Sitagliptin is a time-tested leading drug in the treatment of type 2 diabetes

Dipeptidyl peptidase type 4 (DPP-4) inhibitors hold leadership positions in the treatment of type 2 diabetes worldwide due to their pathogenetically substantiated mechanism of action, low risk of hypoglycemic states and good tolerability. Today, they represent the largest class of glucose-lowering medicines. Sitagliptin, the first antidiabetic agent from this class, is the best known one and along with that remains the most promising medicine. It can be prescribed either as the initial treatment or later in a combination with other classes of hypoglycemic drugs, including sulfonylurea derivatives. Glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide (GIP), which blood concentrations increase under the effect of DPP-4 inhibitors, enhance glucose-stimulated insulin secretion through activating the cyclic adenosine monophosphate (cAMP) signaling pathway in pancreatic β-cells, meanwhile cAMP plays a critical role in an increase in β-cell sensitivity to glucose. Sitagliptin is an antidiabetic agent with significant data on cardiovascular safety. The efficacy of the drug is broadly similar to that of sulfonylurea derivatives. At the same time, the low risk of hypoglycemic states and the absence of side effects create certain advantages of using this drug in elderly patients. Active use of the drug in patients with diabetes in Japan is associated with the predominance of secretory disorders in the pathogenesis of the disease and the efficacy of DPP inhibitors in this ethnic group. The pleiotropic properties of the drug continue to be studied. The positive effects of sitagliptin in coronavirus infection may be associated with the anti-inflammatory and immunomodulatory properties of the drug. The potential of the drug in the treatment of immune-mediated conditions, as well as its neuroprotective properties in the prevention and treatment of Alzheimer's disease, are considered.