Modulating Platelet Function With Selective Thrombin Inhibitors?

Pathophysiology of Haemostasis and Thrombosis

Volumn 26, Issue , 1996, Pages 70-77

  Verstraete, M ^a  

^a UNIVERSITY OF LEUVEN   (Belgium)

Author keywords

Argatroban; DuP714; Efegatran; Hirudin; Hirudisins; Hirulog; Inogatran; Napsagatran

Indexed keywords

ACETYL DEXTRO PHENYLALANYLPROLYLBOROARGININE; ARGATROBAN; EFEGATRAN; HIRUDIN; HIRUDIN DERIVATIVE; HIRULOG; INOGATRAN; NAPSAGATRAN; THROMBIN INHIBITOR;

CONFERENCE PAPER; HUMAN; PRIORITY JOURNAL; THROMBOCYTE FUNCTION;

ADMINISTRATION, ORAL; ADULT; ANIMALS; ANTITHROMBINS; BLOOD PLATELETS; BORON COMPOUNDS; CLINICAL TRIALS; DOGS; DRUG EVALUATION, PRECLINICAL; GLYCINE; HIRUDIN THERAPY; HIRUDINS; HUMANS; NAPHTHALENES; OLIGOPEPTIDES; PEPTIDE FRAGMENTS; PIPECOLIC ACIDS; PIPERIDINES; RECOMBINANT PROTEINS; THROMBIN;

EID: 0029944889     PISSN: 14248832     EISSN: 14248840     Source Type: Journal    
DOI: 10.1159/000217287     Document Type: Article

References (28)

1. Hofsteenge J, Stone SR, Donella-Deane A, Pinna LA: The effect of substitutinphosphotyrosine for sulphotyrosine on the activity of hirudin. Eur J Biochem 1990; 188: 55-59.
2. Markwardt F, Nowak G, Stürzebecher J, Griessbach U, Walsmann P, Vogel G: Pharmacokinetics and anticoagulant effect of hirudin in man. Thromb Haemostas 1984: 52: 160-163.
3. Bichler J, Fichtl B, Siebeck M, Fritz H: Pharmacokinetics and pharmacodynamics of hirudin in man after single subcutaneous and intravenous bolus administration. Drug Res 1988: 38: 704-710.
4. Dahlbäck B, Stenflo J: A natural anticoagulant pathway. Biochemistry and physiology of proteins C, S, C4b-binding protein and thrombomodulin; in Bloom AL, Forbes CD, Thomas DP, Tuddenham EGD (eds): Haemostasis and Thrombosis, third edition. Churchill Livingstone, London, 1993. pp 671-698.
5. Talbot MD, Ambler J, Butler KD, Rindlay VS, Mitchell KA. Peters RF, Tweed MF, Wallis RB: Recombinant desulfatohirudin (CGP 39393) anticoagulant and antithrombotic properties in vivo. Thromb Haemostas 1991; 61: 77-80.
6. Marbel 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.
7. Verstraete M, Nurmohamed M, Kienast J, Siebeck M, Silling-Engelhardt G. Büllcr H, Hoet B, Bichler J, Close P: on behalf of the European Hirudin in Thrombosis Group. Biologic effets of recombinant hirudin (CGP 39393) in human volunteers. J Am Coll Cardiol 1993; 22: 1080-1088.
8. evasc) in immunocompetent volunteers. Coron Art Dis 1994; 5: 943-949.
9. Maraganore JM, Bourdon P, Jablonski J, Ramachandran KL, Fenton JWII: Design and Characterization of hirulogs: A novel class of bivalent peptide inhibitors of thrombin. Biochcm 1990; 29:7095-7101.
10. Skrzypczak-Jankun E. Carpcros VE, Ravichandran KG, Tulinsky A, Westbrook M, Maraganore JM: Structure of hirugen and hirulog 1 complexes of a-thrombin. J Mol Biol 1991; 221: 1379-1393.
11. 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 inhibitor of thrombin. Thromb Haemost 1993; 69, 157-163.
12. Cannon CP, Maraganore JM. Loscalzo J, McAllister A, Eddings K. George D, Selwyn AP. Adelman B, Fox I, Braunwald E, Ganz P: Anticoagulant effect of hirulog, a novel thrombin inhibitor, in patients with coronary artery disease. Am J Cardiol 1993; 71: 778-782.
13. Kikumoto R, Tamao Y, Tezuka T, Tonomura S, Hara S, Nimomiya K, Hijikata A, Okamoto S: Selective inhibition of thrombin by (2R,4R)-4-methyl-1-[N-(3-methyl-l,2,3.4-tetrahydro-8-quinolinyl)sulfonyl]-arginyl]-2-piperidinecarboxylic acid. Biochemistry 1984; 23: 85-90.
14. Imura Y, Stasscn J-M, Collen D: Comparative antithrombotic effects of heparin, recombinant hirudin, and argatroban in a hamster femoral vein platelet-rich mural thrombus model. J Pharmacol ExperTher 1992; 261: 895-898.
15. Jang I, Gold HK. Ziskind AA, Leinbach RC, Fallon JT, Collen D: Prevention of platelet-rich arterial thrombosis by selective thrombin inhibition. Circulation 1990; 81: 219-225.
16. Lunven C, Gauffeny C, Lecoffre C, O’Brien D, Roome NO, Berry CN. Inhibition by argatroban, a specific thrombin inhibitor, of platelet activation by fibrin clot-associated thrombin. Thromb Haemostas 1996; 75: 154-160.
17. Haskel EJ, Prager NA, Sobel BE, Abendschein DR: Relative efficacy of antithrombin compared with antiplatelet agents in accelerating coronary thrombolysis and prevention of rcocclu-sion. Circulation 1991; 83:1048-1056.
18. Zoldhelyi P, Fuster V, Chesebro JH: Antithrombins as conjunctive therapy in arterial thrombolysis. Coronary Artery Dis 1992; 3, 1003-1009.
19. Hilpert K, Ackermann J, Banner DW, Gast A, Gubernator K, Hadvary P. Labler L, Muller K, Schmid G, Tschopp TB, van dc Waterbeemd H: Design and synthesis of potent and highly selective thrombin inhibitors. J Med Chem 1994; 37: 3889-3901.
20. Roux S, Tschopp T. Baumgartner HR: Effects of napsagatran (Ro 46-6240), a new synthetic thrombin inhibitor and of heparin in a canine model of coronary artery thrombosis: comparison with an ex vivo annular perfusion chamber model. J Pharmacol Exper Therap 1996; 277; 71-78.
21. Murphy NP, Pratico D, Jennings L. Doyle C, Fitzgerald DJ: Thrombin-dependent activation of platelet glycoprotein Ilb/IIla during coronary thrombolysis in vivo. Circulation 1995; 92: 302 (Abstract).
22. Teger-Nilsson A-C, Eriksson U, Gustafsson D. Byfund R, Fager G. Held P: Phase 1 studies on inogatran, a new selective thrombin inhibitor. J Am Coll Cardiol 1995; 23: 117 (Abstract).
23. Simoons ML. van Mittenburg A, Scheffer MG, Werner H, Leenders CM. Remme WJ. Stoel I, de Milliano P, Stibbe J, Roberts E: Anticoagulant properties of efegatran, a direct thrombin inhibitor 1 in patients with unstable angina. Eur Heart J 1994; 15; 120 (Abstract).
24. Kettner C. Mersinger L, Knabb R: The selective inhibition of thrombin by peptides of boroar-ginine. J Biol Chem 1990; 265: 18289-18297.
25. Knapp A, Degenhardt T. Dodt J: Hirudisins; hirudin-derived thrombin inhibitors with disinte-grin activity. J Biol. Chem 1992; 267: 24230-24234.
26. Bode C. Hudelmayer M, Mehwald P. Bauer S. Freitag M. von Hodenberg E, Newell JB, Kübler W, Haber E, Runge MS: Fibrin-targeted recombinant hirudin inhibits Fibrin depostion on experimental clots more efficiently than recombinant hirudin. Circulation 1994; 90: 1956-1963.
27. Hung DT, Vu TK, Wheaton VI, Charo IF, Nelken NA, Esmon N, Esmon CT. Coughlin SR: “Mirror image” antagonism of thrombin-induced platelet activation based on thrombin receptor structure. J Clin Invest 1992; 89, 444-450.
28. Bode C, Nordt TK, Runge MS: Thrombolytic treatment in acute myocardial infarction-selected recent developments. Ann Hematol 1994; 69, 35-40.