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.

前蛋白转化酶枯草杆菌蛋白酶/kexin 9 型 (PCSK9) 与低密度脂蛋白 (LDL) 受体相互作用，通过增强其降解，在调节胆固醇稳态中起关键作用。两种靶向 PCSK9 的完全人源化单克隆抗体 evolocumab 和 alirocumab 可用于临床。与他汀类药物联合使用时，PCSK9 抑制剂比依折麦布降低 30% 以上的 LDL-C，比安慰剂多 60%。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，人们对这些药物的成本效益提出了质疑。在本文中，我们回顾了使用 PCSK9 抑制剂降低 LDL-C 的临床证据及其对脑血管健康的影响。