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Research progress of biomarker-activatable photosensitizers with aggregation-induced emission characteristics for photodynamic therapy. [Display omitted] • Elucidated mechanisms of reactive oxygen species generation in photodynamic therapy. • Highlighted regulation processes of reactive oxygen species in activatable aggregation-induced emission photosensitizers. • Reviewed the design strategies for biomarker-activatable aggregation-induced emission photosensitizers. • Identified the challenges faced by activatable photosensitizers and future research needs. Photodynamic therapy (PDT) is a prominent strategy in contemporary oncology for its potential to selectively eradicate cancer cells. However, the non-specific accumulation of photosensitizers (PSs) in healthy cells, particularly those in proximity to tumors, poses a significant challenge to the safety of PDT. A pivotal strategy to mitigate this issue is the development of biomarker-activatable PSs that target cancer-specific biomarkers, thereby generating reactive oxygen species (ROS) exclusively within cancer cells upon biomarker activation. Given the hydrophobic nature of conventional PSs and their tendency to aggregate in biological environments, the integration of aggregation-induced emission (AIE) characteristics is a strategic advancement. This feature ensures that PSs retain or even enhance their efficacy in aggregated states, which is crucial for effective PDT. This review provides a comprehensive overview of the recent advancements in the field of cancer biomarker-activatable AIE PSs. It delves into the design principles of these PSs, focusing on the mechanisms of photosensitization and intersystem crossing that govern their activation. Furthermore, it elucidates the influence of various biomarkers on the activation process, highlighting how they trigger the ROS generation capability of AIE PSs to execute PDT. Additionally, this review examines the challenges and future prospects of biomarker-activatable AIE PSs, offering insights to facilitate their progression towards clinical applications and enhance their therapeutic potential in cancer treatment. [ABSTRACT FROM AUTHOR]