Disclosed is the use of tenecteplase in the preparation of a medicament for treating acute ischemic stroke in a human, the treatment regime comprising administering tenecteplase to the human in a total dose of about 0.05 to 0.5 mg/kg, given as an initial bolus dose of about 0.05 to 0.15 mg/kg, followed by infusion of an amount equaling the total dose minus the initial dose over a period of about 50-90 minutes.