lonidamine

Lonidamine is a small molecule drug originally developed for its potential use in cancer treatment. It acts as an inhibitor of key metabolic pathways in cancer cells by interfering with energy metabolism—principally inhibiting aerobic glycolytic activity through its effect on mitochondrially-bound hexokinase (HK). This inhibition impairs energy-requiring processes such as recovery from potentially lethal damage induced by radiation and some cytotoxic drugs. Lonidamine also inhibits lactate export via proton-linked monocarboxylate transporters (MCT), pyruvate uptake into mitochondria via the mitochondrial pyruvate carrier (MPC), and respiration at mitochondrial electron transport chain Complex II and possibly Complex I. The drug has selective activity against a broad range of tumors with little to no effect on normal tissues at doses below ~400 mg/m²[1][4][7]. It has been used clinically in combination with other anticancer agents for various cancers and has shown radiosensitizing effects[7][9].

Brand names

DoridaminaLonidamin

Other names

1-(2,4-dichlorbenzyl)-indazole-3-carboxylic aciddiclondazolic acidlonidaminalonidaminum