The antidiabetic effect of the dipeptidyl peptidase 4 (DPP-4) inhibitor saxagliptin depends on the prolongation of action of the 2 incretin hormones: glucagon like peptide-1 (GLP-1) and gastric inhibitory polypeptide (GIP) by preventing their rapid degradation by the enzyme DPP-4. The use of saxagliptin (5 mg/d) is associated with mean reduction in glycosylated hemoglobin (HbA1c) levels ranging from 0.5% to 0.9% compared with baseline and 0.6 to 0.8% compared with placebo after 24 weeks of therapy. The main advantages of saxagliptin are the low risk of hypoglycemia, the neutral effect on body weight, the simplicity of use, and reassuring short-term safety profile. However, its mild-to-moderate efficacy, the lack of long-term safety and efficacy data, and relatively high cost represent its major limitations. Overall, saxagliptin may be a useful second agent for patients with type 2 diabetes who are not optimally controlled on metformin. This drug can also be used as monotherapy in patients with mild hyperglycemia who cannot tolerate metformin or a sulfonylurea (SU).