Iron chelation in the treatment of cancer: a new role for deferasirox?

J Clin Pharmacol. 2013 Sep;53(9):885-91. doi: 10.1002/jcph.113. Epub 2013 Jun 6.


Iron plays a crucial role in a number of metabolic pathways including oxygen transport, DNA synthesis, and ATP generation. Although insufficient systemic iron can result in physical impairment, excess iron has also been implicated in a number of diseases including ischemic heart disease, diabetes, and cancer. Iron chelators are agents which bind iron and facilitate its excretion. Experimental iron chelators have demonstrated potent anti-neoplastic properties in a number of cancers in vitro. These agents have yet to be translated into clinical practice, however, largely due to the significant side effects encountered in pre-clinical models. A number of licensed chelators, however, are currently in clinical use for the treatment of iron overload associated with certain non-neoplastic diseases. Deferasirox is one such agent and the drug has shown significant anti-tumor effects in a number of in vitro and in vivo studies. Deferasirox is orally administered and has demonstrated a good side effect profile in clinical practice to date. It represents an attractive agent to take forward into clinical trials of iron chelators as anti-cancer agents.

Keywords: cancer; chelators; deferasirox; iron; tumorigenesis.

Publication types

  • Review

MeSH terms

  • Animals
  • Antineoplastic Agents / pharmacology
  • Antineoplastic Agents / therapeutic use*
  • Benzoates / pharmacology
  • Benzoates / therapeutic use*
  • Deferasirox
  • Deferiprone
  • Deferoxamine / therapeutic use
  • Humans
  • Iron Chelating Agents / pharmacology
  • Iron Chelating Agents / therapeutic use*
  • Neoplasms / drug therapy*
  • Pyridones / therapeutic use
  • Triazoles / pharmacology
  • Triazoles / therapeutic use*


  • Antineoplastic Agents
  • Benzoates
  • Iron Chelating Agents
  • Pyridones
  • Triazoles
  • Deferiprone
  • Deferoxamine
  • Deferasirox