Clinical significance of organic anion transporting polypeptides (OATPs) in drug disposition: Their roles in hepatic clearance and intestinal absorption

Biopharmaceutics and Drug Disposition

Volumn 34, Issue 1, 2013, Pages 45-78

  Shitara, Yoshihisa ^a   Maeda, Kazuya ^b   Ikejiri, Kazuaki ^b   Yoshida, Kenta ^b   Horie, Toshiharu ^c   Sugiyama, Yuichi ^d  

^a MEIJI SEIKA KAISHA LTD   (Japan)

^b UNIVERSITY OF TOKYO   (Japan)

^c CHIBA UNIVERSITY   (Japan)

^d RIKEN   (Japan)

Author keywords

clearance; drug drug interaction; genetic polymorphism; organic anion transporting polypeptide; PBPK modeling; tissue distribution

Indexed keywords

ALISKIREN; ALPRAZOLAM; AMITRIPTYLINE; ATORVASTATIN; CLARITHROMYCIN; DEXTROMETHORPHAN; DILTIAZEM; DOMPERIDONE; ERYTHROMYCIN; FIRTECAN; FLUINDOSTATIN; GEMFIBROZIL; IBUPROFEN; IMIPRAMINE; ITRACONAZOLE; LABETALOL; LAVOLTIDINE; LOPINAVIR; OLMESARTAN; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 1A 2; ORGANIC ANION TRANSPORTER 1B 3; ORGANIC ANION TRANSPORTER 2; ORGANIC ANION TRANSPORTER 2B 1; PACLITAXEL; PRAVASTATIN; ROSUVASTATIN; TALINOLOL; TORASEMIDE; UNCLASSIFIED DRUG; UNINDEXED DRUG; WARFARIN;

APPLE JUICE; AREA UNDER THE CURVE; BLOOD BRAIN BARRIER; BRUSH BORDER; CAPILLARY BLOOD; DRUG ABSORPTION; DRUG ACTIVITY; DRUG BINDING SITE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISPOSITION; DRUG DISTRIBUTION; DRUG ELIMINATION; DRUG EXPOSURE; DRUG METABOLISM; DRUG TRANSPORT; DRUG UPTAKE; GENETIC POLYMORPHISM; GRAPEFRUIT JUICE; HUMAN; IC 50; INTESTINE ABSORPTION; LIVER CELL; LIVER CLEARANCE; LIVER MICROSOME; MEMBRANE TRANSPORT; NONHUMAN; NUCLEOTIDE SEQUENCE; ORANGE JUICE; PHARMACOPHORE; PHYSICAL CHEMISTRY; PROTEIN DETERMINATION; PROTEIN EXPRESSION; PROTEIN FUNCTION; REVIEW; SEQUENCE HOMOLOGY; SIMULATION; TISSUE DISTRIBUTION;

ANIMALS; BIOLOGICAL TRANSPORT; BLOOD-BRAIN BARRIER; COMPUTER SIMULATION; HUMANS; INTESTINAL ABSORPTION; LIVER; MODELS, BIOLOGICAL; ORGANIC ANION TRANSPORTERS; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; PHARMACEUTICAL PREPARATIONS; POLYMORPHISM, GENETIC; TISSUE DISTRIBUTION;

EID: 84872229531     PISSN: 01422782     EISSN: 1099081X     Source Type: Journal    
DOI: 10.1002/bdd.1823     Document Type: Review

References (175)

1. Giacomini KM, Huang SM, Tweedie DJ, et al,. Membrane transporters in drug development. Nat Rev Drug Discov 2010; 9: 215-236.
2. Mizuno N, Niwa T, Yotsumoto Y, Sugiyama Y,. Impact of drug transporter studies on drug discovery and development. Pharmacol Rev 2003; 55: 425-461.
3. Schinkel AH, Jonker JW,. Mammalian drug efflux transporters of the ATP binding cassette (ABC) family: an overview. Adv Drug Deliv Rev 2003; 55: 3-29.
4. Koepsell H, Endou H,. The SLC22 drug transporter family. Pflugers Arch 2004; 447: 666-676.
5. Tsuji A, Tamai I,. Carrier-mediated intestinal transport of drugs. Pharm Res 1996; 13: 963-977.
6. Tamai I,. Oral drug delivery utilizing intestinal OATP transporters. Adv Drug Deliv Rev 2011; 64: 508-514.
7. Giacomini KM, Sugiyama Y,. Membrane transporters and drug response. In Goodman & Gilman's the Pharmacological Basis of Therapeutics (12th edn)., Brunton LL, Blumenthal DK, Murri N, Dandan RH, Knollmann BC, (eds). McGraw-Hill Professional: New York, 2010.
8. Yamazaki M, Suzuki H, Sugiyama Y,. Recent advances in carrier-mediated hepatic uptake and biliary excretion of xenobiotics. Pharm Res 1996; 13: 497-513.
9. Shitara Y, Sugiyama Y,. 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 2006; 112: 71-105.
10. Shitara Y, Horie T, Sugiyama Y,. Transporters as a determinant of drug clearance and tissue distribution. Eur J Pharm Sci 2006; 27: 425-446.
11. Zhang L, Strong JM, Qiu W, Lesko LJ, Huang SM,. Scientific perspectives on drug transporters and their role in drug interactions. Mol Pharm 2006; 3: 62-69.
12. Huang SM, Strong JM, Zhang L, et al,. New era in drug interaction evaluation: US Food and Drug Administration update on CYP enzymes, transporters, and the guidance process. J Clin Pharmacol 2008; 48: 662-670.
13. Zhang L, Zhang YD, Strong JM, Reynolds KS, Huang SM,. A regulatory viewpoint on transporter-based drug interactions. Xenobiotica 2008; 38: 709-724.
14. Meier PJ, Eckhardt U, Schroeder A, Hagenbuch B, Stieger B,. Substrate specificity of sinusoidal bile acid and organic anion uptake systems in rat and human liver. Hepatology 1997; 26: 1667-1677.
15. Hagenbuch B, Meier PJ,. The superfamily of organic anion transporting polypeptides. Biochim Biophys Acta 2003; 1609: 1-18.
16. Ieiri I, Doi Y, Maeda K, et al,. Microdosing clinical study: pharmacokinetic, pharmacogenomic (SLCO2B1), and interaction (grapefruit juice) profiles of celiprolol following the oral microdose and therapeutic dose. J Clin Pharmacol 2012; 52: 1078-1089.
17. Mougey EB, Lang JE, Wen X, Lima JJ,. Effect of citrus juice and SLCO2B1 genotype on the pharmacokinetics of montelukast. J Clin Pharmacol 2011; 51: 751-760.
18. Dawson PA, Hubbert M, Haywood J, et al,. The heteromeric organic solute transporter alpha-beta, Ostalpha-Ostbeta, is an ileal basolateral bile acid transporter. J Biol Chem 2005; 280: 6960-6968.
19. Rao A, Haywood J, Craddock AL, Belinsky MG, Kruh GD, Dawson PA,. The organic solute transporter alpha-beta, Ostalpha-Ostbeta, is essential for intestinal bile acid transport and homeostasis. Proc Natl Acad Sci USA 2008; 105: 3891-3896.
20. Kitamura Y, Hirouchi M, Kusuhara H, Schuetz JD, Sugiyama Y,. Increasing systemic exposure of methotrexate by active efflux mediated by multidrug resistance-associated protein 3 (mrp3/abcc3). J Pharmacol Exp Ther 2008; 327: 465-473.
21. Kitamura Y, Kusuhara H, Sugiyama Y,. Basolateral efflux mediated by multidrug resistance-associated protein 3 (Mrp3/Abcc3) facilitates intestinal absorption of folates in mouse. Pharm Res 2010; 27: 665-672.
22. Murakami T, Takano M,. Intestinal efflux transporters and drug absorption. Expert Opin Drug Metab Toxicol 2008; 4: 923-939.
23. Paine MF, Khalighi M, Fisher JM, et al,. Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 1997; 283: 1552-1562.
24. Kato M,. Intestinal first-pass metabolism of CYP3A4 substrates. Drug Metab Pharmacokinet 2008; 23: 87-94.
25. Tachibana T, Kato M, Takano J, Sugiyama Y,. Predicting drug-drug interactions involving the inhibition of intestinal CYP3A4 and P-glycoprotein. Curr Drug Metab 2010; 11: 762-777.
26. Lee W, Glaeser H, Smith LH, et al,. Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug entry. J Biol Chem 2005; 280: 9610-9617.
27. Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ,. Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther 2000; 294: 73-79.
28. Abe T, Kakyo M, Tokui T, et al,. Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem 1999; 274: 17159-17163.
29. Hsiang B, Zhu Y, Wang Z, et al,. A novel human hepatic organic anion transporting polypeptide (OATP2). Identification of a liver-specific human organic anion transporting polypeptide and identification of rat and human hydroxymethylglutaryl-CoA reductase inhibitor transporters. J Biol Chem 1999; 274: 37161-37168.
30. Konig J, Cui Y, Nies AT, Keppler D,. A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane. Am J Physiol Gastrointest Liver Physiol 2000; 278: G156-G164.
31. Tamai I, Nezu J, Uchino H, et al,. Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun 2000; 273: 251-260.
32. Konig J, Cui Y, Nies AT, Keppler D,. Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide. J Biol Chem 2000; 275: 23161-23168.
33. Abe T, Unno M, Onogawa T, et al,. LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology 2001; 120: 1689-1699.
34. Muto M, Onogawa T, Suzuki T, et al,. Human liver-specific organic anion transporter-2 is a potent prognostic factor for human breast carcinoma. Cancer Sci 2007; 98: 1570-1576.
35. Ose A, Kusuhara H, Endo C, et al,. Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier. Drug Metab Dispos 2010; 38: 168-176.
36. Kusama M, Toshimoto K, Maeda K, et al,. In silico classification of major clearance pathways of drugs with their physiochemical parameters. Drug Metab Dispos 2010; 38: 1362-1370.
37. Karlgren M, Ahlin G, Bergstrom CA, Svensson R, Palm J, Artursson P,. In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res 2012; 29: 411-426.
38. Chang C, Pang KS, Swaan PW, Ekins S,. Comparative pharmacophore modeling of organic anion transporting polypeptides: a meta-analysis of rat Oatp1a1 and human OATP1B1. J Pharmacol Exp Ther 2005; 314: 533-541.
39. Hirouchi M, Kusuhara H, Onuki R, Ogilvie BW, Parkinson A, Sugiyama Y,. Construction of triple-transfected cells [organic anion-transporting polypeptide (OATP) 1B1/multidrug resistance-associated protein (MRP) 2/MRP3 and OATP1B1/MRP2/MRP4] for analysis of the sinusoidal function of MRP3 and MRP4. Drug Metab Dispos 2009; 37: 2103-2111.
40. Rowland M, Benet LZ, Graham GG,. Clearance concepts in pharmacokinetics. J Pharmacokinet Biopharm 1973; 1: 123-136.
41. Nies AS, Shand DG, Wilkinson GR,. Altered hepatic blood flow and drug disposition. Clin Pharmacokinet 1976; 1: 135-155.
42. Maeda K, Ikeda Y, Fujita T, et al,. Identification of the rate-determining process in the hepatic clearance of atorvastatin in a clinical cassette microdosing study. Clin Pharmacol Ther 2011; 90: 575-581.
43. Lam JL, Benet LZ,. Hepatic microsome studies are insufficient to characterize in vivo hepatic metabolic clearance and metabolic drug-drug interactions: studies of digoxin metabolism in primary rat hepatocytes versus microsomes. Drug Metab Dispos 2004; 32: 1311-1316.
44. Brown HS, Wilby AJ, Alder J, Houston JB,. Comparative use of isolated hepatocytes and hepatic microsomes for cytochrome P450 inhibition studies: transporter-enzyme interplay. Drug Metab Dispos 2010; 38: 2139-2146.
45. Parker AJ, Houston JB,. Rate-limiting steps in hepatic drug clearance: comparison of hepatocellular uptake and metabolism with microsomal metabolism of saquinavir, nelfinavir, and ritonavir. Drug Metab Dispos 2008; 36: 1375-1384.
46. Soars MG, Grime K, Sproston JL, Webborn PJ, Riley RJ,. Use of hepatocytes to assess the contribution of hepatic uptake to clearance in vivo. Drug Metab Dispos 2007; 35: 859-865.
47. Soars MG, Webborn PJ, Riley RJ,. 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 2009; 6: 1662-1677.
48. +-independent multispecific anion transporter mediates active transport of pravastatin into rat liver. Am J Physiol 1993; 264: G36-G44.
49. Ménochet K, Kenworthy KE, Houston JB, Galetin A,. Use of mechanistic modeling to assess interindividual variability and interspecies differences in active uptake in human and rat hepatocytes. Drug Metab Dispos 2012; 40: 1744-1756.
50. Pang KS, Rowland M,. Hepatic clearance of drugs. I. Theoretical considerations of a 'well-stirred' model and a 'parallel tube' model. Influence of hepatic blood flow, plasma and blood cell binding, and the hepatocellular enzymatic activity on hepatic drug clearance. J Pharmacokinet Biopharm 1977; 5: 625-653.
51. Yabe Y, Galetin A, Houston JB,. Kinetic characterization of rat hepatic uptake of 16 actively transported drugs. Drug Metab Dispos 2011; 39: 1808-1814.
52. Nakada T, Maeda K, Ikejiri K, Suzuki M, Sugiyama Y,. In vitro methods for estimating the unbound concentration of drugs using hepatocytes. Abstract for the 19th HAB annual meeting (Tokyo, Japan) May, 2012.
53. Kanamitsu S, Shinozaki Y, Ito K, Iwatsubo T, Suzuki H, Sugiyama Y,. Quantitative prediction of in vivo drug-drug interactions from in vitro data: effects of active transport of inhibitors into the liver. Altern Animal Test Exp 2000; 7: 23-29.
54. Lin JH, Sugiyama Y, Awazu S, Hanano M,. In vitro and in vivo evaluation of the tissue-to-blood partition coefficient for physiological pharmacokinetic models. J Pharmacokinet Biopharm 1982; 10: 637-647.
55. Yamazaki M, Suzuki H, Hanano M, Sugiyama Y,. Different relationships between cellular ATP and hepatic uptake among taurocholate, cholate, and organic anions. Am J Physiol 1993; 264: G693-G701.
56. 2 receptor antagonists, cimetidine and nizatidine, into isolated rat hepatocytes: contribution of type I system. J Pharmacol Exp Ther 1994; 269: 1220-1227.
57. Maeda K, Sugiyama Y,. Impact of genetic polymorphisms of transporters on the pharmacokinetic, pharmacodynamic and toxicological properties of anionic drugs. Drug Metab Pharmacokinet 2008; 23: 223-235.
58. Ieiri I, Higuchi S, Sugiyama Y,. 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 2009; 5: 703-729.
59. Kalliokoski A, Niemi M,. Impact of OATP transporters on pharmacokinetics. Br J Pharmacol 2009; 158: 693-705.
60. Niemi M, Pasanen MK, Neuvonen PJ,. Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev 2011; 63: 157-181.
61. Nakanishi T, Tamai I,. Genetic polymorphisms of OATP transporters and their impact on intestinal absorption and hepatic disposition of drugs. Drug Metab Pharmacokinet 2012; 27: 106-121.
62. Tirona RG, Leake BF, Merino G, Kim RB,. Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans. J Biol Chem 2001; 276: 35669-35675.
63. Nozawa T, Nakajima M, Tamai I, et al,. Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis. J Pharmacol Exp Ther 2002; 302: 804-813.
64. Kameyama Y, Yamashita K, Kobayashi K, Hosokawa M, Chiba K,. Functional characterization of SLCO1B1 (OATP-C) variants, SLCO1B1*5, SLCO1B1*15 and SLCO1B1*15 + C1007G, by using transient expression systems of HeLa and HEK293 cells. Pharmacogenet Genomics 2005; 15: 513-522.
65. Iwai M, Suzuki H, Ieiri I, Otsubo K, Sugiyama Y,. Functional analysis of single nucleotide polymorphisms of hepatic organic anion transporter OATP1B1 (OATP-C). Pharmacogenetics 2004; 14: 749-757.
66. Picard N, Yee SW, Woillard JB, et al,. The role of organic anion-transporting polypeptides and their common genetic variants in mycophenolic acid pharmacokinetics. Clin Pharmacol Ther 2010; 87: 100-108.
67. Kiyotani K, Mushiroda T, Kubo M, Zembutsu H, Sugiyama Y, Nakamura Y,. Association of genetic polymorphisms in SLCO1B3 and ABCC2 with docetaxel-induced leukopenia. Cancer Sci 2008; 99: 967-972.
68. Yamada A, Maeda K, Ishiguro N, et al,. The impact of pharmacogenetics of metabolic enzymes and transporters on the pharmacokinetics of telmisartan in healthy volunteers. Pharmacogenet Genomics 2011; 21: 523-530.
69. Kusama M, Maeda K, Chiba K, Aoyama A, Sugiyama Y,. Prediction of the effects of genetic polymorphism on the pharmacokinetics of CYP2C9 substrates from in vitro data. Pharm Res 2009; 26: 822-835.
70. Zhao P, Vieira ML, Grillo JA, et al,. Evaluation of exposure change of nonrenally eliminated drugs in patients with chronic kidney disease using physiologically based pharmacokinetic modeling and simulation. J Clin Pharmacol 2012; 52: 91S-108S.
71. 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 2009; 328: 652-662.
72. Hagenbuch B, Scharschmidt BF, Meier PJ,. Effect of antisense oligonucleotides on the expression of hepatocellular bile acid and organic anion uptake systems in Xenopus laevis oocytes. Biochem J 1996; 316 (3): 901-904.
73. Kouzuki H, Suzuki H, Ito K, Ohashi R, Sugiyama Y,. Contribution of sodium taurocholate co-transporting polypeptide to the uptake of its possible substrates into rat hepatocytes. J Pharmacol Exp Ther 1998; 286: 1043-1050.
74. Kouzuki H, Suzuki H, Ito K, Ohashi R, Sugiyama Y,. Contribution of organic anion transporting polypeptide to uptake of its possible substrates into rat hepatocytes. J Pharmacol Exp Ther 1999; 288: 627-634.
75. Hirano M, Maeda K, Shitara Y, Sugiyama Y,. Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther 2004; 311: 139-146.
76. Polli JW, Jarrett JL, Studenberg SD, et al,. Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor. Pharm Res 1999; 16: 1206-1212.
77. Letrent SP, Pollack GM, Brouwer KR, Brouwer KL,. Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat. Drug Metab Dispos 1999; 27: 827-834.
78. Ishiguro N, Maeda K, Kishimoto W, et al,. Predominant contribution of OATP1B3 to the hepatic uptake of telmisartan, an angiotensin II receptor antagonist, in humans. Drug Metab Dispos 2006; 34: 1109-1115.
79. Li N, Palandra J, Nemirovskiy OV, Lai Y,. LC-MS/MS mediated absolute quantification and comparison of bile salt export pump and breast cancer resistance protein in livers and hepatocytes across species. Anal Chem 2009; 81: 2251-2259.
80. Li N, Zhang Y, Hua F, Lai Y,. Absolute difference of hepatobiliary transporter multidrug resistance-associated protein (MRP2/Mrp2) in liver tissues and isolated hepatocytes from rat, dog, monkey, and human. Drug Metab Dispos 2009; 37: 66-73.
81. Kamiie J, Ohtsuki S, Iwase R, et al,. 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 2008; 25: 1469-1483.
82. Ito K, Uchida Y, Ohtsuki S, et al,. Quantitative membrane protein expression at the blood-brain barrier of adult and younger cynomolgus monkeys. J Pharm Sci 2011; 100: 3939-3950.
83. Uchida Y, Ohtsuki S, Katsukura Y, et al,. Quantitative targeted absolute proteomics of human blood-brain barrier transporters and receptors. J Neurochem 2011; 117: 333-345.
84. Zhang Y, Li N, Brown PW, Ozer JS, Lai Y,. Liquid chromatography/tandem mass spectrometry based targeted proteomics quantification of P-glycoprotein in various biological samples. Rapid Commun Mass Spectrom 2011; 25: 1715-1724.
85. Ohtsuki S, Schaefer O, Kawakami H, et al,. 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 2012; 40: 83-92.
86. Kitamura S, Maeda K, Wang Y, Sugiyama Y,. Involvement of multiple transporters in the hepatobiliary transport of rosuvastatin. Drug Metab Dispos 2008; 36: 2014-2023.
87. Yamada A, Maeda K, Kamiyama E, et al,. Multiple human isoforms of drug transporters contribute to the hepatic and renal transport of olmesartan, a selective antagonist of the angiotensin II AT1-receptor. Drug Metab Dispos 2007; 35: 2166-2176.
88. Shimizu M, Fuse K, Okudaira K, et al,. Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos 2005; 33: 1477-1481.
89. Shitara Y, Itoh T, Sato H, Li AP, Sugiyama Y,. Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. J Pharmacol Exp Ther 2003; 304: 610-616.
90. Shitara Y,. Clinical importance of OATP1B1 and OATP1B3 in drug-drug interactions. Drug Metab Pharmacokinet 2011; 26: 220-227.
91. Lau YY, Huang Y, Frassetto L, Benet LZ,. Effect of OATP1B transporter inhibition on the pharmacokinetics of atorvastatin in healthy volunteers. Clin Pharmacol Ther 2007; 81: 194-204.
92. Hirano M, Maeda K, Shitara Y, Sugiyama Y,. Drug-drug interaction between pitavastatin and various drugs via OATP1B1. Drug Metab Dispos 2006; 34: 1229-1236.
93. Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, Sugiyama Y,. Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver. Pharmacol Rev 1998; 50: 387-412.
94. Ueda K, Kato Y, Komatsu K, Sugiyama Y,. Inhibition of biliary excretion of methotrexate by probenecid in rats: quantitative prediction of interaction from in vitro data. J Pharmacol Exp Ther 2001; 297: 1036-1043.
95. Yoshida K, Maeda K, Sugiyama Y,. Prediction of the degree of transporter-mediated drug-drug interactions involving OATP substrates based on in vitro studies. Clin Pharmacol Ther 2012; 91: 1053-1064.
96. Tachibana T, Kato M, Watanabe T, Mitsui T, Sugiyama Y,. Method for predicting the risk of drug-drug interactions involving inhibition of intestinal CYP3A4 and P-glycoprotein. Xenobiotica 2009; 39: 430-443.
97. Gertz M, Cartwright CM, Hobbs MJ, Kenworthy KE, Rowland M, Houston JB, Galetin A,. Cyclosporine inhibition of hepatic and intestinal CYP3A4, uptake and efflux transporters: Application of PBPK modeling in the assessment of drug-drug interaction potential. Pharm Res; in press.
98. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A,. Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res 2001; 18: 1262-1269.
99. Noe J, Portmann R, Brun ME, Funk C,. Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3. Drug Metab Dispos 2007; 35: 1308-1314.
100. Roth M, Timmermann BN, Hagenbuch B,. Interactions of green tea catechins with organic anion-transporting polypeptides. Drug Metab Dispos 2011; 39: 920-926.
101. Sugiyama D, Kusuhara H, Shitara Y, Abe T, Sugiyama Y,. Effect of 17 beta-estradiol- d -17 beta-glucuronide on the rat organic anion transporting polypeptide 2-mediated transport differs depending on substrates. Drug Metab Dispos 2002; 30: 220-223.
102. Kindla J, Muller F, Mieth M, Fromm MF, Konig J,. Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos 2011; 39: 1047-1053.
103. Shitara Y, Nagamatsu Y, Wada S, Sugiyama Y, Horie T,. Long-lasting inhibition of the transporter-mediated hepatic uptake of sulfobromophthalein by cyclosporin a in rats. Drug Metab Dispos 2009; 37: 1172-1178.
104. Shitara Y, Takeuchi K, Nagamatsu Y, Wada S, Sugiyama Y, Horie T,. Long-lasting inhibitory effects of cyclosporin A, but not tacrolimus, on OATP1B1- and OATP1B3-mediated uptake. Drug Metab Pharmacokinet 2012; 27: 368-378.
105. Amundsen R, Christensen H, Zabihyan B, Asberg A,. Cyclosporine A, but not tacrolimus, shows relevant inhibition of organic anion-transporting protein 1B1-mediated transport of atorvastatin. Drug Metab Dispos 2010; 38: 1499-1504.
106. Cui Y, Konig J, Leier I, Buchholz U, Keppler D,. Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem 2001; 276: 9626-9630.
107. Glaeser H, Bailey DG, Dresser GK, et al,. Intestinal drug transporter expression and the impact of grapefruit juice in humans. Clin Pharmacol Ther 2007; 81: 362-370.
108. Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I,. Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther 2004; 308: 438-445.
109. Satoh H, Yamashita F, Tsujimoto M, et al,. Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. Drug Metab Dispos 2005; 33: 518-523.
110. Dresser GK, Bailey DG, Leake BF, et al,. Fruit juices inhibit organic anion transporting polypeptide-mediated drug uptake to decrease the oral availability of fexofenadine. Clin Pharmacol Ther 2002; 71: 11-20.
111. Lilja JJ, Backman JT, Laitila J, Luurila H, Neuvonen PJ,. Itraconazole increases but grapefruit juice greatly decreases plasma concentrations of celiprolol. Clin Pharmacol Ther 2003; 73: 192-198.
112. Lilja JJ, Raaska K, Neuvonen PJ,. Effects of grapefruit juice on the pharmacokinetics of acebutolol. Br J Clin Pharmacol 2005; 60: 659-663.
113. Schwarz UI, Seemann D, Oertel R, et al,. Grapefruit juice ingestion significantly reduces talinolol bioavailability. Clin Pharmacol Ther 2005; 77: 291-301.
114. Tapaninen T, Neuvonen PJ, Niemi M,. Grapefruit juice greatly reduces the plasma concentrations of the OATP2B1 and CYP3A4 substrate aliskiren. Clin Pharmacol Ther 2010; 88: 339-342.
115. Spahn-Langguth H, Langguth P,. Grapefruit juice enhances intestinal absorption of the P-glycoprotein substrate talinolol. Eur J Pharm Sci 2001; 12: 361-367.
116. Shirasaka Y, Kuraoka E, Spahn-Langguth H, Nakanishi T, Langguth P, Tamai I,. Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther 2010; 332: 181-189.
117. Shirasaka Y, Mori T, Shichiri M, Nakanishi T, Tamai I,. Functional pleiotropy of organic anion transporting polypeptide OATP2B1 due to multiple binding sites. Drug Metab Pharmacokinet 2012; 27: 360-364.
118. Akamine Y, Miura M, Sunagawa S, Kagaya H, Yasui-Furukori N, Uno T,. Influence of drug-transporter polymorphisms on the pharmacokinetics of fexofenadine enantiomers. Xenobiotica 2010; 40: 782-789.
119. Imanaga J, Kotegawa T, Imai H, et al,. The effects of the SLCO2B1 c.1457C > T polymorphism and apple juice on the pharmacokinetics of fexofenadine and midazolam in humans. Pharmacogenet Genomics 2011; 21: 84-93.
120. Mougey EB, Feng H, Castro M, Irvin CG, Lima JJ,. Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet Genomics 2009; 19: 129-138.
121. Watanabe T, Kusuhara H, Debori Y, et al,. Prediction of the overall renal tubular secretion and hepatic clearance of anionic drugs and a renal drug-drug interaction involving organic anion transporter 3 in humans by in vitro uptake experiments. Drug Metab Dispos 2011; 39: 1031-1038.
122. Watanabe T, Maeda K, Kondo T, et al,. Prediction of the hepatic and renal clearance of transporter substrates in rats using in vitro uptake experiments. Drug Metab Dispos 2009; 37: 1471-1479.
123. Lappin G, Shishikura Y, Jochemsen R, et al,. Pharmacokinetics of fexofenadine: evaluation of a microdose and assessment of absolute oral bioavailability. Eur J Pharm Sci 2010; 40: 125-131.
124. Dingemanse J, van Giersbergen PL,. Clinical pharmacology of bosentan, a dual endothelin receptor antagonist. Clin Pharmacokinet 2004; 43: 1089-1115.
125. Prescribing information of olmesartan.
126. Flesch G, Muller P, Lloyd P,. Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man. Eur J Clin Pharmacol 1997; 52: 115-120.
127. Knauf H, Mutschler E,. Clinical pharmacokinetics and pharmacodynamics of torasemide. Clin Pharmacokinet 1998; 34: 1-24.
128. Shitara Y, Hirano M, Sato H, Sugiyama Y,. Gemfibrozil and its glucuronide inhibit the organic anion transporting polypeptide 2 (OATP2/OATP1B1:SLC21A6)- mediated hepatic uptake and CYP2C8-mediated metabolism of cerivastatin: analysis of the mechanism of the clinically relevant drug-drug interaction between cerivastatin and gemfibrozil. J Pharmacol Exp Ther 2004; 311: 228-236.
129. Appendix II,. Design and optimization of dosage regimens: Pharmacokinetic data. In Goodman & Gilman's the Pharmacological Basis of Therapeutics (12th edn)., Brunton LL, Blumenthal DK, Murri N, Dandan RH, Knollmann BC, (eds). McGraw-Hill Professional: New York, 2010.
130. Interview form of temocapril [Japanese].
131. Urien S, Barre J, Morin C, Paccaly A, Montay G, Tillement JP,. Docetaxel serum protein binding with high affinity to alpha 1-acid glycoprotein. Invest New Drugs 1996; 14: 147-151.
132. Prescribing information of paclitaxel.
133. Kosoglou T, Statkevich P, Johnson-Levonas AO, Paolini JF, Bergman AJ, Alton KB,. Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet 2005; 44: 467-494.
134. Prescribing information of caspofungin.
135. Prescribing information of irbesartan.
136. Prescribing information of telmisartan.
137. Prescribing information of valsartan.
138. Prescribing information of lopinavir.
139. Hsu A, Granneman GR, Bertz RJ,. Ritonavir: Clinical pharmacokinetics and interactions with other anti-HIV agents. Clin Pharmacokinet 1998; 35: 275-291.
140. Vella S, Floridia M,. Saquinavir: Clinical pharmacology and efficacy. Clin Pharmacokinet 1998; 34: 189-201.
141. Iwatsubo T, Hirota N, Ooie T, et al,. Prediction of in vivo drug metabolism in the human liver from in vitro metabolism data. Pharmacol Ther 1997; 73: 147-171.
142. Hallifax D, Foster JA, Houston JB,. Prediction of human metabolic clearance from in vitro systems: retrospective analysis and prospective view. Pharm Res 2010; 27: 2150-2161.
143. Carlile DJ, Hakooz N, Bayliss MK, Houston JB,. Microsomal prediction of in vivo clearance of CYP2C9 substrates in humans. Br J Clin Pharmacol 1999; 47: 625-635.
144. Watanabe T, Kusuhara H, Maeda K, et al,. Investigation of the rate-determining process in the hepatic elimination of HMG-CoA reductase inhibitors in rats and humans. Drug Metab Dispos 2010; 38: 215-222.
145. Rawden HC, Carlile DJ, Tindall A, et al,. Microsomal prediction of in vivo clearance and associated interindividual variability of six benzodiazepines in humans. Xenobiotica 2005; 35: 603-625.
146. i determination. Drug Metab Dispos 2007; 35: 2119-2126.
147. Stringer R, Nicklin PL, Houston JB,. Reliability of human cryopreserved hepatocytes and liver microsomes as in vitro systems to predict metabolic clearance. Xenobiotica 2008; 38: 1313-1329.
148. Nakai D, Nakagomi R, Furuta Y, et al,. Human liver-specific organic anion transporter, LST-1, mediates uptake of pravastatin by human hepatocytes. J Pharmacol Exp Ther 2001; 297: 861-867.
149. Nakagomi-Hagihara R, Nakai D, Kawai K, et al,. OATP1B1, OATP1B3, and mrp2 are involved in hepatobiliary transport of olmesartan, a novel angiotensin II blocker. Drug Metab Dispos 2006; 34: 862-869.
150. Poirier A, Cascais AC, Funk C, Lave T,. Prediction of pharmacokinetic profile of valsartan in human based on in vitro uptake transport data. J Pharmacokinet Pharmacodyn 2009; 36: 585-611.
151. Shitara Y, Hirano M, Adachi Y, Itoh T, Sato H, Sugiyama Y,. 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 2004; 32: 1468-1475.
152. Sun H, Huang Y, Frassetto L, Benet LZ,. Effects of uremic toxins on hepatic uptake and metabolism of erythromycin. Drug Metab Dispos 2004; 32: 1239-1246.
153. Ohtawa M, Masuda N, Akasaka I, Nakashima A, Ochiai K, Moriyasu M,. Cellular uptake of fluvastatin, an inhibitor of HMG-CoA reductase, by rat cultured hepatocytes and human aortic endothelial cells. Br J Clin Pharmacol 1999; 47: 383-389.
154. Shimada S, Fujino H, Morikawa T, Moriyasu M, Kojima J,. Uptake mechanism of pitavastatin, a new inhibitor of HMG-CoA reductase, in rat hepatocytes. Drug Metab Pharmacokinet 2003; 18: 245-251.
155. Yamazaki M, Suzuki H, Hanano M, Sugiyama Y,. Different relationships between cellular ATP and hepatic uptake among taurocholate, cholate, and organic anions. Am J Physiol 1993; 264: G693-G701.
156. Nezasa K, Higaki K, Takeuchi M, Nakano M, Koike M,. Uptake of rosuvastatin by isolated rat hepatocytes: comparison with pravastatin. Xenobiotica 2003; 33: 379-388.
157. Smith G, Davidson R, Bloor S, et al,. Pharmacological properties of ZD4522 a new HMG-CoA reductase inhibitor (Abstr.). Atherosclerosis 2000; 151: 39.
158. McTaggart F, Buckett L, Davidson R, et al,. Preclinical and clinical pharmacology of rosuvastatin, a new 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor. Am J Cardiol 2001; 87: 28B-32B.
159. Pasanen MK, Fredrikson H, Neuvonen PJ, Niemi M,. Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin. Clin Pharmacol Ther 2007; 82: 726-733.
160. Kalliokoski A, Backman JT, Kurkinen KJ, Neuvonen PJ, Niemi M,. Effects of gemfibrozil and atorvastatin on the pharmacokinetics of repaglinide in relation to SLCO1B1 polymorphism. Clin Pharmacol Ther 2008; 84: 488-496.
161. He YJ, Zhang W, Chen Y, et al,. Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T > C polymorphism. Clin Chim Acta 2009; 405: 49-52.
162. Niemi M, Pasanen MK, Neuvonen PJ,. SLCO1B1 polymorphism and sex affect the pharmacokinetics of pravastatin but not fluvastatin. Clin Pharmacol Ther 2006; 80: 356-366.
163. Ieiri I, Suwannakul S, Maeda K, et al,. SLCO1B1 (OATP1B1, an uptake transporter) and ABCG2 (BCRP, an efflux transporter) variant alleles and pharmacokinetics of pitavastatin in healthy volunteers. Clin Pharmacol Ther 2007; 82: 541-547.
164. Chung JY, Cho JY, Yu KS, et al,. Effect of OATP1B1 (SLCO1B1) variant alleles on the pharmacokinetics of pitavastatin in healthy volunteers. Clin Pharmacol Ther 2005; 78: 342-350.
165. Nishizato Y, Ieiri I, Suzuki H, et al,. Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: consequences for pravastatin pharmacokinetics. Clin Pharmacol Ther 2003; 73: 554-565.
166. Suwannakul S, Ieiri I, Kimura M, et al,. Pharmacokinetic interaction between pravastatin and olmesartan in relation to SLCO1B1 polymorphism. J Hum Genet 2008; 53: 899-904.
167. Maeda K, Ieiri I, Yasuda K, et al,. Effects of organic anion transporting polypeptide 1B1 haplotype on pharmacokinetics of pravastatin, valsartan, and temocapril. Clin Pharmacol Ther 2006; 79: 427-439.
168. Niemi M, Schaeffeler E, Lang T, et al,. High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1). Pharmacogenetics 2004; 14: 429-440.
169. Igel M, Arnold KA, Niemi M, et al,. Impact of the SLCO1B1 polymorphism on the pharmacokinetics and lipid-lowering efficacy of multiple-dose pravastatin. Clin Pharmacol Ther 2006; 79: 419-426.
170. Mwinyi J, Johne A, Bauer S, Roots I, Gerloff T,. Evidence for inverse effects of OATP-C (SLC21A6) 5 and 1b haplotypes on pravastatin kinetics. Clin Pharmacol Ther 2004; 75: 415-421.
171. Choi JH, Lee MG, Cho JY, Lee JE, Kim KH, Park K,. Influence of OATP1B1 genotype on the pharmacokinetics of rosuvastatin in Koreans. Clin Pharmacol Ther 2008; 83: 251-257.
172. Lee E, Ryan S, Birmingham B, et al,. Rosuvastatin pharmacokinetics and pharmacogenetics in white and Asian subjects residing in the same environment. Clin Pharmacol Ther 2005; 78: 330-341.
173. Niemi M, Kivisto KT, Hofmann U, Schwab M, Eichelbaum M, Fromm MF,. Fexofenadine pharmacokinetics are associated with a polymorphism of the SLCO1B1 gene (encoding OATP1B1). Br J Clin Pharmacol 2005; 59: 602-604.
174. Vormfelde SV, Toliat MR, Schirmer M, Meineke I, Nurnberg P, Brockmoller J,. The polymorphisms Asn130Asp and Val174Ala in OATP1B1 and the CYP2C9 allele *3 independently affect torsemide pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther 2008; 83: 815-817.
175. Werner D, Werner U, Meybaum A, et al,. Determinants of steady-state torasemide pharmacokinetics: impact of pharmacogenetic factors, gender and angiotensin II receptor blockers. Clin Pharmacokinet 2008; 47: 323-332.