奥贝胆酸治疗非酒精性脂肪肝的疗效和机制——胆汁酸药物的利和弊

Efficacy and mechanisms of obeticholic acid in treatment of non-alcoholic fatty liver disease:pros and cons of bile acid drugs in non-alcoholic fatty liver disease

非酒精性脂肪肝(NAFLD)是世界上发病率最高的肝病,但是目前无批准上市治疗NAFLD的药物。近年来,NAFLD被认为是代谢相关性脂肪肝病,其发病机制与胆汁酸代谢的改变有关。奥贝胆酸是一种半合成的胆汁酸,同时也是一种强效且具有高选择性的法尼醇X受体(FXR)激动剂和脂肪酸转运蛋白5(FATP5)的强效抑制剂。目前,与高剂量熊去氧胆酸(UDCA)和其他胆汁酸药物治疗NAFLD相比,小剂量奥贝胆酸在治疗NAFLD中具有更多的优势和探索价值。

Non-alcoholic fatty liver disease(NAFLD)is the most common liver disease in the world,but there are currently no approved drugs for the treatment of NAFLD.In recent years,NAFLD has been considered as metabolic associated fatty liver disease,and the pathogenesis of NAFLD is related to changes in bile acid metabolism.Obeticholic acid is a semi-synthetic bile acid and a potent and highly selective farnesoid X receptor(FXR)agonist,as well as a potent inhibitor of fatty acid transport protein 5(FATP5).At present,compared with high-dose ursodeoxycholic acid(UDCA)and other bile acid drugs in the treatment of NAFLD,low-dose obeticholic acid has more advantages and exploration value in the treatment of NAFLD.