Acute ischemic stroke （AIS） is a clinical syndrome of neurological impairment caused by cerebral ischemia and hypoxia， and antiplatelet therapy is the basis for the prevention and treatment of ischemic stroke. At present， endovascular treatment methods for AIS include mechanical thrombectomy， thrombus aspiration， intra-arterial thrombolysis， and stent implantation， which can effectively improve blood flow and clinical symptoms； however， endovascular treatment may damage vascular endothelial cells， leading to platelet aggregation and thrombosis. The use of antiplatelet agents in the perioperative period of endovascular therapy is a common treatment method to reduce the complications such as thrombosis， embolism， and ischemia during and after surgery. In recent years， the latest reports on the use of antiplatelet agents in the endovascular treatment of AIS， especially platelet glycoprotein （GP） IIb/IIIa receptor antagonists， have given rise to promising prospects for the development of the endovascular treatment of AIS. There are currently three GP IIb/IIIa inhibitors that have been released by the US Food and Drug Administration， i.e.， tirofiban， abciximab， and eptifibatide. Tirofiban is a GP IIb/IIIa receptor antagonist mainly used in China， and since GP IIb/IIIa receptor acts as the final pathway for platelet aggregation and thrombosis， its antagonist exerts an antiplatelet aggregation effect rapidly by directly binding to GP IIb/IIIa receptor. As a novel antiplatelet drug， tirofiban has been basically used in cardiovascular diseases， but its application in cerebrovascular diseases is still in the exploratory stage， with controversies over its specific usage， dosage， and safety， and such use is off-label use. This article reviews the application of tirofiban in the endovascular treatment of AIS and related research advances.