Table 3.

FXR ligands with potential clinical application.

Agonist	Clinical application	Comments
CDCA (Chenofalk TN)	Gallstone disease, cerebrotendinous xanthomatosis	Hepatotoxicity in rhesus monkey, but not in humans
OCA/6-ECDCA/INT-747 (semisynthetic derivative of CDCA)	PBC, NAFLD/NASH, bile acid diarrhoea, gallstone disease, portal hypertension	Beneficial in combination with UDCA (biochemically non-responders to UDCA) or as monotherapy (treatment-naïve patients) in PBC. Dose-dependent pruritus
INT-767 (synthetic derivative of OCA)	Preclinical	Preclinical: biochemical and histological improvement in MDR2−/− mouse model of sclerosing cholangitis
GW4064 (synthetic agonist)	Preclinical	Not further developed for clinical use
FXR-450/WAY-362450 (synthetic agonist)	NAFLD	Phase 1 trial in healthy Japanese men was terminated due to pharmacokinetic issues
PX-104	NAFLD	Phase 2 trial to assess the safety and tolerability in NAFLD patients