Copper and copper oxide nanoparticles (CuNPs) have unique physicochemical properties that make them highly promising for biomedical applications. This review discusses the application of CuNPs in biomedicine, including diagnosis, therapy, and theranostics. Recent synthesis methods, with an emphasis on green approaches, are described, and the latest techniques for nanoparticle characterization are critically analyzed. CuNPs, including Cu2O, CuO, and Cu, have significant potential as anti-cancer agents, drug delivery systems, and photodynamic therapy enhancers, among other applications. While challenges such as ensuring biocompatibility and stability must be addressed, the state-of-the-art research reviewed here provides strong evidence for the efficacy and versatility of CuNPs. These multifunctional properties have been extensively researched and documented, showcasing the immense potential of CuNPs in biomedicine. Overall, the evidence suggests that CuNPs are a promising avenue for future research and development in biomedicine. We strongly support further progress in the development of synthesis and application strategies to enhance the effectiveness and safety of CuNPs for clinical purposes.