The mechanism of the action of dipeptidyl peptidase-4 inhibitors and its use in type 2 diabetes / 中华内分泌代谢杂志

ABSTRACT

The critical role of α- and β-cell dysfunction in the development of type 2 diabetes has been established.Dipeptidyl peptidase-4 (DPP-4) inhibitors are new class of oral anti-hyperglycemia agents that acts to increase active levels of the incretin hormone glucagon-like peptide-1 ( GLP-1 ) and glucose-dependent insulinotropic polypeptide ( GIP),which improved α- and β-cell function.This action is shown as improved α- and β-cell sensitivity to glucose,increased glucose-dependent insulin secretion and decreased glucagon secretion.DPP-4 inhibitors treatment has also been associated with beneficial extrapancreatic effects,including improved peripheral insulin sensitivity and lipid metabolism.Additionally,DPP-4 inhibitors have shown a minimal risk of hypoglycemia and bodyweight neutrality without effects on gastric emptying.Numerous clinical trials have verified the favorable efficacy,safety,and tolerability of DPP-4 inhibitors treatment in monotherapy or combination with other anti-diabetic agents for patients with type 2 diabetes.