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血小板P2Y12拮抗剂的过去与未来简述。

A brief review of the past and future of platelet P2Y12 antagonist.

作者信息

Barn Kulpreet, Steinhubl Steven R

机构信息

Geisinger Medical Center, Danville, Pennsylvania 17822, USA.

出版信息

Coron Artery Dis. 2012 Sep;23(6):368-74. doi: 10.1097/MCA.0b013e3283564930.

Abstract

ADP plays a pivotal role in localized platelet activation and recruitment, and, with that, in the maintenance of thrombus integrity, making it a suitable target for the control of intravascular thrombosis. The limited distribution of one of its receptors, the P2Y12 receptor, primarily to platelets makes it an especially attractive pharmacologic target. For the last several decades the thienopyridine family of P2Y12 antagonists have provided the vast majority of clinical data confirming the clinical benefit of selective P2Y12 inhibition. Recently, new thienopyridine plus nonthienopyridine P2Y12 antagonists have become available or are being studied that will further improve our treatment of patients with coronary disease.

摘要

二磷酸腺苷(ADP)在局部血小板激活和募集过程中发挥关键作用,进而在维持血栓完整性方面发挥作用,使其成为控制血管内血栓形成的合适靶点。其一种受体,即P2Y12受体,主要局限于血小板分布,这使其成为一个特别有吸引力的药理学靶点。在过去几十年里,噻吩并吡啶类P2Y12拮抗剂提供了绝大多数临床数据,证实了选择性P2Y12抑制的临床益处。最近,新型噻吩并吡啶类加非噻吩并吡啶类P2Y12拮抗剂已可供使用或正在研究中,这将进一步改善我们对冠心病患者的治疗。

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