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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

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Zhang, Q, Wang, Z, Wu, J, Zhou, Z ORCID: 0000-0002-0835-8686, Zhou, R and Hu, W 2021 , '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 , 3277–3288 , doi: 10.2147/DDDT.S323169.

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Abstract

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: Article
Authors/Creators:Zhang, Q and Wang, Z and Wu, J and Zhou, Z and Zhou, R and Hu, W
Keywords: regorafenib, phase 1, pharmacokinetic, bioequivalence, Chinese healthy volunteers
Journal or Publication Title: Drug Design, Development and Therapy
Publisher: Dove Press Limited
ISSN: 1177-8881
DOI / ID Number: 10.2147/DDDT.S323169
Copyright Information:

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/

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