Relationship between passive permeability, efflux, and predictability of clearance from in vitro metabolic intrinsic clearance

Drug Metabolism and Disposition

Volumn 38, Issue 2, 2010, Pages 223-231

  Huang, Liyue ^a   Berry, Loren ^a   Ganga, Sindhura ^b   Janosky, Brett ^a   Chen, April ^a   Roberts, Jonathan ^a   Colletti, Adria E ^a   Lin, Min Hwa Jasmine ^a  

^a AMGEN INC   (United States)

^b GENZYME CORPORATION   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BOSENTAN; BREAST CANCER RESISTANCE PROTEIN; BUSPIRONE; CLOZAPINE; CYCLOSPORIN; DICLOFENAC; GEMFIBROZIL; GLYCOPROTEIN P; IMIPRAMINE; INDOMETACIN; METOPROLOL; MONTELUKAST; PRAZOSIN; PROPAFENONE; RITONAVIR; TOLBUTAMIDE; TROGLITAZONE; VERAPAMIL;

ANALYTICAL ERROR; ANIMAL CELL; ANIMAL EXPERIMENT; ARTICLE; BLOOD SAMPLING; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG METABOLISM; DRUG PENETRATION; DRUG TRANSPORT; HUMAN; HUMAN CELL; IN VITRO METABOLIC CLEARANCE; IN VITRO STUDY; IN VIVO CULTURE; INCUBATION TIME; LIVER CELL; LIVER MICROSOME; MALE; METABOLIC CLEARANCE RATE; NONHUMAN; PHARMACOLOGICAL PARAMETERS; PREDICTION; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN TRANSPORT; SINGLE DRUG DOSE;

ALGORITHMS; ANIMALS; ATP-BINDING CASSETTE TRANSPORTERS; BIOLOGICAL TRANSPORT; CELL LINE; CELL MEMBRANE PERMEABILITY; DOGS; GENES, MDR; HEPATOCYTES; HUMANS; MALE; METABOLIC CLEARANCE RATE; MICE; MICROSOMES, LIVER; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; PHYSICOCHEMICAL PHENOMENA; RATS; RATS, SPRAGUE-DAWLEY; SUS SCROFA;

RATTUS;

EID: 76149142438     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.109.029066     Document Type: Article

References (35)

1. Balani SK, Xu X, Pratha V, Koss MA, Amin RD, Dufresne C, Miller RR, Arison BH, Doss GA, Chiba M, et al. (1997) Metabolic profiles of montelukast sodium (Singulair), a potent cysteinyl leukotriene1 receptor antagonist, in human plasma and bile. Drug Metab Dispos 25:1282-1287.
2. Bidstrup TB, Bjørnsdottir I, Sidelmann UG, Thomsen MS, and Hansen KT (2003) CYP2C8 and CYP3A4 are the principal enzymes involved in the human in vitro biotransformation of the insulin secretagogue repaglinide. Br J Clin Pharmacol 56:305-314.
3. Brown HS, Griffin M, and 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.
4. Burger H, van Tol H, Boersma AW, Brok M, Wiemer EA, Stoter G, and Nooter K (2004) Imatinib mesylate (STI571) is a substrate for the breast cancer resistance protein (BCRP)/ ABCG2 drug pump. Blood 104:2940-2942.
5. Cummins CL, Jacobsen W, and Benet LZ (2002) Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther 300:1036-1045.
6. Dai H, Marbach P, Lemaire M, Hayes M, and Elmquist WF (2003) Distribution of STI-571 to the brain is limited by P-glycoprotein-mediated efflux. J Pharmacol Exp Ther 304:1085-1092.
7. Davies B and Morris T (1993) Physiological parameters in laboratory animals and humans. Pharm Res 10:1093-1095.
8. De Kanter R, Monshouwer M, Draaisma AL, De Jager MH, de Graaf IA, Proost JH, Meijer DK, and Groothuis GM (2004) Prediction of whole-body metabolic clearance of drugs through the combined use of slices from rat liver, lung, kidney, small intestine and colon. Xenobiotica 34:229-241.
9. Egan WJ and Lauri G (2002) Prediction of intestinal permeability. Adv Drug Deliv Rev 54:273-289.
10. Feng B, Mills JB, Davidson RE, Mireles RJ, Janiszewski JS, Troutman MD, and de Morais SM (2008) In vitro P-glycoprotein assays to predict the in vivo interactions of P-glycoprotein with drugs in the central nervous system. Drug Metab Dispos 36:268-275.
11. Irvine JD, Takahashi L, Lockhart K, Cheong J, Tolan JW, Selick HE, and Grove JR (1999) MDCK (Madin-Darby canine kidney) cells: a tool for membrane permeability screening. J Pharm Sci 88:28-33.
12. 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 21:785-792.
13. Leusch A, Volz A, Müller G, Wagner A, Sauer A, Greischel A, and Roth W (2002) Altered drug disposition of the platelet activating factor antagonist apafant in mdr1a knockout mice. Eur J Pharm Sci 16:119-128.
14. Mälkiä A, Murtomäki L, Urtti A, and Kontturi K (2004) Drug permeation in biomembranes: in vitro and in silico prediction and influence of physicochemical properties. Eur J Pharm Sci 23:13-47.
15. Mayer U, Wagenaar E, Beijnen JH, Smit JW, Meijer DK, van Asperen J, Borst P, and Schinkel AH (1996) Substantial excretion of digoxin via the intestinal mucosa and prevention of long-term digoxin accumulation in the brain by the mdr 1a P-glycoprotein. Br J Pharmacol 119:1038-1044.
16. Mougey EB, Feng H, Castro M, Irvin CG, and Lima JJ (2009) Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet Genomics 19:129-138.
17. Nakai D, Kumamoto K, Sakikawa C, Kosaka T, and Tokui T (2004) Evaluation of the protein binding ratio of drugs by a micro-scale ultracentrifugation method. J Pharm Sci 93:847-854.
18. 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.
19. 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.
20. Niemi M, Backman JT, Kajosaari LI, Leathart JB, Neuvonen M, Daly AK, Eichelbaum M, Kivistö KT, and Neuvonen PJ (2005) Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Clin Pharmacol Ther 77:468-478.
21. 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.
22. Oostendorp RL, Buckle T, Beijnen JH, van Tellingen O, and Schellens JH (2009) The effect of P-gp (Mdr1a/1b), BCRP (Bcrp1) and P-gp/BCRP inhibitors on the in vivo absorption, distribution, metabolism and excretion of imatinib. Invest New Drugs 27:31-40.
23. Polli JW, Wring SA, Humphreys JE, Huang L, Morgan JB, Webster LO, and Serabjit-Singh CS (2001) Rational use of in vitro P-glycoprotein assays in drug discovery. J Pharmacol Exp Ther 299:620-628.
24. Riley RJ, McGinnity DF, and 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.
25. Robey RW, To KK, Polgar O, Dohse M, Fetsch P, Dean M, and Bates SE (2009) ABCG2: a perspective. Adv Drug Deliv Rev 61:3-13.
26. Seglen PO (1973) Preparation of rat liver cells. 3. Enzymatic requirements for tissue dispersion. Exp Cell Res 82:391-398.
27. Shitara Y, Horie T, and Sugiyama Y (2006) Transporters as a determinant of drug clearance and tissue distribution. Eur J Pharm Sci 27:425-446.
28. Shitara Y, Itoh T, Sato H, Li AP, and Sugiyama Y (2003) Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. J Pharmacol Exp Ther 304:610-616.
29. Sparreboom A, van Asperen J, Mayer U, Schinkel AH, Smit JW, Meijer DK, Borst P, Nooijen WJ, Beijnen JH, and van Tellingen O (1997) Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine. Proc Natl Acad Sci U S A 94:2031-2035.
30. Stouch TR and Gudmundsson O (2002) Progress in understanding the structure-activity relationships of P-glycoprotein. Adv Drug Deliv Rev 54:315-328.
31. Stringer R, Nicklin PL, and Houston JB (2008) Reliability of human cryopreserved hepatocytes and liver microsomes as in vitro systems to predict metabolic clearance. Xenobiotica 38:1313-1329.
32. Tang W, Stearns RA, Chen Q, Bleasby K, Teffera Y, Colletti A, Hafey M, Evers R, Dean DC, Magriotis PA, et al. (2008) Importance of mechanistic drug metabolism studies in support of drug discovery: a case study with an N-sulfonylated dipeptide VLA-4 antagonist in rats. Xenobiotica 38:223-237.
33. Treiber A, Schneiter R, Häusler S, and Stieger B (2007) Bosentan is a substrate of human OATP1B1 and OATP1B3: inhibition of hepatic uptake as the common mechanism of its interactions with cyclosporin A, rifampicin, and sildenafil. Drug Metab Dispos 35:1400-1407.
34. Weber C, Gasser R, and Hopfgartner G (1999) Absorption, excretion, and metabolism of the endothelin receptor antagonist bosentan in healthy male subjects. Drug Metab Dispos 27: 810-815.
35. Wu CY and Benet LZ (2005) Predicting drug disposition via application of BCS: transport/ absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res 22:11-23.