Kinetic characterization of rat hepatic uptake of 16 actively transported drugs

Drug Metabolism and Disposition

Volumn 39, Issue 10, 2011, Pages 1808-1814

  Yabe, Yoshiyuki ^a,b   Galetin, Aleksandra ^a   Houston, J Brian ^a  

^a UNIVERSITY OF MANCHESTER   (United Kingdom)

^b DAIICHI SANKYO CO   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIBIOTIC AGENT; ANTIDIABETIC AGENT; ANTIVIRUS AGENT; ATORVASTATIN; BOSENTAN; CERIVASTATIN; CLARITHROMYCIN; ERYTHROMYCIN; FEXOFENADINE; HYDROXYMETHYLGLUTARYL COENZYME A REDUCTASE INHIBITOR; NATEGLINIDE; OLMESARTAN; PITAVASTATIN; PRAVASTATIN; REPAGLINIDE; RITONAVIR; ROSUVASTATIN; SAQUINAVIR; SARTAN DERIVATIVE; TELMISARTAN; VALSARTAN;

ACTIVE TRANSPORT; ANIMAL CELL; ARTICLE; CONCENTRATION (PARAMETERS); CONCENTRATION RESPONSE; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG CLEARANCE; DRUG METABOLISM; DRUG PENETRATION; DRUG TRANSPORT; DRUG UPTAKE; LIVER CELL; LIVER CLEARANCE; MALE; NONHUMAN; PHARMACOKINETICS; PRIORITY JOURNAL; RAT;

ANIMALS; BIOLOGICAL TRANSPORT, ACTIVE; DRUG INTERACTIONS; FACILITATED DIFFUSION; HEPATOCYTES; LIVER; MALE; PHARMACOKINETICS; RATS; RATS, SPRAGUE-DAWLEY;

RATTUS;

EID: 80053161024     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.111.040477     Document Type: Article

References (41)

1. Bow DA, Perry JL, Miller DS, Pritchard JB, and Brouwer KL (2008) Localization of P-gp (Abcb1) and Mrp2 (Abcc2) in freshly isolated rat hepatocytes. Drug Metab Dispos 36:198-202.
2. Brown HS, Chadwick A, and Houston JB (2007) Use of isolated hepatocyte preparations for cytochrome P450 inhibition studies: comparison with microsomes for Ki determination. Drug Metab Dispos 35:2119-2126. (Pubitemid 350005202)
3. Brown HS, Wilby AJ, Alder J, and Houston JB (2010) Comparative use of isolated hepatocytes and hepatic microsomes for cytochrome P450 inhibition studies: transporter-enzyme interplay. Drug Metab Dispos 38:2139-2146.
4. Gertz M, Harrison A, Houston JB, and Galetin A (2010) Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data. Drug Metab Dispos 38:1147-1158.
5. Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, et al. (2010) Membrane transporters in drug development. Nat Rev Drug Discov 9:215-236.
6. Gui C, Wahlgren B, Lushington GH, and Hagenbuch B (2009) Identification, Ki determination and CoMFA analysis of nuclear receptor ligands as competitive inhibitors of OATP1B1-mediated estradiol-17beta-glucuronide transport. Pharmacol Res 60:50-56.
7. Hagenbuch B, and Gui C (2008) Xenobiotic transporters of the human organic anion transporting polypeptides (OATP) family. Xenobiotica 38:778-801.
8. Hallifax D, Foster JA, and Houston JB (2010) Prediction of human metabolic clearance from in vitro systems: retrospective analysis and prospective view. Pharmacol Res 27:2150-2161.
9. Hallifax D, and Houston JB (2006) Uptake and intracellular binding of lipophilic amine drugs by isolated rat hepatocytes and implications for prediction of in vivo metabolic clearance. Drug Metab Dispos 34:1829-1836. (Pubitemid 44771710)
10. Hayes KA, Brennan B, Chenery R, and Houston JB (1995) In vivo disposition of caffeine predicted from hepatic microsomal and hepatocyte data. Drug Metab Dispos 23:349-353.
11. Hirano M, Maeda K, Shitara Y, and Sugiyama Y (2006) Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos 34:1229-1236.
12. Houston JB, and Galetin A (2008) Methods for predicting in vivo pharmacokinetics using data from in vitro assays. Curr Drug Metab 9:940-951.
13. Ieiri I, Higuchi S, and Sugiyama Y (2009) Genetic polymorphisms of uptake (OATP1B1, 1B3) and efflux (MRP2, BCRP) transporters: implications for inter-individual differences in the pharmacokinetics and pharmacodynamics of statins and other clinically relevant drugs. Expert Opin Drug Metab Toxicol 5:703-729.
14. Ishigami M, Tokui T, Komai T, Tsukahara K, Yamazaki M, and Sugiyama Y (1995) Evaluation of the uptake of pravastatin by perfused rat liver and primary cultured rat hepatocytes. Pharmacol Res 12:1741-1745. (Pubitemid 26004698)
15. 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. Pharmacol Res 21:785-792. (Pubitemid 39011301)
16. Kajosaari LI, Niemi M, Neuvonen M, Laitila J, Neuvonen PJ, and Backman JT (2005) Cyclosporine markedly raises the plasma concentrations of repaglinide. Clin Pharmacol Ther 78:388-399. (Pubitemid 41393674)
17. Kalliokoski A, Neuvonen M, Neuvonen PJ, and Niemi M (2008) The effect of SLCO1B1 polymorphism on repaglinide pharmacokinetics persists over a wide dose range. Br J Clin Pharmacol 66:818-825.
18. Kalliokoski A, and Niemi M (2009) Impact of OATP transporters on pharmacokinetics. Br J Pharmacol 158:693-705.
19. Kitamura S, Maeda K, Wang Y, and Sugiyama Y (2008) Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos 36:2014-2023.
20. Lam JL, Okochi H, Huang Y, and Benet LZ (2006) In vitro and in vivo correlation of hepatic transporter effects on erythromycin metabolism: characterizing the importance of transporter-enzyme interplay. Drug Metab Dispos 34:1336-1344. (Pubitemid 44079874)
21. Mico BA, Federowicz DA, Ripple MG, and Kerns W (1988) In vivo inhibition of oxidative drug metabolism by, and acute toxicity of, 1-aminobenzotriazole (ABT). A tool for biochemical toxicology. Biochem Pharmacol 37:2515-2519.
22. Nakai D, Nakagomi R, Furuta Y, Tokui T, Abe T, Ikeda T, and Nishimura K (2001) Human liver-specific organic anion transporter, LST-1, mediates uptake of pravastatin by human hepatocytes. J Pharmacol Exp Ther 297:861-867. (Pubitemid 32472480)
23. Nezasa K, Higaki K, Takeuchi M, Nakano M, and Koike M (2003) Uptake of rosuvastatin by isolated rat hepatocytes: comparison with pravastatin. Xenobiotica 33:379-388. (Pubitemid 36688114)
24. Noe J, Portmann R, Brun ME, and Funk C (2007) Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab Dispos 35:1308-1314. (Pubitemid 47121771)
25. Paine SW, Parker AJ, Gardiner P, Webborn PJ, and 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. (Pubitemid 351929321)
26. Parker AJ, and Houston JB (2008) Rate-limiting steps in hepatic drug clearance: comparison of hepatocellular uptake and metabolism with microsomal metabolism of saquinavir, nelfinavir, and ritonavir. Drug Metab Dispos 36:1375-1384. (Pubitemid 351929322)
27. Petzinger E, and Fuckel D (1992) Evidence for a saturable, energy-dependent and carrier-mediated uptake of oral antidiabetics into rat hepatocytes. Eur J Pharmacol 213:381-391.
28. Poirier A, Lave T, Portmann R, Brun ME, Senner F, Kansy M, Grimm HP, and Funk C (2008) Design, data analysis, and simulation of in vitro drug transport kinetic experiments using a mechanistic in vitro model. Drug Metab Dispos 36:2434-2444.
29. 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. (Pubitemid 41196973)
30. Sharma P, Holmes VE, Elsby R, Lambert C, and Surry D (2009) Validation of cell-based OATP1B1 assays to assess drug transport and the potential for drug-drug interaction to support regulatory submissions. Xenobiotica 40:24-37.
31. Shimada S, Fujino H, Morikawa T, Moriyasu M, and Kojima J (2003) Uptake mechanism of pitavastatin, a new inhibitor of HMG-CoA reductase, in rat hepatocytes. Drug Metab Pharmacokinet 18:245-251.
32. Shitara Y, and Sugiyama Y (2006) Pharmacokinetic and pharmacodynamic alterations of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors: drug-drug interactions and interindividual differences in transporter and metabolic enzyme functions. Pharmacol Ther 112:71-105. (Pubitemid 44301483)
33. Soars MG, Webborn PJ, and 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.
34. Watanabe T, Kusuhara H, Maeda K, Kanamaru H, Saito Y, Hu Z, and Sugiyama Y (2010) Investigation of the rate-determining process in the hepatic elimination of HMG-CoA reductase inhibitors in rats and humans. Drug Metab Dispos 38:215-222.
35. Watanabe T, Kusuhara H, Maeda K, Shitara Y, and Sugiyama Y (2009a) Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans. J Pharmacol Exp Ther 328:652-662.
36. Watanabe T, Maeda K, Kondo T, Nakayama H, Horita S, Kusuhara H, and Sugiyama Y (2009b) Prediction of the hepatic and renal clearance of transporter substrates in rats using in vitro uptake experiments. Drug Metab Dispos 37:1471-1479.
37. Webborn PJ, Parker AJ,Denton RL, and Riley RJ (2007) In vitro-in vivo extrapolation of hepatic clearance involving active uptake: theoretical and experimental aspects. Xenobiotica 37:1090-1109. (Pubitemid 350035538)
38. Xu L, Chen Y, Pan Y, Skiles GL, and Shou M (2009) Prediction of human drug-drug interactions from time-dependent inactivation of CYP3A4 in primary hepatocytes using a population-based simulator. Drug Metab Dispos 37:2330-2339.
39. Yamano K, Yamamoto K, Kotaki H, Sawada Y, and Iga T (1999) Quantitative prediction of metabolic inhibition of midazolam by itraconazole and ketoconazole in rats: implication of concentrative uptake of inhibitors into liver. Drug Metab Dispos 27:395-402. (Pubitemid 29114249)
40. Yamano K, Yamamoto K, Kotaki H, Takedomi S, Matsuo H, Sawada Y, and Iga T (2000) Quantitative prediction of metabolic inhibition of midazolam by erythromycin, diltiazem, and verapamil in rats: implication of concentrative uptake of inhibitors into liver. J Pharmacol Exp Ther 292:1118-1126. (Pubitemid 30136609)
41. Yamazaki M, Suzuki H, Hanano M, Tokui T, Komai T, and Sugiyama Y (1993) Na(+)-independent multispecific anion transporter mediates active transport of pravastatin into rat liver. Am J Physiol 264:G36-G44. (Pubitemid 23055986)