School of Biotechnology, National Institute of Technology Calicut, Calicut-673601, Kerala, India.
Curr Pharm Des. 2012;18(12):1625-34. doi: 10.2174/138161212799958558.
P2Y12 receptor mediated inhibition of platelet aggregation is one of the most explored and exploited pathways in antiplatelet drug therapy to prevent ischemic events in patients undergoing percutaneous coronary intervention (PCI) for the treatment of the acute coronary syndrome (ACS). Ticlopidine, Clopidogrel, Prasugrel, Ticagrelor, Cangrelor and Elinogrel are the P2Y12 inhibitors that act as antiplatelet drugs. In this review, the features of these drugs and the factors reported to be responsible for drug resistance or drug ineffectiveness were described. The features like drug metabolism, reversible or irreversible binding of drugs to their target protein and the mode of administration were observed to evolve along with the antiplatelet drugs. These features also include the drug-drug interactions, the pharmacogenetics and pharmacodynamics of P2Y12 inhibitors. We attempted to critically analyze how the desirable features were met by the P2Y12 inhibitors in the course of time. This review provides an overview of the evolution of P2Y12 inhibitors and may guide the researchers to develop better antiplatelet drugs in the future.
P2Y12 受体介导的血小板聚集抑制是经皮冠状动脉介入治疗（PCI）治疗急性冠脉综合征（ACS）患者预防缺血事件的抗血小板药物治疗中研究和应用最多的途径之一。噻氯匹定、氯吡格雷、普拉格雷、替格瑞洛、坎格瑞洛和依替巴肽是作为抗血小板药物的 P2Y12 抑制剂。在这篇综述中，描述了这些药物的特征以及报告的导致耐药或无效的因素。药物代谢、药物与靶蛋白的可逆或不可逆结合以及给药方式等特征都随着抗血小板药物的发展而演变。这些特征还包括药物-药物相互作用、P2Y12 抑制剂的药物遗传学和药效学。我们试图批判性地分析 P2Y12 抑制剂在一段时间内如何满足这些理想特征。本综述概述了 P2Y12 抑制剂的发展历程，并可能为未来研究人员开发更好的抗血小板药物提供指导。
