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首页> 外文期刊>Cardiovascular therapeutics >Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist.
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Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist.

机译：替卡格雷（Ticagrelor）：第一种可逆结合的口服P2Y12受体拮抗剂。

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Ticagrelor (AZD6140) is the first reversibly binding oral P2Y(12) receptor antagonist that blocks ADP-induced platelet aggregation. Unlike thienopyridines, which irreversibly bind to the P2Y(12) receptor for the lifetime of the platelet, ticagrelor binds reversibly to the receptor and exhibits rapid onset and offset of effect, which closely follow drug exposure levels. Animal models indicate greater separation between antithrombotic effects and bleeding effects with ticagrelor than with thienopyridines. Unlike the thienopyridines, ticagrelor does not require metabolic activation. It is quickly absorbed and exhibits a rapid antiplatelet effect, with higher and more consistent levels of inhibition of platelet aggregation (IPA) being maintained across the dosing interval than with clopidogrel. IPA levels decline with plasma drug levels after discontinuation of dosing. In the phase II DISPERSE-2 trial of 990 patients with non-ST-elevation acute coronary syndromes (ACS), ticagrelor treatment with 90 mg and 180 mg twice daily showed comparable rates of major and minor bleeding compared with clopidogrel 75 mg while there were numerically fewer myocardial infarctions. Ticagrelor resulted in greater IPA in clopidogrel-naive patients and produced substantial additional reductions in platelet aggregation activity in patients pretreated with clopidogrel. Ticagrelor treatment was well tolerated in DISPERSE-2, and discontinuation rates were comparable to those observed for clopidogrel. An increased risk of mild to moderate dyspnea and mostly asymptomatic ventricular pauses were observed in phase II studies. The mechanisms for these effects are currently being investigated. The efficacy and safety of ticagrelor are being further evaluated in the phase III PLATO trial, involving approximately 18,000 patients with ACS, including both ST-elevation and non-ST-elevation ACS.
机译：替卡格雷（AZD6140）是第一个可逆结合的口服P2Y（12）受体拮抗剂，可阻断ADP诱导的血小板凝集。与噻吩并吡啶在血小板的生命周期中不可逆地结合到P2Y（12）受体上不同，替卡格雷可逆地与受体结合并显示出快速起效和抵消作用，紧随药物暴露水平。动物模型显示，替加吡咯比噻吩并吡啶在抗血栓形成作用和出血作用之间有更大的分离。与噻吩并吡啶类不同，替卡格雷不需要代谢激活。它被迅速吸收并表现出快速的抗血小板作用，与氯吡格雷相比，在整个给药间隔中，对血小板聚集（IPA）的抑制作用保持更高，更一致的水平。停药后IPA水平随血浆药物水平下降。在990例非ST段抬高的急性冠状动脉综合征（ACS）患者的II阶段II期试验中，替卡格雷治疗组每日两次90 mg和180 mg的大，小出血发生率与氯吡格雷75 mg相当，而心肌梗死的数量减少。替卡格雷在未使用氯吡格雷的患者中导致更高的IPA，并在接受氯吡格雷预处理的患者中使血小板凝集活性进一步降低。替卡格雷治疗在DISPERSE-2中耐受性良好，停药率与氯吡格雷相当。在II期研究中观察到轻度至中度呼吸困难和大多数无症状的心室停顿的风险增加。目前正在研究产生这些作用的机制。 ticagrelor的疗效和安全性正在III期PLATO试验中进一步评估，涉及约18,000例ACS患者，包括ST抬高和非ST抬高ACS。

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