Application of a physiologically based pharmacokinetic model to predict OATP1B1-Related variability in pharmacodynamics of rosuvastatin

CPT: Pharmacometrics and Systems Pharmacology

Volumn 3, Issue 7, 2014, Pages

  Rose, R H ^a   Neuhoff, S ^a   Abduljalil, K ^a   Chetty, M ^a   Rostami Hodjegan, A ^a,b   Jamei, M ^a  

^a CERTARA UK LIMITED   (United Kingdom)

^b UNIVERSITY OF MANCHESTER   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ROSUVASTATIN; SOLUTE CARRIER ORGANIC ANION TRANSPORTER 1B1;

AREA UNDER THE CURVE; ARTICLE; CHOLESTEROL SYNTHESIS; CONCENTRATION (PARAMETERS); CONTROLLED STUDY; DNA POLYMORPHISM; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG RESPONSE; GENE; GENETIC VARIABILITY; GENOTYPE; HETEROZYGOTE; IC 50; LIVER; MODEL; OATP1B1 GENE; PHARMACOKINETIC PHARMACODYNAMIC MODEL; PLASMA CONCENTRATION-TIME CURVE; PREDICTION; PRIORITY JOURNAL; WILD TYPE;

EID: 84905370710     PISSN: None     EISSN: 21638306     Source Type: Journal    
DOI: 10.1038/psp.2014.24     Document Type: Article

References (46)

1. Zhao, P., Rowland, M. & Huang, S.M. Best practice in the use of physiologically based pharmacokinetic modeling and simulation to address clinical pharmacology regulatory questions. Clin. Pharmacol. Ther. 92, 17-20 (2012).
2. Zhao, P. et al. Applications of physiologically based pharmacokinetic (PBPK) modeling and simulation during regulatory review. Clin. Pharmacol. Ther. 89, 259-267 (2011).
3. Perera, V., Elmeliegy, M.A., Rao, G. & Forrest, A. The link between pharmacodynamics and physiologically based pharmacokinetic models. Clin. Pharmacol. Ther. 93, 151-152 (2013).
4. Rostami-Hodjegan, A. Response to "The link between pharmacodynamics and physiologically based pharmacokinetic models." Clin. Pharmacol. Ther. 93, 152 (2013).
5. Watanabe, T., Kusuhara, H., Maeda, K., Shitara, Y. & Sugiyama, Y. Physiologically based pharmacokinetic modeling to predict transporter-mediated clearance and distribution of pravastatin in humans. J. Pharmacol. Exp. Ther. 328, 652-662 (2009).
6. Ahmad, S. et al. (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(methyl(1- methyl-1h-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic acid (BMS-644950): a rationally designed orally efficacious 3-hydroxy-3- methylglutaryl coenzyme-A reductase inhibitor with reduced myotoxicity potential. J. Med. Chem. 51, 2722-2733 (2008).
7. Martin, P.D., Mitchell, P.D. & Schneck, D.W. Pharmacodynamic effects and pharmacokinetics of a new HMG-CoA reductase inhibitor, rosuvastatin, after morning or evening administration in healthy volunteers. Br. J. Clin. Pharmacol. 54, 472-477 (2002).
8. Ho, R.H. et al. Drug and bile acid transporters in rosuvastatin hepatic uptake: function, expression, and pharmacogenetics. Gastroenterology 130, 1793-1806 (2006).
9. Kitamura, S., Maeda, K., Wang, Y. & Sugiyama, Y. Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab. Dispos. 36, 2014-2023 (2008).
10. Hu, M., To, K.K., Mak, V.W. & Tomlinson, B. The ABCG2 transporter and its relations with the pharmacokinetics, drug interaction and lipid-lowering effects of statins. Expert Opin. Drug Metab. Toxicol. 7, 49-62 (2011).
11. Ellis, L.C., Hawksworth, G.M. & Weaver, R.J. ATP-dependent transport of statins by human and rat MRP2/Mrp2. Toxicol. Appl. Pharmacol. 269, 187-194 (2013).
12. Li, M. et al. Identification of interspecies difference in efflux transporters of hepatocytes from dog, rat, monkey and human. Eur. J. Pharm. Sci. 35, 114-126 (2008)
13. Jamei, M. et al. 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, 73-87 (2014).
14. Giacomini, K.M. et al.; International Transporter Consortium. International Transporter Consortium commentary on clinically important transporter polymorphisms. Clin. Pharmacol. Ther. 94, 23-26 (2013).
15. Bailey, K.M. et al.; SPACE ROCKET Trial Group. Hepatic metabolism and transporter gene variants enhance response to rosuvastatin in patients with acute myocardial infarction: the GEOSTAT-1 Study. Circ. Cardiovasc. Genet. 3, 276-285 (2010).
16. Niemi, M., Pasanen, M.K. & Neuvonen, P.J. Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol. Rev. 63, 157-181 (2011).
17. Pasanen, M.K., Fredrikson, H., Neuvonen, P.J. & Niemi, M. Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin. Clin. Pharmacol. Ther. 82, 726-733 (2007).
18. Link, E. et al. SLCO1B1 variants and statin-induced myopathy-A genomewide study. N. Engl. J. Med. 359, 789-799 (2008).
19. Puccetti, L., Ciani, F. & Auteri, A. Genetic involvement in statins induced myopathy. Preliminary data from an observational case-control study. Atherosclerosis 211, 28-29 (2010).
20. Voora, D. et al. The SLCO1B1*5 genetic variant is associated with statin-induced side effects. J. Am. Coll. Cardiol. 54, 1609-1616 (2009).
21. Aoyama, T. et al. Pharmacokinetic/pharmacodynamic modeling and simulation of rosuvastatin using an extension of the indirect response model by incorporating a circadian rhythm. Biol. Pharm. Bull. 33, 1082-1087 (2010).
22. Van De Steeg, E. et al. Combined analysis of pharmacokinetic and efficacy data of preclinical studies with statins markedly improves translation of drug efficacy to human trials. J. Pharmacol. Exp. Ther. 347, 635-644 (2013).
23. Jones, H.M. et al. Mechanistic pharmacokinetic modeling for the prediction of transportermediated disposition in humans from sandwich culture human hepatocyte data. Drug Metab. Dispos. 40, 1007-1017 (2012).
24. Hobbs, M., Parker, C., Birch, H. & Kenworthy, K. Understanding the interplay of drug transporters involved in the disposition of rosuvastatin in the isolated perfused rat liver using a physiologically-based pharmacokinetic model. Xenobiotica. 42, 327-338 (2012).
25. Lee, E. et al. Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment. Clin. Pharmacol. Ther. 78, 330-341 (2005).
26. Van De Steeg, E. et al. Drug-drug interactions between rosuvastatin and oral antidiabetic drugs occurring at the level of OATP1B1. Drug Metab Dispos. 41, 592-601 (2013).
27. Prasad, B. et al. Interindividual variability in hepatic organic anion-transporting polypeptides and P-glycoprotein (ABCB1) protein expression: quantification by liquid chromatography tandem mass spectroscopy and influence of genotype, age, and sex. Drug Metab. Dispos. 42, 78-88 (2014).
28. McTaggart, F. et al. Preclinical and clinical pharmacology of Rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am. J. Cardiol. 87, 28B-32B (2001).
29. Holdgate, G.A., Ward, W.H. & McTaggart, F. Molecular mechanism for inhibition of 3-hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase by rosuvastatin. Biochem. Soc. Trans. 31, 528-531 (2003).
30. Pasanen, M.K., Miettinen, T.A., Gylling, H., Neuvonen, P.J. & Niemi, M. Polymorphism of the hepatic influx transporter organic anion transporting polypeptide 1B1 is associated with increased cholesterol synthesis rate. Pharmacogenet. Genomics 18, 921-926 (2008).
31. Tachibana-Iimori, R. et al. Effect of genetic polymorphism of OATP-C (SLCO1B1) on lipid-lowering response to HMG-CoA reductase inhibitors. Drug Metab. Pharmacokinet. 19, 375-380 (2004).
32. Chasman, D.I., Giulianini, F., MacFadyen, J., Barratt, B.J., Nyberg, F. & Ridker, P.M. Genetic determinants of statin-induced low-density lipoprotein cholesterol reduction: the Justification for the Use of Statins in Prevention: an Intervention Trial Evaluating Rosuvastatin (JUPITER) trial. Circ. Cardiovasc. Genet. 5, 257-264 (2012).
33. Levy, G. Predicting effective drug concentrations for individual patients. Determinants of pharmacodynamic variability. Clin. Pharmacokinet. 34, 323-333 (1998).
34. Niemi, M. Transporter pharmacogenetics and statin toxicity. Clin. Pharmacol. Ther. 87, 130-133 (2010).
35. Knauer, M.J. et al. Human skeletal muscle drug transporters determine local exposure and toxicity of statins. Circ. Res. 106, 297-306 (2010).
36. Rodgers, T. & Rowland, M. Physiologically based pharmacokinetic modelling 2: predicting the tissue distribution of acids, very weak bases, neutrals and zwitterions. J. Pharm. Sci. 95, 1238-1257 (2006).
37. Pfeifer, N.D., Yang, K. & Brouwer, K.L. 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, 727-736 (2013).
38. Jamei, M. et al. Population-based mechanistic prediction of oral drug absorption. AAPS J. 11, 225-237 (2009).
39. Man, M. et al. Genetic variation in metabolizing enzyme and transporter genes: comprehensive assessment in 3 major East Asian subpopulations with comparison to Caucasians and Africans. J. Clin. Pharmacol. 50, 929-940 (2010).
40. Mwinyi, J., Köpke, K., Schaefer, M., Roots, I. & Gerloff, T. Comparison of SLCO1B1 sequence variability among German, Turkish, and African populations. Eur. J. Clin. Pharmacol. 64, 257-266 (2008).
41. Niemi, M. et al. High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1). Pharmacogenetics 14, 429-440 (2004).
42. Pasanen, M.K., Backman, J.T., Neuvonen, P.J. & Niemi, M. Frequencies of single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide 1B1 SLCO1B1 gene in a Finnish population. Eur. J. Clin. Pharmacol. 62, 409-415 (2006).
43. Pasanen, M.K., Neuvonen, P.J. & Niemi, M. Global analysis of genetic variation in SLCO1B1. Pharmacogenomics 9, 19-33 (2008).
44. Thompson, J.F. et al. An association study of 43 SNPs in 16 candidate genes with atorvastatin response. Pharmacogenomics J. 5, 352-358 (2005).
45. Tirona, R.G., Leake, B.F., Merino, G. & Kim, R.B. Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European-and African-Americans. J. Biol. Chem. 276, 35669-35675 (2001).
46. Loucks, D.P., van Beek, E., Stedinger, J.R., Dijkman, J.P.M. & Villars, M.T. Water Resources Systems Planning and Management: An Introduction to Methods, Models and Applications. (UNESCO, Paris, 2005).