Predicting carrier-mediated hepatic disposition of rosuvastatin in man by scaling from individual transfected cell-lines in vitro using absolute transporter protein quantification and PBPK modeling

European Journal of Pharmaceutical Sciences

Volumn 65, Issue , 2014, Pages 156-166

  Bosgra, Sieto ^a   Van De Steeg, Evita ^a   Vlaming, Maria L ^a   Verhoeckx, Kitty C ^a   Huisman, Maarten T ^b   Verwei, Miriam ^a   Wortelboer, Heleen M ^a  

^a TNO   (Netherlands)

^b Janssen Pharmaceutica NV   (Netherlands)

Author keywords

Hepatic disposition; OATP; PBPK model; Polymorphisms; Protein abundance; Transfected cell lines

Indexed keywords

DRUG CARRIER; ORGANIC ANION TRANSPORTER B; ROSUVASTATIN; SOLUTE CARRIER ORGANIC ANION TRANSPORTER 1B1; SOLUTE CARRIER ORGANIC ANION TRANSPORTER 1B3; CARRIER PROTEIN; FLUOROBENZENE; ORGANIC ANION TRANSPORTER; PYRIMIDINE DERIVATIVE; SULFONAMIDE;

ARTICLE; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DISPOSITION; DRUG TRANSPORT; ENTEROHEPATIC CIRCULATION; GENE OVEREXPRESSION; GENETIC TRANSFECTION; GENETIC VARIABILITY; HEK293 CELL LINE; HUMAN; HUMAN CELL; HUMAN TISSUE; IN VITRO STUDY; IN VIVO STUDY; INTRINSIC CLEARANCE; LIQUID CHROMATOGRAPHY; LIVER; LIVER CELL; MODEL; OUTER MEMBRANE; PHYSIOLOGY BASED PHARMACOKINETIC MODEL; PREDICTION; PROTEIN ANALYSIS; SIMULATION; SINGLE DRUG DOSE; TANDEM MASS SPECTROMETRY; ADULT; CELL LINE; DRUG INTERACTION; MALE; METABOLISM; PHYSIOLOGY; TRANSPORT AT THE CELLULAR LEVEL;

ADULT; BIOLOGICAL TRANSPORT; CELL LINE; DRUG INTERACTIONS; FLUOROBENZENES; HEK293 CELLS; HEPATOCYTES; HUMANS; LIVER; MALE; MEMBRANE TRANSPORT PROTEINS; ORGANIC ANION TRANSPORTERS; PYRIMIDINES; SULFONAMIDES; TRANSFECTION;

EID: 84908003218     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2014.09.007     Document Type: Article

References (56)

1. A. Asberg Interactions between cyclosporin and lipid-lowering drugs, implications for organ transplant recipients Drugs 63 4 2003 367 378
2. E. Bergman, P. Forsell, A. Tevell, E.M. Persson, M. Hedeland, U. Bondesson, L. Knutson, and H. Lennernäs Biliary secretion of rosuvastatin and bile acids in humans during the absorption phase Eur. J. Pharm. Sci. 29 3-4 2006 205 214
3. Y.A. Bi, X. Qiu, C.J. Rotter, E. Kimoto, M. Piotrowski, M.V. Varma, A.F. Ei-Kattan, and Y. Lai Quantitative assessment of the contribution of sodium-dependent taurocholate co-transporting polypeptide (NTCP) to the hepatic uptake of rosuvastatin, pitavastatin and fluvastatin Biopharm. Drug Dispos. 34 8 2013 452 461
4. P. Borst, and R.O. Elferink Mammalian ABC transporters in health and disease Annu. Rev. Biochem. 71 2002 537 592
5. S. Bosgra, J. van Eijkeren, P. Bos, M. Zeilmaker, and W. Slob An improved model to predict physiologically based model parameters and their inter-individual variability from anthropometry Crit. Rev. Toxicol. 42 9 2012 751 767
6. F. Campolongo, and A. Saltelli Sensitivity analysis of an environmental model; a worked application of different analysis methods Reliab. Eng. Syst. Saf. 57 1997 49 69
7. J.H. Choi, M.G. Lee, J.Y. Cho, J.E. Lee, K.H. Kim, and K. Park Influence of OATP1B1 genotype on the pharmacokinetics of rosuvastatin in Koreans Clin. Pharmacol. Ther. 83 2 2008 251 257
8. C. Fahrmayr, M.F. Fromm, and J. König Hepatic OATP and OCT uptake transporters: their role for drug-drug interactions and pharmacogenetic aspects Drug Metab. Rev. 42 3 2010 380 401
9. L. Fan, W. Zhang, D. Guo, Z.R. Tan, P. Xu, Q. Li, Y.Z. Liu, L. Zhang, T.Y. He, D.L. Hu, D. Wang, and H.H. Zhou The effect of herbal medicine baicalin on pharmacokinetics of rosuvastatin, substrate of organic anion-transporting polypeptide 1B1 Clin. Pharmacol. Ther. 83 3 2008 471 476
10. M. Germani, P. Crivori, M. Rocchetti, P.S. Burton, A.G. Wilson, M.E. Smith, and I. Poggesi Evaluation of a basic physiologically based pharmacokinetic model for simulating the first-time-in-animal study Eur. J. Pharm. Sci. 31 3-4 2007 190 201
11. H. Gutmann, P. Hruz, C. Zimmermann, C. Beglinger, and J. Drewe Distribution of breast cancer resistance protein (BCRP/ABCG2) mRNA expression along the human GI tract Biochem. Pharmacol. 70 5 2005 695 699
12. B. Hagenbuch, and B. Stieger The SLCO (former SLC21) superfamily of transporters Mol. Aspects Med. 34 2-3 2013 396 412
13. S. Hammad, S. Hoehme, A. Friebel, I. von Recklinghausen, A. Othman, B. Begher-Tibbe, R. Reif, P. Godoy, T. Johann, A. Vartak, K. Golka, P.O. Bucur, E. Vibert, R. Marchan, B. Christ, S. Dooley, C. Meyer, I. Ilkavets, U. Dahmen, O. Dirsch, J. Böttger, R. Gebhardt, D. Drasdo, and J.G. Hengstler Protocols for staining of bile canalicular and sinusoidal networks of human, mouse and pig livers, three-dimensional reconstruction and quantification of tissue microarchitecture by image processing and analysis Arch. Toxicol. 88 5 2014 1161 1183
14. M. Hirano, K. Maeda, Y. Shitara, and Y. Sugiyama Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans J. Pharmacol. Exp. Ther. 311 1 2004 139 146
15. R.H. Ho, R.G. Tirona, B.F. Leake, H. Glaeser, W. Lee, C.J. Lemke, Y. Wang, and R.B. Kim Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics Gastroenterology 130 6 2006 1793 1806
16. ICRP Basic Anatomical and Physiological Data for Use in Radiological Protection: Reference Values 2003 Elsevier Science Amsterdam, The Netherlands
17. N. Ishiguro, K. Maeda, T. Ebner, W. Roth, T. Igarashi, and Y. Sugiyama Involvement of OATP1B3 in the hepatic uptake of telmisartan, an angiotensin II receptor antagonist Drug Metab. Rev. 37 suppl. 2 2005 57 (abstract No. 84)
18. K. Ito, and J.B. Houston 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 5 2004 785 792
19. M. Jamei, F. Bajot, S. Neuhoff, Z. Barter, J. Yang, A. Rostami-Hodjegan, and K. Rowland-Yeo A mechanistic framework for in vitro-in vivo extrapolation of liver membrane transporters: prediction of drug-drug interaction between rosuvastatin and cyclosporine Clin. Pharmacokinet. 53 1 2014 73 87
20. H.M. Jones, H.A. Barton, Y. Lai, Y.A. Bi, E. Kimoto, S. Kempshall, S.C. Tate, A. El-Kattan, J.B. Houston, A. Galetin, and K.S. Fenner Mechanistic pharmacokinetic modeling for the prediction of transporter-mediated disposition in humans from sandwich culture human hepatocyte data Drug Metab. Dispos. 40 5 2012 1007 1017
21. J. Kamiie, S. Ohtsuki, R. Iwase, K. Ohmine, Y. Katsukura, K. Yanai, Y. Sekine, Y. Uchida, S. Ito, and T. Terasaki Quantitative atlas of membrane transporter proteins: development and application of a highly sensitive simultaneous LC/MS/MS method combined with novel in-silico peptide selection criteria Pharm. Res. 25 6 2008 1469 1483
22. S. Kitamura, K. Maeda, Y. Wang, and Y. Sugiyama Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin Drug Metab. Dispos. 36 10 2008 2014 2023
23. N. Kotani, K. Maeda, T. Watanabe, M. Hiramatsu, L.K. Gong, Y.A. Bi, T. Takezawa, H. Kusuhara, and Y. Sugiyama Culture period-dependent changes in the uptake of transporter substrates in sandwich-cultured rat and human hepatocytes Drug Metab. Dispos. 39 9 2011 1503 1510
24. X.N. Li, H.R. Xu, W.L. Chen, N.N. Chu, and J.R. Zhu Pharmacokinetics of rosuvastatin in healthy Chinese volunteers living in China: a randomized, open-label, ascending single- and multiple-dose study Clin. Ther. 32 3 2010 575 587
25. J. Lippert, M. Brosch, O. Von Kampen, M. Meyer, H.U. Siegmund, C. Schafmayer, T. Becker, B. Laffert, L. Görlitz, S. Schreiber, P.J. Neuvonen, M. Niemi, J. Hampe, and L. Kuepfer A mechanistic, model-based approach to safety assessment in clinical development CPT Pharmacometrics Syst. Pharmacol. 1 11 2012 e13
26. L. Liu, and K.S. Pang The roles of transporters and enzymes in hepatic drug processing Drug Metab. Dispos. 33 1 2005 1 9
27. L. Liu, and K.S. Pang An integrated approach to model hepatic drug clearance Eur. J. Pharm. Sci. 29 3-4 2006 215 230
28. P.D. Martin, M.J. Warwick, A.L. Dane, C. Brindley, and T. Short Absolute oral bioavailability of rosuvastatin in healthy white adult male volunteers Clin. Ther. 25 10 2003 2553 2563
29. P.D. Martin, M.J. Warwick, A.L. Dane, and M.V. Cantarini A double-blind, randomized, incomplete crossover trial to assess the dose proportionality of rosuvastatin in healthy volunteers Clin. Ther. 25 8 2003 2215 2224
30. P.D. Martin, M.J. Warwick, A.L. Dane, S.J. Hill, P.B. Giles, P.J. Phillips, and E. Lenz Metabolism, excretion, and pharmacokinetics of rosuvastatin in healthy adult male volunteers Clin. Ther. 25 11 2003 2822 2835
31. K. McNally, R. Cotton, and G.D. Loizou A workflow for global sensitivity analysis of PBPK models Front. Pharmacol. 2 2011 31
32. M.D. Morris Factorial sampling plans for preliminary computational experiments Technometrics 33 2 1991 161 174
33. K. Nezasa, A. Takao, K. Kimura, M. Takaichi, K. Inazawa, and M. Koike Pharmacokinetics and disposition of rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, in rat Xenobiotica 32 8 2002 715 727
34. S. Ohtsuki, O. Schaefer, H. Kawakami, T. Inoue, S. Liehner, A. Saito, N. Ishiguro, W. Kishimoto, E. Ludwig-Schwellinger, T. Ebner, and T. Terasaki Simultaneous absolute protein quantification of transporters, cytochromes P450, and UDP-glucuronosyltransferases as a novel approach for the characterization of individual human liver: comparison with mRNA levels and activities Drug Metab. Dispos. 40 1 2012 83 92
35. M.K. Pasanen, H. Fredrikson, P.J. Neuvonen, and M. Niemi Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin Clin. Pharmacol. Ther. 82 6 2007 726 733
36. M.K. Pasanen, P.J. Neuvonen, and M. Niemi Global analysis of genetic variation in SLCO1B1 Pharmacogenomics 9 1 2008 19 33
37. N.D. Pfeifer, K. Yang, and K.L. Brouwer Hepatic basolateral efflux contributes significantly to rosuvastatin disposition I: characterization of basolateral versus biliary clearance using a novel protocol in sandwich-cultured hepatocytes J. Pharmacol. Exp. Ther. 347 3 2013 727 736
38. N.D. Pfeifer, A.S. Bridges, B.C. Ferslew, R.N. Hardwick, and K.L. Brouwer Hepatic basolateral efflux contributes significantly to rosuvastatin disposition II: characterization of hepatic elimination by basolateral, biliary, and metabolic clearance pathways in rat isolated perfused liver J. Pharmacol. Exp. Ther. 347 3 2013 737 745
39. P.A. Pham, C.J. la Porte, L.S. Lee, R. van Heeswijk, J.P. Sabo, M.M. Elgadi, P.J. Piliero, P. Barditch-Crovo, E. Fuchs, C. Flexner, and D.W. Cameron Differential effects of tipranavir plus ritonavir on atorvastatin or rosuvastatin pharmacokinetics in healthy volunteers Antimicrob. Agents Chemother. 53 10 2009 4385 4392
40. A. Poirier, T. Lavé, R. Portmann, M.E. Brun, F. Senner, M. Kansy, H.P. Grimm, and C. Funk Design, data analysis, and simulation of in vitro drug transport kinetic experiments using a mechanistic in vitro model Drug Metab. Dispos. 36 12 2008 2434 2444
41. A. Poirier, A.C. Cascais, C. Funk, and T. Lavé Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data J. Pharmacokinet Pharmacodyn. 36 6 2009 585 611
42. A. Poirier, C. Funk, J.M. Scherrmann, and T. Lavé Mechanistic modeling of hepatic transport from cells to whole body: application to napsagatran and fexofenadine Mol. Pharm. 6 6 2009 1716 1733
43. P. Poulin, and F.P. Theil A priori prediction of tissue:plasma partition coefficients of drugs to facilitate the use of physiologically-based pharmacokinetic models in drug discovery J. Pharm. Sci. 89 1 2000 16 35
44. M.S. Roberts, and M. Rowland A dispersion model of hepatic elimination: 1. Formulation of the model and bolus considerations J. Pharmacokinet. Biopharm. 14 3 1986 227 260
45. A.H. Schinkel, and J.W. Jonker Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview Adv. Drug Deliv. Rev. 64 2003 138 153
46. Y. Shitara, D. Sugiyama, H. Kusuhara, Y. Kato, T. Abe, P.J. Meier, T. Itoh, and Y. Sugiyama Comparative inhibitory effects of different compounds on rat oatp1 (Slc21a1)- and Oatp2 (Slc21a5)-mediated transport Pharm. Res. 19 2002 147 153
47. Y. Shitara, T. Horie, and Y. Sugiyama Transporters as a determinant of drug clearance and tissue distribution Eur. J. Pharm. Sci. 27 5 2006 425 446
48. S.G. Simonson, A. Raza, P.D. Martin, P.D. Mitchell, J.A. Jarcho, C.D. Brown, A.S. Windass, and D.W. Schneck Rosuvastatin pharmacokinetics in heart transplant recipients administered an antirejection regimen including cyclosporine Clin. Pharmacol. Ther. 76 2 2004 167 177
49. A.K. Sohlenius-Sternbeck Determination of the hepatocellularity number for human, dog, rabbit, rat and mouse livers from protein concentration measurements Toxicol. In Vitro 20 8 2006 1582 1586
50. K. Takeuchi, T. Sugiura, K. Matsubara, R. Sato, T. Shimizu, Y. Masuo, M. Horikawa, N. Nakamichi, N. Ishiwata, and Y. Kato Interaction of novel platelet-increasing agent eltrombopag with rosuvastatin via breast cancer resistance protein in humans Drug Metab. Dispos. 42 4 2014 726 734
51. E. Van de Steeg, R. Greupink, M. Schreurs, I.H. Nooijen, K.C. Verhoeckx, R. Hanemaaijer, D. Ripken, M. Monshouwer, M.L. Vlaming, J. DeGroot, M. Verwei, F.G. Russel, M.T. Huisman, and H.M. Wortelboer Drug-drug interactions between rosuvastatin and oral antidiabetic drugs occurring at the level of OATP1B1 Drug Metab. Dispos. 41 3 2013 592 601
52. A. Vildhede, M. Karlgren, E.K. Svedberg, J.R. Wisniewski, Y. Lai, A. Norén, and P. Artursson Hepatic uptake of atorvastatin: influence of variability in transporter expression on uptake clearance and drug-drug interactions Drug Metab. Dispos. 42 7 2014 1210 1218
53. T. Watanabe, K. Maeda, T. Kondo, H. Nakayama, S. Horita, H. Kusuhara, and Y. Sugiyama Prediction of the hepatic and renal clearance of transporter substrates in rats using in vitro uptake experiments Drug Metab. Dispos. 37 7 2009 1471 1479
54. T. Watanabe, H. Kusuhara, K. Maeda, Y. Shitara, and Y. Sugiyama Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans J. Pharmacol. Exp. Ther. 328 2 2009 652 662
55. Y. Yabe, A. Galetin, and J.B. Houston Kinetic characterization of rat hepatic uptake of 16 actively transported drugs Drug Metab. Dispos. 39 10 2011 1808 1814
56. M.J. Zamek-Gliszczynski, C.A. Lee, A. Poirier, J. Bentz, X. Chu, H. Ellens, T. Ishikawa, M. Jamei, J.C. Kalvass, S. Nagar, K.S. Pang, K. Korzekwa, P.W. Swaan, M.E. Taub, P. Zhao, A. Galetin, and International Transporter Consortium ITC recommendations for transporter kinetic parameter estimation and translational modeling of transport-mediated PK and DDIs in humans Clin. Pharmacol. Ther. 94 1 2013 64 79