Administration of a small molecule tissue factor/Factor VIIa inhibitor in a non-human primate thrombosis model of venous thrombosis: Effects on thrombus formation and bleeding time

Thrombosis Research

Volumn 112, Issue 3, 2003, Pages 167-174

  Szalony, James A ^a   Suleymanov, Osman D ^a   Salyers, Anita K ^a   Panzer Knodle, Susan G ^a   Blom, Jason D ^a   LaChance, Rhonda M ^a   Case, Brenda L ^a   Parlow, John J ^a   South, Michael S ^a   Wood, Rhonda S ^a   Nicholson, Nancy S ^a  

^a PFIZER INC   (United States)

Author keywords

Animal models; Aspirin; Cardiovascular; Factor VIIa; Thrombosis; Tissue factor

Indexed keywords

2 [6 (3 AMINO 5 HYDROXYPHENYL) 3 (ISOPROPYLAMINO) 2 OXOPYRAZIN 1(2H) YL] N [4 [AMINO(IMINO)METHYL]BENZYL]ACETAMIDE; ACETYLSALICYLIC ACID; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 7A; BLOOD CLOTTING FACTOR 7A INHIBITOR; PHA 798; THROMBIN; THROMBOPLASTIN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; BLEEDING TIME; CAVA VEIN; CONTROLLED STUDY; DOSE RESPONSE; DRUG EFFECT; DRUG EFFICACY; DRUG SAFETY; DRUG SELECTIVITY; IC 50; MALE; MOLECULAR SIZE; NONHUMAN; PRIMATE; PRIORITY JOURNAL; THROMBOGENESIS; THROMBOSIS; THROMBUS; VEIN THROMBOSIS;

EID: 10744220161     PISSN: 00493848     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.thromres.2003.10.017     Document Type: Article

References (37)

1. Fowkes F.J.I., Price J.F., Fowkes F.G.R. Incidence of diagnosed deep vein thrombosis in the general population: systematic review. Eur. J. Vasc. Endovasc. Surg. 25:2003;1-5.
2. Bick R.L. Proficient and cost-effective approaches for the prevention and treatment of venous thrombosis and thromboembolism. Drugs. 60:2000;575-595.
3. Haas S.K. Venous thromboembolic risk and its prevention in hospitalized medical patients. Semin. Thromb. Hemost. 28:2002;577-583.
4. Geerts W.H., Heit J.A., Clagett G.P., Pineo G.F., Colwell C.W., Anderson F.A.et al. Prevention of venous thromboembolism. Chest. 119:2001;132S-175S.
5. Merli G.J. Current pharmacotherapeutic options for treating deep vein thrombosis. Expert Opin. Pharmacol. 4:2003;55-65.
6. Wong G.C., Giugliano R.P., Antman E.R. Use of low-molecular-weight heparins in the management of acute coronary artery syndromes and percutaneous coronary intervention. JAMA. 289:2003;331-342.
7. Harenberg J., Stehle G., Blauth M., Huck K., Mall K., Heene D.L. Dosage, anticoagulant, and antithrombotic effects of heparin and low-molecular-weight heparin in the treatment of deep vein thrombosis. Semin. Thromb. Hemost. 23(1):1997;83-90.
8. Gurfinkel E., Fareed J., Antman E., Cohen M., Mautner B. Rationale for the management of coronary syndromes with low-molecular-weight heparins. Am. J. Cardiol. 82(5B):1998;15L-18L.
9. Ginsberg J.A., Crowther M.A., White R.H., Ortel T.L. Anticoagulation therapy. Hematology (Am. Soc. Hematol. Educ. Program). 2001;339-357.
10. Rogers J.F., Nafziger A.N., Bertino J.S. Jr. Pharmacogenetics affects dosing, efficacy, and toxicity of cytochrome P450-metabolized drugs. Am. J. Med. 113(9):2002;746-750.
11. Hirsh J., Dalen J., Anderson D.R., Poller L., Bussey H., Ansell J.et al. Oral anticoagulants: mechanism of action, clinical effectiveness, and optimal therapeutic range. Chest. 119(1 Suppl.):2001;8S-21S.
12. Wittkowsky A.K. Drug interactions update: drugs, herbs, and oral anticoagulation. J. Thromb Thrombolysis. 12(1):2001;67-71.
13. Ansell J.E., Weitz J.I., Comerota A.J. Advances in therapy and the management of antithrombotic drugs for venous thromboembolism. Hematology (Am. Soc. Hematol. Educ. Program). 2000;266-284.
14. Eriksson B.I., Arfwidsson A.C., Frison L., Eriksson U.G., Bylock A., Kälebo P.et al. A dose-ranging study of the oral direct thrombin inhibitor, ximelagatran, and its subcutaneous form, melagatran, compared with dalteparin in the prophylaxis of thromboembolism after hip or knee replacement: METHRO I. Thromb. Haemost. 87:2002;231-237.
15. Heit J.A., Colwell C.W., Francis C.W., Ginsberg J.S., Berkowitz S.D., Whipple J.et al. Comparison of the oral direct thrombin inhibitor ximelagatran with enoxaparin as prophylaxis against venous thromboembolism after total knee replacement: a phase 2 dose-finding study. Arch. Intern. Med. 161:2001;2215-2221.
16. Turpie A.G.G., Bauer K.A., Eriksson B.I., Lassen M.R. Fondaparinux vs. enoxaparin for the prevention of venous thromboembolism in major orthopedic surgery: a meta-analysis of 4 randomized double-blind studies. Arch. Intern. Med. 162:2002;1833-1840.
17. Broze G.J. The tissue factor pathway of coagulation. Loscalzo J., Schafer A.I. Thrombosis and hemorrhage. 1994;57-86 Blackwell, Boston.
18. Coughlin S.R. Thrombin signaling and protease-activated receptors. Nature. 407:2000;258-264.
19. Szalony J.A., Taite B.B., Girard T.J., Nicholson N.S., LaChance R.M. Pharmacological intervention at disparate sites in the coagulation cascade: comparison of anti-thrombotic efficacy vs. bleeding propensity in a rat model of acute arterial thrombosis. J. Thromb. Thrombolysis. 14(2):2002;113-121.
20. Himber B., Kirebbofer D., Riederer M., Tschopp T.B., Steiner B., Roux S.P. Dissociation of antithrombotic effect and bleeding time prolongation in rabbits by inhibiting tissue factor function. Thromb. Haemost. 78:1997;1142-1149.
21. Harker L.A., Hanson S.R., Wilcox J.N., Kelly A.B. Antithrombotic and antilesion benefits without hemorrhagic risks by inhibiting tissue factor pathway. Haemostasis. 26(Suppl. 1):1996;76-82.
22. Suleymanov O.D., Szalony J.A., Salyers A.K., LaChance R.M., Parlow J.P., South M.S.et al. Pharmacological interruption of acute thrombus formation with minimal hemorrhagic complications by a small molecule tissue factor/factor VIIa inhibitor: comparison to factor Xa and Thrombin inhibition in a non-human primate thrombosis model. J. Pharmacol. Exp. Ther. 306:2003;1115-1121.
23. Lee A., Agnelli G., Büller H., Ginsberg J., Heit J., Rote W.et al. Dose-response study of recombinant factor VIIa/tissue factor inhibitor recombinant nematode anticoagulant protein c2 in prevention of postoperative venous thromboembolism in patients undergoing total knee replacement. Circulation. 104:2001;74-78.
24. Parlow J.J., Case B.L., Dice T.A., Fenton R.L., Hayes M.J., Jones D.E.et al. Design, parallel synthesis, and crystal structures of pyrazinone antithrombotics as selective inhibitors of the tissue Factor VIIa complex. J. Med. Chem. 46:2003;4050-4062.
25. South M.S., Case B.L., Wood R.S., Jones D.E., Hayes M.J., Girard T.J.et al. Structure-based drug design of pyrazinone antithrombotics as selective inhibitors of the tissue Factor VIIa complex. Bioorg. Med. Chem. Lett. 13:2003;2319-2325.
26. Hollenbach S., Sinha U., Lin P.H., Needham K., Frey L., Hancock T.et al. A comparative study of prothrombinase and thrombin inhibitors in a novel rabbit model of non-occlusive deep vein thrombosis. Thromb. Haemost. 71(3):1994;357-362.
27. Franzeck U.K., Schalch I., Jäger K.A., Schneider E., Grimm J., Bollinger A. Prospective 12-year follow-up study of clinical and hemodynamic sequelae after deep vein thrombosis in low-risk patients (Zurich study). Circulation. 93:1996;74-79.
28. Prandoni P., Lensing A.W.A., Cogo A., Cuppini S., Villalta S., Carta M. et al. The long-term clinical course of acute deep venous thrombosis. Ann. Intern. Med. 125:1996;1-7.
29. Giesen P.L.A., Rauch U., Bohrmann B., Kling D., Roque M., Fallon J.T.et al. Blood-borne tissue factor: another view of thrombosis. Proc. Natl. Acad. Sci. 96:1999;2311-2315.
30. Himber J., Wohlgensinger C., Roux S., Damico L.A., Fallon J.T., Kirchhofer D.et al. Inhbition of tissue factor limits the growth of venous thrombus in the rabbit. J. Thromb. Haemost. 1:2003;889-895.
31. Mehta J.L., Chen L., Nichols W.W., Mattsson C., Gustafsson D., Daldeen T.G. Melagatran, an oral active-site inhibitor of thrombin, prevents or delays formation of electrically induced occlusive thrombus in the canine coronary artery. J. Cardiovasc. Pharm. 31:1998;245-251.
32. Carlsson S., Elg M., Mattsson C. Effects of ximelagatran, the oral form of melagatran, in the treatment of caval vein thrombosis in conscious rats. Thromb. Res. 107:2002;163-168.
33. Eriksson H., Eriksson U.G., Frison L., Hansson P.O., Held P., Holmstrom M.et al. Pharmacokinetics and pharmacodynamics of melagatran, a novel synthetic LMW thrombin inhibitor, in patients with acute DVT. Thromb. Haemost. 81:1999;358-363.
34. Heit J.A. The potential role of fondaparinux as venous thromboembolism prophylaxis after total hip or knee replacement or hip fracture surgery. Arch. Intern. Med. 162(16):2002;1806-1808.
35. Glynn O. The express study: preliminary results. Int. J. Clin. Pract. 57(1):2003;57-59.
36. Reitman R.D., Emerson R.H., Higgins L.L., Tarbox T.R. A multimodality regimen for deep venous thrombosis prophylaxis in total knee arthroplasty. J. Arthroplasty. 18(2):2003;161-168.
37. Brookenthal K.R., Freedman K.B., Lotke P.A., Fitzgerald R.H., Lonner J.H. A meta-analysis of thromboembolic prophylaxis in total knee arthroplasty. J. Arthroplasty. 16(3):2001;293-300.