Zhang, Q and Wang, Z and Wu, J and Zhou, Z and Zhou, R and Hu, W, Bioequivalence and pharmacokinetic evaluation of two oral formulations of regorafenib: An open-label, randomised, single-dose, two-period, two-way crossover clinical trial in healthy Chinese volunteers under fasting and fed conditions, Drug Design, Development and Therapy pp. 3277-3288. ISSN 1177-8881 (2021) [Refereed Article]
Copyright 2021 Zhang et al. Licensed under Creative Commons Attribution-NonCommercial 3.0 Unported (CC BY-NC 3.0) https://creativecommons.org/licenses/by-nc/3.0/
Background: Regorafenib is an oral multi-kinase inhibitor approved for the treatment of solid tumours, but the pharmacokinetic profile of regorafenib in the Chinese population is unclear.
Objective: The aim of this study was to examine the pharmacokinetics, bioequivalence, and safety of two formulations of regorafenib 40 mg in healthy Chinese volunteers under fed and fasting conditions.
Methods: A single-centre, randomised, open-label, two-period, two-way crossover phase 1 trial was conducted by randomising a single oral dose of test (T) or reference (R, Stivarga®) regorafenib (40 mg) to healthy Chinese volunteers under both fasting and fed conditions (high-fat and high-calorie diet). Pharmacokinetic parameters were calculated using non-compartmental methods. Adverse events were recorded to assess drug safety.
Results: Sixty-six participants were enrolled for both fasting and fed treatments. The 90% CIs geometric least-square means of ratioT/R for regorafenib were completely contained within the equivalence margin of 80-125% under both fasting and fed conditions. Both formulations displayed similar and generally good safety profiles.
Conclusion: Single oral dose of the T (40 mg) and R (40 mg) regorafenib was bioequivalent under fasting and fed conditions and had similar favourable safety profiles among healthy Chinese volunteers.
|Item Type:||Refereed Article|
|Keywords:||regorafenib, phase 1, pharmacokinetic, bioequivalence, Chinese healthy volunteers|
|Research Division:||Health Sciences|
|Research Group:||Other health sciences|
|Research Field:||Other health sciences not elsewhere classified|
|Objective Group:||Clinical health|
|Objective Field:||Efficacy of medications|
|UTAS Author:||Wang, Z (Mr Zhiqiang Wang)|
|UTAS Author:||Zhou, Z (Dr Zhen Zhou)|
|Deposited By:||Menzies Institute for Medical Research|
|Downloads:||5 View Download Statistics|
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