Type 2 diabetes mellitus is a worldwide health problem. Adequate glycemic control can help to prevent many chronic diabetic complications. Despite the availability of several classes of oral hypoglycemic agents and insulin, many patients fail to achieve adequate glycemic control. Incretins are gut hormones produced in response to ingestion of nutrients. Glucagon-like peptide-1 (GLP-1), one of the incretin hormones, has pleiotropic actions on the control of blood glucose. Clinical trials with the incretin mimetic and Dipeptidyl peptidase-IV inhibitors demonstrate promising results in the improvement of glucose homeostasis.