Saxagliptin, a dipeptidyl peptidase-IV (DPP-IV) inhibitor, is currently under development by Bristol-Myers Squibb Co, AstraZeneca plc and Otsuka Pharmaceutical Co Ltd for the treatment of type 2 diabetes. The compound has high selectivity for DPP-IV compared with other dipeptidyl peptidases and a duration profile designed for once-daily dosing. DPP-IV inhibitors act by increasing levels of glucagon-like peptide-1, which stimulates insulin secretion. In animal studies, saxagliptin improved glucose clearance and raised insulin levels in rodents. Clinical trials have demonstrated a dose-dependent inhibition of DPP-IV by saxagliptin without serious side effects. Results have demonstrated that treatment with saxagliptin lowers blood glucose levels, with good tolerability and safety. The specific advantages of saxagliptin over other DPP-IV inhibitors may lie in its long-lived, effective and highly specific inhibition of DPP-IV, making once-daily treatment feasible, effective and safe.