The Sound of Evolution
Saxagliptin
Mechanism of action:
Saxagliptin is a dipeptidyl peptidase-4 inhibitor. Dipeptidyl peptidase-4, or DPP-4, is an enzyme responsible for degrading incretins such as glucagon-like peptide-1 and glucose-dependent insulinotropic polypeptide. When saxagliptin inhibits DPP-4, incretins are less readily degraded, and their blood concentration and duration of action are prolonged. This promotes insulin secretion from pancreatic beta cells and suppresses glucagon secretion from pancreatic alpha cells.
Reference(s):
1. Rosenstock J et al. (2008). Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naive patients with type 2 diabetes. Diabetes Obes Metab.
2. Metzler WJ et al. (2008). Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci.
3. Crepaldi G et al. (2007). Dipeptidyl peptidase 4 (DPP-4) inhibitors and their role in Type 2 diabetes management. J Endocrinol Invest.