Platelets play a major role in normal hemostatic and thrombotic processes. Aggregation of platelets presents the key pathophysiological step in the development of cardiovascular diseases; hence, antiplatelet agents remain crucial in the treatment of cardiovascular diseases. They may target the three principal phases leading to thrombogenesis, including platelet adhesion, activation, and aggregation. This review presents an overview of the currently available antiplatelet agents, with a particular focus on their targets, pharmacological properties, and limitation of use.