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[Display omitted] • This review highlights development of copper oxide nanoparticles (CONPs) by green synthesis method using method usingbiocomponents. • The potential of potential of CONPs were corroborated in in vitro breast cancer cell line studies and breast cancer models. • The molecular mechanisms behind the anti-breast cancer activity of CONPs were elucidated for the first time. • Future researcherss will get direction for the synthesis synthesis of CONPs-based nanomedicine for successful breast cancer therapy. Metal oxide nanoparticles are gaining close attention in recent years due to their varied physicochemical characteristics and applications in various fields, particularly nanomedicine and biomedical sciences. Among the various metal oxide nanoparticles, copper is a relatively low-cost metal than the others, such as gold, silver, zinc, etc. It can be biosynthesized easily without using harsh chemicals. Biosynthesis of copper oxide nanoparticles (CONPs) is mainly employed using phytoconstituents and biological agents including plant extract, bacteria, fungi, algae, etc., which can serve as capping and reducing agents. Additionally, due to their high redox cycling nature, CONPs exert superior catalytic activity and promising cytotoxicity on breast cancer cells via oxidative stress. Many studies confirm the anti-breast cancer potential of CONPs. In this review, an effort has been made to present a comprehensive overview and recent developments of CONPs, including their green synthesis approaches using various biocomponents, characterizations, and in vitro as well as in vivo applications in breast cancer treatment. The probable mechanisms of anticancer activity of CONPs have been elucidated for the first time. Thus, this review would help future researchers lay the groundwork for designing nanomedicines based on CONPs, either with or without anti-breast cancer drugs, to create effective treatments that will improve human health in the years to come. [ABSTRACT FROM AUTHOR]