Abstract:The prodrug strategy of oxaliplatin provides an effective solution to the problems of insufficient specificity and toxic side effects associated with oxaliplatin in tumor chemotherapy. On this basis, the photo-controlled activation strategy has been introduced into the design of oxaliplatin prodrugs, which further enables the spatiotemporally precise release of oxaliplatin and effectively improves the targeting ability and safety in tumor therapy. This article summarizes the photoactivatable oxaliplatin prodrugs and their design principles, focuses on investigating the activation mechanisms and release processes of photoactivatable oxaliplatin prodrugs under ultraviolet, visible and near-infrared light irradiation, and introduces their applications in tumor diagnosis and therapy. Finally, some challenges faced by photoactivatable oxaliplatin prodrugs and potential development directions are discussed and prospected.