Abstract: Mitochondria is the "Energy Factory" of the human body. It participates in many physiological activities such as cell energy metabolism, signal transduction, cell differentiation, and plays an important role in the occurrence and development of cancer. In recent years, targeting mitochondria has become a new strategy for cancer treatment, and has attracted extensive attention in the medical field. In this paper, the current mitochondrial targeting small molecule drugs were reviewed in order to provide valuable reference for the research in this field.