Reteplase has an effective half-life of 13–16 minutes and is cleared primarily by the liver and kidneys. In a controlled trial, 36 of 56 patients treated for myocardial infarction had a decrease in fibrinogen levels to below 100 mg/dL by 2 hours following the full administration of reteplase. The mean fibrinogen level returned to the baseline value by 48 hours.

Reteplase has fixed-dosing. A dose of reteplase 10 units is administer intravenously over 2 minutes. After 30 minutes, a second dose of reteplase 10 units is administered to complete the reteplase treatment.