The ideal fibrinolytic: Can drug design improve clinical results?

European Heart Journal

Volumn 20, Issue 20, 1999, Pages 1452-1458

  Van De Werf, F J ^a  

^a UNIVERSITY HOSPITALS LEUVEN   (Belgium)

Author keywords

Acute myocardial infarction; Fibrinolytics; Thrombolytic therapy

Indexed keywords

FIBRIN; FIBRINOLYTIC AGENT; HEPARIN; LANOTEPLASE; PLASMINOGEN ACTIVATOR; PLASMINOGEN ACTIVATOR INHIBITOR 1; RETEPLASE; SARUPLASE; STAPHYLOKINASE; STREPTOKINASE; TENECTEPLASE; TISSUE PLASMINOGEN ACTIVATOR; UNCLASSIFIED DRUG;

ACUTE HEART INFARCTION; ANTIGENICITY; BLEEDING; BLOOD TRANSFUSION; BRAIN HEMORRHAGE; CLINICAL TRIAL; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG SPECIFICITY; FIBRINOLYTIC THERAPY; HEART MUSCLE INJURY; HEART REINFARCTION; HUMAN; INTRAVENOUS DRUG ADMINISTRATION; META ANALYSIS; MORBIDITY; OUTCOMES RESEARCH; PRIORITY JOURNAL; REVIEW; SURVIVAL;

DRUG DESIGN; FIBRINOLYTIC AGENTS; HUMANS; METALLOENDOPEPTIDASES; MOLECULAR STRUCTURE; MYOCARDIAL INFARCTION; RANDOMIZED CONTROLLED TRIALS; RECOMBINANT PROTEINS; THROMBOLYTIC THERAPY; TISSUE PLASMINOGEN ACTIVATOR; URINARY PLASMINOGEN ACTIVATOR;

EID: 0032883289     PISSN: 0195668X     EISSN: None     Source Type: Journal    
DOI: 10.1053/euhj.1999.1659     Document Type: Review

References (41)

1. N Engl J Med. 329:1993;1615-1622.
2. Bode C, Smalling RW, Gunther B. Randomized comparison of coronary thrombolysis achieved with double-bolus reteplase (recombinant plasminogen activator) and front-loaded, accelerated alteplase (recombinant tissue plasminogen activator) in patients with acute myocardial infarction. Circulation. 94:1996;891-898.
3. N Engl J Med. 329:1993;673-682.
4. N Engl J Med. 337:1997;1118-1123.
5. N Engl J Med. 337:1997;1124-1130.
6. Lancet. 346:1995;329-336.
7. Modi NB, Eppler S, Breed J, Cannon CP, Graunwald E, Love TW. Pharmacokinetics of a slower clearing tissue plasminogen activator variant, TNK-tPA, in patients with acute myocardial infarction. Thromb Haemost. 79:1998;134-139.
8. Keyt B, Paoni NF, Refino CJ. A faster-acting and more potent form of tissue plasminogen activator. Proc Natl Acad Sci U S A. 91:1994;3670-3674.
9. DeMarco E, Rebuzzi AG, Quaranta G. Lack of procoagulant effect after TNK-plasminogen activator in patients with acute myocardial infarction. Eur Heart J. 19:1998;5.
10. Benedict CR, Refino CJ, Keyt BA. New variant of human tissue plasminogen activator (TPA) with enhanced efficacy and lower incidence of bleeding compared with recombinant human TPA. Circulation. 92:1995;3032-3040.
11. Collen D, Stassen J-M, Yasuda T. Comparative thrombolytic properties of tissue-type plasminogen activator and of a plasminogen activator inhibitor-1 resistant glycosylation variant, in a combined arterial and venous thrombosis model in the dog. Thromb Haemost. 72:1994;98-104.
12. 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. 19:1992;1071-1075.
13. Cannon CP, McCabe CH, Gibson CM. TNK-tissue plasminogen activator in acute myocardial infarction. Results of the Thrombolysis in Myocardial Infarction (TIMI) 10A Dose-Ranging Trial. Circulation. 95:1997;351-356.
14. Cannon CP, Gibson CM, McCabe CH. TNK-tissue plasminogen activator compared with front-loaded alteplase in acute myocardial infarction. Results of the TIMI 10B trial. Circulation. 98:1998;2805-2814.
15. Gibson M, Cannon CP, McCabe CH, Van de Werf FJ, Braunwald E. A randomized prospective comparison of TPA with TNK using the TIMI frame count: results of TIMI 10B. Circulation. 26:1997;I-330-I-331.
16. Gugliano RP, Cannon CP, McCabe CH, Van de Werf FJ, Braunwald E. Lower dose heparin with thrombolysis is associated with lower rates of intracranial haemorrhage: results from TIMI 10B and ASSENTI. Circulation. 96:1997;I-535.
17. Garabedian HD, Svizzero TA, Guerrero JL. A new dosing strategy for TNK variant of tissue plasminogen activator eliminates heparin and reduces bleeding without loss of thrombolytic efficacy. Circulation. 92:1995;I-740.
18. Lerakis S, Stouffer GA, Runge MS. New thrombolytics. What is under development. BioDrugs. 4:1997;24-32.
19. Liao WC, Beierle FA, Stouffer BC. Single-bolus regimen of lanoteplase (nPA) in acute myocardial infarction: pharmacokinetic evaluation from InTime-1 study. Circulation. 96:1997;260-261.
20. Ogata N, Ogata Y, Hokamaki J, Araki H, Morikami Y, Numata Y. Serial changes of PAI-1 activity in thrombolytic therapy for acute myocardial infarction. Comparison between thrombolytic therapies with lanoteplase and alteplase. Circulation. 94:1996;I-89.
21. den Heijer P, Vermeer F, Ambrosioni E. Evaluation of a weight-adjusted single bolus plasminogen activator in patients with myocardial infarction. Circulation. 98:1998;2117-2125.
22. 2-antiplasmin and fibrin. Biochim Biophys Acta. 1118:1992;144-148.
23. Collen D, Van de Werf F. Coronary thrombolysis with recombinant staphylokinase in patients with evolving myocardial infarction. Circulation. 87:1993;1850-1853.
24. Vanderschueren S, Barrios L, Kerdsinchai P. A randomized trial of recombinant staphylokinase versus alteplase for coronary artery patency in acute myocardial infarction. Circulation. 92:1995;2044-2049.
25. Vanderschueren S, Collen D, Van de Werf F. A pilot study on bolus administration of recombinant staphylokinase for coronary artery thombolysis. Thromb Haemost. 76:1996;541-544.
26. Vanderschueren S, Dens J, Kerdsinchai P. A pilot randomized coronary patency trial of double-bolus recombinant staphylokinase versus front-loaded alteplase in acute myocardial infarction. Am Heart J. 134:1997;213-219.
27. Okada K, Lijnen HR, Moreau H, Vanderschueren S, Collen D. Procoagulant properties of intravenous staphylokinase versus tissue-type plasminogen activator. Thromb Haemost. 76:1996;857-859.
28. Vanderschueren SMF, Stassen JM, Collen D. On the immunogenicity of recombinant staphylokinase in patients and in animal models. Thromb Haemost. 72:1994;297-301.
29. Collen D, Vanderschueren S, Van de Werf F. Fibrin-selective thrombolytic therapy with recombinant staphylokinase. Haemostasis. 26:1996;294-300.
30. Stringer KA. Biochemical and pharmacologic comparison of thrombolytic agents. Pharmacotherapy. 16:1996;119S-26S.
31. Lancet. i:1989;863-868.
32. Tebbe U, Michels R, Adgey J. Randomized, double-blind study comparing saruplase with streptokinase therapy in acute myocardial infarction: the COMPASS equivalence trial. J Am Coll Cardiol. 31:1998;487-493.
33. Spiecker M, Meyer J. Prourokinase for infarct therapy. Herz. 19:1994;326-335.
34. Bär FW, Meyer J, Vermeer F. Comparison of saruplase and alteplase in acute myocardial infarction. Am J Cardiol. 79:1997;727-732.
35. Bär FW. The bolus versus infusion in rescupase (saruplase) development (BIRD). Circulation. 89:1998;I-505.
36. Gardell SJ, Ramjit DR, Stabilito II. Effective thrombolysis without marked plasminemia after bolus intravenous administration of vampire bat salivary plasminogen activator in rabbits. Circulation. 84:1991;244-253.
37. Gulba DC, Bode C, Runge MS, Huber K. Thrombolytic agents - an overview. Ann Hematol. 73:1996;S9-S27.
38. Mellott MJ, Stabilito H, Holahan MA. Vampire bat salivary plasminogen activator promotes rapid and sustained reperfusion without concomitant systemic plasminogen activation in a canine model of arterial thrombosis. Arterioscler Thromb. 12:1992;212-221.
39. Montoney M, Gardell SJ, Marder VJ. Comparison of the bleeding potential of vampire bat salivary plasminogen activator versus tissue plasminogen activator in an experimental rabbit model. Circulation. 91:1995;1540-1544.
40. Witt W, Kirchhoff D, Woy P, Zierz R, Bhargava AS. Antibody formation and effects on endogenous fibrinolysis after repeated administration of DSPA alpha 1 in rats. Fibrinolysis. 8:1994;66.
41. Antman EM, Giugliano RP, Gibson MC. Abciximab facilitates the rate and extent of thrombolysis: results of TIMI 14 trail. Circulation. 99:1999;2720-2732.