Abstract: The TGF-β signaling pathway affects various biological processes of cancers, including proliferation, invasion, metastasis, angiogenesis, and immune escape. Currently, multiple drugs targeting this pathway are in clinical trial stage, which involve three aspects of TGF-β, namely, production, activation, and signal transduction. Based on current evidence, the therapeutic effect of TGF-β monotherapy on advanced solid tumors is limited. Combination therapies that show promising results include combination with PD-1 antibodies, and combination with radiotherapy and chemotherapy. New combination therapies, such as CAR-T therapy modified with TGF-βRⅡ, are also emerging in clinical research. This article systematically reviews the therapeutic strategies targeting TGF-β to provide research basis and ideas for the development of drugs targeting the TGF-β pathway.