Reteplase is a recombinant plasminogen activator used primarily as a thrombolytic agent in the management of acute myocardial infarction (AMI) and acute ischemic stroke.
It is a recombinant non-glycosylated form of human tissue plasminogen activator, which has been modified to contain 357 of the 527 amino acids of the original protein.
It is produced in the bacterium Escherichia coli.
Reteplase is similar to recombinant human tissue plasminogen activator (alteplase), but the modifications give reteplase a longer half-life of 13–16 minutes.
It also binds fibrin with lower affinity than alteplase, improving its ability to penetrate into clots.
As it is able to penetrate inside the thrombi, an enhanced fibrinolytic activity will be achieved with a rapid reperfusion effect and low incidence of bleeding.
A third-generation tissue plasminogen activator (tPA) that catalyzes the conversion of plasminogen to plasmin, leading to the degradation of fibrin and subsequent thrombolysis.
Reteplase is administered as a double-bolus injection, with each bolus consisting of 10 units given 30 minutes apart.
Its dosing regimen is advantageous over other thrombolytics.
However, the GUSTO-III trial found no significant difference in 30-day mortality between reteplase and alteplase
in acute myocardial infarction.
The most common adverse event associated with reteplase is bleeding, including hemorrhagic stroke, with incidence rates similar to those of other thrombolytic agents.
Among patient with ischemic stroke treated within 4 1/2 hours after the symptom onset reteplase was more likely result in an excellent functional outcome than Alteplase (RAISE investigators).