Research Papers

This database includes peer-reviewed publications authored by TB Alliance staff. Use the tags on the left to filter by subject, or search for a particular author or term using the search bar.

Tag: Pharmacokinetics

Displaying 24 papers

The pharmacokinetics of rifampicin, isoniazid, pyrazinamide and ethambutol in infants dosed at revised WHO-recommended treatment guidelines

Publication: Bekker A, Schaaf HS, Murray S, et. al. The pharmacokinetics of rifampicin, isoniazid, pyrazinamide and ethambutol in infants... Antimicrob Agents Chemother. 2016 Jan 25. pii: AAC.02600-15. doi: 10.1128/aac.02600-15.

1/2016

Tags: Childhood TB, Clinical Trial Results, HRZE, Pharmacokinetics, Pyrazinamide

Evaluation of the Pharmacokinetic Interaction between Repeated Doses of Rifapentine or Rifampin and a Single Dose of Bedaquiline in Healthy Adult Subjects

Publication: Winter H, Egizi E, Erondu N, et. al. Evaluation of the pharmacokinetic interaction between repeated doses of rifapentine or rifampin and a single dose of bedaquiline in healthy adult subjects. Antimicrob Agents Chemother. 2015 Feb;59(2):1219-24. doi: 10.1

12/2014

Tags: Bedaquiline (TMC-207), Clinical Development, Clinical Trial Results, Pharmacokinetics, Rifapentine

Rifampicin and rifapentine significantly reduce concentrations of bedaquiline, a new anti-TB drug

Publication: Svensson EM, Murray S, Karlsson MO, Dooley KE. Rifampicin and rifapentine significantly reduce concentrations of bedaquiline, a new anti-TB drug. J Antimicrob Chemother. 2015 Apr;70(4):1106-14. doi: 10.1093/jac/dku504.

12/2014

Tags: Bedaquiline (TMC-207), Clinical Development, Clinical Trial Results, Pharmacokinetics, Rifapentine

In Vitro and In Vivo Activities of the Nitroimidazole TBA-354 against Mycobacterium tuberculosis

Publication: Upton AM, Cho S, Yang TJ, et. al. In vitro and in vivo activities of the nitroimidazole TBA-354 against Mycobacterium tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):136-44. doi: 10.1128/AAC.03823-14.

10/2014

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data, TBA-354

Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 withconcomitant lopinavir-ritonavir, efavirenz, or rifampin

Publication: Dooley KE, Luetkemeyer AF, Park JG, et. al. Phase I safety, pharmacokinetics, and pharmacogenetics study of the antituberculosis drug PA-824 with concomitant lopinavir-ritonavir, efavirenz, or rifampin. Antimicrob Agents Chemother. 2014 Sep;58(9):5245-52.

9/2014

Tags: Clinical Development, Clinical Trial Results, Pharmacokinetics, Pretomanid/PA-824, TB-HIV

1,4-Azaindole, a Potential Drug Candidate for Treatment of Tuberculosis

Publication: Chatterji M, Shandil R, Manjunatha MR, et. al. 1,4-azaindole, a potential drug candidate for treatment of tuberculosis.Antimicrob Agents Chemother. 2014 Sep;58(9):5325-31. doi: 10.1128/AAC.03233-14.

6/2014

Tags: Bedaquiline (TMC-207), Drug Discovery, MDR-TB, Pharmacokinetics, Preclinical Data, Pretomanid/PA-824

Lead optimization of 1,4-azaindoles as antimycobacterial agents

Publication: Shirude PS, Shandil RK, Manjunatha MR, et. al. Lead optimization of 1,4-azaindoles as antimycobacterial agents. J Med Chem. 2014 Jul 10;57(13):5728-37. doi: 10.1021/jm500571f.

6/2014

Tags: Drug Discovery, Pharmacokinetics

Synthesis and biological evaluation of novel 2-methoxypyridylamino-substituted riminophenazine derivatives as antituberculosis agents

Publication: Zhang D, Liu Y, Zhang C, et. al. Synthesis and biological evaluation of novel 2-methoxypyridylamino-substituted riminophenazine derivatives as antituberculosis agents. Molecules. 2014 Apr 9;19(4):4380-94. doi: 10.3390/molecules19044380.

4/2014

Tags: Clofazamine, Pharmacodynamics, Pharmacokinetics

Randomized dose-ranging study of the 14-day early bactericidal activity of bedaquiline (TMC207) in patients withsputum microscopy smear-positive pulmonary tuberculosis

Publication: Diacon AH, Dawson R, Von Groote-Bidlingmaier F, et. al. Randomized Dose-Ranging Study of the 14-Day Early Bactericidal Activity of Bedaquiline (TMC207) in Patients with Sputum Microscopy Smear-Positive Pulmonary Tuberculosis. Antimicrob Agents Chemother.

5/2013

Tags: Bedaquiline (TMC-207), Clinical Development, Clinical Trial Results, Pharmacokinetics

Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents

Publication: Hwang JM, Oh T, Kaneko T., et. al. Design, synthesis, and structure-activity relationship studies of tryptanthrins as antitubercular agents. J Nat Prod. 2013 Mar 22;76(3):354-67. doi: 10.1021/np3007167.

3/2013

Tags: Drug Discovery, Pharmacodynamics, Pharmacokinetics, Preclinical Data

Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors

Publication: Harikrishnan LS, Finlay HJ, Qiao JX, Kamau MG, et. al. Diphenylpyridylethanamine (DPPE) derivatives as cholesteryl ester transfer protein (CETP) inhibitors. J Med Chem. 2012 Jul 12;55(13):6162-75. doi: 10.1021/jm300611v.

7/2012

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

Systematic Evaluation of Structure-Activity Relationships of the Riminophenazine Class and Discovery of a C2 Pyridylamino Series for the Treatment of Multidrug-Resistant Tuberculosis

Publication: Liu B, Liu K, Yang TJ, et. al. Systematic evaluation of structure-activity relationships of... Molecules. 2012 Apr 17;17(4):4545-59. doi: 10.3390/molecules17044545.

4/2012

Tags: Clofazamine, Drug Discovery, Pharmacokinetics, Preclinical Data

Phase II dose-ranging trial of the early bactericidal activity of PA-824

Publication: Diacon AH, Dawson R, du Bois J, et. al. Phase II dose-ranging trial of the early bactericidal activity of PA-824. Antimicrob Agents Chemother. 2012 Jun;56(6):3027-31. doi: 10.1128/AAC.06125-11

3/2012

Tags: Clinical Development, Clinical Trial Results, Pharmacokinetics, Pretomanid/PA-824

New Drugs for the Treatment of Tuberculosis: Needs, Challenges, Promise, and Prospects for the Future

Publication: Lienhardt C, Raviglione M, Spigelman M, et. al. New drugs for the treatment of tuberculosis: needs, challenges, promise, and prospects for the future. J Infect Dis. 2012 May 15;205 Suppl 2:S241-9. doi: 10.1093/infdis/jis034.

3/2012

Tags: Advocacy, Childhood TB, Clinical Development, Drug Discovery, Drug-Sensitivity Testing, Editorials, Global Pipeline, MDR-TB, Moxifloxacin, Pharmacodynamics, Pharmacokinetics, Policy, Preclinical Models, Pretomanid/PA-824, Regimen Change, TB Market, TB-HIV, Trial Design

Synthesis and Structure-activity Relationships of Varied Ether Linker Analogues of the Anti-tubercular Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (

Publication: Thompson AM, Sutherland HS, Palmer BD, et. al. Synthesis and structure-activity relationships of varied ether linker analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5h-imidazo[2,1-b][1,3]oxazine (PA-824).

9/2011

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

Activity of the Fluoroquinolone DC-159a in the Initial and Continuation Phases of Treatment of Murine Tuberculosis

Publication: Vandal OH, Roberts JA, Odaira T, Schnappinger D, Nathan CF, Ehrt S. Acid-susceptible mutants of Mycobacterium tuberculosis share hypersusceptibility to cell wall and oxidative stress and to the host environment. J Bacteriol. 2009 Jan;191(2):625-31. doi: 1

4/2011

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data, XDR-TB

Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

Publication: Kmentova I, Sutherland HS, Palmer BD, et. al. Synthesis and structure-activity relationships of aza- and diazabiphenyl analogues of the antitubercular drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

11/2010

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

PA-824 exhibits time-dependent activity in a murine model of tuberculosis

Publication: Ahmad Z, Peloquin CA, Singh RP, et. al. PA-824 exhibits time-dependent activity in a murine model of tuberculosis. Antimicrob Agents Chemother. 2011 Jan;55(1):239-45. doi: 10.1128/AAC.00849-10.

10/2010

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data, Pretomanid/PA-824

Development of a population pharmacokinetic model for taranabant, a cannibinoid-1 receptor inverse agonist

Publication: Li X (Susie), Nielsen J, Cirincione B, et. al. Development of a Population Pharmacokinetic Model for Taranabant, a Cannibinoid-1 Receptor Inverse Agonist. The AAPS Journal. 2010;12(4):537-547. doi:10.1208/s12248-010-9212-2.

6/2010

Tags: Clinical Trial Results, Drug Discovery, Drug Targets, Pharmacokinetics, Preclinical Models

Synthesis and Structure-Activity Studies of Biphenyl Analogues of the Tuberculosis Drug (6S)-2-Nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824)

Publication: Palmer BD, Thompson AM, Sutherland HS, et. al. Synthesis and structure-activity studies of biphenyl analogues of the tuberculosis drug (6S)-2-nitro-6-{[4-(trifluoromethoxy)benzyl]oxy}-6,7-dihydro-5H-imidazo[2,1-b][1,3]oxazine (PA-824). J Med Chem. 2010 Ja

1/2010

Tags: Drug Discovery, Pharmacokinetics, Preclinical Data

Pages