Bedaquiline metabolism: Enzymes and novel metabolitess

Drug Metabolism and Disposition

Volumn 42, Issue 5, 2014, Pages 863-866

  Liu, Ke ^a   Li, Feng ^a   Lu, Jie ^a   Liu, Shinlan ^a   Dorko, Kenneth ^a   Xie, Wen ^a   Ma, Xiaochao ^a  

^a Universigy of Pittsburgh   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ALDEHYDE DERIVATIVE; BEDAQUILINE; CYTOCHROME P450 2C19; CYTOCHROME P450 2C8; CYTOCHROME P450 3A4; CYP2C19 PROTEIN, HUMAN; CYP2C8 PROTEIN, HUMAN; CYP3A4 PROTEIN, HUMAN; CYTOCHROME P450 3A; QUINOLINE DERIVATIVE; TUBERCULOSTATIC AGENT; UNSPECIFIC MONOOXYGENASE;

ARTICLE; CONTROLLED STUDY; DEMETHYLATION; DRUG INTERACTION; DRUG METABOLISM; ENZYME KINETICS; HUMAN; HUMAN CELL; LIVER CELL; METABOLOMICS; PREDICTION; PRIORITY JOURNAL; CELL CULTURE; DEALKYLATION; DRUG EFFECTS; ENZYMOLOGY; GENETICS; LIVER MICROSOME; METABOLISM; METHYLATION; TUBERCULOSIS, MULTIDRUG-RESISTANT;

ANTITUBERCULAR AGENTS; ARYL HYDROCARBON HYDROXYLASES; CELLS, CULTURED; CYTOCHROME P-450 CYP2C19; CYTOCHROME P-450 CYP2C8; CYTOCHROME P-450 CYP3A; DEALKYLATION; DIARYLQUINOLINES; HEPATOCYTES; HUMANS; METABOLOMICS; METHYLATION; MICROSOMES, LIVER; TUBERCULOSIS, MULTIDRUG-RESISTANT;

EID: 84898797220     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.113.056119     Document Type: Article

References (18)

1. Chang KC and Yew WW (2013) Management of difficult multidrug-resistant tuberculosis and extensively drug-resistant tuberculosis: update 2012. Respirology 18:8-21.
2. Cole ST and Alzari PM (2005) Microbiology. TB-a new target, a new drug. Science 307: 214-215.
3. Cuyckens F, Balcaen LI, De Wolf K, De Samber B, Van Looveren C, Hurkmans R, and Vanhaecke F (2008) Use of the bromine isotope ratio in HPLC-ICP-MS and HPLC-ESIMS analysis of a new drug in development. Anal Bioanal Chem 390:1717-1729.
4. Diacon AH, Donald PR, Pym A, Grobusch M, Patientia RF, Mahanyele R, Bantubani N, Narasimooloo R, De Marez T, and van Heeswijk R, et al. (2012) Randomized pilot trial of eight weeks of bedaquiline (TMC207) treatment for multidrug-resistant tuberculosis: long-term outcome, tolerability, and effect on emergence of drug resistance. Antimicrob Agents Chemother 56:3271-3276.
5. Diacon AH, Pym A, Grobusch M, Patientia R, Rustomjee R, Page-Shipp L, Pistorius C, Krause R, Bogoshi M, and Churchyard G, et al. (2009) The diarylquinoline TMC207 for multidrugresistant tuberculosis. N Engl J Med 360:2397-2405.
6. FDA (2012a) Briefing Package: NDA 204-384: Sirturo, Division of Anti-Infective Products, Office of Antimicrobial Products, US Food and Drug Administration Center for Drug Evaluation, Silver Spring, MD.
7. FDA (Press release, December 31, 2012b) FDA Approves First Drug to Treat Multidrug-Resistant Tuberculosis. US Food and Drug Administration, Silver Spring, MD.
8. Gerbal-Chaloin S, Pascussi JM, Pichard-Garcia L, Daujat M, Waechter F, Fabre JM, Carrère N, and Maurel P (2001) Induction of CYP2C genes in human hepatocytes in primary culture. Drug Metab Dispos 29:242-251.
9. Janssen Pharmaceutical Companies (2012) Briefing Document, TMC207 (Bedaquiline), Treatment of Patients with MDR-TB, NDA 204-384, Janssen Pharmaceutical Companies, Titusville, NJ.
10. Li F, Lu J, Wang L, and Ma X (2011) CYP3A-mediated generation of aldehyde and hydrazine in atazanavir metabolism. Drug Metab Dispos 39:394-401.
11. Luo G, Cunningham M, Kim S, Burn T, Lin J, Sinz M, Hamilton G, Rizzo C, Jolley S, and Gilbert D, et al. (2002) CYP3A4 induction by drugs: correlation between a pregnane X receptor reporter gene assay and CYP3A4 expression in human hepatocytes. Drug Metab Dispos 30:795-804.
12. Ma X, Chen C, Krausz KW, Idle JR, and Gonzalez FJ (2008) A metabolomic perspective of melatonin metabolism in the mouse. Endocrinology 149:1869-1879.
13. Meermann B, Bockx M, Laenen A, Van Looveren C, Cuyckens F, and Vanhaecke F (2012) Speciation analysis of bromine-containing drug metabolites in feces samples from a human in vivo study by means of HPLC/ICP-MS combined with on-line isotope dilution. Anal Bioanal Chem 402:439-448.
14. Mesens N, Verbeeck J, and Rouan M (2007) Elucidating the role of M2 in the preclinical safety profile of TMC207, in 38th World Conference on Lung Health of the International Union Against Tuberculosis and Lung Disease; 2007 Nov 8-12; Cape Town, South Africa.
15. Mukherjee JS, Rich ML, Socci AR, Joseph JK, Virú FA, Shin SS, Furin JJ, Becerra MC, Barry DJ, and Kim JY, et al. (2004) Programmes and principles in treatment of multidrug-resistant tuberculosis. Lancet 363:474-481.
16. O'Brien PJ, Siraki AG, and Shangari N (2005) Aldehyde sources, metabolism, molecular toxicity mechanisms, and possible effects on human health. Crit Rev Toxicol 35:609-662.
17. Uchida K (2000) Role of reactive aldehyde in cardiovascular diseases. Free Radic Biol Med 28: 1685-1696.
18. World Health Organization (2013) The Use of Bedaquiline in the Treatment of Multidrug-Resistant Tuberculosis: Interim Policy Guidance, World Health Organization, Geneva, Switzerland.