Tropifexor is an investigational drug that acts as an agonist of the farnesoid X receptor (FXR).

[1] It was developed for the treatment of cholestatic liver diseases and nonalcoholic steatohepatitis (NASH).

In combination with cenicriviroc, a CCR2 and CCR5 receptor inhibitor, it is undergoing a phase II clinical trial for NASH and liver fibrosis.

[2] Rats treated orally with tropifexor (0.03 to 1 mg/kg) showed an upregulation of the FXR target genes, BSEP and SHP, and a down-regulation of CYP8B1.

The patent that covers tropifexor and related compounds was published in 2010.