Platelets play a key role in thrombosis and haemostasis, which can be either beneficial or deleterious depending on the circumstance. Antiplatelet therapy is the 'cornerstone' in the prevention and treatment of thrombotic diseases. Platelet activation is a complex process known as transmembrane signaling which then serves to activate the platelet via a cascade of biochemical interactions. Currently available strategies of antiplatelet therapy are generally based on the signaling pathway of platelet activation, which possess the characters that mono-agent, mono-target, and mainly irreversible inhibition. Therefore, both established and novel antiplatelet agents have their own pros and cons and such problems as resistance, drug-drug interaction, discontinuation and monitoring, etc. have been appeared. Due to the problems existing in current antiplatelet agents, future new strategies for antiplatelet targets, agent-developing and treatment might probably include three aspects: targeting the factors associated with platelet hyperactivity, developing novel antiplatelet agents with multiple targets, mild and reversible properties from natural products, and keeping healthy lifestyle and emphasizing prevention.