Abstract: Trophoblast cell surface antigen 2(Trop-2) exhibits underexpression in normal tissue, yet overexpression in many tumor tissues. The overexpression of Trop-2 plays a significant role in the initiation, progression, and metastasis of tumor. With the significant breakthrough of sacituzumab govitecan, anti-Trop-2 antibody-drug conjugate(ADC), in treating advanced triple-negative breast cancer,along with its approved indications and the recent positive findings from various phase Ⅲ clinical trials regarding ADC targeting Trop-2,the development of ADC targeting Trop-2 has become a promising new strategy for tumor treatment. This review provides a comprehensive overview of the structure and function of Trop-2, the recent advances in clinical research regarding ADC targeting Trop-2 for breast cancer and the existing challenges, aiming to offer some valuable insight for the selection of therapeutic strategies for breast cancer patients.