Aggregation‐Induced Emission Luminogens (AIEgens): From Intrinsic Therapeutic Effect to Sensitization of Conventional Antitumor Modalities

Traditional cancer treatment methods, such as chemotherapy, radiotherapy, and immunotherapy, are often limited by poor treatment efficacy, poor targeting, and adverse side effects, as well as intrinsic or acquired drug resistance, which are mainly caused by the complex and immunosuppressive tumor microenvironment. The development of aggregation‐induced emission (AIE) photosensitizers provides a promising strategy to address these challenges. In addition to being high‐performance imaging agents, AIE luminogens (AIEgens) have inherent phototherapeutic capabilities, including photodynamic and photothermal effects, which can directly achieve tumor ablation. More importantly, they can act as multifunctional sensitizers to enhance the efficacy of traditional anti‐cancer treatments, reverse drug resistance, alleviate tumor hypoxia, and reshape the immune microenvironment. This review summarizes the basic mechanisms and rational design of AIEgens, emphasizing their transformation from independent therapeutic agents to synergistic sensitizers for combined treatment. By combining imaging guidance, intrinsic therapy, and enhanced treatment sensitivity technologies, the AIEgens‐based system provides a new model for precise, efficient, and safe integrated tumor diagnosis and treatment, which has profound significance for future clinical applications.