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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

Citation

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]


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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/

DOI: doi:10.2147/DDDT.S323169

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 Details

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 Division:Health
Objective Group:Clinical health
Objective Field:Efficacy of medications
UTAS Author:Wang, Z (Mr Zhiqiang Wang)
UTAS Author:Zhou, Z (Dr Zhen Zhou)
ID Code:146593
Year Published:2021
Deposited By:Menzies Institute for Medical Research
Deposited On:2021-09-14
Last Modified:2021-10-28
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