Pharmacological characterization of the active synthetic factor Xa inhibitors M55551 and M55165

European Journal of Pharmacology

Volumn 529, Issue 1-3, 2006, Pages 164-171

  Hosaka, Yoshitaka ^a   Matsumoto, Miwa ^a   Shinozaki, Mikihiko ^a   Ohno, Tamami ^a   Yatagai, Yukiko ^a   Kamiya, Masatsugu ^a   Kurokawa, Misao ^a   Nishida, Hidemistu ^a   Matsusue, Tomokazu ^a   Mizuguchi, Kiyoshi ^a   Ishii, Hidemi ^b  

^a MOCHIDA PHARMACEUTICAL CO   (Japan)

^b SHOWA PHARMACEUTICAL UNIVERSITY   (Japan)

Author keywords

Anticoagulant; Factor Xa inhibitor; M55165; M55551

Indexed keywords

ANTICOAGULANT AGENT; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; M 55165; M 55551; UNCLASSIFIED DRUG; WARFARIN;

ANIMAL EXPERIMENT; ARTICLE; BLEEDING TIME; BLOOD CLOTTING; BLOOD CLOTTING TIME; CONTROLLED STUDY; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG HALF LIFE; DRUG POTENCY; HUMAN; IN VITRO STUDY; MALE; NONHUMAN; PLASMA; PRIORITY JOURNAL; RAT; THROMBOGENESIS;

ADMINISTRATION, ORAL; ANIMALS; ANTICOAGULANTS; BIOLOGICAL AVAILABILITY; BLEEDING TIME; DISEASE MODELS, ANIMAL; FACTOR XA; HALF-LIFE; HUMANS; INJECTIONS, INTRAVENOUS; MALE; PIPERAZINES; RATS; RATS, WISTAR; VENOUS THROMBOSIS;

EID: 29344442845     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejphar.2005.11.002     Document Type: Article

References (26)

1. J.H. Alexander, C.K. Dyke, H. Yang, R.C. Becker, V. Hasselblad, L.A. Zillman, N.S. Kleiman, J.S. Hochman, P.B. Berger, E.A. Cohen, A.M. Lincoff, H. Saint-Jacques, S. Chetcuti, J.R. Burton, J.M. Buergler, F.P. Spence, Y. Shimoto, T.L. Robertson, S. Kunitada, E.G. Bovill, P.W. Armstrong, R.A. Harrington The XaNADU-PCI PILOT Investigators Initial experience with factor-Xa inhibition in percutaneous coronary intervention: the XaNADU-PCI Pilot J. Thromb. Haemost. 2 2004 234 241
2. H.K. Breddin Experimental and clinical results with the thrombin inhibitor argatroban Hamostaseologie 22 2002 55 59
3. J.T. Call, E.N. Deliargyris, and D.C. Sane Direct thrombin inhibitors in the treatment of immune-mediated heparin-induced thrombocytopenia Semin. Thromb. Hemost. 30 2004 297 304
4. C.K. Dyke, R.C. Becker, N.S. Kleiman, J.S. Hochman, E.G. Bovill, A.M. Lincoff, G. Gerstenblith, V. Dzavik, L.H. Gardner, V. Hasselblad, L.A. Zillman, Y. Shimoto, T.L. Robertson, S. Kunitada, P.W. Armstrong, and R.A. Harrington First experience with direct factor Xa inhibition in patients with stable coronary disease. A pharmacokinetic and pharmacodynamic evaluation Circulation 105 2002 2385 2391
5. F. Fourrier, C. Chopin, J.J. Huart, I. Runge, C. Caron, and J. Goudemand Double-blind, placebo-controlled trial of antithrombin III concentrates in septic shock with disseminated intravascular coagulation Chest 104 1993 882 888
6. C.W. Francis, V.D. Pellegrini Jr., C.M. Harris, and V.J. Marder Antithrombin III prophylaxis of venous thromboembolic disease after total hip or total knee replacement Am. J. Med. 87 3B 1989 61S 66S
7. T. Hara, A. Yokoyama, H. Ishihara, Y. Yokoyama, T. Nagahara, and M. Iwamoto DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa Thromb. Haemost. 71 1994 314 319
8. T. Hara, A. Yokoyama, K. Tanabe, H. Ishihara, and M. Iwamoto DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats Thromb. Haemost. 74 1995 635 639
9. J.M. Herbert, J.P. Hérault, A. Bernat, R.G.M. van Amsterdam, J.C. Lormeau, M. Petitou, C. van Boeckel, P. Hoffmann, and D.G. Meuleman Biochemical and pharmacological properties of SANORG 34006, a potent and long-acting synthetic pentasaccharide Blood 91 1998 4197 4205
10. J. Hirsh, J.E. Dalen, D.R. Anderson, L. Poller, H. Bussey, J. Ansell, and D. Deykin Oral anticoagulants: mechanism of action, clinical effectiveness, and optimal therapeutic range Chest 119 2001 8S 21S
11. J. Hirsh, T.E. Warkentin, S.G. Shaughnessy, S.S. Anand, J.L. Halperin, R. Raschke, C. Granger, E.M. Ohman, and J.E. Dalen Heparin and low-molecular-weight heparin. Mechanisms of action, pharmacokinetics, dosing, monitoring, efficacy, and safety Chest 119 2001 64S 94S
12. B. Kaiser DX-9065a, a direct inhibitor of factor Xa Cardiovasc. Drug Rev. 21 2003 91 104
13. L.-A. Linkins, and J.I. Weitz New anticoagulants Semin. Thromb. Hemost. 29 2003 619 631
14. K.G. Mann Biochemistry and physiology of blood coagulation Thromb. Haemost. 82 1999 165 174
15. T. Nagahara, Y. Yokoyama, K. Inamura, S. Katakura, S. Komoriya, H. Yamaguchi, T. Hara, and M. Iwamoto Dibasic (amidinoaryl)propanoic acid derivatives as novel blood coagulation factor Xa inhibitors J. Med. Chem. 37 1994 1200 1207
16. H. Nishida, Y. Miyazaki, Y. Kitamura, M. Ohashi, T. Matsusue, A. Okamoto, Y. Hosaka, S. Ohnishi, and H. Mochizuki Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitor Chem. Pharm. Bull. 49 2001 1237 1244
17. H. Nishida, Y. Miyazaki, T. Mukaihira, F. Saitoh, M. Fukui, K. Harada, M. Itoh, A. Muraoka, T. Matsusue, A. Okamoto, Y. Hosaka, M. Matsumoto, S. Ohnishi, and H. Mochizuki Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as a factor Xa inhibitor II. Substituent effect on biological activities Chem. Pharm. Bull. 50 2002 1187 1194
18. H. Nishida, Y. Miyazaki, T. Mukaihira, H. Shimada, K. Suzuki, F. Saitoh, M. Mizuno, T. Matsusue, A. Okamoto, Y. Hosaka, M. Matsumoto, S. Ohnishi, and H. Mochizuki Synthesis and evaluation of 1-arylsulfonyl-3-piperazinone derivatives as factor Xa inhibitors III. Effect of ring opening of piperazinone moiety on inhibition Chem. Pharm. Bull. 52 2004 459 462
19. F. Paolucci, M.-C. Claviés, F. Donat, and J. Necciari Fondaparinux sodium mechanism of action. Identification of specific binding to purified and human plasma-derived proteins Clin. Pharmacokinet. 41 Suppl. 2 2002 11 18
20. K. Sato, T. Kawasaki, Y. Taniuchi, F. Hirayama, H. Koshio, and Y. Matsumoto YM-60828, a novel factor Xa inhibitor: separation of its antithrombotic effects from its prolongation of bleeding time Eur. J. Pharmacol. 339 1997 141 146
21. L. Stella, M.B. Donati, and G. de Gaetano Bleeding time in laboratory animals. I. Aspirin dose not prolong bleeding time in rats Thromb. Res. 7 1975 709 716
22. Y. Taniuchi, Y. Sakai, N. Hisamichi, M. Kayama, Y. Mano, K. Sato, F. Hirayama, H. Koshio, Y. Matsumoto, and T. Kawasaki Biochemical and pharmacological characterization of YM-60828, a newly synthesized and orally active inhibitor of human factor Xa Thromb. Haemost. 79 1998 543 548
23. A.H. Tran, and G. Lee Fondaparinux for prevention of venous thromboembolism in major orthopedic surgery Ann. Pharmacother. 37 2003 1632 1643
24. G.M. Vogel, D.G. Meuleman, F.G. Bourgondien, and P.M. Hobbelen Comparison of two experimental thrombosis models in rats effects of four glycosaminoglycans Thromb. Res. 54 1989 399 410
25. J.M. Walenga, W.P. Jeske, D. Hoppensteadt, and J. Fareed Factor Xa inhibitors: today and beyond Curr. Opin. Investig. Drugs 4 2003 272 281
26. T.E. Warkentin An overview of the heparin-induced thrombocytopenia syndrome Semin. Thromb. Hemost. 30 2004 273 283