Platelet glycoprotein Ⅱb/Ⅲa receptor antagonists could block the final common pathway of platelet aggregation and effectively inhibit platelet function, thereby they reduce no-reflow phenomenon in patients treated with percutaneous coronary intervention for acute coronary syndrome. This review summarizes platelet glycoprotein Ⅱb/Ⅲa receptor antagonist therapy in patients with acute coronary syndrome.