Hepatobiliary transport of YM466, a novel factor Xa inhibitor, in rats

European Journal of Drug Metabolism and Pharmacokinetics

Volumn 31, Issue 2, 2006, Pages 117-121

  Mano, Yuji ^a   Usui, Takashi ^a   Kamimura, Hidetaka ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

EHBR; Hepatobiliary transport; Mrp2; YM466

Indexed keywords

BLOOD CLOTTING FACTOR 10A INHIBITOR; MULTIDRUG RESISTANCE PROTEIN 2; UNCLASSIFIED DRUG; YM 466;

ANIMAL EXPERIMENT; ARTICLE; BILIARY EXCRETION; CONTROLLED STUDY; DRUG BILE LEVEL; DRUG BINDING; DRUG BLOOD LEVEL; DRUG EXCRETION; DRUG LIVER LEVEL; DRUG METABOLISM; DRUG STRUCTURE; DRUG TRANSPORT; HEPATOBILIARY SYSTEM; IN VIVO STUDY; MALE; NONHUMAN; PROTEIN TRANSPORT; RAT;

EID: 33746711039     PISSN: 03787966     EISSN: None     Source Type: Journal    
DOI: 10.1007/bf03191128     Document Type: Article

References (24)

1. Kawasaki T., Sato K., Sakai Y., Hirayama F., Koshio H., Taniuchi Y., Matsumoto Y. (1998): Comparative studies of an orally-active factor Xa inhibitor, YM-60828, with other antithrombotic agents in a rat model of arterial thrombosis. Thromb. Haemost., 79, 410-416.
2. Sato K., Kawasaki T., Hisamichi N., Taniuchi Y., Hirayama F., Koshio H., Matsumoto Y. (1998): Antithrombotic effects of YM-60828, a newly synthesized factor Xa inhibitor, in rat thrombosis models and its effects on bleeding time. Br. J. Pharmacol., 123, 92-96.
3. Sato K., Kawasaki T., Taniuchi Y., Hirayama F., Koshio H., Ichihara M., Matsumoto Y. (1998): Antithrombotic effects of YM-60828 in three thrombosis models in guinea pigs. Eur. J. Pharmcol., 350, 87-91.
4. Taniuchi Y., Sakai Y., Hisamichi N., Kayama M., Mano Y., Sato K., Hirayama F., Koshio H., Matsumoto Y., Kawasaki T. (1998): Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa. Thromb. Haemost., 79, 543-548.
5. Mano Y., Sonoda T., Nakamura E., Usui T., Kamimura H. (2004): Absorption, distribution, metabolism and excretion of YM466, a novel factor Xa inhibitor, in rats. Biopharm. Drug Dispos., 25, 253-260.
6. Eckhardt U., Stuber W., Dickneite G., Reers M., Petzinger E. (1996): First-pass elimination of a peptidomimetic thrombin inhibitor is due to carrier-mediated uptake by the liver. Interaction with bile acid transport systems. Biochem. Pharmacol., 52, 85-96.
7. Lave T., Portmann R., Schenker G., Gianni A., Guenzi A., Girometta M. A., Schmitt M. (1999): Interspecies pharmacokinetic comparisons and allometric scaling of napsagatran, a low molecular weight thrombin inhibitor. J. Pharm. Pharmacol., 51, 85-91.
8. Hauptmann J., Sturzebecher J. (1998): Influence of indocyanine green on plasma disappearance and biliary excretion of a synthetic thrombin inhibitor of the 3-amidinophenyl-alanine piperazide-type in rats. Pharm. Res., 15, 751-754.
9. Chandra P. and Brouwer K.L.R. (2004): The complexities of hepatic drug transport: current knowledge and emerging concepts. Pharm. Res., 5, 719-735.
10. Yamazaki M., Akiyama S., Niinuma K., Nishigaki R., Sugiyama Y. (1997): Biliary excretion of pravastatin in rats: Contribution of excretion pathway mediated by canalicular multispecific organic anion transporter. Drug Metab. Dispos., 25, 1123-1129.
11. Ishizuka H., Konno K., Naganuma H., Sasahara K., Kawahara Y., Niinuma K., Suzuki H., Sugiyama Y. (1997): Temocaprilat, a novel angiotensin-converting enzyme inhibitor, is excreted in bile via an ATP-dependent active transporter (cMOAT) that is deficient in Eisai hyperbilirubinemic mutant rats (EHBR). J. Pharmacol. Exp. Ther., 280, 1304-1311.
12. Buchler M., Konig J., Brom M., Kartenbeck J., Spring H., Horie T., Keppler D. (1996): cDNA cloning of the hepatocyte canalicular isoform of the multidrug resistance protein, cMrp, reveals a novel conjugate export pump deficient in hyperbilirubinemic mutant rats. J. Biol. Chem., 271, 15091-15098.
13. Mano Y., Higuchi S., Kamimura H. (2002): Investigation of the high partition of YM992, a novel antidepressant, in rat brain - in vitro and in vivo evidence for the high binding in brain and the high permeability at the BBB. Biopharm. Drug Dispos., 23, 351-360.
14. Mano Y., Usui T., Kamimura H. (2004): A liquid chromatographic-tandem mass spectrometric method for the determination of YM466, a novel Factor Xa inhibitor, in rat plasma. J. Pharm. Biomed. Anal., 36, 883-887.
15. Tsuji A., Yoshikawa T., Nishide K., Minami H., Kimura M., Nakashima E., Terasaki T., Miyamoto E., Nightingale C.H., Yamana T. (1983): Physiologically based pharmacokinetic model for β-lactam antibiotics. I: Tissue distribution and elimination in rats. J. Pharm. Sci., 72, 1239-1252.
16. Mano Y., Usui T., Kamimura H. (2004): Pharmacokinetics of YM466, a new factor Xa inhibitor, in rats and dogs. Eur. J. Drug Metab. Pharmacokinet, 29, 7-13.
17. Akita H., Suzuki H., Sugiyama Y. (2001): Sinusoidal efflux of taurocholate is enhanced in Mrp2-deficient rat liver. Pharm. Res., 18, 1119-1125.
18. Yamada T., Niinuma K., Lemaire M., Terasaki T., Sugiyama Y. (1997): Carrier-mediated hepatic uptake of the cationic cyclopeptide, octreotide, in rats. Comparison between in vivo and in vitro. Drug Metab. Dispos., 25, 536-543.
19. Ito K., Wakabayashi T., Horie T. (2005): Mrp2/Abcc2 transport activity is stimulated by protein kinase Ca in a baculovirus co-expression system. Life Sci., 77, 539-550.
20. Chu X.Y., Huskey S.E., Braun M.P., Sarkadi B., Evans D.C., Evers R. (2004): Transport of ethinylestradiol glucuronide and ethinylestradiol sulfate by the multidrug resistance proteins MRP1, MRP2, and MRP3. J. Pharmacol. Exp. Ther., 309, 156-164.
21. Fickert P., Zollner G., Fuchsbichler A., Stumptner C., Pojer C., Zenz R., Lammert F., Stieger B., Meier P.J., Zatloukal K., Denk H., Trauner M. (2001): Effects of ursodeoxycholic and cholic acid feeding on hepatocellular transporter expression in mouse liver. Gastroenterology, 121, 170-183.
22. 3 antagonists in rat. Xenobiotica, 33, 1125-1137.
23. Kullak-Ublick G.A., Hagenbuch B., Stieger B., Wolkoff A.W., Meier P.J. (1994): Functional characterization of the basolateral rat liver organic anion transporting polypeptide. Hepatology, 20, 411-416.
24. Eckhardt U., Horz J.A., Petzinger E., Stuber W., Reers M., Dickneite G., Daniel H., Wagener M., Hagenbuch B., Stieger B., Meier P.J. (1996): The peptide-based thrombin inhibitor CRC 220 is a new substrate of the basolateral rat liver organic anion-transporting polypeptide. Hepatology, 24, 380-384.