非他汀类药物在家族性高胆固醇血症的研究新进展

Drugs beyond stains for management of familial hypercholesterolemia

家族性高胆固醇血症是一种常见的遗传性疾病,为心血管事件发生的高危因素之一,但是目前常用的他汀类及依折麦布等仍不能使家族性高胆固醇血症患者达到目标低密度脂蛋白水平。因此,开发新一代降脂药物具有重要的临床价值。本文对目前正在研发的7种新的降脂药物,包括酰基辅酶A-胆固醇酰基转移酶(ACAT)抑制剂、三酰甘油转运蛋白(MTP)抑制剂、反义寡核苷酸、胆固醇转运蛋白(CETP)抑制剂、前蛋白转化酶枯草杆菌蛋白酶kexin-9(PCSK9)抑制剂、甲状腺受体激动剂和角鲨烯合成酶抑制剂进行综述。

Familial hypercholesterolemia（ FH） is an inherited condition resulting in increased risk of premature cardiovascular diseases. Despite the considerable reduction of LDL level by stains or ezetimibe,the majority of FH individuals still do not reach the LDL treatment targets. This review will provide a comprehensive overview of novel therapies to lower LDL-C in FH,including ACAT inhibitors,apo B mRNA antisence drugs,CETP inhibitors,MTP inhibitors,PCSK9 inhibitors,squalence synthase inhibitors,and thyroxin receptor agonists.