The extraordinarily high prevalence of coronary heart disease, coupled with the alarming incidence of MI in Western society, has encouraged the investigation and development of pharmacologic agents that can be employed widely, quickly, effectively, and safely. Recombinant t-PA has played a vital role in the treatment of MI, restoring coronary arterial patency, limiting infarct size, preserving ventricular function, and improving patient survival. It has been shown to be safe when given to carefully selected patients and, although indications for clinical use have been relatively restricted, they appear to be expanding considerably. Future investigations must continue to focus on patient selection to allow treatment for all patients who would derive benefit and to establish dosing regimens and adjuvant therapies that will maximize coronary reperfusion while concomitantly limiting reocclusion and hemorrhagic complications.