Factors confounding the successful extrapolation of in vitro CYP3A inhibition information to the in vivo condition

European Journal of Pharmaceutical Sciences

Volumn 15, Issue 3, 2002, Pages 239-242

  Wienkers, Larry C ^a  

^a PFIZER INC   (United States)

Author keywords

CYP inhibition; In vitro in vivo

Indexed keywords

ENZYMES; EXTRAPOLATION; METABOLISM; OXIDATION; PHARMACOKINETICS;

DRUG-DRUG INTERACTIONS;

DRUG PRODUCTS;

ARTEETHER; BROTIZOLAM; BUPRENORPHINE; CYTOCHROME P450; CYTOCHROME P450 3A; CYTOCHROME P450 3A4; CYTOCHROME P450 ISOENZYME; DIHYDROARTEMISININ; HYDROCORTISONE; MIDAZOLAM; QUINIDINE; SILDENAFIL; TERFENADINE; TRIAZOLAM; VINBLASTINE;

CATALYSIS; DRUG DEVELOPMENT; DRUG INTERACTION; DRUG METABOLISM; DRUG OXIDATION; ENZYME INDUCTION; ENZYME INHIBITION; ENZYME SUBSTRATE; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MICHAELIS MENTEN KINETICS; PREDICTION; PRIORITY JOURNAL; REVIEW;

EID: 0036118686     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(02)00002-7     Document Type: Note

References (39)

1. Cortisol metabolism in vitro-III. Inhibition of microsomal 6 beta-hydroxylase and cytosolic 4-ene-reductase
2. Allosteric behavior in cytochrome p450-dependent in vitro drug-drug interactions: a prospective based on conformational dynamics
3. Use of in vitro and in vivo data to estimate the likelihood of metabolic pharmacokinetic interactions
4. Warfarin-fluconazole. II. A metabolically based drug interaction: in vivo studies
5. Biotransformation of tirilazad in human: 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability
6. Effect of inhibitor depletion on inhibitory potency: tight binding inhibition of CYP3A by clotrimazole
7. Metabolism of artelinic acid to dihydroqinqhaosu by human liver cytochrome P4503A
8. Metabolism of beta-arteether to dihydroqinghaosu by human liver microsomes and recombinant cytochrome P450
9. Common and uncommon cytochrome P450 reactions related to metabolism and chemical toxicity
10. Analysis of human cytochrome P450 3A4 cooperativity: Construction and characterization of a site-directed mutant that displays hyperbolic steroid hydroxylation kinetics
11. The mechanism of the interaction between amiodarone and warfarin in humans
12. Elucidation of distinct ligand binding sites for cytochrome P450 3A4
13. In vitro-in vivo scaling of CYP kinetic data not consistent with the classical Michaelis-Menten model
14. Dapsone activation of CYP2C9-mediated metabolism: evidence for activation of multiple substrates and a two-site model
15. Identification of the cytochrome P450 enzymes involved in the N-demethylation of sildenafil
16. High rates of substrate hydroxylation by human cytochrome P450 3A4 in reconstituted membranous vesicles: influence of membrane charge
17. Involvement of cytochrome P450 3A4 in N-dealkylation of buprenorphine in human liver microsomes
18. CYP3A4 drug interactions: correlation of 10 in vitro probe substrates
19. Warfarin-fluconazole. I. Inhibition of the human cytochrome P450-dependent metabolism of warfarin by fluconazole: in vitro studies
20. Substrate inhibition kinetics for cytochrome P450-catalyzed reactions
21. In vitro metabolism of quinidine: The (3S)-3-hydroxylation of quinidine is a specific marker reaction for cytochrome P-4503A4 activity in human liver microsomes
22. Prediction of human clearance of twenty-nine drugs from hepatic microsomal intrinsic clearance data: An examination of in vitro half-life approach and nonspecific binding to microsomes
23. Rapid equilibrium partial and mixed-type inhibition
24. Identification of human cytochrome P450 isoforms involved in the metabolism of brotizolam
25. Covalent alteration of the CYP3A4 active site: evidence for multiple substrate binding domains
26. Triazolam substrate inhibition: evidence of competition for heme-bound reactive oxygen within the CYP3A4 active site
27. Topological alteration of the CYP3A4 active site by the divalent cation Mg(2+)
28. Activation of CYP3A4: evidence for the simultaneous binding of two substrates in a cytochrome P450 active site
29. In vitro and in vivo drug interactions involving human CYP3A
30. Extrapolating concentrations-in vitro to in vivo
31. Cooperativity in oxidations catalyzed by cytochrome P450 3A4
32. Triazolam biotransformation by human liver microsomes in vitro: effects of metabolic inhibitors and clinical confirmation of a predicted interaction with ketoconazole
33. Inhibition of terfenadine metabolism in vitro by azole antifungal agents and by selective serotonin reuptake inhibitor antidepressants: relation to pharmacokinetic interactions in vivo
34. Human cytochrome P-450 3A4: In vitro drug-drug interaction patterns are substrate dependent
35. Biotransformation of tirilazad in human: 1. Cytochrome P450 3A-mediated hydroxylation of tirilazad mesylate in human liver microsomes
36. Assessment of potential interactions between dopamine receptor agonists and various human cytochrome P450 enzymes using a simple in vitro inhibition screen
37. Lack of electron transfer from cytochrome b5 in stimulation of catalytic activities of cytochrome P450 3A4. Characterization of a reconstituted cytochrome P450 3A4/NADPH-cytochrome P450 reductase system and studies with apo-cytochrome b5
38. Involvement of human liver cytochrome P450 3A in vinblastine metabolism: drug interactions