Thrombin and factor Xa inhibitors

Drugs of the Future

Volumn 23, Issue 4, 1998, Pages 423-426

  Kaiser, Brigitte ^a  

^a FRIEDRICH SCHILLER UNIVERSITY JENA   (Germany)

Author keywords

[No Author keywords available]

Indexed keywords

2 [4 [(1 ACETIMIDOYL 3 PYRROLIDINYL)OXY]PHENYL] 3 (7 AMIDINO 2 NAPHTHYL)PROPIONIC ACID; ANTICOAGULANT AGENT; ANTISTATIN; ARGATROBAN; BLOOD CLOTTING FACTOR 10A INHIBITOR; DESULFATOHIRUDIN; HEPARIN; HIRUDIN; HIRUDIN DERIVATIVE; HIRULOG; LEPIRUDIN; LOW MOLECULAR WEIGHT HEPARIN; N ACETYL 4 (AMINOIMINOMETHYL)PHENYLALANYL 2 CYCLOHEXYLGLYCYL 3 (1 METHYLPYRIDINIUM 3 YL) ALANYLLEUCYLPROLINAMIDE; THROMBIN INHIBITOR; TICK ANTICOAGULANT PEPTIDE; UNCLASSIFIED DRUG; YAGIN;

ANTICOAGULATION; CLINICAL TRIAL; DRUG EFFICACY; DRUG STRUCTURE; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; ORAL DRUG ADMINISTRATION; REVIEW; THROMBOSIS;

EID: 0031838598     PISSN: 03778282     EISSN: None     Source Type: Journal    
DOI: 10.1358/dof.1998.023.04.858356     Document Type: Review

References (119)

1. Fenton, J.W.II. Thrombin functions and antithrombotic intervention. Thromb Haemost 1995, 74: 493-8.
2. Stubbs, M.T., Bode, W. A player of many parts: The spotlight falls on thrombin's structure. Thromb Res 1993, 69: 1-58.
3. Kanthou, C., Benzakour, O. Cellular effects of thrombin and their signalling pathways. Cell Pharmacol 1995, 2: 293-302.
4. Esmon, C.T. Cell mediated events that control blood coagulation and vascular injury. Annu Rev Cell Biol 1993, 9: 1-26.
5. Vu, T.K.H., Hung, D.T., Wheaton, V.I., Coughlin, S.R. Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation. Cell 1991, 64: 1057-68.
6. Brinkman, H.J.M., Mertens, K., Holthuis, J., Zwarthuinink, L.A., Grijm, K., Vanmourik, J.A. The activation of human blood coagulation factor X on the surface of endothelial cells: A comparison with various vascular cells, platelets and monocytes. Br J Haematol 1994, 87: 332-42.
7. Mann, K.G. The assembly of blood clotting complexes on membranes. Trends Biochem Sci 1987, 12: 229-33.
8. Mann, K.G., Kalafatis, M. The coagulation explosion. Cerebrovasc Dis 1995, 5: 93-7.
9. Nicholson, A.C., Nachman, R.L., Altieri, D.C. et al. Effector cell protease receptor-1 is a vascular receptor for coagulation factor Xa. J Biol Chem 1996, 271: 28407-13.
10. Bono, F., Herault, J.P., Avril, C., Schaeffer, P., Lormeau, J.C., Herbert, J.M. Human umbilical vein endothelial cells express high affinity receptors for factor Xa. J Cell Physiol 1997, 172: 36-43.
11. Bouchard, B.A., Catcher, C.S., Thrash, B.R., Adida, C., Tracy, P.B. Effector cell protease receptor-1, a platelet activation-dependent membrane protein, regulates prothrombinase-catalyzed thrombin generation. J Biol Chem 1997, 272: 9244-51.
12. Rosenberg, R.D., Rosenberg, J.S. Natural anticoagulant mechanisms. J Clin Invest 1984, 74: 1-6.
13. Mann, K.G., Nesheim, M.E., Church, W.R. Haley, P., Krishnaswamy, S. Surface-dependent reactions of the vitamin K-dependent enzyme complexes. Blood 1990, 76: 1-16.
14. Tollefsen, D.M., Majerus, D.W., Blank, M.K. Heparin cofactor II. Purification and properties of a heparin-dependent inhibitor of thrombin in human plasma. J Biol Chem 1982, 257: 2162-9.
15. Dahlbäck, B. The protein C anticoagulant system: Inherited defects as basis for venous thrombosis. Thromb Res 1995, 77: 1-43.
16. Broze, G.J. Jr. Tissue factor pathway inhibitor and the current concept of blood coagulation. Blood Coag Fibrinol 1995, 6: S7-13.
17. Fenton, J.W. II. Thrombin bioregulatory functions. Adv Clin Enzymol 1988, 6: 186-93.
18. Talbot, M.D., Butler, K.D. Potential clinical uses of thrombin inhibitors. Drug News Perspect 1990, 3: 357-63.
19. Callas, D., Fareed J. Comparative pharmacology of site directed antithrombin agents. Implication in drug development. Thromb Haemost 1995, 74: 473-81.
20. Noeske-Jungblut, C., Haendler, B., Donner, P., Alagon, A., Possani, L., Schleuning, W.D. Triabin: A highly potent exosite inhibitor of thrombin. J Biol Chem 1995, 270: 28629-34.
21. Glusa, E., Bretschneider, E., Daum, J., Noeske-Jungblut, C. Inhibition of thrombin-mediated cellular effects by triabin, a highly potent anion-binding exosite thrombin inhibitor. Thromb Haemost 1997, 77: 1196-200.
22. Hauptmann, J., Markwardt, F. Pharmacological aspects of the development of selective synthetic thrombin inhibitors as anticoagulants. Semin Thromb Hemost 1992, 18: 200-17.
23. Markwardt, F., Stürzebecher, J. Inhibitors of trypsin and trypsin-like enzymes with a physiological role. In: Design of Enzyme Inhibitors as Drugs. Sandler, M., Smith, H.J. (Eds.). Oxford University Press: Oxford 1989, 619-49.
24. Shafer, J.A. Direct thrombin inhibitors: Active-site inhibitors of thrombin. In: New Therapeutic Agents in Thrombosis and Thrombolysis. Sasahara, A.A., Loscalzo, J. (Eds.). Marcel Dekker, Inc.: New York 1997, 143-57.
25. Powers, J.C., Kam, C.M. Synthetic substrates and inhibitors of thrombin. In: Thrombin: Structure and Function. Berliner, L.J. (Ed.). Plenum Press: New York 1992, 117-58.
26. Maraganore, J.M., Bourdon, P., Jablonski, J., Ramachandran, K.L., Fenton, J.W. II. Design and characterization of hirulogs: A novel class of bivalent peptide inhibitors of thrombin. Biochemistry 1990, 29: 7095-101.
27. Maraganore, J.M. Direct thrombin inhibitors: Hirulog. In: New Therapeutic Agents in Thrombosis and Thrombolysis. Sasahara. A.A., Loscalzo, J. (Eds.). Marcel Dekker, Inc.: New York 1997, 191-208.
28. Fenton, J.W. II, Ni, F., Witting, J.I., Brezniak, D.V., Andersen, T.T., Malik, A.B. The rational design of thrombin-directed antithrombotics. In: The Design of Synthetic Inhibitors of Thrombin. Claeson, G. (Ed.). Plenum Press: New York 1993, 1-13.
29. Kaiser, B., Hauptmann, J. Factor Xa inhibitors as novel antithrombotic agents: Facts and perspectives. Cardiovasc Drug Rev 1994, 12: 225-36.
30. 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.
31. 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.
32. 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.): 88-100s.
33. Nutt, E., Gasic, T., Rodkey, J. et al. The amino acid sequence of antistasin. J Biol Chem 1988, 263: 10162-7.
34. Nutt, E.M., Jain, D., Lenny, A.B., Schaffer, L., Siegl, P.K., Dunwiddie, C.T. Purification and characterization of recombinant antistasin: A leech-derived inhibitor of coagulation factor Xa. Arch Biochem Biophys 1991, 285: 37-44.
35. Tuszynski, G.P., Gasic, T.B., Gasic, G.J. Isolation and characterization of antistasin. An inhibitor of metastasis and coagulation. J Biol Chem 1987, 262: 9718-23.
36. Dunwiddie, C.T., Thornberry, N.A., Bull, H.G. 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: 16694-9.
37. Waxman, L., Smith, D.E., Arcuri, K.E., Vlasuk, G.P. Tick anticoagulant peptide (TAP) is a novel inhibitor of blood coagulation factor Xa. Science 1990, 248: 593-6.
38. Jordan, S.P., Mao, S.S., Lewis, S.D., Shafer, J.A. Reaction pathway for inhibition of blood coagulation factor Xa by tick anticoagulant peptide. Biochemistry 1992, 31: 5374-80.
39. Jordan, S.P., Waxman, L., Smith, D.E., Vlasuk, G.P. Tick anticoagulant peptide: Kinetic analysis of the recombinant inhibitor with blood coagulation factor Xa. Biochemistry 1990, 29: 11095-100.
40. Krishnaswamy, S., Vlasuk, G.P., Bergum, P.W. Assembly of the prothrombinase complex enhances the inhibition of bovine factor Xa by tick anticoagulant peptide. Biochemistry 1994, 33: 7897-907.
41. Vlasuk, G.P. 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.
42. Rigbi, M., Jackson, C.M., Atamna, H. et al. FXa inhibitor from the saliva of the leech Hirudo medicinalis. Thromb Haemost 1995, 73: 1306.
43. Vlasuk, G.P., Bergum, P.W., Brunck, T.K. et al. Anticoagulant repertoire of hematophagous nematodes. Thromb Haemost 1995, 73: 1305.
44. Yokoyama, T., Kelly, A.B., Marzec, U.M., Hanson, S.R., Kunitada, S., Harker, L.A. Antithrombotic effects of orally active synthetic antagonists of activated factor X in nonhuman primates. Circulation 1995, 92: 485-91.
45. Hara, T., Yokoyama, A., Ishihara, H., Yokoyama, Y., Nagakara, T., Iwamoto, M. DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa. Thromb Haemost 1994, 71: 314-9.
46. Katakura, S., Nagakara, T., Hara, T., Iwamoto, M. A novel factor Xa inhibitor: Structure-activity relationships and selectivity between factor Xa and thrombin. Biochem Biophys Res Commun 1993, 197: 965-72.
47. Katakura, S., Nagakara, T., Hara, T., Kunitada, S., Iwamoto, M. 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: 387-94.
48. 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.): 140-3s.
49. th IBC International Symposium: Advances in Anticoagulants & Antithrombotics, Washington, DC 1995.
50. Ostrem, J.A., Stringer, S., Al-Obedi, F. et al. Characterization of an orally available and highly specific synthetic factor Xa inhibitor. Thromb Haemost 1995, 73: 1306.
51. Taniuchi, Y., Sakai, Y., Kawasaki, T. et al. Anticoagulant and pharmacokinetic profiles of YM-60828, an orally active and potent synthetic inhibitor of factor Xa. Thromb Haemost 1997; Suppl.: 294.
52. Sato, K., Kawasaki, T., Hisamichi, N. et al. A selective and potent factor Xa inhibitor, YM-60828, exerts its antithrombotic effect with little prolongation of bleeding time. Thromb Haemost 1997, Suppl.: 292.
53. Gunn, A.C., Wong, P.W., Marlowe, C.K., Zhu, B.Y., Scarborough, R.M., Sinha, U. Design, synthesis and characterization of specific inhibitors of coagulation factor Xa. Thromb Haemost 1997, Suppl.: 294.
54. Wong, A.G., Ku, P., Lin, P.H. et al. Inhibition of rabbit deep vein thrombosis by specific inhibitors of coagulation factor Xa. Thromb Haemost 1997, Suppl.: 293.
55. Lormeau, J.C., Herault, J.P. The effect of the synthetic pentasaccharide SR 90107/Org 31540 on thrombin generation ex vivo is uniquely due to ATIII-mediated neutralization of factor Xa. Thromb Haemost 1995, 74: 1474-7.
56. Olson, S.T., Björk, I., Sheffer, R., Craig, P.A., Shore, J.D., Choay, J. Role of antithrombin-binding pentasaccharide in heparin acceleration of antithrombin-proteinase reactions. J Biol Chem 1992, 267: 12528-38.
57. Benedict, C.R., Ryan, J., Todd, J. et al. Active site-blocked factor Xa prevents thrombus formation in the coronary vasculature in parallel with inhibition of extravascular coagulation in a canine thrombosis model. Blood 1993, 81: 2059-66.
58. Sinha, U., Hollenbach, S., Wolf, D.L. Macromolecu-lar complex assembly of prothrombinase is a central process of thrombosis. In: Ann NY Acad Sci, Vol. 714: Platelet-Dependent Vascular Occlusion. G.A. FitzGerald, L.K. Jennings, C. Patrono (Eds.). New York 1994, 32-40.
59. Bush, L.R. Argatroban, a selective, potent thrombin inhibitor. Cardiovasc Drug Rev 1991, 9: 247-63.
60. Kaiser, B. Anticoagulant and antithrombotic actions of recombinant hirudin. Semin Thromb Hemost 1991, 2: 130-6.
61. Walsmann, P., Kaiser, B. Biochemical and pharmacological properties of recombinant hirudin. Drugs Today 1989, 25: 473-85.
62. Kaiser, B., Hauptmann, J. Pharmacology of synthetic thrombin inhibitors of the tripeptide type. Cardiovasc Drug Rev 1992, 10: 71-87.
63. Kaiser, B., Koza, M., Walenga, J.M., Fareed, J. Flow cytometric evaluation of the effect of various thrombin inhibitors on platelet activation in whole blood. Thromb Res 1996, 82; 257-63.
64. Herbert, J.M., Bernat, A., Dol, F., Hérault, J.P., Crépon, B., Lormeau, J.C. 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.
65. Hara, T., Yokoyama, A., Morishima, Y., Kunitada, S. Species differences in anticoagulant and anti-Xa activity of DX-9065a, a highly selective factor Xa inhibitor. Thromb Res 1995, 80: 99-104.
66. Hauptmann, J., Kaiser, B. Anticoagulant and antithrombotic action of the factor Xa inhibitor antistasin (ATS). Thromb Res 1993, 71: 169-74.
67. Vlasuk, G.P., Ramjit, D., Fujita, T. 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: 257-62.
68. 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.
69. Kaiser, B., Fareed, J., Hoppensteadt, D., Birdsong, B., Walenga, J.M., Markwardt, F. Influence of recombinant hirudin and unfractionated heparin on thrombin and factor Xa generation in extrinsic and intrinsic activated systems. Thromb Res 1992, 65: 157-64.
70. Kaiser, B., Callas, D., Hoppensteadt, D., Mallinows-ka, K., Fareed, J. 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: 327-35.
71. Ofosu, F.A., Fenton, J.W. II, Maraganore, J. et al. Inhibition of the amplification reactions of blood coagulation by site-specific inhibitors of α-thrombin. Biochem J 1992, 283: 893-7.
72. Gallistl, S., Muntean, W. Thrombin-hirudin complex formation, thrombin-antithrombin III complex formation, and thrombin generation after intrinsic activation of plasma. Thromb Haemost 1994, 72: 387-92.
73. Gallistl, S., Muntean, W., Leis, H.J. Effects of heparin and hirudin on thrombin generation and platelet aggregation after intrinsic activation of platelet rich plasma. Thromb Haemost 1995, 74: 1163-8.
74. Kaiser, B., Fareed, J., Walenga, J.M., Hoppensteadt, D., Markwardt, F. In vitro studies on thrombin generation in citrated, r-hirudinized and heparinized whole blood. Thromb Res 1991, 64: 589-96.
75. Gold, H.K., Torres, F.W., Garabedian, H.D. et al. 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: 1039-47.
76. Zoldhelyi, P., Bichler, J., Owen, W.G. et al. Persistent thrombin generation in humans during specific thrombin inhibition with hirudin. Circulation 1994, 90: 2671-8.
77. Ginsberg, J.S., Nurmohamed, M.T., Gent, M. et al. Effects on thrombin generation of single injections of Hirulog™ in patients with calf vein thrombosis. Thromb Haemost 1994, 72: 523-5.
78. Bittl, J.A., Strony, J., Brinker, J.A. et al. Treatment with bivalirudin (Hirulog) as compared with heparin during coronary angioplasty for unstable or postinfarction angina. New Engl J Med 1995, 333: 764-9.
79. Mirshahi, M., Soria, J., Soria, C. et al. Evaluation of the inhibition by heparin and hirudin of coagulation activation during r-t-PA-induced thrombolysis. Blood 1989, 74: 1025-30.
80. Weitz, J.I., 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: 385-91.
81. Berry, C.N., Girardot, C., Lecoffre, C., Lunven, C. Effects of the synthetic thrombin inhibitor argatroban on fibrin-or clot-incorporated thrombin: Comparison with heparin and recombinant hirudin. Thromb Haemost 1994, 72: 381-6.
82. Prager, N.A., Abendschein, D.R., McKenzie, C.R., Eisenberg, P.R. Role of thrombin compared with factor Xa in the procoagulant activity of whole blood clots. Circulation 1995, 92: 962-7.
83. Eisenberg, P.R., Siegel, J.E., Abendschein, D.R., Miletich, J.P. Importance of factor Xa in determining the procoagulant activity of whole-blood clots. J Clin Invest 1993, 91: 1877-83.
84. Hérault, J.P., Pflieger, A.M., Bernat, A., Lormeau, J.C., Herbert, J.M. Comparative effects of two factor Xa inhibitors: The synthetic pentasaccharide SR 90107 A/Org 31540 and DX 90675 on free and clot-bound prothrombinase. Thromb Haemost 1997, Suppl.: 293.
85. Meddahi, S., Bara, L., Fessi, H., Samama, M.M. Evaluation of clot-associated procoagulant activities in the presence of DX-9065a, rhirudin, enoxaparin and heparin: By a chromogenic technique, F1+2 and TAT measurements. Thromb Haemost 1997, Suppl.: 294.
86. Berry, C.N., Girard, D., Girardot, C., Lochot, S., Lunven, C., Visconte, C. Antithrombotic activity of argatroban in experimental thrombosis in the rabbit. Semin Thromb Hemost 1996, 22: 233-41.
87. Berry, C.N., Girard, D., Lochot, S., Lecoffre, C. Antithrombotic actions of argatroban in rat models of venous, 'mixed' and arterial thrombosis, and its effect on the tail transection bleeding time. Br J Pharmacol 1994, 113: 1209-14.
88. Markwardt, F., Kaiser, B., Nowak, G. Studies on antithrombotic effects of recombinant hirudin. Thromb Res 1989, 54: 377-88.
89. Kaiser, B., Markwardt, F. Experimental studies on the antithrombotic action of a highly effective, synthetic thrombin inhibitor. Thromb Haemost 1986, 55: 194-6.
90. Hoffmann, A., Markwardt, F. Inhibition of the thrombin-platelet reaction by hirudin. Haemostasis 1984, 14: 164-9.
91. Benzakour, O., Kanthou, C. Cellular and molecular events in atherogenesis: basis for pharmacological and gene therapy approaches to restenosis. Cell Pharmacol 1996, 3: 7-22.
92. Schwartz, R.S., Holmes, D.R. Jr., Topol, E.J. The restenosis paradigm revisited: an alternative proposal for cellular mechanisms. J Am Coll Cardiol 1992; 20: 1284-1293.
93. McNamara, C.A., Sarembock, I.J., Bachhuber, B.G. et al. Thrombin and vascular smooth muscle cell proliferation: Implications for atherosclerosis and restenosis. Semin Thromb Hemost 1996, 22: 139-44.
94. Ali, M.N., Villarreal-Levy, G., Schafer, A.I. The role of thrombin and thrombin inhibitors in coronary angioplasty. Chest 1995, 108: 1409-19.
95. Sarembock, I.J., Gertz, S.D., Gimple, L.W., Owen, R.M., Powers, E.R., Roberts, W.C. Effectiveness of recombinant desulphatohirudin in reducing restenosis after balloon angioplasty of atherosclerotic femoral arteries in rabbits. Circulation 1991, 84: 232-43.
96. Heras, M., Chesebro, J.H., Webster, M.W.I. et al. Hirudin, heparin, and placebo during deep arterial injury in the pig: The in vivo role of thrombin in platelet-mediated thrombosis. Circulation 1990, 82: 1476-84.
97. Kaiser, B., Simon, A., Markwardt, F. Antithrombotic effects of recombinant hirudin in experimental angioplasty and intravascular thrombolysis. Thromb Haemost 1990, 63: 44-7.
98. Imanishi, T., Arita, M., Hamada, M., Tomobuchi, Y., Hano, T., Nishio, I. Effects of locally administration of argatroban using a hydrogel-coated balloon catheter on intimal thickening induced by balloon injury. Jpn Circ J 1997, 61: 256-62.
99. Abendschein, D.R., Recchia, D., Meng, Y.Y., Oltrona, L., Wickline, S.A., Eisenberg, P.R. Inhibition of thrombin attenuates stenosis after arterial injury in minipigs. J Am Coll Cardiol 1996, 28: 1849-55.
100. Unterberg, C., Sandrock, D., Nebendahl, K., Buchwald, A.B. Reduced acute thrombus formation results in decreased neointimal proliferation after coronary angioplasty. J Am Coll Cardiol 1995, 26: 1747-54.
101. Barry, W.L., Wiegman, P.J., Gimple, L.W. et al. A new single-injury model of balloon angioplasty in cholesterol-fed rabbits: Beneficial effect of hirudin and comparison with double-injury model. Lab Invest 1997, 77: 109-16.
102. Van de Boos, A.A., Deckers, J.W., Heyndrickx, G.R. et al. Safety and efficacy of recombinant hirudin (CGP 39393) versus heparin in patients with stable angina undergoing coronary angioplasty. Circulation 1993, 88: 2058-66.
103. Topol, E.J., Bonan, R., Jewitt, D. et al. Use of a direct antithrombin, hirulog, in place of heparin during coronary angioplasty. Circulation 1993, 87: 1622-9.
104. Serryus, P.W., Herrman, J.P.R., Simon, R. et al. A comparison of hirudin with heparin in the prevention of restenosis after coronary angioplasty. New Engl J Med 1995, 333: 757-63.
105. Herrman, J.P.R., Suryapranata, H., den Heijer, P., Kutryk, M.J.B., Gabriël, L., Serryus, P.W. Argatroban during percutaneous transluminal angioplasty: Results of a dose verification study. J Thromb Thrombolysis 1996, 3: 367-75.
106. Ko, F.N., Yang, Y.C., Huang, S-.C., Ou, J.T. Coagulation factor Xa stimulates platelet-derived growth factor release and mitogenesis in cultured vascular smooth muscle cells of rat. J Clin Invest 1996, 98: 1493-501.
107. Gasic, G.P., Arenas, C.P., Gasic, T.B., Gasic, G.J. Coagulation factors X, Xa, and protein S as potent mitogens of cultured aortic smooth muscle cells. Proc Natl Acad Sci USA 1992, 89: 2317-20.
108. Ragosta, M., Gimple, L.W., Gertz, D. et al. Specific factor Xa inhibition reduces restenosis after balloon angioplasty of atherosclerotic femoral arteries in rabbits. Circulation 1994, 89: 1262-71.
109. Schwartz, R.S., Holder, D.J., Holmes, D.R. Jr. et al. Neointimal thickening after severe coronary artery injury is limited by short-term administration of a factor Xa inhibitor. Results in a porcine model. Circulation 1996, 93: 1542-8.
110. Erickson, B.R., Topol, E.J. Direct thrombin inhibitors in arterial thrombosis. In: New Therapeutic Agents in Thrombosis and Thrombolysis. Sasahara, A.A., Loscalzo, J. (Eds.). Marcel Dekker, Inc.: New York 1997, 169-89.
111. Crowther, M.A., Ginsberg, J.S. Direct thrombin inhibitors in venous thromboembolism. In: New Therapeutic Agents in Thrombosis and Thrombolysis. Sasahara, A.A., Loscalzo, J. (Eds.). Marcel Dekker, Inc.: New York 1997, 159-68.
112. Hermann, J.P.R., Kutryk, M.J.B., Serruys, P.W. Clinical trials of direct thrombin inhibitors during invasive procedures. Thromb Haemost 1997, 78: 367-76.
113. Verstraete, M. Direct thrombin inhibitors: Appraisal of the antithrombotic/hemorrhagic balance. Thromb Haemost 1997, 78: 357-63.
114. White, H.D. Clinical trials of direct thrombin inhibitors in acute ischemic syndromes. Thromb Haemost 1997, 78: 364-6.
115. Vermeer, F., Vahanian, A., Fels, P.W. et al. Intravenous argatroban versus heparin as co-medication to alteplase in the treatment of acute myocardial infarction: Preliminary results of the ARGAMI pilot study. J Am Coll Cardiol 1997, 29: 185-6.
116. Lewis, B.E., Grassmann, E.D., Wrona, L., Rangel, Y. Novastan® anticoagulation during renal stent implant in a patient with heparin-induced thrombocytopenia. Blood Coag Fibrinol 1997, 8: 54-8.
117. Kaiser, B. A survey of anti-Xa-based drugs: Potential use in cardiovascular indications. In: New Anti-coagulants for the Cardiovascular Patient. Pifarré, R. (Ed.). Hanley & Belfus, Inc.: Philadelphia 1997, 431-41.
118. Wong, P.C., Crain, E.J., Nguan, O., Watson, C.A., Racanelli, A. Antithrombotic actions of selective inhibitors of blood coagulation factor Xa in rat models of thrombosis. Thromb Res 1996, 83: 117-26.
119. Yamashita, T., Tsuji, T., Matsuoka, A., Giddings, J.C., Yamamoto, J. The antithrombotic effect of synthetic low molecular weight human factor Xa inhibitor, DX-9065a, on He-Ne laser-induced thrombosis in rat mesenteric microvessels. Thromb Res 1997, 85: 45-51.