Tirofiban is a non-
peptide selective
glycoprotein (
GP) IIb/IIIa receptor inhibitor that reversibly inhibits
fibrinogen-dependent platelet aggregation and subsequent formation of thrombi, which contribute to the major atherosclerotic complications in the development, progression, and resolution of
ischemic stroke. The adjunctive use of
tirofiban has been extensively evaluated in progressive
stroke, combined intravenous thrombolysis (IVT), and endovascular treatment (EVT) in both preclinical and clinical studies. A body of evidence has been accumulated on the risks and benefits associated with
tirofiban in terms of prevention of
stroke progression,
stent thrombosis, improvement in functional independence, and mortality, especially among high-risk
ischemic stroke patients as a further strategy alongside conventional treatment. In general,
tirofiban has a favorable tolerability and efficacy profile in the improvement of vascular recanalization and long-term functional outcome, although the optimum dosage, application setting, and precise target patients are not yet well-established. However, its specific inhibition of ongoing platelet aggregation and
thrombus formation rather than absolute thrombolysis suggests that
tirofiban, one of the most widely used
GP IIb/IIIa inhibitors, with high affinity and a short plasma/
biologic half-life, may have great potential in the acute treatment of
ischemic stroke. Substantial practical progress is likely as our understanding of the mechanism of action and pharmacological actions of
tirofiban in atherosclerotic ischemic disease improves. Therefore, we classify and summarize the available findings regarding
tirofiban in
acute ischemic stroke to stimulate and guide further research and clinical practice.