Involvement of transporters in the hepatic uptake and biliary excretion of valsartan, a selective antagonist of the angiotensin II AT1-receptor, in humans

Drug Metabolism and Disposition

Volumn 34, Issue 7, 2006, Pages 1247-1254

  Yamashiro, Wakaba ^a   Maeda, Kazuya ^a   Hirouchi, Masakazu ^a   Adachi, Yasuhisa ^b   Hu, Zhuohan ^c   Sugiyama, Yuichi ^a  

^a UNIVERSITY OF TOKYO   (Japan)

^b DAIICHI PURE CHEMICALS CO LTD   (Japan)

^c Research Institute for Liver Diseases Shanghai Co Ltd   (China)

Author keywords

[No Author keywords available]

Indexed keywords

CHOLECYSTOKININ OCTAPEPTIDE; ESTRONE SULFATE; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 2; ORGANIC ANION TRANSPORTER 1; ORGANIC ANION TRANSPORTER 1B1; ORGANIC ANION TRANSPORTER 2; UNCLASSIFIED DRUG; VALSARTAN;

ANIMAL CELL; ARTICLE; CELL MEMBRANE; CONTROLLED STUDY; DRUG ELIMINATION; DRUG EXCRETION; DRUG METABOLISM; DRUG UPTAKE; HUMAN; HUMAN CELL; IN VIVO STUDY; LIVER CELL; LIVER METABOLISM; MEMBRANE VESICLE; NONHUMAN; PRIORITY JOURNAL; RAT;

ADENOSINE TRIPHOSPHATE; ANGIOTENSIN II TYPE 1 RECEPTOR BLOCKERS; ANIMALS; BILE; CELL LINE; CELL MEMBRANE; DISEASE MODELS, ANIMAL; ESTRONE; HEPATOCYTES; HUMANS; HYPERBILIRUBINEMIA; MALE; MEMBRANE TRANSPORT PROTEINS; MULTIDRUG RESISTANCE-ASSOCIATED PROTEINS; ORGANIC ANION TRANSPORTERS; ORGANIC ANION TRANSPORTERS, SODIUM-INDEPENDENT; RATS; RATS, SPRAGUE-DAWLEY; SINCALIDE; TETRAZOLES; TRANSFECTION; VALINE;

EID: 33745231761     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.105.008938     Document Type: Article

References (25)

1. Abe T, Unno M, Onogawa T, Tokui T, Kondo TN, Nakagomi R, Adachi H, Fujiwara K, Okabe M, Suzuki T, et al. (2001) LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology 120:1689-1699.
2. Chandra P and Brouwer KL (2004) The complexities of hepatic drug transport: current knowledge and emerging concepts. Pharm Res (NY) 21:719-735.
3. Colussi DM, Parisot C, Rossolino ML, Brunner LA, and Lefevre GY (1997) Protein binding in plasma of valsartan, a new angiotensin II receptor antagonist. J Clin Pharmacol 37:214-221.
4. Evers R, Kool M, van Deemter L, Janssen H, Calafat J, Oomen LC, Paulusma CC, Oude Elferink RP, Baas F, Schinkel AH, et al. (1998) Drug export activity of the human canalicular multispecific organic anion transporter in polarized kidney MDCK cells expressing cMOAT (MRP2) cDNA. J Clin Investig 101:1310-1319.
5. Flesch G, Muller P, and Lloyd P (1997) Absolute bioavailability and pharmacokinetics of valsartan, an angiotensin II receptor antagonist, in man. Eur J Clin Pharmacol 52:115-120.
6. Hagenbuch B and Meier PJ (2004) Organic anion transporting polypeptides of the OATP/SLC21 family: phylogenetic classification as OATP/SLCO superfamily, new nomenclature and molecular/functional properties. Pflueg Arch Eur J Physiol 447:653-665.
7. 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.
8. 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.
9. Hirouchi M, Suzuki H, Itoda M, Ozawa S, Sawada J, Ieiri I, Ohtsubo K, and Sugiyama Y (2004) Characterization of the cellular localization, expression level and function of SNP variants of MRP2/ABCC2. Pharm Res (NY) 21:742-748.
10. 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.
11. 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.
12. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, and Hagenbuch B (2001) Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gasteroenterology 120:525-533.
13. Lowry OH, Rosebrough NJ, Farr AL, and Randall RJ (1951) Protein measurement with the Folin phenol reagent. J Biol Chem 193:265-267
14. Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, and Sugiyama Y (2005) Identification of the hepatic efflux transporters of organic anions using double transfected MDCKII cells expressing human OATP1B1/MRP2, OATP1B1/MDR1 and OATP1B1/BCRP. J Pharmacol Exp Ther 314:1059-1067.
15. Morikawa A, Goto Y, Suzuki H, Hirohashi T, and Sugiyama Y (2000) Biliary excretion of 17beta-estradiol 17beta-D-glucuronide is predominantly mediated by cMOAT/MRP2. Pharm Res (NY) 17:546-552.
16. Nakai D, Nakagomi R, Furuta Y, Tokui T, Abe T, Ikeda T, and Nishimura K (2001) Human liver-specific organic anion transporter, LST-1, mediates uptake of pravastatin by human hepatocytes. J Pharmacol Exp Ther 297:861-867.
17. Nishizato Y, Ieiri I, Suzuki H, Kimura M, Kawabata K, Hirota T, Takane H, Irie S, Kusuhara H, Urasaki Y, et al. (2003) Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: consequences for pravastatin pharmacokinetics. Clin Pharmacol Ther 73:554-565.
18. Shimizu M, Fuse K, Okudaira K, Nishigaki R, Maeda K, Kusuhara H, and Sugiyama Y (2005) Contribution of OATP (organic anion-transporting polypeptide) family transporters to the hepatic uptake of fexofenadine in humans. Drug Metab Dispos 33:1477-1481.
19. Shitara Y, Itoh T, Sato H, Li AP, and Sugiyama Y (2003a) 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.
20. Shitara Y, Li AP, Kato Y, Lu C, Ito K, Itoh T, and Sugiyama Y (2003b) Function of uptake transporters for taurocholate and estradiol 17beta-D-glucuronide in cryopreserved human hepatocytes. Drug Metab Pharmacokinet 18:33-41.
21. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, and Tsuji A (2000) Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun 273:251-260.
22. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, and Fattinger K (2002) Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology 36:164-172.
23. Waldmeier F, Flesch G, Muller P, Winkler T, Kriemler HP, Buhlmayer P, and De Gasparo M (1997) Pharmacokinetics, disposition and biotransformation of [14C]-radiolabelled valsartan in healthy male volunteers after a single oral dose. Xenobiotica 27:59-71.
24. Yamaoka K, Tanigawara Y, Nakagawa T, and Uno T (1981) A pharmacokinetic analysis program (MULTI) for microcomputer. J Pharmacobio-Dyn 4:879-885.
25. Yamazaki M, Akiyama S, Ni'inuma K, Nishigaki R, and Sugiyama Y (1997) Biliary excretion of pravastatin in rats: contribution of the excretion pathway mediated by canalicular multi-specific organic anion transporter. Drug Metab Dispos 25:1123-1129.