US-based Intercept Pharmaceuticals has started a Phase I trial of INT-767, a dual farnesoid X receptor (FXR) and TGR5 agonist, to treat chronic liver diseases.
Intercept is focused on the development and commercialisation of new therapeutics to treat chronic underserved liver diseases.
INT-767 is the company’s second bile acid analog to enter clinical development. It is three times more potent than Intercept’s lead product candidate obeticholic acid (OCA).
The company noted that NT-767 also activates TGR5, a second bile acid receptor shown to affect energy metabolism, glucose homeostasis, bile composition / secretion, and inflammation.
INT-767 has demonstrated promising preclinical activity in both preventing and reversing organ damage from fibrosis.
The Phase I trial is designed to evaluate the safety and pharmacokinetics in a single ascending dose escalation phase, followed by a multiple ascending dose phase in healthy volunteers.
Intercept president and chief executive officer Mark Pruzanski said: “Advancing INT-767 into clinical development is another important milestone as we work to develop a portfolio of differentiated products to treat chronic liver diseases with high unmet medical need.
“We believe INT-767 has clinical potential based on extensive preclinical study, and we look forward to the first clinical data to guide future development.”
An agonist of the farnesoid X receptor (FXR), OCA is being developed for a variety of chronic liver diseases, including primary biliary cholangitis (PBC), nonalcoholic steatohepatitis (NASH), primary sclerosing cholangitis (PSC), and biliary atresia.
The US Food and Drug Administration (FDA) has also granted OCA breakthrough therapy designation to treat NASH with liver fibrosis, and granted OCA fast track designation to treat patients with PBC.