Abstract: As an antibody-drug conjugate (ADC) targeting trophoblast cell-surface antigen 2 (TROP-2), sacituzumab govitecan consists of a targeting antibody, a hydrolyzable carbonate linker (CL2A), and the potent topoisomerase I inhibitor 7-ethyl-10- hydroxycamptothecin (SN-38). In recent years, with the continuous development of clinical diagnosis and treatment technologies, considerable progress has been made in the treatment of metastatic triple-negative breast cancer (mTNBC) with sacituzumab govitecan. The phase III ASCENT trial has established its role in later-line treatment, and the ASCENT-03 trial has confirmed its first-line therapeutic value. In addition, multiple real-world studies worldwide have verified the efficacy and safety of sacituzumab govitecan in complex clinical settings, indicating that the ADC treatment paradigm has shifted from traditional laboratory-based research to clinical practice optimization. Based on the latest clinical research and real-world data, this review focuses on how sacituzumab govitecan overcomes the existing therapeutic limitations of mTNBC and expands its treatment landscape. It also systematically analyzes the core challenges currently facing this drug, including biomarker testing, resistance mechanisms, and pharmacoeconomics.