Linagliptin: an update of its use in patients with type 2 diabetes mellitus

Drugs. 2014 Oct;74(16):1927-1946. doi: 10.1007/s40265-014-0308-3.


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.

Publication types

  • Review

MeSH terms

  • Diabetes Mellitus, Type 2 / drug therapy*
  • Dipeptidyl Peptidase 4 / metabolism
  • Dipeptidyl-Peptidase IV Inhibitors / pharmacology
  • Dipeptidyl-Peptidase IV Inhibitors / therapeutic use*
  • Humans
  • Linagliptin
  • Purines / pharmacology
  • Purines / therapeutic use*
  • Quinazolines / pharmacology
  • Quinazolines / therapeutic use*


  • Dipeptidyl-Peptidase IV Inhibitors
  • Purines
  • Quinazolines
  • Linagliptin
  • Dipeptidyl Peptidase 4