Pharmacokinetic and pharmacodynamic evaluation of linagliptin for the treatment of type 2 diabetes mellitus, with consideration of Asian patient populations

Antonio Ceriello, Nobuya Inagaki

Research output: Contribution to journalReview articlepeer-review


Our aims were to summarize the clinical pharmacokinetics and pharmacodynamics of the dipeptidyl-peptidase-4 inhibitor, linagliptin, and to consider how these characteristics influence its clinical utility. Differences between linagliptin and other dipeptidyl-peptidase-4 inhibitors were also considered, in addition to the influence of Asian race on the pharmacology of linagliptin. Linagliptin has a xanthine-based structure, a difference that might account for some of the pharmacological differences observed with linagliptin versus other dipeptidyl-peptidase-4 inhibitors. The long terminal half-life of linagliptin results from its strong binding to dipeptidyl-peptidase-4. Despite this, linagliptin shows a short accumulation half-life, as a result of saturable, high-affinity binding to dipeptidyl-peptidase-4. The pharmacokinetic characteristics of linagliptin make it suitable for once-daily dosing in a broad range of patients with type 2 diabetes mellitus. Unlike most other dipeptidyl-peptidase-4 inhibitors, linagliptin has a largely non-renal excretion route, and dose adjustment is not required in patients with renal impairment. Furthermore, linagliptin exposure is not substantially altered in patients with hepatic impairment, and dose adjustment is not necessary for these patients. The 5-mg dose is also suitable for patients of Asian ethnicity. Linagliptin shows unique pharmacological features within the dipeptidyl-peptidase-4 inhibitor class. Although most clinical trials of linagliptin have involved largely Caucasian populations, data on the pharmacokinetic/pharmacodynamic properties of linagliptin show that these features are not substantially altered in Asian populations. The 5-mg dose of linagliptin is suitable for patients with type 2 diabetes mellitus irrespective of their ethnicity or the presence of renal or hepatic impairment.

Original languageEnglish
Pages (from-to)19-28
Number of pages10
JournalJournal of Diabetes Investigation
Issue number1
Publication statusPublished - Jan 1 2017


  • Linagliptin
  • Pharmacodynamics
  • Pharmacokinetics

ASJC Scopus subject areas

  • Internal Medicine
  • Endocrinology, Diabetes and Metabolism


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