DISCOVERY COMPOUNDS

We, together with our collaborators, have discovered other bile acid chemistry-based compounds that are in earlier stages of screening, research and development.*

INT-767: an orally administered dual agonist of the farnesoid X receptor (FXR) and TGR5 receptor. TGR5 is a G-protein coupled bile acid receptor.

• INT-767 is Intercept's second bile acid analog to have completed Phase 1 clinical development, the goal of which was to assess safety and pharmacokinetics in healthy volunteers.
• Like obeticholic acid (OCA), Intercept's lead product, INT-767 is derived from the primary human bile acid chenodeoxycholic acid, however it is a more potent FXR agonist than OCA and has the potential to demonstrate greater efficacy in liver disease.
• INT-767 also activates TGR5, a second bile acid receptor that has been shown to affect energy metabolism, glucose homeostasis, bile composition/secretion and inflammation.
• In animal models, INT-767 has shown both anti-fibrotic and anti-inflammatory effects.

INT-787: an FXR agonist that is currently being evaluated in preclinical studies.

• INT-787 appears to be a more selective FXR agonist than OCA and has shown potential anti-fibrotic and anti-inflammatory effects in animal models.

We believe that bile acid chemistry may have utility in a broad range of diseases outside of our core area of focus and may explore the potential application of our development compounds in non-core areas.

^*The agents discussed are investigational and have not been approved by the FDA or any other worldwide regulatory agency as a treatment for any indication. Safety and efficacy have not been established.