Practical use of the regression offset approach for the prediction of in vivo intrinsic clearance from hepatocytes

Xenobiotica

Volumn 42, Issue 9, 2012, Pages 841-853

  Sohlenius Sternbeck, Anna Karin ^a   Jones, Christopher ^b   Ferguson, Douglas ^b   Middleton, Brian J ^b   Projean, Denis ^b   Floby, Eva ^a   Bylund, Johan ^a,c   Afzelius, Lovisa ^a  

^a ASTRAZENECA R AND D   (Sweden)

^b ASTRAZENECA   (United Kingdom)

^c UPPSALA UNIVERSITY   (Sweden)

Author keywords

CLint; hepatocytes; in vitro to in vivo scaling; Liver; metabolism; regression offset; well stirred model

Indexed keywords

BUFURALOL; CAFFEINE; CARVEDILOL; CHLORPROMAZINE; CLOZAPINE; DESIPRAMINE; DIAZEPAM; DICLOFENAC; DIFLUNISAL; DILTIAZEM; ETODOLAC; FENOPROFEN; GEMFIBROZIL; GLIPIZIDE; GRANISETRON; IBUPROFEN; IMIPRAMINE; IRBESARTAN; KETOPROFEN; METHYLPREDNISOLONE; METOPROLOL; MIDAZOLAM; NALOXONE; OMEPRAZOLE; ONDANSETRON; OXAPROZIN; OXAZEPAM; PARACETAMOL; PINDOLOL; UNINDEXED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; IN VITRO STUDY; IN VIVO STUDY; LINEAR REGRESSION ANALYSIS; LIVER CELL; LIVER CLEARANCE; MALE; NONHUMAN; PREDICTIVE VALIDITY; RAT;

ANIMALS; BIAS (EPIDEMIOLOGY); DATA INTERPRETATION, STATISTICAL; HEPATOCYTES; HUMANS; METABOLIC CLEARANCE RATE; PREDICTIVE VALUE OF TESTS; RATS; REGRESSION ANALYSIS; XENOBIOTICS;

EID: 84863794190     PISSN: 00498254     EISSN: 13665928     Source Type: Journal    
DOI: 10.3109/00498254.2012.669080     Document Type: Article

References (41)

1. Armitage P, Berry G. (1994). Statistical methods in medical research. Oxford: Blackwell Scientific Publications, 3rd edition.
2. Barter ZE, Bayliss MK, Beaune PH, Boobis AR, Carlile DJ, Edwards RJ, Houston JB, Lake BG, Lipscomb JC, Pelkonen OR, Tucker GT, Rostami-Hodjegan A. (2007). Scaling factors for the extrapolation of in vivo metabolic drug clearance from in vitro data: Reaching a consensus on values of human microsomal protein and hepatocellularity per gram of liver. Curr Drug Metab 8:33-45.
3. Bissell DM, Guzelian PS. (1980). Phenotypic stability of adult rat hepatocytes in primary monolayer culture. Ann N Y Acad Sci 349:85-98.
4. Brandon EF, Raap CD, Meijerman I, Beijnen JH, Schellens JH. (2003). An update on in vitro test methods in human hepatic drug biotransformation research: Pros and cons. Toxicol Appl Pharmacol 189:233-246.
5. Briem S, Martinsson S, Bueters T, Skoglund E. (2007). Combined approach for high-throughput preparation and analysis of plasma samples from exposure studies. Rapid Commun Mass Spectrom 21:1965-1972.
6. Brown HS, Griffin M, Houston JB. (2007). Evaluation of cryopreserved human hepatocytes as an alternative in vitro system to microsomes for the prediction of metabolic clearance. Drug Metab Dispos 35:293-301.
7. Brown RP, Delp MD, Lindstedt SL, Rhomberg LR, Beliles RP. (1997). Physiological parameter values for physiologically based pharmacokinetic models. Toxicol Ind Health 13:407-484.
8. Delp MD, Evans MV, Duan C. (1998). Effects of aging on cardiac output, regional blood flow, and body composition in Fischer-344 rats. J Appl Physiol 85:1813-1822.
9. Donato MT, Castell JV. (2003). Strategies and molecular probes to investigate the role of cytochrome P450 in drug metabolism: Focus on in vitro studies. Clin Pharmacokinet 42:153-178.
10. Floby E, Briem S, Terelius Y, Sohlenius-Sternbeck AK. (2004). Use of a cocktail of probe substrates for drug-metabolizing enzymes for the assessment of the metabolic capacity of hepatocyte preparations. Xenobiotica 34:949-959.
11. Floby E, Johansson J, Hoogstraate J, Hewitt NJ, Hill J, Sohlenius- Sternbeck AK. (2009). Comparison of intrinsic metabolic clearance in fresh and cryopreserved human hepatocytes. Xenobiotica 39:656-662.
12. Goodman LS, Limbird LE, Milinoff PB, Ruddon RW, Gilman AG. (1996). Goodman and Gilman's the pharmacological basis of therapeutics, 9th edition. New York: McGraw-Hill.
13. Grime K, Riley RJ. (2006). The impact of in vitro binding on in vitroin vivo extrapolations, projections of metabolic clearance and clinical drug-drug interactions. Curr Drug Metab 7:251-264.
14. Hallifax D, Foster JA, Houston JB. (2010). Prediction of human metabolic clearance from in vitro systems: Retrospective analysis and prospective view. Pharm Res 27:2150-2161.
15. Hallifax D, Galetin A, Houston JB. (2008). Prediction of metabolic clearance using fresh human hepatocytes: Comparison with cryopreserved hepatocytes and hepatic microsomes for five benzodiazepines. Xenobiotica 38:353-367.
16. Hewitt NJ, Lechón MJ, Houston JB, Hallifax D, Brown HS, Maurel P, Kenna JG, Gustavsson L, Lohmann C, Skonberg C, Guillouzo A, Tuschl G, Li AP, LeCluyse E, Groothuis GM, Hengstler JG. (2007). Primary hepatocytes: Current understanding of the regulation of metabolic enzymes and transporter proteins, and pharmaceutical practice for the use of hepatocytes in metabolism, enzyme induction, transporter, clearance, and hepatotoxicity studies. Drug Metab Rev 39:159-234.
17. Houston JB. (1994). Utility of in vitro drug metabolism data in predicting in vivo metabolic clearance. Biochem Pharmacol 47:1469-1479.
18. Houston JB, Carlile DJ. (1997). Prediction of hepatic clearance from microsomes, hepatocytes, and liver slices. Drug Metab Rev 29:891-922.
19. Ito K, Houston JB. (2005). Prediction of human drug clearance from in vitro and preclinical data using physiologically based and empirical approaches. Pharm Res 22:103-112.
20. Ito K, 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 21: 785-792.
21. Kilford PJ, Gertz M, Houston JB, Galetin A. (2008). Hepatocellular binding of drugs: Correction for unbound fraction in hepatocyte incubations using microsomal binding or drug lipophilicity data. Drug Metab Dispos 36:1194-1197.
22. Lave T, Dupin S, Schmitt C, Chou RC, Jaeck D, Coassolo P. (1997). 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.
23. Li AP, Lu C, Brent JA, Pham C, Fackett A, Ruegg CE, Silber PM. (1999). Cryopreserved human hepatocytes: Characterization of drug-metabolizing enzyme activities and applications in higher throughput screening assays for hepatotoxicity, metabolic stability, and drug-drug interaction potential. Chem Biol Interact 121:17-35.
24. Loi CM, Young M, Randinitis E, Vassos A, Koup JR. (1999). Clinical pharmacokinetics of troglitazone. Clin Pharmacokinet 37:91-104.
25. McGinnity DF, Soars MG, Urbanowicz RA, 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.
26. Nagilla R, Frank KA, Jolivette LJ, Ward KW. (2006). Investigation of the utility of published in vitro intrinsic clearance data for prediction of in vivo clearance. J Pharmacol Toxicol Methods 53:106-116.
27. Naritomi Y, Terashita S, Kagayama A, 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.
28. 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.
29. Obach RS, Lombardo F, Waters NJ. (2008). Trend analysis of a database of intravenous pharmacokinetic parameters in humans for 670 drug compounds. Drug Metab Dispos 36:1385-1405.
30. Paine SW, Parker AJ, Gardiner P, Webborn PJ, Riley RJ. (2008). Prediction of the pharmacokinetics of atorvastatin, cerivastatin, and indomethacin using kinetic models applied to isolated rat hepatocytes. Drug Metab Dispos 36:1365-1374.
31. Paixão P, Gouveia LF, Morais JA. (2009). Prediction of drug distribution within blood. Eur J Pharm Sci 36:544-554.
32. Riley RJ, McGinnity DF, Austin RP. (2005). A unified model for predicting human hepatic, metabolic clearance from in vitro intrinsic clearance data in hepatocytes and microsomes. Drug Metab Dispos 33:1304-1311.
33. Shibata Y, Takahashi H, Chiba M, 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.
34. Smith R, Jones RD, Ballard PG, Griffiths HH. (2008). Determination of microsome and hepatocyte scaling factors for in vitro/in vivo extrapolation in the rat and dog. Xenobiotica 38:1386-1398.
35. Soars MG, Webborn PJ, Riley RJ. (2009). Impact of hepatic uptake transporters on pharmacokinetics and drug-drug interactions: Use of assays and models for decision making in the pharmaceutical industry. Mol Pharm 6:1662-1677.
36. Sohlenius-Sternbeck AK, Afzelius L, Prusis P, Neelissen J, Hoogstraate J, Johansson J, Floby E, Bengtsson A, Gissberg O, Sternbeck J, Petersson C. (2010). Evaluation of the human prediction of clearance from hepatocyte and microsome intrinsic clearance for 52 drug compounds. Xenobiotica 40:637-649.
37. Stringer R, Nicklin PL, Houston JB. (2008). Reliability of human cryopreserved hepatocytes and liver microsomes as in vitro systems to predict metabolic clearance. Xenobiotica 38:1313-1329.
38. Tang H, Hussain A, Leal M, Mayersohn M, Fluhler E. (2007). Interspecies prediction of human drug clearance based on scaling data from one or two animal species. Drug Metab Dispos 35:1886-1893.
39. Wenlock MC, Potter T, Barton P, Austin RP. (2011). A method for measuring the lipophilicity of compounds in mixtures of 10. J Biomol Screen 16:348-355.
40. Woodward RH and Goldsmith PL. (1964) Cumulative sum techniques. In: Mathematical and statistical techniques for industry. Monographs, 3. Edinburgh: Oliver and Boyd.
41. Youdim KA, Zayed A, Dickins M, Phipps A, Griffiths M, Darekar A, Hyland R, Fahmi O, Hurst S, Plowchalk DR, Cook J, Guo F, Obach RS. (2008). Application of CYP3A4 in vitro data to predict clinical drug-drug interactions; predictions of compounds as objects of interaction. Br J Clin Pharmacol 65:680-692.