The emerging role of copper-64 radiopharmaceuticals as cancer theranostics

Copper radionuclides are rapidly emerging as potential diagnostic and therapeutic tools in oncology, particularly ⁶⁴Cu-radiopharmaceuticals for targeting neuroendocrine, prostate, and hypoxic tumors. Unexpectedly, experimental results are also revealing the impressive biological behavior of simple [⁶⁴Cu²⁺] ions. For example, it has been demonstrated that administration of ionic [⁶⁴Cu²⁺] in physiological solution allows the selective targeting of a variety of malignancies. These remarkable biological properties appear to be crucially linked to the natural role of copper ions in cell proliferation. Here, we review the current status of ⁶⁴Cu-radiopharmaceuticals in molecular imaging and cancer therapy.