Cancer is the second leading cause of death in the world. The available treatments have a number of limitations, such as side effects and low efficiency. In the search for new treatments, mitochondria have been highlighted as a promising target for cancer treatment due to the existence of an important relationship between mitochondrial dysfunction and tumourigenesis. Thus, an increase in the number of studies has been observed in recent years, with interest in compounds with action on mitochondrial targets ('mitocans') as an alternative for the treatment of cancer. The aim of this narrative review was to describe the advances in cancer therapy with the emergence of mitochondrial drugs.