BMS-510849

BMS-510849 is the main active metabolite of saxagliptin, a dipeptidyl peptidase-4 (DPP4) inhibitor used in the treatment of type 2 diabetes mellitus. BMS-510849 is generated via metabolic transformation of saxagliptin primarily by the CYP3A4/5 enzymes. Like saxagliptin, BMS-510849 also inhibits the DPP4 enzyme, but it is more selective and less potent than the parent compound. The pharmacological effects of BMS-510849 include contributing to the inhibition of DPP4 and therefore to the overall glucose-lowering effect of saxagliptin therapy, though its direct impact is less pronounced than saxagliptin. Protein binding of BMS-510849 is very low, and it is excreted primarily via the kidneys[1][3].