Cytochrome P450 2C8 (CYP2C8)-mediated hydroxylation of an endothelin ETA receptor antagonist in human liver microsomes

Drug Metabolism and Disposition

Volumn 32, Issue 5, 2004, Pages 473-478

  Ma, Bennett ^a   Subramanian, Raju ^a   Schrag, Michael L ^a   Rodrigues, A David ^b   Tang, Cuyue ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

^b BRISTOL MYERS SQUIBB   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

AMODIAQUINE; ANTIBODY; CYTOCHROME P450 2C8; ENDOTHELIN A RECEPTOR ANTAGONIST; OXYGENASE; PACLITAXEL; RECOMBINANT ENZYME;

AEROBIC METABOLISM; ARTICLE; CATALYSIS; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG HYDROXYLATION; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME DEGRADATION; HUMAN; HUMAN CELL; IN VITRO STUDY; INCUBATION TIME; LIVER MICROSOME METABOLISM; MICHAELIS CONSTANT; MICHAELIS MENTEN KINETICS; PRIORITY JOURNAL;

ARYL HYDROCARBON HYDROXYLASES; DOSE-RESPONSE RELATIONSHIP, DRUG; ETHERS; HUMANS; HYDROCARBONS, FLUORINATED; HYDROXYLATION; MICROSOMES, LIVER; RECEPTOR, ENDOTHELIN A;

EID: 2042546727     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.32.5.473     Document Type: Article

References (25)

1. Backman JT, Kyrklund C, Neuvonen M, and Neuvonen PJ (2002) Gemfibrozil greatly increases plasma concentrations of cerivastatin. Clin Pharmacol Ther 72:685-691.
2. Baldwin SJ, Clarke SE, and Chenery RJ (1999) Characterization of the cytochrome P450 enzymes involved in the in vitro metabolism of rosiglitazone. Br J Clin Pharmacol 48:424-432.
3. Becquemont L, Mouajjah S, Escaffre O, Beaune P, Funck-Brentano C, and Jaillon P (1999) Cytochrome P-450 3A4 and 2C8 are involved in zopiclone metabolism. Drug Metab Dispos 27:1068-1073.
4. Chatterjee P and Franklin MR (2003) Human cytochrome P450 inhibition and metabolic-intermediate complex formation by goldenseal extract and its methylenedioxyphenyl components. Drug Metab Dispos 31:1391-1397.
5. Dierks EA, Stams KR, Lim H-K, Cornelius G, Zhang H, and Ball SE (2001) A method for the simultaneous evaluation of the activities of several major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry. Drug Metab Dispos 29:23-29.
6. Klose TS, Blaisdell JA, and Goldstein JA (1999) Gene structure of CYP2C8 and extrahepatic distribution of the human CYP2Cs. J Biochem Mol Toxiocol 13:289-295.
7. Li X-Q, Björkman A, Andersson TB, Ridderström M, and Masimirembwa CM (2002) Amodiaquine clearance and its metabolism to N-desethylamodiaquine is mediated by CYP2C8: a new high affinity and turnover enzyme-specific probe substrate. J Pharmacol Exp Ther 300:399-407.
8. Ma B, Prueksaritanont T, and Lin JH (2000) Drug interactions with calcium channel blockers: possible involvement of metabolite-intermediate complexation with CYP3A. Drug Metab Dispos 28:125-130.
9. Mei Q, Tang C, Assang C, Lin Y, Slaughter D, Rodrigues AD, Baillie TA, Rushmore TH, and Shou M (1999) Role of a potent inhibitory monoclonal antibody to cytochrome P-450 3A4 in assessment of human drug metabolism. J Pharmacol Exp Ther 291:749-759.
10. Mei Q, Tang C, Lin Y, Rushmore TH, and Shou M (2002) Inhibition kinetics of monoclonal antibodies against cytochrome P450. Drug Metab Dispos 30:701-708.
11. Murray M and Reidy GF (1990) Selectivity in the inhibition of mammalian cytochromes P-450 by chemical agents. Pharmacol Rev 42:85-101.
12. Newton DJ, Wang RW, and Lu AYH (1995) Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab Dispos 23:154-158.
13. Ohyama K, Nakajima M, Nakamura S, Shimada N, Yamazakj H, and Yokoi T (2000) A significant role of human cytochrome P450 2C8 in amiodarone N-deethylation: an approach to predict the contribution with relative activity factor. Drug Metab Dispos 28:1303-1310.
14. A receptor antagonist, J-105859. J Hypertension 18:1815-1823.
15. Ong C-E, Coulter S, Birkett DJ, Bhasker CR, and Miners JO (2000) The xenobiotic inhibitor profile of cytochrome P4502C8. Br J Clin Pharmacol 50:573-580.
16. Prueksaritanont T, Zhao JJ, Ma B, Roadcap BA, Tang C, Qiu Y, Liu L, Lin JH, Pearson PG, and Baillie TA (2002) Mechanistic studies on metabolic interactions between gemfibrozil and statins. J Pharmacol Exp Ther 301:1042-1051.
17. Rahman A, Korzekwa KR, Grogan J, Gonzalez FJ, and Harris JW (1994) Selective biotransformation of taxol to 6α-hydroxytaxol by human cytochrome P450 2C8. Cancer Res 54:5543-5556.
18. Rendic S (2002) Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev 34:83-448.
19. Rodrigues AD and Rushmore TH (2002) Cytochrome P450 pharmacogenetics in drug development: in vitro studies and clinical consequences. Curr Drug Metab 3:289-309. [Erratum in: Curr Drug Metab 3:559.]
20. Sai Y, Dai R, Yant TJ, Krausz KW, Gonzalez FJ, Gelboin HV, and Shou M (2000) Assessment of specificity of eight chemical inhibitors using cDNA-expressed cytochromes P450. Xenobiotica 30:327-343.
21. Suzuki H, Kneller MB, Haining RL, Trager WF, and Rettie AE (2002) (+)-N-3-Benzyl-nirvanol and (-)-N-3-benzyl-phenobarbital: new potent and selective in vitro inhibitors of CYP2C19. Drug Metab Dispos 30:235-239.
22. A receptor antagonist in human liver microsomes. Drug Metab Dispos 31:37-45.
23. Tracy TS, Korzekwa KR, Gonzalez FJ, and Wainer IW (1999) Cytochrome P450 isoforms involved in metabolism of the enantiomers of verapamil and norverapamil. Br J Clin Pharmacol 47:545-552.
24. Wang J-S, Neuvonen M, Wen X, Backman JT, and Neuvonen PJ (2002) Gemfibrozil inhibits CYP2C8-mediated cerivastatin metabolism in human liver microsomes. Drug Metab Dispos 30:1352-1356.
25. Yamazaki H, Shibata A, Suzuki M, Nakajima M, Shimada N, Guengerich FP, and Yokoi T (1999) Oxidation of troglitazone to a quinone-type metabolite catalyzed by cytochrome P-450 2C8 and P-450 3A4 in human liver microsomes. Drug Metab Dispos 27:1260-1266.