Mitochondria‐targeted photodynamic therapy (Mt‐PDT), which enables the photogenerated cytotoxic oxygen species with fatal oxidative damage to block mitochondrial functions, has been considered as a promising method to enhance the anticancer effectiveness. Aiming at the challenges of PDT, in the past few decades, numerous mitochondria‐targeting molecular agents have been developed to boost the PDT efficacy via directly destroying the mitochondria or activating mitochondria‐mediated cell death pathways. Herein, a review for recent advances of Mt‐PDT is highlighted including: mitochondrial targeting design principles and strategies, therapeutic performance of mitochondria‐targeted agents‐mediated PDT as well as the agent‐free Mt‐PDT. In addition, it puts together the achievements of the combinatory mitochondria‐anchoring PDT and other anticancer strategies, demonstrating the advantages provided by Mt‐PDT. The existing challenges are discussed and future settlements for the development of mitochondria‐specific agents are also forecasted.

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