This week in therapeutics




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Hepatic disease

Liver disease

Farnesoid X receptor (FXR; NR1H4);
G protein-coupled bile acid receptor 1 (GPBAR1; TGR5)

Mouse studies suggest the FXR and TGR5 dual agonist INT-767 could help treat nonalcoholic fatty liver disease (NAFLD). In a mouse model for obesity-induced NAFLD, INT-767 decreased hepatic steatosis and inflammation compared with no agonist. Next steps could include evaluating INT-767 in additional mouse models of NAFLD.
Intercept Pharmaceuticals Inc. has INT-767 in preclinical development to treat renal diseases.

SciBX 6(11); doi:10.1038/scibx.2013.266
Published online March 21, 2013

Multiple patents covering FXR agonists filed by Intercept Pharmaceuticals; licensing status unavailable

McMahan, R. et al. J. Biol. Chem.; published online March 4, 2013;
Contact: Hugo R. Rosen, University of Colorado Denver, Aurora, Colo.