Copper-64 based radiopharmaceuticals for brain tumors and hypoxia imaging

Pasquali, M.; Martini, Petra; Shahi, Arman; Jalilian, Amir Reza; Osso, João Alberto; Boschi, Alessandra

doi:10.23736/s1824-4785.20.03285-9

Cited by 14 publications

(14 citation statements)

References 74 publications

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“…This class of chelators, bis (thiosemicarbazones), act as tetradentate ligands and coordinate Cu 2+ forming stable and neutral complexes, with a square planar geometry, which show a high permeability of the cell membrane. The preparation of these complexes with radioactive copper isotopes can be carried out under mild conditions in high yield [ 74 , 87 , 88 , 89 ].…”

Section: The Use Of 67 Cu For Medical Applicationsmentioning

confidence: 99%

67Cu Production Capabilities: A Mini Review

et al. 2022

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Is the 67Cu production worldwide feasible for expanding preclinical and clinical studies? How can we face the ingrowing demands of this emerging and promising theranostic radionuclide for personalized therapies? This review looks at the different production routes, including the accelerator- and reactor-based ones, providing a comprehensive overview of the actual 67Cu supply, with brief insight into its use in non-clinical and clinical studies. In addition to the most often explored nuclear reactions, this work focuses on the 67Cu separation and purification techniques, as well as the target material recovery procedures that are mandatory for the economic sustainability of the production cycle. The quality aspects, such as radiochemical, chemical, and radionuclidic purity, with particular attention to the coproduction of the counterpart 64Cu, are also taken into account, with detailed comparisons among the different production routes. Future possibilities related to new infrastructures are included in this work, as well as new developments on the radiopharmaceuticals aspects.

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Section: The Use Of 67 Cu For Medical Applicationsmentioning

confidence: 99%

67Cu Production Capabilities: A Mini Review

et al. 2022

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“…Furthermore, Cu(I) is less stable in the coordination environment established by the ATSM ligand, causing the release of the metal ion and re-chelation by chaperone proteins. For the past twenty years, [ 60/61/62/64 Cu]Cu-ATSM tracers have been used to identify hypoxic tumors as well as monitor patients’ responses to radioimmunotherapy in multiple cancers [ 93 ]. However, the accumulation of [ 60/61/62/64 Cu]Cu-ATSM is not always well correlated with hypoxic conditions.…”

Section: Current Pet Radiopharmaceuticals Beyond [ 18 ...mentioning

confidence: 99%

PET Oncological Radiopharmaceuticals: Current Status and Perspectives

et al. 2022

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Molecular imaging is the visual representation of biological processes that take place at the cellular or molecular level in living organisms. To date, molecular imaging plays an important role in the transition from conventional medical practice to precision medicine. Among all imaging modalities, positron emission tomography (PET) has great advantages in sensitivity and the ability to obtain absolute imaging quantification after corrections for photon attenuation and scattering. Due to the ability to label a host of unique molecules of biological interest, including endogenous, naturally occurring substrates and drug-like compounds, the role of PET has been well established in the field of molecular imaging. In this article, we provide an overview of the recent advances in the development of PET radiopharmaceuticals and their clinical applications in oncology.

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“…64 Cu has been considered for its theranostic properties not only because of its intrinsic β – (39.0%) emission along with its β + (17.9%) but also because 64 Cu could be used as a pair with the therapeutic β – emitting radionuclide 67 Cu, although applications with the latter are still limited due to its rare and expensive production . To reflect on exciting developments regarding 64 Cu radiopharmaceuticals, comprehensive reviews have recently been published. ,,,,− …”

Section: Radiometals Evaluated In Immuno-petmentioning

confidence: 99%

State of the Art in Radiolabeling of Antibodies with Common and Uncommon Radiometals for Preclinical and Clinical Immuno-PET

2021

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Inert and stable radiolabeling of monoclonal antibodies (mAb), antibody fragments, or antibody mimetics with radiometals is a prerequisite for immuno-PET. While radiolabeling is preferably fast, mild, efficient, and reproducible, especially when applied for human use in a current Good Manufacturing Practice compliant way, it is crucial that the obtained radioimmunoconjugate is stable and shows preserved immunoreactivity and in vivo behavior. Radiometals and chelators have extensively been evaluated to come to the most ideal radiometal–chelator pair for each type of antibody derivative. Although PET imaging of antibodies is a relatively recent tool, applications with 89Zr, 64Cu, and 68Ga have greatly increased in recent years, especially in the clinical setting, while other less common radionuclides such as 52Mn, 86Y, 66Ga, and 44Sc, but also 18F as in [18F]AlF are emerging promising candidates for the radiolabeling of antibodies. This review presents a state of the art overview of the practical aspects of radiolabeling of antibodies, ranging from fast kinetic affibodies and nanobodies to slow kinetic intact mAbs. Herein, we focus on the most common approach which consists of first modification of the antibody with a chelator, and after eventual storage of the premodified molecule, radiolabeling as a second step. Other approaches are possible but have been excluded from this review. The review includes recent and representative examples from the literature highlighting which radiometal–chelator–antibody combinations are the most successful for in vivo application.

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Copper-64 based radiopharmaceuticals for brain tumors and hypoxia imaging

Cited by 14 publications

References 74 publications

67Cu Production Capabilities: A Mini Review

67Cu Production Capabilities: A Mini Review

PET Oncological Radiopharmaceuticals: Current Status and Perspectives

State of the Art in Radiolabeling of Antibodies with Common and Uncommon Radiometals for Preclinical and Clinical Immuno-PET

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