Saxagliptin is an orally-available, adamantyl-based, reversible inhibitor of DPP-IV for the treatment of Type 2 diabetes with an IC50 of 26 nM and Ki of 0.6-1.3 nM [1, 2]. Saxagliptin is more selective than other approved DPP-IV inhibitors (vildagliptin, sitagliptin) and is 400-fold and 75-fold selective over DPP-VIII and DPP-IX, respectively. [1] Once-daily administration of saxagliptin either as a monotherapy or in combination results in a significant reductions in fasting and postprandial plasma glucose and HbA1c.

Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, improving b-cell function and suppression of glucagon secretion. [2]