Deferasirox

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Background

Deferasirox is an iron chelator [1].
Iron chelate is a soluble complex of iron, sodium and a chelating agent and used to make the iron soluble in water. Iron chelators were initially developed for the treatment of iron overload for clinical use [1].
Deferasirox is an orally iron chelator used for the treatment of iron-overload disease. In DMS-53 lung carcinoma and SK-N-MC neuroepithelioma cell lines, deferasirox inhibited cells proliferation. Deferasirox inhibited iron uptake from human transferrin and mobilized cellular 59Fe [1]. In two oesophageal adenocarcinoma cell lines OE33 and OE19, deferasirox with a standard chemotherapeutic agent inhibited cellular viability and proliferation [2].
In nude mice bearing DMS-53 lung carcinoma xenografts, deferasirox inhibited tumor growth. Also, deferasirox increased cleaved caspase-3, cleaved poly(ADP-ribose) polymerase 1, the cyclin-dependent kinase inhibitor p21CIP1/WAF1 and the expression of the metastasis suppressor protein N-myc downstream-regulated gene 1 while reducing cyclin D1, which suggested deferasirox is an effective antitumor agent [1]. In human xenograft models, deferasirox significantly inhibited tumour growth, which was associated with the decrease in iron levels [2].

[1]. Lui GY, Obeidy P, Ford SJ, et al. The iron chelator, deferasirox, as a novel strategy for cancer treatment: oral activity against human lung tumor xenografts and molecular mechanism of action. Mol Pharmacol, 2013, 83(1): 179-190.
[2]. Ford SJ, Obeidy P, Lovejoy DB, et al. Deferasirox (ICL670A) effectively inhibits oesophageal cancer growth in vitro and in vivo. Br J Pharmacol, 2013, 168(6): 1316-1328.