A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes

Drug Metabolism and Disposition

Volumn 33, Issue 9, 2005, Pages 1304-1311

  Riley, Robert J ^a   McGinnity, D F ^a   Austin, R P ^a  

^a ASTRAZENECA   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

BUSPIRONE; CARVEDILOL; CHLORPROMAZINE; CIMETIDINE; DESIPRAMINE; DICLOFENAC; DIFLUNISAL; DILTIAZEM; ETODOLAC; FABESETRON; FENOPROFEN; FUROSEMIDE; GEMFIBROZIL; GLIPIZIDE; GRANISETRON; IBUPROFEN; IMIPRAMINE; INDOMETACIN; IRBESARTAN; KETOPROFEN; LIDOCAINE; MONTELUKAST; N [1 (2 FLUOROPHENYL) 3,4,6,7 TETRAHYDRO 4 OXOPYRROLO[3,2,1 JK][1,4]BENZODIAZEPIN 3 YL] 1H INDOLE 2 CARBOXAMIDE; OXAPROZIN; TENOXICAM; TOLBUTAMIDE; TROGLITAZONE; UNINDEXED DRUG; WARFARIN; ZIDOVUDINE;

ANALYTICAL ERROR; ARTICLE; BLOOD; CALCULATION; CATTLE; CONTROLLED STUDY; DRUG CLEARANCE; EVALUATION; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; INFORMATION; LABORATORY; LIVER; LIVER CELL; LIVER CLEARANCE; METABOLISM; MICROSOME; MODEL; PREDICTION; PRIORITY JOURNAL; SERUM; TECHNIQUE;

ANIMALS; CATTLE; CELLS, CULTURED; CULTURE MEDIA, CONDITIONED; CULTURE MEDIA, SERUM-FREE; HEPATOCYTES; HUMANS; LIVER; METABOLIC CLEARANCE RATE; MICROSOMES; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS;

ANIMALIA;

EID: 23944451585     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.004259     Document Type: Article

References (30)

1. Andersson TB, Bredberg E, Ericsson H, and Sjoberg H (2004) An evaluation of in vitro metabolism data for predicting the clearance and drug-drug interaction potential of CYP2C9 substrates. Drug Metab Dispos 32:715-721.
2. Austin RP, Barton P, Cockroft SL, Wenlock MC, and Riley RJ (2002) The influence of nonspecific microsomal binding on apparent intrinsic clearance and its prediction from physicochemical properties. Drug Metab Dispos 30:1497-1503.
3. Austin RP, Barton P, Mohmed S, and Riley RJ (2005) The binding of drugs to hepatocytes and its relationship to physicochemical properties. Drug Metab Dispos 33:419-425.
4. Blanchard N, Alexandre E, Abadie C, Lave T, Heyd B, Mantion G, Jaeck D, Richert L, and Coassolo P (2005) Comparison of clearance predictions using primary cultures and suspensions of human hepatocytes. Xenobiotica 35:1-15.
5. Boxenbaum H (1982) Interspecies scaling, allometry, physiological time and the ground plan of pharmacokinetics. J Pharmacokinet Biopharm 10:201-227.
6. Carlile DJ, Hakooz N, Baylss MK, and Houston JB (1999) Microsomal prediction of in vivo clearance of CYP2C9 substrates in humans. Br J Clin Pharmacol 47:625-635.
7. Davis AM and Riley RJ (2004) Predictive ADMET studies: the challenges and the opportunities. Curr Opin Chem Biol 8:378-386.
8. Houston JB (1984) Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochem Pharmacol 47:1469-1479.
9. Houston BJ and Carlile DJ (1997) Prediction of hepatic clearance from microsomes, hepatocytes and liver slices. Drug Metab Rev 29:891-922.
10. Houston JB and Galetin A (2004) Progress towards prediction of human pharmacokinetic parameters from in vitro technologies. Drug Metab Rev 35:393-415.
11. Ito K and Houston JB (2004) Comparison of the use of liver models for predicting drug clearance using in vitro kinetic data from hepatic microsomes and isolated hepatocytes. Pharm Res (NY) 21:785-792.
12. Iwatsubo, Hirota N, Ooie T, Suzuki H, Shimada N, Chiba K, Ishizaki T, Green CE, Tyson CA, and Sugiyama Y (1997) Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data. Pharmacol Ther 73:147-171.
13. Lau YY, Sapidou E, Cui X, White RE, and Cheng KC (2002) Development of a novel in vitro model to predict hepatic clearance using fresh, cryopreserved and sandwich-cultured hepatocytes. Drug Metab Dispos 30:1446-1454.
14. Lave T, Dupin S, Schmitt C, Chou RC, Jaeck D, and Coassolo P (1997a) Integration of in vitro data into allometric scaling to predict hepatic metabolic clearance in man: application to 10 extensively metabolized drugs. J Pharm Sci 86:584-590.
15. Lave T, Dupin S, Schmitt C, Valles B, Ubeaud G, Chou RC, Jaeck D, and Coassolo P (1997b) The use of human hepatocytes to select compounds based on their expected hepatic extraction ratios in humans. Pharm Res (NY) 14:152-155.
16. Li AP, Lu C, Brent JA, Pham C, Fackett A, Ruegg CE, and Silber PM (1999) Cryopreserved human hepatocytes: characterization of drug-metabolizing activities and applications in higher throughput screening assays for hepatotoxicity, metabolic stability and drug-drug interaction potential. Chem-Biol Interact 121:17-35.
17. Lin HJ, Chiba M, and Baillie TA (1999) Is the role of the small intestine in first-pass metabolism overemphasized? Pharmacol Rev 51:135-157.
18. Liu L and Pang KS (2005) The roles of transporters and enzymes in hepatic drug processing. Drug Metab Dispos 33:1-9.
19. McGinnity DF, Soars MG, Urbanowicz RA, and Riley RJ (2004) Evaluation of fresh and cryopreserved hepatocytes as in vitro drug metabolism tools for the prediction of metabolic clearance. Drug Metab Dispos 32:1247-1253.
20. Nagilla R and Ward KW (2004) A comprehensive analysis of the role of correction factors in the allometric predictivity of clearance from rat, dog and monkey to humans. J Pharm Sci 93:2522-2534.
21. Naritomi Y, Terashita S, Kagayama A, and Sugiyama Y (2003) Utility of hepatocytes in predicting drug metabolism: comparison of hepatic intrinsic clearance in rats and humans in vivo and in vitro. Drug Metab Dispos 31:580-588.
22. Naritomi Y, Terashita S, Kimura S, Suzuki A, Kagayama A, and Sugiyama Y (2001) Prediction of human hepatic clearance from in vivo animal experiments and in vitro metabolic studies with liver microsomes from animals and humans. Drug Metab Dispos 29:1316-1324.
23. Obach RS (1999) 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. Drug Metab Dispos 27:1350-1359.
24. Obach RS, Baxter JG, Liston TE, Silber BM, Jones BC, MacIntyre F, Rance DJ, and Wastall P (1997) The prediction of human pharmacokinetic parameters from preclinical and in vitro metabolism data. J Pharmacol Exp Ther 283:46-58.
25. Riley RJ and Kenna JG (2004) Cellular models for ADMET predictions and evaluation of drug-drug interactions. Curr Opin Drug Discov Dev 7:86-99.
26. Schneider G, Coassolo P, and Lave T (1999) Combining in vitro and in vivo pharmacokinetic data for prediction of hepatic drug clearance in humans by artificial neural networks and multivariate statistical techniques. J Med Chem 42:5072-5076.
27. Shibata Y, Takahashi H, Chiba M, and Ishii Y (2002) Prediction of hepatic clearance and availability by cryopreserved human hepatocytes: an application of serum incubation method. Drug Metab Dispos 30:892-896.
28. Shitara Y, Li AP, Kato Y, Lu C, Ito K, Itoh T, and Sugiyama Y (2003) Function of uptake transporters for taurocholate and estradiol 17-b-D-glucuronide in cryopreserved hepatocytes. Drug Metab Pharmacokinet 18:33-41.
29. Shitara Y, Sato H, and Sugiyama Y (2005) Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol 45:689-723.
30. Theil F-P, Guentert TW, Haddad S, and Poulin P (2003) Utility of physiologically based pharmacokinetic models to drug development and rational drug discovery candidate selection. Toxicol Lett 138:29-49.