Bepridil is an investigational calcium channel blocking agent with antianginal activity that has a distinct and complex pharmacologic profile. Bepridil produces significant coronary vasodilation and modest peripheral effects, in addition to negative inotropic and chronotropic effects. Bepridil favorably modifies both myocardial oxygen demand and supply, supporting its use as an antianginal drug. Electrophysiologically, bepridil exhibits classes I, III, and IV antiarrhythmic activity. Five U.S. trials evaluating the short-term antianginal efficacy of bepridil collectively reported that bepridil causes significant improvement in both subjective and objective parameters of efficacy without depressing left ventricular function. In addition, one U.S. trial reported continued antianginal effects of bepridil after long-term use. There are limited data comparing and/or combining bepridil with other antianginal drugs, but the available information is promising. Limited information also exists on the use of bepridil in acute myocardial infarction and arrhythmias. Tolerance to bepridil therapy has been excellent, with the most common adverse effects being diarrhea and dizziness. It is unclear whether bepridil will be used as a first-line agent in the treatment of chronic stable angina pectoris; however, its long half-life, which makes once daily dosing possible, is certainly a significant advantage.