Mount Sinai School of Medicine, New York, New York, USA.
Curr Opin Lipidol. 2010 Dec;21(6):473-80. doi: 10.1097/MOL.0b013e32833eb581.
Selective inhibitors of secretory phospholipase A2 and lipoprotein-associated phospholipase A2 are potential candidates for reducing recurrent cardiovascular events in patients with established coronary heart disease (CHD). With the active enrollment of CHD patients into phase III clinical trials with both classes of inhibitors, this article reviews the available experimental animal and human trial evidence that provides the rationale for the development of the phospholipase A2 inhibitors varespladib methyl and darapladib as preventive therapy.
Recently completed experimental animal studies, human biomarker data, and vascular imaging studies provide support for proceeding with clinical outcome trials secretory phospholipase A2 and lipoprotein-associated phospholipase A2 inhibition.
Both secretory phospholipase A2 and lipoprotein-associated phospholipase A2 inhibitors hold promise for the reduction of recurrent cardiovascular events in patients treated with current standards of care. The completion of the ongoing clinical event trials has the potential to provide a new dimension to secondary preventive therapy.
选择性分泌型磷脂酶 A2 和脂蛋白相关磷脂酶 A2 抑制剂有可能降低已确诊冠心病患者的心血管事件复发率。随着这两类抑制剂的冠心病患者都被积极纳入 III 期临床试验，本文就现有的实验动物和人体试验证据进行综述，为磷脂酶 A2 抑制剂瓦雷昔帕和达拉昔帕的开发提供预防治疗的理论依据。
最近完成的动物实验研究、人体生物标志物数据和血管成像研究为进行分泌型磷脂酶 A2 和脂蛋白相关磷脂酶 A2 抑制的临床转归试验提供了支持。
分泌型磷脂酶 A2 和脂蛋白相关磷脂酶 A2 抑制剂均有望降低接受现有治疗标准的患者的心血管事件复发率。正在进行的临床事件试验的完成有可能为二级预防治疗提供新的维度。
