Inhibition of thrombin generation in plasma by inhibitors of factor Xa

Thrombosis and Haemostasis

Volumn 78, Issue 4, 1997, Pages 1215-1220

  Prasa, D ^a   Svendsen, L ^b   Sturzebecher J ^a  

^a FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

^b Pentapharm Ltd   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING INHIBITOR; HIRUDIN; LEPIRUDIN; NAPSAGATRAN; RECOMBINANT TICK ANTICOAGULANT PEPTIDE; THROMBIN; THROMBIN INHIBITOR;

ARTICLE; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG SPECIFICITY; HUMAN; MOLECULAR WEIGHT; PRIORITY JOURNAL; THROMBIN TIME;

EID: 0030667455     PISSN: 03406245     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0038-1657717     Document Type: Article

References (38)

1. Tuszynski GP, Gasic TB, Gasic GJ. Isolation and characterization of antistasin. An inhibitor of metastasis and coagulation. J Biol Chem 1987; 262: 9718-23.
2. Waxman L, Smith DE, Arcuri KE, Vlasuk GP. Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa. Science 1990; 248: 593-6.
3. Neeper MP, Waxman L, Smith DE, Schulman CA, Sardana M, Ellis RW, Schaffer LW, Siegl PKS, Vlasuk GP. Characterization of recombinant tick anticoagulant peptide. A highly selective inhibitor of blood coagulation factor Xa. J Biol Chem 1990; 265: 17746-52.
4. Jordan SP, Waxman L, Smith DE, Vlasuk GP. Tick anticoagulant peptide: kinetic analysis of the recombinant inhibitor with blood coagulation factor Xa. Biochemistry 1990; 29: 11095-100.
5. Vlasuk GP. Structural and functional characterization of tick anticoagulant peptide (TAP): a potent and selective inhibitor of blood coagulation factor Xa. Thromb Haemost 1993; 70: 212-6.
6. Vlasuk GP, Ramjit D, Fujita 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: 257-62.
7. Schaffer LW, Davidson JT, Vlasuk GP, Siegl PKS. Antithrombotic efficacy of recombinant tick anticoagulant peptide: a potent inhibitor of coagulation factor X in a primate model of arterial thrombosis. Circulation 1991; 84: 1741-8.
8. 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 a canine model of acute coronary artery thrombosis. Circulation 1992; 85: 805-15.
9. Stürzebecher J, Stürzebecher U, Vieweg H, Wagner G, Hauptmann J, Markwardt F. Synthetic inhibitors of bovine factor Xa and thrombin - comparison of their anticoagulant efficiency. Thromb Res 1989; 54: 245-52.
10. Tidwell RR, Webster WP, Shaver SR, Geratz JP. Strategies for anticoagulation with synthetic protease inhibitors. Xa inhibitors versus thrombin inhibitors. Thromb Res 1980; 19: 339-49.
11. Hara T, Yokoyama A, Ishihara H, Yokoyama Y, Nagahara T, Iwamoto M. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb Haemost 1994; 71: 314-9.
12. Yamaguchi H, Yamada K, Kanetani N, Yokoyama Y, 1993, Patent P 05078344.
13. Stürzebecher J, Stürzebecher U. Are factor Xa inhibitors superior to thrombin inhibitors in anticoagulation? Folia Haematol, Leipzig 1988; 115: 152-6.
14. Hauptmann J, Kaiser B, Nowak G, Stürzebecher J, Markwardt F. Comparison of the anticoagulant and antithrombotic effects of synthetic thrombin and factor Xa inhibitors. Thromb Haemost 1990; 63: 220-3.
15. Hauptmann J, Kaiser B. Anticoagulant potential of synthetic and recombinant inhibitors of factor Xa and thrombin in vitro. Blood Coag Fibrinol 1993; 4: 577-82.
16. Hemker HC, Wielders S, Kessels H, Béguin S. Continuous registration of thrombin generation in plasma, its use for the determination of the thrombin potential. Thromb Haemost 1993; 70: 617-24.
17. Prasa D, Svendsen L, Stürzebecher J. The ability of thrombin inhibitors to reduce the thrombin activity generated in plasma on extrinsic and intrinsic activation. Thromb Haemost 1997; 77: 498-503,
18. Walsmann P. Über die Reinigung von Thrombinpräparaten. Pharmazie 1968; 23: 401-2.
19. Vieweg H, Wagner G. Synthese von Nα-(Arylsulfonylglycyl)-3-amidinophenylalaninestern als aktive und relativ spezifische Inhibitoren von Faktor Xa. Pharmazie 1987; 42: 267.
20. Stürzebecher J, Hauptmann J, Prasa D, Wikström P, Vieweg H. Synthesis and structure-activity relationships of potent thrombin inhibitors derived from piperazides of 3-amidinophenylalanine. J Med Chem 1997; in press.
21. Dixon M. The determination of enzyme inhibitor constants. Biochem J 1953; 55: 170-1.
22. Hemker HC, Béguin S. Thrombin generation in plasma: Its assessment via the endogenous thrombin potential. Thromb Haemost 1995; 74: 134-8.
23. Stone SR, Hofsteenge J. Kinetics of the inhibition of thrombin by hirudin. Biochemistry 1986; 25: 4622-8.
24. Hilpert K, Ackermann J, Banner DW, Gast A, Gubernator K, Schmid G, Tschopp TB, van de Waterbeemd H. The development of potent and highly selective thrombin inhibitors. Eur J Med Chem 1995; 30 Suppl: S132-8.
25. Béguin S, Lindhout T, Hemker HC. The mode of action of heparin in plasma. Thromb Haemost 1988; 60: 457-62.
26. Lindhout T, Blezer R, Hemker HC. The anticoagulant mechanism of action of recombinant hirudin (CGP 39393) in plasma. Thromb Haemost 1990; 64: 464-8.
27. Hemker HC, Béguin S. Mode of action of heparin and related drugs. Semin Thromb Hemost 1991; Suppl 1: 29-34.
28. Béguin S, Wielders S, Lormeau J-C, Hemker HC. The mode of action of CY216 and CY222 in plasma. Thromb Haemost 1992; 67: 33-41.
29. Lormeau J-C, Herault JP. Comparative inhibition of extrinsic and intrinsic thrombin generation by standard heparin, low molecular weight heparin and the synthetic AT III-binding pentasaccharide. Thromb Haemost 1993; 69: 152-6.
30. Kessels H, Béguin S, Andree H, Hemker HC. Measurement of thrombin generation in whole blood - the effect of heparin and aspirin. Thromb Haemost 1994; 72: 78-83.
31. Verhallen PFJ, Gehrmann G, Prasa D, Stürzebecher J. Measurement of thrombin generation in human plasma by two different methods (subsample/continuous): characterization of different anticoagulants. Thromb Haemost 1995; 73: 1247.
32. Gast A, Tschopp TB. Inhibition of extrinsic and intrinsic thrombin generation by a novel synthetic thrombin inhibitor (Ro 46-6240), recombinant hirudin and heparin in human plasma. Blood Coag Fibrinol 1995; 6: 553-60.
33. Hauptmann J, Markwardt F, Walsmann P. Synthetic inhibitors of serine proteinases. XVI. Influence of 3-and 4-amidinobenzyl derivatives on the formation and action of thrombin. Thromb Res 1978; 12: 735-44.
34. Yokoyama T, Kelly AB, Marzec UM, Hanson SR, Kunitada S, Harker LA. Antithrombotic effects of orally active synthetic antagonist of activated factor X in nonhuman primates. Circulation 1995; 92: 485-91.
35. Herbert JM, Bernat A, Dol F, Hérault JP, Crépon B, Lormeau JC. DX 9065a, a novel, synthetic, selective and orally active inhibitor of factor Xa: In vitro and in vivo studies. J Pharmacol Exp Ther 1996; 276: 1030-8.
36. Lynch Jr JJ, Sitko GR, Mellot MJ, Nutt EM, Lehinas ED, Friedman PA, Dunwiddie CT, Vlasuk GP. Maintenance of canine coronary artery patency following thrombolysis with front-loaded plus low dose maintenance conjunctive therapy: a comparison of factor Xa versus thrombin inhibition. J Cardiovasc Res 1994; 28: 78-85.
37. Pieters J, Lindhout T. The limited importance of factor Xa inhibition to the anticoagulant property of heparin in thromboplastin-activated plasma. Blood 1988; 72: 2048-52.
38. Krishnaswamy S, Vlasuk GP, Bergum PW. Assembly of the prothrombinase complex enhances the inhibition of bovine factor Xa by tick anticoagulant peptide. Biochemistry 1994; 33: 7897-907.