GSK1292263 + sitagliptin

**GSK1292263 + sitagliptin** is an investigational oral combination therapy studied for the treatment of type 2 diabetes mellitus. GSK1292263 is a selective agonist of the G protein-coupled receptor 119 (GPR119), designed to enhance incretin and gut hormone secretion such as peptide tyrosine-tyrosine (PYY) and possibly promote glucose-dependent insulin release. Sitagliptin is a small molecule dipeptidyl peptidase-4 (DPP-4) inhibitor that prolongs the activity of incretin hormones, notably GLP-1 and GIP, by preventing their degradation, resulting in increased insulin secretion and reduced glucagon levels. While GSK1292263 was shown in clinical studies to significantly increase circulating levels of PYY, its direct effect on GLP-1 and glucose lowering was limited. Sitagliptin increased active GLP-1 but suppressed gut peptides, an effect modulated by the presence of metformin. The combination was primarily evaluated in clinical studies for its effects on gut hormones and glycemic control in subjects with type 2 diabetes[1][2][4][5].

Other names

GSK263 + sitagliptin