YM-60828, a novel factor Xa inhibitor: Separation of its antithrombotic effects from its prolongation of bleeding time

European Journal of Pharmacology

Volumn 339, Issue 2-3, 1997, Pages 141-146

  Sato, Kazuo ^a   Kawasaki, Tomihisa ^a   Taniuchi, Yuta ^a   Hirayama, Fukushi ^a   Koshio, Hiroyuki ^a   Matsumoto, Yuzo ^a  

^a ASTELLAS PHARMA INC   (Japan)

Author keywords

Argatroban; Arterio venous shunt; Bleeding time; Dalteparin; Heparin; YM 60828

Indexed keywords

[N [4 [(1 ACETIMIDOYL 4 PIPERIDYL)OXY]PHENYL] N [(7 AMIDINO 2 NAPHTHYL)METHYL]SULFAMOYL]ACETIC ACID; ARGATROBAN; DALTEPARIN; HEPARIN; SHIMIZU; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTERIOVENOUS SHUNT; ARTICLE; BLEEDING TIME; BLOOD CLOTTING; BLOOD CLOTTING TIME; CONTROLLED STUDY; DOSE RESPONSE; INTRAVENOUS DRUG ADMINISTRATION; MALE; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PRIORITY JOURNAL; PROTHROMBIN TIME; RAT;

ANIMALS; ANTICOAGULANTS; ANTITHROMBINS; BLEEDING TIME; DALTEPARIN; FACTOR XA; FIBRINOLYTIC AGENTS; HEPARIN; MALE; NAPHTHALENES; PIPECOLIC ACIDS; PIPERIDINES; RATS; RATS, SPRAGUE-DAWLEY;

EID: 0031588348     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(97)01389-7     Document Type: Article

References (27)

1. Andersson L.O., Barrowcliffe T.W., Holmer E., Johnson E.A., Soderstrom G. Molecular weight dependency of the heparin potentiated inhibition of thrombin and activated factor X. Effect of heparin neutralization in plasma. Thromb. Res. 15:1979;531.
2. Berndt M.C., Gregory C., Dowden G., Castaldi P.A. Thrombin interaction with platelet membrane proteins. Ann. NY Acad. Sci. 485:1986;374.
3. Berry C.N., Girard D., Lochot S., Lecoffre C. Antithrombotic actions of argatroban in rat models of venous, mixed, and arterial thrombosis, and its effects on the tail transection bleeding time. Br. J. Pharmacol. 113:1994;1209.
4. Berry C.N., Girardot C., Lecoffre C., Lunven C. Effects of the synthetic thrombin inhibitor argatroban on fibrin- or clot-incorporated thrombin: Comparison with heparin and recombinant hirudin. Thromb. Haemost. 72:1994;381.
5. Carter C.J., Kelton J.G., Hirsh J., Cerskus A., Santos A.V., Gent M. The relationship between the hemorrhagic and antithrombotic properties of low molecular weight heparin in rabbits. Blood. 59:1982;1239.
6. Damus P.S., Hicks M., Rosenberg R.D. Anticoagulant action of heparin. Nature (London). 246:1973;355.
7. Hamano S., Nishiyama M., Komatsu H., Miyata H., Ikeda S., Sakuragawa N. Study of anticoagulant mechanism of low molecular weight heparin. Thromb. Res. 65:1992;801.
8. Hara H., Tamao Y., Kikumoto R. Effect of argatroban (MD-805) on platelet function. Jpn. Pharmacol. Ther. 14 (Suppl. 5):1986;13.
9. Hara T., Yokoyama A., Tanabe K., Ishihara H., Iwamoto M. DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thromb. Haemost. 74:1995;635.
10. Herbert J.M., Bernat A., Dol F., Herault J.P., Crepon B., Lormeau J.C. DX 9065a, a novel, synthetic, selective and orally active inhibitor of factor Xa: In vitro and in vivo studies. J. Pharmacol. Exp. Ther. 276:1996;1030.
11. Higgins D.L., Lewis S.D., Shafer J.A. Steady state kinetic parameters for the thrombin catalyzed conversion of human fibrinogen to fibrin. J. Biol. Chem. 258:1983;9276.
12. Hirsh J. Oral anticoagulant drugs. New Engl. J. Med. 324:1991;1865.
13. Holmer E., Mattson C., Nilsson S. Anticoagulant and antithrombotic effects of heparin and low molecular weight heparin fragments in rabbits. Thromb. Res. 25:1982;475.
14. Imura Y., Stassen J.M., Collen D. Comparative antithrombotic effects of heparin, recombinant hirudin and argatroban in a hamster femoral vein platelet-rich mural thrombosis model. J. Pharmacol. Exp. Ther. 261:1992;895.
15. Lefkovits J., Topol E.J. Direct thrombin inhibitors in cardiovascular medicine. Circulation. 90:1994;1522.
16. Maffrand J.P. Direct thrombin inhibitors. Nouv. Rev. Fr. Hematol. 34:1992;405.
17. Mirshahi M., Soria J., Soria C., Faivre R., Lu H., Courtney M., Roitsch C., Tripier D., Caen J.P. Evaluation of the inhibition by heparin and hirudin of coagulation activation during r-t-PA-induced thrombolysis. Blood. 74:1989;1025.
18. Neeper M.P., Waxman L., Smith D.E., Schulman C.A., Sardana M., Ellis R.W., Schaffer L.W., Siegl P.K., Vlasuk G.P. Characterization of recombinant tick anticoagulant peptide. A highly selective inhibitor of blood coagulation factor Xa. J. Biol. Chem. 265:1990;17746.
19. Okamoto S., Hijikata A., Kikumoto R., Tonomura S., Hara H., Ninomiya K., Maruyama A., Sugano M., Tamao Y. Potent inhibition of thrombin by the newly synthesized arginine derivative No. 805. The importance of stereo-structure of its hydrophobic carboxamide portion. Biochem. Biophys. Res. Commun. 101:1981;440.
20. Peters R.F., Lees C.M., Mitchell K.A., Tweed M.F., Talbot M.D., Wallis R.B. The characterization of thrombus development in an improved model of arterio-venous shunt thrombosis in the rat and the effects of recombinant desulphatohirudin (CGP 39393), heparin, and iloprost. Thromb. Haemost. 65:1991;268.
21. Rosenberg R.D., Damus P.S. Purification and mechanism of action of human antithrombin-heparin cofactor. J. Biol. Chem. 248:1973;6498.
22. Rosenberg J.S., Beeler D.L., Rosenberg R.D. Activation of human prothrombin by highly purified human factors V and X-a in presence of human antithrombin. J. Biol. Chem. 250:1975;1607.
23. Schaffer L.W., Davidson J.T., Siegl P.K., Gould R.J., Nutt R.F., Brady S.F., Connolly T.M. Selective factor Xa inhibition by recombinant antistasin prevents vascular graft thrombosis in baboons. Arterioscler. Thromb. 12:1993;879.
24. Verstraete M., Zoldhelyi P. Novel antithrombotic drugs in development. Drugs. 49:1995;856.
25. Vu T.-K.H., Hung D.T., Wheaton V.I., Coughlin S.R. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell. 64:1991;1057.
26. Weitz J.I., Hudoba M., Masel D., Maraganore J., Hirsh J. Clot bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin III independent inhibitors. J. Clin. Invest. 86:1990;385.
27. Yamazaki M., Asakura H., Aoshima K., Saito M., Jokaji H., Uotani C., Kumabashiri I., Morishita E., Ikeda T., Matsuda T. Effects of DX-9065a, an orally active, newly synthesized and specific inhibitor of factor Xa, against experimental disseminated intravascular coagulation in rats. Thromb. Haemost. 72:1994;393.