Advanced triple-negative breast cancer (TNBC) has poorer outcomes due to its aggressive behaviour and limited treatment options. While therapies like checkpoint inhibitors and PARP inhibitors (PARPi) offer some benefit, chemotherapy remains ineffective beyond the first line of treatment. Antibody-drug conjugates (ADCs) like sacituzumab govitecan-hziy (SG) represent a significant advancement. SG combines SN-38, an irinotecan derivative, with a TROP-2-targeting antibody via a pH-sensitive linking moiety, achieving an good drug:antibody ratio. Infused on Days 1 and 8 over 21 days, SG utilizes a moderately stable linker to ensure effective tumor targeting while minimizing side effects like diarrhea. By delivering SN-38 into the tumor niche, it induces double-stranded DNA damage, promoting cancer apoptosis. In a phase I-II study involving 108 mTNBC patients, SG achieved an overall response rate (ORR) of 33.3% and a median response period of 7.7 months. Common side effects included neutropenia, nausea, and fatigue. This review highlights clinical potential, pharmacokinetics, safety profile, resistance mechanisms of SG along with key ongoing clinical trials, emphasizing its role in managing refractory mTNBC, especially in third-line therapy.