Saxagliptin HCl (also known as BMS-477118; brand name: Onglyza) is a potent, orally bioactive,
selective and reversible DPP4 (dipeptidyl peptidase-4) inhibitor with
IC50 of 26 nM. Saxagliptin was approved in 2008 by FDA for the treatment
of type 2 diabetes. Saxagliptin is a competitive DPP4 inhibitor that
slows the inactivation of the incretin hormones, thereby increasing
their bloodstream concentrations and reducing fasting and postprandial
glucose concentrations in a glucose-dependent manner in patients with
type 2 diabetes mellitus. In vitro, saxagliptin inhibits FBS-, insulin-
and IGF1-induced ERK phosphorylation and cell proliferation, in both MSC
and MC3T3E1 preosteoblasts. In the absence of growth factors,
saxagliptin has no effect on ERK activation or cell proliferation.