The dipeptidyl peptidase‐4 inhibitor linagliptin lowers postprandial glucose and improves measures of β ‐cell function in type 2 diabetes

Progressive deterioration of pancreatic β‐cell function in patients with type 2 diabetes mellitus ( T2DM ) contributes to worsening of hyperglycaemia. To investigate the effects of the dipeptidyl peptidase‐4 inhibitor linagliptin on β‐cell function parameters, a pooled analysis of six randomized, 24‐week, placebo‐controlled, phase 3 trials of 5 mg of linagliptin daily was performed in 2701 patients with T2DM (linagliptin, n = 1905; placebo, n = 796). At week 24, observed improvements in HbA1c , fasting plasma glucose, and 2‐h postprandial glucose were significantly greater for linagliptin than placebo (all p < 0.0001). Homeostasis model assessment ( HOMA )‐%β, as a surrogate marker of fasting β‐cell function, was significantly improved with linagliptin, and did not change with placebo (placebo‐adjusted mean ± s.e. change for linagliptin: 16.5 ± 4.6 ( mU /l)/(mmol/l); p = 0.0003). Further study is required to determine if the significant improvement in HOMA ‐%β with linagliptin will translate into long‐term improvements in β‐cell function.