Effect of food, type of food, and time of food intake on deferasirox bioavailability: Recommendations for an optimal deferasirox administration regimen

Renzo Galanello, Antonio Piga, Maria Domenica Cappellini, Gian Luca Forni, Antonella Zappu, Raffaella Origa, Catherine Dutreix, Rossella Belleli, John M. Ford, Gilles Jacques Rivière, Sébastien Balez, Daniele Alberti, Romain Séchaud

Research output: Contribution to journalArticle

Abstract

Deferasirox (ICL670) is representative of a new class of tridentate iron chelators, formulated as tablets for dispersion. Deferasirox has exhibited high potency and a clinically manageable safety profile in preclinical models and in an extensive clinical program. The effect of food and time of food intake on the pharmacokinetics of deferasirox was investigated in healthy volunteers and patients with transfusional hemosiderosis. The bioequivalence of a single oral dose of deferasirox (20 mg/kg) was assessed following administration either before a high-fat or standard breakfast or concurrent with a standard breakfast in comparison with fasted conditions in healthy volunteers. The bioavailability of deferasirox was determined following a single oral dose (20 mg/kg) under fed and fasted conditions in patients. These data show that the type of food, caloric content, and fat content of the meal influence the bioavailability of deferasirox when consumed concomitantly. In contrast, this is not the case when deferasirox is administered at least 30 minutes before a meal. In conclusion, it is recommended that deferasirox be administered at least 30 minutes prior to meals. When this is not feasible, deferasirox should be administered consistently at the same time before meals to limit the sources of variability that affect absorption.

Original languageEnglish
Pages (from-to)428-435
Number of pages8
JournalJournal of Clinical Pharmacology
Volume48
Issue number4
DOIs
Publication statusPublished - Apr 2008

Keywords

  • Bioavailability
  • Chelation
  • Deferasirox
  • Exjade
  • Food effect
  • ICL670
  • Intake time
  • Iron overload

ASJC Scopus subject areas

  • Pharmacology (medical)
  • Pharmacology, Toxicology and Pharmaceutics(all)

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  • Cite this

    Galanello, R., Piga, A., Domenica Cappellini, M., Luca Forni, G., Zappu, A., Origa, R., Dutreix, C., Belleli, R., Ford, J. M., Rivière, G. J., Balez, S., Alberti, D., & Séchaud, R. (2008). Effect of food, type of food, and time of food intake on deferasirox bioavailability: Recommendations for an optimal deferasirox administration regimen. Journal of Clinical Pharmacology, 48(4), 428-435. https://doi.org/10.1177/0091270007313327