Transforming growth factor-β (TGF-β) belongs to a group of TGF-β superfamily that regulates cell growth and differentiation, mainly TGF-β1, TGF-β2 and TGF-β3 isoforms. The studies show that each TGFβ isoform plays an important role in tumor development, such as: (1) inhibiting the proliferation of immunoreactive cells; (2) inhibiting lymphocyte differentiation; (3) inhibition of cytokine production: e.g., inhibition of IFN-γ and TNF-α production in PBMC; (4) in other regulatory roles: (1) promoting the growth of fibroblasts and osteoblasts; (2) inhibiting the growth of epithelial cells, osteoblasts, endothelial cells and the formation of adipose, cardiac and skeletal muscle; (3) promoting the expression of extracellular matrix (ECM) such as collagen, fibronectin and inhibit the degradation of ECM, which plays an important role in the process of cell morphogenesis, proliferation and differentiation, and facilitates embryonic development and cell repair; ④ chemotactic agent of monocytes and fibroblasts; ⑤ inhibit the adhesion of lymphocytes to endothelial cells; ⑥ promote the release of histamine from basophils. Higher levels of TGF-β are associated with immune escape, treatment resistance (chemotherapy, radiotherapy, checkpoint inhibitors) and poor prognosis in advanced malignancies. There are several small molecule inhibitors and monoclonal antibodies targeting the TGF-β pathway in clinical development worldwide, such as Novartis TGF-β monoclonal antibody NIS793 and PD-L1×TGF-β bifunctional antibody fusion proteins such as M7824 and SHR1701 have shown increased efficacy of anti-TGF-β in some clinical studies, but there is no marketed TGF-β antibody drug class yet.