Copper-64: a real theranostic agent

Ongoing studies of physiological and pathological processes have led to a corresponding need for new radiopharmaceuticals, especially when studies are limited by the absence of a particular radiolabeled target. Thus, the development of new radioactive tracers is highly relevant and can represent a significant contribution to efforts to elucidate important phenomena in biology. Currently, theranostics represents a new frontier in the fields of medicine and nuclear medicine, with the same compound being used for both diagnosis and treatment. In the human body, copper (Cu) is the third most abundant metal and it plays a crucial role in many biological functions. Correspondingly, in various acquired and inherited pathological conditions, such as cancer and Alzheimer’s disease, alterations in Cu levels have been found. Moreover, a wide spectrum of neurodegenerative disorders are associated with higher or lower levels of Cu, as well as inappropriately bound or distributed levels of Cu in the brain. In human cells, the membrane protein, hCtr1, binds Cu in its Cu(I) oxidation state in an energy-dependent manner. Copper-64 ((64)Cu) is a cyclotron-produced radionuclide that has exhibited physical properties that are complementary for diagnosis and/or therapeutic purposes. To date, very few reports have described the clinical development of (64)Cu as a radiotracer for cancer imaging. In this review, we highlight recent insights in our understanding and use of (64)CuCl(2) as a theranostic agent for various types of tumors. To the best of our knowledge, no adverse effects or clinically observable pharmacological effects have been described for (64)CuCl(2) in the literature. Thus, (64)Cu represents a revolutionary radiopharmaceutical for positron emission tomography imaging and opens a new era in the theranostic field.