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新型P2Y12阻滞剂

New P2Y12 blockers.

作者信息

Cattaneo M

机构信息

Unità di Medicina III, Ospedale San Paolo, Università di Milano, Milan, Italy.

出版信息

J Thromb Haemost. 2009 Jul;7 Suppl 1:262-5. doi: 10.1111/j.1538-7836.2009.03382.x.

Abstract

A number of new antiplatelet agents currently in development are anticipated to improve clinical outcomes and safety benefits in patients with acute coronary syndrome (ACS). This article reviews the pharmacology and clinical development of three of these agents: prasugrel, cangrelor, and ticagrelor. Prasugrel, a third-generation, oral thienopyridine, has been shown to be superior to clopidogrel, the current gold standard, in preventing ischemic events in patients with ACS undergoing percutaneous coronary intervention (PCI), although the bleeding rate was higher. Cangrelor, a chemical analog of adenosine triphosphate, is a potent direct platelet P2Y12 antagonist. In development as an intravenous agent, cangrelor is currently being evaluated in two phase III studies in patients requiring PCI. Ticagrelor is the first of a new class of orally available antiplatelet agents antagonizing the effects of ADP mediated by P2Y12; it is currently being studied in a phase III trial in patients with ACS.

摘要

目前正在研发的多种新型抗血小板药物有望改善急性冠状动脉综合征(ACS)患者的临床疗效和安全性。本文综述了其中三种药物的药理学及临床研发情况:普拉格雷、坎格雷洛和替格瑞洛。普拉格雷是第三代口服噻吩并吡啶类药物,在接受经皮冠状动脉介入治疗(PCI)的ACS患者中,它在预防缺血事件方面已被证明优于当前的金标准氯吡格雷,尽管出血率更高。坎格雷洛是三磷酸腺苷的化学类似物,是一种强效的直接血小板P2Y12拮抗剂。作为一种静脉用药正在进行研发,坎格雷洛目前正在两项针对需要PCI的患者的III期研究中进行评估。替格瑞洛是新型口服抗血小板药物中的首个药物,可拮抗由P2Y12介导的ADP的作用;目前正在针对ACS患者进行一项III期试验研究。

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