Photodynamic therapy (PDT) is an emerging non-invasive therapeutic approach that has been employed in preclinical treatment due to its convenient accessibility, minimal toxicity, and reduced likelihood of developing drug resistance. The photosensitizer (PS) serves as the pivotal component in photodynamic therapy, capable of producing two types of ROS when activated by light. Type I ROS depends less on oxygen, including hydroxyl radical (OH • ), superoxide radical (O2 •-) and hydrogen peroxide (H2O2), which demonstrates significant potential for hypoxia-targeted antitumor therapy. Type II ROS involves the consumption of intracellular oxygen to generate a high level of toxic singlet oxygen ( 1 O2) to ablate cancer cells, which can aggravate hypoxia in tumor microenvironment. Therefore, to some degree, PDT especially with type II ROS can accelerate the release the hypoxiaresponsive prodrugs, meanwhile, incorporation with hypoxia-responsive chemotherapy will present an appealing prospect for synergistic antitumor therapy. For example, Zhang reported a prodrug by connection of nitrogen mustard (alkylative drugs) and near infrared region photosensitizer through azo group for PDT and chemotherapy. Adopting similar strategy,