Significant advancements have been noticed in cancer therapy for decades. Despite this, there are still many critical challenges ahead, including multidrug resistance, drug instability, and side effects. To overcome obstacles of these problems, various types of materials in biomedical research have been explored. Chief among them, the applications of natural compounds have grown rapidly due to their superb biological activities. Natural compounds, especially polyphenolic compounds, play a positive and great role in cancer therapy. Tannic acid (TA), one of the most famous polyphenols, has attracted widespread attention in the field of cancer treatment with unique structural, physicochemical, pharmaceutical, anticancer, antiviral, antioxidant and other strong biological features. This review concentrated on the basic structure along with the important role of TA in tuning oncological signal pathways firstly, and then focused on the use of TA in chemotherapy and preparation of delivery systems including nanoparticles and hydrogels for cancer therapy. Besides, the application of TA/Fe³⁺ complex coating in photothermal therapy, chemodynamic therapy, combined therapy and theranostics is discussed.