Abstract: OBJECTIVE To observe the effect of combination of linagliptin and metformin on glycaemic control and safety in patients with type 2 diabetes. METHODS In this 24 weeks, double-blind, placebo-controlled study, 15 patients with type 2 diabetes were randomized to 2 groups: 5 mg linagliptin plus metformin group(Group A, n=10), placebo plus metformin group(Group B, n=5). Hemoglobin Alc(HbAlc), FPG, lipid profile, urinary albumin creatinine ratio(UACR), ALT, AST, ALP, Scr, CK, body mass index(BMI), waist circumstance, systolic blood pressure(SBP) and diastolic blood pressure(DBP) were measured. RESULTS The mean decreasing amplitude for HbA1c in the two groups were -14.9%, -7.3%, respectively (P<0.05). FPG decreased by 4.7%, 8.0%, respectively(P>0.05). SBP changed by -1.6%, +9.0%, respectively(P<0.05). And DBP changed by +0.2%, +13.7%(P<0.05). UACR changed by -33.3%, +91.1%(P<0.01). There were no significant difference in lipid profile, ALT, AST, ALP, Scr, CK, BMI, waist circumstance change and adverse events. There were no hypoglycemic events in each group. CONCLUSION Combination of linagliptin and metformin is superior to metformin monotherapy in HbA1c control and has favorable effect on blood pressure and UACR, with a similar lowering FPG capacity and safety profile, without weight gain and risk of hypoglycemia.