Sible Alexandra M, Nawarskas James J
From the College of Pharmacy, University of New Mexico, Albuquerque, NM.
Cardiol Rev. 2017 May/Jun;25(3):133-139. doi: 10.1097/CRD.0000000000000142.
Antiplatelet therapy with a P2Y12 inhibitor is a key component of treatment for patients with acute coronary syndromes undergoing percutaneous coronary intervention. Before the development of cangrelor (Kengreal, The Medicines Company, Parsippany, NJ), only oral P2Y12 inhibitors were available. Cangrelor is a reversible P2Y12 inhibitor that is administered as an intravenous infusion, and its quick onset and offset make it an appealing option for antiplatelet therapy, particularly for patients who are unable to take oral medications. Although cangrelor struggled to show benefit in early trials, the positive results of the CHAMPION PHOENIX trial led to its approval for use as an adjunct to percutaneous coronary intervention to reduce the risk of periprocedural myocardial infarction, repeat coronary revascularization, and stent thrombosis in patients who have not been treated with another P2Y12 inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor. Cangrelor has also been evaluated as an option for bridging therapy in patients who must discontinue their oral P2Y12 inhibitor before coronary artery bypass grafting. This review of cangrelor will discuss its mechanism of action, its pharmacodynamics and pharmacokinetics, the clinical trial experience, and its potential place in therapy.
对于接受经皮冠状动脉介入治疗的急性冠状动脉综合征患者,使用P2Y12抑制剂进行抗血小板治疗是治疗的关键组成部分。在坎格雷洛(Kengreal,美国医药公司,新泽西州帕西帕尼)研发出来之前,只有口服P2Y12抑制剂可用。坎格雷洛是一种可逆的P2Y12抑制剂,通过静脉输注给药,其起效快和作用消失快使其成为抗血小板治疗的一个有吸引力的选择,特别是对于那些无法口服药物的患者。尽管坎格雷洛在早期试验中难以显示出益处,但CHAMPION PHOENIX试验的阳性结果导致其被批准用作经皮冠状动脉介入治疗的辅助药物,以降低未接受过另一种P2Y12抑制剂治疗且未使用糖蛋白IIb/IIIa抑制剂的患者围手术期心肌梗死、重复冠状动脉血运重建和支架血栓形成的风险。坎格雷洛也被评估为在冠状动脉旁路移植术前必须停用口服P2Y12抑制剂的患者的桥接治疗选择。本文对坎格雷洛的综述将讨论其作用机制、药效学和药代动力学、临床试验经验及其在治疗中的潜在地位。