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首页> 外文期刊>Current vascular pharmacology >Emerging P2Y12 receptor antagonists: role in coronary artery disease.
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Emerging P2Y12 receptor antagonists: role in coronary artery disease.

机译:新兴的P2Y12受体拮抗剂:在冠状动脉疾病中的作用。

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The use of oral antiplatelet therapy in reducing vascular events has been extensively studied. Currently available oral antiplatelet agents include aspirin and the thienopyridine P2Y12 receptor antagonists. These classes are combined frequently in the setting of acute coronary syndrome and percutaneous coronary intervention (PCI). Resistance to either or both of these agents is a major concern, as antiplatelet resistance has been linked to an increase in thrombotic events and worse clinical outcomes. As a result, there is a need for newer, more effective antiplatelet agents to address the limitations of currently available therapy. Prasugrel, a third generation thienopyridine, has been approved by both the FDA and European Commission. Two additional P2Y12 agents, ticagrelor and cangrelor are in advanced stages of development. The possible advantages of prasugrel over clopidogrel include a faster onset of action, reduced inter-patient variability and more potent platelet inhibition. Ticagrelor is an oral reversible P2Y12 antagonist with greater platelet inhibition compared with clopidogrel. Cangrelor is being developed as an intravenous P2Y12 antagonist with a very fast onset and offset, which may offer advantages particularly in the setting of coronary intervention. These emerging antiplatelet agents may offer advantages such as faster onset of action, greater potency and reversibility of platelet inhibition. This article summarizes the available clinical data on the upcoming P2Y12 antiplatelet agents in the treatment of coronary artery disease.
机译:口服抗血小板疗法在减少血管事件方面的用途已得到广泛研究。当前可用的口服抗血小板药包括阿司匹林和噻吩并吡啶P2Y12受体拮抗剂。这些类别在急性冠状动脉综合征和经皮冠状动脉介入治疗(PCI)的情况下经常结合使用。对这两种药物中任何一种或两种药物的耐药性是一个主要问题,因为抗血小板耐药性与血栓形成事件的增加和临床预后差有关。结果,需要更新的,更有效的抗血小板药来解决当前可用疗法的局限性。第三代噻吩并吡啶类普拉格雷(Prasugrel)已获得FDA和欧盟委员会的批准。两种其他的P2Y12剂替卡格雷或坎格雷洛处于研发的晚期阶段。普拉格雷优于氯吡格雷的可能优点包括起效更快,患者间变异性降低和更有效的血小板抑制作用。替卡格雷洛是一种口服可逆P2Y12拮抗剂,与氯吡格雷相比具有更大的血小板抑制作用。 Cangrelor正在被开发为起效快,起效快的静脉内P2Y12拮抗剂,尤其在冠状动脉介入治疗方面可能具有优势。这些新兴的抗血小板药可提供诸如起效更快,效力更高和血小板抑制可逆的优点。本文总结了即将到来的P2Y12抗血小板药物在冠心病治疗中的可用临床数据。

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