Department of Clinical Pharmacology and Toxicology, Korea University College of Medicine, Korea University Anam Hospital, Seoul, Korea.
HANDOK Inc., Seoul, Korea.
J Clin Pharm Ther. 2019 Oct;44(5):720-725. doi: 10.1111/jcpt.12848. Epub 2019 May 15.
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.
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.
No statistically significant difference was found in the effect of glimepiride on teneligliptin pharmacokinetics. The steady-state C values of teneligliptin without and with glimepiride were 207.01 ng/mL and 202.15 ng/mL, respectively. Its AUC 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 and AUC 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.
Glimepiride did not affect the pharmacokinetic characteristics of teneligliptin in healthy subjects.
替格列汀是一种用于治疗 2 型糖尿病的 DPP-4 抑制剂，通常与格列美脲联合使用。替格列汀主要通过 CYP3A4 代谢，而格列美脲可能部分通过 CYP3A4 代谢。本研究旨在探讨格列美脲对健康受试者中替格列汀药代动力学的可能影响。
一项重复剂量、开放标签、固定序列的研究在 26 名健康受试者中进行。所有参与者每天服用 20mg 替格列汀，连续 6 天。第 7 天，同时给予 4mg 格列美脲和 20mg 替格列汀。在稳态时测量替格列汀的血浆浓度，并比较有无格列美脲时的药代动力学特征。
格列美脲对替格列汀药代动力学无统计学显著影响。无格列美脲和有格列美脲时替格列汀的稳态 C 值分别为 207.01ng/mL 和 202.15ng/mL。无格列美脲和有格列美脲时替格列汀的稳态 AUC 值分别为 1527.8ng·h/mL 和 1578.6ng·h/mL。两种 C 和 AUC 的几何均数比值（GMR）的点估计值和 90%置信区间均在 0.8-1.25 的等效范围内。本研究结果表明，格列美脲不会引起替格列汀在健康受试者中的药物相互作用。
格列美脲不影响健康受试者中替格列汀的药代动力学特征。
