Definition
Deferasirox is a rationally designed orally administered iron chelator.
Characteristics
Pharmacological Properties
Deferasirox is a rationally designed oral iron chelator.
Deferasirox is indicated for the treatment of chronic iron overload in patients who are receiving long-term blood transfusions for conditions such as β-thalassemia and other chronic anemias. It was approved by the United States Food and Drug Administration (FDA) in November 2005. It is the first oral medication approved in the USA for this purpose.
Its low molecular weight and high lipophilicity allows the drug to be taken orally unlike deferoxamine (DFO) which has to be administered by IV route. The half-life of deferasirox is between 8 and 16 h allowing once a day dosing. Deferasirox is capable of removing iron from cells as well as removing iron from the blood. Deferasirox is a tridentate iron chelator with high affinity for iron as Fe3+; two molecules of deferasirox bind to...
References
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Chantrel-Groussard K, Gaboriau F, Pasdeloup N, Havouis R, Nick H, Pierre JL, Brissot P, Lescoat G (2006) The new orally active iron chelator ICL670A exhibits a higher antiproliferative effect in human hepatocyte cultures than O-trensox. Eur J Pharmacol 541:129–137
Fukushima T, Kawabata H, Nakamura T, Iwao H, Nakajima A, Miki M, Sakai T, Sawaki T, Fujita Y, Tanaka M, Masaki Y, Hirose Y, Umehara H (2011) Iron chelation therapy with deferasirox induced complete remission in a patient with chemotherapy-resistant acute monocytic leukemia. Anticancer Res 31:1741–1744
Huang X (2003) Iron overload and its association with cancer risk in humans: evidence for iron as a carcinogenic metal. Mutat Res 533:153–171
Vazana-Barad L, Granot G, Mor-Tzuntz R, Levi I, Dreyling M, Nathan I, Shpilberg O (2013) Mechanism of the antitumoral activity of deferasirox, an iron chelation agent, on mantle cell lymphoma. Leuk Lymphoma 54:851–859
See Also
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Granot, G. (2015). Deferasirox. In: Schwab, M. (eds) Encyclopedia of Cancer. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-27841-9_2153-3
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