Seminars in Hematology
Volume 44 , Pages S12-S15 , April 2007

Deferasirox (Exjade®, ICL670) Preclinical Overview

  • Hanspeter Nick

      Affiliations

    • Corresponding Author InformationAddress correspondence to Hanspeter Nick, PhD, Novartis Pharma AG, Lichtstrasse 35, CH-4002 Basel, Switzerland.

References 

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  2. Delea TE, Sofrygin O, Baladi JF, et al. Costs and consequences of inadequate compliance with deferoxamine therapy in patients with transfusion-dependent thalassemia. Blood. 2005;106(11):3134;abstr
  3. Modell B, Khan M, Darlison M. Survival in β-thalassaemia major in the UK: Data from the UK Thalassaemia Register. Lancet. 2000;355:2051–2052
  4. Acklin P. A molecular-mechanics approach for the prediction of the geometry of high-spin feIII complexes with oxygen and nitrogen as coordinating atoms. Helvetica Chima Acta. 2000;83:677
  5. Nick H, Acklin P, Lattmann R, et al. Development of tridentate iron chelators: from desferrithiocin to ICL670. Curr Med Chem. 2003;10:1065–1076
  6. Steinhauser S, Heinz U, Bartholoma M, et al. Complex formation of ICL670 and related ligands with Fe III and Fe II. Eur J Inorg Chem. 2004;21:4177–4192
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  8. Wood JC, Otto-Duessel M, Gonzales I, et al. ICL670 removes cardiac iron in a gerbil model of iron overload. Blood. 2005;106(11):2695;abstr
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  10. Hershko C, Konijn AM, Nick HP, et al. ICL670A: A new synthetic oral chelator: Evaluation in hypertransfused rats with selective radioiron probes of hepatocellular and reticuloendothelial iron stores and in iron-loaded rat heart cells in culture. Blood. 2001;97:1115–1122
  11. Nick H, Wong A, Acklin P, et al. ICL670A: Preclinical profile. Adv Exp Med Biol. 2002;509:185–203
  12. Galanello R, Piga A, Alberti D, et al. Safety, tolerability, and pharmacokinetics of ICL670, a new orally active iron-chelating agent in patients with transfusion-dependent iron overload due to beta-thalassemia. J Clin Pharmacol. 2003;43:565–572
  13. Cappellini MD, Cohen A, Piga A, et al. A Phase III study of deferasirox (ICL670), a once-daily oral iron chelator, in patients with beta-thalassemia. Blood. 2006;107:3455–3462
  14. Vichinsky E, Fischer R, Fung E, et al. A randomized, controlled phase II trial in sickle cell disease patients with chronic iron overload demonstrates that the once-daily oral iron chelator deferasirox (Exjade®, ICL670) is well tolerated and reduces iron burden. Blood. 2005;106(11):313;abstr
  15. Galanello R, Piga A, Forni G-L, et al. Phase II clinical evaluation of deferasirox, a once-daily oral chelating agent, in paediatric patients with b-thalassaemia major. Haematologica. 2006;91:1343–1351
  16. Piga A, Galanello R, Forni G-L, et al. Randomized phase II trial of deferasirox (Exjade®, ICL670), a once-daily, orally-administered iron chelator, in comparison to deferoxamine in thalassemia patients with transfusional iron overload. Haematologica. 2006;91:873–880
  17. Cazzola M, Gattermann N, Greenberg P, et al. ICL670, a once-daily iron chelator, is effective and well tolerated in patients with myelodysplastic syndrome (MDS) and iron overload. Haematologica. 2005;90(suppl 2):306

PII: S0037-1963(07)00056-X

doi: 10.1053/j.seminhematol.2007.03.005

Seminars in Hematology
Volume 44 , Pages S12-S15 , April 2007

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