Abstract: Mitochondrion is an important organelle in cells and plays a crucial role in tumor development. Therefore, improvement of the targeting ability of anticancer drugs to mitochondria will increase the treatment efficacy for tumor and reduce the side effect on normal tissues. Here, research progresses in mitochondrial targeting have been reviewed in three aspects for tumors treatment: the potential, permeability and translocase of mitochondrial membrane. The review provides a reference for the development of mitochondria targeted therapeutic systems.