Effects of Hepatic Impairment on the Pharmacokinetic Profile and Safety of Lobeglitazone

Jungsin Park, Choon Ok Kim, Eun Sil Oh, Jung Il Lee, Ja Kyung Kim, Sang Hoon Ahn, Do Young Kim, Seung Up Kim, Beom Kyung Kim, Yong Eun Chung, Se mi Kim, Min Soo Park

Research output: Contribution to journalArticlepeer-review

Abstract

In this open-label, single-dose, parallel-group study, we compared the pharmacokinetic profile and safety of lobeglitazone, a thiazolidinedione acting as an agonist for peroxisome proliferator-activated receptors, in patients with hepatic impairment (HI) and healthy matched controls for age, sex, and body weight. After a single oral dose of lobeglitazone (0.5 mg), the lobeglitazone (parent drug) and M7 (major metabolite) plasma concentrations and pharmacokinetic parameters were analyzed and compared between the HI patient groups and healthy matched control groups. The geometric mean ratio (GMR; 90% confidence interval [CI]) for maximum concentration (Cmax) and area under the plasma concentration–time curve from time 0 extrapolated to infinity (AUCinf) of lobeglitazone was 1.06 (0.90-1.24) and 1.07 (0.82-1.40), respectively, for mild HI vs control A. The GMR (90%CI) of Cmax and AUCinf was 0.70 (0.56-0.88) and 1.00 (0.72-1.37), respectively, for moderate HI vs control B. For M7, the GMR (90%CI) of Cmax and AUCinf was 1.09 (0.75-1.57) and 1.18 (0.71-1.97), respectively, for mild HI vs control A and 1.50 (0.95-2.38) and 1.79 (1.06-3.04), respectively, for moderate HI vs control B. Notable adverse events or tolerability issues were not observed. Lobeglitazone may be safely used in patients with mild or moderate HI without dose adjustment.

Original languageEnglish
Pages (from-to)576-584
Number of pages9
JournalClinical Pharmacology in Drug Development
Volume11
Issue number5
DOIs
Publication statusPublished - 2022 May

Bibliographical note

Funding Information:
This study was funded by Chong Kun Dang Pharmaceutical Co., Ltd. (Seoul, Republic of Korea).

Publisher Copyright:
© 2022, The American College of Clinical Pharmacology.

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science
  • Pharmacology (medical)

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