Modulating bile acid pathways and TGR5 receptors for treating liver and GI diseases

被引：33

作者：

Malhi, Harmeet

Camilleri, Michael ^{[1
]}

机构：

[1] Mayo Clin, CENTER, Rochester, MN 55905 USA

来源：

CURRENT OPINION IN PHARMACOLOGY | 2017年 / 37卷

关键词：

PRIMARY BILIARY-CIRRHOSIS; PLACEBO-CONTROLLED TRIAL; IRRITABLE-BOWEL-SYNDROME; URSODEOXYCHOLIC ACID; OBETICHOLIC ACID; TRANSPORTER INHIBITOR; FUNCTIONAL CONSTIPATION; CHENODEOXYCHOLIC ACID; DIARRHEA; MULTICENTER;

D O I：

10.1016/j.coph.2017.09.008

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Bile acids are central signals in enterohepatic communication and also integrate microbiota-derived signals into this signaling axis. Discovery of the tissue distribution and signaling pathways activated by the natural receptors for bile acids, farnesoid X receptor and G protein-coupled bile acid receptor 1 (GPBAR1) also known as TGR5, and bile acid transporters has led to the development of therapeutic agents that target these molecules. Obeticholic acid, a selective FXR agonist, and NGM282, a non-mitogenic FGF-19 analog, are two of the agents in this pipeline. Obeticholic acid has been approved by regulatory agencies for use in patients with primary biliary cholangitis.

引用

页码：80 / 86

页数：7