前蛋白转化酶枯草溶菌素9（PCSK9）抑制作用的当前证据及未来方向
Current Evidence and Future Directions of PCSK9 Inhibition.
作者信息
Xu Jiaqian, Shapiro Michael D
机构信息
Center for the Prevention of Cardiovascular Disease, Section on Cardiovascular Medicine, Wake Forest University Baptist Medical Center Winston Salem, NC.
出版信息
US Cardiol. 2021 Feb 16;15:e01. doi: 10.15420/usc.2020.17. eCollection 2021.
Recent scientific and therapeutic advances in proprotein convertase subtilisin kexin type 9 (PCSK9) inhibition have opened a chapter in the management of hypercholesterolemia, especially in patients who are inadequately controlled on or intolerant to statins. The two PCSK9 monoclonal antibodies, evolocumab and alirocumab, reduce LDL cholesterol by 60% and improve cardiovascular outcomes when taken in addition to statin therapy. More recently, inclisiran, a silencing RNA (siRNA) that inhibits translation of PCSK9 mRNA, demonstrated LDL cholesterol reduction by 45-50% with the advantage of dramatically reduced dose frequency. Other modes of PCSK9 inhibition include small molecule antagonists, vaccines, CRISPR gene editing, and antagonism at various steps of translation, and post-translational processing.
前蛋白转化酶枯草溶菌素9型（PCSK9）抑制方面的最新科学与治疗进展为高胆固醇血症的管理开启了新篇章，尤其是对于那些使用他汀类药物控制不佳或不耐受的患者。两种PCSK9单克隆抗体，依洛尤单抗和阿利西尤单抗，在他汀类药物治疗基础上加用后可使低密度脂蛋白胆固醇降低60%，并改善心血管结局。最近，一种抑制PCSK9 mRNA翻译的小干扰RNA（siRNA）药物inclisiran，可使低密度脂蛋白胆固醇降低45%-50%，且具有显著降低给药频率的优势。PCSK9抑制的其他方式包括小分子拮抗剂、疫苗、CRISPR基因编辑，以及在翻译和翻译后加工的各个步骤进行拮抗。
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