Linagliptin: A New DPP-4 Inhibitor for the Treatment of Type 2 Diabetes Mellitus

Incretin-based therapies constitute a relatively new pharmacological approach to the treatment of type 2 diabetes mellitus. As reflected in the rapidly growing body of literature and the number of glucagon-like peptide-1 and dipeptidyl peptidase-4 inhibitor (DPP-4) compounds that are either approved or in development, there is considerable interest in treatments that target the incretin axis. Linagliptin is a recently approved DPP-4 inhibitor with unique pharmacological properties, including very high affinity for the DPP-4 enzyme, postdose DPP-4 inhibition>80% after 24 hours, and a primarily fecal route of elimination. Phase 3 clinical trials on >4000 patients have demonstrated the efficacy of linagliptin as monotherapy or in combination with other antidiabetic agents. Treatment with linagliptin reduced glycated hemoglobin by 0.6% to 0.8%, with a safety profile comparable with placebo. This article provides a review of linagliptin clinical data for primary care physicians treating patients with type 2 diabetes mellitus.