Radiometals for imaging and theranostics, current production, and future perspectives

Mikołajczak, Renata; Meulen, Nicholas P. van der; Lapi, Suzanne E.

doi:10.1002/jlcr.3770

Cited by 55 publications

(32 citation statements)

References 158 publications

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“…Radiometals are widely used for radiopharmaceuticals, in part due to available chelation chemistry and labelling with biomolecules (Krasikova et al 2016 ; Price and Orvig 2014 ; Aluicio-Sarduy et al 2018 ; Vivier et al 2018 ; Tsai and Wu 2018 ; Liu 2008 ). Among the radiometals, following Ga, Cu is one of the most extensively investigated for PET radiopharmaceutical purposes (Mikolajczak et al 2019 ; Brandt et al 2018 ; Wadas et al 2006 ; McCarthy et al 1999 ). One reason for this is the well-understood coordination chemistry and biodistribution of Cu (Wadas et al 2006 ; Wadas et al 2010 ; Wallhaus et al 1998 ; Jalilian et al 2009 ; Woo et al 2019 ), which has resulted in a multitude of chelators and biomolecule options being available for Cu isotopes.…”

Section: Introductionmentioning

confidence: 99%

Automated, cassette-based isolation and formulation of high-purity [61Cu]CuCl2 from solid Ni targets

Svedjehed¹,

Kutyreff

Engle

et al. 2020

EJNMMI radiopharm. chem.

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Background A need for improved, cassette-based automation of 61Cu separation from irradiated Ni targets was identified given the growing interest in theranostics, and generally lengthy separation chemistries for 64Cu/64Ni, upon which 61Cu chemistry is often based. Methods A method for separating 61Cu from irradiated natNi targets was therefore developed, with provision for target recycling. Following deuteron irradiation, electroplated natNi targets were remotely transferred from the cyclotron and dissolved in acid. The dissolved target solution was then transferred to an automated FASTlab chemistry module, where sequential TBP and TK201 (Triskem) resins isolated the [61Cu]CuCl2, removed Ni, Co, and Fe, and concentrated the product into a formulation suitable for anticipated radiolabelling reactions. Results 61Cu saturation yields of 190 ± 33 MBq/μA from energetically thick natNi targets were measured. The average, decay-corrected, activity-based dissolution efficiency was 97.5 ± 1.4% with an average radiochemical yield of 90.4 ± 3.2% (N = 5). The isolated activity was collected approximately 65 min post end of bombardment in ~ 2 mL of 0.06 M HCl (HCl concentration was verified by titration). Quality control of the isolated [61Cu]CuCl2 (N = 5) measured 58Co content of (8.3 ± 0.6) × 10− 5% vs. 61Cu by activity, Ni separation factors ≥ (2.2 ± 1.8) × 106, EoB molar activities 85 ± 23 GBq/μmol and NOTA-based EoB apparent molar activities of 31 ± 8 MBq/nmol and 201 MBq/nmol for the 30 min and 3.3 h (N = 1) irradiations, respectively. Conclusion High purity 61Cu was produced with the developed automated method using a single-use, cassette-based approach. It was also applicable for 64Cu, as demonstrated with a single proof-of-concept 64Ni target production run.

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Section: Introductionmentioning

confidence: 99%

Automated, cassette-based isolation and formulation of high-purity [61Cu]CuCl2 from solid Ni targets

Svedjehed¹,

Kutyreff

Engle

et al. 2020

EJNMMI radiopharm. chem.

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“…Positron emission tomography (PET) and single-photon emission computed tomography (SPECT) are two of the most common imaging modalities for diagnostic purposes, while targeted-radionuclide therapeutic efforts focus on inducing irreversible DNA damage via the emission of either αparticles, β − particles, or low-energy (Auger) electrons 2 . The full potential of nuclear medicine may be realized with theranostics, wherein a molecular targeting vector is labeled with both a diagnostic and a therapeutic radionuclide that are utilized for concomitant imaging and treatment [3][4][5][6] . Ideally, the employed radionuclides are a matched pair, where both are radioisotopes of the same chemical element; however, very few elements have isotope pairs with suitable nuclear decay properties.…”

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confidence: 99%

Developing scandium and yttrium coordination chemistry to advance theranostic radiopharmaceuticals

et al. 2020

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The octadentate siderophore analog 3,4,3-LI(1,2-HOPO), denoted 343-HOPO hereafter, is known to have high affinity for both trivalent and tetravalent lanthanide and actinide cations. Here we extend its coordination chemistry to the rare-earth cations Sc 3+ and Y 3+ and characterize fundamental metal-chelator binding interactions in solution via UV-Vis spectrophotometry, nuclear magnetic resonance spectroscopy, and spectrofluorimetric metalcompetition titrations, as well as in the solid-state via single crystal X-ray diffraction. Sc 3+ and Y 3+ binding with 343-HOPO is found to be robust, with both high thermodynamic stability and fast room temperature radiolabeling, indicating that 343-HOPO is likely a promising chelator for in vivo applications with both metals. As a proof of concept, we prepared a 86 Y-343-HOPO complex for in vivo PET imaging, and the results presented herein highlight the potential of 343-HOPO chelated trivalent metal cations for therapeutic and theranostic applications.

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“…Radiometals’ production is currently still limited, even for the most advanced ones [ 142 , 143 , 144 ]. Fluorine-18, on the contrary, can be mass-produced and distributed daily, thanks to a worldwide network of cyclotrons.…”

Section: Targeting Of Somatostatin Receptors With Radiopharmaceutimentioning

confidence: 99%

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five subtypes described. The interaction between SST and its receptors leads to the internalization of the ligand–receptor complex and triggers different cellular signaling pathways. Interestingly, the expression of SSTRs is significantly enhanced in many solid tumors, especially gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Thus, somatostatin analogs (SSAs) have been developed to improve the stability of the endogenous ligand and so extend its half-life. Radiolabeled analogs have been developed with several radioelements such as indium-111, technetium-99 m, and recently gallium-68, fluorine-18, and copper-64, to visualize the distribution of receptor overexpression in tumors. Internal metabolic radiotherapy is also used as a therapeutic strategy (e.g., using yttrium-90, lutetium-177, and actinium-225). With some radiopharmaceuticals now used in clinical practice, somatostatin analogs developed for imaging and therapy are an example of the concept of personalized medicine with a theranostic approach. Here, we review the development of these analogs, from the well-established and authorized ones to the most recently developed radiotracers, which have better pharmacokinetic properties and demonstrate increased efficacy and safety, as well as the search for new clinical indications.

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Radiometals for imaging and theranostics, current production, and future perspectives

Cited by 55 publications

References 158 publications

Automated, cassette-based isolation and formulation of high-purity [61Cu]CuCl2 from solid Ni targets

Automated, cassette-based isolation and formulation of high-purity [61Cu]CuCl2 from solid Ni targets

Developing scandium and yttrium coordination chemistry to advance theranostic radiopharmaceuticals

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

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