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[Anistreplase. Pharmacology and biological data].

¹Laboratoire central d'hématologie et d'immunologie, Hôtel-Dieu de Paris.

Archives Des Maladies Du Coeur Et Des Vaisseaux

|February 1, 1990

Summary

Anistreplase, a novel thrombolytic, offers improved administration and reduced side effects compared to older agents. Its unique properties enhance clot penetration and retention, demonstrating effectiveness in clinical trials.

Area of Science:

Pharmacology
Cardiovascular Medicine
Biochemistry

Background:

Anistreplase is a second-generation thrombolytic agent.
It is an equimolecular complex of streptokinase and lys-plasminogen, with a temporarily blocked active site.

Purpose of the Study:

To describe the properties and potential benefits of anistreplase as a thrombolytic agent.
To highlight its advantages over existing thrombolytic therapies.

Main Methods:

Anistreplase is administered via bolus intravenous injection.
Its pharmacokinetic profile, including deacylation and elimination half-lives, was characterized.
In vitro studies assessed its fibrin affinity compared to t-PA.
Effectiveness was evaluated in animal models and clinical trials.

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Main Results:

Acylation allows for rapid administration and protection against inhibitors, resulting in a 90-minute plasma elimination half-life.
Slow deacylation (105 minutes) prolongs action within the thrombus and reduces reocclusion risk.
Lys-plasminogen enhances fibrin affinity, leading to greater thrombus accumulation.
Anistreplase demonstrated pronounced fibrinogenolysis in myocardial infarction doses and showed effectiveness in trials.

Conclusions:

Anistreplase offers a favorable pharmacokinetic profile and enhanced fibrin affinity.
Its properties suggest reduced hypotensive effects and lower reocclusion rates.
Clinical trials support its effectiveness as a thrombolytic agent.