从PCSK9抑制剂Inclisiran看降脂类药物的研究进展

Research progress in lipid-lowering drugs:PCSK9 inhibitor Inclisiran

心血管事件发生率逐年上升,其中血脂异常是最常见的危险因素之一,40年前他汀类药物的问世,人类开启了血脂异常防治的新时代,但他汀类药物治疗的个体差异性、不良反应和“他汀疗效6%效应”制约着治疗效果。PCSK9的发现为控制血脂提供了新思路,两种PCSK9单克隆抗体:Alirocumab和Evocumab均已经上市,近年来应用了RNA干扰(RNAi)技术的药物——Inclisiran,也已经进入III期临床试验,本文综述了Inclisiran的药学性质和临床实验结果,以总结Inclisiran的安全性和有效性。

The incidence of cardiovascular events is increasing year by year,among which dyslipidemia is one of the most common risk factors.With the advent of statins 40 years ago,human beings have opened a new era of prevention and treatment of dyslipidemia.However,individual differences,adverse reactions and“6%effect of statins”restrict the benefits of patients.The discovery of PCSK9 provides a new idea for the control of blood lipids.Two kinds of PCSK9 monoclonal antibodies:Alirocumab and Evocumab have been listed on the market.In recent years,Inclisiran,a drug that uses RNA interference(RNAi)technology,has also entered the phase of III clinical trials.This paper reviews the pharmaceutical properties and clinical trial results of Inclisiran to show the safety and efficacy of Inclisiran.