Lonidamine is a derivative of indazole-3-carboxylic acid, which for a long time, has been known to inhibit aerobic glycolysis in cancer cells.

Later studies in Ehrlich ascites tumor cells showed that lonidamine inhibits both respiration and glycolysis leading to a decrease in cellular ATP.

[1] Clinical trials of lonidamine in combination with other anticancer agents for a variety of cancers has begun.

This is due to its proven ability to inhibit energy metabolism in cancer cells, and to enhance the activity of anticancer agents.

[2] An in-vitro study showed that a combination of temozolomide and lonidamine at clinically achievable, low plasma concentrations, could inhibit tumour growth, and lonidamine could reduce the dose of temozolomide required for radiosensitization of brain tumours.