Pharmacokinetic and preclinical studies with reteplase

Drugs of Today

Volumn 33, Issue 9, 1997, Pages 633-639

  Martin, Ulrich ^a   Kohnert, Ulrich ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

Author keywords

[No Author keywords available]

Indexed keywords

RECOMBINANT PLASMINOGEN ACTIVATOR; RETEPLASE;

ANIMAL EXPERIMENT; ANIMAL MODEL; BLOOD CLOT LYSIS; CONCENTRATION RESPONSE; DRUG ACTIVITY; DRUG HALF LIFE; DRUG METABOLISM; ESCHERICHIA COLI; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; NONHUMAN; PHARMACOKINETICS; RABBIT; RAT; REPERFUSION; REVIEW; VEIN THROMBOSIS;

EID: 0030661894     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.1997.33.9.444769     Document Type: Review

References (48)

1. Granger, C.B., Califf, R.M., Topol, E.J. Thrombolytic therapy for acute myocardial infarction - A review. Drugs 1992, 44: 293-325.
2. Task Force on Myocardiai Reperfusion. Reperfusion in acute myocardial infarction. Circulation 1994, 90: 2091-102.
3. Vogt, A., von Essen, R., Tebbe, U., Feuerer, W., Appel, K.F., Neuhaus, K.L. Impact of early perfusion status of the infarct-related artery on short-term mortality after thrombolysis for acute myocardial infarction: Retrospective analysis of four german multicenter studies. J Am Coll Cardiol 1993, 21: 1391-5.
4. Ohman, E.M., Califf, R.M., Topol, E.J. et al. Consequences of reocclusion after successful reperfusion therapy in acute myocardial infarction. Circulation 1990, 82: 781-91.
5. Hoylaerts, M., Rijken, D.C., Lijnen, H.R., Collen, D. Kinetics of the activation of plasminogen by human tissue plasminogen activator. J Biol Chem 1982, 257: 2912-9.
6. van Zonnefeld, A.J., Veerman, H., Pannekoek, H. On the interaction of the finger and the kringle-2 domain of tissue-type plasminogen activator with fibrin. J Biol Chem 1986, 261: 14214-8.
7. van Zonnefeld, A.J., Veerman, H., Pannekoek, H. Autonomous functions of structural domains on human tissue-type plasminogen activator. Proc Natl Acad Sci USA 1986, 83: 4670-4.
8. Verheijen, J.H., Caspers, M.P.M., Chang, G.T.G., de Munk, G.A.W., Pouwels, P.H., Enger-Valk, B.E. Involvement of finger domain and kringle 2 domain of tissue-type plasminogen activator in fibrin binding and stimulation of activity by fibrin. EMBO J 1986, 5: 3525-30.
9. Kohnert, U., Rudolph, R., Verheijen, J.H. et al. Biochemical properties of the kringle 2 and protease domains are maintained in the refolded t-PA deletion variant BM 06.022. Protein Eng 1992, 5: 93-100.
10. Stürzebecher, J., Neumann, U., Kohnert, U., Kresse, G.B., Fischer, S. Mapping of the catalytic site of CHO-t-PA and the t-PA variant BM 06.022 by synthetic inhibitors and substrates. Protein Sci 1992, 1: 1007-13.
11. Kohnert, U., Horsch, B., Fischer, S. A variant of tissue plasminogen activator (t-PA) comprised of the kringle 2 and the protease domain shows a significant difference in the in vitro rate of plasmin formation as compared to the recombinant human t-PA from transformed Chinese hamster ovary cells. Fibrinolysis 1993, 7: 365-72.
12. Rijken, D.C., Groeneveld, E., Barrett-Bergshoeff, M.M. In vitro stability of a tissue-type plasminogen activator mutant, BM 06.022, in human plasma. Thromb Haemostas 1994, 72: 906-11.
13. Grünewald, M., Ellbrück, D., Mohren, M. et al. Single vs double bolus thrombolysis with the recombinant plasminogen activator BM 06.022 in patients with acute myocardial infarction - Pharmacokinetics and hemostatic changes. Thromb Haemostas 1995, 73: 1328.
14. Tanswell, P., Tebbe, U., Neuhaus, K.L., Glasle-Schwarz, L., Wojcik, J., Seifried, E. Pharmacokinetics and fibrin specificity of alteplase during accelerated infusions in acute myocardial infarction. J Am Coll Cardiol 1992, 19: 1071-5.
15. Mulder, M., Kohnert, U., Fischer, S., van Hinsberg, V.W.M., Verheijen, J.H. The interaction of recombinant tissue type plasminogen activator and recombinant plasminogen activator (r-PA/ BM 06.022) with human endothelial cells. Blood Coagul Fibrinol 1997, 8: 124-33.
16. Stockinger, H., Kubbies, M., Rudolph, R., Stern, A., Kohnert, U., Fischer, S. Binding of recombinant variants of human tissue-type plasminogen activator (t-PA) to human umbilical vein endothelial cells. Thromb Res 1992, 67: 589-99.
17. Beebe, D.B., Miles, L.A., Plow, E.F. A linear amino acid sequence involved in the interaction of t-PA with its endothelial cell receptor. Blood 1988, 74: 2034-7.
18. Hajjar, K.A. The endothelial cell tissue plasminogen activator receptor. J Biol Chem 1991, 266: 21962-70.
19. Martin, U., Sponer, G., Strein, K. Differential fibrinolytic properties of the recombinant plasminogen activator BM 06.022 in human plasma and blood clot systems in vitro. Blood Coagul Fibrinolysis 1993, 4: 235-42.
20. Martin, U., Sponer, G., Strein, K. Influence of hepatic and renal failure on pharmacokinetic properties of the novel recombinant plasminogen activator BM 06.022 in rats. Drug Metab Dispos 1993, 21: 236-41.
21. Fischer, S., Kohnert, U. Major mechanistic differences explain the higher clot lysis potency of reteplase over alteplase: The lack of fibrin binding is an advantage for bolus application of fibrin-specific thrombolytics. Fibrinolysis Proteolysis 1997, 11: 129-35.
22. Martin, U., Fischer, S., Kohnert, U. et al. Thrombolysis with an Escherichia coli-produced recombinant plasminogen activator (BM 06.022) in the rabbit model of jugular vein thrombosis. Thromb Haemostas 1991, 65: 560-4.
23. Martin, U., Fischer, S., Kohnert, U. et al. Coronary thrombolytic properties of a novel recombinant plasminogen activator (BM 06.022) in a canine model. J Cardiovasc Pharmacol 1991, 18: 111-9.
24. Martin, U., Sponer, G., Strein, K. Evaluation of thrombolytic and systemic effects of the novel recombinant plasminogen activator BM 06.022 compared with alteplase, anistreplase, streptokinase and urokinase in a canine model of coronary artery thrombosis. J Am Coll Cardiol 1992, 19: 433-40.
25. Martin, U., Sponer, G., Strein, K. Rapid reversal of canine thromboembolic pulmonary hypertension by bolus injection of the novel recombinant plasminogen activator BM 06.022. J Cardiovasc Pharmacol 1993, 21: 455-61.
26. Shebuski, R.J., Sitko, G.R., Claremon, D.A., Baldwin, J., Remy, D.C., Stern, A.M. Inhibition of factor XIIIa in a canine model of coronary artery thrombosis: Effect on reperfusion and acute reocclusion after recombinant tissue type plasminogen activator. Blood 1990, 75: 1455-9.
27. Shebuski, R.J., Stabilito, I.J., Sitko, G.R., Polokoff, M.H. Acceleration of recombinant tissue-type plasminogen activator-induced thrombolysis and prevention of reocclusion by the combination of heparin and the Arg-Gly-Asp-containingpeptide bitistatin in a canine model of coronary thrombosis. Circulation 1990, 82: 169-77.
28. Martin, U., Sponer, G., Konig, R., Smolarz, A., Meyer-Sabellek, W., Strein, K. Double bolus administration of the novel recombinant plasminogen activator BM 06.022 improves coronary blood flow after reperfusion in a canine model of coronary thrombosis. Blood Coagul Fibrinolysis 1992, 3: 139-47.
29. Martin, U., Sponer, G., Strein, K.. Hirudin and sulotroban improve coronary blood flow after reperfusion induced by the novel recombinant plasminogen activator BM 06.022 in a canine model of coronary artery thrombosis. Int J Hematol 1992, 56: 143-53.
30. Martin, U., Doerge, L., Fischer, S. Comparison of desulfatohirudin (REVASC) and heparin as adjuncts to thrombolytic therapy with reteplase in a canine model of coronary artery thrombosis. BrJ Pharmacol 1996, 118: 271-6.
31. Martin, U., Fischer, S., Sponer, G. Influence of heparin and systemic lysis on coronary blood flow after reperfusion induced by the novel recombinant plasminogen activator BM 06.022 in a canine model of coronary thrombosis. J Am Coll Cardiol 1993, 22: 914-20.
32. Marder, V.J., Shulman, N.R. High molecular weight derivatives of human fibrinogen produced by plasmin. J Biol Chem 1969, 244: 2120-4.
33. Stump, D.C., Califf, R.M., Topol, E.J. et al. Pharmacodynamics of thrombolysis with recombinant tissue-type plasminogen activator: Correlation with characteristics of and clinical outcomes in patients with acute myocardial infarction. Circulation 1989, 80: 1222-30.
34. Harrington, R.A., Sane, D.C., Califf, R.M. et al. Clinical importance of thrombocytopenia occurring in the hospital phase after administration of thrombolytic therapy for acute myocardial infarction. J Am Coll Cardiol 1994, 23: 891-8.
35. Parise, P., Agnelli, G. Thrombus resistance to lysis and reocclusion after thrombolysis: The role of platelets. Blood Coagul Fibrinolysis 1991, 2: 749-58.
36. Martin, U., Dalchau, H., Sponer, H. Effects of the novel recombinant plasminogen activator BM 06.022 on platelets and bleeding time in rabbits. Platelets 1992, 3: 247-53.
37. Martin, U., Sponer, G., Strein, K. Effects of the novel recombinant plasminogen activator BM 06.022 on human platelet aggregation in vitro. Fibrinolysis 1993, 7: 203-10.
38. Rijken, D.C., Otter, M., Kuiper, J., van Berkel, T.J.C. Receptor-mediated endocytosis of tissue-type plasminogen activator (t-PA) by liver cells. Thromb Res 1990, Suppl. X: 63-71.
39. Hotchkiss, A., Refino, C.J., Leonard, C.K. et al. The influence of carbohydrate structure on the clearance of recombinant tissue-type plasminogen activator. Thromb Haemostas 1988, 60: 255-61.
40. Larsen, G.R., Metzger, M., Henson, K., Blue, Y., Horgan, P. Pharmacokinetic and distribution analysis of variant forms of tissue-type plasminogen activator with prolonged clearance in rat. Blood 1989, 73: 1842-50.
41. Narita, M., Bu, G., Herz, J., Schwartz, A.L. Two receptor systems are involved in the plasma clearance of tissue-type plasminogen activator (t-PA) in vivo. J Clin Invest 1995, 96: 1164-8.
42. Martin, U., Fischer, S., Kohnert, U. et al. Pharmacokinetic properties of an Escherichia coli-produced recombinant plasminogen activator (BM 06.022) in rabbits. Thromb Res 1991, 62: 137-46.
43. Martin, U., Kohler, J., Sponer, G., Strein, G. Pharmacokinetics of the novel recombinant plasminogen activator BM 06.022 in rats, dogs, and nonhuman primates. Fibrinolysis 1992, 6: 39-43.
44. Seifried, E., Mueller, M.M., Martin U., Koenig, R., Hombach, V. Bolus application of a novel recombinant plasminogen activator in acute myocardial infarction patients: Pharmacokinetics and effects on the hemostatic system. Ann NY Acad Sci 1992, 667: 417-20.
45. Seifried, E., Mueller, M.M., Eggeling, T., Martin, U., Koenig, R., Hombach, V. Bolus application of a mutant of tissue plasminogen activator in acute myocardial infarction patients - Pharmacokinetics and hemostatic effects. Ann Hematol 1993, 66: A40.
46. Kuiper, J., Otter, M., Rijken, D.C., van Berkel, T.J.C. Characterization of the interaction in vivo of tissue-type plasminogen activator with liver cells. J Biol Chem 1988, 263: 18220-4.
47. Kuiper, J., van de Bilt, H., Martin, U., van Berkel, T.J.C. Uptake, internalization and degradation of the novel plasminogen activator reteplase (BM 06.022) in the rat. Thromb Haemostas 1995, 74: 1501-10.
48. Martin, U.. Doerge, L., Stegmeier, K.M., Müller-Beckmann. B. Influence of the degree of renal dysfunction on the pharmacokinetic properties of the novel recombinant plasminogen activator reteplase in rats. Drug Metab Dispos 1996, 24: 288-91.