Stroke is severe neurological disorder characterized by interruption of blood circulation into the brain and the leading cause of serious long-term disability. The central goal of therapy in ischemic stroke is to preserve tissue in the ischemic penumbra, where perfusion is decreased but sufficient to stave off infarction. Therefore, the fundamental treatment of AIS relies on prompt recanalisation and reperfusion of the threatened, but potentially salvageable, ischemic penumbra. Intravenous (iv) thrombolysis with recombinant tissue plasminogen activator (rtPA) remains the current strategy. However, other thrombolysis is underused, owing to various exclusion criteria that limit the number of treated patients. Other thrombolytics are under investigation. Intra-arterial thrombolysis and mechanical thrombectomy devices is also increasingly applied. This review analyses the current status and the problem of the pharmacological treatment of acute ischemic stroke.