The Sound of Evolution
Linagliptin
Mechanism of action:
Linagliptin is a dipeptidyl peptidase-4 inhibitor. Dipeptidyl peptidase-4 (DPP-4) is an enzyme responsible for degrading incretins such as glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. When linagliptin inhibits DPP-4, incretins are less readily degraded, resulting in prolonged circulating levels and duration of action. This enhances incretin-mediated insulin secretion signaling and reduces glucagon secretion signaling.
Reference(s):
1. Forst T et al. (2012). Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes. Expert Opin Pharmacother.
2. Blech S et al. (2010). The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. Drug Metab Dispos.