Type 2 diabetes is based on complex physiopathological mechanisms, mainly represented by insulin resistance and β cell dysfunction, the latter mechanism being in fact the defining one in the clinical expression of the disease and its progressive evolution. Unfortunately though, the conventional class of antihyperglyce-mic drugs only manage to partially fight against the pathogenic components of the disease and are accompanied by a series of limitations on their usage, including: weight gain, digestive intolerance, increased risk of hypoglycemia. Moreover, there have been studies showing that the use of certain hypoglycemiant agents has been associated with an increase in cardiovascular events. In this context, a recently developed strategy in order to obtain an optimal glycemic control is aimed at using a new class of drugs represented by DPP-4 inhibitors. Through their action of inhibiting dipeptidyl peptidase-4 (DPP-4), they extend the life of endogenous incretins: glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP) and amplify their biological effects. Therefore, besides enhanced glycemic control, DPP-4 inhibitors seem to have a number of additional benefits: neutral weight, improved β cell function, cardiovascular protection, which might confer them an important role in current medical practice. [ABSTRACT FROM AUTHOR]