on day 8 by XTT reduction menadione assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID368644Terminal apparent distribution volume in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1304831Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 assessed as biofilm eradication incubated for 24 hrs by CBD assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1335981Antibacterial activity against isoniazid/rifampin-resistant Mycobacterium tuberculosis after 8 to 9 days by BacT/Alert MP bottle assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains.
AID461351Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections.
AID1172690Anti-tubercular activity against Mycobacterium tuberculosis H37Rv by resazurin microtitre assay2014Bioorganic & medicinal chemistry letters, Nov-15, Volume: 24, Issue:22
Design, synthesis and molecular docking of substituted 3-hydrazinyl-3-oxo-propanamides as anti-tubercular agents.
AID1129651Selectivity index, ratio of IC50 for mouse J774A1 cells to MIC for Mycobacterium tuberculosis H37Rv expressing luciferase2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
1,2,3,4,8,9,10,11-octahydrobenzo[j]phenanthridine-7,12-diones as new leads against Mycobacterium tuberculosis.
AID1891919Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1062058Antimicrobial activity against Mycobacterium smegmatis (MC2) ATCC 19420 after 7 days by resazurin assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents.
AID434061Immunomodulatory effect in human A549 cells assessed as reduction in spontaneous release of [3H]arachidonic acid by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID373748Antimicrobial activity against mupirocin-resistant methicillin-resistant Staphylococcus aureus by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID373971Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as sigmoidicity constant for microbial killing2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1627299Growth inhibition of african green monkey Vero cells at highest concentration measured after 72 hrs by MTS assay relative to control2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New antibacterial agents: Hybrid bioisoster derivatives as potential E. coli FabH inhibitors.
AID1359860Inhibition of amyloid beta (1 to 42) (unknown origin) self-induced aggregation at 100 uM incubated for 48 hrs by thioflavin-T fluorescence assay relative to control2018European journal of medicinal chemistry, May-25, Volume: 152Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds.
AID510989Ratio of AUC to MIC for Acinetobacter baumannii 1327 in pharmacokinetic-pharmacodynamic New Zealand rabbit meningitis model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1182136Antitubercular activity against Mycobacterium smegmatis by checkerboard assay in presence of chlorpromazine2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID1658975Antibacterial activity against Streptococcus agalactiae ATCC 12386 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID279351Inhibition of protein synthesis in Staphylococcus aureus ATCC 29213 assessed as [3H]aminoacid incorporation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Dual targeting of GyrB and ParE by a novel aminobenzimidazole class of antibacterial compounds.
AID618759Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis ATCC 35338 harboring His-526-Tri mutation in rpoB gene after 9 days by resazurin reduction assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Quinonoid and phenazine compounds: synthesis and evaluation against H37Rv, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis.
AID700537Antimycobacterial activity against Mycobacterium smegmatis ATCC 19420 at 1 to 100 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID1194622Antimycobacterial activity against Mycobacterium avium complex isolate CIT19/06 incubated for 5 days by alamar blue assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides.
AID356974Inhibition of RNA synthesis in Escherichia coli assessed as incorporation of [3H]uridine at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2001Journal of natural products, Jul, Volume: 64, Issue:7
Biological and mechanistic activities of xanthorrizol and 4-(1',5'-dimethylhex-4'-enyl)-2-methylphenol isolated from Iostephane heterophylla.
AID413209Induction of CYP3A4 activity in cryopreserved human hepatocytes from male DJV donars with no adverse medical history or substance or alcohol abuse at 20 uM relative to 20 uM rifampin2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
AID519833Antimicrobial activity against Aeromonas hydrophila subsp. hydrophila ATCC 7966 harboring plasmid pEX19Gm by agar dilution method in presence of 64 mg/L efflux pump inhibitor phenylalanine-arginine-beta-naphthylamide2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID665372Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate at 80 ug/mL by radiometric growth assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives.
AID285161Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID501185Antimicrobial activity against methicillin sensitive Staphylococcus aureus 375 at 5 ug after 18 hrs by agar diffusion method2009Journal of natural products, Oct, Volume: 72, Issue:10
Norselic acids A-E, highly oxidized anti-infective steroids that deter mesograzer predation, from the Antarctic sponge Crella sp.
AID584116Ratio of MIC for Escherichia coli KAM32 harboring cloned pSP72 lmrS to MIC for Escherichia coli KAM32 harboring pSP722010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.
AID617025Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 2 weeks by BACTEC 460 radiometric method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.
AID1311227Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-52016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1400046Antibacterial activity against Enterococcus faecalis ATCC 349 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID645539Antitubercular activity against kanamycin-resistant Mycobacterium tuberculosis by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1476343Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 under normal pH 6.8 condition2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID285196Antimicrobial activity against Escherichia coli M074 mutant with AG100 lon2::IS186 acrR::IS genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID278678Antibacterial activity against Enterococcus faecium isolate 57492007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID413207Induction of CYP3A4 in cryopreserved human hepatocytes from male DJV donars with no adverse medical history or substance or alcohol abuse assessed as mRNA expression at 20 uM relative to 20 uM rifampin2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
AID645693Antimicrobial activity against Mycobacterium smegmatis by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID368647Tmax in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID247756Inhibitory concentration required to produce cytotoxicity against VERO cells2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Identification of heteroarylenamines as a new class of antituberculosis lead molecules.
AID1287507Selectivity index, ratio of GI50 for human HeLa cells to MIC for active state Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID1326099Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 11168 after 7 days by microplate alamar blue assay
AID1879493Antibacterial activity against Helicobacter pylori clinical isolate USA2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID444055Fraction absorbed in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1253865Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Discovery of the disubstituted oxazole analogues as a novel class anti-tuberculotic agents against MDR- and XDR-MTB.
AID1491512Genotoxicity in Salmonella typhimurium TA104 harboring Pr1 lux operon fusion at 1.28 to 128 uM measured every 5 mins for 4 hrs in presence of S9 liver fraction by vitotox assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID774192Antitubecular activity against Mycobacterium tuberculosis H37Pv assessed as growth inhibition after 4 days by microplate Alamar blue assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Phomapyrrolidones A-C, antitubercular alkaloids from the endophytic fungus Phoma sp. NRRL 46751.
AID1627515Antitubercular activity against Mycobacterium tuberculosis H37Rv INH-R2 ATCC 35822 after 5 days2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID1210917Activity of AADAC in human liver microsome2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID1632663Antitubercular activity against dormant Mycobacterium bovis BCG ATCC 35734 after 12 days by nitrate reductase assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID1730994Antitubercular activity against isoniazid/rifampin/levofloxacin/ofloxacin/kanamycin extensively drug resistance Mycobacterium tuberculosis TF274 XDR by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID620091Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by resazurin assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties.
AID1303895Antibacterial activity against multidrug resistant Pseudomonas aeruginosa NCTC 10332 (ATCC 10145) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID1627518Antitubercular activity against Mycobacterium tuberculosis H37Rv FQ-R1 harboring gyrB D94N mutant after 5 days2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID1299956Antibacterial activity against Mycobacterium tuberculosis H37Rv in 7H12 medium by microplate alamar blue assay2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
AID285157Antimicrobial susceptibility of tetracycline-resistant Streptococcus pneumoniae from respiratory tract disease patient assessed as percent susceptible isolates2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Clonal diversity and resistance mechanisms in tetracycline-nonsusceptible Streptococcus pneumoniae isolates in Poland.
AID606484Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2011Journal of natural products, May-27, Volume: 74, Issue:5
Antituberculosis cycloartane triterpenoids from Radermachera boniana.
AID290253Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Hydroxythiosemicarbazones: synthesis and in vitro antitubercular activity.
AID452742Antibacterial activity against Escherichia coli M15 containing pQE30 expression vector2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.
AID558241Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 20 mg/liter upto 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID588216FDA HLAED, serum glutamic oxaloacetic transaminase (SGOT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1133242Antimicrobial activity against Mycobacterium tuberculosis H37Rv by agar dilution method1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Synthesis and quantitative structure--activity relationships of some antibacterial 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones.
AID1609005Antimycobacterial activity against Mycobacterium aurum DSM 43999 after 72 hr by resazurin dye based microdilution method2019European journal of medicinal chemistry, Nov-01, Volume: 181Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.
AID581192Effect on NF-kappaB activation in 100 ng/ml IL-1beta, TNF-alpha and IFN-gamma-stimulated human A549 cells assessed as degradation of inhibitory subunit IkappaB at 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1053479Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA G96V mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID774603Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene assessed as reduction in bacterial count after 6 days by luminometry2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID1185719Antituberculosis activity against Mycobacterium bovis after 14 days by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID373963Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as rate constant for maximal bacterial growth2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1577335Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 234/2005 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID604021Unbound volume of distribution in Sprague-Dawley rat brain measured per gram of brain tissue administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr b2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID776893Antibacterial activity against Bacillus subtilis2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID1856866Stability of compound in serum measured after 1 to 6 hrs by RP-HPLC analysis2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1557232Antitubercular activity against resistant Mycobacterium tuberculosis 21 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID534361Antibacterial activity against Acinetobacter baumannii GIL1 isolate harboring intrinsic blaOXA-51/69-like gene by Etest method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Carbapenem-resistant Acinetobacter baumannii isolates expressing the blaOXA-23 gene associated with ISAba4 in Belgium.
AID518801Antimycobacterial activity against Mycobacterium avium serovar 8 after 14 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1230065Antibacterial activity against methicillin-resistant Staphylococcus aureus GRE2372 assessed as inhibition of bacterial growth2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and antimicrobial activity of chloramphenicol-polyamine conjugates.
AID571390Antibacterial activity against Acinetobacter baumannii F264 by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID645554Antimicrobial activity against Mycobacterium marinum by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID293591Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID765269fT>MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID669834Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.
AID1887547Antibacterial activity against Escherichia coli ATCC 25922 assessed as reduction in bacterial growth incubated for 16 to 18 hrs in presence of PMBN by broth microdilution method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID531013Antimicrobial activity against Clostridium difficile isolate 60 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1856859Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as growth inhibition measured after 18 to 24 hrs by CLSI based broth microdilution method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID497974Drug level in bone/joint infection patient serum assessed as median concentration at 2400 mg, iv after 40 days2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Continuous clindamycin infusion, an innovative approach to treating bone and joint infections.
AID326289Antibacterial activity against methicillin-resistant Staphylococcus aureus 789 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID1612292Cytotoxicity against African green monkey Vero cells by CellTiter 96 aqueous nonradioactive cell proliferation assay2019Journal of natural products, 03-22, Volume: 82, Issue:3
Isolation of Tryptanthrin and Reassessment of Evidence for Its Isobaric Isostere Wrightiadione in Plants of the Wrightia Genus.
AID144734In vitro inhibition of Mycobacterium tuberculosis H37Rv, determined at 0.2 ug/mL2004Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
AID1879495Antibacterial activity against Staphylococcus aureus ATCC 292132022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID577488fCmax in Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model at 600 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID495236Antimicrobial activity against Mycobacterium tuberculosis NJT210GAC harboring embB406 GGC-GAC(Gly-Asp) mutation in embB gene after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID1447550Antibacterial activity against multidrug-resistant Klebsiella pneumoniae 116381 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1497861Antibacterial activity against Proteus vulgaris PTCC 1182 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID428294Antimicrobial activity against Acinetobacter baumannii BM4652 expressing adeIJK genes with pAT807 isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID531040Antimicrobial activity against Clostridium difficile isolate 7 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID305226Antimicrobial activity against Arr-1 positive Mycobacterium smegmatis DSM 437562007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID1594301Antitubercular activity against dormant stage of Mycobacterium bovis BCG ATCC 35743 by two fold dilution technique2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID370071Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35822 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID583687Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315deltaIP harboring rpoB 621E mutant after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID374182Antimicrobial activity against 2 months old culture of Mycobacterium tuberculosis H37Ra assessed as colony forming unit at 10 ug/ml for 3 days at pH 5.52007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pyrrolidine dithiocarbamate and diethyldithiocarbamate are active against growing and nongrowing persister Mycobacterium tuberculosis.
AID529303Antimicrobial activity against Acinetobacter genospecies 3 isolate Ac057 expressing beta-lactamase Oxa-58 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Characterization of the carbapenem-hydrolyzing oxacillinase oxa-58 in an Acinetobacter genospecies 3 clinical isolate.
AID656233Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, ethambutol-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1825034Selectivity index ratio of MIC90 in Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST-Fe media to Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST media2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
AID373978Antimycobacterial activity against Mycobacterium tuberculosis isolate2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID523664Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta206 with RNA polymerase beta subunit A471S mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID563697Antibacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID1252462Inhibition of DNA gyrase GyrA/GyrB in Mycobacterium tuberculosis incubated for 30 mins assessed as reduction in supercoiling of relaxed relaxed pBR322 DNA by ethidium bromide staining based agarose gel electrophoresis method2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID559914Volume of distribution in epithelial lining fluid of patient with tuberculosis at 600 to 1200 mg/kg, po administered as single dose2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Population modeling and Monte Carlo simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of rifampin in lungs.
AID671448Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as inhibition of microbial growth at 2 ug/ml incubated for 6 days by MABA method2012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors.
AID373947Ratio of fCmax to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1916612Antitubercular activity against Mycobacterium tuberculosis mc 2 7000 assessed as bacterial growth inhibition2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1252191Antimycobacterial activity against Mycobacterium tuberculosis in GAS medium by microplate alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
Syntheses and evaluation of substituted aromatic hydroxamates and hydroxamic acids that target Mycobacterium tuberculosis.
AID1435651Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID352094Antimicrobial activity against Bacillus subtilis ATCC 6633 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID1869572Bactericidal activity against Acinetobacter baumannii DSM 300007 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID530795Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 26 expressing RpoB R505K mutant by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1234656Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated up to 7 days measured on day 7 by microplate Alamar Blue assay2015European journal of medicinal chemistry, Jul-15, Volume: 100Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design.
AID278683Antibacterial activity against Enterococcus faecalis isolate 57452007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID396038Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pAP2 plasmid containing Enterobacter cloacae acrA gene by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID555293Antibacterial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID733061Antitubercular activity against Mycobacterium tuberculosis H37Rv by BacTiter-Gl Microbial Cell Viability assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents.
AID1765764Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth at 1 ug/ml measured by microplate alamar blue assay2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Design and synthesis of novel 5-alkynyl pyrimidine nucleosides derivatives: Influence of C-6-substituent on antituberculosis activity.
AID278860Antiproliferative effect against HeLa cells after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID372540Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 0-48 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1447593Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P262-101856 infected in Galleria mellonella assessed as mortality at 75 mg/kg after 24 hrs relative to control2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID545043Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ068 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID545050Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ250 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID1732052Antibacterial activity against Mycobacterium smegmatis VKPM Ac-13392021European journal of medicinal chemistry, Apr-05, Volume: 215Discovery of novel N
AID1473741Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID727919Antibacterial activity against Enterococcus faecalis ATCC 29212 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID1692049Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth preincubated for 72 hrs followed by phAE202 and Cacl2 addition and measured after 4 hrs by luciferase reporter mycobacterio-phage assay2020European journal of medicinal chemistry, Jul-15, Volume: 198Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis.
AID1304523Bactericidal activity against Staphylococcus aureus XEN36 incubated overnight by microbroth-dilution method2016Journal of natural products, Mar-25, Volume: 79, Issue:3
Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.
AID372462Antimalarial activity as 3rd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs dose then 48 hrs drug-free2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1071102Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1334260Selectivity index, ratio of GI50 for human HCT116 cells to MIC90 for Mycobacterium bovis BCG ATCC 35743 active stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID634283Antimycobacterial activity against Mycobacterium tuberculosis isolate 343 expressing rpoB Asp516Val mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID600829Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents.
AID1063301Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay2014European journal of medicinal chemistry, Jan-24, Volume: 72Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.
AID555737Antibacterial activity against methicillin-resistant and vancomycin-resistant Staphylococcus aureus VRS1 by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID373979Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 2517 infected in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as microbial killing administered at simulated dose of 4200 mg, po onc2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1210914Inhibition of AADAC in human liver microsome2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID543812Bactericidal activity against Streptococcus pyogenes VT 59 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1348987Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1756864Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 5 days by microplate alamar blue assay2021European journal of medicinal chemistry, Apr-05, Volume: 215Antitubercular properties of thiazolidin-4-ones - A review.
AID1055936Antimycobacterial activity against Mycobacterium tuberculosis harboring luxABCDE under hypoxic condition after 10 days by MABA assay in presence of 4% bovine serum albumin2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID530052Antimicrobial activity against Staphylococcus aureus RN4220 expressing gyrB D437N mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1692252Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16883 clinical isolate assessed as inhibition of bacterial growth incubated for 7 days by MABA assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Identification of benzothiazinones containing 2-benzyl-2,7-diazaspiro[3.5]nonane moieties as new antitubercular agents.
AID1888133Antimycobacterial activity against Mycobacterium smegmatis mc2155 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID293586Antibacterial activity against Staphylococcus aureus isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID625279Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for bilirubinemia2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID457432Antitubercular activity against Mycobacterium tuberculosis H37Rv after 28 hrs by low oxygen recovery assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID1887542Antibacterial activity against Acinetobacter baumannii BAA 1605 assessed as reduction in bacterial growth incubated for 16 to 18 hrs by broth microdilution method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID1716773Antibacterial activity against Pseudomonas aeruginosa 260-97103 assessed as reduction in bacterial growth by measuring doxycycline MIC at 2 ug/ml incubated for 18 hrs in presence of doxycycline by broth microdilution assay (Rvb = 16 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID502973Antimicrobial activity against Mycobacterium bovis BCG by alamar blue assay2007Nature chemical biology, Jun, Volume: 3, Issue:6
Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID531044Antimicrobial activity against Clostridium difficile isolate 11 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1179478Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 in 7H9 medium after 3 days and 4 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID520086Antimicrobial activity against acrAB-deficient Escherichia coli TG1 harboring AcrAB efflux pump by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID1401971Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 358222018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID1891920Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTT assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1205464Antitubercular activity against rifampin, isoniazid, kanamycin and ofloxacin-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID368645Apparent oral clearance in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID531042Antimicrobial activity against Clostridium difficile isolate 9 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1297725Antibacterial activity against methicillin resistant Staphylococcus aureus isolate 2 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID373795AUC (0 to 168 hrs) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 600 mg/day, po2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1732051Antibacterial activity against Mycobacterium smegmatis mc21552021European journal of medicinal chemistry, Apr-05, Volume: 215Discovery of novel N
AID1596586Resistance index, ratio of MIC for antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 treated over 1 passage to MIC for antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 treated for 18 to 20 h2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID774300Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID626872Antimicrobial activity against wild type Escherichia coli DH5[alpha] after 16 to 20 hrs2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID1129650Cytotoxicity against mouse J774A1 cells assessed as cell viability after 24 hrs by Trypan blue exclusion assay2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
1,2,3,4,8,9,10,11-octahydrobenzo[j]phenanthridine-7,12-diones as new leads against Mycobacterium tuberculosis.
AID1639085Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue method2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Expansion of a novel lead targeting M. tuberculosis DHFR as antitubercular agents.
AID1825029Antitubercular activity against Mycobacterium smegmatis mc2155 ATCC 700084 cultured in GAST media incubated for 24 hrs by resazurin microtiter assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
AID406467Cmax in albino guinea pig cage fluid at 12.5 mg/kg, ip administered every 12 hrs for 4 days2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID581662Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU after 72 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1500589Antitubercular activity against Mycobacterium tuberculosis INH-R1 harboring katG Y155 truncated mutant after 5 days by fluorescence-based assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID477411Antibacterial activity against MBX-1090-resistant Staphylococcus aureus isolate d20A1 after 16 to 20 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Efflux-mediated bis-indole resistance in Staphylococcus aureus reveals differential substrate specificities for MepA and MepR.
AID531033Antimicrobial activity against Clostridium difficile isolate 80 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID404133Antibacterial activity against Streptococcus pneumoniae MB2122005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID588218FDA HLAED, lactate dehydrogenase (LDH) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID373968Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as sigmoidicity constant for microbial killing2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1626625Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID434072Inhibition of IL-1-beta-induced COX2 expression in human A549 cells at 50 ug/ml measured after 24 hrs of IL1-beta challenge by Western blot analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID523775Antimicrobial activity against Streptomyces lydicus NRRL 2494 after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID565798Antimicrobial activity against Neisseria meningitidis harboring rpoB57 D542N mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID694774Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis ATCC 35338 after 7 days by resazurin microtitre assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
1,3-Azoles from ortho-naphthoquinones: synthesis of aryl substituted imidazoles and oxazoles and their potent activity against Mycobacterium tuberculosis.
AID1678509Antibacterial activity against Clostridium difficile BAA-1805 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID555299Antibacterial activity against Tmp-resistant coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1782928Selectivity index, ratio of CC50 for mouse RAW264.7 cells to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 272942021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID510970Antimicrobial activity against Acinetobacter baumannii infected in C57BL/6 mouse model assessed as reduction in bacterial count in blood at total dose of 100 mg/kg/day, ip administered as four divided doses after 72 hrs2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID532022Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to CFU count by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID408873Protection index, ratio of MNTD50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis 1034712008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID581060Effect on iNOS in human A549 cells assessed as increase in iNOS mRNA expression at 50 ug/ml after 19 hrs by TaqMan real-time RT-PCR relative to control2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1476409Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through carboxymethylcellulose vehicle as single oral dose per gavage after 2 hrs by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1181167Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_1 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID609619Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues.
AID1154350Antimycobacterial activity against Mycobacterium tuberculosis over expressing PimA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1476353Antitubercular activity against dormant stage Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days in anaerobic condition followed by incubation for 28 hrs in ambient gaseous condition measured after day 11 by two fold serial dilution assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID293525Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 1 ug/mL after 24 to 48 hrs by MABA2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Studies on acyclic pyrimidines as inhibitors of mycobacteria.
AID1300864Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two fold serial dilution method2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis, biological evaluation and structure-activity relationship of 2-styrylquinazolones as anti-tubercular agents.
AID305225Antimicrobial activity against rifampin-resistant Staphylococcus aureus ATCC 29213 rpoB (His481Tyr) mutant2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID1278844Antimycobacterial activity against nutrient starved Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial load at 10 ug/ml incubated for 7 days measured after 28 days by microplate reader analysis2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID558280Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in bacterial cfu in peritoneum at 60 mg/kg, sc administered 2 hrs after infection evry 8 hrs as three-dose regimen measured after 19 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID325000Antibacterial activity against Haemophilus influenzae Rd by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID1854276Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID510981Antimicrobial activity against Acinetobacter baumannii 13272010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID558243Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 2 mg/liter after 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1210916Activity of human recombinant AADAC2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID588986Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1A22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1624153Antitubercular activity against isoniazid/rifampicin resistant Mycobacterium tuberculosis isolate 5 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID545930Antimicrobial activity against in Enterobacter cloacae ATCC 23355 in presence of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID326290Antibacterial activity against methicillin-resistant Staphylococcus aureus 4803 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID1293894Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra ATCC 25177 incubated for 40 mins by XTT Reduction Menadione Assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1634890Cytotoxicity against human MRC5 cells assessed as cell survival rate at 16 uM after 24 hrs by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID1653480Antimicrobial activity against Escherichia coli ATCC 35218 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID292305Antibacterial activity against Escherichia coli ATCC 25922 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID727794Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID370101Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po after 1 hr2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID669835Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv ATCC 27294 by low oxygen recovery assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.
AID285567Bactericidal activity against 12-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 1 day by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID411982Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Selective activity against Mycobacteriumtuberculosis of new quinoxaline 1,4-di-N-oxides.
AID1658972Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID515287Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse spleen assessed as reduction of bacterial load at 10 mg/kg, po administered 1 week after infection measured after 4 weeks2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Anti-tubercular agents. Part 5: synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners.
AID1491286Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis MTB11168 after 7 days by microplate Alamar blue assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID774295Antimycobacterial activity against kanamycin-resistant Mycobacterium tuberculosis ATCC 358272013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID1904911Induction of drug resistance in methicillin-resistant Staphylococcus aureus USA400 NRS 123 assessed as fold increase in MIC measured after 15 passages by broth microdilution assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID531028Antimicrobial activity against Clostridium difficile isolate 75 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID373951Ratio of AUC to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L administered for 1 hr2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID518797Antimycobacterial activity against quinolone-resistant multidrug-resistant Mycobacterium tuberculosis after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID727917Antibacterial activity against Bacillus subtilis ATCC 6633 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID1223079Reduction in Ugt1a6b gene expression in wild type mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1297705Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Benzo[d]thiazol-2-yl(piperazin-1-yl)methanones as new anti-mycobacterial chemotypes: Design, synthesis, biological evaluation and 3D-QSAR studies.
AID1460597Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv2017Bioorganic & medicinal chemistry, 11-15, Volume: 25, Issue:22
Anti-tuberculosis activity and structure-activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives.
AID530789Antimicrobial activity against Clostridium difficile isolate 20 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID587297Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 4 weeks by microplate alamar blue assay2011European journal of medicinal chemistry, Mar, Volume: 46, Issue:3
Anti-tubercular agents. Part 6: synthesis and antimycobacterial activity of novel arylsulfonamido conjugated oxazolidinones.
AID537114Cytotoxicity against mouse J774A1 cells after 24 to 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1552793Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial cell growth incubated for 11 days measured under anaerobic LORA condition by luminescence assay2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents.
AID373749Antimicrobial activity against mupirocin-susceptible methicillin-resistant Staphylococcus aureus assessed as resistant rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID206239Antimicrobial activity derived as minimum inhibitory concentration are determined using brain-heart infusion medium against Staphylococcus aureus 209 P(FDA)1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID511021Cmax in New Zealand rabbit meningitis model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID581194Effect on iNOS expression in human A549 cells assessed as fold increase in 100 ng/ml IL1-beta, TNF-alpha and IFN-gamma-stimulated iNOS mRNA expression at 10 ug/ml after 19 hrs by TaqMan real-time RT-PCR relative to control2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1332969Antitubercular activity against clinical isolates of isoniazid/rifampicin/streptomycin/ethambutal resistant Mycobacterium tuberculosis after 7 days by REMA method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID1593910Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero cells to MIC for antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis H37Rv
AID168881Hypolipidemic activity was determined in male rats, and low-density lipoprotein level was determined at 100 mg/kg1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hypolipidemic activity of rifamycin derivatives.
AID545055Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate CC023 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID1265391Induction of P-glycoprotein in human LS180 cells assessed as accumulation of intracellular rhodamine-123 at 10 uM after 48 hrs by fluorescence assay relative to control2016European journal of medicinal chemistry, Jan-01, Volume: 107Discovery of a marine-derived bis-indole alkaloid fascaplysin, as a new class of potent P-glycoprotein inducer and establishment of its structure-activity relationship.
AID531275Antimicrobial activity against Clostridium difficile isolate 47 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1854284Antitubercular activity against clinical isolate isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID530346Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M plasmid carrying blaCTX-M-15 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID368639Half life in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID518796Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID562784Antimicrobial activity against Chlamydia trachomatis J/6276/rifR harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1474167Liver toxicity in human assessed as induction of drug-induced liver injury by measuring verified drug-induced liver injury concern status2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID1506729Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 28 days2017MedChemComm, Mar-01, Volume: 8, Issue:3
Design, synthesis, molecular-docking and antimycobacterial evaluation of some novel 1,2,3-triazolyl xanthenones.
AID1570212Antimycobacterial activity against Mycobacterium tuberculosis2019European journal of medicinal chemistry, 10-15, Volume: 180An insight into the medicinal perspective of synthetic analogs of indole: A review.
AID1601486Antimycobacterial activity against Mycobacterium bovis assessed as 90 percent growth inhibition measured after 120 hrs by turbidometric analysis2019Bioorganic & medicinal chemistry letters, 10-15, Volume: 29, Issue:20
Synthesis and evaluation of a novel quinoline-triazole analogs for antitubercular properties via molecular hybridization approach.
AID1594300Antitubercular activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 by two fold dilution technique2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID1365703Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv INH-R1 harboring katG Y155 mutant after 5 days2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID372539Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 0-24 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1634254Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 12.5 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID581666Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU level after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1244827Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by serial microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID530674Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB H481Y mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID341778AUC (0 to infinity) in Mycobacterium tuberculosis infected patient at 20 mg/kg, po administered daily for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID278576Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum.
AID1209582Unbound volume of distribution in Sprague-Dawley rat brain slices at 100 nM after 5 hrs2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID534112Ratio of MIC for Pasteurella multocida AL435 to MIC for TolC deficient Pasteurella multocida pm19802008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1287512Selectivity index, ratio of GI50 for human PANC1 cells to MIC for dormant state Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID774294Antimycobacterial activity against cycloserine-resistant Mycobacterium tuberculosis ATCC 358262013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID757717Antibacterial activity against Escherichia coli K-12 assessed as growth inhibiiton after 18 hrs2013European journal of medicinal chemistry, Jul, Volume: 65Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: structure-based optimization of a virtual screening hit.
AID1635218Antibacterial activity against Mycobacterium tuberculosis H37Rv by broth microdilution method2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Metabolites from the Fungal Endophyte Aspergillus austroafricanus in Axenic Culture and in Fungal-Bacterial Mixed Cultures.
AID360009Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 48 hrs by modified well microplate assay2001Journal of natural products, May, Volume: 64, Issue:5
Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha.
AID289134Cytotoxicity against Vero cells2007Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17
Synthesis and structure-antituberculosis activity relationship of 1H-indole-2,3-dione derivatives.
AID1181161Antimicrobial activity against clinical isolate Mycobacterium tuberculosis DKU97A assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID531307Antimicrobial activity against Clostridium difficile isolate 79 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1290938Antimycobacterial activity against Mycobacterium tuberculosis H37Rv cultured in GAS medium after 4 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID1311231Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-42016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1416770Antitubercular activity against Mycobacterium tuberculosis H37Rv2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and
AID1471031Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage by XTT dye based two-fold dilution method2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1580092Antibacterial activity against novobiocin and test compound-resistant Acinetobacter baumannii ATCC 17978 mutant generated from seven serial passages in presence of novobiocin by checkerboard assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Homodimeric Tobramycin Adjuvant Repurposes Novobiocin as an Effective Antibacterial Agent against Gram-Negative Bacteria.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID70791In vitro antibacterial activity of compound against Escherichia coli SKF 121401990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID278986Antimycobacterial activity in Mycobacterium ulcerans Cu001 infected BALB/c mouse assessed as mean number of CFU per foot-pad at 10 mg/kg, sc after 2 weeks2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Curing Mycobacterium ulcerans infection in mice with a combination of rifampin-streptomycin or rifampin-amikacin.
AID373036Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate BJ52 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID424322Antimicrobial activity against Dialister micraerophilus assessed as susceptibility breakpoint by CLSI method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID373941AUC (0 to 24 hrs) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model administered at dose simulating 600 mg/day for 7 days schedule2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID545599Bactericidal activity against stationary-phase methicillin-resistant Staphylococcus aureus ATCC 33591 grown on nutrient-depleted CAMHB medium at 2 ug/ml after 24 hrs by time kill analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID301527Antibacterial activity against rifamycin-resistance Staphylococcus aureus CB3722007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
AID372486Cmax in patient with severe malaria at 200 mg, perorally2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1399587Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 16995 after 7 days by microplate alamar blue assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and evaluation of oxime-functionalized nitrofuranylamides as novel antitubercular agents.
AID1235588Antimycobacterial activity against Mycobacterium avium complex isolate CIT19/06 assessed as reduction in bacterial growth incubated at 37 degC for 5 days by alamar blue dye based assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents.
AID577486Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315 assessed as inhibition of bacterial biofilm formation by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID571424Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method by Etest in presence of 4 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1205458Antitubercular activity against isoniazid, rifampin, streptomycin, ethambutol, amikacin, ofloxacin, kanamycin-susceptible Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID530633Antimicrobial activity against Staphylococcus aureus CB811 harboring quinolone-resistant gyrA S84L mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1516022Antibacterial activity against Escherichia coli UB1005 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1861192Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis assessed as mycobacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1334257Selectivity index, ratio of GI50 for human MCF7 cells to MIC90 for Mycobacterium bovis BCG ATCC 35743 dormant stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID530640Inhibition of DNA synthesis in Staphylococcus aureus CB190 assessed as decrease in [methyl-3H]thymidine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID571199Antibacterial activity against Escherichia coli ATCC 25992 in presence of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1602934Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 2 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID438558Cytotoxicity against african green monkey Vero cells after 72 hrs2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.
AID780281Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Inhibitory effect of oxygenated cholestan-3β-ol derivatives on the growth of Mycobacterium tuberculosis.
AID1061927Antimicrobial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and evaluation of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-(2-(4-substitutedpiperazin-1-yl)acetyl)piperazin-1-yl)quinoline-3-carboxylic acid derivatives as anti-tubercular and antibacterial agents.
AID1071099Bacteriostatic activity against Mycobacterium tuberculosis H37Rv SRI 1345 after 16 to 21 days2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID570582Apparent oral clearance in pulmonary tuberculosis patient in first order model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1436931Cytotoxicity against human A549 cells assessed as growth inhibition after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID1212155Induction of CYP2E1 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID373954Ratio of AUC to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L administered for 2 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID495751Antimicrobial activity against Escherichia coli J5 transconjugants expressing beta lactamase CTX-M-9 isolated from human flora associated C3H rat infected with Salmonella enterica serotype Virchow by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime.
AID285183Antimicrobial activity against methicillin-susceptible Staphylococcus aureus by time-kill methodology2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
AID588217FDA HLAED, serum glutamic pyruvic transaminase (SGPT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID1827063Antibacterial activity against Enterococcus faecium ATCC 6569 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID531129Antimicrobial activity against Staphylococcus aureus CB815 harboring rpoB H481Y, gyrA S48L and parC S80F mutant genes2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1476356n-Octanol/water partition coefficient, log P of the compound by HPLC analysis2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID293521Antimycobacterial activity against Mycobacterium bovis BCG at 1 ug/mL after 24 to 48 hrs by MABA2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Studies on acyclic pyrimidines as inhibitors of mycobacteria.
AID289133Antituberculosis activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2007Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17
Synthesis and structure-antituberculosis activity relationship of 1H-indole-2,3-dione derivatives.
AID515917Antibacterial activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID586056Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type 6 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID530770Antimicrobial activity against Clostridium difficile isolate 1 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID555292Antibacterial activity against methicillin-susceptible Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1585696Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID127813Tested in vitro for killing of Mycobacterium tuberculosis Erdman (ATCC 35801) in monolayers of mouse bone marrow macrophages and 90% reduction was reported using level 3 assay2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials.
AID581660Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU after 5 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID446151Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.
AID370261Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as reduction in viable lung bacterial count at 3.5 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID425618Cmax in fasted healthy human serum at 600 mg, po by high-pressure liquid chromatography2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID531029Antimicrobial activity against Clostridium difficile isolate 76 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID565184Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 grown as biofilms by microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Evaluation of analogs of reutericyclin as prospective candidates for treatment of staphylococcal skin infections.
AID765121Cytotoxicity against human A549 cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1869530Antibacterial activity against beta-lactamase-producing Morganella morganii ATCC25830 measured after 24 hrs by broth microdilution method
AID278578Decrease in Plasmodium falciparum FCK2 in erythrocytes at 5 uM after 84 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum.
AID1832326Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis ATCC 35838 harboring RpoBS531L mutant assessed as bacterial growth inhibition measured after 5 days by serial dilution method2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel C-3-(N-alkyl-aryl)-aminomethyl rifamycin SV derivatives exhibit activity against rifampicin-resistant Mycobacterium tuberculosis RpoB
AID1861191Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as mycobacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1071088Antimycobacterial activity against Mycobacterium tuberculosis H37Rv SRI 1345 infected in mouse J774A1 cells assessed as reduction in bacterial growth at 0.1 ug/ml after 7 days relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID700538Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 at 1 to 100 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID408876Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in J744 cells assessed as reduction in number of surviving bacteria at 0.25 ug/mL relative to control2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1053500Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID535820AUC (0 to 24 hrs) in guinea pig at 50 mg/kg2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Metronidazole lacks antibacterial activity in guinea pigs infected with Mycobacterium tuberculosis.
AID657783Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis H37Rv measured 24 hrs post dose by microplate alamar blue assay2012European journal of medicinal chemistry, Jun, Volume: 52Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
AID644320Antitubercular activity against Multidrug-resistant Mycobacterium tuberculosis after 7 days by resazurin assay2012European journal of medicinal chemistry, Mar, Volume: 49Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents.
AID1858572Cytotoxicity against mouse RAW264.7 cells2021European journal of medicinal chemistry, Jan-01, Volume: 209Lipolytic enzymes inhibitors: A new way for antibacterial drugs discovery.
AID428293Antimicrobial activity against Acinetobacter baumannii BM4651 expressing deltaadeIJK genes isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID559913Volume of distribution in patient with tuberculosis at 600 to 1200 mg/kg, po administered as single dose2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Population modeling and Monte Carlo simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of rifampin in lungs.
AID1543322Antimicrobial activity against Enterococcus faecalis ATCC 29212 assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution assay2019Journal of natural products, 07-26, Volume: 82, Issue:7
Antibacterial Salinaphthoquinones from a Strain of the Bacterium
AID767543Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 assessed as growth inhibition at 1 to 100 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID489575Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 21 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID774293Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS-PMS assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID1866096Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth in presence of middlebrook 7H9/BSAADN//tyloxapol/glycerol medium measured for 1 week by resazurin based colorimetric assay2022European journal of medicinal chemistry, Feb-15, Volume: 230A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen).
AID1624149Antitubercular activity against isoniazid/ethionamide resistant Mycobacterium tuberculosis isolate 1 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID445210Antituberculosis activity against Mycobacterium tuberculosis H37Rv by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID535769Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID1716662Antibacterial activity against Pseudomonas aeruginosa 750 harboring efflux mutant assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID444050Fraction unbound in human plasma2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1261247Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate Alamar Blue assay2015European journal of medicinal chemistry, Nov-02, Volume: 104Synthesis, antimycobacterial and antibacterial activity of fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety.
AID103680In vitro activity of compound against slowly growing Mycobacterium marinum 13901990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID669183Inhibition of Mycobacterium tuberculosis RNA polymerase S450L mutant by rolling circle transcription assay in the absence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1395692Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123 USA400 assessed as change in MIC after 1 serial passages by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID780896Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis 1896HF harboring inhA mutant after 7 days by REMA assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids.
AID1658984Antibacterial activity against Streptococcus pneumoniae ATCC 49619 assessed as reduction in pneumolysin release at 0.25 to 0.5 times MIC incubated for 16 to 20 hrs by Western blot analysis2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID444057Fraction escaping hepatic elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID400495Inhibition of AAH in Sprague-Dawley rat liver microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 0.05 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID463977Antitubercular activity against Mycobacterium tuberculosis H37Rv after 24 hrs by broth microdilution method2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
New 1,3-oxazolo[4,5-c]quinoline derivatives: synthesis and evaluation of antibacterial and antituberculosis properties.
AID678984TP_TRANSPORTER: RT-PCR in HepG2 cells2002Toxicology, Feb-28, Volume: 171, Issue:2-3
Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression.
AID1332967n-octanol-water partition coefficient, log P of the compound by HPLC method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID571452Ratio of the MIC for Enterobacter cloacae ATCC 23355 in the absence of NAB7061 to MIC for Enterobacter cloacae ATCC 23355 ATCC 13883 in the presence of 4 ug/ml of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID603129Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 24 hrs by tetrazolium microplate assay2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Dihydro-β-agarofuran sesquiterpenes isolated from Celastrus vulcanicola as potential anti-Mycobacterium tuberculosis multidrug-resistant agents.
AID1435638Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate Alamar blue assay2017European journal of medicinal chemistry, Jan-27, Volume: 126Synthesis, biological evaluation and in silico molecular modeling of pyrrolyl benzohydrazide derivatives as enoyl ACP reductase inhibitors.
AID1716872Antibacterial activity against Pseudomonas aeruginosa 114228 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1879523Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1893 harboring rpoBL525I/D530N/rdxAR16S mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID487843Antimycobacterial activity against Mycobacterium intracellular after 48 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID268913Antibacterial activity against Mycobacterium smegmatis2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID1566204Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harbouring DprE1 Y314S mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID574807Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 horboring rpoB S531L/Q510P, katG S315T/R463L, gyrA D94N/S95T, rrs G1484T by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID683318Antibacterial activity against Mycobacterium tuberculosis H37Rv by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID1603255Antibacterial activity against Mycobacterium tuberculosis H37Rv harboring LuxAB incubated for 10 days under anaerobic conditions followed by incubation under aerobic conditions for 28 hrs by LORA method
AID276757Antimycobacterial activity against rifampicin and rifabutin resistant Mycobacterium tuberculosis2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1484392Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by NCCLS method2017European journal of medicinal chemistry, Jun-16, Volume: 133Isoniazid derivatives and their anti-tubercular activity.
AID333073Cytotoxicity against african green monkey Vero cells2004Journal of natural products, Aug, Volume: 67, Issue:8
Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases.
AID531018Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 65 expressing RpoB H502N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID531026Antimicrobial activity against Clostridium difficile isolate 73 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID535773Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K carrying the luxAB gene under the hsp60 promoter agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID558269Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in intracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 2 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID404304Effect on human MRP2-mediated estradiol-17-beta-glucuronide transport in Sf9 cells inverted membrane vesicles relative to control2008Journal of medicinal chemistry, Jun-12, Volume: 51, Issue:11
Prediction and identification of drug interactions with the human ATP-binding cassette transporter multidrug-resistance associated protein 2 (MRP2; ABCC2).
AID1236138Antitubercular activity against Mycobacterium tuberculosis after 6 days by resazurin dye reduction method2015Journal of natural products, Aug-28, Volume: 78, Issue:8
Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity.
AID1565594Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID1055959Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis ATCC 35838 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID531056Antimicrobial activity against Clostridium difficile isolate 23 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID765273fCmax/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1209457Unbound Cmax in human plasma2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID1593908Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as complete inhibition of bacterial growth incubated for 7 days by rapid direct susceptibility test
AID1152758Antimycobacterial activity against wild-type Mycobacterium tuberculosis H37Rv ATCC 27294 after 16 to 18 days by BACTEC 7H12B microdilution method2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1355416Antimycobacterial activity against Mycobacterium tuberculosis ATCC 25177 after 5 days by Alamar blue based CLSI method2018Journal of natural products, 06-22, Volume: 81, Issue:6
Chloramphenicol Derivatives with Antibacterial Activity Identified by Functional Metagenomics.
AID1908115Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID1435844Antimycobacterial activity against Mycobacterium tuberculosis CDCT-4 (1105/09) clinical isolate after 7 days by resazurin reduction microplate assay2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID560507Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b2k3421 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID626869Inhibition of wild type Mycobacterium tuberculosis RNA polymerase after 10 mins using ribo green staining by rolling circle transcription assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID400496Inhibition of AAH in Sprague-Dawley rat liver microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 0.10 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID577207Antimicrobial activity against Escherichia coli C600::H19B in stationary phase encoding Stx-1 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID1423476Antibacterial activity against Klebsiella pneumoniae ATCC 13883 after 6 to 8 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1365695Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days under aerobic condition2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID285197Antimicrobial activity against Escherichia coli M083 mutant with AG100 lon4::IS186 acrR::IS1 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID292418Antitubercular activity against Mycobacterium tuberculosis SS82007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID369922Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected Swiss mouse assessed as spleen weight at 10 mg/kg after 12 days of infection weekly 5 times for 8 weeks2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID566905Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth in log phase by agar dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection.
AID1888722Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth after 5 days by MTT assay2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Antimycobacterial and anti-inflammatory activities of thiourea derivatives focusing on treatment approaches for severe pulmonary tuberculosis.
AID410027Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Dec-01, Volume: 18, Issue:23
Clubbed [1,2,3] triazoles by fluorine benzimidazole: a novel approach to H37Rv inhibitors as a potential treatment for tuberculosis.
AID425023Antimicrobial activity against Mycobacterium tuberculosis H37Ra by microplate alamar blue assay2009Journal of natural products, May-22, Volume: 72, Issue:5
Biomimetic transformation and biological activities of Globiferin, a terpenoid benzoquinone from Cordia globifera.
AID565229Antimicrobial activity against Mycobacterium chelonae ATCC 35752 harboring pZS01 carrying mspA gene by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID1570244Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID509619Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB513 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID625489Antitubercular activity against rifampicin and isoniazid-resistant Mycobacterium tuberculosis isolate 2199 after 24 hrs by microplate alamar blue assay2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives.
AID1334259Selectivity index, ratio of GI50 for human HCT116 cells to MIC90 for Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1890842Antimycobacterial activity against wild type Mycobacterium smegmatis mc2 155 assessed as inhibition of mycobacterial growth incubated for 3 to 5 days by resazurin microtiter assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID400497Inhibition of AAH in Sprague-Dawley rat liver microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 0.50 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1423475Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC BAA-44 after 6 to 8 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID345803Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 4 days by microplate alamar blue assay2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.
AID1202017Bactericidal activity against Mycobacterium tuberculosis H37Rv infected in Swiss mouse assessed as microbial killing by measuring colony forming units dosed orally daily for 28 days (Rvb = 4800 CFU)2015European journal of medicinal chemistry, May-05, Volume: 95Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis.
AID290254Cytotoxicity against Vero cells after 72 hrs by MTT assay2007Bioorganic & medicinal chemistry letters, Apr-01, Volume: 17, Issue:7
N-Hydroxythiosemicarbazones: synthesis and in vitro antitubercular activity.
AID531020Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 67 expressing RpoB H502N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1626624Antimicrobial activity against methicillin-sensitive Staphylococcus epidermidis clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID555295Antibacterial activity against Tmp-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1215086Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID405624Inhibition of linezolid-induced hematological events in orthopedic implant infection patient assessed as reduction of anemia incidence relative to control2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID523653Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID561165Cmax in in vitro pharmacokinetic/pharmacodynamic model at 30 mg for every 8 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID577208Antimicrobial activity against Escherichia coli C600::H19B in logarithmic phase encoding Stx-1 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID1070199Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis MTB2556 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID530762Induction of PsgtB::lacZ gene expression in Staphylococcus aureus SH1000 at 0.05 ug/ml after 2 hrs by beta-galactosidase reporter gene assay relative to untreated control2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
AID373797fCmax in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 4200 mg, po administered once a week2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1459061Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis ATCC 35828 after 5 days2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
AID531135Antimicrobial activity against Staphylococcus aureus CB1954 harboring rpoB H481Y, gyrA S84L, K809 deficient gyrA, parC S80F, parC A523D mutant genes selected after CBR-2092 exposure for 7 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID511116T>MIC in Acinetobacter baumannii infected C57BL/6 mouse pneumonia model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1626626Antimicrobial activity against Streptococcus pyogenes clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1539493Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123-USA400 clinical isolates assessed as ratio of MIC after and before 13 serial passages by broth microdilution assay
AID380458Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID395772Antibacterial activity against Klebsiella pneumoniae isolate containing extended spectrum beta lactamase after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID558272Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 2 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID717305Antitubercular activity against streptomycin, isoniazid, rifampicin,ethambutol-resistant Mycobacterium tuberculosis clinical isolate assessed as reduction in RLU at 2 ug/mL after 72 hrs by luciferase reporter phage assay2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Microwave-assisted synthesis, molecular docking and antitubercular activity of 1,2,3,4-tetrahydropyrimidine-5-carbonitrile derivatives.
AID144736In vitro inhibition of Mycobacterium tuberculosis H37Rv, determined at 20 ug/mL2004Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
AID1143688Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in spleen at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 62014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
AID1557231Antitubercular activity against resistant Mycobacterium tuberculosis 4 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID565231Antimicrobial activity against Mycobacterium chelonae 9917 harboring pZS01 carrying mspA gene by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID1399857Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv harboring katG Y155 mutant2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID370103Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po after 4 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1399135Lipophilicity, log P of the compound2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
A novel synthesis of 2-arylbenzimidazoles in molecular sieves-MeOH system and their antitubercular activity.
AID406612Terminal half life in albino guinea pig cage fluid at 3 mg/kg, ip administered as single dose2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID680552TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID419828Antibacterial activity against Escherichia coli MTCC 722 at 1000 ug/ml after 24 hrs by agar diffusion method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID1596896Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 incubated for 16 to 18 hrs by broth microdilution assay
AID529535Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 5310 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1212118Induction of CYP2A6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID373025Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PU73 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID564978Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring inactivated p55 gene by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID424319Antimicrobial activity against Dialister pneumosintes by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID561168AUC (0 to 24 hrs) in in vitro pharmacokinetic/pharmacodynamic model at 30 mg for every 8 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID103691In vitro activity of compound against slowly growing Mycobacterium marinum 14471990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID534111Antibacterial activity against Pasteurella multocida pm1980 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1372625Inhibition of recombinant Bacillus subtilis subsp. subtilis 168 N-terminal His-tagged glutamate racemase expressed in Escherichia coli BL21(DE3) using D-glutamate as substrate in presence of NAD+ by spectrophotometric based L-glutamate dehydrogenase enzym2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1627828Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution assay2016Bioorganic & medicinal chemistry letters, 09-01, Volume: 26, Issue:17
A convenient synthesis and screening of benzosuberone bearing 1,2,3-triazoles against Mycobacterium tuberculosis.
AID1467478Antibacterial activity against methicillin resistant Staphylococcus aureus MRSA090 incubated for overnight by microdilution method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID1765577Antibacterial activity against Escherichia coli ATCC 25922 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID1158103Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in macrophages2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.
AID1296384Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 9449/2007 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID494492Antituberculosis activity against multi drug-resistant Mycobacterium tuberculosis after 7 days using resazurin dye by broth microdilution assay2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
New quinoline derivatives: synthesis and investigation of antibacterial and antituberculosis properties.
AID1311225Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID562792Antimicrobial activity against Chlamydophila caviae GPIC/rifR harboring rpoB gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1348985Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 days by rapid direct susceptibility test
AID1311271Antimycobacterial activity against active stage of Mycobacterium bovis BCG ATCC 35734 measured on day 8 by nitrate reductase assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID509516Antitubercular activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse lung at 25 mg/kg, iv after 6 weeks2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs.
AID1471055Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium bovis BCG ATCC 35743 dormant stage2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1209535Activation of human PXR expressed in human HepG2 cells coexpressing CYP3A4 at 10 uM after 24 hrs by dual luciferase reporter gene assay relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID368641Cmax in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID400500Inhibition of AAH in Sprague-Dawley rat intestine microsomes using benzo(a)pyrene as substrate by non-competitive assay relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID202116Inhibitory concentration of compound against Streptococcus pyogenus septicemia in the mouse, administarted in OS route1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID586233Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 6 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID395773Antibacterial activity against Klebsiella pneumoniae RSHM 574 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID409950Inhibition of human brain MAOA2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Quantitative structure-activity relationship and complex network approach to monoamine oxidase A and B inhibitors.
AID624606Specific activity of expressed human recombinant UGT1A12000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID588127Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 5 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID428623Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents.
AID1516029Antibacterial activity against Staphylococcus aureus 11011 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1400051Antibacterial activity against Streptococcus pneumoniae ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1488560Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis 09710 by two fold dilution method
AID1491506Antimycobacterial activity against Mycobacterium tuberculosis H37Ra Lehmann and Neumann ATCC 25177 harboring pSMT1 luciferase reporter after 6 days by luminescence based serial dilution method2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID557091Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 4% human serum albumin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID283237Reduction of bacterial counts in Mycobacterium tuberculosis H37Rv infected Swiss mouse lung at 10 mg/kg, po for 5 days/week after 1 month2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID40798Minimum inhibitory concentration required against Bacillus subtilis ATCC 142892003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Tethered dimers as NAD synthetase inhibitors with antibacterial activity.
AID531039Antimicrobial activity against Clostridium difficile isolate 6 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1077008Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 2 to 3 weeks by broth microdilution assay2014European journal of medicinal chemistry, Apr-09, Volume: 76Sulfur rich 2-mercaptobenzothiazole and 1,2,3-triazole conjugates as novel antitubercular agents.
AID1879571Antibacterial activity against Prevotella bivia MMX 34502022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1890844Antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC::PDFMtb overexpression mutant assessed as inhibition of mycobacterial growth incubated for 3 to 5 days by resazurin microtiter assay2022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID543794Antimicrobial activity against Klebsiella pneumoniae VT 1367 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID581061Induction of iNOS expression in human A549 cells at 25 to 50 ug/ml by Western blot analysis in presence of IFN-gamma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID442524Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Synthesis and antimicrobial activity evaluation of new 1,2,4-triazoles and 1,3,4-thiadiazoles bearing imidazo[2,1-b]thiazole moiety.
AID348180Antimycobacterial activity against non-replicating Mycobacterium tuberculosis assessed as colony forming unit after 8 days2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID1185721Octanol-water partition coefficient, log P of the compound2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1333266Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 4 times MIC measured after 1 hr by luciferase reporter gene assay (Rvb = 90.6%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID369452Ratio of MBC for Staphylococcus epidermidis to MIC for Staphylococcus epidermidis2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activities of different inhibitors of bacterial transcription against Staphylococcus epidermidis biofilm.
AID404132Antibacterial activity against methicillin-resistant Staphylococcus aureus COL MB53932005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID408875Antimycobacterial activity against Mycobacterium tuberculosis 1034712008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID481980Antimycobacterial activity against Mycobacterium tuberculosis Erdman infected in BALB/c mouse assessed as reduction of bacterial load at 10 mg/kg, po qd for 5 days per week administered 60 days after infection measured after 85 days post infection relativ2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Structure-activity relationship of new anti-tuberculosis agents derived from oxazoline and oxazole benzyl esters.
AID69990The compound is evaluated for inhibitory concentration against Escherichia coli and is expressed as minimum inhibitory concentration (MIC).1998Journal of medicinal chemistry, Jun-18, Volume: 41, Issue:13
Comprehensive study on structure-activity relationships of rifamycins: discussion of molecular and crystal structure and spectroscopic and thermochemical properties of rifamycin O.
AID362871Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and antituberculosis activity of new thiazolylhydrazone derivatives.
AID531263Antimicrobial activity against Clostridium difficile isolate 35 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1327575Cytotoxicity against human LS180 cells assessed as effect on cell viability at 50 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID1261214Bacteriostatic activity against Staphylococcus aureus Mu50 after 24 hrs2015Bioorganic & medicinal chemistry, Nov-01, Volume: 23, Issue:21
Evaluation of small molecule SecA inhibitors against methicillin-resistant Staphylococcus aureus.
AID1294363Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 assessed as inhibition of visual growth after 18 to 24 hrs2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID1853627Inhibition of RNA synthesis in Staphylococcus aureus ATCC 29213 at 8 times MIC preincubated for 30 mins followed by [3H]-uridine and measured after 30 mins by [3H]-uridine incorporation based beta scintillation counter analysis2021RSC medicinal chemistry, Oct-20, Volume: 12, Issue:10
Design, synthesis, and antibacterial activity of
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID571429Antibacterial activity against Pseudomonas aeruginosa ATCC 27853by Etest method in presence of 1 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID623579Antimicrobial activity against Mycobacterium diernhoferi ATCC 19340 after 5 days by microbroth dilution antibiotic susceptibility assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
One-pot syntheses of pseudopteroxazoles from pseudopterosins: a rapid route to non-natural congeners with improved antimicrobial activity.
AID1287503Antitubercular activity against dormant state Mycobacterium bovis BCG ATCC 35734 assessed as viable cells after 12 days by nitrate reductase assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID495749Antimicrobial activity against Salmonella enterica serotype Virchow 3464b by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime.
AID565805Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB27 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1879563Antibacterial activity against Mobiluncus curtisii subsp. curtisii ATCC 352412022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1916605Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in relative light units at 2 ug/ml incubated for 4 hrs followed by addition of D-luciferin by luciferase based luminometer analysis relative to control2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID355992Cytotoxicity against african green monkey Vero cells2003Journal of natural products, Jun, Volume: 66, Issue:6
New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge.
AID1888131Antimycobacterial activity against Mycobacterium bovis BCG assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID326292Antibacterial activity against methicillin-resistant Staphylococcus aureus 4930 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID681594TP_TRANSPORTER: transepithelial transport in OATP1B3/MRP2 double transfectant (MDCKII)2001Molecular pharmacology, Nov, Volume: 60, Issue:5
Vectorial transport by double-transfected cells expressing the human uptake transporter SLC21A8 and the apical export pump ABCC2.
AID373973AUC in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 14 mg/L for 0.5 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1220557Fraction unbound in Hartley guinea pig brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1348988Selectivity index, ratio of CC50 against African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv
AID1594637Antimycobacterial activity against Mycobacterium tuberculosis assessed as inhibition of parasite growth at 1 ug/ml incubated for 6 days by REMA method relative to untreated control2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID1181177Inhibition of Mycobacterium tuberculosis InhA using NADH and dodecyl coA substrate by LC-MS/MS method2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1236140Cytotoxicity against human MRC5 cells assessed as cell growth inhibition after 48 hrs by resazurin dye reduction method2015Journal of natural products, Aug-28, Volume: 78, Issue:8
Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity.
AID1071092Antimycobacterial activity against Mycobacterium tuberculosis H37Rv SRI 1345 incubated for 7 days under anaerobic condition measured after 7 days of recovery under gaseous condition by low oxygen recovery assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID555300Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID489574Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 14 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID561166Cmin in in vitro pharmacokinetic/pharmacodynamic model at 30 mg for every 8 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID1384037Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2018European journal of medicinal chemistry, Apr-25, Volume: 150Recent advances of imidazole-containing derivatives as anti-tubercular agents.
AID1597875Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis measured after 7 days by resazurin microtiter assay
AID289153Cytotoxicity against Vero cells2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID1179477Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by CellTiter 96 assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID1542207Antimicrobial activity against Staphylococcus aureus ATCC 6538 incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID1596876Antibacterial activity against Acinetobacter baumannii BAA1605 incubated for 16 to 18 hrs by broth microdilution assay
AID326283Antibacterial activity against methicillin-resistant Staphylococcus aureus 5098 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID535775Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID1879570Antibacterial activity against Prevotella bivia ATCC 29303/MMX 57182022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID563698Antibacterial activity against pyrazinamide-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID678715Inhibition of human CYP2D6 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 4-methylaminoethyl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1594310Antitubercular activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 after 12 days by XRMA2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID283171Decrease in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1326672Growth inhibition of mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID495514Antibacterial activity against multidrug-resistant Acinetobacter baumannii BM4668 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID588124Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 2 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID102997In vitro activity of compound against rapidly growing Mycobacterium phlei 12831990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID558254Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in intracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered 2 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1384565Inhibition of GSTO1-1 (unknown origin) by enzymatic assay2018Journal of medicinal chemistry, 09-13, Volume: 61, Issue:17
Reviewing Hit Discovery Literature for Difficult Targets: Glutathione Transferase Omega-1 as an Example.
AID1272451Cytotoxicity against African green monkey Vero cells by MTS assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes.
AID1483721Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit a K179N mutant supplemented with 8 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1276381Selectivity index, ratio of GI50 for human A431 cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID1337837Growth inhibition of Mycobacterium bovis BCG ATCC 35743 at active stage measured after 8 days by nitrate reductase dye based two fold dilution method2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID489573Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 21 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID531032Antimicrobial activity against Clostridium difficile isolate 79 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID572150Antimicrobial activity against AcrAB-deficient Escherichia coli AG100AX harboring pBAD plasmid after 18 to 24 hrs by two fold dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
AID475038Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
New 3-methylquinoxaline-2-carboxamide 1,4-di-N-oxide derivatives as anti-Mycobacterium tuberculosis agents.
AID442657Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
AID700529Antimycobacterial activity against Mycobacterium smegmatis ATCC 19420 at 0.3125 to 5 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID1772303Non-covalent inhibition of DprE1 in multidrug-resistant Mycobacterium tuberculosis clinical isolate 14862 measured after 7 days by microplate Alamar blue assay
AID1589012Cytotoxicity in African green monkey Vero cells
AID555298Antibacterial activity against Tmp-susceptible coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID571655Ratio of the MIC for Klebsiella oxytoca ATCC 13182 in the absence of NAB7065 to MIC for Klebsiella oxytoca ATCC 13182 in the presence of 4 ug/ml of NAB70652008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID103847In vitro activity of compound against rapidly growing Mycobacterium smegmatis 311990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1477416Antibacterial activity against wild type Mycobacterium tuberculosis H37Rv grown in GAST/Fe medium measured on day 14 post inoculation by broth microdilution method2017Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
AID495748Antimicrobial activity against Escherichia coli ATCC 25922 by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime.
AID1435649Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 4 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1436932Cytotoxicity against human HCT116 cells assessed as growth inhibition after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID374185Antimicrobial activity against 3 weeks old culture of Mycobacterium tuberculosis H37Ra assessed as colony forming unit in aerobic condition at 2 ug/ml for 3 hrs2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pyrrolidine dithiocarbamate and diethyldithiocarbamate are active against growing and nongrowing persister Mycobacterium tuberculosis.
AID425629Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as effect on average time to detection of growth at 10'5 CFU of inoculum by MGIT 960 susceptibility test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID531030Antimicrobial activity against Clostridium difficile isolate 77 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1827050Antibacterial activity against Providencia alcalifaciens ATCC 9886 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID533660Antimicrobial activity against Staphylococcus aureus RN4220 harboring plasmid VGA2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID531117Antimicrobial activity against Staphylococcus aureus CB370 harboring rpoB H481Y mutant gene2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID373948Ratio of AUC to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 2 mg/L administered for 7 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID369924Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected Swiss mouse assessed as reduction of bacterial count in lungs at 10 mg/kg after 12 days of infection weekly 5 times for 8 weeks2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID1402132Antimycobacterial activity against Mycobacterium avium subsp. paratuberculosis CIT03 clinical isolate after 11 days by Alamar Blue assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Primaquine hybrids as promising antimycobacterial and antimalarial agents.
AID1727217Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as percentage inhibition at 250 ug/ml measured after 2 to 4 weeks by Lowensteine-Jensen method relative to control2021European journal of medicinal chemistry, Jan-01, Volume: 209Anti-tuberculosis activity and its structure-activity relationship (SAR) studies of oxadiazole derivatives: A key review.
AID1311224Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID445333Selectivity for Mycobacterium tuberculosis H37Rv over human A549 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID634281Antimycobacterial activity against Mycobacterium tuberculosis isolate 363 expressing rpoB Asp516Val mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID565802Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB5 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1597870Selectivity index, ratio of IC50 for mouse J774.A1 cells to MIC for Mycobacterium tuberculosis INH R2
AID572547AUC (0 to 12 hrs) in kenyan pulmonary tuberculosis patient coinjected with HIV with body weight <=45 kg at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID625281Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholelithiasis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1337873Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium bovis BCG ATCC 35743 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1781724Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as bacterial growth inhibition incubated for 16 to 18 hrs by broth microdilution method
AID1218865Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID1784353Antimycobacterial activity against Mycobacterium tuberculosis H37RvMA in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID530655Inhibition of cell wall synthesis in rifamycin-resistant Staphylococcus aureus CB370 harboring rpoB H481Y mutant gene assessed as [2,3-3H]D-alanine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID388897Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 128 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID1658974Antibacterial activity against Streptococcus pyogenes ATCC 19615 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID532961Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 52010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID414454Antitubercular activity against rifampin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
AID424328Antimicrobial activity against Dialister invisus by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID370124Cmax in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1058231Antibacterial activity against Staphylococcus aureus ATCC 29213 by CLSI method2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID424616Antibacterial activity against Enterococcus avium AIS2007004 isolated from patients rectum by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID644317Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by resazurin assay2012European journal of medicinal chemistry, Mar, Volume: 49Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents.
AID396039Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pACYC184 plasmid by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID1544790Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth after 14 days by green fluorescent protein microplate assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones.
AID1491292Antitubercular activity against rifampin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 after 7 days under normoxic condition by microplate Alamar blue assay2017European journal of medicinal chemistry, Sep-08, Volume: 137QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity.
AID1626615Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y and gyrA S84L mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID520289Antimicrobial activity against Staphylococcus aureus 25462008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Activities of daptomycin and comparative antimicrobials, singly and in combination, against extracellular and intracellular Staphylococcus aureus and its stable small-colony variant in human monocyte-derived macrophages and in broth.
AID1337863Selectivity index, ratio of GI50 for HUVEC to MIC for Mycobacterium bovis BCG ATCC 35743 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID425404Antibacterial activity against Escherichia coli isolate HM95 isolated from ileal mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1232407Cytotoxicity against mouse RAW264.7 cells2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides.
AID438477Selectivity index, ratio of IC50 for Vero cells to IC50 for Mycobacterium tuberculosis H37Rv by Alamar blue susceptibility assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters.
AID103654In vitro activity compound against rapidly growing Mycobacterium fortuitum 14401990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID326296Antibacterial activity against methicillin-resistant Staphylococcus aureus 4875 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID495237Antimicrobial activity against Mycobacterium tuberculosis NJT210TGC harboring embB406 GGC-TGC(Gly-Cys) mutation in embB gene after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID1296385Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 8666/2010 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID557093Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID143698Antimycobacterial activity against Mycobacterium avium NIHJ16052003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.
AID1296402Cytotoxicity against human HuH7 cells assessed as cell viability at 20 uM after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1908123Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID1668172Inhibition of Escherichia coli RNA polymerase2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID605758Agonist activity at human SXR transfected in human HepG2 cells coexpressing GAL4 assessed as activation of receptor-mediated CYP3A4 gene transcription at 1 X 10'-6 M after 48 hrs by luciferase reporter gene assay2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Synthesis of novel vitamin K2 analogues with modification at the ω-terminal position and their biological evaluation as potent steroid and xenobiotic receptor (SXR) agonists.
AID1334248Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage measured on day 12 by XTT reduction menadione based two-fold dilution assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID544829Antimicrobial activity against Staphylococcus epidermidis Xen 43 biofilm assessed as log10 CFU/cm'2 in bacterial count in presence of 2000 microamperes of electric current by bioelectric effect assay2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID1476359Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in presence of 4% fetal bovine serum2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1557236Antitubercular activity against resistant Mycobacterium tuberculosis 26 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID531289Antimicrobial activity against Clostridium difficile isolate 61 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID324989Antibacterial activity against rifampin-resistant Haemophilus influenzae RdRIF by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID530635Antimicrobial activity against Staphylococcus aureus CB814 harboring fluoroquinolone-resistant gyrA S84L and parC S80F mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID265978Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID103857In vitro activity of compound against slowly growing Mycobacterium xenopi 5561990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1634268Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at <3 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID634039Antituberculosis activity against drug-sensitive Mycobacterium tuberculosis isolate Spec. 210 by twofold serial dilution method2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis of novel 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds and their evaluation for tuberculostatic activity.
AID405623Inhibition of linezolid-induced hematological events in orthopedic implant infection patient assessed as thrombocytopenia incidence relative to control2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Comparative study of the effects of pyridoxine, rifampin, and renal function on hematological adverse events induced by linezolid.
AID689773Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiterGlo assay2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis.
AID1205588Antibacterial activity against Haemophilus influenzae acrB by broth microdilution method2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1070193Antimycobacterial activity against Mycobacterium fortuitum MNT1073 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1337840Growth inhibition of Mycobacterium tuberculosis H37Ra ATCC 25177 at active stage measured after 8 days by XTT dye based two fold dilution method2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID562239Antimycobacterial activity against Mycobacterium smegmatis by GFP-based fluorescence assay2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID1497867Antibacterial activity against Proteus vulgaris PTCC 11822018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID1634263Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 12.5 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID529531Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-CTG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1897848Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in human A-THP1 macrophages assessed as viability of infected macrophages incubated for 96 hrs by fluorescence microplate assay
AID1827075Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in human THP-1 cells assessed as log reduction in bacterial growth at 10 uM incubated for 3 to 4 weeks by intracellular killing assay2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID313249Antimicrobial activity against Mycobacterium smegmatis2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID355991Antileishmanial activity against Leishmania donovani promastigotes expressing luciferase2003Journal of natural products, Jun, Volume: 66, Issue:6
New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge.
AID408870Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID545044Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ078 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID571393Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 1 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1193921Inhibition of Mycobacterium smegmatis DNA GyrB domain assessed as inhibition of inorganic phosphate release after 100 mins at room temperature by ATPase assay2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID1427056Selectivity index, ratio of GI50 for human A549 cells to MIC for active stage of Mycobacterium tuberculosis H37Ra ATCC 251772017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID571661Ratio of the MIC for Acinetobacter baumannii in the absence of NAB7071 to MIC for Acinetobacter baumannii in the presence of 4 ug/ml of NAB70712008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID565803Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB9 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID396037Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate in presence of 20 ug/ml efflux pump inhibitor Phe-Arg-beta-naphthylamide by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID1666553Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth by measuring calculated MIC90 measured after 14 days by green fluorescent protein based microplate assay2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Synthesis and biological evaluation of bis-N
AID545054Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ390 from patient secretion by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID545924Antimicrobial activity against Klebsiella pneumoniae ATCC 13883 by Etest method in presence of 2 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1164294Antimicrobial activity against Mycobacterium tuberculosis assessed as growth inhibition after 5 days by microdilution method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1399856Antitubercular activity against fluoroquinolone-resistant Mycobacterium tuberculosis H37Rv harboring gyrA D94N mutant2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID1326098Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay
AID1242343Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase assessed as supercoiling of pBR322 DNA after 90 mins by agarose gel electrophoresis method2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID1887586Synergistic antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 24 hrs in presence of artocarpin by checkerboard method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID611494Antibacterial activity against epidemic methicillin-resistant Staphylococcus aureus isolate 16 isolated from patient graft wound after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID694231Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic condition by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID510533Oral bioavailability in tuberculosis patient at 10 mg/kg by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1181078Antibacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate Alamar Blue assay2014Journal of natural products, Jul-25, Volume: 77, Issue:7
NRPS substrate promiscuity leads to more potent antitubercular sansanmycin analogues.
AID400498Inhibition of AAH in Sprague-Dawley rat liver microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 1 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1879501Antibacterial activity against Helicobacter pylori ATCC 700392 at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID207982Minimum inhibitory concentration of compound tested for antibacterial activity against Staphylococcus aureus 209 P(FDA)1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antibacterial activity of some ester, amides, and hydrazides of 3-carboxyrifamycin S. Relationship between structure and activity of ansamycins.
AID694200Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing GFP after 7 days by reporter gene assay2012Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
Design and synthesis of 1H-1,2,3-triazoles derived from econazole as antitubercular agents.
AID1653413Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by BACTEC radiometric growth assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1326389Antibacterial activity against Bacillus subtilis P10B derived after 10 passage in presence of JBIR-100 after 16 to 18 hrs by microbroth dilution assay relative to Bacillus subtilis ATCC 470962016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
AID776898Inhibition of Escherichia coli RNA polymerase core enzyme by transcription assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID1556522Induction of constitutive - androstane receptor in human primary hepatocytes assessed as upregulation of CYP2B6 protein expression at 10 uM after 72 hrs by Western blot analysis2019European journal of medicinal chemistry, Oct-01, Volume: 179Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.
AID530773Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 4 expressing RpoB S488T and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID563695Antibacterial activity against rifampin-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID634274Antimycobacterial activity against Mycobacterium tuberculosis isolate 361 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1334264Selectivity index, ratio of GI50 for human THP1 cells to MIC90 for Mycobacterium bovis BCG ATCC 35743 active stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID545922Antimicrobial activity against in Escherichia coli IH3080 in presence of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID368648Cmax in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID510530Apparent volume of distribution in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID511009AUC in C57BL/6 mouse pneumonia model at 25 mg/kg, ip2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID510982Antimicrobial activity against Acinetobacter baumannii 9402010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1626609Antimicrobial activity against Staphylococcus aureus isogenic forms expressing gyrA S84L and parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1762627Antibacterial activity against Enterococcus faecium ATCC 51559 by CLSI based microplate assay
AID103667In vitro activity of compound against slowly growing Mycobacterium gordonae 12941990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1634256Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 1.56 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID292417Antitubercular activity against Mycobacterium tuberculosis SS72007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID285160Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID531256Antimicrobial activity against Clostridium difficile isolate 28 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1334250Antitubercular activity against Mycobacterium bovis BCG ATCC 35743 dormant stage measured on day 12 by nitrate reductase based two-fold dilution assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1819097Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 4 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID531011Antimicrobial activity against Clostridium difficile isolate 58 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID408878Antimycobacterial activity against Mycobacterium smegmatis CIP 1035992008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1223078Induction of Ugt1a7c gene expression in PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1427055Selectivity index, ratio of GI50 for human A549 cells to MIC for active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID574788Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 obtained from sputum of patient at 1 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1197134Plasma protein binding in human by equilibrium dialysis assay2015Journal of medicinal chemistry, Feb-12, Volume: 58, Issue:3
Structure-activity relationship for the oxadiazole class of antibiotics.
AID530869Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB A477V mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID145297Tested for antibacterial activity against Mycobacterium tuberculosis H37Rv streptomycin resistant strain1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID560520Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate sh07043 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1191016Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 assessed as reduction in bacterial growth incubated for 6 days by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1294364Ratio of MBC for Mycobacterium tuberculosis H37Rv SRI 1345 to MIC for Mycobacterium tuberculosis H37Rv SRI 13452016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID461171Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate Alamar blue assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
AID562790Antimicrobial activity against Chlamydia trachomatis J/6276/tetR harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID624612Specific activity of expressed human recombinant UGT1A92000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID1759475Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16833 clinical isolate incubated for 7 days by microplate alamar blue assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis.
AID439871Cytotoxicity against african green monkey Vero cells after 72 hrs2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.
AID541817Antibacterial activity against wild-type Bacillus subtilis 168 after 15 hrs2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Inactivation of KsgA, a 16S rRNA methyltransferase, causes vigorous emergence of mutants with high-level kasugamycin resistance.
AID1917332Cytotoxicity against mouse J774.A1 cells after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.
AID1552792Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial cell growth incubated for 8 days measured under aerobic MABA conditions by alamar blue staining based assay2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents.
AID1847062Inhibition of recombinant Mycobacterium tuberculosis MurE expressed in Escherichia coli BL21(DE3) cells using UDP-MurNAc-dipeptide as substrate incubated for 30 mins by phosphate release based colorimetric assay2021European journal of medicinal chemistry, Oct-15, Volume: 222The Mur Enzymes Chink in the Armour of Mycobacterium tuberculosis cell wall.
AID1311244Antibacterial activity against Escherichia coli 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1463958Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 131 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID285191Antimicrobial activity against Escherichia coli M013 mutant with AG100 delta-(lon-hupB-ppiD) dupIS5 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID541819Antibacterial activity against Bacillus subtilis RIK543 after 15 hrs2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Inactivation of KsgA, a 16S rRNA methyltransferase, causes vigorous emergence of mutants with high-level kasugamycin resistance.
AID554577Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 200 mg/kg, sc administered as single dose 2 hrs after infection measured between 4 to 19 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID201407In vitro antibacterial activity of compound against Staphylococcus aureus Tour L 1651990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID340859Antimicrobial activity against vancomycin-intermediate resistant Staphylococcus aureus Mu50 graR mutant microdilution assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus.
AID405151Apparent volume of distribution in tuberculosis patient at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID388900Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 16 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID694232Antibacterial activity against Mycobacterium tuberculosis H37Rv by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID683316Antibacterial activity against Enterococcus faecalis ATCC 29212 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID144296In vitro antibacterial activity against Mycobacterium marinum 64231999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID1336648Induction of membrane damage in methicillin-resistant Staphylococcus aureus USA300 measured for 90 mins by propidium iodide staining based fluorescence spectroscopic analysis2017Bioorganic & medicinal chemistry, 02-01, Volume: 25, Issue:3
Small molecule mimics of DFTamP1, a database designed anti-Staphylococcal peptide.
AID510978Antibacterial activity against Acinetobacter baumannii infected in C57BL/6 mouse model assessed as survival rate at total dose of 100 mg/kg/day, ip administered as four divided doses measured after 72 hrs post last dose2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID536144Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by agar microdilution method2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Design, synthesis and in vitro evaluation of antitubercular and antimicrobial activity of some novel pyranopyrimidines.
AID563690Antibacterial activity against Mycobacterium tuberculosis H37Ra by by 7H9 broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID309398Antitubercular activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Synthesis and antitubercular activity of lipophilic moxifloxacin and gatifloxacin derivatives.
AID1624150Antitubercular activity against isoniazid/ethionamide resistant Mycobacterium tuberculosis isolate 2 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID401740Cytotoxicity against african green monkey Vero cells1998Journal of natural products, Jul, Volume: 61, Issue:7
A new antitubercular mulinane diterpenoid from Azorella madreporica Clos.
AID645551Antimicrobial activity against Mycobacterium tuberculosis H37Rv by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1395972Antibacterial activity against methicillin-resistant Staphylococcus aureus 2 after 16 to 18 hrs by broth microdilution method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID1739762Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of luminescence incubated for 10 days under anaerobic condition followed by incubated for 28 hrs under aerobic condition by low oxygen recovery assay relative to co2020European journal of medicinal chemistry, Sep-01, Volume: 201Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
AID1205462Antitubercular activity against rifampin, isoniazid and ethambutol-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID1627517Antitubercular activity against Mycobacterium tuberculosis H37Rv RIF-R2 ATCC 35828 after 5 days2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID164397Antimicrobial activity derived as minimum inhibitory concentration are determined using brain-heart infusion medium against Pseudomonas aeruginosa ATCC 101451985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID1215095Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay relative to SR128132011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1321806Induction of CYP3A4 expression in human primary hepatocytes at 10 uM incubated for 48 hrs by RT-PCR method
AID278865Increase in lactate production in primary human osteoblasts at 400 ug/ml by ELISA relative to control2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID206394Compound was tested for photoinhibition of Staphylococcus aureus(CIP 53156); Sensitive1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Nitroglycosylated meso-arylporphyrins as photoinhibitors of gram positive bacteria.
AID533663Antimicrobial activity against Staphylococcus aureus RN10242008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID1909951Antibacterial activity against Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph assessed as inhibition of bacterial growth incubated for 11 days2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1634248Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 800 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID586051Antimicrobial activity against Staphylococcus aureus clone 4-4 harboring staphylococcal cassette chromosome mec element type 1 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID671442Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of microbial growth at 0.5 ug/ml incubated for 6 days by MABA method2012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors.
AID1293907Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1765354Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID1879499Antibacterial activity against rifampicin-resistant Clostridioides difficile harboring rpoBQ489K mutant2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID529160Antibacterial activity against Pseudomonas aeruginosa 100609 after 20 hrs by broth microdilution assay in presence of 250 ug/ml polyethylenimine2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID449208Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID1765586Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 incubated for 18 hrs in presence of EDTA by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID545042Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ043 from patient abdominal drainage by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID580321Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by tetrazolium microplate assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents.
AID580619Inhibition of cell wall synthesis in Bacillus subtilis BD54 at 5 X MIC by N-acetyl-D-[1-3H] glucosamine incorporation assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.
AID1471028Growth inhibition of Mycobacterium bovis BCG ATCC 35743 at 30 ug/ml by nitrate reductase based two-fold dilution assay relative to control2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1626594Inhibition of RIF-resistant Staphylococcus aureus RNA polymerase RpoB H481Y mutant assessed as reduction in RNA product formation2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1311277Cytotoxicity against human PANC1 cells by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1707750Bactericidal activity against Mycobacterium tuberculosis H37Rv assessed as reduction in CFU grown under middlebrook 7H9/OADC-Glycerol-Tween80 medium at 1 to 2 times MIC incubated for 7 days2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
Antitubercular 2-Pyrazolylpyrimidinones: Structure-Activity Relationship and Mode-of-Action Studies.
AID1577337Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 7357/1998 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID543797Antimicrobial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1869559Antibacterial activity against Mycobacterium phlei DSM 43239 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1706863Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID1210906Intrinsic clearance in human Liver microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID1879529Antibacterial activity against Clostridioides difficile CB1921 ATCC BAA1382 at 1:1 compound to metronidazole molar ratio measured after 3 days in presence of metronidazole2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID531054Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 21 expressing RpoB H502N and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID700531Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID574808Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 horboring rpoB S531L, katG R463L/E217G, gyrA D94N/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID586039Antimicrobial activity against Staphylococcus aureus clone 1-1 harboring staphylococcal cassette chromosome mec element type 4 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID518798Antimycobacterial activity against Mycobacterium kansasii after 7 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1473740Inhibition of human MRP3 overexpressed in Sf9 insect cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 10 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1174111Antimycobacterial activity against isoniazid, rifampin, ethambutol-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1185146Antimicrobial activity against moxicillin resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase G88N mutant2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID1516020Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID373946Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 2517 infected in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as microbial killing administered at simulated dose of 600 mg/day for 2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID767541Antimycobacterial activity against Mycobacterium smegmatis ATCC 19420 assessed as growth inhibition at 0.3125 to 5 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID1688199Antimycobacterial activity against dormant form of Mycobacterium tuberculosis H37Rv assessed as log fold reduction in bacterial count at 10 ug/ml under nutrient starvation condition after 7 days by MPN assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.
AID292415Antitubercular activity against Mycobacterium tuberculosis SS52007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID1593373Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in drug-susceptible Mycobacterium tuberculosis V4207 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID541070Tmax in cage fluid of Albino guiena pig at 12.5 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID569261Antimicrobial activity against methicillin-resistant Staphylococcus aureus 8732011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID398476Inhibition of protein synthesis in Bacillus subtilis assessed as [3H]amino acid uptake at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2003Journal of natural products, Feb, Volume: 66, Issue:2
Antibacterial diterpenes from Calceolaria pinifolia.
AID541090Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 during stationary growth phase by macrodilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1869573Antibacterial activity against Pseudomonas aeruginosa DSM 19880 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID395774Antibacterial activity against gentamicin-resistant Pseudomonas aeruginosa isolate after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID1497852Antibacterial activity against Staphylococcus epidermidis ATCC 12228 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID285556Bactericidal activity against 19-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 4 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID1471050Growth inhibition of human A549 cells by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID419833Antibacterial activity against Klebsiella pneumoniae MTCC 109 after 24 hrs by liquid dilution method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID571647Antibacterial activity against Serratia marcescens ATCC 8100 by Etest method in presence of 4 ug/ml NAB70722008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID520108Antimicrobial activity against Mycobacterium tuberculosis H37Rv at assessed as growth inhibition at 10 mg/kg following 24 days oxygen depletion by Wayne method relative to control2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID572533Apparent volume of distribution in pulmonary tuberculosis patient in first order and lag time model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1406742Inhibition of replicating Mycobacterium tuberculosis H37Rv InhA assessed as cell growth inhibition after 7 days by MABA method2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis of carbohydrazides and carboxamides as anti-tubercular agents.
AID1781012Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth measured after 5 days by microplate alamar blue assay2021European journal of medicinal chemistry, Nov-05, Volume: 223Discovery of novel nitrogenous heterocyclic-containing quinoxaline-1,4-di-N-oxides as potent activator of autophagy in M.tb-infected macrophages.
AID1294369Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774 cells assessed as log reduction in bacterial burden at 10 times MIC measured 7 days postinfection relative to control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID326294Antibacterial activity against methicillin-resistant Staphylococcus aureus 5004 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID582985Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS06188 harboring MLST sequence type ST78 and pulsotype A expressing vanA gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1500590Antitubercular activity against Mycobacterium tuberculosis INH-R2 ATCC 35822 after 5 days by fluorescence-based assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID1071105Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 0.02 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1406779Antitubercular activity against Mycobacterium tuberculosis H37Rv after 1 week by microplate alamar blue assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.
AID765272Cmax/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1626655Antimicrobial activity against methicillin-resistant Staphylococcus aureus 67-02016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID531297Antimicrobial activity against Clostridium difficile isolate 69 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1891921Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1294361Antimicrobial activity against ofloxacin resistant Mycobacterium tuberculosis SRI 4000 assessed as growth inhibition at MIC after 7 days2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID533664Antimicrobial activity against Staphylococcus aureus RN1024-tms2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID543805Bactericidal activity against Streptococcus pyogenes VT 59 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1058230Antimycobacterial activity against Mycobacterium smegmatis2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID285915Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 433002007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antimicrobial activities of daptomycin, vancomycin, and oxacillin in human monocytes and of daptomycin in combination with gentamicin and/or rifampin in human monocytes and in broth against Staphylococcus aureus.
AID1626612Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1174923Antitubercular activity against Mycobacterium tuberculosis isolate 29/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID584114Antibacterial activity against Escherichia coli KAM32 harboring Staphylococcus aureus cloned pSP72 lmrS by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.
AID360007Antifungal activity against Cryptococcus neoformans ATCC 90113 after 48 hrs by modified well microplate assay2001Journal of natural products, May, Volume: 64, Issue:5
Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha.
AID1198805Anti-tuberculosis activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth by MABA method2015European journal of medicinal chemistry, Mar-26, Volume: 93Synthesis, biological evaluation and 3D QSAR study of 2,4-disubstituted quinolines as anti-tuberculosis agents.
AID360008Antibacterial activity against Staphylococcus aureus ATCC 6535 after 48 hrs by modified well microplate assay2001Journal of natural products, May, Volume: 64, Issue:5
Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha.
AID1194621Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 incubated for 7 days by alamar blue assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides.
AID283162Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2622 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1634253Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 25 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID446150Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.
AID1133238Antimicrobial activity against Bacillus subtilis 104 by serial dilution method1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Synthesis and quantitative structure--activity relationships of some antibacterial 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones.
AID1535474Antitubercular activity against Mycobacterium tuberculosis H37Rv after 6 days by alamar blue reagent based assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Optimization of N-benzyl-5-nitrofuran-2-carboxamide as an antitubercular agent.
AID1293897Antitubercular activity against active Mycobacterium bovis BCG ATCC 35743 incubated for 40 mins by XTT Reduction Menadione Assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID510974Antimicrobial activity against Acinetobacter baumannii infected in C57BL/6 mouse model assessed as reduction in bacterial count per gram of lung at total dose of 100 mg/kg/day, ip administered as four divided doses after 72 hrs (RVb = 10.6+/-0.27 No_unit)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID425403Antibacterial activity Escherichia coli isolate HM419 isolated from ileo-colonic mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1888134Antimycobacterial activity against Mycobacterium tuberculosis DprE1 C387S assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID414458Antitubercular activity against replicating form of Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
AID313234Antimicrobial activity against Streptococcus faecalis at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID1304832Antibacterial activity against methicillin-resistant Staphylococcus aureus clinical isolate 2 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1557243Antitubercular activity against resistant Mycobacterium tuberculosis 23 harboring rpoB His526Asp mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID565812Antimicrobial activity against Neisseria meningitidis assessed as resistant isolate by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Determination of CEM-101 activity tested against clinical isolates of Neisseria meningitidis from a worldwide collection.
AID611495Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 161 (PF161d) isolated from patient buttock abscess after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID577209Antimicrobial activity against Escherichia coli C600::933W in logarithmic phase encoding Stx-2 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID425588Antibacterial activity against gentamicin-treated internalized Escherichia coli isolate HM605 isolated from colonic mucosal biopsies of patient with Crohn's disease in mouse J774A1 cells assessed as intracellular killing of bacteria at 10.5 ug/ml after 3 2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID424321Antimicrobial activity against Dialister pneumosintes assessed as susceptibility breakpoint by CLSI method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID1730992Antitubercular activity against multi drug resistance Mycobacterium tuberculosis V2475 by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID581665Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU level at up to 10'5 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1278190Antimicrobial activity against Mycobacterium tuberculosis infected in mouse J774 cells assessed as log reduction of bacterial burden at 0.8 ug/ml after 7 days2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
AID1634250Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 200 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID511111Antiinflammatory activity in Acinetobacter baumannii 1327-infected New Zealand rabbit meningitis model assessed as brain edema at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID543802Bactericidal activity against Escherichia coli ATCC 25922 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID697852Inhibition of electric eel AChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1557240Antitubercular activity against resistant Mycobacterium tuberculosis 73 harboring rpoB His526Tyr mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID582514Cmin in Staphylococcus epidermidis ATCC 27626 infected Wistar rat tissue cage fluid at 25 mg/kg, ip measured on day 42008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID545912Antimicrobial activity against Escherichia coli ATCC 25922 in presence of 32 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID530867Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB H481N mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID560222Antibacterial activity against Salmonella enterica serovar Typhimurium 01-4 by CLSI M7-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Outer membrane protein STM3031 (Ail/OmpX-like protein) plays a key role in the ceftriaxone resistance of Salmonella enterica serovar Typhimurium.
AID487845Antibacterial activity against Bacillus cereus after 18 to 24 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID1152776Antimycobacterial activity against 2-oxo-1-(2-(4-((3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino)piperidin-1-yl)ethyl)-1,2-dihydroquinoline-7-carbonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA A74V mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID577487Antimicrobial activity against methicillin-susceptible Staphylococcus aureus SH1000 assessed as inhibition of bacterial biofilm formation by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1326671Inhibition of Mycobacterium tuberculosis DNA gyrase subunit A2B2 supercoiling activity using relaxed pBR322 as substrate after 30 mins in presence of ATP by agarose gel electrophoresis2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID442393Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterial tuberculosis H37Rv ATCC 272942010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification of benzofuro[2,3-b]quinoline derivatives as a new class of antituberculosis agents.
AID1762628Antibacterial activity against Acinetobacter baumannii ATCC 19606 by CLSI based microplate assay
AID1557242Antitubercular activity against resistant Mycobacterium tuberculosis 72 harboring rpoB His526Asp mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID1716643Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1209583Unbound drug partitioning coefficient, Kp of the compound assessed as ratio of unbound concentration in Sprague-Dawley rat brain to unbound concentration in plasma2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID559763Antimycobacterial activity against Mycobacterium smegmatis MC2 155 harboring PknG K181M mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID368766Induction of voriconazole metabolism in po dosed bacterial infection patient assessed as increase in hydroxyvoriconazole levels after 30 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Induction of voriconazole metabolism by rifampin in a patient with acute myeloid leukemia: importance of interdisciplinary communication to prevent treatment errors with complex medications.
AID678717Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-benzyloxyquinoline as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1879568Antibacterial activity against Peptostreptococcus anaerobius ATCC 273372022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID529188Antibacterial activity against Klebsiella pneumoniae K56 with arr-5 gene by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID584269Inhibition of Escherichia coli RNA polymerase using Kool NC-45 universal RNA polymerase template2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase.
AID1716772Antibacterial activity against Pseudomonas aeruginosa 259-96918 assessed as reduction in bacterial growth by measuring doxycycline MIC at 2 ug/ml incubated for 18 hrs in presence of doxycycline by broth microdilution assay (Rvb = 32 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1626622Antimicrobial activity against methicillin-sensitive Staphylococcus aureus clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID271342Antitubercular activity against Mycobacterium tuberculosis H37Rv2006Bioorganic & medicinal chemistry letters, Oct-01, Volume: 16, Issue:19
Search of antitubercular activities in tetrahydroacridines: synthesis and biological evaluation.
AID1058224Antimycobacterial activity against Mycobacterium intracellulare2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID144143Antimycobacterial activity against Mycobacterium kansasii (ATCC12478)2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.
AID1567115Antimicrobial activity against Staphylococcus aureus ATCC 25923 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID562786Antimicrobial activity against Chlamydia trachomatis L2/oflR-rifR1 harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID530992Antimicrobial activity against Clostridium difficile isolate 39 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1057527Antimycobacterial activity in Mycobacterium tuberculosis H37Rv after 5 days by Alamar Blue assay2013Bioorganic & medicinal chemistry letters, Dec-15, Volume: 23, Issue:24
Design, synthesis and evaluation of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine analogues as antimycobacterial agents.
AID1597873Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by resazurin microtiter assay
AID1869566Bactericidal activity against Enterococcus faecium DSM 20477 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1634247Antimycobacterial activity against Mycobacterium smegmatis assessed as reduction in microbial growth by CLSI method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1695730Inhibition of alpha-synuclein fibril formation (unknown origin) incubated for 24 hrs to 7 days by thioflavin S based fluorescence assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Toward the discovery and development of effective modulators of α-synuclein amyloid aggregation.
AID531276Antimicrobial activity against Clostridium difficile isolate 48 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1263165Antituberculosis activity against Mycobacterium tuberculosis H37Rv MTCC 300 after 4 weeks by Lowenstein-Jensen medium method2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Pyrazole clubbed triazolo[1,5-a]pyrimidine hybrids as an anti-tubercular agents: Synthesis, in vitro screening and molecular docking study.
AID341774Tmax in Mycobacterium tuberculosis infected patient at 20 mg/kg, po administered daily for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID1395197Antitubercular activity against multi-drug resistant Mycobacterium tuberculosis isolate 16883 after 7 days by Alamar blue assay2018European journal of medicinal chemistry, May-10, Volume: 151Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety.
AID1510688Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as parasite growth inhibition measured after 7 days incubation by microplate alamar blue assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents.
AID1765573Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID373965Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as sigmoidicity constant for drug effect on microbial grow2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID499896Antitubercular activity against Mycobacterium bovis BCG after 6 days by microplate alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Inhibition of mycobacterial replication by pyrimidines possessing various C-5 functionalities and related 2'-deoxynucleoside analogues using in vitro and in vivo models.
AID278858Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID532021Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60H containing pCK0601 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to CFU counts by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID532974Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 182010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID571439Antibacterial activity against Escherichia coli IH3080 by Etest method in presence of 4 ug/ml NAB70642008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID285568Bactericidal activity against 12-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 4 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID1190161Transactivation of human PXR expressed in in human HepG2 cells co-expressing pGL3-CYP3A4-luciferase gene assessed as increase in CYP3A4 promoter activity at 10 uM after 24 hrs by luciferase reporter gene assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
IND-2, a pyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinoline derivative, circumvents multi-drug resistance and causes apoptosis in colon cancer cells.
AID313237Antimicrobial activity against Mycobacterium tuberculosis at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID1262567Kinetic solubility in FaSSIF at pH 6.5 after 2 hours at 25 degC by shake flask method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID1716628Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as reduction in bacterial growth by measuring chloramphenicol MIC at 16 ug/ml incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay (Rvb = 2048 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1223010Induction of Cyp2c55 gene expression in male PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1873198Inhibition of ABCG2 (unknown origin) expressed in human HEK293 cells membrane vesicles assessed inhibition of BCRP- mediated transport of 3[H]-E1S for 1 mins using [3H]-estrone sulfate as substrate by rapid filtration technique2022European journal of medicinal chemistry, Jul-05, Volume: 237Targeting breast cancer resistance protein (BCRP/ABCG2): Functional inhibitors and expression modulators.
AID341769Cmax in Mycobacterium tuberculosis infected patient at 12 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID1463954Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1901704Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.A1 cells assessed as change in log10 CFU at 5 ug/ml2022European journal of medicinal chemistry, Mar-05, Volume: 231Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.
AID103689In vitro activity of compound against slowly growing Mycobacterium marinum 13941990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID541055Ratio of Cmax to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 12.5 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID572544AUC (0 to 24 hrs) in south african pulmonary tuberculosis patient with body weight >50 kg at 600 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID297688Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 0.5-1 uM by microplate alamar blue assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
AID576111Antimicrobial activity against mecA-deficient Staphylococcus sciuri harboring staphylococcus aureus mecA gene assessed as resistant isolates2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Nasal carriage of methicillin-resistant and methicillin-sensitive strains of Staphylococcus sciuri in the Indonesian population.
AID1627513Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition under aerobic conditions after 5 days by dual read-out fluorescence assay2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID510527Apparent oral clearance in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID586054Antimicrobial activity against Staphylococcus aureus clone 4-4 harboring staphylococcal cassette chromosome mec element type 5 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1888654Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as reduction in bacterial growth incubated for 7 days by Alamar blue assay2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.
AID560510Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b5k3529 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1778125Antimicrobial activity against Bacillus anthracis assessed as microbial growth inhibition by CLSI-protocol based broth microdilution assay2021Journal of natural products, 04-23, Volume: 84, Issue:4
Opportunities and Limitations for Assigning Relative Configurations of Antibacterial Bislactones using GIAO NMR Shift Calculations.
AID1879515Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1614 harboring rpoBL525I/D530N mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID525129Suppression of drug resistance development in Staphylococcus aureus RN4220 assessed as prolonged length of subculture to develop Linezolid resistance at 4 times MIC and 0.25 times IC50 after 25 days2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID531282Antimicrobial activity against Clostridium difficile isolate 54 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID306130Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry letters, Mar-15, Volume: 17, Issue:6
New thiopyrazolo[3,4-d]pyrimidine derivatives as anti-mycobacterial agents.
AID1624152Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 4 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID292290Antibacterial activity against Pseudomonas aeruginosa ATCC 13048 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID292416Antitubercular activity against Mycobacterium tuberculosis SS62007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID582499Antimicrobial activity against log phase culture of methicillin-resistant Staphylococcus aureus ATCC 29213 by macrodilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID1577321Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 7 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1542206Antimicrobial activity against methicillin-resistant Staphylococcus aureus incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID305229Antimicrobial activity against Arr-2 positive Escherichia coli DH5-alpha bearing pCTF1042007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID1688941Cytotoxicity against African green monkey Vero cells incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.
AID1705562Inhibition of RNA polymerase in Staphylococcus aureus ATCC 29213 assessed as reduction in total RNA level at 1/4 to 1/8 times MIC by fluorimetric method2020European journal of medicinal chemistry, Dec-15, Volume: 208Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction.
AID530801Antimicrobial activity against Clostridium difficile isolate 32 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1221855Induction of CYP3A4 mRNA expression in human hepatocytes at 5 uM after 12 to 48 hrs by RT-PCR analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Inhibition of human sterol Δ7-reductase and other postlanosterol enzymes by LK-980, a novel inhibitor of cholesterol synthesis.
AID434070Immunomodulatory effect in human A549 cells assessed as inhibition of Ca2+ ionophore A23187 stimulated-[3H]arachidonic acid release measured after 2 hrs of A23187 challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID694779Antimycobacterial activity against pan-susceptible Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin microtitre assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
1,3-Azoles from ortho-naphthoquinones: synthesis of aryl substituted imidazoles and oxazoles and their potent activity against Mycobacterium tuberculosis.
AID144878Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to rifampin (RMP)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID577490AUC (0 to 24 hrs) in Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model at 600 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1293905Cytotoxicity against human THP1 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID529193Antibacterial activity against Escherichia coli DHalpha harboring arr-5 gene after 20 hrs by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID1193495Thermodynamic equilibrium solubility, log S of the compound in simulated intestinal fluid at pH 6.8 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1062056Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 1 to 100 ug/ml after 7 days by resazurin assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents.
AID1236139Cytotoxicity against human THP1 cells assessed as cell growth inhibition after 48 hrs by resazurin dye reduction method2015Journal of natural products, Aug-28, Volume: 78, Issue:8
Callyaerins from the Marine Sponge Callyspongia aerizusa: Cyclic Peptides with Antitubercular Activity.
AID1514454Antitubercular activity against d-cycloserine-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID541027Antiproliferative activity against Theileria parva-induced proliferation of bovine BL3 cells assessed as inhibition of [3H]thymidine uptake after 32 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Theileria apicoplast as a target for chemotherapy.
AID341770Cmax in Mycobacterium tuberculosis infected patient at 20 mg/kg, po administered daily for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID1069162Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 infected in mouse J774 cells assessed as intracellular growth inhibition at 10-fold below MIC after 7 days relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1224527Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 131 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID1311238Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1062057Antimicrobial activity against multi drug-resistant Mycobacterium tuberculosis after 7 days by resazurin assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents.
AID1146809Antibacterial activity against Klebsiella pneumoniae Ottaviani assessed as inhibition of visible growth after 24 hrs by serial dilution method1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Synthesis and antibacterial activity of some derivatives of tolypomycinone. Relationship between structure and activity in ansamycins.
AID559091Antimicrobial activity against bla OXA-66 gene-deficient Acinetobacter baumannii isolate A2 by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
In vivo selection of reduced susceptibility to carbapenems in Acinetobacter baumannii related to ISAba1-mediated overexpression of the natural bla(OXA-66) oxacillinase gene.
AID565810Antimicrobial activity against Neisseria meningitidis by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Determination of CEM-101 activity tested against clinical isolates of Neisseria meningitidis from a worldwide collection.
AID581655Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient at pH 7.4 after 48 hrs by broth microdilution method in presence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1634994Antimicrobial activity against Pseudomonas aeruginosa 5482 assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID555297Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID645553Antimicrobial activity against Mycobacterium chelonae by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID683317Antibacterial activity against Bacillus subtilis ATCC 6633 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID1400057Antibacterial activity against Escherichia coli ATCC 10798 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID545056Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate DL010 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID1601819Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Mar-01, Volume: 165Marine natural products as potential anti-tubercular agents.
AID530779Antimicrobial activity against Clostridium difficile isolate 10 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1594311Antitubercular activity against dormant stage of Mycobacterium bovis BCG ATCC 35743 after 12 days by nitrate reductase assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID541039Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 12.5 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID530769Antimicrobial activity against beta-lactamase producing Staphylococcus aureus SH10002008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
AID292301Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv at 2mg/mL by BACTEC assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID1879540Antibacterial activity against rifampicin/fluoroquinolone-resistant Clostridioides difficile CB1940 harboring rpoBQ489K/gyrAA118S mutant measured after 3 days2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1427049Selectivity index, ratio of GI50 for human A549 cells to MIC for dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID646114Antitubercular activity against multi-drug-resistant Mycobacterium tuberculosis H37Rv clinical isolate after 28 days by 10 fold serial dilution method2012Bioorganic & medicinal chemistry letters, Feb-15, Volume: 22, Issue:4
Camphorsulfonic acid catalysed facile tandem double Friedlander annulation protocol for the synthesis of phenoxy linked bisquinoline derivatives and discovery of antitubercular agents.
AID529163Antibacterial activity against Pseudomonas aeruginosa 100609 assessed as reduction in bacterial count at 0.25 times MIC after 9 hrs by time-kill assay in presence of 250 ug/ml polyethylenimine relative to control2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID1061098Antimicrobial activity against Staphylococcus aureus2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID285185Antimicrobial activity against community-acquired methicillin-resistant Staphylococcus aureus Panton-Valentine leukocidin negative by time-kill methodology2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
AID510525Ratio of half life in diabetic tuberculosis patient to half life in tuberculosis patient2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1079935Cytolytic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is > 5 (see ACUTE). Value is number of references indexed. [column 'CYTOL' in source]
AID1164303Inhibition of protein synthesis in Mycobacterium bovis BCG assessed as inhibition of [3H]leucine incorporation by liquid scintillation counting2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID559761Antimycobacterial activity against Mycobacterium smegmatis MC2 155 by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID609620Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis by agar dilution method2011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Design, synthesis and antimycobacterial evaluation of novel 3-substituted-N-aryl-6,7-dimethoxy-3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide analogues.
AID540235Phospholipidosis-negative literature compound
AID1423473Inhibition of refolded MDH (unknown origin) preincubated with Escherichia coli GroEL/GroES for 45 mins in absence of compound followed by compound addition and measured for 20 to 35 mins by spectrometric analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1653431Antimicrobial activity against Staphylococcus aureus ATCC 25923 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID532976Antimicrobial activity against multidrug drug-resistant Mycobacterium tuberculosis isolate 202010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1856860Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as growth inhibition measured after 18 to 24 hrs by CLSI based broth microdilution method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID748179Inhibition of rifamycin-resistant Escherichia coli RNA polymerase D516V mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID1730991Antitubercular activity against drug susceptible Mycobacterium tuberculosis V4207 by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID1364757Antibacterial activity against Mycobacterium tuberculosis H37Rv infected in 3D culture of human PBMC assessed as colony forming units treated for 4 days measured after 3 days2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID377700Cytotoxicity against african green monkey Vero cells by neutral red assay2006Journal of natural products, Jul, Volume: 69, Issue:7
Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases.
AID571420Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 1 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1276361Antioxidant activity assessed as DPPH radical scavenging activity by spectrophotometric assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID610801Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 4 days by MABA assay2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and antimycobacterial activities of non-purine analogs of 6-aryl-9-benzylpurines: Imidazopyridines, pyrrolopyridines, benzimidazoles, and indoles.
AID1601918Antitubercular activity against multidrug resistant Mycobacterium tuberculosis isolate 1
AID518799Antimycobacterial activity against Mycobacterium fortuitum after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1204851Antitubercular activity against Isoniazid-resistant Mycobacterium tuberculosis assessed as parasite growth inhibition by REMA method2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID494493Antituberculosis activity against Mycobacterium tuberculosis at MIC concentration after 7 days using resazurin dye by broth microdilution assay2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
New quinoline derivatives: synthesis and investigation of antibacterial and antituberculosis properties.
AID530753Induction of PlytR::lacZ gene expression in Staphylococcus aureus SH1000 at 0.05 ug/ml after 2 hrs by beta-galactosidase reporter gene assay relative to untreated control2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
AID1185554Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by MABA method2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis and antimycobacterial evaluation of 1-(4-(2-substitutedthiazol-4-yl)phenethyl)-4-(3-(4-substitutedpiperazin-1-yl)alkyl)piperazine hybrid analogues.
AID520081Antimicrobial activity against aheB deficient kanamycin-resistant Aeromonas hydrophila subsp. hydrophila ATCC 7966 harboring plasmid pEX19Gm by agar dilution method in presence of 64 mg/L efflux pump inhibitor phenylalanine-arginine-beta-naphthylamide2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID487846Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID1856862Hemolytic activity against mouse RBC measured after 1 hrs2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1652706Induction of Escherichia coli K12 MG1655 recA promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID1133239Antimicrobial activity against Staphylococcus aureus 11 by serial dilution method1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Synthesis and quantitative structure--activity relationships of some antibacterial 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones.
AID1262571Cytotoxicity against African green monkey Vero cells assessed as cell viability by MTT assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID1668179Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID545911Antimicrobial activity against Escherichia coli ATCC 25922 in presence of 16 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID292414Antitubercular activity against Mycobacterium tuberculosis SS42007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID1157273Antibacterial activity against Acinetobacter baumannii by resazurin-based assay2014Journal of natural products, May-23, Volume: 77, Issue:5
Mahorones, highly brominated cyclopentenones from the red alga Asparagopsis taxiformis.
AID1784360Antimycobacterial activity against Mycobacterium tuberculosis DprE1 T314H in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID434071Immunomodulatory effect in human A549 cells assessed as inhibition of Ca2+ ionophore A23187 stimulated-[3H]arachidonic acid release measured after 4 hrs of A23187 challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID279814Antimicrobial activity against Escherichia coli DH5-alpha with pYW2 expressing KPC2 and TEM1 gene by agar dilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Plasmid-mediated KPC-2 in a Klebsiella pneumoniae isolate from China.
AID565786Antimicrobial activity against Neisseria meningitidis harboring rpoB23 S548F mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1071098Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv SRI 1369 after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID634272Antimycobacterial activity against Mycobacterium tuberculosis isolate 353 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1323738Growth inhibition of Mycobacterium tuberculosis H37Ra at 0.002 ug/ml after 6 days by microplate alamar blue assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents.
AID392603Antimycobacterial activity against Mycobacterium phlei MTCC 1724 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1293903Cytotoxicity against human PANC1 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID143435In vitro anti-mycobacterial activity against Mycobacterium tuberculosis strain H37Rv2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Mixed steroidal 1,2,4,5-tetraoxanes: antimalarial and antimycobacterial activity.
AID1716655Antibacterial activity against gentamicin-resistant Pseudomonas aeruginosa CAN-ICU 62308 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1781726Antibacterial activity against Escherichia coli ATCC 25922 assessed as bacterial growth inhibition in presence of outermembrane permeabilizer, PMBN incubated for 16 to 18 hrs by broth microdilution method
AID571198Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method in presence of 0.25 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID495474Antimicrobial activity against Mycobacterium tuberculosis NJT210TCC harboring embB406 GGC-TCC(Gly-Ser) mutation in embB gene after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID1139430Bactericidal activity against wild type Mycobacterium tuberculosis H37Rv infected in IFN-gamma-stimulated primary human monocyte-derived macrophages assessed as reduction of log10CFU at 30 times MIC incubated for 7 days followed by compound washout measur2014Journal of medicinal chemistry, May-08, Volume: 57, Issue:9
Synthetic calanolides with bactericidal activity against replicating and nonreplicating Mycobacterium tuberculosis.
AID529519Antibacterial activity against normal-colony variant Staphylococcus aureus derived from cystic fibrosis patient assessed as resistant isolates at 37 degC after 24 hrs by disk diffusion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
The thymidine-dependent small-colony-variant phenotype is associated with hypermutability and antibiotic resistance in clinical Staphylococcus aureus isolates.
AID1706678Antitubercular activity against isoniazid/rifampicin/streptomycin/capreomycin/ofloxacin extensively drug-resistant Mycobacterium tuberculosis FJ05195 clinical isolates assessed as bacterial growth inhibition by MABA2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB.
AID1174008Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as complete growth inhibition at 20 uM after 5 days2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Synthesis and evaluation of the 2,4-diaminoquinazoline series as anti-tubercular agents.
AID529525Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis isolate NJT210EMB-R-C1 assessed as bacterial colony formation at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1564635Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial cell growth incubated for 7 days by microplate alamar blue assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
AID555309Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 197 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1716771Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as reduction in bacterial growth by measuring doxycycline MIC at 4 ug/ml incubated for 18 hrs in presence of doxycycline by broth microdilution assay (Rvb = 64 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1143267Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis 912253 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID1294353Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 assessed as growth inhibition at MIC after 7 days2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID1890845Selectivity index, ratio of MIC50 for antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC empty vector to MIC50 for antimycobacterial activity against wild type Mycobacterium smegmatis mc2 1552022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID1654160Selectivity index, ratio of IC50 for cytotoxicity against African green monkey Vero cells to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID1275925Antibacterial activity against Bacillus subtilis 168 assessed as growth inhibition at 200 uM measured every 10 mins for 16 hrs by FLUOstar Optima plate reader analysis relative to control2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
From indole to pyrrole, furan, thiophene and pyridine: Search for novel small molecule inhibitors of bacterial transcription initiation complex formation.
AID1471049Growth inhibition of human HeLa cells by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1635006Bactericidal activity against Pseudomonas aeruginosa assessed as reduction in bacterial count at 20 uM after 4 hrs by time kill assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID529190Antibacterial activity against Klebsiella pneumoniae K688 with arr-5 gene by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID1602930Selectivity index, ratio of IC50 for mouse J774A.1 cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 272942019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1736274Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days by MABA method2020European journal of medicinal chemistry, Feb-15, Volume: 188Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
AID1759474Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16995 clinical isolate incubated for 7 days by microplate alamar blue assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis.
AID1163981Cytotoxicity against mouse RAW264.7 cells at 100 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1716865Antibacterial activity against Pseudomonas aeruginosa 101885 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID580843Oral bioavailability in healthy human at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID564973Antimicrobial activity against Mycobacterium bovis BCG by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1401976Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv INH-R1 harboring katG Y155 truncated mutant2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID581663Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level per mg of protein at up to 10'5 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1687560Antitubercular activity against PAS/INH/EMB/RMP-resistant Mycobacterium tuberculosis Spec.210 assessed as inhibition of microbial growth by classical test tube method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID1756848Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by filter paper disc diffusion method2021European journal of medicinal chemistry, Apr-05, Volume: 215Antitubercular properties of thiazolidin-4-ones - A review.
AID559771Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 4sy39 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1154348Antimycobacterial activity against Mycobacterium tuberculosis over expressing InhA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1170103Antimicrobial activity against Mycobacterium tuberculosis H37Ra after 4 days by MTT assay2014Journal of natural products, Nov-26, Volume: 77, Issue:11
Isolation of pyrrolocins A-C: cis- and trans-decalin tetramic acid antibiotics from an endophytic fungal-derived pathway.
AID1447478Antibacterial activity against Pseudomonas aeruginosa PAO1 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID634284Antimycobacterial activity against Mycobacterium tuberculosis isolate 364 expressing rpoB Ser522Leu mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID413210Induction of CYP3A4 activity in cryopreserved human hepatocytes from female NPV donars with history of tobacco and substance usage at 20 uM relative to 20 uM rifampin2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
AID558240Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 1.5 mg/liter upto 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1654163Bactericidal activity against Mycobacterium tuberculosis H37Rv harboring LuxAB gene assessed as reduction in microbial growth by measuring reduction in relative luminescence units after 14 days by luminometric method2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID333071Antimalarial activity against chloroquine-resistant Plasmodium falciparum W22004Journal of natural products, Aug, Volume: 67, Issue:8
Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases.
AID1071106Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 0.04 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID406471Ratio of MBC for Staphylococcus aureus ATCC 29213 during logarithmic-growth phase to stationary-growth phase2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID1891913Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID245415Minimum inhibitory concentration against resistant Mycobacterium tuberculosis clinical isolates; N=9; Range=2-162005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents.
AID531120Antimicrobial activity against Staphylococcus aureus CB1947 harboring rpoB R484H, L520 deficient gyrA, gyrA S48L, gyrA E88K, R236 duplicated parC, parCH103Y, parC S80Y, parC E84G mutant genes selected after CBR-2092 exposure for 20 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1491401Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 7 days by rapid direct susceptibility test
AID1869570Bactericidal activity against Klebsiella oxytoca DSM 5175 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1471030Growth inhibition of Mycobacterium bovis BCG ATCC 35743 at 1 ug/ml by nitrate reductase based two-fold dilution assay relative to control2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID283160Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2554 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID345804Cytotoxicity against HEK293 cells after 72 hrs by MTT assay2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.
AID1716651Antibacterial activity against Streptococcus pneumoniae ATCC 49619 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID699540Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1209581Fraction unbound in Sprague-Dawley rat brain homogenates at 5 uM by equilibrium dialysis analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID572550AUC (0 to 10 hrs) in north american pulmonary tuberculosis patient coinjected with HIV with body weight <=50 kg at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID292308Antibacterial activity against Salmonella Typhimurium at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID582989Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0847 harboring MLST sequence type ST78 and pulsotype E expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID373026Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PUA1 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID571640Antibacterial activity against Klebsiella oxytoca ATCC 13182 by Etest method in presence of 4 ug/ml NAB70652008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1287963Antitubercular activity against dormant Mycobacterium bovis BCG ATCC 35743 by NR assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Facile synthesis of 1,3-thiazolidin-4-ones as antitubercular agents.
AID1334245Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage infected in human THP1 cells measured on day 12 by nitrate reductase assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1383955Bactericidal activity against Mycobacterium tuberculosis H37Rv after 4 weeks by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID278677Antibacterial activity against Enterococcus faecium isolate 25472007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1887544Antibacterial activity against Escherichia coli ATCC 25922 assessed as reduction in bacterial growth incubated for 16 to 18 hrs by broth microdilution method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID293533Antimycobacterial activity against Mycobacterium avium ATCC 25291 at 2 ug/mL after 24 to 48 hrs by MABA2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Studies on acyclic pyrimidines as inhibitors of mycobacteria.
AID531269Antimicrobial activity against Clostridium difficile isolate 41 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID558015Antibacterial activity against Staphylococcus aureus E19977 by Etest2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1756033Antitubercular activity against Mycobacterium tuberculosis H37Ra assessed as bacterial growth inhibition
AID1852754Antibacterial activity against wild type Escherichia coli ATCC 25922 assessed as bacterial growth inhibition by broth microdilution assay2022RSC medicinal chemistry, Sep-21, Volume: 13, Issue:9
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria.
AID1365705Antitubercular activity against fluoroquinolone-resistant Mycobacterium tuberculosis H37Rv harboring gyrB D94N mutant after 5 days2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID531267Antimicrobial activity against Clostridium difficile isolate 39 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1716644Antibacterial activity against Pseudomonas aeruginosa 101243 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of doxycycline by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID679957TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID1463953Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1204850Antitubercular activity against Rifampicin-resistant Mycobacterium tuberculosis assessed as parasite growth inhibition by REMA method2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID292292Antibacterial activity against Staphylococcus epidermidis ATCC 14990 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID611486Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 106 isolated from patient nasal swab after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID1055953Antimycobacterial activity against Mycobacterium smegmatis ATCC 700084 under normoxic condition after 72 hrs by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1296403Cytotoxicity against human HeLa cells assessed as cell viability at 20 uM after 24 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1784355Antimycobacterial activity against Mycobacterium tuberculosis QcrB A317T mutant in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID245047Minimum inhibitory concentration against Mycobacterium tuberculosis H37Rv; Range 0.125-0.25 ug/mL2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Identification of heteroarylenamines as a new class of antituberculosis lead molecules.
AID532959Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 32010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID529186Antibacterial activity against Pseudomonas aeruginosa PS1111 with arr-4 gene by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID530864Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB H472 mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID571421Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 0.5 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID729921Cytotoxicity against mouse bone marrow derived macrophage assessed as growth inhibition after 48 hrs by MTS assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents.
AID1071110Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 0.08 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1493159Induction of RNA damage in Bacillus subtilis isolate 1S34 assessed as increase in helD promoter activity at 30 ug after 14 to 18 hrs by beta-galactosidase reporter gene assay2017Journal of natural products, 11-22, Volume: 80, Issue:11
Cyclic Cystine-Bridged Peptides from the Marine Sponge Clathria basilana Induce Apoptosis in Tumor Cells and Depolarize the Bacterial Cytoplasmic Membrane.
AID543803Bactericidal activity against Pseudomonas aeruginosa ATCC 27853 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1856894Induction of cell membrane disruption in Staphylococcus aureus ATCC 25923 assessed as increase in PI uptake measured after 30 to 120 mins by propidium iodide staining based FACS flow cytometry analysis (Rvb = 15%)2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID600828Antimycobacterial activity against Mycobacterium smegmatis ATCC 19420 after 7 days by resazurin method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents.
AID1310890Agonist activity at PXR expressed in human HepG2 cells after 24 hrs by p3A4-luciferase reporter gene assay2016Journal of medicinal chemistry, 05-26, Volume: 59, Issue:10
2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists.
AID292291Antibacterial activity against Salmonella Typhimurium after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID530804Antimicrobial activity against Clostridium difficile isolate 35 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1182141Antitubercular activity against Mycobacterium smegmatis by checkerboard assay in presence of chlorpromazine-N-oxide2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID419830Antibacterial activity against Bacillus subtilis MTCC 619 after 24 hrs by liquid dilution method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID103843In vitro activity of compound against rapidly growing Mycobacterium smegmatis 1391990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1738816Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth incubated for 1 week by alamar blue based assay2020European journal of medicinal chemistry, Aug-01, Volume: 199Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
AID680348TP_TRANSPORTER: inhibition of E217betaG uptake in Xenopus laevis oocytes2000Hepatology (Baltimore, Md.), Jul, Volume: 32, Issue:1
Rifamycin SV and rifampicin exhibit differential inhibition of the hepatic rat organic anion transporting polypeptides, Oatp1 and Oatp2.
AID1403704Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 1 week in presence of piperine by MABA method2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1167360Antibacterial activity against wild type Staphylococcus epidermidis ATCC 35984 after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1185716Antifungal activity against Trichophyton rubrum ATCC 28188 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID292307Antibacterial activity against Pseudomonas aeruginosa ATCC 13048 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID285563Bactericidal activity against 26-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 11 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID1143686Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in lung at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 10 2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
AID586047Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type 6 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID520082Antimicrobial activity against aheB deficient kanamycin-resistant Aeromonas hydrophila subsp. hydrophila ATCC 7966 harboring AheABC efflux pump by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID1577317Antimycobacterial activity against Mycobacterium tuberculosis H37Rv CNCTC My 331/88 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID574794Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 obtained from sputum of patient at 1 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1433098Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Novel amide and sulphonamide derivatives of 6-(piperazin-1-yl)phenanthridine as potent Mycobacterium tuberculosis H37Rv inhibitors.
AID585878Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type 2 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID368765Induction of voriconazole metabolism in po dosed bacterial infection patient assessed as increase in voriconazole N-oxide metabolite levels after 30 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Induction of voriconazole metabolism by rifampin in a patient with acute myeloid leukemia: importance of interdisciplinary communication to prevent treatment errors with complex medications.
AID555515Antibacterial activity against methicillin-resistant, Linezolid non-susceptible coagulase-negative Staphylococcus epidermidis 345 after 9 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1477417Antibacterial activity against 6-((3-Fluorobenzyl)(methyl)amino)-N-(4-methoxyphenyl)-pyrimidine-4-carboxamide-resisitant Mycobacterium tuberculosis H37Rv grown in GAST/Fe medium measured on day 14 post inoculation by broth microdilution method2017Journal of medicinal chemistry, 12-28, Volume: 60, Issue:24
Novel Antitubercular 6-Dialkylaminopyrimidine Carboxamides from Phenotypic Whole-Cell High Throughput Screening of a SoftFocus Library: Structure-Activity Relationship and Target Identification Studies.
AID1601917Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv
AID1247199Anti-tubercular activity against rifampicin, isoniazid, ethambutol and pyrazinamide-sensitive dormant phage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells by neutral red assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Design and synthesis of 11α-substituted bile acid derivatives as potential anti-tuberculosis agents.
AID356774Inhibition of DNA synthesis in Escherichia coli assessed as incorporation of [3H]thymidine at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2001Journal of natural products, Jul, Volume: 64, Issue:7
Biological and mechanistic activities of xanthorrizol and 4-(1',5'-dimethylhex-4'-enyl)-2-methylphenol isolated from Iostephane heterophylla.
AID1654164Binding affinity to recombinant Mycobacterium tuberculosis H37Rv N-terminal His6-tagged ClpC1 (1 to 145 residues) expressed in Escherichia coli BL21 cells by surface plasmon resonance analysis2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID560513Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b6k7974 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID572540Apparent volume of distribution in pulmonary tuberculosis patient in transit compartment model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID373750Antimicrobial activity against mupirocin-resistant methicillin-resistant Staphylococcus aureus assessed as resistant rate by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID1497863Antibacterial activity against Escherichia coli ATCC 105362018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID1726774Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 5 days by resazurin microtiter assay2021RSC medicinal chemistry, Jun-23, Volume: 12, Issue:6
Synthesis and evaluation of pyridine-derived bedaquiline analogues containing modifications at the A-ring subunit.
AID1061103Antimicrobial activity against Mycobacterium tuberculosis H37Rv in presence of 4% BSA2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID1589053Antimycobacterial against Mycobacterium tuberculosis H37Rv incubated for 7 days by MABA assay2019Bioorganic & medicinal chemistry letters, 09-15, Volume: 29, Issue:18
5-Chloro-2-thiophenyl-1,2,3-triazolylmethyldihydroquinolines as dual inhibitors of Mycobacterium tuberculosis and influenza virus: Synthesis and evaluation.
AID313230Antimicrobial activity against Bacillus subtilis at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID565995Antimycobacterial activity against Mycobacterium smegmatis MC2 155 after 72 hrs by broth microdilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID1716660Antibacterial activity against wild type Pseudomonas aeruginosa PAO1 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1716641Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of doxycycline by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID518802Antimycobacterial activity against Mycobacterium intracellular serovar 16 after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1765576Antibacterial activity against Staphylococcus epidermidis ATCC 12228 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID1311278Cytotoxicity against human HeLa cells by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID297684Antimycobacterial activity against Mycobacterium avium ATCC 25291 at 2 uM by microplate alamar blue assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
AID553473Tmax in simulated human serum in in vitro hollow-fiber PK model at 600 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Pharmacodynamics of minocycline against Staphylococcus aureus in an in vitro pharmacokinetic model.
AID279193Antibacterial activity against methicillin-susceptible Staphylococcus aureus isolates from skin or soft tissue infection outpatients2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Treatment and outcomes of infections by methicillin-resistant Staphylococcus aureus at an ambulatory clinic.
AID518804Antimycobacterial activity against Mycobacterium abscessus after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID537120Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774A1 cells assessed as reduction of bacterial growth at 0.125 ug/ml after 6 days relative to untreated control2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID590140Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents.
AID1491285Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate Alamar blue assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID1326390Antibacterial activity against Bacillus subtilis P10C derived after 10 passage in presence of JBIR-100 after 16 to 18 hrs by microbroth dilution assay relative to Bacillus subtilis ATCC 470962016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
AID530643Inhibition of cell wall synthesis in Staphylococcus aureus CB190 assessed as decrease in [2,3-3H]D-alanine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID425399Antibacterial activity against Escherichia coli isolate HM580 isolated from colonic mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID408871Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID501186Antimicrobial activity against methicillin sensitive Staphylococcus aureus 310 at 5 ug after 18 hrs by agar diffusion method2009Journal of natural products, Oct, Volume: 72, Issue:10
Norselic acids A-E, highly oxidized anti-infective steroids that deter mesograzer predation, from the Antarctic sponge Crella sp.
AID1862204In vivo antimycobacterial activity against Mycobacterium tuberculosis Erdman infected mouse acute tuberculosis infection model assessed as reduction lung bacterial load by measuring CFU at 15 mg/kg for 3 weeks at 5 days/week2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
AID1887548Antibacterial activity against Acinetobacter baumannii BAA 1605 assessed as reduction in bacterial growth incubated for 16 to 18 hrs in presence of PMBN by broth microdilution method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID717309Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in RLU at 2 ug/mL after 72 hrs by luciferase reporter phage assay2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Microwave-assisted synthesis, molecular docking and antitubercular activity of 1,2,3,4-tetrahydropyrimidine-5-carbonitrile derivatives.
AID1705576Antimycobacterial activity against Mycobacterium tuberculosis expressing pMV306-pks13 after 10 to 14 days2020European journal of medicinal chemistry, Dec-15, Volume: 208Synthesis and evaluation of thiophene based small molecules as potent inhibitors of Mycobacterium tuberculosis.
AID341773Tmax in Mycobacterium tuberculosis infected patient at 12 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID540213Half life in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID689222Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 culture in GAST media after 7 days by microplate alamar blue assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds.
AID1173026Induction of CYP3A4 mRNA expression in human primary hepatocytes at 10 uM after 24 hrs by RT-PCR analysis2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Cycloartane-type triterpenes from Euphorbia fischeriana stimulate human CYP3A4 promoter activity.
AID1869525Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC33591 measured after 24 hrs by broth microdilution method
AID285203Antimicrobial activity against Escherichia coli M124 mutant with AG100 lon4::IS186 acrR::IS genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID656228Antimycobacterial activity against isoniazid-, rifampin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1070198Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis MTB4000 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1337869Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium bovis BCG ATCC 35743 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID495233Antimicrobial activity against Mycobacterium tuberculosis NJT210CGG harboring embB497 CAG-CGG(Gln-Arg) mutation in embB gene after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID545931Antimicrobial activity against Acinetobacter baumannii ATCC 19606 by Etest method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1467474Antibacterial activity against Klebsiella pneumoniae incubated for overnight by microdilution method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID541091Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 during logarithmic growth phase by macrodilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID326288Antibacterial activity against methicillin-resistant Staphylococcus aureus 293 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID588215FDA HLAED, alkaline phosphatase increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID729923Antitubercular activity Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 4 weeks2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents.
AID1570242Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID571657Ratio of the MIC for Enterobacter cloacae CCUG52947 in the absence of NAB7067 to MIC for Enterobacter cloacae CCUG52947 in the presence of 4 ug/ml of NAB70672008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1879551Antibacterial activity against Bacteroides uniformis MMX 12772022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID326284Antibacterial activity against methicillin-resistant Staphylococcus aureus 5004 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID274948Reduction in log CFU of Mycobacterium tuberculosis Kurono infected in mouse lung at 5 mg/kg, po after 10 days2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles.
AID1869561Antibacterial activity against Mycobacterium smegmatis DSM 43080 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID377694Antimalarial activity after 72 hrs against chloroquine-sensitive Plasmodium falciparum D6 in erythrocytes by LDH reporter assay2006Journal of natural products, Jul, Volume: 69, Issue:7
Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases.
AID1294076Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra after 12 days by XTT-Menadione assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis and docking studies of pyrazine-thiazolidinone hybrid scaffold targeting dormant tuberculosis.
AID733062Antitubercular activity against Mycobacterium tuberculosis H37Rv by microdilution alamar Blue broth assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents.
AID1564638Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability2019European journal of medicinal chemistry, Nov-01, Volume: 181Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
AID283149Antimicrobial susceptibility of Staphylococcus lugdunensis isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID530744Induction of PtcaA::lacZ gene expression in Staphylococcus aureus SH1000 at 0.05 ug/ml after 2 hrs by beta-galactosidase reporter gene assay relative to untreated control2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
AID1476355Selectivity index, ratio of IC50 for human MRC5 cells to IC50 for replicating stage Mycobacterium tuberculosis H37Rv ATCC 272942017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID256054Minimum inhibitory concentration against Mycobacterium bovis2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Design and studies of novel 5-substituted alkynylpyrimidine nucleosides as potent inhibitors of mycobacteria.
AID1483718Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-a K179N mutant supplemented with 4 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1915643Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth by MABA analysis2021European journal of medicinal chemistry, Jan-15, Volume: 210An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
AID1436914Antimycobacterial activity against dormant state of Mycobacterium bovis BCG by two fold dilution method2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID564981Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring inactivated p55 gene by resazurine microtiter assay in presence of 0.5 mg/liter reserpine2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1163982Cytotoxicity against mouse RAW264.7 cells at 50 uM after 72 hrs by MTT assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1602935Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 3 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1297316Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 3 days by microplate Alamar Blue assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1819099Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 2 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID395779Antibacterial activity against Bacillus subtilis ATCC 6633 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID603726Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
Synthesis and screening of (E)-1-(β-D-galactopyranosyl)-4-(aryl)but-3-ene-2-one against Mycobacterium tuberculosis.
AID620088Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties.
AID1065394Oral bioavailability in human2014Journal of medicinal chemistry, Jan-23, Volume: 57, Issue:2
Macrocyclic drugs and clinical candidates: what can medicinal chemists learn from their properties?
AID1133241Antimicrobial activity against Mycobacterium phlei 111 by serial dilution method1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Synthesis and quantitative structure--activity relationships of some antibacterial 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones.
AID1294368Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774 cells assessed as log reduction in bacterial burden at MIC measured 7 days postinfection relative to control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID373940AUC (0 to 168 hrs) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1577318Antimycobacterial activity against Mycobacterium tuberculosis H37Rv CNCTC My 331/88 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1474037AUC in human at 150 to 600 mg, iv QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID373047Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate FZ4A18 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1400035Antibacterial activity against Mycobacterium smegmatis ATCC 607 incubated for 48 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID528946Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 2 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID530781Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 12 expressing RpoB H502N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID104004Antibacterial activity against Mycobacterium tuberculosis H37Rv in BACTEC 12B medium using microplate alamar blue assay2002Journal of medicinal chemistry, Mar-14, Volume: 45, Issue:6
Synthesis and antimycobacterial activity of 6-arylpurines: the requirements for the N-9 substituent in active antimycobacterial purines.
AID1716646Antibacterial activity against methicillin-resistance Staphylococcus aureus ATCC 33592 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1193499Thermodynamic equilibrium solubility, log S of the compound simulated intestinal fluid at pH 6.8 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1759676Inhibition of RNA synthesis in Staphylococcus aureus ATCC 29213 at 8 times MIC measured by liquid scintillation counter2021European journal of medicinal chemistry, Jul-05, Volume: 2194-4-(Anilinomethyl)-3-[4-(trifluoromethyl)phenyl]-1H-pyrazol-1-ylbenzoic acid derivatives as potent anti-gram-positive bacterial agents.
AID571213Antibacterial activity against Acinetobacter baumannii F264 by Etest method in presence of 0.5 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1716649Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID748175Inhibition of rifamycin-resistant Mycobacterium tuberculosis RNA polymerase D435V mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID1467477Antibacterial activity against Escherichia coli incubated for overnight by microdilution method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID1447485Antibacterial activity against multidrug/extremely drug-resistant/colistin-resistant Pseudomonas aeruginosa isolate 101243 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID303654Antibacterial activity against Mycobacterium tuberculosis ATTC 27294 after 5 days by MABA assay2007Bioorganic & medicinal chemistry letters, Dec-15, Volume: 17, Issue:24
Synthesis and biological evaluation of N-(aryl)-2-thiophen-2-ylacetamides series as a new class of antitubercular agents.
AID326282Antibacterial activity against methicillin-resistant Staphylococcus aureus 4930 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID767540Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 assessed as growth inhibition at 0.3125 to 5 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID278582Reduction in Plasmodium falciparum FCK2 in human erythrocyte culture after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum.
AID541085Antibacterial activity against 1 x10'6 to 5 x10'6 CFU/ml methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as bacterial regrowth after 24 hrs by time kill study2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID680823TP_TRANSPORTER: Immunohistochemistry in vivo, apical membrane of enterocytes2000The American journal of pathology, Nov, Volume: 157, Issue:5
The effect of rifampin treatment on intestinal expression of human MRP transporters.
AID515921Antibacterial activity against clofazimine-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID531265Antimicrobial activity against Clostridium difficile isolate 37 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1891914Antimycobacterial activity against Mycobacterium fortuitum ATCC 6841 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID392608Antimycobacterial activity against 6-week-starved culture of Mycobacterium tuberculosis H37Rv by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1062066Antimicrobial activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents.
AID1770383Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as fold increase in MIC value measured after 1 passage by Multi passage resistance assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID340858Antimicrobial activity against wild type vancomycin-intermediate resistant Staphylococcus aureus Mu50 by microdilution assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus.
AID218066In vitro cytotoxicity against vero cells1999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID1869560Bactericidal activity against Mycobacterium phlei DSM 43239 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1272620Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 21 days by broth microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.
AID1765585Antibacterial activity against rifampin-resistant Pseudomonas aeruginosa ATCC 27853 incubated for 18 hrs in presence of EDTA by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID340016Inhibition of refampicin-mediated PXR activation in HepG2 cells2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).
AID1772152Antibacterial activity against Acinetobacter baumannii assessed as inhibition of bacterial growth by CLSI based microdilution method2021Journal of natural products, 11-26, Volume: 84, Issue:11
Antimicrobial and Cytotoxic Angucyclic Quinones from
AID565796Antimicrobial activity against Neisseria meningitidis harboring rpoB51 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID557394Antibacterial activity against Beta-lactamase-negative Neisseria meningitidis assessed as percent resistant isolates by Etest method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antibiotic susceptibility and characteristics of Neisseria meningitidis isolates from the African meningitis belt, 2000 to 2006: phenotypic and genotypic perspectives.
AID1397224Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 16833 after 7 days by Alamar blue assay2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties.
AID586048Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type U1 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID449209Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis ATCC 35838 by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID625290Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver fatty2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1262569Metabolic stability in rat liver microsomes assessed as residual compound at 0.1 uM after 30 mins by LC-MS/MS method in presence or absence of NADPH2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID1908125Antibacterial activity against vancomycin-resistant Enterococcus faecium clinical isolate assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID297115Antibacterial activity against Mycobacterium intracellular ATCC 15984 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID588209Literature-mined public compounds from Greene et al multi-species hepatotoxicity modelling dataset2010Chemical research in toxicology, Jul-19, Volume: 23, Issue:7
Developing structure-activity relationships for the prediction of hepatotoxicity.
AID618758Antitubercular activity against Mycobacterium tuberculosis H37Rv after 9 days by resazurin reduction assay2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
Quinonoid and phenazine compounds: synthesis and evaluation against H37Rv, rifampicin and isoniazid-resistance strains of Mycobacterium tuberculosis.
AID1181160Antimicrobial activity against clinical isolate Mycobacterium tuberculosis DKU76 assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID560975Antimicrobial activity against heteroresistant glycopeptide-intermediate Staphylococcus aureus 1629 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID571658Ratio of the MIC for Enterobacter cloacae in the absence of NAB7068 to MIC for Enterobacter cloacae in the presence of 4 ug/ml of NAB70682008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID530786Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 17 expressing RpoB H502N and I548M mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1879573Antibacterial activity against Prevotella disiens MMX 34572022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID103511In vitro activity of compound against rapidly growing Mycobacterium flavescens 12861990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1908127Antibacterial activity against Escherichia coli ATCC 8739 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID728673Antimicrobial activity against hldE-deficient Escherichia coli O18:K1:H7 after overnight incubation2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Novel HldE-K inhibitors leading to attenuated Gram negative bacterial virulence.
AID405144Ratio of apparent volume of distribution at 600 mg, po to apparent volume of distribution at 450 mg, po in tuberculosis patient2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1449137Antibacterial activity against Mycobacterium tuberculosis by AlamarBlue assay2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections.
AID1690488Inhibition of Mycobacterium tuberculosis H37Rv ATCC 27294 QcrB assessed as reduction in bacterial growth by resazurin reduction microplate assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents.
AID144875Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to kanamycin (KM)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID530632Antimicrobial activity against Staphylococcus aureus CB190 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID555310Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 225 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID558265Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 1 hr after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1536933Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 1 week by microplate alamar blue assay2019Bioorganic & medicinal chemistry letters, 02-15, Volume: 29, Issue:4
Synthesis and evaluation of novel substituted 1,2,3-triazolyldihydroquinolines as promising antitubercular agents.
AID1888846Antibacterial activity against Staphylococcus aureus 1199B measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID396041Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pBGS18 plasmid by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID1262566Antimicrobial activity against Mycobacterium tuberculosis H37RvMA under GAST/Fe medium assessed as growth inhibition after 14 days by alamar blue assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID1334265Selectivity index, ratio of GI50 for human THP1 cells to MIC90 for Mycobacterium bovis BCG ATCC 35743 dormant stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID564983Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID700527Antimycobacterial activity against isoniazid, rifampicin and ethambutol-resistant Mycobacterium tuberculosis at 0.3125 to 5 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID732685Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition measured every 24 hrs by BACTEC radiosusceptibility assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Syntheses of lipophilic chalcones and their conformationally restricted analogues as antitubercular agents.
AID1316914Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID1385220Antitubercular activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis 12525 clinical isolate measured after 7 days by microplate alamar blue assay
AID144139Antibacterial activity against Mycobacterium intracellular.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID689770Antitubercular activity against Mycobacterium tuberculosis H37Rv isolate SRI after 5 days by resazurin-based microplate assay2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis.
AID545057Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate SZ009 from patient pus by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID537733Binding affinity to Candida albicans CaCdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID571662Ratio of the MIC for Serratia marcescens ATCC 8100 in the absence of NAB7072 to MIC for Serratia marcescens ATCC 8100 in the presence of 4 ug/ml of NAB70722008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1765649Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as increase in MIC at sub-MIC level after 15 passages by broth microdilution assay2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID586234Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 7 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID1653477Antimicrobial activity against Listeria monocytogenes ATCC 1911 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID340015Induction of PXR transactivation in HepG2 cells2008Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14
Synthesis of novel ketoconazole derivatives as inhibitors of the human Pregnane X Receptor (PXR; NR1I2; also termed SXR, PAR).
AID1412764Antimycobacterial activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 by XRMA2018MedChemComm, Jul-01, Volume: 9, Issue:7
Triazole-diindolylmethane conjugates as new antitubercular agents: synthesis, bioevaluation, and molecular docking.
AID1562299Antimycobacterial activity against Mycobacterium smegmatis atR14 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID405167Half life in tuberculosis patient assessed as desacetylrifampin level at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID543813Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1716630Antibacterial activity against Pseudomonas aeruginosa 259-96918 assessed as reduction in bacterial growth by measuring chloramphenicol MIC at 2 ug/ml incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay (Rvb = 1024 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID530995Antimicrobial activity against Clostridium difficile isolate 42 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID586038Antimicrobial activity against Staphylococcus aureus clone 1-1 harboring staphylococcal cassette chromosome mec element type U assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID558236Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 2 mg/liter after 12 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID424424Antibacterial activity against vancomycin-resistant Staphylococcus aureus AIS2006032 isolated from patients foot wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID645538Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1167357Antibacterial activity against wild type Staphylococcus aureus ATCC 29213 after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1716625Antibacterial activity against wild type Pseudomonas aeruginosa PAO1 assessed as reduction in bacterial growth by measuring chloramphenicol MIC at 8 ug/ml incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay (Rvb = 32 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID565187Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 by microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Evaluation of analogs of reutericyclin as prospective candidates for treatment of staphylococcal skin infections.
AID332359Inhibition of DNA synthesis in Bacillus subtilis assessed as incorporation of [3H]thymidine at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2003Journal of natural products, Feb, Volume: 66, Issue:2
Antibacterial diterpenes from Calceolaria pinifolia.
AID645532Antitubercular activity against non-replicating Mycobacterium tuberculosis H37Rv expressing vibrio harveyii luciferase gene incubated 10 days under anaerobic condition measured after 28 hrs of recovery in aerobic condition by luciferase based low oxygen r2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1457502Antibacterial activity against Bacillus subtilis assessed as inhibition of DNA synthesis at 2 mg/L after 50 mins by [3H]thymidine incorporation assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents.
AID1167608Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis XDR-TB after 28 days by two-fold agar dilution method2014Bioorganic & medicinal chemistry, Nov-01, Volume: 22, Issue:21
Development of benzo[d]oxazol-2(3H)-ones derivatives as novel inhibitors of Mycobacterium tuberculosis InhA.
AID1337865Selectivity index, ratio of GI50 for human THP1 cells to MIC for Mycobacterium bovis BCG ATCC 35743 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1500579Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days measured under aerobic conditions by fluorescence-based assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID1668177Antibacterial activity against rifampicin-resistant Staphylococcus aureus assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID285193Antimicrobial activity against Escherichia coli M044 mutant with AG100 lon4::IS186 marR::IS genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID1126674Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of colony formation at 250 ug/mL after 2 to 4 weeks by Lowensteine-Jensen method relative to control2014European journal of medicinal chemistry, May-06, Volume: 78Synthesis, characterization and pharmacological screening of some novel 5-imidazopyrazole incorporated polyhydroquinoline derivatives.
AID1879508Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1902 harboring rpoBV149F mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID368652Apparent oral clearance in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID689224Antimycobacterial activity against Mycobacterium against recombinant Mycobacterium tuberculosis H37Rv expressing luxAB incubated for 10 days in anaerobic condition followed by incubation for 28 hrs in aerobic condition by LORA assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds.
AID457434Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID1593377Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in extensively drug-resistant Mycobacterium tuberculosis R506 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID586045Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type 1 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID634275Antimycobacterial activity against Mycobacterium tuberculosis isolate 307 expressing rpoB Ser531Leu mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1311276Cytotoxicity against human HCT116 cells by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID670862Antitubercular activity against non-replicating Mycobacterium tuberculosis assessed as minimum concentration required to inhibit 90% growth after 10 days under anaerobic condition by luciferase-based low-oxygen recovery assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
AID370267Cmax in human at 450 mg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID563689Antibacterial activity against Mycobacterium tuberculosis H37Ra by broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID1861232Antimycobacterial activity against Mycobacterium tuberculosis infected by aerosol in mouse acute infection model assessed as reduction in colony forming unit in lungs at 15 mg/kg, po treated 5 days per week from day 28 to day 38 post infection2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID445330Cytotoxicity against human A549 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1401978Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 INH-R22018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID1400025Selectivity ratio of MIC for antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv harboring pFCA-luxAB to MIC100 for antibacterial activity against replicating Mycobacterium tuberculosis H37Rv2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1772301Non-covalent inhibition of DprE1 in Mycobacterium tuberculosis H37Rv measured after 7 days by microplate Alamar blue assay
AID202132In vitro antibacterial activity of compound against Streptococcus pyogenes C 203 SKF 134001990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1223007Induction of Cyp3a11 gene expression in male PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1778094Antitubercular activity against INH, SM, RFP, EMB, RBT, PAS, OLFX-resistant Mycobacterium tuberculosis 13946 assessed as bacterial growth inhibition incubated for 7 days by MABA
AID1784362Antimycobacterial activity against Mycobacterium tuberculosis KatG T198A in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID408874Cytotoxicity against african green monkey Vero cells after 5 days2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1634249Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 400 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID565230Antimicrobial activity against Mycobacterium chelonae 9917 by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID95566Antimicrobial activity derived as minimum inhibitory concentration are determined using brain-heart infusion medium against Klebsiella Pneumoniae Ottaviani1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID1908128Antibacterial activity against NDM-1 expressing Escherichia coli ATCC BAA2469 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID530663Inhibition of protein synthesis in quinolone-resistant Staphylococcus aureus CB814 harboring gyrA S84L and parC S80F mutant genes assessed as decrease in L-[3,4,5-3H]leucine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1287509Selectivity index, ratio of GI50 for human A549 cells to MIC for active state Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID145142In vitro antimicrobacterial activity to inhibit 90% of Mycobacterium tuberculosis H37Rv (Rifampin and Isoniazid susceptible ATCC 27294 strain), relative to that of controls2000Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7
Isoniazid-related copper(II) and nickel(II) complexes with antimycobacterial in vitro activity. Part 9.
AID1223011Induction of Cyp2c37 gene expression in male PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1462344Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay
AID1634261Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 50 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID479638Antimycobacterial activity against Mycobacterium tuberculosis H37Ra after 6 days by microplate alamar blue assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis.
AID571418Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 4 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID571659Ratio of the MIC for Citrobacter freundii ATCC 8090 in the absence of NAB7069 to MIC for Citrobacter freundii ATCC 8090 in the presence of 4 ug/ml of NAB70692008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID774292Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID541043Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as no. of culture-negative cage fluid samples at 12.5 mg/kg measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID560506Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b3k2345 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID103646In vitro activity of compound against rapidly growing Mycobacterium fortuitum 12851990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID748180Inhibition of wild type Escherichia coli RNA polymerase after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID1716647Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis CANWARD 81388 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID545051Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ274 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID1476349Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through microemulsion vehicle as single oral dose per gavage after 0.3 hrs by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1765756Antimycobacterial activity against Mycobacterium bovis BCG assessed as inhibition of bacterial growth at 1 ug/ml measured by microplate alamar blue assay2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Design and synthesis of novel 5-alkynyl pyrimidine nucleosides derivatives: Influence of C-6-substituent on antituberculosis activity.
AID279567Antimicrobial activity against Salmonella enterica serovar Typhimurium SMP816 in Caenorhabditis elegans2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Caenorhabditis elegans as a model to determine fitness of antibiotic-resistant Salmonella enterica serovar typhimurium.
AID1194333Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining and electrophoresis based DNA supercoiling assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID477409Antibacterial activity against Staphylococcus aureus NCTC 8325 after 16 to 20 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Efflux-mediated bis-indole resistance in Staphylococcus aureus reveals differential substrate specificities for MepA and MepR.
AID1337864Selectivity index, ratio of GI50 for human THP1 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1163983Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by MABA method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1069174Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by BacTiter-Glo assay2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1514471Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as colony forming units at 0.002 to 64 ug/ml measured day 3 post dose by time kill assay (Rvb = 0 log10CFU/ml)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1311226Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-42016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1069160Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 infected in mouse J774 cells assessed as intracellular growth inhibition at 10-fold above MIC after 7 days relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1463956Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 1 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID528947Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 3 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1765580Antibacterial activity against Acinetobacter baumannii ATCC 19606 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID405147Apparent clearance in tuberculosis patient at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1334255Selectivity index, ratio of GI50 for human MCF7 cells to MIC90 for Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1476364Antitubercular activity against streptomycin resistant Mycobacterium tuberculosis H37Rv ATCC 35820 after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID465093Antibacterial activity against Mycobacterium intracellular by after 4 days alamar blue assay2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Anti-infective discorhabdins from a deep-water alaskan sponge of the genus Latrunculia.
AID445289Antibacterial activity against Staphylococcus aureus by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1311241Antibacterial activity against Enterococcus faecalis 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID557094Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 1.6% gamma globulin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID555294Antibacterial activity against Tmp-susceptible Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID368764Effect on voriconazole metabolism in po dosed bacterial infection patient assessed as decrease in voriconazole exposure levels after 30 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Induction of voriconazole metabolism by rifampin in a patient with acute myeloid leukemia: importance of interdisciplinary communication to prevent treatment errors with complex medications.
AID373039Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate ZJ32 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID571427Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method by Etest in presence of 0.5 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID588132Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 3 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID1879539Antibacterial activity against fluoroquinolone-resistant Clostridioides difficile CB1941 harboring gyrAD71Y/T82A mutant at 1:1 compound to metronidazole molar ratio measured after 3 days in presence of metronidazole2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1562303Antimycobacterial activity against Mycobacterium smegmatis atR40 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID1879507Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1903 harboring rpoBD530V mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1412767Antimycobacterial activity against Mycobacterium kansasii Hauduroy ATCC 12478 incubated in dark for 5 days by Alamar Blue assay2018MedChemComm, Apr-01, Volume: 9, Issue:4
Design, synthesis and antimycobacterial activity of hybrid molecules combining pyrazinamide with a 4-phenylthiazol-2-amine scaffold.
AID1772150Antitubercular activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth by green fluorescent protein based method2021Journal of natural products, 11-26, Volume: 84, Issue:11
Antimicrobial and Cytotoxic Angucyclic Quinones from
AID626923Antimycobacterial activity against Mycobacterium smegmatis MC2 ATCC 19420 using compound level ranging from 0.3125 to 5 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID1567118Antimicrobial activity against Enterococcus faecium ATCC 19433 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID529103Cardiotoxicity in pulmonary tuberculosis patient assessed as increase in QT interval at 600 mg/kg, po once daily for 7 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1632658Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells after 12 days by nitrate reductase assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID1262568Metabolic stability in human liver microsomes assessed as residual compound at 0.1 uM after 30 mins by LC-MS/MS method in presence or absence of NADPH2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID1908122Antibacterial activity against Enterococcus faecium ATCC 49624 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID571641Antibacterial activity against Klebsiella oxytoca CCUG51683 by Etest method in presence of 4 ug/ml NAB70662008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID509627Antibacterial activity against Mycobacterium tuberculosis containing phenotypic rpoB531,rpoB526,rpo533 mutation assessed as microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID1071087Antimycobacterial activity against Mycobacterium tuberculosis H37Rv SRI 1345 infected in mouse J774A1 cells assessed as reduction in bacterial growth at 1 ug/ml after 7 days relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID765123Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID531047Antimicrobial activity against Clostridium difficile isolate 14 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1879575Antibacterial activity against Prevotella intermedia ATCC 25611 MMX 30022022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID558755Antibacterial activity against methicillin-susceptible, tetracycline-resistant and chloramphenicol-resistant Staphylococcus aureus H14-KVR by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID1326673Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID1400050Bactericidal activity against Clostridium difficile ATCC 700057 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1311230Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1497853Antibacterial activity against Staphylococcus aureus ATCC 297372018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID442391Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay2010European journal of medicinal chemistry, Feb, Volume: 45, Issue:2
Identification of benzofuro[2,3-b]quinoline derivatives as a new class of antituberculosis agents.
AID1577333Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 9449/2007 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID372541Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 12-24 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID645691Antimicrobial activity against Mycobacterium kansasii by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1303883Antibacterial activity against methicillin resistant Staphylococcus aureus subsp. aureus HPV107 (ATCC BAA-44) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID103855In vitro activity of compound against slowl growingy Mycobacterium xenopi 5551990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID574551Decrease in delta toxin levels in Staphylococcus aureus Sanger 252 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID1869565Antibacterial activity against Enterococcus faecium DSM 20477 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1055960Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis ATCC 35820 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1706864Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID1879572Antibacterial activity against metronidazole-resistant Prevotella bivia MMX 34542022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID619608Antitubercular activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011European journal of medicinal chemistry, Sep, Volume: 46, Issue:9
A facile four-component sequential protocol in the expedient synthesis of novel 2-aryl-5-methyl-2,3-dihydro-1H-3-pyrazolones in water and their antitubercular evaluation.
AID1565593Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID625282Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cirrhosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1304827Antibiofilm activity against methicillin-resistant Staphylococcus aureus isolate 2 assessed as biofilm eradication incubated for 24 hrs by CBD assay2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1400062Bactericidal activity against Bacillus subtilis ATCC 6051 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID348342Antimycobacterial activity against rifampin and isoniazid-susceptible Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by Alamar blue assay2008European journal of medicinal chemistry, Jun, Volume: 43, Issue:6
Synthesis and anti-mycobacterial activity of (E)-N'-(monosubstituted-benzylidene)isonicotinohydrazide derivatives.
AID1652707Induction of Escherichia coli K12 MG1655 lexA promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID1418315Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay
AID1775049Agonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter at 10 uM incubated for 24 hrs by luciferase reporter assay relative to control
AID575170Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose at 200 uM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID1337838Growth inhibition of Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage measured after 12 days by XTT dye based two fold dilution method2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1181154Antimicrobial activity against clinical isolate Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1632660Antitubercular activity against drug resistant dormant Mycobacterium tuberculosis H37Ra ATCC 25177 after 12 days by XTT reduction menadione assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID493953Antimicrobial activity aagainst Mycobacterium sp. Mc2 in log phase assessed as inhibition of growth2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.
AID1634849Antitubercular activity against Mycobacterium tuberculosis H37Rv P887 incubated for 1 to 9 days by inverted microscopic analysis2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID401739Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 272941998Journal of natural products, Jul, Volume: 61, Issue:7
A new antitubercular mulinane diterpenoid from Azorella madreporica Clos.
AID626877Activation of human PXR in DPX2 cells after 24 hrs by microplate reader relative to control2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID352093Antimicrobial activity against Pseudomonas aeruginosa ATCC 25853 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID1378018Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID511018Half life in C57BL/6 mouse pneumonia model at 25 mg/kg, ip2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1666552Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth by measuring visual MIC90 measured after 14 days by green fluorescent protein based microplate assay2020Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5
Synthesis and biological evaluation of bis-N
AID1833894Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth incubated for 5 days by resazurin assay2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthetic Sansanmycin Analogues as Potent
AID1365731Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv RIF-R2 ATCC 35828 after 5 days2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1201995Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse bone-marrow derived macrophages assessed as reduction in intracellular colony forming units at 4 times antimycobacterial MIC measured during 3 hrs infection period2015European journal of medicinal chemistry, May-05, Volume: 95Thiophene containing trisubstituted methanes [TRSMs] as identified lead against Mycobacterium tuberculosis.
AID392600Antimycobacterial activity against Mycobacterium smegmatis ATCC 14468 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID495509Antibacterial activity against Acinetobacter baumannii BM4587 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID580846Tmax in healthy human at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1868116Anti-tubercular activity against Mycobacterium tuberculosis CF61 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID1311236Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1705575Antimycobacterial activity against Mycobacterium tuberculosis expressing pMV306 after 10 to 14 days2020European journal of medicinal chemistry, Dec-15, Volume: 208Synthesis and evaluation of thiophene based small molecules as potent inhibitors of Mycobacterium tuberculosis.
AID572541Mean transient time in pulmonary tuberculosis patient in transit compartment model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID285162Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID395777Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID572532Apparent oral clearance in pulmonary tuberculosis patient in first order and lag time model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID333069Antitubercular activity against Mycobacterium tuberculosis H37Rv2004Journal of natural products, Aug, Volume: 67, Issue:8
Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases.
AID571435Ratio of the MIC for Escherichia coli ATCC 25992 in the absence of NAB7061 to MIC for Escherichia coli ATCC 25992 in the presence of 4 ug/ml of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID530350Antimicrobial activity against Escherichia coli TOP10 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID1716870Antibacterial activity against Pseudomonas aeruginosa 91433 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID520291Antimicrobial activity against Staphylococcus aureus 25482008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Activities of daptomycin and comparative antimicrobials, singly and in combination, against extracellular and intracellular Staphylococcus aureus and its stable small-colony variant in human monocyte-derived macrophages and in broth.
AID1879505Antibacterial activity against metronidazole-resistant Helicobacter pylori CB1573 harboring rdxAR16S mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID541028Induction of apoptosis in bovine BL3 cells assessed as early apoptotic cells after 24 hrs by annexin V/propidium iodide staining-based FACS analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Theileria apicoplast as a target for chemotherapy.
AID683325Antifungal activity against Candida albicans ATCC 10231 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID1334247Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 active stage measured on day 8 by XTT reduction menadione based two-fold dilution assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID348179Antimycobacterial activity against non-replicating Mycobacterium tuberculosis assessed as luciferase activity incubated for 8 days measured after 24 hrs of incubation by low oxygen recover assay2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID373035Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate BJ55 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID545818fCmax in human at 450 mg/kg2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID1334258Selectivity index, ratio of GI50 for human HCT116 cells to MIC90 for Mycobacterium tuberculosis H37Ra ATCC 25177 active stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1739769Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 4 days by Microplate Alamar Blue Assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
AID1278194Cytotoxicity against mouse J774 cells assessed as cell viability at 8 ug/ml by MTT assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
AID1330850Antimycobacterial activity against Mycobacterium smegmatis MC2 155 measured after 48 hrs by resazurin dye-based MABA method2016European journal of medicinal chemistry, Nov-10, Volume: 123FtsZ inhibition and redox modulation with one chemical scaffold: Potential use of dihydroquinolines against mycobacteria.
AID1174925Antitubercular activity against Mycobacterium tuberculosis isolate 756/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID292411Antitubercular activity against Mycobacterium tuberculosis SS12007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID472702Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
AID1205463Antitubercular activity against rifampin, isoniazid, amikacin and ofloxacin-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID531050Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 17 expressing RpoB H502N and I548M mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID356917Antitubercular activity against Mycobacterium tuberculosis H37Rv by alamar blue assay2002Journal of natural products, Dec, Volume: 65, Issue:12
Araguspongines K and L, new bioactive bis-1-oxaquinolizidine N-oxide alkaloids from Red Sea specimens of Xestospongia exigua.
AID1678511Antibacterial activity against Clostridium difficile ATCC 9689 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID1476357Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 under acidic pH 6 condition2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID694227Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID530662Inhibition of RNA synthesis in quinolone-resistant Staphylococcus aureus CB814 harboring gyrA S84L and parC S80F mutant genes assessed as decrease in [5,6-3H]uridine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID565185Antimicrobial activity against Staphylococcus epidermidis RP62A grown as biofilms by microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Evaluation of analogs of reutericyclin as prospective candidates for treatment of staphylococcal skin infections.
AID1154349Antimycobacterial activity against Mycobacterium tuberculosis over expressing TopA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID574546Antimicrobial activity against community-associated methicillin-resistant Staphylococcus aureus Sanger 2522010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID1224519Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 9449/2007 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID1634252Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 50 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1653478Antimicrobial activity against Klebsiella pneumoniae 700603 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID543816Bactericidal activity against Haemophilus influenzae VT450-2006 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1908119Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID370070Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35838 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID531057Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 24 expressing RpoB H502N and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1891916Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1784354Antimycobacterial activity against Mycobacterium tuberculosis delta cyd in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID285200Antimicrobial activity against Escherichia coli M103 mutant with AG100 lon3::IS186 acrR-acrAB genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID1491288Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID1632661Antitubercular activity against active Mycobacterium tuberculosis H37Ra ATCC 25177 after 8 days by XTT reduction menadione assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID1905567Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID531304Antimicrobial activity against Clostridium difficile isolate 76 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1627516Antitubercular activity against Mycobacterium tuberculosis H37Rv RIF-R1 harboring nrpoB S522L mutant after 5 days2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID283169Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5258 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1770376Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as fold increase in MIC value measured after 15 passages by Multi passage resistance assay2021European journal of medicinal chemistry, Nov-15, Volume: 224Modification of 5-methylphenanthridium from benzothiazoles to indoles as potent FtsZ inhibitors: Broadening the antibacterial spectrum toward vancomycin-resistant enterococci.
AID352090Antimicrobial activity against multidrug-resistant Klebsiella pneumoniae after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID640475Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as growth inhibition at 0.5 to 1 ug/ml by microplate alamar blue assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Antimycobacterial activities of 5-alkyl (or halo)-3'-substituted pyrimidine nucleoside analogs.
AID227925The compound was estimated for biosensor analysis2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels.
AID530868Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB N474K mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1212145Induction of CYP2C9 in human hepatocytes at 10 uM after 72 hrs relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1174120Antimicrobial activity against Mycobacterium tuberculosis H37Rv by two-fold serial dilution method2015European journal of medicinal chemistry, Jan-07, Volume: 89Synthesis and evaluation of in vitro antimycobacterial activity of novel 1H-benzo[d]imidazole derivatives and analogues.
AID368651Terminal apparent distribution volume in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID718939Antitubercular activity against non-culturable Mycobacterium tuberculosis assessed as reduction in dormant cell viability at 10 ug/mL measured for 7 days by MPN assay2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
AID1390095Antimycobacterial activity against nutrient starved dormant form of Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial count at 10 ug/ml measured after 7 days by MNP assay relative to control2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis and evaluation of 4',5'-dihydrospiro[piperidine-4,7'-thieno[2,3-c]pyran] analogues against both active and dormant Mycobacterium tuberculosis.
AID532963Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 72010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1888141Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial colony forming units at 20 times MIC concentration measured after 21 days by by time kill assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID373955Ratio of Cmax to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L administered for 2 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID495235Antimicrobial activity against Mycobacterium tuberculosis NJT210GCC harboring embB406 GGC-GCC(Gly-Ala) mutation in embB gene after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID1483730Selectivity ratio of MIC for Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-c D28N mutant supplemented with 4 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione to MIC for Mycobacterium tuberculosis H2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID530866Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB E473 mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID733054Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
A facile three-component [3+2]-cycloaddition for the regioselective synthesis of highly functionalised dispiropyrrolidines acting as antimycobacterial agents.
AID1215094Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID1514452Antitubercular activity against kanamycin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID571449Antibacterial activity against Enterobacter cloacae ATCC 23355 ATCC 13883 by Etest method in presence of 1 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID669182Inhibition of Mycobacterium tuberculosis RNA polymerase H445Y mutant by rolling circle transcription assay in the absence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1614907Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 16995 after 7 days by microplate alamar blue assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties.
AID1326369Antibacterial activity against Bacillus subtilis ATCC 47096 after 16 to 18 hrs by microbroth dilution assay2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
AID297513Antibacterial activity against Mycobacterium tuberculosis H37Rv at 16 ug/mL by micro plate alamar blue assay2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Lysosome and HER3 (ErbB3) selective anticancer agent kahalalide F: semisynthetic modifications and antifungal lead-exploration studies.
AID529539Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 CTG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1721020Antitubercular activity against linezolid-resistant Mycobacterium tuberculosis incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1471032Antitubercular activity against Mycobacterium bovis BCG ATCC 35743 dormant stage by nitrate reductase based two-fold dilution assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1365696Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 10 days under low oxygen condition followed by incubation under aerobic condition for 28 hrs by LORA2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID768666Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 0.125 ug/mL by BACTEC 460 radiometric assay relative to control2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Synthesis of novel isothiazolopyridines and their in vitro evaluation against Mycobacterium and Propionibacterium acnes.
AID530654Inhibition of protein synthesis in rifamycin-resistant Staphylococcus aureus CB370 harboring rpoB H481Y mutant gene assessed as L-[3,4,5-3H]leucine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID689221Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 culture in GAS media after 7 days by microplate alamar blue assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds.
AID368650AUC (24 hrs) in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID693678Antibacterial activity against Staphylococcus aureus ATCC 29213 by NCCLS method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID1212156Induction of UGT1A9 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1879492Antibacterial activity against Clostridioides difficile clinical isolate China2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID362655Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by MTT assay after 4 days by MTT assay2008Journal of natural products, Sep, Volume: 71, Issue:9
Tetrahdroxysqualene from Rhus taitensis shows antimycobacterial activity against Mycobacterium tuberculosis.
AID457431Antitubercular activity against Mycobacterium tuberculosis H37Rv after 72 hrs by microplate alamar blue assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID571642Antibacterial activity against Enterobacter cloacae CCUG52947 by Etest method in presence of 4 ug/ml NAB70672008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID699544Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1256531Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 6133 by alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1285205Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 25177 assessed as growth inhibition at 40 ug/ml after 28 days by Lowenstein-Jensen method2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Novel nicotine analogues with potential anti-mycobacterial activity.
AID509621Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB522 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID520292Antimicrobial activity against Staphylococcus aureus 2549 small colony variants2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Activities of daptomycin and comparative antimicrobials, singly and in combination, against extracellular and intracellular Staphylococcus aureus and its stable small-colony variant in human monocyte-derived macrophages and in broth.
AID1695729Inhibition of human alpha-synuclein filament formation expressed in Escherichia coli BL21(DE3) cells incubated for 72 hrs by thioflavin S based fluorescence assay2019European journal of medicinal chemistry, Apr-01, Volume: 167Toward the discovery and development of effective modulators of α-synuclein amyloid aggregation.
AID571639Antibacterial activity against Klebsiella pneumoniae by Etest method in presence of 4 ug/ml NAB70642008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID583685Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315deltaIP after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1825033Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST-Fe media incubated for 8 days by resazurin microtiter assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
AID1167356Antibacterial activity against Escherichia coli D21 IpxC101/tolC deletion mutant after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID554583Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 60 mg/kg, sc administered as single dose 2 hrs after infection measured upto 19 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID425632Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as minimum drug level resulting in no detectable growth at 10'6 CFU of inoculum after 56 days by MGIT 960 susceptibility test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1542209Antimicrobial activity against Staphylococcus epidermidis ATCC 12228 incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID1812054Cytotoxicity against CHO cells2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Benzoheterocyclic Oxime Carbamates Active against
AID1406217Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1182151Ratio of MIC99 for Mycobacterium smegmatis to ratio of MIC99 for Mycobacterium smegmatis in presence of 7-hydroxy chlorpromazine2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID1063305Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay2014European journal of medicinal chemistry, Jan-24, Volume: 72Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.
AID1888130Antimycobacterial activity against rifampin resistant Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1916609Antitubercular activity against multi-drug-resistant Mycobacterium tuberculosis assessed as bacterial growth inhibition measured after 7 days by direct susceptibility assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1423480Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding after 40 to 60 mins by spect2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID531001Antimicrobial activity against Clostridium difficile isolate 48 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1634889Cytotoxicity against mouse NIH/3T3 cells assessed as cell survival rate at 16 uM after 24 hrs by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID1716719Antibacterial activity against Pseudomonas aeruginosa 101243 assessed as fractional inhibitory concentration index in presence of chloramphenicol incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1069167Antimicrobial activity against ofloxacin-resistant Mycobacterium tuberculosis H37Rv SRI 4000 assessed as growth inhibition after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1459056Antitubercular activity against Mycobacterium tuberculosis H37Ra harboring pTYOK in UAIRa broth culture assessed as concentration required to reduce relative luminescence unit to <10% measured after 4 days by autoluminescence assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
AID1716657Antibacterial activity against Stenotrophomonas maltophilia CAN-ICU 62584 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1401980Antimycobacterial activity against fluoroquinolone-resistant Mycobacterium tuberculosis H37Rv FQ-R1 harboring unidentified mutation2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID1412765Antimycobacterial activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 by XRMA2018MedChemComm, Jul-01, Volume: 9, Issue:7
Triazole-diindolylmethane conjugates as new antitubercular agents: synthesis, bioevaluation, and molecular docking.
AID1418316Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv
AID370073Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35820 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1403702Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 1 week by MABA method2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1326670Inhibition of Mycobacterium smegmatis 155 6His-tagged DNA gyrase B catalytic domain ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as inorganic phosphate release after 120 mins in presence of ATP by malachite green dye based2016European journal of medicinal chemistry, Oct-21, Volume: 122Engineering another class of anti-tubercular lead: Hit to lead optimization of an intriguing class of gyrase ATPase inhibitors.
AID1182142Antitubercular activity against Mycobacterium smegmatis by checkerboard assay in presence of nor-chlorpromazine2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID1596590Resistance index, ratio of MIC for antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 treated repeatedly over 9 passages to MIC for antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 treated fo2019European journal of medicinal chemistry, Aug-01, Volume: 175Lipophilic efficient phenylthiazoles with potent undecaprenyl pyrophosphatase inhibitory activity.
AID370236AUC (0 to t) in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1716869Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID373048Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate FZ84 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID571417Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 8 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1692251Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 7 days by MABA assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Identification of benzothiazinones containing 2-benzyl-2,7-diazaspiro[3.5]nonane moieties as new antitubercular agents.
AID1212159Induction of MRP1 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID324988Antibacterial activity against Haemophilus influenzae MSC06663 by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID445332Selectivity for Mycobacterium tuberculosis H37Rv over human THP1 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID571396Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 0.125 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1298603Antibacterial activity against Escherichia coli after 24 hrs by agar diffusion assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.
AID495512Antibacterial activity against multidrug-resistant Acinetobacter baumannii BM4666 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID103853In vitro activity of compound against slowly growing Mycobacterium xenopi 5541990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID693672Antibacterial activity against Staphylococcus aureus isolate 722 obtained from veterinary sample after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID373977Volume of distribution in central compartment in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1542211Antimicrobial activity against Enterococcus faecalis ATCC 29212 incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID1459062Antitubercular activity against fluoroquinolone resistant Mycobacterium tuberculosis H37Rv harboring gyrB D94N mutant after 5 days2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
AID326281Antibacterial activity against methicillin-resistant Staphylococcus aureus 4913 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID1908129Antibacterial activity against multi-drug resistant Acinetobacter baumannii ATCC 19606 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID569255Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1329993Antitubercular activity against Mycobacterium tuberculosis H37Ra transfected with TYOK plasmid assessed as relative light units after 4 days by selectable marker-free autoluminescent assay2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis.
AID235897Selectivity index (IC50/MIC) was determined2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID581198Effect on iNOS expression in human DLD1 cells assessed as increase in 100 ng/ml IL1-beta, TNF-alpha and IFN-gamma-stimulated iNOS mRNA expression normalized to beta-actin expression level at 10 to 50 ug/ml after 24 hrs by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID582993Antimicrobial activity against Enterococcus faecium BM-0661 transconjugant by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1143268Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis 19000 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID1193496Thermodynamic equilibrium solubility, log S of the compound in water at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1471057Selectivity index, ratio of GI50 for human PANC1 cells to MIC for Mycobacterium bovis BCG ATCC 35743 dormant stage2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID544636Antimicrobial activity against Staphylococcus aureus Xen 30 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID560973Antimicrobial activity against methicillin-resistant Staphylococcus aureus 494 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID372464Antimalarial activity as 3rd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs dose then 48 hrs drug-free2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1706089Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by MABA assay
AID1603259Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC>=90 for Mycobacterium tuberculosis H37Rv
AID545600Bactericidal activity against stationary-phase vancomycin-resistant Staphylococcus aureus isolate VRS5 grown on nutrient-depleted CAMHB medium at 4 ug/ml after 24 hrs by time kill analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID572543AUC (0 to 24 hrs) in south african pulmonary tuberculosis patient with body weight <=50 kg at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1600419Agonist activity at human PXR in human primary hepatocytes assessed as increase in CYP3A4 gene expression at 10 uM incubated for 24 hrs by RT-PCR analysis2019ACS medicinal chemistry letters, Jul-11, Volume: 10, Issue:7
DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor.
AID1856875Antimicrobial activity against Escherichia coli ATCC 25922 in presence of NaCl2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID588219FDA HLAED, gamma-glutamyl transferase (GGT) increase2004Current drug discovery technologies, Dec, Volume: 1, Issue:4
Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
AID677625Antitubercular activity against highly drug-resistant, non replicating, persistent Mycobacterium tuberculosis harboring Vibrio harveyii luciferase gene incubated under anaerobic condition measured after 28 hrs of aerobic recovery by LORA method2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Structural requirements for the antitubercular quaternized triflupromazine pharmacophore.
AID419832Antibacterial activity against Escherichia coli MTCC 722 after 24 hrs by liquid dilution method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID1333272Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 2 times MIC measured after 3 hrs by luciferase reporter gene assay (Rvb = 158.3%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1070203Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1756892Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC27294 measured after 28 days by two-fold serial dilution method2021European journal of medicinal chemistry, Apr-05, Volume: 215Antitubercular properties of thiazolidin-4-ones - A review.
AID405146Ratio of apparent clearance at 600 mg, po to apparent clearance at 450 mg, po in tuberculosis patient2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1406778Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition at 25 ug/ml after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.
AID373027Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PUA6 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID577204Antimicrobial activity against Escherichia coli O157:H7 PT-40 in stationary phase encoding Stx-2 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID1296395Cytotoxicity against human HuH7 cells assessed as cell viability after 24 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID774601Cytotoxicity against human HepG2/C3A cells after 24 hrs by neutral red dye uptake assay2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID1127155Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 24 hrs by Lowenstein-Jensen agar dilution method2014European journal of medicinal chemistry, May-22, Volume: 79Facile synthesis of benzonitrile/nicotinonitrile based s-triazines as new potential antimycobacterial agents.
AID368643AUC (24 hrs) in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID574553Decrease in PSMbeta1 levels in Staphylococcus aureus Sanger 252 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID1399586Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 16833 after 7 days by microplate alamar blue assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and evaluation of oxime-functionalized nitrofuranylamides as novel antitubercular agents.
AID1400019Antibacterial activity against Staphylococcus aureus incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1827051Antibacterial activity against Salmonella enterica ATCC 13311 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID576112Antimicrobial activity against mecA-positive Staphylococcus sciuri harboring staphylococcus aureus mecA gene assessed as resistant isolates2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Nasal carriage of methicillin-resistant and methicillin-sensitive strains of Staphylococcus sciuri in the Indonesian population.
AID425397Antibacterial activity against Escherichia coli isolates isolated from patients with Crohn's disease at 5 ug/disk by susceptibility testing disk method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID530798Antimicrobial activity against Clostridium difficile isolate 29 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1626607Antimicrobial activity against Staphylococcus aureus isogenic forms expressing parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID560500Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate sh06024 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1400049Bactericidal activity against Enterococcus faecalis ATCC 19433 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1323723Growth inhibition of Mycobacterium bovis BCG at 0.5 ug/ml after 6 days by microplate alamar blue assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents.
AID1061928Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 3 weeks by microbroth dilution method2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and evaluation of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-(2-(4-substitutedpiperazin-1-yl)acetyl)piperazin-1-yl)quinoline-3-carboxylic acid derivatives as anti-tubercular and antibacterial agents.
AID1500591Antitubercular activity against Mycobacterium tuberculosis RIF-R1 harboring rpoB S522L mutant after 5 days by fluorescence-based assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID1218864Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID677627Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Structural requirements for the antitubercular quaternized triflupromazine pharmacophore.
AID1603257Antibacterial activity against INH-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay
AID1879549Antibacterial activity against metronidazole-resistant Bacteroides thetaiotaomicron MMX 34092022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID388899Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 32 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID1182153Ratio of MIC99 for Mycobacterium smegmatis to ratio of MIC99 for Mycobacterium smegmatis in presence of nor-chlorpromazine2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID1069165Bactericidal activity against Mycobacterium tuberculosis H37Rv SRI 1345 after 18 to 24 hrs2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID564130Antimicrobial activity against methicillin-resistant Staphylococcus aureus HUSA 304 infected in Wistar rat assessed as decrease in bacterial load in tissue cage fluid at 35 mg/kg, ip administered every 12 hrs for 7 days measured on day 8 post treatment2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID1692253Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16995 clinical isolate assessed as inhibition of bacterial growth incubated for 7 days by MABA assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Identification of benzothiazinones containing 2-benzyl-2,7-diazaspiro[3.5]nonane moieties as new antitubercular agents.
AID1743134Inhibition of ATP synthase in multi-drug resistant Mycobacterium tuberculosis clinical isolate 14862 assessed as reduction in bacterial growth incubated for 7 days by microplate alamar blue assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
AID1832329Antitubercular activity against wild type Mycobacterium tuberculosis HN878 assessed as bacterial growth inhibition measured after 5 days by serial dilution method2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel C-3-(N-alkyl-aryl)-aminomethyl rifamycin SV derivatives exhibit activity against rifampicin-resistant Mycobacterium tuberculosis RpoB
AID1653392Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.3 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1653510Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1406215Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days
AID1381931Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2018European journal of medicinal chemistry, Feb-25, Volume: 146New hydrazides derivatives of isoniazid against Mycobacterium tuberculosis: Higher potency and lower hepatocytotoxicity.
AID1483729Selectivity ratio of MIC for Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-a K179N mutant supplemented with 4 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione to MIC for Mycobacterium tuberculosis 2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1632657Antitubercular activity against active Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells after 8 days by nitrate reductase assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID530636Antimicrobial activity against Staphylococcus aureus CB370 harboring rifampin-resistant rpoB H481Y mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID571211Antibacterial activity against Acinetobacter baumannii F264 by Etest method in presence of NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1668181Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID278859Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID481723Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in GAS medium after 1 week by microplate alamar blue assay2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Structure-activity relationship of new anti-tuberculosis agents derived from oxazoline and oxazole benzyl esters.
AID1653516Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID560522Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gz07030 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1164295Antimicrobial activity against Mycobacterium tuberculosis overexpressing DprE1 assessed as growth inhibition after 5 days by microdilution method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1729225Antibacterial activity against multidrug-resistant Escherichia coli BW25113 harboring AcrB deletion mutant by two-fold broth dilution method2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and structural optimization of novel 2H-benzo[h]chromene derivatives that target AcrB and reverse bacterial multidrug resistance.
AID1303882Antibacterial activity against multidrug resistant Staphylococcus aureus subsp. aureus Seattle 1945 (ATCC 25923) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID1557229Antitubercular activity against resistant Mycobacterium tuberculosis 1 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID729922Cytotoxicity against african green monkey Vero cells assessed as growth inhibition after 24 hrs by MTS assay2013European journal of medicinal chemistry, Apr, Volume: 62Synthesis and biological evaluation of a new class of 4-aminoquinoline-rhodanine hybrid as potent anti-infective agents.
AID531270Antimicrobial activity against Clostridium difficile isolate 42 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID326291Antibacterial activity against methicillin-resistant Staphylococcus aureus 4913 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID446154Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.
AID1678514Antibacterial activity against Clostridium difficile 5680 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1668268Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth by broth dilution method2020Journal of natural products, 05-22, Volume: 83, Issue:5
Antitubercular Ilamycins from Marine-Derived
AID445287Antibacterial activity against Mycobacterium avium SmO by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1220554Fraction unbound in Wistar Han rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1194224Tuberculostatic activity against Mycobacterium tuberculosis Spec. 210 by two-fold classical test-tube method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel 2-(2-phenalkyl)-1H-benzo[d]imidazoles as antitubercular agents. Synthesis, biological evaluation and structure-activity relationship.
AID753132Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 2 to 3 weeks by broth microdilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID541084Antibacterial activity against 1 x10'6 to 5 x10'6 CFU/ml methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as percent resistant isolates at MIC after 24 hrs by time kill study2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1137532Antitubercular activity against 1-ethyl-3-(6-(pyrimidin-5-yl)-5-((tetrahydrofuran-3-yl)methoxy)thiazolo[5,4-b]pyridin-2-yl)urea-resistant Mycobacterium tuberculosis H37Rv clone 8.2 harboring DNA gyraseB ATP domain Ala92Ser mutant assessed as growth inhibi2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B.
AID1565703Antibacterial activity against Escherichia coli ATCC 25922 at 0.5 times MIC incubated for 18 hrs measured at 1 passages by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID392610Antimycobacterial activity against 6-week-starved culture of Mycobacterium smegmatis ATCC 14468 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1908117Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID582268Ratio of MIC for Bacillus cereus ATCC 4342 selected after 20 daily cycles of drug selection followed by 5 days of nonselective growth to MIC for Bacillus cereus ATCC 43422008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Efficacy of oritavancin in a murine model of Bacillus anthracis spore inhalation anthrax.
AID1372631Antibacterial activity against non replicating Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial count at 10 ug/ml incubated for 7 days followed by compound dilution measured after 4 weeks2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1736314Antitubercular activity against INH, SM, RFP, EMB, PAS, Prothionamide 1321, Capreomycin-resistant Mycobacterium tuberculosis 14862 assessed as inhibition of bacterial growth2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis.
AID1473739Inhibition of human MRP2 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1311275Cytotoxicity against human THP1 cells by MTT assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1262574Antimicrobial activity against clinical isolates of Mycobacterium tuberculosis SAWC 2371 Haarlem under 7H9 medium assessed as growth inhibition after 14 days by alamar blue assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID562795Antimicrobial activity against Chlamydia muridarum MoPn/oflR-rifR harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID143714In vitro antibacterial activity against Mycobacterium avium 1033171999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID392601Antimycobacterial activity against Mycobacterium microti MTCC 1727 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID560503Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 6zjsau7 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1069157Cytotoxicity against mouse J774 cells assessed as cell viability at 10-fold above MIC relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1861551Induction of CYP3A4 (unknown origin) at 10 uM2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Discovery and SAR of 4-aminopyrrolidine-2-carboxylic acid correctors of CFTR for the treatment of cystic fibrosis.
AID1566202Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis H37Rv harbouring DprE1 C387G mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1062059Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin assay2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and characterization of new N-(4-(4-chloro-1H-imidazol-1-yl)-3-methoxyphenyl)amide/sulfonamide derivatives as possible antimicrobial and antitubercular agents.
AID1252463Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition incubated for 7 days by microplate alamar blue assay2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID1334253Cytotoxicity against human HCT116 cells by MTT assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1706099Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 assessed as inhibition of bacterial growth by agar plate dilution method
AID362653Antimycobacterial activity against Mycobacterium tuberculosis H37Ra after 4 days by MTT assay2008Journal of natural products, Sep, Volume: 71, Issue:9
Tetrahdroxysqualene from Rhus taitensis shows antimycobacterial activity against Mycobacterium tuberculosis.
AID1182147Ratio of MIC99 for Mycobacterium smegmatis to ratio of MIC99 for Mycobacterium smegmatis in presence of chlorpromazine2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID534109Ratio of MIC for Pasteurella multocida AL435 to MIC for TolC deficient Pasteurella multocida pm05272008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1705564Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 10 to 14 days2020European journal of medicinal chemistry, Dec-15, Volume: 208Synthesis and evaluation of thiophene based small molecules as potent inhibitors of Mycobacterium tuberculosis.
AID1311270Selectivity index, ratio of CC50 for human HeLa cells to MIC for active stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID545932Antimicrobial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 2 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1459060Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis H37Rv harboring rpoB S522L mutant after 5 days2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
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A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
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Design, synthesis and antimycobacterial activity of hybrid molecules combining pyrazinamide with a 4-phenylthiazol-2-amine scaffold.
AID1337866Selectivity index, ratio of GI50 for PMP-differentiated human THP1 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1447549Antibacterial activity against multidrug-resistant Enterobacter cloacae 117029 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
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In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
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Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
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Membrane transporters in drug development.
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Synthesis and biological activity of some derivatives of rifamycin P.
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Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
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Assessment of the health effects of chemicals in humans: II. Construction of an adverse effects database for QSAR modeling.
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Contributions of arylacetamide deacetylase and carboxylesterase 2 to flutamide hydrolysis in human liver.
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Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases.
AID1293902Cytotoxicity against human HeLa cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1359452Antitubercular activity against multidrug-resistant active stage of Mycobacterium tuberculosis H37Ra after 8 days by XRMA2018European journal of medicinal chemistry, May-25, Volume: 152Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life.
AID1908131Antibacterial activity against NDM-1 expressing Klebsiella pneumoniae ATCC BAA 2470 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
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AID1879576Antibacterial activity against Treponema denticola ATCC 354052022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
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Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
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Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
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Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
AID1869576Bactericidal activity against Enterobacter cloacae DSM 30054 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID1399840Antibacterial activity against Mycobacterium tuberculosis H37Rv2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID419831Antibacterial activity against Staphylococcus aureus MTCC 96 after 24 hrs by liquid dilution method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID1247198Anti-tubercular activity against rifampicin, isoniazid, ethambutol and pyrazinamide-sensitive active phage of Mycobacterium tuberculosis H37Ra ATCC 25177 by serial dilution method2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Design and synthesis of 11α-substituted bile acid derivatives as potential anti-tuberculosis agents.
AID1447547Antibacterial activity against multidrug-resistant Acinetobacter baumannii AB031 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID531295Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 67 expressing RpoB H502N and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID408877Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID1463955Antimycobacterial activity against Mycobacterium kansasii 6509/96 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID774606Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene assessed as growth inhibition at 10 uM after 6 days by luminometry relative to control2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID1316985Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in Balb/c mouse assessed as bacterial burden in lungs at 10 mg/kg, po administered daily through gavage starting on day 2 post infection for 4 days per week for 2 weeks measured 2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification and optimization of a new series of anti-tubercular quinazolinones.
AID1727228Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay2021European journal of medicinal chemistry, Jan-01, Volume: 209Anti-tuberculosis activity and its structure-activity relationship (SAR) studies of oxadiazole derivatives: A key review.
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Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
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Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
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Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
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Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
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Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
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AID588126Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 4 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
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Design, Syntheses, and Anti-TB Activity of 1,3-Benzothiazinone Azide and Click Chemistry Products Inspired by BTZ043.
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A new naphthopyrone derivative from Cassia quinquangulata and structural revision of quinquangulin and its glycosides.
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Interference with bile salt export pump function is a susceptibility factor for human liver injury in drug development.
AID1311272Antimycobacterial activity against dormant stage of Mycobacterium bovis BCG ATCC 35734 measured on day 12 by nitrate reductase assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1316915Antimycobacterial activity against dormant stage of Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth under nutrient starved conditions at 10 ug/ml for 7 days measured after 28 days2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
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5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1626623Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
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High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1716654Antibacterial activity against gentamicin, tobramycin, ciprofloxacin-resistant Escherichia coli ATCC 97615 harboring aac(3')IIa gene assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID634277Antimycobacterial activity against Mycobacterium tuberculosis isolate 349 expressing rpoB mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID405150Ratio of AUC (0 to 24 hrs) at 600 mg, po to AUC (0 to 24 hrs) at 450 mg, po in tuberculosis patient2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1400042Antibacterial activity against Staphylococcus aureus BAA 1683 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID780895Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis ATCC 35338 harboring rpoB His-526-Tir gene mutant after 7 days by REMA assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids.
AID1685706Antimicrobial activity against Escherichia coli K-12 assessed as inhibition of bacterial growth incubated for overnight by CLSI method2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Hydraphiles enhance antimicrobial potency against Escherichia coli, Pseudomonas aeruginosa, and Bacillus subtilis.
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[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
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Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
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Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
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Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
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Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
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Synthesis and biological activity of some derivatives of rifamycin P.
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Compounds of Alpinia katsumadai as potential efflux inhibitors in Mycobacterium smegmatis.
AID1287500Antitubercular activity against active state Mycobacterium tuberculosis H37Ra assessed as viable cells after 8 days by XTT reduction menadione assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
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Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
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Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
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Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
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Anti-mycobacterial activities of some cationic and anionic calix[4]arene derivatives.
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Synthesis and biological activity of some derivatives of rifamycin P.
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Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1688940Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as reduction in microbial growth after 7 days by Alamar blue assay2020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.
AID1326388Antibacterial activity against Bacillus subtilis P10A derived after 10 passage in presence of JBIR-100 after 16 to 18 hrs by microbroth dilution assay relative to Bacillus subtilis ATCC 470962016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
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Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
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Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID1055969Antimycobacterial activity against Mycobacterium tuberculosis H37Rv under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
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OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
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AID1497866Antibacterial activity against Shigella dysenteriae PTCC 11882018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
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Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1653517Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.4 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
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Continuous clindamycin infusion, an innovative approach to treating bone and joint infections.
AID1759476Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis.
AID1071101Antimycobacterial activity against Mycobacterium tuberculosis H37Rv SRI 1345 after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID545920Antimicrobial activity against Escherichia coli IH3080 by Etest method in presence of 2 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
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Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
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1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
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Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
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Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties.
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From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters.
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Diguanidino and "reversed" diamidino 2,5-diarylfurans as antimicrobial agents.
AID1577329Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis Praha 4 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
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Synthesis and antimycobacterial properties of ring-substituted 6-hydroxynaphthalene-2-carboxanilides.
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Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
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Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
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(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
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Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID644321Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 7 days by resazurin assay2012European journal of medicinal chemistry, Mar, Volume: 49Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents.
AID1688198Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by MABA assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.
AID634276Antimycobacterial activity against Mycobacterium tuberculosis isolate 311 expressing rpoB mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1854286Antitubercular activity against clinical isolate streptomycin-resistant Mycobacterium tuberculosis ATCC 35820 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID323254Antimicrobial activity against carbapenem-intermediate or resistant Acinetobacter baumannii isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of various antimicrobials alone and in combination with tigecycline against carbapenem-intermediate or -resistant Acinetobacter baumannii.
AID765113Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 1 ug/mL relative to control2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1436935Selectivity index, ratio of GI90 for human HCT116 cells to MIC90 for dormant state of Mycobacterium tuberculosis H37Ra2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID1516027Antibacterial activity against Acinetobacter baumannii AB1902 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID79580In vitro antibacterial activity of compound against Haemophilus influenzae ATCC 194181990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1668174Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID1585115Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA2018European journal of medicinal chemistry, Dec-05, Volume: 160Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
AID1862201Antimycobacterial activity against clinical isolate drug susceptible Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
AID373943AUC in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model after 7 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID541030Induction of apoptosis in bovine BL3 cells assessed as late apoptotic cells after 24 hrs by annexin V/propidium iodide staining-based FACS analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Theileria apicoplast as a target for chemotherapy.
AID368767Induction of voriconazole metabolism in po dosed bacterial infection patient assessed as increase in dihydroxyvoriconazole levels after 30 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Induction of voriconazole metabolism by rifampin in a patient with acute myeloid leukemia: importance of interdisciplinary communication to prevent treatment errors with complex medications.
AID559762Antimycobacterial activity against Mycobacterium smegmatis MAR4 harboring disrupted PknGMsm gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID565808Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB34 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID571646Antibacterial activity against Acinetobacter baumannii by Etest method in presence of 4 ug/ml NAB70712008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1326387Antibacterial activity against Bacillus subtilis P10C derived after 10 passage in presence of JBIR-100 after 16 to 18 hrs by microbroth dilution assay2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
AID1359861Inhibition of recombinant human AChE-induced amyloid beta (1 to 42) aggregation at 100 uM incubated for 48 hrs by thioflavin-T fluorescence assay relative to control2018European journal of medicinal chemistry, May-25, Volume: 152Design, synthesis and evaluation of novel multi-target-directed ligands for treatment of Alzheimer's disease based on coumarin and lipoic acid scaffolds.
AID555303Antibacterial activity against methicillin-resistant Staphylococcus aureus 145 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID571208Antibacterial activity against Pseudomonas aeruginosa ATCC 27853by Etest method in presence of 0.25 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID571391Antibacterial activity against Acinetobacter baumannii F264 by Etest method in presence of 0.125 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID626920Growth inhibition of Mycobacterium tuberculosis H37Rv ATCC 27294 using compound level ranging from 1 to 100 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID1383958Ratio of MBC to MIC for MDR Mycobacterium tuberculosis isolate 5912018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID689771Antitubercular activity against Mycobacterium tuberculosis H37Rv isolate ITR after 7 days by luminescence spectrometry2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis.
AID1311279Selectivity index, ratio of CC50 for human THP1 cells to MIC for active stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID279813Antimicrobial activity against Escherichia coli DH5-alpha pYW1 transformants expressing KPC2 gene by agar dilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Plasmid-mediated KPC-2 in a Klebsiella pneumoniae isolate from China.
AID1071097Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv SRI 1369 at MIC after 7 days by broth microdilution assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID509958Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 24 hrs by BACTEC radiometric susceptibility assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
A bioactive labdane diterpenoid from Curcuma amada and its semisynthetic analogues as antitubercular agents.
AID1397223Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by Alamar blue assay2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties.
AID1497865Antibacterial activity against Klebsiella pneumoniae ATCC 100312018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID1296452Inhibition of RNA biosynthesis in Mycobacterium tuberculosis H37Ra assessed as reduction of [14C]-uracil incorporation at 0.05 ug/ml preincubated for 1 hr followed by radiolabeling with [14C]-uracil for 24 hrs by scintillation spectrometry2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID571428Antibacterial activity against Pseudomonas aeruginosa ATCC 27853by Etest method in presence of 0.5 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID745299Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 12 to 28 days by Lowenstein-Jensen method2013European journal of medicinal chemistry, May, Volume: 63Synthesis and identification of β-aryloxyquinoline based diversely fluorine substituted N-aryl quinolone derivatives as a new class of antimicrobial, antituberculosis and antioxidant agents.
AID1879525Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1893 harboring rpoBL525I/D530N/rdxAR16S mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1273398Anti-tubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294T after 7 days by mircodilution method2016European journal of medicinal chemistry, Jan-01, Volume: 107Hybrid triazoles: Design and synthesis as potential dual inhibitor of growth and efflux inhibition in tuberculosis.
AID1276362Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 by XTT Reduction Menadione Assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID1691023Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 1 week by microplate alamar blue assay2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID530349Antimicrobial activity against Escherichia coli TOP10 harboring pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID1061100Antimicrobial activity against Candida albicans2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID580617Inhibition of RNA synthesis in Bacillus subtilis BD54 at 5 X MIC by [5-3H]uridine incorporation assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.
AID1436937Selectivity index, ratio of GI90 for human A549 cells to MIC90 for dormant state of dormant state of Mycobacterium bovis BCG2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID557090Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 0.1% alpha-1-acid glycoprotein2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID557208Antibacterial activity against Beta-lactamase-negative Neisseria meningitidis by Etest method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antibiotic susceptibility and characteristics of Neisseria meningitidis isolates from the African meningitis belt, 2000 to 2006: phenotypic and genotypic perspectives.
AID1497851Antibacterial activity against Bacillus subtilis ATCC 6633 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID292287Antibacterial activity against Escherichia coli ATCC 25922 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID370072Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35837 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID565780Antimicrobial activity against Neisseria meningitidis harboring rpoB14 S548F mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1143264Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID682059TP_TRANSPORTER: RT-PCR in HepG2 cells2001Toxicology letters, Mar-31, Volume: 120, Issue:1-3
Up-regulation of transporters of the MRP family by drugs and toxins.
AID1383954Antimycobacterial activity against MDR Mycobacterium tuberculosis isolate 591 after 15 days by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID531255Antimicrobial activity against Clostridium difficile isolate 27 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1163985Antimycobacterial activity against isoniazid and rifampicin resistant Mycobacterium tuberculosis 11277 by MABA method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1542210Antimicrobial activity against Staphylococcus epidermidis ATCC 49134 incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID404136Antibacterial activity against lpxC mutant gene expressing Escherichia coli MB49022005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID1061102Antimicrobial activity against Mycobacterium smegmatis2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID1516023Antibacterial activity against Escherichia coli ATCC 25922 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1705563Inhibition of RNA polymerase in Staphylococcus aureus ATCC 29213 assessed as reduction in total protein level at 1/4 to 1/8 times MIC by fluorimetric method2020European journal of medicinal chemistry, Dec-15, Volume: 208Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction.
AID545938Ratio of MIC for Enterobacter cloacae ATCC 23355 to MIC for Enterobacter cloacae ATCC 23355 in presence of 4 ug/ml of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1183263Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of colony formation at 250 ug/ml after 4 weeks of incubation2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis and characterization of fluoro substituted novel pyrazolylpyrazolines scaffold and their pharmacological screening.
AID1891915Antimycobacterial activity against Mycobacterium chelonae ATCC 6841 assessed as inhibition of bacterial growth after 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1463957Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate Praha 4 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1070200Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 35820 by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID278681Antibacterial activity against Enterococcus faecium isolate 57522007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1457507Antibacterial activity against Bacillus subtilis assessed as inhibition of RNA synthesis at 2 mg/L after 50 mins by [3H]-uridine incorporation assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents.
AID562793Antimicrobial activity against Chlamydia trachomatis L2/oflR-rifR2 harboring ampA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1691028Antitubercular activity against 6-weeks nutrient starved phase cultures of Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial growth at 10 uM treated for 7 days measured after 4 weeks relative to control2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID611487Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 124 isolated from patient open wound after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID1294365Antimicrobial activity against non-replicating Mycobacterium tuberculosis H37Rv SRI 1345 assessed as inhibition of visual growth incubated for 7 days under anaerobic condition by low oxygen recovery assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID285156Antimicrobial activity against Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Clonal diversity and resistance mechanisms in tetracycline-nonsusceptible Streptococcus pneumoniae isolates in Poland.
AID1467461Antibacterial activity against methicillin resistant Staphylococcus aureus MRSA090 at 100 ug/ml after 24 hrs by agar well diffusion method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID1772309Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.1 cells assessed as change in bacterial colony forming units at 5 ug/ml incubated for 3 days
AID531021Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 68 expressing RpoB H502Y mutant by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1736312Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis.
AID1504967Cytotoxicity against African green monkey Vero cells after 72 hrs by MTS/PMS assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID1055935Antimycobacterial activity against Mycobacterium tuberculosis harboring luxABCDE under hypoxic condition after 10 days by MABA assay in presence of 10% fetal bovine serum2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID565777Antimicrobial activity against Neisseria meningitidis harboring rpoB11 H552N mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1400034Bactericidal activity against replicating Mycobacterium tuberculosis H37Rv incubated for 15 days under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1510686Antitubercular activity against multidrug resistant Mycobacterium tuberculosis isolate 9160 assessed as parasite growth inhibition measured after 7 days incubation by microplate alamar blue assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents.
AID1832328Antitubercular activity against wild type Mycobacterium tuberculosis H37Rv ATCC 25618 assessed as bacterial growth inhibition measured after 5 days by serial dilution method2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel C-3-(N-alkyl-aryl)-aminomethyl rifamycin SV derivatives exhibit activity against rifampicin-resistant Mycobacterium tuberculosis RpoB
AID704584Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as disruption of membrane potential at 0.4 ug/ml after 20 mins at pH 7.4 by DiOC2-based spectrofluorimetric analysis
AID440894Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis by agar dilution method2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
L-proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines.
AID1471051Growth inhibition of human PANC1 cells by MTT assay2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1334252Cytotoxicity against human MCF7 cells by MTT assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID523654Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta' after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID680918TP_TRANSPORTER: Western in vivo, quantitative immunohistochemistry1999The Journal of clinical investigation, Jul, Volume: 104, Issue:2
The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin.
AID1252459Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID531261Antimicrobial activity against Clostridium difficile isolate 33 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1152777Antimycobacterial activity against 5-(((3S,4R)-3-Fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA D89N mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1244820Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by serial microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID373040Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate ZJ58 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1210908Intrinsic clearance in rat Liver microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID545916Antimicrobial activity against Escherichia coli ATCC 25922 by Etest method in presence of 2 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID727918Antibacterial activity against Micrococcus luteus ATCC 9341 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID727791Antifungal activity against Candida albicans ATCC 10231 after 48 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID1879569Antibacterial activity against metronidazole-resistant Prevotella asaccharolytica MMX 35522022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1879536Antibacterial activity against fluoroquinolone-resistant Clostridioides difficile CB1939 at 1:1 compound to metronidazole molar ratio measured after 3 days in presence of metronidazole2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID313236Antimicrobial activity against Mycobacterium smegmatis at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID103841In vitro activity of compound against slowly growing Mycobacterium scrofulaceum 13011990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID285557Bactericidal activity against 19-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 11 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID289152Antimycobacterial activity against streptomycin, isoniazid, ethambutol-resistant Mycobacterium tuberculosis CIBIN 112 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID1775046Displacement of BODIPY FL vindoline from GST-tagged human PXR LBD incubated for 60 mins by TR-FRET assay
AID1759473Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate alamar blue assay2021European journal of medicinal chemistry, Jun-05, Volume: 218Design, synthesis and biological activity of N-(amino)piperazine-containing benzothiazinones against Mycobacterium tuberculosis.
AID694356Antibacterial activity against Mycobacterium tuberculosis H37Rv under anaerobic condition assessed as growth inhibition at 1 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID656231Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1688942Selectivity index, ratio of IC50 for cytotoxicity against African green monkey Vero cells to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 251772020European journal of medicinal chemistry, Mar-01, Volume: 189Synthesis and antimycobacterial activity of thiazolidine-2,4-dione based derivatives with halogenbenzohydrazones and pyridinecarbohydrazones substituents.
AID1493794Ratio of MIC for methicillin-resistant Staphylococcus aureus USA300 NRS384 after 14 passages to MIC for methicillin-resistant Staphylococcus aureus USA300 NRS384 before passage2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID413208Induction of CYP3A4 in cryopreserved human hepatocytes from female NPV donars with history of tobacco and substance usage assessed as mRNA expression at 20 uM relative to 20 uM rifampin2008Journal of medicinal chemistry, Dec-25, Volume: 51, Issue:24
Further studies with the 2-amino-1,3-thiazol-4(5H)-one class of 11beta-hydroxysteroid dehydrogenase type 1 inhibitors: reducing pregnane X receptor activity and exploring activity in a monkey pharmacodynamic model.
AID679360TP_TRANSPORTER: inhibition of Salicylate uptake (salicylate: 1 uM, Rifampicin: 1000 uM) in Xenopus laevis oocytes1998FEBS letters, Jun-12, Volume: 429, Issue:2
Identification of multispecific organic anion transporter 2 expressed predominantly in the liver.
AID1777209Agonist activity at human PXR transfected in human HEK293T cells co-transfected with CYP3A4-Luc plasmid incubated for 24 hrs by dual-luciferase reporter gene assay2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Lathyrane Diterpenoids as Novel hPXR Agonists: Isolation, Structural Modification, and Structure-Activity Relationships.
AID1315652Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured daily for 8 days by GFP-based fluorescence assay2016Journal of natural products, 06-24, Volume: 79, Issue:6
Lovastatin Analogues from the Soil-Derived Fungus Aspergillus sclerotiorum PSU-RSPG178.
AID424330Antimicrobial activity against Dialister invisus assessed as susceptibility breakpoint by CLSI method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID1224744Antitubercular activity against Mycobacterium tuberculosis H37Rv at 250 ug/ml2014European journal of medicinal chemistry, Aug-18, Volume: 83Ultrasound-assisted one-pot four-component synthesis of novel 2-amino-3-cyanopyridine derivatives bearing 5-imidazopyrazole scaffold and their biological broadcast.
AID681463TP_TRANSPORTER: increase in Vinblastine intracellular accumulation (Vinblastine: 0.0125 uM, Rifampicin: 200 uM) in RHC1 cells1995Biochemical pharmacology, May-11, Volume: 49, Issue:9
Rifampicin enhances anti-cancer drug accumulation and activity in multidrug-resistant cells.
AID1435648Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 1 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID531043Antimicrobial activity against Clostridium difficile isolate 10 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1562245Antimycobacterial activity against Mycobacterium smegmatis atR8 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID1888146Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse macrophage J774A.1 cell assessed as reduction in bacterial colony forming units incubated for 21 days2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID564097Bactericidal activity against stationary-phase methicillin-resistant Staphylococcus aureus HUSA 304 after 24 hrs by time kill analysis in presence of 50 mg/L calcium ions2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID530774Antimicrobial activity against Clostridium difficile isolate 5 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID577494Antimicrobial activity against methicillin-susceptible Staphylococcus aureus SH1000 by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1775050Inverse agonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs by luciferase reporter assay
AID408879Antimycobacterial activity against Mycobacterium marinum CIP 64232008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID292293Antibacterial activity against Staphylococcus aureus ATCC 25923 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID571438Antibacterial activity against Escherichia coli IH3080 by Etest method in presence of 2 ug/ml NAB70622008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID144879Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to thiacetazone (TAC)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID541031Induction of apoptosis in bovine BL3 cells assessed as necrotic after 24 hrs by annexin V/propidium iodide staining-based FACS analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Theileria apicoplast as a target for chemotherapy.
AID544824Antimicrobial activity against Staphylococcus aureus Xen 30 biofilm assessed as log10 CFU/cm'2 in bacterial count2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID555326Antibacterial activity against methicillin-resistant Staphylococcus aureus 145 after 10 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1460595Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2017Bioorganic & medicinal chemistry, 11-15, Volume: 25, Issue:22
Anti-tuberculosis activity and structure-activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives.
AID1887614Synergistic antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as fractional inhibitory concentration incubated for 24 hrs in presence of artocarpin by checkerboard method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID405161Tmax in tuberculosis patient at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1247197Anti-tubercular activity against rifampicin, isoniazid, ethambutol and pyrazinamide-sensitive dormant phage of Mycobacterium tuberculosis H37Ra ATCC 25177 by serial dilution method2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Design and synthesis of 11α-substituted bile acid derivatives as potential anti-tuberculosis agents.
AID1500592Antitubercular activity against Mycobacterium tuberculosis RIF-R2 ATCC 35828 after 5 days by fluorescence-based assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID657787Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 431 from Chinese tuberculosis patient measured 24 hrs post dose by microplate alamar blue assay2012European journal of medicinal chemistry, Jun, Volume: 52Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
AID699543Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID529885Antibacterial activity against Staphylococcus aureus RN4220 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID1055964Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate X004244 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1058222Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by BacTiter-Glo method2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID434058Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced PGE2 formation at 25 ug/ml after 48 hrs by enzyme immunoassay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1278845Antimycobacterial activity against nutrient starved Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial load for 7 days measured after 28 days by microplate reader analysis2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID531003Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 50 expressing RpoB R505K mutant by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID416847Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load at 10 mg/kg, po administered for 5 days per week measured after 8 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1278193Cytotoxicity against mouse J774 cells assessed as cell viability at 0.8 ug/ml by MTT assay2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
AID1566203Antimycobacterial activity against 1,4-azaindole resistant Mycobacterium tuberculosis H37Rv harbouring DprE1 Y314H mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1497859Antibacterial activity against Klebsiella pneumoniae ATCC 10031 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID292312Antibacterial activity Listeria monocytogenes ATCC 15313 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID558271Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 1 hr after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1504662Bactericidal activity against Mycobacterium bovis BCG ATCC 35734 assessed as reduction in membrane potential by measuring red to green fluorescent ratio at 0.08 uM measured at 20 mins to 3 hrs by DiOC2-dye based fluorescence assay2017ACS medicinal chemistry letters, Nov-09, Volume: 8, Issue:11
Indolylalkyltriphenylphosphonium Analogues Are Membrane-Depolarizing Mycobactericidal Agents.
AID1276363Antitubercular activity against Mycobacterium bovis BCG ATCC 35743 after 10 mins by NR assay2016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID1192373Antimicrobial activity against Xanthomonas campestris after 18 hrs by broth micro dilution method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.
AID1401966Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID1491287Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis MTB9160 after 7 days by microplate Alamar blue assay2017European journal of medicinal chemistry, Sep-08, Volume: 137Design, synthesis and antimycobacterial activity of novel imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID1435650Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 131 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1557230Antitubercular activity against resistant Mycobacterium tuberculosis 3 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID1197663Potentiation of antituberculosis activity against Mycobacterium marinum assessed as UBS-109-induced growth inhibition at 0.3 uM after 72 hrs by by liquid culture assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Monocarbonyl analogs of curcumin inhibit growth of antibiotic sensitive and resistant strains of Mycobacterium tuberculosis.
AID1706090Antimycobacterial activity against non-replicating Mycobacterium tuberculosis H37Rv expressing pFCA-LuxAB assessed as bacterial growth inhibition incubated for 10 days under anerobic condition by low oxygen recovery assay
AID166859Percent inhibition at a concentration of 100 ug/mL of RNA polymerase isolated from Escherichia coli K12 (Sigma)1989Journal of medicinal chemistry, May, Volume: 32, Issue:5
Aromatic dienoyl tetramic acids. Novel antibacterial agents with activity against anaerobes and staphylococci.
AID265979Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID665371Antitubercular activity against Mycobacterium tuberculosis H37Rv at 80 ug/mL by radiometric growth assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives.
AID1616315Agonist activity at PXR in human DPX2 cells at 10 uM after 24 hrs by luciferase reporter gene assay relative to control2019Journal of medicinal chemistry, 11-14, Volume: 62, Issue:21
Identification of CNS-Penetrant Aryl Sulfonamides as Isoform-Selective Na
AID1212153Induction of CYP3A5 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID380459Antibacterial activity against Bacteroides fragilis DSM 2151 by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID543819Bactericidal activity against Pseudomonas aeruginosa ATCC 27853 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID608160Agonist activity at SXR/RXR expressed in human HepG2 cells co-transfected with pGL4.10-CYP3A4 vector assessed as induction of CYP3A4 gene expression at 5 x 10'-6 M after 48 hrs by dual-luciferase reporter gene assay2011Journal of medicinal chemistry, Jul-14, Volume: 54, Issue:13
Synthesis of new vitamin K analogues as steroid and xenobiotic receptor (SXR) agonists: insights into the biological role of the side chain part of vitamin K.
AID1403710Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability at 25 uM after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID144880Antimycobacterial activity against Mycobacterium tuberculosis wild type (WT, H37Rv)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1716760Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID618417Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis and antitubercular evaluation of novel dibenzo[b,d]furan and 9-methyl-9H-carbazole derived hexahydro-2H-pyrano[3,2-c]quinolines via Povarov reaction.
AID1395690Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123 USA400 assessed as change in MIC after 9 serial passages by broth microdilution assay2018European journal of medicinal chemistry, May-10, Volume: 151Phenylthiazoles with tert-Butyl side chain: Metabolically stable with anti-biofilm activity.
AID1432970Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay
AID1869569Antibacterial activity against Klebsiella oxytoca DSM 5175 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1706092Antimycobacterial activity against Mycobacterium smegmatis mc2155 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution method
AID1265397Cytotoxicity against human LS180 cells assessed as cell viability at 10 uM after 48 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Jan-01, Volume: 107Discovery of a marine-derived bis-indole alkaloid fascaplysin, as a new class of potent P-glycoprotein inducer and establishment of its structure-activity relationship.
AID1244178Cytotoxicity against African green monkey Vero cells after 72 hrs by CCK8 assay2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
AID143106Minimal inhibitory activity of compound against Mycobacterium tuberculosis H37Rv2004Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
AID1557235Antitubercular activity against resistant Mycobacterium tuberculosis 6 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID1879067Antibacterial activity against pET28a-NDM-1 positive Escherichia coli BL21(DE3) isolates assessed as inhibition of bacterial growth incubated for 18 to 24 hrs by CLSI based broth microdilution method2022European journal of medicinal chemistry, Mar-05, Volume: 231Metallo-β-lactamases inhibitor fisetin attenuates meropenem resistance in NDM-1-producing Escherichia coli.
AID1378014Antimycobacterial activity against Mycobacterium tuberculosis MC2 62302017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID1230064Antibacterial activity against methicillin-resistant Staphylococcus aureus GRE2272 assessed as inhibition of bacterial growth2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and antimicrobial activity of chloramphenicol-polyamine conjugates.
AID529538Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 GTG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID571443Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by Etest method in presence of 1 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID739225Antitubercular activity against Mycobacterium tuberculosis Erdman ATCC 35801 infected in C57BL/6 mouse assessed as viable bacterial load in spleen at 10 mg/kg/day through gavage 5 days per week for 4 weeks starting on 10th day post-infection (Rvb = 4.79 +2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents.
AID296146Antitubercular activity against Mycobacterium tuberculosis H37Rv2007European journal of medicinal chemistry, Aug, Volume: 42, Issue:8
Synthesis of amphiphilic galactopyranosyl diamines and amino alcohols as antitubercular agents.
AID1071094Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis H37Rv SRI 4000 after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID518800Antimycobacterial activity against Mycobacterium avium serovar 4 after 14 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1167354Antibacterial activity against Escherichia coli D21 tolC deletion mutant after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1365604Antitubercular activity against Mycobacterium tuberculosis H37Rv at 100 ug/ml by broth microdilution method relative to control2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
Recently reported biological activities of pyrazole compounds.
AID1220559Fraction unbound in cynomolgus monkey brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1167359Antibacterial activity against Staphylococcus aureus ATCC 29213 expressing norA after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID454541Antitubercular activity against Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
A highly atom economic, chemo-, regio- and stereoselective synthesis and evaluation of spiro-pyrrolothiazoles as antitubercular agents.
AID1333172Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 after 5 days by broth dilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1227981Antimycobacterial activity against GFP expressing Mycobacterium tuberculosis H37Ra assessed as microbial growth inhibition incubated at 37 degC for 7 days by fluorescence based assay2015Journal of natural products, Apr-24, Volume: 78, Issue:4
Eremophilane Sesquiterpenes and Diphenyl Thioethers from the Soil Fungus Penicillium copticola PSU-RSPG138.
AID679417TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID678718Metabolic stability in human liver microsomes assessed as high signal/noise ratio (S/N of >100) by measuring GSH adduct formation at 100 uM after 90 mins by HPLC-MS analysis2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1654162Bactericidal activity against Mycobacterium tuberculosis H37Rv harboring LuxAB gene assessed as reduction in microbial growth by measuring reduction in relative luminescence units after 7 days by luminometric method2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID582992Antimicrobial activity against rifampin-, fusidic acid-resistant Enterococcus faecium BM-4105 by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID571430Antibacterial activity against Pseudomonas aeruginosa ATCC 27853by Etest method in presence of 2 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1242345Antimycobacterial activity against 1-(2-(4-((5-chloro-6-methylpyridin-3-yl)methylamino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA D89N mutant incubated for 7 days by microdilu2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID1562247Antimycobacterial activity against Mycobacterium smegmatis atR11 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID372545Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 24-48 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1164940Antimicrobial activity against Mycobacterium tuberculosis H37Rv by microbroth dilution method2014Journal of medicinal chemistry, Oct-23, Volume: 57, Issue:20
Synthesis, structure-activity relationship studies, and antibacterial evaluation of 4-chromanones and chalcones, as well as olympicin A and derivatives.
AID1516021Antibacterial activity against Salmonella enterica serovar typhimurium C77-31 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1585121Antimicrobial activity against multi drug-resistant Mycobacterium tuberculosis 14231 after 7 days by MABA2018European journal of medicinal chemistry, Dec-05, Volume: 160Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
AID370102Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po after 2 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID103675In vitro activity of compound against slowly growing Mycobacterium kansasii 12991990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1298598Antibacterial activity against Pseudomonas aeruginosa after 24 hrs by agar diffusion assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.
AID1298604Antibacterial activity against Klebsiella pneumoniae after 24 hrs by agar diffusion assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.
AID1196886Cytotoxicity against mouse RAW264.7 cells at 50 uM after 48 hrs by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID1426439Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis CF104 clinical isolate incubated for 7 days measured 24 hrs post incubation by resazurin microtiter assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
AID531014Antimicrobial activity against Clostridium difficile isolate 61 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1209593Dissociation constant, pKa of the acidic compound by capillary electrophoresis-mass spectrometry analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID1400041Bactericidal activity against Staphylococcus aureus BAA 2094 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1476407Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through carboxymethylcellulose vehicle as single oral dose per gavage after 0.3 hrs by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1383956Bactericidal activity against MDR Mycobacterium tuberculosis isolate 591 after 4 weeks by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID535772Antimicrobial activity against Mycobacterium ulcerans 1059 agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID565183Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 grown as biofilms by microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Evaluation of analogs of reutericyclin as prospective candidates for treatment of staphylococcal skin infections.
AID1557241Antitubercular activity against resistant Mycobacterium tuberculosis 74 harboring rpoB His526Tyr mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID427284Antitubercular activity against Mycobacterium tuberculosis H37Rv by microdilution resazurin assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Antimycobacterial activity of new 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-one derivatives. Molecular modeling investigations.
AID679507TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID1304527Bactericidal activity against Mycobacterium tuberculosis BSG001 incubated overnight by microbroth-dilution method2016Journal of natural products, Mar-25, Volume: 79, Issue:3
Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.
AID529189Antibacterial activity against Klebsiella pneumoniae K224 with arr-5 gene by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID1594308Growth inhibition of human PANC1 cells by MTT assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID545933Antimicrobial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 4 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID292285Antimycobacterial activity against Mycobacterium avium ATCC 25291 by microplate Alamar blue assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID425631Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as lowest drug level producing inhibition at 10'6 CFU of inoculum by agar counting method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1427051Selectivity index, ratio of GI50 for human PANC1 cells to MIC for dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID1589011Anti-mycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis
AID585879Antimicrobial activity against Staphylococcus aureus clone 1-1 harboring staphylococcal cassette chromosome mec element type 5 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID530990Antimicrobial activity against Clostridium difficile isolate 37 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID303890% inhibition of the 20 Mycobacterium avium complex (MAC) clinical isolates1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1594306Growth inhibition of human HeLa cells by MTT assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID313233Antimicrobial activity against Klebsiella pneumoniae at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID297186Antibacterial activity against multidrug resistant Staphylococcus aureus 495892007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Structure-activity relationships of phenyl-furanyl-rhodanines as inhibitors of RNA polymerase with antibacterial activity on biofilms.
AID1192376Antimicrobial activity against Candida albicans MTCC 183 after 48 to 72 hrs by broth micro dilution method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.
AID1174024Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as complete growth inhibition after 5 days using solid media by serial proportion method2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Synthesis and evaluation of the 2,4-diaminoquinazoline series as anti-tubercular agents.
AID572552AUC (0 to 12 hrs) in german pulmonary tuberculosis patient at 600 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID558244Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 1.5 mg/liter after 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID528962Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured on day 8 after starting standard TB therapy2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID582515AUC in Staphylococcus epidermidis ATCC 27626 infected Wistar rat serum at 25 mg/kg, ip measured on day 42008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID1143689Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in spleen at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 12014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
AID325001Antibacterial activity against rifampin and cefdinir-resistant Haemophilus influenzae RdRIF/MSC06647 mutant by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID1812060Kinetic solubility of the compound in pH 6.52021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Benzoheterocyclic Oxime Carbamates Active against
AID588987Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP2B12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1334246Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 active stage infected in human THP1 cells measured on day 8 by nitrate reductase assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1879554Antibacterial activity against metronidazole-resistant Bacteroides ovatus MMX 35042022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID369923Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected Swiss mouse assessed as reduction of bacterial count in spleen at 10 mg/kg after 12 days of infection weekly 5 times for 8 weeks2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID1244842Octanol-water partition coefficient, log P of the compound by UV-vis method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID1488561Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID509623Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB515 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID571419Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 2 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID373043Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate CY7 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1133240Antimicrobial activity against Clostridium perfringens 2 by serial dilution method1978Journal of medicinal chemistry, Dec, Volume: 21, Issue:12
Synthesis and quantitative structure--activity relationships of some antibacterial 3-formylrifamycin SV N-(4-substituted phenyl)piperazinoacethydrazones.
AID1296387Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 4 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1182152Ratio of MIC99 for Mycobacterium smegmatis to ratio of MIC99 for Mycobacterium smegmatis in presence of chlorpromazine-N-oxide2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID1678507Antibacterial activity against Clostridium difficile ATCC 43255 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID529540Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 ATC mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1563898Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days in presence of middlebrook 7H9/ADC medium by microplate alamar blue assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights.
AID678716Inhibition of human CYP3A4 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using diethoxyfluorescein as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID373953Post antibiotic effect against Mycobacterium tuberculosis H37Rv ATCC 2517 infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L administered for 1 hr2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID437961Antitubercular activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
1,3-Dipolar cycloaddition of C-aryl-N-phenylnitrones to (R)-1-(1-phenylethyl)-3-[(E)-arylmethylidene]tetrahydro-4(1H)-pyridinones: synthesis and antimycobacterial evaluation of enantiomerically pure spiroisoxazolidines.
AID429374Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 21 days by agar proportion method2009European journal of medicinal chemistry, Aug, Volume: 44, Issue:8
Synthesis and antitubercular activity of novel 4-substituted imidazolyl-2,6-dimethyl-N3,N5-bisaryl-1,4-dihydropyridine-3,5-dicarboxamides.
AID278861Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID428295Antimicrobial activity against Acinetobacter baumannii BM4579 expressing adeIJK genes with pAT807 isolated from patient with urinary tract infection by agar dilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID739228Antitubercular activity against Mycobacterium tuberculosis Erdman ATCC 35801 infected in C57BL/6 mouse assessed as viable bacterial load in lung at 10 mg/kg/day through gavage 5 days per week for 4 weeks starting on 10th day post-infection (Rvb = 6.49 +/-2013Journal of natural products, Mar-22, Volume: 76, Issue:3
Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents.
AID1205587Inhibition of Escherichia coli switch region of RNA polymerase after 1 hr by transcription-coupled translation assay2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1567123Antimicrobial activity against Enterobacter cloacae ATCC 13047 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID487842Antimycobacterial activity against Mycobacterium avium after 48 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID1767893Antitubercular activity against isoniazid,streptomycin,rifampicin,ethambutol, rifabutin, para-aminosalicylat, ofloxacin-resistant Mycobacterium tuberculosis clinical isolate 13946 assessed as inhibition of bacterial growth incubated for 7 days by MABA ass2021European journal of medicinal chemistry, Oct-15, Volume: 222Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis.
AID1143265Antimycobacterial activity against Mycobacterium tuberculosis D-211 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID1871134Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 7 days by resazurin assay2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties.
AID545909Antimicrobial activity against Escherichia coli ATCC 25922 in presence of 4 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1544791Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth after 7 days by green fluorescent protein microplate assay2019Bioorganic & medicinal chemistry letters, 07-01, Volume: 29, Issue:13
Synthesis and biological evaluation of 2-chloro-3-[(thiazol-2-yl)amino]-1,4-naphthoquinones.
AID1543323Antimicrobial activity against vancomycin-resistant Enterococcus faecalis ATCC 51212 assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution assay2019Journal of natural products, 07-26, Volume: 82, Issue:7
Antibacterial Salinaphthoquinones from a Strain of the Bacterium
AID1634851Antitubercular activity against MDR Mycobacterium tuberculosis X23 incubated for 1 to 9 days by inverted microscopic analysis2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID545929Antimicrobial activity against Enterobacter cloacae ATCC 23355 by Etest method in presence of 4 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID370238Half life in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1272622Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 21 days by broth microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.
AID1636440Drug activation in human Hep3B cells assessed as human CYP2D6-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID560511Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b5k3578 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1563899Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days in presence of middlebrook 7H9/CAS medium by microplate alamar blue assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights.
AID1776723Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured by Resazurin microtitre assay2021Bioorganic & medicinal chemistry letters, 06-15, Volume: 422,2,2-trifluoro-1-(1,4,5,6-tetrahydropyridin-3-yl)ethanone derivative as efflux pump inhibitor in Mycobacterium tuberculosis.
AID780898Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by REMA assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids.
AID559915Volume of distribution in alveolar cells of patient with tuberculosis at 600 to 1200 mg/kg, po administered as single dose2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Population modeling and Monte Carlo simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of rifampin in lungs.
AID555308Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 074 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1393797Antibacterial activity against multidrug resistant Mycobacterium tuberculosis after 7 days by two fold dilution assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID581188Induction of NF-kappaB activation in human A549 cells assessed as fold increase in NF-kappaB/DNA binding at 50 ug/ml by electrophoretic mobility shift assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1311243Antibacterial activity against Escherichia coli 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID357637Antibacterial activity against Staphylococcus aureus ATCC 6538 after 24 hrs2001Journal of natural products, Sep, Volume: 64, Issue:9
A new naphthopyrone derivative from Cassia quinquangulata and structural revision of quinquangulin and its glycosides.
AID1474042Ratio of drug concentration at steady state in human at 150 to 600 mg, iv QD after 24 hrs to IC50 for human MRP4 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID373959Post antibiotic effect against Mycobacterium tuberculosis H37Rv ATCC 2517 infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 14 mg/L administered for 0.5 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1297720Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1856872Antimicrobial activity against Staphylococcus aureus ATCC 25923 in presence of KCl2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID373045Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate ZS15 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID776888Induction of resistant frequency in Escherichia coli expressing TolC mutant at 2 times MIC treated for every 3 days2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID543798Antimicrobial activity against Streptococcus pyogenes VT 59 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1213957Induction of CYP3A4 in human hepatocytes using midazolam as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID1500580Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luxABCDE operon incubated for 10 days under hypoxic conditions followed by incubation under aerobic conditions for 28 hrs by LORA method2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID776897Ratio of IC50 for Escherichia coli RNA polymerase core enzyme to IC50 for Escherichia coli RNA polymerase holo enzyme2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID217175In vitro cytotoxicity against VERO cell line2002Journal of medicinal chemistry, Aug-01, Volume: 45, Issue:16
Mixed steroidal 1,2,4,5-tetraoxanes: antimalarial and antimycobacterial activity.
AID586053Antimicrobial activity against Staphylococcus aureus clone 4-4 harboring staphylococcal cassette chromosome mec element type 4 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1653481Antimicrobial activity against Escherichia coli ATCC 25922 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID292278Antimycobacterial activity against Mycobacterium bovis BCG by microplate Alamar blue assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID530999Antimicrobial activity against Clostridium difficile isolate 46 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID604025Unbound CSF to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID326297Antibacterial activity against methicillin-resistant Staphylococcus aureus 4342 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID571650Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by Etest method in presence of 4 ug/ml NAB70752008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1784361Antimycobacterial activity against Mycobacterium tuberculosis InhA-OE overexpressing H37Rv-LP:fabGl/inhA-c-15t in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID1879496Antibacterial activity against Clostridioides difficile ATCC 96892022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID283238Reduction of bacterial counts in Mycobacterium tuberculosis H37Rv infected Swiss mouse lung at 10 mg/kg, po for 5 days/week after 2 months2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID373042Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate ZJ49 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID586231Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 4 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID780282Cytotoxicity against african green monkey Vero cells by tetrazolium dye reduction assay2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Inhibitory effect of oxygenated cholestan-3β-ol derivatives on the growth of Mycobacterium tuberculosis.
AID1311246Antibacterial activity against Escherichia coli 14-2 expressing extended-spectrum beta-lactamase2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID530787Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 18 expressing RpoB R505K mutant by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1435842Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by resazurin reduction microplate assay2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID689223Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 culture in 7H12 media after 7 days by microplate alamar blue assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds.
AID530637Antimicrobial activity against Staphylococcus aureus CB812 harboring rpo B H481Y and gyrA S84L mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1205461Antitubercular activity against rifampin, isoniazid and streptomycin-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID1636548Antitubercular activity against Mycobacterium tuberculosis H37Rv by microbroth dilution method2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Synthesis and antibacterial evaluation of macrocyclic diarylheptanoid derivatives.
AID341775AUC (0 to infinity) in Mycobacterium tuberculosis infected patient at 3 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID582267Antimicrobial activity against Bacillus cereus ATCC 4342 selected after 20 daily cycles of drug selection followed by 5 days of nonselective growth by broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Efficacy of oritavancin in a murine model of Bacillus anthracis spore inhalation anthrax.
AID558266Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 2 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID626918Antimycobacterial activity against Mycobacterium smegmatis MC2 ATCC 19420 using compound level ranging from 1 to 100 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID1412769Antimycobacterial activity against Mycobacterium smegmatis ATCC 607 incubated in dark for 48 hrs by resazurin assay2018MedChemComm, Apr-01, Volume: 9, Issue:4
Design, synthesis and antimycobacterial activity of hybrid molecules combining pyrazinamide with a 4-phenylthiazol-2-amine scaffold.
AID532968Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 122010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID531126Antimicrobial activity against Staphylococcus aureus CB1952 harboring rpoB S486L, gyrA S48L, gyrA E88Q, gyrA G532S, parC S80F, parC E84L mutant genes selected after CBR-2092 exposure for 21 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID283166Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5204 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID472703Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
AID1311229Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1556521Induction of constitutive androstane receptor in human primary hepatocytes assessed as upregulation of CYP3A4 protein expression at 10 uM after 72 hrs by Western blot analysis2019European journal of medicinal chemistry, Oct-01, Volume: 179Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.
AID456894Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents.
AID609792Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 to 8 days by microplate alamar blue assay2011Bioorganic & medicinal chemistry letters, Aug-15, Volume: 21, Issue:16
Diversity oriented design of various hydrazides and their in vitro evaluation against Mycobacterium tuberculosis H37Rv strains.
AID555506Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 057 after 9 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID582516AUC in Staphylococcus epidermidis ATCC 27626 infected Wistar rat tissue cage fluid at 25 mg/kg, ip measured on day 42008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID446149Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.
AID1393799Cytotoxicity against African green monkey Vero cells after 72 hrs by MTT assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID1879503Antibacterial activity against metronidazole-resistant Helicobacter pylori CB1573 harboring rdxAR16S mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1484383Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay2017European journal of medicinal chemistry, Jun-16, Volume: 133Isoniazid derivatives and their anti-tubercular activity.
AID531023Antimicrobial activity against Clostridium difficile isolate 70 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID682123TP_TRANSPORTER: Northern blot in vivo, apical membrane of enterocyte2000The American journal of pathology, Nov, Volume: 157, Issue:5
The effect of rifampin treatment on intestinal expression of human MRP transporters.
AID531298Antimicrobial activity against Clostridium difficile isolate 70 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID545928Antimicrobial activity against Enterobacter cloacae ATCC 23355 by Etest method in presence of 2 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID623581Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 22 hrs by microbroth dilution antibiotic susceptibility assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
One-pot syntheses of pseudopteroxazoles from pseudopterosins: a rapid route to non-natural congeners with improved antimicrobial activity.
AID693670Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID1417177Antibacterial activity against Acinetobacter baumannii BAA-1605 after 16 to 18 hrs in presence of PMBN by CLSI method2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis of 1,2,3-triazole linked 4(3H)-Quinazolinones as potent antibacterial agents against multidrug-resistant Staphylococcus aureus.
AID555501Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 051 after 9 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1497862Antibacterial activity against Salmonella paratyphi A serotype ATCC 57022018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID352095Antimicrobial activity against ceftriazone-resistant Bacillus subtilis after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID537113Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 3 to 28 days by twofold dilution method2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1311285Selectivity index, ratio of CC50 for human HeLa cells to MIC for dormant stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1436934Selectivity index, ratio of GI90 for human A549 cells to MIC90 for dormant state of Mycobacterium tuberculosis H37Ra2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID1185709Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1772151Antibacterial activity against Staphylococcus aureus assessed as inhibition of bacterial growth by CLSI based microdilution method2021Journal of natural products, 11-26, Volume: 84, Issue:11
Antimicrobial and Cytotoxic Angucyclic Quinones from
AID373038Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate NJ59 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1185717Antifungal activity against Candida albicans ATCC 10231 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID444056Fraction escaping gut-wall elimination in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID679646TP_TRANSPORTER: inhibition of BSP uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID571422Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 0.25 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1334251Cytotoxicity against human THP1 cells by MTT assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1634991Antimicrobial activity against Staphylococcus aureus clinical isolates from Liberec regional hospital assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID560514Antimicrobial activity against SCCmec type IV vancomycin-intermediate Staphylococcus aureus isolate 06b41 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID564976Antimicrobial activity against Mycobacterium bovis BCG by resazurine microtiter assay in presence of 0.5 mg/liter reserpine2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1183300Antimycobacterial activity against Mycobacterium smegmatis assessed as growth inhibition after 32 hrs by spectrophotometry2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives.
AID1868110Anti-tubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID1272450Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate alamar blue assay2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes.
AID1436930Cytotoxicity against human MCF7 cells assessed as growth inhibition after 48 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID555742Antibacterial activity against methicillin-resistant, Linezolid non-susceptible coagulase-negative Staphylococcus epidermidis 345 by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1474039Ratio of drug concentration at steady state in human at 150 to 600 mg, iv QD after 24 hrs to IC50 for human BSEP overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID461352Antifungal activity against Candida albicans ATCC 900282010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections.
AID424327Antimicrobial activity against Dialister propionicifaciens by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID611492Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 1533 isolated from patient arm cellulitis after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID693675Antibacterial activity against Staphylococcus aureus isolate 723 obtained from veterinary sample after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID1297722Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID441081Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 to 7 days by microplate alamar blue assay2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID509617Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB516 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID518017Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent resistant isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro activity of fidaxomicin (OPT-80) tested against contemporary clinical isolates of Staphylococcus spp. and Enterococcus spp.
AID531283Antimicrobial activity against Clostridium difficile isolate 55 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID574810Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 horboring rpoB D516V, katG S315T/R463L, gyrA D94G/S95T/R128S/Y129C, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1721014Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1602936Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 4 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID278682Antibacterial activity against Enterococcus faecium isolate 57532007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID581199Cmax in serum of human patient undergoing fibre-optic bronchoscopy at 600 mg, po administered as single dose2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID445329Cytotoxicity against human THP1 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID495516Antibacterial activity against multidrug-resistant Acinetobacter baumannii AYE by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID510985Antimicrobial activity against Acinetobacter baumannii 1327 after 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID405154Cmax in tuberculosis patient at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1223014Activation of mouse PXR expressed in human HepG2 cells at 2.5 uM after 24 hrs by firefly luciferase DR3 reporter gene assay2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID582986Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0661 harboring MLST sequence type ST78 and pulsotype C expressing vanM gene cluster isolated from exudate of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1516086Resistance index, ratio of MIC for antibacterial activity against ciprofloxacin-resistant Escherichia coli to MIC for Escherichia coli ATCC 25922 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1634853Antitubercular activity against XDR Mycobacterium tuberculosis X59 incubated for 1 to 9 days by inverted microscopic analysis2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID1311239Antibacterial activity against Enterococcus faecalis 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1678513Antibacterial activity against Clostridium difficile 8282 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID1173784Inhibition of Mycobacterium tuberculosis DNA gyrase using relaxed pBR322 as substrate after 30 mins by supercoiling assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID1626627Antimicrobial activity against Streptococcus agalactiae clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID560519Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate zj07028 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1447484Antibacterial activity against multidrug/extremely drug-resistant/colistin-resistant Pseudomonas aeruginosa isolate 91433 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID293584Antibacterial activity against Escherichia coli isolate assessed after 24 hrs by by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID1055746Antimycobacterial activity against Mycobacterium smegmatis MC2 155 ATCC 14468 after 32 hrs by turbidimetry2013European journal of medicinal chemistry, , Volume: 70Design, diversity-oriented synthesis and structure activity relationship studies of quinolinyl heterocycles as antimycobacterial agents.
AID1406780Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition after 48 hrs by MTT assay2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis and biological evaluation of dihydroquinoline carboxamide derivatives as anti-tubercular agents.
AID1738818Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in colony forming unit at 1 to 10 ug/ml incubated for 7 days in nutrient starvation medium by alamar blue based serial dilution method2020European journal of medicinal chemistry, Aug-01, Volume: 199Design and synthesis of thiourea-based derivatives as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
AID1577323Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1609004Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ITM-M006710 after 48 hr by resazurin dye based microdilution method2019European journal of medicinal chemistry, Nov-01, Volume: 181Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.
AID531058Antimicrobial activity against Clostridium difficile isolate 25 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1334249Antitubercular activity against Mycobacterium bovis BCG ATCC 35743 active stage measured on day 8 by nitrate reductase based two-fold dilution assay2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID297111Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1412768Antimycobacterial activity against Mycobacterium avium subsp. avium Chester ATCC 15769 incubated in dark for 5 days by Alamar Blue assay2018MedChemComm, Apr-01, Volume: 9, Issue:4
Design, synthesis and antimycobacterial activity of hybrid molecules combining pyrazinamide with a 4-phenylthiazol-2-amine scaffold.
AID103671In vitro activity compound against slowly growing Mycobacterium kansasii 12911990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1246787Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by micro alamar blue assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Re-engineering nalidixic acid's chemical scaffold: A step towards the development of novel anti-tubercular and anti-bacterial leads for resistant pathogens.
AID1163979Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay in presence of 8 mg/mL piperine efflux pump inhibitor2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID520083Antimicrobial activity against aheB-deficient kanamycin-resistant Aeromonas hydrophila subsp. hydrophila ATCC 7966 harboring AheABC efflux pump by agar dilution method in presence of 64 mg/L efflux pump inhibitor phenylalanine-arginine-beta-naphthylamide2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID1403711Antimycobacterial activity against Mycobacterium tuberculosis H37Rv dormant stage assessed as log reduction in bacterial load at 10 ug/ml incubated for 7 days2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1856876Antimicrobial activity against Escherichia coli ATCC 25922 in presence of KCl2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID531041Antimicrobial activity against Clostridium difficile isolate 8 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID530788Antimicrobial activity against Clostridium difficile isolate 19 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID555508Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 197 after 12 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1617943Antibacterial activity against Mycobacterium aurum ATCC 23366 after 16 to 48 hrs2019Journal of natural products, 12-27, Volume: 82, Issue:12
Structure Determination, Functional Characterization, and Biosynthetic Implications of Nybomycin Metabolites from a Mining Reclamation Site-Associated
AID305230Antimicrobial activity against Arr-2 negative Escherichia coli DH5alpha bearing pCTF104P2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID557107Binding affinity to human serum albumin assessed as fraction of binding sites occupied by compound at 80 to 120 ug/ml by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID1400024Antibacterial activity against non-replicating Mycobacterium tuberculosis H37Rv harboring pFCA-luxAB preincubated for 10 days under anaerobic condition followed by incubation under ambient gaseous condition for 28 hrs by LORA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1287502Antitubercular activity against active state Mycobacterium bovis BCG ATCC 35734 assessed as viable cells after 8 days by nitrate reductase assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID1571560Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 to 14 days by broth micro dilution method2019MedChemComm, Feb-01, Volume: 10, Issue:2
Quinolone-isoniazid hybrids: synthesis and preliminary
AID1585704Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis after 3 to 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID767545Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 1 to 100 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID405163AUC (0 to 24 hrs) in tuberculosis patient assessed as desacetylrifampin level at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1543321Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution assay2019Journal of natural products, 07-26, Volume: 82, Issue:7
Antibacterial Salinaphthoquinones from a Strain of the Bacterium
AID1447480Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 101885 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1634259Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 200 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID562787Antimicrobial activity against Chlamydia suis R19/tetR harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID373747Antimicrobial activity against mupirocin-susceptible methicillin-resistant Staphylococcus aureus by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Mupirocin-resistant, methicillin-resistant Staphylococcus aureus strains in Canadian hospitals.
AID626917Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 using compound level ranging from 1 to 100 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID571643Antibacterial activity against Enterobacter cloacae by Etest method in presence of 4 ug/ml NAB70682008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1626628Antimicrobial activity against Streptococcus pneumoniae clinical isolates by broth dilution method2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID373939fAUC (0 to 168 hrs) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 4200 mg, po administered once a week2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID588125Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 3 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID681502TP_TRANSPORTER: increase in Calcein intracellular accumulation (Calcein: 0.5 uM, Rifampicin: 200 uM) in GLC4/ADR cells1999Cancer letters, May-03, Volume: 139, Issue:1
Inhibition of multidrug resistance-associated protein (MRP) activity by rifampicin in human multidrug-resistant lung tumor cells.
AID1427054Selectivity index, ratio of GI50 for human HeLa cells to MIC for dormant stage of Mycobacterium tuberculosis H37Ra ATCC 251772017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID449210Antimycobacterial activity against Mycobacterium avium CIP 103317 by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID571453Antibacterial activity against Enterobacter cloacae ATCC 23355 ATCC 13883 by Etest method in presence of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID424320Antimicrobial activity against Dialister micraerophilus by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID377698Antileishmanial activity against Leishmania donovani after 72 hrs by alamar blue assay2006Journal of natural products, Jul, Volume: 69, Issue:7
Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases.
AID1164304Inhibition of DNA synthesis in Mycobacterium bovis BCG assessed as inhibition of [3H]adenine incorporation by liquid scintillation counting2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1514447Antitubercular activity against Mycobacterium tuberculosis H37Rv after 15 days by turbidometric method2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID510520Ratio of Cmax in diabetic tuberculosis patient to Cmax in tuberculosis patient2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID645690Antimicrobial activity against Mycobacterium avium by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1716637Antibacterial activity against Escherichia coli ATCC 25922 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID434056Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced PGE2 formation at 100 ug/ml after 48 hrs by enzyme immunoassay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1436913Antimycobacterial activity against dormant state of Mycobacterium tuberculosis H37Ra by two fold dilution method2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID1653511Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.3 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID200516Antimicrobial activity derived as minimum inhibitory concentration are determined using brain-heart infusion medium against Salmonella paratyphi B0248 K(Sclavo)1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID278856Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID1634265Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 3.125 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID625280Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for cholecystitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID581057Effect on p38 phosphorylation in human A549 cells assessed as increase in IL1-beta, TNF-alpha and IFN-gamma-induced phosphorylation at 50 ug/ml after 15 to 30 mins by Western immunoblotting analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID531285Antimicrobial activity against Clostridium difficile isolate 57 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID532967Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 112010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID562796Antimicrobial activity against Chlamydia trachomatis J/6276/oflR-rifR2 harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID554574Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 60 mg/kg, sc administered 2 hrs after infection evry 8 hrs as three-dose regimen measured after 192009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1851924Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as bacterial growth inhibition incubated for 5 days under hypoxic condition by resazurin microtiter assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID1223074Induction of Ugt1a10 gene expression in PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID373937Half life in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 4200 mg, po administered once a week2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID680208TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID1173785Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID1716867Antibacterial activity against Pseudomonas aeruginosa 260-97103 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1626593Inhibition of wild type Staphylococcus aureus RNA polymerase assessed as reduction in RNA product formation2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1276380Selectivity index, ratio of GI50 for human A431 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID1244834Antibacterial activity against Staphylococcus epidermidis ATCC 49134 after 18 hrs by serial microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID1716661Antibacterial activity against Pseudomonas aeruginosa 200 harboring efflux mutant assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID457437Antitubercular activity against Mycobacterium tuberculosis H37Rv at pH 6 by microplate alamar blue assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID372488Half life in patient with severe malaria at 200 mg, perorally2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1427041Antitubercular activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells after 12 days by nitrate reductase assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID509622Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB518 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID541029Induction of apoptosis in bovine BL3 cells assessed as viable cells after 24 hrs by annexin V/propidium iodide staining-based FACS analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Theileria apicoplast as a target for chemotherapy.
AID683323Antibacterial activity against multidrug-resistant Morganella morganii 07-09 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID373041Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate ZJ36 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID560521Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate xa07029 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID333072Antileishmanial activity against Leishmania donovani2004Journal of natural products, Aug, Volume: 67, Issue:8
Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases.
AID1782924Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth incubated for 9 days by resazurin microtiter assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID545910Antimicrobial activity against Escherichia coli ATCC 25922 in presence of 8 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1293913Selectivity index, ratio of GI50 for human THP1 cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID541103Antimicrobial activity against Bacillus pumilus SJ15542009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Continuous cefazolin infusion to treat bone and joint infections: clinical efficacy, feasibility, safety, and serum and bone concentrations.
AID545934Antimicrobial activity against in Acinetobacter baumannii ATCC 19606 in presence of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID581058Effect on JNK phosphorylation in human A549 cells assessed as increase in IL1-beta, TNF-alpha and IFN-gamma-induced phosphorylation at 50 ug/ml after 15 to 30 mins by Western immunoblotting analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID729739Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by agar dilution method2013Bioorganic & medicinal chemistry letters, Mar-01, Volume: 23, Issue:5
Synthesis and antitubercular activity of amino alcohol fused spirochromone conjugates.
AID1069171Antimicrobial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv SRI 1369 assessed as growth inhibition after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1181163Antimicrobial activity against clinical isolate Mycobacterium tuberculosis DKU220 assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1623449Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by Alamar blue assay2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis of novel morpholine, thiomorpholine and N-substituted piperazine coupled 2-(thiophen-2-yl)dihydroquinolines as potent inhibitors of Mycobacterium tuberculosis.
AID611489Antibacterial activity against epidemic methicillin-resistant Staphylococcus aureus isolate 15 isolated from patient urine infection after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID529518Antibacterial activity against normal-colony variant Staphylococcus aureus derived from non cystic fibrosis patient assessed as resistant isolates at 37 degC after 24 hrs by disk diffusion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
The thymidine-dependent small-colony-variant phenotype is associated with hypermutability and antibiotic resistance in clinical Staphylococcus aureus isolates.
AID537736Antifungal activity against yeast AD1-8u expressing Candida albicans CaCdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID529541Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 ATA mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1497860Antibacterial activity against Shigella dysenteriae PTCC 1188 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID774600Therapeutic index, ratio of IC50 for human HepG2/C3A cells to GI50 for Mycobacterium tuberculosis H37Rv ATCC 272942013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID1174678Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by MABA method2015European journal of medicinal chemistry, Jan-07, Volume: 89Synthesis, molecular docking and anti-mycobacterial evaluation of new imidazo[1,2-a]pyridine-2-carboxamide derivatives.
AID1716721Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as fractional inhibitory concentration index in presence of doxycycline incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1602933Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 1 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1879566Antibacterial activity against Peptoniphilus asaccharolyticus ATCC 297432022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID168876Hypolipidemic activity was determined in male rats, and high-density lipoprotein level was determined at 100 mg/kg1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hypolipidemic activity of rifamycin derivatives.
AID530775Antimicrobial activity against Clostridium difficile isolate 6 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1706677Antitubercular activity against isoniazid/rifampicin multidrug-resistant Mycobacterium tuberculosis FJ05120 clinical isolates assessed as bacterial growth inhibition by MABA2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB.
AID626867Antimicrobial activity against replicating Mycobacterium tuberculosis after 8 days by micro plate alamar blue assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID1288636Antituberculosis activity against Mycobacterium tuberculosis H37Rv in 7H12 medium incubated for 4 days by Microplate Alamar Blue assay2016MedChemComm, Jan-01, Volume: 7, Issue:1
Syntheses and Biological Evaluations of Highly Functionalized Hydroxamate Containing and
AID1905613Antimicrobial activity against rifampicin-resistant Escherichia coli ATCC 259222022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID1888132Antimycobacterial activity against Mycobacterium bovis BCG overexpressing DprE1 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1596894Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated for 16 to 18 hrs by broth microdilution assay
AID1463961Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 7357/1998 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1304836Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1869563Antibacterial activity against Bacillus cereus DSM 31 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID1297727Antibacterial activity against methicillin resistant Staphylococcus aureus isolate 4 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1423481Cytotoxicity against human THLE3 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID537116Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis after 3 to 28 days by twofold dilution method2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1205590Fraction unbound (%) in human plasma at 10 uM by LC/MS-MS analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1856911Antibacterial activity against Staphylococcus aureus ATCC 25923 assessed as fold increase in MIC measured after 15 passages by resistance development assay2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1575939Antimycobacterial activity against Mycobacterium tuberculosis H37RvMA ATCC 27294 cultured in protein-based Middlebrook 7H9 medium supplemented with glucose, albumin-dextrose-catalase and Tween 80 assessed as inhibition of bacterial growth incubated for 7
AID611493Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 105 isolated from patient toe wound after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID380456Antibacterial activity against Enterococcus faecalis by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID1632662Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra ATCC 25177 after 12 days by XTT reduction menadione assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID1447479Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 100036 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID644319Antitubercular activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin assay2012European journal of medicinal chemistry, Mar, Volume: 49Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents.
AID1879543Antibacterial activity against rifampicin/fluoroquinolone-resistant Clostridioides difficile CB1942 harboring rpoBQ489K/gyrAD71Y/T82A mutant measured after 3 days2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1879565Antibacterial activity against Peptococcus niger ATCC 277312022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID406602Ratio of peak drug level in albino guinea pig cage fluid at 12.5 mg/kg, ip to MIC for Staphylococcus aureus ATCC 292132007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID640334Antimycobacterial activity against Mycobacterium bovis BCG assessed as growth inhibition at 0.5 ug/ml by microplate alamar blue assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Antimycobacterial activities of 5-alkyl (or halo)-3'-substituted pyrimidine nucleoside analogs.
AID583692Antimicrobial activity against methicillin-resistant Staphylococcus aureus 10*3d1 harboring hypothetical protein SA1826 14E mutant gene after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1731071Antitubercular activity against Mycobacterium tuberculosis harboring gfp reporter gene and wild type DrpE1 assessed as inhibition of bacterial growth incubated for 14 days by fluorescence based analysis2021European journal of medicinal chemistry, Mar-05, Volume: 213Easily accessed nitroquinolones exhibiting potent and selective anti-tubercular activity.
AID555296Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID670863Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
AID1653522Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.2 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID493952Antimicrobial activity aagainst Mycobacterium tuberculosis ATCC 14468 in log phase by agar dilution method2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.
AID1378013Antimycobacterial activity against Mycobacterium tuberculosis MC2 70002017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID1716723Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as fractional inhibitory concentration index in presence of chloramphenicol incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID584115Antibacterial activity against Escherichia coli KAM32 harboring pSP72 by broth microdilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
LmrS is a multidrug efflux pump of the major facilitator superfamily from Staphylococcus aureus.
AID571395Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 0.25 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID586050Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type U8 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1058227Antimycobacterial activity against Mycobacterium fortuitum2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID557210Antibacterial activity against Beta-lactamase-negative Neisseria meningitidis assessed as percent intermediate isolates by Etest method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antibiotic susceptibility and characteristics of Neisseria meningitidis isolates from the African meningitis belt, 2000 to 2006: phenotypic and genotypic perspectives.
AID618737Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 4 weeks by agar dilution assay2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Synthesis and biological evaluation of substituted 4-arylthiazol-2-amino derivatives as potent growth inhibitors of replicating Mycobacterium tuberculosis H₃₇Rv.
AID518803Antimycobacterial activity against Mycobacterium chelonae after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID1566201Antimycobacterial activity against Mycobacterium tuberculosis H37Rv overexpressing DprE1 assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID677626Cytotoxicity against african green monkey Vero cells at < 10 uM after 3 days2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Structural requirements for the antitubercular quaternized triflupromazine pharmacophore.
AID558758Antibacterial activity against homo-Methicillin-resistant and tetracycline-resistant and rifampicin-resistant Staphylococcus aureus deltaIP-rifR::vraSH14 by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID562238Antimycobacterial activity against Mycobacterium smegmatis assessed as growth inhibition in mid-logarithmic phase by spectrophotometry2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Modifying culture conditions in chemical library screening identifies alternative inhibitors of mycobacteria.
AID776900Inhibition of Escherichia coli RNA polymerase-RNA polymerase sigma factor RpoD interaction at 10 uM by ELISA2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID523291Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as 2 log reduction in bacterial burden in lungs orally treated in water-20% encapsine upto 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID530771Antimicrobial activity against Clostridium difficile isolate 2 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1210910Intrinsic clearance in rat kidney microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID1784356Antimycobacterial activity against Mycobacterium tuberculosis MmpL3 G253E in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID1264494Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis by resazurin microtiter assay2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents.
AID1332966Induction of nitric oxide production assessed as nitrite level at 10'-4M measured after 1 hr in presence 1:50 molar excess of of L-cysteine by Griess reagent based spectrophotometer relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID571426Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method by Etest in presence of 1 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1298607Antibacterial activity against Staphylococcus aureus after 24 hrs by agar diffusion assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.
AID1716645Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID581190Effect on NF-kappaB activation in human A549 cells assessed as degradation of inhibitory subunit IkappaB after 30 mins at 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1079938Chronic liver disease either proven histopathologically, or through a chonic elevation of serum amino-transferase activity after 6 months. Value is number of references indexed. [column 'CHRON' in source]
AID1847536Antimycobacterial activity against Mycobacterium tuberculosis incubated for 7 days by microplate alamar blue assay
AID406468Antibacterial activity against Staphylococcus aureus ATCC 29213 by macrotube dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID634270Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID145295Tested for antibacterial activity against Mycobacterium tuberculosis H37Rv isonicotinic acid hydrazide-resistant strain1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID1459058Antitubercular activity against isoniazid resistant Mycobacterium tuberculosis H37Rv harboring KAtG Y155 deletion mutant after 5 days2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
AID1905563Antimicrobial activity against Staphylococcus epidermidis ATCC 12228 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID510523Half life in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID588981Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1624155Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 7 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID438557Antimycobacterial activity against non replicating persistent form of Mycobacterium tuberculosis H37Rv after 10 days by low oxygen recovery assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.
AID554579Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in intracellular bacterial cfu in peritoneum at 60 mg/kg, sc administered as single dose 2 hrs after infection measured within 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID571648Antibacterial activity against Proteus mirabilis ATCC 29906 by Etest method in presence of 4 ug/ml NAB70732008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID545048Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ210 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID617280Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by Microplate Alamar blue assay2011Journal of medicinal chemistry, Sep-08, Volume: 54, Issue:17
Novel 1,2,3-triazole derivatives for use against Mycobacterium tuberculosis H37Rv (ATCC 27294) strain.
AID285194Antimicrobial activity against Escherichia coli M064 mutant with AG100 lon1::IS186 acrR::IS genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID541087Antibacterial activity against 1 x10'6 to 5 x10'6 CFU/ml methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as log decrease in bacterial count at MIC after 6 hrs by time kill study2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID285184Antimicrobial activity against community-acquired methicillin-resistant Staphylococcus aureus Panton-Valentine leukocidin positive by time-kill methodology2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
AID406469Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as logarithmic-growth-phase minimal bactericidal concentration after 24 hrs by macrotube dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID1427043Antitubercular activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 after 12 days by XTT reduction menadione assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID1220558Fraction unbound in Beagle dog brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1411652Antimycobacterial activity against Mycobacterium tuberculosis2017MedChemComm, Nov-01, Volume: 8, Issue:11
The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents.
AID1399136Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by BACTEC 460 radiometric method2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
A novel synthesis of 2-arylbenzimidazoles in molecular sieves-MeOH system and their antitubercular activity.
AID294763Antibacterial activity against methicillin-resistant Staphylococcus aureus 906 after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID599450Antitubercular activity against Mycobacterium tuberculosis H37Rv after 24 hrs by BACTEC radiometric susceptibility assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
2,3-dideoxy hex-2-enopyranosid-4-uloses as promising new anti-tubercular agents: design, synthesis, biological evaluation and SAR studies.
AID1212119Induction of CYP1A2 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID292288Antibacterial activity against Enterobacter aerogenes after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID305234Ratio of MIC for Arr-2 positive Escherichia coli CGSC 5163 lpxC101 mutant bearing pCTV104 to MIC for Arr-2 negative Escherichia coli CGSC 5163 lpxC101 mutant bearing pCTV104P2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID1687559Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 assessed as inhibition of microbial growth by classical test tube method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID305224Antimicrobial activity against rifampin-sensitive Staphylococcus aureus ATCC 292132007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID1400052Bactericidal activity against Streptococcus pneumoniae ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1476352Antitubercular activity against replicating stage Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1819093Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 1 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID1061123Antimicrobial activity against Mycobacterium tuberculosis H37Rv-CV-Lux AB after 10 days by low oxygen recovery assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazines that have antibacterial activity and also inhibit inorganic pyrophosphatase.
AID406606Cmax in albino guinea pig cage fluid at 12.5 mg/kg, ip administered as single dose2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID1626618Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y and parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID69954Antimicrobial activity derived as minimum inhibitory concentration are determined using brain-heart infusion medium against Escherichia coli ML/35.1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID103837In vitro activity of compound against slowly growing Mycobacterium scrofulaceum 12931990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID369918Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected Swiss mouse assessed as reduction of bacterial count in lungs at 10 mg/kg after 12 days infection weekly 5 times for 1 month2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID1210924Inhibition of AADAC in human jejunum microsome2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID1706098Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 assessed as inhibition of bacterial growth by agar plate dilution method
AID1827059Antibacterial activity against Listeria ivanovii BAA-139 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID559096Antimicrobial activity against Escherichia coli K-12 BW25113 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The chromosomal toxin gene yafQ is a determinant of multidrug tolerance for Escherichia coli growing in a biofilm.
AID1327576Cytotoxicity against human SH-SY5Y cells assessed as effect on cell viability at 50 uM measured after 24 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID1781727Antibacterial activity against Acinetobacter baumannii BAA-1605 ssessed as bacterial growth inhibition in presence of outermembrane permeabilizer, PMBN incubated for 16 to 18 hrs by broth microdilution method
AID1483732Selectivity ratio of MIC for Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit a K179N mutant supplemented with 8 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione to MIC for Mycobacterium tuberculosis 2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1678518Antibacterial activity against Staphylococcus aureus ATCC 29213 incubated overnight by broth dilution method2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID373956Post antibiotic effect against Mycobacterium tuberculosis H37Rv ATCC 2517 infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L administered for 2 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID425400Antibacterial activity against Escherichia coli isolate HM605 isolated from colonic mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID94213Minimum inhibitory concentration of compound tested for antibacterial activity against Klebsiella pneumoniae ottaviani1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antibacterial activity of some ester, amides, and hydrazides of 3-carboxyrifamycin S. Relationship between structure and activity of ansamycins.
AID1596895Antibacterial activity against Escherichia coli ATCC 25922 incubated for 16 to 18 hrs by broth microdilution assay
AID1827061Antibacterial activity against methicillin-resistant Staphylococcus aureus BAA-44 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID534425Antibacterial activity against Mycobacterium bovis BCG-Glaxo2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID531291Antimicrobial activity against Clostridium difficile isolate 63 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID313231Antimicrobial activity against Micrococcus luteus at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID582810Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS05417 harboring MLST sequence type ST17 and pulsotype A expressing vanA gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID104011Activity against Mycobacterium tuberculosis (H37Rv) using the standard BACTEC radiometric growth assay2000Journal of medicinal chemistry, Aug-24, Volume: 43, Issue:17
A new class of antituberculosis agents.
AID398475Inhibition of RNA synthesis in Bacillus subtilis assessed as incorporation of [3H]uridine at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2003Journal of natural products, Feb, Volume: 66, Issue:2
Antibacterial diterpenes from Calceolaria pinifolia.
AID1653508Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.3 mg/L incubated for 24 hrs (Rvb = 1.05 +/- 0.16 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1687470Antitubercular activity against PAS/INH/EMB/RMP-resistant Mycobacterium tuberculosis Spec.210 assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID572554AUC (0 to 24 hrs) in indonesian pulmonary tuberculosis patient at 600 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1879547Antibacterial activity against Bacteroides fragilis ATCC 252852022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID209408In vitro antibacterial activity of compound against Streptococcus faecalis ATCC 7080.1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID372543Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 12-48 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID564986Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay in presence of 0.5 mg/liter reserpine2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID369451Antimicrobial activity against Staphylococcus epidermidis2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activities of different inhibitors of bacterial transcription against Staphylococcus epidermidis biofilm.
AID373972Clearance in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1462367Antitubercular activity against Mycobacterium tuberculosis H37Ra BSL2 infected in THP-1 macrophages after 5 days post infection by luciferase reporter gene assay2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
2-N-Arylthiazole inhibitors of Mycobacterium tuberculosis.
AID1862200Antimycobacterial activity against clinical isolate multidrug resistant Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
AID1891917Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID669844Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.
AID529191Antibacterial activity against Klebsiella pneumoniae ATCC 10031 with arr-5 gene by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID1287501Antitubercular activity against dormant state Mycobacterium tuberculosis H37Ra assessed as viable cells after 12 days by XTT reduction menadione assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID534108Antibacterial activity against Pasteurella multocida pm0527 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1194334Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate alamar blue assay method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID1143266Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis 136570 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID529523Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis isolate NJT210EMB-R-C3 assessed as bacterial colony formation at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID669187Antitubercular activity against Mycobacterium tuberculosis H37Rv in anaerobic conditions after 11 days by luminescnece-based low-oxygen recovery assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1566194Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial cell growth by resazurin reduction method2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID571194Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 1 ug/ml NAB739 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1359430Antibacterial activity against methicillin-resistant Staphylococcus aureus USA400 NRS123 after 1 passages over 2 weeks by broth microdilution method2018European journal of medicinal chemistry, May-25, Volume: 152Alkoxyphenylthiazoles with broad-spectrum activity against multidrug-resistant gram-positive bacterial pathogens.
AID582987Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0761 harboring MLST sequence type ST78 and pulsotype C expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1185138Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase A2B2 holoenzyme supercoiling activity using relaxed pBR322 substrate incubated for 90 mins by ethidium bromide staining based gel electrophoresis method2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID1901697Antimycobacterial activity against Mycobacterium tuberculosis 14862 clinical isolate measured by MABA assay2022European journal of medicinal chemistry, Mar-05, Volume: 231Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.
AID1290448Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 2 to 4 weeks by Lowensteine-Jensen method2016European journal of medicinal chemistry, Apr-13, Volume: 112Novel morpholinoquinoline nucleus clubbed with pyrazoline scaffolds: Synthesis, antibacterial, antitubercular and antimalarial activities.
AID1827047Antibacterial activity against Escherichia coli K-12 MG1655 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID576902Antimicrobial activity against Bacillus anthracis Sterne 7702 selected at 80 uM after 6 passages by macrodilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Oligochlorophens are potent inhibitors of Bacillus anthracis.
AID560508Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b3k5923 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID683322Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID1493169Induction of cell envelope stress in Bacillus subtilis isolate 1S34 assessed as increase in ypuA promoter activity at 30 ug after 14 to 18 hrs by beta-galactosidase reporter gene assay2017Journal of natural products, 11-22, Volume: 80, Issue:11
Cyclic Cystine-Bridged Peptides from the Marine Sponge Clathria basilana Induce Apoptosis in Tumor Cells and Depolarize the Bacterial Cytoplasmic Membrane.
AID1635729Transactivation of PXR (unknown origin) assessed as upregulation of CYP3A42016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Indole-2-carboxamide-based MmpL3 Inhibitors Show Exceptional Antitubercular Activity in an Animal Model of Tuberculosis Infection.
AID1778128Antimicrobial activity against Escherichia coli assessed as microbial growth inhibition by CLSI-protocol based broth microdilution assay2021Journal of natural products, 04-23, Volume: 84, Issue:4
Opportunities and Limitations for Assigning Relative Configurations of Antibacterial Bislactones using GIAO NMR Shift Calculations.
AID292311Antibacterial activity against Bacillus subtilis ATCC 6633 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID511061Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at MIC concentration after up to 28 days2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles.
AID582984Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS0649 harboring MLST sequence type ST17 and pulsotype B expressing vanA gene cluster isolated from exudate of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID293589Antibacterial activity against Escherichia coli ATCC 25922 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1071104Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate Alamar blue assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1868117Anti-tubercular activity against Mycobacterium tuberculosis CF76 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID529528Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT30167 expressing embB codon 306 ATG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1891923Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in log10CFU at 10 X MIC measured after 5 to 6 days by time kill assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID341772Tmax in Mycobacterium tuberculosis infected patient at 6 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID1716713Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as fractional inhibitory concentration index in presence of doxycycline incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1879555Antibacterial activity against Bifidobacterium ATCC 156982022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID571392Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID279350Inhibition of RNA synthesis in Staphylococcus aureus ATCC 29213 assessed as [3H]uridine incorporation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Dual targeting of GyrB and ParE by a novel aminobenzimidazole class of antibacterial compounds.
AID1739763Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition incubated for 3 weeks by Microplate Alamar Blue Assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
AID495750Antimicrobial activity against Escherichia coli J5 by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime.
AID625276FDA Liver Toxicity Knowledge Base Benchmark Dataset (LTKB-BD) drugs of most concern for DILI2011Drug discovery today, Aug, Volume: 16, Issue:15-16
FDA-approved drug labeling for the study of drug-induced liver injury.
AID531262Antimicrobial activity against Clostridium difficile isolate 34 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1879550Antibacterial activity against Bacteroides gracilis ATCC 33236 MMX 12702022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1626602Antimicrobial activity against Staphylococcus aureus isogenic forms expressing gyrA S84L mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1247200Anti-tubercular activity against rifampicin, isoniazid, ethambutol and pyrazinamide-sensitive active phage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells by neutral red assay2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Design and synthesis of 11α-substituted bile acid derivatives as potential anti-tuberculosis agents.
AID509625Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB529 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID604023Ratio of total drug level in brain to plasma in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID540210Clearance in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID425189Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
A microwave-assisted facile regioselective Fischer indole synthesis and antitubercular evaluation of novel 2-aryl-3,4-dihydro-2H-thieno[3,2-b]indoles.
AID559097Antimicrobial activity against yafQ gene-deficient Escherichia coli K-12 BW25113 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The chromosomal toxin gene yafQ is a determinant of multidrug tolerance for Escherichia coli growing in a biofilm.
AID1577324Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 7 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID328110Antibacterial activity against Mycobacterium tuberculosis H37Rv at 0.5 ug/mL by microplate alamar blue assay2008Journal of natural products, Mar, Volume: 71, Issue:3
Semisynthetic studies on the manzamine alkaloids.
AID381900Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by broth microdilution assay2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
N-Aroyl-3,5-bis(benzylidene)-4-piperidones: a novel class of antimycobacterial agents.
AID530776Antimicrobial activity against Clostridium difficile isolate 7 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID571455Antibacterial activity against Escherichia coli NCTC13353 by Etest method in presence of 4 ug/ml NAB70622008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID583691Antimicrobial activity against methicillin-resistant Staphylococcus aureus 10*3d1 harboring hypothetical protein SA1826 14A mutant gene after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1055938Antimycobacterial activity against Mycobacterium tuberculosis H37Rv under normoxic condition after 7 days by MABA assay in presence of 4% bovine serum albumin2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID757715Antibacterial activity against Bacillus subtilis subsp. subtilis assessed as growth inhibiiton after 18 hrs2013European journal of medicinal chemistry, Jul, Volume: 65Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: structure-based optimization of a virtual screening hit.
AID360006Antifungal activity against Candida albicans B311 after 48 hrs by modified well microplate assay2001Journal of natural products, May, Volume: 64, Issue:5
Antimalarial, cytotoxic, and antifungal alkaloids from Duguetia hadrantha.
AID1890848Selectivity index, ratio of MIC90 for antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC::PDFMtb overexpression mutant to MIC90 for antimycobacterial activity against wild type Mycobacterium smegmatis mc2 1552022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID1296407Cytotoxicity against primary human hepatocytes assessed as cell viability after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1395985Bactericidal activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 planktonic cells after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID525124Suppression of resistance related recombination in Staphylococcus aureus RN4220 at 0.25 times MIC at 42 degC2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID1514472Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as colony forming units at 0.002 to 64 ug/ml measured day 7 post dose by time kill assay (Rvb = 0 log10CFU/ml)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1069172Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 assessed as growth inhibition at MIC after 7 days by broth microdilution assay relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1079941Liver damage due to vascular disease: peliosis hepatitis, hepatic veno-occlusive disease, Budd-Chiari syndrome. Value is number of references indexed. [column 'VASC' in source]
AID375939Antibacterial activity against methicillin-resistant Staphylococcus aureus 78-13607A after 24 hrs by broth microdilution method2006Journal of natural products, Apr, Volume: 69, Issue:4
Antibacterial, partially acetylated oligorhamnosides from Cleistopholis patens.
AID1443991Induction of mitochondrial dysfunction in Sprague-Dawley rat liver mitochondria assessed as inhibition of mitochondrial respiration per mg mitochondrial protein measured for 20 mins by A65N-1 oxygen probe based fluorescence assay2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1276378Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID1632664Antitubercular activity against active Mycobacterium bovis BCG ATCC 35734 after 8 days by nitrate reductase assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID1386454Antibacterial activity against Mycobacterium bovis BCG Pasteur infected in mouse J774A.1 cells assessed as reduction in bacterial burden at 0.3 ug/ml after 72 hrs post infection relative to control2018Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18
Structure-Based Design of MptpB Inhibitors That Reduce Multidrug-Resistant Mycobacterium tuberculosis Survival and Infection Burden in Vivo.
AID1856893Induction of cell membrane disruption in Escherichia coli ATCC 25922 assessed as increase in PI uptake measured after 30 to 120 mins by propidium iodide staining based FACS flow cytometry analysis (Rvb = 6.0 %)2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID580850Antimicrobial activity against Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID493955Antimicrobial activity aagainst Mycobacterium sp. Mc2 in presence of acetate2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.
AID1423479Antibacterial activity against Enterobacter cloacae subsp. cloacae ATCC 13047 after 24 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1567122Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID1232406Antimycobacterial activity against Mycobacterium bovis BCG after 7 days2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides.
AID698819Antimycobacterial activity against Mycobacterium tuberculosis infected in human assessed as log reduction of bacterial count at 400 mg, qd measured up to 7 days2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID776899Inhibition of Escherichia coli RNA polymerase holo enzyme by transcription assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID268909Cytotoxicity against Vero cell line2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID1304526Antibacterial activity against Mycobacterium tuberculosis BSG001 incubated overnight by microbroth-dilution method2016Journal of natural products, Mar-25, Volume: 79, Issue:3
Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.
AID294759Antibacterial activity against Mycobacterium tuberculosis H37Rv after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID1252190Antimycobacterial activity against Mycobacterium tuberculosis in 7H12 medium by microplate alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-01, Volume: 25, Issue:21
Syntheses and evaluation of substituted aromatic hydroxamates and hydroxamic acids that target Mycobacterium tuberculosis.
AID1879553Antibacterial activity against metronidazole-resistant Bacteroides vulgatus 34902022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID285561Bactericidal activity against 26-day old non-replicating Mycobacterium tuberculosis H37Rv at 1 ug/ml after 1 day by Wayne in anaerobic condition dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID1825032Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 cultured in GAST media incubated for 8 days by resazurin microtiter assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
AID297685Antimycobacterial activity against Mycobacterium bovis BCG by microplate alamar blue assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
AID520088Antimicrobial activity against Aeromonas hydrophila subsp. hydrophila ATCC 7966 harboring plasmid pEX19Gm by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID531031Antimicrobial activity against Clostridium difficile isolate 78 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID564092Antimicrobial activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 by M7-A6 method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID1636357Drug activation in human Hep3B cells assessed as human CYP3A4-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID395778Antibacterial activity against ceftriaxone-resistant Bacillus subtilis isolate after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID1664593Antitubercular activity against Mycobacterium bovis BCG assessed as bacterial growth inhibition by alamar blue staining based assay2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives.
AID434060Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced [3H]arachidonic acid release measured after 4 hrs of IL1-beta challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1337862Selectivity index, ratio of GI50 for HUVEC to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID531038Antimicrobial activity against Clostridium difficile isolate 5 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1668175Antibacterial activity against vancomycin-resistant Staphylococcus aureus assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID523662Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta204 with RNA polymerase beta subunit L463I mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID664308Antituberculosis activity against Mycobacterium tuberculosis H37Rv by BACTEC MGIT method2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents.
AID1185708Antibacterial activity against Staphylococcus aureus ATCC 4163 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID580849Antimicrobial activity against Mycobacterium avium2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1467476Antibacterial activity against Bacillus subtilis incubated for overnight by microdilution method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID414461Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
AID530778Antimicrobial activity against Clostridium difficile isolate 9 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID531051Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 18 expressing RpoB R505K mutant by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID325119Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 2 ug/ml after 4 weeks by BACTED460 method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis.
AID586046Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type 2 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1542213Solubility of the compound in water at pH 7 by UV-vis spectrophotometric analysis2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID1879494Antibacterial activity against Helicobacter pylori clinical isolate China2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID530870Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB D471G mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1154347Antimycobacterial activity against Mycobacterium tuberculosis over expressing DprE1 after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1154351Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis over expressing DprE1 C387S mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1634255Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 6.25 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID217726Compound was tested for its cytotoxicity on Vero cells2000Bioorganic & medicinal chemistry letters, Apr-03, Volume: 10, Issue:7
Isoniazid-related copper(II) and nickel(II) complexes with antimycobacterial in vitro activity. Part 9.
AID1242346Antimycobacterial activity against moxifloxacin resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA G88N mutant incubated for 7 days by microdilution method2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID1743131Inhibition of ATP synthase in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth incubated for 7 days by microplate alamar blue assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
AID487839Antimycobacterial activity against Mycobacterium fortuitum after 48 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID1778095Antitubercular activity against INH, SM, RFP, EMB, PAS, Prothionamide 1321, Capreomycin-resistant Mycobacterium tuberculosis 14862 assessed as bacterial growth inhibition incubated for 7 days by MABA
AID1869567Antibacterial activity against Staphylococcus aureus DSM 20231 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID297686Antimycobacterial activity against Mycobacterium bovis BCG at 0.5 to 1.0 uM by microplate alamar blue assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
AID774608Antimicrobial activity against Mycobacterium intracellulare2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID1634260Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 100 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1194223Tuberculostatic activity against Mycobacterium tuberculosis Spec. 192 by two-fold classical test-tube method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel 2-(2-phenalkyl)-1H-benzo[d]imidazoles as antitubercular agents. Synthesis, biological evaluation and structure-activity relationship.
AID571664Ratio of the MIC for Proteus vulgaris ATCC 13315 in the absence of NAB7074 to MIC for Proteus vulgaris ATCC 13315 in the presence of 4 ug/ml of NAB70742008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID511120T>MIC in Acinetobacter baumannii infected New Zealand rabbit meningitis model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID672350Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by BACTEC method2012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives.
AID1262570Metabolic stability in mouse liver microsomes assessed as residual compound at 0.1 uM after 30 mins by LC-MS/MS method in presence or absence of NADPH2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID656232Antimycobacterial activity against isoniazid-, rifampin-, ofloxacin-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID452744Antibacterial activity against Escherichia coli MG16552010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.
AID1212154Induction of CYP2D6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1296400Cytotoxicity against MDCK2-MDR1 cells assessed as cell viability after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID268911Antibacterial activity against Mycobacterium avium2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID144146Antibacterial activity against Mycobacterium kansasii1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID1703747Aqueous solubility of compound in phosphate-buffered saline at pH 7.4 incubated for 2 hrs by turbidometric analysis2020European journal of medicinal chemistry, Sep-15, Volume: 202Evaluation of N-phenyl-2-aminothiazoles for treatment of multi-drug resistant and intracellular Staphylococcus aureus infections.
AID616940Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 2 weeks by BACTEC 460 radiometric method2011Bioorganic & medicinal chemistry letters, Sep-15, Volume: 21, Issue:18
Discovery of novel antitubercular 3a,4-dihydro-3H-indeno[1,2-c]pyrazole-2-carboxamide/carbothioamide analogues.
AID1916622Antitubercular activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as bacterial growth inhibition by XTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID1355415Antimycobacterial activity against Mycobacterium intracellulare ATCC 23068 after 70 to 74 hrs by Alamar blue based CLSI method2018Journal of natural products, 06-22, Volume: 81, Issue:6
Chloramphenicol Derivatives with Antibacterial Activity Identified by Functional Metagenomics.
AID545045Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ082 from patient bile by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID555302Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1427052Selectivity index, ratio of GI50 for human PANC1 cells to MIC for dormant stage of Mycobacterium tuberculosis H37Ra ATCC 251772017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID495510Antibacterial activity against Acinetobacter baumannii BM4454 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID1551812Antibacterial activity against Bacillus anthracis incubated for 18 hrs post 30 mins pre-diffusion by disk diffusion method2019European journal of medicinal chemistry, Jul-01, Volume: 173Antibacterial activity study of 1,2,4-triazole derivatives.
AID515224Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 4 weeks by broth microdilution assay2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Anti-tubercular agents. Part 5: synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners.
AID292419Antitubercular activity against Mycobacterium tuberculosis SS92007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID313250Antimicrobial activity against Mycobacterium tuberculosis2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID326287Antibacterial activity against methicillin-resistant Staphylococcus aureus 4342 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID514969Selectivity index, ratio of CC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives.
AID545918Antimicrobial activity against in Escherichia coli ATCC 25922 in presence of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1423482Cytotoxicity against HEK293 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue reporter assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1589013Selectivity index, ratio of CC50 for cytotoxicity in African green monkey Vero cells to MIC for anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv
AID1564636Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 16995 assessed as reduction in bacterial cell growth incubated for 7 days by microplate alamar blue assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
AID543800Bactericidal activity against Haemophilus influenzae VT450-2006 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID285198Antimicrobial activity against Escherichia coli M084 mutant AG100 lon4::IS186 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID683685Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2012European journal of medicinal chemistry, Nov, Volume: 57The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
AID1557244Antitubercular activity against resistant Mycobacterium tuberculosis 8 harboring rpoB His526Pro mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID373938fAUC (0 to 168 hrs) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 2100 mg, po administered twice a week2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID571448Antibacterial activity against Enterobacter cloacae ATCC 23355 by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID604022Fraction unbound in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID283159Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2526 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1272964Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth at 50 uM after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.
AID1296404Cytotoxicity against human HeLa cells assessed as cell viability at 20 uM after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID531287Antimicrobial activity against Clostridium difficile isolate 59 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID309703Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Preparation and antitubercular activities of alkylated amino alcohols and their glycosylated derivatives.
AID1856874Antimicrobial activity against Staphylococcus aureus ATCC 25923 in presence of FeCl32022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID774299Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by normoxic environment for 28 hrs by low oxygen recovery assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID425407Antibacterial activity against mucosa-associated Escherichia coli isolate HM456 isolated from patient with irritable bowel syndrome or sporadic polyps after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID559095Bactericidal activity against Escherichia coli K-12 BW25113 biofilm harboring pCA24N ptac::yafQ plasmid assessed as log reduction of viable cells after 24 hrs pretreated with 5 uM of IPTG for 4 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The chromosomal toxin gene yafQ is a determinant of multidrug tolerance for Escherichia coli growing in a biofilm.
AID774296Antimycobacterial activity against streptomycin-resistant Mycobacterium tuberculosis ATCC 358202013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID29851Half life was measured as time taken to decrease half of its initial concentration2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Property-based design: optimization of drug absorption and pharmacokinetics.
AID571660Ratio of the MIC for Acinetobacter baumannii ATCC 19606 in the absence of NAB7070 to MIC for Acinetobacter baumannii ATCC 19606 in the presence of 4 ug/ml of NAB70702008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID509624Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB534 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID565781Antimicrobial activity against Neisseria meningitidis harboring rpoB15 H552N mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1400054Bactericidal activity against Klebsiella pneumoniae ATCC 12019 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1400059Antibacterial activity against Streptococcus salivarius ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID581659Fraction unbound in human plasma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID666966Growth inhibition of Mycobacterium tuberculosis H37Rv at 6.25 ug/mL after 12 to 28 days relative to control2012European journal of medicinal chemistry, Aug, Volume: 54New N-arylamino biquinoline derivatives: synthesis, antimicrobial, antituberculosis, and antimalarial evaluation.
AID533863Antibacterial activity against toxin-positive Clostridium difficile clinical isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
In vitro activity of OPT-80 tested against clinical isolates of toxin-producing Clostridium difficile.
AID671436Antimycobacterial activity against Mycobacterium bovis BCG assessed as inhibition of microbial growth at 0.5 ug/ml incubated for 6 days by MABA method2012Bioorganic & medicinal chemistry, Jul-01, Volume: 20, Issue:13
Discovery of novel 5-(ethyl or hydroxymethyl) analogs of 2'-'up' fluoro (or hydroxyl) pyrimidine nucleosides as a new class of Mycobacterium tuberculosis, Mycobacterium bovis and Mycobacterium avium inhibitors.
AID278674Antibacterial activity against Enterococcus faecalis isolate 57442007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1293908Selectivity index, ratio of GI50 for human PANC1 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1411649Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days by broth dilution method2017MedChemComm, Nov-01, Volume: 8, Issue:11
The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents.
AID1908124Antibacterial activity against vancomycin resistant Enterococcus faecium ATCC 700221 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID1454448Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis 12525 after 7 days by microplate alamar blue assay2017ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents.
AID1716631Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as reduction in bacterial growth by measuring chloramphenicol MIC at 4 ug/ml incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay (Rvb = 1024 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1459057Antitubercular activity against Mycobacterium tuberculosis H37Rv measured on day 7 post dose by microplate alamar blue assay2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
AID1311235Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-42016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1854290Bactericidal activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in colony formation at 1 to 10 times of MIC incubated for 6 to 7 days by time-kill assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID296133Antimicrobial activity against Mycobacterium tuberculosis after 20 hrs by broth microdilution method2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
Antimicrobial and cytotoxic activity of agelasine and agelasimine analogs.
AID1444296Antimycobacterial activity against Mycobacterium avium CNCTC My 330/80 after 14 days by micromethod2017European journal of medicinal chemistry, Apr-21, Volume: 130Structure-activity relationship studies on 3,5-dinitrophenyl tetrazoles as antitubercular agents.
AID1636356Drug activation in human Hep3B cells assessed as human CYP2C9-mediated drug metabolism-induced cytotoxicity measured as decrease in cell viability at 300 uM pre-incubated with BSO for 18 hrs followed by incubation with compound for 3 hrs in presence of NA2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
Development of a cell viability assay to assess drug metabolite structure-toxicity relationships.
AID1185145Antimicrobial activity against 5-(((3S,4R)-3-fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase D89N mutant2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID1287402Antimicrobial activity against Candida albicans after 48 hrs by serial two-fold microbroth dilution method2016Bioorganic & medicinal chemistry letters, Mar-15, Volume: 26, Issue:6
One-pot synthesis and antimicrobial evaluation of novel 3-cyanopyridine derivatives of (-)-β-pinene.
AID531016Antimicrobial activity against Clostridium difficile isolate 63 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1400060Bactericidal activity against Streptococcus salivarius ATCC 6301 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1869575Antibacterial activity against Enterobacter cloacae DSM 30054 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID582513Cmax in Staphylococcus epidermidis ATCC 27626 infected Wistar rat tissue cage fluid at 25 mg/kg, ip measured on day 42008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID297683Antimycobacterial activity against Mycobacterium avium ATCC 25291 by microplate alamar blue assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
AID571203Antibacterial activity against Escherichia coli ATCC 25992 by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID665277Antitubercular activity against Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2012European journal of medicinal chemistry, Jul, Volume: 53A solvent free, four-component synthesis and 1,3-dipolar cycloaddition of 4(H)-pyrans with nitrile oxides: synthesis and discovery of antimycobacterial activity of enantiomerically pure 1,2,4-oxadiazoles.
AID1406743Cytotoxicity against HEK293 cells assessed as inhibition of cell viability at 25 ug/ml after 48 hrs by MTT assay relative to control2018European journal of medicinal chemistry, Aug-05, Volume: 156Synthesis of carbohydrazides and carboxamides as anti-tubercular agents.
AID1191017Antimycobacterial activity against Mycobacterium kansasii ATCC 12478 assessed as reduction in bacterial growth incubated for 6 days by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID297687Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by microplate alamar blue assay2007Journal of medicinal chemistry, Sep-20, Volume: 50, Issue:19
Inhibition of Mycobacterium tuberculosis, Mycobacterium bovis, and Mycobacterium avium by novel dideoxy nucleosides.
AID1077231Antimycobacterial activity against Mycobacterium smegmatis MC2 155 ATCC 14468 after 32 hrs by broth microdilution method2014European journal of medicinal chemistry, Apr-09, Volume: 76Convenient one-pot synthesis, anti-mycobacterial and anticancer activities of novel benzoxepinoisoxazolones and pyrazolones.
AID511113Antiinflammatory activity in Acinetobacter baumannii 1327-infected New Zealand rabbit meningitis model assessed as in WBC count at 25 mg/kg, iv after 6 hrs (RVb = 1 cells/ul)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID245618In vitro actual minimum inhibitory concentration value of the compound was determined against Mycobacterium tuberculosis H37Rv strain; Range is 0.015-0.1252005Journal of medicinal chemistry, Mar-24, Volume: 48, Issue:6
Synthesis of new quinoxaline-2-carboxylate 1,4-dioxide derivatives as anti-Mycobacterium tuberculosis agents.
AID373964Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as concentration needed to achieve 50% effect on maximal g2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID369459Inhibition of Staphylococcus epidermidis biofilm formation assessed as reduction of >2 log 10 bacterial count in biofilm after 24 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activities of different inhibitors of bacterial transcription against Staphylococcus epidermidis biofilm.
AID144877Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to pyrazinamide (PZA)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1664592Antitubercular activity against Mycobacterium tuberculosis H37Ra assessed as bacterial growth inhibition at 1 ug/ml by MABA relative to control2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives.
AID1437019Antimycobacterial activity against isoniazid/rifampicin/ethambutol-sensitive Mycobacterium tuberculosis H37Rv after 4 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
AID510987Antimicrobial activity against Acinetobacter baumannii 506 after 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1167353Antibacterial activity against Escherichia coli D21 IpxC101 deletion mutant after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1235587Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as reduction in bacterial growth incubated at 37 degC for 7 days by alamar blue dye based assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents.
AID683686Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 10 days by low oxygen recovery assay2012European journal of medicinal chemistry, Nov, Volume: 57The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
AID625289Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver disease2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1827055Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID143695Antimycobacterial activity against Mycobacterium avium (NIHJ1605)2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.
AID1337870Selectivity index, ratio of GI50 for human PANC1 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1634243Antimycobacterial activity against Mycobacterium abscessus subsp. bolletii assessed as reduction in microbial growth by CLSI method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID341768Cmax in Mycobacterium tuberculosis infected patient at 6 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID529192Antibacterial activity against Escherichia coli DHalpha harboring arr-4 gene after 20 hrs by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID1497854Antibacterial activity against Bacillus subtilis ATCC 66332018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID1296448Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as growth inhibition at 0.05 ug/ml preincubated for 1 hr followed by radiolabeling with [14C]-uracil, [14C]-methionine for 24 hrs2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1287510Selectivity index, ratio of GI50 for human A549 cells to MIC for dormant state Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID144208In vitro antibacterial activity of compound against Neisseria gonorrhoeae ISM 68/1261990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1070192Antimycobacterial activity against Mycobacterium szulgai MNT1100 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1775048Agonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs by luciferase reporter assay
AID276758Antimycobacterial activity against rifampicin and rifabutin sensitive Mycobacterium tuberculosis2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1337872Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1879537Antibacterial activity against fluoroquinolone-resistant Clostridioides difficile CB1941 harboring gyrAD71Y/T82A mutant measured after 3 days2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1164281Antimicrobial activity against wild-type Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 5 days by microdilution method2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID1869526Antibacterial activity against methicillin-resistant Staphylococcus aureus R6101 measured after 24 hrs by broth microdilution method
AID1891918Antimycobacterial activity against Streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 35820 assessed as inhibition of bacterial growth incubated for 48 hrs by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID493951Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.
AID355266Antitubercular activity against Mycobacterium tuberculosis H37Rv after 21 days by broth microdilution method1997Journal of natural products, Dec, Volume: 60, Issue:12
Norditerpenoids and diterpenoids from Salvia multicaulis with antituberculous activity.
AID574800Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 obtained from sputum of patient at 1 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1296396Cytotoxicity against human HuH7 cells assessed as cell viability after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1685705Antimicrobial activity against Escherichia coli DH5alpha assessed as inhibition of bacterial growth incubated for overnight by CLSI method2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Hydraphiles enhance antimicrobial potency against Escherichia coli, Pseudomonas aeruginosa, and Bacillus subtilis.
AID1692050Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth at 100 ug/ml preincubated for 72 hrs followed by phAE202 and Cacl2 addition and measured after 4 hrs by by luciferase reporter mycobacterio-phag2020European journal of medicinal chemistry, Jul-15, Volume: 198Indole chalcones: Design, synthesis, in vitro and in silico evaluation against Mycobacterium tuberculosis.
AID1372628Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week in presence of efflux pump inhibitor verapamil by MABA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID246808Effective concentration required to reduce CFU of Mycobacterium tuberculosis Erdman (ATCC 35801) strain was determined in monolayers of mouse bone marrow macrophages; Range is 0.5-1.52004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
In vitro advanced antimycobacterial screening of cobalt(II) and copper(II) complexes of fluorinated isonicotinoylhydrazones.
AID582517Ratio of AUC in Wistar rat tissue cage fluid to MIC for Staphylococcus epidermidis ATCC 27626 at 25 mg/kg, ip measured on day 42008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID1678517Antimycobacterial activity against recombinant Mycobacterium tuberculosis H37Rv expressed in green fluorescence protein by measuring increase in fluorescence after 10 days in presence of middlebrook 7H9/OADC medium by GFP reporter gene assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID1851923Antimycobacterial activity against Mycobacterium smegmatis mc2155 ATCC 700084 assessed as bacterial growth inhibition incubated for 24 hrs under normoxic condition by resazurin microtiter assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID532975Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 192010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID515924Antibacterial activity against Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID1185715Antibacterial activity against Salmonella abony NCTC 6017 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1444299Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 14 days by micromethod2017European journal of medicinal chemistry, Apr-21, Volume: 130Structure-activity relationship studies on 3,5-dinitrophenyl tetrazoles as antitubercular agents.
AID1055963Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate X004439 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1685707Antimicrobial activity against Pseudomonas aeruginosa assessed as inhibition of bacterial growth incubated for overnight by CLSI method2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Hydraphiles enhance antimicrobial potency against Escherichia coli, Pseudomonas aeruginosa, and Bacillus subtilis.
AID1457522Antibacterial activity against Bacillus subtilis assessed as inhibition of protein synthesis at 2 mg/L after 50 mins by [35S]-methionine incorporation assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents.
AID560509Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b4k6307 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1765757Antimycobacterial activity against Mycobacterium bovis BCG assessed as inhibition of bacterial growth at measured by microplate alamar blue assay2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Design and synthesis of novel 5-alkynyl pyrimidine nucleosides derivatives: Influence of C-6-substituent on antituberculosis activity.
AID297117Antibacterial activity against Mycobacterium fortuitum NIHJ1615 after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1447545Antibacterial activity against multidrug-resistant Acinetobacter baumannii AB027 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID411981Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Selective activity against Mycobacteriumtuberculosis of new quinoxaline 1,4-di-N-oxides.
AID1687471Antitubercular activity against Mycobacterium tuberculosis Spec.192 assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID1398739Agonist activity at VP16-fused human PXR expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 08-15, Volume: 26, Issue:15
Development of novel silanol-based human pregnane X receptor (PXR) agonists with improved receptor selectivity.
AID1337839Growth inhibition of Mycobacterium bovis BCG ATCC 35743 at dormant stage measured after 12 days by nitrate reductase dye based two fold dilution method2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1827080Antimycobacterial activity against Mycobacterium marinum infected in zebrafish assessed as reduction in bacterial burden at 10 uM after 6 days post infection2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
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Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1383953Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 10 days by MABA2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID256373Inhibition of growth of Mycobacterium bovis was determined using microplate alamar blue assay at 0.5-1 ug/mL concentration with compound dissolved in DMSO2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Design and studies of novel 5-substituted alkynylpyrimidine nucleosides as potent inhibitors of mycobacteria.
AID1634996Hemolytic activity in human type RBC after 1 hr2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID1781820Antimycobacterial activity against Mycobacterium smegmatis CIP7326 assessed as inhibition of mycobacterial growth incubated for 24 hrs by broth microdilution method2021Journal of natural products, 10-22, Volume: 84, Issue:10
Voatriafricanines A and B, Trimeric Vobasine-Aspidosperma-Aspidosperma Alkaloids from
AID1866010Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Isolation and biological activity of azocine and azocane alkaloids.
AID530777Antimicrobial activity against Clostridium difficile isolate 8 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID305233Antimicrobial activity against Arr-2 negative Escherichia coli CGSC 5163 lpxC101 mutant bearing pCTV104P2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID245441Minimum inhibitory concentration against sensitive Mycobacterium tuberculosis clinical isolates; N=9; Range=0.03-0.52005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents.
AID571212Antibacterial activity against Acinetobacter baumannii F264 by Etest method in presence of 1 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID341776AUC (0 to infinity) in Mycobacterium tuberculosis infected patient at 6 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID373952Ratio of Cmax to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L administered for 1 hr2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1427060Selectivity index, ratio of GI50 for human HeLa cells to MIC for active stage of Mycobacterium tuberculosis H37Ra ATCC 251772017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID1716658Antibacterial activity against Acinetobacter baumannii CAN-ICU 63169 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
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Effect of DNase and antibiotics on biofilm characteristics.
AID1210909Intrinsic clearance in rat jejunum microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
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Synthesis and biological activity of some derivatives of rifamycin P.
AID370254Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 20 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1411650Selectivity ratio of MIC for Mycobacterium smegmatis to MIC for Mycobacterium tuberculosis2017MedChemComm, Nov-01, Volume: 8, Issue:11
The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents.
AID445286Antibacterial activity against Mycobacterium avium 724S by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1706866Antimycobacterial activity against Mycobacterium chelonae ATCC 35752 by broth microdilution method2021European journal of medicinal chemistry, Feb-15, Volume: 212Synthesis and evaluation of new quinazoline-benzimidazole hybrids as potent anti-microbial agents against multidrug resistant Staphylococcus aureus and Mycobacterium tuberculosis.
AID444051Total clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID510518Cmax in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID523660Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta104 with RNA polymerase beta subunit A639S mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID400488Increase in hepatic ethylmorphine N-demethylase activity in mouse1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID669188Activation of PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID564985Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay in presence of 1 mg/liter CCCP2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1476408Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through carboxymethylcellulose vehicle as single oral dose per gavage after 1 hr by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1403701Inhibition of recombinant N-terminal His-tagged Bacillus subtilis subsp. subtilis 168 glutamate racemase expressed in Escherichia coli BL21(DE3) using D-Glutamate as substrate in presence of NADH by spectrophotometric based GDH enzyme coupled assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1174920Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID1653389Antimicrobial activity against Enterococcus faecalis ATCC 29212 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1850012Induction of CYP3A4 in human hepatocytes assessed as maximum efficacy relative to control2022Journal of medicinal chemistry, 03-10, Volume: 65, Issue:5
Synthesis and Preclinical Characterization of LY3154885, a Human Dopamine D1 Receptor Positive Allosteric Modulator with an Improved Nonclinical Drug-Drug Interaction Risk Profile.
AID580848Plasma protein binding in healthy human at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID774411Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of cell viability measured on day 3 by XTT assay in presence of menadione2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Antimycobacterial labdane diterpenes from Leucas stelligera.
AID144874Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to isoniazid (INH)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1890846Selectivity index, ratio of MIC90 for antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC empty vector to MIC90 for antimycobacterial activity against wild type Mycobacterium smegmatis mc2 1552022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID324986Antibacterial activity against Haemophilus influenzae MSC06647 by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID373044Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate CY6 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1154352Antimycobacterial activity against TMC207R-resistant Mycobacterium tuberculosis clone 8.1 over expressing DprE1 mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1241592Induction of CYP3A5 activation in human hepatocytes at 2 uM incubated for 48 hrs using testosterone substrate2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
AID465092Antibacterial activity against methicillin-resistant Staphylococcus aureus by modified NCCLS method2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Anti-infective discorhabdins from a deep-water alaskan sponge of the genus Latrunculia.
AID1400036Bactericidal activity against Mycobacterium smegmatis ATCC 607 incubated for 48 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID305231Ratio of MIC for Arr-2 positive Escherichia coli DH5-alpha bearing pCTF104 to MIC for Arr-2 negative Escherichia coli DH5-alpha bearing pCTF104P2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID293587Antibacterial activity against Klebsiella pneumoniae RSHM 574 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1303896Antibacterial activity against multidrug resistant Enterobacter cloacae subsp. cloacae CDC 442-68 (ATCC 13047) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID373032Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate FW-F1 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID543809Bactericidal activity against Escherichia coli ATCC 25922 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1182140Antitubercular activity against Mycobacterium smegmatis by checkerboard assay in presence of 7-hydroxy chlorpromazine2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID1330475Half life in rat serum at 60 mg/kg, iv2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Animal models in the pharmacokinetic/pharmacodynamic evaluation of antimicrobial agents.
AID535774Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60H containing pCK0601 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID564984Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay in presence of 0.1 mg/liter valinomycin2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1055939Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 20 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID583690Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315deltaIP harboring hypothetical protein SA1826 14E mutant gene after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1055967Antimycobacterial activity against Mycobacterium tuberculosis harboring luxABCDE under hypoxic condition after 10 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID103652In vitro activity of compound against rapidly growing Mycobacterium fortuitum 1401990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1061099Antimicrobial activity against Escherichia coli2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID530791Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 22 expressing RpoB H502N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1334262Selectivity index, ratio of GI50 for human THP1 cells to MIC90 for Mycobacterium tuberculosis H37Ra ATCC 25177 active stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID285199Antimicrobial activity against Escherichia coli M093 mutant with AG100 lon3::IS186 acrR::IS1 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID499895Antitubercular activity against Mycobacterium bovis BCG at 1 ug/ml after 6 days by microplate alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Inhibition of mycobacterial replication by pyrimidines possessing various C-5 functionalities and related 2'-deoxynucleoside analogues using in vitro and in vivo models.
AID545935Ratio of MIC for Escherichia coli ATCC 25922 to MIC for Escherichia coli ATCC 25922 in presence of 4 ug/ml of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID569259Antimycobacterial activity against Mycobacterium avium subsp. avium ATCC 2529I2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1471052Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID572546AUC (0 to 12 hrs) in kenyan pulmonary tuberculosis patient with body weight >45 kg at 600 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID370259Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 3.5 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID532960Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 42010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1476358Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in presence of 10% fetal bovine serum2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID531055Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 22 expressing RpoB H502N and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID582496Ratio of MBC to MIC for stationary phase culture of methicillin-resistant Staphylococcus aureus ATCC 292132008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID1463960Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 234/2005 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1514473Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as colony forming units at 0.002 to 64 ug/ml measured day 14 post dose by time kill assay (Rvb = 0 log10CFU/ml)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID207119Effective dose against Staphylococcus aureus in mice for subcutaneous administration.1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID1567121Antimicrobial activity against Acinetobacter baumannii ATCC 19606 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID501187Antimicrobial activity against vancomycin-resistant Enterococcus faecium 379 at 5 ug after 18 hrs by agar diffusion method2009Journal of natural products, Oct, Volume: 72, Issue:10
Norselic acids A-E, highly oxidized anti-infective steroids that deter mesograzer predation, from the Antarctic sponge Crella sp.
AID1402130Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 after 7 days by Alamar Blue assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Primaquine hybrids as promising antimycobacterial and antimalarial agents.
AID297118Antibacterial activity against Mycobacterium smegmatis Takeo after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1223080Reduction in Ugt1a6b gene expression in PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID103512In vitro activity of compound against rapidly growing Mycobacterium chelonae 14431990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1418314Antimycobacterial activity against ethambutol/isoniazid/rifampicin-resistant Mycobacterium tuberculosis incubated for 7 days by rapid direct susceptibility test
AID389102Cytotoxicity against african green monkey Vero cells2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID566906Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth in dormant phase2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Novel isatinyl thiosemicarbazones derivatives as potential molecule to combat HIV-TB co-infection.
AID532966Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 102010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1596877Antibacterial activity against Klebsiella pneumoniae ATCC BAA-1705 incubated for 16 to 18 hrs by broth microdilution assay
AID532964Antimicrobial activity against streptomycin-resistant Mycobacterium tuberculosis isolate 82010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID586052Antimicrobial activity against Staphylococcus aureus clone 4-4 harboring staphylococcal cassette chromosome mec element type 2 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1634244Antimycobacterial activity against Mycobacterium fortuitum assessed as reduction in microbial growth by CLSI method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1546638Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth after 7 days by alamar blue assay2020Journal of natural products, 01-24, Volume: 83, Issue:1
Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents.
AID1411651Antimycobacterial activity against Mycobacterium smegmatis2017MedChemComm, Nov-01, Volume: 8, Issue:11
The synthesis, biological evaluation and structure-activity relationship of 2-phenylaminomethylene-cyclohexane-1,3-diones as specific anti-tuberculosis agents.
AID531286Antimicrobial activity against Clostridium difficile isolate 58 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID765754Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 to 8 days by microplate alamar blue assay2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and binary QSAR study of antitubercular quinolylhydrazides.
AID620089Antimicrobial activity against Mycobacterium smegmatis ATCC 19420 after 7 days by resazurin assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties.
AID388040Selectivity index, ratio of IC50 for african green monkey Vero cells to IC90 for Mycobacterium tuberculosis H37Rv2008Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19
Synthesis and antituberculosis activity of 5-methyl/trifluoromethoxy-1H-indole-2,3-dione 3-thiosemicarbazone derivatives.
AID297514Antibacterial activity against Mycobacterium tuberculosis H37Rv by micro plate alamar blue assay2007Journal of medicinal chemistry, Sep-06, Volume: 50, Issue:18
Lysosome and HER3 (ErbB3) selective anticancer agent kahalalide F: semisynthetic modifications and antifungal lead-exploration studies.
AID530639Antimicrobial activity against Staphylococcus aureus CB812 harboring rpoB H481Y, gyrA S84L and gyrA S80F mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1402131Antimycobacterial activity against Mycobacterium avium complex CIT19/06 clinical isolate after 5 days by Alamar Blue assay2018European journal of medicinal chemistry, Jan-01, Volume: 143Primaquine hybrids as promising antimycobacterial and antimalarial agents.
AID1879542Antibacterial activity against rifampicin/fluoroquinolone-resistant Clostridioides difficile CB1940 harboring rpoBQ489K/gyrAA118S mutant at 1:1 compound to metronidazole molar ratio measured after 3 days in presence of metronidazole2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1426438Antimycobacterial activity against drug-succeptible Mycobacterium tuberculosis CF73 incubated for 7 days measured 24 hrs post incubation by resazurin microtiter assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
AID326293Antibacterial activity against methicillin-resistant Staphylococcus aureus 5098 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID560974Antimicrobial activity against methicillin-susceptible Staphylococcus aureus 1199 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID565794Antimicrobial activity against Neisseria meningitidis harboring rpoB46 H552N mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID429087Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates from tuberculosis patient assessed as percent resistant isolates at 40 ug/ml by absolute-concentration method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations.
AID424617Antibacterial activity against vancomycin-resistant Staphylococcus aureus AIS2006049 isolated from patients arm wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID326285Antibacterial activity against methicillin-resistant Staphylococcus aureus 859 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID727790Inhibition of Escherichia coli RNA polymerase after 1 hr by fluorescence assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID1224523Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 1 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID555322Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 after 9 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID144724Concentration required for inhibition of growth of Mycobacterium tuberculosis in level 2 assay2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials.
AID1185720Solubility in water at pH 7 and 25 degC by UV-vis spectrophotometry2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1612598Antibacterial activity against Mycobacterium tuberculosis H37Rv by resazurin dye-based assay2019European journal of medicinal chemistry, Feb-01, Volume: 163Recent advances of tetrazole derivatives as potential anti-tubercular and anti-malarial agents.
AID768652Cytotoxicity against African green monkey Vero cells2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Synthesis of novel isothiazolopyridines and their in vitro evaluation against Mycobacterium and Propionibacterium acnes.
AID400489Increase in aryl hydrocarbon hydroxylase activity in mouse1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID511122Antiinflammatory activity in Acinetobacter baumannii 1327-infected New Zealand rabbit meningitis model assessed as effect on lactate level in CSF at 25 mg/kg, iv measured at 12 hrs post dose2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID645530Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in GAS medium after 1 week by microplate alamar blue assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1304525Bactericidal activity against Escherichia coli ATCC 25922 incubated overnight by microbroth-dilution method2016Journal of natural products, Mar-25, Volume: 79, Issue:3
Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.
AID288605Antibacterial activity against Bacillus subtilis ATCC 142892007Journal of medicinal chemistry, May-31, Volume: 50, Issue:11
Antibacterial nicotinamide adenine dinucleotide synthetase inhibitors: amide- and ether-linked tethered dimers with alpha-amino acid end groups.
AID1577319Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID495753Antimicrobial activity against Escherichia coli J5 transconjugants expressing beta lactamase CTX-M-9 isolated from human flora associated C3H rat infected with Salmonella enterica serotype Virchow and treated with Cefixime-cluvulanic acid by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime.
AID449212Protection index, ratio of MNTD for african green monkey Vero cells to MIC for Mycobacterium tuberculosis CIP 1034712009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID571210Antibacterial activity against Pseudomonas aeruginosa ATCC 27853by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID145132In vitro antibacterial activity against Mycobacterium tuberculosis 1034711999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID545802Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 planktonic cells by broth microdilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID510983Antimicrobial activity against Acinetobacter baumannii 5062010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID531017Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 64 expressing RpoB H502R mutant by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID438475Antitubercular activity against Mycobacterium tuberculosis H37Rv by low oxygen recovery assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters.
AID531004Antimicrobial activity against Clostridium difficile isolate 51 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID582990Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS08257 harboring MLST sequence type ST341 and pulsotype F expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID625286Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatitis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID313232Antimicrobial activity against Escherichia coli at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID1193494Thermodynamic equilibrium solubility, log S of the compound in simulated gastric fluid at pH 1.2 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1546639Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial population at 10 ug/ml under starvation condition after 7 days by MPN assay2020Journal of natural products, 01-24, Volume: 83, Issue:1
Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents.
AID472727Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by low oxygen recovery assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
AID1070202Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35838 by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID257538Antitubercular activity against Mycobacterium tuberculosis H37Rv by agar microdilution technique2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Synthesis and antitubercular activity of 2-hydroxy-aminoalkyl derivatives of diaryloxy methano phenanthrenes.
AID1716866Antibacterial activity against Pseudomonas aeruginosa 259-96918 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1055962Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate X005282 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1905606Induction of drug resistance in Staphylococcus aureus ATCC 25923 assessed as fold increase in MIC after 5 passages by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID523655Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-CASbeta after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID572059Antibacterial activity against Acinetobacter baumannii AC0037 by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID502972Antimicrobial activity against Mycobacterium tuberculosis by alamar blue assay2007Nature chemical biology, Jun, Volume: 3, Issue:6
Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID531273Antimicrobial activity against Clostridium difficile isolate 45 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID276759Antimycobacterial activity against Mycobacterium avium-intracellulare complex measured as susceptibility at 1 ug/mL2006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1565596Antibacterial activity against Bacillus subtilis ATCC 23857 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID495752Antimicrobial activity against Escherichia coli J5 transconjugants expressing beta lactamase CTX-M-9 isolated from human flora associated C3H rat infected with Salmonella enterica serotype Virchow and treated with Cefixime by Etest method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Transfer of plasmid-mediated CTX-M-9 from Salmonella enterica serotype Virchow to Enterobacteriaceae in human flora-associated rats treated with cefixime.
AID144735In vitro inhibition of Mycobacterium tuberculosis H37Rv, determined at 2 ug/mL2004Journal of medicinal chemistry, Jun-17, Volume: 47, Issue:13
Novel pyridazino[4,3-b]indoles with dual inhibitory activity against Mycobacterium tuberculosis and monoamine oxidase.
AID1601631Antitubercular activity against multi drug resistant Mycobacterium tuberculosis 16833 after 7 days by MABA method2019European journal of medicinal chemistry, Mar-01, Volume: 165Synthesis and antitubercular evaluation of reduced lipophilic imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID292282Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by microplate Alamar blue assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID373046Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate ZS5 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID530638Antimicrobial activity against Staphylococcus aureus CB812 harboring rpoB H481Y and gyrA S80F mutant genes by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID530793Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 24 expressing RpoB H502N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID767539Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as growth inhibition at 0.3125 to 5 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID313235Antimicrobial activity against Mycobacterium phlei at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID424329Antimicrobial activity against Dialister propionicifaciens assessed as susceptibility breakpoint by CLSI method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID510522Tmax in tuberculosis patient at 10 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1274537Antibacterial activity against Mycobacterium tuberculosis H37Rv2016European journal of medicinal chemistry, Jan-27, Volume: 108Synthesis and evaluation of antibacterial and antitumor activities of new galactopyranosylated amino alcohols.
AID531293Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 65 expressing RpoB H502N and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1556504Induction of constitutive - androstane receptor in human primary hepatocytes assessed as upregulation of CYP2B6 mRNA expression at 10 uM after 24 hrs by RT-PCR analysis2019European journal of medicinal chemistry, Oct-01, Volume: 179Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.
AID1224745Antitubercular activity against Mycobacterium tuberculosis H37Rv2014European journal of medicinal chemistry, Aug-18, Volume: 83Ultrasound-assisted one-pot four-component synthesis of novel 2-amino-3-cyanopyridine derivatives bearing 5-imidazopyrazole scaffold and their biological broadcast.
AID1869574Bactericidal activity against Pseudomonas aeruginosa DSM 19880 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID208937In vitro antibacterial activity of compound against Streptococcus pneumoniae UC 411990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID145020In vitro anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv2001Bioorganic & medicinal chemistry letters, Feb-12, Volume: 11, Issue:3
Antimycobacterial in vitro activity of cobalt(II) isonicotinoylhydrazone complexes. Part 10.
AID278580Inhibition of Plasmodium falciparum FCK2 second cycle growth in erythrocytes at 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum.
AID144574The compound was tested for its ability to inhibit the growth of Mycobacterium tuberculosis strain H6/99; Resistant2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Antimycobacterial activity of ionic fullerene derivatives.
AID1905609Induction of drug resistance in Escherichia coli ATCC 25922 assessed as increase in MIC measured after 20 passages by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID369933Drug level in human plasma2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID543796Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1901696Antimycobacterial activity against Mycobacterium tuberculosis 13946 clinical isolate measured by MABA assay2022European journal of medicinal chemistry, Mar-05, Volume: 231Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.
AID1220560Fraction unbound in human occipital cortex at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID537118Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774A1 cells assessed as reduction of bacterial growth at 0.5 ug/ml after 6 days relative to untreated control2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1278839Antimycobacterial activity against Mycobacterium marinum ATCC BAA-535 infected in Zebra fish model assessed as reduction in bacterial load at 5 mg/kg, po administered for 7 days measured after 14 days by MPN assay2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID434073Drug level in serum at 600 mg2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID558239Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 2 mg/liter upto 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID487837Antimycobacterial activity against Mycobacterium smegmatis after 48 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID571456Antibacterial activity against Klebsiella pneumoniae CCUG45421 by Etest method in presence of 4 ug/ml NAB70632008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1264462Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID408867Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in J744 cells assessed as reduction in number of surviving bacteria at 0.5 ug/mL relative to control2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID404134Antibacterial activity against vancomycin-sensitive Enterococcus faecalis CL85162005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID1577326Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID329348Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in presence of iron deficient GAST-D medium2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.
AID1185714Antibacterial activity against Enterococcus faecalis ATCC 19433 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1653476Antimicrobial activity against Enterococcus faecalis ATCC 51922 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID410232Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by radiometric respiratory technique2008Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24
A facile synthesis, antibacterial, and antitubercular studies of some piperidin-4-one and tetrahydropyridine derivatives.
AID376993Antimicrobial activity against Mycobacterium tuberculosis H37Rv by alamar blue assay2006Journal of natural products, May, Volume: 69, Issue:5
Aegicerin, the first oleanane triterpene with wide-ranging antimycobacterial activity, isolated from Clavija procera.
AID370069Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1287964Antitubercular activity against dormant Mycobacterium tuberculosis H37Ra by XTT reduction menadione assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Facile synthesis of 1,3-thiazolidin-4-ones as antitubercular agents.
AID297116Antibacterial activity against Mycobacterium aurum after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1491507Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 24 hrs by neutral red uptake assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID358518Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by radiometric BACTEC 460 system2001Journal of natural products, Jan, Volume: 64, Issue:1
Antitubercular activity of triterpenoids from Lippia turbinata.
AID559764Antimycobacterial activity against PknGMsm-deficient Mycobacterium smegmatis by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID1653524Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.4 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1209482Activation of PXR in human Hu1108 hepatocytes assessed as upregulation of CYP3A4 mRNA expression at 10 uM after 24 hrs by RT-PCR analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID1331257Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by micro plate alamar blue assay2017Bioorganic & medicinal chemistry letters, 01-01, Volume: 27, Issue:1
Synthesis, screening and docking analysis of hispolon analogs as potential antitubercular agents.
AID290680Antimycobacterial activity against Mycobacterium tuberculosis H37Rv relative to control2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Synthesis and cytotoxic activity of trisubstituted-1,3,5-triazines.
AID1603258Cytotoxicity against African green monkey Vero cells measured after 72 hrs by CellTiter 96 aqueous non-radioactive cell proliferation assay
AID329355Cytotoxicity against human HeLa cells after 24 hrs2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.
AID586040Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type 1 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID681846TP_TRANSPORTER: inhibition of Digoxin uptake in Oatp2-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID297112Antibacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID1278192Antimicrobial activity against Mycobacterium tuberculosis infected in mouse J774 cells assessed as log reduction of bacterial burden at 80 ug/ml after 7 days2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
AID1332962Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by REMA method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID430079Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2009Bioorganic & medicinal chemistry, Aug-15, Volume: 17, Issue:16
Development of antitubercular compounds based on a 4-quinolylhydrazone scaffold. Further structure-activity relationship studies.
AID1400038Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1167350Antibacterial activity against wild type Pseudomonas aeruginosa PAO1 after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1296453Inhibition of proteosynthesis in Mycobacterium tuberculosis H37Ra assessed as reduction of [14C]-methionine incorporation at 0.05 ug/ml preincubated for 1 hr followed by radiolabeling with [14C]-methionine for 24 hrs by scintillation spectrometry2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID370237Tmax in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1500593Antitubercular activity against Mycobacterium tuberculosis FQ-R1 harboring gyrB D94N mutant after 5 days by fluorescence-based assay2017European journal of medicinal chemistry, Sep-29, Volume: 138The antitrypanosomal and antitubercular activity of some nitro(triazole/imidazole)-based aromatic amines.
AID1395195Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC27395 after 7 days by Alamar blue assay2018European journal of medicinal chemistry, May-10, Volume: 151Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety.
AID1427059Selectivity index, ratio of GI50 for human HeLa cells to MIC for active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID419580Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 24 hrs by microplate alamar blue assay2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
A macrolactone from benzo[a]phenazine with potent activity against Mycobacterium tuberculosis.
AID1433175Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & medicinal chemistry letters, Oct-01, Volume: 25, Issue:19
Design of novel dispirooxindolopyrrolidine and dispirooxindolopyrrolothiazole derivatives as potential antitubercular agents.
AID143856The compound was tested for its ability to inhibit the growth of Mycobacterium avium; Resistant2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Antimycobacterial activity of ionic fullerene derivatives.
AID757718Antibacterial activity against Escherichia coli expressing ToLC mutant assessed as growth inhibiiton after 18 hrs2013European journal of medicinal chemistry, Jul, Volume: 65Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: structure-based optimization of a virtual screening hit.
AID1467460Antibacterial activity against methicillin resistant Staphylococcus aureus MRSA090 at 75 ug/ml after 24 hrs by agar well diffusion method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID554582Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in intracellular bacterial cfu in peritoneum at 60 mg/kg, sc administered as single dose 2 hrs after infection measured upto 19 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID545915Antimicrobial activity against Escherichia coli ATCC 25922 by Etest method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID144031Antimycobacterial activity against Mycobacterium intracellular ATCC 1954 E-32003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.
AID1194330Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID1173022Induction of CYP3A4 in human HepG2 cells at 10 uM after 24 hrs by luciferase reporter gene assay in presence of hPXR relative to control2014Bioorganic & medicinal chemistry letters, Dec-01, Volume: 24, Issue:23
Cycloartane-type triterpenes from Euphorbia fischeriana stimulate human CYP3A4 promoter activity.
AID414459Antitubercular activity against non replicating persistent form of Mycobacterium tuberculosis H37Rv ATCC 27294 after 10 days by LORA2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
AID765104Bacteriostatic activity against rifampicin, isoniazid, streptomycin, ethambutol and pyrazinamide-resistant Mycobacterium tuberculosis MS-115 assessed as growth inhibition2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1537663Inhibition of human amyloid beta (1 to 42) self-induced aggregation assessed as Amyloid beta (1 to 42) aggregation at 100 uM incubated for 48 hrs by thioflavin T-based fluorescence assay (Rvb = 100%)2019MedChemComm, Jun-01, Volume: 10, Issue:6
Synthesis, molecular docking, and biological evaluation of novel 2-pyrazoline derivatives as multifunctional agents for the treatment of Alzheimer's disease.
AID256386Inhibition of growth of Mycobacterium avium (ATCC 25291) was determined using microplate alamar blue assay at 2 ug/mL concentration with compound dissolved in DMSO2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Design and studies of novel 5-substituted alkynylpyrimidine nucleosides as potent inhibitors of mycobacteria.
AID1427053Selectivity index, ratio of GI50 for human HeLa cells to MIC for dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 infected in human THP1 cells2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID1493171Induction of translation arrest in Bacillus subtilis isolate 1S34 assessed as increase in bmrC promoter activity at 30 ug after 14 to 18 hrs by beta-galactosidase reporter gene assay2017Journal of natural products, 11-22, Volume: 80, Issue:11
Cyclic Cystine-Bridged Peptides from the Marine Sponge Clathria basilana Induce Apoptosis in Tumor Cells and Depolarize the Bacterial Cytoplasmic Membrane.
AID376027Antimycobacterial activity against Mycobacterium intracellular ATCC 23068 after 48 hrs1999Journal of natural products, Sep, Volume: 62, Issue:9
New antimycobacterial saponin from Colubrina retusa.
AID1716653Antibacterial activity against Escherichia coli CAN-ICU 63074 (AMK 32) assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID626919Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 using compound level ranging from 1 to 100 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID583689Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315deltaIP harboring hypothetical protein SA1826 14A mutant after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID581657Antibacterial activity against normal phenotype Staphylococcus aureus at pH 7.4 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1716868Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID531114Antimicrobial activity against Staphylococcus aureus CB1887 harboring rpoB R484H, L520 deficient gyrA, gyrA S48L, R236 duplicated parC and parC H103Y mutant genes selected after ABT-719 exposure for 20 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1262038Selectivity index, ratio of CC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2015European journal of medicinal chemistry, Nov-13, Volume: 105Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents.
AID523657Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta101 with RNA polymerase beta subunit N474S mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID445288Antibacterial activity against Mycobacterium smegmatis by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1557238Antitubercular activity against resistant Mycobacterium tuberculosis 7 harboring rpoB His526Tyr mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID424332Antimicrobial activity against Dialister invisus assessed as susceptibility breakpoint by CA-SFM method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID558246Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 0.5 mg/liter after 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1827060Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1311240Antibacterial activity against Enterococcus faecalis 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1782925Cytotoxicity against mouse RAW264.7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID373796fCmax in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 2100 mg, po administered twice a week2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1055961Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate X005319 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1223075Induction of Ugt1a1 gene expression in PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID1137526Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition by standard microdilution method2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B.
AID1209455Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
In vitro inhibition of the bile salt export pump correlates with risk of cholestatic drug-induced liver injury in humans.
AID571432Antibacterial activity against Escherichia coli ATCC 25992 by Etest method in presence of 1 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1444302Antimycobacterial activity against Mycobacterium kansasii isolate 6509/96 after 14 days by micromethod2017European journal of medicinal chemistry, Apr-21, Volume: 130Structure-activity relationship studies on 3,5-dinitrophenyl tetrazoles as antitubercular agents.
AID553476Half life in simulated human serum in in vitro hollow-fiber PK model at 600 mg administered every 24 hrs2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Pharmacodynamics of minocycline against Staphylococcus aureus in an in vitro pharmacokinetic model.
AID555301Antibacterial activity against methicillin-susceptible Staphylococcus aureus 505 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1061104Antimicrobial activity against Mycobacterium tuberculosis H37Rv by low oxygen recovery assay2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID557108Binding affinity to human serum albumin assessed as fraction of binding sites occupied by compound at >325 ug/ml by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID510521Tmax in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID279192Antibacterial activity against methicillin-resistant Staphylococcus aureus isolates from skin or soft tissue infection outpatients2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Treatment and outcomes of infections by methicillin-resistant Staphylococcus aureus at an ambulatory clinic.
AID1348986Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis after 3 days by rapid direct susceptibility test
AID1879564Antibacterial activity against Mobiluncus mulieris ATCC 352432022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID727793Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID581062Induction of iNOS expression in human A549 cells at 25 to 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID765122Cytotoxicity against human Jurkat cells after 72 hrs by MTT assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1311228Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID406604Ratio of peak drug level in albino guinea pig cage fluid at 12.5 mg/kg, ip to MIC for Staphylococcus aureus ATCC 29213 during stationary-growth phase2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID1181168Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID571446Ratio of the MIC for Klebsiella pneumoniae ATCC 13883 in the absence of NAB7061 to MIC for Klebsiella pneumoniae ATCC 13883 in the presence of 4 ug/ml of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1467475Antibacterial activity against Staphylococcus aureus incubated for overnight by microdilution method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID581196Effect on PPARgamma expression in human A549 cells assessed as decrease in PPARgamma expression normalized to beta-actin expression level at 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1905564Antimicrobial activity against Enterococcus faecalis ATCC 29212 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID370105Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po after 8 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID530862Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB Q468K mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1417156Antibacterial activity against Acinetobacter baumannii BAA-1605 after 16 to 18 hrs by CLSI method2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis of 1,2,3-triazole linked 4(3H)-Quinazolinones as potent antibacterial agents against multidrug-resistant Staphylococcus aureus.
AID322753Inhibition of human CYP51 expressed in Topp 3 cells by lanosterol demethylase assay2007Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 35, Issue:3
Three-dimensional quantitative structure-activity relationship analysis of human CYP51 inhibitors.
AID27900Plasma clearance of the compound2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Property-based design: optimization of drug absorption and pharmacokinetics.
AID543793Antimicrobial activity against Haemophilus influenzae VT450-2006 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1055965Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate X003899 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID456895Antimycobacterial activity against Mycobacterium smegmatis MC2 155 ATCC 19420 after 7 days by resazurin assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents.
AID530785Antimicrobial activity against Clostridium difficile isolate 16 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID530997Antimicrobial activity against Clostridium difficile isolate 44 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID581652Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID358597Antitubercular activity against Mycobacterium tuberculosis2001Journal of natural products, Nov, Volume: 64, Issue:11
Isolation and biological evaluation of filiformin, plakortide F, and plakortone G from the Caribbean sponge Plakortis sp.
AID1904930Induction of drug resistance in methicillin-resistant Staphylococcus aureus USA400 NRS 123 assessed as fold increase in MIC measured after 7 passages by broth microdilution assay2022European journal of medicinal chemistry, Apr-15, Volume: 234Exploring the structure-activity relationships of diphenylurea as an antibacterial scaffold active against methicillin- and vancomycin-resistant Staphylococcus aureus.
AID1181166Antimicrobial activity against clinical isolate Rifampin-resistant Mycobacterium tuberculosis assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID634040Antituberculosis activity against multidrug-resistant Mycobacterium tuberculosis isolate Spec. 192 by twofold serial dilution method2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis of novel 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds and their evaluation for tuberculostatic activity.
AID144023In vitro antibacterial activity against Mycobacterium gordonae 64271999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID531288Antimicrobial activity against Clostridium difficile isolate 60 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID581056Effect on STAT-1 phosphorylation in human A549 cells assessed as increase in IL1-beta, TNF-alpha and IFN-gamma-induced phosphorylation at 50 ug/ml after 15 to 30 mins by Western immunoblotting analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1164302Inhibition of RNA synthesis in Mycobacterium bovis BCG assessed as inhibition of [3H]uracil incorporation by liquid scintillation counting2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID373967Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as concentration needed to achieve 50% maximal killing rat2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1323725Growth inhibition of Mycobacterium avium ATCC 25291 at 2 ug/ml after 6 days by microplate alamar blue assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents.
AID1372629Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week in presence of efflux pump inhibitor piperine by MABA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1762630Antibacterial activity against Klebsiella pneumoniae ATCC 700603 by CLSI based microplate assay
AID341765Antimycobacterial activity against Mycobacterium tuberculosis infected patient assessed as sputum bacterial count at 20 mg/kg, po administered daily for 2 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID555311Antibacterial activity against methicillin-resistant coagulase-negative Staphylococcus epidermidis 345 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID581059Effect on ERK1/2 phosphorylation in human A549 cells assessed as increase in IL1-beta, TNF-alpha and IFN-gamma-induced phosphorylation at 50 ug/ml after 15 to 30 mins by Western immunoblotting analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1542212Antimicrobial activity against Escherichia coli ATCC 25922 incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID586049Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type U6 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1493158Induction of cell envelope stress in Bacillus subtilis isolate 1S34 assessed as increase in liaI promoter activity at 30 ug after 14 to 18 hrs by beta-galactosidase reporter gene assay2017Journal of natural products, 11-22, Volume: 80, Issue:11
Cyclic Cystine-Bridged Peptides from the Marine Sponge Clathria basilana Induce Apoptosis in Tumor Cells and Depolarize the Bacterial Cytoplasmic Membrane.
AID1730995Antitubercular activity against extensively drug resistance Mycobacterium tuberculosis R506 XDR by MABA2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID405157AUC (0 to 24 hrs) in tuberculosis patient at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1174110Antimycobacterial activity against isoniazid, rifampin, streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID424323Antimicrobial activity against Dialister pneumosintes assessed as susceptibility breakpoint by CA-SFM method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID537115Protection index, ratio of CC50 for Mycobacterium tuberculosis infected mouse J774A1 cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1580091Antibacterial activity against colistin-resistant Acinetobacter baumannii ATCC 17978 mutant generated from seven serial passages by checkerboard assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Homodimeric Tobramycin Adjuvant Repurposes Novobiocin as an Effective Antibacterial Agent against Gram-Negative Bacteria.
AID210952In vitro inhibition of translocase I; Not determined.2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.
AID1297719Antibacterial activity against Staphylococcus aureus ATCC 4163 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1400045Bactericidal activity against Staphylococcus aureus BAA 44 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1326385Antibacterial activity against Bacillus subtilis P10A derived after 10 passage in presence of JBIR-100 after 16 to 18 hrs by microbroth dilution assay2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
AID292412Antitubercular activity against Mycobacterium tuberculosis SS22007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID1687561Antitubercular activity against Mycobacterium tuberculosis Spec.192 assessed as inhibition of microbial growth by classical test tube method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID699542Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID583688Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315deltaIP harboring rpoB A621E mutant gene after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1210911Intrinsic clearance in rat lung microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID406619Antibacterial activity against Staphylococcus aureus ATCC 29213 infected albino guinea pig tissue-cage infection model assessed as infection cure rate at 12.5 mg/kg, ip administered every 12 hrs for 4 days2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID581195Reduction in PPARgamma expression in human A549 cells assessed as increase in 100 ng/ml IL1-beta, TNF-alpha and IFN-gamma-induced PPARgamma down regulation normalized to beta-actin expression level at 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1296383Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 234/2005 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1163978Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution assay2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1908126Antibacterial activity against Escherichia coli ATCC 25922 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID562785Antimicrobial activity against Chlamydia muridarum MoPn/oflR harboring ompA gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1063302Antitubercular activity against rifampin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay2014European journal of medicinal chemistry, Jan-24, Volume: 72Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.
AID1219161Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]E217betaG substrate uptake at 100 uM by liquid scintillation counting2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods.
AID565806Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB28 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID103687In vitro activity of compound against slowly growing Mycobacterium marinum 13931990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID558235Half life in human at 600 mg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1335982Antibacterial activity against rifampin-resistant Mycobacterium tuberculosis after 8 to 9 days by BacT/Alert MP bottle assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains.
AID283157Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2414 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID404135Antibacterial activity against vancomycin-resistant Enterococcus faecium CL57912005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID1602931Cytotoxicity against human MRC5 cells after 24 hrs by resazurin dye-based fluorescence assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1624156Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 8 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID373980Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 2517 infected in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as microbial killing administered at simulated dose of 2100 mg, po twi2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1055968Cytotoxicity against african green monkey Vero cells2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1367810Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by two-fold serial dilution method2017Bioorganic & medicinal chemistry letters, 12-01, Volume: 27, Issue:23
Design, synthesis and in vitro anti-tuberculosis activity of benzo[6,7]cyclohepta[1,2-b]pyridine-1,2,3-triazole derivatives.
AID1624151Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 3 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID1915644Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 16833 assessed as reduction in bacterial growth by MABA analysis2021European journal of medicinal chemistry, Jan-15, Volume: 210An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
AID530792Antimicrobial activity against Clostridium difficile isolate 23 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID419344Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 6 weeks2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, antitubercular activity and docking study of novel cyclic azole substituted diphenyl ether derivatives.
AID634282Antimycobacterial activity against Mycobacterium tuberculosis isolate 352 expressing rpoB Asp516Leu and Phe514Phe double mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1443986Inhibition of recombinant human BSEP expressed in baculovirus infected sf9 cell membrane vesicles assessed as reduction in ATP or AMP-dependent [3H]-taurocholic acid uptake in to vesicles preincubated for 5 mins followed by ATP/AMP addition measured after2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1653417Inhibition of PGL1 synthesis in Mycobacterium leprae infected Swiss Webster mouse macrophages assessed as decrease in [U-14C]PA incorporation at 2 uM preincubated for 4 days post infection followed by [U-14C]PA addition and measured after 7 days by liquid2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID355990Antimalarial activity against chloroquine-resistant Plasmodium falciparum W22003Journal of natural products, Jun, Volume: 66, Issue:6
New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge.
AID531012Antimicrobial activity against Clostridium difficile isolate 59 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID529304Antimicrobial activity against Acinetobacter baumannii isolate Ac058 expressing beta-lactamase Oxa-58 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Characterization of the carbapenem-hydrolyzing oxacillinase oxa-58 in an Acinetobacter genospecies 3 clinical isolate.
AID683324Antibacterial activity against Escherichia coli ATCC 25922 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID326286Antibacterial activity against methicillin-resistant Staphylococcus aureus 4875 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID392599Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1888847Antibacterial activity against Staphylococcus aureus 1199 measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID1290503Antitubercular activity against Mycobacterium tuberculosis in acute tuberculosis infection BALB/c mouse model assessed as reduction in parasite burden at 15 mg/kg, po administered 5 days per week for 3 weeks started on day 11 post infection2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis.
AID1061814Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 45 days2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
Synthesis and antimycobacterial activity of novel camphane-based agents.
AID1879532Antibacterial activity against rifampicin-resistant Clostridioides difficile CB1934 harboring rpoBQ489K mutant at 1:1 compound to metronidazole molar ratio measured after 3 days in presence of metronidazole2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID530783Antimicrobial activity against Clostridium difficile isolate 14 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID283172Effect on biofilm formation of Staphylococcus lugdunensis assessed as percent non-biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID373030Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PU78 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID604020Unbound drug concentration in Sprague-Dawley rat plasma administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr by LC-MS/MS method2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID207004Effective dose against Staphylococcus aureus in mice for peroral administration.1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
4-Deoxypyrido[1',2':1,2]imidazo[5,4-c]rifamycin SV derivatives. A new series of semisynthetic rifamycins with high antibacterial activity and low gastroenteric absorption.
AID561167Half life in in vitro pharmacokinetic/pharmacodynamic model at 30 mg for every 8 hrs2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID289151Antimycobacterial activity against streptomycin, isoniazid, rifampicin, pyrazinamide-resistant Mycobacterium tuberculosis CIBIN 234 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID1272454Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes.
AID1436933Selectivity index, ratio of GI90 for human MCF7 cells to MIC90 for dormant state of Mycobacterium tuberculosis H37Ra2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID376995Antimicrobial activity against isoniazid-resistant Mycobacterium tuberculosis isolate by alamar blue assay2006Journal of natural products, May, Volume: 69, Issue:5
Aegicerin, the first oleanane triterpene with wide-ranging antimycobacterial activity, isolated from Clavija procera.
AID1252464Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 50 uM incubated for 48 hrs at 37 degC by MTT assay relative to control2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID292296Antibacterial activity Streptococcus pyogenes ATCC 19615 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID1179475Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in 7H12 medium after 7 days by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID370250Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 1.25 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1871136Antitubercular activity against Multidrug-resistant Mycobacterium tuberculosis clinical isolate PT12 assessed as bacterial growth inhibition incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Aug-11, Volume: 13, Issue:8
Antitubercular Activity of Novel 2-(Quinoline-4-yloxy)acetamides with Improved Drug-Like Properties.
AID577206Antimicrobial activity against Escherichia coli O157:H7 PT-32 in stationary phase encoding Stx-1 and Stx-2 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID1417154Antibacterial activity against Escherichia coli ATCC 25922 after 16 to 18 hrs by CLSI method2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis of 1,2,3-triazole linked 4(3H)-Quinazolinones as potent antibacterial agents against multidrug-resistant Staphylococcus aureus.
AID283167Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5254 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1556502Induction of constitutive androstane receptor in human primary hepatocytes assessed as upregulation of CYP3A4 mRNA expression at 10 uM after 24 hrs by RT-PCR analysis2019European journal of medicinal chemistry, Oct-01, Volume: 179Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies.
AID1916599Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition measured after 7 days by MABA method2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID511123Antiinflammatory activity in Acinetobacter baumannii 1327-infected New Zealand rabbit meningitis model assessed as effect on lactate level in CSF at 12 mg/kg, im measured at 12 hrs post dose2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1868115Anti-tubercular activity against Mycobacterium tuberculosis CF16 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID145299The compound was tested for its minimum inhibitory activity against Mycobacterium tuberculosis H37Rv in BACTEC 12B medium using the Microplate Alamar Blue Assay2000Bioorganic & medicinal chemistry letters, Jun-05, Volume: 10, Issue:11
9-Benzylpurines with inhibitory activity against Mycobacterium tuberculosis.
AID1552790Antimycobacterial activity against Mycobacterium bovis ATCC 35737 assessed as reduction in bacterial cell growth incubated for 8 days by alamar blue staining based assay2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents.
AID1436936Selectivity index, ratio of GI90 for human MCF7 cells to MIC90 for dormant state of dormant state of Mycobacterium bovis BCG2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID745300Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 250 ug/mL after 12 to 28 days by Lowenstein-Jensen method relative to control2013European journal of medicinal chemistry, May, Volume: 63Synthesis and identification of β-aryloxyquinoline based diversely fluorine substituted N-aryl quinolone derivatives as a new class of antimicrobial, antituberculosis and antioxidant agents.
AID1602937Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 5 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID1167367Antibacterial activity against Escherichia coli D21 tolC deletion mutant assessed as mutant prevention concentration after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID293585Antibacterial activity against Bacillus subtilis isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID352097Antimicrobial activity against multidrug-resistant Staphylococcus aureus after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID495515Antibacterial activity against Acinetobacter baumannii CIP70-10 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID753130Antitubercular activity against Mycobacterium tuberculosis XDR-1 assessed as growth inhibition after 2 to 3 weeks by broth microdilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID1765356Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis H37Rv ATCC 35837 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID1241591Induction of CYP3A4 activation in human hepatocytes at 2 uM incubated for 48 hrs using testosterone substrate2015Journal of medicinal chemistry, Sep-10, Volume: 58, Issue:17
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
AID1488559Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by two fold dilution method
AID1449139Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC=<90 for Mycobacterium tuberculosis2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections.
AID144870Antimycobacterial activity against Mycobacterium tuberculosis H37Rv using Microplate Alamar Blue Assay (MABA) assay2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID530790Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 21 expressing RpoB H502N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID581191Effect on NF-kappaB activation in 100 ng/ml IL-1beta, TNF-alpha and IFN-gamma-stimulated human A549 cells assessed as degradation of inhibitory subunit IkappaB measured upto 3 hrs at 50 ug/ml by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID1743439Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1426440Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis CF81 clinical isolate incubated for 7 days measured 24 hrs post incubation by resazurin microtiter assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
AID1335980Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 8 to 9 days by BacT/Alert MP bottle assay2017Bioorganic & medicinal chemistry, 01-01, Volume: 25, Issue:1
Preliminary SAR and biological evaluation of antitubercular triazolothiadiazine derivatives against drug-susceptible and drug-resistant Mtb strains.
AID530863Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpo BH481D mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1638915Antimicrobial activity against penicillin-resistant Staphylococcus aureus ATCC 29213 assessed as ratio of MIC after and before 15 serial passages preincubated followed by replating and measured after 24 hrs2019Bioorganic & medicinal chemistry, 04-01, Volume: 27, Issue:7
Antibacterial activity of indolyl-quinolinium derivatives and study their mode of action.
AID1705555Inhibition of RNA polymerase in Staphylococcus aureus ATCC 29213 assessed as total DNA level at 1/4 to 1/8 times MIC by fluorimetric method2020European journal of medicinal chemistry, Dec-15, Volume: 208Benzyl and benzoyl benzoic acid inhibitors of bacterial RNA polymerase-sigma factor interaction.
AID1888135Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD1 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1917331Cytotoxicity against African green monkey Vero cells after 48 hrs by MTT assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.
AID1196883Inhibition of Mycobacterium tuberculosis AlaDH using L-alanine as substrate after 20 mins by spectrophotometry2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID1296388Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 131 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID531010Antimicrobial activity against Clostridium difficile isolate 57 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1879561Antibacterial activity against Gardnerella vaginalis ATCC 140182022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID718942Cytotoxicity against HEK293T cells assessed as cellular growth at 100 uM by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
AID699539Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake at 20 uM by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID1455930Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2017Journal of natural products, 02-24, Volume: 80, Issue:2
Flavonoids from Erythrina schliebenii.
AID510997Ratio of Cmax to MIC for Acinetobacter baumannii 1327 in pharmacokinetic-pharmacodynamic New Zealand rabbit meningitis model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1326100Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 9160 after 7 days by microplate alamar blue assay
AID1224517Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 234/2005 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID681166TP_TRANSPORTER: Western blot, LS180 cell1996Molecular pharmacology, Feb, Volume: 49, Issue:2
Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells.
AID1359449Antitubercular activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 after 12 days by XRMA2018European journal of medicinal chemistry, May-25, Volume: 152Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life.
AID3039Minimum inhibitory concentration of compound against 20 Mycobacterium avium complex (MAC) clinical isolates1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID510515AUC (0 to 24 hrs) in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1556639Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16995 clinical isolate assessed as reduction in bacterial cell viability incubated for 7 days by microplate alamar blue assay2019European journal of medicinal chemistry, Oct-01, Volume: 179hERG optimizations of IMB1603, discovery of alternative benzothiazinones as new antitubercular agents.
AID574581Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 obtained from sputum of patient at 1 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID453816Antitubercular activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar blue assay2009Bioorganic & medicinal chemistry, Oct-15, Volume: 17, Issue:20
Natural product leads for drug discovery: isolation, synthesis and biological evaluation of 6-cyano-5-methoxyindolo[2,3-a]carbazole based ligands as antibacterial agents.
AID1887539Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 16 to 18 hrs by broth microdilution method2022Journal of natural products, 10-28, Volume: 85, Issue:10
Developing the Natural Prenylflavone Artocarpin from
AID530994Antimicrobial activity against Clostridium difficile isolate 41 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1516019Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1264465Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID529533Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-ATA mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID558757Antibacterial activity against homo-Methicillin-resistant and tetracycline-resistant Staphylococcus aureus deltaIP::vraSH14 harboring vraSH14 S329L mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID1210912Intrinsic clearance in mouse Liver microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID449435Antimycobacterial activity against Mycobacterium tuberculosis XDR infected in MDBK by BACTEC analysis2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
Pentacyclo-undecane derived cyclic tetra-amines: synthesis and evaluation as potent anti-tuberculosis agents.
AID1908120Antibacterial activity against Staphylococcus epidermidis ATCC 12228 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID1652708Induction of Escherichia coli K12 MG1655 recN promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID1888848Antibacterial activity against Staphylococcus aureus K1758 measured after 24 hrs by Muller Hinton broth based MTT assay2022Bioorganic & medicinal chemistry, 01-15, Volume: 54Potentiating the intracellular killing of Staphylococcus aureus by dihydroquinazoline analogues as NorA efflux pump inhibitor.
AID644318Antitubercular activity against Mycobacterium smegmatis ATCC 19420 after 7 days by resazurin assay2012European journal of medicinal chemistry, Mar, Volume: 49Design, synthesis of some new (2-aminothiazol-4-yl)methylester derivatives as possible antimicrobial and antitubercular agents.
AID1685941Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth incubated for 5 days by alamar blue assay2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Inhibitors of the Cysteine Synthase CysM with Antibacterial Potency against Dormant Mycobacterium tuberculosis.
AID1493793Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 at sub MIC after 4 passages by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID285569Bactericidal activity against 12-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 11 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID571423Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method by Etest in presence of 8 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID774190Cytotoxicity against African green monkey Vero cells after 72 hrs by MTS-PMS assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Phomapyrrolidones A-C, antitubercular alkaloids from the endophytic fungus Phoma sp. NRRL 46751.
AID1315571Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay2016European journal of medicinal chemistry, Oct-04, Volume: 121Synthesis, characterization and antitubercular activities of novel pyrrolyl hydrazones and their Cu-complexes.
AID525127Suppression of drug resistance development in recA-deficient Staphylococcus aureus KB103 assessed as prolonged length of subculture to develop Linezolid resistance at 4 times MIC and 0.25 times IC50 after 20 days2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Delayed development of linezolid resistance in Staphylococcus aureus following exposure to low levels of antimicrobial agents.
AID285555Bactericidal activity against 19-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 1 day by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID392605Antimycobacterial activity against Mycobacterium kansasii MTCC 3058 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID545809Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 assessed as inhibition of biofilm formation after 24 hrs by serial dilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID103669In vitro activity of compound against slowly growing Mycobacterium gordonae 14411990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID565800Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB2 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID623585Antituberculosis activity against 5 x 10'4 inoculum per tube Mycobacterium tuberculosis H37Rv after 24 hrs by Lowenstein-Jensen method2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study.
AID1879068Antibacterial activity against NDM-1 positive Escherichia coli ZC-YN3 isolates assessed as inhibition of bacterial growth incubated for 18 to 24 hrs by CLSI based broth microdilution method2022European journal of medicinal chemistry, Mar-05, Volume: 231Metallo-β-lactamases inhibitor fisetin attenuates meropenem resistance in NDM-1-producing Escherichia coli.
AID680558TP_TRANSPORTER: uptake in OATP-C-expressing HeLa cells2003The Journal of pharmacology and experimental therapeutics, Jan, Volume: 304, Issue:1
Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation.
AID1491290Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days under normoxic condition by microplate Alamar blue assay2017European journal of medicinal chemistry, Sep-08, Volume: 137QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity.
AID1852760Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 assessed as bacterial growth inhibition by broth microdilution assay2022RSC medicinal chemistry, Sep-21, Volume: 13, Issue:9
Design and evaluation of poly-nitrogenous adjuvants capable of potentiating antibiotics in Gram-negative bacteria.
AID372546Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 36-48 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID680462TP_TRANSPORTER: inhibition of Gadoxetate uptake (Gadoxetate: 100 uM, Rifampicin: 100 uM) in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, Jul, Volume: 290, Issue:1
Hepatic uptake of the magnetic resonance imaging contrast agent gadoxetate by the organic anion transporting polypeptide Oatp1.
AID1435653Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 7357/1998 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1566231Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis H37Rv harbouring DprE1 C387S mutant assessed as reduction in bacterial cell growth2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Scaffold Morphing To Identify Novel DprE1 Inhibitors with Antimycobacterial Activity.
AID1664573Antitubercular activity against Mycobacterium tuberculosis H37Ra assessed as bacterial growth inhibition by MABA2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives.
AID325117Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 2 ug/ml after 2 weeks by BACTED460 method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Isoniazid induces its own resistance in nonreplicating Mycobacterium tuberculosis.
AID571663Ratio of the MIC for Proteus mirabilis ATCC 29906 in the absence of NAB7073 to MIC for Proteus mirabilis ATCC 29906 in the presence of 4 ug/ml of NAB70732008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID557097Protein binding in serum2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID577210Antimicrobial activity against Escherichia coli C600::933W in stationary phase encoding Stx-2 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID1557239Antitubercular activity against resistant Mycobacterium tuberculosis 5 harboring rpoB His526Tyr mutant by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID305228Ratio of MIC for Arr-1 positive Mycobacterium smegmatis DSM 43756 to MIC for Arr-1 negative Mycobacterium smegmatis DSM 43756Kml2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID510526Apparent oral clearance in tuberculosis patient at 10 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1765355Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 assessed as inhibition of bacterial growth incubated for 48 hrs by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID463978Antitubercular activity against Mycobacterium tuberculosis H37Rv at MIC after 24 hrs by broth microdilution method2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
New 1,3-oxazolo[4,5-c]quinoline derivatives: synthesis and evaluation of antibacterial and antituberculosis properties.
AID543792Antimicrobial activity against Acinetobacter baumannii VT 126 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1223008Induction of Cyp2b10 gene expression in male PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID523774Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Abeta207 with RNA polymerase beta subunit S470N/A471S mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID1400047Bactericidal activity against Enterococcus faecalis ATCC 349 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID392819Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 21 days by agar proportion method2009Bioorganic & medicinal chemistry, Feb-15, Volume: 17, Issue:4
Synthesis and biological evaluation of some new 1,4-dihydropyridines containing different ester substitute and diethyl carbamoyl group as anti-tubercular agents.
AID144871Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to cycloserine (CS)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1514474Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as colony forming units at 0.002 to 64 ug/ml measured day 21 post dose by time kill assay (Rvb = 0 log10CFU/ml)2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID103685In vitro activity of compound against slowly growing Mycobacterium marinum 1392 h1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID665370Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate at 40 ug/mL by radiometric growth assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives.
AID541035Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 12.5 mg/kg after measured on day 10 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID555307Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 057 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1298606Antibacterial activity against Streptococcus pneumoniae after 24 hrs by agar diffusion assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.
AID278675Antibacterial activity against Enterococcus faecalis isolate 57432007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1765587Antibacterial activity against gentamicin-resistant Pseudomonas aeruginosa ATCC 27853 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID565799Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB1 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1311368Antibacterial activity against Mycobacterium tuberculosis 124R measured after 14 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID1825031Selectivity index ratio of MIC90 in Mycobacterium smegmatis mc2155 ATCC 700084 cultured in GAST-Fe media to Mycobacterium smegmatis mc2155 cultured in GAST media2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
AID1634251Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 100 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID279812Antimicrobial activity against carbapenem-resistant Klebsiella pneumoniae ZR01 from patient sputum by agar dilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Plasmid-mediated KPC-2 in a Klebsiella pneumoniae isolate from China.
AID1244806Antibacterial activity against Staphylococcus aureus ATCC 6538 after 18 hrs by serial microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID1705577Antimycobacterial activity against INH-resistant Mycobacterium tuberculosis mc2497 after 10 to 14 days2020European journal of medicinal chemistry, Dec-15, Volume: 208Synthesis and evaluation of thiophene based small molecules as potent inhibitors of Mycobacterium tuberculosis.
AID1210064Induction of CYP2B6 mRNA expression in human donor hepatocytes after 48 hrs by real-time PCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.
AID1447546Antibacterial activity against multidrug-resistant Acinetobacter baumannii AB030 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID261195Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Synthesis and antimycobacterial activity of some alkyl [5-(nitroaryl)-1,3,4-thiadiazol-2-ylthio]propionates.
AID1287460Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay relative to T09013172016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1716638Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1337867Selectivity index, ratio of GI50 for PMP-differentiated human THP1 cells to MIC for Mycobacterium bovis BCG ATCC 35743 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID541045Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 infected in Albino guiena pig assessed as decrease in planktonic bacterial counts in cage fluid at 12.5 mg/kg measured on day 4 postinfection2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID572534Absorption rate constant in pulmonary tuberculosis patient in first order and lag time model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID774604Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene assessed as growth inhibition at 0.1 uM after 6 days by luminometry relative to control2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID1400028Inhibition of protein translation/transcription in Escherichia coli S30 cell extract at 0.1 ug/ml using circular DNA with pBESTluc after 60 mins by luciferase reporter gene assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID645692Antimicrobial activity against Mycobacterium bovis BCG by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID340860Antimicrobial activity against vancomycin-intermediate resistant Staphylococcus aureus Mu50 vraG mutant microdilution assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Interaction of the GraRS two-component system with the VraFG ABC transporter to support vancomycin-intermediate resistance in Staphylococcus aureus.
AID529532Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG-ATC mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID580845Cmax in healthy human at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1400037Bactericidal activity against Staphylococcus aureus incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID694229Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 1 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID1634995Antimicrobial activity against Pseudomonas aeruginosa clinical isolates assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID1765650Antibacterial activity against rifampin-resistant Pseudomonas aeruginosa ATCC 27853 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID529526Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate A2558 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1262575Antimicrobial activity against clinical isolates of Mycobacterium tuberculosis SAWC 3385 Cas1/Delhi under 7H9 medium assessed as growth inhibition after 14 days by alamar blue assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID424331Antimicrobial activity against Dialister propionicifaciens assessed as susceptibility breakpoint by CA-SFM method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID434065Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced [3H]arachidonic acid release at 50 ug/ml measured after 19 hrs of IL1-beta challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID531264Antimicrobial activity against Clostridium difficile isolate 36 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID571209Antibacterial activity against Pseudomonas aeruginosa ATCC 27853by Etest method in presence of 0.125 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID700539Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 1 to 100 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID523295Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as assessed as lowest concentration to reduce bacterial burden in lungs to level of reduction achieved with higher doses orally treated in water-20% encapsin2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID216023Cytotoxicity determined in VERO cells at concentrations less than or equal to 62.5 mg/mL or 10 times the MIC against Mycobacterium tuberculosis H37Rv.2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID977599Inhibition of sodium fluorescein uptake in OATP1B1-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1332968Selectivity index, ratio of IC50 for mouse J774A.1 cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 272942016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID268908Antibacterial activity against Mycobacterium tuberculosis 1034712006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID559089Antimicrobial activity against carbapenem-susceptible Acinetobacter baumannii isolate A1 by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
In vivo selection of reduced susceptibility to carbapenems in Acinetobacter baumannii related to ISAba1-mediated overexpression of the natural bla(OXA-66) oxacillinase gene.
AID603130Antimycobacterial activity against Mycobacterium tuberculosis isolate 02TBDM039EP097 after 24 hrs by tetrazolium microplate assay2011Bioorganic & medicinal chemistry, Apr-01, Volume: 19, Issue:7
Dihydro-β-agarofuran sesquiterpenes isolated from Celastrus vulcanicola as potential anti-Mycobacterium tuberculosis multidrug-resistant agents.
AID1634262Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 25 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1181164Antimicrobial activity against clinical isolate Mycobacterium tuberculosis JAL assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID768664Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition by BACTEC 460 radiometric assay2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Synthesis of novel isothiazolopyridines and their in vitro evaluation against Mycobacterium and Propionibacterium acnes.
AID530348Antimicrobial activity against azide-resistant Escherichia coli J53 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID1856861Antibacterial activity against Bacillus subtilis ATCC 23857 assessed as growth inhibition measured after 18 to 24 hrs by CLSI based broth microdilution method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1658967Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID583693Antimicrobial activity against methicillin-resistant Staphylococcus aureus 10*3d1 harboring hypothetical protein SA1826 14A mutant and rpoB 621A mutant after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID398494Inhibition of protein synthesis in Bacillus subtilis assessed as incorporation of [3H]amino acid at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2003Journal of natural products, Feb, Volume: 66, Issue:2
Antibacterial diterpenes from Calceolaria pinifolia.
AID69354Minimum inhibitory concentration of compound tested for antibacterial activity against Escherichia coli ML/351981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antibacterial activity of some ester, amides, and hydrazides of 3-carboxyrifamycin S. Relationship between structure and activity of ansamycins.
AID558759Antibacterial activity against hetero-vancomycin-intermediate Staphylococcus aureus Mu3 by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID558019Cmax in human at 600 mg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1437020Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis clinical isolate after 4 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Synthesis, antimycobacterial and cytotoxic activity of α,β-unsaturated amides and 2,4-disubstituted oxazoline derivatives.
AID1892311Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated for 16 to 24 hrs in presence of ampicillin by broth microdilution based spectrophotometric analysis2022Journal of natural products, 06-24, Volume: 85, Issue:6
Glenthmycins A-M: Macrocyclic Spirotetronate Polyketide Antibacterials from the Australian Pasture Plant-Derived
AID1393798Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by two fold dilution assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID1658970Antibacterial activity against Staphylococcus aureus ATCC 25923 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID251157Effective concentration required compared to that of Minimum inhibition concentration required against Mycobacterium tuberculosis H37Rv strain was determined; Range is 0.16-1.672004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
In vitro advanced antimycobacterial screening of cobalt(II) and copper(II) complexes of fluorinated isonicotinoylhydrazones.
AID543808Bactericidal activity against Klebsiella pneumoniae VT 1367 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID345805Antagonist activity at guinea pig ileum histamine H1 receptor at 0.3 x 10'4 M2008Bioorganic & medicinal chemistry, Dec-15, Volume: 16, Issue:24
Antimycobacterial and H1-antihistaminic activity of 2-substituted piperidine derivatives.
AID530624Inhibition of Staphylococcus aureus wild-type RNA polymerase RpoB2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1383957Ratio of MBC to MIC for Mycobacterium tuberculosis H37Rv2018European journal of medicinal chemistry, Apr-25, Volume: 150Synthesis and antimycobacterial activity of 1-(β-d-Ribofuranosyl)-4-coumarinyloxymethyl- / -coumarinyl-1,2,3-triazole.
AID1634990Antimicrobial activity against Staphylococcus epidermidis assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID1879521Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1771 harboring rpoBL525I/D530N/rdxAE75stop mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution meth2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID541086Antibacterial activity against 1 x10'6 to 5 x10'6 CFU/ml methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as log decrease in bacterial count at 4 times MIC after 6 hrs by time kill study2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID581654Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient at pH 7.4 after 48 hrs by broth microdilution method in absence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1782923Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as inhibition of bacterial growth incubated for 9 days by resazurin microtiter assay2021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID1294077Antitubercular activity against dormant Mycobacterium bovis BCG after 12 days by nitrate reductase assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis and docking studies of pyrazine-thiazolidinone hybrid scaffold targeting dormant tuberculosis.
AID1634246Antimycobacterial activity against Mycobacterium abscessus subsp. abscessus assessed as reduction in microbial growth by CLSI method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID523659Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta103 with RNA polymerase beta subunit T638K mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID499901Antitubercular activity against Mycobacterium tuberculosis H37Ra at 1 ug/ml after 6 days by microplate alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Inhibition of mycobacterial replication by pyrimidines possessing various C-5 functionalities and related 2'-deoxynucleoside analogues using in vitro and in vivo models.
AID1304833Antibacterial activity against Staphylococcus epidermidis ATCC 12228 incubated for 16 to 18 hrs by broth microdilution method2016Journal of medicinal chemistry, 04-28, Volume: 59, Issue:8
Structure-Activity Relationships of a Diverse Class of Halogenated Phenazines That Targets Persistent, Antibiotic-Tolerant Bacterial Biofilms and Mycobacterium tuberculosis.
AID1393800Antitubercular activity against Mycobacterium tuberculosis H37Rv after 21 days by broth dilution assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID531132Antimicrobial activity against Staphylococcus aureus CB1953 harboring rpoB H481Y, gyrA S84L, gyrA V598I, parC S80F, parC R570H mutant genes selected after CBR-2092 exposure for 7 days2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1181158Antimicrobial activity against clinical isolate Mycobacterium tuberculosis Harlingen assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID392609Antimycobacterial activity against log-phase culture of Mycobacterium smegmatis ATCC 14468 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1401975Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis H37Rv ATCC 358282018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID400499Inhibition of AAH in Sprague-Dawley rat liver microsomes using benzo(a)pyrene as substrate by non-competitive assay relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID574593Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2403 obtained from sputum of patient at 1 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID604024Unbound brain to plasma concentration ratio in Sprague-Dawley rat administered in casettes of 2/3 drugs at 4 hr constant rate intravenous infusions using flow rate of 1 (ml/kg)/hr corresponding to dosage rate of 2 (umol/kg)/hr2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID683687Kinetic solubility of the compound at pH 7.42012European journal of medicinal chemistry, Nov, Volume: 57The design, synthesis, in silico ADME profiling, antiplasmodial and antimycobacterial evaluation of new arylamino quinoline derivatives.
AID1067041Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 days by microplate Alamar Blue assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of anti-tubercular activity of 6-(4-substitutedpiperazin-1-yl) phenanthridine analogues.
AID1191014Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial growth incubated for 7 days under GAS medium by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID748173Inhibition of rifamycin-resistant Mycobacterium tuberculosis RNA polymerase S450L mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID441082Ratio of ethambutol MIC to compound MIC for Mycobacterium tuberculosis H37Rv ATCC 272942009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID1063300Antitubercular activity against moxifloxacin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay2014European journal of medicinal chemistry, Jan-24, Volume: 72Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.
AID1504965Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days under aerobic condition by alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID565783Antimicrobial activity against Neisseria meningitidis harboring rpoB17 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1212147Induction of CYP3A4 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1493792Antibacterial activity against methicillin-resistant Staphylococcus aureus USA300 NRS384 by broth microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Biphenylthiazole antibiotics with an oxadiazole linker: An approach to improve physicochemical properties and oral bioavailability.
AID1634888Cytotoxicity against human HaCaT cells assessed as cell survival rate at 16 uM after 24 hrs by MTT assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID509514Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis H37Rv after 6 weeks2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs.
AID1070196Antimycobacterial activity against isoniazid and rifampicin-resistant Mycobacterium tuberculosis MTB411 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1256530Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1483720Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-c D28N mutant supplemented with 8 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1209483Activation of PXR in human Hu1043 hepatocytes assessed as increase in CYP3A-mediated testosterone 6beta-hydroxylation at 10 uM after 24 hrs by HPLC analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID285554Bactericidal activity against 5-day old actively replicating Mycobacterium tuberculosis H37Rv in aerobic condition at 1 ug/ml after 11 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID590141Antitubercular activity against Mycobacterium tuberculosis H37Rv by LORA assay2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents.
AID771922Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 28 days by agar dilution method2014Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents, , Volume: 23, Issue:4
Synthesis, antitubercular and anticancer activity of new Baylis-Hillman adduct-derived
AID1384036Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by serial dilution assay2018European journal of medicinal chemistry, Apr-25, Volume: 150Recent advances of imidazole-containing derivatives as anti-tubercular agents.
AID657784Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 44 from Chinese tuberculosis patient measured 24 hrs post dose by microplate alamar blue assay2012European journal of medicinal chemistry, Jun, Volume: 52Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
AID537119Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in mouse J774A1 cells assessed as reduction of bacterial growth at 0.25 ug/ml after 6 days relative to untreated control2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID30135Volume of distribution of the compound2001Journal of medicinal chemistry, Apr-26, Volume: 44, Issue:9
Property-based design: optimization of drug absorption and pharmacokinetics.
AID610802Antimycobacterial activity against Mycobacterium tuberculosis H37Rv transfected with pFPCA-luxAB grown under anaerobic condition for 10 days followed by 24 hrs incubation under aerobic condition by LORA assay2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Synthesis and antimycobacterial activities of non-purine analogs of 6-aryl-9-benzylpurines: Imidazopyridines, pyrrolopyridines, benzimidazoles, and indoles.
AID1297730Antibacterial activity against Pseudomonas aeruginosa NCTC 6749 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID405162Tmax in tuberculosis patient assessed as desacetylrifampin level at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1491402Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis after 3 to 7 days by rapid direct susceptibility test
AID571645Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 4 ug/ml NAB70702008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1210066Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.
AID1174023Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as complete growth inhibition after 5 days using liquid media2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Synthesis and evaluation of the 2,4-diaminoquinazoline series as anti-tubercular agents.
AID352096Antimicrobial activity against Staphylococcus aureus ATCC 25923 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID559766Antimycobacterial activity against PknGMsm-deficient Mycobacterium smegmatis harboring PknG Mtb gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID378572Antimicrobial activity against Mycobacterium tuberculosis2005Journal of natural products, Mar, Volume: 68, Issue:3
Ambigol C and 2,4-dichlorobenzoic acid, natural products produced by the terrestrial cyanobacterium Fischerella ambigua.
AID1193920Inhibition of Mycobacterium tuberculosis DNA GyrA/B heterotetramer assessed as inhibition of pBR322 supercoiling after 30 mins by gel electrophoresis2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID1635005Bactericidal activity against Pseudomonas aeruginosa assessed as induction of bacteria killing at 20 uM after 4 hrs by time kill assay2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID1856858Antibacterial activity against Klebsiella pneumoniae ATCC 700603 assessed as growth inhibition measured after 18 to 24 hrs by CLSI based broth microdilution method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID355988Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2003Journal of natural products, Jun, Volume: 66, Issue:6
New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge.
AID1716776Antibacterial activity against wild type Pseudomonas aeruginosa PAO1 assessed as reduction in bacterial growth by measuring doxycycline MIC at 8 ug/ml incubated for 18 hrs in presence of doxycycline by broth microdilution assay (Rvb = 16 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID427286Antitubercular activity against Mycobacterium tuberculosis H37Rv at 30 ug/disk by microdilution resazurin assay2009Bioorganic & medicinal chemistry, Jul-01, Volume: 17, Issue:13
Antimycobacterial activity of new 3,5-disubstituted 1,3,4-oxadiazol-2(3H)-one derivatives. Molecular modeling investigations.
AID445285Antibacterial activity against Mycobacterium bovis BCG str. Tokyo 172 by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1493170Induction of DNA damage in Bacillus subtilis isolate 1S34 assessed as increase in yorB promoter activity at 30 ug after 14 to 18 hrs by beta-galactosidase reporter gene assay2017Journal of natural products, 11-22, Volume: 80, Issue:11
Cyclic Cystine-Bridged Peptides from the Marine Sponge Clathria basilana Induce Apoptosis in Tumor Cells and Depolarize the Bacterial Cytoplasmic Membrane.
AID1291989Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as inhibition of mycobacterial replication after 6 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Investigation of 4-amino-5-alkynylpyrimidine-2(1H)-ones as anti-mycobacterial agents.
AID574545Antimicrobial activity against community-associated methicillin-resistant Staphylococcus aureus USA3002010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID1360819Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by Two-fold serial dilution assay2018European journal of medicinal chemistry, Jul-15, Volume: 155Benzo[d]thiazole-2-carbanilides as new anti-TB chemotypes: Design, synthesis, biological evaluation, and structure-activity relationship.
AID545919Antimicrobial activity against Escherichia coli IH3080 by Etest method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1193498Thermodynamic equilibrium solubility, log S of the compound simulated gastric fluid at pH 1.2 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID1634993Antimicrobial activity against Escherichia coli assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID1514450Antitubercular activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1891922Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in log10CFU at 1XMIC measured after 5 to 6 days by time kill assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID201070Activity in the murine model (OS route) of Staphylococcus aureus tour septicemia1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID444052Hepatic clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1917330Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured by microplate alamar blue assay2022Bioorganic & medicinal chemistry, 11-01, Volume: 73Discovery of biphenyls bearing thiobarbiturate fragment by structure-based strategy as Mycobacterium tuberculosis protein tyrosine phosphatase B inhibitors.
AID373957Ratio of AUC to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 14 mg/L administered for 0.5 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID678714Inhibition of human CYP2C19 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 3-butyryl-7-methoxycoumarin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1333278Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 4 times MIC measured after 6 hrs by luciferase reporter gene assay (Rvb = 212.7%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1296398Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID430947Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of RNA synthesis at 8 times MIC treated 5 mins before [3H]uridine challenge measured after 30 mins by [3H]uridine incorporation assay2009Journal of medicinal chemistry, Aug-27, Volume: 52, Issue:16
Design, synthesis, and structure-activity relationships of benzophenone-based tetraamides as novel antibacterial agents.
AID369916Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected Swiss mouse assessed as spleen weight at 10 mg/kg after 12 days infection weekly 5 times for 1 month2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID515285Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in BALB/c mouse lung assessed as reduction of bacterial load at 10 mg/kg, po administered 1 week after infection measured after 4 weeks2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Anti-tubercular agents. Part 5: synthesis and biological evaluation of benzothiadiazine 1,1-dioxide based congeners.
AID531305Antimicrobial activity against Clostridium difficile isolate 77 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID626871Antimicrobial activity against wild type Escherichia coli TG2 after 16 to 20 hrs2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID529536Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 CTG-ATG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1163984Antimycobacterial activity against isoniazid and rifampicin resistant Mycobacterium tuberculosis 6133 by MABA method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1517150Antimycobacterial activity against multidrug (ethambutol, INH and RIF)-resistant Mycobacterium tuberculosis clinical isolate 2 assessed as inhibition of bacterial growth incubated for 7 days by rapid direct susceptibility test technique
AID1501037Antitubercular activity against Mycobacterium tuberculosis H37Rv by Lowensteine-Jensen method2017European journal of medicinal chemistry, Oct-20, Volume: 139Recent advances of pyrazole-containing derivatives as anti-tubercular agents.
AID465094Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 4 days by alamar blue assay2010Journal of natural products, Mar-26, Volume: 73, Issue:3
Anti-infective discorhabdins from a deep-water alaskan sponge of the genus Latrunculia.
AID1781822Antimycobacterial activity against Mycobacterium bovis BCG assessed as inhibition of visible mycobacterial growth by broth microdilution method2021Journal of natural products, 10-22, Volume: 84, Issue:10
Voatriafricanines A and B, Trimeric Vobasine-Aspidosperma-Aspidosperma Alkaloids from
AID425190Antimycobacterial activity against multi drug-resistant Mycobacterium tuberculosis2009Bioorganic & medicinal chemistry letters, Jun-01, Volume: 19, Issue:11
A microwave-assisted facile regioselective Fischer indole synthesis and antitubercular evaluation of novel 2-aryl-3,4-dihydro-2H-thieno[3,2-b]indoles.
AID445290Antibacterial activity against Escherichia coli by broth dilution method2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID1418313Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by rapid direct susceptibility test
AID1447583Antibacterial activity against Pseudomonas aeruginosa PAO1 after 25 serial passages at 0.125 times MIC by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID425401Antibacterial activity against Escherichia coli isolate HM615 isolated from colonic mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1668178Antifungal activity against Candida albicans ATCC 10231 assessed as fungal growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID283163Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2639 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1614908Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 16833 after 7 days by microplate alamar blue assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties.
AID246800Effective concentration required to reduce CFU of Mycobacterium tuberculosis Erdman (ATCC 35801) strain was determined in monolayers of mouse bone marrow macrophages; Range is 0.04-0.12004Bioorganic & medicinal chemistry letters, Dec-06, Volume: 14, Issue:23
In vitro advanced antimycobacterial screening of cobalt(II) and copper(II) complexes of fluorinated isonicotinoylhydrazones.
AID103673In vitro activity compound against slowly growing Mycobacterium kansasii 12981990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1400023Antibacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 15 days under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID548358Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010European journal of medicinal chemistry, Dec, Volume: 45, Issue:12
A regio- and stereoselective 1,3-dipolar cycloaddition for the synthesis of novel spiro-pyrrolothiazolyloxindoles and their antitubercular evaluation.
AID1467458Antibacterial activity against methicillin resistant Staphylococcus aureus MRSA090 at 25 ug/ml after 24 hrs by agar well diffusion method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID1330476Half life in rat serum at 60 mg/kg, po2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Animal models in the pharmacokinetic/pharmacodynamic evaluation of antimicrobial agents.
AID501190Antimicrobial activity against Candida albicans 54 at 5 ug after 18 hrs by agar diffusion method2009Journal of natural products, Oct, Volume: 72, Issue:10
Norselic acids A-E, highly oxidized anti-infective steroids that deter mesograzer predation, from the Antarctic sponge Crella sp.
AID1170646Antitubercular activity against Mycobacterium tuberculosis H37Rv by MABA assay2014Journal of natural products, Dec-26, Volume: 77, Issue:12
Tetrahydroxanthene-1,3(2H)-dione derivatives from Uvaria valderramensis.
AID388903Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 2 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID292304Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 0.5 to 1 ug/mL by microplate Alamar blue assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID103678In vitro activity of compound against slowly growing Mycobacterium marinum 13881990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1879513Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1903 harboring rpoBD530V mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1570240Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID449207Antimycobacterial activity against Mycobacterium tuberculosis CIP 103471 by twofold agar dilution method2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID1827064Antibacterial activity against Enterococcus faecalis ATCC 29212 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1416249Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis clinical isolate2017MedChemComm, Jun-01, Volume: 8, Issue:6
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant
AID545937Ratio of MIC for Klebsiella pneumoniae ATCC 13883 to MIC for Klebsiella pneumoniae ATCC 13883 in presence of 4 ug/ml of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID571389Antibacterial activity against Acinetobacter baumannii F264 by Etest method in presence of 0.25 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID560517Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 07b63 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1244177Antitubercular activity against Mycobacterium tuberculosis H37Ra after 7 days by microplate alamar blue assay2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Design, Synthesis, and Biological Evaluation of Pyrazolo[1,5-a]pyridine-3-carboxamides as Novel Antitubercular Agents.
AID323256Antimicrobial activity against carbapenem-intermediate or resistant Acinetobacter baumannii assessed as percent susceptible isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
In vitro activities of various antimicrobials alone and in combination with tigecycline against carbapenem-intermediate or -resistant Acinetobacter baumannii.
AID509515Cytotoxicity against african green monkey Vero after 72 hrs by MTT assay2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs.
AID583694Antimicrobial activity against methicillin-resistant Staphylococcus aureus 10*3d1 harboring hypothetical protein SA1826 14A(-) and rpoB 621E mutant gene after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1261248Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis 6133 clinical isolate incubated for 7 days by microplate Alamar Blue assay2015European journal of medicinal chemistry, Nov-02, Volume: 104Synthesis, antimycobacterial and antibacterial activity of fluoroquinolone derivatives containing an 3-alkoxyimino-4-(cyclopropylanimo)methylpyrrolidine moiety.
AID1909953Selectivity ratio of MIC99 for wild type Mycobacterium tuberculosis H37Rv to MIC99 for Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1154327Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1179481Antimycobacterial activity against Mycobacterium avium ATCC 15769 in 7H9 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID1812053Antitubercular activity against Mycobacterium tuberculosis H37RvMA incubated for 14 days in GAST/FE medium by Alamar blue assay2021Journal of medicinal chemistry, 07-08, Volume: 64, Issue:13
Benzoheterocyclic Oxime Carbamates Active against
AID564967Ratio of MIC for wild type Mycobacterium bovis BCG to MIC for wild type Mycobacterium bovis BCG in presence of 1 mg/liter CCCP2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID611491Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 126 isolated from patient nasal swab after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID523661Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta105 with RNA polymerase beta subunit N474S/S475A mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID529543Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 CTG mutant assessed as bacterial growth rate at 0.04 ug/ml by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1192375Antimicrobial activity against Escherichia coli MTCC 1089 after 18 hrs by broth micro dilution method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.
AID1262576Antimicrobial activity against clinical isolates of Mycobacterium tuberculosis SAWC 3906 Atyp-beijing under 7H9 medium assessed as growth inhibition after 14 days by alamar blue assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID144873Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to ethionamide (ETA)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1570246Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 2 incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID693676Antibacterial activity against Staphylococcus aureus isolate 357 obtained from veterinary sample after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID753131Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis assessed as growth inhibition after 2 to 3 weeks by broth microdilution method2013European journal of medicinal chemistry, Jun, Volume: 64Anti-tubercular agents. Part 7: a new class of diarylpyrrole-oxazolidinone conjugates as antimycobacterial agents.
AID560518Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 15b52 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1179480Antimycobacterial activity against Mycobacterium marinum ATCC 927 in 7H9 medium after 5 days and 6 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID510531Ratio of apparent volume of distribution in diabetic tuberculosis patient to apparent volume of distribution in tuberculosis patient2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1334254Selectivity index, ratio of GI50 for human MCF7 cells to MIC90 for Mycobacterium tuberculosis H37Ra ATCC 25177 active stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1668330Antitubercular activity against autoluminescent Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth by two-fold serial dilution method2020Journal of natural products, 05-22, Volume: 83, Issue:5
Production of Antitubercular Depsipeptides via Biosynthetic Engineering of Cinnamoyl Units.
AID1716650Antibacterial activity against Enterococcus faecium ATCC 27270 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1213968Induction of CYP2C9 in human hepatocytes using diclofenac as substrate at 0.3 to 30 uM treated every 24 hrs for 2 days measured on day 5 by LC-MS/MS analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.
AID309277Antitubercular activity against Mycobacterium tuberculosis H37Rv by Agar dilution method2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Design, synthesis and antitubercular activity of diarylmethylnaphthol derivatives.
AID487840Antimycobacterial activity against Mycobacterium kansasii after 48 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID494491Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days using resazurin dye by broth microdilution assay2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
New quinoline derivatives: synthesis and investigation of antibacterial and antituberculosis properties.
AID1174927Antitubercular activity against Mycobacterium tuberculosis isolate 917/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID699541Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake at 20 uM incubated for 5 mins by scintillation counting2012Journal of medicinal chemistry, May-24, Volume: 55, Issue:10
Classification of inhibitors of hepatic organic anion transporting polypeptides (OATPs): influence of protein expression on drug-drug interactions.
AID588129Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 7 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID735212Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 12 to 28 days by L.J. agar MIC method2013European journal of medicinal chemistry, Apr, Volume: 62New 2-benzylsulfanyl-nicotinic acid based 1,3,4-oxadiazoles: their synthesis and biological evaluation.
AID1162181Antimicrobial activity against Mycobacterium smegmatis assessed as intracellular bacterial killing2014European journal of medicinal chemistry, Oct-30, Volume: 86SAR analysis of new anti-TB drugs currently in pre-clinical and clinical development.
AID1212117Induction of MRP2 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID624609Specific activity of expressed human recombinant UGT1A62000Annual review of pharmacology and toxicology, , Volume: 40Human UDP-glucuronosyltransferases: metabolism, expression, and disease.
AID765270AUC/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID103658In vitro activity of compound against rapidly growing Mycobacterium fortuitum 6461990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID581667Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID388902Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 4 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID1476348Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through microemulsion vehicle as single oral dose per gavage after 1 hr by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID727792Antibacterial activity against Serratia marcescens ATCC 13880 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID453949Antitubercular activity against Mycobacterium tuberculosis H37Rv by BACTEC460 radiometric susceptibility assay2010Bioorganic & medicinal chemistry letters, Jan-15, Volume: 20, Issue:2
Antitubercular potential of some semisynthetic analogues of phytol.
AID577205Antimicrobial activity against Escherichia coli O157:H7 PT-32 in logarithmic phase encoding Stx-1 and Stx-2 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID719008Antitubercular activity against log phase culture of Mycobacterium tuberculosis H37Rv ATCC 27294 by agar dilution method2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
AID1221854Activity of CYP3A4 in human hepatocytes assessed as increase in nifedipine oxidation activity using nifedipine as substrate at 5 uM relative to control2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Inhibition of human sterol Δ7-reductase and other postlanosterol enzymes by LK-980, a novel inhibitor of cholesterol synthesis.
AID574552Decrease in delta toxin levels in Staphylococcus aureus USA300 at subinhibitory concentrations after 24 hrs by RP-HPLC/ESI- MS2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Subinhibitory concentrations of protein synthesis-inhibiting antibiotics promote increased expression of the agr virulence regulator and production of phenol-soluble modulin cytolysins in community-associated methicillin-resistant Staphylococcus aureus.
AID540209Volume of distribution at steady state in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID581671Antibacterial activity against normal phenotype Staphylococcus aureus in cation-adjusted MH 2 broth at pH 5.5 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID283245Reduction of lung lesions in Mycobacterium tuberculosis H37Rv infected Swiss mouse at 10 mg/kg, po for 5 days/week after 2 months2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID1326386Antibacterial activity against Bacillus subtilis P10B derived after 10 passage in presence of JBIR-100 after 16 to 18 hrs by microbroth dilution assay2016Bioorganic & medicinal chemistry, 12-15, Volume: 24, Issue:24
Biological characterization of the hygrobafilomycin antibiotic JBIR-100 and bioinformatic insights into the hygrolide family of natural products.
AID1497855Antibacterial activity against Staphylococcus epidermidis ATCC 122282018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID1706097Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth by agar plate dilution method
AID1290937Antimycobacterial activity against Mycobacterium tuberculosis H37Rv cultured in 7H12 medium after 4 days by microplate Alamar blue assay2016Bioorganic & medicinal chemistry letters, Apr-15, Volume: 26, Issue:8
Design, syntheses, and anti-tuberculosis activities of conjugates of piperazino-1,3-benzothiazin-4-ones (pBTZs) with 2,7-dimethylimidazo [1,2-a]pyridine-3-carboxylic acids and 7-phenylacetyl cephalosporins.
AID1716627Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as reduction in bacterial growth by measuring chloramphenicol MIC at 4 ug/ml incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay (Rvb = 4096 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID368640Tmax in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID373031Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PU4A22 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1716706Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of doxycycline by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID776894Antibacterial activity against Staphylococcus aureus2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID1593907Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis H37Rv assessed as complete inhibition of bacterial growth incubated for 7 days by rapid direct susceptibility test
AID1174121Antimicrobial activity against Mycobacterium tuberculosis Spec. 192 by two-fold serial dilution method2015European journal of medicinal chemistry, Jan-07, Volume: 89Synthesis and evaluation of in vitro antimycobacterial activity of novel 1H-benzo[d]imidazole derivatives and analogues.
AID530532Induction of Ppbp2::lacZ gene expression in Staphylococcus aureus SH1000 at 0.05 ug/ml after 2 hrs by beta-galactosidase reporter gene assay relative to untreated control2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
AID1423477Antibacterial activity against Acinetobacter baumannii ATCC 19606 after 24 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID582266Antimicrobial activity against Bacillus cereus ATCC 4342 by broth microdilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Efficacy of oritavancin in a murine model of Bacillus anthracis spore inhalation anthrax.
AID422130Cytotoxicity against african green monkey Vero cells2009Journal of natural products, May-22, Volume: 72, Issue:5
Antimicrobial ambiguine isonitriles from the cyanobacterium Fischerella ambigua.
AID656230Antimycobacterial activity against isoniazid-, rifampin-, streptomycin-, ethambutol-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID774297Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis ATCC 358222013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID283165Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2664 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID310058Antimicrobial activity against Mycobacterium tuberculosis H37Rv assessed per disk after 24 hrs2007Bioorganic & medicinal chemistry, Dec-01, Volume: 15, Issue:23
Synthesis, antifungal and antimycobacterial activities of new bis-imidazole derivatives, and prediction of their binding to P450(14DM) by molecular docking and MM/PBSA method.
AID680380TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 2 uM, Rifampicin: 75 uM) in OATP8-expressing HEK293 cells2001The Journal of biological chemistry, Mar-30, Volume: 276, Issue:13
Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6.
AID577203Antimicrobial activity against Escherichia coli O157:H7 PT-40 in logarithmic phase encoding Stx-2 gene by broth macrodilution assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Different classes of antibiotics differentially influence shiga toxin production.
AID531053Antimicrobial activity against Clostridium difficile isolate 20 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID493954Antimicrobial activity aagainst Mycobacterium tuberculosis ATCC 14468 in starved phase by agar dilution method2010Bioorganic & medicinal chemistry letters, Aug-01, Volume: 20, Issue:15
5-Nitro-2-furoic acid hydrazones: design, synthesis and in vitro antimycobacterial evaluation against log and starved phase cultures.
AID1908130Antibacterial activity against penicillin-susceptible Pseudomonas aeruginosa ATCC 27853 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID582495Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 tissue cage Wistar rat infected model assessed as bacterial load reduction at 25 mg/kg, ip bid treated for 7 days measured 24 hrs after last dose (Rvb = 6.8 +/-0.8 logCF2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID530998Antimicrobial activity against Clostridium difficile isolate 45 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID767544Antimycobacterial activity against Mycobacterium smegmatis ATCC 19420 assessed as growth inhibition at 1 to 100 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID533665Antimicrobial activity against Staphylococcus aureus ATCC 292132008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID296125Antitubercular activity against Mycobacterium tuberculosis H37Rv by MABA assay2007Bioorganic & medicinal chemistry, Jun-15, Volume: 15, Issue:12
Synthesis of new S-derivatives of clubbed triazolyl thiazole as anti-Mycobacterium tuberculosis agents.
AID510965Antibacterial activity against Acinetobacter baumannii 1327 infected in New Zealand rabbit meningitis model assessed as reduction in bacterial count in CSF at 25 mg/kg, iv measured after 6 hrs of last dose (RVb = 5.5 No_unit)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1721019Antitubercular activity against Mycobacterium tuberculosis isolate 12525 incubated for 7 days by microplate alamar blue assay2020Journal of medicinal chemistry, 09-10, Volume: 63, Issue:17
Discovery of a Conformationally Constrained Oxazolidinone with Improved Safety and Efficacy Profiles for the Treatment of Multidrug-Resistant Tuberculosis.
AID1564637Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 16833 assessed as reduction in bacterial cell growth incubated for 7 days by microplate alamar blue assay2019European journal of medicinal chemistry, Nov-01, Volume: 181Identification of benzothiazinones containing an oxime functional moiety as new anti-tuberculosis agents.
AID1303894Antibacterial activity against multidrug resistant Acinetobacter baumannii 2208 (ATCC 19606) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID572548AUC (0 to infinity) in indian pulmonary tuberculosis patient at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1879519Antibacterial activity against metronidazole/rifampicin-resistant Helicobacter pylori CB1771 harboring rpoBL525I/D530N/rdxAE75stop mutant measured after 5 days by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID510980Antimicrobial activity against Acinetobacter baumannii 14172010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID586042Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type U3 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID416839Antimycobacterial activity against Mycobacterium ulcerans isolate CU0012007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1174109Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID565801Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB4 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1070194Antimycobacterial activity against Mycobacterium chelonae MNT1407 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID102999In vitro activity of compound against rapidly growing Mycobacterium phlei 12891990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1658969Antibacterial activity against Enterococcus faecalis ATCC 19433 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID1124850Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2014Bioorganic & medicinal chemistry letters, Apr-01, Volume: 24, Issue:7
Synthesis and antimycobacterial activities of some new thiazolylhydrazone derivatives.
AID1364760Growth inhibition of mouse RAW264.7 cells at 50 ug/ml after 48 hrs by MTT assay relative to control2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID1869571Antibacterial activity against Acinetobacter baumannii DSM 300007 assessed as reduction in bacterial growth measured after 3 days by broth microdilution method2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID341766Antimycobacterial activity against Mycobacterium tuberculosis infected patient assessed as sputum bacterial count at 20 mg/kg, po administered daily for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID510986Antimicrobial activity against Acinetobacter baumannii 940 after 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID531302Antimicrobial activity against Clostridium difficile isolate 74 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1416771Selectivity ratio of MIC for Mycobacterium smegmatis to MIC for Mycobacterium tuberculosis H37Rv2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and
AID683320Antibacterial activity against drug-resistant Mycobacterium tuberculosis 164 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID581189Induction of NF-kappaB activation in IL1-beta, TNF-alpha and IFN-gamma-stimulated human A549 cells assessed as fold increase in NF-kappaB/DNA binding at 50 ug/ml by electrophoretic mobility shift assay2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID373974AUC in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L for 1 hr2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID520290Antimicrobial activity against Staphylococcus aureus 2547 small colony variants2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Activities of daptomycin and comparative antimicrobials, singly and in combination, against extracellular and intracellular Staphylococcus aureus and its stable small-colony variant in human monocyte-derived macrophages and in broth.
AID530051Antimicrobial activity against Staphylococcus aureus 286607-R1 harboring wild type gyrB by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID558253Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in bacterial cfu in peritoneum at 10 mg/kg, sc administered 2 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID571665Ratio of the MIC for Pseudomonas aeruginosa ATCC 27853 in the absence of NAB7075 to MIC for Pseudomonas aeruginosa ATCC 27853 in the presence of 4 ug/ml of NAB70752008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1186606Antitubercular activity against Mycobacterium tuberculosis H37Rv strain by BACTEC 460 radiometric assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and 3D-QSAR study of hydrazide, semicarbazide and thiosemicarbazide derivatives of 4-(adamantan-1-yl)quinoline as anti-tuberculosis agents.
AID588128Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 6 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID333229Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay2004Journal of natural products, Sep, Volume: 67, Issue:9
Constituents of Senecio chionophilus with potential antitubercular activity.
AID373950Post antibiotic effect against Mycobacterium tuberculosis H37Rv ATCC 2517 infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 2 mg/L administered for 7 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1205589Partition coefficient, log D of the compound at pH 7.4 by shake flask method2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1690490Inhibition of multidrug-resistant Mycobacterium tuberculosis PT12 clinical isolate QcrB assessed as reduction in bacterial growth by resazurin reduction microplate assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents.
AID586041Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type 5 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1179483Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 in 7H12 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID1263164Antituberculosis activity against Mycobacterium tuberculosis H37Rv MTCC 300 at 6.25 ug/ml after 4 weeks by Lowenstein-Jensen medium method2015Bioorganic & medicinal chemistry, Dec-15, Volume: 23, Issue:24
Pyrazole clubbed triazolo[1,5-a]pyrimidine hybrids as an anti-tubercular agents: Synthesis, in vitro screening and molecular docking study.
AID1634270Drug metabolism in Mycobacterium abscessus ATCC 19977 assessed as adenine ribosylated diphosphate derivative formation by LC/MS analysis2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1293911Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID559917Ratio of AUC (0 to 24 hrs) to MIC in epithelial lining fluid of patient with Mycobacterium tuberculosis infection at 600 to 1200 mg/kg, po administered as single dose2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Population modeling and Monte Carlo simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of rifampin in lungs.
AID1916621Antitubercular activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as bacterial growth inhibition by XTT assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID285188Antimicrobial activity against vancomycin-resistant Staphylococcus aureus by time-kill methodology2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
AID776906Inhibition of Escherichia coli RNA polymerase by transcription assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID586055Antimicrobial activity against Staphylococcus aureus clone 4-4 harboring staphylococcal cassette chromosome mec element type U3 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1296405Cytotoxicity against MDCK2-MDR1 cells assessed as cell viability at 20 uM after 24 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID144872Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to ethambutol (EMB)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1276379Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID626921Antimycobacterial activity against isoniazid, rifampicin and ethambuto-resistant Mycobacterium tuberculosis using compound level ranging from 0.3125 to 5 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID1146810Antibacterial activity against Escherichia coli MC/35 assessed as inhibition of visible growth after 24 hrs by serial dilution method1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Synthesis and antibacterial activity of some derivatives of tolypomycinone. Relationship between structure and activity in ansamycins.
AID1879567Antibacterial activity against Peptostreptococcus magnus ATCC 149562022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1212148Induction of CYP2C9 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID511861Antibacterial activity against Mycobacterium smegmatis UFPEDA 71 after 24 to 48 hrs by serial dilution method2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Synthesis and evaluation of anti-Toxoplasma gondii and antimicrobial activities of thiosemicarbazides, 4-thiazolidinones and 1,3,4-thiadiazoles.
AID1916608Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition measured after 7 days by direct susceptibility assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Emerging impact of triazoles as anti-tubercular agent.
AID545917Antimicrobial activity against Escherichia coli ATCC 25922 by Etest method in presence of 4 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID495232Antimicrobial activity against wild type Mycobacterium tuberculosis 210 after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID565228Antimicrobial activity against Mycobacterium chelonae ATCC 35752 by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of porins in the susceptibility of Mycobacterium smegmatis and Mycobacterium chelonae to aldehyde-based disinfectants and drugs.
AID531266Antimicrobial activity against Clostridium difficile isolate 38 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1191015Antimycobacterial activity against Mycobacterium marinum ATCC 927 assessed as reduction in bacterial growth incubated for 5 days by MABA method2015ACS medicinal chemistry letters, Feb-12, Volume: 6, Issue:2
Syntheses and Antituberculosis Activity of 1,3-Benzothiazinone Sulfoxide and Sulfone Derived from BTZ043.
AID1447579Bactericidal activity against Pseudomonas aeruginosa PAO1 at 0.125 times antibacterial MIC after 6 hrs2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID292294Antibacterial activity against Bacillus subtilis ATCC 6633 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID1471056Selectivity index, ratio of GI50 for human PANC1 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1194335Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth at 50 uM after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID1071107Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 0.16 to 5 ug/ml after 7 days by microplate Alamar blue assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1593375Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in multidrug-resistant Mycobacterium tuberculosis KZN494 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1423469Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured MDH refolding after 20 to 40 mins by spectrometric analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1567338Antitubercular activity against replicating Mycobacterium tuberculosis H37Rv assessed as growth inhibition measured after 7 days incubation by microplate alamar blue assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and biological evaluation of 2,4,5-trisubstituted thiazoles as antituberculosis agents effective against drug-resistant tuberculosis.
AID283168Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5256 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID700528Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 at 0.3125 to 5 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID566037Antimycobacterial activity against Mycobacterium smegmatis CMCC 93202 after 72 hrs by serial double dilution technique2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and in vitro antimycobacterial activity of 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives.
AID1543320Antimicrobial activity against Staphylococcus aureus ATCC 29213 assessed as inhibition of microbial growth incubated for 24 hrs by broth microdilution assay2019Journal of natural products, 07-26, Volume: 82, Issue:7
Antibacterial Salinaphthoquinones from a Strain of the Bacterium
AID1825030Antitubercular activity against Mycobacterium smegmatis mc2155 ATCC 700084 cultured in GAST-Fe media incubated for 24 hrs by resazurin microtiter assay2022Journal of medicinal chemistry, 01-13, Volume: 65, Issue:1
Mycobactin Analogues with Excellent Pharmacokinetic Profile Demonstrate Potent Antitubercular Specific Activity and Exceptional Efflux Pump Inhibition.
AID355989Antimalarial activity against Plasmodium falciparum D62003Journal of natural products, Jun, Volume: 66, Issue:6
New manzamine alkaloids with activity against infectious and tropical parasitic diseases from an Indonesian sponge.
AID581664Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level per mg of protein after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID373790Half life in serum of Mycobacterium tuberculosis infected guinea pig2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1856857Antibacterial activity against Escherichia coli ATCC 25922 assessed as growth inhibition measured after 18 to 24 hrs by CLSI based broth microdilution method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID569262Antimicrobial activity against Escherichia coli DH5alpha2011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1413523Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2018MedChemComm, Aug-01, Volume: 9, Issue:8
Design, synthesis, and biological evaluation of
AID1915645Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis 16995 assessed as reduction in bacterial growth by MABA analysis2021European journal of medicinal chemistry, Jan-15, Volume: 210An appraisal of anti-mycobacterial activity with structure-activity relationship of piperazine and its analogues: A review.
AID1311237Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-22016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID405145AUC (0 to 24 hrs) in tuberculosis patient assessed as desacetylrifampin level at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID580847Half life in healthy human at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID532965Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 92010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID545811Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as inhibition of biofilm formation after 24 hrs by serial dilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID1856898Induction of cytoplasmic membrane depolarization in Staphylococcus aureus ATCC 25923 assessed as increase in fluorescence intensity at 1 to 4 times MIC measured within 1 min by DiSC3-5 dye based fluorescence method2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID388898Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 64 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID479650Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 2.5 ug/ml after 4 days2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis.
AID406609Cmin in albino guinea pig cage fluid at 12.5 mg/kg, ip administered as single dose measured after 12 hrs2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID1069173Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 assessed as growth inhibition after 7 days by broth microdilution assay2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID313229Antimicrobial activity against Staphylococcus aureus at 100 ug/disc2008Bioorganic & medicinal chemistry, Jan-01, Volume: 16, Issue:1
Synthesis, anti-Toxoplasma gondii and antimicrobial activities of benzaldehyde 4-phenyl-3-thiosemicarbazones and 2-[(phenylmethylene)hydrazono]-4-oxo-3-phenyl-5-thiazolidineacetic acids.
AID1204849Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as parasite growth inhibition after 7 days by broth microdilution assay2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, antimalarial and antitubercular activities of meridianin derivatives.
AID1879527Antibacterial activity against Clostridioides difficile CB1921 ATCC BAA1382 measured after 3 days2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID396035Antibacterial activity against drug-resistant Enterobacter cloacae EcDC64 isolate expressing AcrAB-TolC efflux pump in presence of 20 ug/ml efflux pump inhibitor Phe-Arg-beta-naphthylamide by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID545598Bactericidal activity against stationary-phase methicillin-resistant Staphylococcus aureus ATCC 33591 grown on nutrient-depleted CAMHB medium at 4 ug/ml after 24 hrs by time kill analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID1706676Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition by MABA2021European journal of medicinal chemistry, Jan-01, Volume: 209Design, synthesis, and evaluation of substituted 2-acylamide-1,3-benzo[d]zole analogues as agents against MDR- and XDR-MTB.
AID404131Antibacterial activity against methicillin-sensitive Staphylococcus aureus MB26852005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID1209484Activation of PXR in human Hu1108 hepatocytes assessed as increase in CYP3A-mediated testosterone 6beta-hydroxylation at 10 uM after 24 hrs by HPLC analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID510967Antibacterial activity against Acinetobacter baumannii 1327 infected in New Zealand rabbit meningitis model assessed as reduction in bacterial count in CSF at 25 mg/kg, iv measured after 2 hrs of last dose (RVb = 5.1 No_unit)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1294351Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by BacTiter-Glo cell viability assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID370252Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 5 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1690491Inhibition of multidrug-resistant Mycobacterium tuberculosis PT20 clinical isolate QcrB assessed as reduction in bacterial growth by resazurin reduction microplate assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents.
AID408868Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in J744 cells assessed as reduction in number of surviving bacteria at 1 ug/mL relative to control2008Journal of medicinal chemistry, Jun-26, Volume: 51, Issue:12
1,5-Diphenylpyrrole derivatives as antimycobacterial agents. Probing the influence on antimycobacterial activity of lipophilic substituents at the phenyl rings.
AID510532Bioavailability in diabetic tuberculosis patient at 10 mg/kg, po and 10 mg/kg, iv by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1614909Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties.
AID416843Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load at 10 mg/kg, po administered for 5 days per week measured after 4 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1462368Antitubercular activity against Mycobacterium tuberculosis H37Ra BSL2 cultured in broth2017Bioorganic & medicinal chemistry letters, 09-01, Volume: 27, Issue:17
2-N-Arylthiazole inhibitors of Mycobacterium tuberculosis.
AID419826Antibacterial activity against Bacillus subtilis MTCC 619 at 1000 ug/ml after 24 hrs by agar diffusion method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID1654161Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as reduction in microbial growth after 7 days by alamar blue assay2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID775853Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition by micro plate alamar blue assay2013Bioorganic & medicinal chemistry letters, Nov-01, Volume: 23, Issue:21
Studies on substituted benzo[h]quinazolines, benzo[g]indazoles, pyrazoles, 2,6-diarylpyridines as anti-tubercular agents.
AID531123Antimicrobial activity against Staphylococcus aureus CB814 harboring gyrA S48L and parC S80F mutant genes2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID571644Antibacterial activity against Citrobacter freundii ATCC 8090 by Etest method in presence of 4 ug/ml NAB70692008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1860214Aqueous solubility of compound by HPLC analysis2022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of new quinoline derivatives as selective C-RAF kinase inhibitors with potent anticancer activity.
AID276755Antimycobacterial activity against isoniazid resistant Mycobacterium tuberculosis ATCC 358222006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID474491Biodistribution in rat brain at 100 mg/kg, ip after 3 to 7 hrs2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Radiosynthesis and bioimaging of the tuberculosis chemotherapeutics isoniazid, rifampicin and pyrazinamide in baboons.
AID1888731Antitubercular activity against Mycobacterium tuberculosis M299 assessed as reduction in microbial growth after 5 days by MTT assay2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Antimycobacterial and anti-inflammatory activities of thiourea derivatives focusing on treatment approaches for severe pulmonary tuberculosis.
AID461353Antifungal activity against Cryptococcus neoformans ATCC 901132010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections.
AID558752Antibacterial activity against hetero-Methicillin-resistant and tetracycline-resistant Staphylococcus aureus deltaIP by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID588130Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 1 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID645529Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in GAST medium after 1 week by microplate alamar blue assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1055958Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID368642Cmin in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 300 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID532973Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 172010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1192652Inhibition of Mycobacterium tuberculosis H37Rv ATP synthase assessed as reduction in total ATP content at 0.5 ug/ml after 18 hrs by bead-vortexing settling method2015Bioorganic & medicinal chemistry, Feb-15, Volume: 23, Issue:4
Novel, potent, orally bioavailable and selective mycobacterial ATP synthase inhibitors that demonstrated activity against both replicating and non-replicating M. tuberculosis.
AID1484397Growth inhibition of Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 5 to 8 days2017European journal of medicinal chemistry, Jun-16, Volume: 133Isoniazid derivatives and their anti-tubercular activity.
AID446153Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing pFCA-luxAB after 10 days by low-oxygen recovery assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.
AID478058Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 to 10 days by microplate alamar blue assay2010Journal of natural products, Apr-23, Volume: 73, Issue:4
Structure and anti-TB activity of trachylobanes from the liverwort Jungermannia exsertifolia ssp. cordifolia.
AID559767Antimycobacterial activity against Mycobacterium smegmatis harboring PknG Msm gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID509626Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB519 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID571397Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID554573Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in intracellular bacterial cfu in peritoneum at 60 mg/kg, sc administered 2 hrs after infection evry 8 hrs as three-dose regimen measured after 192009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID541066Half life in cage fluid of Albino guiena pig at 12.5 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID776895Antibacterial activity against Pseudomonas aeruginosa PAO12013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID1359451Antitubercular activity against multidrug-resistant dormant stage of Mycobacterium tuberculosis H37Ra after 12 days by XRMA2018European journal of medicinal chemistry, May-25, Volume: 152Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life.
AID530347Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M carrying blaCTX-M-15 and pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID163949In vitro antibacterial activity of compound against Pseudomonas aeruginosa ATCC 101451990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1869529Antibacterial activity against multidrug-resistant Morganella morganii KL-225 measured after 24 hrs by broth microdilution method
AID285195Antimicrobial activity against Escherichia coli M073 mutant with AG100 lon2::IS186 acrR::IS5 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID634279Antimycobacterial activity against Mycobacterium tuberculosis isolate 309 expressing rpoB His526Arg mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID679145TP_TRANSPORTER: inhibition of Taurocholate uptake in membrane vesicles from Bsep-expressing Sf9 cells2000Gastroenterology, Feb, Volume: 118, Issue:2
Drug- and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver.
AID1570731Antimicrobial activity against Enterococcus faecium AUS0004 at 5 ug/disk incubated for 20 +/- 4 hrs by agar disk diffusion method2019Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21
Synthesis and evaluation of 1,3,4-oxadiazole derivatives for development as broad-spectrum antibiotics.
AID1061101Antimicrobial activity against Mycobacterium tuberculosis H37Rv in presence of 10% FBS2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID1209481Activation of PXR in human Hu1043 hepatocytes assessed as upregulation of CYP3A4 mRNA expression at 10 uM after 24 hrs by RT-PCR analysis relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID1399858Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv harboring RpoB S522L mutant2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID1716629Antibacterial activity against Pseudomonas aeruginosa 260-97103 assessed as reduction in bacterial growth by measuring chloramphenicol MIC at 2 ug/ml incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay (Rvb = 128 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID442658Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis by agar dilution method2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
AID1312204Antibacterial activity against nutrient-starved dormant Mycobacterium tuberculosis H37Rv assessed in log reduction in bacterial count at 10 ug/ml measured after 7 days by MPN assay relative to control2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors.
AID1497856Antibacterial activity against Salmonella paratyphi A serotype ATCC 5702 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID565795Antimicrobial activity against Neisseria meningitidis harboring rpoB50 S557F mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID206207In vitro antibacterial activity of compound against Staphylococcus epidermidis ATCC 122281990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1079936Choleostatic liver toxicity, either proven histopathologically or where the ratio of maximal ALT or AST activity above normal to that of Alkaline Phosphatase is < 2 (see ACUTE). Value is number of references indexed. [column 'CHOLE' in source]
AID1400058Bactericidal activity against Escherichia coli ATCC 10798 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID534110Antibacterial activity against TolC deficient Pasteurella multocida pm1980 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1232411Selectivity index, ratio of GIC50 for mouse RAW264.7 cells to MIC for Mycobacterium tuberculosis H37Rv2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides.
AID1716711Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as fractional inhibitory concentration index in presence of chloramphenicol incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1678512Antibacterial activity against Clostridium difficile 8260 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID531278Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 50 expressing RpoB R505K mutant by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID545923Antimicrobial activity against Klebsiella pneumoniae ATCC 13883 by Etest method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID588982Inhibitors of transporters of clinical importance in the absorption and disposition of drugs, OATP1B32010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID1491298Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 27294 under normoxic condition2017European journal of medicinal chemistry, Sep-08, Volume: 137QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity.
AID1784359Antimycobacterial activity against Mycobacterium tuberculosis DprE1 P116S in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID530634Antimicrobial activity against Staphylococcus aureus CB808 harboring quinolone-resistant parC S80F mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID297110Antibacterial activity against Mycobacterium tuberculosis H37Rv after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID456896Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents.
AID530782Antimicrobial activity against Clostridium difficile isolate 13 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID560516Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 11b091 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID693665Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID309184Antibacterial activity against Mycobacterium tuberculosis H37Rv by nitrate reductase assay2007Bioorganic & medicinal chemistry letters, Oct-01, Volume: 17, Issue:19
Anti-tubercular agents. Part IV: Synthesis and antimycobacterial evaluation of nitroheterocyclic-based 1,2,4-benzothiadiazines.
AID1577339Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis 8666/2010 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID1678508Antibacterial activity against Clostridium difficile ATCC 700057 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID495513Antibacterial activity against Acinetobacter baumannii BM4467 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID103644In vitro activity of compound against rapidly growing Mycobacterium fortuitum 1141990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1772302Non-covalent inhibition of DprE1 in multidrug-resistant Mycobacterium tuberculosis clinical isolate 13946 measured after 7 days by microplate Alamar blue assay
AID441083Antimycobacterial activity against Mycobacterium tuberculosis CIB99 after 5 to 7 days by microplate alamar blue assay2009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID523656Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta100 with RNA polymerase beta subunit I467L mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID1209592Dissociation constant, pKa of the basic compound by capillary electrophoresis-mass spectrometry analysis2011Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 39, Issue:3
Measurement of unbound drug exposure in brain: modeling of pH partitioning explains diverging results between the brain slice and brain homogenate methods.
AID565809Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB40 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1778126Antimicrobial activity against methicillin-resistant Staphylococcus aureus assessed as microbial growth inhibition by CLSI-protocol based broth microdilution assay2021Journal of natural products, 04-23, Volume: 84, Issue:4
Opportunities and Limitations for Assigning Relative Configurations of Antibacterial Bislactones using GIAO NMR Shift Calculations.
AID1416768Antitubercular activity against Mycobacterium tuberculosis H37Rv after 2 weeks by broth microdilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and
AID569256Antimycobacterial activity against Mycobacterium bovis BCG str. Tokyo 1722011Bioorganic & medicinal chemistry letters, Feb-01, Volume: 21, Issue:3
Synthesis and evaluation of anti-tubercular activity of new dithiocarbamate sugar derivatives.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID434063Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced [3H]arachidonic acid release at 50 ug/ml measured after 2 hrs of IL1-beta challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1181162Antimicrobial activity against clinical isolate Mycobacterium tuberculosis DKU211 assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID558242Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 9 mg/liter after 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID634280Antimycobacterial activity against Mycobacterium tuberculosis isolate 344 expressing rpoB Ser522Leu mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID757722Inhibition of Escherichia coli RNAP assessed as incorporation of [5,6-3H]UTP preincubated for 10 mins followed by DNA template and ATP, CTP, GTP, UTP, [5,6-3H]UTP addition measured after 10 mins by scintillation counting analysis2013European journal of medicinal chemistry, Jul, Volume: 65Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: structure-based optimization of a virtual screening hit.
AID436697Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by BACTEC radiometric respiratory technique2009European journal of medicinal chemistry, Oct, Volume: 44, Issue:10
Synthesis, spectral and biological evaluation of some new thiazolidinones and thiazoles based on t-3-alkyl-r-2,c-6-diarylpiperidin-4-ones.
AID694775Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 after 7 days by resazurin microtitre assay2012Bioorganic & medicinal chemistry, Nov-01, Volume: 20, Issue:21
1,3-Azoles from ortho-naphthoquinones: synthesis of aryl substituted imidazoles and oxazoles and their potent activity against Mycobacterium tuberculosis.
AID531052Antimicrobial activity against Clostridium difficile isolate 19 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1634258Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 400 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1716652Antibacterial activity against gentamicin-resistant Escherichia coli CAN-ICU 61714 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1293880Antitubercular activity against Mycobacterium bovis BCG ATCC 35743 incubated for 40 mins by XTT Reduction Menadione Assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1667186Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth by MABA assay2020Bioorganic & medicinal chemistry letters, 04-15, Volume: 30, Issue:8
Synthesis and efficacy of pyrvinium-inspired analogs against tuberculosis and malaria pathogens.
AID1667678Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 5 days by alamar blue based colorimetric assay2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from l-serine.
AID508221Inhibition of enteroaggregative Escherichia coli 042 adherence to human Hep2 cells pretreated by adherence assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Pretreatment of epithelial cells with rifaximin alters bacterial attachment and internalization profiles.
AID565779Antimicrobial activity against Neisseria meningitidis harboring rpoB13 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID532957Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 12010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID537734Antifungal activity against yeast AD1-8u expressing Candida albicans CaMdr1p by agar disk diffusion assay2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1311274Antimycobacterial activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 measured on day 12 by XTT reduction menadione assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID571451Antibacterial activity against Enterobacter cloacae ATCC 23355 ATCC 13883 by Etest method in presence of 4 ug/ml NAB70642008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID370268AUC (0 to t) in human at 450 mg, po2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID539834Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2010Bioorganic & medicinal chemistry letters, Dec-15, Volume: 20, Issue:24
A facile 1,3-dipolar cycloaddition of azomethine ylides to 2-arylidene-1,3-indanediones: synthesis of dispiro-oxindolylpyrrolothiazoles and their antimycobacterial evaluation.
AID584273Inhibition of bovine Chymotrypsin at 0.0472 uM2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase.
AID1332963Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in presence of nitric oxide scavanger PTIO after 7 days by REMA method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID1542194Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 12 to 28 days by agar dilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Pyridine and nitro-phenyl linked 1,3,4-thiadiazoles as MDR-TB inhibitors.
AID1580096Antibacterial activity against wild type Acinetobacter baumannii ATCC 17978 by checkerboard assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Homodimeric Tobramycin Adjuvant Repurposes Novobiocin as an Effective Antibacterial Agent against Gram-Negative Bacteria.
AID530784Antimicrobial activity against Clostridium difficile isolate 15 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID530803Antimicrobial activity against Clostridium difficile isolate 34 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID530991Antimicrobial activity against Clostridium difficile isolate 38 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID531034Antimicrobial activity against Clostridium difficile isolate 1 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID558754Antibacterial activity against methicillin-susceptible, tetracycline-resistant and chloramphenicol-resistant Staphylococcus aureus deltaIP-KVR by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID562794Antimicrobial activity against Chlamydia trachomatis J/6276/oflR-rifR1 harboring ompA and rpoB genes2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1403703Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Rv incubated for 1 week in presence of verapamil by MABA method2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID565811Antimicrobial activity against Neisseria meningitidis assessed as susceptible isolate by broth microdilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Determination of CEM-101 activity tested against clinical isolates of Neisseria meningitidis from a worldwide collection.
AID479636Antimycobacterial activity against Mycobacterium tuberculosis H37Ra at 0.5 to 1 ug/ml after 6 days by microplate alamar blue assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis.
AID545049Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ249 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID565188Antimicrobial activity against Staphylococcus epidermidis RP62A by microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Evaluation of analogs of reutericyclin as prospective candidates for treatment of staphylococcal skin infections.
AID728674Antimicrobial activity against wild type Escherichia coli O18:K1:H7 after overnight incubation2013Journal of medicinal chemistry, Feb-28, Volume: 56, Issue:4
Novel HldE-K inhibitors leading to attenuated Gram negative bacterial virulence.
AID1193493Thermodynamic equilibrium solubility, log S of the compound in PBS at pH 7.4 at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID425612Cytotoxicity against mouse J774A1 cells assessed as release of adenylate kinase at 100 ug/ml after 3 hrs by total cell protein assay relative to control2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1185144Antimicrobial activity against 2-oxo-1-(2-(4-((3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino)piperidin-1-yl)ethyl)-1,2-dihydroquinoline-7-carbonitrile resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase A74V mutant2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID1399839Antibacterial activity against Mycobacterium smegmatis ATCC 194202018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID395781Antibacterial activity against Staphylococcus aureus ATCC 25923 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID520085Antimicrobial activity against acrAB-deficient Escherichia coli TG1 harboring plasmid pEX19Gm by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID1879545Antibacterial activity against rifampicin/fluoroquinolone-resistant Clostridioides difficile CB1942 harboring rpoBQ489K/gyrAD71Y/T82A mutant at at 1:1 compound to metronidazole molar ratio measured after 3 days in presence of metronidazole2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1210907Intrinsic clearance in human jejunum microsome at 0.05 to 1 mM2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID325002Antibacterial activity against rifampin and cefdinir-resistant Haemophilus influenzae RdRIF/MSC06651 mutant by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID1879676Antibacterial activity against Clostridioides difficile BAA 13822022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1558530Cmax in rat at 10 mg/kg, po2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R).
AID530772Antimicrobial activity against Clostridium difficile isolate 3 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1179482Antimycobacterial activity against Mycobacterium kansasii ATCC 12478 in 7H9 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID560223Antibacterial activity against Salmonella enterica serovar Typhimurium R200 expressing Outer membrane protein STM3031 by CLSI M7-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Outer membrane protein STM3031 (Ail/OmpX-like protein) plays a key role in the ceftriaxone resistance of Salmonella enterica serovar Typhimurium.
AID1311367Antibacterial activity against Mycobacterium tuberculosis 115R measured after 14 days by broth microdilution assay2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
An evolved oxazolidinone with selective potency against Mycobacterium tuberculosis and gram positive bacteria.
AID765268T>MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID104012In vitro antibacterial activity of compound against Mycobacterium tuberculosis H37Rv ATCC 96601990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID245086Minimum inhibitory concentration against Mycobacterium tuberculosis H37Rv ATCC 272942005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
Synthesis of isonicotinic acid N'-arylidene-N-[2-oxo-2-(4-aryl-piperazin-1-yl)-ethyl]-hydrazides as antituberculosis agents.
AID445331Cytotoxicity against human MRC5 cells2009Bioorganic & medicinal chemistry letters, Nov-15, Volume: 19, Issue:22
Synthesis of new sugar derivatives and evaluation of their antibacterial activities against Mycobacterium tuberculosis.
AID545925Antimicrobial activity against Klebsiella pneumoniae ATCC 13883 by Etest method in presence of 4 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID475037Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 4 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
New 3-methylquinoxaline-2-carboxamide 1,4-di-N-oxide derivatives as anti-Mycobacterium tuberculosis agents.
AID1597872Selectivity index, ratio of IC50 for mouse J774.A1 cells to MIC for Mycobacterium tuberculosis H37Rv
AID1182131Antitubercular activity against Mycobacterium smegmatis by checkerboard assay2014Bioorganic & medicinal chemistry, Aug-15, Volume: 22, Issue:16
Pharmacologically active metabolites, combination screening and target identification-driven drug repositioning in antituberculosis drug discovery.
AID559093Bactericidal activity against yafQ gene-deficient Escherichia coli K-12 BW25113 biofilm assessed as log reduction of viable cells after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
The chromosomal toxin gene yafQ is a determinant of multidrug tolerance for Escherichia coli growing in a biofilm.
AID680732TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 2 uM, Rifampicin: 75 uM) in OATP-C-expressing HEK293 cells2001The Journal of biological chemistry, Mar-30, Volume: 276, Issue:13
Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6.
AID577495Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315 by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1565654Ratio of MIC for antibacterial activity against Escherichia coli ATCC 25922 after 15 passages to MIC for antibacterial activity against Escherichia coli ATCC 25922 incubated for 18 hrs2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID1293909Selectivity index, ratio of GI50 for human PANC1 cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1193492Thermodynamic equilibrium solubility, log S of the compound in water at RT after 4 hrs by 96 well plate method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID434057Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced PGE2 formation at 50 ug/ml after 48 hrs by enzyme immunoassay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID563696Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Ra2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID765271fAUC/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID293685Antituberculosis activity against Mycobacterium tuberculosis H37Rv by Microplate Alamar Blue Assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Clubbed triazoles: a novel approach to antitubercular drugs.
AID1716656Antibacterial activity against gentamicin, tobramycin-resistant Pseudomonas aeruginosa CANWARD 96846 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID289147Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID373961Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as concentration needed to achieve 50% effect on maximal g2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID442659Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010European journal of medicinal chemistry, Jan, Volume: 45, Issue:1
Discovery of novel antitubercular 2,10-dihydro-4aH-chromeno[3,2-c]pyridin-3-yl derivatives.
AID1220556Fraction unbound in CD-1 mouse brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1860215n-Octanol/PBS partition coefficient, logD of the compound at pH 7.42022European journal of medicinal chemistry, Aug-05, Volume: 238Design and synthesis of new quinoline derivatives as selective C-RAF kinase inhibitors with potent anticancer activity.
AID529529Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 30167 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1262565Antimicrobial activity against GFP expressing recombinant Mycobacterium tuberculosis H37RvMA under GAST/Fe medium assessed as growth inhibition after 14 days by broth microdilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID406470Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as stationary-growth-phase minimal bactericidal concentration after 24 hrs by macrotube dilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID588123Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 1 expressing beta-lactamase NDM-1 obtained from urine of patient by Etest2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID1594636Antimycobacterial activity against replicating Mycobacterium tuberculosis SS18b assessed as inhibition of parasite growth incubated for 6 days by REMA method2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID1879557Antibacterial activity against Clostridium sporogenes ATCC 194042022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID400492Inhibition of AAH in Sprague-Dawley rat intestine microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 0.10 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1436938Selectivity index, ratio of GI90 for human HCT116 cells to MIC90 for dormant state of dormant state of Mycobacterium bovis BCG2017Bioorganic & medicinal chemistry letters, 02-15, Volume: 27, Issue:4
Quinolidene based monocarbonyl curcumin analogues as promising antimycobacterial agents: Synthesis and molecular docking study.
AID294762Antibacterial activity against methicillin-resistant Staphylococcus aureus 873 after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID504180Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days2010Bioorganic & medicinal chemistry, Sep-15, Volume: 18, Issue:18
Identification of novel antitubercular compounds through hybrid virtual screening approach.
AID532972Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 162010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1614906Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties.
AID444053Renal clearance in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID545907Antimicrobial activity against Escherichia coli ATCC 259222010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID657788Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 926 from Chinese tuberculosis patient measured 24 hrs post dose by microplate alamar blue assay2012European journal of medicinal chemistry, Jun, Volume: 52Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
AID103845In vitro activity of compound against rapidly growing Mycobacterium smegmatis 14421990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1177944Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition2014European journal of medicinal chemistry, Apr-09, Volume: 76Recent advances in the structural library of functionalized quinazoline and quinazolinone scaffolds: synthetic approaches and multifarious applications.
AID1678515Antibacterial activity against Clostridium difficile 8264 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID1739761Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by Microplate Alamar Blue Assay2020European journal of medicinal chemistry, Sep-01, Volume: 201Antitubercular polyhalogenated phenothiazines and phenoselenazine with reduced binding to CNS receptors.
AID694364Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis MS-115 under anaerobic condition assessed as growth inhibition at 1 ug/ml by BACTEC method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
The synthesis and antituberculosis activity of 5'-nor carbocyclic uracil derivatives.
AID265977Cytotoxicity against Vero cell line2006Journal of medicinal chemistry, Jun-15, Volume: 49, Issue:12
Discovery of new antitubercular oxazolyl thiosemicarbazones.
AID428290Antimicrobial activity against Acinetobacter baumannii BM4454 isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID1333139Induction of membrane disruption in Mycobacterium smegmatis MC2 155 assessed as increased cytoplasmic membrane permeability at 60 uM up to 3 hrs by Sytox green uptake assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1127156Cytotoxicity against African green monkey Vero cells assessed as cell viability after 72 hrs by MTT assay2014European journal of medicinal chemistry, May-22, Volume: 79Facile synthesis of benzonitrile/nicotinonitrile based s-triazines as new potential antimycobacterial agents.
AID1634989Antimicrobial activity against Staphylococcus aureus 6271 assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID1297723Antibacterial activity against Staphylococcus epidermidis ATCC 49134 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1516024Antibacterial activity against Staphylococcus epidermidis ATCC 12228 incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1603256Antibacterial activity against RMP-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay
AID530642Inhibition of protein synthesis in Staphylococcus aureus CB190 assessed as decrease in L-[3,4,5-3H]leucine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1223076Induction of Ugt2b34 gene expression in PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID403754Antitubercular activity against Mycobacterium tuberculosis 90-2213872005Journal of natural products, Sep, Volume: 68, Issue:9
Antitubercular constituents from the stem wood of Cinnamomum kotoense.
AID571454Antibacterial activity against Escherichia coli by Etest method in presence of 4 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1634245Antimycobacterial activity against Mycobacterium chelonae assessed as reduction in microbial growth by CLSI method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1888125Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1777208Agonist activity at human PXR transfected in human HEK293T cells co-transfected with CYP3A4-Luc plasmid at 10 uM incubated for 24 hrs by dual-luciferase reporter gene assay relative to control2021ACS medicinal chemistry letters, Jul-08, Volume: 12, Issue:7
Lathyrane Diterpenoids as Novel hPXR Agonists: Isolation, Structural Modification, and Structure-Activity Relationships.
AID1400026Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID572058Ratio of MIC for Escherichia coli KAM32 harboring plasmid pUC18 to MIC for Escherichia coli KAM32 harboring recombinant plasmid pVBS1 encoding Acinetobacter baumannii abeS gene2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID103509In vitro activity of compound against rapidly growing Mycobacterium flavescens 12841990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1333106Antimycobacterial activity against Mycobacterium smegmatis MC2 155 after 24 hrs by broth dilution assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID625284Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic failure2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1126675Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of colony formation at 100 ug/mL after 2 to 4 weeks by Lowensteine-Jensen method relative to control2014European journal of medicinal chemistry, May-06, Volume: 78Synthesis, characterization and pharmacological screening of some novel 5-imidazopyrazole incorporated polyhydroquinoline derivatives.
AID1567339Antimycobacterial activity against dormant stage of Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as growth inhibition at 10 uM incubated for 12 days by XRMA method relative to control2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and biological evaluation of 2,4,5-trisubstituted thiazoles as antituberculosis agents effective against drug-resistant tuberculosis.
AID1557233Antitubercular activity against resistant Mycobacterium tuberculosis 75 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID1706093Cytotoxicity against human PBMC assessed as reduction in cell growth after 72 hrs by MTT assay
AID1897864Bactericidal activity against Non-replicating Mycobacterium tuberculosis ss18b-lux model assessed as decrease in luminescence at 10 to 10000 nM
AID285190Antimicrobial activity against Escherichia coli AG100 mutant with argE3 thi-3 rpsL xyl mtl supE44 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID1053480Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA M103L mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID1781821Antimycobacterial activity against Mycobacterium abscessus subsp. bolletii assessed as inhibition of mycobacterial growth incubated for 2 to 3 days by broth microdilution method2021Journal of natural products, 10-22, Volume: 84, Issue:10
Voatriafricanines A and B, Trimeric Vobasine-Aspidosperma-Aspidosperma Alkaloids from
AID1510690Acute toxicity in ICR mouse assessed as animal survival at 500 mg/kg, po administered as single dose measured for 7 days2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents.
AID1625576Bactericidal activity against wild-type non-replicating Mycobacterium tuberculosis H37Rv at 1 to 100 ug/ml incubated for 7 days measured at OD580 = 0.1 in presence of 1 mM NaNO22016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID564980Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring inactivated p55 gene by resazurine microtiter assay in presence of 0.1 mg/liter valinomycin2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID600827Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents.
AID558023Protein binding in human serum at 600 mg, po2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1858570Antibacterial activity against Mycobacterium tuberculosis H37Rv expressing GFP incubated for 7 days2021European journal of medicinal chemistry, Jan-01, Volume: 209Lipolytic enzymes inhibitors: A new way for antibacterial drugs discovery.
AID292289Antibacterial activity against Proteus vulgaris ATCC 49132 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1435652Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 234/2005 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1609006Antimycobacterial activity against Mycobacterium smegmatis DSM 43465 after 120 hr by resazurin dye based microdilution method2019European journal of medicinal chemistry, Nov-01, Volume: 181Phenolic N-monosubstituted carbamates: Antitubercular and toxicity evaluation of multi-targeting compounds.
AID1471026Growth inhibition of Mycobacterium tuberculosis H37Ra ATCC 25177 at 10 ug/ml by XTT dye based two-fold dilution method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID1888137Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD3 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID565797Antimicrobial activity against Neisseria meningitidis harboring rpoB53 G560S mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID689774Selectivity index, ratio of CC50 for Vero cells to MIC90 for Mycobacterium tuberculosis H37Rv isolate SRI2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis.
AID144140In vitro anti-mycobacterial activity against Mycobacterium intracellular ATCC 23068. 1992Journal of medicinal chemistry, Oct-30, Volume: 35, Issue:22
Copyrine alkaloids: synthesis, spectroscopic characterization, and antimycotic/antimycobacterial activity of A- and B-ring-functionalized sampangines.
AID1337871Selectivity index, ratio of GI50 for human PANC1 cells to MIC for Mycobacterium bovis BCG ATCC 35743 at dormant stage2017European journal of medicinal chemistry, Jan-05, Volume: 125Quinolidene-rhodanine conjugates: Facile synthesis and biological evaluation.
AID1400040Antibacterial activity against Staphylococcus aureus BAA 2094 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID293932Effect on RNA transcription in Staphylococcus aureus ATCC 25923 assessed as [3H]uridine incorporation after 20 mins relative to control2007Bioorganic & medicinal chemistry, Mar-15, Volume: 15, Issue:6
N-thiolated beta-lactams: Studies on the mode of action and identification of a primary cellular target in Staphylococcus aureus.
AID294764Antibacterial activity against methicillin-resistant Staphylococcus aureus 908 after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID1395986Induction of biofilm eradication of methicillin-resistant Staphylococcus epidermidis ATCC 35984 after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID571442Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID292309Antibacterial activity against Staphylococcus epidermidis ATCC 14990 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID1517149Antimycobacterial activity against multidrug (INH and RIF)-resistant Mycobacterium tuberculosis clinical isolate 1 assessed as inhibition of bacterial growth incubated for 7 days by rapid direct susceptibility test technique
AID564975Antimicrobial activity against Mycobacterium bovis BCG by resazurine microtiter assay in presence of 0.1 mg/liter valinomycin2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1303881Antibacterial activity against multidrug resistant Enterococcus faecium NCTC 7171 (ATCC 19434) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID1594307Growth inhibition of human A549 cells by MTT assay2019Bioorganic & medicinal chemistry letters, 05-15, Volume: 29, Issue:10
Thiazolyl-pyrazole derivatives as potential antimycobacterial agents.
AID571425Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method by Etest in presence of 2 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1879510Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1902 harboring rpoBV149F mutant at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1224525Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis Praha 4 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID1447575Bactericidal activity against Pseudomonas aeruginosa PAO1 at 4 times antibacterial MIC after 2 hrs2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID560505Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate b2k4781 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID565994Antimycobacterial activity against Mycobacterium tuberculosis H37Ra by twofold agar dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID543818Bactericidal activity against Escherichia coli ATCC 25922 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1297721Antibacterial activity against Staphylococcus aureus ATCC 6538 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1634992Antimicrobial activity against Staphylococcus aureus clinical isolates from university hospital in Motol assessed as reduction in bacterial growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID352089Antimicrobial activity against Klebsiella pneumoniae RSHM 574 after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID1570241Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID1577327Antimycobacterial activity against multi-drug resistant Mycobacterium tuberculosis Praha 1 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID617850Antitubercular activity against drug sensitive Mycobacterium tuberculosis H37Rv ATCC 27294 by microplate Alamar blue assay2011Journal of natural products, Sep-23, Volume: 74, Issue:9
Stereochemical analysis of leubethanol, an anti-TB-active serrulatane, from Leucophyllum frutescens.
AID562799Antimicrobial activity against Chlamydia muridarum MoPn/tetR1 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1634241Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at 3.125 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1699965Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition by MABA relative to control2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and biological evaluation of anti-tubercular activity of Schiff bases of 2-Amino thiazoles.
AID1457512Antibacterial activity against Bacillus subtilis assessed as inhibition of peptidoglycan synthesis at 2 mg/L after 50 mins by [3H]-N-acetylglucosamine incorporation assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents.
AID680469TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing LLC-PK1 cells2002Pharmaceutical research, Feb, Volume: 19, Issue:2
Comparative inhibitory effects of different compounds on rat oatpl (slc21a1)- and Oatp2 (Slc21a5)-mediated transport.
AID1262573Antimicrobial activity against GFP expressing recombinant Mycobacterium tuberculosis H37RvMA under 7H9 medium assessed as growth inhibition after 14 days by broth microdilution method2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID163581In vitro antibacterial activity of compound against Proteus vulgaris X19H ATCC 8811990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1223009Induction of Cyp2c29 gene expression in male PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID380452Antibacterial activity against Mycobacterium tuberculosis H37Rv at 6.25 mg/ml2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID531009Antimicrobial activity against Clostridium difficile isolate 56 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1457517Antibacterial activity against Bacillus subtilis assessed as inhibition of plasma membrane lipids synthesis at 2 mg/L after 50 mins by [3H]-sodium acetate incorporation assay2017Journal of medicinal chemistry, 07-27, Volume: 60, Issue:14
Lipophosphonoxins II: Design, Synthesis, and Properties of Novel Broad Spectrum Antibacterial Agents.
AID1196884Antimycobacterial activity against dormant Mycobacterium tuberculosis H37Rv model assessed as log reduction at 10 ug/ml incubated for 7 days measured after 28 days in presence of nutrient deprived condition2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID456898Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Design and synthesis of some new quinoline-3-carbohydrazone derivatives as potential antimycobacterial agents.
AID531292Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 64 expressing RpoB H502R mutant by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID565186Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 by microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Evaluation of analogs of reutericyclin as prospective candidates for treatment of staphylococcal skin infections.
AID268910Protection index, cytotoxicity against Vero cell line/antibacterial activity against Mycobacterium tuberculosis 1034712006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID1212143Induction of CYP2B6 in human hepatocytes at 10 uM after 72 hrs relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID380457Antibacterial activity against Escherichia coli ATCC 25922 by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID572539Apparent oral clearance in pulmonary tuberculosis patient in transit compartment model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1224521Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 7 days by micromethod2014European journal of medicinal chemistry, Jul-23, Volume: 821-Substituted-5-[(3,5-dinitrobenzyl)sulfanyl]-1H-tetrazoles and their isosteric analogs: A new class of selective antitubercular agents active against drug-susceptible and multidrug-resistant mycobacteria.
AID373793fCmax in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 600 mg/day, po2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1070204Antimycobacterial activity against streptomycin, isoniazid, rifampicin, ethambutol and pirazynamide-susceptible Mycobacterium tuberculosis H37Rv ATCC 27294 by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1637724Antitubercular activity against auto-luminescent Mycobacterium tuberculosis H37Ra measured for 5 days by luminescence assay2019MedChemComm, Jan-01, Volume: 10, Issue:1
Design, synthesis, and
AID565791Antimicrobial activity against Neisseria meningitidis harboring rpoB39 D542V mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID706038Induction of drug resistance in methicillin-sensitive Staphylococcus aureus 8325-4 assessed as increase in MIC measured after 8 incubation cycles by stepwise broth microdilution method relative to initial compound MIC2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.
AID1879517Antibacterial activity against rifampicin-resistant Helicobacter pylori CB1614 harboring rpoBL525I/D530N at 1:1 compound to metronidazole molar ratio measured after 5 days in presence of metronidazole by agar dilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID748177Inhibition of rifamycin-resistant Escherichia coli RNA polymerase S531L mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID1058223Antimycobacterial activity against Mycobacterium avium2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID501188Antimicrobial activity against Escherichia coli 442 at 5 ug after 18 hrs by agar diffusion method2009Journal of natural products, Oct, Volume: 72, Issue:10
Norselic acids A-E, highly oxidized anti-infective steroids that deter mesograzer predation, from the Antarctic sponge Crella sp.
AID1426437Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days measured 24 hrs post incubation by resazurin microtiter assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
AID289149Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis CIBIN 650 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID565792Antimicrobial activity against Neisseria meningitidis harboring rpoB44 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID727920Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID495517Antibacterial activity against multidrug-resistant Acinetobacter baumannii BM4675 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID689772Antitubercular activity against Mycobacterium tuberculosis H37Rv incubated for 10 days in anaerobic condition followed by 48 hrs incubation in aerobic condition by LORA assay2012Journal of medicinal chemistry, Jul-12, Volume: 55, Issue:13
Discovery and optimization of benzotriazine di-N-oxides targeting replicating and nonreplicating Mycobacterium tuberculosis.
AID531299Antimicrobial activity against Clostridium difficile isolate 71 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID71055Compound was tested for photoinhibition of Escherichia coli (CIP 548T); Sensitive1998Bioorganic & medicinal chemistry letters, Nov-03, Volume: 8, Issue:21
Nitroglycosylated meso-arylporphyrins as photoinhibitors of gram positive bacteria.
AID1055941Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 16 hrs2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID531006Antimicrobial activity against Clostridium difficile isolate 53 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1202204Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 24 hrs by two-fold broth microdilution method2015European journal of medicinal chemistry, May-05, Volume: 95Novel imidazo[2,1-b]-1,3,4-thiadiazoles as promising antifungal agents against clinical isolate of Cryptococcus neoformans.
AID1234657Antitubercular activity against recombinant Mycobacterium tuberculosis H37Rv expressing Vibrio harveyii luciferase gene with acetamidase promoter assessed as prevention of metabolic recovery incubated for 10 days in anaerobic environment followed by 28 hr2015European journal of medicinal chemistry, Jul-15, Volume: 100Discovery of antitubercular 2,4-diphenyl-1H-imidazoles from chemical library repositioning and rational design.
AID1220079Drug metabolism assessed as human recombinant AADAC-mediated compound hydrolysis expressed in SF21 cells at 50 uM2012Drug metabolism and disposition: the biological fate of chemicals, Jun, Volume: 40, Issue:6
Contributions of arylacetamide deacetylase and carboxylesterase 2 to flutamide hydrolysis in human liver.
AID285202Antimicrobial activity against Escherichia coli M114 mutant with AG100 lon4::IS186 marR::IS2 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID332358Inhibition of DNA synthesis in Bacillus subtilis assessed as [3H]thymidine uptake at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2003Journal of natural products, Feb, Volume: 66, Issue:2
Antibacterial diterpenes from Calceolaria pinifolia.
AID558273Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 3 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID411980Antimicrobial activity against Mycobacterium tuberculosis H37Rv at 6.25 ug/ml by microplate alamar blue assay2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Selective activity against Mycobacteriumtuberculosis of new quinoxaline 1,4-di-N-oxides.
AID474485Lipophilicity, log D of the compound2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Radiosynthesis and bioimaging of the tuberculosis chemotherapeutics isoniazid, rifampicin and pyrazinamide in baboons.
AID565782Antimicrobial activity against Neisseria meningitidis harboring rpoB16 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID530802Antimicrobial activity against Clostridium difficile isolate 33 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID657786Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 164 from Chinese tuberculosis patient measured 24 hrs post dose by microplate alamar blue assay2012European journal of medicinal chemistry, Jun, Volume: 52Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
AID1827048Antibacterial activity against Klebsiella aerogenes ATCC 35029 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID373792Half life in Mycobacterium tuberculosis H37Rv ATCC 2517-infected patient serum at 600 mg/day, po2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID566038Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by serial double dilution technique2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and in vitro antimycobacterial activity of 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives.
AID400947Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2004Journal of natural products, Apr, Volume: 67, Issue:4
Mycobacterium tuberculosis growth inhibition by constituents of Sapium haematospermum.
AID305232Antimicrobial activity against Arr-2 positive Escherichia coli CGSC 5163 lpxC101 mutant bearing pCTV1042007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID535776Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID1417176Antibacterial activity against Escherichia coli ATCC 25922 after 16 to 18 hrs in presence of PMBN by CLSI method2018European journal of medicinal chemistry, Sep-05, Volume: 157Synthesis of 1,2,3-triazole linked 4(3H)-Quinazolinones as potent antibacterial agents against multidrug-resistant Staphylococcus aureus.
AID1775052Antagonist activity at human PXR expressed in HepG2 cells co-expressing luciferase gene under control of CYP3A4 promoter incubated for 24 hrs in presence of 5 uM rifampicin by luciferase reporter assay
AID532971Antimicrobial activity against isoniazid-resistant Mycobacterium tuberculosis isolate 152010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1593371Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID414462Antitubercular activity against streptomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2009Journal of medicinal chemistry, Apr-09, Volume: 52, Issue:7
Structure-activity relationships for a series of quinoline-based compounds active against replicating and nonreplicating Mycobacterium tuberculosis.
AID534422Antibacterial activity against Mycobacterium bovis BCG-japan2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID1827052Antibacterial activity against Shigella sonnei ATCC 25931 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1658973Antibacterial activity against Staphylococcus saprophyticus ATCC 15305 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID356981Inhibition of protein synthesis in Escherichia coli assessed as incorporation of [3H]amino acid at 0.25 ug/mL by LKB Betaplate scintillation counter relative to control2001Journal of natural products, Jul, Volume: 64, Issue:7
Biological and mechanistic activities of xanthorrizol and 4-(1',5'-dimethylhex-4'-enyl)-2-methylphenol isolated from Iostephane heterophylla.
AID553470Cmax in simulated human serum in in vitro hollow-fiber PK model at 600 mg administered every 24 hrs by HPLC2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Pharmacodynamics of minocycline against Staphylococcus aureus in an in vitro pharmacokinetic model.
AID571653Ratio of the MIC for Klebsiella pneumoniae CCUG45421 in the absence of NAB7063 to MIC for Klebsiella pneumoniae CCUG45421 in the presence of 4 ug/ml of NAB70632008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID581670Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth at pH 5.5 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1688445Antibacterial activity against methicillin resistant Staphylococcus aureus ATCC 43300 persisters assessed as reduction in colony formation at 4 ug/ml incubated for 8 hrs by colony counting method2020European journal of medicinal chemistry, Feb-15, Volume: 188Biological evaluation and chemoproteomics reveal potential antibacterial targets of a cajaninstilbene-acid analogue.
AID1603275Antitubercular activity against Mycobacterium tuberculosis H37Ra harboring pTYOK infected in Balb/c mouse assessed as reduction in spleen bacterial burden at 10 mg/kg, po administered once daily via gavage for 5 days measured post last dose by luminometri
AID395780Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID429095Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates from tuberculosis patient assessed as percent specific isolates at 40 ug/ml by absolute-concentration method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations.
AID1762629Antibacterial activity against Escherichia coli ATCC 25922 by CLSI based microplate assay
AID1778129Antimicrobial activity against Pseudomonas aeruginosa assessed as microbial growth inhibition by CLSI-protocol based broth microdilution assay2021Journal of natural products, 04-23, Volume: 84, Issue:4
Opportunities and Limitations for Assigning Relative Configurations of Antibacterial Bislactones using GIAO NMR Shift Calculations.
AID1655160Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth incubated for 7 days by resazurin based assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Improving the Potency of
AID1767892Antitubercular activity against isoniazid,streptomycin,rifampicin,ethambutol,para-aminosalicylate,prothionamide,capreomycin-resistant Mycobacterium tuberculosis clinical isolate 14862 assessed as bacterial growth inhibition incubated for 7 days by MABA as2021European journal of medicinal chemistry, Oct-15, Volume: 222Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis.
AID278577Inhibition of Plasmodium falciparum FCK2 growth as [3H]hypoxanthine uptake after 96 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum.
AID562800Antimicrobial activity against Chlamydia trachomatis F/70/rifR-tetR harboring rpoB gene and tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1691024Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis clinical isolate measured after 1 week by microplate alamar blue assay2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID1854285Antitubercular activity against clinical isolate ethambutol-resistant Mycobacterium tuberculosis ATCC 35837 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID1852779Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth for 5 weeks by spot culture growth inhibition assay2022RSC medicinal chemistry, Nov-16, Volume: 13, Issue:11
Synthesis, biological evaluation and computational studies of pyrazole derivatives as
AID285158Antimicrobial susceptibility of tetracycline-resistant Streptococcus pneumoniae from respiratory tract disease patient assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Clonal diversity and resistance mechanisms in tetracycline-nonsusceptible Streptococcus pneumoniae isolates in Poland.
AID103682In vitro activity of compound against slowly growing Mycobacterium marinum 13911990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1190162Cytotoxicity against human HepG2 cells assessed as reduction in cell viability at 10 uM after 24 hrs by Celltiter-Glo luminescent cell viability assay2015Bioorganic & medicinal chemistry, Feb-01, Volume: 23, Issue:3
IND-2, a pyrimido[1″,2″:1,5]pyrazolo[3,4-b]quinoline derivative, circumvents multi-drug resistance and causes apoptosis in colon cancer cells.
AID543801Bactericidal activity against Klebsiella pneumoniae VT 1367 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID69603Antibacterial activity against Escherichia coli2002Journal of medicinal chemistry, Sep-12, Volume: 45, Issue:19
Inhibition of the antibacterial target UDP-(3-O-acyl)-N-acetylglucosamine deacetylase (LpxC): isoxazoline zinc amidase inhibitors bearing diverse metal binding groups.
AID565776Antimicrobial activity against Neisseria meningitidis harboring rpoB10 H552R mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID373791Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID518015Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent resistant isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro activity of fidaxomicin (OPT-80) tested against contemporary clinical isolates of Staphylococcus spp. and Enterococcus spp.
AID540212Mean residence time in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID603876Antitubercular activity against non-replicating Mycobacterium tuberculosis H37Rv ATCC 27294 incubated 10 days under anaerobic condition measured after 28 hrs of recovery in air by luciferase based low oxygen recovery assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID693671Antibacterial activity against Staphylococcus aureus ATCC 6538 after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID1908121Antibacterial activity against Bacillus subtilis CMCC (B) 63501 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID380455Antibacterial activity against Streptococcus pyogenes ATCC 19615 by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID329347Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in presence of iron rich GAST-D medium2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.
AID1652709Induction of Escherichia coli K12 MG1655 sulA promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID1781721Antibacterial activity against Acinetobacter baumannii BAA 1605 assessed as bacterial growth inhibition incubated for 16 to 18 hrs by broth microdilution method
AID372461Antimalarial activity as 2nd generation ring-stage chloroquine-sensitive Plasmodium falciparum 3D7 after 48 hrs by flow cytometry2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1869568Bactericidal activity against Staphylococcus aureus DSM 20231 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID424420Antibacterial activity against vancomycin-resistant Staphylococcus aureus HIP14300 isolated from patients foot wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID625285Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatic necrosis2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1365723Solubility of compound in Middlebrook 7H9 broth media at pH 6.4 at 200 uM after 90 mins by UV-VIS spectrophotometric method2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID489570Antimycobacterial activity against Mycobacterium tuberculosis CNCTC My 331/88 after 14 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID1391061Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by MABA2018Bioorganic & medicinal chemistry, 05-01, Volume: 26, Issue:8
Synthesis, evaluation and CoMFA/CoMSIA study of nitrofuranyl methyl N-heterocycles as novel antitubercular agents.
AID1767888Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition incubated for 7 days by MABA assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis.
AID1827057Antibacterial activity against Ochrobactrum anthropi ATCC 49687 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID289148Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis CIBIN 687 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID315581Antitubercular activity against Mycobacterium tuberculosis H37Rv by agar dilution method2008Bioorganic & medicinal chemistry letters, Jan-01, Volume: 18, Issue:1
Thiophene containing triarylmethanes as antitubercular agents.
AID1716717Antibacterial activity against Pseudomonas aeruginosa 101243 assessed as fractional inhibitory concentration index in presence of doxycycline incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1491403Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1551811Antibacterial activity against methicillin-resistant Staphylococcus aureus incubated for 18 hrs post 30 mins pre-diffusion by disk diffusion method2019European journal of medicinal chemistry, Jul-01, Volume: 173Antibacterial activity study of 1,2,4-triazole derivatives.
AID1879489Antibacterial activity against Actinomyces naeslundii ATCC 12102022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID428291Antimicrobial activity against Acinetobacter baumannii BM4652 expressing adeABC adeIJK double mutant isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID127814Tested in vitro for killing of Mycobacterium tuberculosis Erdman (ATCC 35801) in monolayers of mouse bone marrow macrophages and 99% reduction was reported using level 3 assay2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials.
AID1447481Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P259-96918 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1215093Activation of rat PXR expressed in human HepG2 cells up to 46 uM after 24 hrs by luciferase reporter gene based luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID279566Antimicrobial activity against Salmonella enterica serovar Typhimurium SMP807 in Caenorhabditis elegans2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Caenorhabditis elegans as a model to determine fitness of antibiotic-resistant Salmonella enterica serovar typhimurium.
AID376994Antimicrobial activity against drug-susceptible Mycobacterium tuberculosis isolate by alamar blue assay2006Journal of natural products, May, Volume: 69, Issue:5
Aegicerin, the first oleanane triterpene with wide-ranging antimycobacterial activity, isolated from Clavija procera.
AID528951Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 7 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID625488Antitubercular activity against Mycobacterium tuberculosis H37Rv after 24 hrs by microplate alamar blue assay2011Bioorganic & medicinal chemistry letters, Nov-15, Volume: 21, Issue:22
Synthesis and in vitro antitubercular evaluation of novel sansanmycin derivatives.
AID1296406Cytotoxicity against MDCK2-MDR1 cells assessed as cell viability at 20 uM after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID530641Inhibition of RNA synthesis in Staphylococcus aureus CB190 assessed as decrease in [5,6-3H]uridine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID571434Antibacterial activity against Escherichia coli ATCC 25992 by Etest method in presence of 4 ug/ml NAB70642008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID574806Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 horboring rpoB S531L/G566R/I569L, katG S315T/R463L, gyrA A90V/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1242344Antimycobacterial activity against 6-((1-(2-(7-chloro-2-oxo-1,8-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA A74V mutant incubated for 7 days2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID543817Bactericidal activity against Klebsiella pneumoniae VT 1367 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1297731Solubility in water at pH 7 by UV-vis spectrophotometric analysis2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID481724Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in GAST medium after 1 week by microplate alamar blue assay2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Structure-activity relationship of new anti-tuberculosis agents derived from oxazoline and oxazole benzyl esters.
AID1891907Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth measured after 7 days by resazurin microtitre assay2022Bioorganic & medicinal chemistry, 06-15, Volume: 64Identification of nitrofuranylchalcone tethered benzoxazole-2-amines as potent inhibitors of drug resistant Mycobacterium tuberculosis demonstrating bactericidal efficacy.
AID1275927Antibacterial activity against Escherichia coli DH5[alpha] assessed as growth inhibition at 200 uM measured every 10 mins for 16 hrs by FLUOstar Optima plate reader analysis relative to control2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
From indole to pyrrole, furan, thiophene and pyridine: Search for novel small molecule inhibitors of bacterial transcription initiation complex formation.
AID560512Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate b6k1642 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1212158Induction of MDR1 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID405165Cmax in tuberculosis patient assessed as desacetylrifampin level at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1706091Antimycobacterial activity against replicating Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth incubated for 7 days by MABA assay
AID588208Literature-mined public compounds from Lowe et al phospholipidosis modelling dataset2010Molecular pharmaceutics, Oct-04, Volume: 7, Issue:5
Predicting phospholipidosis using machine learning.
AID487838Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 48 hrs by green fluorescent protein-based assay2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID1053481Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA M103I mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID1888655Antitubercular activity against multi-drug resistant Mycobacterium tuberculosis 16833 assessed as reduction in bacterial growth incubated for 7 days by Alamar blue assay2022Bioorganic & medicinal chemistry, 01-01, Volume: 53Design, synthesis and biological evaluation of nitrofuran-1,3,4-oxadiazole hybrids as new antitubercular agents.
AID1668182Antibacterial activity against Bacillus subtilis ATCC 6633 assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID558756Antibacterial activity against hetero-Methicillin-resistant and tetracycline-resistant and rifampicin-resistant Staphylococcus aureus deltaIP-rifR harboring RpoB H481Y mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Selection of heterogeneous vancomycin-intermediate Staphylococcus aureus by imipenem.
AID1690489Inhibition of multidrug-resistant Mycobacterium tuberculosis PT2 clinical isolate QcrB assessed as reduction in bacterial growth by resazurin reduction microplate assay2020European journal of medicinal chemistry, Apr-15, Volume: 192Design, synthesis, and evaluation of new 2-(quinoline-4-yloxy)acetamide-based antituberculosis agents.
AID375938Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 after 24 hrs by broth microdilution method2006Journal of natural products, Apr, Volume: 69, Issue:4
Antibacterial, partially acetylated oligorhamnosides from Cleistopholis patens.
AID1516028Antibacterial activity against Pseudomonas aeruginosa 25349 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID678983TP_TRANSPORTER: Western blot, HepG2 cells2002Toxicology, Feb-28, Volume: 171, Issue:2-3
Influence of redox-active compounds and PXR-activators on human MRP1 and MRP2 gene expression.
AID510517Ratio of AUC (0 to 24 hrs) for diabetic tuberculosis patient to AUC (0 to 24 hrs) for tuberculosis patient2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID1603274Antitubercular activity against Mycobacterium tuberculosis H37Ra harboring pTYOK infected in Balb/c mouse assessed as reduction in lung bacterial burden at 10 mg/kg, po administered once daily via gavage for 5 days measured post last dose by luminometric
AID582991Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS08369 harboring MLST sequence type ST18 and pulsotype G expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID680737TP_TRANSPORTER: inhibition of E217betaG uptake (E217betaG: 0.5 uM, Rifampicin: 10 uM) in OATP-C-expressing HeLa cells2003The Journal of pharmacology and experimental therapeutics, Jan, Volume: 304, Issue:1
Human organic anion transporting polypeptide-C (SLC21A6) is a major determinant of rifampin-mediated pregnane X receptor activation.
AID541080Cmax in cage fluid of Albino guiena pig at 12.5 mg/kg, ip after 12 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID285186Antimicrobial activity against nosocomially-acquired methicillin-resistant Staphylococcus aureus by time-kill methodology2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Activity of daptomycin alone and in combination with rifampin and gentamicin against Staphylococcus aureus assessed by time-kill methodology.
AID1601915Antitubercular activity against Mycobacterium tuberculosis H37Rv
AID1467459Antibacterial activity against methicillin resistant Staphylococcus aureus MRSA090 at 50 ug/ml after 24 hrs by agar well diffusion method2017Bioorganic & medicinal chemistry letters, 07-15, Volume: 27, Issue:14
Synthesis, SAR and molecular docking studies of benzo[d]thiazole-hydrazones as potential antibacterial and antifungal agents.
AID424324Antimicrobial activity against Dialister micraerophilus assessed as susceptibility breakpoint by CA-SFM method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID664309Antituberculosis activity against Mycobacterium tuberculosis H37Rv at 6.25 ug/ml by BACTEC MGIT method2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis of benzimidazolyl-1,3,4-oxadiazol-2ylthio-N-phenyl (benzothiazolyl) acetamides as antibacterial, antifungal and antituberculosis agents.
AID1186605Antitubercular activity against Mycobacterium tuberculosis H37Rv strain at 6.25 ug/ml by microplate alamar blue assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Synthesis, biological evaluation and 3D-QSAR study of hydrazide, semicarbazide and thiosemicarbazide derivatives of 4-(adamantan-1-yl)quinoline as anti-tuberculosis agents.
AID1856873Antimicrobial activity against Staphylococcus aureus ATCC 25923 in presence of MgCl22022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1311280Selectivity index, ratio of CC50 for human HCT116 cells to MIC for active stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID575169Inhibition of acrAB AcrAB-TolC-mediated Nile Red efflux in Escherichia coli K-12 3-AG100 overexpressing acrAB AcrAB-TolC assessed as time needed for 50% efflux after energization with 50 mM glucose at 1000 uM by spectrofluorometric assay2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Optimized Nile Red efflux assay of AcrAB-TolC multidrug efflux system shows competition between substrates.
AID1678519Antibacterial activity against Bacillus subtilis DSM3256 incubated overnight by broth dilution method2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID1432973Antitubercular activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis 16892 clinical isolate after 7 days by microplate alamar blue assay
AID1634242Antimycobacterial activity against Mycobacterium abscessus subsp. massiliense assessed as reduction in microbial growth by CLSI method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID557209Antibacterial activity against Beta-lactamase-negative Neisseria meningitidis assessed as percent susceptible isolates by Etest method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antibiotic susceptibility and characteristics of Neisseria meningitidis isolates from the African meningitis belt, 2000 to 2006: phenotypic and genotypic perspectives.
AID1294370Cytotoxicity against mouse J774 cells assessed as cell viability at 10 times lower MIC by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID531048Antimicrobial activity against Clostridium difficile isolate 15 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1601919Antitubercular activity against multidrug resistant Mycobacterium tuberculosis isolate 2
AID511012Half life in New Zealand rabbit meningitis model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID528950Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 6 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1264464Antimycobacterial activity against non-replicating streptomycin starved Mycobacterium tuberculosis 18b after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID1858571Antibacterial activity against Mycobacterium tuberculosis H37Rv expressing GFP infected in mouse Raw264.7 cells incubated for 5 days by SYTO 60 staining method2021European journal of medicinal chemistry, Jan-01, Volume: 209Lipolytic enzymes inhibitors: A new way for antibacterial drugs discovery.
AID1372630Cytotoxicity against mouse RAW264.7 cells assessed as growth inhibition at 25 uM after 48 hrs by MTT assay relative to control2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID416845Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as incidence of bacterial infection at 10 mg/kg, po administered for 5 days per week measured after 8 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1716774Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as reduction in bacterial growth by measuring doxycycline MIC at 16 ug/ml incubated for 18 hrs in presence of doxycycline by broth microdilution assay (Rvb = 1024 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID626868Antimicrobial activity against non-replicating Mycobacterium tuberculosis after 11 days by luminescence based low oxygen recovery assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID1473738Inhibition of human BSEP overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-taurocholate in presence of ATP measured after 15 to 20 mins by membrane vesicle transport assay2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID530653Inhibition of RNA synthesis in rifamycin-resistant Staphylococcus aureus CB370 harboring rpoB H481Y mutant gene assessed as [5,6-3H]uridine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID294761Antibacterial activity against Staphylococcus aureus after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID373049Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate JN45 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1593374Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in multidrug-resistant Mycobacterium tuberculosis V2475 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1416247Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis clinical isolate2017MedChemComm, Jun-01, Volume: 8, Issue:6
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant
AID1174106Antimycobacterial activity against isoniazid, rifampin, ethambutol, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID774409Antibacterial activity against Escherichia coli DH5[alpha] assessed as growth inhibition after 6 hrs2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Antimycobacterial labdane diterpenes from Leucas stelligera.
AID292413Antitubercular activity against Mycobacterium tuberculosis SS32007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID373975AUC in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 7 mg/L for 2 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID202120Minimum inhibitory concentration of compound against Streptococcus pyogenus septicemia in the mouse1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID534424Antibacterial activity against Mycobacterium bovis BCG-Pasteur2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID1443992Total Cmax in human administered as single dose2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID1333275Antimycobacterial activity against Mycobacterium smegmatis MC2 155 assessed as inhibition of respiratory ATP synthesis by measuring ATP level at 4 times MIC measured after 6 hrs by luciferase reporter gene assay (Rvb = 152%)2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1167352Antibacterial activity against wild type Escherichia coli D21 after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID434066Immunomodulatory effect in human A549 cells assessed as reduction in basal release of [3H]arachidonic acid at 50 ug/ml up to 2 hrs by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1879562Antibacterial activity against Gardnerella vaginalis ATCC 491452022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID372544Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 24-36 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID292295Antibacterial activity Listeria monocytogenes ATCC 15313 after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID425608Cytotoxicity against mouse J774A1 cells assessed as macrophage number at 10.5 ug/ml after 3 hrs by total cell protein assay2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID438476Cytotoxicity against african green monkey Vero cells after 72 hrs2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters.
AID497973Drug level in bone/joint infection patient serum assessed as median concentration at 2400 mg, iv after 40 days in presence of rifampin2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Continuous clindamycin infusion, an innovative approach to treating bone and joint infections.
AID1778127Antimicrobial activity against Staphylococcus aureus assessed as microbial growth inhibition by CLSI-protocol based broth microdilution assay2021Journal of natural products, 04-23, Volume: 84, Issue:4
Opportunities and Limitations for Assigning Relative Configurations of Antibacterial Bislactones using GIAO NMR Shift Calculations.
AID1220555Fraction unbound in Sprague-Dawley rat brain homogenates at 1 uM after 6 hrs by equilibrium dialysis method2011Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 39, Issue:7
Species independence in brain tissue binding using brain homogenates.
AID1423474Antibacterial activity against Enterococcus faecium ATCC 19434 after 24 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1079931Moderate liver toxicity, defined via clinical-chemistry results: ALT or AST serum activity 6 times the normal upper limit (N) or alkaline phosphatase serum activity of 1.7 N. Value is number of references indexed. [column 'BIOL' in source]
AID562797Antimicrobial activity against Chlamydia trachomatis L2/tetR1 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID626873Antimicrobial activity against Escherichia coli EC2880 mutant after 16 to 20 hrs2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID369917Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected Swiss mouse assessed as reduction of bacterial count in spleen at 10 mg/kg after 12 days infection weekly 5 times for 1 month2005Science (New York, N.Y.), Jan-14, Volume: 307, Issue:5707
A diarylquinoline drug active on the ATP synthase of Mycobacterium tuberculosis.
AID1193868Anti-tubercular activity against Mycobacterium smegmatis str. MC2 1552015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis, in vitro anticancer and antimycobacterial evaluation of new 5-(2,5-dimethoxyphenyl)-1,3,4-thiadiazole-2-amino derivatives.
AID611490Antibacterial activity against scottish methicillin-resistant Staphylococcus aureus isolate 161 (PF161) isolated from patient thigh abscess after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID285562Bactericidal activity against 26-day old non-replicating Mycobacterium tuberculosis H37Rv in anaerobic condition at 1 ug/ml after 4 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID425604Antibacterial activity against gentamicin-treated internalized Escherichia coli isolate HM615 in mouse J774A1 cells isolated from colonic mucosal biopsies of patient with Crohn's disease assessed as intracellular killing of bacteria at 10% compound Cmax a2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1152778Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis harboring DNA gyraseA G88N mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1272621Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 14 days by broth microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.
AID1892313Antibacterial activity against Enterococcus faecalis incubated for 16 to 24 hrs in presence of ampicillin by broth microdilution based spectrophotometric analysis2022Journal of natural products, 06-24, Volume: 85, Issue:6
Glenthmycins A-M: Macrocyclic Spirotetronate Polyketide Antibacterials from the Australian Pasture Plant-Derived
AID544828Antimicrobial activity against Staphylococcus epidermidis Xen 43 biofilm assessed as log10 CFU/cm'2 in bacterial count2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID1491291Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 treated for 10 days under hypoxic condition followed by 28 hrs of normoxic recovery2017European journal of medicinal chemistry, Sep-08, Volume: 137QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity.
AID333070Antimalarial activity against Plasmodium falciparum D62004Journal of natural products, Aug, Volume: 67, Issue:8
Three new manzamine alkaloids from a common Indonesian sponge and their activity against infectious and tropical parasitic diseases.
AID1664584Antitubercular activity against Mycobacterium bovis BCG assessed as bacterial growth inhibition at 1 ug/ml by MABA relative to control2020Bioorganic & medicinal chemistry letters, 08-15, Volume: 30, Issue:16
The synthesis and antituberculosis activity of 5-alkynyl uracil derivatives.
AID425402Antibacterial activity Escherichia coli isolate HM413 isolated from ileo-colonic mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID572553AUC (0 to 24 hrs) in indonesian pulmonary tuberculosis patient at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID325003Antibacterial activity against rifampin and cefdinir-resistant Haemophilus influenzae RdRIF/MSC06663 mutant by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID352092Antimicrobial activity against multidrug-resistant Escherichia coli after 24 hrs2009European journal of medicinal chemistry, Feb, Volume: 44, Issue:2
Synthesis, biological evaluation and 2D-QSAR analysis of benzoxazoles as antimicrobial agents.
AID1262577Antimicrobial activity against clinical isolates of Mycobacterium tuberculosis SAWC 3933 LCC under 7H9 medium assessed as growth inhibition after 14 days by alamar blue assay2015Journal of medicinal chemistry, Dec-10, Volume: 58, Issue:23
Pyrrolo[3,4-c]pyridine-1,3(2H)-diones: A Novel Antimycobacterial Class Targeting Mycobacterial Respiration.
AID1542195Antimycobacterial activity against Mycobacterium tuberculosis MDR-TB incubated for 12 to 28 days by agar dilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Pyridine and nitro-phenyl linked 1,3,4-thiadiazoles as MDR-TB inhibitors.
AID276752Antimycobacterial activity against rifampicin and rifabutin resistant Mycobacterium tuberculosis ATCC 358382006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID515080Antimycobacterial activity against Mycobacterium tuberculosis H37Ra after 24 hrs by microtiter alamar blue assay2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Isoxazole analogs of curcuminoids with highly potent multidrug-resistant antimycobacterial activity.
AID530865Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB D471Y mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1497864Antibacterial activity against Pseudomonas aeruginosa ATCC 278532018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID611483Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID285159Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID563693Antibacterial activity against Mycobacterium tuberculosis H37Ra by by 7H10 agar plate method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID1181157Antimicrobial activity against clinical isolate Mycobacterium tuberculosis Beijing assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1573723Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2019Bioorganic & medicinal chemistry letters, 01-15, Volume: 29, Issue:2
Synthesis and biological evaluation of 1H-pyrrolo[2,3-d]pyrimidine-1,2,3-triazole derivatives as novel anti-tubercular agents.
AID1901691Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured by MABA assay2022European journal of medicinal chemistry, Mar-05, Volume: 231Identification of thiophene-benzenesulfonamide derivatives for the treatment of multidrug-resistant tuberculosis.
AID626924Antimycobacterial activity against Mycobacterium fortuitum ATCC 19542 using compound level ranging from 0.3125 to 5 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID440893Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
L-proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines.
AID1626604Antimicrobial activity against wild type Staphylococcus aureus2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1879497Antibacterial activity against Helicobacter pylori ATCC 7003922022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID144015In vitro anti-mycobacterial activity expressed as minimum inhibitory concentration against Mycobacterium fortuitum ATCC 68412001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Some 3-thioxo/alkylthio-1,2,4-triazoles with a substituted thiourea moiety as possible antimycobacterials.
AID1449138Cytotoxicity against African green monkey Vero cells2017Journal of medicinal chemistry, 07-13, Volume: 60, Issue:13
Targeting Mycolic Acid Transport by Indole-2-carboxamides for the Treatment of Mycobacterium abscessus Infections.
AID1334256Selectivity index, ratio of GI50 for human MCF7 cells to MIC90 for Mycobacterium bovis BCG ATCC 35743 active stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1915885Antibacterial activity against Mycobacterium tuberculosis mc2 6206 harboring mLux plasmid infected in mouse J774.A1 cells assessed as inhibition of bacterial cell viability incubated for 72 hrs by multimode microplate reader analysis
AID1294360Antimicrobial activity against ofloxacin resistant Mycobacterium tuberculosis SRI 4000 after 7 days2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID1772308Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.1 cells assessed as reduction in bacterial colony forming units at 5 ug/ml incubated for 3 days (Rvb = 5.52 +/- 0.18 log10CFU)
AID1055957Antimycobacterial activity against kanamycin-resistant Mycobacterium tuberculosis ATCC 35827 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1061106Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in african green monkey Vero cells2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID1070201Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv ATCC 35822 by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1058229Antibacterial activity against Bacillus cereus by CLSI method2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID1471027Growth inhibition of Mycobacterium tuberculosis H37Ra ATCC 25177 at 3 ug/ml by XTT dye based two-fold dilution method relative to control2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID677624Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2012Bioorganic & medicinal chemistry letters, Sep-01, Volume: 22, Issue:17
Structural requirements for the antitubercular quaternized triflupromazine pharmacophore.
AID1653390Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.2 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID278581Reduction in Plasmodium falciparum FCK2 in human blood cell culture after 96 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Inhibitors of nonhousekeeping functions of the apicoplast defy delayed death in Plasmodium falciparum.
AID1335283Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in BL21(DE3)pLysS cells assessed as inhibition of DNA supercoiling activity in presence of ATP measured after 30 mins by malachite green dye based assay2016European journal of medicinal chemistry, Nov-29, Volume: 124Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
AID1626621Antimicrobial activity against Staphylococcus aureus isogenic forms expressing rpoB H481Y/gyrA S84L/parC S80F mutant2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID760170Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing pCHERRY3 after 4 days by plate format assay2013ACS medicinal chemistry letters, Jul-11, Volume: 4, Issue:7
Advancement of Imidazo[1,2-
AID1174926Antitubercular activity against Mycobacterium tuberculosis isolate 778/10 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID1474040Ratio of drug concentration at steady state in human at 150 to 600 mg, iv QD after 24 hrs to IC50 for human MRP2 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1585120Antimicrobial activity against multi drug-resistant Mycobacterium tuberculosis 12611 after 7 days by MABA2018European journal of medicinal chemistry, Dec-05, Volume: 160Identification of novel benzothiopyranone compounds against Mycobacterium tuberculosis through scaffold morphing from benzothiazinones.
AID1597869Selectivity index, ratio of IC50 for mouse J774.A1 cells to MIC for Mycobacterium tuberculosis INH R1 ATCC 35822
AID1069166Antimicrobial activity against ofloxacin-resistant Mycobacterium tuberculosis H37Rv SRI 4000 assessed as growth inhibition at MIC after 7 days by broth microdilution assay relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1192374Antimicrobial activity against Pseudomonas aeruginosa MTCC 1034 after 18 hrs by broth micro dilution method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.
AID283155Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL856 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1401979Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv ATCC 35828 RIF-R22018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID279816Antimicrobial activity against Escherichia coli DH5alpha by agar dilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Plasmid-mediated KPC-2 in a Klebsiella pneumoniae isolate from China.
AID1071093Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis H37Rv SRI 4000 at MIC after 7 days by broth microdilution assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID425398Antibacterial activity against Escherichia coli isolate HM154 isolated from colonic mucosal biopsies of patient with Crohn's disease after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID501189Antimicrobial activity against Escherichia coli 389 at 5 ug after 18 hrs by agar diffusion method2009Journal of natural products, Oct, Volume: 72, Issue:10
Norselic acids A-E, highly oxidized anti-infective steroids that deter mesograzer predation, from the Antarctic sponge Crella sp.
AID571394Antibacterial activity against Acinetobacter baumannii ATCC 19606 by Etest method in presence of 0.5 ug/ml NAB7392008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1331132Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 28 days by MABA method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Design, development of new synthetic methodology, and biological evaluation of substituted quinolines as new anti-tubercular leads.
AID1327574Activation of PXR/LXR in human LS180 cells assessed as induction of P-gp by measuring intracellular accumulation of Rhodamine-123 at 10 uM preincubated for 48 hrs followed by 40 mins incubation with HANKS buffer and subsequent addition of Rhodamine-123 me2016European journal of medicinal chemistry, Oct-21, Volume: 122Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs.
AID103650In vitro activity compound against rapidly growing Mycobacterium fortuitum 13021990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID693673Antibacterial activity against Staphylococcus aureus isolate 708 obtained from veterinary sample after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID373945Ratio of AUC (0 to 168 hrs) to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model administered at simulated dose of 600 mg/day for 7 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID511000Ratio of Cmax to MIC for Acinetobacter baumannii 1327 in pharmacokinetic-pharmacodynamic C57BL/6 mouse pneumonia model at 25 mg/kg, ip2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1705642Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth incubated by measuring turbidity for 5 days by serial microdilution based colorimetric assay2020European journal of medicinal chemistry, Dec-15, Volume: 208New one-pot synthesis of anti-tuberculosis compounds inspired on isoniazid.
AID1298605Antibacterial activity against Bacillus licheniformis after 24 hrs by agar diffusion assay2016Bioorganic & medicinal chemistry letters, 06-15, Volume: 26, Issue:12
Synthesis of novel triazole/isoxazole functionalized 7-(trifluoromethyl)pyrido[2,3-d]pyrimidine derivatives as promising anticancer and antibacterial agents.
AID530625Inhibition of Staphylococcus aureus RpoB H481Y mutant2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1129649Antimycobacterial activity against Mycobacterium tuberculosis H37Rv expressing luciferase assessed as growth inhibition after 6 days by luminometry2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
1,2,3,4,8,9,10,11-octahydrobenzo[j]phenanthridine-7,12-diones as new leads against Mycobacterium tuberculosis.
AID530541Induction of PvraSr::lacZ gene expression in Staphylococcus aureus SH1000 at 0.05 ug/ml after 2 hrs by beta-galactosidase reporter gene assay relative to untreated control2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Staphylococcus aureus cell wall stress stimulon gene-lacZ fusion strains: potential for use in screening for cell wall-active antimicrobials.
AID577489Half life in Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model at 600 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID509681Antitubercular activity against Mycobacterium tuberculosis ATCC 35801 infected in CD1 mouse spleen at 25 mg/kg, iv after 6 weeks2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs.
AID1355395Disruption of cell membrane potential in Mycobacterium bovis BCG ATCC 35734 at 0.08 uM after 20 mins to 5 days by DiOC2 dye-based fluorescence assay2018Journal of medicinal chemistry, 07-12, Volume: 61, Issue:13
Indolyl Azaspiroketal Mannich Bases Are Potent Antimycobacterial Agents with Selective Membrane Permeabilizing Effects and in Vivo Activity.
AID645537Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID531002Antimicrobial activity against Clostridium difficile isolate 49 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1879560Antibacterial activity against Fusobacterium nucleatum ATCC 255862022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID457436Antitubercular activity against Mycobacterium tuberculosis H37Rv at pH 6.8 by microplate alamar blue assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID565778Antimicrobial activity against Neisseria meningitidis harboring rpoB12 H552L mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID372470Antimalarial activity as trophozoite arrest after 24 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 96 hrs post infection2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID560502Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gz06051 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID378285Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by BACTEC 460 radiorespirometric assay2000Journal of natural products, Dec, Volume: 63, Issue:12
Oleanane triterpenes from Junellia tridens.
AID571416Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 16 ug/ml NAB7061 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1463962Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 8666/2010 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID560976Antimicrobial activity against glycopeptide-intermediate Staphylococcus aureus NJ992 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Activity of telavancin against Staphylococcus aureus strains with various vancomycin susceptibilities in an in vitro pharmacokinetic/pharmacodynamic model with simulated endocardial vegetations.
AID405166Tmax in tuberculosis patient assessed as desacetylrifampin level at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1654165Binding affinity to recombinant full length Mycobacterium tuberculosis H37Rv ClpC1 (1 to 842 residues) expressed in Escherichia coli BL21 cells by surface plasmon resonance analysis2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID294760Antibacterial activity against Mycobacterium avium 724S after 2 weeks by broth dilution method2007Bioorganic & medicinal chemistry letters, May-01, Volume: 17, Issue:9
Synthesis of new sugar derivatives from Stachys sieboldi Miq and antibacterial evaluation against Mycobacterium tuberculosis, Mycobacterium avium, and Staphylococcus aureus.
AID1427044Antitubercular activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 after 8 days by XTT reduction menadione assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID571193Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 by Etest method by Etest in presence of 0.25 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1069159Cytotoxicity against mouse J774 cells assessed as cell viability at 10-fold below MIC relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID509615Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB531 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID555319Antibacterial activity against methicillin-susceptible, vancomycin-intermediate Staphylococcus aureus 505 after 9 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID532970Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 142010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID780283Antitubercular activity against Mycobacterium tuberculosis H37Rv by MABA assay2013Bioorganic & medicinal chemistry letters, Nov-15, Volume: 23, Issue:22
Inhibitory effect of oxygenated cholestan-3β-ol derivatives on the growth of Mycobacterium tuberculosis.
AID1174107Antimycobacterial activity against isoniazid, rifampin, streptomycin, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1909950Antibacterial activity against wild type Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 11 days2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1423471Antibacterial activity against Staphylococcus aureus ATCC 25923 after 6 to 8 hrs by bacterial proliferation assay2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID1584703Antimicrobial activity against Klebsiella pneumoniae ATCC 43816 after 20 hrs by CLSI protocol-based microdilution assay2018Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20
Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline.
AID438474Antitubercular activity against Mycobacterium tuberculosis H37Rv at pH 6.8 by Alamar blue susceptibility assay2009Journal of medicinal chemistry, Nov-26, Volume: 52, Issue:22
From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters.
AID1730993Antitubercular activity against isoniazid/rifampin resistance Mycobacterium tuberculosis KZN494 by MABA assay2021European journal of medicinal chemistry, Mar-05, Volume: 213Design and synthesis of mycobacterial pks13 inhibitors: Conformationally rigid tetracyclic molecules.
AID1827058Antibacterial activity against Bacillus subtilis ATCC 6051 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1909952Selectivity ratio of MIC50 for wild type Mycobacterium tuberculosis H37Rv to MIC50 for Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID611484Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID1459059Antitubercular activity against isoniazid resistant Mycobacterium tuberculosis ATCC 35822 after 5 days2017European journal of medicinal chemistry, Jan-05, Volume: 125Pyrazolo[1,5-a]pyridine-3-carboxamide hybrids: Design, synthesis and evaluation of anti-tubercular activity.
AID1716864Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1242341Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microdilution method2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID531290Antimicrobial activity against Clostridium difficile isolate 62 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID765510Cytotoxicity against HEK293 cells after 24 hrs2013Journal of medicinal chemistry, Aug-08, Volume: 56, Issue:15
Cushing's syndrome: development of highly potent and selective CYP11B1 inhibitors of the (pyridylmethyl)pyridine type.
AID1517151Cytotoxicity against CHO cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
AID373958Ratio of Cmax to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 14 mg/L administered for 0.5 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1562246Antimycobacterial activity against Mycobacterium smegmatis atR10 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID603879Antitubercular activity against replicating Mycobacterium tuberculosis H37Rv ATCC 27294 after 1 week by microplate alamar blue assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID520084Antimicrobial activity against Escherichia coli TG1 harboring plasmid pEX19Gm by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID531024Antimicrobial activity against Clostridium difficile isolate 71 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID405152Apparent volume of distribution in tuberculosis patient at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID572545AUC (0 to 12 hrs) in kenyan pulmonary tuberculosis patient with body weight <=45 kg at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID572549AUC (0 to infinity) in indian pulmonary tuberculosis patient coinjected with HIV at 450 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1782929Selectivity index, ratio of CC50 for human HepG2 cells to MIC for antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 272942021European journal of medicinal chemistry, Aug-05, Volume: 220Synthesis of alkynylated 1,2,4-oxadiazole/1,2,3-1H-triazole glycoconjugates: Discovering new compounds for use in chemotherapy against lung carcinoma and Mycobacterium tuberculosis.
AID405153Half life in tuberculosis patient at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1058225Antimycobacterial activity against Mycobacterium chelonae2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID373024Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PU4A1 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID103656In vitro activity of compound against rapidly growing Mycobacterium fortuitum 6451990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1653479Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 by broth microdilution assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1334263Selectivity index, ratio of GI50 for human THP1 cells to MIC90 for Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1400055Antibacterial activity against Acinetobacter baumannii ATCC 19606 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID509620Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB511 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID532962Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 62010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1868119Anti-tubercular activity against Mycobacterium tuberculosis CF161 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID555314Antibacterial activity against methicillin-susceptible Staphylococcus aureus ATCC 29213 after 9 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID434059Cytotoxicity against human A549 cells assessed as cell viability by neutral red uptake assay2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID434068Effect on IL-1-beta-induced cPLA2 phosphorylation in human A549 cells at 50 ug/ml up to 15 mins by Western blot analysis2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID543806Bactericidal activity against Acinetobacter baumannii VT 126 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1602929Cytotoxicity against mouse J774A.1 cells after 24 hrs by resazurin dye-based fluorescence assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID283164Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2640 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID509629Antibacterial activity against Mycobacterium tuberculosis containing phenotypic embB306 mutation assessed as microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID1589010Anti-mycobacterial activity against Mycobacterium tuberculosis H37Rv
AID1253866Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis FJ05120 after 3 to 4 weeks by microplate alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Discovery of the disubstituted oxazole analogues as a novel class anti-tuberculotic agents against MDR- and XDR-MTB.
AID1179474Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in glycerol-alanine-salts medium after 7 days by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID283158Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2492 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID392606Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID405168Half life in tuberculosis patient assessed as desacetylrifampin level at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID545601Bactericidal activity against stationary-phase vancomycin-resistant Staphylococcus aureus ATCC 33591 grown on nutrient-depleted CAMHB medium at 2 ug/ml after 24 hrs by time kill analysis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID560499Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 5zjsau3 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1205460Antitubercular activity against rifampin and isoniazid-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID1497858Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID665278Antitubercular activity against isoniazid, rifampicin and ethambutol-resistant Mycobacterium tuberculosis clinical isolate after 28 days by agar dilution method2012European journal of medicinal chemistry, Jul, Volume: 53A solvent free, four-component synthesis and 1,3-dipolar cycloaddition of 4(H)-pyrans with nitrile oxides: synthesis and discovery of antimycobacterial activity of enantiomerically pure 1,2,4-oxadiazoles.
AID445929Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar blue assay2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents.
AID1463959Antimycobacterial activity MDR/XDR against Mycobacterium tuberculosis isolate 9449/2007 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID419827Antibacterial activity against Staphylococcus aureus MTCC 96 at 1000 ug/ml after 24 hrs by agar diffusion method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID559916Ratio of AUC (0 to 24 hrs) to MIC in plasma of patient with Mycobacterium tuberculosis infection at 600 to 1200 mg/kg, po administered as single dose2009Antimicrobial agents and chemotherapy, Jul, Volume: 53, Issue:7
Population modeling and Monte Carlo simulation study of the pharmacokinetics and antituberculosis pharmacodynamics of rifampin in lungs.
AID1296408Cytotoxicity against primary human hepatocytes assessed as cell viability at 20 uM after 48 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1154353Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis clone 4.1 over expressing DprE1 mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID510524Half life in tuberculosis patient at 10 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1556638Antimycobacterial activity against multidrug resistance Mycobacterium tuberculosis 16883 clinical isolate assessed as reduction in bacterial cell viability incubated for 7 days by microplate alamar blue assay2019European journal of medicinal chemistry, Oct-01, Volume: 179hERG optimizations of IMB1603, discovery of alternative benzothiazinones as new antitubercular agents.
AID520087Antimicrobial activity against acrAB-deficient Escherichia coli TG1 harboring AheABC efflux pump by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID605759Binding affinity to human SXR transfected in human HepG2 cells coexpressing GAL4 assessed as transcriptional activation at 5 X 10'-6 M after 48 hrs by luciferase reporter gene assay2011Journal of medicinal chemistry, Jun-23, Volume: 54, Issue:12
Synthesis of novel vitamin K2 analogues with modification at the ω-terminal position and their biological evaluation as potent steroid and xenobiotic receptor (SXR) agonists.
AID619448Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis H37Rv after 28 days by agar dilution method2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Synthesis of 3-heteroarylthioquinoline derivatives and their in vitro antituberculosis and cytotoxicity studies.
AID1905612Antimicrobial activity against rifampicin-resistant Staphylococcus aureus ATCC 259232022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID1063299Antitubercular activity against capreomycin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 16 to 24 hrs by microplate-Alamar Blue assay2014European journal of medicinal chemistry, Jan-24, Volume: 72Design, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents.
AID1908118Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC BAA-1720 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID502971Antimicrobial activity against Mycobacterium smegmatis ATCC 607 by alamar blue assay2007Nature chemical biology, Jun, Volume: 3, Issue:6
Diarylquinolines target subunit c of mycobacterial ATP synthase.
AID1653518Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as ATP level per 10'7 cells at 0.4 mg/L measured by bioluminescence assay (Rvb = 425 +/- 64 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID572538Absorption rate constant in pulmonary tuberculosis patient in Sequential 0 order and first order model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1460596Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by tetrazolium dye assay2017Bioorganic & medicinal chemistry, 11-15, Volume: 25, Issue:22
Anti-tuberculosis activity and structure-activity relationships of oxygenated tricyclic carbazole alkaloids and synthetic derivatives.
AID479643Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis H37Rv at 2 ug/ml by radiometric BACTEC assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis.
AID1577331Antimycobacterial activity against XDR Mycobacterium tuberculosis Praha 131 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID373976AUC in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 2 mg/L for 7 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1542208Antimicrobial activity against MLSB-resistant Staphylococcus aureus incubated for 18 hrs by serial microdilution method2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID1769967Antibacterial activity against methicillin resistant Staphylococcus aureus ATCC 43300 persisters assessed as reduction in colony formation at 40 ug/ml incubated for 8 hrs by colony counting method2021European journal of medicinal chemistry, Nov-15, Volume: 224Synthetic cajaninstilbene acid derivatives eradicate methicillin-resistant Staphylococcus aureus persisters and biofilms.
AID425601Antibacterial activity against gentamicin-treated internalized Escherichia coli isolate HM605 in mouse J774A1 cells isolated from colonic mucosal biopsies of patient with Crohn's disease assessed as intracellular killing of bacteria at 10% compound Cmax a2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID532958Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 22010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID774298Antimycobacterial activity against rifampin-resistant Mycobacterium tuberculosis ATCC 358382013Journal of natural products, Oct-25, Volume: 76, Issue:10
Chlorinated coumarins from the polypore mushroom Fomitopsis officinalis and their activity against Mycobacterium tuberculosis.
AID1716659Antibacterial activity against Klebsiella pneumoniae ATCC 13883 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID406615Antibacterial activity against Staphylococcus aureus ATCC 29213 infected albino guinea pig tissue-cage infection model assessed as bacterial count at 12.5 mg/kg, ip administered every 12 hrs after 5 days2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID580616Inhibition of DNA synthesis in Bacillus subtilis BD54 at 5 X MIC by [3H]thymidine incorporation assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Novel broad-spectrum bis-(imidazolinylindole) derivatives with potent antibacterial activities against antibiotic-resistant strains.
AID487844Antibacterial activity against Staphylococcus aureus ATCC 29213 after 18 to 24 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID1212150Induction of CYP2A6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1400039Bactericidal activity against Staphylococcus aureus ATCC 25923 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1400065Bactericidal activity against non-replicating Mycobacterium tuberculosis CDC1551 expressing tdTomato infected in mouse J774A.1 cells at 2 times MIC after 48 hrs by UV-Visible spectroscopic method2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID292303Antimycobacterial activity against Mycobacterium bovis BCG at 0.5 to 1 ug/mL by microplate Alamar blue assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID425405Antibacterial activity against mucosa-associated Escherichia coli isolate HM428 isolated from patient with irritable bowel syndrome or sporadic polyps after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1765575Antibacterial activity against Enterococcus faecalis ATCC 29212 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID534419Antibacterial activity against Mycobacterium bovis BCG-Connaught2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Susceptibility of Mycobacterium bovis BCG vaccine strains to antituberculous antibiotics.
AID1856871Antimicrobial activity against Staphylococcus aureus ATCC 25923 in presence of NaCl2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID268914Antibacterial activity against intramacrophagic Mycobacterium tuberculosis2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID529187Antibacterial activity against Klebsiella pneumoniae K830 with arr-5 gene by Etest method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Detection of new arr-4 and arr-5 gene cassettes in clinical Pseudomonas aeruginosa and Klebsiella pneumoniae strains from Brazil.
AID283218Antimicrobial susceptibility of Burkholderia cepacia complex isolated from cystic fibrosis patient assessed as percent susceptible isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Antimicrobial susceptibility and synergy studies of Burkholderia cepacia complex isolated from patients with cystic fibrosis.
AID1237430Antimycobacterial activity against Mycobacterium smegmatis str. MC2 155 incubated for 30 hrs by turbidometric assay2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and evaluation of novel fluorinated pyrazolo-1,2,3-triazole hybrids as antimycobacterial agents.
AID580844AUC in healthy human at 10 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1311282Selectivity index, ratio of CC50 for human THP1 cells to MIC for dormant stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1416246Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by microplate alamar blue assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant
AID405155Cmax in human tuberculosis patient at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1563897Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days in presence of middlebrook 7H9/CAS medium by broth microdilution method2019European journal of medicinal chemistry, Oct-15, Volume: 180Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights.
AID1736277Antitubercular activity at Mycobacterium tuberculosis H37Rv in nutrition starved condition medium assessed as log reduction of cell growth at 10 ug/ml measured after 7 days by MPN method2020European journal of medicinal chemistry, Feb-15, Volume: 188Discovery of hydrazone containing thiadiazoles as Mycobacterium tuberculosis growth and enoyl acyl carrier protein reductase (InhA) inhibitors.
AID1183298Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Design, synthesis and anti-mycobacterial activity of 1,2,3,5-tetrasubstituted pyrrolyl-N-acetic acid derivatives.
AID1311242Antibacterial activity against Enterococcus faecalis 14-52016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID1908166Induction of drug resistance against Staphylococcus aureus ATCC 29213 assessed as fold increase in MIC after 16 passage2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID1212157Induction of UGT2B7 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1562248Antimycobacterial activity against Mycobacterium smegmatis atR1 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID285916Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 292132007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antimicrobial activities of daptomycin, vancomycin, and oxacillin in human monocytes and of daptomycin in combination with gentamicin and/or rifampin in human monocytes and in broth against Staphylococcus aureus.
AID694202Antifungal activity against Candida albicans ATCC 90027 after 48 hrs by broth microdilution method2012Bioorganic & medicinal chemistry letters, Nov-15, Volume: 22, Issue:22
Design and synthesis of 1H-1,2,3-triazoles derived from econazole as antitubercular agents.
AID1174108Antimycobacterial activity against isoniazid, rifampin, ethambutol, ofloxacin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1167361Antibacterial activity against wild type Enterococcus faecalis ATCC 29212 after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1854287Antitubercular activity against clinical isolate rifampicin-resistant Mycobacterium tuberculosis ATCC 35838 assessed as inhibition of bacterial growth incubated for 7 days by Presto blue resazurin microtiter plate assay2022RSC medicinal chemistry, May-25, Volume: 13, Issue:5
Synthesis and evaluation of triazole congeners of nitro-benzothiazinones potentially active against drug resistant
AID530993Antimicrobial activity against Clostridium difficile isolate 40 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1601916Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID489571Antimycobacterial activity against Mycobacterium tuberculosis CNCTC My 331/88 after 21 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID1403707Antibiofilm activity against Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial load at 10 ug/ml incubated for 1 week by MPN assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID285201Antimicrobial activity against Escherichia coli M104 mutant with AG100 dupIS3 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID1765765Antimycobacterial activity against Mycobacterium tuberculosis H37Ra assessed as inhibition of bacterial growth measured by microplate alamar blue assay2021Bioorganic & medicinal chemistry letters, 09-15, Volume: 48Design and synthesis of novel 5-alkynyl pyrimidine nucleosides derivatives: Influence of C-6-substituent on antituberculosis activity.
AID582988Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS07261 harboring MLST sequence type ST78 and pulsotype D expressing vanM gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID406611Cmin in albino guinea pig cage fluid at 12.5 mg/kg, ip administered every 12 hrs for 4 days2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID1879533Antibacterial activity against Atopobium vaginae BAA-552022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID301526Antibacterial activity against rifamycin-sensitive Staphylococcus aureus CB190 ATCC 292132007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
AID424423Antibacterial activity against Enterococcus faecalis HIP15179 coisolated with vancomycin-resistant Staphylococcus aureus by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID1287511Selectivity index, ratio of GI50 for human PANC1 cells to MIC for active state Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID1351230Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 25618 after 7 days by resazurin dye based assay2018European journal of medicinal chemistry, Mar-25, Volume: 148Broad activity of diphenyleneiodonium analogues against Mycobacterium tuberculosis, malaria parasites and bacterial pathogens.
AID529534Antimycobacterial activity against isoniazid, rifampin, ethambutol resistant Mycobacterium tuberculosis isolate NJT5310 expressing embB codon 306 ATG mutant at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID411979Antimicrobial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2009Bioorganic & medicinal chemistry, Jan-01, Volume: 17, Issue:1
Selective activity against Mycobacteriumtuberculosis of new quinoxaline 1,4-di-N-oxides.
AID1276377Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium bovis BCG ATCC 357432016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID511104Cmax in C57BL/6 mouse pneumonia model at 25 mg/kg, ip2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID572062Antibacterial activity against abeS sigma abeS-deficient Acinetobacter baumannii AC0037 by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID1146811Antibacterial activity against Salmonella paratyphi B 0248 K assessed as inhibition of visible growth after 24 hrs by serial dilution method1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Synthesis and antibacterial activity of some derivatives of tolypomycinone. Relationship between structure and activity in ansamycins.
AID1851922Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as bacterial growth inhibition incubated for 6 days under normoxic condition by resazurin microtiter assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID256055Minimum inhibitory concentration against Mycobacterium avium (ATCC 25291)2005Journal of medicinal chemistry, Nov-03, Volume: 48, Issue:22
Design and studies of novel 5-substituted alkynylpyrimidine nucleosides as potent inhibitors of mycobacteria.
AID509618Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB533 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID1267219Antitubercular activity against multi drug resistant Mycobacterium tuberculosis H37Rv after 5 days by microplate alamar blue assay2016European journal of medicinal chemistry, Jan-01, Volume: 107Synthesis, antimycobacterial screening and ligand-based molecular docking studies on novel pyrrole derivatives bearing pyrazoline, isoxazole and phenyl thiourea moieties.
AID1483719Antimycobacterial activity against Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-c D28N mutant supplemented with 4 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID677138Antimicrobial activity against Mycobacterium tuberculosis H37Rv by microplate Alamar blue assay2012Bioorganic & medicinal chemistry, Sep-01, Volume: 20, Issue:17
Indole alkaloids from two cultured cyanobacteria, Westiellopsis sp. and Fischerella muscicola.
AID1601829Antibiofilm activity against Mycobacterium bovis BCG2019European journal of medicinal chemistry, Mar-01, Volume: 165Marine natural products as potential anti-tubercular agents.
AID290679Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry letters, Jun-15, Volume: 17, Issue:12
Synthesis and cytotoxic activity of trisubstituted-1,3,5-triazines.
AID678712Inhibition of human CYP1A2 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using ethoxyresorufin as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1612291Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 1 week by MABA2019Journal of natural products, 03-22, Volume: 82, Issue:3
Isolation of Tryptanthrin and Reassessment of Evidence for Its Isobaric Isostere Wrightiadione in Plants of the Wrightia Genus.
AID1293896Antitubercular activity against dormant Mycobacterium bovis BCG ATCC 35743 incubated for 40 mins by XTT Reduction Menadione Assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID362872Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 6.25 ug/ml by microplate alamar blue assay2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis and antituberculosis activity of new thiazolylhydrazone derivatives.
AID1634997Antifungal activity against Candida albicans assessed as reduction in fungal growth after 20 hrs by drop diffusion test2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antimicrobial Peptide from the Wild Bee Hylaeus signatus Venom and Its Analogues: Structure-Activity Study and Synergistic Effect with Antibiotics.
AID520293Antimicrobial activity against intracellular Staphylococcus aureus 2548 infected in human monocyte-derived macrophages after 48 hrs2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Activities of daptomycin and comparative antimicrobials, singly and in combination, against extracellular and intracellular Staphylococcus aureus and its stable small-colony variant in human monocyte-derived macrophages and in broth.
AID144030Antimycobacterial activity against Mycobacterium intracellular (ATCC 1954 E-3)2003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 1: substitution of the azepan-2-one moiety of capuramycin.
AID1765574Antibacterial activity against Bacillus subtilis ATCC 23857 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID529161FIC index, ratio of MIC for Pseudomonas aeruginosa 100609 in presence of 250 ug/ml polyethylenimine to MIC for Pseudomonas aeruginosa 1006092008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID1165081Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by MABA method2014European journal of medicinal chemistry, Nov-24, Volume: 87Design, synthesis and antimycobacterial activity of various 3-(4-(substitutedsulfonyl)piperazin-1-yl)benzo[d]isoxazole derivatives.
AID274942Antituberculosis activity against Mycobacterium tuberculosis H37Rv2006Journal of medicinal chemistry, Dec-28, Volume: 49, Issue:26
Synthesis and antituberculosis activity of a novel series of optically active 6-nitro-2,3-dihydroimidazo[2,1-b]oxazoles.
AID1069161Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 infected in mouse J774 cells assessed as intracellular growth inhibition at MIC after 7 days relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID534107Antibacterial activity against TolC deficient Pasteurella multocida pm0527 after 24 hrs by broth dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Characterization of TolC efflux pump proteins from Pasteurella multocida.
AID1632659Antitubercular activity against drug resistant active Mycobacterium tuberculosis H37Ra ATCC 25177 after 8 days by XTT reduction menadione assay2016ACS medicinal chemistry letters, Aug-11, Volume: 7, Issue:8
Synthesis and Antitubercular Activity of New Benzo[b]thiophenes.
AID537735Binding affinity to Candida albicans CaMdr1p expressed in yeast AD1-8u2010European journal of medicinal chemistry, Nov, Volume: 45, Issue:11
Analysis of physico-chemical properties of substrates of ABC and MFS multidrug transporters of pathogenic Candida albicans.
AID1567119Antimicrobial activity against Staphylococcus aureus ATCC 29213 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID545046Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ085 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID276754Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis ATCC 358372006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID373028Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PU86 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID559765Antimycobacterial activity against PknGMsm-deficient Mycobacterium smegmatis harboring PknG K181M mutant gene by Etest method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Protein kinase G is required for intrinsic antibiotic resistance in mycobacteria.
AID531022Antimicrobial activity against Clostridium difficile isolate 69 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID758267Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 250 ug/ml after 12 to 28 days by Lowenstein-Jensen method relative to control2013European journal of medicinal chemistry, Jul, Volume: 65Design and synthesis of biquinolone-isoniazid hybrids as a new class of antitubercular and antimicrobial agents.
AID1223081Reduction in Ugt1a6a gene expression in PXR-humanized mouse liver at 10 mg/kg dosed through gavage daily for 4 days by qPCR method2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Cytochrome P450 regulation by α-tocopherol in Pxr-null and PXR-humanized mice.
AID543814Bactericidal activity against Streptococcus pyogenes VT 59 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID441084Ratio of ethambutol MIC to compound MIC for Mycobacterium tuberculosis CIB992009Bioorganic & medicinal chemistry letters, Oct-01, Volume: 19, Issue:19
Simple dihydrosphyngosine analogues with potent activity against MDR-Mycobacterium tuberculosis.
AID529524Antimycobacterial activity against ethambutol resistant Mycobacterium tuberculosis isolate NJT210EMB-R-C2 assessed as bacterial colony formation at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID543799Bactericidal activity against Acinetobacter baumannii VT 126 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1476346Growth inhibition of Mycobacterium tuberculosis H37Rv exposed to plasma from BALB/c mouse treated with 20 mg/kg, po administered through microemulsion vehicle as single oral dose per gavage after 4 hrs by Resazurin microtiter assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID285552Bactericidal activity against 5-day old actively replicating Mycobacterium tuberculosis H37Rv in aerobic condition at 1 ug/ml after 1 day by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID425603Antibacterial activity against gentamicin-treated internalized Escherichia coli isolate HM580 in mouse J774A1 cells isolated from colonic mucosal biopsies of patient with Crohn's disease assessed as intracellular killing of bacteria at 10% compound Cmax a2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID529159Antibacterial activity against Pseudomonas aeruginosa 100609 after 20 hrs by broth microdilution assay2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Synergy between polyethylenimine and different families of antibiotics against a resistant clinical isolate of Pseudomonas aeruginosa.
AID566039Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 09710 after 7 days by serial double dilution technique2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and in vitro antimycobacterial activity of 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives.
AID1575940Antimycobacterial activity against Mycobacterium tuberculosis H37RvMA ATCC 27294 cultured in non protein-based Middlebrook 7H9 medium supplemented with glucose-casitone-tyloxapol assessed as inhibition of bacterial growth incubated for 7 days in by alamar
AID1447483Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P264-104354 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1557237Antitubercular activity against resistant Mycobacterium tuberculosis 2 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID1294352Antimicrobial activity against Mycobacterium tuberculosis H37Rv SRI 1345 after 7 days2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID373942AUC (0 to 168 hrs) in Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model administered at dose simulating 4200 mg once weekly schedule2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID679884TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Hepatology (Baltimore, Md.), Jul, Volume: 36, Issue:1
Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver.
AID565993Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by twofold agar dilution method2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and anti-mycobacterial activities of triazoloquinolones.
AID1055937Antimycobacterial activity against Mycobacterium tuberculosis H37Rv under normoxic condition after 7 days by MABA assay in presence of 10% fetal bovine serum2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1264492Antimicrobial activity against nonreplicating Mycobacterium tuberculosis 18b by resazurin microtiter assay2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents.
AID545939Ratio of MIC for Acinetobacter baumannii ATCC 19606 to MIC for Acinetobacter baumannii ATCC 19606 in presence of 4 ug/ml of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1476363Antitubercular activity against capreomycin resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1562249Antimycobacterial activity against Mycobacterium smegmatis atR2 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID1294372Cytotoxicity against mouse J774 cells assessed as cell viability at 10 times MIC by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID386623Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells at 100 uM by confocal microscopy2008Journal of medicinal chemistry, Oct-09, Volume: 51, Issue:19
Structural requirements for drug inhibition of the liver specific human organic cation transport protein 1.
AID1297729Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID617851Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis CIBIN/UMF15:99 isolate by microplate Alamar blue assay2011Journal of natural products, Sep-23, Volume: 74, Issue:9
Stereochemical analysis of leubethanol, an anti-TB-active serrulatane, from Leucophyllum frutescens.
AID1416274Antitubercular activity against Mycobacterium tuberculosis H37Ra harboring pTYOK infected in Balb/c mouse assessed as bacterial growth inhibition at 10 mg/kg qd measured at 2 days interval for 6 days by luminometric method2017MedChemComm, Jun-01, Volume: 8, Issue:6
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant
AID1264463Antimycobacterial activity against rifamypicin-resistant Mycobacterium tuberculosis after 7 days by REMA method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Nitrofuranyl Methyl Piperazines as New Anti-TB Agents: Identification, Validation, Medicinal Chemistry, and PK Studies.
AID560523Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate gs07022 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1297726Antibacterial activity against methicillin resistant Staphylococcus aureus isolate 3 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1471029Growth inhibition of Mycobacterium bovis BCG ATCC 35743 at 10 ug/ml by nitrate reductase based two-fold dilution assay relative to control2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID565804Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB18 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1143269Antimycobacterial activity against ethambutol-resistant Mycobacterium tuberculosis 17003 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID370253Antimycobacterial activity against Mycobacterium tuberculosis Kurono infected ICR mouse assessed as viable lung bacterial count at 10 mg/kg, po administered once daily measured after 28 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID581656Antibacterial activity against revertant Staphylococcus aureus at pH 7.4 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1304524Antibacterial activity against Escherichia coli ATCC 25922 incubated overnight by microbroth-dilution method2016Journal of natural products, Mar-25, Volume: 79, Issue:3
Biologically Active Acetylenic Amino Alcohol and N-Hydroxylated 1,2,3,4-Tetrahydro-β-carboline Constituents of the New Zealand Ascidian Pseudodistoma opacum.
AID370106Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po after 16 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID1668183Antibacterial activity against Staphylococcus aureus ATCC 29213 assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID530661Inhibition of DNA synthesis in quinolone-resistant Staphylococcus aureus CB814 harboring gyrA S84L and parC S80F mutant genes assessed as decrease in [methyl-3H]thymidine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID373029Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate PUA7 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1264493Antimicrobial activity against rifamycin-resistant Mycobacterium tuberculosis by resazurin microtiter assay2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Synthesis and Biological Evaluation of Polar Functionalities Containing Nitrodihydroimidazooxazoles as Anti-TB Agents.
AID499888Antitubercular activity against Mycobacterium tuberculosis H37Ra after 6 days by microplate alamar blue assay2010Journal of medicinal chemistry, Aug-26, Volume: 53, Issue:16
Inhibition of mycobacterial replication by pyrimidines possessing various C-5 functionalities and related 2'-deoxynucleoside analogues using in vitro and in vivo models.
AID1601629Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA method2019European journal of medicinal chemistry, Mar-01, Volume: 165Synthesis and antitubercular evaluation of reduced lipophilic imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID406614Antibacterial activity against Staphylococcus aureus ATCC 29213 infected albino guinea pig tissue-cage infection model assessed as bacterial count at 12.5 mg/kg, ip administered every 12 hrs after 4 days2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Efficacy of a novel rifamycin derivative, ABI-0043, against Staphylococcus aureus in an experimental model of foreign-body infection.
AID558267Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 3 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1634267Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition zone diameter at <3 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1323721Growth inhibition of Mycobacterium tuberculosis H37Ra at 0.5 ug/ml after 6 days by microplate alamar blue assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Investigation of C-5 alkynyl (alkynyloxy or hydroxymethyl) and/or N-3 propynyl substituted pyrimidine nucleoside analogs as a new class of antimicrobial agents.
AID531036Antimicrobial activity against Clostridium difficile isolate 3 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID509616Antibacterial activity against drug resistant Mycobacterium tuberculosis containing phenotypic rpoB526 mutation assessed as cumulative microbial sensitivity by phenotypic drug susceptibility testing2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Selection of mutations to detect multidrug-resistant Mycobacterium tuberculosis strains in Shanghai, China.
AID1577322Antimycobacterial activity against Mycobacterium kansasii CNCTC My 235/80 after 14 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID293583Antibacterial activity against Pseudomonas aeruginosa isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID530675Antimicrobial activity against rifampin-sensitive Staphylococcus aureus CB190 harboring rpoB Q468L mutant gene by broth microdilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID1905565Antimicrobial activity against Klebsiella pneumoniae ATCC 700603 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID1476360Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis H37Rv ATCC 35838 after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID326299Antibacterial activity against methicillin-resistant Staphylococcus aureus 789 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID543795Antimicrobial activity against Escherichia coli ATCC 25922 by broth microdilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID519834Antimicrobial activity against aheB deficient kanamycin-resistant Aeromonas hydrophila subsp. hydrophila ATCC 7966 harboring plasmid pEX19Gm by agar dilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Role of the AheABC efflux pump in Aeromonas hydrophila intrinsic multidrug resistance.
AID1743942Antitubercular activity against Mycobacterium tuberculosis resistant mutants generated by plating on 7H11/0ADC agar plates in presence of 3.75 to 15 uM 2-((3,5-Dinitrobenzyl)thio)quinazolin-4(3H)-one followed by sensitivity testing2021Journal of medicinal chemistry, 01-14, Volume: 64, Issue:1
2-((3,5-Dinitrobenzyl)thio)quinazolinones: Potent Antimycobacterial Agents Activated by Deazaflavin (F
AID1230066Antibacterial activity against methicillin-resistant Staphylococcus aureus GRE2691 assessed as inhibition of bacterial growth2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis and antimicrobial activity of chloramphenicol-polyamine conjugates.
AID1516025Antibacterial activity against Escherichia coli 20411 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1716709Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as fractional inhibitory concentration index in presence of doxycycline incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID571654Ratio of the MIC for Klebsiella pneumoniae in the absence of NAB7064 to MIC for Klebsiella pneumoniae in the presence of 4 ug/ml of NAB70642008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID670861Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as minimum concentration required to inhibit 90% growth after 1 week by fluorescence-based microplate Alamar Blue assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
AID560504Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate bd4768 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID1443995Hepatotoxicity in human assessed as drug-induced liver injury2014Hepatology (Baltimore, Md.), Sep, Volume: 60, Issue:3
Human drug-induced liver injury severity is highly associated with dual inhibition of liver mitochondrial function and bile salt export pump.
AID531300Antimicrobial activity against Clostridium difficile isolate 72 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID765755Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition at 6.25 ug/ml after 5 to 8 days by microplate alamar blue assay relative to control2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
Synthesis and binary QSAR study of antitubercular quinolylhydrazides.
AID452745Antibacterial activity against Escherichia coli M152010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.
AID1454449Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2017ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents.
AID1879548Antibacterial activity against metronidazole-resistant Bacteroides fragilis MMX 33872022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID537111Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 3 to 28 days by twofold dilution method2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID540211Fraction unbound in human after iv administration2008Drug metabolism and disposition: the biological fate of chemicals, Jul, Volume: 36, Issue:7
Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds.
AID144572The compound was tested for its ability to inhibit the growth of Mycobacterium tuberculosis strain H37Rv; Sensitive2000Bioorganic & medicinal chemistry letters, May-15, Volume: 10, Issue:10
Antimycobacterial activity of ionic fullerene derivatives.
AID1514448Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID487841Antimycobacterial activity against Mycobacterium chelonae after 48 hrs by microtiter plate method2010Bioorganic & medicinal chemistry, Jun-15, Volume: 18, Issue:12
A new class of potential anti-tuberculosis agents: Synthesis and preliminary evaluation of novel acrylic acid ethyl ester derivatives.
AID368649Cmin in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID1565591Antibacterial activity against Escherichia coli ATCC 43837 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID1634264Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 6.25 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID1365730Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis INH-R2 ATCC 35822 after 5 days2017Bioorganic & medicinal chemistry, 11-01, Volume: 25, Issue:21
The antitubercular activity of various nitro(triazole/imidazole)-based compounds.
AID1212144Induction of CYP3A4 in human hepatocytes at 10 uM after 72 hrs relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID571447Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by Etest method in presence of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1765579Antibacterial activity against Klebsiella pneumoniae ATCC 700603 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID305227Antimicrobial activity against Arr-1 negative Mycobacterium smegmatis DSM 43756Kml2007Bioorganic & medicinal chemistry letters, Jan-15, Volume: 17, Issue:2
New C25 carbamate rifamycin derivatives are resistant to inactivation by ADP-ribosyl transferases.
AID748178Inhibition of rifamycin-resistant Escherichia coli RNA polymerase H526Y mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID369453Inhibition of Staphylococcus epidermidis RNA polymerase mediated transcription2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vitro activities of different inhibitors of bacterial transcription against Staphylococcus epidermidis biofilm.
AID634038Antituberculosis activity against Mycobacterium tuberculosis H37Rv by twofold serial dilution method2012Bioorganic & medicinal chemistry, Jan-01, Volume: 20, Issue:1
Synthesis of novel 3-cyclohexylpropanoic acid-derived nitrogen heterocyclic compounds and their evaluation for tuberculostatic activity.
AID623633Antituberculosis activity against 10'7 cfu/mL Mycobacterium tuberculosis H37Rv after 28 days2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
A facile synthesis of carbocycle-fused mono and bis-1,2,3-selenadiazoles and their antimicrobial and antimycobacterial studies.
AID1055955Antimycobacterial activity against cycloserine-resistant Mycobacterium tuberculosis ATCC 35826 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID623580Antimicrobial activity against vancomycin-resistant Enterococcus faecium Ef 379 after 22 hrs by microbroth dilution antibiotic susceptibility assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
One-pot syntheses of pseudopteroxazoles from pseudopterosins: a rapid route to non-natural congeners with improved antimicrobial activity.
AID656227Antimycobacterial activity against isoniazid-, rifampin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1851968Antimycobacterial activity against Mycobacterium tuberculosis infected in BALB/c mouse assessed as log reduction in bacterial load in lung by measuring colony forming unit at 15 mg/kg, po administered 5 days per week for 3 weeks starting from day 10 post 2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID457435Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv by low oxygen recovery assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID1055954Antimycobacterial activity against capreomycin-resistant Mycobacterium tuberculosis under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID1879574Antibacterial activity against Prevotella disiens MMX 34462022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1071083Cytotoxicity against mouse J774A1 cells assessed as cell viability at 0.01 ug/ml after 7 days by MTT assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1185718Antituberculosis activity against Mycobacterium tuberculosis H37Rv after 7 days by serial two fold dilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID405156AUC (0 to 24 hrs) in tuberculosis patient at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID576109Antimicrobial activity against mecA-deficient Staphylococcus sciuri assessed as resistant isolates2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Nasal carriage of methicillin-resistant and methicillin-sensitive strains of Staphylococcus sciuri in the Indonesian population.
AID555315Antibacterial activity against methicillin-susceptible, vancomycin-intermediate Staphylococcus aureus 505 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID557092Antimicrobial activity against Staphylococcus aureus CIP 76.25 by microdilution method in presence of 50% human serum2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID563691Antibacterial activity against Mycobacterium tuberculosis H37Ra by by BACTEC method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
New approach for drug susceptibility testing: monitoring the stress response of mycobacteria.
AID438556Antimycobacterial activity against Mycobacterium tuberculosis H37Rv replicating form by alamar blue assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.
AID555512Antibacterial activity against methicillin-resistant, vancomycin-intermediate coagulase-negative Staphylococcus epidermidis 225 after 11 passages by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID1739636Antimycobacterial activity activity against GFP-tagged Mycobacterium tuberculosis H37Rv assessed as inhibition of microbial growth incubated for 5 days by fluorescence assay2020European journal of medicinal chemistry, Aug-15, Volume: 200Discovery of the first Mycobacterium tuberculosis MabA (FabG1) inhibitors through a fragment-based screening.
AID1474166Liver toxicity in human assessed as induction of drug-induced liver injury by measuring severity class index2016Drug discovery today, Apr, Volume: 21, Issue:4
DILIrank: the largest reference drug list ranked by the risk for developing drug-induced liver injury in humans.
AID571196Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 0.25 ug/ml NAB739 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1447548Antibacterial activity against multidrug-resistant Acinetobacter baumannii 110193 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID144372Inhibitory activity against Bacillus subtilis NAD synthetase2003Journal of medicinal chemistry, Jul-17, Volume: 46, Issue:15
Tethered dimers as NAD synthetase inhibitors with antibacterial activity.
AID373969Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as rate constant for maximal bacterial kill2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1716759Antibacterial activity against Pseudomonas aeruginosa 262-101856 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of doxycycline by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID326279Antibacterial activity against methicillin-resistant Staphylococcus aureus at 4 hrs daily exposure for 5 day2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID1890847Selectivity index, ratio of MIC50 for antimycobacterial activity against Mycobacterium smegmatis mc2 155 harbouring pMyC::PDFMtb overexpression mutant to MIC50 for antimycobacterial activity against wild type Mycobacterium smegmatis mc2 1552022Bioorganic & medicinal chemistry letters, 05-15, Volume: 64Design, synthesis and antibacterial activity against pathogenic mycobacteria of conjugated hydroxamic acids, hydrazides and O-alkyl/O-acyl protected hydroxamic derivatives.
AID1668176Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID574809Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 horboring rpoB H526Y, katG D329A/R463L, gyrA D94G/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID531280Antimicrobial activity against Clostridium difficile isolate 52 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID531025Antimicrobial activity against Clostridium difficile isolate 72 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1395982Induction of biofilm eradication of methicillin-resistant Staphylococcus aureus 2 after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID532956Antimicrobial activity against Mycobacterium tuberculosis ATCC 358022010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID543804Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as eradication of pre-formed biofilm at 1 to 10 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1312205Antibacterial activity against actively replicative Mycobacterium tuberculosis H37Rv measured after 7 days by MABA assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors.
AID1784363Antimycobacterial activity against Mycobacterium tuberculosis EthA C253R in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID1691029Antibiofilm activity against Mycobacterium tuberculosis assessed as log reduction in bacterial growth at 10 uM measured after 1 week relative to control2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID1879498Antibacterial activity against rifampicin resistant Helicobacter pylori harboring rpoBL525I/D530N mutant2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1594635Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of parasite growth incubated for 6 days by REMA method2019Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11
Synthesis of diphenoxyadamantane alkylamines with pharmacological interest.
AID1416248Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate2017MedChemComm, Jun-01, Volume: 8, Issue:6
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant
AID531059Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 26 expressing RpoB R505K mutant by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1397225Antimycobacterial activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis isolate 16995 after 7 days by Alamar blue assay2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antimycobacterial activity of 3,5-dinitrobenzamide derivatives containing fused ring moieties.
AID292313Antibacterial activity Streptococcus pyogenes ATCC 19615 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID562791Antimicrobial activity against Chlamydia trachomatis F/70/rifR harboring rpoB gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1436578Antitubercular activity against Mycobacterium tuberculosis H37Rv at 6 ug/mL2017Bioorganic & medicinal chemistry letters, 02-01, Volume: 27, Issue:3
Synthesis, identification and in vitro biological evaluation of some novel quinoline incorporated 1,3-thiazinan-4-one derivatives.
AID555743Antibacterial activity against methicillin-resistant, vancomycin-intermediate coagulase-negative Staphylococcus epidermidis 225 by agar dilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID586044Antimicrobial activity against Staphylococcus aureus clone 3-3 harboring staphylococcal cassette chromosome mec element type 4 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1192372Antimicrobial activity against Bacillus megaterium MTCC 3382 after 18 hrs by broth micro dilution method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Synthesis and antimicrobial activity of novel benzoxazine sulfonamide derivatives.
AID1580090Antibacterial activity against novobiocin-resistant Acinetobacter baumannii ATCC 17978 mutant generated from seven serial passages by checkerboard assay2019Journal of medicinal chemistry, 10-24, Volume: 62, Issue:20
Homodimeric Tobramycin Adjuvant Repurposes Novobiocin as an Effective Antibacterial Agent against Gram-Negative Bacteria.
AID1905566Antimicrobial activity against Escherichia coli ATCC 25922 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID1491297Antimycobacterial activity against Mycobacterium smegmatis ATCC MC2155 after 7 days under normoxic condition by microplate Alamar blue assay2017European journal of medicinal chemistry, Sep-08, Volume: 137QSAR-driven design, synthesis and discovery of potent chalcone derivatives with antitubercular activity.
AID581197Effect on iNOS expression in human HT-29 cells assessed as increase in 100 ng/ml IL1-beta, TNF-alpha and IFN-gamma-stimulated iNOS mRNA expression normalized to beta-actin expression level at 10 to 50 ug/ml after 24 hrs by Western blot analysis2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID457433Cytotoxicity against african green monkey Vero cells after 72 hrs2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis and antituberculosis activity of novel mefloquine-isoxazole carboxylic esters as prodrugs.
AID205648Antibacterial activity against Staphylococcus aureus 10B1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hypolipidemic activity of rifamycin derivatives.
AID425602Antibacterial activity against gentamicin-treated internalized Escherichia coli isolate LF82 in mouse J774A1 cells isolated from chronic ileal lesions of patient with Crohn's disease assessed as intracellular killing of bacteria at 10% compound Cmax after2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID767542Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 0.3125 to 5 ug/mL by resazurin assay2013Bioorganic & medicinal chemistry letters, Sep-15, Volume: 23, Issue:18
Design and synthesis of positional isomers of 5 and 6-bromo-1-[(phenyl)sulfonyl]-2-[(4-nitrophenoxy)methyl]-1H-benzimidazoles as possible antimicrobial and antitubercular agents.
AID558255Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered 2 hrs after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID1311245Antibacterial activity against Escherichia coli 14-1 expressing extended-spectrum beta-lactamase2016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID358297Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by BACTEC 460 radiometric assay2001Journal of natural products, Nov, Volume: 64, Issue:11
Inhibition of Mycobacterium tuberculosis growth by saringosterol from Lessonia nigrescens.
AID292286Antimycobacterial activity against Mycobacterium avium ATCC 25291 at 2 ug/mL by microplate Alamar blue assay2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID341779Antimycobacterial activity against Mycobacterium tuberculosis infected patient assessed as sputum bacterial count at 600 mg, po after 2 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID1563896Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days in presence of middlebrook 7H9/ADC medium by broth microdilution method2019European journal of medicinal chemistry, Oct-15, Volume: 180Bioisosteric ferrocenyl aminoquinoline-benzimidazole hybrids: Antimicrobial evaluation and mechanistic insights.
AID1329995Cytotoxicity against African green monkey Vero cells assessed as reduction cell survival rate after 72 hrs by CCK8 assay2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Discovery of new chemical entities as potential leads against Mycobacterium tuberculosis.
AID1716871Antibacterial activity against Pseudomonas aeruginosa 101243 assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1879556Antibacterial activity against Bifidobacterium longum ATCC 157072022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1215087Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis2011Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 39, Issue:1
Identification of clinically used drugs that activate pregnane X receptors.
AID523663Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta205 with RNA polymerase beta subunit S470N mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID1294354Antimicrobial activity against isoniazid resistant Mycobacterium tuberculosis SRI 1369 after 7 days2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID1435654Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 8666/2010 after 14 days by micromethod2017European journal of medicinal chemistry, Jan-27, Volume: 126S-substituted 3,5-dinitrophenyl 1,3,4-oxadiazole-2-thiols and tetrazole-5-thiols as highly efficient antitubercular agents.
AID1687469Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 25618 assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID515920Antibacterial activity against kanamycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID623625Antituberculosis activity against 5 x 10'4 bacilli per tube Mycobacterium tuberculosis H37Rv assessed as growth inhibition at 40 ug/mL incubated for 24 hrs measured after 28 days2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
1,3-Dihydro-2H-indol-2-ones derivatives: design, synthesis, in vitro antibacterial, antifungal and antitubercular study.
AID1400061Antibacterial activity against Bacillus subtilis ATCC 6051 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID531294Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 66 expressing RpoB D492N and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1146808Antibacterial activity against Staphylococcus aureus 209 P(FDA) assessed as inhibition of visible growth after 24 hrs by serial dilution method1977Journal of medicinal chemistry, Oct, Volume: 20, Issue:10
Synthesis and antibacterial activity of some derivatives of tolypomycinone. Relationship between structure and activity in ansamycins.
AID530780Antimicrobial activity against Clostridium difficile isolate 11 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID341777AUC (0 to infinity) in Mycobacterium tuberculosis infected patient at 12 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID1593909Cytotoxicity against African green monkey Vero cells assessed as decrease in cell viability after 72 hrs by MTT assay
AID1866097Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth in presence of Mycobacterial minimal medium with cholesterol measured for 2 weeks by resazurin based colorimetric assay2022European journal of medicinal chemistry, Feb-15, Volume: 230A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen).
AID1827053Antibacterial activity against Yersinia pseudotuberculosis ATCC 6904 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID559770Antimicrobial activity against SCCmec type II vancomycin-intermediate Staphylococcus aureus isolate 4sy32 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID580859Toxicity in patients with tuberculosis assessed as adverse effects at 1200 mg/kg, po once a week2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID541074Cmin in cage fluid of Albino guiena pig at 12.5 mg/kg, ip after 12 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1627514Antitubercular activity against Mycobacterium tuberculosis H37Rv INH-R1 harboring katG Y155 mutant after 5 days2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID425630Antituberculosis activity against Mycobacterium paratuberculosis ATCC 19698 isolated from bovine assessed as lowest drug level producing inhibition at 10'6 CFU of inoculum by MGIT 960 susceptibility test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Thiopurine drugs azathioprine and 6-mercaptopurine inhibit Mycobacterium paratuberculosis growth in vitro.
AID1400056Bactericidal activity against Acinetobacter baumannii ATCC 19606 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID541092Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 by macrodilution method2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID103864In vitro activity of compound against rapidly growing Mycobacterium phlei 1411990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID600830Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as inhibition of bacterial growth at 1 to 100 ug/ml after 7 days by resazurin method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
New quinolin-4-yl-1,2,3-triazoles carrying amides, sulphonamides and amidopiperazines as potential antitubercular agents.
AID1456569Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay
AID496058Induction of CYP3A4 in human hepatocytes at 10 uM after 72 hrs relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro.
AID461354Antimycobacterial activity against Mycobacterium intracellular ATCC 230682010Journal of medicinal chemistry, Jan-14, Volume: 53, Issue:1
Structure-activity relationship and mechanism of action studies of manzamine analogues for the control of neuroinflammation and cerebral infections.
AID1297724Antibacterial activity against methicillin resistant Staphylococcus aureus isolate 1 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID1888140Antimycobacterial activity against Mycobacterium bovis BCG assessed as reduction in bacterial colony forming units at 20 times MIC concentration measured after 21 days by by time kill assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1827065Antibacterial activity against Streptococcus pneumoniae ATCC 49619 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1626656Bactericidal activity against methicillin-resistant Staphylococcus aureus 67-02016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID531306Antimicrobial activity against Clostridium difficile isolate 78 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID743656Antibacterial activity against Escherichia coli EB2120 conditional lolA strain with lolA deletion and complementing copy placed at araBAD locus at 1 to 256 ug/mL after 18 hrs in presence of 0.00002 to 0.2% of arabinose2013Bioorganic & medicinal chemistry letters, Apr-15, Volume: 23, Issue:8
Degradation of MAC13243 and studies of the interaction of resulting thiourea compounds with the lipoprotein targeting chaperone LolA.
AID558268Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in intracellular bacterial cfu in peritoneum at 10 mg/kg, sc administered as single dose 1 hr after infection measured after 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID645533Cytotoxicity against african green monkey Vero cells after 72 hrs2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID586043Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type U5 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID541060AUC (0 to 24 hrs) in cage fluid of Albino guiena pig at 12.5 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1908116Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 assessed as inhibition of bacterial growth incubated for 20 to 24 hrs by broth micro dilution method2022European journal of medicinal chemistry, Jun-05, Volume: 236Design and synthesis of quinolinium-based derivatives targeting FtsZ for antibacterial evaluation and mechanistic study.
AID103839In vitro activity of compound against slowly growing Mycobacterium scrofulaceum 12971990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1179308Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by MABA method2014Bioorganic & medicinal chemistry letters, Jul-15, Volume: 24, Issue:14
Synthesis of new verapamil analogues and their evaluation in combination with rifampicin against Mycobacterium tuberculosis and molecular docking studies in the binding site of efflux protein Rv1258c.
AID33556The ability concentration.)2000Journal of medicinal chemistry, May-18, Volume: 43, Issue:10
Biosensor analysis of the interaction between immobilized human serum albumin and drug compounds for prediction of human serum albumin binding levels.
AID532023Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to CFU count by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID765105Bacteriostatic activity against rifampicin, isoniazid, streptomycin, ethambutol and pyrazinamide-resistant Mycobacterium tuberculosis MS-115 assessed as growth inhibition at 2 to 200 ug/mL relative to control2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1129361Unbound fraction in HEK293 cell homogenate at 0.1 uM by equilibrium dialysis based UPLC-MS/MS analysis2014Journal of medicinal chemistry, Apr-10, Volume: 57, Issue:7
A high-throughput cell-based method to predict the unbound drug fraction in the brain.
AID1634266Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 1.56 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID511054Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after up to 28 days2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Pharmacological evaluation and characterizations of newly synthesized 1,2,4-triazoles.
AID531279Antimicrobial activity against Clostridium difficile isolate 51 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1517152Selectivity index, ratio of CC50 for CHO cells to MIC for multidrug (INH and RIF)-resistant Mycobacterium tuberculosis clinical isolate 1
AID293529Antimycobacterial activity against Mycobacterium avium ATCC 25291 at 1 ug/mL after 24 to 48 hrs by MABA2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Studies on acyclic pyrimidines as inhibitors of mycobacteria.
AID543811Bactericidal activity against Staphylococcus aureus ATCC 29213 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1685708Antimicrobial activity against Bacillus subtilis assessed as inhibition of bacterial growth incubated for overnight by CLSI method2016Bioorganic & medicinal chemistry, 06-15, Volume: 24, Issue:12
Hydraphiles enhance antimicrobial potency against Escherichia coli, Pseudomonas aeruginosa, and Bacillus subtilis.
AID1194222Tuberculostatic activity against Mycobacterium tuberculosis H37Rv by two-fold classical test-tube method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Novel 2-(2-phenalkyl)-1H-benzo[d]imidazoles as antitubercular agents. Synthesis, biological evaluation and structure-activity relationship.
AID1262036Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2015European journal of medicinal chemistry, Nov-13, Volume: 105Design, synthesis and evaluation of diarylpiperazine derivatives as potent anti-tubercular agents.
AID1716775Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as reduction in bacterial growth by measuring doxycycline MIC at 4 ug/ml incubated for 18 hrs in presence of doxycycline by broth microdilution assay (Rvb = 64 ug/ml)2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID585877Antimicrobial activity against Staphylococcus aureus clone 2-2 harboring staphylococcal cassette chromosome mec element type 4 assessed as percent susceptible isolates by kirby-bauer method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Diversity of staphylococcal cassette chromosome mec elements in predominant methicillin-resistant Staphylococcus aureus clones in a small geographic area.
AID1905202Antibacterial activity against MDR-methicillin-resistant Staphylococcus aureus ATCC BAA-44 assessed as reduction in bacterial growth measured after 18 hrs by broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Spermine-Conjugated Short Proline-Rich Lipopeptides as Broad-Spectrum Intracellular Targeting Antibacterial Agents.
AID1557234Antitubercular activity against resistant Mycobacterium tuberculosis 76 harboring rpoB Ser531Leu mutant after 4 weeks by absolute concentration-microtiter method2019MedChemComm, Aug-01, Volume: 10, Issue:8
Drug-resistance in
AID780897Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis ATCC 35822 harboring katG mutant after 7 days by REMA assay2013Bioorganic & medicinal chemistry, Nov-15, Volume: 21, Issue:22
Synthesis and antimycobacterial activity of isoniazid derivatives from renewable fatty acids.
AID531284Antimicrobial activity against Clostridium difficile isolate 56 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID586232Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 5 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID1294371Cytotoxicity against mouse J774 cells assessed as cell viability at MIC by MTT assay relative to control2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Design and synthesis of novel quinoxaline derivatives as potential candidates for treatment of multidrug-resistant and latent tuberculosis.
AID669189Activation of PXR in human DPX2 cells after 24 hrs by luciferase reporter gene assay relative to control2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1212152Induction of CYP2C19 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID278676Antibacterial activity against Enterococcus faecalis isolate 57422007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID329350Ratio of MIC90 for Mycobacterium tuberculosis H37Rv in iron rich GAST-D medium to MIC90 for Mycobacterium tuberculosis H37Rv in presence of iron limiting GAST-D medium2008Bioorganic & medicinal chemistry letters, Apr-15, Volume: 18, Issue:8
Small molecules with structural similarities to siderophores as novel antimicrobials against Mycobacterium tuberculosis and Yersinia pestis.
AID1372627Antibacterial activity against Mycobacterium tuberculosis H37Rv after 1 week by MABA2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID144442Antimycobacterial activity was determined against Mycobacterium smegmatis SANK750752003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.
AID571195Antibacterial activity against 5 x 10'5 CFU/ml Escherichia coli ATCC 25992 in presence of 0.5 ug/ml NAB739 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1593376Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in extensively drug-resistant Mycobacterium tuberculosis TF274 assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID1143263Antimycobacterial activity against Mycobacterium tuberculosis Beijing (E-47/94) assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID289150Antimycobacterial activity against streptomycin and isoniazid-resistant Mycobacterium tuberculosis CIBIN 675 isolates2007Bioorganic & medicinal chemistry, Aug-15, Volume: 15, Issue:16
Synthesis and antimycobacterial activity of 4-(5-substituted-1,3,4-oxadiazol-2-yl)pyridines.
AID449211Cytotoxicity against african green monkey Vero cells after 72 hrs2009European journal of medicinal chemistry, Nov, Volume: 44, Issue:11
1,5-Diaryl-2-ethyl pyrrole derivatives as antimycobacterial agents: design, synthesis, and microbiological evaluation.
AID531259Antimicrobial activity against Clostridium difficile isolate 31 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID531274Antimicrobial activity against Clostridium difficile isolate 46 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1164301Inhibition of Mycobacterium tuberculosis RNA polymerase by spectrophotometry2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID444058Volume of distribution at steady state in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID268912Antibacterial activity against Mycobacterium marinum2006Journal of medicinal chemistry, Aug-10, Volume: 49, Issue:16
Antimycobacterial agents. Novel diarylpyrrole derivatives of BM212 endowed with high activity toward Mycobacterium tuberculosis and low cytotoxicity.
AID440895Antimycobacterial activity against multidrug resistant Mycobacterium smegmatis MC2 by agar dilution method2009European journal of medicinal chemistry, Dec, Volume: 44, Issue:12
L-proline-catalysed facile green protocol for the synthesis and antimycobacterial evaluation of [1,4]-thiazines.
AID533659Antimicrobial activity against Staphylococcus aureus RN42202008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID1232405Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days2015Bioorganic & medicinal chemistry, Jul-01, Volume: 23, Issue:13
Synthesis, anti-mycobacterial activity and DNA sequence-selectivity of a library of biaryl-motifs containing polyamides.
AID681586TP_TRANSPORTER: quantitative PCR in vivo, liver of mouse2003Drug metabolism and disposition: the biological fate of chemicals, Nov, Volume: 31, Issue:11
Induction of ABCC3 (MRP3) by pregnane X receptor activators.
AID1296386Antimycobacterial activity against multi drug resistant Mycobacterium tuberculosis Praha 1 after 14 days by microdilution method2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1316968Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in Balb/c mouse assessed as bacterial burden in lungs at 10 mg/kg, po administered daily through gavage for 2 weeks starting on day 2 post infection measured on day 12 post infec2016Bioorganic & medicinal chemistry letters, 11-01, Volume: 26, Issue:21
Identification and optimization of a new series of anti-tubercular quinazolinones.
AID582498Bactericidal activity against log phase culture of methicillin-resistant Staphylococcus aureus ATCC 29213 at 8 times MIC2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID1290447Antituberculosis activity against Mycobacterium tuberculosis H37Rv at 250 ug/ml incubated for 24 hrs measured after 2 to 4 weeks by Lowensteine-Jensen method2016European journal of medicinal chemistry, Apr-13, Volume: 112Novel morpholinoquinoline nucleus clubbed with pyrazoline scaffolds: Synthesis, antibacterial, antitubercular and antimalarial activities.
AID528945Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 1 day2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1476354Cytotoxicity against human MRC5 cells assessed as reduction in cell viability after 24 hrs by fluorescence assay2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1634257Antimycobacterial activity against Mycobacterium abscessus FM0058 clinical isolate assessed as inhibition zone diameter at 800 ng after 3 days by disc diffusion method2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID368646Half life in HIV-negative human at 600 mg, po administered every 24 hrs coadministered with 400 mg of atazanavir every 12 hrs2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Effect of concomitantly administered rifampin on the pharmacokinetics and safety of atazanavir administered twice daily.
AID565793Antimicrobial activity against Neisseria meningitidis harboring rpoB45 D542V mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID285192Antimicrobial activity against Escherichia coli M043 mutant with AG100 lon4::IS186 marR::IS2 genotype2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Increased genome instability in Escherichia coli lon mutants: relation to emergence of multiple-antibiotic-resistant (Mar) mutants caused by insertion sequence elements and large tandem genomic amplifications.
AID395775Antibacterial activity against Pseudomonas aeruginosa ATCC 25853 after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID571882Antibacterial activity against Escherichia coli KAM32 harboring plasmid pUC18 by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID1905562Antimicrobial activity against Bacillus subtilis ATCC 23857 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID531037Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 4 expressing RpoB S488T and R505K mutants by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1311283Selectivity index, ratio of CC50 for human HCT116 cells to MIC for dormant stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID657785Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis isolate 83 from Chinese tuberculosis patient measured 24 hrs post dose by microplate alamar blue assay2012European journal of medicinal chemistry, Jun, Volume: 52Synthesis, structure-activity relationship and in vitro anti-mycobacterial evaluation of 13-n-octylberberine derivatives.
AID1716648Antibacterial activity against methicillin-resistance Staphylococcus epidermidis CAN-ICU 61589 (CAZ>32) assessed as reduction in bacterial growth incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID1781720Antibacterial activity against Escherichia coli ATCC 25922 assessed as bacterial growth inhibition incubated for 16 to 18 hrs by broth microdilution method
AID565785Antimicrobial activity against Neisseria meningitidis harboring rpoB20 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID645540Antitubercular activity against streptomycin-resistant Mycobacterium tuberculosis by microbroth dilution assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID1385219Antitubercular activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by microplate alamar blue assay
AID529527Antimycobacterial activity against rifampin, ethambutol resistant Mycobacterium tuberculosis isolate 5041 at 37 degC after 3 to 4 weeks by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID1272619Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 14 days by broth microdilution method2016Bioorganic & medicinal chemistry letters, Feb-01, Volume: 26, Issue:3
Synthesis, in vitro antimycobacterial evaluation and docking studies of some new 5,6,7,8-tetrahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-4(3H)-one schiff bases.
AID1278191Antimicrobial activity against Mycobacterium tuberculosis infected in mouse J774 cells assessed as log reduction of bacterial burden at 8 ug/ml after 7 days2016Bioorganic & medicinal chemistry, Mar-01, Volume: 24, Issue:5
Discovery of potent anti-tuberculosis agents targeting leucyl-tRNA synthetase.
AID1333143Induction of membrane disruption in Mycobacterium bovis BCG ATCC 35734 at 60 uM up to 3 hrs by Sytox green uptake assay2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID424425Antibacterial activity against Enterococcus faecalis AIS2007003 isolated from patients rectum by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID1181159Antimicrobial activity against clinical isolate Mycobacterium tuberculosis ATCC35811 assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID571433Antibacterial activity against Escherichia coli ATCC 25992 by Etest method in presence of 2 ug/ml NAB70622008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1869562Bactericidal activity against Mycobacterium smegmatis DSM 43080 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID625292Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) combined score2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1567120Antimicrobial activity against Streptococcus pneumoniae ATCC 49619 incubated for 20 hrs by microdilution method2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological evaluation of antimicrobial diarylimine and -amine compounds targeting the interaction between the bacterial NusB and NusE proteins.
AID1158102Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in liquid broth culture medium2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
Lead optimization of a novel series of imidazo[1,2-a]pyridine amides leading to a clinical candidate (Q203) as a multi- and extensively-drug-resistant anti-tuberculosis agent.
AID400494Inhibition of AAH in Sprague-Dawley rat intestine microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 1 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1299855Antibacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse RAW 264.7 cells assessed reduction in bacterial count per well at 5 uM after 3 days (Rvb = 2.5 +/- 0.15 log10CFU)2016ACS medicinal chemistry letters, Mar-10, Volume: 7, Issue:3
2-(Quinolin-4-yloxy)acetamides Are Active against Drug-Susceptible and Drug-Resistant Mycobacterium tuberculosis Strains.
AID1061926Antimicrobial activity against Escherichia coli ATCC 25922 after 24 hrs by broth microdilution method2014European journal of medicinal chemistry, Jan, Volume: 71Synthesis and evaluation of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(4-(2-(4-substitutedpiperazin-1-yl)acetyl)piperazin-1-yl)quinoline-3-carboxylic acid derivatives as anti-tubercular and antibacterial agents.
AID1570727Antimicrobial activity against Enterococcus faecalis ATCC 29212 at 5 ug/disk incubated for 20 +/- 4 hrs by agar disk diffusion method2019Bioorganic & medicinal chemistry, 11-01, Volume: 27, Issue:21
Synthesis and evaluation of 1,3,4-oxadiazole derivatives for development as broad-spectrum antibiotics.
AID571450Antibacterial activity against Enterobacter cloacae ATCC 23355 ATCC 13883 by Etest method in presence of 2 ug/ml NAB70622008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID496046Induction of CYP1A2 in human hepatocytes at 10 uM after 72 hrs relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro.
AID1205591Equilibrium solubility of the compound in phosphate buffer by LC-MS analysis2015Journal of medicinal chemistry, Apr-09, Volume: 58, Issue:7
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
AID1602932Selectivity index, ratio of IC50 for human MRC5 cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 272942019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID572551AUC (0 to 10 hrs) in north american pulmonary tuberculosis patient coinjected with HIV with body weight >50 kg at 600 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID434062Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced [3H]arachidonic acid release at 10 to 100 ug/ml measured after 4 hrs of IL1-beta challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1585702Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID533662Antimicrobial activity against Staphylococcus aureus RN4220 harboring vgaAv positive plasmid CU12008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
Genetic characterization of Vga ABC proteins conferring reduced susceptibility to pleuromutilins in Staphylococcus aureus.
AID370074Antimycobacterial activity against Mycobacterium tuberculosis ATCC 35812 after 14 days2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID461172Antitubercular activity against Mycobacterium tuberculosis H37Rv by low-oxygen-recovery assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
AID530664Inhibition of cell wall synthesis in quinolone-resistant Staphylococcus aureus CB814 harboring gyrA S84L and parC S80F mutant genes assessed as decrease in [2,3-3H]D-alanine incorporation at 0.032 ug/ml2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
In vitro evaluation of CBR-2092, a novel rifamycin-quinolone hybrid antibiotic: studies of the mode of action in Staphylococcus aureus.
AID719007Cytotoxicity against HEK293T cells assessed as cellular growth at 25 uM by MTT assay2012Bioorganic & medicinal chemistry letters, Dec-15, Volume: 22, Issue:24
Development of 5-nitrothiazole derivatives: identification of leads against both replicative and latent Mycobacterium tuberculosis.
AID378857Antimalarial activity against multidrug-resistant Plasmodium falciparum K12006Journal of natural products, Oct, Volume: 69, Issue:10
Integerrimides A and B, cyclic heptapeptides from the latex of Jatropha integerrima.
AID640480Antimycobacterial activity against Mycobacterium avium ATCC 25291 assessed as growth inhibition at 2 ug/ml by microplate alamar blue assay2012Bioorganic & medicinal chemistry letters, Jan-15, Volume: 22, Issue:2
Antimycobacterial activities of 5-alkyl (or halo)-3'-substituted pyrimidine nucleoside analogs.
AID693674Antibacterial activity against Staphylococcus aureus isolate 100 obtained from veterinary sample after 24 hrs by broth microdilution method2012European journal of medicinal chemistry, Dec, Volume: 58Synthesis and anti-staphylococcal activity of new 4-diazopyrazole derivatives.
AID144144Antimycobacterial activity against Mycobacterium kansasii ATCC 124782003Bioorganic & medicinal chemistry letters, Sep-01, Volume: 13, Issue:17
Synthesis and antimycobacterial activity of capuramycin analogues. Part 2: acylated derivatives of capuramycin-related compounds.
AID571652Ratio of the MIC for Escherichia coli NCTC13353 in the absence of NAB7062 to MIC for Escherichia coli NCTC13353 in the presence of 4 ug/ml of NAB70622008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1866095Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth in presence of middlebrook 7H9/ADC/tyloxapol/glycerol medium measured for 1 week by resazurin based colorimetric assay2022European journal of medicinal chemistry, Feb-15, Volume: 230A new strategy for hit generation: Novel in cellulo active inhibitors of CYP121A1 from Mycobacterium tuberculosis via a combined X-ray crystallographic and phenotypic screening approach (XP screen).
AID1143270Antimycobacterial activity against ofloxacin-resistant Mycobacterium tuberculosis 12119 assessed as growth inhibition after 2 to 3 weeks by turbidometry2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Discovery of pyrazolopyridones as a novel class of noncovalent DprE1 inhibitor with potent anti-mycobacterial activity.
AID496052Induction of CYP2B6 in human hepatocytes at 10 uM after 72 hrs relative to control2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
SCY-635, a novel nonimmunosuppressive analog of cyclosporine that exhibits potent inhibition of hepatitis C virus RNA replication in vitro.
AID1634269Drug metabolism in Mycobacterium abscessus ATCC 19977 assessed as C23 ribosylated derivative formation by LC/MS analysis relative to control2019Bioorganic & medicinal chemistry letters, 08-15, Volume: 29, Issue:16
Rifamycin derivatives active against pathogenic rapidly-growing mycobacteria.
AID489572Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 14 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID1510687Antitubercular activity against multidrug resistant Mycobacterium tuberculosis isolate 11168 assessed as parasite growth inhibition measured after 7 days incubation by microplate alamar blue assay2019European journal of medicinal chemistry, Sep-15, Volume: 178Design, synthesis and biological activity of N-(2-phenoxy)ethyl imidazo[1,2-a]pyridine-3-carboxamides as new antitubercular agents.
AID1565592Antibacterial activity against Klebsiella pneumoniae ATCC 700603 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID509513Antitubercular activity against Mycobacterium tuberculosis H37Rv after 6 weeks2010European journal of medicinal chemistry, Sep, Volume: 45, Issue:9
Design, synthesis, and antitubercular evaluation of novel series of 3-benzofuran-5-aryl-1-pyrazolyl-pyridylmethanone and 3-benzofuran-5-aryl-1-pyrazolylcarbonyl-4-oxo-naphthyridin analogs.
AID523658Antimicrobial activity against transconjugant Streptomyces albus carrying pEM4T-Sbeta102 with RNA polymerase beta subunit S475A mutant after 5 to 7 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Involvement of the beta subunit of RNA polymerase in resistance to streptolydigin and streptovaricin in the producer organisms Streptomyces lydicus and Streptomyces spectabilis.
AID545927Antimicrobial activity against Enterobacter cloacae ATCC 23355 by Etest method2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1272963Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by alamar blue assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.
AID511006AUC in New Zealand rabbit meningitis model at 25 mg/kg, iv2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID689225Cytotoxicity against african green monkey Vero cells after 72 hrs by CellTiter assay2012Bioorganic & medicinal chemistry, Apr-01, Volume: 20, Issue:7
Generation and exploration of new classes of antitubercular agents: The optimization of oxazolines, oxazoles, thiazolines, thiazoles to imidazo[1,2-a]pyridines and isomeric 5,6-fused scaffolds.
AID1653523Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae subcultures at 4 weeks assessed as [3H]thymidine uptake per 5 times 10'7 cells at 0.3 mg/L incubated for 24 hrs (Rvb = 1.41 +/- 0.20 pmol)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID531303Antimicrobial activity against Clostridium difficile isolate 75 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1276376Selectivity index, ratio of GI50 for human HeLa cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, Jan-15, Volume: 26, Issue:2
Synthesis and bioactivity of novel triazole incorporated benzothiazinone derivatives as antitubercular and antioxidant agent.
AID574587Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 obtained from pus of patient at 1 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1856863Cytotoxicity against human Glomerular mesenchymal cell assessed as reduction in cell viability at 0 to 128 uM incubated for 1 hr by Resazurin cell viability kit2022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1756897Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by Lowenstein-Jensen agar method2021European journal of medicinal chemistry, Apr-05, Volume: 215Antitubercular properties of thiazolidin-4-ones - A review.
AID545804Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 planktonic cells by broth microdilution method in presence of 0.002% polysorbate 802009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Oritavancin kills stationary-phase and biofilm Staphylococcus aureus cells in vitro.
AID531019Antimicrobial activity against rifaximin-resistant Clostridium difficile isolate 66 expressing RpoB D492N and R505K mutants by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID604026Unbound CSF to plasma concentration ratio in human2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Structure-brain exposure relationships in rat and human using a novel data set of unbound drug concentrations in brain interstitial and cerebrospinal fluids.
AID510993Ratio of AUC to MIC for Acinetobacter baumannii 1327 in pharmacokinetic-pharmacodynamic C57BL/6 mouse pneumonia model at 25 mg/kg, ip2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1869527Antibacterial activity against Staphylococcus epidermidis ATCC12228 measured after 24 hrs by broth microdilution method
AID572542Absorption rate constant in pulmonary tuberculosis patient in transit compartment model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1851921Antimycobacterial activity against Mycobacterium tuberculosis H37Ra ATCC 25177 assessed as bacterial growth inhibition incubated for 6 days under normoxic condition by resazurin microtiter assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID392604Antimycobacterial activity against Mycobacterium vaccae MTCC 997 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID1827062Antibacterial activity against Staphylococcus epidermidis ATCC 14990 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID444054Oral bioavailability in human2010Journal of medicinal chemistry, Feb-11, Volume: 53, Issue:3
Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination.
AID1372636Antibiofilm activity against Mycobacterium tuberculosis H37Rv at 10 ug/ml after 1 week2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1385221Antitubercular activity against isoniazid/rifampicin-resistant Mycobacterium tuberculosis 14231 clinical isolate measured after 7 days by microplate alamar blue assay
AID426145Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as parasite growth inhibition at 25 ug/ml after 4 days by microplate alamar blue assay2009Journal of natural products, Jul, Volume: 72, Issue:7
Macrophyllin-type bicyclo[3.2.1]octanoid neolignans from the leaves of Pleurothyrium cinereum.
AID1784357Antimycobacterial activity against Mycobacterium tuberculosis MmpL3 G758A in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID472699Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay2010Bioorganic & medicinal chemistry, Apr-15, Volume: 18, Issue:8
Trypanoside, anti-tuberculosis, leishmanicidal, and cytotoxic activities of tetrahydrobenzothienopyrimidines.
AID599009Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by agar dilution method2011Bioorganic & medicinal chemistry, Jun-01, Volume: 19, Issue:11
Antimycobacterial activity of novel 1,2,4-oxadiazole-pyranopyridine/chromene hybrids generated by chemoselective 1,3-dipolar cycloadditions of nitrile oxides.
AID372463Antimalarial activity as 2nd generation ring-stage chloroquine-resistant Plasmodium falciparum W2 after 48 hrs by flow cytometry2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID530800Antimicrobial activity against Clostridium difficile isolate 31 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID562789Antimicrobial activity against Chlamydia trachomatis L2/tetR13 harboring tet(C) allele2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1474041Ratio of drug concentration at steady state in human at 150 to 600 mg, iv QD after 24 hrs to IC50 for human MRP3 overexpressed in Sf9 insect cells2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID475039Selectivity ratio of IC50 for Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
New 3-methylquinoxaline-2-carboxamide 1,4-di-N-oxide derivatives as anti-Mycobacterium tuberculosis agents.
AID774605Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene assessed as growth inhibition at 1 uM after 6 days by luminometry relative to control2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID582497Antimicrobial activity against stationary phase culture of methicillin-resistant Staphylococcus aureus ATCC 29213 by macrodilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID565790Antimicrobial activity against Neisseria meningitidis harboring rpoB37 G560S mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID656229Antimycobacterial activity against isoniazid-, rifampin-, streptomycin-resistant Mycobacterium tuberculosis after 16 to 24 hrs by alamar blue assay2012Bioorganic & medicinal chemistry letters, Apr-15, Volume: 22, Issue:8
Antimycobacterial activity of bisbenzylisoquinoline alkaloids from Tiliacora triandra against multidrug-resistant isolates of Mycobacterium tuberculosis.
AID1364752Antibacterial activity against Mycobacterium tuberculosis H37Rv nutrient starvation model assessed as log reduction in bacterial colonies at 10 ug/ml measured after 7 days by MPN assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID531308Antimicrobial activity against Clostridium difficile isolate 80 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID581193Effect on iNOS expression in human A549 cells assessed as fold increase in 100 ng/ml IL1-beta, TNF-alpha and IFN-gamma-stimulated iNOS mRNA expression at 50 ug/ml after 19 hrs by TaqMan real-time RT-PCR relative to control2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Roles of NF-kappaB activation and peroxisome proliferator-activated receptor gamma inhibition in the effect of rifampin on inducible nitric oxide synthase transcription in human lung epithelial cells.
AID603301Antitubercular activity against Mycobacterium tuberculosis H37Rv by Bactec 460 method2011Bioorganic & medicinal chemistry letters, Jul-01, Volume: 21, Issue:13
1-Chloro-2-formyl indenes and tetralenes as antitubercular agents.
AID445930Cytotoxicity against african green monkey Vero cells after 72 hrs2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents.
AID1185713Antibacterial activity against Escherichia coli ATCC 10538 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1888138Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD4 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID531268Antimicrobial activity against Clostridium difficile isolate 40 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID495234Antimicrobial activity against wild type Mycobacterium tuberculosis NJT210CGG-CAG after 4 weeks2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Allelic exchange and mutant selection demonstrate that common clinical embCAB gene mutations only modestly increase resistance to ethambutol in Mycobacterium tuberculosis.
AID1556636Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as reduction in bacterial cell viability incubated for 7 days by microplate alamar blue assay2019European journal of medicinal chemistry, Oct-01, Volume: 179hERG optimizations of IMB1603, discovery of alternative benzothiazinones as new antitubercular agents.
AID1297728Antibacterial activity against methicillin resistant Staphylococcus aureus isolate 5 after 18 hrs by microdilution method2016European journal of medicinal chemistry, Jun-30, Volume: 116Structure-activity relationship studies of new rifamycins containing l-amino acid esters as inhibitors of bacterial RNA polymerases.
AID400490Inhibition of ethylmorphine N-demethylase in hepatic microsomes1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1212146Induction of CYP2B6 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1491508Therapeutic index, ratio of CC50 for human MRC5 cells to MIC90 for Mycobacterium tuberculosis H37Ra Lehmann and Neumann ATCC 25177 harboring pSMT1 luciferase reporter2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID380454Antibacterial activity against Staphylococcus aureus ATCC 25923 by standard broth microdilution technique2006Journal of natural products, Mar, Volume: 69, Issue:3
(+)-agelasine D: improved synthesis and evaluation of antibacterial and cytotoxic activities.
AID1406216Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis after 7 days
AID1827054Antibacterial activity against Acinetobacter baumannii ATCC 19606 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1879534Antibacterial activity against fluoroquinolone-resistant Clostridioides difficile CB1939 measured after 3 days2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID560515Antimicrobial activity against SCCmec type III vancomycin-intermediate Staphylococcus aureus isolate 13b16 by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Prevalence and characterization of heterogeneous vancomycin-intermediate Staphylococcus aureus isolates from 14 cities in China.
AID531005Antimicrobial activity against Clostridium difficile isolate 52 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID555305Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS1 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID373970Antimycobacterial activity against drug-resistant Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as concentration needed to achieve 50% maximal killing rat2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID626922Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 using compound level ranging from 0.3125 to 5 ug/mL after 7 days by resazurin reduction test2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Design, synthesis and docking studies of new quinoline-3-carbohydrazide derivatives as antitubercular agents.
AID14138650% inhibition of the 20 Mycobacterium (MAC) avium complex clinical isolates1990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1212121Cytotoxicity against human hepatocytes assessed as cell viability relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1254280Antimycobacterial activity against Mycobacterium tuberculosis H37Rv in 7H9/ADC/Tween medium measured at day 14 by Alamar Blue assay2015Bioorganic & medicinal chemistry, Nov-15, Volume: 23, Issue:22
Aminopyrazolo[1,5-a]pyrimidines as potential inhibitors of Mycobacterium tuberculosis: Structure activity relationships and ADME characterization.
AID1868118Anti-tubercular activity against Mycobacterium tuberculosis CF152 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID1179476Antitubercular activity against Mycobacterium tuberculosis H37Rv transfected with pFCA-luxAB in 7H12 medium after 10 days by low-oxygen recovery assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID683321Antibacterial activity against drug-resistant Mycobacterium tuberculosis 926 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID429091Antimycobacterial activity against Mycobacterium tuberculosis clinical isolates from tuberculosis patient assessed as percent sensitive isolates at 40 ug/ml by absolute-concentration method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Prevalence of and molecular basis for tuberculosis drug resistance in the Republic of Georgia: validation of a QIAplex system for detection of drug resistance-related mutations.
AID554580Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in extracellular bacterial cfu in peritoneum at 60 mg/kg, sc administered as single dose 2 hrs after infection measured within 4 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID103660In vitro activity of compound against rapidly growing Mycobacterium fortuitum 7261990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1210913Inhibition of human recombinant AADAC2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID1174122Antimicrobial activity against Mycobacterium tuberculosis Spec. 210 by two-fold serial dilution method2015European journal of medicinal chemistry, Jan-07, Volume: 89Synthesis and evaluation of in vitro antimycobacterial activity of novel 1H-benzo[d]imidazole derivatives and analogues.
AID531015Antimicrobial activity against Clostridium difficile isolate 62 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1516085Antibacterial activity against ciprofloxacin-resistant Escherichia coli ATCC 25922 incubated for 18 to 24 hrs2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1897868Bactericidal activity against Non-replicating Mycobacterium tuberculosis ss18b-lux assessed as decrease in colony forming unit measured at 0.6 uM after 1 weeks
AID454542Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
A highly atom economic, chemo-, regio- and stereoselective synthesis and evaluation of spiro-pyrrolothiazoles as antitubercular agents.
AID1577320Antimycobacterial activity against Mycobacterium avium CNCTC My 330/88 after 21 days2019Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17
Development of 3,5-Dinitrophenyl-Containing 1,2,4-Triazoles and Their Trifluoromethyl Analogues as Highly Efficient Antitubercular Agents Inhibiting Decaprenylphosphoryl-β-d-ribofuranose 2'-Oxidase.
AID584271Inhibition of pig Malate dehydrogenase at 0.0472 uM2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Furanyl-rhodanines are unattractive drug candidates for development as inhibitors of bacterial RNA polymerase.
AID1888136Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD2 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID1071100Antimycobacterial activity against Mycobacterium tuberculosis H37Rv SRI 1345 at MIC after 7 days by broth microdilution assay relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID580322Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate after 5 days by tetrazolium microplate assay2011Bioorganic & medicinal chemistry, Mar-15, Volume: 19, Issue:6
Synthesis and biological evaluation of benzimidazole-5-carbohydrazide derivatives as antimalarial, cytotoxic and antitubercular agents.
AID1218863Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate2012Drug metabolism and disposition: the biological fate of chemicals, Aug, Volume: 40, Issue:8
The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery.
AID292310Antibacterial activity against Staphylococcus aureus ATCC 25923 at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID1069158Cytotoxicity against mouse J774 cells assessed as cell viability at MIC relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1667679Antimycobacterial activity against multidrug resistant Mycobacterium tuberculosis G122 incubated for 5 days by alamar blue based colorimetric assay2020Bioorganic & medicinal chemistry letters, 05-01, Volume: 30, Issue:9
Synthesis and in vitro evaluation of antimycobacterial and cytotoxic activity of new α,β-unsaturated amide, oxazoline and oxazole derivatives from l-serine.
AID1427058Selectivity index, ratio of GI50 for human PANC1 cells to MIC for active stage of Mycobacterium tuberculosis H37Ra ATCC 251772017European journal of medicinal chemistry, Feb-15, Volume: 127Hybrids of thienopyrimidinones and thiouracils as anti-tubercular agents: SAR and docking studies.
AID562783Antimicrobial activity against Chlamydia suis S45/rifR harboring rpoB gene2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Horizontal transfer of tetracycline resistance among Chlamydia spp. in vitro.
AID1167351Antibacterial activity against Pseudomonas aeruginosa PAO1 mexAB/mexCD/mexXY/mexHI/opmH deletion mutant after 18 to 24 hrs by two-fold broth microdilution method2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID1070190Antimycobacterial activity against Mycobacterium intracellulare MNT1408 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID1491510Genotoxicity in Salmonella typhimurium TA104 harboring RecN2-4 lux operon fusion at 1.28 to 128 uM measured every 5 mins for 4 hrs in presence of S9 liver fraction by vitotox assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID1681007Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth incubated for 7 days by alamar blue assay2020Bioorganic & medicinal chemistry letters, 10-01, Volume: 30, Issue:19
Novel isoniazid embedded triazole derivatives: Synthesis, antitubercular and antimicrobial activity evaluation.
AID373949Ratio of Cmax to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model at 2 mg/L administered for 7 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1497857Antibacterial activity against Escherichia coli ATCC 10536 assessed as diameter of inhibition zone at 200 ug per disc after 24 hrs by agar disc diffusion method2018Bioorganic & medicinal chemistry, 07-23, Volume: 26, Issue:12
Design, synthesis and biological evaluation of benzofuran appended benzothiazepine derivatives as inhibitors of butyrylcholinesterase and antimicrobial agents.
AID625287Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for hepatomegaly2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1293904Cytotoxicity against human A549 cells after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1244841Solubility of the compound in water at pH 72015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
The effect of complexation of 3-formylrifamycin SV macrocyclic ether derivatives with metal cations and small nitrogen-containing organic molecules on antibacterial activity against S. aureus and S. epidermidis.
AID389101Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID446152Cytotoxicity against african green monkey Vero cells after 72 hrs2010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Rational design of 5-phenyl-3-isoxazolecarboxylic acid ethyl esters as growth inhibitors of Mycobacterium tuberculosis. a potent and selective series for further drug development.
AID557095Binding affinity to first site on human serum albumin by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID292422Antitubercular activity against Mycobacterium tuberculosis H37Rv2007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID1333168Induction of membrane integrity impairment in Mycobacterium bovis BCG ATCC 35734 assessed as reduction in intracellular pH at 16 times MIC by CMFDA dye based fluorescence spectroscopic method2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID1476362Antitubercular activity against bedaquiline resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1720196Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2020Bioorganic & medicinal chemistry, 07-01, Volume: 28, Issue:13
Structure-activity relationship analyses of fusidic acid derivatives highlight crucial role of the C-21 carboxylic acid moiety to its anti-mycobacterial activity.
AID1851920Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as bacterial growth inhibition incubated for 5 days under normoxic condition by resazurin microtiter assay2022Journal of medicinal chemistry, 10-13, Volume: 65, Issue:19
Nitroimidazopyrazinones with Oral Activity against Tuberculosis and Chagas Disease in Mouse Models of Infection.
AID544825Antimicrobial activity against Staphylococcus aureus Xen 30 biofilm assessed as log10 CFU/cm'2 in bacterial count in presence of 2000 microamperes of electric current by bioelectric effect assay2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID665369Antitubercular activity against Mycobacterium tuberculosis H37Rv at 40 ug/mL by radiometric growth assay2012European journal of medicinal chemistry, Jul, Volume: 53Synthesis and antimycobacterial activity of novel 1,3-dimethylisocyanurate derivatives.
AID405148Half life in tuberculosis patient at 450 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID545047Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ088 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID1627298Cytotoxicity against african green monkey Vero cells assessed as reduction in cell viability measured after 72 hrs by MTS assay2016Bioorganic & medicinal chemistry letters, 08-15, Volume: 26, Issue:16
New antibacterial agents: Hybrid bioisoster derivatives as potential E. coli FabH inhibitors.
AID144445In vitro antibacterial activity against Mycobacterium smegmatis 1035991999Bioorganic & medicinal chemistry letters, Oct-18, Volume: 9, Issue:20
New pyrrole derivatives as antimycobacterial agents analogs of BM212.
AID1378486Antitubercular activity against Mycobacterium tuberculosis H37Rv by broth microdilution Alamar blue assay
AID1476361Antitubercular activity against moxifloxacin resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID572536Apparent volume of distribution in pulmonary tuberculosis patient in Sequential 0 order and first order model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID1143687Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in spleen at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 32014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
AID1614910Inhibition of human ERG at 10 uM relative to control2019Bioorganic & medicinal chemistry, 03-01, Volume: 27, Issue:5
Design, synthesis and antimycobacterial activity of less lipophilic Q203 derivatives containing alkaline fused ring moieties.
AID669845Antibacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Discovery of selective menaquinone biosynthesis inhibitors against Mycobacterium tuberculosis.
AID531008Antimicrobial activity against Clostridium difficile isolate 55 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID405149Ratio of Cmax at 600 mg, po to Cmax at 450 mg, po in tuberculosis patient2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1332964Cytotoxicity against human MRC5 cells measured after 24 hrs by resazurin based fluorescence method2016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID1272956Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.
AID289132Growth inhibition of Mycobacterium tuberculosis H37Rv at 6.25 ug/mL by microplate alamar blue assay2007Bioorganic & medicinal chemistry, Sep-01, Volume: 15, Issue:17
Synthesis and structure-antituberculosis activity relationship of 1H-indole-2,3-dione derivatives.
AID530050Antimicrobial activity against Staphylococcus aureus 286607-R1 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Discovery and characterization of QPT-1, the progenitor of a new class of bacterial topoisomerase inhibitors.
AID683319Antibacterial activity against Mycobacterium smegmatis MC2 155 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID1454450Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis 14231 after 7 days by microplate alamar blue assay2017ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6
Identification of Better Pharmacokinetic Benzothiazinone Derivatives as New Antitubercular Agents.
AID1654159Cytotoxicity against African green monkey Vero cells2020Journal of natural products, 03-27, Volume: 83, Issue:3
Antimycobacterial Rufomycin Analogues from
AID1514449Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1185712Antibacterial activity against Staphylococcus epidermidis ATCC 49134 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID515919Antibacterial activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID1484387Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 5 to 8 days2017European journal of medicinal chemistry, Jun-16, Volume: 133Isoniazid derivatives and their anti-tubercular activity.
AID1399585Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
Design, synthesis and evaluation of oxime-functionalized nitrofuranylamides as novel antitubercular agents.
AID529520Antibacterial activity against thymidine-dependent small-colony variant Staphylococcus aureus derived from cystic fibrosis patient assessed as resistant isolates at 37 degC after 24 hrs by disk diffusion method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
The thymidine-dependent small-colony-variant phenotype is associated with hypermutability and antibiotic resistance in clinical Staphylococcus aureus isolates.
AID1173783Inhibition of purified Mycobacterium smegmatis GyrB at 50 to 100 uM after 100 mins by ATPase assay2014Bioorganic & medicinal chemistry, Dec-01, Volume: 22, Issue:23
An efficient synthesis and biological screening of benzofuran and benzo[d]isothiazole derivatives for Mycobacterium tuberculosis DNA GyrB inhibition.
AID1719084Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as reduction in microbial growth after 7 to 14 days by broth dilution method2021Bioorganic & medicinal chemistry letters, 03-01, Volume: 35Synthesis of novel quinoxaline-alkynyl derivatives and their anti-Mycobacterium tuberculosis activity.
AID543807Bactericidal activity against Haemophilus influenzae VT450-2006 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs by serial dilution2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1395981Bactericidal activity against methicillin-resistant Staphylococcus aureus 2 planktonic cells after 24 hrs by calgary biofilm device method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID634278Antimycobacterial activity against Mycobacterium tuberculosis isolate 308 expressing rpoB His526Asp mutant gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1832327Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis H37Rv harboring RpoBS522L mutant assessed as bacterial growth inhibition measured after 5 days by serial dilution method2021European journal of medicinal chemistry, Dec-05, Volume: 225Novel C-3-(N-alkyl-aryl)-aminomethyl rifamycin SV derivatives exhibit activity against rifampicin-resistant Mycobacterium tuberculosis RpoB
AID292306Antibacterial activity against Enterobacter aerogenes at 1 ug/ml after 16 to 20 hrs by broth microdilution method2007Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15
Growth inhibition of Mycobacterium bovis, Mycobacterium tuberculosis and Mycobacterium avium in vitro: effect of 1-beta-D-2'-arabinofuranosyl and 1-(2'-deoxy-2'-fluoro-beta-D-2'-ribofuranosyl) pyrimidine nucleoside analogs.
AID372542Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 12-36 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1212149Induction of CYP1A2 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID1061105Cytotoxicity against african green monkey Vero cells2014Bioorganic & medicinal chemistry letters, Jan-01, Volume: 24, Issue:1
A novel indigoid anti-tuberculosis agent.
AID374186Antimicrobial activity against 3 weeks old culture of Mycobacterium tuberculosis H37Ra assessed as colony forming unit in hypoxic condition at 2 ug/ml for 3 hrs2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Pyrrolidine dithiocarbamate and diethyldithiocarbamate are active against growing and nongrowing persister Mycobacterium tuberculosis.
AID623578Antimicrobial activity against Mycobacterium smegmatis ATCC 12051 after 5 days by microbroth dilution antibiotic susceptibility assay2011Journal of natural products, Oct-28, Volume: 74, Issue:10
One-pot syntheses of pseudopteroxazoles from pseudopterosins: a rapid route to non-natural congeners with improved antimicrobial activity.
AID1311234Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-32016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID977602Inhibition of sodium fluorescein uptake in OATP1B3-transfected CHO cells at an equimolar substrate-inhibitor concentration of 10 uM2013Molecular pharmacology, Jun, Volume: 83, Issue:6
Structure-based identification of OATP1B1/3 inhibitors.
AID1137531Antitubercular activity against 1-ethyl-3-(6-(pyrimidin-5-yl)-5-((tetrahydrofuran-3-yl)methoxy)thiazolo[5,4-b]pyridin-2-yl)urea-resistant Mycobacterium tuberculosis H37Rv clone 8.1 harboring DNA gyraseB ATP domain Ala92Ser mutant assessed as growth inhibi2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Thiazolopyridine ureas as novel antitubercular agents acting through inhibition of DNA Gyrase B.
AID279815Antimicrobial activity against Escherichia coli DH5-alpha with pGEM-T EASY expressing TEM1 gene by agar dilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Plasmid-mediated KPC-2 in a Klebsiella pneumoniae isolate from China.
AID776903Antibacterial activity against Escherichia coli expressing TolC mutant2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID1058226Antimycobacterial activity against Mycobacterium kansasii2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID324987Antibacterial activity against Haemophilus influenzae MSC06651 by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Horizontal gene transfer of ftsI, encoding penicillin-binding protein 3, in Haemophilus influenzae.
AID529542Antimycobacterial activity against Mycobacterium tuberculosis isolate 210 at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID680077TP_TRANSPORTER: inhibition of Azidopine photoaffinity labelling (Rifampicin: 200 uM) in membranes from K562 R7 cells1995Biochemical pharmacology, May-11, Volume: 49, Issue:9
Rifampicin enhances anti-cancer drug accumulation and activity in multidrug-resistant cells.
AID1291995Antimycobacterial activity against rifampicin resistant Mycobacterium tuberculosis H37Rv ATCC 35838 at 2 ug/ml2016Bioorganic & medicinal chemistry, Apr-15, Volume: 24, Issue:8
Investigation of 4-amino-5-alkynylpyrimidine-2(1H)-ones as anti-mycobacterial agents.
AID278684Antibacterial activity against Enterococcus faecalis isolate 57462007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
High-level vancomycin-resistant Staphylococcus aureus isolates associated with a polymicrobial biofilm.
AID1395974Antibacterial activity against methicillin-resistant Staphylococcus epidermidis ATCC 35984 after 16 to 18 hrs by broth microdilution method2018Journal of medicinal chemistry, 05-10, Volume: 61, Issue:9
An Efficient Buchwald-Hartwig/Reductive Cyclization for the Scaffold Diversification of Halogenated Phenazines: Potent Antibacterial Targeting, Biofilm Eradication, and Prodrug Exploration.
AID582811Antimicrobial activity against glycopeptide-resistant Enterococcus faecalis isolate HS05446 harboring MLST sequence type ST17 and pulsotype B expressing vanA gene cluster isolated from urine of patient by Etest2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
vanM, a new glycopeptide resistance gene cluster found in Enterococcus faecium.
AID1058228Antibacterial activity against Escherichia coli ATCC 29522 by CLSI method2013Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24
Design and synthesis of novel antimicrobials with activity against Gram-positive bacteria and mycobacterial species, including M. tuberculosis.
AID1359450Antitubercular activity against active stage of Mycobacterium tuberculosis H37Ra ATCC 25177 after 8 days by XRMA2018European journal of medicinal chemistry, May-25, Volume: 152Antibacterial and anti-TB tat-peptidomimetics with improved efficacy and half-life.
AID700530Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 at 0.3125 to 5 ug/mL after 7 days by Resazurin assay2011European journal of medicinal chemistry, Nov, Volume: 46, Issue:11
Synthesis and biological evaluation of novel pyrazole derivatives with anticancer activity.
AID557096Binding affinity to human alpha-1-acid glycoprotein assessed as compound binding sites level by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID1209529Activation of rat PXR expressed in rat hepatocytes coexpressing CYP3A4 at 10 uM after 24 hrs by dual luciferase reporter gene assay relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID376996Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate by alamar blue assay2006Journal of natural products, May, Volume: 69, Issue:5
Aegicerin, the first oleanane triterpene with wide-ranging antimycobacterial activity, isolated from Clavija procera.
AID1603254Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay
AID1624154Antitubercular activity against multidrug-resistant Mycobacterium tuberculosis isolate 6 after 7 days2019European journal of medicinal chemistry, Feb-15, Volume: 164Synthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis.
AID683315Antibacterial activity against Staphylococcus aureus ATCC 25923 by microbroth dilution method2012Bioorganic & medicinal chemistry letters, Oct-01, Volume: 22, Issue:19
Three new 12-carbamoylated streptothricins from Streptomyces sp. I08A 1776.
AID1439666Antitubercular activity against Mycobacterium tuberculosis H37Rv after 7 days by Alamar blue assay2017Bioorganic & medicinal chemistry letters, 04-01, Volume: 27, Issue:7
A robust synthesis of functionalized 2H-indazoles via solid state melt reaction (SSMR) and their anti-tubercular activity.
AID285553Bactericidal activity against 5-day old actively replicating Mycobacterium tuberculosis H37Rv in aerobic condition at 1 ug/ml after 4 days by Wayne dormancy culture model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Metronidazole plus rifampin sterilizes long-term dormant Mycobacterium tuberculosis.
AID758266Antituberculosis activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition after 12 to 28 days by Lowenstein-Jensen method2013European journal of medicinal chemistry, Jul, Volume: 65Design and synthesis of biquinolone-isoniazid hybrids as a new class of antitubercular and antimicrobial agents.
AID1819098Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 3 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID530989Antimicrobial activity against Clostridium difficile isolate 36 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID565807Antimicrobial activity against Neisseria meningitidis expressing wild type rpoB31 allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID1504966Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by second incubation under aerobic condition for 28 hrs by LORA2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID1293912Selectivity index, ratio of GI50 for human THP1 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1474038Drug concentration at steady state in human at 150 to 600 mg, iv QD after 24 hrs2013Toxicological sciences : an official journal of the Society of Toxicology, Nov, Volume: 136, Issue:1
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.
AID1767891Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 48 hrs by MTT assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Identification of novel benzothiopyranones with ester and amide motifs derived from active metabolite as promising leads against Mycobacterium tuberculosis.
AID276756Antimycobacterial activity against Mycobacterium tuberculosis H37 Rv ATCC 272942006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID419829Antibacterial activity against Klebsiella pneumoniae MTCC 109 at 1000 ug/ml after 24 hrs by agar diffusion method2009European journal of medicinal chemistry, Jun, Volume: 44, Issue:6
Physicochemical and biological characterization of novel macrocycles derived from o-phthalaldehyde.
AID510984Antimicrobial activity against Acinetobacter baumannii 1417 after 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1765578Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 incubated for 18 hrs by CLSI based broth dilution method2021Journal of medicinal chemistry, 08-12, Volume: 64, Issue:15
Novel Broad-Spectrum Antimicrobial Peptide Derived from Anoplin and Its Activity on Bacterial Pneumonia in Mice.
AID678713Inhibition of human CYP2C9 assessed as ratio of IC50 in absence of NADPH to IC50 for presence of NADPH using 7-methoxy-4-trifluoromethylcoumarin-3-acetic acid as substrate after 30 mins2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID564979Antimicrobial activity against Mycobacterium bovis BCG KOP55 harboring inactivated p55 gene by resazurine microtiter assay in presence of 1 mg/liter CCCP2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1879577Antibacterial activity against Veillonella parvula ATCC 17745 MMX 12722022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID530799Antimicrobial activity against Clostridium difficile isolate 30 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID645531Antituberculosis activity against Mycobacterium tuberculosis H37Rv ATCC 27294 in 7H12 medium after 1 week by microplate alamar blue assay2011ACS medicinal chemistry letters, Jun-09, Volume: 2, Issue:6
Advent of Imidazo[1,2-a]pyridine-3-carboxamides with Potent Multi- and Extended Drug Resistant Antituberculosis Activity.
AID200519Minimum inhibitory concentration of compound tested for antibacterial activity against Salmonella paratyphi BO 248 K(Sclavo)1981Journal of medicinal chemistry, Nov, Volume: 24, Issue:11
Synthesis and antibacterial activity of some ester, amides, and hydrazides of 3-carboxyrifamycin S. Relationship between structure and activity of ansamycins.
AID583686Antimicrobial activity against methicillin-resistant Staphylococcus aureus 10*3d1 harboring rpoB 621A mutation after 24 hrs by Etest method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
An RpoB mutation confers dual heteroresistance to daptomycin and vancomycin in Staphylococcus aureus.
AID1462360Antitubercular activity against Mycobacterium tuberculosis H37Rv at 50 ug/ml after 5 days by microplate alamar blue assay relative to control
AID582518Ratio of Cmax in Wistar rat tissue cage fluid to MIC for Staphylococcus epidermidis ATCC 27626 at 25 mg/kg, ip measured on day 42008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Antagonistic effect of rifampin on the efficacy of high-dose levofloxacin in staphylococcal experimental foreign-body infection.
AID757714Antibacterial activity against Staphylococcus aureus subsp. aureus Newman assessed as growth inhibiiton after 18 hrs2013European journal of medicinal chemistry, Jul, Volume: 65Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: structure-based optimization of a virtual screening hit.
AID1335286Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 100 uM measured after 72 hrs by MTT assay relative to control2016European journal of medicinal chemistry, Nov-29, Volume: 124Mycobacterium Tuberculosis (MTB) GyrB inhibitors: An attractive approach for developing novel drugs against TB.
AID1432974Antitubercular activity against isoniazid/rifampicin/streptomycin/ethambutol/levofloxacin-resistant Mycobacterium tuberculosis 16802 clinical isolate after 7 days by microplate alamar blue assay
AID1435852Bactericidal activity against Mycobacterium tuberculosis H37Rv infected in mouse RAW264.7 cells assessed as bacterial colony formation at 5 uM after 5 days (Rvb = 4.1 to 4.73 log10CU)2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID564988Antimicrobial activity against Mycobacterium bovis BCG harboring pPAZ23 carrying p27-p55 operon by resazurine microtiter assay2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Role of the Mycobacterium tuberculosis P55 efflux pump in intrinsic drug resistance, oxidative stress responses, and growth.
AID1879558Antibacterial activity against rifampicin-resistant Clostridium difficile MMX 35872022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID341767Cmax in Mycobacterium tuberculosis infected patient at 3 mg/kg2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Early bactericidal activity of high-dose rifampin in patients with pulmonary tuberculosis evidenced by positive sputum smears.
AID396040Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate expressing pAP3 plasmid containing Enterobacter aerogenes acrR gene by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID545926Antimicrobial activity against in Klebsiella pneumoniae ATCC 13883 in presence of NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1293879Antitubercular activity against Mycobacterium tuberculosis H37Ra ATCC 25177 incubated for 40 mins by XTT Reduction Menadione Assay2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID531301Antimicrobial activity against Clostridium difficile isolate 73 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID144876Antimycobacterial activity against Mycobacterium tuberculosis strain resistant to para-aminosalicilyc acid (PAS)2001Bioorganic & medicinal chemistry letters, Jul-09, Volume: 11, Issue:13
Antimycobacterial activity of 9-sulfonylated/sulfenylated-6-mercaptopurine derivatives.
AID1400048Antibacterial activity against Enterococcus faecalis ATCC 19433 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID537112Antimycobacterial activity against Mycobacterium tuberculosis CIP 103471 after 3 to 28 days by twofold dilution method2010Bioorganic & medicinal chemistry, Nov-15, Volume: 18, Issue:22
Identification of a novel pyrrole derivative endowed with antimycobacterial activity and protection index comparable to that of the current antitubercular drugs streptomycin and rifampin.
AID1539492Antibacterial activity against methicillin-resistant Staphylococcus aureus NRS123-USA400 clinical isolates assessed as ratio of MIC after and before 1 serial passages by broth microdilution assay
AID168258Compound was tested for hypolipidemic activity in male rats, cholesterol was determined in serum at 100 mg/kg1990Journal of medicinal chemistry, Feb, Volume: 33, Issue:2
Hypolipidemic activity of rifamycin derivatives.
AID1756898Antimycobacterial activity against Mycobacterium tuberculosis H37Rv measured after 12 to 28 days by Lowenstein-Jensen method2021European journal of medicinal chemistry, Apr-05, Volume: 215Antitubercular properties of thiazolidin-4-ones - A review.
AID396048Antitubercular activity against Mycobacterium tuberculosis H37Rv after 5 to 8 days2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, anti-tubercular activity and 3D-QSAR study of coumarin-4-acetic acid benzylidene hydrazides.
AID572061Ratio of MIC for Acinetobacter baumannii AC0037 to MIC for abeS-deficient Acinetobacter baumannii AC00372009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID1879559Antibacterial activity against Fusobacterium nucleatum ATCC 109532022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID510519Cmax in tuberculosis patient at 10 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1288637Antituberculosis activity against Mycobacterium tuberculosis H37Rv in glycerol-alanine salts medium incubated for 4 days by Microplate Alamar Blue assay2016MedChemComm, Jan-01, Volume: 7, Issue:1
Syntheses and Biological Evaluations of Highly Functionalized Hydroxamate Containing and
AID1678510Antibacterial activity against Clostridium difficile BAA-1875 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID531046Antimicrobial activity against Clostridium difficile isolate 13 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID571200Antibacterial activity against Escherichia coli ATCC 25992 by Etest method in presence of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1179479Antimycobacterial activity against Mycobacterium chelonae ATCC 35752 in 7H9 medium after 3 days and 4 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID1193923Cytotoxicity against mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID566040Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assat2011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and in vitro antimycobacterial activity of 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives.
AID701628Activation of CYP3A4 expressed in DPX cells co-transfected with human PXR at 10 uM2012Journal of medicinal chemistry, Aug-23, Volume: 55, Issue:16
Identification of a potent sodium hydrogen exchanger isoform 1 (NHE1) inhibitor with a suitable profile for chronic dosing and demonstrated cardioprotective effects in a preclinical model of myocardial infarction in the rat.
AID1491509Genotoxicity in Salmonella typhimurium TA104 harboring RecN2-4 lux operon fusion at 1.28 to 128 uM measured every 5 mins for 4 hrs in absence of S9 liver fraction by vitotox assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID588210Human drug-induced liver injury (DILI) modelling dataset from Ekins et al2010Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 38, Issue:12
A predictive ligand-based Bayesian model for human drug-induced liver injury.
AID510528Ratio of apparent clearance in diabetic tuberculosis patient to apparent clearance in tuberculosis patient2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1070191Antimycobacterial activity against Mycobacterium scrofulaceum MNT1193 clinical isolate by MTT assay2014European journal of medicinal chemistry, Mar-03, Volume: 74Microwave induced three-component synthesis and antimycobacterial activity of benzopyrazolo[3,4-b]quinolindiones.
AID293582Antibacterial activity against Klebsiella pneumoniae isolate assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID1856877Antimicrobial activity against Escherichia coli ATCC 25922 in presence of MgCl22022Journal of medicinal chemistry, 10-27, Volume: 65, Issue:20
Improving the Antimicrobial Performance of Amphiphilic Cationic Antimicrobial Peptides Using Glutamic Acid Full-Scan and Positive Charge Compensation Strategies.
AID1185710Antibacterial activity against Staphylococcus aureus ATCC 6538 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1193922Antibacterial activity against multidrug-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015Bioorganic & medicinal chemistry, Apr-01, Volume: 23, Issue:7
Development of 2-amino-5-phenylthiophene-3-carboxamide derivatives as novel inhibitors of Mycobacterium tuberculosis DNA GyrB domain.
AID1570245Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 1 incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID425408Antibacterial activity against Escherichia coli K-12 after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID545921Antimicrobial activity against Escherichia coli IH3080 by Etest method in presence of 4 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID1634852Antitubercular activity against XDR Mycobacterium tuberculosis X24 incubated for 1 to 9 days by inverted microscopic analysis2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Antituberculosis Activity of a Naturally Occurring Flavonoid, Isorhamnetin.
AID560224Antibacterial activity against Salmonella enterica serovar Typhimurium R200 expressing stm3031 gene deletion mutant by CLSI M7-A7 agar dilution method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Outer membrane protein STM3031 (Ail/OmpX-like protein) plays a key role in the ceftriaxone resistance of Salmonella enterica serovar Typhimurium.
AID292420Antitubercular activity against Mycobacterium tuberculosis SS102007Bioorganic & medicinal chemistry letters, Sep-01, Volume: 17, Issue:17
[1,2,3]Triazolo[4,5-h]quinolones. A new class of potent antitubercular agents against multidrug resistant Mycobacterium tuberculosis strains.
AID434069Immunomodulatory effect in human A549 cells assessed as inhibition of Ca2+ ionophore A23187 stimulated-[3H]arachidonic acid release measured after 45 mins of A23187 challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID530797Antimicrobial activity against Clostridium difficile isolate 28 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1888139Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis clinical isolate HD5 assessed as inhibition of bacterial growth incubated for 7 days by by microplate alamar blue assay2022European journal of medicinal chemistry, Jan-05, Volume: 227Exploring disordered loops in DprE1 provides a functional site to combat drug-resistance in Mycobacterium strains.
AID528949Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 5 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID1716715Antibacterial activity against Pseudomonas aeruginosa 264-101354 assessed as fractional inhibitory concentration index in presence of chloramphenicol incubated for 18 hrs by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID425406Antibacterial activity against mucosa-associated Escherichia coli isolate HM454 isolated from patient with irritable bowel syndrome or sporadic polyps after 24 hrs by Etest antibiotic concentration gradient method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Replication of Colonic Crohn's Disease Mucosal Escherichia coli Isolates within Macrophages and Their Susceptibility to Antibiotics.
AID1300865Cytotoxicity against HEK293T cells assessed as cell viability at 50 ug/ml after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry letters, 06-01, Volume: 26, Issue:11
Synthesis, biological evaluation and structure-activity relationship of 2-styrylquinazolones as anti-tubercular agents.
AID650748Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 5 days by microplate alamar blue assay2012Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5
Novel imidazo[2,1-b][1,3,4]thiadiazole carrying rhodanine-3-acetic acid as potential antitubercular agents.
AID293590Antibacterial activity against Bacillus subtilis ATCC 6633 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID706036Antimicrobial effect against 3x10'9 CFU/ml methicillin-sensitive Staphylococcus aureus 8325-4 at 4 to 32 times MIC assessed as incidence of colonies growth measured after 24 incubation by large inoculation approach based drug resistance detection method2012Journal of medicinal chemistry, Nov-26, Volume: 55, Issue:22
A bactericidal guanidinomethyl biaryl that alters the dynamics of bacterial FtsZ polymerization.
AID348182Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for non-replicating Mycobacterium tuberculosis2009Bioorganic & medicinal chemistry, Jan-15, Volume: 17, Issue:2
Synthesis and evaluation of rifabutin analogs against Mycobacterium avium and H(37)Rv, MDR and NRP Mycobacterium tuberculosis.
AID1069170Antimicrobial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv SRI 1369 assessed as growth inhibition at MIC after 7 days by broth microdilution assay relative to control2014European journal of medicinal chemistry, Feb-12, Volume: 73Design, synthesis and evaluation of acridine and fused-quinoline derivatives as potential anti-tuberculosis agents.
AID1163980Antimycobacterial activity against isoniazid, rifampicin, ofloxacin and kanamycin-resistant Mycobacterium tuberculosis H37Rv ATCC 27294 clinical isolate after 28 days by two-fold serial dilution assay in presence of 8 mg/mL piperine efflux pump inhibitor2014European journal of medicinal chemistry, Oct-30, Volume: 86Development of 2-(4-oxoquinazolin-3(4H)-yl)acetamide derivatives as novel enoyl-acyl carrier protein reductase (InhA) inhibitors for the treatment of tuberculosis.
AID1627523Antibacterial activity against Mycobacterium avium assessed as reduction in bacterial metabolic activity after 5 days by Alamar blue assay2016ACS medicinal chemistry letters, Jul-14, Volume: 7, Issue:7
Dehydrozingerone Inspired Styryl Hydrazine Thiazole Hybrids as Promising Class of Antimycobacterial Agents.
AID531000Antimicrobial activity against Clostridium difficile isolate 47 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1071089Antimycobacterial activity against Mycobacterium tuberculosis H37Rv SRI 1345 infected in mouse J774A1 cells assessed as reduction in bacterial growth at 0.01 ug/ml after 7 days relative to control2014European journal of medicinal chemistry, Mar-03, Volume: 74Antimycobacterial activity of nitrogen heterocycles derivatives: bipyridine derivatives. Part III.
AID1061124Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 4 days by microplate Alamar blue assay2014Bioorganic & medicinal chemistry, Jan-01, Volume: 22, Issue:1
Synthesis of 3-(3-aryl-pyrrolidin-1-yl)-5-aryl-1,2,4-triazines that have antibacterial activity and also inhibit inorganic pyrophosphatase.
AID571436Antibacterial activity against Escherichia coli IH3080 by Etest method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID565788Antimicrobial activity against Neisseria meningitidis harboring rpoB32 H552Y mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID405158Apparent clearance in tuberculosis patient at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID1565595Antibacterial activity against methicillin-resistant Staphylococcus aureus 936 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID1212151Induction of CYP2C8 mRNA expression in human hepatocytes at 10 uM after 72 hrs by RT-PCR analysis relative to vehicle-treated control2012Drug metabolism and disposition: the biological fate of chemicals, Sep, Volume: 40, Issue:9
Evaluation of P450 inhibition and induction by artemisinin antimalarials in human liver microsomes and primary human hepatocytes.
AID428624Antitubercular activity against Mycobacterium tuberculosis H37Rv at 6.25 mg by microplate alamar blue assay2009European journal of medicinal chemistry, Jul, Volume: 44, Issue:7
SAR study of clubbed [1,2,4]-triazolyl with fluorobenzimidazoles as antimicrobial and antituberculosis agents.
AID1210920Ratio Vmax to Km in human recombinant AADAC2012Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 40, Issue:4
Species differences in tissue distribution and enzyme activities of arylacetamide deacetylase in human, rat, and mouse.
AID422125Antimicrobial activity against Mycobacterium tuberculosis H37Rv by microplate Alamar blue assay2009Journal of natural products, May-22, Volume: 72, Issue:5
Antimicrobial ambiguine isonitriles from the cyanobacterium Fischerella ambigua.
AID1668180Antibacterial activity against Escherichia coli ATCC 25922 assessed as bacterial growth inhibition2020Bioorganic & medicinal chemistry letters, 06-01, Volume: 30, Issue:11
Design, synthesis and biological evaluation of novel hybrids of N-aryl pyrrothine-base α-pyrone as bacterial RNA polymerase inhibitors.
AID1552791Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay2019Bioorganic & medicinal chemistry letters, 09-01, Volume: 29, Issue:17
Discovery and evaluation of novel nitrodihydroimidazooxazoles as promising anti-tuberculosis agents.
AID571441Antibacterial activity against Escherichia coli IH3080 by Etest method in presence of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1447482Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P262-101856 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1565590Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by CLSI based broth microdilution method2019European journal of medicinal chemistry, Nov-15, Volume: 182Design and synthesis of new N-terminal fatty acid modified-antimicrobial peptide analogues with potent in vitro biological activity.
AID1219162Inhibition of OATP1B3 (unknown origin) expressed in HEK293 cells assessed as reduction of [3H]CCK8 substrate uptake at 100 uM by liquid scintillation counting2013Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 41, Issue:1
Evaluation and prediction of potential drug-drug interactions of linagliptin using in vitro cell culture methods.
AID326280Antibacterial activity against methicillin-resistant Staphylococcus aureus 4803 at 4 hrs daily exposure for 1 day by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID544820Antimicrobial activity against Staphylococcus epidermidis Xen 43 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID572537AUC (0 to 12 hrs) in kenyan pulmonary tuberculosis patient coinjected with HIV with body weight >45 kg at 600 mg/day, po2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID634273Antimycobacterial activity against Mycobacterium tuberculosis isolate 359 expressing wild-type rpoB gene by resazurin microtiter assay2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Pharmacophore insights into rpoB gene mutations in Mycobacterium tuberculosis rifampicin resistant isolates.
AID1311284Selectivity index, ratio of CC50 for human PANC1 cells to MIC for dormant stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1471054Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 25177 dormant stage2017European journal of medicinal chemistry, May-26, Volume: 132Synthesis and antimycobacterial screening of new thiazolyl-oxazole derivatives.
AID416840Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load per culture-positive foot-pad at 10 mg/kg, po administered for 5 days per week measured after 4 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID389103Selectivity index, ratio of IC50 for against african green monkey VERO cells to MIC for Mycobacterium tuberculosis H37Rv2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID474492Biodistribution in human brain at 600 mg administered by infusion after 3 to 7 hrs2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Radiosynthesis and bioimaging of the tuberculosis chemotherapeutics isoniazid, rifampicin and pyrazinamide in baboons.
AID145296Tested for antibacterial activity against Mycobacterium tuberculosis H37Rv kanamycin resistant strain1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Synthesis and antibacterial activity of 2,2'-dithiobis(benzamide) derivatives against Mycobacterium species.
AID532969Antimicrobial activity against Mycobacterium tuberculosis isolate 13 isolated from Beijing2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID554581Antibacterial activity against Staphylococcus aureus E19977 infected in NMRI mouse assessed as log reduction in bacterial cfu in peritoneum at 60 mg/kg, sc administered as single dose 2 hrs after infection measured upto 19 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID545908Antimicrobial activity against Escherichia coli ATCC 25922 in presence of 2 ug/ml NAB7412010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
A novel polymyxin derivative that lacks the fatty acid tail and carries only three positive charges has strong synergism with agents excluded by the intact outer membrane.
AID765112Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
Inhibition of Mycobacterium tuberculosis strains H37Rv and MDR MS-115 by a new set of C5 modified pyrimidine nucleosides.
AID1253867Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis FJ05195 after 3 to 4 weeks by microplate alamar blue assay2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Discovery of the disubstituted oxazole analogues as a novel class anti-tuberculotic agents against MDR- and XDR-MTB.
AID1905561Antimicrobial activity against Staphylococcus aureus ATCC 25923 assessed as reduction of bacterial growth incubated for 18 hrs by CLSI protocol based broth microdilution method2022Journal of medicinal chemistry, 04-14, Volume: 65, Issue:7
Novel β-Hairpin Antimicrobial Peptides Containing the β-Turn Sequence of -RRRF- Having High Cell Selectivity and Low Incidence of Drug Resistance.
AID1332979Selectivity index, ratio of IC50 for human MRC5 cells to MIC90 for Mycobacterium tuberculosis H37Rv ATCC 272942016European journal of medicinal chemistry, Nov-10, Volume: 123Synthesis and biological activity of furoxan derivatives against Mycobacterium tuberculosis.
AID581658Cmax in human plasma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1491511Genotoxicity in Salmonella typhimurium TA104 harboring Pr1 lux operon fusion at 1.28 to 128 uM measured every 5 mins for 4 hrs in absence of S9 liver fraction by vitotox assay2017European journal of medicinal chemistry, Sep-29, Volume: 138Design, synthesis and antitubercular potency of 4-hydroxyquinolin-2(1H)-ones.
AID283156Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2394 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID529537Antimycobacterial activity against Mycobacterium tuberculosis isolate NJT210 expressing embB codon 306 ATC-ATG mutant at 37 degC after 10 to 11 days by radiometric Bactec 460TB method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Transfer of embB codon 306 mutations into clinical Mycobacterium tuberculosis strains alters susceptibility to ethambutol, isoniazid, and rifampin.
AID257539Antitubercular activity against Mycobacterium tuberculosis H37Rv by standard BACTEC radiometric growth assay2005Bioorganic & medicinal chemistry letters, Dec-01, Volume: 15, Issue:23
Synthesis and antitubercular activity of 2-hydroxy-aminoalkyl derivatives of diaryloxy methano phenanthrenes.
AID1562302Antimycobacterial activity against Mycobacterium smegmatis atR37 assessed as decrease in drug resistance development at 100 ug/disc after 2 to 3 days by paper disc method2019European journal of medicinal chemistry, Sep-15, Volume: 178Synthesis and antimycobacterial activity of imidazo[1,2-b][1,2,4,5]tetrazines.
AID1395196Antitubercular activity against multi-drug resistant Mycobacterium tuberculosis isolate 16995 after 7 days by Alamar blue assay2018European journal of medicinal chemistry, May-10, Volume: 151Design, synthesis and antitubercular evaluation of benzothiazinones containing a piperidine moiety.
AID570583Apparent volume of distribution in pulmonary tuberculosis patient in first order model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID452746Antibacterial activity against fabI-overexpressing Escherichia coli M152010Bioorganic & medicinal chemistry letters, Jan-01, Volume: 20, Issue:1
Novel enoyl-ACP reductase (FabI) potential inhibitors of Escherichia coli from Chinese medicine monomers.
AID669181Inhibition of Mycobacterium tuberculosis RNA polymerase D435V mutant by rolling circle transcription assay in the absence of sigmaA factor2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID1916815Antimycobacterial activity against Mycobacterium tuberculosis H37Ra incubated for 8 to 12 days by XTT reduction menadione assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID545053Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ372 from patient sputum by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID1483712Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by turbidometric method2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID576110Antimicrobial activity against mecA-positive Staphylococcus sciuri assessed as resistant isolates2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Nasal carriage of methicillin-resistant and methicillin-sensitive strains of Staphylococcus sciuri in the Indonesian population.
AID625288Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for jaundice2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID510966Antibacterial activity against Acinetobacter baumannii 1327 infected in New Zealand rabbit meningitis model assessed as reduction in bacterial count in CSF at 25 mg/kg, iv measured after 4 hrs of last dose (RVb = 5.2 No_unit)2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Efficacy of rifampin and its combinations with imipenem, sulbactam, and colistin in experimental models of infection caused by imipenem-resistant Acinetobacter baumannii.
AID1784358Antimycobacterial activity against Mycobacterium tuberculosis DprE1 Y314C in presence of middlebrook 7H9/glucose/BSA/tyloxapol medium measured for 2 weeks by bioluminescence reporter assay2021Journal of medicinal chemistry, 09-09, Volume: 64, Issue:17
1,3-Diarylpyrazolyl-acylsulfonamides as Potent Anti-tuberculosis Agents Targeting Cell Wall Biosynthesis in
AID496819Antimicrobial activity against Plasmodium falciparum2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Multi-target spectral moment QSAR versus ANN for antiparasitic drugs against different parasite species.
AID681167TP_TRANSPORTER: Northern blot from LS174T cell2001The Journal of biological chemistry, May-04, Volume: 276, Issue:18
Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin.
AID424421Antibacterial activity against Enterococcus faecalis HIP14333 isolated from patients rectum by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID1827049Antibacterial activity against Klebsiella pneumoniae ATCC 700603 assessed as bacterial growth inhibition incubated for 18 to 20 hrs by broth microdilution method2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Potent Bactericidal Antimycobacterials Targeting the Chaperone ClpC1 Based on the Depsipeptide Natural Products Ecumicin and Ohmyungsamycin A.
AID1833911Antimycobacterial activity against Mycobacterium marinum infected in zebrafish assessed as reduction in bacterial burden at 100 uM after 5 days post infection by microscopic analysis2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Synthetic Sansanmycin Analogues as Potent
AID589951Antimicrobial activity against Mycobacterium tuberculosis H37Rv after 48 hrs by resazurin microplate broth microdilution method2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Design, synthesis and antimycobacterial activity of cinnamide derivatives: a molecular hybridization approach.
AID776896Antibacterial activity against Escherichia coli K-122013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Discovery of novel bacterial RNA polymerase inhibitors: pharmacophore-based virtual screening and hit optimization.
AID535771Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60H carrying the luxAB gene under the hsp60 promoter agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID1364753Antibiofilm activity against Mycobacterium tuberculosis assessed as log reduction in bacterial count at 10 ug/ml measured after 7 days by MPN assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID1687473Antitubercular activity against INH-resistant Mycobacterium tuberculosis Spec.800 harboring InhA promoter mutation assessed as inhibition of microbial growth incubated for 1 week by MABA method2020European journal of medicinal chemistry, Jan-15, Volume: 186Development of (4-methoxyphenyl)-1H-tetrazol-5-amine regioisomers as a new class of selective antitubercular agents.
AID531272Antimicrobial activity against Clostridium difficile isolate 44 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1852583Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 7 days by MABA
AID531007Antimicrobial activity against Clostridium difficile isolate 54 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID341070Half life in human at 600 mg, po once daily after 14 days coadministered with moxifloxacin at 400 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID774191Antitubecular activity against Mycobacterium tuberculosis H37Pv assessed as growth inhibition by low oxygen recovery assay2013Journal of natural products, Oct-25, Volume: 76, Issue:10
Phomapyrrolidones A-C, antitubercular alkaloids from the endophytic fungus Phoma sp. NRRL 46751.
AID1174112Antimycobacterial activity against isoniazid, rifampin-resistant Mycobacterium tuberculosis after 7 days by microplate Alamar blue assay2015European journal of medicinal chemistry, Jan-07, Volume: 89Antimycobacterial activity of natural products and synthetic agents: pyrrolodiquinolines and vermelhotin as anti-tubercular leads against clinical multidrug resistant isolates of Mycobacterium tuberculosis.
AID1423472Inhibition of refolded rhodanese (unknown origin) preincubated with Escherichia coli GroEL/GroES for 60 mins in absence of compound followed by compound addition by spectrometric analysis2018Journal of medicinal chemistry, 12-13, Volume: 61, Issue:23
Hydroxybiphenylamide GroEL/ES Inhibitors Are Potent Antibacterials against Planktonic and Biofilm Forms of Staphylococcus aureus.
AID424422Antibacterial activity against vancomycin-resistant Staphylococcus aureus HIP15178 isolated from patients surgical wound by broth microdilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Vancomycin-resistant Staphylococcus aureus isolates associated with Inc18-like vanA plasmids in Michigan.
AID514968Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 microplate alamar blue assay2010European journal of medicinal chemistry, Oct, Volume: 45, Issue:10
Synthesis and antimycobacterial activity of new quinoxaline-2-carboxamide 1,4-di-N-oxide derivatives.
AID293588Antibacterial activity against Pseudomonas aeruginosa ATCC 25853 assessed after 24 hrs by serial dilution method2007Bioorganic & medicinal chemistry, Mar-01, Volume: 15, Issue:5
Synthesis and biological evaluation of new N-(2-hydroxy-4(or 5)-nitro/aminophenyl)benzamides and phenylacetamides as antimicrobial agents.
AID445931Selectivity index, ratio of IC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942010Journal of medicinal chemistry, Jan-28, Volume: 53, Issue:2
Identification, synthesis, and pharmacological evaluation of tetrahydroindazole based ligands as novel antituberculosis agents.
AID531258Antimicrobial activity against Clostridium difficile isolate 30 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID531049Antimicrobial activity against Clostridium difficile isolate 16 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1316917Inhibition of Mycobacterium tuberculosis ADH assessed as decrease in conversion of L-alanine to pyruvate by measuring NADH by spectrophotometry2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID309276Antitubercular activity against Mycobacterium tuberculosis H37Rv by MABA assay2007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Design, synthesis and antitubercular activity of diarylmethylnaphthol derivatives.
AID1400027Selectivity index, ratio of IC50 for African green monkey Vero cells to MIC100 for replicating Mycobacterium tuberculosis H37Rv by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID565784Antimicrobial activity against Neisseria meningitidis harboring rpoB19 S557F mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID530345Antimicrobial activity against Escherichia coli BicA expressing blaTEM-1, blaCTX-M-15 and qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID428292Antimicrobial activity against Acinetobacter baumannii BM4579 expressing deltaadeIJK genes isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID697853Inhibition of horse BChE at 2 mg/ml by Ellman's method2012Bioorganic & medicinal chemistry, Nov-15, Volume: 20, Issue:22
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
AID1143685Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 infected in Balb/c mouse assessed as reduction in bacterial load in lung at 100 mg/kg, po qd administered five days in a week starting 2 weeks post challenge measured after 6 w2014European journal of medicinal chemistry, Jun-23, Volume: 81Synthesis of novel 1,2,3-triazole derivatives of isoniazid and their in vitro and in vivo antimycobacterial activity evaluation.
AID559090Antimicrobial activity against carbapenem-resistant Acinetobacter baumannii isolate A2 by Etest method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
In vivo selection of reduced susceptibility to carbapenems in Acinetobacter baumannii related to ISAba1-mediated overexpression of the natural bla(OXA-66) oxacillinase gene.
AID545052Antibacterial activity against hospital-acquired methicillin-resistant Staphylococcus aureus clinical isolate BJ363 from patient secretion by agar dilution method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Molecular evidence for spread of two major methicillin-resistant Staphylococcus aureus clones with a unique geographic distribution in Chinese hospitals.
AID396036Antibacterial activity against drug-resistant AcrAB-TolC efflux pump deficient Enterobacter cloacae EcdeltaacrA isolate by standard disk diffusion method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Cloning, nucleotide sequencing, and analysis of the AcrAB-TolC efflux pump of Enterobacter cloacae and determination of its involvement in antibiotic resistance in a clinical isolate.
AID571656Ratio of the MIC for Klebsiella oxytoca CCUG51683 in the absence of NAB7066 to MIC for Klebsiella oxytoca CCUG51683 in the presence of 4 ug/ml of NAB70662008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID588131Antibacterial activity against carbapenem-resistant Klebsiella pneumoniae isolate 2 expressing beta-lactamase NDM-1 obtained from urine of patient by liquid microdilution method2011Antimicrobial agents and chemotherapy, Feb, Volume: 55, Issue:2
Detection of NDM-1-producing Klebsiella pneumoniae in Kenya.
AID405160Tmax in tuberculosis patient at 600 mg, po2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Pharmacokinetics and tolerability of a higher rifampin dose versus the standard dose in pulmonary tuberculosis patients.
AID541050Ratio of AUC (0 to 24 hrs) to MIC for methicillin-resistant Staphylococcus aureus ATCC 43300 in Albino guiena pig model of foreign-body infection at 12.5 mg/kg, ip2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Linezolid alone or combined with rifampin against methicillin-resistant Staphylococcus aureus in experimental foreign-body infection.
AID1185711Antibacterial activity against Staphylococcus epidermidis ATCC 12228 after 18 hrs by serial microdilution method2014European journal of medicinal chemistry, Sep-12, Volume: 84Structure and evaluation of antibacterial and antitubercular properties of new basic and heterocyclic 3-formylrifamycin SV derivatives obtained via 'click chemistry' approach.
AID1235589Antimycobacterial activity against Mycobacterium avium subsp. paratuberculosis isolate CIT03 assessed as reduction in bacterial growth incubated at 37 degC for 11 days by alamar blue dye based assay2015Bioorganic & medicinal chemistry, Aug-01, Volume: 23, Issue:15
Ring-substituted 8-hydroxyquinoline-2-carboxanilides as potential antimycobacterial agents.
AID620090Antimicrobial activity against Mycobacterium fortuitum ATCC 19542 after 7 days by resazurin assay2011European journal of medicinal chemistry, Oct, Volume: 46, Issue:10
Design, synthesis and docking studies of quinoline-oxazolidinone hybrid molecules and their antitubercular properties.
AID1181155Antimicrobial activity against clinical isolate Mycobacterium tuberculosis ATCC25618 assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID373033Antimicrobial activity against imipenem and meropenem-resistant Acinetobacter baumannii isolate BJ3-23 by CLSI agar dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Molecular epidemiology of clinical isolates of carbapenem-resistant Acinetobacter spp. from Chinese hospitals.
AID1716705Antibacterial activity against Pseudomonas aeruginosa 100036 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID481725Cytotoxicity against african green monkey Vero cells by colorimetric assay2010European journal of medicinal chemistry, May, Volume: 45, Issue:5
Structure-activity relationship of new anti-tuberculosis agents derived from oxazoline and oxazole benzyl esters.
AID625291Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for liver function tests abnormal2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1174924Antitubercular activity against Mycobacterium tuberculosis isolate 439/11 after 7 days by REMA resazurin microtiter assay2014Bioorganic & medicinal chemistry, Dec-15, Volume: 22, Issue:24
Antitubercular activity of quinolizidinyl/pyrrolizidinylalkyliminophenazines.
AID571445Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by Etest method in presence of 4 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1483731Selectivity ratio of MIC for Mycobacterium tuberculosis H37Rv harboring ATP synthase subunit-c D28N mutant supplemented with 8 fold MIC of 3-(4-Morpholinophenyl)-4-((pyridin-2-ylmethyl)amino)cyclobut-3-ene-1,2-dione to MIC for Mycobacterium tuberculosis H2017Journal of medicinal chemistry, 02-23, Volume: 60, Issue:4
Discovery of Imidazo[1,2-a]pyridine Ethers and Squaramides as Selective and Potent Inhibitors of Mycobacterial Adenosine Triphosphate (ATP) Synthesis.
AID1765351Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition after 7 days by broth microdilution assay2021European journal of medicinal chemistry, Oct-15, Volume: 222Synthesis and structure-activity relationship of new chalcone linked 5-phenyl-3-isoxazolecarboxylic acid methyl esters potentially active against drug resistant Mycobacterium tuberculosis.
AID1516026Antibacterial activity against Acinetobacter baumannii AB1901 clinical isolate incubated for 18 to 24 hrs by broth microdilution method2019Journal of medicinal chemistry, 08-08, Volume: 62, Issue:15
Design of Trp-Rich Dodecapeptides with Broad-Spectrum Antimicrobial Potency and Membrane-Disruptive Mechanism.
AID1736313Antitubercular activity against INH, SM, RFP, EMB, RBT, PAS, OLFX-resistant Mycobacterium tuberculosis 13946 assessed as inhibition of bacterial growth2020European journal of medicinal chemistry, Mar-01, Volume: 189Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis.
AID276753Antimycobacterial activity against streptomycin resistant Mycobacterium tuberculosis ATCC 358202006Bioorganic & medicinal chemistry letters, Nov-15, Volume: 16, Issue:22
New rifabutin analogs: synthesis and biological activity against Mycobacterium tuberculosis.
AID1293910Selectivity index, ratio of GI50 for human A549 cells to MIC for Mycobacterium tuberculosis H37Ra ATCC 251772016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Novel tetrazoloquinoline-rhodanine conjugates: Highly efficient synthesis and biological evaluation.
AID1463952Antimycobacterial activity against Mycobacterium tuberculosis H37Rv CNCTC My 331/88 incubated for 14 days by micromethod2017Bioorganic & medicinal chemistry, 10-15, Volume: 25, Issue:20
Development of water-soluble 3,5-dinitrophenyl tetrazole and oxadiazole antitubercular agents.
AID1743133Inhibition of ATP synthase in multi-drug resistant Mycobacterium tuberculosis clinical isolate 13946 assessed as reduction in bacterial growth incubated for 7 days by microplate alamar blue assay2020European journal of medicinal chemistry, Nov-15, Volume: 206Design, synthesis and biological evaluation of diamino substituted cyclobut-3-ene-1,2-dione derivatives for the treatment of drug-resistant tuberculosis.
AID681334TP_TRANSPORTER: transepithelial transport in Caco 2 cell2004Pharmaceutical research, May, Volume: 21, Issue:5
Predicting P-glycoprotein effects on oral absorption: correlation of transport in Caco-2 with drug pharmacokinetics in wild-type and mdr1a(-/-) mice in vivo.
AID326298Antibacterial activity against methicillin-resistant Staphylococcus aureus 293 at 4 hrs daily exposure for 5 days by broth microdilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Comparative activities of daptomycin, linezolid, and tigecycline against catheter-related methicillin-resistant Staphylococcus bacteremic isolates embedded in biofilm.
AID489576Antimycobacterial activity against Mycobacterium kansasii 6509/96 after 14 days by microdilution method2010European journal of medicinal chemistry, Jul, Volume: 45, Issue:7
A note to the biological activity of benzoxazine derivatives containing the thioxo group.
AID388901Antimycobacterial activity against Mycobacterium tuberculosis H37Rv at 8 ug/mL by microplate alamar blue assay2008Bioorganic & medicinal chemistry letters, Oct-15, Volume: 18, Issue:20
Synthesis and in vitro biological evaluation of ring B abeo-sterols as novel inhibitors of Mycobacterium tuberculosis.
AID572535Apparent oral clearance in pulmonary tuberculosis patient in Sequential 0 order and first order model2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Population pharmacokinetics of rifampin in pulmonary tuberculosis patients, including a semimechanistic model to describe variable absorption.
AID252250Selectivity ratio for IC50 of VERO cells to that of MIC of Mycobacterium tuberculosis H37Rv2005Bioorganic & medicinal chemistry letters, Sep-15, Volume: 15, Issue:18
Identification of heteroarylenamines as a new class of antituberculosis lead molecules.
AID301528Antibacterial activity against rifamycin-resistance Staphylococcus aureus CB3702007Bioorganic & medicinal chemistry letters, Oct-15, Volume: 17, Issue:20
Preparation and in vitro anti-staphylococcal activity of novel 11-deoxy-11-hydroxyiminorifamycins.
AID495518Antibacterial activity against multidrug-resistant Acinetobacter baumannii BM4676 by antimicrobial susceptibility assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Screening and quantification of the expression of antibiotic resistance genes in Acinetobacter baumannii with a microarray.
AID1869524Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC29213 measured after 24 hrs by broth microdilution method
AID434064Immunomodulatory effect in human A549 cells assessed as reduction in IL-1-beta-induced [3H]arachidonic acid release at 50 ug/ml measured after 6 hrs of IL1-beta challenge by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID377696Antimalarial activity after 72 hrs against chloroquine-resistant Plasmodium falciparum W2 in erythrocytes by LDH reporter assay2006Journal of natural products, Jul, Volume: 69, Issue:7
Manzamine B and E and ircinal A related alkaloids from an Indonesian Acanthostrongylophora sponge and their activity against infectious, tropical parasitic, and Alzheimer's diseases.
AID571444Antibacterial activity against Klebsiella pneumoniae ATCC 13883 by Etest method in presence of 2 ug/ml NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID531281Antimicrobial activity against Clostridium difficile isolate 53 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID611485Antibacterial activity against Staphylococcus aureus RN4220 after 18 hrs by microtiter plate reader assay2011Journal of natural products, Jun-24, Volume: 74, Issue:6
Chaxamycins A-D, bioactive ansamycins from a hyper-arid desert Streptomyces sp.
AID1426436Antimycobacterial activity against Mycobacterium tuberculosis MC2 7000 by microplate alamar blue assay2017European journal of medicinal chemistry, Feb-15, Volume: 127Synthesis and SAR evaluation of novel thioridazine derivatives active against drug-resistant tuberculosis.
AID1316919Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell proliferation at 50 ug/ml after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID1658971Antibacterial activity against Staphylococcus aureus ATCC 29213 after 20 hrs by CLSI based-broth microdilution method2020Journal of medicinal chemistry, 07-23, Volume: 63, Issue:14
Discovery of Antibacterials That Inhibit Bacterial RNA Polymerase Interactions with Sigma Factors.
AID531027Antimicrobial activity against Clostridium difficile isolate 74 by agar dilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1055966Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate X001354 under normoxic condition after 7 days by MABA assay2013Journal of natural products, Nov-22, Volume: 76, Issue:11
Hytramycins V and I, anti-Mycobacterium tuberculosis hexapeptides from a Streptomyces hygroscopicus strain.
AID400491Inhibition of AAH in Sprague-Dawley rat intestine microsomes assessed as enzyme activity using benzo(a)pyrene as substrate at 0.05 mM relative to control1983Journal of natural products, Jan, Volume: 46, Issue:1
Non-competitive inhibition of hepatic and intestinal aryl hydrocarbon hydroxylase activities from rats by rifampin.
AID1303893Antibacterial activity against multidrug resistant Klebsiella pneumoniae subsp. pneumoniae NCTC 9633 (ATCC 13883) assessed as reduction in bacterial growth incubated for 6 to 8 hrs2016Bioorganic & medicinal chemistry letters, 07-01, Volume: 26, Issue:13
GroEL/ES inhibitors as potential antibiotics.
AID528948Bactericidal activity against Mycobacterium tuberculosis in pulmonary tuberculosis patient assessed as reduction in sputum bacterial count at 600 mg/kg, po once daily measured after 4 days2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Early bactericidal activity and pharmacokinetics of the diarylquinoline TMC207 in treatment of pulmonary tuberculosis.
AID531277Antimicrobial activity against Clostridium difficile isolate 49 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID434067Immunomodulatory effect in human A549 cells assessed as reduction in basal release of [3H]arachidonic acid at 50 ug/ml up to 19 hrs by liquid scintillation counting2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Rifampin inhibits prostaglandin E2 production and arachidonic acid release in human alveolar epithelial cells.
AID1209534Activation of human PXR expressed in rat hepatocytes coexpressing CYP3A4 at 10 uM after 24 hrs by dual luciferase reporter gene assay relative to control2012Drug metabolism and disposition: the biological fate of chemicals, Jan, Volume: 40, Issue:1
Species-dependent and receptor-selective action of bilobalide on the function of constitutive androstane receptor and pregnane X receptor.
AID373960Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis H37Rv ATCC 2517-infected hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model assessed as rate constant for maximal bacterial growth2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID1333153Induction of membrane damage in CI/DOPG/DOPI large unilamellar vesicles assessed as calcein leakage at compound to lipid ratio of 1:2 to 1:8 by fluorescence based total phosphorous determination assay relative to control2016European journal of medicinal chemistry, Nov-10, Volume: 123Amphiphilic xanthones as a potent chemical entity of anti-mycobacterial agents with membrane-targeting properties.
AID297114Antibacterial activity against Mycobacterium avium Flamingo after 18 hrs by agar plate dilution method2007Journal of medicinal chemistry, Aug-23, Volume: 50, Issue:17
Discovery of 1,4-dihydroxy-2-naphthoate [corrected] prenyltransferase inhibitors: new drug leads for multidrug-resistant gram-positive pathogens.
AID392602Antimycobacterial activity against Mycobacterium fortuitum MTCC 951 by agar dilution method2009Bioorganic & medicinal chemistry letters, Feb-15, Volume: 19, Issue:4
5-Nitrofuran-2-yl derivatives: synthesis and inhibitory activities against growing and dormant mycobacterium species.
AID683731Antimalarial activity against liver stages of Plasmodium yoelii 17XNL expressing GFP infected in human HepG2 cells transfected with CD81 assessed as growth inhibition of hepatic parasite after 40 hrs by flow cytometry2012Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3
Targeting the liver stage of malaria parasites: a yet unmet goal.
AID1400044Antibacterial activity against Staphylococcus aureus BAA 44 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID373944Ratio of AUC (0 to 24 hrs) to MIC for Mycobacterium tuberculosis H37Rv ATCC 2517 in hollow fiber system based in vitro pharmacokinetic-pharmacodynamic tuberculosis model administered at simulated dose of 600 mg/day for 7 days2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Concentration-dependent Mycobacterium tuberculosis killing and prevention of resistance by rifampin.
AID541032Antiproliferative activity against Theileria parva-induced proliferation of bovine B lymphocyte assessed as inhibition of [3H]thymidine uptake after 48 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Theileria apicoplast as a target for chemotherapy.
AID555306Antibacterial activity against methicillin-susceptible coagulase-negative Staphylococcus epidermidis 051 by broth macrodilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Antistaphylococcal activity of dihydrophthalazine antifolates, a family of novel antibacterial drugs.
AID404126Inhibition of type II fatty acid synthesis in Staphylococcus aureus using n-octanoyl-CoA and [14C]malonyl CoA substrate2005Journal of natural products, Sep, Volume: 68, Issue:9
Anthrabenzoxocinones from Streptomyces sp. as liver X receptor ligands and antibacterial agents.
AID1181165Antimicrobial activity against clinical isolate Isoniazid-resistant Mycobacterium tuberculosis assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1210067Induction of CYP2B6 activity in human donor hepatocytes assessed as hydroxybupropion formation after 48 hrs by LC/MS method relative to untreated control2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.
AID372537Antimalarial activity as 2nd generation parasitaemia after 48 hrs against chloroquine-sensitive Plasmodium falciparum 3D7 infected human erythrocytes at 6 uM 0-12 hrs post invasion2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID1653512Anti-leprotic activity against rifampicin-susceptible Mycobacterium leprae primary cultures at 4 weeks assessed as ATP level per 10'7 cells at 0.4 mg/L measured by bioluminescence assay (Rvb = 332 +/- 46 pg)2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID285917Antimicrobial activity against methicillin-resistant Staphylococcus aureus 81112007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Antimicrobial activities of daptomycin, vancomycin, and oxacillin in human monocytes and of daptomycin in combination with gentamicin and/or rifampin in human monocytes and in broth against Staphylococcus aureus.
AID293686Growth inhibition of Mycobacterium tuberculosis H37Rv at 6.25 ug/ml by Microplate Alamar Blue Assay2007European journal of medicinal chemistry, Jun, Volume: 42, Issue:6
Clubbed triazoles: a novel approach to antitubercular drugs.
AID395776Antibacterial activity against Escherichia coli isolate containing extended spectrum beta lactamase after 24 hrs by twofold serial dilution technique2008European journal of medicinal chemistry, Nov, Volume: 43, Issue:11
Synthesis, antimicrobial activity, pharmacophore analysis of some new 2-(substitutedphenyl/benzyl)-5-[(2-benzofuryl)carboxamido]benzoxazoles.
AID1334261Selectivity index, ratio of GI50 for human HCT116 cells to MIC90 for Mycobacterium bovis BCG ATCC 35743 dormant stage2017Bioorganic & medicinal chemistry letters, 01-15, Volume: 27, Issue:2
New bithiazolyl hydrazones: Novel synthesis, characterization and antitubercular evaluation.
AID1542214Lipophilicity, log P of the compound in octanol and water incubated for 1 h under shaking condition2019European journal of medicinal chemistry, Apr-01, Volume: 167Synthesis, docking and antibacterial studies of more potent amine and hydrazone rifamycin congeners than rifampicin.
AID531257Antimicrobial activity against Clostridium difficile isolate 29 by Etest2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Rifampin and rifaximin resistance in clinical isolates of Clostridium difficile.
AID1869564Bactericidal activity against Bacillus cereus DSM 31 assessed as reduction in colony count and measured after 3 days by agar diffusion assay2022Journal of natural products, 06-24, Volume: 85, Issue:6
Triculamin: An Unusual Lasso Peptide with Potent Antimycobacterial Activity.
AID370100Plasma concentration in Mycobacterium bovis BCG infected tuberculosis mouse model at 5 mg/kg, po after 0.5 hrs2006PLoS medicine, Nov, Volume: 3, Issue:11
OPC-67683, a nitro-dihydro-imidazooxazole derivative with promising action against tuberculosis in vitro and in mice.
AID574811Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis H37Rv by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1287454Agonist activity at human PXR transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay2016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Altered activity profile of a tertiary silanol analog of multi-targeting nuclear receptor modulator T0901317.
AID1653482Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate alamar blue assay2019Bioorganic & medicinal chemistry, 07-01, Volume: 27, Issue:13
Insights of synthetic analogues of anti-leprosy agents.
AID1400053Antibacterial activity against Klebsiella pneumoniae ATCC 12019 incubated for 24 hrs under aerobic condition by MABA2018Bioorganic & medicinal chemistry, 09-15, Volume: 26, Issue:17
An antimycobacterial pleuromutilin analogue effective against dormant bacilli.
AID1311232Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-12016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
New peptide deformylase inhibitors design, synthesis and pharmacokinetic assessment.
AID564095Bactericidal activity against log-phase methicillin-resistant Staphylococcus aureus HUSA 304 after 24 hrs by time kill analysis in presence of 50 mg/L calcium ions2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Efficacy of high doses of daptomycin versus alternative therapies against experimental foreign-body infection by methicillin-resistant Staphylococcus aureus.
AID103835In vitro activity of compound against slowly growing Mycobacterium scrofulaceum 12921990Journal of medicinal chemistry, May, Volume: 33, Issue:5
Synthesis and biological activity of some derivatives of rifamycin P.
AID1210065Induction of CYP2B6 mRNA expression in human donor hepatocytes after 48 hrs by real-time PCR method relative to untreated control2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Quantitative prediction of CYP2B6 induction by estradiol during pregnancy: potential explanation for increased methadone clearance during pregnancy.
AID510529Apparent volume of distribution in tuberculosis patient at 10 mg/kg, po by HPLC analysis2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Pharmacokinetics of antituberculosis drugs in pulmonary tuberculosis patients with type 2 diabetes.
AID1401977Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv RIF-R1 harboring rpoB S522L mutant2018European journal of medicinal chemistry, Jan-01, Volume: 143Synthesis and antimycobacterial activity of triterpeni≿ A-ring azepanes.
AID1869528Antibacterial activity against Bacillus subtilis ATCC6633 measured after 24 hrs by broth microdilution method
AID1879530Antibacterial activity against rifampicin-resistant Clostridioides difficile CB1934 harboring rpoBQ489K mutant measured after 3 days2022Journal of medicinal chemistry, 03-24, Volume: 65, Issue:6
Design, Synthesis, and Characterization of TNP-2198, a Dual-Targeted Rifamycin-Nitroimidazole Conjugate with Potent Activity against Microaerophilic and Anaerobic Bacterial Pathogens.
AID1181156Antimicrobial activity against clinical isolate Mycobacterium tuberculosis Erdman assessed as growth inhibition after 7 days by turbidometry2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1416769Antimycobacterial activity against Mycobacterium smegmatis after 72 hrs by broth microdilution method2018MedChemComm, Jan-01, Volume: 9, Issue:1
Synthesis and
AID774602Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 expressing luciferase reporter gene assessed as growth inhibition after 6 days by luminometry2013European journal of medicinal chemistry, Sep, Volume: 67Synthesis and antimycobacterial activity of analogues of the bioactive natural products sampangine and cleistopholine.
AID571649Antibacterial activity against Proteus vulgaris ATCC 13315 by Etest method in presence of 4 ug/ml NAB70742008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1716640Antibacterial activity against Pseudomonas aeruginosa 101243 assessed as fractional inhibitory concentration incubated for 18 hrs in presence of chloramphenicol by broth microdilution assay2019European journal of medicinal chemistry, Jul-15, Volume: 174Heterodimeric Rifampicin-Tobramycin conjugates break intrinsic resistance of Pseudomonas aeruginosa to doxycycline and chloramphenicol in vitro and in a Galleria mellonella in vivo model.
AID341067Plasma concentration in human at 600 mg, po once daily after 14 days coadministered with moxifloxacin at 400 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID757716Antibacterial activity against Pseudomonas aeruginosa PAO1 assessed as growth inhibiiton after 18 hrs2013European journal of medicinal chemistry, Jul, Volume: 65Novel small molecule inhibitors targeting the "switch region" of bacterial RNAP: structure-based optimization of a virtual screening hit.
AID1601630Antitubercular activity against multi drug resistant Mycobacterium tuberculosis 16995 after 7 days by MABA method2019European journal of medicinal chemistry, Mar-01, Volume: 165Synthesis and antitubercular evaluation of reduced lipophilic imidazo[1,2-a]pyridine-3-carboxamide derivatives.
AID557106Binding affinity to human serum albumin assessed as fraction of binding sites occupied by compound at 245 ug/ml by SPR2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Use of a surface plasmon resonance method to investigate antibiotic and plasma protein interactions.
AID543815Bactericidal activity against Acinetobacter baumannii VT 126 assessed as eradication of pre-formed biofilm at 50 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
Effect of DNase and antibiotics on biofilm characteristics.
AID1287508Selectivity index, ratio of GI50 for human HeLa cells to MIC for dormant state Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, Apr-01, Volume: 26, Issue:7
Synthesis, biological evaluation and molecular docking study of some novel indole and pyridine based 1,3,4-oxadiazole derivatives as potential antitubercular agents.
AID372487Tmax in patient with severe malaria at 200 mg, perorally2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Multiple antibiotics exert delayed effects against the Plasmodium falciparum apicoplast.
AID572147Antimicrobial activity against AcrAB-deficient Escherichia coli AG100AX harboring pBADomeganorM plasmid containing Neisseria gonorrhoeae multidrug efflux pump NorM after 18 to 24 hrs by two fold dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Functional cloning and characterization of the multidrug efflux pumps NorM from Neisseria gonorrhoeae and YdhE from Escherichia coli.
AID1296401Cytotoxicity against human HuH7 cells assessed as cell viability at 20 uM after 24 hrs by MTS assay2016Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6
Development of 3,5-Dinitrobenzylsulfanyl-1,3,4-oxadiazoles and Thiadiazoles as Selective Antitubercular Agents Active Against Replicating and Nonreplicating Mycobacterium tuberculosis.
AID1558529Tmax in rat at 10 mg/kg, po2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
Design, Synthesis, and Pharmacological Evaluation of Potent Positive Allosteric Modulators of the Glucagon-like Peptide-1 Receptor (GLP-1R).
AID625283Drug Induced Liver Injury Prediction System (DILIps) training set; hepatic side effect (HepSE) score for elevated liver function tests2011PLoS computational biology, Dec, Volume: 7, Issue:12
Translating clinical findings into knowledge in drug safety evaluation--drug induced liver injury prediction system (DILIps).
AID1205459Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis assessed as inhibition of bacterial growth after 4 weeks by two-fold dilution technique2015European journal of medicinal chemistry, Apr-13, Volume: 94Synthesis, crystal structure and biological evaluation of substituted quinazolinone benzoates as novel antituberculosis agents targeting acetohydroxyacid synthase.
AID439870Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2009Journal of medicinal chemistry, Nov-12, Volume: 52, Issue:21
Searching for new cures for tuberculosis: design, synthesis, and biological evaluation of 2-methylbenzothiazoles.
AID474486Plasma protein binding in baboon2010Journal of medicinal chemistry, Apr-08, Volume: 53, Issue:7
Radiosynthesis and bioimaging of the tuberculosis chemotherapeutics isoniazid, rifampicin and pyrazinamide in baboons.
AID571201Antibacterial activity against Escherichia coli ATCC 25992 by Checkerboard method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1193497Thermodynamic equilibrium solubility, log S of the compound PBS at pH 7.4 at RT after 24 hrs by shake-flask method2015Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7
Thermodynamic equilibrium solubility measurements in simulated fluids by 96-well plate method in early drug discovery.
AID566041Selectivity index, ratio of CC50 for african green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv ATCC 272942011European journal of medicinal chemistry, Jan, Volume: 46, Issue:1
Synthesis and in vitro antimycobacterial activity of 8-OCH(3) ciprofloxacin methylene and ethylene isatin derivatives.
AID1185139Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 272942014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID571440Ratio of the MIC for Escherichia coli IH3080 in the absence of NAB7061 to MIC for Escherichia coli IH3080 in the presence of 4 ug/ml of NAB70612008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Novel polymyxin derivatives carrying only three positive charges are effective antibacterial agents.
AID1167366Ratio of MPC for Escherichia coli D21 tolC deletion mutant to MIC for Escherichia coli D21 tolC deletion mutant2014Journal of medicinal chemistry, Nov-13, Volume: 57, Issue:21
Design, synthesis, and antibacterial properties of dual-ligand inhibitors of acetyl-CoA carboxylase.
AID571884Antibacterial activity against Escherichia coli KAM32 harboring recombinant plasmid pVBS1 encoding Acinetobacter baumannii abeS gene by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Role of AbeS, a novel efflux pump of the SMR family of transporters, in resistance to antimicrobial agents in Acinetobacter baumannii.
AID479647Antimycobacterial activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv at 0.5 to 1 ug/ml by radiometric BACTEC assay2010Journal of medicinal chemistry, May-27, Volume: 53, Issue:10
3'-bromo analogues of pyrimidine nucleosides as a new class of potent inhibitors of Mycobacterium tuberculosis.
AID565789Antimicrobial activity against Neisseria meningitidis harboring rpoB36 H552N mutant allele by Etest2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Multicenter study for defining the breakpoint for rifampin resistance in Neisseria meningitidis by rpoB sequencing.
AID558245Bactericidal activity against Staphylococcus aureus E19977 assessed as log reduction in cfu at 20 mg/liter after 24 hrs by time-kill study2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Intracellular activity of antibiotics against Staphylococcus aureus in a mouse peritonitis model.
AID283161Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2588 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID727921Antibacterial activity against Bacillus subtilis ATCC 6633 at 30 ug/disk after 12 hrs by paper disk diffusion assay2013ACS medicinal chemistry letters, Feb-14, Volume: 4, Issue:2
Novel hybrid-type antimicrobial agents targeting the switch region of bacterial RNA polymerase.
AID678722Covalent binding affinity to human liver microsomes assessed per mg of protein at 10 uM after 60 mins presence of NADPH2012Chemical research in toxicology, Oct-15, Volume: 25, Issue:10
Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds.
AID1311281Selectivity index, ratio of CC50 for human PANC1 cells to MIC for active stage of Mycobacterium bovis BCG ATCC 357342016Bioorganic & medicinal chemistry letters, 08-01, Volume: 26, Issue:15
Synthesis and antitubercular activity of new 1,3,4-oxadiazoles bearing pyridyl and thiazolyl scaffolds.
AID1678516Antibacterial activity against Clostridium difficile 8290 incubated for 46 hrs in anaerobic condition by CLSI-based broth microdilution assay2020ACS medicinal chemistry letters, Dec-10, Volume: 11, Issue:12
Semisynthetic Analogs of the Antibiotic Fidaxomicin-Design, Synthesis, and Biological Evaluation.
AID748174Inhibition of rifamycin-resistant Mycobacterium tuberculosis RNA polymerase H445Y mutant after 10 mins by rolling circle transcription assay in presence of DNA nanocircle template NC452013Journal of medicinal chemistry, Jun-13, Volume: 56, Issue:11
X-ray crystal structures of the Escherichia coli RNA polymerase in complex with benzoxazinorifamycins.
AID588519A screen for compounds that inhibit viral RNA polymerase binding and polymerization activities2011Antiviral research, Sep, Volume: 91, Issue:3
High-throughput screening identification of poliovirus RNA-dependent RNA polymerase inhibitors.
AID540299A screen for compounds that inhibit the MenB enzyme of Mycobacterium tuberculosis2010Bioorganic & medicinal chemistry letters, Nov-01, Volume: 20, Issue:21
Synthesis and SAR studies of 1,4-benzoxazine MenB inhibitors: novel antibacterial agents against Mycobacterium tuberculosis.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (19,089)

TimeframeStudies, This Drug (%)All Drugs %
pre-19906060 (31.75)18.7374
1990's2514 (13.17)18.2507
2000's3475 (18.20)29.6817
2010's5126 (26.85)24.3611
2020's1914 (10.03)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Trials1,499 (7.32%)5.53%
Reviews0 (0.00%)6.00%
Reviews1,256 (6.14%)6.00%
Case Studies0 (0.00%)4.05%
Case Studies2,849 (13.92%)4.05%
Observational0 (0.00%)0.25%
Observational104 (0.51%)0.25%
Other9 (100.00%)84.16%
Other14,760 (72.11%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (411)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Drug-Drug Interaction Study to Assess the Effect of Rifampin on the Pharmacokinetics of an Oral Dose of BMS-986278 in Healthy Participants[NCT03712540]Phase 139 participants (Actual)Interventional2018-09-06Completed
Studying the Blood Levels of First-line Anti-tuberculosis Drugs in Relation to Treatment Outcomes Among Newly Diagnosed Adults With Pulmonary Tuberculosis on the Thai-Myanmar Border[NCT02457208]Phase 161 participants (Actual)Interventional2015-07-07Completed
Randomized Drug Interaction Study of RO4929097 for Advanced Solid Tumors[NCT01218620]Phase 117 participants (Actual)Interventional2010-09-30Completed
PXR-aktivaation Vaikutukset Sokeri-, Kolesteroli- ja Hormonitasapainoon[NCT01293422]Phase 412 participants (Actual)Interventional2011-01-31Completed
A Phase 1, Open Label, Fixed-Sequence Study To Estimate The Effect Of Repeat-Dose Rifampin On The Pharmacokinetics Of CP-690,550 In Healthy Volunteers[NCT01204112]Phase 112 participants (Actual)Interventional2010-09-30Completed
A Phase I Open-Label Trial To Investigate the Pharmacokinetic Interaction Between Rifabutin Or Rifampin And A Single Dose Of TMC207 In Healthy Subjects[NCT01341184]Phase 133 participants (Actual)Interventional2011-10-21Completed
A Phase 1, Non-Randomized, Open Label Study to Determine the Effect of Rifampin on the Pharmacokinetics of a Single Oral Dose of 160 mg Regorafenib (BAY73-4506) in Healthy Volunteers[NCT01322438]Phase 124 participants (Actual)Interventional2011-03-31Completed
A Open-Label, Two-sequence Phase I Drug-drug Interaction Clinical Study to Investigate the Pharmacokinetics of Leritrelvir With Midazolam, Omeprazole, Rosuvastatin, Verapamil, and Rifampin in Healthy Participants[NCT06031454]Phase 156 participants (Anticipated)Interventional2023-09-01Recruiting
A Phase 2/3, Multicenter, Randomized, Open-label, Active-controlled Study to Evaluate the Efficacy and Safety of Bedaquiline Administered as Part of a Treatment Regimen With Clarithromycin and Ethambutol in Adult Patients With Treatment-refractory Mycobac[NCT04630145]Phase 2/Phase 3124 participants (Anticipated)Interventional2021-01-08Recruiting
Phase 1, Open Label, Two Arm, Fixed Sequence Study to Evaluate the Effect of Rifampin and Rifabutin on GSK1349572 Pharmacokinetics in Healthy Male and Female Volunteers[NCT01231542]Phase 127 participants (Actual)Interventional2011-05-31Completed
Short Course Rifapentine and Isoniazid for the Preventive Treatment of Tuberculosis(SCRIPT-TB)[NCT03900858]566 participants (Anticipated)Interventional2018-12-01Recruiting
Six Weeks of Daily Rifapentine vs. a Comparator Arm of 12-16 Week Rifamycin-based Treatment of Latent M. Tuberculosis Infection: Assessment of Safety, Tolerability and Effectiveness[NCT03474029]Phase 2/Phase 33,400 participants (Anticipated)Interventional2019-08-01Recruiting
A Non-Randomized, Open-Label, Three-Part, Drug-Drug Interaction Study to Evaluate the Effects of Itraconazole, Rifampin, and Quinidine on the Pharmacokinetics and Safety of EDP-938 in Healthy Subjects[NCT03755778]Phase 172 participants (Actual)Interventional2018-11-29Completed
Comparison of Efficacy and Safety of Colistin-rifampin Combination and Colistin Monotherapy in Extensively Drug-resistant Acinetobacter Baumannii: Utility of the Synergy Test Results (E-test) in Vitro[NCT03622918]9 participants (Actual)Interventional2016-10-27Completed
Randomized Control Trial Comparing Efficacy of Antibiotic Therapy Alone Versus Antibiotic Therapy in Conjunction With Quadruple Pulse Therapy Using NdYag Laser in Treatment of Hidradenitis Suppurativa[NCT01063270]18 participants (Actual)Interventional2010-02-28Completed
A Phase 1 Study to Evaluate the Effects of Rifampin on Pharmacokinetics of Pevonedistat in Patients With Advanced Solid Tumors[NCT03486314]Phase 120 participants (Actual)Interventional2018-08-13Completed
A Phase I Study to Assess the Effect of a CYP3A Inducer (Rifampin) on the Pharmacokinetics of ABT-263 (Navitoclax)[NCT01121133]Phase 112 participants (Actual)Interventional2010-05-31Completed
A Phase I, Open-Label Study to Evaluate the Effect of Rifampin on the Single Dose Pharmacokinetics, Safety and Tolerability of BMS-986224 in Healthy Subjects[NCT03563950]Phase 142 participants (Actual)Interventional2018-06-01Completed
Clinical Evaluation of Adjusted Doses of Darunavir/Ritonavir With Rifampicin in HIV-infected Volunteers[NCT03892161]Phase 117 participants (Actual)Interventional2018-04-12Terminated(stopped due to Risks to participation)
Phase One, Open Lab Study to Investigate the Impact of Rifampicin Administration on the PK of Dolutegravir When Dosed Once Daily at 50 or 100 mg in Healthy Volunteers[NCT03199690]Phase 116 participants (Anticipated)Interventional2017-10-31Not yet recruiting
A Phase I Study Assessing the Effects of Rifampin on the Pharmacokinetics of Ataluren in Healthy Subjects[NCT02409004]Phase 115 participants (Actual)Interventional2015-02-28Completed
Safety and Tolerability of Ultra-short Course Rifapentine and Isoniazid (1HP) for Prevention of Tuberculosis in HIV-Uninfected Individuals[NCT04703075]Phase 4500 participants (Anticipated)Interventional2022-03-24Recruiting
Evaluating Pharmacokinetics and Whole Blood Bactericidal Activity Against Mycobacterium Tuberculosis of Single 'High' Doses of Rifampicin in Healthy Volunteers[NCT02387242]Phase 118 participants (Anticipated)Interventional2015-02-28Suspended(stopped due to New relevant data published)
Trial of Faropenem and Cefadroxil (in Combination With Amoxicillin/Clavulanic Acid and Standard TB Drugs) in Patients With Pulmonary Tuberculosis: Measurement of Early Bactericidal Activity and Effects on Novel Biomarkers[NCT02381470]Phase 258 participants (Actual)Interventional2019-02-11Completed
A Phase 1, Open-Label, Fixed-sequence, 5-part, Drug-drug Interaction Study of Tucatinib to Evaluate the Effects of CYP3A4 and CYP2C8 Inhibition and Induction on the Pharmacokinetics of Tucatinib and to Evaluate the Effects of Tucatinib on the Pharmacokine[NCT03723395]Phase 1116 participants (Actual)Interventional2018-09-17Completed
A PHASE 1 OPEN-LABEL, TWO-ARM,DRUG-DRUG INTERACTION STUDY TO EVALUATE THE EFFECT OF ITRACONAZOLE AND RIFAMPIN ON THE PHARMACOKINETICS OF TALAZOPARIB IN PATIENTS WITH ADVANCED SOLID TUMORS[NCT03077607]Phase 136 participants (Actual)Interventional2016-11-07Completed
A PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO ESTIMATE THE EFFECT OF REPEAT-DOSE RIFAMPIN ON THE PHARMACOKINETICS OF PF-04965842 IN HEALTHY SUBJECTS[NCT03637790]Phase 112 participants (Actual)Interventional2018-09-13Completed
A Pharmacokinetic, Multi-cohort Study in Healthy Adult Subjects to Assess Gepotidacin as Victim and as Perpetrator of Drug-Drug Interactions Via CYP450, Renal and Intestinal Transporters, and to Assess Gepotidacin Pharmacokinetics in Japanese Healthy Adul[NCT04493931]Phase 164 participants (Actual)Interventional2020-08-14Completed
A Prospective Study of Shortening the Duration of Standard Short Course Chemotherapy From 6 Months to 4 Months in HIV-non-infected Patients With Fully Drug-Susceptible, Non-cavitary Pulmonary Tuberculosis With Negative Sputum Cultures After 2 Months of An[NCT00130247]Phase 3394 participants (Actual)Interventional2002-04-08Completed
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics[NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
A Single-centre, Open, Single-dose, Self-control Study to Investigate the Effect of Rifampicin on the Pharmacokinetics of SHR6390 in Healthy Chinese Adult Subjects.[NCT04439578]Phase 118 participants (Actual)Interventional2020-06-23Completed
An Adaptive, Part Open-label, Part Randomised Phase 1 Clinical Trial in Healthy Volunteers to Study Drug Interactions With RV521 Including Those Mediated by CYP3A4 and P-glycoprotein[NCT03782662]Phase 182 participants (Actual)Interventional2018-11-06Completed
A Single-Center, Non-Randomized, Open-Label, One-Sequence, Two-Period Within-Subject Study to Investigate the Effect of Rifampicin on the Pharmacokinetics of Multiple Doses of Balovaptin In Healthy Volunteers[NCT03586726]Phase 116 participants (Actual)Interventional2018-07-24Completed
A Randomized, Four-arm Open Label Phase Two-b Clinical Trial to Evaluate the Pharmacokinetics, Safety/Tolerability and Efficacy of High Dose Rifampicin in TB-HIV Co-infected Patients on Efavirenz- or Dolutegravir-based Antiretroviral Therapy[NCT03982277]Phase 2130 participants (Actual)Interventional2019-04-30Completed
A Two-part, Phase I, Open-label, Multicenter, Two-period, One-sequence Study to Investigate the Effect of Itraconazole and Rifampin on the PK of Vemurafenib at Steady State[NCT02608034]Phase 132 participants (Anticipated)Interventional2016-05-26Completed
An Open-label, Fixed-sequence, Phase 1 Clinical Trial to Evaluate the Effect of Clarithromycin/Rifampicin on the Pharmacokinetics of DA-8010 in Healthy Adults[NCT05991401]Phase 118 participants (Anticipated)Interventional2023-08-18Recruiting
The Study of Standardized Preoperative Anti-tuberculosis Treatment of Surgical Treatment of Spinal Tuberculosis Patients[NCT02477852]Phase 4400 participants (Anticipated)Interventional2015-04-30Recruiting
A Phase 1 Open-Label Study to Evaluate the Drug-Drug Interaction of Rifampin as a Strong CYP3A Inducer on Soticlestat Pharmacokinetics in Healthy Adult Participants[NCT05098041]Phase 115 participants (Actual)Interventional2021-11-22Completed
Randomized, Open Label, Multiple Dose Phase 2a Study of the Early Bactericidal Activity of AZD5847 in Adults With Pulmonary Tuberculosis[NCT01516203]Phase 275 participants (Actual)Interventional2012-12-05Completed
A Single-Center, Open-Label, Randomized, Two-Stage, Two-Way Crossover Study Evaluating Drug-Drug Interaction (DDI) Between HSK3486 Injectable Emulsion and Rifampin Capsules in Healthy Subjects.[NCT03758469]Phase 116 participants (Actual)Interventional2018-12-14Completed
The Effect of Fermented Soybean Supplementation on the Body Weight and Physical Function of Tuberculosis Patients With Standard Therapy in Indonesia[NCT02554318]147 participants (Actual)Interventional2013-11-30Completed
Open-Label Pharmacokinetics Study to Evaluate Drug-Drug Interactions and Safety of ELPIDA® in Co-Administration With Other Drugs in Healthy Volunteers[NCT03709355]Phase 156 participants (Actual)Interventional2018-11-14Completed
The Effect of Rifampicin on the Plasma Pharmacokinetics of Emtricitabine (FTC) and Tenofovir Alafenamide Fumarate (TAF) and Intracellular Tenofovir-diphosphate (TFV-DP) and FTC-triphosphate (FTC-TP)[NCT03186482]Phase 121 participants (Actual)Interventional2017-06-01Completed
A Phase 1, Randomized, Parallel-Group, Open-Label Study to Evaluate the Effect of the Modulators of the Cytochrome P450 (CYP) 2C8 and/or 3A on the Single-Dose Pharmacokinetics of Ozanimod and CC112273 in Healthy Adult Subjects[NCT03624959]Phase 1100 participants (Actual)Interventional2018-06-20Completed
An Open Labe Study to Evaluate the Drug-Drug Interaction of Itraconazole, Rifampicin and Midazolam With SIM0417/Ritonavir in Healthy Adult Chinese Participants[NCT05665647]Phase 136 participants (Actual)Interventional2022-12-29Completed
Systematic Empirical vs. Test-guided Anti-tuberculosis Treatment Impact in Severely Immunosuppressed HIV-infected Adults Initiating Antiretroviral Therapy With CD4 Cell Counts <100/mm3: the STATIS Randomized Controlled Trial[NCT02057796]Phase 41,050 participants (Actual)Interventional2014-09-30Completed
A Phase 1,Parallel Assignment,Fixed-Sequence Study to Assess the Effect of Itraconazole, Rifampicin on the Pharmacokinetics of TPN171H in Healthy Subjects[NCT06090123]Phase 124 participants (Actual)Interventional2020-01-01Completed
Six- Versus Twelve-Week Therapy for Non-Surgically-Treated Diabetic Foot Osteomyelitis: A Multicenter Open-Label Controlled Randomized Study[NCT02123628]Phase 440 participants (Actual)Interventional2007-06-30Completed
An Open-label Study to Evaluate the Drug-drug Interaction Effect of Rifampin, a CYP3A4 Inducer, on the Pharmacokinetics of AMG 510 in Healthy Subjects[NCT05577624]Phase 114 participants (Actual)Interventional2019-11-05Completed
An Open-label Non-randomized, Phase 1 Study to Evaluate the Effect of (a) Itraconazole or Rifampin on the Pharmacokinetics of a Single Intravenous Dose of Copanlisib and (b) Copanlisib on Cardiovascular Safety in Subjects With Advanced Solid Tumors and No[NCT02253420]Phase 151 participants (Actual)Interventional2014-10-08Completed
A Study to Evaluate the Relative Bioavailability of Different Strengths of STI-1558 Capsules and the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and Inducer (Rifampin) on the Pharmacokinetics of STI-1558 in Healthy Volunteers[NCT05685719]Phase 137 participants (Actual)Interventional2023-01-04Completed
Pharmacokinetics of Anti-tuberculosis and Antiretroviral Drugs in Children[NCT03800381]92 participants (Anticipated)Observational2019-01-28Recruiting
A Randomized Double Blinded Phase 2b Clinical Trial Comparing Standard Dose With Two Higher Doses of Rifampicin for Treatment of Adults With Tuberculous Meningitis[NCT02169882]Phase 2/Phase 360 participants (Actual)Interventional2014-12-01Completed
Effect of a Strong Enzyme Inducer, Rifampin, on the Single-Dose Pharmacokinetics of Istradefylline in Healthy Subjects[NCT02174250]Phase 120 participants (Actual)Interventional2014-06-30Completed
A Phase 1, Single-center, Open-label, 2-period, Single Sequence Drug-drug Interaction Study to Evaluate the Effects of Multiple-dose Rifampicin on the Pharmacokinetics and Pharmacodynamics of Single Dose Sotagliflozin in Healthy Male and Female Subjects[NCT03063580]Phase 116 participants (Actual)Interventional2017-02-27Completed
Evaluation of the Efficacy and Safety of a Short-course, Daily, 4-month Regimen Including Isoniazid, Pyrazinamide, Rifapentine and Moxifloxacin (2HZPM/2HPM) for the Treatment of Drug-susceptible Pulmonary Tuberculosis in Taiwan (ESCAPE-TB)[NCT04856644]Phase 3366 participants (Anticipated)Interventional2021-05-01Not yet recruiting
A Seamless Phase 2B/C Platform Trial to Evaluate Multiple Regimens and Durations of Treatment in Pulmonary Tuberculosis[NCT06114628]Phase 22,500 participants (Anticipated)Interventional2023-12-08Not yet recruiting
A Phase I, Randomized, Open-label, 2-arm Parallel-design Study to Determine the Effect of Multiple-dose Rifampin on the Pharmacokinetics, Safety and Tolerability of Single-dose Enzalutamide in Healthy Male Subjects[NCT02138799]Phase 128 participants (Actual)Interventional2013-07-31Completed
An Open Label, Two-period, Fixed Sequence, Phase 1 Trial to Evaluate the Effect of Multiple Doses of Rifampicin on the Multiple-dose Pharmacokinetics of Linagliptin[NCT02183584]Phase 116 participants (Actual)Interventional2009-09-30Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum[NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
Induction of Drug Metabolism by Rifampicin to Compare the Endogenous Biomarker 4beta-OHcholesterol With the Probe Drug Midazolam as Quantitative Markers for Cytochrome P450 3A4 Induction[NCT01340456]24 participants (Actual)Interventional2011-05-31Completed
A Phase 2A Trial to Evaluate the Extended Early Bactericidal Activity, Safety, Tolerability, and Pharmacokinetics of SQ109 in Adult Subjects With Newly Diagnosed, Uncomplicated, Smear-Positive, Pulmonary Tuberculosis[NCT01218217]Phase 290 participants (Actual)Interventional2010-11-30Completed
TB YOUTH - TB sYstemic Management Using One-month, Ultra-short TPT Regimen for scHool Contacts[NCT06022146]Phase 33,520 participants (Anticipated)Interventional2023-09-01Recruiting
Phase IIA Trial of the Safety and Tolerability of Increased Dose Rifampicin and Adjunctive Linezolid With or Without Aspirin, for HIV-associated Tuberculous Meningitis[NCT03927313]Phase 252 participants (Actual)Interventional2019-06-12Completed
A Phase 2 Trial to Evaluate the Early Bactericidal Activity, Safety and Tolerability of Sanfetrinem Cilexetil Administered Orally to Adults With Newly Diagnosed, Smear-Positive, Rifampicin-Susceptible Pulmonary Tuberculosis[NCT05388448]Phase 2105 participants (Anticipated)Interventional2022-04-21Recruiting
A Phase 1, Open Label, Fixed Sequence Design, Multiple Dose Study To Assess The Effect Of Rifampin On The Pharmacokinetics Of Sitaxsentan In Healthy Subjects[NCT01251835]Phase 10 participants (Actual)Interventional2010-12-31Withdrawn
Characterization of Immune Responses in Treatment-induced Latency in Pulmonary Tuberculosis[NCT01154959]Phase 3120 participants (Actual)Interventional2010-02-28Completed
MESS- MRSA Eradication Study Skåne. A Comparison Between Systemic Antibiotic Treatment in Combination With Topical Mupirocintreatment With Only Topical Mupiroicintreatment to Eradicate MRSA in Throat Carriers[NCT01269541]69 participants (Actual)Interventional2011-03-01Completed
Postoperative Antibiotic Management Duration Following Surgery for Intravenous Drug Abuse (IVDA) Endocarditis (OPTIMAL)[NCT05156437]Phase 420 participants (Anticipated)Interventional2022-03-16Enrolling by invitation
Randomized Controlled Trial of Colistin Versus Colistin Plus Rifampicin in MDR P.Aeruginosa and A.Baumanii[NCT01297855]Phase 3130 participants (Anticipated)Interventional2010-06-30Recruiting
A Study to Assess the Pharmacokinetics of Midazolam, Dabigatran, Pitavastatin, Atorvastatin, and Rosuvastatin Administered as Microdoses in Subjects With Varying Degrees of Renal Insufficiency in the Presence and Absence of Rifampin[NCT03311841]Phase 132 participants (Actual)Interventional2018-03-01Completed
Staphylococcal Acute Post-Operative Prosthetic Joint Infection Treated With 'DAIR' (Debridement and Implant Retention) And Impact Of Rifampin: A Retrospective Cohort Study In France[NCT03750721]79 participants (Actual)Observational2018-04-01Completed
An Open-Label, Phase 1 Study in Healthy Volunteers to Evaluate the Drug-Drug Interaction Potential of CCX168 With Concomitant Medications[NCT06004947]Phase 132 participants (Actual)Interventional2016-01-14Completed
Gemifloxacin Versus Ciprofloxacin Versus Rifampicin in Treatment of Rhinoscleroma[NCT03326050]Early Phase 160 participants (Anticipated)Interventional2018-02-28Not yet recruiting
An Open-Label, Non-Randomized, 2-Period, Single Center Study to Assess the Single Dose Pharmacokinetics of R406 in Healthy Subjects When Fostamatinib 150 mg is Administered Alone and in Combination With Rifampicin[NCT01336218]Phase 115 participants (Anticipated)Interventional2011-04-30Completed
A Phase 1, Single-center, Open-label, Two-cohort, Two-period, One-sequence, Two Treatment, Drug-drug Interaction Study of the Effects of Gemfibrozil and Rifampicin on SAR442168 in Healthy Subjects[NCT06064539]Phase 130 participants (Actual)Interventional2020-05-18Completed
Phase I, Open-label, 3-way Crossover Trial in Healthy Volunteers to Determine the Drug-drug Interaction Between TMC435350 and Rifampin After Multiple Dosing.[NCT00741169]Phase 121 participants (Actual)Interventional2008-06-30Completed
TBTC Study 31 PK/PD: Population Pharmacokinetic and Pharmacodynamic Study of Efficacy and Safety of High-Dose Rifapentine and Moxifloxacin for Treatment of Tuberculosis in the Study 31 Treatment Trial: Intensive PK Sampling[NCT02563327]Phase 360 participants (Anticipated)Interventional2016-05-30Recruiting
TBTC Study 29: Evaluation of a Rifapentine-containing Regimen for Intensive Phase Treatment of Pulmonary Tuberculosis[NCT00694629]Phase 2865 participants (Actual)Interventional2008-12-31Completed
An International Multicentre Controlled Clinical Trial to Evaluate 1200mg and 1800mg Rifampicin Daily for Four Months in the Reduction of the Duration of Standard Treatment of Pulmonary Tuberculosis[NCT02581527]Phase 3672 participants (Actual)Interventional2017-02-01Completed
A Phase I Study to Assess the Effect of Itraconazole and Rifampicin on Pharmacokinetics Profile of BPI-7711 in Chinese Healthy Volunteers[NCT04135833]Phase 131 participants (Actual)Interventional2019-12-12Completed
A Phase I, Open-label Multi-dose Two-part Study to Characterize the Effects of a Strong CYP3A4 Inhibitor and a Strong CYP3A4 Inducer on the Steady-State Pharmacokinetics of Tazemetostat (EPZ-6438) in Subjects With Advanced Malignancies[NCT04537715]Phase 142 participants (Actual)Interventional2020-04-23Completed
Prospective, Randomized Study of Oral Metronidazole vs. Oral Metronidazole and Rifampin for Treatment of Clostridium Difficile-associated Diarrhea (CDAD)[NCT00182429]Phase 3100 participants Interventional2004-02-29Completed
Comparing Oral Versus Parenteral Antimicrobial Therapy (COPAT) Trial[NCT05977868]Phase 4135 participants (Anticipated)Interventional2023-08-04Enrolling by invitation
Interaction of Buprenorphine With HIV Medications and Tuberculosis Medications[NCT00877591]Phase 163 participants (Actual)Interventional2008-04-30Completed
A Phase I Study to Evaluate Drug-Drug Interaction of TQB3909 Tablets[NCT06165822]Phase 140 participants (Anticipated)Interventional2023-12-31Not yet recruiting
Rosuvastatin Evaluation as a Tuberculosis Treatment Adjunct[NCT04504851]Phase 2154 participants (Anticipated)Interventional2020-08-12Not yet recruiting
Evaluation of Pharmacokinetics and Safety Tolerability of Higher Doses of Rifampicin in Children With Newly Diagnosed Uncomplicated Tuberculosis[NCT04437836]Phase 1/Phase 240 participants (Anticipated)Interventional2019-07-01Recruiting
A Phase 1, Open-label, Parallel-group, Fixed-sequence Study to Investigate the Effect of the CYP3A Inducer Rifampin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of Pamiparib (BGB-290) in Cancer Patients[NCT03994211]Phase 125 participants (Actual)Interventional2019-05-29Completed
[NCT02055703]Phase 1195 participants (Actual)Interventional2014-01-31Completed
A Three-part, Single-center, Open-label, Phase I Drug-drug Interaction Clinical Study to Investigate the Effect of Itraconazole, Gemfibrozil or Rifampicin on Pharmacokinetics of SKLB1028 in Healthy Subjects[NCT05069870]Phase 142 participants (Actual)Interventional2021-06-07Active, not recruiting
[NCT02085967]Phase 1106 participants (Actual)Interventional2014-02-28Completed
A Drug-drug Interaction Study to Evaluate the Effect of Rifampicin and Febuxostat on the Pharmacokinetics of Methotrexate in Healthy Subjects[NCT05575297]Phase 112 participants (Actual)Interventional2021-12-20Completed
A Phase One, Open Label, Two-period, Two-treatment, Fixed Sequence, Cross-over Study To Estimate The Effect Of Multiple Dose Rifampin On The Single Dose Pharmacokinetics Of Pf-06463922 In Healthy Volunteers.[NCT02804399]Phase 112 participants (Actual)Interventional2016-07-31Completed
A Phase I, Non-randomized, Open-label, Fixed-sequence Study to Investigate the Effect of a Probe CYP3A4 Inhibitor and Inducer on the Pharmacokinetics of BAY1841788 (ODM 201) in Healthy Male Volunteers[NCT03048110]Phase 115 participants (Actual)Interventional2017-02-15Completed
Influence of Rifampin Co-Administration on the Pharmacokinetic Profile of Daptomycin[NCT02097953]Early Phase 112 participants (Actual)Interventional2014-05-31Completed
The Effects of Single-Dose Rifampin on the Pharmacokinetics of Rosuvastatin in Healthy White and Asian Volunteers[NCT02106767]Phase 116 participants (Actual)Interventional2014-11-30Completed
Rifampicin Combination Therapy Versus Targeted Antimicrobial Monotherapy in the Oral Antimicrobial Treatment Phase of Staphylococcal Prosthetic Joint Infection[NCT06172010]Phase 4316 participants (Anticipated)Interventional2023-04-01Recruiting
A Single-center, Open-label, Drug-drug Interaction Study of SH-1028 Tablets in Healthy Subjects[NCT04808648]Phase 140 participants (Anticipated)Interventional2021-04-06Not yet recruiting
A Drug-drug Interaction Study to Evaluate the Effect of Rifampicin on the Pharmacokinetics of Methotrexate in Elderly Subjects[NCT06108453]Phase 110 participants (Anticipated)Interventional2023-08-21Enrolling by invitation
Relative Bioavailability of Single Doses of 150 mg Dabigatran Etexilate (Capsule)When Administered Alone, After Seven Days of Dosing With 600 mg Rifampicin(Tablet), and Seven Days and Fourteen Days After Last Administration of Rifampicin in Healthy Male a[NCT02173717]Phase 124 participants (Actual)Interventional2009-06-30Completed
a Single-center, Open-label, Fixed Sequence Study in Healthy Chinese Subjects to Evaluate the Pharmacokinetic Effects of Itraconazole and Rifampicin on Oral Administration of a Single Dose of ABSK021[NCT06089733]Phase 132 participants (Anticipated)Interventional2023-04-11Enrolling by invitation
A Drug Interaction Study of KW-6356 and Clarithromycin or Rifampicin (A Drug Interaction Study With a CYP3A4/5 Inhibitor or Inducer)[NCT04070495]Phase 120 participants (Actual)Interventional2019-08-27Completed
A Randomized Clinical Trial of 4 Months of Rifampin vs. 9 Months of Isoniazid for Latent Tuberculosis Infection. Part 3 - Effectiveness[NCT00931736]Phase 36,031 participants (Actual)Interventional2009-08-31Completed
An Open-label Study to Evaluate the Safety, Tolerability and Pharmacokinetics of Cytochrome P450 Probe Drugs in Healthy Adult Subjects[NCT00964106]Phase 187 participants (Actual)Interventional2009-08-26Completed
A Phase I, Single-center, Open-label, Fixed-sequence Study of AB-106 in Chinese Healthy Adult Men Evaluated the Effects of Itraconazole and Rifampicin on AB-106 Pharmacokinetics[NCT05357820]Phase 156 participants (Actual)Interventional2021-07-19Completed
Active Screening of Latent TB Infection, Treatment and Long Term Follow-up in Prison[NCT00767975]Phase 32,384 participants (Actual)Interventional2008-01-31Completed
The Effect of Rifampicin on the Pharmacokinetics of Intracellular Tenofovir-diphosphate and Tenofovir When Coadministered With Tenofovir Alafenamide Fumarate During the Maintenance Phase of Tuberculosis Treatment in TB/HIV-1 Coinfected Participants[NCT04424264]Phase 118 participants (Actual)Interventional2019-12-05Completed
Evaluating Celecoxib Activity in Mycobacterium Tuberculosis: A Whole Blood Bactericidal Activity Study in Healthy Volunteers[NCT02602509]Phase 118 participants (Actual)Interventional2015-11-30Completed
PHASE 1, OPEN-LABEL, FIXED-SEQUENCE STUDY TO EVALUATE THE EFFECT OF REPEAT-DOSE RIFAMPIN ON THE PHARMACOKINETICS OF PF-06651600 IN HEALTHY PARTICIPANTS[NCT04266509]Phase 112 participants (Actual)Interventional2020-06-25Completed
A Prospective, Randomized Open-Label Phase II Study of the Safety and Tolerability of Metformin in Combination With Standard Antimicrobial Treatment of Pulmonary Tuberculosis in People With TB and Co-infected With HIV[NCT04930744]Phase 2112 participants (Anticipated)Interventional2021-08-03Recruiting
2R2: Higher Dose Rifampin for 2 Months vs Standard Dose Rifampin for Latent TB: a 3-arm Randomized Trial.[NCT03988933]Phase 21,368 participants (Actual)Interventional2019-09-20Active, not recruiting
The Effect of Rifampin on Etonogestrel Concentrations in Contraceptive Implant Users[NCT04463680]Phase 424 participants (Actual)Interventional2020-09-23Completed
An Open Label, Single Dose, Randomized, Two-Way Cross-Over Bioequivalence Study Comparing Rifampicin In A Fixed-Dose Combination Rifampicin + Isoniazid (Myrin© 2, Pfizer Inc) Tablet With The Reference Drug (Rimactane®, Novartis Sandoz) Capsule In Healthy [NCT01311505]Phase 121 participants (Actual)Interventional2011-04-30Completed
Oral Switch During Treatment of Left-sided Endocarditis Due to Multi-susceptible Staphylococcus (Relais Oral Dans le Traitement Des Endocardites à Staphylocoques Multi-sensibles)[NCT02701608]Phase 3324 participants (Anticipated)Interventional2016-02-29Recruiting
An Open-Label, Single-Dose Study to Assess the Pharmacokinetics, Safety, and Tolerability of Intranasally Administered Esketamine in Healthy Han Chinese, Korean, Japanese, and Caucasian Subjects and the Effects of Rifampin on the Pharmacokinetics of Intra[NCT02846519]Phase 166 participants (Actual)Interventional2016-02-26Completed
The Bioavailability of Rifampicin in Fixed Dose Combinations (FDCs) Widely Used in South Africa to Treat Drug-susceptible Tuberculosis (TB)[NCT02953847]Phase 121 participants (Actual)Interventional2016-11-30Completed
Pharmacokinetic Interaction Between Coartem® and Either Nevirapine, Efavirenz or Rifampicin in HIV Positive Ugandan Patients[NCT00620438]Phase 490 participants (Anticipated)Interventional2008-02-29Active, not recruiting
A Single-center, Open, Single Does, Drug-drug Interaction Study to Investigate the Effects of Rifampin on the Pharmacokinetics of Healthy Chinese Adult Subjects After Oral Administration of SHR2554 Tablets[NCT04577885]Phase 118 participants (Actual)Interventional2020-05-28Completed
A Phase 1, Open-label, Single-center Study to Evaluate the Effect of Cytochrome P450 (CYP) 3A Inhibition and Induction on the Pharmacokinetics of CC-220 in Healthy Subjects[NCT02820935]Phase 136 participants (Actual)Interventional2016-07-31Completed
A Pilot Study Comparing Inflammatory Biomarkers in Blood and CSF in Patients With Alzheimer's Disease and Age-Matched Controls[NCT00715858]Phase 321 participants (Anticipated)Interventional2008-05-31Recruiting
Shortened Regimens for First Diagnosed Smear Positive Drug Susceptible Pulmonary Tuberculosis: a Randomised Controlled Non-inferiority Trial[NCT02901288]Phase 43,900 participants (Anticipated)Interventional2016-08-31Recruiting
A Two-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effect of Multiple Doses of Itraconazole and Rifampin on the Single-Dose Pharmacokinetics of Mitapivat Sulfate (AG-348) in Healthy Adult Subjects[NCT03991312]Phase 128 participants (Actual)Interventional2019-06-20Completed
[NCT00935363]Phase 10 participants (Actual)Interventional2010-02-28Withdrawn
An Open-Label Phase 1 Study to Examine the Effect of Multiple Doses of Rifampin on the Single-Dose Pharmacokinetics of VX 770 in Healthy Subjects[NCT01018368]Phase 124 participants (Anticipated)Interventional2009-11-30Completed
Evaluation of the CYP2C9 Activity With Dried Blood Spots on Filter Paper Obtained With a Simple Finger Prick[NCT01026714]Phase 1/Phase 210 participants (Anticipated)Interventional2009-11-30Completed
Study of the Potentiation of the Effects of Clopidogrel by Rifampicin in Healthy Volunteers[NCT00696566]Phase 112 participants (Actual)Interventional2007-11-30Completed
"Single-center, Randomized, Open-label, Two-way Crossover Study to Characterize Phenotyping Metrics of the Basel Cocktail After CYP Induction or Inhibition in Healthy Male Subjects"[NCT01386593]Phase 116 participants (Actual)Interventional2011-05-31Completed
A Phase I, Open Label Study in Healthy Subjects to Evaluate the Effect of Itraconazole and Rifampicin Upon the Pharmacokinetics of a Single Oral Dose of Olorofim.[NCT04171739]Phase 124 participants (Actual)Interventional2019-11-18Completed
An Open-Label Drug Interaction Study to Assess the Pharmacokinetics of JNJ-42847922 When Administered Alone and in Combination With Rifampin in Healthy Male and Female Subjects[NCT02661893]Phase 114 participants (Actual)Interventional2016-01-31Completed
Open-label, Randomized, Multicenter, Controlled, Parallel, Comparative Study of Efficacy and Safety of Treatment of Tuberculosis With Isoniazid, Rifampicin, Ethambutol for Intravenous Infusion in Comparison With Oral Forms While the Intensive Phase of Tre[NCT04150367]166 participants (Actual)Observational2017-03-03Terminated(stopped due to According to Sponsor decision.)
A Phase 1, Open-Label, Drug-Interaction Study to Evaluate the Effect of Rifampin, a Potent CYP3A4 Inducer, on the Systemic Exposure of Pacritinib in Healthy Subjects[NCT02807116]Phase 118 participants (Actual)Interventional2015-01-31Completed
Effect of Rifampin on the Pharmacokinetics of Intravenous (IV) Vinflunine in Subjects With Advanced Cancer[NCT00534807]Phase 10 participants (Actual)Interventional2007-09-30Withdrawn
An Open-Label Clinical Pharmacology Study of Brentuximab Vedotin (SGN-35) in Patients With CD30-Positive Hematologic Malignancies: CYP3A4 Drug-Drug Interactions, Excretion, and Special Populations[NCT01026415]Phase 173 participants (Actual)Interventional2009-12-31Completed
Testing New Strategies for Patients Hospitalised With HIV-associated Disseminated Tuberculosis[NCT04951986]Phase 3732 participants (Anticipated)Interventional2021-08-11Recruiting
Pharmacokinetics and Pharmacodynamics of High Versus Standard Dose Rifampicin in Patients With Pulmonary Tuberculosis in the Kilimanjaro Region, Tanzania.[NCT00760149]Phase 2150 participants (Actual)Interventional2010-07-31Completed
Phenotypic Drug Probes as Predictors of Drug-drug Interactions With Tacrolimus[NCT02576366]Phase 424 participants (Actual)Interventional2016-06-30Completed
Randomized Clinical Trial to Compare a Regimen of Trimethoprim-sulfamethoxazole (TMP-SMX) Plus Rifampicin With a Regimen of Linezolid in the Treatment of Infections Caused by Methicillin-resistant Staphylococcus Aureus (MRSA)[NCT00711854]Phase 4150 participants (Actual)Interventional2009-01-31Completed
Independent Study to Establish the Efficacy of the Six Doses Uniform MDT Regimen (U-MDT) for Leprosy Patients[NCT00669643]Phase 4859 participants (Actual)Interventional2007-02-28Completed
A 3-Part, Open-Label Study to Assess Pharmacokinetic Drug-Drug Interaction Between Avatrombopag When Co-Administered With Fluconazole (Moderate Inhibitor of CYP2C9 and CYP3A), Itraconazole (Strong CYP3A Inhibitor), or Rifampin (Strong CYP3A and Moderate C[NCT02809768]Phase 148 participants (Actual)Interventional2016-04-30Completed
A Phase 1, Fixed Sequence, Cross-Over Study To Estimate The Effect Of Multiple Dose Rifampin On The Single Dose Pharmacokinetics Of Crizotinib (PF-02341066) In Healthy Volunteers[NCT01147055]Phase 115 participants (Actual)Interventional2010-07-31Completed
Pharmacological Interaction of Rifampicin on Clindamycin in Staphylococcic Osteoarticular Infections[NCT02782078]20 participants (Actual)Interventional2017-03-06Completed
Pharmacokinetic and Pharmacodynamic Studies of Efficacy, Tolerability and Safety of Higher Dosage Rifapentine for Treatment of Tuberculosis[NCT01043575]Phase 260 participants (Actual)Interventional2009-04-30Completed
A Randomized Controlled Clinical Trial Comparing Daily Vs. Intermittent 6 - Month Short Course Chemotherapy in Reducing Failures & Emergence of Acquired Rifampicin Resistance (ARR) in Patients With HIV and Pulmonary Tuberculosis[NCT00933790]Phase 3331 participants (Actual)Interventional2009-09-14Completed
Phase I Clinical Trial to Evaluate the Efficacy of Sulforaphane as an Antagonist to Human PXR-mediated Drug-drug Interactions[NCT00621309]Phase 129 participants (Actual)Interventional2008-03-31Completed
A Single Center, Open-label, Single Sequence Study to Evaluate the Potential Drug Interaction of CYP3A4 Inducer Rifampicin With SY-004 Capsules in Healthy Subjects[NCT04907019]Phase 124 participants (Actual)Interventional2021-07-06Completed
A Single Center, Single Arm, Open and Fixed Sequence Study to Investigate the Pharmacokinetic Effects of Rifampicin on Fluzoparib in Healthy Male Subjects[NCT04011124]Phase 116 participants (Actual)Interventional2019-07-24Completed
[NCT01388075]150 participants (Anticipated)Interventional2011-07-31Not yet recruiting
A Randomized, Open-Label, Four-Cohort, Parallel Design Study to Evaluate the Effect of Itraconazole or Rifampin on the Single-Dose Pharmacokinetics of BMS-986205 in Normal Healthy Participants[NCT03346837]Phase 153 participants (Actual)Interventional2017-11-22Completed
An Open-Label, Fixed-Sequence Study to Assess Effects of Steady-State Rifampin on the Single-Dose Pharmacokinetics of Canagliflozin in Healthy Subjects[NCT01395927]Phase 114 participants (Actual)Interventional2011-07-31Completed
Comparing the Efficacy of Two Preventive Regimens for Adult Household Contacts With Latent Tuberculosis Infection[NCT01398618]Phase 3300 participants (Anticipated)Interventional2011-05-31Active, not recruiting
IMPI-3 - A Randomized Controlled Trial of High vs. Standard Dose Rifampicin for Effusive Tuberculous Pericarditis[NCT04521803]Phase 280 participants (Anticipated)Interventional2022-01-10Recruiting
An Open-Label Study to Assess the Effect of CYP3A4 Induction on the Pharmacokinetics of VELCADE (Bortezomib)[NCT00608907]Phase 161 participants (Actual)Interventional2007-09-30Completed
PXR-agonisti Rifampisiinin Vaikutukset Glukoosi-, Lipidi- ja Hormonihomeostaasiin[NCT00985270]Phase 412 participants (Anticipated)Interventional2009-09-30Completed
A Phase 1, Open-label Study in Healthy Adult Subjects to Evaluate Effects of Cytochrome P450 Inhibition and Induction on the Pharmacokinetics of CC-99677 and the Effects of CC-99677 on the Pharmacokinetics of Digoxin, Metformin, Methotrexate, Midazolam, R[NCT04268394]Phase 148 participants (Actual)Interventional2020-03-13Completed
A Phase 1 Two-Part Study to Evaluate the Potential Drug Interactions Between ALXN2050 and Fluconazole, and Between ALXN2050 and Rifampin in Healthy Adult Participants[NCT04933682]Phase 116 participants (Actual)Interventional2021-06-23Completed
Phase I/II Study of the Effects of Antibiotics on Sarcoidosis Pathogenesis[NCT01074554]Phase 1/Phase 230 participants (Actual)Interventional2010-02-28Completed
An Open-label, 3-period Fixed-sequence Study in Healthy Subjects to Assess the Pharmacokinetics of Savolitinib When Administered Alone and in Combination With Rifampicin[NCT04118842]Phase 140 participants (Actual)Interventional2019-10-17Completed
A Phase 1, Open-label, 2-part Study to Evaluate the Effect of Rifampin and Efavirenz on the Pharmacokinetics of Fedratinib in Healthy Adult Subjects[NCT03983239]Phase 132 participants (Actual)Interventional2019-06-21Completed
The Effect of Rifapentine on Plasma Concentrations of Raltegravir[NCT00809718]Phase 127 participants (Actual)Interventional2009-02-28Completed
Comparative Evaluation of Intensified Short Course Regimen and Standard Regimen for Adults TB Meningitis : an Open-label Randomized Controlled Trial[NCT05917340]Phase 3372 participants (Anticipated)Interventional2024-03-31Not yet recruiting
A Phase 1, Open-Label, Drug Interaction Study to Evaluate the Effect of Repeat Doses of Rifampin on the Single-Dose Pharmacokinetics of Mirabegron (YM178)[NCT00776516]Phase 124 participants (Actual)Interventional2008-10-31Completed
CSP #2001 - Investigation of Rifampin to Reduce Pedal Amputations for Osteomyelitis in Diabetics (VA Intrepid)[NCT03012529]Phase 4880 participants (Anticipated)Interventional2018-01-22Recruiting
Pharmacokinetics of Standard First and Second Line Anti-TB Drugs in the Lung and Lesions of Subjects Elected for Resection Surgery[NCT00816426]Phase 119 participants (Actual)Interventional2008-12-29Completed
A Phase 1 Open-label, Two-cohort, One-sequence Crossover Study to Investigator the Effect of P-glycoprotien Inhibitor (Itraconazole) and Inducer (Rifampin) on the Pharmacokinetics, Safety, and Tolerability of Sitravatinib in Health Subjects[NCT05255276]Phase 136 participants (Actual)Interventional2022-01-29Completed
A Randomised Controlled Trial Comparing the Effectiveness of Heparin Bonded or Antibiotic Impregnated Central Venous Catheters (CVCs) With Standard CVCs for the Prevention of Hospital Acquired Blood Stream Infection in Children[NCT01029717]Phase 31,859 participants (Actual)Interventional2010-12-31Completed
Phase 2C Clinical Trial of Novel, Short-course Regimens for the Treatment of Pulmonary Tuberculosis: CRUSH-TB (Combination Regimens for Shortening TB Treatment)[NCT05766267]Phase 2/Phase 3288 participants (Anticipated)Interventional2023-03-01Not yet recruiting
EVRIOS : Comparative Evaluation of Low Versus High Doses of Rifampicin in the Treatment of Staphylococcal Bone and Joint Infections[NCT02599493]Phase 4544 participants (Actual)Interventional2016-01-31Completed
A Phase I Open-label, Single-center Study to Assess the Effect of the CYP3A4 Inducer Rifampicin on the Pharmacokinetics of a 75 mg Single Oral Dose of Selumetinib (AZD6244; ARRY-142886) (Hyd-Sulfate) in Healthy Volunteers Aged 18 to 45 Years[NCT02046850]Phase 124 participants (Anticipated)Interventional2014-02-28Completed
A Phase 4, Single-center, Open-label, Parallel Study to Evaluate the Drug Interaction Between Albuvirtide (ABT) and Rifampin(RIF) in Healthy Adult Subjects[NCT04006353]Phase 424 participants (Actual)Interventional2019-07-11Completed
Phase 3 Trial to Assess the Efficacy of Long-term (6 Months) Combination Antibiotics as a Treatment for Chlamydia-induced Reactive Arthritis[NCT00351273]Phase 342 participants (Actual)Interventional2006-05-31Completed
Clinical Trial of Short Course Rifampin Versus INH for LTBI in Jail[NCT00128206]Phase 3364 participants (Actual)Interventional2004-11-30Completed
Effect of Rifampin on the Pharmacokinetics of Dapagliflozin in Healthy Subjects[NCT01068756]Phase 114 participants (Actual)Interventional2010-03-31Terminated
Effect of Rifampin on the Pharmacokinetics of Ixabepilone in Patients With Advanced Cancer[NCT00207090]Phase 119 participants (Actual)Interventional2005-09-30Completed
[NCT01932268]Phase 22 participants (Actual)Interventional2011-01-31Completed
A Phase 2a Study of the Early Bactericidal Activity of Rifampin (RIF) in Combination With Meropenem Plus Amoxicillin/Clavulanate Among Adults With Rifampin-resistant or Rifampin-susceptible Pulmonary Tuberculosis[NCT03174184]Phase 2112 participants (Actual)Interventional2017-08-23Completed
A Phase 1, Open-Label, Single-Sequence, 2-Period Study to Evaluate the Effect of Rifampin (a CYP3A Inducer) on the Pharmacokinetics of IPI-145 in Healthy Subjects[NCT01947777]Phase 114 participants (Actual)Interventional2013-10-31Completed
A Phase 1, Open-Label Fixed-Sequence 2-Period Study To Investigate The Effect Of Multiple Doses Of Rifampin On Palbociclib (PD-0332991) Pharmacokinetics In Healthy Volunteers[NCT01953731]Phase 115 participants (Actual)Interventional2013-10-31Completed
An Open-label Study to Evaluate the Effects of a Potent CYP3A4 Inducer and the Effects of a pH Elevating Agent on the Repeat Dose Pharmacokinetics of Dabrafenib (GSK2118436) in Subjects With BRAF V600 Mutation Positive Tumors[NCT01954043]Phase 123 participants (Actual)Interventional2013-12-20Completed
Phase 1, Open-label, Parallel, 2-arm, Fixed-sequence Study to Investigate the Effect of Coadministration of CYP3A4 Inhibitor and CYP3A4 Inducer on the Pharmacokinetics, Safety, and Tolerability of KBP-5074 in Healthy Subjects[NCT04606537]Phase 124 participants (Actual)Interventional2020-10-24Completed
Controlled Trial: 5-day Course of Rifampin Versus Doxycycline for the Treatment of Mild to Moderate Scrub Typhus[NCT00568711]476 participants (Actual)Interventional2006-09-30Completed
Investigation of the Efficacy of Antimycobacterial Therapy on Pulmonary Sarcoidosis Phase II Randomized, Double-blind, Placebo-controlled Trial[NCT02024555]Phase 297 participants (Actual)Interventional2014-03-31Completed
The Treatment of Pulmonary Mycobacterium Tuberculosis in HIV Infection[NCT00001033]Phase 3650 participants InterventionalCompleted
Phase I Dose Escalation Study of the Pharmacokinetics, Safety and Tolerability of Rifapentine and the Effects of Increasing Doses of Rifapentine on Induction of Metabolizing Enzymes in Healthy Volunteers[NCT01162486]Phase 137 participants (Actual)Interventional2010-04-30Completed
A Phase I, Open-label, Fixed-Sequence Study to Evaluate the Effect of Multiple-dose Itraconazole or Rifampicin Capsules on the Single-dose PK (Pharmacokinetics) Profiles of IMP4297 Capsules in Healthy Subjects[NCT04584515]Phase 132 participants (Actual)Interventional2020-11-02Completed
An Open-Label Study of the Effect of Tesetaxel on the QTc Interval and the Effect of Food, Itraconazole, and Rifampin on Tesetaxel Pharmacokinetics in Patients With Advanced Solid Tumors[NCT04312282]Phase 193 participants (Actual)Interventional2020-03-06Terminated(stopped due to The Sponsor has discontinued the development of tesetaxel)
A Study of the Pharmacokinetic and Pharmacodynamic Interactions Between Bictegravir, Tenofovir Alafenamide and Rifapentine in Healthy Adult Subjects[NCT04551573]Phase 40 participants (Actual)Interventional2021-05-31Withdrawn(stopped due to COVID-19 Pandemic)
A Phase I Open-label Trial to Investigate the Pharmacokinetic Interaction Between Rifapentine or Rifampicin and a Single Dose of TMC207 in Healthy Subjects[NCT02216331]Phase 132 participants (Actual)Interventional2010-03-31Completed
Beta-Lactam Containing Regimen for the Shortening of Buruli Ulcer Disease Therapy: Comparison of 8 Weeks Standard Therapy (Rifampicin Plus Clarithromycin) vs. 4 Weeks Standard Plus Amoxicillin/Clavulanate Therapy [RC8 vs. RCA4][NCT05169554]Phase 2140 participants (Anticipated)Interventional2021-12-01Recruiting
A Phase IIc Trial of Clofazimine- and Rifapentine-Containing Treatment Shortening Regimens in Drug-Susceptible Tuberculosis: The CLO-FAST Study[NCT04311502]Phase 2104 participants (Actual)Interventional2021-06-16Active, not recruiting
A Phase 1 Study to Assess the Effect of Rifampin on the Pharmacokinetics of ABT-199[NCT01969682]Phase 10 participants (Actual)Interventional2014-04-30Withdrawn(stopped due to This study will be conducted in healthy volunteer subjects.)
Open, Noncomparative Trial of Multidrug Regimens Containing Azithromycin and Rifabutin Administered Three Times Per Week for the Treatment of M. Avium Complex (MAC) Lung Disease[NCT00598962]Phase 458 participants (Actual)Interventional1994-12-31Completed
Reducing Early Mortality and Early Morbidity by Empiric Tuberculosis Treatment Regimens (REMEMBER)[NCT01380080]Phase 4851 participants (Actual)Interventional2011-10-31Completed
A Phase I Open-label, 2-period Study to Evaluate the Influence of Multiple Oral Doses of Rifampin on the Single Dose Pharmacokinetics of Romidepsin in Subjects With Advanced Cancer[NCT01324323]Phase 114 participants (Actual)Interventional2011-04-01Completed
Investigation of the Efficacy of Antibiotics on Pulmonary Sarcoidosis[NCT01169038]Phase 115 participants (Actual)Interventional2010-07-31Completed
A Multicentric Randomized Double-Blind Phase 3 Trial Evaluating the Efficacy of an Adapted Antibiotherapy in Hurley Stage 2 Active Hidradenitis Suppurativa Patients Versus Tetracycline Derivative[NCT05821478]Phase 392 participants (Anticipated)Interventional2023-11-15Not yet recruiting
Dose-Finding and Pharmacogenetic Study of Efavirenz in HIV-infected and HIV/TB Co-infected Infants and Children 3 Months to Less Than 36 Months of Age[NCT00802802]Phase 167 participants (Actual)Interventional2010-02-10Completed
A National, Multicenter, Non-comparative Study Evaluating the Efficacy of the Combination of Levofloxacin (500 mg) and Rifampicin (600 or 900 mg Depending on Weight) Administered Once Daily by Oral Route, as Replacement of Empirical Antibiotic Therapy Giv[NCT00906048]Phase 310 participants (Actual)Interventional2009-04-30Terminated(stopped due to lack of recruitment)
An Open-label, Three-treatment, Three-period, One-sequence, Crossover Study to Evaluate the Effect of Ketoconazole and Rifampicin on the Pharmacokinetics of Fimasartan in Healthy Male Volunteers[NCT00938262]Phase 124 participants (Actual)Interventional2009-04-30Completed
Epidemiology and Treatment of Small-colony Variant Staphylococcus Aureus in Cystic Fibrosis[NCT02547116]Phase 40 participants (Actual)Interventional2020-12-31Withdrawn(stopped due to Administrative delay)
A Study of the Effect of Concomitant Administration of Rifampin on the Pharmacokinetics of BMS-708163 in Healthy Subjects[NCT01002079]Phase 120 participants (Actual)Interventional2010-08-31Completed
Efficacy of Thrice Weekly Intermittent Short Course Antituberculosis Chemotherapy in Tuberculosis Patients With and Without HIV Infection[NCT00698334]Phase 3150 participants (Anticipated)Interventional2006-04-30Completed
An Open-Label Fixed-Sequence Study to Assess the Effects of Itraconazole and Rifampicin on the Single-Dose Pharmacokinetics of JNJ-53718678 in Healthy Adult Subjects[NCT02729467]Phase 133 participants (Actual)Interventional2016-03-31Completed
A Single Center, Two Part, Randomized, Open Label Cross-over Study to Evaluate the Effect of Itraconazole and Rifampicin on the Pharmacokinetics of GSK525762 in Healthy Female Subjects of Non Child Bearing Potential[NCT02706535]Phase 129 participants (Actual)Interventional2016-05-05Completed
A Single-center, Open-label, Randomized, Two-part, Two-treatment, Two-period Crossover Study to Investigate the Effect of Gemfibrozil or Rifampicin on the Pharmacokinetics of Selexipag and Its Metabolite ACT-333679 in Healthy Male Subjects.[NCT02770222]Phase 140 participants (Actual)Interventional2016-06-30Completed
An Open-Label, Fixed-Sequence, Clinical Drug Interaction Study to Evaluate The Effect of a CYP3A-Inducer, Rifampin, on the Pharmacokinetics of Vonoprazan in Healthy Volunteers[NCT04558216]Phase 10 participants (Actual)Interventional2020-09-30Withdrawn(stopped due to Withdrawn due to unavailability of rifampin for clinical trial use)
A Prospective, Randomized Controlled Study for the Efficacy and Safety of the Substitution of Pyrazinamide and Ethambutol With Moxifloxacin During the Intensive Phase of Treatment of Pulmonary Tuberculosis[NCT04187469]286 participants (Anticipated)Interventional2020-03-01Not yet recruiting
A Drug-Drug Interaction Study to Evaluate the Effects of Strong CYP3A Induction and Inhibition on the Pharmacokinetics of Segesterone Acetate and Ethinyl Estradiol From the Annovera™ Contraceptive Vaginal System[NCT04290390]Phase 167 participants (Actual)Interventional2020-02-12Completed
CLArithromycin Versus AZIthromycin in the Treatment of Mycobacterium Avium Complex (MAC) Lung Infections[NCT03236987]Phase 3424 participants (Anticipated)Interventional2018-02-05Recruiting
Rifabutin Versus Rifampicin for Treatment of Staphylococcal Prosthetic Joint Infection Treated With Debridement, Antibiotics and Implant Retention (DAIR Strategy): a Multicenter Randomized, Open-label, Non-inferiority Trial[NCT04672525]Phase 3436 participants (Anticipated)Interventional2021-11-08Recruiting
A 2-Part, Open-Label, Fixed-Sequence Study to Evaluate the Effects of Multiple Doses of Itraconazole and Rifampin on the Single-Dose Pharmacokinetics of LOXO-292 in Healthy Adult Subjects[NCT05338489]Phase 124 participants (Actual)Interventional2018-05-11Completed
A Phase IIA Dose Ranging Trial to Evaluate the Safety, Tolerability, Extended Early Bactericidal Activity and Pharmacokinetics of Higher Doses of Rifampicin in Adult Subjects With Newly Diagnosed, Uncomplicated, Smear-Positive, Pulmonary Tuberculosis[NCT01392911]Phase 2128 participants (Anticipated)Interventional2011-06-30Completed
Different Reintroduction Regimens of Antituberculosis Drugs After Development of Hepatitis During Anti-tuberculosis Treatment[NCT01395654]Phase 4100 participants (Anticipated)Interventional2011-07-31Recruiting
A Phase 1 Study To Assess the Effect of Rifampin on the Pharmacokinetics of Linifanib in Subjects With Advanced or Metastatic Solid Tumors[NCT01401933]Phase 114 participants (Actual)Interventional2011-05-31Completed
An Open-label, One-sequence Study to Evaluate the Effect of Multiple Doses of Rifampicin on the Pharmacokinetics of YM150 (Darexaban) and Metabolites in Young Healthy Male Subjects[NCT01406002]Phase 126 participants (Actual)Interventional2010-01-31Completed
A Single Arm, 3 Phase Study to Determine the Effect of Intermittent Dosing of Rifampicin on the Pharmacokinetics of Raltegravir in Healthy Volunteers[NCT01424826]Phase 118 participants (Actual)Interventional2012-01-31Completed
A Randomized, Open-Label, Drug-Drug Interaction Study To Evaluate The Effect Of Ketoconazole Or Rifampicin On The Pharmacokinetic Characteristics And Safety Of Lc15-0444 In Healthy Male Volunteers[NCT01426906]Phase 124 participants (Actual)Interventional2011-01-31Completed
Co-SAM: An Adaptive Multi-arm Trial to Improve Clinical Outcomes Among Children Recovering From Complicated Severe Acute Malnutrition[NCT05994742]Phase 31,266 participants (Anticipated)Interventional2024-03-01Not yet recruiting
Rifampin Combination Therapy Versus Monotherapy in Early Staphylococcal Infections After Total Hip and Knee Arthroplasty[NCT00423982]Phase 4100 participants (Anticipated)Interventional2006-04-30Active, not recruiting
Safety, Tolerability, and Pharmacokinetic Interactions of Atazanavir and Rifampin in Healthy Volunteers[NCT00096850]18 participants (Actual)InterventionalCompleted
[NCT01756924]Phase 214 participants (Actual)Interventional2012-12-31Terminated(stopped due to This study has been terminated; alternative study designs are being considered. Fusidic acid remains available under an Expanded Access Protocol.)
Effect of Rifampicin on the Pharmacokinetics of Apatinib in Chinese Healthy Volunteers[NCT02836821]Phase 120 participants (Actual)Interventional2016-05-31Completed
An Open-Label, Two Period, Fixed Sequence Study of Healthy Subjects to Assess the Effect of Repeat Oral Dosing of [Rifampin] on the Pharmacokinetics of a Single Oral Dose of [GW679769][NCT00405080]Phase 112 participants (Actual)Interventional2006-11-11Completed
Impact of LTBI Treatment on Glucose Tolerance and Chronic Inflammation[NCT04830462]Phase 432 participants (Actual)Interventional2021-04-15Completed
Effects of Rifampicin on the Pharmacokinetics and Pharmacodynamics of Sublingual and Intravenous Buprenorphine: A Four-phase Cross-over Study in Healthy Subjects.[NCT01854489]Phase 412 participants (Actual)Interventional2013-04-30Completed
A Phase I Study to Evaluate Drug-Drug Interaction of TQ05105 Tablets[NCT06024915]Phase 140 participants (Anticipated)Interventional2023-09-30Not yet recruiting
A Phase 1, Open-Label, Fixed-Sequence Study to Evaluate CYP3A4-Mediated, Oral Contraceptive, and pH Modifier Drug Interactions for ABI-H2158 in Healthy Adult Subjects[NCT04142762]Phase 180 participants (Actual)Interventional2019-10-18Completed
A Phase 1, Open-label Study to Evaluate the Effect of Rifampin on the Single Dose Pharmacokinetics, Safety, and Tolerability of BMS-986235 in Healthy Participants[NCT04301310]Phase 10 participants (Actual)Interventional2020-03-09Withdrawn(stopped due to Business objectives have changed)
A Phase 2 Randomized, Open-label Trial of Daily Rifapentine 450mg or 600mg in Place of Rifampicin 600mg for Intensive Phase Treatment of Smear-positive Pulmonary Tuberculosis[NCT00814671]Phase 2153 participants (Actual)Interventional2010-04-30Completed
A Phase 2b/c, Multi-Arm, 2-Stage, Duration Randomized Trial of the Efficacy and Safety of Two to Four Months Treatment With Regimens Containing Bedaquiline, OPC-167832, and Sutezolid, Plus Either Pretomanid or Delamanid, in Adults With Pulmonary Tuberculo[NCT05971602]Phase 2514 participants (Anticipated)Interventional2023-07-26Recruiting
Prophylaxis Against Tuberculosis (TB) in Patients With Human Immunodeficiency Virus (HIV) Infection and Confirmed Latent Tuberculous Infection[NCT00000636]2,000 participants InterventionalCompleted
A Phase II Randomized, Open-label Trial of a Rifapentine Plus Moxifloxacin-Based Regimen for Intensive Phase Treatment of Smear-Positive Pulmonary Tuberculosis[NCT00728507]Phase 2121 participants (Actual)Interventional2009-11-30Terminated(stopped due to Funding withdrawn)
Effects of Treatment With Doxycycline and Rifampicin on Biomarkers of Alzheimer's Disease in the Cerebrospinal Fluid[NCT00439166]Phase 3100 participants (Actual)Interventional2007-02-28Completed
A Randomized, Single-center, Open-label, One-sequence, Two-period Crossover Study in 3 Parts to Investigate the Effects of Multiple Doses of Ketoconazole (Part 1), Rifampicin (Part 2), and Ritonavir-boosted Atazanavir (Part 3) on the PK of a Single Dose o[NCT01591850]Phase 151 participants (Actual)Interventional2011-09-30Completed
[NCT02275962]Phase 120 participants (Actual)Interventional2014-09-30Completed
Randomized Non-inferiority Trial Comparing the Nevirapine-based Antiretroviral Therapy Versus the Standard Efavirenz-based ART for the Treatment of HIV-TB Co-infected Patients on Rifampicin-based Therapy (ANRS 12146 CARINEMO)[NCT00495326]Phase 2/Phase 3570 participants (Actual)Interventional2007-12-31Completed
An Open-label, Single-sequence Study in Two Cohorts of Healthy Subjects to Evaluate the Single-dose Pharmacokinetics of Tasimelteon Alone and in Combination With a CYP3A4 Inhibitor, Ketoconazole, or a CYP3A4 Inducer, Rifampin.[NCT01637636]Phase 148 participants (Actual)Interventional2012-06-30Completed
Evaluation of Three Regimens of Chemoprophylaxis for Tuberculosis in Patients co-Infected by HIV and Mycobacterium Tuberculosis[NCT00402454]Phase 4300 participants Interventional1994-01-31Completed
A Single-Center, Single-Arm, Open-Label, Fixed-Sequence Phase I Drug-Drug Interaction Clinical Study of the Effect of Rifampicin on Pharmacokinetics of SHR1459 in Chinese Healthy Subjects.[NCT04649723]Phase 120 participants (Actual)Interventional2020-11-24Completed
Effects of Rifampicin on the Pharmacokinetics of BI 425809 Following Oral Administration in Healthy Male Subjects (an Open-label, Two-period, Fixed-sequence Trial)[NCT03082183]Phase 116 participants (Actual)Interventional2017-03-28Completed
A Phase 1, Open-Label, 4-Part, Fixed-Sequence Study to Assess the Effect of Itraconazole, a Strong CYP3A Inhibitor, the Effect of Fluconazole, a Moderate CYP3A/2C9 Inhibitor, the Effect of Rifampin, a Strong CYP3A Inducer, and the Effect of Rabeprazole, a[NCT05602597]Phase 159 participants (Actual)Interventional2022-06-01Completed
Mind the Gaps: Pharmacokinetic Research to Advance Pediatric HIV/TB Cotreatment and TB Prevention[NCT05069688]Phase 120 participants (Anticipated)Interventional2023-07-07Recruiting
A Phase 1 Study of Oral TAK-788 to Evaluate the Drug-Drug Interaction With Itraconazole and Rifampin in Healthy Adult Subjects[NCT03928327]Phase 124 participants (Actual)Interventional2019-05-02Completed
A Study In Healthy Subjects To Assess The Effects Of Rifampicin Capsules and Probenecid Tablets On The Pharmacokinetic Profile Of Rongliflozin Capsules[NCT05497674]Phase 128 participants (Actual)Interventional2022-02-21Completed
Comparison of Two- Versus Three-antibiotic Therapy for Pulmonary Mycobacterium Avium Complex Disease[NCT03672630]Phase 2/Phase 3500 participants (Anticipated)Interventional2019-02-22Recruiting
A Phase 1, Open Label, Fixed Sequence Study to Assess the Pharmacokinetics of Brensocatib When Administered Alone and With Multiple Doses of Rifampin (CYP3A Inducer) or Esomeprazole (Proton Pump Inhibitor) in Healthy Subjects[NCT05826574]Phase 132 participants (Actual)Interventional2023-05-10Completed
TBTC Study 28: Evaluation of a Moxifloxacin-based, Isoniazid-sparing Regimen for Tuberculosis Treatment[NCT00144417]Phase 2433 participants (Actual)Interventional2006-02-28Completed
The Effect of CYP3A Induction by Rifampicin on the Pharmacokinetics of Baricitinib in Healthy Subjects[NCT01910311]Phase 118 participants (Actual)Interventional2013-08-31Completed
TBTC Study 27: An Evaluation of the Activity and Tolerability of Moxifloxacin During the First Two Months of Treatment for Pulmonary Tuberculosis--A Double-Blind, Randomized, Multicenter Study by the Tuberculosis Trials Consortium[NCT00140309]Phase 2350 participants Interventional2003-07-31Completed
A Single-center, Randomized, Double-blind, Two-period Cross-over Study to Investigate the Effect of Rifampicin on the Pharmacokinetics of Clazosentan in Healthy Male Subjects[NCT03596294]Phase 114 participants (Actual)Interventional2018-07-19Completed
An Open-label, 3-Treatment, 3-Period, Fixed Sequence Study in Healthy Subjects to Assess the Pharmacokinetics of Verinurad and Allopurinol When Administered Alone, and in Combination With Single Doses of Cyclosporine or Rifampicin[NCT04532918]Phase 114 participants (Actual)Interventional2020-09-10Completed
Double-Blind, Placebo-Controlled Study of Rifampicin in Multiple System Atrophy[NCT01287221]Phase 3100 participants (Actual)Interventional2011-03-31Terminated(stopped due to DSMB recommended stopping the study after an interim analysis of the primary endpoint revealed that futility criteria were met.)
A Phase 1, Open-label Drug-drug Interaction Study to Evaluate the Effects of Omeprazole and Rifampin on the Pharmacokinetics of VX-548 in Healthy Subjects[NCT05635110]Phase 131 participants (Actual)Interventional2022-12-15Completed
Ph. 1, Open-label, 2 Part, 2 Period Fixed-Sequence Crossover Study to Assess the Effect of Rabeprazole, a Proton Pump Inhibitor, and the Effect of Rifampin, a Strong CYP3A Inducer, on the Pharmacokinetics of Surufatinib in Healthy Subjects[NCT04510649]Phase 128 participants (Actual)Interventional2020-07-09Completed
Pharmacokinetics of Antituberculosis Agents in HIV-Infected Persons With Tuberculosis[NCT00000950]50 participants InterventionalCompleted
An Open-label, Fixed-sequence, Three-period, Single Group Study to Investigate the Effects of Rifampicin as an OATP1B1 Inhibitor and a CYP2C8 Inducer on the Pharmacokinetics of Aleglitazar in Healthy Subjects[NCT01679639]Phase 124 participants (Actual)Interventional2012-08-31Completed
Phase I/II Randomized, Open-label Trial to Evaluate the PK, Safety, and Outcomes of Treatment Including High Dose Rifampicin +/- Levofloxacin vs Standard Treatment for Pediatric Tuberculous Meningitis (TBM)[NCT02958709]Phase 1/Phase 238 participants (Actual)Interventional2017-02-22Completed
An Open-label, Fixed-sequence, 3-period, 3-treatment, Crossover Study to Assess the Effects of Rifampin on Pharmacokinetics of NKTR-118 in Healthy Subjects[NCT01533870]Phase 122 participants (Actual)Interventional2012-03-31Completed
TBTC Study 24: A Non-Comparative Study of the Efficacy of a Largely-Intermittent, Six-Month Tuberculosis Treatment Regimen Among Patients Who Will Not Receive Isoniazid Due to Initial Isoniazid Resistance or Intolerance[NCT00023374]98 participants (Actual)Interventional2000-08-31Completed
A Phase II/III Trial of Rifampin, Ciprofloxacin, Clofazimine, Ethambutol, and Amikacin in the Treatment of Disseminated Mycobacterium Avium Infection in HIV-Infected Individuals.[NCT00000641]Phase 290 participants InterventionalCompleted
Antibiotic Treatment Trial Directed Against Chlamydia Pneumonia in Multiple Sclerosis[NCT00043264]Phase 240 participants InterventionalCompleted
Study on Food Influence and Drug-drug Interaction of HLX208 Tablets in Chinese Healthy Subjects[NCT05902728]Phase 152 participants (Anticipated)Interventional2023-07-04Not yet recruiting
Study of Safety and Efficacy of Different Regimes of Reintroduction of Anti-TB Drugs in Antituberculosis Treatment Induced Hepatotoxicity[NCT00405301]Phase 4175 participants (Actual)Interventional2006-12-31Completed
Effect of Rifampicin on the Pharmacokinetics of BI 409306 Following Oral Administration in Healthy Male Subjects (an Open-label, Two-period, Fixed Sequence Trial)[NCT03151499]Phase 115 participants (Actual)Interventional2017-05-30Completed
Intensive Pharmacokinetic Study of Three Doses of Rifapentine (600, 900 and 1200mg) During Continuation Phase Therapy of Tuberculosis in HIV-Negative Adults[NCT00023387]36 participants Interventional2000-03-31Completed
Trial of Rifampin and Azithromycin for Treatment of Endosymbiotic Bacteria (Wolbachia) in Onchocerca Volvulus in Guatemala[NCT00127504]Phase 280 participants Interventional2003-07-31Completed
A Randomized Trial of Three Regimens to Prevent Tuberculosis in HIV-Infected Patients With Anergy[NCT00402610]Phase 4332 participants Interventional1994-01-31Completed
Short-Course Isoniazid and Rifampin Compared With Isoniazid for Latent Tuberculosis Infection: A Randomized Clinical Trial.[NCT00397709]Phase 4228 participants Interventional1996-03-31Terminated
A Randomized Trial to Compare Effectiveness of 4 Months Rifampin (4 RIF) With 9 Months Isoniazid (9 INH) in the Prevention of Active TB in Children: The P4v9 Trial[NCT00170209]Phase 3844 participants (Actual)Interventional2011-08-31Completed
Relative Bioavailability of a Single Oral Dose of 40 mg Afatinib Given Alone and After Multiple Doses of Rifampicin - an Open-label, Two-period, Fixed Sequence Clinical Phase I Trial in Healthy Male Volunteers[NCT01396265]Phase 122 participants (Actual)Interventional2011-07-31Completed
Novel TB Prevention Regimens for HIV-Infected Adults[NCT00057122]Phase 31,148 participants (Actual)Interventional2002-09-30Completed
Rifampin to Reduce Elevated Levels of Blood and Urine Calcium in Patients With Inactivating Mutations in the CYP24A1 Gene[NCT03301038]Phase 230 participants (Anticipated)Interventional2018-07-25Recruiting
A Phase 1, Open-label, Fixed-sequence, 2-period Study In Healthy Volunteers To Investigate The Effect Of Multiple Doses Of Rifampin On Single Dose Glasdegib (Pf-04449913) Plasma Pharmacokinetics[NCT02430545]Phase 112 participants (Actual)Interventional2015-05-31Completed
A Non-Randomized, Open-Label, Two-Part, Drug-Drug Interaction Study to Evaluate the Effects of Itraconazole and Rifampin on the Pharmacokinetics and Safety of EDP-305 in Healthy Volunteers[NCT03213145]Phase 148 participants (Actual)Interventional2017-07-11Completed
A Randomised Placebo - Controlled Double Blind Trial Comparing 1) a Two Month Intensive Phase of Ethambutol, Moxifloxacin, Rifampicin, Pyrazinamide Versus the Standard Regimen (Ethambutol, Isoniazid, Rifampicin, Pyrazinamide) and 2) a Treatment Shortening[NCT00864383]Phase 31,931 participants (Actual)Interventional2008-01-31Completed
A Multiple Arm, Multiple Stage, Phase 2, OL, Randomized, Controlled Trial to Evaluate 4 Treatment Regimens of SQ109, Increased Doses of Rifampicin, and Moxifloxacin in Adults With Newly Diagnosed, Smear-positive Pulmonary Tuberculosis[NCT01785186]Phase 2365 participants (Actual)Interventional2013-04-30Completed
An Open-label Fixed Sequence Trial to Investigate the Potential Drug-drug Interaction When BI 907828 is Co-administered With an OATP1B1 and/or OATP1B3 Transporter Inhibitor or With a CYP3A4 Inhibitor in Patients With Various Solid Tumours[NCT05372367]Phase 132 participants (Anticipated)Interventional2022-06-30Recruiting
Prediction of Potential Drug Interaction With CYP2C9 Substrate by Using Phenytoin Metabolic Ratio as a Marker of Its Activity in-Vivo.[NCT00226538]16 participants Interventional1999-08-31Completed
A Phase 1 Open-label 2-Part 2-Period Fixed-sequence Crossover Study To Assess The Effect Of Itraconazole, A Strong CYP3A Inhibitor, And The Effect Of Rifampin, A Strong CYP3A Inducer, On Pharmacokinetics Of Fruquintinib In Healthy Subjects[NCT04557397]Phase 128 participants (Actual)Interventional2020-09-02Completed
Immune Activation and Drug Absorption in HIV-Infected Patients[NCT01845298]7 participants (Actual)Interventional2014-06-30Completed
Phase 2 Trial to Evaluate the Early EBA, Safety and Tolerability of Amoxicillin/Clavulanate With or Without Meropenem, Ertapenem or Rifampicin in Adults With Newly Diagnosed, Smear-Positive Rifampicin-Susceptible Pulmonary Tuberculosis[NCT05896930]Phase 2134 participants (Actual)Interventional2017-11-09Completed
A Phase 2 Dose-ranging Trial to Evaluate the Bactericidal Activity, Safety, Tolerability and Pharmacokinetics of Linezolid in Adult Subjects With Newly Diagnosed Drug-Sensitive, Smear-Positive Pulmonary Tuberculosis.[NCT02279875]Phase 2113 participants (Actual)Interventional2014-11-30Completed
A Phase I, Single Center, Open-label, One-sequence Cross-over Study to Investigate the Effect of a Potent Inducer Rifampicin on the Pharmacokinetics of Deferasirox in Healthy Volunteers[NCT00419172]Phase 122 participants (Anticipated)Interventional2007-01-31Completed
A Phase 2 Randomized, Open-Label Trial of PA-824-Containing Regimens Versus Standard Treatment for Drug-Sensitive Sputum Smear-Positive Pulmonary Tuberculosis[NCT02256696]Phase 2157 participants (Actual)Interventional2015-04-29Completed
Vancomycin Versus Vancomycin Plus Gentamycin For Treating Bacteremic Infection Due to Methicillin-Resistant Staphylococcus Aureus (MRSA)[NCT00304811]Phase 4160 participants (Anticipated)Interventional2006-01-31Completed
Efficacy and Safety of Short-course Treatment for Drug-sensitive Tuberculosis in China[NCT05401071]Phase 2/Phase 32,442 participants (Anticipated)Interventional2023-01-13Recruiting
Treatment of Methicillin-sensitive Staphylococcus Aureus Orthopaedic Infections With Clindamycin in Combination With Rifampin or Levofloxacin: a Randomized Pharmacological and Clinical Study (the CLINDOS Trial)[NCT01500837]23 participants (Actual)Interventional2010-10-31Completed
Effect of P-gp Inhibition, OATP-inhibition and Food on the Kinetics of a Single Oral Dose BI 685509 in Healthy Male Subjects[NCT03116893]Phase 115 participants (Actual)Interventional2017-04-19Completed
An Open-Label Drug-Drug Interaction Study to Assess the Effect of Rifampicin on the Pharmacokinetics of Abiraterone (JNJ-589485) Following Administration of Abiraterone Acetate (JNJ-212082) Tablets in Healthy Male Subjects[NCT01655147]Phase 119 participants (Actual)Interventional2012-01-31Completed
A Single-center, Open, Self-controlled Design Clinical Study to Evaluate the Pharmacokinetic Effects of Rifampicin or Itraconazole on Single-dose Laolotinib Mesylate Capsules in Healthy Subjects[NCT05057949]Phase 132 participants (Anticipated)Interventional2021-11-24Active, not recruiting
The Effect of PXR Activation on Blood Pressure Regulation[NCT01690104]Phase 422 participants (Actual)Interventional2012-08-31Completed
Implementation for Tuberculosis Preventive Therapy Among Latent Tuberculosis Infection in HIV-infected Individuals Using Novel Regimen of Isoniazid/Rifapentine Daily (4 Weeks) Compared to Isoniazid/Rifapentine Weekly (12 Weeks)[NCT03785106]Phase 32,500 participants (Anticipated)Interventional2019-08-15Recruiting
Efficacy, Security, Adherence, Tolerability and Cost Effectiveness of Latent TB Treatment in Patients With TB/DM2[NCT03278483]Phase 4396 participants (Actual)Interventional2019-02-28Completed
Hypertonic Saline for Treatment of Pulmonary Mycobacterium Avium Complex (MAC) Disease[NCT04921943]Phase 450 participants (Anticipated)Interventional2021-05-18Recruiting
Prospective,Randomized,Open Label,European Multicenter Study of the Efficacy of the Linezolid-rifampin Combination Versus Standard of Care in the Treatment of Gram-positive.[NCT01757236]Phase 2100 participants (Anticipated)Interventional2012-10-31Recruiting
Identification and Evaluation of Endogenous Markers for the Assessment of CYP3A Activity in Female Subjects Using Metabolomics[NCT01760642]Phase 116 participants (Actual)Interventional2012-12-31Completed
An Open-Label, Sequential Design Study to Assess the Effect of Rifampin on the Pharmacokinetics of PCI-32765 in Healthy Subjects[NCT01763021]Phase 118 participants (Actual)Interventional2012-12-31Completed
Randomized Double Blind Comparison of an Antibiotic Impregnated PICC Catheter Versus a Regular PICC Catheter in a Tertiary Care Setting[NCT01765738]Phase 20 participants (Actual)Interventional2013-02-28Withdrawn(stopped due to Project never received funding.)
A Phase 1, Open-Label Study to Examine the Effect of Ciprofloxacin, Itraconazole, and Rifampin on the Pharmacokinetics of Lumacaftor in Combination With Ivacaftor in Healthy Adult Subjects[NCT01768663]Phase 180 participants (Actual)Interventional2013-01-31Completed
Evaluation of the Pharmacokinetics of Antituberculosis Drugs and Tuberculosis Treatment Outcomes in HIV-tuberculosis Co-infected Ugandan Adults[NCT01782950]Phase 4400 participants (Anticipated)Interventional2013-02-28Recruiting
Explorative PK Study Comparing 600 mg Rifampicin i.v. With 750 mg and 900 mg Rifampicin Oral in Tuberculous Meningitis Patients[NCT01802502]Phase 230 participants (Actual)Interventional2013-06-30Completed
A Phase 1, Open-Label Study to Evaluate the Effect of Rifampin or Itraconazole on the Pharmacokinetics of GDC-0032 in Healthy Subjects[NCT01814709]Phase 132 participants (Actual)Interventional2013-04-30Completed
A Phase 1, Open-Label, 2-Arm, Fixed-Sequence Study to Evaluate the Potential Effects of Multiple Doses of Rifampin (CYP3A4 Inducer) and Clarithromycin (CYP3A4 Inhibitor) on the Single Dose Pharmacokinetics of Deflazacort in Healthy Subjects[NCT02286635]Phase 158 participants (Actual)Interventional2014-11-30Completed
A Phase I, Single-center, Open-label, Fixed-sequence Clinical Study to Evaluate the Effects of Multiple Administrations of Rifampin or Itraconazole on the Pharmacokinetic Characteristics of a Single Administration of Orelabrutinib Tablets in Healthy Subje[NCT05316857]Phase 136 participants (Actual)Interventional2021-12-16Completed
A Randomised, Pragmatic, Open-Label Trial To Evaluate The Effect Of Three Months Of High Dose Rifapentine Plus Isoniazid Administered As A Single Round Or Given Annually In HIV-Positive Individuals[NCT02980016]Phase 34,027 participants (Actual)Interventional2016-11-30Completed
A Randomized Controlled Non-Inferiority Study for Shortening Tuberculosis Treatment With Sitafloxacin-Containing Regimens[NCT05454345]Phase 3620 participants (Anticipated)Interventional2022-10-01Not yet recruiting
A Phase 3 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of the Combination of Moxifloxacin Plus PA-824 Plus Pyrazinamide After 4 and 6 Months of Treatment in Adult Subjects With Drug-Sensitive Smear-Positive Pulmo[NCT02342886]Phase 3284 participants (Actual)Interventional2015-02-28Completed
A Single-center, Randomized, Double-blind, Two-period Cross-over Study to Investigate the Effect of a Single Intravenous Dose of Rifampicin on the Pharmacokinetics of ACT-246475 in Healthy Subjects[NCT03814200]Phase 114 participants (Actual)Interventional2019-01-03Completed
Using Biomarkers to Predict TB Treatment Duration[NCT02821832]Phase 2946 participants (Actual)Interventional2017-06-21Active, not recruiting
A Phase I, Open-label, Randomised, Crossover Study in 3 Parallel Groups to Evaluate the Effect of Rifampicin, Ketoconazole, and Omeprazole on the Pharmacokinetics of Sativex in Healthy Volunteers[NCT01323465]Phase 136 participants (Actual)Interventional2008-02-29Completed
An Open-lable, Two- Period, Single-sequence, Self-controlled Study to Evaluate the Effect of Oral Rifampicin or Itraconazole on the Pharmacokinetics of ASK120067 Tablets[NCT05631678]Phase 148 participants (Actual)Interventional2022-06-06Completed
A Phase I, Open-Label, Multicenter, Three-Period, One-Sequence Study to Investigate the Effect of Rifampin on the Pharmacokinetics of a Single Oral Dose of 960 mg of Vemurafenib[NCT01765543]Phase 127 participants (Actual)Interventional2013-07-31Completed
A Phase 1, 2-part, Open-label, Fixed-sequence Study Evaluating the Effect of Rifampin (Part 1) and Rabeprazole (Part 2) on the Pharmacokinetics of a Single Dose of Camlipixant (BLU-5937) 50 mg Tablet in Healthy Participants Under Fasting Conditions[NCT05899829]Phase 132 participants (Anticipated)Interventional2023-06-30Not yet recruiting
An Open-Label, Three-Period, Fixed Sequence Study to Investigate the Effect of Multiple Oral Doses of Rifampin, a Potent Cytochrome P450 3A Inducer, on the Single Dose Pharmacokinetics of RO5424802 in Healthy Subjects[NCT01940510]Phase 124 participants (Actual)Interventional2013-10-31Completed
Effect of Rifampicin on the Pharmacokinetics of a Single Oral Dose of BI 894416 in Healthy Male Subjects (an Open-label, One-way Crossover Study)[NCT04060719]Phase 116 participants (Actual)Interventional2019-09-04Completed
Randomized Controlled Trial of Chlorhexidine Gluconate, Intranasal Mupirocin, Rifampin and Doxycycline Versus Chlorhexidine Gluconate and Intranasal Mupirocin Alone for the Eradication of Methicillin-resistant Staphylococcus Aureus Among an Ambulatory Pat[NCT01438515]100 participants (Actual)Interventional2008-08-31Completed
Safety and Pharmacokinetics of Single and Multiple Dose Rifampin in Infants[NCT01441206]Phase 12 participants (Actual)Interventional2011-09-30Terminated(stopped due to Study to be redesigned.)
An Open-Label, Single-Dose Study to Assess the Effect of Food Intake and Drug-Drug Interactions of E7090 When Co-administered With Rabeprazole (Gastric Acid-Reducing Agent), or Rifampin (Strong CYP3A Inducer) in Healthy Subjects[NCT04565574]Phase 142 participants (Actual)Interventional2020-10-16Completed
Pharmacokinetics of Antistaphylococcal Antibiotics in Infants[NCT01728363]Phase 163 participants (Actual)Interventional2013-01-31Completed
Randomized Clinical Trial to Assess the Efficacy of Short Course Intermittent Regimens for the Treatment of HIV-Associated Tuberculosis[NCT00376012]Phase 3300 participants (Actual)Interventional2001-02-28Active, not recruiting
A Prospective Study of Multidrug Resistance and a Pilot Study of the Safety of and Clinical and Microbiologic Response to Levofloxacin in Combination With Other Antimycobacterial Drugs for Treatment of Multidrug-Resistant Pulmonary Tuberculosis (MDRTB) in[NCT00000796]525 participants InterventionalCompleted
An Open Label, 2-period, Sequential Study to Determine the Impact of Multiple Doses of Rifampin on Single-dose Pharmacokinetics of HCV-796[NCT00384280]Phase 124 participants Interventional2006-09-30Completed
A Phase 1, Single-Center, Open-Label, Fixed-Sequence, 2-Period, 3-Part Study to Evaluate the One-Way Interaction of Calcium Carbonate, Omeprazole, or Rifampin on ACP-196 in Healthy Adult Subjects[NCT04914936]Phase 172 participants (Actual)Interventional2014-09-21Completed
An Open-Label Phase I Study to Assess the Effect of Rifampicin on the Pharmacokinetics of Eribulin Mesylate (E7389) in Subjects With Advanced Solid Tumors[NCT03002493]Phase 114 participants (Actual)Interventional2009-12-31Completed
An Open-Label, Single-Sequence Study to Evaluate the Effect of Rifampin on the Single-dose Pharmacokinetics of BMS-986177 in Healthy Subjects[NCT02959060]Phase 116 participants (Actual)Interventional2016-11-30Completed
Non-randomized, Non-blinded, Non-placebo-controlled Study to Investigate the Influence of Repeated Daily Administration of 600 mg Rifampicin Given Once Daily Over 11 Days on the Pharmacokinetics, Safety, and Tolerability of a Single Oral Dose of 4 mg Vila[NCT02975440]Phase 112 participants (Actual)Interventional2016-11-10Completed
Study to Evaluate the Safety of the Use of doTBal (Rifampicin, Isoniazid, Pyrazinamide and Ethambutol) in Patients With Tuberculosis: Conduction of an Intensive Pharmacovigilance Program[NCT04916899]47 participants (Actual)Observational2014-11-30Completed
Evaluating Pharmacokinetics and Whole Blood Bactericidal Activity Against Mycobacterium Tuberculosis of Single Doses of Faropenem Plus Amoxicillin/Clavulanic Acid in Healthy Volunteers[NCT02393586]Phase 143 participants (Actual)Interventional2015-02-28Completed
A Phase 1, Open-Label, Non-Randomized, Fixed-Sequence Composite Study to Evaluate the Effects of Probenecid, Rifampin, and Verapamil on the Pharmacokinetics and Pharmacodynamics of Bexagliflozin in Healthy Subjects[NCT03296800]Phase 148 participants (Actual)Interventional2017-09-27Completed
A Prospective Multicenter Phase II-study: Pharmacokinetics and Safety of High-Dose Rifampicin and Pyrazinamide in a Shorter Tuberculosis Treatment Compared With Standardized Treatment in Patients With Mild to Moderate Pulmonary TB[NCT04694586]Phase 240 participants (Anticipated)Interventional2022-11-30Recruiting
A Phase I, Three-Arm Safety, Tolerability, and Pharmacokinetic Interaction Study of PA-824, an Investigational Nitroimidazole for the Treatment of Tuberculosis, Together With Efavirenz, Ritonavir-Boosted Lopinavir, or Rifampin[NCT01571414]Phase 152 participants (Actual)Interventional2012-05-31Completed
Randomised, Open-Label Clinical Trial on The Efficacy of Colistin Plus Rifampicin Treatment Versus Colistin Alone for Severe Infections Due to Multidrug-Resistant Acinetobacter Baumannii[NCT01577862]Phase 3210 participants (Actual)Interventional2008-11-30Completed
A Randomized Trial of DOTS Versus Enhanced DOTS for Community Control of Tuberculosis[NCT00317330]Phase 36,400 participants Interventional2004-12-31Completed
An Open-Label, Single-Sequence Study to Evaluate the Effect of Rifampin on the Single-dose Pharmacokinetics of BMS-986141 in Healthy Subjects[NCT02957448]Phase 116 participants (Actual)Interventional2016-11-30Completed
Prophylaxis Against Tuberculosis (TB) in Patients With Human Immunodeficiency Virus (HIV) Infection and Confirmed Latent Tuberculous Infection[NCT00000638]2,000 participants InterventionalCompleted
A Phase 1, Open-label, 2-Part, 2-Period Fixed-Sequence Crossover Study to Assess the Effect of Itraconazole, and the Effect of Rifampin on the Pharmacokinetics of HMPL-523 in Healthy Volunteers[NCT05720767]Phase 128 participants (Actual)Interventional2022-11-04Completed
Pharmacokinetic Evaluation of Nontuberculous Mycobacterial Antibiotics in Cystic Fibrosis Versus Controls[NCT02372383]31 participants (Actual)Interventional2014-10-31Completed
An Open-label, Fixed Sequence Study to Evaluate the Effects of Multi-dose of Itraconazole or Rifampin on the Pharmacokinetic Profiles of Single Dose of SPH3127 in Healthy Volunteers[NCT05359055]Phase 1/Phase 240 participants (Actual)Interventional2021-12-13Completed
A Non-randomised, Open-label, Sequential, Multicentre, Two-part, Phase I Study to Assess the Effect of Rifampicin, a CYP Inducer, on the Pharmacokinetics of Olaparib Following Oral Dosing of a Tablet Formulation in Patients With Advanced Solid Tumours[NCT01929603]Phase 132 participants (Actual)Interventional2013-12-31Completed
A Multiple Arm, Multiple Stage (MAMS), Phase 2B/C, Open Label, Randomized, Controlled Platform Trial to Evaluate Experimental Arms Including an Increased Dose of Rifampicin, an Optimized Dose of Pyrazinamide, Moxifloxacin and Sutezolid, in Adult Subjects [NCT05807399]Phase 2360 participants (Anticipated)Interventional2023-04-14Recruiting
Treatment of Pulmonary Disease Caused by MAIS, M.Xenopi or M.Malmoense: A Comparison of Two Triple Drug Regimens and an Assessment of the Value of Immunotherapy With M.Vaccae[NCT00367913]Phase 4400 participants Interventional1995-03-31Completed
Safety of Rifampicin at High Dose for the Treatment of Adult Subjects With Complex Drug Susceptible Pulmonary and Extrapulmonary Tuberculosis[NCT04768231]Phase 2130 participants (Anticipated)Interventional2021-04-01Not yet recruiting
Efficacy Of Doxycycline & Versus Rifampin In Treatment Of Rhinoscleroma[NCT05431673]Phase 145 participants (Anticipated)Interventional2022-08-21Not yet recruiting
A Phase 1, Open-Label, 4-Part Study to Evaluate the Effect of Food, Cytochrome P 450 Inhibition and Induction on the Pharmacokinetics of CC 122 in Healthy Adult Subjects[NCT03340662]Phase 181 participants (Actual)Interventional2017-11-09Completed
Two-month Regimens Using Novel Combinations to Augment Treatment Effectiveness for Drug-sensitive Tuberculosis[NCT03474198]Phase 2/Phase 3675 participants (Actual)Interventional2018-03-21Completed
Early MRSA Therapy in CF - Culture Based vs. Observant Therapy (Treat or Observe) (Star-TOO - STaph Aureus Resistance - Treat or Observe)[NCT01349192]Phase 247 participants (Actual)Interventional2011-04-30Terminated(stopped due to Interim review showed a statistically significant treatment effect and the DMC recommended that the study be stopped with ongoing follow-up of enrolled subjects)
A Randomised, Open-label, Three-way Crossover Trial to Investigate the Effect of Rifampicin and Probenecid on Empagliflozin Pharmacokinetics in Healthy Male and Female Subjects[NCT01634100]Phase 118 participants (Actual)Interventional2012-06-30Completed
[NCT00004689]Phase 250 participants Interventional1991-01-31Completed
A Phase 1, Open-Label, Randomized, Two-Way Crossover Study to Evaluate the Effect of Single-Dose Intravenous Rifampin as a Prototypic Inhibitor of OATP1B1 and OATP1B3 on the Single-Dose Pharmacokinetics of Oral TAK-906 in Healthy Adult Subjects[NCT04121078]Phase 112 participants (Actual)Interventional2019-10-15Completed
The Effects of Single Dose Rifampin on Pharmacokinetics of Fluvastatin in Uninduced and Hepatically Induced Healthy Volunteers[NCT04029584]Phase 410 participants (Actual)Interventional2019-04-25Completed
A Phase 1, Open-label, Three-period, Fixed-sequence Study to Evaluate the Effects of Rifampin on the Pharmacokinetics of Apremilast (CC-10004) in Healthy Subjects[NCT01561963]Phase 121 participants (Actual)Interventional2012-02-01Completed
A Phase 1, Open-label, Parallel-group, Fixed-sequence Study to Investigate the Effect of the CYP3A Inducer Rifampin and the CYP3A Inhibitor Itraconazole on the Pharmacokinetics of BGB-3111 in Healthy Subjects[NCT03301181]Phase 140 participants (Actual)Interventional2017-09-18Completed
A Single-center, Open-label, Drug-drug Interaction Study of XZP-3287 Tablets in Healthy Subjects[NCT04951713]Phase 160 participants (Anticipated)Interventional2021-07-31Recruiting
Persistent MRSA Eradication Protocol (PMEP)[NCT01594827]Phase 229 participants (Actual)Interventional2012-10-31Completed
A Phase I, Open Label, Drug-drug Interaction Study to Evaluate the Effects of Itraconazole and Rifampin on the Pharmacokinetics of ASC40 in Healthy Subjects[NCT04843449]Phase 124 participants (Actual)Interventional2021-04-04Completed
Single Center, Open-Label, Single-Sequence, Within-Subject Study In Two Cohorts Of Healthy Male Subjects Comparing Single-Dose Pharmacokinetics Of Fedovapagon Alone And In Combination With A CYP3A4 Inhibitor, Itraconazole, Or A CYP3A4 Inducer, Rifampicin[NCT02440841]Phase 129 participants (Actual)Interventional2015-05-31Completed
Evaluation and Validation of Metabolic Markers for the Assessment of CYP3A Activity and Prediction of Drug-drug Interaction in Korean Healthy Subjects[NCT02328443]Phase 124 participants (Actual)Interventional2014-01-31Completed
A Phase 1, Open Label, Two-part, Fixed-sequence Drug Interaction Study to Investigate the Effect of Strong CYP3A4 Inhibitor (Itraconazole) and CYP3A4 Inducer (Rifampin) on the Pharmacokinetics of LOXO 305 in Healthy Adult Subjects[NCT05134337]Phase 124 participants (Actual)Interventional2020-02-12Completed
Multi-centric Prospective Cohort Study of TB Recurrence Free Cure Among Microbiologically Confirmed New Pulmonary Tuberculosis Patients Treated Under NTEP With the 4-month Moxifloxacin Containing Daily Regimen[NCT05047055]550 participants (Anticipated)Observational2021-10-01Not yet recruiting
A Phase 1 Study to Estimate MMAE Metabolites in Human Plasma and Urine in Patients With Relapsed or Refractory Classical Hodgkin Lymphoma or Relapsed or Refractory Systemic Anaplastic Large Cell Lymphoma Receiving Brentuximab Vedotin[NCT01950364]Phase 120 participants (Actual)Interventional2013-11-30Completed
PXR-aktivaation Vaikutus Maksan Rasvoittumiseen[NCT02329405]Phase 416 participants (Actual)Interventional2014-12-31Completed
Pharmacogenetics of Warfarin Induction and Inhibition[NCT01447511]39 participants (Actual)Interventional2009-05-31Completed
PHASE 1 SAFETY, PHARMACOKINETIC AND PHARMACODYNAMIC STUDY OF PF-02341066, A MET/HGFR SELECTIVE TYROSINE KINASE INHIBITOR, ADMINISTERED ORALLY TO PATIENTS WITH ADVANCED CANCER[NCT00585195]Phase 1596 participants (Actual)Interventional2006-04-19Completed
Relative Bioavailability of a Single Oral Dose of Nintedanib Given Alone and in Combination With Multiple Oral Doses of Rifampicin in Healthy Male Volunteers (an Open-label, Two-period, Fixed Sequence Phase I Trial)[NCT01770392]Phase 126 participants (Actual)Interventional2013-01-31Completed
Influence of CYP3A Modulation on Buprenorphine Disposition and Clinical Effects[NCT01576575]21 participants (Actual)Interventional2010-06-30Completed
Post ExpOsure Prophylaxis for LEprosy in the Comoros and Madagascar[NCT03662022]Phase 3144,000 participants (Actual)Interventional2019-01-02Completed
A Drug-drug Interaction Study Evaluating the Pharmacokinetic Effects of Itraconazole or Rifampin or Esomeprazole on XZP-3621 Tablets in Healthy Subjects[NCT05586568]Phase 172 participants (Anticipated)Interventional2022-11-15Not yet recruiting
A Phase 1, Parallel-group, 3-part, 2-period, Fixed-sequence, Crossover, Open-label, Nonrandomized, Drug-drug Interaction Study to Assess the Pharmacokinetics of CC-92480 (BMS-986348) After Coadministration With Rifampin and Itraconazole, and Pharmacokinet[NCT05389722]Phase 124 participants (Actual)Interventional2022-06-09Completed
A Phase I Single Site Open Label Clinical Trial for the Development of a Human BCG Challenge Model to Assess TB Drugs and Vaccines.[NCT05592223]Phase 120 participants (Actual)Interventional2022-12-06Active, not recruiting
Effect of Modulating CYP3A4 Activity on Mineral Homeostasis[NCT02019875]Early Phase 192 participants (Actual)Interventional2014-06-30Completed
Pragmatic Trial on the Safety and Tolerability of an Optimized Dose of Rifampicin in Tuberculosis Patients[NCT06057519]Phase 3164 participants (Anticipated)Interventional2023-11-01Not yet recruiting
Essentiality of Isoniazid in Tuberculosis Therapy[NCT01589497]Phase 269 participants (Actual)Interventional2015-06-30Completed
Comparison of 3-month Once-weekly Isoniazid Plus Rifapentine, 4-month Daily Rifampicin, and 3-month Daily Isoniazid Plus Rifampicin for the Treatment Latent Tuberculosis in Patients With End-stage Kidney Disease: A Randomised Clinical Trial[NCT05021731]Phase 4225 participants (Anticipated)Interventional2022-04-01Not yet recruiting
A Single-center, Non-randomized, Open-lable, Self-controlled Clinical Trial to Evaluate JAB-21822 Drug-drug Interactions in Healthy Subjects[NCT06162169]Phase 166 participants (Anticipated)Interventional2023-11-25Recruiting
A Phase 1, Open-label, Dose Finding Study to Assess the Safety, Tolerability, Pharmacokinetics and Preliminary Efficacy of CC-90011 in Subjects With Relapsed and/or Refractory Solid Tumors and Non-Hodgkin's Lymphomas[NCT02875223]Phase 191 participants (Anticipated)Interventional2016-08-31Active, not recruiting
Effect of Rifampin on the Pharmacokinetics of Evacetrapib in Healthy Subjects[NCT01908582]Phase 126 participants (Actual)Interventional2013-07-31Completed
Impact of Rifampicin in Treatment Outcome of Cutibacterium Acnes Prosthetic Joint Infections[NCT05902221]Phase 3235 participants (Anticipated)Interventional2023-07-01Not yet recruiting
A Phase 1, Two-Part, Open-label Study in Healthy Adult Volunteers to Assess a Single Dose of Vadadustat as a Victim in Drug-Drug Interactions With Cyclosporine, Probenecid and Rifampin[NCT03801746]Phase 140 participants (Actual)Interventional2018-07-20Completed
"A Randomized Trial Comparing Treatment Completion of Daily Rifapentine & Isoniazid for One Month (1HP) To Weekly Rifapentine & Isoniazid For 3 Months (3HP) In Persons Living With HIV and in HIV-negative Household Contacts of Recently Diagnosed Tuberculos[NCT05118490]Phase 41,000 participants (Anticipated)Interventional2023-04-01Not yet recruiting
Bedaquiline Enhanced Post ExpOsure Prophylaxis for Leprosy: Phase 3 Study[NCT05597280]Phase 3124,000 participants (Anticipated)Interventional2023-03-22Recruiting
Long-term StaphyloCoccus Aureus decolonizAtion in Patients on Home parenteRal nutRition: a randomIzed multicEnter tRial.[NCT03173053]63 participants (Actual)Interventional2018-02-08Terminated(stopped due to Results interim-analysis)
A Phase 1, Open-Label, Fixed-Sequence, Crossover Drug-Drug Interaction Study in Healthy Subjects to Determine the Effects of a Strong Inducer of Cytochrome P450 3A on Exposure to Mifepristone and Its Metabolites[NCT03258372]Phase 148 participants (Actual)Interventional2017-08-16Completed
Rifampin to Reduce Elevated Levels of Blood and Urine Calcium in Patients With Idiopathic Infantile Hypercalcemia[NCT03384121]Phase 15 participants (Anticipated)Interventional2018-02-22Recruiting
A Phase 1 Study of Oral IXAZOMIB (MLN9708) to Assess Relative Bioavailability, Food Effect, Drug-Drug Interaction With Ketoconazole, Clarithromycin or Rifampin; and Safety and Tolerability in Patients With Advanced Nonhematologic Malignancies or Lymphoma[NCT01454076]Phase 1112 participants (Actual)Interventional2011-11-10Completed
Randomized Trial of High-Dose Rifampin in Patients With New, Smear-Positive TB[NCT01408914]Phase 2180 participants (Actual)Interventional2013-09-30Completed
A Phase I, Open-label, Non-randomised Study to Assess the Effect of Itraconazole (a CYP3A4 Inhibitor), Rifampicin (a CYP3A4 Inducer), and Omeprazole (a Proton Pump Inhibitor) on the Pharmacokinetics of a Single Oral Dose of Adavosertib in Patients With Ad[NCT04959266]Phase 15 participants (Actual)Interventional2021-06-28Terminated(stopped due to The study terminated because the clinical development programme for Adavosertib has been discontinued)
The Efficacy and Safety Evaluation of Standardized Treatment Included Rifampicin or Rifabutin in HIV/AIDs Patients Combined With Pulmonary Tuberculosis. A Prospective Study.[NCT03478033]230 participants (Anticipated)Interventional2018-04-15Recruiting
A Randomized, Phase 2b Study of a Double-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifampin-Based Tuberculosis Treatment Versus a Standard-Dose Lopinavir/Ritonavir-Based Antiretroviral Regimen With Rifabutin-Based Tuberculosis Treatment W[NCT01601626]Phase 271 participants (Actual)Interventional2013-07-13Terminated(stopped due to The study was stopped early due to feasibility concerns.)
A 2-Part, Non-randomized, Open-label Study to Evaluate the Effect of Itraconazole, Rifampicin, Rabeprazole, and Omeprazole on the Pharmacokinetics of Belumosudil (KD025)[NCT03530995]Phase 173 participants (Actual)Interventional2018-04-09Completed
Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis[NCT05398679]Phase 4360 participants (Anticipated)Interventional2022-06-01Not yet recruiting
Novel Triple-dose Tuberculosis Retreatment Regimen: How to Overcome Resistance Without Creating More in Niger[NCT04260477]Phase 3370 participants (Anticipated)Interventional2021-03-01Recruiting
Rifapentine-containing Treatment Shortening Regimens for Pulmonary Tuberculosis: A Randomized, Open-label, Controlled Phase 3 Clinical Trial. TBTC Study 31, ACTG Study A5349[NCT02410772]Phase 32,516 participants (Actual)Interventional2016-01-25Completed
Prospective Cohort Study on Patients With Tedizolid Prolonged Therapy for Orthopedic Device Infections[NCT03378427]35 participants (Actual)Interventional2018-08-28Completed
Open-label, Randomized, Fixed Sequence Cross-over Study With Five Parallel Treatment Arms and Three Treatment Periods to Quantify the Drug-drug Interactions of Two Rifampicin Dose Strengths on Four Progestins and a Fixed Progestin-ethinylestradiol Combina[NCT03353857]Phase 168 participants (Actual)Interventional2017-11-29Completed
A Phase II, Randomized, Open-Label Trial of a Six-Month Regimen of High-Dose Rifampicin, High-Dose Isoniazid, Linezolid, and Pyrazinamide Versus a Standard Nine-Month Regimen for the Treatment of Adults and Adolescents With Tuberculous Meningitis: Improve[NCT05383742]Phase 2330 participants (Anticipated)Interventional2024-01-02Not yet recruiting
An Open-Label, Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of a 4-month Treatment of Bedaquiline Plus Pretomanid Plus Moxifloxacin Plus Pyrazinamide (BPaMZ) Compared to a 6-month Treatment of HRZE/HR (Control) in Adult Par[NCT03338621]Phase 2/Phase 3455 participants (Actual)Interventional2018-07-30Completed
The Effect of Potent Inhibitors of Drug Transporters (Verapamil, Rifampin, Cimetidine, Probenecid) on Pharmacokinetics of a Transporter Probe Drug Cocktail Consisting of Digoxin, Furosemide, Metformin and Rosuvastatin (an Open-label, Randomised, Crossover[NCT03307252]Phase 145 participants (Actual)Interventional2017-10-25Completed
The Effects of Rifampin on the Pharmacokinetics of Warfarin in Healthy Volunteers.[NCT00777855]10 participants (Actual)Interventional2008-11-30Completed
A Phase I, Open-Label, Non-Randomised, Multicentre Study to Assess the Effect of Rifampicin (a CYP3A4 Inducer) on the Pharmacokinetics of AZD9291 in Patients With EGFRm Positive NSCLC Whose Disease Has Progressed on an EGFR TKI[NCT02197247]Phase 141 participants (Actual)Interventional2014-12-04Completed
Study of the Effect of Esomeprazole or Rifampin on the Pharmacokinetics of Alisertib and Evaluation of the Effect of Alisertib on the QTc Interval in Patients With Advanced Solid Tumors or Lymphomas[NCT01844583]Phase 155 participants (Actual)Interventional2013-06-25Completed
Impact of Two Genetic Variants of OATP 1B3 or MRP 2 or Rifampin Mediated Transporter Inhibition on Systemic Disposition and Biological Efficacy of CCK-8 in 36 Healthy Male Individuals[NCT02507167]Phase 119 participants (Actual)Interventional2012-11-30Completed
The Effect of High Dose Rifampicin on the Activity of Cytochrome P450 Enzymes and P-glycoprotein in Patients With Pulmonary Tuberculosis: a Cocktail Phenotyping Study[NCT04525235]Phase 125 participants (Actual)Interventional2021-01-07Completed
A Phase 1, Open-label, Drug-Drug Interaction Study to Assess the Steady State Pharmacokinetics of N91115 Alone and in the Presence of Multiple Dose Administration of Rifampin in Healthy Adult Subjects (SNO-5)[NCT02500667]Phase 115 participants (Actual)Interventional2015-06-30Completed
A Single Center, Single Arm, Open and Fixed Sequence Study to Investigate the Pharmacokinetic Effects of Rifampicin on Famitinib in Healthy Male Subjects[NCT04494659]Phase 121 participants (Actual)Interventional2020-07-20Completed
A Phase IIc, Open-Label, Randomized Controlled Trial of Ultra-Short Course Bedaquiline, Clofazimine, Pyrazinamide and Delamanid Versus Standard Therapy for Drug-Susceptible Tuberculosis (PRESCIENT)[NCT05556746]Phase 2156 participants (Anticipated)Interventional2023-10-31Not yet recruiting
MRSA Decolonization in Complicated Carriage - Cluster Randomized Trial[NCT05268120]211 participants (Anticipated)Interventional2022-07-25Recruiting
Treatment Shortening of Drug-Sensitive Pulmonary Tuberculosis Using High Dose Rifampicin to 3 Months After Culture Conversion (Hi-DoRi-3): A Phase 3, Multicenter, Randomized, Open-label, Clinical Trial[NCT04485156]Phase 3926 participants (Anticipated)Interventional2020-09-30Not yet recruiting
A Phase 1, Open-Label, Fixed-Sequence, Drug-Drug Interaction Study of APX001 to Evaluate the Effects of CYP3A4 Inhibition and Pan-CYP Induction in Two Parallel Groups of Healthy Male and Female Subjects[NCT04166669]Phase 136 participants (Actual)Interventional2019-11-12Completed
Effects of CYP3A Induction by Rifampin on the Pharmacokinetics of LY2835219 and Its Metabolites in Healthy Subjects[NCT02256267]Phase 124 participants (Actual)Interventional2014-10-31Completed
A Phase 2 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of Combinations of Bedaquiline, Moxifloxacin, PA-824 and Pyrazinamide During 8 Weeks of Treatment in Adult Subjects With Newly Diagnosed Drug-Sensitive or Mu[NCT02193776]Phase 2240 participants (Actual)Interventional2014-10-23Completed
A Phase 1 Open-Label, Fixed-Sequence Drug-Drug Interaction Study to Evaluate the Effects of Steady-state Itraconazole and Rifampin on the Single-dose Pharmacokinetics of Lazertinib Tablets in Healthy Adult Participants[NCT04410094]Phase 132 participants (Actual)Interventional2020-09-14Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00128206 (2) [back to overview]Number of Participants With Laboratory Test or Clinical Judgment Resulting in the Need to Stop Study Medication
NCT00128206 (2) [back to overview]Completion of Therapy
NCT00130247 (6) [back to overview]Acquired Drug Resistance in Patients Who Relapsed
NCT00130247 (6) [back to overview]Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-TB Treatment - Per-protocol
NCT00130247 (6) [back to overview]Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-tuberculosis (TB) Treatment - Intention-to-treat
NCT00130247 (6) [back to overview]Relapses at 1 and 2 Years
NCT00130247 (6) [back to overview]Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Intention to Treat
NCT00130247 (6) [back to overview]Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Per Protocol
NCT00207090 (18) [back to overview]Time Taken for Plasma Concentration to Reduce by 50 Percent or Apparent Terminal Plasma Elimination Half-life (T Half)
NCT00207090 (18) [back to overview]Time to Reach Maximum Observed Concentration (T Max)
NCT00207090 (18) [back to overview]Total Body Clearance (CLT)
NCT00207090 (18) [back to overview]Volume of Distribution at Steady-state (Vss)
NCT00207090 (18) [back to overview]Number of Participants Who Died and Who Experienced Other Serious AEs (SAEs), Grade 3-4 AEs, Drug-related AEs and AEs Leading to Study Drug Discontinuation
NCT00207090 (18) [back to overview]Number of Participants With Grade 3-4 Hematology Abnormalities
NCT00207090 (18) [back to overview]Number of Participants With Grade 3-4 Serum Chemistry Abnormalities in Alanine Aminotransferase, Aspartate Aminotransferase, Bilirubin, Albumin and Phosphorous
NCT00207090 (18) [back to overview]Number of Participants With Grade 3-4 Serum Chemistry Abnormalities in Calcium, Magnesium, Potassium, Sodium, Glucose and Uric Acid.
NCT00207090 (18) [back to overview]Number of Participants With Identified ECG Abnormalities
NCT00207090 (18) [back to overview]QT Interval Corrected for Heart Rate (QTcF)
NCT00207090 (18) [back to overview]Urine 6B-Hydroxycortisol to Cortisol Ratio on Day -1
NCT00207090 (18) [back to overview]Urine 6B-Hydroxycortisol to Cortisol Ratio on Day 22
NCT00207090 (18) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinite Time (AUC [INF])
NCT00207090 (18) [back to overview]Number of Participants With Abnormal Physical Examination Findings
NCT00207090 (18) [back to overview]Maximum Plasma Concentration (Cmax)
NCT00207090 (18) [back to overview]Mean Residence Time Adjusted for Infusion Time (MRT [INF])
NCT00207090 (18) [back to overview]Number of Participants With Clinically Meaningful Vital Signs Measures
NCT00207090 (18) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC [0-T])
NCT00351273 (8) [back to overview]Swollen 76 Joint Count (SJC)
NCT00351273 (8) [back to overview]Number of Patients With a Complete Response (Resolution of All Symptoms)
NCT00351273 (8) [back to overview]78 Tender Joint Count (TJC)
NCT00351273 (8) [back to overview]Erythrocyte Sedimentation Rate (ESR)
NCT00351273 (8) [back to overview]HAQ DI Score
NCT00351273 (8) [back to overview]hsCRP
NCT00351273 (8) [back to overview]PhGA Assessment
NCT00351273 (8) [back to overview]Investigate Whether a 6 Month Course of Combined Antibiotics Was Effective Treatment.
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Progression Free Survival (PFS)
NCT00585195 (53) [back to overview]Rifampin Cohort: Ctrough of Crizotinib Alone and When Taken With Rifampin
NCT00585195 (53) [back to overview]Rifampin Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib Alone and When Taken With Rifampin
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Time to Response (TTR)
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 15 Day 1
NCT00585195 (53) [back to overview]RP2D Cohort: Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Crizotinib When Taken With Food
NCT00585195 (53) [back to overview]RP2D Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken With Food
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at End of Treatment
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 9 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 6 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 4 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 30 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 27 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 24 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Number of Participants With Treatment Emergent Adverse Events (TEAES) and Serious Adverse Events (SAEs)
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 21 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 2 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 18 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 12 Day 1
NCT00585195 (53) [back to overview]Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 1 Day 15
NCT00585195 (53) [back to overview]Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib Alone and When Taken With Rifampin
NCT00585195 (53) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Midazolam When Taken Alone or Taken With Crizotinib
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Cycle 1 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Cycle 1 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Plasma Decay Half-Life (t1/2) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib on Cycle 1 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib on Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Time to Reach Maximum Observed Plasma Concentration (Tmax) of Crizotinib on Day -7
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Trough Concentration (Ctrough) of Crizotinib Cycle 1 Day 15
NCT00585195 (53) [back to overview]Dose-Escalation and Recommended Phase 2 Dose (RP2D) Cohort: Trough Concentration (Ctrough) of Crizotinib on Cycle 2 Day 1
NCT00585195 (53) [back to overview]Dose-Escalation Cohort: Maximum Tolerated Dose (MTD) of Crizotinib
NCT00585195 (53) [back to overview]Dose-Escalation Cohort: Number of Participants With Dose-limiting Toxicities (DLT)
NCT00585195 (53) [back to overview]Dose-Escalation Cohort: Recommended Phase 2 Dose (RP2D) of Crizotinib
NCT00585195 (53) [back to overview]Itraconazole Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib When Taken Alone and When Taken With Itraconazole
NCT00585195 (53) [back to overview]Itraconazole Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken Alone and When Taken With Itraconazole
NCT00585195 (53) [back to overview]Itraconazole Cohort: Trough Plasma Concentration (Ctrough) of Crizotinib When Taken Alone and When Taken With Itraconazole
NCT00585195 (53) [back to overview]Midazolam Interaction Cohort: Maximum Observed Plasma Concentration (Cmax) of Midazolam When Taken Alone or Taken With Crizotinib
NCT00585195 (53) [back to overview]Probability of Participant Survival at Month 12
NCT00585195 (53) [back to overview]Probability of Participant Survival at Month 6
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Duration of Response (DOR)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Overall Survival (OS)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Percentage of Participants With Disease Control at Week 16
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Percentage of Participants With Disease Control at Week 8
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Percentage of Participants With Objective Response (OR)
NCT00585195 (53) [back to overview]Recommended Phase 2 Dose (RP2D) Cohort: Probability of Being Event Free at Month 6
NCT00608907 (1) [back to overview]Area Under the Plasma Concentration-time Curve (AUC) 0-72 Hours
NCT00621309 (1) [back to overview]Midazolam Clearance (Pharmacokinetic Measure of Cytochrome P450 3A4 Activity)
NCT00728507 (1) [back to overview]To Compare, by Treatment Group, the Percentage of Patients With a Negative Sputum Culture at the End of Intensive Phase Therapy.
NCT00777855 (3) [back to overview]Maximum Plasma Concentration (Cmax) of S-warfarin and R-warfarin
NCT00777855 (3) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to Infinity of S-warfarin and R-warfarin
NCT00777855 (3) [back to overview]S- and R- Enantiomers of Warfarin (S-warfarin and R-warfarin) Area Under the Plasma Concentration-time Curve (AUC) From 0 to 12 Hours.
NCT00814671 (5) [back to overview]Time to Stable Culture Conversion on Solid Medium
NCT00814671 (5) [back to overview]Pharmacokinetics of Rifapentine
NCT00814671 (5) [back to overview]Percentage of Participants With Negative Lowenstein Jensen Cultures at Week 8
NCT00814671 (5) [back to overview]Tolerability
NCT00814671 (5) [back to overview]Time to Stable Culture Conversion on Liquid MGIT Media
NCT00864383 (9) [back to overview]Combined Failure of Bacteriological Cure and Relapse Within One Year of Completion of Therapy as Defined by Culture Using Solid Media (Lowenstein-Jensen - LJ).
NCT00864383 (9) [back to overview]Combined Failure of Bacteriological Cure and Relapse as Defined by Culture Using Liquid Media (Mycobacteria Growth Indicator Tube-MGIT).
NCT00864383 (9) [back to overview]Sensitivity Analyses Assuming All Losses to Follow-up and Non-tuberculous Deaths Have a Favourable Outcome Using Solid (L-J) Media.
NCT00864383 (9) [back to overview]Time to First Culture Negative Sputum Sample (MGIT Liquid Media)
NCT00864383 (9) [back to overview]Time to First Culture Negative Sputum Sample (LJ Solid Media)
NCT00864383 (9) [back to overview]Sensitivity Analysis Assuming All Losses to Follow-up and Non-tuberculous Deaths Have an Unfavorable Outcome Using Solid (L-J) Media.
NCT00864383 (9) [back to overview]Number of Patients With Grade 3 or 4 Adverse Events (Using a Modified Division of Acquired Immunodeficiency Syndrome National Institute of Allergy and Infectious Diseases [DAIDS] Scale of Adverse Event Reporting)
NCT00864383 (9) [back to overview]Number of Patients Who Are Culture Negative (Solid LJ Culture)
NCT00864383 (9) [back to overview]Number of Patients Who Are Culture Negative (Liquid MGIT Culture)
NCT01074554 (3) [back to overview]Change in Lesion Size at the Completion of Antibiotic Therapy, Measured on a Continuous Scale; Change Will be Determined by Change in Diameter of the Lesions
NCT01074554 (3) [back to overview]Change in Modified Sarcoidosis Activity and Severity Index (SASI) at Completion of Therapy.
NCT01074554 (3) [back to overview]Granuloma Burden
NCT01147055 (14) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for Crizotinib Metabolite (PF-06260182)
NCT01147055 (14) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] for Crizotinib Metabolite (PF-06260182)
NCT01147055 (14) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)
NCT01147055 (14) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]
NCT01147055 (14) [back to overview]Apparent Volume of Distribution (Vz/F)
NCT01147055 (14) [back to overview]Apparent Oral Clearance (CL/F)
NCT01147055 (14) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax)
NCT01147055 (14) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) for Crizotinib Metabolite (PF-06260182)
NCT01147055 (14) [back to overview]Plasma Decay Half-Life (t1/2)
NCT01147055 (14) [back to overview]Metabolite to Parent Ratio Area Under the Curve From Time Zero to Last Quantifiable Concentration (MRAUClast)
NCT01147055 (14) [back to overview]Metabolite to Parent Ratio Maximum Observed Plasma Concentration (MRCmax)
NCT01147055 (14) [back to overview]Maximum Observed Plasma Concentration (Cmax) for Crizotinib Metabolite (PF-06260182)
NCT01147055 (14) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT01147055 (14) [back to overview]Metabolite to Parent Ratio Area Under the Curve From Time Zero to Extrapolated Infinite Time [MRAUC (0 - ∞)]
NCT01162486 (3) [back to overview]Pharmacokinetics (AUC of RPT Over 24 Hours Post-dose)
NCT01162486 (3) [back to overview]Midazolam, AUC Over 12 Hours Post-dose
NCT01162486 (3) [back to overview]Number of Participants With Grade 2 or Higher Adverse Events Over the Course of the 26 Day Trial
NCT01169038 (1) [back to overview]Change in Absolute FVC From Baseline to Post Completion of 8 Weeks of Antibiotic Therapy.
NCT01287221 (7) [back to overview]Change From Baseline to 12 Months in UMSARS Part II
NCT01287221 (7) [back to overview]Change From Baseline to 12 Months in Total UMSARS (i.e., UMSARS Part I Minus Question 11 + UMSARS Part II)
NCT01287221 (7) [back to overview]Change From Baseline to 12 Months in UMSARS Part I Score (Minus Question 11)
NCT01287221 (7) [back to overview]Change in the COMPASS-Select-Change Scale From Baseline to 12 Months
NCT01287221 (7) [back to overview]Rate of Change From Baseline to 12 Months in the Total Unified Multiple System Atrophy Rating Scale (UMSARS) Part I Score (Minus Question 11)
NCT01287221 (7) [back to overview]Rate of Change From Baseline to 12 Months in Total UMSARS (i.e., UMSARS Part I Minus Question 11 + UMSARS Part II) Using Slope Estimate
NCT01287221 (7) [back to overview]Change From Baseline to 12 Months in the COMPASS-Select Scale
NCT01311505 (8) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT01311505 (8) [back to overview]Extrapolated Area Under the Curve (AUC Percent [%] Extrapolated)
NCT01311505 (8) [back to overview]Number of Participants With Abnormal Safety Laboratory Test Values
NCT01311505 (8) [back to overview]Number of Participants With Adverse Events (AEs)
NCT01311505 (8) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC [0-t])
NCT01311505 (8) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC [0-∞])
NCT01311505 (8) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax)
NCT01311505 (8) [back to overview]Plasma Decay Half-life (t1/2)
NCT01324323 (9) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax)
NCT01324323 (9) [back to overview]Summary of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT01324323 (9) [back to overview]Maximum Observed Plasma Concentration (Cmax)of Romidepsin
NCT01324323 (9) [back to overview]Apparent Total Volume of Distribution (Vz).
NCT01324323 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC0-24) for Romidepsin
NCT01324323 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin
NCT01324323 (9) [back to overview]Area Under the Plasma Concentration Time-curve From Time Zero Extrapolated to Infinity (AUC0-∞).
NCT01324323 (9) [back to overview]Estimate of the Terminal Elimination Half-life in Plasma (t1/2)
NCT01324323 (9) [back to overview]Clearance (CL): Apparent Total Plasma Clearance.
NCT01349192 (4) [back to overview]Antibiotic Use (Proportion of Subjects)
NCT01349192 (4) [back to overview]Antibiotic Use (Days of Use Per Subject)
NCT01349192 (4) [back to overview]MRSA Culture Status
NCT01349192 (4) [back to overview]Pulmonary Exacerbations
NCT01380080 (16) [back to overview]Cumulative Probability of First AIDS Progression by Week 96
NCT01380080 (16) [back to overview]Proportion of Participants Who Prematurely Discontinued Antiretroviral Therapy by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants Who Prematurely Discontinued Any Component of TB Treatment by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With at Least One New Grade 3 or 4 Adverse Event That is at Least a One-grade Increase From Baseline by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With at Least One New Grade 3 or 4 Targeted Laboratory Value That is at Least a One-grade Increase From Baseline by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With Reportable Hospitalization by Week 48
NCT01380080 (16) [back to overview]Proportion of Participants With TB Diagnosis by Week 96
NCT01380080 (16) [back to overview]Time to Initiation of TB Treatment by Week 96
NCT01380080 (16) [back to overview]CD4+ T-cell Count
NCT01380080 (16) [back to overview]CD4+ T-cell Count Change From Baseline
NCT01380080 (16) [back to overview]Proportion of Participants With HIV-1 RNA Level <400 Copies/mL
NCT01380080 (16) [back to overview]Proportion of Participants With Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48
NCT01380080 (16) [back to overview]Cumulative Probability of Death by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of Death or AIDS Progression by Week 24
NCT01380080 (16) [back to overview]Cumulative Probability of Death or AIDS Progression by Week 48
NCT01380080 (16) [back to overview]Cumulative Probability of Death or Unknown Vital Status by Week 24
NCT01396265 (10) [back to overview]Area Under Curve From 0 to Infinity Hours (AUC0-∞)
NCT01396265 (10) [back to overview]Area Under Curve From 0 to 24 h (AUC0-24)
NCT01396265 (10) [back to overview]Apparent Volume of Distribution During the Terminal Phase lambda_z Following an Extravascular Dose (V_z/F)
NCT01396265 (10) [back to overview]Area Under Curve From 0 to tz (AUC0-tz)
NCT01396265 (10) [back to overview]Apparent Clearance of Afatinib in the Plasma After Extravascular Administration (CL/F)
NCT01396265 (10) [back to overview]Maximum Concentration (Cmax)
NCT01396265 (10) [back to overview]Mean Residence Time of Afatinib in the Body After Oral Administration (MRTpo)
NCT01396265 (10) [back to overview]Percentage of the AUCtz-∞ Obtained by Extrapolation (%AUCtz-∞)
NCT01396265 (10) [back to overview]Terminal Half-life of Afatinib in Plasma (t1/2)
NCT01396265 (10) [back to overview]Time From Dosing to the Maximum Concentration of Afatinib in Plasma (Tmax)
NCT01408914 (3) [back to overview]Steady State Pharmacokinetic Exposure of RIF
NCT01408914 (3) [back to overview]Incidence of Rifampin-related Grade 2 or Higher Adverse Events
NCT01408914 (3) [back to overview]Sputum Culture Sterilization During the Initial 8 Weeks of Treatment
NCT01447511 (1) [back to overview]Warfarin Clearance.
NCT01454076 (7) [back to overview]Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Ixazomib
NCT01454076 (7) [back to overview]Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT01454076 (7) [back to overview]Cmax: Maximum Observed Plasma Concentration for Ixazomib
NCT01454076 (7) [back to overview]Number of Participants With Clinically Significant TEAEs Related to Laboratory Abnormalities
NCT01454076 (7) [back to overview]Percentage of Participants With Best Overall Response
NCT01454076 (7) [back to overview]Number of Participants With Clinically Significant Vital Sign Abnormalities
NCT01454076 (7) [back to overview]AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Ixazomib
NCT01561963 (7) [back to overview]Estimate of the Terminal Elimination Half-life (T1/2) of Apremilast in Plasma
NCT01561963 (7) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero to the Last Quantifiable Concentration (AUCt) of Apremilast
NCT01561963 (7) [back to overview]Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC∞) of Apremilast
NCT01561963 (7) [back to overview]Apparent Volume of Distribution (Vz/F) of Apremilast
NCT01561963 (7) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast
NCT01561963 (7) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Apremilast
NCT01561963 (7) [back to overview]Apparent Total Plasma Clearance (CL/F) of Apremilast
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter CL/F
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter CLast
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter Cmax
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Clearance (CL/F)
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Last Concentration (CLast)
NCT01589497 (32) [back to overview]Ethambutol PK Parameter Cmax
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter Cmax at Day 14
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Maximum Plasma Concentration (Cmax)
NCT01589497 (32) [back to overview]AUC0-24hour for Isoniazid (INH) at Day 1
NCT01589497 (32) [back to overview]AUC0-24hour for Isoniazid at Day 14
NCT01589497 (32) [back to overview]AUC0-24hour for Moxifloxacin (Mox) at Day 14
NCT01589497 (32) [back to overview]Correlation Between Time to Positivity (TTP) and log10 Transformed Colony-forming Unit (CFU) Counts Per mL
NCT01589497 (32) [back to overview]Daily Change in log10 Colony-forming Unit (CFU) Counts Per mL Sputum From Day 2 to Day 14
NCT01589497 (32) [back to overview]Daily Change in log10 Transformed Colony-forming Unit (CFU) Counts Per mL Sputum From Baseline (Study Treatment Initiation) to Day 2
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 14
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 2
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Day 2 to Day 14
NCT01589497 (32) [back to overview]Daily Decrease in log10 Transformed Colony-forming Unit (CFU) Counts Per ml Sputum From Baseline (Study Treatment Initiation) to Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CL/F at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CL/F at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CLast at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CLast at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter Cmax at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter Cmax at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter CL/F at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter CLast at Day 14
NCT01589497 (32) [back to overview]AUC0-24hour for Ethambutol (EMB)
NCT01589497 (32) [back to overview]AUC0-24hour for Pyrazinamide (PZA)
NCT01589497 (32) [back to overview]Ethambutol PK Parameter CL/F
NCT01589497 (32) [back to overview]Ethambutol PK Parameter CLast
NCT01589497 (32) [back to overview]Log10 Transformed Colony-forming Unit (CFU) Count Per mL From Sputum Samples at Baseline and Day 14
NCT01589497 (32) [back to overview]Pharmacokinetic Parameter (PK) Area Under the Concentration-time Curve (AUC0-24hour) for Rifampicin (RIF)
NCT01594827 (9) [back to overview]Change in Patient Reported Quality of Life (CFQ-R)(Respiratory)
NCT01594827 (9) [back to overview]Change if FEV1% Predicted From Screening
NCT01594827 (9) [back to overview]Time to First CF Exacerbation
NCT01594827 (9) [back to overview]Time to First Anti-MRSA Antibiotics (After Treatment Period)
NCT01594827 (9) [back to overview]Percentage of Patients MRSA Free by Induced Sputum Respiratory Tract Culture
NCT01594827 (9) [back to overview]Development of Antibiotic Resistance
NCT01594827 (9) [back to overview]Number of Patients MRSA Free by Induced Sputum Respiratory Tract Culture
NCT01594827 (9) [back to overview]Total Number of Pulmonary Exacerbations
NCT01594827 (9) [back to overview]Change in Forced Expiratory Volume (FEV1)% Predicted From Baseline to Day 58
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Sign or Symptom
NCT01601626 (26) [back to overview]Number of Participants Who Experienced MTB IRIS
NCT01601626 (26) [back to overview]Percent of Participants Who Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced a New AIDS-defining Illness or Died
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced HIV Virologic Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced Sputum Conversion at Week 8.
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance
NCT01601626 (26) [back to overview]Percent of Participants Who Experienced TB Treatment Failure
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.
NCT01601626 (26) [back to overview]Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48
NCT01601626 (26) [back to overview]RAL AUC in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]RBT AUC in Participants Enrolled in Arms A and C
NCT01601626 (26) [back to overview]LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C
NCT01601626 (26) [back to overview]RAL Cmax and Cmin in Participants Enrolled in Arm C
NCT01601626 (26) [back to overview]RBT Cmax and Cmin in Participants Enrolled in Arms A and C
NCT01601626 (26) [back to overview]Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 24
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 48
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 72
NCT01601626 (26) [back to overview]CD4 Count Change From Baseline to Week 8
NCT01601626 (26) [back to overview]Cumulative Probability of HIV Virologic Failure at Week 72
NCT01601626 (26) [back to overview]LPV AUC in Participants Enrolled in Arms A, B, and C
NCT01634100 (3) [back to overview]Total Empa: Maximum Measured Concentration (Cmax)
NCT01634100 (3) [back to overview]Total Empagliflozin: Area Under the Curve 0 to Infinity (AUC0-∞)
NCT01634100 (3) [back to overview]Total Empagliflozin: Area Under the Curve 0 to Time of Last Quantifiable Data Point (AUC0-tz)
NCT01765543 (8) [back to overview]Area Under the Plasma Concentration Time-curve From Zero to 168 Hours [AUC(0-168)] of Vemurafenib
NCT01765543 (8) [back to overview]Plasma Apparent Clearance (CL/F) of Vemurafenib
NCT01765543 (8) [back to overview]Plasma Elimination Half Life (t1/2) of Vemurafenib
NCT01765543 (8) [back to overview]Percent Extrapolated AUC(0-inf) (AUCpeo) of Vemurafenib
NCT01765543 (8) [back to overview]Time to Reach Cmax (Tmax) of Vemurafenib
NCT01765543 (8) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Vemurafenib
NCT01765543 (8) [back to overview]Area Under the Plasma Concentration Time-curve From Zero to the Last Measurable Concentration Time Point (AUClast) of Vemurafenib
NCT01765543 (8) [back to overview]Area Under the Plasma Concentration Time-curve From Zero to Extrapolated Infinite Time (AUC[0-inf]) of Vemurafenib
NCT01770392 (3) [back to overview]Area Under the Curve From 0 Extrapolated to Infinity (AUC0-∞)
NCT01770392 (3) [back to overview]Area Under the Curve From 0 to the Last Quantifiable Concentration (AUC0-tz)
NCT01770392 (3) [back to overview]Maximum Measured Concentration (Cmax)
NCT01785186 (3) [back to overview]Frequency of Adverse Events
NCT01785186 (3) [back to overview]Sputum Culture Conversion (2 Negative Cultures) Using Liquid Media
NCT01785186 (3) [back to overview]Pharmacokinetics Including AUC, Cl, t1/2, Vd, and Protein Binding
NCT01844583 (13) [back to overview]Cmax: Maximum Observed Concentration for Alisertib in Presence and Absence of Rifampin
NCT01844583 (13) [back to overview]Phase Elimination Half-life (T1/2) for Alisertib in Presence and Absence of Rifampin
NCT01844583 (13) [back to overview]Terminal Phase Elimination Half-life (T1/2) for Alisertib in Presence and Absence of Esomeprazole
NCT01844583 (13) [back to overview]Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Alisertib in Presence and Absence of Esomeprazole
NCT01844583 (13) [back to overview]Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Alisertib in Presence and Absence of Rifampin
NCT01844583 (13) [back to overview]Change From the Time-matched Baseline in the Fridericia Correction of QTc (QTcF)
NCT01844583 (13) [back to overview]Change From the Time-matched Baseline in the Individually Corrected QTc Interval (QTcI)
NCT01844583 (13) [back to overview]Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT01844583 (13) [back to overview]Cmax: Maximum Observed Concentration for Alisertib in Presence and Absence of Esomeprazole
NCT01844583 (13) [back to overview]AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Alisertib in Presence and Absence of Esomeprazole
NCT01844583 (13) [back to overview]AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Alisertib in Presence or Absence of Rifampin
NCT01844583 (13) [back to overview]AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Alisertib in Presence and Absence of Esomeprazole
NCT01844583 (13) [back to overview]AUC(Last): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Alisertib in Presence and Absence of Rifampin
NCT01908582 (3) [back to overview]Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib
NCT01908582 (3) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib
NCT01908582 (3) [back to overview]Pharmacokinetics, Area Under the Plasma Concentration-Time Curve From Time 0 Hour (h) to Infinity (AUC0-∞) of Evacetrapib
NCT01910311 (3) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Baricitinib
NCT01910311 (3) [back to overview]PK: Maximum Concentration (Cmax) of Baricitinib
NCT01910311 (3) [back to overview]PK: Area Under the Concentration Versus Time Curve From 0 to Infinity [AUC(0-∞)] of Baricitinib
NCT01940510 (13) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC[0-inf]) of Alectinib
NCT01940510 (13) [back to overview]Apparent Oral Clearance (CL/F) of Alectinib
NCT01940510 (13) [back to overview]Plasma Terminal Half-Life (t1/2) of Alectinib and RO5468924
NCT01940510 (13) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of Alectinib and RO5468924
NCT01940510 (13) [back to overview]AUC(0-inf) of RO5468924
NCT01940510 (13) [back to overview]Cmax of RO5468924
NCT01940510 (13) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Alectinib
NCT01940510 (13) [back to overview]Apparent Volume of Distribution (Vz/F) of Alectinib
NCT01940510 (13) [back to overview]Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for AUC(0-inf)
NCT01940510 (13) [back to overview]Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for Cmax
NCT01940510 (13) [back to overview]Total Molar Concentration of Alectinib and RO5468924 as Derived by AUC(0-inf)
NCT01940510 (13) [back to overview]Total Molar Concentration of Alectinib and RO5468924 as Derived by Cmax
NCT01940510 (13) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC[0-last]) of Alectinib and RO5468924
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 0-24 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 144-168 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 24-48 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 48-72 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 480-504 Hours Postdose
NCT01950364 (47) [back to overview]Number of Participants With Markedly Abnormal Laboratory Values
NCT01950364 (47) [back to overview]Number of Participants With Clinically Significant Change From Baseline in Vital Signs
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 96-120 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 336-360 Hours Postdose
NCT01950364 (47) [back to overview]Number of Participants With Anti-therapeutic Antibodies (ATA) to Brentuximab Vedotin
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, Predose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 144-168 Hours Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 480 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 48 Hour Postdose
NCT01950364 (47) [back to overview]Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 4 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 336 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 24 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 0.5 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 144 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 24 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 336 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 4 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 48 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 72 Hour Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 72-96 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 336-360 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 24-48 Hours Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 144 Hour Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 120-144 Hours Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 96 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 0.5 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, Predose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 2, 0.5 Hour Postdose
NCT01950364 (47) [back to overview]Serum Concentrations of Antibody-drug Conjugate (ADC)
NCT01950364 (47) [back to overview]Serum Concentration of Total Antibody (TAb)
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, Predose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 96 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 72 Hour Postdose
NCT01950364 (47) [back to overview]Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 2, Predose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 48-72 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 480-504 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 72-96 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 96-120 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, Predose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 0-24 Hours Postdose
NCT01950364 (47) [back to overview]Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 120-144 Hours Postdose
NCT02019875 (7) [back to overview]Phosphate/Creatinine (mg/g)
NCT02019875 (7) [back to overview]Parathyroid Hormone
NCT02019875 (7) [back to overview]Calcium/Creatinine (mg/g)
NCT02019875 (7) [back to overview]Calcium, Ionized
NCT02019875 (7) [back to overview]25(OH) D3 Vitamin D
NCT02019875 (7) [back to overview]1, 25(OH) D3 Vitamin D
NCT02019875 (7) [back to overview]Osteocalcin
NCT02024555 (8) [back to overview]FEV1%
NCT02024555 (8) [back to overview]Six Minute Walk, Distance in Meters
NCT02024555 (8) [back to overview]Change in Oxygen Saturation
NCT02024555 (8) [back to overview]Adverse Events
NCT02024555 (8) [back to overview]Abnormal Lab Values
NCT02024555 (8) [back to overview]Change in the Saint George's Respiratory Questionnaire (SGRQ)
NCT02024555 (8) [back to overview]Change in Percent Predicted Absolute Forced Vital Capacity (FVC) in Participants With Pulmonary Sarcoidosis, Comparing Baseline With Performance After Completion of 16 Weeks of Therapy.
NCT02024555 (8) [back to overview]Failure of Standard Therapy
NCT02193776 (2) [back to overview]Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System
NCT02193776 (2) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02197247 (18) [back to overview]Assessment of Tss,Max for AZD9291, and AZ5104 and AZ7550 (Metabolites)
NCT02197247 (18) [back to overview]Assessment of Area Under the Plasma Concentration-time Curve During the Dosing Interval for AZD9291 After Dosing Alone and in Combination With Rifampicin (AUCtau)
NCT02197247 (18) [back to overview]Assessment of Css,Max for AZ7550 (Metabolite)
NCT02197247 (18) [back to overview]Assessment of AUCtau for AZD9291 Before and After Rifampicin
NCT02197247 (18) [back to overview]Assessment of AUCtau for Rifampicin
NCT02197247 (18) [back to overview]Assessment of CLss/F for AZD9291
NCT02197247 (18) [back to overview]Assessment of CLss/F for Rifampicin
NCT02197247 (18) [back to overview]Assessment of Css,Max for AZ5104 (Metabolite)
NCT02197247 (18) [back to overview]Assessment of the Metabolic Ratios of Css,Max for AZ5104 and AZ7550 (MRCss,Max)
NCT02197247 (18) [back to overview]Assessment of the Metabolic Ratios of AUCtau for AZ5104 and AZ7550 (MRAUCtau)
NCT02197247 (18) [back to overview]Assessment of Css,Min for AZD9291, and AZ5104 and AZ7550 (Metabolites)
NCT02197247 (18) [back to overview]Assessment of Tss,Max for Rifampicin
NCT02197247 (18) [back to overview]Assessment of Maximum Plasma Concentration for AZD9291 After Dosing Alone and in Combination With Rifampicin (Css,Max)
NCT02197247 (18) [back to overview]Assessment of Css,Min for Rifampicin
NCT02197247 (18) [back to overview]Assessment of Css,Max for Rifampicin
NCT02197247 (18) [back to overview]Assessment of Css,Max for AZD9291 Before and After Rifampicin
NCT02197247 (18) [back to overview]Assessment of AUCtau for AZ5104 (Metabolite)
NCT02197247 (18) [back to overview]Assessment of AUCtau for AZ7550 (Metabolite)
NCT02256267 (2) [back to overview]PK: Area Under the Concentration Time Curve AUC(0-∞) of LY2835219
NCT02256267 (2) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of LY2835219
NCT02256696 (8) [back to overview]Steady State Pharmacokinetics (PK) (AUC) of PA-824 When Given With Rifampin or Rifabutin
NCT02256696 (8) [back to overview]Time to Sputum Culture Conversion on Liquid Medium
NCT02256696 (8) [back to overview]Time to Culture Conversion on Solid Medium
NCT02256696 (8) [back to overview]Percentage of Participants With Sputum Culture Conversion by 8 Weeks of Treatment
NCT02256696 (8) [back to overview]Number of Participants With Grade 3 or Higher Adverse Events
NCT02256696 (8) [back to overview]Number of Participants With Permanent Discontinuation of Assigned Study Regimen
NCT02256696 (8) [back to overview]PK (Cmax) of PA-824 at 200 mg Once Daily With Rifampin or Rifabutin-containing Treatment
NCT02256696 (8) [back to overview]Relationship Between PA-824 Exposure (AUC) and Rate of Change in Time to Positivity (TTP) Over 12 Weeks
NCT02372383 (10) [back to overview]Covariates of PK Measures: C-reactive Protein (CRP)
NCT02372383 (10) [back to overview]Covariates of PK Measures: Circulating Neutrophil Count
NCT02372383 (10) [back to overview]Covariates of PK Measures: Creatinine
NCT02372383 (10) [back to overview]Other PK Measures: Half-life (t1/2)
NCT02372383 (10) [back to overview]Other PK Measures: Drug Clearance
NCT02372383 (10) [back to overview]Other PK Measures: Median Time to Maximal Drug Concentration (Tmax)
NCT02372383 (10) [back to overview]Area Under the Curve (AUC)
NCT02372383 (10) [back to overview]Median Maximal Drug Concentration (Cmax)
NCT02372383 (10) [back to overview]Covariates of PK Measures: Body Mass Index
NCT02372383 (10) [back to overview]Other PK Measures: Volume of Distribution (Vd)
NCT02410772 (1) [back to overview]TB Disease-free Survival at 12M After Study Treatment Assignment Among Participants in Control Regimen, Regimen1 (2HRZE/4HR) to Experimental Regimens, Regimen3 (2HPZM/2HPM) and Regimen2 (2HPZ/2HP) (Assessable Population)
NCT02554318 (6) [back to overview]Change in Body Mass Index (BMI) From Baseline at 2 Months
NCT02554318 (6) [back to overview]Change in Hand-grip Strength on a Digital Dynamometer Scale From Baseline at 2 Months
NCT02554318 (6) [back to overview]Protein Intake on 24-hour Dietary Recall Method.
NCT02554318 (6) [back to overview]Caloric Intake on 24-hour Dietary Recall Method at the 2nd and 6th.
NCT02554318 (6) [back to overview]Change in Distance on 6-minute Walk Test (6MWT) From Baseline at 2 Months
NCT02554318 (6) [back to overview]Change in Bodyweight on a Digital Weight Scale From Baseline at 2 Months
NCT02804399 (22) [back to overview]Plasma CL/F for PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma AUClast for PF-06895751 When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma AUClast for PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma AUCinf for PF-06895751 When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma AUCinf for PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Number of Participants With Physical Examination Findings Meeting the Criteria of Potentially Significant Clinical Concern
NCT02804399 (22) [back to overview]Number of Participants With Concomitant Treatments Meeting the Criteria of Potentially Significant Clinical Concerns
NCT02804399 (22) [back to overview]Plasma Tmax for PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs) (All Causalities and Treatment-Related)
NCT02804399 (22) [back to overview]Number of Participants With End of Study Abnormal Laboratory Findings Meeting the Criteria of Potentially Significant Clinical Concern
NCT02804399 (22) [back to overview]Number of Participants With Electrocardiogram (ECG) Findings Meeting the Criteria of Potentially Significant Clinical Concerns
NCT02804399 (22) [back to overview]Number of Participants With Changes From Baseline and Absolute Values in Vital Signs Meeting the Criteria of Potentially Significant Clinical Concerns
NCT02804399 (22) [back to overview]Number of Participants With Changes From Baseline and Absolute Values in Vital Signs Meeting the Criteria of Potentially Significant Clinical Concerns
NCT02804399 (22) [back to overview]Plasma Vz/F for PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma Tmax for PF-06895751 When PF-06463922 Given Alone and With Rifampin.
NCT02804399 (22) [back to overview]Plasma t1/2 for PF-06895751 When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma t1/2 for PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for Cmax (MRCmax) of PF-06463922 and Its Metabolite: When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for AUClast (MRAUClast) of PF-06463922 and Its Metabolite: When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for AUCinf (MRAUCinf) of PF-06463922 and Its Metabolite: When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma Cmax for PF-06895751 When PF-06463922 Given Alone and With Rifampin
NCT02804399 (22) [back to overview]Plasma Cmax for PF-06463922 Given Alone and With Rifampin
NCT02821832 (1) [back to overview]Comparison of the Rate of Treatment Success at 18 Months (After Treatment Initiation) Between Arms B and C
NCT03077607 (19) [back to overview]Number of Participants With Clinical Significance Abnormalities in Laboratory Parameters
NCT03077607 (19) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT03077607 (19) [back to overview]Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Number of Participants With Clinically Significant Physical Examination Findings
NCT03077607 (19) [back to overview]Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC0-inf) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Area Under the Plasma Concentration-Time Profile From Time Zero to Extrapolated Infinity (AUC0-inf) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Itraconazole
NCT03077607 (19) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Rifampin
NCT03077607 (19) [back to overview]Number of Participants With Clinically Significant Abnormalities in Electrocardiogram (ECG)
NCT03077607 (19) [back to overview]Number of Participants With Clinically Significant Abnormalities in Vital Signs
NCT03174184 (5) [back to overview]Estimate the Antimycobacterial Activity Based on Liquid Culture Time-to-positivity
NCT03174184 (5) [back to overview]Distribution of Minimum Inhibitory Concentration (MIC) of Rifampin
NCT03174184 (5) [back to overview]Estimate of the 14-day Early Bactericidal Activity (EBA), Based on Colony Forming Unit Counts, of the Combination of Meropenem and Amoxicillin/Clavulanate, Without Versus With Rifampin
NCT03174184 (5) [back to overview]AUC for Rifampin
NCT03174184 (5) [back to overview]Frequency of Grade 2 or Higher Adverse Events
NCT03296800 (5) [back to overview]AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)
NCT03296800 (5) [back to overview]Urinary Glucose Excretion 0-48 hr
NCT03296800 (5) [back to overview]Tmax (Time of Maximum Observed Plasma Concentration)
NCT03296800 (5) [back to overview]T1/2 (Apparent Terminal Elimination Half-life)
NCT03296800 (5) [back to overview]Cmax (Maximum Observed Plasma Concentration)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T4 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T4 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T3 vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T1 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Verapamil + R1 (T1) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Rifampin + R1 (T2) vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Probenecid + R1 (T4) vs. R1)
NCT03307252 (12) [back to overview]Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T2 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T3 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T2 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T1 vs. R1)
NCT03307252 (12) [back to overview]Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Cimetidine + R1 (T3) vs. R1)
NCT03311841 (18) [back to overview]Effect of Rifampin on Cmax Post-dose Period 2
NCT03311841 (18) [back to overview]Effect of Rifampin on CL/F Post-dose Period 2
NCT03311841 (18) [back to overview]Effect of Rifampin on C24 Post-dose Period 2
NCT03311841 (18) [back to overview]Effect of Rifampin on AUC0-last Post-dose Period 2
NCT03311841 (18) [back to overview]Apparent Clearance After Extravascular Administration (CL/F) Post-dose Period 1
NCT03311841 (18) [back to overview]Effect of Rifampin on AUC0-inf Post-dose Period 2
NCT03311841 (18) [back to overview]Effect of Rifampin on AUC0-24 Post-dose Period 2
NCT03311841 (18) [back to overview]Area Under the Plasma Concentration-time Curve From Time 0 to Last (AUC0-last) Post-dose Period 1
NCT03311841 (18) [back to overview]Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC0-inf) Post-dose Period 1
NCT03311841 (18) [back to overview]Area Under the Plasma Concentration-time Curve From Time 0 to 24 Hours (AUC0-24) Post-dose Period 1
NCT03311841 (18) [back to overview]Apparent Volume of Distribution During the Terminal Phase (Vz/F) Post-dose Period 1
NCT03311841 (18) [back to overview]Apparent Plasma Terminal Half-life (t1/2) Post-dose Period 1
NCT03311841 (18) [back to overview]Effect of Rifampin on t1/2 Post-dose Period 2
NCT03311841 (18) [back to overview]Effect of Rifampin on Tmax Post-dose Period 2
NCT03311841 (18) [back to overview]Effect of Rifampin on Vz/F Post-dose Period 2
NCT03311841 (18) [back to overview]Maximum Plasma Concentration (Cmax) Post-dose Period 1
NCT03311841 (18) [back to overview]Plasma Concentration at 24 Hours (C24) Post-dose Period 1
NCT03311841 (18) [back to overview]Time to Maximum Plasma Concentration (Tmax) Post-dose Period 1
NCT03338621 (2) [back to overview]Time to Culture Negative Status
NCT03338621 (2) [back to overview]Number of Participants With Culture Negative Status by 8 Weeks
NCT03486314 (7) [back to overview]Part A: Ratio of Maximum Observed Plasma Concentration (Cmax) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)
NCT03486314 (7) [back to overview]Part A: Terminal Disposition Phase Half-life (T1/2z) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)
NCT03486314 (7) [back to overview]Part A: Total Clearance After Intravenous Administration (CL) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)
NCT03486314 (7) [back to overview]Part A: Volume of Distribution at Steady State After Intravenous Administration (Vss) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)
NCT03486314 (7) [back to overview]Part B: Number of Participants With Best Overall Response as Per Investigator's Assessment
NCT03486314 (7) [back to overview]Part A: Ratio of Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)
NCT03486314 (7) [back to overview]Part A: Ratio of Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC∞) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025m1 in Part 1
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025, KD025m1, and KD025m2 in Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: Cmax of KD025 and KD025m2 in Part 1
NCT03530995 (5) [back to overview]Pharmacokinetics: AUC(0-inf) and AUC(0-24) of KD025 and KD025 m2 for Subject in Part 1 and Part 2
NCT03530995 (5) [back to overview]Pharmacokinetics: AUC(0-24) of KD025m1 for Part 1 and for Part 2
NCT03586726 (14) [back to overview]Area Under the Plasma Concentration Curve From Time 0 to 24 Hours (AUC0-24) for Balovaptan
NCT03586726 (14) [back to overview]Metabolite to Parent Ratio for M2 Metabolite Based on AUC0-24
NCT03586726 (14) [back to overview]Percentage of Participants With Adverse Events
NCT03586726 (14) [back to overview]Time to Maximum Observed Plasma Concentration for M3 Metabolite
NCT03586726 (14) [back to overview]Time to Maximum Observed Plasma Concentration for M2 Metabolite
NCT03586726 (14) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) for Balovaptan
NCT03586726 (14) [back to overview]Metabolite to Parent Ratio for M3 Metabolite Based on Cmax
NCT03586726 (14) [back to overview]Metabolite to Parent Ratio for M3 Metabolite Based on AUC0-24
NCT03586726 (14) [back to overview]Metabolite to Parent Ratio for M2 Metabolite Based on Cmax
NCT03586726 (14) [back to overview]Maximum Plasma Concentration (Cmax) for M3 Metabolite
NCT03586726 (14) [back to overview]Maximum Plasma Concentration (Cmax) for M2 Metabolite
NCT03586726 (14) [back to overview]Maximum Plasma Concentration (Cmax) for Balovaptan
NCT03586726 (14) [back to overview]Area Under the Plasma Concentration Curve From Time 0 to 24 Hours for M3 Metabolite
NCT03586726 (14) [back to overview]Area Under the Plasma Concentration Curve From Time 0 to 24 Hours for M2 Metabolite
NCT03928327 (7) [back to overview]Treatment B vs Treatment A (Part 1), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914
NCT03928327 (7) [back to overview]Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914
NCT03928327 (7) [back to overview]Treatment B Vs Treatment A (Part 1), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914
NCT03928327 (7) [back to overview]Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of TAK-788
NCT03928327 (7) [back to overview]Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32960
NCT03928327 (7) [back to overview]Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32914
NCT03928327 (7) [back to overview]Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914
NCT03994211 (20) [back to overview]AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part B
NCT03994211 (20) [back to overview]Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part A
NCT03994211 (20) [back to overview]AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part A
NCT03994211 (20) [back to overview]Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)
NCT03994211 (20) [back to overview]Number of Participants With Clinically Significant Abnormalities in Laboratory Assessments, Vital Signs, ECG Parameters and Physical Examinations
NCT03994211 (20) [back to overview]Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part B
NCT03994211 (20) [back to overview]AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part B
NCT03994211 (20) [back to overview]AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part A
NCT03994211 (20) [back to overview]AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part A
NCT04029584 (3) [back to overview]Cmax
NCT04029584 (3) [back to overview]Tmax
NCT04029584 (3) [back to overview]AUC
NCT04060719 (3) [back to overview]Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)
NCT04060719 (3) [back to overview]Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)
NCT04060719 (3) [back to overview]Maximum Measured Concentration of BI 894416 in Plasma (Cmax)
NCT04121078 (7) [back to overview]Number of Participants With Clinically Significant Change From Baseline in Clinical Laboratory Values
NCT04121078 (7) [back to overview]Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings
NCT04121078 (7) [back to overview]Number of Participants With Clinically Significant Change From Baseline in Vital Sign Values
NCT04121078 (7) [back to overview]Cmax: Maximum Observed Plasma Concentration for TAK-906
NCT04121078 (7) [back to overview]AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-906
NCT04121078 (7) [back to overview]AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-906
NCT04121078 (7) [back to overview]Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)
NCT04463680 (1) [back to overview]Serum Etonogestrel Concentrations
NCT04493931 (139) [back to overview]Cohort 2: Lag Time Before Observation of Drug Concentrations (Tlag) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 2: T1/2 of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Tmax of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose )
NCT04493931 (139) [back to overview]Cohort 3: AUC (0-48) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 4: Accumulation Ratio Based on AUC(0-tau) (RoAUC) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Serious Adverse Events (SAE) and Non-serious Adverse Events (Non-SAE)
NCT04493931 (139) [back to overview]Cohort 4: Number of Participants With Any Increase in Maximum Post-Baseline Electrocardiogram (ECG) Parameter Corrected QT (QTc) Interval
NCT04493931 (139) [back to overview]Cohort 4: Ae(t1-t2) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Ae(t1-t2) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Terminal Phase Half-life (t1/2) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With SAE and Non-SAE
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval
NCT04493931 (139) [back to overview]Cohort 3: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With SAE and Non-SAE
NCT04493931 (139) [back to overview]Cohort 2: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval
NCT04493931 (139) [back to overview]Cohort 2: Ae(t1-t2) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With SAE and Non-SAE
NCT04493931 (139) [back to overview]Cohort 1: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval
NCT04493931 (139) [back to overview]Cohort 1: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 4: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Vz/F of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Tlag of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose )-Fed State
NCT04493931 (139) [back to overview]Cohort 3: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline
NCT04493931 (139) [back to overview]Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) for Gepotidacin 1500 mg Under Fed Condition
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: CLr of Gepotidacin Following Two 3000 mg Dose-Fed State
NCT04493931 (139) [back to overview]Cohort 4: CLr of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition
NCT04493931 (139) [back to overview]Cohort 4: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: CL/F of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Evening Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-tau) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-48) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-48) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 4: AUC(0-24) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: AUC From Time 0 (Predose) to Time Tau (AUC[0-tau]) of Gepotidacin in Plasma After the First Dose of 3000 Mg-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 48 Hours Post-dose (AUC[0-48]) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 24 Hours Post-dose (AUC[0-24]) of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04493931 (139) [back to overview]Cohort 4: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State
NCT04493931 (139) [back to overview]Cohort 4: Ae Total of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine
NCT04493931 (139) [back to overview]Cohort 4: Accumulation Ratio Based on Cmax (RoCmax) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State
NCT04493931 (139) [back to overview]Cohort 3: Vz/F of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Vz/F of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: Tmax of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tlag of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: Tlag of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: T1/2 of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose+ Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: T1/2 of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: RoCmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: RoAUC of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Percentage of the Given Dose of Drug Excreted in Urine (fe%) Following Two 3000 mg Doses of Gepotidacin (First Dose + Second Dose )
NCT04493931 (139) [back to overview]Cohort 3: Minimum Observed Concentration (Cmin) of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Cmin of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Apparent Oral Clearance (CL/F) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Apparent Volume of Distribution (Vz/F) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC (0-24) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC[0-infinity]) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC(0-24) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 1: AUC(0-48) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: AUC(0-48) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 1: Maximum Observed Concentration (Cmax) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 1: Renal Clearance (CLr) of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 1: Time to Reach Maximum Observed Concentration (Tmax) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Tlag of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 1: Total Unchanged Drug (Ae Total) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: Ae Total of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-24) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: Cmax of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-24) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-48) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: Vz/F of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-48) of Gepotidacin in Urine
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-infinity) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: AUC(0-t) of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: CL/F of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 2: CLr of Gepotidacin
NCT04493931 (139) [back to overview]Cohort 2: Cmax of Gepotidacin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: CLr of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: CL/F of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: CL/F of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-tau) of Gepotidacin in Plasma First Dose of 3000 mg (First Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-t) of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-t) of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-infinity) of Midazolam in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-infinity) of Digoxin in Plasma
NCT04493931 (139) [back to overview]Cohort 3: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)
NCT04493931 (139) [back to overview]Cohort 4: T1/2 of Gepotidacin Following Single Dose of 1500 mg in Plasma
NCT04532918 (21) [back to overview]Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Vss/F) of Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Based on the Terminal Phase) (Vz/F) of Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Time to Reach Peak or Maximum Plasma Concentration (Tmax) for Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Terminal Elimination Rate Constant (λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Number of Participants With Adverse Events (AEs) and Serious AEs (SAEs)
NCT04532918 (21) [back to overview]Metabolite:Parent (MP) Cmax Ratios for M1 and M8: Verinurad
NCT04532918 (21) [back to overview]Metabolite:Parent (MP) AUClast Ratios for M1 and M8: Verinurad
NCT04532918 (21) [back to overview]Metabolite:Parent (MP) AUCinf Ratios for M1 and M8: Verinurad
NCT04532918 (21) [back to overview]Mean Residence Time of the Unchanged Drug in the Systemic Circulation (MRTinf) for Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUCinf for Verinurad Metabolites: M1 and M8
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUCinf for Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Area Under Plasma Concentration-time Curve From Zero to 24 Hours Post-dose AUC(0-24) of Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUClast for Verinurad Metabolites: M1 and M8
NCT04532918 (21) [back to overview]Geometric Mean Ratio of AUClast for Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Apparent Total Body Clearance of Drug From Plasma After Extravascular Administration (CL/F) for Verinurad and Allopurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Maximum Observed Plasma Peak Concentration (Cmax) for Verinurad
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Area Under the Plasma Concentration-time Curve From Zero to Time of Last Quantifiable Concentration (AUClast) for Verinurad
NCT04532918 (21) [back to overview]Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration Time Curve (t½λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Cmax for Verinurad Metabolites: M1 and M8
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Cmax for Allopurinol and Oxypurinol
NCT04532918 (21) [back to overview]Geometric Mean Ratio of Area Under Plasma Concentration-time Curve From Time Zero to Infinity (AUCinf) for Verinurad
NCT05098041 (5) [back to overview]Number of Participants Reported One or More Treatment-Emergent Adverse Events (TEAEs)
NCT05098041 (5) [back to overview]Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Soticlestat When Administered Alone and With Rifampin
NCT05098041 (5) [back to overview]AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Soticlestat When Administered Alone and With Rifampin
NCT05098041 (5) [back to overview]AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Soticlestat When Administered Alone and With Rifampin
NCT05098041 (5) [back to overview]Cmax: Maximum Observed Plasma Concentration for Soticlestat When Administered Alone and With Rifampin

Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,,,,,,,,,,,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
2nd Trimester3rd TrimesterPostpartum
ATV/RTV Arm 1: 300/100mg q.d.11212
DRV/COBI 800/150 mg q.d.3414
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.71622
DRV/RTV 600/100mg b.i.d.71922
DRV/RTV 800/100mg q.d.91922
DTG 50mg q.d.92023
EFV 600 mg q.d. (Outside THA)123334
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.82927
ETR 200mg b.i.d.5137
EVG/COBI 150/150mg q.d.81018
FPV/RTV 700/100mg b.i.d.82622
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)101926
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.93027
ATV/COBI 300/150 mg q.d.125
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA1514
RAL 400mg b.i.d.113330
RPV 25mg q.d.142625
TAF 10mg q.d. w/COBI152322
TAF 25mg q.d.132324
TAF 25mg q.d. w/COBI or RTV Boosting102418
TFV 300mg q.d.22727
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.11112
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.72332

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. (NCT00042289)
Timeframe: Blood samples were collected at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

,,,
Interventionmcg/mL (Median)
2-10 hours after birth18-28 hours after birth36-72 hours after birth5-9 days after birth
DRV/COBI 800/150 mg q.d.0.351.431.871.72
DTG 50mg q.d.1.731.531.000.06
EFV 600 mg q.d. (Outside THA)1.11.00.90.4
EVG/COBI 150/150mg q.d.0.1320.0320.0050.005

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

Interventionng*hour/mL (Geometric Mean)
2nd Trimester3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.NA27173645

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.55.151.879.6
DRV/RTV 600/100mg b.i.d.45.845.961.7
FPV/RTV 700/100mg b.i.d.43.5032.1551.60
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA34.233.5

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24 (area under the curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

,,,,,,,,,,,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.25.3318.8536.20
ATV/RTV Arm 1: 300/100mg q.d.88.241.957.9
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.30.645.748.8
DRV/COBI 800/150 mg q.d.50.0042.0595.55
DRV/RTV 800/100mg q.d.64.663.5103.9
DTG 50mg q.d.47.649.265.0
EFV 600 mg q.d. (Outside THA)47.3060.0262.70
EVG/COBI 150/150mg q.d.15.314.021.0
TAF 10mg q.d. w/COBI0.1970.2060.216
TAF 25mg q.d.0.1710.2120.271
TAF 25mg q.d. w/COBI or RTV Boosting0.1810.2570.283
TFV 300mg q.d.1.92.43.0
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.14.528.839.6
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.26.237.758.7

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Plasma Concentration for Contraceptives

Serum concentrations of the contraceptives. Note that no historical controls were provided by team pharmacologists and thus no comparisons were done for contraceptive concentrations in women using hormonal contraceptives and selected ARV drugs as compared to historical controls not using those ARV drugs. (NCT00042289)
Timeframe: Measured at 6-7 weeks after contraceptive initiation postpartum

Interventionpg/mL (Median)
ATV/RTV/TFV 300/100/300mg q.d. With ENG604
LPV/RTV 400/100 b.i.d. With ENG428
EFV 600mg q.d. With ENG125

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Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12h (area-under-the-curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8 and 12 hours post dosing.

Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
LPV/RTV 400/100 b.i.d. With ENG115.97100.20

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Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC (area under the curve) were determined using the linear trapezoidal rule. See PK target in the Protocol Appendix V. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 (and 24) hours post dosing.

,
InterventionParticipants (Count of Participants)
3rd TrimesterPostpartum
EFV 600mg q.d.2021
MVC 150 or 300mg b.i.d.87

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PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC12 (area under the curve from 0 to 12 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured in 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, and 12 hrs post dosing.

,,,
Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.4.58.35.3
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)14.916.127.1
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.7296133
RAL 400mg b.i.d.6.65.411.6

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.701.010.63
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.8.410.714.6
RAL 400mg b.i.d.2.2501.7703.035
RPV 25mg q.d.0.1450.1340.134

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.2.822.203.90
ATV/RTV Arm 1: 300/100mg q.d.NA3.64.1
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.3.114.514.52
DRV/COBI 800/150 mg q.d.4.593.677.04
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.6.226.558.96
DRV/RTV 600/100mg b.i.d.5.645.537.78
DRV/RTV 800/100mg q.d.6.775.788.11
DTG 50mg q.d.3.623.544.85
EFV 600 mg q.d. (Outside THA)3.875.134.41
FPV/RTV 700/100mg b.i.d.5.615.126.75
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)3.893.625.37
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA5.15.0
TFV 300mg q.d.0.2500.2450.298
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.1.22.54.1
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.2.733.565.43

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PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.2.842.524.51
DRV/RTV 600/100mg b.i.d.2.122.222.51
FPV/RTV 700/100mg b.i.d.2.121.642.87
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.NA0.470.52

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PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.5.445.10

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.1.9691.6692.387

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PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8, 12 and 24 hours post dosing.

Interventionmg*hour/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.55.458.3

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

Interventionng/mL (Median)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.448647

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PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Cmax was the maximum observed concentration after a dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm; Blood samples were drawn pre-dose and at 1, 2, 4, 6, 8,12 (and 24) hours post dosing.

,,,
Interventionng/mL (Median)
2nd Trimester3rd TrimesterPostpartum
EVG/COBI 150/150mg q.d.1447.11432.81713.1
TAF 10mg q.d. w/COBI80.491.298.2
TAF 25mg q.d.69.796133
TAF 25mg q.d. w/COBI or RTV Boosting87.8107141

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PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

Interventionng/mL (Geometric Mean)
3rd TrimesterPostpartum
MVC 150 or 300mg b.i.d.108128

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
3rd TrimesterPostpartum
EFV 600mg q.d.1.602.05

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PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs

"Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose.~For the TAF 25 mg q.d., 10 mg q.d. w/COBI, and 25 mg q.d. w/COBI or RTV boosting arms, samples were all below the limit of quantification and statistical analyses were not conducted." (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

,,,,,,,,,,,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ATV/COBI 300/150 mg q.d.0.210.210.61
ATV/RTV Arm 1: 300/100mg q.d.2.00.71.2
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.490.710.90
DRV/COBI 800/150 mg q.d.0.330.271.43
DRV/RTV 800/100mg q.d.0.991.172.78
DTG 50mg q.d.0.730.931.28
EFV 600 mg q.d. (Outside THA)1.491.481.94
EVG/COBI 150/150mg q.d.0.02580.04870.3771
TAF 10mg q.d. w/COBI0.001950.001950.00195
TAF 25mg q.d.0.001950.001950.00195
TAF 25mg q.d. w/COBI or RTV Boosting0.001950.001950.00195
TFV 300mg q.d.0.0390.0540.061
TFV/ATV/RTV Arm 1: 300/300/100mg q.d.0.30.50.8
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.440.571.26

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PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 12h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation); 3rd trimester (30-38 gestation); and either 2-3 wks, 2-8 wks, or 6-12 wks postpartum, depending on study arm. Trough concentration was measured 12 hrs after an observed dose.

,,,
Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
ETR 200mg b.i.d.0.360.480.38
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.130.130.28
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.3.75.17.2
RAL 400mg b.i.d.0.06210.0640.0797

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PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. Trough concentration was the measured concentration from the 24h post-dose sample after an observed dose. (NCT00042289)
Timeframe: Measured at 2nd trimester (20-26 wks gestation), 3rd trimester (30-38 wks gestation), and either 2-3 wks, 2-8 wks or 6-12 wks postpartum depending on study arm. Trough concentration was measured 24 hrs after an observed dose.

Interventionmg/L (Median)
2nd Trimester3rd TrimesterPostpartum
RPV 25mg q.d.0.0630.0560.081

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Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms

Pharmacokinetic parameters were determined from plasma concentration-time profiles using noncompartmental methods. AUC24h (area-under-the-curve from 0 to 24 hours) were determined using the linear trapezoidal rule. (NCT00042289)
Timeframe: Measured at 2-12 wks postpartum before contraceptive initiation and 6-7 wks after contraceptive initiation. Blood samples were drawn pre-dose and at 0, 1, 2, 6, 8, 12, and 24 hours post dosing.

,
Interventionmcg*hr/mL (Median)
Before contraceptive initiationAfter contraceptive initiation
ATV/RTV/TFV 300/100/300mg q.d. With ENG53.9655.25
EFV 600mg q.d. With ENG53.6456.65

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Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs

Infant plasma concentrations were collected and measured during the first 9 days of life. Half-life is defined as 0.693/k, where k, the elimination rate constant, is the slope of the decline in concentrations. (NCT00042289)
Timeframe: Infant plasma samples at 2-10, 18-28, 36-72 hours and 5-9 days after birth.

Interventionhour (Median)
DTG 50mg q.d.32.8
EVG/COBI 150/150mg q.d.7.6
DRV/COBI 800/150 mg q.d.NA
EFV 600 mg q.d. (Outside THA)65.6

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
DRV/RTV 600 or 800 or 900/100mg b.i.d. Then 800 or 900/100mg b.i.d. Then 600/100mg b.i.d.0.15
DTG 50mg q.d.1.25
EVG/COBI 150/150mg q.d.0.91
DRV/COBI 800/150 mg q.d.0.07
ATV/COBI 300/150 mg q.d.0.07
TFV 300mg q.d.0.88

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PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs

Cord blood and maternal plasma concentrations were collected and measured at delivery, and compared as a ratio. For arms with zero overall participants analyzed, samples were below the limit of quantification and ratios could not be calculated. (NCT00042289)
Timeframe: Measured at time of delivery with single cord blood and single maternal plasma sample.

Interventionunitless (Median)
TAF 10mg q.d. w/COBI0.97
EFV 600 mg q.d. (Outside THA)0.67
EFV 600mg q.d.0.49
LPV/RTV Arm 3: 400/100mg b.i.d. Then 600/150mg b.i.d. Then 400/100mg b.i.d.0.2
RAL 400mg b.i.d.1.5
ETR 200mg b.i.d.0.52
MVC 150 or 300mg b.i.d.0.33
ATV/RTV Arm 2: 300/100mg q.d. Then 400/100mg q.d. Then 300/100mg q.d.0.14
TFV/ATV/RTV Arm 2: 300/300/100mg q.d. Then 300/400/100mg q.d Then 300/300/100mg q.d.0.16
NFV Arm 2: 1250mg b.i.d. Then 1875mg b.i.d. Then 1250mg b.i.d.0.19
IDV/RTV Arm 2: 400/100mg q.d. (Only THA)0.12
RPV 25mg q.d.0.55
ATV/RTV 300/100mg q.d. or TFV/ATV/RTV 300/300/100mg q.d.0.18
DRV/RTV 800/100mg q.d. or DRV/RTV 600/100mg b.i.d.0.18

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Number of Participants With Laboratory Test or Clinical Judgment Resulting in the Need to Stop Study Medication

Liver function tests were taken at regular intervals and clinical symptoms were reviewed at regular intervals in both study groups. On the basis of these tests and examinations, physicians determined whether the study drug needed to be stopped. (NCT00128206)
Timeframe: up to one year

Interventionparticipants (Number)
Isoniazid6
Rifampin3

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Completion of Therapy

(NCT00128206)
Timeframe: course of treatment

InterventionParticipants (Count of Participants)
Isoniazid47
Rifampin60

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Acquired Drug Resistance in Patients Who Relapsed

(NCT00130247)
Timeframe: 2 years

InterventionParticipants (Number)
4-Month Arm0
6-Month Arm0

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Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-TB Treatment - Per-protocol

Patients who presented with TB after completion of study phase treatment but before the end of follow-up were classified as relapses. A bacteriologic relapse was defined as a patient who became consistently culture-positive [defined as at least 1 of the following]: (a) at least 1 sputum mycobacterial culture growing at least 10 colonies of MTB on solid medium; (b) 2 or more respiratory secretion cultures that are positive for MTB in liquid media; or (c) any culture from an extrapulmonary site that is positive for MTB during follow-up after successful completion of initial anti-TB treatment. (NCT00130247)
Timeframe: 30 months

InterventionParticipants (Number)
4-Month Arm13
6-Month Arm3

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Bacteriologic or Clinical Relapse at 30 Months After Onset of Initial Anti-tuberculosis (TB) Treatment - Intention-to-treat

Patients who presented with TB after completion of study phase treatment but before the end of follow-up were classified as relapses. A bacteriologic relapse was defined as a patient who became consistently culture-positive [defined as at least 1 of the following]: (a) at least 1 sputum mycobacterial culture growing at least 10 colonies of MTB on solid medium; (b) 2 or more respiratory secretion cultures that are positive for MTB in liquid media; or (c) any culture from an extrapulmonary site that is positive for MTB during follow-up after successful completion of initial anti-TB treatment. (NCT00130247)
Timeframe: 30 months

InterventionParticipants (Number)
4-Month Arm13
6-Month Arm3

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Relapses at 1 and 2 Years

(NCT00130247)
Timeframe: 1 and 2 years after successful completion of initial anti-TB treatment

,
InterventionParticipants (Number)
Relapses at 1 yearRelapses at 2 years
4-Month Arm1013
6-Month Arm33

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Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Intention to Treat

A culture-positive treatment failure was defined as initial culture conversion but subsequent reversion to culture positivity. A clinical treatment failure was defined as a patient with clinical and/or radiographic evidence of progressive tuberculosis not confirmed by a positive culture after 4 or more months of anti-TB treatment while still receiving treatment. Patients who defaulted before completing study treatment and returned later with culture-positive tuberculosis were termed failures after non-adherence. (NCT00130247)
Timeframe: 2 years

,
InterventionParticipants (Number)
Treatment FailuresRelapses
4-Month Arm013
6-Month Arm03

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Treatment Failures or Relapses at 2 Years After Completion of TB Treatment: Per Protocol

A culture-positive treatment failure was defined as initial culture conversion but subsequent reversion to culture positivity. A clinical treatment failure was defined as a patient with clinical and/or radiographic evidence of progressive tuberculosis not confirmed by a positive culture after 4 or more months of anti-TB treatment while still receiving treatment. Patients who defaulted before completing study treatment and returned later with culture-positive tuberculosis were termed failures after non-adherence. (NCT00130247)
Timeframe: 2 years

,
InterventionParticipants (Number)
Treatment FailuresRelapses
4-Month Arm013
6-Month Arm03

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Time Taken for Plasma Concentration to Reduce by 50 Percent or Apparent Terminal Plasma Elimination Half-life (T Half)

T half was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

InterventionHrs (Mean)
Ixabepilone50.85
Ixabepilone + Rifampin36.45

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Time to Reach Maximum Observed Concentration (T Max)

T max was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

InterventionHrs (Median)
Ixabepilone1.57
Ixabepilone + Rifampin1.50

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Total Body Clearance (CLT)

CLT was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

InterventionLitres(L)/hr (Mean)
Ixabepilone28.36
Ixabepilone + Rifampin49.99

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Volume of Distribution at Steady-state (Vss)

Vss was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

InterventionL (Mean)
Ixabepilone1323.26
Ixabepilone + Rifampin1447.54

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Number of Participants With Grade 3-4 Hematology Abnormalities

Abnormalities occurring at any time during the study were graded per NCI CTC, v3.0 criteria (Grade 1 = mild, Grade 2 = moderate, Grade 3 = severe, Grade 4 = life threatening). Grade 3 and 4 criteria are given below. Neutrophils: Grade 3: 0.5 - <1.0x10^9/L, Grade 4: <0.5x10^9/L. Leukocytes: Grade 3: 1.0 - <2.0x10^9/L, Grade 4: <1.0x10^9/L. Neutrophils + bands (absolute): Grade 3: 0.5 - <1.0x10^9/L, Grade 4: <0.5x10^9/L. Hemoglobin: Grade 3:6.5 - <8.0g/dL, Grade 4: <6.5g/dL. Lymphocytes: Grade 3: 0.2 - <0.5x10^9/L, Grade 4: <0.2x10^9/L. Platelets: Grade 3: 25.0 - <50.0x10^9/L, Grade 4: <25.0x10. (NCT00207090)
Timeframe: Screening, Day 1, Day 8, Day 15, Day 22 and Day 29-36.

Interventionparticipants (Number)
Neutrophils (absolute)LeukocytesNeutrophils + bands (absolute)HemoglobinLymphocytes (absolute)Platelet count
All Participants565160

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Number of Participants With Grade 3-4 Serum Chemistry Abnormalities in Alanine Aminotransferase, Aspartate Aminotransferase, Bilirubin, Albumin and Phosphorous

Abnormalities occurring at any time during the study were graded per the NCI CTC (1=mild, 2=moderate, 3=severe, 4=life threatening). Grade 3 and 4 criteria were as follows: Alanine aminotransferase, aspartate aminotransferase and alkaline phosphatase: Grade 3: >5-20 x upper limit of normal (ULN), Grade 4: >20 x ULN. Bilirubin: Grade 3: >3-10 x ULN, Grade 4: >10 x ULN. Albumin: Grade 3: <2g/dL (Grade 4 not defined in NCI CTC). Creatinine: Grade 3: >3-6 x ULN, Grade 4: >6 x ULN. Phosphorous: Grade 3: 1-<2mg/dL, Grade 4: <1mg/dL. (NCT00207090)
Timeframe: Screening, Days 1 and 22.

Interventionparticipants (Number)
Alanine AminotransferaseAspartate AminotransferaseAlkaline PhosphataseBilirubinAlbuminCreatininePhosphorous (inorganic)
All Participants0000001

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Number of Participants With Grade 3-4 Serum Chemistry Abnormalities in Calcium, Magnesium, Potassium, Sodium, Glucose and Uric Acid.

Abnormalities occurring at any time during the study were graded per NCI CTC (1=mild, 2=moderate, 3=severe, 4=life threatening). Grade 3 and 4 criteria were as follows:Calcium: Grade 3: 6-<7 or >12.5-13.5mg/dL, Grade 4:<6 or >13.5mg/dL. Magnesium: Grade 3:0.6-<0.8 or >2.46-6.6mEq/L, Grade 4:<0.6 or >6.6mEq/L. Potassium: Grade 3:2.5-<3 or >6-7mmol/L, Grade 4:<2.5 or >7.0 mmol/L. Sodium: Grade 3:120-<130 or >155-160 mEq/L, Grade 4:<120 or >160mEq/L. Glucose: Grade 3:30-<40 or >250-500mg/dL, Grade 4:<30 or >500mg/dL. Uric acid: Grade 3:>ULN-10mg/dL with physiologic consequences, Grade 4:>10mg/dL. (NCT00207090)
Timeframe: Screening, Days 2 and 22.

InterventionParticipants (Number)
Calcium (total)Magnesium (serum)Potassium (serum)Sodium (serum)Glucose (serum)Uric acid
All Participants000100

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Number of Participants With Identified ECG Abnormalities

Triplicate 12-lead serial ECGs were performed pre-dose (just prior to infusion), 1.5, 3 (just prior to end of the infusion even if infusion lasted for less than or more than planned 3 hrs), 4, 6, 8 and 24 hrs after start of ixabepilone infusion. Triplicate 12-lead serial ECGs were also to be performed on the date prior to dosing at times approximating post-dose schedule (pre-dose triplicate set of ECGs also qualified as the 24-hr baseline ECGs). Normal ranges for ECG are as follows: heart rate: 40 - 125 bpm; PR: 0.1 - 0.2 msec; QRS: 0.06 - 0.12 msec; QTC: 0.3 - 0.45 msec; QT: 0.3 - 0.5 msec. (NCT00207090)
Timeframe: Data collected at screening, Day -1 and Day 1 (at 0, 1.5, 3, 4, 6, 8 and 24 hours) after start of infusion.

InterventionParticipants (Number)
Newly identified ECG abnormalitiesDiscontinuation due to ECG abnormalitiesAbnormalities related to QT/QTc intervalTotal number of ECG abnormalities
All Participants131013

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QT Interval Corrected for Heart Rate (QTcF)

QT interval corrected for heart rate (QTcF) was assessed using triplicate 12-lead serial electrocardiograms (ECGs) that were performed at selected times after the first dose of ixabepilone without rifampin and at matched times prior to the first dose of ixabepilone. Abnormalities occurring at any time during the study were recorded. (NCT00207090)
Timeframe: Data collected at 0, 1.5, 3, 4, 6, 8 and 24 hours after start of infusion.

Interventionmillisecond (Mean)
0 hour (n=9)1.5 hour (n=14)3 hour (n=14)4 hour (n=11)6 hour (n=13)8 hour (n=3)24 hour (n=10)
Ixabepilone3.445.640.577.826.54-10.70-1.90

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Urine 6B-Hydroxycortisol to Cortisol Ratio on Day -1

The urine 6B-hydroxycortisol to cortisol ratio is a measure of hepatic CYP3A4/3A5 activity, which is a potential marker of the rate of clearance of ixabepilone. The urine 6B-hydroxycortisol to cortisol ratios were calculated on Day -1. (NCT00207090)
Timeframe: Day -1 (0-8 hours and 8-24 hours), 24 hours before starting of ixabepilone administration.

InterventionRatio (Mean)
0-8 hours8-24 hours
All Participants10.049.29

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Urine 6B-Hydroxycortisol to Cortisol Ratio on Day 22

The urine 6B-hydroxycortisol to cortisol ratio is a measure of hepatic CYP3A4/3A5 activity, which is a potential marker of the rate of clearance of ixabepilone. The urine 6B-hydroxycortisol to cortisol ratios were calculated on Day -1. (NCT00207090)
Timeframe: Day 22 (0-8 hours and 8-24 hours) during ixabepilone and rifampin co-administration.

InterventionRatio (Median)
0-8 hours8-24 hours
Ixabepilone + Rifampin110.8862.42

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Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinite Time (AUC [INF])

AUC (INF) was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

Interventionnanogram (ng)*hour(hr)/mL (Geometric Mean)
Ixabepilone3028.70
Ixabepilone + Rifampin1713.07

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Number of Participants With Abnormal Physical Examination Findings

"Physical examination included height (screening only),weight,BSA,Eastern Cooperative Oncology Group Performance Status (ECOG PS),tendon reflexes,sensory function,motor strength. ECOG PS used to assess disease severity:score of 0 is fully active;1 is restricted physically strenuous activity;2 is ambulatory but unable to work;3 is capable of only limited self care;4 is completely disabled;5 is dead. Normal ranges:height:137-200cm or 54-79 inches;weight:40-135kg or 88-298 pounds (lbs);ECOG Scale:0-4. Abnormalities displayed here are those considered clinically significant by the investigator." (NCT00207090)
Timeframe: From screening to the off treatment visit.

Interventionparticipants (Number)
Weight-related abnormalitiesOther physical examination abnormalities
All Participants30

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Maximum Plasma Concentration (Cmax)

Cmax was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

Interventionnanogram (ng)/millilter(mL) (Geometric Mean)
Ixabepilone338.23
Ixabepilone + Rifampin308.37

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Mean Residence Time Adjusted for Infusion Time (MRT [INF])

(MRT [INF]) was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

InterventionHrs (Mean)
Ixabepilone50.93
Ixabepilone + Rifampin29.86

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Number of Participants With Clinically Meaningful Vital Signs Measures

"Vital signs were recorded throughout the study and included investigations related to body temperature, respiratory rate, seated blood pressure (systolic and diastolic), and heart rate. Normal ranges for the above are as follows: heart rate: 40 - 125 beats per minute (bpm); systolic BP: 65 - 200 millimeters of mercury (mmHg); diastolic BP: 40 - 120 mmHg; respiratory rate: 10 - 25 breaths per minute; temperature: 95 - 105F or 35 - 40.5C. The abnormalities displayed here are those considered clinically significant by the investigator and include abnormalities recorded at any time during study." (NCT00207090)
Timeframe: From screening to the off treatment visit.

Interventionparticipants (Number)
All Participants0

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Area Under the Plasma Concentration-time Curve From Time Zero to Time of Last Quantifiable Concentration (AUC [0-T])

AUC (0-T) was obtained directly from the concentration-time data. (NCT00207090)
Timeframe: Blood samples were collected on Day 1 (pre-dose, then 1h30, 3h, 3h15, 3h30, 4h, 6h and 8h), Day 2, Day 3, Day 4 and Day 8 during ixabepilone administration and repeated for Cycle 2 (Days 22-25 and 29) during ixabepilone and rifampin co-administration.

Interventionnanogram (ng)*hr/mL (Mean)
Ixabepilone3015.45
Ixabepilone + Rifampin1478.31

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Swollen 76 Joint Count (SJC)

Comparison of modified Swollen Joint Counts between combination antibiotic and placebo groups at Baseline, Month 1, 3, 6 and 9. Determination of swelling in each of the 76 joints was determined by any swelling or absence of swelling. Each swollen joint receives a value of 1, ranging from 0-76 as a possible score. (NCT00351273)
Timeframe: Baseline, month 1,3,6 and 9

,
InterventionSwollen Joints (Mean)
BaselineMonth 1Month 3Month 6Month 9
Combination Antibiotic4.11.70.90.90.5
Placebo4.53.54.35.25.1

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Number of Patients With a Complete Response (Resolution of All Symptoms)

Patients who completed full 6 months of treatment that reported feeling complete resolution of symptoms at month 6 visit and had no worsening of condition at the month 9 follow up visit. (NCT00351273)
Timeframe: Months 6 and 9

InterventionParticipants (Count of Participants)
Azithromycin and Rifampin5
Doxycycline and Rifampin1
Received Placebo0

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78 Tender Joint Count (TJC)

Comparison of modified 78 Tender Joint Count (TJC) between combination antibiotic and placebo groups at Baseline, Month 1, 3, 6 and 9. Determination of tender joing in each of the 78 joints was determined by examination. Each tender joint receives a value of 1, ranging from 0-78 as a possible score. (NCT00351273)
Timeframe: Baseline, Month 1, 3, 6 and 9

,
InterventionTender Joints (Mean)
BaselineMonth 1Month 3Month 6Month 9
Combination Antibiotic7.45.03.32.01.9
Placebo9.610.610.811.810.9

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Erythrocyte Sedimentation Rate (ESR)

Comparison of mean ESR rates of combination antibiotic group vs placebo group at Baseline, Month 1, 3, 6 and 9 (NCT00351273)
Timeframe: Baseline Month 1, 3, 6 and 9

,
Interventionmillimeters/hour (Mean)
BaselineMonth 1Month 3Month 6Month 9
Combination Antibiotic25.117.817.712.714.0
Placebo18.925.219.817.018.4

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HAQ DI Score

"Comparison of HAQ-DI score of combination antibiotic group vs placebo group at Baseline, Month 1,3,6 and 9 The Health assessment questionnaire disability index (HAQ-DI) is a questionnaire for the assessment of Rheumatoid Arthritis. The questionnaire is a patient reported outcome (PRO) which is usually self-administered by the patient There are 8 sections: dressing, arising, eating, walking, hygiene, reach, grip, and activities. There are 2 or 3 questions for each section. Scoring within each section is from 0 (without any difficulty) to 3 (unable to do). For each section the score given to that section is the worst score within the section, i.e. if one question is scored 1 and another 2, then the score for the section is 2. In addition, if an aide or device is used or if help is required from another individual, then the minimum score for that section is 2. If the section score is already 2 or more then no modification is made.~The 8 scores of the 8 sections are summed and divided" (NCT00351273)
Timeframe: Baseline, Month 1,3,6 and 9

,
Interventionscore on a scale (Mean)
BaselineMonth 1Month 3Month 6Month 9
Combination Antibiotic0.840.790.680.710.57
Placebo1.10.920.870.990.92

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hsCRP

Comparison of high sensitivity C-reactive protein measurement in combination antibiotic group vs placebo group at Baseline, Month 1, 3, and 6 (NCT00351273)
Timeframe: Baseline, Month 1, 3, and 6

,
Interventionmg/litre (Mean)
BaselineMonth 1Month 3Month 6
Combination Antibiotic1.070.560.630.41
Placebo0.420.270.550.34

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PhGA Assessment

Comparison of Physician's global assessment of disease activity (PhGA) using 0-100mm visual analog scale (VAS) , where 0 indicates the best possible outcome and 100 indicates the worst possible outcome, in combination antibiotic vs placebo groups at Baseline, month 1,3,6 and 9 (NCT00351273)
Timeframe: Baseline, month 1,3,6 and 9

,
Interventionunits on a scale (Mean)
BaselineMonth 1Month 3Month 6Month 9
Combination Antibiotic63.935.223.216.317.7
Placebo60.252.949.445.743.8

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Investigate Whether a 6 Month Course of Combined Antibiotics Was Effective Treatment.

The outcome measure was a composite endpoint. Participants had to meet 4/6 clinical criteria. 17/24 subjects randomized to combination antibiotics did respond to treatment when compared to 3/10 randomized to placebo. (NCT00351273)
Timeframe: Month 6

Interventionparticipants (Number)
Azithromycin & Rifampin10
Doxycycline & Rifampin7
Placebo3

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Rifampin Cohort: Ctrough of Crizotinib Alone and When Taken With Rifampin

Ctrough refers to plasma concentration of Crizotinib observed just before treatment administration. (NCT00585195)
Timeframe: pre-dose on Cycle 1 Day 15 (Crizotinib alone arm) and Cycle 2 Day 1 (Crizotinib with Rifampin arm)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg Alone251.7
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg With Rifampin26.67

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Rifampin Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib Alone and When Taken With Rifampin

(NCT00585195)
Timeframe: pre-dose, 2, 4, 6, 8 and 10 hours on Cycle 1 Day 15 (Crizotinib alone) and Cycle 2 Day 1 (Crizotinib with Rifampin)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg Alone326.4
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg With Rifampin71.53

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 15 Day 1

Geometric mean of ratio (Cycle 15 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 15 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.491.031.320.900.811.710.240.76

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RP2D Cohort: Area Under the Curve From Time Zero to Last Quantifiable Concentration [AUC (0-24)] of Crizotinib When Taken With Food

AUC0-24 of Crizotinib was defined as the area under the free plasma concentration time curve from time 0 to 24 hours post-dose. (NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9, and 24 hours post-dose on Day -7

Interventionnanogram*hour per milliliter (Geometric Mean)
RP2D Cohort: Crizotinib 250 mg With Food1212.86

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RP2D Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken With Food

Cmax is defined as the observed maximum plasma concentration post drug administration. (NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9, and 24 hours post-dose on Day -7

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Crizotinib 250 mg With Food106.24

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at End of Treatment

Geometric mean of ratio (End of treatment/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, End of Treatment (28 days post last dose)

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.400.661.480.520.850.620.640.41

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 9 Day 1

Geometric mean of ratio (Cycle 9 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 9 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.380.561.190.720.831.230.190.72

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 6 Day 1

Geometric mean of ratio (Cycle 6 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 6 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.490.750.690.781.071.710.250.87

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 4 Day 1

Geometric mean of ratio (Cycle 4 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 4 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.480.660.840.750.881.630.220.81

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 30 Day 1

Geometric mean of ratio (Cycle 30 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 30 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.160.381.140.850.801.250.090.71

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 27 Day 1

Geometric mean of ratio (Cycle 27 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 27 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.460.971.480.700.661.860.240.95

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 24 Day 1

Geometric mean of ratio (Cycle 24 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 24 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.390.701.130.690.532.350.200.90

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 21 Day 1

Geometric mean of ratio (Cycle 21 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 21 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.230.481.460.530.771.230.150.72

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 2 Day 1

Geometric mean of ratio (Cycle 2 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 2 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.470.720.890.420.691.310.240.85

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 18 Day 1

Geometric mean of ratio (Cycle 18 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 18 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.320.551.640.690.891.100.180.69

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 12 Day 1

Geometric mean of ratio (Cycle 12 Day 1/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. 95% CI should be interpreted with cautions due to the limited sample size at this time point. (NCT00585195)
Timeframe: Baseline, Cycle 12 Day 1

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLH SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.380.661.060.881.021.390.230.75

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Geometric Mean of Ratio of Total Testosterone, Free Testosterone, Sex Hormone Binding Globulin (SHBG), Luteinizing Hormone, Follicle Stimulating Hormone, Dihydroepiandrosterone Sulfate, Estradiol and Prolactin Levels in Males at Cycle 1 Day 15

Geometric mean of ratio (Cycle1Day15/Baseline) of hypogonadism parameters (total testosterone, free testosterone, sex hormone binding globulin, luteinizing hormone, follicle stimulating hormone, dihydroepiandrosterone sulfate, estradiol and prolactin) levels in males was analyzed. Data for this outcome measure was planned to be collected for combined RP2D Cohort only, excluding arms of low and high dose escalation cohorts. (NCT00585195)
Timeframe: Baseline, Cycle 1 Day 15

InterventionRatio (Geometric Mean)
TestosteroneEstradiolProlactinLuteinizing Hormone (LH) SerumFollicle Stimulating HormoneFree TestosteroneSex Hormone Binding GlobulinDihydroepiandrosterone Sulfate
RP2D Cohort: Crizotinib 250 mg0.460.531.190.580.770.960.360.97

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Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib Alone and When Taken With Rifampin

Area under the plasma concentration versus time curve from time 0 to end of dosing interval (AUCtau). (NCT00585195)
Timeframe: pre-dose, 2, 4, 6, 8 and 10 hours on Cycle 1 Day 15 (Crizotinib alone arm) and Cycle 2 Day 1 (Crizotinib with Rifampin arm)

Interventionnanogram*hour per milliliter (Geometric Mean)
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg Alone3110
RP2D Cohort: Rifampin Interaction: Crizotinib 250 mg With Rifampin509.6

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Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUCinf) of Midazolam When Taken Alone or Taken With Crizotinib

AUCinf = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). (NCT00585195)
Timeframe: pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Day -7 (midazolam alone arm), pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Cycle 2 Day 1 (midazolam with crizotinib arm)

Interventionnanogram*hour per milliliter (Geometric Mean)
Low Dose Escalation Cohort: Crizotinib 100 mg QD (Midazolam Alone)41.77
Low Dose Escalation Cohort: Crizotinib 100 mg QD + Midazolam90.78
Low Dose Escalation Cohort: Crizotinib 300 mg BID (Midazolam Alone)37.71
Low Dose Escalation Cohort: Crizotinib 300 mg BID + Midazolam151.45
RP2D Cohort: Crizotinib 250 mg (Midazolam Alone)32.10
RP2D Cohort: Crizotinib 250 mg +Midazolam112.78

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Dose-Escalation Cohort: Maximum Tolerated Dose (MTD) of Crizotinib

MTD: Dose level at which at most 1 of 6 participants experienced DLT within and including 28 days of treatment (during Cycle 1 [1 cycle=28 days]) with next higher dose having at least 2/3 or 2/6 participants experiencing a DLT. DLT was defined as any of following: Hematologic toxicities- 1) prolonged grade 4 neutropenia for >7 days. 2) Febrile neutropenia: grade 4 neutropenia with fever greater than (>) 38.5 degree Celsius, both sustained over a 24 hour period (3) neutropenic infection: greater than or equal to (>=) Grade 3 neutropenia with Grade >=3 infection. (4) Grade >=3 thrombocytopenia with bleeding/grade 4 lasting >=7 days. Other non-hematologic toxicity included: Grade 3/4 toxicities (except for alopecia, Grade 3/4 hypophosphatemia, grade 3 hypertension with controlled blood pressure [less than (<) 140/90 millimeter of mercury, and Grade 3/4 hyperuricemia without signs and symptoms of gout). Nausea, vomiting/diarrhea must persist at grade 3/4 despite maximal medical therapy. (NCT00585195)
Timeframe: Cycle 1 (28 days)

Interventionmilligram (Number)
Low Dose Escalation Cohort: Crizotinib 50 mg QD250
Low Dose Escalation Cohort: Crizotinib 100 mg QD250
Low Dose Escalation Cohort: Crizotinib 200 mg QD250
Low Dose Escalation Cohort: Crizotinib 200 mg BID250
Low Dose Escalation Cohort: Crizotinib 250 mg BID250
Low Dose Escalation Cohort: Crizotinib 300 mg BID250
High Dose Escalation Cohort: Crizotinib 300 mg QD250
High Dose Escalation Cohort: Crizotinib 400 mg QD250
High Dose Escalation Cohort: Crizotinib 500 mg QD250
High Dose Escalation Cohort: Crizotinib 650 mg QD250
High Dose Escalation Cohort: Crizotinib 800 mg QD250

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Dose-Escalation Cohort: Number of Participants With Dose-limiting Toxicities (DLT)

Dose-limiting toxicity (DLT) was defined as any of the following: Hematologic- prolonged grade 4 neutropenia for >7 days. Febrile neutropenia, defined as grade 4 neutropenia with fever greater than (>)38.5 degree Celsius, both sustained over a 24 hour period, neutropenic infection: greater than or equal to (>=)Grade 3 neutropenia with Grade >=3 infection. Grade >=3 thrombocytopenia with bleeding or grade 4 lasting >=7 days Lymphopenia was not considered a DLT unless accompanied by infection. Other non-hematologic toxicity: Grade 3 or 4 toxicities (except for alopecia, Grade 3/4 hypophosphatemia, grade 3 hypertension with controlled blood pressure [less than (<) 140/90], and Grade 3/4 hyperuricemia without signs and symptoms of gout). Nausea, vomiting or diarrhea must persist at grade 3 or 4 despite maximal medical therapy. (NCT00585195)
Timeframe: Cycle 1 (28 days)

InterventionParticipants (Count of Participants)
Low Dose Escalation Cohort: Crizotinib 50 mg QD0
Low Dose Escalation Cohort: Crizotinib 100 mg QD0
Low Dose Escalation Cohort: Crizotinib 200 mg QD1
Low Dose Escalation Cohort: Crizotinib 200 mg BID0
Low Dose Escalation Cohort: Crizotinib 250 mg BID0
Low Dose Escalation Cohort: Crizotinib 300 mg BID2
High Dose Escalation Cohort: Crizotinib 300 mg QD0
High Dose Escalation Cohort: Crizotinib 400 mg QD0
High Dose Escalation Cohort: Crizotinib 500 mg QD0
High Dose Escalation Cohort: Crizotinib 650 mg QD0
High Dose Escalation Cohort: Crizotinib 800 mg QD0

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Itraconazole Cohort: Area Under the Curve From Time Zero to End of Dosing Interval (AUCtau) of Crizotinib When Taken Alone and When Taken With Itraconazole

Area under the plasma concentration versus time curve from time 0 to end of dosing interval (AUCtau), where dosing interval is 24 hours. (NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9 and 24 hours post dose on Cycle 1 Day 15 (Crizotinib with itraconazole) and Cycle 2 Day 1 (itraconazole alone)

Interventionnanogram*hour per milliliter (Geometric Mean)
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg Alone4102
Itraconazole Interaction Cohort: Crizotinib 250 mg + Itraconazole6665

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Itraconazole Cohort: Maximum Observed Plasma Concentration (Cmax) of Crizotinib When Taken Alone and When Taken With Itraconazole

(NCT00585195)
Timeframe: pre-dose, 1, 2, 4, 6, 8, 9 and 24 hours post dose on Cycle 1 Day 15 (Crizotinib with itraconazole) and Cycle 2 Day 1 (itraconazole alone)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg Alone259.9
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg With Itraconazole353.2

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Itraconazole Cohort: Trough Plasma Concentration (Ctrough) of Crizotinib When Taken Alone and When Taken With Itraconazole

Ctrough refers to plasma concentration of Crizotinib observed just before treatment administration. (NCT00585195)
Timeframe: pre-dose on Cycle 1 Day 15 (crizotinib with itraconazole) and Cycle 2 Day 1 (itraconazole alone)

Interventionnanogram per milliliter (Geometric Mean)
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg Alone136.0
RP2D Cohort: Itraconazole Interaction: Crizotinib 250 mg With Itraconazole214.0

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Midazolam Interaction Cohort: Maximum Observed Plasma Concentration (Cmax) of Midazolam When Taken Alone or Taken With Crizotinib

Cmax is defined as the observed maximum plasma concentration post drug administration. (NCT00585195)
Timeframe: pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Day -7 (midazolam alone arm), pre-dose, 0.5, 1, 2, 4, 6, 8, 9, and 24 hours post dose on Cycle 2 Day 1 (midazolam with crizotinib arm)

Interventionnanogram per milliliter (Geometric Mean)
Low Dose Escalation Cohort: Crizotinib 100 mg QD (Midazolam Alone)14.98
Low Dose Escalation Cohort: Crizotinib 100 mg QD + Midazolam19.26
Low Dose Escalation Cohort: Crizotinib 300 mg BID (Midazolam Alone)13.65
Low Dose Escalation Cohort: Crizotinib 300 mg BID + Midazolam32.62
RP2D Cohort: Crizotinib 250 mg (Midazolam Alone)12.78
RP2D Cohort: Crizotinib 250 mg + Midazolam25.37

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Probability of Participant Survival at Month 12

Probability of survival was defined as the probability of being alive at Month 12. (NCT00585195)
Timeframe: Month 12

Interventionprobability of participants survival (Number)
RP2D Cohort: ROS1-Positive NSCLC: Crizotinib 250 mg78.8
RP2D Cohort: MET Exon 14 Alterations NSCLC: Crizotinib 250 mg66.0
RP2D Cohort: MET Amplification NSCLC: Crizotinib 250 mg37.1
RP2D Cohort: ALK-Positive Cohort, NSCLC: Crizotinib 250 mg80.5

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Probability of Participant Survival at Month 6

Probability of survival was defined as the probability of being alive at Month 6. (NCT00585195)
Timeframe: Month 6

InterventionProbability of participants survival (Number)
RP2D Cohort: ROS1-Positive NSCLC: Crizotinib 250 mg90.5
RP2D Cohort: MET Exon 14 Alterations NSCLC: Crizotinib 250 mg86.7
RP2D Cohort: MET Amplification NSCLC: Crizotinib 250 mg67.8
RP2D Cohort: ALK-Positive Cohort, NSCLC: Crizotinib 250 mg90.0

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Area Under the Plasma Concentration-time Curve (AUC) 0-72 Hours

(NCT00608907)
Timeframe: Cycle 3 day 14 (72 hours post last dose)

Interventionng*h/mL (Mean)
VELCADE + Rifampicin123
VELCADE + Dexamethasone170
VELCADE215

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Midazolam Clearance (Pharmacokinetic Measure of Cytochrome P450 3A4 Activity)

(NCT00621309)
Timeframe: 7 days

,,
Interventionng*min/ml (Mean)
MDZ AUC Day 1MDZ AUC Day 8
Broccoli Sprout Extract Alone541558
Broccoli Sprout Extract Plus Rifampin552135
Rifampicin Alone604156

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To Compare, by Treatment Group, the Percentage of Patients With a Negative Sputum Culture at the End of Intensive Phase Therapy.

LJ culture conversion (NCT00728507)
Timeframe: Week 8

Interventionpercentage of participants (Number)
HPZM78.3
HRZE84.3

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Maximum Plasma Concentration (Cmax) of S-warfarin and R-warfarin

Blood collection 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, and 120 hours after warfarin dosing. (NCT00777855)
Timeframe: 0-120 hours after warfarin dosing

,
Interventionng/ml (Mean)
Cmax of S-warfarinCmax of R-warfarin
Warfarin329375
Warfarin Plus Rifampin303351

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Area Under the Plasma Concentration-time Curve From Time Zero to Infinity of S-warfarin and R-warfarin

Analysis of all concentration-time data. Blood collection 1, 2, 4, 6, 8, 12, 24, 48, 72, 96, and 120 hours after warfarin dosing. (NCT00777855)
Timeframe: 0-120 hours after warfarin dosing

,
Interventionng/ml*h (Mean)
AUC(0-infinity) of S-warfarinAUC(0-infinity) of R-warfarin
Warfarin8,42018,600
Warfarin Plus Rifampin7,41014,100

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S- and R- Enantiomers of Warfarin (S-warfarin and R-warfarin) Area Under the Plasma Concentration-time Curve (AUC) From 0 to 12 Hours.

Uptake effects on warfarin pharmacokinetics during time period of hepatic organic anion-transporting polypeptide (OATP) inhibition by rifampin. Blood collection 1, 2, 4, 6, 8, and 12 hours after warfarin dosing. (NCT00777855)
Timeframe: 0-12 hours after warfarin dosing

,
Interventionng/ml*h (Mean)
AUC (0-12 hours) of S-warfarinAUC (0-12 hours) of R-warfarin
Warfarin2,2502,850
Warfarin Plus Rifampin2,2302,930

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Time to Stable Culture Conversion on Solid Medium

Time to stable culture conversion (in days) on Lowenstein Jensen solid medium (NCT00814671)
Timeframe: 12 weeks

Interventiondays (Median)
RPT45037
RIF 60043
RPT 60036

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Pharmacokinetics of Rifapentine

area under the concentration time curve (AUC[0-24]) for rifapentine administered once daily at doses of 450 mg or 600 mg in the context of multi drug intensive phase TB treatment (NCT00814671)
Timeframe: 8 weeks

Interventionug x h/ml (Median)
Rifapentine 450 mg330
Rifapentine 600 mg435

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Percentage of Participants With Negative Lowenstein Jensen Cultures at Week 8

(NCT00814671)
Timeframe: 8 weeks

Interventionpercentage of participants w/LJ cx con (Number)
RPT45085
RIF 60094
RPT 60096

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Tolerability

percentage of participants discontinuing assigned treatment (NCT00814671)
Timeframe: 10 weeks

Interventionpercentage of participants (Number)
RPT4502.0
RIF 6008.3
RPT 6002.0

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Time to Stable Culture Conversion on Liquid MGIT Media

Time (in days) to stable culture conversion on liquid MGIT media (NCT00814671)
Timeframe: 12 weeks

Interventiondays (Median)
RPT45050
RIF 60059
RPT 60057

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Combined Failure of Bacteriological Cure and Relapse Within One Year of Completion of Therapy as Defined by Culture Using Solid Media (Lowenstein-Jensen - LJ).

The primary efficacy outcome was the proportion of patients who had bacteriologically or clinically defined failure or relapse within 18 months after randomization (a composite unfavorable outcome). Culture-negative status was defined as two negative-culture results at different visits without an intervening positive result. The date of culture-negative status was defined as the date of the first negative-culture result. This status continued until there were two positive cultures, without an intervening negative culture, or until there was a single positive culture that was not followed by two negative cultures. Relapse strains were those shown to be identical on 24-locus Mycobacterial interspersed repetitive units (MIRU) analysis. For the final 18 month study visit when both L-J samples were contaminated or missing, if the subject could not be brought back, liquid medium culture results were used in place of solid medium culture results. (NCT00864383)
Timeframe: 18 months (within one year of completion of therapy)

Interventionparticipants with failure or relapse (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)43
Regimen 2 - 2MHRZ/2MHR78
Regimen 3 - 2EMRZ/2MR105

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Combined Failure of Bacteriological Cure and Relapse as Defined by Culture Using Liquid Media (Mycobacteria Growth Indicator Tube-MGIT).

The secondary analysis of efficacy outcome was the proportion of patients who had bacteriologically or clinically defined failure or relapse within 18 months after randomization (a composite unfavorable outcome) based on MGIT. Culture-negative status was defined as two negative-culture results at different visits without an intervening positive result. The date of culture-negative status was defined as the date of the first negative-culture result. This status continued until there were two positive cultures, without an intervening negative culture, or until there was a single positive culture that was not followed by two negative cultures. Relapse strains were those shown to be identical on 24-locus Mycobacterial interspersed repetitive units (MIRU) analysis. (NCT00864383)
Timeframe: 18 months (within one year of completion of therapy)

Interventionparticipants with failure or relapse (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)65
Regimen 2 - 2MHRZ/2MHR98
Regimen 3 - 2EMRZ/2MR131

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Sensitivity Analyses Assuming All Losses to Follow-up and Non-tuberculous Deaths Have a Favourable Outcome Using Solid (L-J) Media.

"Sensitivity Analysis of Primary Efficacy Results of All Randomized Subjects Imputing Favorable for Missing Outcomes. Analysis is the number of subjects with an unfavorable outcome. Favorable outcome is defined as the number of subjects with a negative TB culture status at 18 months (at or after 72 weeks), who had not already been classified as having an unfavorable outcome, and whose last positive TB culture result (isolated positive culture) was followed by at least two negative culture results." (NCT00864383)
Timeframe: 18 months

Interventionparticipants with unfavorable outcome (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)87
Regimen 2 - 2MHRZ/2MHR132
Regimen 3 - 2EMRZ/2MR132

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Time to First Culture Negative Sputum Sample (MGIT Liquid Media)

(NCT00864383)
Timeframe: 18 months

InterventionTime to culture negative status / weeks (Median)
Regimen 1 - 2EHRZ/4HR (Control Regimen)11.9
Regimen 2 - 2MHRZ/2MHR8.0
Regimen 3 - 2EMRZ/2MR8.0

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Time to First Culture Negative Sputum Sample (LJ Solid Media)

Culture negative for TB using LJ cultures. (NCT00864383)
Timeframe: 18 months

InterventionTime to culture negative status / weeks (Median)
Regimen 1 - 2EHRZ/4HR (Control Regimen)6.0
Regimen 2 - 2MHRZ/2MHR6.0
Regimen 3 - 2EMRZ/2MR6.0

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Sensitivity Analysis Assuming All Losses to Follow-up and Non-tuberculous Deaths Have an Unfavorable Outcome Using Solid (L-J) Media.

"Sensitivity Analysis of Primary Efficacy Results of All Randomized Subjects Imputing Unfavorable for Missing Outcomes. Analysis is the number of subjects with an unfavorable outcome. Favorable outcome is defined as the number of subjects with a negative TB culture status at 18 months (at or after 72 weeks), who had not already been classified as having an unfavorable outcome, and whose last positive TB culture result (isolated positive culture) was followed by at least two negative culture results." (NCT00864383)
Timeframe: 18 months

Interventionparticipants with unfavorable outcome (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)172
Regimen 2 - 2MHRZ/2MHR219
Regimen 3 - 2EMRZ/2MR217

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Number of Patients With Grade 3 or 4 Adverse Events (Using a Modified Division of Acquired Immunodeficiency Syndrome National Institute of Allergy and Infectious Diseases [DAIDS] Scale of Adverse Event Reporting)

The number of participants includes all patients who had at least one grade 3 or 4 adverse event. (NCT00864383)
Timeframe: 18 months (within one year of completion of therapy)

Interventionparticipants with Grade 3 or 4 AEs (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)123
Regimen 2 - 2MHRZ/2MHR127
Regimen 3 - 2EMRZ/2MR111

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Number of Patients Who Are Culture Negative (Solid LJ Culture)

Number of patients who are TB LJ culture negative at 8 weeks. (NCT00864383)
Timeframe: 8 weeks

Interventionparticipants who are culture negative (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)352
Regimen 2 - 2MHRZ/2MHR394
Regimen 3 - 2EMRZ/2MR401

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Number of Patients Who Are Culture Negative (Liquid MGIT Culture)

Number of patients who are TB MGIT culture negative at 8 weeks. (NCT00864383)
Timeframe: 8 weeks

Interventionparticipants who are culture negative (Number)
Regimen 1 - 2EHRZ/4HR (Control Regimen)235
Regimen 2 - 2MHRZ/2MHR274
Regimen 3 - 2EMRZ/2MR260

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Change in Lesion Size at the Completion of Antibiotic Therapy, Measured on a Continuous Scale; Change Will be Determined by Change in Diameter of the Lesions

(NCT01074554)
Timeframe: Baseline to 8 weeks

Interventionmm (Median)
Antibiotic Regimen-8.4
Placebo Regimen0.07

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Change in Modified Sarcoidosis Activity and Severity Index (SASI) at Completion of Therapy.

Characterization of lesion severity was conducted using Modified Sarcoidosis Activity and Severity Index (SASI), measuring erythema, induration and desquamation. The modification was that the same scale was applied to any part of the body, instead of the face alone. The scale range is 0 (no problem) to 72 (very severe). (NCT01074554)
Timeframe: Baseline to 8 weeks

Interventionunits on a scale (Mean)
Antibiotic Regimen-2.9
Placebo Regimen-0.6

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Granuloma Burden

Number of patients with a decrease in Granuloma Burden (only in those patients having granulomas present at baseline biopsy) (NCT01074554)
Timeframe: Baseline to 8 weeks

Interventionparticipants (Number)
Antibiotic Regimen7
Placebo Regimen0

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for Crizotinib Metabolite (PF-06260182)

Area under the plasma concentration time-curve from zero (pre-dose) to the last measured concentration (AUClast) of crizotinib metabolite (PF-06260182). (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionng*hr/mL (Geometric Mean)
Crizotinib 250 mg369.50
Crizotinib 250 mg + Rifampin 600 mg20.28

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Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] for Crizotinib Metabolite (PF-06260182)

AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞) of crizotinib metabolite (PF-06260182). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionng*hr/mL (Geometric Mean)
Crizotinib 250 mg378.60
Crizotinib 250 mg + Rifampin 600 mg21.78

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast)

Area under the plasma concentration time-curve from zero (pre-dose) to the last measured concentration (AUClast). (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionng*hr/mL (Geometric Mean)
Crizotinib 250 mg2103.00
Crizotinib 250 mg + Rifampin 600 mg368.60

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Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)]

AUC (0 - ∞) = Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hours (hrs) post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionng*hr/mL (Geometric Mean)
Crizotinib 250 mg2192.00
Crizotinib 250 mg + Rifampin 600 mg397.20

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Apparent Volume of Distribution (Vz/F)

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired blood concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction absorbed. (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

InterventionL (Geometric Mean)
Crizotinib 250 mg5940.0
Crizotinib 250 mg + Rifampin 600 mg45720.0

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Apparent Oral Clearance (CL/F)

Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the body. Clearance obtained after oral dose CL/F is influenced by the fraction of the dose absorbed. (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

InterventionL/hr (Geometric Mean)
Crizotinib 250 mg118.80
Crizotinib 250 mg + Rifampin 600 mg648.60

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Time to Reach Maximum Observed Plasma Concentration (Tmax)

(NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionhr (Median)
Crizotinib 250 mg5.0
Crizotinib 250 mg + Rifampin 600 mg3.0

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Time to Reach Maximum Observed Plasma Concentration (Tmax) for Crizotinib Metabolite (PF-06260182)

(NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionhr (Median)
Crizotinib 250 mg5.0
Crizotinib 250 mg + Rifampin 600 mg5.0

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Plasma Decay Half-Life (t1/2)

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionhr (Mean)
Crizotinib 250 mg33.07
Crizotinib 250 mg + Rifampin 600 mg48.23

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Metabolite to Parent Ratio Area Under the Curve From Time Zero to Last Quantifiable Concentration (MRAUClast)

Molar ratio of metabolite to parent area under the plasma concentration time-curve from zero (pre-dose) to the last measured concentration (MRAUClast). (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

InterventionRatio (Geometric Mean)
Crizotinib 250 mg0.1703
Crizotinib 250 mg + Rifampin 600 mg0.0533

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Metabolite to Parent Ratio Maximum Observed Plasma Concentration (MRCmax)

Metabolite to parent molar ratio of maximum observed plasma concentration (MRCmax). (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

InterventionRatio (Geometric Mean)
Crizotinib 250 mg0.2839
Crizotinib 250 mg + Rifampin 600 mg0.0996

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Maximum Observed Plasma Concentration (Cmax) for Crizotinib Metabolite (PF-06260182)

(NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionng/mL (Geometric Mean)
Crizotinib 250 mg29.88
Crizotinib 250 mg + Rifampin 600 mg3.29

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Maximum Observed Plasma Concentration (Cmax)

(NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

Interventionng/mL (Geometric Mean)
Crizotinib 250 mg102.10
Crizotinib 250 mg + Rifampin 600 mg32.06

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Metabolite to Parent Ratio Area Under the Curve From Time Zero to Extrapolated Infinite Time [MRAUC (0 - ∞)]

Molar ratio of metabolite to parent area under the curve from time zero to extrapolated infinite time [MRAUC (0-∞)]. (NCT01147055)
Timeframe: 0 (pre-dose), 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 1 and Day 0, 0 (pre-dose) , 1, 2, 4, 5, 6, 8, 10, 12, 24, 36, 48, 72, 96 and 144 hrs post crizotinib dose in period 2

InterventionRatio (Geometric Mean)
Crizotinib 250 mg0.1676
Crizotinib 250 mg + Rifampin 600 mg0.0532

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Pharmacokinetics (AUC of RPT Over 24 Hours Post-dose)

To determine and compare the steady-state pharmacokinetics and dose linearity of escalating daily doses of rifapentine in dose cohorts of 5 mg/kg, 10 mg/kg, 15 mg/kg and 20 mg/kg in healthy volunteers after a single dose (Day 2) or multiple doses (Day 15) (NCT01162486)
Timeframe: days: 2, 15

,,,
Intervention(mcg*h/ml) (Median)
RPT AUC, Day 2 single doseRPT AUC, Day 15 multiple dose
RPT 1128218
RPT 2242330
RPT 3363560
RPT 4403483

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Midazolam, AUC Over 12 Hours Post-dose

To compare and describe, the pharmacokinetics of single-dose midazolam alone (Day 1) versus midazolam co-administered with either steady-state rifapentine at multiple daily doses (5, 10, 15, and 20 mg/kg) or rifampin at 10 mg/kg daily (Day 15) (NCT01162486)
Timeframe: days: 1, 15

,,,,
Interventionng*h/ml (Median)
AUC 0-12 Midazolam alone (Day 1)AUC 0-12 Midazolam with RIF (Day 15)
Rifampin Control15126.9
RPT 115014.2
RPT 211410.2
RPT 320414.0
RPT 417311.7

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Number of Participants With Grade 2 or Higher Adverse Events Over the Course of the 26 Day Trial

Number of Participants with Grade 2 or higher adverse events over 26 days (NCT01162486)
Timeframe: 26 days

InterventionParticipants (Count of Participants)
Rifampin Control1
RPT 10
RPT 21
RPT 31
RPT 40

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Change in Absolute FVC From Baseline to Post Completion of 8 Weeks of Antibiotic Therapy.

The primary endpoint was improvement in absolute FVC from baseline to completion of therapy. Spirometry testing was performed using a standardized calibrated laptop spirometer, Flowscreen II USA Spirometer (VIASYS Healthcare Inc., Yorba Linda, CA). The volume accuracy of the spirometer was checked daily using a three liter calibration syringe. Each subject was given at least three attempts and the greatest measurement for absolute FVC and Forced Expiratory Volume (FEV1) at baseline, four week, and eight week assessments was recorded. (NCT01169038)
Timeframe: 8 weeks

Interventionliters (Mean)
Antibiotics2.61

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Change From Baseline to 12 Months in UMSARS Part II

UMSARS is a scale measuring disease progression that comprises 4 parts; only Parts I and II were used in this study. Part I scores symptoms of neurological and autonomic dysfunction. Part II is a motor examination. Part II has 14 items with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Therefore the total score for Part II could range from 0 (normal) to 56 (extreme dysfunction). (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale (Mean)
Rifampicin7.0
Placebo5.4

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Change From Baseline to 12 Months in Total UMSARS (i.e., UMSARS Part I Minus Question 11 + UMSARS Part II)

UMSARS is a scale measuring disease progression that comprises 4 parts; only Parts I and II were used in this study. Part I scores symptoms of neurological and autonomic dysfunction. Part II is a motor examination. Part I has 12 questions with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Part II has 14 items with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Therefore the total score for total UMSARS Parts I minus Question 11 + Part II could range from 0 (normal) to 104 (extreme dysfunction). (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale (Mean)
Rifampicin12.9
Placebo10.8

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Change From Baseline to 12 Months in UMSARS Part I Score (Minus Question 11)

UMSARS is a scale measuring disease progression that comprises 4 parts, only Parts I and II were used in this study. Part I scores symptoms of neurological and autonomic dysfunction. Part II is a motor examination. Part I has 12 questions with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Therefore the total score for Part I could range from 0 (normal) to 48 (extreme dysfunction). (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale (Mean)
Rifampicin6.2
Placebo5.6

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Change in the COMPASS-Select-Change Scale From Baseline to 12 Months

"The change in COMPASS is a derivative of COMPASS and evaluates the change in symptoms over time on selected domains of symptoms as a function of natural history or intervention therapy. The focus is on 7 selected domains. The version of the COMPASS-Change -Select Scale used (06-09-2009 Ver. 1) has 16 questions, with multiple parts, scores ranging from much worse to no such symptoms. The score could range from 0 (no such symptoms) to 94 (much worse)." (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale (Mean)
Rifampicin41.4
Placebo32.1

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Rate of Change From Baseline to 12 Months in the Total Unified Multiple System Atrophy Rating Scale (UMSARS) Part I Score (Minus Question 11)

"UMSARS is a scale measuring disease progression that comprises 4 parts; only Parts I and II were used in this study. Part I scores symptoms of neurological and autonomic dysfunction. Part II is a motor examination. Part I has 12 questions with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Therefore the total score for Part I could range from 0 (normal) to 48 (extreme dysfunction).~Participant-specific rate of change in points per month was estimated using slope estimate from least square regression where for each participant, their UMSARS I scores were plotted over time measured in months." (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale per month (Mean)
Rifampicin0.5
Placebo0.5

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Rate of Change From Baseline to 12 Months in Total UMSARS (i.e., UMSARS Part I Minus Question 11 + UMSARS Part II) Using Slope Estimate

"UMSARS is a scale measuring disease progression that comprises 4 parts; only Parts I and II were used in this study. Part I scores symptoms of neurological and autonomic dysfunction. Part II is a motor examination. Part I has 12 questions with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Part II has 14 items with a rating scale ranging from 0 (normal) to 4 (extreme dysfunction). Therefore the total score for total UMSARS Parts I minus Question 11 + Part II could range from 0 (normal) to 104 (extreme dysfunction).~Participant-specific rate of change in points per month was estimated using slope estimate from least square regression where for each participant, their total UMSARS scores were plotted over time measured in months." (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale per month (Mean)
Rifampicin1.1
Placebo1.2

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Change From Baseline to 12 Months in the COMPASS-Select Scale

"The composite autonomic symptoms score (COMPASS) provides a score of autonomic symptom severity with appropriate weighting. In the COMPASS_select, symptoms are confined to 6 select domains of symptoms. The version of the COMPASS-Select used (06-09-2009 v1) has 46 questions, with multiple parts, scores ranging from much worse to no such symptoms. Scores could range from 0 (no such symptoms) to 85 (much worse)." (NCT01287221)
Timeframe: baseline, 12 months

Interventionunits on a scale (Mean)
Rifampicin6.9
Placebo4.6

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Maximum Observed Plasma Concentration (Cmax)

(NCT01311505)
Timeframe: 0 (pre-dose), 1, 2, 3, 4, 6, 8 and 10 hrs post-dose

Interventionmcg/mL (Geometric Mean)
Myrin 27.89
Rimactane8.02

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Extrapolated Area Under the Curve (AUC Percent [%] Extrapolated)

AUC%extrapolated is the extrapolated area under the plasma concentration time profile following the last measured concentration. It is calculated as (AUC [0-∞] minus AUC[0-10])*100/ AUC (0-∞), where AUC (0-∞) = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time (0-∞) and AUC(0-10) = area under the plasma concentration time-curve from zero (pre-dose) to the last quantifiable concentration. (NCT01311505)
Timeframe: 0 (pre-dose), 1, 2, 3, 4, 6, 8 and 10 hrs post-dose

InterventionPercent AUC (Geometric Mean)
Myrin 218.84
Rimactane17.53

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Number of Participants With Abnormal Safety Laboratory Test Values

Participants were evaluated for following safety laboratory tests: Hematology, chemistry, urinalysis. (NCT01311505)
Timeframe: Screening and Follow-up (1 week post-baseline)

,
Interventionparticipants (Number)
ScreeningFollow-up
Myrin 200
Rimactane00

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Number of Participants With Adverse Events (AEs)

Any untoward medical occurrence in a participant who received study treatment was considered an AE without regard to possibility of causal relationship. (NCT01311505)
Timeframe: Baseline (Day 0), Day 1 and Follow-up (1 week post-baseline)

,
Interventionparticipants (Number)
Day 0Day 1Follow-up
Myrin 2000
Rimactane000

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC [0-t])

AUC (0-t)= Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t) (NCT01311505)
Timeframe: 0 (pre-dose), 1, 2, 3, 4, 6, 8 and 10 hours (hrs) post-dose

Interventionmicrogram*hour/milliliter (mcg*h/mL) (Geometric Mean)
Myrin 238.59
Rimactane38.81

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Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC [0-∞])

AUC (0-∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-∞). It is obtained from AUC (0-t) plus AUC (t-∞). (NCT01311505)
Timeframe: 0 (pre-dose), 1, 2, 3, 4, 6, 8 and 10 hrs post-dose

Interventionmcg*hr/mL (Geometric Mean)
Myrin 247.72
Rimactane47.15

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Time to Reach Maximum Observed Plasma Concentration (Tmax)

(NCT01311505)
Timeframe: 0 (pre-dose), 1, 2, 3, 4, 6, 8 and 10 hrs post-dose

Interventionhrs (Median)
Myrin 22.0
Rimactane1.0

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Plasma Decay Half-life (t1/2)

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. (NCT01311505)
Timeframe: 0 (pre-dose), 1, 2, 3, 4, 6, 8 and 10 hrs post-dose

Interventionhrs (Mean)
Myrin 24.0750
Rimactane3.8635

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Time to Maximum Observed Plasma Concentration (Tmax)

Time to maximum observed plasma concentration (Tmax) was obtained directly from the observed concentration versus time data. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionhours (Median)
Romidepsin Day 13.0
Romidepsin and Rifampin Day 83.00

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Summary of Participants With Treatment Emergent Adverse Events (TEAEs)

AEs were considered related if assessed by the Investigator as possibly, probably or definitely related to study drug. Serious AEs (SAEs) are those that resulted in death, were life-threatening, required or prolonged inpatient hospitalization, resulted in persistent or significant disability/incapacity, congenital anomaly, or resulted in an important medical event that may have jeopardized the patient or required medical or surgical intervention to prevent one of the outcomes listed above. (NCT01324323)
Timeframe: Day 1 up to Day 36 (28 days after the last treatment)

Interventionparticipants (Number)
= > 1 TEAE= > 1 TEAE related to any study drug= > 1 TEAE related to Romidepsin= > 1 TEAE related to Rifampin= > 1 Serious TEAE= > 1 Serious TEAE related to any drug= > 1 Serious TEAE related to Romidepsin= > 1 Serious TEAE related to Rifampin= > 1 TEAE leading to discontinuation= > 1 TEAE related discontinuation to any drug= > 1 Romidepsin related TEAE discontinuation= > 1 Rifampin related TEAE discontinuationParticipants who died
Romidepsin Plus Rifampin1313132211100000

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Maximum Observed Plasma Concentration (Cmax)of Romidepsin

Maximum observed plasma concentration (Cmax)was obtained directly from the observed concentration versus time data. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng/mL (Geometric Mean)
Romidepsin Day 1571.2
Romidepsin and Rifampin Day 8900.1

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Apparent Total Volume of Distribution (Vz).

Apparent total volume of distribution (Vz) was calculated as [(CL)/λz] for Romidepsin and co-administered with Rifampin. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

InterventionLiters (Geometric Mean)
Romidepsin Day 1161.48
Romidepsin and Rifampin Day 877.6

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Area Under the Plasma Concentration Time-curve From Time 0 to 24-hour (AUC0-24) for Romidepsin

Individual and mean romidepsin plasma concentrations by treatment and scheduled time data were collected. AUC0-24: area under the plasma concentration time-curve from Time 0 to 24 hours, calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing. (NCT01324323)
Timeframe: Day 1 and Day 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 12204.2
Romidepsin and Rifampin Day 83903.9

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Area Under the Plasma Concentration Time-curve From Time 0 to the Time of the Last Quantifiable Concentration (AUC0-t)of Romidepsin

AUC0-t: area under the plasma concentration time-curve from Time 0 to the time of the last quantifiable concentration (Ct), calculated by linear trapezoidal method when concentrations are increasing and the logarithmic trapezoidal method when concentrations are decreasing. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (pre-dose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 12225.1
Romidepsin and Rifampin Day 83966.3

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Area Under the Plasma Concentration Time-curve From Time Zero Extrapolated to Infinity (AUC0-∞).

AUC0-∞: area under the plasma concentration time-curve from Time 0 extrapolated to infinity, calculated as [AUCt + Ct/λz]. λz is the apparent terminal rate constant. No AUC extrapolation was performed with unreliable λz. If the percentage of AUC extrapolated is ≥ 25%, AUC0-∞ will not be reported. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionng*hr/mL (Geometric Mean)
Romidepsin Day 12229.8
Romidepsin and Rifampin Day 83980.7

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Estimate of the Terminal Elimination Half-life in Plasma (t1/2)

The terminal elimination half-life (t1/2) in plasma, was calculated as [(ln 2)/λz]. This was only calculated when a reliable estimate for λz could be obtained. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

Interventionhours (Geometric Mean)
Romidepsin Day 19.666
Romidepsin and Rifampin Day 88.341

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Clearance (CL): Apparent Total Plasma Clearance.

The apparent total plasma clearance (CL) was calculated as [Dose/AUC0-∞] for Romidepsin alone and co-administered with rifampin plasma concentrations. (NCT01324323)
Timeframe: Days 1 and 8; at 0 (predose), 1, 2, 3, and 4 hours (end of infusion) and at 4.25, 4.5, 5, 6, 8, 10, 12, 24 and 48 hours after the initiation of IV infusion.

InterventionL/hr (Geometric Mean)
Romidepsin Day 111.59
Romidepsin and Rifampin Day 86.45

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Antibiotic Use (Proportion of Subjects)

Proportion of subjects treated with oral, inhaled, and IV antibiotics over the 6 month study. (NCT01349192)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Treatment17
Observation13

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Antibiotic Use (Days of Use Per Subject)

Days of use of oral, inhaled, and IV antibiotics over the 6 month study. (NCT01349192)
Timeframe: 6 months

Interventiondays (Mean)
Treatment21.9
Observational31.3

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MRSA Culture Status

Proportion of subjects with a negative culture for MRSA at Day 28. (NCT01349192)
Timeframe: Day 28

InterventionParticipants (Count of Participants)
Treatment18
Observation5

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Pulmonary Exacerbations

Proportion of subjects with a protocol-defined pulmonary exacerbation (PE) between baseline and day 28 who are treated with antibiotics active against MRSA. (NCT01349192)
Timeframe: 28 days

InterventionParticipants (Count of Participants)
Treatment2
Observation6

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Cumulative Probability of First AIDS Progression by Week 96

The Kaplan-Meier estimate of the cumulative probability of first AIDS progression which was defined as the identification of a new World Health Organization (WHO) stage 3 or 4 condition (NCT01380080)
Timeframe: From study entry to week 96

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric16.6
Arm B: IPT11.3

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Proportion of Participants Who Prematurely Discontinued Antiretroviral Therapy by Week 48

Proportion of participants with premature discontinuation of antiretroviral therapy (ART) by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.19
Arm B: IPT0.21

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Proportion of Participants Who Prematurely Discontinued Any Component of TB Treatment by Week 48

Proportion of participants with premature discontinuation of any component of TB treatment by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.13
Arm B: IPT0.05

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Proportion of Participants With at Least One New Grade 3 or 4 Adverse Event That is at Least a One-grade Increase From Baseline by Week 48

Proportion of participants with at least one new Grade 3 or 4 laboratory or sign or symptom that is at least a one-grade increase from baseline by Week 48. Grade 3=Severe, Grade 4=Life-Threatening according to DAIDS AE Grading Table (see references). (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.32
Arm B: IPT0.30

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Proportion of Participants With at Least One New Grade 3 or 4 Targeted Laboratory Value That is at Least a One-grade Increase From Baseline by Week 48

"Proportion of participants with at least one new Grade 3 or 4 that is at least a one-grade increase from baseline for the following targeted laboratory values by Week 48~The targeted laboratory events include hemoglobin, serum creatinine, ALT and AST" (NCT01380080)
Timeframe: From study entry to week 48. The lab events were collected at study entry, weeks 2, 4, 8, 12, 16, 20, 24, and 48.

InterventionProportion of participants (Number)
Arm A: Empiric0.11
Arm B: IPT0.13

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Proportion of Participants With Reportable Hospitalization by Week 48

Proportion of participants with reportable hospitalization reported by Week 48 (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.10
Arm B: IPT0.12

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Proportion of Participants With TB Diagnosis by Week 96

Proportion of participants with TB diagnosis per current ACTG Diagnosis Appendix 60 by week 96 (NCT01380080)
Timeframe: From study entry to week 96

InterventionProportion of participants (Number)
Arm A: Empiric0.08
Arm B: IPT0.05

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Time to Initiation of TB Treatment by Week 96

Median time to TB treatment initiation since study entry (NCT01380080)
Timeframe: From study entry to week 96

InterventionDays (Median)
Arm A: Empiric0
Arm B: IPT0

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CD4+ T-cell Count

The absolute levels of CD4+ T-cell counts (cells/mm^3) (NCT01380080)
Timeframe: At weeks 0, 4, 24, and 48

,
Interventioncells/ mm^3 (Median)
Week 0Week 4Week 24Week 48
Arm A: Empiric1874121176
Arm B: IPT1976121172

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CD4+ T-cell Count Change From Baseline

Change was calculated as the CD4+ T-cell count at the later weeks (4, 24 and 48) minus the baseline (week 0) CD4+ T-cell count. (NCT01380080)
Timeframe: Weeks 0, 4, 24 and 48

,
Interventioncells/ mm^3 (Median)
Week 4Week 24Week 48
Arm A: Empiric4996158
Arm B: IPT54102146

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Proportion of Participants With HIV-1 RNA Level <400 Copies/mL

Proportion of participants with HIV-1 RNA level <400 copies/mL. (NCT01380080)
Timeframe: At weeks 0, 4, 24, and 48

,
InterventionProportion of participants (Number)
Week 0Week 4Week 24Week 48
Arm A: Empiric00.460.840.87
Arm B: IPT0.010.490.850.89

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Proportion of Participants With Immune Reconstitution Inflammatory Syndrome (IRIS) by Week 48

Proportion of participants with IRIS (using current ACTG definition Appendix 60, see References) by Week 48. IRIS in participants with TB and other opportunistic infections may occur shortly after the initiation of potent combination ART, particularly in participants with advanced HIV disease. (NCT01380080)
Timeframe: From study entry to week 48

InterventionProportion of participants (Number)
Arm A: Empiric0.04
Arm B: IPT0.05

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Cumulative Probability of Death by Week 24

The Kaplan-Meier estimate of cumulative probability of death by week 24 (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric4.8
Arm B: IPT5.2

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Cumulative Probability of Death or AIDS Progression by Week 24

The Kaplan-Meier estimate of the cumulative probability of death or AIDS progression by week 24. AIDS progression was defined as new WHO stage 3 or 4 conditions occurred after study entry. (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric17.1
Arm B: IPT12.5

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Cumulative Probability of Death or AIDS Progression by Week 48

The Kaplan-Meier estimate of the cumulative probability of death or AIDS progression by week 48. AIDS progression was defined as new WHO stage 3 or 4 conditions occurred after study entry. (NCT01380080)
Timeframe: From study entry to week 48

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric19.3
Arm B: IPT15.3

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Cumulative Probability of Death or Unknown Vital Status by Week 24

"The Kaplan-Meier estimate of the cumulative probability of death or unknown vital status by week 24.~The vital status was considered unknown at week 24 if a participant prematurely discontinued from the study before week 24 and no vital status was obtained at week 48." (NCT01380080)
Timeframe: From study entry to week 24

InterventionCumulative probability per 100 persons (Number)
Arm A: Empiric5.2
Arm B: IPT5.2

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Area Under Curve From 0 to Infinity Hours (AUC0-∞)

AUC0-∞ represents the area under the concentration-time curve of the analyte in plasma over the time interval from 0 extrapolated to infinity. (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionng*h/mL (Geometric Mean)
Afatinib912
Afatinib + Rifa610

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Area Under Curve From 0 to 24 h (AUC0-24)

AUC0-24 represents the area under the concentration-time curve of the analyte in plasma over the time interval from 0 to 24 hours (h) (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionng*h/mL (Geometric Mean)
Afatinib491
Afatinib + Rifa353

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Apparent Volume of Distribution During the Terminal Phase lambda_z Following an Extravascular Dose (V_z/F)

V_z/F represents the apparent volume of distribution during the terminal phase λz following an extravascular dose (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

InterventionLitres (Geometric Mean)
Afatinib2080
Afatinib + Rifa3410

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Area Under Curve From 0 to tz (AUC0-tz)

AUC0-tz represents the area under the concentration-time curve of the analyte in plasma over the time interval from 0 to the last quantifiable drug plasma concentration. (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionng*h/mL (Geometric Mean)
Afatinib860
Afatinib + Rifa575

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Apparent Clearance of Afatinib in the Plasma After Extravascular Administration (CL/F)

CL/F represents the apparent clearance of the analyte in the plasma after extravascular administration (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

InterventionmL/min (Geometric Mean)
Afatinib731
Afatinib + Rifa1090

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Maximum Concentration (Cmax)

Cmax represents the maximum concentration of the analyte in plasma. (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionng/mL (Geometric Mean)
Afatinib38.3
Afatinib + Rifa30.0

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Mean Residence Time of Afatinib in the Body After Oral Administration (MRTpo)

MRTpo represents the mean residence time of the analyte in the body after oral administration (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionhours (Geometric Mean)
Afatinib36.9
Afatinib + Rifa35.1

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Percentage of the AUCtz-∞ Obtained by Extrapolation (%AUCtz-∞)

%AUCtz-∞ represents the percentage of the AUCtz-∞ obtained by extrapolation (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionpercentage of AUCtz-∞ (Geometric Mean)
Afatinib5.25
Afatinib + Rifa5.48

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Terminal Half-life of Afatinib in Plasma (t1/2)

t1/2 represents the terminal half-life of the analyte in plasma (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionhours (Geometric Mean)
Afatinib32.8
Afatinib + Rifa36.0

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Time From Dosing to the Maximum Concentration of Afatinib in Plasma (Tmax)

tmax represents the time from dosing to the maximum concentration of the analyte in plasma (NCT01396265)
Timeframe: 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, 24, 36, 48, 72, 96, 120 hours post dose

Interventionhours (Median)
Afatinib6.00
Afatinib + Rifa6.00

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Steady State Pharmacokinetic Exposure of RIF

The endpoint is the (dimensionless) ratio of AUC0-6 mcg/ml*h to MIC99.9 mcg/ml (NCT01408914)
Timeframe: At any time during the intensive phase of treatment, after steady state has been reached (at a minimum, after 14 days of daily RIF delivery)

InterventionRatio (Median)
10 mg/kg115.6988
15 mg/kg201.9725
20 mg/kg284.4278

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Sputum Culture Sterilization During the Initial 8 Weeks of Treatment

Number of participants that are sputum culture (in LJ) negative for TB at 8 weeks (NCT01408914)
Timeframe: Until 8 weeks of treatment are completed

InterventionParticipants (Count of Participants)
10 mg/kg46
15 mg/kg44
20 mg/kg45

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Warfarin Clearance.

Warfarin enantiomer (S-warfarin and R-warfarin) clearance was measured in healthy volunteers genotyped for CYP2C9*1/*1, CYP2C9*1B/*1B, CYP2C9*1/*3, CYP2C9*2/*3 and CYP2C9*3/*3 to determine the magnitude of the warfarin-fluconazole (inhibition) and warfarin-rifampin (induction) drug interactions. (NCT01447511)
Timeframe: Over three (two for CYP2C9*1B/*1B participants) 12-16 day study periods.

,,,,
InterventionmL/h (Mean)
S warfarin - Control PeriodR warfarin - Control PeriodS warfarin - Fluconazole PeriodR warfarin - Fluconazole PeriodS warfarin - Rifampin PeriodR warfarin - Rifampin Period
CYP2C9*1/*1 Genotype2821368966520342
CYP2C9*1/*3 Genotype1801226868347339
CYP2C9*1B/*1B Haplotype246124NANA486307
CYP2C9*2/*3 Genotype84953555195368
CYP2C9*3/*3 Genotype711533672157406

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Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Ixazomib

(NCT01454076)
Timeframe: Arm 1:Days 1, 15 and Arm 5:Day 6 pre-dose and at multiple time points(up to 264 hrs)post-dose;Arm 2, 3:Days 1,15 pre-dose and at multiple time points(up to 216 hrs)post-dose;Arm 4:Day 8 pre-dose and at multiple time points(up to 168 hrs)post-dose

Interventionhours (Median)
Arm 1: Ixazomib 2.5 mg1.090
Arm 1: Ixazomib 2.5 mg + Ketoconazole 400 mg1.500
Arm 2: Ixazomib 4 mg Capsule A1.290
Arm 2: Ixazomib 4 mg Capsule B1.250
Arm 3: Ixazomib 4 mg Fasted1.020
Arm 3: Ixazomib 4 mg Fed4.000
Arm 4: Ixazomib 4 mg + Rifampin 600 mg1.450
Arm 5: Ixazomib 2.5 mg + Clarithromycin 500 mg1

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Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

(NCT01454076)
Timeframe: Cycle 1 Day 1 up to 30 days after last dose of study drug (Arm 1 and 5: Cycle 19 Day 45; Arm 2: Cycle 7 Day 45; Arm 3: Cycle 22 Day 45; Arm 4: Cycle 25 Day 45)

,,,,
Interventionparticipants (Number)
TEAEsSAEs
Arm 1: Ixazomib 2.5 mg + Ketoconazole 400 mg2912
Arm 2: Ixazomib 4 mg Capsule A or B205
Arm 3: Ixazomib 4 mg Fasted or Fed2412
Arm 4: Ixazomib 4 mg + Rifampin 600 mg183
Arm 5: Ixazomib 2.5 mg + Clarithromycin 500 mg2110

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Cmax: Maximum Observed Plasma Concentration for Ixazomib

(NCT01454076)
Timeframe: Arm 1:Days 1, 15 and Arm 5:Day 6 pre-dose and at multiple time points(up to 264 hours[hrs])post-dose;Arm 2, 3:Days 1,15 pre-dose and at multiple time points(up to 216 hrs)post-dose;Arm 4:Day 8 pre-dose and at multiple time points(up to 168 hrs)post-dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Arm 1: Ixazomib 2.5 mg38.975
Arm 1: Ixazomib 2.5 mg + Ketoconazole 400 mg39.250
Arm 2: Ixazomib 4 mg Capsule A61.866
Arm 2: Ixazomib 4 mg Capsule B71.949
Arm 3: Ixazomib 4 mg Fasted77.001
Arm 3: Ixazomib 4 mg Fed22.752
Arm 4: Ixazomib 4 mg + Rifampin 600 mg25.706
Arm 5: Ixazomib 2.5 mg + Clarithromycin 500 mg37.245

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Percentage of Participants With Best Overall Response

Best overall response for a participant is best observed post-baseline disease response as per Response Evaluation Criteria in Solid Tumors (RECIST) 1.1: Complete response (CR) was defined as complete disappearance of all target lesions and non-target disease, with the exception of nodal disease. All nodes, both target and non-target, must decrease to normal (short axis less than (<) 10 millimeter [mm]). No new lesions. Partial response (PR) was defined as greater than or equal to (>=) 30% decrease under baseline of the sum of diameters of all target lesions. The short axis was used in the sum for target nodes, while the longest diameter was used in the sum for all other target lesions. No unequivocal progression of non-target disease. No new lesions. Stable disease (SD) was defined as not qualifying for CR, PR, Progressive Disease (PD). An increase of >=20% from the nadir (or baseline, if it represents the point at which the sum of target disease was lowest) represents PD. (NCT01454076)
Timeframe: Baseline up to end of treatment (approximately 1.9 years)

,,,,
Interventionpercentage of participants (Number)
CRPRSDPD
Arm 1: Ixazomib 2.5 mg + Ketoconazole 400 mg006338
Arm 2: Ixazomib 4 mg Capsule A or B005050
Arm 3: Ixazomib 4 mg Fasted or Fed063559
Arm 4: Ixazomib 4 mg + Rifampin 600 mg005347
Arm 5: Ixazomib 2.5 mg + Clarithromycin 500 mg015347

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Number of Participants With Clinically Significant Vital Sign Abnormalities

(NCT01454076)
Timeframe: Cycle 1 Day 1 up to 30 days after last dose of study drug (Arm 1 and 5: Cycle 19 Day 45; Arm 2: Cycle 7 Day 45; Arm 3: Cycle 22 Day 45; Arm 4: Cycle 25 Day 45

Interventionparticipants (Number)
Arm 1: Ixazomib 2.5 mg + Ketoconazole 400 mg0
Arm 2: Ixazomib 4 mg Capsule A or B0
Arm 3: Ixazomib 4 mg Fasted or Fed0
Arm 4: Ixazomib 4 mg + Rifampin 600 mg0
Arm 5: Ixazomib 2.5 mg + Clarithromycin 500 mg0

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AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Ixazomib

(NCT01454076)
Timeframe: Arm 1:Days 1, 15 and Arm 5:Day 6 pre-dose and at multiple time points(up to 264 hrs)post-dose;Arm 2, 3:Days 1,15 pre-dose and at multiple time points(up to 216 hrs)post-dose;Arm 4:Day 8 pre-dose and at multiple time points(up to 168 hrs)post-dose

Interventionnanogram*hour per milliliter (ng*hr/mL)] (Geometric Mean)
Arm 1: Ixazomib 2.5 mg551.985
Arm 1: Ixazomib 2.5 mg + Ketoconazole 400 mg1148.778
Arm 2: Ixazomib 4 mg Capsule A1284.079
Arm 2: Ixazomib 4 mg Capsule B1334.659
Arm 3: Ixazomib 4 mg Fasted1465.979
Arm 3: Ixazomib 4 mg Fed998.698
Arm 4: Ixazomib 4 mg + Rifampin 600 mg231.527
Arm 5: Ixazomib 2.5 mg + Clarithromycin 500 mg613.112

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Estimate of the Terminal Elimination Half-life (T1/2) of Apremilast in Plasma

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

Interventionhours (Geometric Mean)
Apremilast Alone8.12
Apremilast + IV Rifampin7.35
Apremilast + Multiple Dose Oral Rifampin6.13

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Area Under the Plasma Concentration-time Curve From Time Zero to the Last Quantifiable Concentration (AUCt) of Apremilast

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

Interventionng*h/mL (Geometric Mean)
Apremilast Alone3070
Apremilast + IV Rifampin2940
Apremilast + Multiple Dose Oral Rifampin850

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Area Under the Plasma Concentration-time Curve From Time Zero Extrapolated to Infinity (AUC∞) of Apremilast

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

Interventionng*h/mL (Geometric Mean)
Apremilast Alone3120
Apremilast + IV Rifampin2980
Apremilast + Multiple Dose Oral Rifampin869

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Apparent Volume of Distribution (Vz/F) of Apremilast

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

Interventionliters (Geometric Mean)
Apremilast Alone112
Apremilast + IV Rifampin107
Apremilast + Multiple Dose Oral Rifampin305

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Time to Maximum Observed Plasma Concentration (Tmax) of Apremilast

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

Interventionhours (Median)
Apremilast Alone2.00
Apremilast + IV Rifampin1.50
Apremilast + Multiple Dose Oral Rifampin1.00

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Maximum Observed Plasma Concentration (Cmax) of Apremilast

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

Interventionng/mL (Geometric Mean)
Apremilast Alone290
Apremilast + IV Rifampin331
Apremilast + Multiple Dose Oral Rifampin166

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Apparent Total Plasma Clearance (CL/F) of Apremilast

Plasma concentrations of apremilast were determined by means of a validated, sensitive, and specific high performance liquid chromatography/tandem mass spectrometric (LC-MS/MS) assay. (NCT01561963)
Timeframe: Pre-dose and at 0.5, 1, 1.5, 2, 3, 5, 8, 12, 16, 24, 36, and 48 hours following apremilast dosing on Days 1, 5, and 20

InterventionL/h (Geometric Mean)
Apremilast Alone9.60
Apremilast + IV Rifampin10.1
Apremilast + Multiple Dose Oral Rifampin34.5

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Pyrazinamide PK Parameter CL/F

Pyrazinamide PK parameter CL/F obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
InterventionL/hour (Median)
PZA CL/F Day 1PZA CL/F Day 14
RHZE-RHZE4.14.5
RHZE-RMZE4.74.7
RHZE-RZE4.85.4
RZE-RZE4.24.7

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Pyrazinamide PK Parameter CLast

Pyrazinamide PK parameter CLast obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
PZA CLast at Day 1PZA CLast at Day 14
RHZE-RHZE33701955.0
RHZE-RMZE31301790
RHZE-RZE28501280
RZE-RZE27101770

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Pyrazinamide PK Parameter Cmax

Pyrazinamide PK parameter Cmax obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
PZA Cmax at Day 1PZA Cmax at Day 14
RHZE-RHZE2765029300
RHZE-RMZE2880029300
RHZE-RZE2700027000
RZE-RZE2580028000

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Rifampicin PK Parameter Clearance (CL/F)

Rifampicin PK parameter Clearance (CL/F) obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
InterventionL/hour (Median)
RIF CL/F Day 1RIF CL/F Day 14
RHZE-RHZE14.018.0
RHZE-RMZE10.521.5
RHZE-RZE12.522.1
RZE-RZE14.317.0

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Rifampicin PK Parameter Last Concentration (CLast)

Rifampicin (RIF) PK parameter Last Concentration (CLast) obtained Day 1 and Day 14. The lower limit of quantification of the assay (LLOQ) for RIF was 40 ng/mL. The results below the lower limit of quantification were assigned as one-half the value of the LLOQ, which was 20 ng/mL. (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
RIF CLast at Day 1RIF CLast at Day 14
RHZE-RHZE74.520
RHZE-RMZE13320
RHZE-RZE2020
RZE-RZE2020

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Ethambutol PK Parameter Cmax

Ethambutol PK parameter Cmax obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
EMB Cmax at Day 1EMB Cmax at Day 14
RHZE-RHZE26502980
RHZE-RMZE24702780
RHZE-RZE20403090
RZE-RZE22202920

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Moxifloxacin PK Parameter Cmax at Day 14

Moxifloxacin PK parameter Cmax obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

Interventionng/mL (Median)
RHZE-RMZE3010

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Rifampicin PK Parameter Maximum Plasma Concentration (Cmax)

Rifampicin PK parameter Parameter Maximum Plasma Concentration (Cmax) obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
RIF Cmax at Day 1RIF Cmax at Day 14
RHZE-RHZE55657145
RHZE-RMZE86607370
RHZE-RZE60606960
RZE-RZE48808350

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AUC0-24hour for Isoniazid (INH) at Day 1

PK AUCs of Isoniazid (INH) from 0 to 24 hours obtained at Day 1 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

Interventionh*ng/mL (Median)
RHZE-RHZE10725.8
RHZE-RZE7970.6
RHZE-RMZE7165.1

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AUC0-24hour for Isoniazid at Day 14

PK AUCs of Isoniazid from 0 to 24 hours obtained at Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

Interventionh*ng/mL (Median)
RHZE-RHZE9797.2

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AUC0-24hour for Moxifloxacin (Mox) at Day 14

PK AUCs of Moxiflozacin (Mox) from 0 to 24 hours obtained at Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

Interventionh*ng/mL (Median)
RHZE-RMZE22498.4

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Correlation Between Time to Positivity (TTP) and log10 Transformed Colony-forming Unit (CFU) Counts Per mL

Pearson correlation coefficient was used to examine the correlation between TTP and log10 CFU among all qualified samples obtained on study (NCT01589497)
Timeframe: Pre-entry, Day 0, Day 1, Day 2, Day 3, Day 5, Day 7, Day 9, Day 11 and Day 14

Interventioncorrelation coefficient (Number)
Overall-0.75

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Daily Change in log10 Colony-forming Unit (CFU) Counts Per mL Sputum From Day 2 to Day 14

"The daily change in log10 CFU/mL sputum was calculated as follows:~EBA2-14(CFU) = (log10 CFU/mL at day 2 - log10 CFU/mL at day 14)/12.~For a CFU/mL count of 0, the log10 CFU/mL was set to 0." (NCT01589497)
Timeframe: Day 2 and day 14

Interventionlog10 CFU/ mL (Median)
RHZE-RHZE0.143
RHZE-RZE0.093
RHZE-RMZE0.123
RZE-RZE0.104

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Daily Change in log10 Transformed Colony-forming Unit (CFU) Counts Per mL Sputum From Baseline (Study Treatment Initiation) to Day 2

"The daily change in log10 CFU/mL sputum was calculated as follows:~EBA0-2(CFU) = (baseline log10 CFU/mL sputum (mean of log10 CFU/mL at pre-entry and day 0) - log10 CFU/mL at day 2)/2.~For a CFU/mL count of 0, the log10 CFU/mL was set to 0." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 2

Interventionlog10 CFU/ mL (Median)
RHZE-RHZE0.255
RHZE-RZE0.385
RHZE-RMZE0.111
RZE-RZE0.034

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Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 14

"The daily change in TTP was calculated as follows:~EBA0-14(TTP) = [baseline TTP (mean of TTP at pre-entry and day 0) - TTP at day 14]/14." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 14

Interventionhours (Median)
RHZE-RHZE-12
RHZE-RZE-12
RHZE-RMZE-13
RZE-RZE-11

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Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 2

"The daily change in TTP was calculated as follows:~EBA0-2(TTP) = (baseline TTP (mean of TTP at pre-entry and day 0) - TTP at day 2)/2." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 2

Interventionhours (Median)
RHZE-RHZE-31
RHZE-RZE-30
RHZE-RMZE-29
RZE-RZE-25

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Daily Change in Time to Positivity (TTP) From Day 2 to Day 14

"The daily change in TTP was calculated as follows:~EBA2-14(TTP) = (TTP at day 2 - TTP at day 14)/12." (NCT01589497)
Timeframe: Day 2 and Day 14

Interventionhours (Median)
RHZE-RHZE-9
RHZE-RZE-9
RHZE-RMZE-12
RZE-RZE-9

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Daily Decrease in log10 Transformed Colony-forming Unit (CFU) Counts Per ml Sputum From Baseline (Study Treatment Initiation) to Day 14

"The daily decrease was calculated as follows:~EBA0-14(CFU)= [baseline log10 CFU/mL sputum (mean of log10 CFU/mL at pre-entry and day 0) - log10 CFU/mL at day 14]/14. For a CFU/ml count of 0, the log10 CFU/mL was set to 0.~No formal statistical testing was conducted to compare the arms. Please refer to the explanation in the Protocol Section." (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 14

Interventionlog10 CFU/ mL (Median)
RHZE-RHZE0.134
RHZE-RZE0.096
RHZE-RMZE0.136
RZE-RZE0.119

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Isoniazid PK Parameter CL/F at Day 1

Isoniazid PK parameter CL/F obtained Day 1 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

InterventionL/hour (Median)
RHZE-RHZE28.0
RHZE-RZE37.6
RHZE-RMZE41.9

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Isoniazid PK Parameter CL/F at Day 14

Isoniazid PK parameter CL/F obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

InterventionL/hour (Median)
RHZE-RHZE30.6

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Isoniazid PK Parameter CLast at Day 1

Isoniazid (INH) PK parameter CLast obtained Day 1. The lower limit of quantification of the assay (LLOQ) for INH was 100 ng/mL. The results below the lower limit of quantification were assigned as one-half the value of the LLOQ, which was 50 ng/mL. (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

Interventionng/mL (Median)
RHZE-RHZE50
RHZE-RZE50
RHZE-RMZE50

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Isoniazid PK Parameter CLast at Day 14

Isoniazid (INH) PK parameter CLast obtained Day 14. The lower limit of quantification of the assay (LLOQ) for INH was 100 ng/mL. The results below the lower limit of quantification were assigned as one-half the value of the LLOQ, which was 50 ng/mL. (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

Interventionng/mL (Median)
RHZE-RHZE50

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Isoniazid PK Parameter Cmax at Day 1

Isoniazid PK parameter Cmax obtained Day 1 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 1

Interventionng/mL (Median)
RHZE-RHZE3165
RHZE-RZE2920
RHZE-RMZE2760

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Isoniazid PK Parameter Cmax at Day 14

Isoniazid PK parameter Cmax obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Isoniazid dosing at Day 14

Interventionng/mL (Median)
RHZE-RHZE3130

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Moxifloxacin PK Parameter CL/F at Day 14

Moxifloxacin PK parameter CL/F obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

InterventionL/hour (Median)
RHZE-RMZE17.8

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Moxifloxacin PK Parameter CLast at Day 14

Moxifloxacin PK parameter CLast obtained Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Moxifloxacin dosing at Day 14

Interventionng/mL (Median)
RHZE-RMZE178

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AUC0-24hour for Ethambutol (EMB)

PK AUCs of Ethambutol (EMB) from 0 to 24 hours obtained at Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
Interventionh*ng/mL (Median)
EMB AUC0-24hour at Day 1EMB AUC0-24hour at Day 14
RHZE-RHZE11918.816414.9
RHZE-RMZE11322.415181.2
RHZE-RZE11145.816675.9
RZE-RZE10716.816574.6

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AUC0-24hour for Pyrazinamide (PZA)

PK AUCs of Pyrazinamide (PZA) from 0 to 24 hours obtained at Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Pyrazinamide dosing at Day 1 and Day 14

,,,
Interventionh*ng/mL (Median)
PZA AUC0-24hour at Day 1PZA AUC0-24hour at Day 14
RHZE-RHZE301214.5249879.1
RHZE-RMZE292078.2280071.0
RHZE-RZE255283.0201389.7
RZE-RZE272853.9252276.8

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Ethambutol PK Parameter CL/F

Ethambutol PK parameter CL/F obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
InterventionL/hour (Median)
EMB CL/F Day 1EMB CL/F Day 14
RHZE-RHZE93.657.9
RHZE-RMZE83.856.8
RHZE-RZE85.463.5
RZE-RZE76.560.1

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Ethambutol PK Parameter CLast

Ethambutol PK parameter CLast obtained Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Ethambutol dosing at Day 1 and Day 14

,,,
Interventionng/mL (Median)
EMB CLast at Day 1EMB CLast at Day 14
RHZE-RHZE86.5205.0
RHZE-RMZE40164
RHZE-RZE85176
RZE-RZE86159

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Log10 Transformed Colony-forming Unit (CFU) Count Per mL From Sputum Samples at Baseline and Day 14

The log10 CFU count per mL from sputum samples processed by standard method or decontaminated method. (NCT01589497)
Timeframe: Pre-entry, Day 0 and Day 14

,
Interventionlog10 CFU/ mL (Median)
Pre-entryDay 0Day 14
Decontaminated Processing Method5.895.583.74
Standard Processing Method5.805.684.01

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Pharmacokinetic Parameter (PK) Area Under the Concentration-time Curve (AUC0-24hour) for Rifampicin (RIF)

Pharmacokinetic Parameter Area Under the Concentration-time Curve (AUCs) of Rifampicin from 0 to 24 hours obtained at Day 1 and Day 14 (NCT01589497)
Timeframe: -0.5 hour (pre-dose), 1, 2, 3, 5, 7, 10, 12 and 24 hours after Rifampicin dosing at Day 1 and Day 14

,,,
Interventionh*ng/mL (Median)
RIF AUC0-24hour at Day 1RIF AUC0-24hour at Day 14
RHZE-RHZE37358.831361.4
RHZE-RMZE51434.126751.2
RHZE-RZE42062.627161.7
RZE-RZE39294.030521.0

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Change in Patient Reported Quality of Life (CFQ-R)(Respiratory)

Change in Patient Reported Quality of Life (CFQ-R)(respiratory) from baseline to Days 29 and 58. CFQ-R stands for Cystic Fibrosis Quality of Life Measure, Respiratory Domain. Overall range of absolute score 0 to +80. Higher score means better quality of life. Positive change in score means improvement in quality of life. Minimally clinically significant difference: +/- 4.0 units. (NCT01594827)
Timeframe: Days 29 and 58

,
Interventionunits on a scale (Mean)
Day 29Day 58
Inhaled Placebo (Sterile Water) and Oral Antibiotics11.53.2
Inhaled Vancomycin and Oral Antibiotics3.3-4.4

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Change if FEV1% Predicted From Screening

Change in FEV1% predicted from Screening at Days 29, 58, and 118 in treatment vs. standard care group (NCT01594827)
Timeframe: Days 29, 58, and 118

,
InterventionFEV1% predicted (Mean)
Day 29Day 58Day 118
Inhaled Placebo (Sterile Water) and Oral Antibiotics1.11.3-0.3
Inhaled Vancomycin and Oral Antibiotics0.0-3.0-2.1

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Time to First CF Exacerbation

Time to First CF Exacerbation using a standardized exacerbation definition from Day 1 to Day 118 (NCT01594827)
Timeframe: Day 1 to Day 118

InterventionDays (Mean)
Inhaled Vancomycin and Oral AntibioticsNA
Inhaled Placebo (Sterile Water) and Oral Antibiotics68.4

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Time to First Anti-MRSA Antibiotics (After Treatment Period)

Time between completion of Study Drug and need for anti-MRSA antibiotics to control or treat symptoms (NCT01594827)
Timeframe: Completion of Study Drug to Day 118

Interventiondays (Mean)
Inhaled Vancomycin and Oral AntibioticsNA
Inhaled Placebo (Sterile Water) and Oral Antibiotics58

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Percentage of Patients MRSA Free by Induced Sputum Respiratory Tract Culture

Percentage of patients MRSA free by induced sputum respiratory tract culture one day after completion of four-week eradication protocol (Day 29) in intervention arm vs standard treatment arm (NCT01594827)
Timeframe: Day 29

InterventionParticipants (Count of Participants)
Inhaled Vancomycin and Oral Antibiotics5
Inhaled Placebo (Sterile Water) and Oral Antibiotics6

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Development of Antibiotic Resistance

Number of patients with newly developed MRSA resistance to vancomycin, TMP/SMX, doxycycline, or rifampin. (NCT01594827)
Timeframe: Day 58 (Visit 5)

InterventionParticipants (Count of Participants)
Inhaled Vancomycin and Oral Antibiotics3
Inhaled Placebo (Sterile Water) and Oral Antibiotics3

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Number of Patients MRSA Free by Induced Sputum Respiratory Tract Culture

The hypothesis for our primary outcome is that the aggressive treatment arm will result in significantly greater eradication of persistent MRSA from the respiratory tract of CF adolescents and adults on day 58 (1 month after completion of therapy) compared to the placebo/standard treatment arm. Our primary outcome will be comparing the proportion of CF patients in the treatment arm who have a negative induced sputum MRSA culture at Day 58 to the proportion of patients in the placebo arm who have a negative induced sputum MRSA culture at Day 58. (NCT01594827)
Timeframe: Day 58 (Visit 5), approximately 1 month after completion of the MRSA treatment protocol

InterventionParticipants (Count of Participants)
Inhaled Vancomycin and Oral Antibiotics2
Inhaled Placebo (Sterile Water) and Oral Antibiotics3

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Total Number of Pulmonary Exacerbations

Total Number of Pulmonary Exacerbations using a standardized exacerbation definition at Days 58 and Days 118 in treatment vs. standard care group (NCT01594827)
Timeframe: Days 58 and 118

,
InterventionExacerbations (Number)
Day 58Day 118
Inhaled Placebo (Sterile Water) and Oral Antibiotics13
Inhaled Vancomycin and Oral Antibiotics00

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Change in Forced Expiratory Volume (FEV1)% Predicted From Baseline to Day 58

Change in Forced Expiratory Volume (FEV1)% predicted from baseline to day number 58 (NCT01594827)
Timeframe: Baseline, Day 58

Intervention% predicted FEV1 (Median)
Inhaled Vancomycin and Oral Antibiotics-2.5
Inhaled Placebo (Sterile Water) and Oral Antibiotics1.0

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Number of Participants Reporting a Grade 3 or 4 Sign or Symptom

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) sign or symptom were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF5
C: Standard-Dose LPV/r + RAL w/RBT5

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Number of Participants Who Experienced MTB IRIS

The number of participants who experienced MTB immune reconstitution inflammatory syndrome (IRIS) was summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT1
B: Double-dose LPV/r w/RIF2
C: Standard-Dose LPV/r + RAL w/RBT3

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Percent of Participants Who Died

The percent of participants who died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF4.7
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced a New AIDS-defining Illness

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Percent of Participants Who Experienced a New AIDS-defining Illness or Died

New post-randomization diagnoses were considered AIDS-defining based on the CDC classification system. The percent of participants who experienced a new AIDS-defining illness or died was calculated with an associated standard error. Confidence intervals were calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT4.2
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced HIV Virologic Failure

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. Participants who were missing data due to being lost-to-follow-up or dead were coded as virologic failures. The percent of participants who experienced HIV virologic failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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Percent of Participants Who Experienced Sputum Conversion at Week 8.

Sputum conversion was defined as culture MTB-negative at week 8 or AFB smear negative at week 8 (and culture contaminated or missing at week 8); there were no Xpert MTB/RIF results at week 8. The percent of participants experienced sputum conversion at week 8 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 8 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT87.5
B: Double-dose LPV/r w/RIF81.8
C: Standard-Dose LPV/r + RAL w/RBT70.0

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Percent of Participants Who Experienced TB Relapse/Recurrence

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The percent of participants who experienced TB relapse/recurrence was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF4.2
C: Standard-Dose LPV/r + RAL w/RBT4.3

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Percent of Participants Who Experienced TB Relapse/Recurrence and Who Had TB Drug Resistance

TB relapse/recurrence was defined as having had 2 consecutive MTB-negative cultures and subsequently had clinical or radiographic deterioration consistent with active TB at or after week 24 and before week 72. The drug resistance was determined based on phenotypic methods. The percent of participants who experienced TB relapse/recurrence and who had TB drug resistance was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At or after 24 weeks and through week 72

Interventionparticipants (Number)
B: Double-dose LPV/r w/RIF0
C: Standard-Dose LPV/r + RAL w/RBT0

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Percent of Participants Who Experienced TB Treatment Failure

TB treatment failure was defined as having a MTB-positive culture after 16 weeks of TB treatment for a participant who was documented to be taking TB medications. The percent of participants who experienced TB treatment failure was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After 16 weeks and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT0.0
B: Double-dose LPV/r w/RIF0.0
C: Standard-Dose LPV/r + RAL w/RBT0.0

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Percent of Participants Who Interrupted or Discontinued at Least One HIV Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one HIV drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF16.7
C: Standard-Dose LPV/r + RAL w/RBT21.7

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Percent of Participants Who Interrupted or Discontinued at Least One TB Drug Due to Toxicity

The percent of participants who interrupted or discontinued at least one TB drug due to toxicity was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through to the discontinuation of the last TB drug

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT20.8
B: Double-dose LPV/r w/RIF8.3
C: Standard-Dose LPV/r + RAL w/RBT13.0

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Percent of Participants Whose HIV Viral Load Was Less Than 400 Copies/mL at Week 48.

The percent of participants whose HIV viral load was less than 400 copies/mL at week 48 was calculated with an associated standard error. The confidence interval was calculated using Wilson's score method. Participants who were lost-to-follow-up or dead by week 48 or had missing results at week 48 were coded as having HIV viral load greater than 400 copies/mL. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT58.3
B: Double-dose LPV/r w/RIF66.7
C: Standard-Dose LPV/r + RAL w/RBT60.9

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Percent of Participants Whose HIV Viral Load Was Less Than 50 Copies/mL at Week 48

The percent of participants whose HIV viral load was less than 50 copies/mL at week 48 was calculated with an associated standard error. Participants who were lost-to-follow-up or dead by week 48 or had missing RNA at week 48 were coded as having HIV viral load greater than 50 copies/mL. The confidence interval was calculated using Wilson's score method. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: 48 weeks

Interventionpercentage of participants (Number)
A: Standard-dose LPV/r w/RBT45.8
B: Double-dose LPV/r w/RIF54.2
C: Standard-Dose LPV/r + RAL w/RBT56.5

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RAL AUC in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
C: Standard-Dose LPV/r + RAL w/RBT11338

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RBT AUC in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (area under the curve [AUC] between 0 and 24 hours) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT7374
C: Standard-Dose LPV/r + RAL w/RBT5516

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LPV Cmax and Cmin in Participants Enrolled in Arms A, B, and C

Describe LPV plasma pharmacokinetic (PK) characteristics (maximum concentration [Cmax] and minimum concentration [Cmin]) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

,,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT185319920
B: Double-dose LPV/r w/RIF181388033
C: Standard-Dose LPV/r + RAL w/RBT168028548

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RAL Cmax and Cmin in Participants Enrolled in Arm C

Describe RAL plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arm C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous RAL dose and was used as the 12-hour RAL concentration. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
C: Standard-Dose LPV/r + RAL w/RBT2830166

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RBT Cmax and Cmin in Participants Enrolled in Arms A and C

Describe RBT plasma PK characteristics (Cmax and Cmin) in participants enrolled in Arms A and C, determined by non-compartmental analysis of 24-hour PK sampling. The pre-dose concentration was determined using a sample drawn 24 hours after the previous RBT dose. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, 6, and 24 hours post-dose

,
Interventionng/mL (Median)
Maximum Concentration (Cmax)Minimum Concentration (Cmin)
A: Standard-dose LPV/r w/RBT461161
C: Standard-Dose LPV/r + RAL w/RBT349115

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Number of Participants Reporting a Grade 3 or 4 Laboratory Abnormality

The number of participants reporting a grade 3 (severe) or grade 4 (life-threatening) laboratory abnormality were summarized. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: After randomization and through week 72

InterventionParticipants (Count of Participants)
A: Standard-dose LPV/r w/RBT6
B: Double-dose LPV/r w/RIF3
C: Standard-Dose LPV/r + RAL w/RBT5

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CD4 Count Change From Baseline to Week 24

The difference in CD4 count from baseline to week 24 was calculated as the CD4 count at week 24 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 24 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT20
B: Double-dose LPV/r w/RIF56
C: Standard-Dose LPV/r + RAL w/RBT13

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CD4 Count Change From Baseline to Week 48

The difference in CD4 count from baseline to week 48 was calculated as the CD4 count at week 48 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 48 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT99
B: Double-dose LPV/r w/RIF119
C: Standard-Dose LPV/r + RAL w/RBT74

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CD4 Count Change From Baseline to Week 72

The difference in CD4 count from baseline to week 72 was calculated as the CD4 count at week 72 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 72 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT126
B: Double-dose LPV/r w/RIF212
C: Standard-Dose LPV/r + RAL w/RBT54

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CD4 Count Change From Baseline to Week 8

The difference in CD4 count from baseline to week 8 was calculated as the CD4 count at week 8 minus the CD4 count at baseline. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: Baseline and 8 weeks

Interventioncells/mm^3 (Median)
A: Standard-dose LPV/r w/RBT7
B: Double-dose LPV/r w/RIF26
C: Standard-Dose LPV/r + RAL w/RBT37

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Cumulative Probability of HIV Virologic Failure at Week 72

Virologic failure was defined as the occurrence of two consecutive plasma HIV-1 RNA levels ≥1000 copies/mL at or after 16 weeks and within 24 weeks of treatment initiation or ≥400 copies/mL at or after 24 weeks of treatment, regardless of whether randomized ART was being taken at the time of virologic failure. The percent of participants with HIV virologic failure at week 72 was calculated using a Kaplan-Meier estimator with an associated standard error. The confidence interval was calculated using a log-log transformation. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At weeks 16, 24, 48, and 72

Interventioncumulative events per 100 participants (Number)
A: Standard-dose LPV/r w/RBT29.2
B: Double-dose LPV/r w/RIF50.0
C: Standard-Dose LPV/r + RAL w/RBT30.4

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LPV AUC in Participants Enrolled in Arms A, B, and C

Describe LPV plasma PK characteristics (area under the curve [AUC] between 0 and 12 hours) in participants enrolled in Arms A, B, and C, determined by non-compartmental analysis of 12-hour PK sampling. The pre-dose concentration was determined using a sample drawn 12 hours after the previous LPV dose and was used as the 12-hour LPV concentration. As stated in the Detailed Study Description of the Protocol Section, formal statistical comparisons were not undertaken because of limited sample size. (NCT01601626)
Timeframe: At 2 weeks: pre-dose and at 2, 4, 5, and 6 hours post-dose

Interventionhours*ng/mL (Median)
A: Standard-dose LPV/r w/RBT159796
B: Double-dose LPV/r w/RIF161772
C: Standard-Dose LPV/r + RAL w/RBT149247

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Total Empa: Maximum Measured Concentration (Cmax)

Maximum measured concentration of total empa in plasma, per period. (NCT01634100)
Timeframe: 15 minutes (min) prior to the first dose and 20min, 40min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h, 24h, 36h, 48h and 72h after the first dose

Interventionnmol/L (Geometric Mean)
Empa Alone301
Empa + Rifampicin527
Empa + Probenecid373

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Total Empagliflozin: Area Under the Curve 0 to Infinity (AUC0-∞)

Area under the concentration-time curve of total empagliflozin (empa) in plasma over the time interval from 0 extrapolated to infinity. (NCT01634100)
Timeframe: 15 minutes (min) prior to the first dose and 20min, 40min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h, 24h, 36h, 48h and 72h after the first dose

Interventionnmol*h/L (Geometric Mean)
Empa Alone2240
Empa + Rifampicin3020
Empa + Probenecid3400

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Total Empagliflozin: Area Under the Curve 0 to Time of Last Quantifiable Data Point (AUC0-tz)

Area under the concentration-time curve of total empagliflozin (empa) in plasma over the time interval from 0 extrapolated to the time of last the quantifiable data point. (NCT01634100)
Timeframe: 15 minutes (min) prior to the first dose and 20min, 40min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h, 24h, 36h, 48h and 72h after the first dose

Interventionnmol*h/L (Geometric Mean)
Empa Alone2200
Empa + Rifampicin3000
Empa + Probenecid3350

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Area Under the Plasma Concentration Time-curve From Zero to 168 Hours [AUC(0-168)] of Vemurafenib

AUC(0-168) is the AUC from time zero (pre-dose) to 168 hours (time point for last blood sample collection). AUC is a measure of the plasma concentration of a drug over time. AUC(0-168) is presented in mcg*h/mL. (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionmcg*h/mL (Geometric Mean)
Vemurafenib (Intervention Period A)126
Vemurafenib + Rifampin (Intervention Period C)78.0

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Plasma Apparent Clearance (CL/F) of Vemurafenib

Clearance of a drug is a measure of the rate at which a drug is removed (metabolized or eliminated by normal biological processes) from the blood. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionliters/hour (Geometric Mean)
Vemurafenib (Intervention Period A)7.35
Vemurafenib + Rifampin (Intervention Period C)12.3

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Plasma Elimination Half Life (t1/2) of Vemurafenib

Plasma elimination half-life is the time measured during drug elimination phase for the plasma drug concentration to decrease by one half. (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionhours (Mean)
Vemurafenib (Intervention Period A)29.7
Vemurafenib + Rifampin (Intervention Period C)11.6

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Percent Extrapolated AUC(0-inf) (AUCpeo) of Vemurafenib

The AUCpeo, that is, percent area obtained after extrapolation from Tlast to infinity is calculated by using the formula AUCpeo = 100*(AUC[0-inf] minus AUC[0-last])/AUC(0-inf). This parameter provides information about what percentage of the theoretical curve AUC(0-inf) is possible to determine experimentally (AUC0-last). (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionpercent AUC (Geometric Mean)
Vemurafenib (Intervention Period A)2.75
Vemurafenib + Rifampin (Intervention Period C)1.26

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Time to Reach Cmax (Tmax) of Vemurafenib

Tmax is the time from vemurafenib administration to reach Cmax for vemurafenib. (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionhours (Median)
Vemurafenib (Intervention Period A)4.00
Vemurafenib + Rifampin (Intervention Period C)4.00

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Maximum Observed Plasma Concentration (Cmax) of Vemurafenib

Cmax is the maximum observed plasma vemurafenib concentration, presented in microgram per milliliter (mcg/mL). (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionmcg/mL (Geometric Mean)
Vemurafenib (Intervention Period A)4.45
Vemurafenib + Rifampin (Intervention Period C)4.95

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Area Under the Plasma Concentration Time-curve From Zero to the Last Measurable Concentration Time Point (AUClast) of Vemurafenib

AUClast is the area under the vemurafenib plasma concentration versus time curve from time zero to the time of last measured concentration of vemurafenib (Tlast). Area under the curve (AUC) is a measure of the plasma concentration of a drug over time. AUClast is presented in micrograms times (*) hour per milliliter (mcg*h/mL). (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionmcg*h/mL (Geometric Mean)
Vemurafenib (Intervention Period A)125
Vemurafenib + Rifampin (Intervention Period C)76.7

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Area Under the Plasma Concentration Time-curve From Zero to Extrapolated Infinite Time (AUC[0-inf]) of Vemurafenib

AUC(0-inf) is the AUC from time zero (pre-dose) to extrapolated infinite time (0-inf). AUC is a measure of the plasma concentration of a drug over time. AUC(0-inf) is presented in mcg*h/mL. (NCT01765543)
Timeframe: Predose (0 hour), 1, 2, 4, 6, 8, 12, 24, 30-32, 48, 72, 96, 120, 168 hours post vemurafenib-dose on Day 1 (Period A) and Day 17 (Period C)

Interventionmcg*h/mL (Geometric Mean)
Vemurafenib (Intervention Period A)131
Vemurafenib + Rifampin (Intervention Period C)78.1

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Area Under the Curve From 0 Extrapolated to Infinity (AUC0-∞)

"AUC0-∞ represents the Area under the concentration-time curve of nintedanib in plasma over the time interval from 0 extrapolated to infinity.~For this endpoint, the measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01770392)
Timeframe: 1.5 hour (h) before the first drug administration and 0.5h, 1h, 2h, 2.5h, 3h, 3.5h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after administration of nintedanib

Interventionng*h/mL (Geometric Mean)
Nintedanib183
Nintedanib + Rifampicin89.4

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Area Under the Curve From 0 to the Last Quantifiable Concentration (AUC0-tz)

"AUC0-tz represents the area under the plasma concentration-time curve of nintedanib from 0 to the last quantifiable analyte plasma concentration.~For this endpoint, the measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01770392)
Timeframe: 1.5 hour (h) before the first drug administration and 0.5h, 1h, 2h, 2.5h, 3h, 3.5h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after administration of nintedanib

Interventionng*h/mL (Geometric Mean)
Nintedanib173
Nintedanib + Rifampicin84.1

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Maximum Measured Concentration (Cmax)

"Cmax represents the maximum concentration of nintedanib in plasma. For this endpoint, the measured values show inter-individual variabilities, whereas the statistical analyses show intra-individual variabilities." (NCT01770392)
Timeframe: 1.5 hour (h) before the first drug administration and 0.5h, 1h, 2h, 2.5h, 3h, 3.5h, 4h, 5h, 6h, 8h, 10h, 12h, 24h, 36h, 48h and 72h after administration of nintedanib

Interventionng/mL (Geometric Mean)
Nintedanib22.1
Nintedanib + Rifampicin12.8

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Frequency of Adverse Events

All Adverse Events (AE), and AEs considered to be drug-related will coded using standard AE dictionaries. (NCT01785186)
Timeframe: 0 - 12 weeks

,,,,
Interventionparticipants (Number)
Number of Patients with at least 1 AENumber of patients with at least 1 SAE
Arm 1 (R35)534
HR20ZM494
HR20ZQ425
HRZE926
HRZQ494

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Sputum Culture Conversion (2 Negative Cultures) Using Liquid Media

From enrollment, the time to stable culture conversion (2 consecutive negative weekly cultures) in liquid media. (NCT01785186)
Timeframe: 0 - 12 weeks

Interventiondays (Median)
Arm 1 (R35)48
HRZQ63
HR20ZQ66
HR20ZM55
HRZE62

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Pharmacokinetics Including AUC, Cl, t1/2, Vd, and Protein Binding

"Pharmacokinetic parameters will be assessed for rifampicin, moxifloxacin and SQ109:~area under the plasma concentration curve from dosing to the end of the dosing interval (AUC 0-24) (in h*ng/mL)~the observed maximum concentration (Cmax( (in ng/mL)~time to reach Cmax (Tmax)(in hours)~the minimum observed plasma concentration 24 hours following the last dose (Cmin) (in hours),~clearance (Cl) (in mL/minute),~volume of distribution (Vd) (in L),~elimination half-life (T1/2,) (in hours)~free (protein-unbound) fraction (for rifampicin only) (in percent)." (NCT01785186)
Timeframe: 0 - 12 weeks

InterventionRifampicin AUC(mg*h/l) (Geometric Mean)
HRZQ17.4
Arm 1 (R35)170
HR20ZQ68.3
HR20ZM57.8
HRZE24.2

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Cmax: Maximum Observed Concentration for Alisertib in Presence and Absence of Rifampin

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without rifampin arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with rifampin arm

Interventionnmol/L (Mean)
Alisertib Without Rifampin1561.4
Alisertib With Rifampin1581.5

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Phase Elimination Half-life (T1/2) for Alisertib in Presence and Absence of Rifampin

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without rifampin arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with rifampin arm

Interventionhours (Mean)
Alisertib Without Rifampin16.30
Alisertib With Rifampin8.17

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Terminal Phase Elimination Half-life (T1/2) for Alisertib in Presence and Absence of Esomeprazole

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without esomeprazole arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with esomeprazole arm

Interventionhours (Mean)
Alisertib Without Esomeprazole16.06
Alisertib With Esomeprazole15.96

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Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Alisertib in Presence and Absence of Esomeprazole

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without esomeprazole arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with esomeprazole arm

Interventionhours (Median)
Alisertib Without Esomeprazole4.0
Alisertib With Esomeprazole3.0

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Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Alisertib in Presence and Absence of Rifampin

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without rifampin arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with rifampin arm

Interventionhours (Median)
Alisertib Without Rifampin4.0
Alisertib With Rifampin2.1

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Change From the Time-matched Baseline in the Fridericia Correction of QTc (QTcF)

(NCT01844583)
Timeframe: Baseline, Days 1 and 10 multiple timepoints postdose (up to 24 hours) in Cycle 1

Interventionmilliseconds (msec) (Mean)
Day 10, 0 hour postdoseDay 1, 0.5 hour postdoseDay 10, 0.5 hour postdoseDay 1, 1 hour postdoseDay 10, 1 hour postdoseDay 1, 2 hours postdoseDay 10, 2 hours postdoseDay 1, 3 hours postdoseDay 10, 3 hours postdoseDay 1, 4 hours postdoseDay 10, 4 hours postdoseDay 1, 6 hours postdoseDay 10, 6 hours postdoseDay 1, 8 hours postdoseDay 10, 8 hours postdoseDay 1, 10 hours postdoseDay 10, 10 hours postdoseDay 1, 24 hours postdose
Alisertib-2.4-3.9-5.3-4.6-3.9-3.5-2.5-2.1-2.60-1.3-0.5-4.10-1.6-1.2-3.5-3.8

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Change From the Time-matched Baseline in the Individually Corrected QTc Interval (QTcI)

(NCT01844583)
Timeframe: Baseline, Days 1 and 10 multiple timepoints postdose (up to 24 hours) in Cycle 1

Interventionmilliseconds (msec) (Mean)
Day 10, 0 hour postdoseDay 1, 0.5 hour postdoseDay 10, 0.5 hour postdoseDay 1, 1 hour postdoseDay 10, 1 hour postdoseDay 1, 2 hours postdoseDay 10, 2 hours postdoseDay 1, 3 hours postdoseDay 10, 3 hours postdoseDay 1, 4 hours postdoseDay 10, 4 hours postdoseDay 1, 6 hours postdoseDay 10, 6 hours postdoseDay 1, 8 hours postdoseDay 10, 8 hours postdoseDay 1, 10 hours postdoseDay 10, 10 hours postdoseDay 1, 24 hours postdose
Alisertib-2.2-3.7-5.4-4.5-3.5-4.0-1.6-2.5-2.3-1.2-1.2-0.9-3.5-0.5-0.4-1.5-2.4-3.3

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Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs)

An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. A Serious Adverse Event (SAE) A serious is any experience that suggests a significant hazard, contraindication, side effect or precaution that: results in death, is life-threatening, required in-patient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or is medically significant. (NCT01844583)
Timeframe: From the first dose through 30 days after administration of the last dose of study drug (up to 328 days)

,
Interventionparticipants (Number)
AEsSAEs
Esomeprazole 40 mg + Alisertib 50 mg259
Rifampin 600 mg + Alisertib 50 mg2711

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Cmax: Maximum Observed Concentration for Alisertib in Presence and Absence of Esomeprazole

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without esomeprazole arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with esomeprazole arm

Interventionnmol/L (Mean)
Alisertib Without Esomeprazole1542.6
Alisertib With Esomeprazole1804.8

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AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Alisertib in Presence and Absence of Esomeprazole

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without esomeprazole arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with esomeprazole arm

Interventionhr*nmol/L (Mean)
Alisertib Without Esomeprazole20427.8
Alisertib With Esomeprazole25094.4

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AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Alisertib in Presence or Absence of Rifampin

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without rifampin arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with rifampin arm

Interventionhr*nmol/L (Mean)
Alisertib Without Rifampin17258.3
Alisertib With Rifampin8955.0

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AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Alisertib in Presence and Absence of Esomeprazole

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without esomeprazole arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with esomeprazole arm

Interventionhr*nmol/L (Mean)
Alisertib Without Esomeprazole21371.4
Alisertib With Esomeprazole26612.5

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AUC(Last): Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Alisertib in Presence and Absence of Rifampin

(NCT01844583)
Timeframe: Day 1 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 1 for alisertib without rifampin arm; Day 8 pre-dose and at multiple time points (up to 72 hours) post-dose in Cycle 2 for alisertib with rifampin arm

Interventionhr*nmol/L (Mean)
Alisertib Without Rifampin19732.0
Alisertib With Rifampin9470.5

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Pharmacokinetics (PK): Time of Maximum Observed Drug Concentration (Tmax) of Evacetrapib

(NCT01908582)
Timeframe: Day 1 and Day 16, predose of evacetrapib and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Interventionhours (Median)
Evacetrapib2.00
Evacetrapib + Rifampin2.00

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Evacetrapib

(NCT01908582)
Timeframe: Day 1 and Day 16, predose of evacetrapib and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Evacetrapib599
Evacetrapib + Rifampin269

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Pharmacokinetics, Area Under the Plasma Concentration-Time Curve From Time 0 Hour (h) to Infinity (AUC0-∞) of Evacetrapib

(NCT01908582)
Timeframe: Day 1 and Day 16, predose of evacetrapib and 1, 2, 3, 4, 6, 8, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose

Interventionnanograms * hours per milliliter (Geometric Mean)
Evacetrapib9810
Evacetrapib + Rifampin2070

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Baricitinib

(NCT01910311)
Timeframe: Period 1, Day 1 and Period 2, Day 10: Predose, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose

Interventionhours (h) (Median)
Baricitinib1.00
Baricitinib and Rifampicin1.00

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PK: Maximum Concentration (Cmax) of Baricitinib

(NCT01910311)
Timeframe: Period 1, Day 1 and Period 2, Day 10: Predose, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose

Interventionnanograms per milliliter (ng/mL) (Geometric Mean)
Baricitinib96.1
Baricitinib and Rifampicin101

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PK: Area Under the Concentration Versus Time Curve From 0 to Infinity [AUC(0-∞)] of Baricitinib

(NCT01910311)
Timeframe: Period 1, Day 1 and Period 2, Day 10: Predose, 0.5, 1, 2, 4, 6, 8, 12, 16, 24, 36, and 48 hours postdose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
Baricitinib634
Baricitinib and Rifampicin416

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Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC[0-inf]) of Alectinib

AUC(0-inf) is the area under the alectinib plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). AUC is a measure of the plasma concentration of a drug over time. AUC(0-inf) is presented in nanogram times (*) hour per milliliter (ng*hour/mL). (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionng*hour/mL (Mean)
Treatment Period 1: Alectinib3990
Treatment Period 3: Alectinib + Rifampin1020

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Apparent Oral Clearance (CL/F) of Alectinib

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. Clearance obtained after oral dose (apparent oral clearance) is influenced by the fraction of the dose absorbed. Drug clearance is a quantitative measure of the rate at which a drug substance is removed from the blood. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionliters/hour (Mean)
Treatment Period 1: Alectinib179
Treatment Period 3: Alectinib + Rifampin627

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Plasma Terminal Half-Life (t1/2) of Alectinib and RO5468924

Plasma terminal half-life is the time measured during drug elimination phase for the plasma drug concentration to decrease by one half. RO5468924 is the major pharmacologically active metabolite of alectinib. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

,
Interventionhours (Mean)
AlectinibRO5468924
Treatment Period 1: Alectinib19.224.0
Treatment Period 3: Alectinib + Rifampin11.023.0

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Time to Reach Maximum Observed Plasma Concentration (Tmax) of Alectinib and RO5468924

The Tmax is the time from alectinib administration to reach Cmax for alectinib and RO5468924 (the major pharmacologically active metabolite of alectinib). (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

,
Interventionhours (Median)
AlectinibRO5468924
Treatment Period 1: Alectinib6.008.00
Treatment Period 3: Alectinib + Rifampin4.006.00

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AUC(0-inf) of RO5468924

AUC(0-inf) is the area under the RO5468924 (the major pharmacologically active metabolite of alectinib) plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). AUC is a measure of the plasma concentration of the drug over time. AUC(0-inf) is presented in ng*hour/mL. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionng*hour/mL (Mean)
Treatment Period 1: Alectinib2250
Treatment Period 3: Alectinib + Rifampin3970

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Cmax of RO5468924

Cmax is the maximum observed RO5468924 (the major pharmacologically active metabolite of alectinib) plasma concentration, presented in ng/mL. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionng/mL (Mean)
Treatment Period 1: Alectinib90.5
Treatment Period 3: Alectinib + Rifampin194

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Maximum Observed Plasma Concentration (Cmax) of Alectinib

Cmax is the maximum observed alectinib plasma concentration, presented in nanogram per milliliter (ng/mL). (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionng/mL (Mean)
Treatment Period 1: Alectinib212
Treatment Period 3: Alectinib + Rifampin101

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Apparent Volume of Distribution (Vz/F) of Alectinib

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. Apparent volume of distribution after oral dose (Vz/F) is influenced by the fraction of drug absorbed. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionliters (Mean)
Treatment Period 1: Alectinib4710
Treatment Period 3: Alectinib + Rifampin9960

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Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for AUC(0-inf)

AUC(0-inf) is the area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0-inf). AUC is a measure of the plasma concentration of the alectinib and RO5468924 (major pharmacologically active metabolite of alectinib) over time. The molecular weight adjusted M/P ratio (RO5468924/alectinib) for AUC(0-inf) is presented. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionratio (Geometric Mean)
Treatment Period 1: Alectinib0.59
Treatment Period 3: Alectinib + Rifampin3.96

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Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for Cmax

Cmax is the maximum observed plasma concentration of the alectinib and RO5468924 (major pharmacologically active metabolite of alectinib). The molecular weight adjusted M/P ratio (RO5468924/alectinib) for Cmax is presented. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionratio (Geometric Mean)
Treatment Period 1: Alectinib0.42
Treatment Period 3: Alectinib + Rifampin1.92

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Total Molar Concentration of Alectinib and RO5468924 as Derived by AUC(0-inf)

AUC(0-inf) is the area under the alectinib + RO5468924 (major pharmacologically active metabolite of alectinib) molar plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time (0-inf). AUC is a measure of the molar plasma concentration of the alectinib + RO5468924 over time. AUC(0-inf) is presented in nanomoles times (*) hour per liter (nmol*hour/L). (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionnmol*hour/L (Mean)
Treatment Period 1: Alectinib13200
Treatment Period 3: Alectinib + Rifampin10800

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Total Molar Concentration of Alectinib and RO5468924 as Derived by Cmax

Cmax is the maximum observed molar plasma concentration for alectinib + RO5468924 (major pharmacologically active metabolite of alectinib). Cmax is presented in nanomoles per liter (nmol/L). (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

Interventionnmol/L (Mean)
Treatment Period 1: Alectinib614
Treatment Period 3: Alectinib + Rifampin594

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Area Under the Plasma Concentration-Time Curve From Time Zero to Last Measurable Concentration (AUC[0-last]) of Alectinib and RO5468924

AUC(0-last) is the area under the alectinib and RO5468924 (major pharmacologically active metabolite of alectinib) plasma concentration time-curve from time zero to the last measured concentration. AUC is a measure of the plasma concentration of a drug over time. AUC(0-last) is presented in ng*hour/mL. (NCT01940510)
Timeframe: Predose (0 hour), 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 36, 48, 72, and 96 hours post alectinib-dose in each intervention period

,
Interventionng*hour/mL (Mean)
AlectinibRO5468924
Treatment Period 1: Alectinib38602140
Treatment Period 3: Alectinib + Rifampin9763850

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 0-24 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 0-24 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin12.56680.08780.0883NA0.59670.0786
Brentuximab Vedotin + Rifampicin12.50200.05210.0254NA0.10470.0456

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 144-168 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 144-168 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin6.11250.05380.0662NA0.34850.0402
Brentuximab Vedotin + Rifampicin4.68230.05620.0308NA0.06510.0481

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 24-48 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 24-48 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin11.13600.06040.0808NA0.57500.0637
Brentuximab Vedotin + Rifampicin13.24830.04130.0311NA0.16000.0507

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 48-72 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 48-72 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin12.72670.06200.0746NA0.69500.0632
Brentuximab Vedotin + Rifampicin13.80720.05240.0406NA0.15980.0746

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 480-504 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 480-504 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.46600.02480.0377NA0.0620NA
Brentuximab Vedotin + Rifampicin0.3334NANANA0.0221NA

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Number of Participants With Markedly Abnormal Laboratory Values

The number of participants with any markedly abnormal standard safety laboratory values collected throughout study. (NCT01950364)
Timeframe: Baseline up to 30 days after last dose of study drug (30 Days after Cycle 16)

Interventionparticipants (Number)
Brentuximab Vedotin5
Brentuximab Vedotin + Rifampicin5

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Number of Participants With Clinically Significant Change From Baseline in Vital Signs

Vital signs included body temperature, body weight, blood pressure and heart rate. (NCT01950364)
Timeframe: Baseline up to 30 days after last dose of study drug (30 Days after Cycle 16)

Interventionparticipants (Number)
Brentuximab Vedotin1
Brentuximab Vedotin + Rifampicin2

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 96-120 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 96-120 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin8.38170.07100.0916NA0.51980.0607
Brentuximab Vedotin + Rifampicin8.14260.05120.0435NA0.10880.0524

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 336-360 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 336-360 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin1.28110.03770.0347NA0.07340.0227
Brentuximab Vedotin + Rifampicin0.8271NANANA0.0277NA

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Number of Participants With Anti-therapeutic Antibodies (ATA) to Brentuximab Vedotin

Participants with positive ATA at both Cycle 1 and 3, negative ATA at both Cycle 1 and 3, and transient positive (positive at one time point, but negative at the other) ATA for brentuximab vedotin were reported. (NCT01950364)
Timeframe: Day 1 of Cycle 1 and 3

,
Interventionparticipants (Number)
Negative in both Cycle 1 and 3Positive in both Cycle 1 and 3Transient Positive
Brentuximab Vedotin512
Brentuximab Vedotin + Rifampicin702

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, Predose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: Predose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.3171NANANA0.0392NA
Brentuximab Vedotin + Rifampicin0.4227NANANANANA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 144-168 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 144-168 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin5.56930.05790.0747NA0.39160.0438
Brentuximab Vedotin + Rifampicin5.80250.04480.0287NA0.07060.0363

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 480 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 480 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.1189NANANA0.0114NA
Brentuximab Vedotin + Rifampicin0.0941NANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 48 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 48 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin3.47330.01930.01980.01700.07460.0124
Brentuximab Vedotin + Rifampicin2.2156NANANA0.0195NA

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Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An Adverse Event (AE) is defined as any untoward medical occurrence in a clinical investigation participant administered a drug; it does not necessarily have to have a causal relationship with this treatment. An AE can therefore be any unfavorable and unintended sign (example, a clinically significant abnormal laboratory finding), symptom, or disease temporally associated with the use of a drug, whether or not it is considered related to the drug. A treatment-emergent adverse event (TEAE) is defined as an adverse event with an onset that occurs after receiving study drug. A serious adverse event (SAE) is an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; or congenital anomaly; or a medically important event. AEs included both SAE and non-SAE. (NCT01950364)
Timeframe: Baseline up to 30 days after last dose of study drug (30 days after Cycle 16)

,
Interventionparticipants (Number)
AEsSAEs
Brentuximab Vedotin94
Brentuximab Vedotin + Rifampicin90

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 4 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 4 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin1.71710.03970.01630.01180.04460.0191
Brentuximab Vedotin + Rifampicin1.4529NANANA0.0190NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 336 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 336 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.4258NANANA0.0168NA
Brentuximab Vedotin + Rifampicin0.2578NANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 24 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 24 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin3.23360.02000.02030.01640.07150.0105
Brentuximab Vedotin + Rifampicin2.2558NANANA0.0177NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 0.5 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 0.5 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.39020.0184NANA0.02670.0108
Brentuximab Vedotin + Rifampicin0.2149NANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 144 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 144 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin2.33260.02970.01740.01960.0497NA
Brentuximab Vedotin + Rifampicin1.7990NANANA0.0120NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 24 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 24 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin3.79500.04430.02180.02060.08050.0142
Brentuximab Vedotin + Rifampicin3.12270.0191NANA0.01960.0113

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 336 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 336 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.3130NANANA0.0127NA
Brentuximab Vedotin + Rifampicin0.2723NANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 4 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 4 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin2.27780.05470.02540.01950.05570.0151
Brentuximab Vedotin + Rifampicin1.7836NANANA0.0160NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 48 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 48 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin4.21400.04240.01680.01870.09590.0134
Brentuximab Vedotin + Rifampicin3.37270.0128NANA0.0210NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 72 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 72 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin3.89310.05010.01900.02410.08990.0133
Brentuximab Vedotin + Rifampicin3.09480.0127NANA0.0187NA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 72-96 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 72-96 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin11.25270.07020.0937NA0.52760.0573
Brentuximab Vedotin + Rifampicin12.22630.06110.0437NA0.15100.0564

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 336-360 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 336-360 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin1.07270.04590.0289NA0.0751NA
Brentuximab Vedotin + Rifampicin1.3326NANANA0.0401NA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 24-48 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 24-48 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin12.62250.06900.0863NA0.72750.0722
Brentuximab Vedotin + Rifampicin11.79950.03920.0277NA0.15680.0405

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 144 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 144 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin2.05550.01980.01400.01370.0441NA
Brentuximab Vedotin + Rifampicin1.2920NANANA0.0145NA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 120-144 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 120-144 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin6.71610.07300.0836NA0.44770.0551
Brentuximab Vedotin + Rifampicin7.98300.03350.0301NA0.09100.0345

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, 96 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 96 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin2.91480.01360.0120NA0.0660NA
Brentuximab Vedotin + Rifampicin3.29560.14200.05930.03740.02280.0108

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 0.5 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 0.5 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.33070.0256NANA0.03230.0210
Brentuximab Vedotin + Rifampicin0.2577NANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 1, Predose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The lower limit of Quantification (LLQ) for all the observations was 0.01 nanogram/milliliter (ng/mL). (NCT01950364)
Timeframe: Cycle 1: Predose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab VedotinNANANANANANA
Brentuximab Vedotin + RifampicinNANANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 2, 0.5 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 2: 0.5 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.3119NANANANANA
Brentuximab Vedotin + Rifampicin0.2929NANANA0.0228NA

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Serum Concentrations of Antibody-drug Conjugate (ADC)

The LLQ for all the observations was 12.5 ng/mL. (NCT01950364)
Timeframe: Cycle 1 and 3: Predose, 0.5, 4, 72, 336 hours post-dose; Cycle 2: Predose, 0.5 hours post-dose; Cycle 3: 480 hours post-dose

,
Interventionng/mL (Geometric Mean)
Cycle 1, PredoseCycle 1, 0.5 hourCycle 1, 4 hourCycle 1, 72 hourCycle 1, 336 hourCycle 2, PredoseCycle 2, 0.5 hourCycle 3, PredoseCycle 3, 0.5 hourCycle 3, 4 hourCycle 3, 72 hourCycle 3, 336 hourCycle 3, 480 hour
Brentuximab VedotinNA29609.775924398.64824265.75421167.0713794.385116032.6494611.057320991.961815378.82743258.72371381.2290648.2492
Brentuximab Vedotin + RifampicinNA33125.002524533.23725958.05691108.6515435.155031627.2566536.369233040.224524496.72034262.03641363.9488734.5557

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Serum Concentration of Total Antibody (TAb)

The LLQ for all the observations was 12.5 ng/mL. (NCT01950364)
Timeframe: Cycle 1 and 3: Predose, 0.5, 4, 72, 336 hours post-dose; Cycle 2: Predose, 0.5 hours post-dose; Cycle 3: 480 hours post-dose

,
Interventionng/mL (Geometric Mean)
Cycle 1, PredoseCycle 1, 0.5 hourCycle 1, 4 hourCycle 1, 72 hourCycle 1, 336 hourCycle 2, PredoseCycle 2, 0.5 hourCycle 3, PredoseCycle 3, 0.5 hourCycle 3, 4 hourCycle 3, 72 hourCycle 3, 336 hourCycle 3, 480 hour
Brentuximab VedotinNA30874.495728577.38699931.29432898.29242055.387117378.21051361.314715974.372311609.143013594.20163206.69251329.0886
Brentuximab Vedotin + RifampicinNA30884.907428865.467411626.21473066.58591363.831931583.77931517.650633892.473127548.17739588.93743628.91751866.5746

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, Predose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: Predose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.1046NANANANANA
Brentuximab Vedotin + Rifampicin0.0727NANANANANA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 96 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 96 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin2.44490.01400.02050.01210.06220.0105
Brentuximab Vedotin + Rifampicin2.23440.04180.02940.02520.0392NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 3, 72 Hour Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 72 hour postdose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin3.30470.03100.02560.01680.0728NA
Brentuximab Vedotin + Rifampicin1.9732NANANA0.0187NA

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Plasma Concentration of Monomethylauristatin E (MMAE) and Its Metabolites at Cycle 2, Predose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. The LLQ for all the observations was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 2: Predose

,
Interventionng/mL (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.0919NANANANANA
Brentuximab Vedotin + Rifampicin0.0795NANANANANA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 48-72 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 48-72 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin12.40890.08120.0867NA0.79730.0786
Brentuximab Vedotin + Rifampicin11.66000.04190.0322NA0.11890.0382

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 480-504 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 480-504 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin0.4420NANANA0.0578NA
Brentuximab Vedotin + Rifampicin0.3505NANANANANA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 72-96 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 72-96 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin10.77660.08670.0882NA0.74800.0754
Brentuximab Vedotin + Rifampicin12.84260.04270.0394NA0.12470.0415

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, 96-120 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: 96-120 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin10.80180.08850.1053NA0.73600.0630
Brentuximab Vedotin + Rifampicin9.56260.04140.0406NA0.10340.0380

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 1, Predose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 1: Predose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab VedotinNANANANANANA
Brentuximab Vedotin + Rifampicin7.8900NANANA0.0712NA

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 0-24 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 0-24 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin10.71740.04540.0509NA0.46570.0516
Brentuximab Vedotin + Rifampicin12.44380.04510.0301NA0.12850.0676

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Amount of Monomethylauristatin E (MMAE) and Its Metabolites Excreted in Urine at Cycle 3, 120-144 Hours Postdose

Metabolites of MMAE includes C4, C5, C7, C8 and C13. Amount of MMAE and its metabolites in urine were determined by multiplying the volume of urine obtained and the concentration of MMAE and its metabolites present in it, respectively. The LLQ for determining the concentration was 0.01 ng/mL. (NCT01950364)
Timeframe: Cycle 3: 120-144 hours postdose

,
Interventionng (Geometric Mean)
MMAEC4C5C7C8C13
Brentuximab Vedotin7.35000.04610.0657NA0.47000.0386
Brentuximab Vedotin + Rifampicin7.58710.05200.0342NA0.08690.0429

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Phosphate/Creatinine (mg/g)

Urine Phosphate/Creatinine(mg/g) (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

Interventionratio (mg/g) (Mean)
Water8.3
Rifampin11.1
Grapefruit Juice23.3
Grapefruit Juice Plus Rifampin79.6
Clarithromycin5.5
Clarithromycin Plus Rifampin60.0

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Parathyroid Hormone

Blood Parathyroid Hormone (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

Interventionpg/mL (Mean)
Water0.3
Rifampin0.4
Grapefruit Juice1.6
Grapefruit Juice Plus Rifampin1.0
Clarithromycin2.7
Clarithromycin Plus Rifampin0.6

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Calcium/Creatinine (mg/g)

Urine Calcium/Creatinine (mg/g) (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

Interventionratio (mg/g) (Mean)
Water3.4
Rifampin-9.2
Grapefruit Juice-41.1
Grapefruit Juice Plus Rifampin-3.8
Clarithromycin6.3
Clarithromycin Plus Rifampin41.4

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Calcium, Ionized

Serum (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

InterventionmM (Mean)
Water0.0
Rifampin-0.008
Grapefruit Juice-0.017
Grapefruit Juice Plus Rifampin-0.011
Clarithromycin-0.005
Clarithromycin Plus Rifampin-0.009

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25(OH) D3 Vitamin D

Serum 25(OH) D3 Vitamin D (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

InterventionnM (Mean)
Water-3.1
Rifampin-4.3
Grapefruit Juice-1.3
Grapefruit Juice Plus Rifampin-1.6
Clarithromycin0.6
Clarithromycin Plus Rifampin-5.0

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1, 25(OH) D3 Vitamin D

Serum 1, 25(OH) D3 Vitamin D (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

InterventionpM (Mean)
Water3.2
Rifampin1.7
Grapefruit Juice3.7
Grapefruit Juice Plus Rifampin-3.3
Clarithromycin-4.7
Clarithromycin Plus Rifampin0.4

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Osteocalcin

Serum Osteocalcin (NCT02019875)
Timeframe: Samples will be collected on days 1, 4 and 7, and day 22 (last day of intervention). Treatment began on day 8. Data presented is day 22 concentration - Baseline (the average of day 1, day 4 and day 7 concentrations).

Interventionng/mL (Mean)
Water0.0
Rifampin-1.1
Grapefruit Juice0.7
Grapefruit Juice Plus Rifampin0.0
Clarithromycin3.7
Clarithromycin Plus Rifampin4.0

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FEV1%

FEV1% was measure pre and post 6 minute walk test (NCT02024555)
Timeframe: Baseline, 4, 8, and 16 and 24 weeks

,
InterventionPercentage of predicted FEV1 (Mean)
Baseline preBaseline post4 weeks pre4 weeks post8 weeks pre8 weeks post16 weeks pre16 weeks post24 weeks pre24 weeks post
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin69.1169.9771.5771.9669.3070.3669.8871.3972.2273.09
Placebo67.4573.8169.5673.8173.7174.368.2770.4163.2766.27

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Six Minute Walk, Distance in Meters

The 6-min walk test (6 MWT) is a submaximal exercise test that entails measurement of distance walked over a span of 6 minutes. (NCT02024555)
Timeframe: Baseline, 4, 8, and 16 and 24 weeks

,
Interventionmeters (Mean)
BaselineWeek 4Week 8Week 16Week 24
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin416.25432.65451.59440.37444.68
Placebo416.41428.35420.21430.85425.18

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Change in Oxygen Saturation

measured using pulse oximetry (NCT02024555)
Timeframe: Baseline, 4, 8, and 16 and 24 weeks

,
Interventionpercentage of oxygen saturation (Mean)
Baseline to week 4Baseline to week 8Baseline to week 16
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin0.39-0.122.54
Placebo-0.85-0.43-0.46

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Adverse Events

Safety profile of regimen as evidenced by the number of adverse events (NCT02024555)
Timeframe: 24 weeks

,
Interventionnumber of events (Number)
Serious Adverse EventsNon-Serious Adverse Events
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin424
Placebo316

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Abnormal Lab Values

Safety profile of regimen as evidenced by the number of abnormal lab values classified as Adverse Events (NCT02024555)
Timeframe: baseline to 16 weeks

,
Interventionparticipants (Number)
low platelet countlow WBC countelevated glucoselow glucose
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin1531
Placebo0021

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Change in the Saint George's Respiratory Questionnaire (SGRQ)

"The SGRQ is a 50-item questionnaire developed to measure health status (quality of life) in patients with diseases of airways obstruction.~Scores range from 0 to 100, with higher scores indicating more limitations.~A minimum change in score of 4 units was established as clinically relevant after patient and clinician testing." (NCT02024555)
Timeframe: Baseline and 16 weeks

Interventionscore on a scale (Mean)
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin-2.23
Placebo-6.30

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Change in Percent Predicted Absolute Forced Vital Capacity (FVC) in Participants With Pulmonary Sarcoidosis, Comparing Baseline With Performance After Completion of 16 Weeks of Therapy.

Change in percent predicted absolute forced vital capacity (FVC) in participants with pulmonary sarcoidosis, comparing baseline with performance after completion of 16 weeks of therapy. This will involve comparing sarcoidosis and placebo after 16 weeks of therapy. (NCT02024555)
Timeframe: Baseline to 16 weeks

Interventionpercentage predicted absolute FVC (Mean)
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin0.35
Placebo0.17

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Failure of Standard Therapy

We will assess how many subjects in either arm need escalation of their standard regimen (ie increase in prednisone) during the 16 weeks. (NCT02024555)
Timeframe: Baseline to 16 weeks

InterventionParticipants (Count of Participants)
Concomitant Levaquin, Ethambutol, Azithromycin and Rifampin3
Placebo2

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Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System

The bactericidal activity (BA) was determined by the rate of change in TTP collected from overnight sputum samples over 8 weeks of treatment in the liquid culture media MGIT system, represented by the model-fitted log(TTP) results as calculated by the regression of the observed log(TTP) results over time. The bactericidal activity of log(TTP) over Day 0 to Day 56 (BATTP[0-56]) was presented and expressed as the daily percentage change in TTP from Day 0 to Day 56. The mean BATTP (0-56) was calculated from Bayesian non-linear mixed effects regression models fitted to log(TTP) collected from sputum samples (observed from Day 0 to Day 56). (NCT02193776)
Timeframe: Day 0 to Day 56 (8 weeks)

Interventionpercentage change in TTP/day (Mean)
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide4.878
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide5.182
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)4.046
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide5.194

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

A TEAE was defined as any AE which started or worsened on or after first study drug administration up to and including the Day 70 follow-up visit (or up to and including 14 days after last study drug administration for participants not having Day 70 follow-up visit). Drug-related TEAEs were defined as TEAEs for which relationship to study drug was indicated as 'possible', 'probable', 'certain' or missing. TEAEs leading to death were defined as TEAEs resulted 'fatal' outcome. Serious TEAEs were defined as TEAEs for which serious was indicated as 'yes'. TEAEs leading to discontinuation of study drug were defined as TEAEs for which action taken with study drug was indicated as 'study drug stopped'. TEAEs leading to early withdrawal from study were defined as TEAEs resulted study discontinuation. Grade III and IV TEAEs were defined as TEAEs for which severity (DMID grade) was indicated as 'Grade 3 (severe)' and 'Grade 4 (potentially life-threatening)' or missing, respectively. (NCT02193776)
Timeframe: First study drug administration (Day 1) up to and including the Day 70 follow-up visit (or up to and including 14 days after last study drug administration for participants not having the Day 70 follow-up visit) (70 days)

,,,
InterventionParticipants (Count of Participants)
Any TEAEDrug-related TEAETEAE leading to deathAny serious TEAEDrug-related serious TEAETEAE leading to discontinuation of study drugTEAE leading to early withdrawal from studyGrade III TEAEGrade IV TEAE
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide452913055177
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide503814265198
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)442914122142
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide574604222131

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Assessment of Tss,Max for AZD9291, and AZ5104 and AZ7550 (Metabolites)

Rate and extent of absorption of AZD9291, and AZ5104 and AZ7550 (metabolites) by assessment of time to reach maximum plasma concentration at steady state (tss,max). AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

,,
Interventionh (Median)
AZD9291 tss,maxAZ5104 tss,maxAZ7550 tss,max
AZD9291 + Rifampicin (Period 2)5.886.037.95
AZD9291 Alone (Period 1)4.976.006.14
AZD9291 Alone (Period 3)6.006.007.03

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Assessment of Area Under the Plasma Concentration-time Curve During the Dosing Interval for AZD9291 After Dosing Alone and in Combination With Rifampicin (AUCtau)

Rate and extent of absorption of AZD9291 by assessment of AUCtau. AZD9291 doses were first without, then with rifampicin (Periods 1 and 2, respectively). (NCT02197247)
Timeframe: Samples collected on Day 28 following AZD9291 alone and Day 49 following AZD9291 and rifampicin at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM * hour (nM*h) (Geometric Mean)
AZD9291 Alone (Period 1)10870
AZD9291 + Rifampicin (Period 2)2192

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Assessment of Css,Max for AZ7550 (Metabolite)

Rate and extent of absorption of AZ7550 (metabolite) by assessment of Css,max. AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM (Geometric Mean)
AZD9291 Alone (Period 1)53.54
AZD9291 + Rifampicin (Period 2)73.14
AZD9291 Alone (Period 3)53.24

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Assessment of AUCtau for AZD9291 Before and After Rifampicin

Rate and extent of absorption of AZD9291 by assessment of AUCtau. AZD9291 alone before rifampicin (Period 1) and AZD9291 alone after rifampicin (Period 3). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 following AZD9291 alone at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone (Period 1)10870
AZD9291 Alone (Period 3)10060

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Assessment of AUCtau for Rifampicin

Rate and extent of absorption of rifampicin by assessment of AUCtau. AZD9291 dosing in combination with rifampicin (Period 2). (NCT02197247)
Timeframe: Samples collected on Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

Interventionng*h/mL (Geometric Mean)
AZD9291 + Rifampicin (Period 2)58610

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Assessment of CLss/F for AZD9291

Rate and extent of absorption of AZD9291 by assessment of the apparent plasma clearance following oral administration and multiple dosing (CLss/F). AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionLitre per hour (L/h) (Geometric Mean)
AZD9291 Alone (Period 1)14.74
AZD9291 + Rifampicin (Period 2)73.07
AZD9291 Alone (Period 3)15.92

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Assessment of CLss/F for Rifampicin

Rate and extent of absorption of rifampicin by assessment of CLss/F. AZD9291 dosing in combination with rifampicin (Period 2). (NCT02197247)
Timeframe: Samples collected on Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionL/h (Geometric Mean)
AZD9291 + Rifampicin (Period 2)10.23

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Assessment of Css,Max for AZ5104 (Metabolite)

Rate and extent of absorption of AZ5104 (metabolite) by assessment of Css,max. AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM (Geometric Mean)
AZD9291 Alone (Period 1)60.40
AZD9291 + Rifampicin (Period 2)12.28
AZD9291 Alone (Period 3)50.73

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Assessment of the Metabolic Ratios of Css,Max for AZ5104 and AZ7550 (MRCss,Max)

Assessment of the metabolite to parent ratio (calculated as AZ5104 to AZD9291 and AZ7550 to AZD9291) for Css,max (MRCss,max). AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

,,
InterventionRatio (Geometric Mean)
AZ5104 Css,max / AZD9291 Css,maxAZ7550 Css,max / AZD9291 Css,max
AZD9291 + Rifampicin (Period 2)0.083270.4960
AZD9291 Alone (Period 1)0.10460.09276
AZD9291 Alone (Period 3)0.095440.1002

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Assessment of the Metabolic Ratios of AUCtau for AZ5104 and AZ7550 (MRAUCtau)

Assessment of the metabolite to parent ratio (calculated as AZ5104 to AZD9291 and AZ7550 to AZD9291) for AUCtau (MRAUCtau). AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

,,
InterventionRatio (Geometric Mean)
AZ5104 AUCtau / AZD9291 AUCtauAZ7550 AUCtau / AZD9291 AUCtau
AZD9291 + Rifampicin (Period 2)0.095950.6459
AZD9291 Alone (Period 1)0.11090.1019
AZD9291 Alone (Period 3)0.10230.1104

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Assessment of Css,Min for AZD9291, and AZ5104 and AZ7550 (Metabolites)

Rate and extent of absorption of AZD9291, and AZ5104 and AZ7550 (metabolites) by assessment of minimum plasma concentration at steady state (Css,min). AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

,,
InterventionnM (Geometric Mean)
AZD9291 Css,minAZ5104 Css,minAZ7550 Css,min
AZD9291 + Rifampicin (Period 2)50.565.81644.89
AZD9291 Alone (Period 1)354.741.8037.99
AZD9291 Alone (Period 3)326.935.3737.68

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Assessment of Tss,Max for Rifampicin

Rate and extent of absorption of rifampicin by assessment of tss,max. AZD9291 dosing in combination with rifampicin (Period 2). (NCT02197247)
Timeframe: Samples collected on Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

Interventionh (Median)
AZD9291 + Rifampicin (Period 2)2.00

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Assessment of Maximum Plasma Concentration for AZD9291 After Dosing Alone and in Combination With Rifampicin (Css,Max)

Rate and extent of absorption of AZD9291 by assessment of maximum plasma concentration at steady state (Css,max). AZD9291 doses were first without, then with rifampicin (Periods 1 and 2, respectively). (NCT02197247)
Timeframe: Samples collected on Day 28 following AZD9291 alone and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

Interventionnanomolar (nM) (Geometric Mean)
AZD9291 Alone (Period 1)577.4
AZD9291 + Rifampicin (Period 2)147.5

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Assessment of Css,Min for Rifampicin

Rate and extent of absorption of rifampicin by assessment of minimum plasma concentration at steady state (Css,min). AZD9291 dosing in combination with rifampicin (Period 2). (NCT02197247)
Timeframe: Samples collected on Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

Interventionng/mL (Geometric Mean)
AZD9291 + Rifampicin (Period 2)NA

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Assessment of Css,Max for Rifampicin

Rate and extent of absorption of rifampicin by assessment of Css,max. AZD9291 dosing in combination with rifampicin (Period 2). (NCT02197247)
Timeframe: Samples collected on Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

Interventionnanogram per millilitre (ng/mL) (Geometric Mean)
AZD9291 + Rifampicin (Period 2)13810

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Assessment of Css,Max for AZD9291 Before and After Rifampicin

Rate and extent of absorption of AZD9291 by assessment of Css,max. AZD9291 alone before rifampicin (Period 1) and AZD9291 alone after rifampicin (Period 3). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 following AZD9291 alone at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM (Geometric Mean)
AZD9291 Alone (Period 1)577.4
AZD9291 Alone (Period 3)531.4

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Assessment of AUCtau for AZ5104 (Metabolite)

Rate and extent of absorption of AZ5104 (metabolite) by assessment of AUCtau. AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone (Period 1)1206
AZD9291 + Rifampicin (Period 2)210.3
AZD9291 Alone (Period 3)1029

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Assessment of AUCtau for AZ7550 (Metabolite)

Rate and extent of absorption of AZ7550 (metabolite) by assessment of AUCtau. AZD9291 dosing alone and in combination with rifampicin (all periods). (NCT02197247)
Timeframe: Samples collected on Day 28 and 77 (following AZD9291 alone) and Day 49 (following AZD9291 and rifampicin) at pre-dose, 1, 2, 3, 4, 6, 8, 10, 12, and 24 hours post dose in Part A.

InterventionnM*h (Geometric Mean)
AZD9291 Alone (Period 1)1107
AZD9291 + Rifampicin (Period 2)1416
AZD9291 Alone (Period 3)1111

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PK: Area Under the Concentration Time Curve AUC(0-∞) of LY2835219

(NCT02256267)
Timeframe: Period 1: Day 1- Predose,1, 2, 4, 6, 8, 10 hours, Days 2-9: 24, 48, 72, 96, 120, 144, 168, and 192 hours; Period 2: Day 7- Predose,1, 2, 4, 6, 8, 10 hours, Days 8-15: 24, 48, 72, 96, 120, 144, 168, 192 hours

Interventionnanogram x hour per mL (ng x h/mL) (Geometric Mean)
200 mg LY28352194570
200 mg LY2835219 + 600 mg Rifampin229

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of LY2835219

(NCT02256267)
Timeframe: Period 1: Day 1- Predose,1, 2, 4, 6, 8, 10 hours, Days 2-9: 24, 48, 72, 96, 120, 144, 168, and 192 hours; Period 2: Day 7- Predose,1, 2, 4, 6, 8, 10 hours, Days 8-15: 24, 48, 72, 96, 120, 144, 168, 192 hours

Interventionnanogram per milliliter (ng/ml) (Geometric Mean)
200 mg LY2835219134
200 mg LY2835219 + 600 mg Rifampin10.5

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Steady State Pharmacokinetics (PK) (AUC) of PA-824 When Given With Rifampin or Rifabutin

AUC of PA-824 when given with either rifampicin or rifabutin to determine steady state Pharmacokinetics (PK) of PA-824. (NCT02256696)
Timeframe: pre-dose and 1, 2, 5, 8, and 24 hours post-dose on Day 14

Interventionmg*h/L (Mean)
Arm 131.91
Arm 259.05

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Time to Sputum Culture Conversion on Liquid Medium

The time (days) it takes for the sputum to convert from positive to negative. (NCT02256696)
Timeframe: 12 weeks

,,
Interventiondays (Median)
Time to culture conversion (mITT)Time to culture conversion (per protocol)
Arm 14242
Arm 22828
Arm 35656

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Time to Culture Conversion on Solid Medium

The time (days) it takes for the sputum to convert form positive to negative on solid medium (NCT02256696)
Timeframe: 12 weeks

,,
Interventiondays (Median)
Time to conversion on solid culture (mITT)Time to conversion on solid culture (per protocol)
Arm 12828
Arm 22121
Arm 34242

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Percentage of Participants With Sputum Culture Conversion by 8 Weeks of Treatment

Percentage of participants whose sputum converts from positive to negative at Week 8 time point, on solid and liquid media. (NCT02256696)
Timeframe: 8 weeks

,,
Interventionpercentage of participants (Number)
Liquid mediaSolid media
Arm 17998
Arm 289100
Arm 36996

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Number of Participants With Grade 3 or Higher Adverse Events

Any Grade 3 event according to the Division of AIDS (DAIDS) toxicity table (NCT02256696)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm 13
Arm 26
Arm 32

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Number of Participants With Permanent Discontinuation of Assigned Study Regimen

If it is in the best interest of a participant to stop the study regimen for any reason (NCT02256696)
Timeframe: 12 weeks

InterventionParticipants (Count of Participants)
Arm 12
Arm 27
Arm 30

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PK (Cmax) of PA-824 at 200 mg Once Daily With Rifampin or Rifabutin-containing Treatment

The Pharmacokinetic results (Cmax) of the study drug when given with a rifampin or a rifabutin. (NCT02256696)
Timeframe: pre-dose and 1, 2, 5, 8, and 24 hours post-dose on Day 14

Interventionmg/L (Mean)
Arm 12.03
Arm 22.69

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Relationship Between PA-824 Exposure (AUC) and Rate of Change in Time to Positivity (TTP) Over 12 Weeks

Relationship between PA-824 exposure (AUC) and rate of change in TTP over 12 weeks, using non-linear mixed effects modeling. The data is reported as percentage increase in TTP per 10 unit increase in PA-824 AUC (% increase/10 unit increase PA-824 AUC). (NCT02256696)
Timeframe: 12 weeks

Intervention% increase/10 unit increase PA-824 AUC (Number)
Arms 1 and 2 (Pretomanid-containing Arms)9.4

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Covariates of PK Measures: C-reactive Protein (CRP)

Median Concentration of C-reactive Protein. Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs. (NCT02372383)
Timeframe: baseline

Interventionmg/dL (Median)
Healthy Controls0.2
CF Fasting0.8

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Covariates of PK Measures: Circulating Neutrophil Count

Circulating neutrophil count. Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs (NCT02372383)
Timeframe: baseline

Intervention10^3 cells/uL (Median)
Healthy Controls3.0
CF Fasting3.8

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Covariates of PK Measures: Creatinine

Creatinine. Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs (NCT02372383)
Timeframe: baseline

Interventionmg/dL (Median)
Healthy Controls1.0
CF Fasting0.9

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Other PK Measures: Half-life (t1/2)

t1/2 of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionhours (Median)
RifampinEthambutolAzithromycin
CF Fasting3.44.35.2
CF Food3.44.76.6
Healthy Controls3.85.36.2

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Other PK Measures: Drug Clearance

"drug clearance of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls~Reported here are the Median (range) CL in the CF fasting state compared to HC for Rifampin." (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
InterventionL/h (Median)
RifampinEthambutolAzithromycin
CF Fasting7.942.473.6
CF Food7.637.382.8
Healthy Controls5.145.388.6

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Other PK Measures: Median Time to Maximal Drug Concentration (Tmax)

Tmax of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionhours (Median)
RifampinEthambutolAzithromycin
CF Patients, Fasting1.52.32.0
CF Patients, Food2.52.02.0
Healthy Controls1.52.32.0

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Area Under the Curve (AUC)

AUC of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls. (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionmg*h/L (Median)
RifampinEthambutolAzithromycin
CF Fasting7621.86.8
CF Food79.223.66
Healthy Controls118.321.45.6

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Median Maximal Drug Concentration (Cmax)

Cmax of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls. (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
Interventionmg/L (Median)
RifampinEthambutolAzithromycin
CF Fasting12.54.22.0
CF Food11.24.32.2
Healthy Controls16.563.01.1

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Covariates of PK Measures: Body Mass Index

Body mass index (BMI). Begin to investigate the influence of inflammation, host characteristics, and drug metabolism on the PK of the antimycobacterial drugs (NCT02372383)
Timeframe: baseline

Interventionkg/m^2 (Median)
Healthy Controls23.0
CF Fasting21.9

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Other PK Measures: Volume of Distribution (Vd)

Vd of the oral antimycobacterial drugs (azithromycin, rifampin and ethambutol) under both fasting conditions and when taken with food plus supplemental pancreatic enzymes in subjects with pancreatic insufficient CF, compared to healthy controls (NCT02372383)
Timeframe: 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, and 12 hours post dose

,,
InterventionL (Median)
RifampinEthambutolAzithromycin
CF Fasting39.7274.6549.2
CF Food37.4354.3621.3
Healthy Controls31.3352.8717.0

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TB Disease-free Survival at 12M After Study Treatment Assignment Among Participants in Control Regimen, Regimen1 (2HRZE/4HR) to Experimental Regimens, Regimen3 (2HPZM/2HPM) and Regimen2 (2HPZ/2HP) (Assessable Population)

"To evaluate the efficacy of a rifapentine-containing regimen to determine whether the single substitution of rifapentine for rifampin makes it possible to reduce to seventeen weeks the duration of treatment for drug-susceptible pulmonary tuberculosis~To evaluate the efficacy of a rifapentine-containing regimen that in addition substitutes moxifloxacin for ethambutol and continues moxifloxacin during the continuation phase, to determine whether it is possible to reduce to seventeen weeks the duration of treatment for drug-susceptible pulmonary tuberculosis A primary outcome status of favorable, unfavorable, or not assessable was assigned. For detailed definitions of outcomes please refer to: Dorman SE, at al. N Engl J Med. 2021 May 6;384(18):1705-1718." (NCT02410772)
Timeframe: Twelve months after treatment assignment

,,
InterventionParticipants (Count of Participants)
FavorableUnfavorable
Regimen 1 (2HRZE/4HR)65670
Regimen 2 (2HPZ/2HP)645107
Regimen 3 (2HPMZ/2HPM)66888

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Change in Body Mass Index (BMI) From Baseline at 2 Months

The change in BMI was assessed by a digital weight scale and height scale (kg/m²). The formula for BMI is weight in kilograms divided by height in meters squared. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Higher scores reflected the better nutritional status results of the patients. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionKg/m² (Mean)
Intervention1.13
Control0.54

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Change in Hand-grip Strength on a Digital Dynamometer Scale From Baseline at 2 Months

The change of hand-grip strength of the participants over the two months intervention period was measured on a kilograms scale. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Positive numbers represent increases and negative numbers represent decreases. The higher scores reflected the better physical function outcomes of the patients. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionKilogram (Mean)
Intervention3.90
Control0.84

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Protein Intake on 24-hour Dietary Recall Method.

The average protein intake (in Gram/day) was assessed by the 24-hour dietary recall questionnaire and calculated using NutriSurvey software version 2005, with the country specific food database for Indonesia. (NCT02554318)
Timeframe: In the course of the 8 week intervention, two interviews were conducted; at the 2nd and 6th week.

,
InterventionGram/day (Mean)
2nd week6th weekAverage
Control69.4973.3571.42
Intervention77.3477.7077.52

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Caloric Intake on 24-hour Dietary Recall Method at the 2nd and 6th.

The average calorie intake (in kcal/day) was assessed by the 24-hour dietary recall questionnaire and calculated by NutriSurvey software version 2005, with the country-specific food database for Indonesia. (NCT02554318)
Timeframe: In the course of the 8 week intervention, two interviews were conducted; at the 2nd and 6th week.

,
InterventionKcal/day (Mean)
2nd week6th weekAverage
Control1844.642059.271972.12
Intervention1980.102227.982113.16

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Change in Distance on 6-minute Walk Test (6MWT) From Baseline at 2 Months

The change distance in meters scale as assessed by 6MWT according to American Thoracic Society (ATS) 2002 guidelines. The 6MWT was carried out on a track along the 30-meter corridor marked by two colored cones placed at both ends of the track alignment. The participants were asked using the standard instruction to walk at their self-selected pace back and forth between the cones as far as they could for 6 minutes. The distance taken by each participant was measured and then recorded. Instructions were given to every patient by reading a guideline with the same intonations to every patient before performing the test. The result of the 6MWT was expressed in meters. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Higher scores reflected better physical function outcomes. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionMeter (Mean)
Intervention49.67
Control25.75

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Change in Bodyweight on a Digital Weight Scale From Baseline at 2 Months

Change of body weight of the participants over the two months intervention period as measured on a kilograms scale. The change was calculated from two-time points as the value at the later time point minus the value at the earlier time point. Positive numbers represent increases and negative numbers represent decreases. A higher value score in change means a better outcome on nutritional status for the patients after the study. (NCT02554318)
Timeframe: Baseline, 2 months

InterventionKilogram (Mean)
Intervention2.80
Control1.44

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Plasma CL/F for PF-06463922 Given Alone and With Rifampin

CL/F is the apparent oral clearance. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

InterventionL/hr (Geometric Mean)
PF-06463922 100 mg11.39
Rifampin 600 mg + PF-06463922 100 mg76.91

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Plasma AUClast for PF-06895751 When PF-06463922 Given Alone and With Rifampin

AUClast was the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. PF-06895751 was the metabolite of PF-06463922. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionng*hr/mL (Geometric Mean)
PF-06463922 100 mg4105
Rifampin 600 mg + PF-06463922 100 mg3169

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Plasma AUClast for PF-06463922 Given Alone and With Rifampin

AUClast is the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionng•hr/mL (Geometric Mean)
PF-06463922 100 mg8597
Rifampin 600 mg + PF-06463922 100 mg1200

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Plasma AUCinf for PF-06895751 When PF-06463922 Given Alone and With Rifampin

AUCinf was the area under the plasma concentration-time profile from time 0 extrapolated to infinite time. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. PF-06895751 was the metabolite of PF-06463922. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionng•hr/mL (Geometric Mean)
PF-06463922 100 mg4453
Rifampin 600 mg + PF-06463922 100 mg3291

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Plasma AUCinf for PF-06463922 Given Alone and With Rifampin

AUCinf is the plasma area under the plasma concentration-time profile from time 0 extrapolated to infinite time. The pharmacokinetics (PK) parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionnanogram (ng)*hr/ millilitre (mL) (Geometric Mean)
PF-06463922 100 mg8766
Rifampin 600 mg + PF-06463922 100 mg1299

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Number of Participants With Physical Examination Findings Meeting the Criteria of Potentially Significant Clinical Concern

A full physical examination included head, ears, eyes, nose, mouth, skin, heart and lung examinations, lymph nodes, gastrointestinal, musculoskeletal, and neurological systems. The limited or abbreviated physical examination focused on general appearance, the respiratory and cardiovascular systems, as well as towards participant reported symptoms. Clinical significance was judged by the investigator. (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose.

InterventionParticipants (Count of Participants)
PF-06463922 100 mg0
Rifampin 600 mg + PF-06463922 100 mg0

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Number of Participants With Concomitant Treatments Meeting the Criteria of Potentially Significant Clinical Concerns

Participants abstained from all concomitant treatments, except for the treatment of adverse events. Limited use of non-prescription medications that were not believed to affect participant safety or the overall results of the study might be permitted on a case by case basis following approval by the sponsor. All participants were questioned about concomitant treatment at each clinic visit. Treatments taken within 28 days before the first dose of study investigational product were documented as a prior treatment. Treatment taken after the first dose of study investigational product were documented as concomitant treatments. Females taking hormone replacement therapy might be eligible to participate in this study if they were willing to discontinue therapy at least 28 days prior to the first dose of study treatment and remained off hormonal therapy for duration of the study. Clinical significance was judged by the investigator. (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose.

InterventionParticipants (Count of Participants)
PF-06463922 100 mg0
Rifampin 600 mg + PF-06463922 100 mg0

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Plasma Tmax for PF-06463922 Given Alone and With Rifampin

Tmax is the time for maximum observed plasma concentration (Cmax). The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionhr (Median)
PF-06463922 100 mg1.50
Rifampin 600 mg + PF-06463922 100 mg1.51

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs) (All Causalities and Treatment-Related)

An adverse event (AE) was any untoward medical occurrence in a clinical investigation participant administered a product or medical device; the event need not necessarily have a casual relationship with the treatment or usage. A serious adverse event (SAE) was any untoward medical occurrence at any dose that: 1) resulted in death; 2) was life threatening (immediate risk of death); 3) required inpatient hospitalization or prolongation of existing hospitalization; 4) resulted in persistent or significant disability/incapacity (substantial disruption of the ability to conduct normal life functions); 5) resulted in congenital anomaly/birth defect. TEAE included both non-serious adverse events and serious adverse events. (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose.

,,
InterventionParticipants (Count of Participants)
No. of Participants with AEs (all Causalities)No. of Participants with SAEs (all Causalities)Participants with Severe AEs (all Causalities)Discontinued due to AEs (all Causality)No. of Participants with AEs (Treatment Related)No. of Participants with SAEs (Treatment Related)Participants with Severe AEs (Treatment Related)Discontinued due to AEs (Treatment Related)
PF-06463922 100 mg10001000
Rifampin 600 mg + PF-06463922 100 mg125712125712
Rifampin 600 mg QD50004000

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Number of Participants With End of Study Abnormal Laboratory Findings Meeting the Criteria of Potentially Significant Clinical Concern

The total number of participants with laboratory test abnormalities was assessed. Clinical laboratory tests included hematology, chemistry, urinalysis and some other tests (including follicle-simulating hormone[FSH], urine drug screening, hepatitis B surface antigen [HBsAg], hepatitis B core antibody [HBcAb], hepatitis C virus antibody [HCVAb] and human immunodeficiency virus [HIV]. Clinical significance was judged by the investigator. (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose

,,
InterventionParticipants (Count of Participants)
No. of Participants Evaluable for Lab. AbnormalityNo. With Lab. Abnormalities
PF-06463922 100 mg125
Rifampin 600 mg + PF-06463922 100 mg1211
Rifampin 600 mg QD126

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Number of Participants With Electrocardiogram (ECG) Findings Meeting the Criteria of Potentially Significant Clinical Concerns

PR interval was the interval between the start of the P wave and the start of the QRS complex, corresponding to the time between the onset of the atrial depolarization and onset of ventricular depolarization. Criteria for potentially clinically important changes (chg) in ECG were defined as: absolute values of PR interval >=200 to <220 msec, >=220 to <240 msec, >=240 to <260 msec and >=260 msec. Increase from baseline >=40, <60, >=60 and <80, >=80, and relative change from baseline >25%. The beginning of the Q wave to the end of the T wave corresponding to electrical systole (QT) interval corrected using the Fridericia formular (QTCF) of 450 to <480 msec, 480 to <500 msec and >=500 msec, or an increase of 30 to <60 msec of >=60 msec. Maximum is abbreviated as Max. (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose.

,
InterventionParticipants (Count of Participants)
Maximum (Max) PR Interval (msec) 200-<220Max PR Interval (msec) 220-<240Max PR Interval (msec) 240-<260Max PR Interval (msec) >=260Max QT Interval (msec) >=500Max QTCF Interval (msec) 450-<480Max QTCF Interval (msec) 480-<500Max QTCF Interval (msec) >=500Max PR Interval Inc. From Baseline (msec) 40-<60Max PR Interval Inc. From Baseline (msec) 60-<80Max PR Interval Inc. From Baseline (msec) >=80Max PR Interval Inc.From Baseline(msec)PctChg>25%Max QTCF Inc. From Baseline (msec) 30<=Chg<60Max QTCF Inc. From Baseline (msec) Chg>=60
PF-06463922 100 mg00000000000000
Rifampin 600 mg + PF-06463922 100 mg00001100000010

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Number of Participants With Changes From Baseline and Absolute Values in Vital Signs Meeting the Criteria of Potentially Significant Clinical Concerns

"Criteria for potentially clinically important changes in vital signs were defined as: supine and standing systolic blood pressure (SBP) of less than (<90) millimeters of mercury (mm Hg) or change in supine and standing SBP more than or equal to (>=) 30 mm Hg; supine and standing diastolic blood pressure (DBP) of < 50 mm Hg or change in supine and standing DBP of >= 20 mm Hg; supine and standing pulse rate of < 40 or >120 beats per minute (bpm). Figure 99999 signifies data not measurable/applicable. Maximum Decrease is abbreviated as Max.Dec., and Maximum Increase is abbreviated as Max.Inc. n is the number of participants contributing to the parameter, not applicable is abbreviated as N/A." (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose.

InterventionParticipants (Count of Participants)
Supine SBP (mmHg) <90Supine DBP (mmHg) <50Supine PR (BPM) >120Supine PR (BPM) <40Max.Dec. From Baseline in Supine SBP (mm Hg) >=30Max.Dec. From Baseline in Supine DBP (mm Hg) >=20Max.Inc. From Baseline in Supine SBP (mm Hg) >=30Max.Inc. From Baseline in Supine DBP (mm Hg) >=20
PF-06463922 100 mg00000000

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Number of Participants With Changes From Baseline and Absolute Values in Vital Signs Meeting the Criteria of Potentially Significant Clinical Concerns

"Criteria for potentially clinically important changes in vital signs were defined as: supine and standing systolic blood pressure (SBP) of less than (<90) millimeters of mercury (mm Hg) or change in supine and standing SBP more than or equal to (>=) 30 mm Hg; supine and standing diastolic blood pressure (DBP) of < 50 mm Hg or change in supine and standing DBP of >= 20 mm Hg; supine and standing pulse rate of < 40 or >120 beats per minute (bpm). Figure 99999 signifies data not measurable/applicable. Maximum Decrease is abbreviated as Max.Dec., and Maximum Increase is abbreviated as Max.Inc. n is the number of participants contributing to the parameter, not applicable is abbreviated as N/A." (NCT02804399)
Timeframe: Baseline to about 18 days after the first PF-06463922 dose.

InterventionParticipants (Count of Participants)
Supine SBP (mmHg) <90Standing SBP (mmHg) <90Supine DBP (mmHg) <50Standing DBP (mmHg) <50Supine PR (BPM) >120Supine PR (BPM) <40Standing PR (BPM) >120Standing PR (BPM) <40Max.Dec. From Baseline in Supine SBP (mm Hg) >=30Max.Dec. From Baseline in Supine DBP (mm Hg) >=20Max.Inc. From Baseline in Supine SBP (mm Hg) >=30Max.Inc. From Baseline in Supine DBP (mm Hg) >=20
Rifampin 600 mg + PF-06463922 100 mg100000000010

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Plasma Vz/F for PF-06463922 Given Alone and With Rifampin

Vz/F is the apparent volume of distribution (only after single dose).The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg administration with rifampin in Period 2.

Interventionliter (Geometric Mean)
PF-06463922 100 mg342.6
Rifampin 600 mg + PF-06463922 100 mg1095

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Plasma Tmax for PF-06895751 When PF-06463922 Given Alone and With Rifampin.

Tmax was the time for maximum observed plasma concentration (Cmax). The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. PF-06895751 was the metabolite of PF-06463922. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionhr (Median)
PF-06463922 100 mg30.1
Rifampin 600 mg + PF-06463922 100 mg12.0

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Plasma t1/2 for PF-06895751 When PF-06463922 Given Alone and With Rifampin

T1/2 was the terminal plasma half-life. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. PF-06895751 was the metabolite of PF-06463922. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionhr (Mean)
PF-06463922 100 mg29.14
Rifampin 600 mg + PF-06463922 100 mg18.43

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Plasma t1/2 for PF-06463922 Given Alone and With Rifampin

Terminal plasma half-life (t1/2) is the time measured for the plasma concentration of drug to decrease by one half. The PK parameter analysis population is defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionhr (Mean)
PF-06463922 100 mg21.22
Rifampin 600 mg + PF-06463922 100 mg10.16

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Plasma Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for Cmax (MRCmax) of PF-06463922 and Its Metabolite: When PF-06463922 Given Alone and With Rifampin

Cmax was the maximum observed plasma concentration of PF-06463922 and PF-06895751 ( metabolite of PF-06463922). The molecular weight adjusted metabolite/parent ratio (PF-06895751/PF-06463922) for Cmax was presented. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionratio (Geometric Mean)
PF-06463922 100 mg0.2094
Rifampin 600 mg + PF-06463922 100 mg1.136

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Plasma Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for AUClast (MRAUClast) of PF-06463922 and Its Metabolite: When PF-06463922 Given Alone and With Rifampin

AUClast was the plasma area under the plasma concentration-time profile from time 0 to the time of the last quantifiable concentration of PF-06463922 and PF-06895751 ( metabolite of PF-06463922). The molecular weight adjusted metabolite/parent ratio (PF-06895751/PF-06463922) for AUClast was presented. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. PF-06895751 was the metabolite of PF-06463922. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionratio (Geometric Mean)
PF-06463922 100 mg1.053
Rifampin 600 mg + PF-06463922 100 mg5.831

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Plasma Molecular Weight Adjusted Metabolite to Parent (M/P) Ratio for AUCinf (MRAUCinf) of PF-06463922 and Its Metabolite: When PF-06463922 Given Alone and With Rifampin

AUCinf was the plasma area under the plasma concentration-time profile from time 0 extrapolated to infinite time of PF-06463922 and PF-06895751 ( metabolite of PF-06463922). The molecular weight adjusted metabolite/parent ratio (PF-06895751/PF-06463922) for AUCinf was presented. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionratio (Geometric Mean)
PF-06463922 100 mg1.166
Rifampin 600 mg + PF-06463922 100 mg5.521

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Plasma Cmax for PF-06895751 When PF-06463922 Given Alone and With Rifampin

Cmax was the maximum observed plasma concentration. The PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. PF-06895751 was the metabolite of PF-06463922. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionng/mL (Geometric Mean)
PF-06463922 100 mg59.02
Rifampin 600 mg + PF-06463922 100 mg76.45

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Plasma Cmax for PF-06463922 Given Alone and With Rifampin

Cmax is the maximum observed plasma concentration. PK parameter analysis population was defined as all participants enrolled and treated who have at least 1 of the PF-06463922 PK parameters of primary interest in at least 1 treatment period. (NCT02804399)
Timeframe: Predose, 0.5, 1, 1.5, 2, 4, 6, 12, 24, 36, 48, 60, 72, 96, 120 hours postdose on Day 1 after PF-06463922 100 mg administration in Period 1, and at the same time points on Day 8 after PF-06463922 100 mg with rifampin administration in Period 2.

Interventionng/mL (Geometric Mean)
PF-06463922 100 mg621.4
Rifampin 600 mg + PF-06463922 100 mg148.4

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Comparison of the Rate of Treatment Success at 18 Months (After Treatment Initiation) Between Arms B and C

Estimation of the lower bound of a one-sided 95% confidence interval of the difference in success rates between arms B and C. If the lower bound is greater than -7%, this will be evidence that the treatment-shortening arm is not inferior to the standard duration arm. (NCT02821832)
Timeframe: 18 months

,,
InterventionParticipants (Count of Participants)
CuredConfirmed relapsesLate withdrawal, lost to follow-upProbable relapsesTreatment Failure
Arm A21751311
Arm B1211910
Arm C1179634

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Number of Participants With Clinical Significance Abnormalities in Laboratory Parameters

Chemistry:(sodium135-146,potassium3.5-5.5,chloride95-109,glucose3.3-5.5,urea2.8-7.2,calcium2.2-2.65,phosphate0.8-1.45,triglyceride0.4-1.7,cholesterol2.6-5.2)millimoles/L, (bilirubin[direct0-3,total2-21],creatinine53- 110)micromole/L, (albumin35-52,protein65-83)g/L,(alkaline phosphatase30-120, aspartate amino[A]transferase[T]4-46, alanine AT4-49, lactic acid dehydrogenase200-460, gammaglutamylT7-50,creatinine kinase24-170)U/L. Hematology: hemoglobin(Hb)120-177, hematocrit0.35-0.49L/L, RBC4-5.9T/L, (platelet150- 400,WBC4-10,basophil<0.10,eosinophil<0.40, neutrophil1.50-7.00,monocyte<1.20,lymphocyte1.0 -3.70)G/L. Urine:(glucose,protein,ketone,Hb:negative/positive), specific gravity1.010-1.030g/cm^3, pH4.8-7.8, pale yellow-deep amber, microscopy[WBC0-5,leukocyte0-5,Hb0-3,cast0-1,bacteria0-500,epithelial0-6])Pcs/area. Coagulation:(activated partial thromboplastine time25-43,prothrombin time13.7-15.6) seconds,international normalized ratio0.89-1.1. Investigator judged clinical significance. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone3
Itraconazole 100 mg BID Alone0
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1
Talazoparib 1.0 mg Alone2
Rifampin 600 mg QD Alone1
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD1

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Number of Participants With Treatment Emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

An AE was any untoward medical occurrence in a participant who received study treatment without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death, initial or prolonged inpatient hospitalization, life-threatening experience (immediate risk of dying), persistent or significant disability or incapacity, congenital anomaly. A TEAE was defined as an event that emerged during the treatment period that was absent before treatment, or worsened during the treatment period relative to the pre-treatment state. AEs included both serious and non-serious adverse events. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

,,,,,
InterventionParticipants (Count of Participants)
AEsSAEs
Itraconazole 100 mg BID Alone30
Rifampin 600 mg QD Alone92
Talazoparib 0.5 mg Alone123
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID51
Talazoparib 1.0 mg Alone60
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD50

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Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionHours (Median)
Talazoparib 1.0 mg Alone1.00
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD1.00

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Number of Participants With Clinically Significant Physical Examination Findings

Physical examination included examination of abdomen, cardiovascular, eyes, ears, nose, throat, general appearance, head, neck, thyroid, lymph nodes, musculoskeletal, neurological, skin / subcutaneous tissue, thorax / lungs, abdomen including spleen size, breasts (female only) and respiratory. Clinical significance of physical examination was judged by investigator. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone0
Itraconazole 100 mg BID Alone0
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1
Talazoparib 1.0 mg Alone1
Rifampin 600 mg QD Alone0
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD0

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Time to Attain Maximum Observed Plasma Concentration (Tmax) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionHours (Median)
Talazoparib 0.5 mg Alone1.00
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1.02

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Area Under the Plasma Concentration-Time Curve From Time Zero to Extrapolated Infinite Time (AUC0-inf) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

Interventionhr*pg/mL (Geometric Mean)
Talazoparib 1.0 mg Alone209521.62
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD194307.67

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Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Itraconazole

"Clearance of talazoparib was measure of the rate at which it was metabolized or eliminated by normal biological processes. T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionLiter per hour (Geometric Mean)
Talazoparib 0.5 mg Alone4.55
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID3.29

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Apparent Clearance (CL/F) of Talazoparib: Alone and in Combination With Rifampin

"Clearance of talazoparib was measure of the rate at which it was metabolized or eliminated by normal biological processes. T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionLiter per hour (Geometric Mean)
Talazoparib 1.0 mg Alone4.77
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD5.15

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Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Itraconazole

"Apparent volume of distribution was defined as the theoretical volume in which the total amount of talazoparib would need to be uniformly distributed to produce its desired plasma concentration. T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionLiter (Geometric Mean)
Talazoparib 0.5 mg Alone644.81
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID552.01

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Apparent Volume of Distribution During Terminal Phase (Vz/F) of Talazoparib: Alone and in Combination With Rifampin

"Apparent volume of distribution was defined as the theoretical volume in which the total amount of talazoparib would need to be uniformly distributed to produce its desired plasma concentration. T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionLiter (Geometric Mean)
Talazoparib 1.0 mg Alone623.89
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD588.14

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Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Itraconazole

"Terminal elimination half-life was defined as time measured for the plasma concentration of talazoparib to decrease by one half. T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionHours (Mean)
Talazoparib 0.5 mg Alone101.26
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID118.47

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Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionHour*picogram per milliliter (hr*pg/mL) (Geometric Mean)
Talazoparib 0.5 mg Alone98532.30
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID145944.59

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Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Concentration (AUC0-last) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

Interventionhr*pg/mL (Geometric Mean)
Talazoparib 1.0 mg Alone196631.34
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD196100.69

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Area Under the Plasma Concentration-Time Profile From Time Zero to Extrapolated Infinity (AUC0-inf) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

Interventionhr*pg/mL (Geometric Mean)
Talazoparib 0.5 mg Alone109762.10
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID151919.63

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Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Itraconazole

"T1= Time frame for Talazoparib 0.5 mg Alone and T2= time frame for Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID." (NCT03077607)
Timeframe: T1=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T2=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 23

InterventionPicogram per milliliter (pg/mL) (Geometric Mean)
Talazoparib 0.5 mg Alone2092.00
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID2936.82

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Maximum Observed Plasma Concentration (Cmax) of Talazoparib: Alone and in Combination With Rifampin

"T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

Interventionpg/mL (Geometric Mean)
Talazoparib 1.0 mg Alone6007.01
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD8336.83

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Terminal Elimination Half-Life (t1/2) of Talazoparib: Alone and in Combination With Rifampin

"Terminal elimination half-life was defined as time measured for the plasma concentration of talazoparib to decrease by one half. T3= Time frame for Talazoparib 1.0 mg Alone and T4= time frame for Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD." (NCT03077607)
Timeframe: T3=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 1; T4=Predose, 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 168, 216, 264 and 336 hours post Talazoparib dose on Day 25

InterventionHours (Mean)
Talazoparib 1.0 mg Alone92.05
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD80.61

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Number of Participants With Clinically Significant Abnormalities in Electrocardiogram (ECG)

ECG abnormalities: a) QT Interval: new absolute values greater than (>) 450, >480, >500 milliseconds (msec), increase from baseline >30 and >60 msec, b) QT interval using Fridericia's correction (QTcF) Interval: new absolute values >450, >480, >500 msec, increase from baseline >30 and > 60 msec, c) Heart rate: increase from baseline >25 percentage (%) and to a value >100 bpm, decrease from baseline >25% and to a value <50 bpm, d) PR Interval: increase from baseline > 25% and to a value >200 msec, e) QRS duration: increase from baseline > 25% and to a value >100 msec. Clinical significance of ECG abnormalities was judged by investigator. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone0
Itraconazole 100 mg BID Alone1
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID0
Talazoparib 1.0 mg Alone0
Rifampin 600 mg QD Alone0
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD0

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Number of Participants With Clinically Significant Abnormalities in Vital Signs

Vital sign abnormalities: a) systolic blood pressure (SBP): 1) minimum less than (<) 90 millimeter of mercury (mmHg), 2) change from baseline maximum decrease greater than equal to (>=) 30 mmHg, 3) change from baseline maximum increase >=30 mmHg; b) diastolic blood pressure (DBP): 1) minimum <50 mmHg, 2) change from baseline maximum decrease >=20 mmHg, 3) change from baseline maximum increase >=20 mmHg; c) supine pulse rate: 1) minimum <40 beats per minute (bpm), 2) maximum >120 bpm; d) standing pulse rate: 1) minimum <40 bpm and 2) maximum >140 bpm. Clinical significance of vital signs abnormalities was judged by investigator. (NCT03077607)
Timeframe: Baseline up to end of study (up to 61 days)

InterventionParticipants (Count of Participants)
Talazoparib 0.5 mg Alone0
Itraconazole 100 mg BID Alone0
Talazoparib 0.5 mg in Combination With Itraconazole 100 mg BID1
Talazoparib 1.0 mg Alone0
Rifampin 600 mg QD Alone0
Talazoparib 1.0 mg in Combination With Rifampin 600 mg QD1

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Estimate the Antimycobacterial Activity Based on Liquid Culture Time-to-positivity

Change in time-to-positivity in Mycobacteria Growth Indicator Tube (MGIT) liquid media over 14 days of treatment (EBA0-14(TTP)) (time to positivity) for the study treatments. The Early Bactericidal Activity (EBA) over a 14 days period (EBA0-14), as determined by the median rate of change in TTP (expressed in log10 hours/day). A non-linear mixed effects model of log10 hours/day on time was developed using aggregated participant data for each treatment arm. A basic model was developed based on mono- or bi-exponential bacterial killing functions. Afterwards, covariate modelling to identify relationships between demographics, disease severity, secondary pharmacokinetic summary indices (area under the curve from time 0 to last measured concentration (AUC0-last) and maximum observed plasma concentration (Cmax), and model parameters describing TTP over time was performed. Finally, the treatment regimen was tested using different functions supported by the graphical analysis. (NCT03174184)
Timeframe: 14 days

Interventionrate of change in log10 hours/day (Mean)
Rifampin Resistant A0.19
Rifampin Resistant B0.31
Rifampin Susceptible C0.53
Rifampin Susceptible D0.20
Rifampin Susceptible E0.09
Rifampin Susceptible F0.09

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Distribution of Minimum Inhibitory Concentration (MIC) of Rifampin

The distribution of rifampin MIC in the drug-resistant arms (NCT03174184)
Timeframe: 14 days

Interventionmcg/mL (Median)
Rifampin Resistant A1.28
Rifampin Resistant B1.28

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Estimate of the 14-day Early Bactericidal Activity (EBA), Based on Colony Forming Unit Counts, of the Combination of Meropenem and Amoxicillin/Clavulanate, Without Versus With Rifampin

The Early Bactericidal Activity (EBA) over a 14 days period (EBA0-14), as determined by the median rate of change in log10 Colony Forming Units (CFU) per mL sputum. A non-linear mixed effects model of log10 CFU/mL sputum on time was developed using aggregated participant data for each treatment arm. A basic model was developed based on mono- or bi-exponential bacterial killing functions. Afterwards, covariate modelling to identify relationships between demographics, disease severity, secondary pharmacokinetic summary indices (area under the curve from time 0 to last measured concentration (AUC0-last) and maximum observed plasma concentration (Cmax), and model parameters describing log10 CFU/mL sputum over time was performed. Finally, the treatment regimen was tested using different functions supported by the graphical analysis. (NCT03174184)
Timeframe: 14 days

Interventionrate of change in log10 CFU/mL/day (Mean)
Rifampin Resistant A-0.06
Rifampin Resistant B-0.11
Rifampin Susceptible C-0.14
Rifampin Susceptible D-0.12
Rifampin Susceptible E-0.05
Rifampin Susceptible F-0.02

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AUC for Rifampin

Rifampin AUC0-last in Arms A and C (NCT03174184)
Timeframe: 14 days

Interventionh*mg/L (Mean)
Rifampin Resistant A105
Rifampin Susceptible C109

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Frequency of Grade 2 or Higher Adverse Events

Grade 2 or higher Adverse Events (AE) that constitute any untoward medical occurrence in a study participant and which does not necessarily have a causal relationship with this treatment. An adverse event can therefore be any unfavorable and unintended sign (including an abnormal laboratory finding), symptom, or disease temporally associated with the use of a medicinal product, whether or not related to the medicinal product. (NCT03174184)
Timeframe: From the time a study participant receives the first dose of study drug through the final study visit, up to 28 days

InterventionEvents (Number)
Rifampin Resistant A28
Rifampin Resistant B15
Rifampin Susceptible C5
Rifampin Susceptible D8
Rifampin Susceptible E3
Rifampin Susceptible F7

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AUC0-inf (Area Under the Plasma Concentration-time Curve From Time 0 to Infinity)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

Interventionhr*ng/mL (Geometric Mean)
Study 1: Bexagliflozin Alone1118.741
Study 1: Bexagliflozin/Probenecid1583.188
Study 2: Bexagliflozin Alone698.254
Study 2: Bexagliflozin/Rifampin601.334
Study 3: Bexagliflozin Alone1025.101
Study 3: Bexagliflozin/Verapamil1003.931

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Urinary Glucose Excretion 0-48 hr

Pre-dose urine samples were collected from -12 to 0 h for baseline measurement of pharmacodynamic parameters. Post-dose urine samples were collected without preservative in four batches: 0 to 12 h, 12 to 24 h, 24 to 36h, and 36 to 48 h after dosing. Urine aliquots were prepared from well mixed collections for the assessment of pharmacodynamics. (NCT03296800)
Timeframe: 0 to 48 hours

,,,,,
Interventiong (Mean)
Pre-dose (-12 - 0 hours)0 - 12 hours post-dose12 - 24 hours post-dose24 - 36 hours post-dose36 - 48 hours post-dose0 - 24 hours post-dose0 - 48 hours post-dose
Bexagliflozin/Probenecid0.4725.9020.9222.109.5346.8278.44
Bexagliflozin/Rifampin0.1231.4015.7216.323.4147.1266.86
Bexagliflozin/Verapamil1.3731.4620.5120.944.7851.9777.69
Study 1: Bexagliflozin Alone0.0225.0421.2822.0411.1547.7381.67
Study 2: Bexagliflozin Alone0.0231.5019.4321.516.9950.9379.43
Study 3: Bexagliflozin Alone0.0231.1422.3024.5411.3153.4489.29

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Tmax (Time of Maximum Observed Plasma Concentration)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

,,
Interventionhours (Median)
Bexagliflozin aloneBexagliflozin + additional drug
Bexagliflozin/Probenecid2.0003.000
Bexagliflozin/Rifampin2.0002.000
Bexagliflozin/Verapamil3.03.000

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T1/2 (Apparent Terminal Elimination Half-life)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

,,
Interventionhours (Geometric Mean)
Bexagliflozin aloneBexagliflozin + additional drug
Bexagliflozin/Probenecid12.09013.894
Bexagliflozin/Rifampin12.1905.318
Bexagliflozin/Verapamil10.70911.675

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Cmax (Maximum Observed Plasma Concentration)

Whole venous blood samples of 3 mL were collected from a peripheral vein prior to dosing and at 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, 24, 36, and 48 h after administration of bexagliflozin; On Day 1 and Day 5 for Study 1, Day 1 and Day 6 for Study 2, Day 1 and Day 4 for Study 3. The pharmacokinetic parameters were estimated from the bexagliflozin plasma concentration data for each subject by non-compartmental analysis (NCA). (NCT03296800)
Timeframe: Up to 48 hours

Interventionng/mL (Geometric Mean)
Study 1: Bexagliflozin Alone161.675
Study 1: Bexagliflozin and Probenecid193.366
Study 2: Bexagliflozin Alone97.811
Study 2: Bexagliflozin and Rifampin117.001
Study 3: Bexagliflozin Alone159.355
Study 3: Bexagliflozin and Verapamil169.000

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T4 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)188.111330.47113.78
Probenecid + R1 (T4)489.281346.62244.94

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T4 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.3090.00243.4910.11
Probenecid + R1 (T4)1.13110.64246.7843.29

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T3 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)1.6597.69316.8313.21
Cocktail (R1)1.3593.23258.3311.30

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T1 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.1788.59223.786.84
Verapamil + R1 (T1)1.4284.32179.457.90

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Verapamil + R1 (T1) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. Geometric mean (gMean) presented here is an adjusted gMean and standard error (SE) presented is a geometric SE (gSE). (NCT03307252)
Timeframe: Samples were taken within 0:20 hour:minutes (hh:mm) prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.61176.851357.3487.29
Verapamil + R1 (T1)13.71165.801126.2298.98

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Rifampin + R1 (T2) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.61176.851357.3487.29
Rifampin + R1 (T2)17.89211.821473.38303.81

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Probenecid + R1 (T4) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)13.52177.961321.20106.69
Probenecid + R1 (T4)14.44483.381331.83238.16

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Maximum Measured Concentration of the Analytes: Digoxin, Furosemide, Metformin, and Rosuvastatin (Cmax) (T2 vs. R1)

Cmax, maximum measured concentration of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole/ litre (nmol/ L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cocktail (R1)1.1788.59223.786.84
Rifampin + R1 (T2)2.55119.66251.3277.00

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T3 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)202.172023.33148.32
Cocktail (R1)200.611540.21139.21

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T2 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)191.291365.8594.14
Rifampin + R1 (T2)215.631482.76320.72

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞) (T1 vs. R1)

AUC0-∞, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 extrapolated to infinity is presented. AUC0-∞ not displayed for Digoxin analyte as precision was considered non-sufficient. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
FurosemideMetforminRosuvastatin
Cocktail (R1)191.291365.8594.14
Verapamil + R1 (T1)176.441147.23116.80

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Area Under the Concentration-time Curve of the Analyte in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz) (Cimetidine + R1 (T3) vs. R1)

AUC0-tz, area under the concentration-time curve of the analytes: digoxin, furosemide, metformin, and rosuvastatin (at cocktail doses) in plasma over the time interval from 0 to the last quantifiable data point is presented. gMean presented here is an adjusted gMean and SE presented is a gSE. (NCT03307252)
Timeframe: Samples were taken within 0:20 hh:mm prior to first study drug administration and at 0:20, 0:40, 1:00, 1:30, 2:00, 2:30, 3:00, 4:00, 5:00, 6:00, 8:00, 10:00, 11:00, 12:00, 24:00, 36:00, 47:00, 71:00 and 95:00 after drug administration.

,
InterventionNanomole*hour/litre (nmol*h/L) (Geometric Mean)
DigoxinFurosemideMetforminRosuvastatin
Cimetidine + R1 (T3)19.03196.392006.60139.54
Cocktail (R1)15.15194.051532.41129.90

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Effect of Rifampin on Cmax Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the Cmax of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. Cmax is the peak plasma concentration of study drug after administration. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionpg/mL (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)81.4351599102405198236
Mild Impairment (Period 2)73.0243819131505215254
Moderate Impairment (Period 2)92.5443860119508174396
Severe Impairment (Period 2)75.442298188.4531150208

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Effect of Rifampin on CL/F Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the CL/F of midazolam, dabigatran, pitavastatin, atorvastatin, and rosuvatatin. CL/F is the rate at which study drug was removed from the body. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionliters/hour (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinAtorvastatinRosuvastatin
Healthy Control (Period 2)41.885.65.2456.457.9
Mild Impairment (Period 2)53.092.83.9558.647.1
Moderate Impairment (Period 2)27.838.92.8641.128.9
Severe Impairment (Period 2)40.526.33.5744.238.6

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Effect of Rifampin on C24 Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the C24 of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. C24 is a measure of the plasma study drug concentration 24 hours post-dose. C24 is reported as median (minimum and maximum) in severe renal impairment arm due to zero values. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: 24 hours post-dose

,,,
Interventionpg/mL (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)0.60127.54.7217.11.355.572.42
Mild Impairment (Period 2)0.0031.14.7020.71.766.284.18
Moderate Impairment (Period 2)1.4210010.534.02.989.966.97
Severe Impairment (Period 2)0.3941747.0121.32.987.234.47

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Effect of Rifampin on AUC0-last Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the AUC0-last of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. AUC0-last is the area under the plasma concentration-time curve from time zero to time of last measurable concentration. It is a measure of the amount of study drug in the blood plasma from pre-dose until the last measurable concentration of study drug could be determined. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0 hour (pre-dose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0 hour (pre-dose) and 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionpg*hr/mL (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)23131401890127017601630854
Mild Impairment (Period 2)182283025101850169017501040
Moderate Impairment (Period 2)353683034802380242018501740
Severe Impairment (Period 2)2361040028501470222016101150

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Apparent Clearance After Extravascular Administration (CL/F) Post-dose Period 1

CL/F is the rate at which study drug was removed from the body. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. CL/F was to be calculated for the parent plasma analytes only, midazolam, dabigatran, pitavastatin, atorvastatin, and rosuvastatin. (NCT03311841)
Timeframe: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionliters/hour (Geometric Mean)
MidazolamDabigatranPitavastatinAtorvastatinRosuvastatin
End-Stage Renal Disease90.852.514.8304240
Healthy Control36.617819.2343171
Mild Impairment56.917514.5304191
Moderate Impairment27.561.89.8419687.0
Severe Impairment38.535.715.4210137

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Effect of Rifampin on AUC0-inf Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the AUC0-inf of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. AUC0-inf is the area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include data from the end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0 hour (pre-dose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0 hour (pre-dose) and 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionpg*hr/mL (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)23932901910134017701650830
Mild Impairment (Period 2)189304025301930171017601060
Moderate Impairment (Period 2)359724035002500243018701800
Severe Impairment (Period 2)2441070028501560224016201240

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Effect of Rifampin on AUC0-24 Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the AUC0-24 of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. AUC0-24 is the area under the plasma concentration-time curve from time 0 to 24 hours post-dose. This is a measure of the average amount of study drug in the blood plasma over a period of 24 hours after the dose. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0 hour (pre-dose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, and 24 hours post-dose; rifampin: 0 hour (pre-dose) and 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionpg*hr/mL (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)23430301860100017601620842
Mild Impairment (Period 2)186266024601490170017201010
Moderate Impairment (Period 2)346548033601780242018001670
Severe Impairment (Period 2)238654027601070223015801100

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Area Under the Plasma Concentration-time Curve From Time 0 to Last (AUC0-last) Post-dose Period 1

AUC0-last is the area under the plasma concentration-time curve from time zero to time of last measurable concentration. This is a measure of the amount of study drug in the blood plasma from pre-dose until the last measurable concentration of study drug could be determined. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. (NCT03311841)
Timeframe: 0 hour (pre-dose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionpg*hr/mL (Geometric Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease10537406491060298126171
Healthy Control26414104831450255152181
Mild Impairment16714406431490295221231
Moderate Impairment34442309502020459256479
Severe Impairment24874506021570419176269

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Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC0-inf) Post-dose Period 1

AUC0-inf is the area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease (ESRD) requiring hemodialysis. (NCT03311841)
Timeframe: 0 hour (pre-dose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionpg*hr/mL (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease11053706761100329163208
Healthy Control27315805201540292208292
Mild Impairment17616106881610329286262
Moderate Impairment364455010202240511273575
Severe Impairment26079006481680476226365

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Area Under the Plasma Concentration-time Curve From Time 0 to 24 Hours (AUC0-24) Post-dose Period 1

AUC0-24 is the area under the plasma concentration-time curve from time 0 to 24 hours post-dose. This is a measure of the average amount of study drug in the blood plasma over a period of 24 hours after the dose. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. (NCT03311841)
Timeframe: 0 hour (pre-dose) and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, and 24 hours post-dose

,,,,
Interventionpg*hr/mL (Geometric Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease1062100593858287115162
Healthy Control25214404151010198108153
Mild Impairment16813805431040219139191
Moderate Impairment31734407641280329143343
Severe Impairment23544705251100300112223

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Apparent Volume of Distribution During the Terminal Phase (Vz/F) Post-dose Period 1

Vz/F is the distribution of study drug between the plasma and the rest of the body after the dose. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. Vz/F was to be calculated for the parent plasma analytes only, midazolam, dabigatran, pitavastatin, atorvastatin, and rosuvastatin. (NCT03311841)
Timeframe: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionliters (Geometric Mean)
MidazolamDabigatranPitavastatinAtorvastatinRosuvastatin
End-Stage Renal Disease579314025235204870
Healthy Control422173049573804010
Mild Impairment555212040573004270
Moderate Impairment409106031752403120
Severe Impairment433123045453103720

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Apparent Plasma Terminal Half-life (t1/2) Post-dose Period 1

T1/2 is the elimination half-life of study drug. T1/2 is the time it takes for half of the study drug in the blood plasma to dissipate. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. (NCT03311841)
Timeframe: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionhours (Geometric Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease4.4141.411.811.08.0312.414.0
Healthy Control7.996.7517.818.514.921.216.2
Mild Impairment6.768.4019.320.516.722.815.5
Moderate Impairment10.311.922.422.018.624.624.9
Severe Impairment7.7924.020.418.117.521.918.8

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Effect of Rifampin on t1/2 Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the t1/2 of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. T1/2 is the elimination half-life of study drug. T1/2 is the time it takes for half of the study drug in the blood plasma to dissipate. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionhours (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)4.976.486.5016.52.763.496.76
Mild Impairment (Period 2)4.127.578.4021.03.223.839.64
Moderate Impairment (Period 2)5.4911.311.517.72.994.257.48
Severe Impairment (Period 2)4.1419.46.9917.23.144.564.89

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Effect of Rifampin on Tmax Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the Tmax of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. Tmax is the amount of time to reach maximum (peak) plasma drug concentration following drug administration. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionhours (Median)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
Healthy Control (Period 2)1.002.501.002.001.503.002.00
Mild Impairment (Period 2)0.502.501.003.001.001.751.00
Moderate Impairment (Period 2)0.753.001.004.001.502.502.00
Severe Impairment (Period 2)0.503.501.003.000.501.751.00

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Effect of Rifampin on Vz/F Post-dose Period 2

To evaluate the effect of a single oral dose of rifampin on the Vz/F of midazolam, dabigatran, pitavastatin, pitavastatin lactone, atorvastatin, ortho-hydroxyatorvastatin, and rosuvatatin. Vz/F is the distribution of study drug between the plasma and the rest of the body after the dose. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail and rifampin in healthy participants and participants with renal impairment. As pre-specified in the protocol, this outcome measure does not include end-stage renal disease participants as they did not receive rifampin during Period 2. (NCT03311841)
Timeframe: Microdose cocktail: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose; rifampin: 0.5, 1, 1.5, 2, 3, 4, 6, 12, and 24 hours post-dose

,,,
Interventionliters (Geometric Least Squares Mean)
MidazolamDabigatranPitavastatinAtorvastatinRosuvastatin
Healthy Control (Period 2)30080049.2225565
Mild Impairment (Period 2)315101047.8272654
Moderate Impairment (Period 2)22063247.3177313
Severe Impairment (Period 2)24273336.0200272

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Maximum Plasma Concentration (Cmax) Post-dose Period 1

Cmax is the peak plasma concentration of study drug after administration. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. (NCT03311841)
Timeframe: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionpg/mL (Geometric Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease39.913224278.563.78.5822.5
Healthy Control73.218316488.121.67.6721.5
Mild Impairment70.715324410531.98.5023.6
Moderate Impairment77.231230310655.09.5040.4
Severe Impairment68.431921895.446.77.2224.4

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Plasma Concentration at 24 Hours (C24) Post-dose Period 1

C24hr is a measure of the plasma study drug concentration 24 hours post-dose. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. (NCT03311841)
Timeframe: 24 hours post-dose

,,,,
Interventionpg/mL (Geometric Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease0.28370.26.0712.94.283.672.64
Healthy Control1.577.704.1021.73.853.081.94
Mild Impairment0.73418.75.3222.45.045.023.59
Moderate Impairment2.6459.38.1332.86.034.436.01
Severe Impairment1.831074.0423.25.733.253.40

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Time to Maximum Plasma Concentration (Tmax) Post-dose Period 1

Tmax is the amount of time to reach maximum (peak) plasma drug concentration following drug administration. Plasma pharmacokinetic data presented in the table below are following the administration of a single oral dose of a microdose cocktail in healthy participants, participants with renal impairment, and 24 hours prior to hemodialysis in participants with end-stage renal disease requiring hemodialysis. (NCT03311841)
Timeframe: 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 16, 24, 32, 48, and 72 hours post-dose

,,,,
Interventionhours (Geometric Mean)
MidazolamDabigatranPitavastatinPitavastatin lactone (metabolite)AtorvastatinOrtho-hydroxyatorvastatin (metabolite)Rosuvastatin
End-Stage Renal Disease0.502.000.502.500.255.003.00
Healthy Control1.001.500.752.000.506.003.50
Mild Impairment0.501.500.522.000.256.002.00
Moderate Impairment0.502.501.002.500.256.004.00
Severe Impairment0.503.000.504.000.256.004.00

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Time to Culture Negative Status

Culture conversion is a diagnostic criteria indicating the point at which samples taken from a patient infected with a tuberculosis can no longer produce tuberculosis cell cultures, that point is considered culture negativity (NCT03338621)
Timeframe: During treatment (17 or 26 weeks)

Interventionweeks (Median)
Drug Sensitive-TB BPaMZ6
Drug Sensitive-TB 2HRZE/4HR11
Drug Resistant-TB BPaMZ5

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Number of Participants With Culture Negative Status by 8 Weeks

Culture negative status is achieved when a participant produces at least two negative culture results at different visits (at least 7 days apart) without an intervening positive culture result for M.tb. (NCT03338621)
Timeframe: Days 0-56 (8 weeks)

InterventionParticipants (Count of Participants)
Drug Sensitive-TB 2HRZE/4HR70
Drug Sensitive-TB 4BPaMZ122

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Part A: Ratio of Maximum Observed Plasma Concentration (Cmax) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)

The Least square (LS) means ratio of Day 10 over Day 1 were calculated from a mixed-model analysis of variance model. (NCT03486314)
Timeframe: Days 1 and 10 pre-dose and at multiple time points (up to 48 hours) post-dose

Interventionratio (Least Squares Mean)
Part A: Pevonedistat 50 mg/m^2 + Rifampin 600 mg0.962

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Part A: Terminal Disposition Phase Half-life (T1/2z) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)

(NCT03486314)
Timeframe: Days 1 and 10 pre-dose and at multiple time points (up to 48 hours) post-dose

Interventionhour (Mean)
Pevonedistat without rifampin (Day 1)Pevonedistat with rifampin (Day 10)
Part A: Pevonedistat 50 mg/m^2 + Rifampin 600 mg7.4425.708

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Part A: Total Clearance After Intravenous Administration (CL) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)

(NCT03486314)
Timeframe: Days 1 and 10 pre-dose and at multiple time points (up to 48 hours) post-dose

Interventionliter per hour (L/h) (Mean)
Pevonedistat without rifampin (Day 1)Pevonedistat with rifampin (Day 10)
Part A: Pevonedistat 50 mg/m^2 + Rifampin 600 mg35.2243.77

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Part A: Volume of Distribution at Steady State After Intravenous Administration (Vss) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)

(NCT03486314)
Timeframe: Days 1 and 10 pre-dose and at multiple time points (up to 48 hours) post-dose

Interventionliter (Mean)
Pevonedistat without rifampin (Day 1)Pevonedistat with rifampin (Day 10)
Part A: Pevonedistat 50 mg/m^2 + Rifampin 600 mg312.82296.10

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Part B: Number of Participants With Best Overall Response as Per Investigator's Assessment

Best overall response was defined as participants with best response among complete response (CR) or partial response (PR) or stable disease (SD), or progressive disease (PD). It was assessed by investigator according to Response Evaluation Criteria in Solid Tumors (RECIST) version 1.1. CR: disappearance of all target lesions. Any pathological lymph nodes (whether target and non-target) must have reduction in short axis to less than (<) 10 millimeter (mm). PR: at least 30 percent (%) decrease in sum of diameter of target lesions, taking as reference baseline sum of diameter. SD: neither sufficient shrinkage to qualify for PR nor sufficient increase to qualify for PD, taking as reference smallest sum of diameter. PD: at least 20% increase in sum of diameter of target lesions, taking as reference, smallest sum on study. (NCT03486314)
Timeframe: Up to Cycle 17 (end of treatment) (Cycle length =21 days)

,
InterventionParticipants (Count of Participants)
CRPRSDPD
Part B: Pevonedistat 20 mg/m^2 + Carboplatin AUC5 + Paclitaxel 175 mg/m^20133
Part B: Pevonedistat 25 mg/m^2 + Docetaxel 75 mg/m^20222

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Part A: Ratio of Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration (AUClast) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)

The LS means ratio of Day 10 over Day 1 were calculated from a mixed-model analysis of variance model. (NCT03486314)
Timeframe: Days 1 and 10 pre-dose and at multiple time points (up to 48 hours) post-dose

Interventionratio (Least Squares Mean)
Part A: Pevonedistat 50 mg/m^2 + Rifampin 600 mg0.785

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Part A: Ratio of Area Under the Plasma Concentration-time Curve From Time 0 to Infinity (AUC∞) for Pevonedistat Without Rifampin (Day 1) and With Rifampin (Day 10)

The LS means ratio of Day 10 over Day 1 were calculated from a mixed-model analysis of variance model. (NCT03486314)
Timeframe: Days 1 and 10 pre-dose and at multiple time points (up to 48 hours) post-dose

Interventionratio (Least Squares Mean)
Part A: Pevonedistat 50 mg/m^2 + Rifampin 600 mg0.790

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Pharmacokinetics: Cmax of KD025m1 in Part 1

Maximum concentration (Cmax) of Metabolite 1 (KD025m1) for belumosudil alone and for belumosudil + rifampicin up to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose

Interventionng/mL (Geometric Mean)
Part 1, Period 1: Belumosudil Alone23.2
Part 1, Period 4: Belumosudil + Rifampicin52.5

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Pharmacokinetics: Cmax of KD025, KD025m1, and KD025m2 in Part 2

Maximum concentration (Cmax) of the parent drug (KD025), for Metabolite 1 (KD025m1), and for Metabolite 2 (KD025m2), for belumosudil alone and for belumosudil + omeprazole up to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22,24,36, and 48 hours post-dose

,
Interventionng/mL (Geometric Mean)
Cmax--1st dose: KD025Cmax--2nd dose: KD025Cmax--1st Dose: KD025m1Cmax--2nd Dose: KD025m1Cmax--1st Dose: KD025m2Cmax--2nd Dose: KD025m2
Part 2, Period 1: Belumosudil Alone1790176023.823.6282257
Part 2, Period 2: Belumosudil + Omeprazole57590318.018.972.3115

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Pharmacokinetics: Cmax of KD025 and KD025m2 in Part 1

Maximum concentration (Cmax) of the parent drug, KD025, Metabolite 1 (KD025m1), and Metabolite 2 (KD025m2) for belumosudil alone, belumosudil + itraconazole, belumosudil + rabeprazole, and belumosudil + rifampicin at 0 to 48 hours post-dose (NCT03530995)
Timeframe: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose

,,,
Interventionng/mL (Geometric Mean)
Parent Drug KD025KD025m2
Part 1, Period 1: Belumosudil Alone1770337
Part 1, Period 2: Belumosudil + Itraconazole2130221
Part 1, Period 3: Belumosudil + Rabeprazole22723.5
Part 1, Period 4: Belumosudil + Rifampicin712148

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Pharmacokinetics: AUC(0-inf) and AUC(0-24) of KD025 and KD025 m2 for Subject in Part 1 and Part 2

Area under concentration-time curve from zero hours to infinity (AUC[0-inf]) and from zero hours to 24 hours post-dose (AUC[0-24)) for the parent drug KD025, and Metabolite 2, KD025m2, for subjects up to 48 hours each for Part 1 and for Part 2 (NCT03530995)
Timeframe: Part 1: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,24,36, and 48 hours post-dose; Part 2: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22,24,36, and 48 hours post-dose

,,,,,
Intervention(ng*h)/mL (Geometric Mean)
AUC(0-inf): KD025AUC(0-inf): KD025m2AUC(0-24): KD025AUC(0-24): KD025m2
Part 1, Period 1: Belumosudil Alone9080123084301100
Part 1, Period 2: Belumosudil + Itraconazole1120084310400745
Part 1, Period 3: Belumosudil + Rabeprazole16801741510110
Part 1, Period 4: Belumosudil + Rifampicin25003962490376
Part 2, Period 1: Belumosudil Only188001900168001950
Part 2, Period 2: Belumosudil + Omeprazole988011107970767

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Pharmacokinetics: AUC(0-24) of KD025m1 for Part 1 and for Part 2

Area under concentration-time curve from zero hours to 24 hours post-dose (AUC[0-24]) for Metabolite 1, KD025m1, for subjects in Part 1 and for subjects in Part 2 (NCT03530995)
Timeframe: Part 1: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12, and 24 hours post-dose; Part 2: Pre-dose and 0.5,1,1.5,2,3,4,5,6,8,10,12,12.5,13,13.5,14,15,16,17,18,20,22, and 24 hours post-dose

Intervention(ng*h)/mL (Geometric Mean)
Part 1, Period 1: Belumosudil Alone75.6
Part 1, Period 4: Belumosudil + Rifampicin148
Part 2, Period 1: Belumosudil Alone138
Part 2, Period 2: Belumosudil + Omeprazole91.5

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Area Under the Plasma Concentration Curve From Time 0 to 24 Hours (AUC0-24) for Balovaptan

AUC0-24 is the area under the plasma concentration-time curve from time 0 to 24 hours post dose. (NCT03586726)
Timeframe: Day 10 and 11 of Period 1; Day 16 and 17 of Period 2

Interventionng.h/mL (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin100067.0

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Metabolite to Parent Ratio for M2 Metabolite Based on AUC0-24

(NCT03586726)
Timeframe: Day 10 and 11 of Period 1; Day 16 and 17 of Period 2

InterventionRatio (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin0.4302.14

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Percentage of Participants With Adverse Events

(NCT03586726)
Timeframe: Up to 21 days postdose

InterventionPercentage (Number)
Balovaptan + Rifampicin94

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Time to Maximum Observed Plasma Concentration for M3 Metabolite

Tmax is the first observed time to reach peak analyte concentration obtained directly from the experimental data without interpolation, expressed in time units. (NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

InterventionHour(s) (Median)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin1.001.00

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Time to Maximum Observed Plasma Concentration for M2 Metabolite

Tmax is the first observed time to reach peak analyte concentration obtained directly from the experimental data without interpolation, expressed in time units. (NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

InterventionHours (Median)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin2.503.00

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Time to Maximum Observed Plasma Concentration (Tmax) for Balovaptan

Tmax is the first observed time to reach peak analyte concentration obtained directly from the experimental data without interpolation, expressed in time units. (NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

InterventionHour (Median)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin1.001.00

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Metabolite to Parent Ratio for M3 Metabolite Based on Cmax

(NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

InterventionRatio (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin0.5450.873

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Metabolite to Parent Ratio for M3 Metabolite Based on AUC0-24

(NCT03586726)
Timeframe: Day 10 and 11 of Period 1; Day 16 and 17 of Period 2

InterventionRatio (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin0.8721.70

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Metabolite to Parent Ratio for M2 Metabolite Based on Cmax

(NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

InterventionRatio (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin0.2250.606

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Maximum Plasma Concentration (Cmax) for M3 Metabolite

Cmax is the observed peak analyte concentration obtained directly from the experimental data without interpolation, expressed in concentration units. (NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

Interventionng/mL (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin49.610.9

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Maximum Plasma Concentration (Cmax) for M2 Metabolite

Cmax is the observed peak analyte concentration obtained directly from the experimental data without interpolation, expressed in concentration units. (NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

Interventionng/mL (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin22.08.09

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Maximum Plasma Concentration (Cmax) for Balovaptan

Cmax is the observed peak analyte concentration obtained directly from the experimental data without interpolation, expressed in concentration units. (NCT03586726)
Timeframe: Day 10 of Period 1 and Day 16 of Period 2

Interventionng/mL (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin94.212.9

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Area Under the Plasma Concentration Curve From Time 0 to 24 Hours for M3 Metabolite

AUC0-24 is the area under the plasma concentration-time curve from time 0 to 24 hours post dose. (NCT03586726)
Timeframe: Day 10 and 11 of Period 1; Day 16 and 17 of Period 2

Interventionng.h/mL (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin844110

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Area Under the Plasma Concentration Curve From Time 0 to 24 Hours for M2 Metabolite

AUC0-24 is the area under the plasma concentration-time curve from time 0 to 24 hours post dose. (NCT03586726)
Timeframe: Day 10 and 11 of Period 1; Day 16 and 17 of Period 2

Interventionng.h/mL (Geometric Mean)
Balovaptan (Period 1)Balovaptan + rifampicin (Period 2)
Balovaptan + Rifampicin448149

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Treatment B vs Treatment A (Part 1), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure Cmax for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar Cmax which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

InterventionnM (Geometric Mean)
Part 1, Treatment A13.7
Part 1, Treatment B39.2

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Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure AUC∞ for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar AUC∞ which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in hour*nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

Interventionhr*nM (Geometric Mean)
Part 2, Treatment C3610
Part 2, Treatment D194

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Treatment B Vs Treatment A (Part 1), Combined Molar Exposure for AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity, Calculated Using the Observed Value of the Last Quantifiable Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure AUC∞ for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar AUC∞ which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in hour*nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr*nM (Geometric Mean)
Part 1, Treatment A298
Part 1, Treatment B1820

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Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of TAK-788

(NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr (Median)
Part 1, Treatment A6.00
Part 1, Treatment B8.00
Part 2, Treatment C6.00
Part 2, Treatment D4.00

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Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32960

(NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr (Median)
Part 1, Treatment A6.00
Part 1, Treatment B8.00
Part 2, Treatment C6.00
Part 2, Treatment D2.00

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Tmax - Time to Reach the Maximum Plasma Concentration (Cmax) of AP32914

(NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 240 hours) post-dose

Interventionhr (Median)
Part 1, Treatment A6.00
Part 1, Treatment B8.00
Part 2, Treatment C6.00
Part 2, Treatment D4.00

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Treatment D Vs Treatment C (Part 2), Combined Molar Exposure for Cmax: Maximum Observed Plasma Concentration of TAK-788, AP32960, and AP32914

The combined molar exposure Cmax for TAK-788 and its metabolites AP32960 and AP3914 value was calculated as the sum of each molar Cmax which was multiplied by 1000 and divided by molecular weight of each analyte, TAK-788, AP32960, and AP32914 respectively. The combined molar exposure was presented in nanomolar. (NCT03928327)
Timeframe: Day 1 pre-dose and at multiple time points (up to 168 hours) post-dose

InterventionnM (Geometric Mean)
Part 2, Treatment C177
Part 2, Treatment D14.9

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AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, and 9 hours post-dose

Interventionhr*ng/mL (Median)
Part B: Pamiparib4267.86
Part B:Pamiparib + Itraconazole3812.39

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AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhr*ng/mL (Median)
Part A: Pamiparib28142
Part A: Pamiparib + Rifampin18563

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AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge) 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhours*nanograms/milliLiter (h*ng/mL) (Median)
Part B: Pamiparib9163
Part B: Pamiparib + Itraconazole8894

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Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionng/mL (Median)
Part A: Pamiparib1970
Part A: Pamiparib + Rifampin1820

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Maximum Observed Concentration (Cmax) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge; ) 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionng/mL (Median)
Part B: Pamiparib730.5
Part B: Pamiparib + Itraconazole752.5

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Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part A: Pamiparib2.000
Part A: Pamiparib + Rifampin2.000

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AUC From Time Zero to Time of Last Quantifiable Concentration Post-dose (AUC0-tlast) in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhours*nanograms/milliLiter (h*ng/mL) (Median)
Part A: Pamiparib28868
Part A: Pamiparib + Rifampin18351

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Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters (Median)
Part B: Pamiparib34.697
Part B:Pamiparib + Itraconazole37.589

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Apparent Volume of Distribution (Vz/F) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters (Median)
Part A: Pamiparib35.491
Part A: Pamiparib + Rifampin37.712

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Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part B: Pamiparib9.290
Part B:Pamiparib + Itraconazole11.179

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Number of Participants With Treatment-emergent Adverse Events (TEAEs) and Serious Adverse Events (SAEs)

TEAE is defined as any AE with an onset date on or after the date of first dose of study medication until the date of last study medication dose plus 30 days. Seriousness of the AE is determined by the investigator based on seriousness criteria. (NCT03994211)
Timeframe: From the date informed consent has been signed until last study medication dose plus 30 days (up to approximately 26 months)

,,
InterventionNumber of participants (Number)
All TEAEsSerious TEAEs
Core Phase: Arm A: Pamiparib + Rifampin50
Core Phase: Arm B: Pamiparib + Itraconazole61
Extension Phase182

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Number of Participants With Clinically Significant Abnormalities in Laboratory Assessments, Vital Signs, ECG Parameters and Physical Examinations

(NCT03994211)
Timeframe: Up to approximately 26 months

,,
InterventionNumber of participants (Number)
Laboratory AssessmentsVital SignsPhysical ExaminationsECG Parameters
Core Phase: Arm A: Pamiparib + Rifampin0000
Core Phase: Arm B: Pamiparib + Itraconazole0000
Extension Phase0000

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Apparent Terminal Elimination Half-life (t1/2) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part A: Pamiparib13.381
Part A: Pamiparib + Rifampin7.667

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Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters/hour (L/h) (Median)
Part B: Pamiparib1.987
Part B:Pamiparib + Itraconazole2.147

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Apparent Oral Clearance (CL/F) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

InterventionLiters/hour (L/h) (Median)
Part A: Pamiparib2.132
Part A: Pamiparib + Rifampin3.232

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Time of the Maximum Observed Concentration (Tmax) of Pamiparib for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12 hours post-dose

Interventionhours (Median)
Part B: Pamiparib2.000
Part B:Pamiparib + Itraconazole1.000

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AUC From Zero to Infinity (AUC0-inf) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge) 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, 12, 24, and 48 hours post-dose

Interventionhr*ng/mL (Median)
Part B: Pamiparib10072
Part B:Pamiparib + Itraconazole9353

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AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part B

(NCT03994211)
Timeframe: Part B: from Day -1 (admission) to Day 9 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, and 12 hours post-dose

Interventionhr*ng/mL (Median)
Part B: Pamiparib5097.06
Part B: Pamiparib + Itraconazole4647.47

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AUC From Zero to 9 Hours (AUC0-9) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, and 9 hours post-dose

Interventionhr*ng/mL (Median)
Part A: Pamiparib11821.06
Part A: Pamiparib + Rifampin10515.14

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AUC From Zero to 12 Hours (AUC0-12) of Pamiparib in Plasma for Part A

(NCT03994211)
Timeframe: Part A: from Day -1 (admission) to Day 12 (discharge); 30 min pre-dose, 0.5, 1, 2, 4, 6, 9, and 12 hours post-dose

Interventionhr*ng/mL (Median)
Part A: Pamiparib14642.90
Part A: Pamiparib + Rifampin12262.61

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Cmax

Secondary outcomes will include fluvastatin maximum plasma concentration (Cmax). (NCT04029584)
Timeframe: Cmax will be assessed over a 12 hour study period.

Interventionng/mL (Mean)
Fluvastatin Control176
Fluvastatin and IV Rifampin447
Fluvastatin + Oral Rifampin Induction87.8
Fluvastatin +Oral Rifampin Induced +IV Rifampin379

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Tmax

Secondary outcomes will include time to Cmax (Tmax). (NCT04029584)
Timeframe: Tmax will be assessed over a 12 hour study period.

Interventionhr (Mean)
Fluvastatin Control1.20
Fluvastatin and IV Rifampin1.17
Fluvastatin + Oral Rifampin Induction1.28
Fluvastatin +Oral Rifampin Induced +IV Rifampin1.23

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AUC

The primary outcome will be fluvastatin Area under the concentration vs time curve (AUC0-12h and AUC0-INF) (NCT04029584)
Timeframe: AUC will be assessed over a 12 hour study at 0, 0.33, 0.67,1,1.5, 2, 2.5, 3, 4, 6, 9, 12h

,,,
Interventionng/mL·h (Mean)
AUC(0-12)AUC(0-INF)
Fluvastatin + Oral Rifampin Induction124136
Fluvastatin +Oral Rifampin Induced +IV Rifampin371385
Fluvastatin and IV Rifampin642679
Fluvastatin Control242266

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Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 to the Last Quantifiable Data Point (AUC0-tz)

Area under the concentration-time curve of BI 894416 in plasma over the time interval from 0 to the last quantifiable data point (AUC0-tz). (NCT04060719)
Timeframe: Within 3 hours before administration of BI 894416 and at 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 34 and 48 hours after administration of BI 894416.

Interventionhour * nanomole / liter (Geometric Least Squares Mean)
BI 894416 Alone (Reference, R)9047.51
BI 894416 + Rifampicin (Test, T)939.98

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Area Under the Concentration-time Curve of BI 894416 in Plasma Over the Time Interval From 0 Extrapolated to Infinity (AUC0-∞)

Area under the concentration-time curve of BI 894416 in plasma over the time interval from 0 extrapolated to infinity (AUC0-∞). (NCT04060719)
Timeframe: Within 3 hours before administration of BI 894416 and at 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 34 and 48 hours after administration of BI 894416.

Interventionhour * nanomole / liter (Geometric Least Squares Mean)
BI 894416 Alone (Reference, R)9077.08
BI 894416 + Rifampicin (Test, T)951.58

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Maximum Measured Concentration of BI 894416 in Plasma (Cmax)

Maximum measured concentration of BI 894416 in plasma (Cmax). (NCT04060719)
Timeframe: Within 3 hours before administration of BI 894416 and at 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 10, 12, 24, 34 and 48 hours after administration of BI 894416.

Interventionnanomole / liter (Geometric Least Squares Mean)
BI 894416 Alone (Reference, R)1624.79
BI 894416 + Rifampicin (Test, T)487.98

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Number of Participants With Clinically Significant Change From Baseline in Clinical Laboratory Values

(NCT04121078)
Timeframe: Baseline up to 14 days after the last dose of study drug in Study Period 2 (up to Day 23)

InterventionParticipants (Count of Participants)
Treatment A: TAK-906 25 mg0
Treatment B: Rifampin 600 mg and TAK-906 25 mg0

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Number of Participants With Clinically Significant Change From Baseline in 12-lead Electrocardiogram (ECG) Findings

(NCT04121078)
Timeframe: Baseline up to 14 days after the last dose of study drug in Study Period 2 (up to Day 23)

InterventionParticipants (Count of Participants)
Treatment A: TAK-906 25 mg0
Treatment B: Rifampin 600 mg and TAK-906 25 mg0

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Number of Participants With Clinically Significant Change From Baseline in Vital Sign Values

(NCT04121078)
Timeframe: Baseline up to 14 days after the last dose of study drug in Study Period 2 (up to Day 23)

InterventionParticipants (Count of Participants)
Treatment A: TAK-906 25 mg0
Treatment B: Rifampin 600 mg and TAK-906 25 mg0

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Cmax: Maximum Observed Plasma Concentration for TAK-906

(NCT04121078)
Timeframe: Day 1: time zero and at multiple time points (up to 48 hours) post dose

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Treatment A: TAK-906 25 mg14.37
Treatment B: Rifampin 600 mg and TAK-906 25 mg89.62

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AUClast: Area Under the Plasma Concentration-Time Curve From Time 0 to the Time of the Last Quantifiable Concentration for TAK-906

(NCT04121078)
Timeframe: Day 1: time zero and at multiple time points (up to 48 hours) post dose

Interventionng*hr/mL (Geometric Mean)
Treatment A: TAK-906 25 mg32.32
Treatment B: Rifampin 600 mg and TAK-906 25 mg168.3

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AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for TAK-906

(NCT04121078)
Timeframe: Day 1: time zero and at multiple time points (up to 48 hours) post dose

Interventionnanogram*hour per milliliter (ng*hr/mL) (Geometric Mean)
Treatment A: TAK-906 25 mg32.68
Treatment B: Rifampin 600 mg and TAK-906 25 mg168.5

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Number of Participants Reporting One or More Treatment-emergent Adverse Events (TEAEs)

(NCT04121078)
Timeframe: Baseline up to 14 days after the last dose of study drug in Study Period 2 (up to Day 23)

InterventionParticipants (Count of Participants)
Treatment A: TAK-906 25 mg6
Treatment B: Rifampin 600 mg and TAK-906 25 mg2

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Serum Etonogestrel Concentrations

Blood drawn before and after rifampin administration (2 weeks) for serum extraction and etonogestrel analysis (NCT04463680)
Timeframe: 2 weeks

Interventionpg/mL (Median)
BaselinePost-rifampin
Rifampin 600 mg164.047.8

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Cohort 2: Lag Time Before Observation of Drug Concentrations (Tlag) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 2:Period 1: Gepotidacin 1500 mg0.000
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg0.000

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Cohort 2: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 %. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg20.85
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg10.42

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Cohort 2: T1/2 of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg10.882
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg10.972

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Cohort 2: Tmax of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 2:Period 1: Gepotidacin 1500 mg2.500
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg2.000

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Cohort 3: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose )

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1066.21

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Cohort 3: AUC (0-48) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg16682.1

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Cohort 3: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg73.2

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Cohort 3: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg14333.9

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Cohort 4: Accumulation Ratio Based on AUC(0-tau) (RoAUC) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as AUC(0-tau) after the second dose, where 0 is the timepoint prior to second dose, divided by AUC(0-tau) after the first dose, where 0 is the predose timepoint prior to the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionRatio (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1.254

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Cohort 4: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including systolic blood pressure (SBP), diastolic blood pressure (DBP) and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 4: Gepotidacin 1500 mg Fasted011011000110
Cohort 4: Gepotidacin 1500 mg Fed110011000110
Cohort 4: Gepotidacin 3000 mg Fed011001100110
Cohort 4: Placebo030030030

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Cohort 4: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including potential of hydrogen (pH) of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChangeSpecific Gravity; To High
Cohort 4: Gepotidacin 1500 mg Fasted11011011011011010111001100110
Cohort 4: Gepotidacin 1500 mg Fed1101101109211011011001100110
Cohort 4: Gepotidacin 3000 mg Fed1101101109210110111001100110
Cohort 4: Placebo30302121302130030030

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Cohort 4: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, Erythrocyte Mean Corpuscular Hemoglobin (MCH), Erythrocyte Mean Corpuscular Volume (MCV), Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose laboratory (lab) value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100 (%). High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 4: Gepotidacin 1500 mg Fasted09201010110010101100110011001100110011011000110
Cohort 4: Gepotidacin 1500 mg Fed011001010110010101010101010101100110011001100110
Cohort 4: Gepotidacin 3000 mg Fed01010101011009211000101011011000110011011001100
Cohort 4: Placebo030030030021030030030030030030030030

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Cohort 4: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including Alanine Aminotransferase (ALT), Albumin, Alkaline Phosphatase (Alk Phos), Aspartate Aminotransferase (AST), Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, Blood Urea Nitrogen (BUN). Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine;To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 4: Gepotidacin 1500 mg Fasted01100110011001100110011011000110011001100110011001100110011001100110
Cohort 4: Gepotidacin 1500 mg Fed01100110011001100110011001100110011001100110011001100110011001100110
Cohort 4: Gepotidacin 3000 mg Fed0110011001100110011001100110011019101100110011001100110011001100110
Cohort 4: Placebo030120030030021030030030120030021030030021030030030

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Cohort 4: Number of Participants With Serious Adverse Events (SAE) and Non-serious Adverse Events (Non-SAE)

An adverse event (AE) is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 4: Gepotidacin 1500 mg Fasted02
Cohort 4: Gepotidacin 1500 mg Fed01
Cohort 4: Gepotidacin 3000 mg Fed04
Cohort 4: Placebo00

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Cohort 4: Number of Participants With Any Increase in Maximum Post-Baseline Electrocardiogram (ECG) Parameter Corrected QT (QTc) Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the Bazett formula (QTcB) Interval and corrected QT interval using the Fridericia formula (QTcF) Interval has been reported. (NCT04493931)
Timeframe: Up to 22 days

,,,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 4: Gepotidacin 1500 mg Fasted30
Cohort 4: Gepotidacin 1500 mg Fed81
Cohort 4: Gepotidacin 3000 mg Fed92
Cohort 4: Placebo11

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Cohort 4: Ae(t1-t2) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionMilligrams (Geometric Mean)
Ae (0-2); n=11Ae (2-4); n=10Ae (4-6); n=11Ae (6-8); n=11Ae (8-12); n=11Ae (12-14); n=11Ae (14-16); n=11Ae (16-18); n=11Ae (18-20); n=11Ae (20-24); n=11Ae (24-36); n=11Ae (36-48); n=11Ae (48-60); n=10
Cohort 4: Gepotidacin 3000 mg FedNA221.19103.6867.5865.06112.83174.62136.6690.8180.5457.6214.479.67

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Cohort 4: Ae(t1-t2) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Ae (0-2)Ae (2-4)Ae (4-6)Ae (6-8)Ae (8-12)Ae (12-24)Ae (24-36)Ae (36-48)
Cohort 4: Gepotidacin 1500 mg FedNA102.2360.0531.6116.5117.165.724.28

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Cohort 3: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including SBP, DBP and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg019001900190
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg018001800180

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Cohort 1: Terminal Phase Half-life (t1/2) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg11.344
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg12.415

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Cohort 3: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, MCH, MCV, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg019001900190018121701171018101900190018101900190
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg018001620180018011702142115201710171117001710180

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Cohort 3: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including ALT, Albumin, Alk Phos, AST, Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, BUN. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine; To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg01901180019001810190118001900190018101900190019001900181019001900190
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg01710171018001800180117001800171018001800180018001800180018001801170

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Cohort 3: Number of Participants With SAE and Non-SAE

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg01
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg011

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Cohort 3: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the QTcB Interval and QTcF Interval has been reported. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg20
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg50

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Cohort 3: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Ae (0-2), n=17Ae (2-4), n=18Ae (4-6), n=16Ae (6-8); n=16Ae (8-12), n=18Ae (12-14), n=17Ae (14-16), n=15Ae (16-18), n=14Ae (18-20), n=15Ae (20-24), n=17Ae (24-36), n=18Ae (36-48); n=18Ae (48-60), n=18
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mgNA117.61103.1170.9867.4264.49142.36146.8993.0574.4470.0120.168.51

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Cohort 2: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including SBP, DBP and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 2: Period 1: Gepotidacin 1500 mg016101700170
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg014001400140

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Cohort 2: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including pH of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChangeSpecific Gravity; To High
Cohort 2: Period 1: Gepotidacin 1500 mg17017017016117017017001700143
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg16016016014215114216001600151

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Cohort 2: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, MCH, MCV, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 2: Period 1: Gepotidacin 1500 mg017001520170017001700143017001700170115101700170
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg016101430170017001700152017011600152314041300161

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Cohort 2: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including ALT, Albumin, Alk Phos, AST, Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, BUN. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine; To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 2: Period 1: Gepotidacin 1500 mg01700170017001700170017001700170017001610170017001700161017001700170
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg01520170017001612150017031400170017001610170016101700152017001700170

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Cohort 2: Number of Participants With SAE and Non-SAE

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 26 days

,,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 2: Period 1: Gepotidacin 1500 mg03
Cohort 2: Period 2 (Days 1 to 7) Rifampicin 600 mg02
Cohort 2: Period 2 (Days 8 to 9) Gepotidacin 1500 mg + Rifampicin 600 mg02

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Cohort 2: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the QTcB Interval and QTcF Interval has been reported. (NCT04493931)
Timeframe: Up to 26 days

,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 2: Period 1: Gepotidacin 1500 mg20
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg21

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Cohort 2: Ae(t1-t2) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

,
InterventionMilligrams (Geometric Mean)
Ae (0-2)Ae (2-4)Ae (4-6)Ae (6-8)Ae (8-12)Ae (12-24)Ae (24-36)Ae (36-48)
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mgNA55.8121.6613.829.1911.514.742.75
Cohort 2:Period 1: Gepotidacin 1500 mg12.6779.8467.4833.9227.5921.1711.043.61

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Cohort 1: Number of Participants With Worst Case Vital Sign Results Relative to Normal Range Post-Baseline Relative to Baseline

Vital signs including SBP, DBP and pulse rate were measured in a semi-supine position after 5 minutes rest. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose value category was unchanged (e.g., High to High), or whose value became normal, were recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
DBP; To LowDBP; To Normal or No ChangeDBP; To HighSBP; To LowSBP; To Normal or No ChangeSBP; To HighPulse rate; To LowPulse rate; To Normal or No ChangePulse rate; To High
Cohort 1: Gepotidacin 1500 mg014001400140
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg013001300130

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Cohort 1: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including pH of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChangeSpecific Gravity; To High
Cohort 1: Gepotidacin 1500 mg14014014012214013114001400131
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg13013013013013011213001300130

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Cohort 1: Number of Participants With Worst Case Hematology Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of hematology parameters including Basophils, Eosinophils, MCH, MCV, Erythrocytes, Hematocrit, Hemoglobin, Leukocytes, Lymphocytes, Monocytes, Neutrophils, Platelets. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100 %. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
Basophils; To LowBasophils; To Normal or No ChangeBasophils; To HighEosinophils; To LowEosinophils; To Normal or No ChangeEosinophils; To HighMCH; To LowMCH; To Normal or No ChangeMCH; To HighMCV; To LowMCV; To Normal or No ChangeMCV; To HighErythrocytes; To LowErythrocytes; To Normal or No ChangeErythrocytes; To HighHematocrit; To LowHematocrit; To Normal or No ChangeHematocrit; To HighHemoglobin; To LowHemoglobin; To Normal or No ChangeHemoglobin; To HighLeukocytes; To LowLeukocytes; To Normal or No ChangeLeukocytes; To HighLymphocytes; To LowLymphocytes; To Normal or No ChangeLymphocytes; To HighMonocytes; To LowMonocytes; To Normal or No ChangeMonocytes; To HighNeutrophils; To LowNeutrophils; To Normal or No ChangeNeutrophils; To HighPlatelets; To LowPlatelets; To Normal or No ChangePlatelets; To High
Cohort 1: Gepotidacin 1500 mg014001400140013101400131014001310140013101310140
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg011201300130013021101120013001300121013011200130

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Cohort 1: Number of Participants With Worst Case Clinical Chemistry Results Relative to Normal Range Post-Baseline Relative to Baseline

Blood samples were collected at indicated time points for analysis of clinical chemistry parameters including ALT, Albumin, Alk Phos, AST, Bilirubin, Calcium, Carbon Dioxide, Chloride, Creatine Kinase, Creatinine, Direct Bilirubin, Glucose, Magnesium, Potassium, Protein, Sodium, BUN. Participants were counted in the worst case category that their value changes to (low, normal or high), unless there was no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant had values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
ALT; To LowALT; To Normal or No ChangeALT; To HighAlbumin; To LowAlbumin; To Normal or No ChangeAlbumin; To HighAlk Phos; To LowAlk Phos; To Normal or No ChangeAlk Phos; To HighAST; To LowAST; To Normal or No ChangeAST; To HighBilirubin; To LowBilirubin; To Normal or No ChangeBilirubin; To HighCalcium; To LowCalcium; To Normal or No ChangeCalcium; To HighCarbon Dioxide; To LowCarbon Dioxide; To Normal or No ChangeCarbon Dioxide; To HighChloride; To LowChloride; To Normal or No ChangeChloride; To HighCreatine Kinase; To LowCreatine Kinase; To Normal or No ChangeCreatine Kinase; To HighCreatinine; To LowCreatinine; To Normal or No ChangeCreatinine; To HighDirect Bilirubin; To LowDirect Bilirubin; To Normal or No ChangeDirect Bilirubin; To HighGlucose; To LowGlucose; To Normal or No ChangeGlucose; To HighMagnesium; To LowMagnesium; To Normal or No ChangeMagnesium; To HighPotassium; To LowPotassium; To Normal or No ChangePotassium; To HighProtein; To LowProtein; To Normal or No ChangeProtein; To HighSodium; To LowSodium; To Normal or No ChangeSodium; To HighBUN; To LowBUN; To Normal or No ChangeBUN; To High
Cohort 1: Gepotidacin 1500 mg01400140014001400140014011300140113001400140014001400140014001400140
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg01121120013001211120013001300121013001030130013001300121013001300130

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Cohort 1: Number of Participants With SAE and Non-SAE

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any serious adverse event that, at any dose results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability/incapacity, is a congenital anomaly/birth defect or any other situations as per Medical or scientific judgment. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
Any SAEAny non-SAE
Cohort 1: Gepotidacin 1500 mg00
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg00

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Cohort 1: Number of Participants With Any Increase in Maximum Post-Baseline ECG Parameter QTc Interval

A 12-lead ECG was recorded with the participant in a semi-supine position after a rest of at least 10 minutes using an ECG machine that automatically calculated the QTc interval. Number of participants with any increase of >450 milliseconds in corrected QT interval using the QTcB Interval and QTcF Interval has been reported. (NCT04493931)
Timeframe: Up to 17 days

,
InterventionParticipants (Count of Participants)
QTcB IntervalQTcF Interval
Cohort 1: Gepotidacin 1500 mg30
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg41

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Cohort 1: Amount of Drug Excreted in Urine in a Time Interval (Ae[t1-t2]) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae(t1-t2) measured the amount of drug excreted in urine at defined time intervals. (NCT04493931)
Timeframe: 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment periods 1 and 2

,
InterventionMilligrams (Geometric Mean)
Ae (0-2), n=14, 13Ae (2-4), n=14, 12Ae (4-6), n=14, 13Ae (6-8); n=14, 13Ae (8-12), n=12, 13Ae (12-24), n=14, 13Ae (24-36), n=14, 13Ae (36-48), n=14, 13
Cohort 1: Gepotidacin 1500 mg28.6689.1850.5234.3829.9025.4410.884.50
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mgNA142.9982.7746.2230.9722.048.764.08

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Cohort 4: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionLiters (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1251.05

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Cohort 4: Vz/F of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed1246.70
Cohort 4: Gepotidacin 1500 mg Fasted1329.83

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Cohort 4: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Median)
Cohort 4: Gepotidacin 3000 mg Fed2.000

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Cohort 4: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Median)
Cohort 4: Gepotidacin 3000 mg Fed2.000

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Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 4: Gepotidacin 1500 mg Fed2.000
Cohort 4: Gepotidacin 1500 mg Fasted1.500

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Cohort 4: Tmax of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 4: Gepotidacin 1500 mg Fed2.000
Cohort 4: Gepotidacin 1500 mg Fasted1.500

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Cohort 4: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Median)
Cohort 4: Gepotidacin 3000 mg Fed0

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Cohort 4: Tlag of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 4: Gepotidacin 1500 mg Fed0.000
Cohort 4: Gepotidacin 1500 mg Fasted0.000

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Cohort 4: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose )-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed12.599

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Cohort 3: Number of Participants With Worst Case Urinalysis Results Relative to Normal Range Post-Baseline Relative to Baseline

Urine samples were collected at indicated time points for the analysis of urinalysis parameters including pH of urine, presence of glucose, protein, blood, ketones, bilirubin, nitrite, leukocyte esterase in urine by dipstick. Specific gravity of urine was measured by microscopic examination. Participants were counted in the worst case category that their value changes to (low, normal, high, or abnormal), unless there is no change in their category. Participants whose lab value category was unchanged (e.g., High to High), or whose value became normal, are recorded in the 'To Normal or No Change' category. Participants were counted twice if the participant has values that changed 'To Low' and 'To High', so the percentages may not add to 100%. High and low indicated that participants had values flagged as high and low respectively for the particular parameter any time on-treatment. (NCT04493931)
Timeframe: Up to 30 days

,
InterventionParticipants (Count of Participants)
Bilirubin; To Normal or No ChangeBilirubin; To AbnormalGlucose; To Normal or No ChangeGlucose; To AbnormalKetones; To Normal or No ChangeKetones; To AbnormalLeukocyte Esterase; To Normal or No ChangeLeukocyte Esterase; To AbnormalNitrite; To Normal or No ChangeNitrite; To AbnormalOccult Blood; To Normal or No ChangeOccult Blood; To AbnormalProtein; To Normal or No ChangeProtein; To AbnormalpH; To LowpH; To Normal or No ChangepH; To HighSpecific Gravity; To LowSpecific Gravity; To Normal or No ChanSpecific Gravity; To High
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg19019016313619014516301900163
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg18018017113518013516201800108

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Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 %. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionPercent dose excreted (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed22.24

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Cohort 4: Percentage of the Given Dose of Drug Excreted in Urine (fe%) for Gepotidacin 1500 mg Under Fed Condition

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100%. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed19.57

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Cohort 4: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed12.363

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Cohort 4: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg -Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed11.204

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Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Least Squares Mean)
Cohort 4: Gepotidacin 1500 mg Fed5.421
Cohort 4: Gepotidacin 1500 mg Fasted5.158

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Cohort 4: Cmax of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed5.436
Cohort 4: Gepotidacin 1500 mg Fasted5.143

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Cohort 4: CLr of Gepotidacin Following Two 3000 mg Dose-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed14.61

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Cohort 4: CLr of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed13.42

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Cohort 4: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed68.83

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Cohort 4: CL/F of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed67.26
Cohort 4: Gepotidacin 1500 mg Fasted73.50

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Cohort 4: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed4996.9

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Cohort 4: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Evening Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed46.7

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Cohort 4: AUC(0-tau) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. AUC(0-tau) can be calculated only for multiple doses and not for single dose as tau refers to the dosing interval. Hence, AUC(0-tau) could not be calculated for Gepotidacin 1500 mg single dose as mentioned in Reporting and Analysis Plan. The results for this outcome measure will never be posted. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg FedNA

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Cohort 4: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed91.4

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Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*Micrograms per milliliter (Geometric Least Squares Mean)
Cohort 4: Gepotidacin 1500 mg Fed21.9
Cohort 4: Gepotidacin 1500 mg Fasted20.0

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Cohort 4: AUC(0-t) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed21.9
Cohort 4: Gepotidacin 1500 mg Fasted20.0

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Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma - Food Effect in Japanese Participants

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*Micrograms per milliliter (Geometric Least Squares Mean)
Cohort 4: Gepotidacin 1500 mg Fed22.3
Cohort 4: Gepotidacin 1500 mg Fasted20.4

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Cohort 4: AUC(0-infinity) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed22.3
Cohort 4: Gepotidacin 1500 mg Fasted20.4

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Cohort 4: AUC(0-48) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed15768.2

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Cohort 4: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed90.8

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Cohort 4: AUC(0-48) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed2293.7

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Cohort 4: AUC(0-24) of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed14729.5

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Cohort 4: AUC(0-24) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed84.6

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Cohort 4: AUC(0-24) of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed2142.4

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Cohort 4: AUC From Time 0 (Predose) to Time Tau (AUC[0-tau]) of Gepotidacin in Plasma After the First Dose of 3000 Mg-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed37.3

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Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 48 Hours Post-dose (AUC[0-48]) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed21.9
Cohort 4: Gepotidacin 1500 mg Fasted20.0

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Cohort 4: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Concentration at 24 Hours Post-dose (AUC[0-24]) of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed20.9
Cohort 4: Gepotidacin 1500 mg Fasted19.0

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Cohort 4: Ae Total of Gepotidacin in Urine Following Two 3000 mg Doses-Fed State

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in Treatment Period 3

InterventionMilligrams (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1334.42

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Cohort 4: Ae Total of Gepotidacin Following Single Dose of 1500 mg Under Fed Condition in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed293.50

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Cohort 4: Accumulation Ratio Based on Cmax (RoCmax) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)-Fed State

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as Cmax after the second dose divided by Cmax after the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 minutes, 14 Hours, 14 Hours 30 minutes, 15, 16, 18, 20, 24, 36, 48, 60 Hours post-dose in Treatment Period 3

InterventionRatio (Geometric Mean)
Cohort 4: Gepotidacin 3000 mg Fed1.103

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Cohort 3: Vz/F of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg615.36
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg371.24

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Cohort 3: Vz/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg959.42

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Cohort 3: Vz/F of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg923.75
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg688.49

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Cohort 3: Tmax of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.650
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.500

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Cohort 3: Tmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg2.000

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Cohort 3: Tmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg2.500

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Cohort 3: Tmax of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg2.000
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1.275

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Cohort 3: Tlag of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.000
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.000

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Cohort 3: Tlag of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.250

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Cohort 3: Tlag of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.000
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.000

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Cohort 3: T1/2 of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg5.320
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg6.075

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Cohort 3: T1/2 of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose+ Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg9.501

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Cohort 3: T1/2 of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg39.367
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg32.777

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Cohort 3: RoCmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as Cmax after the second dose divided by Cmax after the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionRatio (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1.278

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Cohort 3: RoAUC of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Accumulation ratio was calculated as AUC(0-tau) after the second dose, where 0 is the timepoint prior to second dose, divided by AUC(0-tau) after the first dose, where 0 is the predose timepoint prior to the first dose. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionRatio (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg1.406

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Cohort 3: Percentage of the Given Dose of Drug Excreted in Urine (fe%) Following Two 3000 mg Doses of Gepotidacin (First Dose + Second Dose )

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 %. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg17.77

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Cohort 3: Minimum Observed Concentration (Cmin) of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionPicograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg44.127
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg77.447

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Cohort 3: Cmin of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionNanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg0.192
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg0.222

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Cohort 3: Cmax of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionNanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg5.238
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg6.507

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Cohort 1: Apparent Oral Clearance (CL/F) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg72.72
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg64.14

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Cohort 1: Apparent Volume of Distribution (Vz/F) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg1190.16
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg1143.29

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Cohort 1: Area Under the Concentration-time Curve From Time 0 (Pre-dose) to the Time of the Last Quantifiable Concentration (AUC [0-t]) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg20.3
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg23.4

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Cohort 1: AUC (0-24) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg19.3
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg21.9

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Cohort 1: AUC From Time 0 (Pre-dose) Extrapolated to Infinite Time (AUC[0-infinity]) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours* micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg20.6
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg23.9

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Cohort 1: AUC(0-24) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours Post-dose in each Treatment periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg3292.1
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg3612.4

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Cohort 1: AUC(0-48) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg20.3
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg23.0

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Cohort 1: AUC(0-48) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg3578.2
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg3831.1

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Cohort 1: Maximum Observed Concentration (Cmax) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric least square (LS) mean and 90 percent (%) confidence interval (CI) of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg4.817
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg4.548

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Cohort 1: Percentage of the Given Dose of Drug Excreted in Urine (fe%) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. fe% was calculated as: (Ae total divided by Dose) multiplied by 100 percent (%). (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionPercent dose excreted (Geometric Mean)
Cohort 1: Gepotidacin 1500 mg22.72
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg26.90

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Cohort 1: Renal Clearance (CLr) of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg16.06
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg17.59

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Cohort 1: Time to Reach Maximum Observed Concentration (Tmax) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 1: Gepotidacin 1500 mg2.500
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg2.500

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Cohort 1: Tlag of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours (Median)
Cohort 1: Gepotidacin 1500 mg0.000
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg0.000

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Cohort 1: Total Unchanged Drug (Ae Total) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours Post-dose in each Treatment periods 1 and 2

InterventionMilligrams (Geometric Least Squares Mean)
Cohort 1: Gepotidacin 1500 mg337.92
Cohort 1: Gepotidacin 1500 mg + Cimetidine 400 mg410.10

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Cohort 2: Ae Total of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Ae total was calculated by adding all the fractions of drug collected over all the allotted time intervals. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionMilligrams (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg312.73
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg156.05

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Cohort 2: AUC(0-24) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg17.9
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg8.9

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Cohort 3: Cmax of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg10.051

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Cohort 3: Cmax of Gepotidacin in Plasma After the First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg7.867

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Cohort 3: Cmax of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionPicograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg1553.135
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg2381.259

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Cohort 2: AUC(0-24) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg3081.3
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg1352.4

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Cohort 2: AUC(0-48) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg19.0
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg9.5

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Cohort 2: Vz/F of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg1217.45
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg2460.46

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Cohort 2: AUC(0-48) of Gepotidacin in Urine

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg3370.1
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg1476.8

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Cohort 2: AUC(0-infinity) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg19.3
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg9.3

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Cohort 2: AUC(0-t) of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg19.0
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg9.0

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Cohort 2: CL/F of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg77.55
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg155.43

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Cohort 2: CLr of Gepotidacin

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-24 Hours, 24-36 Hours, 36-48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg16.49
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg17.07

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Cohort 2: Cmax of Gepotidacin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90% CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionMicrograms per milliliter (Geometric Least Squares Mean)
Cohort 2:Period 1: Gepotidacin 1500 mg3.735
Cohort 2: Period 2: Gepotidacin 1500 mg + Rifampicin 600 mg2.728

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Cohort 3: CLr of Gepotidacin Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg13.19

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Cohort 3: CL/F of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg80.17
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg42.16

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Cohort 3: CL/F of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg69.99

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Cohort 3: CL/F of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours post-dose in each Treatment Periods 1 and 2

InterventionLiters per Hour (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg16.26
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg14.51

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Cohort 3: AUC(0-tau) of Gepotidacin in Urine Following Two 3000 mg Doses (First Dose + Second Dose)

Urine samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 0-2 Hours, 2-4 Hours, 4-6 Hours, 6-8 Hours, 8-12 Hours, 12-14 Hours, 14-16 Hours, 16-18 Hours, 18-20 Hours, 20-24 Hours, 24-36 Hours, 36-48 Hours, 48-60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg4770.8

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Cohort 3: AUC(0-tau) of Gepotidacin in Plasma First Dose of 3000 mg (First Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg29.8

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Cohort 3: AUC(0-tau) of Gepotidacin in Plasma After the Second Dose of 3000 mg (Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours* micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg41.9

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Cohort 3: AUC(0-t) of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*nanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg23.3
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg44.8

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Cohort 3: AUC(0-t) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48, 60 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg85.2

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Cohort 3: AUC(0-t) of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*picograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg25353.1
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg30842.3

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Cohort 3: AUC(0-infinity) of Midazolam in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of midazolam was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*nanograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg24.9
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg47.4

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Cohort 3: AUC(0-infinity) of Digoxin in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of digoxin was conducted using standard non-compartmental analysis. Analysis was performed using a linear mixed-effect model with treatment as a fixed effect and participant as a random effect. Geometric LS mean and 90 % CI of the geometric LS means have been presented. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 24 Hours, 36 Hours, 48 Hours, 72 Hours, 96 Hours Post-dose in each Treatment Periods 1 and 2

InterventionHours*picograms per milliliter (Geometric Least Squares Mean)
Cohort 3: Digoxin 0.5 mg + Midazolam 2 mg30743.6
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg34456.5

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Cohort 3: AUC(0-48) of Gepotidacin in Plasma Following Two 3000 mg Doses (First Dose + Second Dose)

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hours, 2 Hours 30 minutes, 3, 4, 6, 8, 12 Hours, 12 Hours 30 minutes, 13 Hours, 13 Hours 30 Hours, 14 Hours, 14 Hours 30 Hours, 15, 16,18,20,24,36, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours*micrograms per milliliter (Geometric Mean)
Cohort 3:Gepotidacin 3000 mg + Digoxin 0.5 mg + Midazolam 2 mg81.2

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Cohort 4: T1/2 of Gepotidacin Following Single Dose of 1500 mg in Plasma

Blood samples were collected at indicated time points. Pharmacokinetic analysis of gepotidacin was conducted using standard non-compartmental analysis. (NCT04493931)
Timeframe: Pre-dose, 30 minutes, 1 Hour, 1 Hour 30 minutes, 2 Hour, 2 Hours 30 minutes, 3 Hours, 4 Hours, 6 Hours, 8 Hours, 12 Hours, 24 Hours, 36 Hours, 48 Hours post-dose in each Treatment Periods 1 and 2

InterventionHours (Geometric Mean)
Cohort 4: Gepotidacin 1500 mg Fed12.848
Cohort 4: Gepotidacin 1500 mg Fasted12.540

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Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Vss/F) of Verinurad and Allopurinol

Vss/F of verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionLiters (Geometric Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol1768174.5
Period 2: Verinurad + Allopurinol + Cyclosporine385.2208.0
Period 3: Verinurad + Allopurinol + Rifampicin685.0179.9

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Volume of Distribution (Apparent) at Steady State Following Extravascular Administration (Based on the Terminal Phase) (Vz/F) of Verinurad and Allopurinol

Vz/F of verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionLiters (Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol2455133.5
Period 2: Verinurad + Allopurinol + Cyclosporine721.8137.9
Period 3: Verinurad + Allopurinol + Rifampicin1153122.6

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Time to Reach Peak or Maximum Plasma Concentration (Tmax) for Verinurad, M1, M8, Allopurinol and Oxypurinol

tmax of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionHours (Median)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol4.034.024.520.504.00
Period 2: Verinurad + Allopurinol + Cyclosporine5.005.988.001.004.00
Period 3: Verinurad + Allopurinol + Rifampicin4.004.005.001.003.00

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Terminal Elimination Rate Constant (λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol

λz of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Intervention1/Hours (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol0.038420.042930.041630.57700.03086
Period 2: Verinurad + Allopurinol + Cyclosporine0.061010.065180.044970.56160.03169
Period 3: Verinurad + Allopurinol + Rifampicin0.055570.064170.051330.59500.02990

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Number of Participants With Adverse Events (AEs) and Serious AEs (SAEs)

Assessment the safety and tolerability of verinurad and allopurinol in combination with cyclosporine or rifampicin (NCT04532918)
Timeframe: From screening (Day -28 to -2) until Follow-up or Early Termination (7-14 days after last verinurad dose)

,,
InterventionParticipants (Count of Participants)
Any AEAny AE with outcome = deathAny SAEAny AE leading to discontinuation of study drugAny AE leading to withdrawal from study
Period 1: Verinurad + Allopurinol20000
Period 2: Verinurad + Allopurinol + Cyclosporine100011
Period 3: Verinurad + Allopurinol + Rifampicin30100

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Metabolite:Parent (MP) Cmax Ratios for M1 and M8: Verinurad

Metabolite:parent (MP) Cmax ratios for M1 and M8: verinurad when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionRatio (Geometric Mean)
M1: verinuradM8: verinurad
Period 1: Verinurad + Allopurinol1.2961.171
Period 2: Verinurad + Allopurinol + Cyclosporine1.3880.1130
Period 3: Verinurad + Allopurinol + Rifampicin1.8660.2300

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Metabolite:Parent (MP) AUClast Ratios for M1 and M8: Verinurad

Metabolite:parent (MP) AUClast ratios for M1 and M8: verinurad when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionRatio (Geometric Mean)
M1:verinuradM8:verinurad
Period 1: Verinurad + Allopurinol1.4001.278
Period 2: Verinurad + Allopurinol + Cyclosporine1.6390.2491
Period 3: Verinurad + Allopurinol + Rifampicin1.9550.5491

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Metabolite:Parent (MP) AUCinf Ratios for M1 and M8: Verinurad

Metabolite:parent (MP) AUCinf ratios for M1 and M8: verinurad when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionRatio (Geometric Mean)
M1:verinuradM8:verinurad
Period 1: Verinurad + Allopurinol1.3241.222
Period 2: Verinurad + Allopurinol + Cyclosporine1.6210.2834
Period 3: Verinurad + Allopurinol + Rifampicin1.9190.5604

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Mean Residence Time of the Unchanged Drug in the Systemic Circulation (MRTinf) for Verinurad and Allopurinol

MRTinf for verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionHours (Geometric Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol21.282.316
Period 2: Verinurad + Allopurinol + Cyclosporine11.052.713
Period 3: Verinurad + Allopurinol + Rifampicin12.602.496

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Geometric Mean Ratio of AUCinf for Verinurad Metabolites: M1 and M8

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad metabolites M1 and M8. AUCinf ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
M1M8
Period 1: Verinurad + Allopurinol119.5110.3
Period 2: Verinurad + Allopurinol + Cyclosporine348.760.98
Period 3: Verinurad + Allopurinol + Rifampicin264.977.35

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Geometric Mean Ratio of AUCinf for Allopurinol and Oxypurinol

Evaluation of a single dose of cyclosporine or rifampicin on the PK of allopurinol and oxypurinol. AUCinf ratio of geometric means of test geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol3982196500
Period 2: Verinurad + Allopurinol + Cyclosporine3914181900
Period 3: Verinurad + Allopurinol + Rifampicin4163195500

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Area Under Plasma Concentration-time Curve From Zero to 24 Hours Post-dose AUC(0-24) of Verinurad, M1, M8, Allopurinol and Oxypurinol

AUC(0-24) of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol62.0286.2379.803982100700
Period 2: Verinurad + Allopurinol + Cyclosporine192.2314.438.02391495080
Period 3: Verinurad + Allopurinol + Rifampicin118.4242.948.81416398460

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Geometric Mean Ratio of AUClast for Verinurad Metabolites: M1 and M8

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad metabolites M1 and M8. AUClast ratio of geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
M1M8
Period 1: Verinurad + Allopurinol111.6101.8
Period 2: Verinurad + Allopurinol + Cyclosporine341.951.95
Period 3: Verinurad + Allopurinol + Rifampicin260.673.23

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Geometric Mean Ratio of AUClast for Allopurinol and Oxypurinol

Evaluation of a single dose of cyclosporine or rifampicin on the PK of allopurinol and oxypurinol. AUClast ratio of geometric means of test geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionh*ng/mL (Geometric Mean)
AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol3889183600
Period 2: Verinurad + Allopurinol + Cyclosporine3821170600
Period 3: Verinurad + Allopurinol + Rifampicin4080182100

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Apparent Total Body Clearance of Drug From Plasma After Extravascular Administration (CL/F) for Verinurad and Allopurinol

CL/F for verinurad and allopurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionLiter/Hours (Mean)
VerinuradAllopurinol
Period 1: Verinurad + Allopurinol92.3077.12
Period 2: Verinurad + Allopurinol + Cyclosporine36.3278.09
Period 3: Verinurad + Allopurinol + Rifampicin55.9973.29

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Geometric Mean Ratio of Maximum Observed Plasma Peak Concentration (Cmax) for Verinurad

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad. Verinurad Cmax ratio of geometric mean of test treatment (verinurad+allopurinol with [cyclosporine or rifampicin], relative to reference treatment (verinurad+allopurinol alone) in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

Interventionng/mL (Geometric Mean)
Period 1: Verinurad + Allopurinol13.30
Period 2: Verinurad + Allopurinol + Cyclosporine33.96
Period 3: Verinurad + Allopurinol + Rifampicin26.09

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Geometric Mean Ratio of Area Under the Plasma Concentration-time Curve From Zero to Time of Last Quantifiable Concentration (AUClast) for Verinurad

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad. Verinurad AUClast ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

Interventionh*ng/mL (Geometric Mean)
Period 1: Verinurad + Allopurinol79.67
Period 2: Verinurad + Allopurinol + Cyclosporine208.6
Period 3: Verinurad + Allopurinol + Rifampicin133.4

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Half-life Associated With Terminal Slope (λz) of a Semi-logarithmic Concentration Time Curve (t½λz) of Verinurad, M1, M8, Allopurinol and Oxypurinol

t½λz of verinurad, M1, M8, allopurinol and oxypurinol when verinurad+allopurinol administered alone or in combination with cyclosporine or rifampicin in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
InterventionHours (Mean)
VerinuradM1M8AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol20.3118.0418.251.21023.19
Period 2: Verinurad + Allopurinol + Cyclosporine14.7313.0521.901.26122.36
Period 3: Verinurad + Allopurinol + Rifampicin15.0312.5214.891.17023.76

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Geometric Mean Ratio of Cmax for Verinurad Metabolites: M1 and M8

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad metabolites M1 and M8. Cmax ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionng/mL (Geometric Mean)
M1M8
Period 1: Verinurad + Allopurinol17.2415.57
Period 2: Verinurad + Allopurinol + Cyclosporine47.143.839
Period 3: Verinurad + Allopurinol + Rifampicin48.706.002

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Geometric Mean Ratio of Cmax for Allopurinol and Oxypurinol

Evaluation of a single dose of cyclosporine or rifampicin on the PK of allopurinol and oxypurinol. Cmax ratio of geometric means of test geometric means of test treatment, relative to reference treatment in each treatment period is reported. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

,,
Interventionng/mL (Geometric Mean)
AllopurinolOxypurinol
Period 1: Verinurad + Allopurinol19476064
Period 2: Verinurad + Allopurinol + Cyclosporine14575876
Period 3: Verinurad + Allopurinol + Rifampicin15976051

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Geometric Mean Ratio of Area Under Plasma Concentration-time Curve From Time Zero to Infinity (AUCinf) for Verinurad

Evaluation of a single dose of cyclosporine or rifampicin on the PK of verinurad. Verinurad AUCinf ratio of geometric means of test treatment, relative to reference treatment in each treatment period. (NCT04532918)
Timeframe: Days 1 to 5 (pre-dose and post-dose)

Interventionh*ng/mL (Geometric Mean)
Period 1: Verinurad + Allopurinol90.25
Period 2: Verinurad + Allopurinol + Cyclosporine215.1
Period 3: Verinurad + Allopurinol + Rifampicin138.0

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Number of Participants Reported One or More Treatment-Emergent Adverse Events (TEAEs)

(NCT05098041)
Timeframe: From Day 1 of Period 1 up to 15 days after the last dose of Soticlestat in Period 2 (up to Day 31)

InterventionParticipants (Count of Participants)
Soticlestat 300 mg Alone2
Rifampin 600 mg Alone1
Soticlestat 300 mg + Rifampin 600 mg2

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Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for Soticlestat When Administered Alone and With Rifampin

(NCT05098041)
Timeframe: Soticlestat Alone: Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose in Period 1; Soticlestat with Rifampin: Day 11 pre-dose and at multiple time points (up to 72 hours) post-dose in Period 2

Interventionhour (Median)
Soticlestat 300 mg Alone0.504
Soticlestat 300 mg + Rifampin 600 mg0.499

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AUC∞: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for Soticlestat When Administered Alone and With Rifampin

(NCT05098041)
Timeframe: Soticlestat Alone: Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose in Period 1; Soticlestat with Rifampin: Day 11 pre-dose and at multiple time points (up to 72 hours) post-dose in Period 2

Interventionnanogram*hour per milliliter(ng*hr/mL) (Geometric Mean)
Soticlestat 300 mg Alone1448
Soticlestat 300 mg + Rifampin 600 mg226.2

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AUClast: Area Under the Plasma Concentration-time Curve From Time 0 to the Time of the Last Quantifiable Concentration for Soticlestat When Administered Alone and With Rifampin

(NCT05098041)
Timeframe: Soticlestat Alone: Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose in Period 1; Soticlestat with Rifampin: Day 11 pre-dose and at multiple time points (up to 72 hours) post-dose in Period 2

Interventionng*hr/mL (Geometric Mean)
Soticlestat 300 mg Alone1290
Soticlestat 300 mg + Rifampin 600 mg190.6

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Cmax: Maximum Observed Plasma Concentration for Soticlestat When Administered Alone and With Rifampin

(NCT05098041)
Timeframe: Soticlestat Alone: Day 1 pre-dose and at multiple timepoints (up to 96 hours) post-dose in Period 1; Soticlestat with Rifampin: Day 11 pre-dose and at multiple time points (up to 72 hours) post-dose in Period 2

Interventionnanogram per milliliter (ng/mL) (Geometric Mean)
Soticlestat 300 mg Alone1364
Soticlestat 300 mg + Rifampin 600 mg176.8

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