Photodynamic therapy (PDT), as an efficient treatment method, has the advantages of low toxicity, non-invasiveness and controllability, which has been widely used in the treatment of proliferative skin diseases and tumors.However, the reported PDT photosensitizers still face many challenges in practical biological applications, such as the efficacy of PDT is significantly reduced by the tumor hypoxic environment; the poor targeting of photosensitizers can easily cause damage to normal tissues.In order to solve the above problems, researchers have proposed many effective strategies to improve the therapeutic efficacy of organic photosensitizers.Herein, the structure and property regulation strategies of organic photosensitizers are reviewed.In addition, the practical applications of photosensitizers in antitumor, antibacterial therapy, and afterglow imaging are introduced.In the end, the design strategies of organic small molecule photosensitizers are summarized and prospected in order to promote the development of this field.