Journal
CLINICAL PHARMACOLOGY IN DRUG DEVELOPMENT
Volume 11, Issue 5, Pages 576-584Publisher
WILEY
DOI: 10.1002/cpdd.1045
Keywords
hepatic impairment; lobeglitazone; pharmacokinetics; safety; thiazolidinediones
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Funding
- Chong Kun Dang Pharmaceutical Co., Ltd. (Seoul, Republic of Korea)
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This study compared the pharmacokinetic profile and safety of lobeglitazone in patients with hepatic impairment and healthy controls. The results showed no significant differences in lobeglitazone plasma concentrations and pharmacokinetic parameters between mild or moderate hepatic impairment patients and control groups. The concentrations and pharmacokinetic parameters of the major metabolite M7 also did not differ significantly between the patient groups and controls. These findings suggest that lobeglitazone can be safely used in patients with mild or moderate hepatic impairment.
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 (C-max) and area under the plasma concentration-time curve from time 0 extrapolated to infinity (AUC(inf)) 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 C-max and AUC(inf) 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 C-max and AUC(inf) 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.
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