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Effect of Food, Type of Food, and Time of Food Intake on Deferasirox Bioavailability: Recommendations for an Optimal Deferasirox Administration Regimen

From Ospedale Regionale Microcitemie, Dipartimento di Scienze, Biomediche e Biotecnologie, Università di Cagliari, Italy (Dr Galanello, Dr Zappu, Dr Origa); Centro Microcitemie, Dipartmento di Scienze Pediatriche, Università di Torino, Italy (Dr Piga); Centro Anemie Congenite, Ospedale Policlinico IRCCS, Università di Milano, Milan, Italy (Dr Cappellini); Centro della Microcitemia e delle Anemie Congenite, Odpedale Galliera, Genova, Italy (Dr Forni); Novartis Pharma AG, Basel, Switzerland (Dr Dutreix, Ms Belleli, Dr Ford, Dr Séchaud); Novartis Pharma AG, Rueil Malmaison, France (Dr Rivière, Dr Balez); and Novartis Pharma AG, Origgio, Italy (Dr Alberti).

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.

Key Words: Iron overload • chelation • food effect • intake time • bioavailability • Exjade • ICL670 • deferasirox

Address for correspondence: Romain Séchaud, Exploratory Development—Global Pharmacokinetics/Pharmacodynamics, Novartis Pharma AG, WSJ-210.4.020, CH-4002 Basel, Switzerland; e-mail: romain.sechaud{at}novartis.com.

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				R. Sechaud, A. Robeva, R. Belleli, and S. Balez Absolute Oral Bioavailability and Disposition of Deferasirox in Healthy Human Subjects J. Clin. Pharmacol., August 1, 2008; 48(8): 919 - 925. [Abstract] [Full Text] [PDF]