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

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, an...

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Published in:Clinical pharmacology in drug development 2022-05, Vol.11 (5), p.576-584
Main Authors: Park, Jungsin, Kim, Choon Ok, Oh, Eun Sil, Lee, Jung Il, Kim, Ja Kyung, Ahn, Sang Hoon, Kim, Do Young, Kim, Seung Up, Kim, Beom Kyung, Chung, Yong Eun, Kim, Se‐mi, Park, Min Soo
Format: Article
Language:English
Subjects:
Drug therapy
hepatic impairment
Humans
Hypoglycemic Agents - pharmacokinetics
Liver
Liver Diseases
lobeglitazone
Pharmacokinetics
Pyrimidines - adverse effects
safety
thiazolidinediones
Thiazolidinediones - pharmacokinetics
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Summary: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.
ISSN:2160-763X
2160-7648
DOI:10.1002/cpdd.1045