Predicting human hepatic clearance from in vitro drug metabolism and transport data: A scientific and pharmaceutical perspective for assessing drug-drug interactions

Biopharmaceutics and Drug Disposition

Volumn 33, Issue 4, 2012, Pages 179-194

  Camenisch, Gian ^a   Umehara, Ken Ichi ^a  

^a NOVARTIS PHARMA AG   (Switzerland)

Author keywords

clearance prediction; compound classification; drug drug interactions; metabolism; transporter

Indexed keywords

ALISKIREN; ATORVASTATIN; CARRIER PROTEIN; CIMETIDINE; CIPROFLOXACIN; CYCLOSPORIN A; CYTOCHROME P450 3A4; DIGOXIN; FUROSEMIDE; HYDROCHLOROTHIAZIDE; KETOCONAZOLE; MULTIDRUG RESISTANCE PROTEIN 1; NEW DRUG; PRAVASTATIN; PROBENECID; PROPRANOLOL; QUINIDINE; RIFAMPICIN; VALSARTAN; VERAPAMIL;

AREA UNDER THE CURVE; BILE SECRETION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DECISION TREE; DRUG ABSORPTION; DRUG CLASSIFICATION; DRUG CLEARANCE; DRUG DISPOSITION; DRUG ELIMINATION; DRUG EXCRETION; DRUG INTERACTION; DRUG METABOLISM; DRUG TRANSPORT; DRUG UPTAKE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; LIVER BLOOD FLOW; LIVER CELL; LIVER CLEARANCE; LIVER MICROSOME; MATHEMATICAL MODEL; PREDICTION; REVIEW;

BIOLOGICAL TRANSPORT; DECISION TREES; DRUG DESIGN; DRUG INTERACTIONS; HEPATOCYTES; HUMANS; LINEAR MODELS; MICROSOMES, LIVER; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS;

EID: 84861234645     PISSN: 01422782     EISSN: 1099081X     Source Type: Journal    
DOI: 10.1002/bdd.1784     Document Type: Review

References (49)

1. Ito K, Houston BJ,. Comparison of the use of liver models for predicting drug clearance using in vitro kinetic data from hepatic microsomes and isolated hepatocytes. Pharm Res 2004; 21: 785-792. (Pubitemid 39011301)
2. Watanabe T, Kusuhara H, Sugiyama Y,. Application of physiologically based pharmacokinetic modeling and clearance concept to drugs showing transporter-mediated distribution and clearance in humans. J Pharmacokinet Pharmacodyn 2010; 37: 575-590.
3. Umehara K, Camenisch G,. Novel in vitro-in vivo extrapolation (IVIVE) method to predict hepatic organ clearance in rat. Pharm Res 2012; 29: 603-617.
4. Shitara Y, Sato H, Sugiyama Y,. Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol 2005; 45: 689-723. (Pubitemid 40261822)
5. Liu L, Pang S,. The roles of transporters and enzymes in hepatic drug processing. Drug Metab Dispos 2005; 33: 1-9. (Pubitemid 40023507)
6. Sirianni G, Pang S,. Organ clearance concepts: New perspectives on old principles. J Pharmcokinet Biopharm 1997; 25: 449-470. (Pubitemid 28186446)
7. Kwon Y, Morris ME,. Membrane transport in hepatic clearance of drugs. I: Extended hepatic clearance models incorporating concentration-dependent transport and elimination processes. Pharm Res 1997; 14: 774-779. (Pubitemid 27281673)
8. Wu CY, Benet LZ,. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 2005; 22: 11-23. (Pubitemid 40558141)
9. Wilkinsin GR,. Clearance approaches in pharmacology. Pharmacol Rev 1987; 39: 1-47.
10. Yamazaki M, Suzuki H, Sugiyama Y,. Recent advances in carrier-mediated hepatic uptake and biliary excretion of xenobiotics. Pharm Res 1996; 13: 497-513. (Pubitemid 26119682)
11. Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, Sugiyama Y,. Prediction of pharmacokinetic alterations caused by drug-drug interactions: Metabolic interaction in the liver. Pharmacol Rev 1998; 50: 387-411. (Pubitemid 28477680)
12. Einolf HJ,. Comparison of different approaches to predict metabolic drug-drug interactions. Xenobiotica 2007; 37: 1257-1294. (Pubitemid 350035530)
13. Ring B, Chien JY, Adkison KK, et al,. PhRMA CPCDC initiative on predictive models of human pharmacokinetics, Part 3: Comparative assessment of prediction methods of human clearance. J Pharm Sci 2011; 100: 4090-4110.
14. Custodio JM, Wu CY, Benet LZ,. Predicting drug disposition, absorption/elimination /transporter interplay and the role of food on drug absorption. Adv Drug Del Rev 2008; 60: 717-733.
15. Gertz M, Harrison A, Houston JB, Galetin A,. Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data. Drug Metab Dispos 2010; 38: 1147-1158.
16. Kadono K, Akabane T, Tabata K, Gato K, Terashita S, Teramura T,. Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor. Drug Metab Dispos 2010; 38: 1230-1237.
17. Huang YC, Colaizzi JL, Bierman RH, Woestenborghs R, Heykants J,. Pharmacokinetics and dose proportionality of ketoconazole in normal volunteers. Antimicrob Agents Chemother 1986; 30: 206-210. (Pubitemid 16038748)
18. Nishimuta H, Sato K, Yabuki M, Komuro S,. Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data. Drug Metab Pharmacokinet 2011; 26: 592-601.
19. Vance-Bryan K, Guay DR, Rotschafer JC,. Clinical pharmacokinetics of ciprofloxacin. Clin Pharmacokinet 1990; 19: 434-461.
20. Lavé T, Parrott N, Grimm HP, Fleury A, Reddy M,. Challenges and opportunities with modeling and simulation in drug discovery and drug development. Xenobiotica 2007; 37: 1295-1310. (Pubitemid 350035528)
21. Poirier A, Funk C, Lavé T, Noé J,. New strategies to address drug-drug interactions involving OATPs. Curr Opinion Drug Dis and Dev 2007; 10: 74-83. (Pubitemid 46438260)
22. Kusuhara H, Sugiyama Y,. In vitro-in vivo extrapolation of transporter-mediated clearance in the liver and kidney. Drug Metab Pharmacokin 2009; 24: 37-52.
23. Rowland M, Martin SB,. Kinetics of drug-drug interactions. J Pharmacokinet Biopharm 1973; 1: 553-567.
24. Venkatakrishnan K, von Moltke LL, Obach RS, Greenblatt DJ,. Drug metabolism and drug interactions: Application and clinical value of in vitro models. Curr Drug Metab 2036; 4: 423-459.
25. Clewell HJ, Reddy MJ, Lavé T, Andersen ME,. Physiologically based pharmacokinetic modeling. In Preclinical Development Handbook., Grad S, (ed). John Wiley & Sons: Hoboken, NJ, 2007.
26. Rowland M, Balant L, Peck C,. Physiologically based pharmacokinetics in drug development and regulatory science: A workshop report (Georgetown University, Washington DC, May 29-30, 2002). AAPS Pharm Sci 2004; 61: E6.
27. Bachmann KA,. Inhibition constants, inhibitor concentrations and the prediction of inhibitory drug drug interactions: pitfalls, progress and promise. Curr Drug Metab 2006; 7: 1-14.
28. International Transporter Consortium. Membrane transporters in drug development. Nature Rev Drug Discov 2010; 9: 215-236.
29. Drugs@FDA database.
30. Mazzu AL, Lassetter KC, Shamblen EC, Agarwal V, Lettieri J, Sundaressen P,. Itraconazole alters the pharmacokinetics of atorvastatin to a greater extent than either cerivastatin or pravastatin. Clin Pharmacol Ther 2000; 68: 391-400.
31. Walle T, Walle UK, Olanoff LS, Conradi EC,. Partial metabolic clearances as determinants of the oral bioavailability of propranolol. Br J Clin Pharmacol 1986; 22: 317-323. (Pubitemid 17170721)
32. Ochs HR, Greenblatt DJ, Woo E,. Clinical pharmacokinetics of quinidine. Clin Pharmacokinet 1980; 5: 150-168. (Pubitemid 11248747)
33. Eichelbaum M, Ende M, Remberg G, Schomerus M, Dengler HJ,. The metabolism of DL-[14C]verapamil in man. Drug Metab Dispos 1979; 7: 145-148.
34. Lemaire M, Maurer G, Wood AJ,. Cyclosporin. Pharmacokinetics and metabolism. Prog Allergy 1986; 38: 93-107.
35. Como JA, Dismukes WE,. Oral azole drugs as systemic antifungal therapy. N Engl J Med 1995; 330: 263-272.
36. Everett DW, Chando TJ, Didonato GC, Singhvi SM, Pan HY, Weinstein SH,. Biotransformation of pravastatin sodium in humans. Drug Metab Dispos 1991; 19: 740-748.
37. Waldmeier F, Flesch G, Müller P, et al,. Pharmacokinetics, disposition and biotransformation of [14C]-radiolabelled valsartan in healthy male volunteers after a single oral dose. Xenobiotica 1997; 27: 59-71. (Pubitemid 27068372)
38. Mitchell SC, Idle JR, Smith RL,. The metabolism of [14C]cimetidine in man. Xenobiotica 1982; 12: 283-292.
39. Doherty JE, Kane JJ,. Clinical pharmacology of digitalis glycosides. Annu Rev Med 1975; 26: 159-171.
40. Beermann B, Dalén E, Lindström B, Rosén A,. On the fate of furosemide in man. Eur J Clin Pharmacol 1975; 9: 51-61.
41. Carlile DJ, Zomorodi K, Houston JB,. Scaling factors to relate drug metabolic clearance in hepatic microsomes, isolated hepatocytes, and the intact liver: studies with induced livers involving diazepam. Drug Metab Dispos 1997; 25: 903-911. (Pubitemid 27357686)
42. Swift B, Pfeifer ND, Brouwer KL,. Sandwich-cultured hepatocytes: an in vitro model to evaluate hepatobiliary transporter-based drug interactions and hepatotoxicity. Drug Metab Rev 2010; 42: 446-471.
43. Foradori A, Mezzano S, Videla S, Pefaur J, Elberg A,. Modification of the pharmacokinetics of cyclosporine A and metabolites by concomitant use of Neoral and diltiazem or ketoconazole in stable adult kidney transplants. Transplant Proc 1998; 30: 1685-1687. (Pubitemid 28399280)
44. He YJ, Zhang W, Chen Y, et al,. Rifampicin alters atorvastatin plasma concentrations on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta 2009; 405: 49-52.
45. Vaidyanathan S, Camenisch G, Schuetz H, et al,. Pharmacokinetics of the oral direct renin inhibitor aliskiren in combination with digoxin, atorvastatin, and ketoconazole in healthy subjects: the role of P-glycoprotein in the disposition of aliskiren. J Clin Pharmacol 2008; 48: 1323-1338.
46. Park JW, Sieklmeier R, Merz M, et al,. Pharmacokinetics of pravastatin in heart-transplant patients taking cyclosporine A. Int J Clin Pharmacol Ther 2002; 40: 439-450.
47. Bhad P, Ayalasomayajula S, Kara R, et al,. Evaluation of pharmacokinetic interactions between amlodipine, valsartan, and hydrochlorothiazide in patients with hypertension. J Clin Pharmacol 2011; 51: 933-942.
48. Vree TB, van den Biggelaar-Martea M, Verwey-van Wissen CP,. Probenecid inhibits the renal clearance of furosemide and its acyl glucuronide. Br J Clin Pharmacol 1995; 39: 692-695.
49. University of Washington database.