Population Pharmacokinetic/Pharmacodynamic Analysis of the DPP-4 Inhibitor Linagliptin in Japanese Patients with Type 2 Diabetes Mellitus

Abstract

The nonlinear PK of linagliptin and its plasma DPP-4 inhibition in patients were well characterized by a target-mediated drug disposition model relating DPP-4 occupancy with linagliptin to DPP-4 inhibition. Simulations of plasma DPP-4 inhibition suggest that 5 mg linagliptin once daily is an appropriate therapeutic dose for Japanese patients with T2DM.