The DPP4 inhibitor class of drugs are characterized by good tolerability, low hypoglycemia risk, neutral effect on body weight, intermediate efficacy, and neutral cardiovascular effect. Among the DPP-4 inhibitors, gemigliptin is a potent and highly selective long acting DPP-4 inhibitor and can be used without dose adjustment in renal impairment. Results of two phase 3 trials comparing efficacy and safety of gemigliptin to other DPP-4 inhibitors (sitagliptin and vildagliptin) as add-on therapy to metformin in type 2 diabetic patients inadequately controlled with metformin monotherapy, have shown that the efficacy of gemigliptin was similar to those of sitagliptin 100mg qd and vildagliptin 50mg bid. Gemigliptin was also well tolerated. The GUARD study showed that gemigliptin was efficacious in lowering HbA1c compared to placebo at 12 weeks in patients with moderate to severe renal impairment.