Among metal-based nanomaterials, Copper-based nanomaterials (Cu-BNMs) have become a research hotspot in the biomedical field due to their good biocompatibility and unique properties. However, there are fewer systematic summaries of copper-based nanomaterials, especially in the synthesis of Cu-BNMs. As for the applications, Cu-BNMs have been widely used in the fields of antimicrobial, imaging, and therapeutics, showing excellent promising biomedical properties. Herein, this review firstly introduces the classification of Cu-BNMs and the various methods for synthesizing Cu-BNMs through both top-down and bottom-up types. Then, the applications of Cu-BNMs within the three fields of antimicrobial, imaging, and tumor therapy are classified and summarized. Finally, the challenges faced in the synthesis and application of Cu-BNMs and the future development of c Cu-BNMs are discussed to provide basic information and illustrations for future research in the field of Cu-BNMs.