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Brain metastases from breast cancer present a significant clinical challenge due to limited treatment options and poor prognosis. The development of novel therapeutic approaches is imperative to improve patient outcomes. Antibody-drug conjugates (ADCs) have emerged as a promising strategy for targeted treatment in various cancers. This review discusses the current indications and future perspectives of ADCs in managing brain metastases of breast cancer. We provide an overview of the underlying biology of brain metastasis, the rationale for ADC use, and a comprehensive analysis of ongoing clinical trials and preclinical studies. Key challenges, such as blood-brain barrier penetration and toxicity management, are addressed. Furthermore, we explore innovative ADC designs, including specific antibodies and combination therapies, which hold potential for enhanced efficacy. While early clinical results are promising, further research is needed to optimize ADC design, patient selection, and treatment regimens. Ultimately, ADCs offer a ray of hope for improving the treatment landscape of brain metastases from breast cancer, potentially extending patient survival and enhancing their quality of life.