University of Illinois College of Medicine, Department of Neurology and Rehabilitation, 912 S Wood St, Chicago, IL, United States.
J Stroke Cerebrovasc Dis. 2021 Nov;30(11):106057. doi: 10.1016/j.jstrokecerebrovasdis.2021.106057. Epub 2021 Aug 24.
Proprotein convertase subtilisin/kexin type 9 (PCSK9) interacts with the low-density lipoprotein (LDL) receptor and, by enhancing its degradation, has a pivotal role in the regulation of cholesterol homeostasis. Two fully humanized monoclonal antibodies targeting PCSK9, evolocumab and alirocumab, are available for clinical use. PCSK9 inhibitors reduce LDL-C 30% more than ezetimibe and 60% more than placebo when added to statins. This reduction in LDL-C is accompanied by a decrease in the risk of major cardiovascular and cerebrovascular events. However, questions have been raised in relation to the cost-effectiveness of these medications. In this article, we review the clinical evidence on the use of PCSK9 inhibitors in lowering LDL-C and their effect on cerebrovascular health.
前蛋白转化酶枯草溶菌素 9(PCSK9)与低密度脂蛋白(LDL)受体相互作用,并通过增强其降解,在胆固醇稳态的调节中起关键作用。两种针对 PCSK9 的全人源化单克隆抗体,依洛尤单抗和阿利西尤单抗,可用于临床。当与他汀类药物联合使用时,PCSK9 抑制剂可使 LDL-C 降低 30%,比依折麦布多 60%,比安慰剂多 60%。这种 LDL-C 的降低伴随着主要心血管和脑血管事件风险的降低。然而,这些药物的成本效益问题引起了人们的关注。在本文中,我们回顾了 PCSK9 抑制剂在降低 LDL-C 方面的临床证据及其对脑血管健康的影响。