Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent

Copper is required for cancer cell proliferation and tumor angiogenesis. Copper-64 radionuclide (<sup>64</sup>Cu), a form of copper chloride (<sup>64</sup>CuCl<sub>2</sub>), is rapidly emerging as a diagnostic PET/CT tracer in oncology. It may also represent an in...

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Main Authors: Gabriela Capriotti, Arnoldo Piccardo, Elena Giovannelli, Alberto Signore
Format: Article
Language:English
Published: MDPI AG 2022-12-01
Series:Journal of Clinical Medicine
Subjects:
Online Access:https://www.mdpi.com/2077-0383/12/1/223
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author Gabriela Capriotti
Arnoldo Piccardo
Elena Giovannelli
Alberto Signore
author_facet Gabriela Capriotti
Arnoldo Piccardo
Elena Giovannelli
Alberto Signore
author_sort Gabriela Capriotti
collection DOAJ
description Copper is required for cancer cell proliferation and tumor angiogenesis. Copper-64 radionuclide (<sup>64</sup>Cu), a form of copper chloride (<sup>64</sup>CuCl<sub>2</sub>), is rapidly emerging as a diagnostic PET/CT tracer in oncology. It may also represent an interesting alternative to gallium-68 (<sup>68</sup>Ga) as a radionuclide precursor for labelling radiopharmaceuticals used to investigate neuroendocrine tumors and prostate cancer. This emerging interest is also related to the nuclear properties of <sup>64</sup>CuCl<sub>2</sub> that make it an ideal theragnostic nuclide. Indeed, <sup>64</sup>CuCl<sub>2</sub> emits β<sup>+</sup> and β<sup>-</sup> particles together with high-linear-energy-transfer Auger electrons, suggesting the therapeutic potential of <sup>64</sup>CuCl<sub>2</sub> for the radionuclide cancer therapy of copper-avid tumors. Recently, <sup>64</sup>CuCl<sub>2</sub> was successfully used to image prostate cancer, bladder cancer, glioblastoma multiforme (GBM), and non-small cell lung carcinoma in humans. Copper cancer uptake was related to the expression of human copper transport 1 (hCTR1) on the cancer cell surface. Biodistribution, toxicology and radiation safety studies showed its radiation and toxicology safety. Based on the findings from the preclinical research studies, <sup>64</sup>CuCl<sub>2</sub> PET/CT also holds potential for the diagnostic imaging of human hepatocellular carcinoma (HCC), malignant melanoma, and the detection of the intracranial metastasis of copper-avid tumors based on the low physiological background of radioactive copper uptake in the brain.
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spelling doaj.art-0239257a1bab4a6da0531715b5549b492023-11-16T15:43:08ZengMDPI AGJournal of Clinical Medicine2077-03832022-12-0112122310.3390/jcm12010223Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic AgentGabriela Capriotti0Arnoldo Piccardo1Elena Giovannelli2Alberto Signore3Department of Medical-Surgical Sciences and of Translational Medicine, Sapienza University of Rome, Nuclear Medicine Unit Sant’Andrea University Hospital, 00189 Rome, ItalyS.C. Medicina Nucleare Ente Ospedaliero “Ospedali Galliera”, 16128 Genova, ItalyDepartment of Medical-Surgical Sciences and of Translational Medicine, Sapienza University of Rome, Nuclear Medicine Unit Sant’Andrea University Hospital, 00189 Rome, ItalyDepartment of Medical-Surgical Sciences and of Translational Medicine, Sapienza University of Rome, Nuclear Medicine Unit Sant’Andrea University Hospital, 00189 Rome, ItalyCopper is required for cancer cell proliferation and tumor angiogenesis. Copper-64 radionuclide (<sup>64</sup>Cu), a form of copper chloride (<sup>64</sup>CuCl<sub>2</sub>), is rapidly emerging as a diagnostic PET/CT tracer in oncology. It may also represent an interesting alternative to gallium-68 (<sup>68</sup>Ga) as a radionuclide precursor for labelling radiopharmaceuticals used to investigate neuroendocrine tumors and prostate cancer. This emerging interest is also related to the nuclear properties of <sup>64</sup>CuCl<sub>2</sub> that make it an ideal theragnostic nuclide. Indeed, <sup>64</sup>CuCl<sub>2</sub> emits β<sup>+</sup> and β<sup>-</sup> particles together with high-linear-energy-transfer Auger electrons, suggesting the therapeutic potential of <sup>64</sup>CuCl<sub>2</sub> for the radionuclide cancer therapy of copper-avid tumors. Recently, <sup>64</sup>CuCl<sub>2</sub> was successfully used to image prostate cancer, bladder cancer, glioblastoma multiforme (GBM), and non-small cell lung carcinoma in humans. Copper cancer uptake was related to the expression of human copper transport 1 (hCTR1) on the cancer cell surface. Biodistribution, toxicology and radiation safety studies showed its radiation and toxicology safety. Based on the findings from the preclinical research studies, <sup>64</sup>CuCl<sub>2</sub> PET/CT also holds potential for the diagnostic imaging of human hepatocellular carcinoma (HCC), malignant melanoma, and the detection of the intracranial metastasis of copper-avid tumors based on the low physiological background of radioactive copper uptake in the brain.https://www.mdpi.com/2077-0383/12/1/223copper-64<sup>64</sup>CuCl<sub>2</sub>theragnosticpositron emission tomography
spellingShingle Gabriela Capriotti
Arnoldo Piccardo
Elena Giovannelli
Alberto Signore
Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent
Journal of Clinical Medicine
copper-64
<sup>64</sup>CuCl<sub>2</sub>
theragnostic
positron emission tomography
title Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent
title_full Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent
title_fullStr Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent
title_full_unstemmed Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent
title_short Targeting Copper in Cancer Imaging and Therapy: A New Theragnostic Agent
title_sort targeting copper in cancer imaging and therapy a new theragnostic agent
topic copper-64
<sup>64</sup>CuCl<sub>2</sub>
theragnostic
positron emission tomography
url https://www.mdpi.com/2077-0383/12/1/223
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