Table 2. Bile Acids and FXR agonists: Current Clinical Status.

Clinically approved treatments that involve bile acid sequestrants, bile acids or specific FXR agonists are listed, together with their target disease and real or potential beneficial effect. Where noted, FXR agonists are in phase I-III clinical trials. LDL, low density lipoprotein; LDLR, LDL receptor.

Compound	Clinical Status	Target	Target Disease	Effect
Bile Acid (BA) Sequestrant	Approved	Increased BA excretion	Hyperlipidemia	Increased hepatic LDLR Decreased plasma LDL
			Type 2 Diabetes	Increased insulin sensitivity
Cholic Acid	Approved	Provide bile acids (BAs) for lipid absorption	Inborn errors of BA metabolism that inhibit BA synthesis	Increased lipid absorption Improved liver function
CDCA	Approved	Replacement BA	Cerebrotendinous xanthomatosis	Reduce endogenous BA synthesis
UDCA	Approved	Gallstone dissolution	Gallstones	Solubilize cholesterol gallstones
UDCA	Approved	Liver	Primary biliary cirrhosis (PBC)	Improved liver function
INT-747 (6-ECDCA; Obeticholic Acid/OCA)	Phase III (2011)	FXR	Type 2 Diabetes	Improved insulin sensitivity
OCA	Phase I (2011)	FXR	Non-alcoholic steatohepatitis (NAFLD)	Improved insulin sensitivity Improved liver function
OCA	Phase III (2011)	FXR	PBC	Improved liver function
PX-102	Phase I (2011)	FXR	Metabolic Syndrome NAFLD	Improved insulin sensitivity Improved liver function
nor-UDCA	Phase I (2011)	Liver	Sclerosing cholangitis	Improved liver function