Pharmacotherapeutic Group: Drugs used in diabetes; dipeptidyl peptidase 4 (DPP-4) inhibitor.
Pharmacology: Linagliptin is an inhibitor of the enzyme DPP-4 (Dipeptidyl peptidase 4, EC 220.127.116.11) an enzyme which is involved in the inactivation of the incretin hormones GLP-1 and GIP (glucagon-like peptide-1, glucose-dependent insulinotropic polypeptide). These hormones are rapidly degraded by the enzyme DPP-4.
Linagliptin binds very effectively to DPP-4 in a reversible manner and thus leads to a sustained increase and a prolongation of active incretin levels.
Linagliptin glucose-dependently increases insulin secretion and lowers glucagon secretion thus resulting in an overall improvement in the glucose homeostasis. Linagliptin binds selectively to DPP-4 and exhibits a > 10,000 fold selectivity versus DPP-8 or DPP-9 activity in vitro.