Substrate-dependent inhibition of organic anion transporting polypeptide 1B1: Comparative analysis with prototypical probe substrates estradiol-17β-glucuronide, estrone-3-sulfate, and sulfobromophthalein

Drug Metabolism and Disposition

Volumn 41, Issue 10, 2013, Pages 1859-1866

  Izumi, Saki ^a   Nozaki, Yoshitane ^a   Komori, Takafumi ^a   Maeda, Kazuya ^b   Takenaka, Osamu ^a   Kusano, Kazutomi ^a   Yoshimura, Tsutomu ^a   Kusuhara, Hiroyuki ^b   Sugiyama, Yuichi ^c  

^a EISAI CO LTD   (Japan)

^b UNIVERSITY OF TOKYO   (Japan)

^c RIKEN   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

BROMSULFOPHTHALEIN; CIMETIDINE; CYCLOSPORIN A; ERYTHROMYCIN; ESTRADIOL 17 GLUCURONIDE; ESTRONE SULFATE; GEMFIBROZIL; KETOCONAZOLE; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTING POLYPEPTIDE 1B1; PROBENECID; RIFAMPICIN; RITONAVIR; TACROLIMUS; TAUROCHOLIC ACID; UNCLASSIFIED DRUG; VERAPAMIL;

ARTICLE; CELL LEVEL; COMPARATIVE STUDY; CONTROLLED STUDY; DRUG METABOLISM; DRUG POTENCY; DRUG PURIFICATION; DRUG STRUCTURE; DRUG UPTAKE; ENZYME INHIBITION; ENZYME KINETICS; HUMAN; HUMAN CELL; IC 50; OPEN READING FRAME; PRIORITY JOURNAL;

BIOLOGICAL TRANSPORT; CELL LINE; ESTRADIOL; ESTRONE; HEK293 CELLS; HUMANS; HYDROXYMETHYLGLUTARYL-COA REDUCTASE INHIBITORS; KINETICS; ORGANIC ANION TRANSPORTERS; SULFOBROMOPHTHALEIN;

EID: 84884676629     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.113.052290     Document Type: Article

References (40)

1. Abe T, Kakyo M, Tokui T, Nakagomi R, Nishio T, Nakai D, Nomura H, Unno M, Suzuki M, and Naitoh T, et al. (1999) Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1. J Biol Chem 274:17159-17163.
2. Center for Drug Evaluation and Research (2012) Drug interaction studies - study design, data analysis, implications for dosing, and labeling recommendations: Draft guidance. Food and Drug Administration, Silver Spring, MD.
3. Committee for Human Medicinal Products (2012) Guideline on the Investigation of Drug Interactions. European Medicines Agency, London.
4. Cui Y, König J, Leier I, Buchholz U, and Keppler D (2001) Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem 276:9626-9630.
5. International Transporter ConsortiumGiacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, and Hillgren KM, et al. (2010) Membrane transporters in drug development. Nat Rev Drug Discov 9:215-236.
6. 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. (Pubitemid 39287793)
7. 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.
8. Hsiang B, Zhu Y, Wang Z, Wu Y, Sasseville V, Yang WP, and Kirchgessner TG (1999) 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 274:37161-37168.
9. Imamura Y, Murayama N, Okudaira N, Kurihara A, Okazaki O, Izumi T, Inoue K, Yuasa H, Kusuhara H, and Sugiyama Y (2011) Prediction of fluoroquinolone- induced elevation in serum creatinine levels: a case of drug-endogenous substance interaction involving the inhibition of renal secretion. Clin Pharmacol Ther 89:81-88.
10. Ito K, Iwatsubo T, Kanamitsu S, Ueda K, Suzuki H, and Sugiyama Y (1998) Prediction of pharmacokinetic alterations caused by drug-drug interactions: metabolic interaction in the liver. Pharmacol Rev 50:387-412.
11. Katz DA, Carr R, Grimm DR, Xiong H, Holley-Shanks R, Mueller T, Leake B, Wang Q, Han L, and Wang PG, et al. (2006) Organic anion transporting polypeptide 1B1 activity classified by SLCO1B1 genotype influences atrasentan pharmacokinetics. Clin Pharmacol Ther 79:186-196.
12. Kenworthy KE, Bloomer JC, Clarke SE, and Houston JB (1999) CYP3A4 drug interactions: correlation of 10 in vitro probe substrates. Br J Clin Pharmacol 48:716-727. (Pubitemid 29520596)
13. Kindla J, Müller F, Mieth M, Fromm MF, and König J (2011) Influence of non-steroidal anti-inflammatory drugs on organic anion transporting polypeptide (OATP) 1B1- and OATP1B3-mediated drug transport. Drug Metab Dispos 39:1047-1053.
14. Kudo T, Hisaka A, Sugiyama Y, and Ito K (2013) Analysis of the repaglinide concentration increase produced by gemfibrozil and itraconazole based on the inhibition of the hepatic uptake transporter and metabolic enzymes. Drug Metab Dispos 41:362-371.
15. Link E, Parish S, Armitage J, Bowman L, Heath S, Matsuda F, Gut I, Lathrop M, and Collins R; SEARCH Collaborative Group (2008) SLCO1B1 variants and statin-induced myopathy - a genomewide study. N Engl J Med 359:789-799.
16. Maeda K, Ikeda Y, Fujita T, Yoshida K, Azuma Y, Haruyama Y, Yamane N, Kumagai Y, and Sugiyama Y (2011) Identification of the rate-determining process in the hepatic clearance of atorvastatin in a clinical cassette microdosing study. Clin Pharmacol Ther 90:575-581.
17. Miyagawa M, Maeda K, Aoyama A, and Sugiyama Y (2009) The eighth and ninth transmembrane domains in organic anion transporting polypeptide 1B1 affect the transport kinetics of estrone-3-sulfate and estradiol-17beta-D-glucuronide. J Pharmacol Exp Ther 329:551-557.
18. Mizuno N, Niwa T, Yotsumoto Y, and Sugiyama Y (2003) Impact of drug transporter studies on drug discovery and development. Pharmacol Rev 55:425-461. (Pubitemid 37013212)
19. Niemi M, Backman JT, Kajosaari LI, Leathart JB, Neuvonen M, Daly AK, Eichelbaum M, Kivistö KT, and Neuvonen PJ (2005) Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics. Clin Pharmacol Ther 77:468-478. (Pubitemid 40824960)
20. Niemi M, Pasanen MK, and Neuvonen PJ (2011) Organic anion transporting polypeptide 1B1: a genetically polymorphic transporter of major importance for hepatic drug uptake. Pharmacol Rev 63:157-181.
21. Noé 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)
22. Obach RS, Walsky RL, Venkatakrishnan K, Gaman EA, Houston JB, and Tremaine LM (2006) The utility of in vitro cytochrome P450 inhibition data in the prediction of drug-drug interactions. J Pharmacol Exp Ther 316:336-348. (Pubitemid 41832613)
23. Sharma P, Butters CJ, Smith V, Elsby R, and Surry D (2012) Prediction of the in vivo OATP1B1-mediated drug-drug interaction potential of an investigational drug against a range of statins. Eur J Pharm Sci 47:244-255.
24. Sharma P, Holmes VE, Elsby R, Lambert C, and Surry D (2010) 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.
25. Shirasaka Y, Mori T, Shichiri M, Nakanishi T, and Tamai I (2012) Functional pleiotropy of organic anion transporting polypeptide OATP2B1 due to multiple binding sites. Drug Metab Pharmacokinet 27:360-364.
26. Shitara Y, Itoh T, Sato H, Li AP, and Sugiyama Y (2003) Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A. J Pharmacol Exp Ther 304:610-616. (Pubitemid 36152336)
27. Shitara Y, Maeda K, Ikejiri K, Yoshida K, Horie T, and Sugiyama Y (2013) Clinical significance of organic anion transporting polypeptides (OATPs) in drug disposition: their roles in hepatic clearance and intestinal absorption. Biopharm Drug Dispos 34:45-78.
28. Shitara Y, Sato H, and Sugiyama Y (2005) Evaluation of drug-drug interaction in the hepatobiliary and renal transport of drugs. Annu Rev Pharmacol Toxicol 45:689-723. (Pubitemid 40261822)
29. 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)
30. Soars MG, Barton P, Ismair M, Jupp R, and Riley RJ (2012) The development, characterization, and application of an OATP1B1 inhibition assay in drug discovery. Drug Metab Dispos 40:1641-1648.
31. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, and Tsuji A (2001) Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res 18:1262-1269. (Pubitemid 32846318)
32. van Giersbergen PL, Treiber A, Schneiter R, Dietrich H, and Dingemanse J (2007) Inhibitory and inductive effects of rifampin on the pharmacokinetics of bosentan in healthy subjects. Clin Pharmacol Ther 81:414-419. (Pubitemid 46364484)
33. Vormfelde SV, Toliat MR, Schirmer M, Meineke I, Nürnberg P, and Brockmöller J (2008) The polymorphisms Asn130Asp and Val174Ala in OATP1B1 and the CYP2C9 allele*3 independently affect torsemide pharmacokinetics and pharmacodynamics. Clin Pharmacol Ther 83:815-817. (Pubitemid 351704920)
34. Yamada A, Maeda K, Kamiyama E, Sugiyama D, Kondo T, Shiroyanagi Y, Nakazawa H, Okano T, Adachi M, and Schuetz JD, et al. (2007) 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 35:2166-2176. (Pubitemid 350146202)
35. Yamaoka K, Tanigawara Y, Nakagawa T, and Uno T (1981) A pharmacokinetic analysis program (multi) for microcomputer. J Pharmacobiodyn 4:879-885. (Pubitemid 12174128)
36. 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.
37. Yoshida K, Maeda K, and Sugiyama Y (2012) Transporter-mediated drug-drug interactions involving OATP substrates: predictions based on in vitro inhibition studies. Clin Pharmacol Ther 91:1053-1064.
38. Yoshida K, Maeda K, and Sugiyama Y (2013) Hepatic and intestinal drug transporters: prediction of pharmacokinetic effects caused by drug-drug interactions and genetic polymorphisms. Annu Rev Pharmacol Toxicol 53:581-612.
39. Zhang W, He YJ, Han CT, Liu ZQ, Li Q, Fan L, Tan ZR, Zhang WX, Yu BN, and Wang D, et al. (2006) Effect of SLCO1B1 genetic polymorphism on the pharmacokinetics of nateglinide. Br J Clin Pharmacol 62:567-572. (Pubitemid 44571578)
40. Zolk O, Solbach TF, König J, and Fromm MF (2009) Structural determinants of inhibitor interaction with the human organic cation transporter OCT2 (SLC22A2). Naunyn Schmiedebergs Arch Pharmacol 379:337-348.