Clinical overview of linagliptin, a dipeptidyl peptidase-4 inhibitor, in patients with Type 2 diabetes mellitus

Abstract

Linagliptin is a pharmacologically unique, orally active, once-daily dipeptidyl peptidase-4 inhibitor indicated for the treatment of hyperglycemia in patients with Type 2 diabetes mellitus. Compared with other dipeptidyl peptidase-4 inhibitors, linagliptin has a favorable pharmacokinetic profile with a primarily nonrenal route of elimination that avoids the need for dose adjustment in patients with renal impairment. When administered as monotherapy or in combination with other antihyperglycemic drugs, linagliptin treatment leads to clinically meaningful reductions in glycated hemoglobin, fasting plasma glucose and postprandial plasma glucose levels. In addition, pancreatic β-cell function is enhanced. Linagliptin treatment is well tolerated, with weight-neutral effects and no increased risk of hypoglycemia. Of note, linagliptin treatment was associated with a significantly reduced risk of cardiovascular events in clinical trials of ≤2 years, although this finding remains to be confirmed in larger and longer clinical outcomes studies.

Keywords::

• dipeptidyl peptidase-4 inhibitor
• linagliptin
• Type 2 diabetes mellitus

Acknowledgements

The authors were fully responsible for all content and editorial decisions, were involved at all stages of manuscript development and have approved the final version of the article that reflects the authors’ interpretation and conclusions.

Financial & competing interests disclosure

T Forst has received advisory and speaker fees from Boehringer Ingelheim. A Pfützner has received speaker fees from Boehringer Ingelheim. Boehringer Ingelheim was given the opportunity to check the data used in the review for factual accuracy only. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Medical writing assistance, supported financially by Boehringer Ingelheim, was provided by Howard Christian, Catherine Rees and Giles Brooke, of Envision Scientific Solutions, during the preparation of this review.