Deferasirox (Fe3+ chelate)

Deferasirox Fe3+ chelate is a rationally-designed oral iron chelator; its main use is to reduce chronic iron overload in patients who are receiving long-term blood transfusions for conditions such as beta-thalassemia and other chronic anemias.

Signaling Pathways >> Others >> Others

Research Areas >> Others

Deferasirox is the first oral medication approved in the USA for this purpose. The half-life of deferasirox is between 8 and 16 hours allowing once a day dosing. Two molecules of deferasirox are capable of binding to 1 atom of iron which are subsequently eliminated by fecal excretion. Its low molecular weight and high lipophilicity allows the drug to be taken orally unlike desferoxamine which has to be administered by IV route (intravenous infusion). Together with deferiprone, deferasirox seems to be capable of removing iron from cells (cardiac myocytes and hepatocytes) as well as removing iron from the blood.

[1]. Yang LP, Keam SJ, Keating GM. Deferasirox : a review of its use in the management of transfusional chronic iron overload. Drugs. 2007;67(15):2211-30.

[2]. Kontoghiorghes GJ. Introduction of higher doses of deferasirox: better efficacy but not effective iron removal from the heart and increased risks of serious toxicities. Expert Opin Drug Saf. 2010 Jul;9(4):633-41.

[3]. Galanello R, Campus S, Origa R. Deferasirox: pharmacokinetics and clinical experience. Expert Opin Drug Metab Toxicol. 2012 Jan;8(1):123-34.

[4]. Donnelly JP, Lahav M. Deferasirox as adjunctive therapy for mucormycosis. J Antimicrob Chemother. 2012 Mar;67(3):519-20.

[5]. Lui GY, Obeidy P, Ford SJ et al. The Iron Chelator, Deferasirox, as a Novel Strategy for Cancer Treatment: Oral Activity Against Human Lung Tumor Xenografts and Molecular Mechanism of Action. Mol Pharmacol. 2012 Oct 16. [Epub ahead of print]

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