South Australian Health and Medical Research Institute, University of Adelaide, PO Box 11050, Adelaide, SA, 5001, Australia.
Curr Cardiol Rep. 2019 Mar 4;21(4):18. doi: 10.1007/s11886-019-1103-2.
To review the clinical rationale for use of proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitors in clinical practice.
Despite widespread use of statins for lipid lowering, many patients at high cardiovascular risk continue to demonstrate unsatisfactory cholesterol levels and experience clinical events. This highlights the ongoing need to develop additional strategies to achieve more effective risk reduction in a greater number of patients. Proprotein convertase subtilisin kexin type 9 (PCSK9) plays an important role in the regulation of low-density lipoprotein metabolism. Inhibitory approaches that reduce PCSK9 activity have been demonstrated to produce substantive reductions in LDL cholesterol levels, when administered as either monotherapy or in addition to statin therapy. More recently, PCSK9 monoclonal antibodies have been reported to reduce cardiovascular event rates in large scale clinical trials. Increasing evidence suggests that PCSK9 inhibitors can produce effective lipid lowering in high risk patients. Ongoing work will identify those patients most likely to derive cost effective risk reduction with their use.
探讨前蛋白转化酶枯草溶菌素 9（PCSK9）抑制剂在临床实践中的应用的临床原理。
尽管广泛使用他汀类药物降低血脂，但许多高心血管风险的患者仍表现出不理想的胆固醇水平并发生临床事件。这突出表明，需要开发额外的策略，以使更多的患者能够更有效地降低风险。前蛋白转化酶枯草溶菌素 9（PCSK9）在调节低密度脂蛋白代谢中发挥重要作用。当作为单药治疗或与他汀类药物联合使用时，已证明抑制 PCSK9 活性的方法可显著降低 LDL 胆固醇水平。最近，PCSK9 单克隆抗体已在大规模临床试验中报告可降低心血管事件发生率。越来越多的证据表明，PCSK9 抑制剂可使高危患者有效降低血脂。正在进行的工作将确定那些最有可能通过使用 PCSK9 抑制剂获得成本效益风险降低的患者。
