The oncology drug elesclomol selectively transports copper to the mitochondria to induce oxidative stress in cancer cells

► Elesclomol is a novel investigational drug with potent anticancer activity. ► Elesclomol chelates extracellular copper and enters cells as elesclomol-Cu(II). ► The elesclomol-Cu(II) complex is rapidly and selectively transported to mitochondria. ► Cu(II) is reduced to Cu(I), leading to reactive oxygen species and apoptosis. ► This unique mechanism of action can be exploited for therapeutic benefit.