Nowadays, diabetes affects about 200 million people worldwide, and represents the sixth-leading cause of death. Approximately 90 to 95% of those affected have type 2 diabetes, caused by two main mechanisms: insulin deficiency or peripheral insulin resistance. Early in the approach, diabetic patients are encouraged to make healthy lifestyle modifications including changes in diet, exercise patterns, and weight control. However, in most of patients, as the disease progresses, pharmacologic treatment becomes necessary. Despite the many pharmacological treatment modalities currently available, glucose control remains unsatisfactory in the type 2 diabetes population as evidenced by average hemoglobin A1c (HbA1c). The incretin mimetics and DPP-IV inhibitors are the new class of medications available for treating patients with diabetes type 2. The glycemic profiles of patients after administrations of incretin mimetics and DPP-IV inhibitors show improvement in postprandial glucose levels and ultimately in HbA1c. Therefore, incretin mimetics and DPP-IV inhibitors may play a clinically significant role in the treatment of patients with type 2 diabetes.