Effect of glimepiride on the pharmacokinetics of teneligliptin in healthy Korean subjects

Jin Woo Park, Kyoung Ah Kim, Yun Jung Choi, Soo Hyun Yoon, Ji-Young Park

Research output: Contribution to journalArticle


What is known and objective: Teneligliptin is a DPP-4 inhibitor used for the treatment of type 2 diabetes mellitus, commonly prescribed in combination with glimepiride. Teneligliptin is metabolized by CYP3A4, and glimepiride might be partly metabolized by CYP3A4. The aim of the study was to investigate the possible effect of glimepiride on the pharmacokinetics of teneligliptin in healthy subjects. Methods: A repeated dose, open-label, fixed-sequence study was conducted in 26 healthy subjects. All participants were administered 20 mg teneligliptin daily for 6 days. On day 7, 4 mg glimepiride was administered together with 20 mg teneligliptin. Plasma teneligliptin concentrations were measured at a steady state, and its pharmacokinetic characteristics were compared without and with glimepiride. Results and discussion: No statistically significant difference was found in the effect of glimepiride on teneligliptin pharmacokinetics. The steady-state C max,ss values of teneligliptin without and with glimepiride were 207.01 ng/mL and 202.15 ng/mL, respectively. Its AUC τ values at steady-state without and with glimepiride were 1527.8 ng · h/mL and 1578.6 ng · h/mL, respectively. The point estimation of geometric mean ratios (GMR) and the 90% confidence interval for both C max,ss and AUC τ were within the equivalence range of 0.8-1.25. The results of the present study revealed that glimepiride did not cause pharmacokinetic interaction with teneligliptin in humans. What is new and conclusion: Glimepiride did not affect the pharmacokinetic characteristics of teneligliptin in healthy subjects.

Original languageEnglish
JournalJournal of Clinical Pharmacy and Therapeutics
Publication statusPublished - 2019 Jan 1


  • drug interaction
  • glimepiride
  • pharmacokinetics
  • teneligliptin

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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