Lonidamine (LNA) has been investigated both alone and in combination with different chemotherapeutic agents in various types of tumors at an advanced stage. Acute and long-term treatments were studied. LNA has been shown to be devoid of the most typical side effects of currently used chemotherapeutic agents. It has revealed a characteristic profile of side effects, comprising myalgia, photosensitivity and altered hearing. LNA alone, tested in a limited number of patients, produced a partial remission in one ovary adenocarcinoma and a stabilization in two breast carcinomas and one microcytoma. When used in combination with chemotherapeutic agents, it potentiated them, particularly in brain metastases and lung adenocarcinomas.