Abstract: Significant research progress has been made in the development of antibody-drug conjugates (ADCs) for the treatment of advanced breast cancer (ABC), ushering new hope for patients with this refractory disease. Through the conjugation of specific antibodies with highly potent cytotoxic drugs, tumor cells can be precisely targeted and killed while minimizing damage to normal tissues. ADCs such as trastuzumab-emtansine (T-DM1) and trastuzumab deruxtecan (T-DXd), have shown excellent efficacy in the treatment of HER2-positive ABC, significantly prolonging patient survival. Furthermore, ADCs targeting triple-negative breast cancer (TNBC), such as sacituzumab govitecan (SG), have also achieved positive results in clinical trials. With the continuous research, development, and optimization of ADCs, as well as the exploration of combination treatment strategies, ADCs are expected to play an increasingly important role in the treatment of ABC in the future. This article provides an overview of the research progress of ADCs in the treatment of ABC, exploring their efficacy and safety. We aim to offer more treatment options and renewed hope for patients with ABC.