This week in therapeutics




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Endocrine/metabolic disease


G protein-coupled receptor 119 (GPR119)

Mouse studies identified a series of indolines that act as selective GPR119 agonists and could help treat type 2 diabetes. In mouse islets, a lead indoline-based GPR119 agonist increased glucose-stimulated insulin secretion compared with vehicle. In mice, the agonist increased insulin secretion in response to glucose and decreased gastric emptying without altering food intake compared with vehicle control. GlaxoSmithKline plc did not disclose next steps, which could include testing the agonist in additional diabetes models.
At least five companies have GPR119 agonists in clinical and preclinical testing to treat diabetes.

SciBX 6(1); doi:10.1038/scibx.2013.13
Published online Jan. 10, 2013

Patent and licensing status undisclosed

Katamreddy, S.R. et al. J. Med. Chem.; published online Dec. 5, 2012;
Contact: Andrew J. Carpenter, GlaxoSmithKline Research & Development, Research Triangle Park, N.C.