Advances in Antithrombotic Therapy: Novel Agents

• References

• 1 Rosenberg RD. The heparin-antithrombin system: a natural anticoagulant mechanism. In: Colman RW, Hirsh J, Marder VJ, Salzman EW. (eds) Hemostasis and Thrombosis: Basic Principles and Clinical Practice. 3rd. ed. JB Lippincott; Philadelphia: 1994. pp 837-860
• 2 Weitz JI, Hirsh J. New anticoagulant strategies. J Lab Clin Med 1993; 122: 364-373
• 3 Hirsh J, Salzman EW, Marder VJ, Colman RW. Therapeutic agents and their practical use in thrombotic disorders: Approach to the thrombophilic patient for hemostasis and thrombosis. In: Colman RW, Hirsh J, Marder VJ, Salzman EW. (eds) Hemostasis and Thrombosis: Basic Principles and Clinical Practice. 3rd. ed. JB Lippincott; Philadelphia: 1994
• 4 Harker LA, Gent M. Pathogenesis of arterial thrombosis. In Colman RW, Hirsh J, Marder VJ, Salzman EW. (eds) Hemostasis and Thrombosis: Basic Principles and Clinical Practice. 3rd. ed. JB Lippincott; Philadelphia: 1994
• 5 Hirsh J. Heparin. N Engl J Med 1991; 324: 1565-1574
• 6 Hirsh J. Oral anticoagulant drugs. N Engl J Med 1991; 324: 1865-1875
• 7 Harker LA, Maraganore JM, Hirsh J. Novel antithrombotic agents. In: Colman RW, Hirsh J, Marder VJ, Salzman EW. (eds) Hemostasis and Thrombosis: Basic Principles and Clinical Practice. 3rd. ed. JB Lippincott; Philadelphia: 1994
• 8 Levine M, Hirsh J, Gent M, Turpie AG G, Cruickshank M, Weitz J, Anderson D, Johnson M. A randomized trial comparing active thromboplastin time with heparin assay in patients with acute venous thromboembolism requiring large daily doses of heparin. Arch Int Med 1994; 154: 49-56
• 9 Hirsh J, Levine MN. Low molecular weight heparin. Blood 1992; 79: 1-17
• 10 Weitz JI, Hudoba M, Massel D, Maraganore J, Hirsh J. Clot-bound thrombin is protected from inhibition by heparin-antithrombin III but is susceptible to inactivation by antithrombin Ill-independent inhibitors. J Clin Invest 1990; 86: 385-391
• 11 Markwardt F. Hirudin and derivatives as anticoagulant agents. Thromb Haemostas 1991; 66: 141-152
• 12 Rydel TJ, Ravichandran KG, Tulinsky A. et al. The structure of a complex of recombinant hirudin and human α-thrombin. Science 1990; 249: 277-180
• 13 Maraganore JM, Chao B, Joseph ML, Jablonski J, Ramachandron KL. Anticoagulant activity of synthetic hirudin fragments. J Biol Chem 1989; 264: 8692-8698
• 14 Maraganore JM, Bourdon P, Jablonski J, Ramachandron KL, Fenton II JW. Design and characterization of hirulogs: a novel class of bivalent peptide inhibitors of thrombin. Biochemistry 1990; 29: 7095-7801
• 15 Haskel EJ, Prager NA, Sobel BE, Abendschein DR. Relative efficacy of antithrombin compared with antiplatelet agents in accelerating coronary thrombolysis and preventing early reocclusion. Circulation 1991; 83: 1048-1056
• 16 Heras M, Chesebro JH, Penny WJ, Bailey KR, Badimon L, Fuster V. Effects of thrombin inhibition on the development of acute platelet-thrombus deposition during angioplasty in pigs. Heparin versus recombinant hirudin, a specific thrombin inhibitor Circulation 1989; 79: 657-665
• 17 Klement P, Borm A, Hirsh J, Maraganore J, Wilson G, Weitz JI. The effect of thrombin inhibitors on tissue plasminogen activator induced thrombolysis in a rat model. Thromb Haemost 1992; 68: 64-68
• 18 Sitko GR, Ramjit DR, Stabilito II, Lehman D, Lynch JJ, Vlasuk GP. 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 an animal model of acute coronary artery thrombosis. Circulation 1992; 85: 805-815
• 19 Agnelli G, Pascucci C, Cosmi B, Nenci GG. The comparative effects of recombinant hirudin (CGP 39393) and standard heparin on thrombus growth in rabbits. Thromb Haemost 1990; 63: 204-207
• 20 Agnelli G, Renga C, Weitz JI, Nenci GG, Hirsh J. Sustained antithrombotic activity of hirudin after its plasma clearance: Comparison with heparin. Blood 1992; 80: 960-965
• 21 Kikumoto R, Tamao Y, Tesuka T, Tonomura S, Hara H, Ninomiya K, Hijikata A, Okamoto S. Selective inhibition of thrombin by (2R,4R)-4-methyl-1 [N²-[(3-methy 1-1,2,3,4-tetrahydro-8-quinoliny 1) sulfonyl]-L-arginyl)]-2-piperidinecarboxylic acid. Biochemistry 1984; 23: 85-90
• 22 Kettner C, Shaw E. D-Phe-Pro-ArgCH₂Cl. A selective affinity label for thrombin. Thromb Res 1979; 14: 969-973
• 23 Bagdy D, Barabas E, Szabo G, Bajusz S, Szell E. In vivo anticoagulant and antiplatelet effect of D-Phe-Pro-Arg-H and D-MePhe-Pro-Arg-H. Thromb Haemost 1992; 67: 357-365
• 24 Krupski WC, Bass A, Kelly AB. et al. Heparin-resistant thrombus formation by endovascular stents in baboons: Interruption by a synthetic antithrombin. Circulation 1990; 82: 570
• 25 Kettner C, Mersinger L, Knabb R. The selective inhibition of thrombin by peptides of boroarginine. J Biol Chem 1990; 265: 18289
• 26 Kotze H, Lumsden A, Harker LA. et al. In vivo antithrombotic effects of local vs systemic therapy with potent antithrombins (Abstract). Circulation 1990; 82 Suppl (Suppl. 03) 111-659
• 27 Hanson SR, Harker LA. Interruption of acute platelet-dependent thrombosis by the synthetic antithrombin D-phenylalanyl-L-propyl-arginyl chloromethyl ketone. Proc Natl Acad Sci USA 1988; 85: 3184-3188
• 28 Lumsden AB, Kelly AB, Schneider PA. et al. Lasting safe interruption of endarterectomy thrombosis by transiently infused antithrombin peptide D-Phe-Pro-argCH2C 1 in baboons. Blood 1993; 81: 7
• 29 Bagdy D, Barabas E, Szabo G. et al. In vivo anticoagulant and antiplatelet effect of D-Phe-Pro-Arg-H and D-MePhe-Pro-Arg-H. Thromb Haemost 1992; 67: 357
• 30 Markwardt F. Pharmacological approaches to thrombin regulation. Ann N Y Acad Sci 1986; 485: 204
• 31 Waxman L, Smith DE, Arcuri KE, Vlasuk GP. Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa. Science 1990; 248: 593-596
• 32 Neeper MP, Waxman L, Smith DE, Schulman CA, Sardina M, Ellis RW, Schaffer LW, Siegl PK S, Vlasuk GP. Characterization of recombinant tick anticoagulant peptide. J Biol Chem 1990; 265: 17746-17752
• 33 Dunwiddie CT, Thornberry N, Bull H, Sardana M, Friedman P, Jacobs J, Simpson E. Antistasin, a leech-derived inhibitor of factor Xa: Kinetic analysis of enzyme inhibition and identification of the reactive site. J Biol Chem 1989; 264: 16694-16699
• 34 Nutt EM, Gasic T, Rodkey J, Gasic G, Jacobs J, Friedman P, Simpson E. The amino acid sequence of antistasin. J Biol Chem 1988; 263: 10162-10167
• 35 Nutt EM, Jain D, Lenny A, Schaffer L, Siegl P, Dunwiddie CT. Purification and characterization of recombinant antistasin: A leech-derived inhibitor of coagulation factor Xa. Arch Biochem Biophy 1991; 285: 37-44
• 36 Tuszynski G, Gasic T, Gasic G. Isolation and characterization of antistasin. J Biol Chem 1987; 262: 9718-9723
• 37 Dunwiddie CT, Nutt EM, Vlasuk GP, Siegel PK S, Schaffer LW. Anticoagulant efficacy and immunogenicity of the selective factor Xa inhibitor antistasin following subcutaneous administration in the Rhesus monkey. Thromb Haemost 1992; 67: 371-376
• 38 Vlasuk GP, Ramjit D, Fijita T, Dunwiddie CT, Nutt EM, Smith DE, Shebuski RJ. Comparison of the in vivo anticoagulant properties of standard heparin and the highly selective factor Xa inhibitors antistasin and tick anticoagulant peptide (TAP) in a rabbit model of venous thrombosis. Thromb Haemost 1991; 65: 257-262
• 39 Esmon CT. The roles of protein C and thrombomodulin in the regulation of blood coagulation. J Biol Chem 1989; 264: 4723
• 40 Gruber A, Griffin JH, Harker LA, Hanson SR. Inhibition of platelet dependent thrombus formation by human activated protein C in a primate model. Blood 1989; 73: 639-642
• 41 Gruber A, Hanson SR, Kelly AB, Yan BS, Bang N, Griffin JH, Harker LA. Inhibition of thrombus formation by activated recombinant protein C in a primate model of arterial thrombosis. Circulation 1990; 82: 578-585
• 42 Gruber A, Harker LA, Hanson SR, Kelly AB, Griffin JH. Anti-thrombotic effects of combining activated protein C and urokinase in nonhuman primates. Circulation 1991; 84: 2454-2464
• 43 Hanson SR, Kelly AB, Gruber A. et al. Antithrombotic efficacy and hemostatic safety of activated protein C in vivo. Advances Appl Biotech 1990; 11: 187
• 44 Grinnell BW, Berg DT, Walls J, Yan SB. Trans-activated expression of fully gamma-carboxylated recombinant human protein C, an antithrombotic factor. Biotech 1987; 5: 1189-1192
• 45 Wu Q, Sheehan JP, Tsiang M. et al. Single amino acid substitutions dissociate fibrinogen-clotting and thrombomodulin-binding activities of human thrombin. Proc Nati Acad Sci USA 1991; 88: 6775
• 46 Weiss HJ, Turitto VT, Baumgartner HR, Nemerson Y, Hoffman T. Evidence for the presence of tissue factor activity on subendothelium. Blood 1989; 73: 968-975
• 47 Wilcox JN, Smith KM, Schwartz SM, Gordon D. Localization of tissue factor in the normal vessel wall and in the atherosclerotic plaque. Proc Natl Acad Sci USA 1989; 86: 2839-2843
• 48 Zeldis SM, Nemerson Y, Pitlick FA, Lentz TL. Tissue factor (thromboplastin): Localization to plasma membranes by peroxidase-conjugated antibodies. Science 1972; 175: 766-768
• 49 Broze GJ, Warren LA, Novotny WF, Higuchi DA, Girard JJ, Miletich JP. The lipoprotein-associated coagulation inhibitor that inhibits the factor Vll-tissue factor complex also inhibits factor Xa: Insight into its possible mechanism of action. Blood 1988; 71: 335-343
• 50 Rapaport SI. Inhibition of factor Vila/tissue factor-induced blood coagulation: With particular emphasis upon a factor Xa-dependent inhibitory mechanism. Blood 1989; 73: 359-365
• 51 Haskel EJ, Torr SR, Day KC, Palmier MO, Wun T-C, Sobel BE, Abendschein DR. Prevention of arterial reocclusion after thrombolysis with recombinant lipoprotein-associated coagulation inhibitor. Circulation 1991; 84: 821-827
• 52 Cannon CP, McCabe CH, Henry TD, Rogers WJ, Schweiger M, Gibson RS, Anderson JL, Williams DO. Braunwald E for the TIMI 5 investigators: A pilot trial of recombinant desulfatohirudin compared with heparin in conjunction with tissue-type plasminogen activator and aspirin for acute myocardial infarction: results of the thrombolysis in myocardial infarction (TIMI) 5 trial. JACC 1994; 23: 993-1003
• 53 The global use of strategies to open occluded coronary arteries (GUSTO) Ha investigators: Randomized trial of intravenous heparin versus recombinant Hirudin for acute coronary syndromes. Circulation 1994; 90: 1631-1637
• 54 Antman EM for the TIMI 9A investigators: Hirudin in acute myocardial infarction: a safety report from the thrombolysis and thrombin inhibition of in myocardial infarction (TIMI) 9A trial. Circulation 1994; 90: 1624-1630
• 55 Neuhaus KL, Essen Rv, Tebbe U, Jessel A, Heinrichs H. et al. Safety observations from the pilot phase of the randomized r-Hirudin for improvement of thrombolysis (HIT-HI) Study. Circulation 1994; 90: 1638-1642
• 56 Lidon RM, Theroux P, Lesperance J. et al. A pilot angiographic patency study using a direct thrombin inhibitor as adjunctive therapy to streptokinase in acute myocardial infarction. Circulation 1994; 89: 1567-1572
• 57 Topol AJ, Fuster V. et al. Recombinant hirudin for unstable angina: A multicenter, randomized angiographic trial subtitle. Circulation 1994; 89: 1-10
• 58 Gold HK, Torres FW, Garabedian HD, Werner W, Jang IK, Khan A, Hagstrom JN, Yasuda T, Leinbach RC, Newwell JB, Bovill EG, Stump DC, Collen D. Evidence for a rebound coagulation phenomenon after cessation of a 4-hour infusion of a specific thrombin inhibitor in patients with unstable angina pectoris. J Am Coll Cardiol 1993; 21: 1039-1047
• 59 Lidon RM, Theroux P, Juneau M, Adelman B, Maraganore J. Initial experience with a direct antithrombin, hirulog, in unstable angina: anticoagulant antithrombotic and clinical effects. Circulation 1993; 88: 1495-1501
• 60 Fuchs J, McCabe CH, Antman EM, Borzak S, Palisaitis D, Herson S. et al. Hirulog in the treatment of unstable angina: Results of the TIMI 7 trial. Circulation. 1995 in press
• 61 Topol EJ, Bonan R, Jewitt D, Sigwart U, Kakkar VV, Rothman M. et al. Use of a direct antithrombin, hirulog, in place of heparin during coronary angioplasty. Circulation 1993; 87: 1622-1629
• 62 Eriksson BI, Kalebo P, Ekman S, Kerry R, Baur M, Bach D, Close P. Effective prevention of thromboembolic complications after total hip replacement with three different doses of recombinant hirudin, CGP 39393 (Revas-®), Ciba, compared to unfractionated heparin. Circulation 1994; 94: #3066
• 63 Ginsberg J, Nurmohamed MT, Gent M, MacKinnon B, Sicurella J, Brill-Edwards P, Levine MN, Panju AA, Powers P, Stevens P, Turpie AG G. et al Use of hirulog in the prevention of venous thrombosis after major hip or knee surgery. Circulation 1994; 90: 2385-2389