Elacridar

A potent inhibitor of multidrug resistance (MDR) that fully reverses multidrug resistance CHRC5, OV1/DXR and MCF7/ADR cells to the cytotoxicity of doxorubicin and vincristine with IC50 of 0.02 uM; effectively competes with [3H]azidopine for binding P-glycoprotein; restores sensitivity of the tumor to a single dose of doxorubicin in mice; orally bioavailable.Breast Cancer Phase 1 Discontinued (In Vitro) :Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells.Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines.Elacridar (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells. (In Vivo) :Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma.