Evogliptin, also known as DA-1229, is a potent and selective DPP4 inhibitor (dipeptidyl peptidase 4 inhibitor). Evogliptin improves insulin resistance and delays the onset of diabetes. Evogliptin improves the insulin sensitivity in HF mice and delays the onset of diabetes in young db/db mice. DA-1229 monotherapy (5 mg for 12 weeks) improved HbA1c, fasting plasma glucose level, OGTT results and β-cell function. This drug was well tolerated in Korean subjects with type 2 diabetes mellitus.