molecules of the month


oral FXR agonist for NASH

robust in vivo PD, phase I HV study withdrawn

from prior FXR agonists

ACS Med. Chem. Lett

Bristol Myers Squibb, Princeton, NJ, USA

1 min read

The BMS spirocyclobutene-containing FXR agonist, BMS-986318, appears to have been intended as a clinical candidate, but was withdrawn from a planned Ph. I study. The molecule exhibits potent in vitro and in vivo activation of FXR (FXR Gal4 reporter EC50 = 53 nM, SRC-1 recruitment assay EC50 = 350 nM) and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis. This novel molecule displayed robust target engagement in vivo and is a rare example of a cyclobutene-containing, rationally designed drug-like molecule.

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