Effects of fondaparinux and a direct factor Xa inhibitor TAK-442 on platelet-associated prothrombinase in the balloon-injured artery of rats

Journal of Cardiovascular Pharmacology

Volumn 57, Issue 2, 2011, Pages 201-206

  Konishi, Noriko ^a   Hiroe, Katsuhiko ^a   Kawamura, Masaki ^b  

^a TAKEDA PHARMACEUTICAL COMPANY LIMITED   (Japan)

^b TAKEDA PHARMACEUTICALS   (United States)

Author keywords

endothelial damage; factor Xa inhibitor; percutaneous coronary intervention; platelet associated prothrombinase

Indexed keywords

BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; FONDAPARINUX; TAK 442; THROMBIN; UNCLASSIFIED DRUG;

ANIMAL TISSUE; AORTA; ARTERY INJURY; ARTICLE; BLOOD CLOTTING; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; ENZYME ACTIVITY; HUMAN; IC 50; MALE; NONHUMAN; PRIORITY JOURNAL; RAT; THROMBOCYTE;

ANGIOPLASTY, BALLOON, CORONARY; ANIMALS; AORTA, THORACIC; BLOOD PLATELETS; DOSE-RESPONSE RELATIONSHIP, DRUG; FACTOR XA; HUMANS; MALE; POLYSACCHARIDES; PYRIMIDINONES; RATS; RATS, SPRAGUE-DAWLEY; SULFONES; THROMBOPLASTIN;

EID: 79951551161     PISSN: 01602446     EISSN: None     Source Type: Journal    
DOI: 10.1097/FJC.0b013e31820382a9     Document Type: Article

References (27)

1. Yusuf S, Mehta SR, Chrolavicius S, et al; OASIS-6 Trial Group. Effects of fondaparinux on mortality and reinfarction in patients with acute ST-segment elevation myocardial infarction: the OASIS-6 randomized trial. JAMA. 2006;295:1519-1530.
2. McCann CJ, Menown IB. New anticoagulant strategies in ST elevation myocardial infarction: trials and clinical implications. Vasc Health Risk Manag. 2008;4:305-313. (Pubitemid 351711959)
3. Sabatine MS, Antman EM, Widimsky P, et al. Otamixaban for the treatment of patients with non-ST-elevation acute coronary syndromes (SEPIA-ACS1 TIMI 42): a randomised, double-blind, active-controlled, phase 2 trial. Lancet. 2009;374:787-95.
4. Smith SC Jr., Feldman TE, Hirshfeld JW Jr, et al; American College of Cardiology/American Heart Association Task Force on Practice Guidelines; ACC/AHA/SCAI Writing Committee to Update the 2001 Guidelines for Percutaneous Coronary Intervention. ACC/AHA/SCAI 2005 guideline update for percutaneous coronary intervention-summary article: a report of the American College of Cardiology/American Heart Association Task Force on practice guidelines (ACC/AHA/SCAI Writing Committee to update the 2001 guidelines for percutaneous coronary intervention). J Am Coll Cardiol. 2006;47:216-235.
5. Ruggeri ZM. Platelets in atherothrombosis. Nat Med. 2002;8:1227-1234. (Pubitemid 35373553)
6. Mann KG, Nesheim ME, Church WR, et al. Surface-dependent reactions of the vitamin K-dependent enzyme complexes. Blood. 1990;76:1-16. (Pubitemid 20220784)
7. Ghigliotti G, Waissbluth AR, Speidel C, et al. Prolonged activation of prothrombin on the vascular wall after arterial injury. Arterioscler Thromb Vasc Biol. 1998;18:250-257. (Pubitemid 28277602)
8. Rezaie AR. Prothrombin protects factor Xa in the prothrombinase complex from inhibition by the heparin-antithrombin complex. Blood. 2001;97:2308-2313. (Pubitemid 32291476)
9. Rezaie AR. DX-9065a inhibition of factor Xa and the prothrombinase complex: mechanism of inhibition and comparison with therapeutic heparins. Thromb Haemost. 2003;89:112-121. (Pubitemid 36149800)
10. Chu V, Brown K, Colussi D, et al. Pharmacological characterization of a novel factor Xa inhibitor, FXV673. Thromb Res. 2001;103:309-324. (Pubitemid 32787022)
11. Perzborn E, Strassburger J, Wilmen A, et al. In vitro and in vivo studies of the novel antithrombotic agent BAY 59-7939-an oral, direct Factor Xa inhibitor. J Thromb Haemost. 2005;3:514-521. (Pubitemid 41632877)
12. Furugohri T, Isobe K, Honda Y, et al. DU-176b, a potent and orally active factor Xa inhibitor: in vitro and in vivo pharmacological profiles. J Thromb Haemost. 2008;6:1542-1549.
13. Fujimoto T, Imaeda Y, Konishi N, et al. Discovery of a tetrahydropyr-imidin-2(1H)-one derivative (TAK-442) as a potent, selective, and orally active factor Xa inhibitor. J Med Chem. 2010;53:3517-3531.
14. Hocheberg Y, Tamhane AC. Multiple Comparison Procedures. New York, NY: Wiley, 1987.
15. Monković DD, Tracy PB. Functional characterization of human platelet-released factor V and its activation by factor Xa and thrombin. J Biol Chem. 1990;265:17132-17140.
16. Marmur JD, Merlini PA, Sharma SK, et al. Thrombin generation in human coronary arteries after percutaneous transluminal balloon angioplasty. J Am Coll Cardiol. 1994;24:1484-1491. (Pubitemid 24344244)
17. Wittkowsky AK. The role of thrombin inhibition during percutaneous coronary intervention. Pharmacotherapy. 2002;22(6 pt 2):S97-S104.
18. Donat F, Duret JP, Santoni A, et al. The pharmacokinetics of fondaparinux sodium in healthy volunteers. Clin Pharmacokinet. 2002;41(Suppl 2):1-9. (Pubitemid 35155551)
19. Cohen M, Bhatt DL, Alexander JH, et al; SEPIA-PCI Trial Investigators. Randomized, double-blind, dose-ranging study of otamixaban, a novel, parenteral, short-acting direct factor Xa inhibitor, in percutaneous coronary intervention: the SEPIA-PCI trial. Circulation. 2007;115:2642-2651. (Pubitemid 46791363)
20. Samama MM, Gerotziafas GT, Elalamy I, et al. Biochemistry and clinical pharmacology of new anticoagulant agents. Pathophysiol Haemost Thromb. 2002;32:218-224. (Pubitemid 37490542)
21. Koopman MM, Büller HR. Short- and long-acting synthetic pentasac-charides. J Intern Med. 2003;254:335-342.
22. Brufatto N, Ward A, Nesheim ME. Factor Xa is highly protected from antithrombin-fondaparinux and antithrombin-enoxaparin when incorporated into the prothrombinase complex. J Thromb Haemost. 2003;1:1258-1263.
23. Konishi N, Hiroe K, Kawamura M. Synergistic effect of a factor Xa inhibitor, TAK-442, and antiplatelet agents on whole blood coagulation and arterial thrombosis in rats. Thromb Res. 2010;126:124-129.
24. Annex BH, Denning SM, Channon KM, et al. Differential expression of tissue factor protein in directional atherectomy specimens from patients with stable and unstable coronary syndromes. Circulation. 1995;91: 619-622.
25. Marmur JD, Thiruvikraman SV, Fyfe BS, et al. Identification of active tissue factor in human coronary atheroma. Circulation. 1996;94:1226-1232. (Pubitemid 26307246)
26. Steffel J, Lüscher TF, Tanner FC. Tissue factor in cardiovascular diseases: molecular mechanisms and clinical implications. Circulation. 2006;113: 722-731.
27. Mallat Z, Tedgui A. Current perspective on the role of apoptosis in atherothrombotic disease. Circ Res. 2001;88:998-1003. (Pubitemid 34137111)