Deferasirox

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Image:Deferasirox.svg
Deferasirox
Systematic (IUPAC) name
[4-[(3Z,5E)-3,5-bis(6-oxo-1-cyclohexa-2,4-
dienylidene)-1,2,4-triazolidin-1-yl]benzoic acid
Identifiers
CAS number 201530-41-8
ATC code  ?
PubChem 5493381
Chemical data
Formula C21H15N3O4 
Mol. mass 373.362 g/mol
Pharmacokinetic data
Bioavailability 70%
Protein binding 99%
Metabolism Hepatic glucuronidation
Half life 8 to 16 hours
Excretion Fecal (84%) and renal (8%)
Therapeutic considerations
Pregnancy cat.

C(AU) B(US)

Legal status

-only(US)

Routes Oral

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][1] It is the first oral medication approved in the USA for this purpose.[1]

It was approved by the United States Food and Drug Administration (FDA) in November 2005.[1][1]

Properties of deferasirox

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


Acknowledgement and Attribution Regarding Sources of Content

Some of the initial content on this page may be incorporated in part from copyleft sources in the public domain including wikis such as Wikipedia and AskDrWiki. Drug information for patients came from the The National Library of Medicine. Infectious disease information may have come from the Centers for Disease Control (CDC). Differential Diagnoses are drawn from clinicians as well as an amalgamation of 3 sources: 1.The Disease Database; 2. Kahan, Scott, Smith, Ellen G. In A Page: Signs and Symptoms. Malden, Massachusetts: Blackwell Publishing, 2004:3; 3. Sailer, Christian, Wasner, Susanne. Differential Diagnosis Pocket. Hermosa Beach, CA: Borm Bruckmeir Publishing LLC, 2002:7 .

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