Department of Pharmacy, Methodist University Hospital, University of Tennessee College of Pharmacy, Memphis, TN 38104, USA.
Curr Vasc Pharmacol. 2010 Jan;8(1):93-101. doi: 10.2174/157016110790226615.
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.
口服抗血小板治疗在减少血管事件方面已得到广泛研究。目前可用的口服抗血小板药物包括阿司匹林和噻吩吡啶 P2Y12 受体拮抗剂。这两类药物在急性冠脉综合征和经皮冠状动脉介入治疗(PCI)中经常联合使用。对这些药物中的一种或两种产生耐药性是一个主要关注点,因为抗血小板耐药性与血栓形成事件增加和临床结局恶化有关。因此,需要更新、更有效的抗血小板药物来解决现有治疗方法的局限性。普拉格雷是一种第三代噻吩吡啶,已获得 FDA 和欧盟委员会的批准。另外两种 P2Y12 药物替卡格雷和坎格雷洛处于开发的后期阶段。普拉格雷与氯吡格雷相比可能具有的优势包括起效更快、患者间变异性降低和更强的血小板抑制作用。替卡格雷是一种口服可逆性 P2Y12 拮抗剂,与氯吡格雷相比具有更强的血小板抑制作用。坎格雷洛正在开发为一种静脉内 P2Y12 拮抗剂,具有非常快速的起始和终止作用,这在冠状动脉介入治疗中可能具有优势。这些新兴的抗血小板药物可能具有起效更快、作用更强和血小板抑制作用可逆等优势。本文总结了即将上市的 P2Y12 抗血小板药物在治疗冠状动脉疾病方面的现有临床数据。