Purpose: To study the influence of sitagliptin on blood glucose, lipid and pancreatic β cell function in type II diabetes mellitus (T2DM) patients. Methods: Two groups of T2DM patients (100/group) received either metformin only (control group), or metformin plus sitaglipin (study group) for 3 months. Blood lipid profiles, fasting blood glucose (FBG), indices of pancreatic function and insulin resistance were assayed using standard biochemical methods. Results: The metformin-sitaglipin combination resulted in significant decreases in FBG, 2-h PBG, HbAlc total cholesterol (TC), triacylglycerol, and low-density lipoprotein cholesterol (LDL-C), when compared with the metformin-only treatment (p < 0.05). Although there were significant decreases in pancreatic secretion of insulin, fasting insulin, and 2 h postprandial insulin in the two groups, these parameters were significantly lower in the metformin-only treated patients than in those with combination treatment (p < 0.05). Conclusion: Sitagliptin normalizes fasting blood glucose, lipid profiles and insulin secretion in type II diabetes mellitus (T2DM) patients.