Aspirin, which has been the mainstay of antiplatelet agent for many decades, affects a single pathway in the platelet activation process and provides incomplete protection against cardiovascular events. Aspirin also may blunt the hemodynamic effect of angiotensin-converting enzyme inhibitors. Dipyridamole may provide some additional benefit, but there is little evidence to suggest its superiority alone or in combination with aspirin compared to standard doses of aspirin. Oral platelet glycoprotein IIb/IIIa inhibitors, although initially promising, have had disappointing results in recent clinical studies. A new class of medications, the thienopyridines, blocks the activity of platelet adenosine 5'-diphosphate (ADP) receptors, thereby reducing platelet activation. This review discusses the pharmacology, clinical studies, and potential uses of these agents, which include ticlopidine and clopidogrel. ADP inhibitors, by blocking an alternate pathway of platelet activation, are slightly more effective than aspirin in reducing cardiovascular events.