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

Antimicrobial Agents and Chemotherapy

Volumn 57, Issue 11, 2013, Pages 5516-5520

  Winter, Helen ^a   Ginsberg, Ann ^b   Egizi, Erica ^b   Erondu, Ngozi ^b   Whitney, Karl ^c   Pauli, Elliott ^c   Everitt, Daniel ^b  

^a UNIVERSITY OF OTAGO   (New Zealand)

^b Global Alliance for TB Drug Development   (United States)

^c RTI INTERNATIONAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

6,7 DIHYDRO 2 NITRO 6 (4 TRIFLUOROMETHOXYBENZYLOXY) 5H IMIDAZO[2,1 B][1,3]OXAZINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; CROSSOVER PROCEDURE; DIARRHEA; DIET; DIET RESTRICTION; DIZZINESS; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG ELIMINATION; DRUG EXPOSURE; DRUG HALF LIFE; DRUG SAFETY; DRUG TOLERABILITY; FEMALE; GASTROINTESTINAL PAIN; HEADACHE; HIGH CALORIE DIET; HUMAN; HUMAN EXPERIMENT; KIDNEY CLEARANCE; LIPID DIET; MALE; MAXIMUM PLASMA CONCENTRATION; NAUSEA; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; PLASMA CONCENTRATION-TIME CURVE; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SINGLE DRUG DOSE; TIME TO MAXIMUM PLASMA CONCENTRATION;

ADMINISTRATION, ORAL; ADULT; ANTITUBERCULAR AGENTS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CROSS-OVER STUDIES; DIETARY FATS; DRUG ADMINISTRATION SCHEDULE; FASTING; FEMALE; FOOD-DRUG INTERACTIONS; HEALTHY VOLUNTEERS; HUMANS; MALE; MIDDLE AGED; NITROIMIDAZOLES;

EID: 84885909128     PISSN: 00664804     EISSN: 10986596     Source Type: Journal    
DOI: 10.1128/AAC.00798-13     Document Type: Article

References (10)

1. Lenaerts AJ, Gruppo V, Marietta KS, Johnson CM, Driscoll DK, Tompkins NM, Rose JD, Reynolds RC, Orme IM. 2005. Preclinical testing of the nitroimidazopyran PA-824 for activity against Mycobacterium tuberculosis in a series of in vitro and in vivo models. Antimicrob. Agents Chemother. 49:2294-2301.
2. Singh R, Manjunatha U, Boshoff HI, Ha YH, Niyomrattanakit P, Ledwidge R, Dowd CS, Lee IY, Kim P, Zhang L, Kang S, Keller TH, Jiricek J, Barry CE. 2008. PA-824 kills nonreplicating Mycobacterium tuberculosis by intracellular NO release. Science 322:1392-1395.
3. Stover CK, Warrener P, VanDevanter DR, Sherman DR, Arain TM, Langhorne MH, Anderson SW, Towell JA, Yuan Y., McMurray DN, Kreiswirth BN, Barry CE, Baker WR. 2000. A small-molecule nitroimidazopyran drug candidate for the treatment of tuberculosis. Nature 405:962-966.
4. Nuermberger E, Tyagi S, Tasneen R, Williams KN, Almeida D, Rosenthal I, Grosset JH. 2008. Powerful bactericidal and sterilizing activity of a regimen containing PA-824, moxifloxacin, and pyrazinamide in a murine model of tuberculosis. Antimicrob. Agents Chemother. 52: 1522-1524.
5. Diacon AH, Dawson R, Hanekom M, Narunsky K, Maritz SJ, Venter A, Donald PR, van Niekerk C, Whitney K, Rouse DJ, Laurenzi MW, Ginsberg AM, Spigelman MK. 2010. Early bactericidal activity and pharmacokinetics of PA-824 in smear-positive tuberculosis patients. Antimicrob. Agents Chemother. 54:3402-3407.
6. Diacon AH, Dawson R, du Bois J, Narunsky K, Venter A, Donald PR, van Niekerk C, Erondu N, Ginsberg AM, Becker P, Spigelman MK. 2012. Phase II dose-ranging trial of the early bactericidal activity of PA-824. Antimicrob. Agents Chemother. 56:3027-3031.
7. Diacon AH, Dawson R, von Grotte-Bidlingmaier F, Symons G, Venter A, Donald PR, van Niekerk C, Everitt D, Winter H, Becker P, Mendel C, Spigelman MK. 2012. 14-Day bactericidal activity of PA-824, bedaquiline, pyrazinamide, and moxifloxacin combinations: a randomised trial. Lancet 380:986-993.
8. Ginsberg AM, Laurenzi MW, Rouse DJ, Whitney K, Spigelman MK. 2009. Safety, tolerability, and pharmacokinetics of PA-824 in healthy subjects. Antimicrob. Agents Chemother. 53:3720-3725.
9. U.S. Department of Health and Human Services and Food and Drug Administration, Center for Drug Evaluation and Research. 2002. Guidance for industry: food-effect bioavailability and fed bioequivalence studies. Office of Training and Communications, Division of Drug Information, document HFD-240. DHHS and FDA, CDER, Washington, DC.
10. Ginsberg AM, Laurenzi MW, Rouse DJ, Whitney KD, Spigelman MK. 2009. Assessment of the effects of the nitroimidazo-oxazine PA-824 on renal function in healthy subjects. Antimicrob. Agents Chemother. 53: 3726-3733.