Given the few options that are currently available for patients following ischemic stroke, the search for novel therapeutic approaches becomes more critical. Pharmaceutical intervention strategies for the treatment of stroke include preventative (prophylactic or stroke pretreatment), neuroprotective (early acute post-stroke treatment) and regenerative (delayed post-stroke treatment for long-term benefit) therapeutic approaches. Experimental evidence has suggested that the majority of stroke patients have a slow evolution of brain injury that occurs over several hours. This 'evolving stroke' may ultimately be a realistic target for therapeutic intervention, with the goal of inhibiting the progression of detrimental changes that normally follow the acute ischemic event. Preventing or reducing this delayed cellular injury may improve neurological outcome and also facilitate brain recovery from injury. Significant impact on stroke can be expected as additional research is conducted on biological targets or processes important in facilitating the brain's regenerative capacity following cellular/tissue loss. This review provides updates on stroke prevention therapies (anticoagulant and antiplatelet), the advances in the development of pharmacological agents that target the acute phase of stroke (thrombolytics and neuroprotective drugs), and newly evolving approaches that may facilitate brain regeneration (i.e., neurobehavioral recovery) following brain damage.