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European Heart Journal 1997 18(Supplement F):11-16; doi:10.1093/eurheartj/18.suppl_F.11
Copyright © 1997 by the European Society of Cardiology.
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© 1997 The European Society of Cardiology

Pharmacological and clinical impact of the unique molecular structure of a new plasminogen activator

R. W. Smalling

Division of Cardiology, University of Texas Medical School at Houston and Hermann Heart Center, Hermann Hospital Houston, Texas, U.S.A.

Correspondence: Richard W. Smalling, MD, PhD, Division of Cardiology, UT-Houston Medical School, 6431 Fannin, MSB 1.246, Houston, TX 77030 U.S.A.

Thrombolytic therapy has been recognized as a significant improvement in the management of acute myocardial infarction. Thrombolytic agents however have been limited by short half-lives that necessitate complex administration protocols and by the potential for bleeding complications.

The native t-PA molecule has since been modified in an attempt to achieve improved lytic characteristics with less risk of bleeding.

Reteplase is a third-generation recombinant mutant of tissue-type plasminogen activator (t-PA) that is expressed in Escherichia coli cells and consists of the kringle 2 and the protease domains of t-PA. Compared with t-PA, reteplase has a lower fibrin binding, which may translate to improved clot penetration. As well as a longer half-life and a more rapid initiation of thrombolysis. Preclinical pharmacology studies have indicated that reteplase has potent in vivo thrombolytic activity and leads to rapid reperfusion; these findings have been confirmed by promising results obtained in large-scale clinical trials.

Other new agents developed by modifying the native t-PA molecule include the n-PA and the TNK mutants of t-PA. These novel, genetically modified thrombolytic agents all lyse clots better than the native t-PA; however, they differ with respect to their half-lives and fibrin-binding activity.

Although all the third-generation thrombolytic agents have shown considerable potential in improving the efficacy of thrombolytic therapy, their risk of intracranial bleeding remains problematic and is still somewhat uncertain.

Key Words: Reteplase • molecular biology • thrombolytic therapy • acute myocardial infarction


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