Photodynamic therapy (PDT) is an established clinical treatment technology which utilizes excitation light of a specific wavelength to activate photosensitizers (PSs) to generate reactive oxygen species (ROS), which leads to cancer cell death. Over the past decades of PDT research, progress have been made in the development of PSs. However, many inherent characteristics of traditional PSs have caused various problems in PDT, such as low treatment efficiency at aggregation state and shallow treatment depth. In solution to these problems, aggregation-induced emission (AIE)-based PSs have been reported in recent years. Here, this article reviews the design strategy and the biomedical applications of AIE PSs in detail, which begins with a summary of traditional PSs for a comparison between traditional PSs and AIE PSs. Subsequently, the different functional AIE PSs in photodynamic cancer cells ablation and image-guided therapy are discussed in detail taking controllable excitation wavelength, stimulus response and PDT/photothermal therapy synergistic effect as examples. These studies have demonstrated the great potential of AIE PSs as effective theranostic agents. And the review provides references for the development of new PSs and hopefully spur research interest in AIE PSs for future clinical application.