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

Author(s): Galanello R, Piga A, Cappellini MD, Forni GL, Zappu A, Origa R, Dutreix C, Belleli R, Ford JM, Riviere GJ, Balez S, Alberti D, Sechaud R

Affiliation(s): Ospedale Regionale Microcitemie, Dipartimento di Scienze, Biomediche e Biotechnologie, Universita di Cagliari, Italy.

Publication date & source: 2008-04, J Clin Pharmacol., 48(4):428-35. Epub 2008 Feb 15.

Publication type: Randomized Controlled Trial; Research Support, Non-U.S. Gov't

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.