Lonidamine, a new approach to cancer therapy.

The experimental and theoretical bases for the use of Lonidamine in cancer therapy are reviewed and discussed. In murine tumors Lonidamine has a narrow spectrum of antitumor effects. It lacks the characteristic properties of antiproliferative drugs, as well as other important pharmacological actions, with the exception of antispermatogenic and embryotoxic effects which are closely related to the antitumor ones. Lonidamine appears not to affect the cell division processes. Available data instead show that it specifically affects the condensed or oxidized mitochondrion; since tumor cells have a mitochondrially bound hexokinase, both respiration and glycolysis are decreased. There is some evidence that hyperthermia, X rays and some chemotherapeutic agents, when used in combination with Lonidamine, increase the response of tumor cells or systems to this drug.