Antithrombotic effects of YM466, a synthesized direct inhibitor of factor Xa, in an arterio-venous shunt thrombosis model in squirrel monkeys

Drug Development Research

Volumn 58, Issue 2, 2003, Pages 190-195

  Iwatsuki, Yoshiyuki ^a   Kaku, Seiji ^a   Moritani, Yumiko ^a   Taniuchi, Yuta ^a   Hirayama, Fukushi ^a   Koshio, Hiroyuki ^a   Matsumoto, Yuzo ^a   Mano, Yuji ^b   Kawasaki, Tomihisa ^a  

^a ASTELLAS PHARMA INC   (Japan)

^b INSTITUTE FOR DEVELOPMENTAL RESEARCH   (Japan)

Author keywords

Anti FXa activity; Arterio venous shunt thrombosis; Factor Xa inhibitor; Squirrel monkey; YM466

Indexed keywords

ANTICOAGULANT AGENT; BLOOD CLOTTING FACTOR 10A; N [4 [(1 ACETIMIDYL 4 PIPERIDYL)OXY]PHENYL] N [(7 AMIDINO 2 NAPHTHYL)METHYL]SULFAMOYL ACETIC ACID MESYLATE; PROTHROMBIN; THROMBIN ANTITHROMBIN COMPLEX; THROMBOPLASTIN; UNCLASSIFIED DRUG; YM 466;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTERIOVENOUS SHUNT THROMBOSIS; ARTICLE; BLEEDING TIME; CONTROLLED STUDY; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG EFFECT; DRUG INFUSION; DRUG SAFETY; MALE; MASS SPECTROMETRY; NONHUMAN; PARTIAL THROMBOPLASTIN TIME; PROTHROMBIN TIME; SQUIRREL MONKEY; THROMBOGENESIS; THROMBOSIS;

EID: 0037310402     PISSN: 02724391     EISSN: None     Source Type: Journal    
DOI: 10.1002/ddr.10159     Document Type: Article

References (23)

1. Bauer KA, Eriksson BI, Lassen MR, Turpie AGG. 2001. Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after elective major knee surgery. New Engl J Med 345:1305-1310.
2. Boneu B, Bes G, Pelzer H, Sie P, Boccalon H. 1991. D-Dimers, thrombin antithrombin III complexes and prothrombin fragments 1+2: diagnostic value in clinically suspected deep vein thrombosis. Thromb Haemost 65:28-31.
3. Bostwick JS, Bentley R, Morgan S, Brown K, Chu V, Ewing WR, Spada AP, Pauls H, Perrone MH, Dunwiddie CT, Leadley RJ. 1999. RPR120844, a novel, specific inhibitor of coagulation factor Xa inhibits venous thrombosis in the rabbit. Thromb Haemost 81:157-160.
4. Chu V, Brown K, Colussi D, Gao J, Bostwick J, Kasiewski C, Bentley R, Susan, Morgan, Guertin K, Pauls HW, Gong Y, Zulli A, Perrone MH, Dunwiddie CT, Leadley aRJ. 2001. Pharmacological characterization of a novel factor Xa inhibitor, FXV673. Thromb Res 103:309-324.
5. Eisenberg PR, Siegel JE, Abendschein DR, Miletich JP. 1993. Importance of factor Xa in determining the procoagulant activity of whole-blood clots. J Clin Invest 91:1877-1883.
6. Eriksson BI, Bauer KA, Lassen MR, Turpie AGG. 2001. Fondaparinux compared with enoxaparin for the prevention of venous thromboembolism after hip-fracture surgery. New Engl J Med 345:1298-1304.
7. Hara T, Yokoyama A, Ishihara H, Yokoyama Y, Nagahara T, Iwamoto M. 1994. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb Haemost 71:314-319.
8. Hara T, Yokoyama A, Tanabe K, Ishihara H, Iwamoto M. 1995. DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thromb Haemost 74:635-639.
9. Hayashi M, Matsuo A, Nakamoto H, Aisaka K. 2001. Antithrombotic effects of a synthetic inhibitor of activated factor X, JTV-803, in animals. Eur J Pharmacol 412:61-66.
10. 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.
11. Lassen MR, Bauer KA, Eriksson BI, Turpie AGG. 2002. Postoperative fondaparinux versus preoperative enoxaparin for prevention of venous thromboembolism in elective hip-replacement surgery: a randomised double-blind comparison. Lancet 359:1715-1720.
12. Pelzer H, Schwarz A, Heimburger N. 1988. Determination of human thrombin-antithrombin III complex in plasma with an enzyme-linked immunosorbent assay. Thromb Haemost 59:101-106.
13. Peters RF, Lees CM, Mitchell KA, Tweed MF, Talbot MD, Wallis RB. 1991. The characterization of thrombus development in an improved model of arterio-venous shunt thrombosis in the rat and the effect of recombinant desulphatohirudin (CGP 39393), heparin, and iloprost. Thromb Haemost 65:268-274.
14. Sato K, Kawasaki T, Hisamichi N, Taniuchi Y, Hirayama F, Koshio H, Ichihara M, Matsumoto Y. 1998a. Antithrombotic effects of YM-60828 in three thrombosis models in guinea pigs. Eur J Pharmacol 350:87-91.
15. Sato K, Kawasaki T, Hisamichi N, Taniuchi Y, Hirayama F, Koshio H, Matsumoto Y. 1998b. 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.
16. Sato K, Taniuchi Y, Kawasaki T, Hirayama F, Koshio H, Matsumoto Y. 1998c. Relationship between the antithrombotic effect of YM-75466, a novel factor Xa inhibitor, and coagulation parameters in rats. Eur J Pharmacol 347:231-236.
17. Sato K, Taniuchi Y, Kawasaki T, Hirayama F, Koshio H, Matsumoto Y, Iizumi Y. 1998d. Comparison of the anticoagulant and antithrombotic effects of YM-75466, a novel orally-active factor Xa inhibitor, and warfarin in mice. Jpn J Pharmacol 78:191-197.
18. Sitko GR, Ramjit DR, Stabilito, II, Lehman D, Lynch JJ, Vlasuk GP. 1992. Conjunctive enhancement of enzymatic thrombolysis and prevention of thrombotic reocclusion with the selective factor Xa inhibitor, tick anticoagulant peptide. Comparison to hirudin and heparin in a canine model of acute coronary artery thrombosis. Circulation 85:805-815.
19. 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.
20. Turpie AGG, Bauer KA, Eriksson BI, Lassen MR. 2002. Postoperative fondaparinux versus postoperative enoxaparin for prevention of venous thromboembolism after elective hip-replacement surgery: a randomised double-blind trial. Lancet 359:1721-1726.
21. Turpie AGG, Gallus AS, Hoek JA. 2001. A synthetic pentasaccharide for the prevention of deep-vein thrombosis after total hip replacement. New Engl J Med 344:619-625.
22. Weitz JI, Hirsh J. 2001. New anticoagulant drugs. Chest 119:95S-107S.
23. Wong PC, Quan ML, Crain EJ, Watson CA, Wexler RR, Knabb RM. 2000. Nonpeptide factor Xa inhibitors: I. Studies with SF303 and SK549, a new class of potent antithrombotics. J Pharmacol Exp Ther 292:351-357.