Department of Neurology, Beijing Tiantan Hospital, Capital Medical University, No. 119 Nan Sihuan West Road, Fengtai District, Beijing, 100160, People's Republic of China.
Department of Interventional Neurology, Beijing Tiantan Hospital, Capital Medical University, Beijing, People's Republic of China.
Drugs. 2019 Apr;79(5):515-529. doi: 10.1007/s40265-019-01078-0.
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.
替罗非班是一种非肽类选择性糖蛋白（GP）IIb/IIIa 受体抑制剂，可可逆地抑制纤维蛋白原依赖性血小板聚集和随后血栓的形成，这有助于缺血性中风发展、进展和缓解过程中的主要动脉粥样硬化并发症。在进展性中风、联合静脉溶栓（IVT）和血管内治疗（EVT）的临床前和临床研究中，已经广泛评估了替罗非班的辅助应用。已经积累了大量证据，涉及替罗非班在预防中风进展、支架内血栓形成、改善功能独立性和死亡率方面的风险和益处，特别是在高风险缺血性中风患者中，作为常规治疗之外的进一步策略。一般来说，替罗非班在改善血管再通和长期功能结局方面具有良好的耐受性和疗效，尽管最佳剂量、应用场景和精确的目标患者尚未得到充分确立。然而，其对正在进行的血小板聚集和血栓形成的特定抑制而不是绝对溶栓表明，替罗非班作为最广泛使用的 GP IIb/IIIa 抑制剂之一，具有高亲和力和较短的血浆/生物半衰期，在急性缺血性中风的治疗中可能具有很大的潜力。随着我们对替罗非班在动脉粥样硬化性缺血性疾病中的作用机制和药理学作用的理解的提高，可能会取得实质性的实际进展。因此，我们对急性缺血性中风中替罗非班的现有发现进行分类和总结，以激发和指导进一步的研究和临床实践。
