In the current cancer treatment, various combination therapies have been widely used, such as photodynamic therapy (PDT) combined with chemokinetic therapy (CDT). However, due to the complexity of the tumor microenvironment (TME) and the limitations of treatment, the efficacy of current treatment options for some cancers is unsatisfactory. Nowadays, cascade technology has been used in cancer treatment and achieved good therapeutic effect. Cascade technology based on nanotechnology can trigger cascade reactions under specific tumor conditions to achieve precise positioning and controlled release, or amplify the efficacy of each drug to improve anticancer efficacy and reduce side effects. Compared with the traditional treatment, the application of cascade technology has achieved the controllability, specificity, and effectiveness of cancer treatment. This paper reviews the application of cascade technology in drug delivery, targeting, and release via nano-drug delivery systems in recent years, and introduces their application in reactive oxygen species (ROS)-induced cancer treatment. Finally, we briefly describe the current challenges and prospects of cascade technology in cancer treatment in the future.