Breast cancer is the second-most common cause of cancer-related death among women worldwide, with a gradual annual increase of 0.5 % in its occurrence rate in recent years. This complex ailment exhibits considerable diversity, with a mortality rate of 2.5 %. One promising area of research for its treatment is the development of MOFs, which are intricate three-dimensional (3D) structures constructed from metal ions or clusters joined with organic ligands through coordinate bonds. MOFs have emerged as versatile platform overcoming the limitations of conventional chemotherapeutics including poor drug solubility, non-specific targeting, and multidrug resistance. These applications are attributed to their adjustable porosity, chemical makeup, dimensions, straightforward surface customization capabilities, biocompatibility, nontoxicity etc. These properties position MOFs as excellent candidates for diverse regimes of cancer therapeutics including innovative approaches such as phototherapy, chemotherapy, immunotherapy, gene therapy, sonodynamic therapy, and various combination therapies. The article emphasizes the functionalization and applications of MOFs, with a primary focus on their therapeutic capabilities, synergistic approaches, and theranostic strategies that integrate diagnostic and therapeutic functions. Strategies to improve MOF biocompatibility and stability, such as surface modifications and biocompatible coatings are also discussed. Insights on various challenges and future prospects are provided to address current limitations and inspire further research, paving the way for clinical translation of MOF-based breast cancer therapies.