Elsevier

Drug Discovery Today

Volume 23, Issue 8, August 2018, Pages 1489-1501
Drug Discovery Today

Review
Keynote
The emerging role of copper-64 radiopharmaceuticals as cancer theranostics

Highlights

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Copper radionuclides for in vivo imaging of biological functions of copper ions.

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Copper-64 has suitable nuclear properties for cancer theranostics.

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Radioactive copper ions as early biomarkers of cancer progression.

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Copper radionuclides can be used for developing novel radiopharmaceuticals.

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.

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Alessandra Boschi is currently the head of the Radiation Safety and Control Section at the University of Ferrara and a assistant professor of radiochemistry. Her research interests focus mainly on the development of novel chelating systems for radiometals and the application of radionuclide imaging in preclinical studies.

Petra Martini is currently a postdoc at the Legnaro National Laboratories of the INFN. She is also a researcher fellow at the University of Ferrara. She has also worked at TRIUMF Canada’s Particle Accelerator Centre. Her main research interests focus on the production of novel radionuclides for medicine and the development of automated methods for target processing, separation, and purification of radionuclides from cyclotron-irradiated targets.

Emilija Janevik-Ivanovska is currently a professor in pharmaceutical chemistry and technology at the University of Stip. She is also the director of the University Institute for Positron Emission Tomography in Skopje. She is also expert consultant to the International Atomic Energy Agency and the European Directorate for the Quality of Medicines. Her broad research interests range from radiolabeling of peptides and antibodies to the development of molecular imaging agents labeled with positron-emitting radionuclides and radionuclide therapy. She is also involved in various expert committees for the analysis of regulatory aspects related to radiopharmaceuticals.

Adriano Duatti is currently a professor of general and inorganic chemistry at the University of Ferrara and a research associate of the Italian National Institute of Nuclear Physics (INFN). He is Head of the LARAMED project at the INFN Legnaro National Laboratories, which aims develop the production of innovative and nonstandard radionuclides for medical applications using a high-energy (70 MeV) and high-current (800 microA) cyclotron. He is also a radiopharmaceutical consultant to the Italian Ministry of Health. He has also worked at the International Atomic Energy in Vienna, Austria in the Radioisotope Products and Radiation Technology Section. His main research interests focus on the chemistry of metallic radiopharmaceuticals, molecular imaging, and targeted radionuclide therapy.

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