1000403-03-1

INT-767 is a G-protein coupled/Farnesoid X-activated receptor agonist potentially for the treatment of hepatic fibrosis. INT-767 significantly improved serum liver enzymes, hepatic inflammation, and biliary fibrosis in Mdr2(-/-) mice. INT-767 significantly induced bile flow and biliary HCO?3- output, as well as gene expression of carbonic anhydrase 14, an important enzyme able to enhance HCO?3- transport, in an Fxr-dependent manner. In addition, INT-767 dramatically reduced bile acid synthesis via the induction of ileal Fgf15 and hepatic Shp gene expression, thus resulting in significantly reduced biliary bile acid output in Mdr2(-/-) mice.

INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively[1][2].

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[1] Baghdasaryan A, et al. Dual farnesoid X receptor/TGR5 agonist INT-767 reduces liver injury in the Mdr2-/- (Abcb4-/-) mousecholangiopathy model by promoting biliary HCO3- output. Hepatology. 2011 Oct;54(4):1303-1312. DOI:10.1002/hep.24537
[2] Rizzo G, et al. Functional characterization of the semisynthetic bile acid derivative INT-767, a dual farnesoid X receptor andTGR5 agonist. Mol Pharmacol. 2010 Oct;78(4):617-630. DOI:10.1124/mol.110.064501