Type 2 diabetes mellitus is a multifactorial multiorgan disease. Over the last decade, the implementation of brand-new therapeutic opportunities led to tremendous rise of research studies in the field of diabetes as well as to shift in priorities of the management of patients with type 2 diabetes from a glucocentric approach and towards holistic control of the key underlying pathophysiological processes of the disease development and progression. The use of dipeptidyl peptidase-4 inhibitors shows good glycemic control because of physiological glucose — dependent mechanism of action mediated with the improvement of incretin hormones effects. Moreover, dipeptidyl peptidase-4 inhibitors have a wide range of pleiotropic effects owning to additional properties of incretins and inhibition of dipeptidyl peptidase enzymatic activity, which leads to beneficial impact on metabolic and pathogenetic processes of type 2 diabetes mellitus. Dipeptidyl peptidase-4 inhibitors are effective drugs with good safety profile as for risks related to type 2 diabetes and have no limitative disadvantages such as hypoglycemia and weight gain. This publication reviews vildagliptin, the first developed dipeptidyl peptidase-4 inhibitor, with an emphasis on its use in different clinical settings of diabetes management.