tcsc0901 Deferasirox

Deferasirox (ICL 670) is an orally available iron chelator used for the management of transfusional iron overload.

In Vitro: In LX-2 cells treated with 50 μM deferasirox for 12 h, α1(I)procollagen expression is decreased by 25%, with maximal reductions (10-fold) seen following 24-120 h of treatment. Similarly, α-smooth muscle actin (αSMA) expression is significantly lower^[1]. Deferasirox had anti-proliferative effects on HL-60 or KG-1 myeloid leukemia cell lines at a concentration as low as 5 μM . The cytotoxicity is both dose and time dependent^[2]. The viability of both EL4 cells and L1210 cells incubated with deferasirox decrease in a concentration-dependent manner^[3].

In Vivo: The tumor is significantly smaller in the SIO mice treated with deferasirox compared with control. Mice treated with DFX showed longer survival than the other groups. Deferasirox has a survival benefit for SIO leukemia murine model in terms of iron chelation and antileukemic therapy^[3].