The induction of regulated cell death (RCD) through photo/ultrasound sensitization therapeutic agents has gained significant attention as a vital approach to combat drug resistance in tumors. Aggregation‐induced emission (AIE) therapeutic agents generate reactive oxygen species through photo/ultrasound activation, which can synergize with RCD inducers or directly induce RCD, ultimately resulting in the death of tumor cells. The presented comprehensive review delves into recent advancements in AIE therapeutic agents designed to trigger RCD or synergize with RCD inducers, encompassing apoptosis, necroptosis, pyroptosis, immunogenic cell death, autophagy, ferroptosis, and cuproptosis. Additionally, the intricate regulatory mechanisms through which activatory‐AIE therapeutics influence distinct RCD pathways are examined. A forward‐looking perspective on future developments and pertinent challenges within this exciting realm is presented, anticipating the continued evolution of activatable AIE therapeutics as a transformative approach to enhance tumor therapy.