Direct thrombin inhibitors for treatment of arterial thrombosis: Potential differences between bivalirudin and hirudin

American Journal of Cardiology

Volumn 82, Issue 8 SUPPL. 1, 1998, Pages 12P-18P

  Bates, Shannon M ^a   Weitz, Jeffrey I ^a,b  

^a MCMASTER UNIVERSITY   (Canada)

^b HAMILTON HEALTH SCIENCES   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

FIBRIN; FIBRINOGEN RECEPTOR ANTAGONIST; HEPARIN; HIRUDIN; HIRULOG; PROTEIN C; THROMBIN; THROMBIN INHIBITOR; THROMBOCYTE FACTOR 4; THROMBOMODULIN;

ANTICOAGULATION; ARTERY THROMBOSIS; CONFERENCE PAPER; DRUG EFFICACY; DRUG SAFETY; HUMAN; HUMAN CELL; HUMAN TISSUE; PREDICTION; PRIORITY JOURNAL; RISK BENEFIT ANALYSIS; THROMBOGENESIS; THROMBOSIS PREVENTION;

ACUTE DISEASE; ANTITHROMBINS; CORONARY THROMBOSIS; DRUG MONITORING; FIBRINOLYTIC AGENTS; HEPARIN; HIRUDIN THERAPY; HIRUDINS; HUMANS; PEPTIDE FRAGMENTS; PROTEIN C; RECOMBINANT PROTEINS;

EID: 0031729548     PISSN: 00029149     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0002-9149(98)00660-2     Document Type: Article

References (64)

1. Fuster V, Badimon L, Badimon JJ, Chesebro JH. The pathogenesis of coronary artery disease and the acute coronary syndromes. I. N Engl J Med 1992;326:242-250.
2. Fuster V, Badimon L, Badimon JJ, Chesebro JH. The pathogenesis of coronary artery disease and the acute coronary syndromes. II. N Engl J Med 1992;326:310-318.
3. Falk E, Shah PK, Fuster V. Coronary plaque disruption. Circulation 1995;92:657-671.
4. Furie B, Furie BC. Molecular and cellular biology of blood coagulation. N Engl J Med 1992;326:800-806.
5. 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 III-independent inhibitors. J Clin Invest 1990;86:385-391.
6. Kumar R, Béguin S, Hemker C. The effect of fibrin clots and clot-bound thrombin on the development of platelet procoagulant activity. Thromb Haemost 1995;74:962-968.
7. Kumar R, Béguin S, Hemker HC. The influence of fibrinogen and fibrin on thrombin generation evidence for feedback activation of the clotting system by clot bound thrombin. Thromb Haemost 1994;72:713-721.
8. Bajzar L, Manuel R, Nesheim ME. Purification and characterization of TAFI, a thrombin-activable fibrinolysis inhibitor. J Biol Chem 1995;270:14477-14784.
9. Sakharov DV, Plow EF, Rijken DC. On the mechanism of the antifibrinolytic activity of plasma carboxypeptidase B. J Biol Chem 1997;272:14477-14482.
10. Ewald GA, Eisenberg PR. Plasmin-mediated activation of contact system in response to pharmacological thrombolysis. Circulation 1995;91:28-36.
11. Lee CD, Mann KG. Activation/inactivation of human factor V by plasmin. Blood 1989;73:185-190.
12. Eisenberg PR, Miletich JP, Sobel BE, Jaffe AS. Differential effects of activation of prothrombin by streptokinase compared with urokinase and tissue-type plasminogen activator (t-PA). Thromb Res 1988;50:707-717.
13. Seitz R, Pelzer H, Immel A, Egbring R. Prothrombin activation by thrombolytic agents. Fibrinolysis 1993;7:109-115.
14. Mirshahi M, Soria J, Soria C, Faivre F, Lu H, Courtney M, Roitsch C, Tripier D, Caen JP. Evaluation of the inhibition by heparin and hirudin of coagulation activation during rt-PA-induced thrombolysis. Blood 1989;74:1025-1030.
15. Weitz JI, Leslie B, Hudoba M. Thrombin binds to soluble fibrin degradation products where it is protected from inhibition by heparin-antithrombin but susceptible to inactivation by antithrombin-independent inhibitors. Circulation 1998;97:544-552.
16. Fuster V, Badimon J, Chesebro JH, Fallon JT. Plaque rupture, thrombosis, and therapeutic implications. Haemostasis 1996;26(suppl 4):269-284.
17. Hirsh J. Heparin. N Engl J Med 1991;324:1565-1574.
18. Weitz JI. Low-molecular-weight heparins. N Engl J Med 1997;337:688-698.
19. Hogg PJ, Jackson CM. Fibrin monomer protects thrombin from inactivation by heparin-antithrombin III: implications for heparin efficacy. Proc Natl Acad Sci USA 1989;86:3619-3623.
20. Teitel JM, Rosenberg RD. Protection of factor Xa from neutralization by the heparin-antithrombin complex. J Clin Invest 1983;71:1383-1391.
21. Pieters J, Willems G, Hemker HC, Lindhout T. Inhibition of factor IXa and factor Xa by antithrombin III/heparin during factor X activation. J Biol Chem 1988;263:15313-15318.
22. Wilner GD, Danitz MP, Mudd MS, Hsieh KH, Fenton JW II. Selective immobilization of α-thrombin by surface-bound fibrin. J Lab Clin Med 1981;97:403-411.
23. Berliner LJ, Sugawara Y, Fenton JW II. Human α-thrombin binding to nonpolymerized fibrin-Sepharose: evidence for an anionic binding region. Biochemistry 1985;27:7005-7009.
24. Kaminski M, McDonagh J. Inhibited thrombins. Interactions with fibrinogen and fibrin. Biochem J 1987;242:881-887.
25. Hogg PJ, Bock PE. Modulation of thrombin and heparin activities by fibrin. Thromb Haemost 1997;77:424-433.
26. Hogg PJ, Jackson CM. Formation of a ternary complex between thrombin, fibrin monomer, and heparin influences the action of thrombin on its substrates. J Biol Chem 1990;265:248-255.
27. Hogg PJ Jackson CM, Labanowski JK, Bock PE. Binding of fibrin monomer and heparin to thrombin in a ternary complex alters the environment of the thrombin catalytic site, reduces affinity for hirudin, and inhibits cleavage of fibrinogen. J Biol Chem 1996;271:26088-26095.
28. Lane DA. Heparin binding and neutralizing proteins. In: Lane DA, Lindahl U, eds. Heparin: Chemical and Biological Properties and Clinical Applications. Boca Raton, FL: CRC Press, 1989:363-391.
29. de Romeuf C, Mazurier C. Heparin binding assay of von Willebrand factor (vWF) in plasma milieu: evidence of the importance of the multimerization degree of vWF. Thromb Haemost 1993;69:436-440.
30. Young E, Prins M, Levine MN, Hirsh J. Heparin binding to plasma proteins, an important mechanism for heparin resistance. Thromb Haemost 1992;67:639-643.
31. Young E, Wells P, Holloway S, Weitz J, Hirsh J. Ex-vivo and in-vitro evidence that low molecular weight heparins exhibit less binding to plasma proteins than unfractionated heparin. Thromb Haemost 1994;71:300-304.
32. Young E, Cosmi B, Weitz J, Hirsh J. Comparison of the non-specific binding of unfractionated heparin and low molecular weight heparin (Enoxaparin) to plasma proteins. Thromb Haemost 1993;70:625-630.
33. Stubbs MT, Bode W. A player of many parts: the spotlight falls on thrombin's structure. Thromb Res 1993;69:1-58.
34. Markwardt F. Past, present, and future of hirudin. Haemostasis 1991;21(suppl 1):11-26.
35. Rydel TJ, Ravichandran KG, Tulinsky A, Bode W, Huber R, Roitsch C, Fenton JW II. The structure of a complex of recombinant hirudin and human α-thrombin. Science 1990;249:277-280.
36. Maraganore JM, Bourdon P, Jablonski J, Ramachandran KL, Fenton JW II. Design and characterization of hirulogs: a novel class of bivalent peptide inhibitors of thrombin. Biochemistry 1990;29:7095-7101.
37. Skrzypczak-Jankun E, Carperos VE, Ravichandran KG, Tulinsky A, Westbrook M, Maraganore JM. Structure of the hirugen and hirulog 1 complexes of α-thrombin. J Mol Biol 1991;221:1379-1393.
38. Witting JI, Bourdon P, Brezniak DV, Maraganore JM, Fenton JW. Thrombin-specific inhibition by and slow cleavage of hirulog-1. Biochem J 1992;283:737-743.
39. Parry MA, Maraganore JM, Stone SR. Kinetic mechanism for the interaction of Hirulog with thrombin. Biochemistry 1994;33:14807-14814.
40. Lyle TA. Small-molecule inhibitors of thrombin. Perspect Drug Discov Design 1993;1:453-460.
41. Tapparelli G, Metternich R, Ehrhardt C, Cook NS. Synthetic low-molecular weight thrombin inhibitors: molecular design and pharmacological profile. Trends Pharmacol Sci 1993;14:366-376.
42. Das J, Kimball SD. Thrombin active site inhibitors. Bioorg Med Chem 1995;3:999-1007.
43. Kikumoto R, Tamao Y, Tezuka T, Tonomura S, Hara H, Ninomiya K, Hijikata A, Okamoto S. Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N2-[(3-methyl-1,2,3,4-tetrahydro-8-quinolinyl)sulfonyl]-1- arginyl)]-2-piperidinecarboxylic acid. Biochemistry 1984;23:85-90.
44. Hilpert K, Ackermann J, Banner DW, Gast A, Gubernator K, Hadváry P, Labler L, Müller K, Schmid G, Tschopp TB. Design and synthesis of potent and highly selective thrombin inhibitors. J Med Chem 1994;37:3889-3901.
45. Teger Nilsson AC, Bylund R, Gutsafsson D, Gyzander E, Eriksson U. In vitro effects of inogatran, a selective low molecular weight thrombin inhibitor. Thromb Res 1997;85:133-145.
46. Gustafsson D, Antonsson T, Bylund R, Eriksson U, Gyzander E, Nilsson I, Elg M, Mattsson C, Deinum J, Pehrsson S, Karlsson O, Nilsson A, Sörensen H. Effect of melagatran, a new low-molecular-weight thrombin inhibitor, on thrombin and fibrinolytic enzymes. Thromb Haemost 1998;79:110-118.
47. Mehdi S. Synthetic and naturally occurring protease inhibitors containing an electrophilic carbonyl group. Bioorg Chem 1993;21:249-259.
48. Shuman RT, Rothenberger RB, Campbell CS, Smith GF, Gifford-Moore DS, Gesellchen PD. Highly selective tripeptide thrombin inhibitors. J Med Chem 1993;36:314-319.
49. Kettner C, Mersinger L, Knabb R. The selective inhibition of thrombin by peptides of boroarginine. J Biol Chem 1990;265:18289-18297.
50. Marbet GA, Verstraete M, Kienast J, Graf P, Hoet B, Tsakiris DA, Silling-Engelhardt G, Close P. Clinical pharmacology of intravenously administered recombinant desulfatohirudin (CGP 39393) in healthy volunteers. J Cardiovasc Pharmacol 1993;22:364-372.
51. Fox I, Dawson A, Loynds P, Eisner J, Findlen K, Levin E, Hanson D, Mant T, Wagner J, Maraganore J. Anticoagulant activity of Hirulog, a direct thrombin inhibitor, in humans. Thromb Haemost 1993;69:157-163.
52. Antman EM, for the TIMI 9A Investigators. Hirudin in acute myocardial infarction. Safety report from the Thrombolysis and Thrombin Inhibition in Myocardial Infarction (TIMI) 9A Trial. Circulation 1994;90:1624-1630.
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. Neuhause KL, von Essen R, Tebbe U, Jessel A, Heinrichs H, Mäurer W, Döring W, Harmjanz D, Kötter V, Kalhammer E, Simon H, Horacek T. Safety observations from the pilot phase of the randomized r-Hirudin for Improvement of Thrombolysis (HIT-III) study. A study of the Arbeitsgemeinschaft Leitender Kardiologischer Krankenausärzte (ALKK). Circulation 1994;90:1638-1642.
55. Bittl JA, Strony J, Brinker JA, Ahmed WH, Meckel CR, Chaitman BR, Maraganore J, Deutsch E, Adelman B, for the Hirulog Angioplasty Study Investigators. Treatment with bivalirudin (Hirulog) as compared with heparin during coronary angioplasty for unstable or postinfarction angina. N Engl J Med 1995;333:764-769.
56. Bittl JA. Comparative safety profiles of hirulog and heparin in patients undergoing coronary angioplasty. The Hirulog Angioplasty Study Investigators. Am Heart J 1995;130:658-665.
57. White HD, Aylward PE, Frey MJ, Adgey AA, Nair R, Hillis WS, Shalev Y, Brown MA, French JK, Collins R, Maraganore J, Adelman B, for the Hirulog Early Reperfusion/Occlusion (HERO) Trial Investigators. Randomized, double-blind comparison of hirulog versus heparin in patients receiving streptokinase and aspirin for acute myocardial infarction (HERO). Circulation 1997;96:2155-2161.
58. Esmon CT. Molecular events that control the protein C anticoagulant pathway. Thromb Haemost 1993;70:29-35.
59. Topol EJ. Toward a new frontier in myocardial reperfusion therapy. Emerging platelet preeminence. Circulation 1998;97:211-218.
60. The Platelet Receptor Inhibition in Ischemic Syndrome Management in Patients Limited by Unstable Signs and Symptoms (PRISM-PLUS) Study Investigators. Inhibition of the platelet glycoprotein IIb/IIIa receptor with tirofiban in unstable angina and non-Q-wave myocardial infarction. N Engl J Med 1998;338:1488-1497.
61. The Global Use of Strategies to Open Occluded Coronary Arteries (GUSTO) IIb Investigators. A comparison of recombinant hirudin with heparin for the treatment of acute coronary syndromes. N Engl J Med 1996;335:775-782.
62. Antman EM. Hirudin in acute myocardial infarction. Thrombolysis and Thrombin Inhibition in Myocardial Infarction (TIMI) 9B trial. Circulation 1996;94:911-921.
63. Serruys PW, Herrman JP, Simon P, Rutsch W, Bode C, Laarman GJ, van Dijk R, van den Bos AA, Umans VA, Fox KA, Close P, Deckers JW, for the HELVETICA Investigators. A comparison of hirudin with heparin in the prevention of restenosis after coronary angioplasty. N Engl J Med 1995;333:757-763.
64. Eriksson BI, Ekman S, Kalebo P, Zachrisson B, Bach D, Close P. Prevention of deep-vein thrombosis after total hip replacement: direct thrombin inhibition with recombinant hirudin, CGP 39393. Lancet 1996;347:635-639.