Praktické lekárnictvo 1/2011

Sitagliptin

Sitagliptin is an oral antidiabetic incretin-based drug. It is a specific inhibitor of DPP-4 (dipeptidyl peptidase-4), which regulates the degradation and the bioactivity of native GLP-1 (glucagon-like peptide – 1) and GIP (glucose-dependent insulinotropic polypeptide). Sitagliptin is characterized by low incidence of hypoglycemia during the therapy. Sitagliptin reduces mean HbA1c and has a neutral inpact on body weight. Sitagliptin is generally well tolerated, with no significant side effects. Sitagliptin is being used in combination with metformin and thiazonlidindiones. In experimental studies sitagliptin inhibits apoptosis of islets β-cells and stimulates their proliferation, which results in increasing of β-cell mass.

Keywords: Sitagliptin, DPP-4 inhibitors, incretin hormones, GLP-1, GIP, type 2 diabetes mellitus.