Evaluation of time-dependent inactivation of CYP3A in cryopreserved human hepatocytes

Drug Metabolism and Disposition

Volumn 33, Issue 6, 2005, Pages 853-861

  Zhao, Ping ^a   Kunze, Kent L ^b   Lee, Caroline A ^a  

^a PFIZER INC   (United States)

^b UNIVERSITY OF WASHINGTON   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 (6,7 DIMETHOXY 3,4 DIHYDROISOQUINOLIN 2(1H) YL) N [2 (3,4 DIMETHOXYPHENYL)ETHYL] 6,7 DIMETHOXYQUINAZOLIN 2 AMINE; AMPRENAVIR; CP 100356; CYTOCHROME P450 3A; DICLOFENAC; DILTIAZEM; ERYTHROMYCIN; GLYCOPROTEIN P INHIBITOR; KETOCONAZOLE; RALOXIFENE; TROLEANDOMYCIN; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; CELL TRANSFER; CONTROLLED STUDY; CRYOPRESERVATION; DRUG POTENCY; DRUG STRUCTURE; ENZYME INACTIVATION; ENZYME INHIBITION; ENZYME KINETICS; HUMAN; HUMAN CELL; IC 50; LIVER CELL; LIVER MICROSOME; PRIORITY JOURNAL;

CRYOPRESERVATION; CYTOCHROME P-450 ENZYME SYSTEM; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; FEMALE; HEPATOCYTES; HUMANS; LIVER; MALE; TIME FACTORS;

EID: 18844445670     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.104.002832     Document Type: Article

References (28)

1. Banker MJ, Clark TH, and Williams JA (2003) Development and validation of a 96-well equilibrium dialysis apparatus for measuring plasma protein binding. J Pharm Sci 92:967-974.
2. Chen Q, Ngui JS, Doss GA, Wang RW, Cai X, DiNinno FP, Blizzard TA, Hammond ML, Stearns RA, Evans DC, et al. (2002) Cytochrome P450 3A4-mediated bioactivation of raloxifene: irreversible enzyme inhibition and thiol adduct formation. Chem Res Toxicol 15:907-914.
3. Choo EF, Leake B, Wandel C, Imamura H, Wood AJ, Wilkinson GR, and Kim RB (2000) Pharmacological inhibition of P-glycoprotein transport enhances the distribution of HIV-I protease inhibitors into brain and testes. Drug Metab Dispos 28:655-660.
4. th North American ISSX Meeting. Providence, RI. Drug Metab Rev 35 (Suppl 2):341.
5. th North American ISSX Meeting. Providence, RI. Drug Metab Rev 35 (Suppl 2):339.
6. Gibbs MA, Kunze KL, Howald WN, and Thummel KE (1999a) Effect of inhibitor depletion on inhibitory potency: tight binding inhibition of CYP3A by clotrimazole. Drug Metab Dispos 27:596-569.
7. Gibbs MA, Thummel KE, Shen DD, and Kunze KL (1999b) Inhibition of cytochrome P-450 3A (CYP3A) in human intestinal and liver microsomes: comparison of Ki values and impact of CYP3A5 expression. Drug Metab Dispos 27:180-187.
8. Habig WH, Pabst MJ, and Jakoby WB (1974) Glutathione S-transferases: the first enzymatic step in mercapturic acid formation. J Biol Chem 240:7130-7139.
9. Huang L, Wring SA, Woolley JL, Brouwer KR, Serabjit-Singh C, and Polli JW (2001) Induction of P-glycoprotein and cytochrome P450 3A by HIV protease inhibitors. Drug Metab Dispos 29:754-760.
10. Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, and Sugiyama Y (1998) Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver. Pharmacol Rev 50:387-412.
11. Ito K, Ogihara K, Kanamitsu S, and Itoh T (2003) Prediction of the in vivo interaction between midazolam and macrolides based on in vitro studies using human liver microsomes. Drug Metab Dispos 31:945-954.
12. Jones DR, Gorski JC, Hamman MA, Mayhew BS, Rider S, and Hall SD (1999) Diltiazem inhibition of cytochrome P-450 3A activity is due to metabolite intermediate complex formation. J Pharmacol Exp Ther 290:1116-1125.
13. Kanamitsu S, Ito K, Green CE, Tyson CA, Shimada N, and Sugiyama Y (2000) Prediction of in vivo interaction between triazolam and erythromycin based on in vitro studies using human liver microsomes and recombinant human CYP3A4. Pharm Res (NY) 17:419-426.
14. Kemp DC, Fan PW, and Stevens JC (2002) Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance. Drug Metab Dispos 30:694-700.
15. Kitz R and Wilson IB (1962) Esters of methanesulfonic acid as irreversible inhibitors of acetylcholinesterase. J Biol Chem 237:3245-3249.
16. Kosuge K, Nishimoto M, Kimura M, Umemura K, Nakashima M, and Ohashi K (1997) Enhanced effect of triazolam with diltiazem. Br J Clin Pharmacol 43:367-372.
17. Lam JL and Benet LZ (2004) Hepatic microsome studies are insufficient to characterize in vivo hepatic metabolic clearance and metabolic drug-drug interactions: studies of digoxin metabolism in primary rat hepatocytes versus microsomes. Drug Metab Dispos 32:1311-1316.
18. Lin JH and Lu AY (1998) Inhibition and induction of cytochrome P450 and the clinical implications. Clin Pharmacokinet 35:361-390.
19. th International Conference on Drug-Drug Interactions, San Diego, CA, June 23-25, 2003. Institute for Scientific Exchange, Inc., Baltimore, MD.
20. Masubuchi Y, Ose A, and Horie T (2002) Diclofenac-induced inactivation of CYP3A4 and its stimulation by quinidine. Drug Metab Dispos 30:1143-1148.
21. Mayhew BS, Jones DR, and Hall SD (2000) An in vitro model for predicting in vivo inhibition of cytochrome P450 3A4 by metabolic intermediate complex formation. Drug Metab Dispos 28:1031-1037.
22. Obach RS (1997) Nonspecific binding to microsomes: impact on scale-up of in vitro intrinsic clearance to hepatic clearance as assessed through examination of warfarin, imipramine and propranolol. Drug Metab Dispos 25:1359-1369.
23. Periti P, Mazzei T, Mini E, and Novelli A (1992) Pharmacokinetic drug interactions of macrolides. Clin Pharmacokinet 23:106-131.
24. Polli JW, Jarrett JL, Studenberg SD, Humphreys JE, Dennis SW, Brouwer KR, and Woolley JL (1999) Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor. Pharm Res (NY) 16:1206-1212.
25. Roelofsen H, Bakker CT, Schoemaker B, Heijn M, Jansen PL, and Elferink RP (1995) Redistribution of canalicular organic anion transport activity in isolated and cultured rat hepatocytes. Hepatology 21:1649-1657.
26. Treluyer JM, Bowers G, Cazali N, Sonnier M, Rey E, Pons G, and Cresteil T (2003) Oxidative metabolism of amprenavir in the human liver. Effect of the CYP3A maturation. Drug Metab Dispos 31:275-281.
27. Wandel C, Kim RB, Kajiji S, Guengerich FP, Wilkinson GR, and Wood AJJ (1999) P-Glycoprotein and cytochrome P-450 3A inhibition: dissociation of inhibitory potencies. Cancer Res 59:3944-3948.
28. th North American ISSX Meeting. Providence, RI. Drug Metab Rev 35 (Suppl 2):353.