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Diabetes Obes Metab. 2014 Oct;16(10):1036-9. doi: 10.1111/dom.12312. Epub 2014 Jun 9.

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

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Profil Institut für Stoffwechselforschung GmbH, Neuss, Germany.


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.


DPP-IV inhibitor; beta cell; drug mechanism; glycaemic control; type 2 diabetes

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