ABSTRACT
Glucagon-like peptide-1 (GLP-1) can maintain glucose homeostasis, improve islet function,delay and even reverse deterioration of type 2 diabetes by several pathways.But shortly after secreting and releasing into the blood, endogenous intact GLP-1 is cleavaged by dipeptidyl peptidase-4 (DPP-4) into inactive forms.DPP4 inhibitors prevent the inactivation and enhance the physiological effects of GLP-1 through selectively suppressing the enzymic activity of DPP-4, resulting in reduction of HbA1C, fasting and postprandial plasma glucose in type 2diabetes mellitus.The favorable efficacy, safety, and tolerability of DPP-4 inhibitors, which have been well verified in numerous clinical trials and clinical practice for type 2 diabetes mellitus, render them a novel type of oral antidiabetic drugs.