Research Papers

Antitubercular nitroimidazoles revisited: synthesis and activity of the authentic 3-nitro isomer of pretomanid

Publication: ACS Medicinal Chemistry Letters

Author(s): Andrew M. Thompson, Muriel Bonnet, Ho H. Lee, Scott G. Franzblau, Baojie Wan, George S. Wong, Christopher B. Cooper, William A. Denny

12/2017

Tags: Pretomanid/PA-824

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...

Publication: Dawson R, Diacon AH, Everitt D, et. al. Efficiency and safety of.... Lancet. 2015 May 2;385(9979):1738-47. doi: 10.1016/S0140-6736(14)62002-X.

5/2015

Tags: Clinical Development, Clinical Trial Results, MDR-TB, Moxifloxacin, NC-002, PaMZ, Pretomanid/PA-824, Pyrazinamide

Bactericidal Activity of Pyrazinamide and Clofazimine Alone and in Combinations with Pretomanid and Bedaquiline

Publication: Diacon AH, Dawson R, von Groote-Bidlingmaier F, et. al. Bactericidal activity of pyrazinamide and clofazimine alone and in combinations with pretomanid and bedaquiline. Am J Respir Crit Care Med. 2015 Apr 15;191(8):943-53. doi: 10.1164/rccm.201410-1801OC.

4/2015

Tags: Bedaquiline (TMC-207), BPaZ, Clinical Development, Clinical Trial Results, Clofazamine, NC-003, Pretomanid/PA-824, Pyrazinamide, TB-HIV

Contribution of the Nitroimidazoles PA-824 and TBA-354 to the Activity of Novel Regimens in Murine Models of Tuberculosis

Publication: Tasneen R, Williams K, Amoabeng O, Minkowski A, Mdluli KE, Upton AM, Nuermberger EL. Contribution of the nitroimidazoles PA-824 and TBA-354 to the activity of novel regimens in murine models of tuberculosis. Antimicrob Agents Chemother. 2015 Jan;59(1):129

1/2015

Tags: Drug Discovery, Linezolid, Preclinical Data, Pretomanid/PA-824, Pyrazinamide, Sutezolid, 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

Effect of a high-calorie, high-fat meal on the bioavailability and pharmacokinetics of PA-824 in healthy adult subjects

Publication: Winter H, Ginsberg A, Egizi E, et. al. Effect of a High-Calorie, High-Fat Meal on the Bioavailability and Pharmacokinetics of PA-824 in Healthy Adult Subjects. Antimicrob Agents Chemother. 2013 Nov; 57(11): 5516–5520. doi: 10.1128/AAC.00798-13

11/2013

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

Potent rifamycin-sparing regimen cures guinea pig tuberculosis as rapidly as the standard regimen

Publication: Dutta NK, Alsultan A, Gniadek TJ, et. al. Potent rifamycin-sparing regimen cures guinea pig tuberculosis as rapidly as the standard regimen. Antimicrob Agents Chemother. 2013 Aug;57(8):3910-6. doi: 10.1128/AAC.00761-13.

8/2013

Tags: HRZE, Moxifloxacin, PaMZ, Preclinical Data, Pretomanid/PA-824, Pyrazinamide

Evaluation of pharmacokinetic interaction between PA-824 and midazolam in healthy adult subjects

Publication: Winter H, Egizi E, Erondu N, et. al. Evaluation of Pharmacokinetic Interaction between PA-824 and Midazolam in Healthy Adult Subjects. Antimicrob Agents Chemother. 2013 Aug; 57(8): 3699–3703.doi: 10.1128/AAC.02632-12

4/2013

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

Early bactericidal activity of new drug regimens for tuberculosis - Authors' reply

Publication: Diacon AH, Donald PR, Mendel CM. Early bactericidal activity of new drug regimens for tuberculosis - Authors' reply. Lancet. 2013 Jan 12;381(9861):112-3. doi: 10.1016/S0140-6736(13)60042-2.

1/2013

Tags: Clinical Development, Editorials, Moxifloxacin, NC-001, PaMZ, Pretomanid/PA-824, Pyrazinamide, Trial Design

Sterilizing Activities of Novel Combinations Lacking First- and Second-Line Drugs in a Murine Model of Tuberculosis

Publication: Williams K, Minkowski A, Amoabeng O, et. al. Sterilizing activities of novel combinations lacking first- and second-line drugs in a murine model of tuberculosis. Antimicrob Agents Chemother. 2012 Jun;56(6):3114-20. doi: 10.1128/AAC.00384-12.

4/2012

Tags: Bedaquiline (TMC-207), Clofazamine, Preclinical Data, Pretomanid/PA-824, Pyrazinamide, Rifapentine, Sutezolid

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

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

Sterilizing activity of novel TMC207- and PA-824-containing regimens in a murine model of tuberculosis

Publication: Tasneen R, Li SY, Peloquin CA, et. al. Sterilizing activity of novel TMC207- and PA-824-containing regimens in a murine model of tuberculosis. Antimicrob Agents Chemother. 2011 Dec;55(12):5485-92. doi: 10.1128/AAC.05293-11

9/2011

Tags: Bedaquiline (TMC-207), BPaZ, Clofazamine, Preclinical Data, Pretomanid/PA-824

14-day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial.

Publication: Diacon AH, Dawson R, von Groote-Bidlingmaier F, et. al. 14-day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial. Lancet. 2012 Sep 15;380(9846):986-93. doi: 10.1016/S0140-6736(12)61080-0.

9/2011

Tags: Bedaquiline (TMC-207), Clinical Development, Clinical Trial Results, MDR-TB, Moxifloxacin, NC-001, PaMZ, Pretomanid/PA-824, Pyrazinamide

Drugs in development for tuberculosis

Publication: Ginsberg AM, Drugs in development for tuberculosis. Drugs. 2010 Dec 3;70(17):2201-14. doi: 10.2165/11538170-000000000-00000.

12/2010

Tags: Advocacy, Bedaquiline (TMC-207), Clinical Development, Editorials, Global Pipeline, Pretomanid/PA-824, Rifapentine, TB Burden

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

Current development and future prospects in chemotherapy of tuberculosis

Publication: Nuermberger EL, Spigelman MK, Yew WW. Current development and future prospects in chemotherapy of tuberculosis. Respirology. 2010 Jul;15(5):764-78. doi: 10.1111/j.1440-1843.2010.01775.x.

7/2010

Tags: Bedaquiline (TMC-207), Clinical Development, Drug Discovery, Editorials, Global Pipeline, Moxifloxacin, Pretomanid/PA-824, TB Market

Global tuberculosis drug development pipeline: the need and the reality

Publication: Ma Z, Lienhardt C, McIlleron H, Nunn AJ, Wang X. Global tuberculosis drug development pipeline: the need and the reality. Lancet. 2010 Jun 12;375(9731):2100-9. doi: 10.1016/S0140-6736(10)60359-9.

5/2010

Tags: Advocacy, Bedaquiline (TMC-207), Biomarkers, Childhood TB, Clinical Development, Editorials, Global Pipeline, MDR-TB, Moxifloxacin, Policy, Pretomanid/PA-824, Rifapentine, Sutezolid, Trial Design

Early Bactericidal Activity and Pharmacokinetics of PA-824 in Smear-Positive Tuberculosis Patients (AAC01354-09)

Publication: Diacon AH, Dawson R, Hanekom M, et. al. Early bactericidal activity and pharmacokinetics of PA-824 in smear-positive tuberculosis patients. Antimicrob Agents Chemother. 2010 Aug;54(8):3402-7. doi: 10.1128/AAC.01354-09.