Drug profile-Saxagliptin, a novel dipeptidyl peptidase-4 inhibitor for the treatment of type 2 diabetes

Abstract

Saxagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor for the treatment of type 2 diabetes. It is a novel DPP-4 inhibitor with a high selectivity for DPP-4 compared with other dipeptidyl peptidases and a duration profile designed for once-daily application. DPP-4 inhibitors enhance endogenous concentrations of the incretin hormones glucagon-like peptide-1 (GLP-1) and gastric inhibitory polypeptide. This action leads to a glucose-dependent stimulation of insulin and inhibition of glucagon secretion post-prandially. DPP-4 inhibitors have no intrinsic risk of hypoglycemia and are weightneutral. Saxagliptin has been approved in the US and other countries. Phase I clinical trials demonstrated a dose-dependent inhibition of DPP-4 by saxagliptin in a dose range from 2.5 to 100mg daily without serious side effects. Patients with type 2 diabetes receiving 10mg saxagliptin once-daily in phase II trials showed a lowering of HbA1c and glucose together with good tolerability and safety. Phase III clinical studies demonstrated a good efficacy regarding glycemic parameters in different patient populations, either in monotherapy or in combination with metformin, as well as a favorable cardiovascular profile. © TOUCH BRIEFINGS 2009.