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cephalexin

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Description

Cephalexin is a first-generation cephalosporin antibiotic. It is a semi-synthetic derivative of cephalosporin C, a naturally occurring antibiotic produced by the fungus Cephalosporium acremonium. Cephalexin is widely used to treat bacterial infections, including skin infections, respiratory tract infections, urinary tract infections, and ear infections. The drug acts by inhibiting the synthesis of peptidoglycan, a major component of bacterial cell walls. Cephalexin is administered orally and is available in capsule, tablet, and suspension forms. It is generally well-tolerated, but side effects may include diarrhea, nausea, and vomiting. Cephalexin is an important antibiotic because it is effective against a wide range of bacteria, including gram-positive and gram-negative organisms. It is also relatively safe for most patients. Cephalexin is studied to investigate its efficacy and safety in treating various bacterial infections and to explore its potential for new therapeutic applications.'

Cephalexin: A semisynthetic cephalosporin antibiotic with antimicrobial activity similar to that of CEPHALORIDINE or CEPHALOTHIN, but somewhat less potent. It is effective against both gram-positive and gram-negative organisms. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

cephalexin : A semisynthetic first-generation cephalosporin antibiotic having methyl and beta-(2R)-2-amino-2-phenylacetamido groups at the 3- and 7- of the cephem skeleton, respectively. It is effective against both Gram-negative and Gram-positive organisms, and is used for treatment of infections of the skin, respiratory tract and urinary tract. [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]

6-chlorohydroxyquinol: structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID27447
CHEMBL ID1727
CHEBI ID3534
SCHEMBL ID2961
MeSH IDM0003820
PubMed CID440980
CHEBI ID2177
SCHEMBL ID12804729
MeSH IDM0003820

Synonyms (233)

Synonym
BRD-K90733503-002-03-6
(6r,7r)-7-{[(2r)-2-amino-2-phenylacetyl]amino}-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
BPBIO1_000501
PRESTWICK3_000358
BSPBIO_000455
15686-71-2
cephalexin
cefalexin
C06895
5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid, 7-[[(2r)-aminophenylacetyl]amino]-3-methyl-8-oxo-, (6r,7r)-
(6r,7r)-7-[[(2r)-2-amino-2-phenyl-acetyl]amino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
MLS000759527
smr000338536
cephalexin anhydrous
anhydrous cefalexin
cefalexin anhydrous
7-(d-alpha-aminophenylacetamido)desacetoxycephalosporanic acid
DB00567
7-beta-(d-alpha-amino-alpha-phenylacetylamino)-3-methyl-3-cephem-4-carboxylic acid
NCGC00159522-02
anhydrous cephalexin
D00263
cefalexin (jp17)
cex
keflex (tn)
syncle
mamlexin
keflex
check
cefax
cepexin
carnosporin
roceph distab
ceporexin-e
cefalexina [inn-spanish]
larixin
cephin
lenocef
pectril
l-keflex
sepexin
fexin
synecl
lilly 66873
cophalexin
sencephalin
kefalospes
oroxin
keflet
hsdb 3022
cefalin
kefolan
neokef
factagard
pyassan
voxxim
syncl
cefovit
lonflex
sanaxin
cepol
ceporex
neolexina
nufex
cephalexine
brn 0965503
ibrexin
oracef
cepastar
zozarine
uphalexin
lafarine
cephalexinum
celexin
durantel
ceporex forte
servispor
kekrinal
cefaseptin
felexin
sporicef
ceporexin
cefadal
alexin
cefablan
medoxine
cephanasten
cefa-iskia
lopilexin
ceporexine
sporidex
inphalex
roceph
lexibiotico
alsporin
ospexin
sartosona
alcephin
kidolex
einecs 239-773-6
sialexin
tokiolexin
7-(d-2-amino-2-phenylacetamido)-3-methyl-delta3-cephem-4-carboxylic acid
cefalexinum [inn-latin]
madlexin
cephacillin
cefalessina [dcit]
5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(2-amino-2-phenylacetamido)-3-methyl-8-oxo-, d-
ceforal
erocetin
ed a-ceph
7-(d-2-amino-2-phenylacetamido)-3-methyl-delta (sup 3)-cephem-4- carboxylic acid
cefadin
cefaleksin
s 6437
cefalexine [inn-french]
winlex
cefaloto
oriphex
cephaxin
cefadina
ibilex
ortisporina
sinthecillin
5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((aminophenylacetyl)amino)-3-methyl-8-oxo-, (6r-(6alpha,7beta(r*)))-
tepaxin
5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-(((2r)-aminophenylacetyl)amino)-3-methyl-8-oxo-, (6r,7r)-
(6r,7r)-7-((r)-2-amino-2-phenylacetamido)-3-methyl-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-en-2-carbonsaeure
mamalexin
durantel ds
cephalexin [usan:ban]
PRESTWICK1_000358
SPBIO_002376
PRESTWICK0_000358
PRESTWICK2_000358
NCGC00159522-03
HMS2051A04
bdbm50139896
(6r,7r)-7-((r)-2-amino-2-phenylacetamido)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
(6r,7r)-7-((r)-2-amino-2-phenyl-acetylamino)-3-methyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
CHEMBL1727 ,
cefalexinum
CHEBI:3534 ,
cefalexina
cefalexine
7beta-[(2r)-2-amino-2-phenylacetamido]-3-methyl-3,4-didehydrocepham-4-carboxylic acid
(6r,7r)-7-[[(2r)-2-amino-2-phenylacetyl]amino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
AKOS004119846
nsc 758162
cerexins
optocef
unii-5sff1w6677
cefalexin [inn]
ceflax
5sff1w6677 ,
panixine disperdose
cerexin
dtxsid9022780 ,
dtxcid002780
cas-15686-71-2
tox21_111740
MLS001424036
BCP9000509
cefalessina
CCG-100831
cephalexin 1-hydrate
BCPP000289
EPITOPE ID:117132
taicelexin
(6r,7r)-7-[(2r)-2-amino-2-phenylacetamido]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
gtpl4832
cefalexin [jan]
(6r,7r)-7-((r)-2-amino-2-phenylacetamido)-3-methyl-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
cefalexin [who-dd]
kefloridina
s-6437 ,
oracocin
cephamasten
cephalexin [mi]
5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid, 7-((aminophenylacetyl)amino)-3-methyl-8-oxo-,(6r-(6.alpha.,7.beta.(r*)))-
iwalexin
efalexin
garasin
cephalexin [hsdb]
lilly-66873
7-(d-.alpha.-amino-.alpha.-phenylacetamido)-3-methyl-3-cephem-4-carboxylic acid
cefadros
HY-B0200
CS-2137
NC00081
SCHEMBL2961
tox21_111740_1
NCGC00159522-05
ZAIPMKNFIOOWCQ-UEKVPHQBSA-N
C-2660
cephalexin monohydrate, antibiotic for culture media use only
Q-200819
cephalexin, antibiotic for culture media use only
cephalexin, pharmaceutical secondary standard; certified reference material
(6r,7r)-7-((r)-2-amino-2-phenylacetamido)-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
cefalexin, vetranal(tm), analytical standard
cefalexin, british pharmacopoeia (bp) reference standard
7-(d-2-amino-2-phenylacetamido)-3-methyl-delta (sup 3)-cephem-4-carboxylic acid
Q411417
cephalexin (cefalexin)
DS-11971
cefalexin,(s)
H10995
amplex
Z1880962282
cefalexin 1000 microg/ml in acetonitrile:water
cephalexin (usp-rs)
7-(d-alpha-amino-alpha-phenylacetamido)-3-methyl-3-cephem-4-carboxylic acid
cefalexin monohydrate (ep impurity)
cephalexin (usp monograph)
(6r,7r)-7-(((2r)-2-amino-2-phenylacetyl)amino)-3-methyl-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
(6r,7r)-7-((2r)-2-amino-2-phenylacetylamino)-3-methyl-8-oxo-5-thia-1-azabicyclo(4.2.0)oct-2-ene-2-carboxylic acid
7beta-((2r)-2-amino-2-phenylacetamido)-3-methyl-3,4-didehydrocepham-4-carboxylic acid
cefalexin monohydrate (ep monograph)
C06328
6-chlorohydroxyquinol
6-chlorobenzene-1,2,4-triol
6-chloro-1,2,4-trihydroxybenzene
2-chlorobenzene-1,4,6-triol
6-CHQ
AC1L9ABM ,
1,2,4-benzenetriol, 6-chloro-
ACMC-20N5WK ,
150097-90-8
SCHEMBL12804729
CHEBI:2177
DTXSID60331549
Q27105571

Research Excerpts

Overview

Cephalexin is a first-generation cephalosporin with antimicrobial sensitivity ranging from Gram-positive to Gram-negative organisms. It is a promising alternative treatment for acne, with 78% of patients exhibiting at least some clinical improvement.

ExcerptReferenceRelevance
"Cephalexin is a first-generation cephalosporin with antimicrobial sensitivity ranging from Gram-positive to Gram-negative organisms."( A rare case of cephalexin-induced acute interstitial nephritis with hypokalemic periodic paralysis.
Kumar, R; Sharma, K; Singh, AK; Talwar, V,
)
1.21
"Cephalexin (CEX) is an antibiotic commonly used to treat bacterial infections in humans and animals. "( Degradation of micropollutant cephalexin by ultraviolet (UV) and assessment of residual antimicrobial activity of transformation products.
Cordeiro, SG; Costa, B; Ethur, EM; Haas, P; Heidrich, D; Hoehne, L; Kuhn, D; Schweizer, YA; Steffens, C; Weber, AC; Ziem, R, 2021
)
2.35
"Cephalexin is a first generation cephalosporin commonly used in dogs for treatment of pyoderma. "( Selection of CMY-2 producing Escherichia coli in the faecal flora of dogs treated with cephalexin.
Damborg, P; Gaustad, IB; Guardabassi, L; Olsen, JE, 2011
)
2.03
"Cephalexin is a promising alternative treatment for acne, with 78% of patients exhibiting at least some clinical improvement."( Oral cephalexin for acne vulgaris: clinical experience with 93 patients.
Fenner, JA; Levin, NA; Wiss, K,
)
1.37
"Cephalexin is an oral cephalosporin which is widely used in the treatment of urinary tract infections. "( Cephalexin in the therapy of infections of the urinary tract.
Weinstein, AJ, 1983
)
3.15
"Cephalexin is a constituent of the cephalosporin group used for the treatment of bronchitis and other heart diseases due to its enhanced oral activity. "( Bioaugmentation and treatment of cephalexin drug-based pharmaceutical effluent in an upflow anaerobic fluidized bed system.
Krishnaiah, K; Murthy, DV; Saravanane, R, 2001
)
2.03
"Cephalexin appears to be a highly effective antibiotic. "( Cephalexin: clinical and laboratory evaluation in infants and children.
Riley, HD; Rudoy, RC, 1977
)
3.14
"Cephalexin is a more effective drug than penicillin in the treatment of group A beta-hemolytic streptococcal throat infection in children."( Cephalexin and penicillin in the treatment of group A beta-hemolytic streptococcal throat infections.
Blumer, JL; Dillon, H; Disney, FA; Dudding, BA; McLinn, SE; Nelson, DB; Selbst, SM, 1992
)
3.17

Effects

Cephalexin has an antimicrobial spectrum that includes those pathogens most frequently encountered in clinical practice. No bioequivalence problems have been reported.

Cephalexin has an antimicrobial spectrum that includes those pathogens most frequently encountered in clinical practice. No bioequivalence problems have been reported. CephaleXin has had 12 years of extensive clinical usage in the management of respiratory tract and other infections.

ExcerptReferenceRelevance
"Cephalexin has a wide therapeutic index and no bioequivalence problems have been reported."( Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Cephalexin Monohydrate.
Abrahamsson, B; Cristofoletti, R; Dressman, J; Groot, DW; Langguth, P; Mehta, MU; Parr, A; Plöger, GF; Polli, JE; Quizon, PM; Shah, VP; Tajiri, T, 2020
)
1.51
"Cephalexin has an antimicrobial spectrum that includes those pathogens most frequently encountered in clinical practice. "( The pharmacology of cephalexin.
Griffith, RS, 1983
)
2.03
"Cephalexin has a wide therapeutic index and no bioequivalence problems have been reported."( Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Cephalexin Monohydrate.
Abrahamsson, B; Cristofoletti, R; Dressman, J; Groot, DW; Langguth, P; Mehta, MU; Parr, A; Plöger, GF; Polli, JE; Quizon, PM; Shah, VP; Tajiri, T, 2020
)
1.51
"Cephalexin has in vitro activity against methicillin-susceptible Staphylococcus aureus, a predominant pathogen in osteoarticular infection."( Pharmacokinetics and pharmacodynamics of oral cephalexin in children with osteoarticular infections.
Autmizguine, J; Kassir, N; Laferrière, C; Ovetchkine, P; Parent, S; Tapiéro, B; Théorêt, Y; Watt, KM, 2013
)
1.37
"Cephalexin has been noted to be efficacious in some instances."( Oral cephalexin for acne vulgaris: clinical experience with 93 patients.
Fenner, JA; Levin, NA; Wiss, K,
)
1.37
"Cephalexin has an antimicrobial spectrum that includes those pathogens most frequently encountered in clinical practice. "( The pharmacology of cephalexin.
Griffith, RS, 1983
)
2.03
"Cephalexin has had 12 years of extensive clinical usage in the management of respiratory tract and other infections. "( Cephalexin in lower respiratory tract infections.
Raff, MJ, 1983
)
3.15

Treatment

Oral treatment with cephalexin resulted in bacteriologic cure in 24 of 25 (96%) dogs with urinary tract infection caused by Klebsiella pneumoniae.

ExcerptReferenceRelevance
"Cephalexin had an 87% treatment success rate without recurrence during a median follow-up of 119 (IQR, 48.5-350) days."( Effectiveness of oral cephalexin in antibiotic-course completion for methicillin-susceptible Staphylococcus aureus-induced bacteremic vertebral osteomyelitis.
Hayakawa, K; Mezaki, K; Ohmagari, N; Okumura, N; Yamada, G; Yamamoto, K, 2023
)
1.95
"Oral treatment with cephalexin resulted in bacteriologic cure in 24 of 25 (96%) dogs with urinary tract infection caused by Klebsiella pneumoniae. "( Cephalexin for oral treatment of canine urinary tract infection caused by Klebsiella pneumoniae.
Ling, GV; Ruby, AL, 1983
)
2.03
"Treatment with cephalexin 1 g twiec daily and cotrimoxazole 2 tablets twice daily was compared in a double-blind, randomised study of 100 women with urinary tract infections. "( Comparative double-blind study of cephalexin and co-trimoxazole in urinary tract infections.
Gower, PE; Tasker, PR, 1976
)
0.89

Toxicity

ExcerptReferenceRelevance
" The results of these studies indicate that cefaclor has a low toxic potential in the species tested."( An evaluation of the toxicity of cefaclor in laboratory animals.
Gibson, WR; Hanasono, GK; Hoffman, DG; Morton, DM; Owen, NV, 1979
)
0.26
" Overall clinical and bacteriologic responses were nearly identical in the two groups, and both antibiotics proved to equally safe and effective for use paediatric practice."( Comparative efficacy and safety of cephradine and cephalexin in children.
Mouallem, R, 1976
)
0.51
" Both biotin and sulfathiazole are shown to be promising candidates for use in the suppression of the adverse effects of cisplatin, and other sulfur-containing compounds currently in clinical use may have equivalent or superior properties in this respect."( Control of the nephrotoxicity of cisplatin by clinically used sulfur-containing compounds.
Basinger, MA; Holscher, MA; Jones, MM, 1992
)
0.28
" The response to therapy and adverse reaction rate did not differ between groups."( Prospective randomized study comparing the efficacy and safety of ciprofloxacin with cefaclor in the treatment of patients with purulent bronchitis.
Davis, RL; Neidhart, MM; Quenzer, RW,
)
0.13
" Adverse effects were not reported during the study."( Safety and efficacy of cefixime versus cefaclor in respiratory tract infections.
Dorow, P, 1989
)
0.28
"Cephaloglycin (Cgl) and cephaloridine (Cld) are acutely toxic to the proximal renal tubule, in part because of their cellular uptake by a contraluminal anionic secretory carrier and in part through their intracellular attack on the mitochondrial transport and oxidation of tricarboxylic acid (TCA) cycle anionic substrates."( Toxicity of cephalosporins to fatty acid metabolism in rabbit renal cortical mitochondria.
Hsu, CY; Tune, BM, 1995
)
0.29
" Cld has little or no in vivo toxicity to mitochondrial butyrate metabolism, whereas in vivo Cgl is as toxic as Cld to respiration with PCarn."( Toxicity of cephalosporins to fatty acid metabolism in rabbit renal cortical mitochondria.
Hsu, CY; Tune, BM, 1995
)
0.29
" Mupirocin cream was as well tolerated as cephalexin; 9% and 13% of patients reported adverse events related or possibly related to study medication in the mupirocin and cephalexin groups, respectively."( A comparison of the efficacy and safety of mupirocin cream and cephalexin in the treatment of secondarily infected eczema.
Bushnell, WD; Capin, LR; Cupo, MA; Parish, LC; Rist, T; Sulica, V, 2002
)
0.82
"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
)
0.32
"The contamination of surface and ground water by antibiotics is of significant importance due to their potential chronic toxic effects to the aquatic and human lives."( Electrochemical mineralization of cephalexin using a conductive diamond anode: A mechanistic and toxicity investigation.
Aquino, JM; Coledam, DAC; Eguiluz, KIB; Pupo, MMS; Salazar-Banda, GR; Silva, AJ; Silva, BF, 2017
)
0.73

Pharmacokinetics

Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties. CephaleXin increased Cmax and AUC by an average of 34% and 24%, respectively, and reduced renal clearance to 14%.

ExcerptReferenceRelevance
"A review is given on the pharmacokinetic characteristics of some cephalosporin antibiotics."( On the pharmacokinetics of cephalosporin antibiotics.
Andersson, KE, 1978
)
0.26
"The pharmacokinetic distribution of 10 cephalosporin compounds, cephalothin, cephaloridine, cephaloglycine, cephalexin, cefazolin, cephapirin, cephradine, cephacentrile, cefoxitin, and cefamandole, in patients with various degrees of renal function was reviewed."( Pharmacokinetics of cephalosporins in patients with normal or reduced renal function.
Andriole, VT, 1978
)
0.47
"Cefadroxil (Duricef, Mead Johnson and Company), resembles cephalexin and cephradine in spectrum of antibacterial activity but differs in human pharmacokinetic properties."( Bactericidal activity of cefadroxil, cephalexin, and cephradine in an in vitro pharmacokinetic model.
Buck, RE; Goodhines, RA; Leitner, F; Price, KE, 1979
)
0.78
"1 min; the half-life was 42."( [Pharmacokinetics of cefaclor and initial therapeutical experience (author's transl)].
Köppe, P; Lode, H; Stahlmann, R, 1979
)
0.26
" The effects of protein binding of some of the commonly used cephalosporins on antibacterial activity and several pharmacokinetic parameters are discussed in this communication."( Pharmacokinetics of cephalosporin antibiotics: protein-binding considerations.
Heald, AF; Schreiber, EC; Singhvi, SM, 1978
)
0.26
" In a comparative evaluation of nine different cephalosporin antibiotics, not only the objective antibacterial and pharmacokinetic properties are taken into consideration, but also the dosage recommendations of the manufacturers as subjective factors."( [Cephalosporin antibiotics from microbiologic viewpoint. A comparison of antibacterial and pharmacokinetic properties].
Naumann, P, 1975
)
0.25
" The elimination half-life of cefprozil (1."( Comparison of cefprozil and cefaclor pharmacokinetics and tissue penetration.
Barbhaiya, RH; Gleason, CR; Pittman, KA; Shukla, UA; Shyu, WC; Wilber, RB, 1990
)
0.28
"The dependence of the antibacterial activity of the two oral cephalosporins cefixime and cefaclor on pharmacokinetic properties was investigated in an in vitro model using strains of enterobacteria and a streptococcal strain."( Comparative activity of cefixime and cefaclor in an in vitro model simulating human pharmacokinetics.
Nies, BA, 1989
)
0.28
" LMOX disappeared from plasma in a monoexponential manner with a half-life of 43 min after intravenous administration at a dose of 50 mg/kg."( Ocular pharmacokinetics of latamoxef and cefaclor in rabbits. Penetration into aqueous humor.
Arai, S; Fukuchi, H; Kimura, M; Kitaura, T; Miyake, K; Tsukiai, S, 1988
)
0.27
" Although the pharmacokinetic characteristics of the drugs after intravenous injection were similar to other beta-lactam antibiotics, significant differences between the cephalosporins examined were found in respect of certain kinetic parameters."( Clinical pharmacokinetics of five oral cephalosporins in calves.
Kurtz, B; Paz, R; Soback, S; Ziv, G, 1987
)
0.27
"A three-way crossover study was carried out in 10 dogs and nine cats to establish the pharmacokinetic parameters of the semi-synthetic cephalosporin antibiotic, cephalexin sodium, when administered orally, subcutaneously or intramuscularly."( Pharmacokinetics of cephalexin in dogs and cats after oral, subcutaneous and intramuscular administration.
Rudd, AP; Silley, P; Symington, WM; Tait, AJ, 1988
)
0.79
"Cefadroxil is an oral cephalosporin which is similar to cephalexin and cephradine in structure and spectrum of antibacterial activity, but has different pharmacokinetic properties."( Cefadroxil. A review of its antibacterial, pharmacokinetic and therapeutic properties in comparison with cephalexin and cephradine.
Santella, PJ; Tanrisever, B, 1986
)
0.73
" This review addresses the clinical pharmacokinetic aspects of drug therapy in patients undergoing peritoneal dialysis and considers: the efficiency of the peritoneal membrane as a dialysing membrane; the effects of peritoneal dialysis on the pharmacokinetics of drugs; the pharmacokinetic models and estimation methods for peritoneal dialysis clearance and the effects of peritoneal dialysis on drug elimination; the influence of the pharmacokinetic parameters of drugs on drug dialysability; and the application of pharmacokinetic principles to the adjustment of drug dosage regimens in peritoneal dialysis patients."( Drug therapy in patients undergoing peritoneal dialysis. Clinical pharmacokinetic considerations.
Cornish, WR; Hardy, BG; Manuel, MA; Paton, TW,
)
0.13
"The effect of cefaclor on the steady state pharmacokinetics of theophylline was investigated in healthy young adults by comparing the pharmacokinetic parameters as found during a nine days course of theophylline alone and as obtained during co-medication with the antibiotic cefaclor."( Clinical pharmacokinetics of theophylline during co-treatment with cefaclor.
Hempenius, J; Holtkamp, A; Jonkman, JH; Schoenmaker, R; van der Boon, WJ, 1986
)
0.27
"The effect of the antibiotic drug cefaclor on steady state pharmacokinetics of theophylline was studied in healthy adults by comparing the pharmacokinetic parameters as found during a 9 days course of theophylline alone and as obtained during comedication with cefaclor."( No effect of cefaclor on theophylline pharmacokinetics.
Hempenius, J; Holtkamp, A; Jonkman, JH; Schoenmaker, R; van der Boon, WJ, 1985
)
0.27
" The therapeutic significance of the different pharmacokinetic characteristics of cephalexin and cefadroxil, if any, may be a function also of their pharmacologic activity and/or the sensitivity of the target organism."( A pharmacokinetic comparison of cephalexin and cefadroxil using HPLC assay procedures.
Craig, WA; Ifan, A; Johnson, CA; Kwok, F; Marrero, D; Pearson, JG; Rogge, MC; Selen, A; Welling, PG,
)
0.64
"The effects of probenecid on the pharmacokinetic parameters of cefadroxil administered in a single dose of 500 mg are studied."( The pharmacokinetics of cefadroxil associated with probenecid.
Dominguez-Gil, A; Mariño, EL, 1981
)
0.26
"A pharmacokinetic model has been developed, by means of which all possible time courses of the concentrations of antibiotics in the plasma of treated individuals can be exactly simulated in vitro without diluting the test organism and affecting the growth curves."( Antibacterial effects of cefroxadine, cephalexin and cephradine in a new in vitro pharmacokinetic model.
Maurer, M; Schneider, P; Tosch, W; Zak, O, 1982
)
0.54
" The analysis of the pharmacokinetic data obtained with the one-compartmental model showed that the rate of the antibiotic absorption in the rats was higher than that in the dogs."( [Cephalexin pharmacokinetics].
Danilova, VI; Firsov, AA; Koroleva, VG; Vasil'ev, VK, 1981
)
1.17
" The biological half-life of cephalothin was 16 to 54 minutes; the half-life varied directly with increased species body weight, with the exception of the ducks studied."( Pharmacokinetics of cephalothin and cephalexin in selected avian species.
Bush, M; Carpenter, JW; Locke, D; Neal, LA, 1981
)
0.54
"The pharmacokinetic parameters of cefroxadin and cephalexin were compared after simultaneous oral administration of the two cephalosporins to 21 subjects."( Pharmacokinetic comparison of cefroxadin (CGP 9000) and cephalexin by simultaneous administration to humans.
Hirtz, JL; Humbert, G; Lecaillon, JB; Schoeller, JP; Vischer, W, 1980
)
0.76
" The elimination half-life (t1/2) of cefadroxil (about 2 h) was significantly longer than that of cephalexin (about 1 h)."( A pharmacokinetic comparison of cefadroxil and cephalexin after administration of 250, 500 and 1000 mg solution doses.
Barbhaiya, RH, 1996
)
0.77
" The pharmacokinetic factors were analysed using a computer."( Pharmacokinetics of cephalexin in cats after oral administration of the antibiotic in tablet and paste preparations.
Martin, PJ; Thornton, JR, 1997
)
0.62
"There were no significant differences between the peak concentration of cephalexin, or the other pharmacokinetic factors obtained from the tablet and paste formulations."( Pharmacokinetics of cephalexin in cats after oral administration of the antibiotic in tablet and paste preparations.
Martin, PJ; Thornton, JR, 1997
)
0.85
"Oligopeptidic drugs such as beta-lactams and angiotensin-converting enzyme inhibitors share the same carriers in humans and animals, which results in possible pharmacokinetic interactions."( Analysis of the pharmacokinetic interaction between cephalexin and quinapril by a nonlinear mixed-effect model.
Padoin, C; Perret, G; Petitjean, O; Tod, M, 1998
)
0.55
" The other calculated pharmacokinetic parameters were also in the area of the data for dogs stated in the literature."( [Pharmacokinetics of cephalexin from two oral formulations in dogs].
Ehinger, AM; Kietzmann, M,
)
0.45
" Cephalexin increased Cmax and AUC by an average of 34% and 24%, respectively, and reduced renal clearance to 14%."( Effect of cephalexin on the pharmacokinetics of metformin in healthy human volunteers.
Chandrasekhar, K; Jayasagar, G; Krishna Kumar, M; Madhusudan Rao, C; Madhusudan Rao, Y, 2002
)
1.63
"Limited data characterize pharmacokinetic interactions between cephalexin and ranitidine, and no data exist for an interaction with proton pump inhibitors."( A randomized crossover study investigating the influence of ranitidine or omeprazole on the pharmacokinetics of cephalexin monohydrate.
Adejare, A; George, M; Madaras-Kelly, K; May, MP; Michas, P, 2004
)
0.77
"The aims of this study were to describe and compare the pharmacokinetic profiles and T(>MIC90) of two commercially available once-daily recommended cephalexin formulations in healthy adult dogs administered by the intramuscular (i."( Pharmacokinetics of two once-daily parenteral cephalexin formulations in dogs.
Albarellos, G; Ambros, L; Hallu, R; Kreil, V; Montoya, L; Rebuelto, M; Waxman, S, 2005
)
0.79
" The present LC method was successfully applied to the pharmacokinetic studies of coformulated cefalexin dispersible tablets after oral administration to beagle dogs."( Liquid chromatographic method for the simultaneous determination of cefalexin and trimethoprim in dog plasma and application to the pharmacokinetic studies of a coformulated preparation.
Liu, X; Qi, M; Sun, P; Wang, P, 2006
)
0.33
" No differences between treatments were found for other pharmacokinetic parameters."( Metoclopramide modifies oral cephalexin pharmacokinetics in dogs.
Albarellos, G; Kreil, V; Prados, AP; Rebuelto, M; Waxman, S, 2007
)
0.63
" 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
)
0.35
"24microg/ml) and lower half-life (1."( Comparative pharmacokinetics of an injectable cephalexin suspension in beef cattle.
Albarellos, G; Ambros, L; Hallu, R; Kreil, V; Montoya, L; Rebuelto, M; Waxman Dova, S, 2008
)
0.6
"The purpose of this study was to investigate the pharmacokinetic mechanism of interaction between JBP485 (cyclo-trans-4-L-hydroxyprolyl-L-serine, a dipeptide) and cephalexin when they were coadministered in rats."( Pharmacokinetic interaction between JBP485 and cephalexin in rats.
Cang, J; Gao, Y; Kaku, T; Liu, K; Liu, Q; Meng, Q; Sun, H; Wang, C; Zhang, J, 2010
)
0.81
" In the present study, we carried out transport experiments of cephalexin via MATE1 and performed pharmacokinetic analyses of cephalexin in Mate1 knockout [Mate1(-/-)] mice."( Reduced renal clearance of a zwitterionic substrate cephalexin in MATE1-deficient mice.
Inui, K; Katsura, T; Terada, T; Tsuda, M; Watanabe, S, 2010
)
0.85
"The pharmacokinetic profile and bioavailability of a long-acting formulation of cephalexin after intramuscular administration to cats was investigated."( Pharmacokinetics and bioavailability of a long-acting formulation of cephalexin after intramuscular administration to cats.
Albarellos, GA; Landoni, MF; Montoya, L; Quaine, PC, 2011
)
0.83
" Relevant pharmacokinetic parameters were calculated using noncompartmental analysis."( Comparative pharmacokinetics of intravenous cephalexin in pregnant, lactating, and nonpregnant, nonlactating goats.
Ambros, L; Hallu, R; Kreil, V; Monfrinotti, A; Rebuelto, M; Tarragona, L, 2011
)
0.63
" No differences were observed for other pharmacokinetic parameters."( Effects of sodium bicarbonate and ammonium chloride pre-treatments on PEPT2 (SLC15A2) mediated renal clearance of cephalexin in healthy subjects.
Lee, EJ; Limenta, LM; Liu, R; Tan, YL; Tang, AM, 2011
)
0.58
" Standard pharmacokinetic measures and contemporary PK/PD targets were compared."( Probenecid effects on cephalexin pharmacokinetics and pharmacodynamics in healthy volunteers.
Begg, EJ; Begg, R; Chambers, ST; Everts, RJ; Gardiner, SJ; Turnidge, J; Zhang, M, 2021
)
0.94

Compound-Compound Interactions

The phosphonopeptide alafosfalin (L-alanyl-L-1-aminoethylphosphonic acid) exhibited synergy in vitro and in animal studies when combined with cephalexin.

ExcerptReferenceRelevance
"In vitro and in vivo antibacterial activities of cefmetazole alone and in combination with fosfomycin against methicillin- and cephem-resistant (MR) strains of Staphylococcus aureus were investigated, and the mechanism of synergistic effect between cefmetazole and fosfomycin was also studied."( Antibacterial activity of cefmetazole alone and in combination with fosfomycin against methicillin- and cephem-resistant Staphylococcus aureus.
Magaribuchi, T; Ohya, S; Tajima, M; Utsui, Y; Yokota, T, 1986
)
0.27
"The phosphonopeptide alafosfalin (L-alanyl-L-1-aminoethylphosphonic acid) exhibited synergy in vitro and in animal studies against a range of bacterial genera when combined with cephalexin."( Antibacterial properties of alafosfalin combined with cephalexin.
Atherton, FR; Hall, MJ; Hassall, CH; Holmes, SW; Lambert, RW; Lloyd, WJ; Nisbet, LJ; Ringrose, PS; Westmacott, D, 1981
)
0.7
"The purpose of this randomized, single blinded clinical trial was to evaluate cytologically and clinically the efficacy of oral cephalexin alone and its combination with terbinafine or ketoconazole for the treatment of Malassezia dermatitis in dogs."( Comparison of the clinical efficacy of oral terbinafine and ketoconazole combined with cephalexin in the treatment of Malassezia dermatitis in dogs--a pilot study.
Harris, BL; Kunkle, G; Lopez, J; Marsella, R; Nicklin, CF; Rosales, MS, 2005
)
0.76
" These results suggest that the inhibition of MATEs, but not OCT2, is a likely mechanism underlying the drug-drug interactions with cimetidine in renal elimination."( Competitive inhibition of the luminal efflux by multidrug and toxin extrusions, but not basolateral uptake by organic cation transporter 2, is the likely mechanism underlying the pharmacokinetic drug-drug interactions caused by cimetidine in the kidney.
Inoue, K; Ito, S; Kusuhara, H; Sugiyama, Y; Toyoshima, J; Yokochi, M; Yuasa, H, 2012
)
0.38
" This work was designed to investigate the recognition and binding of three typical β-lactam antibiotics including penicillin G (Pen G), penicillin V (Pen V) and cefalexin (Cef) with bovine serum albumin (BSA) by frontal affinity chromatography in combination with UV-vis absorption spectra, fluorescence emission spectra, binding site marker competitive experiment and molecular docking under simulated physiological conditions."( Recognition and binding of β-lactam antibiotics to bovine serum albumin by frontal affinity chromatography in combination with spectroscopy and molecular docking.
Bian, L; Li, Q; Zhang, T, 2016
)
0.43

Bioavailability

Cephalexin was well absorbed based on a mean 24-hour urinary recovery of 89 and 93% in pediatric and adult patients. The proposed procedure for in vitro estimation of the cephaleXin release rate reflects bioavailability of the antibiotic dosage forms and may be used in quality control of finished dosage forms.

ExcerptReferenceRelevance
" The significant parameters of bioavailability of an orally administered substance were determined."( Comparative pharmacokinetics of cephalexin, cefaclor, cefadroxil, and CGP 9000.
Koeppe, P; Lode, H; Stahlmann, R, 1979
)
0.54
" No difference was observed in the overall bioavailability of the three antibiotics based on comparable FD/V values."( The pharmacokinetics of the oral cephalosporins cefaclor, cephradine and cephalexin.
Dean, S; Kendall, MJ; Selen, A; Welling, PG; Wise, R, 1979
)
0.49
" Calculated pharmacokinetic constants indicate that the absorption rate of cefaclor was nearly the same as that of cephalexin."( Serum and sputum levels of cefaclor.
Gatzemeier, U; Simon, C, 1979
)
0.47
" The rate of absorption varied, there being marked differences in the time."( [Investigations on the excretion of cefaclor in human bile (author's transl)].
Fabricius, K; Müller, O; Rückert, U, 1979
)
0.26
" Bioavailability comparisons showed that the prolonged-release formulation was completely available, as was the commercial oral capsule."( Evaluation of an oral prolonged-release antibiotic formulation.
Flanagan, DR; Nightingale, CH; Quintiliani, R; Schneider, H, 1978
)
0.26
" The compounds were only poorly absorbed by the oral route in mice, but the 3-(carboxybenzyl) compounds gave more prolonged useful serum levels than the usual cephalosporins."( Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
Basker, MJ; Brain, EG; Eglington, AJ; James, BG; Mizen, LW; Nayler, JH; Osborne, NF; Pearson, MJ; Smale, TC; Southgate, R; Sutherland, R; Tolliday, P, 1977
)
0.48
" Although the absorption rate decreased as the dose increased, the systemic availability of cefadroxil was essentially complete at all doses, as judged by the 24 h urinary recoveries of the antibiotic."( Dose-dependent absorption and elimination of cefadroxil in man.
Garrigues, TM; Martin, U; Peris-Ribera, JE; Prescott, LF, 1991
)
0.28
" However, these cephems were not well absorbed orally."( Synthesis and biological activity of novel 3-(2-propenyl)-cephalosporins. I.
Kim, H; Kim, WJ; Ko, KY; Oh, J, 1991
)
0.28
" However, the absorption rate of cefaclor is significantly reduced in the presence of food, while that of cefprozil remains unaltered."( Comparison of the effects of food on the pharmacokinetics of cefprozil and cefaclor.
Barbhaiya, RH; Gleason, CR; Pittman, KA; Shukla, UA; Shyu, WC, 1990
)
0.28
" The antacid, pirenzepine, and ranitidine had no influence on the bioavailability of amoxicillin, cephalexin, and amoxicillin-clavulanic acid."( Influence of ranitidine, pirenzepine, and aluminum magnesium hydroxide on the bioavailability of various antibiotics, including amoxicillin, cephalexin, doxycycline, and amoxicillin-clavulanic acid.
Deppermann, KM; Höffken, G; Kalz, C; Koeppe, P; Lode, H; Tschink, G, 1989
)
0.7
" Bioavailability in mice, rats, dogs, and monkeys was determined after oral or parenteral administration."( Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
Cooper, RD; Counter, FT; Draheim, SE; Eudaly, JA; Johnson, RJ; Kukolja, S; Ott, JL; Pfeil-Doyle, J; Quay, JF; Wright, WE, 1988
)
0.27
" The bioavailability of the drugs was about 35 per cent of the administered dose."( Clinical pharmacokinetics of five oral cephalosporins in calves.
Kurtz, B; Paz, R; Soback, S; Ziv, G, 1987
)
0.27
" The various brands did not differ from each other with respect to urinary excretion rate, time to reach the urinary peak height, elimination rate constant and absorption rate constant."( A bioequivalence study of six brands of cephalexin.
Abdulhameed, ME; el-Sayed, YM; Najib, NM; Suleiman, MS, 1988
)
0.54
" The proposed procedure for in vitro estimation of the cephalexin release rate reflects bioavailability of the antibiotic dosage forms and may be used in quality control of finished dosage forms."( [Biopharmaceutical aspects of the medicinal forms of cephalexin].
Berezovskaia, LN; Garsheva, GB; Grakovskaia, LK, 1987
)
0.77
" Tigemonam was well absorbed in laboratory animals and with its excellent gram-negative spectrum of activity should prove of value in oral antibiotic therapy in humans."( In vivo evaluation of tigemonam, a novel oral monobactam.
Bonner, DP; Clark, JM; Dalvi, M; Olsen, SJ; Sykes, RB; Weinberg, DS; Whitney, RR, 1987
)
0.27
" There were no significant differences between capsule and granule forms of S6472 regarding Cmax and AUC, and it was confirmed that bioavailability of both preparations was the same."( [Phase I clinical studies of S6472 (sustained release preparations of cefaclor)].
Iida, M; Ito, M; Matsuda, S; Ohtomo, M; Sonoyama, T; Yasuda, M, 1985
)
0.27
" Cephalexin was well absorbed based on a mean 24-hour urinary recovery of 89 and 93% in pediatric and adult patients."( Cephalexin pharmacokinetics in patients with cystic fibrosis.
Lubin, AH; Nahata, MC; Visconti, JA, 1984
)
2.62
" Bioavailability testing was carried by administering the capsules to four volunteers before storage and after 70 days of storage."( Effect of storage on the bioavailability of cephalexin from its capsules.
Molokhia, AM, 1984
)
0.53
" It is well absorbed when given orally on an empty stomach; absorption is delayed by the presence of food."( Evaluation of cefaclor.
Derry, JE, 1981
)
0.26
" It is concluded that cefaclor is a well absorbed and tolerated cephalosporin for use in newborn infants."( A pharmacological study of cefaclor in the newborn infant.
Chin, KC; Cockburn, F; Kerr, MM; McAllister, TA, 1981
)
0.26
" This showed that cefadroxil was well absorbed from digestive tract, and a major part was excreted rapidly through kidney."( [Clinical results of cefadroxil in children and pharmacokinetics of the drug (author's transl)].
Cho, K; Maruyama, S; Sanae, N; Takimoto, M; Yoshioka, H, 1981
)
0.26
" The significant parameters of bioavailability of an orally administered substance were determined."( [Comparative pharmacokinetics of oral cephalosporins: cephalexin, cefaclor and cefadroxil (author's transl)].
Dzwillo, G; Koeppe, P; Lode, H; Stahlmann, R, 1980
)
0.51
" Oral bioavailability was approximately 50% and was largely independent of dose."( Pharmacokinetics of alafosfalin, alone and in combination with cephalexin, in humans.
Allen, JG; Lees, LJ, 1980
)
0.5
" Both drugs were equally well absorbed from all of the tested formulations; identical percentages of the dose were recovered in the urine in all cases."( Pharmacokinetic comparison of cefroxadin (CGP 9000) and cephalexin by simultaneous administration to humans.
Hirtz, JL; Humbert, G; Lecaillon, JB; Schoeller, JP; Vischer, W, 1980
)
0.51
"In a previous study we have shown that cultured epithelial cell lines can be used to measure the transepithelial passage of antimicrobial agents across the intestine and to obtain information on the mechanisms of transport utilized and predict the bioavailability of the antimicrobial agents after oral administration."( D-cycloserine uses an active transport mechanism in the human intestinal cell line Caco 2.
Islam, K; Ranaldi, G; Sambuy, Y, 1994
)
0.29
" The overestimated plasma profile of propranolol suggests that the low bioavailability of propranolol is a result of first-pass metabolism by the intestine wall and the liver, because the calculated absolute absorption is almost perfect."( Prediction of the plasma concentration profiles of orally administered drugs in rats on the basis of gastrointestinal transit kinetics and absorbability.
Haruta, S; Higaki, K; Kimura, T; Kurosaki, Y; Sawamoto, T, 1997
)
0.3
" Three clinically evaluated orally absorbed carbacephems were taken up by Caco-2 cells, consistent with their excellent bioavailability in humans."( Structure-activity relationship of carbacephalosporins and cephalosporins: antibacterial activity and interaction with the intestinal proton-dependent dipeptide transport carrier of Caco-2 cells.
Berry, DM; Dantzig, AH; Duckworth, DC; Snyder, NJ; Spry, DO; Tabas, LB, 1997
)
0.3
"A new method has been developed for simultaneous evaluation of local absorption from the intestine into the portal system and local disposition through the liver, and for assessment of the bioavailability of a drug in a single conscious rat."( Short-period double-dosing for simultaneous evaluation of intestinal absorption and hepatic disposition in a single conscious rat using cephalexin as test drug.
Ito, T; Nakagawa, T; Yamaoka, K, 1997
)
0.5
" However, the extent of bioavailability was not changed in theophylline and cephalexin."( Absorption behavior of orally administered drugs in rats treated with propantheline.
Haruta, S; Higaki, K; Iwasaki, N; Kimura, T; Ogawara, K, 1998
)
0.53
" treatment, it can be envisaged to apply this effect to increase bioavailability of poorly absorbed peptidomimetic drugs in man."( Chronic nifedipine dosing enhances cephalexin bioavailability and intestinal absorption in conscious rats.
Berlioz, F; Carbon, C; Farinotti, R; Julien, S; Lepére-Prevot, B; Rozé, C; Tsocas, A, 2000
)
0.58
" Bioavailability (F), local absorption ratio (Fa), hepatic recovery ratio (FH), and local mean absorption time (ta) estimated by recirculatory analysis were close to those calculated by moment analysis with numerical integration."( Introduction of recirculatory analysis into portal and systemic concentration difference method.
Nakagawa, T; Sawai, Y; Ueda, S; Yamaoka, K, 2001
)
0.31
"Variability in valacyclovir bioavailability and the potential for cephalexin-valacyclovir interaction were evaluated."( Intra- and interindividual variabilities of valacyclovir oral bioavailability and effect of coadministration of an hPEPT1 inhibitor.
Anderle, P; Chin-Hong, P; Guglielmo, BJ; Lin, ET; Phan, DD; Sadee, W, 2003
)
0.56
"The utilization of the membrane transport protein PEPT1 as a drug delivery system is a promising strategy to enhance the oral bioavailability of drugs."( Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
Biegel, A; Brandsch, M; Gebauer, S; Hartrodt, B; Neubert, K; Thondorf, I, 2005
)
0.33
" Due to the poor oral bioavailability of many drugs in the horse, this method may be useful for screening drugs before development to determine if they warrant further study."( Mucosal permeability of water-soluble drugs in the equine jejunum: a preliminary investigation.
Blikslager, AT; Davis, JL; Little, D; Papich, MG, 2006
)
0.33
" because of its rapid intestinal metabolism, whereas d-CEX is well absorbed in the unchanged form."( Functional expression of stereoselective metabolism of cephalexin by exogenous transfection of oligopeptide transporter PEPT1.
Kato, Y; Kubo, Y; Mitsuoka, K; Tsuji, A, 2007
)
0.59
"The effect of colitis induced with dextran sodium sulfate (DSS) in rats on the bioavailability of drugs transported by the oligopeptide transporter PepT-1 was analyzed by studying the pharmacokinetics of PepT-1 substrates: cephalexin and valacyclovir, the prodrug of antiviral acyclovir."( Regulation of the oligopeptide transporter, PEPT-1, in DSS-induced rat colitis.
Bado, A; Beaufils, B; Buyse, M; Farinotti, R; Hindlet, P; Radeva, G; Walker, F, 2007
)
0.52
" These findings may have relevance in modulation of dietary nitrogen supply and PepT1 substrate bioavailability in obesity."( Long-term effect of leptin on H+-coupled peptide cotransporter 1 activity and expression in vivo: evidence in leptin-deficient mice.
Bado, A; Buyse, M; Farinotti, R; Hindlet, P, 2007
)
0.34
" 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
)
0.34
"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
)
0.36
"The pharmacokinetic profile and bioavailability of a long-acting formulation of cephalexin after intramuscular administration to cats was investigated."( Pharmacokinetics and bioavailability of a long-acting formulation of cephalexin after intramuscular administration to cats.
Albarellos, GA; Landoni, MF; Montoya, L; Quaine, PC, 2011
)
0.83
"5-fold higher than that in control rats, whereas the bioavailability of cephalexin remained unchanged."( Modulation in concentrative nucleoside transporters-mediated intestinal absorption of mizoribine, an immunosuppressive agent, in lipopolysaccharide-treated rats.
Ishiguro, M; Kamio, Y; Mori, N; Murakami, T; Shimomukai, Y; Yokooji, T, 2011
)
0.6
"In this study, the authors compared the effects of amlodipine (AML) on the bioavailability of cephalexin (LEX) and cefuroxime axetil (CXM)."( Effects of amlodipine on the oral bioavailability of cephalexin and cefuroxime axetil in healthy volunteers.
Ding, L; Ding, Y; Jia, Y; Jin, X; Liu, W; Lu, C; Song, Y; Wen, A; Yang, J; Yang, L; Zhu, Y, 2013
)
0.86
" Compared with conventional capsules, the gastro-floating tablets presented a sustained-release behavior with a relative bioavailability of 99."( Gastro-floating tablets of cephalexin: preparation and in vitro/in vivo evaluation.
Cao, H; Chen, K; He, W; Qin, C; Yin, L; Zhang, Q; Zhou, J; Zhu, C, 2013
)
0.69
"The objective of this study was to investigate the pharmacokinetics and to compare the bioavailability of three cephalexin products, Ospexin® versus MPI Cephalexin® tablet and MPI Cephalexin® capsule, in healthy Malay ethnic male volunteers in Malaysia."( Three-ways crossover bioequivalence study of cephalexin in healthy Malay volunteers.
Liew, KB; Loh, GO; Peh, KK; Tan, YT, 2014
)
0.87
" The findings of our study show that the improvement of cephalexin bioavailability and prolonged drug release profile could be obtained by niosomal formulation as a favorable antibiotic drug delivery system."( Preparation, physicochemical properties, in vitro evaluation and release behavior of cephalexin-loaded niosomes.
Akbarzadeh, I; Fatemizadeh, M; Ghafelehbashi, R; Heidarpoor Saremi, L; Lajevardi, A; Tavakkoli Yaraki, M, 2019
)
0.98
"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
)
0.51
" The pharmacokinetic behavior, results of bioequivalence studies published in the literature, as well as the therapeutic uses, potential toxicity and potential excipient effects on bioavailability were also assessed."( Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Cephalexin Monohydrate.
Abrahamsson, B; Cristofoletti, R; Dressman, J; Groot, DW; Langguth, P; Mehta, MU; Parr, A; Plöger, GF; Polli, JE; Quizon, PM; Shah, VP; Tajiri, T, 2020
)
0.79
"Higher levels of 5-HT in brain, plasma and small intestines were recognized in 5-HT-excessive rats, where the oral bioavailability of CEX was significantly enhanced."( Effect of Excessive Serotonin on Pharmacokinetics of Cephalexin after Oral Administration: Studies with Serotonin-Excessive Model Rats.
Higaki, K; Iwamoto, T; Maruyama, M; Nakashima, S; Ogawara, KI; Takanashi, M, 2022
)
0.97
"5-HT-excessive condition enhanced the oral bioavailability of CEX in rats, which would be attributed to the enhanced permeability across the intestinal mucosa via passive diffusion through the paracellular route even though the transport via PEPT1 was decreased."( Effect of Excessive Serotonin on Pharmacokinetics of Cephalexin after Oral Administration: Studies with Serotonin-Excessive Model Rats.
Higaki, K; Iwamoto, T; Maruyama, M; Nakashima, S; Ogawara, KI; Takanashi, M, 2022
)
0.97
" The oral bioavailability of CEX significantly decreased to 76% of that in control rats."( Irinotecan-induced gastrointestinal damage alters the expression of peptide transporter 1 and absorption of cephalexin in rats.
Akiyoshi, T; Hattori, T; Imaoka, A; Ohtani, H, 2023
)
1.12

Dosage Studied

The aim of the present work is to develop and validate a novel and simple Chromatographic and MCR methods for simultaneous quantification of cephalexin (CPH) and sodium benzoate (SDM) in their dosage form. Prospective, controlled data regarding optimal dosing of cephalothin in pediatric osteomyelitis are not available.

ExcerptRelevanceReference
" Cefaclor was administered orally in a dosage of 1 to 3 g per day for 7 to 11 days."( Cefaclor: clinical and bacteriological evaluation in 45 cases.
Clavel, A; Espinosa, C; Gómez-Agudo, G; Gómez-Lus, R; Guillen, G; Martinez-Piriz, R, 1979
)
0.26
" calcoaceticus in mice, minocycline was, in general, more active than gentamicin or polymyxin on a dosage basis and significantly more active on a blood-level basis."( In vitro and in vivo activities of minocycline and other antibiotics against Acinetobacter (Herellea-Mima).
Kuck, NA, 1976
)
0.26
" Although for each unit of creatinine clearance the poorly functioning kidney had a higher peak urinary drug concentration than the better functioning kidney, for each kidney the peak urinary drug concentration seemed to be directly proportional to the creatinine clearance, the drug dosage and the renal mechanisms of drug excretion."( Nitrofurantoin, sulfamethizole and cephalexin urinary concentration in unequally functioning pyelonephritic kidneys.
Bueschen, AJ; Schlegel, JU; Sullivan, JW, 1975
)
0.53
" The usual dosage was 100 mg/kg/day given orally in divided doses for 10 to 12 days."( Cephalexin monohydrate suspension. Treatment of otitis media.
Daly, JF; Jones, JE; McLinn, SE, 1975
)
1.7
" The dosage of cefaclor was 20 to 40 mg/kg/day in three or four divided doses for ten days."( Cefaclor in the treatment of susceptible infections in infants and children.
Spencer, MJ, 1979
)
0.26
" The significance of this dosage schedule advantage is discussed."( Clinical comparison of cefadroxil, new oral cephalosporin, and cephalexin in uncomplicated urinary tract infection.
Bolding, OT, 1978
)
0.5
" The dosage of cefaclor used was either 250 mg or 500 mg taken orally three times daily."( Treatment of acute bronchitis and pneumonia with cefaclor.
Laitinen, L; Mattson, K; Nikander-Hurme, R; Renkonen, OV, 1979
)
0.26
" There was no evidence of any haematological, renal or hepatic toxicity from either drug at the dosage used."( Comparison of cefaclor and amoxycillin in the treatment of urinary infections in a chronic disease hospital.
Lindan, R, 1979
)
0.26
" Total urinary recovery of antibiotic activity accounted for almost 90 percent of dosed cephradine and cephalexin compared to 55 percent of dosed cefaclor."( The pharmacokinetics of the oral cephalosporins cefaclor, cephradine and cephalexin.
Dean, S; Kendall, MJ; Selen, A; Welling, PG; Wise, R, 1979
)
0.71
" At this dosage peak concentrations of 13."( [Serum and tissue concentrations after a single dose of cefaclor].
Bethke, RO; Fabricius, K; Müller, O; Plaue, R, 1979
)
0.26
" The dosage consisted of 500 mg cefaclor three times daily, and the treatment lasted between 4 and 43 days (average 14 days)."( [Experience with cefaclor in the treatment of ear, nose and throat infections. Indications for cefaclor therapy (author's transl)].
Bach, R; Federspil, P; Schätzle, W; Tiesler, E; Weich, C; Wilhelm, HJ, 1979
)
0.26
" Only in one relatively severe case of erysipelas did the disease continue to spread despite the daily doses of 3 x 500 mg of oral cefaclor prescribed by the dosage regimen."( [Cefaclor in dermatological therapy (author's transl)].
Paul, E, 1979
)
0.26
" We present a dosage nomogram for calculating the appropriate adjustments to the loading dose based on patient weight and maintenence dose based on corrected creatinine clearance."( Pharmacokinetics of cefaclor and cephalexin: dosage nomograms for impaired renal function.
Bolton, WK; Sande, MA; Spyker, DA; Thomas, BL, 1978
)
0.54
" The influence of the thickness of the base layer and the form of the dose-response line were tested."( Microbiological diffusion assay II: design and applications.
Kavanagh, F, 1975
)
0.25
" Neither drug showed accumulation over the dosing period, and both were well tolerated."( Comparative pharmacology of cefaclor and cephalexin.
Korzeniowski, OM; Sande, MA; Scheld, WM, 1977
)
0.52
" Thirty pediatric patients with various types of infections such as tonsillitis, bronchitis, pneumonia, cystitis, pyelitis, lymphadenitis colli and pyodermia were treated with S-6437 at the daily dosage of 50 mg/kg orally, the clinical effectiveness was 89."( [Clinical and laboratory studies on S-6437 (a new longacting granule of cephalexin) in pediatric field (author's transl)].
Fukaya, K; Jose, H; Koide, T; Kondo, K; Kuno, K, 1977
)
0.49
" The result shows that cephalexin given twice a day in the dosage of 1 g has as good an effect in the treatment of urinary tract infections as when the dosage is given 4 times a day."( Treatment of chronic urinary tract infections with cephalexin (Ceporexine) orally administered at 12-hourly intervals.
Nilsson, LB, 1976
)
0.82
" Laboratory and clinical data are presented to question the validity of selected advertisements which (1) encourage the use of Keflex for severe respiratory infections in children, (2) recommend the use of Keflex for the treatment of bacterial bronchitis, (3) suggest that high tissue penetration is a unique property of Vibramycin, (4) present pooled susceptability data which do not reflect microbial resistance patterns in the patient's hospital, (5) recommend twice-daily administration of Ancef for urinary tract infections but do not clearly state the potential danger of this regimen for other infections, (6) suggest that gentamicin should be given to adults in only two dosage sizes for the treatment of serious Gram-negative infections, and (7) lead the reader to assume that only women need to be treated for Trichomonas infections."( Need for "counter-detailing" antibiotics.
Hendeles, L, 1976
)
0.26
" In a comparative evaluation of nine different cephalosporin antibiotics, not only the objective antibacterial and pharmacokinetic properties are taken into consideration, but also the dosage recommendations of the manufacturers as subjective factors."( [Cephalosporin antibiotics from microbiologic viewpoint. A comparison of antibacterial and pharmacokinetic properties].
Naumann, P, 1975
)
0.25
" The relative distribution volume of drugs during maturation and in pathological states varies greatly and thus makes conventional dosage in short-term therapy ineffective."( [Special pharmacokinetic aspects in newborns and young infants].
von Hattingberg, HM, 1975
)
0.25
" Initial loading doses, maintenance doses, and intervals adjusted to creatinine clearances were calculated from these data; accurate dosage schedules well adjusted to the renal status of each individual patient were derived from the calculated values."( Determination of cefalexin pharmacokinetics and dosage adjustments in relation to renal function.
Brogard, JM; Dorner, M; Lavillaureix, J; Pinget, M, 1975
)
0.25
" With the dosage regimen and duration of treatment used in this study cotrimoxazole appears to be superior to cephalexin in the management of acute urinary infections."( Comparative double-blind study of cephalexin and co-trimoxazole in urinary tract infections.
Gower, PE; Tasker, PR, 1976
)
0.75
" However, a range of dosage needs to be further explored for inducing neovascularity and neocellularity in the irradiated tissues."( The conservative management of osteoradionecrosis of the mandible with ultrasound therapy.
Harris, M, 1992
)
0.28
" A satisfactory intramuscular dosage regimen of cephalexin in cow calves would be 15 mg/kg administered at 9-h intervals."( Disposition kinetics and dosage of cephalexin in cow calves following intramuscular administration.
Chaudhary, RK; Garg, SK; Srivastava, AK, 1992
)
0.82
" Seventy-three children with impetigo were randomly assigned to receive penicillin V potassium or cephalexin monohydrate, both administered in dosages of 40 to 50 mg/kg per day, or erythromycin estolate administered in a dosage of 30 to 40 mg/kg per day."( Impetigo. Current etiology and comparison of penicillin, erythromycin, and cephalexin therapies.
Bass, JW; Browning, WC; Demidovich, CW; Ruff, ME; Wittler, RR, 1990
)
0.73
" If the therapeutic concept is maintained that levels of beta-lactam antibiotics in plasma should exceed the MIC for the offending organisms over a period that approximates the dosing interval, then cefprozil would appear to be suitable for twice-daily administration, whereas cefaclor should probably be administered three or even four times a day."( Phase I study of multiple-dose cefprozil and comparison with cefaclor.
Barbhaiya, RH; Gleason, CR; Martin, RR; Pittman, KA; Shukla, UA; Shyu, WC; Wilber, RB, 1990
)
0.28
"In two prospective, randomized multicenter double-blind studies with a dosage of either 250 mg given four times a day (study A) or 500 mg given two times a day (study B), the comparative efficacy and safety of cephalexin hydrochloride (LY061188; Keftab) and cephalexin monohydrate (Keflex) for treatment of skin and soft tissue infections were determined."( Comparative study of cephalexin hydrochloride and cephalexin monohydrate in the treatment of skin and soft tissue infections.
Bundy, JM; Drucker, WR; Finnerty, EF; Folan, DW; Hanna, CB; Jacobson, KD; Kreindler, TG; Kumar, A; Murray, DL; Waxman, K, 1988
)
0.78
" The results are discussed in relation to in vivo dosage regimens."( Kill kinetics of the cephalosporin antibiotics cephalexin and cefuroxime against bacteria of veterinary importance.
Brewster, G; Silley, P, 1988
)
0.53
" One hundred four children with pharyngitis and serologically confirmed Group A streptococci were randomly treated with cefaclor or penicillin using a mean dosage of 20 mg/kg/day for 10 days."( Comparison of oral cephalosporins with penicillin therapy for group A streptococcal pharyngitis.
Stillerman, M,
)
0.13
"S 6472 granule preparation, a sustained-release cefaclor, was orally administered to 20 acutely exacerbated cases of chronic bronchitis at a daily dosage of 750 mg (titer) in 2 divided doses for a duration of 7-15 days and its clinical usefulness was evaluated."( [Clinical evaluation of S 6472 granule preparation (sustained-release cefaclor) in chronic bronchitis].
Hiraga, Y; Omichi, M; Sasaoka, S, 1988
)
0.27
"The S 6472 granule preparation (sustained-release cefaclor preparation) was administered to 15 cases of chronic bronchitis for its clinical evaluation; a daily dosage of 750 mg was orally given in 2 divided doses after breakfast and dinner for a duration of 7 to 22 days."( [Clinical evaluation of S 6472 granule preparation (sustained-release cefaclor) in chronic bronchitis].
Nakamori, Y; Tanimoto, H, 1988
)
0.27
"S 6472 granule preparation, a sustained-release preparation of cefaclor, was administered to 21 patients with chronic respiratory airway infections for its clinical study; a daily dosage between 750 and 1,500 mg was orally given in 2 divided doses after breakfast and dinner for a duration of 3 to 14 days."( [Clinical study of S 6472 granule preparation (sustained-release cefaclor) in chronic respiratory airway infections].
Ishii, S; Matsunaga, K; Murohashi, K; Numata, H; Odagiri, S; Suzuki, K; Takahashi, K; Yamaki, I, 1988
)
0.27
" The dosage of cefaclor was 40 mg/kg/day administered orally in equally divided doses at 12-hour intervals."( Five vs. ten days of therapy for acute otitis media.
Hendrickse, WA; Kusmiesz, H; Nelson, JD; Shelton, S, 1988
)
0.27
" Provisional oral dosage regimens were computed for each cephalosporin on the basis of the MIC data and the kinetic parameters derived from intravenous and oral drug administration."( Clinical pharmacokinetics of five oral cephalosporins in calves.
Kurtz, B; Paz, R; Soback, S; Ziv, G, 1987
)
0.27
"The rate of cephalexin release from various dosage forms such as tablets, capsules and suspensions manufactured by several firms was studied."( [Biopharmaceutical aspects of the medicinal forms of cephalexin].
Berezovskaia, LN; Garsheva, GB; Grakovskaia, LK, 1987
)
0.9
" Individual dosage with control of serum levels is, therefore, recommended."( [Serum level of antibiotics in burn patients].
Csiba, A; Firr, M; Gráber, H; Novák, J; Syposs, T, 1986
)
0.27
" In the case of cefixime, single daily doses of 400 mg were taken; with cefaclor, the dosage was 250 mg three times daily."( Bowel flora changes in humans receiving cefixime (CL 284,635) or cefaclor.
Edelstein, MA; Finegold, SM; Gee, R; Ingram-Drake, L; MacDonald, K; Reinhardt, J; Wexler, H, 1987
)
0.27
" Since serum and tissue concentrations of Mb-12 after 200 mg administration in humans have been reported to be 1-2 micrograms/ml, it can be presumed that the causative bacteria would be eradicated by a usual dosage of MOM used in the present study."( [Midecamycin acetate-susceptibility of clinical isolates from dental and oral surgical infections].
Deguchi, K; Fukayama, S; Ikegami, R; Matsumoto, Y; Nishimura, Y; Oda, S; Sato, K; Tanaka, S; Yokota, N; Yoshihara, H, 1986
)
0.27
"The dose-response relationship between the frequencies or concentration of exposure to powdered drug allergens and drug induced allergic onsets was studied in a pharmaceutical plant for 15 years from 1974 to 1984."( [A study on dose-response relationship of occupational allergy in a pharmaceutical plant].
Chida, T, 1986
)
0.27
" The need for adjustment of drug dosage in patients with endstage renal disease and the need for supplemental dosages following haemodialysis are well recognised."( Drug therapy in patients undergoing peritoneal dialysis. Clinical pharmacokinetic considerations.
Cornish, WR; Hardy, BG; Manuel, MA; Paton, TW,
)
0.13
" As the volume of distribution and the clearance were not affected by cefaclor, it is concluded that both drugs can be given concomitantly without any dosage adjustment of theophylline."( Clinical pharmacokinetics of theophylline during co-treatment with cefaclor.
Hempenius, J; Holtkamp, A; Jonkman, JH; Schoenmaker, R; van der Boon, WJ, 1986
)
0.27
" It is concluded that both drugs can be given concomitantly without any dosage adjustment of theophylline."( No effect of cefaclor on theophylline pharmacokinetics.
Hempenius, J; Holtkamp, A; Jonkman, JH; Schoenmaker, R; van der Boon, WJ, 1985
)
0.27
" The important difference between cefadroxil and cefaclor is the remarkably longer half-life of cefadroxil, which makes once-a-day dosing possible and offers greater patient convenience and the likelihood of better compliance."( Comparative efficacy of cefadroxil and cefaclor in the treatment of skin and soft-tissue infections.
Ballantyne, FN, 1985
)
0.27
"We describe a new method of drug dosage adjustment."( A new dosing regimen in renal insufficiency: application to cephalexin.
Akagi, K; Hori, R; Kamiya, A; Nakano, H; Nihira, H; Okumura, K, 1985
)
0.51
" Although dosage modification of CCL is necessary in patients with renal dysfunction, multiple doses of 250 mg every 8 hours may be safe and effective even in patients with impaired renal function."( [Cefaclor dosage change with renal dysfunction].
Sekine, O; Usuda, Y, 1985
)
0.27
" Each drug was given in a daily dosage of approximately 40 mg/kg in three divided doses for ten days."( Comparative treatment trial of augmentin versus cefaclor for acute otitis media with effusion.
Kusmiesz, H; Nelson, JD; Odio, CM; Shelton, S, 1985
)
0.27
" On the basis of the above results, it was concluded that S6472 can provide sufficient clinical efficacy when it is administered at daily dosage of 750 mg or 1,500 mg in 2 divided doses after the breakfast and dinner."( [Clinical studies of S6472 in otorhinolaryngologic infections].
Baba, S; Furuta, S; Katsuta, K; Kinoshita, H; Mori, Y; Noboru, T; Ohno, I; Ohyama, M; Suzuki, K; Yamamoto, M, 1985
)
0.27
"The effectiveness of cephalexin, an oral cephalosporin using a dosage equivalent to available capsular dosage forms, was studied in relation to the effectiveness of phenoxymethyl penicillin and benzathine penicillin in the treatment of 128 patients with beta-hemolytic streptococcal pharyngitis, all but six of whom had group A streptococci isolated from throat cultures."( Use of available dosage forms of cephalexin in clinical comparison with phenoxymethyl penicillin and benzathine penicillin in the treatment of streptococcal pharyngitis in children.
Bacaner, H; Matsen, JM; Siegel, SE; Torstenson, O, 1974
)
0.85
" This work holds considerable promise for the study of dosage adjustments in patients with renal disease."( Quantitative investigation of renal handling of drugs in dogs with renal insufficiency.
Hori, R; Kamiya, A; Okumura, K, 1984
)
0.27
" Infants were randomly assigned to receive either oral amoxicillin or cefaclor in a dosage of 40 mg/kg/day divided into 3 doses for 10 days."( A controlled trial of cefaclor versus amoxicillin for treatment of acute otitis media in early infancy.
Berman, S; Lauer, BA,
)
0.13
" Cefaclor and amoxicillin were given three times daily before meals in a dosage of 500 and 750 mg respectively for seven days."( Cefaclor versus amoxicillin in the treatment of bacterial pneumonia: a comparative double-blind study.
Leuenberger, P; Vrantchev, S, 1983
)
0.27
" Amoxycillin and cefaclor were given three times daily in a dosage of 375 and 250 mg, respectively, for 7 days."( Influence of amoxycillin and cefaclor on the colonization resistance of oropharynx.
van Saene, HK; Willems, FT; Zweens, J, 1983
)
0.27
" In the CEX group, CEX was orally administered 4 times a day at a daily dosage of 1,000 mg for 3 to 5 days."( [A double-blind comparison between cefaclor and cephalexin in the treatment of dental infections].
Horii, M; Morinaga, T; Nishimura, T; Noshi, Y; Okada, T; Sasaki, T; Shimada, S; Takada, S; Takeuchi, T; Yamanaka, H, 1984
)
0.52
" Three dogs and four cats were similarly dosed using a liquid preparation of the same antibiotic."( Antibiotic concentration in the serum of dogs and cats following a single oral dose of cephalexin.
Burt, DG; Crosse, R, 1984
)
0.49
" These findings point out to the importance of proper formulation and protection of solid dosage forms handled in places where high temperature and humidity conditions are likely to exist."( Effect of storage on the bioavailability of cephalexin from its capsules.
Molokhia, AM, 1984
)
0.53
" In 10 patients (from all dosage groups) cefaclor was undetectable in the bronchial mucosa but in every case the serum concentration was low, suggesting incomplete absorption."( Penetration of cefaclor into bronchial mucosa.
Bradbury, R; Funnell, GR; Marlin, GE; Nicholls, AJ, 1984
)
0.27
" Clinical or animal studies are needed to establish whether the higher titers observed with patient serum containing highly protein-bound drugs diluted in low protein-content media would foster inadequate dosage regiments."( Laboratory evaluation of the serum dilution test in serious staphylococcal infection.
Bartlett, RC; Marcon, MJ, 1983
)
0.27
" Our results indicate that dosage adjustment based on creatinine clearance is not appropriate for patients receiving drugs requiring active tubular secretion for urinary excretion."( Ampicillin and cephalexin in renal insufficiency.
Hori, R; Kamiya, A; Nakano, H; Nihira, H; Okumura, K, 1983
)
0.62
" Twice-daily dosing with oral antibiotics is obviously convenient and may enhance compliance."( Treatment of staphylococcal skin infections: a comparison of cephalexin and dicloxacillin.
Dillon, HC, 1983
)
0.51
"The oral cephalosporin derivative Cefaclor was administered to 22 patients with respiratory tract infections at a daily dosage of 3 x 500 mg."( [Report of experiences with the oral cephalosporin-derivative cephaclor in respiratory tract infections].
Spath, P, 1983
)
0.27
" Cefaclor in a twice daily dosage schedule appears to be a safe and useful drug in the treatment of urinary tract infections caused by the common gram-negative organisms and it appears to be as efficacious as the trimethoprim-sulfamethoxazole combination."( A comparison of cefaclor versus trimethoprim-sulfamethoxazole combination in the treatment of acute urinary infections.
Rous, SN, 1981
)
0.26
"The chemistry, pharmacology, pharmacokinetics, bacterial spectrum, clinical use, dosage, adverse reactions, and dosage forms and cost of cefaclor are reviewed."( Evaluation of cefaclor.
Derry, JE, 1981
)
0.26
" Each patient received carbenicillin indanyl sodium (Geocillin) tablets, at a dosage of two 500 mg tablets (each tablet equivalent to 382 mg of carbenicillin) four times daily for either 14 days (acute patients) or 28 days (chronic patients)."( Bacterial prostatitis: treatment with carbenicillin indanyl sodium.
Mobley, DF, 1981
)
0.26
" Parenteral aminoglycoside antibiotics in usual dosage did not change the pharyngeal flora."( Changes in aerobic pharyngeal flora related to antibiotic use and the emergence of gram-negative bacilli.
Fujita, K; Maruyama, S; Oka, R; Yoshioka, H, 1982
)
0.26
" In patients on dialysis, dosage interval or quantity should be increased to compensate for doubled drug clearance dialysis."( Pharmacokinetics of cefaclor in renal failure: effects of multiple doses and hemodialysis.
Bolton, WK; Gober, LL; Sande, MA; Scheld, WM; Spyker, DA, 1982
)
0.26
" The total daily dosage was the same in each regimen."( Efficacy of two dosage schedules of cephalexin in dermatologic infections.
DiMattia, AF; Knapp, WH; Sexton, MJ; Smialowicz, CR, 1981
)
0.54
" Each drug was dosed at 50 mg/kg/day and was given every 12 hours in two equally divided doses."( Cefadroxil monohydrate versus erythromycin in paediatric patients.
Trujillo, H, 1981
)
0.26
"A multi-centre study in general practice was carried out to compare the efficacy of two doses of cephalexin-500 mg or 1 g - given in a twice daily dosage regimen to 752 patients with respiratory or soft tissue infections."( The efficacy of twice daily cephalexin.
Browning, AK, 1981
)
0.77
" Dosage regimens for cephalothin of 100 mg/kg 4 times a day and for cephalexin of 35 to 50 mg/kg 4 times a day would be expected to establish and maintain therapeutic plasma concentrations in large birds (pigeons, cranes, and emus)."( Pharmacokinetics of cephalothin and cephalexin in selected avian species.
Bush, M; Carpenter, JW; Locke, D; Neal, LA, 1981
)
0.77
" The possibility of different dosage requirements for male and female patients, based on the difference in the availability of lipid deposit sites, cannot be considered clinically significant at this time."( Tissue and fluid concentrations of cefadroxil monohydrate.
Bernhardt, LL, 1980
)
0.26
" The satisfactory intravenous dosage regimen of cephalexin for calves would be 11."( Pharmacokinetics of cephalexin in calves after intravenous and subcutaneous administration.
Chaudhary, RK; Garg, SK; Srivastava, AK, 1996
)
0.87
" Three patients were treated with intravenous acyclovir with concomitant reduction of steroid dosage and recovered completely."( Management of varicella infection during the course of inflammatory bowel disease.
Balasubramanian, S; Giannadaki, E; Greenstein, AJ; Manousos, ON; Mouzas, IA; Sachar, DB, 1997
)
0.3
" If varicella infection occurs, prompt diagnosis and treatment with acyclovir and concomitant reduction in immunosuppressive therapy (reduction in steroid dosage and discontinuation of azathioprine) should be initiated immediately to limit viremia and avoid fatal complications."( Management of varicella infection during the course of inflammatory bowel disease.
Balasubramanian, S; Giannadaki, E; Greenstein, AJ; Manousos, ON; Mouzas, IA; Sachar, DB, 1997
)
0.3
" The method is found to be reproducible and convenient for the quantitative analysis of cephalexin and cefaclor in its dosage forms."( HPTLC assay of cephalexin and cefaclor in pharmaceuticals.
Agbaba, D; Eric, S; Vladimirov, S; Zivanov Stakic, D,
)
0.71
" The results suggest that the proposed method may be used in place of HPLC for the routine quantitation of cephalexin in both pure and dosage forms."( Development of a densitometric method for the determination of cephalexin as an alternative to the standard HPLC procedure.
Baldi, A; Bambagiotti-Alberti, M; Coran, SA; Giannellini, V; Paoli, F; Picchioni, G, 1998
)
0.75
" The dosage was always 20 mg/kg of active ingredient."( Absorption kinetics and bioavailability of cephalexin in the dog after oral and intramuscular administration.
Anfossi, P; Carli, S; Castellani, G; Mengozzi, G; Montesissa, C; Villa, R, 1999
)
0.57
"Recirculatory analysis was introduced into the portal and systemic concentration difference method with double dosing (PS-DD method), which is an evaluation system for the local intestinal and hepatic first-pass effect."( Introduction of recirculatory analysis into portal and systemic concentration difference method.
Nakagawa, T; Sawai, Y; Ueda, S; Yamaoka, K, 2001
)
0.31
"Six beagle dogs were treated with cephalexin-monohydrate from 2 oral formulations (Rilexine tablets and Cefaseptin dragees, respectively) in a dosage of 25 mg/kg and plasma concentrations of cephalexin were measured over 8 hours."( [Pharmacokinetics of cephalexin from two oral formulations in dogs].
Ehinger, AM; Kietzmann, M,
)
0.73
" Cephalexin dosed twice daily or three times daily and cefadroxil dosed once daily appear equivalent in bacteriologic and clinical cure of GABHS tonsillopharyngitis."( Efficacy of cephalexin two vs. three times daily vs. cefadroxil once daily for streptococcal tonsillopharyngitis.
Casey, JR; Cleary, CT; Curtin, CD; Francis, AB; Hoeger, WJ; Marsocci, SM; Murphy, ML; Murray, PC; Pichichero, ME,
)
1.42
" Prophylactic oral antiviral agents are administered routinely to patients undergoing laser resurfacing to prevent postoperative HSV-1 eruptions; however, dosage and duration of treatment vary in the literature."( Herpes simplex virus prophylaxis with famciclovir in patients undergoing aesthetic facial CO2 laser resurfacing.
Bisaccia, E; Scarborough, D, 2003
)
0.32
" The proposed method is applied to the individual tablet dosage form and human serum."( Polarographic behavior of cephalexin and its determination in pharmaceuticals and human serum.
Ma, H; Song, J; Xu, M, 2004
)
0.62
" The percentage of time that serum concentrations remain above the MIC(90) during the dosing interval (T > MIC(90)) for Streptococcus pyogenes and Staphylococcus aureus associated with the pharmacokinetic profiles was calculated."( A randomized crossover study investigating the influence of ranitidine or omeprazole on the pharmacokinetics of cephalexin monohydrate.
Adejare, A; George, M; Madaras-Kelly, K; May, MP; Michas, P, 2004
)
0.53
"7% of the dosing interval for formulations A and B, respectively."( Pharmacokinetics of two once-daily parenteral cephalexin formulations in dogs.
Albarellos, G; Ambros, L; Hallu, R; Kreil, V; Montoya, L; Rebuelto, M; Waxman, S, 2005
)
0.59
" Urine samples were taken every 2 h during the whole dosing interval of the particular antibiotic."( Urinary bactericidal activity of oral antibiotics against common urinary tract pathogens in an ex vivo model.
Bedenic, B; Bubonja, M; Budimir, A; Topic, M, 2006
)
0.33
"5 microg/mL) was>70% of each of the 12 h dosing intervals (i."( Chronopharmacological study of cephalexin in dogs.
Ambros, L; Montoya, L; Prados, AP; Rebuelto, M, 2007
)
0.63
" Thus, route of administration may be an important issue to be considered when calculating dosage schedules for successful treatments and safe withdrawal times for veterinary medicines."( Comparative pharmacokinetics of an injectable cephalexin suspension in beef cattle.
Albarellos, G; Ambros, L; Hallu, R; Kreil, V; Montoya, L; Rebuelto, M; Waxman Dova, S, 2008
)
0.6
" The cytotoxicity studies on NCO-MPA show cell viability of ∼100% up to a dosage of 40 μg/mL on SiHa, MCF7, and B16F10 cell lines, and on mouse primary fibroblasts."( Characterization of biocompatible NiCo2O4 nanoparticles for applications in hyperthermia and drug delivery.
Dhole, SD; Jadhav, AD; Kale, SN; Kaul-Ghanekar, R; Koppikar, SJ; Ogale, SB; Verma, S, 2012
)
0.38
"To investigate the effect of zinc sulfate on pharmacokinetics of cephalexin when administered concurrently or at strategically spaced dosing times designed to avoid the potential interaction in healthy volunteers."( The effect of staggered administration of zinc sulfate on the pharmacokinetics of oral cephalexin.
Ding, LK; Ding, Y; Jia, YY; Li, F; Liu, WX; Lu, CT; Wen, AD; Yang, J; Yang, L; Zhu, YR, 2012
)
0.84
" The dosing recommendation is that zinc sulfate can be safely administered 3h after a cephalexin dose."( The effect of staggered administration of zinc sulfate on the pharmacokinetics of oral cephalexin.
Ding, LK; Ding, Y; Jia, YY; Li, F; Liu, WX; Lu, CT; Wen, AD; Yang, J; Yang, L; Zhu, YR, 2012
)
0.83
" Several product labels provided inadequate information on how to calculate therapeutic dosage and further stated withdrawal time despite lack of pharmacokinetic data on the antimicrobials in catfish."( Quality of Antimicrobial Products Used in Striped Catfish (Pangasianodon hypophthalmus) Aquaculture in Vietnam.
Dalsgaard, A; Phu, TM; Phuong, NT; Scippo, ML, 2015
)
0.42
"Identification of adequate antimicrobial dosing regimens for morbidly obese patients is essential given the simultaneous increase in morbid obesity and cellulitis prevalence in recent years."( Evaluation of cephalexin failure rates in morbidly obese patients with cellulitis.
Kashiwagi, DT; Kaufman, KR; Langworthy, DR; O'Meara, JG; Thurber, KM, 2016
)
0.79
" Until further study with a larger sample size is completed, empiric adjustment of cephalexin dosing based solely on BMI may not be necessary."( Evaluation of cephalexin failure rates in morbidly obese patients with cellulitis.
Kashiwagi, DT; Kaufman, KR; Langworthy, DR; O'Meara, JG; Thurber, KM, 2016
)
1.02
" It is, therefore, desirable to carry out a pre-formulation study to determine its pharmaceutical properties which will be useful in conversion of the new molecule into various dosage forms."( Pre-formulation Study of Salicylidine-cephalexin-Zn(II) dihydrate, a New Derivative of Cefalexin.
Iqbal, MS; Khan, AH, 2016
)
0.71
"Various pharmaceutical properties essentially required for formulation of salicylidine-cefalexin-Zn(II)·2H2O into dosage forms were determined."( Pre-formulation Study of Salicylidine-cephalexin-Zn(II) dihydrate, a New Derivative of Cefalexin.
Iqbal, MS; Khan, AH, 2016
)
0.71
"Current dosing recommendations for cephalosporin antibiotics are on the basis of pharmacokinetic studies and are frequently ignored in practice."( Clinical Outcomes of Failing to Dose-Reduce Cephalosporin Antibiotics in Older Adults with CKD.
Bathini, L; Battistella, M; Garg, AX; Jain, AK; Jandoc, R; Kuwornu, P; Liu, A; McArthur, E; Muanda, FT; Sood, MM; Weir, MA, 2019
)
0.51
"Literature data and results of experimental studies relevant to the decision to allow waiver of bioequivalence studies in humans for the approval of immediate release solid oral dosage forms containing cephalexin monohydrate are presented."( Biowaiver Monographs for Immediate Release Solid Oral Dosage Forms: Cephalexin Monohydrate.
Abrahamsson, B; Cristofoletti, R; Dressman, J; Groot, DW; Langguth, P; Mehta, MU; Parr, A; Plöger, GF; Polli, JE; Quizon, PM; Shah, VP; Tajiri, T, 2020
)
0.98
" Prospective, controlled data regarding optimal dosing of cephalexin in pediatric osteomyelitis are not available."( Frequency of Dosing of Cephalexin for Oral Step-Down Therapy of Pediatric Osteoarticular Infections Caused by Methicillin-Sensitive Staphylococcus Aureus.
Arnold, J; Bradley, JS; Cannavino, C; Ramchandar, N, 2020
)
1.11
" Although 4 times daily dosing is recommended, less frequent dosing regimens are often prescribed to improve treatment acceptability and adherence."( Twice- and Thrice-daily Cephalexin Dosing for Staphylococcus aureus Infections in Children.
Autmizguine, J; Curtis, N; Duffull, SB; Gwee, A, 2020
)
0.87
" Simulations were performed to determine a BID and TID dosing regimen so that ≥90% of children in this age group would achieve the pharmacodynamic target for MSSA (ie, time that the free drug concentration exceeds the minimum inhibitory concentration of the bacteria for at least 40% of the dosing interval)."( Twice- and Thrice-daily Cephalexin Dosing for Staphylococcus aureus Infections in Children.
Autmizguine, J; Curtis, N; Duffull, SB; Gwee, A, 2020
)
0.87
"Our study proposes a BID and TID cephalexin dosing regimen that can be prospectively evaluated."( Twice- and Thrice-daily Cephalexin Dosing for Staphylococcus aureus Infections in Children.
Autmizguine, J; Curtis, N; Duffull, SB; Gwee, A, 2020
)
1.15
"The aim of the present work is to develop and validate a novel and simple Chromatographic and MCR methods for simultaneous quantification of cephalexin (CPH) and sodium benzoate (SDM) in their dosage form and application of Lean Six Sigma (LSS) to reduce variation and improve quality."( Simultaneous Quantification of Cephalexin and Sodium Benzoate in their Dosage forms by high analytical technique. Application of Lean Six Sigma and In-Vitro Dissolution studies.
Mohamed, MA, 2021
)
1.11
"The proposed method is accurate and could be applied to dosage form and LSS to interpret the data of quality attributes."( Simultaneous Quantification of Cephalexin and Sodium Benzoate in their Dosage forms by high analytical technique. Application of Lean Six Sigma and In-Vitro Dissolution studies.
Mohamed, MA, 2021
)
0.91
"5 and 20 ppm); CZ-BNC-APP dosage (10, 55 and 100 mg/L); time (10, 55 and 100 min), temperature (20, 32."( Cephalexin removal by a novel Cu-Zn bionanocomposite biosynthesized in secondary metabolic products of Aspergillus arenarioides EAN603 with pumpkin peels medium: Optimization, kinetic and artificial neural network models.
Al-Gheethi, A; Algaifi, HA; Noman, E; Saphira Radin Mohamed, RM; Talip, B; Vo, DN, 2021
)
2.06
"5-HT-excessive rats were prepared by multiple intraperitoneal dosing of 5-HT and clorgyline, an inhibitor for 5-HT metabolism, and utilized to examine the pharmacokinetics, absorption behavior and the intestinal permeability for CEX."( Effect of Excessive Serotonin on Pharmacokinetics of Cephalexin after Oral Administration: Studies with Serotonin-Excessive Model Rats.
Higaki, K; Iwamoto, T; Maruyama, M; Nakashima, S; Ogawara, KI; Takanashi, M, 2022
)
0.97
"Selection of an antibiotic and dosing regimen requires consideration of multiple factors including microbiological data, site of infection, pharmacokinetics, and how it relates to the pharmacodynamic target."( Shedding Light on Amoxicillin, Amoxicillin-clavulanate, and Cephalexin Dosing in Children from a Pharmacist's Perspective.
Bio, LL; Yu, D, 2022
)
0.96
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Roles (1)

RoleDescription
antibacterial drugA drug used to treat or prevent bacterial infections.
[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 (4)

ClassDescription
cephalosporinA class of beta-lactam antibiotics differing from the penicillins in having a 6-membered, rather than a 5-membered, side ring. Although cephalosporins are among the most commonly used antibiotics in the treatment of routine infections, and their use is increasing over time, they can cause a range of hypersensitivity reactions, from mild, delayed-onset cutaneous reactions to life-threatening anaphylaxis in patients with immunoglobulin E (IgE)-mediated allergy.
semisynthetic derivativeAny organic molecular entity derived from a natural product by partial chemical synthesis.
beta-lactam antibiotic allergenAny beta-lactam antibiotic which causes the onset of an allergic reaction.
benzenetriolA triol in which three hydroxy groups are substituted onto a benzene ring.
[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 (1)

PathwayProteinsCompounds
2,4,6-trichlorophenol degradation413

Protein Targets (21)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Chain A, TYROSYL-DNA PHOSPHODIESTERASEHomo sapiens (human)Potency50.11870.004023.8416100.0000AID485290
Chain A, Putative fructose-1,6-bisphosphate aldolaseGiardia intestinalisPotency11.87650.140911.194039.8107AID2451
phosphopantetheinyl transferaseBacillus subtilisPotency42.23950.141337.9142100.0000AID1490
TDP1 proteinHomo sapiens (human)Potency29.85540.000811.382244.6684AID686979
Microtubule-associated protein tauHomo sapiens (human)Potency14.12540.180013.557439.8107AID1460
aldehyde dehydrogenase 1 family, member A1Homo sapiens (human)Potency31.62280.011212.4002100.0000AID1030
glucocorticoid receptor [Homo sapiens]Homo sapiens (human)Potency2.68320.000214.376460.0339AID720691
bromodomain adjacent to zinc finger domain 2BHomo sapiens (human)Potency89.12510.707936.904389.1251AID504333
euchromatic histone-lysine N-methyltransferase 2Homo sapiens (human)Potency3.98110.035520.977089.1251AID504332
15-hydroxyprostaglandin dehydrogenase [NAD(+)] isoform 1Homo sapiens (human)Potency35.48130.001815.663839.8107AID894
vitamin D3 receptor isoform VDRAHomo sapiens (human)Potency50.11870.354828.065989.1251AID504847
mitogen-activated protein kinase 1Homo sapiens (human)Potency7.94330.039816.784239.8107AID1454
nuclear factor erythroid 2-related factor 2 isoform 1Homo sapiens (human)Potency27.38930.000627.21521,122.0200AID743202; AID743219
Interferon betaHomo sapiens (human)Potency0.21010.00339.158239.8107AID1347407
[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)
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)IC50 (µMol)2,000.00000.50000.50000.5000AID681363
Solute carrier family 22 member 6Rattus norvegicus (Norway rat)Ki2,310.00001.60005.744010.0000AID678786
Solute carrier family 15 member 1Homo sapiens (human)IC50 (µMol)9,450.00000.18000.19000.2000AID679007; AID681608
Solute carrier family 15 member 1Homo sapiens (human)Ki14,200.00000.18003.39339.8000AID238858; AID681115
Solute carrier family 15 member 2Homo sapiens (human)Ki73.01930.79434.22108.0000AID612540; AID679325
Solute carrier family 15 member 2Rattus norvegicus (Norway rat)Ki62.00003.00006.47788.5000AID681114; AID681347
Solute carrier family 22 member 8Rattus norvegicus (Norway rat)IC50 (µMol)630.00006.03006.03006.0300AID681344
[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)
B2 metallo-beta-lactamase Chryseobacterium indologenesKm3.00003.00003.00003.0000AID562337
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (44)

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)
monoatomic ion transportSolute carrier family 15 member 1Homo sapiens (human)
protein transportSolute carrier family 15 member 1Homo sapiens (human)
peptide transportSolute carrier family 15 member 1Homo sapiens (human)
dipeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
tripeptide import across plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
proton transmembrane transportSolute carrier family 15 member 1Homo sapiens (human)
monoatomic ion transportSolute carrier family 15 member 2Homo sapiens (human)
protein transportSolute carrier family 15 member 2Homo sapiens (human)
peptide transportSolute carrier family 15 member 2Homo sapiens (human)
peptidoglycan transportSolute carrier family 15 member 2Homo sapiens (human)
xenobiotic transportSolute carrier family 15 member 2Homo sapiens (human)
dipeptide transportSolute carrier family 15 member 2Homo sapiens (human)
renal absorptionSolute carrier family 15 member 2Homo sapiens (human)
regulation of nucleotide-binding domain, leucine rich repeat containing receptor signaling pathwaySolute carrier family 15 member 2Homo sapiens (human)
dipeptide import across plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
tripeptide import across plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
antibacterial innate immune responseSolute carrier family 15 member 2Homo sapiens (human)
transport across blood-brain barrierSolute carrier family 15 member 2Homo sapiens (human)
proton transmembrane transportSolute carrier family 15 member 2Homo sapiens (human)
xenobiotic detoxification by transmembrane export across the plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

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)
proton-dependent oligopeptide secondary active transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
peptide:proton symporter activitySolute carrier family 15 member 1Homo sapiens (human)
tripeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
dipeptide transmembrane transporter activitySolute carrier family 15 member 1Homo sapiens (human)
protein bindingSolute carrier family 15 member 2Homo sapiens (human)
peptide:proton symporter activitySolute carrier family 15 member 2Homo sapiens (human)
tripeptide transmembrane transporter activitySolute carrier family 15 member 2Homo sapiens (human)
dipeptide transmembrane transporter activitySolute carrier family 15 member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (8)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
brush borderSolute carrier family 15 member 1Homo sapiens (human)
membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 1Homo sapiens (human)
phagocytic vesicle membraneSolute carrier family 15 member 2Homo sapiens (human)
plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
membraneSolute carrier family 15 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
extracellular exosomeSolute carrier family 15 member 2Homo sapiens (human)
apical plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
plasma membraneSolute carrier family 15 member 2Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (441)

Assay IDTitleYearJournalArticle
AID43600Hydrolysis rate by the beta-lactamase from Klebsiella sp. 363 relative to cephaloridine (100)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
1-Oxacephalosporins: enhancement of beta-lactam reactivity and antibacterial activity.
AID562337Activity at Chryseobacterium indologenes 597 metallo-beta-lactamase IND-6 expressed in Escherichia coli DH5alpha by Michaelis-Menten equation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
IND-6, a highly divergent IND-type metallo-beta-lactamase from Chryseobacterium indologenes strain 597 isolated in Burkina Faso.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID556831Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human keratinocytes assessed as bacterial count per mg of cell protein at high extracellular compound concentration after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID94130Minimum inhibitory concentration (MIC) against Klebsiella pneumoniae by 2-fold microdilution technique.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
AID680855TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 20 uM, Cephalexin: 10000 uM) in PEPT1-expressing HeLa cells1995The Journal of biological chemistry, Mar-24, Volume: 270, Issue:12
Human intestinal H+/peptide cotransporter. Cloning, functional expression, and chromosomal localization.
AID1134624Drug level in mouse blood at 50 mg/kg, sc after 1 hr by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
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.
AID420215Antimicrobial activity against Enterococcus faecalis UFPEDA 138 after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1625537Antimycobacterial activity against replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 3 days measured at OD580 = 0.01 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID83644The compound was tested for antibacterial activity against sensitive Haemophilus influenzae C.L.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
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.
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.
AID1146311Antibacterial activity against Serratia marcescens assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
AID524398Antibacterial activity against methicillin-susceptible beta-lactamase negative Staphylococcus aureus using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID556827Ratio of MIC for beta-lactamase-negative methicillin-susceptible Staphylococcus aureus ATCC 25923 by microdilution method at pH 7.4 to ratio of MIC for beta-lactamase-negative methicillin-susceptible Staphylococcus aureus ATCC 25923 by microdilution metho2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID1134623Drug level in mouse blood at 50 mg/kg, sc after 30 mins by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1625549Permeability of compound by PAMPA2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID562338Ratio of Kcat to Km for Chryseobacterium indologenes 597 metallo-beta-lactamase IND-6 expressed in Escherichia coli DH5alpha by Michaelis-Menten equation2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
IND-6, a highly divergent IND-type metallo-beta-lactamase from Chryseobacterium indologenes strain 597 isolated in Burkina Faso.
AID198183Minimum inhibitory concentration (MIC) against Streptococcus pneumoniae by 2-fold microdilution technique1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
AID1378013Antimycobacterial activity against Mycobacterium tuberculosis MC2 70002017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID1147072In vitro antibacterial activity against Salmonella schottmuelleri assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID363007Antibacterial activity against Salmonella Typhimurium at 500 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID420213Antimicrobial activity against Bacillus subtilis UFPEDA 16 after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID420222Antimicrobial activity against multidrug-resistant Staphylococcus aureus H.C. 20794 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1399258Antimicrobial activity against Streptococcus pneumoniae R6 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID681114TP_TRANSPORTER: inhibition of Gly-Sar uptake (pH6.0) in SKPT cells2005European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, Jan, Volume: 59, Issue:1
Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.
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.
AID205954Compound was tested in vitro for the antibacterial activity against Staphylococcus aureus (ATCC 6538P)1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Synthesis of delta 3-1-methylene-1-carbacephems.
AID1399266Antimicrobial activity against Proteus mirabilis ATCC 25933 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID70600In vitro antibacterial activity against Escherichia coli (ESS)1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Synthesis of delta 3-1-methylene-1-carbacephems.
AID43748Hydrolysis rate by the beta-lactamase from Proteus vulgaris 31 relative to cephaloridine (100)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
1-Oxacephalosporins: enhancement of beta-lactam reactivity and antibacterial activity.
AID519108Antibacterial activity against Proteus mirabilis M 44 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID681363TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells2002Life sciences, Mar-08, Volume: 70, Issue:16
Involvement of rat organic anion transporter 3 (rOAT3) in cephaloridine-induced nephrotoxicity: in comparison with rOAT1.
AID420223Antimicrobial activity against multidrug-resistant Staphylococcus aureus H.C. 20905 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1625540Stability in pH 5 non-replicating medium assessed as parent compound remaining at 5 to 50 ug/ml at 37 degC measured every 12 hrs up to 144 hrs by LC-MS analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID612540Binding affinity to human PepT2 in SKTP cells2011Bioorganic & medicinal chemistry, Aug-01, Volume: 19, Issue:15
Fragmental modeling of hPepT2 and analysis of its binding features by docking studies and pharmacophore mapping.
AID481444Octanol-water partition coefficient, log P of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID524399Antibacterial activity against methicillin-susceptible Bla-producing Staphylococcus aureus type A using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID524395Antibacterial activity against methicillin-susceptible beta-lactamase positive Staphylococcus aureus using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
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.
AID420225Antimicrobial activity against multidrug-resistant Enterococcus faecalis H.C. 21944 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID409954Inhibition of mouse 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.
AID1625573Bactericidal activity against wild-type non-replicating Mycobacterium tuberculosis H37Rv multi-stress model incubated for 7 days measured at OD580 = 0.01 by charcoal agar resazurin assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID519109Antibacterial activity against Proteus mirabilis M 48 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
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).
AID1134621Drug level in mouse blood at 50 mg/kg, sc after 10 mins by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID207035Antibacterial activity against penicillin G sensitive Staphylococcus aureus X1.11985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID519123Antibacterial activity against Proteus mirabilis M 35 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1147070In vitro antibacterial activity against Klebsiella pneumoniae assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID206177Tested for inhibition of visible growth of Staphylococcus aureus1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID524400Antibacterial activity against methicillin-susceptible Bla-producing Staphylococcus aureus type B using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID206042The compound was tested for antibacterial activity against Staphylococcus epidermidis EP11.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID519118Antibacterial activity against Proteus mirabilis M 31 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1916814Antibacterial activity against Pseudomonas aeruginosa NCIM 2036 assessed as bacterial growth inhibition incubated for 8 hrs by absorbance based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID1147071In vitro antibacterial activity against Proteus mirabilis assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID1625545Stability of compound in pH 2 solution assessed as parent compound remaining incubated for 4 hrs at 37 degC2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID74716In vitro antibacterial activity was determined by 2 fold serial agar dilution method with multilocular device in gram positive bacteria1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and antibacterial activities of new (alpha-hydrazinobenzyl)cephalosporins.
AID1219875Inhibition of recombinant human ABCC4 expressed in baculovirus infected insect Sf21 cell plasma membrane vesicles assessed as inhibition of transporter-mediated [3H]-estradiol-17beta-glucuronide uptake by liquid scintillation counting analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Oral availability of cefadroxil depends on ABCC3 and ABCC4.
AID208458Tested for inhibition of visible growth of Streptococcus pneumoniae1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID680868TP_TRANSPORTER: inhibition of Cefadroxil uptake (apical pH 5.5, Cefadroxil: 1000 uM, Cephalexin: 10000 uM) in Caco-2 cells1996The Journal of pharmacology and experimental therapeutics, May, Volume: 277, Issue:2
Transport characteristics of differently charged cephalosporin antibiotics in oocytes expressing the cloned intestinal peptide transporter PepT1 and in human intestinal Caco-2 cells.
AID524403Antibacterial activity against methicillin-susceptible Bla-producing Staphylococcus aureus type C using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID519252Antibacterial activity against Proteus mirabilis M 26 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID74719Inhibition of gram positive (resistant) bacteria growth.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and antimicrobial properties of substituted beta-aminoxypropionyl penicillins and cephalosporins.
AID1147084In vivo antibacterial activity against Escherichia coli infected in sc dosed albino CD-1 mouse assessed as protection against bacterial infection by measuring host survival administered at 1 hr and 4 hrs after infection1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID209893Antibacterial activity against Streptococcus pneumoniae Park.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1625558Stability in human plasma at 1 ug/ml measured up to 180 mins by LC-MS analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID524397Antibacterial activity against methicillin-susceptible beta-lactamase positive Staphylococcus aureus using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID206028Tested for antibacterial activity against methicillin resistant Staphylococcus aureus S13E.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID132258Efficacy against lethal mouse infected ip with park strain of Streptococcus pneumoniae administered po to 19-21-g random sex ICR mice at 1 hr and 5 hr1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID1916833Antibacterial activity against Bacillus subtilis NCIM 2079 assessed as reduction in bacterial growth incubated for 8 hrs by absorbance based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID208960Antibacterial activity in mice infected with Streptococcus pyogenes C203 after subcutaneous administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID113296Dose administered orally in mice infected with Streptococcus pyogenes.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID524404Antibacterial activity against methicillin-susceptible Bla-producing Staphylococcus aureus type A using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID25035Hydrolysis rate constant at pH 9.61984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Substituent effects on reactivity and spectral parameters of cephalosporins.
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).
AID1134637Antibacterial activity against Proteus mirabilis 13 infected in sc dosed mouse administered 1 hr post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1399253Antimicrobial activity against Bacillus anthracis Sterne 34F2 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID91481Binding constant against human serum albumin (HSA)2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
Cheminformatic models to predict binding affinities to human serum albumin.
AID679326TP_TRANSPORTER: uptake in Xenopus laevis oocytes1997The Journal of pharmacy and pharmacology, Aug, Volume: 49, Issue:8
The predominant contribution of oligopeptide transporter PepT1 to intestinal absorption of beta-lactam antibiotics in the rat small intestine.
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).
AID681344TP_TRANSPORTER: inhibition of Estrone sulfate uptake in OAT3-expressing S2 cells2002Life sciences, Mar-08, Volume: 70, Issue:16
Involvement of rat organic anion transporter 3 (rOAT3) in cephaloridine-induced nephrotoxicity: in comparison with rOAT1.
AID113298Dose administered subcutaneously in mice infected with Streptococcus pneumoniae1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID25034Hydrolysis rate constant at pH 101984Journal of medicinal chemistry, May, Volume: 27, Issue:5
Substituent effects on reactivity and spectral parameters of cephalosporins.
AID420229Antimicrobial activity against coagulase-negative Staphylococcus H.A.M. 338 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1146306Antibacterial activity against Shigella sp. assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
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.
AID1625546Stability of compound in pH 7 solution assessed as parent compound remaining incubated for 4 hrs at 37 degC2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID679325TP_TRANSPORTER: inhibition of Gly-Sar uptake in SKPT cells1995The Journal of biological chemistry, Oct-27, Volume: 270, Issue:43
Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2.
AID1149742Antibacterial activity against Proteus mirabilis assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID195438Affinity against Renal peptide transporter PepT2 in SKPT cells was measured by the inhibition of [14C]Gly-Sar uptake2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.
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.
AID481446Effective permeability across human jejunum2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID206156Tested for antibacterial activity against penicillin G resistant Staphylococcus aureus V41.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID198313Minimum inhibitory concentration (MIC) against Streptococcus pyogenes by 2-fold microdilution technique1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
AID1625548Solubility of compound in pH 7.4 solution measured after shaking for 4 hrs2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID524402Antibacterial activity against methicillin-susceptible Bla-producing Staphylococcus aureus type B using 5x10'7 CFU/ml high inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID420218Antimicrobial activity against multidrug-resistant Staphylococcus aureus H.C. 20981 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID556828Ratio of MIC for hospital-acquired methicillin-resistant Staphylococcus aureus ATCC 33591 by microdilution method at pH 7.4 to ratio of MIC for hospital-acquired methicillin-resistant Staphylococcus aureus ATCC 33591 by microdilution method at pH 5.52009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID781326pKa (acid-base dissociation constant) as determined by Avdeef ref: DOI: 10.1002/047145026X2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
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.
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).
AID1134614Drug level in mouse blood at 50 mg/kg, po after 15 mins by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID420227Antimicrobial activity against multidrug-resistant Enterococcus faecalis H.C. 24962 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1149736Antibacterial activity against Staphylococcus aureus Oxford assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID238858Binding affinity against membrane transport protein PEPT1 in human Caco-2 cells2005Journal of medicinal chemistry, Jun-30, Volume: 48, Issue:13
Three-dimensional quantitative structure-activity relationship analyses of beta-lactam antibiotics and tripeptides as substrates of the mammalian H+/peptide cotransporter PEPT1.
AID1399267Antimicrobial activity against Stenotrophomonas maltophilia ATCC 700475 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1146308Antibacterial activity against Klebsiella pneumoniae assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
AID209920The compound was tested for antibacterial activity against Streptococcus pyogenes C203.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1147069In vitro antibacterial activity against Escherichia coli assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID1774075Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli assessed as ANS saturation ratio at 400 uM incubated for 1 hr in presence of 7.5 uM ANS by fluorescence method (Rvb = 56 +/- 2.3%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID1209733Binding affinity to mouse OAT3 expressed in CHO cells at 10 to 1000 uM measured over 20 mins2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID70153Minimum inhibitory concentration against 30 strains of Escherichia coli1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Synthesis and beta-lactamase inhibitory properties of 2 beta-[(1,2,3-triazol-1-yl)methyl]-2 alpha-methylpenam-3 alpha-carboxylic acid 1,1-dioxide and related triazolyl derivatives.
AID70152Minimum inhibitory concentration against 30 strains of Escherichia coli1987Journal of medicinal chemistry, Aug, Volume: 30, Issue:8
Synthesis and beta-lactamase inhibitory properties of 2 beta-[(1,2,3-triazol-1-yl)methyl]-2 alpha-methylpenam-3 alpha-carboxylic acid 1,1-dioxide and related triazolyl derivatives.
AID69810Tested for inhibition of visible growth of Escherichia coli1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
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
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]
AID679007TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 25000 uM) in PEPT1-expressing CHO cells1996Pharmaceutical research, Nov, Volume: 13, Issue:11
Human dipeptide transporter, hPEPT1, stably transfected into Chinese hamster ovary cells.
AID1134638Antibacterial activity against Proteus mirabilis 13 infected in sc dosed mouse administered 1 hr and 5 hrs post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID556830Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human keratinocytes assessed as bacterial count per mg of cell protein at low extracellular compound concentration after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID362999Antibacterial activity against Staphylococcus aureus at 200 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
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]
AID1134619Drug level in mouse blood at 50 mg/kg, po after 2 hrs by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1134635Antibacterial activity against Escherichia coli 8 infected in sc dosed mouse administered 1 hr post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID207141Antibacterial activity in mice infected with Staphylococcus aureus 30551985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1134625Drug level in mouse blood at 50 mg/kg, sc after 2 hrs by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID1147081In vivo antibacterial activity against Streptococcus pasteurianus infected in sc dosed albino CD-1 mouse assessed as protection against bacterial infection by measuring host survival administered at 1 hr and 4 hrs after infection1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID420212Antimicrobial activity against Staphylococcus aureus UFPEDA 01 after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1134622Drug level in mouse blood at 50 mg/kg, sc after 20 mins by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID519124Antibacterial activity against Proteus mirabilis M 40 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1399255Antimicrobial activity against Enterococcus faecalis ATCC 33186 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID588214FDA HLAED, liver enzyme composite activity2004Current 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.
AID1134620Drug level in mouse blood at 50 mg/kg, po after 4 hrs by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1147065In vitro antibacterial activity against benzylpenicillin-resistant Staphylococcus aureus assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID198019Minimum inhibitory concentration (MIC) against Streptococcus faecalis by 2-fold microdilution technique.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
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.
AID1146309Antibacterial activity against Enterobacter aerogenes assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
AID64069Minimum inhibitory concentration (MIC) against Escherichia coli by 2-fold microdilution technique.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
AID679146TP_TRANSPORTER: uptake in Xenopus laevis oocytes2002Drug metabolism and pharmacokinetics, , Volume: 17, Issue:2
Rat renal organic anion transporter rOAT1 mediates transport of urinary-excreted cephalosporins, but not of biliary-excreted cefoperazone.
AID420226Antimicrobial activity against multidrug-resistant Enterococcus faecalis H.C. 24708 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1147083In vitro antibacterial activity against Streptococcus pneumoniae assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID1399261Antimicrobial activity against Enterobacter cloacae ATCC 13047 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID519119Antibacterial activity against Proteus mirabilis NP43 after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
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.
AID363008Antibacterial activity against Salmonella Typhimurium after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID70446Percentage zonal reduction was evaluated against Escherichia coli1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Dependence of beta-lactamase stability on substructures within beta-lactam antibiotics.
AID1625535Antimycobacterial activity against non-replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 3 days measured at OD580 = 0.01 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID206157Tested for antibacterial activity against penicillin G sensitive Staphylococcus aureus X1.11985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID1134626Drug level in mouse blood at 50 mg/kg, sc after 4 hrs by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID208729The compound was tested for antibacterial activity against Streptococcus group D X66.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID83645The compound was tested for antibacterial activity against sensitive Haemophilus influenzae C.L.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID74715In vitro antibacterial activity was determined by 2 fold serial agar dilution method in gram positive resistant bacteria1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and antibacterial activities of new (alpha-hydrazinobenzyl)cephalosporins.
AID209921The compound was tested for antibacterial activity against Streptococcus pyogenes C203.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID1378014Antimycobacterial activity against Mycobacterium tuberculosis MC2 62302017European journal of medicinal chemistry, Sep-29, Volume: 138Triazole derivatives and their anti-tubercular activity.
AID85958Antibacterial activity against sensitive Haemophilus influenzae C.L.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID363003Antibacterial activity against Salmonella Typhimurium at 1 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID588971Substrates of transporters of clinical importance in the absorption and disposition of drugs, PEPT22010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID133286Minimum inhibitory concentration against mouse infected with C203 strain of Streptococcus pyogenes1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID200262Minimum inhibitory concentration (MIC) against Staphylococcus aureus by 2-fold microdilution technique.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
AID151367Minimum inhibitory concentration (MIC) against Proteus mirabilis by 2-fold microdilution technique.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
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).
AID1134613Antibacterial activity against Proteus mirabilis after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1399260Antimicrobial activity against Acinetobacter baumannii ATCC 19606 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1399256Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 29213 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1134639Antibacterial activity against Staphylococcus aureus Smith infected in po dosed mouse administered 1 hr post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1399252Antimicrobial activity against Bacillus subtilis ATCC 23857 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID556832Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human keratinocytes assessed as change in bacterial count after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
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.
AID1916813Antibacterial activity against Escherichia coli NCIM 2688 assessed as bacterial growth inhibition incubated for 8 hrs by absorbance based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID481439Absolute bioavailability in human2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID524401Antibacterial activity against methicillin-susceptible Bla-producing Staphylococcus aureus type C using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID420224Antimicrobial activity against multidrug-resistant Enterococcus faecalis H.C. 21752 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1134617Drug level in mouse blood at 50 mg/kg, po after 30 mins by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID67862Tested for inhibition of visible growth of Enterobacter aerogenes1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID1625544Antimycobacterial activity against replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID556834Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human keratinocytes assessed as bacterial count per mg of cell protein at low extracellular compound concentration after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID1774078Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 4 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID209260Tested for inhibition of visible growth of Streptococcus faecalis1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID1146310Antibacterial activity against Salmonella heidelberg assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
AID556829Ratio of MIC for hospital-acquired methicillin-resistant Staphylococcus aureus ATCC 33591 by microdilution method at pH 5.5 to MIC for beta-lactamase-negative methicillin-susceptible Staphylococcus aureus ATCC 25923 by microdilution method at pH 5.52009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID1134611Antibacterial activity against Shigella sonnei after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID209781Tested for inhibition of visible growth of Streptococcus pyogenes1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID681608TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 20 uM) in PEPT1-expressing CHO cells1999Journal of pharmaceutical sciences, Mar, Volume: 88, Issue:3
CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs.
AID113295Dose administered orally in mice infected with Streptococcus pneumoniae1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
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.
AID1219873Inhibition of recombinant human ABCC2 expressed in insect Sf21 cell plasma membrane vesicles assessed as inhibition of transporter-mediated [3H]-estradiol-17beta-glucuronide uptake by liquid scintillation counting analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Oral availability of cefadroxil depends on ABCC3 and ABCC4.
AID519107Antibacterial activity against Proteus mirabilis B2 after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID20050Human absorption A (%)1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
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]
AID575340Antimicrobial activity against Listeria monocytogenes EGD-e at 30 ug after 16 hrs by disk diffusion assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
The ABC transporter AnrAB contributes to the innate resistance of Listeria monocytogenes to nisin, bacitracin, and various beta-lactam antibiotics.
AID1134390Drug recovery in ICR mouse feces at 1.6 mg/ml, po after 24 hrs1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cephalosporin degradations.
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.
AID680655TP_TRANSPORTER: uptake in PEPT1-expressing HeLa cells1995The Journal of biological chemistry, Oct-27, Volume: 270, Issue:43
Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2.
AID524396Antibacterial activity against methicillin-susceptible beta-lactamase negative Staphylococcus aureus using 5x10'5 CFU/ml standard inoculum after 24 hrs by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Determination of an inoculum effect with various cephalosporins among clinical isolates of methicillin-susceptible Staphylococcus aureus.
AID1219874Inhibition of recombinant human ABCC3 expressed in baculovirus infected insect Sf21 cell plasma membrane vesicles assessed as inhibition of transporter-mediated [3H]-estradiol-17beta-glucuronide uptake by liquid scintillation counting analysis2012Drug metabolism and disposition: the biological fate of chemicals, Mar, Volume: 40, Issue:3
Oral availability of cefadroxil depends on ABCC3 and ABCC4.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID1625543Antimycobacterial activity against non-replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 7 days measured at OD580 = 0.01 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID679005TP_TRANSPORTER: uptake in PEPT1-expressing CHO cells1999Journal of pharmaceutical sciences, Mar, Volume: 88, Issue:3
CHO/hPEPT1 cells overexpressing the human peptide transporter (hPEPT1) as an alternative in vitro model for peptidomimetic drugs.
AID420214Antimicrobial activity against Micrococcus luteus UFPEDA 06 after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID362997Antibacterial activity against Staphylococcus aureus at 10 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID1625542Antimycobacterial activity against non-replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 7 days measured at OD580 = 0.1 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID1399257Antimicrobial activity against methicillin-resistant Staphylococcus aureus NRS70 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID363002Antibacterial activity against Salmonella Typhimurium at 0.1 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID678850TP_TRANSPORTER: uptake in SKPT cells1995The Journal of biological chemistry, Oct-27, Volume: 270, Issue:43
Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2.
AID207033Antibacterial activity against penicillin G resistant Staphylococcus aureus V41.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1134641Antibacterial activity against Escherichia coli 8 infected in po dosed mouse administered 1 hr post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID522388Activity of Aeromonas enteropelogenes Beta-lactamase TRU12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic and biochemical characterization of TRU-1, the endogenous class C beta-lactamase from Aeromonas enteropelogenes.
AID207020Antibacterial activity against methicillin resistant Staphylococcus aureus S13E.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1147064In vitro antibacterial activity against Staphylococcus aureus assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID68043In vitro minimum inhibitory concentration against Enterococcus faecalis (STCO-19)1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 1. The "B" group.
AID522392Ratio of Kcat Km for Aeromonas enteropelogenes Beta-lactamase TRU12010Antimicrobial agents and chemotherapy, Apr, Volume: 54, Issue:4
Genetic and biochemical characterization of TRU-1, the endogenous class C beta-lactamase from Aeromonas enteropelogenes.
AID1916811Antibacterial activity against Staphylococcus aureus NCIM 2010 assessed as bacterial growth inhibition incubated for 8 hrs by absorbance based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID1149740Antibacterial activity against Shigella sonnei assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID43595Hydrolysis rate by the beta-lactamase from Escherichia coli 6 relative to cephaloridine.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
1-Oxacephalosporins: enhancement of beta-lactam reactivity and antibacterial activity.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID519120Antibacterial activity against Proteus mirabilis M 12 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1147068In vitro antibacterial activity against Streptococcus pyogenes assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID1399265Antimicrobial activity against Pseudomonas aeruginosa PAO1 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1146307Antibacterial activity against Escherichia coli assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
AID208928Antibacterial activity in mice infected with Streptococcus pneumoniae Park1 by oral administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID420228Antimicrobial activity against coagulase-negative Staphylococcus H.A.M. 278 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID519106Antibacterial activity against Escherichia coli 10418 after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID519115Antibacterial activity against Proteus mirabilis NP37 after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1211802Drug excretion in iv dosed rat assessed as compound excreted into bile2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Species differences in biliary clearance and possible relevance of hepatic uptake and efflux transporters involvement.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID519110Antibacterial activity against Proteus mirabilis M 55 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
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]
AID519111Antibacterial activity against Proteus mirabilis NP14 after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID682280TP_TRANSPORTER: inhibition of Carnitine uptake (Carnitine: 0.02 uM, Cephalexin: 2500 uM) in OCTN2-expressing HeLa cells2000The Journal of biological chemistry, Jan-21, Volume: 275, Issue:3
beta-lactam antibiotics as substrates for OCTN2, an organic cation/carnitine transporter.
AID1147067In vitro antibacterial activity against Streptococcus pasteurianus assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
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).
AID1399259Antimicrobial activity against Streptococcus pyogenes ATCC 700294 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID556837Bacteriostatic activity against methicillin-resistant Staphylococcus aureus ATCC 33591 infected in human keratinocytes assessed as change in bacterial count after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
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).
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID43420Hydrolysis rate by the beta-lactamase from Enterobacter cloacae 53 relative to cephaloridine.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
1-Oxacephalosporins: enhancement of beta-lactam reactivity and antibacterial activity.
AID207022Antibacterial activity against methicillin resistant Staphylococcus aureus X4001985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID681115TP_TRANSPORTER: inhibition of Gly-Sar uptake (pH6.0) in Caco-2 cells2005European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V, Jan, Volume: 59, Issue:1
Interaction of 31 beta-lactam antibiotics with the H+/peptide symporter PEPT2: analysis of affinity constants and comparison with PEPT1.
AID363000Antibacterial activity against Staphylococcus aureus at 500 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID207036Antibacterial activity against penicillin G sensitive Staphylococcus aureus X1.1.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID113297Dose administered subcutaneously in mice infected with Staphylococcus aureus.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID519112Antibacterial activity against Proteus mirabilis M 19 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID681350TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT1-expressing LLC-PK1 cells1997The American journal of physiology, 11, Volume: 273, Issue:5
Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells.
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.
AID592681Apparent permeability across human Caco2 cell membrane after 2 hrs by LC-MS/MS analysis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
QSAR-based permeability model for drug-like compounds.
AID362995Antibacterial activity against Staphylococcus aureus at 0.1 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
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).
AID679558TP_TRANSPORTER: inhibition of Gly-Sar uptake (Gly-Sar: 30 uM, Cephalexin: 10000 uM) in PEPT2-expressing HeLa cells1995Biochimica et biophysica acta, May-04, Volume: 1235, Issue:2
Molecular cloning of PEPT 2, a new member of the H+/peptide cotransporter family, from human kidney.
AID481440Dissociation constant, pKa of the compound2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID519122Antibacterial activity against Proteus mirabilis NP55 after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1134607Antibacterial activity against Staphylococcus aureus Oxford after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
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).
AID206212Antibacterial activity against Staph. epidermis EP111985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1916812Antibacterial activity against Bacillus subtilis NCIM 2079 assessed as bacterial growth inhibition incubated for 8 hrs by absorbance based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID132254Efficacy against lethal mouse infected ip with 3055 strain of Staphylococcus aureus, administered po to 19-21-g random sex ICR mice at 1 hr and 5 hr1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID1134636Antibacterial activity against Escherichia coli 8 infected in sc dosed mouse administered 1 hr and 5 hrs post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID207023Antibacterial activity against methicillin resistant Staphylococcus aureus X400.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID132255Efficacy against lethal mouse infected ip with 3055 strain of Staphylococcus aureus, administered sc to 19-21-g random sex ICR mice at 1 hr and 5 hr1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID206416Antibacterial activity in mice infected with Staphylococcus aureus 3055 by oral administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1625539Stability in pH 7.4 phosphate buffer solution assessed as parent compound remaining at 5 to 50 ug/ml at 37 degC measured every 12 hrs up to 144 hrs by LC-MS analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID362998Antibacterial activity against Staphylococcus aureus at 100 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID1147080In vivo antibacterial activity against Streptococcus pyogenes infected in sc dosed albino CD-1 mouse assessed as protection against bacterial infection by measuring host survival administered at 1 hr and 4 hrs after infection1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID476929Human intestinal absorption in po dosed human2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Neural computational prediction of oral drug absorption based on CODES 2D descriptors.
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]
AID1134387Drug recovery in Purdue-Wistar rat urine at 1.6 mg/ml, po after 24 hrs by liquid scintillation counting analysis1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cephalosporin degradations.
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).
AID1916832Antibacterial activity against Staphylococcus aureus NCIM 2010 assessed as reduction in bacterial growth incubated for 8 hrs by absorbance based assay2022European journal of medicinal chemistry, Aug-05, Volume: 238Recent contribution of medicinally active 2-aminothiophenes: A privileged scaffold for drug discovery.
AID420221Antimicrobial activity against multidrug-resistant Staphylococcus aureus H.C. 20489 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID208728The compound was tested for antibacterial activity against Streptococcus group D X66.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID680828TP_TRANSPORTER: inhibition of VACV uptake (VACV: 20 uM, Cephalexin: 10000 uM) in PEPT1-expressing CHO cells1999The Journal of pharmacology and experimental therapeutics, Apr, Volume: 289, Issue:1
Interactions of a nonpeptidic drug, valacyclovir, with the human intestinal peptide transporter (hPEPT1) expressed in a mammalian cell line.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID420217Antimicrobial activity against Candida albicans UFPEDA 1007 after 48 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID363006Antibacterial activity against Salmonella Typhimurium at 200 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID1149741Antibacterial activity against Klebsiella aerogenes assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID19419Partition coefficient (logD7.4)1998Journal of medicinal chemistry, Mar-26, Volume: 41, Issue:7
Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes.
AID481442Transcellular permeability at pH 6.5 calculated from in vitro P app values in Caco-2 and/or MDCK cells2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
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).
AID575417Antimicrobial activity against anrB-deficient Listeria monocytogenes EGD-e at 30 ug after 16 hrs by disk diffusion assay2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
The ABC transporter AnrAB contributes to the innate resistance of Listeria monocytogenes to nisin, bacitracin, and various beta-lactam antibiotics.
AID79398Minimum inhibitory concentration (MIC) against Haemophilus influenzae by 2-fold microdilution technique.1988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
An examination of O-2-isocephems as orally absorbable antibiotics.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID83642The compound was tested for antibacterial activity against resistant Haemophilus influenzae 76.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
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.
AID588970Substrates of transporters of clinical importance in the absorption and disposition of drugs, PEPT12010Nature reviews. Drug discovery, Mar, Volume: 9, Issue:3
Membrane transporters in drug development.
AID162890Tested for inhibition of visible growth of Proteus mirabilis1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID1134618Drug level in mouse blood at 50 mg/kg, po after 1 hr by microbiological assay1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
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.
AID40775In vitro antibacterial activity against B. subtilis( NCTC 8236)1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Synthesis of delta 3-1-methylene-1-carbacephems.
AID85957Antibacterial activity against resistant Haemophilus influenzae 76.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID362996Antibacterial activity against Staphylococcus aureus at 1 ug/ml after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
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.
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.
AID1146302Antibacterial activity against penicillin-resistant, coagulase-positive Staphylococcus aureus assessed as growth inhibition by gradient-plate assay1977Journal of medicinal chemistry, Sep, Volume: 20, Issue:9
Orally active esters of cephalosporin antibiotics. Synthesis and biological properties of acyloxymethyl esters of 7-(D-2-amino-2-phenylacetamido)-3-[5-methyl-(1,3,4-thiadiazol-2-yl)thiomethyl]-3-cephem-4-carboxylic acid.
AID207034Antibacterial activity against penicillin G sensitive Staphylococcus aureus V411985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID195437Concentration required to inhibit the maximum [14C]Gly-Sar uptake by Renal peptide transporter PepT2 in SKPT cells2004Journal of medicinal chemistry, Feb-12, Volume: 47, Issue:4
Phe-Gly dipeptidomimetics designed for the di-/tripeptide transporters PEPT1 and PEPT2: synthesis and biological investigations.
AID207021Antibacterial activity against methicillin resistant Staphylococcus aureus S13E.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
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).
AID133288Minimum inhibitory concentration against mouse infected with park strain of Streptococcus pneumoniae1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
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).
AID206155Tested for antibacterial activity against methicillin resistant Staphylococcus aureus X400.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID207263In vitro minimum inhibitory concentration against Staphylococcus aureus (SFCO-1a)1989Journal of medicinal chemistry, Aug, Volume: 32, Issue:8
Antibacterials. Synthesis and structure-activity studies of 3-aryl-2-oxooxazolidines. 1. The "B" group.
AID1625557Stability in CD-1 mouse plasma at 1 ug/ml measured up to 180 mins by LC-MS analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID481441Aqueous diffusivity at 37C2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
How well can the Caco-2/Madin-Darby canine kidney models predict effective human jejunal permeability?
AID1774076Inhibition of 8-anilinonaphthalene-l-sulfonic acid binding to TTR V3OM mutant (unknown origin) expressed in Escherichia coli at 400 uM incubated for 1 hr in presence of 75 uM ANS by fluorescence method (Rvb = 91 +/- 0.92%)2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID208929Antibacterial activity in mice infected with Streptococcus pneumoniae Park1 by subcutaneous administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID43599Hydrolysis rate by the beta-lactamase from Escherichia coli W3110 RTEM relative to cephaloridine.1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
1-Oxacephalosporins: enhancement of beta-lactam reactivity and antibacterial activity.
AID113294Dose administered orally in mice infected with Staphylococcus aureus.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1625532Antimycobacterial activity against non-replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 3 days measured at OD580 = 0.1 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID74700Inhibition of gram negative bacteria growth.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and antimicrobial properties of substituted beta-aminoxypropionyl penicillins and cephalosporins.
AID1625534Antimycobacterial activity against non-replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 6 days measured at OD580 = 0.1 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
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.
AID1134640Antibacterial activity against Staphylococcus aureus Smith infected in po dosed mouse administered 1 hr and 5 hrs post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID519125Antibacterial activity against Proteus mirabilis M 42 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID113299Dose administered subcutaneously in mice infected with Streptococcus pyogenes1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID68542Tested for inhibition of visible growth of Enterobacter cloacae1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID420216Antimicrobial activity against Mycobacterium smegmatis UFPEDA 71 after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1211878Unbound biliary clearance in iv dosed rat2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Species differences in biliary clearance and possible relevance of hepatic uptake and efflux transporters involvement.
AID1134610Antibacterial activity against Salmonella typhi after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID420220Antimicrobial activity against multidrug-resistant Staphylococcus aureus H.C. 21036 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1399263Antimicrobial activity against tolC deficient Escherichia coli JW5503-1 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1625550Stability in mouse liver microsomes assessed as compound metabolism up to 60 mins2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID83643The compound was tested for antibacterial activity against resistant Haemophilus influenzae 76.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
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.
AID519121Antibacterial activity against Proteus mirabilis M 17 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID1134388Drug recovery in Purdue-Wistar rat feces at 1.6 mg/ml, po after 24 hrs1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cephalosporin degradations.
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).
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.
AID1209736Inhibition of human OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID43598Hydrolysis rate by the beta-lactamase from Enterobacter cloacae 214 relative to cephaloridine (100)1981Journal of medicinal chemistry, Jan, Volume: 24, Issue:1
1-Oxacephalosporins: enhancement of beta-lactam reactivity and antibacterial activity.
AID200526Tested for inhibition of visible growth of Salmonella schottmuelleri1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID519117Antibacterial activity against Proteus mirabilis M 29 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID681347TP_TRANSPORTER: inhibition of Gly-Sar uptake in PEPT2-expressing LLC-PK1 cells1997The American journal of physiology, 11, Volume: 273, Issue:5
Recognition of beta-lactam antibiotics by rat peptide transporters, PEPT1 and PEPT2, in LLC-PK1 cells.
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.
AID432063Apparent permeability at pH 7.4 after 24 hrs by PAMPA method2009European journal of medicinal chemistry, Sep, Volume: 44, Issue:9
Determination of permeability and lipophilicity of pyrazolo-pyrimidine tyrosine kinase inhibitors and correlation with biological data.
AID132256Efficacy against lethal mouse infected ip with C203 strain of Streptococcus pyogenes, administered po to 19-21-g random sex ICR mice at 1 hr and 5 hr1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID420219Antimicrobial activity against multidrug-resistant Staphylococcus aureus H.C. 21141 isolate after 20 hrs by twofold serial dilution technique2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
Synthesis, antimicrobial and cytotoxic activities of some 5-arylidene-4-thioxo-thiazolidine-2-ones.
AID1399254Antimicrobial activity against Bacillus cereus ATCC 14579 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1147082In vivo antibacterial activity against Salmonella schottmuelleri infected in sc dosed albino CD-1 mouse assessed as protection against bacterial infection by measuring host survival administered at 1 hr and 4 hrs after infection1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID556833Bacteriostatic activity against methicillin-susceptible Staphylococcus aureus ATCC 25923 infected in human keratinocytes assessed as change in bacterial count after 24 hrs2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Activities of ceftobiprole and other cephalosporins against extracellular and intracellular (THP-1 macrophages and keratinocytes) forms of methicillin-susceptible and methicillin-resistant Staphylococcus aureus.
AID209127Antibacterial activity against Streptococcus pyogenes C203.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1399264Antimicrobial activity against Klebsiella pneumoniae ATCC 33495 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1149739Antibacterial activity against Salmonella typhi assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID208471The compound was tested for antibacterial activity against Streptococcus pneumoniae Park.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID207137In vitro antibacterial activity against Sarcina lutea (ATCC 9341)1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Synthesis of delta 3-1-methylene-1-carbacephems.
AID21261Tested for the peak time in mice following 43 mg/kg oral dose of cephalosporin1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID1149738Antibacterial activity against Escherichia coli assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID1209735Inhibition of mouse OAT3 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
AID1134389Drug recovery in ICR mouse urine at 1.6 mg/ml, po after 24 hrs by liquid scintillation counting analysis1977Journal of medicinal chemistry, Jul, Volume: 20, Issue:7
Cephalosporin degradations.
AID74702In vitro antibacterial activity was determined by 2 fold serial agar dilution method in gram negative resistant bacteria1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and antibacterial activities of new (alpha-hydrazinobenzyl)cephalosporins.
AID1625541Stability in pH 5 non-replicating medium containing 0.5 mM NaNO2 assessed as parent compound remaining at 5 to 50 ug/ml at 37 degC measured every 12 hrs up to 144 hrs by LC-MS analysis2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID74703In vitro antibacterial activity was determined by 2 fold serial agar dilution method with multilocular device in gram negative bacteria1983Journal of medicinal chemistry, Nov, Volume: 26, Issue:11
Synthesis and antibacterial activities of new (alpha-hydrazinobenzyl)cephalosporins.
AID1399262Antimicrobial activity against Escherichia coli BW25113 after 18 to 20 hrs by microbroth dilution method2018Bioorganic & medicinal chemistry letters, 10-01, Volume: 28, Issue:18
New β-lactam - Tetramic acid hybrids show promising antibacterial activities.
AID1625538Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 2 days by Celltiter-Glo reagent based assay2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
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.
AID1211870Total biliary clearance in iv dosed rat2013Drug metabolism and disposition: the biological fate of chemicals, Feb, Volume: 41, Issue:2
Species differences in biliary clearance and possible relevance of hepatic uptake and efflux transporters involvement.
AID132259Efficacy against lethal mouse infected ip with park strain of Streptococcus pneumoniae administered sc to 19-21-g random sex ICR mice at 1 hr and 5 hr1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID207113Percentage zonal reduction was evaluated against Staphylococcus aureus1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
Dependence of beta-lactamase stability on substructures within beta-lactam antibiotics.
AID679553TP_TRANSPORTER: uptake in PEPT2-expressing HeLa cells1995The Journal of biological chemistry, Oct-27, Volume: 270, Issue:43
Differential recognition of beta -lactam antibiotics by intestinal and renal peptide transporters, PEPT 1 and PEPT 2.
AID208470The compound was tested for antibacterial activity against Streptococcus pneumoniae Park.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 2. Structure-activity studies of bicyclic glycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID206180Tested for inhibition of visible growth of Staphylococcus aureus, benzyl-penicillin sensitive1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID1134633Antibacterial activity against Staphylococcus aureus Smith infected in sc dosed mouse administered 1 hr post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1625551Stability in human liver microsomes assessed as compound metabolism up to 60 mins2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID74714Inhibition of gram positive bacteria growth.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and antimicrobial properties of substituted beta-aminoxypropionyl penicillins and cephalosporins.
AID208959Antibacterial activity in mice infected with Streptococcus pyogenes C203 after oral administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1134634Antibacterial activity against Staphylococcus aureus Smith infected in sc dosed mouse administered 1 hr and 5 hrs post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1625536Antimycobacterial activity against non-replicating Mycobacterium tuberculosis mc2 6220 harboring panCD/lysA deletion mutant incubated for 6 days measured at OD580 = 0.01 by two-fold serial dilution method2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
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.
AID206417Antibacterial activity in mice infected with Staphylococcus aureus 3055 by subcutaneous administration1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID133285Minimum inhibitory concentration against mouse infected with 3055 strain of Staphylococcus aureus1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID363001Antibacterial activity against Staphylococcus aureus after 48 hrs by tube dilution method2008European journal of medicinal chemistry, May, Volume: 43, Issue:5
Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(4-phenylethynyl-phenyl)-1H-benzimidazoles and N-substituted 2[4-(4,4-dimethyl-thiochroman-6-yl-ethynyl)-phenyl)-1H-benzimidazoles.
AID1147079In vivo antibacterial activity against Streptococcus pyogenes infected in po dosed albino CD-1 mouse assessed as protection against bacterial infection by measuring host survival administered at 1 hr and 4 hrs after infection1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID519114Antibacterial activity against Proteus mirabilis M 23 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID1067498Inhibition of Staphylococcus aureus PBP2a2014ACS medicinal chemistry letters, Feb-13, Volume: 5, Issue:2
Neutral β-Lactams Inactivate High Molecular Mass Penicillin-Binding Proteins of Class B1, Including PBP2a of MRSA.
AID1134608Antibacterial activity against beta-lactamase producing benzylpenicillin-resistant Staphylococcus aureus Russell after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID25254Pseudo-first-order Rate constant for hydrolysis at pH 101988Journal of medicinal chemistry, Jun, Volume: 31, Issue:6
The acylating potential of gamma-lactam antibacterials: base hydrolysis of bicyclic pyrazolidinones.
AID1134609Antibacterial activity against Escherichia coli after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID94045Tested for inhibition of visible growth of Klebsiella pneumoniae1980Journal of medicinal chemistry, Apr, Volume: 23, Issue:4
Orally active cephalosporins and penicillins.
AID1147066In vitro antibacterial activity against benzylpenicillin-resistant Staphylococcus epidermidis assessed as growth inhibition after 17 hrs by serial two-fold dilution technique1979Journal of medicinal chemistry, Nov, Volume: 22, Issue:11
Cephalosporin derivatives with 2- and 4-pyridone groups at carbon-3.
AID132257Efficacy against lethal mouse infected ip with C203 strain of Streptococcus pyogenes, administered sc to 19-21-g random sex ICR mice at 1 hr and 5 hr1988Journal of medicinal chemistry, Oct, Volume: 31, Issue:10
Oral absorption of cephalosporin antibiotics. 1. Synthesis, biological properties, and oral bioavailability of 7-(arylacetamido)-3-chloro cephalosporins in animals.
AID678786TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes1999The Journal of pharmacology and experimental therapeutics, Aug, Volume: 290, Issue:2
The interaction and transport of beta-lactam antibiotics with the cloned rat renal organic anion transporter 1.
AID1774079Stabilization of TTR V3OM mutant (unknown origin) assessed as acid-mediated protein aggregation inhibition ratio at 10 uM incubated for 1 week by absorbance method2021Journal of medicinal chemistry, 10-14, Volume: 64, Issue:19
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.
AID208931Antibacterial activity in mice infected with Streptococcus pneumoniae Park11985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID74713Inhibition of gram negative (resistant) growth.1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Synthesis and antimicrobial properties of substituted beta-aminoxypropionyl penicillins and cephalosporins.
AID1149737Antibacterial activity against beta-lactamase producing benzylpenicillin-resistant Staphylococcus aureus Russell assessed as growth inhibition after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids.
AID206095Antibacterial activity against Streptococcus group D X66.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1134642Antibacterial activity against Escherichia coli 8 infected in po dosed mouse administered 1 hr and 5 hrs post infection1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID1209734Inhibition of mouse OAT1 expressed in CHO cells assessed as inhibition of fluorescein uptake at 500 uM over 20 mins relative to untreated-control2013Drug metabolism and disposition: the biological fate of chemicals, Apr, Volume: 41, Issue:4
Organic anion transporter 3 interacts selectively with lipophilic β-lactam antibiotics.
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.
AID519113Antibacterial activity against Proteus mirabilis M 21 mutant after 18 hrs by Etest method2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Reduced Susceptibility of Proteus mirabilis to triclosan.
AID206043The compound was tested for antibacterial activity against Staphylococcus epidermidis EP11.1985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 3. Preparation of biologically active R isomer of 7-(3-benzothienylglycylamido)deacetoxycephalosporanic acid.
AID1625547Stability of compound in pH 12 solution assessed as parent compound remaining incubated for 4 hrs at 37 degC2016Journal of medicinal chemistry, 07-14, Volume: 59, Issue:13
Novel Cephalosporins Selectively Active on Nonreplicating Mycobacterium tuberculosis.
AID209132Antibacterial activity in mice infected with Streptococcus pyogenes C2031985Journal of medicinal chemistry, Dec, Volume: 28, Issue:12
Orally absorbable cephalosporin antibiotics. 1. Structure-activity relationships of benzothienyl- and naphthylglycine derivatives of 7-aminodeacetoxycephalosporanic acid.
AID1134612Antibacterial activity against Klebsiella aerogenes after 18 hrs by serial dilution method1977Journal of medicinal chemistry, Aug, Volume: 20, Issue:8
Structure--activity relationships in cephalosporins prepared from penicillins. 2. Analogues of cephalexin substituted in the 3-methyl group.
AID680865TP_TRANSPORTER: inhibition of Cefadroxil uptake (apical pH 6.5, Cefadroxil: 1000 uM, Cephalexin: 10000 uM) in Caco-2 cells1996The Journal of pharmacology and experimental therapeutics, May, Volume: 277, Issue:2
Transport characteristics of differently charged cephalosporin antibiotics in oocytes expressing the cloned intestinal peptide transporter PepT1 and in human intestinal Caco-2 cells.
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.
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.
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.
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.
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.
AID1347412qHTS assay to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: Counter screen cell viability and HiBit confirmation2020ACS 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.
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.
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.
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.
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.
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.
AID1745845Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
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.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID504812Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
AID504810Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign2010Endocrinology, Jul, Volume: 151, Issue:7
A small molecule inverse agonist for the human thyroid-stimulating hormone receptor.
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.
AID1159550Human Phosphogluconate dehydrogenase (6PGD) Inhibitor Screening2015Nature cell biology, Nov, Volume: 17, Issue:11
6-Phosphogluconate dehydrogenase links oxidative PPP, lipogenesis and tumour growth by inhibiting LKB1-AMPK signalling.
AID1159607Screen for inhibitors of RMI FANCM (MM2) intereaction2016Journal of biomolecular screening, Jul, Volume: 21, Issue:6
A High-Throughput Screening Strategy to Identify Protein-Protein Interaction Inhibitors That Block the Fanconi Anemia DNA Repair Pathway.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (2,099)

TimeframeStudies, This Drug (%)All Drugs %
pre-19901204 (57.36)18.7374
1990's267 (12.72)18.2507
2000's264 (12.58)29.6817
2010's258 (12.29)24.3611
2020's106 (5.05)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 133.26

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be very strong demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index133.26 (24.57)
Research Supply Index7.85 (2.92)
Research Growth Index4.45 (4.65)
Search Engine Demand Index257.65 (26.88)
Search Engine Supply Index2.04 (0.95)

This Compound (133.26)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials338 (15.16%)5.53%
Trials0 (0.00%)5.53%
Reviews79 (3.54%)6.00%
Reviews0 (0.00%)6.00%
Case Studies242 (10.86%)4.05%
Case Studies0 (0.00%)4.05%
Observational1 (0.04%)0.25%
Observational0 (0.00%)0.25%
Other1,569 (70.39%)84.16%
Other5 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (67)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Prospective, Randomized, Open Label, Crossover Study to Compare the Bioavailability Between Optocef From Bayer (Cephalexin Suspension 250 mg/5 mL and Equivalent Concentration of Keflex Pediatrico From Eli Lilly (Cephalexin Suspension 125 mg/5mL) in Health [NCT01105208]Phase 126 participants (Actual)Interventional2010-03-31Completed
The Role of Antibiotics in Full Thickness Skin Graft Survival for Facial Reconstructive Surgery [NCT01912651]Phase 4300 participants (Anticipated)Interventional2013-07-31Recruiting
Randomized Noninferiority Study of an Antibacterial Envelope Alone Versus Envelope Plus Intraoperative Antibacterial Irrigant and Postoperative Antibiotics to Prevent Cardiac Implantable Electronic Device Infections in High-Risk Patients [NCT02809131]Phase 31,010 participants (Actual)Interventional2016-04-01Completed
Combination Vs Single Antibiotics for Prevention of SSI in Obese Women Undergoing CS [NCT03736187]280 participants (Anticipated)Interventional2019-04-30Not yet recruiting
Impact of Antibiotic Treatment Following Implantation of Cardiac Electronic Device on Patient's Outcome [NCT03148444]Phase 4400 participants (Anticipated)Interventional2017-06-01Not yet recruiting
Antibiotic Treatment for Intermittent Bladder Catheterisation: A Randomised Controlled Trial of Once Daily Prophylaxis [NCT02145338]Phase 4404 participants (Actual)Interventional2013-09-30Completed
Prospective, Randomized, Open Label, Crossover Study to Compare the Bioavailability Between Optocef Suspension From Bayer (Cephalexin Suspension 250 mg/5 mL) and Equivalent Concentration of Keflex Pediatrico From Eli Lilly (Cephalexin Suspension 125 mg/5m [NCT01073540]Phase 126 participants (Actual)Interventional2009-09-30Completed
Use of 48 Hour Course of Antibiotics to Prevent Surgical Site Infection in Obese Patients Undergoing Cesarean Delivery [NCT01194115]475 participants (Anticipated)Interventional2010-09-30Enrolling by invitation
Postoperative Antibiotic Management Duration Following Surgery for Intravenous Drug Abuse (IVDA) Endocarditis (OPTIMAL) [NCT05156437]Phase 420 participants (Anticipated)Interventional2022-03-16Enrolling by invitation
Does Post-operative Antibiotic Prophylaxis Reduce Urinary Tract Infection Rates After Holmium Laser Enucleation of Prostate? a Prospective Randomized Multi-center Study [NCT05274672]Phase 4100 participants (Anticipated)Interventional2022-03-01Not yet recruiting
Comparing Oral Versus Parenteral Antimicrobial Therapy (COPAT) Trial [NCT05977868]Phase 4135 participants (Anticipated)Interventional2023-08-04Enrolling by invitation
High-dose Cephalexin for Cellulitis (HI-DOCC) [NCT05852262]Phase 4446 participants (Anticipated)Interventional2023-08-30Recruiting
Personalized Antibiotic Treatment in the Emergency Department: Panther Trial [NCT06127160]Phase 440 participants (Anticipated)Interventional2024-01-31Not yet recruiting
Use of Prophylactic Antibiotics Prior to OnabotulinumtoxinA Treatment of Overactive Bladder: a Randomized Controlled Trial [NCT05519072]Phase 4140 participants (Anticipated)Interventional2022-08-16Recruiting
Microbiome and Association With Implant Infections: Investigating the Impact of Antibiotics on the Gut and Breast Microbiomes Post-mastectomy With Implant-based Breast Reconstruction [NCT05020574]Phase 2200 participants (Anticipated)Interventional2021-09-28Recruiting
Early Bactericidal Activity of Cephalexin and Amoxicillin-clavulanate for Susceptible Tuberculosis - BLAST 1 Trial [NCT05664568]Phase 230 participants (Anticipated)Interventional2023-03-15Recruiting
A Randomized, Placebo Controlled Trial of the Effect of Prophylactic Antibiotics on Surgical Site Infection Lower Limb Skin Excisions [NCT03357419]0 participants (Actual)Interventional2021-03-31Withdrawn(stopped due to difficulties in production placebo antibiotics)
Surgical Site Infection (SSI) Rates in Patients Undergoing Mastectomy Without Reconstruction, a Comparison Among Those Receiving Preoperative Prophylactic Antibiotics Alone Versus Continued Prophylactic Antibiotics Postoperatively-A Multicenter, Double-bl [NCT04577846]Phase 3384 participants (Anticipated)Interventional2020-11-01Not yet recruiting
Prevention of Arrhythmia Device Infection Trial (PADIT) Cluster Crossover Study [NCT01628666]Phase 412,814 participants (Actual)Interventional2012-12-31Completed
Post-procedure Antibiotic Prophylaxis for Cardiac Electrical Device Implantation: ABxFREE Study [NCT04146883]800 participants (Anticipated)Interventional2019-08-20Recruiting
A Multicenter, Randomized, Observer-Blinded, Active-Controlled Study to Evaluate the Safety, Tolerability, Efficacy, and Pharmacokinetics of Ceftaroline Versus Comparator in Pediatric Subjects With Acute Bacterial Skin and Skin Structure Infections [NCT01400867]Phase 2/Phase 3163 participants (Actual)Interventional2011-12-31Completed
High-dose Cephalexin for Cellulitis: A Pilot Randomized Controlled Trial [NCT04471246]Phase 466 participants (Actual)Interventional2021-08-16Completed
Intravenous Cefazolin Plus Oral Probenecid vs. Oral Cephalexin for the Treatment of Cellulitis: a Randomized Controlled Trial [NCT01029782]Phase 2206 participants (Actual)Interventional2010-05-31Completed
Randomized Trial of Trimethoprim-Sulfamethoxazole Versus Placebo Added to Standard Treatment of Uncomplicated Cellulitis in Emergency Department Patients [NCT00676130]153 participants (Actual)Interventional2007-05-31Completed
"Strategies Using Off-Patent Antibiotics for Methicillin-Resistant Staphylococcus Aureus (STOP MRSA) - A Phase IIB, Multi-Center, Randomized, Double-Blind Clinical Trial" [NCT00729937]Phase 2/Phase 32,265 participants (Actual)Interventional2009-04-30Completed
Phase III Pilot Study - A Simple Randomized Trial of Conventional Versus Multimodal Prevention of Arrhythmia Device Infection [NCT01002911]Phase 3500 participants (Actual)Interventional2009-12-31Completed
Comparison of Outcomes in Rhinoplasty With the Use of Intraoperative Versus Postoperative Antibiotics [NCT04194216]Phase 3864 participants (Anticipated)Interventional2020-05-20Enrolling by invitation
Prospective, Randomized, Open Label, Crossover Study to Compare the Bioavailability Between Optocef (Cephalexin 500 mg Capsules) From Bayer and Keflex (Cephalexin 250 mg Capsules) From Eli Lilly po in Healthy Subjects Using Equivalent Concentrations [NCT01073553]Phase 126 participants (Actual)Interventional2009-10-31Completed
Antibiotic Prophylaxis in Prosthetic Breast Reconstructions [NCT02012517]Phase 4160 participants (Anticipated)Interventional2014-01-31Not yet recruiting
A Phase 1/2 Open-Label, Dose Escalation Study Investigating the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of ASP2215 in Patients With Relapsed or Refractory Acute Myeloid Leukemia [NCT02014558]Phase 1/Phase 2265 participants (Actual)Interventional2013-10-09Completed
Postoperative Healthcare Utilization in Adenotonsillectomy Patients With Postoperative Antibiotic Administration Compared to Patients Without Antibiotic Administration [NCT01561703]58 participants (Actual)Interventional2012-03-31Completed
Antibiotics After Breast Reduction:Clinical Trial With Randomization [NCT02569866]Phase 2124 participants (Actual)Interventional2014-11-30Completed
Prophylactic Antibiotics After Cesarean [NCT03187106]Phase 1321 participants (Actual)Interventional2017-08-01Completed
[NCT02911662]13 participants (Actual)Interventional2016-09-30Terminated(stopped due to Inability to enroll patients at anticipated rate.)
[NCT01248078]1,112 participants (Actual)Interventional2004-03-31Completed
Open, Two Periods, Two Treatments, Two Sequences, Cross-over, Randomized Study With Single Dosage of Two Oral Preparations Containing 1 g of Cephalexin (GlaxoSmithKline México, S.A. de C.V. vs. Keflex® 1g, Eli Lilly y Compañía de México, S.A. de C.V.) in [NCT01767584]Phase 126 participants (Actual)Interventional2009-04-06Completed
A Comparative Study of the Safety, Tolerability, and Efficacy of Cefdinir and Cephalexin for the Treatment of Subjects With Mild to Moderate Uncomplicated Skin and Skin Structure Infections [NCT00234949]Phase 4380 participants Interventional2005-03-31Completed
Antibiotic Prophylaxis in High-Risk Arthroplasty Patients [NCT04297592]Phase 44,618 participants (Anticipated)Interventional2020-06-11Enrolling by invitation
A Placebo Controlled, Randomized, and Blinded Study of Antibiotic Treatment of Patients With Uncomplicated Soft Tissue Infection [NCT00187759]500 participants Interventional2004-11-30Completed
Single Dose Aminoglycosides for Acute Uncomplicated Cystitis in the Emergency Department Setting [NCT05702762]Phase 2160 participants (Anticipated)Interventional2022-10-01Recruiting
CHOICE UTI - Clinical Efficacy of Single Dose (Daily) IV Antibiotics Followed by 2 Days Oral Antibiotics Compared to 3 Doses (Daily) IV Antibiotics for Children With Complicated Urinary Tract Infections: a Multicentre Randomised Trial [NCT04876131]Phase 4452 participants (Anticipated)Interventional2022-05-30Recruiting
A Randomized, Open-label, Two-period, Two-treatment, Two-sequence, Crossover Study to Evaluate the Bioequivalence of Single Doses of Two Oral Preparations in Suspension With 250 mg/5 ml of Cephalexin (Keflex® Liquido Made in Mexico by Eli Lilly y compañía [NCT02490670]Phase 128 participants (Actual)Interventional2015-07-31Completed
Oral Amoxicillin and Cephalexin Pharmacokinetics/Pharmacodynamics (PK/PD) in the Neonatal Intensive Care Unit [NCT04916951]Phase 160 participants (Anticipated)Interventional2021-07-14Enrolling by invitation
The Placebo Effect May Involve Modulating Drug Bioavailability [NCT01501747]162 participants (Actual)Interventional2012-02-29Completed
The Efficacy of Preventive Antibiotic Treatment During the Puerperium Among Pregnant Women With Recurrent Urinary Tract Infections [NCT01507974]220 participants (Actual)Interventional2012-01-16Completed
Comparison of Cephalexin Versus Clindamycin in the Empiric, Outpatient Treatment of Suspected Staphylococcal Cutaneous Infections in the Era of Community-associated Methicillin-resistant Staphylococcus Aureus (CA-MRSA) [NCT00352612]Phase 4200 participants (Actual)Interventional2006-09-30Completed
A Randomized, Open-label, Two-period, Two-treatment, Two-sequence, Crossover Study to Evaluate the Bioequivalence of Single Doses of Two Oral Preparations in Capsules With 250 mg of Cephalexin (Keflex® Made in Mexico by Eli Lilly y Compañía de México, S.A [NCT02123446]Phase 128 participants (Actual)Interventional2014-04-30Completed
Effects of Treatments on the Microbiome in Healthy Volunteers and Patients With Atopic Dermatitis [NCT01631617]Phase 2130 participants (Anticipated)Interventional2012-09-18Recruiting
Open, Two Periods, Two Treatments, Two Sequences, Cross-over, Randomized Study With Single Dosage of Two Oral Preparation of Cephalexin 125 mg/ 5 ml (Ceporex® GlaxoSmithKline México, S.A. de C.V. vs. Keflex®, Eli Lilly y Compañía de México, S.A. de C.V.) [NCT01767532]Phase 128 participants (Actual)Interventional2011-01-30Completed
Open, Two Periods, Two Treatments, Two Sequences, Cross-over, Randomized Study With Single Dosage of Two Oral Preparation of Cephalexin 250 mg/5mL (Ceporex®, GlaxoSmithKline México, S.A. de C.V. vs. Keflex® , Eli Lilly y Compañía de México, S.A. de C.V.) [NCT01767571]Phase 128 participants (Actual)Interventional2011-01-30Completed
Orthognathic Surgery and Postoperative Antibiotic Use [NCT01823523]300 participants (Anticipated)Interventional2013-06-30Recruiting
Randomized, Open-label, 2-period, 2-treatment, 2-sequence, Crossover Study to Evaluate the Bioequivalence of Single Doses of 2 Oral Preparations in Tablets With 1g of Cephalexin (Keflex® Made in Mexico by Eli Lilly vs. Keflex® Made in Italy by Facta) in F [NCT02100826]Phase 128 participants (Actual)Interventional2014-04-30Completed
Antibiotic Treatment Of Staphylococcus Aureus In Stable People With CF (ASAP-CF) Clinical Research Protocol [NCT04553419]Phase 386 participants (Anticipated)Interventional2020-07-27Recruiting
Prevention of Arrhythmia Device Infection Trial (PADIT) Cluster Crossover Pilot Study [NCT01613092]Phase 4241 participants (Actual)Interventional2011-05-31Completed
Impact of Prophylactic Perioperative Antibiotic Administration on Surgical Site Infections Following Implant-based Breast Reconstruction. [NCT01899690]Phase 40 participants (Actual)Interventional2016-06-30Withdrawn(stopped due to The study was withdrawn prior to IRB approval.)
Antibiotic Prophylaxis for Prevention of Infection in Emergency Department Patients With Simple Hand Lacerations [NCT01155154]73 participants (Actual)Interventional2010-02-28Terminated
The Effect of Fluoroquinolones on the Disease-Free Interval in Patients With Stage Ta Transitional Cell Carcinoma of the Bladder [NCT00003824]Phase 3114 participants (Actual)Interventional1999-04-30Terminated(stopped due to Permanently Closed Due to Poor Accrual)
A Randomized, Open-label, Two-period, Two-treatment, Two-sequence, Crossover Study to Evaluate the Bioequivalence of Single Doses of Two Oral Preparations in Suspension With 125 mg/5 ml of Cephalexin (Keflex® Pediatrico Made in Mexico by Eli Lilly y Compa [NCT02123472]Phase 128 participants (Actual)Interventional2014-05-31Completed
Prophylactic Use of Antibiotics for Through and Through Lacerations of the Lip [NCT00957827]4 participants (Actual)Interventional2009-08-31Terminated(stopped due to Not enough subject enrolled)
"Targeted Clinical Trials to Reduce the Risk of Antimicrobial Resistance The SCOUT Study: Short Course Therapy for Urinary Tract Infections in Children" [NCT01595529]Phase 2717 participants (Actual)Interventional2012-05-18Completed
Comparative Pharmacokinetics and Pharmacodynamics (PK/PD) of Cefadroxil and Cephalexin for Pediatric Musculoskeletal (MSK) Infections [NCT03802552]Phase 117 participants (Actual)Interventional2019-05-01Completed
Utility of Single-dose Oral Antibiotic Prophylaxis in Prevention of Surgical Site Infection in Dermatologic Surgery [NCT04580472]Phase 41,600 participants (Anticipated)Interventional2020-10-01Recruiting
Phase 3 Study of IV to Oral 6-Day Tedizolid Phosphate Compared With 10-day Comparator in Subjects 12 to < 18 Years With cSSTI. [NCT02276482]Phase 3120 participants (Actual)Interventional2015-03-25Completed
BonE and Joint Infections - Simplifying Treatment in Children Trial [NCT04538053]Phase 4285 participants (Anticipated)Interventional2021-06-01Recruiting
A Randomized, Open-label, Two-period, Two-treatment, Two-sequence, Crossover Study to Evaluate the Bioequivalence of Single Doses of Two Oral Preparations in Suspension With 250 mg/5 ml of Cephalexin (Keflex® Liquido Made in Mexico by Eli Lilly y Compañía [NCT02123459]Phase 128 participants (Actual)Interventional2014-05-31Completed
Antibiotic Prophylaxis in Pediatric Open Fractures [NCT06055712]Phase 4800 participants (Anticipated)Interventional2023-09-11Enrolling by invitation
Postoperative Antibiotics Following Primary and Secondary Breast Augmentation: A Double-Blinded, Randomized Trial [NCT04834310]Phase 40 participants (Actual)Interventional2021-04-01Withdrawn(stopped due to Do not have adequate funding to proceed with project.)
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00352612 (1) [back to overview]Clinical Improvement at the 48-72 Hour Clinical Follow-up
NCT00676130 (2) [back to overview]Progression to Abscess
NCT00676130 (2) [back to overview]Relative Efficacy
NCT00729937 (31) [back to overview]Number of Participants With Development of an Invasive Infection Through the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Mean Days Missed From Normal Activities in the Intent to Treat Population
NCT00729937 (31) [back to overview]Mean Days Missed From Normal Activities in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants Requiring Surgical Intervention Through the Extended Follow-up Visit (EFV) in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants Requiring Surgical Intervention Through the Extended Follow-up Visit (EFV) in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants Requiring Surgical Intervention Through the TOC Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants Requiring Surgical Intervention Through the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the EFV Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the EFV Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the TOC Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Development of an Invasive Infection Through the EFV Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants With Development of an Invasive Infection Through the EFV Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Development of an Invasive Infection Through the TOC Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants Reporting 1-14 Days of Analgesic Use in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants With Infections in Household Contacts Through the EFV Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants With Infections in Household Contacts Through the EFV Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Infections in Household Contacts Through the TOC Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants With Infections in Household Contacts Through the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants by Composite Clinical Outcome at the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the End-of-therapy Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants Reporting 1-14 Days of Analgesic Use in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Adverse Events Considered Associated With the Study Product by MedDRA System Organ Class
NCT00729937 (31) [back to overview]Number of Participants With Clinical Cure as of the Test-of-Cure (TOC) Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Clinical Cure as of the TOC Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants With Each Microbiological Outcome at the TOC Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the End-of-therapy Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the On-therapy Visit in the Intent to Treat Population
NCT00729937 (31) [back to overview]Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the On-therapy Visit in the Per Protocol Population
NCT00729937 (31) [back to overview]Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the TOC Visit in the Intent to Treat Population
NCT01029782 (1) [back to overview]The Number of Patients Failing Therapy After 72 Hours of Antibiotic Treatment With Oral Cephalexin or Intravenous Cefazolin Plus Oral Probenecid.
NCT01155154 (1) [back to overview]Number of Participants With Presence of Wound Infection
NCT01561703 (1) [back to overview]Healthcare Utilization
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects With Asymptomatic Bacteriuria Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population.
NCT01595529 (12) [back to overview]Comparison of Efficacy Based on Symptomatic Urinary Tract Infection (UTI) Between Short-course and Standard-course of Antibiotics.
NCT01595529 (12) [back to overview]Comparison of Efficacy Based on Symptomatic Urinary Tract Infection (UTI) Between Short-course and Standard-course of Antibiotics. Per-protocol Population.
NCT01595529 (12) [back to overview]Comparison of Number of Subjects That Have a Recurrent Infection (Includes a Relapse UTI or a Reinfection) Following Short-course Versus Standard-course of Antibiotics.
NCT01595529 (12) [back to overview]Comparison of Number of Subjects That Have a Recurrent Infection (Includes a Relapse UTI or a Reinfection) Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population.
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects With Asymptomatic Bacteriuria Following Short-course Versus Standard-course of Antibiotics.
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects With Clinical Symptoms That May be Related to a UTI Following Short-course Versus Standard-course of Antibiotics.
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects With Clinical Symptoms That May be Related to a UTI Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects With Positive Urine Cultures Following Short-course Versus Standard-course of Antibiotics.
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects With Positive Urine Cultures Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population.
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects That Become Colonized With Antimicrobial Resistant E. Coli and K. Pneumoniae in the Gastrointestinal Tract Following Short-course Versus Standard Course of Antibiotics. Per-protocol Population.
NCT01595529 (12) [back to overview]Comparison of the Number of Subjects That Become Colonized With Antimicrobial Resistant Escherichia Coli (E. Coli) and Klebsiella Pneumoniae (K. Pneumoniae) in the Gastrointestinal Tract Following Short-course Versus Standard Course of Antibiotics.
NCT02014558 (70) [back to overview]Apparent Total Systemic Clearance After Single or Multiple Extravascular Dosing (CL/F) of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Apparent Volume of Distribution During the Terminal Elimination Phase After Single Extravascular Dosing (Vz/F) of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Area Under the Concentration-time Curve From the Time of Dosing Extrapolated to Time Infinity (AUCinf) of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Area Under the Concentration-time Curve From the Time of Dosing to the Last Measurable Concentration (AUClast) After Single and Multiple Doses of Gilteritinib
NCT02014558 (70) [back to overview]Area Under the Concentration-time Curve Over the 24-Hour Dosing Interval (AUC24) After Single and Multiple Doses of Gilteritinib
NCT02014558 (70) [back to overview]AUC24 of Metabolite 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib
NCT02014558 (70) [back to overview]AUC24 of Midazolam Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]AUClast of 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib
NCT02014558 (70) [back to overview]AUClast of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]AUClast of Midazolam Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Cmax of 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib
NCT02014558 (70) [back to overview]Cmax of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Cmax of Midazolam Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Duration of CR (DCR)
NCT02014558 (70) [back to overview]Duration of CR (DCR)
NCT02014558 (70) [back to overview]Duration of CRc (DCRc)
NCT02014558 (70) [back to overview]Duration of CRc (DCRc)
NCT02014558 (70) [back to overview]Duration of CRi (DCRi)
NCT02014558 (70) [back to overview]Duration of CRi (DCRi)
NCT02014558 (70) [back to overview]Duration of CRp (DCRp)
NCT02014558 (70) [back to overview]Duration of Response
NCT02014558 (70) [back to overview]Duration of Response
NCT02014558 (70) [back to overview]Event Free Survival (EFS)
NCT02014558 (70) [back to overview]Fraction of Drug Excreted Into Urine in Percentage (%Ae) of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Leukemia Free Survival (LFS)
NCT02014558 (70) [back to overview]Leukemia Free Survival (LFS)
NCT02014558 (70) [back to overview]Maximum Concentration (Cmax) After Single and Multiple Doses of Gilteritinib
NCT02014558 (70) [back to overview]Number of Participants With Adverse Events (AEs)
NCT02014558 (70) [back to overview]Number of Participants With Dose Limiting Toxicities (DLTs)
NCT02014558 (70) [back to overview]Overall Survival (OS)
NCT02014558 (70) [back to overview]Percentage of Participants Who Achieved Transfusion Conversion
NCT02014558 (70) [back to overview]Percentage of Participants Who Achieved Transfusion Maintenance
NCT02014558 (70) [back to overview]Percentage of Participants Who Achieved Transfusion Maintenance
NCT02014558 (70) [back to overview]Percentage of Participants With Best Response
NCT02014558 (70) [back to overview]Percentage of Participants With Complete Remission (CR) During the First 2 Cycles
NCT02014558 (70) [back to overview]Percentage of Participants With Composite CR (CRc)
NCT02014558 (70) [back to overview]Percentage of Participants With CR During Treatment
NCT02014558 (70) [back to overview]Percentage of Participants With CR With Incomplete Hematological Recovery (CRi)
NCT02014558 (70) [back to overview]Percentage of Participants With CR With Incomplete Platelet Recovery (CRp)
NCT02014558 (70) [back to overview]Percentage of Participants With Partial Remission (PR)
NCT02014558 (70) [back to overview]Renal Clearance (CLr) of Cephalexin in Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]T1/2 of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Time to Best Response (TTBR)
NCT02014558 (70) [back to overview]Time to Best Response (TTBR)
NCT02014558 (70) [back to overview]Time to CR (TTCR)
NCT02014558 (70) [back to overview]Time to CR (TTCR)
NCT02014558 (70) [back to overview]Time to CRc (TTCRc)
NCT02014558 (70) [back to overview]Time to CRc (TTCRc)
NCT02014558 (70) [back to overview]Time to CRi (TTCRi)
NCT02014558 (70) [back to overview]Time to CRi (TTCRi)
NCT02014558 (70) [back to overview]Time to CRp (TTCRp)
NCT02014558 (70) [back to overview]Time to Observed Cmax (Tmax) After Single and Multiple Doses of Gilteritinib
NCT02014558 (70) [back to overview]Time to Response (TTR)
NCT02014558 (70) [back to overview]Time to Response (TTR)
NCT02014558 (70) [back to overview]Tmax of 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib
NCT02014558 (70) [back to overview]Tmax of Cephalexin Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Tmax of Midazolam Administered With and Without Gilteritinib
NCT02014558 (70) [back to overview]Accumulation Ratio After Multiple Doses of Gilteritinib
NCT02014558 (70) [back to overview]AUC24 of Gilteritinib in Co-administration With Voriconazole
NCT02014558 (70) [back to overview]AUClast of Gilteritinib in Co-administration With Voriconazole
NCT02014558 (70) [back to overview]Cmax of Gilteritinib in Co-administration With Voriconazole
NCT02014558 (70) [back to overview]Duration of CR/CRh (DCRCRh)
NCT02014558 (70) [back to overview]Duration of CRh (DCRh)
NCT02014558 (70) [back to overview]Percentage of Participants With Complete Remission and Complete Remission With Partial Hematologic Recovery (CR/CRh)
NCT02014558 (70) [back to overview]Percentage of Participants With Complete Remission With Partial Hematologic Recovery (CRh)
NCT02014558 (70) [back to overview]Terminal Elimination Half-life (t1/2) After Multiple Doses of Gilteritinib
NCT02014558 (70) [back to overview]Time to Best CR/CRh (TTBCRCRh)
NCT02014558 (70) [back to overview]Time to First CR/CRh (TTFCRCRh)
NCT02014558 (70) [back to overview]Tmax of Gilteritinib in Co-administration With Voriconazole
NCT02014558 (70) [back to overview]Amount of Drug Excreted in Urine (Aelast) of Cephalexin Administered With and Without Gilteritinib
NCT02100826 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose
NCT02100826 (3) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin
NCT02100826 (3) [back to overview]Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum
NCT02123446 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve of Cephalexin From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose
NCT02123446 (3) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin
NCT02123446 (3) [back to overview]Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum
NCT02123459 (3) [back to overview]Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum
NCT02123459 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose
NCT02123459 (3) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin
NCT02123472 (3) [back to overview]Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum
NCT02123472 (3) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose
NCT02123472 (3) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin
NCT02276482 (9) [back to overview]Area Under the Plasma Concentration Versus Time Curve Time 0 to 24 Hours (AUC0-24h) of Tedizolid
NCT02276482 (9) [back to overview]Number of Participants With Adverse Events on Tedizolid Phosphate and Comparator Drugs
NCT02276482 (9) [back to overview]Number of Participants With Early Clinical Responses Measured by Lesion Reduction
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at End of Therapy (EOT) Visit (Intent to Treat Analysis Set)
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at EOT Visit (Clinically Evaluable-End of Therapy [CE-EOT] Analysis Set)
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at Test of Cure (TOC) Visit (Intent to Treat Analysis Set)
NCT02276482 (9) [back to overview]Number of Participants With Investigator's Assessment Indicating Clinical Success at TOC Visit (Clinically Evaluable-Test of Cure [CE-TOC] Analysis Set)
NCT02276482 (9) [back to overview]Peak Plasma Concentration (Cmax) of Tedizolid
NCT02276482 (9) [back to overview]Change From Baseline in Lesion Size
NCT02490670 (2) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin Following a Single Dose
NCT02490670 (2) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Cephalexin Following a Single Dose
NCT02809131 (2) [back to overview]Number of Patients With a Major Cardiac Implantable Electronic Devices (CIED) Infection
NCT02809131 (2) [back to overview]Number of Patients With a Minor Cardiac Implantable Electronic Devices (CIED) Infection

Clinical Improvement at the 48-72 Hour Clinical Follow-up

Clinical improvement was defined as improvement in at least one of the following four measures without regression in any: (1) erythema (2) pain (3) induration (4) patient or families self report of improvement. (NCT00352612)
Timeframe: 48-72 hour clinical follow-up

Interventionparticipants (Number)
Cephalexin94
Clindamycin97

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Progression to Abscess

Proportion of subjects in each arm with progression from cellulitis to abscess. (NCT00676130)
Timeframe: 12 +/- 2 days, 30 days +/- 2 days

Interventionparticipants (Number)
Trimethoprim-sulfamethoxazole5
Placebo5

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Relative Efficacy

"Proportion of subjects in each arm with successful treatment.~Treatment success was assessed by physician examination at 12 +/- 2 days. Non-success was defined as subsequent hospitalization, change in antibiotics, surgical or needle drainage of an abscess, or recurrence of infection within 30 days. Cure was defined as resolution of all symptoms other than mild residual erythema or edema. We confirmed the determination of cure by telephone interview and medical record review at 30 +/- 2 days." (NCT00676130)
Timeframe: 12 +/- 2 days; 30 +/- 2 days

Interventionparticipants (Number)
Trimethoprim-sulfamethoxazole62
Placebo60

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Number of Participants With Development of an Invasive Infection Through the TOC Visit in the Per Protocol Population

Participants were evaluated for invasive infection, which included, but was not limited to, findings of severe sepsis/septic shock, endocarditis, pneumonia, necrotizing soft tissue, osteomyelitis, and bacteremia. A positive response to at least one finding was considered invasive infection for this outcome measure. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo0
Abscess, TMP/SMX1
Infected Wound, TMP/SMX0
Infected Wound, Clindamycin0
Cellulitis, Cephalexin and TMP/SMX0
Cellulitis, Cephalexin0

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Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the TOC Visit in the Per Protocol Population

The area of erythema was measured in square centimeters at baseline and at the TOC visit. For each subject, the change in area was calculated as the area at TOC subtracted from the area at baseline. The change in area was then divided by the original area to determine the proportional change. Participants were then categorized by reductions in 5% intervals, with participants whose erythema did not change or increased categorized as no reduction. (NCT00729937)
Timeframe: Day 1 to Day 14-21

,,,,,
Interventionparticipants (Number)
No reduction>0%-5% reduction>5%-10% reduction>10%-15% reduction>15%-20% reduction>20%-25% reduction>25%-30% reduction>30%-35% reduction>35%-40% reduction>40%-45% reduction>45%-50% reduction>50%-55% reduction>55%-60% reduction>60%-65% reduction>65%-70% reduction>70%-75% reduction>75%-80% reduction>80%-85% reduction>85%-90% reduction>90%-95% reduction>95%-100% reduction
Abscess, Placebo20000000000000002044520
Abscess, TMP/SMX00000100000000000211516
Cellulitis, Cephalexin00100000000000011000189
Cellulitis, Cephalexin and TMP/SMX20000000010000121100207
Infected Wound, Clindamycin10000000000000000001199
Infected Wound, TMP/SMX10010010000100110000191

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Mean Days Missed From Normal Activities in the Intent to Treat Population

As a quality of life measure, participants maintained a memory aid from Day 1 to Day 14 to track measures such as participation in normal life activities. The maximum number of days assessed, 14, was assigned to participants who had not yet resumed normal activities by the end of the assessment period. (NCT00729937)
Timeframe: Day 1 through 14

Interventiondays (Mean)
Abscess, Placebo2.5
Abscess, TMP/SMX2.1
Infected Wound, TMP/SMX2.6
Infected Wound, Clindamycin2.1
Cellulitis, Cephalexin and TMP/SMX2.2
Cellulitis, Cephalexin2.7

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Mean Days Missed From Normal Activities in the Per Protocol Population

As a quality of life measure, participants maintained a memory aid from Day 1 to Day 14 to track measures such as participation in normal life activities. The maximum number of days assessed, 14, was assigned to participants who had not yet resumed normal activities by the end of the assessment period. (NCT00729937)
Timeframe: Day 1 through 14

Interventiondays (Mean)
Abscess, Placebo2.6
Abscess, TMP/SMX2.0
Infected Wound, TMP/SMX2.7
Infected Wound, Clindamycin2.1
Cellulitis, Cephalexin and TMP/SMX2.2
Cellulitis, Cephalexin2.5

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Number of Participants Requiring Surgical Intervention Through the Extended Follow-up Visit (EFV) in the Intent to Treat Population

All surgical procedures such as incision and drainage (I&D) and debridement that were related to the current infection under study or significant to the health of the subject, except for the initial I&D of an abscess for participants in the abscess or infected wound arms, were recorded. Participants who required a surgical intervention between the initial enrollment (excluding the initial I&D as applicable) and the extended follow-up visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo76
Abscess, TMP/SMX52
Infected Wound, TMP/SMX20
Infected Wound, Clindamycin12
Cellulitis, Cephalexin and TMP/SMX33
Cellulitis, Cephalexin31

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Number of Participants Requiring Surgical Intervention Through the Extended Follow-up Visit (EFV) in the Per Protocol Population

All surgical procedures such as incision and drainage (I&D) and debridement that were related to the current infection under study or significant to the health of the subject, except for the initial I&D of an abscess for participants in the abscess or infected wound arms, were recorded. Participants who required a surgical intervention between the initial enrollment (excluding the initial I&D as applicable) and the extended follow-up visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo69
Abscess, TMP/SMX42
Infected Wound, TMP/SMX17
Infected Wound, Clindamycin8
Cellulitis, Cephalexin and TMP/SMX33
Cellulitis, Cephalexin20

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Number of Participants Requiring Surgical Intervention Through the TOC Visit in the Intent to Treat Population

All surgical procedures such as incision and drainage (I&D) and debridement that were related to the current infection under study or significant to the health of the subject, except for the initial I&D of an abscess for participants in the abscess or infected wound arms, were recorded. Participants who required a surgical intervention between the initial enrollment (excluding the initial I&D as applicable) and the test-of-cure visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo52
Abscess, TMP/SMX25
Infected Wound, TMP/SMX16
Infected Wound, Clindamycin9
Cellulitis, Cephalexin and TMP/SMX26
Cellulitis, Cephalexin28

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Number of Participants Requiring Surgical Intervention Through the TOC Visit in the Per Protocol Population

All surgical procedures such as incision and drainage (I&D) and debridement that were related to the current infection under study or significant to the health of the subject, except for the initial I&D of an abscess for participants in the abscess or infected wound arms, were recorded. Participants who required a surgical intervention between the initial enrollment (excluding the initial I&D as applicable) and the test-of-cure visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo46
Abscess, TMP/SMX18
Infected Wound, TMP/SMX13
Infected Wound, Clindamycin6
Cellulitis, Cephalexin and TMP/SMX26
Cellulitis, Cephalexin17

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Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the EFV Visit in the Intent to Treat Population

Participants were evaluated for the development of a recurrent, or repeat, infection at the original infection site. Participants who were reported to have developed a recurrent infection though the extended follow-up visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo26
Abscess, TMP/SMX30
Infected Wound, TMP/SMX16
Infected Wound, Clindamycin6
Cellulitis, Cephalexin and TMP/SMX35
Cellulitis, Cephalexin31

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Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the EFV Visit in the Per Protocol Population

Participants were evaluated for the development of a recurrent, or repeat, infection at the original infection site. Participants who were reported to have developed a recurrent infection though the extended follow-up visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo23
Abscess, TMP/SMX26
Infected Wound, TMP/SMX14
Infected Wound, Clindamycin4
Cellulitis, Cephalexin and TMP/SMX33
Cellulitis, Cephalexin24

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Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the TOC Visit in the Intent to Treat Population

Participants were evaluated for the development of a recurrent, or repeat, infection at the original infection site. Participants who were reported to have developed a recurrent infection though the test-of-cure visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo17
Abscess, TMP/SMX13
Infected Wound, TMP/SMX15
Infected Wound, Clindamycin4
Cellulitis, Cephalexin and TMP/SMX32
Cellulitis, Cephalexin29

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Number of Participants Who Developed a Recurrent Infection at the Original Infection Site Through the TOC Visit in the Per Protocol Population

Participants were evaluated for the development of a recurrent, or repeat, infection at the original infection site. Participants who were reported to have developed a recurrent infection though the test-of-cure visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo16
Abscess, TMP/SMX11
Infected Wound, TMP/SMX13
Infected Wound, Clindamycin3
Cellulitis, Cephalexin and TMP/SMX30
Cellulitis, Cephalexin22

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Number of Participants With Development of an Invasive Infection Through the EFV Visit in the Intent to Treat Population

Participants were evaluated for invasive infection, which included, but was not limited to, findings of severe sepsis/septic shock, endocarditis, pneumonia, necrotizing soft tissue, osteomyelitis, and bacteremia. A positive response to at least one finding was considered invasive infection for this outcome measure. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo3
Abscess, TMP/SMX2
Infected Wound, TMP/SMX0
Infected Wound, Clindamycin0
Cellulitis, Cephalexin and TMP/SMX1
Cellulitis, Cephalexin0

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Number of Participants With Development of an Invasive Infection Through the EFV Visit in the Per Protocol Population

Participants were evaluated for invasive infection, which included, but was not limited to, findings of severe sepsis/septic shock, endocarditis, pneumonia, necrotizing soft tissue, osteomyelitis, and bacteremia. A positive response to at least one finding was considered invasive infection for this outcome measure. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo2
Abscess, TMP/SMX2
Infected Wound, TMP/SMX0
Infected Wound, Clindamycin0
Cellulitis, Cephalexin and TMP/SMX1
Cellulitis, Cephalexin0

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Number of Participants With Development of an Invasive Infection Through the TOC Visit in the Intent to Treat Population

Participants were evaluated for invasive infection, which included, but was not limited to, findings of severe sepsis/septic shock, endocarditis, pneumonia, necrotizing soft tissue, osteomyelitis, and bacteremia. A positive response to at least one finding was considered invasive infection for this outcome measure. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo1
Abscess, TMP/SMX1
Infected Wound, TMP/SMX0
Infected Wound, Clindamycin0
Cellulitis, Cephalexin and TMP/SMX0
Cellulitis, Cephalexin0

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Number of Participants Reporting 1-14 Days of Analgesic Use in the Intent to Treat Population

As a quality of life measure, participants maintained a memory aid from Day 1 to Day 14 to track measures such as use of other, non-study medications such as analgesics. Each participant is summarized by the last day of reported analgesic usage, from the start of treatment with study intervention. The maximum number of days assessed, 14, was assigned to participants who were still taking analgesic medications by the end of the assessment period. (NCT00729937)
Timeframe: Day 1 through 14

,,,,,
Interventionparticipants (Number)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14
Abscess, Placebo58384547273427342414191915146
Abscess, TMP/SMX8134643442293240261510145127
Cellulitis, Cephalexin2861013422866426345
Cellulitis, Cephalexin and TMP/SMX187151610109109531251
Infected Wound, Clindamycin3710241091312119443750
Infected Wound, TMP/SMX321518169131384624259

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Number of Participants With Infections in Household Contacts Through the EFV Visit in the Intent to Treat Population

At each follow-up visit, participants were asked about history of skin infections in household members (e.g., similar skin infection in a family member). This outcome measure relied solely on participant reporting. Participants who reported having a family member with a similar infection though the extended follow-up visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo35
Abscess, TMP/SMX25
Infected Wound, TMP/SMX6
Infected Wound, Clindamycin11
Cellulitis, Cephalexin and TMP/SMX11
Cellulitis, Cephalexin5

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Number of Participants With Infections in Household Contacts Through the EFV Visit in the Per Protocol Population

At each follow-up visit, participants were asked about history of skin infections in household members (e.g., similar skin infection in a family member). This outcome measure relied solely on participant reporting. Participants who reported having a family member with a similar infection though the extended follow-up visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 49-63

Interventionparticipants (Number)
Abscess, Placebo33
Abscess, TMP/SMX20
Infected Wound, TMP/SMX6
Infected Wound, Clindamycin9
Cellulitis, Cephalexin and TMP/SMX10
Cellulitis, Cephalexin5

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Number of Participants With Infections in Household Contacts Through the TOC Visit in the Intent to Treat Population

At each follow-up visit, participants were asked about history of skin infections in household members (e.g., similar skin infection in a family member). This outcome measure relied solely on participant reporting. Participants who reported having a family member with a similar infection though the test-of-cure visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo22
Abscess, TMP/SMX12
Infected Wound, TMP/SMX1
Infected Wound, Clindamycin6
Cellulitis, Cephalexin and TMP/SMX7
Cellulitis, Cephalexin4

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Number of Participants With Infections in Household Contacts Through the TOC Visit in the Per Protocol Population

At each follow-up visit, participants were asked about history of skin infections in household members (e.g., similar skin infection in a family member). This outcome measure relied solely on participant reporting. Participants who reported having a family member with a similar infection though the test-of-cure visit are summarized. (NCT00729937)
Timeframe: Day 1 through Day 14-21

Interventionparticipants (Number)
Abscess, Placebo22
Abscess, TMP/SMX9
Infected Wound, TMP/SMX1
Infected Wound, Clindamycin5
Cellulitis, Cephalexin and TMP/SMX6
Cellulitis, Cephalexin4

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Number of Participants by Composite Clinical Outcome at the TOC Visit in the Per Protocol Population

Participants were categorized as composite clinical cure if they had resolution of all symptoms/signs of infection, or improvement to such an extent that no additional antibiotic therapy and/or surgical procedures were necessary. Participants were categorized as composite clinical failure if they had lack of resolution of all signs and symptoms of infection to such an extent that further antibiotic therapy and/or surgical procedures were necessary. (NCT00729937)
Timeframe: Day 14-21

,,,,,
Interventionparticipants (Number)
Composite Clinical CureComposite Clinical Failure
Abscess, Placebo396137
Abscess, TMP/SMX45371
Cellulitis, Cephalexin14944
Cellulitis, Cephalexin and TMP/SMX16058
Infected Wound, Clindamycin11489
Infected Wound, TMP/SMX11385

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Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the End-of-therapy Visit in the Intent to Treat Population

The area of erythema was measured in square centimeters at baseline and at the end-of-therapy visit. For each subject, the change in area was calculated as the area at end-of-therapy subtracted from the area at baseline. The change in area was then divided by the original area to determine the proportional change. Participants were then categorized by reductions in 5% intervals, with participants whose erythema did not change or increased categorized as no reduction. (NCT00729937)
Timeframe: Day 1 to Day 8-10

,,,,,
Interventionparticipants (Number)
No reduction>0%-5% reduction>5%-10% reduction>10%-15% reduction>15%-20% reduction>20%-25% reduction>25%-30% reduction>30%-35% reduction>35%-40% reduction>40%-45% reduction>45%-50% reduction>50%-55% reduction>55%-60% reduction>60%-65% reduction>65%-70% reduction>70%-75% reduction>75%-80% reduction>80%-85% reduction>85%-90% reduction>90%-95% reduction>95%-100% reduction
Abscess, Placebo50100020202402436479531
Abscess, TMP/SMX30010011130150322597532
Cellulitis, Cephalexin50010011010222322267188
Cellulitis, Cephalexin and TMP/SMX50100101100015253042198
Infected Wound, Clindamycin30010000001112121442208
Infected Wound, TMP/SMX30010110031213232125197

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Number of Participants Reporting 1-14 Days of Analgesic Use in the Per Protocol Population

As a quality of life measure, participants maintained a memory aid from Day 1 to Day 14 to track measures such as use of other, non-study medications such as analgesics. Each participant is summarized by the last day of reported analgesic usage, from the start of treatment with study intervention. The maximum number of days assessed, 14, was assigned to participants who were still taking analgesic medications by the end of the assessment period. (NCT00729937)
Timeframe: Day 1 through 14

,,,,,
Interventionparticipants (Number)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14
Abscess, Placebo44374139242924312212161812130
Abscess, TMP/SMX5632493240272735211310123107
Cellulitis, Cephalexin17577419654316238
Cellulitis, Cephalexin and TMP/SMX147131599999431245
Infected Wound, Clindamycin29918991112107441640
Infected Wound, TMP/SMX231117147101073524246

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Number of Participants With Adverse Events Considered Associated With the Study Product by MedDRA System Organ Class

All adverse events were recorded through the test of cure visit; serious adverse events and new and recurrent skin infections were recorded though the extended follow-up visit. All AEs were assessed for association with the study product by a clinician and were considered associated with study product if the event was temporally related to the administration of the study product and no other etiology more likely explains the event. Associated adverse events are summarized by MedDRA System Organ Class. (NCT00729937)
Timeframe: Day 1 through Day 49-63

,,,,,
Interventionparticipants (Number)
Cardiac disordersEye disordersGastrointestinal disordersGeneral disorders and administration site conditioInfections and infestationsInjury, poisoning and procedural complicationsInvestigationsMetabolism and nutrition disordersMusculoskeletal and connective tissue disordersNervous system disordersPsychiatric disordersRenal and urinary disordersReproductive system and breast disordersRespiratory, thoracic and mediastinal disordersSkin and subcutaneous tissue disordersVascular disorders
Abscess, Placebo03164651173380213102
Abscess, TMP/SMX0119811400113441000140
Cellulitis, Cephalexin007321000020000070
Cellulitis, Cephalexin and TMP/SMX0087210030160110150
Infected Wound, Clindamycin109311004015001060
Infected Wound, TMP/SMX008231012016010050

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Number of Participants With Clinical Cure as of the Test-of-Cure (TOC) Visit in the Per Protocol Population

Clinical cure at TOC was defined as no failure on any previous visit up through the TOC, absence of fever, and resolution or minimal presence of all the following signs and symptoms from baseline based on clinician assessment of erythema, swelling, and tenderness. A participant would have been a clinical failure at the On Therapy (OTV) visit with presence of fever attributable to the infection being studied, increase in erythema by 25% or more, or worsening of both swelling and tenderness based on clinical assessment. A participant would have been a clinical failure at the End of Therapy (EOT) visit with presence of fever attributable to the infection being studied, increase or no improvement in erythema, or no improvement in either swelling or tenderness based on clinical assessment. (NCT00729937)
Timeframe: Days 14-21

,,,,,
Interventionparticipants (Number)
Clinical CureClinical Failure
Abscess, Placebo45776
Abscess, TMP/SMX48737
Cellulitis, Cephalexin16528
Cellulitis, Cephalexin and TMP/SMX18236
Infected Wound, Clindamycin18716
Infected Wound, TMP/SMX18216

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Number of Participants With Clinical Cure as of the TOC Visit in the Intent to Treat Population

Clinical cure at TOC was defined as no failure on any previous visit up through the TOC, absence of fever, and resolution or minimal presence of all the following signs and symptoms from baseline based on clinician assessment of erythema, swelling, and tenderness. A participant would have been a clinical failure at the On Therapy (OTV) visit with presence of fever attributable to the infection being studied, increase in erythema by 25% or more, or worsening of both swelling and tenderness based on clinical assessment. A participant would have been a clinical failure at the End of Therapy (EOT) visit with presence of fever attributable to the infection being studied, increase or no improvement in erythema, or no improvement in either swelling or tenderness based on clinical assessment. (NCT00729937)
Timeframe: Days 14-21

,,,,,
Interventionparticipants (Number)
Clinical CureClinical Failure
Abscess, Placebo454163
Abscess, TMP/SMX507123
Cellulitis, Cephalexin17177
Cellulitis, Cephalexin and TMP/SMX18959
Infected Wound, Clindamycin19851
Infected Wound, TMP/SMX19753

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Number of Participants With Each Microbiological Outcome at the TOC Visit in the Per Protocol Population

Participants were categorized for the microbiological outcome with Presumed eradication if they were not deemed a clinical failure through TOC. Those who were deemed a clinical failure through the TOC were classified as one of the following: Persistence=persistent growth of a pre-therapy pathogen; New infection=growth of a new pathogen and eradication of initial pathogen; Super-infection=growth of a new pathogen in addition to persistent growth of pre-therapy pathogen; Unclassified=no specimen for culture or growth of a pathogen in subsequent culture specimen of cellulitis participants, or for whom initial culture specimens were negative or were not obtained for infected wound and abscess participants; or Indeterminate=not meeting any one of the above microbiologic outcome criteria. (NCT00729937)
Timeframe: Day 14-21

,,,,,
Interventionparticipants (Number)
Presumed eradicationPersistenceNew infectionSuper-infectionUnclassifiedIndeterminate
Abscess, Placebo4573918280
Abscess, TMP/SMX4871504180
Cellulitis, Cephalexin1650001117
Cellulitis, Cephalexin and TMP/SMX1820001323
Infected Wound, Clindamycin18761090
Infected Wound, TMP/SMX18252090

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Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the End-of-therapy Visit in the Per Protocol Population

The area of erythema was measured in square centimeters at baseline and at the end-of-therapy visit. For each subject, the change in area was calculated as the area at end-of-therapy subtracted from the area at baseline. The change in area was then divided by the original area to determine the proportional change. Participants were then categorized by reductions in 5% intervals, with participants whose erythema did not change or increased categorized as no reduction. (NCT00729937)
Timeframe: Day 1 to Day 8-10

,,,,,
Interventionparticipants (Number)
No reduction>0%-5% reduction>5%-10% reduction>10%-15% reduction>15%-20% reduction>20%-25% reduction>25%-30% reduction>30%-35% reduction>35%-40% reduction>40%-45% reduction>45%-50% reduction>50%-55% reduction>55%-60% reduction>60%-65% reduction>65%-70% reduction>70%-75% reduction>75%-80% reduction>80%-85% reduction>85%-90% reduction>90%-95% reduction>95%-100% reduction
Abscess, Placebo40100020202401436479478
Abscess, TMP/SMX30010011130150322577478
Cellulitis, Cephalexin50000011010221222144162
Cellulitis, Cephalexin and TMP/SMX50100101100015252041183
Infected Wound, Clindamycin30000000001112101341182
Infected Wound, TMP/SMX30010010021213232113167

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Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the On-therapy Visit in the Intent to Treat Population

The area of erythema was measured in square centimeters at baseline and at the on-therapy visit. For each subject, the change in area was calculated as the area at on-therapy subtracted from the area at baseline. The change in area was then divided by the original area to determine the proportional change. Participants were then categorized by reductions in 5% intervals, with participants whose erythema did not change or increased categorized as no reduction. (NCT00729937)
Timeframe: Day 1 to Day 3-4

,,,,,
Interventionparticipants (Number)
No reduction>0%-5% reduction>5%-10% reduction>10%-15% reduction>15%-20% reduction>20%-25% reduction>25%-30% reduction>30%-35% reduction>35%-40% reduction>40%-45% reduction>45%-50% reduction>50%-55% reduction>55%-60% reduction>60%-65% reduction>65%-70% reduction>70%-75% reduction>75%-80% reduction>80%-85% reduction>85%-90% reduction>90%-95% reduction>95%-100% reduction
Abscess, Placebo67323271213122013141215211817202015298
Abscess, TMP/SMX43243756815171571124102022201616328
Cellulitis, Cephalexin412102537661098496869880
Cellulitis, Cephalexin and TMP/SMX34165545469549167119116674
Infected Wound, Clindamycin181145346476827691731111108
Infected Wound, TMP/SMX121314655386741271011957111

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Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the On-therapy Visit in the Per Protocol Population

The area of erythema was measured in square centimeters at baseline and at the on-therapy visit. For each subject, the change in area was calculated as the area at on-therapy subtracted from the area at baseline. The change in area was then divided by the original area to determine the proportional change. Participants were then categorized by reductions in 5% intervals, with participants whose erythema did not change or increased categorized as no reduction. (NCT00729937)
Timeframe: Day 1 to Day 3-4

,,,,,
Interventionparticipants (Number)
No reduction>0%-5% reduction>5%-10% reduction>10%-15% reduction>15%-20% reduction>20%-25% reduction>25%-30% reduction>30%-35% reduction>35%-40% reduction>40%-45% reduction>45%-50% reduction>50%-55% reduction>55%-60% reduction>60%-65% reduction>65%-70% reduction>70%-75% reduction>75%-80% reduction>80%-85% reduction>85%-90% reduction>90%-95% reduction>95%-100% reduction
Abscess, Placebo59313261113121612131014191413191813262
Abscess, TMP/SMX3724363671315126102191721181316284
Cellulitis, Cephalexin33210243726968375768667
Cellulitis, Cephalexin and TMP/SMX3015534526854915798105571
Infected Wound, Clindamycin1710352353666265716381089
Infected Wound, TMP/SMX111314554375641268684587

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Number of Participants With Reduction in Erythema Dimensions by 5% Intervals at the TOC Visit in the Intent to Treat Population

The area of erythema was measured in square centimeters at baseline and at the TOC visit. For each subject, the change in area was calculated as the area at TOC subtracted from the area at baseline. The change in area was then divided by the original area to determine the proportional change. Participants were then categorized by reductions in 5% intervals, with participants whose erythema did not change or increased categorized as no reduction. (NCT00729937)
Timeframe: Day 1 to Day 14-21

,,,,,
Interventionparticipants (Number)
No reduction>0%-5% reduction>5%-10% reduction>10%-15% reduction>15%-20% reduction>20%-25% reduction>25%-30% reduction>30%-35% reduction>35%-40% reduction>40%-45% reduction>45%-50% reduction>50%-55% reduction>55%-60% reduction>60%-65% reduction>65%-70% reduction>70%-75% reduction>75%-80% reduction>80%-85% reduction>85%-90% reduction>90%-95% reduction>95%-100% reduction
Abscess, Placebo20000000000000002044561
Abscess, TMP/SMX00000100000000001211559
Cellulitis, Cephalexin00100000100000011000217
Cellulitis, Cephalexin and TMP/SMX20000000010000121100220
Infected Wound, Clindamycin10000010000000100001219
Infected Wound, TMP/SMX10010010000100110001216

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The Number of Patients Failing Therapy After 72 Hours of Antibiotic Treatment With Oral Cephalexin or Intravenous Cefazolin Plus Oral Probenecid.

(NCT01029782)
Timeframe: 72 hours

InterventionParticipants (Count of Participants)
IV Cefazolin Plus Oral Probenecid and Placebo Cephalexin6
Oral Cephalexin and Saline IV Plus Probenecid Placebo4

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Number of Participants With Presence of Wound Infection

Hand lacerations will be examined 10-14 days after initial wound closure and will be assessed for presence of infection. (NCT01155154)
Timeframe: 2 weeks

Interventionparticipants (Number)
Clindamycin0
Cepahlexin0
Placebo1

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Healthcare Utilization

Questionnaire designed to evaluate healthcare utilization following surgery. Unit of measure will be the number of participants utilizing each category of healthcare. (NCT01561703)
Timeframe: 6 wks post-operative appointment

,
Interventionparticipants (Number)
Reported FeverMade a phone call to clinicER/UR/Clinic visit"Received additional antibiotic"Diagnostic workup at ER
Control168966
Intervention55200

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Comparison of the Number of Subjects With Asymptomatic Bacteriuria Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population.

"Asymptomatic Bacteriuria is defined in any SCOUT subject by:~Absence of symptoms attributable to UTI including fever AND/OR the following:~Symptoms for all children (ages two months to 10 years):~fever (a documented temperature of at least 100.4 °F OR 38°C measured anywhere on the body)~dysuria~Additional symptoms for children > 2 years of age:~suprapubic, abdominal, or flank pain or tenderness OR~urinary urgency, frequency, or hesitancy (defined as an increase in these symptoms from pre-diagnosis conditions)~Additional symptoms for children = 2 months to 2 years of age:~poor feeding OR~vomiting AND~A positive urine culture~5 x 104 CFU/mL (catheterized or suprapubic aspiration urine specimen) OR~>105 CFU/mL (clean void specimen)." (NCT01595529)
Timeframe: Day 11 through Day 14

InterventionParticipants (Count of Participants)
Standard Course Treatment11
Short Course Treatment29

[back to top]

Comparison of Efficacy Based on Symptomatic Urinary Tract Infection (UTI) Between Short-course and Standard-course of Antibiotics.

"A subject will be categorized as a treatment failure, if he/she has a symptomatic UTI in period between Day 6 through the Day 11 - 14 Test of Cure (TOC) Visit:~Symptoms~Symptoms for all subjects (ages two months to 10 years): fever (a documented temperature of at least 100.4 °F OR 38°C measured anywhere on the body) ,dysuria~Additional symptoms for subjects > 2 years of age: suprapubic, abdominal, or flank pain or tenderness OR urinary urgency, frequency, or hesitancy (defined as an increase in these symptoms from pre-diagnosis conditions)~Additional symptoms for subjects = 2 months to 2 years of age: poor feeding OR vomiting AND~Pyuria on urinalysis AND~Culture proven infection with a single uropathogen NOTE: As per the above criteria, asymptomatic subjects (including subjects assessed as having asymptomatic bacteriuria) at the Day 11-14 TOC visit will NOT be considered a treatment failure for the primary outcome measure." (NCT01595529)
Timeframe: Day 11 through Day 14

InterventionParticipants (Count of Participants)
Standard Course Treatment2
Short Course Treatment14

[back to top]

Comparison of Efficacy Based on Symptomatic Urinary Tract Infection (UTI) Between Short-course and Standard-course of Antibiotics. Per-protocol Population.

"A subject will be categorized as a treatment failure, if he/she has a symptomatic UTI in period between Day 6 through the Day 11 - 14 Test of Cure (TOC) Visit:~Symptoms~Symptoms for all subjects (ages two months to 10 years): fever (a documented temperature of at least 100.4 °F OR 38°C measured anywhere on the body) ,dysuria~Additional symptoms for subjects > 2 years of age: suprapubic, abdominal, or flank pain or tenderness OR urinary urgency, frequency, or hesitancy (defined as an increase in these symptoms from pre-diagnosis conditions)~Additional symptoms for subjects = 2 months to 2 years of age: poor feeding OR vomiting AND~Pyuria on urinalysis AND~Culture proven infection with a single uropathogen NOTE: As per the above criteria, asymptomatic subjects (including subjects assessed as having asymptomatic bacteriuria) at the Day 11-14 TOC visit will NOT be considered a treatment failure for the primary outcome measure." (NCT01595529)
Timeframe: Day 11 through Day 14

InterventionParticipants (Count of Participants)
Standard Course Treatment2
Short Course Treatment9

[back to top]

Comparison of Number of Subjects That Have a Recurrent Infection (Includes a Relapse UTI or a Reinfection) Following Short-course Versus Standard-course of Antibiotics.

(NCT01595529)
Timeframe: Day 11 through Day 44

InterventionParticipants (Count of Participants)
Standard Course Treatment12
Short Course Treatment13

[back to top]

Comparison of Number of Subjects That Have a Recurrent Infection (Includes a Relapse UTI or a Reinfection) Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population.

(NCT01595529)
Timeframe: Day 11 through Day 44

InterventionParticipants (Count of Participants)
Standard Course Treatment10
Short Course Treatment13

[back to top]

Comparison of the Number of Subjects With Asymptomatic Bacteriuria Following Short-course Versus Standard-course of Antibiotics.

"Asymptomatic Bacteriuria is defined in any SCOUT subject by:~Absence of symptoms attributable to UTI including fever AND/OR the following:~Symptoms for all children (ages two months to 10 years):~fever (a documented temperature of at least 100.4 °F OR 38°C measured anywhere on the body)~dysuria~Additional symptoms for children > 2 years of age:~suprapubic, abdominal, or flank pain or tenderness OR~urinary urgency, frequency, or hesitancy (defined as an increase in these symptoms from pre-diagnosis conditions)~Additional symptoms for children = 2 months to 2 years of age:~poor feeding OR~vomiting AND~A positive urine culture~5 x 104 CFU/mL (catheterized or suprapubic aspiration urine specimen) OR~>105 CFU/mL (clean void specimen)." (NCT01595529)
Timeframe: Day 11 through Day 14

InterventionParticipants (Count of Participants)
Standard Course Treatment11
Short Course Treatment29

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Comparison of the Number of Subjects With Positive Urine Cultures Following Short-course Versus Standard-course of Antibiotics.

(NCT01595529)
Timeframe: Up to Day 14

InterventionParticipants (Count of Participants)
Standard Course Treatment6
Short Course Treatment41

[back to top]

Comparison of the Number of Subjects With Positive Urine Cultures Following Short-course Versus Standard-course of Antibiotics. Per-protocol Population.

(NCT01595529)
Timeframe: Up to Day 14

InterventionParticipants (Count of Participants)
Standard Course Treatment6
Short Course Treatment35

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Comparison of the Number of Subjects That Become Colonized With Antimicrobial Resistant E. Coli and K. Pneumoniae in the Gastrointestinal Tract Following Short-course Versus Standard Course of Antibiotics. Per-protocol Population.

"A child would have emergent antibiotic resistance if they:~Had no antibiotic-resistant E.coli or K.pneumoniae at enrollment but one or both are now present. OR~Had either antibiotic-resistant E.coli or K.pneumoniae at enrollment but now the other antibiotic-resistant organism is present OR~Had antibiotic-resistant E.coli and/or K.pneumoniae at enrollment, but have now developed resistance to new antibiotics in either organism." (NCT01595529)
Timeframe: Day 11 through Day 30

,
InterventionParticipants (Count of Participants)
Test of Cure Visit (Day 11-14)Outcome Assessment Visit (Day 24-30)
Short Course Treatment2823
Standard Course Treatment2223

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Comparison of the Number of Subjects That Become Colonized With Antimicrobial Resistant Escherichia Coli (E. Coli) and Klebsiella Pneumoniae (K. Pneumoniae) in the Gastrointestinal Tract Following Short-course Versus Standard Course of Antibiotics.

"A child would have emergent antibiotic resistance if they:~Had no antibiotic-resistant E.coli or K.pneumoniae at enrollment but one or both are now present. OR~Had either antibiotic-resistant E.coli or K.pneumoniae at enrollment but now the other antibiotic-resistant organism is present OR~Had antibiotic-resistant E.coli and/or K.pneumoniae at enrollment, but have now developed resistance to new antibiotics in either organism." (NCT01595529)
Timeframe: Day 11 through Day 30

,
InterventionParticipants (Count of Participants)
Test of Cure Visit (Day 11-14)Outcome Assessment Visit (Day 24-30)
Short Course Treatment3128
Standard Course Treatment2223

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Apparent Total Systemic Clearance After Single or Multiple Extravascular Dosing (CL/F) of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

InterventionL/h (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase9.71310.58

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Apparent Volume of Distribution During the Terminal Elimination Phase After Single Extravascular Dosing (Vz/F) of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

Interventionliters (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase24.0725.86

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Area Under the Concentration-time Curve From the Time of Dosing Extrapolated to Time Infinity (AUCinf) of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

Interventionng*h/mL (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase5765051873

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Area Under the Concentration-time Curve From the Time of Dosing to the Last Measurable Concentration (AUClast) After Single and Multiple Doses of Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -2 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose

,,,,,,
Interventionng*h/mL (Mean)
Day -2Cycle 1 day -15
Gilteritinib 120 mg in Escalation Phase24806943
Gilteritinib 20 mg in Escalation Phase303.01030
Gilteritinib 200 mg in Escalation Phase302432248
Gilteritinib 300 mg in Escalation Phase418131749
Gilteritinib 40 mg in Escalation Phase360.41990
Gilteritinib 450 mg in Escalation Phase254435506
Gilteritinib 80 mg in Escalation Phase12167111

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Area Under the Concentration-time Curve Over the 24-Hour Dosing Interval (AUC24) After Single and Multiple Doses of Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -2 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose

,,,,,,
Interventionng*h/mL (Mean)
Day -2Cycle 1 Day 15
Gilteritinib 120 mg in Escalation Phase24806943
Gilteritinib 20 mg in Escalation Phase302.11299
Gilteritinib 200 mg in Escalation Phase302231428
Gilteritinib 300 mg in Escalation Phase416331005
Gilteritinib 40 mg in Escalation Phase360.02482
Gilteritinib 450 mg in Escalation Phase332434768
Gilteritinib 80 mg in Escalation Phase12166958

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AUC24 of Metabolite 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionng*h/mL (Mean)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase20.4423.10

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AUC24 of Midazolam Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionng*h/mL (Mean)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase66.5581.56

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AUClast of 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionng*h/mL (Mean)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase17.0523.58

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AUClast of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

Interventionng*h/mL (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase5318354963

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AUClast of Midazolam Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionng*h/mL (Mean)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase59.4882.44

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Cmax of 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionng/mL (Mean)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase4.5625.053

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Cmax of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

Interventionng/mL (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 day 15)
Gilteritinib 200 mg in Expansion Phase1768816075

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Cmax of Midazolam Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionng/mL (Mean)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase14.6818.45

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Duration of CR (DCR)

DCR was defined as the time from the date of first CR until the date of documented relapse for participants who achieved CR. Participants who died without report of relapse were considered non-events and censored at their last relapse-free disease assessment date. Other participants who did not relapse on study were considered non-events and censored at the last relapse-free disease assessment date. DCR was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
FLT3 Mutation NegativeAll Participants
Gilteritinib 20 mgNANA

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Duration of CR (DCR)

DCR was defined as the time from the date of first CR until the date of documented relapse for participants who achieved CR. Participants who died without report of relapse were considered non-events and censored at their last relapse-free disease assessment date. Other participants who did not relapse on study were considered non-events and censored at the last relapse-free disease assessment date. DCR was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 120 mgNANA
Gilteritinib 200 mg419.0419.0
Gilteritinib 300 mgNANA
Gilteritinib 80 mgNANA

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Duration of CRc (DCRc)

DCRc was defined as the time from the date of first CRc until the date of documented relapse for participants who achieved CRc. Participants who died without report of relapse and participants who did not relapse were considered non-events and censored at the last relapse-free disease assessment date. DCRc was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 300 mgNANA

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Duration of CRc (DCRc)

DCRc was defined as the time from the date of first CRc until the date of documented relapse for participants who achieved CRc. Participants who died without report of relapse and participants who did not relapse were considered non-events and censored at the last relapse-free disease assessment date. DCRc was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg98.099.099.0
Gilteritinib 20 mgNANANA
Gilteritinib 200 mg191.0NA191.0
Gilteritinib 80 mgNA41.079.0

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Duration of CRi (DCRi)

DCRi was defined as the time from the date of first CRi until the date of documented relapse for participants who achieved CRi. Participants who died without report of relapse and participants who did not relapse were considered non-events and censored at the last relapse-free disease assessment date. DCRi was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 20 mgNANA
Gilteritinib 200 mg191.0191.0
Gilteritinib 300 mgNANA

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Duration of CRi (DCRi)

DCRi was defined as the time from the date of first CRi until the date of documented relapse for participants who achieved CRi. Participants who died without report of relapse and participants who did not relapse were considered non-events and censored at the last relapse-free disease assessment date. DCRi was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg120.099.0120.0
Gilteritinib 80 mgNA41.079.0

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Duration of CRp (DCRp)

DCRp was defined as the time from the date of first CRp until the date of documented relapse for participants who achieved CRp. Participants who died without report of relapse were considered non-events and censored at their last relapse-free disease assessment date. Other participants who did not relapse on study were considered non-events and censored at the last relapse-free disease assessment date. DCRp was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 120 mgNANA
Gilteritinib 200 mg450.0450.0
Gilteritinib 300 mgNANA
Gilteritinib 80 mgNANA

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Duration of Response

Duration of response was defined as the time from the date of either first CRc or PR until the date of documented relapse of any type for participants who achieved CRc or PR. Participants who died without report of relapse were considered non-events and censored at their last relapse-free disease assessment date. Other participants who did not relapse on study are considered non-events and censored at the last relapse-free assessment date. Duration of response was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 300 mg59.059.0
Gilteritinib 40 mgNANA
Gilteritinib 450 mgNANA

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Duration of Response

Duration of response was defined as the time from the date of either first CRc or PR until the date of documented relapse of any type for participants who achieved CRc or PR. Participants who died without report of relapse were considered non-events and censored at their last relapse-free disease assessment date. Other participants who did not relapse on study are considered non-events and censored at the last relapse-free assessment date. Duration of response was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg141.0109.5126.0
Gilteritinib 20 mgNANANA
Gilteritinib 200 mg220.085.0220.0
Gilteritinib 80 mg88.041.079.0

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Event Free Survival (EFS)

"EFS was defined as the time from the date of first dose of study drug until the date of documented relapse, treatment failure or death from any cause, whichever occurred first. For a participant with none of these events, EFS was censored at the date of last relapse-free disease assessment. A participant without post-treatment disease assessment was censored at randomization date. Treatment failure included those participants who discontinued the treatment due to progressive disease or lack of efficacy without a previous response of CR, CRp, CRi or PR. Treatment failure date referred to the start of new anti-leukemia therapy or the last treatment evaluation date when new anti-leukemia therapy date was not available. For participants who were censored, last relapse-free disease assessment date referred to the participant's last disease assessment date. EFS was calculated using Kaplan-Meier method and therefore data are estimated." (NCT02014558)
Timeframe: From first dose of study drug up to end of study (median time on study was 157.0 days, minimum of 5 days and maximum of 1320 days)

,,,,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg112.085.5108.0
Gilteritinib 20 mg52.058.058.0
Gilteritinib 200 mg121.045.0118.0
Gilteritinib 300 mg85.043.065.0
Gilteritinib 40 mg109.039.055.5
Gilteritinib 450 mg86.071.071.0
Gilteritinib 80 mg93.574.076.0

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Fraction of Drug Excreted Into Urine in Percentage (%Ae) of Cephalexin Administered With and Without Gilteritinib

Urine samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: 0-3 hours, 3-6 hours, 6-24 hours postdose (cephalexin)

Interventionpercentage (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase109.889.75

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Leukemia Free Survival (LFS)

LFS was defined as the time from the date of first CRc until the date of documented relapse or death for participants who achieved CRc. For a participant who was not known to have relapsed or died, LFS was censored on the date of last relapse-free disease assessment date. LFS was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From first dose of study drug up to end of study (median time on study was 157.0 days, minimum of 5 days and maximum of 1320 days)

Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 300 mg296.0296.0

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Leukemia Free Survival (LFS)

LFS was defined as the time from the date of first CRc until the date of documented relapse or death for participants who achieved CRc. For a participant who was not known to have relapsed or died, LFS was censored on the date of last relapse-free disease assessment date. LFS was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From first dose of study drug up to end of study (median time on study was 157.0 days, minimum of 5 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg98.099.098.0
Gilteritinib 20 mg242.0NA242.0
Gilteritinib 200 mg146.038.0146.0
Gilteritinib 80 mg98.041.079.0

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Maximum Concentration (Cmax) After Single and Multiple Doses of Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -2 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose

,,,,,,
Interventionng/mL (Mean)
Day -2Cycle 1 day 15
Gilteritinib 120 mg in Escalation Phase136.7374.2
Gilteritinib 20 mg in Escalation Phase28.1364.64
Gilteritinib 200 mg in Escalation Phase168.21462
Gilteritinib 300 mg in Escalation Phase204.31525
Gilteritinib 40 mg in Escalation Phase24.98107.6
Gilteritinib 450 mg in Escalation Phase207.61528
Gilteritinib 80 mg in Escalation Phase75.29376.4

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Number of Participants With Adverse Events (AEs)

Safety was assessed by AEs, which included abnormalities identified during a medical test (e.g. laboratory tests, vital signs, electrocardiogram, etc.) if the abnormality induced clinical signs or symptoms, needed active intervention, interruption or discontinuation of study medication or was clinically significant. A treatment-emergent AE (TEAE) was defined as an AE observed after starting administration of the study drug up to 30 days after last dose of study drug (for participants who underwent hematopoietic stem cell transplantation [HSCT]: defined as AEs observed after starting study drug until the last dose before on study HSCT plus 30 days, and AEs that began after resumption of gilteritinib and within 30 days after the last dose of gilteritinib). AEs were graded using the National Cancer Institute Common Terminology Criteria for Adverse Events Version 4.03 (1-Mild, 2-Moderate, 3-Severe, 4-LifeThreatening, 5-Death). (NCT02014558)
Timeframe: From first dose of study drug up to 30 days after last dose of study drug (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
AEsDrug-Related AEsDeathsSerious AEsDrug-Related Serious AEsAEs Leading to Discontinuation of Study DrugDrug-Related AEs Leading to Discont. of Study DrugGrade 3 or Higher TEAEsAEs During On-Study HSCT PeriodSerious AEs During On-Study HSCT
Gilteritinib 120 mg in Escalation Phase3311100100
Gilteritinib 120 mg in Expansion Phase64522352191255930
Gilteritinib 20 mg in Escalation Phase5322020300
Gilteritinib 20 mg in Expansion Phase12738221900
Gilteritinib 200 mg in Escalation Phase3312110200
Gilteritinib 200 mg in Expansion Phase1007749923646109973
Gilteritinib 300 mg in Escalation Phase3212000200
Gilteritinib 300 mg in Expansion Phase17137144631400
Gilteritinib 40 mg in Escalation Phase3222000200
Gilteritinib 40 mg in Expansion Phase1364121511300
Gilteritinib 450 mg in Escalation Phase3312210300
Gilteritinib 80 mg in Escalation Phase3102010200
Gilteritinib 80 mg in Expansion Phase20171119101142000

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Number of Participants With Dose Limiting Toxicities (DLTs)

To determine the maximum tolerated dose, safety was assessed by DLTs, defined as any grade ≥ 3 non-hematologic or extramedullary toxicity that occurred within 30 days starting with the first dose taken on day -2, and included the first treatment cycle in the dose escalation phase and in the first treatment cycle (28 days) in the dose expansion phase, that was considered to be possibly or probably related to study drug. Exceptions to this were the following: (1) Alopecia, anorexia or fatigue, (2) Grade 3 nausea and/or vomiting if not required tube feeding or total parenteral nutrition, or diarrhea if not required or prolonged hospitalization that was managed to grade ≤ 2 with standard antiemetic or antidiarrheal medications used at prescribed dose within 7 days of onset, (3) Grade 3 fever with neutropenia, with or without infection, (4) Grade 3 infection. (NCT02014558)
Timeframe: From first dose up to end of cycle 1 (30 days)

,,,,,,,,,,,,
InterventionParticipants (Count of Participants)
Any DLTBlood and lymphatic system disordersCardiac disordersEye disordersGastrointestinal disordersGeneral disorders & administration site conditionsHepatobiliary disordersInfections and infestationsInvestigationsMetabolism and nutrition disordersMusculoskeletal and connective tissue disordersNervous system disordersRenal and urinary disordersReproductive system and breast disordersRespiratory, thoracic and mediastinal disordersVascular disorders
Gilteritinib 120 mg in Escalation Phase0000000000000000
Gilteritinib 120 mg in Expansion Phase7010101020001010
Gilteritinib 20 mg in Escalation Phase0000000000000000
Gilteritinib 20 mg in Expansion Phase1000000000010000
Gilteritinib 200 mg in Escalation Phase0000000000000000
Gilteritinib 200 mg in Expansion Phase15000410062130122
Gilteritinib 300 mg in Escalation Phase0000000000000000
Gilteritinib 300 mg in Expansion Phase3100100020100011
Gilteritinib 40 mg in Escalation Phase0000000000000000
Gilteritinib 40 mg in Expansion Phase1000000100000000
Gilteritinib 450 mg in Escalation Phase2000100010000000
Gilteritinib 80 mg in Escalation Phase0000000000000000
Gilteritinib 80 mg in Expansion Phase2001000100000000

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Overall Survival (OS)

The time from the date of first dose of study drug until the date of death from any cause. For a participant who was not known to have died by the end of study follow-up, OS was censored at the date of last contact. OS was calculated using Kaplan-Meier method and therefore data are estimated. (NCT02014558)
Timeframe: From first dose of study drug up to end of study (median time on study was 157.0 days, minimum of 5 days and maximum of 1320 days)

,,,,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg246.0144.0216.0
Gilteritinib 20 mg123.0NA149.5
Gilteritinib 200 mg214.067.0176.0
Gilteritinib 300 mg157.068.0128.5
Gilteritinib 40 mg199.571.595.0
Gilteritinib 450 mg204.089.089.0
Gilteritinib 80 mg197.5136.0154.0

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Percentage of Participants Who Achieved Transfusion Conversion

Participants who achieved transfusion conversion were defined as the number of participants who were transfusion dependent at baseline period but became transfusion independent at post-baseline period divided by the total number of participants who were transfusion dependent at baseline period. Participants were considered baseline transfusion dependent if there were RBC or platelet transfusions within the baseline period. Participants were considered post-baseline transfusion independent if they were on treatment >=84 days, and if there was one consecutive 56 days without any RBC or platelet transfusion within post-baseline period. If participants were on treatment >28 days but <84 days, and there was no RBC or platelet transfusion within post-baseline period, or on treatment <=28 days, post-baseline transfusion status was not evaluable. Exact 95% confidence interval was estimated using the binomial distribution. (NCT02014558)
Timeframe: Baseline (28 days prior to first dose until 28 days after the first dose) and postbaseline (from 29 days after first dose date until last dose date); median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg27.522.226.5
Gilteritinib 20 mg0NANA
Gilteritinib 200 mg40.433.339.7
Gilteritinib 300 mgNANANA
Gilteritinib 40 mg0NANA
Gilteritinib 450 mgNANANA
Gilteritinib 80 mg37.512.525.0

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Percentage of Participants Who Achieved Transfusion Maintenance

Participants who achieved transfusion maintenance were defined as the number of participants who were transfusion independent at baseline period and still maintained transfusion independent at post-baseline period divided by the total number of participants who were transfusion independent at baseline period. (NCT02014558)
Timeframe: Baseline (28 days prior to first dose until 28 days after the first dose) and postbaseline (from 29 days after first dose date until last dose date); median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days

,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveAll Participants
Gilteritinib 200 mg80.080.0
Gilteritinib 450 mg100.0100.0
Gilteritinib 80 mg100.0100.0

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Percentage of Participants Who Achieved Transfusion Maintenance

Participants who achieved transfusion maintenance were defined as the number of participants who were transfusion independent at baseline period and still maintained transfusion independent at post-baseline period divided by the total number of participants who were transfusion independent at baseline period. (NCT02014558)
Timeframe: Baseline (28 days prior to first dose until 28 days after the first dose) and postbaseline (from 29 days after first dose date until last dose date); median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days

Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg75.033.357.1

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Percentage of Participants With Best Response

Best response was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). BR was defined as the best measured response for all visits (in the order of CR, CRp, CRi, and PR) post-treatment. Participants who achieved the best response of CR, CRp, CRi or PR were classified as responders. Participants who did not achieve at least PR were considered as non-responders. Exact 95% confidence interval was estimated using the binomial distribution. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg53.614.345.7
Gilteritinib 20 mg14.350.018.8
Gilteritinib 200 mg48.318.245.0
Gilteritinib 300 mg60.0030.0
Gilteritinib 40 mg37.5018.8
Gilteritinib 450 mg50.0033.3
Gilteritinib 80 mg66.716.741.7

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Percentage of Participants With Complete Remission (CR) During the First 2 Cycles

CR was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in CR when they had bone marrow regenerating normal hematopoietic cells, achieved a morphologic leukemia-free state, had an absolute neutrophil count (ANC) > 1 x 10^9/L, platelet count ≥ 100 x 10^9/L, normal marrow differential with < 5% blasts, had been red blood cell (RBC) and platelet transfusion independent (defined as 1 week without RBC transfusion and 1 week without platelet transfusion), had no presence of Auer rods and no evidence of extramedullary leukemia, and blast counts in peripheral blood had been ≤ 2%. Exact 95% confidence interval was estimated using binomial distribution. (NCT02014558)
Timeframe: During the first 2 cycles (56 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg3.602.9
Gilteritinib 20 mg050.06.3
Gilteritinib 200 mg3.403.0
Gilteritinib 300 mg1005.0
Gilteritinib 40 mg000
Gilteritinib 450 mg000
Gilteritinib 80 mg8.304.2

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Percentage of Participants With Composite CR (CRc)

CRc was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in CRc when they had achieved either CR, complete remission with incomplete platelet recovery (CRp, defined as had achieved CR except for incomplete platelet recovery (< 100 x 10^9/L) or complete remission with incomplete hematologic recovery (CRi, defined as had fulfilled all the criteria for CR except for incomplete hematological recovery with residual neutropenia < 1 x 10^9/L with or without complete platelet recovery; RBC platelet transfusion independence not required). Exact 95% confidence interval was estimated using the binomial distribution. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg46.47.138.6
Gilteritinib 20 mg7.150.012.5
Gilteritinib 200 mg40.49.137.0
Gilteritinib 300 mg30.0015.0
Gilteritinib 40 mg000
Gilteritinib 450 mg000
Gilteritinib 80 mg41.716.729.2

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Percentage of Participants With CR During Treatment

CR was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in CR when they had bone marrow regenerating normal hematopoietic cells, achieved a morphologic leukemia-free state, had an absolute neutrophil count (ANC) > 1 x 10^9/L, platelet count ≥ 100 x 10^9/L, normal marrow differential with < 5% blasts, had been red blood cell (RBC) and platelet transfusion independent (defined as 1 week without RBC transfusion and 1 week without platelet transfusion), had no presence of Auer rods and no evidence of extramedullary leukemia, and blast counts in peripheral blood had been ≤ 2%. Exact 95% confidence interval was estimated using binomial distribution. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg12.5010.0
Gilteritinib 20 mg050.06.3
Gilteritinib 200 mg11.2010.0
Gilteritinib 300 mg10.005.0
Gilteritinib 40 mg000
Gilteritinib 450 mg000
Gilteritinib 80 mg16.708.3

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Percentage of Participants With CR With Incomplete Hematological Recovery (CRi)

CRi was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in CRi when they fulfilled all the criteria for CR except for incomplete hematological recovery with residual neutropenia < 1 x 10^9/L with or without complete platelet recovery. RBC and platelet transfusion independence were not required. Exact 95% confidence interval was estimated using the binomial distribution. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg30.47.125.7
Gilteritinib 20 mg7.106.3
Gilteritinib 200 mg20.29.119.0
Gilteritinib 300 mg10.005.0
Gilteritinib 40 mg000
Gilteritinib 450 mg000
Gilteritinib 80 mg25.016.720.8

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Percentage of Participants With CR With Incomplete Platelet Recovery (CRp)

CRp was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in CRp when they achieved CR except for incomplete platelet recovery (< 100 x 10^9/L). Exact 95% confidence interval was estimated using the binomial distribution. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg3.602.9
Gilteritinib 20 mg000
Gilteritinib 200 mg9.008.0
Gilteritinib 300 mg10.005.0
Gilteritinib 40 mg000
Gilteritinib 450 mg000
Gilteritinib 80 mg000

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Percentage of Participants With Partial Remission (PR)

PR was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in PR when they had bone marrow regenerating normal hematopoietic cells with evidence of peripheral recovery with no (or only a few regenerating) circulating blasts and with a decrease of at least 50% in the percentage of blasts in the bone marrow aspirate with the total marrow blasts between 5% and 25%. A value of less or equal than 5% blasts was also considered a PR if Auer rods were present. There should be no evidence of extramedullary leukemia. Exact 95% confidence interval was estimated using the binomial distribution. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,,,,
Interventionpercentage of participants (Number)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg7.17.17.1
Gilteritinib 20 mg7.106.3
Gilteritinib 200 mg7.99.18.0
Gilteritinib 300 mg30.0015.0
Gilteritinib 40 mg37.5018.8
Gilteritinib 450 mg50.0033.3
Gilteritinib 80 mg25.0012.5

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Renal Clearance (CLr) of Cephalexin in Administered With and Without Gilteritinib

Urine samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: 0-3 hours, 3-6 hours, 6-24 hours postdose (cephalexin)

InterventionL/h (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase8.78411.04

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T1/2 of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

Interventionhours (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase1.8221.827

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Time to Best Response (TTBR)

TTBR was defined as the time from the first dose of study drug until the first disease assessment date when participant achieved best response. TTBR was evaluated in participants who achieved best response of CR, CRp, CRi, or PR. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 300 mg29.029.0
Gilteritinib 40 mg57.057.0
Gilteritinib 450 mg31.031.0

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Time to Best Response (TTBR)

TTBR was defined as the time from the first dose of study drug until the first disease assessment date when participant achieved best response. TTBR was evaluated in participants who achieved best response of CR, CRp, CRi, or PR. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg43.529.530.0
Gilteritinib 20 mg75.530.057.0
Gilteritinib 200 mg57.029.556.0
Gilteritinib 80 mg44.071.558.0

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Time to CR (TTCR)

TTCR was defined as the time from the first dose of study drug until the date of first CR. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
FLT3 Mutation NegativeAll Participants
Gilteritinib 20 mg30.030.0

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Time to CR (TTCR)

TTCR was defined as the time from the first dose of study drug until the date of first CR. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 120 mg141.0141.0
Gilteritinib 200 mg93.093.0
Gilteritinib 300 mg56.056.0
Gilteritinib 80 mg171.5171.5

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Time to CRc (TTCRc)

TTCRc was defined as the time from the first dose of study drug until the date of first CRc. TTCRc was evaluated for participants who achieved CRc. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 300 mg28.028.0

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Time to CRc (TTCRc)

TTCRc was defined as the time from the first dose of study drug until the date of first CRc. TTCRc was evaluated for participants who achieved CRc. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg30.030.030.0
Gilteritinib 20 mg57.030.043.5
Gilteritinib 200 mg31.530.031.0
Gilteritinib 80 mg56.071.557.0

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Time to CRi (TTCRi)

TTCRi was defined as the time from the first dose of study drug until the date of first CRi. TTCRi was evaluated for participants who achieved CRi. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 20 mg57.057.0
Gilteritinib 300 mg28.028.0

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Time to CRi (TTCRi)

TTCRi was defined as the time from the first dose of study drug until the date of first CRi. TTCRi was evaluated for participants who achieved CRi. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg57.030.043.5
Gilteritinib 200 mg39.530.035.0
Gilteritinib 80 mg57.071.564.0

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Time to CRp (TTCRp)

TTCRp was defined as the time from the first dose of study drug until the date of first CRp. TTCRp was evaluated for participants who achieved CRp. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 120 mg195.0195.0
Gilteritinib 200 mg84.584.5
Gilteritinib 300 mg29.029.0
Gilteritinib 80 mg140.0140.0

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Time to Observed Cmax (Tmax) After Single and Multiple Doses of Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -2 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose

,,,,,,
Interventionhours (Median)
Day -2Cycle 1 day 15
Gilteritinib 120 mg in Escalation Phase2.0832.167
Gilteritinib 20 mg in Escalation Phase2.004.008
Gilteritinib 200 mg in Escalation Phase5.2336.033
Gilteritinib 300 mg in Escalation Phase6.0676.050
Gilteritinib 40 mg in Escalation Phase5.9833.867
Gilteritinib 450 mg in Escalation Phase5.7835.933
Gilteritinib 80 mg in Escalation Phase4.0004.333

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Time to Response (TTR)

TTR was defined as the time from the first dose of study drug until the date of either first CRc or PR. TTR was evaluated for participants who achieved CRc or PR. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,
Interventiondays (Median)
FLT3 Mutation PositiveAll Participants
Gilteritinib 300 mg28.028.0
Gilteritinib 40 mg57.057.0
Gilteritinib 450 mg31.031.0

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Time to Response (TTR)

TTR was defined as the time from the first dose of study drug until the date of either first CRc or PR. TTR was evaluated for participants who achieved CRc or PR. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

,,,
Interventiondays (Median)
FLT3 Mutation PositiveFLT3 Mutation NegativeAll Participants
Gilteritinib 120 mg29.029.529.0
Gilteritinib 20 mg61.530.030.0
Gilteritinib 200 mg29.029.529.0
Gilteritinib 80 mg31.071.543.5

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Tmax of 1-Hydroxymidazolam After Administration of Midazolam With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionhours (Median)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase0.55831.00

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Tmax of Cephalexin Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 1.5, 2, 3, 4, 6, 24 hours postdose (cephalexin)

Interventionhours (Median)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase1.5001.483

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Tmax of Midazolam Administered With and Without Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (midazolam)

Interventionhours (Median)
Midazolam Alone (Day -1)Midazolam + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 300 mg in Expansion Phase0.50001.00

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Accumulation Ratio After Multiple Doses of Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose

Interventionratio (Mean)
Gilteritinib 20 mg in Escalation Phase4.259
Gilteritinib 40 mg in Escalation Phase9.640
Gilteritinib 80 mg in Escalation Phase5.693
Gilteritinib 120 mg in Escalation Phase3.290
Gilteritinib 200 mg in Escalation Phase9.041
Gilteritinib 300 mg in Escalation Phase9.057

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AUC24 of Gilteritinib in Co-administration With Voriconazole

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Cycle 1 Day 15 and Cycle 2 Day 1: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (gilteritinib)

Interventionng*h/mL (Mean)
Gilteritinib 20 mg in Expansion Phase919.3

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AUClast of Gilteritinib in Co-administration With Voriconazole

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Cycle 1 Day 15 and Cycle 2 Day 1: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (gilteritinib)

Interventionng*h/mL (Mean)
Gilteritinib 20 mg in Expansion Phase919.3

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Cmax of Gilteritinib in Co-administration With Voriconazole

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Cycle 1 Day 15 and Cycle 2 Day 1: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (gilteritinib)

Interventionng/mL (Mean)
Gilteritinib 20 mg in Expansion Phase63.79

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Duration of CR/CRh (DCRCRh)

DCRCRh was defined as the time from the date of first DCRCRh until the date of documented relapse for participants who achieved CR or CRh. For participants who achieved both CR and CRh, the first CR date or CRh date, whichever occurred first, was used. Participants who died without report of relapse and participants who did not relapse were considered non-events and censored at the last relapse-free disease assessment date. DCRCRh was calculated using Kaplan-Meier method and therefore data are estimated. DCRCRh was calculated only for participants who were FLT3 mutation positive. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
Gilteritinib 20 mgNA
Gilteritinib 80 mgNA
Gilteritinib 120 mg307.0
Gilteritinib 200 mg308.0
Gilteritinib 300 mgNA

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Duration of CRh (DCRh)

DCRh was defined as the time from the date of first CRh until the date of documented relapse for participants who achieved CRh but did not have a best response of CR. Participants who died without report of relapse and participants who did not relapse were considered non-events and censored at the last relapse-free disease assessment date. DCRh was calculated using Kaplan-Meier method and therefore data are estimated. DCRh was calculated only for participants who were FLT3 mutation positive. (NCT02014558)
Timeframe: From date of remission until end of study (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
Gilteritinib 20 mgNA
Gilteritinib 80 mgNA
Gilteritinib 120 mg64.0
Gilteritinib 200 mg101.0
Gilteritinib 300 mgNA

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Percentage of Participants With Complete Remission and Complete Remission With Partial Hematologic Recovery (CR/CRh)

Participants with CR/CRh were defined as participants who achieved either CR or CRh. Participants with CR had bone marrow regenerating normal hematopoietic cells, achieved a morphologic leukemia-free state, had an ANC > 1 x 10^9/L, platelet count ≥ 100 x 10^9/L, and normal marrow differential with < 5% blasts, had been RBC and platelet transfusion independent (defined as 1 week without RBC transfusion and 1 week without platelet transfusion). Also, there had been no presence of Auer rods, no evidence of extramedullary leukemia, and blast counts in peripheral blood had been ≤ 2%. Participants with CRh could not be classified as being in CR and had bone marrow blasts < 5%, partial hematologic recovery ANC >= 0.5 x 10^9/L and platelets >= 50 x 10^9/L. There should not be evidence of extramedullary leukemia. Exact 95% confidence interval was estimated using the binomial distribution. CR/CRh was calculated only for participants who were FLT3 mutation positive. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventionpercentage of participants (Number)
Gilteritinib 20 mg7.1
Gilteritinib 40 mg0
Gilteritinib 80 mg25.0
Gilteritinib 120 mg23.2
Gilteritinib 200 mg19.1
Gilteritinib 300 mg30.0
Gilteritinib 450 mg0

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Percentage of Participants With Complete Remission With Partial Hematologic Recovery (CRh)

CRh was defined according to modified Cheson criteria (2003), using centrally evaluated myeloblast counts from bone marrow aspirate/biopsy assessments and centrally evaluated hematology results; if neither central bone marrow aspirate nor biopsy was available, myeloblast was imputed with locally evaluated bone marrow aspirate/biopsy assessments (derived response). Participants were classified as being in CRh when they could not be classified as being in CR and had bone marrow blasts < 5% and partial hematologic recovery ANC >= 0.5 x 10^9/L and platelets >= 50 x 10^9/L. There should not be evidence of extramedullary leukemia. Exact 95% confidence interval was estimated using the binomial distribution. CRh was calculated only for participants who were FLT3 mutation positive. (NCT02014558)
Timeframe: Up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventionpercentage of participants (Number)
Gilteritinib 20 mg7.1
Gilteritinib 40 mg0
Gilteritinib 80 mg8.3
Gilteritinib 120 mg10.7
Gilteritinib 200 mg7.9
Gilteritinib 300 mg20.0
Gilteritinib 450 mg0

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Terminal Elimination Half-life (t1/2) After Multiple Doses of Gilteritinib

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Cycle 1 day 15: predose, 0.5, 1, 2, 4, 6, 24 hours postdose

Interventionhours (Mean)
Gilteritinib 20 mg in Escalation Phase62.14
Gilteritinib 40 mg in Escalation Phase151.8
Gilteritinib 80 mg in Escalation Phase86.11
Gilteritinib 120 mg in Escalation Phase45.85
Gilteritinib 200 mg in Escalation Phase141.9
Gilteritinib 300 mg in Escalation Phase142.2

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Time to Best CR/CRh (TTBCRCRh)

TTBCRCRh was defined as the time from the first dose of study drug until the first date that the best response of CR or CRh was achieved. TTBCRCRh was evaluated for participants who achieved CR or CRh. For participants who achieve both CR and CRh, the first CR date was used. TTBCRCRh was calculated only for participants who were FLT3 mutation positive. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
Gilteritinib 20 mg57.0
Gilteritinib 80 mg57.0
Gilteritinib 120 mg63.0
Gilteritinib 200 mg88.0
Gilteritinib 300 mg30.0

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Time to First CR/CRh (TTFCRCRh)

TTFCRCRh was defined as the time from the first dose of study drug until the date of first either CR or CRh. TTFCRCRh was evaluated for participants who achieved CR or CRh. For participants who achieve both CR and CRh, the first CR date or CRh date, whichever occurs first was used. TTFCRCRh was calculated only for participants who were FLT3 mutation positive. (NCT02014558)
Timeframe: From first dose of study drug up to end of treatment (median treatment duration was 69.5 days, minimum of 3 days and maximum of 1320 days)

Interventiondays (Median)
Gilteritinib 20 mg57.0
Gilteritinib 80 mg57.0
Gilteritinib 120 mg59.0
Gilteritinib 200 mg57.0
Gilteritinib 300 mg28.0

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Tmax of Gilteritinib in Co-administration With Voriconazole

Plasma samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Cycle 1 Day 15 and Cycle 2 Day 1: predose, 0.5, 1, 2, 4, 6, 24 hours postdose (gilteritinib)

Interventionhours (Median)
Gilteritinib 20 mg in Expansion Phase2.08

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Amount of Drug Excreted in Urine (Aelast) of Cephalexin Administered With and Without Gilteritinib

Urine samples were used for pharmacokinetic assessments. (NCT02014558)
Timeframe: Day -1 and cycle 1 day 15: 0-3 hours, 3-6 hours, 6-24 hours postdose (cephalexin)

Interventionmg (Mean)
Cephalexin Alone (Day -1)Cephalexin + Gilteritinib (Cycle 1 Day 15)
Gilteritinib 200 mg in Expansion Phase548.9448.8

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose

(NCT02100826)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

Interventionhour*microgram per milliliter(h*μg/mL) (Geometric Mean)
Cephalexin (Test)77.430
Cephalexin (Reference)76.374

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Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin

(NCT02100826)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionMicrogram per milliliter(µg/ml) (Geometric Mean)
Cephalexin (Test)34.002
Cephalexin (Reference)33.522

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Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum

(NCT02100826)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionHours (Median)
Cephalexin (Test)2.000
Cephalexin (Reference)1.250

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Pharmacokinetics: Area Under the Concentration Versus Time Curve of Cephalexin From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose

(NCT02123446)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionHour*microgram per milliliter(h*µg/mL) (Geometric Mean)
Cephalexin (Reference)19.102
Cephalexin (Test)19.207

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Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin

(NCT02123446)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionMicrogram per milliliter(µg/ml) (Geometric Mean)
Cephalexin (Reference)10.976
Cephalexin (Test)9.710

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Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum

(NCT02123446)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

Interventionhours (Median)
Cephalexin (Reference)1.000
Cephalexin (Test)1.000

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Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum

(NCT02123459)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionHours (Median)
Cephalexin (Reference)1.500
Cephalexin (Test)1.500

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose

(NCT02123459)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionHours*microgram per milliliter(h*μg/mL) (Geometric Mean)
Cephalexin (Reference)29.539
Cephalexin (Test)35.857

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Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin

(NCT02123459)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

Interventionμg/mL (Geometric Mean)
Cephalexin (Reference)10.378
Cephalexin (Test)12.610

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Pharmacokinetics: Time to Reach Maximum Observed Concentration (Tmax) of Cephalexin Following a Single Dose Maximum

(NCT02123472)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionHours (Median)
Cephalexin (Test)0.750
Cephalexin (Reference)0.750

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Pharmacokinetics: Area Under the Concentration Versus Time Curve From Time Zero to Infinity [AUC(0-∞)] of Cephalexin Following a Single Dose

(NCT02123472)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

Interventionhour*microgram per milliliter (h*µg/mL) (Geometric Mean)
Cephalexin (Test)36.256
Cephalexin (Reference)38.198

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Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin

(NCT02123472)
Timeframe: Pre-dose, 0.25, 0.5, 0.75, 1.0, 1.25, 1.5, 1.75, 2.0, 2.5, 3.0, 3.5, 4.0, 5.0, 6.0, and 7.0 hours in each period

InterventionMicrogram per milliliter(μg/mL) (Geometric Mean)
Cephalexin (Test)24.608
Cephalexin (Reference)26.410

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Area Under the Plasma Concentration Versus Time Curve Time 0 to 24 Hours (AUC0-24h) of Tedizolid

AUC0-24h is a measure of the total tedizolid exposure in the plasma from the dose to 24 hours after last dose. AUC0-24h was estimated based on population pharmacokinetic analysis of observed pharmacokinetic data. Blood samples were collected for pharmacokinetic analysis at specific time points. (NCT02276482)
Timeframe: Day 1 at 5-80 min and 4-12 hrs post-infusion or 2 samples collected between 4-12 hrs after oral dose, at least 60 min apart; at 48-72 hrs: within 60 min prior to administration and 4-12 hrs after administration; and anytime between Day 7 and 9

Interventionµg*h/mL (Geometric Mean)
Tedizolid Phosphate28.6

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Number of Participants With Adverse Events on Tedizolid Phosphate and Comparator Drugs

An adverse event (AE) refers to a treatment-emergent adverse event (TE-AE). A TE-AE is any AE that newly appeared, increased in frequency, or worsened in severity following initiation of study drug. (NCT02276482)
Timeframe: Up to 40 days (including 30-day follow-up)

InterventionParticipants (Count of Participants)
Tedizolid Phosphate13
Antibiotic Comparator Drug3

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Number of Participants With Early Clinical Responses Measured by Lesion Reduction

Early clinical response is defined as ≥20% reduction from baseline lesion area (defined as length multiplied by the width of the erythema, edema, and/or induration [EEI]) at the 48-72 hour (hr) visit. (NCT02276482)
Timeframe: 48-72 hr after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate84
Antibiotic Comparator Drug28

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Number of Participants With Investigator's Assessment Indicating Clinical Success at End of Therapy (EOT) Visit (Intent to Treat Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2)absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: EOT Visit: up to 13 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate88
Antibiotic Comparator Drug28

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Number of Participants With Investigator's Assessment Indicating Clinical Success at EOT Visit (Clinically Evaluable-End of Therapy [CE-EOT] Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2) absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: EOT Visit: up to 13 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate87
Antibiotic Comparator Drug27

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Number of Participants With Investigator's Assessment Indicating Clinical Success at Test of Cure (TOC) Visit (Intent to Treat Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2)absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: TOC Visit: 18-25 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate88
Antibiotic Comparator Drug27

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Number of Participants With Investigator's Assessment Indicating Clinical Success at TOC Visit (Clinically Evaluable-Test of Cure [CE-TOC] Analysis Set)

Investigator's assessment of clinical success is defined as (1) resolution or near resolution of most disease-specific signs and symptoms, (2)absence or near resolution of regional or systemic signs of infection (lymphadenopathy, fever, >10% immature neutrophils, abnormal white blood cell count), if present at baseline, and (3) no new signs, symptoms, or complications attributable to the infection under study so no further antibiotic therapy is required for the treatment of the primary lesion. (NCT02276482)
Timeframe: TOC Visit: 18-25 days after first drug infusion

InterventionParticipants (Count of Participants)
Tedizolid Phosphate87
Antibiotic Comparator Drug26

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Peak Plasma Concentration (Cmax) of Tedizolid

The Cmax of tedizolid in plasma after the last dose was estimated based on population pharmacokinetic analysis of observed pharmacokinetic data. Blood samples were collected for pharmacokinetic analysis at specific time points. (NCT02276482)
Timeframe: Day 1 at 5-80 minutes (min) and 4-12 hrs post-infusion or 2 samples collected between 4-12 hrs after oral dose, at least 60 min apart; at 48-72 hrs: within 60 min prior to administration and 4-12 hrs after administration; and anytime between Day 7 and 9

Interventionµg/mL (Geometric Mean)
Tedizolid Phosphate3.13

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Change From Baseline in Lesion Size

Lesion size is the area in cm^2 of erythema, edema or induration. A negative number corresponds to a decrease in lesion size. (NCT02276482)
Timeframe: Baseline and TOC visit (18 to 25 days after infusion)

,
Interventioncm^2 (Mean)
BaselineChange at Day 25
Antibiotic Comparator Drug83.22-82.51
Tedizolid Phosphate135.44-134.27

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Pharmacokinetics: Maximum Concentration (Cmax) of Cephalexin Following a Single Dose

(NCT02490670)
Timeframe: Predose,0.167, 0.333, 0.5, 0.75, 1, 1.25, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, and 7 hours after drug administration in each period

InterventionMicrogram per milliliter (μg/mL) (Geometric Mean)
Cephalexin (Reference)13.634
Cephalexin (Test)13.636

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Pharmacokinetics (PK): Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC[0-∞]) of Cephalexin Following a Single Dose

(NCT02490670)
Timeframe: Predose, 0.167, 0.333, 0.5, 0.75, 1, 1.25, 1.500, 2, 2.5, 3, 3.5, 4, 5, 6, and 7 hours after drug administration in each period

Interventionhour*microgram per milliliter (h*μg/mL) (Geometric Mean)
Cephalexin (Reference)38.038
Cephalexin (Test)37.913

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Number of Patients With a Major Cardiac Implantable Electronic Devices (CIED) Infection

The primary study endpoint will be the number of patients with CIED infection resulting in complete CIED system removal, antibiotic therapy in patients who are not candidates for system removal, or death due to CIED infection. (NCT02809131)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Saline Irrigation5
Antibiotic Irrigation and Oral Antibiotics6

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Number of Patients With a Minor Cardiac Implantable Electronic Devices (CIED) Infection

A minor superficial infection of the incision that does not involve the generator pocket, does not result in any systemic symptoms or signs, and is treated with either observation or a short course of oral antibiotics (NCT02809131)
Timeframe: 6 months

InterventionParticipants (Count of Participants)
Saline Irrigation5
Antibiotic Irrigation and Oral Antibiotics5

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