Deferasirox

Deferasirox is an orally bioavailable tridentate iron chelator. It is selective for iron (Fe(III)) over Cu(II), Zn(II), Mg(II), and Ca(II) but does bind to Al(III). Deferasirox decreases iron levels in iron-loaded rat heart cells in vitro by 45.8 and 55.6% compared to control levels when used at concentrations of 160 and 320 µM, respectively. Deferasirox also inhibits proliferation of SAS human oral squamous carcinoma cells (EC50 = 21 µM), decreases cyclin D1 protein levels, and increases protein levels of N-Myc downregulated gene 1 (NDRG1) and NDRG3.