Saxagliptin is the latest addition to incretin-based therapies in the management of type 2 diabetes. The oral selective dipeptidyl peptidase 4 (DPP-4) inhibitor is just the second in its class to be approved in the U.S. It has been designed to exert long-lasting yet reversible inhibition of the DPP-4 enzyme, thereby slowing down the inactivation of the incretin hormones and enhancing the incretin effect. Saxagliptin is approved in the U.S. as an adjunct therapy to diet and exercise to improve glycemic control. In Canada and Europe, saxagliptin is approved as add-on therapy to one of long-existing antihyperglycemic agents when these drugs, together with diet and exercise, do not adequately achieve glycemic goals. Published clinical trial data indicate that saxagliptin as monotherapy or add-on therapy to metformin, sulfonylureas and thiazolidinediones is effective in improving glycemic control (as measured by hemoglobin A1(C) [HbA1(C)] levels) and achieving glycemic targets (<7% HbA1(C)). It has also been shown to be well-tolerated, with the additional advantage of not having any clinically relevant effect on weight and hypoglycemia incidence. These added benefits are expected to improve therapy adherence.