Deferasirox

Deferasirox, sold under the brand name Exjade & Asunra (in injectable form) & Oleptiss (Tablet formulation) both by Novartis among others, is an 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. It is the first oral medication approved in the United States for this purpose.

Deferasirox
Clinical data
Pronunciationde FER a sir ox
Trade namesExjade, Jadenu
Other namesCGP-72670, ICL-670A, IC L670
AHFS/Drugs.comMonograph
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth
ATC code
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: WARNINGRx-only
  • EU: Rx-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability70%
Protein binding99%
MetabolismHepatic glucuronidation
Elimination half-life8 to 16 hours
ExcretionFecal (84%) and renal (8%)
Identifiers
  • 4-(3,5-Bis(2-hydroxyphenyl)-1H-1,2,4-triazol-1-yl)benzoic acid
CAS Number
PubChem CID
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.211.077
Chemical and physical data
FormulaC21H15N3O4
Molar mass373.368 g·mol−1
3D model (JSmol)
Density1.4±0.1 g/cm3
  • OC(=O)c1ccc(cc1)n2nc(nc2c3ccccc3O)c4ccccc4O
  • InChI=1S/C21H15N3O4/c25-17-7-3-1-5-15(17)19-22-20(16-6-2-4-8-18(16)26)24(23-19)14-11-9-13(10-12-14)21(27)28/h1-12,25-26H,(H,27,28) Y
  • Key:BOFQWVMAQOTZIW-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

It was approved by the U.S. Food and Drug Administration (FDA) in November 2005. According to the FDA (May 2007), kidney failure and cytopenias have been reported in patients receiving deferasirox tablets for oral suspension. It is approved in the European Union by the European Medicines Agency (EMA) for children six years and older for chronic iron overload from repeated blood transfusions. It is on the World Health Organization's List of Essential Medicines.

In July 2020, Teva decided to discontinue deferasirox. It is available as a generic medication.

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