Page last updated: 2024-11-07

moxifloxacin

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Description

Moxifloxacin: A fluoroquinolone that acts as an inhibitor of DNA TOPOISOMERASE II and is used as a broad-spectrum antibacterial agent. [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

moxifloxacin : A quinolone that consists of 4-oxo-1,4-dihydroquinoline-3-carboxylic acid bearing a cyclopropyl substituent at position 1, a fluoro substitiuent at position 6, a (4aS,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl group at position 7 and a methoxy substituent at position 8. A member of the fluoroquinolone class of antibacterial agents. [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]

Cross-References

ID SourceID
PubMed CID152946
CHEBI ID63611
SCHEMBL ID24007
MeSH IDM0273433

Synonyms (80)

Synonym
moxifloxacin [inn:ban]
AB00171653-14
moxifloxacin
151096-09-2
mxfx
mxf ,
(1's,6's)-1-cyclopropyl-7-(2,8-diazabicyclo[4.3.0]non-8-yl)-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
actira (*hydrochloride*)
avelox (*hydrochloride*)
bay 12-8039 (*hydrochloride*)
7-[(4as,7as)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-quinoline-3-carboxylic acid
DB00218
1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-((4as,7as)-octahydro-6h-pyrrolo(3,4-b)pyridin-6-yl)-4-oxo-3-quinolinecarboxylic acid
1-cyclopropyl-6-fluoro-8-methoxy-7-[(4as,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
mfx ,
avelox iv
zimoxin
chebi:63611 ,
7-[(4as,7as)-1,2,3,4,4a,5,7,7a-octahydropyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxoquinoline-3-carboxylic acid
D08237
moxifloxacin (inn)
avelox iv (tn)
avolex
hsdb 8026
unii-u188xyd42p
moxifloxacine
ccris 8690
3-quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-((4as,7as)-octahydro-6h-pyrrolo(3,4-b)pyridin-6-yl)-4-oxo-
u188xyd42p ,
1-cyclopropyl-6-fluoro-7-((4as,7as)-hexahydro-1h-pyrrolo[3,4-b]pyridin-6(2h)-yl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
BCP9000962
bdbm50366824
BCP0726000137
moxifloxacin [inn]
moxifloxacin [who-dd]
moxifloxacin [vandf]
moxifloxacin [mi]
AM84644
3-quinolinecarboxylic acid, 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4as,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-
AKOS015895251
S5535
CCG-221192
HY-66011A
CS-1895
AB00171653-11
SCHEMBL24007
AB00171653-13
FABPRXSRWADJSP-MEDUHNTESA-N
DTXSID3048491 ,
moxyfloxacin
AC-25913
AB00171653_15
7-[(4as,7as)-octahydro-1h-pyrrolo[3,4-b]pyridin-6-yl]-1-cyclopropyl-6-fluoro-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid
mfcd04117996
EX-A016
SR-01000763482-3
sr-01000763482
SBI-0206792.P001
HMS3715P05
rkl10080
3-quinolinecarboxylic acid,1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4as,7as)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-
BCP22895
Q424940
AS-41986
naproxendiisopropylamide
1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4ar,7ar)-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid
1-cyclopropyl-6-fluoro-8-methoxy-7-octahydro-6h-pyrrolo[3,4-b]pyridin-6-yl-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid
AR-270/43507941
NCGC00271749-08
gtpl10915
nsc782304
nsc-782304
bay128039
1-cyclopropyl-6-fluoro-7-((4as,7as)-hexahydro-1h-pyrrolo[3,4-b]pyridin-6(2h)-yl)-8-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylicacid
EN300-1726094
moxifloxacinum
j01ma14
moxifloxacino
dtxcid9028465
s01ae07

Research Excerpts

Overview

Moxifloxacin is a fluoroquinolone with a broad spectrum of activity and good penetration into many tissues, including bone. It is an important drug in the regimen for treating Drug-resistant TB and the decision to exclude this drug from the regimen sho

ExcerptReferenceRelevance
"Moxifloxacin (MXF) is a fluoroquinolone antibiotic that is effective against respiratory infections. "( P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
Brillault, J; Couet, W; De Castro, WV; Harnois, T; Kitzis, A; Olivier, JC, 2009
)
2.07
"Moxifloxacin is a fluoroquinolone with a broad spectrum of activity and good penetration into many tissues, including bone. "( Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
Bulitta, JB; Drusano, GL; Gusinde, J; Hennig, FF; Holzgrabe, U; Kinzig, M; Landersdorfer, CB; Sörgel, F, 2009
)
2.15
"Moxifloxacin is a fourth-generation fluoroquinolone used as a second-line treatment for multiple bacterial infections. "( Severe sequelae in bilateral acute iris transillumination syndrome secondary to the use of oral moxifloxacin: a case report.
Arteaga-Rivera, K; de-la-Torre, A; Neira-Segura, N; Reyes-Guanes, J; Rivera-Valdivia, N, 2021
)
2.28
"Moxifloxacin is a fluoroquinolone that is commonly used in adults, but not children. "( Population Pharmacokinetics of Moxifloxacin in Children.
Conrad, T; Ghazaryhan, V; Greenberg, RG; Gu, K; Harward, M; Kirkpatrick, CM; Landersdorfer, CB; Nakamura, A; Osborn, B; Rivera-Chaparro, N; Walter, EB, 2022
)
2.45
"Moxifloxacin (MOX) is a fourth-generation fluoroquinolone and a broad spectrum antibiotic used in the management of bacterial keratitis (BK). "( Cationic Chitosan/Pectin Polyelectrolyte Nanocapsules of Moxifloxacin as Novel Topical Management System for Bacterial Keratitis.
Kesavan, K; Mohan, P; Rangari, VD, 2022
)
2.41
"Moxifloxacin is a wide range antibacterial drug that is available as an eye drops for topical use for different types of ocular infections including post-operative endophthalmitis."( Efficacy Of Injecting Intra-Vitreal Moxifloxacin In Acute Post-Operative Endophthalmitis.
Ahmad, A; Rehman, M,
)
1.13
"Moxifloxacin (MOX) is a fourth-generation fluoroquinolone used in the form of tablets, infusion solutions and ophthalmic solutions. "( Moxifloxacin: Physical-chemical and Microbiological Analytical Methods in the Context of Green Analytical Chemistry.
da Silva, TAC; Kogawa, AC; Lustosa, IA, 2023
)
3.8
"Moxifloxacin is an important drug in the regimen for treating Drug-resistant TB and the decision to exclude this drug from the regimen should not be taken merely on the basis of mutational patterns. "( Correlating clinical breakpoint concentration of moxifloxacin with gyrA mutations using the GenoType MTBDRsl assay Version 2.0.
Chopra, KK; Dwivedi, KK; Hanif, M; Khanna, A; Sidiq, Z; Vashishat, BK, 2023
)
2.61
"Moxifloxacin is a fourth-generation fluoroquinolone (FQ) that is approved for use in people to treat a variety of infections. "( A pilot study on the comparative minimum inhibitory and mutant prevention concentration values for moxifloxacin and pradofloxacin against canine and human isolates of Staphylococcus pseudintermedius and S. schleiferi.
Blondeau, JM; Levinson, M; Plowgian, C; Rosenkrantz, W, 2019
)
2.17
"Moxifloxacin is a fourth generation widely used fluoroquinolone antibiotic. "( Moxifloxacin-induced neutropenia in 26-year-old man.
Aytekin, A; Bedir, O; Ispir, E; Kula Atik, T; Tas, D; Turhan, U; Yeniiz, E, 2018
)
3.37
"Moxifloxacin is an orally administrated fourth-generation quinolone with broad-spectrum coverage against tumor-associated bacteria."( Efficacy of Moxifloxacin plus Treatment of Physician's Choice in Patients with Metastatic Breast Cancer.
Bi, X; Huang, J; Huang, Z; Li, J; Shi, W; Shi, Y; Su, Y; Wang, S; Wang, X; Xia, W; Yuan, Z, 2020
)
1.66
"Moxifloxacin is a BCS class I drug with a wide therapeutic index."( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Moxifloxacin Hydrochloride.
Abdallah, DB; Abrahamsson, B; Charoo, NA; Cristofoletti, R; Dressman, J; Groot, DW; Langguth, P; Mehta, M; Parr, A; Parveen, T; Polli, JE; Shah, VP; Tajiri, T, 2020
)
1.52
"Moxifloxacin is a third-generation fluoroquinolone antibiotic with broad spectrum activity and also used as component of anti-tubercular therapy (ATT). "( Moxifloxacin induced encephalopathy in disseminated tuberculosis: A case report.
Akhtar, SM; Kaur, H; Mittal, GK; Reddy, VASK, 2020
)
3.44
"Moxifloxacin is a fourth-generation fluoroquinolone that has shown good antibacterial activity against both gram-positive cocci and gram-negative bacteria. "( Moxifloxacin is a safe and effective candidate agent for tuberculosis treatment: a meta-analysis of randomized controlled trials.
Fan, J; Sun, M, 2021
)
3.51
"Moxifloxacin is an antibiotic used in the clinic to both treat and prevent bacterial infections, and it has both good pharmacokinetic properties for tissue penetration and intrinsic fluorescence under ultraviolet (UV) excitation."( Clinically Compatible Fluorescence Microscopy Based on Moxifloxacin Antibiotic.
Kim, KH; Lee, S, 2021
)
1.59
"Moxifloxacin is a recommended drug for rifampin-resistant tuberculosis (RR-TB) treatment, but there is limited pediatric pharmacokinetic and safety data, especially in young children. "( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
3.61
"Moxifloxacin is a fluoroquinolone with excellent activity in community-acquired respiratory tract infections. "( Moxifloxacin-induced oral erythema multiforme: An unusual adverse effect hitherto unreported.
Das, S; Mallick, S; Rudra, O; Sharma, S,
)
3.02
"Moxifloxacin (MX) is an 8-methoxyquinolone antimicrobial drug, which is often used as a positive control in thorough QT (TQT) studies. "( Population pharmacokinetics of moxifloxacin and its concentration-QT interval relationship modeling in Chinese healthy volunteers.
He, YC; Huang, JH; Li, LJ; Liang, LY; Wang, K; Xu, FY; Xu, L; Yang, J; Yin, F; Zheng, QS, 2017
)
2.18
"Moxifloxacin is a second-line anti-TB drug that is useful in the treatment of drug-resistant TB. "( Moxifloxacin target site concentrations in patients with pulmonary TB utilizing microdialysis: a clinical pharmacokinetic study.
Bablishvili, N; Bernheim, A; Blumberg, HM; Derendorf, H; Gogishvili, S; Guarner, J; Heinrichs, MT; Kempker, RR; Little, BP; Nikolaishvili, K; Peloquin, CA; Sabulua, I; Tukvadze, N; Vashakidze, S, 2018
)
3.37
"Moxifloxacin is an antibiotic used in clinics and has recently been used as a clinically compatible cell-labeling agent for two-photon (2P) imaging. "( Three-photon tissue imaging using moxifloxacin.
Jang, WH; Jun, YW; Kim, B; Kim, KH; Kim, MJ; Lee, JH; Lee, S; Wang, T; Yoon, Y, 2018
)
2.2
"Moxifloxacin (MXF) is a broad-spectrum antibiotic orally administrated."( Novel polymeric dressing to the treatment of infected chronic wound.
Borges, FA; de Barros, NR; de Souza Salvador, SL; Del Arco, MC; Frade, MAC; Garms, BC; Herculano, RD; Leite, MN; Marcelino, MY; Oliveira, KSM; Pegorin, GS, 2019
)
1.24
"Moxifloxacin is a widely used fluoroquinolone for the treatment of complicated intra-abdominal infections. "( Application of Physiologically-Based and Population Pharmacokinetic Modeling for Dose Finding and Confirmation During the Pediatric Development of Moxifloxacin.
Coboeken, K; Eissing, T; Frei, M; Lippert, J; Stass, H; Sutter, G; Wendl, T; Willmann, S, 2019
)
2.16
"Moxifloxacin is a Food and Drug Administration (FDA) approved antibiotic and was used as a cell labeling agent through topical administration."( Fast and sensitive delineation of brain tumor with clinically compatible moxifloxacin labeling and confocal microscopy.
Chang, H; Chung, E; Jang, WH; Kim, B; Kim, EH; Kim, KH; Kim, MJ; Kim, S; Lee, KH; Lee, S; Park, WY; Shin, Y, 2020
)
1.51
"Moxifloxacin (MXF), is a fluoroquinolone drug thought to have some antifungal activity against Candida albicans. "( Vitreous and aqueous penetration of intravitreally and orally administered moxifloxacin in an experimental rabbit model of fungal endophthalmitis.
Aktas, Z; Arikan, S; Dinçel, A; Hasanreisoglu, B; Ozdek, S, 2013
)
2.06
"Moxifloxacin is an interesting adjuvant to consider as it is effectively prevents encystation of the amoeba which often complicates infection resolution."( Evaluation of the in vitro activity of commercially available moxifloxacin and voriconazole eye-drops against clinical strains of Acanthamoeba.
Arnalich-Montiel, F; López-Arencibia, A; Lorenzo-Morales, J; Martín-Navarro, CM; Piñero, JE; Valladares, B, 2013
)
1.35
"Moxifloxacin is an 8-methoxy quinolone with a broad spectrum of activity against clinically important pathogens. "( Pharmacokinetics of moxifloxacin in critically ill patients with impaired renal function undergoing pulse high-volume haemofiltration.
Chen, Y; Li, L; Li, R; Liang, X; Liu, S; Shi, W; Wang, WJ; Wang, X; Ye, Z; Yu, C; Zhang, B; Zhang, L; Zhuo, L, 2013
)
2.16
"moxifloxacin monotherapy is an effective and relatively safe option for the treatment of cSSSIs."( Sequential intravenous/oral moxifloxacin monotherapy for complicated skin and skin structure infections: a meta-analysis of randomised controlled trials.
Chen, F; Du, YQ; Lin, JM; Tu, WF; Wang, Y; Wen, JL; Zheng, N, 2013
)
1.41
"Moxifloxacin (MFLX) is a respiratory quinolone, and is effective against not only Gram-positive and negative bacteria but also anaerobes. "( [Efficacy and safety of moxifloxacin in patients with nursing and healthcare-associated pneumonia].
Akata, K; Awaya, Y; Choujin, Y; Inoue, N; Ishimoto, H; Kawajiri, T; Kawanami, Y; Kawanaml, T; Mukae, H; Nagata, S; Nishida, C; Noguchi, S; Obata, H; Ogoshi, T; Orihashi, T; Suzuki, Y; Taura, Y; Tokuyama, S; Yamasaki, K; Yatera, K; Yoshida, Y; Yoshii, C, 2013
)
2.14
"Moxifloxacin 400 mg is a widely used positive control in thorough QT (TQT) studies, but its QT-prolonging effects in Korean subjects have not been studied. "( The effects of moxifloxacin on QTc interval in healthy Korean male subjects.
An, H; Cho, JY; Chung, JY; Lee, J; Lim, KS; Moon, SJ; Yim, DS; Yu, KS, 2014
)
2.2
"Moxifloxacin 400 mg is an adequate positive control in Korean TQT studies. "( The effects of moxifloxacin on QTc interval in healthy Korean male subjects.
An, H; Cho, JY; Chung, JY; Lee, J; Lim, KS; Moon, SJ; Yim, DS; Yu, KS, 2014
)
2.2
"Moxifloxacin is a synthetic antibacterial agent belonging to the fluoroquinolone family. "( Moxifloxacin modulates inflammation during murine pneumonia.
Bals, R; Beisswenger, C; Bischoff, M; Honecker, A; Kamyschnikow, A; Tschernig, T, 2014
)
3.29
"Moxifloxacin is a leading fourth generation quinolone antibiotic that has been used worldwide perioperatively."( Comparison of the Anti-angiogenic and Anti-inflammatory Effects of Two Antibiotics: Clarithromycin Versus Moxifloxacin.
Ambati, BK; Archer, B; Cho, YK; Das, SK; Uehara, H, 2016
)
1.37
"Moxifloxacin is an effective therapeutic option for patients with AV."( Efficacy of oral moxifloxacin for aerobic vaginitis.
Fan, A; Geng, N; Han, C; Wang, C; Wang, Y; Xue, F; Yue, Y; Zhang, H, 2016
)
1.5
"Moxifloxacin (MOX) is a Mycobacterium tuberculosis DNA gyrase inhibitor. "( Effect of PEG and water-soluble chitosan coating on moxifloxacin-loaded PLGA long-circulating nanoparticles.
Devi, VK; Mustafa, S; Pai, RS, 2017
)
2.15
"Moxifloxacin is a fourth-generation fluoroquinolone that has been shown to be effective against Gram-positive, Gram-negative, and atypical strains, as well as multi-drug resistant Streptococcus pneumoniae."( Moxifloxacin: a respiratory fluoroquinolone.
Anzueto, A; Miravitlles, M, 2008
)
2.51
"Moxifloxacin is an advanced-generation fluoroquinolone with a broad spectrum of antimicrobial activity that is not metabolized by cytochrome P450 system. "( A significant interaction between moxifloxacin and warfarin in a patient with a mitral bioprosthetic valve.
Candevir, A; Cayli, M; Kurtaran, B; Sümbül, Z; Yildiz, F, 2008
)
2.07
"Moxifloxacin (MXF) is an 8-methoxyquinolone with high activity against Gram-positive bacteria. "( Successful treatment with moxifloxacin of experimental aortic valve endocarditis due to methicillin-resistant Staphylococcus aureus (MRSA).
Donta, I; Galani, L; Giamarellou, H; Iliopoulos, D; Karayiannakos, P; Pefanis, A; Sakka, V; Skiadas, I; Triantafyllidi, H, 2009
)
2.1
"Moxifloxacin is a new fourth-generation 8-methoxy fluoroquinolone developed primarily for the treatment of community-acquired pneumonia and upper respiratory tract infections. "( Pharmacokinetics and bioavailability of moxifloxacin in calves following different routes of administrations.
Goudah, A; Hasabelnaby, S, 2010
)
2.07
"Moxifloxacin is confirmed to be an effective alternative to ofloxacin/metronidazole for the treatment of PID in a large urban genitourinary clinic setting."( A comparison of treatment outcomes for moxifloxacin versus ofloxacin/metronidazole for first-line treatment of uncomplicated non-gonococcal pelvic inflammatory disease.
Boothby, M; Page, J; Pryor, R; Ross, JD, 2010
)
1.35
"Moxifloxacin (MFX) is a useful agent in the treatment of multi-drug-resistant tuberculosis (MDR-TB). "( Determination of moxifloxacin in human plasma, plasma ultrafiltrate, and cerebrospinal fluid by a rapid and simple liquid chromatography- tandem mass spectrometry method.
Alffenaar, JW; Greijdanus, B; Pranger, AD; Uges, DR; Wessels, AM, 2010
)
2.14
"Moxifloxacin therapy is an effective alternative to teicoplanin for chronic implant-related MSSA osteomyelitis."( Efficacy of moxifloxacin compared to teicoplanin in the treatment of implant-related chronic osteomyelitis in rats.
Cakici, H; Guven, M; Kocoglu, E; Ozturan, KE; Yucel, I, 2010
)
1.46
"Moxifloxacin is a quinolone up to 10 times more active against staphylococci than ciprofloxacin and the risk of resistance development during monotherapy against staphylococci is theoretically lower for moxifloxacin, but information regarding its use in bone infections is lacking."( Safety and efficacy of moxifloxacin monotherapy for treatment of orthopedic implant-related staphylococcal infections.
Aguado, JM; Caba, P; Chaves, F; Garcia-Reyne, A; Lizasoain, M; Llanos, F; López-Medrano, F; Resines, C; San Juan, R, 2010
)
1.39
"Moxifloxacin is a fluoroquinolone antibiotic that demonstrates potent activity against Y."( Use of an in vitro pharmacodynamic model to derive a moxifloxacin regimen that optimizes kill of Yersinia pestis and prevents emergence of resistance.
Brown, DL; Drusano, GL; Eichas, A; Fikes, S; Files, K; Heine, HS; Kinzig-Schippers, M; Liu, W; Louie, A; Sörgel, F; VanScoy, B, 2011
)
1.34
"Moxifloxacin (MFX) is a powerful second-line anti-tuberculosis (TB) agent, but the optimal dose has not yet been established and long-term safety data are scarce. "( Evaluation of moxifloxacin for the treatment of tuberculosis: 3 years of experience.
Aarnoutse, RE; Alffenaar, JW; Kosterink, JG; Pranger, AD; Uges, DR; van Altena, R; van der Werf, TS; van Soolingen, D, 2011
)
2.17
"Moxifloxacin is a fluoroquinolone antibiotic which has been associated with QT prolongation and, as a result, is recommended by the regulatory authorities as a positive control in thorough QT studies performed to evaluate the potential of new chemical entities to induce QT prolongation in humans."( Pharmacokinetic-pharmacodynamic modelling of the effect of Moxifloxacin on QTc prolongation in telemetered cynomolgus monkeys.
Chen, X; Fermini, B; Gorczyca, WP; Holbrook, M; Sun, SZ; Umland, J; Van Der Graaf, PH; Watson, KJ; Zhang, Y,
)
1.1
"Moxifloxacin (MFX) is a potential oral agent use in the treatment of multidrug-resistance tuberculosis (MDR-TB). "( Determination of moxifloxacin in dried blood spots using LC-MS/MS and the impact of the hematocrit and blood volume.
Alffenaar, JW; Brouwers, JR; Koster, RA; Uges, DR; Vu, DH, 2011
)
2.15
"Moxifloxacin (MFX) is a potent drug for multidrug resistant tuberculosis(TB) treatment and is also useful if first-line agents are not tolerated. "( Limited-sampling strategies for therapeutic drug monitoring of moxifloxacin in patients with tuberculosis.
Aarnoutse, RE; Alffenaar, JW; Kosterink, JG; Pranger, AD; Uges, DR; van Altena, R; van der Werf, TS, 2011
)
2.05
"Moxifloxacin is a respiratory quinolone that is expected to be useful for treating community-acquired bacterial pneumonia, but few clinical studies and not a detailed evaluation of its pharmacokinetics have been conducted in Japan in patients with pneumonia. "( Efficacy and safety of moxifloxacin for community-acquired bacterial pneumonia based on pharmacokinetic analysis.
Fukano, H; Hara, H; Kawanishi, M; Kimura, M; Kishimoto, M; Matsushima, T; Moriya, O; Niki, Y; Okimoto, N; Yoneyama, H; Yoshida, K, 2011
)
2.12
"Moxifloxacin is an effective and relatively safe option for the treatment of patients with intra-abdominal infections."( Moxifloxacin monotherapy for treatment of complicated intra-abdominal infections: a meta-analysis of randomised controlled trials.
Deng, X; Liu, RL; Mu, YP; Wang, LQ; Wang, Y; Wei, MD; Zhu, N, 2012
)
2.54
"Moxifloxacin is a quinolone antibiotic and is one of the treatment options."( The use of moxifloxacin for acute exacerbations of chronic obstructive pulmonary disease and chronic bronchitis.
Macklin-Doherty, A; Wilson, R, 2012
)
1.49
"Moxifloxacin is an antibiotic of the fluoroquinolone class, marketed in France since 2002. "( [Severe pseudouveitis associated with moxifloxacin therapy].
Chapuzet, C; Duncombe, A; Gueit, I; Gueudry, J; Massy, N; Muraine, M, 2013
)
2.1
"Moxifloxacin is an advanced-generation, 8-methoxy fluoroquinolone that is active against a broad spectrum of pathogens, including antibiotic resistant Streptococcus pneumoniae. "( Determination of moxifloxacin in human plasma by liquid chromatography electrospray ionization tandem mass spectrometry.
Bartlett, MG; Stewart, JT; Vishwanathan, K, 2002
)
2.1
"Moxifloxacin is a new fluoroquinolone antimicrobial approved for the treatment of acute bacterial rhinosinusitis. "( Sinus tissue concentration of moxifloxacin after a single oral dose.
Dinis, PB; Martins, ML; Monteiro, MC; Morais, JG; Silva, N, 2004
)
2.05
"Moxifloxacin is an advanced-generation fluoroquinolone used primarily for the treatment of respiratory tract infections."( Clinical experience with moxifloxacin in patients with respiratory tract infections.
Arcuri, P; Brar, JS; Celesk, RA; Church, DA; Faich, GA; Haverstock, DC; Kowalsky, SF; Morganroth, J; Whitehouse, AB, 2004
)
2.07
"Moxifloxacin is a recently developed fourth-generation methoxyquinolone with a broad spectrum of activity against both Gram-positive and Gram-negative aerobic bacteria and anaerobes. "( Moxifloxacin penetration into human gastrointestinal tissues.
Büchler, MW; Friess, H; Geiss, HK; Halaceli, I; Hoppe-Tichy, T; Kleeff, J; Swoboda, S; Wirtz, M, 2004
)
3.21
"Moxifloxacin is a recent fluoroquinolone with an antibacterial spectrum encompassing both aerobic Gram-negative and Gram-positive strains, as well as anaerobic bacteria. "( Effect of moxifloxacin on bacterial pathogenicity factors in comparison with amoxicillin, clarithromycin and ceftriaxone.
De Vecchi, E; Drago, L; Gismondo, MR; Nicola, L; Tocalli, L, 2004
)
2.17
"Moxifloxacin is a broad-spectrum, advanced-generation fluoroquinolone that has potent activity against respiratory tract infections in adults in both oral and IV formulations."( Safety profile of oral and intravenous moxifloxacin: cumulative data from clinical trials and postmarketing studies.
Ball, P; Choudhri, S; Kubin, R; Owens, R; Stahlmann, R, 2004
)
1.31
"Moxifloxacin is an 8-methoxy quinolone with a broad range of activity against clinically important pathogens. "( Pharmacokinetics of moxifloxacin in patients undergoing continuous venovenous haemodiafiltration.
Ahmed, S; Fuhrmann, V; Jaeger, W; Schenk, P; Thalhammer, F, 2004
)
2.09
"Moxifloxacin (Avelox) is a fluoroquinolone antibacterial with a methoxy group in the C-8 position and a bulky C-7 side chain. "( Moxifloxacin: a review of its use in the management of bacterial infections.
Keating, GM; Scott, LJ, 2004
)
3.21
"Moxifloxacin is a quinolone antimicrobial that has potent activity against Mycobacterium tuberculosis. "( Selection of a moxifloxacin dose that suppresses drug resistance in Mycobacterium tuberculosis, by use of an in vitro pharmacodynamic infection model and mathematical modeling.
Deziel, MR; Drusano, GL; Gumbo, T; Louie, A; Parsons, LM; Salfinger, M, 2004
)
2.12
"Moxifloxacin (Avelox) is a recently-developed fluoroquinolone that has a broad spectrum of antimicrobial activity, including typical respiratory pathogens, atypical and intracellular respiratory pathogens, Gram-negative pathogens and many anaerobes. "( Moxifloxacin (Avelox): a novel fluoroquinolone with a broad spectrum of activity.
Caeiro, JP; Iannini, PB, 2003
)
3.2
"Moxifloxacin is a newly developed fluoroquinolone with a potent antimicrobial activity."( Treatment of Staphylococcus epidermidis endophthalmitis with intravitreal moxifloxacin in a rabbit model.
Cetinkaya, Z; Ermis, SS; Kiyici, H; Ozturk, F, 2005
)
1.28
"Moxifloxacin is a fourth-generation fluoroquinolone that has been shown to be effective against respiratory pathogens, including Gram-positive (Streptococcus pneumoniae), Gram-negative (Haemophilus influenzae, Moraxella catarrhalis), and atypical strains (Chlamydia pneumoniae, Mycoplasma pneumoniae), as well as multi-drug resistant S. "( Moxifloxacin in respiratory tract infections.
Miravitlles, M, 2005
)
3.21
"Moxifloxacin is a new fluoroquinolone antibacterial agent with a broad spectrum activity."( Tolerability of moxifloxacin in patients with antibiotic hypersensitivity.
Bozkurt, B; Kalyoncu, AF; Karakaya, G,
)
1.2
"Moxifloxacin is an quinolone chemically different from other fluoroquinolones."( Immediate hypersensitivity to quinolones: moxifloxacin cross-reactivity.
Blasco, A; del Pozo, MD; González, I; Lobera, T, 2005
)
1.31
"Moxifloxacin is a new generation fluoroquinolone antimicrobial agent used worldwide. "( Effects of enteral feeding on the oral bioavailability of moxifloxacin in healthy volunteers.
Borner, K; Burkhardt, O; Stass, H; Thuss, U; Welte, T, 2005
)
2.02
"Moxifloxacin is a fluoroquinolone antimicrobial agent with proven efficacy against community-acquired respiratory pathogens. "( Acute interstitial nephritis associated with moxifloxacin use.
Argirov, M; Fischereder, M; Ricken, G; Zecher, D, 2005
)
2.03
"Moxifloxacin is a fourth-generation fluoroquinolone approved for ophthalmic use as moxifloxacin ophthalmic solution 0.5% (VIGAMOX, Alcon, Fort Worth, TX)."( Safety of moxifloxacin as shown in animal and in vitro studies.
Holt, WF; Kastner, PR; McGee, DH; Rice, RL, 2005
)
1.45
"Moxifloxacin was shown to be an effective and well tolerated treatment for this group of patients with RTIs and was highly rated by both physicians and patients because of rapid symptom improvement and good tolerability."( Efficacy and tolerability of moxifloxacin in patients with respiratory tract infections treated in general practice: Results of a post-marketing surveillance study.
Bai, C; Chen, W; Li, Z; Wu, C, 2006
)
2.07
"Moxifloxacin is a new fluorquinolone with broad-spectrum activity. "( Stability of moxifloxacin injection in peritoneal dialysis solution bags (Dianeal PD1 1.36% and Dianeal PD1 3.86%).
Cárceles, C; Escudero, E; Espuny, A; Fernández-Varón, E; Marín, P; Villamayor, L, 2006
)
2.15
"Moxifloxacin, which is an 8-MeO-substituted fluoroquinolone, is less phototoxic than the other compounds."( Photophysical and phototoxic properties of the antibacterial fluoroquinolones levofloxacin and moxifloxacin.
Aloisi, GG; Amelia, M; Barbafina, A; Canton, M; Dall'Acqua, F; Elisei, F; Facciolo, L; Latterini, L; Vedaldi, D; Viola, G, 2004
)
1.26
"Moxifloxacin (MXF) is a fluoroquinolone that acts against both Gram positive and Gram negative bacteria."( Anti-inflammatory effects of moxifloxacin and human beta-defensin 2 association in human lung epithelial cell line (A549) stimulated with lipopolysaccharide.
Buommino, E; Cozza, V; Donnarumma, G; Iovene, MR; Paoletti, I; Tudisco, L; Tufano, MA, 2007
)
1.35
"Moxifloxacin is a novel antibacterial agent that undergoes extensive metabolism in the liver to the glucuronide M1 and the sulfate M2, which are eliminated via the bile. "( Involvement of Mrp2 (Abcc2) in biliary excretion of moxifloxacin and its metabolites in the isolated perfused rat liver.
Ahmed, S; Gattringer, KB; Jäger, W; Thalhammer, F; Thalhammer, T; Vo, NT, 2008
)
2.04
"Moxifloxacin is an 8-methoxyfluoroquinolone currently used in second-line regimens."( Daily dosing of rifapentine cures tuberculosis in three months or less in the murine model.
Bishai, WR; Chaisson, RE; Grosset, JH; Nuermberger, EL; Peloquin, CA; Rosenthal, IM; Tyagi, S; Vernon, AA; Williams, KN; Zhang, M, 2007
)
1.06
"Moxifloxacin is a fourth-generation fluoroquinolone that has been shown to be effective against respiratory pathogens, including atypicals and those resistant to most common antibiotics."( Moxifloxacin in the management of exacerbations of chronic bronchitis and COPD.
Miravitlles, M, 2007
)
2.5
"Moxifloxacin is a respiratory fluoroquinolone with a community acquired pneumonia indication. "( Fluoroquinolone resistance during 2000-2005: an observational study.
Lindsell, C; Ryan, RJ; Sheehan, P, 2008
)
1.79
"Moxifloxacin is a new 8-methoxyquinolone with high activity against gram-positive bacteria, including penicillin-resistant pneumococci. "( Evaluation of moxifloxacin, a new 8-methoxyquinolone, for treatment of meningitis caused by a penicillin-resistant pneumococcus in rabbits.
Frimodt-Møller, N; Knudsen, JD; Ostergaard, C; Sørensen, TK, 1998
)
2.1
"Moxifloxacin (BAY12-8039) is a new 8-methoxyquinolone shown to be active against Mycobacterium tuberculosis in vitro. "( Moxifloxacin (BAY12-8039), a new 8-methoxyquinolone, is active in a mouse model of tuberculosis.
Bishai, WR; Chaisson, RE; Chen, JM; Miyazaki, E; Miyazaki, M, 1999
)
3.19
"Moxifloxacin (BAY 12-8039) is an investigational 8-methoxy-fluoroquinolone with broad-spectrum gram-positive and gram-negative activity. "( Absolute bioavailability of moxifloxacin.
Agarwal, V; Ballow, C; Lettieri, J; Liu, P; Stass, H; Sullivan, JT, 1999
)
2.04
"Moxifloxacin is an 8-methoxyquinolone compound with activity against a wide range of bacteria. "( Activity of moxifloxacin against mycobacteria.
Billington, O; Gillespie, SH, 1999
)
2.13
"Moxifloxacin is a new 8-methoxyquinolone with improved in vitro activity against gram-positive bacteria."( In vitro activity of moxifloxacin, a new 8-methoxyquinolone, against gram-positive bacteria.
Malathum, K; Murray, BE; Singh, KV, 1999
)
1.34
"Moxifloxacin is an extended-spectrum fluoroquinolone which has improved coverage against gram-positive cocci and atypical pathogens compared with older fluoroquinolone agents, while retaining good activity against gram-negative bacteria. "( Moxifloxacin: a review of its clinical potential in the management of community-acquired respiratory tract infections.
Balfour, JA; Lamb, HM, 2000
)
3.19
"Moxifloxacin (BAY 12-8039) is a new 8-methoxy-fluoroquinolone antibacterial agent. "( Moxifloxacin, a new antibiotic designed to treat community-acquired respiratory tract infections: a review of microbiologic and pharmacokinetic-pharmacodynamic characteristics.
Nightingale, CH, 2000
)
3.19
"Moxifloxacin is a novel 8-methoxyquinolone with enhanced potency against important Gram-positive pathogens, notably Streptococcus pneumoniae. "( Moxifloxacin (Avelox): an 8-methoxyquinolone antibacterial with enhanced potency.
Ball, P, 2000
)
3.19
"Moxifloxacin appears to be a promising choice for the treatment of pneumococcal infections, including situations where therapeutic choices are limited due to penicillin and macrolide resistance."( Activity of moxifloxacin and twelve other antimicrobial agents against 216 clinical isolates of Streptococcus pneumoniae.
Esposito, S; Ianniello, F; Noviello, S,
)
1.95
"Moxifloxacin is a new fluoroquinolone. "( Effect of a single oral dose of moxifloxacin (400 mg and 800 mg) on ventricular repolarization in healthy subjects.
Démolis, JL; Funck-Brentano, C; Kubitza, D; Tennezé, L, 2000
)
2.03
"Moxifloxacin is a new broad-spectrum antibacterial agent for treatment of respiratory tract infection of pathogens, including the major pathogens isolated in respiratory tract infections. "( Evaluation of the clinical microbiology profile of moxifloxacin.
Krasemann, C; Meyer, J; Tillotson, G, 2001
)
2.01
"Moxifloxacin is an oral 8-methoxyquinolone antimicrobial approved in December 1999 for use in the treatment of acute bacterial sinusitis, acute bacterial exacerbations of chronic bronchitis, and community-acquired pneumonia."( Moxifloxacin: clinical efficacy and safety.
Culley, CM; Edwards, B; Klutman, N; Lacy, MK, 2001
)
2.47
"Moxifloxacin is a new 8-methoxyfluoroquinolone with a broad antibacterial spectrum. "( The influence of age and gender on the pharmacokinetics of moxifloxacin.
Heller, AH; Lettieri, JT; Liu, P; Sullivan, JT, 2001
)
2
"Moxifloxacin is a new oral 8-methoxy-quinolone with a wide spectrum of activity against Gram-negative and anaerobic bacteria, atypical micro-organisms and multi-resistant Gram-positive bacteria. "( Minimal inhibitory concentrations and time-kill determination of moxifloxacin against aerobic and anaerobic isolates.
Blandino, G; Caccamo, F; Milazzo, I; Musumeci, R; Nicoletti, G; Speciale, A, 2002
)
2
"Moxifloxacin is a broad spectrum fluoroquinolone with single daily administration, currently used, above all, for respiratory tract infections."( Mono, dual and triple moxifloxacin-based therapies for Helicobacter pylori eradication.
Bartolozzi, F; Cammarota, G; Candelli, M; Cremonini, F; Di Caro, S; Gasbarrini, A; Lupascu, A; Nista, EC; Ojetti, V; Zocco, MA, 2002
)
2.07
"Moxifloxacin is a fluoroquinolone antibacterial agent which attains good penetration into peripheral tissues and inflammatory fluids. "( Moxifloxacin in uncomplicated skin and skin structure infections.
Jarvis, B; Muijsers, RB, 2002
)
3.2
"Moxifloxacin (MXF) is a new 8-methoxyquinolone with potent activity against Mycobacterium tuberculosis and a half-life of 9 to 12 h in humans. "( Bactericidal activity of increasing daily and weekly doses of moxifloxacin in murine tuberculosis.
Bishai, W; Chaisson, R; Grosset, J; Nuermberger, E; Tyagi, S; Yoshimatsu, T, 2002
)
2

Effects

Moxifloxacin has a broad spectrum of antibacterial activity, including activity against penicillin-resistant Streptococcus pneumoniae. The drug has an impressive spectrum of coverage and this pharmacokinetic study reinforces its potential as a prophylactic drug against intraocular infections.

Moxifloxacin has been demonstrated to penetrate efficiently into human pancreatic tissue following iv or oral administration. It has a low propensity for causing phototoxic reactions relative to other fluoroquinolones, and animal data suggest that it has alow potential for causing excitatory CNS and hepatotoxic effects.

ExcerptReferenceRelevance
"Moxifloxacin has a rapid bactericidal effect against intracellular reservoirs of bacteria, whereas amoxicillin is only bacteriostatic and appears to prevent cellular lysis and the subsequent bacterial spreading to adjacent cells."( Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
Desroches, MC; Grayo, S; Join-Lambert, O; Le Monnier, A, 2008
)
1.33
"Moxifloxacin has an important role in the treatment of tuberculosis (TB). "( Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling.
Aarnoutse, RE; Boeree, MJ; Bolwerk, C; Burger, DM; Greupink, R; Hoefsloot, W; Koenderink, JB; Kuipers, S; Litjens, CHC; Magis-Escurra, C; Ruslami, R; Russel, FGM; Svensson, EM; Te Brake, LHM; van Crevel, R; van den Broek, PHH; van den Heuvel, JJMW; van Ingen, J; van Laarhoven, A; Verscheijden, LFM, 2022
)
2.52
"Moxifloxacin has an impressive spectrum of coverage and this pharmacokinetic study reinforces its potential as a prophylactic drug against intraocular infections, given the high aqueous levels post topical administration."( Aqueous penetration of orally and topically administered moxifloxacin.
Bairy, KL; Kamath, MG; Kamath, MM; Musmade, PB; Nayak, RR; Sharma, T, 2015
)
2.1
"Moxifloxacin has a broad antibacterial spectrum and rapid bactericidal activity, and is thus a good option for the treatment of bacterial infections in patients who have undergone organ or bone marrow transplantation. "( Moxifloxacin does not alter ciclosporin pharmacokinetics in transplant patients: a multiple-dose, uncontrolled, single-centre study.
Bauer, S; Delesen, H; Kubitza, D; Mai, I; Roots, I; Stass, H, 2010
)
3.25
"Moxifloxacin has a low potential to cause endotoxin-mediated detrimental clinical effects. "( Low endotoxin release from Escherichia coli and Bacteroides fragilis during exposure to moxifloxacin.
Holst, O; Lepper, PM; Scheibe, C; Trautmann, M; Wellinghausen, N, 2010
)
2.03
"Moxifloxacin has an activity similar to rifampin in human subjects with pulmonary tuberculosis, suggesting that it should undergo further assessment as part of a short course regimen for the treatment of drug-susceptible tuberculosis."( The bactericidal activity of moxifloxacin in patients with pulmonary tuberculosis.
Bongard, E; Gillespie, SH; Gosling, RD; Kanduma, EG; Morris, RW; Nyindo, M; Sam, NE; Uiso, LO, 2003
)
1.33
"Moxifloxacin has a broad spectrum of antibacterial activity, including activity against penicillin-resistant Streptococcus pneumoniae."( Moxifloxacin: a review of its use in the management of bacterial infections.
Keating, GM; Scott, LJ, 2004
)
2.49
"Moxifloxacin has a spectrum of coverage that appropriately encompasses the most common organisms in endophthalmitis."( Penetration pharmacokinetics of topically administered 0.5% moxifloxacin ophthalmic solution in human aqueous and vitreous.
Apte, RS; Blinder, KJ; Chi, J; Hariprasad, SM; Holekamp, NM; Mieler, WF; Prince, RA; Rosenblatt, B; Shah, GK; Thomas, MA, 2005
)
1.29
"Moxifloxacin has a spectrum of coverage that encompasses the most common organisms in endophthalmitis. "( Vitreous and aqueous penetration of orally administered moxifloxacin in humans.
Blinder, KJ; Feiner, L; Gao, H; Hariprasad, SM; Holekamp, NM; Mieler, WF; Prince, RA; Shah, GK, 2006
)
2.02
"Moxifloxacin has a low propensity for causing phototoxic reactions relative to other fluoroquinolones, and animal data suggest that it has a low potential for causing excitatory CNS and hepatotoxic effects."( Moxifloxacin: a review of its clinical potential in the management of community-acquired respiratory tract infections.
Balfour, JA; Lamb, HM, 2000
)
2.47
"Moxifloxacin has a greater bactericidal rate as determined by regression of log CFU versus time data."( Streptococcus pneumoniae response to repeated moxifloxacin or levofloxacin exposure in a rabbit tissue cage model.
Bui, KQ; Mattoes, H; McNabb, J; Nicolau, DP; Nightingale, CH; Quintiliani, R; Xuan, D; Zhong, M, 2001
)
1.29
"Moxifloxacin thus has a unique drug interaction profile that is advantageous for its safe use."( Profile of moxifloxacin drug interactions.
Kubitza, D; Stass, H, 2001
)
1.42
"Moxifloxacin has an absolute bioavailability of 90% after oral administration and a mean elimination half-life of 12 hours."( Moxifloxacin: clinical efficacy and safety.
Culley, CM; Edwards, B; Klutman, N; Lacy, MK, 2001
)
2.47
"Moxifloxacin has a rapid bactericidal effect against intracellular reservoirs of bacteria, whereas amoxicillin is only bacteriostatic and appears to prevent cellular lysis and the subsequent bacterial spreading to adjacent cells."( Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
Desroches, MC; Grayo, S; Join-Lambert, O; Le Monnier, A, 2008
)
1.33
"Moxifloxacin has an important role in the treatment of tuberculosis (TB). "( Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling.
Aarnoutse, RE; Boeree, MJ; Bolwerk, C; Burger, DM; Greupink, R; Hoefsloot, W; Koenderink, JB; Kuipers, S; Litjens, CHC; Magis-Escurra, C; Ruslami, R; Russel, FGM; Svensson, EM; Te Brake, LHM; van Crevel, R; van den Broek, PHH; van den Heuvel, JJMW; van Ingen, J; van Laarhoven, A; Verscheijden, LFM, 2022
)
2.52
"Moxifloxacin has rarely been reported to be a drug that is associated with DRESS syndrome."( A typical presentation of moxifloxacin-induced DRESS syndrome with pulmonary involvement: a case report and review of the literature.
Cheng, Y; Wang, X; Zhang, Y, 2022
)
1.74
"Moxifloxacin doses may have been insufficient in eyes with larger ACV."( Endophthalmitis Prophylaxis Failures in Patients Injected With Intracameral Antibiotic During Cataract Surgery.
Carolan, JA; Herrinton, L; Liu, L; Shorstein, NH, 2021
)
1.34
"Moxifloxacin (MXF) has antibacterial activity in Gram‑positive and Gram‑negative bacteria."( Bidirectional effects of moxifloxacin on the pro‑inflammatory response in lipopolysaccharide‑stimulated mouse peritoneal macrophages.
Chen, B; Hu, X; Li, N; Qiu, Z; Su, F; Yang, X; Yuan, H, 2018
)
1.51
"Moxifloxacin (MXF) has in vitro and in vivo activity against Mycobacterium avium complex (MAC) in experimental models. "( Treatment of refractory Mycobacterium avium complex lung disease with a moxifloxacin-containing regimen.
Hong, G; Jeon, K; Jeong, BH; Kim, CK; Kim, SY; Koh, WJ; Kwon, OJ; Lee, SH; Park, HY; Shin, SJ, 2013
)
2.06
"Moxifloxacin has potent bactericidal activity against Streptococcus pneumoniae; a major causative organism of lower respiratory tract infections. "( Moxifloxacin in lower respiratory tract infections: in silico simulation of different bacterial resistance and drug exposure scenarios.
Noreddin, AM; Salem, AH, 2014
)
3.29
"Moxifloxacin has good MICs for M."( Rapid drug tolerance and dramatic sterilizing effect of moxifloxacin monotherapy in a novel hollow-fiber model of intracellular Mycobacterium kansasii disease.
Gumbo, T; Leff, R; Meek, C; Pasipanodya, J; Sherman, CM; Srivastava, S, 2015
)
1.38
"Moxifloxacin has an impressive spectrum of coverage and this pharmacokinetic study reinforces its potential as a prophylactic drug against intraocular infections, given the high aqueous levels post topical administration."( Aqueous penetration of orally and topically administered moxifloxacin.
Bairy, KL; Kamath, MG; Kamath, MM; Musmade, PB; Nayak, RR; Sharma, T, 2015
)
2.1
"Moxifloxacin has bright intrinsic multiphoton fluorescence, good tissue penetration and high intracellular concentration."( Moxifloxacin: Clinically compatible contrast agent for multiphoton imaging.
Ahn, GO; Bok, S; Chung, E; Gho, YS; Hong, CP; Hwang, S; Jang, MH; Jang, WH; Kim, B; Kim, KH; Kim, MJ; Kim, S; Le, VH; Lee, G; Lee, J; Lee, JH; Lee, S; Myung, SJ; So, PT; Wang, T; Yoon, CJ; Yoon, Y, 2016
)
2.6
"Moxifloxacin has demonstrated a faster resolution of symptoms in community-acquired pneumonia and exacerbations of chronic bronchitis patients compared with first-line therapy together with excellent eradication rates."( Moxifloxacin: a respiratory fluoroquinolone.
Anzueto, A; Miravitlles, M, 2008
)
2.51
"Moxifloxacin has potent activity against Mycobacterium tuberculosis in vitro and in a mouse model of antituberculosis (TB) chemotherapy, but data regarding its activity in humans are limited."( Substitution of moxifloxacin for isoniazid during intensive phase treatment of pulmonary tuberculosis.
Bernardo, J; Bozeman, L; Chaisson, RE; Choudhri, S; Dorman, SE; Goldberg, S; Grosset, JH; Guy, E; Guyadeen, P; Heilig, CM; Johnson, JL; Leus, MC; Maltas, G; Menzies, D; Muzanye, G; Nuermberger, EL; Padayatchi, N; Vernon, A; Villarino, M, 2009
)
2.14
"Moxifloxacin has been used in the first-line treatment of Helicobacter pylori infection. "( Efficacy of four different moxifloxacin-based triple therapies for first-line H. pylori treatment.
Amitrano, M; Grossi, L; Manzoli, L; Marzio, L; Sacco, F; Spezzaferro, M, 2010
)
2.1
"Moxifloxacin has unique side chains at positions 7 and 8 on its bicyclic ring structure."( Immediate hypersensitivity to moxifloxacin with tolerance to ciprofloxacin: report of three cases and review of the literature.
Chang, B; Knowles, SR; Weber, E, 2010
)
1.37
"Moxifloxacin has been the most commonly used positive control in "thorough" QTc (TQT) studies. "( Statistical characteristics of moxifloxacin-induced QTc effect.
Dang, Q; Ng, MJ; Yan, LK; Zhang, J, 2010
)
2.09
"Moxifloxacin has a broad antibacterial spectrum and rapid bactericidal activity, and is thus a good option for the treatment of bacterial infections in patients who have undergone organ or bone marrow transplantation. "( Moxifloxacin does not alter ciclosporin pharmacokinetics in transplant patients: a multiple-dose, uncontrolled, single-centre study.
Bauer, S; Delesen, H; Kubitza, D; Mai, I; Roots, I; Stass, H, 2010
)
3.25
"Moxifloxacin has a low potential to cause endotoxin-mediated detrimental clinical effects. "( Low endotoxin release from Escherichia coli and Bacteroides fragilis during exposure to moxifloxacin.
Holst, O; Lepper, PM; Scheibe, C; Trautmann, M; Wellinghausen, N, 2010
)
2.03
"Moxifloxacin has demonstrated a broad spectrum coverage of both aerobic and anaerobic pathogens, good tissue penetration into the gastrointestinal tract, and a good tolerability profile."( Role of moxifloxacin for the treatment of community-acquired [corrected] complicated intra-abdominal infections in Taiwan.
Chen, CW; Chen, YH; Hsueh, PR; Huang, CT; Ko, WC; Lau, YJ; Lee, WS; Lee, YJ; Liu, CY; Liu, HD; Liu, JW, 2012
)
1.53
"Moxifloxacin monotherapy has similar efficacy to combination therapy."( Moxifloxacin monotherapy for treatment of complicated intra-abdominal infections: a meta-analysis of randomised controlled trials.
Deng, X; Liu, RL; Mu, YP; Wang, LQ; Wang, Y; Wei, MD; Zhu, N, 2012
)
2.54
"Moxifloxacin (MXF) has been shown to possess immunomodulatory properties in addition to its antimicrobial effects. "( Anti-inflammatory effects of moxifloxacin on rat airway smooth muscle cells exposed to allergen: Inhibition of extracellular-signal-regulated kinase and nuclear factor-κB activation and of interleukin-8 and eotaxin synthesis.
Hao, L; He, S; Li, H; Zhu, S, 2012
)
2.11
"Moxifloxacin has shown favorable safety and efficacy profiles in DFI patients and could be an alternative antibiotic therapy in the management of DFI."( Efficacy and safety of IV/PO moxifloxacin and IV piperacillin/tazobactam followed by PO amoxicillin/clavulanic acid in the treatment of diabetic foot infections: results of the RELIEF study.
Alder, J; Arvis, P; Dryden, M; Gyssens, IC; Kujath, P; Nathwani, D; Reimnitz, P; Schaper, NC, 2013
)
2.12
"Moxifloxacin has enhanced potency against Staphylococcus aureus, lower propensity to select for resistant mutants, and higher bactericidal activity against highly resistant strains than ciprofloxacin. "( Activity of and resistance to moxifloxacin in Staphylococcus aureus.
Hooper, DC; Ince, D; Zhang, X, 2003
)
2.05
"Moxifloxacin has an activity similar to rifampin in human subjects with pulmonary tuberculosis, suggesting that it should undergo further assessment as part of a short course regimen for the treatment of drug-susceptible tuberculosis."( The bactericidal activity of moxifloxacin in patients with pulmonary tuberculosis.
Bongard, E; Gillespie, SH; Gosling, RD; Kanduma, EG; Morris, RW; Nyindo, M; Sam, NE; Uiso, LO, 2003
)
1.33
"Moxifloxacin has a broad spectrum of antibacterial activity, including activity against penicillin-resistant Streptococcus pneumoniae."( Moxifloxacin: a review of its use in the management of bacterial infections.
Keating, GM; Scott, LJ, 2004
)
2.49
"Moxifloxacin has pharmacologic characteristics that support once-daily dosing regimens and dual routes of excretion that require little or no adjustment for renal or hepatic insufficiency."( Moxifloxacin (Avelox): a novel fluoroquinolone with a broad spectrum of activity.
Caeiro, JP; Iannini, PB, 2003
)
2.48
"Moxifloxacin has a spectrum of coverage that appropriately encompasses the most common organisms in endophthalmitis."( Penetration pharmacokinetics of topically administered 0.5% moxifloxacin ophthalmic solution in human aqueous and vitreous.
Apte, RS; Blinder, KJ; Chi, J; Hariprasad, SM; Holekamp, NM; Mieler, WF; Prince, RA; Rosenblatt, B; Shah, GK; Thomas, MA, 2005
)
1.29
"Moxifloxacin has been suggested as an option for monotherapy of intra-abdominal infections. "( Levofloxacin plus metronidazole administered once daily versus moxifloxacin monotherapy against a mixed infection of Escherichia coli and Bacteroides fragilis in an in vitro pharmacodynamic model.
Hermsen, ED; Hovde, LB; Rodvold, KA; Rotschafer, JC; Sprandel, KA, 2005
)
2.01
"Moxifloxacin has demonstrated a faster resolution of symptoms in CAP and exacerbations of CB patients compared with first-line therapy."( Moxifloxacin in respiratory tract infections.
Miravitlles, M, 2005
)
2.49
"Moxifloxacin has been shown to induce QT prolongation in both clinical and preclinical models. "( Effects of moxifloxacin on QT interval in conscious dogs.
Hart, SM; Mittelstadt, SW, 2005
)
2.16
"Moxifloxacin also has better mutant prevention characteristics than other fluoroquinolones."( Overview of the potency of moxifloxacin ophthalmic solution 0.5% (VIGAMOX).
Alfonso, E; Schlech, BA, 2005
)
1.35
"Moxifloxacin has a spectrum of coverage that encompasses the most common organisms in endophthalmitis. "( Vitreous and aqueous penetration of orally administered moxifloxacin in humans.
Blinder, KJ; Feiner, L; Gao, H; Hariprasad, SM; Holekamp, NM; Mieler, WF; Prince, RA; Shah, GK, 2006
)
2.02
"Moxifloxacin has promising preclinical activity against Mycobacterium tuberculosis, but has not been evaluated in multidrug treatment of tuberculosis in humans."( Moxifloxacin versus ethambutol in the first 2 months of treatment for pulmonary tuberculosis.
Burman, WJ; Chaisson, RE; Choudhri, S; Daley, CL; Engle, M; Goldberg, S; Johnson, JL; Mosher, AW; Munsiff, SS; Muzanye, G; Vernon, A; Zhao, Z, 2006
)
3.22
"Moxifloxacin has been demonstrated to penetrate efficiently into human pancreatic tissue following iv or oral administration. "( Penetration of moxifloxacin into the human pancreas following a single intravenous or oral dose.
Adam, U; Drewelow, B; Förster, S; Hopt, UT; Klar, E; Mundkowski, RG; Wacke, R, 2006
)
2.13
"Moxifloxacin has demonstrated better eradication in exacerbations of CB and COPD compared with standard therapy, in particular, with macrolides."( Moxifloxacin in the management of exacerbations of chronic bronchitis and COPD.
Miravitlles, M, 2007
)
2.5
"Moxifloxacin has a low propensity for causing phototoxic reactions relative to other fluoroquinolones, and animal data suggest that it has a low potential for causing excitatory CNS and hepatotoxic effects."( Moxifloxacin: a review of its clinical potential in the management of community-acquired respiratory tract infections.
Balfour, JA; Lamb, HM, 2000
)
2.47
"Moxifloxacin also has excellent penetration into upper and lower respiratory tissues."( Moxifloxacin, a new antibiotic designed to treat community-acquired respiratory tract infections: a review of microbiologic and pharmacokinetic-pharmacodynamic characteristics.
Nightingale, CH, 2000
)
2.47
"Moxifloxacin has a greater bactericidal rate as determined by regression of log CFU versus time data."( Streptococcus pneumoniae response to repeated moxifloxacin or levofloxacin exposure in a rabbit tissue cage model.
Bui, KQ; Mattoes, H; McNabb, J; Nicolau, DP; Nightingale, CH; Quintiliani, R; Xuan, D; Zhong, M, 2001
)
1.29
"Moxifloxacin also has excellent in vitro activity against strains resistant to penicillin, erythromycin, and other fluoroquinolones, such as levofloxacin."( Clinical perspectives on new antimicrobials: focus on fluoroquinolones.
Talan, DA, 2001
)
1.03
"Moxifloxacin thus has a unique drug interaction profile that is advantageous for its safe use."( Profile of moxifloxacin drug interactions.
Kubitza, D; Stass, H, 2001
)
1.42
"Moxifloxacin has an absolute bioavailability of 90% after oral administration and a mean elimination half-life of 12 hours."( Moxifloxacin: clinical efficacy and safety.
Culley, CM; Edwards, B; Klutman, N; Lacy, MK, 2001
)
2.47
"Moxifloxacin has good in vitro activity against common organisms associated with community and nosocomial infections, with the exception of enterococci, methicillin-resistant Staphylococcus aureus and ciprofloxacin-resistant gram-negative bacteria. "( In vitro activity of moxifloxacin against local bacterial isolates.
Ling, ML; Tan, PL, 2001
)
2.07
"Moxifloxacin has immunomodulatory activity through its capacity to alter the secretion of IL-1alpha and TNF-alpha by human monocytes."( Effect of moxifloxacin on secretion of cytokines by human monocytes stimulated with lipopolysaccharide.
Araujo, FG; Remington, JS; Slifer, TL, 2002
)
2.16
"Moxifloxacin has been developed to address many of these problems."( Improving care for patients with respiratory tract infections.
Garau, J; Lode, H, 2002
)
1.04

Actions

Moxifloxacin seems to inhibit the yeast to Hyphal morphogenesis by affecting signaling pathways. The drug had a much lower CR than other drugs and is therefore not recommended for the management of scrub typhus.

ExcerptReferenceRelevance
"Moxifloxacin had a much lower CR than other drugs and is, therefore, not recommended for the management of scrub typhus."( Evaluation of the Therapeutic Effect of Antibiotics on Scrub Typhus: A Systematic Review and Network Meta-Analysis.
Lu, D; Luo, Z; Qian, J; Wang, C; Wang, T; Ye, F; Zhang, J, 2022
)
1.44
"Moxifloxacin seems to inhibit the yeast to Hyphal morphogenesis by affecting signaling pathways."( The antibacterial agent, moxifloxacin inhibits virulence factors of Candida albicans through multitargeting.
Bansode, B; Gade, W; Jadhav, A; Karuppayil, SM; Kharat, K; Patil, R; Phule, D; Shelar, A, 2017
)
1.48
"Moxifloxacin caused an increase in the QTcI, with a lower bound of the 2-sided 95% CI always higher than 5 milliseconds, around the tmax of peak concentration, demonstrating assay sensitivity."( Evaluation of opicapone on cardiac repolarization in a thorough QT/QTc study.
Falcão, A; Homery, MC; l'Hostis, P; Nunes, T; Patat, A; Pinto, R; Rocha, JF; Soares-da-Silva, P, 2015
)
1.14

Treatment

Moxifloxacin-treated mice developed less pulmonary vascular permeability during pneumonia. Neither combination therapy nor examination of endothelial monolayer integrity in vitro supported direct barrier-stabilizing effects of moxifLoxacins. Moxif LoxacIN treatment exhibited a superior anti-biofilm effect.

ExcerptReferenceRelevance
"With moxifloxacin treatment, the mean (SD) time to improvement of symptoms was 3.0 (1.5), 3.4 (1.6) and 3.2 (1.5) days, and the time to resolution of symptoms was 4.8 (2.6) days, 5.7 (2.4) days and 5.5 (2.5) days, in the Asia Pacific, Europe and Middle East regions, respectively."( Characterisation of patients receiving moxifloxacin for acute bacterial rhinosinusitis in clinical practice: results from an international, observational cohort study.
Arvis, P; Desrosiers, M; Heldner, S; Mösges, R, 2013
)
1.11
"Moxifloxacin-treated mice developed less pulmonary vascular permeability during pneumonia, but neither combination therapy with moxifloxacin and ampicillin in vivo nor examination of endothelial monolayer integrity in vitro supported direct barrier-stabilizing effects of moxifloxacin."( Moxifloxacin is not anti-inflammatory in experimental pneumococcal pneumonia.
Berg, J; Gruber, AD; Gutbier, B; Hellwig, K; Hippenstiel, S; Hocke, AC; Kershaw, O; Mayer, K; Müller-Redetzky, HC; Neudecker, J; Opitz, B; Rückert, J; Suttorp, N; Wienhold, SM; Witzenrath, M, 2015
)
2.58
"Moxifloxacin-treated subjects (n = 4) were PCR negative within 1 week."( Time to eradication of Mycoplasma genitalium after antibiotic treatment in men and women.
Enger, M; Falk, L; Jensen, JS, 2015
)
1.14
"moxifloxacin treatment were estimated after adjusting for pre-treatment demographics, health care resource use and pneumonia-specific risk factors using propensity score and exact factor matching."( Hospital visits and costs following outpatient treatment of CAP with levofloxacin or moxifloxacin.
Fisher, AC; Grant, R; Gu, A; Mody, SH; Ng, D; Raut, M; Schein, J; Sengupta, A; Sheng Duh, M; Signorovitch, JE, 2010
)
1.31
"Moxifloxacin treatment was not associated with consistent changes in moxifloxacin susceptibility."( Pulsed moxifloxacin for the prevention of exacerbations of chronic obstructive pulmonary disease: a randomized controlled trial.
Jones, PW; Miravitlles, M; Rubinstein, E; Sethi, S; Theron, MS; Wedzicha, JA; Wilson, R, 2010
)
1.54
"Moxifloxacin treatment, on the other hand, exhibited a superior anti-biofilm activity and resulted in a 2.5- and 3.7-log reduction in the MRSA and MRSE bacterial bioburdens, respectively, after 24 h of exposure."( Pharmacodynamics of moxifloxacin versus vancomycin against biofilms of methicillin-resistant Staphylococcus aureus and epidermidis in an in vitro model.
Ahmed, GF; Elkhatib, WF; Noreddin, AM; Salem, AH, 2010
)
1.41
"In moxifloxacin-treated rats, an increase in the EDHF response was observed, which was largely attributed to SK(Ca)-activation."( The effect of levofloxacin and moxifloxacin on cardiovascular functions of rats with streptozotocin-induced diabetes.
Absi, M; Ghareeb, H; Khalil, A; Ruegg, UT, 2013
)
1.19
"Moxifloxacin treatment was associated with an improvement in survival in the SB animals (13 of 13 [100%] vs. "( The impact of mechanical ventilation on the moxifloxacin treatment of experimental pneumonia caused by Streptococcus pneumoniae.
Charles, PE; Chavanet, P; Croisier, D; Etienne, M; Lequeu, C; Piroth, L; Portier, H; Pugin, J, 2005
)
2.03
"All moxifloxacin treatment regimens were well tolerated. "( Effects of enteral feeding on the oral bioavailability of moxifloxacin in healthy volunteers.
Borner, K; Burkhardt, O; Stass, H; Thuss, U; Welte, T, 2005
)
1.13
"In moxifloxacin-treated mice, 75% survived infection compared to 10% of controls."( Effect of recombinant murine granulocyte colony-stimulating factor with or without fluoroquinolone therapy on mixed-infection abscesses in mice.
Gyssens, IC; Kullberg, BJ; Stearne, LE; Vonk, AG, 2005
)
0.84
"One moxifloxacin-treated patient had sustained monomorphic VT (> 30 s), and one levofloxacin-treated patient had torsade de pointes."( A randomized trial comparing the cardiac rhythm safety of moxifloxacin vs levofloxacin in elderly patients hospitalized with community-acquired pneumonia.
Anzueto, A; Choudhri, S; Dimarco, JP; Morganroth, J; Niederman, MS, 2005
)
1.05
"Moxifloxacin treatment protocols were significantly more effective on both ITT and PP analyses than the clarithromycin based protocols with only one exception (MAL vs."( High eradication rate of H. pylori with moxifloxacin-based treatment: a randomized controlled trial.
Bago, J; Bago, P; Marusić, M; Rozankovic, M; Tomic, M; Vcev, A, 2007
)
1.33
"Moxifloxacin treatment resulted in culture-negative vegetations in a total of 20 of 21 (95%) rats infected with P8, 10 of 11 (91%) rats infected with COL, and 19 of 24 (79%) rats infected with P8-4 (P < 0.05 compared to the results for the controls)."( Efficacies of moxifloxacin, ciprofloxacin, and vancomycin against experimental endocarditis due to methicillin-resistant Staphylococcus aureus expressing various degrees of ciprofloxacin resistance.
Entenza, JM; Glauser, MP; Moreillon, P; Que, YA; Vouillamoz, J, 2001
)
1.39
"Treatment with moxifloxacin was associated with rapid relief in symptoms, with 93.2% of patients experiencing either complete resolution of symptoms or improvement at follow-up."( Moxifloxacin in complicated skin and skin structure infections (cSSSIs): A prospective, international, non-interventional, observational study.
Arvis, P; Bogner, JR; Esguerra-Alcalen, M; Heldner, S; Kutaiman, A, 2013
)
2.17
"Eyes treated with moxifloxacin or moxifloxacin alternative formulation contained significantly fewer CFUs than untreated controls or besifloxacin-treated eyes with either treatment (P≤.0020)."( Penetration and effectiveness of prophylactic fluoroquinolones in experimental methicillin-sensitive or methicillin-resistant Staphylococcus aureus anterior chamber infections.
Balzli, CL; Caballero, AR; O'Callaghan, RJ; Tang, A; Weeks, AC, 2010
)
0.68
"Eyes treated with moxifloxacin/cholesterol had a significantly lower mean slit lamp examination (SLE) score than eyes treated with phosphate-buffered saline (PBS), moxifloxacin alone, or cholesterol alone (P ≤ 0.02). "( Moxifloxacin and cholesterol combined treatment of pneumococcal keratitis.
King, LB; Marquart, ME; Norcross, EW; Sanders, ME; Taylor, SD; Tolo, I; Tullos, NA, 2010
)
2.14
"Treatment with moxifloxacin resulted in savings of 266 euro and 381 euro for Germany and France respectively, primarily due to the shorter length of hospital stay."( An economic evaluation of sequential i.v./po moxifloxacin therapy compared to i.v./po co-amoxiclav with or without clarithromycin in the treatment of community-acquired pneumonia.
Becker, DL; Chancellor, JV; Drummond, MF; Duprat-Lomon, I; Hux, M; Kubin, R; Sagnier, PP, 2003
)
0.92
"Eyes treated with moxifloxacin healed faster and had smaller defects compared with those treated with gatifloxacin. "( The effect of fourth-generation fluoroquinolones gatifloxacin and moxifloxacin on epithelial healing following photorefractive keratectomy.
Bower, KS; Burka, JM; Howard, RS; Kuzmowych, CP; Stutzman, RD; Vanroekel, RC, 2005
)
0.9
"Treatment with moxifloxacin resulted in significant and sustained improvement."( Treatment of ankylosing spondylitis with moxifloxacin.
Ogrendik, M, 2007
)
0.95

Toxicity

Lefamulin was noninferior to moxifloxacin for the primary efficacy endpoints and was generally safe and well tolerated. gastrointestinal complaints were the most common adverse drug reactions (ADRs) associated with both formulations. No correlation or systematic relationship between adverse events and investigational gels was found. The cumulative frequency of ocular adverse events was similar between treatments.

ExcerptReferenceRelevance
" Safety and tolerability were assessed by evaluation of vital signs, electrocardiograms, electroencephalograms, clinical chemistry parameters, results of urinalysis, and adverse events."( Pharmacokinetics, safety, and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subjects.
Dalhoff, A; Kubitza, D; Schühly, U; Stass, H, 1998
)
0.53
" adverse effects on the central nervous and cardiovascular systems, phototoxicity, arthrotoxicity and oculotoxicity."( Preclinical safety evaluation of moxifloxacin, a novel fluoroquinolone.
Schlüter, G; von Keutz, E, 1999
)
0.58
" There were slightly more adverse events in the moxifloxacin group than in the cefuroxime axetil group, but there were fewer serious adverse events following moxifloxacin treatment (three vs."( A comparison of the safety and efficacy of moxifloxacin (BAY 12-8039) and cefuroxime axetil in the treatment of acute bacterial sinusitis in adults. The Sinusitis Study Group.
Bagger-Sjöbäck, D; Gehanno, P; Hampel, B; Ibanez, JM; Nikolaidis, P; Siegert, R; Sommerauer, B, 2000
)
0.83
" Reported adverse effects were primarily gastrointestinal (nausea, diarrhea) and were mild to moderate in severity."( Moxifloxacin: clinical efficacy and safety.
Culley, CM; Edwards, B; Klutman, N; Lacy, MK, 2001
)
1.75
" The adverse event profile was comparable between the three treatment groups."( The efficacy and safety of two oral moxifloxacin regimens compared to oral clarithromycin in the treatment of community-acquired pneumonia.
Hoeffken, G; Meyer, HP; Verhoef, L; Winter, J, 2001
)
0.59
" There was a low incidence of adverse events (10."( Efficacy and safety of short course (5-day) moxifloxacin vs 7-day ceftriaxone in the treatment of acute exacerbations of chronic bronchitis (AECB).
Casali, L; Curti, E; Grassi, C; Lazzaro, C; Schito, G; Tellarini, M, 2002
)
0.58
" Trovafloxacin recipients were also more than twice as likely to discontinue treatment due to adverse events than moxifloxacin-treated patients."( Comparison of the efficacy and safety of moxifloxacin and trovafloxacin for the treatment of acute, bacterial maxillary sinusitis in adults.
Arvis, P; Klossek, JM; Leberre, MA; Nikolaidis, P; Siegert, R, 2003
)
0.8
"The established safety profile of the fluoroquinolones has been disrupted in the past decade by the detection of low-frequency but potentially serious adverse events that have led to the license suspension, voluntary withdrawal, or restricted use of specific members of the class."( Safety profile of oral and intravenous moxifloxacin: cumulative data from clinical trials and postmarketing studies.
Ball, P; Choudhri, S; Kubin, R; Owens, R; Stahlmann, R, 2004
)
0.59
" Overall treatment-emergent adverse events for both drugs (mostly gastrointestinal) were mild to moderate in intensity."( Efficacy and safety of oral telithromycin once daily for 5 days versus moxifloxacin once daily for 10 days in the treatment of acute bacterial rhinosinusitis.
Ferguson, BJ; Guzzetta, RV; Hadley, JA; Spector, SL, 2004
)
0.56
" Drug-related adverse events occurred in 18."( Safety and efficacy of sequential i.v. to p.o. moxifloxacin versus conventional combination therapies for the treatment of community-acquired pneumonia in patients requiring initial i.v. therapy.
Choudhri, S; Fogarty, CM; Hamed, K; Katz, E; Larsen, LS; Song, J, 2004
)
0.58
" The primary endpoints included rates of treatment-emergent adverse events (all adverse events regardless of causality), drug-related adverse events, drug-related serious adverse events, deaths and premature discontinuations because of a treatment-emergent adverse event."( Retrospective analysis of the safety profile of oral moxifloxacin in elderly patients enrolled in clinical trials.
Andriole, VT; Choudhri, SH; Haverstock, DC, 2005
)
0.58
"Drug-related adverse event rates associated with oral moxifloxacin or the comparator therapy used in these studies did not significantly increase with advancing age."( Retrospective analysis of the safety profile of oral moxifloxacin in elderly patients enrolled in clinical trials.
Andriole, VT; Choudhri, SH; Haverstock, DC, 2005
)
0.83
" Safety evaluations included 72 h of digital continuous 12-lead Holter monitoring, 12-lead ECGs at baseline and at maximum serum concentration on day 3, and adverse events."( A randomized trial comparing the cardiac rhythm safety of moxifloxacin vs levofloxacin in elderly patients hospitalized with community-acquired pneumonia.
Anzueto, A; Choudhri, S; Dimarco, JP; Morganroth, J; Niederman, MS, 2005
)
0.57
" There were no statistically significant differences between the treatment groups with regard to drug-related adverse events."( Community-Acquired Pneumonia Recovery in the Elderly (CAPRIE): efficacy and safety of moxifloxacin therapy versus that of levofloxacin therapy.
Anzueto, A; Choudhri, SH; Heyder, A; Niederman, MS; Pearle, J; Restrepo, MI, 2006
)
0.56
"Intravenous/oral moxifloxacin therapy was efficacious and safe for hospitalized elderly patients with CAP, achieving > 90% cure in all severity and age subgroups, and was associated with faster clinical recovery than intravenous/oral levofloxacin therapy, with a comparable safety profile."( Community-Acquired Pneumonia Recovery in the Elderly (CAPRIE): efficacy and safety of moxifloxacin therapy versus that of levofloxacin therapy.
Anzueto, A; Choudhri, SH; Heyder, A; Niederman, MS; Pearle, J; Restrepo, MI, 2006
)
0.9
" These results indicate that moxifloxacin is a safe intravitreal antibiotic in mouse and rabbit animal models."( Intravitreal moxifloxacin: retinal safety study with electroretinography and histopathology in animal models.
Gao, H; Holz, ER; Iyer, MN; Mieler, WF; Pennesi, ME; Qiao, X; Wu, SM, 2006
)
0.99
" In addition, both drugs were well-tolerated in this trial, with the number of drug-related adverse events being comparable."( Efficacy and safety of intravenous moxifloxacin versus cefoperazone with azithromycin in the treatment of community acquired pneumonia.
Liu, H; Liu, J; Xiong, S; Xiong, W; Xu, S; Xu, Y; Zhao, J, 2006
)
0.61
"Moxifloxacin (250 microg/mL) seems to be safe as an additive agent for cornea storage media."( Efficacy and safety of moxifloxacin as an additive in Optisol-GS a preservation medium for corneal donor tissue.
Dahl, P; Hu, DN; Koplin, RS; McCormick, S; Meskin, SW; Ritterband, DC; Seedor, JA; Shah, MK; Shao, S; Shapiro, DE, 2006
)
2.09
" The incidence of at least one treatment-related adverse event (AE) in the azithromycin and moxifloxacin groups was 18."( Efficacy and safety of 3-day azithromycin versus 5-day moxifloxacin for the treatment of acute bacterial exacerbations of chronic bronchitis.
Amsden, GW; Martinez, FJ; Rothermel, CD; Treadway, G; Zervos, M, 2007
)
0.81
"Review of data from fluoroquinolone studies, with an emphasis on the associated rare, but potentially clinically important, adverse events in specific patient populations."( The safety profile of moxifloxacin and other fluoroquinolones in special patient populations.
Iannini, PB, 2007
)
0.65
"A literature search was conducted using terms including fluoroquinolones, moxifloxacin, ciprofloxacin, levofloxacin, gatifloxacin, gemifloxacin, safety, adverse events, drug interactions, and pharmacokinetic parameters to identify literature providing information regarding the safety profile of specified fluoroquinolones in special patient populations (i."( The safety profile of moxifloxacin and other fluoroquinolones in special patient populations.
Iannini, PB, 2007
)
0.89
"Fluoroquinolones, are associated with rare, but clinically important, adverse events in special patient populations (including the elderly; those with hepatic, renal, or glycemic disorders; and those at risk for cardiovascular events)."( The safety profile of moxifloxacin and other fluoroquinolones in special patient populations.
Iannini, PB, 2007
)
0.65
"In vitro cell cultures are useful for evaluating cell response to potentially toxic insults, although cell cultures may lack tissue components that may prevent or ameliorate damage in vivo."( Intrinsic cytotoxic effects of fluoroquinolones on human corneal keratocytes and endothelial cells.
Bezwada, P; Clark, LA; Schneider, S, 2008
)
0.35
" Possible toxic effects and median inhibitory concentration were evaluated after 24 hours as well as under conditions of oxidative stress."( In vitro safety of intravitreal moxifloxacin for endophthalmitis treatment.
Kampik, A; Kernt, M; Neubauer, AS; Ulbig, MW; Welge-Lüssen, U, 2008
)
0.63
"At concentrations higher than 150 microg/mL, moxifloxacin had adverse effects on primary RPE, ARPE19, and ONHA cell proliferation and viability."( In vitro safety of intravitreal moxifloxacin for endophthalmitis treatment.
Kampik, A; Kernt, M; Neubauer, AS; Ulbig, MW; Welge-Lüssen, U, 2008
)
0.89
" Intravitreal use of moxifloxacin up to this concentration may be safe and effective for the treatment of endophthalmitis."( In vitro safety of intravitreal moxifloxacin for endophthalmitis treatment.
Kampik, A; Kernt, M; Neubauer, AS; Ulbig, MW; Welge-Lüssen, U, 2008
)
0.95
" There are also concerns that there is currently no safe alternative to ciprofloxacin for patients with a nonintact eardrum."( Ototoxicity of topical moxifloxacin in a chinchilla animal model.
Akache, F; Daniel, SJ; Duval, M; Sahmkow, S, 2007
)
0.65
" No drug-related adverse effects were reported."( Safety of intracameral moxifloxacin for prophylaxis of endophthalmitis after cataract surgery.
Arbisser, LB, 2008
)
0.66
" No study-related adverse events occurred."( Evaluation of the safety of prophylactic intracameral moxifloxacin in cataract surgery.
Belani, S; Lane, SS; Masket, S; Osher, RH, 2008
)
0.59
"050 mL intracameral injection of moxifloxacin, which appears to be safe in the prophylaxis of endophthalmitis after cataract surgery."( Evaluation of the safety of prophylactic intracameral moxifloxacin in cataract surgery.
Belani, S; Lane, SS; Masket, S; Osher, RH, 2008
)
0.88
"Earlier this year, a 'Dear Doctor' letter was sent to Dutch health care professionals, describing the rare occurrence of fulminant hepatitis and the Stevens-Johnson syndrome or toxic epidermal necrolysis in patients using moxifloxacin."( [Novel side effects of moxifloxacin: making a balanced decision again].
Koopmans, RP; Prins, JM, 2008
)
0.84
" Computed tomography revealed interstitial lung fibrosis which was attributed to the toxic effects of nitrofurantoin (50 mg/d) that the patient used for approximately one year for recurrent urinary tract infection."( [Unwanted side effects of antibacterials--a diagnostic challenge].
Fux, R; Gleiter, CH; Mörike, K, 2008
)
0.35
" Global analysis did not reveal significantly higher incidences of drug-related adverse effects than for comparators."( Safety profile of the respiratory fluoroquinolone moxifloxacin: comparison with other fluoroquinolones and other antibacterial classes.
Tulkens, PM; Van Bambeke, F, 2009
)
0.61
" It is safe and effective for systemic and topical use, but only limited data are available on prophylactic intracameral administration to prevent endophthalmitis."( Intracameral moxifloxacin: in vitro safety on human ocular cells.
A, AK; Alge, CS; Eibl, KH; Kernt, M; Lackerbauer, CA; Liegl, RG; Neubauer, AS; Ulbig, MW, 2009
)
0.72
" Possible toxic effects of moxifloxacin (10-750 microg/mL) in corneal endothelial cells (CEC), primary human trabecular meshwork cells (TMC), and primary human retinal pigment epithelial (RPE) cells were evaluated after 24 hours and under conditions of oxidative and inflammatory stress by treatment with tumor necrosis factor alpha, lipopolysaccharides, or interleukin-6."( Intracameral moxifloxacin: in vitro safety on human ocular cells.
A, AK; Alge, CS; Eibl, KH; Kernt, M; Lackerbauer, CA; Liegl, RG; Neubauer, AS; Ulbig, MW, 2009
)
1.02
" The cumulative frequency of ocular adverse events was similar between treatments (12% and 14% with besifloxacin and moxifloxacin, respectively)."( Efficacy and safety of besifloxacin ophthalmic suspension 0.6% compared with moxifloxacin ophthalmic solution 0.5% for treating bacterial conjunctivitis.
Brunner, LS; Comstock, TL; Haas, W; McDonald, MB; Morris, TW; Paterno, MR; Protzko, EE; Usner, DW, 2009
)
0.79
" It is safe and effective for systemic and topical use; however, only very limited data are available on prophylactic intracameral administration to prevent endophthalmitis."( [Intracameral moxifloxacin: a safe option for endophthalmitis prophylaxis? In vitro safety profile for intraocular application].
de Kaspar, H; Eibl, KH; Hirneiss, C; Kampik, A; Kernt, M; Liegl, RG; Neubauer, AS; Ulbig, MW; Wolf, A, 2010
)
0.72
" Toxic effects were evaluated after 24 h (MTT assay and live-dead assay)."( [Intracameral moxifloxacin: a safe option for endophthalmitis prophylaxis? In vitro safety profile for intraocular application].
de Kaspar, H; Eibl, KH; Hirneiss, C; Kampik, A; Kernt, M; Liegl, RG; Neubauer, AS; Ulbig, MW; Wolf, A, 2010
)
0.72
" Primary RPEs, TMCs, LECs, and CECs showed adverse effects on proliferation and viability only at concentrations higher than 150 microg/ml moxifloxacin."( [Intracameral moxifloxacin: a safe option for endophthalmitis prophylaxis? In vitro safety profile for intraocular application].
de Kaspar, H; Eibl, KH; Hirneiss, C; Kampik, A; Kernt, M; Liegl, RG; Neubauer, AS; Ulbig, MW; Wolf, A, 2010
)
0.92
" Therefore, intracameral use of Vigamox at concentrations up to 150 microg/ml may be safe and effective for preventing endophthalmitis after intraocular surgery."( [Intracameral moxifloxacin: a safe option for endophthalmitis prophylaxis? In vitro safety profile for intraocular application].
de Kaspar, H; Eibl, KH; Hirneiss, C; Kampik, A; Kernt, M; Liegl, RG; Neubauer, AS; Ulbig, MW; Wolf, A, 2010
)
0.72
" Adverse event rates were comparable between treatment groups."( Efficacy and safety of sequential intravenous/oral moxifloxacin vs intravenous/oral amoxicillin/clavulanate for complicated skin and skin structure infections.
Amábile-Cuevas, CF; Arvis, P; Bogner, JR; Cruz-Alcázar, J; Hernández-Oliva, G; Reimnitz, P; Vick-Fragoso, R, 2009
)
0.6
" Fampridine was well tolerated, with a higher frequency of adverse events at the supratherapeutic dose."( Assessment of the cardiac safety of fampridine-SR sustained-release tablets in a thorough QT/QTc evaluation at therapeutic and supratherapeutic doses in healthy individuals.
Cardi, T; March, B, 2009
)
0.35
" Besifloxacin was well tolerated, with similar incidences of adverse events in the besifloxacin, vehicle, and moxifloxacin groups."( Efficacy and safety of besifloxacin ophthalmic suspension 0.6% in children and adolescents with bacterial conjunctivitis: a post hoc, subgroup analysis of three randomized, double-masked, parallel-group, multicenter clinical trials.
Comstock, TL; Paterno, MR; Pichichero, ME; Usner, DW, 2010
)
0.57
"6% was shown to be safe and effective for the treatment of bacterial conjunctivitis in children and adolescents aged 1-17 years."( Efficacy and safety of besifloxacin ophthalmic suspension 0.6% in children and adolescents with bacterial conjunctivitis: a post hoc, subgroup analysis of three randomized, double-masked, parallel-group, multicenter clinical trials.
Comstock, TL; Paterno, MR; Pichichero, ME; Usner, DW, 2010
)
0.36
"4 mm at 6 weeks and 3 months and any adverse events were determined."( Efficacy and safety of adjunctive local moxifloxacin delivery in the treatment of periodontitis.
Beikler, T; Flemmig, TF; Gravemeier, M; Mross, D; Petersilka, G; Prior, K; Völp, A; Yamamoto, J; Zilly, M, 2011
)
0.64
" No correlation or systematic relationship between adverse events, including bacterial resistance against moxifloxacin, and the investigational gels was found."( Efficacy and safety of adjunctive local moxifloxacin delivery in the treatment of periodontitis.
Beikler, T; Flemmig, TF; Gravemeier, M; Mross, D; Petersilka, G; Prior, K; Völp, A; Yamamoto, J; Zilly, M, 2011
)
0.85
" Rates of adverse events were lower in moxifloxacin- than in clindamycin-treated patients."( Comparative efficacy and safety of moxifloxacin and clindamycin in the treatment of odontogenic abscesses and inflammatory infiltrates: a phase II, double-blind, randomized trial.
Böger, RH; Cachovan, G; Giersdorf, I; Haddad, M; Hallier, O; Platzer, U; Schön, G; Sobottka, I; Streichert, T; Wegscheider, K, 2011
)
0.92
" Two patients (11%) experienced three adverse effects [one nausea, another increased aspartate aminotransferase (AST) and alanine aminotransferase (ALT)], but the events were not serious."( Efficacy and safety of moxifloxacin for community-acquired bacterial pneumonia based on pharmacokinetic analysis.
Fukano, H; Hara, H; Kawanishi, M; Kimura, M; Kishimoto, M; Matsushima, T; Moriya, O; Niki, Y; Okimoto, N; Yoneyama, H; Yoshida, K, 2011
)
0.68
" There was no difference in adverse events or toxicities between the groups."( Efficacy and safety of moxifloxacin as antibacterial prophylaxis for patients receiving autologous haematopoietic stem cell transplantation: a randomised trial.
Arenz, D; Böll, B; Bredenfeld, H; Chemnitz, J; Cornely, OA; Cremer, B; Hallek, M; Kaul, I; Klein, F; Mahne, M; Moritz, G; Scheid, C; Vehreschild, JJ; Vehreschild, MJ; Wassmer, G, 2012
)
0.69
" No study-related adverse events were noted."( Safety of prophylactic intracameral moxifloxacin use in cataract surgery.
Aslan, BS; Ekinci Koktekir, B, 2012
)
0.65
"050 mL intracameral injection of moxifloxacin, which appears to be safe in the prophylaxis of endophthalmitis after cataract surgery."( Safety of prophylactic intracameral moxifloxacin use in cataract surgery.
Aslan, BS; Ekinci Koktekir, B, 2012
)
0.94
"Treatments that offer two medications in a fixed combination have the potential to offer efficacious and safe treatment with advantages such as a regimen that is simpler than administering two separate solutions."( Safety and efficacy of moxifloxacin-dexamethasone eyedrops as treatment for bacterial ocular infection associated with bacterial blepharitis.
Bartell, J; Belfort, R; Bell, B; Clark, L; Gabriel, L; Höfling-Lima, AL; Martins Bispo, PJ; Muccioli, C; Stroman, DW; Zacharias Serapicos, PC, 2012
)
0.69
" Both regimens were safe and well tolerated."( Safety and efficacy of moxifloxacin-dexamethasone eyedrops as treatment for bacterial ocular infection associated with bacterial blepharitis.
Bartell, J; Belfort, R; Bell, B; Clark, L; Gabriel, L; Höfling-Lima, AL; Martins Bispo, PJ; Muccioli, C; Stroman, DW; Zacharias Serapicos, PC, 2012
)
0.69
"Crude incidences and relative risk estimates (Mantel-Haenszel analysis) of patients with any adverse event (AE), adverse drug reaction (ADR), serious AE (SAE), serious ADR (SADR), treatment discontinuation due to an AE or ADR, and fatal outcomes related to an AE or ADR."( Moxifloxacin safety: an analysis of 14 years of clinical data.
Arvis, P; Kruesmann, F; Tulkens, PM, 2012
)
1.82
" Vigamox(®) containing moxifloxacin and Tosuflo(®) containing tosufloxacin were more toxic when compared with the other antibiotics."( In vitro assessment of the cytotoxicity of six topical antibiotics to four cultured ocular surface cell lines.
Ayaki, M; Iwasawa, A; Niwano, Y, 2012
)
0.69
" Treatment-emergent cardiac adverse event (AE) rates were similar for moxifloxacin and comparators in PO (6."( Update on the cardiac safety of moxifloxacin.
Arvis, P; Fritsch, A; Haverkamp, W; Kruesmann, F; van Veenhuyzen, D, 2012
)
0.9
" A similar proportion of patients (ITT population) experienced any adverse events in both treatment groups (MXF: 30."( Efficacy and safety of IV/PO moxifloxacin and IV piperacillin/tazobactam followed by PO amoxicillin/clavulanic acid in the treatment of diabetic foot infections: results of the RELIEF study.
Alder, J; Arvis, P; Dryden, M; Gyssens, IC; Kujath, P; Nathwani, D; Reimnitz, P; Schaper, NC, 2013
)
0.68
"3%) patients had treatment-emergent adverse events (TEAEs) and 4 (0."( Efficacy and safety of moxifloxacin in acute exacerbations of chronic bronchitis: a prospective, multicenter, observational study (AVANTI).
Chuchalin, A; Dokic, D; Marschall, HP; Petri, T; Tokić, M; Zakharova, M, 2013
)
0.7
"Peroperative intracameral moxifloxacin injection for endophthalmitis prophylaxis is a safe and effective method in uncomplicated phacoemulsification surgery."( Ocular pharmacokinetics, safety and efficacy of intracameral moxifloxacin 0.5% solution in a rabbit model.
Akova, YA; Asena, L; Bozkurt, A; Demiralay, E; Goktaş, MT; Karabay, G; Yaşar, U, 2013
)
0.93
" QTcI was not affected by plasma concentrations of cangrelor metabolites, and cangrelor had no other adverse effects on electrocardiographic parameters."( Electrocardiographic safety of cangrelor, a new intravenous antiplatelet agent: a randomized, double-blind, placebo- and moxifloxacin-controlled thorough QT study.
Bellibas, SE; Green, CL; Krucoff, MW; Lambe, L; Prats, J; Whellan, DJ; Wijngaard, P, 2013
)
0.6
" MFLX is effective and safe in patients with NHCAP."( [Efficacy and safety of moxifloxacin in patients with nursing and healthcare-associated pneumonia].
Akata, K; Awaya, Y; Choujin, Y; Inoue, N; Ishimoto, H; Kawajiri, T; Kawanami, Y; Kawanaml, T; Mukae, H; Nagata, S; Nishida, C; Noguchi, S; Obata, H; Ogoshi, T; Orihashi, T; Suzuki, Y; Taura, Y; Tokuyama, S; Yamasaki, K; Yatera, K; Yoshida, Y; Yoshii, C, 2013
)
0.7
" The primary safety endpoint was the incidence of treatment-emergent adverse events (TEAEs)."( Safety of besifloxacin ophthalmic suspension 0.6% in cataract and LASIK surgery patients.
Clinch, TE; Majmudar, PA, 2014
)
0.4
" Our study aimed to assess whether moxifloxacin in comparison to levofloxacin plus metronidazole are effective and safe in the treatment of community-acquired pneumonia with aspiration factors."( Clinical efficacy and safety of moxifloxacin versus levofloxacin plus metronidazole for community-acquired pneumonia with aspiration factors.
Li, F; Liu, Y; Pu, C; Ren, X; Ren, Y; Sui, DJ; Sun, L; Sun, T; Wang, R; Yang, Z, 2014
)
0.96
" The overall adverse event rate was 10."( Clinical efficacy and safety of moxifloxacin versus levofloxacin plus metronidazole for community-acquired pneumonia with aspiration factors.
Li, F; Liu, Y; Pu, C; Ren, X; Ren, Y; Sui, DJ; Sun, L; Sun, T; Wang, R; Yang, Z, 2014
)
0.69
"Moxifloxacin is effective and safe for treatment of community-acquired pneumonia with aspiration factors."( Clinical efficacy and safety of moxifloxacin versus levofloxacin plus metronidazole for community-acquired pneumonia with aspiration factors.
Li, F; Liu, Y; Pu, C; Ren, X; Ren, Y; Sui, DJ; Sun, L; Sun, T; Wang, R; Yang, Z, 2014
)
2.13
" The proportion of patients experiencing any treatment-emergent adverse events was slightly higher with moxifloxacin (67."( Efficacy and safety of moxifloxacin in hospitalized patients with secondary peritonitis: pooled analysis of four randomized phase III trials.
Alder, J; Arvis, P; De Waele, JJ; Hussain, T; Kruesmann, F; Solomkin, JS; Tellado, JM; Weiss, G, 2014
)
0.93
"9%) patients had treatment-emergent adverse events (TEAEs) and 40 (1."( Efficacy and safety of moxifloxacin in community acquired pneumonia: a prospective, multicenter, observational study (CAPRIVI).
Bezlepko, A; Iudina, L; Kondova Topuzovska, I; Kuzman, I; Marschall, HP; Petri, T; Rókusz, L, 2014
)
0.71
"In the present study, there was no adverse effect associated with intracameral injection of 150-500 μg/mL MFLX."( Safety of intracameral injection of moxifloxacin using total replacement technique (bag and chamber flushing).
Gotou, T; Inoue, Y; Matsuura, K; Odawara, S; Sasaki, S; Suto, C, 2014
)
0.68
" Except in 1 child with hepatotoxicity, all adverse effects were mild and nonpersistent."( Pharmacokinetics and safety of moxifloxacin in children with multidrug-resistant tuberculosis.
Castel, S; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Schaaf, HS; Thee, S; Wiesner, L, 2015
)
0.7
" It highlights available intracameral antibiotics with respect to pharmacology, spectrum of activity, dosage and preparation, safety, and efficacy profiles, as well as toxic anterior segment syndrome risks to better define the potential use of these medications in the prevention of endophthalmitis."( Intracameral antibiotics: Safety, efficacy, and preparation.
Braga-Mele, R; Chang, DF; Henderson, BA; Mamalis, N; Talley-Rostov, A; Vasavada, A, 2014
)
0.4
" The results also inspired us to think about a "supplementary regimen" to increase safety and decrease the adverse effect in the treatment of corneal infections."( The effect of resveratrol on protecting corneal epithelial cells from cytotoxicity caused by moxifloxacin and benzalkonium chloride.
Chen, RH; Chen, TC; Hu, FR; Su, MJ; Tsai, TH; Tsai, TY; Wang, IJ; Yeh, CY, 2015
)
0.64
" We also assessed safety and tolerability by monitoring adverse events."( Efficiency and safety of the combination of moxifloxacin, pretomanid (PA-824), and pyrazinamide during the first 8 weeks of antituberculosis treatment: a phase 2b, open-label, partly randomised trial in patients with drug-susceptible or drug-resistant pul
Burger, DA; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Eisenach, K; Everitt, D; Ive, P; Mendel, CM; Ntinginya, NE; Page-Shipp, L; Pym, A; Reither, K; Schall, R; Spigelman, M; van Niekerk, C; Variava, E; Venter, A; von Groote-Bidlingmaier, F, 2015
)
0.68
" Frequencies of adverse events were similar to standard treatment in all groups."( Efficiency and safety of the combination of moxifloxacin, pretomanid (PA-824), and pyrazinamide during the first 8 weeks of antituberculosis treatment: a phase 2b, open-label, partly randomised trial in patients with drug-susceptible or drug-resistant pul
Burger, DA; Conradie, A; Dawson, R; Diacon, AH; Donald, PR; Eisenach, K; Everitt, D; Ive, P; Mendel, CM; Ntinginya, NE; Page-Shipp, L; Pym, A; Reither, K; Schall, R; Spigelman, M; van Niekerk, C; Variava, E; Venter, A; von Groote-Bidlingmaier, F, 2015
)
0.68
" Safety was assessed by the incidence of ocular and nonocular treatment-emergent adverse events (AEs), changes in visual acuity, and biomicroscopy and ophthalmoscopy findings."( Clinical and Antibacterial Efficacy and Safety of Besifloxacin Ophthalmic Suspension Compared With Moxifloxacin Ophthalmic Solution.
Comstock, TL; Garg, P; Mathur, U; Morris, TW; Sony, P; Tandon, R,
)
0.35
"5 % moxifloxacin can be safely injected intracamerally following cataract surgery without additional postoperative antibiotic prophylaxis to prevent endophthalmitis without adverse effects on patient outcomes."( Safety of undiluted intracameral moxifloxacin without postoperative topical antibiotics in cataract surgery.
Ambati, BK; Messenger, WB; Sargent, S; Zhou, AX, 2016
)
1.27
" 43 (10%) of 155 treatment-emergent adverse events in the solithromycin group and 54 (13%) of 154 such events in the moxifloxacin group were deemed to be related to study drug."( Efficacy and safety of oral solithromycin versus oral moxifloxacin for treatment of community-acquired bacterial pneumonia: a global, double-blind, multicentre, randomised, active-controlled, non-inferiority trial (SOLITAIRE-ORAL).
Antonovsky, Y; Barrera, CM; Clark, K; Das, AF; Doreski, PA; Fernandes, P; Flores-Figueroa, J; Horwith, G; Jamieson, B; Karimjee, N; Keedy, K; Metev, H; Mitha, I; Molina, JM; Mykietiuk, A; Nitu, MF; Oldach, D; Rewerska, B; Rowe, BH; Scott, D; Sheets, A; Tanaseanu, CM; Van Rensburg, DJ, 2016
)
0.89
" Mostly mild/moderate infusion events led to higher incidence of adverse events overall in the solithromycin group."( SOLITAIRE-IV: A Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of Intravenous-to-Oral Solithromycin to Intravenous-to-Oral Moxifloxacin for Treatment of Community-Acquired Bacterial Pneumonia.
Das, AF; Fernandes, P; File, TM; Gonong, JRV; Jamieson, BD; Keedy, K; Oldach, D; Rewerska, B; Sheets, A; Taylor, D; Vucinic-Mihailovic, V, 2016
)
0.63
" Efficacy (by intention to treat) was analyzed using the inverse variance method; safety data were recorded as the occurrence of any adverse event."( Efficacy and Safety of Quinolone-Containing Rescue Therapies After the Failure of Non-Bismuth Quadruple Treatments for Helicobacter pylori Eradication: Systematic Review and Meta-Analysis.
Gisbert, JP; Marin, AC; McNicholl, AG; Nyssen, OP, 2017
)
0.46
"989), demonstrating that adding moxifloxacin to the recommended regimen does not cause more adverse events during TB treatment."( Moxifloxacin is an effective and safe candidate agent for tuberculosis treatment: a meta-analysis.
Chen, H; Chen, S; Wang, F; Wu, M; Xu, J; Xu, P; Zhu, X, 2017
)
2.18
"Current practice methods are unclear as to the most safe and effective prophylactic pharmacotherapy and method of delivery to reduce postoperative endophthalmitis occurrence."( Comparative analysis of the safety and efficacy of intracameral cefuroxime, moxifloxacin and vancomycin at the end of cataract surgery: a meta-analysis.
Ambati, BK; Bardsley, T; Bondalapati, S; Bowen, RC; Evans, PR; Greene, T; Kliethermes, M; Lawyer, TW; Mamalis, CA; McFarland, M; Rudnisky, CJ; Shi, D; Snow, KB; Zhou, AX, 2018
)
0.71
" Although rare, vancomycin was associated with toxic retinal events."( Comparative analysis of the safety and efficacy of intracameral cefuroxime, moxifloxacin and vancomycin at the end of cataract surgery: a meta-analysis.
Ambati, BK; Bardsley, T; Bondalapati, S; Bowen, RC; Evans, PR; Greene, T; Kliethermes, M; Lawyer, TW; Mamalis, CA; McFarland, M; Rudnisky, CJ; Shi, D; Snow, KB; Zhou, AX, 2018
)
0.71
" Safety variables included adverse events (AEs), lisamine green, fluorescein ocular surface stains, and clinical signs of tolerability."( Efficacy and Safety of 0.6% Pazufloxacin Ophthalmic Solution Versus Moxifloxacin 0.5% and Gatifloxacin 0.5% in Subjects with Bacterial Conjunctivitis: A Randomized Clinical Trial.
Baiza-Durán, L; Casillas-Magallanes, M; Gómez-Bastar, PA; González-Lomelí, M; Lizárraga-Corona, A; Mercado-Sesma, AR; Montoya-Sánchez, IM; Mora-González, A; Ochoa-Tabares, JC; Olvera-Montaño, O; Oregon-Miranda, AA; Orozco-Carroll, M; Páez-Garza, JH; Pérez-Balbuena, AL; Sandoval-Delgadillo, LI; Saucedo-Rodríguez, LR; Villanueva-Najera, MA, 2018
)
0.72
" Patient demographics, clinical characteristics, indication for moxifloxacin use, and adverse events (AEs) were extracted via chart review."( Safety and Tolerability of Moxifloxacin in Children.
Dixit, A; Jones, S; Karandikar, MV; Nakamura, MM, 2018
)
1.02
"All grade 3 & 4 adverse events (AEs) and their relationship to treatment for patients who had taken at least one dose of therapy in the REMoxTB clinical trial were recorded."( Toxicity associated with tuberculosis chemotherapy in the REMoxTB study.
Amukoye, EI; Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; Hanekom, M; McHugh, TD; Mendel, CM; Meredith, SK; Murphy, ME; Murthy, SE; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD; Wills, GH, 2018
)
0.48
" The most common adverse events on standard therapy related to hepatobiliary, musculoskeletal and metabolic disorders."( Toxicity associated with tuberculosis chemotherapy in the REMoxTB study.
Amukoye, EI; Crook, AM; Dawson, R; Diacon, AH; Gillespie, SH; Hanekom, M; McHugh, TD; Mendel, CM; Meredith, SK; Murphy, ME; Murthy, SE; Nunn, AJ; Phillips, PPJ; Singh, KP; Spigelman, M; Tweed, CD; Wills, GH, 2018
)
0.48
" There were few differences in the frequency of adverse effects between the two groups."( Effectiveness and safety of the pre-prescription of garenoxacin in comparison to moxifloxacin for low-risk febrile neutropenia in breast cancer patients undergoing adjuvant and neoadjuvant chemotherapy.
Asano, Y; Kashiwagi, S; Nagayama, K; Noda, S; Ogawa, K; Ohira, M; Onoda, N; Takahashi, K; Takahashi, M; Takashima, T, 2019
)
0.74
" Adverse events related to moxifloxacin were mild or moderate in intensity and showed no correlation with increased weight-adjusted doses."( Pharmacokinetics, Safety, and Tolerability of Single-Dose Intravenous Moxifloxacin in Pediatric Patients: Dose Optimization in a Phase 1 Study.
Arrieta, AC; Bradley, JS; James, LP; Lettieri, J; Stass, H; Sullivan, JE; Vanevski, KM; Willmann, S, 2019
)
1.04
" No ocular or systemic study-related adverse events were observed."( Safety and efficacy of intracameral moxifloxacin for prevention of post-cataract endophthalmitis: Randomized controlled clinical trial.
Alves, M; Assis Filho, HL; Cardoso da Silva, I; Cavalcanti Lira, RP; Dias Freire, LM; Ferreira, BG; Leite Arieta, CE; Martini, AAF; Melega, MV; Pedreira Chaves, FR; Reis, RD, 2019
)
0.79
"Lefamulin was noninferior to moxifloxacin for the primary efficacy endpoints and was generally safe and well tolerated."( Efficacy and Safety of Intravenous-to-oral Lefamulin, a Pleuromutilin Antibiotic, for the Treatment of Community-acquired Bacterial Pneumonia: The Phase III Lefamulin Evaluation Against Pneumonia (LEAP 1) Trial.
Das, A; File, TM; Gasink, LB; Gelone, SP; Goldberg, L; Paukner, S; Saviski, J; Seltzer, E; Sweeney, C; Talbot, GH; Wicha, WW, 2019
)
0.81
" We aimed to examine fluoroquinolone (ciprofloxacin, levofloxacin and moxifloxacin) associated aortic aneurysm or dissection through data mining of the US Food and Drug Administration Adverse Event Reporting System (FAERS)."( Assessing fluoroquinolone-associated aortic aneurysm and dissection: Data mining of the public version of the FDA adverse event reporting system.
Huang, H; Huang, J; Jia, Y; Meng, L; Qiu, F; Sun, S, 2019
)
0.75
" Pharmacovigilance tools were used for quantitative detection of signals that is, drug-associated adverse events, including reporting odds ratio, proportional reporting ratio, information component given by a Bayesian confidence propagation neural network and empirical Bayes geometric mean."( Assessing fluoroquinolone-associated aortic aneurysm and dissection: Data mining of the public version of the FDA adverse event reporting system.
Huang, H; Huang, J; Jia, Y; Meng, L; Qiu, F; Sun, S, 2019
)
0.51
"Based on 3721 adverse event reports, all three fluoroquinolones are associated with aortic aneurysm, and levofloxacin is associated with aortic dissection."( Assessing fluoroquinolone-associated aortic aneurysm and dissection: Data mining of the public version of the FDA adverse event reporting system.
Huang, H; Huang, J; Jia, Y; Meng, L; Qiu, F; Sun, S, 2019
)
0.51
" Patients were followed up for sputum smear and culture conversion and adverse events during the treatment."( Early efficacy and safety of Bedaquiline and Delamanid given together in a "Salvage Regimen" for treatment of drug-resistant tuberculosis.
Khalid, UK; Mathuria, KK; Munjal, SK; Myneedu, VP; Puri, MM; Sarin, R; Singla, N; Singla, R; Verma, A; Vohra, V, 2019
)
0.51
" 29 adverse events (AE) were reported among 17 patients and there were 11 deaths."( Early efficacy and safety of Bedaquiline and Delamanid given together in a "Salvage Regimen" for treatment of drug-resistant tuberculosis.
Khalid, UK; Mathuria, KK; Munjal, SK; Myneedu, VP; Puri, MM; Sarin, R; Singla, N; Singla, R; Verma, A; Vohra, V, 2019
)
0.51
"BDQ and DLM given together in a salvage regimen is efficacious with low rate of adverse events."( Early efficacy and safety of Bedaquiline and Delamanid given together in a "Salvage Regimen" for treatment of drug-resistant tuberculosis.
Khalid, UK; Mathuria, KK; Munjal, SK; Myneedu, VP; Puri, MM; Sarin, R; Singla, N; Singla, R; Verma, A; Vohra, V, 2019
)
0.51
" Pooled safety data across both studies suggested that the safety profile of odanacatib at high exposures was similar to placebo, with a small clustering of oral cavity adverse events."( Thorough QTc Evaluation and the Safety of Supratherapeutic Doses of Odanacatib in Healthy Subjects.
Brandquist, C; Chakravarthy, M; Gutierrez, M; Liu, C; Liu, F; Mahon, C; McCrea, J; Mostoller, K; Panebianco, D; Stoch, SA; Zajic, S, 2019
)
0.51
" The use of IC-Mox (250 μg) for endophthalmitis prophylaxis appears to be safe in the pediatric population."( Safety of intracameral moxifloxacin in the pediatric population: an equivalence study.
Ali, A; Imtirat, A; Khalili, S; Mireskandari, K; Tehrani, N; Williams, S, 2020
)
0.87
"This meta-analysis revealed that the addition of moxifloxacin to the recommended regimen significantly improved the rate of treatment success in the treatment of MDR-TB, with no additional adverse moxifloxacin events."( Meta-analysis on Effectiveness and Safety of Moxifloxacin in Treatment of Multidrug Resistant Tuberculosis in Adults.
Guan, Y; Liu, Y, 2020
)
1.07
" Safety evaluations included treatment-emergent adverse events and laboratory measures."( Safety and efficacy of omadacycline by body mass index in patients with community-acquired bacterial pneumonia: Subanalysis from a randomized controlled trial.
Chitra, S; McGovern, P; Pai, MP; Wilcox, M, 2021
)
0.62
" Common adverse effects are gastrointestinal symptoms, headache, dizziness, etc."( Moxifloxacin-induced oral erythema multiforme: An unusual adverse effect hitherto unreported.
Das, S; Mallick, S; Rudra, O; Sharma, S,
)
1.57
"Quinolones comprise a class of antibiotics that are globally preferred for treating a wide range of bacterial infections due to their potency, broad coverage, favorable pharmacologic profile, and mostly mild to moderate adverse reactions."( Systemic quinolones and risk of retinal detachment I: analysis of data from the US FDA adverse event reporting system.
Alami, A; Bjerre, LM; Gravel, CA; Krewski, D; Mattison, D; Momoli, F; Taher, MK; Tsui, D, 2022
)
0.72
" The outcomes of interest were culture conversion and incidence of adverse events."( Efficacy and safety of daily treatments for drug-susceptible pulmonary tuberculosis: a systematic review and network meta-analysis.
Beraldi-Magalhães, F; Fernandez-Llimos, F; Imazu, P; Pontarolo, R; Santos, JM; Tonin, FS, 2022
)
0.72
" The use of rifapentine 450 mg instead of rifampicin in the standard regimen demonstrated to be statistically safer than all other options for serious adverse events (e."( Efficacy and safety of daily treatments for drug-susceptible pulmonary tuberculosis: a systematic review and network meta-analysis.
Beraldi-Magalhães, F; Fernandez-Llimos, F; Imazu, P; Pontarolo, R; Santos, JM; Tonin, FS, 2022
)
0.72
"The WHO standard regimen remains an overall effective and safe alternative for DS-TB."( Efficacy and safety of daily treatments for drug-susceptible pulmonary tuberculosis: a systematic review and network meta-analysis.
Beraldi-Magalhães, F; Fernandez-Llimos, F; Imazu, P; Pontarolo, R; Santos, JM; Tonin, FS, 2022
)
0.72
" All adverse events were mild to moderate in severity, and no deaths occurred."( A Randomized, Double-Blind, Parallel Design Thorough QT Study With a Nested Crossover to Compare the Cardiac Safety of Amiselimod With Placebo and Positive Control in Healthy Volunteers.
Franklin, H; Israel, RJ; Lee, J; Lester, R; Lowe, ER; O'Reilly, T; Slatkin, NE, 2023
)
0.91
"Dropless cataract regime was found to be an effective and safe alternative that was easy to administer."( Efficacy and safety of intravitreal injection of triamcinolone-moxifloxacin after cataract surgery in a low to middle income country - a one-year audit.
Jeeva, IK; Masud, S; Siddiqui, MAR, 2023
)
1.15
" A multidisciplinary team reviewed all adverse events and determined their relationship with moxifloxacin."( Safety study of moxifloxacin in children with severe refractory Mycoplasma pneumoniae pneumonia.
He, YS; Ji, J; Liu, G; Qian, SY; Yang, M, 2023
)
1.48
" As for the adverse events, 11 patients in moxifloxacin group were deemed to be doubtfully related and one possibly related to moxifloxacin; in the azithromycin group, four patients were regarded to be doubtfully related to azithromycin and one not related."( Safety study of moxifloxacin in children with severe refractory Mycoplasma pneumoniae pneumonia.
He, YS; Ji, J; Liu, G; Qian, SY; Yang, M, 2023
)
1.52
"Moxifloxacin was well tolerated and safe for treating SRMPP in children."( Safety study of moxifloxacin in children with severe refractory Mycoplasma pneumoniae pneumonia.
He, YS; Ji, J; Liu, G; Qian, SY; Yang, M, 2023
)
2.7
"Linezolid is an effective, but toxic anti-tuberculosis drug that is currently recommended for the treatment of drug-resistant tuberculosis."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91
"DECODE is an innovative dose-finding trial, designed to support exposure-response modelling for safe and effective dose selection."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
0.91

Pharmacokinetics

The median maximum serum concentration (Cmax), area under the curve from 0-8 hours (AUC0-8), time until Cmax (Tmax), and half-life for moxifloxacin were 3. Changes in QTcF mirrored the pharmacokinetic changes, and there was a linear relationship between plasma concentration of mox iflxacin and change in QtcF.

ExcerptReferenceRelevance
" The pharmacodynamic data demonstrated that BAY 12-8039 has marked activity against gram-positive and gram-negative organisms (under both anaerobic and aerobic conditions) and anaerobes."( Pharmacodynamic properties of BAY 12-8039 on gram-positive and gram-negative organisms as demonstrated by studies of time-kill kinetics and postantibiotic effect.
Andrews, JM; Boswell, FJ; Wise, R, 1997
)
0.3
" Within 4 to 5 h they fell to about 30 to 55% of the Cmax, and thereafter a terminal half-life of 11 to 14 h accounted for the major part of the area under the concentration-time curve (AUC)."( Pharmacokinetics, safety, and tolerability of ascending single doses of moxifloxacin, a new 8-methoxy quinolone, administered to healthy subjects.
Dalhoff, A; Kubitza, D; Schühly, U; Stass, H, 1998
)
0.53
" The plasma concentration vs time courses of the unchanged compound (determined by HPLC) and the derived pharmacokinetic parameters were used to evaluate the absorption process, to compare the pharmacokinetics in these species and to perform an interspecies scaling."( Pharmacokinetics of the 8-methoxyquinolone, moxifloxacin: a comparison in humans and other mammalian species.
Domdey-Bette, A; Henninger, K; Hucke, F; Kohlsdorfer, C; Siefert, HM; Stass, HH, 1999
)
0.56
" The AUC for both formulations was comparable with bioequivalence criteria fulfilled, with Cmax after oral treatment approximately 31% lower."( Pharmacokinetics and elimination of moxifloxacin after oral and intravenous administration in man.
Kubitza, D; Stass, H, 1999
)
0.58
" Standard pharmacokinetic parameters were estimated by noncompartmental methods."( Pharmacokinetics of a once-daily oral dose of moxifloxacin (Bay 12-8039), a new enantiomerically pure 8-methoxy quinolone.
Agarwal, V; Heller, AH; Krol, GJ; Leese, PT; Lettieri, J; Sullivan, JT; Watson, S; Woodruff, M, 1999
)
0.56
" The pharmacodynamic parameters AUC/MIC, T > MIC, (AUC > MIC)/MIC (AUC = area under the curve, T = time) and WAUC ((AUC/MIC) (T > MIC/100)) (WAUC = weighted area under the curve) were related to AUBKC(24) and AUBKC(48) using an inhibitory sigmoid E(max) model."( Exploration of the in-vitro pharmacodynamic activity of moxifloxacin for Staphylococcus aureus and Streptococci of lancefield groups A and G.
Bowker, KE; Holt, HA; MacGowan, AP; Wootton, M, 1999
)
0.55
"2 mg/L, area under the curve (AUC) 37 mg x hour/L, and terminal elimination half-life 12."( Moxifloxacin, a new antibiotic designed to treat community-acquired respiratory tract infections: a review of microbiologic and pharmacokinetic-pharmacodynamic characteristics.
Nightingale, CH, 2000
)
1.75
" With each organism, a series of monoexponential pharmacokinetic profiles of single doses of moxifloxacin (T:1/2 = 12."( Comparative pharmacodynamics of moxifloxacin and levofloxacin in an in vitro dynamic model: prediction of the equivalent AUC/MIC breakpoints and equiefficient doses.
Firsov, AA; Kononenko, OV; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2000
)
0.81
"The aim of the present investigation was to study and compare the killing activity of two new fluoroquinolone compounds, moxifloxacin and grepafloxacin, and a new generation macrolide, clarithromycin, against three clinical isolates of Streptococcus pneumoniae (penicillin-susceptible, -intermediate and -resistant) and two Streptococcus pyogenes (erythromycin-susceptible and -resistant) strains by simulating their human pharmacokinetics in a pharmacodynamic model."( Bactericidal activity of moxifloxacin compared to grepafloxacin and clarithromycin against Streptococcus pneumoniae and Streptococcus pyogenes investigated using an in vitro pharmacodynamic model.
Esposito, S; Ianniello, F; Noviello, S, 2000
)
0.82
"An in vitro pharmacokinetic model was used to compare the pharmacodynamics of moxifloxacin and levofloxacin against 3 Staphylococcus aureus and 3 Staphylococcus epidermidis strains."( Pharmacodynamics of moxifloxacin and levofloxacin against Staphylococcus aureus and Staphylococcus epidermidis in an in vitro pharmacodynamic model.
Lister, PD, 2001
)
0.86
" The terminal elimination half-life was 14 to 15 hours, supporting once daily administration of the drug."( Pharmacokinetics, safety and tolerability of moxifloxacin, a novel 8-methoxyfluoroquinolone, after repeated oral administration.
Kubitza, D; Schühly, U; Stass, H, 2001
)
0.57
"These studies indicate that, based on the safety profile and the pharmacokinetic behaviour of moxifloxacin, a dosage regimen of 400mg given once daily should be effective and well tolerated for the treatment of various infections."( Pharmacokinetics, safety and tolerability of moxifloxacin, a novel 8-methoxyfluoroquinolone, after repeated oral administration.
Kubitza, D; Schühly, U; Stass, H, 2001
)
0.79
"Maximum plasma concentration (Cmax) and area under the plasma concentration-time curve (AUC) were higher in elderly females than in elderly males; however, when normalised for bodyweight, these pharmacokinetic parameters were not significantly different between the groups."( The influence of age and gender on the pharmacokinetics of moxifloxacin.
Heller, AH; Lettieri, JT; Liu, P; Sullivan, JT, 2001
)
0.55
"18 young, healthy, male volunteers were enrolled in the study, of whom 16 were considered evaluable for the pharmacokinetic analysis."( Effect of food on the pharmacokinetics of a single oral dose of moxifloxacin 400mg in healthy male volunteers.
Agarwal, V; Lettieri, J; Liu, P; Vargas, R, 2001
)
0.55
"Pharmacokinetic parameters such as maximum concentration (Cmax), time to reach Cmax (tmax), area under the concentration-time curve from zero to 48 hours (AUC48h), AUC from zero extrapolated to infinity (AUCinfinity) and elimination half-life (t1/2z) were estimated using noncompartmental methods."( Effect of food on the pharmacokinetics of a single oral dose of moxifloxacin 400mg in healthy male volunteers.
Agarwal, V; Lettieri, J; Liu, P; Vargas, R, 2001
)
0.55
" The plasma pharmacokinetics of moxifloxacin for treatments A and C were equivalent with respect to Css(max) (estimated true ratio 109%, 90% CI 97 to 123%) and AUCss(tau) (ratio 104%, 90% CI 100 to 108%); the median tmax values were also similar (0."( Lack of pharmacokinetic interaction between moxifloxacin, a novel 8-methoxyfluoroquinolone, and theophylline.
Kubitza, D; Stass, H, 2001
)
0.86
"An in vitro pharmacokinetic model (IVPM) was used to simulate the human serum pharmacokinetics of moxifloxacin, levofloxacin and sparfloxacin, and to compare their pharmacodynamics against Streptococcus pneumoniae exhibiting a wide range of susceptibilities to fluoroquinolones."( Pharmacodynamics of moxifloxacin, levofloxacin and sparfloxacin against Streptococcus pneumoniae.
Lister, PD; Sanders, CC, 2001
)
0.85
" The purposes of this study were to evaluate the bactericidal effectiveness and the pharmacodynamic profile of moxifloxacin in cerebrospinal fluid (CSF) and to compare the bactericidal activity with that of ceftriaxone and meropenem therapy."( Pharmacodynamics and bactericidal activity of moxifloxacin in experimental Escherichia coli meningitis.
Ghaffar, F; Hardy, RD; Jafri, HS; McCoig, CC; McCracken, GH; Michelow, IC; Olsen, K; Patel, C; Rodriguez-Cerrato, V, 2001
)
0.78
"0001) were reduced with decreasing CLCR, mean Cmax was slightly reduced (Cmax-ratio 85."( Pharmacokinetics of moxifloxacin, a novel 8-methoxy-quinolone, in patients with renal dysfunction.
Delesen, H; Halabi, A; Kubitza, D; Stass, H, 2002
)
0.64
"A new pharmacodynamic parameter, the composite recovery time (CRT), is described and used to calculate species-specific MIC breakpoints."( Calculation of composite recovery time: a new pharmacodynamic parameter.
Gould, IM; MacKenzie, FM; Milne, KE, 2002
)
0.31
"The pharmacodynamics of moxifloxacin against Streptococcus pneumoniae and Pseudomonas aeruginosa were investigated in a pharmacokinetic infection model."( Activities of moxifloxacin against, and emergence of resistance in, Streptococcus pneumoniae and Pseudomonas aeruginosa in an in vitro pharmacokinetic model.
Bowker, KE; Holt, HA; MacGowan, AP; Rogers, CA, 2003
)
0.99
"The differential effects of moxifloxacin and levofloxacin on the development of resistance in four Streptococcus pneumoniae isolates were examined by using an in vitro pharmacodynamic model."( Activities of mutant prevention concentration-targeted moxifloxacin and levofloxacin against Streptococcus pneumoniae in an in vitro pharmacodynamic model.
Allen, GP; Kaatz, GW; Rybak, MJ, 2003
)
0.86
"Our objective was to construct a population pharmacokinetic model for moxifloxacin disposition in plasma and bronchial secretions in patients with severe bronchopneumonia who were mechanically ventilated."( Population pharmacokinetics of moxifloxacin in plasma and bronchial secretions in patients with severe bronchopneumonia.
Albanese, J; Arvis, P; Bruguerolle, B; Lacarelle, B; Martin, C; Sampol, E; Simon, N; Urien, S, 2003
)
0.84
" The population pharmacokinetic modeling was performed with NONMEM."( Population pharmacokinetics of moxifloxacin in plasma and bronchial secretions in patients with severe bronchopneumonia.
Albanese, J; Arvis, P; Bruguerolle, B; Lacarelle, B; Martin, C; Sampol, E; Simon, N; Urien, S, 2003
)
0.6
" The population pharmacokinetic parameters were as follows (given as estimate with percent interindividual variability in parentheses except where otherwise indicated): clearance, 14."( Population pharmacokinetics of moxifloxacin in plasma and bronchial secretions in patients with severe bronchopneumonia.
Albanese, J; Arvis, P; Bruguerolle, B; Lacarelle, B; Martin, C; Sampol, E; Simon, N; Urien, S, 2003
)
0.6
" The pharmacokinetic findings of this investigation show that relatively high aqueous levels can be achieved after topical administration."( Penetration pharmacokinetics of topically administered 0.5% moxifloxacin ophthalmic solution in human aqueous and vitreous.
Apte, RS; Blinder, KJ; Chi, J; Hariprasad, SM; Holekamp, NM; Mieler, WF; Prince, RA; Rosenblatt, B; Shah, GK; Thomas, MA, 2005
)
0.57
"A complete a literature search was undertaken to establish the MIC90 values of the five microorganisms most frequently isolated in odontogenic infections and the pharmacokinetic parameters of 13 antibiotics used in these infections."( [Pharmacokinetic/pharmacodynamic analysis of antibiotic therapy in dentistry and stomatology].
Ardanza-Trevijano, B; Canut, A; Isla, A; Labora, A; Pedraz, JL; Rodríguez-Gascón, A; Solinís, MA, 2005
)
0.33
"Human pharmacokinetic parameters are often predicted prior to clinical study from in vivo preclinical pharmacokinetic data."( Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
Jolivette, LJ; Ward, KW, 2005
)
0.33
"The objective of this study was to determine the pharmacodynamic (PD) activity of moxifloxacin against four selected Bacteroides fragilis strains (three strains with low MICs and one strain with a high MIC) and two Escherichia coli strains (one strain with a low MIC and one strain with a high MIC) in a pharmacokinetic (PK) in vitro model in pure cultures as well as in mixed cultures."( Activity of moxifloxacin against Bacteroides fragilis and Escherichia coli in an in vitro pharmacokinetic/pharmacodynamic model employing pure and mixed cultures.
Forberg, J; Goldstein, EJ; Rodloff, AC; Schaumann, R, 2005
)
0.93
"The antibacterial effects of moxifloxacin against Bacteroides fragilis, Clostridium perfringens, and gram-positive anaerobic cocci (GPAC) were studied in an in vitro pharmacokinetic model."( Pharmacodynamics of moxifloxacin against anaerobes studied in an in vitro pharmacokinetic model.
Bowker, KE; Macgowan, AP; Noel, AR, 2005
)
0.94
" The pharmacokinetic data suggest that intravitreal moxifloxacin may have a role in the treatment of bacterial endophthalmitis."( Clearance of intravitreal moxifloxacin.
Benz, MS; He, F; Holz, ER; Iyer, MN; Mieler, WF; Wensel, TG, 2006
)
0.88
"To assess the pharmacokinetic and pharmacodynamic behaviour of moxifloxacin in 15 consecutive elderly patients with acute exacerbation of chronic bronchitis (AECB) treated with the fixed oral moxifloxacin 400 mg/day regimen with the intent of verifying which degree of exposure may be ensured by this standard regimen against AECB pathogens."( Pharmacokinetic and pharmacodynamic aspects of oral moxifloxacin 400 mg/day in elderly patients with acute exacerbation of chronic bronchitis.
Dolcet, F; Furlanut, M; Lugatti, E; Pavan, F; Pea, F; Screm, MC; Talmassons, G, 2006
)
0.82
" Standard pharmacokinetic parameters and pharmacodynamic determinants (peak concentration [C(max)]/minimum inhibitory concentration [MIC], area under the plasma concentration-time curve during the 24-hour observational period [AUC(24)]/MIC, pharmacodynamic breakpoints [PDBPs]) were assessed."( Pharmacokinetic and pharmacodynamic aspects of oral moxifloxacin 400 mg/day in elderly patients with acute exacerbation of chronic bronchitis.
Dolcet, F; Furlanut, M; Lugatti, E; Pavan, F; Pea, F; Screm, MC; Talmassons, G, 2006
)
0.58
"In patients with AECB the pharmacokinetic behaviour of moxifloxacin is not significantly altered by aging processes."( Pharmacokinetic and pharmacodynamic aspects of oral moxifloxacin 400 mg/day in elderly patients with acute exacerbation of chronic bronchitis.
Dolcet, F; Furlanut, M; Lugatti, E; Pavan, F; Pea, F; Screm, MC; Talmassons, G, 2006
)
0.83
" These data demonstrate that not all fluoroquinolones share the same pharmacodynamic targets needed to maximize their antibacterial effect."( Pharmacodynamics of moxifloxacin and levofloxacin simulating human serum and lung concentrations.
Dalhoff, A; Schubert, S; Stass, H; Ullmann, U, 2005
)
0.65
" Therefore, the attempt was made to introduce immunocompetence into an in vitro pharmacodynamic model."( Contribution of immunocompetence to the antibacterial activities of ciprofloxacin and moxifloxacin in an in vitro pharmacodynamic model.
Dalhoff, A, 2005
)
0.55
" The method was successfully applied to an in vitro pharmacokinetic study and patient samples as well."( Validation of a levofloxacin HPLC assay in plasma and dialysate for pharmacokinetic studies.
Siewert, S, 2006
)
0.33
" A pharmacokinetic computerized device was used to simulate serum and epithelial lining fluid (ELF) concentrations."( A pharmacodynamic approach to antimicrobial activity in serum and epithelial lining fluid against in vivo-selected Streptococcus pneumoniae mutants and association with clinical failure in pneumonia.
Aguilar, L; Alou, L; Cafini, F; Echeverría, O; Giménez, MJ; Pérez-Trallero, E; Prieto, J; Sevillano, D, 2006
)
0.33
"An in vitro pharmacodynamic model was used to simulate the epithelial lining fluid (ELF) concentrations following oral administration of levofloxacin 500 mg once daily and moxifloxacin 400 mg once daily in older adults."( Evaluation of bacterial kill when modelling the bronchopulmonary pharmacokinetic profile of moxifloxacin and levofloxacin against parC-containing isolates of Streptococcus pneumoniae.
Deryke, CA; Du, X; Nicolau, DP, 2006
)
0.75
" This method was applied in pharmacokinetic studies moxifloxacin preparations in healthy volunteers."( High-performance liquid chromatography assay for moxifloxacin: pharmacokinetics in human plasma.
Tatar Ulu, S, 2007
)
0.84
" The area under the concentration-time curve (AUC) tended to be greater in exudate; the time to peak concentrations (T(max)) was longer in exudate than in plasma, as were half-life and mean residence time (MRT)."( Pharmacokinetics and peritoneal penetration of moxifloxacin in peritonitis.
Delesen, H; Kubitza, D; Rink, AD; Stass, H; Vestweber, KH, 2006
)
0.59
"A correlation was seen between both the area under the serum concentration curve and MIC (AUC/MIC) and the peak concentration/MIC (Cmax/MIC) versus area under the bactericidal killing curve (AUBKC) or Deltalog0-24 cfu/mL."( Pharmacodynamics of moxifloxacin and levofloxacin against Streptococcus pneumoniae, Staphylococcus aureus, Klebsiella pneumoniae and Escherichia coli: simulation of human plasma concentrations after intravenous dosage in an in vitro kinetic model.
Cars, O; Odenholt, I, 2006
)
0.66
" The aim of the present study was to develop a semimechanistic pharmacokinetic (PK)/pharmacodynamic (PD) model characterizing the events seen in a bacterial system when it is exposed to antibacterial agents with different mechanisms of action."( Semimechanistic pharmacokinetic/pharmacodynamic model for assessment of activity of antibacterial agents from time-kill curve experiments.
Cars, O; Karlsson, MO; Löwdin, E; Nielsen, EI; Sandström, M; Viberg, A, 2007
)
0.34
"Members of the fluoroquinolone class are being actively evaluated for inclusion in tuberculosis chemotherapy regimens, and we sought to determine the best in vitro and pharmacodynamic predictors of in vivo efficacy in mice."( Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
Balasubramanian, V; Bharath, S; Gaonkar, S; Jayaram, R; Jayashree, R; Kaur, P; Mahesh, BN; Nandi, V; Shandil, RK; Suresh, BL, 2007
)
1.78
"To compare pharmacodynamic indices and minimal inhibitory concentrations for vancomycin, gatifloxacin, moxifloxacin, linezolid, and combined quinupristin and dalfopristin for historic and current human coagulase-negative staphylococcus (CoNS) endophthalmitis isolates."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.55
" Peak concentration (C(max)) was defined as the maximum attainable aqueous concentration using topical or oral therapy, or both."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
"Plasma, dialysate and urine pharmacokinetic parameters for moxifloxacin and its main metabolites were calculated after single and multiple (7 days) dosing with 400 mg day(-1)."( The influence of continuous venovenous haemodialysis on the pharmacokinetics of multiple oral moxifloxacin administration to patients with severe renal dysfunction.
Bührmann, S; Kribben, A; Kubitza, D; Mitchell, A; Möller, JG; Schäfers, RF; Stass, H; Wenzel, RR, 2007
)
0.8
"The objective of this study was to investigate the relationship between pharmacokinetic and pharmacodynamic parameters, on the basis of the mutant prevention concentration (MPC) concept, and the emergence of resistant mutants of Streptococcus pneumoniae to fluoroquinolone antibacterials."( Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
Homma, T; Hori, T; Sugimori, G; Yamano, Y, 2007
)
0.34
" In addition to standard pharmacokinetic parameters, the total dialysate concentration of both drugs was measured using a technically simple single-pass batch dialysis system for EDD."( Pharmacokinetics of moxifloxacin and levofloxacin in intensive care unit patients who have acute renal failure and undergo extended daily dialysis.
Czock, D; de Groot, K; Fliser, D; Hafer, C; Haller, H; Hüsig-Linde, C; Keller, F; Kielstein, JT; Kuse, E; Langhoff, A; Schöpke, T; Swoboda, S, 2006
)
0.66
"The purpose of this study was to examine the allometric analyses of marbofloxacin, moxifloxacin, danofloxacin and difloxacin using pharmacokinetic data from the literature."( Allometric scaling of marbofloxacin, moxifloxacin, danofloxacin and difloxacin pharmacokinetics: a retrospective analysis.
Cox, SK, 2007
)
0.84
"The objective of this study was to determine the population pharmacokinetic parameters of levofloxacin, gatifloxacin, and moxifloxacin following multiple oral doses."( Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
Boom, WH; Dietze, R; Hadad, DJ; Johnson, JL; Molino, LP; Palaci, M; Peloquin, CA, 2008
)
0.79
"This study used Monte Carlo simulations to assess the potential for attainment of pharmacodynamic targets with the fluoroquinolones garenoxacin, gemifloxacin, and moxifloxacin against Streptococcus pneumoniae in serum and epithelial lining fluid (ELF) from hospitalized patients with community-acquired pneumonia (CAP)."( Comparative pharmacodynamics of garenoxacin, gemifloxacin, and moxifloxacin in community-acquired pneumonia caused by Streptococcus pneumoniae: a Monte Carlo simulation analysis.
Hoban, DJ; Noreddin, AM; Ostroski, M; Reese, AA; Zhanel, GG, 2007
)
0.78
"Data on the free AUC over 24 hours (fAUC(0-24)), a measure of drug exposure, were derived from previously described population pharmacokinetic models for therapeutic doses of the 3 fluoroquinolones."( Comparative pharmacodynamics of garenoxacin, gemifloxacin, and moxifloxacin in community-acquired pneumonia caused by Streptococcus pneumoniae: a Monte Carlo simulation analysis.
Hoban, DJ; Noreddin, AM; Ostroski, M; Reese, AA; Zhanel, GG, 2007
)
0.58
" Thus, in addition to adequate drainage, empirical coverage with broad-spectrum antimicrobials is central to the management of such abscesses and an understanding of pharmacokinetic properties can be valuable when selecting antimicrobial agents."( Pharmacokinetics and tissue penetration of moxifloxacin in intervention therapy for intra-abdominal abscess.
Delesen, H; Kubitza, D; Rink, AD; Stass, H; Vestweber, KH, 2008
)
0.61
" Eight patients with CT or ultrasound evidence of a localized intra-abdominal abscess requiring interventional drainage without signs of generalized peritonitis were considered suitable candidates for pharmacokinetic analysis."( Pharmacokinetics and tissue penetration of moxifloxacin in intervention therapy for intra-abdominal abscess.
Delesen, H; Kubitza, D; Rink, AD; Stass, H; Vestweber, KH, 2008
)
0.61
" Half-life and mean residence time were longer in abscess fluid than in plasma, suggesting that moxifloxacin accumulates in abscess fluid."( Pharmacokinetics and tissue penetration of moxifloxacin in intervention therapy for intra-abdominal abscess.
Delesen, H; Kubitza, D; Rink, AD; Stass, H; Vestweber, KH, 2008
)
0.83
" Based on the pharmacokinetic data, moxifloxacin is a good candidate therapy for use in patients with intra-abdominal abscesses undergoing CT-guided percutaneous drainage and may also prove valuable in the general systemic management of intra-abdominal abscesses in the future."( Pharmacokinetics and tissue penetration of moxifloxacin in intervention therapy for intra-abdominal abscess.
Delesen, H; Kubitza, D; Rink, AD; Stass, H; Vestweber, KH, 2008
)
0.88
" The concentration-time data were analysed by compartmental (after IV dose) and non-compartmental (after IV, IM and SC administration) pharmacokinetic methods."( Pharmacokinetics after intravenous, intramuscular and subcutaneous administration of moxifloxacin in sheep.
Cárceles, CM; Escudero, E; Fernández-Varón, E; Marín, P, 2009
)
0.58
" 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
" The developed assay method was applied to a pharmacokinetic study in human volunteers following oral administration of 400 mg GFC tablet."( Development and validation of a HPLC method for simultaneous quantitation of gatifloxacin, sparfloxacin and moxifloxacin using levofloxacin as internal standard in human plasma: application to a clinical pharmacokinetic study.
Mullangi, R; Narasu, L; Shankar, BP; Srinivas, N, 2008
)
0.56
" Ciprofloxacin, a carboxyfluoroquinolone, was previously observed to demonstrate the pharmacodynamic interactions with antifungal agents by altering their growth inhibitory activity against Candida albicans and Aspergillus fumigatus."( Comparative pharmacodynamic interaction analysis between ciprofloxacin, moxifloxacin and levofloxacin and antifungal agents against Candida albicans and Aspergillus fumigatus.
Meletiadis, J; Papaioannidou, P; Roilides, E; Sein, T; Stergiopoulou, T; Tsiouris, I; Walsh, TJ, 2009
)
0.59
"The knowledge of the pharmacodynamic interactions between fluoroquinolones and antifungal agents may guide selection and potentially improve the outcome of immunosuppressed patients with concurrent bacterial and fungal infections."( Comparative pharmacodynamic interaction analysis between ciprofloxacin, moxifloxacin and levofloxacin and antifungal agents against Candida albicans and Aspergillus fumigatus.
Meletiadis, J; Papaioannidou, P; Roilides, E; Sein, T; Stergiopoulou, T; Tsiouris, I; Walsh, TJ, 2009
)
0.59
" This bio-analytical method was finally applied to the analysis of samples which have been obtained from patients, participating in a pharmacokinetic study on moxifloxacin."( Pharmacokinetics of fluoroquinolones in critical care patients: A bio-analytical HPLC method for the simultaneous quantification of ofloxacin, ciprofloxacin and moxifloxacin in human plasma.
Boussery, K; Colpaert, K; De Paepe, P; De Smet, J; De Sutter, P; Decruyenaere, J; Van Bocxlaer, J, 2009
)
0.75
"African green monkeys (vervets) have been proposed as an alternate species that might allow improved access and provide high-quality pharmacokinetic results comparable with other primates."( Exploration of the African green monkey as a preclinical pharmacokinetic model: oral pharmacokinetic parameters and drug-drug interactions.
Bhadresa, S; Coon, DJ; Lawrence, MS; Magiera, D; Struharik, M; Ward, KW, 2009
)
0.35
"This study used a whole-body physiologically based pharmacokinetic (WB-PBPK) model for moxifloxacin, plus in vitro and in vivo literature data on its interaction with macrophages, to interpret biopsy results generated from patients undergoing primarily colorectal surgery."( Defining the role of macrophages in local moxifloxacin tissue concentrations using biopsy data and whole-body physiologically based pharmacokinetic modelling.
Ahr, G; Edginton, AN; Stass, H; Willmann, S, 2009
)
0.84
" observed biopsy half-life = 21 hours) was similar to that of moxifloxacin in macrophages (20."( Defining the role of macrophages in local moxifloxacin tissue concentrations using biopsy data and whole-body physiologically based pharmacokinetic modelling.
Ahr, G; Edginton, AN; Stass, H; Willmann, S, 2009
)
0.86
" Pharmacokinetic parameters were estimated using standard noncompartmental methods."( Pharmacokinetics of moxifloxacin in patients undergoing continuous ambulatory peritoneal dialysis.
Boletis, J; Giamarellos-Bourboulis, EJ; Kanellakopoulou, K; Skalioti, C; Stamatiadis, D; Tsaganos, T,
)
0.45
"Antibiotic pharmacodynamic modeling allows variations in pathogen susceptibility and human pharmacokinetics to be accounted for when considering antibiotic doses, potential bacterial pathogen targets for therapy, and clinical susceptibility breakpoints."( Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
Bowker, KE; MacGowan, AP; Noel, AR; Reynolds, R, 2009
)
0.35
" Population pharmacokinetic parameters and their variability encountered in tuberculosis patients were utilized in Monte Carlo simulations to determine the probability that particular daily doses of the drugs would achieve or exceed the EC(90) in the epithelial lining fluid of 10,000 tuberculosis patients."( New susceptibility breakpoints for first-line antituberculosis drugs based on antimicrobial pharmacokinetic/pharmacodynamic science and population pharmacokinetic variability.
Gumbo, T, 2010
)
0.36
"This study investigates the potential pharmacokinetic interactions between an antimicrobial agent, moxifloxacin, and 2 immunosuppressant drugs, cyclosporine and tacrolimus, in kidney transplant recipients."( Absence of pharmacokinetic interference of moxifloxacin on cyclosporine and tacrolimus in kidney transplant recipients.
Basile, V; Capone, D; Carrano, R; Federico, S; Kadilli, I; Nappi, R; Polichetti, G; Sabbatini, M; Tarantino, G, 2010
)
0.84
" Changes in QTcF mirrored the pharmacokinetic changes, and there was a linear relationship between plasma concentration of moxifloxacin and change in QTcF."( Pharmacokinetics and pharmacodynamics of three moxifloxacin dosage forms: implications for blinding in active-controlled cardiac repolarization studies.
Florian, JA; Garnett, CE; Mason, JW; Moon, TE; Selness, DS; Spaulding, RR, 2010
)
0.82
" Pharmacokinetic analysis of disposition data indicated that intravenous administration data were best described by a two compartment open model, whereas intramuscular administration data were best described by a one compartment open model."( Pharmacokinetics and bioavailability of moxifloxacin in buffalo calves.
Pathania, R; Sharma, SK, 2010
)
0.63
" Moxifloxacin pharmacokinetic parameters in the presence of ciclosporin were compared with previously published pharmacokinetic data for moxifloxacin in healthy individuals."( Moxifloxacin does not alter ciclosporin pharmacokinetics in transplant patients: a multiple-dose, uncontrolled, single-centre study.
Bauer, S; Delesen, H; Kubitza, D; Mai, I; Roots, I; Stass, H, 2010
)
2.71
" The pharmacokinetic parameters for moxifloxacin were unaffected by the presence of ciclosporin."( Moxifloxacin does not alter ciclosporin pharmacokinetics in transplant patients: a multiple-dose, uncontrolled, single-centre study.
Bauer, S; Delesen, H; Kubitza, D; Mai, I; Roots, I; Stass, H, 2010
)
2.08
"Concomitant administration of moxifloxacin does not alter the pharmacokinetic parameters of ciclosporin or ciclosporin plus its metabolites in immunosuppressed patients."( Moxifloxacin does not alter ciclosporin pharmacokinetics in transplant patients: a multiple-dose, uncontrolled, single-centre study.
Bauer, S; Delesen, H; Kubitza, D; Mai, I; Roots, I; Stass, H, 2010
)
2.09
" After validation studies, the method was applied in order to conclude the effects of pregnancy on postoperative pharmacokinetic profiles of moxifloxacin."( Comparison of pharmacokinetic profiles of moxifloxacin in Caesarean versus non-pregnant sectioned women by fully validated HPLC with fluorescence detection.
Beksaç, MS; Eroglu, H; Katlan, D; Kir, S; Nemutlu, E; Oyüncü, O; Ozek, A; Özyüncü, Ö, 2010
)
0.83
" Azithromycin also showed an extended half-life (65."( Pharmacokinetics of azithromycin and moxifloxacin in human conjunctiva and aqueous humor during and after the approved dosing regimens.
Brubaker, K; Crean, CS; Haque, RM; Hwang, DG; Stewart, WC; Zink, RC, 2010
)
0.63
"To increase our understanding of important subject characteristics and design variables affecting the performance of oral moxifloxacin in thorough QT studies, population pharmacokinetic and concentration-QTc models were developed by pooling data from 20 studies."( Population pharmacokinetic and concentration--QTc models for moxifloxacin: pooled analysis of 20 thorough QT studies.
Brundage, R; Florian, JA; Garnett, CE; Parekh, A; Tornøe, CW, 2011
)
0.82
" The SLOPE model, relating the QT increase as a linear function of concentration, provided a better description of the pharmacodynamic effect than did the Emax model."( Reevaluation of moxifloxacin pharmacokinetics and their direct effect on the QT interval.
Grosjean, P; Urien, S, 2012
)
0.72
" Since moxifloxacin has a longer half-life than rifampin, rifampin concentrations are <1% of the maximum concentration in serum (C(max)) on day 6 and nondetectable on day 7, while concentrations of moxifloxacin remain and are able to induce error-prone replication."( Effect of administration of moxifloxacin plus rifampin against Mycobacterium tuberculosis for 7 of 7 days versus 5 of 7 days in an in vitro pharmacodynamic system.
Brown, D; Drusano, GL; Eichas, A; Kulawy, R; Louie, A; Sgambati, N, 2011
)
1.12
" This is despite the availability of antibiotics that have good activity against Mycobacterium tuberculosis in vitro and favorable pharmacokinetic profiles in plasma."( Pharmacokinetic evaluation of the penetration of antituberculosis agents in rabbit pulmonary lesions.
Barry, CE; Dartois, V; Goh, A; Kern, S; Kjellsson, MC; Low, KM; Pillai, G; Via, LE; Weiner, D, 2012
)
0.38
" Further, the method was also successfully applied to a single-dose pharmacokinetic study in rats."( Development and validation of liquid chromatography-mass spectrometric method for simultaneous determination of moxifloxacin and ketorolac in rat plasma: application to pharmacokinetic study.
Banerjee, SK; Borkar, RM; Padiya, R; Raju, B; Ramesh, M; Srinivas, R, 2012
)
0.59
"A baseline pharmacokinetic study of MFX (400 mg once daily) was conducted in 36 healthy adults and repeated after one week of daily MFX with either RMP (450/600 mg) (n = 18) or INH (300 mg) (n = 18)."( Effect of rifampicin & isoniazid on the steady state pharmacokinetics of moxifloxacin.
Geetharani, A; Hemanth Kumar, AK; Nandhakumar, B; Nandini, R; Ramachandran, G; Srinivasan, R; Sugirda, P; Tharani, CB, 2012
)
0.61
"Plasma peak concentration and exposure of MFX was significantly lower and plasma clearance significantly higher when combined with RMP (P<0."( Effect of rifampicin & isoniazid on the steady state pharmacokinetics of moxifloxacin.
Geetharani, A; Hemanth Kumar, AK; Nandhakumar, B; Nandini, R; Ramachandran, G; Srinivasan, R; Sugirda, P; Tharani, CB, 2012
)
0.61
"To describe the plasma concentration-time profile of moxifloxacin after intravenous and enteral administration in intensive care unit (ICU) patients and to provide a pharmacodynamic (PD) evaluation with regard to pneumonia."( Population pharmacokinetics and pharmacodynamic evaluation of intravenous and enteral moxifloxacin in surgical intensive care unit patients.
Haeberle, HA; Heininger, A; Kees, F; Kees, MG; Kloft, C; Schaeftlein, A, 2013
)
0.86
" A population pharmacokinetic (PK) model was developed using NONMEM VII."( Population pharmacokinetics and pharmacodynamic evaluation of intravenous and enteral moxifloxacin in surgical intensive care unit patients.
Haeberle, HA; Heininger, A; Kees, F; Kees, MG; Kloft, C; Schaeftlein, A, 2013
)
0.61
"This study evaluated the pharmacokinetics of intravenous moxifloxacin 400 mg once and levofloxacin 500 mg twice daily in patients with lower respiratory tract infections (LRTIs) and assessed their pharmacodynamic adequacy against common respiratory pathogens."( Pharmacokinetics of moxifloxacin and high-dose levofloxacin in severe lower respiratory tract infections.
Chatzika, K; Kioumis, I; Kontou, P; Manika, K; Papaioannou, M; Pitsiou, G; Sionidou, M, 2013
)
0.96
" The validated method was applied to assay real plasma samples used for pharmacokinetic studies and therapeutic drug monitoring of the selected drugs."( Simultaneous quantification of linezolid, tinidazole, norfloxacin, moxifloxacin, levofloxacin, and gatifloxacin in human plasma for therapeutic drug monitoring and pharmacokinetic studies in human volunteers.
Helmy, SA, 2013
)
0.63
"This assay method was valid within a wide range of plasma concentrations and may be proposed as a suitable method for pharmacokinetic studies, therapeutic drug monitoring implementation, and routine clinical applications, especially for some populations of patients who receive a combination of these drugs."( Simultaneous quantification of linezolid, tinidazole, norfloxacin, moxifloxacin, levofloxacin, and gatifloxacin in human plasma for therapeutic drug monitoring and pharmacokinetic studies in human volunteers.
Helmy, SA, 2013
)
0.63
" Further studies should determine the optimal pharmacodynamic target for moxifloxacin in a multidrug regimen and clarify safety issues when it is administered at higher doses."( Moxifloxacin population pharmacokinetics and model-based comparison of efficacy between moxifloxacin and ofloxacin in African patients.
Charalambous, S; Chigutsa, E; Denti, P; Harrison, T; Hatherill, M; Jindani, A; McIlleron, HM; Mungofa, S; Simonsson, US; Sirgel, FA; Wiesner, L; Zvada, SP, 2014
)
2.08
" Pharmacokinetic parameters of moxifloxacin were determined in rats following oral administration to rats in the presence and absence of diclofenac."( Effect of diclofenac on the pharmacokinetics of moxifloxacin in rats.
Chen, L; Guo, S; Wu, LX; Xu, M; Zhang, JH, 2014
)
0.94
" A single-dose pharmacokinetic study was performed after intravenous administration of 400 mg MXF."( Moxifloxacin pharmacokinetics and pleural fluid penetration in patients with pleural effusion.
Chatzika, K; Kioumis, I; Kontou, P; Manika, K; Papakosta, D; Pitsiou, G; Zarogoulidis, K, 2014
)
1.85
" The method had been successfully applied to a pharmacokinetic study of fixed dose administration of PA-824, moxifloxacin, pyrazinamide and their combination in SD rat."( LC-MS/MS method for the simultaneous determination of PA-824, moxifloxacin and pyrazinamide in rat plasma and its application to pharmacokinetic study.
Diao, C; Liang, L; Liu, X; Wang, L; Xu, Y; Zhang, J; Zhang, S, 2014
)
0.86
" AUC₀₋₂₄ and other pharmacokinetic (PK) parameters were determined following intensive PK sampling in two Dutch TB referral centres."( Population pharmacokinetics and limited sampling strategy for first-line tuberculosis drugs and moxifloxacin.
Aarnoutse, RE; Alffenaar, JW; Boeree, MJ; Broeders, J; Burger, DM; Donders, AR; Later-Nijland, HM; Magis-Escurra, C; van Altena, R; van Crevel, R; van der Werf, TS, 2014
)
0.62
"The purpose of this study was to explore the population pharmacokinetic features of moxifloxacin in infected patients."( Population pharmacokinetics of intravenous moxifloxacin 400 mg once-daily dosage in infected patients.
Ji, S; Wang, N; Yang, W; Zhang, Y; Zhao, X; Zhu, L, 2014
)
0.89
" A nonlinear mixed effect model was used to model the population pharmacokinetic (PK) behavior of moxifloxacin."( Population pharmacokinetics of intravenous moxifloxacin 400 mg once-daily dosage in infected patients.
Ji, S; Wang, N; Yang, W; Zhang, Y; Zhao, X; Zhu, L, 2014
)
0.88
" The typical population values of moxifloxacin for the pharmacokinetic parameters of apparent clearance (CL) and apparent distribution volume (V) were 12."( Population pharmacokinetics of intravenous moxifloxacin 400 mg once-daily dosage in infected patients.
Ji, S; Wang, N; Yang, W; Zhang, Y; Zhao, X; Zhu, L, 2014
)
0.94
"The present study developed population pharmacokinetic models for moxifloxacin in infected Chinese patients."( Population pharmacokinetics of intravenous moxifloxacin 400 mg once-daily dosage in infected patients.
Ji, S; Wang, N; Yang, W; Zhang, Y; Zhao, X; Zhu, L, 2014
)
0.9
"5-10 mg/kg for children with multidrug-resistant (MDR) tuberculosis, but pharmacokinetic and long-term safety data of moxifloxacin in children with tuberculosis are lacking."( Pharmacokinetics and safety of moxifloxacin in children with multidrug-resistant tuberculosis.
Castel, S; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Schaaf, HS; Thee, S; Wiesner, L, 2015
)
0.91
"In a prospective pharmacokinetic and safety study, children 7-15 years of age routinely receiving moxifloxacin 10 mg/kg daily as part of multidrug treatment for MDR tuberculosis in Cape Town, South Africa, for at least 2 weeks, underwent intensive pharmacokinetic sampling (predose and 1, 2, 4, 8, and either 6 or 11 hours) and were followed for safety."( Pharmacokinetics and safety of moxifloxacin in children with multidrug-resistant tuberculosis.
Castel, S; Draper, HR; Garcia-Prats, AJ; Hesseling, AC; McIlleron, HM; Schaaf, HS; Thee, S; Wiesner, L, 2015
)
0.92
"The purpose of this report was to assess the impact of poor compliance on the efficacy of levofloxacin (LFX) and moxifloxacin (MOX), two fluoroquinolones with different pharmacokinetic (PK) and pharmacodynamic (PD) properties, in respiratory infections."( Impact of poor compliance with levofloxacin and moxifloxacin on respiratory tract infection antimicrobial efficacy: a pharmacokinetic/pharmacodynamic simulation study.
Carral, N; Lukas, JC; Oteo, I; Suarez, E, 2015
)
0.88
" A two-compartment population pharmacokinetic model was developed, identifying as covariates total body weight on central and peripheral volume of distribution (V1, V2) and ideal body weight on clearance (CL), respectively."( Population pharmacokinetics and target attainment analysis of moxifloxacin in patients with diabetic foot infections.
Haak, T; Kees, F; Kees, MG; Kloft, C; Wicha, SG; Zink, K, 2015
)
0.66
" Accordingly, we determined the pharmacokinetic (PK) profile of moxifloxacin at 400 mg/day in 18 patients treated empirically for community-acquired pneumonia."( Moxifloxacin pharmacokinetic profile and efficacy evaluation in empiric treatment of community-acquired pneumonia.
Brock, B; Hardlei, TF; Jensen-Fangel, S; Kragh Thomsen, M; Kreilgaard, M; Öbrink-Hansen, K; Petersen, E, 2015
)
2.1
" Pharmacokinetic sampling was performed once in every patient during the first three critical days."( Pharmacokinetic/pharmacodynamic analysis of an intensified regimen containing rifampicin and moxifloxacin for tuberculous meningitis.
Aarnoutse, R; Burger, D; Dian, S; Donders, R; Ganiem, AR; Ruesen, C; Ruslami, R; Te Brake, L; van Crevel, R, 2015
)
0.64
" Thus, we aimed to develop a pharmacokinetic (PK)-pharmacodynamic (PD) model for moxifloxacin, to evaluate the time course of its effect on QT intervals in Koreans."( Pharmacokinetic-pharmacodynamic analysis to evaluate the effect of moxifloxacin on QT interval prolongation in healthy Korean male subjects.
Chung, JY; Han, S; Hong, T; Jeon, S; Lee, J; Lim, KS; Park, GJ; Park, WS; Yim, DS; Yu, KS, 2015
)
0.88
" Moreover, both Cmax and AUC of moxifloxacin decreased and AUC of moxifloxacin sulfate conjugate metabolite increased significantly when moxifloxacin was administered to rats with DA pretreatment."( Exogenous dopamine induces dehydroepiandrosterone sulfotransferase (rSULT2A1) in rat liver and changes the pharmacokinetic profile of moxifloxacin in rats.
Chen, G; Ji, X; Li, J; Li, L; Lu, W; Shao, X; Wang, S; Xu, J; Zhou, T, 2015
)
0.9
" To evaluate the pharmacokinetic (PK) characteristics of clinically relevant, multidrug treatment regimens and to improve the feasibility of TDM, we conducted an open-label, multiple-dosing study with 16 healthy subjects who were divided into two groups."( Pharmacokinetics of Second-Line Antituberculosis Drugs after Multiple Administrations in Healthy Volunteers.
Chung, JY; Jang, IJ; Jang, K; Lee, JH; Moon, SJ; Oh, J; Park, JS; Park, SI; Song, J; Yoon, J; Yu, KS, 2015
)
0.42
" Based on the MICs and the population pharmacokinetic parameters of the investigated antimicrobials, a Monte Carlo simulation was performed to simulate the pharmacokinetic/pharmacodynamic (PK/PD) indices of different regimens."( A Monte Carlo pharmacokinetic/pharmacodynamic simulation to evaluate the efficacy of minocycline, tigecycline, moxifloxacin, and levofloxacin in the treatment of hospital-acquired pneumonia caused by Stenotrophomonas maltophilia.
Cai, X; Cui, J; Ni, W; Wei, C, 2015
)
0.63
" A pharmacokinetic study of moxifloxacin N-sulfate after a single oral dose of moxifloxacin in rats was carried out using this new method."( A Simple LC/MS/MS Method for the Determination of Moxifloxacin N-Sulfate in Rat Plasma and Its Application in a Pharmacokinetic Study.
Fan, R; Li, J; Lu, W; Su, Q; Wang, S; Yuan, Y; Zhou, T,
)
0.68
"A population pharmacokinetic analysis was performed to investigate the pharmacokinetics of moxifloxacin (400 mg) following a once-daily oral administration in 28 patients with respiratory tract infection disease."( Pharmacokinetics of consecutive oral moxifloxacin (400 mg/day) in patients with respiratory tract infection.
Endo, J; Funaguchi, N; Ito, F; Kaito, D; Kamamiya, F; Koumei, Y; Minatoguchi, S; Mori, H; Mori, M; Morishita, M; Ohno, Y; Toyoshi, S, 2016
)
0.93
"To examine whether strict control of clinical trial conditions could reduce apparent differences of pharmacokinetic (PK) parameters among ethnic groups."( Absence of ethnic differences in the pharmacokinetics of moxifloxacin, simvastatin, and meloxicam among three East Asian populations and Caucasians.
Hasunuma, T; Jang, IJ; Kaneko, M; Kaniwa, N; Kawai, S; Saito, Y; Takeuchi, M; Tohkin, M; Uyama, Y; Watanabe, H; Yamazoe, Y; Yimin, C, 2016
)
0.68
" Cmax values of moxifloxacin and simvastatin, but not meloxicam, showed significant differences."( Absence of ethnic differences in the pharmacokinetics of moxifloxacin, simvastatin, and meloxicam among three East Asian populations and Caucasians.
Hasunuma, T; Jang, IJ; Kaneko, M; Kaniwa, N; Kawai, S; Saito, Y; Takeuchi, M; Tohkin, M; Uyama, Y; Watanabe, H; Yamazoe, Y; Yimin, C, 2016
)
1.03
" Plasma concentrations of moxifloxacin and rifampicin were determined using LC-MS at the designated time points after drug administration, and the main pharmacokinetic parameters were calculated."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
1.02
" Serial blood sampling was conducted for pharmacokinetic analysis of moxifloxacin."( Population Pharmacokinetic-Pharmacodynamic Analysis to Compare the Effect of Moxifloxacin on QT Interval Prolongation Between Healthy Korean and Japanese Subjects.
Amano, H; Choi, HK; Fujita, T; Ghim, JL; Jung, JA; Kumagai, Y; Lee, DH; Maeda, M; Mendzelevski, B; Shin, JG; Song, ID; Tabata, K, 2016
)
0.9
" The concentration-effect analysis revealed that there was no change in slope (and confirmed that the difference was caused by a change in the pharmacokinetic model of moxifloxacin)."( Population Pharmacokinetic-Pharmacodynamic Analysis to Compare the Effect of Moxifloxacin on QT Interval Prolongation Between Healthy Korean and Japanese Subjects.
Amano, H; Choi, HK; Fujita, T; Ghim, JL; Jung, JA; Kumagai, Y; Lee, DH; Maeda, M; Mendzelevski, B; Shin, JG; Song, ID; Tabata, K, 2016
)
0.86
" There are no studies describing the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" The estimated pharmacokinetic parameters and the estimated slope of the MX concentration-QT/ΔQTc/ΔΔQTc relationship were described using models and were compared to results for other ethnicities from the literature."( Population pharmacokinetics of moxifloxacin and its concentration-QT interval relationship modeling in Chinese healthy volunteers.
He, YC; Huang, JH; Li, LJ; Liang, LY; Wang, K; Xu, FY; Xu, L; Yang, J; Yin, F; Zheng, QS, 2017
)
0.74
" Most patients (71%) had suboptimal steady-state serum Cmax (total drug) concentrations."( Moxifloxacin target site concentrations in patients with pulmonary TB utilizing microdialysis: a clinical pharmacokinetic study.
Bablishvili, N; Bernheim, A; Blumberg, HM; Derendorf, H; Gogishvili, S; Guarner, J; Heinrichs, MT; Kempker, RR; Little, BP; Nikolaishvili, K; Peloquin, CA; Sabulua, I; Tukvadze, N; Vashakidze, S, 2018
)
1.92
"6% increased clearance, respectively) and ABCB1 SNP rs2032582 (40% reduced bioavailability in one individual) were significantly associated with changes in moxifloxacin pharmacokinetic parameters."( Effect of genetic variation in UGT1A and ABCB1 on moxifloxacin pharmacokinetics in South African patients with tuberculosis.
Chaudhry, M; Chirehwa, M; Denti, P; McIlleron, H; Naidoo, A; Naidoo, K; Ngcapu, S; Padayatchi, N; Pepper, MS; Ramsuran, V; Singh, R; Yende-Zuma, N, 2018
)
0.93
" Clinical relevance of the effects of genetic variation on moxifloxacin pharmacokinetic requires further investigation."( Effect of genetic variation in UGT1A and ABCB1 on moxifloxacin pharmacokinetics in South African patients with tuberculosis.
Chaudhry, M; Chirehwa, M; Denti, P; McIlleron, H; Naidoo, A; Naidoo, K; Ngcapu, S; Padayatchi, N; Pepper, MS; Ramsuran, V; Singh, R; Yende-Zuma, N, 2018
)
0.98
" The validated analytical method was successfully applied in a pharmacokinetic study of a single-dose oral administration of a moxifloxacin 400 mg tablet in Thai healthy volunteers."( A simple and sensitive HPLC-fluorescence method for the determination of moxifloxacin in human plasma and its application in a pharmacokinetic study.
Jithavech, P; Kiatkumjorn, T; Na Bhuket, PR; Rojsitthisak, P; Thanawattanawanich, P; Wichitnithad, W, 2018
)
0.92
" However, moxifloxacin blood levels demonstrated that the nanoparticle formulation and intramuscular route provided the longest half-life and longest time above the minimal inhibitory concentration."( Nanoparticle Formulation of Moxifloxacin and Intramuscular Route of Delivery Improve Antibiotic Pharmacokinetics and Treatment of Pneumonic Tularemia in a Mouse Model.
Clemens, DL; Dillon, BJ; Horwitz, MA; Lee, BY; Li, Z; Plamthottam, S; Tullius, MV; Wang, R; Yu, CJ; Zink, JI, 2019
)
1.21
"This study aimed to evaluate the pharmacokinetic profile of moxifloxacin (MXF) in serum and sputum/bronchial secretions of 22 patients with acute exacerbation of chronic obstructive pulmonary disease (AECOPD) hospitalized in the ward and intensive care unit (ICU)."( Moxifloxacin in Chronic Obstructive Pulmonary Disease: Pharmacokinetics and Penetration into Bronchial Secretions in Ward and Intensive Care Unit Patients.
Chatzika, K; Kioumis, I; Kontou, P; Manika, K; Pitsiou, G; Sionidou, M; Zarogoulidis, P, 2019
)
2.2
" A dosing strategy for each age cohort (Cohort 1: ≥6 years to ≤14 years; Cohort 2: ≥2 years to <6 years; Cohort 3: >3 month to <2 years) was developed using physiology-based pharmacokinetic modeling combined with a stepwise dosing scheme to obtain a similar exposure to adults receiving 400 mg of moxifloxacin."( Pharmacokinetics, Safety, and Tolerability of Single-Dose Intravenous Moxifloxacin in Pediatric Patients: Dose Optimization in a Phase 1 Study.
Arrieta, AC; Bradley, JS; James, LP; Lettieri, J; Stass, H; Sullivan, JE; Vanevski, KM; Willmann, S, 2019
)
0.92
" We aim to compare the culture conversion between new-generation (levofloxacin and moxifloxacin) and old-generation (ciprofloxacin and ofloxacin) fluoroquinolones, develop pharmacokinetic models, and calculate target attainment for levofloxacin and moxifloxacin."( Fluoroquinolones in Drug-Resistant Tuberculosis: Culture Conversion and Pharmacokinetic/Pharmacodynamic Target Attainment To Guide Dose Selection.
Ahmed, S; Al-Shaer, MH; Alghamdi, WA; Alkabab, Y; Alsultan, A; An, G; Banu, S; Barbakadze, K; Cegielski, JP; Heysell, SK; Houpt, E; Kempker, RR; Kipiani, M; Mikiashvili, L; Peloquin, CA, 2019
)
0.74
" We applied physiologically-based pharmacokinetic (PBPK) and population pharmacokinetic (popPK) modeling to support dose selection in pediatric patients."( Application of Physiologically-Based and Population Pharmacokinetic Modeling for Dose Finding and Confirmation During the Pediatric Development of Moxifloxacin.
Coboeken, K; Eissing, T; Frei, M; Lippert, J; Stass, H; Sutter, G; Wendl, T; Willmann, S, 2019
)
0.71
" Here, we used high-content imaging screening and pharmacodynamic intracellular (PDi) modeling to identify and prioritize fluoroquinolones for TB treatment."( Intracellular Pharmacodynamic Modeling Is Predictive of the Clinical Activity of Fluoroquinolones against Tuberculosis.
Aljayyoussi, G; Ardrey, A; Biagini, GA; Donnellan, S; Martinez-Rodriguez, C; Moyo, E; Ward, SA, 2019
)
0.51
" Moxifloxacin CSF levels were obtained for pharmacokinetic analysis."( The Pharmacokinetics of Moxifloxacin in Cerebrospinal Fluid Following Intravenous Administration: A Report of Successfully Treated Infant with Mycoplasma hominis Meningitis.
Berman, DM; Messina, A; Namtu, K; Nohren, J; Peloquin, C; Tuite, G, 2020
)
1.78
" The pharmacokinetic parameters of MOX were calculated based on the plasma drug concentration-time profile."( Pharmacokinetics and Bioequivalence Study of a New Branded Generic Moxifloxacin Tablet Among Healthy Volunteers.
Amran, A; Anand, AK; Ho, RM; Leong, CW; Tan, CY; Tan, KL, 2021
)
0.86
" The pharmacodynamic study was conducted on rabbit eye model of induced keratitis and it is compared with marketed formulation (MF)."( Cationic Polyelectrolyte Nanocapsules of Moxifloxacin for Microbial Keratitis Therapy: Development, Characterization, and Pharmacodynamic Study.
Kesavan, K; Mohan, P, 2021
)
0.89
"Moxifloxacin is a recommended drug for rifampin-resistant tuberculosis (RR-TB) treatment, but there is limited pediatric pharmacokinetic and safety data, especially in young children."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
3.61
" Pharmacokinetic simulations were performed to predict expected exposure and optimal weight-banded dosing."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
2.16
" We developed a physiologically based pharmacokinetic model in Simcyp version 19, with available and newly generated in vitro and in vivo data, to estimate pharmacokinetic parameters of moxifloxacin alone and when administered with rifampicin."( Prediction of Moxifloxacin Concentrations in Tuberculosis Patient Populations by Physiologically Based Pharmacokinetic Modeling.
Aarnoutse, RE; Boeree, MJ; Bolwerk, C; Burger, DM; Greupink, R; Hoefsloot, W; Koenderink, JB; Kuipers, S; Litjens, CHC; Magis-Escurra, C; Ruslami, R; Russel, FGM; Svensson, EM; Te Brake, LHM; van Crevel, R; van den Broek, PHH; van den Heuvel, JJMW; van Ingen, J; van Laarhoven, A; Verscheijden, LFM, 2022
)
1.27
" Some pharmacokinetic parameters, calculated by the concentration of moxifloxacin in saliva and plasma, are statistically different."( A study of the pharmacokinetics of moxifloxacin by the dynamics of its distribution in the blood plasma and saliva of healthy volunteers: a comparative analysis and possible extrapolation methods.
Kondratenko, SN; Shikh, EV; Zolkina, IV, 2020
)
1.07
"The developed method of concentration extrapolation allows the use of saliva for pharmacokinetic studies of the tablet preparations of moxifloxacin."( A study of the pharmacokinetics of moxifloxacin by the dynamics of its distribution in the blood plasma and saliva of healthy volunteers: a comparative analysis and possible extrapolation methods.
Kondratenko, SN; Shikh, EV; Zolkina, IV, 2020
)
1.04
" Thus, we used this method to assess the pharmacokinetic (PK) characteristics of MFH and DSP in rabbit ocular tissues and plasma after single doses."( Simultaneous Determination of Moxifloxacin Hydrochloride and Dexamethasone Sodium Phosphate in Rabbit Ocular Tissues and Plasma by LC-MS/MS: Application for Pharmacokinetics Studies.
Qiao, H; Shao, Q; Yuan, Y; Zhao, X, 2022
)
1.01

Compound-Compound Interactions

Study describes the synergistic activity of oritavancin in combination with gentamicin, linezolid, moxifloxacin, or rifampin in time-kill studies against methicillin-susceptible and vancomycin-resistant Staphylococcus aureus.

ExcerptReferenceRelevance
"Killing kinetic experiments were performed with moxifloxacin, a novel fluoroquinolone, vancomycin, clarithromycin, cotrimoxazole, gentamicin, rifampicin and with moxifloxacin in combination with each of the above drugs against six methicillin-resistant Staphylococcus aureus clinical isolates."( In-vitro activity of moxifloxacin combined with other antibacterials against methicillin-resistant Staphylococcus aureus.
Bottura, P; Capra, R; Maggiolo, F; Migliorino, M; Pravettoni, G; Suter, F, 2000
)
0.88
" Moxifloxacin at both concentrations in combination with ethambutol was significantly more active than each drug alone."( Activity of moxifloxacin by itself and in combination with ethambutol, rifabutin, and azithromycin in vitro and in vivo against Mycobacterium avium.
Aralar, P; Bermudez, LE; Inderlied, CB; Kolonoski, P; Petrofsky, M; Wu, M; Young, LS, 2001
)
1.6
"The bactericidal activity of moxifloxacin alone and in combination with cefepime or piperacillin-tazobactam against clinical isolates of Klebsiella pneumoniae, Enterobacter cloacae, and Acinetobacter baumannii was evaluated by using time-kill methods and antimicrobial concentrations of one-half and one times the MIC."( Synergistic activities of moxifloxacin combined with piperacillin-tazobactam or cefepime against Klebsiella pneumoniae, Enterobacter cloacae, and Acinetobacter baumannii clinical isolates.
Choi, MK; Fish, DN; Husain, M; Jung, R, 2004
)
0.91
"In previous studies, the diarylquinoline R207910 (also known as TMC207) was demonstrated to have high bactericidal activity when combined with first- or second-line antituberculous drugs."( Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
Andries, K; Chauffour, A; Ibrahim, M; Jarlier, V; Lounis, N; Truffot-Pernot, C; Veziris, N, 2007
)
0.34
" When the three FQs were individually combined with CLR in vitro, mild antagonism was observed for 53 to 57% of the tested isolates."( In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
Fukushima, K; Higashiyama, Y; Hirakata, Y; Kohno, S; Kohno, Y; Miyazaki, Y; Ohno, H; Yanagihara, K, 2007
)
0.34
"Our objective is to determine in vitro efficiency of moxifloxacin (MXF) alone or in combination with cefotaxime (CTX) on Group B streptococcus (GBS)."( [In vitro activity of moxifloxacin (8-methoxyquinolone) alone or in combination with cefotaxime against group B streptococci].
Collignon, A; Cruaud, P; Gaudelus, J; Jacquier, H; Lachassinne, E; Poilane, I, 2007
)
0.9
" This study describes the synergistic activity of oritavancin in combination with gentamicin, linezolid, moxifloxacin, or rifampin in time-kill studies against methicillin-susceptible, vancomycin-intermediate, and vancomycin-resistant Staphylococcus aureus."( Assessment by time-kill methodology of the synergistic effects of oritavancin in combination with other antimicrobial agents against Staphylococcus aureus.
Arhin, FF; Belley, A; McKay, GA; Moeck, G; Neesham-Grenon, E; Parr, TR, 2008
)
0.56
"To evaluate the effectiveness of pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration."( Pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration.
Bennett, MD; Bryan, JS; Yee, W,
)
0.61
"This retrospective review included patients who received pegaptanib combined with 165 microg of moxifloxacin every 6 weeks."( Pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration.
Bennett, MD; Bryan, JS; Yee, W,
)
0.6
"Pegaptanib combined with intravitreal injection of moxifloxacin appears to be effective treatment of wet macular degeneration."( Pegaptanib combined with intravitreal injection of moxifloxacin as treatment of wet macular degeneration.
Bennett, MD; Bryan, JS; Yee, W,
)
0.64
" To assess drug-drug interactions, co-administration experiments were conducted with ketoconazole and either propranolol or erythromycin."( Exploration of the African green monkey as a preclinical pharmacokinetic model: oral pharmacokinetic parameters and drug-drug interactions.
Bhadresa, S; Coon, DJ; Lawrence, MS; Magiera, D; Struharik, M; Ward, KW, 2009
)
0.35
"This thorough corrected QT (QTc) study evaluated the effect of sugammadex alone and in combination with rocuronium or vecuronium on the individually corrected QTc interval (QTcI)."( Effects of sugammadex doses up to 32 mg/kg alone or in combination with rocuronium or vecuronium on QTc prolongation: a thorough QTc study.
de Kam, PJ; Peeters, P; Prohn, M; Thomsen, T; van Kuijk, J, 2010
)
0.36
"Based on the results of this study of healthy subjects, it can be concluded that sugammadex alone or in combination with rocuronium or vecuronium is not associated with QTc prolongation."( Effects of sugammadex doses up to 32 mg/kg alone or in combination with rocuronium or vecuronium on QTc prolongation: a thorough QTc study.
de Kam, PJ; Peeters, P; Prohn, M; Thomsen, T; van Kuijk, J, 2010
)
0.36
" Simulated regimens included vancomycin (VAN) plus rifampin (RIF), moxifloxacin (MOX), and high doses (10 mg/kg of body weight/day) of daptomycin (DAP) alone or combined with RIF or clarithromycin (CLA)."( Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
Parra-Ruiz, J; Rose, WE; Rybak, MJ; Vidaillac, C, 2010
)
0.85
"In vivo metabolites of moxifloxacin have been identified and characterized by using LC/ESI-MS/MS in combination with an online hydrogen/deuterium (H/D) exchange technique."( In vivo metabolic investigation of moxifloxacin using liquid chromatography/electrospray ionization tandem mass spectrometry in combination with online hydrogen/deuterium exchange experiments.
Banerjee, SK; Borkar, RM; Padiya, R; Raju, B; Ramesh, M; Srinivas, R, 2012
)
0.97
"A total of 19 in vivo metabolites of moxifloxacin have been characterized using LC/ESI-MS/MS in combination with accurate mass measurements and online H/D exchange experiments."( In vivo metabolic investigation of moxifloxacin using liquid chromatography/electrospray ionization tandem mass spectrometry in combination with online hydrogen/deuterium exchange experiments.
Banerjee, SK; Borkar, RM; Padiya, R; Raju, B; Ramesh, M; Srinivas, R, 2012
)
0.93
" Therefore, this fluoroquinolone seems to be the most appropriate in combination with this tyrosine kinase inhibitor."( Pharmacokinetics of sunitinib in combination with fluoroquinolones in rabbit model.
Grabowski, T; Grześkowiak, E; Karbownik, A; Sobańska, K; Szałek, E; Wolc, A, 2013
)
0.39
"5 months) with PBCO underwent autogenously fecal peritonitis, and were treated with moxifloxacin combined with dexamethasone, and followed-up for 45 days."( Severe autogenously fecal peritonitis in Wistar rats with permanent bilateral carotid occlusion. Response to intra peritoneal moxifloxacin combined with dexamethasone.
Brandt, CT; Gadelha, DN; Melo, MC; Oliveira, TK, 2014
)
0.83
"The treatment of severe autogenously fecal peritonitis with intraperitoneal moxifloxacin combined with dexamethasone was very effective in young rats without permanent bilateral carotid occlusion."( Severe autogenously fecal peritonitis in Wistar rats with permanent bilateral carotid occlusion. Response to intra peritoneal moxifloxacin combined with dexamethasone.
Brandt, CT; Gadelha, DN; Melo, MC; Oliveira, TK, 2014
)
0.84
"To evaluate and compare the antimicrobial properties of propolis and calcium hydroxide alone and in combination with ciprofloxacin and moxifloxacin against Enterococcus faecalis (E."( An in vitro Comparison of Endodontic Medicaments Propolis and Calcium Hydroxide alone and in Combination with Ciprofloxacin and Moxifloxacin against Enterococcus Faecalis.
Gupta, K; Kumar, A; Rai, VK; Sabharwal, S; Shrivastava, R; Sinha, S; Tripathi, P, 2015
)
0.83
"The laboratory study was carried out to test the effectiveness of propolis and calcium hydroxidealone as well as in combination with the established endodontic medicaments (moxifloxacin and ciprofloxacin)."( An in vitro Comparison of Endodontic Medicaments Propolis and Calcium Hydroxide alone and in Combination with Ciprofloxacin and Moxifloxacin against Enterococcus Faecalis.
Gupta, K; Kumar, A; Rai, VK; Sabharwal, S; Shrivastava, R; Sinha, S; Tripathi, P, 2015
)
0.82
" Propolis in combination with antibiotics and alone is more effective than calcium hydroxide."( An in vitro Comparison of Endodontic Medicaments Propolis and Calcium Hydroxide alone and in Combination with Ciprofloxacin and Moxifloxacin against Enterococcus Faecalis.
Gupta, K; Kumar, A; Rai, VK; Sabharwal, S; Shrivastava, R; Sinha, S; Tripathi, P, 2015
)
0.62
"Since propolis alone and in combination with antibiotics was observed to be more effective than calcium hydroxide, propolis can be considered as an intracanal medicament when compared to traditional calcium hydroxide."( An in vitro Comparison of Endodontic Medicaments Propolis and Calcium Hydroxide alone and in Combination with Ciprofloxacin and Moxifloxacin against Enterococcus Faecalis.
Gupta, K; Kumar, A; Rai, VK; Sabharwal, S; Shrivastava, R; Sinha, S; Tripathi, P, 2015
)
0.62
" However, the potential drug-drug interactions between moxifloxacin and rifampicin were unknown."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
0.97
" Ultimately, the good permeability, moderate rates of metabolism and low risk of drug-drug interactions displayed by some of the synthesized compounds indicate that 2-(quinolin-4-yloxy)acetamides may yield candidates to use in the development of novel alternative therapeutics for tuberculosis treatment."( New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
Abbadi, BL; Back, DF; Basso, LA; Campos, MM; Giacobbo, BC; Grams, ES; Machado, P; Pissinate, K; Rodrigues-Junior, V; Santos, DS; Sperotto, N; Subtil, FT; Trindade, RV; Villela, AD, 2017
)
0.46
" In addition, the activity of the moxifloxacin + linezolid backbone in combination with one of the potentiator drugs was assessed."( Activity of moxifloxacin and linezolid against Mycobacterium tuberculosis in combination with potentiator drugs verapamil, timcodar, colistin and SQ109.
Aarnoutse, RE; de Knegt, GJ; de Steenwinkel, JE; de Vogel, CP; van der Meijden, A, 2017
)
1.11
" In this regard, the present study was conducted with the aim of studying the efficacy of using fixed drug combination (Difluprednate and Moxifloxacin) in reducing ocular inflammation and pain in post-operative patients undergoing cataract surgery."( Safety of Fixed drug Combination in Post -Operative Cataract Patients, at Tertiary Care Centre - In South India.
Anuradha, A; Nishath, S; Rashmi, G; Shilpa, R; Vidyadevi, M, 2017
)
0.66
"Our study clearly shows that fixed drug combination of antibiotic and steroid does not cause raised IOP in about 97% of cases of SICS in the post-operative period and also improves the compliance of the patients."( Safety of Fixed drug Combination in Post -Operative Cataract Patients, at Tertiary Care Centre - In South India.
Anuradha, A; Nishath, S; Rashmi, G; Shilpa, R; Vidyadevi, M, 2017
)
0.46
"3% solutions alone or when treatment was combined with steroids, and to correlate these concentrations with the minimum inhibitory concentrations (MIC) for the most common endophthalmitis-causing organisms."( Aqueous humor concentrations of topical fluoroquinolones alone or in combination with a steroid.
Campos, M; Cruz, AC; Gomes, RLR; Lima, AAS; Melo, LAS; Suenaga, EM; Viana, RG,
)
0.13
" Pretomanid (PA-824), a nitroimidazooxazine compound, is a new drug for the treatment of pulmonary TB that was recently approved in the United States and Europe in the context of a regimen combined with bedaquiline and linezolid."( Phase 1 Study of the Effects of the Tuberculosis Treatment Pretomanid, Alone and in Combination With Moxifloxacin, on the QTc Interval in Healthy Volunteers.
El-Amin, W; Everitt, D; Li, M; Makhene, MK; Nedelman, J; Osborn, B; Saviolakis, GA; Yang, TJ, 2021
)
0.84
" Given the prohibitive drug-drug interactions between bedaquiline and rifampin or rifapentine, the BZMRb regimen represents the best opportunity to combine, in one regimen, the treatment-shortening potential of the rifamycin class with that of BZM and deserves high priority for evaluation in clinical trials."( Novel Regimens of Bedaquiline-Pyrazinamide Combined with Moxifloxacin, Rifabutin, Delamanid and/or OPC-167832 in Murine Tuberculosis Models.
Carr, W; Converse, PJ; Dartois, V; Dooley, KE; Garcia, A; Kurbatova, E; Nuermberger, EL; Stout, JE; Tasneen, R; Vernon, AA; Zimmerman, MD, 2022
)
0.97
" Delpazolid is administered in combination with bedaquiline, delamanid and moxifloxacin."( A phase IIb, open-label, randomized controlled dose ranging multi-centre trial to evaluate the safety, tolerability, pharmacokinetics and exposure-response relationship of different doses of delpazolid in combination with bedaquiline delamanid moxifloxaci
Aarnoutse, R; Boeree, M; Cho, YL; Dierig, A; Geiter, L; Gong, X; Heinrich, N; Hoelscher, M; Hoffmann, L; Jarchow-MacDonald, A; Liyoyo, A; Mbeya, B; McHugh, TD; Mhimbira, FA; Minja, LT; Mpagama, S; Ntinginya, N; Phillips, P; Rassool, M; Schultz, S; Sebe, M; Svensson, EM; Te Brake, L; Wallis, RS; Wildner, LM, 2023
)
1.14

Bioavailability

Concomitant ingestion with sucralfate and/or oral Al3+-containing antacids significantly reduces the bioavailability of moxifloxacin. ABCB1 SNP rs2032582 (40% reduced bioavailability in one individual) was significantly associated with changes in mox iflxacin pharmacokinetic parameters.

ExcerptReferenceRelevance
" In common with other fluoroquinolones, moxifloxacin attains good penetration into respiratory tissues and fluids and its bioavailability is substantially reduced by coadministration with an antacid or iron preparation."( Moxifloxacin.
Balfour, JA; Wiseman, LR, 1999
)
2.01
" To determine the absolute bioavailability of moxifloxacin, this open-label, randomized, crossover study compared the pharmacokinetic characteristics of a single 100-mg dose administered either orally or intravenously as a 60-minute infusion in 10 healthy male volunteers (mean age [+/- SD], 29."( Absolute bioavailability of moxifloxacin.
Agarwal, V; Ballow, C; Lettieri, J; Liu, P; Stass, H; Sullivan, JT, 1999
)
0.86
" Bioavailability was high to moderate (91-52%) in all species."( Pharmacokinetics of the 8-methoxyquinolone, moxifloxacin: a comparison in humans and other mammalian species.
Domdey-Bette, A; Henninger, K; Hucke, F; Kohlsdorfer, C; Siefert, HM; Stass, HH, 1999
)
0.56
" The absolute bioavailability was 86%."( Pharmacokinetics and elimination of moxifloxacin after oral and intravenous administration in man.
Kubitza, D; Stass, H, 1999
)
0.58
" Moxifloxacin has an absolute bioavailability of 90% after oral administration and a mean elimination half-life of 12 hours."( Moxifloxacin: clinical efficacy and safety.
Culley, CM; Edwards, B; Klutman, N; Lacy, MK, 2001
)
2.66
"The extent of absorption of moxifloxacin is not affected by concomitant Ca2+ intake, whereas the rate of absorption is slightly reduced, an effect not considered to be of clinical relevance."( Effect of calcium supplements on the oral bioavailability of moxifloxacin in healthy male volunteers.
Delesen, H; Möller, JG; Stass, H; Wandel, C, 2001
)
0.85
"To determine the effect of concomitant administration of the antacid Maalox 70 or the histamine H2 receptor antagonist ranitidine on the bioavailability of moxifloxacin."( Evaluation of the influence of antacids and H2 antagonists on the absorption of moxifloxacin after oral administration of a 400mg dose to healthy volunteers.
Böttcher, MF; Ochmann, K; Stass, H, 2001
)
0.74
"3 mg/L x h with versus without ranitidine; relative bioavailability 103%, 90% confidence interval (CI) 97."( Evaluation of the influence of antacids and H2 antagonists on the absorption of moxifloxacin after oral administration of a 400mg dose to healthy volunteers.
Böttcher, MF; Ochmann, K; Stass, H, 2001
)
0.54
"The bioavailability of moxifloxacin is not affected by concurrent administration of ranitidine."( Evaluation of the influence of antacids and H2 antagonists on the absorption of moxifloxacin after oral administration of a 400mg dose to healthy volunteers.
Böttcher, MF; Ochmann, K; Stass, H, 2001
)
0.85
" The concomitant administration of Al3+ reduced the bioavailability of moxifloxacin [geometric mean area under the concentration-time curve from zero to infinity (AUCinfinity) 12."( Effects of sucralfate on the oral bioavailability of moxifloxacin, a novel 8-methoxyfluoroquinolone, in healthy volunteers.
Delesen, H; Möller, JG; Schühly, U; Stass, H, 2001
)
0.79
"Concomitant ingestion with sucralfate and/or oral Al3+-containing antacids significantly reduces the bioavailability of moxifloxacin."( Effects of sucralfate on the oral bioavailability of moxifloxacin, a novel 8-methoxyfluoroquinolone, in healthy volunteers.
Delesen, H; Möller, JG; Schühly, U; Stass, H, 2001
)
0.77
" The concomitant administration of Eryfer reduced the bioavailability of moxifloxacin [geometric mean area under the plasma concentration-time curve 20."( Effects of iron supplements on the oral bioavailability of moxifloxacin, a novel 8-methoxyfluoroquinolone, in humans.
Kubitza, D; Stass, H, 2001
)
0.79
"Concomitant ingestion of iron supplements significantly reduces the bioavailability of moxifloxacin."( Effects of iron supplements on the oral bioavailability of moxifloxacin, a novel 8-methoxyfluoroquinolone, in humans.
Kubitza, D; Stass, H, 2001
)
0.78
" The bioavailability of moxifloxacin is substantially reduced by coadministration with antacids or iron preparations."( Moxifloxacin in uncomplicated skin and skin structure infections.
Jarvis, B; Muijsers, RB, 2002
)
2.06
" The bioavailability and half-life of moxifloxacin provides potent bactericidal effects at a dose of 400mg/day."( Moxifloxacin in respiratory tract infections.
Miravitlles, M, 2005
)
2.04
"To evaluate the extent to which enterohepatic recycling circulation contributes to moxifloxacin bioavailability in healthy, males by administration of activated charcoal and to evaluate the efficacy of activated charcoal administration in decreasing systemic concentrations of moxifloxacin in the event of overdose."( Influence of activated charcoal on the pharmacokinetics of moxifloxacin following intravenous and oral administration of a 400 mg single dose to healthy males.
Delesen, H; Kubitza, D; Möller, JG; Stass, H, 2005
)
0.8
" The bioavailability of moxifloxacin was significantly decreased when given with charcoal (AUC = 35."( Influence of activated charcoal on the pharmacokinetics of moxifloxacin following intravenous and oral administration of a 400 mg single dose to healthy males.
Delesen, H; Kubitza, D; Möller, JG; Stass, H, 2005
)
0.88
" The absolute bioavailability was 96."( Pharmacokinetics and milk penetration of moxifloxacin after intravenous and subcutaneous administration to lactating goats.
Cárceles, CM; Escudero, E; Espuny, A; Fernández-Varón, E; Villamayor, L, 2006
)
0.6
" These agents are highly bioavailable and can facilitate the oral treatment of certain patients who otherwise might be admitted to the hospital, as outpatients."( Challenges in the management of community-acquired pneumonia: the role of quinolones and moxifloxacin.
Niederman, MS, 2005
)
0.55
" Thus, the rate of absorption of moxifloxacin was not affected by administration through a nasogastric tube."( Effects of enteral feeding on the oral bioavailability of moxifloxacin in healthy volunteers.
Borner, K; Burkhardt, O; Stass, H; Thuss, U; Welte, T, 2005
)
0.85
"5% exhibits enhanced bioavailability due to a unique molecular structure that combines high lipophilicity for enhanced corneal penetration with high aqueous solubility at physiological pH."( Ophthalmic infections and their anti-infective challenges.
Alfonso, E; Crider, J, 2005
)
0.33
" 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
" The IM bioavailability was 96."( Disposition kinetics of moxifloxacin in lactating ewes.
Goudah, A, 2008
)
0.65
" The bioavailability and half-life ofmoxifloxacin provides potent bactericidal effects at a dose of 400 mg once daily."( Moxifloxacin in the management of exacerbations of chronic bronchitis and COPD.
Miravitlles, M, 2007
)
2.06
"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
" Meanwhile, plasma protein binding and bioavailability of moxifloxacin were also estimated."( Pharmacokinetics and bioavailability of moxifloxacin in calves following different routes of administrations.
Goudah, A; Hasabelnaby, S, 2010
)
0.87
"A high peak plasma concentration, area under the curve, rapid absorption and bioavailability following intramuscular and subcutaneous administration characterize the pharmacokinetics of moxifloxacin in calves."( Pharmacokinetics and bioavailability of moxifloxacin in calves following different routes of administrations.
Goudah, A; Hasabelnaby, S, 2010
)
0.82
" The systemic bioavailability (F) of moxifloxacin in buffalo calves was 80."( Pharmacokinetics and bioavailability of moxifloxacin in buffalo calves.
Pathania, R; Sharma, SK, 2010
)
0.9
"Conventional eye drops show relatively low bioavailability due to poor precorneal contact time."( Design and Development of Thermoreversible Ophthalmic In Situ Hydrogel of Moxifloxacin HCl.
Patel, LD; Prajapati, ST; Shastri, DH, 2010
)
0.59
" Mean (95% confidence interval) values for oral clearance, apparent volume of distribution, the first-order absorption rate constant, and mean transit time were 11."( Population pharmacokinetic and concentration--QTc models for moxifloxacin: pooled analysis of 20 thorough QT studies.
Brundage, R; Florian, JA; Garnett, CE; Parekh, A; Tornøe, CW, 2011
)
0.61
" Oral bioavailability was 79."( Pharmacokinetics of moxifloxacin in plasma and tissue of morbidly obese patients.
Horbach, T; Kees, F; Kees, MG; Weber, S, 2011
)
0.69
" This anatomical alteration may affect the absorption and consequently the bioavailability of oral drugs."( Oral bioavailability of moxifloxacin after Roux-en-Y gastric bypass surgery.
Batens, H; Blot, S; Boussery, K; Colin, P; De Paepe, P; De Smet, J; Ruige, J; Van Bocxlaer, J; Van Bortel, LM; Van Nieuwenhove, Y; Vogelaers, D, 2012
)
0.69
"3 mg · h/L after intravenous dosing, resulting in a mean oral bioavailability of 88."( Oral bioavailability of moxifloxacin after Roux-en-Y gastric bypass surgery.
Batens, H; Blot, S; Boussery, K; Colin, P; De Paepe, P; De Smet, J; Ruige, J; Van Bocxlaer, J; Van Bortel, LM; Van Nieuwenhove, Y; Vogelaers, D, 2012
)
0.69
" Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms."( Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.
Deshmukh, RV; Gaikwad, KR; Manvi, FV; Nanjwade, BK; Parikh, KA, 2012
)
0.63
" An early switch from intravenous to enteral moxifloxacin may be considered because of its good oral bioavailability in healthy volunteers."( Switch from intravenous to enteral moxifloxacin in critically ill patients: a pilot study.
Boussery, K; Colpaert, K; de Paepe, P; de Smet, J; Decruyenaere, J; van Bocxlaer, J, 2012
)
0.92
"Thorough QT studies are typically conducted for drugs with systemic bioavailability and include a positive control, typically moxifloxacin, with a well-described QTc effect."( Impact of electrocardiographic data quality on moxifloxacin response in thorough QT/QTc studies.
Garnett, C; Johannesen, L; Malik, M, 2014
)
0.87
" Lead optimization resulted in the identification of potent compounds with improved oral bioavailability and reduced cardiac ion channel liability."( Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
Achar, V; Arora, U; Awasthy, D; Bharath, S; Bheemarao, U; Chinnapattu, M; Coulson, M; de Sousa, SM; Ganguly, S; Gaonkar, S; Ghosh, A; Hameed P, S; Hoffner, S; Humnabadkar, V; Kaur, P; Kumar K N, M; Kumar, CN; Madhavapeddi, P; Manjrekar, P; Menasinakai, S; Mukherjee, K; Nandishaiah, R; Narayan, C; Panduga, V; Patil, V; Puttur, J; Raichurkar, A; Ramya, VK; Reddy, J; Rudrapatana, S; Sambandamurthy, VK; Shanbhag, G; Sharma, S; Sharma, U; Shinde, V; Solapure, S; Waterson, D; Werngren, J, 2014
)
0.4
"The aim of this investigation was to identify the impact of physicochemical properties of three fluoroquinolones (second, third, and fourth generation) on bioavailability in relation to the Biopharmaceutics Classification System (BCS) by in silico and in vitro methods."( Physicochemical properties of lomefloxacin, levofloxacin, and moxifloxacin relevant to the biopharmaceutics classification system.
Betlejewska-Kielak, K; Biernacka, J; Grudzień, M; Kłosińska-Szmurło, E; Mazurek, AP; Pluciński, F, 2014
)
0.64
"The developed MEs are a viable alternative to conventional eye drops, because of its ability to enhance bioavailability through its longer precorneal residence time and its ability to sustain the release of the drug."( Phase-transition W/O Microemulsions for Ocular Delivery: Evaluation of Antibacterial Activity in the Treatment of Bacterial Keratitis.
Bharti, SK; Kesavan, K, 2017
)
0.46
" However, the Caco-2 cell transwell experiment showed that moxifloxacin could not affect the absorption rate of rifampicin."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
0.96
"Currently, infections following cataract surgery are not as effectively managed with antibiotic eye drops, which suffer from poor bioavailability of drug and low patient compliance."( Sustained Antibiotic-Eluting Intra-Ocular Lenses: A New Approach.
Lim, SG; Tan, DW; Venkatraman, SS; Wong, TT, 2016
)
0.43
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
" The addition of other orally bioavailable anti-staphylococcal agents to tedizolid may be unlikely to improve killing but further research is warranted to assess the impact of these combinations on resistance prevention, or against biofilm-embedded organisms."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
"6% increased clearance, respectively) and ABCB1 SNP rs2032582 (40% reduced bioavailability in one individual) were significantly associated with changes in moxifloxacin pharmacokinetic parameters."( Effect of genetic variation in UGT1A and ABCB1 on moxifloxacin pharmacokinetics in South African patients with tuberculosis.
Chaudhry, M; Chirehwa, M; Denti, P; McIlleron, H; Naidoo, A; Naidoo, K; Ngcapu, S; Padayatchi, N; Pepper, MS; Ramsuran, V; Singh, R; Yende-Zuma, N, 2018
)
0.93
" These compounds were found to be orally bioavailable and highly effective."( Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
Eswaran, S; Narayanan, S; Shivarudraiah, P; Shruthi, TG; Subramanian, S, 2019
)
0.51
" Two modified melittin peptides displayed rapid bactericidal properties against antibiotic-resistant strains, low innate resistance development by pathogenic bacteria, remained nonimmunogenic for T lymphocytes, and increased bioavailability in tear fluids."( Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
Agrawal, R; Barathi, VA; Beuerman, RW; Chan, LW; Jie, TY; Koh, SK; Lakshminarayanan, R; Leng, ET; Mayandi, V; Sebastian, TM; Somaraju Chalasani, ML; Ting, DSJ; Urf Turabe Fazil, MH; Varadarajan, J; Verma, NK; Xi, Q; Zhou, L, 2020
)
0.56
"Considering the low ocular bioavailability of conventional formulations used for ocular bacterial infection treatment, there is a need to design efficient novel drug delivery systems that may enhance precorneal retention time and corneal permeability."( Moxifloxacin Hydrochloride-Loaded Eudragit® RL 100 and Kollidon® SR Based Nanoparticles: Formulation, In vitro Characterization and Cytotoxicity.
Büyükköroğlu, G; Kırımlıoğlu, GY; Özer, S; Yazan, Y, 2021
)
2.06
"Maribavir is an orally bioavailable benzimidazole riboside in clinical development for treatment of cytomegalovirus infection in patients who undergo transplantation."( Evaluation of the Effect of Maribavir on Cardiac Repolarization in Healthy Participants: Thorough QT/QTc Study.
Ilic, K; Martin, P; Song, I; Wu, J, 2020
)
0.56
"In situ gels have been extensively explored as ocular drug delivery system to enhance bioavailability and efficacy."( Experimental design, formulation and in vivo evaluation of a novel topical in situ gel system to treat ocular infections.
Al-Dhubiab, BE; Attimarad, M; Gupta, S; Jacob, S; Morsy, MA; Nair, AB; Shah, J; Shinu, P; Sreeharsha, N; Venugopala, KN, 2021
)
0.62
" The estimated extent of oral bioavailability was highly variable (range 20-91%)."( Population Pharmacokinetics of Moxifloxacin in Children.
Conrad, T; Ghazaryhan, V; Greenberg, RG; Gu, K; Harward, M; Kirkpatrick, CM; Landersdorfer, CB; Nakamura, A; Osborn, B; Rivera-Chaparro, N; Walter, EB, 2022
)
1.01
" To address this issue, we utilized a murine model of antibiotic-induced dysbiosis to assay the bioavailability of rifampicin, moxifloxacin, pyrazinamide, and isoniazid in mouse plasma over a period of 12 h following individual oral administration."( The Dysbiosis Triggered by First-Line Tuberculosis Antibiotics Fails to Reduce Their Bioavailability.
Dartois, V; Mittereder, LR; Namasivayam, S; Oland, S; Sher, A; Wang, H; Zimmerman, M, 2023
)
1.12

Dosage Studied

Moxifloxacin hydrochloride may be administered together with Ca2+ without dosage adjustments or special recommendations. According to these findings, anuric critically ill patients who are undergoing EDD should be treated with the standard dosage of moxifLoxacins intravenously.

ExcerptRelevanceReference
" The activity of moxifloxacin could be described by a sigmoid dose-response curve with a maximum effect of -0."( Moxifloxacin in the therapy of experimental pneumococcal meningitis.
Brück, W; Chen, V; Dalhoff, A; Kohlsdorfer, C; Nau, R; Schmidt, H; Schneider, O; Stuertz, K; Trostdorf, F, 1998
)
2.08
" tuberculosis, whereas both SPFX and MXFX were effective; administration six times weekly of either of the latter two drugs demonstrated dosage-dependent bactericidal effects, as measured by enumeration of CFU in the spleens, and MXFX appeared more bactericidal than the same dosage of SPFX."( In vitro and in vivo activities of moxifloxacin and clinafloxacin against Mycobacterium tuberculosis.
Bonnafous, P; Grosset, J; Ji, B; Lounis, N; Maslo, C; Truffot-Pernot, C, 1998
)
0.58
" Gram-positive and gram-negative organisms were also exposed to concentrations of moxifloxacin, sparfloxacin and amoxycillin that simulated the drug concentrations obtained in human serum after standard oral dosing schedules."( Bactericidal properties of moxifloxacin and post-antibiotic effect.
Andrews, JM; Boswell, FJ; Dalhoff, A; Wise, R, 1999
)
0.83
" and oral dosing similar concentrations of the unchanged compound were determined in skin suction blister fluid and plasma."( Pharmacokinetics of the 8-methoxyquinolone, moxifloxacin: tissue distribution in male rats.
Kohlsdorfer, C; Siefert, HM; Steinke, W; Witt, A, 1999
)
0.56
" On the basis of preclinical studies a terminal half-life appropriate for once-daily dosing in humans was predicted and confirmed by Phase I data."( Pharmacokinetics of the 8-methoxyquinolone, moxifloxacin: a comparison in humans and other mammalian species.
Domdey-Bette, A; Henninger, K; Hucke, F; Kohlsdorfer, C; Siefert, HM; Stass, HH, 1999
)
0.56
" After an overnight fast the volunteers were given a single 400 mg dosage of moxifloxacin either as a tablet or a 1 h infusion with a washout phase of at least 1 week between the two treatments."( Pharmacokinetics and elimination of moxifloxacin after oral and intravenous administration in man.
Kubitza, D; Stass, H, 1999
)
0.81
" Plasma moxifloxacin concentrations exceeded the MIC for Streptococcus pneumoniae throughout the 24-h dosing period."( Pharmacokinetics of a once-daily oral dose of moxifloxacin (Bay 12-8039), a new enantiomerically pure 8-methoxy quinolone.
Agarwal, V; Heller, AH; Krol, GJ; Leese, PT; Lettieri, J; Sullivan, JT; Watson, S; Woodruff, M, 1999
)
1
" It shows a low potential for drug interactions and dosage adjustment is not required for patients of advanced age or those with renal or mild hepatic impairment."( Moxifloxacin: a review of its clinical potential in the management of community-acquired respiratory tract infections.
Balfour, JA; Lamb, HM, 2000
)
1.75
" Because of a balanced system of excretion, no dosage adjustments are required in patients with renal or hepatic impairment."( Moxifloxacin, a new antibiotic designed to treat community-acquired respiratory tract infections: a review of microbiologic and pharmacokinetic-pharmacodynamic characteristics.
Nightingale, CH, 2000
)
1.75
" The possibility of once-daily dosing of the drug is strengthened."( Effects of subinhibitory concentrations of moxifloxacin in an in-vitro dynamic model.
Bartoli, A; Bottura, P; Capra, R; Maggiolo, F; Migliorino, M; Suter, F, 2000
)
0.57
"4 (100%), respectively, over the dosing period."( Streptococcus pneumoniae response to repeated moxifloxacin or levofloxacin exposure in a rabbit tissue cage model.
Bui, KQ; Mattoes, H; McNabb, J; Nicolau, DP; Nightingale, CH; Quintiliani, R; Xuan, D; Zhong, M, 2001
)
0.57
" Administered as single doses, MXFX in a dosage of 150 mg per kg was more active than OFLO in the same dosage, and displayed the same level of activity as RMP in a dosage of 10 mg per kg; the combination MXFX-minocycline (MINO) (MM) was more bactericidal than the combination OFLO-MINO (OM); RPT in a dosage of 10 mg per kg was more bactericidal than RMP administered in the same dosage, and even more active than the combination RMP-OFLO-MINO (ROM); the combination RPT-MXFX-MINO (PMM) killed 99."( Combination of rifapentine-moxifloxacin-minocycline (PMM) for the treatment of leprosy.
Grosset, J; Ji, B, 2000
)
0.6
"The activity, pharmacokinetics, pharmacodynamics, efficacy, safety, drug interactions, and dosage and administration of moxifloxacin are reviewed."( Moxifloxacin: clinical efficacy and safety.
Culley, CM; Edwards, B; Klutman, N; Lacy, MK, 2001
)
1.96
" Accumulation ratios ranged between 87% for the lowest dosage and 111% after repeated doses of 600mg once daily, indicating the absence of clinically relevant accumulation due to non-linear pharmacokinetics."( Pharmacokinetics, safety and tolerability of moxifloxacin, a novel 8-methoxyfluoroquinolone, after repeated oral administration.
Kubitza, D; Schühly, U; Stass, H, 2001
)
0.57
"These studies indicate that, based on the safety profile and the pharmacokinetic behaviour of moxifloxacin, a dosage regimen of 400mg given once daily should be effective and well tolerated for the treatment of various infections."( Pharmacokinetics, safety and tolerability of moxifloxacin, a novel 8-methoxyfluoroquinolone, after repeated oral administration.
Kubitza, D; Schühly, U; Stass, H, 2001
)
0.79
" Hence, moxifloxacin may be administered together with Ca2+ without dosage adjustments or special recommendations."( Effect of calcium supplements on the oral bioavailability of moxifloxacin in healthy male volunteers.
Delesen, H; Möller, JG; Stass, H; Wandel, C, 2001
)
0.99
" Moxifloxacin, given once daily, is free of many drug-drug interactions and requires no dosage adjustments in most renal hepatic deficient patients."( The efficacy and safety of two oral moxifloxacin regimens compared to oral clarithromycin in the treatment of community-acquired pneumonia.
Hoeffken, G; Meyer, HP; Verhoef, L; Winter, J, 2001
)
1.5
" All quinolones tested selected for resistance; judicious use and proper dosing will be necessary to avoid resistance selection of newer broad-spectrum fluoroquinolones."( Single- and multi-step resistance selection study of gemifloxacin compared with trovafloxacin, ciprofloxacin, gatifloxacin and moxifloxacin in Streptococcus pneumoniae.
Appelbaum, PC; Davies, TA; Dewasse, BE; Jacobs, MR; Nagai, K, 2001
)
0.52
"The aim of this study was to compare the efficacy and safety of once daily dosing with moxifloxacin (BAY 12-8039) with that of coamoxiclav given three times daily for the treatment of acute exacerbation of chronic bronchitis (AECB)."( A multinational, multicentre, non-blinded, randomized study of moxifloxacin oral tablets compared with co-amoxiclav oral tablets in the treatment of acute exacerbation of chronic bronchitis.
Ballin, I; Bassaris, H; Hampel, B; Huchon, G; Reimnitz, P; Schaberg, T,
)
0.59
" Gatifloxacin should be avoided in the same patient population, and the recommended dosage of 400 mg/day should not be exceeded."( Rates of torsades de pointes associated with ciprofloxacin, ofloxacin, levofloxacin, gatifloxacin, and moxifloxacin.
Frothingham, R, 2001
)
0.53
" Dosage adjustments are not required in patients with renal impairment or in patients with mild to moderate hepatic insufficiency."( Moxifloxacin in uncomplicated skin and skin structure infections.
Jarvis, B; Muijsers, RB, 2002
)
1.76
" The concentration at which the CRT equals the dosing interval is the minimum effective concentration, and is effectively the breakpoint."( Calculation of composite recovery time: a new pharmacodynamic parameter.
Gould, IM; MacKenzie, FM; Milne, KE, 2002
)
0.31
"Most integral endpoints of antimicrobial effect, including area between the control growth and time-kill curves (ABBC), area above the curve (AAC) and area under the time-kill curve (AUBC) are determined over a dosing interval (tau), regardless of the actual effect duration."( AUC/MIC relationships to different endpoints of the antimicrobial effect: multiple-dose in vitro simulations with moxifloxacin and levofloxacin.
Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2002
)
0.53
" Sixteen hours after inoculation, therapy was given by intravenous administration of BMS at 20 mg/kg of body weight, followed 5 h later by administration at a dosage of 10 mg/kg (n = 9 animals) or MOX as two doses of 20 mg/kg every 5 h (n = 8 animals)."( Garenoxacin (BMS-284756) and moxifloxacin in experimental meningitis caused by vancomycin-tolerant pneumococci.
Barton, T; Bowlware, K; Hardy, RD; Iglehart, J; Katz, K; McCoig, CC; McCracken, GH; Michelow, IC; Rodriguez-Cerrato, V; Saavedra, J, 2003
)
0.61
" AUC0-t/MIC was strongly associated with bacterial kill throughout the dosing interval."( AUC(0-t)/MIC is a continuous index of fluoroquinolone exposure and predictive of antibacterial response for Streptococcus pneumoniae in an in vitro infection model.
Ariano, RE; Harding, GK; Iacovides, H; Sun, S; Zelenitsky, SA, 2003
)
0.32
" For example, the cost implications of using manufacturers' recommendations for dosing in patients with renal dysfunction may be important, depending on the distribution of various levels of renal function within a patient population."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Also, costs of failing to adjust dosing regimens for decreased renal function were determined."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Costs potentially incurred by failing to adjust dosing for renal function were substantial."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
"Formulary decisions can be facilitated by considering factors such as patient characteristics and related dosing in addition to simple acquisition costs."( A novel method of estimating cost of therapy by using patient population characteristics: analysis of fluoroquinolones in various populations with different distributions of renal function.
Bosso, JA; Enzweiler, KA; White, RL, 2003
)
0.32
" Penetration of moxifloxacin into the interstitial space fluid of healthy and inflamed subcutaneous adipose tissues was measured by use of in vivo microdialysis following administration of a single intravenous dosage of 400 mg in six diabetic and six nondiabetic patients with STIs."( Penetration of moxifloxacin into healthy and inflamed subcutaneous adipose tissues in humans.
Joukhadar, C; Kovar, F; Lackner, E; Minar, E; Müller, M; Müller-Zellenberg, U; Stass, H, 2003
)
1.02
" For a dose-response study, moxifloxacin was given immediately after MCAO in different doses and at different time points."( Preventive antibacterial treatment improves the general medical and neurological outcome in a mouse model of stroke.
Braun, J; Dirnagl, U; Halle, E; Megow, D; Meisel, A; Meisel, C; Prass, K; Victorov, I; Volk, HD; Wolf, T, 2004
)
0.62
" The described methods were successfully employed with high precision and accuracy for estimation of the total drug content of human plasma and for pharmaceutical dosage forms of moxifloxacin."( Voltammetric behaviour and determination of moxifloxacin in pharmaceutical products and human plasma.
Erk, N, 2004
)
0.78
"To determine the steady-state, extracellular, and intracellular pulmonary disposition of moxifloxacin (MXF), levofloxacin (LEVO), and azithromycin (AZI) relative to that of the plasma over a 24-h dosing interval."( Steady-state intrapulmonary concentrations of moxifloxacin, levofloxacin, and azithromycin in older adults.
Braman, S; Capitano, B; Mattoes, HM; Nicolau, DP; O'Brien, A; Shore, E; Sutherland, C, 2004
)
0.8
"0 micro g/mL) throughout the dosing interval."( Steady-state intrapulmonary concentrations of moxifloxacin, levofloxacin, and azithromycin in older adults.
Braman, S; Capitano, B; Mattoes, HM; Nicolau, DP; O'Brien, A; Shore, E; Sutherland, C, 2004
)
0.58
" Significant increases in MIC were observed with monotherapy where moxifloxacin or doxycycline concentrations fell into the mutant selection window (MSW) for more than 80% of the dosing interval (AUC(24)/MIC 60 h)."( Prevention of the selection of resistant Staphylococcus aureus by moxifloxacin plus doxycycline in an in vitro dynamic model: an additive effect of the combination.
Firsov, AA; Lubenko, IY; Portnoy, YA; Vostrov, SN; Zinner, SH, 2004
)
0.8
" A placebo-controlled and positive-controlled, period-balanced, double-blinded, 6-way crossover study evaluated therapeutic and supratherapeutic oral doses of vardenafil (10 and 80 mg, respectively) and sildenafil (50 and 400 mg, respectively), therapeutic doses of moxifloxacin (400 mg), and a placebo in 58 healthy men (mean age 53 years), with dosing every 3 days."( Evaluation of vardenafil and sildenafil on cardiac repolarization.
Boyle, DA; Dabiri, GA; Ilson, BE; Montague, TH; Morganroth, J; Patel, BR; Sethuraman, VS; Shaddinger, BC, 2004
)
0.5
" Eyes were dosed according to a keratitis protocol; ie, every 15 minutes for 4 hours."( Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing.
Herrygers, L; Lane, LC; Levine, JM; Nix, D; Noecker, RJ; Snyder, RW, 2004
)
0.62
"In the keratitis dosing protocol, the mean concentration of moxifloxacin in the aqueous (n=9) was 11."( Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing.
Herrygers, L; Lane, LC; Levine, JM; Nix, D; Noecker, RJ; Snyder, RW, 2004
)
0.86
" There was no statistically significant difference between the 2 drugs in the cataract prophylaxis dosing model."( Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing.
Herrygers, L; Lane, LC; Levine, JM; Nix, D; Noecker, RJ; Snyder, RW, 2004
)
0.62
" Moxifloxacin has pharmacologic characteristics that support once-daily dosing regimens and dual routes of excretion that require little or no adjustment for renal or hepatic insufficiency."( Moxifloxacin (Avelox): a novel fluoroquinolone with a broad spectrum of activity.
Caeiro, JP; Iannini, PB, 2003
)
2.67
"To compare the effects of the commercial formulations of moxifloxacin and gatifloxacin on rabbit corneal epithelium using two dosing protocols: high-frequency dosing for bacterial keratitis and cataract surgery prophylaxis."( Comparison of corneal surface effects of gatifloxacin and moxifloxacin using intensive and prolonged dosing protocols.
Herrygers, LA; Lane, LC; Levine, JM; Noecker, RJ, 2005
)
0.82
"Despite differences in formulations, with short-term dosing neither gatifloxacin nor moxifloxacin appears to be toxic to the corneal epithelium in this rabbit model."( Comparison of corneal surface effects of gatifloxacin and moxifloxacin using intensive and prolonged dosing protocols.
Herrygers, LA; Lane, LC; Levine, JM; Noecker, RJ, 2005
)
0.8
" A dose-response effect on QT and QTc prolongation was observed."( Effects of moxifloxacin on QT interval in conscious dogs.
Hart, SM; Mittelstadt, SW, 2005
)
0.72
" We evaluated with the same model similar regimens in which we increased the dosing of rifapentine from 10 to 15 mg/kg of body weight and of moxifloxacin from 100 to 400 mg/kg."( Efficient intermittent rifapentine-moxifloxacin-containing short-course regimen for treatment of tuberculosis in mice.
Chauffour, A; Jarlier, V; Lounis, N; Truffot-Pernot, C; Veziris, N, 2005
)
0.81
" By selecting optimal antibiotics and dosing regimens, clinicians can avoid treatment failures and adverse events and can help prevent the emergence of further antibiotic resistance."( Overview of the potency of moxifloxacin ophthalmic solution 0.5% (VIGAMOX).
Alfonso, E; Schlech, BA, 2005
)
0.63
"5% ophthalmic solutions are toxic to the corneal epithelium when used with 1 of 2 dosing regimens in healthy human eyes."( Effect of gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions on human corneal epithelium following 2 dosing regimens.
Maclellan, D; Price, FW; Price, MO, 2005
)
0.61
"5% did not result in clinically significant epithelial toxicity in healthy human corneas after dosing regimens of 4 times a day for 7 days or hourly for 10 hours dosing regimens."( Effect of gatifloxacin 0.3% and moxifloxacin 0.5% ophthalmic solutions on human corneal epithelium following 2 dosing regimens.
Maclellan, D; Price, FW; Price, MO, 2005
)
0.61
" Of note, the unmodified pharmacokinetic behaviour with no need for age-related dosage adjustments combined with the once-daily administration favouring compliance and the low potential for drug-drug pharmacokinetic interactions in case of polytherapy, make moxifloxacin particularly attractive in the treatment of elderly subpopulations at a very high risk of AECB."( Pharmacokinetic and pharmacodynamic aspects of oral moxifloxacin 400 mg/day in elderly patients with acute exacerbation of chronic bronchitis.
Dolcet, F; Furlanut, M; Lugatti, E; Pavan, F; Pea, F; Screm, MC; Talmassons, G, 2006
)
0.76
"3% solution in the aqueous humor (AH) in humans after topical application with published levels of other available fluoroquinolones under similar dosing conditions."( Fourth-generation fluoroquinolone penetration into the aqueous humor in humans.
Aronowicz, JD; Caudle, D; McCulley, JP; Shine, WE, 2006
)
0.33
" This regimen simulated a realistic postoperative dosing schedule."( Fourth-generation fluoroquinolone penetration into the aqueous humor in humans.
Aronowicz, JD; Caudle, D; McCulley, JP; Shine, WE, 2006
)
0.33
"Aqueous humor antibiotic concentrations achieved at the time of cataract surgery after topical application can serve as an effective surrogate for what can be achieved with typical postoperative topical dosing (e."( Fourth-generation fluoroquinolone penetration into the aqueous humor in humans.
Aronowicz, JD; Caudle, D; McCulley, JP; Shine, WE, 2006
)
0.33
" Dosing frequency had little effect on 2-mo culture status or tolerability of therapy."( Moxifloxacin versus ethambutol in the first 2 months of treatment for pulmonary tuberculosis.
Burman, WJ; Chaisson, RE; Choudhri, S; Daley, CL; Engle, M; Goldberg, S; Johnson, JL; Mosher, AW; Munsiff, SS; Muzanye, G; Vernon, A; Zhao, Z, 2006
)
1.78
"Once daily IV/PO moxifloxacin monotherapy was as least as effective as standard IV piperacillin-tazobactam/PO amoxicillin-clavulanate dosed multiple times daily for the treatment of cIAIs."( Randomized controlled trial of moxifloxacin compared with piperacillin-tazobactam and amoxicillin-clavulanate for the treatment of complicated intra-abdominal infections.
Choudhri, S; Herrington, J; Malangoni, MA; Pertel, P; Song, J, 2006
)
0.96
" Moxifloxacin causes no significant epithelial or endothelial toxicity, and has no effect on visual acuity or ocular surface integrity in healthy subjects treated using a dosing regimen that simulated prophylactic use following cataract surgery."( The effect of moxifloxacin on the normal human cornea.
Alfonso, EC; Donaldson, KE; Marangon, FB; Schatz, L; Venkatraman, AS, 2006
)
1.6
" The value of dosing of antimicrobial agents based on MPC thresholds results in a rapid reduction in viable cells--even at higher inocula which are more reflective of organism burden in pneumonia."( Application of two methods to determine killing of Streptococcus pneumoniae by various fluoroquinolones.
Blondeau, JM; Blondeau, LD; Borsos, S; Hesje, C, 2006
)
0.33
" The semimechanistic model that was developed might, after further refinement, serve as a tool for the development of optimal dosing strategies for antibacterial agents."( Semimechanistic pharmacokinetic/pharmacodynamic model for assessment of activity of antibacterial agents from time-kill curve experiments.
Cars, O; Karlsson, MO; Löwdin, E; Nielsen, EI; Sandström, M; Viberg, A, 2007
)
0.34
"Both cases presented here describe corneal ulcers that persisted and showed signs of worsening during weeks of frequent topical dosing with moxifloxacin."( Severe corneal toxicity after topical fluoroquinolone therapy: report of two cases.
Tyler, ME; Walter, K, 2006
)
0.54
" The proposed methods were also applied for the determination of the investigated drugs in their pharmaceutical dosage forms and their validity was assessed using the standard addition technique with mean percentage recovery ranging from 100."( Stability indicating methods for the determination of some fluoroquinolones in the presence of their decarboxylated degrades.
Abd-El-Fattah, Lel-S; El-Guindi, NM; Mikael, HK; Salem, MY, 2006
)
0.33
" The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation <2%), while being simple, cheap and less time consuming and hence can be suitably applied for the estimation of moxifloxacin in different dosage forms and dissolution studies."( Validated spectrophotometric methods for the estimation of moxifloxacin in bulk and pharmaceutical formulations.
Ahmad, FJ; Chopra, S; Khar, RK; Motwani, SK, 2007
)
0.77
" Pharmacokinetic indices (C(max)/MIC90) for topical dosing were all <1."( In vitro efficacy and pharmacodynamic indices for antibiotics against coagulase-negative staphylococcus endophthalmitis isolates.
Flynn, HW; Harper, T; Miller, D, 2007
)
0.34
"Plasma, dialysate and urine pharmacokinetic parameters for moxifloxacin and its main metabolites were calculated after single and multiple (7 days) dosing with 400 mg day(-1)."( The influence of continuous venovenous haemodialysis on the pharmacokinetics of multiple oral moxifloxacin administration to patients with severe renal dysfunction.
Bührmann, S; Kribben, A; Kubitza, D; Mitchell, A; Möller, JG; Schäfers, RF; Stass, H; Wenzel, RR, 2007
)
0.8
" According to these findings, anuric critically ill patients who are undergoing EDD should be treated with the standard dosage of moxifloxacin (400 mg/d intravenously)."( Pharmacokinetics of moxifloxacin and levofloxacin in intensive care unit patients who have acute renal failure and undergo extended daily dialysis.
Czock, D; de Groot, K; Fliser, D; Hafer, C; Haller, H; Hüsig-Linde, C; Keller, F; Kielstein, JT; Kuse, E; Langhoff, A; Schöpke, T; Swoboda, S, 2006
)
0.86
"The present study was planned to investigate the plasma disposition kinetics and the pattern of moxifloxacin elimination in the milk of lactating ewes (n=6) following a single intravenous (IV) bolus or intramuscular (IM) injections at a dosage of 5 mg/kg in all animals."( Disposition kinetics of moxifloxacin in lactating ewes.
Goudah, A, 2008
)
0.87
" Rabbits were subsequently dosed with 1 drop, 3 times per day for 4 days with either moxifloxacin, gatifloxacin, or a commercially available irrigating solution."( Corneal wound healing in New Zealand White Rabbits following anterior keratectomy and treatment with moxifloxacin ophthalmic solution 0.5% or gatifloxacin ophthalmic solution 0.3%.
Hiddemen, JW; McCartney, MD; Rice, RL; Shepard, AR; Wax, MB; Williams, KK, 2007
)
0.78
"To evaluate the ocular surface and aqueous antimicrobial effects of gatifloxacin and moxifloxacin administered in two dosing regimens to patients undergoing phacoemulsification."( Antimicrobial efficacy of prophylactic gatifloxacin 0.3% and moxifloxacin 0.5% in patients undergoing phacoemulsification surgery.
Amico, LM; Bucci, FA; Evans, RE, 2008
)
0.81
"8 years) undergoing elective pars plana vitrectomy were assigned to a dosing group: control (n = 3), which received no medication; single-dose (n = 11), which received one 400 mg oral dose of moxifloxacin 3 hours before surgery; and five-dose (n = 10), which received one 400 mg dose on each of the 4 days preceding surgery and a fifth dose 3 hours before surgery."( Vitreal penetration of oral moxifloxacin in humans.
Fuller, JJ; Hancock, HA; Lott, MN; Marcus, DM; McGwin, G; Singh, H; Singh, J, 2008
)
0.83
"To evaluate the effect of 2 etravirine dosing regimens on QT/corrected QT interval (QTc) in HIV-negative volunteers and assess pharmacokinetic and additional safety parameters."( Etravirine has no effect on QT and corrected QT interval in HIV-negative volunteers.
De Smedt, G; Hoetelmans, RM; Janssen, K; Kakuda, TN; Lachaert, R; Peeters, M; Schöller-Gyüre, M; Woodfall, B, 2008
)
0.35
" Short-term dosing of etravirine in HIV-negative volunteers was generally safe and well tolerated."( Etravirine has no effect on QT and corrected QT interval in HIV-negative volunteers.
De Smedt, G; Hoetelmans, RM; Janssen, K; Kakuda, TN; Lachaert, R; Peeters, M; Schöller-Gyüre, M; Woodfall, B, 2008
)
0.35
" Placebo-adjusted mean changes from baseline in QTcF (Fridericia corrected), QTcI (individualized correction), PR, and QRS intervals were compared at each time point (time-matched analysis) and for values averaged across the dosing period (baseline-averaged analysis)."( Effects of aliskiren, a direct Renin inhibitor, on cardiac repolarization and conduction in healthy subjects.
Ayalasomayajula, S; Bedigian, MP; Dieterich, HA; Dole, WP; Flannery, B; Howard, D; Vaidyanathan, S; Yeh, CM, 2008
)
0.35
" In dose-response studies (0."( Cooperation between prokaryotic (Lde) and eukaryotic (MRP) efflux transporters in J774 macrophages infected with Listeria monocytogenes: studies with ciprofloxacin and moxifloxacin.
Courvalin, P; Lismond, A; Mingeot-Leclercq, MP; Tulkens, PM; Van Bambeke, F, 2008
)
0.54
"Both dosing regimens produced substantially higher aqueous concentrations than the known minimum inhibitory concentration for Staphylococcus epidermidis."( Comparison of 2 moxifloxacin regimens for preoperative prophylaxis: prospective randomized triple-masked trial. Part 1: aqueous concentration of moxifloxacin.
Gajjar, D; Raj, SM; Vasavada, AR; Vasavada, V, 2008
)
0.69
"5% administered three times daily is safe and cures bacterial conjunctivitis more effectively and significantly faster than polymyxin/trimethoprim dosed four times daily."( A multicenter comparison of polymyxin B sulfate/trimethoprim ophthalmic solution and moxifloxacin in the speed of clinical efficacy for the treatment of bacterial conjunctivitis.
Cockrum, P; Dorfman, M; Granet, DB; Stroman, D,
)
0.36
" Drug concentration analysis at various time points following instillation allows interpretation of the residence time and a rationale for dosing frequency."( Conjunctival tissue pharmacokinetic properties of topical azithromycin 1% and moxifloxacin 0.5% ophthalmic solutions: a single-dose, randomized, open-label, active-controlled trial in healthy adult volunteers.
O'Brien, TP; Torkildsen, G, 2008
)
0.57
" After oral dosing of moxifloxacin, a substantial, dose-dependent increase in the QT-interval duration could be shown, as anticipated for this agent."( Validation of the normal, freely moving Göttingen minipig for pharmacological safety testing.
Guth, B; Klumpp, A; Markert, M; Mayer, K; Schuler-Metz, A; Schumacher, K; Stubhan, M; Trautmann, T,
)
0.45
" Concentrations of all agents are predicted to exceed the MPC for ATCC 49226 for the entire dosage interval, while concentrations of moxifloxacin alone will exceed the MPC for m-49226."( Evaluation of the mutant selection window for fluoroquinolones against Neisseria gonorrhoeae.
Allen, GP; Hankins, CD, 2009
)
0.56
" coli (ATCC 25922, MG1655 and EC28044) were studied by exposing approximately 2 x 10(8) cfu/mL (20 mL) to escalating dosing regimens of moxifloxacin (ranging from 30 to 400 mg, once daily)."( Pharmacodynamics of moxifloxacin against a high inoculum of Escherichia coli in an in vitro infection model.
Chang, KT; Hou, JG; Ledesma, KR; Prince, RA; Singh, R; Tam, VH, 2009
)
0.88
" Electrocardiograms were recorded periodically over 24 hours at the end of placebo and highest dosing periods."( Absence of QTc prolongation in a thorough QT study with subcutaneous liraglutide, a once-daily human GLP-1 analog for treatment of type 2 diabetes.
Chatterjee, DJ; Khutoryansky, N; Litwin, JS; Sprenger, CR; Zdravkovic, M, 2009
)
0.35
" Once-daily dosing and proven efficacy suggest that moxifloxacin may be of value in acute, uncomplicated PID."( A randomized double-blind comparison of moxifloxacin and doxycycline/metronidazole/ciprofloxacin in the treatment of acute, uncomplicated pelvic inflammatory disease.
Heystek, M; Ross, JD, 2009
)
0.87
" The optimal dosage and duration have not been assessed."( Efficacy of four different moxifloxacin-based triple therapies for first-line H. pylori treatment.
Amitrano, M; Grossi, L; Manzoli, L; Marzio, L; Sacco, F; Spezzaferro, M, 2010
)
0.66
"1%) rates on day 5 +/- 1 of treatment (coprimary endpoints) in a randomized, double-blind, multicentre trial; both drugs were administered at a dosage of one drop in the affected eye(s) three times daily for 5 days."( Besifloxacin ophthalmic suspension 0.6%.
Carter, NJ; Scott, LJ, 2010
)
0.36
" The patients were given ciclosporin (Sandimmun Optoral) capsules twice daily (total daily dosage 150-380 mg/day) throughout the study period."( Moxifloxacin does not alter ciclosporin pharmacokinetics in transplant patients: a multiple-dose, uncontrolled, single-centre study.
Bauer, S; Delesen, H; Kubitza, D; Mai, I; Roots, I; Stass, H, 2010
)
1.8
" The once-daily dosing of moxifloxacin monotherapy may be a useful alternative for beta-lactam-based standard therapy."( Moxifloxacin monotherapy versus beta-lactam-based standard therapy for community-acquired pneumonia: a meta-analysis of randomised controlled trials.
An, MM; Cao, YB; Gao, PH; Jiang, YY; Shen, H; Zou, Z, 2010
)
2.1
"To determine the aqueous humor concentrations of moxifloxacin and besifloxacin after routine preoperative topical dosing in patients having cataract surgery."( Aqueous penetration of moxifloxacin 0.5% ophthalmic solution and besifloxacin 0.6% ophthalmic suspension in cataract surgery patients.
Kim, A; Pratzer, KA; Stark, WJ; Yoshida, J, 2010
)
0.93
" Likewise, no safety/tolerability concerns were observed after either supratherapeutic or 20-mg dosing to either population."( Evaluation of the effects of AZD3480 on cardiac repolarization: a thorough QT/QTc study using moxifloxacin as a positive control.
Alverlind, S; Dalén, P; Hårdemark, HG; Jostell, KG; Vik, T, 2010
)
0.58
"5% throughout the 7-day dosing period and for at least 7 days thereafter."( Pharmacokinetics of azithromycin and moxifloxacin in human conjunctiva and aqueous humor during and after the approved dosing regimens.
Brubaker, K; Crean, CS; Haque, RM; Hwang, DG; Stewart, WC; Zink, RC, 2010
)
0.63
"Azithromycin 1% demonstrated high, therapeutic levels in the conjunctiva that were maintained up to 7 days after completion of a 1-week dosing regimen."( Pharmacokinetics of azithromycin and moxifloxacin in human conjunctiva and aqueous humor during and after the approved dosing regimens.
Brubaker, K; Crean, CS; Haque, RM; Hwang, DG; Stewart, WC; Zink, RC, 2010
)
0.63
"3% eye drops administered in two different dosing regimens during phacoemulsification surgery."( Aqueous humour penetration of moxifloxocin and gatifloxacin eye drops in different dosing regimens before phacoemulsification surgery.
Akova, YA; Babaoğlu, MÖ; Bozkurt, A; Çetinkaya, A; Çolak, M; Güngör, SG; Yasar, Ü, 2011
)
0.37
" The penetration of both antibiotics increased significantly when the dosage of the agent was doubled."( Aqueous humour penetration of moxifloxocin and gatifloxacin eye drops in different dosing regimens before phacoemulsification surgery.
Akova, YA; Babaoğlu, MÖ; Bozkurt, A; Çetinkaya, A; Çolak, M; Güngör, SG; Yasar, Ü, 2011
)
0.37
" We had previously developed a mathematical modelling framework to describe the dynamics of bacterial populations under the effect of antimicrobials, which could facilitate the design of optimal dosing regimens."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
" Based on the best-fit model parameters, the likelihood of resistance development associated with various dosing regimens was predicted."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
"Bacterial regrowth and resistance development were observed with suboptimal dosing regimens."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
"Our model was found to be reasonable in characterizing biphasic killing of fluoroquinolones and predicting dosing regimens to suppress resistance development."( Modelling biphasic killing of fluoroquinolones: guiding optimal dosing regimen design.
Bhagunde, P; Chang, KT; Ledesma, KR; Nikolaou, M; Singh, R; Tam, VH, 2011
)
0.37
"An 89-year-old man receiving long-term anticoagulation with warfarin sodium (total weekly dosage of 19 mg) arrived at the anticoagulation clinic for his monthly visit."( Moxifloxacin-acetaminophen-warfarin interaction during bacille Calmette-Guerin treatment for bladder cancer.
Berube, C; Lee, R; Wen, A, 2011
)
1.81
" Use of pharmacodynamic/pharmacokinetic models has resulted in design of new doses and dosing schedules for disseminated MAC, as well as new susceptibility breakpoints for ethambutol and moxifloxacin."( Pharmacokinetic/pharmacodynamic-based treatment of disseminated Mycobacterium avium.
Deshpande, D; Gumbo, T, 2011
)
0.56
" MOXI-AF or its vehicle was dosed one drop twice-daily for 3 days."( Microbiological efficacy of a new ophthalmic formulation of moxifloxacin dosed twice-daily for bacterial conjunctivitis.
Bartell, J; Cupp, G; Garber, R; Stroman, D; Tauber, S; Vohra, F, 2011
)
0.61
"5% moxifloxacin ophthalmic formulation, MOXI-AF, provides effective eradication of the three principle causative pathogens of bacterial conjunctivitis across all age groups when dosed twice-daily for 3 days."( Microbiological efficacy of a new ophthalmic formulation of moxifloxacin dosed twice-daily for bacterial conjunctivitis.
Bartell, J; Cupp, G; Garber, R; Stroman, D; Tauber, S; Vohra, F, 2011
)
1.23
"5, 1 (end of infusion), 2, 4, 8, 12, and 24 h after intravenous dosing of linezolid 600 and 1,200 mg."( Lack of an effect of standard and supratherapeutic doses of linezolid on QTc interval prolongation.
Alvey, C; Choo, HW; Cuozzo, C; Damle, B; Kirby, D; Labadie, RR; Riley, S, 2011
)
0.37
" The selection and magnitude of the PK/PD index were, however, shown to be sensitive to differences in PK in subpopulations, uncertainty in MICs, and investigated dosing intervals."( Pharmacokinetic/pharmacodynamic (PK/PD) indices of antibiotics predicted by a semimechanistic PKPD model: a step toward model-based dose optimization.
Cars, O; Friberg, LE; Nielsen, EI, 2011
)
0.37
" Serial venous blood samples were drawn up to 72 h after dosing and moxifloxacin plasma levels were measured by a validated HPLC method with fluorescence detection."( Oral bioavailability of moxifloxacin after Roux-en-Y gastric bypass surgery.
Batens, H; Blot, S; Boussery, K; Colin, P; De Paepe, P; De Smet, J; Ruige, J; Van Bocxlaer, J; Van Bortel, LM; Van Nieuwenhove, Y; Vogelaers, D, 2012
)
0.92
"4 mg · h/L after oral dosing and 52."( Oral bioavailability of moxifloxacin after Roux-en-Y gastric bypass surgery.
Batens, H; Blot, S; Boussery, K; Colin, P; De Paepe, P; De Smet, J; Ruige, J; Van Bocxlaer, J; Van Bortel, LM; Van Nieuwenhove, Y; Vogelaers, D, 2012
)
0.69
" The dose of moxifloxacin was 400 mg daily in all studies, but dosing frequency differed from 3 to 7 days per week."( Moxifloxacin as an alternative or additive therapy for treatment of pulmonary tuberculosis.
Fouad, M; Gallagher, JC, 2011
)
2.18
" Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms."( Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.
Deshmukh, RV; Gaikwad, KR; Manvi, FV; Nanjwade, BK; Parikh, KA, 2012
)
0.63
" Regarding antibiotic susceptibilities: (i) amoxicillin is still useful for empirical therapy but with a high daily dose; (ii) cefuroxime axetil and macrolides (but not telithromycin) are inappropriate for empirical therapy; and (iii) moxifloxacin and levofloxacin are the next 'best empirical choice' (no resistant isolates) but levofloxacin will require 500 mg twice-daily dosing for effective coverage."( Antimicrobial susceptibility of Streptococcus pneumoniae isolates from vaccinated and non-vaccinated patients with a clinically confirmed diagnosis of community-acquired pneumonia in Belgium.
Carbonnelle, S; De Bel, A; Dediste, A; Glupczynski, Y; Huang, TD; Jacobs, F; Jordens, P; Lismond, A; Schatt, P; Tulkens, PM; Van Bambeke, F; Verhaegen, J; Verschuren, F, 2012
)
0.56
" Its primary objective was to compare supratherapeutic repeated dosing of strontium ranelate (4 g day⁻¹ for 15 days) with placebo on the largest time-matched mean QT(c) variation, from baseline to under treatment values, in healthy subjects."( Repeated supratherapeutic dosing of strontium ranelate over 15 days does not prolong QT(c) interval in healthy volunteers.
Arezina, R; Camm, AJ; Lorch, U; Naseem, A; Taubel, J; Wang, D, 2012
)
0.38
"5 years) were included to receive 1 day of placebo followed by 15 days of supratherapeutic repeated dosing of strontium ranelate (4 g day⁻¹), in a 4 month, randomized, placebo (16 days) and positive-controlled (single dose of moxifloxacin 400 mg preceded by 15 days of placebo), double-blind, double dummy, crossover design."( Repeated supratherapeutic dosing of strontium ranelate over 15 days does not prolong QT(c) interval in healthy volunteers.
Arezina, R; Camm, AJ; Lorch, U; Naseem, A; Taubel, J; Wang, D, 2012
)
0.56
"The safety of moxifloxacin is essentially comparable to that of standard therapies for patients receiving the currently registered dosage and for whom contraindications and precautions of use (as in the product label) are taken into account."( Moxifloxacin safety: an analysis of 14 years of clinical data.
Arvis, P; Kruesmann, F; Tulkens, PM, 2012
)
2.18
" Ten second electrocardiograms were obtained for time-matched baseline on days -2 and -1, three time points after dosing on day 1 for moxifloxacin and five time points on day 7 for atomoxetine and placebo."( Effects of atomoxetine on the QT interval in healthy CYP2D6 poor metabolizers.
Allen, AJ; April, J; Beasley, CM; Haber, H; Jin, L; Kauffman, L; Kothare, PA; Loghin, C; Mitchell, MI, 2013
)
0.59
" Triplicate ECGs were performed continuously at baseline (day 0), before dosing, and over 24 hours after dosing in each treatment period."( Effects of a supratherapeutic dose of investigational orally inhaled dihydroergotamine (MAP0004) on QT interval: a randomized, double-blind, active- and placebo-controlled crossover study in healthy volunteers.
Haugen, G; Kellerman, DJ; Kori, S; Voloshko, P, 2012
)
0.38
"Multiple dosing with bitopertin 30 mg or 175 mg did not affect QTcF in these healthy male volunteers."( Evaluation of the effects of bitopertin (RG1678) on cardiac repolarization: a thorough corrected QT study in healthy male volunteers.
Banken, L; Hahn, M; Hofmann, C; Martin-Facklam, M; Nagel, S; Swearingen, D, 2012
)
0.38
"There was no effect of vismodegib on the QTc interval when dosed daily at 150 mg to steady state."( Daily dosing of vismodegib to steady state does not prolong the QTc interval in healthy volunteers.
Ayache, JA; Chang, I; Dresser, MJ; Dufek, MB; Ezzet, F; Graham, RA; Jin, JY; Low, JA; Wang, B; Zerivitz, K, 2013
)
0.39
" Physicians complied with the recommended 400 mg once-daily dose in a large proportion of patients, confirming the advantages of this simple dosing regimen."( Efficacy and safety of moxifloxacin in acute exacerbations of chronic bronchitis: a prospective, multicenter, observational study (AVANTI).
Chuchalin, A; Dokic, D; Marschall, HP; Petri, T; Tokić, M; Zakharova, M, 2013
)
0.7
"5 h after intravenous dosing with a supratherapeutic dose (1,500 mg) of ceftaroline fosamil, 400 mg moxifloxacin (positive control), and placebo."( Evaluation of the effect of a supratherapeutic dose of intravenous ceftaroline fosamil on the corrected QT interval.
Llorens, L; Rank, D; Rekeda, L; Riccobene, TA, 2013
)
0.61
"Levofloxacin dosing regimens with low AUC/MIC ratios select for efflux pump overexpression, leading to fluoroquinolone resistance."( Comparative antibacterial effects of moxifloxacin and levofloxacin on Streptococcus pneumoniae strains with defined mechanisms of resistance: impact of bacterial inoculum.
Bowker, KE; Garvey, MI; Macgowan, AP; Noel, AR; Tomaselli, SG, 2013
)
0.66
" The standard dosing provides sufficient drug exposure for treatment of CAP but for HAP it does so only when a highly susceptible pathogen is present."( Population pharmacokinetics and pharmacodynamic evaluation of intravenous and enteral moxifloxacin in surgical intensive care unit patients.
Haeberle, HA; Heininger, A; Kees, F; Kees, MG; Kloft, C; Schaeftlein, A, 2013
)
0.61
" The typical moxifloxacin PK profile is also altered by food prior to dosing reducing the Cmax and delays the peak effects on QTc up to several hours thereby reducing the overall magnitude of the effect and delaying the peak QTc prolongation."( Thorough QT study of the effect of oral moxifloxacin on QTc interval in the fed and fasted state in healthy Japanese and Caucasian subjects.
Batchvarov, V; Camm, AJ; Ferber, G; Lorch, U; Savelieva, I; Taubel, J, 2014
)
1.04
" The methods were validated in terms of accuracy and precision and were successfully applied to the determination of MOX in its pharmaceutical dosage form."( New spectrophotometric methods for the determination of moxifloxacin in pharmaceutical formulations.
Aboul-Enein, HY; Ebraheem, SA; Elbashir, AA; Elwagee, AH, 2013
)
0.64
"The goal of this study was to assess the effect on cardiac repolarization (QTc interval) of repeated oral dosing of ipragliflozin at therapeutic (100 mg/d) and supratherapeutic (600 mg/d) levels in healthy subjects."( Ipragliflozin does not prolong QTc interval in healthy male and female subjects: a phase I study.
Abeyratne, A; Dietz, A; Kadokura, T; Keirns, J; Krauwinkel, W; Smulders, R; Zhang, W, 2013
)
0.39
" Study treatments were administered orally for 3 days in five separate periods in which subjects were dosed with (1) a single dose of 75 mg lomitapide on Day 1 followed by a single dose of 200 mg on Day 3; (2) ketoconazole 200 mg BID; (3) ketoconazole with a single dose of 75 mg lomitapide on Day 3; (4) a single dose of 400 mg moxifloxacin on Day 3 and (5) placebo."( Lomitapide at supratherapeutic plasma levels does not prolong the Qtc interval--results from a TQT study with moxifloxacin and ketoconazole.
Darpo, B; Ferber, G; Sager, P; Sumeray, M; Zhou, M, 2013
)
0.77
" Digital 12-lead ECGs were recorded at baseline and at 10 time points over 24 hours after dosing in each treatment period."( Evaluation of the effect of Naloxegol on cardiac repolarization: a randomized, placebo- and positive-controlled crossover thorough QT/QTc study in healthy volunteers.
Carlson, G; Gottfridsson, C; Lappalainen, J; Sostek, M, 2013
)
0.39
" Similar findings were observed using QTcB; the upper limits of the 2-sided 90% CI were <10 msec at all time points after dosing with naloxegol 25 or 150 mg."( Evaluation of the effect of Naloxegol on cardiac repolarization: a randomized, placebo- and positive-controlled crossover thorough QT/QTc study in healthy volunteers.
Carlson, G; Gottfridsson, C; Lappalainen, J; Sostek, M, 2013
)
0.39
" The primary end point was the comparison of evacetrapib effect on the population-corrected QT interval (QTcP) to that of placebo at 7 time points following dosing on day 10."( Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants.
Friedrich, S; Krueger, KA; Suico, JG; Zhang, W, 2014
)
0.4
" A 1200-mg supratherapeutic dose of evacetrapib was considered to be well tolerated after 10 days of daily dosing in healthy participants."( Evacetrapib at a supratherapeutic steady state concentration does not prolong QT in a thorough QT/QTc study in healthy participants.
Friedrich, S; Krueger, KA; Suico, JG; Zhang, W, 2014
)
0.4
"Given the ever increasing number of obese patients and obesity related bypass surgery, dosing recommendations in the post-bypass population are needed."( Moxifloxacin dosing in post-bariatric surgery patients.
Bortel, LM; Boussery, K; Colin, P; De Waele, J; Eleveld, DJ; Ruige, J; Struys, MM; T'Jollyn, H; Van Bocxlaer, J, 2014
)
1.85
"25 mg l(-1) , standard moxifloxacin dosing does not attain adequate levels in this population."( Moxifloxacin dosing in post-bariatric surgery patients.
Bortel, LM; Boussery, K; Colin, P; De Waele, J; Eleveld, DJ; Ruige, J; Struys, MM; T'Jollyn, H; Van Bocxlaer, J, 2014
)
2.16
"Throughout our PK-PD simulation study, it became apparent that, whenever optimal bacterial resistance suppression is deemed necessary, the standard moxifloxacin dosing will not be sufficient."( Moxifloxacin dosing in post-bariatric surgery patients.
Bortel, LM; Boussery, K; Colin, P; De Waele, J; Eleveld, DJ; Ruige, J; Struys, MM; T'Jollyn, H; Van Bocxlaer, J, 2014
)
2.04
" The frequency of preoperative and/or postoperative dosing was generally lower for besifloxacin than that for moxifloxacin."( Safety of besifloxacin ophthalmic suspension 0.6% in cataract and LASIK surgery patients.
Clinch, TE; Majmudar, PA, 2014
)
0.61
" In non-adherent dosing scenarios, LFX 500 mg q24 h was not able to reach the PK/PD index guaranteeing clinical efficacy."( Impact of poor compliance with levofloxacin and moxifloxacin on respiratory tract infection antimicrobial efficacy: a pharmacokinetic/pharmacodynamic simulation study.
Carral, N; Lukas, JC; Oteo, I; Suarez, E, 2015
)
0.67
" It highlights available intracameral antibiotics with respect to pharmacology, spectrum of activity, dosage and preparation, safety, and efficacy profiles, as well as toxic anterior segment syndrome risks to better define the potential use of these medications in the prevention of endophthalmitis."( Intracameral antibiotics: Safety, efficacy, and preparation.
Braga-Mele, R; Chang, DF; Henderson, BA; Mamalis, N; Talley-Rostov, A; Vasavada, A, 2014
)
0.4
" The two treatment groups consisted of SRP combined with systemically administered MOX at the dosage of 400 mg once daily for 7 days or SRP + placebo once daily for 7 days."( Adjunctive moxifloxacin in the treatment of generalized aggressive periodontitis patients: clinical and microbiological results of a randomized, triple-blind and placebo-controlled clinical trial.
Ardila, CM; Ariza-Garcés, AA; Boderth-Acosta, G; Guzmán, IC; Martelo-Cadavid, JF, 2015
)
0.81
" The proposed method has been applied successfully for the estimation of moxifloxacin hydrochloride in tablet dosage form with no interference from the excipients."( Development and validation of sensitive kinetic spectrophotometric method for the determination of moxifloxacin antibiotic in pure and commercial tablets.
Ashour, S; Bayram, R, 2015
)
0.87
" Modeling demonstrated that the discrepant results may have been due to a baseline shift after repeat dosing and baseline differences between the treatments."( Utility of concentration-effect modeling and simulation in a thorough QT study of losmapimod.
Arya, N; Barbour, AM; Fossler, MJ; Glaser, R; Magee, M; Patel, BR; Shaddinger, B; Tao, W; Tombs, L, 2015
)
0.42
" The effect of moxifloxacin on QT interval prolongation was well explained by the nonlinear dose-response (Emax) model, and the effect by 800 mg was only slightly greater than that of 400 mg."( Pharmacokinetic-pharmacodynamic analysis to evaluate the effect of moxifloxacin on QT interval prolongation in healthy Korean male subjects.
Chung, JY; Han, S; Hong, T; Jeon, S; Lee, J; Lim, KS; Park, GJ; Park, WS; Yim, DS; Yu, KS, 2015
)
1.01
"5, 3, 4, 5, 6, 12, 18, and 24 h after dosing with delafloxacin at 300 mg intravenously (i."( A thorough QT study to evaluate the effects of therapeutic and supratherapeutic doses of delafloxacin on cardiac repolarization.
Benedict, MS; Cammarata, SK; Lawrence, LE; Litwin, JS; Sun, E; Thorn, MD, 2015
)
0.42
" Each dose was administered on a separate dosing day."( Effects of group housing on ECG assessment in conscious cynomolgus monkeys.
Adkins, D; Hu, M; Lu, J; Oldman, K; Platz, S; Ren, J; Schofield, J; Skinner, M; Wang, S; Xing, G; Yu, H; Zhao, L; Zheng, W,
)
0.13
"Therapeutic drug monitoring (TDM) of second-line antituberculosis drugs would allow for optimal individualized dosage adjustments and improve drug safety and therapeutic outcomes."( Pharmacokinetics of Second-Line Antituberculosis Drugs after Multiple Administrations in Healthy Volunteers.
Chung, JY; Jang, IJ; Jang, K; Lee, JH; Moon, SJ; Oh, J; Park, JS; Park, SI; Song, J; Yoon, J; Yu, KS, 2015
)
0.42
" The once-daily dosing of moxifloxacin monotherapy may be a useful alternative for other recommended antibiotic therapy."( A Meta-analysis of Sequential Intravenous/Oral Moxifloxacin Monotherapy for Treatment of Skin and Skin Structure Infections.
Chu, Y; Jiang, MY; Luo, YF; Qu, J; Qu, LY, 2015
)
0.97
" The results of these studies suggest the continued effectiveness of the dosage of 400 mg a short course (7 days) over 15 years of practical use of the drug, which in its clinical efficacy is superior to amoxicillin/clavulanate, cefuroxime axetil and levofloxacin."( [15-year experience of moxifloxacin in the treatment of patients with bacterial rhinosinusitis].
Edzhe, MA; Hon, EM; Korostelev, SA; Miroshnichenko, NA; Ovchinnikov, AY, 2015
)
0.72
" ECG data were extracted from a continuous recording predose and serially after dosing on the treatment day."( Differentiating the Effect of an Opioid Agonist on Cardiac Repolarization From µ-Receptor-mediated, Indirect Effects on the QT Interval: A Randomized, 3-way Crossover Study in Healthy Subjects.
Bai, SA; Darpo, B; Ferber, G; Finn, A; Xiang, Q; Zhou, M, 2016
)
0.43
" In ECG evaluations performed after dosing with pomalidomide 4 mg (therapeutic dose) or 20 mg (supratherapeutic dose), the upper limit of the two-sided 90 % CI for mean change from baseline and placebo-corrected QTcF was <10 ms at all postdose time points, which is below the defined threshold of regulatory concern."( A Phase 1, double-blind, 4-period crossover study to investigate the effects of pomalidomide on QT interval in healthy male subjects.
Assaf, M; Liu, L; Mondal, SA; O'Mara, E, 2016
)
0.43
" These changes could enhance the drug efficacy, but they could also cause drug accumulation, which might induce adverse effect, so it was suggested that the drug dosage should be adjusted and the drug concentration in plasma should be monitored if moxifloxacin and rifampicin are co-administered."( Drug-drug interactions between moxifloxacin and rifampicin based on pharmacokinetics in vivo in rats.
Huang, L; Huang, Y; Liu, J; Shi, L; Xiao, H; Yu, X, 2016
)
0.9
" Electrocardiograms (ECGs) and pharmacokinetic samples were obtained on each dosing day; baseline ECGs were taken pre-dose."( Evaluation of the effect of ruxolitinib on cardiac repolarization: A thorough QT study.
Bowman, J; Chen, X; Punwani, N; Soloviev, M; Williams, W; Yeleswaram, S, 2014
)
0.4
" Median rifapentine area under the concentration-time curve (AUC0-24) was 313 mcg*h/mL, similar to recent studies of rifapentine dosed at 450-600 mg daily."( A Phase 2 Randomized Trial of a Rifapentine plus Moxifloxacin-Based Regimen for Treatment of Pulmonary Tuberculosis.
Armstrong, DT; Barnes, GL; Cavalcante, SC; Chaisson, RE; Cohn, S; Conde, MB; Dalcolmo, M; Dooley, KE; Dorman, SE; Duarte, RS; Durovni, B; Efron, A; Loredo, C; Marzinke, MA; Mello, FC; Moulton, LH; Rolla, V; Savic, RM, 2016
)
0.69
"Solithromycin, a novel macrolide antibiotic with both intravenous and oral formulations dosed once daily, has completed 2 global phase 3 trials for treatment of community-acquired bacterial pneumonia."( SOLITAIRE-IV: A Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of Intravenous-to-Oral Solithromycin to Intravenous-to-Oral Moxifloxacin for Treatment of Community-Acquired Bacterial Pneumonia.
Das, AF; Fernandes, P; File, TM; Gonong, JRV; Jamieson, BD; Keedy, K; Oldach, D; Rewerska, B; Sheets, A; Taylor, D; Vucinic-Mihailovic, V, 2016
)
0.63
" All patients received 400 mg intravenously on day 1 and were permitted to switch to oral dosing when clinically indicated."( SOLITAIRE-IV: A Randomized, Double-Blind, Multicenter Study Comparing the Efficacy and Safety of Intravenous-to-Oral Solithromycin to Intravenous-to-Oral Moxifloxacin for Treatment of Community-Acquired Bacterial Pneumonia.
Das, AF; Fernandes, P; File, TM; Gonong, JRV; Jamieson, BD; Keedy, K; Oldach, D; Rewerska, B; Sheets, A; Taylor, D; Vucinic-Mihailovic, V, 2016
)
0.63
" Surface modified NPs (MOX-PEG-WSC NPs) were prepared to provide controlled delivery and circulate in the bloodstream for an extended period of time, thus minimizing dosing frequency."( Effect of PEG and water-soluble chitosan coating on moxifloxacin-loaded PLGA long-circulating nanoparticles.
Devi, VK; Mustafa, S; Pai, RS, 2017
)
0.71
"To review current and past practices of intracameral antibiotic administration for infection prophylaxis in cataract surgery; to review the benefits and liabilities of available prophylactic drugs, dosage determination, and administration protocols; and to devise an optimum dose and administration protocol for intracameral moxifloxacin."( Dose and administration of intracameral moxifloxacin for prophylaxis of postoperative endophthalmitis.
Arshinoff, SA; Modabber, M, 2016
)
0.87
" Animals received either vehicle or vehicle followed by ascending doses of moxifloxacin each on a different dosing day."( Detecting drug-induced changes in ECG parameters using jacketed telemetry: Effect of different data reduction techniques.
Lu, J; Oldman, K; Ren, J; Skinner, M; Xing, G,
)
0.36
" There were fewer statistically significant differences between dosing days in animals given vehicle when the large duration averages and super-interval reduction techniques were used."( Detecting drug-induced changes in ECG parameters using jacketed telemetry: Effect of different data reduction techniques.
Lu, J; Oldman, K; Ren, J; Skinner, M; Xing, G,
)
0.13
" Use of larger duration averages or super-intervals may facilitate data interpretation by reducing the incidence of spurious significant differences that occur by chance between dosing days."( Detecting drug-induced changes in ECG parameters using jacketed telemetry: Effect of different data reduction techniques.
Lu, J; Oldman, K; Ren, J; Skinner, M; Xing, G,
)
0.13
" There were no serious side effects observed with the use of linezolid in reduced dosage of 600 mg×1/day for a duration of 9 months."( Mycobacterium chelonae hand infection after steroid injection in a patient with rheumatoid arthritis receiving long-term linezolid therapy.
Olesen, JS; Wang, M; Wejse, C, 2017
)
0.46
"Tedizolid is an orally bioavailable oxazolidinone with once-daily dosing and broad-spectrum Gram-positive activity."( Exploring the pharmacodynamic interactions between tedizolid and other orally bioavailable antimicrobials against Staphylococcus aureus and Staphylococcus epidermidis.
Werth, BJ, 2017
)
0.46
"We compared the pharmacokinetics of moxifloxacin during rifampicin co-treatment or when dosed alone in African patients with drug-susceptible recurrent TB."( Effect of rifampicin and efavirenz on moxifloxacin concentrations when co-administered in patients with drug-susceptible TB.
Adamson, J; Chirehwa, M; Denti, P; Essack, S; Govender, K; Kimba-Phongi, E; McIlleron, H; Naidoo, A; Naidoo, K; Padayatchi, N; Yende-Zuma, N, 2017
)
1
" Other options such as ertapenem and moxifloxacin may be reasonable where multiple daily dosing or intravenous administration is inappropriate."( Clinical efficacy of piperacillin/tazobactam in the treatment of complicated skin and soft tissue infections.
Hayashi, Y; Katayama, M; Suzuki, D; Takimoto, K; Wang, Q, 2017
)
0.73
" There was no significant difference in SLE history, Systemic Lupus Erythematosus Disease Activity Index-2000 (SLEDAI-2000), Systemic Lupus International Collaborating Clinics/American College of Rheumatology damage index (SLICC/ACR), hematologic examination results, and corticosteroid dosage between 2 groups."( Successful treatment using corticosteroid combined antibiotic for acute acalculous cholecystitis patients with systemic lupus erythematosus.
Chen, W; He, X; Hong, T; Li, B; Liu, W; Qu, Q, 2017
)
0.46
" Fixed drug combinations not only cut the cost but also the dosage and improve the compliance of patients in the immediate post operative period."( Safety of Fixed drug Combination in Post -Operative Cataract Patients, at Tertiary Care Centre - In South India.
Anuradha, A; Nishath, S; Rashmi, G; Shilpa, R; Vidyadevi, M, 2017
)
0.46
" Dosing errors led to the majority of toxicities with cefuroxime."( Comparative analysis of the safety and efficacy of intracameral cefuroxime, moxifloxacin and vancomycin at the end of cataract surgery: a meta-analysis.
Ambati, BK; Bardsley, T; Bondalapati, S; Bowen, RC; Evans, PR; Greene, T; Kliethermes, M; Lawyer, TW; Mamalis, CA; McFarland, M; Rudnisky, CJ; Shi, D; Snow, KB; Zhou, AX, 2018
)
0.71
" The developed sustained release in situ gel formulations could enhance patient's compliance by reducing the dosing frequency and also act as an alternative treatment to curb periodontitis."( Investigation on solution-to-gel characteristic of thermosensitive and mucoadhesive biopolymers for the development of moxifloxacin-loaded sustained release periodontal in situ gels.
Jnanendrappa, N; Meka, VS; Quah, SY; Sahu, PS; Sheshala, R; Tan, GC, 2019
)
0.72
" After oral dosing of moxifloxacin to the dogs, a substantial, dose-dependent increase in the QT-interval duration could be shown, as anticipated for this agent."( A new telemetry-based system for assessing cardiovascular function in group-housed large animals. Taking the 3Rs to a new level with the evaluation of remote measurement via cloud data transmission.
Cioaga, M; Guth, BD; Krause, F; Markert, M; Mouriot, S; Trautmann, T; Wetzel, M,
)
0.45
"A simplified dosing regimen was selected to follow the development of ophthalmic pazufloxacin based on its efficacy and safety profile."( Efficacy and Safety of 0.6% Pazufloxacin Ophthalmic Solution Versus Moxifloxacin 0.5% and Gatifloxacin 0.5% in Subjects with Bacterial Conjunctivitis: A Randomized Clinical Trial.
Baiza-Durán, L; Casillas-Magallanes, M; Gómez-Bastar, PA; González-Lomelí, M; Lizárraga-Corona, A; Mercado-Sesma, AR; Montoya-Sánchez, IM; Mora-González, A; Ochoa-Tabares, JC; Olvera-Montaño, O; Oregon-Miranda, AA; Orozco-Carroll, M; Páez-Garza, JH; Pérez-Balbuena, AL; Sandoval-Delgadillo, LI; Saucedo-Rodríguez, LR; Villanueva-Najera, MA, 2018
)
0.72
"There was a good correlation between QTcF and J-Tpeak_c prolongation after oral dosing of 400 mg moxifloxacin with placebo-adjusted, change-from-baseline (ΔΔ) J-Tpeak_c of ~12 ms at concentrations that caused ΔΔQTcF of ~20 ms."( Challenges in implementing and obtaining acceptance for J-Tpeak assessment as the clinical component of CiPA.
Couderc, JP; Darpo, B,
)
0.35
" Through Monte Carlo simulations the quantitative output of this in vitro study was bridged to the human patient population to inform optimal dosage regimens while accounting for clinical minimum inhibitory concentration (MIC) distributions."( Dose optimization of moxifloxacin and linezolid against tuberculosis using mathematical modeling and simulation.
Brown, DL; Derendorf, H; Drusano, GL; Heinrichs, MT; Louie, A; Maynard, MS; Peloquin, CA; Rand, KH; Sy, SKB, 2019
)
0.83
" However, based on their pharmacokinetics (PK) and pharmacodynamics (PD), these drugs are also promising for TB meningitis and might perhaps have the potential to shorten pulmonary TB treatment if dosing could be optimized."( The Role of Fluoroquinolones in the Treatment of Tuberculosis in 2019.
Alffenaar, JWC; Kosterink, JGW; Pranger, AD; van der Werf, TS, 2019
)
0.51
" A dosing strategy for each age cohort (Cohort 1: ≥6 years to ≤14 years; Cohort 2: ≥2 years to <6 years; Cohort 3: >3 month to <2 years) was developed using physiology-based pharmacokinetic modeling combined with a stepwise dosing scheme to obtain a similar exposure to adults receiving 400 mg of moxifloxacin."( Pharmacokinetics, Safety, and Tolerability of Single-Dose Intravenous Moxifloxacin in Pediatric Patients: Dose Optimization in a Phase 1 Study.
Arrieta, AC; Bradley, JS; James, LP; Lettieri, J; Stass, H; Sullivan, JE; Vanevski, KM; Willmann, S, 2019
)
0.92
" In study 1 (N = 12), the supratherapeutic dosing regimen achieved exposure ∼3."( Thorough QTc Evaluation and the Safety of Supratherapeutic Doses of Odanacatib in Healthy Subjects.
Brandquist, C; Chakravarthy, M; Gutierrez, M; Liu, C; Liu, F; Mahon, C; McCrea, J; Mostoller, K; Panebianco, D; Stoch, SA; Zajic, S, 2019
)
0.51
" The resulting model proposed an age-dependent dosing regimen that was tested in a phase I study."( Application of Physiologically-Based and Population Pharmacokinetic Modeling for Dose Finding and Confirmation During the Pediatric Development of Moxifloxacin.
Coboeken, K; Eissing, T; Frei, M; Lippert, J; Stass, H; Sutter, G; Wendl, T; Willmann, S, 2019
)
0.71
" We previously reported this variability in a study of four human ether-a-go-go-related gene (hERG) potassium channel-blocking drugs in which each subject underwent intensive pharmacokinetic and pharmacodynamic sampling such that subjects had 15 time-matched plasma drug concentration and electrocardiogram measurements throughout 24 hours after dosing in a phase I clinical research unit."( Clinical Trial in a Dish: Personalized Stem Cell-Derived Cardiomyocyte Assay Compared With Clinical Trial Results for Two QT-Prolonging Drugs.
Blinova, K; Daluwatte, C; Patel, D; Schocken, D; Strauss, DG; Vicente, J; Wu, JC, 2019
)
0.51
"To test the effect of injection volume and concentration on dosing and residence time of moxifloxacin in the anterior chamber (AC)."( Injection volume and intracameral moxifloxacin dose.
Gardner, S; Shorstein, NH, 2019
)
1.01
" The AC concentrations and elimination rates of the drug for two AC volumes were modeled for each dosing method."( Injection volume and intracameral moxifloxacin dose.
Gardner, S; Shorstein, NH, 2019
)
0.79
" The mathematical model predicted that variation in dosing in each group would result in differences of 12 minutes or less for the presence of the drug in the AC."( Injection volume and intracameral moxifloxacin dose.
Gardner, S; Shorstein, NH, 2019
)
0.79
" A 12-lead electrocardiogram was recorded in triplicate before dosing and at selected time points up to 72 hours after dosing."( A Thorough QT Study to Evaluate the Effects of a Supratherapeutic Dose of Sertraline on Cardiac Repolarization in Healthy Subjects.
Abbas, R; Bachinsky, M; Chappell, PB; Crownover, PH; Damle, B; LaBadie, RR; Riley, S, 2020
)
0.56
"The present investigation explores the development and characterization of moxifloxacin hydrochloride and ketorolac tromethamine combination loaded Eudragit RL 100 nanosuspension for ocular drug delivery in order to overcome the problems associated with conventional dosage forms."( Eudragit RL100 Based Moxifloxacin Hydrochloride and Ketorolac Tromethamine Combination Nanoparticulate System for Ocular Drug Delivery.
Pawar, P; Salvi, V, 2020
)
1.11
"In this monograph, literature data is reviewed to evaluate the feasibility of waiving in vivo bioequivalence testing and instead applying the Biopharmaceutics Classification System (BCS) based methods to the approval of immediate-release solid oral dosage forms containing moxifloxacin hydrochloride as the sole active pharmaceutical ingredient."( Biowaiver Monograph for Immediate-Release Solid Oral Dosage Forms: Moxifloxacin Hydrochloride.
Abdallah, DB; Abrahamsson, B; Charoo, NA; Cristofoletti, R; Dressman, J; Groot, DW; Langguth, P; Mehta, M; Parr, A; Parveen, T; Polli, JE; Shah, VP; Tajiri, T, 2020
)
0.97
" 12-Lead Holter ECGs were recorded from 1 h before dosing until at least 24 h after each dose."( Absence of QTc prolongation in a thorough QT study with imeglimin, a first in class oral agent for type 2 diabetes mellitus.
Bolze, S; Dubourg, J; Felices, M; Fouqueray, P; Perrimond-Dauchy, S; Voiriot, P, 2020
)
0.56
"The effect of AT on QT interval prolongation may not have been significant at the dosage of 400 mg."( Relationship between antofloxacin concentration and QT prolongation and estimation of the possible false-positive rate.
He, YC; Huang, JH; Li, LJ; Li, YF; Liang, LY; Wang, K; Xu, FY; Yang, J; Zheng, QS, 2020
)
0.56
" Although supratherapeutic exposure of pretomanid relative to the now-recommended dosing with food was not achieved, these findings contribute to the favorable assessment of cardiac safety for pretomanid."( Phase 1 Study of the Effects of the Tuberculosis Treatment Pretomanid, Alone and in Combination With Moxifloxacin, on the QTc Interval in Healthy Volunteers.
El-Amin, W; Everitt, D; Li, M; Makhene, MK; Nedelman, J; Osborn, B; Saviolakis, GA; Yang, TJ, 2021
)
0.84
"5% moxifloxacin eye drops alone, administered every 4 or 6 hours, achieve an AC concentration just above or at the mutant prevention concentration (MPC) for MSSA, respectively, whereas 8-hour dosing produces levels generally below the MPC."( Incremental effect of topical and oral moxifloxacin administration with surgical intracameral prophylaxis.
Arshinoff, SA; Hu, A; Lukewich, MK; Modabber, M, 2021
)
1.51
" The results indicate that MOX-HME inserts could potentially provide a once-a-day application, consequently reducing the dosing frequency and acting as an alternative delivery system in the management of bacterial infections."( Development and optimization of hot-melt extruded moxifloxacin hydrochloride inserts, for ocular applications, using the design of experiments.
Dudhipala, N; Komanduri, N; Majumdar, S; Repka, MA; Thakkar, R; Tripathi, S, 2021
)
0.87
"A reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed and validated for the identification and quantification of moxifloxacin hydrochloride-related substances in finished dosage forms."( A rapid RP-HPLC stability-indicating method development and validation of moxifloxacin hydrochloride-related substances in finished dosage forms.
Algete, P; Boodida, S; Vankalapati, KR, 2021
)
1.05
" The typical telemetry study involves a dose-response analysis of QTc intervals over time using a crossover (CO) design."( Evaluation of moxifloxacin in canine and non-human primate telemetry assays: Comparison of QTc interval prolongation by timepoint and concentration-QTc analysis.
Baublits, J; Chandra, FA; Chui, RW; Engwall, MJ; Jones, ZW; Vargas, HM, 2021
)
0.98
" We characterize moxifloxacin population pharmacokinetics and QT interval prolongation and evaluate optimal dosing in children with RR-TB."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
2.5
" Model-based simulations of moxifloxacin pharmacokinetics predicted that current dosing recommendations are too low in children."( Moxifloxacin Pharmacokinetics, Cardiac Safety, and Dosing for the Treatment of Rifampicin-Resistant Tuberculosis in Children.
Draper, HR; Fourie, B; Garcia-Prats, AJ; Hesseling, AC; Nielsen, J; Radtke, KK; Savic, RM; Schaaf, HS; Solans, BP; Thee, S; van der Laan, LE; Wiesner, L; Winckler, JL, 2022
)
2.46
" Continuous electrocardiogram monitoring was performed from >60 min before dosing until 48 h after dosing."( An evaluation of a supratherapeutic dose of inclisiran on cardiac repolarization in healthy volunteers: A phase I, randomized study.
He, Y; Kallend, D; Koren, MJ; Mason, J; Smith, PF; Stoekenbroek, R; Wijngaard, P, 2022
)
0.72
" Subsequently, the effects of pH value, photocatalyst dosage and MOX concentration on the photocatalytic behavior were also studied."( Aminobenzaldehyde convelently modified graphitic carbon nitride photocatalyst through Schiff base reaction: Regulating electronic structure and improving visible-light-driven photocatalytic activity for moxifloxacin degradation.
Bian, C; Dong, X; Li, Y; Liu, Y; Sun, P; Wang, W; Xiao, X; Xiao, Y, 2023
)
1.1
" One oral dose of vehicle, LEVO (10 mg/kg/species) or moxifloxacin (MOXI; 30 mg/kg/dog; 80 mg/kg/NHP) was administered to instrumented animals (N = 8/species) using a cross-over dosing design; MOXI was the in-study positive control."( Evaluation of levocetirizine in beagle dog and cynomolgus monkey telemetry assays: Defining the no QTc effect profile by timepoint and concentration-QTc analysis.
Baublits, J; Chandra, FA; Chui, RW; Engwall, MJ; Jones, ZW; Vargas, HM; Wahlstrom, J, 2023
)
1.16
" For designing an effective clinical cure, a combination of these three agents is required at a therapeutic dosage regimen."( Simultaneous estimation of voriconazole, moxifloxacin, and pirfenidone in rabbit lacrimal matrix using LC-MS/MS: an application to preclinical ocular pharmacokinetics.
Agrawal, S; Bhatta, RS; Bisen, AC; Biswas, A; Mishra, A; Sanap, SN; Verma, SK, 2023
)
1.18
" The recommended volume to be injected is different for the 2 concentrations, and incorrect dosing can increase the risk of toxic anterior segment syndrome or endophthalmitis."( ASCRS clinical advisory on intracameral moxifloxacin injection for infection prophylaxis.
Chang, DF; Mah, FS; Mamalis, N; Miller, KM; Myers, WG; Shorstein, NH, 2023
)
1.18
", minimizing total drug dosage and lowering time needed to sterilize granulomas."( Optimizing tuberculosis treatment efficacy: Comparing the standard regimen with Moxifloxacin-containing regimens.
Borish, HJ; Budak, M; Chishti, HB; Cicchese, JM; Dartois, V; Fillmore, D; Flynn, JL; Frye, LJ; Kirschner, DE; Kracinovsky, K; Lin, PL; Linderman, JJ; Maiello, P; Sakal, J; Scanga, CA; Tomko, J; White, AG, 2023
)
1.14
[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 (7)

ClassDescription
quinolinemonocarboxylic acidAny aromatic carboxylic acid that contains a quinoline moiety that is substituted by one carboxy substituent.
quinolone
cyclopropanesCyclopropane and its derivatives formed by substitution.
pyrrolidinopiperidineAny organic heterobicyclic compound containing ortho-fused pyrrolidine and piperidine rings.
aromatic etherAny ether in which the oxygen is attached to at least one aryl substituent.
quinolone antibioticAn organonitrogen heterocyclic antibiotic whose structure contains a quinolone or quinolone-related skeleton.
fluoroquinolone antibioticAn organonitrogen heterocyclic antibiotic containing a quinolone (or quinolone-like) moiety and which have a fluorine atom attached to the central ring system.
[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]

Protein Targets (24)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Spike glycoproteinSevere acute respiratory syndrome-related coronavirusPotency39.81070.009610.525035.4813AID1479145
[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)
Voltage-dependent L-type calcium channel subunit alpha-1CCavia porcellus (domestic guinea pig)IC50 (µMol)168.90000.02201.64228.9000AID1207666
Voltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)IC50 (µMol)173.00000.00032.63119.0000AID1207753
Bile salt export pumpHomo sapiens (human)IC50 (µMol)1,000.00000.11007.190310.0000AID1449628
Cytochrome P450 3A4Homo sapiens (human)IC50 (µMol)79.43280.00011.753610.0000AID1207530
DNA gyrase subunit BStaphylococcus aureusIC50 (µMol)14.80170.00401.50207.7000AID1801385; AID1909942; AID275463; AID406832; AID595856; AID695234
DNA gyrase subunit AEscherichia coli K-12IC50 (µMol)1.40000.02390.56295.2300AID262137; AID530379
DNA gyrase subunit BEscherichia coli K-12IC50 (µMol)1.40000.00500.43985.2300AID262137; AID530379
DNA topoisomerase 4 subunit AStaphylococcus aureusIC50 (µMol)0.80000.30003.55799.1600AID261732; AID262138
DNA gyrase subunit BMycolicibacterium smegmatisIC50 (µMol)50.00000.04600.16100.2000AID1188153; AID1194330; AID1252459
Replicase polyprotein 1abSevere acute respiratory syndrome-related coronavirusKi249.00000.00753.00839.1100AID1805801
Replicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2Ki249.00000.00001.63079.0000AID1805801
Potassium voltage-gated channel subfamily E member 1Homo sapiens (human)IC50 (µMol)278.29800.12004.048010.0000AID1207376; AID1207406
DNA gyrase subunit AStaphylococcus aureusIC50 (µMol)73.57140.00401.98397.7000AID1909942; AID275463; AID406832; AID406833; AID595856; AID595934; AID695234
Voltage-dependent L-type calcium channel subunit alpha-1CRattus norvegicus (Norway rat)IC50 (µMol)238.76990.00132.24956.9000AID1207530; AID1207564
Potassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)IC50 (µMol)278.29800.12004.048010.0000AID1207376; AID1207406
DNA gyrase subunit BMycobacterium tuberculosis H37RvIC50 (µMol)10.39000.01502.467610.0000AID1152759; AID1164298; AID1188154; AID1194333; AID1242343; AID1252462; AID1266236; AID1272956; AID1909946; AID530368
DNA gyrase subunit AMycobacterium tuberculosis H37RvIC50 (µMol)15.62310.01503.477310.0000AID1152759; AID1164298; AID1188154; AID1194333; AID1242343; AID1252462; AID1266236; AID1272956; AID1909946; AID530368; AID532977; AID532978; AID532979
Voltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)IC50 (µMol)173.00000.00032.59559.0000AID1207753
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)IC50 (µMol)137.06830.00091.901410.0000AID1207470; AID1207530; AID161281; AID1750823; AID243151; AID243188; AID408340; AID420668; AID51930; AID576612; AID695451; AID755684
Voltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)IC50 (µMol)173.00000.00032.63119.0000AID1207753
Voltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)IC50 (µMol)246.66900.00032.25459.6000AID1207564; AID1207666; AID1207753
Sodium channel protein type 5 subunit alphaHomo sapiens (human)IC50 (µMol)145.49980.00033.64849.2000AID1207316; AID1207346
[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)
DNA gyrase subunit AEscherichia coli K-12CC250.50000.20000.35000.5000AID530391
DNA gyrase subunit BEscherichia coli K-12CC250.50000.20000.35000.5000AID530391
DNA gyrase subunit BMycobacterium tuberculosis H37RvCC252.00002.00004.50007.0000AID530380
DNA gyrase subunit AMycobacterium tuberculosis H37RvCC252.00002.00004.50007.0000AID530380
Potassium voltage-gated channel subfamily H member 2Homo sapiens (human)INH129.00007.40007.40007.4000AID1723736
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (190)

Processvia Protein(s)Taxonomy
visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
detection of light stimulus involved in visual perceptionVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
fatty acid metabolic processBile salt export pumpHomo sapiens (human)
bile acid biosynthetic processBile salt export pumpHomo sapiens (human)
xenobiotic metabolic processBile salt export pumpHomo sapiens (human)
xenobiotic transmembrane transportBile salt export pumpHomo sapiens (human)
response to oxidative stressBile salt export pumpHomo sapiens (human)
bile acid metabolic processBile salt export pumpHomo sapiens (human)
response to organic cyclic compoundBile salt export pumpHomo sapiens (human)
bile acid and bile salt transportBile salt export pumpHomo sapiens (human)
canalicular bile acid transportBile salt export pumpHomo sapiens (human)
protein ubiquitinationBile salt export pumpHomo sapiens (human)
regulation of fatty acid beta-oxidationBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transportBile salt export pumpHomo sapiens (human)
bile acid signaling pathwayBile salt export pumpHomo sapiens (human)
cholesterol homeostasisBile salt export pumpHomo sapiens (human)
response to estrogenBile salt export pumpHomo sapiens (human)
response to ethanolBile salt export pumpHomo sapiens (human)
xenobiotic export from cellBile salt export pumpHomo sapiens (human)
lipid homeostasisBile salt export pumpHomo sapiens (human)
phospholipid homeostasisBile salt export pumpHomo sapiens (human)
positive regulation of bile acid secretionBile salt export pumpHomo sapiens (human)
regulation of bile acid metabolic processBile salt export pumpHomo sapiens (human)
transmembrane transportBile salt export pumpHomo sapiens (human)
lipid hydroxylationCytochrome P450 3A4Homo sapiens (human)
lipid metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid catabolic processCytochrome P450 3A4Homo sapiens (human)
xenobiotic metabolic processCytochrome P450 3A4Homo sapiens (human)
steroid metabolic processCytochrome P450 3A4Homo sapiens (human)
cholesterol metabolic processCytochrome P450 3A4Homo sapiens (human)
androgen metabolic processCytochrome P450 3A4Homo sapiens (human)
estrogen metabolic processCytochrome P450 3A4Homo sapiens (human)
alkaloid catabolic processCytochrome P450 3A4Homo sapiens (human)
monoterpenoid metabolic processCytochrome P450 3A4Homo sapiens (human)
calcitriol biosynthetic process from calciolCytochrome P450 3A4Homo sapiens (human)
xenobiotic catabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D metabolic processCytochrome P450 3A4Homo sapiens (human)
vitamin D catabolic processCytochrome P450 3A4Homo sapiens (human)
retinol metabolic processCytochrome P450 3A4Homo sapiens (human)
retinoic acid metabolic processCytochrome P450 3A4Homo sapiens (human)
long-chain fatty acid biosynthetic processCytochrome P450 3A4Homo sapiens (human)
aflatoxin metabolic processCytochrome P450 3A4Homo sapiens (human)
oxidative demethylationCytochrome P450 3A4Homo sapiens (human)
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit AEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit AEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit AEscherichia coli K-12
response to antibioticDNA gyrase subunit AEscherichia coli K-12
chromosome organizationDNA gyrase subunit AEscherichia coli K-12
negative regulation of DNA-templated DNA replicationDNA gyrase subunit AEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
DNA-templated transcriptionDNA gyrase subunit BEscherichia coli K-12
response to xenobiotic stimulusDNA gyrase subunit BEscherichia coli K-12
DNA-templated DNA replicationDNA gyrase subunit BEscherichia coli K-12
DNA topological changeDNA gyrase subunit BEscherichia coli K-12
response to antibioticDNA gyrase subunit BEscherichia coli K-12
chromosome organizationDNA gyrase subunit BEscherichia coli K-12
symbiont-mediated perturbation of host ubiquitin-like protein modificationReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
hematopoietic progenitor cell differentiationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topological changeDNA topoisomerase 2-alphaHomo sapiens (human)
DNA ligationDNA topoisomerase 2-alphaHomo sapiens (human)
DNA damage responseDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome segregationDNA topoisomerase 2-alphaHomo sapiens (human)
female meiotic nuclear divisionDNA topoisomerase 2-alphaHomo sapiens (human)
apoptotic chromosome condensationDNA topoisomerase 2-alphaHomo sapiens (human)
embryonic cleavageDNA topoisomerase 2-alphaHomo sapiens (human)
regulation of circadian rhythmDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of apoptotic processDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of single stranded viral RNA replication via double stranded DNA intermediateDNA topoisomerase 2-alphaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIDNA topoisomerase 2-alphaHomo sapiens (human)
rhythmic processDNA topoisomerase 2-alphaHomo sapiens (human)
negative regulation of DNA duplex unwindingDNA topoisomerase 2-alphaHomo sapiens (human)
resolution of meiotic recombination intermediatesDNA topoisomerase 2-alphaHomo sapiens (human)
sister chromatid segregationDNA topoisomerase 2-alphaHomo sapiens (human)
epithelial cell maturationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
male gonad developmentPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
vestibular nucleus developmentPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
secretory granule organizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to cAMPPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to acidic pHPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cellular response to light stimulusPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cardiac muscle cell action potential involved in contractionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cardiac muscle cell contractionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
negative regulation of protein targeting to membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
regulation of delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
negative regulation of delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
gastrin-induced gastric acid secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
glucose metabolic processPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
heart developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
sensory perception of soundPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
rhythmic behaviorPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of heart contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of blood pressurePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of heart ratePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
iodide transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
erythrocyte differentiationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
intracellular chloride ion homeostasisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
response to insulinPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
social behaviorPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
corticosterone secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
inner ear morphogenesisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
inner ear developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
intestinal absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
detection of mechanical stimulus involved in sensory perception of soundPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
auditory receptor cell developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of cardiac muscle contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of gastric acid secretionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
stomach developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
renal absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
renal sodium ion absorptionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to cAMPPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cellular response to epinephrine stimulusPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
adrenergic receptor signaling pathwayPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cardiac muscle cell contractionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
atrial cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cochlea developmentPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during atrial cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
non-motile cilium assemblyPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
action potentialPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
adenylate cyclase-modulating G protein-coupled receptor signaling pathwayVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
sensory perception of soundVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
positive regulation of calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion importVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
membrane depolarization during SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transporter activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of potassium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by hormonePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of DNA-templated transcriptionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion homeostasisPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cardiac muscle contractionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cellular response to xenobiotic stimulusPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane depolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of heart rate by cardiac conductionPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
membrane repolarization during ventricular cardiac muscle cell action potentialPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
positive regulation of potassium ion transmembrane transportPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
negative regulation of potassium ion export across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
potassium ion import across plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
skeletal system developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
extraocular skeletal muscle developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
striated muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
endoplasmic reticulum organizationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
myoblast fusionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
neuromuscular junction developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle adaptationVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
skeletal muscle fiber developmentVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
release of sequestered calcium ion into cytosolVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cellular response to caffeineVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
immune system developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of cytosolic calcium ion concentrationVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
heart developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of cardiac muscle contraction by regulation of the release of sequestered calcium ionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
embryonic forelimb morphogenesisVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
camera-type eye developmentVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of adenylate cyclase activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
positive regulation of muscle contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transport into cytosolVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transport via high voltage-gated calcium channelVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion transmembrane transportVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cardiac muscle cell action potential involved in contractionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
cell communication by electrical coupling involved in cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rate by cardiac conductionVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of ventricular cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calcium ion import across plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
regulation of heart rateSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac conduction system developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac ventricle developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
brainstem developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of sodium ion transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
response to denervation involved in regulation of muscle adaptationSodium channel protein type 5 subunit alphaHomo sapiens (human)
telencephalon developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
cerebellum developmentSodium channel protein type 5 subunit alphaHomo sapiens (human)
sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
odontogenesis of dentin-containing toothSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
positive regulation of epithelial cell proliferationSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of atrial cardiac muscle cell membrane repolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of ventricular cardiac muscle cell membrane depolarizationSodium channel protein type 5 subunit alphaHomo sapiens (human)
cellular response to calcium ionSodium channel protein type 5 subunit alphaHomo sapiens (human)
cardiac muscle cell action potential involved in contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of cardiac muscle cell contractionSodium channel protein type 5 subunit alphaHomo sapiens (human)
ventricular cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during Purkinje myocyte cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
AV node cell to bundle of His cell communicationSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of heart rate by cardiac conductionSodium channel protein type 5 subunit alphaHomo sapiens (human)
membrane depolarization during atrial cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
regulation of sodium ion transmembrane transportSodium channel protein type 5 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (97)

Processvia Protein(s)Taxonomy
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
protein bindingBile salt export pumpHomo sapiens (human)
ATP bindingBile salt export pumpHomo sapiens (human)
ABC-type xenobiotic transporter activityBile salt export pumpHomo sapiens (human)
bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
canalicular bile acid transmembrane transporter activityBile salt export pumpHomo sapiens (human)
carbohydrate transmembrane transporter activityBile salt export pumpHomo sapiens (human)
ABC-type bile acid transporter activityBile salt export pumpHomo sapiens (human)
ATP hydrolysis activityBile salt export pumpHomo sapiens (human)
monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
steroid bindingCytochrome P450 3A4Homo sapiens (human)
iron ion bindingCytochrome P450 3A4Homo sapiens (human)
protein bindingCytochrome P450 3A4Homo sapiens (human)
steroid hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
retinoic acid 4-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
oxidoreductase activityCytochrome P450 3A4Homo sapiens (human)
oxygen bindingCytochrome P450 3A4Homo sapiens (human)
enzyme bindingCytochrome P450 3A4Homo sapiens (human)
heme bindingCytochrome P450 3A4Homo sapiens (human)
vitamin D3 25-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
caffeine oxidase activityCytochrome P450 3A4Homo sapiens (human)
quinine 3-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
testosterone 6-beta-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1-alpha,25-dihydroxyvitamin D3 23-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 8,9 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 11,12 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
anandamide 14,15 epoxidase activityCytochrome P450 3A4Homo sapiens (human)
aromatase activityCytochrome P450 3A4Homo sapiens (human)
vitamin D 24-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 16-alpha-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
estrogen 2-hydroxylase activityCytochrome P450 3A4Homo sapiens (human)
1,8-cineole 2-exo-monooxygenase activityCytochrome P450 3A4Homo sapiens (human)
DNA bindingDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit AEscherichia coli K-12
protein bindingDNA gyrase subunit AEscherichia coli K-12
ATP bindingDNA gyrase subunit AEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit AEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit AEscherichia coli K-12
identical protein bindingDNA gyrase subunit AEscherichia coli K-12
DNA bindingDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase activityDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA gyrase subunit BEscherichia coli K-12
protein bindingDNA gyrase subunit BEscherichia coli K-12
ATP bindingDNA gyrase subunit BEscherichia coli K-12
ATP-dependent activity, acting on DNADNA gyrase subunit BEscherichia coli K-12
DNA negative supercoiling activityDNA gyrase subunit BEscherichia coli K-12
metal ion bindingDNA gyrase subunit BEscherichia coli K-12
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K63-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
K48-linked deubiquitinase activityReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
3'-5'-RNA exonuclease activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA-dependent RNA polymerase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
cysteine-type endopeptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA 5'-cap (guanine-N7-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA (nucleoside-2'-O-)-methyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
mRNA guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
RNA endonuclease activity, producing 3'-phosphomonoestersReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
ISG15-specific peptidase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
5'-3' RNA helicase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
protein guanylyltransferase activityReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
magnesium ion bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
chromatin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
RNA bindingDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) activityDNA topoisomerase 2-alphaHomo sapiens (human)
protein kinase C bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP bindingDNA topoisomerase 2-alphaHomo sapiens (human)
ATP-dependent activity, acting on DNADNA topoisomerase 2-alphaHomo sapiens (human)
DNA binding, bendingDNA topoisomerase 2-alphaHomo sapiens (human)
protein homodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
ubiquitin bindingDNA topoisomerase 2-alphaHomo sapiens (human)
protein heterodimerization activityDNA topoisomerase 2-alphaHomo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
potassium channel regulator activityPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
telethonin bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
protein-containing complex bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
transmembrane transporter bindingPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
calmodulin bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
phosphatidylinositol-4,5-bisphosphate bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein phosphatase 1 bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
outward rectifier potassium channel activityPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein kinase A catalytic subunit bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
protein kinase A regulatory subunit bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
transmembrane transporter bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in atrial cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
ankyrin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel activity involved SA node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
transcription cis-regulatory region bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
delayed rectifier potassium channel activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
ubiquitin protein ligase bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
identical protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
protein homodimerization activityPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
C3HC4-type RING finger domain bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
scaffold protein bindingPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarizationPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
small molecule bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
molecular function activator activityVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
protein bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
calmodulin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
high voltage-gated calcium channel activityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
metal ion bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
alpha-actinin bindingVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in cardiac muscle cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel activity involved in AV node cell action potentialVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated sodium channel activitySodium channel protein type 5 subunit alphaHomo sapiens (human)
protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
calmodulin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
fibroblast growth factor bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
enzyme bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein kinase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
protein domain specific bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ankyrin bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
ubiquitin protein ligase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
transmembrane transporter bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
nitric-oxide synthase bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in cardiac muscle cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in AV node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in bundle of His cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in Purkinje myocyte action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel activity involved in SA node cell action potentialSodium channel protein type 5 subunit alphaHomo sapiens (human)
scaffold protein bindingSodium channel protein type 5 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (62)

Processvia Protein(s)Taxonomy
photoreceptor outer segmentVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1FHomo sapiens (human)
basolateral plasma membraneBile salt export pumpHomo sapiens (human)
Golgi membraneBile salt export pumpHomo sapiens (human)
endosomeBile salt export pumpHomo sapiens (human)
plasma membraneBile salt export pumpHomo sapiens (human)
cell surfaceBile salt export pumpHomo sapiens (human)
apical plasma membraneBile salt export pumpHomo sapiens (human)
intercellular canaliculusBile salt export pumpHomo sapiens (human)
intracellular canaliculusBile salt export pumpHomo sapiens (human)
recycling endosomeBile salt export pumpHomo sapiens (human)
recycling endosome membraneBile salt export pumpHomo sapiens (human)
extracellular exosomeBile salt export pumpHomo sapiens (human)
membraneBile salt export pumpHomo sapiens (human)
cytoplasmCytochrome P450 3A4Homo sapiens (human)
endoplasmic reticulum membraneCytochrome P450 3A4Homo sapiens (human)
intracellular membrane-bounded organelleCytochrome P450 3A4Homo sapiens (human)
chromosomeDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
cytosolDNA gyrase subunit AEscherichia coli K-12
membraneDNA gyrase subunit AEscherichia coli K-12
cytoplasmDNA gyrase subunit AEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit AEscherichia coli K-12
chromosomeDNA gyrase subunit BEscherichia coli K-12
cytoplasmDNA gyrase subunit BEscherichia coli K-12
cytosolDNA gyrase subunit BEscherichia coli K-12
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA gyrase subunit BEscherichia coli K-12
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome-related coronavirus
double membrane vesicle viral factory outer membraneReplicase polyprotein 1abSevere acute respiratory syndrome coronavirus 2
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
nuclear chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
centrioleDNA topoisomerase 2-alphaHomo sapiens (human)
chromosome, centromeric regionDNA topoisomerase 2-alphaHomo sapiens (human)
condensed chromosomeDNA topoisomerase 2-alphaHomo sapiens (human)
male germ cell nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
nucleoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
nucleolusDNA topoisomerase 2-alphaHomo sapiens (human)
cytoplasmDNA topoisomerase 2-alphaHomo sapiens (human)
DNA topoisomerase type II (double strand cut, ATP-hydrolyzing) complexDNA topoisomerase 2-alphaHomo sapiens (human)
protein-containing complexDNA topoisomerase 2-alphaHomo sapiens (human)
ribonucleoprotein complexDNA topoisomerase 2-alphaHomo sapiens (human)
nucleusDNA topoisomerase 2-alphaHomo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
lysosomePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
Z discPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily E member 1Homo sapiens (human)
early endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytoplasmPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
lysosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
early endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
late endosomePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
endoplasmic reticulumPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
basolateral plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
apical plasma membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
transport vesiclePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
cytoplasmic vesicle membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
neuron projectionPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
neuronal cell bodyPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membrane raftPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
ciliary basePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
lumenal side of membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
basolateral part of cellPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
monoatomic ion channel complexPotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
membranePotassium voltage-gated channel subfamily KQT member 1Homo sapiens (human)
virion membraneSpike glycoproteinSevere acute respiratory syndrome-related coronavirus
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1D Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cell surfacePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
perinuclear region of cytoplasmPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
voltage-gated potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
inward rectifier potassium channel complexPotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
plasma membranePotassium voltage-gated channel subfamily H member 2Homo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
sarcoplasmic reticulumVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
T-tubuleVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
I bandVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1SHomo sapiens (human)
cytoplasmVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
plasma membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic densityVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
Z discVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
dendriteVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
perikaryonVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
postsynaptic density membraneVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
L-type voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
voltage-gated calcium channel complexVoltage-dependent L-type calcium channel subunit alpha-1CHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
nucleolusSodium channel protein type 5 subunit alphaHomo sapiens (human)
endoplasmic reticulumSodium channel protein type 5 subunit alphaHomo sapiens (human)
plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
caveolaSodium channel protein type 5 subunit alphaHomo sapiens (human)
cell surfaceSodium channel protein type 5 subunit alphaHomo sapiens (human)
intercalated discSodium channel protein type 5 subunit alphaHomo sapiens (human)
membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
lateral plasma membraneSodium channel protein type 5 subunit alphaHomo sapiens (human)
Z discSodium channel protein type 5 subunit alphaHomo sapiens (human)
T-tubuleSodium channel protein type 5 subunit alphaHomo sapiens (human)
sarcolemmaSodium channel protein type 5 subunit alphaHomo sapiens (human)
perinuclear region of cytoplasmSodium channel protein type 5 subunit alphaHomo sapiens (human)
voltage-gated sodium channel complexSodium channel protein type 5 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (3673)

Assay IDTitleYearJournalArticle
AID1318903Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33592 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID279207Antibacterial activity against Streptococcus pneumoniae 3676 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID1600103Antibacterial activity against Bacillus subtilis ATCC 6633 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID559069Antibacterial activity against Acinetobacter baumannii by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID571366Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID575079Antimicrobial activity against Streptococcus pneumoniae serotype 7F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID341089Antimicrobial activity against Clostridium difficile clinical isolates by agar dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
In vitro activities of 15 antimicrobial agents against 110 toxigenic clostridium difficile clinical isolates collected from 1983 to 2004.
AID570795Half life in healthy human at 400 mg, po qd measured on day 4 by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID511393Antibacterial activity against Levofloxacin resistant Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID518617Antimicrobial activity against Mycobacterium avium by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID558629Antimicrobial activity against Streptococcus pneumoniae isolate 3791 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID531526Antibacterial activity against Bacteroides distasonis isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1740327Antimicrobial activity against Listeria monocytogenes ATCC 19115 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID422657Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3665 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID279265Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3243 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID1398607Inhibition of human ERG expressed in CHOK1 cells at 30 uM2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID285973Antimicrobial susceptibility against Haemophilus influenzae D4 isolate with GyrA Ser84Tyr, ParC Glu88Lys and AcrR Leu31His, Ile121Val and Gln134Lys mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID283400Antimicrobial activity against Nocardia sp. after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID553806Antimicrobial activity against Clostridium difficile PCR ribotype 001 expressing gyrB Glu466Lys mutant grown on fluoroquinolone-containing medium after 48 hrs2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID530596Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr8 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID530347Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M carrying blaCTX-M-15 and pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID695234Inhibition of Staphylococcus aureus DNA gyrase by supercoiling assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID508372Antibacterial activity against Streptococcus pneumoniae harboring erm(B) and mef(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID530372Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID341068Half life in human at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID574488Antimicrobial activity against Bacteroides distasonis after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID563216Antimycobacterial activity against Mycobacterium tuberculosis 08-0815 harboring gyrA Thr80Ala and Ala90Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID574778Antimicrobial activity against Clostridium difficile assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1877413Antibacterial activity against Neisseria gonorrhoeae Barla1942022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID522951Antibacterial activity against methicillin-, ciprofloxacin-resistant Staphylococcus aureus by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1126755Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 741 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID580758Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559078Antibacterial activity against Klebsiella oxytoca by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1243290Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis clinical isolates by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID428781Cmax in human at 400 mg, po administered once a day2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID456046Antibacterial activity against vancomycin-resistant Enterococcus faecium after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID425813Antimicrobial activity against avirulent Mycobacterium tuberculosis H37Ra2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID531517Antibacterial activity against Bacteroides vulgatus assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID559172Antimicrobial activity against Clostridium difficile BI2f harboring GyrB Arg447Lys and Asp426Asn mutant gene selected after 32 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID522967Antibacterial activity against Serratia marcescens by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID249970Ratio of MPC to MIC against methicillin resistant Staphylococcus aureus-50232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1318901Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 860522016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1152777Antimycobacterial activity against 5-(((3S,4R)-3-Fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA D89N mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID558700Antimicrobial activity against Clostridium difficile 630 expressing tcdA and tcdB gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID562439Antibacterial activity against Staphylococcus aureus SMH36633 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID573594Antibacterial activity against Fusobacterium varium assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID580900Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559533Antibacterial activity against Klebsiella oxytoca assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID532675Antimicrobial activity against ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID593809Antimicrobial activity against Escherichia coli ATCC 8739 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID574760Antimicrobial activity against Peptoniphilus asaccharolyticus assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID570689Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID425544Antibacterial activity against Streptococcus pneumoniae HMC 1541 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1877420Antibacterial activity against Neisseria gonorrhoeae WHO A2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID1067082Antimicrobial activity against Staphylococcus aureus 209 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID559176Antimicrobial activity against Clostridium difficile C253A selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1514449Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID574518Antimicrobial activity against Prevotella intermedia after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1551299Antibacterial activity against Quinolone-resistant Staphylococcus aureus CCARM 3505 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1909954Stabilization of mycobacterium tuberculosis DNA gyrase/Doubly-cleaved DNA complex at 100 uM incubated for 30 mins by gel electrophoresis method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1164015Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID559488Antibacterial activity against Peptostreptococcus sp. by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1348987Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 72 hrs by MTT assay
AID1557288Antibacterial activity against Clostridium perfringens by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID520108Antimicrobial activity against Mycobacterium tuberculosis H37Rv at assessed as growth inhibition at 10 mg/kg following 24 days oxygen depletion by Wayne method relative to control2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID562457Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH367422009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID574734Antimicrobial activity against Fusobacterium necrogenes after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID562646Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH366332009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID425548Antibacterial activity against Streptococcus pneumoniae HMC 1062 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID520375Ratio of AUC (0 to 24 hrs) in plasma to CSF in patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QID2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
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.
AID576139Antibacterial activity against 10'4 to 10'5 CFU Streptococcus pneumoniae after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID574482Antimicrobial activity against Bacteroides fragilis after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID283159Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2526 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID571145Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID523161Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC4222 harboring gyrA S84L and parC S80F mutant gene by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID593900Antimicrobial activity against Aspergillus niger ATCC 6275 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID425543Antibacterial activity against Streptococcus pneumoniae HMC 1156 harboring S81F and S79F mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively showing efflux to ciprofloxacin, gemifloxacin by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1381460Toxicity in C57BL/6 mouse infected with Mycobacterium tuberculosis H37Rv at 30 mg/kg, po for 8 consecutive days starting from day 1 post infection2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
AID422650Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3665 after 38 passages with moxifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1297347Antibacterial activity against Streptococcus pneumoniae ATCC 19615 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID571926Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-N623S-Q624S mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID562945Upregulation of cwp84 gene expression in Clostridium difficile CD196 M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1877410Antibacterial activity against methicillin-resistant Staphylococcus aureus 1962022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID1391313Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate CCARM 3167 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID388870Antibacterial activity against Staphylococcus aureus ATCC 13709 after 24 hrs by microdilution method2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID1398636In vivo antibacterial activity against quinolone-sensitive and penicillin-resistant Streptococcus pneumoniae 033806 infected in CBA/JNCrj mouse assessed as reduction in bacterial count at 40 to 80 mg/kg, sc administered twice per day starting from 1 day a2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID436985Inhibition of human HeLa cell proliferation assessed as bromodeoxyuridine incorporation during DNA synthesis after 48 hrs by ELISA2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
7-((4-Substituted)piperazin-1-yl) derivatives of ciprofloxacin: synthesis and in vitro biological evaluation as potential antitumor agents.
AID562926Antimicrobial activity against Clostridium difficile CD196 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID563057Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0821 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559486Antibacterial activity against Clostridium perfringens by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID571374Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID575005Antimicrobial activity against Eubacterium sp. after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID586640Antibacterial activity against Escherichia coli ATCC 25922 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID422666Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1076 after 35 passages with moxifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID573581Antibacterial activity against beta-lactamase producing Bacteroides caccae by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID581483Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID518802Antimycobacterial activity against Mycobacterium intracellular serovar 16 after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID571576Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID285284Susceptibility of penicillin-resistant Streptococcus pneumoniae 334 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID528975Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID563050Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0797 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1053480Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA M103L mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID522964Antibacterial activity against Enterobacter cloacae by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID498187Antibacterial activity against Stenotrophomonas maltophilia D457 containing chromosomally encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID553685Antimicrobial activity against Bacteroides sp. in three-stage chemostat gut model assessed as log reduction in bacterial count at 43 mg/liter administered daily for 7 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID570798AUC (0 to 24 hrs ) in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID580761Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID530589Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr1 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID422658Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1077 after 49 passages with clindamycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID540219Volume of distribution at steady state in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID574746Antimicrobial activity against Peptostreptococcus anaerobius assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID278600Inhibitory activity against Klebsiella pneumoniae 07-0062007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID433401Inhibition of Mycobacterium leprae DNA gyrase subunit A G89C mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1447483Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P264-104354 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID518629Ratio of AUC (0 to 24 hrs) in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic model to MIC for Mycobacterium avium at 90% maximal effective concentration2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID275450Antibacterial activity against methicillin-resistant Staphylococcus aureus2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID563008Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0790 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID283396Antimicrobial activity against Nocardia veterana after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID518803Antimycobacterial activity against Mycobacterium chelonae after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID573593Antibacterial activity against Fusobacterium necrophorum by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID559047Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus epidermidis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID580996Ratio of Cmax in healthy human at 400 mg/kg, po administered as a single dose to MIC90 for Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID533425Antimicrobial activity against Peptostreptococcus sp. by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1570244Antimycobacterial activity against rifampicin-resistant Mycobacterium tuberculosis incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID342062Antimicrobial activity against nonepidemic Clostridium difficile ATCC 9689 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID438557Antimycobacterial activity against non replicating persistent form of Mycobacterium tuberculosis H37Rv after 10 days by low oxygen recovery assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.
AID323659Antibacterial activity against Peptostreptococcus anaerobius2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Antimicrobial susceptibilities of Peptostreptococcus anaerobius and the newly described Peptostreptococcus stomatis isolated from various human sources.
AID534362Ratio of MIC for Escherichia coli K-12 KD2934 harboring gyrB K447E mutant gene to MIC for Escherichia coli K-12 KD1397 harboring wild type gyrB gene2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones.
AID559059Antibacterial activity against non-levofloxacin susceptible Streptococcus pneumoniae by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID424334Antimicrobial activity against Dialister invisus assessed as susceptibility breakpoint by CLSI-M11-A7 method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID571111Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID571846Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1164298Inhibition of Mycobacterium tuberculosis DNA gyrase-mediated relaxed pBR322 DNA supercoiling by gel electrophoresis2014ACS medicinal chemistry letters, Sep-11, Volume: 5, Issue:9
2-Phenylindole and Arylsulphonamide: Novel Scaffolds Bactericidal against Mycobacterium tuberculosis.
AID531521Antibacterial activity against Bacteroides stercoris isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
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.
AID1903315Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 8 days by Alamar blue assay2022European journal of medicinal chemistry, Mar-15, Volume: 232Discovery of 3H-pyrrolo[2,3-c]quinolines with activity against Mycobacterium tuberculosis by allosteric inhibition of the glutamate-5-kinase enzyme.
AID1476364Antitubercular activity against streptomycin resistant Mycobacterium tuberculosis H37Rv ATCC 35820 after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1079942Steatosis, proven histopathologically. Value is number of references indexed. [column 'STEAT' in source]
AID425069Antimicrobial activity against multidrug-resistant Klebsiella pneumoniae M7943 bearing qnrB10 gene with aac(6)-Ib-cr-blaOXA-30 catB3-arr-3 integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID533135Antimicrobial activity against Bacteroides ovatus by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID574953Antimicrobial activity against Streptococcus pneumoniae serotype 6C by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID520617Antimicrobial activity against Nocardia brasiliensis HUJEG-1 by broth macrodilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
In vivo therapeutic effect of gatifloxacin on BALB/c mice infected with Nocardia brasiliensis.
AID522955Antibacterial activity against Streptococcus pyogenes by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1399856Antitubercular activity against fluoroquinolone-resistant Mycobacterium tuberculosis H37Rv harboring gyrA D94N mutant2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID406834Inhibition of Staphylococcus aureus wild-type topoisomerase 4 decatenation activity assessed as unlinking of DNA microcircles from kinetoplast DNA2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID433404Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1318902Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1237403Antibacterial activity against Staphylococcus aureus KCTC 209 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1164003Antibacterial activity against methicillin-sensitive Staphylococcus aureus 12-2 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1254068Antibacterial activity against Staphylococcus aureus 209 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID323887Antimicrobial activity against qnrA1 expressing Escherichia coli J53/pMG252 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1297325Antibacterial activity against Klebsiella pneumoniae 14-1 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1318912Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID561324Antimicrobial activity against Klebsiella pneumoniae isolate 132 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID1890604Antibacterial activity against methicillin resistant Staphylococcus aureus 5076 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI based serial agar dilution method2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID323886Antimicrobial activity against qnrA1 expressing Escherichia coli J53/pMG252 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1254074Antibacterial activity against Pseudomonas aeruginosa 2004 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID563340Effect on Cwp84 protease expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID581101Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID601779Antibacterial activity against 10'4 CFU methicillin-resistant Staphylococcus aureus 08-1 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID529896Antimicrobial activity against Leptospira interrogans serovar Pomona isolate 4 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1750819Cytotoxicity against human K562 cells after 72 hrs by CellTiter Glo assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID531522Antibacterial activity against Bacteroides merdae isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID581298Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID558622Antimicrobial activity against Streptococcus pneumoniae isolate 3374 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID428771Bactericidal activity against Streptococcus pneumoniae isolate SR-26137 by broth dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1391316Antibacterial activity against Escherichia coli 1924 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID164231Antibacterial activity was evaluated against Pseudomonas aeruginosa2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID424326Antimicrobial activity against Dialister micraerophilus assessed as susceptibility breakpoint by CLSI-M11-A7 method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID1877417Antibacterial activity against Neisseria gonorrhoeae WHO E2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID425564Antibacterial activity against quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 5048 expressing mefA after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425555Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 99 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID494416Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 72 hrs by serial double dilution method2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.
AID521152Antibacterial activity against intracellular Listeria monocytogenes EGDe infected in bone marrow-derived BALB/c mouse macrophage assessed as prevention of bacterial release and spread of infection by preventing macrophage lysis after 24 hrs2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID562464Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH380022009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID581287Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID522953Antibacterial activity against methicillin-resistant Staphylococcus epidermidis by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID573823Antibacterial activity against beta-lactamase producing Clostridium paraputrificum by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID428847Time above the mutant prevention concentration in Streptococcus pneumoniae isolate SR-26134 infected human at 80 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID574051Antibacterial activity against beta-lactamase producing Finegoldia magna assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1564359Antimycobacterial activity against Mycobacterium avium subsp. avium ATCC 25291 by resazurin dye based fluorimetric assay2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID586638Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrB gene and pBK-QnrB1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1256562Antibacterial activity against Streptococcus pneumoniae ATCC 19615 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID574985Antimicrobial activity against Actinomyces naeslundii assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID511392Antibacterial activity against Levofloxacin susceptible Streptococcus pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID576132Antibacterial activity against 10'4 to 10'5 CFU Haemophilus influenzae after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID322791Antimicrobial activity against Bacteroides merdae assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID728907Inhibition of human ERG expressed in CHOK1 cells at 30 uM2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1398590Antibacterial activity against Staphylococcus aureus SMITH after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID562623Antimicrobial activity against Coagulase-negative Staphylococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1318931Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 920142016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID532969Antimicrobial activity against Mycobacterium tuberculosis isolate 13 isolated from Beijing2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID580766Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID571355Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1185144Antimicrobial activity against 2-oxo-1-(2-(4-((3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino)piperidin-1-yl)ethyl)-1,2-dihydroquinoline-7-carbonitrile resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase A74V mutant2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID322781Antimicrobial activity against Bacteroides stercoris isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID562454Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH380022009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID699004Antimycobacterial activity against Mycobacterium tuberculosis H37Rv2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1067071Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolate 3506 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1318909Antibacterial activity against gentamicin-resistant Escherichia coli isolate CAN-ICU 61714 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID581654Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient at pH 7.4 after 48 hrs by broth microdilution method in absence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID559182Antimicrobial activity against Clostridium difficile C253D selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1297351Antibacterial activity against Enterococcus faecalis 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID523175Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC8525 harboring wild type quinolone resistance-determining region assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID372979Antimycobacterial activity against Mycobacterium intracellular JATA52-01 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID559512Antibacterial activity against Lancefield Streptococcus sp. 'group G' assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID530380Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID425774Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB after 36 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID562651Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH380022009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID508380Antibacterial activity against macrolide-resistant Streptococcus pneumoniae harboring mutation in L4 ribosomal protein after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID544820Antimicrobial activity against Staphylococcus epidermidis Xen 43 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID563013Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2614 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID430964Antibacterial activity against Escherichia coli 1596 containing gyrA L83 and parC I80, G84 mutants assessed as increase in MIC by Etest relative to MIC for Escherichia coli 1608 containing gyrA mutant2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID521329AUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1067078Antimicrobial activity against Escherichia coli CCARM 1356 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID570693Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID573796Antibacterial activity against Prevotella bivia assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1164000Antibacterial activity against Pseudomonas aeruginosa 12-14 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID518311Cardiotoxicity in healthy human assessed as change in corrected QT interval at 400 mg/kg, po within 3 hrs by ECG2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID562633Antimicrobial activity against Streptococcus pneumoniae assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID531629Antimicrobial activity against Ureaplasma parvum by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID405456Antibacterial activity against Escherichia coli C600Rif in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID341074AUC (0 to 24 hrs) in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID518623Antimicrobial activity against Mycobacterium avium subsp. hominissuis ATCC 700898 infected in human THP1 cells in presence of 20% FBS2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID571841Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID669186Antitubercular activity against Mycobacterium tuberculosis H37Rv in aerobic conditions after 7 days by microplate-based alamar blue assay2012Journal of medicinal chemistry, Apr-26, Volume: 55, Issue:8
Structure-based design of novel benzoxazinorifamycins with potent binding affinity to wild-type and rifampin-resistant mutant Mycobacterium tuberculosis RNA polymerases.
AID522959Antibacterial activity against Enterococcus faecium by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1237405Antibacterial activity against Streptococcus mutans 3065 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID425805Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung after 1 day after 1st successive aerosol infection run2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID428814Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID581667Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level after 24 hrs in presence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID570698Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID562624Antimicrobial activity against Group A Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID511304Antibacterial activity against ciprofloxacin and methicillin resistant Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID559177Antimicrobial activity against Clostridium difficile C253B selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID571144Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1256559Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-22 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1551292Antibacterial activity against Staphylococcus aureus KCTC503 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID511398Antibacterial activity against Pseudomonas aeruginosa by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID571851Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID573591Antibacterial activity against Fusobacterium nucleatum by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID285971Antimicrobial susceptibility against Haemophilus influenzae D2 isolate with GyrA Ser84Tyr, ParC Glu88Lys and AcrR Leu31His, Ile121Val and Gln134Lys mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID1256532Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID576612Inhibition of human ERG2011European journal of medicinal chemistry, Feb, Volume: 46, Issue:2
Predicting hERG activities of compounds from their 3D structures: development and evaluation of a global descriptors based QSAR model.
AID285291Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID428859Bactericidal activity against Streptococcus pneumoniae isolate SR-26134 assessed as prevention of bacterial regrowth under condition simulating oral administration of 400 mg once daily after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID522960Antibacterial activity against Haemophilus influenzae by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID484799Antibacterial activity against Staphylococcus aureus K1134 bearing wild-type GyrA and S80Y mutant GrlA by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID563058Antimycobacterial activity against Mycobacterium tuberculosis 04-0649 harboring gyrA Asp94Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID283149Antimicrobial susceptibility of Staphylococcus lugdunensis isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID324749Antibacterial activity in Mycobacterium leprae infected mouse foot-pad model assessed as parasite killing at 150 mg/kg/day after 9 months2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID1256541Antibacterial activity against Klebsiella pneumoniae 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID511394Antibacterial activity against Streptococcus pyogenes by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID1237415Bactericidal activity against Streptococcus mutans 3065 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID531520Antibacterial activity against Bacteroides fragilis assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1330187Antibacterial activity against Staphylococcus aureus 209 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID565328Antibacterial activity against Mycoplasma genitalium M6282 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID544843Antibacterial activity against Streptococcus pneumoniae U2A1693 harboring parC Asp83Asn mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID456027Antibacterial activity against Staphylococcus epidermidis 56500 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID563028Antimycobacterial activity against Mycobacterium tuberculosis 08-0815 harboring gyrA Thr80Ala and Ala90Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1403709Antimycobacterial activity against Mycobacterium marinum ATCC BAA-535 infected in zebrafish at 5 mg/kg, po treated for 7 days by MPN assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID1601848Antibacterial activity against Escherichia coli CMCC 44568 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID534363Ratio of MIC for Escherichia coli K-12 KD2932 harboring gyrB D426N mutant gene to MIC for Escherichia coli K-12 KD1397 harboring wild type gyrB gene2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones.
AID558583Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559153Antimicrobial activity against Clostridium difficile 630e selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID580894Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID285300Effect on 4 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID574526Antimicrobial activity against Prevotella intermedia assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID484793Antibacterial activity against Escherichia coli ATCC 25922 by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID1154327Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID279817Antimicrobial activity against Mycobacterium tuberculosis H37Rv in 7H9 broth2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID522970Antibacterial activity against Citrobacter freundii by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581480Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID571386Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID571931Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB-S623N mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID588213Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in non-rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID581074Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID584563Antimicrobial activity against Acinetobacter lwoffii isolate J expressing beta-lactamase OXA-58 isolated from bedsore by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID543391Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as increase in mouse survival at 50 mg/kg, ip administered 36 hrs postinfection as single dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID558882Antimicrobial activity against Clostridium difficile C253c selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID556021P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID559081Antibacterial activity against Moraxella catarrhalis by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID571876Antibacterial activity against Acinetobacter baumannii assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1179482Antimycobacterial activity against Mycobacterium kansasii ATCC 12478 in 7H9 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID558613Antimicrobial activity against Streptococcus pneumoniae isolate 2686 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559075Antibacterial activity against Enterobacter cloacae by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID244998Antibacterial activity against Enterococcus faecalis ATCC 19433 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID323890Antimicrobial activity against qnrA1 expressing Escherichia coli J53/p1960 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID570808Ratio of Apparent oral clearance in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose to Apparent oral clearance in healthy human at 400 mg, po qd m2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID570906Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559004Antibacterial activity against Streptococcus pneumoniae W001 harboring wild-type parC and gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1256546Antibacterial activity against Pseudomonas aeruginosa 14-14 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID559048Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus epidermidis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1256549Antibacterial activity against Pseudomonas aeruginosa 14-19 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID518626Half life in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic modell by LC analysis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID341374Antibacterial activity against Staphylococcus aureus at 0.5 mg/liter by time kill assay2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID425338Antibacterial activity against azithromycin-susceptible Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID562939Effect on fbp69 gene expression in Clostridium difficile 6425 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID574776Antimicrobial activity against Clostridium difficile after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID728918Antibacterial activity against Klebsiella pneumoniae TYPE1 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1760640Antibacterial activity against Mycobacterium tuberculosis H37Ra ATCC2517 assessed as inhibition of bacterial growth measured after 17 hrs by resazurin based flourimetric assay2021European journal of medicinal chemistry, Feb-05, Volume: 211Synthesis and structure-activity studies of novel anhydrohexitol-based Leucyl-tRNA synthetase inhibitors.
AID565325Antibacterial activity against Mycoplasma genitalium M6328 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID283392Antimicrobial activity against Nocardia otitidiscaviarum after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID531530Antibacterial activity against Bacteroides thetaiotaomicron isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1237427Bactericidal activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1909951Antibacterial activity against Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph assessed as inhibition of bacterial growth incubated for 11 days2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID574782Antimicrobial activity against Actinomyces odontolyticus after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID581487Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID574486Antimicrobial activity against Bacteroides caccae after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1067073Antimicrobial activity against Candida albicans 7535 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1890603Antibacterial activity against Staphylococcus aureus ATCC 25293 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI based serial agar dilution method2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID1676599Binding affinity to cupric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID562446Antibacterial activity against Staphylococcus aureus SMH37276 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID573786Antibacterial activity against Prevotella melaninogenica by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID574995Antimicrobial activity against Bifidobacterium sp. assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID580897Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID246829Efficacy against mice infected with MRSA-33 upon s.c. administration2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID535772Antimicrobial activity against Mycobacterium ulcerans 1059 agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID518618Antimicrobial activity against Mycobacterium avium subsp. hominissuis ATCC 700898 by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID556777Volume of distribution in peripheral compartment in osteomyelitis patient at 400 mg, po administered for every 24 hrs by MAP-Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID586729Antibacterial activity against qnrS gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrS1 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID373002Antimycobacterial activity against Mycobacterium avium complex N018 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1877402Antibacterial activity against Escherichia coli 2022022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID1256539Antibacterial activity against ESBL-positive Klebsiella pneumoniae 14-19 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID369227Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae by microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Serotypes, Clones, and Mechanisms of Resistance of Erythromycin-Resistant Streptococcus pneumoniae Isolates Collected in Spain.
AID261737Antibacterial activity against Streptococcus pneumoniae ATCC 496192006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID558910Antimicrobial activity against Clostridium difficile CD5 1-g harboring GyrA Ala92Glu and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID521327AUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1600107Antibacterial activity against Pseudomonas aeruginosa ATCC 9027 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID523143Antibacterial activity against Streptococcus pneumoniae isolate OC7348 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID570889Antibacterial activity against Levofloxacin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1398596Antibacterial activity against Escherichia coli NIHJ after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID728920Antibacterial activity against Streptococcus pyogenes G-36 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID531524Antibacterial activity against Bacteroides spp. isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1154349Antimycobacterial activity against Mycobacterium tuberculosis over expressing TopA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID521825Antimicrobial activity against beta-lactam resistant Streptococcus pneumoniae clinical isolate by broth dilution method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Clonal spread of highly beta-lactam-resistant Streptococcus pneumoniae isolates in Taiwan.
AID559485Antibacterial activity against Bacteroides fragilis by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID759325Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID565320Antibacterial activity against Mycoplasma genitalium M2341 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1398595Antibacterial activity against Bacillus subtilis ATCC 6633 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID278601Inhibitory activity against azide-resistant Escherichia coli J53 T07-0062007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID285301Effect on 8 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID580887Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID573834Antibacterial activity against beta-lactamase producing Clostridium perfringens assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID533421Antimicrobial activity against Anaerococcus prevotii by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID586727Antibacterial activity against qnrA gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrA1 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID425652Total body clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1877415Antibacterial activity against Neisseria gonorrhoeae WHO O2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID425547Antibacterial activity against Streptococcus pneumoniae HMC 4026 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID565308Antibacterial activity against Mycoplasma genitalium by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID245040Minimum inhibitory concentration against Staphylococcus saprophyticus ATCC 153052005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID559073Antibacterial activity against Citrobacter koseri by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559141Antimicrobial activity against Clostridium difficile A422h harboring GyrA Asp81Asn mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID244991Minimum inhibitory concentration against vancomycin intermediate Staphylococcus aureus MU 502005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID562647Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH370992009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID672348Antibacterial activity against Escherichia coli ATCC 259222012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives.
AID323874Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae1960 GyrA Ser83Phe mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID422664Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1077 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID425572Antibacterial activity against penicillin-, macrolide- and quinolone-susceptible Streptococcus pneumoniae HMC 63 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83Y mutation in QRDR of ParC gene and I460V mutation in QRDR2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID563011Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 99-1914 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID518058Toxicity in healthy human assessed as abdominal pain at 400 mg/kg, po administered as single dose2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID1601849Antibacterial activity against Pseudomonas aeruginosa CMCC 27853 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID586633Antibacterial activity against qnrA gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrA1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1330188Antibacterial activity against Streptococcus mutans 3065 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID406653Antibacterial activity against Staphylococcus aureus ACH-0210 isolate with gyrA Ser84Leu and grlA Ser80Phe mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID518801Antimycobacterial activity against Mycobacterium avium serovar 8 after 14 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID430965Antibacterial activity against Escherichia coli 1596 containing parC K84 mutant assessed as decrease in MIC by Etest relative to MIC for Escherichia coli 1608 containing gyrA mutant2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID425549Antibacterial activity against Streptococcus pneumoniae HMC 1068 harboring E85K mutation in quinolone-resistant determining regions of GyrA gene, S79Y, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to ciproflox2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID508378Antibacterial activity against macrolide-resistant Streptococcus pneumoniae harboring mef(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID581067Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID542718Drug level in human plasma at 400 mg/day after 8 hrs2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Efficacy of ciprofloxacin and moxifloxacin against Nocardia brasiliensis in vitro and in an experimental model of actinomycetoma in BALB/c mice.
AID1164006Antibacterial activity against methicillin-resistant Staphylococcus aureus 12-2 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1164013Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 12-1 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID484797Antibacterial activity against Staphylococcus aureus SA-1199B norA++ and A116E GrlA mutation by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID586631Antibacterial activity against qnrS gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrS1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID581314Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID283239Reduction of bacterial counts in Mycobacterium tuberculosis H37Rv infected Swiss mouse lung at 100 mg/kg, po for 5 days/week after 1 month2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID1319010Selectivity ratio of MIC for Pseudomonas aeruginosa PAO1 to MIC for Pseudomonas aeruginosa PAO7502016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1126762Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1256 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID496637Antibacterial activity against Streptococcus pneumoniae ATCC 49619 assessed as 90% mutant prevention concentration2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID533128Antimicrobial activity against Bacteroides caccae by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID425975Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 24 after 14 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1685385Potentiation of conjugate 10-induced antibacterial activity against wild type Pseudomonas aeruginosa PAO1 assessed as conjugate 10 MIC measured after 18 hrs by CLSI protocol based microbroth dilution method (Rvb = 64 to 128 ug/ml)2019MedChemComm, Apr-01, Volume: 10, Issue:4
Polybasic peptide-levofloxacin conjugates potentiate fluoroquinolones and other classes of antibiotics against multidrug-resistant Gram-negative bacteria.
AID562630Antimicrobial activity against Group G Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID533428Antimicrobial activity against Peptostreptococcus sp. assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID395715Antibacterial activity against Lactococcus lactis IL-1419 containing ORI23::qnr-cat promoter mutant by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID562622Antimicrobial activity against Coagulase-negative Staphylococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1272963Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by alamar blue assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.
AID1551291Antibacterial activity against Staphylococcus aureus KCTC209 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID425351Antibacterial activity against Streptococcus pneumoniae HMC 1147 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to gemifloxacin by 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID428848Time above the mutant prevention concentration in Streptococcus pneumoniae isolate SR-26137 infected human at 80 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID523148Antibacterial activity against Streptococcus pneumoniae isolate OC6585 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1152767Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase holoenzyme using pBR322 DNA as substrate assessed as linear DNA level at 0.02 to 11 uM after 60 mins by cleavable complex assay relative to control2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID322778Antimicrobial activity against Bacteroides vulgatus isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID425552Antibacterial activity against penicillin-, macrolide-susceptible and quinolone-resistant Streptococcus pneumoniae HMC 1074 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutat2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID584562Antimicrobial activity against Acinetobacter lwoffii isolate I expressing beta-lactamase OXA-58 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID543398AUC (24 hrs) in brain of Listeria monocytogenes EGD-e infected BALB/c mouse central nervous system listeriosis model at 50 mg/kg, ip administered 36 hrs postinfection as single dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID1266238Cytotoxicity against mouse RAW264.7 cells at 50 uM after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.
AID261738Antibacterial activity against Haemophilus influenzae type b ACH-00562006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID406845Antibacterial activity against Escherichia coli TOP10 containing pS1B plasmid expressing quinolone resistance determinant QnrS1 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID530371Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A, I85V, F96W and P101M mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
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
AID428816Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1391315Antifungal activity against Candida albicans 7535 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID533369Antimicrobial activity against Bacteroides vulgatus by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID533401Antimicrobial activity against Clostridium subterminale by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID575944Antimicrobial activity against erythromycin-resistant Streptococcus pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.
AID246828Efficacy against mice infected with MRSA-32 upon s.c. administration2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID558582Antimicrobial activity against penicillin-intermediate Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID428773Bactericidal activity against Streptococcus pneumoniae isolate SR-23958 assessed as mutant prevention concentration after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1743460Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Ala-90-Val/gyrB Glu-540-Val mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID428778Ratio of mutant prevention concentration for Streptococcus pneumoniae isolate SR-26134 to MIC for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID556026P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side at 50 uM in presence of in presence of 25 uM of p-glycoprotein and MRP transport inducer rifampin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID574975Antimicrobial activity against Actinomyces meyeri after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1243283Antimicrobial activity against Staphylococcus aureus ATCC 25923 by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID573825Antibacterial activity against beta-lactamase producing Clostridium tertium by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID728911Antibacterial activity against Chlamydophila pneumoniae AR39 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID574003Antibacterial activity against beta-lactamase producing Clostridium perfringens assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1601841Antibacterial activity against Staphylococcus aureus CMCC(B) 26003 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID574042Antibacterial activity against beta-lactamase producing Peptoniphilus asaccharolyticus assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID695443Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 2-FQR2M NY2746 expressing GyrA Ser84Leu mutant and GrlA Ser80Phe mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1164010Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 12-3 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID428805Ratio of Cmax in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-239582007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID368421Antimicrobial activity against Escherichia coli KAM32 pSTV28 containing chloramphenicol-resistant vector by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID51930K+ channel blocking activity in Chinese hamster ovary cells expressing HERG Kv11.12002Journal of medicinal chemistry, Aug-29, Volume: 45, Issue:18
Toward a pharmacophore for drugs inducing the long QT syndrome: insights from a CoMFA study of HERG K(+) channel blockers.
AID522954Antibacterial activity against methicillin-, ciprofloxacin-resistant Staphylococcus epidermidis by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID571105Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID573824Antibacterial activity against beta-lactamase producing Clostridium septicum by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID635060Antibacterial activity against methicillin-sensitive Staphylococcus aureus 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID456026Antibacterial activity against Staphylococcus aureus FDA 209-P after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID428818Ratio of AUC (0 to 24 hrs) in human at 80 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID422690Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3413 after 30 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID559385Antimicrobial activity against Clostridium difficile A422G harboring GyrA Thr82Ile and GyrB Leu451Phe mutant genes selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID593806Antimicrobial activity against quinilone-pencillin-resistant Staphylococcus epidermidis clinical isolate by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID425994Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3243 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID556770fAUC/MIC in osteomyelitis patient serum at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 0.19 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID528973Antimicrobial activity against methicillin-resistant Staphylococcus aureus assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1380669Fraction unbound in mouse plasma at 1 uM by equilibrium dialysis method2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID1398598Antibacterial activity against Haemophilus influenzae ATCC 49247 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID425074Antimicrobial activity against Escherichia coli DH10B in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID1187836Cytotoxicity against mouse RAW264.7 cells at 100 uM after 48 hrs by MTT assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID425359Antibacterial activity against Streptococcus pneumoniae HMC 1074 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425545Antibacterial activity against Streptococcus pneumoniae HMC 2527 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1256544Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID533635Antimicrobial activity against Propionibacterium sp. by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID523152Antibacterial activity against Streptococcus pneumoniae isolate OC6610 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1494120Antibacterial activity against Enterococcus faecalis NCTC 12697 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID521341Tmax in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID559541Antibacterial activity against ciprofloxacin-susceptible Pseudomonas aeruginosa assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559051Antibacterial activity against Staphylococcus lugdunensis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID406835Inhibition of Staphylococcus aureus wild-type topoisomerase 4 grlA S80F mutant decatenation activity assessed as unlinking of DNA microcircles from kinetoplast DNA2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID573592Antibacterial activity against Fusobacterium mortiferum by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID341391Toxicity in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit assessed as tissue valve damage median score at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose by histopathology2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID581076Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1179483Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35734 in 7H12 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID1294769Antibacterial activity against quinolone-resistant Streptococcus pneumoniae TPS3 after 18 to 24 hrs by broth microdilution method2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.
AID1242345Antimycobacterial activity against 1-(2-(4-((5-chloro-6-methylpyridin-3-yl)methylamino)piperidin-1-yl)ethyl)-7-fluoro-1,5-naphthyridin-2(1H)-one resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA D89N mutant incubated for 7 days by microdilu2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID523178Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC12501 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID574730Antimicrobial activity against Porphyromonas asaccharolytica after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID522957Antibacterial activity against Streptococcus sp. group C by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID574032Antibacterial activity against beta-lactamase producing Micromonas micros by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID261742Antibacterial activity against Klebsiella pneumoniae ATCC 138832006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID559159Antimicrobial activity against Clostridium difficile 630h harboring GyrB Asp26Val mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID535771Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60H carrying the luxAB gene under the hsp60 promoter agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID586744Antibacterial activity against qnrB gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrB1 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID558587Antimicrobial activity against Streptococcus pneumoniae 19A by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID586728Antibacterial activity against qnrB gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrB1 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID562458Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH369452009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1319016Inhibition of Pseudomonas aeruginosa DNA gyrase A assessed as inhibition of DNA supercoiling using PBR322 DNA as substrate after 30 mins by SYBR Gold staining based agarose gel electrophoresis2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1372636Antibiofilm activity against Mycobacterium tuberculosis H37Rv at 10 ug/ml after 1 week2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID1404053Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as change in bacterial burden in lungs at 30 mg/kg, po once daily for 8 days2018European journal of medicinal chemistry, Feb-10, Volume: 145In vivo potent BM635 analogue with improved drug-like properties.
AID285307Effect on 16 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID574492Antimicrobial activity against Bacteroides ovatus after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID586650Antibacterial activity against Escherichia coli ATCC 25922 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1188154Inhibition of Mycobacterium tuberculosis DNA gyrase supercoiling activity using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID524824Antibacterial activity against erythromycin resistant Campylobacter sp. by agar plate dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID695442Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 1-FQR2M BK2384 expressing GyrA Ser84Leu mutant and GrlA Ser80Phe mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID456030Antibacterial activity against Streptococcus mitis IID685 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID563337Induction of Cwp84 protease expression in Clostridium difficile CD196 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID574005Antibacterial activity against beta-lactamase producing Clostridium septicum assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID425967Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3274 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID562618Antimicrobial activity against Heterovancomycin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID574004Antibacterial activity against beta-lactamase producing Clostridium paraputrificum assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID278858Antiproliferative effect against MG63 cells assessed as BrdU incorporation into DNA after 48 hrs after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID285295Effect on 32 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID601786Antibacterial activity against 10'4 CFU Enterococcus faecium 06-7 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID570929Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID279271Antibacterial activity against azithromycin resistance selected Streptococcus pneumoniae 2527 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID341397Drug level in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit serum at 20 mg/kg, iv administered every 12 hrs measured 12 hrs after seventh dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID633629Antibacterial activity against methicillin-sensitive Staphylococcus aureus 10-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID571764Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring acrB::rpsLneo mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID601787Antibacterial activity against 10'4 CFU Escherichia coli ATCC 25922 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID522961Antibacterial activity against Moraxella catarrhalis by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID559518Antibacterial activity against Streptococcus constellatus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1909948Antibacterial activity against Staphylococcus aureus ATTC 25923 assessed as inhibition of bacterial growth measured after 8 days by Alamar blue reagent based broth microdilution method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID588212Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in rodents2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID581858Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559490Antibacterial activity against Propionibacterium acnes by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID573572Antibacterial activity against beta-lactamase producing Bacteroides uniformis by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID508386Antibacterial activity against macrolide-resistant Streptococcus pyogenes harboring erm(B) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID559065Antibacterial activity against Streptococcus mitis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425567Antibacterial activity against Streptococcus pneumoniae HMC 3041 after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID573394Antibacterial activity against Bacteroides fragilis by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID416841Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load per culture-positive foot-pad at 100 mg/kg, po administered for 5 days per week measured after 4 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1196883Inhibition of Mycobacterium tuberculosis AlaDH using L-alanine as substrate after 20 mins by spectrophotometry2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID531512Antibacterial activity against Bacteroides eggerthii assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID559507Antibacterial activity against Staphylococcus saprophyticus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1877408Antibacterial activity against Streptococcus pneumoniae ATCC 491692022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID523142Antibacterial activity against Streptococcus pneumoniae isolate OC7348 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID562632Antimicrobial activity against Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID275464Inhibition of human topoisomerase 2 by DNA cleavage assay2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID531527Antibacterial activity against Bacteroides vulgatus isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID425335Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID572517Antimicrobial activity against qnrS-positive Salmonella enterica serovar Braenderup isolate s2856 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID322782Antimicrobial activity against Bacteroides merdae isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID1610996Antibacterial activity against mid-exponential growth phase of methicillin-resistant Staphylococcus aureus ATCC 700699 assessed as increase in cell lysis at 25 uM2019Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria.
AID1264564Half-life in mouse at 2 mg/kg, iv by LC-MS/MS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID1163993Antibacterial activity against Klebsiella pneumoniae 12-2 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID559140Antimicrobial activity against Clostridium difficile A422g harboring GyrA Asp81Asn mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID322786Antimicrobial activity against Bacteroides thetaiotaomicron assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID428775Bactericidal activity against Streptococcus pneumoniae isolate SR-26137 ParC Ser79Phe assessed as mutant prevention concentration after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1877407Antibacterial activity against Pseudomonas aeruginosa 1432022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID553812Induction of cytotoxin production in Clostridium difficile PCR ribotype 001 in three-stage chemostat gut model at 43 mg/liter administered daily for 7 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID1154352Antimycobacterial activity against TMC207R-resistant Mycobacterium tuberculosis clone 8.1 over expressing DprE1 mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1381413Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as log reduction in bacterial load in lungs at 30 mg/kg, po for 8 consecutive days starting from day 1 post infection measured on day 9 post last dose2018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
AID515920Antibacterial activity against kanamycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID1601851Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 43300 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID1179479Antimycobacterial activity against Mycobacterium chelonae ATCC 35752 in 7H9 medium after 3 days and 4 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID279284Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79Y and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID323871Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae UAB1 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1154350Antimycobacterial activity against Mycobacterium tuberculosis over expressing PimA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID563331Upregulation of slpA gene expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID559509Antibacterial activity against Streptococcus agalactiae assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID573599Antibacterial activity against Fusobacterium nucleatum assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID522987Antibacterial activity against Streptococcus pneumoniae isolate OC5462 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID523172Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11223 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID342253Drug level in Clostridium difficile infected CF1 mouse stool at 0.2 mg/day for 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID553803Antimicrobial activity against Clostridium difficile PCR ribotype 027 after 48 hrs2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID484795Antibacterial activity against Staphylococcus aureus SA-K1904 bearing norA++ efficient mutation by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID559202Antibacterial activity against Streptococcus pneumoniae S003 harboring wild-type parC and gyrA Ser81Phe mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID570922Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID406813Antibacterial activity against Staphylococcus aureus ACH-0231 isolate with gyrA Ser84Leu, Glu88Lys and grlA Ser80Tyr, Glu84Gly mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID544858Antibacterial activity against Streptococcus pneumoniae H548 clinical isolate harboring gyrA Ser81Phe mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID574764Antimicrobial activity against Finegoldia magna after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1154547Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 Rv1937/F426C mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID279293Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1264560Antibacterial activity against Streptococcus pneumoniae 402 infected in sc dosed mouse assessed as reduction in 2 log CFU in lung compound administered as BID for 1 day measured 24 hrs after last dose2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID531528Antibacterial activity against Bacteroides caccae isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID562944Upregulation of fbp68 gene expression in Clostridium difficile CD196 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID576326Antibacterial activity against 10'4 to 10'5 CFU methicillin-susceptible Staphylococcus aureus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID559071Antibacterial activity against Acinetobacter lwoffii by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID279837Reduction of Mycobacterium tuberculosis H37Rv in orally dosed BALB/c mouse lung2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID559066Antibacterial activity against Streptococcus oralis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID562636Antimicrobial activity against Listeria monocytogenes by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID520366Ratio of AUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID278857Inhibition of metabolic activity in primary human osteoblasts assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID518620Antimicrobial activity against intracellular Mycobacterium avium subsp. hominissuis ATCC 700898 after 7 days by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID570673Antibacterial activity against Enterobacteriaceae by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID540215Volume of distribution at steady state in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID573551Antibacterial activity against Bacteroides fragilis assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1494124Antibacterial activity against Norfloxacin-resistant Staphylococcus aureus 1199B over-expressing NorA after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID245237Minimum inhibitory concentration against vancomycin-resistant Staphylococcus aureus (Hershey)2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID522993Antibacterial activity against Streptococcus pneumoniae isolate OC7376 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID765272Cmax/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1514448Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID1652708Induction of Escherichia coli K12 MG1655 recN promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID342256Effect on growth of fluoroquinolone-resistant epidemic Clostridium difficile NAP1 in CF1 mouse assessed as increase in bacterial density in cecal content at 2.0 mg/day, sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID283162Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2622 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID369965AUC (0 to 24 hrs) in human serum at 400 mg, po administered as single dose2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID558607Antimicrobial activity against Streptococcus pneumoniae isolate 1384 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID285296Susceptibility of penicillin-resistant Streptococcus pneumoniae 217 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID531523Antibacterial activity against Bacteroides eggerthii isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID559410Antimicrobial activity against Clostridium difficile BI2E harboring GyrB Glu466Lys mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID571339Antibacterial activity against Enterococcus faecium assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559510Antibacterial activity against Lancefield Streptococcus sp. 'group C' assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558893Antimicrobial activity against Clostridium difficile C253h harboring GyrA Ala118Ser mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1207286Inhibition of long-lasting type calcium current (ICaL) in HEK293 cells (alpha1C/beta2a/alpha2delta1) cells measured using IonWorks Barracuda automated patch clamp platform
AID532960Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 42010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID572523Antimicrobial activity against qnrS-positive Salmonella enterica serovar Corvallis isolate s2052 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID581478Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID518799Antimycobacterial activity against Mycobacterium fortuitum after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID558630Antimicrobial activity against Streptococcus pneumoniae isolate 4747 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1393792Antibacterial activity against multidrug resistant Mycobacterium tuberculosis ATTC 27294 by Alamar Blue assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID496649Antibacterial activity against Streptococcus pneumoniae 1151 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID570802Apparent oral clearance in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID533125Antimicrobial activity against Bacteroides distasonis by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID565312Antibacterial activity against Mycoplasma genitalium R32 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID586632Antibacterial activity against qnrB gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrB1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID243188Inhibition of human voltage-gated potassium channel subunit Kv11.1 (ERG K+ channel) in open state2005Bioorganic & medicinal chemistry letters, Mar-15, Volume: 15, Issue:6
A two-state homology model of the hERG K+ channel: application to ligand binding.
AID428799Ratio of AUC (0 to 24 hrs) in human at 80 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID531511Antibacterial activity against Bacteroides merdae assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID571127Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID562660Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH375032009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID574589Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 obtained from pus of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID562635Antimicrobial activity against Corynebacterium spp. assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID558592Antimicrobial activity against Streptococcus pneumoniae 4 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID574766Antimicrobial activity against Finegoldia magna assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID584555Antimicrobial activity against Acinetobacter lwoffii isolate B expressing beta-lactamase OXA-164 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID243151Inhibitory concentration against potassium channel HERG2005Bioorganic & medicinal chemistry letters, Jun-02, Volume: 15, Issue:11
A discriminant model constructed by the support vector machine method for HERG potassium channel inhibitors.
AID593804Antimicrobial activity against quinilone-pencillin-resistant Staphylococcus aureus isolate SAR 4790 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID1237416Bactericidal activity against Escherichia coli KCTC 1924 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1348982Elimination half life in ICR mouse at 50 mg/kg, po by HPLC analysis
AID1877418Antibacterial activity against Neisseria gonorrhoeae WHO C2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID521343Cmin in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID368424Ratio of MIC for Escherichia coli KAM32 pSTVqepA mutant to MIC for Escherichia coli KAM32 pSTV28 mutant2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID559260Antibacterial activity against non-ciprofloxacin-susceptible Pseudomonas aeruginosa by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID586644Antibacterial activity against qnrB gene expressing Escherichia coli ATCC 25922 harboring ParC S80R mutant, ParC S80R mutant and pBK-QnrB1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1743461Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Asp-94-Gly/gyrB Asp-500-Asn mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID533381Antimicrobial activity against Bacteroides nordii by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID575099Antimicrobial activity against Streptococcus pneumoniae serotype 15A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1237424Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID581481Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563101Upregulation of fbp68 gene expression in Clostridium difficile CD196 M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID571368Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID562824Antimycobacterial activity against Mycobacterium tuberculosis 00-0715 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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).
AID1740319Antimicrobial activity against Escherichia coli NCTC 11954 producing penicillinase assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID1256552Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1861192Antimycobacterial activity against drug-sensitive Mycobacterium tuberculosis assessed as mycobacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID595855Inhibition of wild-type Staphylococcus aureus topoisomerase 4-mediated decatenation of kDNA after 30 mins by gel electrophoresis assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID1207346Inhibition of fast sodium current (INa) in HEK293 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID341392Toxicity in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit assessed as inflammatory cell infiltration median score at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose by histopathology2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID405462Antibacterial activity against Escherichia coli TOP10 in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID733007Inhibition of Mycobacterium leprae DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 2 hrs at 30 degC by ethidium bromide based gel electrophoresis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID286043Susceptibility of Streptococcus pneumoniae ATCC 49619 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID571352Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID278432Antibacterial activity against Streptococcus pyogenes M12 by time-kill curve assay2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Semimechanistic pharmacokinetic/pharmacodynamic model for assessment of activity of antibacterial agents from time-kill curve experiments.
AID518797Antimycobacterial activity against quinolone-resistant multidrug-resistant Mycobacterium tuberculosis after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID601790Antibacterial activity against 10'4 CFU Klebsiella pneumoniae 09-23 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1163991Antibacterial activity against extended-spectrum beta-lactamase producing Escherichia coli 12-15 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID558609Antimicrobial activity against Streptococcus pneumoniae isolate 1397 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID511386Antibacterial activity against ciprofloxacin resistant Escherichia coli by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID570804Ratio of AUC (0 to 24 hrs ) in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose to AUC (0 to 24 hrs ) in healthy human at 400 mg, po qd measured on2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID580907Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559536Antibacterial activity against Moraxella catarrhalis assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID586726Antibacterial activity against Escherichia coli ATCC 25922 harboring GyrA S83L mutant assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID286082fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 50 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID581105Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1330192Antibacterial activity against Pseudomonas aeruginosa 2742 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID484794Antibacterial activity against Staphylococcus aureus ATCC 25923 by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID425339Antibacterial activity against azithromycin-resistant Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID581108Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID556782Ratio of drug level in cancellous bone to serum in osteomyelitis patient at 400 mg, po administered for every 24 hrs by MAP-Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID580883Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559074Antibacterial activity against Enterobacter aerogenes by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID590141Antitubercular activity against Mycobacterium tuberculosis H37Rv by LORA assay2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents.
AID1465261Antibacterial activity against multidrug resistant Staphylococcus aureus by broth microdilution assay
AID635058Antibacterial activity against methicillin-resistant Staphylococcus aureus 10-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1318917Antibacterial activity against Klebsiella pneumoniae ATCC 13883 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID428854Bactericidal activity against Streptococcus pneumoniae isolate SR-23958 assessed as reduction in number of viable cells under condition simulating oral administration of 400 mg once daily2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID580905Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID511302Antibacterial activity against methicillin susceptible Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID595933Inhibition of Staphylococcus aureus topoisomerase 4 Ser80Phe mutant-mediated decatenation of kDNA after 30 mins by gel electrophoresis assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID559052Antibacterial activity against Staphylococcus saprophyticus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1163988Antibacterial activity against extended-spectrum beta-lactamase producing Escherichia coli 12-2 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID574752Antimicrobial activity against Anaerococcus prevotii after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID581072Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1185139Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 272942014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID1075024Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as reduction of bacterial CFU in lung at 30 mg/kg, po administered for 8 days measured 24 hrs post last dose relative to control2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.
AID283390Antimicrobial activity against Nocardia cyriacigeorgica after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID425803Cmax in human at 400 mg, po2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID1743452Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in human macrophages assessed as intracellular bacterial load at 0.5 MIC measured after 6 days (Rvb = 5.57 to 6.43 logCFU/ml)2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID405466Antibacterial activity against Escherichia coli TOP10 containing pIP1206 plasmid in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1437920Antibacterial activity against vancomycin-resistant Enterococcus faecalis ATCC 51299 by broth microdilution method2017Journal of natural products, 01-27, Volume: 80, Issue:1
Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.
AID574948Antimicrobial activity against Streptococcus pneumoniae serotype 19A by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID511390Antibacterial activity against Proteus mirabilis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID544868Antibacterial activity against Streptococcus pneumoniae U2A1414 harboring gyrA Glu85Lys parC Ser79Phe mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID570806Ratio of Tmax in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose to Tmax in healthy human at 400 mg, po qd measured on day 62008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID593813Antimicrobial activity against Saccharomyces cerevisiae ATCC 9763 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID584565Antimicrobial activity against Acinetobacter lwoffii isolate L expressing beta-lactamase OXA-58 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID575076Antimicrobial activity against Streptococcus pneumoniae serotype 19A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID406623Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae isolates assessed as percent resistant isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.
AID518628Ratio of AUC (0 to 24 hrs) in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic model to MIC for Mycobacterium avium at 80% maximal effective concentration2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID521334Cmax in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID595858Antibacterial activity against Escherichia coli ATCC25922 after 24 hrs by microdilution method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID559171Antimicrobial activity against Clostridium difficile BI2e harboring GyrB Arg447Lys and Asp426Asn mutant gene selected after 32 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID422665Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1077 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID406646Antibacterial activity against Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID508369Antibacterial activity against Streptococcus pneumoniae harboring erm(B) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID508379Antibacterial activity against macrolide-resistant Streptococcus pneumoniae harboring erm(B) and mef(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID406806Antibacterial activity against Staphylococcus aureus ACH-0201 isolate with gyrA Ser84Leu, Glu88Val and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID1297323Antibacterial activity against extended-spectrum beta-lactamase-producing Klebsiella pneumoniae 14-18 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID523293Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as 2 log reduction in bacterial burden in lungs orally treated in water-20% captisol upto 8 days2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID1430297Antibacterial activity against Listeria monocytogenes ATCC 7644 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID581104Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID523154Antibacterial activity against Streptococcus pneumoniae isolate OC6610 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID544295Antibacterial activity against vancomycin-intermediate Staphylococcus aureus after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID559484Antibacterial activity against non-levofloxacin susceptible Stenotrophomonas maltophilia by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID576136Antibacterial activity against 10'4 to 10'5 CFU Enterococcus faecalis after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID562931Antimicrobial activity against Clostridium difficile 6269 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID425978Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 24 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1256563Antibacterial activity against Enterococcus faecalis 14-1 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID422683Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 37 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID559053Antibacterial activity against Staphylococcus warneri by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1819732Antimycobacterial activity against Mycobacterium abscessus K21 assessed as inhibition of mycobacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID511385Antibacterial activity against vancomycin resistant Enterococcus faecium by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID581297Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID544854Antibacterial activity against Streptococcus pneumoniae U2A1686 harboring gyrA Glu85Lys mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID565291Antimicrobial activity against Mycoplasma hominis by agar dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activity of a new quinoline derivative, ER-2, against clinical isolates of Mycoplasma pneumoniae and Mycoplasma hominis.
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).
AID369980Antibacterial activity against ciprofloxacin and methicillin-resistant Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID695450Inhibition of human ERG expressed in mammalian cells at 10 uM by patch clamp method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID322777Antimicrobial activity against Bacteroides uniformis isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID518622Antimicrobial activity against Mycobacterium avium subsp. hominissuis ATCC 700898 infected in human THP1 cells in presence of 10% FBS2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID323877Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae 1132 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1868111Cytotoxicity against mouse J774.A1 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID422672Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3009 after 19 passages with moxifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID425580Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene and I460V, D435N mutation in QRDR of ParE g2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1256535Antibacterial activity against Escherichia coli 14-1 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID581071Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID581277Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1750826Plasma protein binding in CD1 mouse at 10 uM after 4 hrs by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID571763Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-F628F mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID633638Antibacterial activity against Streptococcus pneumoniae 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID570988Tmax in healthy human assessed as 25-desacetyl-rifapentine level at 900 mg, po thrice weekly measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID584556Antimicrobial activity against Acinetobacter lwoffii isolate C expressing beta-lactamase OXA-164 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID425969Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 2527 after 20 passages with azithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID556196P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side at 50 uM2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID563033Antimycobacterial activity against Mycobacterium tuberculosis 08-0762 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID341394Toxicity in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit assessed as fibrous content median score at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose by histopathology2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID542549Antimicrobial activity against Nocardia brasiliensis HUJEG-1 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Efficacy of ciprofloxacin and moxifloxacin against Nocardia brasiliensis in vitro and in an experimental model of actinomycetoma in BALB/c mice.
AID574500Antimicrobial activity against Bacteroides thetaiotaomicron assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID573601Antibacterial activity against Fusobacterium necrophorum assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1600110Bactericidal activity against Proteus vulgaris NCTC 4635 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1164012Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 12-8 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID425808Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung measured after 28 days of aerosol infection run2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID584111Bacteriostatic activity against Escherichia coli K-12 DM41002010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID563334Upregulation of slpA gene expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID342257Effect on growth of fluoroquinolone-susceptible epidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content dosed sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID580890Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID601704Antibacterial activity against 10'4 CFU methicillin-sensitive Staphylococcus aureus 08-1 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1512393Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as reduction in bacterial load in lungs at 30 mg/kg administered once daily starting from 5 days post infection for 4 consecutive days and measured on day 2019ACS medicinal chemistry letters, Oct-10, Volume: 10, Issue:10
Novel Pyrazole-Containing Compounds Active against
AID511389Antibacterial activity against Enterobacter cloacae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID563227Antimycobacterial activity against Mycobacterium tuberculosis 08-0782 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID283171Decrease in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID728925Antibacterial activity against levofloxacin-resistant and methicillin-resistant Staphylococcus aureus 870307 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID559152Antimicrobial activity against Clostridium difficile 630d selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID533131Antimicrobial activity against Bacteroides fragilis by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1909949Antibacterial activity against Escherichia coli ATTC 25922 assessed as inhibition of bacterial growth measured after 8 days by Alamar blue reagent based broth microdilution method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID571340Antibacterial activity against Enterococcus faecium assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1318913Antibacterial activity against gentamicin-resistant Pseudomonas aeruginosa isolate CAN-ICU 62308 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1868118Anti-tubercular activity against Mycobacterium tuberculosis CF152 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID1398597Antibacterial activity against Klebsiella pneumoniae TYPE 1 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID518804Antimycobacterial activity against Mycobacterium abscessus after 3 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID530390Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA M74I and A83S mutant/GyrB R447K mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID249969Ratio of MPC to MIC against methicillin resistant Staphylococcus aureus-332005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID286050Peak free concentration at 50 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285283Effect on 16 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID523317Antibacterial activity against Streptococcus pneumoniae OC7453 harboring gyrA S81F mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID574987Antimicrobial activity against Bifidobacterium adolescentis after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID635057Antibacterial activity against methicillin-resistant Staphylococcus aureus 10-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1194330Inhibition of Mycobacterium smegmatis GyrB ATPase activity expressed in Escherichia coli BL21 (DE3) pLysS cells after 100 mins by inorganic phosphate release detection based malachite green reagent assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID565326Antibacterial activity against Mycoplasma genitalium M6090 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID508376Antibacterial activity against quinolone-resistant Streptococcus pneumoniae after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID544846Antibacterial activity against Streptococcus pneumoniae R6 Tr10 harboring gyrA Ser81Tyr parC Ser79Tyr mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID559077Antibacterial activity against non-ciprofloxacin-susceptible Haemophilus influenzae by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1691029Antibiofilm activity against Mycobacterium tuberculosis assessed as log reduction in bacterial growth at 10 uM measured after 1 week relative to control2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID562448Antibacterial activity against Staphylococcus aureus SMH36945 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID574952Antimicrobial activity against Streptococcus pneumoniae serotype 11A by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID559381Antimicrobial activity against Clostridium difficile A422F harboring GyrB Leu451Phe mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID581663Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level per mg of protein at up to 10'5 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1154544Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 C387S mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID558930Antimicrobial activity against Clostridium difficile A422f selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID322776Antimicrobial activity against Bacteroides thetaiotaomicron isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID428783Cmax in human at 80 mg, po administered once a day2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID533365Antimicrobial activity against Bacteroides uniformis by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID530599Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr11 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID522962Antibacterial activity against ciprofloxacin-susceptible, -intermediate Escherichia coli by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1079934Highest frequency of acute liver toxicity observed during clinical trials, expressed as a percentage. [column '% AIGUE' in source]
AID285972Antimicrobial susceptibility against Haemophilus influenzae D3 isolate with GyrA Ser84Tyr, ParC Glu88Lys and AcrR Leu31His, Ile121Val and Gln134Lys mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID559060Antibacterial activity against Streptococcus pyogenes by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID574484Antimicrobial activity against Bacteroides thetaiotaomicron after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID341373Antibacterial activity against Staphylococcus aureus by manual microdilution technique2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID69597Antibacterial activity was evaluated against Escherichia coli2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID559497Antibacterial activity against vancomycin- resistant Enterococcus faecalis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID531857Tmax in tuberculosis patient at 400 mg/day, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID576135Antibacterial activity against 10'4 to 10'5 CFU Enterococcus faecium after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID368420Antimicrobial activity against Escherichia coli KAM32 pHPA containing mutated GyrA gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID522979Antibacterial activity against Streptococcus pneumoniae isolate OC7189 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581288Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563221Antimycobacterial activity against Mycobacterium tuberculosis 08-0762 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID286077fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 100 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID405117Antimicrobial activity against Escherichia coli TOP10 harbouring pVS2 expressing quinolone resistant Vibrio splendidus LGP32 QnrVS2 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID575084Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 6B assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID508375Antibacterial activity against quinolone-susceptible Streptococcus pneumoniae after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID522997Antibacterial activity against Streptococcus pneumoniae isolate OC6790 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID533372Antimicrobial activity against Bacteroides vulgatus assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID558589Antimicrobial activity against Streptococcus pneumoniae 1 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID531525Antibacterial activity against Bacteroides ovatus isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID522956Antibacterial activity against Streptococcus agalactiae by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID278861Inhibition of metabolic activity in HeLa cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID559534Antibacterial activity against Klebsiella pneumoniae assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID279264Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3676 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID565315Antibacterial activity against Mycoplasma genitalium TW48-5G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID581082Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1909950Antibacterial activity against wild type Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth incubated for 11 days2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID544293Antibacterial activity against community acquired methicillin-resistant Staphylococcus aureus after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID556780Apparent intercompartmental clearance in osteomyelitis patient at 400 mg, po administered for every 24 hrs by three stage hierarchical Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID422684Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 37 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1243284Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolates by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID565317Antibacterial activity against Mycoplasma genitalium M2282 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1750815Selectivity index, ratio of MIC for Fluoroquinolone-resistant Staphylococcus aureus ATCC 49951 to MIC for Fluoroquinolone-sensitive Staphylococcus aureus ATCC 499512021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID563032Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0746 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID522950Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID372985Antimycobacterial activity against Mycobacterium avium JATA51-01 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID286094fAUC/MIC ratio of Staphylococcus aureus BSP-2443 at 50 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID556768fAUC/MIC in osteomyelitis patient cortical bone at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 0.5 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID405460Antibacterial activity against Escherichia coli C600Rif containing pIP1206 plasmid in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID576138Antibacterial activity against 10'4 to 10'5 CFU methicillin-resistant coagulase-negative Staphylococcus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID574770Antimicrobial activity against Clostridium perfringens after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID522985Antibacterial activity against Streptococcus pneumoniae isolate OC6608 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID559063Antibacterial activity against Streptococcus constellatus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID533397Antimicrobial activity against Clostridium paraputrificum by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID428291Antimicrobial activity against Acinetobacter baumannii BM4652 expressing adeABC adeIJK double mutant isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID285533Antibacterial activity against ethidium bromide-resistant Staphylococcus aureus BSA678 after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID1154353Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis clone 4.1 over expressing DprE1 mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID1297320Antibacterial activity against Escherichia coli 14-1 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1557286Antibacterial activity against Streptococcus pyogenes by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID556192Apparent passive permeability across human Calu3 cells at 350 ug/ml2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1297331Antibacterial activity against Pseudomonas aeruginosa 14-14 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1380643Antibacterial activity against wild type Escherichia coli ATCC 25922 by CLSI M100-S17 protocol based method2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID581490Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID573784Antibacterial activity against Prevotella bivia by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1348986Antimycobacterial activity against isoniazid/rifampicin/ethambutol-resistant Mycobacterium tuberculosis after 3 days by rapid direct susceptibility test
AID279828AUC(0-infinity) in BALB/c mouse at 6 to 400 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID406832Inhibition of Staphylococcus aureus wild-type DNA gyrase supercoiling activity assessed as effect on conversion of relaxed pBR322 DNA to supercoiled form2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID1600109Antibacterial activity against Proteus vulgaris NCTC 4635 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID574504Antimicrobial activity against Bacteroides caccae assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID559487Antibacterial activity against Fusobacterium sp. by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559083Antibacterial activity against Neisseria meningitidis by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1393811Antitubercular activity against replicating Mycobacterium tuberculosis H37Rv by Alamar Blue assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID456045Antibacterial activity against vancomycin-resistant Enterococcus faecalis after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID1403711Antimycobacterial activity against Mycobacterium tuberculosis H37Rv dormant stage assessed as log reduction in bacterial load at 10 ug/ml incubated for 7 days2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID484791Antibacterial activity against Staphylococcus aureus SA-K1902 bearing norA- deficient mutation by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID633744Antibacterial activity against Pseudomonas aeruginosa 10-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID522946Antibacterial activity against Streptococcus pneumoniae ATCC 49619 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID428857Bactericidal activity against Streptococcus pneumoniae ATCC 49619 assessed as prevention of bacterial regrowth under condition simulating oral administration of 400 mg once daily after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID511397Antibacterial activity against Acinetobacter baumannii by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID544849Antibacterial activity against Streptococcus pneumoniae U2A1414 harboring gyrA Glu85Lys parC Ser79Phe mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID522968Antibacterial activity against Proteus mirabilis by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID424333Antimicrobial activity against Dialister propionicifaciens assessed as susceptibility breakpoint by CLSI-M11-A7 method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID558614Antimicrobial activity against Streptococcus pneumoniae isolate 2688 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID533413Antimicrobial activity against Peptoniphilus asaccharolyticus by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID574954Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19A by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
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.
AID1243289Antimicrobial activity against Staphylococcus epidermidis ATCC 12228 by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID425542Antibacterial activity against Streptococcus pneumoniae HMC 1139 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1297340Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-5 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID759328Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID342064Antimicrobial activity against epidemic Clostridium difficile BI9 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID498191Antibacterial activity against Stenotrophomonas maltophilia MBS101 containing plasmid encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID574726Antimicrobial activity against Prevotella oralis assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID563208Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-0319 harboring gyrA Asp94Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID581491Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID508382Antibacterial activity against Streptococcus pyogenes harboring erm(B) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID279244Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3676 with GyrA E85G, GyrB S478I and ParC S79Y mutation after 50 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID528848Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID728903Plasma protein binding in human at 5 ug/mL by ultrafiltration method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID244977Antibacterial activity against Klebsiella pneumoniae type II was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID1330190Antibacterial activity against Escherichia coli 1356 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID1126759Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 821 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1254076Antifungal activity against Candida albicans 7535 by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1551290Antibacterial activity against Staphylococcus aureus RN4220 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID577487Antimicrobial activity against methicillin-susceptible Staphylococcus aureus SH1000 assessed as inhibition of bacterial biofilm formation by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID406810Antibacterial activity against Staphylococcus aureus ATCC 700699 isolate with gyrA Ser84Leu, Glu409Lys and grlA Ser80Phe mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID531719Antibacterial activity against Bacteroides fragilis isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID573563Antibacterial activity against beta-lactamase producing Bacteroides vulgatus by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID559245Antibacterial activity against Streptococcus pneumoniae D002 harboring parC Ser79Phe and gyrA Ser81Phe mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID341077Plasma concentration in human with MDR1 3435 CC genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID576137Antibacterial activity against 10'4 to 10'5 CFU Streptococcus pyogenes after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID562661Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH380022009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID580862Cmax in patients with pulmonary tuberculosis at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1256567Antibacterial activity against Enterococcus faecium 14-5 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID562614Antimicrobial activity against methicillin-sensitive Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID563040Antimycobacterial activity against Mycobacterium tuberculosis 08-0789 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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).
AID1297318Antibacterial activity against extended-spectrum beta-lactamase-producing Escherichia coli 14-1 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID520381Antimicrobial activity against Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID532975Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 192010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID499771Antimicrobial activity against quinolone and penicillin-resistant Pseudomonas aeruginosa after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID533412Antimicrobial activity against Finegoldia magna assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID422667Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1076 after 14 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID428844Time above the mutant prevention concentration in Streptococcus pneumoniae isolate SR-23958 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID553689Antimicrobial activity against Clostridium in three-stage chemostat gut model assessed as log reduction in bacterial count at 43 mg/liter administered daily for 7 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID576140Antibacterial activity against 10'4 to 10'5 CFU methicillin-susceptible coagulase-negative Staphylococcus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID245138Minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus-332005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID523180Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC8530 harboring gyrA S84L and parC I143V mutant gene assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID675093Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis clinical isolate after 18-24 hrs by two-fold serial dilution method2012European journal of medicinal chemistry, Sep, Volume: 55Synthesis and in vitro antibacterial activity of gemifloxacin derivatives containing a substituted benzyloxime moiety.
AID1494125Antibacterial activity against erythromycin-resistant Staphylococcus aureus RN4220 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID1600104Bactericidal activity against Bacillus subtilis ATCC 6633 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1890605Antibacterial activity against methicillin resistant Staphylococcus aureus 5076 harbouring DNA gyrase and topoisomerase IV mutant and efflux pump assessed as inhibition of bacterial growth incubated for 18 hrs in presence of efflux inhibitor by CLSI based2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID522963Antibacterial activity against ciprofloxacin-resistant Escherichia coli by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID428824Ratio of Cmax in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID571132Antibacterial activity against penicillin-resistant Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID556761fAUC/MIC in osteomyelitis patient cortical bone at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 0.25 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID559068Antibacterial activity against Streptococcus sanguinis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID522971Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1430294Antibacterial activity against Klebsiella pneumoniae ATCC 700603 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID442254Antimalarial activity against Plasmodium falciparum 3D72009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.
AID341076AUC (0 to 24 hrs) in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID522999Antibacterial activity against Streptococcus pneumoniae isolate OC6790 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID559045Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus aureus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1243287Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae clinical isolates by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID1557281Antibacterial activity against Klebsiella by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID574811Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis H37Rv by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID633644Antibacterial activity against Enterococcus faecalis 09-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID561327Antimicrobial activity against Klebsiella pneumoniae isolate 202 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID563224Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0777 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559072Antibacterial activity against Citrobacter freundii by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID728922Antibacterial activity against quinolone, penicillin-resistant Streptococcus pneumoniae 104835 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID531630Antimicrobial activity against Ureaplasma urealyticum by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID570691Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID571126Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID425345Antibacterial activity against Streptococcus pneumoniae HMC 1060 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID544857Antibacterial activity against Streptococcus pneumoniae U2A1266 harboring gyrA Ser81Cys mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID494417Cytotoxicity against african green monkey Vero cells after 72 hrs by MTT assay2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.
AID533417Antimicrobial activity against Micromonas micros by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID518059Toxicity in healthy human assessed as dizziness at 400 mg/kg, po administered as single dose2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID286065Half life at 75 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID765269fT>MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID562455Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH380042009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID633743Antibacterial activity against Pseudomonas aeruginosa 10-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID428774Bactericidal activity against Streptococcus pneumoniae isolate SR-26134 assessed as mutant prevention concentration after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID532685Antimicrobial activity against ciprofloxacin-nonsusceptible, BT PFGE pattern, emm28 type Streptococcus pyogenes with ST52 sequence type, ParC D83G mutant isolated from skin/soft tissue infection2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID456044Antibacterial activity against penicillin-intermediate resistant Streptococcus pneumoniae after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID1318918Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 1000362016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID543394Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as log reduction in bacterial CFU in brain at 50 mg/kg, ip administered 36 hrs postinfection as single dose measured within 1 hr2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID392220Antibacterial activity against Lactococcus lactis IL-1419 containing ORI23 promoter by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID586743Antibacterial activity against qnrA gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrA1 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1297337Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-3 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID565329Antibacterial activity against Mycoplasma genitalium M6283 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1079945Animal toxicity known. [column 'TOXIC' in source]
AID572519Antimicrobial activity against qnrS-positive Salmonella enterica serovar Typhimurium isolate s2425 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID574768Antimicrobial activity against Finegoldia magna assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID406833Inhibition of Staphylococcus aureus DNA gyrase gyrA S84L mutant supercoiling activity assessed as effect on conversion of relaxed pBR322 DNA to supercoiled form2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID553809Drug level in human feces2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID563024Antimycobacterial activity against Mycobacterium tuberculosis 08-0745 harboring gyrA Asp89Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID562444Antibacterial activity against Staphylococcus aureus SMH38002 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID499681Antimicrobial activity against Pseudomonas aeruginosa ATCC 9027 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID531633Bactericidal activity against Mycoplasma pneumoniae at MIC after 48 hrs2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID559079Antibacterial activity against Klebsiella pneumoniae by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID586642Antibacterial activity against Escherichia coli ATCC 25922 harboring GyrA S83L mutant and ParC S80R mutant by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID563213Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-1234 harboring gyrA Asn533Thr gyrB mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID521335Cmax in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID571849Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID531726Antibacterial activity against Bacteroides fragilis assessed as percent resistant isolates2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1600100Bactericidal activity against Staphylococcus epidermidis ATCC 14990 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID530374Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA S69V, A71G, E72D, T73V, M74I, N76K, A83S, S84A, I85V, F96W and P101M mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID544304Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS5 harboring GyrA S84L, E88K and GrlA S80F, E84G mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID574050Antibacterial activity against beta-lactamase producing Finegoldia magna by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID283163Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2639 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID544859Antibacterial activity against Streptococcus pneumoniae R6 Tr1 harboring parC Ser79Tyr mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID574758Antimicrobial activity against Peptoniphilus asaccharolyticus after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID781330pKa (acid-base dissociation constant) as determined by potentiometric titration2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1163999Antibacterial activity against Pseudomonas aeruginosa 12-12 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID581662Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU after 72 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1685386Potentiation of conjugate 11-induced antibacterial activity against wild type Pseudomonas aeruginosa PAO1 assessed as conjugate 11 MIC measured after 18 hrs by CLSI protocol based microbroth dilution method (Rvb = 64 to 128 ug/ml)2019MedChemComm, Apr-01, Volume: 10, Issue:4
Polybasic peptide-levofloxacin conjugates potentiate fluoroquinolones and other classes of antibiotics against multidrug-resistant Gram-negative bacteria.
AID208611Antibacterial activity was determined against clinically isolated penicillin resistant Streptococcus pneumoniae (PRSP) strains (50 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID369969AUC (0 to 24 hrs) in Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID511384Antibacterial activity against Enterococcus faecium by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID559483Antibacterial activity against Serratia marcescens by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1154543Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 OE mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1364755Antibacterial activity against Mycobacterium marinum ATCC BAA-535 infected in Zebra fish assessed as log reduction in bacterial counts at 10 mg/kg, po administered for 7 days by MPN assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID520365Ratio of AUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID562649Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH373902009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID573552Antibacterial activity against Bacteroides fragilis assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID461171Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate Alamar blue assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
AID522949Antibacterial activity against methicillin-susceptible Staphylococcus aureus by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID565324Antibacterial activity against Mycoplasma genitalium M6286 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID544303Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS3 harboring GyrA S84L and GrlA S80F, E84K mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID559056Antibacterial activity against Lancefield Streptococcus sp. group F by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1181171Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_16.5 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1272956Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of DNA supercoiling after 30 mins by electrophoresis2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.
AID523316Antibacterial activity against Streptococcus pneumoniae OC7452 harboring parC S79Y mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID580760Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1164004Antibacterial activity against methicillin-sensitive Staphylococcus aureus 12-4 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID283172Effect on biofilm formation of Staphylococcus lugdunensis assessed as percent non-biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID484801Antibacterial activity against Staphylococcus aureus K1628 bearing S84L mutant GyrA and S80F mutant GrlA by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID1557280Antibacterial activity against Pseudomonas aeruginosa by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID563055Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0744 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID373140Antimycobacterial activity against Mycobacterium avium complex N084 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID511387Antibacterial activity against ciprofloxacin susceptible Escherichia coli by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID1237429Bactericidal activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID570793Cmax in healthy human at 400 mg, po qd measured on day 4 by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID530370Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A and I85V mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID286051Peak free concentration at 75 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID528972Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID425560Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1318934Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 806212016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID341075AUC (0 to 24 hrs) in human with MDR1 3435 CC genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID341079Plasma concentration in human with MDR1 3435 CC genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID522948Antibacterial activity against Staphylococcus aureus ATCC 29213 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID532681Antimicrobial activity against ciprofloxacin-nonsusceptible, AD PFGE pattern, emm89 type Streptococcus pyogenes with ST382 sequence type, ParC S79A mutant isolated from oropharyngeal colonization2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID405121Antimicrobial activity against Escherichia coli TOP102007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID433578Inhibition of Mycobacterium leprae wild type DNA gyrase subunit A G89A mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1126742Antibacterial activity against 1 ug/ml Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID586641Antibacterial activity against Escherichia coli ATCC 25922 harboring GyrA S83L mutant by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID430963Antibacterial activity against Escherichia coli 1608 containing gyrA L83, L87 mutants assessed as increase in MIC by Etest relative to MIC for wild type Escherichia coli 16092007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID571874Antibacterial activity against Acinetobacter baumannii assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID544827Antimicrobial activity against Staphylococcus aureus Xen 30 biofilm assessed as log10 CFU/cm'2 in bacterial count in presence of 20 microamperes of electric current by bioelectric effect assay2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID286154Bactericidal activity against Staphylococcus aureus BSP-2443 at fAUC/MIC of 16 after 24 to 48 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID586736Ratio of mutant prevention concentration to MIC for qnrB gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrB12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID532023Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to CFU count by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID581097Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID593805Antimicrobial activity against Staphylococcus epidermidis ATCC 12228 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID1079932Highest frequency of moderate liver toxicity observed during clinical trials, expressed as a percentage. [column '% BIOL' in source]
AID1256534Antibacterial activity against ESBL-positive Escherichia coli 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1126761Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1237 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID244926Minimum inhibitory concentration against Bacteroides vulgatus ATCC 293272005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1430298Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID531513Antibacterial activity against Bacteroides spp. assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID533392Antimicrobial activity against Clostridium perfringens assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID425988Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3243 after 29 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID499670Antimicrobial activity against quinolone and penicillin-resistant Staphylococcus aureus SAR72 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID559042Antibacterial activity against vancomycin- resistant Enterococcus faecalis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID425561Antibacterial activity against penicillin-, quinolone-resistant Streptococcus pneumoniae HMC 1541 harboring mutation in L4 protein by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559489Antibacterial activity against Prevotella sp. by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID497758Apparent permeability across basolateral to apical side in human Calu3 cells2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID1224810CL/F in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID341390Cardiovascular activity in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit assessed as increase in fractional shortening at 20 mg/kg, iv administered every 12 hrs for 5 days by ECG2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID559061Antibacterial activity against Streptococcus anginosus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID562627Antimicrobial activity against Group B Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1067070Antimicrobial activity against quinolone-resistant Staphylococcus aureus clinical isolate 3505 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID406649Antibacterial activity against Staphylococcus aureus ACH-0221 isolate with gyrA Ser84Leu mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID424324Antimicrobial activity against Dialister micraerophilus assessed as susceptibility breakpoint by CA-SFM method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID535775Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID562829Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0757 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID279268Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 19 with GyrA S81F mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID428788Antibacterial activity against 80 mg q.d. moxifloxacin-pretreated Streptococcus pneumoniae isolate SR-26134 after 48 hrs of incubation by population analysis2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID571356Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID574999Antimicrobial activity against Eubacterium lentum after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID695446Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 5-FQR4M BSA678 expressing GyrA Ser84Leu and Ser85Pro mutant and GrlA Ser80Phe and Glu84Lys mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID574762Antimicrobial activity against Peptoniphilus asaccharolyticus assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID563018Antimycobacterial activity against Mycobacterium tuberculosis 04-0649 harboring gyrA Asp94Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID283394Antimicrobial activity against Nocardia beijingensis after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID529892Antimicrobial activity against Leptospira interrogans isolate 7 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID286049Peak free concentration at 400 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID559058Antibacterial activity against levofloxacin-susceptible Streptococcus pneumoniae by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1740332Antifungal activity against Penicillium chrysogenum ATCC 10106 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID698997Antimycobacterial activity against Mycobacterium tuberculosis infected in human assessed as log reduction of bacterial count at 400 mg, qd measured up to 2 days2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID570989Toxicity in healthy human assessed as incidence of adverse events at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID1256547Antibacterial activity against Pseudomonas aeruginosa 14-15 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID581090Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID574530Antimicrobial activity against Prevotella bivia assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID496652Antibacterial activity against Streptococcus pneumoniae 1065 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID528846Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID496642Antibacterial activity against Streptococcus pneumoniae 1151 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID586733Ratio of mutant prevention concentration to MIC for Escherichia coli ATCC 25922 expressing qnrS gene and pBK-QnrS12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1297327Antibacterial activity against Klebsiella pneumoniae 14-3 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID496644Antibacterial activity against Streptococcus pneumoniae 1058 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID520107Oral bioavailability in mouse at 300 mg/kg, po measured after 2 hrs2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID530368Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID559057Antibacterial activity against Lancefield Streptococcus sp. 'group G' by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID571835Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID532686Antimicrobial activity against ciprofloxacin-nonsusceptible, CJ PFGE pattern, emm89 type Streptococcus pyogenes with ST101 sequence type isolated from tonsillitis/pharyngitis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID342080Effect on growth of nonepidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID279237Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3009 with GyrA S81F and ParC D83N mutation after 19 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID323873Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae N5 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID508374Antibacterial activity against Streptococcus pneumoniae harboring mutation in 23S rRNA after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID574041Antibacterial activity against beta-lactamase producing Peptoniphilus asaccharolyticus by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID572518Antimicrobial activity against qnrS-positive Salmonella enterica serovar Typhimurium isolate s2705 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1430286Inhibition of Escherichia coli DNA gyrase assessed as inhibition of enzyme-mediated supercoiling of relaxed pHOT1 DNA substrate at 1.95 to 15.6 ug/ml after 30 mins by gel electrophoresis method2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID323895Antimicrobial activity against Klebsiella pneumoniae C2 GyrA Ser83Phe/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID581295Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1126756Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 753 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID1743456Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Ala-90-Val mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID322784Antimicrobial activity against Bacteroides distasonis assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID433402Inhibition of Mycobacterium leprae DNA gyrase subunit A A91V mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID573397Antibacterial activity against beta-lactamase producing Bacteroides thetaiotaomicron by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID571149Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID285294Effect on 4 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID586635Antibacterial activity against qnrB gene expressing Escherichia coli ATCC 25922 harboring ParC S80R mutant and pBK-QnrB1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID283166Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5204 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID560259Antimicrobial activity against Salmonella enterica serovar Typhimurium STYM61/9 expressing qnrB19 gene variant carried by IncL/M-like plasmid by Etest2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.
AID323660Antibacterial activity against Peptostreptococcus stomatis2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Antimicrobial susceptibilities of Peptostreptococcus anaerobius and the newly described Peptostreptococcus stomatis isolated from various human sources.
AID574742Antimicrobial activity against Peptostreptococcus micros after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID570899Antibacterial activity against non-levofloxacin susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1398603Antibacterial activity against penicillin-resistant Streptococcus pneumoniae 033806 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID544636Antimicrobial activity against Staphylococcus aureus Xen 30 by broth microdilution method2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID245331Antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA) 870307 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID456033Antibacterial activity against Klebsiella pneumoniae type 2 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID531516Antibacterial activity against Bacteroides caccae assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID521330fAUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID556779Apparent intercompartmental clearance in osteomyelitis patient at 400 mg, po administered for every 24 hrs by MAP-Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID497761Apparent permeability across basolateral to apical side in human Calu3 cells in presence of 3 uM PSC-833 P-gp inhibitor2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID571372Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1465260Antibacterial activity against clinical isolates of Escherichia coli by broth microdilution assay
AID1254071Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID523312Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC17042 harboring gyrA S84L/G106D, parC S80F and parE D732N mutant gene assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID285280Effect on 0.5 ug/ml sitofloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID368422Antimicrobial activity against Escherichia coli KAM32 pSTVqepA containing qepA gene ligated to pSTV28 plasmid by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID544867Antibacterial activity against Streptococcus pneumoniae U2A1060 harboring gyrA Ser81Phe parC Asp83His mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID283158Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2492 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID563336Induction of Cwp84 protease expression in Clostridium difficile 6425 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID574512Antimicrobial activity against Bacteroides vulgatus assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1750818Cytotoxicity against human HepG2 cells after 72 hrs by CellTiter Glo assay2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID559183Antimicrobial activity against Clostridium difficile C253E selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1297328Antibacterial activity against Klebsiella pneumoniae 14-4 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID406812Antibacterial activity against Staphylococcus aureus BSA678 isolate with gyrA Ser84Leu, Ser85Pro and grlA Ser80Phe, Glu84Gly mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID522966Antibacterial activity against Klebsiella pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID341383Concentration in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit serum at 20 mg/kg, iv administered every 12 hrs measured 30 mins after third dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID424327Antimicrobial activity against Dialister propionicifaciens by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID540232Dose normalised AUC in monkey after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID556769fAUC/MIC in osteomyelitis patient cancellous bone at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 0.375 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID1163997Antibacterial activity against extended-spectrum beta-lactamase producin Klebsiella pneumoniae 12-7 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID562456Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH372762009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID574524Antimicrobial activity against Prevotella oralis after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID66572Antibacterial activity was determined against clinically isolated vancomycin-A resistant enterococci (VRE) strains (33 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID533377Antimicrobial activity against Bacteroides merdae by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1398606Antibacterial activity against methicillin-resistant Staphylococcus aureus after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID518796Antimycobacterial activity against drug-susceptible Mycobacterium tuberculosis after 21 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID533389Antimicrobial activity against Clostridium perfringens by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID574965Antimicrobial activity against Actinomyces odontolyticus assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1676602Binding affinity to ferric ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID559049Antibacterial activity against Staphylococcus haemolyticus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1819733Antimycobacterial activity against Mycobacterium avium 11 assessed as inhibition of mycobacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID522947Antibacterial activity against ciprofloxacin-resistant Streptococcus pneumoniae by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1194335Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth at 50 uM after 48 hrs by MTT assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID518630Ratio of AUC (0 to 24 hrs) in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic model to MIC for Mycobacterium avium at 1 log10 CFU/ml bacterial concentration2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID511388Antibacterial activity against Klebsiella pneumoniae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID572270Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 13709 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID428804Ratio of Cmax in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID531626Antimicrobial activity against Mycoplasma genitalium by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID571384Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID586746Antibacterial activity against Escherichia coli ATCC 25922 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1380685Antibacterial activity against Escherichia coli infected in cyclophosphamide treated neutropenic CD1 mouse septicemia model assessed as mouse survival at 1.5 mg/kg, iv dosed at 1 hr post infection followed by redosing at 5 hrs post infection measured at 92018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID586734Ratio of mutant prevention concentration to MIC for Escherichia coli ATCC 25922 harboring GyrA S83L mutant2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID433581Selectivity index, ratio of IC50 for Mycobacterium leprae DNA gyrase subunit A G89C mutant to IC50 for Mycobacterium leprae wild type DNA gyrase A2B22008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID497760Apparent permeability across apical to basolateral side in human Calu3 cells in presence of 3 uM PSC-833 P-gp inhibitor2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID1743458Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Gly-88-Cys mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID1272964Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell growth at 50 uM after 72 hrs by MTT assay2016Bioorganic & medicinal chemistry, Feb-15, Volume: 24, Issue:4
Development of acridine derivatives as selective Mycobacterium tuberculosis DNA gyrase inhibitors.
AID425347Antibacterial activity against Streptococcus pneumoniae HMC 1070 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID574520Antimicrobial activity against Prevotella bivia after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1318914Antibacterial activity against gentamicin/tobramycin-resistant Pseudomonas aeruginosa isolate CANWARD-2011 96846 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID570986AUC (0 to 48 hrs) in healthy human assessed as 25-desacetyl-rifapentine level at 900 mg, po thrice weekly measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID424319Antimicrobial activity against Dialister pneumosintes by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID425554Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID586645Antibacterial activity against qnrS gene expressing Escherichia coli ATCC 25922 harboring ParC S80R mutant, ParC S80R mutant and pBK-QnrS1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1524623Antibacterial activity against Streptococcus mutans 3289 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID574774Antimicrobial activity against Clostridium perfringens assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID586637Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrA gene and pBK-QnrA1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID285535Effect on cellular viability of methicillin-sensitive Staphylococcus aureus ATCC 29213 by measuring the time required for recovery at 10 times MIC after 1 hr2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID323879Antimicrobial activity against Escherichia coli DH10B GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID530592Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr4 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID323870Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae UAB1 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID581098Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1676592Binding affinity to Gallium ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID571343Antibacterial activity against Enterococcus faecium assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID262136Cytotoxicity against human Hep2 laryngeal carcinoma cell line2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID249968Ratio of MPC to MIC aganist methicillin resistant Staphylococcus aureus-322005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID523156Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11223 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1372631Antibacterial activity against non replicating Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial count at 10 ug/ml incubated for 7 days followed by compound dilution measured after 4 weeks2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID496635Antibacterial activity against Streptococcus pneumoniae ATCC 496192010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID1600105Antibacterial activity against Escherichia coli ATCC 8739 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1079940Granulomatous liver disease, proven histopathologically. Value is number of references indexed. [column 'GRAN' in source]
AID323882Antimicrobial activity against qnrA1 expressing Escherichia coli DH10B expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID425986Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3243 after 41 passages with clarithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID369972Ratio of Cmax in Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po to MIC for methicillin-sensitive Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID571367Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID279292Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N and gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID530385Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I and A83S mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID574951Antimicrobial activity against Streptococcus pneumoniae serotype 7F by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID322779Antimicrobial activity against Bacteroides caccae isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID456051Inhibition of Staphylococcus aureus DNA gyrase Ser84Leu mutant2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID573783Antibacterial activity against Prevotella buccae by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID728914Antibacterial activity against Pseudomonas aeruginosa PAO1 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1600116Bactericidal activity against Streptococcus pneumoniae cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID559146Antimicrobial activity against Clostridium difficile 630a selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID484792Antibacterial activity against methicillin and ciprofloxacin-resistant Staphylococcus aureus 25A by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID562620Antimicrobial activity against vancomycin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID372984Antimycobacterial activity against Mycobacterium avium JATA51-01 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID508365Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID521103Antimicrobial activity against Streptococcus sp. 'group B' isolate 1 harboring gyrA Glu85Lys mutant, parC Ser79Tyr mutant and parE Ileu495Leu mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
AID574993Antimicrobial activity against Bifidobacterium sp. after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID570931Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID278859Inhibition of metabolic activity in MG63 cells assessed as MTT reduction after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID581077Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID341396Drug level in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit serum at 20 mg/kg, iv administered every 12 hrs measured 30 mins after seventh dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID1256564Antibacterial activity against Enterococcus faecalis 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID323894Antimicrobial activity against Klebsiella pneumoniae C2 GyrA Ser83Phe mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID372982Antimycobacterial activity against Mycobacterium avium complex N084 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID285162Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as bacterial density after 10 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID341375Antibacterial activity against Staphylococcus aureus by Etest2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID424325Antimicrobial activity against Dialister pneumosintes assessed as susceptibility breakpoint by CLSI-M11-A7 method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID559043Antibacterial activity against vancomycin- resistant Enterococcus faecium by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID373141Antimycobacterial activity against Mycobacterium avium complex N084 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID528849Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID574490Antimicrobial activity against Bacteroides vulgatus after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID571106Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID580763Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID425563Antibacterial activity against penicillin-, macrolide- and quinolone-susceptible Streptococcus pneumoniae HMC 63 after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1564360Antimycobacterial activity against Mycobacterium bovis BCG ATCC 35737 by resazurin dye based fluorimetric assay2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID558627Antimicrobial activity against Streptococcus pneumoniae isolate 3587 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID508366Antibacterial activity against penicillin-intermediate Streptococcus pneumoniae after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID283088Antibacterial activity against Staphylococcus aureus SA1199B overexpressing NorA at 5 ug by disk diffusion method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synthesis of omeprazole analogues and evaluation of these as potential inhibitors of the multidrug efflux pump NorA of Staphylococcus aureus.
AID584559Antimicrobial activity against Acinetobacter lwoffii isolate F expressing beta-lactamase OXA-164 isolated from tracheostoma of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID1297339Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-4 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID563339Induction of Cwp84 protease expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID633630Antibacterial activity against methicillin-sensitive Staphylococcus aureus 10-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1585702Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 to 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID556348Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae clinical isolates obtained from bronchial aspirations expressing 23S rRNA A2063G mutant gene and P1 RFLP type I gene by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Antimicrobial susceptibility of Mycoplasma pneumoniae isolates and molecular analysis of macrolide-resistant strains from Shanghai, China.
AID1364752Antibacterial activity against Mycobacterium tuberculosis H37Rv nutrient starvation model assessed as log reduction in bacterial colonies at 10 ug/ml measured after 7 days by MPN assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID428290Antimicrobial activity against Acinetobacter baumannii BM4454 isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID523318Antibacterial activity against Streptococcus pneumoniae OC6755 harboring gyrA S81F and parC S79Y mutant gene by agar dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID210029Antibacterial activity was determined against Streptococcus pneumoniae J-24 strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID405468Antibacterial activity against Escherichia coli TOP10 containing pAT851 in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID576133Antibacterial activity against 10'4 to 10'5 CFU Moraxella catarrhalis after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID563333Upregulation of cwp84 gene expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID518041Cardiotoxicity in healthy human assessed as change in corrected QT interval at 400 mg/kg, po within 12 hrs by ECG2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID540218Clearance in monkey after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID496647Antibacterial activity against Streptococcus pneumoniae 1072 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID559055Antibacterial activity against Lancefield Streptococcus sp. 'group C' by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID428835TMSW in Streptococcus pneumoniae isolate SR-23958 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID577500Bactericidal activity against Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model assessed as decrease in biofilm bacterial count at 400 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID561313Antimicrobial activity against Enterobacter cloacae isolate 37 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID520368Ratio of AUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID523314Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11521 harboring gyrA S84L/S85P, parC E84G mutant gene assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1224808CL/F in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID425577Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I4602008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559080Antibacterial activity against Legionella pneumophila by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID563212Antimycobacterial activity against Mycobacterium tuberculosis 08-0745 harboring gyrA Asp89Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID581485Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1126743Antibacterial activity against 0.5 ug/ml Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID456043Antibacterial activity against ciprofloxacin, methicillin-resistant Staphylococcus aureus after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID1504965Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days under aerobic condition by alamar blue assay2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID535774Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60H containing pCK0601 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID733004Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB G89C mutant-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID559076Antibacterial activity against ciprofloxacin-susceptible Haemophilus influenzae by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285279Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID562663Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH372762009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID405119Antimicrobial activity against Escherichia coli TOP10 harbouring pS2 plasmid expressing quinolone resistant QnrS2 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID581282Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID283157Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2414 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID581309Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1256550Antibacterial activity against Staphylococcus aureus CMCC 26003 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID553687Antimicrobial activity against Bifidobacterium in three-stage chemostat gut model assessed as log reduction in bacterial count at 43 mg/liter administered daily for 7 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID518800Antimycobacterial activity against Mycobacterium avium serovar 4 after 14 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID543403Cmax in brain of Listeria monocytogenes EGD-e infected BALB/c mouse central nervous system listeriosis model at 50 mg/kg, ip administered 36 hrs postinfection as single dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID559005Antibacterial activity against Streptococcus pneumoniae W002 harboring wild-type parC and gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID562451Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH373122009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID559499Antibacterial activity against Listeria monocytogenes assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID562462Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH373902009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID562659Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH373902009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID556771Drug level in osteomyelitis patient cortical bone at 400 mg, po administered for every 24 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID1600117Antibacterial activity against Serratia marcescens ATCC 12795 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID558929Antimicrobial activity against Clostridium difficile A422e selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559064Antibacterial activity against Streptococcus intermedius by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1252464Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 50 uM incubated for 48 hrs at 37 degC by MTT assay relative to control2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID556772Drug level in osteomyelitis patient cancellous bone at 400 mg, po administered for every 24 hrs2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID581086Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID508368Antibacterial activity against macrolide-susceptible Streptococcus pneumoniae after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID1154347Antimycobacterial activity against Mycobacterium tuberculosis over expressing DprE1 after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID556030P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side at 50 uM in presence of in presence of 10 uM of p-glycoprotein and MRP transport inducer rifampin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
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]
AID456052Selectivity ratio of IC50 for Staphylococcus aureus DNA gyrase Ser84Leu mutant to IC50 for Staphylococcus aureus wild type DNA gyrase2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID286160Bactericidal activity against Staphylococcus aureus BSP-2443 with parC S52G, N91D mutation and gyrA S114G mutation at fAUC/MIC of 24 after 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID699003Antimycobacterial activity against Mycobacterium tuberculosis clinical isolate2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID285966Antimicrobial susceptibility against Haemophilus influenzae C1 isolate with GyrA Asp88Asn, AcrR Leu31His and Arg34Glu mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID571148Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID496638Ratio of 50% mutant prevention concentration to MIC50 in Streptococcus pneumoniae ATCC 496192010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID570898Antibacterial activity against non-levofloxacin susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID728913Antibacterial activity against Mycoplasma pneumoniae 18-1 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID559392Antimicrobial activity against Clostridium difficile 630B selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID279279Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID533368Antimicrobial activity against Bacteroides uniformis assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1126764Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1288 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID581291Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1398033Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6J mouse assessed as log10 CFU reduction in bacterial lung count at 30 mg/kg, po administered once daily for 8 days measured post last dose relative to control2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
An efficient synthetic route for preparation of antimycobacterial wollamides and evaluation of their in vitro and in vivo efficacy.
AID286155Bactericidal activity against Staphylococcus aureus BSP-2443 at fAUC/MIC of 24 after 24 to 48 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1318924Antibacterial activity against pandrug-resistant Pseudomonas aeruginosa isolate 914332016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1399840Antibacterial activity against Mycobacterium tuberculosis H37Rv2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID571856Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1242343Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase assessed as supercoiling of pBR322 DNA after 90 mins by agarose gel electrophoresis method2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID571845Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID428808Ratio of Cmax in human at 80 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID556198P-glycoprotein-mediated transport in human Calu3 cells assessed as efflux ratio of permeability from apical to basolateral side over basolateral to apical side at 50 uM2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1256545Antibacterial activity against Pseudomonas aeruginosa 14-9 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID558880Antimicrobial activity against Clostridium difficile C253a selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID571123Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID593814Antimicrobial activity against Candida tropicalis ATCC 1369 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID574949Antimicrobial activity against Streptococcus pneumoniae serotype 3 by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1207436Inhibition of transient outward potassium current (Ito) current in Chinese Hamster Ovary (CHO) K1 cells expressing human Kv4.3 measured using IonWorks Quattro automated patch clamp platform
AID574989Antimicrobial activity against Bifidobacterium adolescentis assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID581305Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID571385Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID580875Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID543393Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as log reduction in bacterial CFU per ml of blood at 50 mg/kg, ip administered 36 hrs postinfection as single dose measured withi2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID543401Ratio of Cmax in plasma in Listeria monocytogenes EGD-e infected BALB/c mouse to MIC for Listeria monocytogenes EGD-e2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID558924Antimicrobial activity against Clostridium difficile A422c selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID532977Inhibition of DNA supercoiling activity of wild type Mycobacterium tuberculosis DNA gyrase A2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID571122Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID558605Antimicrobial activity against Streptococcus pneumoniae isolate 1146 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1585699Antimycobacterial activity against Mycobacterium smegmatis CMCC 93202 after 72 hrs by double dilution method2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID573557Antibacterial activity against beta-lactamase producing Bacteroides thetaiotaomicron assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID498781Antimicrobial activity against mild ciprofloxacin-resistant Streptococcus pyogenes by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID562616Antimicrobial activity against methicillin-resistant Staphylococcus aureus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID581310Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID511401Antibacterial activity against levofloxacin resistant Neisseria gonorrhoeae isolates by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID570686Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID523147Antibacterial activity against Streptococcus pneumoniae isolate OC6585 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID323880Antimicrobial activity against Escherichia coli DH10B/pACYC184 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID601781Antibacterial activity against 10'4 CFU methicillin-resistant Staphylococcus epidermidis 09-2 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID563048Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0790 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID341072Tmax in human at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID511396Antibacterial activity against Streptococcus viridans by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID559054Antibacterial activity against Streptococcus agalactiae by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID574006Antibacterial activity against beta-lactamase producing Clostridium tertium assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID369967Antibacterial activity against methicillin-sensitive Staphylococcus aureus by broth microdilution technique2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID1237412Bactericidal activity against Staphylococcus aureus RN4220 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID244988Minimum inhibitory concentration against Streptococcus pneumoniae ATCC 63032005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID544837Antibacterial activity against Streptococcus pneumoniae U2A1051 harboring gyrA Ser81Tyr mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID601780Antibacterial activity against 10'4 CFU methicillin-sensitive Staphylococcus epidermidis 09-6 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID425810Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung measured after 53 days after aerosol infection2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID1266237Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by alamar blue assay2016Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.
AID574981Antimicrobial activity against Actinomyces naeslundii after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID573800Antibacterial activity against Prevotella bivia assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1391311Antibacterial activity against Staphylococcus aureus 4220 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID544833Antibacterial activity against Streptococcus pneumoniae CP1000 by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID323872Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae N5 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1164007Antibacterial activity against methicillin-resistant Staphylococcus aureus 12-4 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1207470Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) K1 cells stably expressing hERG measured using IonWorks Quattro automated patch clamp platform
AID576325Antibacterial activity against 10'4 to 10'5 CFU methicillin-resistant Staphylococcus aureus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID580768Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID574809Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 horboring rpoB H526Y, katG D329A/R463L, gyrA D94G/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID574802Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2474 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1318911Antibacterial activity against gentamicin/tobramycin/ciprofloxacin-resistant Escherichia coli isolate CANWARD-2011 97615 harboring AAC3-2A after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID559067Antibacterial activity against Streptococcus salivarius by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID580764Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID533130Antimicrobial activity against Bacteroides distasonis assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID520367Ratio of AUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID262134Antimicrobial activity against Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID1601852Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID571840Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID558597Antimicrobial activity against Streptococcus pneumoniae 9 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID533393Antimicrobial activity against Clostridium innocuum by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID544829Antimicrobial activity against Staphylococcus epidermidis Xen 43 biofilm assessed as log10 CFU/cm'2 in bacterial count in presence of 2000 microamperes of electric current by bioelectric effect assay2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID562664Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH367422009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1207564Inhibition of long-lasting type calcium current (hICa) in Chinese Hamster Ovary (CHO) cells expressing hCav1.2 measured using IonWorks Quattro automated patch clamp platform
AID286153Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 449 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID531856Cmax in tuberculosis patient at 400 mg/day, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID1557313Half life in human at 0.4 g, po by HPLC analysis2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID581109Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID575007Antimicrobial activity against Eubacterium sp. assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID422675Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3009 after 25 passages with clarithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1264551Antibacterial activity against Staphylococcus aureus 1118 infected in sc and iv dosed mouse assessed as septicemia compound administered 1 hr post-infection twice for 1 day measured for 7 days2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID530348Antimicrobial activity against azide-resistant Escherichia coli J53 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID586747Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrA gene and pBK-QnrA1 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1398613Binding affinity to human serum albumin after 60 mins at 37 degC by ultrafiltration-based LC-MS analysis2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID759321Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID322785Antimicrobial activity against Bacteroides ovatus assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID532963Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 72010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID420669Lipophilicity, log D at pH 7.02009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID1398592Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae J41 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID1256560Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-37 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID279833Ratio of fraction AUC in Mycobacterium tuberculosis infected BALB/c mouse to MIC in Mycobacterium tuberculosis infected BALB/c mouse model at 38 to 19000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID422680Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3009 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1079949Proposed mechanism(s) of liver damage. [column 'MEC' in source]
AID275468Cytotoxicity against rat hepatocytes after 48 hrs2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID66574Antibacterial activity was determined against clinically isolated vancomycin-B resistant enterococci (VRE) strains (10 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1297335Antibacterial activity against Staphylococcus aureus CMCC 26003 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1380667Clearance in CD1 mouse plasma at 10 mg/kg, iv by LC-MS/MS analysis2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID511381Antibacterial activity against methicillin resistant coagulase negative Staphylococcus epidermidis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID422653Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3665 after 38 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1391314Antibacterial activity against Streptococcus mutans 3289 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID1740320Antimicrobial activity against Escherichia coli ATCC 8739 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID553805Antimicrobial activity against Clostridium difficile PCR ribotype 027 expressing gyrB Glu466Lys mutant grown on fluoroquinolone-containing medium after 48 hrs2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID425072Antimicrobial activity against Escherichia coli DH10B expressing pCRQB10 in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID1318906Antibacterial activity against Enterococcus faecalis ATCC 29212 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID428785Cmax in human at 200 mg, po administered twice a day2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1318915Antibacterial activity against Stenotrophomonas maltophilia isolate CAN-ICU 62584 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID278595Inhibitory activity against Escherichia coli 12-15022007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID559545Antibacterial activity against levofloxacin-susceptible Stenotrophomonas maltophilia by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID581300Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID456042Antibacterial activity against levofloxacin, methicillin-resistant Staphylococcus aureus after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID261739Antibacterial activity against Moraxella catarrhalis ATCC 81762006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID511400Antibacterial activity against ciprofloxacin resistant Neisseria gonorrhoeae isolates by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID278603Inhibitory activity against azide-resistant Escherichia coli J53 T03-2222007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID562650Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH375032009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID279261Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3665 with GyrA S81Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID580864Half life in patients with pulmonary tuberculosis at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID279280Antimicrobial activity against Streptococcus pneumoniae R6 transformants with gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
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).
AID574732Antimicrobial activity against Fusobacterium varium after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
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).
AID508367Antibacterial activity against penicillin-resistant Streptococcus pneumoniae after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID425578Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I4602008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID244995Minimum inhibitory concentration against Streptococcus agalactiae ATCC 138132005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID369968Cmax in Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID416848Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load at 100 mg/kg, po administered for 5 days per week measured after 8 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1318922Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 262-1018562016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID580750Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID523136Antibacterial activity against Streptococcus pneumoniae isolate OC7368 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID562941Effect on fbp69 gene expression in Clostridium difficile 6269 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID580868Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1600113Antibacterial activity against methicillin resistant Staphylococcus epidermidis ATCC 13199 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID580876Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID572522Antimicrobial activity against qnrA-positive Salmonella enterica serovar Mbandaka isolate s2093 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1164011Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 12-6 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID558581Antimicrobial activity against penicillin-susceptible Streptococcus pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1196885Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 28 days by agar dilution method2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID323875Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae 1960 GyrA Ser83Phe/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID558591Antimicrobial activity against Streptococcus pneumoniae 3 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID580895Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
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.
AID559526Antibacterial activity against Acinetobacter lwoffii assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID571373Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1242341Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microdilution method2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID342066Antimicrobial activity against fluoroquinolone-resistant epidemic Clostridium difficile NAP1 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID565314Antibacterial activity against Mycoplasma genitalium TW10-6G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID528966Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID581099Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID499677Antimicrobial activity against quinolone and penicillin-resistant Acinetobacter baumannii after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID520371Ratio of fAUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID523179Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC12501 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID496646Antibacterial activity against Streptococcus pneumoniae 1135 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID511383Antibacterial activity against vancomycin resistant Enterococcus faecalis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID581085Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563035Antimycobacterial activity against Mycobacterium tuberculosis 08-0774 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1348983Half life in mouse microsomes
AID1570247Cmax in SPF ICR mouse at 100 mg/kg, sc2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID574956Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 6B by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID425344Antibacterial activity against Streptococcus pneumoniae HMC 1058 harboring S79F, K137N mutation in quinolone-resistant determining regions of ParC gene and 460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID559204Antibacterial activity against Streptococcus pneumoniae D001 harboring parC Ser79Phe and gyrA Gly85Lys mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID532022Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to CFU count by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID586629Antibacterial activity against qnrS gene expressing Escherichia coli ATCC 25922 harboring ParC S80R mutant and pBK-QnrS1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID341087Half life in human with MDR1 3435 CC genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID565290Antimicrobial activity against Mycoplasma pneumoniae by agar dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
In vitro activity of a new quinoline derivative, ER-2, against clinical isolates of Mycoplasma pneumoniae and Mycoplasma hominis.
AID580881Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID728921Antibacterial activity against Enterococcus faecalis ATCC 19433 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1601850Antibacterial activity against Pseudomonas aeruginosa CMCC 10104 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID244996Minimum inhibitory concentration against Streptococcus pneumoniae ATCC 496192005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1319017Ratio of MIC for Pseudomonas aeruginosa PAO1 after 25 serial passages to MIC for Pseudomonas aeruginosa PAO1 prior to 25 serial passages2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1909942Inhibition of Staphylococcus aureus ATTC 25923 DNA gyrase2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1237411Antifungal activity against Candida albicans 7535 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1318925Antibacterial activity against pandrug-resistant Pseudomonas aeruginosa isolate 1012432016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID584112Bactericidal activity against Escherichia coli K-12 DM4100 after 2 hrs in presence of protein synthesis inhibitor chloramphenicol treated 10 mins before compound challenge2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID283170Increase in biofilm formation of Staphylococcus lugdunensis assessed as percent biofilm forming isolates2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID530387Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB R447K mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1256557Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID574728Antimicrobial activity against Prevotella oralis assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID559539Antibacterial activity against Proteus mirabilis assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID522980Antibacterial activity against Streptococcus pneumoniae isolate OC7189 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID496651Antibacterial activity against Streptococcus pneumoniae 1058 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID425340Antibacterial activity against quinolone-susceptible Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425973Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 2527 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID533360Antimicrobial activity against Bacteroides ovatus assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID574748Antimicrobial activity against Peptostreptococcus micros assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID574997Antimicrobial activity against Bifidobacterium sp. assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID601783Antibacterial activity against 10'4 CFU Enterococcus faecalis 08-10 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1164005Antibacterial activity against methicillin-sensitive Staphylococcus aureus 12-5 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID425358Antibacterial activity against Streptococcus pneumoniae HMC 1072 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID571133Antibacterial activity against penicillin-resistant Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID574969Antimicrobial activity against Actinomyces israelii after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID518798Antimycobacterial activity against Mycobacterium kansasii after 7 days by agar dilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
In vitro activities of DC-159a, a novel fluoroquinolone, against Mycobacterium species.
AID559046Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus aureus by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID581488Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559084Antibacterial activity against Proteus mirabilis by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID532957Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 12010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID425355Antibacterial activity against Streptococcus pneumoniae HMC 1055 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID573785Antibacterial activity against Prevotella intermedia by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID559405Antimicrobial activity against Clostridium difficile BI2C selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1557283Antibacterial activity against Haemophilus influenzae with horse blood by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID558912Antimicrobial activity against Clostridium difficile CD5i harboring GyrA Ala92Glu and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID544865Antibacterial activity against Streptococcus pneumoniae R6 Tr10 harboring gyrA Ser81Tyr parC Ser79Tyr mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID1243291Antimicrobial activity against Escherichia coli ATCC 25922 by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID1254075Antibacterial activity against Salmonella typhimurium 2421 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1468619Antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL6 mouse cornea assessed as mean corneal thickness at 0.3% administered tropically 2 times on day 1, 4 times on day 2 and 2 times on day 3 starting from 6 hrs post infection m2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo.
AID544294Antibacterial activity against hospital acquired methicillin-resistant Staphylococcus aureus after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID563225Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0779 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID523164Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11521 harboring gyrA S84L/S85P, parC E84G mutant gene by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID633637Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 10-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID574522Antimicrobial activity against Prevotella buccae after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID391988Antibacterial activity against Staphylococcus aureus RN4220 containing ORI23::qnr-cat promoter mutant by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID581063Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID456048Inhibition of Staphylococcus aureus DNA topoisomerase 4 Ser80Phe mutant2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID391989Antibacterial activity against Lactococcus lactis IL-1419 by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1890607Induction of drug resistance in methicillin resistant Staphylococcus aureus assessed as increase in MIC measured after 10 passages (Rvb = 0.4 ug/ml)2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID494414Antimycobacterial activity against Mycobacterium smegmatis CMCC 93202 after 72 hrs by serial double dilution method2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.
AID523311Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC17042 harboring gyrA S84L/G106D, parC S80F and parE D732N mutant gene assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID733008Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB assessed as reduction of enzyme supercoiling activity using relaxed pBR322 DNA substrate incubated for 1 hr at 37 degC by ethidium bromide based gel electrophoresis2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID574033Antibacterial activity against beta-lactamase producing Micromonas micros assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1743457Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Asp-94-Gly mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID633631Antibacterial activity against methicillin-sensitive Staphylococcus aureus 10-4 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1256566Antibacterial activity against Enterococcus faecium 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID544297Antibacterial activity against vancomycin-susceptible methicillin-resistant Staphylococcus aureus 32 harboring GyrA S84L and GrlA S80Y mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID405454Antibacterial activity against Escherichia coli C600Rif by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID556783Ratio of drug level in cortical bone to serum in osteomyelitis patient at 400 mg, po administered for every 24 hrs by by three stage hierarchical Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID575001Antimicrobial activity against Eubacterium lentum assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID559528Antibacterial activity against Citrobacter koseri assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID759326Antibacterial activity against Staphylococcus aureus KCTC 503 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID1256555Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-4 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID556190Cmax in healthy human at 400 mg/kg2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID286157Bactericidal activity against Staphylococcus aureus BSP-2443 with parC S52G, N91D mutation and gyrA S81Y mutation at fAUC/MIC of 16 after 72 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID571134Antibacterial activity against penicillin-resistant Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID389912Antibacterial activity against Staphylococcus aureus ATCC 13709 after 24 hrs by microdilution method2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.
AID428780AUC (0 to 24 hrs) in human at 400 mg, po administered once a day2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1888648Antibacterial activity against rifampicin resistant Staphylococcus aureus harboring RpoBH481Y mutant assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID1163994Antibacterial activity against Klebsiella pneumoniae 12-4 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID66578Antibacterial activity was determined against clinically isolated vancomycin-B resistant enterococci (VRE) strains (10 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1890601Antibacterial activity against methicillin resistant Staphylococcus aureus 032 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI based serial agar dilution method2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID542717Cmax in Nocardia brasiliensis HUJEG-1 infected BALB/c mouse at 25 mg/kg, sc every 8 hrs by HPLC2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Efficacy of ciprofloxacin and moxifloxacin against Nocardia brasiliensis in vitro and in an experimental model of actinomycetoma in BALB/c mice.
AID406648Antibacterial activity against Staphylococcus aureus ACH-0206 isolate with gyrA Ser84Leu mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID563036Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0777 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID586639Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrS gene and pBK-QnrS1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID559241Antibacterial activity against Streptococcus pneumoniae S002 harboring parC Ser79Phe mutant and wild-type gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID601784Antibacterial activity against 10'4 CFU Enterococcus faecalis 08-12 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID311524Oral bioavailability in human2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Hologram QSAR model for the prediction of human oral bioavailability.
AID565309Antibacterial activity against Mycoplasma genitalium by quantitative TaqMan PCR method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID571353Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1254070Antibacterial activity against Streptococcus mutans 3065 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID529903Antimicrobial activity against Leptospira kirschneri serovar Grippotyphosa isolate 13 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1256565Antibacterial activity against Enterococcus faecium 14-1 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1447480Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 101885 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1626632Bactericidal activity against methicillin-sensitive Staphylococcus aureus 29213 infected in mouse macrophages assessed as induction of bacterial kill at 4 ug/ml in presence of 4 ug/ml rifampin after 24 hrs2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1297341Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID559062Antibacterial activity against Streptococcus bovis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID533373Antimicrobial activity against Bacteroides eggerthii by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1318910Antibacterial activity against amikacin-resistant Escherichia coli isolate CAN-ICU 63074 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID408340Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Support vector machines classification of hERG liabilities based on atom types.
AID562449Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH366332009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID532961Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 52010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID556022P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side at 50 uM in presence of 100 uM of p-glycoprotein and MRP inhibitor verapamil2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID571844Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID570665Antibacterial activity against methicillin-resistant Staphylococcus aureus by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID556034P-glycoprotein-mediated transport in human Calu3 cells assessed as efflux ratio of permeability from apical to basolateral side over basolateral to apical side at 50 uM in presence of 100 uM of MRP inhibitor Probenecid2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID573590Antibacterial activity against Fusobacterium varium by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID406622Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae isolates assessed as percent susceptible isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.
AID484798Antibacterial activity against Staphylococcus aureus K1035 bearing wild-type GyrA and S80F mutant GrlA by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID531627Antimicrobial activity against Mycoplasma hominis by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID1319007Antimicrobial activity against Pseudomonas aeruginosa PAO2002016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID571115Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1819734Antibacterial activity against Staphylococcus aureus assessed as inhibition of bacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID279291Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parE D435N and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
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.
AID563016Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0810 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID574023Antibacterial activity against beta-lactamase producing Peptostreptococcus anaerobius by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID523162Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC2838 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581270Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1207753Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits2013Scientific reports, , Volume: 3MICE models: superior to the HERG model in predicting Torsade de Pointes.
AID498782Antimicrobial activity against ciprofloxacin-susceptible Streptococcus pyogenes harboring Asp91/Asn mutation in parC gene by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID1437918Antibacterial activity against methicilin-resistant Staphylococcus aureus ATCC 700699 by broth microdilution method2017Journal of natural products, 01-27, Volume: 80, Issue:1
Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.
AID372997Antimycobacterial activity against Mycobacterium avium complex N016 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID285308Susceptibility of methicillin-sensitive/resistant Staphylococcus aureus single-step mutant by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID571765Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID580865Plasma protein binding in healthy human at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID245330Antibacterial activity against Penicillin-resistant Streptococcus pneumoniae (PRSP) J-24 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID461172Antitubercular activity against Mycobacterium tuberculosis H37Rv by low-oxygen-recovery assay2010Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3
Synthesis, antimalarial and antitubercular activity of acetylenic chalcones.
AID572512Antimicrobial activity against Salmonella enterica serovar Montevideo isolate s2317 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID283398Antimicrobial activity against Nocardia carnea after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID528977Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID67078Antibacterial activity was determined against Enterococcus faecalis ATCC 19433 strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID573822Antibacterial activity against beta-lactamase producing Clostridium perfringens by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID425995Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3676 after 50 passages with moxifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID520380Renal toxicity in patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID323876Antimicrobial activity against qnrA1 expressing Klebsiella pneumoniae 1132 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID278856Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID728916Antibacterial activity against Haemophilus influenzae ATCC 49247 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID425557Antibacterial activity against quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 5048 expressing mefA by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1163996Antibacterial activity against extended-spectrum beta-lactamase producin Klebsiella pneumoniae 12-4 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID571925Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-G616N mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID532965Antimicrobial activity against multidrug-resistant Mycobacterium tuberculosis isolate 92010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1187837Selectivity index, ratio of CC50 for mouse RAW264.7 cells to MIC for Mycobacterium tuberculosis H37Rv2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID286149Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 32 after 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1447485Antibacterial activity against multidrug/extremely drug-resistant/colistin-resistant Pseudomonas aeruginosa isolate 101243 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID533361Antimicrobial activity against Bacteroides thetaiotaomicron by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID574516Antimicrobial activity against Bacteroides ovatus assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID278597Inhibitory activity against azide-resistant Escherichia coli J53 T12-11832007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID279246Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3243 after 20 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID559178Antimicrobial activity against Clostridium difficile C253C selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID695236Cytotoxicity against human Hep2 cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID695232Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 292132011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1600099Antibacterial activity against Staphylococcus epidermidis ATCC 14990 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID425361Antibacterial activity against Streptococcus pneumoniae HMC 1078 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID573819Antibacterial activity against Veillonella parvula by by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID544291Antibacterial activity against Staphylococcus aureus after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID405464Antibacterial activity against Escherichia coli TOP10 containing pIP1206 plasmid by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID558697Antimicrobial activity against Clostridium difficile C253 expressing tcdA and tcdB gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID428845Time above the mutant prevention concentration in Streptococcus pneumoniae isolate SR-26134 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID428853Bactericidal activity against Streptococcus pneumoniae ATCC 49619 assessed as reduction in number of viable cells under condition simulating oral administration of 400 mg once daily2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID531628Antimicrobial activity against Mycoplasma fermentans by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID1877397Antibacterial activity against methicillin-resistant Staphylococcus aureus 1972022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID563029Antimycobacterial activity against Mycobacterium tuberculosis 08-0773 harboring gyrA Pro8Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID422674Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3009 after 21 passages with gemifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID556029P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side at 50 uM in presence of 100 uM of MRP inhibitor Probenecid2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1868123Anti-tubercular activity against Mycobacterium tuberculosis infected in mouse J774.A1 cells assessed as inhibition of intracellular bacilli growth incubated for 72 hrs2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID422682Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1635 after 14 passages with clindamycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID559508Antibacterial activity against Staphylococcus warneri assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID581068Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID558618Antimicrobial activity against Streptococcus pneumoniae isolate 3263 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID575077Antimicrobial activity against Streptococcus pneumoniae serotype 3 assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID601793Cytotoxicity against MDCK cells after 48 hrs by CPE assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID406647Antibacterial activity against Staphylococcus aureus ACH-0204 isolate with gyrA Ser84Leu mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID574034Antibacterial activity against beta-lactamase producing Micromonas micros assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1600095Antibacterial activity against Staphylococcus aureus ATCC 6538 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID559050Antibacterial activity against Staphylococcus hominis by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1862200Antimycobacterial activity against clinical isolate multidrug resistant Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
AID425341Antibacterial activity against quinolone-resistant Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1602937Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 5 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID562932Antimicrobial activity against Clostridium difficile 6425 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID601791Antibacterial activity against 10'4 CFU Pseudomonas aeruginosa ATCC 27853 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID322326Antimicrobial activity against Streptococcus pneumoniae WB4 by broth macrodilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Daptomycin produces an enhanced bactericidal activity compared to ceftriaxone, measured by [3H]choline release in the cerebrospinal fluid, in experimental meningitis due to a penicillin-resistant pneumococcal strain without lysing its cell wall.
AID522994Antibacterial activity against Streptococcus pneumoniae isolate OC7376 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID558590Antimicrobial activity against Streptococcus pneumoniae 2 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID563210Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 04-0519 harboring gyrA Ala90Val and Asp94Asn mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID322773Antimicrobial activity against Bacteroides fragilis isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID1181169Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID574955Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19F by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID581659Fraction unbound in human plasma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID279256Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3009 with GyrA S81F and ParC D83N mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID511305Antibacterial activity against methicillin resistant coagulase negative Staphylococcus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID1877405Antibacterial activity against Pseudomonas aeruginosa ATCC 278532022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID728923Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae J24 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID341069Half life in human at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID425353Antibacterial activity against Streptococcus pneumoniae HMC 2538 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to ciproflox2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1600102Bactericidal activity against Enterococcus hirae ATCC 1052 cultured in BHI medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1862201Antimycobacterial activity against clinical isolate drug susceptible Mycobacterium tuberculosis H37Rv assessed as bacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-15, Volume: 72Discovery and preclinical evaluations of JBD0131, a novel nitrodihydro-imidazooxazole anti-tuberculosis agent.
AID279259Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 1076 with ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID520363Half-life in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID571767Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB-M626I mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID497762Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Calu3 cells in presence of 3 uM PSC-833 P-gp inhibitor2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID1256537Antibacterial activity against ESBL-positive Klebsiella pneumoniae 14-17 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID422670Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1076 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID341377Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as cured animals in blood culture at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 hrs after end of treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID593811Antimicrobial activity against Haemophilus influenzae ATCC 19418 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID531625Antimicrobial activity against Mycoplasma pneumoniae by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID581095Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
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).
AID1600111Antibacterial activity against methicillin resistant Staphylococcus aureus 6347 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID558887Antimicrobial activity against Clostridium difficile C253e selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1819731Antimycobacterial activity against Mycobacterium abscessus subsp. massiliense CCUG 48898T assessed as inhibition of mycobacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID1316917Inhibition of Mycobacterium tuberculosis ADH assessed as decrease in conversion of L-alanine to pyruvate by measuring NADH by spectrophotometry2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID559514Antibacterial activity against non-levofloxacin susceptible Streptococcus pneumoniae assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID573837Antibacterial activity against beta-lactamase producing Clostridium tertium assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID511391Antibacterial activity against Citrobacter freundii by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID562626Antimicrobial activity against Group B Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID580997Antimicrobial activity against Mycobacterium tuberculosis infected in patients with tuberculosis assessed as percentage of patients with negative culture after 4 weeks2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1126757Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 758 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID570687Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559158Antimicrobial activity against Clostridium difficile 630g harboring GyrB Asp26Val mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559387Antimicrobial activity against Clostridium difficile A422I harboring GyrA Thr82Ile and GyrB Leu451Phe mutant genes selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID543396Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as reduction in bacterial count in liver at 50 mg/kg, ip administered 36 hrs postinfection as single dose measured within 1 hr2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID520379Renal toxicity in patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1391312Antibacterial activity against quinolone-resistant Staphylococcus aureus isolate CCARM 3505 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID1819729Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 assessed as inhibition of mycobacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID1318932Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 1085902016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID279821Bactericidal activity in Mycobacterium tuberculosis H37Rv on day 12007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID422652Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3665 after 14 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID563015Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0744 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID561316Antimicrobial activity against Enterobacter cloacae isolate 101 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID279249Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 19 with GyrA S81F mutation after 32 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID433580Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID511303Antibacterial activity against ciprofloxacin susceptible and methicillin resistant Staphylococcus aureus by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID425964Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3274 after 48 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID581307Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID556781Ratio of drug level in cortical bone to serum in osteomyelitis patient at 400 mg, po administered for every 24 hrs by MAP-Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID262135Antimicrobial activity against methicillin-resistant Staphylococcus aureus 7006992006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID586731Ratio of mutant prevention concentration to MIC for Escherichia coli ATCC 25922 expressing qnrA gene and pBK-QnrA12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1435844Antimycobacterial activity against Mycobacterium tuberculosis CDCT-4 (1105/09) clinical isolate after 7 days by resazurin reduction microplate assay2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID279818Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774A.1 macrophages2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID1601854Antibacterial activity against multidrug-resistant Pseudomonas aeruginosa ATCC BAA-2111 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID283155Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL856 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID558601Antimicrobial activity against Streptococcus pneumoniae isolate 24 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1318908Antibacterial activity against Streptococcus pneumoniae ATCC 49619 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID285298Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID581312Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1465273Antibacterial activity against wild-type Escherichia coli ATCC 25922 infected in iv dosed CD-1 mouse assessed as mouse survival treated for 1 hr followed by reinfection with bacteria measured at 96 hrs post infection
AID572515Antimicrobial activity against Salmonella enterica serovar Stanley isolate s2043 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID105998In vitro inhibitory activity on MRC5 fibroblast tissue cultures inoculated with virulent RH strain of Toxoplasma gondii2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
AID496640Antibacterial activity against Streptococcus pneumoniae 1072 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID1264565Clearance in mouse at 2 mg/kg, iv by LC-MS/MS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID1676589Binding affinity to Nickel cation assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID574532Antimicrobial activity against Prevotella bivia assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1514453Antitubercular activity against moxifloxacin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID533380Antimicrobial activity against Bacteroides merdae assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID595854Cytotoxicity against human Hep2 cells after 72 hrs by alamar blue assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID1237407Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID558698Antimicrobial activity against Clostridium difficile CD25 expressing tcdA, tcdB gene and GyrB Ser416Ala mutant by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID322790Antimicrobial activity against Bacteroides eggerthii assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID562653Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH372762009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID571379Antibacterial activity against Klebsiella oxytoca assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID580904Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID518619Antimicrobial activity against extracellular Mycobacterium avium subsp. hominissuis ATCC 700898 after 7 days by CLSI method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID279286Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79F and gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID577495Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315 by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID283399Antimicrobial activity against Nocardia brasiliensis after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID530594Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr6 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID581075Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID498190Antibacterial activity against Stenotrophomonas maltophilia MBS82 deficient in Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID528838Antimicrobial activity against vancomycin-resistant Enterococcus sp. assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID369973Cmin in synovial fluid of Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po after 7 days2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID581664Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU level per mg of protein after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID442255Antimalarial activity against Plasmodium falciparum NF542009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Enhancement of the antimalarial activity of ciprofloxacin using a double prodrug/bioorganometallic approach.
AID406652Antibacterial activity against Staphylococcus aureus ACH-0126 isolate with gyrA Ser84Leu and grlA Ser80Phe mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID246862Efficacy against mice infected with Staphylococcus aureus ATCC 25923 upon s.c. administration2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID484796Antibacterial activity against wild-type norA expressing Staphylococcus aureus SA-1199 by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID581083Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID508373Antibacterial activity against Streptococcus pneumoniae harboring mutation in L4 ribosomal protein after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID570799Cmax in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID559403Antimicrobial activity against Clostridium difficile BI2A selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425558Antibacterial activity against penicillin-, quinolone-resistant and macrolide-susceptible Streptococcus pneumoniae HMC 1058 harboring S79F, K137N mutation in quinolone-resistant determining regions of ParC gene and 460V mutation in QRDR of ParE gene by br2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID562928Antimicrobial activity against Clostridium difficile ATCC 43603 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1079937Severe hepatitis, defined as possibly life-threatening liver failure or through clinical observations. Value is number of references indexed. [column 'MASS' in source]
AID279834Ratio of fraction Cmax in Mycobacterium tuberculosis infected BALB/c mouse to MIC in Mycobacterium tuberculosis infected BALB/c mouse model at 38 to 19000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID530383Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A, I85V, F96W and P101M mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1254079Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID497756Distribution coefficient, log D of the compound2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID532956Antimicrobial activity against Mycobacterium tuberculosis ATCC 358022010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID520362Half-life in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1570241Cytotoxicity against African green monkey Vero cells incubated for 72 hrs by MTT assay2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID574502Antimicrobial activity against Bacteroides caccae assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID576134Antibacterial activity against 10'4 to 10'5 CFU vancomycin-resistant Enterococcus after 18 hrs by CLSI 2-fold agar dilution method2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vitro and in vivo activities of LCB01-0371, a new oxazolidinone.
AID574977Antimicrobial activity against Actinomyces meyeri assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1868112Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID574514Antimicrobial activity against Bacteroides ovatus assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID559397Antimicrobial activity against Clostridium difficile 630D harboring GyrA Ala118Val mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1187835Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID209273Antibacterial activity was determined against Streptococcus pyogenes G-36 strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID574750Antimicrobial activity against Peptostreptococcus micros assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID556033P-glycoprotein-mediated transport in human Calu3 cells assessed as efflux ratio of permeability from apical to basolateral side over basolateral to apical side at 50 uM in presence of 3 uM of p-glycoprotein transport inhibitor PSC-8332009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID695449Cytotoxicity against human HepG2 cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID556773Apparent total clearance in osteomyelitis patient at 400 mg, po administered for every 24 hrs by MAP-Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID1152773Bactericidal activity against Mycobacterium tuberculosis infected in human THP1 cells at 1 ug/ml for 7 days2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID428846Time above the mutant prevention concentration in Streptococcus pneumoniae isolate SR-26137 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1297330Antibacterial activity against Pseudomonas aeruginosa 14-9 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1067076Antimicrobial activity against Pseudomonas aeruginosa 2004 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID245696Mutant prevention concentration aganist methicillin resistant Staphylococcus aureus-33 done for 48 hr at 37 degree C with compound2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID285968Antimicrobial susceptibility against Haemophilus influenzae C3 isolate with GyrA Asp88Asn, ParC Ser84Ile, AcrR Leu31His and Arg34Glu mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID570907Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID522995Antibacterial activity against Streptococcus pneumoniae isolate OC7376 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1551297Antibacterial activity against Methicillin-resistant Staphylococcus aureus CCARM 3167 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1524626Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1318964Antibacterial activity against extremely drug-resistant Pseudomonas aeruginosa isolate 104354 infected in Galleria mellonella assessed as larvae survival at 75 mg/kg administered as single dose measured after 96 hrs2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID530591Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr3 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID533409Antimicrobial activity against Finegoldia magna by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID425337Antibacterial activity against penicillin-resistant Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1551300Antibacterial activity against Quinolone-resistant Staphylococcus aureus CCARM 3519 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1154348Antimycobacterial activity against Mycobacterium tuberculosis over expressing InhA after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID324746Effect on Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as enhancement of supercoiled pBR322 DNA cleavage2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID279254Antibacterial activity against levofloxacin resistance selected Streptococcus pneumoniae 3009 with GyrA S81Y and ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID559500Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus aureus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID561326Antimicrobial activity against Klebsiella pneumoniae isolate 135 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID1601847Antibacterial activity against Escherichia coli CMCC 25922 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID581268Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563020Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-0319 harboring gyrA Asp94Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID425553Antibacterial activity against penicillin- and quinolone-susceptible Streptococcus pneumoniae HMC 5055 expressing mefA by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID522952Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1348984Cmax in ICR mouse at 50 mg/kg, po by HPLC analysis
AID544860Antibacterial activity against Streptococcus pneumoniae U2A1053 harboring parC Ser79Phe mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID406807Antibacterial activity against Staphylococcus aureus ACH-0141 isolate with gyrA Ser84Leu, Glu88Val and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID1476363Antitubercular activity against capreomycin resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID584554Antimicrobial activity against Acinetobacter lwoffii isolate A expressing beta-lactamase OXA-164 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID341081Tmax in human with MDR1 3435 CC genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID1381459Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse assessed as bacterial load in lungs at 30 mg/kg, po for 8 consecutive days starting from day 1 post infection measured on day 9 post last dose (Rvb = 6.8 +/- 0.22018Journal of medicinal chemistry, Aug-09, Volume: 61, Issue:15
Identification of Morpholino Thiophenes as Novel Mycobacterium tuberculosis Inhibitors, Targeting QcrB.
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]
AID528974Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID695447Cytotoxicity against human CHO cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1570245Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 1 incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID279242Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3665 with GyrA S81Y mutation after 38 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID1164001Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID565318Antibacterial activity against Mycoplasma genitalium M2300 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID275466Antibacterial activity against fluoroquinolone-resistant Staphylococcus aureus 273/T/T/T2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID733009Antimicrobial activity against Mycobacterium tuberculosis H37Rv assessed as drug concentration causing =<1% reduction in bacterial growth incubated for 21 to 30 days by proportion method2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID563223Antimycobacterial activity against Mycobacterium tuberculosis 08-0774 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID574026Antibacterial activity against beta-lactamase producing Peptostreptococcus anaerobius assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID406846Antibacterial activity against Escherichia coli TOP10 containing pS1A plasmid expressing quinolone resistance determinant QnrB4 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID580896Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID581296Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1278845Antimycobacterial activity against nutrient starved Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial load for 7 days measured after 28 days by microplate reader analysis2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID341085Half life in human with MDR1 3435 CC genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID580754Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID395718Antibacterial activity against Escherichia coli DH10B containing ORI23::qnr-cat promoter mutant by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID322780Antimicrobial activity against Bacteroides eggerthii isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID728909Antibacterial activity against levofloxacin-intermediate and levofloxacin-resistant Streptococcus pneumoniae after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1861191Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis assessed as mycobacterial growth inhibition2022Bioorganic & medicinal chemistry letters, 09-01, Volume: 71Discovery and preclinical profile of sudapyridine (WX-081), a novel anti-tuberculosis agent.
AID1152781Ratio of MIC for 5-(((3S,4R)-3-Fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA D89N mutant to MIC for wild-type Mycobacterium tuber2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID405116Antimicrobial activity against Escherichia coli TOP10 harbouring pVS1 expressing quinolone resistant Vibrio splendidus 12B01 QnrVS1 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID580882Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1750817Dissociation constant, pKa of the compound by UV metric method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID559085Antibacterial activity against Proteus vulgaris by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID572525Antimicrobial activity against qnrS-positive Salmonella enterica serovar Corvallis isolate s2017 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID522936Antibacterial activity against Streptococcus pneumoniae isolate OC6608 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID562662Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH380042009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID544844Antibacterial activity against Streptococcus pneumoniae U2A1411 harboring parC Asp83Gly mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID499679Antimicrobial activity against quinolone and penicillin-resistant Escherichia coli after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
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).
AID1600106Bactericidal activity against Escherichia coli ATCC 8739 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID580857Antimicrobial activity against rifampicin-sensitive Mycobacterium tuberculosis2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID580902Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID586643Antibacterial activity against qnrA gene expressing Escherichia coli ATCC 25922 harboring ParC S80R mutant, ParC S80R mutant and pBK-QnrA1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID428834TMSW in Streptococcus pneumoniae ATCC 49619 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID323884Antimicrobial activity against Escherichia coli J53 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1053481Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA M103I mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID323897Antimicrobial activity against Klebsiella pneumoniae C2/pMG252 GyrA Ser83Phe/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1723736Inhibition of human ERG by whole-cell patch clamp method2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID573801Antibacterial activity against Prevotella intermedia assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID425767Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 99 after 41 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID518057Toxicity in healthy human assessed as diarrhea at 400 mg/kg, po administered as single dose2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID508388Antibacterial activity against macrolide-resistant Streptococcus pyogenes harboring erm(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID574950Antimicrobial activity against Streptococcus pneumoniae serotype 35B by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID544848Antibacterial activity against Streptococcus pneumoniae U2A1060 harboring gyrA Ser81Phe parC Asp83His mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID558899Antimicrobial activity against Clostridium difficile CD5b harboring GyrB Ser416Ala mutant gene selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1380670AUC (0 to 24 hrs) in CD1 mouse plasma at 3 mg/kg, iv by LC-MS/MS analysis2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID571358Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID425350Antibacterial activity against Streptococcus pneumoniae HMC 1146 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, and D435N mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1179481Antimycobacterial activity against Mycobacterium avium ATCC 15769 in 7H9 medium after 6 days and 18 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID372990Antimycobacterial activity against Mycobacterium intracellular JATA52-01 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID484802Antibacterial activity against Staphylococcus aureus K1640 bearing S84L mutant GyrA and S80Y mutant GrlA by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID533863Antibacterial activity against toxin-positive Clostridium difficile clinical isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
In vitro activity of OPT-80 tested against clinical isolates of toxin-producing Clostridium difficile.
AID1185145Antimicrobial activity against 5-(((3S,4R)-3-fluoro-1-(2-(7-methoxy-2-oxo-1,5-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2-methylnicotinonitrile resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase D89N mutant2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID575080Antimicrobial activity against Streptococcus pneumoniae serotype 11A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID283165Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2664 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID285289Effect on 32 ug/ml ciprofloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID759322Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID601782Antibacterial activity against 10'4 CFU Streptococcus pneumoniae 08-4 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1312205Antibacterial activity against actively replicative Mycobacterium tuberculosis H37Rv measured after 7 days by MABA assay2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors.
AID1743462Antitubercular activity against Mycobacterium tuberculosis XDR measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID522983Antibacterial activity against Streptococcus pneumoniae isolate OC6608 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1079946Presence of at least one case with successful reintroduction. [column 'REINT' in source]
AID369974Ratio of Cmin in synovial fluid of Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po to MIC for methicillin-sensitive Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID544853Antibacterial activity against Streptococcus pneumoniae R6 Tr6 harboring gyrA Ser81Phe mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID559492Antibacterial activity against Clostridium perfringens assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID522965Antibacterial activity against Enterobacter aerogenes by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1416246Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 measured after 7 days by microplate alamar blue assay2017MedChemComm, Jun-01, Volume: 8, Issue:6
Benzylsulfanyl benzo-heterocycle amides and hydrazones as new agents against drug-susceptible and resistant
AID586742Antibacterial activity against Escherichia coli ATCC 25922 harboring GyrA S83L mutant assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID523153Antibacterial activity against Streptococcus pneumoniae isolate OC6610 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID508384Antibacterial activity against Streptococcus pyogenes harboring erm(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID523151Antibacterial activity against Streptococcus pneumoniae isolate OC6610 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID573802Antibacterial activity against Prevotella melaninogenica assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID341385AUC (0 to 12 hrs) in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit at 20 mg/kg, iv administered every 12 hrs measured after third dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID728906Inhibition of human ERG expressed in CHOK1 cells at 100 uM2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1256533Antibacterial activity against ESBL-positive Escherichia coli 14-1 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1601844Antibacterial activity against Streptococcus pneumoniae CMCC 31968 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID424323Antimicrobial activity against Dialister pneumosintes assessed as susceptibility breakpoint by CA-SFM method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID544847Antibacterial activity against Streptococcus pneumoniae U2A1056 harboring gyrA Ser81Tyr parC Asp83His mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID498188Antibacterial activity against Stenotrophomonas maltophilia MBS108 containing both chromosomally and plasmid encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID562443Antibacterial activity against Staphylococcus aureus SMH37503 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID520113Antimicrobial activity against Mycobacterium tuberculosis H37Rv by alamar blue assay2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID581272Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1303042Antibacterial activity against methicillin-susceptible Staphylococcus aureus 42 incubated for 18 to 24 hrs by broth microdilution assay2016ACS medicinal chemistry letters, Apr-14, Volume: 7, Issue:4
Discovery of Pyrazolopyridones as a Novel Class of Gyrase B Inhibitors Using Structure Guided Design.
AID559523Antibacterial activity against Streptococcus sanguinis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559086Antibacterial activity against ciprofloxacin-susceptible Pseudomonas aeruginosa by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID323878Antimicrobial activity against Escherichia coli DH10B expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID559082Antibacterial activity against Morganella morganii by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1318916Antibacterial activity against Acinetobacter baumannii isolate CAN-ICU 63169 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID574740Antimicrobial activity against Peptostreptococcus anaerobius after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID559165Antimicrobial activity against Clostridium difficile BI2b harboring GyrB Arg447Lys mutant gene selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID285528Antibacterial activity against ethidium bromide-resistant Staphylococcus aureus ATCC 29213 after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID1546639Antitubercular activity against Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial population at 10 ug/ml under starvation condition after 7 days by MPN assay2020Journal of natural products, 01-24, Volume: 83, Issue:1
Usnic Acid Enaminone-Coupled 1,2,3-Triazoles as Antibacterial and Antitubercular Agents.
AID571766Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-615-628MexB-N616 mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID581477Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID405461Antibacterial activity against Escherichia coli TOP10 by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID571104Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID563217Antimycobacterial activity against Mycobacterium tuberculosis 08-0773 harboring gyrA Pro8Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID571870Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID543397AUC (24 hrs) in plasma in Listeria monocytogenes EGD-e infected BALB/c mouse central nervous system listeriosis model at 50 mg/kg, ip administered 36 hrs postinfection as single dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID1557287Antibacterial activity against Enterococcus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID1819098Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 3 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID559044Antibacterial activity against Listeria monocytogenes by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558611Antimicrobial activity against Streptococcus pneumoniae isolate 1564 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID563220Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0746 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1297352Antibacterial activity against Enterococcus faecalis 14-3 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID283156Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2394 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID563045Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0930 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID571120Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1297319Antibacterial activity against extended-spectrum beta-lactamase-producing Escherichia coli 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID559411Antimicrobial activity against Clostridium difficile BI2F harboring GyrB Glu466Lys mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID544292Antibacterial activity against methicillin-susceptible Staphylococcus aureus after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID285304Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID559537Antibacterial activity against Morganella morganii assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID574510Antimicrobial activity against Bacteroides vulgatus assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID562940Effect on fbp69 gene expression in Clostridium difficile CD07-259 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID580756Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563341Induction of Cwp84 protease expression in Clostridium difficile 6269 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID586740Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrB gene and pBK-QnrB1 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID571350Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID572271Antimicrobial activity against methicillin-resistant Staphylococcus aureus NB01021 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID571371Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1264557Antibacterial activity against Streptococcus pneumoniae for 18 to 24 hrs by broth microdilution method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID1243292Antimicrobial activity against ciprofloxacin-resistant Escherichia coli clinical isolates by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID511382Antibacterial activity against Enterococcus faecalis by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID1743453Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in human macrophages assessed as intracellular bacterial load at MIC measured after 6 days (Rvb = 5.57 to 6.43 logCFU/ml)2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID581660Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient infected in human THP-1 cells assessed as log reduction of intracellular CFU after 5 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1524627Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID574991Antimicrobial activity against Bifidobacterium adolescentis assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID559164Antimicrobial activity against Clostridium difficile BI2a harboring GyrB Arg447Lys mutant gene selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID279263Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 3676 with GyrA E85G, GyrB S478I and ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID428827Ratio of Cmax in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1403707Antibiofilm activity against Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial load at 10 ug/ml incubated for 1 week by MPN assay2018European journal of medicinal chemistry, Feb-10, Volume: 145Identification and development of benzoxazole derivatives as novel bacterial glutamate racemase inhibitors.
AID581285Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1447484Antibacterial activity against multidrug/extremely drug-resistant/colistin-resistant Pseudomonas aeruginosa isolate 91433 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID559194Antimicrobial activity against Clostridium difficile CD5D harboring GyrB Ser416Ala mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1237409Antibacterial activity against Pseudomonas aeruginosa 2004 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID497757Apparent permeability across apical to basolateral side in human Calu3 cells2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID405459Antibacterial activity against Escherichia coli C600Rif containing pIP1206 plasmid in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID518625Volume of distribution in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic modell by LC analysis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID556189Apparent passive permeability across human Calu3 cells at < 10 ug/ml2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID570902Antibacterial activity against non-levofloxacin susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID523173Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11223 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID563047Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0785 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID245697Mutant prevention concentration aganist methicillin resistant Staphylococcus aureus-5023 done for 48 hr at 37 degree C with compound2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID559200Antibacterial activity against Streptococcus pneumoniae S001 harboring parC Asp83Asn mutant and wild-type gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID556027P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side at 50 uM in presence of 100 uM of p-glycoprotein and MRP inhibitor verapamil2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID533631Antimicrobial activity against Propionibacterium acnes by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID558621Antimicrobial activity against Streptococcus pneumoniae isolate 3346 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559166Antimicrobial activity against Clostridium difficile BI2c harboring GyrB Arg447Lys mutant gene selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID406654Antibacterial activity against Staphylococcus aureus ACH-0186 isolate with gyrA Ser84Leu and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID279822Bactericidal activity in Mycobacterium tuberculosis H37Rv on day 72007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID581102Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563041Antimycobacterial activity against Mycobacterium tuberculosis 00-0715 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1297345Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-37 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID456029Antibacterial activity against Streptococcus pyogenes G-36 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID1318923Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 264-1043542016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1252459Inhibition of Mycobacterium smegmatis DNA gyrase B expressed in Escherichia coli BL21 (DE3) pLysS cells assessed as reduction in ATPase activity incubated for 100 mins by inorganic phosphate detection assay2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID559238Antibacterial activity against Streptococcus pneumoniae W001 harboring wild-type parC and gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID530389Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA A83S mutant/GyrB R447K mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID562927Antimicrobial activity against Clostridium difficile ATCC 43603-M1 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID580906Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID341379Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as cured animals in blood culture at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID540230Dose normalised AUC in rat after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID580753Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID544866Antibacterial activity against Streptococcus pneumoniae U2A1056 harboring gyrA Ser81Tyr parC Asp83His mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID532964Antimicrobial activity against streptomycin-resistant Mycobacterium tuberculosis isolate 82010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID580874Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559505Antibacterial activity against Staphylococcus hominis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID562628Antimicrobial activity against Group C Streptococcus by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID581093Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID558922Antimicrobial activity against Clostridium difficile A422a selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID341376Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as number of survival days at 20 mg/kg, iv administered every 12 hrs for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID562450Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH370992009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1740333Cytotoxicity against rat L6 cells assessed as inhibition of cell viability incubated for 24 hrs by MTT assay2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID416842Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load per culture-positive foot-pad at 10 mg/kg, po administered for 5 days per week measured after 8 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID425348Antibacterial activity against Streptococcus pneumoniae HMC 1073 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID571351Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID520374Cardiotoxicity in patient with intracerebral and leptomeningeal tuberculosis assessed as QT prolongation at 800 mg/kg, po QID2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID635055Antibacterial activity against Staphylococcus aureus ATCC 25923 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID261730Antibacterial activity against Staphylococcus aureus ATCC 292132006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID323892Antimicrobial activity against Escherichia coli J53/p1132 negative expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID571865Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID590140Antitubercular activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2011Bioorganic & medicinal chemistry letters, Apr-01, Volume: 21, Issue:7
Novel thiolactone-isatin hybrids as potential antimalarial and antitubercular agents.
AID528839Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1655164Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.1 cells assessed as reduction in bacterial colony at 1 to 10 times MIC incubated for 72 hrs by colony counting method2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Improving the Potency of
AID395716Antibacterial activity against Escherichia coli DH10B by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1600101Antibacterial activity against Enterococcus hirae ATCC 1052 cultured in BHI medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID498189Antibacterial activity against Stenotrophomonas maltophilia MBS109 containing chromosomally encoded Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID523174Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC8525 harboring wild type quinolone resistance-determining region assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581303Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1152775Antimycobacterial activity against spontaneously resistant mutant of Mycobacterium tuberculosis H37Rv at 10 to 20 times MIC up to 6 to 8 weeks2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID581283Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID341082Tmax in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID369977Antibacterial activity against methicillin-sensitive Staphylococcus aureus infected rabbit arthritis model assessed as change in bacterial load per gram of synovial fluid at 45 mg/kg, po after 7 days by broth microdilution technique2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID562929Antimicrobial activity against Clostridium difficile CD196 M1 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1254080Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1664938Antimalarial activity against CQ-sensitive Plasmodium falciparum 3D7 assessed as inhibition of parasite growth2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity.
AID535776Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60K containing pMH94 carrying the luxAB gene under the hsp60 promoter after 7 days determined according to RLU count by real-time luminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID245137Minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus-322005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID522958Antibacterial activity against Enterococcus faecalis ATCC 29212 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID532976Antimicrobial activity against multidrug drug-resistant Mycobacterium tuberculosis isolate 202010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1676600Binding affinity to zinc ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID581269Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID558606Antimicrobial activity against Streptococcus pneumoniae isolate 1147 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID577501Bactericidal activity against Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model assessed as decrease in planktonic cell count at 400 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1252462Inhibition of DNA gyrase GyrA/GyrB in Mycobacterium tuberculosis incubated for 30 mins assessed as reduction in supercoiling of relaxed relaxed pBR322 DNA by ethidium bromide staining based agarose gel electrophoresis method2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID559154Antimicrobial activity against Clostridium difficile 630f selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID544863Antibacterial activity against Streptococcus pneumoniae U2A1411 harboring parC Asp83Gly mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID728919Antibacterial activity against Bacillus subtilis IID 685 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID559195Antimicrobial activity against Clostridium difficile CD5E harboring GyrB Ser416Ala mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID581281Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID528976Antimicrobial activity against methicillin-susceptible Staphylococcus aureus isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID286059Peak free concentration at 800 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1514452Antitubercular activity against kanamycin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID433579Inhibition of Mycobacterium leprae wild type DNA gyrase subunit A A91V mutant assessed as formation of DNA cleavable complex2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID559205Antibacterial activity against Streptococcus pneumoniae D002 harboring parC Ser79Phe and gyrA Ser81Phe mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID559501Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus aureus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID563044Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-1647 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285160Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed as bacterial density after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID573583Antibacterial activity against beta-lactamase producing Bacteroides caccae assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID522978Antibacterial activity against Streptococcus pneumoniae isolate OC7189 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID558596Antimicrobial activity against Streptococcus pneumoniae 8 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID558918Antimicrobial activity against Clostridium difficile CD5i harboring GyrA Ala118Ser, Thr82Ala and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
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.
AID456028Antibacterial activity against Streptococcus pneumoniae J-24 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID521342Cmin in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1312204Antibacterial activity against nutrient-starved dormant Mycobacterium tuberculosis H37Rv assessed in log reduction in bacterial count at 10 ug/ml measured after 7 days by MPN assay relative to control2016Bioorganic & medicinal chemistry, 09-15, Volume: 24, Issue:18
Design and development of new class of Mycobacterium tuberculosisl-alanine dehydrogenase inhibitors.
AID1264555Antibacterial activity against methicillin-resistant Staphylococcus aureus 1118 for 18 to 20 hrs by broth microdilution method2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID1750827Plasma protein binding in Sprague-Dawley rat at 10 uM after 4 hrs by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID581079Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID285290Susceptibility of penicillin-resistant Streptococcus pneumoniae 216 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID341387Concentration in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit serum at 20 mg/kg, iv administered every 12 hrs measured 30 mins after seventh dose in presence of Dexamethasone2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID1676595Binding affinity to Ferric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1626633Bactericidal activity against methicillin-resistant Staphylococcus aureus 29213 infected in mouse macrophages assessed as induction of bacterial kill at 4 ug/ml in presence of 4 ug/ml rifampin after 24 hrs2016Journal of medicinal chemistry, 07-28, Volume: 59, Issue:14
Development of a Dual-Acting Antibacterial Agent (TNP-2092) for the Treatment of Persistent Bacterial Infections.
AID1053479Antitubercular activity against Mycobacterium tuberculosis H37Rv expressing inhA G96V mutant assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID422686Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 37 after 14 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID544296Antibacterial activity against quinolone-resistant Staphylococcus aureus after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID206214Antibacterial activity was determined against Staphylococcus epidermis 56500 strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID341084Tmax in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID520100Antimicrobial activity against Mycobacterium tuberculosis Erdman injected into gamma interferon gene knockout C57BL/6 mouse assessed as bacterial load in lung of mouse at 300 mg/kg measured 9 days post drug treatment2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID1601845Antibacterial activity against Enterococcus faecalis CMCC 29212 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID562938Upregulation of cwp84 gene expression in Clostridium difficile 6269 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID342078Effect on growth of epidemic Clostridium difficile BI9 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID633739Antibacterial activity against Klebsiella pneumoniae 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID484800Antibacterial activity against Staphylococcus aureus K1305 bearing wild-type GyrA and E84K mutant GrlA by microdilution technique2010Journal of medicinal chemistry, Jun-10, Volume: 53, Issue:11
From 6-aminoquinolone antibacterials to 6-amino-7-thiopyranopyridinylquinolone ethyl esters as inhibitors of Staphylococcus aureus multidrug efflux pumps.
AID1316915Antimycobacterial activity against dormant stage of Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth under nutrient starved conditions at 10 ug/ml for 7 days measured after 28 days2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID286162fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 800 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID285306Effect on 16 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID574810Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 horboring rpoB D516V, katG S315T/R463L, gyrA D94G/S95T/R128S/Y129C, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID342254Effect on growth of fluoroquinolone-resistant epidemic Clostridium difficile NAP1 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID528847Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1468618Antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL6 mouse cornea assessed as decrease in corneal infiltrates at 0.3% administered tropically 2 times on day 1, 4 times on day 2 and 2 times on day 3 starting from 6 hrs post in2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo.
AID574736Antimicrobial activity against Fusobacterium nucleatum after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID428837TMSW in Streptococcus pneumoniae isolate SR-26137 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID342255Effect on growth of fluoroquinolone-resistant epidemic Clostridium difficile NAP1 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 5 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID416839Antimycobacterial activity against Mycobacterium ulcerans isolate CU0012007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID755684Inhibition of human ERG current by patch clamp assay2013Bioorganic & medicinal chemistry letters, Jul-01, Volume: 23, Issue:13
The synergic modeling for the binding of fluoroquinolone antibiotics to the hERG potassium channel.
AID428819Ratio of AUC (0 to 24 hrs) in human at 80 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1398600Antibacterial activity against Pseudomonas aeruginosa PAO1 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID428806Ratio of Cmax in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID323888Antimicrobial activity against qnrA1 expressing Escherichia coli J53/pN5 expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID425571Antibacterial activity against penicillin-, macrolide-susceptible and quinolone-resistant Streptococcus pneumoniae HMC 1074 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutat2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1551294Antibacterial activity against Escherichia coli 1924 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID532684Antimicrobial activity against ciprofloxacin-nonsusceptible, AM PFGE pattern, emm6 type Streptococcus pyogenes with ST382 sequence type, ParC S79A mutant isolated from oropharyngeal colonization2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID586630Antibacterial activity against Escherichia coli ATCC 25922 harboring ParC S80R mutant by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID593808Antimicrobial activity against quinilone-pencillin-resistant Acinetobacter baumannii clinical isolate by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID544861Antibacterial activity against Streptococcus pneumoniae U2A1413 harboring parC Ser79Tyr mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID571370Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID577494Antimicrobial activity against methicillin-susceptible Staphylococcus aureus SH1000 by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1163989Antibacterial activity against extended-spectrum beta-lactamase producing Escherichia coli 12-3 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID534364Antibacterial activity against wild type Escherichia coli K-12 KD1397 harboring gyr gene2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Use of gyrase resistance mutants to guide selection of 8-methoxy-quinazoline-2,4-diones.
AID532687Antimicrobial activity against ciprofloxacin-nonsusceptible, K PFGE pattern, emm5 type Streptococcus pyogenes with ST99 sequence type, ParC D83G isolated from oropharyngeal colonization2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID425360Antibacterial activity against Streptococcus pneumoniae HMC 1077 harboring S81Y and S79F mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1750823Inhibition of human ERG expressed in CHO cells by whole cell patch-clamp method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID581308Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID584557Antimicrobial activity against Acinetobacter lwoffii isolate D expressing beta-lactamase OXA-164 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID1740328Antifungal activity against Candida albicans ATCC 10231 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID521150Antibacterial activity against intracellular Listeria monocytogenes EGDe infected in bone marrow-derived BALB/c mouse macrophage assessed as changes in morphology of intracellular bacteria observed to be ghostly, chained, and elongated at >= MIC after 48 2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID562937Upregulation of cwp84 gene expression in Clostridium difficile CD07-259 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID553686Antimicrobial activity against Enterococcus in three-stage chemostat gut model assessed as log reduction in bacterial count at 43 mg/liter administered daily for 7 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID285281Effect on 1 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID572524Antimicrobial activity against qnrS-positive Salmonella enterica serovar Stanley isolate s2018 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID556766Antimicrobial activity against Staphylococcus aureus2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID586652Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrB gene and pBK-QnrB1 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1254073Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID531529Antibacterial activity against Bacteroides uniformis isolate by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1600108Bactericidal activity against Pseudomonas aeruginosa ATCC 9027 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID496653Antibacterial activity against Streptococcus pneumoniae 1135 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID368418Antimicrobial activity against multidrug-resistant Escherichia coli C316 pHPA containing mutated GyrA gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID285959Antimicrobial susceptibility against Haemophilus influenzae A2 with GyrA Glu83Cys, ParC Ser84Arg and AcrR 97stop codon mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID164393Antibacterial activity was determined against Pseudomonas aeruginosa PAO1 strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID586752Antibacterial activity against qnrA gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrA1 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID341071Tmax in human at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID425972Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 2527 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID540221Volume of distribution at steady state in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID571388Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID508370Antibacterial activity against Streptococcus pneumoniae harboring mef(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID575082Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID561322Antimicrobial activity against Escherichia coli isolate 48 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID633742Antibacterial activity against Pseudomonas aeruginosa 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID524825Antibacterial activity against erythromycin susceptible Campylobacter sp. by agar plate dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Antimicrobial susceptibilities of multidrug-resistant Campylobacter jejuni and C. coli strains: in vitro activities of 20 antimicrobial agents.
AID558904Antimicrobial activity against Clostridium difficile CD5d harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID369966Antibacterial activity against methicillin-resistant Staphylococcus aureus by broth microdilution technique2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID570692Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1557284Antibacterial activity against Staphylococcus aureus by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID286048Peak free concentration at 200 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID496645Antibacterial activity against Streptococcus pneumoniae 1065 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID424320Antimicrobial activity against Dialister micraerophilus by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID285286Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID522969Antibacterial activity against Providencia stuartii by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID561315Antimicrobial activity against Enterobacter cloacae isolate 101 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID1399858Antitubercular activity against rifampicin-resistant Mycobacterium tuberculosis H37Rv harboring RpoB S522L mutant2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID563226Antimycobacterial activity against Mycobacterium tuberculosis 08-0781 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID562648Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH373122009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID556762fAUC/MIC in osteomyelitis patient cancellous bone at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 0.25 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID285302Susceptibility of penicillin-resistant Streptococcus pneumoniae 218 by by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID559070Antibacterial activity against Acinetobacter calcoaceticus by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1570248Half life in SPF ICR mouse at 100 mg/kg, sc2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID556197P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side at 50 uM2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID562452Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH373902009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID728905Aqueous solubility of the compound2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID570794Tmax in healthy human at 400 mg, po qd measured on day 4 by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID559375Antimicrobial activity against Clostridium difficile A422C selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID593812Antimicrobial activity against Pseudomonas aeruginosa ATCC 9027 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID285530Antibacterial activity against ethidium bromide-resistant Staphylococcus aureus Mu50 after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID565331Antibacterial activity against Mycoplasma genitalium M6287 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID1237413Bactericidal activity against Staphylococcus aureus KCTC 209 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1877421Antibacterial activity against Neisseria gonorrhoeae WHO Z2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
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).
AID322787Antimicrobial activity against Bacteroides uniformis assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID1740329Antifungal activity against Aspergillus flavus ATCC 9643 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID515921Antibacterial activity against clofazimine-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID556191Activity at P-glycoprotein in human Calu3 cells2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1430303Cytotoxicity against mouse NIH/3T3 cells assessed as reduction in cell proliferation after 24 hrs by MTT assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID533405Antimicrobial activity against Clostridium tertium by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID496636Antibacterial activity against Streptococcus pneumoniae ATCC 49619 assessed as 50% mutant prevention concentration2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID388878Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 10 mg/kg, iv administered as single dose 1 hr before bacterial challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID533385Antimicrobial activity against Clostridium difficile by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID520359Cmin in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID406844Antibacterial activity against Escherichia coli TOP10 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID511399Antibacterial activity against Haemophilus influenzae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID520105Oral bioavailability in mouse at 300 mg/kg, po measured after 30 mins2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID1868113Selectivity index, ratio of IC50 for cytotoxicity against mouse J774.A1 cells to MIC90 for anti-tubercular activity against Mycobacterium tuberculosis H37Rv2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID279269Antibacterial activity against levofloxacin resistance selected Streptococcus pneumoniae 19 with GyrA S81Y and ParC D83Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID369964Cmax in human serum at 400 mg, po administered as single dose after 1 hr2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID562634Antimicrobial activity against Corynebacterium spp. by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID406658Antibacterial activity against Staphylococcus aureus ACH-0129 isolate with gyrA Ser84Leu, Glu88Val and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID530590Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr2 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID581489Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID499678Antimicrobial activity against Escherichia coli ATCC 8739 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID574052Antibacterial activity against beta-lactamase producing Finegoldia magna assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID245695Mutant prevention concentration against methicillin resistant Staphylococcus aureus-32 done for 48 h at 37 degree C with compound2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1318927Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 860532016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID562619Antimicrobial activity against Heterovancomycin-resistant Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID279273Antibacterial activity against Streptococcus pneumoniae assessed as period of suppression of bacterial growth2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID530593Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr5 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID535769Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID279272Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 37 with GyrA S81Y, GyrB E474K and ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID1868110Anti-tubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID556195P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as minimum apparent permeability from basolateral to apical side2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1611014Induction of membrane integrity impairment in methicillin-resistant Staphylococcus aureus ATCC 700699 at 20 uM measured for 30 mins by DiOC2(3) probe based fluorescence assay2019Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria.
AID278853Cytotoxicity against primary human osteoblasts at 400 ug/ml assessed as LDH release after 24 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID559391Antimicrobial activity against Clostridium difficile 630A selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1602928Antibacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID497759Efflux ratio of apparent permeability across basolateral to apical side over apical to basolateral side in human Calu3 cells2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Relative contributions of active mediated transport and passive diffusion of fluoroquinolones with various lipophilicities in a Calu-3 lung epithelial cell model.
AID728926Antibacterial activity against Staphylococcus aureus FDA 209-P after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID559520Antibacterial activity against Streptococcus mitis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID535773Antimicrobial activity against Mycobacterium ulcerans 1059 harboring pTY60K carrying the luxAB gene under the hsp60 promoter agar dilution method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID425336Antibacterial activity against penicillin-intermediate Streptococcus pneumoniae ATCC 49619 by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID406657Antibacterial activity against Staphylococcus aureus ACH-0129 isolate with gyrA Ser84Leu, Glu88Val and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID575102Antimicrobial activity against Streptococcus pneumoniae serotype 19F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID491950Antibacterial activity against Staphylococcus aureus ATCC 12600 after 48 hrs by microtiter plate assay2010Journal of natural products, Jul-23, Volume: 73, Issue:7
Mayamycin, a cytotoxic polyketide from a Streptomyces strain isolated from the marine sponge Halichondria panicea.
AID581289Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID425573Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 99 harboring S81Y and S79Y mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively after 41 passages 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID580909Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1585700Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID283391Antimicrobial activity against Nocardia farcinica after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID158681In vitro inhibitory activity against chloroquine-resistant Plasmodium falciparum NF54-R in blood2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
AID581267Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID425977Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 24 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID558894Antimicrobial activity against Clostridium difficile C253i harboring GyrA Ala118Ser mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID544824Antimicrobial activity against Staphylococcus aureus Xen 30 biofilm assessed as log10 CFU/cm'2 in bacterial count2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID511395Antibacterial activity against Streptococcus agalactiae by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID626867Antimicrobial activity against replicating Mycobacterium tuberculosis after 8 days by micro plate alamar blue assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID1297348Antibacterial activity against Enterococcus faecium 14-1 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID543402Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as mouse survival at 50 mg/kg, ip administered 36 hrs postinfection every 12 hrs for 5 days measured after 2 months2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID570792AUC (0 to 24 hrs ) in healthy human at 400 mg, po qd measured on day 4 by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID581673Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1476361Antitubercular activity against moxifloxacin resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID279206Antibacterial activity against Streptococcus pneumoniae 3243 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID533866Antibacterial activity against toxin-positive Clostridium difficile clinical isolate assessed as percent of susceptible isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
In vitro activity of OPT-80 tested against clinical isolates of toxin-producing Clostridium difficile.
AID425562Antibacterial activity against penicillin- and quinolone-susceptible Streptococcus pneumoniae HMC 5055 expressing mefA after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID161281Inhibition of human Potassium channel HERG expressed in mammalian cells2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Prediction of hERG potassium channel affinity by traditional and hologram qSAR methods.
AID425352Antibacterial activity against Streptococcus pneumoniae HMC 1150 harboring S81C mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1207376Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells expressing hKvLQT1/hminK measured using IonWorks Quattro automated patch clamp platform
AID562656Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH366332009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID279836Toxicity in Mycobacterium tuberculosis infected BALB/c mouse model at 38 to 19000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID559532Antibacterial activity against non-ciprofloxacin-susceptible Haemophilus influenzae assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID583102Apparent permeability from apical to basolateral side of human Calu3 cells after 6 hrs2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Aerosol therapy with colistin methanesulfonate: a biopharmaceutical issue illustrated in rats.
AID562617Antimicrobial activity against methicillin-resistant Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID422676Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3009 after 19 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID581084Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID574724Antimicrobial activity against Prevotella buccae assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID562946Upregulation of slpA gene expression in Clostridium difficile CD196 M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID406621Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae isolates by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Prevalence, characteristics, and molecular epidemiology of macrolide and fluoroquinolone resistance in clinical isolates of Streptococcus pneumoniae at five tertiary-care hospitals in Korea.
AID531635Antimicrobial activity against fluoroquinolone-resistant Ureaplasma parvum by broth microdilution method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Comparative in vitro activities of the investigational fluoroquinolone DC-159a and other antimicrobial agents against human mycoplasmas and ureaplasmas.
AID244957Minimum inhibitory concentration against Streptococcus sanguis ATCC 105562005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID586739Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrA gene and pBK-QnrA1 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID562440Antibacterial activity against Staphylococcus aureus SMH37099 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1398610Inhibition of human ERG expressed in CHOK1 cells at 100 uM2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID633642Antibacterial activity against Enterococcus faecium 09-5 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID342077Effect on growth of nonepidemic Clostridium difficile J29 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1393810Antitubercular activity against non-replicating Mycobacterium tuberculosis H37Rv after 10 days by low oxygen recovery assay2018European journal of medicinal chemistry, Feb-25, Volume: 146Fluoroquinolone derivatives and their anti-tubercular activities.
AID580759Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1256543Antibacterial activity against Klebsiella pneumoniae 14-4 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID406651Antibacterial activity against Staphylococcus aureus ACH-0218 isolate with grlA Glu84Lys mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID574534Antimicrobial activity against Prevotella buccae assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID562637Antimicrobial activity against Listeria monocytogenes assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID425984Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1635 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID286148Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 32 after 72 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1254078Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1318930Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 861412016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID428839TMSW in Streptococcus pneumoniae isolate SR-26137 infected human at 80 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID558881Antimicrobial activity against Clostridium difficile C253b selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID518060Toxicity in healthy human assessed as headache at 400 mg/kg, po administered as single dose2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID1237414Bactericidal activity against Staphylococcus aureus KCTC 503 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID424329Antimicrobial activity against Dialister propionicifaciens assessed as susceptibility breakpoint by CLSI method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID593902Inhibition of Escherichia coli topoisomerase 4 assessed as decatenation of kDNA after 30 mins by electrophoresis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID425575Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene after 22 passages with moxifloxacin measured afte2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1187838Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 as substrate at 0.97 uM after 30 mins by DNA supercoiling assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID285285Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID558898Antimicrobial activity against Clostridium difficile CD5a harboring GyrB Ser416Ala mutant gene selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID533388Antimicrobial activity against Clostridium difficile assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1319008Antimicrobial activity against Pseudomonas aeruginosa PAO7502016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1256536Antibacterial activity against Escherichia coli 14-2 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID520360Cmin in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID279831Half life in BALB/c mouse at 6 to 400 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID586735Ratio of mutant prevention concentration to MIC for qnrA gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrA12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1600094Lipophilicity, log k of the compound at 100 ug/ml by micellar electrokinetic chromatography2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID1447482Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P262-101856 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID562934Upregulation of slpA gene expression in Clostridium difficile CD07-259 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID428826Ratio of Cmax in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1909953Selectivity ratio of MIC99 for wild type Mycobacterium tuberculosis H37Rv to MIC99 for Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID422128Antimicrobial activity against Mycobacterium smegmatis by broth microdilution assay2009Journal of natural products, May-22, Volume: 72, Issue:5
Antimicrobial ambiguine isonitriles from the cyanobacterium Fischerella ambigua.
AID584561Antimicrobial activity against Acinetobacter lwoffii isolate H expressing beta-lactamase OXA-58 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID561323Antimicrobial activity against Klebsiella pneumoniae isolate 132 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID521145Antibacterial activity against extracellular Listeria monocytogenes EGDe assessed as reduction in bacterial count at four times of MIC after 6 hrs by time-kill study2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID275463Inhibition of Staphylococcus aureus DNA gyrase by supercoiling assay2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID626868Antimicrobial activity against non-replicating Mycobacterium tuberculosis after 11 days by luminescence based low oxygen recovery assay2011Bioorganic & medicinal chemistry letters, Oct-15, Volume: 21, Issue:20
Synthesis and structure-activity relationships of novel substituted 8-amino, 8-thio, and 1,8-pyrazole congeners of antitubercular rifamycin S and rifampin.
AID556776Volume of distribution in central compartment in osteomyelitis patient at 400 mg, po administered for every 24 hrs by three stage hierarchical Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID433403Inhibition of Mycobacterium leprae wild type DNA gyrase subunit B D205N mutant assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID570690Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID530595Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr7 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID279202Antibacterial activity against Streptococcus pneumoniae 3009 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID425354Antibacterial activity against Streptococcus pneumoniae HMC 5041 harboring S81F and S79F mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID586754Antibacterial activity against qnrS gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrS1 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID428776Ratio of mutant prevention concentration for Streptococcus pneumoniae ATCC 49619 to MIC for Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID573798Antibacterial activity against Prevotella melaninogenica assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID341083Tmax in human with MDR1 3435 CC genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID531519Antibacterial activity against Bacteroides thetaiotaomicron assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1600097Antibacterial activity against methicillin resistant Staphylococcus aureus N315 cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID561318Antimicrobial activity against Enterobacter cloacae isolate 153 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID584113Ratio of LD99 for Escherichia coli K-12 DM4100 to MIC for Escherichia coli K-12 DM41002010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
Effect of N-1/c-8 ring fusion and C-7 ring structure on fluoroquinolone lethality.
AID586741Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrS gene and pBK-QnrS1 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1570246Antimycobacterial activity against multidrug (isoniazid and rifampicin) resistant Mycobacterium tuberculosis 2 incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID563038Antimycobacterial activity against Mycobacterium tuberculosis 08-0781 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID581652Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1398605Antibacterial activity against Escherichia coli 5-037042'98 harboring gyrase A Asp87Gly mutation after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID456049Selectivity ratio of IC50 for Staphylococcus aureus DNA topoisomerase 4 Ser80Phe mutant to IC50 for Staphylococcus aureus wild type DNA topoisomerase 42009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID1430292Antibacterial activity against Escherichia coli ATCC 35218 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID285965Antimicrobial susceptibility against Haemophilus influenzae C isolate with AcrR Leu31His and Arg34Glu mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID1237422Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1819097Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 4 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID581103Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID558617Antimicrobial activity against Streptococcus pneumoniae isolate 3260 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID580767Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID635059Antibacterial activity against methicillin-resistant Staphylococcus aureus 10-4 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID699002Cmax in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1868119Anti-tubercular activity against Mycobacterium tuberculosis CF161 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID1600118Bactericidal activity against Serratia marcescens ATCC 12795 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID341088Half life in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID559524Antibacterial activity against Acinetobacter baumannii assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1316914Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by MABA2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID581656Antibacterial activity against revertant Staphylococcus aureus at pH 7.4 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1237404Antibacterial activity against Staphylococcus aureus KCTC 503 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID556023P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side at 50 uM in presence of 3 uM P-gp inhibitor PSC-8332009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID428836TMSW in Streptococcus pneumoniae isolate SR-26134 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID96072Antibacterial activity was determined against Klebsiella pneumoniae type II strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID286152Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 236 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1750814Antibacterial activity against Fluoroquinolone-resistant Staphylococcus aureus ATCC 49951 assessed as reduction in bacterial growth by CLSI based broth microdilution method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID540233Dose normalised AUC in human after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID759323Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID581657Antibacterial activity against normal phenotype Staphylococcus aureus at pH 7.4 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID286147Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 32 after 24 to 48 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID341381Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as reduction in bacterial burdens in heart valve tissue culture at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 hrs afte2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID573582Antibacterial activity against beta-lactamase producing Bacteroides caccae assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID633632Antibacterial activity against methicillin-sensitive Staphylococcus aureus 10-5 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID438556Antimycobacterial activity against Mycobacterium tuberculosis H37Rv replicating form by alamar blue assay2009Journal of medicinal chemistry, Oct-22, Volume: 52, Issue:20
Synthesis, biological evaluation, and structure-activity relationships for 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl ester derivatives as valuable antitubercular chemotypes.
AID580870Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1372638Antibacterial activity against Mycobacterium marinum ATCC BAA-535 infected in zebra fish assessed as log reduction in bacterial load at 10 mg/kg, po for 7 days2018Bioorganic & medicinal chemistry, 01-01, Volume: 26, Issue:1
Lead identification and optimization of bacterial glutamate racemase inhibitors.
AID559399Antimicrobial activity against Clostridium difficile 630F harboring GyrA Ala118Val mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1890606Antibacterial activity against beta-lactams, macrolide and fluoroquinolone resistant Streptococcus pneumoniae 718 infected in po dosed Swiss mouse septicemia model assessed as protective dose administered on 1 and 5 hrs post infection and measured on day 2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID1154351Antimycobacterial activity against BTZ043-resistant Mycobacterium tuberculosis over expressing DprE1 C387S mutant after 5 days by standard microdilution method2014Journal of medicinal chemistry, Jun-26, Volume: 57, Issue:12
4-aminoquinolone piperidine amides: noncovalent inhibitors of DprE1 with long residence time and potent antimycobacterial activity.
AID580995Drug excretion in feces of healthy human at 800 mg/kg2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID559147Antimicrobial activity against Clostridium difficile 630b selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID562643Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH372762009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID581070Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563021Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0172 harboring gyrA Asp94Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID286159Bactericidal activity against Staphylococcus aureus BSP-2443 with parC S52G, N91D mutation and gyrA S114G mutation at fAUC/MIC of 24 after 72 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID341393Toxicity in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit assessed as collagenization median score at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose by histopathology2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID563026Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2834 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID603876Antitubercular activity against non-replicating Mycobacterium tuberculosis H37Rv ATCC 27294 incubated 10 days under anaerobic condition measured after 28 hrs of recovery in air by luciferase based low oxygen recovery assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID695448Cytotoxicity against human HeLa cell line after 72 hrs2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1600115Antibacterial activity against Streptococcus pneumoniae cultured in MH medium assessed as reduction in bacterial growth incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID574784Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2403 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1888649Antibacterial activity against wild type Staphylococcus aureus assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID553804Antimicrobial activity against Clostridium difficile PCR ribotype 001 after 48 hrs2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID570706Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID341066Plasma concentration in human at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID529893Antimicrobial activity against Leptospira interrogans serovar Bataviae isolate 1 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1601853Antibacterial activity against multidrug-resistant Escherichia coli ATCC BAA-196 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID523146Antibacterial activity against Streptococcus pneumoniae isolate OC6585 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID244990Antibacterial activity against Staphylococcus aureus FDA 209P was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID433400Inhibition of Mycobacterium leprae wild type DNA gyrase A2B2 assessed as DNA supercoiling inhibition2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID369963Half life in human serum at 400 mg, po administered as single dose2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID1877414Antibacterial activity against Neisseria gonorrhoeae WHO Q2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID558615Antimicrobial activity against Streptococcus pneumoniae isolate 2874 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1494123Antibacterial activity against methicillin-resistant Staphylococcus aureus NCTC 13373 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID279239Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 1076 with ParC S79Y mutation after 35 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID285293Effect on 2 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID586753Antibacterial activity against qnrB gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrB1 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID279277Antimicrobial activity agaisnt Streptococcus pneumoniae R6 transformants with parC S79Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID405115Antimicrobial activity against Vibrio splendidus LGP32 expressing plasmid-mediated QnrS-like quinolone resistance determinants2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID571378Antibacterial activity against Klebsiella oxytoca assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID422668Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1076 after 35 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID633847Antibacterial activity against Enterococcus faecium 09-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID581665Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU level at up to 10'5 times MIC after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID428789Antibacterial activity against 200 mg b.i.d. levofloxacin-pretreated Streptococcus pneumoniae isolate SR-26134 after 48 hrs of incubation by population analysis2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID558594Antimicrobial activity against Streptococcus pneumoniae 6 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID560261Antimicrobial activity against Escherichia coli CSH26RifR receiving qnrB19 gene variant carried by IncL/M-like plasmid from Salmonella enterica serovar Typhimurium STYM61/9 by Etest2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.
AID1330186Antibacterial activity against Staphylococcus aureus 4220 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID1237408Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID562645Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH369452009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID556031P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side at 50 uM in presence of in presence of 25 uM of p-glycoprotein and MRP transport inducer rifampin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID521830Antimicrobial activity against Streptococcus pneumoniae isolated from meningitis patient assessed as percent susceptible isolates by CLSI method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Clonal spread of highly beta-lactam-resistant Streptococcus pneumoniae isolates in Taiwan.
AID584560Antimicrobial activity against Acinetobacter lwoffii isolate G expressing beta-lactamase OXA-58 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID523160Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC8530 harboring gyrA S84L and parC I143V mutant gene by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID286081fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 400 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID373004Antimycobacterial activity against Mycobacterium avium complex N018 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID530376Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB N464S mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID580911Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID581088Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID593798Antimicrobial activity against Bacillus cereus ATCC 11778 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID342083Effect on growth of epidemic Clostridium difficile BI6-8-17 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1740323Antimicrobial activity against Salmonella enterica ATCC 13312 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID422649Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3676 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1699553Induction of cell membrane permeabilization in methicillin resistant Staphylococcus aureus ATCC 700699 measured at 5 mins interval for 2 hrs by propidium iodide staining based fluorescence assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial
AID581106Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1699554Induction of cell membrane permeabilization in GFP-expressing Staphylococcus aureus ATCC 700699 assessed as increase in cellular ATP leakage at 5 fold MIC measured after 0.5 hrs by Bactiter-glo assay2020Journal of medicinal chemistry, 11-12, Volume: 63, Issue:21
Nature-Inspired (di)Azine-Bridged Bisindole Alkaloids with Potent Antibacterial
AID574494Antimicrobial activity against Bacteroides fragilis assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID570803Volume of distribution in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID428772Bactericidal activity against Streptococcus pneumoniae ATCC 49619 assessed as mutant prevention concentration after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID279276Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID559530Antibacterial activity against Enterobacter cloacae assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1164009Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 12-1 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID283240Reduction of bacterial counts in Mycobacterium tuberculosis H37Rv infected Swiss mouse lung at 100 mg/kg, po for 5 days/week after 2 months2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID559498Antibacterial activity against vancomycin- resistant Enterococcus faecium assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID558620Antimicrobial activity against Streptococcus pneumoniae isolate 3282 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID372978Antimycobacterial activity against Mycobacterium avium JATA51-01 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1476362Antitubercular activity against bedaquiline resistant Mycobacterium tuberculosis H37Rv after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID406847Antibacterial activity against Enterobacter cloacae S1 isolate expressing quinolone resistance determinant QnrB4 by E-test2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Plasmid-mediated quinolone resistance determinant QnrB4 identified in France in an Enterobacter cloacae clinical isolate coexpressing a QnrS1 determinant.
AID699000Half life in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID532966Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 102010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID523313Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11521 harboring gyrA S84L/S85P, parC E84G mutant gene assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID563037Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0779 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID608513Antibacterial activity against Mycobacterium smegmatis KD11632011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones.
AID456034Antibacterial activity against Pseudomonas aeruginosa PAO1 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID159910In vitro inhibitory activity against hepatic stages of Plasmodium yoelii yoelii 265 BY; No data2004Bioorganic & medicinal chemistry letters, Jun-07, Volume: 14, Issue:11
Synthesis of new fluoroquinolones and evaluation of their in vitro activity on Toxoplasma gondii and Plasmodium spp.
AID1318907Antibacterial activity against Enterococcus faecium ATCC 27270 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID580762Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID540217Volume of distribution at steady state in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID342073Effect on growth of nonepidemic Clostridium difficile J29 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID285531Antibacterial activity against ethidium bromide-resistant Staphylococcus aureus Mu50 in presence of 20 ug/ml reserpine after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID695235Inhibition of Staphylococcus aureus topoisomerase 4 by decatenation assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID1398604Antibacterial activity against quinolone-resistant Escherichia coli DNS5101 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID425574Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 harboring S81Y and S79Y mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively after 42 passages2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID581100Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID406650Antibacterial activity against Staphylococcus aureus ACH-0216 isolate with grlA Ser80Phe mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID633648Antibacterial activity against Escherichia coli 09-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID586636Antibacterial activity against qnrA gene expressing Escherichia coli ATCC 25922 harboring ParC S80R mutant and pBK-QnrA1 by broth microdilution method2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID530382Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S, S84A and I85V mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
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.
AID1877400Antibacterial activity against Acinetobacter baumannii 1402022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID322789Antimicrobial activity against Bacteroides caccae assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID556188P-glycoprotein-mediated transport in human Calu3 cells assessed as efflux ratio of permeability from apical to basolateral side over basolateral to apical side at 50 uM in presence of 25 uM of p-glycoprotein and MRP transport inducer rifampin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1585704Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis after 3 to 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID530375Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB R447K mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID532973Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 172010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID559546Antibacterial activity against levofloxacin-susceptible Stenotrophomonas maltophilia assessed as assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID544836Antibacterial activity against Streptococcus pneumoniae U2A1050 harboring gyrA Ser81Phe mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID285532Antibacterial activity against ethidium bromide-resistant Staphylococcus aureus BSA643 after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID425804AUC in human at 400 mg, po2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID574738Antimicrobial activity against Fusobacterium mortiferum after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID286062Half life at 200 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID563215Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0794 harboring gyrA Thr80Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID586751Antibacterial activity against Escherichia coli ATCC 25922 harboring GyrA S83L mutant assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID286060Half life at 100 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID581306Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID558623Antimicrobial activity against Streptococcus pneumoniae isolate 3412 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1163995Antibacterial activity against extended-spectrum beta-lactamase producin Klebsiella pneumoniae 12-3 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1819730Antimycobacterial activity against Mycobacterium abscessus subsp. bolletii CCUG 50184T assessed as inhibition of mycobacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID522996Antibacterial activity against Streptococcus pneumoniae isolate OC6790 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID571869Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID581671Antibacterial activity against normal phenotype Staphylococcus aureus in cation-adjusted MH 2 broth at pH 5.5 after 24 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID1602933Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 1 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID570800Tmax in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID1468622Antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL6 mouse cornea assessed as decrease in log bacterial load/tissue at 0.3% administered tropically 2 times on day 1, 4 times on day 2 and 2 times on day 3 starting from 6 hrs p2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo.
AID633738Antibacterial activity against Klebsiella pneumoniae 09-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID530373Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I and A83S mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1318928Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 860672016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID428791Antibacterial activity against 200 mg b.i.d. levofloxacin-pretreated Streptococcus pneumoniae isolate SR-26137 after 48 hrs of incubation by population analysis2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID322788Antimicrobial activity against Bacteroides vulgatus assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID422644Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3676 after 44 passages with clarithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1398591Antibacterial activity against penicillin-susceptible Streptococcus pneumoniae J24 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID530377Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA A83S mutant/GyrB R447K mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID275462Inhibition of Staphylococcus aureus topoisomerase 4 by decatenation assay2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID562652Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH380042009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID644238Antitubercular activity against Mycobacterium tuberculosis H37Rv after 16 to 24 hrs by microplate alamar blue assay2012European journal of medicinal chemistry, Mar, Volume: 49Synthesis and evaluation of anti-tubercular and antibacterial activities of new 4-(2,6-dichlorobenzyloxy)phenyl thiazole, oxazole and imidazole derivatives. Part 2.
AID540220Clearance in human after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID562930Antimicrobial activity against Clostridium difficile CD07-259 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
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).
AID523158Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11696 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID595862Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 700699 after 24 hrs by microdilution method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID533376Antimicrobial activity against Bacteroides eggerthii assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID424879Antimicrobial activity against multidrug-resistant Enterobacter cloacae E705 bearing qnrB10 gene with aac(6)-IId-aadA1a integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID279275Antimicrobial activity against Streptococcus pneumoniae R62007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID244935Minimum inhibitory concentration against Klebsiella pneumoniae ATCC 100312005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID278594Inhibitory activity against azide-resistant Escherichia coli J532007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID580863Tmax in patients with pulmonary tuberculosis at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1297332Antibacterial activity against Pseudomonas aeruginosa 14-15 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1237428Bactericidal activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID563023Antimycobacterial activity against Mycobacterium tuberculosis 08-0787 harboring gyrA Asp94His mutant gene and deletion of codons 678 and 679 in gyrB mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID533364Antimicrobial activity against Bacteroides thetaiotaomicron assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID496641Antibacterial activity against Streptococcus pneumoniae 1149 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID521147Antibacterial activity against extracellular Listeria monocytogenes EGDe assessed as reduction in bacterial count at eight times of MIC after 6 hrs by time-kill study2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID1877403Antibacterial activity against Escherichia coli 2032022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID528835Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID556765fAUC/MIC in osteomyelitis patient cancellous bone at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 1 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID559538Antibacterial activity against Neisseria meningitidis assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID522984Antibacterial activity against Streptococcus pneumoniae isolate OC6608 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID425073Antimicrobial activity against Escherichia coli DH10B expressing pCR2.1 in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID533404Antimicrobial activity against Clostridium subterminale assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID559148Antimicrobial activity against Clostridium difficile 630c selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID633737Antibacterial activity against Escherichia coli 10-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID733005Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB A91V mutant-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID559190Antimicrobial activity against Clostridium difficile CD5C harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1604891Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6 mouse model of acute infection assessed as reduction in mycobacterial burden in lung at 100 mg/kg, po treated for 8 consecutive days starting from day 1 post-infection an2020Journal of medicinal chemistry, 03-12, Volume: 63, Issue:5
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.
AID279820Antimicrobial activity against Mycobacterium tuberculosis H3Rv on day 72007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID571357Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID574528Antimicrobial activity against Prevotella intermedia assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID498786Antimicrobial activity against strong ciprofloxacin-resistant Streptococcus pyogenes at 10 ug by disk diffusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID562936Upregulation of cwp84 gene expression in Clostridium difficile 6425 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID390114Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 10 mg/kg, iv administered as single dose 1 hr after bacterial challenge2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.
AID563332Upregulation of fbp68 gene expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1740325Antimicrobial activity against methicillin-resistant Staphylococcus aureus ATCC 33591 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID391987Antibacterial activity against Staphylococcus aureus RN4220 containing ORI23 promoter by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID581080Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID508387Antibacterial activity against macrolide-resistant Streptococcus pyogenes harboring mef(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID563039Antimycobacterial activity against Mycobacterium tuberculosis 08-0782 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID558628Antimicrobial activity against Streptococcus pneumoniae isolate 3681 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID572513Antimicrobial activity against Salmonella enterica serovar Mbandaka isolate s2159 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID562638Antimicrobial activity against Streptococcus mitis by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID528844Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID286044Susceptibility of Streptococcus pneumoniae BSP-2443 by microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID428769Bactericidal activity against Streptococcus pneumoniae isolate SR-23958 by broth dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID562441Antibacterial activity against Staphylococcus aureus SMH37312 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1164014Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 12-6 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID580893Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID570796Apparent oral clearance in healthy human at 400 mg, po qd measured on day 4 by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID574027Antibacterial activity against beta-lactamase producing Peptostreptococcus anaerobius assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID531851Clearance in tuberculosis patient at 400 mg/day, po administered for 7 days measured after 24 hrs by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID1181167Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_1 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID570923Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559491Antibacterial activity against Bacteroides fragilis assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID573564Antibacterial activity against beta-lactamase producing Bacteroides vulgatus assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID581107Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID283393Antimicrobial activity against Nocardia abscessus after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID544850Antibacterial activity against Streptococcus pneumoniae CIP104485 by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID559196Antimicrobial activity against Clostridium difficile CD5F harboring GyrB Ser416Ala mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID227416Fold reduction in minimum inhibitory concentration of antibiotic in presence of Reserpine2004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID559240Antibacterial activity against Streptococcus pneumoniae S001 harboring parC Asp83Asn mutant and wild-type gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID563335Upregulation of fbp68 gene expression in Clostridium difficile ATCC 43603-M1 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1256568Antibacterial activity against Enterococcus faecium 14-6 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID523298Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as 2 log reduction in bacterial burden in per lung at 30mg/kg, po2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID279835Drug level in Mycobacterium tuberculosis infected BALB/c mouse model at 38 to 19000 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID523308Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC4222 harboring gyrA S84L and parC S80F mutant gene assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID523141Antibacterial activity against Streptococcus pneumoniae isolate OC7348 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1297321Antibacterial activity against Escherichia coli 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID425349Antibacterial activity against Streptococcus pneumoniae HMC 1076 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1126758Antibacterial activity against drug-sensitive 1 ug/ml Mycobacterium tuberculosis clinical isolate 760 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID496639Ratio of 90% mutant prevention concentration to MIC90 in Streptococcus pneumoniae ATCC 496192010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID499671Antimicrobial activity against Bacillus subtilis ATCC 6633 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID532979Inhibition of DNA supercoiling activity of Mycobacterium tuberculosis DNA gyrase subunit A D94G mutant2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID373008Antimycobacterial activity against Mycobacterium avium complex N084 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID544301Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS1 harboring GyrA S84L and GrlA S80F mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID528836Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID521326AUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1297342Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-4 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID571879Antibacterial activity against Acinetobacter baumannii assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID572272Antimicrobial activity against Streptococcus pneumoniae ATCC 6301 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
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]
AID244934Minimum inhibitory concentration against Enterococcus faecalis ATCC 292122005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID425801AUC (0 to 24 hrs) in CD-1 mouse at 0.41 to 2.2 ug/kg administered through gavage2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID570891Antibacterial activity against Levofloxacin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID581089Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559529Antibacterial activity against Enterobacter aerogenes assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID528841Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID580861AUC in healthy human at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1297350Antibacterial activity against Enterococcus faecalis 14-1 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1877416Antibacterial activity against Neisseria gonorrhoeae WHO M2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID561314Antimicrobial activity against Enterobacter cloacae isolate 37 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID586730Ratio of mutant prevention concentration to MIC for Escherichia coli ATCC 259222011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID278602Inhibitory activity against Klebsiella pneumoniae 03-2222007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID1318926Antibacterial activity against Pseudomonas aeruginosa PAO12016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID425968Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 2527 after 14 passages with gemifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1398593Antibacterial activity against Streptococcus pyogenes ATCC 12344 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID1635217Antibacterial activity against Staphylococcus aureus ATCC 700699 by broth microdilution method2016Journal of natural products, Apr-22, Volume: 79, Issue:4
Metabolites from the Fungal Endophyte Aspergillus austroafricanus in Axenic Culture and in Fungal-Bacterial Mixed Cultures.
AID733006Inhibition of Mycobacterium leprae wild type DNA gyrase GyrA/GyrB-mediated DNA cleavable complex formation assessed as compound concentration inducing 25% DNA cleavage using relaxed pBR322 DNA substrate incubated for 1 hr at 30 degC by agarose gel electro2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of gatifloxacin derivatives and their biological activities against Mycobacterium leprae and Mycobacterium tuberculosis.
AID286156Bactericidal activity against Staphylococcus aureus BSP-2443 at fAUC/MIC of 31 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID581302Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID518627Ratio of AUC (0 to 24 hrs) in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic model to MIC for Mycobacterium avium at 50% maximal effective concentration2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID1468620Antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL6 mouse cornea assessed as mean corneal thickness at 0.3% administered tropically 2 times on day 1, 4 times on day 2 and 2 times on day 3 starting from 6 hrs post infection m2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo.
AID586745Antibacterial activity against qnrS gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrS1 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID523138Antibacterial activity against Streptococcus pneumoniae isolate OC7368 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581293Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1564358Antimycobacterial activity against Mycobacterium marinum NCTC 2275 by resazurin dye based fluorimetric assay2019European journal of medicinal chemistry, Nov-01, Volume: 181The synthesis and in vitro biological evaluation of novel fluorinated tetrahydrobenzo[j]phenanthridine-7,12-diones against Mycobacterium tuberculosis.
AID571344Antibacterial activity against Enterococcus faecium assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID279270Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 24 with GyrA S81Y, GyrB P413S and ParC S79F mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID286080fAUC/MIC ratio of Staphylococcus aureus ATCC 49610 at 200 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID559244Antibacterial activity against Streptococcus pneumoniae D001 harboring parC Ser79Phe and gyrA Gly85Lys mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID279209Antibacterial activity against Streptococcus pneumoniae 24 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID341080Plasma concentration in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID559380Antimicrobial activity against Clostridium difficile A422E harboring GyrB Leu451Phe mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID562442Antibacterial activity against Staphylococcus aureus SMH37390 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID580757Growth rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID425809Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung measured after 56 days after aerosol infection2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID562942Upregulation of cwp84 gene expression in Clostridium difficile CD196 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID521340Tmax in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID558917Antimicrobial activity against Clostridium difficile CD5h harboring GyrA Ala118Ser, Thr82Ala and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID572520Antimicrobial activity against qnrS-positive Salmonella enterica serovar Virginia isolate s2219 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID1067079Antimicrobial activity against Escherichia coli KCTC 1924 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1551295Antibacterial activity against Pseudomonas aeruginosa 2742 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID562654Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH367422009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID570809Ratio of Volume of distribution in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose to Volume of distribution in healthy human at 400 mg, po qd mea2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID765273fCmax/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1278839Antimycobacterial activity against Mycobacterium marinum ATCC BAA-535 infected in Zebra fish model assessed as reduction in bacterial load at 5 mg/kg, po administered for 7 days measured after 14 days by MPN assay2016Bioorganic & medicinal chemistry, Mar-15, Volume: 24, Issue:6
Design, synthesis and biological evaluation of imidazo[2,1-b]thiazole and benzo[d]imidazo[2,1-b]thiazole derivatives as Mycobacterium tuberculosis pantothenate synthetase inhibitors.
AID559170Antimicrobial activity against Clostridium difficile BI2d harboring GyrB Arg447Lys and Asp426Asn mutant gene selected after 32 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1242346Antimycobacterial activity against moxifloxacin resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA G88N mutant incubated for 7 days by microdilution method2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID580880Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1266236Inhibition of Mycobacterium tuberculosis DNA gyrase assessed as inhibition of supercoiling activity using relaxed pBR322 plasmid as substrate after 30 mins2016Bioorganic & medicinal chemistry, Jan-01, Volume: 24, Issue:1
Replacement of cardiotoxic aminopiperidine linker with piperazine moiety reduces cardiotoxicity? Mycobacterium tuberculosis novel bacterial topoisomerase inhibitors.
AID1524622Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID532679Antimicrobial activity against ciprofloxacin-nonsusceptible, AD PFGE pattern, emm6 type Streptococcus pyogenes with ST382 sequence type, ParC S79A mutant isolated from oropharyngeal colonization, tonsillitis/pharyngitis and skin/soft tissue infection2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID428782AUC (0 to 24 hrs) in human at 80 mg, po administered once a day2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID577499Bactericidal activity against Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model assessed as decrease in planktonic cell count at 400 mg every 24 hrs measured after 72 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID1819099Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 2 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID244953Minimum inhibitory concentration against Staphylococcus aureus ATCC 259232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1067080Antimicrobial activity against Streptococcus mutans 3065 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID586737Ratio of mutant prevention concentration to MIC for qnrS gene expressing Escherichia coli ATCC 25922 harboring GyrA S83L mutant and pBK-QnrS12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1237423Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3506 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID595856Inhibition of wild-type Staphylococcus aureus DNA gyrase assessed as inhibition of supercoiling of pBR322 DNA after 60 min by gel electrophoresis assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID1067074Antimicrobial activity against Salmonella typhimurium 1926 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID283169Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5258 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1868122Anti-tubercular activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth at 0.07 ug/ml incubated for 12 days by time-kill kinetics analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID522981Antibacterial activity against Streptococcus pneumoniae isolate OC7189 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID559160Antimicrobial activity against Clostridium difficile 630i harboring GyrB Asp26Val mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID496650Antibacterial activity against Streptococcus pneumoniae 3321 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID279838Fraction unbound ligand in mouse plasma at 0.01 to 10 mg/litre2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID279285Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79F and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID580752Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID521333fAUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1264561Antibacterial activity against Streptococcus pneumoniae 402 infected in sc dosed mouse assessed as reduction in 3 log CFU in lung compound administered as BID for 1 day measured 24 hrs after last dose2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID1868117Anti-tubercular activity against Mycobacterium tuberculosis CF76 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID425653Renal clearance in human2009Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15
Physicochemical determinants of human renal clearance.
AID1909947Antibacterial activity against Mycobacterium tuberculosis H37Rv assessed as inhibition of bacterial growth measured after 8 days by Alamar blue reagent based broth microdilution method2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID728917Antibacterial activity against Escherichia coli NIHJ after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID322775Antimicrobial activity against Bacteroides ovatus isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID456050Inhibition of Staphylococcus aureus wild type DNA gyrase2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID580903Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID572274Antimicrobial activity against multiple drug-resistant Streptococcus pneumoniae ATCC 700677 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID528845Antimicrobial activity against methicillin-resistant Staphylococcus epidermidis isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID285961Antimicrobial susceptibility against Haemophilus influenzae A4 isolate with GyrA Glu83Cys, ParC Ser84Arg and AcrR 97stop codon mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID428294Antimicrobial activity against Acinetobacter baumannii BM4652 expressing adeIJK genes with pAT807 isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID1067077Antimicrobial activity against Pseudomonas aeruginosa 2742 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1297336Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID575009Antimicrobial activity against Eubacterium sp. assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1398601Antibacterial activity against levofloxacin and methicillin-resistant Staphylococcus aureus 870307 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID575078Antimicrobial activity against Streptococcus pneumoniae serotype 35B assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID562463Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH375032009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID433582Selectivity index, ratio of IC50 for Mycobacterium leprae DNA gyrase subunit A A91V mutant to IC50 for Mycobacterium leprae wild type DNA gyrase A2B22008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID1430295Antibacterial activity against Enterococcus faecalis ATCC 29212 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID278860Antiproliferative effect against HeLa cells after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID508371Antibacterial activity against Streptococcus pneumoniae harboring erm(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID1181168Antimicrobial activity against first mutant generation Mycobacterium tuberculosis 1024_18 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID341065Plasma concentration in human at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID580873Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID556193P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side by measuring compound level at 50 uM after 180 mins2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID532959Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 32010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID433583Selectivity index, ratio of CC25 for Mycobacterium leprae DNA gyrase subunit A A91V mutant to CC25 for Mycobacterium leprae wild type DNA gyrase A2B2 by DNA cleavage assay2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
Are all the DNA gyrase mutations found in Mycobacterium leprae clinical strains involved in resistance to fluoroquinolones?
AID532021Antimicrobial activity against Mycobacterium ulcerans ATCC 19423 harboring pTY60H containing pCK0601 carrying the luxAB gene under the hsp60 promoter after 14 days determined according to CFU counts by bioluminescence method2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
Rapid assessment of antibacterial activity against Mycobacterium ulcerans by using recombinant luminescent strains.
AID428815Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-239582007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID532967Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 112010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID543399Cmax in plasma in Listeria monocytogenes EGD-e infected BALB/c mouse central nervous system listeriosis model at 50 mg/kg, ip administered 36 hrs postinfection as single dose2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID521101Antimicrobial activity against Streptococcus sp. 'group B' isolate 16 harboring gyrA Ser81Leu mutant, parC Ser79Tyr mutant and parE Ileu495Leu mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
AID581066Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID428292Antimicrobial activity against Acinetobacter baumannii BM4579 expressing deltaadeIJK genes isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID1557279Antibacterial activity against Escherichia coli by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID518624Clearance in Mycobacterium avium infected human THP1 cell-based pharmacokinetic-pharmacodynamic modell by LC analysis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID528970Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID544828Antimicrobial activity against Staphylococcus epidermidis Xen 43 biofilm assessed as log10 CFU/cm'2 in bacterial count2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Effect of electrical current on the activities of antimicrobial agents against Pseudomonas aeruginosa, Staphylococcus aureus, and Staphylococcus epidermidis biofilms.
AID1437922Antibacterial activity against Enterococcus faecium ATCC 700221 by broth microdilution method2017Journal of natural products, 01-27, Volume: 80, Issue:1
Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.
AID237458Partition coefficient (logD7.4)2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID425342Antibacterial activity against Streptococcus pneumoniae HMC 1149 harboring S81F and S79Y mutation in quinolone-resistant determining regions of GyrA and ParC genes respectively showing efflux to ciprofloxacin, gemifloxacin by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID425569Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA after 50 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID395717Antibacterial activity against Escherichia coli DH10B containing ORI23 promoter by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1380659Terminal half life in CD1 mouse plasma at 10 mg/kg, iv by LC-MS/MS analysis2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID544302Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS2 harboring GyrA S84L and GrlA S80F mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID544851Antibacterial activity against Streptococcus pneumoniae R6 by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID1447481Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate P259-96918 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1570249Tmax in SPF ICR mouse at 100 mg/kg, sc2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID1297343Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 14-6 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID523176Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11696 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1163998Antibacterial activity against extended-spectrum beta-lactamase producin Klebsiella pneumoniae 12-14 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID581479Total resistant organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID603879Antitubercular activity against replicating Mycobacterium tuberculosis H37Rv ATCC 27294 after 1 week by microplate alamar blue assay2011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Mycobacterium tuberculosis and cholinesterase inhibitors from Voacanga globosa.
AID1237402Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID570705Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID581311Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1207500Inhibition of rapid delayed inward rectifying potassium current (IKr) in Chinese hamster ovary (CHO) cells stable expressing hERG measured using IonWorks Barracuda automated patch clamp platform
AID508383Antibacterial activity against Streptococcus pyogenes harboring mef(A) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID520373Cardiotoxicity in patient with intracerebral and leptomeningeal tuberculosis assessed as QT prolongation at 400 mg/kg, po QID2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID372998Antimycobacterial activity against Mycobacterium avium complex N016 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID556764fAUC/MIC in osteomyelitis patient cortical bone at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 1 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID558602Antimicrobial activity against Streptococcus pneumoniae isolate 33 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID781329pKa (acid-base dissociation constant) as determined by other workers2014Pharmaceutical research, Apr, Volume: 31, Issue:4
Comparison of the accuracy of experimental and predicted pKa values of basic and acidic compounds.
AID1188156Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell viability at 100 uM after 48 hrs by MTT assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID428795Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-239582007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID522998Antibacterial activity against Streptococcus pneumoniae isolate OC6790 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID279290Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID341384Concentration in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit serum at 20 mg/kg, iv administered every 12 hrs measured 12 hrs after third dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID580867Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID372980Antimycobacterial activity against Mycobacterium avium complex N016 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID580879Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1380683Antibacterial activity against Escherichia coli infected in cyclophosphamide treated neutropenic CD1 mouse septicemia model assessed as mouse survival at 3 mg/kg, iv dosed at 1 hr post infection followed by redosing at 5 hrs post infection measured at 96 2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
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.
AID544842Antibacterial activity against Streptococcus pneumoniae U2A1413 harboring parC Ser79Tyr mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID553811Induction of cytotoxin production in Clostridium difficile PCR ribotype 027 in three-stage chemostat gut model at 32 mg/liter2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID496648Antibacterial activity against Streptococcus pneumoniae 1149 assessed as mutant prevention concentration by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID580749Antimicrobial activity against toxin and capsule gene-deficient Bacillus anthracis Sterne after 24 hrs by macrobroth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID570807Ratio of Half life in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose to Half life in healthy human at 400 mg, po qd measured on day 72008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID521102Antimicrobial activity against Streptococcus sp. 'group B' isolate 9 harboring gyrA Ser81Leu mutant, parC Ser79Tyr mutant and parE Ileu495Leu mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Emergence of fluoroquinolone resistance in group B streptococcal isolates in Taiwan.
AID570900Antibacterial activity against non-levofloxacin susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID245007Antibacterial activity against Staphylococcus epidermidis 56500 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID521339Tmax in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID580886Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1237410Antibacterial activity against Salmonella typhimurium 2421 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1207406Inhibition of slow delayed inward rectifying potassium current (Iks) in Chinese Hamster Ovary (CHO) cells transfected with KCNQ1 / Kv1.7 / KvLQT1 and KCNE1/minK measured using IonWorks automated patch clamp platform
AID571380Antibacterial activity against Klebsiella oxytoca assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID372983Antimycobacterial activity against Mycobacterium avium complex after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID558624Antimicrobial activity against Streptococcus pneumoniae isolate 3455 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID580899Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID573573Antibacterial activity against beta-lactamase producing Bacteroides uniformis assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID571113Antibacterial activity against methicillin-resistant Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID558928Antimicrobial activity against Clostridium difficile A422d selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1435842Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by resazurin reduction microplate assay2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID559542Antibacterial activity against non-ciprofloxacin-susceptible Pseudomonas aeruginosa assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID570805Ratio of Cmax in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose to Cmax in healthy human at 400 mg, po qd measured on day 5 post compound dose2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID584564Antimicrobial activity against Acinetobacter lwoffii isolate K expressing beta-lactamase OXA-58 isolated from blood culture of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID1348981AUC (0 to infinity) in ICR mouse at 50 mg/kg, po by HPLC analysis
AID1676591Binding affinity to Nickel cation assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1318936Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 847452016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID530346Antimicrobial activity against azide-resistant Escherichia coli J53 harboring pCTX-M plasmid carrying blaCTX-M-15 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID728915Antibacterial activity against Moraxella catarrhalis ATCC 25238 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID580751Antimicrobial activity against toxin and capsule gene-deficient Bacillus anthracis Sterne after 24 hrs by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1067083Antimicrobial activity against Staphylococcus aureus RN4220 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1819093Antimycobacterial activity against Mycobacterium tuberculosis H37Rv clinical isolates 1 assessed as reduction in bacterial growth incubated for 7 days by resazurin dye based assay2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID581064Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID523155Antibacterial activity against Streptococcus pneumoniae isolate OC6610 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1243288Antimicrobial activity against Streptococcus pyogenes ATCC 19615 by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID1256538Antibacterial activity against ESBL-positive Klebsiella pneumoniae 14-18 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1163986Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID558599Antimicrobial activity against Streptococcus pneumoniae 11 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID580889Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1676593Binding affinity to Gallium ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID571369Antibacterial activity against Klebsiella pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID558600Antimicrobial activity against Streptococcus pneumoniae 12 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID372996Antimycobacterial activity against Mycobacterium avium complex N016 infected C57BL/6J mouse assessed as lung bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1079943Malignant tumor, proven histopathologically. Value is number of references indexed. [column 'T.MAL' in source]
AID1154546Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 Y314H mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID563214Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2834 by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID608511Antibacterial activity against Escherichia coli KD652011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones.
AID532962Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 62010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID540216Clearance in dog after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
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).
AID1570242Selectivity index, ratio of CC50 for African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID341062AUC (0 to 24 hrs) in human at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID522938Antibacterial activity against Streptococcus pneumoniae isolate OC6608 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID563059Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2399 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID562644Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH367422009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID323889Antimicrobial activity against qnrA1 expressing Escherichia coli J53/pN5 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID530386Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA S69V, A71G, E72D, T73V, M74I, N76K, A83S, S84A, I85V, F96W and P101M mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
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.
AID556784Ratio of drug level in cancellous bone to serum in osteomyelitis patient at 400 mg, po administered for every 24 hrs by by three stage hierarchical Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID571354Antibacterial activity against Escherichia coli assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1185146Antimicrobial activity against moxicillin resistant Mycobacterium tuberculosis H37Rv ATCC 27294 containing DNA gyrase G88N mutant2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
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).
AID559201Antibacterial activity against Streptococcus pneumoniae S002 harboring parC Ser79Phe mutant and wild-type gyrA genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1704241Antibacterial activity against methicillin-resistant Staphylococcus aureus2020European journal of medicinal chemistry, Nov-15, Volume: 2061,2,3-Triazole-containing hybrids with potential antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
AID522990Antibacterial activity against Streptococcus pneumoniae isolate OC5462 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID553688Antimicrobial activity against Lactobacillus in three-stage chemostat gut model assessed as log reduction in bacterial count at 43 mg/liter administered daily for 7 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID1610997Bactericidal activity against methicillin-resistant Staphylococcus aureus ATCC 700699 assessed as reduction in bacterial CFU at 4 times MIC measured for 30 mins2019Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria.
AID558699Antimicrobial activity against Clostridium difficile A422 expressing tcdA and tcdB gene by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1294803Antibacterial activity against quinolone-resistant Streptococcus pneumoniae TPS3 in rat respiratory tract infection model assessed as decrease in bacterial burden in lung at 100 mg/kg, po bid administered through gavage at 1, 7, 24,31 hrs post infection m2016Bioorganic & medicinal chemistry letters, 05-15, Volume: 26, Issue:10
Novel tricyclics (e.g., GSK945237) as potent inhibitors of bacterial type IIA topoisomerases.
AID575103Antimicrobial activity against Streptococcus pneumoniae serotype 23A assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID523307Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC4222 harboring gyrA S84L and parC S80F mutant gene assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1740326Antimicrobial activity against methicillin-sensitive Staphylococcus aureus ATCC 9253 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID494413Antimycobacterial activity against Mycobacterium phlei CMCC 93201 after 72 hrs by serial double dilution method2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.
AID1447478Antibacterial activity against Pseudomonas aeruginosa PAO1 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID1888650Antibacterial activity against ciprofloxacin resistant Staphylococcus aureus harboring ParCS80F and GyrAS84L double mutant assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID534771Antimicrobial activity against Acinetobacter baumannii-calcoaceticus obtained from war-wounded patient assessed as susceptible isolates2010Antimicrobial agents and chemotherapy, Jul, Volume: 54, Issue:7
In vitro activity of the aminoglycoside antibiotic arbekacin against Acinetobacter baumannii-calcoaceticus isolated from war-wounded patients at Walter Reed Army Medical Center.
AID556028P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side at 50 uM in presence of 3 uM P-gp inhibitor PSC-8332009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID1398599Antibacterial activity against Moraxella catarrhalis ATCC 25238 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID342063Antimicrobial activity against nonepidemic Clostridium difficile J29 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID1297324Antibacterial activity against extended-spectrum beta-lactamase-producing Klebsiella pneumoniae 14-19 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID425559Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID695445Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 4-FQR3M BSA643 expressing GyrA Ser84Leu mutant and GrlA Ser80Tyr and Glu84Gly mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID572511Antimicrobial activity against Salmonella enterica serovar Typhimurium isolate s2878 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID601789Antibacterial activity against 10'4 CFU Klebsiella pneumoniae 09-22 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1676596Binding affinity to Ferric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID559398Antimicrobial activity against Clostridium difficile 630E harboring GyrA Ala118Val mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID285964Antimicrobial susceptibility against Haemophilus influenzae B2 isolate with GyrA Asp88Tyr and AcrR Leu31His mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID563046Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0757 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1398609Apparent partition coefficient, log P of the compound in CHCL3/03.1 M phosphate buffer at pH 7.42018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID422661Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1077 after 15 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID529900Antimicrobial activity against Leptospira interrogans serovar Icterohaemorrhagiae isolate 9 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1318963Antibacterial activity against extremely drug-resistant Pseudomonas aeruginosa isolate 104354 infected in Galleria mellonella assessed as larvae survival at 50 mg/kg administered as single dose measured after 24 hrs (Rvb = 27 %)2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID523310Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC2838 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1430296Antibacterial activity against Enterococcus faecalis ATCC 51299 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID558604Antimicrobial activity against Streptococcus pneumoniae isolate 1055 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID565327Antibacterial activity against Mycoplasma genitalium M6151 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID521336Cmax in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID559184Antimicrobial activity against Clostridium difficile C253F selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559527Antibacterial activity against Citrobacter freundii assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID520364Half-life in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID425985Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3243 after 20 passages with moxifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID575946Antimicrobial activity against erythromycin-resistant Streptococcus pneumoniae assessed as susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.
AID528842Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID530598Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr10 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID633639Antibacterial activity against Enterococcus faecium 09-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID580888Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID580878Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID544845Antibacterial activity against Streptococcus pneumoniae U2A1681 harboring parC Ser79Tyr Asp83Ala mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID1318935Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 831822016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID559243Antibacterial activity against Streptococcus pneumoniae S004 harboring wild-type parC and gyrA Gly85Asn mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID574807Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 761 horboring rpoB S531L/Q510P, katG S315T/R463L, gyrA D94N/S95T, rrs G1484T by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID261741Antibacterial activity against Salmonella Typhimurium ATCC 140282006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID556775Volume of distribution in central compartment in osteomyelitis patient at 400 mg, po administered for every 24 hrs by MAP-Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID581081Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1494127Antibacterial activity against tetracycline/methicillin-resistant Staphylococcus aureus XU212 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID759327Antibacterial activity against Staphylococcus aureus KCTC 209 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID581274Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563219Antimycobacterial activity against Mycobacterium tuberculosis 08-0771 harboring gyrA putative promoter mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID572514Antimicrobial activity against Salmonella enterica serovar Corvallis isolate s2064 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID511402Antibacterial activity against moxifloxacin resistant Neisseria gonorrhoeae isolates by broth dilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Comparative in vitro activities of nemonoxacin (TG-873870), a novel nonfluorinated quinolone, and other quinolones against clinical isolates.
AID523177Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC11696 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581301Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1524624Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1551293Antibacterial activity against Streptococcus mutans KCTC3289 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID1601843Antibacterial activity against Streptococcus pyogenes CMCC 32067 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID575081Antimicrobial activity against Streptococcus pneumoniae serotype 6C assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID581294Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID261734Antibacterial activity against Enterococcus faecium ATCC 490322006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID601792Antibacterial activity against 10'4 CFU Pseudomonas aeruginosa 09-32 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID520369Ratio of fAUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID571836Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID425550Antibacterial activity against penicillin-susceptible, quinolone-resistant Streptococcus pneumoniae 1072 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I460V muta2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID262138Inhibitory activity against wild type Staphylococcus aureus topoisomerase 42006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID593801Antimicrobial activity against Bacillus thuringiensis var.kurstaki BGSC 4D1 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID581486Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID586651Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrA gene and pBK-QnrA1 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1909946Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID372986Antimycobacterial activity against Mycobacterium avium JATA51-01 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1256551Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-1 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID563042Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 03-0738 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID533638Antimicrobial activity against Propionibacterium sp. assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID285958Antimicrobial susceptibility against Haemophilus influenzae A1 isolate with GyrA Glu83Cys, ParC Ser84Arg and AcrR 97stop codon mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID425987Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3243 after 33 passages with azithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID572516Antimicrobial activity against qnrS-positive Salmonella enterica serovar Montevideo isolate s2944 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID570699Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559519Antibacterial activity against Streptococcus intermedius assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285310Susceptibility of drug-selected vancomycin-resistant Enterococcus species mutant by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID422688Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3413 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID601785Antibacterial activity against 10'4 CFU Enterococcus faecium 08-2 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID279282Antimicrobial activity against Streptococcus pneumoniae R6 transformants with gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID425979Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1635 after 49 passages with clarithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID341380Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as reduction in bacterial burdens in blood culture at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID533134Antimicrobial activity against Bacteroides fragilis assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID562935Upregulation of slpA gene expression in Clostridium difficile 6269 at 0.5 times MIC by real-time PCR analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID698999Tmax in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID544835Antibacterial activity against Streptococcus pneumoniae U2A1686 harboring gyrA Glu85Lys mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID520372Ratio of fAUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID531727Antibacterial activity against Bacteroides vulgatus assessed as percent resistant isolates2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID562657Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH370992009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1330193Antifungal activity against Candida albicans 7535 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID558610Antimicrobial activity against Streptococcus pneumoniae isolate 1424 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID496643Antibacterial activity against Streptococcus pneumoniae 3321 by standard agar dilution method2010Antimicrobial agents and chemotherapy, Feb, Volume: 54, Issue:2
Comparative study of the mutant prevention concentrations of moxifloxacin, levofloxacin, and gemifloxacin against pneumococci.
AID574973Antimicrobial activity against Actinomyces israelii assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1330185Antibacterial activity against Staphylococcus aureus 503 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID425974Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 24 after 50 passages with moxifloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1600114Bactericidal activity against methicillin resistant Staphylococcus epidermidis ATCC 13199 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID530391Inhibition of Escherichia coli DNA gyrase GyrA/GyrB assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID581666Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth assessed as log reduction of extracellular CFU level after 24 hrs2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID528968Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID206629Antibacterial activity was determined against clinically isolated Levofloxacin-methicillin resistant Staphylococcus aureus (LVFX-r MRSA) strains (74 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1330189Antibacterial activity against Escherichia coli 1924 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID581292Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID422648Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3676 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID1297326Antibacterial activity against Klebsiella pneumoniae 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID559496Antibacterial activity against Propionibacterium acnes assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1348985Antimycobacterial activity against Mycobacterium tuberculosis H37Rv after 3 days by rapid direct susceptibility test
AID529901Antimicrobial activity against Leptospira interrogans serovar Icterohaemorrhagiae isolate 10 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID633649Antibacterial activity against Escherichia coli 09-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID425812Half life in mouse2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID574983Antimicrobial activity against Actinomyces naeslundii assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID530381Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1152758Antimycobacterial activity against wild-type Mycobacterium tuberculosis H37Rv ATCC 27294 after 16 to 18 days by BACTEC 7H12B microdilution method2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1743459Antitubercular activity against FQ resistant Mycobacterium tuberculosis H37Rv harboring gyrA Ser-91-Pro mutant measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID430967Antibacterial activity against Escherichia coli SKM18 containing gyrA L83, Y87 and parC L80, G84 mutants assessed as increase in MIC by Etest relative to MIC for Escherichia coli SKM9 containing gyrA L83, Y87 and parC L80 mutants2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID508381Antibacterial activity against macrolide-susceptible Streptococcus pyogenes after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID1430291Antibacterial activity against Staphylococcus aureus ATCC 25923 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID428797Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID508377Antibacterial activity against macrolide-resistant Streptococcus pneumoniae harboring erm(B) gene after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID341395Toxicity in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit assessed as calcification median score at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days after last dose by histopathology2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID1888651Antibacterial activity against Staphylococcus aureus harboring RpoBH481Y/ParCS80F/GyrAS84L triple mutant assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID1319009Selectivity ratio of MIC for Pseudomonas aeruginosa PAO1 to MIC for Pseudomonas aeruginosa PAO2002016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID369970Half life in Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID522992Antibacterial activity against Streptococcus pneumoniae isolate OC7376 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1256556Antibacterial activity against methicillin-resistant Staphylococcus aureus 14-5 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID520376Ratio of AUC (0 to 24 hrs) in plasma to CSF in patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QID2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID279258Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 1076 with ParC S79Y mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID586749Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrB gene and pBK-QnrB1 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID562658Ratio of AUC (0 to 24 hrs) to MIC required for 3-log drop in bacterial count in Staphylococcus aureus SMH373122009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID261743Antibacterial activity against Pseudomonas aeruginosa ATCC 278532006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID341389AUC (0 to 12 hrs) in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit at 20 mg/kg, iv administered every 12 hrs measured after seventh dose in presence of Dexamethasone2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID1605834In vivo antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL/6 mouse assessed as reduction in bacterial burden by measuring log10 CFU/cornea at 0.3% administered topically as two times on day 1, four times on day 2 and two tim2020Journal of medicinal chemistry, 04-09, Volume: 63, Issue:7
Rational Substitution of ε-Lysine for α-Lysine Enhances the Cell and Membrane Selectivity of Pore-Forming Melittin.
AID572269Antimicrobial activity against methicillin-susceptible Staphylococcus aureus ATCC 49951 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
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).
AID286096fAUC/MIC ratio of Staphylococcus aureus BSP-2443 at 100 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID562445Antibacterial activity against Staphylococcus aureus SMH38004 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
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.
AID1676601Binding affinity to Zinc ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID563012Antimycobacterial activity against Mycobacterium tuberculosis 02-1975 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID556025P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side at 50 uM in presence of in presence of 10 uM of p-glycoprotein and MRP transport inducer rifampin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID528840Antimicrobial activity against penicillin-resistant Streptococcus pneumoniae isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID572492Antimicrobial activity against Streptococcus pneumoniae ATCC 6303 infected in po dosed BALB/c mouse pneumonia model assessed as complete eradication of bacteria administered twice daily 3 days starting 16 hrs post infection2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID406808Antibacterial activity against Staphylococcus aureus ATCC 33591 isolate after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID544832Antibacterial activity against Streptococcus pneumoniae R6 by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID565322Antibacterial activity against Mycoplasma genitalium M6280 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID563342Induction of Cwp84 protease expression in Clostridium difficile CD07-259 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID428768Bactericidal activity against Streptococcus pneumoniae ATCC 49619 by broth dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID670862Antitubercular activity against non-replicating Mycobacterium tuberculosis assessed as minimum concentration required to inhibit 90% growth after 10 days under anaerobic condition by luciferase-based low-oxygen recovery assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
AID633643Antibacterial activity against Enterococcus faecium 09-6 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID559517Antibacterial activity against Streptococcus bovis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID323885Antimicrobial activity against Escherichia coli J53 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1297317Antibacterial activity against Escherichia coli ATCC 25922 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID285534Antibacterial activity against Staphylococcus aureus Mu50 at pH 52007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID529899Antimicrobial activity against Leptospira weilii isolate 8 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1570240Antimycobacterial activity against Mycobacterium tuberculosis H37Rv incubated for 7 days by rapid direct susceptibility test2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID570704Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID532978Inhibition of DNA supercoiling activitysof Mycobacterium tuberculosis DNA gyrase subunit A A90V mutant2010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID1524625Antifungal activity against Candida albicans 7535 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID369230Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae assessed as percent sensitive isolates by CLSI breakpoint method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Serotypes, Clones, and Mechanisms of Resistance of Erythromycin-Resistant Streptococcus pneumoniae Isolates Collected in Spain.
AID672349Antibacterial activity against Staphylococcus aureus ATCC 292132012Bioorganic & medicinal chemistry letters, Aug-01, Volume: 22, Issue:15
Synthesis, antitubercular and antimicrobial evaluation of 3-(4-chlorophenyl)-4-substituted pyrazole derivatives.
AID1557312AUC in human at 0.4 g, po by HPLC analysis2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID574043Antibacterial activity against beta-lactamase producing Peptoniphilus asaccharolyticus assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID528967Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient blood assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID544299Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu3 harboring GyrA S84L and GrlA S80F mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID765270AUC/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID765268T>MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID1723734Oral bioavailability in human at 400 mg measured every 12 hrs2020Bioorganic & medicinal chemistry letters, 10-15, Volume: 30, Issue:20
Novel C-7 carbon substituted fourth generation fluoroquinolones targeting N. Gonorrhoeae infections.
AID520370Ratio of fAUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID593802Antimicrobial activity against Staphylococcus aureus ATCC 6538 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID428858Bactericidal activity against Streptococcus pneumoniae isolate SR-23958 assessed as prevention of bacterial regrowth under condition simulating oral administration of 400 mg once daily after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID563010Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0797 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID588211Literature-mined compound from Fourches et al multi-species drug-induced liver injury (DILI) dataset, effect in humans2010Chemical research in toxicology, Jan, Volume: 23, Issue:1
Cheminformatics analysis of assertions mined from literature that describe drug-induced liver injury in different species.
AID559393Antimicrobial activity against Clostridium difficile 630C selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID558892Antimicrobial activity against Clostridium difficile C253g harboring GyrA Ala118Ser mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID581279Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID372992Antimycobacterial activity against Mycobacterium intracellular JATA52-01 infected C57BL/6J mouse assessed as spleen bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last do2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1297322Antibacterial activity against extended-spectrum beta-lactamase-producing Klebsiella pneumoniae 14-17 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID428295Antimicrobial activity against Acinetobacter baumannii BM4579 expressing adeIJK genes with pAT807 isolated from patient with urinary tract infection by agar dilution method2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID283161Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2588 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1877406Antibacterial activity against Pseudomonas aeruginosa 1422022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID342076Effect on growth of nonepidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID283168Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5256 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID586725Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrS gene and pBK-QnrS1 assessed as mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID323896Antimicrobial activity against Klebsiella pneumoniae C2/pMG252 GyrA Ser83Phe mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID1179480Antimycobacterial activity against Mycobacterium marinum ATCC 927 in 7H9 medium after 5 days and 6 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID528837Antimicrobial activity against vancomycin-resistant Enterococcus sp. isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID425581Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring I460V mutation in QRDR of ParE gene after 41 passages with gemifloxacin measured after 10 daily antibiotic-free s2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID261729Antibacterial activity against Escherichia coli ATCC 259222006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID556187P-glycoprotein-mediated transport in human Calu3 cells assessed as efflux ratio of permeability from apical to basolateral side over basolateral to apical side at 50 uM in presence of 10 uM of p-glycoprotein and MRP transport inducer rifampin2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID575101Antimicrobial activity against Streptococcus pneumoniae serotype 23B assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID425980Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1635 after 14 passages with azithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID633647Antibacterial activity against Escherichia coli 09-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID559379Antimicrobial activity against Clostridium difficile A422D harboring GyrB Leu451Phe mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID571855Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559188Antimicrobial activity against Clostridium difficile CD5A harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425777Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 after 22 passages by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1524628Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3505 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1524629Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by microtiter ELISA2019Bioorganic & medicinal chemistry letters, 05-01, Volume: 29, Issue:9
Synthesis of novel dihydrotriazine derivatives bearing 1,3-diaryl pyrazole moieties as potential antibacterial agents.
AID1664939Antimalarial activity against CQ-resistant Plasmodium falciparum NF54-R assessed as inhibition of parasite growth2020ACS medicinal chemistry letters, Jul-09, Volume: 11, Issue:7
Synthesis of Novel Ciprofloxacin-Based Hybrid Molecules toward Potent Antimalarial Activity.
AID580877Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1256554Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-4 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID529894Antimicrobial activity against Leptospira interrogans serovar Grippotyphosa isolate 2 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID428856Bactericidal activity against Streptococcus pneumoniae isolate SR-26137 assessed as reduction in number of viable cells under condition simulating oral administration of 400 mg once daily2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID405457Antibacterial activity against Escherichia coli C600Rif in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1256540Antibacterial activity against Klebsiella pneumoniae 14-1 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID498787Antimicrobial activity against ciprofloxacin-susceptible Streptococcus pyogenes harboring Asp91/Asn mutation in parC gene at 10 ug by disk diffusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID1256558Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-21 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID286158Bactericidal activity against Staphylococcus aureus BSP-2443 with parC S52G, N91D mutation and gyrA S81Y mutation at fAUC/MIC of 16 after 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID561328Antimicrobial activity against Klebsiella pneumoniae isolate 202 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID533408Antimicrobial activity against Clostridium tertium assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID531860Ratio of fAUC in patient with tuberculosis at 400 mg/day, po administered for 7 days to MIC for Mycobacterium tuberculosis2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID322774Antimicrobial activity against Bacteroides distasonis isolates by agar dilution method2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID456032Antibacterial activity against Escherichia coli NIHJ after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID559189Antimicrobial activity against Clostridium difficile CD5B harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID425579Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I462008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID544862Antibacterial activity against Streptococcus pneumoniae U2A1693 harboring parC Asp83Asn mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID581304Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1152778Antimycobacterial activity against moxifloxacin-resistant Mycobacterium tuberculosis harboring DNA gyraseA G88N mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1909945Cytotoxicity against human HepG2 cells assessed as reduction in cell viability by MTT assay2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID1740321Antimicrobial activity against Escherichia coli O157:H7 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID559515Antibacterial activity against Streptococcus pyogenes assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1437921Antibacterial activity against Enterococcus faecium ATCC 35667 by broth microdilution method2017Journal of natural products, 01-27, Volume: 80, Issue:1
Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.
AID285299Effect on 0.5 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID581313Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID285969Antimicrobial susceptibility against Haemophilus influenzae D isolate with AcrR Leu31His, Ile121Val and Gln134Lys mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID728924Antibacterial activity against Staphylococcus epidermidis 56500 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID581658Cmax in human plasma2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID573565Antibacterial activity against beta-lactamase producing Bacteroides vulgatus assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1318920Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 259-969182016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1194333Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 substrate incubated for 30 mins by ethidium bromide staining and electrophoresis based DNA supercoiling assay2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID1053500Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as parasite growth inhibition after 7 days by Alamar Blue assay2013Journal of medicinal chemistry, Nov-14, Volume: 56, Issue:21
Methyl-thiazoles: a novel mode of inhibition with the potential to develop novel inhibitors targeting InhA in Mycobacterium tuberculosis.
AID369981Cmax in human serum at 400 mg, po administered as single dose2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID563007Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0785 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1330191Antibacterial activity against Salmonella typhimurium 1926 measured after 24 hrs by two-fold serial dilution method2016Bioorganic & medicinal chemistry letters, 12-15, Volume: 26, Issue:24
Synthesis and biological evaluation of chalcone derivatives containing aminoguanidine or acylhydrazone moieties.
AID405463Antibacterial activity against Escherichia coli TOP10 in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1557314Protein binding in human at 0.4 g, po by HPLC analysis2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID523135Antibacterial activity against Streptococcus pneumoniae isolate OC6790 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1067081Antimicrobial activity against Staphylococcus aureus 503 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID571125Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1676597Binding affinity to cupric ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID571383Antibacterial activity against Enterobacter cloacae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID405114Antimicrobial activity against Vibrio splendidus 12B01 expressing plasmid-mediated QnrS-like quinolone resistance determinants2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID562621Antimicrobial activity against vancomycin-resistant Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID1750813Antibacterial activity against Fluoroquinolone-sensitive Staphylococcus aureus ATCC 49951 assessed as reduction in bacterial growth by CLSI based broth microdilution method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID1877404Antibacterial activity against Neisseria gonorrhoeae ATCC 194242022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID523157Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC8525 harboring wild type quinolone resistance-determining region by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID562625Antimicrobial activity against Group A Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID285529Antibacterial activity against ethidium bromide-resistant Staphylococcus aureus ATCC 29213 in presence of 20 ug/ml reserpine after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID279287Antimicrobial activity agaisnt Streptococcus pneumoniae R6 transformants with parC S79F and gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID322783Antimicrobial activity against Bacteroides fragilis assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID66576Antibacterial activity was determined against clinically isolated vancomycin-A resistant enterococci (VRE) strains (33 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1909952Selectivity ratio of MIC50 for wild type Mycobacterium tuberculosis H37Rv to MIC50 for Mycobacterium tuberculosis H37Rv gyrA -FDASTetON-1 hypomorph2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID275451Cytotoxicity against human Hep2 cell line after 72 hrs2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID581087Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID428786Fraction unbound in human serum at 400 mg, po2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1242344Antimycobacterial activity against 6-((1-(2-(7-chloro-2-oxo-1,8-naphthyridin-1(2H)-yl)ethyl)piperidin-4-ylamino)methyl)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one resistant Mycobacterium tuberculosis H37Rv harboring DNA gyraseA A74V mutant incubated for 7 days2015ACS medicinal chemistry letters, Jul-09, Volume: 6, Issue:7
Left-Hand Side Exploration of Novel Bacterial Topoisomerase Inhibitors to Improve Selectivity against hERG Binding.
AID574508Antimicrobial activity against Bacteroides distasonis assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID529902Antimicrobial activity against Leptospira interrogans serovar Pomona isolate 12 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1877398Antibacterial activity against Acinetobacter baumannii ATCC 196062022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID563338Induction of Cwp84 protease expression in Clostridium difficile CD196 M1 at 0.5 times MIC by immunoblot analysis2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID1079948Times to onset, minimal and maximal, observed in the indexed observations. [column 'DELAI' in source]
AID425966Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3274 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID523144Antibacterial activity against Streptococcus pneumoniae isolate OC7348 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1224811CL/F in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID574806Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 horboring rpoB S531L/G566R/I569L, katG S315T/R463L, gyrA A90V/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID562828Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0930 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID522986Antibacterial activity against Streptococcus pneumoniae isolate OC5462 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID565310Antibacterial activity against Mycoplasma genitalium G37 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID528969Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient respiratory tract assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID544838Antibacterial activity against Streptococcus pneumoniae U2A1266 harboring gyrA Ser81Cys mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID420668Inhibition of human ERG in MCF7 cells2009European journal of medicinal chemistry, May, Volume: 44, Issue:5
GRIND-based 3D-QSAR and CoMFA to investigate topics dominated by hydrophobic interactions: the case of hERG K+ channel blockers.
AID565321Antibacterial activity against Mycoplasma genitalium M6257 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID581078Total sensitive organism counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID544840Antibacterial activity against Streptococcus pneumoniae R6 Tr1 harboring parC Ser79Tyr mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID580869Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID369228Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae assessed as percent resistant isolates by microdilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Serotypes, Clones, and Mechanisms of Resistance of Erythromycin-Resistant Streptococcus pneumoniae Isolates Collected in Spain.
AID559506Antibacterial activity against Staphylococcus lugdunensis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1194334Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 7 days by microplate alamar blue assay method2015Bioorganic & medicinal chemistry, May-01, Volume: 23, Issue:9
Design and synthesis of novel quinoline-aminopiperidine hybrid analogues as Mycobacterium tuberculosis DNA gyraseB inhibitors.
AID1611012Induction of membrane integrity impairment in methicillin-resistant Staphylococcus aureus ATCC 700699 at 10 uM measured for 3 hrs by PI staining based fluorescence assay2019Bioorganic & medicinal chemistry, 12-01, Volume: 27, Issue:23
The plant-derived chalcone Xanthoangelol targets the membrane of Gram-positive bacteria.
AID577486Antimicrobial activity against methicillin-resistant Staphylococcus aureus N315 assessed as inhibition of bacterial biofilm formation by CLSI broth microdilution method2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID556774Apparent total clearance in osteomyelitis patient at 400 mg, po administered for every 24 hrs by three stage hierarchical Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID574754Antimicrobial activity against Anaerococcus prevotii assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID565316Antibacterial activity against Mycoplasma genitalium UTMB-10G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID279278Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID562825Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 03-0738 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID285962Antimicrobial susceptibility against Haemophilus influenzae B isolate with AcrR Leu31His mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID530350Antimicrobial activity against Escherichia coli TOP10 by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID570987Tmax in healthy human assessed as 25-desacetyl-rifapentine level at 900 mg, po administered as a single dose measured on day 5 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID1318905Antibacterial activity against methicillin-resistant Staphylococcus epidermidis isolate CAN-ICU 61589 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID581484Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID559409Antimicrobial activity against Clostridium difficile BI2D harboring GyrB Glu466Lys mutant gene selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID563052Antimycobacterial activity against Mycobacterium tuberculosis 02-1975 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID570797Volume of distribution in healthy human at 400 mg, po qd measured on day 4 by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID430968Antibacterial activity against Escherichia coli 1608 containing gyrA L83 mutant assessed as increase in MIC by Etest relative to MIC for wild type Escherichia coli 16092007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID428794Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae ATCC 496192007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID595857Antibacterial activity against methicillin- and quinolone-resistant Staphylococcus aureus ATCC700699 after 24 hrs by microdilution method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID283167Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL5254 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID599556Antimycobacterial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 after 7 days by microplate alamar blue assay2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Facile transformation of Biginelli pyrimidin-2(1H)-ones to pyrimidines. In vitro evaluation as inhibitors of Mycobacterium tuberculosis and modulators of cytostatic activity.
AID1163990Antibacterial activity against extended-spectrum beta-lactamase producing Escherichia coli 12-14 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1164016Antibacterial activity against Streptococcus pneumoniae 12-18 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1740330Antifungal activity against Fusarium solani ATCC 36031 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID571107Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1152776Antimycobacterial activity against 2-oxo-1-(2-(4-((3-oxo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino)piperidin-1-yl)ethyl)-1,2-dihydroquinoline-7-carbonitrile-resistant Mycobacterium tuberculosis harboring DNA gyraseA A74V mutant2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID1743439Antitubercular activity against Mycobacterium tuberculosis H37Rv measured after 7 days by resazurin microtiter assay2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID279260Antibacterial activity against azithromycin resistance selected Streptococcus pneumoniae 1077 with 23S rRNA A2058G mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID1188155Antibacterial activity against Mycobacterium tuberculosis H37Rv after 7 days by microplate alamar blue assay method2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID1237426Bactericidal activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID581290Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID520377Hepatotoxicity in patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID436986Inhibition of human MG63 cell proliferation assessed as bromodeoxyuridine incorporation during DNA synthesis after 48 hrs by ELISA2009Bioorganic & medicinal chemistry, Aug-01, Volume: 17, Issue:15
7-((4-Substituted)piperazin-1-yl) derivatives of ciprofloxacin: synthesis and in vitro biological evaluation as potential antitumor agents.
AID341386AUC (0 to 12 hrs) in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit at 20 mg/kg, iv administered every 12 hrs measured after seventh dose2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID341073AUC (0 to 24 hrs) in human with MDR1 3435 CC genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID1688199Antimycobacterial activity against dormant form of Mycobacterium tuberculosis H37Rv assessed as log fold reduction in bacterial count at 10 ug/ml under nutrient starvation condition after 7 days by MPN assay2020European journal of medicinal chemistry, Feb-15, Volume: 188Novel benzimidazole-acrylonitrile hybrids and their derivatives: Design, synthesis and antimycobacterial activity.
AID342067Antimicrobial activity against fluoroquinolone-susceptible nonepidemic Clostridium difficile strain6 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID530378Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA M74I and A83S mutant/GyrB R447K mutant gene2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID570801Half life in healthy human at 400 mg, po qd coadministered with 900 mg, po thrice weekly of rifapentine on day 5 post compound dose measured on day 19 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID1877401Antibacterial activity against Escherichia coli ATCC 352182022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID1256553Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-3 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1551296Antifungal activity against Candida albicans 7535 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID425807Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID580898Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1399839Antibacterial activity against Mycobacterium smegmatis ATCC 194202018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID571877Antibacterial activity against Acinetobacter baumannii assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1254072Antibacterial activity against Escherichia coli CCARM 1356 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID558911Antimicrobial activity against Clostridium difficile CD5h harboring GyrA Ala92Glu and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID388879Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 10 mg/kg, iv administered as single dose 24 hrs after bacterial challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID1750816Lipophilicity, logD of compound in octanol and water at pH 7.4 incubated overnight by LC/UV/qTOF method2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID530369Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA A83S mutant2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID532680Antimicrobial activity against ciprofloxacin-nonsusceptible, AD PFGE pattern, emm1 type Streptococcus pyogenes with ST382 sequence type, ParC S79A mutant isolated from oropharyngeal colonization and onsillitis/pharyngitis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID560260Antimicrobial activity against Salmonella enterica serovar Typhimurium transconjugant p61/9T expressing qnrB19 gene variant carried by IncL/M-like plasmid by Etest2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Characterization of the plasmid-borne quinolone resistance gene qnrB19 in Salmonella enterica serovar Typhimurium.
AID571839Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID424330Antimicrobial activity against Dialister invisus assessed as susceptibility breakpoint by CLSI method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID558603Antimicrobial activity against Streptococcus pneumoniae isolate 37 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1602935Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 3 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID208626Antibacterial activity was determined against clinically isolated penicillin resistant Streptococcus pneumoniae (PRSP) strains (50 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID521151Antibacterial activity against intracellular Listeria monocytogenes EGDe infected in bone marrow-derived BALB/c mouse macrophage assessed as reduction in bacterial count at four-eitght times of MIC after 3 hrs2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID425765Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 228 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I4602008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID499680Antimicrobial activity against Haemophilus influenzae ATCC 19418 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID1551298Antibacterial activity against Methicillin-resistant Staphylococcus aureus CCARM 3506 assessed as reduction in bacterial cell growth incubated for 24 hrs by ELISA2019European journal of medicinal chemistry, Jun-15, Volume: 172Synthesis and biological evaluation of tryptophan-derived rhodanine derivatives as PTP1B inhibitors and anti-bacterial agents.
AID206650Antibacterial activity was determined against clinically isolated Levofloxacin-methicillin resistant Staphylococcus aureus (LVFX-r MRSA) strains (74 strains)2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID581271Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID580860Oral bioavailability in healthy human at 400 mg/kg, po2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID1514454Antitubercular activity against d-cycloserine-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID405118Antimicrobial activity against Escherichia coli TOP10 harbouring pS1 plasmid expressing quinolone resistant QnrS1 gene2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID1224809CL/F in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID529904Antimicrobial activity against Leptospira interrogans serovar Canicola isolate 11 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID1430293Antibacterial activity against Escherichia coli ATCC 25922 incubated after 24 hrs by resazurin dye based broth microdilution assay2017Bioorganic & medicinal chemistry letters, 03-01, Volume: 27, Issue:5
New 1,4-dihydro[1,8]naphthyridine derivatives as DNA gyrase inhibitors.
AID1256548Antibacterial activity against Pseudomonas aeruginosa 14-16 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1740324Antimicrobial activity against Pseudomonas aeruginosa ATCC 9627 assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID425556Antibacterial activity against quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 441 expressing ermB by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID573595Antibacterial activity against Fusobacterium nucleatum assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID558923Antimicrobial activity against Clostridium difficile A422b selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID244721Frequency of resistance emergence for methicillin resistant Staphylococcus aureus-332005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID522982Antibacterial activity against Streptococcus pneumoniae isolate OC7189 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID563054Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2230 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
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]
AID261731Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 7006992006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID323893Antimicrobial activity against Escherichia coli J53/p1132 negative GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID633635Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 10-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID424328Antimicrobial activity against Dialister invisus by agar dilution method2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Antimicrobial susceptibilities and clinical sources of Dialister species.
AID1868116Anti-tubercular activity against Mycobacterium tuberculosis CF61 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID530345Antimicrobial activity against Escherichia coli BicA expressing blaTEM-1, blaCTX-M-15 and qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID428779Ratio of mutant prevention concentration for Streptococcus pneumoniae isolate SR-26137 to MIC for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1871982Antimycobacterial activity against Mycobacterium tuberculosis2022European journal of medicinal chemistry, Feb-05, Volume: 229Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.
AID1652707Induction of Escherichia coli K12 MG1655 lexA promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID405458Antibacterial activity against Escherichia coli C600Rif containing pIP1206 plasmid by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID601703Antibacterial activity against 10'4 CFU Staphylococcus aureus ATCC 25923 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID285957Antimicrobial susceptibility against Haemophilus influenzae A isolate with GyrA Glu83Cys and AcrR 97stop codon mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID275465Antibacterial activity against methicillin-sensitive Staphylococcus aureus2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID575083Antimicrobial activity against multiple drug resistant Streptococcus pneumoniae serotype 19F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID1079939Cirrhosis, proven histopathologically. Value is number of references indexed. [column 'CIRRH' in source]
AID279289Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y and gyrA S81Y mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID570674Antibacterial activity against Pseudomonas aeruginosa by CLSI M7-A7 broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID523181Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC8530 harboring gyrA S84L and parC I143V mutant gene assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID494415Antimycobacterial activity against Mycobacterium tuberculosis 09710 after 72 hrs by serial double dilution method2010European journal of medicinal chemistry, Aug, Volume: 45, Issue:8
Synthesis and in vitro antimycobacterial activity of balofloxacin ethylene isatin derivatives.
AID428855Bactericidal activity against Streptococcus pneumoniae isolate SR-26134 assessed as reduction in number of viable cells under condition simulating oral administration of 400 mg once daily2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID563022Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 04-0519 harboring gyrA Ala90Val and Asp94Asn mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID529895Antimicrobial activity against Leptospira interrogans serovar Icterohaemorrhagiae isolate 3 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID581276Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID635056Antibacterial activity against methicillin-resistant Staphylococcus aureus 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID286063Half life at 400 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1318937Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 853222016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID584566Antimicrobial activity against Acinetobacter lwoffii isolate M expressing beta-lactamase OXA-58 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID558916Antimicrobial activity against Clostridium difficile CD5 2-g harboring GyrA Ala118Ser, Thr82Ala and GyrB Ser416Ala mutant genes selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID580892Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID422645Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3676 after 14 passages with Telithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID558874Antimicrobial activity against Clostridium difficile BI2 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID571927Ratio of MIC for Escherichia coli K-12 3-AG300 harboring acrB::rpsLneo mutant gene to MIC for Escherichia coli K-12 3-AG3002009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID1075036Bactericidal activity against Mycobacterium tuberculosis H37Rv assessed as log reduction of bacterial CFU at 1.2 ug/mL after 1 week2014Journal of medicinal chemistry, Feb-27, Volume: 57, Issue:4
Encoded library technology as a source of hits for the discovery and lead optimization of a potent and selective class of bactericidal direct inhibitors of Mycobacterium tuberculosis InhA.
AID523163Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC17042 harboring gyrA S84L/G106D, parC S80F and parE D732N mutant gene by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1297344Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-22 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID533400Antimicrobial activity against Clostridium paraputrificum assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID574496Antimicrobial activity against Bacteroides fragilis assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID341388Concentration in Staphylococcus aureus infection-induced aortic valve endocarditis rabbit serum at 20 mg/kg, iv administered every 12 hrs measured 12hrs after seventh dose in presence of Dexamethasone2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID1437917Antibacterial activity against Staphylococcus aureus ATCC 25923 by broth microdilution method2017Journal of natural products, 01-27, Volume: 80, Issue:1
Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.
AID1557282Antibacterial activity against Bacteroides fragilis by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID279208Antibacterial activity against Streptococcus pneumoniae 19 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID593799Antimicrobial activity against Bacillus megaterium ATCC 19213 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID561320Antimicrobial activity against Escherichia coli isolate 17 transconjugant expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID728910Antibacterial activity against Chlamydophila pneumoniae CM-1 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID563031Antimycobacterial activity against Mycobacterium tuberculosis 08-0771 harboring gyrA putative promoter mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID573574Antibacterial activity against beta-lactamase producing Bacteroides uniformis assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID521831Antimicrobial activity against Streptococcus pneumoniae isolated from meningitis patient assessed as percent resistant isolates by CLSI method2008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Clonal spread of highly beta-lactam-resistant Streptococcus pneumoniae isolates in Taiwan.
AID528971Antimicrobial activity against methicillin-resistant Staphylococcus aureus isolated from ICU patient urine assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1398614Inhibition of CYP3A4 in human liver microsomes at 10 uM assessed as remaining activity by measuring 1'-hydroxylation of midazolam after 30 mins2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID261733Cytotoxicity against Hep2 cell line2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID533396Antimicrobial activity against Clostridium innocuum assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID558631Antimicrobial activity against Streptococcus pneumoniae isolate 4755 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID559242Antibacterial activity against Streptococcus pneumoniae S003 harboring wild-type parC and gyrA Ser81Phe mutant genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID341078Plasma concentration in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID581655Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient at pH 7.4 after 48 hrs by broth microdilution method in presence of thymidine2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID561329Antimicrobial activity against azide-resistant Escherichia coli J532009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID586738Antibacterial activity against Escherichia coli ATCC 25922 assessed as earliest time required to resistant colonies visible one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID1318933Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 791992016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1691028Antitubercular activity against 6-weeks nutrient starved phase cultures of Mycobacterium tuberculosis H37Rv assessed as log reduction in bacterial growth at 10 uM treated for 7 days measured after 4 weeks relative to control2020European journal of medicinal chemistry, May-01, Volume: 193Design and development of ((4-methoxyphenyl)carbamoyl) (5-(5-nitrothiophen-2-yl)-1,3,4-thiadiazol-2-yl)amide analogues as Mycobacterium tuberculosis ketol-acid reductoisomerase inhibitors.
AID695233Antibacterial activity against methicillin-resistant Staphylococcus aureus ATCC 7006992011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID425762Antibacterial activity against penicillin-, macrolide-susceptible and quinolone-resistant Streptococcus pneumoniae HMC 1074 harboring S81F, E85K mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID285963Antimicrobial susceptibility against Haemophilus influenzae B1 isolate with GyrA Asp88Tyr and AcrR Leu31His mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID532958Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 22010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID528978Antimicrobial activity against methicillin-susceptible Staphylococcus aureus assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID584558Antimicrobial activity against Acinetobacter lwoffii isolate E expressing beta-lactamase OXA-164 isolated from tracheal secretion of patient by vitek 2 system2010Antimicrobial agents and chemotherapy, Dec, Volume: 54, Issue:12
In vivo selection of a missense mutation in adeR and conversion of the novel blaOXA-164 gene into blaOXA-58 in carbapenem-resistant Acinetobacter baumannii isolates from a hospitalized patient.
AID279205Antibacterial activity against Streptococcus pneumoniae 3665 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
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).
AID558625Antimicrobial activity against Streptococcus pneumoniae isolate 3458 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID759324Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by broth microdilution method2013Bioorganic & medicinal chemistry letters, Aug-01, Volume: 23, Issue:15
Synthesis and biological evaluation of rhodanine derivatives bearing a quinoline moiety as potent antimicrobial agents.
AID1179478Antimycobacterial activity against Mycobacterium abscessus ATCC 19977 in 7H9 medium after 3 days and 4 hrs after adding resazurin dye/Tween 80 by Microplate Alamar Blue assay2014Bioorganic & medicinal chemistry letters, Aug-01, Volume: 24, Issue:15
Scaffold-switching: an exploration of 5,6-fused bicyclic heteroaromatics systems to afford antituberculosis activity akin to the imidazo[1,2-a]pyridine-3-carboxylates.
AID574756Antimicrobial activity against Anaerococcus prevotii assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID1685387Potentiation of conjugate 12-induced antibacterial activity against wild type Pseudomonas aeruginosa PAO1 assessed as conjugate 12 MIC measured after 18 hrs by CLSI protocol based microbroth dilution method (Rvb = 64 to 128 ug/ml)2019MedChemComm, Apr-01, Volume: 10, Issue:4
Polybasic peptide-levofloxacin conjugates potentiate fluoroquinolones and other classes of antibiotics against multidrug-resistant Gram-negative bacteria.
AID586750Antibacterial activity against Escherichia coli ATCC 25922 expressing qnrS gene and pBK-QnrS1 assessed as resistant colonies recovered one step below mutant prevention concentration2011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID207483Antibacterial activity was determined against Staphylococcus aureus FDA 209-P strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1819727Antimycobacterial activity against Mycobacterium abscessus subsp. abscessus bamboo strain assessed as inhibition of mycobacterial growth incubated for 3 days by broth microdilution method2022ACS medicinal chemistry letters, Mar-10, Volume: 13, Issue:3
Structure-Activity Relationship of Anti-
AID425346Antibacterial activity against Streptococcus pneumoniae HMC 1066 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID558888Antimicrobial activity against Clostridium difficile C253f selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559504Antibacterial activity against Staphylococcus haemolyticus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID562461Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH373122009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID574796Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2911 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID244891Minimum inhibitory concentration against Escherichia coli ATCC 259222005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1163992Antibacterial activity against Klebsiella pneumoniae 12-1 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID1067075Antimicrobial activity against Salmonella typhimurium 2421 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID559513Antibacterial activity against levofloxacin susceptible Streptococcus pneumoniae assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID581284Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1067072Antimicrobial activity against methicillin-resistant Staphylococcus aureus clinical isolate 3167 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID279266Antibacterial activity against azithromycin resistance selected Streptococcus pneumoniae 3243 with L22 insertion 93SFRPRA94 mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID570928Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID499673Antimicrobial activity against Staphylococcus epidermidis ATCC 12228 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID518621Antimicrobial activity against Mycobacterium avium subsp. hominissuis ATCC 700898 infected in human THP1 cells in presence of 2% FBS2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID1254069Antibacterial activity against Staphylococcus aureus 503 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID573600Antibacterial activity against Fusobacterium mortiferum assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID556349Antimicrobial activity against macrolide-resistant Mycoplasma pneumoniae ATCC 15531 by broth microdilution method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Antimicrobial susceptibility of Mycoplasma pneumoniae isolates and molecular analysis of macrolide-resistant strains from Shanghai, China.
AID428807Ratio of Cmax in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID286073Half life at 800 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID563014Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2230 harboring gyrA Asp94Gly mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID422659Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1077 after 29 passages with azithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID428784AUC (0 to 24 hrs) in human at 200 mg, po administered twice a day2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID573799Antibacterial activity against Prevotella buccae assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID532682Antimicrobial activity against ciprofloxacin-nonsusceptible, DX PFGE pattern, emm6 type Streptococcus pyogenes with ST382 sequence type, ParC S79A mutant isolated from oropharyngeal colonization2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID521338Tmax in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID562447Antibacterial activity against Staphylococcus aureus SMH36742 by broth dilution method2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID391986Antibacterial activity against Staphylococcus aureus RN4220 by twofold dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Role of a qnr-like gene in the intrinsic resistance of Enterococcus faecalis to fluoroquinolones.
AID1909943Kinetic solubility of compound at 200 uM incubated for 20 hrs by shake flask method based HPLC-DAD analysis2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID244924Antibacterial activity against Streptococcus mitis IID685 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID573797Antibacterial activity against Prevotella intermedia assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID499672Antimicrobial activity against Staphylococcus aureus ATCC 6538 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID559521Antibacterial activity against Streptococcus oralis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID532972Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 162010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID428809Ratio of Cmax in human at 80 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID571342Antibacterial activity against Enterococcus faecium assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID593901Inhibition of Escherichia coli DNA gyrase assessed as reduction of DNA supercoiling activity using pBR322 DNA substrate after 30 mins by electrophoresis2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID285970Antimicrobial susceptibility against Haemophilus influenzae D1 isolate with GyrA Ser84Tyr, ParC Glu88Lys and AcrR Leu31His, Ile121Val and Gln134Lys mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID559535Antibacterial activity against Legionella pneumophila assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID390106Binding affinity to bone assessed as drug level bound to cattle bone meal powder by fluorescence assay2008Journal of medicinal chemistry, Nov-13, Volume: 51, Issue:21
Linking bisphosphonates to the free amino groups in fluoroquinolones: preparation of osteotropic prodrugs for the prevention of osteomyelitis.
AID498192Antibacterial activity against Stenotrophomonas maltophilia MBS100 deficient in Smqnr gene by epsilon test2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
SmQnr contributes to intrinsic resistance to quinolones in Stenotrophomonas maltophilia.
AID562460Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH370992009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID1494126Antibacterial activity against Staphylococcus aureus EMRSA-15 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID279825Cmax in BALB/c mouse at 6 to 400 mg/kg, po2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID261732Inhibitory activity against Staphylococcus aureus ATCC 29213 wild type Topo 42006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID1254067Antibacterial activity against Staphylococcus aureus RN4220 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID368419Antimicrobial activity against Escherichia coli KAM32 expressing deltaacrB ydhE hsd gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID425070Antimicrobial activity against multidrug-resistant Escherichia coli M7943-TC2 bearing qnrB10 gene with aac(6)-Ib-cr-blaOXA-30 catB3-arr-3 integron in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID558900Antimicrobial activity against Clostridium difficile CD5c harboring GyrB Ser416Ala mutant gene selected after 2 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID428838TMSW in Streptococcus pneumoniae isolate SR-26134 infected human at 80 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1877409Antibacterial activity against Staphylococcus aureus ATCC 292132022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID523159Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC12501 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID529897Antimicrobial activity against Leptospira interrogans serovar Pyrogenes isolate 5 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID558626Antimicrobial activity against Streptococcus pneumoniae isolate 3481 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID571768Antimicrobial activity against Escherichia coli K-12 3-AG300 harboring AcrB-I626M mutant gene2009Antimicrobial agents and chemotherapy, Jan, Volume: 53, Issue:1
Site-directed mutagenesis reveals amino acid residues in the Escherichia coli RND efflux pump AcrB that confer macrolide resistance.
AID571867Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID558619Antimicrobial activity against Streptococcus pneumoniae isolate 3275 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID571854Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID244877Antibacterial activity against Escherichia coli NIHJ was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID278863Increase in lactate production in primary human osteoblasts at 25 to 50 ug/ml by ELISA2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID670861Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as minimum concentration required to inhibit 90% growth after 1 week by fluorescence-based microplate Alamar Blue assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
AID558598Antimicrobial activity against Streptococcus pneumoniae 10 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1557285Antibacterial activity against Streptococcus pneumoniae by agar diffusion method2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID558886Antimicrobial activity against Clostridium difficile C253d selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID533384Antimicrobial activity against Bacteroides nordii assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID571866Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID261740Antibacterial activity against Stenotrophomonas maltophilia ATCC 136372006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID425766Antibacterial activity against penicillin-resistant and quinolone-susceptible Streptococcus pneumoniae HMC 3583 expressing mefA and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, D83N mutation in QRDR of ParC gene and I462008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID286150Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 63 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
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.
AID1297333Antibacterial activity against Pseudomonas aeruginosa 14-16 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID559502Antibacterial activity against ciprofloxacin-susceptible and methicillin-resistant Staphylococcus epidermidis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID563027Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0794 harboring gyrA Thr80Ala mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID575100Antimicrobial activity against Streptococcus pneumoniae serotype 22F assessed as percent susceptible isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Activity of ceftaroline against recent emerging serotypes of Streptococcus pneumoniae in the United States.
AID571868Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559543Antibacterial activity against levofloxacin susceptible Serratia marcescens assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1196884Antimycobacterial activity against dormant Mycobacterium tuberculosis H37Rv model assessed as log reduction at 10 ug/ml incubated for 7 days measured after 28 days in presence of nutrient deprived condition2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID565330Antibacterial activity against Mycoplasma genitalium M6284 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID559525Antibacterial activity against Acinetobacter calcoaceticus assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID601788Antibacterial activity against 10'4 CFU Escherichia coli 08-21 after 18 hrs by CLSI agar dilution method2011European journal of medicinal chemistry, Jun, Volume: 46, Issue:6
Synthesis and in vitro antibacterial activity of 7-(3-alkoxyimino-4-amino-4-methylpiperidin-1-yl) fluoroquinolone derivatives.
AID1181170Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_8.12 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID1398612Metabolic stability in human microsomes at 1 uM assessed as compound remaining after 30 mins2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID574967Antimicrobial activity against Actinomyces odontolyticus assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID428817Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID422687Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3413 by NCCLS M7-A7 method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID530588Antimicrobial activity against Escherichia coli TOP10 by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID558595Antimicrobial activity against Streptococcus pneumoniae 7 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID1655162Bacteriostatic activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth at 0.07 ug/ml incubated for 3 to 4 weeks by time kill assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Improving the Potency of
AID237037Dissociation constant (pKa) was determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID521332fAUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1437919Antibacterial activity against Enterococcus faecalis ATCC 29212 by broth microdilution method2017Journal of natural products, 01-27, Volume: 80, Issue:1
Antibacterial and Cytotoxic Phenolic Metabolites from the Fruits of Amorpha fruticosa.
AID283160Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2554 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID1585701Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 09710 by rapid direct susceptibility test2019European journal of medicinal chemistry, Jan-15, Volume: 162Fluoroquinolone-isatin hybrids and their biological activities.
AID428843Time above the mutant prevention concentration in Streptococcus pneumoniae ATCC 49619 infected human at 400 mg, po administered once daily after 24 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID574744Antimicrobial activity against Peptostreptococcus anaerobius assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID278596Inhibitory activity against Klebsiella pneumoniae 12-11832007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID499675Antimicrobial activity against quinolone and penicillin-resistant Staphylococcus epidermidis SER after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID520378Hepatotoxicity in patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID559404Antimicrobial activity against Clostridium difficile BI2B selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID586732Ratio of mutant prevention concentration to MIC for Escherichia coli ATCC 25922 expressing qnrB gene and pBK-QnrB12011Antimicrobial agents and chemotherapy, Mar, Volume: 55, Issue:3
In vitro effect of qnrA1, qnrB1, and qnrS1 genes on fluoroquinolone activity against isogenic Escherichia coli isolates with mutations in gyrA and parC.
AID425551Antibacterial activity against penicillin-, macrolide- and quinolone-susceptible Streptococcus pneumoniae HMC 63 by broth microdilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1602936Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 4 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID515918Antibacterial activity against isoniazid-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID581065Hill constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID508385Antibacterial activity against Streptococcus pyogenes harboring mutation in L4 ribosomal protein after overnight incubation by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
In vitro activity of CEM-101 against Streptococcus pneumoniae and Streptococcus pyogenes with defined macrolide resistance mechanisms.
AID581092Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1297329Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1318904Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis isolate CANWARD-2008 81388 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1297346Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-39 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID581275Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID695444Antibacterial activity against fluoroquinolone resistant Staphylococcus aureus 3-FQR3M ATCC 700699 expressing GyrA Ser84Leu mutant and Glu409Lys mutant and GrlA Ser80Phe mutant2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID69933Antibacterial activity was determined against Escherichia coli NIHJ strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID1607522Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in C57BL/6J mouse assessed as reduction in bacterial burden in lung at 100 mg/kg, po administered once daily for 4 consecutive days starting from 5 days post infection and measur2020Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10
Optimization of Hydantoins as Potent Antimycobacterial Decaprenylphosphoryl-β-d-Ribose Oxidase (DprE1) Inhibitors.
AID633641Antibacterial activity against Enterococcus faecium 09-4 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID341378Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as reduction in bacterial burdens in blood culture at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 hrs after end of trea2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID515919Antibacterial activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID580908Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1877399Antibacterial activity against Acinetobacter baumannii 1392022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID563053Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-2614 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID574780Antimicrobial activity against Clostridium difficile assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID570921Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1676590Binding affinity to Nickel cation assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID1877411Antibacterial activity against Neisseria gonorrhoeae WHO K2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID574808Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 horboring rpoB S531L, katG R463L/E217G, gyrA D94N/S95T, rrs A1401G by CLSI method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID1676598Binding affinity to cupric ion assessed as retention ratio by measuring compound detected in elution fraction/total compound detected at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID574971Antimicrobial activity against Actinomyces israelii assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID698998AUC in human at 400 mg, po2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID1380668Oral bioavailability in CD1 mouse plasma by LC-MS/MS analysis2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
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.
AID570685Antibacterial activity against methicillin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID577482fCmax in Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model at 400 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID530388Inhibition of Mycobacterium tuberculosis DNA gyrase GyrA/GyrB N464S mutant gene assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1740331Antifungal activity against Stachybotrys chartarum IBT 7711 assessed as reduction in fungal growth incubated for 48 hrs by broth microdilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID428777Ratio of mutant prevention concentration for Streptococcus pneumoniae isolate SR-23958 to MIC for Streptococcus pneumoniae isolate SR-239582007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID428770Bactericidal activity against Streptococcus pneumoniae isolate SR-26134 by broth dilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID571142Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID368423Antimicrobial activity against Escherichia coli KAM32 pSTVdeltaqepA containing disrupted qepA gene by agar dilution method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
New plasmid-mediated fluoroquinolone efflux pump, QepA, found in an Escherichia coli clinical isolate.
AID1126763Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 1259 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID523140Antibacterial activity against Streptococcus pneumoniae isolate OC7368 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID372981Antimycobacterial activity against Mycobacterium avium complex N018 after 14 days by broth microdilution method2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID633636Antibacterial activity against methicillin-sensitive Staphylococcus epidermidis 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID285297Effect on 0.03 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID580901Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID262133Antimicrobial activity against Escherichia coli ATCC 259222006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID405469Antibacterial activity against Escherichia coli TOP10 containing pAT851 in presence of 50 ug/ml efflux pump inhibitor phenyl-arginine-beta-naphthylamide by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1318938Antibacterial activity against Escherichia coli ATCC 25922 after 24 hrs by microtitre broth dilution method2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID341086Half life in human with MDR1 3435 CC or CT genotype at 400 mg, po once daily after 14 days coadministered with rifampin at 600 mg/kg, po once daily2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID66893Antibacterial activity was evaluated against Enterococcus faecalis2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID530349Antimicrobial activity against Escherichia coli TOP10 harboring pQep plasmid carrying qepA2 gene by disk diffusion method2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Plasmid-mediated quinolone resistance pump QepA2 in an Escherichia coli isolate from France.
AID1348980Tmax in ICR mouse at 50 mg/kg, po by HPLC analysis
AID324745Inhibition of Mycobacterium leprae recombinant DNA gyrase expressed in Escherichia coli assessed as inhibition of pBR322 DNA supercoiling2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID1237417Fungicidal activity against Candida albicans 7535 after 24 hrs by agar plate method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1380666Volume of distribution at steady state in CD1 mouse plasma at 10 mg/kg, iv by LC-MS/MS analysis2018Journal of medicinal chemistry, 05-24, Volume: 61, Issue:10
Discovery and Optimization of Indolyl-Containing 4-Hydroxy-2-Pyridone Type II DNA Topoisomerase Inhibitors Active against Multidrug Resistant Gram-negative Bacteria.
AID558905Antimicrobial activity against Clostridium difficile CD5e harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID563330Upregulation of cwp84 gene expression in Clostridium difficile ATCC 43603 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID728912Antibacterial activity against Mycoplasma pneumoniae ATCC 29085 after 18 hrs by microbroth dilution method2013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID285292Effect on 0.5 ug/ml sitafloxacin-selected penicillin-resistant Streptococcus pneumoniae 216 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID572521Antimicrobial activity against qnrS-positive Salmonella enterica serovar Montevideo isolate s2209 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID593800Antimicrobial activity against Bacillus subtilis ATCC 6633 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID571141Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID425802Drug level in CD-1 mouse serum at 75 ug/ml administered through gavage after 24 hrs2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID1868114Selectivity index, ratio of IC50 for cytotoxicity against human MRC5 cells to MIC90 for anti-tubercular activity against Mycobacterium tuberculosis H37Rv2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID279288Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC D83Y and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
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.
AID573597Antibacterial activity against Fusobacterium necrophorum assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID556767fAUC/MIC in osteomyelitis patient serum at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 0.375 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID1391317Antibacterial activity against Pseudomonas aeruginosa 2742 after 24 hrs by two-fold serial dilution method2018Bioorganic & medicinal chemistry letters, 05-15, Volume: 28, Issue:9
Synthesis and evaluation of the antibacterial activities of aryl substituted dihydrotriazine derivatives.
AID1163987Antibacterial activity against Escherichia coli 12-1 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID577481Half life in Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model at 400 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID563009Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0791 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1181172Antimicrobial activity against second mutant generation Mycobacterium tuberculosis 1024_16.6 assessed as fold shift in MIC relative to parent strain2014Journal of medicinal chemistry, Aug-14, Volume: 57, Issue:15
Diarylthiazole: an antimycobacterial scaffold potentially targeting PrrB-PrrA two-component system.
AID562453Ratio of AUC (0 to 24 hrs) to MIC required for 24 hrs bacteriostatic effect in Staphylococcus aureus SMH375032009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID581299Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1316919Cytotoxicity against mouse RAW264.7 cells assessed as inhibition of cell proliferation at 50 ug/ml after 48 hrs by MTT assay2016Bioorganic & medicinal chemistry, 11-01, Volume: 24, Issue:21
Anti-tubercular activities of 5,6,7,8-tetrahydrobenzo[4,5]thieno[2,3-d]pyrimidin-4-amine analogues endowed with high activity toward non-replicative Mycobacterium tuberculosis.
AID562631Antimicrobial activity against Group G Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID633633Antibacterial activity against methicillin-sensitive Staphylococcus aureus 10-6 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1494121Antibacterial activity against Bacillus subtilis NCTC 10400 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
AID341382Antibacterial activity against Staphylococcus aureus infection-induced aortic valve endocarditis in rabbit assessed as reduction in bacterial burdens in heart valve tissue culture at 20 mg/kg, iv administered every 12 hrs for 5 days sacrificed 12 days aft2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Dexamethasone as adjuvant therapy to moxifloxacin attenuates valve destruction in experimental aortic valve endocarditis due to Staphylococcus aureus.
AID544864Antibacterial activity against Streptococcus pneumoniae U2A1681 harboring parC Ser79Tyr Asp83Ala mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID523309Antibacterial activity against methicillin-resistant Staphylococcus aureus isolate OC2838 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID425071Antimicrobial activity against Escherichia coli J53-AzR in presence of IPTG2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
Complex class 1 integrons with diverse variable regions, including aac(6')-Ib-cr, and a novel allele, qnrB10, associated with ISCR1 in clinical enterobacterial isolates from Argentina.
AID565311Antibacterial activity against Mycoplasma genitalium M30 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID563034Antimycobacterial activity against Mycobacterium tuberculosis 08-0764 by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID498780Antimicrobial activity against strong ciprofloxacin-resistant Streptococcus pyogenes by agar dilution method2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID571338Antibacterial activity against Enterococcus faecium assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID286095fAUC/MIC ratio of Staphylococcus aureus BSP-2443 at 75 mg2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID373003Antimycobacterial activity against Mycobacterium avium complex N018 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dose2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID1185138Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase A2B2 holoenzyme supercoiling activity using relaxed pBR322 substrate incubated for 90 mins by ethidium bromide staining based gel electrophoresis method2014ACS medicinal chemistry letters, Jul-10, Volume: 5, Issue:7
Benzimidazoles: novel mycobacterial gyrase inhibitors from scaffold morphing.
AID405465Antibacterial activity against Escherichia coli TOP10 containing pIP1206 plasmid in presence of 40 ug/ml efflux pump inhibitor 1-(1-naphthylmethyl)-piperazine by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID1256542Antibacterial activity against Klebsiella pneumoniae 14-3 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID532971Antimicrobial activity against isoniazid-resistant Mycobacterium tuberculosis isolate 152010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID570703Antibacterial activity against methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID574506Antimicrobial activity against Bacteroides distasonis assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID543392Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as increase in mouse survival at 50 mg/kg, ip administered 36 hrs postinfection every 12 hrs for 5 days2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID1237406Antibacterial activity against Escherichia coli KCTC 1924 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID285305Effect on 2 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID1196886Cytotoxicity against mouse RAW264.7 cells at 50 uM after 48 hrs by MTT assay2015European journal of medicinal chemistry, Mar-06, Volume: 92Design and development of novel Mycobacterium tuberculosis L-alanine dehydrogenase inhibitors.
AID570901Antibacterial activity against non-levofloxacin susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 8 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559511Antibacterial activity against Lancefield Streptococcus sp. group F assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID245029Minimum inhibitory concentration against Staphylococcus haemolyticus ATCC 299702005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID595934Inhibition of Staphylococcus aureus DNA gyrase Ser84Leu mutant assessed as inhibition of supercoiling of pBR322 DNA after 60 min by gel electrophoresis assay2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID322792Antimicrobial activity against Bacteroides stercoris assessed as percent resistant isolates2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
National survey on the susceptibility of Bacteroides fragilis group: report and analysis of trends in the United States from 1997 to 2004.
AID559373Antimicrobial activity against Clostridium difficile A422A selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID559544Antibacterial activity against non-levofloxacin susceptible Stenotrophomonas maltophilia assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID498785Antimicrobial activity against mild ciprofloxacin-resistant Streptococcus pyogenes at 10 ug by disk diffusion assay2010Antimicrobial agents and chemotherapy, Jan, Volume: 54, Issue:1
Prevalence and clonal characterization of Streptococcus pyogenes clinical isolates with reduced fluoroquinolone susceptibility in Spain.
AID285282Effect on 16 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 335 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID521331fAUC (0 to 24 hrs) in plasma of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1318929Antibacterial activity against multidrug-resistant/tobramycin-susceptible Pseudomonas aeruginosa isolate 860792016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID543400Ratio of AUC (24 hrs) in plasma in Listeria monocytogenes EGD-e infected BALB/c mouse to MIC for Listeria monocytogenes EGD-e2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID633741Antibacterial activity against Pseudomonas aeruginosa ATCC 27853 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID372991Antimycobacterial activity against Mycobacterium intracellular JATA52-01 infected C57BL/6J mouse assessed as liver bacterial count at 100 mg/kg/day dosed through gavage route administered for 28 days post bacterial challenge measured 2 days after last dos2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
In vitro and in vivo activities of novel fluoroquinolones alone and in combination with clarithromycin against clinically isolated Mycobacterium avium complex strains in Japan.
AID570932Antibacterial activity against methicillin-susceptible Staphylococcus epidermidis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID521142Antibacterial activity against extracellular Listeria monocytogenes EGDe at MIC by time-kill study2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID633645Antibacterial activity against Enterococcus faecalis 09-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID279251Antibacterial activity against moxifloxacin resistance selected Streptococcus pneumoniae 24 with GyrA S81Y, GyrB P413S and ParC S79F mutation after 50 passages by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID571857Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 16 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID244972Minimum inhibitory concentration against Streptococcus pyogenes ATCC 196152005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID532970Antimicrobial activity against pansusceptible Mycobacterium tuberculosis isolate 142010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID543395Antibacterial activity against Listeria monocytogenes EGD-e in BALB/c mouse central nervous system listeriosis model assessed as reduction in bacterial count in spleen at 50 mg/kg, ip administered 36 hrs postinfection as single dose measured within 1 hr2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Rapid eradication of Listeria monocytogenes by moxifloxacin in a murine model of central nervous system listeriosis.
AID562826Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2934 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID529898Antimicrobial activity against Leptospira weilii isolate 6 by broth microdilution method2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Antimicrobial susceptibilities of geographically diverse clinical human isolates of Leptospira.
AID580910Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID279257Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3009 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID563017Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0821 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1514450Antitubercular activity against streptomycin-resistant Mycobacterium tuberculosis after 7 days by resazurin dye based colorimetric assay2019Bioorganic & medicinal chemistry letters, 01-01, Volume: 29, Issue:1
Synthesis, antituberculosis studies and biological evaluation of new quinoline derivatives carrying 1,2,4-oxadiazole moiety.
AID533634Antimicrobial activity against Propionibacterium acnes assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID633634Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID531859Antimicrobial activity against Mycobacterium tuberculosis infected in patient at 400 mg/day, po administered for 7 days by HPLC2008Antimicrobial agents and chemotherapy, Mar, Volume: 52, Issue:3
Population pharmacokinetics of levofloxacin, gatifloxacin, and moxifloxacin in adults with pulmonary tuberculosis.
AID428829Ratio of Cmax in human at 80 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261372007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID581091Resistant spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID563218Antimycobacterial activity against Mycobacterium tuberculosis 08-0769 harboring gyrA putative promoter mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID577480AUC (0 to 24 hrs) in Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model at 400 mg every 24 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID559522Antibacterial activity against Streptococcus salivarius assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID633646Antibacterial activity against Escherichia coli ATCC 25922 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1188153Inhibition of 6-His-tagged Mycobacterium smegmatis GyrB expressed in Escherichia coli BL21 (DE3) pLysS cells incubated for 100 mins in presence of ATP by malachite green dye based ATP assay2014Bioorganic & medicinal chemistry, Sep-01, Volume: 22, Issue:17
Design, synthesis, biological evaluation of substituted benzofurans as DNA gyraseB inhibitors of Mycobacterium tuberculosis.
AID556024P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from apical to basolateral side at 50 uM in presence of 100 uM of MRP inhibitor Probenecid2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID499773Inhibition of Escherichia coli DNA topoisomerase-4-mediated decatenation of pBR322 by electrophoresis2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID209591Antibacterial activity was determined against Streptococcus mitis IID685 strain after incubation at 37 degrees C for 18 h2003Journal of medicinal chemistry, Mar-13, Volume: 46, Issue:6
Synthesis and structure-activity relationships of 5-amino-6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-8-methylquinolonecarboxylic acid antibacterials having fluorinated 7-[(3R)-3-(1-aminocyclopropan-1-yl)pyrrolidin-1-yl] substituents.
AID369971Ratio of AUC (0 to 24 hrs) in Staphylococcus aureus infected rabbit arthritis model at 45 mg/kg, po to MIC for methicillin-sensitive Staphylococcus aureus2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID1126760Antibacterial activity against multidrug-resistant 1 ug/ml Mycobacterium tuberculosis clinical isolate 930 assessed as growth inhibition after 7 days by microtiter plate assay2014Bioorganic & medicinal chemistry letters, Apr-15, Volume: 24, Issue:8
Design, synthesis, and biological evaluation of dihydroartemisinin-fluoroquinolone conjugates as a novel type of potential antitubercular agents.
AID533126Antimicrobial activity against Bacteroides caccae assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID544852Antibacterial activity against Streptococcus pneumoniae CP1000 by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID521337Cmax in CSF of patient with intracerebral and leptomeningeal tuberculosis at 800 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID1877412Antibacterial activity against Neisseria gonorrhoeae WHO G2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID1601846Antibacterial activity against Bacillus subtilis CMCC 63501 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID1297334Antibacterial activity against Pseudomonas aeruginosa 14-19 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1237425Antibacterial activity against quinolone-resistant Staphylococcus aureus CCARM 3519 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Aug-01, Volume: 25, Issue:15
Synthesis and antimicrobial evaluation of 5-aryl-1,2,4-triazole-3-thione derivatives containing a rhodanine moiety.
AID1600098Bactericidal activity against methicillin resistant Staphylococcus aureus N315 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID580755Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1877419Antibacterial activity against Neisseria gonorrhoeae WHO B2022Bioorganic & medicinal chemistry letters, 01-01, Volume: 55Lipophilic quinolone derivatives: Synthesis and in vitro antibacterial evaluation.
AID279283Antimicrobial activity against Streptococcus pneumoniae R6 transformants with parC S79Y and gyrA S81F mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID237034Dissociation constant (pKa) was determined2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID562615Antimicrobial activity against methicillin-sensitive Staphylococcus aureus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID695451Inhibition of human ERG expressed in mammalian cells by patch clamp method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Selenophene-containing inhibitors of type IIA bacterial topoisomerases.
AID520103Antimicrobial activity against Mycobacterium tuberculosis Erdman injected into gamma interferon gene knockout C57BL/6 mouse assessed as bacterial load in spleen of mouse at 300 mg/kg measured 9 days post drug treatment2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Evaluation of a 2-pyridone, KRQ-10018, against Mycobacterium tuberculosis in vitro and in vivo.
AID279262Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3665 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID553810Induction of cytotoxin production in Clostridium difficile PCR ribotype 027 in three-stage chemostat gut model at 43 mg/liter administered daily for 7 days measured after 2 days2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
Effects of exposure of Clostridium difficile PCR ribotypes 027 and 001 to fluoroquinolones in a human gut model.
AID593803Antimicrobial activity against quinilone-pencillin-resistant Staphylococcus aureus isolate SAR 72 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID262137Inhibitory activity against wild type Escherichia coli gyrase2006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Isothiazoloquinolones containing functionalized aromatic hydrocarbons at the 7-position: synthesis and in vitro activity of a series of potent antibacterial agents with diminished cytotoxicity in human cells.
AID285287Effect on 1 ug/ml moxifloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID261736Antibacterial activity against Streptococcus pyogenes ATCC 196152006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID575003Antimicrobial activity against Eubacterium lentum assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
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.
AID286064Half life at 50 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID573795Antibacterial activity against Prevotella buccae assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1600096Bactericidal activity against Staphylococcus aureus ATCC 6538 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID342065Antimicrobial activity against epidemic Clostridium difficile BI6-8-17 by broth dilution method2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID522991Antibacterial activity against Streptococcus pneumoniae isolate OC7376 by broth microdilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1297349Antibacterial activity against Enterococcus faecium 14-2 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID522988Antibacterial activity against Streptococcus pneumoniae isolate OC5462 assessed as log reduction in bacterial growth at 4 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID1740322Antimicrobial activity against fluoroquinolone-resistant Escherichia coli assessed as inhibition of microbial growth incubated for 24 hrs by microbroth dilution method2020European journal of medicinal chemistry, Sep-15, Volume: 202Design, synthesis and antimicrobial evaluation of novel glycosylated-fluoroquinolones derivatives.
AID342072Effect on growth of nonepidemic Clostridium difficile ATCC 9689 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID580884Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID405120Antimicrobial activity against Escherichia coli TOP10 harbouring p0 plasmid expressing pCR-BluntII-TOPO2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Vibrio splendidus as the source of plasmid-mediated QnrS-like quinolone resistance determinants.
AID563228Antimycobacterial activity against Mycobacterium tuberculosis 08-0789 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID559495Antibacterial activity against Prevotella sp. assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID562933Upregulation of slpA gene expression in Clostridium difficile 6425 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID580885Clearance in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID279823Bactericidal activity in Mycobacterium tuberculosis H37Rv on day 142007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Moxifloxacin, ofloxacin, sparfloxacin, and ciprofloxacin against Mycobacterium tuberculosis: evaluation of in vitro and pharmacodynamic indices that best predict in vivo efficacy.
AID523145Antibacterial activity against Streptococcus pneumoniae isolate OC7348 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID531514Antibacterial activity against Bacteroides ovatus assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID532683Antimicrobial activity against ciprofloxacin-nonsusceptible, DY PFGE pattern, emm6 type Streptococcus pyogenes with ST382 sequence type, ParC S79A mutant isolated from oropharyngeal colonization2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Emergence of ciprofloxacin-nonsusceptible Streptococcus pyogenes isolates from healthy children and pediatric patients in Portugal.
AID1152759Inhibition of Mycobacterium tuberculosis H37Rv DNA gyrase holoenzyme-mediated supercoiling of pBR322 DNA after 90 mins by agarose gel electrophoresis2014Journal of medicinal chemistry, Jun-12, Volume: 57, Issue:11
Novel N-linked aminopiperidine-based gyrase inhibitors with improved hERG and in vivo efficacy against Mycobacterium tuberculosis.
AID283164Antimicrobial susceptibility of Staphylococcus lugdunensis IDRL2640 biofilms after 24 hrs assessed as bacterial regrowth2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro effects of antimicrobial agents on planktonic and biofilm forms of Staphylococcus lugdunensis clinical isolates.
AID580912Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1079944Benign tumor, proven histopathologically. Value is number of references indexed. [column 'T.BEN' in source]
AID574498Antimicrobial activity against Bacteroides thetaiotaomicron assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID286151Bactericidal activity against Staphylococcus aureus ATCC 49619 at fAUC/MIC of 114 after 24 to 96 hrs in pharmacodynamic model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID1398594Antibacterial activity against Enterococcus faecalis ATCC 19433 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID1557311Cmax in human at 0.4 g, po by HPLC analysis2019MedChemComm, Oct-01, Volume: 10, Issue:10
Quinolone antibiotics.
AID565313Antibacterial activity against Mycoplasma genitalium TW10-5G by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID573835Antibacterial activity against beta-lactamase producing Clostridium paraputrificum assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID523149Antibacterial activity against Streptococcus pneumoniae isolate OC6585 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID369229Antibacterial activity against erythromycin-resistant Streptococcus pneumoniae assessed as percent resistant isolates by CLSI breakpoint method2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
Serotypes, Clones, and Mechanisms of Resistance of Erythromycin-Resistant Streptococcus pneumoniae Isolates Collected in Spain.
AID559493Antibacterial activity against Fusobacterium sp. assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID559494Antibacterial activity against Peptostreptococcus sp. assessed as percent susceptible isolates by CLSI M11-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID285536Effect on cellular viability of methicillin-resistant Staphylococcus aureus Mu50 at 10 times MIC by measuring the time required for recovery at 10 times MIC after 1 hr2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro and in vivo antibacterial activities of heteroaryl isothiazolones against resistant gram-positive pathogens.
AID1256561Antibacterial activity against methicillin-resistant Staphylococcus epidermidis 14-39 after 18 to 24 hrs2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis, antimycobacterial and antibacterial activity of l-[(1R,2S)-2-fluorocyclopropyl]naphthyridone derivatives containing an oxime-functionalized pyrrolidine moiety.
AID1348988Selectivity index, ratio of CC50 against African green monkey Vero cells to MIC for Mycobacterium tuberculosis H37Rv
AID425343Antibacterial activity against Streptococcus pneumoniae HMC 1151 harboring D83N, K137N mutation in quinolone-resistant determining regions of ParC gene and I460V mutation in QRDR of ParE gene showing efflux to ciprofloxacin, gemifloxacin by agar dilution 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID573596Antibacterial activity against Fusobacterium mortiferum assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID1676594Binding affinity to gallium ion assessed as accounting ratio by measuring total compound detected/total compound adsorbed at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID523137Antibacterial activity against Streptococcus pneumoniae isolate OC7368 assessed as log reduction in bacterial growth at 2 times MIC measured at 6 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID570890Antibacterial activity against Levofloxacin-susceptible Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID562827Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-1647 harboring gyrA Ala90Val mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID562943Upregulation of slpA gene expression in Clostridium difficile CD196 at 0.5 times MIC by real-time PCR analysis relative to control2009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Effects of subinhibitory concentrations of antibiotics on colonization factor expression by moxifloxacin-susceptible and moxifloxacin-resistant Clostridium difficile strains.
AID558616Antimicrobial activity against Streptococcus pneumoniae isolate 2880 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID581280Concentrations at which the kill rate is half-maximal for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID593807Antimicrobial activity against Acinetobacter baumannii ATCC 19606 by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID532974Antimicrobial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 182010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID572273Antimicrobial activity against Streptococcus pneumoniae ATCC 6303 by broth microdilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
In vivo characterization of the peptide deformylase inhibitor LBM415 in murine infection models.
AID558608Antimicrobial activity against Streptococcus pneumoniae isolate 1394 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID593810Antimicrobial activity against quinilone-pencillin-resistant Escherichia coli clinical isolate by broth dilution method2011Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8
Synthesis and biological evaluation of tetracyclic thienopyridones as antibacterial and antitumor agents.
AID1207666Inhibition of L-type calcium channel measured using 2-electrode voltage-clamp in human embryonic kidney cells heterologically expressing alpha-1C subunit2012Journal of applied toxicology : JAT, Oct, Volume: 32, Issue:10
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
AID1570243Inhibition of Mycobacterium tuberculosis DNA gyrase2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID559239Antibacterial activity against Streptococcus pneumoniae W002 harboring wild-type parC and gyrA genes assessed as mutation prevention concentration after 48 hrs2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID728904Chloroform-phosphate buffer apparent partition coefficient of the compound, log P at pH 7.42013Journal of medicinal chemistry, Mar-14, Volume: 56, Issue:5
Design, synthesis, and biological evaluations of novel 7-[7-amino-7-methyl-5-azaspiro[2.4]heptan-5-yl]-8-methoxyquinolines with potent antibacterial activity against respiratory pathogens.
AID1468617Antibacterial activity against Staphylococcus aureus ATCC 29213 infected in C57BL6 mouse cornea assessed as decrease in conjunctival chemosis at 0.3% administered tropically 2 times on day 1, 4 times on day 2 and 2 times on day 3 starting from 6 hrs post 2018Journal of medicinal chemistry, 03-08, Volume: 61, Issue:5
Design and Syntheses of Highly Potent Teixobactin Analogues against Staphylococcus aureus, Methicillin-Resistant Staphylococcus aureus (MRSA), and Vancomycin-Resistant Enterococci (VRE) in Vitro and in Vivo.
AID278862Antiproliferative effect against primary human osteoblasts assessed as BrdU incorporation into DNA at 10 ug/ml after 48 hrs2007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Influence on mitochondria and cytotoxicity of different antibiotics administered in high concentrations on primary human osteoblasts and cell lines.
AID245205Minimum inhibitory concentration against vancomycin intermediate Staphylococcus aureus MU 32005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID261735Antibacterial activity against Enterococcus faecalis ATCC 292122006Bioorganic & medicinal chemistry letters, Mar-01, Volume: 16, Issue:5
Biological evaluation of isothiazoloquinolones containing aromatic heterocycles at the 7-position: In vitro activity of a series of potent antibacterial agents that are effective against methicillin-resistant Staphylococcus aureus.
AID428798Ratio of AUC (0 to 24 hrs) in human at 80 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID559503Antibacterial activity against non-ciprofloxacin-susceptible and methicillin-susceptible Staphylococcus epidermidis assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID342081Effect on growth of nonepidemic Clostridium difficile J29 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.4 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID562459Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH366332009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID577498Bactericidal activity against Staphylococcus aureus in in vitro pharmacokinetic/pharmacodynamic model assessed as decrease in biofilm bacterial count at 400 mg every 24 hrs measured after 72 hrs2010Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10
Activities of high-dose daptomycin, vancomycin, and moxifloxacin alone or in combination with clarithromycin or rifampin in a novel in vitro model of Staphylococcus aureus biofilm.
AID425814AUC (0 to 24 hrs)/MIC in Mycobacterium tuberculosis H37Rv infected in CD-1 mouse2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID556032P-glycoprotein-mediated transport in human Calu3 cells assessed as efflux ratio of permeability from apical to basolateral side over basolateral to apical side at 50 uM in presence of 100 uM of p-glycoprotein and MRP inhibitor verapamil2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID531518Antibacterial activity against Bacteroides uniformis assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID285159Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in aerobic condition assessed by relative light units after 7 days2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID544831Antibacterial activity against Streptococcus pneumoniae CIP104485 by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID633740Antibacterial activity against Klebsiella pneumoniae 10-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID285278Susceptibility of penicillin-resistant Streptococcus pneumoniae 335 by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID425983Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 1635 after 50 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID342075Effect on growth of epidemic Clostridium difficile BI6-8-17 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.2 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID581096Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 150 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1318921Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 260-971032016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID1602934Antibacterial activity against drug-resistant Mycobacterium tuberculosis isolate 2 after 7 days by resazurin microtiter assay2019Bioorganic & medicinal chemistry letters, 04-15, Volume: 29, Issue:8
Exploiting the furo[2,3-b]pyridine core against multidrug-resistant Mycobacterium tuberculosis.
AID521149Antibacterial activity against intracellular Listeria monocytogenes EGDe infected in bone marrow-derived BALB/c mouse macrophage assessed as reduction in the formation of filopodium-like projections at >= MIC after 48 hrs by microscopy2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID670863Cytotoxicity against african green monkey Vero cells after 72 hrs by MTS assay2012Bioorganic & medicinal chemistry letters, Jul-15, Volume: 22, Issue:14
Construction and functionalization of fused pyridine ring leading to novel compounds as potential antitubercular agents.
AID285960Antimicrobial susceptibility against Haemophilus influenzae A3 isolate with GyrA Glu83Cys, ParC Ser84Arg and AcrR 97stop codon mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID521146Antibacterial activity against extracellular Listeria monocytogenes EGDe assessed as reduction in bacterial count at four times of MIC after 24 hrs by time-kill study2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID580871Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID633735Antibacterial activity against Escherichia coli 10-1 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID1652709Induction of Escherichia coli K12 MG1655 sulA promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID574583Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 625 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID422651Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3665 after 26 passages with clarithromycin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID533416Antimicrobial activity against Peptoniphilus asaccharolyticus assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID563019Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2399 harboring gyrA Asp94Tyr mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID563211Antimycobacterial activity against Mycobacterium tuberculosis 08-0787 harboring gyrA Asp94His mutant gene assessed as microbial susceptibility and deletion of codons 678 and 679 in gyrB mutant gene assessed as microbial susceptibility by agar proportion m2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1398615Cmax in Crj:CD rat at 5 mg/kg, po2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID571842Antibacterial activity against Proteus mirabilis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
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.
AID278598Inhibitory activity against Klebsiella pneumoniae 352007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID425989Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3243 after 20 passages by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID559142Antimicrobial activity against Clostridium difficile A422i harboring GyrA Asp81Asn mutant gene selected after 8 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1593371Inhibition of Pks13 D1644G/N1640K double mutant thioesterase domain in Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth by microplate alamar blue assay2019Journal of medicinal chemistry, 04-11, Volume: 62, Issue:7
Identification of Novel Coumestan Derivatives as Polyketide Synthase 13 Inhibitors against Mycobacterium tuberculosis. Part II.
AID425570Antibacterial activity against penicillin-susceptible, quinolone-resistant Streptococcus pneumoniae HMC 1072 expressing ermB and harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79Y mutation in QRDR of ParC gene and I460V 2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID456047Inhibition of Staphylococcus aureus wild type DNA topoisomerase 42009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID581286Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 100 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID244722Frequency of resistance emergence for methicillin resistant Staphylococcus aureus-50232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1154542Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID425356Antibacterial activity against Streptococcus pneumoniae HMC 1059 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460N mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID275467Cytotoxicity against human HepG2 cells after 72 hrs2007Journal of medicinal chemistry, Jan-25, Volume: 50, Issue:2
Isothiazoloquinolones with enhanced antistaphylococcal activities against multidrug-resistant strains: effects of structural modifications at the 6-, 7-, and 8-positions.
AID571852Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.5 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1252463Antimycobacterial activity against Mycobacterium tuberculosis H37Rv assessed as growth inhibition incubated for 7 days by microplate alamar blue assay2015European journal of medicinal chemistry, Oct-20, Volume: 1034-Aminoquinoline derivatives as novel Mycobacterium tuberculosis GyrB inhibitors: Structural optimization, synthesis and biological evaluation.
AID521143Antibacterial activity against extracellular Listeria monocytogenes EGDe at four times of MIC by time-kill study2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID530384Inhibition of Mycobacterium tuberculosis DNA gyrase GyrB/GyrA M74I mutant assessed as concentration required for inducing cleavage2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID558593Antimicrobial activity against Streptococcus pneumoniae 5 by time-kill analysis2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
AID608512Antibacterial activity against tolC knockout Escherichia coli KD13972011Bioorganic & medicinal chemistry letters, Aug-01, Volume: 21, Issue:15
Synthesis and evaluation of 1-cyclopropyl-2-thioalkyl-8-methoxy fluoroquinolones.
AID279255Antibacterial activity against gatifloxacin resistance selected Streptococcus pneumoniae 3009 after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID430966Antibacterial activity against Escherichia coli SKM9 containing gyrA L83, Y87 and parC L80 mutants assessed as increase in MIC by Etest relative to MIC for Escherichia coli 1596 containing gyrA L83 and parC I80 mutants2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Contributions of the combined effects of topoisomerase mutations toward fluoroquinolone resistance in Escherichia coli.
AID571875Antibacterial activity against Acinetobacter baumannii assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1449628Inhibition of human BSEP expressed in baculovirus transfected fall armyworm Sf21 cell membranes vesicles assessed as reduction in ATP-dependent [3H]-taurocholate transport into vesicles incubated for 5 mins by Topcount based rapid filtration method2012Drug metabolism and disposition: the biological fate of chemicals, Dec, Volume: 40, Issue:12
Mitigating the inhibition of human bile salt export pump by drugs: opportunities provided by physicochemical property modulation, in silico modeling, and structural modification.
AID556194P-glycoprotein-mediated transport in human Calu3 cells expressing P-glycoprotein assessed as maximum apparent permeability from basolateral to apical side by measuring compound level at 50 uM after 180 mins2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
P-glycoprotein-mediated transport of moxifloxacin in a Calu-3 lung epithelial cell model.
AID521148Antibacterial activity against extracellular Listeria monocytogenes EGDe assessed as reduction in bacterial count at eight times of MIC after 24 hrs by time-kill study2008Antimicrobial agents and chemotherapy, May, Volume: 52, Issue:5
Comparison of the in vitro efficacies of moxifloxacin and amoxicillin against Listeria monocytogenes.
AID575948Antimicrobial activity against erythromycin-resistant Streptococcus pneumoniae assessed as resistant isolates by broth microdilution method2010Antimicrobial agents and chemotherapy, Mar, Volume: 54, Issue:3
Distribution of serotypes, genotypes, and resistance determinants among macrolide-resistant Streptococcus pneumoniae isolates.
AID544298Antibacterial activity against vancomycin-susceptible methicillin-resistant Staphylococcus aureus 34 harboring GyrA S84L and GrlA S80F mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID531515Antibacterial activity against Bacteroides distasonis assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID1743454Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in human macrophages assessed as intracellular bacterial load at 2 times MIC measured after 6 days (Rvb = 5.57 to 6.43 logCFU/ml)2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID285309Susceptibility of vancomycin-resistant Enterococcus species single-step mutant by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID428293Antimicrobial activity against Acinetobacter baumannii BM4651 expressing deltaadeIJK genes isolated from patient with urinary tract infection by E test2008Antimicrobial agents and chemotherapy, Feb, Volume: 52, Issue:2
AdeIJK, a resistance-nodulation-cell division pump effluxing multiple antibiotics in Acinetobacter baumannii.
AID522989Antibacterial activity against Streptococcus pneumoniae isolate OC5462 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID279203Antibacterial activity against Streptococcus pneumoniae 1076 by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID562655Ratio of AUC (0 to 24 hrs) to MIC required for 2-log drop in bacterial count in Staphylococcus aureus SMH369452009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID369976Antibacterial activity against methicillin-resistant Staphylococcus aureus infected rabbit arthritis model assessed as change in bacterial load per gram of synovial fluid at 45 mg/kg, po after 7 days by broth microdilution technique2007Antimicrobial agents and chemotherapy, Sep, Volume: 51, Issue:9
In vivo efficacy of moxifloxacin compared with cloxacillin and vancomycin in a Staphylococcus aureus rabbit arthritis experimental model.
AID416844Antimycobacterial activity against Mycobacterium ulcerans isolate CU001 infected in BALB/c mouse left hind foot-pad assessed as bacterial load at 100 mg/kg, po administered for 5 days per week measured after 4 weeks2007Antimicrobial agents and chemotherapy, Oct, Volume: 51, Issue:10
Orally administered combined regimens for treatment of Mycobacterium ulcerans infection in mice.
AID1435843Antimycobacterial activity against Mycobacterium tuberculosis PE-003 clinical isolate after 7 days by resazurin reduction microplate assay2017European journal of medicinal chemistry, Jan-27, Volume: 126New insights into the SAR and drug combination synergy of 2-(quinolin-4-yloxy)acetamides against Mycobacterium tuberculosis.
AID570916Antibacterial activity against hospital-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.06 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID562629Antimicrobial activity against Group C Streptococcus assessed as susceptible isolates by agar dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activities of three new dihydrofolate reductase inhibitors against clinical isolates of gram-positive bacteria.
AID523297Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in B6 mouse assessed as assessed as lowest concentration to reduce bacterial burden in lungs to level of reduction achieved with higher doses orally treated in water-20% captisol2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
Fast standardized therapeutic-efficacy assay for drug discovery against tuberculosis.
AID406656Antibacterial activity against Staphylococcus aureus ACH-0203 isolate with gyrA Ser84Leu and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID1207530Inhibition of rapid delayed inward rectifying potassium current (IKr) measured using manual patch clamp assay
AID563030Antimycobacterial activity against Mycobacterium tuberculosis 08-0769 harboring gyrA putative promoter mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID515917Antibacterial activity against rifampicin-resistant Mycobacterium tuberculosis after 7 days by microplate alamar blue assay2010Bioorganic & medicinal chemistry, Oct-15, Volume: 18, Issue:20
Synthesis of non-purine analogs of 6-aryl-9-benzylpurines, and their antimycobacterial activities. Compounds modified in the imidazole ring.
AID580891Growth rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1600112Bactericidal activity against methicillin resistant Staphylococcus aureus 6347 cultured in MH medium assessed as reduction in bacterial survival incubated for 48 hrs by microbroth dilution method2019European journal of medicinal chemistry, Oct-01, Volume: 179Synthesis and biological evaluation of hybrid quinolone-based quaternary ammonium antibacterial agents.
AID425806Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung after 1 day after 2nd successive aerosol infection run2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID563049Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0791 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID581094Virtual volume of the central compartment in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID523139Antibacterial activity against Streptococcus pneumoniae isolate OC7368 assessed as log reduction in bacterial growth at 2 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID425576Antibacterial activity against macrolide-, quinolone-susceptible and penicillin-intermediate Streptococcus pneumoniae HMC 100 harboring S79Y mutation in quinolone-resistant determining regions of ParC gene after 34 passages with gemifloxacin measured afte2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID580765Concentrations at which the kill rate is half-maximal for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered for every 24 hrs2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID595853Antibacterial activity against methicillin-sensitive Staphylococcus aureus ATCC 29213 after 24 hrs by microdilution method2011Journal of medicinal chemistry, May-12, Volume: 54, Issue:9
Exploration of the activity of 7-pyrrolidino-8-methoxyisothiazoloquinolones against methicillin-resistant Staphylococcus aureus (MRSA).
AID406809Antibacterial activity against Staphylococcus aureus NY2746 isolate with gyrA Ser84Leu and grlA Ser80Phe mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID1243293Antimicrobial activity against Pseudomonas aeruginosa ATCC 27853 by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID1264562Dose-normalized AUC in mouse at 2 mg/kg, iv by LC-MS/MS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID285161Antimicrobial activity against non replicating persistence Mycobacterium tuberculosis H37Rv in anaerobic condition assessed as relative light unit after 11 days by LORA assay2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Low-oxygen-recovery assay for high-throughput screening of compounds against nonreplicating Mycobacterium tuberculosis.
AID518632Volume of distribution in human by LC analysis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID563056Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 08-0810 harboring gyrA Asp94Tyr mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID1297338Antibacterial activity against methicillin-sensitive Staphylococcus aureus 14-4 after 18 to 24 hrs by CLSI M100-S11 method2016Bioorganic & medicinal chemistry letters, May-01, Volume: 26, Issue:9
Synthesis, antimycobacterial and antibacterial activity of 1-(6-amino-3,5-difluoropyridin-2-yl)fluoroquinolone derivatives containing an oxime functional moiety.
AID1319005Induction of cytoplasmic membrane depolarization in Pseudomonas aeruginosa PAO1 at 1 ug/ml by DiSC3(5) dye based fluorescence assay2016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID574790Antimycobacterial activity against extensively drug-resistant Mycobacterium tuberculosis isolate 2301 obtained from sputum of patient at 2 ug/ml by Bactec MGIT960 modified proportion method2010Antimicrobial agents and chemotherapy, Nov, Volume: 54, Issue:11
Emergence and molecular characterization of extensively drug-resistant Mycobacterium tuberculosis clinical isolates from the Delhi Region in India.
AID765271fAUC/MIC in Mycobacterium tuberculosis infected mouse2013Bioorganic & medicinal chemistry letters, Sep-01, Volume: 23, Issue:17
A medicinal chemists' guide to the unique difficulties of lead optimization for tuberculosis.
AID425546Antibacterial activity against Streptococcus pneumoniae HMC 2536 harboring S81Y mutation in quinolone-resistant determining regions of GyrA gene, S79F, K137N mutation in QRDR of ParC gene and I460V mutation in QRDR of ParE gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1888652Antibacterial activity against Escherichia coli assessed as inhibition of bacterial growth2022Bioorganic & medicinal chemistry letters, 02-01, Volume: 57Synthesis and evaluation of dual-action kanglemycin-fluoroquinolone hybrid antibiotics.
AID1890602Antibacterial activity against beta-lactams, macrolide and fluoroquinolone resistant Streptococcus pneumoniae 718 assessed as inhibition of bacterial growth incubated for 18 hrs by CLSI based serial agar dilution method2022Bioorganic & medicinal chemistry letters, 05-01, Volume: 63WCK 1152, WCK 1153: Discovery and structure activity relationship for the treatment of resistant pneumococcal and staphylococcal respiratory infections.
AID561319Antimicrobial activity against Escherichia coli isolate 17 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID324747Antibacterial activity against Mycobacterium leprae at 5 ug/mL after 11 to 18 days2007Antimicrobial agents and chemotherapy, May, Volume: 51, Issue:5
Expression and purification of an active form of the Mycobacterium leprae DNA gyrase and its inhibition by quinolones.
AID565319Antibacterial activity against Mycoplasma genitalium M2321 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID581482Total spore counts of toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 50 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1743455Antitubercular activity against Mycobacterium tuberculosis H37Rv infected in human macrophages assessed as intracellular bacterial load at 4 times MIC measured after 6 days (Rvb = 5.57 to 6.43 logCFU/ml)2020European journal of medicinal chemistry, Dec-01, Volume: 207Phenanthrolinic analogs of quinolones show antibacterial activity against M. tuberculosis.
AID456031Antibacterial activity against Enterococcus faecalis ATCC 19433 after 18 hrs by twofold microbroth dilution method2009Bioorganic & medicinal chemistry, Oct-01, Volume: 17, Issue:19
Design, synthesis and biological evaluations of novel 7-[3-(1-aminocycloalkyl)pyrrolidin-1-yl]-6-desfluoro-8-methoxyquinolones with potent antibacterial activity against multi-drug resistant Gram-positive bacteria.
AID544839Antibacterial activity against Streptococcus pneumoniae H548 clinical isolate harboring gyrA Ser81Phe mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID1652706Induction of Escherichia coli K12 MG1655 recA promotor measured at 30 mins interval for 20 hrs by fluorescence assay relative to control
AID428796Ratio of AUC (0 to 24 hrs) in human at 400 mg, po administered once daily to MIC for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID531510Antibacterial activity against Bacteroides stercoris assessed as percent resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Jul, Volume: 52, Issue:7
Resistance trends of the Bacteroides fragilis group over a 10-year period, 1997 to 2006, in Madrid, Spain.
AID520361Half-life in plasma of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID518056Toxicity in healthy human assessed as nausea at 400 mg/kg, po administered as single dose2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Effect of vicriviroc on the QT/corrected QT interval and central nervous system in healthy subjects.
AID699001Bioavailability in human2012European journal of medicinal chemistry, May, Volume: 51Tuberculosis: the drug development pipeline at a glance.
AID574979Antimicrobial activity against Actinomyces meyeri assessed as percent resistant isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID633736Antibacterial activity against Escherichia coli 10-2 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID571143Antibacterial activity against Enterococcus faecalis assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.25 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID523315Antibacterial activity against Streptococcus pneumoniae R6 by agar dilution method2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID581069Hill constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID283246Reduction of lung lesions in Mycobacterium tuberculosis H37Rv infected Swiss mouse at 100 mg/kg, po for 5 days/week after 2 months2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
Synergistic activity of R207910 combined with pyrazinamide against murine tuberculosis.
AID1819096Antimycobacterial activity against Mycobacterium tuberculosis H37Rv infected in mouse J774.A1 cells assessed as log reduction of bacterial growth at 1X MIC measured after 3 days by visual colony counting analysis2022ACS medicinal chemistry letters, Jan-13, Volume: 13, Issue:1
Structural Rigidification of
AID405467Antibacterial activity against Escherichia coli TOP10 containing pAT851 plasmid by Etest2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Transferable resistance to aminoglycosides by methylation of G1405 in 16S rRNA and to hydrophilic fluoroquinolones by QepA-mediated efflux in Escherichia coli.
AID428825Ratio of Cmax in human at 400 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-239582007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID1187834Inhibition of Mycobacterium tuberculosis GyrA/GyrB using relaxed pBR322 as substrate after 30 mins by DNA supercoiling assay2014European journal of medicinal chemistry, Oct-06, Volume: 85Extending the N-linked aminopiperidine class to the mycobacterial gyrase domain: pharmacophore mapping from known antibacterial leads.
AID571121Antibacterial activity against Streptococcus pneumoniae assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID533420Antimicrobial activity against Micromonas micros assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID1398602Antibacterial activity against levofloxacin and methicillin-resistant Staphylococcus aureus 890325-1 after 18 hrs by two-fold microbroth dilution method2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID565323Antibacterial activity against Mycoplasma genitalium M6285 by broth dilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Antimicrobial susceptibilities of Mycoplasma genitalium strains examined by broth dilution and quantitative PCR.
AID558612Antimicrobial activity against Streptococcus pneumoniae isolate 2617 by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Comparative antipneumococcal activities of sulopenem and other drugs.
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).
AID1243285Antimicrobial activity against levofloxacin-resistant Staphylococcus aureus clinical isolates by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID573558Antibacterial activity against beta-lactamase producing Bacteroides thetaiotaomicron assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID580872Growth rate constant of spore-phase cells going to vegetative phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model administered as continuous infusion2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID285288Effect on 4 ug/ml levofloxacin-selected penicillin-resistant Streptococcus pneumoniae 334 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID580866Drug excretion in urine of healthy human at 800 mg/kg2009Antimicrobial agents and chemotherapy, Mar, Volume: 53, Issue:3
New drugs against tuberculosis: problems, progress, and evaluation of agents in clinical development.
AID428790Antibacterial activity against 80 mg q.d. moxifloxacin-pretreated Streptococcus pneumoniae isolate SR-26137 after 48 hrs of incubation by population analysis2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID544855Antibacterial activity against Streptococcus pneumoniae U2A1050 harboring gyrA Ser81Phe mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID544300Antibacterial activity against vancomycin-intermediate Staphylococcus aureus Mu50 harboring GyrA S84L and GrlA S80F mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID530597Antimicrobial activity against Escherichia coli TOP10 harboring pSmQnr9 carrying Smqnr gene by Etest2008Antimicrobial agents and chemotherapy, Oct, Volume: 52, Issue:10
Smqnr, a new chromosome-carried quinolone resistance gene in Stenotrophomonas maltophilia.
AID544305Antibacterial activity against vancomycin-resistant Staphylococcus aureus VRS6 harboring GyrA S84L and GrlA S80F, E84G mutant after 24 hrs by CLSI method2009Antimicrobial agents and chemotherapy, Feb, Volume: 53, Issue:2
In vitro activity of the quinolone WCK 771 against recent U.S. hospital and community-acquired Staphylococcus aureus pathogens with various resistance types.
AID1164008Antibacterial activity against methicillin-resistant Staphylococcus aureus 12-5 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID563209Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 01-0172 harboring gyrA Asp94Ala mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID245172Minimum inhibitory concentration against methicillin-resistant Staphylococcus aureus-50232005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID1399857Antitubercular activity against isoniazid-resistant Mycobacterium tuberculosis H37Rv harboring katG Y155 mutant2018Bioorganic & medicinal chemistry letters, 09-15, Volume: 28, Issue:17
Design, synthesis and antibacterial properties of pyrimido[4,5-b]indol-8-amine inhibitors of DNA gyrase.
AID518631Clearance in human by LC analysis2010Antimicrobial agents and chemotherapy, Jun, Volume: 54, Issue:6
Moxifloxacin pharmacokinetics/pharmacodynamics and optimal dose and susceptibility breakpoint identification for treatment of disseminated Mycobacterium avium infection.
AID428860Bactericidal activity against Streptococcus pneumoniae isolate SR-26137 assessed as prevention of bacterial regrowth under condition simulating oral administration of 400 mg once daily after 72 hrs2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID499674Antimicrobial activity against quinolone and penicillin-resistant Staphylococcus aureus SAR4790 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID1318919Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 1018852016Journal of medicinal chemistry, 09-22, Volume: 59, Issue:18
Hybrid Antibiotic Overcomes Resistance in P. aeruginosa by Enhancing Outer Membrane Penetration and Reducing Efflux.
AID532968Antimicrobial activity against quinolone-resistant Mycobacterium tuberculosis isolate 122010Antimicrobial agents and chemotherapy, Aug, Volume: 54, Issue:8
In vitro antituberculosis activities of ACH-702, a novel isothiazoloquinolone, against quinolone-susceptible and quinolone-resistant isolates.
AID323891Antimicrobial activity against qnrA1 expressing Escherichia coli J53/p1960 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID528850Antimicrobial activity against methicillin-susceptible Staphylococcus epidermidis isolated from ICU patient wound assessed as resistant isolates by broth microdilution method2008Antimicrobial agents and chemotherapy, Apr, Volume: 52, Issue:4
Antimicrobial-resistant pathogens in intensive care units in Canada: results of the Canadian National Intensive Care Unit (CAN-ICU) study, 2005-2006.
AID1067069Antimicrobial activity against quinolone-resistant Staphylococcus aureus clinical isolate 3519 after 20 hrs by two-fold serial dilution technique2014European journal of medicinal chemistry, Mar-03, Volume: 74Synthesis and evaluation of the antimicrobial activities of 3-((5-phenyl-1,3,4-oxadiazol-2-yl)methyl)-2-thioxothiazolidin-4-one derivatives.
AID1447479Antibacterial activity against multidrug/extremely drug-resistant/colistin-susceptible Pseudomonas aeruginosa isolate 100036 after 18 hrs by microtiter dilution assay2017Journal of medicinal chemistry, 05-11, Volume: 60, Issue:9
Amphiphilic Tobramycin-Lysine Conjugates Sensitize Multidrug Resistant Gram-Negative Bacteria to Rifampicin and Minocycline.
AID285303Effect on 0.06 ug/ml DQ113-selected penicillin-resistant Streptococcus pneumoniae 218 mutant after five passages assessed as susceptibility by agar dilution method2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
In vitro studies with DQ-113 and comparison fluoroquinolones to determine propensities to select resistance in gram-positive cocci.
AID633640Antibacterial activity against Enterococcus faecium 09-3 after 18 hrs by two fold serial dilution method2012European journal of medicinal chemistry, Jan, Volume: 47, Issue:1
Synthesis and antibacterial activity of naphthyridone derivatives containing mono/difluoro-methyloxime pyrrolidine scaffolds.
AID425811Antimicrobial activity against Mycobacterium tuberculosis H37Rv infected in CD-1 mouse lung at 75 mg/kg administered through gavage2007Antimicrobial agents and chemotherapy, Dec, Volume: 51, Issue:12
In vivo validation of the mutant selection window hypothesis with moxifloxacin in a murine model of tuberculosis.
AID559540Antibacterial activity against Proteus vulgaris assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID1750828Plasma protein binding in human at 10 uM after 4 hrs by LC-MS/MS analysis2021Journal of medicinal chemistry, 05-13, Volume: 64, Issue:9
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
AID285967Antimicrobial susceptibility against Haemophilus influenzae C2 isolate with GyrA Asp88Asn, AcrR Leu31His and Arg34Glu mutation2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Haemophilus influenzae is associated with hypermutability.
AID428828Ratio of Cmax in human at 80 mg, po administered once daily to mutant prevention concentration for Streptococcus pneumoniae isolate SR-261342007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Pharmacodynamic assessment based on mutant prevention concentrations of fluoroquinolones to prevent the emergence of resistant mutants of Streptococcus pneumoniae.
AID562642Ratio of AUC (0 to 24 hrs) to MIC required for 1-log drop in bacterial count in Staphylococcus aureus SMH380042009Antimicrobial agents and chemotherapy, Dec, Volume: 53, Issue:12
Bacterial strain-to-strain variation in pharmacodynamic index magnitude, a hitherto unconsidered factor in establishing antibiotic clinical breakpoints.
AID227415Fold reduction in minimum inhibitory concentration of antibiotic in presence of GG9182004Bioorganic & medicinal chemistry letters, Feb-23, Volume: 14, Issue:4
Inhibitors of multidrug resistance (MDR) have affinity for MDR substrates.
AID561317Antimicrobial activity against Enterobacter cloacae isolate 153 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID544834Antibacterial activity against Streptococcus pneumoniae R6 Tr6 harboring gyrA Ser81Phe mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID1570250AUC (0 to infinity) in SPF ICR mouse at 100 mg/kg, sc2019European journal of medicinal chemistry, Oct-15, Volume: 180Synthesis and biological evaluation of moxifloxacin-acetyl-1,2,3-1H-triazole-methylene-isatin hybrids as potential anti-tubercular agents against both drug-susceptible and drug-resistant Mycobacterium tuberculosis strains.
AID572509Antimicrobial activity against Salmonella enterica serovar Typhimurium isolate SL1344 harboring wild type ParC gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID278599Inhibitory activity against azide-resistant Escherichia coli J53 T352007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID571864Antibacterial activity against Stenotrophomonas maltophilia assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 0.12 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559386Antimicrobial activity against Clostridium difficile A422H harboring GyrA Thr82Ile and GyrB Leu451Phe mutant genes selected after 8 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1254077Antibacterial activity against methicillin-resistant Staphylococcus aureus CCARM 3167 after 24 hrs by two-fold serial dilution method2015Bioorganic & medicinal chemistry letters, Nov-15, Volume: 25, Issue:22
Synthesis and biological evaluation of 1,3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents.
AID1494122Antibacterial activity against methicillin-sensitive Staphylococcus aureus NCTC 12981 after 16 hrs by microdilution method2018European journal of medicinal chemistry, Jan-01, Volume: 143Design, synthesis and biological evaluation of novel aryldiketo acids with enhanced antibacterial activity against multidrug resistant bacterial strains.
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]
AID1154545Antimicrobial activity against Mycobacterium tuberculosis H37Rv ATCC 27294 harboring DprE1 C387G mutant assessed as growth inhibition after 5 days by microdilution method2014Journal of medicinal chemistry, Jul-10, Volume: 57, Issue:13
Lead optimization of 1,4-azaindoles as antimycobacterial agents.
AID1164002Antibacterial activity against methicillin-sensitive Staphylococcus aureus 12-1 after 18 to 24 hrs by standard twofold serial dilution method2014European journal of medicinal chemistry, Oct-30, Volume: 86Synthesis, antimycobacterial and antibacterial evaluation of l-[(1R, 2S)-2-fluorocyclopropyl]fluoroquinolone derivatives containing an oxime functional moiety.
AID523150Antibacterial activity against Streptococcus pneumoniae isolate OC6585 assessed as log reduction in bacterial growth at 4 times MIC measured at 24 hrs by time-kill assay2010Antimicrobial agents and chemotherapy, May, Volume: 54, Issue:5
In vitro antibacterial activities of JNJ-Q2, a new broad-spectrum fluoroquinolone.
AID561321Antimicrobial activity against Escherichia coli isolate 48 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID533424Antimicrobial activity against Anaerococcus prevotii assessed as resistant isolates by agar dilution method2008Antimicrobial agents and chemotherapy, Dec, Volume: 52, Issue:12
In vitro activities of doripenem, a new broad-spectrum carbapenem, against recently collected clinical anaerobic isolates, with emphasis on the Bacteroides fragilis group.
AID556778Volume of distribution in peripheral compartment in osteomyelitis patient at 400 mg, po administered for every 24 hrs by three stage hierarchical Bayesian method2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID1601842Antibacterial activity against Staphylococcus aureus CMCC 25923 measured after 24 hrs by ELISA2019European journal of medicinal chemistry, Mar-15, Volume: 166Synthesis, antimicrobial and cytotoxic activities, and molecular docking studies of N-arylsulfonylindoles containing an aminoguanidine, a semicarbazide, and a thiosemicarbazide moiety.
AID279267Antibacterial activity against clarithromycin resistance selected Streptococcus pneumoniae 3243 with 23S rRNA A2059T mutation after 10 antibiotic-free subcultures by macrodilution method2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Multistep resistance selection and postantibiotic-effect studies of the antipneumococcal activity of LBM415 compared to other agents.
AID581073Growth rate constant of vegetative-phase cells going to spore phase in toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 250 mg administered as continuous infusion by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID1476350Antitubercular activity against isoniazid resistant Mycobacterium tuberculosis H37Rv ATCC 35822 after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID1504966Antitubercular activity against Mycobacterium tuberculosis H37Rv ATCC 27294 incubated for 10 days under low oxygen condition followed by second incubation under aerobic condition for 28 hrs by LORA2017ACS medicinal chemistry letters, Dec-14, Volume: 8, Issue:12
Antitubercular Nitroimidazoles Revisited: Synthesis and Activity of the Authentic 3-Nitro Isomer of Pretomanid.
AID559516Antibacterial activity against Streptococcus anginosus assessed as percent susceptible isolates by CLSI M100-S18 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID244929Antibacterial activity against Streptococcus pyogenes G-36 was determined2004Bioorganic & medicinal chemistry letters, Oct-18, Volume: 14, Issue:20
Synthesis and antibacterial activity of novel 6-fluoro-1-[(1R,2S)-2-fluorocyclopropan-1-yl]-4-oxoquinoline-3-carboxylic acids bearing cyclopropane-fused 2-amino-8-azabicyclo[4.3.0]nonan-8-yl substituents at the C-7 position.
AID544841Antibacterial activity against Streptococcus pneumoniae U2A1053 harboring parC Ser79Phe mutant gene by agar disk diffusion method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID581278Kill rate constant for compound-resistant toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID388877Protective effect against Staphylococcus aureus ATCC 13709-induced bone infection in CD rat at 10 mg/kg, iv administered as single dose 2 days before bacterial challenge2008Bioorganic & medicinal chemistry, Oct-15, Volume: 16, Issue:20
Bisphosphonated fluoroquinolone esters as osteotropic prodrugs for the prevention of osteomyelitis.
AID425357Antibacterial activity against Streptococcus pneumoniae HMC 1071 harboring S81F mutation in quinolone-resistant determining regions of GyrA gene and S79F, K137N mutation in QRDR of ParC gene by agar dilution method2008Antimicrobial agents and chemotherapy, Jan, Volume: 52, Issue:1
In vitro activity of DC-159a, a new broad-spectrum fluoroquinolone, compared with that of other agents against drug-susceptible and -resistant pneumococci.
AID1676588Binding affinity to Zinc ion assessed as performance ratio ratio by measuring product of accounting ratio and retention ratio at 2.55 umol by immobilized metal-ion affinity chromatography2020Journal of medicinal chemistry, 10-22, Volume: 63, Issue:20
Immobilized Metal Affinity Chromatography as a Drug Discovery Platform for Metalloenzyme Inhibitors.
AID499676Antimicrobial activity against Acinetobacter baumannii ATCC 19606 after 24 hrs by broth microdilution method2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID1264563Volume of distribution at steady state in mouse at 2 mg/kg, iv by LC-MS/MS analysis2015ACS medicinal chemistry letters, Oct-08, Volume: 6, Issue:10
Discovery of Indazole Derivatives as a Novel Class of Bacterial Gyrase B Inhibitors.
AID1868115Anti-tubercular activity against Mycobacterium tuberculosis CF16 assessed as inhibition of mycobacterial growth incubated for 7 days by resazurin-dye based analysis2022European journal of medicinal chemistry, Jul-05, Volume: 237Tapping into the antitubercular potential of 2,5-dimethylpyrroles: A structure-activity relationship interrogation.
AID573836Antibacterial activity against beta-lactamase producing Clostridium septicum assessed as susceptible isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID571853Antibacterial activity against Pseudomonas aeruginosa assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 1 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID323881Antimicrobial activity against Escherichia coli DH10B/pACYC184 GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID573598Antibacterial activity against Fusobacterium varium assessed as resistant isolates by CLSI agar dilution method2008Antimicrobial agents and chemotherapy, Sep, Volume: 52, Issue:9
Increasing trends in antimicrobial resistance among clinically important anaerobes and Bacteroides fragilis isolates causing nosocomial infections: emerging resistance to carbapenems.
AID581670Antibacterial activity against Staphylococcus aureus SCV isolated from cystic fibrosis patient in cation-adjusted MH 2 broth at pH 5.5 after 48 hrs by broth microdilution method2009Antimicrobial agents and chemotherapy, Apr, Volume: 53, Issue:4
Intracellular activity of antibiotics in a model of human THP-1 macrophages infected by a Staphylococcus aureus small-colony variant strain isolated from a cystic fibrosis patient: pharmacodynamic evaluation and comparison with isogenic normal-phenotype a
AID544856Antibacterial activity against Streptococcus pneumoniae U2A1051 harboring gyrA Ser81Tyr mutant gene by agar dilution method2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Real-time PCR detection of gyrA and parC mutations in Streptococcus pneumoniae.
AID206728Antibacterial activity was evaluated against Staphylococcus aureus2004Journal of medicinal chemistry, Jun-03, Volume: 47, Issue:12
Chemometric studies on the bactericidal activity of quinolones via an extended VolSurf approach.
AID563051Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 99-1914 harboring gyrA Asp94Gly mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID556763fAUC/MIC in osteomyelitis patient serum at 400 mg, po administered for every 24 hrs at PKPD breakpoint at 1 mg/liter2009Antimicrobial agents and chemotherapy, May, Volume: 53, Issue:5
Penetration of moxifloxacin into bone evaluated by Monte Carlo simulation.
AID563025Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-1234 harboring gyrA Asn533Thr gyrB mutant gene by resazurin microtiter assay2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID570911Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 2 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID559203Antibacterial activity against Streptococcus pneumoniae S004 harboring wild-type parC and gyrA Gly85Asn mutant genes2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
In vitro activity of garenoxacin against Streptococcus pneumoniae mutants with characterized resistance mechanisms.
AID1364753Antibiofilm activity against Mycobacterium tuberculosis assessed as log reduction in bacterial count at 10 ug/ml measured after 7 days by MPN assay2017Bioorganic & medicinal chemistry, 05-15, Volume: 25, Issue:10
Mycobacterium tuberculosis lysine-ɛ-aminotransferase a potential target in dormancy: Benzothiazole based inhibitors.
AID1655163Bactericidal activity against Mycobacterium tuberculosis H37Rv assessed as reduction in bacterial growth at 0.35 ug/ml incubated for 3 to 4 weeks by time kill assay2020ACS medicinal chemistry letters, May-14, Volume: 11, Issue:5
Improving the Potency of
AID499772Inhibition of Escherichia coli DNA gyrase-mediated supercoiling of pBR322 using bromothymol blue by electrophoresis2010Bioorganic & medicinal chemistry, Aug-15, Volume: 18, Issue:16
Synthesis and biological evaluation of tetracyclic fluoroquinolones as antibacterial and anticancer agents.
AID561325Antimicrobial activity against Klebsiella pneumoniae isolate 135 expressing aac(6')-Ib-cr gene2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Prevalence of aac(6')-Ib-cr encoding a ciprofloxacin-modifying enzyme among Enterobacteriaceae blood isolates in Korea.
AID323883Antimicrobial activity against qnrA1 expressing Escherichia coli DH10B GyrA/ParC mutant expressing porins by microdilution method2007Antimicrobial agents and chemotherapy, Jun, Volume: 51, Issue:6
Mutant prevention concentrations of fluoroquinolones for Enterobacteriaceae expressing the plasmid-carried quinolone resistance determinant qnrA1.
AID422673Antimicrobial activity against drug-resistant Streptococcus pneumoniae isolate 3009 after 18 passages with levofloxacin measured after 10 antibiotic-free subculture by multi-step resistance selection technique2007Antimicrobial agents and chemotherapy, Nov, Volume: 51, Issue:11
Capability of 11 antipneumococcal antibiotics to select for resistance by multistep and single-step methodologies.
AID563043Antimycobacterial activity against multidrug-resistant Mycobacterium tuberculosis 02-2934 harboring gyrA Ala90Val mutant gene assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID283395Antimicrobial activity against Nocardia nova after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID406811Antibacterial activity against Staphylococcus aureus BSA643 isolate with gyrA Ser84Leu and grlA Ser80Tyr, Glu84Gly mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID574772Antimicrobial activity against Clostridium perfringens assessed as percent susceptible isolates after 48 hrs by agar dilution method2010Antimicrobial agents and chemotherapy, Sep, Volume: 54, Issue:9
Antimicrobial susceptibility patterns for recent clinical isolates of anaerobic bacteria in South Korea.
AID570912Antibacterial activity against community-associated methicillin-resistant Staphylococcus aureus assessed as percent cumulative susceptible isolates at minimum inhibitory concentration of 4 ug/ml by CLSI broth microdilution method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
In vitro activity of nemonoxacin, a novel nonfluorinated quinolone, against 2,440 clinical isolates.
AID1207316Inhibition of fast sodium current (INa) in Chinese Hamster Ovary (CHO) K1 cells transfected with human Nav1.5 measured using IonWorks Quattro automated patch clamp platform
AID570828AUC (0 to 48 hrs) in healthy human assessed as 25-desacetyl-rifapentine level at 900 mg, po administered as a single dose measured on day 5 post compound dose by HPLC2008Antimicrobial agents and chemotherapy, Nov, Volume: 52, Issue:11
Repeated administration of high-dose intermittent rifapentine reduces rifapentine and moxifloxacin plasma concentrations.
AID406655Antibacterial activity against Staphylococcus aureus ACH-0192 isolate with gyrA Ser84Leu and grlA Ser80Phe, Ala116Val mutant after 24 hrs by broth microdilution method2007Antimicrobial agents and chemotherapy, Jul, Volume: 51, Issue:7
Dual targeting of DNA gyrase and topoisomerase IV: target interactions of heteroaryl isothiazolones in Staphylococcus aureus.
AID540231Dose normalised AUC in dog after po administration2005Xenobiotica; the fate of foreign compounds in biological systems, Feb, Volume: 35, Issue:2
Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human.
AID1476360Antitubercular activity against rifampicin resistant Mycobacterium tuberculosis H37Rv ATCC 35838 after 24 hrs by MABA method2017Journal of medicinal chemistry, 10-26, Volume: 60, Issue:20
Design, Synthesis, and Characterization of N-Oxide-Containing Heterocycles with in Vivo Sterilizing Antitubercular Activity.
AID521328AUC (0 to 24 hrs) in CSF of patient with intracerebral and leptomeningeal tuberculosis at 400 mg/kg, po QD measured on day 32008Antimicrobial agents and chemotherapy, Jun, Volume: 52, Issue:6
Plasma and cerebrospinal fluid pharmacokinetics of moxifloxacin in a patient with tuberculous meningitis.
AID237457Partition coefficient (logD2.0)2005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID244968Minimum inhibitory concentration against Pseudomonas aeruginosa ATCC 278532005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID559374Antimicrobial activity against Clostridium difficile A422B selected after 4 ug/ml of levofloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID1079947Comments (NB not yet translated). [column 'COMMENTAIRES' in source]
AID278604Inhibitory activity against azide-resistant Escherichia coli J53 T12-15022007Antimicrobial agents and chemotherapy, Jan, Volume: 51, Issue:1
Association of QnrB determinants and production of extended-spectrum beta-lactamases or plasmid-mediated AmpC beta-lactamases in clinical isolates of Klebsiella pneumoniae.
AID530379Inhibition of Escherichia coli DNA gyrase GyrA/GyrB2008Antimicrobial agents and chemotherapy, Aug, Volume: 52, Issue:8
Mutagenesis in the alpha3alpha4 GyrA helix and in the Toprim domain of GyrB refines the contribution of Mycobacterium tuberculosis DNA gyrase to intrinsic resistance to quinolones.
AID1243286Antimicrobial activity against Streptococcus pneumoniae ATCC 49619 by standard broth microdilution method2015Bioorganic & medicinal chemistry letters, Sep-15, Volume: 25, Issue:18
Synthesis and biological evaluation of levofloxacin core-based derivatives with potent antibacterial activity against resistant Gram-positive pathogens.
AID572510Antimicrobial activity against Salmonella enterica serovar Braenderup isolate s2906 harboring ParC QRDR mutant gene by agar dilution method2009Antimicrobial agents and chemotherapy, Sep, Volume: 53, Issue:9
Mechanisms of resistance in nontyphoidal Salmonella enterica strains exhibiting a nonclassical quinolone resistance phenotype.
AID286045Peak free concentration at 100 mg/24 hrs regimen in vitro PK model2007Antimicrobial agents and chemotherapy, Apr, Volume: 51, Issue:4
Fluoroquinolone resistance in Streptococcus pneumoniae: area under the concentration-time curve/MIC ratio and resistance development with gatifloxacin, gemifloxacin, levofloxacin, and moxifloxacin.
AID563222Antimycobacterial activity against Mycobacterium tuberculosis 08-0764 assessed as microbial susceptibility by agar proportion method2009Antimicrobial agents and chemotherapy, Oct, Volume: 53, Issue:10
Fluoroquinolone resistance in Mycobacterium tuberculosis and mutations in gyrA and gyrB.
AID279281Antimicrobial activity against Streptococcus pneumoniae R6 transformants with gyrA E85K mutation2007Antimicrobial agents and chemotherapy, Feb, Volume: 51, Issue:2
Fitness costs of fluoroquinolone resistance in Streptococcus pneumoniae.
AID1909944n-Octanol/phosphate buffer partition coefficient, logD of the compound at pH 7.4 incubated for 3 hrs by shake flask method based HPLC-DAD analysis2022Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9
Spiropyrimidinetrione DNA Gyrase Inhibitors with Potent and Selective Antituberculosis Activity.
AID558906Antimicrobial activity against Clostridium difficile CD5f harboring GyrB Ser416Ala mutant gene selected after 4 ug/ml of moxifloxacin by agar dilution method2009Antimicrobial agents and chemotherapy, Jun, Volume: 53, Issue:6
Molecular analysis of the gyrA and gyrB quinolone resistance-determining regions of fluoroquinolone-resistant Clostridium difficile mutants selected in vitro.
AID283397Antimicrobial activity against Nocardia transvalensis after 72 hrs by microdilution method2007Antimicrobial agents and chemotherapy, Mar, Volume: 51, Issue:3
In vitro activities of tigecycline and eight other antimicrobials against different Nocardia species identified by molecular methods.
AID559531Antibacterial activity against ciprofloxacin-susceptible Haemophilus influenzae assessed as percent susceptible isolates by CLSI M7-A7 method2009Antimicrobial agents and chemotherapy, Aug, Volume: 53, Issue:8
Besifloxacin, a novel fluoroquinolone, has broad-spectrum in vitro activity against aerobic and anaerobic bacteria.
AID540214Clearance in rat after iv administration2005Journal of pharmaceutical sciences, Jul, Volume: 94, Issue:7
Extrapolation of human pharmacokinetic parameters from rat, dog, and monkey data: Molecular properties associated with extrapolative success or failure.
AID342079Effect on growth of epidemic Clostridium difficile BI6-8-17 in CF1 mouse assessed as increase in bacterial density in cecal content at 0.375 mg/day, sc for 4 days assessed after 2 days of last treatment2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effect of fluoroquinolone treatment on growth of and toxin production by epidemic and nonepidemic clostridium difficile strains in the cecal contents of mice.
AID581273Kill rate constant for compound-sensitive toxin and capsule gene-deficient Bacillus anthracis Sterne in hollow-fiber pharmacodynamic infection model at 200 mg, qd by Bayesian method2009Antimicrobial agents and chemotherapy, Nov, Volume: 53, Issue:11
Impact of spore biology on the rate of kill and suppression of resistance in Bacillus anthracis.
AID244720Frequency of resistance emergence for methicillin resistant Staphylococcus aureus-322005Journal of medicinal chemistry, Aug-11, Volume: 48, Issue:16
A chiral benzoquinolizine-2-carboxylic acid arginine salt active against vancomycin-resistant Staphylococcus aureus.
AID341063AUC (0 to 24 hrs) in human at 400 mg, po once daily after 4 days2007Antimicrobial agents and chemotherapy, Aug, Volume: 51, Issue:8
Effects of rifampin and multidrug resistance gene polymorphism on concentrations of moxifloxacin.
AID1398616AUC (0 to 8 hrs) in Crj:CD rat at 5 mg/kg, po2018Journal of medicinal chemistry, 08-23, Volume: 61, Issue:16
Design, Synthesis, and Biological Evaluation of Novel 7-[(3 aS,7 aS)-3 a-Aminohexahydropyrano[3,4- c]pyrrol-2(3 H)-yl]-8-methoxyquinolines with Potent Antibacterial Activity against Respiratory Pathogens.
AID1801385GyraseB Assay from Article 10.1111/cbdd.12529: \\Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.\\2015Chemical biology & drug design, Oct, Volume: 86, Issue:4
Design and Biological Evaluation of Furan/Pyrrole/Thiophene-2-carboxamide Derivatives as Efficient DNA GyraseB Inhibitors of Staphylococcus aureus.
AID1805801Various Assay from Article 10.1021/acs.jmedchem.1c00409: \\Perspectives on SARS-CoV-2 Main Protease Inhibitors.\\2021Journal of medicinal chemistry, 12-09, Volume: 64, Issue:23
Perspectives on SARS-CoV-2 Main Protease Inhibitors.
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 (3,016)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's68 (2.25)18.2507
2000's1085 (35.97)29.6817
2010's1401 (46.45)24.3611
2020's462 (15.32)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 111.00

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 Index111.00 (24.57)
Research Supply Index8.22 (2.92)
Research Growth Index5.50 (4.65)
Search Engine Demand Index206.51 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (111.00)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials552 (17.48%)5.53%
Reviews200 (6.34%)6.00%
Case Studies349 (11.05%)4.05%
Observational22 (0.70%)0.25%
Other2,034 (64.43%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (533)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Four Way Crossover Thorough QT/QTc Study to Evaluate the Electrocardiographic Effects of Therapeutic and Supratherapeutic Doses of Cytisinicline in Healthy Smokers [NCT05566288]Phase 127 participants (Actual)Interventional2022-10-17Completed
Double-blind, Randomized, Mono-center, Placebo-controlled Pilot Study to Investigate the Efficacy and Safety of Moxifloxacin in the Prevention of Bacteremia After High-dose Chemotherapy and Transplantation of Peripheral Stem Cells [NCT00398411]Phase 366 participants (Actual)Interventional2006-10-31Completed
A Randomised, Placebo-controlled, Four-way Crossover Repeat Dose Study to Evaluate the Effect of the Inhaled Fluticasone Furoate (FF)/GW642444M Combination on Electrocardiographic Parameters, With Moxifloxacin as a Positive Control, in Healthy Subjects [NCT01209026]Phase 185 participants (Actual)Interventional2010-06-23Completed
A Single-centre, Randomised, Double-blind, Double-dummy, Placebo Controlled, 4-way Crossover Phase I Study to Investigate the Effect of 2 Single Doses (400 μg and 1200 µg) of Inhaled AZD3199 on QT/QTc Interval, Compared to Placebo, Using Moxifloxacin (Ave [NCT01222442]Phase 140 participants (Actual)Interventional2010-11-30Completed
A Multiple-Dose, Randomized, Double-Blind, Placebo-Controlled, Active-Comparator, Parallel-Group Study to Investigate the Effect of GDC-0449 on the QT/QTc Interval in Healthy Female Subjects [NCT01173536]Phase 161 participants (Actual)Interventional2010-08-25Completed
Efficacy of Clarithromycin or Moxifloxacin Containing Regimen in 6 Months Sputum Conversion of Mycobacterium Xenopi [NCT01298336]Phase 392 participants (Actual)Interventional2011-03-02Completed
A Prospective, Randomized, Double-blinded, Multi-center Trial Assessing the Safety and Efficacy of Intravenous Administration BAY12-8039 (Moxifloxacin) 400mg Every 24 h Compared to Intravenous Ceftriaxone 2g Every 24h and Metronidazole 500mg Every 12h for [NCT00769171]Phase 3364 participants (Actual)Interventional2005-10-31Completed
Investigation of the Effect on the QT/QTc Interval After Multiple Dose Oral Administration (100 and 200 mg Bid) of CG5503 PR in a Randomised, Double-blind, Double-dummy Placebo- and Moxifloxacin-controlled 4- Way Cross-over Phase I Study in 48 Healthy Mal [NCT03951402]Phase 148 participants (Actual)Interventional2003-03-31Completed
A Study to Evaluate the Effect of Therapeutic and Supratherapeutic Oral Doses of GSK3640254 on Cardiac Conduction as Assessed by 12-Lead Electrocardiogram Compared to Placebo and a Single Oral Dose of Moxifloxacin in Healthy Adult Participants [NCT04563845]Phase 150 participants (Actual)Interventional2020-11-09Completed
A Double Blind, Randomized, Multiple Dose, Placebo And Active Controlled 4-Way Crossover Study To Investigate The Effects Of Inhaled PF-00610355 On QT/QTC Interval In Healthy Subjects [NCT01107054]Phase 148 participants (Actual)Interventional2010-06-30Completed
Genetics of QT Response to Moxifloxacin [NCT01936480]Phase 451 participants (Actual)Interventional2013-10-31Terminated(stopped due to Recruitment difficulties)
Prospective, Single-center, Randomized, Double-blind, Placebo- and Moxifloxacin-controlled, 4-way Crossover Phase 1 Study to Assess the Effect of Multiple Therapeutic and Supratherapeutic Doses of Aprocitentan on the QT Interval Duration in Healthy Subjec [NCT04281342]Phase 148 participants (Actual)Interventional2020-01-14Completed
Patient-reported Experiences and Quality of Life Outcomes in the TB-PRACTECAL Clinical Trial [NCT03942354]Phase 2/Phase 354 participants (Anticipated)Interventional2019-09-01Recruiting
Pharmacokinetic Evaluation of Moxifloxacin Administered Intravenously and Orally in Healthy Volunteers Who Have Had a Gastric Bypass. [NCT01130922]Phase 412 participants (Anticipated)Interventional2010-03-31Completed
Double-Blind Randomized Placebo-Control Trial to Evaluate Electrocardiogram Effects of HPN-100 as Defined by Clinical and Supratherapeutic Dose in Healthy Men and Women [NCT01135680]Phase 198 participants (Actual)Interventional2010-05-31Completed
Standard Chemotherapy Plus Moxifloxacin as First-line Treatment for Metastatic Triple-negative Breast Cancer : a Multicenter, Double-blind, Placebo-controlled, Phase 3 Trial [NCT04722978]Phase 3228 participants (Anticipated)Interventional2021-04-20Recruiting
The Comparison of Outcomes of Antibiotic Drugs and Appendectomy (CODA) Trial [NCT02800785]1,552 participants (Actual)Interventional2016-05-31Completed
A Randomized, Double-Blind, 3-arm, Parallel Group, Placebo- and Positive-controlled Study to Investigate the Effects of Setmelanotide on QTc Interval in Healthy Subjects [NCT05046132]Phase 477 participants (Actual)Interventional2021-08-05Completed
A Placebo- and Positive-Controlled Study of the Electrophysiological Effects on the QT Interval After a Supratherapeutic Dose of LY2140023 in Subjects With Schizophrenia [NCT01606436]Phase 186 participants (Actual)Interventional2012-06-30Completed
Single-dose, Open-label, Randomized, Non-blinded, Three-fold Crossover Study in Healthy Subjects to Compare the Bioavailability of Moxifloxacin (BAY12-8039) 400 mg Tablet and 400 mg Oral Suspension Under Fasting Conditions, and to Investigate the Effect o [NCT01073891]Phase 124 participants (Actual)Interventional2010-05-31Completed
A Double-blind, Double-dummy, Randomized, 4-period Cross-over, Placebo- and Positive-controlled Study to Evaluate the Effect of TMC435 on the QTc Interval in Healthy Subjects [NCT01269294]Phase 160 participants (Actual)Interventional2011-01-31Completed
A Single-centre, Randomised, Double-blind, Placebo-controlled, Four Way Crossover Phase I Study to Investigate the Effect on QT/QTc Interval of a Single Dose of Intravenous Ceftazidime NXL104 (3000/2000 mg) or Ceftaroline Fosamil NXL104 (1500/2000 mg), Co [NCT01290900]Phase 154 participants (Actual)Interventional2011-02-28Completed
Randomized, Single-blind, Double-dummy, 4-fold Cross-over, Placebo- and Active-controlled Study to Investigate the Influence of BAY 1817080 on the QTc Interval in Healthy Male and Female Participants (TQT Study) [NCT04423744]Phase 142 participants (Actual)Interventional2020-06-18Completed
Single-dose and Randomized, Single-center, Placebo- and Active-controlled, Crossover Study to Assess the Effect of Omecamtiv Mecarbil (OM) on QT/QTc Intervals in Healthy Subjects [NCT04175808]Phase 170 participants (Actual)Interventional2019-11-14Completed
Utility of Antibiotic Treatment in Acute Non-purulent Exacerbations of COPD: a Double Blinded, Randomized, Placebo-controlled Trial of Security and Efficacy [NCT01091493]Phase 473 participants (Actual)Interventional2010-07-31Completed
Evaluation of Topical Vigamox in the Initial Management of Ocular Graft-Versus-Host Disease [NCT04204122]Phase 20 participants (Actual)Interventional2020-06-15Withdrawn(stopped due to Investigator decided to close study)
A Randomized, Double-blind, Multicenter Trial to Evaluate the Safety and Efficacy of Sequential (Intravenous, Oral) Moxifloxacin Versus Comparator in Pediatric Subjects With Complicated Intra-abdominal Infection [NCT01069900]Phase 3458 participants (Actual)Interventional2010-07-21Completed
Thorough QT Study to Evaluate the Effects of BI 409306 as Single Dose on Cardiac Safety Parameters in Healthy Male and Female Subjects. A Randomized, Placebo Controlled, Double-blind, Five-period Crossover Study With (Open-label) Moxifloxacin as Positive [NCT03934203]Phase 147 participants (Actual)Interventional2019-05-09Completed
Evaluating Newly Approved Drugs for Multidrug-resistant TB (endTB): A Clinical Trial [NCT02754765]Phase 3754 participants (Actual)Interventional2016-12-31Completed
A Double-blind, Randomized, Placebo- and Active-controlled, Parallel-group Trial to Evaluate the Effect of Single-dose TMC207 on the QT/QTc Interval in Healthy Subjects [NCT01291563]Phase 188 participants (Actual)Interventional2011-02-28Completed
A Phase 1, Randomized, Double-Blind, Placebo and Active Controlled, Parallel Crossover Study to Evaluate the Effect of Repeat Oral Doses of Mirabegron on Cardiac Repolarization in Healthy Male and Female Adult Subjects [NCT01199523]Phase 1352 participants (Actual)Interventional2010-05-31Completed
Microbiome Effect of Omadacycline on Healthy Volunteers [NCT06030219]Phase 132 participants (Actual)Interventional2020-10-12Completed
A Single-centre, Randomised, Double-blind, Placebo Controlled Phase I Study in Two Parts: Part A to Assess a Safe and Tolerable Supratherapeutic Dose of TC-5214 After Single Ascending Oral Doses in Healthy Male Subjects, Followed by Part B: A Four-period [NCT01359618]Phase 116 participants (Actual)Interventional2011-06-30Terminated(stopped due to Sponsor decision to terminate)
A Phase I, Randomized, Placebo-Controlled, Four-Way Crossover Study to Evaluate the Effect of Intravenous (IV) Zanamivir on Cardiac Conduction as Assessed by 12-lead Electrocardiogram (ECG) With Moxifloxacin as a Positive Control in Healthy Volunteers [NCT01353729]Phase 140 participants (Actual)Interventional2011-05-19Completed
A Single-Center, Randomized, Placebo-Controlled, 3 Treatment Period Crossover Study to Assess the Effect of Padsevonil on Cardiac Repolarization (QTc Interval) (Using Moxifloxacin as a Positive Control) in Healthy Study Participants [NCT04126343]Phase 154 participants (Actual)Interventional2019-10-23Terminated(stopped due to Based on available data, UCB has decided to stop development of padsevonil as adjunctive treatment of focal-onset seizures)
Evaluation of the Effects of Sequential Multiple-Dose Regimens of Cariprazine on Cardiac Repolarization in Patients With Schizophrenia [NCT01376076]Phase 1129 participants (Actual)Interventional2011-06-30Completed
A Randomized, Double-Blind, Placebo/Positive Controlled, Evaluation of the Effects of MNTX on ECG Parameters and Cardiac Repolarization in Normal Volunteers [NCT01363323]Phase 1546 participants (Actual)Interventional2004-11-30Completed
A Phase 1, Randomized, Double-blinded, Four-period Crossover, Thorough QT/QTC (TQT) Clinical Trial to Evaluate the Effect of Zoliflodacin on Cardiac Repolarization in Healthy Male and Female Subjects [NCT03613649]Phase 172 participants (Actual)Interventional2018-09-25Completed
A Phase 1, Randomized, Blinded, Placebo and Moxifloxacin Controlled, 4-Period Crossover, Study Evaluating the Effect of ZTI-01 on 12-Lead Electrocardiogram Parameters in Healthy Adult Subject [NCT03709927]Phase 141 participants (Actual)Interventional2018-01-11Completed
Randomized, Double-blind (for Clazosentan), Placebo- and Moxifloxacincontrolled, 3-way Cross-over Phase 1 Study to Assess the Effect of Two Intravenous Doses of Clazosentan on the QTc Interval Duration in Healthy Subjects [NCT03657446]Phase 136 participants (Actual)Interventional2018-09-18Completed
A Prospective, Single-center, Open-label, Clinical Trial to Compare the 10-day Sequential Therapy and 7-day Culture Based Tailored Therapy for the Eradication of Helicobacter Pylori [NCT02373280]600 participants (Anticipated)Interventional2014-08-31Recruiting
Thorough QT/QTc Study to Assess the Electrocardiographic Safety of a New Gadolinium-based Contrast Agent P03277 in Healthy Volunteers [NCT03657264]Phase 148 participants (Actual)Interventional2017-08-21Completed
A Phase 1 Active- and Placebo-Controlled Study of the Electrocardiogram Effects and Pharmacokinetics of Ferumoxytol in Healthy Men and Women [NCT00360425]Phase 1174 participants Interventional2006-05-31Completed
A Single-Dose, Randomized, Double-Blind, Placebo- and Positive-Controlled, 4-Way Crossover Study to Evaluate the Effect of LC350189 on the QTc (Corrected QT) Interval in Healthy Adult Subjects [NCT04966325]Early Phase 137 participants (Actual)Interventional2021-09-23Completed
A PHASE 1, RANDOMIZED, PLACEBO-AND POSITIVE-CONTROLLED CROSSOVER STUDY TO DETERMINE THE EFFECT OF SINGLE-DOSE PF-06700841 ON QTC INTERVAL IN HEALTHY VOLUNTEERS [NCT03656952]Phase 133 participants (Actual)Interventional2018-09-05Completed
"A Phase 2, Randomized, Double-Blind, Placebo Controlled, 3-Period Crossover, Positive Control, QT-Evaluation Study of APL-130277 in Subjects With Parkinson's Disease Complicated by Motor Fluctuations (OFF Episodes)" [NCT03187301]Phase 248 participants (Actual)Interventional2017-08-03Completed
Study on Pharmacokinetics of Moxifloxacin in Serum and Liver Tissue of Patients Undergoing Liver Resection Due to Primary or Secondary Tumor of the Liver [NCT01302951]Phase 434 participants (Actual)Interventional2008-07-31Completed
A Phase 1, Randomized, Placebo-And Positive-Controlled Crossover Study To Determine The Effect Of A Single-Dose Of PH-797804 On QTc Interval In Healthy Volunteers [NCT01862887]Phase 148 participants (Actual)Interventional2013-04-30Completed
A Two-part Phase I Study Composed of a Randomized, Double-blind, 4-parallel Group Study to Evaluate the Effect of Multiple Oral Doses of GFT505 on the QT/QTc Interval Compared to Placebo With Moxifloxacin (400 mg in Single Oral Dose) as a Positive Control [NCT02091310]Phase 1200 participants (Actual)Interventional2014-02-28Completed
Antibiotic Prophylaxis for ERCP: a Comparison of Intravenous Ceftriaxone With Intravenous Moxifloxacin in the Prophylaxis of Cholangitis [NCT02098486]Phase 286 participants (Actual)Interventional2014-03-31Completed
A 2 PART STUDY IN HEALTHY SUBJECTS: PART A: A MULTIPLE DOSE, RANDOMIZED, PLACEBO CONTROLLED STUDY TO EVALUATE THE SAFETY AND TOLERABILITY OF SUPRA-THERAPEUTIC DOSES OF RO4602522; PART B: A MULTIPLE-DOSE, RANDOMIZED, DOUBLE-BLIND, DOUBLE DUMMY, PLACEBO CON [NCT02104648]Phase 1203 participants (Actual)Interventional2014-04-30Completed
A Thorough QT/QTc Study to Assess the Effects of Androxal in Healthy Male Subjects [NCT02117830]Phase 154 participants (Anticipated)Interventional2014-04-30Completed
A Randomized, Placebo- and Positive-Controlled, Crossover Study to Evaluate the Effect of Meropenem-Vaborbactam on the QT/QTc Interval in Healthy Volunteers [NCT03564158]Phase 153 participants (Actual)Interventional2018-05-01Completed
A Double-blind, Randomized, Placebo-controlled, Four-way Crossover Phase 1 Study Including an Open-label Positive Control (Moxifloxacin) to Assess the Effect of Repeated Daily Doses of 10 mg and 30 mg Macitentan on the QT/QTc Interval of the ECG in Health [NCT02050802]Phase 164 participants (Actual)Interventional2011-08-31Completed
Prospective Randomized Study to Compare Clinical Outcomes in Patients With Osteomyelitis Treated With Intravenous Antibiotics Versus Intravenous Antibiotics With an Early Switch to Oral Antibiotics [NCT02099240]Early Phase 111 participants (Actual)Interventional2014-03-06Terminated(stopped due to Not enough patient enrollment and lack of staffing)
A Prospective, Single-center, Randomized, Open-label, Parallel Design Clinical Trial to Compare the 14-day Bismuth Quadruple Therapy and 7-day Culture Based Tailored Therapy for the Eradication of Helicobacter as a Rescue 2nd Therapy. [NCT02359331]370 participants (Actual)Interventional2014-08-31Terminated
Contraceptive Hormones and Women With Cystic Fibrosis: Satisfaction and Effects on Disease [NCT02144246]Phase 15 participants (Actual)Interventional2014-05-31Terminated
A Phase 3, Randomized, Double-Blind, Double-Dummy Study to Compare the Efficacy and Safety of Oral Lefamulin (BC 3781) Versus Oral Moxifloxacin in Adults With Community-Acquired Bacterial Pneumonia [NCT02813694]Phase 3738 participants (Actual)Interventional2016-08-31Completed
STREAM: The Evaluation of a Standard Treatment Regimen of Anti-tuberculosis Drugs for Patients With MDR-TB [NCT02409290]Phase 3588 participants (Actual)Interventional2016-03-31Completed
Efficacy of the Application of Moxifloxacin and Cefixime in Reduction of Inflammatory Sequelae and Complications After Mandibular Third Molar Surgery [NCT05027893]157 participants (Actual)Interventional2019-06-07Active, not recruiting
A Double-blind, Randomized, Placebo-controlled, 4-Period Cross-over Study to Evaluate the Effect of JNJ-53718678 on the Cardiac Repolarization Interval in Healthy Adult Subjects [NCT03696459]Phase 152 participants (Actual)Interventional2018-10-02Completed
Assessment of the Effect of 480 mg and 1200 mg of BI 201335 as Single Dose on the QT Interval in Healthy Female and Male Subjects. A Randomised, Placebo Controlled, Double-blind, Four-way Crossover Phase-I-study With Moxifloxacin as Positive Control [NCT02182310]Phase 156 participants (Actual)Interventional2008-06-30Completed
A Randomized, Multiple-dose, Placebo- and Positive-controlled Parallel Group Study to Evaluate the Effects of Indacaterol on Cardiac Safety in Healthy Subjects [NCT01263808]Phase 1404 participants (Actual)Interventional2008-04-30Completed
A Multicenter, Randomized, Double-blind, Active-controlled, Parallel Group, 2-arm Study to Show Superiority of the Oral Contraceptive SH T00658ID Over Ortho Tri-Cyclen Lo on Hormone Withdrawal-associated Symptoms After 6 Cycles of Treatment. [NCT00754065]Phase 3409 participants (Actual)Interventional2008-09-30Completed
Phase 2 Randomized Trial of a Moxifloxacin-Containing Regimen For Treatment of Smear-Positive Pulmonary Tuberculosis in Adults With and Without HIV Infection [NCT00082173]Phase 2170 participants (Actual)Interventional2004-10-31Completed
A Single-Center, Multiple-Dose, Randomized, Double-Blind, Placebo-Controlled, Cross-Over Study to Investigate the Effect of Balovaptan on the QTC Interval in Healthy Subjects [NCT03808298]Phase 157 participants (Actual)Interventional2019-02-07Completed
A Randomized, Double-Blind and Nested Crossover (For Placebo and Moxifloxacin) Thorough QT Study to Evaluate the Effect of Rodatristat Ethyl, Rodatristat, and Its Major Metabolites on Cardiac Repolarization in Healthy Volunteers [NCT05933447]Phase 127 participants (Actual)Interventional2023-05-12Completed
A Randomized, Double-blind, Placebo-controlled, 4-way Crossover Study to Compare the Effects on the Cardiac De- and Repolarization Duration as Well as Other Cardiac Safety Parameters of Two Doses of Oral Lasmiditan (100 mg and 400 mg) With Those of Moxifl [NCT03465436]Phase 156 participants (Actual)Interventional2011-09-16Completed
An Open-Label Phase 2 Trial to Evaluate the Male Reproductive Safety of a 6-Month Combination Treatment for Pulmonary Tuberculosis (TB) of Bedaquiline Plus Pretomanid Plus Moxifloxacin Plus Pyrazinamide (BPaMZ) in Adult Male Participants With Drug Resista [NCT04179500]Phase 226 participants (Actual)Interventional2021-09-16Active, not recruiting
A Double-blinded, Randomised, Placebo Controlled, Five-way Crossover Study With One Positive Control (Open-label) (Moxifloxacin) to Assess the Influence of Oral Single Dose KUC 7483 BS (40 mg, 80 mg, 160 mg, 320 mg) on the QT/QTc Interval of the ECG in He [NCT02256735]Phase 139 participants (Actual)Interventional2005-08-31Completed
[NCT00750633]Phase 3990 participants (Actual)Interventional2008-06-30Completed
A Phase 3, Randomized, Double-Blind, Double-Dummy Study to Compare the Efficacy and Safety of Lefamulin (BC 3781) Versus Moxifloxacin (With or Without Adjunctive Linezolid) in Adults With Community-Acquired Bacterial Pneumonia [NCT02559310]Phase 3551 participants (Actual)Interventional2015-09-30Completed
Reason Evaluation of Initial Treatment Failure in Patients With Community Acquired Pneumonia [NCT03280004]314 participants (Anticipated)Observational [Patient Registry]2017-11-20Recruiting
A Randomized, Placebo-Controlled, Four-Period Crossover, Study to Evaluate the Effect of Volanesorsen on the QTc Interval Using a Therapeutic and Supra-Therapeutic Dose Compared With Placebo in Healthy Volunteers: a Thorough QT Study [NCT02910635]Phase 152 participants (Actual)Interventional2016-09-19Completed
Safety and Efficacy of a Topical Otic Formulation in the Treatment of Acute Otitis Media With Otorrhea Through Tympanostomy Tubes (AOMT) [NCT00579189]Phase 3776 participants (Actual)Interventional2006-01-31Completed
A Phase 1, Randomized, Double-Blind, Cross-Over, Placebo- and Active-Controlled Cardiac Safety Study of Therapeutic and Supratherapeutic Doses of Fumaryl Diketopiperazine Administered as Technosphere® Inhalation Powder in Healthy Subjects [NCT00721344]Phase 148 participants (Actual)Interventional2008-04-30Completed
Population Pharmacokinetics of Anti-tuberculosis Drugs in Children With Tuberculosis [NCT03625739]800 participants (Anticipated)Observational [Patient Registry]2018-07-01Recruiting
A Randomized, Double-blind, Placebo- and Positive-controlled, Single-dose, 4-way Crossover Study to Evaluate the Effects of Seltorexant (JNJ-42847922) on Electrocardiogram Intervals in Healthy Adult Subjects [NCT03494907]Phase 152 participants (Actual)Interventional2018-04-09Completed
Clinical Trials to Evaluate Efficacy and Safety of Zabofloxacin Tablet 400mg and Moxifloxacin Tablet 400mg After Multi-dose Oral Administration in Patients With Acute Bacterial Exacerbation of Chronic Obstructive Pulmonary Disease. [NCT01658020]Phase 3345 participants (Actual)Interventional2012-08-31Completed
A Phase IIb, Open Label, Randomized Controlled Dose Ranging Multi-Center Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Exposure-Response Relationship of Different Doses of Delpazolid in Combination With Bedaquiline Delamanid Moxifloxaci [NCT04550832]Phase 276 participants (Actual)Interventional2021-10-22Active, not recruiting
Safety and Efficacy of Topical Moxifloxacin for Prevention of Post-Traumatic Endophthalmitis: Randomized Controlled Clinical Trial [NCT05162625]Phase 2100 participants (Anticipated)Interventional2021-12-10Recruiting
A Randomized, Double Blind, Phase II Multicenter Trial to Evaluate the Safety and Efficacy of PRO-157 Ophthalmic Solution in Three Different Dosing Regimen Versus Moxifloxacin Versus Gatifloxacin in Patients With Bacterial Conjunctivitis. [NCT02980523]Phase 2150 participants (Actual)Interventional2015-03-31Completed
A Phase 3b Randomized, Double-Blind, Multi-Center Study to Compare the Safety and Efficacy of Omadacycline IV/PO to Moxifloxacin IV/PO for Treating Adult Subjects With Community-Acquired Bacterial Pneumonia (CABP) [NCT04779242]Phase 3670 participants (Anticipated)Interventional2021-02-25Recruiting
A Thorough QTc Evaluation of the Effect of Semaglutide on Cardiac Repolarisation in Healthy Subjects: A Randomised, Double-Blind,Placebo-Controlled, Three-Arm Parallel Trial With a Nested Cross-Over Design for Positive Control With Moxifloxacin Administra [NCT02064348]Phase 1168 participants (Actual)Interventional2014-02-26Completed
Risk of QT-prolongation and Torsade de Pointes in Patients Treated With Acute Medication in a University Hospital [NCT02068170]178 participants (Actual)Observational2014-02-28Completed
[NCT02073084]Phase 156 participants (Actual)Interventional2014-01-31Completed
A Randomized, Double-Blind, Placebo and Active-Controlled, Single-Dose, 4-Treatment Crossover Study to Evaluate the Effects of E2609 on QTc Interval in Healthy Subjects [NCT02222324]Phase 160 participants (Actual)Interventional2014-08-31Completed
A Phase 1, Randomized, Double-blind, Sponsor-Open, Placebo- and Positive-Controlled Crossover Study to Investigate the Effect of Multiple Doses of Sisunatovir on QTc Interval in Healthy Adult Participants [NCT05878522]Phase 143 participants (Actual)Interventional2023-05-15Active, not recruiting
Safety and Efficacy Evaluation of Topical Moxidex Otic Solution in the Treatment of Acute Otitis Media With Otorrhea in Tympanostomy Tubes [NCT01071902]Phase 3400 participants (Actual)Interventional2010-02-28Terminated(stopped due to Management decision)
An Evaluation of Moxidex Ophthalmic Solution for Treatment of Marginal Corneal Infiltrates [NCT00579020]Phase 2144 participants (Actual)Interventional2007-12-31Terminated(stopped due to Management decision)
A Randomized, Double-Blind, Double-Dummy, Placebo- and Positive-Controlled, Crossover Study to Evaluate the Effect of WCK 5222 on the QT/QTc Interval in Healthy Volunteers [NCT03554304]Phase 160 participants (Actual)Interventional2017-02-09Completed
Adjunctive Systemic Administration of Moxifloxacin in the Treatment of Aggressive Periodontitis: Double-blind Controlled Clinical Trial [NCT02125812]Phase 440 participants (Actual)Interventional2011-08-31Completed
A Open-label, Single Sequence Clinical Trial to Investigate the Pharmacokinetic Characteristics of Second-Line Anti-Tuberculosis Agents After Multiple Oral/Intramuscular Administration in Healthy Male Volunteers [NCT02128308]Phase 116 participants (Actual)Interventional2013-11-30Completed
A Single-center, Double-blind, Randomized, Placebo- and Positive-controlled, Parallel-group, Multiple-dose, Up-titration Study of the Electrocardiographic Effects of Ponesimod in Healthy Male and Female Subjects [NCT02136888]Phase 1116 participants (Actual)Interventional2011-08-31Completed
A Phase 1, Single-dose, Randomized, 4-treatment, 4-period Crossover, Placebo- And Positive-controlled, Double-blind (Open-label For Positive Control), Sponsor-open Study To Determine The Effect Of PF-04447943 On Qtc Interval In Healthy Adult Subjects [NCT02785770]Phase 144 participants (Actual)Interventional2016-06-29Completed
A Two-part Study to Evaluate the Pharmacokinetics, Safety, and Tolerability of a High, Single Oral Dose of GSK1278863 (Part A), and a Randomized, Single-blind, Placebo- and Positive-controlled, Four-way Crossover Study to Assess the Effect of Single, Oral [NCT02293148]Phase 161 participants (Actual)Interventional2014-11-17Completed
A Randomized, Double-blind, Placebo- and Positive-controlled, Multiple-dose, Four-way, Cross-over Study to Evaluate the Effects of Repeated Oral Doses of JNJ-54861911 on Electrocardiogram Intervals in Healthy Subjects [NCT02152332]Phase 164 participants (Actual)Interventional2014-07-31Completed
Adequate Duration of Antibiotic Treatment in Community-acquired Pneumonia With High Risk Class and Adequate Initial Clinical Response [NCT03609099]Phase 4424 participants (Anticipated)Interventional2019-02-15Recruiting
A Randomized, Double-Blind, Parallel, Nested Crossover Study to Investigate the Effect of JNJ-64565111 on Cardiac Repolarization (Corrected QT Interval) Compared With Placebo in Healthy Adults: a Thorough ECG Study Employing Placebo, JNJ-64565111, and a P [NCT03606057]Phase 1188 participants (Actual)Interventional2018-07-13Completed
A Three-Way Crossover Thorough QT/QTc Study to Evaluate the Electrocardiographic Effects of a Supratherapeutic Dose of Carbidopa in Healthy Subjects [NCT06161220]Phase 136 participants (Anticipated)Interventional2023-10-30Recruiting
A Study to Determine the Concentration-Electrocardiographic Effects of Efavirenz in Healthy Subjects Enriched for CYP2B6 Polymorphisms [NCT02164812]Phase 158 participants (Actual)Interventional2014-07-31Completed
A Double-blind, Randomised, Placebo Controlled, Six-way Crossover Study Including an Open-label Positive Control (Moxifloxacin) to Assess the Influence of Via Respimat® Inhaled BI 1744 CL (Single Doses of 10 μg, 20 μg, 30 μg and 50 μg) on the QT/QTc Inter [NCT02172144]Phase 124 participants (Actual)Interventional2007-06-30Completed
A Phase I, Randomized, Double-Blinded, Placebo- and Moxifloxacin-Controlled, 4-Period Crossover Study to Evaluate the Effect of GSK2140944 on Cardiac Conduction as Assessed by 12-lead Electrocardiogram in Healthy Volunteers [NCT02257398]Phase 155 participants (Actual)Interventional2014-10-06Completed
Is Combination Antibiotic Therapy Superior to Monotherapy in the Treatment of Acute Exacerbations of Chronic Obstructive Pulmonary Disease [NCT04879030]Phase 2/Phase 3170 participants (Actual)Interventional2020-01-01Completed
A Phase 1, Single-Center, Partially Double-Blinded, Active and Placebo Controlled, Randomized 4-Way Crossover Study to Evaluate the Effect of AKB-6548 on Cardiac Repolarization Intervals in Healthy Volunteers [NCT02062203]Phase 150 participants (Actual)Interventional2014-01-31Completed
Evaluation of the Efficacy and Safety of a Short-course, Daily, 4-month Regimen Including Isoniazid, Pyrazinamide, Rifapentine and Moxifloxacin (2HZPM/2HPM) for the Treatment of Drug-susceptible Pulmonary Tuberculosis in Taiwan (ESCAPE-TB) [NCT04856644]Phase 3366 participants (Anticipated)Interventional2021-05-01Not yet recruiting
A Double-blind, Randomised, Placebo Controlled Study With Two Sequential Two-way Cross-over Parts to Demonstrate That the Influence of Pramipexole up to 4.5 mg Daily on the QT Interval of the ECG in Healthy Male and Female Volunteers is Comparable With Pl [NCT02262546]Phase 160 participants (Actual)Interventional2007-05-31Completed
A Seamless Phase 2B/C Platform Trial to Evaluate Multiple Regimens and Durations of Treatment in Pulmonary Tuberculosis [NCT06114628]Phase 22,500 participants (Anticipated)Interventional2023-12-08Not yet recruiting
A Double-Blind, Placebo-Controlled, Randomized, Crossover Design Study With an Open-Label Active Control to Evaluate the Potential of Nestorone® to Delay Cardiac Repolarization in Healthy Female Volunteers: A Thorough QT/QTc Study [NCT02236026]Phase 144 participants (Actual)Interventional2014-09-30Completed
A Randomized, Controlled, Double Blind, Multicenter, Phase 2 Study of the Safety/Tolerability and Efficacy of JNJ-32729463 Compared With Moxifloxacin for the Treatment of Subjects Requiring Hospitalization for Community-Acquired Bacterial Pneumonia (CABP) [NCT01198626]Phase 232 participants (Actual)Interventional2010-10-31Terminated(stopped due to Enrollment would not have been met prior to the end of the pneumonia season. Termination is based on slow enrollment and not related to safety or efficacy.)
A Two-Part Study Consisting of a Randomized, Placebo-Controlled, Single Dose Safety and Tolerability Study (Part A) Evaluating a Supratherapeutic Dose of Zanubrutinib Followed by a Randomized, Placebo- and Positive-Controlled, Crossover Study (Part B) to [NCT03432884]Phase 140 participants (Actual)Interventional2018-01-25Completed
A Randomized, Placebo- and Positive Controlled, Three-Way, Crossover Study to Evaluate the Effects of an Intravenous Infusion of Eravacycline (TP-434) on Cardiac Repolarization in Healthy Male and Female Subjects: A Thorough QT/QTc Study [NCT01941446]Phase 154 participants (Actual)Interventional2013-03-31Completed
A Phase 1, Double-blind, Four Period Crossover Study to Investigate the Effects of Pomalidomide (CC 4047) on the QT Interval in Healthy Male Subjects [NCT01986894]Phase 172 participants (Actual)Interventional2013-10-18Completed
Single Centre, Single Dose, Randomised, Negative and Positive-controlled, Double-blind Trazodone vs. Negative Control (Placebo), Open-label vs. Positive Control (Moxifloxacin), 5-way Cross-over QT/QTc Study [NCT03516630]Phase 120 participants (Actual)Interventional2017-03-20Completed
A Randomized, Double-Blind, Placebo- and Positive-Controlled, Multiple Dose, Four Way Crossover Study to Evaluate the Effects of Tramadol Hydrochloride on Cardiac Repolarization in Healthy Subjects at Therapeutic and Supratherapeutic Dose Levels [NCT02307864]Phase 168 participants (Actual)Interventional2014-12-04Completed
Phase I, Randomized, Parallel Group Study to Evaluate the Effect of Multiple Oral Doses of Eurartesim on the QT/QTc Interval Compared to Riamet, Placebo and Moxifloxacin in Healthy Male and Female Volunteers [NCT01103830]Phase 1287 participants (Actual)Interventional2010-02-28Completed
Pharmacokinetics and Safety of Moxifloxacin; a Dose Escalation in Patients With Tuberculosis [NCT01329250]Phase 49 participants (Actual)Interventional2011-05-31Terminated(stopped due to slow enrolment of patients and new insights)
[NCT00414011]40 participants (Actual)InterventionalCompleted
Single-center, Double-blind, Randomized, Placebo- and Positive-controlled, Parallel-group With Nested Cross-over, Multiple-dose, Up-titration Study of the Effects of Selexipag and Its Metabolite ACT-333679 on Cardiac Repolarization in Healthy Male and Fem [NCT02206204]Phase 1159 participants (Actual)Interventional2012-06-30Completed
A Randomized Double-Blinded Crossover Trial to Define the ECG Effects of Mipomersen (ISIS 301012) Using a Therapeutic and Supratherapeutic Dose Compared to Placebo and Moxifloxacin (a Positive Control) in Healthy Men and Women: A Thorough ECG Trial [NCT01090661]Phase 160 participants (Actual)Interventional2010-03-31Completed
Clinical Effectiveness and Safety Study of Moxifloxacin i.v. in the Treatment of Complicated Intra-Abdominal Infection (cIAI) [NCT01096511]1,001 participants (Actual)Observational2009-12-31Completed
Pharmacokinetic Properties of Antiretroviral and Related Drugs During Pregnancy and Postpartum [NCT00042289]1,578 participants (Actual)Observational2003-06-09Completed
A Randomized, Positive and Placebo-Controlled Trial to Evaluate the Effects of Milademetan Administration on Cardiac Repolarization in Healthy Subjects [NCT05758818]Phase 16 participants (Actual)Interventional2023-04-17Terminated(stopped due to sponsor decision)
A Thorough QTc Study Evaluating the Effect of Cagrilintide on Cardiac Repolarisation in Healthy Participants [NCT05804162]Phase 1107 participants (Actual)Interventional2023-04-12Completed
Finding the Optimal Regimen for Mycobacterium Abscessus Treatment (FORMaT) [NCT04310930]Phase 2/Phase 3300 participants (Anticipated)Interventional2020-03-02Recruiting
Study to Clinically Evaluate the QT/QTc Interval Prolongation Potential of Vericiguat in Patients With Stable Coronary Artery Disease in a 2-arm, Placebo-controlled, Randomized, Double-blind, Double-dummy Design Including a Vericiguat Multiple-dose Part W [NCT03504982]Phase 174 participants (Actual)Interventional2018-05-17Completed
A Phase 1, Randomized, Double-Blind, Placebo- and Active-Controlled Crossover Study to Evaluate the Effect of Repeat Oral Doses of ASP1941 on Cardiac Repolarization in Healthy Male and Female Adult Subjects [NCT01232413]Phase 188 participants (Actual)Interventional2010-09-30Completed
Characterization of Immune Responses in Treatment-induced Latency in Pulmonary Tuberculosis [NCT01154959]Phase 3120 participants (Actual)Interventional2010-02-28Completed
A Single-centre, Double-blind, Double-dummy, Randomised, Placebo Controlled, Four-period Crossover Study in Healthy Male Volunteers, to Assess the Effect on QT/QTc Interval of Single Oral Doses of AZD1981 (200 mg and 2000 mg) Using Moxifloxacin (Avelox®) [NCT01265641]Phase 144 participants (Anticipated)Interventional2011-01-31Completed
A Single-center, Randomized, Double-blind (for OPC-61815 and Placebo), Placebo- and Moxifloxacin Positive-controlled, 4-Period Crossover Trial to Evaluate the Effect of Single Intravenous Administration of OPC-61815 at 16 and 32 mg on QT/QTc Interval in H [NCT03510663]Phase 148 participants (Actual)Interventional2018-05-08Completed
Randomized, 4-Way, Crossover Single Dose, Placebo And Active Controlled Study To Evaluate The Effect Of Single Intravenous Doses Of Tigecycline On QTc Intervals In Healthy Subjects [NCT01287793]Phase 148 participants (Anticipated)Interventional2011-01-31Completed
A Phase 1, Randomized, Multiple Dose, Placebo And Active Controlled, 4-Way Crossover Study To Evaluate The Effect Of A Multiple Oral Dose of PF-00232798 On Qt Intervals In Healthy Subjects [NCT01140425]Phase 144 participants (Actual)Interventional2010-07-31Completed
A Single-Dose, Randomized, Double-Blind, Placebo-Controlled, Positive-Controlled, Four-Way Crossover Study to Investigate the Effect of BL-8040 (Motixafortide) on the QTc Interval in Healthy Subjects [NCT05293171]Phase 138 participants (Actual)Interventional2021-06-11Completed
The Optimization of Mycoplasm Pneumonia Antibiotic Therapy: Multi-centre, Prospective, Randomized Controlled Study [NCT01259141]208 participants (Actual)Interventional2010-10-31Completed
Comparison of Intensive Treatment Regimens and Standard Treatment Regimen for Tuberculous Meningitis: Pharmacokinetics, Pharmacodynamics and Tolerability Study [NCT01158755]Phase 260 participants (Actual)Interventional2010-10-31Completed
A Double-blind, Placebo-controlled, Safety, Tolerability and Pharmacokinetic Study in Healthy Male Volunteers in Order to Define Lanifibranor (IVA337) Supra-therapeutic Dose in a Multiple Dosing Regimen [NCT03866369]Phase 136 participants (Actual)Interventional2019-01-17Completed
A Crossover Study to Assess the Effects of FYU-981 on the QT/QTc Interval in Healthy Male and Female Volunteers [NCT02515864]Phase 248 participants (Actual)Interventional2015-08-31Completed
High Eradication Rate of Helicobacter Pylori Infection With Moxifloxacin-Based Triple Therapy in Comparison With Levofloxacin-Based Sequential Therapy: Randomized Controlled Trials [NCT05863858]Phase 3162 participants (Actual)Interventional2020-06-01Completed
A Phase 1, Randomized, Partially Double-Blind, Placebo- and Positive-controlled Study to Evaluate the Effect of Tucatinib on Cardiac Repolarization in Healthy Subjects [NCT03777761]Phase 155 participants (Actual)Interventional2018-12-06Completed
A Randomized, Phase 1, Three-Period, Placebo- and Positive-Controlled, Double-Blind, Crossover Study to Assess the Electrophysiological Effects of Exenatide at Therapeutic and Supratherapeutic Concentrations on the 12-Lead Electrocardiogram QT Interval in [NCT01297062]Phase 194 participants (Actual)Interventional2011-02-28Completed
A Randomized, Double-Blind, Double-Dummy, Positive-Controlled, Crossover Study to Determine Electrocardiographic Effects of BMS-955176 in Healthy Subjects [NCT02576119]Phase 1315 participants (Actual)Interventional2015-10-19Terminated(stopped due to This study was terminated early due to neuropsychiatric serious adverse events reported by 2 participants.)
A Study to Evaluate the Relationship Between Ramucirumab (IMC-1121B) Therapy and Corrected QT (QTc) Interval Changes in Patients With Advanced Cancer [NCT01017731]Phase 268 participants (Actual)Interventional2009-11-30Completed
[NCT00759148]Phase 31,179 participants (Actual)Interventional2008-10-31Completed
TBTC Study 31 PK/PD: Population Pharmacokinetic and Pharmacodynamic Study of Efficacy and Safety of High-Dose Rifapentine and Moxifloxacin for Treatment of Tuberculosis in the Study 31 Treatment Trial: Intensive PK Sampling [NCT02563327]Phase 360 participants (Anticipated)Interventional2016-05-30Recruiting
Comparison of Efficacy and Safety of Tricilest (Norgestimate-ethinyl Estradiol) and Diane-35 (Cyproterone Acetate-ethinyl Estradiol) in the Treatment of Acne Vulgaris [NCT00752635]Phase 448 participants (Actual)Interventional2004-09-30Completed
Multi-Centre, Prospective, Open Label, Randomized Trial to Assess the Efficacy and Safety of Moxifloxacin Versus Levofloxacin Plus Metronidazole in the Treatment of Community-Acquired Pneumonia With Aspiration Factors [NCT00752947]Phase 4186 participants (Anticipated)Interventional2008-09-30Recruiting
A Randomized, Double Blind, Single Dose, Positive and Placebo Controlled, Crossover Study of the Effects of Inhaled Carmoterol, at the Proposed Therapeutic and Supratherapeutic Doses, on the QTc Intervals in Healthy Subjects [NCT00777595]Phase 147 participants (Actual)Interventional2008-10-31Completed
A Single Center Four Part Study in Healthy Adult Subjects to Evaluate: the Safety, Tolerability and Pharmacokinetics of a Single Oral Dose and Repeat Escalating Oral Doses of GSK945237; the Effect of Linezolid on Hematology Safety Parameters; and the Effe [NCT01039610]Phase 10 participants (Actual)Interventional2009-11-30Withdrawn(stopped due to Internal decision to progress alternate molecule with more preferable profile)
A Placebo- and Positive-Controlled Study of the Electrophysiological Effects of a Single 10 μg Dose of Exenatide on the 12-Lead Electrocardiogram QT Interval in Healthy Subjects [NCT00672399]Phase 170 participants (Actual)Interventional2008-04-30Completed
Single Centre, Prospective, Comparative, Open-label, Randomised Study to Evaluate the Efficacy and Tolerability of the Combination of Moxifloxacin Plus Metronidazole Versus Piperacillin/Tazobactam for the Treatment of Patients With Intra-abdominal Abscess [NCT00629135]Phase 3180 participants (Actual)Interventional2005-11-15Completed
Comparing Oral Versus Parenteral Antimicrobial Therapy (COPAT) Trial [NCT05977868]Phase 4135 participants (Anticipated)Interventional2023-08-04Enrolling by invitation
VICTOR - Avelox® i.v. in Acute Exacerbations of Chronic Bronchitis [NCT00876577]1,206 participants (Actual)Observational2009-05-31Completed
Thorough QT Study to Evaluate the Effects of BI 1015550 as Single Doses Following Oral Administration on Cardiac Safety Parameters (Double-blind, Randomized, Placebo-controlled, Five-period Crossover, With Open-label Moxifloxacin as Positive Control) in H [NCT06107036]Phase 145 participants (Anticipated)Interventional2024-02-26Not yet recruiting
Effects of Iclepertin on the QT Interval Following Oral Administration in Healthy Male and Female Subjects (a Double-blind, Randomised, Placebo-controlled, Multiple-dose, Parallel Group With Nested Crossover Design Trial, With Moxifloxacin as Positive Con [NCT06070597]Phase 156 participants (Anticipated)Interventional2024-01-25Not yet recruiting
A Randomized Clinical Trial of Oral Clarithromycin in Community-acquired Pneumonia to Attenuate Inflammatory Responses and Improve Outcomes: the ACCESS Clinical Trial [NCT04724044]Phase 3278 participants (Actual)Interventional2021-01-25Completed
A Phase 3, Multicenter, Randomized, Double-Blind, Comparator-Controlled Study to Evaluate the Safety and Efficacy of Intravenous to Oral Delafloxacin in Adult Subjects With Community-Acquired Bacterial Pneumonia [NCT02679573]Phase 3860 participants (Actual)Interventional2016-12-14Completed
A Phase 1, Randomized, Placebo-and Positive-Controlled Crossover Study to Determine the Effect of Single-Dose GC4419 on QTc Interval in Healthy Volunteers [NCT03164109]Phase 128 participants (Actual)Interventional2017-08-18Completed
The Effect of Coadministration of BMS-955176 on the Pharmacokinetics of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norgestimate in Female Subjects [NCT02157467]Phase 146 participants (Actual)Interventional2014-06-02Completed
A Single Dose, Crossover, Placebo- and Moxifloxacin- Controlled Study of the Effects of Bosutinib on Cardiac Repolarization in Healthy Adult Subjects [NCT00914121]Phase 160 participants (Anticipated)Interventional2009-06-30Completed
Effect of LY2216684 on Oral Contraceptive Pharmacokinetics in Healthy Female Subjects [NCT01373931]Phase 120 participants (Actual)Interventional2011-06-30Completed
Randomized, Double-blind, Placebo-controlled, Positive Controlled, 3-period, 6-sequence, Crossover Study to Define the Electrocardiogram Effects of a Single Dose of Telotristat Etiprate (LX1606) 1500 mg Compared With Placebo and Open Label Moxifloxacin in [NCT02155205]Phase 148 participants (Actual)Interventional2014-05-31Completed
A Phase 1, Randomized, Single Dose, Placebo And Active Controlled, 3-Way Crossover Study To Evaluate The Effect Of A Single Oral Dose Of Lersivirine (UK-453,061) On Qt Intervals In Healthy Subjects [NCT00936871]Phase 166 participants (Anticipated)Interventional2010-01-31Completed
Safety and Efficacy of a Topical Otic Formulation in the Treatment of Peri-Operative Tube Otorrhea [NCT00578773]Phase 2303 participants (Actual)Interventional2007-11-30Completed
A Study to Evaluate the Effect of Extended Release Rosiglitazone (RSG XR) on Cardiac Conduction as Compared to Placebo and a Single Oral Dose of Moxifloxacin [NCT00884533]Phase 10 participants (Actual)Interventional2009-06-30Withdrawn(stopped due to The whole project was terminated)
A Randomized, Double-blind, Placebo- and Moxifloxacin-controlled Study to Investigate the Safety and Pharmacokinetics of Single Ascending Supratherapeutic Doses of Elinzanetant in Healthy Participants [NCT05481528]Phase 151 participants (Actual)Interventional2022-08-19Completed
A Randomized, Single-center, Placebo and Positive Control, 4-period and 4-crossover Clinical Study Evaluating the Effect of a Single-dose Oral Administration of Nemonoxacin Malate Capsule on QTc Intervals and Heart Rhythms of Healthy Subjects as Well as t [NCT03362853]Phase 148 participants (Actual)Interventional2012-06-25Completed
A PHASE 1, OPEN-LABEL, RANDOMIZED, 2-WAY CROSSOVER STUDY ON THE EFFECTS OF CC-99677 ON THE PHARMACOKINETICS OF AN ORAL CONTRACEPTIVE IN HEALTHY FEMALE SUBJECTS [NCT04718636]Phase 128 participants (Actual)Interventional2020-09-30Completed
A Double-Blind, Double-Dummy, Randomized, Moxifloxacin and Placebo Controlled, Four-Way Crossover Study of the Effects of a Single Intravenous Supra-Therapeutic Dose and Single Intravenous Therapeutic Dose of CXA-101/Tazobactam on the QT/QTC Intervals in [NCT02508753]Phase 152 participants (Actual)Interventional2010-06-30Completed
Use Of Intracameral Moxifloxacin For Prophylaxis Of Open Globe Endophthalmitis [NCT05079854]Phase 4100 participants (Anticipated)Interventional2021-10-01Recruiting
A Multicenter, Placebo-Controlled, Phase III Trial of Standard Adjuvant Chemotherapy Plus Moxifloxacin in Operable Breast Cancer [NCT05114720]Phase 3520 participants (Anticipated)Interventional2021-11-11Recruiting
A Multicenter, Randomized, Open-Label, Parallel-Controlled Clinical Study to Evaluate the Efficacy and Safety of Sitafloxacin in Adult Subjects With Acute Exacerbation of Chronic Obstructive Pulmonary Disease [NCT05400369]Phase 4268 participants (Anticipated)Interventional2022-08-10Recruiting
A Randomized, Double-Blinded, Positive-Controlled, Placebo-Controlled, 3-Way Crossover Study to Determine the Electrocardiographic Effects of BMS-791325 in Healthy Subjects [NCT02084953]Phase 159 participants (Actual)Interventional2014-04-30Completed
A Single Ascending Dose, Randomized, Double-Blind, Double-Dummy, Placebo- and Positive Controlled Study to Evaluate the Effect of ACH-0144471 on the QT Interval in Healthy Adult Subjects [NCT05016206]Phase 133 participants (Actual)Interventional2018-07-26Completed
Optimizing the Antibiotic Treatment of Uncomplicated Acute Appendicitis: a Prospective Randomised Multicenter Study (The APPAC II Study) [NCT03236961]552 participants (Anticipated)Interventional2017-04-03Active, not recruiting
A Double-center, Randomized, Double-blinded, 2-way Crossover, Placebo-controlled Study: Comparison of Single Oral Dose 400mg Moxifloxacin-induced QT Prolongation Between Healthy Chinese Volunteers and Caucasian Volunteers [NCT02119091]Phase 180 participants (Anticipated)Interventional2014-04-30Recruiting
Steroids and Cross-linking for Ulcer Treatment [NCT04097730]Phase 3279 participants (Actual)Interventional2020-09-24Active, not recruiting
A Single-Dose, Open-Label, Randomized, 2-Way Crossover Pivotal Study to Assess the Bioequivalence of NGM/EE Tablets Manufactured at 2 Different Facilities [NCT02127593]Phase 1101 participants (Actual)Interventional2013-06-30Completed
Assessment of Electrophysiological Effects of 150 mg and 600 mg of Dabigatran Etexilate as Single Dose on the QT Interval in Healthy Female and Male Subjects. A Randomised, Placebo Controlled, Double-blind Three-way Crossover Study With an Open Label Posi [NCT02170987]Phase 140 participants (Actual)Interventional2006-03-31Completed
A Randomized, Double-blind, Positive and Placebo-controlled, Single-dose, Crossover Study of the Effects of CHF5993 pMDI (BDP/FF/GB) at the Proposed Therapeutic and Supratherapeutic Doses, on the Cardiovascular Safety in Healthy Subjects [NCT05830071]Phase 195 participants (Actual)Interventional2023-03-29Completed
A Non-randomized, Non-Interventional, Prospective, Multicenter, Post Marketing Surveillance Study to Assess the Antibacterial Effectiveness and Safety of 0.5% Moxifloxacin Hydrochloride Ophthalmic Solution in Perioperative (Preoperative and Postoperative) [NCT05413980]102 participants (Anticipated)Observational2023-11-15Not yet recruiting
Assessment of the Effect of 5 mg and 100 mg of BI 1356 as Single Dose on the QT Interval in Healthy Female and Male Subjects. A Randomised, Placebo Controlled, Double-blind, Four-way Crossover Study With Moxifloxacin as Positive Control [NCT02183467]Phase 144 participants (Actual)Interventional2008-01-31Completed
A Single-Center, Randomized, Masked Study Comparing the Concentration of Besifloxacin, Gatifloxacin, and Moxifloxacin in Human Conjunctiva After a Single Topical Instillation [NCT00905762]Phase 1119 participants (Actual)Interventional2009-03-31Completed
A Phase IIb, Open-Label, Randomized Controlled Dose Ranging Multi-Center Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Exposure-Response Relationship of Different Doses of BTZ-043 in Combination With Bedaquiline and Delamanid in Adult S [NCT05926466]Phase 290 participants (Anticipated)Interventional2023-09-21Recruiting
Treatment of Patients With Acute Sinusitis in Daily Practice [NCT00930488]6,777 participants (Actual)Observational2007-03-31Completed
A Comparative Study of Ampicillin/Sulbactam Versus Moxifloxacin in the Treatment of Complicated Intra-abdominal Infections [NCT00952796]Phase 4100 participants (Anticipated)Interventional2009-01-31Completed
A Phase I, Double-blind, Double-dummy, Randomized, Placebo Controlled and Active Controlled Trial to Evaluate the Effect of TMC278 25 mg Daily at Steady-state and the Effect of Efavirenz (EFV) 600 mg Daily at Steady-state on the QT/QTc Interval, in 2 Rand [NCT00744809]Phase 1120 participants (Actual)Interventional2008-08-31Completed
CAPRIVI: Community Acquired Pneumonia: Treatment With Avelox® in Hospitalized Patients [NCT00987792]2,595 participants (Actual)Observational2009-09-30Completed
A Phase I, Single-Center, Double-Blind, Randomized, Placebo- and Positive- Controlled, Parallel Group, Thorough QT/QTc Study to Evaluate the Effect of Talampanel on Cardiac Repolarization in Healthy Male and Female Volunteers [NCT00964730]Phase 1135 participants (Anticipated)Interventional2009-10-31Completed
A Double-blind, Double-dummy, Randomized, Placebo- and Active-controlled, Four-period Crossover Trial to Evaluate the Effect of Telaprevir (TVR) on the QT/QTc Interval in Healthy Subjects [NCT00973388]Phase 144 participants (Actual)Interventional2009-10-31Completed
Randomized, Double-Blinded, Placebo-Controlled, Open Label Positive- Controlled, Four-Way Crossover Study of the Electrocardiographic Effects of BMS-708163 in Healthy Subjects [NCT00979316]Phase 162 participants (Actual)Interventional2009-09-30Completed
Thorough QT/QTc Study of Staccato® Prochlorperazine for Inhalation in Healthy Volunteers [NCT00543062]Phase 148 participants (Actual)Interventional2007-10-31Completed
A Single-center, Randomized, Blinded, Placebo- and Active-controlled Crossover Study to Evaluate the Effect of Saroglitazar Magnesium on the QTc Interval in Healthy Volunteers [NCT04045769]Phase 152 participants (Actual)Interventional2019-08-19Completed
Randomized, Embedded, Multifactorial Adaptive Platform Trial for Community- Acquired Pneumonia [NCT02735707]Phase 310,000 participants (Anticipated)Interventional2016-04-11Recruiting
A Randomized, Double-Blind, Placebo- and Positive-Controlled, Single- and Multiple-Dose, 4-Way Crossover Study to Evaluate the Effects of Domperidone on Cardiac Repolarization in Healthy Subjects [NCT01643889]Phase 144 participants (Actual)Interventional2012-07-31Completed
Evaluation of the Effect of Benzonatate on QT Intervals Following Single Dose Administration of Benzonatate to Healthy Volunteers [NCT02207699]Phase 168 participants (Actual)Interventional2014-05-31Completed
A Randomized, Blinded, Placebo- and Positive-Controlled, Four-Period, Crossover-Design Thorough QT/QTc (TQT) Study to Evaluate the Effect of Orelabrutinib on Cardiac Repolarization in Healthy Subjects [NCT05660720]Phase 148 participants (Anticipated)Interventional2022-11-19Active, not recruiting
A Phase 1, Double-blind, Single-dose, Randomized, Placebo and Active-Controlled, Four-Way Crossover Study Evaluating the Effects of Bemnifosbuvir on Cardiac Repolarization in Healthy Adult Subjects [NCT05905484]Phase 135 participants (Actual)Interventional2023-04-25Completed
A Double-Blind, Cross-Over Placebo-Controlled and Active-Controlled Trial To Evaluate The Effect Of A Supratherapeutic Dose Of MK-8189 On The QTc Interval In Participants With Schizophrenia [NCT05893862]Phase 184 participants (Anticipated)Interventional2023-06-26Recruiting
Safety Profile Comparison of Undiluted Intracameral Moxifloxacin vs. Levofloxacin in Cataract Surgery [NCT05741632]Phase 168 participants (Actual)Interventional2023-02-01Completed
A Double-blind, Double-dummy, Randomized, 3-Period Cross-over, Placebo- and Positive-controlled Study to Evaluate the Effect of JNJ-63623872 on Cardiac Repolarization Interval in Healthy Subjects [NCT02658825]Phase 166 participants (Actual)Interventional2016-01-31Completed
Two-Part, Randomized, Placebo and Active-Controlled, Double-Blind, Thorough QT Study Evaluating the Effects of Intravenous Exenatide on Cardiac Repolarization in Healthy Male and Female Volunteers [NCT02650479]Phase 182 participants (Actual)Interventional2016-01-31Completed
The Effect of Pink Grapefruit Juice on the QT Interval in Healthy Volunteers and Patients With Congenital Long QT Syndrome [NCT02680080]25 participants (Actual)Interventional2016-12-01Completed
Efficacy of Moxifloxacin, Amoxicillin+Metronidazole for Aggressive Periodontitis Treatment [NCT02839421]Phase 436 participants (Actual)Interventional2015-12-31Active, not recruiting
A Randomized, Double-Blind, Placebo- and Active-Controlled, 3-Way Crossover Study in Healthy Subjects to Determine the Effect of Omaveloxolone on QTc Interval [NCT05927649]Phase 130 participants (Actual)Interventional2023-07-11Completed
A Single-Dose, Randomized, Placebo- and Active-Control, Four-Way, Cross-Over Study for the Evaluation of the Effect of Tebipenem Pivoxil Hydrobromide (TBPM-PI-HBr) on the QT/QTc Intervals in Adult Healthy Subjects [NCT04238195]Phase 124 participants (Actual)Interventional2020-01-19Completed
Prospective, Randomized, Double-blind, Multicenter, Multinational Study Comparing Efficacy and Safety of Moxifloxacin 400 mg po od for 14 Days With Ofloxacin 400 mg po Bid Plus Metronidazole 500 mg po Bid for 14 Days in Patients With Uncomplicated Pelvic [NCT00683865]Phase 3749 participants (Actual)Interventional2003-04-30Completed
A Phase I Single Centre, Randomized, Double Blind (Except For Moxifloxacin), Placebo And Active Controlled, Four Way Cross Over Study Investigating The Effect Of Single Therapeutic And Supra Therapeutic Doses Of Fedovapagon On The QT/QTC Interval In Healt [NCT02537288]Phase 143 participants (Actual)Interventional2015-10-31Completed
Laboratory-masked, Randomized Parallel, Comparative, Pilot Study on the Bioavailability of Vigamox in the Aqueous Humor When Administered Either as Commercially Available Eye Drops or in a Spray Form [NCT00666042]16 participants (Anticipated)Interventional2009-02-28Completed
Prospective, Multicenter, Open, Uncontrolled Trial to Evaluate the Time to Bacterial Eradication and Key Symptom Relief in the Treatment of Acute Bacterial Maxillary Sinusitis With Moxifloxacin 400 mg QD [NCT00668304]Phase 4192 participants (Actual)Interventional2004-06-30Completed
A Single Blinded Clinical Trial Comparing Polytrim Ophthalmic Solution and Moxifloxacin Ophthalmic Solution for Treatment of Conjunctivitis. [NCT00581542]Phase 4124 participants (Actual)Interventional2007-03-31Completed
A Randomized, Double-Blind, Placebo- and Moxifloxacin Positive-Controlled (Open-Label), Cross-Over Study to Evaluate the Potential Effect of Naltrexone and Bupropion Extended-Release Combination on Cardiac Repolarization in Healthy Subjects [NCT02735603]Phase 184 participants (Actual)Interventional2016-04-30Completed
A Prospective, Randomized, Open Label, Active Comparator, Multicenter, National Trial to Compare the Efficacy and Safety of Sequential IV/PO Moxifloxacin 400 mg Once Daily Versus IV Amoxicillin/Clavulanate 2,0/0,2 g Every 8 Hours Followed by Oral Amoxicil [NCT00828971]Phase 316 participants (Actual)Interventional2008-11-30Completed
A Randomized, Blinded Placebo-Controlled Study to Evaluate the Effect of Repeat Oral Doses of Pazopanib (GW786034) on the Electrocardiogram (ECG) With Focus on Cardiac Repolarization (QTc Duration) in Subjects With Solid Tumors [NCT00861029]Phase 12 participants (Actual)Interventional2009-03-19Completed
COVID-19: A MULTIPART, PHASE 1 STUDY WITH RANDOMIZED, DOUBLE-BLIND, SPONSOR-OPEN, PLACEBO-CONTROLLED, SINGLE- AND MULTIPLE-DOSE ESCALATION TO EVALUATE THE SAFETY, TOLERABILITY AND PHARMACOKINETICS OF PF-07817883 AND OPTIONAL OPEN-LABEL, RANDOMIZED STUDY T [NCT05580003]Phase 194 participants (Actual)Interventional2022-10-17Completed
A Prospective, Randomized, Double-dummy, Double-blind, Multicenter Trial Comparing the Safety and Efficacy of Intravenous Moxifloxacin 400 mg IV QD 24 Hours to That of Ertapenem 1.0 g IV QD 24 Hours for 5 to 14 Days for the Treatment of Subjects With Comp [NCT00492726]Phase 3804 participants (Actual)Interventional2006-07-31Completed
Prospective, Multicenter, Randomized, Double-Blind, Placebo Controlled Trial to Evaluate the Efficacy and Safety of Moxifloxacin 400 mg QD for 5 Days Versus Placebo in the Treatment of Acute Bacterial Sinusitis [NCT00492024]Phase 3374 participants (Actual)Interventional2005-01-31Completed
A Phase 1, Randomized, Double Blind, Placebo and Active Controlled, Parallel Study to Evaluate the Effect of Repeat Doses of Isavuconazole on Cardiac Repolarization in Healthy Adult Subjects [NCT01565720]Phase 1161 participants (Actual)Interventional2012-03-31Completed
Prospective, Multicenter, Randomized, Double Blind, Parallel Arm Study to Evaluate the Efficacy and Safety of Moxifloxacin 400 mg OD for 7 Days Versus a Standard Antibiotic Therapy for 10 Days in the Treatment of Acute Bacterial Rhino Sinusitis [NCT00493038]Phase 4293 participants (Actual)Interventional2006-02-28Terminated(stopped due to The study was prematurely terminated due to slow enrollment beyond the planned study timelines.)
A Randomized, Double-Blind, Positive-Controlled, Placebo-Controlled, 4-Period Crossover Study to Investigate the Electrocardiographic Effects of BMS-986165 in Healthy Subjects [NCT03541564]Phase 184 participants (Actual)Interventional2018-05-30Completed
A Two-part, Single-center, Single-dose, Randomized, Double-blind, Double-dummy, Placebo-controlled, Positive-controlled, Four-way Crossover Study to Investigate the Effect of RO7033877 on the QT/QTc Interval in Healthy Subjects [NCT02165332]Phase 164 participants (Actual)Interventional2014-07-31Completed
A Single Dose, Crossover, Placebo- and Moxifloxacin-Controlled Study of the Effects of HKI-272 on Cardiac Repolarization in Healthy Adult Subjects [NCT00708903]Phase 160 participants (Actual)Interventional2008-05-31Completed
Prospective, Randomized Study Comparing Effect on Wound Healing of Vigamox (Moxifloxacin 0.5% Ophthalmic Solution) and Cravit (Levofloxacin 0.5% Ophthalmic Solution) Administered Post-Surgically in Patients Undergoing Cataract Extraction [NCT00840580]Phase 479 participants (Actual)Interventional2009-01-31Completed
[NCT00703313]Phase 472 participants (Anticipated)Interventional2008-05-31Completed
A Prospective, Randomized, Double Dummy, Double Blind, Multi-center Multinational Trial Comparing the Efficacy and Safety of Moxifloxacin 400 mg PO QD 24 Hours for 14 Days to That of Levofloxacin 500 mg PO QD 24 Hours Plus Metronidazole 500 mg BID for 14 [NCT00453349]Phase 3460 participants (Actual)Interventional2007-01-31Completed
A Double-blind, Randomized, Placebo-controlled Study to Investigate Chronic Intermittent-pulse-therapy of Moxifloxacin as a Prevention of Acute in Exacerbation Out-patients With Chronic Bronchitis. [NCT00473460]Phase 31,404 participants (Actual)Interventional2004-10-31Completed
Pharmacokinetic Evaluation of Moxifloxacin IV to Enteral Switch Therapy in Intensive Care Patients [NCT00458900]Phase 24 participants (Actual)Interventional2007-07-31Completed
MAESTRAL - A Prospective, Multinational, Multicenter, Randomized, Double Blind, Double Dummy, Controlled Study Comparing the Efficacy and Safety of Moxifloxacin to That of Amoxicillin Clavulanic Acid for the Treatment of Subjects With Acute Exacerbations [NCT00656747]Phase 41,372 participants (Actual)Interventional2008-03-31Completed
A Double Blind, Randomized, Repeat-Dose, Parallel Group Study to Define the ECG Effects of Lixivaptan Using a Clinical and a Supratherapeutic Dose, Compared to Placebo and Moxifloxacin (a Positive Control), in Healthy Adult Men and Women: A Thorough ECG S [NCT00675701]Phase 1298 participants (Actual)Interventional2008-05-31Completed
A Multi-Center, Open-Label, Randomized Study of the Pharmacokinetics of Azithromycin Versus Moxifloxacin in Conjunctiva and Aqueous Humor Following Single or Multiple Ocular Administration of AzaSite Ophthalmic Solution, 1% or Vigamox in Subjects Undergoi [NCT00575380]Phase 4116 participants (Actual)Interventional2007-12-31Completed
A Double-blind, Randomized, Four-period Crossover Study to Assess the Effects of Single Oral Dose Dapagliflozin Administration on QTc Interval Compared to Placebo, Using AVELOX™ (Moxifloxacin) as a Positive Control, in Healthy Male Volunteers Age 18 to 45 [NCT00688493]Phase 136 participants (Actual)Interventional2007-07-31Completed
A Randomized, Evaluator-Blinded, Phase 3 Study to Compare the Safety and Efficacy of PTK 0796 With Linezolid in the Treatment of Adults With Complicated Skin and Skin Structure Infection [NCT00865280]Phase 3143 participants (Actual)Interventional2009-04-04Terminated(stopped due to Terminated)
Side Effect Profiles of Brand Name Versus Generic Oral Contraceptives [NCT00775190]12 participants (Actual)Interventional2008-10-31Terminated(stopped due to unale to recruit , progress report not filed by PI)
Pharmacokinetics and Pharmacodynamics Sub-study for TB-PRACTECAL Clinical Trial ( PRACTECAL-PKPD) [NCT04081077]Phase 2/Phase 3240 participants (Anticipated)Interventional2019-08-06Active, not recruiting
A Randomized, Double-Blind, Placebo- and Positive-Controlled, Four-way Crossover Study to Investigate the Effects of Single Intravenous Doses of Difelikefalin (CR845) on the QTc Interval in Healthy Subjects [NCT04019574]Phase 157 participants (Actual)Interventional2019-06-20Completed
A Phase 1, Randomized, Placebo- and Active-controlled Crossover Study to Evaluate the Effects of Sapropterin Dihydrochloride Oral Administration on QTc Intervals in Healthy Adult Subjects [NCT00789568]Phase 156 participants (Actual)Interventional2008-10-31Completed
A National, Prospective, Randomized, Open Label Study to Assess the Efficacy and Safety of IV/PO Moxifloxacin vs IV Ceftriaxone + IV Azithromycin Followed by PO Amoxicilline/Clavulanate and PO Clarithromycin in Subjects With Community-acquired Pneumonia [NCT00717561]Phase 360 participants (Actual)Interventional2008-02-29Completed
A Randomized, Double-Blind, Single-Dose, Placebo- and Positive-Controlled Crossover Study to Evaluate the Effect of Therapeutic and Supratherapeutic Exposure to CS-3150 on QTc Interval Duration in Healthy Male and Female Subjects [NCT04019652]Phase 155 participants (Actual)Interventional2015-11-19Completed
Comparison of Moxifloxacin With Ciprofloxacin/Metronidazole as Adjunctive Therapy to Mechanical Treatment of Patients With Chronic Periodontitis [NCT00805558]Phase 476 participants (Actual)Interventional2009-02-28Completed
A Randomised, Controlled, Open-Label, Phase II-III Trial to Evaluate the Safety and Efficacy of Regimens Containing Bedaquiline and Pretomanid for the Treatment of Adult Patients With Pulmonary Multidrug Resistant Tuberculosis [NCT02589782]Phase 2/Phase 3552 participants (Actual)Interventional2017-01-31Active, not recruiting
Determination of Optimum Duration of Treatment With Bromfenac (Xibrom) Eyedrops Following Cataract Surgery [NCT00758199]Phase 449 participants (Actual)Interventional2008-07-31Completed
The Pharmacokinetics of Topical Levofloxacin 1.5% vs Topical Moxifloxacin 0.5% [NCT04214821]Phase 1/Phase 2128 participants (Anticipated)Interventional2019-09-23Recruiting
A Blinded, Randomized Crossover Trial to Define the ECG Effects of TA-1790 (Avanafil) Using a Single Clinical and a Supratherapeutic Dose Compared to Placebo and Moxifloxacin in Healthy Men: A Thorough ECG Trial [NCT00769041]Phase 157 participants (Actual)Interventional2008-10-31Completed
A Prospective Trial Evaluating a Intracanalicular Insert Delivery System Compared to Traditional Topical Drops in Controlling Post-operative Pain and inFlammation in Subjects Undergoing Sequential Bilateral Cataract Surgery [NCT04205916]Phase 450 participants (Anticipated)Interventional2019-11-04Recruiting
A Phase I, Double-blind, Double-dummy, Placebo-controlled, Randomised, Four-period Crossover Study to Assess the Effects of Single Oral Doses of ZD4054 (Zibotentan) (10mg and 30mg) on QTc Interval Compared to Placebo, Using AVELOX (Moxifloxacin) as a Posi [NCT00713336]Phase 140 participants (Anticipated)Interventional2008-06-30Completed
A Phase 1, Single-Center, Double-Blind, Randomized, Placebo- and Positive Controlled, Double-Dummy, Parallel-Group, Repeated Dose Study With a Nested Cross-Over Comparison Between Moxifloxacin and Placebo to Evaluate the Effect of MD1003 on Cardiac Repola [NCT04168723]Phase 164 participants (Anticipated)Interventional2019-11-11Recruiting
EFFECTS OF MOXIFLOXACIN AND GEMIFLOXACIN ON BLOOD GLUCOSE LEVEL OF EUGLYCEMICS:A PRE-CLINICAL AND CLINICAL STUDY [NCT04692623]Phase 125 participants (Actual)Interventional2021-03-01Completed
Efficacy of Antibiotic Steroid Combination Compared With Individual Administration in Prevention of Post Operative Inflammation in Patients Having LASIK Surgery [NCT00330824]64 participants (Actual)Interventional2006-04-30Completed
An Evaluation of the Safety and Efficacy of the Administration of a Fixed Combination of Moxifloxacin 0.5% and Dexamethasone 0.1% Eye Drops Compared With the Individual Administration of Moxifloxacin 0.5% and Dexamethasone 0.1% in the Treatment of Bacteri [NCT00732446]Phase 3100 participants (Anticipated)Interventional2008-08-31Completed
A Randomized, Multiple Dose, Placebo and Active Controlled 3-way Crossover Study to Investigate the Effects of Esreboxetine on QTc Interval in Healthy Volunteers [NCT00809289]Phase 140 participants (Anticipated)Interventional2008-12-31Completed
A Single Center, Three Period, Randomized, Three-way Crossover, Double-blind Placebo And Moxifloxacincontrolled Study To Assess The Effects Of Effexor Xr On Cardiac Repolarization In Healthy Adult Subjects [NCT02637193]Phase 154 participants (Actual)Interventional2015-12-31Completed
A Single-center, Randomized, Double-blind, Placebo- and Moxifloxacin-controlled, Phase 1 Study to Assess the Effect of Single Therapeutic and Supratherapeutic Doses of Daridorexant on the QT Interval Duration in Healthy Subjects [NCT04250506]Phase 136 participants (Actual)Interventional2020-02-28Completed
A Prospective, Randomized, Double Dummy, Double Blind, Multinational, Multicenter Trial Comparing the Safety and Efficacy of Sequential (Intravenous/Oral) Moxifloxacin 400 mg OD to Intravenous Piperacillin/Tazobactam 4.0/0.5 g Every 8 Hours Followed by Or [NCT00402727]Phase 3813 participants (Actual)Interventional2006-09-30Completed
A Single-centre, Double-blind, Double-dummy, Randomised, Placebo-controlled, Four-period Crossover Study to Assess the Effect of Single Oral Doses of AZD5672 (600 mg and 150 mg) on QT/QTc Interval, Compared to Placebo, Using Moxifloxacin (Avelox®) as a Po [NCT00887770]Phase 164 participants (Anticipated)Interventional2009-04-30Completed
A Randomized Clinical Trial Comparing the Effect of Moxifloxacin Versus Gatifloxacin Following Pterygium Excision on Corneal Epithelial Healing and Epithelial Toxicity. [NCT00892918]40 participants (Anticipated)Interventional2009-06-30Not yet recruiting
Interventional, Randomised, Partially Double-blind, Crossover, Positive-controlled, Single-dose Trial Investigating the Effect of LEO 152020 on Cardiac Repolarisation in Healthy Men and Women [NCT05508776]Phase 128 participants (Actual)Interventional2022-09-16Completed
A Double-Blind, Randomised, Multicentre, Placebo-Controlled, 4-Ways Crossover Study to Investigate the Effect on the QT/QTc Interval of Repeated and Escalating Doses of AZD3480 During 6 Days, Using Moxifloxacin as a Positive Control, in Healthy Male Volun [NCT00686179]Phase 175 participants (Actual)Interventional2008-01-31Completed
To Compare the Efficacy of Topical Vigamox Eye Drops at Tid 3 Days Prior to Intravitreal Injection Versus Tid 1 Day Prior to Intravitreal Injection [NCT00690313]Phase 422 participants (Actual)Interventional2008-08-31Completed
Thorough QT/QTc Study of Staccato® Loxapine for Inhalation in Healthy Volunteers [NCT00874237]Phase 148 participants (Actual)Interventional2009-04-30Completed
A Randomized, Double-blind, Placebo- & Positive-Controlled, Parallel Group, Dose Escalating Study to Evaluate the Effect of Buprenorphine Delivered by Buprenorphine Transdermal System at 10- and 40-mg Dose Levels on QT Intervals in Healthy Adult Volunteer [NCT01148537]Phase 1132 participants (Actual)Interventional2004-07-31Completed
A Single Dose, Double Blind, Randomized, Crossover Placebo- and Moxifloxacin (Open Label)-Controlled Study to Evaluate the Cardiac Effects of a Novel Food Ingredient in Healthy Male Subjects [NCT02616913]48 participants (Actual)Interventional2013-03-31Completed
A Randomized, Double-blind, Placebo- and Positive-Controlled, Parallel Group, Dose Escalating Study of the Effect of Hydrocodone Bitartrate (HYD) Extended-Release Tablets at Doses up to 160 mg on QT/QTc in Healthy Adult Subjects [NCT02243241]Phase 1208 participants (Actual)Interventional2012-11-30Completed
Parallel-group Study of Ocular Penetration of Peri-operative Topically Administered Fluoroquinolones With Cataract Surgery [NCT00924729]Phase 450 participants (Actual)Interventional2009-09-30Completed
A Phase I, Randomized, Gender Stratified, Double-Blind, Placebo- and Positive-Controlled, Three Period Crossover Trial to Assess the Effect of Guanfacine Hydrochloride on QT/QTc Interval in Healthy Men and Women [NCT00672984]Phase 183 participants (Actual)Interventional2008-04-18Completed
A Blinded Randomized Parallel Trial to Define the ECG Effects of Bardoxolone Methyl Using a Clinical and a Supratherapeutic Dose Compared to Placebo and Moxifloxacin (a Positive Control) in Healthy Men and Women: A Thorough ECG Trial. [NCT01689116]Phase 1179 participants (Actual)Interventional2012-08-31Completed
A Single-center, Single-dose, Randomized, Double-blind, Double-dummy, Placebo-controlled, Positive-controlled, Four-way Crossover Study to Investigate the Effect of Danoprevir With Low Dose Ritonavir (DNV/r) on the QT/QTc Interval in Healthy Subjects [NCT01398293]Phase 152 participants (Actual)Interventional2011-08-31Completed
SYMPROVE III: Health Services Research Study for Treatment of the Moderate and Severe AECB [NCT00879008]345 participants (Actual)Observational2009-12-31Completed
A Study to Evaluate the Effect of a Single 250 mg Oral Dose of GSK1349572 on Cardiac Conduction as Assessed by 12-lead Electrocardiogram Compared to Placebo and a Single Oral Dose of Moxifloxacin (ING111856). [NCT00996021]Phase 142 participants (Actual)Interventional2009-09-30Completed
Prospective, Randomized, Open-Labeled, Active-Controlled Comparison of Moxifloxacin Versus Ceftriaxone in the Treatment of Primary Pyogenic Liver Abscess: A Pilot Study [NCT00895089]Phase 424 participants (Actual)Interventional2009-05-31Completed
A Phase I Thorough QT/QTc Study To Evaluate The Effect of Therapeutic and Supratherapeutic Multiple Doses of Prucalopride on Cardiac Repolarisation in Healthy Male and Female Volunteers [NCT00903747]Phase 1120 participants (Actual)Interventional2009-01-31Completed
An Open-Label Study to Evaluate Pharmacokinetic Profile of Agile TCDS AG200-15 and to Compare Exposure to Ethinyl Estradiol to Oral Contraceptive (Orthocyclen®) in Healthy Female Volunteers [NCT01243580]Phase 136 participants (Actual)Interventional2009-08-31Completed
A Randomized, Placebo- and Positive-Controlled, Multiple-Dose, 4-Way Crossover Study to Evaluate the Effects of Domperidone on Cardiac Repolarization in Chinese Healthy Subjects [NCT02816853]Phase 144 participants (Actual)Interventional2016-05-31Completed
A Randomized, Double-blind, Placebo and Positive Controlled, Parallel Group Trial to Investigate the Effect of Multiple Doses of NOMAC-E2 on QT/QTc Interval in Healthy Women [NCT00779532]Phase 1189 participants (Actual)Interventional2008-05-31Completed
A Phase 1, Single-Dose, Randomized, Placebo- and Positive-Control, Four-Way, Crossover Study for the Evaluation of the Effect of Epetraborole on QT Intervals in Healthy Adult Subjects [NCT05995444]Phase 124 participants (Actual)Interventional2023-06-05Completed
Comparative Evaluation of Intensified Short Course Regimen and Standard Regimen for Adults TB Meningitis : an Open-label Randomized Controlled Trial [NCT05917340]Phase 3372 participants (Anticipated)Interventional2024-03-31Not yet recruiting
A Randomized, Observer-masked, Parallel-group, Multicenter Trial Evaluating the Ocular Penetration of 1.5% Levofloxacin Ophthalmic Solution and 0.5% Moxifloxacin Ophthalmic Solution in Subjects Undergoing Corneal Transplant Surgery [NCT00764582]Phase 460 participants (Anticipated)Interventional2008-09-30Terminated(stopped due to Study terminated due to lack of enrollment.)
A Randomized, Double-Blind (Periods 1 to 3), Placebo- and Positive-Controlled, Single Dose, 4-Period, Crossover Study to Evaluate the Effects of Esketamine on Cardiac Repolarization in Healthy Subjects [NCT02737605]Phase 162 participants (Actual)Interventional2016-07-01Completed
Pharmacokinetics of Standard First and Second Line Anti-TB Drugs in the Lung and Lesions of Subjects Elected for Resection Surgery [NCT00816426]Phase 119 participants (Actual)Interventional2008-12-29Completed
A Single-Center, Randomized, Double-Blinded, Placebo-Controlled, 4-way Cross-over Study to Assess the Effect of a Single Oral Dose of AZD3293 Administration on QTc Interval Compared to Placebo, Using Open-Label AVELOX (Moxifloxacin) as a Positive Control, [NCT02040987]Phase 152 participants (Actual)Interventional2014-01-31Completed
A Phase 1, Randomized, Double-Blind, Placebo- and Active- Controlled, Crossover Study to Evaluate the Effect of Repeat Oral Doses of YM443 on Cardiac Repolarization in Healthy Male and Female Adult Subjects [NCT00850746]Phase 180 participants (Actual)Interventional2009-02-28Completed
Intracameral Moxifloxacin for Prevention of Postcataract Endophthalmitis [NCT02595359]Phase 21,000 participants (Actual)Interventional2013-01-31Completed
Evaluation of the Effects of Multiple Therapeutic and Supratherapeutic Doses of Cebranopadol on Cardiac Repolarization in Healthy Subjects [NCT03958123]Phase 1171 participants (Actual)Interventional2013-07-10Completed
A Phase 1, Randomized, Double-Blind, Placebo- and Positive-Controlled, Thorough QT Study to Evaluate the Effect of Ampreloxetine on Cardiac Repolarization in Healthy Subjects [NCT04688632]Phase 172 participants (Actual)Interventional2021-01-18Completed
A Two-part, Phase I, Double-blind, Placebo- and Positive-controlled Crossover Study to Investigate the Effects of Brensocatib on QT Interval in Healthy Subjects [NCT05355935]Phase 148 participants (Actual)Interventional2022-04-27Completed
A Thorough QTc Trial Evaluating the Effect of SNAC on Cardiac Repolarisation in Healthy Male Subjects [NCT02911870]Phase 184 participants (Actual)Interventional2016-09-23Completed
Acceptability of the NuvaRing Among College and Graduate Students [NCT00635570]Phase 4273 participants (Actual)Interventional2008-07-31Completed
A Randomized, Parallel Group Safety Evaluation of Electrocardiographic Intervals and Blood Pressure in Normal Healthy Volunteers After Nebivolol, Atenolol, Moxifloxacin, or Placebo Administration After Single and Repeated Doses [NCT00158093]Phase 1260 participants Interventional2003-06-30Completed
GIANT - Greatest International Antiinfective Trial With Avelox® [NCT00932802]50,000 participants (Actual)Observational2004-02-29Completed
Comparison of the Effect Between Levofloxacin and Moxifloxacin on the Culture Conversion After 3 Months Treatment Among MDR-TB Patients; Prospective Multicenter Randomized Open Label Phase III Trial [NCT01055145]Phase 3182 participants (Actual)Interventional2010-03-31Terminated
ARTOS - Avelox® in Routine Treatment of Complicated Skin and Skin Structure Infections [NCT00997997]6,127 participants (Actual)Observational2005-10-31Completed
A Single Center, Randomized, Double-blinded, Placebo-controlled, Open-label, Positive-controlled, Four-way Crossover Study to Assess the Effect of a Single Oral Dose NKTR-118 Administration on QTc Interval Compared to Placebo, Using AVELOX (Moxifloxacin) [NCT01325415]Phase 145 participants (Actual)Interventional2011-04-30Completed
A Phase 1, Single Center Randomized, Three-way Crossover, Double-blinded, Placebo- And Moxifloxacin-controlled Thorough Qt (Tqt) Study To Determine The Effects Of Sertraline (Zoloft (Registered)) On The Cardiac Repolarization In Healthy Subjects [NCT02651623]Phase 154 participants (Actual)Interventional2016-01-31Completed
Effect of BMS-650032 on the Pharmacokinetics of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norgestimate (Ortho Tri- Cyclen (R)) in Healthy Female Subjects [NCT01063023]Phase 120 participants (Actual)Interventional2010-01-31Completed
Prospective, Multi-center, Randomized, Non-blind Trial to Assess the Efficacy and Safety of Moxifloxacin Versus Sulbactam/Ampicillin in the Treatment of Pulmonary Abscess and Aspiration Pneumonia [NCT01045902]Phase 3139 participants (Actual)Interventional2001-02-28Completed
Double-blind, Randomized, Placebo- and Positive-controlled, Parallel-group Trial to Assess the Potential Electrocardiographic Effects of Rotigotine Transdermal System up to 120 cm2/54.0 mg/Day in Subjects With Advanced-stage Idiopathic Parkinson's Disease [NCT00292227]Phase 1130 participants (Actual)Interventional2006-01-31Completed
Randomized, Open Label, Multiple Dose Phase I Study of the Early Bactericidal Activity of Linezolid, Gatifloxacin, Levofloxacin, and Moxifloxacin in HIV-non-infected Adults With Initial Episodes of Sputum Smear-Positive Pulmonary Tuberculosis [NCT00396084]Phase 1/Phase 270 participants (Actual)Interventional2004-02-10Completed
A Phase 3B Multicenter, Randomized, Double-Blind, Double-Dummy Comparative Trial To Evaluate The Efficacy and Safety Of Azithromycin SR (Microspheres Formulation) Versus Moxifloxacin For The Treatment Of Acute Exacerbation Of Chronic Bronchitis (AECB). [NCT00254566]Phase 3398 participants (Actual)Interventional2006-02-28Completed
Safety, Tolerability and Pharmacokinetics of Single Dose Intravenous Moxifloxacin in Pediatric Patients [NCT01049022]Phase 131 participants (Actual)Interventional2010-05-31Completed
A Study to Evaluate the Clinical and Microbial Efficacy of 0.6% ISV-403 Compared to Vigamox in the Treatment of Bacterial Conjunctivitis [NCT00348348]Phase 31,161 participants (Actual)Interventional2006-06-30Completed
A Randomized, Three Period Crossover Thorough QT (TQT) Study Evaluating the Effect of ETX2514 on Cardiac Repolarization in Healthy Male or Female Volunteers [NCT03985410]Phase 132 participants (Actual)Interventional2019-05-23Completed
A Double Blind, Placebo Controlled, Positive Controlled, Randomized, Crossover Study to Assess the Effect of Cangrelor at the Therapeutic Dose and a Supratherapeutic Dose Level on the QT/QTc Interval in Healthy Volunteers [NCT00699504]Phase 167 participants (Actual)Interventional2008-06-30Completed
Topical Treatment of Bacterial Conjunctivitis and Its Effect on Microbial Flora [NCT00312338]Phase 4137 participants (Actual)Interventional2006-06-30Completed
A Double-Blind Randomized Crossover Trial to Define the Ecg Effects of Droxidopa Using a Clinical and a Supratherapeutic Dose Compared With Placebo and Moxifloxacin (a Positive Control) in Healthy Men and Women: a Thorough ECG Trial [NCT01327066]Phase 152 participants (Actual)Interventional2011-03-31Completed
Phase 1 Crossover Study to Assess the Effects of SQ109 on QTc Interval in Healthy Subjects [NCT01874314]Phase 10 participants (Actual)InterventionalWithdrawn
A Single-Center, Double-Blind, Randomized, Placebo- and Positive-Controlled, Parallel Group, Thorough QT/QTc Study to Evaluate the Effect of Custirsen (640 mg) on Cardiac Repolarization in Healthy Men [NCT01874561]Phase 1155 participants (Actual)Interventional2013-05-31Completed
A Randomized, Double-blind, Placebo-controlled, Two-way Crossover Trial to Compare Moxifloxacin Induced QT Interval Prolongation in Japanese and Korean Healthy Subjects [NCT01876316]40 participants (Actual)Interventional2011-11-30Completed
A Phase 1, Randomized, Placebo and Active Controlled, Double-Blind, Parallel, Electrocardiogram Study to Evaluate the Effect of Lumacaftor in Combination With Ivacaftor on the QT/QTc Interval in Healthy Subjects [NCT01910415]Phase 1200 participants (Actual)Interventional2013-06-30Completed
Randomized, Double-blind, Placebo-controlled, Positive-controlled, 4-period, 4-way Crossover Study to Define the Electrocardiogram Effects of a Single Dose of LX4211 800 mg and 2000 mg Compared With Placebo and Open-label Moxifloxacin in Healthy Subjects: [NCT01913002]Phase 163 participants (Actual)Interventional2013-07-31Completed
A Single Centre, Placebo Controlled, Phase I Study to Evaluate the Effect of Glucose and Moxifloxacin on Cardiac Repolarisation in Male and Female Patients With Type I Diabetes. [NCT01984827]Phase 124 participants (Actual)Interventional2019-02-10Completed
A Comparison of Prophylactic Antibacterial Efficacy of Besivance Versus VIGAMOX Administered for Three Days and One Hour Prior to Phacoemulsification [NCT01296542]Phase 460 participants (Actual)Interventional2011-05-31Completed
Effect of Gatifloxacin 0.3% and Moxifloxacin 0.5% on Epithelial Wound Healing After Photorefractive Keratectomy [NCT00569881]22 participants (Actual)Observational2007-01-31Completed
[NCT00630019]Phase 496 participants (Anticipated)Interventional2008-02-29Completed
Moxifloxacin In Situ Gel as an Adjunct in the Treatment of Periodontal Pocket: A Randomized Clinical Trial. [NCT02016157]Phase 45 participants (Actual)Interventional2011-09-30Completed
A Study to Evaluate the Effect of GSK1265744 150mg Administered Orally Every 12h x 3 Doses on Cardiac Conduction as Assessed by 12-lead Electrocardiogram Compared to Placebo and a Single Oral Dose of Moxifloxacin [NCT02027454]Phase 142 participants (Actual)Interventional2014-01-31Completed
A Randomized, Double-blind, 2-way Crossover, Placebo-controlled Study to Investigate the Influence of a Single-dose of Moxifloxacin on the QTc Interval in Healthy Male and Female Subjects for Positive Control Validation in Selected Centers of the PATENT-1 [NCT01014247]Phase 156 participants (Actual)Interventional2009-11-30Completed
A Randomized, Double-Blind, Double-Dummy, Placebo- and Positive- Controlled, Crossover Study to Evaluate the Effect Of WCK 2349 on the QT/QTc Interval in Health Volunteers [NCT02217930]Phase 180 participants (Actual)Interventional2014-08-31Completed
Assessment of the Effect of 25 mg and 200 mg of BI 10773 as Single Dose on the QT Interval in Healthy Female and Male Subjects. A Randomised, Placebo Controlled, Double-blind, Five-period Crossover Phase-I-study With Moxifloxacin as Positive Control [NCT01195675]Phase 130 participants (Actual)Interventional2010-08-31Completed
A Study of Avelox for Treatment of Elderly Patients With Community Acquired Pneumonia [NCT00665327]Phase 4401 participants (Actual)Interventional2002-11-30Completed
A Randomized, Double-blind, Placebo- and Positive-controlled, Single-dose, 4-way Crossover Study to Evaluate the Effects of Aticaprant (JNJ-67953964) on Electrocardiogram Intervals in Healthy Adult Participants [NCT05387759]Phase 160 participants (Actual)Interventional2022-05-30Completed
TBTC Study 28: Evaluation of a Moxifloxacin-based, Isoniazid-sparing Regimen for Tuberculosis Treatment [NCT00144417]Phase 2433 participants (Actual)Interventional2006-02-28Completed
A Randomized, Double-Blind, Placebo- and Positive-Controlled, Single-Dose, Four-Way Crossover Study to Evaluate the Effects of Ibrutinib on Cardiac Repolarization in Healthy Subjects [NCT02271438]Phase 128 participants (Actual)Interventional2014-10-31Completed
Reduction of Premature Discontinuation of Contraceptive Implants by Advance Provision of an OCP-based Participant Intervention: Randomized Clinical Trial [NCT04828824]Phase 4600 participants (Anticipated)Interventional2021-06-18Recruiting
Use of Intracameral Moxifloxacin for the Prevention of Acute Endophthalmitis Following Cataract Surgery: a Controlled and Randomized Clinical Trial [NCT02770729]Phase 33,640 participants (Actual)Interventional2017-01-31Terminated
A Phase II Trial to Evaluate the Early Bactericidal Activity, Safety and Tolerability of the Following: TMC207 Alone, TMC207 Plus Pyrazinamide,TMC207 Plus PA-824,PA-824 Plus Pyrazinamide and PA-824 Plus Pyrazinamide and Moxifloxacin, in Adult Patients Wit [NCT01215851]Phase 285 participants (Actual)Interventional2010-10-31Completed
Economic Evaluation of New MDR TB Regimens (PRACTECAL EE) [NCT04207112]Phase 2/Phase 3200 participants (Anticipated)Interventional2020-10-20Recruiting
An Evaluation of the Prophylactic Efficacy and Safety of the Administration of the Combination Formulation of Moxifloxacin 0.5% and Dexamethasone 0.1% Eye Drops in Inflammation and Infection Post-cataract Surgery [NCT00870103]Phase 464 participants (Actual)Interventional2008-09-30Completed
A Prospective, Randomized Controlled Study for the Efficacy and Safety of the Substitution of Pyrazinamide and Ethambutol With Moxifloxacin During the Intensive Phase of Treatment of Pulmonary Tuberculosis [NCT04187469]286 participants (Anticipated)Interventional2020-03-01Not yet recruiting
A Double-blind, Double-dummy, Randomized, 3-Period Cross-over, Placebo- and Positive Controlled Study to Evaluate the Effect of ALS-008176 on Cardiac Repolarization Interval in Healthy Subjects [NCT02833831]Phase 1103 participants (Actual)Interventional2016-06-02Completed
Prospective, Randomized, Open, Multicentre Study About the Effect of an Empirical Antibiotic Monotherapy With Meropenem (Meronem®) Versus a Combination Therapy With Moxifloxacin (Avalox®) on Organ Dysfunction in Patients With Severe Sepsis and Septic Shoc [NCT00534287]Phase 3600 participants (Actual)Interventional2007-10-31Completed
A Phase I, Multicenter, Randomized, Double-blind, Double-dummy, Placebo- and Positive-Controlled Study to Investigate the Effects of CBP-307 on the QTc Interval in Healthy Subjects [NCT04818229]Phase 1112 participants (Actual)Interventional2021-06-01Completed
A Phase III Single-blind, Randomised Placebo Controlled Trial of Long Term Therapy in Patients With Stable COPD Using Moxifloxacin, Azithromycin and Doxycycline: a Bayesian Decision Analysis, Including Other Criteria, Will be Used to Distinguish the Optim [NCT01398072]Phase 3200 participants (Anticipated)Interventional2011-12-31Recruiting
A Randomized, Double-blind, Parallel, Nested Crossover Study to Investigate the Effect of Albiglutide on Cardiac Repolarization (Corrected QT Interval) Compared With Placebo in Healthy Male and Female Subjects: A Thorough ECG Study Employing Placebo, Albi [NCT01406262]Phase 194 participants (Actual)Interventional2011-07-06Completed
A Randomized, Double-Blind, Multi-Center Study to Evaluate the Efficacy and Safety of Intravenous to Oral Solithromycin (CEM-101) Compared to Intravenous to Oral Moxifloxacin in the Treatment of Adult Patients With Community-Acquired Bacterial Pneumonia [NCT01968733]Phase 3863 participants (Actual)Interventional2013-11-30Completed
A Methodological Open-Label Cross-Over Controlled Study To Assess The Effect Of Drugs On Ventricular Repolarisation and QT Interval At Fixed Heart Rate Under Autonomic Blockade [NCT00174512]Phase 136 participants Interventional2005-03-31Completed
Prospective, Doubleblind, Randomized Multicenter Study to Proof the Clinical and Bacteriological Non-inferiority of Ampicillin/Amoxicillin Versus Moxifloxacin in Hospitalized Patients With Non-severe Community-acquired Pneumonia [NCT00887276]Phase 4290 participants (Actual)Interventional2008-11-30Terminated
Swiss PACK-CXL (Photoactivated Chromophore for Infectious Keratitis Cross-linking) Multicenter Trial for the Treatment of Infectious Keratitis [NCT02717871]Phase 335 participants (Actual)Interventional2016-03-31Completed
The Clinical Safety of Topical Levofloxacin 1.5% vs Topical Moxifloxacin 0.5% [NCT04212429]Phase 1/Phase 2128 participants (Anticipated)Interventional2019-09-23Recruiting
Evaluation of Possible Effects on the QT/ QTc Interval of Rupatadine in Healthy Volunteers: A Randomised, Parallel, Placebo and Positive Controlled Study [NCT00199225]Phase 1160 participants Interventional2005-02-28Completed
Clinical Trial to Investigate the Effect on Corrected QT Interval Prolongation by Psychotropic Drugs in Healthy Korean Adults After a Single Oral Administration of Escitalopram, Quetiapine, and Moxifloxacin [NCT01871701]Phase 140 participants (Actual)Interventional2012-11-30Completed
A Randomised, Double-blind, Placebo and Active Controlled Crossover Study to Assess the Effect of Single Dose Administration of 2 Doses of Imeglimin on QT/QTc Intervals in Healthy Subjects [NCT02924337]Phase 155 participants (Actual)Interventional2016-09-30Completed
Impact of Different DAV132 Dose Regimens (From 2 to 22.5 g/Day During 7 Days, Bid and Tid) on the Fecal Moxifloxacin Concentrations and the Intestinal Microbiota of Healthy Volunteers Treated With Moxifloxacin 400 mg/Day During 5 Days [NCT02917200]Phase 1150 participants (Actual)Interventional2016-05-11Completed
A Randomized, 2-Part, Crossover Trial to Evaluate the Effect of Carbetocin on the QT/QTc Interval in Healthy Subjects [NCT05924321]Phase 140 participants (Actual)Interventional2023-05-25Completed
A Phase 1 Blinded, Placebo-controlled Crossover Study to Evaluate the Effects of Oral TR 701 Free Acid on the Electrocardiogram [NCT01461460]Phase 148 participants (Actual)Interventional2011-11-28Completed
Influence of the Administration of DAV132 7.5g Tid for 7 Days on the Fecal Levels of Moxifloxacin During and After a 5-day Oral Treatment With Moxifloxacin 400mg Oad in Healthy Volunteers [NCT02176005]Phase 144 participants (Actual)Interventional2014-03-31Completed
Routine Therapy Plus Moxifloxacin in Advanced Breast Cancer [NCT03405168]Phase 235 participants (Actual)Interventional2018-01-01Completed
A Randomized, Single-dose, Crossover Study of the Effects of SEP-363856 on Electrocardiogram (ECG) Intervals in Subjects With Schizophrenia [NCT04369391]Phase 1150 participants (Actual)Interventional2020-06-18Completed
Prospective Study Comparing the Effectiveness of Zymar and Vigamox for Preoperative Antibiotic Sterilization of the Ocular Surface After Loading Dose [NCT00347828]Phase 440 participants Interventional2006-06-30Active, not recruiting
A Multinational, Prospective, Randomized, Double-blind Study to Investigate the Efficacy and Safety of Sequential Intravenous/Oral Moxifloxacin in Comparison to Intravenous Levofloxacin Plus Intravenous Ceftriaxone Followed by Oral Levofloxacin, in the Tr [NCT00431678]Phase 3738 participants (Actual)Interventional2004-01-31Completed
Safety and Efficacy of Intracameral Zimoxin (0.1% Moxifloxacin Solution) for Prevention of Endophthalmitis After Cataract Surgery [NCT03244072]Phase 2/Phase 360,000 participants (Anticipated)Interventional2024-06-01Not yet recruiting
A Randomized, Placebo-Controlled, Two-Period, Crossover Study to Evaluate the Effect of Lurasidone HCl on Oral Contraceptive Pharmacokinetics in Healthy Female Subjects [NCT00549666]Phase 123 participants (Actual)Interventional2007-08-31Completed
[NCT00874887]Phase 466 participants (Actual)Interventional2009-03-31Completed
A Phase 1, Randomized, Partial Double-Blind, Placebo- and Positive-Controlled, Three-way Crossover Study to Evaluate the Effect of MT-7117 on the QT/QTc Interval in Healthy Subjects [NCT05241535]Phase 129 participants (Actual)Interventional2022-01-12Completed
A Phase I, Single-Centre, Randomised, Placebo and Positive- Controlled, Parallel-Group Study of the Electrocardiographic Effects of TA-8995 in Healthy Male and Female Subjects [NCT02241759]Phase 1136 participants (Actual)Interventional2014-08-31Completed
A Four-Arm, Randomized, Crossover, Placebo and Active Controlled Study for the Evaluation of the Effect of Therapeutic and Supratherapeutic Doses of CTP-543 on the QT/QTc Intervals in Healthy Volunteers [NCT05192369]Phase 148 participants (Actual)Interventional2022-01-04Completed
A Randomized, Double-blind, Placebo- and Active-controlled, 3-way Crossover, Phase 1 Study to Evaluate the Effect of EVP-6124 at Therapeutic and Supratherapeutic Concentrations Following a 2-dose EVP-6124 Regimen on the QT Interval in Healthy Male and Fem [NCT01487135]Phase 160 participants (Actual)Interventional2011-12-31Completed
A Double-blind, Randomised, Placebo Controlled, Three-way Cross-over Study With an Open Label Positive Control (Moxifloxacin) to Assess the Influence of Inhaled Tiotropium Once Daily Over Twelve Days on the QTC Interval of the ECG in Healthy Male and Fema [NCT00257452]Phase 156 participants Interventional2004-10-31Completed
Pharmacokinetic Interaction Study of Rifampicin, Isoniazid and Moxifloxacin in Tuberculosis Patients in Bandung, Indonesia [NCT00306319]Phase 223 participants Interventional2006-01-31Completed
Dropless Pars Plana Vitrectomy Study [NCT05331664]Phase 4168 participants (Anticipated)Interventional2022-07-25Recruiting
An Evaluation of the Safety and Efficacy of Moxifloxacin AF Ophthalmic Solution 0.5% for the Treatment of Bacterial Conjunctivitis in India [NCT00332293]Phase 3695 participants (Actual)Interventional2006-05-31Completed
Efficacy of Antibiotic Steroid Combination Compared With Individual Administration in Prevention of Postoperative Inflammation in Patients Having Cataract Surgery [NCT00331084]132 participants (Actual)Interventional2006-04-30Completed
A Randomized, Placebo-Controlled, Double-Blind, Four-way Crossover Study to Assess the Effect of Single Oral Doses of Retosiban on Cardiac Repolarization, With Moxifloxacin as a Positive Control in Healthy Volunteers [NCT01702376]Phase 152 participants (Actual)Interventional2012-10-03Completed
Comparison of Oral and Patch Forms of Hormonal Contraception on Plasma Lipoproteins, Glycemia, Clotting Factors, Indices of Inflammation and Vascular Reactivity [NCT00439972]Phase 236 participants (Anticipated)Interventional2007-02-28Active, not recruiting
Randomized, Controlled, Multicenter Phase III Study for the Efficacy and Tolerability of Triple Therapy With Esomeprazole, Moxifloxacin and Amoxicillin for Rescue Therapy of Helicobacter Pylori Infection [NCT00455806]Phase 3132 participants Interventional2007-01-31Recruiting
Acute Cholecystitis - Early Laparoscopic Surgery Versus Antibiotic Therapy and Delayed Elective Cholecystectomy = ACDC-study [NCT00447304]Phase 3644 participants (Anticipated)Interventional2006-10-31Completed
Pharmacokinetic Issues in the Use of Moxifloxacin Plus Rifapentine [NCT00460759]Phase 115 participants (Actual)Interventional2007-06-30Terminated
A Single-Dose, Double-Blind, Crossover, Placebo- and Moxifloxacin (Open-Label)-Controlled Study of the Effects of Lecozotan SR on Cardiac Repolarization in Healthy Adult Subjects [NCT00499642]Phase 10 participants Interventional2007-06-30Completed
TBTC Study 27: An Evaluation of the Activity and Tolerability of Moxifloxacin During the First Two Months of Treatment for Pulmonary Tuberculosis--A Double-Blind, Randomized, Multicenter Study by the Tuberculosis Trials Consortium [NCT00140309]Phase 2350 participants Interventional2003-07-31Completed
Prospective Randomized Comparison of Zymar(Gatifloxacin) and Vigamox (Moxifloxacin) in Killing Conjunctival Bacterial Flora Following a One-hour [NCT00466570]0 participants (Actual)Interventional2007-04-30Withdrawn
Phase 2C Clinical Trial of Novel, Short-course Regimens for the Treatment of Pulmonary Tuberculosis: CRUSH-TB (Combination Regimens for Shortening TB Treatment) [NCT05766267]Phase 2/Phase 3288 participants (Anticipated)Interventional2023-03-01Not yet recruiting
An Open-Label, Randomized Assessment of the Concentrations of Besifloxacin, Moxifloxacin, or Gatifloxacin in the Aqueous Humor of Subjects After a Single Topical Dose [NCT00824070]Phase 1105 participants (Actual)Interventional2009-02-28Completed
A Randomized, Partially Double-Blind, Four-Period, Four-Treatment, Crossover Study Investigating the Placebo-Corrected Effects of a Therapeutic Dose (100 mg) and a Supratherapeutic Dose (300 mg) of ITF2357 (Givinostat) and Moxifloxacin on QT/QTC Interval [NCT04821063]Phase 131 participants (Actual)Interventional2021-04-13Completed
TBTC Study 27/28 PK: Pharmacokinetic Issues in the Use of Moxifloxacin for Treatment of Tuberculosis [NCT00164463]Phase 272 participants (Actual)Interventional2004-07-31Completed
A Randomized, Double-Blind, Multi-Center Study to Evaluate the Efficacy and Safety of Oral Solithromycin (CEM-101) Compared to Oral Moxifloxacin in the Treatment of Adult Patients With Community-Acquired Bacterial Pneumonia [NCT01756339]Phase 3860 participants (Actual)Interventional2012-12-31Completed
A Phase II Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of the Combination of Moxifloxacin Plus PA-824 Plus Pyrazinamide After 8 Weeks of Treatment in Adult Patients With Newly Diagnosed Drug-Sensitive or Multi D [NCT01498419]Phase 2207 participants (Actual)Interventional2012-03-31Completed
Pilot Study on Bioavailability of Vigamox Administered as Drops vs. as Spray [NCT00565630]16 participants (Anticipated)Interventional2008-01-31Withdrawn(stopped due to Replaced with ongoing study)
Evaluation of the Effects of Therapeutic and Supra-therapeutic Single Doses of SKY0402 Given as Subcutaneous Injection on the QT/QTc Interval in Young Healthy Volunteers. A Prospective, Randomized, Placebo- and Positive-controlled, Double Blind, Single-ce [NCT00485667]Phase 148 participants (Actual)Interventional2007-06-30Completed
Evaluation of the Safety and Efficacy of VIGADEXA Ophthalmic Gel Compared to VIGADEXA Ophthalmic Solution in Preventing Inflammation and Infection Following Cataract Surgery [NCT01515826]Phase 30 participants (Actual)Interventional2014-03-31Withdrawn(stopped due to Management decision)
A Thorough QTc Evaluation of the Effect of Liraglutide on Cardiac Repolarization in Healthy Volunteers: A Randomized, Double-blind, Placebo-controlled, Two Period Crossover Study Followed by Open-label Moxifloxacin (Positive Control) Administration [NCT01516255]Phase 164 participants (Actual)Interventional2006-07-31Completed
A Randomized, Double-blind, Single Dose Crossover Study to Assess the Effect of Gabapentin Enacarbil on Cardiac Conduction as Compared With Placebo and Moxifloxacin in Healthy Volunteers [NCT01516372]Phase 152 participants (Actual)Interventional2012-01-31Completed
A Randomised, Placebo-controlled, Incomplete Block, Four Period Crossover , Repeat Dose Study to Evaluate the Effect of the Inhaled GSK573719/Vilanterol Combination and GSK573719 Monotherapy on Electrocardiographic Parameters, With Moxifloxacin as a Posit [NCT01521377]Phase 1100 participants (Actual)Interventional2011-12-19Completed
A Randomized, Double-blind, Placebo-controlled and Open-label Active-controlled, 4-period Crossover Trial to Evaluate the Effect of BIA 9-1067 on Cardiac Repolarization in Healthy Adult Men and Women [NCT01532115]Phase 164 participants (Actual)Interventional2010-05-31Completed
A Randomized, Double-Blind, Double-Dummy Pharmacokinetic and Exploratory Electrocardiogram (ECG) Safety Study of a Standard Acute Gout Regimen [NCT01018420]Phase 118 participants (Actual)Interventional2007-11-30Completed
A Phase I, Double-blind (Selumetinib [AZD6244; ARRY-142886] [Hyd-Sulfate]), Placebo-controlled, Open-Label (Moxifloxacin) Positive-controlled, Randomized, Three-period Crossover Study to Assess the Effects of Single Oral Dose of Selumetinib (75 mg) on QTc [NCT02056392]Phase 154 participants (Actual)Interventional2014-03-31Completed
A Randomized, Double-Blind, Placebo and Positive-Controlled, Crossover Study to Evaluate the Effect of IV ACHN-490 Injection on the QT/QTc Interval in Healthy Volunteers [NCT01514929]Phase 164 participants (Actual)Interventional2011-10-31Completed
Study to Evaluate the Effect of Efavirenz Coadministration on the Pharmacokinetics of the Active Moieties of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norgestimate in Healthy Female Subjects [NCT00399685]Phase 128 participants (Actual)Interventional2006-12-31Completed
AVANTI - Avelox® in Acute Exacerbations of Chronic Bronchitis [NCT00846911]2,672 participants (Actual)Observational2008-04-30Completed
Assistant Professor, Ophthalmology Department, Al Azhar University [NCT05428683]84 participants (Actual)Interventional2020-12-03Completed
A Single Part, Four-Way Crossover, Randomized, Partially-Blinded Study to Evaluate the Effect of Intravenous ANG-3777 on Baseline-Adjusted QT/QTc Interval in the Fasted State in Healthy Male and Female Subjects [NCT04898907]Phase 148 participants (Anticipated)Interventional2021-06-30Not yet recruiting
[NCT00407017]Phase 40 participants InterventionalCompleted
A Phase IIB, Open-Label, Randomized Controlled Dose Ranging Multi-Center Trial to Evaluate the Safety, Tolerability, Pharmacokinetics and Exposure-Response Relationship of Different Doses of Sutezolid in Combination With Bedaquiline, Delamanid and Moxiflo [NCT03959566]Phase 275 participants (Actual)Interventional2021-05-06Completed
Oral Empirical Therapy of Fever in Low-Risk Neutropenic Cancer Patients: A Prospective, Double-Blind, Randomized, Multicenter Trial Comparing Monotherapy (Single Daily Dose Moxifloxacin) With Combination Therapy (Ciprofloxacin Plus Amoxicillin/Clavulanic [NCT00062231]351 participants (Actual)Interventional2002-04-30Terminated(stopped due to low accrual)
A Four Period, Four-Arm, Crossover Design, Randomized, Placebo and Active Controlled Study for the Evaluation of the Effect of Therapeutic and Supratherapeutic Single-Dose ANX-188 on the QT/QTc Intervals in Healthy Volunteers [NCT01790087]Phase 172 participants (Actual)Interventional2013-02-28Completed
The Effect of ALKS 5461 on QT Intervals in Healthy Volunteers [NCT02479308]Phase 1129 participants (Actual)Interventional2015-06-30Completed
A Parallel-arm, Double-blind, Placebo and Positive Controlled Multiple Oral Dose Administration Trial to Evaluate the Effects of OPC-34712 on QT/QTc in Subjects With Schizophrenia or Schizoaffective Disorder [NCT01423916]Phase 1218 participants (Actual)Interventional2011-07-31Completed
A Single-center, Double-blind for Cenerimod, Open-label for Moxifloxacin, Placebo-controlled, Parallel-group, Randomized Study in Healthy Male and Female Subjects to Investigate I: the Effect of Cenerimod on the QTc Interval II: the Effect of Cenerimod on [NCT04255277]Phase 197 participants (Actual)Interventional2020-01-31Completed
Phase I, Double-Blind, Randomized, Single-Center, Five-Period Crossover Study to Assess the Effects of Single Oral Doses of 400 mg and 1000 mg of PA-824 and 400 mg of PA-824 Plus 400 mg of Moxifloxacin on QTc Interval Compared to Placebo, Using AVELOX™ (M [NCT01674218]Phase 174 participants (Actual)Interventional2012-09-30Completed
New Super-short Course Regimen for Retreatment Pulmonary Tuberculosis [NCT02331823]Phase 4864 participants (Anticipated)Interventional2013-06-30Recruiting
A Phase II Randomized, Open-label Trial of a Rifapentine Plus Moxifloxacin-Based Regimen for Intensive Phase Treatment of Smear-Positive Pulmonary Tuberculosis [NCT00728507]Phase 2121 participants (Actual)Interventional2009-11-30Terminated(stopped due to Funding withdrawn)
Evaluation of Energy Drink Consumption on Electrocardiographic, Vascular and Hematologic Parameters in Young Healthy Volunteers: A Randomized, Double Blind, Active-Controlled, Crossover Study [NCT03021616]2 participants (Actual)Interventional2017-06-26Terminated(stopped due to Results from sister study at University of the Pacific were conclusive.)
[NCT01792700]Phase 4648 participants (Actual)Interventional2003-01-31Completed
A Randomised Placebo - Controlled Double Blind Trial Comparing 1) a Two Month Intensive Phase of Ethambutol, Moxifloxacin, Rifampicin, Pyrazinamide Versus the Standard Regimen (Ethambutol, Isoniazid, Rifampicin, Pyrazinamide) and 2) a Treatment Shortening [NCT00864383]Phase 31,931 participants (Actual)Interventional2008-01-31Completed
A Multiple Arm, Multiple Stage, Phase 2, OL, Randomized, Controlled Trial to Evaluate 4 Treatment Regimens of SQ109, Increased Doses of Rifampicin, and Moxifloxacin in Adults With Newly Diagnosed, Smear-positive Pulmonary Tuberculosis [NCT01785186]Phase 2365 participants (Actual)Interventional2013-04-30Completed
Clinical Evaluation of Systemic Moxifloxacin Compared to Amoxicillin Plus Metronidazole Adjunct to Non-surgical Treatment in Generalized Aggressive Periodontitis: A Randomized Clinical Trial [NCT02223702]Phase 439 participants (Actual)Interventional2011-05-31Completed
[NCT00464438]Phase 4171 participants (Actual)Interventional2007-06-30Completed
Aqueous Absorption and Pharmacokinetics of Besivance Versus VIGAMOX in Patients Undergoing Phacoemulsification [NCT01296191]Phase 4120 participants (Actual)Interventional2011-05-31Completed
A Randomized, Double-Blind, Placebo- and Positive Controlled, Crossover, Thorough QT/QTc Study to Evaluate the Effects of a Therapeutic and Supratherapeutic Dose of Ecopipam (EBS-101) on Cardiac Repolarization in Healthy Subjects [NCT05841160]Phase 129 participants (Actual)Interventional2023-03-15Completed
Efficacy of Moxifloxacin 0.5%/Prednisolone 1% Fixed Combination Compared With Individual Administration of Moxifloxacin 0.5% and Prednisolone 1% in the Prevention of Post Operative Inflammation in Patients Having Lasik Surgery [NCT01603030]Phase 366 participants (Anticipated)Interventional2012-06-30Not yet recruiting
A Randomized, Double-Blind, Two-Part, Parallel-Group, Comparative Study to Evaluate Blood Folate Levels in Women Taking an Oral Contraceptive With and Without Folic Acid [NCT00301587]Phase 30 participants (Actual)InterventionalWithdrawn(stopped due to Company decision to not fund further development of women's health new drug development programs.)
Plasma and Abscess Fluid Pharmacokinetics of Cefpirome and Moxifloxacin After Single and Multiple Dose Administration [NCT00280514]Phase 420 participants (Anticipated)Interventional2006-01-31Completed
Cardiovascular Safety Study of 0.1 and 0.3 mmol/kg Magnevist® Injection at Two Injection Rates (Bolus and 10 mL/15 Sec.) in Normal Subjects Following a Randomized, Cross-over Design Using Placebo and a Concurrent Positive Control [NCT00310596]Phase 171 participants (Actual)Interventional2004-01-31Completed
Randomized, Double Blinded, Placebo-Controlled Trial of Antibacterial Prophylaxis for the Prevention of Bacterial Infections in the Post-Engraftment Phase After Allogeneic Hematopoeitic Stem Cell Transplantation [NCT00324324]Phase 3240 participants (Anticipated)Interventional2006-05-31Terminated
[NCT00335088]Phase 3500 participants (Anticipated)Interventional2006-06-30Recruiting
A Double-Blind Study to Evaluate the Pharmacokinetics of an Oral Contraceptive Containing Norgestimate and Ethinyl Estradiol When Co-administered With Dolutegravir in Healthy Adult Female Subjects [NCT01498861]Phase 116 participants (Actual)Interventional2011-12-31Completed
Single Dose Safety, Tolerability And Pharmacokinetics Of Escalating Intravenous Doses Of Linezolid Followed By Evaluation Of The Effect Of Single Intravenous Doses Of Linezolid On QTc Interval In Healthy Subjects [NCT00795145]Phase 149 participants (Actual)Interventional2008-12-31Completed
A Single-Center, Randomized, Blinded, Placebo- and Active-Controlled Crossover Study to Evaluate the Effect of Dexpramipexole (BIIB050) on the QTc Interval in Healthy Volunteers [NCT01511029]Phase 168 participants (Actual)Interventional2012-01-31Completed
A Thorough QTc Evaluation of the Effect of Cotadutide on Cardiac Repolarization in Healthy Participants: A Randomized, Double-blind, Placebo-controlled, 3-arm Parallel Study With a Nested Crossover Design for Positive Control With Moxifloxacin Administrat [NCT05668936]Phase 131 participants (Actual)Interventional2023-01-03Terminated(stopped due to Discontinuing the development of cotadutide, a daily injectable GLP-1/glucagon co-agonist, is based on strategic pipeline considerations. The premature closure is not due to any newly observed safety signals or a change in the risk/benefit profile.)
A Single-center, Randomized, Double-blinded, 2-way Crossover, Placebo-controlled Study to Assess the QT/QTc Interval After Administration of Single Oral Dose of 400mg Moxifloxacin in Healthy Chinese Subjects [NCT01653990]36 participants (Anticipated)Interventional2012-07-31Recruiting
Special Drug Use Investigation - Assessment of Efficacy and Safety in Treating Secondary Infection of Chronic Respiratory Disease [NCT01690533]497 participants (Actual)Observational2008-05-13Completed
A Placebo-Controlled, Single Dose, Dose Escalation (Part A) and a Placebo- and Positive-Controlled Study of the Effect on the Electrocardiographic QT Interval of a Single Dose (Part B) of LY3009104 in Healthy Subjects [NCT01536951]Phase 162 participants (Actual)Interventional2012-02-29Completed
A Four-Arm, Parallel Design, Randomized, Double-Blinded, Placebo and Active Controlled Study for the Evaluation of the Effect of Maximum Therapeutic and Supratherapeutic Single-Dose ATX-101 on the QT/QTc Intervals in Healthy Volunteers [NCT01706679]Phase 1218 participants (Actual)Interventional2012-10-31Completed
A Randomized, 2-Part, Single-Dose, Crossover Study to Evaluate the Effect of Aficamten Administration on QT/QTc Interval in Healthy Participants [NCT05924815]Phase 144 participants (Actual)Interventional2023-05-15Completed
A Single Center Phase 1 Double Blind Study to Evaluate the Effect of Losmapimod on Cardiac Conduction as Compared to Placebo and Moxifloxacin in Healthy Adult Subjects [NCT01756495]Phase 156 participants (Actual)Interventional2013-01-10Completed
A Multi-center, Randomized, Open-label, Placebo-controlled, 3-way Crossover Study to Investigate the Effect on QT/QTc Interval of Moxifloxacin After a Single Dose in Healthy Male Subjects [NCT01756521]Phase 139 participants (Actual)Interventional2013-01-31Completed
Bacteriology and Sputum and Systemic Inflammation in Steady-state, Acute Exacerbation and Recovery of Bronchiectasis [NCT01761214]80 participants (Anticipated)Interventional2012-09-30Recruiting
A Double-Blind, Randomized, Placebo-Controlled, Parallel-Design, Study With an Open-Label Positive-Control, to Assess the Cardiac Safety of Oritavancin in Healthy Volunteers [NCT01762839]Phase 1150 participants (Actual)Interventional2013-01-31Completed
A Randomized, Placebo- And Positive-Controlled Cross-Over Study To Evaluate The Effect Of Tafamidis On The QTC Interval In Healthy Volunteers [NCT01775761]Phase 142 participants (Actual)Interventional2013-01-31Completed
A Randomized, Double-Blind, Double-Dummy, Placebo- and Positive-Controlled, Four-Way Crossover Study Evaluating ECG Intervals in Healthy Adults Receiving a Single, Oral Dose of JNJ-28431754 at Therapeutic and Supra-Therapeutic Doses [NCT01787357]Phase 160 participants (Actual)Interventional2008-06-30Completed
A Phase I, Randomized, Partially Blinded, Placebo- and Moxifloxacin-Controlled, 4-Period Crossover Study to Evaluate the Effect of GSK1322322 on Cardiac Conduction as Assessed by 12-lead Electrocardiogram in Healthy Volunteers (PDF112166) [NCT01803399]Phase 10 participants (Actual)Interventional2014-08-31Withdrawn(stopped due to Emerging GSK1322322 pre-clinical data ID'd potentially reactive metabolites previously not seen that changed the risk: benefit profile and led to a termination)
A Single Center, Open Label, Randomized, Single-dose, 2 Way Cross-over Study to Explore the Relative Bioavailability of Moksi 400mg (Moxifloxacin) Tablet and Avelox 400mg (Moxifloxacin) Tablet Under Fasting Conditions in Healthy Male Pakistani Subjects [NCT05307614]Phase 138 participants (Actual)Interventional2019-03-27Completed
Essentiality of Isoniazid in Tuberculosis Therapy [NCT01589497]Phase 269 participants (Actual)Interventional2015-06-30Completed
A PHASE 1, RANDOMIZED, PLACEBO- AND POSITIVE-CONTROLLED CROSS-OVER STUDY TO DETERMINE THE EFFECT OF SINGLE-DOSE CP-690,550 ON QTC INTERVAL IN HEALTHY VOLUNTEERS [NCT01743677]Phase 160 participants (Actual)Interventional2007-10-26Completed
A Randomized Controlled Non-Inferiority Study for Shortening Tuberculosis Treatment With Sitafloxacin-Containing Regimens [NCT05454345]Phase 3620 participants (Anticipated)Interventional2022-10-01Not yet recruiting
Intraperitoneal (IP) Vancomycin Plus Oral Moxifloxacin Versus IP Vancomycin Plus IP Ceftazidime for the Treatment of Peritoneal Dialysis-related Peritonitis: a Pilot Randomized Controlled Study [NCT02787057]80 participants (Actual)Interventional2012-11-30Completed
A Single-site, Single Masked, Prospective Comparison of Three Fluoroquinolone Topical Therapies (Besifloxacin 0.6% or Gatifloxacin 0.5% or Moxifloxacin 0.5%) in the Treatment of Infectious Corneal Ulcers. [NCT01928693]Phase 22 participants (Actual)Interventional2013-07-31Terminated(stopped due to study terminated due to slow accrual)
A Phase 3 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of the Combination of Moxifloxacin Plus PA-824 Plus Pyrazinamide After 4 and 6 Months of Treatment in Adult Subjects With Drug-Sensitive Smear-Positive Pulmo [NCT02342886]Phase 3284 participants (Actual)Interventional2015-02-28Completed
A Randomised, Partially Double Blind, Placebo and Positive Controlled, 4 Way Crossover Study to Evaluate the Effect of Icosabutate (NST 4016) on the QT/QTc Interval in Healthy Subjects [NCT03577275]Phase 132 participants (Actual)Interventional2018-06-15Completed
Effects of Evacetrapib (LY2484595) on the Pharmacokinetics of an Oral Contraceptive in Healthy Female Subjects [NCT01746732]Phase 123 participants (Actual)Interventional2012-12-31Completed
Rose Bengal Electromagnetic Activation With Green Light for Infection Reduction [NCT05110001]Phase 3330 participants (Anticipated)Interventional2022-08-03Recruiting
A Multiple-Dose, Randomized, Double-Blind, Placebo- and Active-Controlled, Four-Arm, Parallel Group Thorough QT/QTc Study to Evaluate the Electrophysiologic Effects of Sativex. [NCT01322139]Phase 1258 participants (Actual)Interventional2007-12-31Completed
A Single-Dose, Randomized, Double-Blind, Placebo- and Positive-Controlled, 4-Way Crossover Study to Evaluate the Effect of LOXO-292 on the QTc Interval in Healthy Adult Subjects [NCT05630274]Phase 132 participants (Actual)Interventional2019-04-16Completed
Risk of Acute Liver Injury in Users of Antimicrobials in the HealthCore Integrated Research Database Population [NCT01434173]1,299,056 participants (Actual)Observational2001-07-31Completed
A Randomized, Double-blind, Four-period Crossover Study to Investigate the Effect of Intravenous Ondansetron, a 5-HT3 Antagonist, on Cardiac Conduction as Compared to Placebo and Moxifloxacin in Healthy Adult Subjects [NCT01449188]Phase 160 participants (Actual)Interventional2011-08-16Completed
A Phase 1, Randomized, Double-blind, Placebo- and Active-controlled, Thorough QT/QTc Study of VX-548 in Healthy Subjects [NCT05818852]Phase 172 participants (Actual)Interventional2023-04-12Completed
A Randomized, Placebo- and Active-controlled 4-way Crossover Study in Healthy Subjects to Evaluate the Effect of E4 on the QTc Interval [NCT04819906]Phase 132 participants (Actual)Interventional2021-03-09Completed
A Phase 1, Single-Center, Pacritinib- Versus Placebo-Blinded, Active- and Placebo-Controlled, Randomized, 3-Way Crossover Study to Evaluate the Cardiac Safety and Pharmacokinetics Following a Single Oral Dose Administration of Pacritinib in Healthy Subjec [NCT02807207]Phase 142 participants (Actual)Interventional2014-10-31Completed
Pharmacodynamic Effects, Safety and Tolerability of 2 mg and 5 mg Cilobradine, Administered p.o. Once Daily Over 14 Days to Healthy Male and Female Volunteers in a Randomised, Placebo-controlled, Double Blind Study, With an Open-label Uncontrolled Intra-i [NCT02264015]Phase 1125 participants (Actual)Interventional2004-01-31Completed
Rifapentine-containing Treatment Shortening Regimens for Pulmonary Tuberculosis: A Randomized, Open-label, Controlled Phase 3 Clinical Trial. TBTC Study 31, ACTG Study A5349 [NCT02410772]Phase 32,516 participants (Actual)Interventional2016-01-25Completed
A Randomized, Double Blind, Placebo Controlled, Three- Period Crossover Study Comparing the Acute Effects of Orally Inhaled Dihydroergotamine (DHE), Oral Moxifloxacin, and Placebo on QT Intervals in Healthy Adults [NCT01191723]Phase 154 participants (Actual)Interventional2010-08-31Completed
The Effect of the Co-administration of BMS-790052 on the Pharmacokinetics of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norgestimate (Ortho Tri-Cyclen®) in Healthy Female Subjects [NCT00983957]Phase 147 participants (Actual)Interventional2009-10-31Completed
Randomized, Double-Blind, Double-Dummy, Placebo- and Positive Controlled, 4-Way Crossover Study to Assess the Effect of Single-Dose ACP-196 on the QTc Interval in Healthy Adult Subjects [NCT04867980]Phase 148 participants (Actual)Interventional2016-04-01Completed
Phase IV Study: A Prospective Two-Site Study to Evaluate the Safety and Tolerance of Besivance Versus Vigamox Prophylactically Pre and Post Operatively in Subjects Undergoing Routine Cataract Surgery [NCT01455233]Phase 460 participants (Actual)Interventional2010-09-30Completed
Evaluation of the Effect of Different Foods, Carbohydrate Meal, and a Euglycaemic Insulin Clamp on the QT/QTc Interval Using a Single Dose of Moxifloxacin as a Positive Control in Healthy Male and Female, Caucasian and Japanese Volunteers [NCT01642485]Phase 132 participants (Actual)Interventional2011-07-31Completed
Postoperative Safety Outcomes in Patients Undergoing Routine Phacoemulsification Cataract Surgery With Intraoperative Intracameral Injection of Preservative-Free Moxifloxacin Versus Levofloxacin [NCT04403334]Phase 4114 participants (Actual)Interventional2018-01-02Completed
A Randomized, Double-blind, Placebo- and Positive-controlled, Single-dose, 4 Way Crossover Study to Evaluate the Effects of Loperamide (JNJ-289679) on Electrocardiogram Intervals in Healthy Adult Subjects [NCT04225078]Phase 166 participants (Actual)Interventional2020-01-17Completed
A Phase II, Randomized, Double-Blind, Multicenter, Comparative Study to Determine the Safety, Tolerability, Pharmacokinetics and Efficacy of Oral Nafithromycin Versus Oral Moxifloxacin in the Treatment of Community-Acquired Bacterial Pneumonia (CABP) in A [NCT02903836]Phase 2231 participants (Actual)Interventional2016-11-18Completed
A Phase 1, Open Label Study To Evaluate The Pharmacokinetics, Pharmacodynamics, And Effect On QT/QTc Interval For CP-751,871 Following Single Intravenous Administration To Healthy Adult Subjects [NCT00926263]Phase 128 participants (Actual)Interventional2009-07-31Terminated(stopped due to See termination reason in detailed description.)
A Randomised, Placebo Controlled, Four-way Cross-over Study to Assess Cardiac Re-polarisation Following Repeat Dosing With GSK2190915 and Placebo for Five Days, With Moxifloxacin as a Positive Control, in Healthy Male and Female Subjects. [NCT01721135]Phase 10 participants (Actual)Interventional2010-09-30Withdrawn(stopped due to Study was terminated due to toxicology findings after screening started but before first subject first dose.)
A Phase 1, Randomized, Double-blind, Placebo- and Positive-controlled, Thorough QT/QTc Study of Vanzacaftor Monotherapy in Healthy Subjects [NCT05867147]Phase 156 participants (Actual)Interventional2023-04-26Completed
A Two Different Chemoprophylaxis Approaches After Phacoemulsification Surgery in One Thousand Patients in Iraq :a Clinical Trial [NCT03634852]Phase 41,000 participants (Actual)Interventional2016-10-01Completed
A Study to Evaluate the Effects on QT/QTc Interval of TS-142 in Healthy Adult Subjects [NCT04873323]Phase 159 participants (Actual)Interventional2021-06-07Completed
Determining the Effect of Antibiotic Drop Prophylaxis on the Conjunctival Flora [NCT01577342]56 participants (Actual)Interventional2010-11-30Completed
A Randomized, Partially Blinded, 4-period, Crossover Study to Assess the Effects of Single-dose AEB071 Administration (300 and 900 mg) on Electrocardiographic QT Intervals Compared to Placebo in Healthy Volunteers [NCT01594255]Phase 1100 participants (Actual)Interventional2009-07-31Completed
A Multiple-center, Multiple-dose, Randomized, Double-blind, Double-dummy, Placebo-controlled, Positive-controlled, Parallel Group Study to Investigate the Effect of RO4917838 on the QTc Interval in Healthy Subjects. [NCT01613040]Phase 1169 participants (Actual)Interventional2009-01-31Completed
Prospective, Single-center, Randomized, Double-blind, Placebo-controlled, Two-part Phase 1 Study to Assess the Effect of Single Therapeutic and Supra-therapeutic Doses of Lucerastat on the QT/QTc Interval Duration in Healthy Subjects [NCT03832452]Phase 144 participants (Actual)Interventional2019-02-14Completed
Oral Moxifloxacin Versus Cefazolin and Oral Probenecid in the Management of Skin and Soft Tissue Infections in the Emergency Department [NCT00323219]Phase 3390 participants (Anticipated)Interventional2004-01-31Recruiting
A Phase 1, Randomized, Multiple Dose, Double Blind, 5-way Crossover Study of the Electrocardiographic Effects of Bilastine in Healthy Adult Subjects [NCT00419783]Phase 130 participants (Actual)Interventional2006-08-31Completed
Comparison of Dropless Prophylaxis After Routine Phacoemulsification to Standard Drops Regimen [NCT02515045]Phase 459 participants (Actual)Interventional2015-01-31Completed
A Phase 2 Open-Label Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of Combinations of Bedaquiline, Moxifloxacin, PA-824 and Pyrazinamide During 8 Weeks of Treatment in Adult Subjects With Newly Diagnosed Drug-Sensitive or Mu [NCT02193776]Phase 2240 participants (Actual)Interventional2014-10-23Completed
A Multi-Center, Randomized, Double-Blind, Parallel Comparative, Phase II Study to Evaluate the Efficacy and Safety of Intravenous Infusion With Nemonoxacin Versus Moxifloxacin in Treating Adult Patients With Community-Acquired Pneumonia (CAP) [NCT01944774]Phase 2207 participants (Actual)Interventional2013-03-31Completed
A Randomized, Double-blinded, Double-dummy, Placebo-controlled Thorough QTC Study With Single Oral Doses of Cedazuridine in Healthy Subjects [NCT04953923]Phase 136 participants (Actual)Interventional2021-07-01Completed
A Multiple Arm, Multiple Stage (MAMS), Phase 2B/C, Open Label, Randomized, Controlled Platform Trial to Evaluate Experimental Arms Including an Increased Dose of Rifampicin, an Optimized Dose of Pyrazinamide, Moxifloxacin and Sutezolid, in Adult Subjects [NCT05807399]Phase 2360 participants (Anticipated)Interventional2023-04-14Recruiting
The Physiological Effects of hERG Blockade on Metabolism [NCT03868657]44 participants (Actual)Interventional2019-01-28Completed
Intracameral Antibiotic Safety Study [NCT02590523]Phase 3500 participants (Anticipated)Interventional2023-01-31Suspended(stopped due to Lack of antibiotic availability)
A Multiple-dose, Randomized, Double-blind, Placebo-controlled, Active-Comparator, Parallel Study to Investigate the Effect of Avacopan at Therapeutic and Supratherapeutic Doses on the QT/QTc Interval in Healthy Subjects [NCT05988034]Phase 158 participants (Actual)Interventional2019-11-08Completed
A Phase 1, Two-Part Study in Healthy Volunteers to Evaluate The Effect of Psilocybin on Cardiac Repolarization and The Effect of Food on Psilocybin Pharmacokinetics [NCT05478278]Phase 160 participants (Actual)Interventional2022-06-22Completed
A Through QT/QTc Study of KW-6356 in Japanese Healthy Adults [NCT04342273]Phase 1128 participants (Actual)Interventional2020-03-31Completed
A Randomised, Double-blind, Four-period Crossover Study to Investigate the Effect of Intravenous APD421 on Cardiac Conduction as Compared to Placebo and Moxifloxacin in Healthy Adult Subjects [NCT02661594]Phase 140 participants (Actual)Interventional2013-11-30Completed
Evaluation of Antibiogram Results and Clinical Response to Prescribed Antimicrobials in Microbial Keratitis Patients [NCT05655689]123 participants (Actual)Observational2021-12-31Completed
A Single-center, Randomized, Double-blind, Placebo-controlled, Three-way Crossover Phase I Study to Investigate the Effect on the QTc Interval of a Single Dose of AZD6094 (600 mg) Compared With Placebo, Using Open-label Moxifloxacin (Avelox®) as a Positiv [NCT03258515]Phase 145 participants (Actual)Interventional2017-09-06Completed
Acute Appendicitis and Microbiota - Ethology of Appendicitis and Effects of the Antimicrobial Treatment - The MAPPAC (Microbiology Appendicitis Acuta) Trial [NCT03257423]200 participants (Anticipated)Interventional2017-04-04Enrolling by invitation
A Randomized, Partial Double-Blind, Placebo- and Positive- Controlled, Multiple-Dose, 4-Way Crossover, Thorough QT/QTc (TQT) Study to Investigate the Effect of Relacorilant on Cardiac Repolarization in Healthy Volunteers [NCT04795479]Phase 136 participants (Actual)Interventional2021-01-22Completed
A Phase 1, Randomized, Double-Blind, Placebo- and Positive-Controlled, 4-Period Crossover Thorough QT Study to Evaluate the Effect of a Single Dose of TD-4208 on Cardiac Repolarization in Healthy Subjects [NCT02820311]Phase 148 participants (Actual)Interventional2016-05-31Completed
A Multicenter, Randomized, Open-Label Study To Evaluate The Efficacy And Safety Of A Contezolid, Delamanid and Bedaquiline-Containing Short Regimen For The Treatment Of Rifampicin-Resistant Pulmonary Tuberculosis [NCT06081361]Phase 3186 participants (Anticipated)Interventional2023-11-01Not yet recruiting
A Randomized, Triple-blind, Placebo- and Positive-Controlled, Parallel Group Study of the Effect of Buprenorphine Delivered by the Buprenorphine Transdermal System (BTDS) at Doses up to 80 mcg/Hour and Naltrexone on ECG Intervals in Healthy Adult Subjects [NCT01999114]Phase 1328 participants (Actual)Interventional2012-03-31Completed
Multi-centric Prospective Cohort Study of TB Recurrence Free Cure Among Microbiologically Confirmed New Pulmonary Tuberculosis Patients Treated Under NTEP With the 4-month Moxifloxacin Containing Daily Regimen [NCT05047055]550 participants (Anticipated)Observational2021-10-01Not yet recruiting
A Double-blind, Single-center, Randomized, Placebo- and Positive-controlled, Parallel-group Trial With a Nested Crossover Part on the Electrocardiographic Effects 100 and 400 mg Pritelivir Per Day in Healthy Subjects: a Thorough QT/QTc Trial [NCT05671029]Phase 164 participants (Actual)Interventional2022-12-04Completed
A Randomized, 3-Treatment, 3-Period, 6-Sequence, Crossover, Placebo- and Active-Controlled, Double-Blind for ALXN1840 (Open-Label for Moxifloxacin) Thorough QT/QTc Study to Evaluate ALXN1840 on Cardiac Repolarization in Healthy Adults [NCT04560816]Phase 157 participants (Actual)Interventional2020-07-24Completed
Clinical ECG Study to Evaluate Electrophysiological Effects of Potential QT Prolonging Drugs With Novel ECG Biomarkers With Exposure-Response Analysis [NCT05716854]Phase 144 participants (Actual)Interventional2023-03-21Completed
A Double-Blind Study in Healthy Volunteers to Assess the Effect of E7080 on the QTc Interval [NCT01525394]Phase 152 participants (Actual)Interventional2010-12-31Completed
A Single-dose, Open-label, Fixed Sequence, Two Period Cross Over Study to Assess the Tolerability of a Supra Therapeutic Dose of TRV130 Followed by A Single Dose, Randomized, Double Blind, Comparative, Positive and Placebo Controlled, Four Period Cross-ov [NCT02344303]Phase 163 participants (Actual)Interventional2014-12-31Completed
An Evaluation of the Safety and Efficacy of Moxifloxacin Ophthalmic Solution 0.5% Versus Ofloxacin Ophthalmic Solution 0.3% in the Treatment of Bacterial Conjunctivitis in Chinese Patients [NCT01573910]Phase 3985 participants (Actual)Interventional2012-05-31Completed
A Phase 1, Randomized, Double-blind, Placebo- and Positive-controlled, 4-Period Crossover Trial to Assess the Effect of Anagrelide Hydrochloride on QT/QTc Interval in Healthy Men and Women. [NCT01552928]Phase 160 participants (Actual)Interventional2012-03-29Completed
A Single-Center, Open-Label, Randomized Study of the Pharmacokinetics of AzaSite Ophthalmic Solution Versus Vigamox in the Conjunctiva of Healthy Volunteers Following a Single Ocular Administration [NCT00564447]Phase 448 participants (Actual)Interventional2007-12-31Completed
A Single-Center, Open-Label, Randomized Study of the Pharmacokinetics of AzaSite Ophthalmic Solution Versus Vigamox in the Tears of Healthy Volunteers Following a Single Ocular Administration [NCT00575367]Phase 437 participants (Actual)Interventional2008-03-31Completed
Assessment of Electrophysiological Effects of Tipranavir Co-administered With Ritonavir Given b.i.d. for 2.5 Days on the QT Interval in Healthy Female and Male Subjects. A Double-blind, Randomised, Placebo Controlled, Two-way Crossover Study With a Positi [NCT02248883]Phase 181 participants (Actual)Interventional2005-12-31Completed
Thorough QT/QTc Study of 2 Doses of ADASUVE® in Healthy Volunteers [NCT01854710]Phase 460 participants (Actual)Interventional2013-05-31Completed
The D3 Study: Drug Delivery vs Drops - A Prospective Clinical Study Evaluating Dexycu vs Prednisolone Acetate 1% in Controlling Post-operative Pain and Inflammation in Patients Undergoing Sequential Cataract Surgery [NCT04273282]Phase 431 participants (Actual)Interventional2019-12-16Completed
A Randomized, Open-label, Negative and Positive Control, Crossover Clinical Study to Evaluate Effect on QT/QTc Interval After Multiple Dose of Celecoxib in Healthy Adult Volunteers [NCT03822520]Phase 128 participants (Actual)Interventional2017-06-30Completed
A Placebo- and Positive-Controlled Study of the Effect of LY2484595 on QT Interval in Healthy Subjects [NCT01537887]Phase 172 participants (Actual)Interventional2012-02-29Completed
A Randomized, Placebo-Controlled Study to Evaluate the Effect of Tafenoquine (SB252263) on the Electrocardiogram (ECG) With Focus on Cardiac Repolarization (QTc Duration) in Healthy Subjects [NCT01928914]Phase 1260 participants (Actual)Interventional2011-07-26Completed
Oral Contraceptives in the Metabolic Syndrome [NCT00205504]Phase 446 participants (Actual)Interventional2005-06-30Completed
Comparative Study of the Effect on Acne With Norgestimate Containing Triphasic Oral Contraceptive and Biphasic Preparation Containing Desogestrel [NCT01466673]Phase 4201 participants (Actual)Interventional2008-12-31Completed
A Randomized, Double-Blind, Placebo- and Active-Controlled Study to Evaluate the Effect of Ha44 Gel on the ECG in Healthy Adult Subjects [NCT01518699]Phase 157 participants (Actual)Interventional2012-01-31Completed
A Double-Blind, Randomized, Crossover, Thorough QT/QTc Trial to Evaluate the Potential of Deferiprone to Prolong the QT Interval in Healthy Subjects [NCT01860703]Phase 450 participants (Actual)Interventional2012-11-30Completed
[NCT01799356]Phase 41,303 participants (Actual)Interventional2010-06-30Completed
Phase II, National, Multicenter, Randomized, Double Blind Clinical Trial, to Evaluate the Efficacy and Safety of Saturno IIB Association on the Control of Ocular Inflammation Post-phacoemulsification [NCT03580473]Phase 2118 participants (Actual)Interventional2020-02-27Completed
Thorough QT Study to Evaluate the Effects of BI 207127 (Deleobuvir) Combined With Faldaprevir on Cardiac Safety Parameters in Healthy Female and Male Subjects. Randomised, Placebo Controlled, Single-blind, Three-period Crossover Phase-I-study With Moxiflo [NCT01965431]Phase 148 participants (Actual)Interventional2013-10-31Completed
A Phase 3b Randomized, Double-blind, Multi-center Study to Compare the Safety and Efficacy of Omadacycline IV/PO to Moxifloxacin IV/PO for Treating Adult Subjects With Community-acquired Bacterial Pneumonia (CABP) [NCT06162286]Phase 3100 participants (Anticipated)Interventional2023-11-17Recruiting
Impact of Rifampicin in Treatment Outcome of Cutibacterium Acnes Prosthetic Joint Infections [NCT05902221]Phase 3235 participants (Anticipated)Interventional2023-07-01Not yet recruiting
Oral Contraceptives, Insulin Resistance and Cardiovascular Risk Profile in Pre-Menopausal Women [NCT01475513]Phase 447 participants (Actual)Interventional2011-11-30Completed
Pharmacokinetic Evaluation of Moxifloxacin in Vigadexa® in Aqueous Humor Samples Following Preoperative Antibiotic/Steroid Dosing in Cataract Surgery Patients [NCT01859702]Phase 436 participants (Actual)Interventional2012-04-30Completed
A Multiple-Ascending-Dose, Randomized, Double-Blind, Double-Dummy, Placebo- and Positive-Controlled Study to Evaluate the Effect of ALXN2050 on the QT Interval in Healthy Adult Participants [NCT04660890]Phase 139 participants (Actual)Interventional2020-12-12Completed
A Randomized, Double-blind, Placebo-controlled and Open-label, Active Controlled, 4 Period Crossover Trial to Evaluate the Effect of BIA 5 1058 on Cardiac Repolarization in Healthy Adult Males and Females Under Fed Conditions [NCT03489005]Phase 149 participants (Actual)Interventional2018-04-09Completed
Effect of Dulaglutide (LY2189265) on Oral Contraceptive Pharmacokinetics in Healthy Female Subjects [NCT01458210]Phase 122 participants (Actual)Interventional2011-10-31Completed
A Randomized, Double-blind, Double-dummy, Placebo- and Positive-controlled Study to Evaluate the Cardiac Safety of a Single Dose of AL-335 Administered on a Background of Simeprevir and Odalasvir and of Repeated Doses of Odalasvir Administered Alone in He [NCT03155893]Phase 159 participants (Actual)Interventional2017-05-12Completed
A Phase 3 Randomized, Double-Blind, Multi-Center Study to Compare the Safety and Efficacy of Omadacycline Intravenous (IV)/Oral (PO) to Moxifloxacin IV/PO for Treating Adults Subjects With Community-Acquired Bacterial Pneumonia [NCT02531438]Phase 3774 participants (Actual)Interventional2015-11-30Completed
An Open Label, Balanced, Randomized, Two-treatment, Two-period, Two-sequence, Single Dose, Crossover, Oral Bioequivalence Study of Moxifloxacin Tablets, 400 mg of Dr. Reddy's Laboratories Limited, Comparing With Avelox® Tablets 400 mg of Bayer Healthcare [NCT02322619]Phase 126 participants (Actual)Interventional2012-11-30Completed
A Single Center, Open Label, Randomized, Single-dose, Two-period, Two-way Cross-over Study to Compare the Rate and Extent of Absorption of Mofest® 400mg (Moxifloxacin) Tablet With Avelox® 400mg (Moxifloxacin) Tablet in Healthy Pakistani Subjects. [NCT04873570]Phase 138 participants (Actual)Interventional2021-05-28Completed
A Phase 1, Double-Blinded, Placebo- and Active-Controlled, Randomized Study to Investigate the Potential of Soticlestat to Prolong the QTc Interval in Healthy Adult Participants [NCT05309902]Phase 10 participants (Actual)Interventional2022-10-11Withdrawn(stopped due to Study not needed)
Oral Antimicrobial Treatment vs. Outpatient Parenteral for Infective Endocarditis [NCT05398679]Phase 4360 participants (Anticipated)Interventional2022-06-01Not yet recruiting
A PHASE 1, RANDOMIZED, PLACEBO-AND POSITIVE-CONTROLLED CROSSOVER STUDY TO DETERMINE THE EFFECT OF SINGLE-DOSE PF-04965842 ON QTC INTERVAL IN HEALTHY VOLUNTEERS [NCT03386279]Phase 136 participants (Actual)Interventional2018-07-02Completed
Evaluation and Comparison of Macular and Choroidal Thickness After Intracameral Moxifloxacin for Prevention of Postcataract Endophthalmitis [NCT03363295]Phase 4120 participants (Actual)Interventional2017-07-01Completed
An Open-Label, Partially Randomized Trial to Evaluate the Efficacy, Safety and Tolerability of a 4-month Treatment of Bedaquiline Plus Pretomanid Plus Moxifloxacin Plus Pyrazinamide (BPaMZ) Compared to a 6-month Treatment of HRZE/HR (Control) in Adult Par [NCT03338621]Phase 2/Phase 3455 participants (Actual)Interventional2018-07-30Completed
A Placebo- and Positive-Controlled Study of the Electrophysiological Effects of a Supratherapeutic Dose of LY2409021 in Healthy Subjects [NCT01460368]Phase 167 participants (Actual)Interventional2011-10-31Completed
Antibiotic Resistance In Eye Surgeries (ARIES) [NCT04750655]Phase 4108 participants (Anticipated)Interventional2021-03-01Recruiting
An Open Label Randomized Controlled Clinical Trial Comparing a 24Week Oral Regimen Containing Moxifloxacin With a 24 Week Standard Drug Regimen for the Treatment of Smear-positive Pulmonary Tuberculosis in Patients Previously Treated for TB [NCT02114684]Phase 1/Phase 2197 participants (Actual)Interventional2013-11-30Completed
A Partial-Blind, Randomized, Parallel Design Study With a Nested Crossover Comparison to Define the ECG Effects of Tizanidine Compared to Placebo and the Positive Control, Moxifloxacin, in Healthy Men and Women Using a Blinded ECG Evaluator: A Thorough EC [NCT01839279]Phase 2136 participants (Actual)Interventional2013-04-30Completed
Evaluating a New Treatment Regimen for Patients With Multidrug-resistant TB (MDR-TB) - a Prospective Open-label Randomised Controlled Trial [NCT02454205]Phase 2/Phase 3154 participants (Actual)Interventional2015-11-12Completed
The Effect of the Co-administration of Atazanavir (ATV) and Ritonavir (RTV) on the Pharmacokinetics of a Combined Oral Contraceptive Containing Ethinyl Estradiol and Norgestimate in Healthy Female Subjects [NCT00357604]Phase 122 participants Interventional2006-07-31Completed
Interventional, Randomised, Double-blind, Placebo- and Positive Controlled, Single-dose, Cross-over Study Investigating the Effect of Idalopirdine on Cardiac Repolarisation in Healthy Men [NCT02436486]Phase 176 participants (Actual)Interventional2015-05-31Completed
A PHASE 1, SINGLE CENTER, RANDOMIZED, 4-WAY CROSSOVER, DOUBLE BLINDED, PLACEBO AND MOXIFLOXACIN CONTROLLED STUDY TO EVALUATE THE EFFECT OF GLASDEGIB ON THE CARDIAC REPOLARIZATION IN HEALTHY SUBJECTS [NCT03162900]Phase 136 participants (Actual)Interventional2017-06-09Completed
Five Period Crossover Study of the Ability of Late Sodium or Calcium Current Block (Mexiletine, Lidocaine, or Diltiazem) to Balance the Electrocardiographic Effects of hERG Potassium Current Block (Dofetilide or Moxifloxacin) [NCT02308748]Phase 122 participants (Actual)Interventional2014-05-31Completed
A Randomized, Double-blind, Placebo-controlled and Open Label Active-controlled, 4-period Crossover Trial to Evaluate the Effect of Eslicarbazepine Acetate on Cardiac Repolarization in Healthy Adult Men and Women [NCT02283788]Phase 167 participants (Actual)Interventional2007-03-31Completed
Efficacy of Oral Antibiotic Therapy Compared to Intravenous Antibiotic Therapy for the Treatment of Diabetic Foot Osteomyelitis (CRO-OSTEOMYELITIS) [NCT02168816]Phase 230 participants (Actual)Interventional2014-03-19Terminated(stopped due to The study was stopped for feasibility (i.e., low recruitment))
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Trial Outcomes

TrialOutcome
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Concentration of ARVs and TB Drugs
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 24 Hours (AUC24) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 12 Hours (AUC12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Area Under the Curve From 0 to 12 Hours (AUC12) of ARVs for Contraceptive Arms
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]Number of Women Who Met PK Target of Area Under the Curve (AUC) for ARVs
NCT00042289 (26) [back to overview]Pharmacokinetic (PK) Parameter: Infant Plasma Washout Half-life (T1/2) of ARVs and TB Drugs
NCT00042289 (26) [back to overview]Plasma Concentration for Contraceptives
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in ng/mL With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Cord/Maternal Blood Concentration Ratio With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Geometric Mean (95% CI) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C12) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Maximum Concentration (Cmax) in mg/L With Median (IQR) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Trough Concentration (C24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (Range) for ARVs and TB Drugs
NCT00042289 (26) [back to overview]PK Parameter: Area Under the Curve From 0 to 24 Hours (AUC24) With Median (IQR) for ARVs and TB Drugs
NCT00082173 (2) [back to overview]Proportion of Patients With Sterile Sputum Cultures
NCT00082173 (2) [back to overview]Proportion of Patients With Grade 3 or 4 Adverse Reactions Attributable to Study Medications
NCT00205504 (10) [back to overview]Changes in Waist-to-Hip Ratio Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Inflammatory Marker Changes, High Sensitive C-reactive Protein (Hs-CRP) and Adiponectin, Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Inflammatory Marker Changes (MCP-1) Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Changes in Waist Circumference Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Changes in Lipid Profile Compared Associated With OC Use Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Changes in Insulin Sensitivity Associated With Oral Contraceptive (OC) Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Changes in Estrogen Metabolites (Plasma) Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Changes in Blood Pressure Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Changes in Body Mass Index (BMI) Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00205504 (10) [back to overview]Inflammatory Marker Changes, Soluble Vascular Cell Adhesion Molecule (sVCAM) and Soluble Intercellular Adhesion Molecule (sICAM), Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women
NCT00254566 (9) [back to overview]Percentage of Bacteriologic Response at Test of Cure Visit
NCT00254566 (9) [back to overview]Percentage of Clinical Cure (Success) at Test of Cure Visit (Full Analysis Set)
NCT00254566 (9) [back to overview]Percentage of Clinical Cure (Success) at Test of Cure Visit(Clinical Per Protocol Population)
NCT00254566 (9) [back to overview]Percentage of Clinical Cure (Success)at Test of Cure Visit(Clinically Eligible Set)
NCT00254566 (9) [back to overview]Change From Baseline in Clinical COPD Questionnaire(CCQ)Functional State Score
NCT00254566 (9) [back to overview]Change From Baseline in Clinical COPD Questionnaire(CCQ)Symptoms Score
NCT00254566 (9) [back to overview]Change From Baseline in Clinical COPD Questionnaire(CCQ)Total Score
NCT00254566 (9) [back to overview]Time Taken for First Quartile (25%) of Subjects to Have AECB Recurrence
NCT00254566 (9) [back to overview]Change From Baseline in Clinical COPD Questionnaire(CCQ)Mental State Score
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 17 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 16 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 15 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 14 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 13 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 11 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 10 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 1 Hour After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 18 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 7 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 6 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 5 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 4 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 3 Hours After Patch Application on Day 42(Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 12 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 24 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 23 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 22 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 21 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 20 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 2 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI at Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 9 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 8 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 7 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 6 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 5 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 4 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 3 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 2 Hours Before Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 2 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 10 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 19 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 1 Hour Before Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 1 Hour After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI at Time of Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 9 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00292227 (38) [back to overview]Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 8 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)
NCT00312338 (3) [back to overview]Susceptability Changes in Haemophilus Influenzae Distal to the Site of Instillation
NCT00312338 (3) [back to overview]Susceptability Changes in Staphylococcus Aureus Distal to the Site of Instillation
NCT00312338 (3) [back to overview]Susceptability Changes in Streptococcus Pneumoniae Distal to the Site of Instillation
NCT00348348 (4) [back to overview]Clinical Resolution
NCT00348348 (4) [back to overview]Clinical Resolution
NCT00348348 (4) [back to overview]Microbial Eradication
NCT00348348 (4) [back to overview]Microbial Eradication
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC) Adjusted for Free Drug Concentrations
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC)
NCT00396084 (19) [back to overview]Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)
NCT00396084 (19) [back to overview]Time to Maximum Plasma Drug Concentration (Tmax) and Half-life
NCT00396084 (19) [back to overview]Time to Maximum Plasma Drug Concentration (Tmax) and Half-life
NCT00396084 (19) [back to overview]Pharmacokinetic Parameters: Area Under the Curve (AUC) During First 12 and 24 Hours
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration (Cmax)
NCT00396084 (19) [back to overview]Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Fluoroquinolones/Isoniazid (INH) Comparison
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentration (Cmax)
NCT00396084 (19) [back to overview]Difference in Sputum Bacillary Loads: Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Linezolid Once Daily/Linezolid Twice Daily/INH Comparison
NCT00396084 (19) [back to overview]Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Linezolid Once Daily/Linezolid Twice Daily/Isoniazid (INH) Comparison
NCT00396084 (19) [back to overview]Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Fluoroquinolones/Isoniazid (INH) Comparison
NCT00396084 (19) [back to overview]Area Under the Curve During First 12 or 24 Hours / Minimum Inhibitory Concentration (AUC/MIC)
NCT00396084 (19) [back to overview]Area Under the Curve (AUC) Adjusted for Free Drug Concentrations/Minimum Inhibitory Concentration (MIC)
NCT00396084 (19) [back to overview]Area Under the Curve (AUC) During First 12 and 24 Hours Adjusted for Free Drug Concentrations
NCT00396084 (19) [back to overview]Pharmacokinetic Parameters: Area Under the Curve During First 12 and 24 Hours
NCT00396084 (19) [back to overview]Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)
NCT00396084 (19) [back to overview]Percent Dosing Interval Above Minimum Inhibitory Concentration (MIC)
NCT00396084 (19) [back to overview]Maximum Plasma Drug Concentrations (Cmax), Adjusted for Free Drug Concentration
NCT00398411 (6) [back to overview]Incidence of Clinically Significant Bacteremia
NCT00398411 (6) [back to overview]Overall Survival
NCT00398411 (6) [back to overview]Time to Occurrence of Fever >= 38°C
NCT00398411 (6) [back to overview]Reason for Discontinuation of Treatment
NCT00398411 (6) [back to overview]Type of Infection
NCT00398411 (6) [back to overview]Type of Isolates and Infections
NCT00402727 (12) [back to overview]Percentage of Participants With Bacteriological Success (BS) at 3 to 5 Days After Start of Treatment in the Microbiological Valid (MBV) Population
NCT00402727 (12) [back to overview]Percentage of Cured Participants as Determined by the Data Review Committee (DRC) at Test of Cure Visit in the Intent to Treat (ITT) Population
NCT00402727 (12) [back to overview]Percentage of Cured Participants as Determined by the Data Review Committee (DRC) at Test of Cure Visit in the Per Protocol (PP) Population
NCT00402727 (12) [back to overview]Percentage of Participants Assessed as Improvements by the Data Review Committee (DRC) at the During Treatment Day 3-5 in the Per Protocol (PP) Population
NCT00402727 (12) [back to overview]Percentage of Participants Assessed as Resolution by the Data Review Committee (DRC) at End of Therapy in the Intent to Treat (ITT) Population
NCT00402727 (12) [back to overview]Percentage of Participants Assessed as Resolution by the Data Review Committee (DRC) at End of Therapy in the Per Protocol (PP) Population
NCT00402727 (12) [back to overview]Percentage of Participants With Bacteriological Success (BS) at 3 to 5 Days After Start of Treatment in the ITT Population With Causative Organisms
NCT00402727 (12) [back to overview]Percentage of Participants With Bacteriological Success (BS) After 14 - 28 Days After Last Dose of Study Medication in the ITT Population With Causative Organisms
NCT00402727 (12) [back to overview]Percentage of Participants With Bacteriological Success (BS) After 14 - 28 Days After Last Dose of Study Medication in the Microbiological Valid (MBV) Population
NCT00402727 (12) [back to overview]Percentage of Participants With Bacteriological Success (BS) After 7 - 21 Days of Treatment in the ITT Population With Causative Organisms
NCT00402727 (12) [back to overview]Percentage of Participants With Bacteriological Success (BS) After 7 - 21 Days of Treatment in the Microbiological Valid (MBV) Population
NCT00402727 (12) [back to overview]Percentage of Participants Assessed as Improvements by the Data Review Committee (DRC) at the During Treatment Day 3-5 in the Intent to Treat (ITT) Population
NCT00414011 (1) [back to overview]Corneal Epithelial Healing Time
NCT00453349 (11) [back to overview]Number of Subjects Who Received Alternative Medicine
NCT00453349 (11) [back to overview]Bacteriological Response at Test Of Cure (TOC) Visit in Intent To Treat Population With Causative Organism
NCT00453349 (11) [back to overview]Bacteriological Response at Test Of Cure (TOC) Visit Microbiologically Valid
NCT00453349 (11) [back to overview]Clinical Response 7 to 14 Days After Completion of Study Drug Therapy in Per Protocol (PP) Population
NCT00453349 (11) [back to overview]Clinical Response 7 to 14 Days After Completion of Study Drug Therapy on Intent To Treat (ITT) Population
NCT00453349 (11) [back to overview]Clinical Response at Follow-up Visit on Per Protocol Population
NCT00453349 (11) [back to overview]Clinical Response on Treatment for Intent To Treat Population
NCT00453349 (11) [back to overview]Clinical Response at Follow-up Visit on Intent To Treat Population
NCT00453349 (11) [back to overview]Clinical Response on Treatment for Per Protocol Population
NCT00453349 (11) [back to overview]Bacteriological Response at Follow-up Visit in Intent To Treat Population With Causative Organism
NCT00453349 (11) [back to overview]Bacteriological Response at Follow-up Visit Microbiologically Valid
NCT00464438 (4) [back to overview]Percentage of Patients With Microbiological Improvement
NCT00464438 (4) [back to overview]Percentage of Patients With Clearing (Clinical Success) of Conjunctival Erythema and Conjunctival Discharge at Day 7
NCT00464438 (4) [back to overview]Percentage of Patients With Improvement in Ocular Signs for Conjunctival Discharge at Day 7
NCT00464438 (4) [back to overview]Percentage of Patients With Improvement in Ocular Signs for Lid Erythema
NCT00492024 (6) [back to overview]Treatment Day When Patients Returned to Normal Activities as Measured by Patient Reported Data, Using LOCF Approach
NCT00492024 (6) [back to overview]Percentage of Subjects With Clinical Cure (Modified Intent-to-Treat (MITT))
NCT00492024 (6) [back to overview]Percentage of Subjects With Clinical Cure (Per Protocol Population (PP))
NCT00492024 (6) [back to overview]Percentage of Subjects With Clinical Improvement During Therapy
NCT00492024 (6) [back to overview]Percentage of Subjects With Continued Clinical Cure During Long-Term Follow-Up
NCT00492024 (6) [back to overview]Treatment Day When Patients Reached Symptom Improvement as Measured by Patient Reported Data, Using Last Observation Carried Forward (LOCF) Approach
NCT00492726 (10) [back to overview]Number of Subjects Achieving Bacteriological Success at EOT Visit in the Per Protocol Population With Causative Organism(s)
NCT00492726 (10) [back to overview]Number of Subjects Achieving Clinical Cure at TOC Visit in the Per Protocol Population With Causative Organism(s)
NCT00492726 (10) [back to overview]Number of Subjects Achieving Clinical Improvement During Treatment in the Per Protocol Population
NCT00492726 (10) [back to overview]Duration of Hospitalization
NCT00492726 (10) [back to overview]Duration of Hospitalization Postoperatively
NCT00492726 (10) [back to overview]Number of Subjects Who Died Due to Intra-abdominal Infections
NCT00492726 (10) [back to overview]Number of Subjects Achieving Bacteriological Success at TOC Visit in the Per Protocol Population With Causative Organism(s)
NCT00492726 (10) [back to overview]Number of Subjects Achieving Clinical Cure at End of Therapy (EOT) Visit in the Per Protocol Population
NCT00492726 (10) [back to overview]Number of Subjects Achieving Clinical Cure at Test of Cure (TOC) Visit in the Per Protocol Population
NCT00492726 (10) [back to overview]Number of Subjects Achieving Bacteriological Success During Treatment in the Per Protocol Population With Causative Organism(s)
NCT00493038 (5) [back to overview]Number of Participants With Response (Intent-to-treat Population)
NCT00493038 (5) [back to overview]Number of Participants With Response (Per-protocol Population)
NCT00493038 (5) [back to overview]Number of Participants With Response (Per-protocol Population)
NCT00493038 (5) [back to overview]Number of Participants With Response (Microbiologically Valid Patients)
NCT00493038 (5) [back to overview]Number of Participants With Response (Microbiologically Valid Patients)
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 30 ms
NCT00543062 (7) [back to overview]Maximum Effect of Inhaled Prochlorperazine on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo
NCT00543062 (7) [back to overview]QTcI Versus Prochlorperazine Concentration
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 60 ms
NCT00543062 (7) [back to overview]Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI > 450 ms
NCT00543062 (7) [back to overview]Numbers and % of Subjects With QTcI > 480 ms
NCT00564447 (1) [back to overview]Assessment of Pharmacokinetic Parameters
NCT00575367 (1) [back to overview]Concentration of AzaSite and Vigamox in the Tear Fluid Across Six Time Points Ranging From 15 Minutes to 24 Hours Following Administration.
NCT00575380 (2) [back to overview]Conjunctiva Concentration Prior to Cataract Surgery at One of Ten Time Points Ranging From 1 to 14 Days (Per Protocol Pharmacokinetic Population)
NCT00575380 (2) [back to overview]Aqueous Humor Concentration Prior to Cataract Surgery at One of Ten Time Points Ranging From 1 to 14 Days (Per Protocol Pharmacokinetic Population)
NCT00581542 (2) [back to overview]Number of Participants With a Negative Bacterial Culture
NCT00581542 (2) [back to overview]Number of Participants With Normal Physical Examination of the Eye
NCT00635570 (4) [back to overview]Satisfaction Rate
NCT00635570 (4) [back to overview]Continuation Rate
NCT00635570 (4) [back to overview]Adherence Rate (Rate of Perfect Method Use)
NCT00635570 (4) [back to overview]Continuation Rate
NCT00672984 (14) [back to overview]Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 6
NCT00672984 (14) [back to overview]Change From Baseline in Electrocardiogram Results (QTcNi) at Time of Maximum Plasma Concentration (Tmax) on Day 1
NCT00672984 (14) [back to overview]Change From Baseline in Electrocardiogram Results (QTcNi) at Tmax on Day 6
NCT00672984 (14) [back to overview]Change From Baseline in Heart Rate (HR) at Tmax on Day 1
NCT00672984 (14) [back to overview]Change From Baseline in Heart Rate (HR) at Tmax on Day 6
NCT00672984 (14) [back to overview]Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 1
NCT00672984 (14) [back to overview]Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 6
NCT00672984 (14) [back to overview]Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 1
NCT00672984 (14) [back to overview]Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 6
NCT00672984 (14) [back to overview]Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 6
NCT00672984 (14) [back to overview]Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 1
NCT00672984 (14) [back to overview]Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 6
NCT00672984 (14) [back to overview]Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 1
NCT00672984 (14) [back to overview]Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 1
NCT00728507 (1) [back to overview]To Compare, by Treatment Group, the Percentage of Patients With a Negative Sputum Culture at the End of Intensive Phase Therapy.
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - General Activities
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Household Duties
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Item Satisfaction
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Leisure Time Activities
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Overall Life Satisfaction and Contentment
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Participant Feeling
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Physical Health
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - School/Course Work
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Social Relationship
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Work
NCT00754065 (117) [back to overview]Mean Length of Bleeding / Spotting Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Mean Length of Bleeding / Spotting Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Mean Length of Bleeding / Spotting Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Mean Length of Bleeding / Spotting Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Mean Length of Spotting-only Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Mean Length of Spotting-only Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Mean Length of Spotting-only Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Mean Length of Spotting-only Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Number of Bleeding / Spotting Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Number of Bleeding / Spotting Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Number of Bleeding / Spotting Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Number of Bleeding / Spotting Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Number of Days With Bleeding or Spotting in Reference Period 1
NCT00754065 (117) [back to overview]Number of Days With Bleeding or Spotting in Reference Period 2
NCT00754065 (117) [back to overview]Number of Days With Bleeding or Spotting in Reference Period 3
NCT00754065 (117) [back to overview]Number of Days With Bleeding or Spotting in Reference Period 4
NCT00754065 (117) [back to overview]Number of Days With Spotting-only in Reference Period 1
NCT00754065 (117) [back to overview]Number of Days With Spotting-only in Reference Period 2
NCT00754065 (117) [back to overview]Number of Days With Spotting-only in Reference Period 3
NCT00754065 (117) [back to overview]Number of Days With Spotting-only in Reference Period 4
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Days at Cycle 1
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Days at Cycle 13
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Days at Cycle 3
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Days at Cycle 6
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Episodes at Cycle 1
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Episodes at Cycle 13
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Episodes at Cycle 3
NCT00754065 (117) [back to overview]Number of Intracyclic Bleeding Episodes at Cycle 6
NCT00754065 (117) [back to overview]Number of Spotting-only Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Number of Spotting-only Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Number of Spotting-only Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Number of Spotting-only Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Onset of Withdrawal Bleeding Episodes at Cycle 1
NCT00754065 (117) [back to overview]Onset of Withdrawal Bleeding Episodes at Cycle 13
NCT00754065 (117) [back to overview]Onset of Withdrawal Bleeding Episodes at Cycle 3
NCT00754065 (117) [back to overview]Onset of Withdrawal Bleeding Episodes at Cycle 6
NCT00754065 (117) [back to overview]The Change in Average of the 3 Highest Visual Analog Scale (VAS) Values of the Hormone Withdrawal-associated Symptoms Pelvic Pain or Headache During Cycle Days 22 to 28 From Baseline to Cycle 6
NCT00754065 (117) [back to overview]The Change of Pelvic Pain or Headache as Determined by the Highest Visual Analog Scale (VAS) Values During Cycle Days 22 to 28 From Baseline to Cycle 6
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 13 in the Number of Days With at Least Moderate Pain/Intensity of Individual Hormone-related Symptoms During Cycle Days 1-21
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 13 in the Number of Days With at Least Moderate Pain/Intensity of Individual Hormone-related Symptoms During the Hormone-free Interval Cycle Days 27 to 28 for EV/DNG and Cycle Days 22 to 28 for EE/NGM
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 13 in the Number of Days With at Least Moderate Pain/Intensity of Other Hormone-related Symptoms During Cycle Days 22-28
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 6 in the Number of Days With at Least Moderate Pain/Intensity of Individual Hormone-related Symptoms During Cycle Days 1-21
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 6 in the Number of Days With at Least Moderate Pain/Intensity of Individual Hormone-related Symptoms During the Hormone-free Interval Cycle Days 27 to 28 for EV/DNG and Cycle Days 22 to 28 for EE/NGM
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 6 in the Number of Days With at Least Moderate Pain/Intensity of Other Hormone-related Symptoms During Cycle Days 22-28
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Psychological General Well-Being Index (PGWBI)
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 6 in Psychological General Well-Being Index (PGWBI)
NCT00754065 (117) [back to overview]Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 1
NCT00754065 (117) [back to overview]Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 13
NCT00754065 (117) [back to overview]Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 3
NCT00754065 (117) [back to overview]Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 6
NCT00754065 (117) [back to overview]Percentage of Participants With / Without Withdrawal Bleeding at Cycle 1
NCT00754065 (117) [back to overview]Percentage of Participants With / Without Withdrawal Bleeding at Cycle 13
NCT00754065 (117) [back to overview]Percentage of Participants With / Without Withdrawal Bleeding at Cycle 3
NCT00754065 (117) [back to overview]Percentage of Participants With / Without Withdrawal Bleeding at Cycle 6
NCT00754065 (117) [back to overview]Percentage of Participants With at Least 1 Intracyclic Bleeding Episode at Cycles 2 to 13
NCT00754065 (117) [back to overview]Percentage of Participants With at Least 1 Intracyclic Bleeding Episode at Cycles 2 to 6
NCT00754065 (117) [back to overview]Percentage of Participants With Improvement in the Investigator's Assessment in Clinical Global Impression (CGI) at Cycle 13
NCT00754065 (117) [back to overview]Percentage of Participants With Improvement in the Investigator's Assessment in Clinical Global Impression (CGI) at Cycle 6
NCT00754065 (117) [back to overview]Percentage of Participants With Improvement in the Participant's Assessment in Clinical Global Impression (CGI) at Cycle 13
NCT00754065 (117) [back to overview]Percentage of Participants With Improvement in the Participant's Assessment in Clinical Global Impression (CGI) at Cycle 6
NCT00754065 (117) [back to overview]Percentage of Participants With no Increase in Rescue Medication and VAS Decrease During Cycle Days 22 to 28 From Baseline to Cycle 6
NCT00754065 (117) [back to overview]Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 1
NCT00754065 (117) [back to overview]Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 13
NCT00754065 (117) [back to overview]Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 3
NCT00754065 (117) [back to overview]Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 6
NCT00754065 (117) [back to overview]The Change From Baseline to Cycle 13 in the Number of Ibuprofen Tablets Used as Rescue Medication
NCT00754065 (117) [back to overview]The Change From Baseline to Cycle 6 in the Number of Ibuprofen Tablets Used as Rescue Medication
NCT00754065 (117) [back to overview]Maximum Length of Spotting-only Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 13 in the Average of the Three Highest VAS Values of the Hormone Withdrawal-associated Symptoms Pelvic Pain or Headache During Cycle Days 22 to 28
NCT00754065 (117) [back to overview]Change From Baseline to Cycle 3 in the Average of the Three Highest VAS Values of the Hormone Withdrawal-associated Symptoms Pelvic Pain or Headache During Cycle Days 22 to 28
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Length of Withdrawal Bleeding Episodes at Cycle 1
NCT00754065 (117) [back to overview]Length of Withdrawal Bleeding Episodes at Cycle 13
NCT00754065 (117) [back to overview]Length of Withdrawal Bleeding Episodes at Cycle 3
NCT00754065 (117) [back to overview]Length of Withdrawal Bleeding Episodes at Cycle 6
NCT00754065 (117) [back to overview]Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 1
NCT00754065 (117) [back to overview]Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 13
NCT00754065 (117) [back to overview]Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 3
NCT00754065 (117) [back to overview]Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 6
NCT00754065 (117) [back to overview]Maximum Length of Bleeding / Spotting Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Maximum Length of Bleeding / Spotting Episodes in Reference Period 2
NCT00754065 (117) [back to overview]Maximum Length of Bleeding / Spotting Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Maximum Length of Bleeding / Spotting Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Maximum Length of Intracyclic Bleeding Episodes at Cycle 1
NCT00754065 (117) [back to overview]Maximum Length of Intracyclic Bleeding Episodes at Cycle 13
NCT00754065 (117) [back to overview]Maximum Length of Intracyclic Bleeding Episodes at Cycle 3
NCT00754065 (117) [back to overview]Maximum Length of Intracyclic Bleeding Episodes at Cycle 6
NCT00754065 (117) [back to overview]Maximum Length of Spotting-only Episodes in Reference Period 1
NCT00754065 (117) [back to overview]Maximum Length of Spotting-only Episodes in Reference Period 3
NCT00754065 (117) [back to overview]Maximum Length of Spotting-only Episodes in Reference Period 4
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - General Activities
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Household Duties
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Item Satisfaction
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Leisure Time Activities
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Overall Life Satisfaction and Contentment
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Participant Feeling
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Physical Health
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - School/Course Work
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Social Relationship
NCT00754065 (117) [back to overview]Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Work
NCT00759148 (2) [back to overview]Microbiological Success at the Day 4 (EOT)/Exit Visit
NCT00759148 (2) [back to overview]Clinical Cure at the Day 4 (EOT)/Exit Visit
NCT00795145 (15) [back to overview]Cohort 2: Tmax and t1/2
NCT00795145 (15) [back to overview]Cohort 1: Number of Subjects With Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT00795145 (15) [back to overview]Cohort 1: Time to Reach Maximum Observed Plasma Concentration (Tmax) and Plasma Decay Half-Life (t1/2)
NCT00795145 (15) [back to overview]Cohort 2: AUC Inf and AUC Last
NCT00795145 (15) [back to overview]Cohort 2: Mean Time-Matched Difference in Time Corresponding to Beginning of Depolarization to Repolarization of the Ventricles, Corrected for Heart Rate Using Fridericia's Formula (QTcF Interval) Between Linezolid 600 mg and 1200 mg Compared to Placebo
NCT00795145 (15) [back to overview]Cohort 2: Mean Time-Matched Difference in Uncorrected QT Intervals Between Linezolid 600 mg and 1200 mg Compared to Placebo
NCT00795145 (15) [back to overview]Cohort 2: Number of Subjects With AEs and SAEs
NCT00795145 (15) [back to overview]Cohort 2: Cmax
NCT00795145 (15) [back to overview]Cohort 2: CL
NCT00795145 (15) [back to overview]Cohort 1: Steady-State Volume of Distribution (Vss)
NCT00795145 (15) [back to overview]Cohort 1: Maximum Observed Plasma Concentration (Cmax)
NCT00795145 (15) [back to overview]Cohort 1: Clearance of Linezolid (CL)
NCT00795145 (15) [back to overview]Cohort 2: Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin and Placebo
NCT00795145 (15) [back to overview]Cohort 1: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC Inf) and Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC Last)
NCT00795145 (15) [back to overview]Cohort 2: Vss
NCT00824070 (1) [back to overview]The Aqueous Humor Drug Concentration.
NCT00864383 (9) [back to overview]Number of Patients Who Are Culture Negative (Liquid MGIT Culture)
NCT00864383 (9) [back to overview]Time to First Culture Negative Sputum Sample (MGIT Liquid Media)
NCT00864383 (9) [back to overview]Combined Failure of Bacteriological Cure and Relapse as Defined by Culture Using Liquid Media (Mycobacteria Growth Indicator Tube-MGIT).
NCT00864383 (9) [back to overview]Time to First Culture Negative Sputum Sample (LJ Solid Media)
NCT00864383 (9) [back to overview]Sensitivity Analysis Assuming All Losses to Follow-up and Non-tuberculous Deaths Have an Unfavorable Outcome Using Solid (L-J) Media.
NCT00864383 (9) [back to overview]Sensitivity Analyses Assuming All Losses to Follow-up and Non-tuberculous Deaths Have a Favourable Outcome Using Solid (L-J) Media.
NCT00864383 (9) [back to overview]Number of Patients With Grade 3 or 4 Adverse Events (Using a Modified Division of Acquired Immunodeficiency Syndrome National Institute of Allergy and Infectious Diseases [DAIDS] Scale of Adverse Event Reporting)
NCT00864383 (9) [back to overview]Number of Patients Who Are Culture Negative (Solid LJ Culture)
NCT00864383 (9) [back to overview]Combined Failure of Bacteriological Cure and Relapse Within One Year of Completion of Therapy as Defined by Culture Using Solid Media (Lowenstein-Jensen - LJ).
NCT00865280 (7) [back to overview]Number of Participants Classified as a Sponsor-defined Clinical Success in the ITT Population at Test of Cure
NCT00865280 (7) [back to overview]Number of Participants With Cellulitis Classified as a Sponsor-defined Clinical Success in the CE Population at Test of Cure
NCT00865280 (7) [back to overview]Number of Participants With Wound Infections Classified as a Sponsor-defined Clinical Success in the CE Population at Test of Cure
NCT00865280 (7) [back to overview]Number of Participants With Cellulitis Classified as a Sponsor-defined Clinical Success in the CE Population at End of Treatment
NCT00865280 (7) [back to overview]Number of Participants Classified as a Sponsor-defined Clinical Success in the Intent-to-Treat (ITT) Population at End of Treatment
NCT00865280 (7) [back to overview]Number of Participants With the Indicated Type of Adverse Event (AE)
NCT00865280 (7) [back to overview]Number of Participants With Wound Infections Classified as a Sponsor-defined Clinical Success in the Clinically Evaluable (CE) Population at End of Treatment
NCT00870103 (2) [back to overview]The Percentage of Patients With no Ocular Pain
NCT00870103 (2) [back to overview]The Percentage of Patients With a Score of Zero for Anterior Chamber Cells.
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 30 ms
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI Change > 60 ms
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI > 480 ms
NCT00874237 (7) [back to overview]Numbers and % of Subjects With QTcI > 450 ms
NCT00874237 (7) [back to overview]Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)
NCT00874237 (7) [back to overview]Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo
NCT00874237 (7) [back to overview]Cardiac Repolarization Change (QTcI) Versus Loxapine Concentration Relationship Following Treatment With Staccato Loxapine in Healthy Volunteers.
NCT00874887 (1) [back to overview]Percentage of Subjects With Strain Resistance of the Conjunctiva as Determined by Minimum Inhibitory Concentration (MIC) at Day 14
NCT00924729 (1) [back to overview]Aqueous Humor Concentration of Study Drug
NCT00926263 (12) [back to overview]Serum Concentration of Fasting Glucose
NCT00926263 (12) [back to overview]Anti-drug Antibodies (ADA) Against CP-751,871 in Serum Samples
NCT00926263 (12) [back to overview]Serum Concentration of Insulin-like Growth Factor Binding Protein 3 (IGFBP-3)
NCT00926263 (12) [back to overview]Serum Concentration of Free Insulin-like Growth Factor 1 (IGF-1)
NCT00926263 (12) [back to overview]Serum Concentration of Insulin
NCT00926263 (12) [back to overview]Plasma Decay Half-Life (t1/2)
NCT00926263 (12) [back to overview]Plasma Clearance (CL)
NCT00926263 (12) [back to overview]Maximum Observed Plasma Concentration (Cmax)
NCT00926263 (12) [back to overview]Area Under the Curve From Time Zero to the Last Time Point With Quantifiable Concentration (AUClast)
NCT00926263 (12) [back to overview]Apparent Volume of Distribution (Vz)
NCT00926263 (12) [back to overview]Serum Concentration of Insulin-like Growth Factor 1 (IGF-1)
NCT00926263 (12) [back to overview]Serum Concentration of Insulin-like Growth Factor 2 (IGF-2)
NCT00983957 (13) [back to overview]Area Under the Concentration-Time Curve in 1 Dosing Interval of Norgestrel
NCT00983957 (13) [back to overview]Area Under the Concentration-Time Curve in 1 Dosing Interval of Norelgestromin
NCT00983957 (13) [back to overview]Maximum Observed Plasma Concentration of Norelgestromin
NCT00983957 (13) [back to overview]Number of Participants Demonstrating a Clinically Meaningful Effect in Vital Signs
NCT00983957 (13) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Ethinyl Estradiol
NCT00983957 (13) [back to overview]Number of Participants With Serious Adverse Events (SAEs), Adverse Events (AEs) Leading to Discontinuation, and Who Died
NCT00983957 (13) [back to overview]Number of Participants With Laboratory Test Abnormalities
NCT00983957 (13) [back to overview]Area Under the Concentration-Time Curve (AUC) in 1 Dosing Interval of Ethinyl Estradiol
NCT00983957 (13) [back to overview]Time of Maximum Observed Plasma Concentration of Norgestrel
NCT00983957 (13) [back to overview]Time of Maximum Observed Plasma Concentration of Norelgestromin
NCT00983957 (13) [back to overview]Time of Maximum Observed Plasma Concentration of Ethinyl Estradiol
NCT00983957 (13) [back to overview]Number of Participants Demonstrating a Clinically Meaningful Effect in ECG Parameters
NCT00983957 (13) [back to overview]Maximum Observed Plasma Concentration of Norgestrel
NCT01017731 (6) [back to overview]Area Under Concentration (AUC) During Cycle 1
NCT01017731 (6) [back to overview]Number of Participants With Drug-Related Adverse Events (AEs)
NCT01017731 (6) [back to overview]Maximum Concentration (Cmax) During Cycle 3
NCT01017731 (6) [back to overview]Maximum Concentration (Cmax) During Cycle 1
NCT01017731 (6) [back to overview]Area Under Concentration (AUC) During Cycle 3
NCT01017731 (6) [back to overview]Change From Baseline to Cycle 3 in QT/Corrected QT (QTc) Interval Prolongation in Participants
NCT01018420 (5) [back to overview]Maximum Plasma Concentration (Cmax)
NCT01018420 (5) [back to overview]Electrocardiogram (ECG) Evaluation of the QTcF Interval (Moxifloxacin)
NCT01018420 (5) [back to overview]Electrocardiogram (ECG) Evaluation of the QTcF Interval (Colchicine)
NCT01018420 (5) [back to overview]Area Under the Concentration Versus Time Curve From Time 0 to Time t [AUC(0-t)]
NCT01018420 (5) [back to overview]Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-∞)]
NCT01069900 (20) [back to overview]QT Interval Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01069900 (20) [back to overview]QRS Interval Changes in Electrocardiogram (ECG) Profiles From Predose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01069900 (20) [back to overview]PR Interval Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01069900 (20) [back to overview]Potentially Clinically Significant Electrocardiogram (ECG) QTc Interval Prolongation - by QTc Interval Calc Fridericia Correction on Treatment Day 1 and During Therapy Day 3
NCT01069900 (20) [back to overview]Bacteriological Response at the End of Treatment (EOT) Visit
NCT01069900 (20) [back to overview]Potentially Clinically Significant Electrocardiogram (ECG) QTc Interval Prolongation - by QTc Calc Bazett Correction on Treatment Day 1 and During Therapy Day 3
NCT01069900 (20) [back to overview]Number of Subjects With Adverse Events
NCT01069900 (20) [back to overview]Bacteriological Response at Test-of-Cure (TOC) Visit
NCT01069900 (20) [back to overview]Bacteriological Response at a 'During Therapy' Visit
NCT01069900 (20) [back to overview]Number of Subjects With Musculoskeletal Adverse Events
NCT01069900 (20) [back to overview]Number of Subjects With Clinical Cardiac Adverse Events
NCT01069900 (20) [back to overview]Incidence Rates of Musculoskeletal Adverse Events by Primary System Organ Class (SOC) and Preferred Term
NCT01069900 (20) [back to overview]Heart Rate Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01069900 (20) [back to overview]Corrected QT (QTc) Interval Calculated (Calc) Fridericia Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01069900 (20) [back to overview]Corrected QT (QTc) Interval Calculated (Calc) Bazett Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01069900 (20) [back to overview]Clinical Response at the End-of-Treatment (EOT) Visit
NCT01069900 (20) [back to overview]Clinical Response at Test-of-Cure (TOC) Visit in Subjects With Bacteriologically Confirmed Complicated Intra-abdominal Infection (cIAI)
NCT01069900 (20) [back to overview]Clinical Response at Test-of-Cure (TOC) Visit
NCT01069900 (20) [back to overview]Clinical Response at a 'During Therapy' Visit
NCT01069900 (20) [back to overview]RR Interval Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3
NCT01148537 (8) [back to overview]The Average Differences From Baseline Between Moxifloxacin and Placebo by Fridericia's Corrected Interval (QTcF) on Day 6 and Day 13
NCT01148537 (8) [back to overview]The Average Differences From Baseline Between BTDS and Placebo by Fridericia's Corrected Interval (QTcF) on Day 6 and Day 13
NCT01148537 (8) [back to overview]The Average Differences From Baseline Between BTDS and Placebo by Bazett Corrected QT Interval (QTcB) on Day 6 and Day 13
NCT01148537 (8) [back to overview]The Comparison of Moxifloxacin to Placebo Transdermal System (TDS): the Average Difference From Baseline Using QT Interval Corrected From Within-subject Data (QTci) on Day 13
NCT01148537 (8) [back to overview]The Comparison of BTDS to Placebo Transdermal System (TDS): the Average Difference From Baseline Using QT Corrected From Within-subject Data (QTci) on Day 13
NCT01148537 (8) [back to overview]The Average Differences Between Moxifloxacin vs Placebo From Baseline by Interval Corrected From Within-subject Data (QTci) on Day 6
NCT01148537 (8) [back to overview]The Average Differences Between BTDS vs Placebo From Baseline by Interval Corrected From Within-subject Data (QTci) on Day 6
NCT01148537 (8) [back to overview]The Average Differences From Baseline Between Moxifloxacin and Placebo of Bazett Corrected QT Interval (QTcB) on Day 6 and Day 13
NCT01191723 (5) [back to overview]Change From Baseline in QTcI for MAP0004 3.0mg and Placebo at 30 Minutes
NCT01191723 (5) [back to overview]Change From Baseline in QTcF for MAP0004 3.0mg, Placebo, and Moxifloxacin at 2 Hours
NCT01191723 (5) [back to overview]Change From Baseline in QTcF for MAP0004 3.0mg and Placebo at 30 Minutes
NCT01191723 (5) [back to overview]Change From Baseline in Heart Rate for MAP0004 3.0mg, Placebo, and Moxifloxacin at 30 Minutes and 2 Hours
NCT01191723 (5) [back to overview]Change From Baseline in QTcI for MAP0004 3.0mg, Placebo, and Moxifloxacin at 2 Hours
NCT01195675 (10) [back to overview]Empa 25 mg: Mean QTcN Change From Baseline Between 30 Minutes and 24 Hours After Dosing
NCT01195675 (10) [back to overview]Mean QTcN Change From Baseline Between 2 and 4 Hours After Dosing
NCT01195675 (10) [back to overview]Placebo Corrected Change From Mean Baseline at Any Time Point Between 30 Minutes and 24 Hours After Dosings.
NCT01195675 (10) [back to overview]Time-matched Change From Placebo in QTcN Between 30 Minutes and 24 Hours After Dosing.
NCT01195675 (10) [back to overview]Empa 200mg: Mean QTcN Change From Baseline Between 1 and 4 Hours After Dosing
NCT01195675 (10) [back to overview]Empa 200mg: Change From Mean Baseline in QTcN at Each Time Point Between 30 Minutes and 24 Hours After Dosings
NCT01195675 (10) [back to overview]Clinically Relevant Abnormalities for Physical Examination, Vital Signs, ECG, Blood Chemistry and Assessment of Tolerability by the Investigator
NCT01195675 (10) [back to overview]Empa 200 mg: Mean QTcN Change From Baseline Between 30 Minutes and 24 Hours After Dosing
NCT01195675 (10) [back to overview]Empa 25mg: Mean QTcN Change From Baseline Between 1 and 4 Hours After Dosing
NCT01195675 (10) [back to overview]Empa 25mg: Change From Mean Baseline in QTcN at Each Time Point Between 30 Minutes and 24 Hours After Dosings
NCT01215851 (5) [back to overview]Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 2-14).
NCT01215851 (5) [back to overview]Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 7-14).
NCT01215851 (5) [back to overview]Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 0-14)
NCT01215851 (5) [back to overview]Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-14).
NCT01215851 (5) [back to overview]Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-2).
NCT01243580 (13) [back to overview]Evaluation of LNG Css (1) Between AG200-15 in Week 1 and 3
NCT01243580 (13) [back to overview]Evaluation of LNG Cmax Between AG200-15 in Week 1 and 3
NCT01243580 (13) [back to overview]Evaluation of LNG AUC (0-168hrs Post-first Dose) Between AG200-15 in Week 1 and 3
NCT01243580 (13) [back to overview]Comparative Evaluation of Ethinyl Estradiol (EE) Cmax Between AG200-15 and Ortho-Cyclen® in Week 1
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Css (2) Between AG200-15 and Ortho-Cyclen® in Week 1
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Css (2) Between AG200-15 and Ortho-Cyclen® in Week 3
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Css (3) Between AG200-15 and Ortho-Cyclen® in Week 3
NCT01243580 (13) [back to overview]Comparative Evaluation of EE AUC (0-168hrs Post-first Dose) Between AG200-15 and Ortho-Cyclen® in Week 3
NCT01243580 (13) [back to overview]Comparative Evaluation of EE AUC(0-168hrs Post-first Dose) Between AG200-15 and Ortho-Cyclen® in Week 1
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Cmax Between AG200-15 and Ortho-Cyclen® in Week 3
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Css (1) Between AG200-15 and Ortho-Cyclen® in Week 1
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Css (1) Between AG200-15 and Ortho-Cyclen® in Week 3
NCT01243580 (13) [back to overview]Comparative Evaluation of EE Css (3) Between AG200-15 and Ortho-Cyclen® in Week 1
NCT01296191 (1) [back to overview]Pharmacokinetics in Aqueous Humor Samples.
NCT01296542 (1) [back to overview]Number of Subjects With a Change in Bacterial Colonization of Lid and Conjunctival Cultures After 3 Days
NCT01297062 (9) [back to overview]Number of Subjects With Increase of QTcP Interval From Baseline >30msec at Any Timepoint on Any Day in Exenatide and Placebo
NCT01297062 (9) [back to overview]Comparison of LS Mean Changes From Baseline in QTcP Intervals Between Exenatide and Placebo on Day 3 Averaged Over 1300h, 1400h, 1500h (Target Steady State Exenatide Concentration of 500 pg/mL)
NCT01297062 (9) [back to overview]Comparison of LS Mean Changes From Baseline in QTcP Intervals Between Exenatide and Placebo on Day 2 Averaged Over 1300h, 1400h, 1500h (Target Steady State Exenatide Concentration of 300 pg/mL)
NCT01297062 (9) [back to overview]Comparison of Least Squares (LS) Mean Changes From Baseline in Population-based Corrected QT Intervals (QTcP) Between Exenatide and Placebo on Day 1 Averaged Over 1300h, 1400h, 1500h (Target Steady State Exenatide Concentration of 200 pg/mL)
NCT01297062 (9) [back to overview]Assay Sensitivity of Moxifloxacin at 1100h (2 Hour Post-administration of Moxifloxacin) on Day 2
NCT01297062 (9) [back to overview]Assay Sensitivity of Moxifloxacin at 1000h (1 Hour Post-administration of Moxifloxacin) on Day 2
NCT01297062 (9) [back to overview]Assay Sensitivity of Moxifloxacin at 1200h (3 Hour Post-administration of Moxifloxacin) on Day 2
NCT01297062 (9) [back to overview]Plasma Exenatide Concentrations at Steady State on Day 1, 2 and 3
NCT01297062 (9) [back to overview]Number of Subjects With QTcP Interval >450msec at Any Timepoint on Any Day in Exenatide and Placebo
NCT01373931 (3) [back to overview]Pharmacokinetics: Time to Maximum Plasma Concentration (Tmax) of Ethinyl Estradiol and Norelgestromin
NCT01373931 (3) [back to overview]Area Under the Concentration-Time Curve Over a Dosing Interval (AUCτ) of Ethinyl Estradiol and Norelgestromin
NCT01373931 (3) [back to overview]Pharmacokinetics: Maximum Plasma Concentration (Cmax) of Ethinyl Estradiol and Norelgestromin
NCT01423916 (13) [back to overview]Change From Baseline in Summary of Maximum QTcI on Day 11 Minus Mean QTcI on Day -1 (Baseline).
NCT01423916 (13) [back to overview]Change From Baseline in Summary of Maximum QTcI on Day 11 Minus Maximum QTcI on Day -1 (Baseline).
NCT01423916 (13) [back to overview]Area Under the Plasma Concentration-time Curve During Dosing (AUCT).
NCT01423916 (13) [back to overview]Number Participants Noted With New Incidence of QT Interval of > 500 Msec on Day 11.
NCT01423916 (13) [back to overview]Number of Participants With QTcI Interval Between 30 and 60 Msec on Day 11.
NCT01423916 (13) [back to overview]Maximum Peak Plasma Concentration (Cmax) of Brexpiprazole and Moxifloxacin.
NCT01423916 (13) [back to overview]Time-matched QTcI Change From Baseline (Day -1) Corrected for Placebo on Day 11 Following Brexpiprazole Treatment.
NCT01423916 (13) [back to overview]Number of Participants With New Incidence of ECG Morphology Abnormalities on Day 11.
NCT01423916 (13) [back to overview]Number of Participants With Maximum Change From Baseline to the On-treatment ECG Values on Day 11 for Heart Rate (HR), PR Interval, and QRS Interval.
NCT01423916 (13) [back to overview]Number of Participants With Adverse Events (AE) and Clinically Important Changes in Vital Signs, Physical Examinations, Laboratory Tests, and Standard ECGs (Electrocardiogram).
NCT01423916 (13) [back to overview]Number of Participants Noted With Time-matched Change in Mean QTcI Change From Baseline for Assay Sensitivity of Moxifloxacin Treatment Corrected for Placebo at Day 11.
NCT01423916 (13) [back to overview]Number of Participants With QTcI Interval > 60 Msec on Day 11.
NCT01423916 (13) [back to overview]Time to Maximum (Peak) Plasma Concentration (Tmax) of Brexpiprazole and Moxifloxacin.
NCT01458210 (6) [back to overview]Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of Ortho-Cyclen - Norelgestromin (NGMN)
NCT01458210 (6) [back to overview]Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of Ortho-Cyclen - Ethinyl Estradiol (EE)
NCT01458210 (6) [back to overview]Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Ortho-Cyclen - Norelgestromin (NGMN)
NCT01458210 (6) [back to overview]Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Ortho-Cyclen - Ethinyl Estradiol (EE)
NCT01458210 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) at Steady State of Ortho-Cyclen - Norelgestromin (NGMN)
NCT01458210 (6) [back to overview]Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) at Steady State of Ortho-Cyclen - Ethinyl Estradiol (EE)
NCT01460368 (2) [back to overview]Part B: Mean Change From Baseline in 12-lead Electrocardiogram (ECG) Corrected QT Intervals (Moxifloxacin)
NCT01460368 (2) [back to overview]Part B: Mean Change From Baseline in 12-lead Electrocardiogram (ECG) Corrected QT Intervals (LY2409021)
NCT01466673 (10) [back to overview]Change From Baseline in Blood Pressure (BP) at Month 6
NCT01466673 (10) [back to overview]Change From Baseline in Body Weight at Month 6
NCT01466673 (10) [back to overview]Change From Baseline in Total and Each Type of Acne Lesions Count at Month 6
NCT01466673 (10) [back to overview]Number of Participants Non-Compliant With Therapy
NCT01466673 (10) [back to overview]Number of Participants With Treatment Response at the End-of-Therapy by Participant's Self-Assessment at Month 6
NCT01466673 (10) [back to overview]Percentage of Participants Showing Treatment Response on the Investigator's Global Assessment at Month 6
NCT01466673 (10) [back to overview]Number of Participants With Abnormal Vaginal Blood Loss at Month 1, 3 and 6
NCT01466673 (10) [back to overview]Change From Baseline in Total and Each Type of Acne Lesions Count at Month 3
NCT01466673 (10) [back to overview]Percentage of Participants With Categorical Score for Sebum Assessment at Month 1, 3 and 6
NCT01466673 (10) [back to overview]Change From Baseline in Total and Each Type of Acne Lesions Count at Month 1
NCT01475513 (16) [back to overview]Change From Baseline in Fasting Glucose at 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Body Mass Index in 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Disposition Index at 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Carotid Intima Media Thickness
NCT01475513 (16) [back to overview]Change From Baseline in Areas-under-the-curve for Insulin at 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Areas-under-the-curve for Glucose
NCT01475513 (16) [back to overview]Change From Baseline in Acute Insulin Response to Glucose
NCT01475513 (16) [back to overview]Change in Triglycerides From Baseline to 6 Months
NCT01475513 (16) [back to overview]Change in LDL From Baseline to 6 Months
NCT01475513 (16) [back to overview]Change in Diastolic Blood Pressure From Baseline to 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Systolic Blood Pressure at 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Insulin Sensitivity
NCT01475513 (16) [back to overview]Change From Baseline in HDL at 6 Months
NCT01475513 (16) [back to overview]Change From Baseline in Glucose Effectiveness
NCT01475513 (16) [back to overview]Change From Baseline in Flow-mediated Vasodilatation
NCT01475513 (16) [back to overview]Change From Baseline in Fasting Insulin at 6 Months
NCT01498419 (7) [back to overview]Percentage of Participants Who Discontinue Due to an Adverse Event in Each Experimental Arm.
NCT01498419 (7) [back to overview]Percentage of Patients With Sputum Culture Conversion at 8 Weeks on Liquid Media
NCT01498419 (7) [back to overview]Percentage of Patients With Sputum Culture Conversion at 8 Weeks on Solid Media
NCT01498419 (7) [back to overview]The Rate of Change in Colony Forming Units (CFUs) Using Non-linear Mixed Effects Modeling of the Serial Sputum Colony Counts (SSCC) Over 8 Weeks of Treatment.
NCT01498419 (7) [back to overview]The Rate of Change in Time to Sputum Culture Positivity (TTP) Through 8 Weeks in the MGIT System in Sputum Over 8 Weeks in Participants as Derived From a Non-linear Regression Model.
NCT01498419 (7) [back to overview]Time to Sputum Conversion Using Data From Weekly Cultures Through 8 Weeks on Liquid Media
NCT01498419 (7) [back to overview]Time to Sputum Conversion Using Data From Weekly Cultures Through 8 Weeks on Solid Media
NCT01518699 (1) [back to overview]Difference Between Active and Placebo for Time Matched Baseline Adjusted Mean QTcF
NCT01536951 (4) [back to overview]Pharmacokinetics: Area Under the Concentration Curve From Time 0 to Infinity [AUC(0-inf)] of LY3009104
NCT01536951 (4) [back to overview]Pharmacokinetics: Maximum Concentration (Cmax) of LY3009104
NCT01536951 (4) [back to overview]Change From Baseline Through 24 Hours Postdose in Population-Corrected QT (QTcP) Interval
NCT01536951 (4) [back to overview]Number of Participants With 1 or More Drug-Related Adverse Events (AEs) or Any Serious AEs (SAEs)
NCT01537887 (4) [back to overview]Change From Baseline to Day 10 in QT Interval Corrected for Heart Rate (QTc) for LY2484595 Versus Placebo
NCT01537887 (4) [back to overview]Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2484595 During One Dosing Interval at Steady State
NCT01537887 (4) [back to overview]Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY2484595 During One Dosing Interval at Steady State
NCT01537887 (4) [back to overview]Percentage Change From Baseline to Day 11 in Fasting Lipids and Apolipoproteins
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in Heart Rate From Time-Matched Analysis by Largest Time Point
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QTcF Intervals at Subject-Specific Tmax
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QTcF Intervals From Time-Matched Analysis by Largest Time Point
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QTcNi Intervals at Subject-Specific Time of Maximum Plasma Concentration (Tmax)
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QTcNi Intervals From Time-Matched Analysis by Largest Time Point
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in Heart Rate at Subject-Specific Tmax
NCT01552928 (14) [back to overview]Maximum Plasma Concentration (Cmax) of Metabolite of 2.5 mg Anagrelide (BCH24426) in Males and Females
NCT01552928 (14) [back to overview]Maximum Plasma Concentration (Cmax) of 2.5 mg Anagrelide in Males and Females
NCT01552928 (14) [back to overview]Maximum Plasma Concentration (Cmax) of 0.5 mg Anagrelide in Males and Females
NCT01552928 (14) [back to overview]Maximum Plasma Concentration (Cmax) of Metabolite of 0.5 mg Anagrelide (BCH24426) in Males and Females
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QTcB Intervals From Time-Matched Analysis by Largest Time Point
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QTcB Intervals at Subject-Specific Tmax
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QT Intervals From Time-Matched Analysis by Largest Time Point
NCT01552928 (14) [back to overview]Mean Difference Changes From Baseline Versus Placebo in QT Intervals at Subject-Specific Tmax
NCT01573910 (2) [back to overview]Clinical Cure Rate
NCT01573910 (2) [back to overview]Microbiological Success Rate
NCT01589497 (32) [back to overview]AUC0-24hour for Pyrazinamide (PZA)
NCT01589497 (32) [back to overview]Isoniazid PK Parameter Cmax at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CLast at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CLast at Day 1
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CL/F at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter CL/F at Day 1
NCT01589497 (32) [back to overview]Daily Decrease in log10 Transformed Colony-forming Unit (CFU) Counts Per ml Sputum From Baseline (Study Treatment Initiation) to Day 14
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Day 2 to Day 14
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 2
NCT01589497 (32) [back to overview]Daily Change in Time to Positivity (TTP) From Baseline (Study Treatment Initiation) to Day 14
NCT01589497 (32) [back to overview]Daily Change in log10 Transformed Colony-forming Unit (CFU) Counts Per mL Sputum From Baseline (Study Treatment Initiation) to Day 2
NCT01589497 (32) [back to overview]Daily Change in log10 Colony-forming Unit (CFU) Counts Per mL Sputum From Day 2 to Day 14
NCT01589497 (32) [back to overview]Correlation Between Time to Positivity (TTP) and log10 Transformed Colony-forming Unit (CFU) Counts Per mL
NCT01589497 (32) [back to overview]AUC0-24hour for Isoniazid at Day 14
NCT01589497 (32) [back to overview]AUC0-24hour for Isoniazid (INH) at Day 1
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Maximum Plasma Concentration (Cmax)
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Last Concentration (CLast)
NCT01589497 (32) [back to overview]Rifampicin PK Parameter Clearance (CL/F)
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter Cmax
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter CLast
NCT01589497 (32) [back to overview]Pyrazinamide PK Parameter CL/F
NCT01589497 (32) [back to overview]Pharmacokinetic Parameter (PK) Area Under the Concentration-time Curve (AUC0-24hour) for Rifampicin (RIF)
NCT01589497 (32) [back to overview]Log10 Transformed Colony-forming Unit (CFU) Count Per mL From Sputum Samples at Baseline and Day 14
NCT01589497 (32) [back to overview]Ethambutol PK Parameter Cmax
NCT01589497 (32) [back to overview]Ethambutol PK Parameter CLast
NCT01589497 (32) [back to overview]Ethambutol PK Parameter CL/F
NCT01589497 (32) [back to overview]AUC0-24hour for Ethambutol (EMB)
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter Cmax at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter CLast at Day 14
NCT01589497 (32) [back to overview]Moxifloxacin PK Parameter CL/F at Day 14
NCT01589497 (32) [back to overview]Isoniazid PK Parameter Cmax at Day 14
NCT01589497 (32) [back to overview]AUC0-24hour for Moxifloxacin (Mox) at Day 14
NCT01606436 (2) [back to overview]Change From Baseline up to 12 Hours Postdose in QT Interval Corrected for Heart Rate (QTc)
NCT01606436 (2) [back to overview]Change From Baseline up to 12 Hours Postdose in QT Interval Corrected for Heart Rate (QTc)
NCT01642485 (5) [back to overview]The QTcF Profile of Oral Moxifloxacin (400 mg) in Healthy Japanese Versus Caucasian Subjects
NCT01642485 (5) [back to overview]The Effect of Food (Fasted and Fed State) on the Degree of QT Prolongation Caused by Moxifloxacin
NCT01642485 (5) [back to overview]The Food Effects (Calorie Reduced FDA Breakfast and Carbohydrate Rich Continental Style) on QTcF
NCT01642485 (5) [back to overview]Moxifloxacin 400 mg (Single Dose) Compared to Placebo on the Mean QT/QTc Interval.
NCT01642485 (5) [back to overview]Insulin, Glucose and C-Peptide Effects on the QT/QTc Interval
NCT01658020 (6) [back to overview]Clinical Response in the Clinical Population
NCT01658020 (6) [back to overview]Clinical Cure Rate in the Microbiological Per Protocol(PP) Population
NCT01658020 (6) [back to overview]Change in EXACT-PRO Score
NCT01658020 (6) [back to overview]Change in CAT Scores
NCT01658020 (6) [back to overview]Microbiological Response Rate
NCT01658020 (6) [back to overview]Clinical Response in the Clinical Populations
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 12 Hours Post-Dose
NCT01743677 (21) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for CP-690,550
NCT01743677 (21) [back to overview]Maximum Observed Plasma Concentration (Cmax) of CP-690,550
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 0.25 Hour Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 0.5 Hour Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 1 Hour Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 16 Hours Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 24 Hours Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 4 Hours Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 8 Hours Post-Dose
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin Compared to Placebo
NCT01743677 (21) [back to overview]Plasma Decay Half-Life (t1/2) of CP-690,550
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcB Intervals Between CP-690,550 Compared to Placebo
NCT01743677 (21) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] for CP-690,550
NCT01743677 (21) [back to overview]Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 2 Hours Post-Dose
NCT01743677 (21) [back to overview]Plasma Decay Half-Life (t1/2) of CP-690,550 by CYP2C19 Genotype
NCT01743677 (21) [back to overview]Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of CP-690,550 by Cytochrome P450 2C19 (CYP2C19) Genotype
NCT01743677 (21) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) for CP-690,550
NCT01743677 (21) [back to overview]Maximum Observed Plasma Concentration (Cmax) of CP-690,550 by CYP2C19 Genotype
NCT01743677 (21) [back to overview]Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of CP-690,550 by CYP2C19 Genotype
NCT01743677 (21) [back to overview]Time to Reach Maximum Observed Plasma Concentration (Tmax) of CP-690,550 by CYP2C19 Genotype
NCT01746732 (8) [back to overview]PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Norelgestromin
NCT01746732 (8) [back to overview]PK: Time of Maximum Observed Drug Concentration (Tmax) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Minimum Observed Drug Concentration (Cmin) of Norelgestromin
NCT01746732 (8) [back to overview]PK: Minimum Observed Drug Concentration (Cmin) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Ethinyl Estradiol
NCT01746732 (8) [back to overview]PK: Maximum Concentration (Cmax) of Norelgestromin
NCT01746732 (8) [back to overview]PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Norelgestromin
NCT01785186 (3) [back to overview]Frequency of Adverse Events
NCT01785186 (3) [back to overview]Pharmacokinetics Including AUC, Cl, t1/2, Vd, and Protein Binding
NCT01785186 (3) [back to overview]Sputum Culture Conversion (2 Negative Cultures) Using Liquid Media
NCT01839279 (6) [back to overview]Maximum Plasma Concentration (Cmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.
NCT01839279 (6) [back to overview]Time to Reach Maximum Plasma Concentration (Tmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.
NCT01839279 (6) [back to overview]The Baseline-adjusted, Placebo-corrected (ΔΔQTc) on QTc Method Not Selected as Primary Endpoint.
NCT01839279 (6) [back to overview]Assessing the Relationship Between Changes in the QTc Interval and Plasma Levels of Tizanidine Using Concentration-effect Modeling
NCT01839279 (6) [back to overview]The Primary Endpoint Will be the Baseline-adjusted, Placebo-corrected Effect on QTc (ΔΔQTc) on Day 14.
NCT01839279 (6) [back to overview]Area Under the Plasma Concentration-time Curve During a Dosing Interval (AUCt) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.
NCT01854710 (7) [back to overview]Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo
NCT01854710 (7) [back to overview]QTc Versus Loxapine Concentration
NCT01854710 (7) [back to overview]Subjects With QTcI > 450 ms
NCT01854710 (7) [back to overview]Subjects With QTcI > 480 ms
NCT01854710 (7) [back to overview]Subjects With QTcI Increase > 30 ms From Baseline
NCT01854710 (7) [back to overview]Subjects With QTcI Increase > 60 ms From Baseline
NCT01854710 (7) [back to overview]Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)
NCT01859702 (1) [back to overview]Mean Aqueous Humor Concentration of Moxifloxacin
NCT01860703 (10) [back to overview]Tmax of Deferiprone and Deferiprone 3-O-glucuronide
NCT01860703 (10) [back to overview]T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01860703 (10) [back to overview]Maximum Postdose QT/QTc Interval
NCT01860703 (10) [back to overview]Maximum Change From Baseline (dQT/dQTc)
NCT01860703 (10) [back to overview]Cmax of Deferiprone and Deferiprone 3-O Glucuronide
NCT01860703 (10) [back to overview]AUC0-infinity for Serum Deferiprone and Deferiprone 3-O-glucuronide
NCT01860703 (10) [back to overview]Number of Participants With Adverse Events
NCT01860703 (10) [back to overview]Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of Moxifloxacin
NCT01860703 (10) [back to overview]Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 50 mg/kg Deferiprone
NCT01860703 (10) [back to overview]Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 33 mg/kg Deferiprone
NCT01928693 (6) [back to overview]Scarring
NCT01928693 (6) [back to overview]Complete Healing
NCT01928693 (6) [back to overview]Healing Rate
NCT01928693 (6) [back to overview]Number of Participants With Treatment Failure
NCT01928693 (6) [back to overview]Patient Pain Scores
NCT01928693 (6) [back to overview]Patient Satisfaction Scores
NCT01944774 (12) [back to overview]Subject Number for Microbiologically Cured and Failure at Visit 3 in b-mITT (Bacteriological mITT) Population
NCT01944774 (12) [back to overview]Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 3 in the mITT Population
NCT01944774 (12) [back to overview]Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 4 in the Clinically Evaluable (CE) Population
NCT01944774 (12) [back to overview]Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 4 in the mITT Population
NCT01944774 (12) [back to overview]Subject Number for Microbiologically Cured and Failure at Visit 3 in BE (Bacteriological Evaluable) Population
NCT01944774 (12) [back to overview]Subject Number for Microbiologically Cured and Failure at Visit 4 in b-mITT (Bacteriological mITT) Population
NCT01944774 (12) [back to overview]Subject Number of Success and Failure in Overall Efficacy at Visit 3 in b-mITT (Bacteriological mITT) Population
NCT01944774 (12) [back to overview]Subject Number for Microbiologically Cured and Failure at Visit 4 in BE (Bacteriological Evaluable) Population
NCT01944774 (12) [back to overview]Subject Number of Success and Failure in Overall Efficacy at Visit 3 in BE (Bacteriological Evaluable) Population
NCT01944774 (12) [back to overview]Subject Number of Success and Failure in Overall Efficacy at Visit 4 in b-mITT (Bacteriological mITT) Population
NCT01944774 (12) [back to overview]Subject Number of Success and Failure in Overall Efficacy at Visit 4 in BE (Bacteriological Evaluable) Population
NCT01944774 (12) [back to overview]Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 3 in the CE Population
NCT01965431 (4) [back to overview]Maximum Mean Placebo-corrected QTcN Change From Baseline Between 1 to 24 Hours on Day 1 for the Combination Therapy
NCT01965431 (4) [back to overview]Maximum Mean Placebo-corrected HR Change From Baseline Between 1 to 24 Hours on Day 1 for the Combination Therapy
NCT01965431 (4) [back to overview]Minimum Mean Placebo-corrected HR (Heart Rate) Change From Baseline Between 1 to 24 Hours on Day 1 for the Combination Therapy
NCT01965431 (4) [back to overview]Maximum Mean Placebo-corrected QTcN Change From Baseline Between 1 to 6 Hours on Day 1 for the Moxifloxacin Treatment
NCT01999114 (12) [back to overview]ECG Morphology
NCT01999114 (12) [back to overview]ECG Morphology
NCT01999114 (12) [back to overview]The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)
NCT01999114 (12) [back to overview]The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)
NCT01999114 (12) [back to overview]The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)
NCT01999114 (12) [back to overview]Heart Rate (HR)
NCT01999114 (12) [back to overview]Heart Rate (HR)
NCT01999114 (12) [back to overview]Heart Rate (HR)
NCT01999114 (12) [back to overview]QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval
NCT01999114 (12) [back to overview]QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval
NCT01999114 (12) [back to overview]QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval
NCT01999114 (12) [back to overview]ECG Morphology
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02056392 (10) [back to overview]Change From Baseline in QTcF
NCT02114684 (5) [back to overview]Sputum Culture Conversion Rates at Week 8 and Month 6 Post Tuberculosis Treatment Initiation
NCT02114684 (5) [back to overview]Number of Participants With Adverse Events and 8-week Culture Conversion Rates Among HIV-infected Patients vs. HIV-uninfected Patients
NCT02114684 (5) [back to overview]Time to Culture-conversion of the Moxifloxacin Regimen and the Ethambutol Regimen
NCT02114684 (5) [back to overview]Proportion of Patients With Unfavourable Outcomes or Tuberculosis Recurrence in the Moxifloxacin and Control Arm.
NCT02114684 (5) [back to overview]Proportion of Patients With Any Grade 3 or 4 Adverse Reactions in the Two Study Arms
NCT02176005 (8) [back to overview]Moxifloxacin Fecal Pharmacokinetics: Area Under the Free Moxifloxacin Fecal Concentration-time Curve Over the Period Time From Beginning of Treatment to 37 Days After the Beginning of Treatment (AUC D1-D37)
NCT02176005 (8) [back to overview]Moxifloxacin Plasma Pharmacokinetics: AUC(0-24h) of Moxifloxacin Plasma Concentrations Over Time on D1
NCT02176005 (8) [back to overview]Moxifloxacin Plasma Pharmacokinetics: AUC(0-24h) of Moxifloxacin Plasma Concentrations Over Time on D5
NCT02176005 (8) [back to overview]Moxifloxacin Plasma Pharmacokinetics: Cmax of Moxifloxacin in Plasma on D1
NCT02176005 (8) [back to overview]Percentage of Subjects With Adverse Events Related to Study Product
NCT02176005 (8) [back to overview]Number of Adverse Events (Including Abnormal Laboratory Findings) Related to Study Product
NCT02176005 (8) [back to overview]Moxifloxacin Plasma Pharmacokinetics: Cmax of Moxifloxacin in Plasma on D5
NCT02176005 (8) [back to overview]Moxifloxacin Fecal Pharmacokinetics: Area Under the Free Moxifloxacin Fecal Concentration-time Curve Over the Period Time From Beginning of Treatment to 16 Days After the Beginning of Treatment (AUC D1-D16)
NCT02193776 (2) [back to overview]Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System
NCT02193776 (2) [back to overview]Number of Participants With Treatment Emergent Adverse Events (TEAEs)
NCT02223702 (2) [back to overview]The Primary Outcome Variable Was Probing Depth.
NCT02223702 (2) [back to overview]The Attachment Loss Were Considered as a Secondary Measure.
NCT02283788 (1) [back to overview]QTcI - QT Interval Individually Corrected for Heart Rate - Day 5
NCT02308748 (2) [back to overview]Change in Placebo Corrected Change From Baseline QTc Interval on the ECG Measured in Milliseconds When Moxifloxacin is Administered With Diltiazem at the Evening Dose Compared to When Moxifloxacin is Administered Alone at Afternoon Dose on Treatment Day.
NCT02308748 (2) [back to overview]Change in Placebo Corrected Change From Baseline QTc and J-Tpeakc Intervals on the ECG Measured in Milliseconds When Dofetilide is Administered With Mexiletine or Lidocaine Compared to When Dofetilide is Administered Alone at Evening Dose on Treatment Day
NCT02409290 (5) [back to overview]Failure or Recurrence (FoR)
NCT02409290 (5) [back to overview]Favourable Outcome After Long-term Follow-up (132 Weeks)
NCT02409290 (5) [back to overview]Proportion of Patients With Acquired Drug Resistance
NCT02409290 (5) [back to overview]STREAM Stage 2 Primary Outcome Measure (the Proportion of Patients With a Favourable Outcome at Week 76)
NCT02409290 (5) [back to overview]Failure or Recurrence (FoR)
NCT02410772 (1) [back to overview]TB Disease-free Survival at 12M After Study Treatment Assignment Among Participants in Control Regimen, Regimen1 (2HRZE/4HR) to Experimental Regimens, Regimen3 (2HPZM/2HPM) and Regimen2 (2HPZ/2HP) (Assessable Population)
NCT02515045 (3) [back to overview]Change From Baseline (Preoperative Exam) in Pachymetry (Corneal Thickness)
NCT02515045 (3) [back to overview]Change From Baseline (Preoperative Exam) in Macular Thickness
NCT02515045 (3) [back to overview]Change From Baseline (Preoperative Exam) in Intraocular Pressure (IOP)
NCT02531438 (3) [back to overview]Number of Participants With Early Clinical Response
NCT02531438 (3) [back to overview]Number of Participants With the Indicated Investigator Assessment of Clinical Response in the ITT Population at the Post Therapy Evaluation (PTE) Visit
NCT02531438 (3) [back to overview]Number of Participants With the Indicated Investigator Assessment of Clinical Response in the Clinically Evaluable-Post Therapy Evaluation (CT-PTE) Population
NCT02559310 (1) [back to overview]Early Clinical Response (ECR)
NCT02661594 (1) [back to overview]Maximal Mean ΔΔQTcF
NCT02679573 (4) [back to overview]Microbiologic Response
NCT02679573 (4) [back to overview]Early Clinical Response Plus Improvement in Vital Signs and no Worsening of the 4 Symptoms
NCT02679573 (4) [back to overview]All-cause Mortality
NCT02679573 (4) [back to overview]Early Clinical Response
NCT02785770 (20) [back to overview]Number of Participants With Laboratory Test Abnormalities
NCT02785770 (20) [back to overview]Maximum Plasma Concentration (Cmax) of PF-04447943
NCT02785770 (20) [back to overview]Area Under the Plasma Concentration-Time Curve From Time Zero to Time of Last Measurable Concentration (AUClast) of PF-04447943
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in QRS Interval for PF-04447943 and Placebo
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Heart Rate for PF-04447943 and Placebo
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in PR Interval for PF-04447943 and Placebo
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for Moxifloxacin and Placebo
NCT02785770 (20) [back to overview]Number of Participants With Vital Sign Abnormalities
NCT02785770 (20) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (AEs) and Serious Adverse Events (SAEs)
NCT02785770 (20) [back to overview]Number of Participants With Electrocardiogram (ECG) Abnormalities
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 8 Hours Post-Dose
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 3 Hours Post-Dose
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 24 Hours Post-Dose
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 2 Hours Post-Dose
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 4 Hours Post-Dose
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 1 Hour Post-Dose
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 0.5 Hour Post-Dose
NCT02785770 (20) [back to overview]Time of Observed Maximum Plasma Concentration (Tmax) of PF-04447943
NCT02785770 (20) [back to overview]Number of Participants With Physical Examination Abnormalities
NCT02785770 (20) [back to overview]Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 12 Hours Post-Dose
NCT02787057 (4) [back to overview]Secondary Treatment Failure Rate
NCT02787057 (4) [back to overview]Primary Treatment Failure Rate
NCT02787057 (4) [back to overview]Primary Response Rate
NCT02787057 (4) [back to overview]Complete Cure Rate
NCT02800785 (8) [back to overview]Number of Participants With at Least One Complications From Treatment
NCT02800785 (8) [back to overview]Number of Clinic Visits or Emergency Room Visits
NCT02800785 (8) [back to overview]Total Number of Patients Who Had Resolution of Appendicitis Symptoms at 30 Days
NCT02800785 (8) [back to overview]Eventual Appendectomy Incidence Proportion
NCT02800785 (8) [back to overview]Rates of Participants With Appendiceal Cancer
NCT02800785 (8) [back to overview]Rate of Participants With Perforated Appendicitis
NCT02800785 (8) [back to overview]Patient-reported Quality of Life as Measured by EuroQol (EQ-5D)
NCT02800785 (8) [back to overview]Days in Hospital After Index Treatment Within 90 Days
NCT02903836 (2) [back to overview]Clinical Response in the Micro-ITT Population
NCT02903836 (2) [back to overview]Clinical Response in the ITT Population
NCT02980523 (7) [back to overview]Change From Baseline Bacterial Culture
NCT02980523 (7) [back to overview]Number of Cases of Conjunctival Hyperemia
NCT02980523 (7) [back to overview]Frequency of Corneal Epithelial Defects
NCT02980523 (7) [back to overview]Eyelid Edema Frequency
NCT02980523 (7) [back to overview]Chemosis Frequency
NCT02980523 (7) [back to overview]Cases Frequency of Ocular Secretion
NCT02980523 (7) [back to overview]Adverse Events
NCT03187301 (14) [back to overview]Number of Patients With Treatment-Emergent Adverse Events (TEAEs)
NCT03187301 (14) [back to overview]ECG Assessments: Mean Change From Baseline to Post-Baseline Value for Uncorrected QT Interval During Randomized Crossover Assessment Phase
NCT03187301 (14) [back to overview]ECG Assessments: Mean Change From Baseline to Post-Baseline Value for QRS Interval During Randomized Crossover Assessment Phase
NCT03187301 (14) [back to overview]Tmax of Apomorphine and Apomorphine Sulfate (Metabolite) Following the Administration of APL-130277
NCT03187301 (14) [back to overview]ECG Assessments: Mean Change From Baseline to Post-Baseline Value for QTcB Interval During Randomized Crossover Assessment Phase
NCT03187301 (14) [back to overview]Median Duration of 'ON' During the Dose Titration Phase
NCT03187301 (14) [back to overview]Mean Change From Pre-Dose to Post-Baseline Value in the Movement Disorders Society Unified Parkinson's Disease Rating Scale Part III Motor Examination (MDS-UPDRS Part III) Score During the Dose Titration Phase
NCT03187301 (14) [back to overview]AUClast of Apomorphine and Apomorphine Sulfate (Metabolite) Following the Administration of APL-130277
NCT03187301 (14) [back to overview]Cmax of Apomorphine and Apomorphine Sulfate (Metabolite) Following the Administration of APL-130277
NCT03187301 (14) [back to overview]ECG Assessments: Mean Change From Baseline to Post-Baseline Value for Heart Rate During Randomized Crossover Assessment Phase
NCT03187301 (14) [back to overview]ECG Assessments: Mean Change From Baseline to Post-Baseline Value for PR Interval During Randomized Crossover Assessment Phase
NCT03187301 (14) [back to overview]Time-Matched Change From Baseline in QTc, Placebo-Adjusted and Corrected for Heart Rate Based on QTcF Using ΔΔQTcF: Comparison Between Moxifloxacin and Placebo (Assay Sensitivity Analysis)
NCT03187301 (14) [back to overview]Time-Matched Change From Baseline in QTc, Placebo-Adjusted and Corrected for Heart Rate Based on the Fridericia Correction Method (QTcF) Using Delta Delta Method (ΔΔQTcF): Comparison Between APL-130277 and Placebo (Central Tendency Analysis)
NCT03187301 (14) [back to overview]Median Time to 'ON' During the Dose Titration Phase
NCT03338621 (2) [back to overview]Number of Participants With Culture Negative Status by 8 Weeks
NCT03338621 (2) [back to overview]Time to Culture Negative Status
NCT03465436 (8) [back to overview]Change From Time Matched Baseline in Mean Individually-Corrected QT (QTcI) Values of Lasmiditan and Moxifloxacin
NCT03465436 (8) [back to overview]Change From Baseline in Mean Heart Rate (HR) of Lasmiditan and Moxifloxacin
NCT03465436 (8) [back to overview]Change From Baseline in Mean Cardiac Intervals:QRS of Lasmiditan and Moxifloxacin
NCT03465436 (8) [back to overview]Number of Incidents in Electrocardiogram (ECG) Abnormalities in QTcF Interval Greater Than 450 Milliseconds
NCT03465436 (8) [back to overview]Pharmacokinetics (PK): Area Under the Concentration Time Curve (AUC-t) of Lasmiditan
NCT03465436 (8) [back to overview]Pharmacokinetics (PK): Maximum Concentration (Cmax) of Lasmiditan
NCT03465436 (8) [back to overview]Change From Baseline in Mean Cardiac Intervals: RR Interval of Lasmiditan and Moxifloxacin
NCT03465436 (8) [back to overview]Change From Time Matched Baseline in Mean Fridericia-Corrected QT (QTcF) Values of Lasmiditan and Moxifloxacin
NCT03510663 (1) [back to overview]Time-matched Difference Between the OPC-61815/Moxifloxacin and Placebo Data in Change From Baseline for QTcF in 12-lead Holter Electrocardiogram (ECG)
NCT03577275 (5) [back to overview]Change From Baseline in PR Interval (PR)
NCT03577275 (5) [back to overview]Change From Baseline in QRS Interval (QRS)
NCT03577275 (5) [back to overview]Change From Baseline in Fridericia's Correction for QT Interval (QTcF)
NCT03577275 (5) [back to overview]Change From Baseline in Fridericia's Correction for QT Interval (QTcF)
NCT03577275 (5) [back to overview]Change From Baseline in Heart Rate (HR)
NCT03613649 (36) [back to overview]Changes From Baseline in ECG Measures: Ventricular Rate
NCT03613649 (36) [back to overview]Changes From Baseline in ECG Measures: PR Interval, QRS Duration, QT Interval, QTcF Interval and RR Interval
NCT03613649 (36) [back to overview]Changes From Baseline for Blood Pressure - Diastolic
NCT03613649 (36) [back to overview]Time-matched, Placebo-corrected, Baseline-adjusted, the Time From the Onset of the P Wave to the Start of the QRS Complex (PR Interval) Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]Time-matched, Placebo-corrected, Baseline-adjusted QRS Duration Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]Number of Participants With Treatment-emergent Adverse Events Following Administration of Study Product
NCT03613649 (36) [back to overview]Maximum Observed Concentration (Cmax) of Zoliflodacin
NCT03613649 (36) [back to overview]Elimination Rate Constant (Ke) of Zoliflodacin
NCT03613649 (36) [back to overview]Area Under the Concentration Time-curve From Time Zero to the Last Concentration Above the Lower Limit of Quantitation (AUC(0-last)) for Zoliflodacin
NCT03613649 (36) [back to overview]Time-matched, Placebo-corrected, Baseline-adjusted the Time Elapsed Between Two Successive R Waves of the QRS (RR Interval) Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]Area Under the Concentration Time-curve From Time Zero to Infinity (AUC(0 - Infinity)) for Zoliflodacin
NCT03613649 (36) [back to overview]Apparent Volume of Distribution (Vz/F) of Zoliflodacin
NCT03613649 (36) [back to overview]Apparent Oral Clearance (CL/F) of Zoliflodacin
NCT03613649 (36) [back to overview]Changes From Baseline for Temperature
NCT03613649 (36) [back to overview]Changes From Baseline for Blood Pressure - Systolic
NCT03613649 (36) [back to overview]Changes From Baseline for Glomerular Filtration Rate (GFR) - Estimated
NCT03613649 (36) [back to overview]Changes From Baseline for Hematocrit
NCT03613649 (36) [back to overview]Changes From Baseline for Hemoglobin
NCT03613649 (36) [back to overview]Changes From Baseline for Magnesium, Glucose (Fasting), Blood Urea Nitrogen (BUN), Creatinine, Total Bilirubin, Direct Bilirubin
NCT03613649 (36) [back to overview]Changes From Baseline for Platelets
NCT03613649 (36) [back to overview]Changes From Baseline for Pulse Rate
NCT03613649 (36) [back to overview]Changes From Baseline for Respiratory Rate
NCT03613649 (36) [back to overview]Changes From Baseline for Erythrocytes
NCT03613649 (36) [back to overview]Changes From Baseline for Total Protein and Albumin
NCT03613649 (36) [back to overview]Incidence of Abnormal T-wave Morphology Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]Occurrence of Urinalysis Adverse Events Following Administration of Study Product
NCT03613649 (36) [back to overview]The One-sided 95% Confidence Interval (CI) for the Largest Time-matched, Placebo-corrected, Baseline-adjusted Mean QTcF Interval (Delta Delta QTcF) Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]The One-sided 95% Confidence Interval (CI) of the Time-matched, Placebo-corrected, Baseline-adjusted Mean QTcF Interval (Delta Delta QTcF) After a Single Dose of Moxifloxacin
NCT03613649 (36) [back to overview]Number of Participants With Treatment-emergent Serious Adverse Events Following Administration of Zoliflodacin and Moxifloxacin
NCT03613649 (36) [back to overview]Time-matched, Placebo-corrected, Baseline-adjusted Heart Rate (HR) Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]Changes From Baseline for White Blood Cells With Differentials
NCT03613649 (36) [back to overview]Changes From Baseline for Sodium, Potassium, Chloride and Bicarbonate
NCT03613649 (36) [back to overview]Relationship Between Plasma Concentrations of Zoliflodacin and Time-matched, Placebo-corrected, Baseline-adjusted Mean QTcF Interval (Delta Delta QTcF) Following Administration of Zoliflodacin
NCT03613649 (36) [back to overview]Terminal Elimination Half-life (t1/2) of Zoliflodacin
NCT03613649 (36) [back to overview]Time of Maximum Observed Concentration (Tmax) of Zoliflodacin
NCT03613649 (36) [back to overview]Changes From Baseline for Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT) and Alkaline Phosphatase (AP)
NCT03657264 (3) [back to overview]Predicted Value of ∆∆QTc at Cmax
NCT03657264 (3) [back to overview]Change-from-baseline Mean Effect of Moxifloxacin on QT Interval Expressed as QTc According to Fridericia's Formula (∆QTcF)
NCT03657264 (3) [back to overview]Change-from-baseline Mean Effect of P03277 on QT Interval Expressed as QTc According to Fridericia's Formula (∆QTcF)
NCT03808298 (29) [back to overview]Number of Categorical Outliers for PR
NCT03808298 (29) [back to overview]Tmax of M2 Metabolite
NCT03808298 (29) [back to overview]Tmax of Balovaptan
NCT03808298 (29) [back to overview]Tmax M3 Metabolite
NCT03808298 (29) [back to overview]Number of Treatment Emergent Changes of T-Wave Morphology
NCT03808298 (29) [back to overview]Number of Categorical Outliers for QTcF
NCT03808298 (29) [back to overview]Number of Categorical Outliers for HR
NCT03808298 (29) [back to overview]Cmax of M2 Metabolite
NCT03808298 (29) [back to overview]Cmax of Balovaptan
NCT03808298 (29) [back to overview]Change-From-Baseline QTcF Measured on 12 Lead ECGs Extracted From Continuous Records
NCT03808298 (29) [back to overview]Change-From-Baseline QTcF at Dose Level B Measured on 12-Lead ECGs Extracted From Continuous Recordings
NCT03808298 (29) [back to overview]Change-From-Baseline QTcF at Dose Level B Measured on 12-Lead ECGs Extracted From Continuous Recordings
NCT03808298 (29) [back to overview]Change-From-Baseline QRS Interval Measured on 12-Lead ECGs Extracted From Continuous Recordings
NCT03808298 (29) [back to overview]Change-From-Baseline QTcF of Balovaptan at Dose Level A Measurred on 12-Lead ECGs Extracted From Continuous Recordings
NCT03808298 (29) [back to overview]Change-From-Baseline PR Interval Measured on 12-Lead ECGs Extracted From Continuous Recordings
NCT03808298 (29) [back to overview]Change-From-Baseline Heart Rate Measured on 12-Lead ECGs Extracted From Continuous Recordings
NCT03808298 (29) [back to overview]AUC0-24 of M3 Metabolite
NCT03808298 (29) [back to overview]AUC0-24 of M2 Metabolite
NCT03808298 (29) [back to overview]AUC0-24 of Balovaptan
NCT03808298 (29) [back to overview]Tmax of Moxifloxacin
NCT03808298 (29) [back to overview]Predicted ΔΔQTcF Interval at Geometric Mean Peak Concentrations at Tmax of M2 From Concentration-QTc Analysis
NCT03808298 (29) [back to overview]Predicted ΔΔQTcF Interval at Geometric Mean Peak Concentrations at Tmax of Balovaptan From Concentration-QTc Analysis
NCT03808298 (29) [back to overview]Predicted ΔΔQTcF Interval at Geometric Mean Peak Concentration for M3 From Concentration-QTc Analysis
NCT03808298 (29) [back to overview]Percentage of Participants With Treatment Emergent Adverse Events
NCT03808298 (29) [back to overview]Number of Treatment Emergent Changes of U-Wave Presence
NCT03808298 (29) [back to overview]Cmax of Moxifloxacin
NCT03808298 (29) [back to overview]Number of Categorical Outliers for QRS
NCT03808298 (29) [back to overview]Cmax of M3 Metabolite
NCT03808298 (29) [back to overview]AUC0-24 of Moxifloxacin
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline for PR Interval on Day 8
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline for QRS Interval on Day 1
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline for QRS Interval on Day 8
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline in Heart Rate (HR) Interval on Day 1
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline in Heart Rate (HR) Interval on Day 8
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline in QTcF After a Single Dose of Moxifloxacin on Day 8
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline in QTcF on Day 8 for Padsevonil
NCT04126343 (19) [back to overview]Time of Observed Maximum Concentration (Tmax) at Steady State for Padsevonil
NCT04126343 (19) [back to overview]Percentage of Participants With Treatment Related Adverse Events From Baseline to Safety Follow-up (up to Day 67)
NCT04126343 (19) [back to overview]Percentage of Participants With Serious Adverse Events From Baseline to Safety Follow-up (up to Day 67)
NCT04126343 (19) [back to overview]Percentage of Participants With Adverse Events Leading to Discontinuation of the Study From Baseline to Safety Follow-up (up to Day 67)
NCT04126343 (19) [back to overview]Percentage of Participants With Adverse Events From Baseline to Safety Follow-up (up to Day 67)
NCT04126343 (19) [back to overview]Maximum Observed Plasma Concentration at Steady State (Cmax, ss) for Padsevonil
NCT04126343 (19) [back to overview]Change From Baseline in QTcF Evaluated at Drug-specific Tmax for Padsevonil
NCT04126343 (19) [back to overview]Change From Baseline in QTcF Evaluated at Drug-Specific Tmax for Metabolite 2
NCT04126343 (19) [back to overview]Change From Baseline in QTcF Evaluated at Drug-specific Tmax for Metabolite 1
NCT04126343 (19) [back to overview]Area Under the Plasma Concentration Time Curve (AUCtau) at Steady State for Padsevonil
NCT04126343 (19) [back to overview]Number of Participants With Treatment-emergent Changes for T-wave Morphology and U-wave Presence
NCT04126343 (19) [back to overview]Placebo-corrected Change From Baseline for PR Interval on Day 1
NCT04175808 (25) [back to overview]Change From Baseline in QRS After Each Treatment In Part 2
NCT04175808 (25) [back to overview]Change From Baseline in QRS After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Change From Baseline in QTcF After Each Treatment In Part 2
NCT04175808 (25) [back to overview]Change From Baseline in QTcF After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Number of Participants With Clinically Significant Abnormalities in Vital Signs, Laboratory Tests, or Electrocardiogram Findings
NCT04175808 (25) [back to overview]Number of Participants With Recorded Outlier Values for QTcF, HR, PR, and QRS After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Based on the Fridericia Method (QTcF) After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Placebo-corrected Change From Baseline in QRS After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Maximum Observed Plasma Concentration (Cmax) of Omecamtiv Mecarbil in Part B
NCT04175808 (25) [back to overview]Apparent Total Plasma Clearance (CL/F) for Omecamtiv Mecarbil in Part B
NCT04175808 (25) [back to overview]Apparent Volume of Distribution (VZ/F) for Omecamtiv Mecarbil in Part B
NCT04175808 (25) [back to overview]Area Under the Concentration-time Curve From Time 0 to the Time of Last Quantifiable Concentration (AUC0-t) for Omecamtiv Mecarbil in Part B
NCT04175808 (25) [back to overview]AUC From Time 0 to Infinity (AUCinf) for Omecamtiv Mecarbil in Part B
NCT04175808 (25) [back to overview]Slope of Omecamtiv Mecarbil Plasma Concentration Estimated From Concentration-QTc Analysis in Part B
NCT04175808 (25) [back to overview]Time to Maximum Observed Plasma Concentration (Tmax) of Omecamtiv Mecarbil In Part B
NCT04175808 (25) [back to overview]Change From Baseline in Heart Rate After Each Treatment In Part 2
NCT04175808 (25) [back to overview]Change From Baseline in Heart Rate After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Change From Baseline in PR Interval After Each Treatment In Part 2
NCT04175808 (25) [back to overview]Apparent Terminal Elimination Half-life (T1/2) of Omecamtiv Mecarbil in Part B
NCT04175808 (25) [back to overview]Change From Baseline in PR Interval After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Number of Participants With Treatment-emergent Adverse Events (TEAEs)
NCT04175808 (25) [back to overview]Number of Participants With Treatment-emergent Changes in T-wave Morphology and U-wave Presence After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Placebo-corrected Change From Baseline in Heart Rate After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Placebo-corrected Change From Baseline in PR Interval After Omecamtiv Mecarbil Dosing in Part B
NCT04175808 (25) [back to overview]Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Based on the Fridericia Method (QTcF) After Moxifloxacin Dosing in Part B
NCT04560816 (14) [back to overview]ALXN1840 PK Parameter: Area Under The Concentration Versus Time Curve From Time 0 To The Last Quantifiable Concentration (AUC0-t) Of Total Molybdenum And Plasma Ultrafiltrate (PUF) Molybdenum Following a Single Oral Dose of ALXN1840
NCT04560816 (14) [back to overview]ALXN1840 PK Parameter: Maximum Observed Concentration (Cmax) Of Total Molybdenum And PUF Molybdenum Following a Single Oral Dose of ALXN1840
NCT04560816 (14) [back to overview]ALXN1840 PK Parameter: Time To Maximum Observed Concentration (Tmax) Of Total Molybdenum And PUF Molybdenum Following a Single Oral Dose of ALXN1840
NCT04560816 (14) [back to overview]Change From Baseline For Heart Rate (ΔHR)
NCT04560816 (14) [back to overview]Change From Baseline PR Interval (ΔPR)
NCT04560816 (14) [back to overview]Change From Baseline QRS Interval (ΔQRS)
NCT04560816 (14) [back to overview]Change From Baseline QT Interval Using Fridericia's Formula (ΔQTcF)
NCT04560816 (14) [back to overview]Number of Participants With Treatment-Emergent Adverse Events (TEAEs)
NCT04560816 (14) [back to overview]Number of Participants With Treatment-emergent T-wave Morphology Abnormalities and U-waves
NCT04560816 (14) [back to overview]Placebo-corrected Change From Baseline For QTcF (ΔΔQTcF) for ALXN1840 Using The By-time Point Analysis
NCT04560816 (14) [back to overview]Placebo-corrected Change From Baseline Heart Rate (ΔΔHR)
NCT04560816 (14) [back to overview]Placebo-corrected Change From Baseline PR Interval (ΔΔPR)
NCT04560816 (14) [back to overview]Placebo-corrected Change From Baseline QRS Interval (ΔΔQRS)
NCT04560816 (14) [back to overview]ΔΔQTcF For Moxifloxacin Using The By-time Point Analysis
NCT04563845 (89) [back to overview]Part 1: Area Under the Plasma Concentration-time Curve From Time Zero to Time t (AUC[0-t]) of GSK3640254
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Chemistry Parameters: Albumin, Globulin, and Total Protein
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Vital Parameters: Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Vital Parameter: Temperature
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Vital Parameter: Pulse Rate
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Urinalysis Parameter: Specific Gravity
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Urinalysis Parameter: Specific Gravity
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Urinalysis Parameter: pH
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in QTcF - For Placebo and Moxifloxacin Arm
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in QT Interval Corrected for Heart Rate Using Fridericia's Formula (QTcF) - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Urinalysis Parameter: Potential of Hydrogen (pH)
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Hematology Parameter: Hemoglobin
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Hematology Parameter: Hematocrit
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Volume
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Hematology Parameter: Erythrocytes
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, and Blood Urea Nitrogen
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Chemistry Parameters: Creatinine, Urate, Total Bilirubin, and Direct Bilirubin
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Chemistry Parameters: Amylase and Lipase
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in QRS Interval - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in PR Interval - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Hematology Parameter: Hemoglobin
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Hematology Parameter: Hematocrit
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Hematology Parameter: Erythrocytes
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Heart Rate (HR) - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, Blood Urea Nitrogen
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Chemistry Parameters: Creatinine, Urate, Total Bilirubin, Direct Bilirubin
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Chemistry Parameters: Albumin, Globulin, and Total Protein
NCT04563845 (89) [back to overview]Part 2: Plasma Concentration of GSK3640254
NCT04563845 (89) [back to overview]Part 1: Absolute Values for Chemistry Parameters: Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Gamma-glutamyl Transferase (GGT), Creatine Kinase, and Lactate Dehydrogenase
NCT04563845 (89) [back to overview]Part 2: Tmax of Moxifloxacin 400 mg
NCT04563845 (89) [back to overview]Part 2: Tmax of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Using Fridericia's Formula (QTcF) Following Administration of GSK3640254 100 mg and GSK3640254 500 mg Using Concentration-QTc (C-QTc) Analysis
NCT04563845 (89) [back to overview]Part 2: Ctau of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: Cmax of Moxifloxacin 400 mg
NCT04563845 (89) [back to overview]Part 2: Cmax of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: AUC(0-tau) of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: AUC(0-t) of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 1: Time of Maximum Observed Concentration (Tmax) of GSK3640254
NCT04563845 (89) [back to overview]Part 1: Plasma Concentration at the End of the Dosing Interval (Ctau) of GSK3640254
NCT04563845 (89) [back to overview]Part 1: Maximum Observed Concentration (Cmax) of GSK3640254
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Chemistry Parameters: Amylase, Lipase
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Chemistry Parameters: ALT, ALP, AST, GGT, Creatine Kinase, Lactate Dehydrogenase
NCT04563845 (89) [back to overview]Part 2: Change From Baseline in Chemistry Parameters: Albumin, Globulin, Total Protein
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Vital Parameters: SBP and DBP
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Vital Parameter: Temperature
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Vital Parameter: Pulse Rate
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Urinalysis Parameter: Specific Gravity
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Urinalysis Parameter: pH
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Hematology Parameter: Hemoglobin
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Hematology Parameter: Hematocrit
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Volume
NCT04563845 (89) [back to overview]Part 2: Placebo-corrected Change From Baseline in QTcF Following Administration of Moxifloxacin
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Hematology Parameter: Erythrocytes
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, Blood Urea Nitrogen
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Chemistry Parameters: Creatinine, Urate, Total Bilirubin, Direct Bilirubin
NCT04563845 (89) [back to overview]Part 1: AUC From Time Zero to the End of the Dosing Interval at Steady State (AUC[0-tau]) of GSK3640254
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Chemistry Parameters: Amylase and Lipase
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Chemistry Parameters: ALT, ALP, AST, GGT, Creatine Kinase, Lactate Dehydrogenase
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Chemistry Parameters: Albumin, Globulin, Total Protein
NCT04563845 (89) [back to overview]Part 1: Plasma Concentration of GSK3640254
NCT04563845 (89) [back to overview]Part 1: Number of Participants With Serious Adverse Events (SAEs) and Non-SAEs
NCT04563845 (89) [back to overview]Part 1: Number of Participants With Clinically Significant Abnormal 12-Lead Electrocardiogram (ECG) Findings
NCT04563845 (89) [back to overview]Part 2: Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Using Fridericia's Formula (QTcF) Following Administration of GSK3640254 100 mg and GSK3640254 500 mg By-time Point Analysis
NCT04563845 (89) [back to overview]Part 2: Placebo-corrected Change From Baseline in QRS Following Administration of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: Placebo-corrected Change From Baseline in PR Following Administration of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: Placebo-corrected Change From Baseline in HR Following Administration of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 2: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Urinalysis Parameter: Specific Gravity
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Urinalysis Parameter: pH
NCT04563845 (89) [back to overview]Part 2: Number of Participants With Treatment Emergent Changes of T-wave Morphology and Presence of U-wave Following Administration of GSK3640254 100 mg and GSK3640254 500 mg
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, Blood Urea Nitrogen
NCT04563845 (89) [back to overview]Part 2: Number of Participants With Non-SAEs and SAEs
NCT04563845 (89) [back to overview]Part 2: Number of Participants With Clinically Significant Abnormal 12-Lead ECG Findings
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Chemistry Parameters: Creatinine, Urate, Total Bilirubin, Direct Bilirubin
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Hematology Parameter: Hemoglobin
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Hematology Parameter: Hematocrit
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Hematology Parameter: Erythrocytes
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Chemistry Parameters: Amylase and Lipase
NCT04563845 (89) [back to overview]Part 1: Change From Baseline in Chemistry Parameters: ALT, ALP, AST, GGT, Creatine Kinase, Lactate Dehydrogenase
NCT04563845 (89) [back to overview]Part 2: Number of Participants With Outlier Results for HR, QTcF, ΔQTcF, PR Interval and QRS Interval for GSK3640254 100 mg and GSK3640254 500 mg

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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Plasma Concentration for Contraceptives

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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Proportion of Patients With Sterile Sputum Cultures

Proportion of patients with sterile sputum cultures (NCT00082173)
Timeframe: 8 weeks

InterventionParticipants (Number)
Experimental Arm59
Control Arm45

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Proportion of Patients With Grade 3 or 4 Adverse Reactions Attributable to Study Medications

Proportion of patients with Grade 3 or 4 adverse reactions attributable to study medications (NCT00082173)
Timeframe: 8 weeks

InterventionParticipants (Number)
Experimental Arm0
Control Arm0

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Changes in Waist-to-Hip Ratio Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

Waist-to-hip ratio is assessed through calculated ratio of waist and hip circumference. (NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionratio (Mean)
Baseline Waist-Hip Ratio6 months Waist-Hip Ratio
Lean Women0.730.73
Obese Women0.790.81

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Inflammatory Marker Changes, High Sensitive C-reactive Protein (Hs-CRP) and Adiponectin, Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

Inflammatory markers are assessed through blood analysis for C-reactive protein (hs-CRP) and adiponectin. (NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionng/mL (Mean)
Baseline Hs-CRP6 months Hs-CRPBaseline Adiponectin6 months Adiponectin
Lean Women2050.772266.0221976.5322221.36
Obese Women4908.766207.7617568.8618408.43

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Inflammatory Marker Changes (MCP-1) Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

Inflammatory marker is assessed through blood analysis for Monocyte chemotactic protein-1 (MCP-1). (NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionpg/mL (Mean)
Baseline MCP-16 months MCP-1
Lean Women156.14206.66
Obese Women209.56219.86

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Changes in Waist Circumference Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

(NCT00205504)
Timeframe: Baseline and 6 months

,
Interventioncm (Mean)
Baseline Waist circumference6 months Waist circumference
Lean Women70.270.9
Obese Women100.0101.0

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Changes in Lipid Profile Compared Associated With OC Use Among (1) Obese Women and (2) Lean Women

The lipid profile is assessed through blood sample analysis for low-density lipoprotein (LDL), Triglycerides and high-density lipoprotein (HDL). (NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionmg/dL (Mean)
Baseline LDL6 months LDLBaseline Triglycerides6 months TriglyceridesBaseline HDL6 months HDL
Lean Women84104721065361
Obese Women9511372835158

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Changes in Insulin Sensitivity Associated With Oral Contraceptive (OC) Use Compared Among (1) Obese Women and (2) Lean Women

Insulin sensitivity was assessed by frequent sampling intravenous glucose tolerance test (FSIVGTT). (NCT00205504)
Timeframe: Baseline and 6 months

,
InterventionmIU/L (Mean)
Baseline Insulin sensitivity6 months Insulin sensitivity
Lean Women6.628.23
Obese Women4.363.82

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Changes in Estrogen Metabolites (Plasma) Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

(NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionpg/mL (Mean)
Baseline 16aE16 months 16aE1Baseline 2ME16 months 2ME1Baseline 4ME16 months 4ME1Baseline 2ME26 months 2ME2Baseline E16 months E1Baseline 4ME26 months 4ME2Baseline E26 months E2Baseline 2OHE16 months 2OHE1Baseline 2OHE26 months 2OHE2Baseline 4OHE16 months 4OHE1Baseline Total plasma6 months Total plasma
Lean Women317.47383.3932.3945.584.457.420.911.74245.99227.40.591.1436.79647.3285.6257.968.016.0533.9829.121022.161007.89
Obese Women314.76421.625.9252.845.266.11.481.5217.23315.030.730.8934.1174.73101.07135.959.8111.5533.7827.2910681342.21

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Changes in Blood Pressure Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

(NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionmm Hg (Mean)
Baseline Systolic Blood Pressure6 months Systolic Blood PressureBaseline Diastolic Blood Pressure6 months Diastolic Blood Pressure
Lean Women105.7106.568.066.5
Obese Women121.1123.574.473.4

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Changes in Body Mass Index (BMI) Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

Body Mass Index is a calculation of height and weight: kg/m² (NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionkg/m² (Mean)
Baseline BMI6 months BMI
Lean Women21.321.4
Obese Women37.137.6

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Inflammatory Marker Changes, Soluble Vascular Cell Adhesion Molecule (sVCAM) and Soluble Intercellular Adhesion Molecule (sICAM), Associated With OC Use Compared Among (1) Obese Women and (2) Lean Women

These inflammatory markers are assessed through blood analysis of Soluble Vascular Cell Adhesion Molecule (sVCAM) and soluble intercellular adhesion molecule (sICAM). (NCT00205504)
Timeframe: Baseline and 6 months

,
Interventionng/mL (Mean)
Baseline sVCAM6 months sVCAMBaseline sICAM6 months sICAM
Lean Women1139.61003.29182.11160.21
Obese Women905880.14163.34163.2

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Percentage of Bacteriologic Response at Test of Cure Visit

Bacteriogical response assessed on per pathogen basis for Bacteriologic Per Protcol (BPP) set at TOC Visit. If no repeat culture, response is presumed from sponsor assessment of clinical response. Eradication =# of pathogens eradicated at TOC/N; Persistence =# of pathogens persistent at TOC/N; N=# of unique pathogens identified at baseline (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

,
InterventionPercent (Number)
EradicationPersistence
Azithromycin964
Moxifloxacin96.73.3

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Percentage of Clinical Cure (Success) at Test of Cure Visit (Full Analysis Set)

Clinical response (Cure vs Failure) at the TOC visit for the Full Analysis Set (FAS), Cure=Signs&symptoms(S&S) of infection return to normal baseline level or clin improvement requiring no other antibiotics(AB); Failure=other AB due to S&S of acute infection persisted/worsened,new clinical S&S of acute infection,or clinical/radiological evidence of pneumonia developed during treatment; percent = # of cure or failure/total # of sub (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

,
InterventionPercent (Number)
CureFailure
Azithromycin88.411.6
Moxifloxacin90.99.1

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Percentage of Clinical Cure (Success) at Test of Cure Visit(Clinical Per Protocol Population)

Cure=Signs&symptoms(S&S) of infection return to normal baseline level or clin improvement requiring no other antibiotics(AB); Failure=other AB due to S&S of acute infection persisted/worsened,new clinical S&S of acute infection,or clinical/radiological evidence of pneumonia developed during treatment; percent = # of cure or failure/total # of sub (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

,
Interventionpercent (Number)
CureFailure
Azithromycin93.07.0
Moxifloxacin94.25.8

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Percentage of Clinical Cure (Success)at Test of Cure Visit(Clinically Eligible Set)

Clinical Response at TOC Visit for clinically Eligible Subjects, Cure=Signs&symptoms(S&S) of infection return to normal baseline level or clin improvement requiring no other antibiotics(AB); Failure=other AB due to S&S of acute infection persisted/worsened,new clinical S&S of acute infection,or clinical/radiological evidence of pneumonia developed during treatment; percent = # of cure or failure/total # of sub (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

,
InterventionPercent (Number)
CureFailure
Azithromycin88.411.6
Moxifloxacin90.99.1

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Change From Baseline in Clinical COPD Questionnaire(CCQ)Functional State Score

1 of 3 domains that combined into the CCQ Total score. Items 7,8,9, and 10 address functional state. Subject record their experiences during last 24 hrs. 7 pt scale - 0=asymptomatic and 6=extremely; change=mean score at observation minus mean score at baseline (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

InterventionScore on Scale (Least Squares Mean)
Azithromycin-0.61
Moxifloxacin-0.52

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Change From Baseline in Clinical COPD Questionnaire(CCQ)Symptoms Score

1 of 3 domains that combined into the CCQ Total score. Items 1,2,5,and 6 address symptoms. Subject record their experiences during last 24 hrs. 7 pt scale - 0=asymptomatic and 6=extremely symptomatic; change=mean score at observation minus mean score at baseline (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

InterventionScore on Scale (Least Squares Mean)
Azithromycin-0.99
Moxifloxacin-0.96

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Change From Baseline in Clinical COPD Questionnaire(CCQ)Total Score

CCQ was developed to measure health status of Chronic obstructive pulmonary disease (COPD) subjects. 10 items divided into 3 domains: symtoms, functional state, and mental state. Subject record their experiences during last 24 hrs. 7 pt scale - 0=asymptomatic and 6=extremely symptomatic/totally limited; change=mean score at observation minus mean score at baseline (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

InterventionScore on Scale (Least Squares Mean)
Azithromycin-0.76
Moxifloxacin-0.71

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Time Taken for First Quartile (25%) of Subjects to Have AECB Recurrence

Subject is considered to have AECB recurrence if they had a clinical response of cure at the TOC visit and then met the definition of AECB during the follow-up period. (NCT00254566)
Timeframe: Number of Days

InterventionDays (Number)
Azithromycin152
Moxifloxacin204

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Change From Baseline in Clinical COPD Questionnaire(CCQ)Mental State Score

1 of 3 domains that combined into the CCQ Total score. Items 3 and 4 address mental state. Subject record their experiences during last 24 hrs. 7 pt scale - 0=asymptomatic and 6=extremely; change=mean score at observation minus mean score at baseline (NCT00254566)
Timeframe: Test of Cure (TOC) Visit (Day 12-19)

InterventionScore on Scale (Least Squares Mean)
Azithromycin-0.60
Moxifloxacin-0.54

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 17 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 13:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 13:00h, Day 43 13:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.35
Placebo Patch2.59

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 16 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 12:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 12:00h, Day 43 12:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch2.21
Placebo Patch1.99

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 15 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 11:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 11:00h, Day 43 11:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.15
Placebo Patch1.60

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 14 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 10:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 10:00h, Day 43 10:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.83
Placebo Patch2.12

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 13 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 9:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 9:00h, Day 43 9:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch0.83
Placebo Patch1.40

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 11 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 7:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 7:00h, Day 43 7:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.94
Placebo Patch0.30

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 10 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 6:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 6:00h, Day 43 6:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch0.92
Placebo Patch0.58

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 1 Hour After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 21:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 21:00h, Day 42 21:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.82
Placebo Patch1.67

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 18 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 14:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 14:00h, Day 43 14:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.31
Placebo Patch1.29

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 7 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 3:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 3:00h, Day 43 3:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.63
Placebo Patch-0.26

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 6 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 2:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 2:00h, Day 43 2:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.62
Placebo Patch0.05

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 5 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 1:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 1:00h, Day 43 1:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.17
Placebo Patch0.03

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 4 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 00:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 00:00h, Day 43 00:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch0.54
Placebo Patch0.83

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 3 Hours After Patch Application on Day 42(Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 23:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 23:00h, Day 42 23:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.02
Placebo Patch0.89

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 12 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 8:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 8:00h, Day 43 8:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.16
Placebo Patch1.31

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 24 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 20:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 20:00h, Day 43 20:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.96
Placebo Patch-0.58

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 23 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 19:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 19:00h, Day 43 19:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.50
Placebo Patch0.64

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 22 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 18:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 18:00h, Day 43 18:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.45
Placebo Patch0.27

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 21 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 17:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 17:00h, Day 43 17:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.13
Placebo Patch0.57

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 20 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 16:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 16:00h, Day 43 16:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch1.58
Placebo Patch1.90

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 2 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 22:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 22:00h, Day 42 22:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch2.55
Placebo Patch1.78

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI at Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 10:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 10:00h, Day 32/ Day 39 10:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion2.21
Placebo Infusion0.82

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 9 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 19:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 19:00h, Day 32/ Day 39 19:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion7.33
Placebo Infusion-0.25

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 8 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 18:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 18:00h, Day 32/ Day 39 18:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion7.74
Placebo Infusion0.22

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 7 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 17:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 17:00h, Day 32/ Day 39 17:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion8.97
Placebo Infusion0.37

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 6 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 16:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 16:00h, Day 32/ Day 39 16:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion9.98
Placebo Infusion1.10

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 5 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 15:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 15:00h, Day 32/ Day 39 15:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion10.06
Placebo Infusion0.08

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 4 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 14:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 14:00h, Day 32/ Day 39 14:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion9.48
Placebo Infusion1.28

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 3 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 13:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 13:00h, Day 32/ Day 39 13:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion12.68
Placebo Infusion1.44

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 2 Hours Before Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 8:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 8:00h, Day 32/ Day 39 8:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion1.70
Placebo Infusion1.29

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 2 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 12:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 12:00h, Day 32/ Day 39 12:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion12.44
Placebo Infusion1.42

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 10 Hours After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 20:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 20:00h, Day 32/ Day 39 20:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion6.34
Placebo Infusion0.14

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 19 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 15:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 15:00h, Day 43 15:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch0.71
Placebo Patch1.51

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 1 Hour Before Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 9:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 9:00h, Day 32/ Day 39 9:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion1.84
Placebo Infusion1.36

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTcI 1 Hour After Start of Infusion on Day 32 or Day 39 (Positive Control) and Respective Day 39 or Day 32 (Corresponding Placebo) (Cross-over Comparison)

Change in QTcI was analyzed by a cross-over comparison between moxifloxacin infusion and placebo infusion. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 11:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 11:00h, Day 32/ Day 39 11:00h

Interventionmilliseconds [ms] (Mean)
Moxifloxacin Infusion17.19
Placebo Infusion3.70

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI at Time of Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 20:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 20:00h, Day 42 20:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch0.46
Placebo Patch1.13

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 9 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 5:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 5:00h, Day 43 5:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.39
Placebo Patch-1.97

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Time-matched Change From Baseline (Average of Day -2 and Day -1) in QTc Based on the QTcI 8 Hours After Patch Application on Day 42 (Rotigotine Dose of 54 mg/Day) (Parallel-group Comparison)

Change in QTcI was analyzed by a parallel-group comparison between rotigotine patch and placebo patch. The QT interval refers to the respective time interval in the Electrocardiogram (ECG). The QT interval was corrected for heart rate using an individualized heart rate correction formula including QT/RR curvature optimization (QTcI). The baseline QTcI value was obtained from the average of the ECG assessment on Day -2 and Day -1. Absolute values are presented as unadjusted Mean and Standard Deviation. Baseline and final measures were taken at 4:00h. (NCT00292227)
Timeframe: Baseline (Day -2/ Day -1) 4:00h, Day 43 4:00h

Interventionmilliseconds [ms] (Mean)
Rotigotine Patch-0.31
Placebo Patch0.95

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Susceptability Changes in Haemophilus Influenzae Distal to the Site of Instillation

"Susceptibility change refers to a change in vulnerability of a specified bacterial strain to antibiotic treatment. Susceptibility was assessed by broth microdilution methods recommended by the Clinical and Laboratory Standards Institute (CLSI).~0% = zero isolates were resistant to antibiotic 100% = all isolates were resistant to antibiotic" (NCT00312338)
Timeframe: Day 0, Day 42

,
InterventionPercent of resistant isolates (Number)
Day 0Day 42
Healthy Subjects00
Infected Patients00

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Susceptability Changes in Staphylococcus Aureus Distal to the Site of Instillation

"Susceptibility change refers to a change in vulnerability of a specified bacterial strain to antibiotic treatment. Susceptibility was assessed by broth microdilution methods recommended by the Clinical and Laboratory Standards Institute (CLSI).~0% = zero isolates were resistant to antibiotic 100% = all isolates were resistant to antibiotic" (NCT00312338)
Timeframe: Day 0, Day 42

,
InterventionPercent of resistant isolates (Number)
Day 0Day 42
Healthy Subjects00
Infected Patients8.30

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Susceptability Changes in Streptococcus Pneumoniae Distal to the Site of Instillation

"Susceptibility change refers to a change in vulnerability of a specified bacterial strain to antibiotic treatment. Susceptibility was assessed by broth microdilution methods recommended by the Clinical and Laboratory Standards Institute (CLSI).~0% = zero isolates were resistant to antibiotic 100% = all isolates were resistant to antibiotic" (NCT00312338)
Timeframe: Day 0 and Day 42

,
InterventionPercent of resistant isolates (Number)
Day 0Day 42
Healthy Subjects00
Infected Patients00

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Clinical Resolution

Clinical resolution of conjunctival discharge and bulbar conjunctival injection, modified intent to treat (mITT), culture confirmed, as treated (NCT00348348)
Timeframe: Day 8 or Day 9

InterventionParticipants (Number)
Moxifloxacin Solution236
Besifloxacin Suspension213

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Clinical Resolution

Resolution of conjunctival discharge and bulbar conjunctival injection. (mITT, culture confirmed, as treated) (NCT00348348)
Timeframe: Day 5(+/- 1 day)

InterventionParticipants (Number)
Moxifloxacin Solution167
Besifloxacin Suspension147

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Microbial Eradication

eradication of baseline bacterial infection. modified intent to treat (mITT), culture confirmed, as treated (NCT00348348)
Timeframe: Day 5 (+/- 1 day)

InterventionParticipants (Number)
Moxifloxacin Solution256
Besifloxacin Suspension235

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Microbial Eradication

Microbial eradication of baseline bacterial infection. modified intent to treat (mITT), culture confirmed, as treated (NCT00348348)
Timeframe: Day 8 or Day 9

InterventionParticipants (Number)
Moxifloxacin Solution238
Besifloxacin Suspension220

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Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC) Adjusted for Free Drug Concentrations

(NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Isoniazid 300 mg/Day62.7
Linezolid 600 mg/Once Daily20.0
Linezolid 600 mg/Twice Daily16.2

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Maximum Plasma Drug Concentration/Minimum Inhibitory Concentration (Cmax/MIC)

(NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Gatifloxacin 400 mg/Day9.5
Levofloxacin 1000 mg/Day15.6
Moxifloxacin 400 mg/Day12.3
Isoniazid (INH) 300 mg/Day70.6

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Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)

The adjusted area under the curve (aAUC) for sputum colony forming units (cfu) for each day on treatment was calculated. The aAUC represents the percentage of the expected AUC given no change in log cfu in response to study drug administration. (NCT00396084)
Timeframe: Study drug administration duration - 7 days monotherapy

,,,
InterventionPercentage (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
Gatifloxacin 400 mg/Day0.980.960.920.890.870.850.82
Isoniazid (INH) 300 mg/Day0.950.900.870.840.810.800.80
Levofloxacin 1000 mg/Day0.980.950.910.880.850.830.81
Moxifloxacin 400 mg/Day0.960.940.910.890.870.850.83

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Time to Maximum Plasma Drug Concentration (Tmax) and Half-life

(NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionhours (Median)
Tmax in h (apparent time of max plasma conc.)Half-life
Isoniazid 300 mg/Day1.03.6
Linezolid 600 mg/Once Daily1.53.20
Linezolid 600 mg/Twice Daily1.04.56

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Time to Maximum Plasma Drug Concentration (Tmax) and Half-life

(NCT00396084)
Timeframe: Day 5 (7 time points)

,,,
Interventionhours (Median)
TmaxHalf-life
Gatifloxacin 400 mg/Day1.56.0
Isoniazid (INH) 300 mg/Day12.5
Levofloxacin 1000 mg/Day1.07.6
Moxifloxacin 400 mg/Day1.08.1

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Pharmacokinetic Parameters: Area Under the Curve (AUC) During First 12 and 24 Hours

Area under the curve (AUC), from time 0-12 hours for INH or 0-24 hours for gatifloxacin, levofloxacin, and moxifloxacin. (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/h/ml (Median)
Gatifloxacin 400 mg/Day42.8
Levofloxacin 1000 mg/Day129.1
Moxifloxacin 400 mg/Day55.3
Isoniazid (INH) 300 mg/Day11.9

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Maximum Plasma Drug Concentration (Cmax)

Maximum plasma concentration, given sampling scheme (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Gatifloxacin 400 mg/Day4.8
Levofloxacin 1000 mg/Day15.6
Moxifloxacin 400 mg/Day6.1
Isoniazid (INH) 300 mg/Day3.6

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Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Fluoroquinolones/Isoniazid (INH) Comparison

The rate of fall in sputum cfu between day 2 and day 7 of monotherapy was estimated by the slope of the linear regression obtained by fitting the 6 sputum cfu values corresponding to Days 2 through 7. (NCT00396084)
Timeframe: Day 2 to Day 7 Monotherapy

Interventionlog10 cfu/ml/day (Mean)
Gatifloxacin 400 mg/Day0.17
Levofloxacin 1000 mg/Day0.18
Moxifloxacin 400 mg/Day0.17
Isoniazid (INH) 300 mg/Day0.08

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Maximum Plasma Drug Concentration (Cmax)

Maximum Plasma Drug Concentration (Cmax), given sampling scheme (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Isoniazid 300 mg/Day3.3
Linezolid 600 mg/Once Daily15.0
Linezolid 600 mg/Twice Daily19.4

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Difference in Sputum Bacillary Loads: Extended Early Bactericidal Activity (EBA) From Days 2 to 7; Linezolid Once Daily/Linezolid Twice Daily/INH Comparison

The rate of fall in sputum cfu between day 2 and day 7 of monotherapy was estimated by the slope of the linear regression obtained by fitting the 6 sputum cfu values corresponding to Days 2 through 7. (NCT00396084)
Timeframe: Day 2 to Day 7 Monotherapy

Interventionlog10 cfu/ml (Mean)
Isoniazid 300 mg/Day0.16
Linezolid 600 mg/Once Daily0.09
Linezolid 600 mg/Twice Daily0.04

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Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Linezolid Once Daily/Linezolid Twice Daily/Isoniazid (INH) Comparison

Early bactericidal activity (EBA 0-2) was calculated as the rate of fall in sputum cfu (expressed in log10 units) during the first 2 days of monotherapy. Mean values for the 3 treatment groups were compared. (NCT00396084)
Timeframe: Day 0 to Day 2 Monotherapy

Interventionlog10 cfu/ml/day (Mean)
Isoniazid 300 mg/Day0.67
Linezolid 600 mg/Once Daily0.18
Linezolid 600 mg/Twice Daily0.26

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Difference in Sputum Bacillary Loads: Early Bactericidal Activity (EBA) Days 0 to 2; Fluoroquinolones/Isoniazid (INH) Comparison

Early bactericidal activity (EBA 0-2) was calculated as the rate of fall in sputum colony forming units (cfu) (expressed in log10 units) during the first 2 days of monotherapy. (NCT00396084)
Timeframe: Day 0 to Day 2 Monotherapy

Interventionlog10 cfu/ml/day (Mean)
Gatifloxacin 400 mg/Day0.35
Levofloxacin 1000 mg/Day0.45
Moxifloxacin 400 mg/Day0.33
Isoniazid (INH) 300 mg/Day0.67

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Area Under the Curve During First 12 or 24 Hours / Minimum Inhibitory Concentration (AUC/MIC)

Area Under the Curve (AUC) During First 12 or 24 Hours /Minimum Inhibitory Concentration. AUC reflects total drug (bound and unbound). MIC values were determined using protein-containing media. (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Gatifloxacin 400 mg/Day85.6
Levofloxacin 1000 mg/Day129.1
Moxifloxacin 400 mg/Day110.5
Isoniazid (INH) 300 mg/Day215.2

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Area Under the Curve (AUC) Adjusted for Free Drug Concentrations/Minimum Inhibitory Concentration (MIC)

Area Under the Curve 0-12 (AUC 0-12) Adjusted for Free Drug Concentrations/Minimum Inhibitory Concentration (MIC) and AUC 0-24/MIC (NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionug/h/ml (Median)
AUC 0-12/MICAUC 0-24/MIC
Isoniazid 300 mg/Day306.7344.6
Linezolid 600 mg/Once Daily107.8116.2
Linezolid 600 mg/Twice Daily121.6243.2

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Area Under the Curve (AUC) During First 12 and 24 Hours Adjusted for Free Drug Concentrations

Median pharmacodynamic parameters (range) adjusted for free drug concentrations. AUC 0-12 and AUC 0-24 = area under the curve during the first 12 and 24 hours after dosing, respectively (NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionug/h/ml (Median)
AUC 0-12AUC 0-24
Isoniazid 300 mg/Day15.317.2
Linezolid 600 mg/Once Daily60.166.8
Linezolid 600 mg/Twice Daily80.3160.7

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Pharmacokinetic Parameters: Area Under the Curve During First 12 and 24 Hours

Median pharmacokinetic parameters (range). AUC 0-12 and AUC 0-24 = area under the curve during the first 12 and 24 hours after dosing, respectively (NCT00396084)
Timeframe: Day 5 (7 time points)

,,
Interventionug/h/ml (Median)
AUC 0-12 (ug/h/ml)AUC 0-24 (ug/h/ml)
Isoniazid 300 mg/Day17.019.2
Linezolid 600 mg/Once Daily87.096.9
Linezolid 600 mg/Twice Daily116.4232.9

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Sputum Bacillary Loads: Adjusted Area Under the Curve (aAUC)

The adjusted area under the curve (aAUC) for sputum colony forming unit (cfu) for each day on treatment was calculated for patients in the INH arm and those in the Linezolid once daily and Linezolid twice daily arms. The aAUC represents the percentage of the expected AUC given no change in log cfu in response to study drug administration. (NCT00396084)
Timeframe: Study drug administration duration - 7 days monotherapy

,,
InterventionPercentage (Mean)
Day 1Day 2Day 3Day 4Day 5Day 6Day 7
Isoniazid 300 mg/Day0.940.890.890.850.830.810.83
Linezolid 600 mg/Once Daily0.980.970.960.960.950.950.95
Linezolid 600 mg/Twice Daily0.980.960.950.940.940.930.93

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Percent Dosing Interval Above Minimum Inhibitory Concentration (MIC)

Determined by linear extrapolation of concentration-versus-time curve to intersection with MIC. (NCT00396084)
Timeframe: Day 5 (7 time points)

InterventionPercentage (Mean)
Isoniazid (INH) 300 mg/Day95.5
Linezolid 600 mg/Once Daily62.8
Linezolid 600 mg/Twice Daily100.0

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Maximum Plasma Drug Concentrations (Cmax), Adjusted for Free Drug Concentration

Cmax adjusted for free drug concentrations after 5 days of monotherapy with study drugs (NCT00396084)
Timeframe: Day 5 (7 time points)

Interventionug/ml (Median)
Isoniazid 300 mg/Day3.1
Linezolid 600 mg/Once Daily10.3
Linezolid 600 mg/Twice Daily13.4

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Incidence of Clinically Significant Bacteremia

"Failure was defined as clinically significant bacteraemia occurring in the period of neutropenia and an intervention with a systemic antibacterial becoming necessary.~With this being a discontinuation criteria and the outcome being measured at end of treatment, only one episode is taken into account for each participant." (NCT00398411)
Timeframe: end of treatment (mean duration of treatment was 9.7 days; 10.2 days in moxifloxacin arm, 9.2 days in placebo arm)

Interventionparticipants (Number)
Moxifloxacin3
Placebo9

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Overall Survival

(NCT00398411)
Timeframe: follow up visit (at discharge from hospital up to a maximum of 28 days after transplantation)

Interventionparticipants (Number)
Moxifloxacin34
Placebo31

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Time to Occurrence of Fever >= 38°C

(NCT00398411)
Timeframe: end of treatment (mean duration of treatment was 9.7 days; 10.2 days in moxifloxacin arm, 9.2 days in placebo arm)

Interventiondays (Mean)
Moxifloxacin9.50
Placebo7.69

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Reason for Discontinuation of Treatment

Absolute neutrophil count (ANC) recovered to > 500 /µl on two consecutive days Maximum of 20 days of treatment Occurrence of fever >= 38°C Systemic antibiotic treatment despite patient being afebrile Death Other adverse event (AE) Other reason (NCT00398411)
Timeframe: end of treatment (mean duration of treatment was 9.7 days; 10.2 days in moxifloxacin arm, 9.2 days in placebo arm)

,
Interventionparticipants (Number)
recovery of absolute neutrophil countmaximum of 20 days of treatmentpremature discontinuation: occurence of feverpremature discontinuation: antibiotic treatmentpremature discontinuation: deathpremature discontinuation: other adverse eventpremature discontinuation: other reason
Moxifloxacin60181063
Placebo00231125

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Type of Infection

(NCT00398411)
Timeframe: follow up visit (at discharge from hospital up to a maximum of 28 days after transplantation)

,
Interventionparticipants (Number)
peri-anal abscessmucositispulmonary infiltrateinfection at venous catheterherpes infectioncandida infectionacute respiratory syndromeclostridium difficile infectionatypical pneumonia
Moxifloxacin011181100
Placebo110180011

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Type of Isolates and Infections

(NCT00398411)
Timeframe: end of treatment (mean duration of treatment was 9.7 days; 10.2 days in moxifloxacin arm, 9.2 days in placebo arm)

,
Interventionparticipants (Number)
bacteremia isolate: enterococcus faecalisbacteremia isolate: escherichia colibacteremia isolate: klebsiella pneumoniaebacteremia isolate: pseudomonas aeruginosabacteremia isolate: staphylococcus aureusbacteremia isolate: staphylococcus epidermidisbacteremia isolate: streptococcus speciesclostridium difficile infectionmucositis
Moxifloxacin010110010
Placebo231011111

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Percentage of Participants With Bacteriological Success (BS) at 3 to 5 Days After Start of Treatment in the Microbiological Valid (MBV) Population

Bacteriological success was defined as presumed eradication or eradication without superinfection. Presumed eradication was defined as clinical cure in absence of a culture, eradication as a negative culture, superinfection as appearance of a new organism. (NCT00402727)
Timeframe: 3 - 5 days after start of treatment

Interventionpercentage of participants (Number)
Moxifloxacin55.2
PIP/TAZ-AMC63.8

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Percentage of Cured Participants as Determined by the Data Review Committee (DRC) at Test of Cure Visit in the Intent to Treat (ITT) Population

"Clinical response was evaluated by the DRC and graded as cure, failure or indeterminate at the TOC visit. Members of the DRC were provided with subject data from the study database that included clinical signs and symptoms at each visit, concomitant medication, microbiology results, laboratory tests and interpretation of photographs." (NCT00402727)
Timeframe: 14 - 28 days after last dose of study medication

Interventionpercentage of participants (Number)
Moxifloxacin82.2
PIP/TAZ-AMC80.9

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Percentage of Cured Participants as Determined by the Data Review Committee (DRC) at Test of Cure Visit in the Per Protocol (PP) Population

"Clinical response was evaluated by the DRC and graded as cure, failure or indeterminate at the TOC visit. Members of the DRC were provided with subject data from the study database that included clinical signs and symptoms at each visit, concomitant medication, microbiology results, laboratory tests and interpretation of photographs." (NCT00402727)
Timeframe: 14 - 28 days after last dose of study medication

Interventionpercentage of participants (Number)
Moxifloxacin88.6
PIP/TAZ-AMC89.6

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Percentage of Participants Assessed as Improvements by the Data Review Committee (DRC) at the During Treatment Day 3-5 in the Per Protocol (PP) Population

"Clinical response was evaluated by the investigator and graded as improvement in signs and symptoms, or failure to respond, or indeterminate at Day 3 to 5 after treatment start based on subject data for clinical signs and symptoms at each visit, concomitant medication, microbiology results, laboratory tests and interpretation of photographs." (NCT00402727)
Timeframe: 3 - 5 days after start of treatment

Interventionpercentage of participants (Number)
Moxifloxacin98.3
PIP/TAZ-AMC99.0

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Percentage of Participants Assessed as Resolution by the Data Review Committee (DRC) at End of Therapy in the Intent to Treat (ITT) Population

"Clinical response was evaluated by the investigator and graded as resolution, or failure to respond, or indeterminate at the end of therapy based on subject data for clinical signs and symptoms at each visit, concomitant medication, microbiology results, laboratory tests and interpretation of photographs." (NCT00402727)
Timeframe: after 7 - 21 days of treatment

Interventionpercentage of participants (Number)
Moxifloxacin92.3
PIP/TAZ-AMC90.7

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Percentage of Participants Assessed as Resolution by the Data Review Committee (DRC) at End of Therapy in the Per Protocol (PP) Population

"Clinical response was evaluated by the investigator and graded as resolution, or failure to respond, or indeterminate at the end of therapy based on subject data for clinical signs and symptoms at each visit, concomitant medication, microbiology results, laboratory tests and interpretation of photographs." (NCT00402727)
Timeframe: after 7 - 21 days of treatment

Interventionpercentage of participants (Number)
Moxifloxacin95.3
PIP/TAZ-AMC95.1

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Percentage of Participants With Bacteriological Success (BS) at 3 to 5 Days After Start of Treatment in the ITT Population With Causative Organisms

Bacteriological success was defined as presumed eradication or eradication without superinfection. Presumed eradication was defined as clinical cure in absence of a culture, eradication as a negative culture, superinfection as appearance of a new organism. (NCT00402727)
Timeframe: 3 - 5 days after start of treatment

Interventionpercentage of participants (Number)
Moxifloxacin54.6
PIP/TAZ-AMC63.1

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Percentage of Participants With Bacteriological Success (BS) After 14 - 28 Days After Last Dose of Study Medication in the ITT Population With Causative Organisms

BS is presumed eradication or eradication without recurrence, super- or reinfection. Presumed eradication was defined as clinical cure in absence of a culture, eradication as a negative culture, recurrence as reappearance of organism present at start of study; super-, reinfection as appearance of a new organism during/after treatment. (NCT00402727)
Timeframe: 14 - 28 days after last dose of study medication

Interventionpercentage of participants (Number)
Moxifloxacin78.9
PIP/TAZ-AMC79.0

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Percentage of Participants With Bacteriological Success (BS) After 14 - 28 Days After Last Dose of Study Medication in the Microbiological Valid (MBV) Population

BS is presumed eradication or eradication without recurrence, super- or reinfection. Presumed eradication was defined as clinical cure in absence of a culture, eradication as a negative culture, recurrence as reappearance of organism present at start of study; super-, reinfection as appearance of a new organism during/after treatment. (NCT00402727)
Timeframe: 14 - 28 days after last dose of study medication

Interventionpercentage of participants (Number)
Moxifloxacin84.3
PIP/TAZ-AMC87.2

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Percentage of Participants With Bacteriological Success (BS) After 7 - 21 Days of Treatment in the ITT Population With Causative Organisms

Bacteriological success is presumed eradication or eradication without recurrence or superinfection. Presumed eradication was defined as clinical cure in absence of a culture, eradication as a negative culture, recurrence as reappearance of organism present at start of study, superinfection as appearance of a new organism. (NCT00402727)
Timeframe: after 7 - 21 days of treatment

Interventionpercentage of participants (Number)
Moxifloxacin84.0
PIP/TAZ-AMC87.9

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Percentage of Participants With Bacteriological Success (BS) After 7 - 21 Days of Treatment in the Microbiological Valid (MBV) Population

Bacteriological success is presumed eradication or eradication without recurrence or superinfection. Presumed eradication was defined as clinical cure in absence of a culture, eradication as a negative culture, recurrence as reappearance of organism present at start of study, superinfection as appearance of a new organism. (NCT00402727)
Timeframe: after 7 - 21 days of treatment

Interventionpercentage of participants (Number)
Moxifloxacin85.8
PIP/TAZ-AMC91.4

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Percentage of Participants Assessed as Improvements by the Data Review Committee (DRC) at the During Treatment Day 3-5 in the Intent to Treat (ITT) Population

"Clinical response was evaluated by the investigator and graded as improvement in signs and symptoms, or failure to respond, or indeterminate at Day 3 to 5 after treatment start based on subject data for clinical signs and symptoms at each visit, concomitant medication, microbiology results, laboratory tests and interpretation of photographs" (NCT00402727)
Timeframe: 3 - 5 days after start of treatment

Interventionpercentage of participants (Number)
Moxifloxacin97.2
PIP/TAZ-AMC95.8

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Corneal Epithelial Healing Time

patients' eyes will be observed daily after surgery until the corneal epithelium has completely healed (usually 3 to 4 days) (NCT00414011)
Timeframe: 3 to 4 days after surgery

Interventiondays to complete epithelial healing (Median)
Moxifloxacin4
Gatifloxacin4

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Number of Subjects Who Received Alternative Medicine

As alternative medicine any systemic antibacterial medication was considered. (NCT00453349)
Timeframe: Up to 42 days after end of treatment

,
Interventionparticipants (Number)
Receiving alternative medicineNot receiving alternative medicine
Levofloxacin Plus Metronidazole1189
Moxifloxacin4190

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Bacteriological Response at Test Of Cure (TOC) Visit in Intent To Treat Population With Causative Organism

Bacteriological response at the TOC was analyzed exploratively in the same way as the primary efficacy variable based on the subgroup of microbiologically valid subjects. At the TOC visit, eradication was considered a bacteriological success, and persistence, presumed persistence and superinfection were considered bacteriological failures. (NCT00453349)
Timeframe: 7 - 14 days at TOC visit

,
Interventionparticipants (Number)
EradicationPersistence, indeterminate, missing
Levofloxacin Plus Metronidazole259
Moxifloxacin288

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Bacteriological Response at Test Of Cure (TOC) Visit Microbiologically Valid

The bacteriological responses was based on the results of appropriate cultures taken before and, if necessary, during treatment, at the TOC visit and within the follow-up period. Bacteriological response at the TOC visit would also be based on repeated PCR tests for N. gonorrhoeae and C. trachomatis. (NCT00453349)
Timeframe: 7 - 14 days at TOC visit

,
Interventionparticipants (Number)
EradicationPersistence
Levofloxacin Plus Metronidazole224
Moxifloxacin273

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Clinical Response 7 to 14 Days After Completion of Study Drug Therapy in Per Protocol (PP) Population

Clinical cure was defined as: Reduction of the tenderness score (modified McCormack) by > 70% and apyrexia (rectal/tympanic/oral temperature value < 38.0°C or axillary temperature value < 37.5°C) and white blood cell count < 10,500/mm^3. (NCT00453349)
Timeframe: 7 - 14 days after completion of study drug therapy

,
Interventionparticipants (Number)
Clinical cureClinical non-success
Levofloxacin Plus Metronidazole15535
Moxifloxacin15242

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Clinical Response 7 to 14 Days After Completion of Study Drug Therapy on Intent To Treat (ITT) Population

"For any subject in the ITT population also valid for the PP analysis, same clinical response as in the PP analysis was applied to the ITT analysis. For those subjects in the ITT population invalid for the PP analysis, any clinical response different from clinical cure was set to non-success." (NCT00453349)
Timeframe: 7 - 14 days after completion of study drug therapy

,
Interventionparticipants (Number)
Clinical cureClinical non-success
Levofloxacin Plus Metronidazole17159
Moxifloxacin16362

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Clinical Response at Follow-up Visit on Per Protocol Population

Clinical response at follow up was analyzed exploratively in the same way as the primary efficacy variable. At Follow-up, the clinical response was graded as continued cure, clinical relapse, or indeterminate, of which only continued cure was considered success. Failures from end of treatment were carried forward. (NCT00453349)
Timeframe: 28 - 42 days after completion of study drug therapy

,
Interventionparticipants (Number)
Continued clinical cureContinued failure, clinical recurrence/relapse
Levofloxacin Plus Metronidazole15822
Moxifloxacin15727

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Clinical Response on Treatment for Intent To Treat Population

Clinical response during treatment was analyzed exploratively in the same way as the primary efficacy variable. At the During Therapy (Day 4 to 7) assessment, the clinical response was graded as clinical Improvement, clinical failure or indeterminate accordingly. Clinical improvement was considered success, all other outcomes as non-success. (NCT00453349)
Timeframe: 4 - 7 days after start of therapy

,
Interventionparticipants (Number)
Clinical improvementFailure, indeterminate, missing
Levofloxacin Plus Metronidazole17060
Moxifloxacin16659

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Clinical Response at Follow-up Visit on Intent To Treat Population

"All successfully treated subjects and subjects evaluated asindeterminate at TOC, who were not administered an additional antibiotic therapy would have their clinical response rate assessed at the follow-up visit. Patients with missing or indeterminate outcome were treated as non-successes." (NCT00453349)
Timeframe: 28 - 42 days after completion of study drug therapy

,
Interventionparticipants (Number)
Continued clinical cureFailure, relapse, indeterminate, missing
Levofloxacin Plus Metronidazole17060
Moxifloxacin16659

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Clinical Response on Treatment for Per Protocol Population

At the During Therapy (Day 4 to 7) assessment, the clinical response was graded as clinical Improvement (severity score reduced by >30% with improvement in temperature, clinical failure (reduction in severity score of < or equal 30% and/or no improvement in temperature) or indeterminate (clinical assessment not possible to determine). (NCT00453349)
Timeframe: 4 - 7 days after start of therapy

,
Interventionparticipants (Number)
Clinical ImprovementClinical failure
Levofloxacin Plus Metronidazole1815
Moxifloxacin17711

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Bacteriological Response at Follow-up Visit in Intent To Treat Population With Causative Organism

Subjects with at least one causative organism identified in the pre-therapy culture or a positive pre-therapy PCR result and an appropriate post-therapy bacteriological evaluation available were analyzed. Bacteriological responses at follow-up visit was analyzed exploratively in the same way as the primary efficacy variable. (NCT00453349)
Timeframe: 28 - 42 days after completion of study drug therapy

,
Interventionparticipants (Number)
EradicationEradication with recurrence, persistence
Levofloxacin Plus Metronidazole2311
Moxifloxacin2313

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Bacteriological Response at Follow-up Visit Microbiologically Valid

Subjects with at least one causative organism identified in the pre-therapy culture or a positive pre-therapy PCR result and an appropriate post-therapy bacteriological evaluation available were analyzed. Bacteriological responses at follow-up visit was analyzed exploratively in the same way as the primary efficacy variable. (NCT00453349)
Timeframe: 28 - 42 days after completion of study drug therapy

,
Interventionparticipants (Number)
EradicationEradication with recurrence, persistence
Levofloxacin Plus Metronidazole224
Moxifloxacin235

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Percentage of Patients With Microbiological Improvement

Percentage of patients with microbiological improvement, defined such that all bacteria present above threshold at Day 1 (Baseline) are eradicated (absent) or reduced at Day 7 based on a Classification of Microbial Response (Eradication=pathogen is absent in follow-up culture; Reduction=pathogen is reduced from baseline below threshold count in follow-up culture; Persistence=pathogen reduced from baseline but is above or equal to threshold count in follow-up culture; and Proliferation=pathogen has increased in count from baseline in follow-up culture). (NCT00464438)
Timeframe: Day 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%94.6
Moxifloxacin 0.5%92.2

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Percentage of Patients With Clearing (Clinical Success) of Conjunctival Erythema and Conjunctival Discharge at Day 7

Percentage of patients that achieved clinical success, defined as a score of 0 for both conjunctival erythema and conjunctival discharge at Day 7. Conjunctival erythema and conjunctival discharge were each assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00464438)
Timeframe: Day 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%78.6
Moxifloxacin 0.5%84.4

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Percentage of Patients With Improvement in Ocular Signs for Conjunctival Discharge at Day 7

"Percentage of patients with at least a 1-grade improvement in ocular signs for conjunctival discharge at Day 7 from Day 1 (Baseline). Conjunctival discharge was assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate,~+3=severe)." (NCT00464438)
Timeframe: Day 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%94.6
Moxifloxacin 0.5%92.2

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Percentage of Patients With Improvement in Ocular Signs for Lid Erythema

Percentage of patients with at least a 1-grade improvement in ocular signs for lid erythema at Day 7 from Day 1 (Baseline). Lid erythema was assessed on a 4-point severity grade scale (0=none, +1=mild, +2=moderate, +3=severe). (NCT00464438)
Timeframe: Days 7

InterventionPercentage of Patients (Number)
Gatifloxacin 0.3%76.8
Moxifloxacin 0.5%75.0

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Treatment Day When Patients Returned to Normal Activities as Measured by Patient Reported Data, Using LOCF Approach

The Activity Impairment Assessment (AIA) questionnaire was used to assess activity impairment at baseline and time to return to normal activities. The AIA was administered prior to first dose, every 24 hours during treatment, and at the TOC visit. Improvement in the AIA total score was defined as a decrease of at least 3 units. (NCT00492024)
Timeframe: Daily until 'Test-Of-Cure' (Day 1-5 after end of treatment)

,
Interventionparticipants (Number)
Day 2Day 3Day 4Day 5Test-Of-Cure
Moxifloxacin 400 mg2231353742
Placebo1517171922

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Percentage of Subjects With Clinical Cure (Modified Intent-to-Treat (MITT))

The primary efficacy variable was clinical response (CR) at the TOC visit, and was rated as improvement, complete resolution, failure, or indeterminate. Clinical cure, ie, success, was defined as complete resolution or improvement in the signs and symptoms such that no further therapy (antimicrobial, steroid, or irrigation) was required. (NCT00492024)
Timeframe: At 'Test-of-Cure' (TOC), Day 1-5 after end of treatment

,
InterventionPercentage of subjects (Number)
Success (Clinical Cure)FailureIndeterminateComplete resolutionImprovement
Moxifloxacin 400 mg78.119.22.712.365.8
Placebo66.733.3011.155.6

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Percentage of Subjects With Clinical Cure (Per Protocol Population (PP))

The primary efficacy variable was clinical response (CR) at the TOC visit, and was rated as improvement, complete resolution, failure, or indeterminate. Clinical cure, ie, success, was defined as complete resolution or improvement in the signs and symptoms such that no further therapy (antimicrobial, steroid, or irrigation) was required. (NCT00492024)
Timeframe: At 'Test-of-Cure', Day 1-5 after end of treatment

,
InterventionPercentage of subjects (Number)
SuccessFailureIndeterminateComplete resolutionImprovement
Moxifloxacin 400 mg82.317.7011.371.0
Placebo66.733.309.557.1

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Percentage of Subjects With Clinical Improvement During Therapy

A secondary efficacy variable was clinical response (CR) at the During Therapy visit at day 3 or 4 of treatment. CR was rated as improvement, cure, failure, or indeterminate. Clinical evaluation was based on the presence and severity (mild, moderate, or severe) of several signs and symptoms of acute sinusitis. (NCT00492024)
Timeframe: Day 3 of treatment

,
InterventionPercentage of subjects (Number)
ImprovementIndeterminateMissing
Moxifloxacin 400 mg84.94.111.0
Placebo73.34.422.2

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Percentage of Subjects With Continued Clinical Cure During Long-Term Follow-Up

A secondary efficacy variable was clinical response (CR) at the Follow-up visit 17-21 days following the start of treatment. CR was rated as continued cure, failure/relapse, or indeterminate. Clinical evaluation was based on the presence and severity (mild, moderate, or severe) of several signs and symptoms of acute sinusitis. (NCT00492024)
Timeframe: Day 12 to 26 after end of treatment

,
InterventionPercentage of subjects (Number)
Combined Clinical CureClinical Failure / RelapseMissing
Moxifloxacin 400 mg73.921.94.1
Placebo57.740.02.2

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Treatment Day When Patients Reached Symptom Improvement as Measured by Patient Reported Data, Using Last Observation Carried Forward (LOCF) Approach

The Sino-Nasal Outcome Test (SNOT-16) was used to assess subject-reported time to symptom improvement. Improvement was defined as a decrease of at least 14 units on the test. This difference is the smallest difference that has been identified as beneficial to subjects. (NCT00492024)
Timeframe: Daily until 'Test-Of-Cure' (Day 1-5 after end of treatment)

,
Interventionparticipants (Number)
Day 2Day 3Day 4Day 5Test-Of-Cure
Moxifloxacin 400 mg1426313943
Placebo710131619

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Number of Subjects Achieving Bacteriological Success at EOT Visit in the Per Protocol Population With Causative Organism(s)

Bacteriological success = response classified as 'eradication' or 'presumed eradication' without occurrence of a superinfection. Bacteriological failure = response classified as 'persistence', 'presumed persistence', or 'superinfection'. (NCT00492726)
Timeframe: After 5 - 14 days of therapy

,
Interventionparticipants (Number)
EradicationPresumed EradicationPersistencePresumed PersistenceSuperinfectionsIndeterminate/missing
Ertapenem724791120
Moxifloxacin (Avelox, BAY12-8039)5257201311

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Number of Subjects Achieving Clinical Cure at TOC Visit in the Per Protocol Population With Causative Organism(s)

Clinical cure at TOC = resolution or improvement of clinical signs and symptoms related to the infection without the occurrence of a wound infection requiring a systemic antibiotic treatment. Clinical failure at TOC = either failure to respond or insufficient lessening of the signs and symptoms of infection at end of treatment (EOT) or reappearance of the signs and symptoms of the original infection from EOT up to TOC or wound infection requiring additional systemic antimicrobial therapy at any time up to TOC. (NCT00492726)
Timeframe: 21 - 28 days after end of therapy

,
Interventionparticipants (Number)
Clinical CureClinical Failure
Ertapenem25422
Moxifloxacin (Avelox, BAY12-8039)26532

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Number of Subjects Achieving Clinical Improvement During Treatment in the Per Protocol Population

Clinical improvement = Reduction in the severity and/or number of signs and symptoms of infection.Clinical failure = Failure to respond/insufficient lessening of signs and symptoms of infection requiring a modification/addition of antibacterial therapy, or a second surgical intervention (unless the original surgery was deemed inadequate). Development of a wound infection requiring alternative/additional antibiotic therapy was considered a failure. Failed subjects must have had 3 full days of therapy administered. (NCT00492726)
Timeframe: During treatment at day 5 +/- 1 day

,
Interventionparticipants (Number)
Clinical ImprovementClinical FailureMissing
Ertapenem1942151
Moxifloxacin (Avelox, BAY12-8039)2100142

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Duration of Hospitalization

Duration of hospitalization in the per protocol population. (NCT00492726)
Timeframe: From the first admission date to the discharge date (from 4 to 71 days after start of study medication)

Interventiondays (Mean)
Moxifloxacin (Avelox, BAY12-8039)11.7
Ertapenem11.2

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Duration of Hospitalization Postoperatively

Duration of hospitalization after the first surgery until discharge in the per protocol population. (NCT00492726)
Timeframe: Duration of hospitalization after the first surgery until discharge date (from 4 to 71 days after start of study medication)

Interventiondays (Mean)
Moxifloxacin (Avelox, BAY12-8039)11.1
Ertapenem10.7

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Number of Subjects Who Died Due to Intra-abdominal Infections

Number of subjects who had died due to intra abdominal infections by the time of TOC visit. (NCT00492726)
Timeframe: 21 - 28 days after end of treatment at TOC Visit

,
Interventionparticipants (Number)
YesNo
Ertapenem1346
Moxifloxacin (Avelox, BAY12-8039)3349

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Number of Subjects Achieving Bacteriological Success at TOC Visit in the Per Protocol Population With Causative Organism(s)

Bacteriological success = response classified as 'eradication' or 'presumed eradication' without occurrence of a superinfection. Bacteriological failure = response classified as 'persistence', 'presumed persistence', or 'superinfection' - additionally, any recurrence or reinfection was treated as bacteriological failure at TOC. (NCT00492726)
Timeframe: 21 - 28 days after end of therapy

,
Interventionparticipants (Number)
EradicationPresumed EradicationPersistencePresumed PersistenceSuperinfectionsReinfections
Ertapenem024991800
Moxifloxacin (Avelox, BAY12-8039)0257202000

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Number of Subjects Achieving Clinical Cure at End of Therapy (EOT) Visit in the Per Protocol Population

Clinical cure = resolution/improvement of clinical signs and symptoms related to the infection without wound infection requiring systemic antibiotic treatment. Clinical failure = Failure to respond/insufficient lessening of signs and symptoms of infection requiring a modification/addition of antibacterial therapy, or a second surgical intervention (unless the original surgery was deemed inadequate). Development of a wound infection requiring alternative/additional antibiotic therapy was considered a failure. Failed subjects must have had 3 full days of therapy administered. (NCT00492726)
Timeframe: after 5 - 14 days of therapy

,
Interventionparticipants (Number)
Clinical CureClinical FailureMissing
Ertapenem330170
Moxifloxacin (Avelox, BAY12-8039)328231

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Number of Subjects Achieving Clinical Cure at Test of Cure (TOC) Visit in the Per Protocol Population

Clinical cure at TOC = resolution or improvement of clinical signs and symptoms related to the infection without the occurrence of a wound infection requiring a systemic antibiotic treatment. Clinical failure at TOC = either failure to respond or insufficient lessening of the signs and symptoms of infection at end of treatment (EOT) or reappearance of the signs and symptoms of the original infection from EOT up to TOC or wound infection requiring additional systemic antimicrobial therapy at any time up to TOC. (NCT00492726)
Timeframe: 21 to 28 days after completion of study drug therapy

,
Interventionparticipants (Number)
Clinical CureClinical Failure
Ertapenem32423
Moxifloxacin (Avelox, BAY12-8039)31537

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Number of Subjects Achieving Bacteriological Success During Treatment in the Per Protocol Population With Causative Organism(s)

Bacteriological success = response classified as 'eradication' or 'presumed eradication' without occurrence of a superinfection. Bacteriological failure = response classified as 'persistence', 'presumed persistence', or 'superinfection'. (NCT00492726)
Timeframe: During treatment at day 5 +/- 1 day

,
Interventionparticipants (Number)
EradicationPresumed EradicationPersistencePresumed PersistenceSuperinfections
Ertapenem5149721
Moxifloxacin (Avelox, BAY12-8039)51701600

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Number of Participants With Response (Intent-to-treat Population)

"Number of patients in the population who received at least one dose of study medication whose clinical response 1-3 days after treatment was assessed by the investigator as clinical cure" (NCT00493038)
Timeframe: At 'Test-of-Cure', Day 1-3 after treatment

Interventionparticipants (Number)
Moxifloxacin (Avelox, BAY12-8039)128
Amoxicillin/Clavulanate127

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Number of Participants With Response (Per-protocol Population)

"Number of patients in the population who met criteria pre-specified in the protocol whose clinical response 1-3 days after treatment was assessed by the investigator as clinical cure" (NCT00493038)
Timeframe: At 'Test-of-Cure', Day 1-3 after treatment

Interventionparticipants (Number)
Moxifloxacin (Avelox, BAY12-8039)119
Amoxicillin/Clavulanate125

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Number of Participants With Response (Per-protocol Population)

"Number of patients in the population who met criteria pre-specified in the protocol whose clinical response 24-30 days after treatment was assessed by the investigator as continued clinical cure" (NCT00493038)
Timeframe: End of Follow-up, Day 24-30 after treatment

Interventionparticipants (Number)
Moxifloxacin (Avelox, BAY12-8039)108
Amoxicillin/Clavulanate117

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Number of Participants With Response (Microbiologically Valid Patients)

Bacteriological Efficacy Rate at the 'Test-of-Cure' visit, measured in patients defined as 'microbiologically valid'. A bacteriological success is an eradication without super- or reinfection or presumed eradication. (NCT00493038)
Timeframe: At 'Test-of-Cure', Day 1-3 after treatment

,
InterventionParticipants (Number)
Bacteriological successFailure
Amoxicillin/Clavulanate251
Moxifloxacin (Avelox, BAY12-8039)210

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Number of Participants With Response (Microbiologically Valid Patients)

Bacteriological Efficacy Rate at the End of Follow-up period, measured in patients defined as 'microbiologically valid'. A bacteriological success is an eradication without super- or reinfection or presumed eradication. (NCT00493038)
Timeframe: End of Follow-up, Day 24-30 after treatment

,
InterventionParticipants (Number)
Bacteriological successFailureMissing / Indeterminate
Amoxicillin/Clavulanate2303
Moxifloxacin (Avelox, BAY12-8039)1902

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Numbers and % of Subjects With QTcI Change > 30 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 30 ms at any of the outcome measure time points (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

InterventionParticipants (Count of Participants)
Placebo0
Inhaled Prochlorperazine 5 mg1
Inhaled Prochlorperazine 10 mg0

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Maximum Effect of Inhaled Prochlorperazine on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo

Time-matched differences in QTcI values between the maximum of the mean difference from baseline of the QTcI interval after time-matched placebo subtraction for treatment at 11 post-inhalation times. (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

Interventionmilliseconds (Least Squares Mean)
Placebo+Inhaled Prochlorperazine 5 mg Crossover Subjects5.493
Placebo+Inhaled Prochlorperazine 10 mg Crossover Subjects5.229

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QTcI Versus Prochlorperazine Concentration

QTcI @ median prochlorperazine concentration (3.75 mcg/mL) based on linear and nonlinear regression of QTcI versus time matched serum prochlorperazine concentrations (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

Interventionmilliseconds (Least Squares Mean)
Inhaled Prochlorperazine2.83

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Numbers and % of Subjects With QTcI Change > 60 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 60 ms at any of the outcome measure time points (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

InterventionParticipants (Count of Participants)
Placebo0
Inhaled Prochlorperazine 5 mg0
Inhaled Prochlorperazine 10 mg0

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Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)

A thorough QT/QTc study may be considered to have demonstrated assay sensitivity if 1 or more of the lower 95% CI values exceeds 5 msec (NCT00543062)
Timeframe: 1, 1.5, 2, 2.5, 3, 5 hours

Interventionmilliseconds (Least Squares Mean)
Placebo+Oral Moxifloxacin 400 mg Crossover Subjects9.595

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Numbers and % of Subjects With QTcI > 450 ms

Numbers and Percents of Subjects with QTcI exceeding 450 ms (NCT00543062)
Timeframe: 24 hours

InterventionParticipants (Count of Participants)
Placebo3
Inhaled Prochlorperazine 5 mg4
Inhaled Prochlorperazine 10 mg6

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Numbers and % of Subjects With QTcI > 480 ms

Numbers and Percents of Subjects with QTcI exceeding 480 ms at any of the outcome measure time points (NCT00543062)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 22 hr

InterventionParticipants (Count of Participants)
Placebo0
Inhaled Prochlorperazine 5 mg0
Inhaled Prochlorperazine 10 mg1

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Assessment of Pharmacokinetic Parameters

Conjunctiva Concentration of Azithromycin and Moxifloxacin (NCT00564447)
Timeframe: Over 24 hours

Interventionμg/g (Mean)
Azithromycin Ophthalmic Solution, 1% -30 Minutes Post Dose130.8
Azithromycin Ophthalmic Solution, 1% -2 Hours Post Dose51.6
Azithromycin Ophthalmic Solution, 1% -12 Hours Post Dose67.1
Azithromycin Ophthalmic Solution, 1% -24 Hours Post Dose31.9
Moxifloxacin 0.5% Ophthalmic Solution-30 Minutes Post Dose1.9
Moxifloxacin 0.5% Ophthalmic Solution-2 Hours Post Dose3.8
Moxifloxacin 0.5% Ophthalmic Solution-12 Hours Post Dose0.0
Moxifloxacin 0.5% Ophthalmic Solution-24 Hours Post Dose0.0

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Concentration of AzaSite and Vigamox in the Tear Fluid Across Six Time Points Ranging From 15 Minutes to 24 Hours Following Administration.

(NCT00575367)
Timeframe: 15 minutes, 1 hour, 2 hours, 4 hours, 8 hours, and 24 hours

,
Interventionµg/mL (Mean)
15 Minutes1 Hour2 Hours4 Hours8 Hours24 Hours
AzaSite16.4854.0071.9661.5582.5900.195
Vigamox8.1992.2212.9850.6031.3640.021

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Conjunctiva Concentration Prior to Cataract Surgery at One of Ten Time Points Ranging From 1 to 14 Days (Per Protocol Pharmacokinetic Population)

Nominal time is scheduled time relative to administration of the first eye drop (NCT00575380)
Timeframe: Az(hr): 1,12,48,49,72,144,145,168,216,312; Vig(hr): 1,8,48,49,56,144,145,168,216,312

,
Interventionug/g (Mean)
Timepoint 1 - 1 hr (AzaSite and Vigamox)Timepoint 2 - 12 hrs (AzaSite)/8 hrs (Vigamox)Timepoint 3 - 48 hrs (AzaSite and Vigamox)Timepoint 4 - 49 hrs (AzaSite and Vigamox)Timepoint 5 -72 hrs (AzaSite)/56 hrs (Vigamox)Timepoint 6 - 144 hrs (AzaSite and Vigamox)Timepoint 7 - 145 hrs (AzaSite and Vigamox)Timepoint 8 - 168 hrs (AzaSite and Vigamox)Timepoint 9 - 216 hrs (AzaSite and Vigamox)Timepoint 10 - 312 (AzaSite and Vigamox)
Azasite40.433.55559.73398.6287.75175.017269.46261.125273.963.867
Vigamox5.7471.0511.12915.754.862.3055.432.322.165.011

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Aqueous Humor Concentration Prior to Cataract Surgery at One of Ten Time Points Ranging From 1 to 14 Days (Per Protocol Pharmacokinetic Population)

(NCT00575380)
Timeframe: Az(hr): 1,12,48,49,72,144,145,168,216,312; Vig(hr): 1,8,48,49,56,144,145,168,216,312

,
Interventionug/mL (Mean)
Timepoint 1- 1 hr (AzaSite and Vigamox)Timepoint 2- 12 hrs (AzaSite)/ 8 hrs (Vigamox)Timepoint 3 - 48 hrs (AzaSite and Vigamox)Timepoint 4 - 49 hrs (AzaSite and Vigamox)Timepoint 5 - 72 hrs (AzaSite)/ 56 hr (Vigamox)Timepoint 6 - 144 hrs (AzaSite and Vigamox)Timepoint 7 - 145 hrs (AzaSite and Vigamox)Timepoint 8 - 168 hrs (AzaSite and Vigamox)Timepoint 9 - 216 hrs (AzaSite and Vigamox)Timepoint 10 - 312 hrs (AzaSite and Vigamox)
Azasite.022.088.047.023.02.026.052.035.028.011
Vigamox.582.113.079.765.084.225.669.059.071.017

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Number of Participants With a Negative Bacterial Culture

Conjunctival swab specimens were inoculated onto tryptic soy agar with 5% sheep blood and GC II agar supplemented with hemoglobin and isovialex with incubation at 35 degrees C in ambient air supplemented with 5% carbon dioxide for 48 hours. S pneumoniae, H influenzai and M Catarrhalis were identified. (NCT00581542)
Timeframe: 10 days

Interventionparticipants (Number)
Moxifloxin Group22
Polytrim Group19

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Number of Participants With Normal Physical Examination of the Eye

(NCT00581542)
Timeframe: 10 days

Interventionparticipants (Number)
Polytrim Arm49
Moxifloxacin37

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Satisfaction Rate

(NCT00635570)
Timeframe: at 3 months

,
InterventionPercentage of Participants (Number)
Satisfaction - YesSatisfaction - NoMissing
Contraceptive Vaginal Ring68239
Oral Contraceptive Pill71254

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Continuation Rate

Rate of intention to continue the contraceptive method at 6 months (NCT00635570)
Timeframe: at 6 month (3 month after the end of the study period)

,
InterventionPercentage of Participants (Number)
Continuation - YesContinuation - NoMissing
Contraceptive Vaginal Ring26722
Oral Contraceptive Pill29682

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Adherence Rate (Rate of Perfect Method Use)

"Perfect use was defined as reporting never missing a pill or never removing the contraceptive vaginal ring for more than 2 hours during days 1-21 of all three monthly cycles" (NCT00635570)
Timeframe: For the first 3 months

InterventionPercentage of Participants (Number)
Contraceptive Vaginal Ring57
Oral Contraceptive Pill45

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Continuation Rate

Rate of intention to continue the contraceptive method at 3 months (NCT00635570)
Timeframe: at 3 months

,
InterventionPercentage of Participants (Number)
Continuation - YesContinuation - NoMissing
Contraceptive Vaginal Ring43525
Oral Contraceptive Pill52480

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Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 6

QTcF is the QT interval using Fridericia's correction formula. QT interval is a measure of time between the start of the Q wave and the end of the T wave and is dependent on the heart rate (e.g., the faster the heart rate, the shorter the QT interval). The QT interval has to be corrected in order to aid interpretation. (NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionmsec (Least Squares Mean)
Guanfacine 8 mg-2.67
Moxifloxacin6.44
Placebo (Guanfacine)-4.31
Placebo (Moxifloxacin)-4.35

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Change From Baseline in Electrocardiogram Results (QTcNi) at Time of Maximum Plasma Concentration (Tmax) on Day 1

QTcNi is the QT interval using a subject-specific correction formula. QT interval is a measure of time between the start of the Q wave and the end of the T wave and is dependent on the heart rate (e.g., the faster the heart rate, the shorter the QT interval). The QT interval has to be corrected in order to aid interpretation. (NCT00672984)
Timeframe: Baseline, Tmax (time of subject-specific maximum plasma concentration)

Interventionmsec (Least Squares Mean)
Guanfacine 4 mg-3.37
Moxifloxacin12.96
Placebo (Guanfacine)-0.94
Placebo (Moxifloxacin)-0.91

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Change From Baseline in Electrocardiogram Results (QTcNi) at Tmax on Day 6

QTcNi is the QT interval using a subject-specific correction formula. QT interval is a measure of time between the start of the Q wave and the end of the T wave and is dependent on the heart rate (e.g., the faster the heart rate, the shorter the QT interval). The QT interval has to be corrected in order to aid interpretation. (NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionmsec (Least Squares Mean)
Guanfacine 8 mg-12.45
Moxifloxacin8.99
Placebo (Guanfacine)-4.37
Placebo (Moxifloxacin)-4.13

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Change From Baseline in Heart Rate (HR) at Tmax on Day 1

(NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionbpm (Least Squares Mean)
Guanfacine 4 mg-7.18
Moxifloxacin5.46
Placebo (Guanfacine)-0.42
Placebo (Moxifloxacin)0.73

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Change From Baseline in Heart Rate (HR) at Tmax on Day 6

(NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionbpm (Least Squares Mean)
Guanfacine 8 mg-19.74
Moxifloxacin4.66
Placebo (Guanfacine)0.11
Placebo (Moxifloxacin)1.22

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Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 1

(NCT00672984)
Timeframe: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, and 24 hours post-dose

Interventionng.h/ml (Mean)
Guanfacine 4 mg110.8
Moxifloxacin19892

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Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 6

(NCT00672984)
Timeframe: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, and 24 hours post-dose

Interventionhours (Mean)
Guanfacine 8 mg5.2
Moxifloxacin1.78

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Time of Maximum Plasma Concentration (Tmax) of Guanfacine and Moxifloxacin on Day 1

(NCT00672984)
Timeframe: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, and 24 hours post-dose

Interventionhours (Mean)
Guanfacine 4 mg3.9
Moxifloxacin2.13

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Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 6

(NCT00672984)
Timeframe: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, and 24 hours post-dose

Interventionng/ml (Mean)
Guanfacine 8 mg24.70
Moxifloxacin2003.4

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Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 6

QT interval is a measure of time between the start of the Q wave and the end of the T wave and is dependent on the heart rate (e.g., the faster the heart rate, the shorter the QT interval). (NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionmsec (Least Squares Mean)
Guanfacine 8 mg46.21
Moxifloxacin-3.09
Placebo (Guanfacine)-3.63
Placebo (Moxifloxacin)-6.71

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Maximum Plasma Concentration (Cmax) of Guanfacine and Moxifloxacin on Day 1

(NCT00672984)
Timeframe: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, and 24 hours post-dose

Interventionng/ml (Mean)
Guanfacine 4 mg8.51
Moxifloxacin1943.1

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Area Under the Steady-state Plasma Concentration-time Curve (AUC) for Guanfacine and Moxifloxacin on Day 6

(NCT00672984)
Timeframe: pre-dose and 1, 2, 3, 4, 5, 6, 8, 12, and 24 hours post-dose

Interventionng.h/ml (Mean)
Guanfacine 8 mg370.3
Moxifloxacin20767

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Change From Baseline in Electrocardiogram Results (QT) Interval at Tmax on Day 1

QT interval is a measure of time between the start of the Q wave and the end of the T wave and is dependent on the heart rate (e.g., the faster the heart rate, the shorter the QT interval). (NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionmsec (Least Squares Mean)
Guanfacine 4 mg15.88
Moxifloxacin-1.27
Placebo (Guanfacine)0.56
Placebo (Moxifloxacin)-2.20

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Change From Baseline in Electrocardiogram Results (QTcF) at Tmax on Day 1

QTcF is the QT interval using Fridericia's correction formula. QT interval is a measure of time between the start of the Q wave and the end of the T wave and is dependent on the heart rate (e.g., the faster the heart rate, the shorter the QT interval). The QT interval has to be corrected in order to aid interpretation. (NCT00672984)
Timeframe: Baseline and Tmax (time of subject-specific maximum plasma concentration)

Interventionmsec (Least Squares Mean)
Guanfacine 4 mg0.15
Moxifloxacin9.96
Placebo (Guanfacine)-0.83
Placebo (Moxifloxacin)-1.14

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

LJ culture conversion (NCT00728507)
Timeframe: Week 8

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

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - General Activities

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (general activities - 16 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.56
Ortho Tri-Cyclen Lo1.27

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Household Duties

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (household duties - yes or no; if yes, then 4 choices, and 10 items with a scale of 1-5 [very poor, poor, fair, good, very good]). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.50
Ortho Tri-Cyclen Lo3.08

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Item Satisfaction

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (item satisfaction). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.1
Ortho Tri-Cyclen Lo0.1

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Leisure Time Activities

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (leisure time activities - 6 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.22
Ortho Tri-Cyclen Lo2.77

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Overall Life Satisfaction and Contentment

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (overall life satisfaction and contentment). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.1
Ortho Tri-Cyclen Lo0.0

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Participant Feeling

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (participant feeling - 14 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.12
Ortho Tri-Cyclen Lo2.19

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Physical Health

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (physical health - 13 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.13
Ortho Tri-Cyclen Lo3.44

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - School/Course Work

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (school / course work - yes or no; if yes, then 4 choices, and 10 items with a scale of 1-5 (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.18
Ortho Tri-Cyclen Lo5.13

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Social Relationship

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (social relationship - 11 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.30
Ortho Tri-Cyclen Lo0.41

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Mean Change From Baseline to Cycle 6 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Work

Change from Baseline to Cycle 6 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (work - yes or no; if yes, then 4 choices, and 13 items with a scale of 1-5 [very poor, poor, fair, good, very good]). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.54
Ortho Tri-Cyclen Lo0.08

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Mean Length of Bleeding / Spotting Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment and includes the initial bleeding episode that triggered the first intake of study medication, meaning that the first treatment cycle includes 2 bleeding episodes. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.82
Ortho Tri-Cyclen Lo6.20

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Mean Length of Bleeding / Spotting Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.46
Ortho Tri-Cyclen Lo5.71

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Mean Length of Bleeding / Spotting Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.70
Ortho Tri-Cyclen Lo5.85

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Mean Length of Bleeding / Spotting Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.25
Ortho Tri-Cyclen Lo5.65

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Mean Length of Spotting-only Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)2.64
Ortho Tri-Cyclen Lo2.53

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Mean Length of Spotting-only Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)2.74
Ortho Tri-Cyclen Lo2.77

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Mean Length of Spotting-only Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)2.75
Ortho Tri-Cyclen Lo2.44

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Mean Length of Spotting-only Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)2.77
Ortho Tri-Cyclen Lo2.10

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Number of Bleeding / Spotting Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment and includes the initial bleeding episode that triggered the first intake of study medication, meaning that the first treatment cycle includes 2 bleeding episodes. (Episode is a set of days with bleeding/spotting) (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.6
Ortho Tri-Cyclen Lo3.7

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Number of Bleeding / Spotting Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (Episode is a set of days with bleeding/spotting) (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.3
Ortho Tri-Cyclen Lo3.4

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Number of Bleeding / Spotting Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (Episode is a set of days with bleeding/spotting) (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.0
Ortho Tri-Cyclen Lo3.3

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Number of Bleeding / Spotting Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (Episode is a set of days with bleeding/spotting) (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.0
Ortho Tri-Cyclen Lo3.7

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Number of Days With Bleeding or Spotting in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment and includes the initial bleeding episode that triggered the first intake of study medication, meaning that the first treatment cycle includes 2 bleeding episodes. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)19.0
Ortho Tri-Cyclen Lo23.7

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Number of Days With Bleeding or Spotting in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.3
Ortho Tri-Cyclen Lo18.8

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Number of Days With Bleeding or Spotting in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)14.1
Ortho Tri-Cyclen Lo19.1

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Number of Days With Bleeding or Spotting in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)12.8
Ortho Tri-Cyclen Lo19.4

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Number of Days With Spotting-only in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)9.3
Ortho Tri-Cyclen Lo8.6

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Number of Days With Spotting-only in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)6.8
Ortho Tri-Cyclen Lo6.4

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Number of Days With Spotting-only in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)6.6
Ortho Tri-Cyclen Lo6.3

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Number of Days With Spotting-only in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)5.6
Ortho Tri-Cyclen Lo5.6

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Number of Intracyclic Bleeding Days at Cycle 1

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.5
Ortho Tri-Cyclen Lo0.5

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Number of Intracyclic Bleeding Days at Cycle 13

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.5
Ortho Tri-Cyclen Lo0.4

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Number of Intracyclic Bleeding Days at Cycle 3

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.4
Ortho Tri-Cyclen Lo0.7

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Number of Intracyclic Bleeding Days at Cycle 6

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.9
Ortho Tri-Cyclen Lo1.1

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Number of Intracyclic Bleeding Episodes at Cycle 1

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (Episode is a set of days with intracyclic bleeding) (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.3
Ortho Tri-Cyclen Lo0.1

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Number of Intracyclic Bleeding Episodes at Cycle 13

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (Episode is a set of days with intracyclic bleeding) (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.2
Ortho Tri-Cyclen Lo0.1

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Number of Intracyclic Bleeding Episodes at Cycle 3

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (Episode is a set of days with intracyclic bleeding) (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.2
Ortho Tri-Cyclen Lo0.2

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Number of Intracyclic Bleeding Episodes at Cycle 6

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (Episode is a set of days with intracyclic bleeding) (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.2
Ortho Tri-Cyclen Lo0.2

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Number of Spotting-only Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.2
Ortho Tri-Cyclen Lo0.5

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Number of Spotting-only Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.0
Ortho Tri-Cyclen Lo0.5

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Number of Spotting-only Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.7
Ortho Tri-Cyclen Lo0.3

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Number of Spotting-only Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionEpisodes (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.6
Ortho Tri-Cyclen Lo0.2

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Onset of Withdrawal Bleeding Episodes at Cycle 1

Onset was defined as the number of days between progestogen withdrawal and the first day of the withdrawal bleeding episode (ie, starting on or after Day 25 for EV/DNG and on or after Day 22 for EE/NGM). (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.7
Ortho Tri-Cyclen Lo4.0

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Onset of Withdrawal Bleeding Episodes at Cycle 13

Onset was defined as the number of days between progestogen withdrawal and the first day of the withdrawal bleeding episode (ie, starting on or after Day 25 for EV/DNG and on or after Day 22 for EE/NGM). (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.1
Ortho Tri-Cyclen Lo2.1

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Onset of Withdrawal Bleeding Episodes at Cycle 3

Onset was defined as the number of days between progestogen withdrawal and the first day of the withdrawal bleeding episode (ie, starting on or after Day 25 for EV/DNG and on or after Day 22 for EE/NGM). (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.3
Ortho Tri-Cyclen Lo3.3

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Onset of Withdrawal Bleeding Episodes at Cycle 6

Onset was defined as the number of days between progestogen withdrawal and the first day of the withdrawal bleeding episode (ie, starting on or after Day 25 for EV/DNG and on or after Day 22 for EE/NGM). (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)5.3
Ortho Tri-Cyclen Lo3.1

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The Change in Average of the 3 Highest Visual Analog Scale (VAS) Values of the Hormone Withdrawal-associated Symptoms Pelvic Pain or Headache During Cycle Days 22 to 28 From Baseline to Cycle 6

Subject self-assessed pelvic pain or headache per visual analog scale (VAS) values during the menstrual/withdrawal bleeding episode and Baseline. The VAS consists of a 100 mm long straight line, with verbal anchors at either end, representing a continuum of pain intensity. Accordingly, the scale ranges from 0 mm (absence of pain) to 100 mm (unbearable pain), and the change ranges from -100 mm (best) to 100 mm (worst). (NCT00754065)
Timeframe: Day 22-28 from Baseline to Day 22-28 from Cycle 6 (28 days per Cycle)

Interventionmm (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)43.05
Ortho Tri-Cyclen Lo34.97

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The Change of Pelvic Pain or Headache as Determined by the Highest Visual Analog Scale (VAS) Values During Cycle Days 22 to 28 From Baseline to Cycle 6

Subject self-assessed pelvic pain or headache per visual analog scale (VAS) values during the menstrual/withdrawal bleeding episode and Baseline. The VAS consists of a 100 mm long straight line, with verbal anchors at either end, representing a continuum of pain intensity. Accordingly, the scale ranges from 0 mm (absence of pain) to 100 mm (unbearable pain), and the change ranges from -100 mm (best) to 100 mm (worst). (NCT00754065)
Timeframe: Days 22-28 from Baseline to Days 22-28 from Cycle 6 (28 days per Cycle)

Interventionmm (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)43.60
Ortho Tri-Cyclen Lo34.55

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Mean Change From Baseline to Cycle 13 in Psychological General Well-Being Index (PGWBI)

Change from Baseline to Cycle 13 in PGWBI Questionnaire's assessment of participant's overall sense of well-being or distress. The PGWBI includes 22 items that, apart from combining into a global overall score, are divided into 6 dimensions: anxiety, depressed mood, positive well-being, self-control, health, and vitality. The response format used a 6-grade Likert scale and the change in the normalized PGWBI global score as well as all the sub-domains score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

,
InterventionScores on a scale (Mean)
Global scoreAnxietyDepressed moodPositive well-beingSelf-controlGeneral healthVitality
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.14-1.2-0.650.60-0.490.860.28
Ortho Tri-Cyclen Lo-0.18-0.8-0.980.38-0.161.35-0.51

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Mean Change From Baseline to Cycle 6 in Psychological General Well-Being Index (PGWBI)

Change from Baseline to Cycle 6 in PGWBI Questionnaire's assessment of participant's overall sense of well-being or distress. The PGWBI includes 22 items that, apart from combining into a global overall score, are divided into 6 dimensions: anxiety, depressed mood, positive well-being, self-control, health, and vitality. The response format used a 6-grade Likert scale and the change in the normalized PGWBI global score as well as all the sub-domains score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 6 (28 days per Cycle)

,
InterventionScores on a scale (Mean)
Global scoreAnxietyDepressed moodPositive well-beingSelf-controlGeneral healthVitality
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.410.30.1849.660.6981.81-0.17
Ortho Tri-Cyclen Lo1.102.8-1.0450.290.1281.120.19

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Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 1

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
SpottingLightNormalHeavy
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)46.223.115.415.4
Ortho Tri-Cyclen Lo50.018.818.812.5

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Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 13

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
SpottingLightNormalHeavy
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)31.652.610.55.3
Ortho Tri-Cyclen Lo57.10.028.614.3

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Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 3

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
SpottingLightNormalHeavy
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)47.123.520.68.8
Ortho Tri-Cyclen Lo57.715.423.13.8

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Percentage of Participants by Maximum Intensity of Intracyclic Bleeding Episodes at Cycle 6

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
SpottingLightNormalHeavy
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)44.425.918.511.1
Ortho Tri-Cyclen Lo61.33.219.416.1

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Percentage of Participants With / Without Withdrawal Bleeding at Cycle 1

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
without withdrawal bleedingwith withdrawal bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)25.075.0
Ortho Tri-Cyclen Lo12.887.2

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Percentage of Participants With / Without Withdrawal Bleeding at Cycle 13

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
without withdrawal bleedingwith withdrawal bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)58.241.8
Ortho Tri-Cyclen Lo19.180.9

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Percentage of Participants With / Without Withdrawal Bleeding at Cycle 3

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
without withdrawal bleedingwith withdrawal bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)21.079.0
Ortho Tri-Cyclen Lo7.792.3

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Percentage of Participants With / Without Withdrawal Bleeding at Cycle 6

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
without withdrawal bleedingwith withdrawal bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)17.782.3
Ortho Tri-Cyclen Lo8.391.7

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Percentage of Participants With at Least 1 Intracyclic Bleeding Episode at Cycles 2 to 13

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: Cycles 2 to 13 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
YesNo
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)62.038.0
Ortho Tri-Cyclen Lo49.750.3

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Percentage of Participants With at Least 1 Intracyclic Bleeding Episode at Cycles 2 to 6

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: Cycles 2 to 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
YesNo
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)53.846.2
Ortho Tri-Cyclen Lo40.559.5

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Percentage of Participants With Improvement in the Investigator's Assessment in Clinical Global Impression (CGI) at Cycle 13

CGI is used to collect information regarding the subject's total clinical experience. The assessment scale ranges from 0 to 7: (0=not assessed; 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; 7=very much worse). The scale of 1, 2, and 3 were categorized as improvement. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
Very much improvedMuch improvedMinimally improved
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)37.932.315.3
Ortho Tri-Cyclen Lo20.326.627.3

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Percentage of Participants With Improvement in the Investigator's Assessment in Clinical Global Impression (CGI) at Cycle 6

CGI is used to collect information regarding the subject's total clinical experience. The assessment scale ranges from 0 to 7: (0=not assessed; 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; 7=very much worse). The scale of 1, 2, and 3 were categorized as improvement. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
Very much improvedMuch improvedMinimally improved
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)21.141.527.2
Ortho Tri-Cyclen Lo20.025.233.5

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Percentage of Participants With Improvement in the Participant's Assessment in Clinical Global Impression (CGI) at Cycle 13

In 1 section of the CGI the subject rates their total improvement and rate of satisfaction with sexuality during treatment. The assessment scale ranges from 0 to 7: (0=not assessed; 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; 7=very much worse). The scale of 1, 2, and 3 were categorized as improvement. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
Very much improvedMuch improvedMinimally improved
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)33.935.516.9
Ortho Tri-Cyclen Lo17.225.028.1

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Percentage of Participants With Improvement in the Participant's Assessment in Clinical Global Impression (CGI) at Cycle 6

In 1 section of the CGI the subject rates their total improvement and rate of satisfaction with sexuality during treatment. The assessment scale ranges from 0 to 7: (0=not assessed; 1=very much improved; 2=much improved; 3=minimally improved; 4=no change; 5=minimally worse; 6=much worse; 7=very much worse). The scale of 1, 2, and 3 were categorized as improvement. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
Very much improvedMuch improvedMinimally improved
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)25.232.729.3
Ortho Tri-Cyclen Lo11.630.332.2

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Percentage of Participants With no Increase in Rescue Medication and VAS Decrease During Cycle Days 22 to 28 From Baseline to Cycle 6

Rescue medication was standardized intake of 200 mg Ibuprofen tablets. Baseline: 7 days (Day 22) before first menstrual bleeding to Day 28. Treatment: 7 days (Day 22) before withdrawal bleeding of 6th cycle to Day 28 before the same cycle. The visual analog scale (VAS) is a subject-assessed measure of pelvic pain or headache consisting of a 100 mm long straight line, with verbal anchors at either end, representing a continuum of pain intensity. Accordingly, the scale ranges from 0 mm (absence of pain) to 100 mm (unbearable pain), and the change ranges from -100 mm (best) to 100 mm (worst). (NCT00754065)
Timeframe: Day 22-28 from Baseline to Day 22-28 from Cycle 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
15 mm VAS decrease30 mm VAS decrease45 mm VAS decrease25% VAS decrease50% VAS decrease75% VAS decreaseHalf-SD decrease
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)68.158.138.267.056.038.270.2
Ortho Tri-Cyclen Lo54.442.626.054.442.225.559.8

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Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 1

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
with absence of intracyclic bleedingwithout absence of intracyclic bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)78.321.7
Ortho Tri-Cyclen Lo91.58.5

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Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 13

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
with absence of intracyclic bleedingwithout absence of intracyclic bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)82.717.3
Ortho Tri-Cyclen Lo93.66.4

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Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 3

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
with absence of intracyclic bleedingwithout absence of intracyclic bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)79.620.4
Ortho Tri-Cyclen Lo85.714.3

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Percentage of Participants With Presence or Absence of Intracyclic Bleeding at Cycle 6

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

,
InterventionPercentage of participants (Number)
with absence of intracyclic bleedingwithout absence of intracyclic bleeding
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)81.618.4
Ortho Tri-Cyclen Lo80.319.7

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The Change From Baseline to Cycle 13 in the Number of Ibuprofen Tablets Used as Rescue Medication

Rescue medication use was standardized intake of 200 mg Ibuprofen tablets. Baseline period: 7 days (Day 22) before the first menstrual bleeding until Day 28 (normalized to a standard 28-day cycle). Treatment period: 7 days (Day 22) before the withdrawal bleeding (WB) of the 13th treatment cycle until Day 28 before the same cycle (normalized to a standard 28-day cycle). Number of tablets taken by each subject, and then the Mean and standard deviation ((SD) derived. (NCT00754065)
Timeframe: From Baseline to Cycle 13 (28 days per Cycle)

,
InterventionTablets (Mean)
Days 1-21Days 22-28
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-2.3-5.3
Ortho Tri-Cyclen Lo-3.5-5.2

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The Change From Baseline to Cycle 6 in the Number of Ibuprofen Tablets Used as Rescue Medication

Rescue medication use was standardized intake of 200 mg Ibuprofen tablets. Baseline period: 7 days (Day 22) before the first menstrual bleeding until Day 28 (normalized to a standard 28-day cycle). Treatment period: 7 days (Day 22) before the withdrawal bleeding (WB) of the 6th treatment cycle until Day 28 of the same cycle (normalized to a standard 28-day cycle). Number of tablets taken by each subject, and then the Mean and standard deviation (SD) derived. (NCT00754065)
Timeframe: From Baseline to Cycle 6 (28 days per Cycle)

,
InterventionTablets (Mean)
Days 1-21Days 22-28
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-1.6-5.8
Ortho Tri-Cyclen Lo-3.0-4.6

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Maximum Length of Spotting-only Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.2
Ortho Tri-Cyclen Lo3.1

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Change From Baseline to Cycle 13 in the Average of the Three Highest VAS Values of the Hormone Withdrawal-associated Symptoms Pelvic Pain or Headache During Cycle Days 22 to 28

Subject self-assessed pelvic pain or headache per visual analog scale (VAS) values during the menstrual/withdrawal bleeding episode and Baseline. The VAS consists of a 100 mm long straight line, with verbal anchors at either end, representing a continuum of pain intensity. Accordingly, the scale ranges from 0 mm (absence of pain) to 100 mm (unbearable pain), and the change ranges from -100 mm (best) to 100 mm (worst). (NCT00754065)
Timeframe: Days 22-28 from Baseline to Days 22-28 from Cycle 13 (28 days per Cycle)

Interventionmm (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)45.89
Ortho Tri-Cyclen Lo39.19

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Change From Baseline to Cycle 3 in the Average of the Three Highest VAS Values of the Hormone Withdrawal-associated Symptoms Pelvic Pain or Headache During Cycle Days 22 to 28

Subject self-assessed pelvic pain or headache per visual analog scale (VAS) values during the menstrual/withdrawal bleeding episode and Baseline. The VAS consists of a 100 mm long straight line, with verbal anchors at either end, representing a continuum of pain intensity. Accordingly, the scale ranges from 0 mm (absence of pain) to 100 mm (unbearable pain), and the change ranges from -100 mm (best) to 100 mm (worst). (NCT00754065)
Timeframe: Days 22-28 from Baseline to Days 22-28 from Cycle 3 (28 days per Cycle)

Interventionmm (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)36.92
Ortho Tri-Cyclen Lo32.28

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Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment and includes the initial bleeding episode that triggered the first intake of study medication, meaning that the first treatment cycle includes 2 bleeding episodes. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)5.1
Ortho Tri-Cyclen Lo5.1

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Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.3
Ortho Tri-Cyclen Lo3.5

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Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.0
Ortho Tri-Cyclen Lo3.1

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Difference in Duration Between Longest and Shortest Bleeding / Spotting Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)2.7
Ortho Tri-Cyclen Lo2.8

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Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment and includes the initial bleeding episode that triggered the first intake of study medication, meaning that the first treatment cycle includes 2 bleeding episodes. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.2
Ortho Tri-Cyclen Lo0.5

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Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.0
Ortho Tri-Cyclen Lo0.7

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Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.4
Ortho Tri-Cyclen Lo0.6

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Difference in Duration Between Longest and Shortest Spotting-only Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.9
Ortho Tri-Cyclen Lo0.2

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Length of Withdrawal Bleeding Episodes at Cycle 1

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.2
Ortho Tri-Cyclen Lo6.0

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Length of Withdrawal Bleeding Episodes at Cycle 13

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.8
Ortho Tri-Cyclen Lo5.5

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Length of Withdrawal Bleeding Episodes at Cycle 3

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.3
Ortho Tri-Cyclen Lo5.8

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Length of Withdrawal Bleeding Episodes at Cycle 6

Withdrawal bleeding is bleeding that occurs when using oral contraceptives (OCs) caused by falling levels and/or taking away external source of estrogen and progestogen toward cycle end. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)4.6
Ortho Tri-Cyclen Lo5.7

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Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 1

Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.2
Ortho Tri-Cyclen Lo4.0

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Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 13

Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.5
Ortho Tri-Cyclen Lo4.1

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Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 3

Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.2
Ortho Tri-Cyclen Lo4.2

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Maximum Intensity of Withdrawal Bleeding Episodes at Cycle 6

Intensity was scored as 1=none, 2=spotting, 3=light, 4=normal, or 5=heavy. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.4
Ortho Tri-Cyclen Lo4.0

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Maximum Length of Bleeding / Spotting Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment and includes the initial bleeding episode that triggered the first intake of study medication, meaning that the first treatment cycle includes 2 bleeding episodes. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)7.8
Ortho Tri-Cyclen Lo9.0

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Maximum Length of Bleeding / Spotting Episodes in Reference Period 2

Reference Period 2 is defined as Day 91 to Day 180 during study treatment. (NCT00754065)
Timeframe: From Day 91 to Day 180

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)6.2
Ortho Tri-Cyclen Lo7.5

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Maximum Length of Bleeding / Spotting Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)6.2
Ortho Tri-Cyclen Lo7.4

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Maximum Length of Bleeding / Spotting Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)5.7
Ortho Tri-Cyclen Lo7.1

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Maximum Length of Intracyclic Bleeding Episodes at Cycle 1

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 1 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)6.7
Ortho Tri-Cyclen Lo6.2

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Maximum Length of Intracyclic Bleeding Episodes at Cycle 13

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 13 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.0
Ortho Tri-Cyclen Lo6.0

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Maximum Length of Intracyclic Bleeding Episodes at Cycle 3

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 3 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)6.6
Ortho Tri-Cyclen Lo4.2

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Maximum Length of Intracyclic Bleeding Episodes at Cycle 6

Intracyclic bleeding is any unexpected bleeding episode occurring in cyclical treatment regimens. (NCT00754065)
Timeframe: At Cycle 6 (28 days per Cycle)

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)5.0
Ortho Tri-Cyclen Lo5.2

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Maximum Length of Spotting-only Episodes in Reference Period 1

Reference Period 1 is defined as Day 1 to Day 90 during study treatment. (NCT00754065)
Timeframe: From Day 1 to Day 90

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.3
Ortho Tri-Cyclen Lo2.8

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Maximum Length of Spotting-only Episodes in Reference Period 3

Reference Period 3 is defined as Day 181 to Day 270 during study treatment. (NCT00754065)
Timeframe: From Day 181 to Day 270

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.5
Ortho Tri-Cyclen Lo2.8

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Maximum Length of Spotting-only Episodes in Reference Period 4

Reference Period 4 is defined as Day 271 to Day 360 during study treatment. (NCT00754065)
Timeframe: From Day 271 to Day 360

InterventionDays (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)3.2
Ortho Tri-Cyclen Lo2.2

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - General Activities

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (general activities - 16 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.73
Ortho Tri-Cyclen Lo1.34

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Household Duties

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (household duties - yes or no; if yes, then 4 choices, and 10 items with a scale of 1-5 [very poor, poor, fair, good, very good]). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.66
Ortho Tri-Cyclen Lo2.83

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Item Satisfaction

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (item satisfaction). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)0.0
Ortho Tri-Cyclen Lo0.1

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Leisure Time Activities

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (leisure time activities - 6 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)2.72
Ortho Tri-Cyclen Lo2.37

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Overall Life Satisfaction and Contentment

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (overall life satisfaction and contentment). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.1
Ortho Tri-Cyclen Lo0.0

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Participant Feeling

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (participant feeling - 14 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-0.44
Ortho Tri-Cyclen Lo0.39

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Physical Health

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (physical health - 13 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.93
Ortho Tri-Cyclen Lo2.13

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - School/Course Work

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (school / course work - yes or no; if yes, then 4 choices, and 10 items with a scale of 1-5 (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-1.97
Ortho Tri-Cyclen Lo4.39

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Social Relationship

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (social relationship - 11 items). 1-5 scale (very poor, poor, fair, good, very good). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)1.01
Ortho Tri-Cyclen Lo1.75

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Mean Change From Baseline to Cycle 13 in Quality of Life Enjoyment and Satisfaction Questionnaire (Q-LES-Q) - Work

Change from Baseline to Cycle 13 in the overall enjoyment and satisfaction experienced during the past week as scored on the Q-LES-Q (work - yes or no; if yes, then 4 choices, and 13 items with a scale of 1-5 [very poor, poor, fair, good, very good]). The normalized score ranges from 0 (worst) to 100 (best). The change in the normalized score ranges from -100 (worst) to 100 (best). (NCT00754065)
Timeframe: Baseline up to Cycle 13 (28 days per Cycle)

InterventionScores on a scale (Mean)
Estradiol Valerate, Dienogest (Natazia, Qlaira, BAY86-5027)-1.38
Ortho Tri-Cyclen Lo-1.71

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Microbiological Success at the Day 4 (EOT)/Exit Visit

Microbiological success was attained if the pre-therapy bacterial pathogens were eradicated 12-48 hours after the last dose. Microbiological success is reported as a percentage. Only one eye (study eye) contributed to the analysis. (NCT00759148)
Timeframe: Day 4

Interventionpercentage of subjects (Number)
Moxifloxacin AF74.5
Vehicle56

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Clinical Cure at the Day 4 (EOT)/Exit Visit

Clinical cure was attained if the sum of the 2 cardinal ocular signs of bacterial conjunctivitis (bulbar conjunctival injection and conjunctival discharge/exudate) was zero (ie, normal or absent) 12-48 hours after the last dose. Clinical cure was reported as a percentage. Only one eye (study eye) contributed to the analysis. (NCT00759148)
Timeframe: Day 4

Interventionpercentage of subjects (Number)
Moxifloxacin AF62.5
Vehicle50.6

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Cohort 2: Tmax and t1/2

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. Tmax is the time to reach Cmax. (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

,
Interventionhr (Median)
Tmaxt1/2
Cohort 2: 1200 mg Linezolid1.16.796
Cohort 2: 600 mg Linezolid1.0836.095

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Cohort 1: Number of Subjects With Adverse Events (AEs) and Serious Adverse Events (SAEs)

All observed or volunteered AEs and SAEs regardless of treatment group or suspected causal relationship to the investigational product(s) were reported. (NCT00795145)
Timeframe: From the time the subject had taken at least one dose of study treatment up to 5 weeks

,,
Interventionparticipants (Number)
AEsSAEs
Cohort 1: 1200 mg Linezolid20
Cohort 1: 900 mg Linezolid30
Cohort 1: Placebo10

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Cohort 1: Time to Reach Maximum Observed Plasma Concentration (Tmax) and Plasma Decay Half-Life (t1/2)

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

,
Interventionhr (Median)
Tmaxt1/2
Cohort 1: 1200 mg Linezolid1.07.1
Cohort 1: 900 mg Linezolid1.06.9

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Cohort 2: AUC Inf and AUC Last

"AUC inf = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time.~AUC last = Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)." (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

,
Interventionug *hr/mL (Mean)
AUC InfAUC Last
Cohort 2: 1200 mg Linezolid328.75299.40
Cohort 2: 900 mg Linezolid141.75129.52

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Cohort 2: Mean Time-Matched Difference in Time Corresponding to Beginning of Depolarization to Repolarization of the Ventricles, Corrected for Heart Rate Using Fridericia's Formula (QTcF Interval) Between Linezolid 600 mg and 1200 mg Compared to Placebo

The time corresponding to the beginning of depolarization to repolarization of the ventricles (QT interval) was adjusted for ventricular rate (VR) using the QT and VR from each electrocardiogram by Fridericia's formula (QTcF = QT divided by cube root of VR in seconds). A measure of dispersion is not available. (NCT00795145)
Timeframe: 0.5, 1, 2, 4, 8, 12, 24 hours post-dose

,,
Interventionmilliseconds (msec) (Number)
0.5 hour1 hour2 hours4 hours8 hours12 hours24 hours
Cohort 2: 1200 mg Linezolid422.34420.89412.30421.92412.25413.45417.27
Cohort 2: 600 mg Linezolid421.31419.71414.27418.85409.75412.99414.83
Cohort 2: Placebo419.84422.67419.80418.45411.13411.98415.47

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Cohort 2: Mean Time-Matched Difference in Uncorrected QT Intervals Between Linezolid 600 mg and 1200 mg Compared to Placebo

A measure of dispersion is not available. (NCT00795145)
Timeframe: 0.5, 1, 2, 4, 8, 12, 24 hours post-dose

,,
Interventionmsec (Number)
0.5 hour1 hour2 hours4 hours8 hours12 hours24 hours
Cohort 2: 1200 mg Linezolid420.60410.06406.76418.40406.40398.96419.06
Cohort 2: 600 mg Linezolid422.60414.80415.40419.66399.66396.56415.80
Cohort 2: Placebo424.08422.25421.15420.58405.30398.85416.38

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Cohort 2: Number of Subjects With AEs and SAEs

All observed or volunteered AEs and SAEs regardless of treatment group or suspected causal relationship to the investigational product(s) were reported. (NCT00795145)
Timeframe: From the time the subject had taken at least one dose of study treatment up to 5 weeks

,,,
Interventionparticipants (Number)
AEsSAEs
Cohort 2: 1200 mg Linezolid70
Cohort 2: 600 mg Linezolid30
Cohort 2: Placebo40
Moxifloxacin 400 mg100

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Cohort 2: Cmax

(NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

Interventionug/mL (Mean)
Cohort 2: 600 mg Linezolid15.06
Cohort 2: 1200 mg Linezolid30.76

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Cohort 2: CL

Drug clearance = Dose / AUC inf (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

InterventionmL/min/kg (Mean)
Cohort 2: 600 mg Linezolid1.2825
Cohort 2: 1200 mg Linezolid1.1000

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Cohort 1: Steady-State Volume of Distribution (Vss)

Vss = (mean residence time [The average total time molecules of a given dose spend in the body] extrapolated to infinity) multiplied by CL (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

InterventionL/kg (Mean)
Cohort 1: 900 mg Linezolid0.6016
Cohort 1: 1200 mg Linezolid0.5776

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Cohort 1: Maximum Observed Plasma Concentration (Cmax)

(NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

Interventionug/mL (Mean)
Cohort 1: 900 mg Linezolid22.3
Cohort 1: 1200 mg Linezolid29.37

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Cohort 1: Clearance of Linezolid (CL)

Drug clearance = Dose / AUC inf (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

InterventionmL/minute (min)/kilogram (kg) (Mean)
Cohort 1: 900 mg Linezolid1.0173
Cohort 1: 1200 mg Linezolid0.8813

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Cohort 2: Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin and Placebo

A measure of dispersion is not available. (NCT00795145)
Timeframe: 0.5, 1, 2, 4, 8, 12, 24 hours post-dose

,
Interventionmsec (Number)
0.5 hour1 hour2 hours4 hours8 hours12 hours24 hours
Cohort 2: Moxifloxacin423.11429.50430.07428.29420.53419.02421.99
Cohort 2: Placebo419.84422.67419.80418.45411.13411.98415.47

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Cohort 1: Area Under the Curve From Time Zero to Extrapolated Infinite Time (AUC Inf) and Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUC Last)

"AUC inf = Area under the plasma concentration versus time curve from time zero (pre-dose) to extrapolated infinite time.~AUC last = Area under the plasma concentration versus time curve from time zero (pre-dose) to time of last quantifiable concentration (0-t)." (NCT00795145)
Timeframe: predose, 30 minutes, and at 1 (end of infusion), 1.5, 2, 3, 4, 6, 8, 12, 24, and 46 hours after start of infusion

,
Interventionmicrogram (ug)*hours (hr)/mL (Mean)
AUC infAUC last
Cohort 1: 1200 mg Linezolid346.89332.26
Cohort 1: 900 mg Linezolid223.49211.26

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Cohort 2: Vss

Vss = (mean residence time [The average total time molecules of a given dose spend in the body] extrapolated to infinity) multiplied by CL (NCT00795145)
Timeframe: Predose, 30 minutes, 1, 2, 4, 8, 12 hours post-dose

InterventionL/kg (Mean)
Cohort 2: 600 mg Linezolid0.6418
Cohort 2: 1200 mg Linezolid0.6185

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The Aqueous Humor Drug Concentration.

An aqueous humor specimen was collected from the study eye for determination of drug concentration 60 min after study drug instillation. (NCT00824070)
Timeframe: Visit 2, 1-14 days following screening visit

Interventionµg/mL (Mean)
Besifloxacin0.1349
Moxifloxacin0.6681
Gatifloxacin0.1251

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

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

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

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

(NCT00864383)
Timeframe: 18 months

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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Number of Participants With the Indicated Type of Adverse Event (AE)

The assessment of safety was based mainly on the frequency of AEs, and summaries of vital signs and laboratory values (values classified as AE are captured in the AE module). An AE is defined as the appearance or worsening of any undesirable sign, symptom, or medical condition occurring after starting the study drug, whether or not the event was considered causally related to the medical product. An AE could have been a new occurrence or an existing process that increased in intensity or frequency. AEs were deemed treatment-emergent if the start date was on or after the date of the first dose but was not present before that date or if the AE started before the date of the first dose and increased in severity on or after that date. (NCT00865280)
Timeframe: from the time of informed consent to Test of Cure (10 to 17 days after end of treatment [total treatment of up to 14 days)

,
InterventionParticipants (Count of Participants)
Treatment-emergent adverse event (TEAE)Study drug-related TEAEAEs leading to study drug discontinuation
Linezolid58410
Omadacycline56412

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The Percentage of Patients With no Ocular Pain

(NCT00870103)
Timeframe: Day 15 after cataract surgery

InterventionPercentage of participants (Number)
Vigadexa Group96.7

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The Percentage of Patients With a Score of Zero for Anterior Chamber Cells.

"The percentage of patients with a score of zero for Anterior chamber cells.~Anterior chamber inflammation was evaluated based on the number of cells per high-power field measured using the narrowest slit beam of the lamp (0.5 at a height of 8mm).~Anterior chamber cells was recorded on a 0-4 point scale,0 = Less than 5 cells; 1 = Mild: 5-10 cells; 2 = Moderate:11-20 cells; 3 = Marked: 21-50 cells; 4 = Severe: Greater than 50 cells / hypopyon" (NCT00870103)
Timeframe: Day 15 after cataract surgery

InterventionPercentage of participants (Number)
Vigadexa Group91.7

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Numbers and % of Subjects With QTcI Change > 30 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 30 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg1
Inhaled Placebo1

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Numbers and % of Subjects With QTcI Change > 60 ms

Numbers and Percents of Subjects with QTcI increase from baseline exceeding 60 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg0
Inhaled Placebo0

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Numbers and % of Subjects With QTcI > 480 ms

Numbers and Percents of Subjects with QTcI exceeding 480 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg0
Inhaled Placebo0

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Numbers and % of Subjects With QTcI > 450 ms

Numbers and Percents of Subjects with QTcI exceeding 450 ms (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

InterventionParticipants (Count of Participants)
Inhaled Loxapine 10 mg1
Inhaled Placebo1

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Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)

A thorough QT/QTc study may be considered to have demonstrated assay sensitivity if 1 or more of the lower 95% CI values exceeds 5 msec ant any of the 9 predetermined time points (NCT00874237)
Timeframe: 1, 1.5, 2, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmseconds (Least Squares Mean)
Oral Moxifloxacin vs Placebo Crossover Subjects8.356

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Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo

Largest of the upper CIs of the time matched differences in QTcI values between the maximum of the mean difference from baseline of the QTcI interval after time matched placebo subtraction for ADASUVE treatment at 12 prespecified post inhalation times (NCT00874237)
Timeframe: 1, 2, 5, 9, 15, 30 min, 1, 3, 6, 10 and 23 hours

Interventionmseconds (Least Squares Mean)
Inhaled Loxapine 10 mg vs Placebo Crossover Subjects5.418

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Cardiac Repolarization Change (QTcI) Versus Loxapine Concentration Relationship Following Treatment With Staccato Loxapine in Healthy Volunteers.

QTcI change at the median loxapine concentration (32.2 mcg/mL) based on nonlinear regression of QTcI versus log of time matched serum loxapine concentrations. This analysis looks for repolarization versus concentration relationship in a positive or negative thorough QT/QTc study result. (NCT00874237)
Timeframe: 24 hours

Interventionmseconds (Least Squares Mean)
Inhaled Loxapine 10 mg4.238

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Percentage of Subjects With Strain Resistance of the Conjunctiva as Determined by Minimum Inhibitory Concentration (MIC) at Day 14

Percentage of subjects with strain resistance as determined by Minimum Inhibitory Concentration (MIC) of the conjunctiva (clear membrane covering the white surface of the eye) at day 14. MIC is the lowest concentration of an antimicrobial that inhibits the visible growth of a microorganism after incubation. The MIC cut-off values include: Intermediate is 1 to less than 2; Resistant is greater than or equal to 2. (NCT00874887)
Timeframe: Day 14

InterventionPercentage of Subjects (Number)
Vigamox®9.4
Zymar®0

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Aqueous Humor Concentration of Study Drug

Patients were randomly assigned to receive one drop of either moxifloxacin or besifloxacin every 10 minutes for a total of 4 doses, with the last dose given 30 minutes prior to the time of the cataract incision. The aqueous humor was corrected through the paracentesis site. The specimen was transferred immediately to a polypropylene tube and stored upright at ≤ 20° C. Moxifloxacin and besifloxacin concentrations in the aqueous humor were determined using a validated high performance liquid chromatography (HPLC)-tandem mass spectrometry method. (NCT00924729)
Timeframe: approximately 3 to 4 months

Interventionµg/ml (Mean)
Moxifloxacin 0.5% Ophthalmic Solution1.6108
Besifloxacin 0.6% Ophthalmic Suspension0.0312

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Serum Concentration of Fasting Glucose

Glucose is one of the IGF-axis related biomarkers. Part of the secondary objectives of the study was to explore the relationships of plasma CP-751,871 concentrations to such biomarkers. Cmax is the mean ± standard deviation (SD) concentration observed at the time of maximal change from baseline. (NCT00926263)
Timeframe: Day 1 pre-dose, 1 hour post dose, Day 2 (24 hours post-dose), Day 8, 15, 22, 29, 43, 57, 71, 85

,
Interventionmg/dL (Mean)
Baselineat Cmax
CP-751,871 10 mg/kg87.7104
CP-751,871 20 mg/kg87.3101

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Anti-drug Antibodies (ADA) Against CP-751,871 in Serum Samples

Number of participants who tested positive for ADA (NCT00926263)
Timeframe: Day 1 pre-dose, Day 15, 29, 57, 85

,
Interventionnumber of participants (Number)
Nominal Day 1Nominal Day 15Nominal Day 29Nominal Day 57Nominal Day 85
CP-751,871 10 mg/kg00000
CP-751,871 20 mg/kg00000

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Serum Concentration of Insulin-like Growth Factor Binding Protein 3 (IGFBP-3)

IGFBP-3 is one of the IGF-axis related biomarkers. Part of the secondary objectives of the study was to explore the relationships of plasma CP-751,871 concentrations to such biomarkers. Cmax is the mean ± standard deviation (SD) concentration observed at the time of maximal change from baseline. (NCT00926263)
Timeframe: Day 1 pre-dose, 1 hour post dose, Day 2 (24 hours post-dose), Day 8, 15, 22, 29, 43, 57, 71, 85

,
Interventionng/mL (Mean)
Baselineat Cmax
CP-751,871 10 mg/kg20414945
CP-751,871 20 mg/kg19785819

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Serum Concentration of Free Insulin-like Growth Factor 1 (IGF-1)

IGF-1 is one of the IGF-axis related biomarkers. Part of the secondary objectives of the study was to explore the relationships of plasma CP-751,871 concentrations to such biomarkers. Cmax is the mean ± standard deviation (SD) concentration observed at the time of maximal change from baseline. (NCT00926263)
Timeframe: Day 1 pre-dose, 1 hour post dose, Day 2 (24 hours post-dose), Day 8, 15, 22, 29, 43, 57, 71, 85

,
Interventionng/mL (Mean)
Baselineat Cmax
CP-751,871 10 mg/kg17.2143
CP-751,871 20 mg/kg13.9168

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Serum Concentration of Insulin

Insulin is one of the IGF-axis related biomarkers. Part of the secondary objectives of the study was to explore the relationships of plasma CP-751,871 concentrations to such biomarkers. Cmax is the mean ± standard deviation (SD) concentration observed at the time of maximal change from baseline. (NCT00926263)
Timeframe: Day 1 pre-dose, 1 hour post dose, Day 2 (24 hours post-dose), Day 8, 15, 22, 29, 43, 57, 71, 85

,
InterventionmIU/mL (Mean)
Baselineat Cmax
CP-751,871 10 mg/kg5.1337.6
CP-751,871 20 mg/kg4.0740.0

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Plasma Decay Half-Life (t1/2)

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. (NCT00926263)
Timeframe: Day 1 pre-dose and 1 hour post-dose, Day 2 (24 hours post-dose), 8, 15, 22, 29, 43, 57, 71 and 85

Interventiondays (Mean)
CP-751,871 10 mg/kg21.08
CP-751,871 20 mg/kg27.75

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Plasma Clearance (CL)

Clearance of a drug is a measure of the rate at which a drug is metabolized or eliminated by normal biological processes. (NCT00926263)
Timeframe: Day 1 pre-dose and 1 hour post-dose, Day 2 (24 hours post-dose), 8, 15, 22, 29, 43, 57, 71 and 85

InterventionmL/day/kg (Mean)
CP-751,871 10 mg/kg2.808
CP-751,871 20 mg/kg2.353

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Maximum Observed Plasma Concentration (Cmax)

(NCT00926263)
Timeframe: Day 1 pre-dose and 1 hour post-dose, Day 2 (24 hours post-dose), 8, 15, 22, 29, 43, 57, 71 and 85

Interventionmg/L (Mean)
CP-751,871 10 mg/kg225.1
CP-751,871 20 mg/kg420.6

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

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast) (NCT00926263)
Timeframe: Day 1 pre-dose and 1 hour post-dose, Day 2 (24 hours post-dose), 8, 15, 22, 29, 43, 57, 71 and 85

Interventionmg*h/L (Mean)
CP-751,871 10 mg/kg80740
CP-751,871 20 mg/kg184000

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Apparent Volume of Distribution (Vz)

Volume of distribution is defined as the theoretical volume in which the total amount of drug would need to be uniformly distributed to produce the desired plasma concentration of a drug. (NCT00926263)
Timeframe: Day 1 pre-dose and 1 hour post-dose, Day 2 (24 hours post-dose), 8, 15, 22, 29, 43, 57, 71 and 85

InterventionmL/kg (Mean)
CP-751,871 10 mg/kg84.89
CP-751,871 20 mg/kg92.17

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Serum Concentration of Insulin-like Growth Factor 1 (IGF-1)

IGF-1 is one of the IGF-axis related biomarkers. Part of the secondary objectives of the study was to explore the relationships of plasma CP-751,871 concentrations to such biomarkers. Cmax is the mean ± standard deviation (SD) concentration observed at the time of maximal change from baseline. (NCT00926263)
Timeframe: Day 1 pre-dose (Baseline), 1 hour post dose, Day 2 (24 hours post-dose), Day 8, 15, 22, 29, 43, 57, 71, 85

,
Interventionng/mL (Mean)
Baselineat Cmax
CP-751,871 10 mg/kg138566
CP-751,871 20 mg/kg128610

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Serum Concentration of Insulin-like Growth Factor 2 (IGF-2)

IGF-2 is one of the IGF-axis related biomarkers. Part of the secondary objectives of the study was to explore the relationships of plasma CP-751,871 concentrations to such biomarkers. Cmax is the mean ± standard deviation (SD) concentration observed at the time of maximal change from baseline. (NCT00926263)
Timeframe: Day 1 pre-dose, 1 hour post dose, Day 2 (24 hours post-dose), Day 8, 15, 22, 29, 43, 57, 71, 85

,
Interventionng/mL (Mean)
Baselineat Cmax
CP-751,871 10 mg/kg15502039
CP-751,871 20 mg/kg14761909

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Area Under the Concentration-Time Curve in 1 Dosing Interval of Norgestrel

Norgestrel was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. AUC(TAU) was measured in picograms multiplied by hours (h) per milliliter (pg*h/mL) and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionpg*h/mL (Geometric Mean)
Ortho Tri-Cyclen47258.35
Ortho Tri-Cyclen + Daclatasvir51760.43

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Area Under the Concentration-Time Curve in 1 Dosing Interval of Norelgestromin

Norelgestromin was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. AUC(TAU) was measured in nanograms multiplied by hours (h) per milliliter (ng*h/mL) and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionng*h/mL (Geometric Mean)
Ortho Tri-Cyclen15.38
Ortho Tri-Cyclen + Daclatasvir16.84

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Maximum Observed Plasma Concentration of Norelgestromin

Norelgestromin is a major active metabolite of norgestimate (NGM) which is found in Ortho Tri-Cyclen. Norelgestromin was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. Cmax was measured in nanograms per milliliter (ng/mL) and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionnanogram per millilitre (ng/mL) (Geometric Mean)
Ortho Tri-Cyclen1.99
Ortho Tri-Cyclen + Daclatasvir2.10

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Number of Participants Demonstrating a Clinically Meaningful Effect in Vital Signs

Vital Signs were measured after the participant was seated quietly for at least 5 minutes and included systolic and diastolic blood pressure, heart rate, respiratory rate, and temperature. Baseline = Last non-missing pretreatment value. (NCT00983957)
Timeframe: Baseline, Day 28, Day 29, Day 67, Day 68, Day 78, Day of discharge

Interventionparticipants (Number)
Ortho Tri-Cyclen0
Ortho Tri-Cyclen + Daclatasvir0

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Maximum Observed Plasma Concentration (Cmax) of Ethinyl Estradiol

Ethinyl Estradiol is an analyte of Ortho Tri-Cyclen. Ethinyl Estradiol was measured in plasma, using liquid chromatography-tandem mass spectrometry (LC-MS/MS) by a validated analytical method during the period of known analyte stability. Cmax was measured in picograms per milliliter (pg/mL) and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 hours post-dose on Days 49 and 77

Interventionpicogram per millilitre (pg/mL) (Geometric Mean)
Ortho Tri-Cyclen118.53
Ortho Tri-Cyclen + Daclatasvir134.70

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Number of Participants With Serious Adverse Events (SAEs), Adverse Events (AEs) Leading to Discontinuation, and Who Died

AE=any new unfavorable symptom, sign, or disease or worsening of a preexisting condition that may not have a causal relationship with treatment. SAE=a medical event that at any dose results in death, persistent or significant disability/incapacity, or drug dependency/abuse; is life-threatening, an important medical event, or a congenital anomaly/birth defect; or requires or prolongs hospitalization. (NCT00983957)
Timeframe: For AEs from start of treatment (Day 1) up to Day 78 or discharge and for SAEs from Day 1 to 30 days after last dose of study drug

,
Interventionparticipants (Number)
SAEAE Leading to DiscontinuationDeath
Ortho Tri-Cyclen000
Ortho Tri-Cyclen + Daclatasvir010

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Number of Participants With Laboratory Test Abnormalities

Laboratory marked abnormalities were defined as Hematocrit (low) as <0.85*Pre-treatment (PreRx), Hemoglobin (low) as <0.85*PreRx, Aspartate Aminotransferase (AST) (high) as >1.25*PreRx if PreRx > upper limits of normal (ULN); >1.25*ULN if PreRx <=ULN; >1.25*ULN if PreRx = Missing, Blood in urine (high) as ≥2 PreRx if PreRx ≥1; ≥2 if PreRx <1; ≥2 if PreRx = Missing. (NCT00983957)
Timeframe: From start of treatment (Day 1) up to Day 78 or discharge

,
Interventionparticipants (Number)
HematocritHemoglobinASTBlood in Urine
Ortho Tri-Cyclen1110
Ortho Tri-Cyclen + Daclatasvir0001

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Area Under the Concentration-Time Curve (AUC) in 1 Dosing Interval of Ethinyl Estradiol

Ethinyl Estradiol was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. AUC(TAU) was measured in picograms multiplied by hours (h) per milliliter (pg*h/mL) and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionpg*h/mL (Geometric Mean)
Ortho Tri-Cyclen959.37
Ortho Tri-Cyclen + Daclatasvir994.40

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Time of Maximum Observed Plasma Concentration of Norgestrel

Norgestrel was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. Tmax was measured in hours (h), and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionhours (Median)
Ortho Tri-Cyclen1.8
Ortho Tri-Cyclen + Daclatasvir2.0

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Time of Maximum Observed Plasma Concentration of Norelgestromin

Norelgestromin was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. Tmax was measured in hours (h), and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionhours (Median)
Ortho Tri-Cyclen1.3
Ortho Tri-Cyclen + Daclatasvir1.5

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Time of Maximum Observed Plasma Concentration of Ethinyl Estradiol

Ethinyl Estradiol was measured in plasma, using liquid chromatography-tandem mass spectrometry by a validated analytical method during the period of known analyte stability. Tmax was measured in hours (h), and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionhours (Median)
Ortho Tri-Cyclen1.5
Ortho Tri-Cyclen + Daclatasvir1.5

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Number of Participants Demonstrating a Clinically Meaningful Effect in ECG Parameters

The electrocardiogram (ECG) evaluations were performed within ± 15 minutes of the relative time points. ECGs were recorded after the participants were in supine position for at least 5 minutes. ECG parameters measured were: PR interval, QRS complex, QT interval and corrected QT (QTc). (NCT00983957)
Timeframe: Screening, Day 1, Day 67, Day 77

Interventionparticipants (Number)
Ortho Tri-Cyclen0
Ortho Tri-Cyclen + Daclatasvir0

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Maximum Observed Plasma Concentration of Norgestrel

Norgestrel is an NGM metabolite and was measured in plasma using liquid chromatography-mass spectrometry by a validated analytical method during the period of known analyte stability. Cmax was measured in picograms per milliliter (pg/mL) and derived from 24 hour plasma concentration versus time data using non-compartmental methods. Pre-dose concentrations and concentrations prior to the first quantifiable concentration that were below the lower limit of quantitation were treated as missing. (NCT00983957)
Timeframe: Pre-dose, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 24 h post-dose on Days 49 and 77

Interventionpg/mL (Geometric Mean)
Ortho Tri-Cyclen2674.69
Ortho Tri-Cyclen + Daclatasvir2815.98

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Area Under Concentration (AUC) During Cycle 1

The area under the concentration versus time curve from time 0 to infinity [AUC(0-inf)] is reported during Cycle 1 (1 cycle=21 days). (NCT01017731)
Timeframe: Cycle 1 [2.25 hours (h), 3.25 h, 4.25 h, 72 h, 168 h, 336 h postdose]

Interventionhours*micrograms/milliliter (h*mcg/mL) (Geometric Mean)
IMC-1121B (Ramucirumab)67400

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Maximum Concentration (Cmax) During Cycle 3

The maximum observed serum concentration of IMC-1121B (ramucirumab) at steady state (Cmax,ss) during Cycle 3 (1 cycle=21 days). (NCT01017731)
Timeframe: Cycle 3 [predose and 1.25 hours (h), 2.25 h, 3.25 h, 4.25 h, 72 h, 168 h, 336 h, and 504 h postdose]

Interventionmicrograms per milliliter (mcg/mL) (Geometric Mean)
IMC-1121B (Ramucirumab)571

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Maximum Concentration (Cmax) During Cycle 1

Maximum observed concentration of IMC-1121B (ramucirumab) in serum during Cycle 1 (1 cycle=21 days). (NCT01017731)
Timeframe: Cycle 1 [2.25 hours (h), 3.25 h, 4.25 h, 72 h, 168 h, 336 h postdose]

Interventionmicrograms per milliliter (mcg/mL) (Geometric Mean)
IMC-1121B (Ramucirumab)485

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Area Under Concentration (AUC) During Cycle 3

The area under the concentration versus time curve over the dosing interval at steady state [AUC(tau,ss)] is reported during Cycle 3 (1 cycle=21 days). (NCT01017731)
Timeframe: Cycle 3 [predose and 1.25 hours (h), 2.25 h, 3.25 h, 4.25 h, 72 h, 168 h, 336 h, and 504 h postdose]

Interventionhours*micrograms/milliliter (h*mcg/mL) (Geometric Mean)
IMC-1121B (Ramucirumab)69900

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Change From Baseline to Cycle 3 in QT/Corrected QT (QTc) Interval Prolongation in Participants

All electrocardiogram (ECG) tests were performed in triplicate prior to ramucirumab treatment. QT is the interval between the Q and T waves and QTc is the QT corrected for heart rate using Fridericia's formula: QTc = QT/RR^0.33 where RR is the interval between 2 R waves. Each participant's mean QT/QTc value was calculated for each ECG test during Cycle 3 and compared to his/her mean pretreatment QT/QTc value. The greatest change from baseline during Cycle 3 was reported. QTc prolongation is defined as a QTc exceeding 10 milliseconds (msec) with a lower 90% confidence interval (CI) exceeding 5 msec at any postdose time points per the International Conference on Harmonization (ICH) E14 guidelines for non-thorough QT studies (ICH 2005; ICH 2008). Least squares (LS) mean was calculated using a linear mixed model for repeated measures (MMRM) and adjusted for serum concentration. (NCT01017731)
Timeframe: Baseline, Cycle 3 (1 cycle=21 days)

Interventionmilliseconds (msec) (Least Squares Mean)
IMC-1121B (Ramucirumab)3.9132

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Maximum Plasma Concentration (Cmax)

The maximum or peak concentration that colchicine reaches in the plasma. (NCT01018420)
Timeframe: serial pharmacokinetic blood samples collected pre-dose and 1 (prior to second dose), 3 (prior to fourth dose), 6 (prior to final dose), 6.17, 6.33, 6.5, 6.75, 7, 7.25, 7.5, 7.75, 8, 10, 12, 23, 36, 48, 72 and 96 hours post-dose

Interventionng/mL (Mean)
Colchicine6.84

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Electrocardiogram (ECG) Evaluation of the QTcF Interval (Moxifloxacin)

The QT interval assesses cardiac repolarization and risk for arrhythmias. It is a measure of the time between the start of the Q wave and the end of the T wave in the heart's electrical cycle. It is dependent on heart rate and is corrected (c) to aid interpretation via Fridericia's adjustment (F), and is reported as QTcF. (NCT01018420)
Timeframe: 24 hours - measured 0.5 hr prior to dose (baseline), then 1, 3, 6, 7, 8, 10, 12, and 23 hours after dose

Interventionmilliseconds (Mean)
Baseline402.11
Hour 1398.89
Hour 3403.67
Hour 6397.00
Hour 7397.89
Hour 8397.44
Hour 10402.67
Hour 12405.22
Hour 23416.00

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Electrocardiogram (ECG) Evaluation of the QTcF Interval (Colchicine)

The QT interval assesses cardiac repolarization and risk for arrhythmias. It is a measure of the time between the start of the Q wave and the end of the T wave in the heart's electrical cycle. It is dependent on heart rate and is corrected (c) to aid interpretation via Fridericia's adjustment (F), and is reported as QTcF. (NCT01018420)
Timeframe: 24 hours - measured 0.5 hr prior to first dose (baseline), then 1, 3, 6, 7, 8, 10, 12, and 23 hours after first dose

Interventionmilliseconds (Mean)
Baseline401.62
Hour 1397.80
Hour 3401.76
Hour 6394.73
Hour 7388.84
Hour 8393.93
Hour 10396.02
Hour 12396.89
Hour 23399.36

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

The area under the plasma concentration versus time curve, from time 0 to the time of the last measurable concentration (t), as calculated by the linear trapezoidal rule. (NCT01018420)
Timeframe: serial pharmacokinetic blood samples collected pre-dose and 1 (prior to second dose), 3 (prior to fourth dose), 6 (prior to final dose), 6.17, 6.33, 6.5, 6.75, 7, 7.25, 7.5, 7.75, 8, 10, 12, 23, 36, 48, 72 and 96 hours post-dose

Interventionng-hr/mL (Mean)
Colchicine104.95

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Area Under the Concentration Versus Time Curve From Time 0 Extrapolated to Infinity [AUC(0-∞)]

The area under the plasma concentration versus time curve from time 0 to infinity. AUC(0-∞) was calculated as the sum of AUC(0-t) plus the ratio of the last measurable plasma concentration to the elimination rate constant. (NCT01018420)
Timeframe: serial pharmacokinetic blood samples collected pre-dose and 1 (prior to second dose), 3 (prior to fourth dose), 6 (prior to final dose), 6.17, 6.33, 6.5, 6.75, 7, 7.25, 7.5, 7.75, 8, 10, 12, 23, 36, 48, 72 and 96 hours post-dose

Interventionng-hr/mL (Mean)
Colchicine118.20

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QT Interval Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3

"The QT interval is the period that extends from the beginning of ventricular depolarization until the end of ventricular repolarization. N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
Interventionmilliseconds (Mean)
Day 1: Pre-dose (N= 298, 150)Change at Day 1 (N= 290, 148)Day 3: Pre-dose (N= 292, 146)Change at Day 3 (N= 287, 146)
Comparator Ertapenem344.23331.1149356.58223.1644
Moxifloxacin (Avelox, BAY12-8039)341.18122.5828358.30826.0906

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QRS Interval Changes in Electrocardiogram (ECG) Profiles From Predose to Post-dose on Treatment Day 1 and Treatment Day 3

"The QRS interval represents the time it takes for ventricular depolarization to occur. N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
Interventionmilliseconds (Mean)
Day 1: Pre-dose (N= 300, 150)Change at Day 1 (N= 294, 148)Day 3: Pre-dose (N= 293, 146)Change at Day 3 (N= 289, 146)
Comparator Ertapenem88.80671.22389.39040.2877
Moxifloxacin (Avelox, BAY12-8039)89.03330.11989.24230.2768

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PR Interval Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3

"The PR interval is defined as the period that extends from the onset of atrial depolarization (beginning of the P wave) until the onset of ventricular depolarization. N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
Interventionmilliseconds (Mean)
Day 1: Pre-dose (N= 299, 150)Change at Day 1 ( N= 292, 148)Day 3: Pre-dose (N= 293, 146)Change at Day 3 (N= 289, 146)
Comparator Ertapenem140.5933-0.0203139.56851.5616
Moxifloxacin (Avelox, BAY12-8039)136.82940.7123139.49151.5813

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Potentially Clinically Significant Electrocardiogram (ECG) QTc Interval Prolongation - by QTc Interval Calc Fridericia Correction on Treatment Day 1 and During Therapy Day 3

"A significant QTc prolongation was considered when the QTc value was more than (>) upper limit of normal (ULN) range or was prolonged for 30 msec or 60msec in comparison with the pre-treatment value measured on Day 1. N signifies subjects who were evaluable for the specified parameter for each arm, respectively. Percentage of subjects with potentially clinically significant ECG data was reported." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
InterventionPercentage of subjects (Number)
Day1: Pre-dose QTcCalcFridericia>ULN (N= 300, 150)Day1: Post-dose QTcCalcFridericia>ULN (N= 297,148)Day1: Post-dose >30 ms from pre-dose (N= 297,148)Day1: Post-dose >60 ms from pre-dose (N= 297,148)Day3: Pre-dose QTcCalcFridericia>ULN (N= 293, 146)Day3: Post-dose QTcCalcFridericia>ULN (N= 291,148)Day3: Post-dose >30 ms from pre-dose (N= 291,148)Day3: Post-dose >60 ms from pre-dose (N= 291,148)
Comparator Ertapenem1.32001.41.43.40.7
Moxifloxacin (Avelox, BAY12-8039)0.7320.31.49.617.91.7

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Bacteriological Response at the End of Treatment (EOT) Visit

Bacteriological response at EOT were grades as presumed persistence, presumed eradication or indeterminate. 'presumed persistence' was applicable for subjects judged to be clinical failures and appropriate culture material is not available for evaluation; 'presumed eradication' defined as the absence of appropriate culture material for evaluation because the subject has clinically responded (with a response as a resolution or cure) and invasive procedures are not warranted; 'indeterminate' is applicable when the bacteriological response to the study drug was not valid for any reason (eg, pretreatment culture was negative or culture was not obtained when material was available and the subject was not judged a clinical failure). Percentage of subjects with bacteriological response at EOT were reported. (NCT01069900)
Timeframe: Day 5 to Day 14

,
InterventionPercentage of subjects (Number)
Presumed PersistencePresumed EradicationIndeterminate
Comparator Ertapenem0.797.81.5
Moxifloxacin (Avelox, BAY12-8039)5.591.13.4

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Potentially Clinically Significant Electrocardiogram (ECG) QTc Interval Prolongation - by QTc Calc Bazett Correction on Treatment Day 1 and During Therapy Day 3

"A significant QTc prolongation was considered when the QTc value was more than ULN range or was prolonged for 30 msec or 60msec in comparison with the pre-treatment value measured on Day 1. N signifies subjects who were evaluable for the specified parameter for each arm, respectively. Percentage of subjects with potentially clinically significant ECG data was reported." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
InterventionPercentage of subjects (Number)
Day1: Pre-dose QTc Calc Bazett > ULN (N= 300, 150)Day1: Post-dose QTc Calc Bazett > ULN (N= 297,148)Day1: Post-dose >30 ms from pre-dose (N= 297,148)Day1: Post-dose >60 ms from pre-dose (N= 297,148)Day3: Pre-dose QTc Calc Bazett > ULN (N= 293, 146)Day3: Post-dose QTc Calc Bazett > ULN (N= 291,148)Day3: Post-dose >30 ms from pre-dose (N= 291,148)Day3: Post-dose >60 ms from pre-dose (N= 291,148)
Comparator Ertapenem2.74.1001.43.420.7
Moxifloxacin (Avelox, BAY12-8039)7.716.25.403.815.59.60.7

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Number of Subjects With Adverse Events

An adverse event (AE) was any untoward medical occurrence in a subject who received study drug without regard to possibility of causal relationship. An serious adverse event (SAE) was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. (NCT01069900)
Timeframe: All AEs and SAE were recorded from treatment start to test of cure visit; musculoskeletal AEs were recorded up to 1 year post-end of treatment (EOT) visit; subjects with musculoskeletal AEs 1 year after EOT were followed up to 5 years or until resolution.

,
InterventionSubjects (Number)
Any AEAny SAE
Comparator Ertapenem826
Moxifloxacin (Avelox, BAY12-8039)17520

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Bacteriological Response at Test-of-Cure (TOC) Visit

"Bacteriological responses were graded as presumed persistence, presumed eradication or indeterminate.~'Presumed persistence' was applicable for subjects judged to be clinical failures, and appropriate culture material is not available for evaluation; 'presumed eradication' defined as the absence of appropriate culture material for evaluation because the subject has clinically responded and invasive procedures are not warranted; índeterminate' was applicable when the bacteriological response to the study drug was not valid for any reason (eg, pre-treatment culture was negative or culture was not obtained when material was available and the subject was not judged a clinical failure). Percentage of subjects with bacteriological response at TOC were reported." (NCT01069900)
Timeframe: 28 to 42 days

,
InterventionPercentage of subjects (Number)
Presumed PersistencePresumed EradicationIndeterminate
Comparator Ertapenem2.294.92.9
Moxifloxacin (Avelox, BAY12-8039)6.884.78.4

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Bacteriological Response at a 'During Therapy' Visit

Bacteriological response during therapy were graded as presumed persistence, presumed eradication, or indeterminate'Presumed persistence' is applicable for subjects judged to be clinical failures and appropriate culture material is not available for evaluation;'presumed eradication' is defined as the absence of appropriate culture material for evaluation because the subject has clinically responded (with a response as a resolution or cure) and invasive procedures are not warranted; 'indeterminate is applicable when the bacteriological response to the study drug is not valid for any reason (eg, pretreatment culture was negative or culture was not obtained when material was available and the subject is not judged a clinical failure). Percentage of subjects with bacteriological response during therapy visit were reported (NCT01069900)
Timeframe: Day 3 to Day 5

,
InterventionPercentage of subjects (Number)
Presumed PersistencePresumed EradicationIndeterminate
Comparator Ertapenem0.797.81.5
Moxifloxacin (Avelox, BAY12-8039)1.295.63.2

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Number of Subjects With Musculoskeletal Adverse Events

(NCT01069900)
Timeframe: All AEs and SAE were recorded from treatment start to test of cure visit; musculoskeletal AEs were recorded up to 1 year post-end of treatment (EOT) visit; subjects with musculoskeletal AEs 1 year after EOT were followed up to 5 years or until resolution.

,
InterventionSubjects (Number)
Any AEAny SAE
Comparator Ertapenem50
Moxifloxacin (Avelox, BAY12-8039)131

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Number of Subjects With Clinical Cardiac Adverse Events

(NCT01069900)
Timeframe: Clinical cardiac event related to QT interval were recorded from treatment start until day 3 of treatment. All other clinical cardiac events were recorded from treatment start to test of cure visit, up to day 56.

,
InterventionSubjects (Number)
Any AEAny SAE
Comparator Ertapenem70
Moxifloxacin (Avelox, BAY12-8039)380

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Incidence Rates of Musculoskeletal Adverse Events by Primary System Organ Class (SOC) and Preferred Term

"Musculoskeletal adverse events were classified as following SOCs (preferred terms): injury, poisoning and procedural complications (forearm fracture, joint injury, ligament sprain, muscle strain) musculoskeletal and connective tissue disorders (arthralgia, joint swelling, musculoskeletal pain, myalgia). Incidence rates were reported as percentage of subjects categorized under preferred terms." (NCT01069900)
Timeframe: All AEs and SAE were recorded from treatment start to test of cure visit; musculoskeletal AEs were recorded up to 1 year post-end of treatment (EOT) visit; subjects with musculoskeletal AEs 1 year after EOT were followed up to 5 years or until resolution.

,
InterventionPercentage of subjects (Number)
Forearm fractureJoint injuryLigament sprainMuscle strainArthralgiaJoint swellingMusculoskeletal painMyalgia
Comparator Ertapenem00.70.70.71.30.700
Moxifloxacin (Avelox, BAY12-8039)0.300.303010.3

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Heart Rate Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3

"N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
InterventionBeats per minute (bpm) (Mean)
Day 1: Pre-dose (N= 300, 150)Change at Day 1 ((N= 294, 148)Day 3: Pre-dose (N= 293, 146)Change at Day 3 (N= 290, 146)
Comparator Ertapenem90.40.382.6-0.9
Moxifloxacin (Avelox, BAY12-8039)93.42.884.31

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Corrected QT (QTc) Interval Calculated (Calc) Fridericia Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3

"QTc interval Calc Fridericia represent the interval corrected for heart rate (QTc) msec which was calculated by Fridericia's method. N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
Interventionmilliseconds (Mean)
Day 1: Pre-dose (N= 298, 150)Change at Day 1 (N= 290, 148)Day 3: Pre-dose (N= 292, 146)Change at Day 3 (N= 287, 146)
Comparator Ertapenem390.94671.9122392.69181.774
Moxifloxacin (Avelox, BAY12-8039)391.18467.0724397.37678.115

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Corrected QT (QTc) Interval Calculated (Calc) Bazett Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3

"QTc interval Calc Bazett represent the interval corrected for heart rate (QTc) milliseconds (msec) which was calculated by Bazett's method. N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
Interventionmilliseconds (Mean)
Day 1: Pre-dose (N= 298, 150)Change at Day 1 (N= 290, 148)Day 3: Pre-dose (N= 292, 146)Change at Day 3 (N= 287, 146)
Comparator Ertapenem417.342.2905412.79451
Moxifloxacin (Avelox, BAY12-8039)419.58729.731419.20559.2509

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Clinical Response at the End-of-Treatment (EOT) Visit

Clinical responses at EOT were graded as resolution, failure, or indeterminate. 'Resolution' defined as a disappearance of signs and symptoms related to the infection or sufficient improvement of clinical signs and symptoms related to the infection and the subject does not require any further antibiotic therapy or surgical intervention; 'failure' defined as worsening or insufficient lessening of the signs and symptoms of infection requiring a modification or addition of antibacterial therapy; 'indeterminate' is defined as those subjects in whom a clinical assessment is not possible to determine (eg, due to early withdrawal from the study because of adverse events, protocol violation, withdrawn consent; receipt of less than 3 full days of study drug; receipt of an effective concomitant antibacterial for an indication other than study indication; etc). Percentage of subjects with clinical response at EOT were reported. (NCT01069900)
Timeframe: Day 5 to Day 14

,
InterventionPercentage of subjects (Number)
ResolutionClinical FailureIndeterminate
Comparator Ertapenem980.71.4
Moxifloxacin (Avelox, BAY12-8039)92.24.63.2

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Clinical Response at Test-of-Cure (TOC) Visit in Subjects With Bacteriologically Confirmed Complicated Intra-abdominal Infection (cIAI)

Clinical responses were graded as clinical cure, failure or indeterminate. 'Clinical cure' defined as a resolution or sufficient improvement of clinical signs and symptoms related to the infection; 'failure' defined as a reappearance of the signs and symptoms of the original infection, or wound infection requiring further systemic antimicrobial therapy; 'indeterminate' defined as those subjects in whom a clinical assessment was not possible to determine (due to early withdrawal from the study because of adverse events, protocol violation, withdrawn consent). Percentage of subjects with clinical response at TOC were reported (NCT01069900)
Timeframe: 28 to 42 days

,
InterventionPercentage of subjects (Number)
Clinical CureClinical FailureIndeterminate
Comparator Ertapenem95.322.7
Moxifloxacin (Avelox, BAY12-8039)86.25.78.1

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Clinical Response at Test-of-Cure (TOC) Visit

Clinical responses were graded as clinical cure, failure or indeterminate. 'Clinical cure' defined as a resolution or sufficient improvement of clinical signs and symptoms related to the infection; 'failure' defined as a reappearance of the signs and symptoms of the original infection, or wound infection requiring further systemic antimicrobial therapy; 'indeterminate' defined as those subjects in whom a clinical assessment was not possible to determine (due to early withdrawal from the study because of adverse events, protocol violation, withdrawn consent). Percentage of subjects with clinical response at TOC were reported. (NCT01069900)
Timeframe: 28 to 42 days

,
InterventionPercentage of subjects (Number)
Clinical CureClinical FailureIndeterminate
Comparator Ertapenem95.322.7
Moxifloxacin (Avelox, BAY12-8039)86.25.78.1

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Clinical Response at a 'During Therapy' Visit

"Clinical responses during therapy visit were graded as clinical improvement, clinical failure, or indeterminate. Clinical improvement defined as a reduction in the severity and/or the number of signs and symptoms of infection; 'clinical failure' defined as a failure to respond or insufficient lessening of the signs and symptoms of infection requiring a modification or addition of antibacterial therapy.~'Indeterminate' defined as those subjects in whom a clinical assessment is not possible to determine (eg, due to early withdrawal from the study because of adverse events, protocol violation, withdrawn consent, receipt of an effective concomitant antibacterial for an indication other than the study indication and receipt of less than 3 full days of study drug, etc). Percentage of subjects with clinical response during therapy visit were reported." (NCT01069900)
Timeframe: Day 3 to Day 5

,
InterventionPercentage of subjects (Number)
Clinical ImprovementClinical FailureIndeterminate
Comparator Ertapenem980.71.4
Moxifloxacin (Avelox, BAY12-8039)94.314.7

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RR Interval Changes in Electrocardiogram (ECG) Profiles From Pre-dose to Post-dose on Treatment Day 1 and Treatment Day 3

"The RR interval refers to the respective time interval in the Electrocardiogram. N signifies subjects who were evaluable for the specified parameter for each arm, respectively." (NCT01069900)
Timeframe: Baseline (Pre-dose), Day 1, Day 3

,
Interventionmilliseconds (Mean)
Day 1: Pre-dose (N= 300, 150)Change at Day 1 (N= 294, 148)Day 3: Pre-dose (N= 293, 146)Change at Day 3 (N= 290, 146)
Comparator Ertapenem689.3067-3.4797754.602710.5137
Moxifloxacin (Avelox, BAY12-8039)670.7567-20.6429740.4778-9.2862

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The Average Differences From Baseline Between Moxifloxacin and Placebo by Fridericia's Corrected Interval (QTcF) on Day 6 and Day 13

"QT and RR data were determined for each of 4 ECGs over an approximate 10-minute interval at each nominal time point. The average QT and QTc (interval corrected for heart rate) data from the replicate ECGs at each nominal time point were calculated. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected by Fridericia's method (QTcF) msec." (NCT01148537)
Timeframe: Baseline to Day 6 and Day 13

,
InterventionQTcF (msec) (Least Squares Mean)
QTcF Day 6QTcF Day 13
Moxifloxacin4.742.83
Placebo-2.12-1.85

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The Average Differences From Baseline Between BTDS and Placebo by Fridericia's Corrected Interval (QTcF) on Day 6 and Day 13

"QT and RR data were determined for each of 4 ECGs over an approximate 10-minute interval at each nominal time point. The average QT and QTc (interval corrected for heart rate) data from the replicate ECGs at each nominal time point were calculated. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected by Fridericia's method (QTcF) msec." (NCT01148537)
Timeframe: Baseline to Day 6 and Day 13

,
InterventionQTcF (msec) (Least Squares Mean)
QTcF Day 6QTcF Day 13
BTDS-1.044.13
Placebo-2.33-1.88

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The Average Differences From Baseline Between BTDS and Placebo by Bazett Corrected QT Interval (QTcB) on Day 6 and Day 13

"QT and RR data were determined for each of 4 ECGs over an approximate 10-minute interval at each nominal time point. The average QT and QTc (QT interval corrected for heart rate) data from the replicate ECGs at each nominal time point were calculated. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected by Bazett's method (QTcB) msec." (NCT01148537)
Timeframe: Baseline to Day 6 and Day 13

,
InterventionQTcB (msec) (Least Squares Mean)
QTcB Day 6QTcB Day 13
BTDS-0.376.31
Placebo-0.24-0.86

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The Comparison of Moxifloxacin to Placebo Transdermal System (TDS): the Average Difference From Baseline Using QT Interval Corrected From Within-subject Data (QTci) on Day 13

"Observed time from start of the QRS complex to end of the T wave (QT), and the time between the 2 R waves (RR) data for each of 4 electrocardiographs (ECGs) over an approximate 10-minute interval at each nominal time point. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected from within-subject data (QTci) msec." (NCT01148537)
Timeframe: Baseline to Day 13

InterventionQTci (msec) (Least Squares Mean)
Moxifloxacin4.17
Placebo-1.69

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The Comparison of BTDS to Placebo Transdermal System (TDS): the Average Difference From Baseline Using QT Corrected From Within-subject Data (QTci) on Day 13

"Observed time from start of the QRS complex to end of the T wave (QT), and the time between the 2 R waves (RR) data for each of 4 electrocardiographs (ECGs) over an approximate 10-minute interval at each nominal time point. The average QT and QTc data over the 2 pretreatment days were used as the baseline.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected from within-subject data (QTci) msec." (NCT01148537)
Timeframe: Baseline to Day 13

InterventionQTci (msec) (Least Squares Mean)
BTDS4.20
Placebo-1.71

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The Average Differences Between Moxifloxacin vs Placebo From Baseline by Interval Corrected From Within-subject Data (QTci) on Day 6

"QT and RR data were determined for each of 4 ECGs over an approximate 10-minute interval at each nominal time point. The average QT and QTc data from the replicate ECGs at each nominal time point were calculated. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected from within-subject data (QTci) msec." (NCT01148537)
Timeframe: Baseline to Day 6

InterventionQTci (msec) (Least Squares Mean)
Moxifloxacin6.26
Placebo-1.38

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The Average Differences Between BTDS vs Placebo From Baseline by Interval Corrected From Within-subject Data (QTci) on Day 6

"QT and RR data were determined for each of 4 ECGs over an approximate 10-minute interval at each nominal time point. The average QT and QTc data from the replicate ECGs at each nominal time point were calculated. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected from within-subject data (QTci) msec." (NCT01148537)
Timeframe: Baseline to Day 6

InterventionQTci (msec) (Least Squares Mean)
BTDS-1.06
Placebo-1.46

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The Average Differences From Baseline Between Moxifloxacin and Placebo of Bazett Corrected QT Interval (QTcB) on Day 6 and Day 13

"QT and RR data were determined for each of 4 ECGs over an approximate 10-minute interval at each nominal time point. The average QT and QTc data from the replicate ECGs at each nominal time point were calculated. The average QT and QTc data over the 2 pretreatment days were used as the baseline QT and QTc values.~Observed time from start of the QRS complex to end of the T wave (QT); interval corrected for heart rate (QTc) msec; interval corrected by Bazett's method (QTcB) msec." (NCT01148537)
Timeframe: Baseline to Day 6 and Day 13

,
InterventionQTcB (msec) (Least Squares Mean)
QTcB Day 6QTcB Day 13
Mofloxacin8.136.55
Placebo-0.09-0.84

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Change From Baseline in QTcI for MAP0004 3.0mg and Placebo at 30 Minutes

The corrected QT interval, individualized (QTcI) is a measurement of the electrical impulses through the largest part of the heart muscle individualized for subject pre-dose values. A negative change is a shortening of the QTc interval, a positive change is a lengthening of the QTc interval. (NCT01191723)
Timeframe: baseline and 30 minutes

,
Interventionmilliseconds (Mean)
BaselineChange from Baseline at 30 mins
Treatment B (MAP0004 3.0mg)409.6-4.6
Treatment C (Placebo)408.8-4.7

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Change From Baseline in QTcF for MAP0004 3.0mg, Placebo, and Moxifloxacin at 2 Hours

The Fridericia corrected QT interval(QTcF) is a measurement of the electrical impulses through the largest part of the heart muscle. A negative change is a shortening of the QTc interval, a positive change is a lengthening of the QTc interval. (NCT01191723)
Timeframe: baseline and 2 hours

,,
Interventionmilliseconds (Mean)
BaselineChange from Baseline at 2 hours
Treatment A (Moxifloxacin)407.08.5
Treatment B (MAP0004 3.0mg)407.7-3.9
Treatment C (Placebo)406.8-1.8

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Change From Baseline in QTcF for MAP0004 3.0mg and Placebo at 30 Minutes

The Fridericia corrected QT interval(QTcF) is a measurement of the electrical impulses through the largest part of the heart muscle. A negative change is a shortening of the QTc interval, a positive change is a lengthening of the QTc interval. (NCT01191723)
Timeframe: baseline and 30 minutes

,
Interventionmilliseconds (Mean)
BaselineChange from Baseline at 30 mins
Treatment B (MAP0004 3.0mg)407.7-4.7
Treatment C (Placebo)406.8-5.0

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Change From Baseline in Heart Rate for MAP0004 3.0mg, Placebo, and Moxifloxacin at 30 Minutes and 2 Hours

The heart rate is a measure of how fast or slow the heart beats (measured in beats per minute). A negative change indicates a decrease in heart rate and a positive change indicates an increase in heart rate. (NCT01191723)
Timeframe: baseline, 30 minutes, and 2 hours

,,
Interventionbeats per minute (bpm) (Mean)
BaselineChange from Baseline at 30 minutesChange from Baseline at 2 hours
Treatment A (Moxifloxacin)63.82.40.3
Treatment B (MAP0004 3.0mg)64.6-0.2-4.4
Treatment C (Placebo)64.11.0-2.1

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Change From Baseline in QTcI for MAP0004 3.0mg, Placebo, and Moxifloxacin at 2 Hours

The corrected QT interval, individualized (QTcI) is a measurement of the electrical impulses through the largest part of the heart muscle individualized for subject pre-dose values. A negative change is a shortening of the QTc interval, a positive change is a lengthening of the QTc interval. (NCT01191723)
Timeframe: baseline and 2 hours

,,
Interventionmilliseconds (Mean)
BaselineChange from Baseline at 2 hours
Treatment A (Moxifloxacin)408.69.0
Treatment B (MAP0004 3.0mg)409.6-5.1
Treatment C (Placebo)408.8-2.3

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Empa 25 mg: Mean QTcN Change From Baseline Between 30 Minutes and 24 Hours After Dosing

"Mean changes from baseline in QTcN from all ECGs taken between 30 minutes and 24 hours after dosings, for empa 25 mg.~Note, presented means are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 30min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h and 24h after the first dose

Interventionms (Mean)
Placebo0.71
Empa 25 mg1.37

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Mean QTcN Change From Baseline Between 2 and 4 Hours After Dosing

"Mean changes from baseline in QTcN from all ECGs taken between 2 hours and 4 hours after dosings~Note, the means presented are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 2 hour (h), 2.5h, 3h and 4h after the first dose

Interventionms (Mean)
Placebo3.53
Moxifloxacin15.96

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Placebo Corrected Change From Mean Baseline at Any Time Point Between 30 Minutes and 24 Hours After Dosings.

"The placebo corrected change from mean baseline is defined per time point as the difference of the change from baseline for empa or moxifloxacin minus the average change from baseline obtained for the two administrations of placebo. The clinically relevant information (and endpoint resulting from ICH E14) is shown by the maximum mean value of all measurements.~Results are presented for the greatest change, for empa 25mg the greatest change was seen at the 24 hour time point, for empa 200 mg and moxifloxacin the greatest change was seen at the 2.5 hour time point." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 30min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h and 24h after the first dose

Interventionms (Mean)
Empa 25 mg1.70
Empa 200 mg1.67
Moxifloxacin13.43

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Time-matched Change From Placebo in QTcN Between 30 Minutes and 24 Hours After Dosing.

"The time-matched change from placebo is defined per time point as the difference of the ECG measurement following administration of empa or moxifloxacin minus the average of the measurements obtained following the two administrations of placebo. The clinically relevant information (and endpoint resulting from ICH E14) is shown by the maximum mean value of all measurements.~Results are presented for the greatest change, for empa 25mg the greatest change was seen at the 24 hour time point, for empa 200 mg and moxifloxacin the greatest change was seen at the 2.5 hour time point." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 30min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h and 24h after the first dose

Interventionms (Mean)
Empa 25 mg4.05
Empa 200 mg3.45
Moxifloxacin13.99

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Empa 200mg: Mean QTcN Change From Baseline Between 1 and 4 Hours After Dosing

"Mean QTcN (heart rate-corrected QT interval, using a study population-based approach) from the ECGs obtained between 1h to 4h following drug administration minus the mean QTcN from the baseline ECGs obtained pre-dose at each visit, for empa 200mg.~Note, the treatment means presented are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 1 hour (h), 1.5h, 2h, 2.5h, 3h and 4h after the first dose

Interventionms (Mean)
Placebo3.67
Empa 200 mg3.44

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Empa 200mg: Change From Mean Baseline in QTcN at Each Time Point Between 30 Minutes and 24 Hours After Dosings

"Change from mean baseline in QTcN at each time point between 30 minutes and 24 hours after dosings for empa 200mg. The clinically relevant information (and endpoint resulting from ICH E14) is shown by the maximum upper confidence limit value over time.~For this outcome results are presented for the 2.5 hour timepoint as this was when the maximum value was seen.~Note, the presented means are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 0.5 hour (h), 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h and 24h after the first dose

Interventionms (Mean)
Placebo3.05
Empa 200 mg4.64

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Clinically Relevant Abnormalities for Physical Examination, Vital Signs, ECG, Blood Chemistry and Assessment of Tolerability by the Investigator

Clinically relevant abnormalities for physical examination, vital signs, ECG, blood chemistry, haematology, urinanalysis and assessment of tolerability by the investigator. New abnormal findings or worsening of baseline conditions were reported as adverse events (AEs). Time frame for AE reporting includes the period of first drug administration until end of study. A more detailed definition of the used time frame and MedDRA Version can be found in the AE section. (NCT01195675)
Timeframe: Drug administration until beginning of next sequence/end of trial, up to 48 days

Interventionparticipants (Number)
Placebo0
Empa 25 mg0
Empa 200 mg0
Moxifloxacin0

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Empa 200 mg: Mean QTcN Change From Baseline Between 30 Minutes and 24 Hours After Dosing

"Mean changes from baseline in QTcN from all ECGs taken between 30 minutes and 24 hours after dosings, for empa 200 mg.~Note, presented means are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 30min, 1 hour (h), 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h and 24h after the first dose

Interventionms (Mean)
Placebo0.68
Empa 200 mg0.53

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Empa 25mg: Mean QTcN Change From Baseline Between 1 and 4 Hours After Dosing

"Mean QTcN (heart rate-corrected QT interval, using a study population-based approach) from the ECGs obtained between 1h to 4h following drug administration minus the mean QTcN from the baseline electrocardiogram (ECGs) obtained pre-dose at each visit, for empa 25mg.~Note, the treatment means presented are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 1 hour (h), 1.5h, 2h, 2.5h, 3h and 4h after the first dose

Interventionms (Mean)
Placebo3.68
Empa 25 mg4.27

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Empa 25mg: Change From Mean Baseline in QTcN at Each Time Point Between 30 Minutes and 24 Hours After Dosings

"Change from mean baseline in QTcN at each time point between 30 minutes and 24 hours after dosings for empa 25mg. The clinically relevant information (and endpoint resulting from ICH E14) is shown by the maximum upper confidence limit value over time.~For this outcome results are presented for the 24 hour timepoint as this was when the maximum value was seen.~Note, the presented means are actually adjusted means." (NCT01195675)
Timeframe: 60 minutes (min), 50min and 40 min before the first dose and 0.5 hour (h), 1h, 1.5h, 2h, 2.5h, 3h, 4h, 6h, 8h, 12h and 24h after the first dose

Interventionms (Mean)
Placebo-4.46
Empa 25 mg-2.30

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Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 2-14).

Log10 CFU rates of change were calculated for each individual patient from the slopes β1 and β2 of the bi-linear regression fitted to the data for each individual patient (log10CFU versus Day). Mean log10 CFU changes from baseline were compared. A higher slope value indicates a greater change in log10 CFU from baseline. Note that to facilitate interpretation the sign of these slopes are reversed for logCFU. A positive slope value therefore indicates a reduction in log10 CFU from baseline. (NCT01215851)
Timeframe: Day 2-14

Interventionlog10CFU/ml/day (Mean)
TMC2070.076
TMC207 and Pyrazinamide0.143
PA-824 and Pyrazinamide0.148
PA-824 and Moxifloxacin and Pyrazinamide0.222
Rifafour e-275 mg0.135
TMC207 and PA-8240.114

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Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 7-14).

Log10 CFU rates of change were calculated for each individual patient from the slopes β1 and β2 of the bi-linear regression fitted to the data for each individual patient (log10CFU versus Day). Mean log10 CFU changes from baseline were compared. A higher slope value indicates a greater change in log10 CFU from baseline. Note that to facilitate interpretation the sign of these slopes are reversed for logCFU. A positive slope value therefore indicates a reduction in log10 CFU from baseline. (NCT01215851)
Timeframe: Day 7-14

Interventionlog10CFU/ml/day (Mean)
TMC2070.123
TMC207 and Pyrazinamide0.152
PA-824 and Pyrazinamide0.124
PA-824 and Moxifloxacin and Pyrazinamide0.175
Rifafour e-275 mg0.136
TMC207 and PA-8240.114

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Rate of Change in Time to Sputum Culture Positivity (TTP)(Hours) in Liquid Culture Media (Days 0-14)

The TTP was measured in the Mycobacterial Growth Indicator Tube (MGIT) (Bactec MGIT960) automated liquid culture system from overnight sputum. TTP rates of change were calculated for each individual patient from the slopes β1 and β2 of the bi-linear regression fitted to the data for each individual patient (TTP versus Day). (NCT01215851)
Timeframe: 14 Days

Interventiontime (h) to positive per day (Mean)
TMC2075.414
TMC207 and Pyrazinamide9.970
PA-824 and Pyrazinamide8.805
PA-824 and Moxifloxacin and Pyrazinamide18.482
Rifafour e-275 mg11.841
TMC207 and PA-8245.855

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Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-14).

Log10 CFU rates of change were calculated for each individual patient from the slopes β1 and β2 of the bi-linear regression fitted to the data for each individual patient (log10CFU versus Day). Mean log10 CFU changes from baseline were compared. A higher slope value indicates a greater change in log10 CFU from baseline. Note that to facilitate interpretation the sign of these slopes are reversed for logCFU. A positive slope value therefore indicates a reduction in log10 CFU from baseline. (NCT01215851)
Timeframe: 14 consecutive days of treatment

Interventionlog10CFU/ml/day (Mean)
TMC2070.061
TMC207 and Pyrazinamide0.131
PA-824 and Pyrazinamide0.154
PA-824 and Moxifloxacin and Pyrazinamide0.233
Rifafour e-275 mg0.140
TMC207 and PA-8240.114

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Early Bactericidal Activity (EBA) Measured as the Mean Rate of Change of log10 Colony Forming Units (CFU) of M. Tuberculosis Per ml Sputum on Solid Medium Over Time (Days 0-2).

Log10 CFU rates of change were calculated for each individual patient from the slopes β1 and β2 of the bi-linear regression fitted to the data for each individual patient (log10CFU versus Day). Mean log10 CFU changes from baseline were compared. A higher slope value indicates a greater change in log10 CFU from baseline. Note that to facilitate interpretation the sign of these slopes are reversed for logCFU. A positive slope value therefore indicates a reduction in log10 CFU from baseline. (NCT01215851)
Timeframe: Day 0-2

Interventionlog10CFU/ml/day (Mean)
TMC207-0.022
TMC207 and Pyrazinamide0.079
PA-824 and Pyrazinamide0.170
PA-824 and Moxifloxacin and Pyrazinamide0.315
Rifafour e-275 mg0.177
TMC207 and PA-8240.114

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Evaluation of LNG Css (1) Between AG200-15 in Week 1 and 3

Comparative evaluation of EE Css (1) between AG200-15 and Ortho-Cyclen® in week 1 for cycles 2 and 3. For Ortho-Cyclen, steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For Ag200-15, the average concentration at steady-state calculated from trapezoidal AUC within the 48-168h time interval (AUC/time interval). (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Week 1Week 3
AG200-1510601847

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Evaluation of LNG Cmax Between AG200-15 in Week 1 and 3

Evaluation of LNG Cmax Between AG200-15 in Week 1 and 3 for cycles 2 and 3. (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Week 1Week 3
AG200-1513702400

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Evaluation of LNG AUC (0-168hrs Post-first Dose) Between AG200-15 in Week 1 and 3

Evaluation of LNG AUC (0-168hrs post-first dose) Between AG200-15 in Week 1 and 3 for cycles 2 and 3. (NCT01243580)
Timeframe: 3 months

Interventionng.h/ml (Mean)
Week 1Week 3
AG200-15160317

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Comparative Evaluation of Ethinyl Estradiol (EE) Cmax Between AG200-15 and Ortho-Cyclen® in Week 1

Comparative evaluation of ethinyl estradiol (EE) Cmax between AG200-15 and Ortho-Cyclen® in week 1 for cycle 2 and 3. (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®135
AG200-1545.5

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Comparative Evaluation of EE Css (2) Between AG200-15 and Ortho-Cyclen® in Week 1

Comparative evaluation of EE Css (2) between AG200-15 and Ortho-Cyclen® in week 1 for cycles 2 and 3. For Ortho-Cyclen steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For Ag200-15, the average concentration at steady-state calculated from trapezoidal AUC within the 48-168h time interval (AUC/time interval). (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®43.3
AG200-1532.0

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Comparative Evaluation of EE Css (2) Between AG200-15 and Ortho-Cyclen® in Week 3

Comparative evaluation of EE Css (2) between AG200-15 and Ortho-Cyclen® in week 3 for cycles 2 and 3. For Ortho-Cyclen steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For Ag200-15, the average concentration at steady-state calculated from trapezoidal AUC within the 48-168h time interval (AUC/time interval). (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®41.5
AG200-1535.7

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Comparative Evaluation of EE Css (3) Between AG200-15 and Ortho-Cyclen® in Week 3

Comparative evaluation of EE Css (3) between AG200-15 and Ortho-Cyclen® in week 3 for cycles 2 and 3. For Ortho-Cyclen steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For AG200-15, the average concentration at steady-state calculated from trapezoidal AUC within the 0-168h time interval (AUC/time interval). (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®41.5
AG200-1537.3

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Comparative Evaluation of EE AUC (0-168hrs Post-first Dose) Between AG200-15 and Ortho-Cyclen® in Week 3

Comparative evaluation of EE AUC (0-168hrs post-first dose) between AG200-15 and Ortho-Cyclen® in week 3 for cycles 2 and 3. (NCT01243580)
Timeframe: 3 months

Interventionng.h/ml (Mean)
Ortho-Cyclen®6.97
AG200-156.26

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Comparative Evaluation of EE AUC(0-168hrs Post-first Dose) Between AG200-15 and Ortho-Cyclen® in Week 1

Comparative evaluation of EE AUC (0-168hrs post-first dose) between AG200-15 and Ortho-Cyclen® in week 1 for cycles 2 and 3. (NCT01243580)
Timeframe: 3 months

Interventionng.h/ml (Mean)
Ortho-Cyclen®7.28
AG200-155.06

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Comparative Evaluation of EE Cmax Between AG200-15 and Ortho-Cyclen® in Week 3

Comparative evaluation of EE Cmax between AG200-15 and Ortho-Cyclen® in week 3 for cycles 2 and 3. (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®131
AG200-1551.3

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Comparative Evaluation of EE Css (1) Between AG200-15 and Ortho-Cyclen® in Week 1

Comparative evaluation of EE Css (1) between AG200-15 and Ortho-Cyclen® in week 1 for cycles 2 and 3. For Ortho-Cyclen steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For AG200-15 the average concentration within the 48-168 h time-interval was measured. (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®43.3
AG200-1531.4

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Comparative Evaluation of EE Css (1) Between AG200-15 and Ortho-Cyclen® in Week 3

Comparative evaluation of EE Css (1) between AG200-15 and Ortho-Cyclen® in week 3 for cycles 2 and 3. For Ortho-Cyclen steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For AG200-15 the average concentration within the 48-168 h time-interval was measured. (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®41.5
AG200-1535.7

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Comparative Evaluation of EE Css (3) Between AG200-15 and Ortho-Cyclen® in Week 1

Comparative evaluation of EE Css (3) between AG200-15 and Ortho-Cyclen® in week 1 for cycles 2 and 3. For Ortho-Cyclen steady-state concentration calculated as average concentration at steady-state from the 24-hour trapezoidal AUC (AUC0-24h/24). For AG200-15, the average concentration at steady-state calculated from trapezoidal AUC within the 0-168h time interval (AUC/time interval). (NCT01243580)
Timeframe: 3 months

Interventionpg/ml (Mean)
Ortho-Cyclen®43.3
AG200-1530.1

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Pharmacokinetics in Aqueous Humor Samples.

Concentration of Besivance and VIGAMOX in the aqueous humor will be determined by an independent laboratory using standardized high-pressure liquid chromatography and mass spectrometry assays. Pharmacokinetic parameters determined from the aqueous humor concentration will minimally include the area under the curve and the maximum concentration. (NCT01296191)
Timeframe: Measured after 3 days of drug instillation

Interventionng/ml (Mean)
VIGAMOX443.07
Besivance56.4525

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Number of Subjects With a Change in Bacterial Colonization of Lid and Conjunctival Cultures After 3 Days

Lid and Conjunctival cultures will be taken to measure bacterial colonization. (NCT01296542)
Timeframe: Following 3 days of antibiotic drops topically instilled

InterventionParticipants (Count of Participants)
VIGAMOX18
Besivance28

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Number of Subjects With Increase of QTcP Interval From Baseline >30msec at Any Timepoint on Any Day in Exenatide and Placebo

Number of subjects with increase of QTcP interval from baseline >30 msec at any timepoint on any day was summarized by frequency for exenatide and placebo. (NCT01297062)
Timeframe: Baseline, Day 1, 2, or 3

Interventionparticpants (Number)
Exenatide0
Placebo0

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Comparison of LS Mean Changes From Baseline in QTcP Intervals Between Exenatide and Placebo on Day 3 Averaged Over 1300h, 1400h, 1500h (Target Steady State Exenatide Concentration of 500 pg/mL)

Factors in QT correction formulas were first estimated using pre-therapy data. The most appropriate correction method (QTcP) minimized the mean squared individual QTc/RR regression slope with on-exenatide data. Adequacy of correction was validated with on-placebo data. Change from baseline in QTcP was analyzed by a MMRM between exenatide and placebo. (NCT01297062)
Timeframe: Baseline, Day 3

Interventionmsec (Least Squares Mean)
Exenatide-3.54
Placebo-2.41

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Comparison of LS Mean Changes From Baseline in QTcP Intervals Between Exenatide and Placebo on Day 2 Averaged Over 1300h, 1400h, 1500h (Target Steady State Exenatide Concentration of 300 pg/mL)

Factors in QT correction formulas were first estimated using pre-therapy data. The most appropriate correction method (QTcP) minimized the mean squared individual QTc/RR regression slope with on-exenatide data. Adequacy of correction was validated with on-placebo data. Change from baseline in QTcP was analyzed by a MMRM between exenatide and placebo. (NCT01297062)
Timeframe: Baseline, Day 2

Interventionmsec (Least Squares Mean)
Exenatide-2.58
Placebo-0.56

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Comparison of Least Squares (LS) Mean Changes From Baseline in Population-based Corrected QT Intervals (QTcP) Between Exenatide and Placebo on Day 1 Averaged Over 1300h, 1400h, 1500h (Target Steady State Exenatide Concentration of 200 pg/mL)

Factors in QT correction formulas were first estimated using pre-therapy data. The most appropriate correction method (QTcP) minimized the mean squared individual QTc/RR regression slope with on-exenatide data. Adequacy of correction was validated with on-placebo data. Change from baseline in QTcP was analyzed by a mixed-effects model for repeated measures (MMRM) between exenatide and placebo. (NCT01297062)
Timeframe: Baseline, Day 1

Interventionmsec (Least Squares Mean)
Exenatide-2.25
Placebo-0.89

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Assay Sensitivity of Moxifloxacin at 1100h (2 Hour Post-administration of Moxifloxacin) on Day 2

Change from baseline in QTcP was analyzed by a MMRM between moxifloxacin and placebo. (NCT01297062)
Timeframe: Baseline, Day 2

Interventionmsec (Least Squares Mean)
Moxifloxacin9.75
Placebo-0.81

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Assay Sensitivity of Moxifloxacin at 1000h (1 Hour Post-administration of Moxifloxacin) on Day 2

Change from baseline in QTcP was analyzed by a MMRM between moxifloxacin and placebo. (NCT01297062)
Timeframe: Baseline, Day 2

Interventionmsec (Least Squares Mean)
Moxifloxacin1.91
Placebo-3.56

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Assay Sensitivity of Moxifloxacin at 1200h (3 Hour Post-administration of Moxifloxacin) on Day 2

Change from baseline in QTcP was analyzed by a MMRM between moxifloxacin and placebo. (NCT01297062)
Timeframe: Baseline, Day 2

Interventionmsec (Least Squares Mean)
Moxifloxacin12.47
Placebo1.56

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Plasma Exenatide Concentrations at Steady State on Day 1, 2 and 3

The plasma exenatide concentration at steady state was descriptively summarized by geometric mean, standard error, and its effect on placebo-adjusted change from baseline in QTcP was assessed. (NCT01297062)
Timeframe: Baseline, Day 1, 2, and 3

Interventionpg/mL (Geometric Mean)
Day 1Day 2Day 3
Exenatide252.74399.14626.65

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Number of Subjects With QTcP Interval >450msec at Any Timepoint on Any Day in Exenatide and Placebo

Number of subjects with QTcP > 450 msec at any timepoint on any day was summarized by frequency for exenatide and placebo. (NCT01297062)
Timeframe: Day 1, 2, or 3

Interventionparticipants (Number)
Exenatide0
Placebo0

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Pharmacokinetics: Time to Maximum Plasma Concentration (Tmax) of Ethinyl Estradiol and Norelgestromin

(NCT01373931)
Timeframe: Predose up to 24 hours post dose on Day 21

,
Interventionhour (h) (Median)
Ethinyl EstradiolNorelgestromin
OC + LY22166842.003.00
OC + Placebo2.002.03

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Area Under the Concentration-Time Curve Over a Dosing Interval (AUCτ) of Ethinyl Estradiol and Norelgestromin

The results presented are Geometric Least Squares (LS) mean. LS mean values were adjusted for treatment, sequence, period and participant. (NCT01373931)
Timeframe: Predose up to 24 hours post dose on Day 21

,
Interventionpicograms*hour/milliliter (pg*hr/mL) (Geometric Mean)
Ethinyl EstradiolNorelgestromin
OC + LY221668488816156
OC + Placebo82716079

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Pharmacokinetics: Maximum Plasma Concentration (Cmax) of Ethinyl Estradiol and Norelgestromin

The results presented are Geometric Least Squares (LS) mean. LS mean values were adjusted for treatment, sequence, period and participant. (NCT01373931)
Timeframe: Predose up to 24 hours post dose on Day 21

,
Interventionpicograms/milliliter (pg/mL) (Geometric Mean)
Ethinyl EstradiolNorelgestromin
OC + LY221668479.01438
OC + Placebo80.91574

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Change From Baseline in Summary of Maximum QTcI on Day 11 Minus Mean QTcI on Day -1 (Baseline).

The primary QT to QTc correction formula (QTcI) were determined for each participant using the participant's Baseline (Day -1 placebo) ECG data. The QT correction formula QT / (RR)k were derived using log-log-linear regression, where log (QT) = a + k × log (RR) + ε to estimate the exponent (k). The change form Baseline in summary of maximun QTcI on Day 11 minus mean QTcI on Day -1 (Baseline) is presented here. (NCT01423916)
Timeframe: Baseline, Day 11

Interventionmsec (Mean)
Brexpiprazole 4mg11.6
Brexpiprazole 12mg12.4
Moxifloxacin 400mg10.6
Placebo-1.1

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Change From Baseline in Summary of Maximum QTcI on Day 11 Minus Maximum QTcI on Day -1 (Baseline).

The primary QT to QTc correction formula (QTcI) were determined for each participant using the participant's Baseline (Day -1 placebo) ECG data. The QT correction formula QT / (RR)k were derived using log-log-linear regression, where log (QT) = a + k × log (RR) + ε to estimate the exponent (k). The change from Baseline in summary of maximum QTcI on Day 11 minus maximum QTcI on Day -1 (Baseline) is presented here. (NCT01423916)
Timeframe: Baseline, Day 11

Interventionmsec (Mean)
Brexpiprazole 4mg0.4
Brexpiprazole 12mg0.9
Moxifloaxcin 400mg0.0
Placebo-1.2

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Area Under the Plasma Concentration-time Curve During Dosing (AUCT).

Pharmacokinetics endpoint is the area under the concentration-time curve from time zero to 24 hours (AUC0-24h) of brexpiprazole and moxifloxacin. Area under the plasma concentration-time curve during the dosing interval at steady-state (AUCT) value was estimated using the linear trapezoidal rule; the value reported represent the area under the curves to the last time point during that day. Blood samples were collected on Days -1, 1, 11, and 12 at predose, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours postdose or at ET. (NCT01423916)
Timeframe: Day 11

Interventionng*h/mL (Mean)
Brexpiprazole 4mg3100
Brexpiprazole 12mg8880
Moxifloxacin/ Placebo28400

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Number Participants Noted With New Incidence of QT Interval of > 500 Msec on Day 11.

The number of participants who were noted with new incidence of QT interval of > 500 msec on Day 11 and a 12-lead ECG was used. (NCT01423916)
Timeframe: Day 11

Interventionparticipants (Number)
Brexpiprazole 4mg0
Brexpiprazole 12mg0
Moxifloxacin 400mg0
Placebo0

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Number of Participants With QTcI Interval Between 30 and 60 Msec on Day 11.

The primary QT to QTc correction formula (QTcI) were determined for each participant using the participant's Baseline (Day -1 placebo) ECG data. The QT correction formula QT / (RR)k were derived using log-log-linear regression, where log (QT) = a + k × log (RR) + ε to estimate the exponent (k). Participants with QTcI interval change between 30 to 60 msec were presented here. (NCT01423916)
Timeframe: Day 11

Interventionparticipants (Number)
Brexpiprazole 4mg4
Brexpiprazole 12mg1
Moxifloxacin 400mg11
Placebo2

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Maximum Peak Plasma Concentration (Cmax) of Brexpiprazole and Moxifloxacin.

Pharmacokinetics endpoint is the maximum (peak) plasma concentration (Cmax) of brexpiprazole and moxifloxacin. Values for Cmax were determined directly from the observed data. Blood samples were collected on Days -1, 1, 11, and 12 at predose, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours postdose or at ET. (NCT01423916)
Timeframe: Day 11

Interventionng/mL (Mean)
Brexpiprazole 4mg170
Brexpiprazole 12mg462
Moxifloxacin/ Placebo2760

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Time-matched QTcI Change From Baseline (Day -1) Corrected for Placebo on Day 11 Following Brexpiprazole Treatment.

Pharmacodynamics endpoint is the time-matched corrected QT interval (QTcI) change from baseline (Day -1) corrected for placebo on Day 11 following brexpiprazole treatment. The primary QT to QTc correction formula (QTcI) was determined for each participant using the participant's baseline (Day -1 placebo) ECG data. The QT correction formula QT / (RR)k was derived using log-log-linear regression, where log (QT) = a + k × log (RR) + ε to estimate the exponent (k). (NCT01423916)
Timeframe: Day 11 (Hours 1, 2, 3, 4, 5, 6, 8, 12, 16, 24)

,,
Interventionmsec (Mean)
Hours 1 (N=61, 53, 61)Hours 2 (N= 62, 53, 62)Hours 3 (N= 60, 51, 61)Hours 4 (N= 62, 53, 62)Hours 5 (N= 62, 52, 62)Hours 6 (N= 61, 52, 62)Hours 8 (N= 59, 50, 59)Hours 10 (N= 59, 47, 56)Hours 12 (N= 58, 47, 58)Hours 16 (N= 59, 48, 53)Hours 24 (N= 54, 45, 57)
Brexpiprazole 12mg-0.2-0.21.33.1-0.21.32.52.22.60.80.7
Brexpiprazole 4mg2.61.21.13.61.78.34.05.25.34.00.1
Moxifloxacin/Placebo9.29.48.510.56.27.37.59.06.82.22.1

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Number of Participants With New Incidence of ECG Morphology Abnormalities on Day 11.

Participants with incidence of ECG morphology abnormalities on Day 11 (participants who had abnormalities during Day 11 but not at Day -1) were noted. Types of abnormalities included appearance of abnormal U waves, negative T waves, elevation of ST segment, depression of ST segment, second degree heart block, third degree heart block, right bundle branch block, and left bundle branch block. ECGs were sampled at predose and approximately 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours postdose on Days -1, 1, 11, and 12. (NCT01423916)
Timeframe: Day 11

,,,
Interventionparticipants (Number)
U Wave abnormalitiesNegative T WavesDepression of ST segmentElevation of ST segmentSecond degree heart blockThird degree heart blockRight bundle branch blockLeft bundle branch block
Brexpiprazole 12mg07200000
Brexpiprazole 4mg04200000
Moxifloxacin 400mg08400000
Placebo06100000

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Number of Participants With Maximum Change From Baseline to the On-treatment ECG Values on Day 11 for Heart Rate (HR), PR Interval, and QRS Interval.

Changes in HR with values 25% decrease from Day -1 and HR < 50 bpm and 25% increase from Day -1 and HR > 100 bpm; PR interval of greater than or equal to 25% change from Day -1 and PR > 200 msec; QRS interval of Greater than or equal to 25% change from Day -1 and > 100 msec were noted on Day 11. Maximum change from baseline to the on-treatment ECG values on Day 11 for heart rate. (NCT01423916)
Timeframe: Day 11

,,,
Interventionparticipants (Number)
HR: < 50 bpmHR: > 100 bpmPR > 200 msecQRS > 100 msec
Brexpiprazole 12mg0700
Brexpiprazole 4mg0500
Moxifloxacin0200
Placebo0400

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Number of Participants With Adverse Events (AE) and Clinically Important Changes in Vital Signs, Physical Examinations, Laboratory Tests, and Standard ECGs (Electrocardiogram).

Clinically important changes in vital signs, physical examinations, laboratory tests and ECGs were by and large reflected in AE/SAE (which are presented in safety section) of this report. (NCT01423916)
Timeframe: AEs were recorded from Screening (informed consent was signed) during the 12-day treatment period to follow-up 30 (+ 2) days post-last dose of study medication

,,,
Interventionparticipants (Number)
Postural orthostatic tachycardia syndromeTachycardiaBlood creatinine phosphokinase increasedBlood pressure increasedBlood prolactin increasedHepatic enzyme increasedLiver function test abnormalWeight increasedHyperglycaemia
Brexpiprazole 12mg101001111
Brexpiprazole 4mg001001000
Moxifloxacin020010000
Placebo010100000

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Number of Participants Noted With Time-matched Change in Mean QTcI Change From Baseline for Assay Sensitivity of Moxifloxacin Treatment Corrected for Placebo at Day 11.

New onset (> 450, > 480, or > 500 msec) in QTc was defined as a participant who attained a QTc > 450, > 480, > 500 msec during Day 11 but not on Day -1. The number of participants were noted with time-matched change in mean QTcI change from Baseline for assay sensitivity of moxifloxacin treatment corrected for placebo. The primary QT to QTc correction formula (QTcI) were determined for each participant using the participant's Baseline (Day -1 placebo) ECG data. The QT correction formula QT / (RR)k were derived using log-log-linear regression, where log (QT) = a + k × log (RR) + ε to estimate the exponent (k). (NCT01423916)
Timeframe: Baseline, Day 11

,,,
Interventionparticipants (Number)
QTcI (> 450 msec)QTcI (> 480 msec)QTcI (> 500 msec)
Brexpiprazole 12mg410
Brexpiprazole 4mg500
Moxifloxacin 400 mg500
Placebo000

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Number of Participants With QTcI Interval > 60 Msec on Day 11.

The primary QT to QTc correction formula (QTcI) were determined for each participant using the participant's Baseline (Day -1 placebo) ECG data. The QT correction formula QT / (RR)k were derived using log-log-linear regression, where log (QT) = a + k × log (RR) + ε to estimate the exponent (k). Participants with QTcI interval change of > 60 msec on Day 11 were presented here. (NCT01423916)
Timeframe: Day 11

Interventionparticipants (Number)
Brexpiprazole 4mg0
Brexpiprazole 12mg0
Moxifloxacin 400mg0
Placebo0

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Time to Maximum (Peak) Plasma Concentration (Tmax) of Brexpiprazole and Moxifloxacin.

Pharmacokinetics endpoint is the time to maximum (peak) plasma concentration (tmax) of brexpiprazole and moxifloxacin. Values for tmax were determined directly from the observed data. Blood samples were collected on Days -1, 1, 11, and 12 at predose, and 1, 2, 3, 4, 5, 6, 8, 10, 12, 16, and 24 hours postdose or at ET. (NCT01423916)
Timeframe: Day 11

InterventionHours (Median)
Brexpiprazole 4mg3.54
Brexpiprazole 12mg3.00
Moxifloxacin/ Placebo1.25

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Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of Ortho-Cyclen - Norelgestromin (NGMN)

(NCT01458210)
Timeframe: Day 21 Periods 1 and 2: Pre-dose and up to 24 hours post-dose

Interventionhours (Median)
Ortho-Cyclen Alone (Period 1)3.00
Ortho-Cyclen + Dulaglutide (Period 2)4.00

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Pharmacokinetics: Time of Maximum Observed Drug Concentration (Tmax) of Ortho-Cyclen - Ethinyl Estradiol (EE)

(NCT01458210)
Timeframe: Day 21 during Periods 1 and 2: Pre-dose and up to 24 hours post-dose

Interventionhours (Median)
Ortho-Cyclen Alone (Period 1)3.00
Ortho-Cyclen + Dulaglutide (Period 2)4.00

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Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Ortho-Cyclen - Norelgestromin (NGMN)

(NCT01458210)
Timeframe: Day 21 during Periods 1 and 2: Pre-dose and up to 24 hours post-dose

Interventionpicograms per milliliter (pg/mL) (Geometric Mean)
Ortho-Cyclen Alone (Period 1)1770
Ortho-Cyclen + Dulaglutide (Period 2)1310

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Pharmacokinetics: Maximum Observed Drug Concentration (Cmax) of Ortho-Cyclen - Ethinyl Estradiol (EE)

(NCT01458210)
Timeframe: Day 21 during Periods 1 and 2: Pre-dose and up to 24 hours post-dose

Interventionpicograms per milliliter (pg/mL) (Geometric Mean)
Ortho-Cyclen Alone (Period 1)86.9
Ortho-Cyclen + Dulaglutide (Period 2)76.2

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Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) at Steady State of Ortho-Cyclen - Norelgestromin (NGMN)

(NCT01458210)
Timeframe: Day 21 during Periods 1 and 2: Pre-dose and up to 24 hours post-dose

Interventionpicograms*hour/milliliter (pg*h/mL) (Geometric Mean)
Ortho-Cyclen Alone (Period 1)17900
Ortho-Cyclen + Dulaglutide (Period 2)16000

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Pharmacokinetics: Area Under the Concentration Versus Time Curve (AUC) at Steady State of Ortho-Cyclen - Ethinyl Estradiol (EE)

(NCT01458210)
Timeframe: Day 21 during Periods 1 and 2: Pre-dose and up to 24 hours post-dose

Interventionpicograms*hour/milliliter (pg*h/mL) (Geometric Mean)
Ortho-Cyclen Alone (Period 1)901
Ortho-Cyclen + Dulaglutide (Period 2)903

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Part B: Mean Change From Baseline in 12-lead Electrocardiogram (ECG) Corrected QT Intervals (Moxifloxacin)

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave and was calculated from electrocardiogram (ECG) data using Fridericia's formula: QTc = QT/RR^0.33. Corrected QT (QTc) is the QT interval corrected for heart rate and RR, which is the interval between two R waves. Least Squares (LS) means were calculated using mixed effects model with fixed effects for treatment, time, period, sequence, and the time-by-treatment interaction, random effects for participant, the participant-by-treatment interaction, and participant-by-time interaction. (NCT01460368)
Timeframe: Baseline, 2 and 4 hours

,
Interventionmilliseconds (Least Squares Mean)
2 hours postdose4 hours postdose
Part B: Moxifloxacin-7.391.45
Part B: Placebo-15.46-9.11

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Part B: Mean Change From Baseline in 12-lead Electrocardiogram (ECG) Corrected QT Intervals (LY2409021)

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave and was calculated from electrocardiogram (ECG) data using Fridericia's formula: QTc = QT/RR^0.33. Corrected QT (QTc) is the QT interval corrected for heart rate and RR, which is the interval between two R waves. Least Squares (LS) means were calculated using mixed effects model with fixed effects for treatment, time, period, sequence, and the time-by-treatment interaction, random effects for participant, the participant-by-treatment interaction, and participant-by-time interaction. (NCT01460368)
Timeframe: Baseline, 2, 4, 6, 8, 12, and 24 hours

,
Interventionmilliseconds (Least Squares Mean)
2 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
Part B: LY2409021-14.72-5.436.137.80-13.45-1.32
Part B: Placebo-15.35-9.12-3.01-1.29-13.30-4.95

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Change From Baseline in Blood Pressure (BP) at Month 6

Blood pressure is the pressure of blood flowing through blood vessels. Change from Baseline in blood pressure is the value at Month 6 minus value at Baseline. (NCT01466673)
Timeframe: Baseline and Month 6

,
InterventionMillimeters of Mercury (Mean)
Systolic BP: Baseline (n=100/101)Diastolic BP: Baseline (n=100/101)Systolic BP: Change at Month 6 (n=93, 95)Diastolic BP: Change at Month 6 (n=93, 95)
Ethinyl Estradiol/Desogestrel (EE/DSG)110.269.47-0.24-0.48
Ethinyl Estradiol/Norgestimate (EE/NGM)110.670.230.33-0.80

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Change From Baseline in Body Weight at Month 6

Change from Baseline in body weight is the value at Month 6 minus value at Baseline. (NCT01466673)
Timeframe: Baseline and Month 6

,
InterventionKilograms (Mean)
Baseline (n=100,101)Change at Month 6 (n=93,95)
Ethinyl Estradiol/Desogestrel (EE/DSG)54.24-0.20
Ethinyl Estradiol/Norgestimate (EE/NGM)55.62-0.08

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Change From Baseline in Total and Each Type of Acne Lesions Count at Month 6

Total acne (pimples) lesion (abnormal area of tissue, such as a wound, sore, rash, or boil) count is summation of all lesions which includes all comedones (open and closed), papules, pustules, and nodules. Change from Baseline means lesions at Baseline minus lesions at Month 6. Positive value indicates decrease in lesion count while negative value indicates increase in lesion count. (NCT01466673)
Timeframe: Baseline and Month 6

,
InterventionLesions (Mean)
Comedones Counts: Change at Month 6 (n=93, 95)Papules Counts: Change at Month 6 (n=93, 95)Pustules Counts: Change at Month 6 (n=93, 95)Nodules Counts: Change at Month 6 (n=93, 95)Total Counts: Change at Month 6 (n=93, 95)
Ethinyl Estradiol/Desogestrel (EE/DSG)8.212.770.960.0011.94
Ethinyl Estradiol/Norgestimate (EE/NGM)9.023.520.770.1313.44

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Number of Participants Non-Compliant With Therapy

Compliance was assessed by transforming the data of forgotten tablets listed in the diary cards. Number of participants who forgot to take the drug was reported. (NCT01466673)
Timeframe: Month 1, 3 and 6

,
InterventionParticipants (Number)
At Month 1 (n=100, 101)At Month 3 (n=93, 96)At Month 6 (n=93, 95)
Ethinyl Estradiol/Desogestrel (EE/DSG)5106
Ethinyl Estradiol/Norgestimate (EE/NGM)71310

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Number of Participants With Treatment Response at the End-of-Therapy by Participant's Self-Assessment at Month 6

Participant's self-assessment at end-of-therapy was measured by using the self-assessment questionnaire which included 3 questions, about the rating of acne improvement since start of study; comparison of this acne treatment with the one used in past and the continuity of treatment on physician's prescription to evaluate efficacy and acceptability of the study medication. The score was graded at 4 parameters as excellent, better, no change and worse. (NCT01466673)
Timeframe: Month 6

,
InterventionParticipants (Number)
ExcellentBetterNo ChangeWorse
Ethinyl Estradiol/Desogestrel (EE/DSG)355831
Ethinyl Estradiol/Norgestimate (EE/NGM)474534

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Percentage of Participants Showing Treatment Response on the Investigator's Global Assessment at Month 6

Percentage of participants showing treatment response on the Investigator's global assessment was graded on a 5-point scale as 0=worse, 1=no change, 2=fair, 3=good, and 4=excellent. (NCT01466673)
Timeframe: Month 6

,
InterventionPercentage of participants (Number)
0 (Worse)1 (No Change)2 (Fair)3 (Good)4 (Excellent)
Ethinyl Estradiol/Desogestrel (EE/DSG)1.031.0323.7152.5821.65
Ethinyl Estradiol/Norgestimate (EE/NGM)5.054.044.0443.4343.43

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Number of Participants With Abnormal Vaginal Blood Loss at Month 1, 3 and 6

Vaginal blood loss encompasses spotting and bleeding. Spotting is defined as a bleeding requiring no or at most one sanitary pad per day; however, bleeding requires two or more sanitary pads per day. (NCT01466673)
Timeframe: Month 1, 3 and 6

,
InterventionParticipants (Number)
Spotting at Month 1 (n=100,101)Spotting at Month 3 (n=93, 96)Spotting at Month 6 (n=93, 95)Bleeding at Month 1 (n=100,101)Bleeding at Month 3 (n=93, 96)Bleeding at Month 6 (n=93, 95)
Ethinyl Estradiol/Desogestrel (EE/DSG)243473
Ethinyl Estradiol/Norgestimate (EE/NGM)5641346

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Change From Baseline in Total and Each Type of Acne Lesions Count at Month 3

Total acne (pimples) lesion (abnormal area of tissue, such as a wound, sore, rash, or boil) count is summation of all lesions which includes all comedones (open and closed), papules, pustules, and nodules. Change from Baseline means lesions at Baseline minus lesions at Month 3. Positive value indicates decrease in lesion count while negative value indicates increase in lesion count. (NCT01466673)
Timeframe: Baseline and Month 3

,
InterventionLesions (Mean)
Comedones Counts: Change at Month 3 (n=93, 96)Papules Counts: Change at Month 3 (n=93, 96)Pustules Counts: Change at Month 3 (n=93, 96)Nodules Counts: Change at Month 3 (n=93, 96)Total Counts: Change at Month 3 (n=93, 96)
Ethinyl Estradiol/Desogestrel (EE/DSG)5.601.890.700.008.19
Ethinyl Estradiol/Norgestimate (EE/NGM)5.712.830.630.128.84

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Percentage of Participants With Categorical Score for Sebum Assessment at Month 1, 3 and 6

Sebum assessment that is facial seborrhea (very oily skin) was assessed using sebutape strip on the forehead. Percentage of participants with facial seborrhea were assessed using categorical scores ranging from level 1 (lowest) to level 5 (highest). Highest level indicates worsening. (NCT01466673)
Timeframe: Baseline and Month 1, 3 and 6

,
InterventionPercentage of Participants (Number)
Level 1: Baseline (n=100,101)Level 2: Baseline (n=100,101)Level 3: Baseline (n=100,101)Level 4: Baseline (n=100,101)Level 5: Baseline (n=100,101)Level 1: Month 1 (n=100,101)Level 2: Month 1 (n=100,101)Level 3: Month 1 (n=100,101)Level 4: Month 1 (n=100,101)Level 5: Month 1 (n=100,101)Level 1: Month 3 (n=93, 96)Level 2: Month 3 (n=93, 96)Level 3: Month 3 (n=93, 96)Level 4: Month 3 (n=93, 96)Level 5: Month 3 (n=93, 96)Level 1: Month 6 (n=93, 95)Level 2: Month 6 (n=93, 95)Level 3: Month 6 (n=93, 95)Level 4: Month 6 (n=93, 95)Level 5: Month 6 (n=93, 95)
Ethinyl Estradiol/Desogestrel (EE/DSG)3.9612.8744.5534.653.968.9111.8845.5432.670.9910.4214.5859.3814.581.0422.1143.1629.475.260.00
Ethinyl Estradiol/Norgestimate (EE/NGM)3.0010.0043.0031.0013.007.0013.0047.0030.003.006.4534.4145.1611.832.1544.0927.9620.436.451.08

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Change From Baseline in Total and Each Type of Acne Lesions Count at Month 1

Total acne (pimples) lesion (abnormal area of tissue, such as a wound, sore, rash, or boil) count is summation of all lesions which includes all comedones (open and closed), papules, pustules, and nodules. Change from Baseline means lesions at Baseline minus lesions at Month 1. Positive value indicates decrease in lesion count while negative value indicates increase in lesion count. (NCT01466673)
Timeframe: Baseline and Month 1

,
InterventionLesions (Mean)
Comedones Counts: BaselinePapules Counts: BaselinePustules Counts: BaselineNodules Counts: BaselineTotal Counts: BaselineComedones Counts: Change at Month 1Papules Counts: Change at Month 1Pustules Counts: Change at Month 1Nodules Counts: Change at Month 1Total Counts: Change at Month 1
Ethinyl Estradiol/Desogestrel (EE/DSG)11.434.461.120.0017.003.440.620.18-0.024.22
Ethinyl Estradiol/Norgestimate (EE/NGM)10.974.320.900.1216.313.430.200.350.124.10

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Change From Baseline in Fasting Glucose at 6 Months

Higher fasting glucose indicate an increased metabolic risk (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmg/dL (Mean)
African-American Women-0.4
Caucasian Women03

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Change From Baseline in Body Mass Index in 6 Months

Higher values indicate higher metabolic risk (NCT01475513)
Timeframe: Baseline, 6 months

InterventionKg/m2 (Mean)
African-American Women-0.32
Caucasian Women0.39

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Change From Baseline in Disposition Index at 6 Months

Modeled from FISVGTT--higher values indicate better glucose disposition (NCT01475513)
Timeframe: Baseline, 6 months

InterventionAIRG * Si (Mean)
African-American Women-911.73
Caucasian Women-834.53

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Change From Baseline in Carotid Intima Media Thickness

Change in Carotid Intima Media Thickness from baseline to 6 months, measured on the right carotid artery, posterior. Lower values indicate better cardiovascular risk profile (NCT01475513)
Timeframe: baseline, 6 months

Interventionmm (Mean)
African-American Women-0.00008
Caucasian Women0.00118

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Change From Baseline in Areas-under-the-curve for Insulin at 6 Months

Measured during oral glucose tolerance test. Higher values indicate increased metabolic risk (NCT01475513)
Timeframe: Baselines, 6 months

InterventionmIU/mL * min (Mean)
African-American Women760.6
Caucasian Women1062.1

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Change From Baseline in Areas-under-the-curve for Glucose

Measured during oral glucose tolerance test. Higher values indicate increased metabolic risk (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmg/dL * min (Mean)
African-American Women443.4
Caucasian Women514.2

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Change From Baseline in Acute Insulin Response to Glucose

Acute Insulin Response to Glucose values obtained from FSIVGTT models--higher values indicate better insulin response (NCT01475513)
Timeframe: Baseline, 6 months

InterventionmIU* L^-1 * min (Mean)
African-American Women-35.6
Caucasian Women0.48

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Change in Triglycerides From Baseline to 6 Months

Higher values indicate higher cardiovascular risk (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmg/dL (Mean)
African-American Women13.3
Caucasian Women29.3

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Change in LDL From Baseline to 6 Months

Higher value indicates higher cardiovascular risk (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmg/dL (Mean)
African-American Women13.4
Caucasian Women17.1

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Change in Diastolic Blood Pressure From Baseline to 6 Months

Higher value indicates higher cardiovascular risk (NCT01475513)
Timeframe: Baseline, 6 months

InterventionmmHg (Mean)
African-American Women0.6
Caucasian Women2.44

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Change From Baseline in Systolic Blood Pressure at 6 Months

Higher value indicates increased cardiovascular risk (NCT01475513)
Timeframe: Baseline, 6 months

InterventionmmHg (Mean)
African-American Women2.5
Caucasian Women-1.4

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Change From Baseline in Insulin Sensitivity

Insulin sensitivity from Frequently sampled IV glucose tolerance test (FSIVGTT), change from baseline to 6 months. Higher values indicate better insulin sensitivity (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmin ^ -1 / mIU / L (Mean)
African-American Women-1.91
Caucasian Women-5.63

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Change From Baseline in HDL at 6 Months

Lower values indicate increased cardiovascular risk (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmg/dL (Mean)
African-American Women6.8
Caucasian Women6.9

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Change From Baseline in Glucose Effectiveness

Obtained from FSIVGTT models--higher values indicate better effectiveness of glucose inducing its own disposition (NCT01475513)
Timeframe: Baseline, 6 months

Intervention1000 * min ^ -1 (Mean)
African-American Women-0.0255
Caucasian Women-0.0078

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Change From Baseline in Flow-mediated Vasodilatation

Change Flow-mediated Vasodilatation from baseline to 6 months. Higher values indicate less cardiovascular risk (NCT01475513)
Timeframe: Baseline, 6 months

Interventionmm (Mean)
African-American Women0.0503
Caucasian Women-0.0210

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Change From Baseline in Fasting Insulin at 6 Months

Higher fasting insulin values indicate an increased metabolic risk (NCT01475513)
Timeframe: Baseline, 6 months

InterventionuIU/ mL (Mean)
African-American Women1.66
Caucasian Women1.45

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Percentage of Participants Who Discontinue Due to an Adverse Event in Each Experimental Arm.

(NCT01498419)
Timeframe: 8 weeks

Interventionpercentage of participants (Number)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)13
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)19
Drug Sensitive: Rifafour12
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)12

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Percentage of Patients With Sputum Culture Conversion at 8 Weeks on Liquid Media

Sputum culture conversion is defined as a change from a positive growth of M. tuberculosis in a sputum sample to negative M. tuberculosis growth sputum sample in patients with pulmonary TB. This was measured at visit 24(Day 57). (NCT01498419)
Timeframe: Day 57 after eight weeks of daily treatment

Interventionpercentage of patients (Number)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)65.7
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)71.4
Drug Sensitive: Rifafour37.8
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)50.0

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Percentage of Patients With Sputum Culture Conversion at 8 Weeks on Solid Media

Sputum culture conversion is defined as a change from a positive growth of M. tuberculosis in a sputum sample to negative M. tuberculosis growth sputum sample in patients with pulmonary TB. (Day 57) (NCT01498419)
Timeframe: Day 57 after eight weeks of daily treatment

Interventionpercentage of participants (Number)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)82.9
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)94.3
Drug Sensitive: Rifafour87.5
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)62.5

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The Rate of Change in Colony Forming Units (CFUs) Using Non-linear Mixed Effects Modeling of the Serial Sputum Colony Counts (SSCC) Over 8 Weeks of Treatment.

The primary efficacy endpoint was bactericidal activity characterized by the daily rate of change in mean log10CFU counts during 8 weeks of treatment (bactericidal activity assessed by CFU on solid media for days 0-56). (NCT01498419)
Timeframe: 8 weeks

Interventionlog10CFU/ml/day (Mean)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)0.133
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)0.155
Drug Sensitive: Rifafour0.112
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)0.117

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The Rate of Change in Time to Sputum Culture Positivity (TTP) Through 8 Weeks in the MGIT System in Sputum Over 8 Weeks in Participants as Derived From a Non-linear Regression Model.

Measurement of TTP in liquid culture media Mycobacteria growth indicator tube (MGIT) using standard procedures (NCT01498419)
Timeframe: 8 weeks

Interventionlog10hours/day (Mean)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)0.020
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)0.020
Drug Sensitive: Rifafour0.017
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)0.015

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Time to Sputum Conversion Using Data From Weekly Cultures Through 8 Weeks on Liquid Media

liquid culture = Mycobacteria growth indicator tube (MGIT) Sputum culture conversion is defined as a change from a positive growth of M. tuberculosis in a sputum sample to negative M. tuberculosis growth sputum sample in patients with pulmonary TB (NCT01498419)
Timeframe: 8 weeks

Interventiondays (Median)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)42.0
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)49.0
Drug Sensitive: Rifafour56.0
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)56.0

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Time to Sputum Conversion Using Data From Weekly Cultures Through 8 Weeks on Solid Media

Sputum culture conversion is defined as a change from a positive growth of M. tuberculosis in a sputum sample to negative M. tuberculosis growth sputum sample in patients with pulmonary TB (NCT01498419)
Timeframe: 8 weeks

Interventiondays (Median)
Drug Sensitive: M (400 mg) Pa (100 mg) Z (1500 mg)28.0
Drug Sensitive: M (400 mg) Pa (200 mg) Z (1500 mg)28.0
Drug Sensitive: Rifafour35.0
Multi Drug-Resistant: M (400 mg) Pa (200 mg) Z (1500 mg)35.0

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Difference Between Active and Placebo for Time Matched Baseline Adjusted Mean QTcF

The primary endpoint is the difference between the active (HA44) and placebo for time matched baseline adjusted mean QTcF = [ΔQTcF (Ha44 0.74% Gel) - ΔQTcF (placebo)] = ΔΔQTcF. This was compared with the difference between Moxifloxacin and placebo for time matched baseline adjusted mean QTcF = [ΔQTcF (Moxifloxacin) - ΔQTcF (placebo)] = ΔΔQTcF (NCT01518699)
Timeframe: 36 hours

Interventionmilliseconds (Mean)
HA 44 Gel + Moxifloxacin Placebo-9.7
HA 44 Placebo + Moxifloxacin Placebo-9.2
Moxifloxacin 400 mg Tablet +HA 44 Placebo6.1

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Pharmacokinetics: Area Under the Concentration Curve From Time 0 to Infinity [AUC(0-inf)] of LY3009104

(NCT01536951)
Timeframe: Parts A and B, Periods 1 through 3: Predose and 0.5 hours (h), 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 12 h, 24 h, 36 h, 48 h after administration of study drug

Interventionhours*nanomoles per liter (h*nmol/L) (Geometric Mean)
Part A: 20 mg LY30091043960
Part A: 30 mg LY30091045480
Part A: 40 mg LY30091048490
Part B: 40 mg LY30091046440

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Pharmacokinetics: Maximum Concentration (Cmax) of LY3009104

(NCT01536951)
Timeframe: Parts A and B, Periods 1 through 3: Predose and 0.5 hours (h), 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 12 h, 24 h, 36 h, 48 h after administration of study drug

Interventionnanomoles per liter (nmol/L) (Geometric Mean)
Part A: 20 mg LY3009104578
Part A: 30 mg LY3009104734
Part A: 40 mg LY30091041270
Part B: 40 mg LY3009104741

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Change From Baseline Through 24 Hours Postdose in Population-Corrected QT (QTcP) Interval

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave and is calculated from electrocardiogram (ECG) data. Corrected QT (QTc) is the QT interval corrected for heart rate and RR, which is the interval between 2 R waves. Using the population-corrected formula: QTcP = QT/RR^beta, where beta is the population correction factor computed from a log-linear model (ln) QT = alpha+beta*ln RR fitted to all Day -1 and Day 1 predose QT and RR measurements in all periods for all participants. Baseline is the average of data collected for 2 hours before dosing on Day 1 of each period [-2 hours (h), -1.5 h, -1 h, -0.5 h, and 0 h]. The QTcP interval was not assessed during Part A of the study, as specified in the protocol. The QTcP interval at 1 h, 2 h, and 4 h postdose for moxifloxacin was compared to placebo to establish assay sensitivity. (NCT01536951)
Timeframe: Part B, Periods 1 through 3: Baseline, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 12 h, and 24 h postdose

,,
Interventionmilliseconds (msec) (Mean)
1 h postdose (n=52, 53, 53)1.5 h postdose (n=52, 53, 53)2 h postdose (n=52, 53, 53)3 h postdose (n=52, 53, 53)4 h postdose (n=52, 53, 53)6 h postdose (n=51, 53, 53)12 h postdose (n=52, 52, 52)24 h postdose (n=52, 53, 53)
Part B: 40 mg LY3009104-2.40.1-0.1-2.5-0.8-2.20.8-0.8
Part B: Moxifloxacin9.79.39.59.29.95.55.93.4
Part B: Placebo-2.5-1.7-1.4-2.8-1.3-1.3-1.0-1.6

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Change From Baseline to Day 10 in QT Interval Corrected for Heart Rate (QTc) for LY2484595 Versus Placebo

Data were collected using a 12-lead electrocardiogram (ECG). The QT interval is the time between the start of the Q wave and the end of the T wave in the cardiac electrical cycle and corrected for heart rate. Population-corrected QT interval (QTcP) formula: QTcP = QT / RR^ß, where ß is the population correction factor. (NCT01537887)
Timeframe: Predose of Day 1, Day 10

,
Interventionmilliseconds (msec) (Mean)
4-hour postdose on Day 106-hour postdose on Day 10
LY2484595-4.6-1.1
Placebo-2.7-2.0

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Pharmacokinetics: Maximum Drug Concentration (Cmax) of LY2484595 During One Dosing Interval at Steady State

(NCT01537887)
Timeframe: Predose, 1, 2, 3, 4, 6, 12, 24, 72, and 168 Hours Postdose

Interventionnanograms/milliliter (ng/mL) (Geometric Mean)
LY24845955270

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Pharmacokinetics: Area Under the Concentration Curve (AUC) of LY2484595 During One Dosing Interval at Steady State

(NCT01537887)
Timeframe: Predose, 1, 2, 3, 4, 6, 12, 24, 72, and 168 Hours Postdose

Interventionnanograms*hour/milliliter (ng*h/mL) (Geometric Mean)
LY248459548300

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Percentage Change From Baseline to Day 11 in Fasting Lipids and Apolipoproteins

(NCT01537887)
Timeframe: Baseline, Day 11

,
Interventionpercentage change (Mean)
High-density lipoprotein cholesterol (HDL-C)Low-density lipoprotein cholesterol (LDL-C)Apo-A1Apo-B
LY2484595112-3532-24
Placebo-89-98

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Mean Difference Changes From Baseline Versus Placebo in Heart Rate From Time-Matched Analysis by Largest Time Point

The largest time point refers to the estimated largest mean difference between each treatment and placebo among all time points. Values for different treatments can come from different time points. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionbeats per minute (Least Squares Mean)
Anagrelide 0.5 mg7.8
Anagrelide 2.5 mg29.1
Moxifloxacin 400 mg4.3

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Mean Difference Changes From Baseline Versus Placebo in QTcF Intervals at Subject-Specific Tmax

QT interval corrected for heart rate using Fridericia's method (QTcF) at the subject-specific time of maximum plasma concentration. The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg3.7
Anagrelide 2.5 mg4.5
Moxifloxacin 400 mg10.8

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Mean Difference Changes From Baseline Versus Placebo in QTcF Intervals From Time-Matched Analysis by Largest Time Point

QT interval corrected for heart rate using Fridericia's method (QTcF) at the subject-specific time of maximum plasma concentration. The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. The largest time point refers to the estimated largest mean difference between each treatment and placebo among all time points. Values for different treatments can come from different time points. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg5.0
Anagrelide 2.5 mg10.0
Moxifloxacin 400 mg11.8

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Mean Difference Changes From Baseline Versus Placebo in QTcNi Intervals at Subject-Specific Time of Maximum Plasma Concentration (Tmax)

QT interval corrected for heart rate using the subject-specific method (QTcNi) at the subject-specific time of maximum plasma concentration. The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg4.4
Anagrelide 2.5 mg8.2
Moxifloxacin 400 mg11.3

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Mean Difference Changes From Baseline Versus Placebo in QTcNi Intervals From Time-Matched Analysis by Largest Time Point

QT interval corrected for heart rate using the subject-specific method (QTcNi) at the subject-specific time of maximum plasma concentration. The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. The largest time point refers to the estimated largest mean difference between each treatment and placebo among all time points. Values for different treatments can come from different time points. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg7.0
Anagrelide 2.5 mg13.0
Moxifloxacin 400 mg12.6

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Mean Difference Changes From Baseline Versus Placebo in Heart Rate at Subject-Specific Tmax

(NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionbeats per minute (Least Squares Mean)
Anagrelide 0.5 mg4.5
Anagrelide 2.5 mg21.8
Moxifloxacin 400 mg2.9

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Maximum Plasma Concentration (Cmax) of Metabolite of 2.5 mg Anagrelide (BCH24426) in Males and Females

(NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionng/ml (Geometric Mean)
BCH24426 (Males)18.927
BCH24426 (Females)23.785

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Maximum Plasma Concentration (Cmax) of 2.5 mg Anagrelide in Males and Females

(NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionng/ml (Geometric Mean)
Anagrelide 2.5mg (Males)10.592
Anagrelide 2.5mg (Females)16.378

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Maximum Plasma Concentration (Cmax) of 0.5 mg Anagrelide in Males and Females

(NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionng/ml (Geometric Mean)
Anagrelide 0.5 mg (Males)2.083
Anagrelide 0.5 mg (Females)3.64

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Maximum Plasma Concentration (Cmax) of Metabolite of 0.5 mg Anagrelide (BCH24426) in Males and Females

(NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionng/ml (Geometric Mean)
BCH24426 (Males)3.731
BCH24426 (Females)4.534

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Mean Difference Changes From Baseline Versus Placebo in QTcB Intervals From Time-Matched Analysis by Largest Time Point

QT interval corrected for heart rate using Bazett's method (QTcB) at the subject-specific time of maximum plasma concentration. The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. The largest time point refers to the estimated largest mean difference between each treatment and placebo among all time points. Values for different treatments can come from different time points. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg-2.9
Anagrelide 2.5 mg-18.1
Moxifloxacin 400 mg-2.3

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Mean Difference Changes From Baseline Versus Placebo in QTcB Intervals at Subject-Specific Tmax

QT interval corrected for heart rate using Bazett's method (QTcB) at the subject-specific time of maximum plasma concentration. The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg8.5
Anagrelide 2.5 mg25.5
Moxifloxacin 400 mg14.0

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Mean Difference Changes From Baseline Versus Placebo in QT Intervals From Time-Matched Analysis by Largest Time Point

The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. The largest time point refers to the estimated largest mean difference between each treatment and placebo among all time points. Values for different treatments can come from different time points. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg1.7
Anagrelide 2.5 mg-2.4
Moxifloxacin 400 mg9.6

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Mean Difference Changes From Baseline Versus Placebo in QT Intervals at Subject-Specific Tmax

The QT interval is the time it takes for the ventricles of the heart to contract and relax. Data were subtracted from the placebo value. (NCT01552928)
Timeframe: Over 12 hours post-dose

Interventionmsec (Least Squares Mean)
Anagrelide 0.5 mg-6.1
Anagrelide 2.5 mg-34.3
Moxifloxacin 400 mg4.3

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Clinical Cure Rate

Ocular signs of bacterial conjunctivitis (bulbar conjunctival injection and conjunctival discharge/exudates) were rated by the investigator on a 4-point scale, with 0=normal/absent; 1=mild; 2=moderate, and 3=severe. Clinical cure rate is presented as the percentage of participants for which the sum of the numerical scores for the 2 cardinal ocular signs of bacterial conjunctivitis was 0 at Day 9 TOC/Exit Visit. (NCT01573910)
Timeframe: Day 9

Interventionpercentage of participants (Number)
Moxifloxacin85.4
Ofloxacin81.4

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Microbiological Success Rate

Microbiological specimen(s) from the affected eye(s) were collected according to a protocol-defined process. Microbiological success rate is presented as the percentage of participants for which the pre-therapy pathogens at Visit 1 (Day 1) were eradicated at Day 9 TOC/Exit Visit. (NCT01573910)
Timeframe: Day 9

Interventionpercentage of participants (Number)
Moxifloxacin95.3
Ofloxacin94.8

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AUC0-24hour for Pyrazinamide (PZA)

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

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

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Isoniazid PK Parameter Cmax at Day 1

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

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

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Isoniazid PK Parameter CLast at Day 14

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

Interventionng/mL (Median)
RHZE-RHZE50

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Isoniazid PK Parameter CLast at Day 1

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

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

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Isoniazid PK Parameter CL/F at Day 14

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

InterventionL/hour (Median)
RHZE-RHZE30.6

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Isoniazid PK Parameter CL/F at Day 1

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

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

Interventioncorrelation coefficient (Number)
Overall-0.75

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AUC0-24hour for Isoniazid at Day 14

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

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

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

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

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

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Rifampicin PK Parameter Maximum Plasma Concentration (Cmax)

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

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

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Rifampicin PK Parameter Last Concentration (CLast)

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

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

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Rifampicin PK Parameter Clearance (CL/F)

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

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

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Pyrazinamide PK Parameter Cmax

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

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

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Pyrazinamide PK Parameter CLast

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

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

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Pyrazinamide PK Parameter CL/F

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

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

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

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

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

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

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

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

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Ethambutol PK Parameter Cmax

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

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

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Ethambutol PK Parameter CLast

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

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

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Ethambutol PK Parameter CL/F

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

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

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AUC0-24hour for Ethambutol (EMB)

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

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

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Moxifloxacin PK Parameter Cmax at Day 14

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

Interventionng/mL (Median)
RHZE-RMZE3010

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Moxifloxacin PK Parameter CLast at Day 14

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

Interventionng/mL (Median)
RHZE-RMZE178

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Moxifloxacin PK Parameter CL/F at Day 14

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

InterventionL/hour (Median)
RHZE-RMZE17.8

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Isoniazid PK Parameter Cmax at Day 14

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

Interventionng/mL (Median)
RHZE-RHZE3130

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

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

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

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Change From Baseline up to 12 Hours Postdose in QT Interval Corrected for Heart Rate (QTc)

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave. QT intervals from quadruplicate electrocardiogram (ECG) data were corrected for heart rate using Fridericia's formula: QTcF = QT/RR^0.333, where RR is the interval between two R waves. Least squares (LS) mean changes from baseline in QTcF were calculated using a mixed-effects model with baseline QTcF, treatment, time, period, sequence, and the time-by-treatment interaction as fixed effects and participant and the participant-by-period interaction as random effects. (NCT01606436)
Timeframe: Baseline, up to 12 hours postdose in each treatment period

,
Interventionmilliseconds (Least Squares Mean)
0.5 hours2.0 hours3.0 hours4.0 hours5.0 hours6.0 hours8.0 hours12.0 hours
400 mg LY2140023-7.1-4.7-4.0-1.4-2.0-2.6-5.8-6.3
Placebo-7.7-7.6-6.1-2.8-3.5-6.1-7.9-8.0

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Change From Baseline up to 12 Hours Postdose in QT Interval Corrected for Heart Rate (QTc)

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave. QT intervals from quadruplicate electrocardiogram (ECG) data were corrected for heart rate using Fridericia's formula: QTcF = QT/RR^0.333, where RR is the interval between two R waves. Least squares (LS) mean changes from baseline in QTcF were calculated using a mixed-effects model with baseline QTcF, treatment, time, period, sequence, and the time-by-treatment interaction as fixed effects and participant and the participant-by-period interaction as random effects. (NCT01606436)
Timeframe: Baseline, up to 12 hours postdose in each treatment period

Interventionmilliseconds (Least Squares Mean)
0.5 hours2.0 hours3.0 hours4.0 hours12.0 hours
400 mg Moxifloxacin-6.66-2.620.233.52-3.25

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The QTcF Profile of Oral Moxifloxacin (400 mg) in Healthy Japanese Versus Caucasian Subjects

(NCT01642485)
Timeframe: 0 (pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4 and 6 hours post-dose

Interventionms (Mean)
Caucasian Fasted Group9.0
Caucasian Fed Group13.7
Japanese Fasted Group17.3
Japanese Fed Group10.1

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The Effect of Food (Fasted and Fed State) on the Degree of QT Prolongation Caused by Moxifloxacin

The primary baseline corrections were calculated using averaged QTc baseline values (the mean of all median readings recorded for each time-point on the baseline Day -1). This single value (QTcbaselineAV) was used to calculate ΔQTc for each study period. (NCT01642485)
Timeframe: 0 (pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4 and 6 hours post-dose

Interventionms (Mean)
Fasted Group14.4
Fed Group11.6

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The Food Effects (Calorie Reduced FDA Breakfast and Carbohydrate Rich Continental Style) on QTcF

"Scott et al (2002) demonstrated an increase in the heart rate of 10bpm in some healthy subjects following ingestion of a carbohydrate meal. There was significant correlation between the resultant hyperinsulinaemia and an increase in skeletal muscle blood flow, and sympathetic activity, with a reduction in vascular resistance.~If postprandial insulinaemia is a significant influence on the QT interval, then carbohydrate rich meals would be expected to show greater effect. Therefore, to explore this on two separate days of the study subjects will be given one of two different types of breakfast:~A high carbohydrate content breakfast, (>70% carbohydrate)~A reduced calorie FDA standard breakfast, (58% fat, low carbohydrate content) to determine effect on QT interval." (NCT01642485)
Timeframe: 0 (pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4 and 6 hours post-dose

Interventionms (Mean)
FDA Breakfast-6.8
Continental Breakfast-7.9
Placebo at Baseline412.4

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Moxifloxacin 400 mg (Single Dose) Compared to Placebo on the Mean QT/QTc Interval.

"Moxifloxacin 400mg Fasted group is reporting the maximum change in QT/QTc interval from placebo treatment." (NCT01642485)
Timeframe: 0 (pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4 and 6 hours post-dose

Interventionms (Mean)
Moxifloxacin 400 mg Fasted14.4
Placebo414.2

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Insulin, Glucose and C-Peptide Effects on the QT/QTc Interval

The effect on QTc was investigated using linear mixed effect models with placebo corrected QTcF (change from average baseline) as a dependent variable and insulin, glucose and C-peptide (placebo corrected) as covariates for the data obtained under the euglycaemic clamp as well as for all data obtained under the clamp and the two types of breakfast. (NCT01642485)
Timeframe: 0 (pre-dose), 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4 and 6 hours post-dose

Interventionmsec (Median)
Insulin Clamp-0.01
Glucose-0.86
C-peptide-0.71

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Clinical Response in the Clinical Population

Clinical response corresponding clinical cure at End of Study visit. Based on the clinical outcomes, the results of assessment were classified into Clinical Cure, Clinical Failure, Relapse and Indeterminate. (NCT01658020)
Timeframe: 36days

Interventionpercentage of participants (Number)
DW22476.22
Avelox70.99

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Clinical Cure Rate in the Microbiological Per Protocol(PP) Population

"Clinical response corresponding clinical cure in the microbiological per-protocol population.~Microbiological responses were discriminated for the pathogens isolated from the respiratory secretion samples of subjects." (NCT01658020)
Timeframe: 10days

InterventionPercentage of participants (Number)
DW22488.37
Avelox94.87

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Change in EXACT-PRO Score

"The outcome measurement is Change in EXACT-PRO score for clinical populations at Test of cure visit.~EXACT-PRO means that the questionnaires for Exacerbation of Chronic Pulmonary Disease Tool-Patient Reported Outcome of United BioSource Corporation(UBC) of USA that had been standardized, equipped with reliability and feasibility applicable to various COPD patients groups were used in order to quantitate frequency, severity and duration of acute exacerbation as a tool to measure acute exacerbation of COPD.~EXACT-PRO is consisted of 14 questionnaire items were classified into 3 domains, Respiratory Distress Domain, Cough/Sputum Domain, and Chest Symptoms Domain. The Scores of each domain were to be summed into the domain raw summed score or converted into EXACT domain score according to the conversion table. The total score had value in the range from 0 to 100 and higher the value was, severer the respiratory symptoms were in evaluation." (NCT01658020)
Timeframe: 10 days

Interventionscores on a scale (Mean)
DW224-6.90
Avelox-4.29

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Change in CAT Scores

"The outcome measurement is Change in CAT scores for clinical populations at Test of cure visit.~CAT score means that COPD Assessment Test was used as a tool to assess the effects of COPD on physical, mental status and daily life.~CAT is consisted of 8 items in total and each question item was scored from 0 point to 5 point.~The scores of each question item were summed into the total score, which had values between 0 and 40." (NCT01658020)
Timeframe: 10 days

Interventionscores on a scale (Mean)
DW224-4.46
Avelox-2.48

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Microbiological Response Rate

"Microbiological response rate in the microbiological per protocol(PP) population.~Microbiological rate were discriminated for the pathogens isolated from the respiratory secretion samples of subjects." (NCT01658020)
Timeframe: 10days

InterventionPercentage of participants (Number)
DW22467.44
Avelox79.49

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Clinical Response in the Clinical Populations

Clinical response corresponding clinical cure at Test of Cure visit. Based on the clinical outcomes, the results of assessment were classified into Clinical Cure, Clinical Failure, Relapse and Indeterminate. (NCT01658020)
Timeframe: 10days

Interventionpercentage of participants (Number)
DW22486.71
Avelox86.26

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 12 Hours Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 12 hours post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg411.39
Placebo410.24

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) for CP-690,550

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast). (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionng*hr/mL (Geometric Mean)
CP-690,550 100 mg2669.7

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Maximum Observed Plasma Concentration (Cmax) of CP-690,550

(NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionnanogram/milliliter (ng/mL) (Geometric Mean)
CP-690,550 100 mg563.5

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 0.25 Hour Post-Dose

Triplicate 12-lead electrocardiogram (ECG) measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The time corresponding to the beginning of depolarization to repolarization of the ventricles (QT interval) was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as Least Squares (LS) mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 0.25 hour post-dose

Interventionmilliseconds (msec) (Least Squares Mean)
CP-690,550 100 mg416.48
Placebo417.77

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 0.5 Hour Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 0.5 hour post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg414.70
Placebo416.12

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 1 Hour Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 1 hour post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg414.69
Placebo416.98

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 16 Hours Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 16 hours post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg415.87
Placebo413.72

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 24 Hours Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 24 hours post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg412.53
Placebo411.18

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 4 Hours Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 4 hours post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg416.83
Placebo415.76

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 8 Hours Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 8 hours post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg409.25
Placebo408.39

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Mean Time-Matched Difference in QTcF Intervals Between Moxifloxacin Compared to Placebo

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (moxifloxacin minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 2 hours post-dose

Interventionmsec (Least Squares Mean)
Moxifloxacin 400 mg426.34
Placebo415.05

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Plasma Decay Half-Life (t1/2) of CP-690,550

Plasma decay half-life is the time measured for the plasma concentration of drug to decrease by one half. (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionhours (Mean)
CP-690,550 100 mg3.284

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Mean Time-Matched Difference in QTcB Intervals Between CP-690,550 Compared to Placebo

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Bazett's formula (QTcB = QT divided by square root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 0.25, 0.5, 1, 2, 4, 8, 12, 16, and 24 hours post-dose

,
Interventionmsec (Least Squares Mean)
0.25 Hour Post-Dose0.5 Hour Post-Dose1 Hour Post-Dose2 Hours Post-Dose4 Hours Post-Dose8 Hours Post-Dose12 Hours Post-Dose16 Hours Post-Dose24 Hours Post-Dose
CP-690,550 100 mg416.40416.69417.98414.54417.26412.91416.76416.44413.93
Placebo416.24414.91414.99413.46415.10412.86416.27414.33413.14

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Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] for CP-690,550

AUC (0 - ∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionnanogram*hour/milliliter (ng*hr/mL) (Geometric Mean)
CP-690,550 100 mg2682.6

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Mean Time-Matched Difference in QTcF Intervals Between CP-690,550 Compared to Placebo at 2 Hours Post-Dose

Triplicate 12-lead ECG measurements (each recording separated by approximately 2 minutes) were performed and average was calculated. The QT interval was adjusted for RR interval using the QT and RR from each ECG by Fridericia's formula (QTcF = QT divided by cube root of RR). Data is reported as LS mean difference (CP-690,550 minus Placebo, baseline-adjusted). (NCT01743677)
Timeframe: 2 hours post-dose

Interventionmsec (Least Squares Mean)
CP-690,550 100 mg413.70
Placebo415.05

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Plasma Decay Half-Life (t1/2) of CP-690,550 by CYP2C19 Genotype

Plasma decay half-life is the time measured for the plasma concentration to decrease by one half. Variation in CYP2C19 gene affected the pharmacokinetics of CP-690,550. t1/2 categorized by genotype as poor metabolizer, extensive metabolizer and ultra extensive metabolizer of CYP2C19. (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionhours (Mean)
Poor MetabolizerExtensive MetabolizerUltra Extensive Metabolizer
CP-690,550 100 mg3.0053.3203.201

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Area Under the Curve From Time Zero to Extrapolated Infinite Time [AUC (0 - ∞)] of CP-690,550 by Cytochrome P450 2C19 (CYP2C19) Genotype

AUC (0 - ∞)= Area under the plasma concentration versus time curve (AUC) from time zero (pre-dose) to extrapolated infinite time (0 - ∞). It is obtained from AUC (0 - t) plus AUC (t - ∞). Variation in CYP2C19 gene affected the pharmacokinetics of CP-690,550. AUC (0 - ∞) categorized by genotype into poor metabolizer, extensive metabolizer and ultra extensive metabolizer of CYP2C19. (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionng*hr/mL (Geometric Mean)
Poor MetabolizerExtensive MetabolizerUltra Extensive Metabolizer
CP-690,550 100 mg3127.52683.51677.7

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Time to Reach Maximum Observed Plasma Concentration (Tmax) for CP-690,550

(NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionhours (Median)
CP-690,550 100 mg1.000

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Maximum Observed Plasma Concentration (Cmax) of CP-690,550 by CYP2C19 Genotype

Variation in CYP2C19 gene affected the pharmacokinetics of CP-690,550. Cmax categorized by genotype as poor metabolizer, extensive metabolizer and ultra extensive metabolizer of CYP2C19. (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionng/mL (Geometric Mean)
Poor MetabolizerExtensive MetabolizerUltra Extensive Metabolizer
CP-690,550 100 mg647.4565.0346.9

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Area Under the Curve From Time Zero to Last Quantifiable Concentration (AUClast) of CP-690,550 by CYP2C19 Genotype

Area under the plasma concentration time-curve from zero to the last measured concentration (AUClast). Variation in CYP2C19 gene affected the pharmacokinetics of CP-690,550. AUClast categorized by genotype as poor metabolizer, extensive metabolizer and ultra extensive metabolizer of CYP2C19. (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionng*hr/mL (Geometric Mean)
Poor MetabolizerExtensive MetabolizerUltra Extensive Metabolizer
CP-690,550 100 mg3114.32670.21673.1

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Time to Reach Maximum Observed Plasma Concentration (Tmax) of CP-690,550 by CYP2C19 Genotype

Variation in CYP2C19 gene affected the pharmacokinetics of CP-690,550. Tmax categorized by genotype as poor metabolizer, extensive metabolizer and ultra extensive metabolizer of CYP2C19. (NCT01743677)
Timeframe: 0 (pre-dose), and 0.25, 0.5, 1, 2, 4, 8, 12, 16 and 24 hours post-dose

Interventionhours (Median)
Poor MetabolizerExtensive MetabolizerUltra Extensive Metabolizer
CP-690,550 100 mg0.5001.0002.000

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PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpicogram x hour per ml (pg*hour/ml) (Geometric Mean)
Ortho-Cyclen907
Ortho-Cyclen + Evacetrapib840

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

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionhour (Median)
Ortho-Cyclen3.53
Ortho-Cyclen + Evacetrapib4.00

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PK: Time of Maximum Observed Drug Concentration (Tmax) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionhour (Median)
Ortho-Cyclen3.00
Ortho-Cyclen + Evacetrapib4.00

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PK: Minimum Observed Drug Concentration (Cmin) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg/ml (Geometric Mean)
Ortho-Cyclen397
Ortho-Cyclen + Evacetrapib422

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PK: Minimum Observed Drug Concentration (Cmin) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg/ml (Geometric Mean)
Ortho-Cyclen15.9
Ortho-Cyclen + Evacetrapib13.2

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Pharmacokinetics (PK): Maximum Concentration (Cmax) of Ethinyl Estradiol

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpicogram per milliliter (pg/ml) (Geometric Mean)
Ortho-Cyclen71.7
Ortho-Cyclen + Evacetrapib70.6

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PK: Maximum Concentration (Cmax) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg/ml (Geometric Mean)
Ortho-Cyclen1410
Ortho-Cyclen + Evacetrapib1830

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PK: Area Under the Concentration Curve Over a 24 Hour Dosing Interval (AUCτ) of Norelgestromin

(NCT01746732)
Timeframe: Day 21: Predose, 0.5,1,1.5,2,3,4,5,6,8,10,12,16 and 24 hours post dose

Interventionpg*hour/ml (Geometric Mean)
Ortho-Cyclen16200
Ortho-Cyclen + Evacetrapib18100

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Frequency of Adverse Events

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

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

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

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

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

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Sputum Culture Conversion (2 Negative Cultures) Using Liquid Media

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

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

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Maximum Plasma Concentration (Cmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.

(NCT01839279)
Timeframe: 0.5, 1, 1.5, 2, 4, 8, 12 & 24 hours post dose on Days 5 (8 mg) and 14 (24 mg)

Interventionng/mL (Geometric Mean)
Day 5 (Tizanidine 8 mg)11.7
Day 14 (Tizanidine 24 mg)27.4

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Time to Reach Maximum Plasma Concentration (Tmax) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.

(NCT01839279)
Timeframe: 0.5, 1, 1.5, 2, 4, 8, 12 & 24 hours post dose on Days 5 (8 mg) and 14 (24 mg)

Interventionhour (Median)
Day 5 (Tizanidine 8 mg)1.35
Day 14 (Tizanidine 24 mg)2.10

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The Baseline-adjusted, Placebo-corrected (ΔΔQTc) on QTc Method Not Selected as Primary Endpoint.

Change from baseline in Cardiac Repolarization (QTc Interval) at Day 5 (Tizanidine 8 mg). Moxifloxacin was not investigational drug, it was used to assess the sensitivity of the study. (NCT01839279)
Timeframe: Baseline and Day 5

,,
Interventionmsec (Least Squares Mean)
Timepoint (Hour) 00.511.52481224
Tizanidine 8 mg-0.8-0.40.01.1-0.42.6-1.5-0.1-0.5
Tizanidine 8 mg Placebo-corrected0.1-0.8-2.3-0.1-0.71.6-2.2-0.8-1.9
Tizanidine Placebo 8 mg-0.90.42.31.30.41.00.60.71.4

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Assessing the Relationship Between Changes in the QTc Interval and Plasma Levels of Tizanidine Using Concentration-effect Modeling

The relationship will be quantified using a linear mixed effects model with an intercept. Data from Day 5 and Day 14 were fitted into regression model to obtain a slope of change. The measure type 'Number' followed by (90% Confidence Interval) shown in results is the slope from the linear fit. (NCT01839279)
Timeframe: Day 5, Day 14

Interventionmsec per ng/mL (Number)
Tizanidine-0.1209

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The Primary Endpoint Will be the Baseline-adjusted, Placebo-corrected Effect on QTc (ΔΔQTc) on Day 14.

Change from baseline in Cardiac Repolarization (QTc Interval) at Day 14 (Tizanidine 24 mg). Moxifloxacin was not investigational drug, it was used to assess the sensitivity of the study. (NCT01839279)
Timeframe: Baseline and Day 14

,,
Interventionmilliseconds (msec) (Least Squares Mean)
Timepoint (Hour) 00.511.52481224
Tizanidine 24 mg-4.3-2.0-4.0-4.7-3.61.6-2.4-2.00.4
Tizanidine 24 mg Placebo-corrected-3.7-3.2-6.6-7.4-6.4-1.8-5.5-3.0-2.2
Tizanidine Placebo 24 mg-0.51.22.62.72.93.43.11.02.6

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Area Under the Plasma Concentration-time Curve During a Dosing Interval (AUCt) of Single Doses of 8 and 24 mg Tizanidine After Reaching Steady State.

(NCT01839279)
Timeframe: 0.5, 1, 1.5, 2, 4, 8, 12 & 24 hours post dose on Days 5 (8 mg) and 14 (24 mg)

Interventionng*hr/mL (Geometric Mean)
Day 5 (Tizanidine 8 mg)32.4
Day 14 (Tizanidine 24 mg)115

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Maximum Effect of ADASUVE on Cardiac Repolarization (QTc Interval Duration) at the Maximum Clinical Dose Compared to Placebo

Time-matched differences in QTcI values between the maximum of the mean difference from baseline of the QTcI interval after time-matched placebo subtraction for ADASUVE treatment at 12 post-inhalation times. (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmsec (Least Squares Mean)
ADASUVE-Placebo Crossover Subjects4.04

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QTc Versus Loxapine Concentration

QTc @ Cmax based on linear and nonlinear regression of QTcI versus time matched serum loxapine concentrations (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmsec (Least Squares Mean)
ADASUVE 10 mg x 2 Doses2.6

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Subjects With QTcI > 450 ms

Numbers of Subjects with QTcI > 450 ms at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo2
ADASUVE 10 mg x 2 Doses2

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Subjects With QTcI > 480 ms

Numbers of Subjects with QTcI > 480 ms (or 500 ms) at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo0
ADASUVE 10 mg x 2 Doses0

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Subjects With QTcI Increase > 30 ms From Baseline

Numbers of Subjects with QTcI Increase > 30 ms from Baseline at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo0
ADASUVE 10 mg x 2 Doses1

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Subjects With QTcI Increase > 60 ms From Baseline

Numbers of Subjects with QTcI Increase > 60 ms From Baseline at any time point (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

InterventionParticipants (Count of Participants)
Inhaled Placebo + Oral Placebo0
ADASUVE 10 mg x 2 Doses0

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Maximum Effect of Moxifloxacin on Cardiac Repolarization (QTc Interval Duration) Compared to Placebo (Study Assay Sensitivity)

A thorough QT/QTc study may be considered to have demonstrated assay sensitivity if 1 or more of the lower 95% CI values exceeds 5 msec (NCT01854710)
Timeframe: Predose, 2 min, 1, 1.5 hr, 2 hr 2 min, 2 hr 5 min, 2.5, 3, 5, 8, 12, and 24 hr

Interventionmsec (Least Squares Mean)
Moxifloxacin QT Crossover Subjects10.47

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Mean Aqueous Humor Concentration of Moxifloxacin

A 0.150 milliliter sample of the aqueous humor was obtained during cataract surgery. The concentration of moxifloxacin was measured by a validated procedure using high performance liquid-spectrometry. (NCT01859702)
Timeframe: Day 3 (operative day)

Interventionnanograms per milliliter (Mean)
VIGADEXA1110.6

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Tmax of Deferiprone and Deferiprone 3-O-glucuronide

"To evaluate the Tmax of deferiprone and deferiprone 3-O-glucuronide following administration of single doses of 33 and 50 mg/kg deferiprone in healthy volunteers.~Serial blood samples were collected prior to dosing and within 5 minutes following completion of each scheduled post-dose ECG at Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

,
Interventionhour (Median)
Tmax of serum deferiproneTmax of serum deferiprone -O-glucuronide
Arm A - Maximum Therapeutic Dose0.81853.066
Treatment Arm B - Supratherapeutic Dose0.81753.071

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T1/2 for Serum Deferiprone and Deferiprone 3-O-glucuronide

"T1/2 was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite in healthy volunteers.~Serial blood samples were collected prior to dosing and within 5 minutes following completion of each scheduled post-dose ECG at Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

,
Interventionhour (Mean)
T1/2 for serum deferiproneT1/2 for serum deferiprone 3-O-glucuronide
Arm A - Maximum Therapeutic Dose1.82.5
Treatment Arm B - Supratherapeutic Dose1.82.6

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Maximum Postdose QT/QTc Interval

"The maximum post-dose QT/QTc interval for deferiprone and placebo.~ECG recordings were obtained within a 5-minute time window at Hours -0.75, -0.5, and -0.25 (prior to dosing) and Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

,,,
Interventionpercentage of participants (Number)
QTcF ≤ 450 msecQTcF > 450 to ≤ 480 msecQTcF > 480 to ≤ 500 msecQTcF > 500 msec
Arm A - Maximum Therapeutic Dose100000
Arm B - Supratherapeutic Dose96400
Arm C - Placebo Control98200
Arm D - Positive Control891100

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Maximum Change From Baseline (dQT/dQTc)

"Maximum Change From Baseline (dQT/dQTc) for deferiprone and placebo.~ECG recordings were obtained within a 5-minute time window at Hours -0.75, -0.5, and -0.25 (prior to dosing) and Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

,,,
Interventionpercentage of participants (Number)
QTcF ≤ 30 msecQTcF >30 but ≤ 60 msecQTcF >60 msec
Arm A - Maximum Therapeutic Dose10000
Arm B - Supratherapeutic Dose10000
Arm C - Placebo Control10000
Arm D - Positive Control9640

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Cmax of Deferiprone and Deferiprone 3-O Glucuronide

"To evaluate the Cmax of deferiprone and deferiprone 3-O-glucuronide following administration of single doses of 33 and 50 mg/kg deferiprone in healthy volunteers.~Serial blood samples were collected prior to dosing and within 5 minutes following completion of each scheduled post-dose ECG at Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

,
Interventionμg/mL (Mean)
Cmax of serum deferiproneCmax of serum deferiprone 3-O-glucuronide
Arm A - Maximum Therapeutic Dose34.135.2
Treatment Arm B - Supratherapeutic Dose54.451.4

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AUC0-infinity for Serum Deferiprone and Deferiprone 3-O-glucuronide

"AUC0-infinity was assessed over a 24-hour interval for analyses of deferiprone and its 3-O-glucuronide metabolite in healthy volunteers.~Serial blood samples were collected prior to dosing and within 5 minutes following completion of each scheduled post-dose ECG at Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

,
Interventionμg *hr/mL (Mean)
AUC0-infinity for serum deferiproneAUC0-infinity for serum deferiprone -O-glucuronide
Arm A - Maximum Therapeutic Dose95.4205.5
Treatment Arm B - Supratherapeutic Dose152.1331.2

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Number of Participants With Adverse Events

Number of participants with adverse events following therapeutic and supratherapeutic doses of deferiprone (NCT01860703)
Timeframe: From administration of the first dose until 7 days +/- 1 day following the final dose

Interventionparticipants (Number)
Arm A - Maximum Therapeutic Dose12
Treatment Arm B - Supratherapeutic Dose35
Arm C - Placebo Control10
Arm D - Positive Control5

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Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of Moxifloxacin

"Change from baseline in QTcF interval was measured by looking at the post-dose difference in change from baseline in Fridericia's QT corrected heart rate (dQTcF) between treatment and placebo (ddQTcF) at each time interval.~ECG recordings were obtained within a 5-minute time window at Hours -0.75, -0.5, and -0.25 (prior to dosing) and Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

Interventionmilliseconds (Least Squares Mean)
Positive Control14.7
Placebo Control1.2

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Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 50 mg/kg Deferiprone

"Change from baseline in QTcF interval was measured by looking at the post-dose difference in change from baseline in Fridericia's QT corrected heart rate (dQTcF) between treatment and placebo (ddQTcF) at each time interval.~ECG recordings were obtained within a 5-minute time window at Hours -0.75, -0.5, and -0.25 (prior to dosing) and Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

Interventionmilliseconds (Least Squares Mean)
50 mg/kg Deferiprone3.5
Placebo Control-1.7

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Maximum Difference in Change From Baseline in ddQTcF Following a Single Dose of 33 mg/kg Deferiprone

"Change from baseline in QTcF interval was measured by looking at the post-dose difference in change from baseline in Fridericia's QT corrected heart rate (dQTcF) between treatment and placebo (ddQTcF) at each time interval.~ECG recordings were obtained within a 5-minute time window at Hours -0.75, -0.5, and -0.25 (prior to dosing) and Hours 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2, 3, 4, 6, 8, 10, and 24 post-dose." (NCT01860703)
Timeframe: 24-hour interval

Interventionmilliseconds (Least Squares Mean)
33 mg/kg Deferiprone1.4
Placebo Control-1.6

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Scarring

Scarring will be evaluated and measured in millimeters at Day 29 and classified as either peripheral or central. (NCT01928693)
Timeframe: 29 days

Interventionmillimeters (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution0

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Complete Healing

The primary outcome will be complete healing of the corneal ulcer, defined as complete reepithelialization by Day 29. (NCT01928693)
Timeframe: 29 days

Interventionparticipant (Number)
Zymaxid 0.5% Ophthalmic Solution1
Vigamox 0.5% Ophthalmic Solution1

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Healing Rate

Time to corneal ulcer reduction and/or total healing over a treatment course of 21 days. (NCT01928693)
Timeframe: 29 days

InterventionDays (Number)
Zymaxid 0.5% Ophthalmic Solution21
Vigamox 0.5% Ophthalmic Solution21

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Number of Participants With Treatment Failure

(NCT01928693)
Timeframe: 29 days

Interventionparticipants (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution0

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Patient Pain Scores

Patients will be asked to grade the overall pain of the affected eye at each visit on a Scale= 0--None, 1- Mild, 2- Moderate, 3- Severe (NCT01928693)
Timeframe: Average of 6 times in a 29 day period

Interventionunits on a scale (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution2

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Patient Satisfaction Scores

Patient satisfaction outcomes will be assessed using a series of survey questions ranging in both categorical and continuous outcomes. Treatment will be compared using either methods for differences in binomial proportions or the Wilcoxon Rank Sum test. Scale= 0- Very Comfortable, 1- Comfortable, 2- Uncomfortable, 3- Very Uncomfortable (NCT01928693)
Timeframe: Average of 6 times in a 29 day period

Interventionunits on a scale (Number)
Zymaxid 0.5% Ophthalmic Solution0
Vigamox 0.5% Ophthalmic Solution2

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Subject Number for Microbiologically Cured and Failure at Visit 3 in b-mITT (Bacteriological mITT) Population

"Microbiological efficacy at visits 3 would be determined by assessing the identification results from the central laboratory. Subjects must satisfy at least one of the following in order to be evaluated for the microbiological efficacy:~Subjects whose respiratory culture from visit 1 was positive;~Subjects whose blood culture from visit 1 was positive.~The microbiological efficacy at Visit 3 and treatment group (determined by each subject) was determined by the number and percentage of microbiological success subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model." (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 3 (Within 24 hours after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailureNot evaluable
Moxifloxacin 400 mg1601
Nemonoxacin 500 mg2220
Nemonoxacin 650 mg1810

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Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 3 in the mITT Population

The primary efficacy endpoint of this study was to evaluate whether the clinical cure rate of Nemonoxacin malate sodium chloride is non-inferior to that of Moxifloxacin at visit 3 in the mITT population. At visit 3, the Investigator would assess changes in the symptoms/signs/laboratory tests and chest X-rays/or CT scans associated with this infection, and determined the clinical efficacy in the subjects. The clinical efficacy of the study group and the control group was calculated according to the proportion and percentage of overall clinically cured and clinically ineffective patients in the treatment groups. If the lower limit of the 90% confidence interval for the difference in the clinical cure rate between the study drug and the control drug was larger than -15%, it would be established that the efficacy of Nemonoxacin malate sodium chloride injection was not inferior to that of Moxifloxacin Hydrochloride Sodium Chloride Injection in the treatment of moderate to severe adult CAP. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 3 (Within 24 hours after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailNot evaluable
Moxifloxacin 400 mg5923
Nemonoxacin 500 mg6142
Nemonoxacin 650 mg6040

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Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 4 in the Clinically Evaluable (CE) Population

The primary efficacy endpoint of this study was to evaluate whether the clinical cure rate of Nemonoxacin malate sodium chloride is non-inferior to that of Moxifloxacin at visit 4 in the CE population. At visit 4, the Investigator would assess changes in the symptoms/signs/laboratory tests and chest X-rays/or CT scans associated with this infection, and determined the clinical efficacy in the subjects. The clinical efficacy of the study group and the control group was calculated according to the proportion and percentage of overall clinically cured and clinically ineffective patients in the treatment groups. If the lower limit of the 90% confidence interval for the difference in the clinical cure rate between the study drug and the control drug was larger than -15%, it would be established that the efficacy of Nemonoxacin malate sodium chloride injection was not inferior to that of Moxifloxacin Hydrochloride Sodium Chloride Injection in the treatment of moderate to severe adult CAP. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 4 (7-14 days after stopping the drug)

,,
Interventionparticipants (Number)
SuccessNot evaluable
Moxifloxacin 400 mg582
Nemonoxacin 500 mg567
Nemonoxacin 650 mg563

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Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 4 in the mITT Population

The primary efficacy endpoint of this study was to evaluate whether the clinical cure rate of Nemonoxacin malate sodium chloride is non-inferior to that of Moxifloxacin at visit 4 in the mITT population. At visit 4, the Investigator would assess changes in the symptoms/signs/laboratory tests and chest X-rays/or CT scans associated with this infection, and determined the clinical efficacy in the subjects. The clinical efficacy of the study group and the control group was calculated according to the proportion and percentage of overall clinically cured and clinically ineffective patients in the treatment groups. If the lower limit of the 90% confidence interval for the difference in the clinical cure rate between the study drug and the control drug was larger than -15%, it would be established that the efficacy of Nemonoxacin malate sodium chloride injection was not inferior to that of Moxifloxacin Hydrochloride Sodium Chloride Injection in the treatment of moderate to severe adult CAP. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 4 (7-14 days after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailNot evaluable
Moxifloxacin 400 mg5923
Nemonoxacin 500 mg6070
Nemonoxacin 650 mg5842

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Subject Number for Microbiologically Cured and Failure at Visit 3 in BE (Bacteriological Evaluable) Population

"Microbiological efficacy at visits 3 would be determined by assessing the identification results from the central laboratory. Subjects must satisfy at least one of the following in order to be evaluated for the microbiological efficacy:~Subjects whose respiratory culture from visit 1 was positive;~Subjects whose blood culture from visit 1 was positive.~The microbiological efficacy at Visit 3 and treatment group (determined by each subject) was determined by the number and percentage of microbiological success subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model." (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 3 (Within 24 hours after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailureNot evaluable
Moxifloxacin 400 mg1600
Nemonoxacin 500 mg2120
Nemonoxacin 650 mg1810

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Subject Number for Microbiologically Cured and Failure at Visit 4 in b-mITT (Bacteriological mITT) Population

"Microbiological efficacy at visits 4 would be determined by assessing the identification results from the central laboratory. Subjects must satisfy at least one of the following in order to be evaluated for the microbiological efficacy:~Subjects whose respiratory culture from visit 1 was positive;~Subjects whose blood culture from visit 1 was positive.~The microbiological efficacy at Visit 4 and treatment group (determined by each subject) was determined by the number and percentage of microbiological success subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model." (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 4 (7-14 days after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailureNot evaluable
Moxifloxacin 400 mg1601
Nemonoxacin 500 mg2130
Nemonoxacin 650 mg1711

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Subject Number of Success and Failure in Overall Efficacy at Visit 3 in b-mITT (Bacteriological mITT) Population

Only subjects whose bacterial culture from visit 1 was positive would be evaluated for the overall efficacy. The overall efficacy (cured or ineffective) at Visit 3 and treatment group (determined by each subject) was determined by the number and percentage of subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 3 (Within 24 hours after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailureUnevaluable
Moxifloxacin 400 mg1511
Nemonoxacin 500 mg2220
Nemonoxacin 650 mg1720

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Subject Number for Microbiologically Cured and Failure at Visit 4 in BE (Bacteriological Evaluable) Population

"Microbiological efficacy at visits 4 would be determined by assessing the identification results from the central laboratory. Subjects must satisfy at least one of the following in order to be evaluated for the microbiological efficacy:~Subjects whose respiratory culture from visit 1 was positive;~Subjects whose blood culture from visit 1 was positive.~The microbiological efficacy at Visit 4 and treatment group (determined by each subject) was determined by the number and percentage of microbiological success subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model." (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 4 (7-14 days after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailureNot evaluable
Moxifloxacin 400 mg1501
Nemonoxacin 500 mg2030
Nemonoxacin 650 mg1711

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Subject Number of Success and Failure in Overall Efficacy at Visit 3 in BE (Bacteriological Evaluable) Population

Only subjects whose bacterial culture from visit 1 was positive would be evaluated for the overall efficacy. The overall efficacy (cured or ineffective) at Visit 3 and treatment group (determined by each subject) was determined by the number and percentage of subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 3 (Within 24 hours after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailure
Moxifloxacin 400 mg151
Nemonoxacin 500 mg212
Nemonoxacin 650 mg172

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Subject Number of Success and Failure in Overall Efficacy at Visit 4 in b-mITT (Bacteriological mITT) Population

Only subjects whose bacterial culture from visit 1 was positive would be evaluated for the overall efficacy. The overall efficacy (cured or ineffective) at Visit 4 and treatment group (determined by each subject) was determined by the number and percentage of subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 4 (7-14 days after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailure
Moxifloxacin 400 mg161
Nemonoxacin 500 mg213
Nemonoxacin 650 mg172

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Subject Number of Success and Failure in Overall Efficacy at Visit 4 in BE (Bacteriological Evaluable) Population

Only subjects whose bacterial culture from visit 1 was positive would be evaluated for the overall efficacy. The overall efficacy (cured or ineffective) at Visit 4 and treatment group (determined by each subject) was determined by the number and percentage of subjects. The difference in bacteriological success between Nemonoxacin malate sodium chloride injection and Moxifloxacin Hydrochloride Sodium Chloride Injection was tested using the logistic regression model. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 4 (7-14 days after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailure
Moxifloxacin 400 mg151
Nemonoxacin 500 mg203
Nemonoxacin 650 mg172

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Difference in the Clinical Cure Rate of Two Doses of Intravenously Infused Nemonoxacin Malate Sodium Chloride Injection at Visit 3 in the CE Population

The primary efficacy endpoint of this study was to evaluate whether the clinical cure rate of Nemonoxacin malate sodium chloride is non-inferior to that of Moxifloxacin at visit 3 in the CE population. At visit 3, the Investigator would assess changes in the symptoms/signs/laboratory tests and chest X-rays/or CT scans associated with this infection, and determined the clinical efficacy in the subjects. The clinical efficacy of the study group and the control group was calculated according to the proportion and percentage of overall clinically cured and clinically ineffective patients in the treatment groups. If the lower limit of the 90% confidence interval for the difference in the clinical cure rate between the study drug and the control drug was larger than -15%, it would be established that the efficacy of Nemonoxacin malate sodium chloride injection was not inferior to that of Moxifloxacin Hydrochloride Sodium Chloride Injection in the treatment of moderate to severe adult CAP. (NCT01944774)
Timeframe: Visit 1 (baseline, day -1~1) to Visit 3 (Within 24 hours after stopping the drug)

,,
Interventionparticipants (Number)
SuccessFailNot evaluable
Moxifloxacin 400 mg5622
Nemonoxacin 500 mg5841
Nemonoxacin 650 mg5630

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Maximum Mean Placebo-corrected QTcN Change From Baseline Between 1 to 24 Hours on Day 1 for the Combination Therapy

"Maximum mean placebo-corrected QT interval corrected for heart rate according to a parabolic population model (QTcN) change from baseline between 1 to 24 hours on Day 1 for the combination therapy is estimated.~QTcN denotes the population heart rate corrected QT interval length, based on a parabolic model. 'Baseline' denotes the mean of the pre-dose ECG measurements prior to (first) dose at Visits 2, 3 or 4, determined separately for each treatment period. 'Global baseline' refers to the mean of all available period baseline values." (NCT01965431)
Timeframe: 20min,15min and 10min prior to drug administration on day -2 (baseline) and 1h (hours), 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h and 24h after drug adminstration on day 1

Interventionms (Mean)
BI 207127+ Faldaprevir-0.47
Placebo to BI 207127 + Placebo to Faldaprevir-8.37

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Maximum Mean Placebo-corrected HR Change From Baseline Between 1 to 24 Hours on Day 1 for the Combination Therapy

Maximum mean placebo-corrected heart rate (HR) change from baseline between 1 to 24 hours on Day 1 for the combination therapy is estimated. HR was derived from the RR interval. (NCT01965431)
Timeframe: 20min,15min and 10min prior to drug administration on day -2 (baseline) and 1h (hours), 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h and 24h after drug adminstration on day 1

Interventionbpm (Mean)
BI 207127 + Faldaprevir-3.47
Placebo to BI 207127) + Placebo to Faldaprevir-3.64

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Minimum Mean Placebo-corrected HR (Heart Rate) Change From Baseline Between 1 to 24 Hours on Day 1 for the Combination Therapy

Minimum mean placebo-corrected HR (heart rate) change from baseline between 1 to 24 hours on Day 1 for the combination therapy is estimated. HR was derived from the RR interval. (NCT01965431)
Timeframe: 20min,15min and 10min prior to drug administration on day -2 (baseline) and 1h (hours), 2h, 3h, 4h, 5h, 6h, 8h, 10h, 12h and 24h after drug adminstration on day 1

Interventionbpm (Mean)
BI 207127 + Faldaprevir-0.68
Placebo to BI 207127 + Placebo to Faldaprevir3.74

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Maximum Mean Placebo-corrected QTcN Change From Baseline Between 1 to 6 Hours on Day 1 for the Moxifloxacin Treatment

"Maximum mean placebo-corrected QTcN change from baseline between 1 to 6 hours on Day 1 for the Moxifloxacin treatment is estimated.~QTcN denotes the population heart rate corrected QT interval length, based on a parabolic model. 'Baseline' denotes the mean of the pre-dose ECG measurements prior to (first) dose at Visits 2, 3 or 4, determined separately for each treatment period. 'Global baseline' refers to the mean of all available period baseline values." (NCT01965431)
Timeframe: 20min,15min and 10min prior to drug administration on day -2 (baseline) and 1h (hours), 2h, 3h, 4h, 5h and 6h after drug adminstration on day 1

Interventionms (Mean)
Moxifloxacin14.95
Placebo to BI 207127 + Placebo to Faldaprevir2.25

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ECG Morphology

"Morphological analyses were performed with regard to the digital ECG waveform interpretation as defined by a central ECG laboratory's cardiologist blinded to the study treatment. Changes from baseline to each day of treatment were evaluated separately. Any T-U wave complex that suggested an abnormal form compatible with an effect on cardiac repolarization was noted. New ECG morphological onset changes were presented as the percentage of subjects meeting the new criterion (new meant not present on any baseline ECG and became present on at least 1 on-treatment ECG) for the following variables:~Second degree heart block~Third degree heart block~Complete right bundle branch block (RBBB)~Complete left bundle branch block (LBBB)~ST segment changes (elevation and depression separately)~T-wave abnormalities (negative T waves only)~Myocardial infarction (MI) pattern~Any new abnormal U waves" (NCT01999114)
Timeframe: Baseline to Day 17

,,,,
InterventionParticipants (Count of Participants)
New abnormal U wavesNew T wave (negative) invertedNew ST segment depression changesNew ST segment elevation changesNew complete RBBB & LBBBNew MINew 2nd or 3rd degree heart block
BTDS Only0010000
BTDS With Naltrexone0100000
Moxifloxacin0110000
Naltrexone Alone0000000
Placebo0000000

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ECG Morphology

"Morphological analyses were performed with regard to the digital ECG waveform interpretation as defined by a central ECG laboratory's cardiologist blinded to the study treatment. Changes from baseline to each day of treatment were evaluated separately. Any T-U wave complex that suggested an abnormal form compatible with an effect on cardiac repolarization was noted. New ECG morphological onset changes were presented as the percentage of subjects meeting the new criterion (new meant not present on any baseline ECG and became present on at least 1 on-treatment ECG) for the following variables:~Second degree heart block~Third degree heart block~Complete right bundle branch block (RBBB)~Complete left bundle branch block (LBBB)~ST segment changes (elevation and depression separately)~T-wave abnormalities (negative T waves only)~Myocardial infarction (MI) pattern~Any new abnormal U waves" (NCT01999114)
Timeframe: Baseline to Day 13

,,,,
InterventionParticipants (Count of Participants)
New abnormal U wavesNew T wave (negative) invertedNew ST segment depression changesNew ST segment elevation changesNew complete RBBB & LBBBNew MINew 2nd or 3rd degree heart block
BTDS Only1000000
BTDS With Naltrexone0110000
Moxifloxacin0110000
Naltrexone Alone0100000
Placebo0001000

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The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)

The effects of 80 mcg/hr buprenorphine (Day 17) delivered by BTDS alone, or by BTDS dosed with naltrexone, and naltrexone alone on cardiac repolarization, were assessed based on the corrected QT interval since HR inversely affects QT duration. The time-matched analysis was conducted as the primary endpoint as recommended by ICH E14, with the 2-sided 90% confidence interval for each treatment at each time point showing the placebo- and baseline-corrected (ΔΔ) analysis for QTcI. The effect of BTDS 80 on QT intervals was compared with the moxifloxacin-positive control after placebo and baseline correction. (NCT01999114)
Timeframe: Baseline to Day 17

Interventionmsec (Mean)
BTDS Only (Placebo-corrected ΔΔQTcI)11.46
BTDS With Naltrexone (Placebo-corrected ΔΔQTcI)4.47
Naltrexone Alone (Placebo-corrected ΔΔQTcI)1.50
Moxifloxacin (Placebo-corrected ΔΔQTcI)10.78

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The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)

The effects of 40 mcg/hr buprenorphine (Day 13) delivered by BTDS alone, or by BTDS dosed with naltrexone, and naltrexone alone on cardiac repolarization, were assessed based on the corrected QT interval since HR inversely affects QT duration. The time-matched analysis was conducted as the primary endpoint as recommended by ICH E14, with the 2-sided 90% confidence interval for each treatment at each time point showing the placebo- and baseline-corrected (ΔΔ) analysis for QTcI. The effect of BTDS 40 on QT intervals was compared with the moxifloxacin-positive control after placebo and baseline correction. (NCT01999114)
Timeframe: Baseline to Day 13

Interventionmsec (Mean)
BTDS Only (Placebo-corrected ΔΔQTcI)9.16
BTDS With Naltrexone (Placebo-corrected ΔΔQTcI)5.12
Naltrexone Alone (Placebo-corrected ΔΔQTcI)1.81
Moxifloxacin (Placebo-corrected ΔΔQTcI)10.68

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The Maximum Time-matched Change From Baseline in QT Data Corrected for Heart Rate (QTc), Placebo-corrected, Based on an Individual Correction (QTcI) Method (ΔΔQTcI)

The effects of 10 mcg/hr buprenorphine (Day 6) delivered by BTDS alone, or by BTDS dosed with naltrexone, and naltrexone alone on cardiac repolarization, were assessed based on the corrected QT interval since HR inversely affects QT duration. The time-matched analysis was conducted as the primary endpoint as recommended by ICH E14, with the 2-sided 90% confidence interval for each treatment at each time point showing the placebo- and baseline-corrected (ΔΔ) analysis for QTcI. The effect of BTDS 10 on QT intervals was compared with the moxifloxacin-positive control after placebo and baseline correction. (NCT01999114)
Timeframe: Baseline to Day 6

Interventionmilliseconds (msec) (Mean)
BTDS Only (Placebo-corrected ΔΔQTcI)3.36
BTDS With Naltrexone (Placebo-corrected ΔΔQTcI)5.37
Naltrexone Alone (Placebo-corrected ΔΔQTcI)4.34
Moxifloxacin (Placebo-corrected ΔΔQTcI)11.90

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Heart Rate (HR)

Mean change from baseline for the BTDS 80 mcg/hr dose on Day 17, presented as time-averaged mean change from baseline for BTDS only, BTDS with naltrexone, naltrexone alone, moxifloxacin, and placebo. (NCT01999114)
Timeframe: Baseline to Day 17

Interventionbpm (Mean)
BTDS Only1.3
BTDS With Naltrexone-2.4
Naltrexone Alone-0.8
Moxifloxacin2.5
Placebo1.5

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Heart Rate (HR)

Mean change from baseline for the BTDS 40 mcg/hr dose on Day 13, presented as time-averaged mean change from baseline for BTDS only, BTDS with naltrexone, naltrexone alone, moxifloxacin, and placebo. (NCT01999114)
Timeframe: Baseline to Day 13

Interventionbpm (Mean)
BTDS Only1.3
BTDS With Naltrexone-1.9
Naltrexone Alone-0.8
Moxifloxacin2.3
Placebo1.6

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Heart Rate (HR)

Mean change from baseline for the BTDS 10 mcg/hr dose on Day 6, presented as time-averaged mean change from baseline for BTDS only, BTDS with naltrexone, naltrexone alone, moxifloxacin, and placebo. (NCT01999114)
Timeframe: Baseline to Day 6

Interventionbpm (Mean)
BTDS Only-0.1
BTDS With Naltrexone-1.3
Naltrexone Alone-0.5
Moxifloxacin2.0
Placebo1.3

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QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval

Mean change from baseline for the BTDS 80 mcg/hr dose on Day 17, presented as time-averaged mean change from baseline for BTDS only, BTDS with naltrexone, naltrexone alone, moxifloxacin, and placebo. (NCT01999114)
Timeframe: Baseline to Day 17

,,,,
Interventionmsec (Mean)
QTcFQTcBPRQRSQT
BTDS Only9.010.45.40.46.1
BTDS With Naltrexone1.8-0.85.81.57.1
Moxifloxacin6.79.33.80.21.4
Naltrexone Alone-0.8-1.74.31.30.8
Placebo-0.41.23.00.6-3.7

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QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval

Mean change from baseline for the BTDS 40 mcg/hr dose on Day 13, presented as time-averaged mean change from baseline for BTDS only, BTDS with naltrexone, naltrexone alone, moxifloxacin, and placebo. (NCT01999114)
Timeframe: Baseline to Day 13

,,,,
Interventionmsec (Mean)
QTcFQTcBPRQRSQT
BTDS Only5.06.34.50.22.4
BTDS With Naltrexone1.1-1.14.40.95.5
Moxifloxacin5.68.01.3-0.20.9
Naltrexone Alone-1.3-2.23.21.30.4
Placebo-1.60.22.00.3-5.1

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QTcF and QTcB for Historical Purposes, PR Interval, QRS Interval, and Uncorrected QT Interval

Mean change from baseline for the BTDS 10 mcg/hr dose on Day 6, presented as time-averaged mean change from baseline for BTDS only, BTDS with naltrexone, naltrexone alone, moxifloxacin, and placebo. (NCT01999114)
Timeframe: Baseline to Day 6

,,,,
Interventionmsec (Mean)
QTcFQTcBPRQRSQT
BTDS Only-0.1-0.34.70.40.3
BTDS With Naltrexone2.91.52.40.75.6
Moxifloxacin6.99.10.3-0.22.6
Naltrexone Alone1.50.92.10.62.6
Placebo-0.80.50.60.0-3.4

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ECG Morphology

"Morphological analyses were performed with regard to the digital ECG waveform interpretation as defined by a central ECG laboratory's cardiologist blinded to the study treatment. Changes from baseline to each day of treatment were evaluated separately. Any T-U wave complex that suggested an abnormal form compatible with an effect on cardiac repolarization was noted. New ECG morphological onset changes were presented as the percentage of subjects meeting the new criterion (new meant not present on any baseline ECG and became present on at least 1 on-treatment ECG) for the following variables:~Second degree heart block~Third degree heart block~Complete right bundle branch block (RBBB)~Complete left bundle branch block (LBBB)~ST segment changes (elevation and depression separately)~T-wave abnormalities (negative T waves only)~Myocardial infarction (MI) pattern~Any new abnormal U waves" (NCT01999114)
Timeframe: Baseline to Day 6

,,,,
InterventionParticipants (Count of Participants)
New abnormal U wavesNew T wave (negative) invertedNew ST segment depression changesNew ST segment elevation changesNew complete RBBB & LBBBNew MINew 2nd or 3rd degree heart block
BTDS Only0100000
BTDS With Naltrexone0000000
Moxifloxacin0010000
Naltrexone Alone0100000
Placebo0000000

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Change From Baseline in QTcF

Change from baseline in QTcF at 3 hours (msec) (NCT02056392)
Timeframe: 3 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin8.8
Placebo-3.2
Selumetinib-3.3

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Change From Baseline in QTcF

Change from baseline in QTcF at 30 minutes (msec) (NCT02056392)
Timeframe: 30 min

Interventionmsec (Least Squares Mean)
Moxifloxacin2.0
Placebo-4.1
Selumetinib-4.2

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Change From Baseline in QTcF

Change from baseline in QTcF at 4 hours (msec) (NCT02056392)
Timeframe: 4 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin8.6
Placebo-2.2
Selumetinib-3.7

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Change From Baseline in QTcF

Change from baseline in QTcF at 8 hours (msec) (NCT02056392)
Timeframe: 8 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin3.6
Placebo-5.3
Selumetinib-6.5

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Change From Baseline in QTcF

Change from baseline in QTcF at 6 hours (msec) (NCT02056392)
Timeframe: 6 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin4.7
Placebo-4.1
Selumetinib-5.9

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Change From Baseline in QTcF

Change from baseline in QTcF at 1 hour (msec) (NCT02056392)
Timeframe: 1 hour

Interventionmsec (Least Squares Mean)
Moxifloxacin7.9
Placebo-1.4
Selumetinib-1.7

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Change From Baseline in QTcF

Change from baseline in QTcF at 1 hour 30 min (msec) (NCT02056392)
Timeframe: 1 hour 30 min

Interventionmsec (Least Squares Mean)
Moxifloxacin8.1
Placebo-1.8
Selumetinib-0.9

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Change From Baseline in QTcF

Change from baseline in QTcF at 12 hours (msec) (NCT02056392)
Timeframe: 12 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin4.2
Placebo-3.4
Selumetinib-8.2

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Change From Baseline in QTcF

Change from baseline in QTcF at 2 hours (msec) (NCT02056392)
Timeframe: 2 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin7.9
Placebo-2.3
Selumetinib-1.9

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Change From Baseline in QTcF

Change from baseline in QTcF at 24 hours (msec) (NCT02056392)
Timeframe: 24 hours

Interventionmsec (Least Squares Mean)
Moxifloxacin2.4
Placebo-1.6
Selumetinib-4.1

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Sputum Culture Conversion Rates at Week 8 and Month 6 Post Tuberculosis Treatment Initiation

The proportion of patients with negative sputum cultures at the end of the intensive phase (8 weeks) and the proportion of patients with negative sputum cultures at 6 months were compared between the two study arms. All participants with sputum culture results at week 8 and month 6 were included in the analysis. (NCT02114684)
Timeframe: 24 weeks

,
InterventionParticipants (Count of Participants)
culture negative at 8 weeksculture negative at 6 months
Control7392
Moxifloxacin7884

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Number of Participants With Adverse Events and 8-week Culture Conversion Rates Among HIV-infected Patients vs. HIV-uninfected Patients

To compare adverse events and 8-week culture conversion rates among HIV-infected patients vs. HIV-uninfected patients. The proportion of participants with at least one grade 3 or 4 adverse event was measured. (NCT02114684)
Timeframe: up to 2 years for adverse events and 8 weeks for culture conversion rates

,,,
InterventionParticipants (Count of Participants)
participants with grade 3/4 adverse eventsparticipants culture negative at 8 weeks
HIV Negative, Control622
HIV Negative, Moxifloxacin1321
HIV Positive, Control1951
HIV Positive, Moxifloxacin3057

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Time to Culture-conversion of the Moxifloxacin Regimen and the Ethambutol Regimen

To determine the time to culture-conversion of the moxifloxacin regimen and the ethambutol regimen. (NCT02114684)
Timeframe: Up to 2 years

Interventionweeks (Median)
Moxifloxacin6.0
Control7.9

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Proportion of Patients With Unfavourable Outcomes or Tuberculosis Recurrence in the Moxifloxacin and Control Arm.

A patient was defined as having an unfavourable outcome if he/she was not cured at the end of treatment or did not successfully complete treatment. Recurrence after completion of treatment was defined as two positive cultures within a period of four months without an intervening negative culture. (NCT02114684)
Timeframe: up to 2 years

InterventionParticipants (Count of Participants)
Moxifloxacin13
Control6

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Proportion of Patients With Any Grade 3 or 4 Adverse Reactions in the Two Study Arms

To compare the proportion of patients with any Grade 3 or 4 adverse reactions in the two study arms. Outcome measured in terms of number of participants with at least one grade 3 or 4 events, and not in number of events. (NCT02114684)
Timeframe: Up to 2 years

InterventionParticipants (Count of Participants)
Moxifloxacin43
Control25

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Moxifloxacin Fecal Pharmacokinetics: Area Under the Free Moxifloxacin Fecal Concentration-time Curve Over the Period Time From Beginning of Treatment to 37 Days After the Beginning of Treatment (AUC D1-D37)

(NCT02176005)
Timeframe: D1 pre-dose, D2, D3, D4, D5, D6, D7, D8, D9, D12, D16, D23, D30, D37

Interventionμg/g.day (Mean)
Moxifloxacin758.7
Moxifloxacin + DAV1328.74

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Moxifloxacin Plasma Pharmacokinetics: AUC(0-24h) of Moxifloxacin Plasma Concentrations Over Time on D1

(NCT02176005)
Timeframe: D1: at pre-dose; 0h30; 1h; 1h30; 2h; 3h; 4h; 6h; 12h and 24h post-dose

Interventionµg/mL.h (Mean)
Moxifloxacin42.1
Moxifloxacin + DAV13241.9

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Moxifloxacin Plasma Pharmacokinetics: AUC(0-24h) of Moxifloxacin Plasma Concentrations Over Time on D5

(NCT02176005)
Timeframe: D5: at pre-dose; 0h30; 1h; 1h30; 2h; 3h; 4h; 6h; 12h; 24h; 32h; 48h; 56h and 72h post-dose

Interventionµg/mL.h (Mean)
Moxifloxacin57.6
Moxifloxacin + DAV13250.5

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Moxifloxacin Plasma Pharmacokinetics: Cmax of Moxifloxacin in Plasma on D1

(NCT02176005)
Timeframe: D1: at pre-dose; 0h30; 1h; 1h30; 2h; 3h; 4h; 6h; 12h and 24h post-dose

Interventionµg/mL (Mean)
Moxifloxacin4.02
Moxifloxacin + DAV1324.63

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Moxifloxacin Plasma Pharmacokinetics: Cmax of Moxifloxacin in Plasma on D5

(NCT02176005)
Timeframe: D5: at pre-dose; 0h30; 1h; 1h30; 2h; 3h; 4h; 6h; 12h; 24h; 32h; 48h; 56h and 72h post-dose

Interventionµg/mL (Mean)
Moxifloxacin4.89
Moxifloxacin + DAV1324.60

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Moxifloxacin Fecal Pharmacokinetics: Area Under the Free Moxifloxacin Fecal Concentration-time Curve Over the Period Time From Beginning of Treatment to 16 Days After the Beginning of Treatment (AUC D1-D16)

(NCT02176005)
Timeframe: D1 pre-dose, D2, D3, D4, D5, D6, D7, D8, D9, D12, D16

Interventionμg/g.day (Mean)
Moxifloxacin758.4
Moxifloxacin + DAV1328.28

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Rate of Change in Time to Sputum Culture Positivity (TTP) Over 8 Weeks in the Mycobacterial Growth Indicator Tube (MGIT) System

The bactericidal activity (BA) was determined by the rate of change in TTP collected from overnight sputum samples over 8 weeks of treatment in the liquid culture media MGIT system, represented by the model-fitted log(TTP) results as calculated by the regression of the observed log(TTP) results over time. The bactericidal activity of log(TTP) over Day 0 to Day 56 (BATTP[0-56]) was presented and expressed as the daily percentage change in TTP from Day 0 to Day 56. The mean BATTP (0-56) was calculated from Bayesian non-linear mixed effects regression models fitted to log(TTP) collected from sputum samples (observed from Day 0 to Day 56). (NCT02193776)
Timeframe: Day 0 to Day 56 (8 weeks)

Interventionpercentage change in TTP/day (Mean)
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide4.878
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide5.182
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)4.046
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide5.194

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Number of Participants With Treatment Emergent Adverse Events (TEAEs)

A TEAE was defined as any AE which started or worsened on or after first study drug administration up to and including the Day 70 follow-up visit (or up to and including 14 days after last study drug administration for participants not having Day 70 follow-up visit). Drug-related TEAEs were defined as TEAEs for which relationship to study drug was indicated as 'possible', 'probable', 'certain' or missing. TEAEs leading to death were defined as TEAEs resulted 'fatal' outcome. Serious TEAEs were defined as TEAEs for which serious was indicated as 'yes'. TEAEs leading to discontinuation of study drug were defined as TEAEs for which action taken with study drug was indicated as 'study drug stopped'. TEAEs leading to early withdrawal from study were defined as TEAEs resulted study discontinuation. Grade III and IV TEAEs were defined as TEAEs for which severity (DMID grade) was indicated as 'Grade 3 (severe)' and 'Grade 4 (potentially life-threatening)' or missing, respectively. (NCT02193776)
Timeframe: First study drug administration (Day 1) up to and including the Day 70 follow-up visit (or up to and including 14 days after last study drug administration for participants not having the Day 70 follow-up visit) (70 days)

,,,
InterventionParticipants (Count of Participants)
Any TEAEDrug-related TEAETEAE leading to deathAny serious TEAEDrug-related serious TEAETEAE leading to discontinuation of study drugTEAE leading to early withdrawal from studyGrade III TEAEGrade IV TEAE
DS-TB: Bedaquiline (200 mg) + PA-824 + Pyrazinamide452913055177
DS-TB: Bedaquiline (Loading Dose/t.i.w)+ PA-824 + Pyrazinamide503814265198
DS-TB: HRZE (Isoniazid+Rifampicin+Pyrazinamide+Ethambutol)442914122142
MDR-TB: Bedaquiline (200 mg)+Moxifloxacin+PA-824+Pyrazinamide574604222131

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The Primary Outcome Variable Was Probing Depth.

We measured the probing depth at baseline, 1st, 3rd and 6th months. The changes were evaluated among and between groups. (NCT02223702)
Timeframe: 6-months

,
Interventionmm (Mean)
Baseline1st month3rd month6th month
Amoxicillin+Metronidazole4.573.123.113.15
Moxifloxacin4.182.912.793.01

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The Attachment Loss Were Considered as a Secondary Measure.

Attachment loss were recorded at baseline, 1st, 3rd and 6th months as millimeters. The data were compared among and between groups. (NCT02223702)
Timeframe: 6-months

,
Interventionmm (Mean)
Baseline1st month3rd month6th month
Amoxicillin+Metronidazole5.034.374.414.33
Moxifloxacin4.944.143.984.30

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QTcI - QT Interval Individually Corrected for Heart Rate - Day 5

(NCT02283788)
Timeframe: -30 minutes (pre-dose) 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 16, and 23.5 hours post-dose

,,,
Interventionmsec (Mean)
0.5 hr1 hour1.5 hours2 hours3 hours4 hours5 hours6 hours8 hours12 hours16 hours23.5 hours
BIA 2-093 1200 mg-8.05-9.34-8.70-9.48-8.04-7.72-3.54-4.59-2.63-0.01-3.72-3.36
BIA 2-093 2400 mg-6.15-7.34-8.67-8.31-8.50-6.16-1.71-2.64-1.360.03-4.65-0.06
Moxifloxacin 400 mg-2.773.805.306.878.4910.137.075.835.805.855.212.39
Placebo-4.39-4.14-4.22-5.32-3.24-2.10-0.75-3.10-1.77-1.44-1.41-1.71

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Change in Placebo Corrected Change From Baseline QTc Interval on the ECG Measured in Milliseconds When Moxifloxacin is Administered With Diltiazem at the Evening Dose Compared to When Moxifloxacin is Administered Alone at Afternoon Dose on Treatment Day.

Evening dose (moxifloxacin+diltiazem) versus afternoon dose (diltiazem alone). (NCT02308748)
Timeframe: 5 weeks

Interventionms (Mean)
Moxifloxacin Alone29.9
Moxifloxacin + Diltiazem31.3

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Change in Placebo Corrected Change From Baseline QTc and J-Tpeakc Intervals on the ECG Measured in Milliseconds When Dofetilide is Administered With Mexiletine or Lidocaine Compared to When Dofetilide is Administered Alone at Evening Dose on Treatment Day

After 3rd dose of mexiletine or lidocaine (evening dose) on treatment day when combined with dofetilide to evening dose on dofetilide alone day. (NCT02308748)
Timeframe: 5 weeks

,,
Interventionms (Mean)
Placebo corrected change from baseline in QTcPlacebo corrected change from baseline in J-Tpeakc
Dofetilide + Lidocaine183.5
Dofetilide + Mexiletine20.40.8
Dofetilide Alone37.924.0

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Failure or Recurrence (FoR)

The proportion of patients with failure or recurrence (FoR) (NCT02409290)
Timeframe: 132 weeks, control regimen (arm B) using concurrent controls only

InterventionParticipants (Count of Participants)
Regimen B (Control Regimen)14
Regimen D (6-month Regimen)2

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Favourable Outcome After Long-term Follow-up (132 Weeks)

The proportion of patients with a favourable outcome at their last efficacy visit (NCT02409290)
Timeframe: Last efficacy visit, between 96 and 132 weeks

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)17
Regimen B (Control Regimen)126
Regimen C (Oral Regimen)152
Regimen D (6-month Regimen)115

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Proportion of Patients With Acquired Drug Resistance

The proportion of patients with acquired drug resistance (any drug) (NCT02409290)
Timeframe: 132 weeks

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)0
Regimen B (Control Regimen)5
Regimen C (Oral Regimen)5
Regimen D (6-month Regimen)3

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STREAM Stage 2 Primary Outcome Measure (the Proportion of Patients With a Favourable Outcome at Week 76)

The primary efficacy outcome of the STREAM Stage 2 comparison is status at Week 76 i.e. the proportion of patients with a favourable outcome at Week 76 (NCT02409290)
Timeframe: 76 weeks

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)0
Regimen B (Control Regimen)133
Regimen C (Oral Regimen)162
Regimen D (6-month Regimen)122

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Failure or Recurrence (FoR)

probable or definite failure or recurrence (FoR) (NCT02409290)
Timeframe: final efficacy week (between 96 and 132 weeks)

InterventionParticipants (Count of Participants)
Regimen A (Long Regimen)0
Regimen B (Control Regimen)17
Regimen C (Oral Regimen)4
Regimen D (6-month Regimen)0

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TB Disease-free Survival at 12M After Study Treatment Assignment Among Participants in Control Regimen, Regimen1 (2HRZE/4HR) to Experimental Regimens, Regimen3 (2HPZM/2HPM) and Regimen2 (2HPZ/2HP) (Assessable Population)

"To evaluate the efficacy of a rifapentine-containing regimen to determine whether the single substitution of rifapentine for rifampin makes it possible to reduce to seventeen weeks the duration of treatment for drug-susceptible pulmonary tuberculosis~To evaluate the efficacy of a rifapentine-containing regimen that in addition substitutes moxifloxacin for ethambutol and continues moxifloxacin during the continuation phase, to determine whether it is possible to reduce to seventeen weeks the duration of treatment for drug-susceptible pulmonary tuberculosis A primary outcome status of favorable, unfavorable, or not assessable was assigned. For detailed definitions of outcomes please refer to: Dorman SE, at al. N Engl J Med. 2021 May 6;384(18):1705-1718." (NCT02410772)
Timeframe: Twelve months after treatment assignment

,,
InterventionParticipants (Count of Participants)
FavorableUnfavorable
Regimen 1 (2HRZE/4HR)65670
Regimen 2 (2HPZ/2HP)645107
Regimen 3 (2HPMZ/2HPM)66888

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Change From Baseline (Preoperative Exam) in Pachymetry (Corneal Thickness)

"Cornea is the clear part of the front of the eye. Normal corneal thickness is in average 0.540 mm. The corneal thickness is measured with a handheld device called pachymeter.~An increase in corneal thickness may indicate corneal edema (swelling of the cornea) that could be seen after ocular surgery." (NCT02515045)
Timeframe: Month 1

InterventionMicrons (Mean)
TriMoxiVanc14.44
TriMoxiVanc + Ilevro5.94
Control4.47

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Change From Baseline (Preoperative Exam) in Macular Thickness

Macula is the area in the retina that is responsible for the best central vision. Changes in its thickness may occur after cataract surgery due to the normal inflammatory process that occurs postoperatively but it returns to preoperative values unless there is an underlying disease. (NCT02515045)
Timeframe: Month 1.

InterventionMicrons (Mean)
TriMoxiVanc12.34
TriMoxiVanc + Ilevro10.96
Control9.84

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Change From Baseline (Preoperative Exam) in Intraocular Pressure (IOP)

Intraocular pressure refers to the pressure inside the eye. It is measured in mmHg using a device called a tonometer. The mean IOP is 15.5 mmHg. Raised IOP after cataract surgery is common and in most cases it is transient and benign. (NCT02515045)
Timeframe: Month 1.

InterventionmmHg (Mean)
TriMoxiVanc-0.5
TriMoxiVanc + Ilevro-1.03
Control-1.1

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Number of Participants With Early Clinical Response

Early clinical response is defined as clinical success, categorized by survival with improvement of at least 1 level compared to Baseline in at least 2 CABP symptoms (cough, sputum production, pleuritic chest pain, and dyspnea) with no worsening in the other CABP symptoms. Response was determined programmatically using the investigator's assessment of the CABP symptoms. The severity of the participant's CABP symptoms was evaluated on a 4-point scale (absent, mild, moderate, or severe) based upon the CABP Subject Symptom Severity Guidance Framework for Investigator Assessment. An indeterminate response is defined as one that could not be adequately inferred because the participant was not assessed because they withdrew consent, were lost to follow-up, or other specified reason. Clinical failure is defined as no improvement by at least 1 level in CABP symptoms, worsening of any CABP symptom, alternative antibacterial treatment for CABP, discontinuation due to adverse event, or death. (NCT02531438)
Timeframe: Screening; 72 to 120 hours after the first dose of test article

,
InterventionParticipants (Count of Participants)
Clinical successClinical failureIndeterminate
Moxifloxacin3214720
Omadacycline3134924

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Number of Participants With the Indicated Investigator Assessment of Clinical Response in the ITT Population at the Post Therapy Evaluation (PTE) Visit

At the PTE Visit the investigator indicated one of the following outcomes relating to the primary infection under study: Clinical Success: survival after completion of a test article regimen without receiving any systemic antibacterial therapy other than test article, resolution of signs/symptoms of the infection present at Screening with no new symptoms/complications attributable to CABP and no need for further antibacterial therapy. Clinical Failure: alternative antibacterial treatment for CABP was required prior to the PTE Visit related to either (a) progression/development of new CABP symptoms or (b) development of infectious complications of CABP. Other reasons for clinical failure: participant received antibiotics that may have been effective for the infection under study for a different infection from the one under study; death prior to the PTE Visit. Indeterminate: the clinical response to test article could not be adequately inferred. (NCT02531438)
Timeframe: Screening; 5 to 10 days after the last day of therapy

,
InterventionParticipants (Count of Participants)
Clinical successClinical failureIndeterminate
Moxifloxacin3304216
Omadacycline3383216

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Number of Participants With the Indicated Investigator Assessment of Clinical Response in the Clinically Evaluable-Post Therapy Evaluation (CT-PTE) Population

At the PTE Visit the investigator indicated one of the following outcomes relating to the primary infection under study: Clinical Success: survival after completion of a test article regimen without receiving any systemic antibacterial therapy other than test article, resolution of signs/symptoms of the infection present at Screening with no new symptoms/complications attributable to CABP and no need for further antibacterial therapy. Clinical Failure: alternative antibacterial treatment for CABP was required prior to the PTE Visit related to either (a) progression/development of new CABP symptoms or (b) development of infectious complications of CABP. Other reasons for clinical failure: participant received antibiotics that may have been effective for the infection under study for a different infection from the one under study; death prior to the PTE Visit. (NCT02531438)
Timeframe: Screening; 5 to 10 days after the last day of therapy

,
InterventionParticipants (Count of Participants)
Clinical successClinical failure
Moxifloxacin31233
Omadacycline31624

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Early Clinical Response (ECR)

ECR was defined as survival with improvement in at least 2 signs and symptoms of CABP (relative to baseline), no worsening of any CABP sign or symptom, and no use of concomitant antibiotics (other than adjunctive linezolid, as allowed by the study protocol) for the treatment of CABP through the ECR assessment. (NCT02559310)
Timeframe: ECR was assessed 96 +/- 24 hours after the first dose of study drug.

,
InterventionParticipants (Count of Participants)
ResponderNon-ResponderIndeterminate
Lefamulin241296
Moxifloxacin ± Linezolid248216

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Maximal Mean ΔΔQTcF

"Maximal mean placebo-corrected change from baseline of QTcF (QT interval corrected for heart rate using the Fridericia formula) for single 5 mg and 40 mg iv doses of APD421. At each time point (2 mins, 8 mins, etc) the QTcF is compared to the pre-dosing baseline value, in order to calculate the change in QTcF (ΔQTcF). The value of ΔQTcF at each time point is then compared against the same time point for a placebo infusion, and the difference is calculated (ΔΔQTcF)." (NCT02661594)
Timeframe: 24 hours

Interventionmilliseconds (Mean)
5 mg IV APD4215.0
40 mg IV APD42123.4
Placebo0.8
Oral Moxifloxacin12.3

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Microbiologic Response

Microbiological response for subjects in the MITT set will be based on results of the baseline and follow-up cultures and susceptibility testing or serology. (NCT02679573)
Timeframe: 5 to 10 days after the last dose of study drug

InterventionParticipants (Count of Participants)
Delafloxacin231
Moxifloxacin/Linezolid235

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Early Clinical Response Plus Improvement in Vital Signs and no Worsening of the 4 Symptoms

Early clinical response with the addition of improvement in vital signs and no worsening of the following 4 symptoms: chest pain, cough, productive sputum, and difficulty breathing in the ITT population. Symptom severity evaluated by the investigator on a 4-point scale: Absent (0), Mild (1), Moderate (2), Severe (3). Improvement defined as at least a 1-point decrease from baseline. Improvement in vital signs defined as a return to normal of any abnormal vital signs at baseline, and no worsening (ie, be abnormal) of any vital sign that was normal at baseline. (NCT02679573)
Timeframe: 96 (+/- 24) hours after the first dose of study drug

InterventionParticipants (Count of Participants)
Delafloxacin227
Moxifloxacin/Linezolid184

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All-cause Mortality

Time to all-cause Mortality was assessed on Day 28. (NCT02679573)
Timeframe: Day 28 (+/- 2 days)

InterventionParticipants (Count of Participants)
Delafloxacin8
Moxifloxacin/Linezolid6

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Early Clinical Response

Early clinical response defined as improvement in at least 2 of the following symptoms (as assessed by the investigator): chest pain, frequency or severity of cough, amount and quality of productive sputum, and difficulty breathing, and no worsening of the other symptoms in the ITT population. Symptom severity evaluated by the investigator on a 4-point scale: Absent (0), Mild (1), Moderate (2), Severe (3). Improvement defined as at least a 1-point decrease from baseline. (NCT02679573)
Timeframe: 96 (+/- 24) hours after the first dose of study drug

InterventionParticipants (Count of Participants)
Delafloxacin383
Moxifloxacin/Linezolid381

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Number of Participants With Laboratory Test Abnormalities

Hemoglobin(Hgb), hematocrit, red blood cell(RBC)<0.8*lower limit of normal(LLN), mean corpuscular(MC) Hgb, MC volume <0.9*LLN, >1.1*upper limit of normal(ULN), platelet<0.5*LLN,>1.75*ULN, lymphocyte, neutrophil<0.8*LLN, >1.2*ULN, basophil, eosinophil, monocyte>1.2*ULN, white blood cell(WBC)<0.6*LLN,>1.5*ULN, reticulocytes<0.5*LLN,>1.5*ULN; bilirubin>1.5*ULN, aspartate aminotransferase(AT), alanine AT, alkaline phosphatase>3.0*ULN, protein, albumin<0.8*LLN,>1.2*ULN; blood urea nitrogen, creatinine>1.3*ULN, uric acid>1.2*ULN; sodium<0.95*LLN,>1.05*ULN, potassium, chloride, calcium, bicarbonate<0.9*LLN,>1.1*ULN; glucose<0.6*LLN, >1.5*ULN, HbA1c>1.3*ULN, creatinine kinase>2*ULN; urine-specific gravity<1.003,>1.030, pH<4.5,>8, WBC, RBC>=20, bacteria>20, urobilinogen, glucose, ketone, protein, Hgb, nitrite, leukocyte esterase, bilirubin>=1; thyroid stimulating hormone<0.8*LLN,>1.2*ULN; cholesterol, triglycerides>1.3*ULN, high density lipoprotein cholesterol(DL-C) <0.8*LLN, low DL-C>1.2*ULN. (NCT02785770)
Timeframe: Baseline (Pre-dose) up to 24 hours post-dose

InterventionParticipants (Count of Participants)
PF-04447943 25 mg17
PF-04447943 100 mg12
Moxifloxacin 400 mg12
Placebo18

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Maximum Plasma Concentration (Cmax) of PF-04447943

(NCT02785770)
Timeframe: Pre-dose (0 hour), 0.5, 1, 2, 3, 4, 8, 12 and 24 hours post-dose

InterventionNanogram per milliliter (Geometric Mean)
PF-04447943 25 mg225.8
PF-04447943 100 mg947.3

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Area Under the Plasma Concentration-Time Curve From Time Zero to Time of Last Measurable Concentration (AUClast) of PF-04447943

Area under the plasma concentration-time from time zero to time of last measurable concentration. Observed using the linear/log trapezoidal method. (NCT02785770)
Timeframe: Pre-dose (0 hour), 0.5, 1, 2, 3, 4, 8, 12 and 24 hours post-dose

InterventionNanogram*hour per milliliter (Geometric Mean)
PF-04447943 25 mg1454
PF-04447943 100 mg6277

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Time-Matched Mean Difference in QRS Interval for PF-04447943 and Placebo

Least square mean of QRS interval measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 0.5, 1, 2, 3, 4, 8, 12 and 24 hours post-dose

,,
InterventionMsec (Least Squares Mean)
0.5 Hour1 Hour2 Hours3 Hours4 Hours8 Hours12 Hours24 Hours
PF-04447943 100 mg89.2889.1889.1489.3188.9588.2289.0988.61
PF-04447943 25 mg90.7690.5190.8989.3689.8489.1489.6189.31
Placebo89.9690.3789.8889.3991.0288.9489.5889.23

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Time-Matched Mean Difference in Heart Rate for PF-04447943 and Placebo

Least square mean of heart rate measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 0.5, 1 , 2, 3, 4, 8, 12 and 24 hours post-dose

,,
InterventionBeats per minute (bpm) (Least Squares Mean)
0.5 Hour1 Hour2 Hours3 Hours4 Hours8 Hours12 Hours24 Hours
PF-04447943 100 mg63.9164.4361.7361.2160.7463.4066.6060.23
PF-04447943 25 mg60.7260.9858.5558.3758.7361.1366.2259.32
Placebo59.4458.6057.6458.6858.2461.9566.9562.35

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Time-Matched Mean Difference in PR Interval for PF-04447943 and Placebo

Least square mean of PR interval measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 0.5, 1, 2, 3, 4, 8, 12 and 24 hours post-dose

,,
InterventionMsec (Least Squares Mean)
0.5 Hour1 Hour2 Hours3 Hours4 Hours8 Hours12 Hours24 Hours
PF-04447943 100 mg170.52169.28169.72169.34169.22165.25165.48169.50
PF-04447943 25 mg171.59171.15170.43169.86170.59164.86166.08172.09
Placebo172.24172.09171.60170.85171.16167.31166.49171.57

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for Moxifloxacin and Placebo

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across Moxifloxacin and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 0.5, 1 , 2, 3, 4, 8, 12 and 24 hours post-dose

,
InterventionMsec (Least Squares Mean)
0.5 Hour1 Hour2 Hours3 Hours4 Hours8 Hours12 Hours24 Hours
Moxifloxacin 400 mg405.34411.98413.85413.03413.69406.72407.52406.81
Placebo404.38404.09402.52404.43404.73398.66401.99403.06

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Number of Participants With Vital Sign Abnormalities

Criteria for vital sign abnormalities: supine and standing pulse rate <40 bpm or greater than (>) 120 bpm, supine and standing systolic blood pressure (SBP) <90 millimeter of mercury (mmHg), supine and standing diastolic blood pressure (DBP) <50 mmHg, maximum (max.) increase from baseline (IFB) and decrease from baseline (DFB) in supine and standing SBP of >=30 mmHg, maximum IFB and DFB in supine and Standing DBP of >=20 mmHg. (NCT02785770)
Timeframe: Baseline (Pre-dose) up to 24 hours post-dose

,,,
InterventionParticipants (Count of Participants)
Supine SBP: <90 mmHgStanding SBP: <90 mmHgSupine DBP: <50 mmHgStanding DBP: <50 mmHgSupine Pulse Rate: <40 bpmSupine Pulse Rate: >120 bpmStanding Pulse Rate: <40 bpmStanding Pulse Rate: >120 bpmMax. IFB in Supine SBP: >=30mmHgMax. IFB in StandingSBP:>=30 mmHgMax. IFB in Supine DBP: >=20 mmHgMax. IFB in StandingDBP:>=20 mmHgMax. DFB in Supine SBP:>=30 mmHgMax. DFB in StandingSBP:>=30 mmHgMax. DFB in Supine DBP:>=20 mmHgMax. DFB in StandingDBP:>=20 mmHg
Moxifloxacin 400 mg0211100000030101
PF-04447943 100 mg0000000100020104
PF-04447943 25 mg0000000001020202
Placebo0000000121110300

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

An AE was any untoward medical occurrence in a participant who received study drug without regard to possibility of causal relationship. An SAE was an AE resulting in any of the following outcomes or deemed significant for any other reason: death; initial or prolonged inpatient hospitalization; life-threatening experience (immediate risk of dying); persistent or significant disability/incapacity; congenital anomaly. A treatment emergent AE was defined as an event that emerged during the treatment period that was absent before treatment, or worsened during the treatment period relative to the pretreatment state. (NCT02785770)
Timeframe: Baseline (Pre-dose) up to 28 days after last dose of study drug (56 days)

,,,
InterventionParticipants (Count of Participants)
AEsSAEs
Moxifloxacin 400 mg80
PF-04447943 100 mg90
PF-04447943 25 mg110
Placebo80

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Number of Participants With Electrocardiogram (ECG) Abnormalities

Criteria for ECG abnormalities: maximum QTc corrected for heart rate using Bazett's formula (QTcB) and QTcF interval (450 to less than [<] 480 msec, 480 to <500 msec, greater than or equal to [>=] 500 msec; increase from baseline [IFB] >=30 msec and <60 msec, IFB >=60 msec). Baseline was defined as the average of the means obtained from the 3 sets of triplicate measurements taken at -1, -0.5 and 0 hours pre-dose on Day 1 within each intervention period. (NCT02785770)
Timeframe: Baseline up to 24 hours post-dose

,,,
InterventionParticipants (Count of Participants)
QTcB Interval 450 to <480 msecQTcB Interval 480 to <500 msecQTcB Interval >=500 msecQTcB IFB (>= 30 to <60) msecQTcB IFB (>=60) msecQTcF Interval 450 to <480 msecQTcF Interval 480 to <500 msecQTcF Interval >=500 msecQTcF IFB (>=30 to <60) msecQTcF IFB (>=60) msec
Moxifloxacin 400 mg1002010000
PF-04447943 100 mg3001010000
PF-04447943 25 mg1000000000
Placebo0001000000

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 8 Hours Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 8 hours post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg397.31
PF-04447943 100 mg398.55
Placebo398.66

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 3 Hours Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 3 hours post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg403.95
PF-04447943 100 mg406.69
Placebo404.43

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 24 Hours Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 24 hours post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg401.72
PF-04447943 100 mg400.28
Placebo403.06

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 2 Hours Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 2 hours post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg403.76
PF-04447943 100 mg406.78
Placebo402.52

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 4 Hours Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 4 hours post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg402.76
PF-04447943 100 mg405.94
Placebo404.73

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 1 Hour Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 1 hour post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg404.23
PF-04447943 100 mg409.14
Placebo404.09

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 0.5 Hour Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 0.5 hour post-dose

InterventionMillisecond (Msec) (Least Squares Mean)
PF-04447943 25 mg404.09
PF-04447943 100 mg408.92
Placebo404.38

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Time of Observed Maximum Plasma Concentration (Tmax) of PF-04447943

(NCT02785770)
Timeframe: Pre-dose (0 hour), 0.5, 1, 2, 3, 4, 8, 12 and 24 hours post-dose

InterventionHours (Median)
PF-04447943 25 mg1.0
PF-04447943 100 mg1.02

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Number of Participants With Physical Examination Abnormalities

Full physical examination included head, ears, eyes, nose, mouth, skin, heart and lung examinations, lymph nodes, gastrointestinal, musculoskeletal, and neurological systems. Physical examination abnormalities were judged by the investigator. (NCT02785770)
Timeframe: Baseline (Pre-dose)

InterventionParticipants (Count of Participants)
PF-04447943 25 mg1
PF-04447943 100 mg1
Moxifloxacin 400 mg1
Placebo2

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Time-Matched Mean Difference in Corrected QT Interval Using Fridericia's Correction Method (QTcF) for PF-04447943 and Placebo at 12 Hours Post-Dose

Least square mean of QTcF measure for each reporting arm has been reported in summary or descriptive statistics. Least square mean difference across PF-04447943 25 mg and placebo; PF-04447943 100 mg and placebo is reported in statistical analysis. (NCT02785770)
Timeframe: 12 hours post-dose

InterventionMsec (Least Squares Mean)
PF-04447943 25 mg399.83
PF-04447943 100 mg399.38
Placebo401.99

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Secondary Treatment Failure Rate

Secondary treatment failure was defined as treatment failure despite adjustment of antibiotics or changing to second line antibiotics for 3 to 5 days in patients with primary treatment failure (NCT02787057)
Timeframe: after 6 to 8 days of treatment

InterventionParticipants (Count of Participants)
Control Group5
Study Group4

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Primary Treatment Failure Rate

Primary treatment failure was defined as the presence of fever, abdominal pain, and turbid peritoneal dialysate, and if the total peritoneal WBC counts is >50% of the pretreatment values after 3 days of treatment by the assigned antibiotics (NCT02787057)
Timeframe: after 3 days of treatment by the assigned antibiotics

InterventionParticipants (Count of Participants)
Control Group8
Study Group13

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Primary Response Rate

Primary response was defined as resolution of peritonitis (normalization of body temperature, resolution of abdominal pain, clearing of dialysate, and PD effluent neutrophil count less than 100 cells/mL and proportion of polynuclear cell less than 50%) on day 10 by using antibiotics alone (NCT02787057)
Timeframe: on day 10 by using antibiotics alone

InterventionParticipants (Count of Participants)
Control Group32
Study Group27

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Complete Cure Rate

complete cure was defined as complete resolution of peritonitis (normalization of body temperature, resolution of abdominal pain, clearing of dialysate, and PD effluent neutrophil count less than 100 cells/mL and proportion of polynuclear cell less than 50%) by using antibiotics alone without relapse within 4 weeks of completion of therapy (NCT02787057)
Timeframe: within 4 weeks of completion of therapy

InterventionParticipants (Count of Participants)
Control Group32
Study Group31

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Number of Participants With at Least One Complications From Treatment

Comparison of the number of participants with at least one surgical complication and antibiotic complications. (NCT02800785)
Timeframe: 90 days

InterventionParticipants (Count of Participants)
Antibiotics Therapy Arm37
Appendectomy Arm21

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Number of Clinic Visits or Emergency Room Visits

Total number of participants with any visit to emergency department or urgent care clinic after index treatment within 90 days (NCT02800785)
Timeframe: 90 days post randomization

Interventionvisits (Number)
Antibiotics Therapy Arm55
Appendectomy Arm26

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Total Number of Patients Who Had Resolution of Appendicitis Symptoms at 30 Days

Total Number of Patients who had resolution of appendicitis symptoms at 30 Days. This was measured as absence of fever and abdominal pain and tenderness. (NCT02800785)
Timeframe: at 30 days

InterventionParticipants (Count of Participants)
Antibiotics Therapy Arm462
Appendectomy Arm466

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Eventual Appendectomy Incidence Proportion

incidence proportion of appendectomy within 90 days post randomization among those randomized to antibiotics (NCT02800785)
Timeframe: 90 days post randomization

Interventionincidence proportion (Number)
Antibiotics Therapy Arm0.29

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Rates of Participants With Appendiceal Cancer

Rates of appendiceal cancer among participants will be calculated among the antibiotics and appendectomy arms. (NCT02800785)
Timeframe: Through study completion, up to 2 years

InterventionParticipants (Count of Participants)
Antibiotics Therapy Arm4
Appendectomy Arm6

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Rate of Participants With Perforated Appendicitis

Rates of patients who had perforated appendicitis will be calculated for each arm among those received an appendectomy. (NCT02800785)
Timeframe: 90 days post enrollment

InterventionParticipants (Count of Participants)
Antibiotics Therapy Arm59
Appendectomy Arm99

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Patient-reported Quality of Life as Measured by EuroQol (EQ-5D)

The primary evaluation of patient-reported quality of life, as measured by the EuroQuol-5D at four-weeks, will be conducted using an intention-to-treat (ITT) analysis, where patients' data are analyzed according to the patients' randomized treatment assignment. EQ5D assesses health status in terms of five dimensions of health. The maximum score of 1 indicates the best health state, the minimum score is 0 (as score as bad as being dead). (NCT02800785)
Timeframe: Four-weeks after randomization

Interventionscore on a scale (Mean)
Antibiotics Therapy Arm0.92
Appendectomy Arm0.91

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Days in Hospital After Index Treatment Within 90 Days

Mean number of days in the hospital per participant calculated at 90 days post randomization. (Number of days/Number of Participants in Therapy Arm who responded to the 90 day survey question) (NCT02800785)
Timeframe: 90 days post randomization

InterventionDays per participant (rate) (Mean)
Antibiotics Therapy Arm0.68
Appendectomy Arm0.15

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Clinical Response in the Micro-ITT Population

Clinical response (response, non-response, or indeterminate) at Day 4 was also tested in the micro-ITT population as a secondary efficacy endpoint. Clinical response was determined programmatically using the investigator's assessment of CABP symptoms entered into the eCRF. The severity of the subject CABP symptoms of dyspnea (shortness of breath), cough, production of purulent sputum, and pleuritic chest pain were evaluated on a 4-point scale (absent, mild, moderate, or severe) based upon the CABP Symptom Severity Guidance (NCT02903836)
Timeframe: Day 4 from start of drug administration

InterventionParticipants (Count of Participants)
Nafithromycin 800 mg 3 Days21
Nafithromycin 800 mg 5 Days26
Moxifloxacin 400 mg18

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Clinical Response in the ITT Population

The primary efficacy endpoint was clinical response (response, non-response, or indeterminate) at Day 4, tested in the ITT population. Clinical response was determined programmatically using the investigator's assessment of CABP symptoms entered into the eCRF. The severity of the subject CABP symptoms of dyspnea (shortness of breath), cough, production of purulent sputum, and pleuritic chest pain were evaluated on a 4-point scale (absent, mild, moderate, or severe) based upon the CABP Symptom Severity Guidance (NCT02903836)
Timeframe: Day 4 from start of drug administration

InterventionParticipants (Count of Participants)
Nafithromycin 800 mg 3 Days68
Nafithromycin 800 mg 5 Days65
Moxifloxacin 400 mg67

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Change From Baseline Bacterial Culture

"Efficacy will be determined comparing the cultures of the lower conjunctival pouch, of the baseline (day 1) against final visit (day 8), quantifying and identifying the colony forming units (CFU) by genus and species.~The evaluated variable is discrete quantitative type and the scale of measurement used will be CFU x mL considering the eradication, reduction or proliferation of the bacterial agent. It will be determined as effective if there is a reduction in number of bacterial flora in at least 95% of the evaluated subjects." (NCT02980523)
Timeframe: up to one week

,,,,
Interventioncultures (Number)
basal cultures positivesfinal cultures negatives
Gatifloxacin (Zymar®)1715
Moxifloxacin (Vigamox®)2928
PRO-157 BID (2 Times Per Day)3017
PRO-157 QID (4 Times Per Day)2616
PRO-157 TID (3 Times Per Day)1614

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Number of Cases of Conjunctival Hyperemia

Conjunctival hyperemia: qualitative ordinal variable. The conjunctival hyperemia was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group. (NCT02980523)
Timeframe: up to one week

Interventionhyperemia cases reported (Number)
PRO-157 BID (2 Times Per Day)17
PRO-157 TID (3 Times Per Day)1
PRO-157 QID (4 Times Per Day)5
Moxifloxacin (Vigamox®)7
Gatifloxacin (Zymar®)8

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Frequency of Corneal Epithelial Defects

"Corneal epithelial defects: qualitative ordinal variable, measurement scale present or absent.~The corneal epithelial defects was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group." (NCT02980523)
Timeframe: Up to one week

InterventionCorneal defects cases reported (Number)
PRO-157 BID (2 Times Per Day)9
PRO-157 TID (3 Times Per Day)4
PRO-157 QID (4 Times Per Day)6
Moxifloxacin (Vigamox®)5
Gatifloxacin (Zymar®)5

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Eyelid Edema Frequency

"Eyelid edema: qualitative ordinal variable, measurement scale absent or present.Between baseline (day 0) versus final visit (day 7).~The eyelid edema was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group." (NCT02980523)
Timeframe: Up to one week

Interventioneyelid edema cases reported (Number)
PRO-157 BID (2 Times Per Day)6
PRO-157 TID (3 Times Per Day)0
PRO-157 QID (4 Times Per Day)4
Moxifloxacin (Vigamox®)4
Gatifloxacin (Zymar®)6

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Chemosis Frequency

Chemosis: qualitative ordinal variable, measurement scale absent or present. The chemosis was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group. (NCT02980523)
Timeframe: up to one week

Interventionchemosis cases reported (Number)
PRO-157 BID (2 Times Per Day)0
PRO-157 TID (3 Times Per Day)0
PRO-157 QID (4 Times Per Day)0
Moxifloxacin (Vigamox®)6
Gatifloxacin (Zymar®)2

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Cases Frequency of Ocular Secretion

Secretion ocular: qualitative ordinal variable. The secretion was evaluated by subject of study as present / absent, taking into consideration that each study subject represents two probable cases, one for each eye. On this premise, the statistical analysis of the number of cases reported in the final visit was made by study group. (NCT02980523)
Timeframe: Up to one week.

Interventionsecretion cases reported (Number)
PRO-157 BID (2 Times Per Day)0
PRO-157 TID (3 Times Per Day)3
PRO-157 QID (4 Times Per Day)0
Moxifloxacin (Vigamox®)7
Gatifloxacin (Zymar®)2

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Adverse Events

Number of adverse events: dependent variable, discrete quantitative, the number of adverse events per group will be compared at the end of the study and it will be considered safe if there is not greater increase of 5% of serious adverse events. (NCT02980523)
Timeframe: during the intervention period for 7 days, and 15 days after the final visit

Interventionevents (Number)
PRO-157 BID (2 Times Per Day)7
PRO-157 TID (3 Times Per Day)5
PRO-157 QID (4 Times Per Day)7
Moxifloxacin (Vigamox®)4
Gatifloxacin (Zymar®)7

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Number of Patients With Treatment-Emergent Adverse Events (TEAEs)

AE definition: any untoward medical occurrence in a clinical trial participant. Serious AE definition: an AE that is fatal, life threatening, requires in-patient hospitalization or prolongation of existing hospitalization, results in permanent (persistent) disability/incapacity, is a congenital anomaly/birth defect or is an important medical event. Severity of AEs were classified as: mild: causes no limitation of usual activities, moderate: causes some limitation of usual activities; or severe: prevents or severely limits usual activities. The investigator assessed AEs for relatedness to study medication. TEAEs were defined as all AEs that started on or after the first dose of study medication (APL-130277, moxifloxacin or placebo). Results are presented for TEAEs during the Randomized Crossover Assessment Phase. (NCT03187301)
Timeframe: From first dose of study medication up to last study visit for Randomized Crossover Assessment Phase, approximately up to 2 weeks

,,
Interventionparticipants (Number)
Any TEAEDrug-related TEAESevere TEAESerious TEAETEAE leading to death
APL-130277 (Cross-over)1312100
Moxifloxacin (Crossover)40000
Placebo (Crossover)62000

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ECG Assessments: Mean Change From Baseline to Post-Baseline Value for Uncorrected QT Interval During Randomized Crossover Assessment Phase

Uncorrected QT interval was defined as time between start of Q wave and end of T wave. QT interval was determined during continuous 12-lead ECG (Holter) monitoring at each of the 3 treatment period dosing visits at pre-specified timepoints post-dose. Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (pre-dose P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 15, 30, 45 and 60 mins and 2, 3 and 4 hours post-dose at each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. Results are presented for the mean change from baseline at each pre-specified post-dose timepoint. (NCT03187301)
Timeframe: Baseline and at 15, 30, 45, 60 minutes and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase.

,,
Interventionmsec (Least Squares Mean)
15 mins post-dose30 mins post-dose45 mins post-dose60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
APL-130277 (Cross-over)-3.9-2.20.38.3-2.6-12.0-16.4
Moxifloxacin (Crossover)-2.7-0.7-2.23.56.23.02.8
Placebo (Cross-over)-7.1-6.1-4.2-3.5-7.6-8.9-10.1

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ECG Assessments: Mean Change From Baseline to Post-Baseline Value for QRS Interval During Randomized Crossover Assessment Phase

QRS interval was defined as the time of QRS complex (Q, R, and S waves). QRS interval was determined during continuous 12-lead ECG (Holter) monitoring at each of the 3 treatment period dosing visits at pre-specified timepoints post-dose. Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (pre-dose P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 15, 30, 45 and 60 mins and 2, 3 and 4 hours post-dose at each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. Results are presented for the mean change from baseline at each pre-specified post-dose timepoint. (NCT03187301)
Timeframe: Baseline and at 15, 30, 45, 60 minutes and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase.

,,
Interventionmsec (Least Squares Mean)
15 mins post-dose30 mins post-dose45 mins post-dose60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
APL-130277 (Cross-over)-0.7-0.4-1.2-0.81.1-0.20.5
Moxifloxacin (Crossover)-0.7-0.1-0.9-0.4-1.1-1.00.4
Placebo (Cross-over)-1.2-0.9-0.1-1.4-1.3-0.9-0.6

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Tmax of Apomorphine and Apomorphine Sulfate (Metabolite) Following the Administration of APL-130277

The time of maximum observed plasma concentration (Tmax) for apomorphine and apomorphine sulfate (metabolite) was determined in patients treated with APL-130277. PK parameters were derived using a non-compartmental analysis method. Bioanalysis of apomorphine and apomorphine-sulfate plasma concentration were measured using a validated LC/MS-MS method. The calibration range was 0.0200 ng/mL to 20.0 ng/mL apomorphine and 10.0 to 1000 ng/mL apomorphine sulfate. PK assessments were performed at each period of the Randomized Crossover Assessment Phase (at P1V1, P2V2 and P3V3) and results are presented for each of the APL-130277 doses administered (as determined for each patient during the Dose Titration Phase). (NCT03187301)
Timeframe: Blood samples for PK assessments were taken prior to dosing and at 0.5, 0.75, 1, 2, and 4 hours post-dose.

,,,,,
Interventionhours (Median)
ApomorphineApomorphne sulfate
10 mg APL-130277 PK Subset0.752.00
15 mg APL-130277 PK Subset0.751.52
20 mg APL-130277 PK Subset1.002.00
25 mg APL-130277 PK Subset1.501.50
35 mg APL-130277 PK Subset0.582.13
50 mg APL-130277 PK Subset0.780.52

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ECG Assessments: Mean Change From Baseline to Post-Baseline Value for QTcB Interval During Randomized Crossover Assessment Phase

QTcB was defined as QT interval corrected with Bazett's method. QT was defined as time between start of Q wave and end of T wave. QTcB was determined during continuous 12-lead ECG (Holter) monitoring at each of the 3 treatment period dosing visits at pre-specified timepoints post-dose. Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (pre-dose P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 15, 30, 45 and 60 mins and 2, 3 and 4 hours post-dose at each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. Results are presented for the mean change from baseline at each pre-specified post-dose timepoint. (NCT03187301)
Timeframe: Baseline and at 15, 30, 45, 60 minutes and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase.

,,
Interventionmsec (Least Squares Mean)
15 mins post-dose30 mins post-dose45 mins post-dose60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
APL-130277 (Cross-over)2.71.90.1-0.14.77.28.1
Moxifloxacin (Crossover)-2.51.47.88.411.112.812.1
Placebo (Crossover)-1.7-0.7-3.2-3.3-0.42.75.5

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Median Duration of 'ON' During the Dose Titration Phase

"The duration of 'ON' was calculated as minutes from the time when the patient turned fully 'ON' until the time when the patient turned 'OFF', as assessed by the Investigator. If the patient did not turn fully 'ON' within 90 minutes the duration of 'ON' was defined as zero minutes. If the patient turned fully 'ON' and did not turn 'OFF' by 90 minutes, the data was censored at 90 minutes minus the time when the patient turned fully 'ON'.~The median duration of a full 'ON' response during the Dose Titration Phase following the highest tolerated APL-130277 dose level (indicated as Day 2) and the lowest APL-130277 dose resulting in a full 'ON' (indicated as Day 1) are presented. The median duration of 'ON' on Day 1 and Day 2 was calculated using the Kaplan-Meier method." (NCT03187301)
Timeframe: Time of dosing up to 90 minutes post-dose during the Dose Titration Phase.

Interventionminutess (Median)
Day 1Day 2
APL-130277 (Titration)NANA

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Mean Change From Pre-Dose to Post-Baseline Value in the Movement Disorders Society Unified Parkinson's Disease Rating Scale Part III Motor Examination (MDS-UPDRS Part III) Score During the Dose Titration Phase

"The Motor Function section (Part III) of the MDS-UPDRS was administered by the Investigator, and included 33 scores based on 18-items, each anchored with 5 responses: 0 = normal, 1 = slight, 2 = mild, 3 = moderate, and 4 = severe. The scale range was from 0 to 132, with a lower score indicating better motor function and a higher score indicating more severe motor symptoms.~The least squares mean change in the MDS-UPDRS Part III score from pre-dose to 30, 60 and 90 minutes post-dose during the Dose Titration Phase at the highest tolerated APL-130277 dose level (indicated as Day 2) and the lowest APL-130277 dose resulting in a full 'ON' (indicated as Day 1) are presented." (NCT03187301)
Timeframe: Baseline (pre-dose) and at 30, 60 and 90 minutes after dosing during the Dose Titration Phase.

Interventionunits on a scale (Least Squares Mean)
30 mins post-dose (day 1)30 mins post-dose (day 2)60 mins post-dose (day 1)60 mins post-dose (day 2)90 mins post-dose (day 1)90 mins post-dose (day 2)
APL-130277 (Titration)-21.1-26.7-26.3-31.3-25.2-28.9

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AUClast of Apomorphine and Apomorphine Sulfate (Metabolite) Following the Administration of APL-130277

The area under the concentration-time curve from time of dosing to the last measurable point (AUClast) for apomorphine and apomorphine sulfate (metabolite) was determined in patients treated with APL-130277. PK parameters were derived using a non-compartmental analysis method. Bioanalysis of apomorphine and apomorphine-sulfate plasma concentration were measured using a validated LC/MS-MS method. The calibration range was 0.0200 ng/mL to 20.0 ng/mL apomorphine and 10.0 to 1000 ng/mL apomorphine sulfate. PK assessments were performed at each period of the Randomized Crossover Assessment Phase (at P1V1, P2V2 and P3V3) and results are presented for each of the APL-130277 doses administered (as determined for each patient during the Dose Titration Phase). (NCT03187301)
Timeframe: Blood samples for PK assessments were taken prior to dosing and at 0.5, 0.75, 1, 2, and 4 hours post-dose.

,,,,,
Interventionh*ng/mL (Mean)
ApomorphineApomorphine sulfate
10 mg APL-130277 PK Subset7.70558
15 mg APL-130277 PK Subset9.39734
20 mg APL-130277 PK Subset7.55861
25 mg APL-130277 PK Subset7.84870
35 mg APL-130277 PK Subset12.1979
50 mg APL-130277 PK Subset10.91980

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Cmax of Apomorphine and Apomorphine Sulfate (Metabolite) Following the Administration of APL-130277

The maximum observed plasma concentration (Cmax) for apomorphine and apomorphine sulfate (metabolite) was determined in patients treated with APL-130277. Pharmacokinetic (PK) parameters were derived using a non-compartmental analysis method. Bioanalysis of apomorphine and apomorphine-sulfate plasma concentration were measured using a validated liquid chromatography-tandem mass spectrometry (LC/MS-MS) method. The calibration range was 0.0200 nanograms per milliliter (ng/mL) to 20.0 ng/mL apomorphine and 10.0 to 1000 ng/mL apomorphine sulfate (metabolite). PK assessments were performed at each period of the Randomized Crossover Assessment Phase (at P1V1, P2V2 and P3V3) and results are presented for each of the APL-130277 doses administered (as determined for each patient during the Dose Titration Phase). (NCT03187301)
Timeframe: Blood samples for PK assessments were taken prior to dosing and at 0.5, 0.75, 1, 2, and 4 hours post-dose.

,,,,,
Interventionng/mL (Mean)
ApomorphineApomorphine sulfate
10 mg APL-130277 PK Subset5.14220
15mg AP:-130277 PK Subset6.57319
20 mg AP:-130277 PK Subset4.23377
25 mg APL-130277 PK Subset4.16446
35 mg APL-130277 PK Subset9.29458
50 mg AP:-130277 PK Subset4.611420

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ECG Assessments: Mean Change From Baseline to Post-Baseline Value for Heart Rate During Randomized Crossover Assessment Phase

Heart rate was determined during continuous 12-lead ECG (Holter) monitoring at each of the 3 treatment period dosing visits at pre-specified timepoints post-dose. Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (pre-dose P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 15, 30, 45 and 60 mins and 2, 3 and 4 hours post-dose at each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. Results are presented for the mean change from baseline at each pre-specified post-dose timepoint. (NCT03187301)
Timeframe: Baseline and at 15, 30, 45, 60 minutes and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase.

,,
InterventionBeats per minute (Least Squares Mean)
15 mins post-dose30 mins post-dose45 mins post-dose60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
APL-130277 (Cross-over)2.51.50.1-3.03.37.69.5
Moxifloxacin (Crossover)0.10.53.61.81.53.32.9
Placebo (Cross-over)2.12.10.80.12.84.66.2

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ECG Assessments: Mean Change From Baseline to Post-Baseline Value for PR Interval During Randomized Crossover Assessment Phase

PR interval was defined as time from the onset of the P wave to the start of the QRS complex. PR interval was determined during continuous 12-lead ECG (Holter) monitoring at each of the 3 treatment period dosing visits at pre-specified timepoints post-dose. Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (pre-dose P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 15, 30, 45 and 60 mins and 2, 3 and 4 hours post-dose at each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. Results are presented for the mean change from baseline at each pre-specified post-dose timepoint. (NCT03187301)
Timeframe: Baseline (pre-dose P1V1) and at 15, 30, 45, 60 minutes and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase.

,,
Interventionmsec (Least Squares Mean)
15 mins post-dose30 mins post-dose45 mins post-dose60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
APL-130277 (Cross-over)0.4-1.61.22.5-0.2-1.5-3.7
Moxifloxacin (Crossover)-1.1-0.2-1.11.5-0.11.60.8
Placebo (Cross-over)-1.9-0.20.1-0.3-1.7-2.2-3.1

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Time-Matched Change From Baseline in QTc, Placebo-Adjusted and Corrected for Heart Rate Based on QTcF Using ΔΔQTcF: Comparison Between Moxifloxacin and Placebo (Assay Sensitivity Analysis)

For the assay sensitivity analysis in support of the primary central tendency analysis, the changes from baseline (ΔQTcF) were compared between moxifloxacin (positive control) and placebo (ΔΔQTcF). Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 60 mins and 2, 3 and 4 hours post-dose for each of the 3 treatment period dosing visits in the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. These average values were used in all change from baseline calculations. (NCT03187301)
Timeframe: Baseline to 60 mins and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits.

,
Interventionmsec (Least Squares Mean)
60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
Moxifloxacin (Crossover)6.59.39.38.8
Placebo (Cross-over)-3.5-3.0-1.6-0.2

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Time-Matched Change From Baseline in QTc, Placebo-Adjusted and Corrected for Heart Rate Based on the Fridericia Correction Method (QTcF) Using Delta Delta Method (ΔΔQTcF): Comparison Between APL-130277 and Placebo (Central Tendency Analysis)

For the primary central tendency analysis, the changes from baseline (ΔQTcF) were compared between APL-130277 and placebo (ΔΔQTcF). Baseline was defined as the mean of the 9 ECGs (3 sets of triplicate ECGs) recorded at baseline (P1V1). In case any of the 9 ECGs were missing, the baseline was defined as the mean of the available baseline values. The post-dose ECGs were evaluated at 15, 30, 45 and 60 minutes (mins) and 2, 3 and 4 hours post-dose at each of the 3 treatment period dosing visits during the Randomized Crossover Assessment Phase. For each of the time points, an average value was calculated based on the 3 (or all available) ECGs. These average values were used in all change from baseline calculations. (NCT03187301)
Timeframe: Baseline to 15, 30, 45, 60 mins and 2, 3, and 4 hours post-dose for each of the 3 treatment period dosing visits.

,
Interventionmsec (Least Squares Mean)
15 mins post-dose30 mins post-dose45 mins post-dose60 mins post-dose2 hours post-dose3 hours post-dose4 hours post-dose
APL-130277 (Cross-over)0.20.30.02.71.80.1-0.9
Placebo (Cross-over)-3.7-2.7-3.7-3.5-3.0-1.6-0.2

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Median Time to 'ON' During the Dose Titration Phase

"The time to 'ON' was calculated as minutes from the time when the patient received APL-130277 until the time the patient turned fully 'ON', as assessed by the Investigator. Data was censored at 90 minutes.~The median time to a full 'ON' response during the Dose Titration Phase following the highest tolerated APL-130277 dose level (indicated as Day 2) and the lowest APL-130277 dose resulting in a full 'ON' (indicated as Day 1) are presented. The median time to 'ON' on Day 1 and Day 2 was calculated using the Kaplan-Meier method." (NCT03187301)
Timeframe: Time of dosing up to 90 minutes post-dose during the Dose Titration Phase.

Interventionminutes (Median)
Day 1Day 2
APL-130277 (Titration)3030

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Number of Participants With Culture Negative Status by 8 Weeks

Culture negative status is achieved when a participant produces at least two negative culture results at different visits (at least 7 days apart) without an intervening positive culture result for M.tb. (NCT03338621)
Timeframe: Days 0-56 (8 weeks)

InterventionParticipants (Count of Participants)
Drug Sensitive-TB 2HRZE/4HR70
Drug Sensitive-TB 4BPaMZ122

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Time to Culture Negative Status

Culture conversion is a diagnostic criteria indicating the point at which samples taken from a patient infected with a tuberculosis can no longer produce tuberculosis cell cultures, that point is considered culture negativity (NCT03338621)
Timeframe: During treatment (17 or 26 weeks)

Interventionweeks (Median)
Drug Sensitive-TB BPaMZ6
Drug Sensitive-TB 2HRZE/4HR11
Drug Resistant-TB BPaMZ5

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Change From Time Matched Baseline in Mean Individually-Corrected QT (QTcI) Values of Lasmiditan and Moxifloxacin

The corrected QT interval, individualized (QTcI) is a measurement of the electrical impulses through the largest part of the heart muscle individualized for participant pre-dose values. A negative change is a shortening of the QTc interval, a positive change is a lengthening of the QTc interval. (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

,,,
Interventionmilliseconds (Mean)
30 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose3.5 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
100 mg Lasmiditan-9.92-9.50-9.39-8.74-7.90-5.08-3.86-3.25-4.84-7.10-4.081.60
400 mg Lasmiditan-10.56-6.90-4.73-2.65-1.80-0.131.903.27-1.27-3.08-0.640.45
Moxifloxacin2.248.968.618.298.4011.0111.4310.284.854.044.876.74
Placebo-5.27-3.35-2.81-3.49-2.44-1.70-1.67-1.19-3.13-3.89-1.650.81

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Change From Baseline in Mean Heart Rate (HR) of Lasmiditan and Moxifloxacin

Heart rate was determined during ambulatory blood pressure monitoring (ABPM). (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

,,,
Interventionbeats per minute (Mean)
30 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose3.5 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
100 mg Lasmiditan-3.90-7.82-7.55-6.62-6.49-5.96-5.26-4.221.65-0.431.581.01
400 mg Lasmiditan-5.51-8.40-7.41-7.30-7.59-6.82-6.02-5.02-0.10-1.96-0.500.42
Moxifloxacin-1.02-0.42-0.67-1.52-1.48-1.26-0.91-0.555.843.104.950.81
Placebo-2.41-2.77-2.01-2.65-1.75-1.83-2.32-1.826.293.424.170.89

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Change From Baseline in Mean Cardiac Intervals:QRS of Lasmiditan and Moxifloxacin

ECGs were used to calculate cardiac intervals. The QRS interval is the time the segment of the ECG that corresponds to depolarization of the ventricles. (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

,,,
Interventionmilliseconds (Mean)
30 minutes postdose1 hours postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose3.5 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
100 mg Lasmiditan0.11-0.24-0.48-0.73-0.75-0.63-0.58-0.540.20-0.410.340.33
400 mg Lasmiditan-0.100.450.190.100.300.080.150.290.64-0.390.24-0.07
Moxifloxacin-0.00-0.12-0.12-0.29-0.20-0.35-0.57-0.580.13-0.670.320.09
Placebo0.09-0.02-0.37-0.30-0.21-0.26-0.17-0.200.73-0.280.63-0.10

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Number of Incidents in Electrocardiogram (ECG) Abnormalities in QTcF Interval Greater Than 450 Milliseconds

ECGs were assessed for morphology abnormalities or changes in QTcf interval greater than 450 milliseconds by a board-certified cardiologist (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

,,,
InterventionIncidents (Number)
Predose30 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose3.5 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
100 mg Lasmiditan0020111110000
400 mg Lasmiditan0001111210100
Moxifloxacin0122322330000
Placebo0000000000000

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Pharmacokinetics (PK): Area Under the Concentration Time Curve (AUC-t) of Lasmiditan

Pharmacokinetics (PK): Area Under the Concentration Time Curve (AUC-t) of Lasmiditan. (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

Interventionhours*nanogram per milliliter (Geometric Mean)
100 mg Lasmiditan684.66
400 mg Lasmiditan3189.08

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

Pharmacokinetics (PK): Maximum Concentration (Cmax) of Lasmiditan. (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

Interventionnanogram per milliliter (Mean)
100 mg Lasmiditan104.55
400 mg Lasmiditan526.15

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Change From Baseline in Mean Cardiac Intervals: RR Interval of Lasmiditan and Moxifloxacin

ECGs were used to calculate cardiac intervals. The RR interval is the time between two R waves. (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

,,,
Interventionmilliseconds (Mean)
30 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose3.5 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
100 mg Lasmiditan74.40149.22143.29118.39117.90105.5689.8572.22-26.015.63-26.70-16.37
400 mg Lasmiditan98.52153.15130.79128.10132.86119.52101.8683.00-3.0729.015.19-5.64
Moxifloxacin18.669.6313.4426.0126.9024.8719.0113.64-84.12-49.70-74.80-13.02
Placebo42.1349.8736.8444.6929.2830.8436.7730.32-88.95-50.89-61.53-11.66

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Change From Time Matched Baseline in Mean Fridericia-Corrected QT (QTcF) Values of Lasmiditan and Moxifloxacin

The QT interval is a measure of the time between the start of the Q wave and the end of the T wave and was calculated from electrocardiogram (ECG) data using Fridericia's formula: QTcF = QT/RR^0.33. Corrected QT (QTc) is the QT interval corrected for heart rate and R-R wave (RR), which is the interval between two R waves. PR is the interval between the P wave and the ventricular depolarization wave (QRS) complex. (NCT03465436)
Timeframe: Day 1: Predose, 30 minutes postdose, 1 hour (hr), 1.5 hr, 2 hr, 2.5 hr, 3 hr, 3.5 hr, 4 hr, 6 hr, 8, hr, 12 hr and 24 hr postdose

,,,
Interventionmilliseconds (Mean)
30 minutes postdose1 hour postdose1.5 hours postdose2 hours postdose2.5 hours postdose3 hours postdose3.5 hours postdose4 hours postdose6 hours postdose8 hours postdose12 hours postdose24 hours postdose
100 mg Lasmiditan-8.90-7.42-7.63-6.96-5.26-2.81-2.39-2.12-4.33-6.74-3.730.74
400 mg Lasmiditan-9.27-4.58-3.07-1.120.152.063.584.77-0.18-1.84-0.410.38
Moxifloxacin1.908.367.638.168.1210.0110.379.394.913.904.636.61
Placebo-5.49-3.94-3.68-3.83-2.89-2.04-1.85-2.34-3.39-3.99-1.790.45

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Time-matched Difference Between the OPC-61815/Moxifloxacin and Placebo Data in Change From Baseline for QTcF in 12-lead Holter Electrocardiogram (ECG)

For each OPC-61815 dose, the upper limit of the confidence interval (CI) for the time-matched difference in the least squares (LS) mean for the change in QT corrected for heart rate by Fridericia's formula (QTcF) from baseline compared to the placebo data was evaluated to determine if it was lower than 10 msec at all postdose time points. Using a linear mixed effect model with baseline QTcF in each treatment period as a covariate, treatment, sequence, treatment period, time point, and interaction between treatment and time point as fixed effects, and subject as a random effect, point estimates and CIs for the time-matched difference in the LS mean for the change in QTcF from baseline compared to the placebo data were calculated. (NCT03510663)
Timeframe: Baseline, 1h, 1.5h, 2h, 3h, 4h, 6h, 12h, 24h after dosing

,,,
Interventionmsec (Least Squares Mean)
1 hour postdose1.5 hours postdose2 hours postdose3 hours postdose4 hours postdose6 hours postdose12 hours postdose24 hours postdose
Moxifloxacin9.99.510.810.911.11.92.64.3
OPC-61815 16 mg0.92.01.7-1.2-2.6-11.9-9.6-3.6
OPC-61815 32 mg0.01.30.4-2.2-2.2-10.8-9.8-2.8
Placebo-0.9-0.7-0.4-0.61.5-8.5-4.7-2.7

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Change From Baseline in PR Interval (PR)

Electrocardiogram measurement of change from baseline in PR interval (PR) (NCT03577275)
Timeframe: 24 hours

Interventionmsec (Least Squares Mean)
Placebo-11.0
Moxifloxacin 400mg-11.9
NST-4016 600mg-11.4
NST-4016 2000mg-12.4

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Change From Baseline in QRS Interval (QRS)

Electrocardiogram measurement of change from baseline in QRS interval (QRS) (NCT03577275)
Timeframe: 2 hours

Interventionmsec (Least Squares Mean)
Placebo-0.2
Moxifloxacin 400mg-0.1
NST-4016 600mg-0.2
NST-4016 2000mg0.2

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Change From Baseline in Fridericia's Correction for QT Interval (QTcF)

Electrocardiogram measurement of change from baseline in Fridericia's correction for QT interval (QTcF) (NCT03577275)
Timeframe: 24 hours

Interventionmsec (Least Squares Mean)
Placebo-4.6
Moxifloxacin 400mg11.5
NST-4016 600mg-6.0
NST-4016 2000mg-5.7

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Change From Baseline in Fridericia's Correction for QT Interval (QTcF)

Electrocardiogram measurement of the maximum absolute change from baseline in Fridericia's correction for QT interval (QTcF) (NCT03577275)
Timeframe: 24 hours

Interventionmsec (Least Squares Mean)
Placebo Oral Capsule-4.6
Moxifloxacin 400mg11.5
NST-4016 600mg-6.0
NST-4016 2000mg-6.1

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Change From Baseline in Heart Rate (HR)

Electrocardiogram measurement of change from baseline in heart rate (HR) maximum values presented (NCT03577275)
Timeframe: 24 hours

Interventionbeats per minute (Least Squares Mean)
Placebo9.9
Moxifloxacin 400mg12.2
NST-4016 600mg12.6
NST-4016 2000mg15.6

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Changes From Baseline in ECG Measures: Ventricular Rate

Change from baseline in ECG Ventricular Rate is calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h, 24 h after dosing and prior to the next dose (follow up). (NCT03613649)
Timeframe: Baseline, 1 h, 2 h, 4h, 24 h post-dose and follow up

,,,
Interventionbeats/minute (Mean)
Ventricular Rate: 1 hr post doseVentricular Rate: 2 hr post doseVentricular Rate: 4 hr post doseVentricular Rate: 24 hr post doseVentricular Rate: Follow up
2 g of Zoliflodacin2.42.92.83.92.8
4 g of Zoliflodacin3.34.64.14.63.1
400 mg of Moxifloxacin4.73.62.83.53.9
Placebo0.90.40.22.91.8

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Changes From Baseline in ECG Measures: PR Interval, QRS Duration, QT Interval, QTcF Interval and RR Interval

Change from baseline in ECG is calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h, 24 h after dosing and prior to the next dose (follow up). The following ECG Parameters were analyzed: PR Interval (Interval From Onset of P-wave to the Onset of the QRS Complex), QRS Duration (Time From the Start of the Q-wave to the End of the S-wave), QT Interval (Interval From Onset of the Q-wave to the End of the T-wave), QTcF Interval (QT Interval Corrected by Fridericia's Formula) and RR Interval (Interval From the Peak of the R Wave of a QRS Complex to the Peak of the R Wave of the Next QRS Complex). (NCT03613649)
Timeframe: Baseline, 1 h, 2 h, 4h, 24 h post-dose and follow up

,,,
Interventionmilliseconds (msec) (Mean)
PR Interval: 1 hr post dosePR Interval: 2 hr post dosePR Interval: 4 hr post dosePR Interval: 24 hr post dosePR Interval: Follow upQRS Duration: 1 hr post doseQRS Duration: 2 hr post doseQRS Duration: 4 hr post doseQRS Duration: 24 hr post doseQRS Duration: Follow upQT Interval: 1 hr post doseQT Interval: 2 hr post doseQT Interval: 4 hr post doseQT Interval: 24 hr post doseQT Interval: Follow upQTcF Interval: 1 hr post doseQTcF Interval: 2 hr post doseQTcF Interval: 4 hr post doseQTcF Interval: 24 hr post doseQTcF Interval: Follow upRR Interval: 1 hr post doseRR Interval: 2 hr post doseRR Interval: 4 hr post doseRR Interval: 24 hr post doseRR Interval: Follow up
2 g of Zoliflodacin1.21.2-0.31.1-1.2-1.8-1.9-2.0-2.7-1.4-3.6-5.3-5.0-6.8-7.11.50.40.71.5-1.4-34.9-38.5-38.8-57.6-39.6
4 g of Zoliflodacin0.0-0.7-1.40.7-1.9-0.6-1.4-1.0-1.10.3-6.2-7.6-9.1-7.6-6.60.62.0-1.31.9-0.2-48.4-68.7-54.3-66.9-45.6
400 mg of Moxifloxacin1.30.4-0.92.8-0.9-0.5-1.5-1.6-1.1-0.2-1.42.32.0-3.7-10.09.210.68.54.1-1.4-74.5-59.0-46.6-56.8-62.1
Placebo1.30.6-0.40.5-3.10.4-0.7-0.7-0.9-1.1-2.5-3.6-3.8-9.9-8.3-0.4-2.9-3.0-3.5-3.8-14.1-3.3-4.8-45.9-32.4

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Changes From Baseline for Blood Pressure - Diastolic

Change from baseline in diastolic blood pressure was calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h and 24 h after dosing. Follow up is defined as the check in visit for the next dosing period or the final visit. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

,,,
InterventionmmHg (Mean)
1 hour post dose2 hour post dose4 hour post dose24 hour post doseFollow up
2 g of Zoliflodacin0.3-0.4-0.40.22.2
4 g of Zoliflodacin0.3-0.9-2.3-0.50.5
400 mg of Moxifloxacin1.51.2-0.11.13.8
Placebo0.80.61.11.42.7

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Time-matched, Placebo-corrected, Baseline-adjusted, the Time From the Onset of the P Wave to the Start of the QRS Complex (PR Interval) Following Administration of Zoliflodacin

Mean and 90% two-sided confidence intervals (t-intervals) of change from baseline PR intervals by time point and treatment. Note that the upper bound of the 90% two-sided confidence interval can also be interpreted as the upper bound of a 95% one-sided confidence interval. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

,,
Interventionmilliseconds (msec) (Mean)
0.5 hour post dose1 hour post dose2 hour post dose3 hour post dose4 hour post dose6 hour post dose8 hour post dose12 hour post dose24 hour post dose
2 g of Zoliflodacin-0.7-0.9-1.6-2.6-2.8-3.6-5.7-3.0-1.7
4 g of Zoliflodacin-1.1-2.3-1.8-2.9-3.2-3.9-5.4-3.5-0.8
Placebo-0.30.2-0.2-1.1-0.6-1.8-5.3-4.3-0.7

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Time-matched, Placebo-corrected, Baseline-adjusted QRS Duration Following Administration of Zoliflodacin

Mean and 90% two-sided confidence intervals (t-intervals) of change from baseline QRS durations by time point and treatment. Note that the upper bound of the 90% two-sided confidence interval can also be interpreted as the upper bound of a 95% one-sided confidence interval. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

,,
Interventionmilliseconds (msec) (Mean)
0.5 hour post dose1 hour post dose2 hour post dose3 hour post dose4 hour post dose6 hour post dose8 hour post dose12 hour post dose24 hour post dose
2 g of Zoliflodacin-0.3-0.5-0.6-0.4-0.50.1-0.7-0.4-0.5
4 g of Zoliflodacin-0.10.1-0.5-0.4-0.20.1-0.7-0.5-0.2
Placebo-0.30.00.0-0.1-0.10.8-0.3-0.3-0.4

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Number of Participants With Treatment-emergent Adverse Events Following Administration of Study Product

Adverse events are defined as any untoward medical occurrence regardless of its causal relationship to the study treatment. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

InterventionParticipants (Count of Participants)
2 g of Zoliflodacin38
4 g of Zoliflodacin46
Placebo35
400 mg of Moxifloxacin41

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Maximum Observed Concentration (Cmax) of Zoliflodacin

Cmax is defined as the maximum observed drug concentration observed in plasma over all PK sample concentrations computed from concentrations that were measured using a validated HPLC-MS/MS method. Pharmacokinetic (PK) parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

Interventionng/mL (Mean)
2 g of Zoliflodacin12120
4 g of Zoliflodacin20350

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Elimination Rate Constant (Ke) of Zoliflodacin

The terminal phase elimination rate constant (Ke) was defined as the first-order rate constant describing the rate of decrease of drug concentration in the terminal phase (defined as the terminal region of the PK curve where drug concentration follows first-order elimination kinetics) computed from concentrations that were measured using a validated HPLC-MS/MS method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

Intervention1/hour (Mean)
2 g of Zoliflodacin0.1267
4 g of Zoliflodacin0.1174

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Area Under the Concentration Time-curve From Time Zero to the Last Concentration Above the Lower Limit of Quantitation (AUC(0-last)) for Zoliflodacin

AUC(0-last) was defined as the area under the concentration-time curve from dosing (time 0) to the time of the last measured concentration computed from concentrations that were measured using a validated HPLC-MS/MS method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

Interventionh*ng/mL (Mean)
2 g of Zoliflodacin102700
4 g of Zoliflodacin177300

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Time-matched, Placebo-corrected, Baseline-adjusted the Time Elapsed Between Two Successive R Waves of the QRS (RR Interval) Following Administration of Zoliflodacin

Mean and 90% two-sided confidence intervals (t-intervals) of change from baseline RR intervals by time point and treatment. Note that the upper bound of the 90% two-sided confidence interval can also be interpreted as the upper bound of a 95% one-sided confidence interval. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

,,
Interventionmilliseconds (msec) (Mean)
0.5 hour post dose1 hour post dose2 hour post dose3 hour post dose4 hour post dose6 hour post dose8 hour post dose12 hour post dose24 hour post dose
2 g of Zoliflodacin-5.8-22.6-13.8-32.0-23.3-127.1-120.2-141.2-37.4
4 g of Zoliflodacin-33.5-35.0-51.0-63.1-47.6-133.0-111.0-139.8-41.2
Placebo-1.29.73.0-10.1-0.7-113.7-87.5-140.5-50.2

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Area Under the Concentration Time-curve From Time Zero to Infinity (AUC(0 - Infinity)) for Zoliflodacin

AUC(0 - infinity) was defined as the total area under the concentration-time curve from dosing (time 0) taken to the limit as the end time becomes arbitrarily large. AUC(0 - infinity) was calculated by adding AUC(0-last) to an extrapolated value equal to the last measured concentration greater than the lower limit of quantification of the bioanalytical assay divided by the terminal phase elimination rate constant (Ke) computed from concentrations that were measured using a validated HPLC-MS/MS method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

Interventionh x ng/mL (Mean)
2 g of Zoliflodacin108300
4 g of Zoliflodacin181400

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Apparent Volume of Distribution (Vz/F) of Zoliflodacin

Apparent volume of distribution during terminal phase (Vz/F) after non-intravenous administration was calculated as (CL/F)/ Ke computed from concentrations that were measured using a validated HPLC-MS/MS method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

InterventionLiter (Mean)
2 g of Zoliflodacin160.55
4 g of Zoliflodacin204.29

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Apparent Oral Clearance (CL/F) of Zoliflodacin

Apparent oral clearance (CL/F) computed as Dose/Area under the curve (AUC) from time zero to infinity (0-infinity) computed from concentrations that were measured using a validated high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

InterventionLiter/hour (Mean)
2 g of Zoliflodacin20.08
4 g of Zoliflodacin23.77

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Changes From Baseline for Temperature

Change from baseline for temperature was calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h and 24 h after dosing. Follow up is defined as the check in visit for the next dosing period or the final visit. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

,,,
InterventionCelsius (Mean)
1 hour post dose2 hour post dose4 hour post dose24 hour post doseFollow up
2 g of Zoliflodacin0.080.100.080.090.05
4 g of Zoliflodacin0.030.060.050.06-0.02
400 mg of Moxifloxacin0.050.110.130.100.05
Placebo0.030.090.090.040.00

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Changes From Baseline for Blood Pressure - Systolic

Change from baseline in systolic blood pressure was calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h and 24 h after dosing. Follow up is defined as the check in visit for the next dosing period or the final visit. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

,,,
InterventionmmHg (Mean)
1 hour post dose2 hour post dose4 hour post dose24 hour post doseFollow up
2 g of Zoliflodacin0.80.40.10.03.5
4 g of Zoliflodacin1.3-0.3-0.9-0.42.3
400 mg of Moxifloxacin0.4-0.5-1.70.55.0
Placebo0.81.01.01.13.7

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Changes From Baseline for Glomerular Filtration Rate (GFR) - Estimated

Change from baseline calculated by subtracting the Day -1 (baseline) chemistry measurement from the 24 h post dose, and a follow up chemistry measurement. Follow up is defined as either the check-in visit for the next period or the final visit. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
InterventionmL/minute (Mean)
GFR: 24 hour post doseGFR: Follow up
2 g of Zoliflodacin-10.4-5.3
4 g of Zoliflodacin-9.51.8
400 mg of Moxifloxacin-6.21.5
Placebo-0.1-0.7

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Changes From Baseline for Hematocrit

Change from baseline for hematocrit is calculated by subtracting the Day -1 (baseline) hematology measurement from the 24 h post dose, and a follow up hematology measurement. Follow up is defined as either the check-in visit for the next period or the final visit. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Interventionvolume percentage of RBC in blood (Mean)
Hematocrit: 24 hour post doseHematocrit: Follow up
2 g of Zoliflodacin0.39-0.03
4 g of Zoliflodacin-0.10-0.69
400 mg of Moxifloxacin-0.26-0.33
Placebo0.08-0.10

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Changes From Baseline for Hemoglobin

Change from baseline for hemoglobin is calculated by subtracting the Day -1 (baseline) hematology measurement from the 24 h post dose, and a follow up hematology measurement. Follow up is defined as either the check-in visit for the next period or the final visit. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Interventiong/dL (Mean)
Hemoglobin: 24 hour post doseHemoglobin: Follow up
2 g of Zoliflodacin0.15-0.01
4 g of Zoliflodacin0.01-0.23
400 mg of Moxifloxacin-0.06-0.13
Placebo0.04-0.06

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Changes From Baseline for Magnesium, Glucose (Fasting), Blood Urea Nitrogen (BUN), Creatinine, Total Bilirubin, Direct Bilirubin

Change from baseline calculated by subtracting the Day -1 (baseline) chemistry measurement from the 24 h post dose, and a follow up chemistry measurement. Follow up is defined as either the check-in visit for the next period or the final visit. Chemistry parameters included magnesium, glucose (fasting), BUN, creatinine, total bilirubin, direct bilirubin (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Interventionmg/dL (Mean)
Magnesium: 24 hour post doseMagnesium: Follow upGlucose (fasting): 24 hour post doseGlucose (fasting): Follow upBUN: 24 hour post doseBUN: Follow upCreatinine: 24 hour post doseCreatinine: Follow upTotal Bilirubin: 24 hour post doseTotal Bilirubin: Follow upDirect Bilirubin: 24 hour post doseDirect Bilirubin: Follow up
2 g of Zoliflodacin0.050.044.6-1.22.10.70.0820.0340.070.010.00-0.01
4 g of Zoliflodacin0.030.006.41.51.60.00.086-0.0110.14-0.040.020.00
400 mg of Moxifloxacin0.010.013.21.02.5-0.20.059-0.007-0.04-0.02-0.01-0.01
Placebo0.020.024.2-0.61.40.10.0030.006-0.01-0.010.000.01

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Changes From Baseline for Platelets

Change from baseline for platelets is calculated by subtracting the Day -1 (baseline) hematology measurement from the 24 h post dose, and a follow up hematology measurement. Follow up is defined as either the check-in visit for the next period or the final visit. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Intervention10^3 platelets/microliter (Mean)
Platelets: 24 hour post dosePlatelets: Follow up
2 g of Zoliflodacin-8.21.7
4 g of Zoliflodacin-10.32.9
400 mg of Moxifloxacin-15.4-3.8
Placebo-10.56.2

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Changes From Baseline for Pulse Rate

Change from baseline in pulse rate was calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h and 24 h after dosing. Follow up is defined as the check in visit for the next dosing period or the final visit. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

,,,
Interventionbeats/minute (Mean)
1 hour post dose2 hour post dose4 hour post dose24 hour post doseFollow up
2 g of Zoliflodacin5.23.95.44.92.0
4 g of Zoliflodacin5.76.55.85.22.8
400 mg of Moxifloxacin6.95.55.26.34.2
Placebo2.83.83.05.42.0

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Changes From Baseline for Respiratory Rate

Change from baseline in respiratory rate was calculated by subtracting the baseline (pre-dose) measurement from the post-dose measurement. Post-dose measurements were taken 1 h, 2 h, 4 h and 24 h after dosing. Follow up is defined as the check in visit for the next dosing period or the final visit. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

,,,
Interventionbreaths/minute (Mean)
1 hour post dose2 hour post dose4 hour post dose24 hour post doseFollow up
2 g of Zoliflodacin0.80.40.80.90.6
4 g of Zoliflodacin1.10.71.31.01.3
400 mg of Moxifloxacin0.40.00.10.50.6
Placebo1.0-0.3-0.20.60.2

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Changes From Baseline for Erythrocytes

Change from baseline for erythrocytes is calculated by subtracting the Day -1 (baseline) hematology measurement from the 24 h post dose, and a follow up hematology measurement. Follow up is defined as either the check-in visit for the next period or the final visit. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Intervention10^6 cells/microliter (Mean)
Erythrocytes: 24 hour post doseErythrocytes: Follow up
2 g of Zoliflodacin0.050-0.005
4 g of Zoliflodacin-0.008-0.088
400 mg of Moxifloxacin-0.031-0.053
Placebo-0.002-0.029

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Changes From Baseline for Total Protein and Albumin

Change from baseline calculated by subtracting the Day -1 (baseline) chemistry measurement from the 24 h post dose, and a follow up chemistry measurement. Follow up is defined as either the check-in visit for the next period or the final visit. Chemistry parameters included total protein and albumin. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Interventiong/dL (Mean)
Total Protein: 24 hour post doseTotal Protein: Follow upAlbumin: 24 hour post doseAlbumin: Follow up
2 g of Zoliflodacin-0.42-0.01-0.280.00
4 g of Zoliflodacin-0.42-0.06-0.30-0.05
400 mg of Moxifloxacin-0.450.03-0.320.02
Placebo-0.45-0.01-0.300.01

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Incidence of Abnormal T-wave Morphology Following Administration of Zoliflodacin

Categorical T-wave morphology analysis was collected in three ECG replicates at each timepoint (Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose). Abnormalities present in any one or more of the baseline timepoint replicate ECGs recorded for a particular period was considered to be present at baseline for post-dose ECGs from that specific period. If a subject had an ECG morphological abnormality in more than one replicate ECG of a study timepoint, the subject was counted only once for that timepoint. Flat is defined as T amplitude <1 mm (either positive or negative) including flat isoelectric line and Biphasic is defined as T-wave that contains a second component with an opposite phase that was at least 0.1 millivolts (mV) deep (both positive and negative/positive and polyphasic T-waves included). (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

,,,
InterventionParticipants (Count of Participants)
0.5 h post dose: T wave: Abnormal, Biphasic0.5 h post dose: T wave: Abnormal, Flat0.5 h post: T wave:Abnormal, Inverted, Asymmetric1 h post dose: T wave: Abnormal, Biphasic1 h post dose: T wave: Abnormal, Flat1 h post: T wave: Abnormal, Inverted, Asymmetric2 h post dose: T wave: Abnormal, Biphasic2 h post dose: T wave: Abnormal, Flat2 h post: T wave: Abnormal, Inverted, Asymmetric3 h post dose: T wave: Abnormal, Biphasic3 h post dose: T wave: Abnormal, Flat3 h post:T wave: Abnormal, Inverted, Asymmetric4 h post dose: T wave: Abnormal, Biphasic4 h post dose: T wave: Abnormal, Flat4 h post:T wave: Abnormal, Inverted, Asymmetric6 h post dose: T wave: Abnormal, Biphasic6 h post dose: T wave: Abnormal, Flat6 h post:T wave: Abnormal, Inverted, Asymmetric8 h post dose: T wave: Abnormal, Biphasic8 h post dose: T wave: Abnormal, Flat8 h post:T wave: Abnormal, Inverted, Asymmetric12 h post dose: T wave: Abnormal, Biphasic12 h post dose: T wave: Abnormal, Flat12 h post:T wave: Abnormal, Inverted, Asymmetric24 h post dose: T wave: Abnormal, Biphasic24 h post dose: T wave: Abnormal, Flat24 h post:T wave: Abnormal, Inverted, Asymmetric
2 g of Zoliflodacin000000000000000040010041000
4 g of Zoliflodacin000000020021021141121121100
400 mg of Moxifloxacin000000010000000051010010010
Placebo000000000000000062030010000

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Occurrence of Urinalysis Adverse Events Following Administration of Study Product

Urine for the clinical laboratory test was collected on Day -1, 24 hour post dose and the check in for the following dosing period. The results for glucose dipstick, protein dipstick and occult blood - dipstick were reported in categorical results. The possibilities were negative, trace, 1+, 2+, and 3+. If the dipsticks were 1+ or greater, microscopic evaluations were performed for erythrocytes, leukocytes and bacteria. For microscopic results to be deemed abnormal, the results must be reported 6 or greater per high power field. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

,,,
InterventionParticipants (Count of Participants)
Glucose dipstick: 24 hour post doseGlucose dipstick: Follow upProtein dipstick: 24 hour post doseProtein dipstick: Follow upOccult blood dipstick: 24 hour post doseOccult blood dipstick: Follow upErythrocytes microscopic: 24 hour post doseErythrocytes microscopic: Follow upLeukocytes microscopic: 24 hour post doseLeukocytes microscopic: Follow upBacteria microscopic: 24 hour post doseBacteria microscopic: Follow up
2 g of Zoliflodacin001214230002
4 g of Zoliflodacin001042211031
400 mg of Moxifloxacin000131322020
Placebo000050220122

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The One-sided 95% Confidence Interval (CI) for the Largest Time-matched, Placebo-corrected, Baseline-adjusted Mean QTcF Interval (Delta Delta QTcF) Following Administration of Zoliflodacin

Mean and 90% two-sided confidence intervals (t-intervals) of change from baseline QTcF intervals by time point and treatment. Note that the upper bound of the 90% two-sided confidence interval can also be interpreted as the upper bound of a 95% one-sided confidence interval. (NCT03613649)
Timeframe: Baseline, 0.5 hour (h), 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose after 2 and 4 g zolifloadacin

,,
Interventionmilliseconds (msec) (Mean)
0.5 hour post dose1 hour post dose2 hour post dose3 hour post dose4 hour post dose6 hour post dose8 hour post dose12 hour post dose24 hour post dose
2 g of Zoliflodacin-3.2-1.9-2.3-1.6-2.4-2.0-5.6-2.8-2.9
4 g of Zoliflodacin-1.00.10.10.10.1-0.7-4.7-0.4-0.3
Placebo-2.1-2.3-2.2-2.6-3.3-2.3-4.4-2.2-2.2

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The One-sided 95% Confidence Interval (CI) of the Time-matched, Placebo-corrected, Baseline-adjusted Mean QTcF Interval (Delta Delta QTcF) After a Single Dose of Moxifloxacin

Mean and 90% two-sided confidence intervals (t-intervals) of change from baseline QTcF intervals by time point and treatment. Note that the upper bound of the 90% two-sided confidence interval can also be interpreted as the upper bound of a 95% one-sided confidence interval. (NCT03613649)
Timeframe: Baseline, 1 h, 2 h, 3 h, and 4 h post-dose

,
Interventionmilliseconds (msec) (Mean)
1 hour post dose2 hour post dose3 hour post dose4 hour post dose
400 mg of Moxifloxacin7.98.58.07.2
Placebo-2.3-2.2-2.6-3.3

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Number of Participants With Treatment-emergent Serious Adverse Events Following Administration of Zoliflodacin and Moxifloxacin

Serious adverse events included any untoward medical occurrence that resulted in death; was life threatening; was a persistent/significant disability/incapacity; required inpatient hospitalization or prolongation or a congenital anomaly/birth defect. (NCT03613649)
Timeframe: From study product administration (Day 1) through prior to the next dose (Day 8 or Final visit).

InterventionParticipants (Count of Participants)
2 g of Zoliflodacin0
4 g of Zoliflodacin0
Placebo0
400 mg of Moxifloxacin0

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Time-matched, Placebo-corrected, Baseline-adjusted Heart Rate (HR) Following Administration of Zoliflodacin

Mean and 90% two-sided confidence intervals (t-intervals) of change from baseline heart rate by time point and treatment. Note that the upper bound of the 90% two-sided confidence interval can also be interpreted as the upper bound of a 95% one-sided confidence interval. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

,,
Interventionbeats/minute (Mean)
0.5 hour post dose1 hour post dose2 hour post dose3 hour post dose4 hour post dose6 hour post dose8 hour post dose12 hour post dose24 hour post dose
2 g of Zoliflodacin0.41.61.02.21.69.48.710.62.5
4 g of Zoliflodacin2.22.33.64.53.710.08.310.42.8
Placebo0.1-0.60.10.70.007.85.89.73.4

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Changes From Baseline for White Blood Cells With Differentials

Change from baseline calculated by subtracting the Day -1 (baseline) hematology measurement from the 24 h post dose, and a follow up hematology measurement. Follow up is defined as either the check-in visit for the next period or the final visit. Hematology parameters included white blood cell count, and differential (absolute counts of neutrophils, lymphocytes, monocytes, eosinophils, and basophils). (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Interventioncells/microliter (Mean)
Leukocytes: 24 hour post doseLeukocytes: Follow upNeutrophils: 24 hour post doseNeutrophils: Follow upLymphocytes: 24 hour post doseLymphocytes: Follow upMonocytes: 24 hour post doseMonocytes: Follow upEosinophils: 24 hour post doseEosinophils: Follow upBasophils: 24 hour post doseBasophils: Follow up
2 g of Zoliflodacin-246.4-273.5-248.0-272.23.4-19.6-7.84.69.412.9-3.40.6
4 g of Zoliflodacin-129.9140.3-39.6220.4-77.9-74.1-13.9-7.64.02.2-2.5-0.5
400 mg of Moxifloxacin-282.9-84.1-351.3-59.279.4-33.7-16.15.28.22.3-3.11.4
Placebo-64.335.8-54.3-36.1-1.996.9-10.6-25.46.00.7-3.3-0.2

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Changes From Baseline for Sodium, Potassium, Chloride and Bicarbonate

Change from baseline calculated by subtracting the Day -1 (baseline) chemistry measurement from the 24 h post dose, and a follow up chemistry measurement. Follow up is defined as either the check-in visit for the next period or the final visit. Chemistry parameters included sodium, potassium. chloride and bicarbonate. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
Interventionmmol/L (Mean)
Sodium: 24 hour post doseSodium: Follow upPotassium: 24 hour post dosePotassium: Follow upChloride: 24 hour post doseChloride: Follow upBicarbonate: 24 hour post doseBicarbonate: Follow up
2 g of Zoliflodacin0.20.10.260.011.30.30.2-0.2
4 g of Zoliflodacin-0.1-0.30.25-0.021.0-0.30.1-0.3
400 mg of Moxifloxacin0.70.20.11-0.011.40.10.4-0.1
Placebo0.60.60.170.011.40.50.60.3

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Relationship Between Plasma Concentrations of Zoliflodacin and Time-matched, Placebo-corrected, Baseline-adjusted Mean QTcF Interval (Delta Delta QTcF) Following Administration of Zoliflodacin

One-sided 95% confidence intervals of population mean QTcF time-matched, placebo-corrected, baseline-adjusted mean QTcF interval at plasma concentration corresponding to the observed geometric mean Cmax for 2 g and 4 g doses of zoliflodacin were computed using a linear mixed effect model with PK and concentration data collected at baseline and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

Interventionmilliseconds (msec) (Mean)
2 g of Zoliflodacin1.5
4 g of Zoliflodacin3.0

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Terminal Elimination Half-life (t1/2) of Zoliflodacin

The apparent terminal elimination half-life (t1/2) was defined as the time required for the drug concentration to decrease by a factor of one-half in the terminal phase computed from concentrations that were measured using a validated HPLC-MS/MS method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

InterventionHour (Mean)
2 g of Zoliflodacin5.55
4 g of Zoliflodacin5.99

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Time of Maximum Observed Concentration (Tmax) of Zoliflodacin

Tmax is defined as the time at which the maximum concentration (Cmax) occurs in plasma computed from concentrations that were measured using a validated HPLC-MS/MS method. PK parameters were computed using plasma concentrations from samples collected pre-dose and intervals post-dose. (NCT03613649)
Timeframe: Baseline, 0.5 h, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, and 24 h post-dose

Interventionhour (Mean)
2 g of Zoliflodacin2.90
4 g of Zoliflodacin3.03

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Changes From Baseline for Aspartate Aminotransferase (AST), Alanine Aminotransferase (ALT) and Alkaline Phosphatase (AP)

Change from baseline calculated by subtracting the Day -1 (baseline) chemistry measurement from the 24 h post dose, and a follow up chemistry measurement. Follow up is defined as either the check-in visit for the next period or the final visit. Chemistry parameters included AST, ALT and AP. (NCT03613649)
Timeframe: Prior to dosing, 24 hour post dose through prior to the next dose (Day 8 or Final visit).

,,,
InterventionU/L (Mean)
AST: 24 hour post doseAST: Follow upALT: 24 hour post doseALT: Follow upAP: 24 hour post doseAP: Follow up
2 g of Zoliflodacin-2.90.1-2.2-0.7-5.2-1.7
4 g of Zoliflodacin-2.70.0-1.71.6-3.9-0.4
400 mg of Moxifloxacin-2.80.6-1.40.8-4.21.0
Placebo-2.7-0.5-1.7-0.6-4.1-0.7

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Predicted Value of ∆∆QTc at Cmax

Concentration-response relationship was investigated between ∆QTc and P03277 concentrations using a mixed model approach. Plasma concentration of P03277 was measured at the same timepoints as ECG measurements. (NCT03657264)
Timeframe: from 1 hour before any administration until 24 hours post-administration.

Interventionmilliseconds (Number)
P03277 0.1 mmol/kg0.41
P03277 0.3 mmol/kg2.23

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Change-from-baseline Mean Effect of Moxifloxacin on QT Interval Expressed as QTc According to Fridericia's Formula (∆QTcF)

Each subject was monitored with a 12-lead Holter electrocardiogram (ECG). The assay sensitivity was assessed through this outcome. The difference between the positive control (moxifloxacin) and placebo for the largest mean change from baseline for the QTcF had to be greater than 5 milliseconds for at least one time point. The baseline was defined as the mean of the 3 triplicates ECG measured within 1 hour before each product administration. (NCT03657264)
Timeframe: from 1 hour before any administration until 4 hours post-administration at the following timepoints: -1 hour, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours.

,
Interventionmilliseconds (Least Squares Mean)
1 hour1.5 hours2 hours3 hours4 hours
Placebo-2.89-3.27-1.950.170.63
Positive Control (Moxifloxacin)1.736.138.6010.5011.28

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Change-from-baseline Mean Effect of P03277 on QT Interval Expressed as QTc According to Fridericia's Formula (∆QTcF)

"Each subject was monitored with a 12-lead Holter electrocardiogram (ECG). The study had to show that both 0.1 and 0.3 mmol/kg doses of P03277 do not increase the QT interval corrected by Fridericia formula (QTcF).~The study is successful if the difference between each of the two doses of P03277 and placebo for the largest mean change from baseline for the QTcF is lower than 10 milliseconds. The baseline was defined as the mean of the 3 triplicates ECG measured within 1 hour before each product administration." (NCT03657264)
Timeframe: from 1 hour before any administration until 24 hours post-administration at the following timepoints: -1 hour, 5 min, 10 min, 20 min, 30 min, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 8 hours, 24 hours.

,,
Interventionmilliseconds (Least Squares Mean)
5 min10 min20 min30 min1 hour1.5 hours2 hours3 hours4 hours8 hours24 hours
P03277 0.1 mmol/kg0.97-0.11-1.25-1.06-2.72-3.08-2.082.340.61-2.55-3.18
P03277 0.3 mmol/kg5.051.34-1.20-1.26-2.44-4.64-3.22-1.38-0.51-5.59-3.28
Placebo0.24-0.59-1.41-1.69-2.90-3.53-2.05-0.050.33-3.66-3.49

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Number of Categorical Outliers for PR

PR outliers criteria is as an increase of PR from baseline >25% resulting in PR >200 ms. (NCT03808298)
Timeframe: Up to approximately 20 weeks

InterventionParticipants (Count of Participants)
Dose Level A of Balovaptan0
Dose Level B of Balovaptan0
Placebo0

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Tmax of M2 Metabolite

(NCT03808298)
Timeframe: Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionh (Median)
Day 1Day 14
Dose Level A of Balovaptan23.926.00
Dose Level B of Balovaptan23.926.00

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Tmax of Balovaptan

(NCT03808298)
Timeframe: Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionh (Median)
Day 1Day 14
Dose Level A of Balovaptan2.501.00
Dose Level B of Balovaptan1.001.00

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Tmax M3 Metabolite

(NCT03808298)
Timeframe: Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionh (Median)
Day 1Day 14
Dose Level A of Balovaptan23.924.00
Dose Level B of Balovaptan8.004.01

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Number of Treatment Emergent Changes of T-Wave Morphology

Number (%) of participants falling into each of the T-wave categories: Normal (+), Flat, Notched (+), Biphasic, Normal (-), Notched (-). (NCT03808298)
Timeframe: Up to approximately 20 weeks

,,
InterventionParticipants (Count of Participants)
Flat T-waveNotched T-wave (+)Biphasic T-waveNormal T-wave (-)Notched T-wave (-)
Dose Level A of Balovaptan00000
Dose Level B of Balovaptan10100
Placebo10000

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Number of Categorical Outliers for QTcF

The number (percentage) of categorical outliers were participants who had increases in absolute QTcF values > 450 and ≤ 480 ms, > 480 and ≤ 500 ms, or > 500 ms. (NCT03808298)
Timeframe: Up to approximately 20 weeks

,,
InterventionParticipants (Count of Participants)
QTcF>450 and <=480 msQTcF>480 and <=500 msQTcF>500 ms
Dose Level A of Balovaptan000
Dose Level B of Balovaptan100
Placebo0000

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Number of Categorical Outliers for HR

Number (percentage) of categorical outliers were participants with a decrease in HR from pre-dose baseline > 25% to a HR < 50 bpm; and increase in HR from pre-dose baseline > 25% to a HR > 100 bpm. (NCT03808298)
Timeframe: Up to approximately 20 weeks

,,
InterventionParticipants (Count of Participants)
HR < 50 (bpm) with a decrease in ΔHR > 25%HR > 100 (bpm) with an increase in ΔHR > 25%
Dose Level A of Balovaptan00
Dose Level B of Balovaptan00
Placebo00

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Cmax of M2 Metabolite

(NCT03808298)
Timeframe: Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionng/mL (Mean)
Day 1Day 14
Dose Level A of Balovaptan5.6924.77
Dose Level B of Balovaptan42.75152.83

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Cmax of Balovaptan

(NCT03808298)
Timeframe: Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionng/mL (Mean)
Day 1Day 14
Dose Level A of Balovaptan32.589.8
Dose Level B of Balovaptan362.7613.4

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Change-From-Baseline QTcF Measured on 12 Lead ECGs Extracted From Continuous Records

(NCT03808298)
Timeframe: Baseline, Day 15. (Each treatment period is 15 days.)

,
Interventionms (Least Squares Mean)
0.5 hours Post-dose1 hours Post-dose2.5 hours Post-dose4 hours Post-dose8 hours Post-dose12 hours Post-dose24 hours Post-dose
Moxifloxacin-2.03.46.27.5-1.30.13.9
Placebo-3.2-2.0-2.3-1.1-9.9-6.8-2.2

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Change-From-Baseline QTcF at Dose Level B Measured on 12-Lead ECGs Extracted From Continuous Recordings

Change-from-baseline QTcF (ΔΔQTcF) at dose level B of balovaptan measured on 12-lead ECGs extracted from continuous recordings at the specified time points on Day 14. (NCT03808298)
Timeframe: Baseline (Predose Day 1), Day 14. (Each treatment period is 15 days.)

,
Interventionms (Least Squares Mean)
Day 14 0.75 hours Pre-doseDay 14 0.5 hours Pre-doseDay 14 0.25 hours Pre-doseDay 14 0.5 hours Post-doseDay 14 1 hours Post-doseDay 14 2.5 hours Post-doseDay 14 4 hours Post-doseDay 14 8 hours Post-doseDay 14 12 hours Post-doseDay 14 24 hours Post-dose
Dose Level B of Balovaptan-0.1-0.10.2-3.3-2.5-1.9-1.0-9.8-6.6-2.4
Placebo-0.60.1-0.1-3.9-2.3-3.5-2.1-9.6-7.5-2.9

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Change-From-Baseline QTcF at Dose Level B Measured on 12-Lead ECGs Extracted From Continuous Recordings

Change-from-baseline QTcF (ΔΔQTcF) at dose level B of balovaptan measured on 12-lead ECGs extracted from continuous recordings at the specified time points on Day 1. (NCT03808298)
Timeframe: Baseline (Predose Day 1), Day 1. (Each treatment period is 15 days.)

,
Interventionms (Least Squares Mean)
Day 1 0.5 hours Post-doseDay 1 1 hours Post-doseDay 1 2.5 hours Post-doseDay 1 4 hours Post-doseDay 1 8 hours Post-doseDay 1 12 hours Post-doseDay 1 24 hours Post-dose
Dose Level B of Balovaptan-2.3-1.8-0.21.1-8.4-5.5-1.3
Placebo-3.5-2.9-2.2-1.4-11.0-6.9-3.0

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Change-From-Baseline QRS Interval Measured on 12-Lead ECGs Extracted From Continuous Recordings

Change-from-baseline QRS interval at dose level A and dose level B of balovapton measured on 12-Lead ECGs extracted from continuous recordings on Days 1 and 14. (NCT03808298)
Timeframe: Baseline (Predose Day 1), Day 1 and Day 14. (Each treatment period is 15 days.)

,,
Interventionms (Least Squares Mean)
Day 1 0.5 hours Post-doseDay 1 1 hours Post-doseDay 1 2.5 hours Post-doseDay 1 4 hours Post-doseDay 1 8 hours Post-doseDay 1 12 hours Post-doseDay 1 24 hours Post-doseDay 14 0.75 hours Pre-doseDay 14 0.5 hours Pre-doseDay 14 0.25 hours Pre-doseDay 14 0.5 hours Post-doseDay 14 1 hours Post-doseDay 14 2.5 hours Post-doseDay 14 4 hours Post-doseDay 14 8 hours Post-doseDay 14 12 hours Post-doseDay 14 24 hours Post-dose
Dose Level A of Balovaptan-0.10.10.000.0-0.5-0.20.00.40.40.50.50.60.50.40.10.60.6
Dose Level B of Balovaptan-0.10.10.000.1-0.30.20.10.60.50.50.50.60.40.70.40.60.5
Placebo0.0-0.10.10.0-0.4-0.1-0.20.20.00.000.20.20.00.0-0.30.30.00

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Change-From-Baseline QTcF of Balovaptan at Dose Level A Measurred on 12-Lead ECGs Extracted From Continuous Recordings

Change-from-baseline QTcF (ΔΔQTcF) at dose level A of balovaptan measured on 12-lead ECGs extracted from continuous recordings at the specified time points on Days 1 and 14. (NCT03808298)
Timeframe: Baseline (Predose Day 1), Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionms (Least Squares Mean)
Day 1 0.5 hours Post-doseDay 1 1 hours Post-doseDay 1 2.5 hours Post-doseDay 1 4 hours Post-doseDay 1 8 hours Post-doseDay 1 12 hours Post-doseDay 1 24 hours Post-doseDay 14 0.75 hours Pre-doseDay 14 0.5 hours Pre-doseDay 14 0.25 hours Pre-doseDay 14 0.5 hours Post-doseDay 14 1 hours Post-doseDay 14 2.5 hours Post-doseDay 14 4 hours Post-doseDay 14 8 hours Post-doseDay 14 12 hours Post-doseDay 14 24 hours Post-dose
Dose Level A of Balovaptan-2.7-1.6-0.6-0.2-8.7-6.2-2.6-1.1-0.60.2-3.4-2.3-1.7-1.5-9.1-6.9-2.7
Placebo-3.5-2.9-2.2-1.4-11.0-6.9-3.0-0.60.1-0.1-3.9-2.3-3.5-2.1-9.6-7.5-2.9

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Change-From-Baseline PR Interval Measured on 12-Lead ECGs Extracted From Continuous Recordings

Change-from-baseline PR interval at dose level A and dose level B of balovaptan measured on 12-Lead ECGs extracted from continuous recordings on Day 1 and 14. (NCT03808298)
Timeframe: Baseline (Predose Day 1), Day 1 and Day 14. (Each treatment period is 15 days.)

,,
Interventionms (Least Squares Mean)
Day 1 0.5 hours Post-doseDay 1 1 hours Post-doseDay 1 2.5 hours Post-doseDay 1 4 hours Post-doseDay 1 8 hours Post-doseDay 1 12 hours Post-doseDay 1 24 hours Post-doseDay 14 0.75 hours Pre-doseDay 14 0.5 hours Pre-doseDay 14 0.25 hours Pre-doseDay 14 0.5 hours Post-doseDay 14 1 hours Post-doseDay 14 2.5 hours Post-doseDay 14 4 hours Post-doseDay 14 8 hours Post-doseDay 14 12 hours Post-doseDay 14 24 hours Post-dose
Dose Level A of Balovaptan-1.4-0.3-1.6-1.5-6.3-3.9-1.43.84.13.22.93.10.2-0.9-5.1-2.80.9
Dose Level B of Balovaptan-0.9-0.4-2.0-1.9-6.5-5.5-0.34.55.04.52.72.11.80.9-3.7-0.93.1
Placebo-0.2-0.3-2.0-1.2-7.4-4.2-0.33.13.83.02.92.60.7-0.2-4.3-4.21.1

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Change-From-Baseline Heart Rate Measured on 12-Lead ECGs Extracted From Continuous Recordings

Change-from-baseline heart rate at dose level A and dose level B of balovaptan measured on 12-Lead ECGs extracted from continuous recordings on Days 1 and 14. (NCT03808298)
Timeframe: Baseline (Predose Day 1), Day 1 and Day 14. (Each treatment period is 15 days.)

,,
Interventionbpm (Least Squares Mean)
Day 1 0.5 hours Post-doseDay 1 1 hours Post-doseDay 1 2.5 hours Post-doseDay 1 4 hours Post-doseDay 1 8 hours Post-doseDay 1 12 hours Post-doseDay 1 24 hours Post-doseDay 14 0.75 hours Pre-doseDay 14 0.5 hours Pre-doseDay 14 0.25 hours Pre-doseDay 14 0.5 hours Post-doseDay 14 1 hours Post-doseDay 14 2.5 hours Post-doseDay 14 4 hours Post-doseDay 14 8 hours Post-doseDay 14 12 hours Post-doseDay 14 24 hours Post-dose
Dose Level A of Balovaptan0.20.1-0.4-0.44.87.42.2-0.6-0.10.30.40.40.61.55.28.72.3
Dose Level B of Balovaptan0.50.0-0.30.34.77.90.50.90.31.01.41.11.21.85.69.21.6
Placebo0.40.20.10.15.48.12.81.61.61.82.02.02.52.96.39.83.3

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AUC0-24 of M3 Metabolite

(NCT03808298)
Timeframe: Day 1 and Day 14 (Each treatment period is 15 days.)

,
Interventionh*ng/mL (Mean)
Day 1Day 14
Dose Level A of Balovaptan131.21005.2
Dose Level B of Balovaptan1404.25456.9

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AUC0-24 of M2 Metabolite

(NCT03808298)
Timeframe: Day 1 and Day 14 (Each treatment period is 15 days.)

,
Interventionh*ng/mL (Mean)
Day 1Day 14
Dose Level A of Balovaptan90.8527.5
Dose Level B of Balovaptan766.63127.0

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AUC0-24 of Balovaptan

(NCT03808298)
Timeframe: Day 1 and Day 14 (Each treatment period is 15 days.)

,
Interventionh*ng/mL (Mean)
Day 1Day 14
Dose Level A of Balovaptan440.71127.6
Dose Level B of Balovaptan3524.86377.9

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Tmax of Moxifloxacin

(NCT03808298)
Timeframe: Days 2 (Treatment C) or 15 (Treatment D). (Each treatment period is 15 days.)

Interventionh (Median)
Treatment C2.50
Treatment D1.78

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Predicted ΔΔQTcF Interval at Geometric Mean Peak Concentrations at Tmax of M2 From Concentration-QTc Analysis

(NCT03808298)
Timeframe: Baseline, Day 14. (Each treatment period is 15 days.)

Interventionms (Geometric Mean)
Dose Level A of Balovaptan1.01
Dose Level B of Balovaptan0.27

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Predicted ΔΔQTcF Interval at Geometric Mean Peak Concentrations at Tmax of Balovaptan From Concentration-QTc Analysis

(NCT03808298)
Timeframe: Baseline, Day 14. (Each treatment period is 15 days.)

Interventionms (Geometric Mean)
Dose A of Balovaptan1.06
Dose B of Balovaptan0.70

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Predicted ΔΔQTcF Interval at Geometric Mean Peak Concentration for M3 From Concentration-QTc Analysis

(NCT03808298)
Timeframe: Baseline, Day 14. (Each treatment period is 15 days.)

Interventionms (Geometric Mean)
Dose Level A of Balovaptan1.05
Dose Level B of Balovaptan0.23

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Percentage of Participants With Treatment Emergent Adverse Events

(NCT03808298)
Timeframe: Up to approximately 20 weeks.

InterventionPercentage of Participants (Number)
Treatment Sequence A and B and Either C or D42.1

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Number of Treatment Emergent Changes of U-Wave Presence

Number (percentage) of participants with treatment emergent changes of U-wave presence. (NCT03808298)
Timeframe: Up to approximately 20 weeks

InterventionParticipants (Count of Participants)
Dose Level A of Balovaptan0
Dose Level B of Balovaptan0
Placebo0

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Cmax of Moxifloxacin

(NCT03808298)
Timeframe: Days 2 (Treatment C) or 15 (Treatment D) (Each treatment period is 15 days.)

Interventionng/mL (Mean)
Treatment C2056.9
Treatment D2058.8

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Number of Categorical Outliers for QRS

QRS outlier criteria is an increase of QRS from baseline >25% resulting in QRS >120 ms. (NCT03808298)
Timeframe: Up to approximately 20 weeks

InterventionParticipants (Count of Participants)
Dose Level A of Balovaptan0
Dose Level B of Balovaptan0
Placebo0

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Cmax of M3 Metabolite

(NCT03808298)
Timeframe: Day 1 and Day 14. (Each treatment period is 15 days.)

,
Interventionng/mL (Mean)
Day 1Day 14
Dose Level A of Balovaptan6.831005.2
Dose Level B of Balovaptan71.125456.9

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AUC0-24 of Moxifloxacin

(NCT03808298)
Timeframe: Days 2 (Treatment C) or 15 (Treatment D) (Each treatment period is 15 days.)

Interventionh*ng/mL (Mean)
Treatment C22503.9
Treatment D24103.1

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Placebo-corrected Change From Baseline for PR Interval on Day 8

Placebo-corrected change from Baseline in PR, (ΔΔPR) evaluated during the Target Dose Day of the padsevonil/moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24 hours postdose

,
Interventionmilliseconds (Least Squares Mean)
Day 8: 0.75 hour PredoseDay 8: 0.5 hour PredoseDay 8: 0.25 hour PredoseDay 8: 0.25 hour PostdoseDay 8: 0.5 hour PostdoseDay 8: 1 hour PostdoseDay 8: 1.5 hours PostdoseDay 8: 2 hours PostdoseDay 8: 3 hours PostdoseDay 8: 4 hours PostdoseDay 8: 6 hours PostdoseDay 8: 8 hours PostdoseDay 8: 12 hours PostdoseDay 8: 18 hours PostdoseDay 8: 24 hours Postdose
Moxifloxacin (QT/QTc Set)-0.6-1.0-1.2-0.4-1.6-0.8-0.8-1.3-3.1-3.3-2.3-2.3-2.9-2.1-1.9
Padsevonil (QT/QTc Set)2.41.81.22.43.13.84.23.63.64.13.32.61.6-0.2-0.6

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Placebo-corrected Change From Baseline for QRS Interval on Day 1

Placebo-corrected change from Baseline for QRS interval, (ΔΔQRS) evaluated during the Target Dose Day of the padsevonil/moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 1 : 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours postdose

Interventionmilliseconds (Least Squares Mean)
Day 1: 0.25 hour PostdoseDay 1: 0.5 hour PostdoseDay 1: 1 hour PostdoseDay 1: 1.5 hours PostdoseDay 1: 2 hours PostdoseDay1: 3 hours PostdoseDay 1: 4 hours PostdoseDay1: 6 hours PostdoseDay1: 8 hours PostdoseDay1: 12 hours PostdoseDay1: 24 hours Postdose
Padsevonil (QT/QTc Set)-0.2-0.10.0-0.2-0.3-0.3-0.2-0.1-0.30.1-0.3

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Placebo-corrected Change From Baseline for QRS Interval on Day 8

Placebo-corrected change from Baseline for QRS interval, (ΔΔQRS) evaluated during the Target Dose Day of the padsevonil/moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24 hours postdose

,
Interventionmilliseconds (Least Squares Mean)
Day 8: 0.75 hour PredoseDay 8: 0.5 hour PredoseDay 8: 0.25 hour PredoseDay 8: 0.25 hour PostdoseDay 8: 0.5 hour PostdoseDay 8: 1 hour PostdoseDay 8: 1.5 hours PostdoseDay 8: 2 hours PostdoseDay 8: 3 hours PostdoseDay 8: 4 hours PostdoseDay 8: 6 hours PostdoseDay 8: 8 hours PostdoseDay 8: 12 hours PostdoseDay 8: 18 hours PostdoseDay 8: 24 hours Postdose
Moxifloxacin (QT/QTc Set)0.00.00.2-0.1-0.10.0-0.10.10.10.0-0.10.00.5-0.10.8
Padsevonil (QT/QTc Set)-0.2-0.1-0.1-0.2-0.2-0.5-0.6-0.2-0.2-0.3-0.40.0-0.2-1.1-0.1

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Placebo-corrected Change From Baseline in Heart Rate (HR) Interval on Day 1

Placebo-corrected change from Baseline in HR, (ΔΔHR) evaluated during the Target Dose Day of the padsevonil/moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 1 : 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours postdose

Interventionbeats per minute (bpm) (Least Squares Mean)
Day 1: 0.25 hour PostdoseDay 1: 0.5 hour PostdoseDay 1: 1 hour PostdoseDay 1: 1.5 hours PostdoseDay 1: 2 hours PostdoseDay 1: 3 hours PostdoseDay 1: 4 hours PostdoseDay 1: 6 hours PostdoseDay 1: 8 hours PostdoseDay 1: 12 hours PostdoseDay 1: 24 hours Postdose
Padsevonil (QT/QTc Set)0.22.01.4-0.10.1-2.3-2.00.8-2.00.1-0.8

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Placebo-corrected Change From Baseline in Heart Rate (HR) Interval on Day 8

Placebo-corrected change from Baseline in HR, (ΔΔHR) evaluated during the Target Dose Day of the padsevonil/moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24 hours postdose

,
Interventionbeats per minute (bpm) (Least Squares Mean)
Day 8: 0.75 hour PredoseDay 8: 0.5 hour PredoseDay 8: 0.25 hour PredoseDay 8: 0.25 hour PostdoseDay 8: 0.5 hour PostdoseDay 8: 1 hour PostdoseDay 8: 1.5 hours PostdoseDay 8: 2 hours PostdoseDay 8: 3 hours PostdoseDay 8: 4 hours PostdoseDay 8: 6 hours PostdoseDay 8: 8 hours PostdoseDay 8: 12 hours PostdoseDay 8: 18 hours PostdoseDay 8: 24 hours Postdose
Moxifloxacin (QT/QTc Set)-0.40.40.5-0.40.11.91.31.0-1.8-0.40.20.20.31.30.4
Padsevonil (QT/QTc Set)-2.0-2.0-1.1-1.1-2.0-1.9-1.1-3.0-2.2-1.2-1.0-3.3-0.61.1-1.0

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Placebo-corrected Change From Baseline in QTcF After a Single Dose of Moxifloxacin on Day 8

Placebo-corrected change from Baseline in corrected QT interval (QTc), based on Fridericia's correction (QTcF) method (ΔΔQTcF) evaluated during the Target Dose Day of the moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24 hours postdose

Interventionmilliseconds (Least Squares Mean)
0.75 hour Predose0.5 hour Predose0.25 hour Predose0.25 hour Postdose0.5 hour Postdose1 hour Postdose1.5 hours Postdose2 hours Postdose3 hours Postdose4 hours Postdose6 hours Postdose8 hours Postdose12 hours Postdose18 hours Postdose24 hours Postdose
Moxifloxacin (QT/QTc Set)0.91.92.41.83.68.69.810.69.09.08.78.65.57.96.3

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Placebo-corrected Change From Baseline in QTcF on Day 8 for Padsevonil

Placebo-corrected change from Baseline in corrected QT interval (QTc), based on Fridericia's correction (QTcF) method (ΔΔQTcF) evaluated during the Target Dose Day of the padsevonil and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24 hours postdose

Interventionmilliseconds (ms) (Least Squares Mean)
0.75 hour Predose0.5 hour Predose0.25 hour Predose0.25 hour Postdose0.5 hour Postdose1 hour Postdose1.5 hours Postdose2 hours Postdose3 hours Postdose4 hours Postdose6 hours Postdose8 hours Postdose12 hours Postdose18 hours Postdose24 hours Postdose
Padsevonil (QT/QTc Set)-1.2-1.8-0.7-0.5-0.9-1.8-1.3-1.8-2.5-1.5-0.6-2.0-2.9-4.9-1.5

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Time of Observed Maximum Concentration (Tmax) at Steady State for Padsevonil

tmax: Time of observed maximum plasma concentration at steady state. (NCT04126343)
Timeframe: Day 8: 0.5 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18 hours postdose

Interventionhours (h) (Median)
Padsevonil (PKS)0.5100

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Percentage of Participants With Serious Adverse Events From Baseline to Safety Follow-up (up to Day 67)

"A Serious Adverse Event (SAE) is any untoward medical occurrence that at any dose:~Results in death~Is life-threatening~Requires in patient hospitalization or prolongation of existing hospitalization~Is a congenital anomaly or birth defect~Is infection that requires treatment parenteral antibiotics~Other important medical events which based on medical or scientific judgement may jeopardize the patients, or may require medical or surgical intervention to prevent any of the above." (NCT04126343)
Timeframe: From Baseline to Safety Follow-up (up to Day 67)

Interventionpercentage of participants (Number)
Padsevonil (SS)0
Moxifloxacin (SS)0
Placebo (SS)0

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Percentage of Participants With Adverse Events Leading to Discontinuation of the Study From Baseline to Safety Follow-up (up to Day 67)

An Adverse Event is any untoward medical occurrence in a subject or trial subject that is administered a drug or biologic (medicinal product) or that is using a medical device. The event does not necessarily have a causal relationship with that treatment or usage. The results of this Primary Outcome Measure are summarized from the Adverse Event pages of the Case Report Forms. (NCT04126343)
Timeframe: From Baseline to Safety Follow-up (up to Day 67)

Interventionpercentage of participants (Number)
Padsevonil (SS)2.0
Moxifloxacin (SS)0
Placebo (SS)0

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Percentage of Participants With Adverse Events From Baseline to Safety Follow-up (up to Day 67)

An Adverse Event is any untoward medical occurrence in a subject or trial subject that is administered a drug or biologic (medicinal product) or that is using a medical device. The event does not necessarily have a causal relationship with that treatment or usage. (NCT04126343)
Timeframe: From Baseline to Safety Follow-up (up to Day 67)

Interventionpercentage of participants (Number)
Padsevonil (SS)88.2
Moxifloxacin (SS)31.4
Placebo (SS)20.0

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Maximum Observed Plasma Concentration at Steady State (Cmax, ss) for Padsevonil

Cmax,ss: Maximum observed plasma concentration of padsevonil at steady state. (NCT04126343)
Timeframe: Day 8: 0.5 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18 hours postdose

Interventionnanogram per milliliter (ng/ml) (Geometric Mean)
Padsevonil (PKS)2119

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Change From Baseline in QTcF Evaluated at Drug-specific Tmax for Padsevonil

Change from Baseline in QTcF (ΔQTcF) evaluated at drug-specific tmax (Δtmax) for padsevonil, using an analysis of variance (ANOVA) mixed-effect model. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18 hours postdose

Interventionmilliseconds (Least Squares Mean)
Padsevonil (QT/QTc Set)-1.0

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Change From Baseline in QTcF Evaluated at Drug-Specific Tmax for Metabolite 2

Change from Baseline in QTcF (ΔQTcF) evaluated at drug-specific tmax (Δtmax) for metabolite 2, using an analysis of variance (ANOVA) mixed-effect model. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18 hours postdose

Interventionmilliseconds (Least Squares Mean)
Metabolite 2 (QT/QTc Set)-1.0

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Change From Baseline in QTcF Evaluated at Drug-specific Tmax for Metabolite 1

Change from Baseline in QTcF (ΔQTcF) evaluated at drug-specific tmax (Δtmax) for metabolite 1, using an analysis of variance (ANOVA) mixed-effect model. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18 hours postdose

Interventionmilliseconds (Least Squares Mean)
Metabolite 1 (QT/QTc Set)0.1

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Area Under the Plasma Concentration Time Curve (AUCtau) at Steady State for Padsevonil

AUCtau: Area under the plasma concentration time curve over a dosing interval at steady state. (NCT04126343)
Timeframe: Day 8: 0.5 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18 hours postdose

Interventionhour*nanogram per milliliter (h*ng/mL) (Geometric Mean)
Padsevonil (PKS)8586

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Number of Participants With Treatment-emergent Changes for T-wave Morphology and U-wave Presence

Number of Participants with treatment-emergent changes of electrocardiogram waveforms as T-waves and U-waves. If a given morphology occurs multiple times at a given time point, that occurrence was only counted 1 time for that time point. If more than 1 morphology type was observed at a given time point, both morphology types were counted. A subject can appear in more than 1 category. (NCT04126343)
Timeframe: Day 8 : 0.75, 0.5, 0.25 hours predose and 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, 18, 24 hours postdose

,,
InterventionParticipants (Count of Participants)
FlatNotched (+)BiphasicNormal (-)Notched (-)U-Wave Presence
Moxifloxacin (QT/QTc Set)000001
Padsevonil (QT/QTc Set)001000
Placebo (QT/QTc Set)000001

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Placebo-corrected Change From Baseline for PR Interval on Day 1

Placebo-corrected change from Baseline in PR, (ΔΔPR) evaluated during the Target Dose Day of the padsevonil/moxifloxacin and placebo Treatment Periods, using linear mixed-effects model analysis. (NCT04126343)
Timeframe: Day 1 : 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, 12, and 24 hours postdose

Interventionmilliseconds (Least Squares Mean)
Day 1: 0.25 hour PostdoseDay 1: 0.5 hour PostdoseDay 1: 1 hour PostdoseDay 1: 1.5 hours PostdoseDay 1: 2 hours PostdoseDay 1: 3 hours PostdoseDay 1: 4 hours PostdoseDay 1: 6 hours PostdoseDay 1: 8 hours PostdoseDay 1: 12 hours PostdoseDay 1: 24 hours Postdose
Padsevonil (QT/QTc Set)-0.40.52.21.91.92.22.62.33.51.31.3

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Change From Baseline in QRS After Each Treatment In Part 2

The QRS complex is a combination of the Q wave, R wave and S wave on an ECG tracing, and represents ventricular depolarization. Change from baseline was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QRS as covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

,,
Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Moxifloxacin 400 mg-0.2-0.10.00.10.00.10.10.2-0.3-0.70.0
Part B: Omecamtiv Mecarbil 50 mg-0.20.0-0.20.0-0.2-0.30.000.1-0.4-0.7-0.3
Part B: Placebo-0.20.0-0.10.1-0.2-0.3-0.20.0-0.6-1.1-0.1

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Change From Baseline in QRS After Omecamtiv Mecarbil Dosing in Part B

The QRS complex is a combination of the Q wave, R wave and S wave on an ECG tracing, and represents ventricular depolarization. Change from baseline was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QRS as covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg-0.20.0-0.20.0-0.2-0.30.000.1-0.4-0.7-0.3

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Change From Baseline in QTcF After Each Treatment In Part 2

Change from baseline in QTcF was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QTcF as a covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

,,
Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Moxifloxacin 400 mg-1.64.47.28.810.110.19.810.44.84.22.4
Part B: Omecamtiv Mecarbil 50 mg-6.3-9.1-8.6-8.1-5.5-5.2-4.9-3.3-7.1-6.6-4.1
Part B: Placebo-3.8-4.2-2.8-1.4-1.0-2.5-3.4-2.5-4.9-4.7-2.9

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Change From Baseline in QTcF After Omecamtiv Mecarbil Dosing in Part B

Change from baseline in QTcF was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QTcF as a covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg-6.3-9.1-8.6-8.1-5.5-5.2-4.9-3.3-7.1-6.6-4.1

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Number of Participants With Clinically Significant Abnormalities in Vital Signs, Laboratory Tests, or Electrocardiogram Findings

Blood and urine samples were collected for clinical laboratory evaluations (including clinical chemistry, hematology, urinalysis, and serology). Vital signs included blood pressure, pulse rate and body temperature. Standard safety 12-lead ECGs were recorded after the subject had been supine or semi-recumbent and at rest for at least 5 minutes to detect any immediate ECG effects for subject safety. These ECGs were viewed locally. The Investigator determined whether an abnormal value in an individual participant represented a clinically significant change from the participant's baseline values. (NCT04175808)
Timeframe: From first dose up to day 6 of each treatment period

,,,
InterventionParticipants (Count of Participants)
Clinical Laboratory EvaluationsVital Signs12-lead Electrocardiogram
Part A: Omecamtiv Mecarbil 25 mg000
Part B: Moxifloxacin 400 mg000
Part B: Omecamtiv Mecarbil 50 mg000
Part B: Placebo000

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Number of Participants With Recorded Outlier Values for QTcF, HR, PR, and QRS After Omecamtiv Mecarbil Dosing in Part B

"Outliers were predefined according to the following categories:~QTcF:~Treatment-emergent value of > 450 and ≤ 480 ms when not present at baseline (new onset) Treatment-emergent value of > 480 and ≤ 500 ms when not present at baseline (new onset) Treatment-emergent value of > 500 ms when not present at baseline (new onset) Increase of QTcF from baseline of > 30 and ≤ 60 ms Increase of QTcF from baseline > 60 ms Increase of PR from baseline > 25% resulting in PR > 200 ms Increase of QRS from baseline > 25% resulting in QRS > 120 ms Decrease of HR from baseline > 25% resulting in HR < 50 bpm Increase of HR from baseline > 25% resulting in HR > 100 bpm" (NCT04175808)
Timeframe: Day 1 of the OM treatment period at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

InterventionParticipants (Count of Participants)
QTcF > 450 and ≤ 480 ms (new onset)QTcF > 480 and ≤ 500 ms (new onset)QTcF > 500 ms (new onset)Increase in ΔQTcF > 30 and ≤ 60 msIncrease in ΔQTcF > 60 msHR < 50 bpm with a decrease in ΔHR > 25%HR > 100 bpm with an increase in ΔHR > 25%PR > 200 ms with an increase in ΔPR > 25%QRS > 120 ms with an increase in ΔQRS > 25%
Part B: Omecamtiv Mecarbil 50 mg100000000

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Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Based on the Fridericia Method (QTcF) After Omecamtiv Mecarbil Dosing in Part B

"Continuous 12-lead digital ECG recording was performed on day 1 of each period. ECGs were analyzed by a blinded, central reader. At each specified timepoint, ten 14-second 12-lead ECG tracings were extracted from the continuous recordings. The median QT in each replicate was calculated; the mean of available medians was used as the participant's reportable value at that timepoint.~QT interval was corrected for heart rate using Fridericia's correction (QTcF). Change from baseline (ΔQTcF) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QTcF as covariate.~Placebo-corrected ΔQTcF (ΔΔQTcF) was calculated as the adjusted mean ΔQTcF after OM dosing minus adjusted mean ΔQTcF after placebo.~If the upper bound of the confidence interval of ΔΔQTcF was < 10 ms for all post-dose time points, OM was to be concluded to not have a significant effect on QT interval prolongation." (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg-2.6-4.9-5.8-6.7-4.5-2.7-1.5-0.8-2.2-1.9-1.2

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Placebo-corrected Change From Baseline in QRS After Omecamtiv Mecarbil Dosing in Part B

"Change from baseline in QRS (ΔQRS) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QRS as covariate.~Placebo-corrected ΔQRS (ΔΔQRS) was calculated as the adjusted mean ΔQRS after OM dosing minus adjusted mean ΔQRS after placebo dosing." (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg-0.1-0.1-0.1-0.10.00.10.10.10.30.4-0.1

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Maximum Observed Plasma Concentration (Cmax) of Omecamtiv Mecarbil in Part B

Plasma samples at each timepoint were quantified using a validated liquid chromatography-tandem mass spectrometry method. The lower limit of quantification for plasma samples was 1 ng/mL. (NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

Interventionng/mL (Geometric Mean)
Part B: Omecamtiv Mecarbil 50 mg416

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Apparent Total Plasma Clearance (CL/F) for Omecamtiv Mecarbil in Part B

(NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

InterventionL/h (Geometric Mean)
Part B: Omecamtiv Mecarbil 50 mg10.4

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Apparent Volume of Distribution (VZ/F) for Omecamtiv Mecarbil in Part B

(NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

Interventionliters (Geometric Mean)
Part B: Omecamtiv Mecarbil 50 mg299

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Area Under the Concentration-time Curve From Time 0 to the Time of Last Quantifiable Concentration (AUC0-t) for Omecamtiv Mecarbil in Part B

(NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

Interventionh*ng/mL (Geometric Mean)
Part B: Omecamtiv Mecarbil 50 mg4710

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AUC From Time 0 to Infinity (AUCinf) for Omecamtiv Mecarbil in Part B

(NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

Interventionh*ng/mL (Geometric Mean)
Part B: Omecamtiv Mecarbil 50 mg4790

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Slope of Omecamtiv Mecarbil Plasma Concentration Estimated From Concentration-QTc Analysis in Part B

The relationship between omecamtiv mecarbil plasma concentration and ΔQTcF was investigated by linear mixed-effects modeling with ΔQTcF as the dependent variable, time-matched concentration of OM as the explanatory variable (0 for placebo), centered baseline QTcF (i.e., baseline QTcF for individual subject minus the population mean baseline QTcF for all subjects in the same period) as an additional covariate, study treatment (OM = 1 or placebo = 0) and time (i.e., post-dose time point) as fixed effects, and a random intercept and slope per subject. From the model, the slope (i.e., the regression parameter for the concentration) was estimated together with the 2-sided 90% CI. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms per ng/mL (Number)
Part B: Omecamtiv Mecarbil 50 mg-0.011

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Time to Maximum Observed Plasma Concentration (Tmax) of Omecamtiv Mecarbil In Part B

(NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

Interventionhours (Median)
Part B: Omecamtiv Mecarbil 50 mg0.583

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Change From Baseline in Heart Rate After Each Treatment In Part 2

Change from baseline in heart rate (HR) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline HR as a covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

,,
Interventionbpm (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Moxifloxacin 400 mg2.14.05.35.42.02.03.02.99.19.63.4
Part B: Omecamtiv Mecarbil 50 mg1.31.21.40.2-0.5-0.21.11.87.88.32.8
Part B: Placebo2.12.62.12.51.41.42.01.38.09.34.5

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Change From Baseline in Heart Rate After Omecamtiv Mecarbil Dosing in Part B

Change from baseline in heart rate (HR) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline HR as a covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionbpm (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg1.31.21.40.2-0.5-0.21.11.87.88.32.8

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Change From Baseline in PR Interval After Each Treatment In Part 2

The PR interval is the time from the onset of the P-wave to the start of the next QRS complex. Change from baseline was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline PR interval as covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

,,
Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Moxifloxacin 400 mg-1.6-0.6-1.1-1.5-2.1-1.6-3.3-4.5-7.7-7.5-2.6
Part B: Omecamtiv Mecarbil 50 mg-0.51.00.40.4-1.2-0.8-2.0-3.2-7.5-7.8-2.1
Part B: Placebo-1.20.10.7-0.6-1.3-2.6-2.5-3.3-5.8-6.8-2.1

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Apparent Terminal Elimination Half-life (T1/2) of Omecamtiv Mecarbil in Part B

(NCT04175808)
Timeframe: Day 1 of the OM treatment period at pre-dose and 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, 24, 48, 72, 96, and 120 hours post-dose.

Interventionhours (Geometric Mean)
Part B: Omecamtiv Mecarbil 50 mg20.0

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Change From Baseline in PR Interval After Omecamtiv Mecarbil Dosing in Part B

The PR interval is the time from the onset of the P-wave to the start of the next QRS complex. Change from baseline was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline PR interval as covariate. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg-0.51.00.40.4-1.2-0.8-2.0-3.2-7.5-7.8-2.1

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Number of Participants With Treatment-emergent Adverse Events (TEAEs)

"A TEAE was defined as an adverse event (AE) that started during or after the first dose, or started prior to the first dose and increased in severity after the first dose. A treatment-related TEAE was defined as a TEAE with a relationship of related to the study treatment as determined by the investigator.~The Investigator assessed the severity of each AE reported during the study based on the following grading scale:~Mild: Aware of sign or symptom, easily tolerated Moderate: Discomfort enough to cause interference with usual activity Severe: Incapacitating, inability to work or do usual activity~SAEs were defined as any untoward medical occurrence that met at least 1 of the following serious criteria:~Resulted in Death~Was life-threatening~Required in-patient hospitalization or prolongation of existing hospitalization~Resulted in persistent or significant disability/incapacity~Was a congenital anomaly/birth defect~Other medically important serious event" (NCT04175808)
Timeframe: From first dose of study treatment to day 6 of each treatment period

,,,
InterventionParticipants (Count of Participants)
Any TEAESerious TEAETEAE leading to discontinuationTEAE leading to deathMild TEAEModerate TEAESevere TEAETreatment-related TEAETreatment-related serious TEAETreatment-related TEAE leading to discontinuationTreatment-related TEAE leading to deathTreatment-related mild TEAETreatment-related moderate TEAETreatment-related severe TEAE
Part A: Omecamtiv Mecarbil 25 mg2000019202000200
Part B: Moxifloxacin 400 mg2900028202000200
Part B: Omecamtiv Mecarbil 50 mg2400024104000400
Part B: Placebo2600025100000000

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Number of Participants With Treatment-emergent Changes in T-wave Morphology and U-wave Presence After Omecamtiv Mecarbil Dosing in Part B

"T-wave abnormalities were categorized as follows:~Flat T-wave: T amplitude < 1 mm (either positive or negative) including flat isoelectric line Notched T-wave (+): Presence of notch(es) of at least 0.05 mV amplitude on ascending or descending arm of the positive T-wave Biphasic: T-wave that contains a second component with an opposite phase that is at least 0.1 mV deep (both positive/negative and negative/positive and polyphasic T-waves included) Normal T-wave (-): T amplitude that is negative, without biphasic T-wave or notches Notched T-wave (-): Presence of notch(es) of at least 0.05 mV amplitude on descending or ascending arm of the negative T-wave U waves: Presence of abnormal U-waves" (NCT04175808)
Timeframe: Day 1 of the OM treatment period at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

InterventionParticipants (Count of Participants)
Flat T-waveNotched T-wave (+)Biphasic T-waveNormal T-wave (-)Notched T-wave (-)U-Wave presence
Part B: Omecamtiv Mecarbil 50 mg000000

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Placebo-corrected Change From Baseline in Heart Rate After Omecamtiv Mecarbil Dosing in Part B

"Change from baseline in heart rate (ΔHR) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline HR as covariate.~Placebo-corrected ΔHR (ΔΔHR) was calculated as the adjusted mean ΔHR after OM dosing minus adjusted mean ΔHR after placebo dosing." (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionbpm (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg-0.9-1.3-0.6-2.3-1.9-1.5-0.90.5-0.1-1.0-1.7

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Placebo-corrected Change From Baseline in PR Interval After Omecamtiv Mecarbil Dosing in Part B

"Change from baseline in PR interval (ΔPR) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline PR interval as covariate.~Placebo-corrected ΔPR (ΔΔPR) was calculated as the adjusted mean ΔPR after OM dosing minus adjusted mean ΔPR after placebo dosing." (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the OM treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Omecamtiv Mecarbil 50 mg0.60.9-0.31.00.11.90.40.1-1.6-1.0-0.1

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Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Based on the Fridericia Method (QTcF) After Moxifloxacin Dosing in Part B

"Assay sensitivity was validated by analysis of ∆QTcF of moxifloxacin. Continuous 12-lead digital ECG recording was performed on Day 1 of each period. ECGs were analyzed by a blinded, central reader. At each specified timepoint, ten 14-second 12-lead ECG tracings were extracted from the continuous recordings. The median QT in each replicate was calculated; the mean of available medians was used as the participant's reportable value at that timepoint.~QT interval was corrected for heart rate using Fridericia's correction (QTcF). Change from baseline (ΔQTcF) was calculated based on a linear mixed-effects model with period, sequence, time (categorical), treatment, and time-by-treatment interaction as fixed effects and baseline QTcF as covariate.~Placebo-corrected ΔQTcF (ΔΔQTcF) was calculated as the adjusted mean ΔQTcF after moxifloxacin dosing minus adjusted mean ΔQTcF after placebo.~If ∆∆QTcF was larger than 5 ms at 2, 3, or 4 hours, assay sensitivity was considered to be demonstrated. (NCT04175808)
Timeframe: Baseline (average of samples taken at -1.25, -1, and -0.75 hours predose on day 1 of the moxifloxacin treatment period) and at 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 8, 12, and 24 hours post-dose.

Interventionms (Least Squares Mean)
0.25 hours post-dose0.5 hours post-dose0.75 hours post-dose1 hour post-dose1.5 hours post-dose2 hours post-dose3 hours post-dose4 hours post-dose8 hours post-dose12 hours post-dose24 hours post-dose
Part B: Moxifloxacin 400 mg2.28.610.110.211.112.713.112.99.79.05.3

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ALXN1840 PK Parameter: Area Under The Concentration Versus Time Curve From Time 0 To The Last Quantifiable Concentration (AUC0-t) Of Total Molybdenum And Plasma Ultrafiltrate (PUF) Molybdenum Following a Single Oral Dose of ALXN1840

Blood samples for PK analysis of total molybdenum and PUF molybdenum were collected as close as possible to nominal time after completion of the ECG extraction period. (NCT04560816)
Timeframe: Predose (0) to 96 hours post-dose

Interventionh*ng/mL (Geometric Mean)
Total MolybdenumPlasma Ultrafiltrate Molybdenum
ALXN1840184501763

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ALXN1840 PK Parameter: Maximum Observed Concentration (Cmax) Of Total Molybdenum And PUF Molybdenum Following a Single Oral Dose of ALXN1840

Blood samples for PK analysis of total molybdenum and PUF molybdenum were collected as close as possible to nominal time after completion of the ECG extraction period. (NCT04560816)
Timeframe: Predose (0) to 96 hours post-dose

Interventionng/mL (Geometric Mean)
Total MolybdenumPlasma Ultrafiltrate Molybdenum
ALXN1840504.1127.9

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ALXN1840 PK Parameter: Time To Maximum Observed Concentration (Tmax) Of Total Molybdenum And PUF Molybdenum Following a Single Oral Dose of ALXN1840

Blood samples for PK analysis of total molybdenum and PUF molybdenum were collected as close as possible to nominal time after completion of the ECG extraction period. (NCT04560816)
Timeframe: Pre-dose to 96 hours post-dose

Interventionhours (Median)
Total MolybdenumPlasma Ultrafiltrate Molybdenum
ALXN18405.006.00

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Change From Baseline For Heart Rate (ΔHR)

Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,,
Interventionbpm (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-0.27-0.02-0.120.410.515.857.075.594.697.715.762.32
Moxifloxacin1.273.871.972.142.305.827.436.615.379.156.932.92
Placebo0.500.380.19-1.170.244.836.954.323.977.445.181.60

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Change From Baseline PR Interval (ΔPR)

Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,,
Interventionms (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-0.130.411.300.46-0.75-1.72-3.64-5.76-4.52-3.94-2.89-0.13
Moxifloxacin-1.33-1.37-0.77-2.66-3.38-4.22-5.52-7.16-7.07-6.61-4.60-1.68
Placebo1.261.661.541.32-0.10-1.12-3.43-4.05-3.83-3.34-2.980.69

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Change From Baseline QRS Interval (ΔQRS)

Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,,
Interventionms (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-0.010.040.080.100.14-0.23-1.01-0.89-0.66-0.89-0.42-0.14
Moxifloxacin-0.080.06-0.10-0.190.01-0.35-1.13-1.16-0.48-0.87-0.50-0.18
Placebo-0.07-0.04-0.09-0.050.16-0.28-0.73-1.08-0.39-0.71-0.300.02

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Change From Baseline QT Interval Using Fridericia's Formula (ΔQTcF)

Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,,
Interventionms (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-2.56-0.49-0.69-1.04-1.06-0.64-6.05-7.60-7.66-4.96-5.050.52
Moxifloxacin2.299.4710.2810.9610.039.544.002.051.491.700.943.48
Placebo-2.36-0.19-0.76-0.410.02-0.55-5.35-7.85-6.73-5.73-5.10-1.78

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Number of Participants With Treatment-Emergent Adverse Events (TEAEs)

An adverse event (AE) was any untoward medical occurrence in a participant, temporally associated with the use of study intervention, whether or not considered related to the study intervention. TEAE was an AE that started during or after the first dose, or started prior to the first dose and increased in severity after the first dose. A related TEAE was defined as having a reasonable possibility the study intervention caused the AE as assessed by the investigator. Serious AEs were defined as any untoward medical occurrence that met at least 1 of the following serious criteria: resulted in death, was life-threatening, required in-patient hospitalization or prolongation of existing hospitalization, resulted in persistent or significant disability/incapacity, was a congenital anomaly/birth defect, other medically important serious event. (NCT04560816)
Timeframe: Day 1 (after dosing) through Day 70

,,
InterventionParticipants (Count of Participants)
Any TEAEAny serious TEAE (SAE)Any TEAE leading to deathAny related TEAE
ALXN18409004
Moxifloxacin6003
Placebo3000

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Number of Participants With Treatment-emergent T-wave Morphology Abnormalities and U-waves

Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. (NCT04560816)
Timeframe: Day 1 (after dosing) through 24 hours postdose

,,
InterventionParticipants (Count of Participants)
At least one treatment-emergent T-wave abnormalityAt least one treatment-emergent U-wave
ALXN184000
Moxifloxacin10
Placebo00

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Placebo-corrected Change From Baseline For QTcF (ΔΔQTcF) for ALXN1840 Using The By-time Point Analysis

"Twelve-lead electrocardiograms (ECGs) were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. Change from baseline in the QT interval was corrected for heart rate using Fridericia's formula (ΔQTcF). ΔQTcF was based on a mixed-effects model for repeated measures (MMRM) with ΔQTcF as the dependent variable; period, sequence, time, treatment, and time-by-treatment interaction as fixed effects; and baseline QTc and sex as covariates.~ΔΔQTc = LS mean ΔQTcF after ALXN1840 dosing minus LS mean ΔQTcF after placebo. If the upper bound of the confidence interval (CI) of ΔΔQTcF was < 10 ms for all postdose time points, ALXN1840 was concluded to not have a significant effect on QT interval prolongation." (NCT04560816)
Timeframe: Baseline (average of samples taken at -45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

Interventionms (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-0.21-0.310.07-0.64-1.08-0.90-0.710.25-0.930.760.052.30

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Placebo-corrected Change From Baseline Heart Rate (ΔΔHR)

"Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period.~Least square mean difference and its 90% CI were calculated based on MMRM with fixed effects for period, sequence, timepoint, treatment, time-by-treatment interaction as fixed effect and baseline value and sex as covariates." (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,
Interventionbpm (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-0.77-0.40-0.311.580.271.020.131.270.720.270.580.73
Moxifloxacin0.773.501.783.312.060.990.482.291.401.711.751.32

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Placebo-corrected Change From Baseline PR Interval (ΔΔPR)

Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period. (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,
Interventionms (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN1840-1.39-1.25-0.24-0.87-0.65-0.60-0.21-1.71-0.69-0.610.09-0.82
Moxifloxacin-2.60-3.03-2.31-3.99-3.28-3.11-2.09-3.10-3.24-3.28-1.62-2.37

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Placebo-corrected Change From Baseline QRS Interval (ΔΔQRS)

"Twelve-lead ECGs were extracted from approximately 25-hour continuous (Holter) recordings on Day -1 of Treatment Period 1 and Days 1 and 2 in each treatment period.~Least square mean difference and its 90% CI were calculated based on MMRM with fixed effects for period, sequence, timepoint, treatment, time-by-treatment interaction as fixed effect and baseline value and sex as covariates." (NCT04560816)
Timeframe: Baseline (average of samples taken at 45, -30, and -15 minutes before dosing), 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 10, 12, and 24 (Day 2) hours postdose

,
Interventionms (Least Squares Mean)
Day 1, 0.5 hours postdoseDay 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdoseDay 1, 4 hours postdoseDay 1, 5 hours postdoseDay 1, 6 hours postdoseDay 1, 7 hours postdoseDay 1, 8 hours postdoseDay 1, 10 hours postdoseDay 1, 12 hours postdoseDay 2, 24 hours postdose
ALXN18400.070.080.170.15-0.020.05-0.270.19-0.27-0.18-0.12-0.16
Moxifloxacin-0.010.10-0.01-0.13-0.15-0.07-0.40-0.08-0.10-0.15-0.20-0.20

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ΔΔQTcF For Moxifloxacin Using The By-time Point Analysis

"Assay sensitivity was evaluated using the by-time point analysis of the effect on ΔΔQTc of moxifloxacin.~If ΔΔQTcF was larger than 5 ms at 1, 2, and 3 hours postdose, assay sensitivity was considered to be demonstrated." (NCT04560816)
Timeframe: 1, 2, and 3 hours postdose at Day 1

Interventionms (Least Squares Mean)
Day 1, 1 hour postdoseDay 1, 2 hours postdoseDay 1, 3 hours postdose
Moxifloxacin9.6511.0411.37

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Part 1: Area Under the Plasma Concentration-time Curve From Time Zero to Time t (AUC[0-t]) of GSK3640254

Blood samples were collected at indicated time points. Pharmacokinetic (PK) analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hours, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 12 Hours, 24 Hours, 48 Hours post-dose on Day 7

InterventionHours*nanograms per milliliter (Geometric Mean)
Part 1: GSK3640254 500 mg102400

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Part 1: Change From Baseline in Chemistry Parameters: Albumin, Globulin, and Total Protein

Blood samples were collected at indicated timepoints to analyze albumin, globulin, and total protein. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionGrams per liter (Mean)
Albumin, Day 3Albumin, Day 7Albumin, Day 9Globulin, Day 3Globulin, Day 7Globulin, Day 9Total protein, Day 3Total protein, Day 7Total Bilirubin, Day 9
Part 1 : GSK3640254 500 mg-1.21.30.22.22.32.01.03.72.2
Part 1 : Placebo-0.51.0-1.0-0.5-1.5-1.0-1.0-0.5-2.0

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Part 1: Absolute Values for Vital Parameters: Systolic Blood Pressure (SBP) and Diastolic Blood Pressure (DBP)

SBP and DBP were measured in the semi-recumbent or supine position with a completely automated device after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8 and Day 9

,
InterventionMillimeters (mm) of mercury (Mean)
SBP, Baseline (Pre-dose, Day 1)SBP, Day 2SBP, Day 3SBP, Day 4SBP, Day 5SBP, Day 6SBP, Day 7SBP, Day 8SBP, Day 9DBP, Baseline (Pre-dose, Day 1)DBP, Day 2DBP, Day 3DBP, Day 4DBP, Day 5DBP, Day 6DBP, Day 7DBP, Day 8DBP, Day 9
Part 1 : GSK3640254 500 mg109.2103.8106.8107.5105.3107.0107.7109.0109.861.559.859.764.062.361.263.764.564.7
Part 1 : Placebo120.0115.5123.0121.5111.5114.0117.5125.0127.074.070.576.066.069.565.572.067.069.5

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Part 1: Absolute Values for Vital Parameter: Temperature

Temperature was measured in the semi-recumbent or supine position with a completely automated device after at least 5 minutes of rest for the participant in a quiet setting without distractions.Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8 and Day 9

,
InterventionDegrees Celsius (Mean)
Baseline (Pre-dose, Day 1)Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9
Part 1 : GSK3640254 500 mg36.5036.5336.5836.5236.5836.4736.4736.6336.47
Part 1 : Placebo35.9036.1036.1036.1536.3536.4535.9536.3536.35

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Part 1: Absolute Values for Vital Parameter: Pulse Rate

Pulse rate was measured in the semi-recumbent or supine position with a completely automated device after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8 and Day 9

,
InterventionBeats per minute (bpm) (Mean)
Baseline (Pre-dose, Day 1 )Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9
Part 1 : GSK3640254 500 mg67.868.765.068.872.567.270.581.367.8
Part 1 : Placebo70.563.070.571.067.066.570.070.073.0

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Part 1: Absolute Values for Urinalysis Parameter: Specific Gravity

Urine samples were collected at indicated time points to analyze the urine specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionRatio (Mean)
Baseline (Day -2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg1.00921.01251.01671.0097
Part 1 : Placebo1.00801.01501.01901.0145

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Part 2: Change From Baseline in Urinalysis Parameter: Specific Gravity

Urine samples were collected at indicated time points to analyze the urine specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionRatio (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg0.0019-0.00110.0005
Part 2: GSK3640254 500 mg0.0026-0.00200.0016
Part 2: Moxifloxacin 400 mg0.00300.00150.0037
Part 2: Placebo0.00340.00150.0022

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Part 2: Change From Baseline in Urinalysis Parameter: pH

Urine samples were collected at indicated time points to analyze the urine pH by dipstick test. The dipstick test gives results in a semi-quantitative manner indicating proportional concentrations in the urine sample. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acidic pH (5.0 - 6.0). Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionpH (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg-0.08-0.110.06
Part 2: GSK3640254 500 mg-0.180.30-0.09
Part 2: Moxifloxacin 400 mg-0.33-0.23-0.21
Part 2: Placebo-0.19-0.35-0.13

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Part 2: Change From Baseline in QTcF - For Placebo and Moxifloxacin Arm

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits.Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,
InterventionMilliseconds (Least Squares Mean)
Day 7, PredoseDay7, 0.5 Hour Post-doseDay 7, 1 Hour Post-doseDay 7, 2 Hour Post-doseDay 7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: Moxifloxacin 400 mg3.3-2.1-1.11.73.64.55.65.96.95.3-0.82.63.36.2
Part 2: Placebo2.7-1.9-0.3-3.9-4.3-4.4-3.0-2.6-1.3-2.9-7.7-4.2-2.0-0.6

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Part 2: Change From Baseline in QT Interval Corrected for Heart Rate Using Fridericia's Formula (QTcF) - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms

Twelve-lead ECGs were recorded in participant using automated ECG machine & performed with participant in supine position after a rest of at least 10 minutes.Baseline was defined as the latest pre-dose assessment with a non-missing value for each visit. Change from Baseline in QT interval corrected for heart rate using Fridericia's formula (QTcF) was calculated by subtracting Baseline value from post dose value. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,,
InterventionMilliseconds (Least Squares Mean)
Day 7, PredoseDay7, 0.5 Hour Post-doseDay 7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay 7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg4.2-0.90.4-2.2-2.8-2.9-2.0-1.5-1.1-1.2-8.5-4.0-1.5-0.5
Part 2: GSK3640254 500 mg9.85.33.82.63.74.85.68.08.35.70.44.44.07.1
Part 2: Placebo2.7-1.9-0.3-3.9-4.3-4.4-3.0-2.6-1.3-2.9-7.7-4.2-2.0-0.6

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Part 1: Absolute Values for Urinalysis Parameter: Potential of Hydrogen (pH)

Urine samples were collected at indicated time points to analyze the urine pH by dipstick test. The dipstick test gives results in a semi-quantitative manner indicating proportional concentrations in the urine sample. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acidic pH (5.0 - 6.0). Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionpH (Mean)
Baseline (Day -2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg7.086.336.256.25
Part 1 : Placebo6.506.506.256.50

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Part 1: Absolute Values for Hematology Parameter: Hemoglobin

Blood samples were collected at indicated time points to analyze hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionGrams per liter (Mean)
Baseline (Day -2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg131.8137.3140.5137.7
Part 1 : Placebo143.5149.5151.5152.0

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Part 1: Absolute Values for Hematology Parameter: Hematocrit

Blood samples were collected at indicated time points to analyze hematocrit. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionProportion of red blood cells in blood (Mean)
Baseline (Day -2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg0.39200.40480.41400.4062
Part 1 : Placebo0.41550.43650.44050.4465

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Part 1: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Volume

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular volume. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionFemtoliter (Median)
Baseline (Day -2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg84.4283.9584.0583.67
Part 1 : Placebo87.7087.3087.3088.20

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Part 1: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionPicograms (Mean)
Baseline (Day-2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg28.3528.4328.5028.33
Part 1 : Placebo30.3529.8530.0030.00

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Part 1: Absolute Values for Hematology Parameter: Erythrocytes

Blood samples were collected at indicated time points to analyze erythrocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
Intervention10^12 cells per liter (Mean)
Baseline (Day -2)Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg4.6474.8204.9154.852
Part 1 : Placebo4.7405.0105.0605.065

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Part 1: Absolute Values for Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes

Blood samples were collected at indicated time points to analyze basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelets and leukocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. . (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
Intervention10^9 cells per liter (Mean)
Basophils, Baseline (Day -2)Basophils, Day 3Basophils, Day 7Basophils, Day 9Eosinophils, Baseline (Day -2)Eosinophils, Day 3Eosinophils, Day 7Eosinophils, Day 9Lymphocytes, Baseline (Day -2)Lymphocytes, Day 3Lymphocytes, Day 7Lymphocytes, Day 9Monocytes, Baseline (Day -2)Monocytes, Day 3Monocytes, Day 7Monocytes, Day 9Neutrophils, Baseline (Day -2)Neutrophils, Day 3Neutrophils, Day 7Neutrophils, Day 9Platelets, Baseline (Day -2)Platelets, Day 3Platelets, Day 7Platelets, Day 9Leukocytes, Baseline (Day -2)Leukocytes, Day 3Leukocytes, Day 7Leukocytes, Day 9
Part 1 : GSK3640254 500 mg0.0570.0530.0480.0650.1370.1150.1020.0971.8221.6571.6681.9350.5370.4620.4900.5083.9103.0153.2783.168266.5264.2280.0269.86.475.305.585.75
Part 1 : Placebo0.0700.0650.0650.0600.3750.3500.3450.3302.5202.7152.5152.1000.5500.5700.5250.4904.0104.3004.2055.215228.0233.0243.5239.07.358.007.658.15

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Part 1: Absolute Values for Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, and Blood Urea Nitrogen

Blood samples were collected at indicated time points to analyze glucose, cholesterol, magnesium, triglycerides, anion gap, calcium, carbon dioxide, chloride, phosphate, potassium, sodium, and blood urea nitrogen. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionMillimoles per liter (Mean)
Glucose, Baseline (Day -2)Glucose, Day 3Glucose, Day 7Glucose, Day 9Cholesterol, Baseline (Day-2)Cholesterol, Day 3Cholesterol, Day 7Cholesterol, Day 9Magnesium, Baseline (Day -2)Magnesium, Day 3Magnesium, Day 7Magnesium, Day 9Triglycerides, Baseline (Day -2)Triglycerides, Day 3Triglycerides, Day 7Triglycerides, Day 9Anion gap, Baseline (Day-2)Anion gap, Day 3Anion gap, Day 7Anion gap, Day 9Calcium, Baseline (Day -2)Calcium, Day 3Calcium, Day 7Calcium, Day 9Carbon dioxide, Baseline (Day -2)Carbon dioxide, Day 3Carbon dioxide, Day 7Carbon dioxide, Day 9Chloride, Baseline (Day -2)Chloride, Day 3Chloride, Day 7Chloride, Day 9Phosphate, Baseline (Day -2)Phosphate, Day 3Phosphate, Day 7Phosphate, Day 9Potassium, Baseline (Day -2)Potassium, Day 3Potassium, Day 7Potassium, Day 9Sodium, Baseline (Day -2)Sodium, Day 3Sodium, Day 7Sodium, Day 9Blood Urea Nitrogen, Baseline (Day -2)Blood Urea Nitrogen, Day 3Blood Urea Nitrogen, Day 7Blood Urea Nitrogen, Day 9
Part 1 : GSK3640254 500 mg4.6824.7454.7284.6054.1124.3704.4134.2050.7670.7870.7870.8130.7630.8570.6580.61510.39.510.310.72.3322.3702.4082.33728.728.729.229.3103.7102.7102.2103.21.1421.2381.2231.2124.104.284.224.20138.5136.5137.7139.04.4824.6484.6904.332
Part 1 : Placebo5.0504.4954.4654.6355.0255.3905.1805.0000.7600.8000.8000.8001.2951.2051.0050.96512.511.510.011.02.4402.4302.4402.39029.030.030.530.0101.0100.5101.5102.51.1951.2101.1951.1304.054.004.354.05138.5138.0138.0139.54.3004.6255.2304.715

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Part 1: Absolute Values for Chemistry Parameters: Creatinine, Urate, Total Bilirubin, and Direct Bilirubin

Blood samples were collected at indicated timepoints to analyze creatinine, urate, total bilirubin, and direct bilirubin. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, Day 9

,
InterventionMicromoles per liter (Mean)
Creatinine, Baseline (Day -2)Creatinine, Day 3Creatinine, Day 7Creatinine, Day 9Urate, Baseline (Day -2)Urate, Day 3Urate, Day 7Urate, Day 9Total Bilirubin, Baseline (Day -2)Total Bilirubin, Day 3Total Bilirubin, Day 7Total Bilirubin, Day 9Direct Bilirubin, Baseline (Day -2)Direct Bilirubin, Day 3Direct Bilirubin, Day 7Direct Bilirubin, Day 9
Part 1 : GSK3640254 500 mg74.8572.2070.1371.00274.5259.0246.0257.07.009.6311.3310.201.421.682.102.05
Part 1 : Placebo89.7583.1086.6085.30363.0351.0365.5348.05.608.558.757.800.951.451.601.55

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Part 1: Absolute Values for Chemistry Parameters: Amylase and Lipase

Blood samples were collected at indicated timepoints to analyze amylase and lipase. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionUnits per liter (Mean)
Amylase, Baseline (Day -2)Amylase, Day 3Amylase, Day 7Amylase, Day 9Lipase, Baseline (Day -2)Lipase, Day 3Lipase, Day 7Lipase, Day 9
Part 1 : GSK3640254 500 mg63.861.862.859.535.530.232.329.3
Part 1 : Placebo64.564.067.064.533.518.519.518.5

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Part 2: Change From Baseline in QRS Interval - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits.Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7 : Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,,
InterventionMilliseconds (Least Squares Mean)
Day 7, PredoseDay7, 0.5 Hour Post-doseDay 7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay 7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg0.50.70.50.40.60.60.91.11.31.30.51.10.80.4
Part 2: GSK3640254 500 mg1.01.10.80.60.50.91.11.31.51.30.91.20.70.9
Part 2: Placebo0.40.50.1-0.10.10.30.60.91.01.20.20.60.2-0.5

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Part 2: Change From Baseline in PR Interval - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,,
InterventionMilliseconds (Least Squares Mean)
Day 7, PredoseDay7, 0.5 Hour Post-doseDay 7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay 7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg2.53.60.7-3.6-4.3-3.9-3.4-4.7-3.9-3.8-5.6-3.9-3.0-0.5
Part 2: GSK3640254 500 mg3.15.7-0.3-1.2-2.6-1.5-2.9-4.3-3.7-3.9-4.1-3.9-1.8-0.9
Part 2: Placebo1.13.2-0.4-2.8-4.7-4.7-4.6-5.3-3.9-4.1-5.3-5.0-3.60.9

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Part 2: Change From Baseline in Hematology Parameter: Hemoglobin

Blood samples were collected at indicated time points to analyze hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionGrams per liter (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg-0.91.00.8
Part 2: GSK3640254 500 mg0.30.0-0.9
Part 2: Moxifloxacin 400 mg0.1-1.3-0.2
Part 2: Placebo-2.7-0.6-1.9

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Part 2: Change From Baseline in Hematology Parameter: Hematocrit

Blood samples were collected at indicated time points to analyze hematocrit . Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionProportion of red blood cells in blood (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg-0.00180.00360.0035
Part 2: GSK3640254 500 mg-0.0040-0.0007-0.0026
Part 2: Moxifloxacin 400 mg0.0002-0.0076-0.0012
Part 2: Placebo-0.0068-0.0009-0.0052

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Part 2: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular volume. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionFemtoliter (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg-0.45-0.01-0.69
Part 2: GSK3640254 500 mg-0.55-0.20-0.02
Part 2: Moxifloxacin 400 mg-0.260.100.35
Part 2: Placebo-0.570.15-0.33

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Part 2: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionPicograms (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg-0.18-0.06-0.28
Part 2: GSK3640254 500 mg0.150.01-0.01
Part 2: Moxifloxacin 400 mg-0.080.270.19
Part 2: Placebo-0.25-0.05-0.15

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Part 2: Change From Baseline in Hematology Parameter: Erythrocytes

Blood samples were collected at indicated time points to analyze erythrocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
Intervention10^12 cells per liter (Mean)
Day 8Day 9Day 14
Part 2: GSK3640254 100 mg0.0080.0440.081
Part 2: GSK3640254 500 mg-0.0150.004-0.031
Part 2: Moxifloxacin 400 mg0.022-0.090-0.031
Part 2: Placebo-0.049-0.023-0.043

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Part 2: Change From Baseline in Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes

Blood samples were collected at indicated time points to analyze basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelets and leukocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
Intervention10^9 cells per liter (Mean)
Basophils,Day 8Basophils,Day 9Basophils,Day 14Eosinophils,Day 8Eosinophils,Day 9Eosinophils,Day 14Lymphocytes,Day 8Lymphocytes,Day 9Lymphocytes,Day 14Monocytes,Day 8Monocytes,Day 9Monocytes,Day 14Neutrophils,Day 8Neutrophils,Day 9Neutrophils,Day 14Platelets, Day 8Platelets, Day 9Platelets, Day 14Leukocytes,Day 8Leukocytes,Day 9Leukocytes,Day 14
Part 2: GSK3640254 100 mg-0.004-0.010-0.001-0.008-0.011-0.012-0.071-0.067-0.041-0.0150.010-0.040-0.3190.306-0.386-2.20.7-2.5-0.410.20-0.47
Part 2: GSK3640254 500 mg0.0050.0020.007-0.001-0.0020.006-0.0390.0150.0140.0340.038-0.022-0.0220.136-0.262-4.57.9-6.7-0.010.21-0.24
Part 2: Moxifloxacin 400 mg-0.003-0.003-0.0040.007-0.0040.002-0.161-0.092-0.1600.014-0.030-0.022-0.272-0.174-0.437-10.8-3.5-10.1-0.42-0.32-0.63
Part 2: Placebo-0.0020.002-0.0050.0020.008-0.004-0.1290.122-0.0660.0010.047-0.0150.0180.332-0.155-7.4-8.4-3.2-0.110.50-0.24

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Part 2: Change From Baseline in Heart Rate (HR) - For GSK3640254 100 mg, GSK3640254 500 mg and Placebo Arms

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits.Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7 : Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,,
InterventionBeats per minute (Least Squares Mean)
Day 7, PredoseDay7, 0.5 Hour Post-doseDay 7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay 7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg0.04.45.45.94.14.53.75.45.09.67.32.68.52.0
Part 2: GSK3640254 500 mg2.88.59.17.05.66.05.96.97.512.710.57.09.23.3
Part 2: Placebo0.34.65.24.52.72.82.63.73.48.66.31.98.1-0.6

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Part 2: Change From Baseline in Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, Blood Urea Nitrogen

Blood samples were collected at indicated time points to analyze glucose, cholesterol, magnesium, triglycerides, anion gap, calcium, carbon dioxide, chloride, phosphate, potassium, sodium, and blood urea nitrogen.Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionMillimoles per liter (Mean)
Glucose, Day 8Glucose, Day 9Glucose, Day 14Cholesterol, Day 8Cholesterol, Day 9Cholesterol, Day 14Magnesium, Day 8Magnesium, Day 9Magnesium, Day 14Triglycerides, Day 8Triglycerides, Day 9Triglycerides, Day 14Anion gap, Day 8Anion gap, Day 9Anion gap, Day 14Calcium, Day 8Calcium, Day 9Calcium, Day 14Carbon dioxide, Day 8Carbon dioxide, Day 9Carbon dioxide, Day 14Chloride, Day 8Chloride, Day 9Chloride, Day 14Phosphate, Day 8Phosphate, Day 9Phosphate, Day 14Potassium, Day 8Potassium, Day 9Potassium, Day 14Sodium, Day 8Sodium, Day 9Sodium, Day 14Blood Urea Nitrogen, Day 8Blood Urea Nitrogen, Day 9Blood Urea Nitrogen, Day 14
Part 2: GSK3640254 100 mg-0.0230.040-0.109-0.0540.0810.032-0.011-0.0130.008-0.002-0.1530.0310.01.20.1-0.0340.0500.042-1.2-0.80.1-0.2-1.00.50.018-0.0160.054-0.12-0.030.12-0.9-0.40.80.3850.1540.008
Part 2: GSK3640254 500 mg-0.024-0.1390.046-0.201-0.186-0.2730.0050.0090.003-0.100-0.1510.035-0.40.4-0.8-0.063-0.032-0.020-1.2-0.10.3-0.4-1.10.70.004-0.0050.047-0.24-0.160.14-1.7-0.40.10.225-0.0600.010
Part 2: Moxifloxacin 400 mg0.029-0.1190.057-0.1160.005-0.181-0.018-0.0010.002-0.111-0.097-0.1270.11.0-0.3-0.037-0.025-0.003-0.6-1.10.2-0.6-0.20.20.031-0.0010.000-0.08-0.180.07-0.9-0.4-0.10.8900.6310.173
Part 2: Placebo-0.0410.023-0.033-0.148-0.036-0.102-0.017-0.020-0.013-0.019-0.050-0.052-0.20.8-0.4-0.0590.001-0.010-1.0-0.5-0.20.7-0.61.0-0.0090.0160.027-0.02-0.050.07-0.4-0.40.50.7510.5570.098

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Part 2: Change From Baseline in Chemistry Parameters: Creatinine, Urate, Total Bilirubin, Direct Bilirubin

Blood samples were collected at indicated timepoints to analyze creatinine, urate, total bilirubin, and direct bilirubin. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionMicromoles per liter (Mean)
Creatinine, Day 8Creatinine, Day 9Creatinine, Day 14Urate, Day 8Urate, Day 9Urate, Day 14Total Bilirubin, Day 8Total Bilirubin, Day 9Total Bilirubin, Day 14Direct Bilirubin, Day 8Direct Bilirubin, Day 9Direct Bilirubin, Day 14
Part 2: GSK3640254 100 mg-1.15-0.48-0.37-8.117.7-4.6-0.171.101.54-0.060.190.19
Part 2: GSK3640254 500 mg1.742.131.30-23.4-17.1-15.7-0.06-0.070.010.140.220.00
Part 2: Moxifloxacin 400 mg7.073.232.712.713.4-6.3-1.161.211.36-0.170.150.14
Part 2: Placebo-0.031.590.67-6.0-4.7-4.1-2.15-0.52-0.65-0.33-0.12-0.12

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Part 1: Absolute Values for Chemistry Parameters: Albumin, Globulin, and Total Protein

Blood samples were collected at indicated timepoints to analyze albumin, globulin, and total protein. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, Day 9

,
InterventionGrams per liter (Mean)
Albumin, Baseline (Day -2)Albumin, Day 3Albumin, Day 7Albumin, Day 9Globulin, Baseline (Day -2)Globulin, Day 3Globulin, Day 7Globulin, Day 9Total protein, Baseline (Day -2)Total protein, Day 3Total protein, Day 7Total Bilirubin, Day 9
Part 1 : GSK3640254 500 mg43.041.844.343.225.527.727.827.568.569.572.270.7
Part 1 : Placebo46.546.047.545.526.526.025.025.573.072.072.571.0

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Part 2: Plasma Concentration of GSK3640254

Blood samples were collected at indicated time points to analyze the plasma concentration of GSK3640254. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each treatment period

,
InterventionNanograms per milliliter (Mean)
Pre-dose, Day 730 minutes, Day 71 Hour, Day 72 Hour, Day 73 Hour, Day 73 Hours 30 minutes, Day 74 Hour, Day 74 Hours 30 minutes, Day 75 Hour, Day 76 Hour, Day 78 Hour, Day 710 Hour, Day 712 Hour, Day 724 Hour, Day 7
Part 2: GSK3640254 100 mg496.0462.3486.6587.8682.4738.6765.5782.4811.3769.8740.9698.7625.4469.9
Part 2: GSK3640254 500 mg23572252233927793372369840114157417241023762356430982257

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Part 1: Absolute Values for Chemistry Parameters: Alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP), Aspartate Aminotransferase (AST), Gamma-glutamyl Transferase (GGT), Creatine Kinase, and Lactate Dehydrogenase

Blood samples were collected at indicated time points to analyze ALT, ALP, AST, GGT, creatine kinase, and lactate dehydrogenase. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionInternational units per liter (Mean)
ALT, Baseline (Day -2),ALT, Day 3ALT, Day 7ALT, Day 9ALP, Baseline (Day -2)ALP, Day 3ALP, Day 7ALP, Day 9AST, Baseline (Day -2)AST, Day 3AST, Day 7AST, Day 9GGT, Baseline (Day -2)GGT, Day 3GGT, Day 7GGT, Day 9Creatine kinase, Baseline (Day -2)Creatine kinase, Day 3Creatine kinase, Day 7Creatine kinase, Day 9Lactate dehydrogenase, Baseline (Day -2)Lactate dehydrogenase, Day 3Lactate dehydrogenase, Day 7Lactate dehydrogenase, Day 9
Part 1 : GSK3640254 500 mg19.716.817.718.254.350.054.854.519.817.518.017.511.010.812.012.0160.791.271.575.5132.0113.3115.8114.5
Part 1 : Placebo33.037.533.528.573.076.575.075.525.024.521.518.021.021.520.019.593.064.571.560.5161.5150.0142.0133.0

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Part 2: Tmax of Moxifloxacin 400 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each treatment period

InterventionHours (Median)
Part 2: Moxifloxacin 400 mg4.000

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Part 2: Tmax of GSK3640254 100 mg and GSK3640254 500 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each Treatment Period

InterventionHours (Median)
Part 2: GSK3640254 100 mg5.008
Part 2: GSK3640254 500 mg5.000

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Part 2: Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Using Fridericia's Formula (QTcF) Following Administration of GSK3640254 100 mg and GSK3640254 500 mg Using Concentration-QTc (C-QTc) Analysis

Twelve-lead ECGs were recorded in participant using automated ECG machine & performed with participant in supine position after a rest of at least 10 minutes.Baseline was defined as the latest pre-dose assessment with a non-missing value for each visit. Change from Baseline was calculated by subtracting Baseline value from post dose value. Placebo-corrected change from Baseline in QT interval corrected for heart rate using Fridericia's formula (QTcF) was calculated as difference in model-predicted mean change from Baseline in QTcF between treatment groups using C-QTc analysis. A linear mixed-effects model with change from Baseline in QTcF as the dependent variable, time-matched GSK3640254 plasma concentration as a fixed effect, centered Baseline as additional covariate,treatment &time as categorical factors, & a random intercept & slope per participant. In all calculations, concentrations in participants who received placebo were set to 0. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1) and up to Day 7

InterventionMilliseconds (ms) (Geometric Least Squares Mean)
Part 2: GSK3640254 100 mg2.72
Part 2: GSK3640254 500 mg11.49

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Part 2: Ctau of GSK3640254 100 mg and GSK3640254 500 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each Treatment Period

InterventionNanograms per milliliter (Geometric Mean)
Part 2: GSK3640254 100 mg459.9
Part 2: GSK3640254 500 mg2137

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Part 2: Cmax of Moxifloxacin 400 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each treatment period

InterventionNanograms per milliliter (Geometric Mean)
Part 2: Moxifloxacin 400 mg1964

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Part 2: Cmax of GSK3640254 100 mg and GSK3640254 500 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each Treatment Period

InterventionNanograms per milliliter (Geometric Mean)
Part 2: GSK3640254 100 mg830.3
Part 2: GSK3640254 500 mg4261

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Part 2: AUC(0-tau) of GSK3640254 100 mg and GSK3640254 500 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each Treatment Period

InterventionHours*nanograms per milliliter (Geometric Mean)
Part 2: GSK3640254 100 mg13830
Part 2: GSK3640254 500 mg67490

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Part 2: AUC(0-t) of GSK3640254 100 mg and GSK3640254 500 mg

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods . (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 8 Hours, 10 Hours, 12 Hours, 24 Hours post-dose on Day 7 in each Treatment Period

InterventionHours*nanograms per milliliter (Geometric Mean)
Part 2: GSK3640254 100 mg13840
Part 2: GSK3640254 500 mg67520

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Part 1: Time of Maximum Observed Concentration (Tmax) of GSK3640254

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hours, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 12 Hours, 24 Hours, 48 Hours post-dose on Day 7

InterventionHours (Median)
Part 1: GSK3640254 500 mg4.500

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Part 1: Plasma Concentration at the End of the Dosing Interval (Ctau) of GSK3640254

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hours, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 12 Hours, 24 Hours, 48 Hours post-dose on Day 7

InterventionNanograms per milliliter (Geometric Mean)
Part 1: GSK3640254 500 mg2081

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Part 1: Maximum Observed Concentration (Cmax) of GSK3640254

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hours, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 12 Hours, 24 Hours, 48 Hours post-dose on Day 7

InterventionNanograms per milliliter (Geometric Mean)
Part 1: GSK3640254 500 mg4439

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Part 2: Change From Baseline in Chemistry Parameters: Amylase, Lipase

Blood samples were collected at indicated timepoints to analyze amylase, lipase. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionUnits per liter (Mean)
Amylase, Day 8Amylase, Day 9Amylase, Day 14Lipase, Day 8Lipase, Day 9Lipase, Day 14
Part 2: GSK3640254 100 mg-3.6-1.0-4.1-1.50.2-1.8
Part 2: GSK3640254 500 mg-2.50.4-2.3-3.01.7-2.6
Part 2: Moxifloxacin 400 mg-0.12.1-0.7-0.7-0.9-0.5
Part 2: Placebo-0.83.1-2.34.40.9-1.5

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Part 2: Change From Baseline in Chemistry Parameters: ALT, ALP, AST, GGT, Creatine Kinase, Lactate Dehydrogenase

Blood samples were collected at indicated time points to analyze ALT, ALP, AST, GGT, creatine kinase, and lactate dehydrogenase. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionInternational units per liter (Mean)
ALT, Day 8ALT, Day 9ALT, Day 14ALP, Day 8ALP, Day 9ALP, Day 14AST, Day 8AST, Day 9AST, Day 14GGT, Day 8GGT, Day 9GGT, Day 14Creatine kinase, Day 8Creatine kinase, Day 9Creatine kinase, Day 14Lactate dehydrogenase, Day 8Lactate dehydrogenase, Day 9Lactate dehydrogenase, Day 14
Part 2: GSK3640254 100 mg-2.5-0.6-1.6-1.22.10.5-1.90.7-1.2-0.70.3-0.8-31.763.9-22.5-11.90.0-3.3
Part 2: GSK3640254 500 mg2.03.81.7-1.71.1-2.0-0.21.10.0-0.10.3-1.3-45.015.8-22.0-13.44.0-8.1
Part 2: Moxifloxacin 400 mg-0.9-0.90.6-0.7-0.1-1.10.0-0.3-0.7-1.0-0.4-1.328.2-5.7-30.8-12.5-11.6-10.8
Part 2: Placebo-2.10.7-2.3-2.2-3.6-1.8-1.60.9-1.5-0.5-0.1-1.0-18.939.78.8-11.21.9-5.4

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Part 2: Change From Baseline in Chemistry Parameters: Albumin, Globulin, Total Protein

Blood samples were collected at indicated timepoints to analyze albumin, globulin, and total protein. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionGrams per liter (Mean)
Albumin, Day 8Albumin, Day 9Albumin, Day 14Globulin, Day 8Globulin, Day 9Globulin, Day 14Total protein, Day 8Total protein, Day 9Total protein, Day 14
Part 2: GSK3640254 100 mg-1.61.10.1-0.20.40.6-1.81.60.7
Part 2: GSK3640254 500 mg-2.20.7-2.3-0.10.0-0.2-2.20.7-2.6
Part 2: Moxifloxacin 400 mg-2.0-0.5-1.2-0.1-0.50.1-2.1-0.9-1.1
Part 2: Placebo-2.50.4-0.9-0.60.0-0.4-3.10.4-1.3

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Part 2: Absolute Values for Vital Parameters: SBP and DBP

SBP and DBP were measured in the semi-recumbent or supine position with a completely automated device after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9, and Day 14

,,,
InterventionMillimeters of mercury (Mean)
SBP, Baseline (Pre-dose, Day 1)SBP, Day 2SBP, Day 3SBP, Day 4SBP, Day 5SBP, Day 6SBP, Day 7SBP, Day 8,SBP, Day 9SBP, Day 14DBP, Baseline (Pre-dose, Day 1)DBP, Day 2DBP, Day 3DBP, Day 4DBP, Day 5DBP, Day 6DBP, Day 7DBP, Day 8DBP, Day 9DBP, Day 14
Part 2: GSK3640254 100 mg106.8105.6105.1105.3103.7105.7107.4109.4109.0107.862.160.961.061.059.161.661.161.461.361.8
Part 2: GSK3640254 500 mg105.4105.7105.3105.7106.8108.4107.4109.1105.8106.361.460.963.062.861.762.462.362.765.861.2
Part 2: Moxifloxacin 400 mg106.7104.5103.8103.5103.3104.7106.7108.1104.2108.060.959.360.060.059.360.159.662.656.662.8
Part 2: Placebo106.0103.9104.3103.1105.7105.2107.6109.9115.9105.661.159.660.959.860.360.361.062.366.261.6

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Part 2: Absolute Values for Vital Parameter: Temperature

Temperature was measured in the semi-recumbent or supine position with a completely automated device after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 1, Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9, Day 10, Day 11, Day 12, Day 13, and Day 14

,,,
InterventionDegrees Celsius (Mean)
Baseline (Pre-dose, Day 1)Day 1Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 10Day 11Day 12Day 13Day 14
Part 2: GSK3640254 100 mg36.2236.2536.1836.1436.1836.1636.1736.2236.3236.2336.1736.2836.2636.2036.36
Part 2: GSK3640254 500 mg36.3236.2136.1836.1536.2336.1836.1636.2236.3436.1236.1336.1936.0736.2136.31
Part 2: Moxifloxacin 400 mg36.2836.2936.1736.0936.1336.0836.2136.1936.2536.1836.1036.2236.1436.2536.31
Part 2: Placebo36.2536.1436.2236.2036.2136.2636.2136.2036.2836.1636.0536.0536.1036.1236.25

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Part 2: Absolute Values for Vital Parameter: Pulse Rate

Pulse rate was measured in the semi-recumbent or supine position with a completely automated device after at least 5 minutes of rest for the participant in a quiet setting without distractions. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 2, Day 3, Day 4, Day 5, Day 6, Day 7, Day 8, Day 9, and Day 14

,,,
InterventionBeats per minute (Mean)
Baseline (Pre-dose, Day 1)Day 2Day 3Day 4Day 5Day 6Day 7Day 8Day 9Day 14
Part 2: GSK3640254 100 mg61.861.662.263.563.363.762.763.970.363.6
Part 2: GSK3640254 500 mg61.063.263.964.566.066.565.865.770.461.1
Part 2: Moxifloxacin 400 mg60.462.463.063.062.463.061.663.966.863.6
Part 2: Placebo62.561.963.463.464.462.063.463.969.263.6

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Part 2: Absolute Values for Urinalysis Parameter: Specific Gravity

Urine samples were collected at indicated time points to analyze the urine specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionRatio (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg1.01671.01791.01791.0165
Part 2: GSK3640254 500 mg1.01611.01881.01361.0175
Part 2: Moxifloxacin 400 mg1.01531.01641.02191.0170
Part 2: Placebo1.01521.01801.01891.0165

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Part 2: Absolute Values for Urinalysis Parameter: pH

Urine samples were collected at indicated time points to analyze the urine pH by dipstick test. The dipstick test gives results in a semi-quantitative manner indicating proportional concentrations in the urine sample. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acidic pH (5.0 - 6.0). Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionpH (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg6.095.986.066.13
Part 2: GSK3640254 500 mg6.136.026.206.12
Part 2: Moxifloxacin 400 mg6.195.885.916.00
Part 2: Placebo6.105.905.756.00

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Part 2: Absolute Values for Hematology Parameter: Hemoglobin

Blood samples were collected at indicated time points to analyze hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionGrams per liter (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg141.6140.4143.7142.1
Part 2: GSK3640254 500 mg141.7143.4137.7142.2
Part 2: Moxifloxacin 400 mg140.5140.3140.0140.1
Part 2: Placebo141.8139.9139.4140.7

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Part 2: Absolute Values for Hematology Parameter: Hematocrit

Blood samples were collected at indicated time points to analyze hematocrit. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, Day 14

,,,
InterventionProportion of red blood cells in blood (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg0.41570.41230.42470.4175
Part 2: GSK3640254 500 mg0.41670.41710.40290.4189
Part 2: Moxifloxacin 400 mg0.41310.41200.40860.4107
Part 2: Placebo0.41630.40990.41340.4118

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Part 2: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Volume

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular volume. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, Day 14

,,,
InterventionFemtoliter (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg86.2686.2984.6186.05
Part 2: GSK3640254 500 mg85.9284.9187.0885.53
Part 2: Moxifloxacin 400 mg85.9685.5786.4286.17
Part 2: Placebo85.9385.9585.0086.25

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Part 2: Placebo-corrected Change From Baseline in QTcF Following Administration of Moxifloxacin

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline is defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. Placebo-corrected change from Baseline in QTcF was calculated as model-predicted mean change from Baseline in QTcF in moxifloxacin group minus model-predicted mean change from Baseline in QTcF in the placebo group. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

InterventionMilliseconds (Least Squares Mean)
Day 7, PredoseDay7, 0.5 Hour Post-doseDay 7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay 7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: Moxifloxacin 400 mg0.6-0.2-0.85.67.98.98.68.48.28.26.96.85.36.8

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Part 2: Absolute Values for Hematology Parameter: Erythrocytes

Blood samples were collected at indicated time points to analyze Erythrocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
Intervention10^12 cells per liter (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg4.8294.7945.0234.866
Part 2: GSK3640254 500 mg4.8644.9274.6324.910
Part 2: Moxifloxacin 400 mg4.8154.8334.7374.780
Part 2: Placebo4.8594.7754.8904.782

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Part 2: Absolute Values for Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes

Blood samples were collected at indicated time points to analyze basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelets and leukocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, Day 14

,,,
Intervention10^9 cells per liter (Mean)
Basophils,Baseline (Day -2)Basophils,Day 8Basophils,Day 9Basophils,Day 14Eosinophils,Baseline (Day -2)Eosinophils,Day 8Eosinophils,Day 9Eosinophils,Day 14Lymphocytes,Baseline (Day -2)Lymphocytes,Day 8Lymphocytes,Day 9Lymphocytes,Day 14Monocytes,Baseline (Day -2)Monocytes,Day 8Monocytes,Day 9Monocytes,Day 14Neutrophils, Baseline (Day -2)Neutrophils,Day 8Neutrophils,Day 9Neutrophils,Day 14Platelets,Baseline (Day -2)Platelets, Day 8Platelets, Day 9Platelets, Day 14Leukocytes, Baseline (Day -2)Leukocytes,Day 8Leukocytes,Day 9Leukocytes,Day 14
Part 2: GSK3640254 100 mg0.0370.0300.0390.0330.1350.1300.1140.1261.7361.6751.6371.7050.4510.4560.3890.4312.9572.8252.6192.758234.0234.8225.9234.05.315.114.785.05
Part 2: GSK3640254 500 mg0.0310.0390.0250.0400.1230.1350.0810.1411.6771.6881.5401.7550.4290.5010.3500.4482.8292.9522.5302.750230.8224.7235.4226.75.085.324.535.14
Part 2: Moxifloxacin 400 mg0.0360.0320.0360.0310.1270.1360.1200.1311.8301.6051.9071.6060.4420.4360.4680.3992.9022.6712.6182.506237.1226.4233.3227.15.344.875.144.67
Part 2: Placebo0.0350.0350.0320.0330.1240.1160.1670.1131.6941.6411.6031.7100.4270.4260.4850.4132.8422.8892.9902.712233.7228.9221.4231.65.125.105.274.97

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Part 2: Absolute Values for Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, Blood Urea Nitrogen

Blood samples were collected at indicated time points to analyze glucose, cholesterol, magnesium, triglycerides, anion gap, calcium, carbon dioxide, chloride, phosphate, potassium, sodium, and blood urea nitrogen. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionMillimoles per liter (Mean)
Glucose,Baseline (Day -2)Glucose, Day 8Glucose, Day 9Glucose, Day 14Cholesterol, Baseline (Day -2)Cholesterol, Day 8,Cholesterol, Day 9Cholesterol, Day 14Magnesium, Baseline (Day -2)Magnesium, Day 8Magnesium, Day 9Magnesium, Day 14Triglycerides, Baseline (Day -2)Triglycerides, Day 8Triglycerides, Day 9Triglycerides, Day 14Anion gap, Baseline (Day -2)Anion gap, Day 8Anion gap, Day 9Anion gap, Day 14Calcium, Baseline (Day -2)Calcium, Day 8Calcium, Day 9Calcium, Day 14Carbon dioxide, Baseline (Day -2)Carbon dioxide, Day 8Carbon dioxide, Day 9Carbon dioxide, Day 14Chloride, Baseline (Day -2)Chloride, Day 8Chloride, Day 9Chloride, Day 14Phosphate, Baseline (Day -2)Phosphate, Day 8Phosphate, Day 9Phosphate, Day 14Potassium, Baseline (Day -2)Potassium, Day 8Potassium, Day 9Potassium, Day 14Sodium, Baseline (Day -2)Sodium, Day 8Sodium, Day 9Sodium, Day 14Blood Urea Nitrogen, Baseline(Day-2)Blood Urea Nitrogen, Day 8Blood Urea Nitrogen, Day 9Blood Urea Nitrogen, Day 14
Part 2: GSK3640254 100 mg4.8104.7984.8114.7134.2434.1474.4674.2330.7910.7830.7710.8010.9960.9800.8911.0139.910.110.810.22.3502.3162.4022.39130.529.230.030.5103.3103.0102.8103.61.1821.1861.2121.2224.354.204.424.43139.2138.1139.2139.94.5734.8055.2514.428
Part 2: GSK3640254 500 mg4.7534.6704.7914.7494.3504.1864.0504.1450.7930.7930.8170.7960.9780.8940.7781.04910.510.110.89.82.3752.3162.3322.35830.229.328.930.8103.2102.5103.0103.51.1721.1681.1931.2194.324.074.184.44139.4137.8138.6139.64.4144.6754.2434.451
Part 2: Moxifloxacin 400 mg4.7394.7494.6684.7774.3304.2464.2534.1800.7960.7690.8200.7891.0590.9580.9350.94110.210.311.19.92.3632.3162.3662.34930.229.629.230.3103.4102.6103.9103.31.1991.1951.2921.1644.344.264.174.41139.4138.2139.9139.04.4195.1565.4534.440
Part 2: Placebo4.8134.7774.7634.7944.3234.3003.9884.3610.7940.7930.7360.7961.0110.9771.0360.94810.010.110.09.92.3712.3172.3572.36730.429.330.230.3102.8103.5102.4103.91.1901.1941.1661.2334.304.294.264.39138.8138.6138.4139.64.3255.2424.4724.637

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Part 2: Absolute Values for Chemistry Parameters: Creatinine, Urate, Total Bilirubin, Direct Bilirubin

Blood samples were collected at indicated timepoints to analyze creatinine, urate, total bilirubin, and direct bilirubin. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionMicromoles per liter (Mean)
Creatinine, Baseline (Day -2)Creatinine, Day 8Creatinine, Day 9Creatinine, Day 14Urate, Baseline (Day -2)Urate, Day 8Urate, Day 9Urate, Day 14Total Bilirubin, Baseline (Day -2)Total Bilirubin, Day 8Total Bilirubin, Day 9Total Bilirubin, Day 14Direct Bilirubin, Baseline (Day -2)Direct Bilirubin, Day 8Direct Bilirubin, Day 9Direct Bilirubin, Day 14
Part 2: GSK3640254 100 mg81.8678.3889.3879.16293.6286.7307.2290.111.1310.6813.1612.402.051.972.302.22
Part 2: GSK3640254 500 mg79.8382.0180.6381.47295.3277.6261.1285.411.7911.6312.0011.532.072.222.232.10
Part 2: Moxifloxacin 400 mg79.3888.5577.0784.19294.6302.1295.3293.111.7910.3613.7112.892.121.902.392.21
Part 2: Placebo80.5178.4586.8979.56297.5288.3290.2291.412.189.9112.5011.422.221.862.232.06

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Part 1: AUC From Time Zero to the End of the Dosing Interval at Steady State (AUC[0-tau]) of GSK3640254

Blood samples were collected at indicated time points. PK analysis was conducted using standard non-compartmental methods. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hours, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 12 Hours, 24 Hours, 48 Hours post-dose on Day 7

InterventionHours*nanograms per milliliter (Geometric Mean)
Part 1: GSK3640254 500 mg68790

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Part 2: Absolute Values for Chemistry Parameters: Amylase and Lipase

Blood samples were collected at indicated timepoints to analyze amylase and lipase. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionUnits per liter (Mean)
Amylase, Baseline (Day -2)Amylase, Day 8Amylase, Day 9Amylase, Day 14Lipase, Baseline (Day -2),Lipase, Day 8Lipase, Day 9Lipase, Day 14
Part 2: GSK3640254 100 mg58.253.461.052.927.025.228.124.8
Part 2: GSK3640254 500 mg56.257.744.658.027.526.622.726.6
Part 2: Moxifloxacin 400 mg55.959.149.258.526.526.523.726.7
Part 2: Placebo55.752.466.350.925.329.328.423.6

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Part 2: Absolute Values for Chemistry Parameters: ALT, ALP, AST, GGT, Creatine Kinase, Lactate Dehydrogenase

Blood samples were collected at indicated time points to analyze ALT, ALP, AST, GGT, creatine kinase, and lactate dehydrogenase. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionInternational units per liter (Mean)
ALT, Baseline (Day -2)ALT, Day 8ALT, Day 9ALT, Day 14ALP, Baseline (Day -2)ALP, Day 8ALP, Day 9ALP, Day 14AST, Baseline (Day -2)AST, Day 8AST, Day 9AST, Day 14GGT, Baseline (Day -2)GGT, Day 8GGT, Day 9GGT, Day 14Creatine kinase, Baseline (Day -2)Creatine kinase, Day 8Creatine kinase, Day 9Creatine kinase, Day 14Lactatedehydrogenase, Baseline(Day-2)Lactate dehydrogenase, Day 8Lactate dehydrogenase, Day 9Lactate dehydrogenase, Day 14
Part 2: GSK3640254 100 mg17.515.714.216.658.057.158.958.815.513.715.614.516.615.219.115.1112.682.5171.191.7119.6108.0118.2116.6
Part 2: GSK3640254 500 mg16.319.516.419.058.959.653.059.415.315.615.115.816.718.710.817.7117.890.381.1110.1121.2113.5108.1118.8
Part 2: Moxifloxacin 400 mg16.817.212.518.758.355.663.555.115.516.013.615.317.217.912.517.5120.8163.975.5104.9122.8111.8107.4113.5
Part 2: Placebo18.314.026.613.858.756.856.156.715.814.017.314.116.715.020.314.7103.072.8173.4102.1119.9107.5124.0113.4

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Part 2: Absolute Values for Chemistry Parameters: Albumin, Globulin, Total Protein

Blood samples were collected at indicated timepoints to analyze albumin, globulin, and total protein. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visit. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, and Day 14

,,,
InterventionGrams per liter (Mean)
Albumin, Baseline (Day -2)Albumin, Day 8Albumin, Day 9Albumin, Day 14Globulin, Baseline (Day -2)Globulin, Day 8Globulin, Day 9Globulin, Day 14Total protein, Baseline (Day -2)Total protein, Day 8Total protein, Day 9Total protein, Day 14
Part 2: GSK3640254 100 mg43.642.244.043.925.925.526.926.469.567.870.970.3
Part 2: GSK3640254 500 mg44.542.843.542.826.326.425.626.170.769.269.168.8
Part 2: Moxifloxacin 400 mg44.042.043.542.826.026.424.526.670.068.467.969.4
Part 2: Placebo43.841.742.743.226.625.129.325.070.466.872.068.2

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Part 1: Plasma Concentration of GSK3640254

Blood samples were collected at indicated time points to analyze the plasma concentration of GSK3640254. (NCT04563845)
Timeframe: Pre-dose and 30 minutes, 1 Hour, 2 Hour, 3 Hours, 3 Hours 30 minutes, 4 Hours, 4 Hours 30 minutes, 5 Hours, 6 Hours, 12 Hours, 24 Hours, 48 Hours post-dose on Day 7

InterventionNanograms per milliliter (Mean)
Pre-dose, Day 730 minutes, Day 71 Hour, Day 72 Hour, Day 73 Hour, Day 73 Hours 30 minutes, Day 74 Hour, Day 74 Hours 30 minutes, Day 75 Hour, Day 76 Hour, Day 712 Hour, Day 724 Hour, Day 748 Hour, Day 7
Part 1: GSK3640254 500 mg2168200025793513422841554213445238404010277321151070

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Part 1: Number of Participants With Serious Adverse Events (SAEs) and Non-SAEs

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any untoward medical occurrence that, at any dose that results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability or incapacity, is a congenital anomaly or birth defect as per medical and scientific judgment. Adverse events which were not Serious Adverse Events were considered as Non-Serious adverse events. (NCT04563845)
Timeframe: Up to Day 9

,
InterventionParticipants (Count of Participants)
Non SAESAE
Part 1 : GSK3640254 500 mg10
Part 1 : Placebo20

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Part 1: Number of Participants With Clinically Significant Abnormal 12-Lead Electrocardiogram (ECG) Findings

A 12-lead ECG was recorded with the participant in a supine position. 12-lead ECGs were obtained by using an automated ECG machine. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for number of participants with clinically significant abnormal 12-Lead ECG findings has reported (NCT04563845)
Timeframe: Baseline(Day-2), Day1: 2 Hours, 4 Hours, 6 Hours; Day 4: 2 Hours, 4 Hours, 6 Hours, Day 7: 2 Hours, 4 Hours, 6 Hours and Day 9

,
InterventionParticipants (Count of Participants)
Baseline (Day -2)Day 1: 2 hoursDay 1: 4 hoursDay 1: 6 hoursDay 4: 2 hoursDay 4: 4 hoursDay 4: 6 hoursDay 7: 2 hoursDay 7: 4 hoursDay 7: 6 hoursDay 9
Part 1 : GSK3640254 500 mg00000000000
Part 1 : Placebo00000000000

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Part 2: Placebo-corrected Change From Baseline in QT Interval Corrected for Heart Rate Using Fridericia's Formula (QTcF) Following Administration of GSK3640254 100 mg and GSK3640254 500 mg By-time Point Analysis

Twelve-lead ECGs were recorded in participant using automated ECG machine & performed with participant in supine position after a rest of at least 10 minutes.Baseline was defined as the latest pre-dose assessment with a non-missing value for each visit. Change from Baseline was calculated by subtracting Baseline value from post dose value. Placebo-corrected change from Baseline in QT interval corrected for heart rate using Fridericia's formula (QTcF) was calculated as model-predicted mean change from Baseline in QTcF in GSK3640254 group minus model-predicted mean change from Baseline in QTcF in the placebo group (by-time point analysis). Time point analysis was performed based on a linear mixed-effects model: Change from Baseline in QTcF = Time + Treatment + Time*Treatment +Baseline QTcF + Period + Sequence. An unstructured covariance structure was used to specify the repeated measures (time within participant and period). A random intercept per participant was also included. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1), Day 7 : Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,
InterventionMilliseconds (Least Squares Mean)
Day7, PredoseDay7, 0.5 Hour Post-doseDay7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg1.41.00.61.71.51.41.01.00.21.7-0.80.20.50.1
Part 2: GSK3640254 500 mg7.17.24.16.58.19.28.610.69.68.68.18.66.07.7

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Part 2: Placebo-corrected Change From Baseline in QRS Following Administration of GSK3640254 100 mg and GSK3640254 500 mg

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. Placebo-corrected change from Baseline in QRS was calculated as model-predicted mean change from Baseline in QRS interval in GSK3640254 group minus model-predicted mean change from Baseline in QRS interval in the placebo group. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1) Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,
InterventionMilliseconds (Least Squares Mean)
Day7, PredoseDay7, 0.5 Hour Post-doseDay7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg0.10.20.30.50.50.30.30.20.20.10.30.50.60.9
Part 2: GSK3640254 500 mg0.60.50.70.70.40.60.50.40.40.20.70.60.51.4

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Part 2: Placebo-corrected Change From Baseline in PR Following Administration of GSK3640254 100 mg and GSK3640254 500 mg

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline is defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. Placebo-corrected change from Baseline in PR was calculated as model-predicted mean change from Baseline in PR interval in GSK3640254 group minus model-predicted mean change from Baseline in PR interval in the placebo group. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1) Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,
InterventionMilliseconds (Least Squares Mean)
Day7, PredoseDay7, 0.5 Hour Post-doseDay7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg1.50.41.2-0.80.40.91.20.70.00.2-0.31.10.6-1.4
Part 2: GSK3640254 500 mg2.12.50.11.62.03.21.71.10.30.21.11.11.8-1.8

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Part 2: Placebo-corrected Change From Baseline in HR Following Administration of GSK3640254 100 mg and GSK3640254 500 mg

Twelve-lead ECGs were recorded in participant using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Baseline is defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. Placebo-corrected change from Baseline in HR was calculated as model-predicted mean change from Baseline in HR in GSK3640254 group minus model-predicted mean change from Baseline in HR in the placebo group. (NCT04563845)
Timeframe: Baseline (Pre-dose, Day 1) Day 7: Predose and 0.5, 1, 2, 3, 3.5, 4, 4.5, 5, 6, 8, 10, 12, 24 Hours post dose

,
InterventionBeats per minute (Least Squares Mean)
Day7, PredoseDay7, 0.5 Hour Post-doseDay7, 1 Hour Post-doseDay7, 2 Hour Post-doseDay7, 3 Hour Post-doseDay7, 3.5 Hour Post-doseDay7, 4 Hour Post-doseDay7, 4.5 Hour Post-doseDay7, 5 Hour Post-doseDay7, 6 Hour Post-doseDay7, 8 Hour Post-doseDay7, 10 Hour Post-doseDay7, 12 Hour Post-doseDay7, 24 Hour Post-dose
Part 2: GSK3640254 100 mg-0.3-0.20.21.41.41.71.11.81.61.01.10.80.42.6
Part 2: GSK3640254 500 mg2.53.94.02.52.93.23.33.24.14.14.25.11.13.9

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Part 2: Absolute Values for Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value for each period, including those from unscheduled visits. (NCT04563845)
Timeframe: Baseline (Day -2), Day 8, Day 9, Day 14

,,,
InterventionPicograms (Mean)
Baseline (Day -2)Day 8Day 9Day 14
Part 2: GSK3640254 100 mg29.3729.3928.6229.29
Part 2: GSK3640254 500 mg29.2129.1729.7929.02
Part 2: Moxifloxacin 400 mg29.2329.1329.5629.40
Part 2: Placebo29.2729.3428.6729.45

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Part 1: Change From Baseline in Urinalysis Parameter: Specific Gravity

Urine samples were collected at indicated time points to analyze the urine specific gravity. Urine specific gravity is a measure of the concentration of solutes in the urine and provides information on the kidney's ability to concentrate urine. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionRatio (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg0.00330.00750.0005
Part 1 : Placebo0.00700.01100.0065

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Part 1: Change From Baseline in Urinalysis Parameter: pH

Urine samples were collected at indicated time points to analyze the urine pH by dipstick test. The dipstick test gives results in a semi-quantitative manner indicating proportional concentrations in the urine sample. Urine pH is an acid-base measurement. pH is measured on a numeric scale ranging from 0 to 14; values on the scale refer to the degree of alkalinity or acidity. A pH of 7 is neutral. A pH less than 7 is acidic, and a pH greater than 7 is basic. Normal urine has a slightly acidic pH (5.0 - 6.0). Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionpH (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg-0.75-0.83-0.83
Part 1 : Placebo0.00-0.250.00

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Part 2: Number of Participants With Treatment Emergent Changes of T-wave Morphology and Presence of U-wave Following Administration of GSK3640254 100 mg and GSK3640254 500 mg

Twelve-lead ECGs were recorded using an automated ECG machine. Twelve-lead ECGs were performed with the participant in a supine position after a rest of at least 10 minutes. Flat T-wave=T-amplitude < 1 mm (either positive [+] or negative [-]), including flat isoelectric line, Notched T-wave (+)=Presence of notch(es) of at least 0.05 millivolt (mV) amplitude on ascending or descending arm of the positive T-wave, Biphasic= T-wave that contains a second component with an opposite phase that is at least 0.1 mV deep (both positive/negative and negative/positive and polyphasic T-waves included), Normal T-wave (-)=T-amplitude that is negative, without biphasic T-wave or notches, Notched T-wave (-): Presence of notch(es) of at least 0.05 mV amplitude on descending or ascending arm of the negative T-wave, U-waves= Presence of abnormal U-waves. Data has been reported for Flat T-wave, Notched T-wave (Positive), Biphasic, Normal T-wave (Negative), Notched T-wave (Negative) and T-U wave Fusion. (NCT04563845)
Timeframe: Up to Day 51

,
InterventionParticipants (Count of Participants)
Flat T-waveNotched T-wave (Positive)BiphasicNormal T-wave (Negative)Notched T-wave (Negative)T-U wave Fusion
Part 2: GSK3640254 100 mg201000
Part 2: GSK3640254 500 mg100000

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Part 1: Change From Baseline in Chemistry Parameters: Glucose, Cholesterol, Magnesium, Triglycerides, Anion Gap, Calcium, Carbon Dioxide, Chloride, Phosphate, Potassium, Sodium, Blood Urea Nitrogen

Blood samples were collected at indicated time points to analyze glucose, cholesterol, magnesium, triglycerides, anion gap, calcium, carbon dioxide, chloride, phosphate, potassium, sodium, and blood urea nitrogen. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionMillimoles per liter (Mean)
Glucose, Day 3Glucose, Day 7Glucose, Day 9Cholesterol, Day 3Cholesterol, Day 7Cholesterol, Day 9Magnesium, Day 3Magnesium, Day 7Magnesium, Day 9Triglycerides, Day 3Triglycerides, Day 7Triglycerides, Day 9Anion gap, Day 3Anion gap, Day 7Anion gap, Day 9Calcium, Day 3Calcium, Day 7Calcium, Day 9Carbon dioxide, Day 3Carbon dioxide, Day 7Carbon dioxide, Day 9Chloride, Day 3Chloride, Day 7Chloride, Day 9Phosphate, Day 3Phosphate, Day 7Phosphate, Day 9Potassium, Day 3Potassium, Day 7Potassium, Day 9Sodium, Day 3Sodium, Day 7Sodium, Day 9Blood Urea Nitrogen, Day 3Blood Urea Nitrogen, Day 7Blood Urea Nitrogen, Day 9
Part 1 : GSK3640254 500 mg0.0630.047-0.0770.2580.3020.0930.0200.0200.0470.093-0.105-0.148-0.80.00.30.0380.0770.0050.00.50.7-1.0-1.5-0.50.0970.0820.0700.180.120.10-2.0-0.80.50.1670.208-0.150
Part 1 : Placebo-0.555-0.585-0.4150.3650.155-0.0250.0400.0400.040-0.090-0.290-0.330-1.0-2.5-1.5-0.0100.000-0.0501.01.51.0-0.50.51.50.0150.000-0.065-0.050.300.00-0.5-0.51.00.3250.9300.415

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Part 2: Number of Participants With Non-SAEs and SAEs

An AE is any untoward medical occurrence in a clinical study participant, temporally associated with the use of a study intervention, whether or not considered related to the study intervention. An SAE is defined as any untoward medical occurrence that, at any dose that results in death, is life-threatening, requires inpatient hospitalization or prolongation of existing hospitalization, results in persistent or significant disability or incapacity, is a congenital anomaly or birth defect as per medical and scientific judgment. Adverse events which were not Serious Adverse Events were considered as Non-Serious adverse events. (NCT04563845)
Timeframe: Up to Day 51

,,,
InterventionParticipants (Count of Participants)
Non SAESAE
Part 2: GSK3640254 100 mg50
Part 2: GSK3640254 500 mg100
Part 2: Moxifloxacin 400 mg40
Part 2: Placebo70

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Part 2: Number of Participants With Clinically Significant Abnormal 12-Lead ECG Findings

A 12-lead ECG was recorded with the participant in a supine position. 12-lead ECGs were obtained by using an automated ECG machine. Clinically significant abnormal findings are those which are not associated with the underlying disease, unless judged by the investigator to be more severe than expected for the participant's condition. Data for number of participants with clinically significant abnormal 12-Lead ECG findings has reported. (NCT04563845)
Timeframe: Baseline(Day-2), Day1: 1 Hour, 2 Hours, 3 Hours, 4 Hours, 6 Hours; Day 2: 24 Hours, Day 4: 1 Hour, 2 Hours, 3 Hours, 4 Hours, 6 Hours, Day 5: 24 Hours; Day 7: 1 Hour, 2 Hours, 3 Hours, 4 Hours, 6 Hours; Day 8: 24 Hours; Day 9 and Day 14

,,,
InterventionParticipants (Count of Participants)
Baseline (Day -2)Day 1: 1 HoursDay 1: 2 HoursDay 1: 3 HoursDay 1: 4 HoursDay 1: 6 HoursDay 2: 24 HoursDay 4: 1 HoursDay 4: 2 HoursDay 4: 3 HoursDay 4: 4 HoursDay 4: 6 HoursDay 5: 24 HoursDay 7: 1 HoursDay 7: 2 HoursDay 7: 3 HoursDay 7: 4 HoursDay 7: 6 HoursDay 8: 24 HoursDay 9Day 14
Part 2: GSK3640254 100 mg000000000000000000000
Part 2: GSK3640254 500 mg000000000000000000000
Part 2: Moxifloxacin 400 mg000000000000000000000
Part 2: Placebo000000000000000000000

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Part 1: Change From Baseline in Chemistry Parameters: Creatinine, Urate, Total Bilirubin, Direct Bilirubin

Blood samples were collected at indicated timepoints to analyze creatinine, urate, total bilirubin, and direct bilirubin. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionMicromoles per liter (Mean)
Creatinine, Day 3Creatinine, Day 7Creatinine, Day 9Urate, Day 3Urate, Day 7Urate, Day 9Total Bilirubin, Day 3Total Bilirubin, Day 7Total Bilirubin, Day 9Direct Bilirubin, Day 3Direct Bilirubin, Day 7Direct Bilirubin, Day 9
Part 1 : GSK3640254 500 mg-2.65-4.72-3.85-15.5-28.5-17.52.634.333.200.270.680.63
Part 1 : Placebo-6.65-3.15-4.45-12.02.5-15.02.953.152.200.500.650.60

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Part 1: Change From Baseline in Hematology Parameter: Hemoglobin

Blood samples were collected at indicated time points to analyze hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionGrams per liter (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg5.58.75.8
Part 1 : Placebo6.08.08.5

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Part 1: Change From Baseline in Hematology Parameter: Hematocrit

Blood samples were collected at indicated timepoints to analyze hemotocrit. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionProportion of red blood cells in blood (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg0.01280.02200.0142
Part 1 : Placebo0.02100.02500.0310

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Part 1: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Volume

Blood samples were collected at indicated time points to analyze erythrocytes mean corpuscular volume. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionFemtoliter (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg-0.47-0.37-0.75
Part 1 : Placebo-0.40-0.400.50

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Part 1: Change From Baseline in Hematology Parameter: Erythrocytes Mean Corpuscular Hemoglobin

Blood samples were collected at idicated time points to analyze erythrocytes mean corpuscular hemoglobin. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionPicograms (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg0.080.15-0.02
Part 1 : Placebo-0.50-0.35-0.35

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Part 1: Change From Baseline in Hematology Parameter: Erythrocytes

Blood samples were collected at indicated time points to analyze the hematology parameter: Erythrocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
Intervention10^12 cells per liter (Mean)
Day 3Day 7Day 9
Part 1 : GSK3640254 500 mg0.1730.2680.205
Part 1 : Placebo0.2700.3200.325

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Part 1: Change From Baseline in Hematology Parameter: Basophils, Eosinophils, Lymphocytes, Monocytes, Neutrophils, Platelets and Leukocytes

Blood samples were collected at indicated time points to analyze basophils, eosinophils, lymphocytes, monocytes, neutrophils, platelets and leukocytes. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
Intervention10^9 cells per liter (Mean)
Basophils, Day 3Basophils, Day 7Basophils, Day 9Eosinophils, Day 3Eosinophils, Day 7Eosinophils, Day 9Lymphocytes, Day 3Lymphocytes, Day 7Lymphocytes, Day 9Monocytes, Day 3Monocytes, Day 7Monocytes, Day 9Neutrophils, Day 3Neutrophils, Day 7Neutrophils, Day 9Platelets, Day 3Platelets, Day 7Platelets, Day 9Leukocytes, Day 3Leukocytes, Day 7Leukocytes, Day 9
Part 1 : GSK3640254 500 mg-0.003-0.0080.008-0.022-0.035-0.040-0.165-0.1530.113-0.075-0.047-0.028-0.895-0.632-0.742-2.313.53.3-1.17-0.88-0.72
Part 1 : Placebo-0.005-0.005-0.010-0.025-0.030-0.0450.195-0.005-0.4200.020-0.025-0.0600.2900.1951.2055.015.511.00.650.300.80

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Part 1: Change From Baseline in Chemistry Parameters: Amylase and Lipase

Blood samples were collected at indicated timepoints to analyze amylase and lipase. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionUnits per liter (Mean)
Amylase, Day 3Amylase, Day 7Amylase, Day 9Lipase, Day 3Lipase, Day 7Lipase, Day 9
Part 1 : GSK3640254 500 mg-2.0-1.0-4.3-5.3-3.2-6.2
Part 1 : Placebo-0.52.50.0-15.0-14.0-15.0

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Part 1: Change From Baseline in Chemistry Parameters: ALT, ALP, AST, GGT, Creatine Kinase, Lactate Dehydrogenase

Blood samples were collected at indicated time points to analyze ALT, ALP, AST, GGT, creatine kinase, and lactate dehydrogenase. Baseline was defined as the latest pre-dose assessment with a non-missing value, including those from unscheduled visits. Change from Baseline was calculated by subtracting the Baseline value from the post-dose visit value. (NCT04563845)
Timeframe: Baseline (Day -2), Day 3, Day 7, and Day 9

,
InterventionInternational units per liter (Mean)
ALT, Day 3ALT, Day 7ALT, Day 9ALP, Day 3ALP, Day 7ALP, Day 9AST, Day 3AST, Day 7AST, Day 9GGT, Day 3GGT, Day 7GGT, Day 9Creatine kinase, Day 3Creatine kinase, Day 7Creatine kinase, Day 9Lactate dehydrogenase, Day 3Lactate dehydrogenase, Day 7Lactate dehydrogenase, Day 9
Part 1 : GSK3640254 500 mg-2.8-2.0-1.5-4.30.50.2-2.3-1.8-2.3-0.21.01.0-69.5-89.2-85.2-18.7-16.2-17.5
Part 1 : Placebo4.50.5-4.53.52.02.5-0.5-3.5-7.00.5-1.0-1.5-28.5-21.5-32.5-11.5-19.5-28.5

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Part 2: Number of Participants With Outlier Results for HR, QTcF, ΔQTcF, PR Interval and QRS Interval for GSK3640254 100 mg and GSK3640254 500 mg

Twelve-lead ECGs were recorded using an automated ECG machine with participant in a supine position after a rest of at least 10 minutes. Number of participants with outlier results for HR, QTcF, ΔQTcF, PR interval and QRS interval were summarized.Categorical outlier criteria was as follows:change from Baseline in QTcF (ΔQTcF) >60 ms: Increase of QTc from Baseline > 60 ms, QTcF > 500 ms:Treatment-emergent value of > 500 ms when not present at Baseline (new onset), HR < 50 bpm with a decrease in change from Baseline in heart rate (ΔHR) > 25%:Decrease of HR from Baseline >25% resulting in HR < 50 bpm, HR > 100 bpm with an increase in ΔHR > 25% :Increase of HR from Baseline >25% resulting in HR > 100 bpm, PR > 200 ms with an increase in change from Baseline in PR interval (ΔPR) > 25%:Increase of PR from Baseline > 25% resulting in PR > 200 ms, QRS > 120 ms with an increase in change from Baseline in QRS interval (ΔQRS) > 25%:Increase of QRS from Baseline > 25% resulting in QRS > 120 ms. (NCT04563845)
Timeframe: Up to Day 51

,
InterventionParticipants (Count of Participants)
ΔQTcF >60 msQTcF >500 msHR <50 bpm with a decrease in ΔHR > 25%HR >100 bpm with an increase in ΔHR > 25%PR >200 ms with an increase in ΔPR > 25%QRS >120 ms an increase in ΔQRS > 25%
Part 2: GSK3640254 100 mg000100
Part 2: GSK3640254 500 mg000100

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