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Linagliptin: An Update of Its Use in Patients with Type 2 Diabetes Mellitus

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Abstract

Linagliptin (Trajenta®, Tradjenta®) is a dipeptidyl peptidase (DPP)-4 inhibitor approved for the treatment of adults with type 2 diabetes mellitus in several countries. A fixed-dose combination of linagliptin/metformin (Jentadueto®) is also available. This article reviews the pharmacology, therapeutic efficacy and tolerability of linagliptin in the management of type 2 diabetes, with the aim of updating its place in therapy based on recently published data. In randomized, controlled trials, oral linagliptin 5 mg once daily (or 2.5 mg twice daily when combined with metformin) improved glycaemic control when used alone or in combination with other antidiabetic agents, including metformin, a sulfonylurea, thiazolidinedione or insulin. Improvements in glycaemic control were also shown in patients with renal impairment, including severe impairment, and the elderly (aged ≥70 years). Linagliptin is the first DPP-4 inhibitor to be eliminated primarily via a nonrenal route, enabling its use without dosage adjustment in patients with any degree of renal impairment. Linagliptin is generally well tolerated and, as with other DPP-4 inhibitors, it is associated with a low risk of hypoglycaemia and has no effect on bodyweight. Some data indicate that linagliptin may have beneficial effects on cardiovascular and renal safety profiles in patients with type 2 diabetes, but more data are needed. Meanwhile, the low risk of hypoglycaemia and the nonrenal route of elimination may provide important advantages for some patient groups, including elderly or renally impaired patients.

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Disclosure

The preparation of this review was not supported by any external funding. Kate McKeage is a salaried employee of Adis/Springer. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on this article. Changes resulting from comments received were made by the author on the basis of scientific and editorial merit.

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    Kate McKeage

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Correspondence to Kate McKeage.

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The manuscript was reviewed by: D. S. H. Bell, Southside Endocrinology, University of Alabama, Birmingham, AL, USA; G. Dimitriadis, 2nd Department of Internal Medicine, Research Institute and Diabetes Center, Athens University Medical School, ‘Attikon’ University Hospital, Athens, Greece; J. G. Eriksson, Department of General Practice and Primary Healthcare, University of Helsinki, Helsinki, Finland.

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McKeage, K. Linagliptin: An Update of Its Use in Patients with Type 2 Diabetes Mellitus. Drugs 74, 1927–1946 (2014). https://doi.org/10.1007/s40265-014-0308-3

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