Summary
Expert Opinion on Therapeutic Patents
November 2006, Vol. 16, No. 11, Pages 1533-1556
(doi:10.1517/13543776.16.11.1533)

Iron chelators as therapeutic iron depletion agents
Noah Birch‌1, Xiang Wang‌1 & Hyun-Soon Chong‌1
1Chemistry Division, Biological, Chemical and Physical Sciences
Department,Illinois Institute of Technology, Chicago, IL 60616, USA.
Chong@iit.edu
† Author for correspondence

The great promise of iron depletion as a therapeutic strategy for
various diseases, including iron overload, cancers, Alzheimer’s
disease, Parkinson’s disease, tuberculosis, HIV, and fungal and
malaria infection, has stimulated research on the development of iron
chelators as iron depletion agents. In November 2005, the FDA approved
deferasirox (ICL670A; Exjade®), the first once-daily oral drug for
treatment of chronic iron overload. So far, five iron chelators,
deferoxamine, deferiprone, deferasirox, dexrazorane and ciclopirox,
have been approved for use in iron overload, anticancer or antifungal
therapy. Triapine® is in Phase I and II clinical trials for the
treatment of various metastatic and solid cancers. A desferrithiocin
analogue, deferitrin, is presently in a Phase I trial for the
treatment of iron overload diseases. Among the iron chelators being
evaluated in preclinical settings are the analogues of deferiprone,
pyridoxal isonicotinoyl hydrazone, desferrithiocin, deferoxamine,
thiosemicarbazone, tachpyridine, N,N'-bis(2-
hydroxybenzyl)ethylenediamine-N,N'-diacetic acid and hydroxyquinoline.
This review describes the comparative properties of iron chelators in
clinical use and evaluates the patent status of the novel synthetic
iron chelators in preclinical settings.

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