NCIt definition : An orally bioavailable biguanide compound and mitochondrial oxidative phosphorylation
(OxPhos) inhibitor, with potential antineoplastic activity. Upon administration, lixumistat
inhibits oxidative phosphorylation, decreases mitochondrial function, prevents tumor
cell metabolism and deprives tumor cells of energy, thereby preventing tumor cell
proliferation. Mitochondrial OxPhos is overactivated in cancer cells and plays a key
role in tumor cell proliferation. Drug resistant tumor cells are very susceptible
to decreased mitochondrial OxPhos as they cannot easily compensate for the decrease
in mitochondrial function by increasing glycolysis.;