Recent advances in antiplatelet agents.
Platelet aggregation plays a key role in the pathogenesis of thromboembolic diseases such as myocardial infarction, stroke, unstable angina and peripheral artery disease. Until recently, aspirin was the only antiplatelet agent available to prevent or treat these events. Over the past several years, there has been a substantial expansion in the antiplatelet armamentarium as well as in the understanding of the clinical importance of antiplatelet therapy in limiting the complications of thrombosis. Aspirin was one of the first agents to be adopted and it remains as the standard therapy with the higher amount of available clinical information. Following aspirin, ADP receptor antagonists like ticlopidine and clopidogrel as well as phosphodiesterase inhibitors dipyridamole and cilostazol have been introduced. Glycoprotein (GP) IIb/IIIa receptor antagonists like eptifibatide, tirofiban and abciximab are the newer antiplatelet agents which act at the end of the common pathway of platelet aggregation. Although results of clinical studies with the first oral GPIIb/IIIa antagonists were disappointing, agents of the new generation might expand the potential application of GPIIb/IIIa targeted therapy. This review will highlight recent advances in the development of aspirin, phosphodiesterase inhibitors, ADP receptor antagonists and the platelet glycoprotein IIb/IIIa inhibitors. The emphasis of this paper has been placed on the chemical aspects of these agents.
Dogne
Jean-Michel
JM
Department of Medicinal Chemistry, University of Li ge, 1, av. de l H pital, B36 Sart-Tilman, Liege, 4000 Liege, Belgium. Jean-Michel.Dogne@ulg.ac.be
de Leval
Xavier
X
Benoit
Patricia
P
Delarge
Jacques
J
Masereel
Bernard
B
David
Jean-Louis
JL
D000818:Animals; D002317:Cardiovascular Agents / Q000737:chemistry / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D015195:Drug Design; D006801:Humans; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry* / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
D002317:Cardiovascular Agents; D010975:Platelet Aggregation Inhibitors