Encyclopedia of Cancer

Living Edition
| Editors: Manfred Schwab

Deferasirox

  • Galit Granot
Living reference work entry
DOI: https://doi.org/10.1007/978-3-642-27841-9_2153-3

Synonyms

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...

Keywords

Iron Overload Mantle Cell Lymphoma Iron Chelator Transferrin Receptor Iron Chelation Therapy 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.
This is a preview of subscription content, log in to check access.

References

  1. Bedford MR, Ford SJ, Horniblow RD, Iqbal TH, Tselepis C (2013) Iron chelation in the treatment of cancer: a new role for deferasirox? J Clin Pharmacol 53:885–891CrossRefPubMedGoogle Scholar
  2. 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 541:129–137CrossRefPubMedGoogle Scholar
  3. 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 31:1741–1744PubMedGoogle Scholar
  4. Huang X (2003) Iron overload and its association with cancer risk in humans: evidence for iron as a carcinogenic metal. Mutat Res 533:153–171CrossRefPubMedGoogle Scholar
  5. 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 54:851–859CrossRefPubMedGoogle Scholar

See Also

  1. (2001) Hepatoma. In: Schwab M (ed) Encyclopedic reference of cancer. Springer, Berlin/Heidelberg, p 401. doi:10.1007/3-540-30683-8_738Google Scholar
  2. (2001) Reactive oxygen species. In: Schwab M (ed) Encyclopedic reference of cancer. Springer, Berlin/Heidelberg, pp 755–756. doi:10.1007/3-540-30683-8_1440Google Scholar
  3. (2004) Retinoblastoma (Rb) gene. In: Offermanns S, Rosenthal W (eds) Encyclopedic reference of molecular pharmacology. Springer, Berlin/Heidelberg, p 815. doi:10.1007/3-540-29832-0_1404Google Scholar
  4. (2005) Transferrin receptor. In: Vohr HW (ed) Encyclopedic reference of immunotoxicology. Springer, Berlin/Heidelberg, p 658. doi:10.1007/3-540-27806-0_1499Google Scholar
  5. (2006) Adenomatous polyposis coli. In: Ganten D et al (eds) Encyclopedic reference of genomics and proteomics in molecular medicine. Springer, Berlin/Heidelberg, p 20. doi:10.1007/3-540-29623-9_6056Google Scholar
  6. (2006) Apoptosis. In: Ganten D et al (eds) Encyclopedic reference of genomics and proteomics in molecular medicine. Springer, Berlin/Heidelberg, pp 84–85. doi:10.1007/3-540-29623-9_6191Google Scholar
  7. (2006) Cyclin D. In: Ganten D et al (eds) Encyclopedic reference of genomics and proteomics in molecular medicine. Springer, Berlin/Heidelberg, p 363. doi:10.1007/3-540-29623-9_6677Google Scholar
  8. (2006) Dishevelled. In: Ganten D et al (eds) Encyclopedic reference of genomics and proteomics in molecular medicine. Springer, Berlin/Heidelberg, p 409. doi:10.1007/3-540-29623-9_6774Google Scholar
  9. (2008) Btk (Bruton’s tyrosine kinase). In: Rédei GP (ed) Encyclopedia of genetics, genomics, proteomics and informatics. Springer, Netherlands, p 241. doi:10.1007/978-1-4020-6754-9_2087Google Scholar
  10. (2008) Frizzled. In: Offermanns S, Rosenthal W (eds) Encyclopedia of molecular pharmacology, 2nd edn. Springer, Berlin/Heidelberg, p 511. doi:10.1007/978-3-540-38918-7_5730Google Scholar
  11. (2008) GSK3 (glycogen synthase kinase 3β). In: Rédei GP (ed) Encyclopedia of genetics, genomics, proteomics and informatics. Springer, Netherlands, pp 827–828. doi:10.1007/978-1-4020-6754-9_7189Google Scholar
  12. (2008) Iron Chelator. In: Offermanns S, Rosenthal W (eds) Encyclopedia of molecular pharmacology, 2nd edn. Springer, Berlin/Heidelberg, p 665. doi:10.1007/978-3-540-38918-7_6014Google Scholar
  13. (2009) Iron. In: Manutchehr-Danai M (ed) Dictionary of gems and gemology. Springer, Berlin/Heidelberg, p 473. doi:10.1007/978-3-540-72816-0_11678Google Scholar
  14. (2012) Anemia. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 178. doi:10.1007/978-3-642-16483-5_269Google Scholar
  15. (2012) Axin. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 324. doi:10.1007/978-3-642-16483-5_496Google Scholar
  16. (2012) Beta-Catenin. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 385. doi:10.1007/978-3-642-16483-5_889Google Scholar
  17. (2012) Caspase-3. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 675. doi:10.1007/978-3-642-16483-5_874Google Scholar
  18. (2012) Cell Cycle. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 737. doi:10.1007/978-3-642-16483-5_994Google Scholar
  19. (2012) Renal Cancer. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, pp 3225–3226. doi:10.1007/978-3-642-16483-5_6575Google Scholar
  20. (2012) Sarcoma. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 3335. doi:10.1007/978-3-642-16483-5_5161Google Scholar
  21. (2012) TCF/LEF. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 3625. doi:10.1007/978-3-642-16483-5_5705Google Scholar
  22. (2012) Wnt. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 3953. doi:10.1007/978-3-642-16483-5_6255Google Scholar
  23. (2012) βTrCP. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 3777. doi:10.1007/978-3-642-16483-5_5963Google Scholar
  24. (2013) Diabetes Mellitus. In: Gebhart GF, Schmidt RF (eds) Encyclopedia of pain, 2nd edn. Springer, Berlin/Heidelberg, p 954. doi:10.1007/978-3-642-28753-4_200571Google Scholar
  25. (2008) Myelofibrosis. In: Baert AL (ed) Encyclopedia of diagnostic imaging. Springer, Berlin/Heidelberg, p 1183. doi:10.1007/978-3-540-35280-8_1626Google Scholar
  26. (2008) Myoglobin. In: Rédei GP (ed) Encyclopedia of genetics, genomics, proteomics and informatics. Springer, Netherlands, p 1314. doi:10.1007/978-1-4020-6754-9_11113Google Scholar
  27. (2008) S6K1. In: Offermanns S, Rosenthal W (eds) Encyclopedia of molecular pharmacology, 2nd edn. Springer, Berlin/Heidelberg, p 1101. doi:10.1007/978-3-540-38918-7_6664Google Scholar
  28. (2012) E3 Ubiquitin ligase. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 1184. doi:10.1007/978-3-642-16483-5_1771Google Scholar
  29. (2012) Hemoglobin. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 1646. doi:10.1007/978-3-642-16483-5_2632Google Scholar
  30. (2012) Hepatocyte. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 1677. doi:10.1007/978-3-642-16483-5_2665Google Scholar
  31. (2012) Hereditary hemochromatosis. In: Chen H (ed) Atlas of genetic diagnosis and counseling. Springer, pp 1025–1031. doi:10.1007/978-1-4614-1037-9_116Google Scholar
  32. (2012) Leukemia. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2005. doi:10.1007/978-3-642-16483-5_3322Google Scholar
  33. (2012) Liver Cancer. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2063. doi:10.1007/978-3-642-16483-5_3393Google Scholar
  34. (2012) LRP5/6. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2077. doi:10.1007/978-3-642-16483-5_3425Google Scholar
  35. (2012) Lymphoma. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2124. doi:10.1007/978-3-642-16483-5_3463Google Scholar
  36. (2012) Medullary breast carcinoma. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2199. doi:10.1007/978-3-642-16483-5_3599Google Scholar
  37. (2012) MTOR. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2384. doi:10.1007/978-3-642-16483-5_3867Google Scholar
  38. (2012) Poly(ADP-Ribose) Polymerase. In: Schwab M (ed) Encyclopedia of cancer, 3rd edn. Springer, Berlin/Heidelberg, p 2935. doi:10.1007/978-3-642-16483-5_4655Google Scholar
  39. (2013) Ischemic heart disease. In: Gebhart GF, Schmidt RF (eds) Encyclopedia of pain, 2nd edn. Springer, Berlin/Heidelberg, pp 1680–1681. doi:10.1007/978-3-642-28753-4_201097Google Scholar
  40. Angelini C (2009) Neurodegenerative disorders. In: Lang F (ed) Encyclopedia of molecular mechanisms of disease. Springer, Berlin/Heidelberg, pp 1453–1455. doi:10.1007/978-3-540-29676-8_248Google Scholar
  41. Galanello R, Origa R (2010) Beta-thalassemia. Orphanet J Rare Dis 5:11. doi:10.1186/1750-1172-5-11CrossRefPubMedPubMedCentralGoogle Scholar
  42. Gilbert P (1996) Friedrich’s ataxia. In: Gilbert P (ed) The A-Z reference book of syndromes and inherited disorders, 2nd edn. Springer, pp 123–126. doi:10.1007/978-1-4899-6918-7_32Google Scholar

Copyright information

© Springer-Verlag Berlin Heidelberg 2015

Authors and Affiliations

  1. 1.Felsenstein Medical Research Center, Beilinson Hospital, Sackler School of MedicineTel Aviv UniversityPetah TikvaIsrael