Design, data analysis, and simulation of in vitro drug transport kinetic experiments using a mechanistic in vitro model

Drug Metabolism and Disposition

Volumn 36, Issue 12, 2008, Pages 2434-2444

  Poirier, Agnès ^a   Lavé, Thierry ^a   Portmann, Renée ^a   Brun, Marie Elise ^a   Senner, Frank ^a   Kansy, Manfred ^a   Grimm, Hans Peter ^a   Funk, Christoph ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLECYSTOKININ OCTAPEPTIDE; DELTORPHIN; ESTRONE SULFATE; FEXOFENADINE; NAPSAGATRAN; ORGANIC ANION TRANSPORTER; PITAVASTATIN; PRAVASTATIN; PROPRANOLOL; TAUROCHOLIC ACID;

ACTIVE TRANSPORT; ANIMAL CELL; ARTICLE; CHO CELL; COMPARTMENT MODEL; CONTROLLED STUDY; DATA ANALYSIS; DIFFUSION; DRUG TRANSPORT; DRUG UPTAKE; LIVER CELL; MEMBRANE PERMEABILITY; MICHAELIS CONSTANT; NONHUMAN; PRIORITY JOURNAL; RAT; TEMPERATURE DEPENDENCE;

ALGORITHMS; ANIMALS; BIOLOGICAL TRANSPORT, ACTIVE; CHO CELLS; COMPUTER SIMULATION; CRICETINAE; CRICETULUS; DIFFUSION; ESTRONE; FATTY ACIDS, MONOUNSATURATED; HEPATOCYTES; INDOLES; KINETICS; MALE; MEMBRANES, ARTIFICIAL; MODELS, BIOLOGICAL; NAPHTHALENES; OLIGOPEPTIDES; ORGANIC ANION TRANSPORTERS; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; PHARMACOKINETICS; PIPERIDINES; QUINOLINES; RATS; RATS, WISTAR; SINCALIDE; TEMPERATURE; TERFENADINE;

CRICETULUS GRISEUS; RATTUS;

EID: 57349162183     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.108.020750     Document Type: Article

References (46)

1. Avdeef A, Strafford M, Block E, Balogh MP, Chambliss W, and Khan I (2001) Drug absorption in vitro model: filter-immobilized artificial membranes. 2. Studies of the permeability properties of lactones in Piper methysticum Forst. Eur J Pharm Sci 14:271-280.
2. Baker M and Parton T (2007) Kinetic determinants of hepatic clearance: plasma protein binding and hepatic uptake. Xenobiotica 37:1110-1134.
3. m. Pharm Res 22:1667-1677.
4. Blanchard N, Richert L, Notter B, Delobel F, David P, Coassolo P, and Lavé T (2004) Impact of serum on clearance predictions obtained from suspensions and primary cultures of rat hepatocytes. Eur J Pharm Sci 23:189-199.
5. Boelsterli UA, Bouis P, Brouillard JF, and Donatsch P (1988) In vitro toxicity assessment of cyclosporin A and its analogs in a primary rat hepatocyte culture model. Toxicol Appl Pharmacol 96:212-221.
6. Brosnan JT and Qian D (1994) Endotoxin-induced increase in liver mass and hepatocyte volume. Biochem Soc Trans 22:529-532.
7. Chandra P and Brouwer KL (2004) The complexities of hepatic drug transport: current knowledge and emerging concepts. Pharm Res 21:719-735.
8. Cvetkovic M, Leake B, Fromm MF, Wilkinson GR, and Kim RB (1999) OATP and P-glycoprotein transporters mediate the cellular uptake and excretion of fexofenadine. Drug Metab Dispos 27:866-871.
9. Ekins S, Ecker GF, Chiba P, and Swaan PW (2007) Future directions for drug transporter modelling. Xenobiotica 37:1152-1170.
10. Fischer H, Kansy M, Avdeef A, and Senner F (2007) Permeation of permanently positive charged molecules through artificial membranes - influence of physico-chemical properties. Eur J Pharm Sci 31:32-42.
11. Frézard F and Garnier-Suillerot A (1998) Permeability of lipid bilayer to anthracycline derivatives: role of the bilayer composition and of the temperature. Biochim Biophys Acta 1389: 13-22.
12. González-Alvarez I, Fernández-Teruel C, Garrigues TM, Casabo VG, Ruiz-García A, and Bermejo M (2005) Kinetic modelling of passive transport and active efflux of a fluoroquinolone across Caco-2 cells using a compartmental approach in NONMEM. Xenobiotica 35:1067-1088.
13. 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.
14. Hirano M, Maeda K, Shitara Y, and Sugiyama Y (2004) Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther 311:139-146.
15. 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.
16. Ho RH, Tirona RG, Leake BF, Glaeser H, Lee W, Lemke CJ, Wang Y, and Kim RB (2006) Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology 130:1793-1806.
17. Ishiguro N, Maeda K, Kishimoto W, Saito A, Harada A, Ebner T, Roth W, Igarashi T, and Sugiyama Y (2006) Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos 34:1109-1115.
18. Ismair MG, Stieger B, Cattori V, Hagenbuch B, Fried M, Meier PJ, and Kullak-Ublick GA (2001) Hepatic uptake of cholecystokinin octapeptide by organic anion-transporting polypeptides OATP4 and OATP8 of rat and human liver. Gastroenterology 121:1185-1190.
19. Komai T, Shigehara E, Tokui T, Koga T, Ishigami M, Kuroiwa C, and Horiuchi S (1992) Carrier-mediated uptake of pravastatin by rat hepatocytes in primary culture. Biochem Pharmacol 43:667-670.
20. Kopplow K, Letschert K, König J, Walter B, and Keppler D (2005) Human hepatobiliary transport of organic anions analyzed by quadruple- transfected cells. Mol Pharmacol 68:1031-1038.
21. Lançon A, Delmas D, Osman H, Thénot JP, Jannin B, and Latruffe N (2004) Human hepatic cell uptake of resveratrol: involvement of both passive diffusion and carrier-mediated process. Biochem Biophys Res Commun 316:1132-1137.
22. Lindberg V (1997) Uncertainties Error Propagation Graphing and Vernier Caliper: A Reference Manual for University Physics Laboratories, Rochester Institute of Technology, Rochester, NY.
23. Liu L and Pang KS (2006) An integrated approach to model hepatic drug clearance. Eur J Pharm Sci 29:215-230.
24. Luttringer O, Theil FP, Lavé T, Wernli-Kuratli K, Guentert TW, and de Saizieu A (2002) Influence of isolation procedure, extracellular matrix and dexamethasone on the regulation of membrane transporters gene expression in rat hepatocytes. Biochem Pharmacol 64:1637-1650.
25. Neuhoff S, Ungell AL, Zamora I, and Artursson P (2005) pH-dependent passive and active transport of acidic drugs across Caco-2 cell monolayers. Eur J Pharm Sci 25:211-220.
26. Noé J, Portmann R, Brun ME, and Funk C (2007) Substrate dependent drug-drug interactions between gemfibrozil, fluvastatin and other OATP substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab Dispos 35:1308-1314.
27. Obach RS (1996) The importance of nonspecific binding in in vitro matrices, its impact on enzyme kinetic studies of drug metabolism reactions, and implications for in vitro-in vivo correlations. Drug Metab Dispos 24:1047-1049.
28. 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.
29. Petzinger E and Geyer J (2006) Drug transporters in pharmacokinetics. Naunyn Schmiedebergs Arch Pharmacol 372:465-475.
30. Poirier A, Funk C, Lavé T, and Noé J (2007) New strategies to address drug-drug interactions involving OATPs. Curr Opin Drug Discov Devel 10:74-83.
31. Ratanasavanh D, Lamiable D, Biour M, Guédès Y, Gersberg M, Leutenegger E, and Riché C (1996) Metabolism and toxicity of coumarin on cultured human, rat, mouse and rabbit hepatocytes. Fundam Clin Pharmacol 10:504-510.
32. Reinoso RF, Telfer BA, Brennan BS, and Rowland M (2001) Uptake of teicoplanin by isolated rat hepatocytes: comparison with in vivo hepatic distribution. Drug Metab Dispos 29:453-459.
33. Ries J and Wienen W (2003) Serine proteases as targets for antithrombotic therapy. Drugs Future 28:355-370.
34. Sarkadi B, Attisano L, Grinstein S, Buchwald M, and Rothstein A (1984) Volume regulation of Chinese hamster ovary cells in anisoosmotic media. Biochim Biophys Acta 774:159-168.
35. Seglen PO (1979) Hepatocyte suspensions and cultures as tools in experimental carcinogenesis. J Toxicol Environ Health 5:551-560.
36. 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.
37. Shitara Y, Hirano M, Adachi Y, Itoh T, Sato H, and Sugiyama Y (2004) In vitro and in vivo correlation of the inhibitory effect of cyclosporin A on the transporter-mediated hepatic uptake of cerivastatin in rats. Drug Metab Dispos 32:1468-1475.
38. 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.
39. Shitara Y, Li AP, Kato Y, Lu C, Ito K, Itoh T, and Sugiyama Y (2003) Function of uptake transporters for taurocholate and estradiol 17β-D-glucuronide in cryopreserved human hepatocytes. Drug Metab Pharmacokinet 18:33-41.
40. Sun H and Pang KS (2008) Permeability, transport, and metabolism of solutes in Caco-2 cell monolayers: a theoretical study. Drug Metab Dispos 36:102-123.
41. Treiber A, Schneiter R, Delahaye S, and Clozel M (2004) Inhibition of organic anion transporting polypeptide-mediated hepatic uptake is the major determinant in the pharmacokinetic interaction between bosentan and cyclosporin A in the rat. J Pharmacol Exp Ther 308:1121-1129.
42. 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.
43. van Montfoort JE, Hagenbuch B, Groothuis GM, Koepsell H, Meier PJ, and Meijer DK (2003) Drug uptake systems in liver and kidney. Curr Drug Metab 4:185-211.
44. Vickers SE, Stow MW, and Warr JR (1993) Relationship between multidrug resistance, hypersensitivity to resistance modifiers and cell volume in Chinese hamster ovary cells. Cell Biol Int 17:477-485.
45. 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.
46. Yamashiro W, Maeda K, Hirouchi M, Adachi Y, Hu Z, and Sugiyama Y (2006) Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans. Drug Metab Dispos 34:1247-1254.