BioCentury
ARTICLE | Distillery Therapeutics

Endocrine / Metabolic

February 2, 2017 6:15 PM UTC

In vitro, cell culture and mouse studies identified a pyrrolidine-based FFAR1 agonist that could help treat Type II diabetes. Chemical synthesis and testing in cell-based assays of pyrrolidine analogs identified a compound that agonized human and mouse FFAR1 with EC50 values of 110 and 5.4 nM, respectively. In primary mouse islet cells, the compound increased glucose-stimulated insulin secretion compared with vehicle. In mice, the compound increased glucose tolerance. Next steps by Bristol-Myers Squibb Co. could include testing the compound in a mouse models of diabetes.

Japan Tobacco Inc. and Torii Pharmaceutical Co. Ltd. have JTT-851, a FFAR1 agonist, in Phase II testing for Type II diabetes...