Reteplase: a new thrombolytic for the treatment of acute myocardial infarction

• Published in: Annals of Pharmacotherapy 1999-03, Vol.33 (3), p.318-324
• Main Authors: Wooster, MB, Luzier, AB
• Format: Article
• Language: English
• Subjects: Biological and medical sciences; Blood. Blood coagulation. Reticuloendothelial system; Clinical Trials as Topic; Fibrinolytic Agents - pharmacology; Fibrinolytic Agents - therapeutic use; Humans; Medical sciences; Myocardial Infarction - drug therapy; Pharmacology. Drug treatments; Plasminogen Activators - pharmacology; Plasminogen Activators - therapeutic use; Recombinant Proteins - pharmacology; Recombinant Proteins - therapeutic use; Tissue Plasminogen Activator
• ISSN: 1060-0280; 1542-6270
• DOI: 10.1345/aph.18006

OBJECTIVE: To summarize the published data on reteplase, the most recent thrombolytic agent approved by the Food and Drug Administration for use in the management of acute myocardial infarction in adults. DATA SOURCES: Published data on reteplase identified by MEDLINE searches (January 1985–June 1997), as well as other pertinent literature. DATA SYNTHESIS: Reteplase is a new thrombolytic agent derived from human tissue plasminogen activator. Its mechanism of action is similar to that of alteplase, but it differs in pharmacokinetic and pharmacodynamic properties. Certain structural changes contribute to differences in pharmacokinetic properties such as a prolonged half-life (15 min), which allows it to be administered as two 10-MU bolus injections. Reteplase has been shown to have fibrin specificity similar to that of alteplase, but with a lower binding affinity for fibrin. This enables reteplase to bind to the thrombus repeatedly and increases its fibrinolytic potential. In clinical trials, reteplase demonstrated more rapid and complete coronary patency compared with alteplase, without a significant increase in clinical adverse events. However, the improvement in coronary artery patency with reteplase versus alteplase did not result in a reduction in mortality in the GUSTO III trial. CONCLUSIONS: Despite evidence that use of reteplase results in an improved coronary artery patency rate versus accelerated infusion alteplase, an improvement in mortality rate with reteplase was not shown. Reteplase may have an advantage over alteplase due to a more rapid and simpler dosing regimen, but the significance of this difference is yet to be determined.