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Deferasirox

Deferasirox (marketed as Exjade) is a rationally-designed[1] 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.[1][2] It is the first oral medication approved in the USA for this purpose.[3]

It was approved by the United States Food and Drug Administration (FDA) in November 2005.[1][3] According to FDA (May 2007), renal failure and cytopenias have been reported in patients receiving deferasirox oral suspension tablets

Properties of deferasirox

Two deferasirox molecules binding iron
Two deferasirox molecules binding iron
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 molecule 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.

References





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