GSK1292263 + metformin

**GSK1292263 + metformin** is a combination of a novel small molecule GPR119 agonist (GSK1292263) and the established antihyperglycemic agent metformin. GSK1292263 acts selectively on the GPR119 receptor, which is highly expressed in pancreatic beta cells and intestinal enteroendocrine cells; its activation is intended to improve glucose metabolism and alter gut hormone profiles, particularly increasing circulating peptide YY (PYY)[1][6]. Metformin is a biguanide that lowers glucose production by the liver, enhances insulin sensitivity, and slows intestinal glucose absorption[5]. When administered to subjects with type 2 diabetes, co-dosing GSK1292263 and metformin was associated with marked increases in PYY after meals and an augmented increase in total glucagon-like peptide-1 (GLP-1), though did not produce a significant improvement in glucose control compared with controls[1][9]. Developed and evaluated in clinical studies primarily by GSK, this combination targets glycemic modulation and gut hormone regulation in type 2 diabetes mellitus[1][9].

Other names

GSK263 + metformin