Stroke is usually treated by systemic thrombolytic therapy if the patient presents within an ap-propriate time window. There is also widespread interest in the development of thrombolytic agents that can be used in cases of delayed presentation. Current agents that can be used in cases of delayed presentation of nerve damage by thrombus. Current systemic thrombolytic therapy is associated with adverse effects such as ifbrinogenolysis and bleeding. In an attempt to increase the efifcacy, safety, and speciifcity of thrombolytic therapy, a number of targeted thrombolytic agents have been studied in recent years. This review focuses on the concepts underlying targeted thrombolytic therapy and describes recent drug developments in this ifeld.