Abstract: Breast cancer is the most common cancer affecting women's health and its incidence is increasing. With the development of immunohistochemistry and gene expression microarray technology, the study of breast cancer typing has gradually matured, which has also contributed to the development of targeted therapy for breast cancer. At present, the popular breast cancer cell surface markers include: G protein-coupled estrogen receptor 1 [GPER-1], human epidermal growth factor receptor 2 [HER-2], epidermal growth factor receptor [EGFR], c-mesenchymal-epithelial transition factor [C-Met], folate receptor-α [FRα], integrin, programmed death ligand 1 [PD-L1], trophoblast cell surface antigen 2 [Trop-2], etc. Targeted drugs for breast cancer cell surface markers mainly include antibody drugs and small molecule inhibitor drugs, which exert anti-tumor activity by targeting receptors or ligands. This review summarizes the surface markers of breast cancer cells and their targeted drugs, hoping to provide new ideas for breast cancer targeted therapy.