摘要
对于非酒精性脂肪肝炎(NASH)的治疗,目前全球只有一种药物——Saroglitazar被批准上市,治疗手段极度缺乏。核受体法尼酯衍生物X受体(FXR)激动剂能有效降低肝脏脂质的累积,降低肝脏的炎症发生,具有成为治疗NASH药物的潜能。目前全球进入临床研究阶段的针对NASH适应证的FXR激动剂只有6种(Obeticholic acid、EDP-305、Cilofexor、Tropifexor、LMB763、PXL007),该文对这6种化合物进行药理学研究方面的综述,以期为开发以FXR为靶标的治疗NASH药物提供参考。
The treatment of non-alcoholic steatohepatitis(NASH)is extremely lacking,there is only one approved drug in the world,Saroglitazar.The Farnesoid X receptor(FXR)agonist can effectively reduce the accumulation of lipids and the inflammation in the liver,which has the potential to be a drug for the treatment of NASH.At present,there are only 6 FXR agonists for NASH indications(obeticholic acid,EDP-305,cilofexor,tropifexor,LMB763,PXL007)that have entered the clinical research stage globally.This article reviewed the pharmacological research of these 6 compounds to provide a basis for the development of NASH drugs targeting FXR.
作者
向岑
高凤
孔祥舜
刘江
李明媛
袁媛
滕玉鸥
XIANG Cen;GAO Feng;KONG Xiangshun;LIU Jiang;LI Mingyuan;YUAN Yuan;TENG Yuou(College of Biotechnology,Tianjin University of Science and Technology,Tianjin 300457,China)
出处
《医药导报》
CAS
北大核心
2021年第5期645-650,共6页
Herald of Medicine