Bioequivalence and safety assessment of sorafenib tosylate tablets in healthy Chinese subjects under fasting conditions

ObjectiveThis study aimed to assess the bioequivalence and safety of two formulations of sorafenib in healthy Chinese subjects under fasting conditions.MethodsA single-center, randomized, open, single-dose, two-formulation, four-period, crossover study was performed in 36 healthy Chinese subjects un...

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Bibliographic Details
Main Authors: Zhaoyu Wang, Hong Peng, Yun Zhang, Xijing Chen, Jiye A
Format: Article
Language:English
Published: Frontiers Media S.A. 2025-04-01
Series:Frontiers in Pharmacology
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Online Access:https://www.frontiersin.org/articles/10.3389/fphar.2025.1470095/full
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Summary:ObjectiveThis study aimed to assess the bioequivalence and safety of two formulations of sorafenib in healthy Chinese subjects under fasting conditions.MethodsA single-center, randomized, open, single-dose, two-formulation, four-period, crossover study was performed in 36 healthy Chinese subjects under fasting conditions. Blood samples were collected within 120 h after administration. The plasma concentrations of sorafenib were analyzed by a validated UPLC-MS/MS method, and pharmacokinetic parameters were analyzed using a non-compartmental method. Safety was assessed on the basis of the occurrence of adverse events and laboratory findings throughout the study period.ResultsThe GMR point estimators of Cmax, AUC0-t, and AUC0-∞ for the two formulations were 88.97%, 81.67%, and 83.66%, respectively, which were within the bioequivalence criterion range of 80%–125%. The upper limits of the one-sided 95% confidence intervals of Cmax, AUC0-t, and AUC0-∞ after logarithmic transformation were −0.05, −0.04 and −0.03, respectively, which were less than 0. The difference in Tmax between these two formulations was not statistically significant according to the Wilcoxon signed-rank test (P = 0.3650 > 0.05). Therefore, the bioequivalence between the two formulations was established under fasting conditions. All adverse events were mild and transient.ConclusionThe T formulation was bioequivalent and showed a similar safety profile to the R formulation Nexavar® (Bayer AG) in healthy Chinese subjects under fasting conditions.Clinical trial registrationhttp://www.chinadrugtrials.org.cn/index.html, Identifier CTR20233578.
ISSN:1663-9812