Factor Xa versus factor IIa inhibitors

Clinical and Applied Thrombosis/Hemostasis

Volumn 3, Issue 1, 1997, Pages 16-24

  Kaiser, Brigitte ^a  

^a FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

Author keywords

Anticoagulants; Antithrombotics; Factor Xa inhibitors; Thrombin inhibitors

Indexed keywords

2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; ACETYL DEXTRO PHENYLALANYLPROLYLBOROARGININE; ANTICOAGULANT AGENT; ANTISTASIN; ARGATROBAN; ARGININE DERIVATIVE; BENZAMIDINE DERIVATIVE; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; BOROARGININE DERIVATIVE; EFEGATRAN; GABEXATE MESILATE; HIRUDIN; HIRULOG; NAFAMSTAT; PROTHROMBIN A; SDZ 217766; THROMBIN INHIBITOR; UNCLASSIFIED DRUG; YAGIN;

ANTICOAGULATION; BLOOD CLOTTING; DISSEMINATED INTRAVASCULAR CLOTTING; DRUG MECHANISM; ENZYME ACTIVE SITE; HEMOSTASIS; HUMAN; PRIORITY JOURNAL; REVIEW; THROMBOEMBOLISM;

EID: 0031412416     PISSN: 10760296     EISSN: None     Source Type: Journal    
DOI: 10.1177/107602969700300102     Document Type: Review

References (63)

1. Bush LR. Argatroban, a selective, potent thrombin inhibitor. Cardiovasc Drug Rev 1991;9:247.
2. Callas D, Fareed J. Comparative pharmacology of site directed antithrombin agents. Implication in drug development. Thromb Haemost 1995;74:473.
3. Harker LA. Strategies for inhibiting the effects of thrombin. Blood Coag Fibrinol 1994;5:47.
4. Hauptmann J, Markwardt F. Pharmacologic aspects of the development of selective synthetic thrombin inhibitors as anticoagulants. Semin Thromb Hemost 1992;18:200.
5. Johnson PH. Hirudin - clinical potential of a thrombin inhibitor. Annu Rev Med 1994;45:165.
6. Kaiser B. Anticoagulant and antithrombotic actions of recombinant hirudin. Semin Thromb Hemost 1991;2:130.
7. Kaiser B, Hauptmann J. Pharmacology of synthetic thrombin inhibitors of the tripeptide type. Cardiovasc Drug Rev 1992;10:71.
8. Markwardt F. Prospective clinical use of hirudin as an anticoagulant. Biomed Prog 1990;2:19.
9. Tapparelli C, Metternich R, Ehrhardt C, et al. Synthetic low molecular weight thrombin inhibitors: molecular design and pharmacological profile. Trends Pharmacol Sci 1993;14:366.
10. Kaiser B, Hauptmann J. Factor Xa inhibitors as novel antithrombotic agents. Facts and perspectives. Cardiovasc Drug Rev 1994;12:225.
11. Ripka W, Brunck T, Stanssens P, et al. Strategies in the design of inhibitors of serine proteases of the coagulation cascade-factor Xa. Eur J Med Chem 1995;30(Suppl):88s.
12. Hauptmann J, Kaiser B, Nowak G, et al. Comparison of the anticoagulant and antithrombotic effects of synthetic thrombin and factor Xa inhibitors. Thromb Haemost 1990;63:220.
13. Stürzebecher J, Stürzebecher U, Vieweg H, et al. Synthetic inhibitors of bovine factor Xa and thrombin. Comparison of their anticoagulant efficiency. Thromb Res 1989;54:245.
14. Tuszynski GP, Gasic TB, Gasic GJ. Isolation and characterization of antistasin. An inhibitor of metastasis and coagulation. J Biol Chem 1987;262:9718.
15. Waxman L, Smith DE, Arcuri KE, et al. Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa. Science 1990;248:593.
16. Rigbi M, Jackson CM, Atamna H, et al. FXa inhibitor from the saliva of the leech Hirudo medicinalis. Thromb Haemost 1995;73:1306.
17. Katakura S, Nagakara T, Hara T, et al. A novel factor Xa inhibitor: structure-activity relationships and selectivity between factor Xa and thrombin. Biochem Biophys Res Commun 1993;197:965.
18. Katakura S, Nagakara T, Hara T, et al. Molecular model of an interaction between factor Xa and DX-9065a, a novel factor Xa inhibitor: contribution of the acetimidoylpyrrolidine moiety of the inhibitor to potency and selectivity for serine proteases. Eur J Med Chem 1995;30:387.
19. Nagahara T, Katakura S, Yokoyama Y, et al. Design, synthesis and biological activities of orally active coagulation factor Xa inhibitors. Eur J Med Chem 1995;30(Suppl):140s.
20. Markwardt F. Pharmacology of hirudin: one hundred years after the first report of the anticoagulant agent in medicinal leeches. Biomed Biochim Acta 1985;44:1007.
21. Talbot MD, Butler KD. Potential clinical uses of thrombin inhibitors. Drugs News Perspect 1990;3:357.
22. Powers JC, Kam CM. Synthetic substrates and inhibitors of thrombin. In: Berliner LJ, ed. Thrombin: structure and function. New York: Plenum Press, 1992:117.
23. Maraganore JM, Bourdon P, Jablonski J, et al. Design and characterization of hirulogs: A novel class of bivalent peptide inhibitors of thrombin. Biochemistry 1990;29:7095.
24. Dunwiddie CT, Thornberry NA, Bull HG, et al. 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.
25. Jordan SP, Waxman L, Smith DE, et al. Tick anticoagulant peptide: Kinetic analysis of the recombinant inhibitor with blood coagulation factor Xa. Biochemistry 1990;29:11095.
26. Jordan SP, Mao SS, Lewis SD, et al. Reaction pathway for inhibition of blood coagulation factor Xa by tick anticoagulant peptide. Biochemistry 1992;31:5374.
27. 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.
28. 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.
29. Glusa E, Hoffmann A, Markwardt F. Influence of benzamidine derivatives on thrombin-induced platelet reactions. Folia Haematol 1982;109:98.
30. Hara H, Tamao Y, Kikumoto R, et al. Effect of a potent thrombin inhibitor, No. 407, on platelet function in vitro and in vivo. Kobe J Med Sci 1980;26:47.
31. Hoffmann A, Markwardt F. Inhibition of the thrombinplatelet reaction by hirudin. Haemostasis 1984;14:164.
32. Matsuo T, Nakao K, Yamada T, et al. Effect of a new anticoagulant (MD 805) on platelet activation in the hemodialysis circuit. Thromb Res 1986;41:33.
33. Tremoli E, Maderna P, Colli S, et al. GYKI 14,451, a synthetic tripeptide inhibitor of thrombin: activity on platelet aggregation and arachidonic acid metabolism. Pharmacol Res Commun 1981;13:339.
34. Kaiser B, Koza M, Walenga JM, et al. Flow cytometric evaluation of the effect of various thrombin inhibitors on platelet activation in whole blood Thromb Res 1996;82:257.
35. Dunwiddie CT, Smith DE, Nutt EM, et al. Anticoagulant effects of the selective factor Xa inhibitors tick anticoagulant peptide and antistasin in the APTT assay are determined by the relative rate of prothrombinase inhibition. Thromb Res 1991;64:787.
36. Schaffer LW, Davidson JT, Vlasuk GP, et al. Selective factor Xa inhibition by recombinant antistasin prevents vascular graft thrombosis in baboons. Arterioscler Thromb 1991; 12:879.
37. Vlasuk GP, Ramjit D, Fujita, et al. 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.
38. Hauptmann J, Kaiser B. Anticoagulant potential of synthetic and recombinant inhibitors of factor Xa and thrombin in vitro. Blood Coag Fibrinol 1993;4:577.
39. Kaiser B, Fareed J, Hoppensteadt D, et al. Influence of recombinant hirudin and unfractionated heparin on thrombin and factor Xa generation in extrinsic and intrinsic activated systems. Thromb Res 1992;65:157.
40. Kaiser B, Callas D, Hoppensteadt D, et al. Comparative studies on the inhibitory spectrum of recombinant hirudin, DuP 714 and heparin on thrombin and factor Xa generation in biochemically defined systems. Thromb Res 1994;73:327.
41. 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;6:533.
42. Kaiser B, Fareed J, Walenga JM, et al. In vitro studies on thrombin generation in citrated, r-hirudinized and heparinized whole blood. Thromb Res 1991;64:589.
43. Gallistl S, Munteau W. Thrombin-hirudin complex formation, thrombin-antithrombin III complex formation, and thrombin generation after intrinsic activation of plasma. Thromb Haemost 1994;72:387.
44. Markwardt F, Kaiser B, Nowak G. Studies on antithrombotic effects of recombinant hirudin. Thromb Res 1989;54: 377.
45. Kaiser B, Markwardt F. Experimental studies on the antithrombotic action of a highly effective, synthetic thrombin inhibitor. Thromb Haemost 1986;55:194.
46. Mellott MJ, Holahan MA, Lynch JJ, et al. Acceleration of recombinant tissue-type plasminogen activator-induced reperfusion and prevention of reocclusion by recombinant antistasin, a selective factor Xa inhibitor, in a canine model of femoral arterial thrombosis. Circ Res 1992;70:1152.
47. Mellott MJ, Stranieri MT, Sitko GR, et al. Enhancement of recombinant tissue plasminogen activator-induced reperfusion by recombinant tick anticoagulant peptide, a selective factor Xa inhibitor, in a canine model of femoral arterial thrombolysis. Fibrinolysis 1993;7:195.
48. Sitko GR, Ramjit DR, Stabilito II, et al. 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.
49. Eldor A, Werber M, Finkelstein A, et al. Enhancement of rTPA thrombolysis with a selective factor Xa inhibitor derived from the leech: comparison to heparin and hirudin in a rabbit thrombosis model. Thromb Haemost 1995;73:1317.
50. Kaiser B, Markwardt F. Antithrombotic and haemorrhagic effects of synthetic and naturally occurring thrombin inhib-itors. Thromb Res 1986;43:613.
51. Schaffer LW, Davidson JT, Vlasuk GP, et al. Antithrombotic efficacy of recombinant tick anticoagulant peptide. A potent inhibitor of coagulation factor Xa in a primate model of arterial thrombosis. Circulation 1991;84:1741.
52. Hanson SR, Harker LA, Levanon A, et al. Inhibition of factor Xa in baboon thrombosis models. Thromb Haemost 1995;73:1311.
53. Werber MM, Zeelon E, Levanon A, et al. Yagin, a leech-derived FXa inhibitor, expressed in and recovered from E. coli: antithrombotic potency in vitro and in vivo. Thromb Haemost 1995;73:1312.
54. Yamazaki M, Asakura H, Saito M, et al. Effects of DX-9065a, an orally active, newly synthesized and specific inhibitor of factor Xa against experimental disseminated intravascular coagulation in rats. Thromb Haemost 1995;73:1312.
55. Tanabe K, Honda Y, Kunitada S. An orally active, specific inhibitor of factor Xa does not facilitate haemorrhage at the effective doses in rat thrombosis model. Thromb Haemost 1995;73:1312.
56. Hara T, Yokoyama A, Tanabe K, et al. DX-9065a, an orally active, specific inhibitor of factor Xa, inhibits thrombosis without affecting bleeding time in rats. Thromb Haemost 1995;74:635.
57. Hauptmann J, Kaiser B. Anticoagulant and antithrombotic action of the factor Xa inhibitor antistasin (ATS). Thromb Res 1993;71:169.
58. Fioravanti C, Burkholder D, Francis B, et al. Antithrombotic activity of recombinant tick anticoagulant peptide and heparin in a rabbit model of venous thrombosis. Thromb Res 1993;71:317.
59. Ragosta M, Gimple LW, Gertz SD, et al. Specific factor Xa inhibition reduces restenosis after balloon angioplasty of atherosclerotic femoral arteries in rabbits. Circulation 1994;89: 1262.
60. Yamazaki M, Asakura H, Aoshima K, et al. Effects of DX-9065a, an orally active, newly synthesized and specific inhibitor of factor Xa, against experimental disseminated intravascular coagulation in rats. Thromb Haemost 1994;72: 393.
61. Hara T, Morishima Y, Kunitada S. Selective factor Xa inhibitor, DX-9065a, suppressed hypercoagulable state during haemodialysis in cynomorgus monkeys. Thromb Haemost 1995;73:1311.
62. Lynch JJ, Sitko GR, Lehman ED, et al. Primary prevention of coronary arterial thrombosis with the factor Xa inhibitor rTAP in a canine electrolytic injury model. Thromb Haemost 1995;74:640.
63. Prager NA, Abendschein DR, McKenzie CR, et al. Role of thrombin compared with factor Xa in the procoagulant activity of whole blood clots. Circulation 1995;92:962.