Melagatran, a direct thrombin inhibitor, but not edoxaban, a direct factor Xa inhibitor, nor heparin aggravates tissue factor-induced hypercoagulation in rats

European Journal of Pharmacology

Volumn 686, Issue 1-3, 2012, Pages 74-80

  Furugohri, Taketoshi ^a   Fukuda, Toshio ^a   Tsuji, Naoki ^a   Kita, Akemi ^a   Morishima, Yoshiyuki ^a   Shibano, Toshiro ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Edoxaban; Factor Xa inhibitor; Hypercoagulation; Thrombin inhibitor; Tissue factor

Indexed keywords

BLOOD CLOTTING FACTOR 10A; EDOXABAN; HEPARIN; MELAGATRAN; THROMBIN; THROMBOPLASTIN;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLOOD SAMPLING; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG BLOOD LEVEL; DRUG DOSE COMPARISON; DRUG EFFICACY; DRUG MECHANISM; DRUG MEGADOSE; ENZYME ACTIVATION; ENZYME INHIBITION; HEMATOLOGICAL PARAMETERS; HYPERCOAGULABILITY; LOW DRUG DOSE; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; THROMBOCYTE COUNT; TREATMENT RESPONSE;

ANIMALS; ANTITHROMBINS; AZETIDINES; BENZYLAMINES; BLOOD COAGULATION DISORDERS; FACTOR XA; HEPARIN; MALE; PYRIDINES; RATS; RATS, WISTAR; THIAZOLES; THROMBOPLASTIN;

EID: 84861633299     PISSN: 00142999     EISSN: 18790712     Source Type: Journal    
DOI: 10.1016/j.ejphar.2012.04.031     Document Type: Article

References (25)

1. J. Ansell Factor Xa or thrombin: is factor Xa a better target? J. Thromb. Haemost. 5 Suppl. 1 2007 60 64
2. H. Asakura, T. Ichino, T. Yoshida, Y. Suga, Y. Ontachi, T. Mizutani, M. Kato, T. Ito, M. Yamazaki, K. Aoshima, E. Morishita, M. Saito, K.I. Miyamoto, and S. Nakao Beneficial effect of JTV-803, a new synthetic inhibitor of activated factor X, against both lipopolysaccharide-induced and tissue factor-induced disseminated intravascular coagulation in rat models Blood Coagul. Fibrinolysis 13 2002 233 239
3. S.J. Connolly, M.D. Ezekowitz, S. Yusuf, J. Eikelboom, J. Oldgren, A. Parekh, J. Pogue, P.A. Reilly, E. Themeles, J. Varrone, S. Wang, M. Alings, D. Xavier, J. Zhu, R. Diaz, B.S. Lewis, H. Darius, H.C. Diener, C.D. Joyner, L. Wallentin RE-LY Steering Committee and Investigators Dabigatran versus warfarin in patients with atrial fibrillation N. Engl. J. Med. 361 2009 1139 1151
4. B. Dahlback, and B.O. Villoutreix Molecular recognition in the protein C anticoagulant pathway J. Thromb. Haemost. 1 2003 1525 1534
5. G. Dickneite, D. Seiffge, K.H. Diehl, M. Reers, J. Czech, E. Weinmann, D. Hoffmann, and W. Stüber Pharmacological characterization of a new 4-amidinophenyl-alanine thrombin-inhibitor (CRC 220) Thromb. Res. 77 1995 357 368
6. C.T. Esmon The protein C pathway Chest 124 2003 26S 32S
7. FDA Integrated executive summary of FDA review for NDA 21-686 Exanta (Ximelagatran) 2004 Food and Drug Administration Washington (DC)
8. T. Furugohri, Y. Shiozaki, S. Muramatsu, Y. Honda, T. Matsumoto, K. Isobe, and N. Sugiyama Different antithrombotic properties of factor Xa inhibitor and thrombin inhibitor in rat thrombosis models Eur. J. Pharmacol. 514 2005 35 42
9. T. Furugohri, K. Isobe, Y. Honda, C. Kamisato-Matsumoto, N. Sugiyama, T. Nagahara, Y. Morishima, and T. Shibano DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles J. Thromb. Haemost. 6 2008 1542 1549
10. T. Furugohri, N. Sugiyama, Y. Morishima, and T. Shibano Antithrombin-independent thrombin inhibitors, but not direct factor Xa inhibitors, enhance thrombin generation in plasma through inhibition of thrombin-thrombomodulin-protein C system Thromb. Haemost. 106 2011 1076 1083
11. C.B. Granger, J.H. Alexander, J.J. McMurray, R.D. Lopes, E.M. Hylek, M. Hanna, H.R. Al-Khalidi, J. Ansell, D. Atar, A. Avezum, M.C. Bahit, R. Diaz, J.D. Easton, J.A. Ezekowitz, G. Flaker, D. Garcia, M. Geraldes, B.J. Gersh, S. Golitsyn, S. Goto, A.G. Hermosillo, S.H. Hohnloser, J. Horowitz, P. Mohan, P. Jansky, B.S. Lewis, J.L. Lopez-Sendon, P. Pais, A. Parkhomenko, F.W. Verheugt, J. Zhu, L. Wallentin ARISTOTLE Committees and Investigators Apixaban versus warfarin in patients with atrial fibrillation N. Engl. J. Med. 365 2011 981 992
12. 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
13. J. Hathcock Vascular biology-the role of tissue factor Semin. Hematol. 41 2004 30 34
14. R. He, S. Xiong, X. He, F. Liu, J. Han, J. Li, and S. He The role of factor XI in a dilute thromboplastin assay of extrinsic coagulation pathway Thromb. Haemost. 85 2001 1055 1059
15. S. Jander, M. Sitzer, A. Wendt, M. Schroeter, M. Buchkremer, M. Siebler, W. Müller, W. Sandmann, and G. Stoll Expression of tissue factor in high-grade carotid artery stenosis: association with plaque destabilization Stroke 32 2001 850 854
16. C. Mattsson, A. Menschik-Lundin, S. Nylander, E. Gyzander, and J. Deinum Effect of different types of thrombin inhibitors on thrombin/thrombomodulin modulated activation of protein C in vitro Thromb. Res. 104 2001 475 486
17. Y. Morishima, K. Tanabe, Y. Terada, T. Hara, and S. Kunitada Antithrombotic and hemorrhagic effects of DX-9065a, a direct and selective factor Xa inhibitor: comparison with a direct thrombin inhibitor and antithrombin III-dependent anticoagulants Thromb. Haemost. 78 1997 1366 1371
18. Y. Morishima, T. Furugohri, Y. Shiozaki, N. Sugiyama, and T. Shibano Antithrombin-independent thrombin inhibitors, but not factor Xa inhibitors, enhance thrombin generation in human plasma via inhibition of Thrombin-Thrombomodulin-Protein C System Blood (ASH Annual Meeting Abstracts) 108 2006 914
19. M.R. Patel, K.W. Mahaffey, J. Garg, G. Pan, D.E. Singer, W. Hacke, G. Breithardt, J.L. Halperin, G.J. Hankey, J.P. Piccini, R.C. Becker, C.C. Nessel, J.F. Paolini, S.D. Berkowitz, K.A. Fox, R.M. Califf ROCKET AF Investigators Rivaroxaban versus warfarin in nonvalvular atrial fibrillation N. Engl. J. Med. 365 2011 883 891
20. E. Perzborn, and M. Harwardt Direct thrombin inhibitors, but not factor Xa inhibitors, enhance thrombin formation in human plasma by interfering with the Thrombin-Thrombomodulin-Protein C system Blood (ASH Annual Meeting Abstracts) 112 2008 198 199
21. E. Perzborn, U. Buetehorn, E. Fischer, M. Harwardt, M. Klages, and A. Trabandt Hypercoagulability in rats is increased by low doses of the direct thrombin inhibitor melagatran, but is reduced by the direct factor Xa inhibitor rivaroxaban Eur. Heart J. 29 2008 828 829 (abstract supplement)
22. J.I. Weitz Factor Xa or thrombin: Is thrombin a better target? J. Thromb. Haemost. 5 Suppl. 1 2007 65 67
23. A.K. Wittkowsky Why warfarin and heparin need to overlap when treating acute venous thromboembolism Dis. Mon. 51 2005 112 115
24. M. Yamazaki, H. Asakura, K. Aoshima, M. Saito, H. Jokaji, C. Uotani, I. Kumabashiri, E. Morishita, T. Ikeda, and T. Matsuda 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 392 396
25. M.U. Zafar, D.A. Vorchheimer, J. Gaztanaga, M. Velez, D. Yadegar, P.R. Moreno, S. Kunitada, J. Pagan, V. Fuster, and J.J. Badimon Antithrombotic effects of factor Xa inhibition with DU-176b: Phase-I study of an oral, direct factor Xa inhibitor using an ex-vivo flow chamber Thromb. Haemost. 98 2007 883 888