Bile acids: From acient Chinese medicines to modern treatments
In 1999 the landscape evolved further when, bile acids and bile salts were shown to have hormonal activity as bile acid/salts were confirmed to be the endogenous ligand of the nuclear receptor FXR (Farnesoid X Receptor). FXR is widely expressed in high levels in the intestine and the liver and it regulates bile acid homeostasis and is a critical regulator of lipids and glucose homeostasis. During liver injury FXR has been shown to play an anti-inflammatory and anti-fibrosis role and so it is a target for conditions such as PBC, PSC and NASH. A novel bile acid analogue of chenodeoxychlolic acid, Obeticholic acid has been developed and approved for the treatment of PBC for patients who do not respond to UDCA and it’s currently in phase III clinical development for NASH, where there is a large and growing unmet medical need.