INT-777

Overview

INT-777 (also known as one of the INT series of bile acid derivatives; distinct from obeticholic acid/INT-747) is a selective agonist of the TGR5 receptor (GPBAR1). In hepatobiliary disease, TGR5 agonism promotes M2 macrophage polarization and NF-kB suppression in early cholestasis but can drive pro-tumorigenic signaling in advanced cholangiocarcinoma (CHOL) via Src/EGFR transactivation. INT-777 is cited as a pharmacological probe in this context.

Evidence in the corpus

• INT-777 (TGR5/GPBAR1 agonist) is cited among emerging therapeutics targeting the bile acid receptor axis in cholangiocarcinoma; the hepatoprotective vs pro-tumorigenic duality of TGR5 (ERK1/2 phosphorylation via Src/EGFR transactivation, PKA-mediated CD95 apoptosis resistance in advanced CCA) requires careful indication selection PMID:25608663

Resistance mechanisms

Cancer types (linked)

• CHOL — cholangiocarcinoma

Sources

• PMID:25608663

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