A Step-by-Step Guide for the Novel Radiometal Production for Medical Applications: Case Studies with 68Ga, 44Sc, 177Lu and 161Tb

Talip, Zeynep; Favaretto, Chiara; Geistlich, Susanne; Meulen, Nicholas P. van der

doi:10.3390/molecules25040966

Cited by 40 publications

(34 citation statements)

References 140 publications

(286 reference statements)

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“…Assessment of the quality control steps is crucial for the development of novel radionuclides toward nuclear medical applications ( 55 ). As part of the quality control processes, activity, radionuclidic purity, isotope ratio, radiochemical purity and chemical purity measurements were performed to evaluate the success of the mass and chemical separation methods ( Figure 4 ).…”

Section: Resultsmentioning

confidence: 99%

Production of Mass-Separated Erbium-169 Towards the First Preclinical in vitro Investigations

et al. 2021

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The β−-particle-emitting erbium-169 is a potential radionuclide toward therapy of metastasized cancer diseases. It can be produced in nuclear research reactors, irradiating isotopically-enriched 168Er2O3. This path, however, is not suitable for receptor-targeted radionuclide therapy, where high specific molar activities are required. In this study, an electromagnetic isotope separation technique was applied after neutron irradiation to boost the specific activity by separating 169Er from 168Er targets. The separation efficiency increased up to 0.5% using resonant laser ionization. A subsequent chemical purification process was developed as well as activity standardization of the radionuclidically pure 169Er. The quality of the 169Er product permitted radiolabeling and pre-clinical studies. A preliminary in vitro experiment was accomplished, using a 169Er-PSMA-617, to show the potential of 169Er to reduce tumor cell viability.

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Section: Resultsmentioning

confidence: 99%

Production of Mass-Separated Erbium-169 Towards the First Preclinical in vitro Investigations

et al. 2021

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“…We synthesized three kallidin derivatives and appended the 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) chelator at N-terminus, separated by a 6-aminohexanoic acid (Ahx) or 9-amino-4,7-dioxanonanoic acid (dPEG2) linker [77]. The radiotracers were radiolabeled with 68 Ga-gallium (t 1/2 : 68 min), an isotope suited to the fast pharmacokinetics of short peptides [85,86]. 68 Ga-P03083 ( 68 Ga-DOTA-Ahx-[Leu 9 ,des-Arg 10 ]kallidin) retains the native sequence, while 68 Ga-SH01078 ( 68 Ga-DOTA-Ahx-[Hyp 4 ,Cha 6 ,Leu 9 , desArg 10 ]kallidin) and 68 Ga-P03034 ( 68 Ga-DOTA-dPEG2-[Hyp 4 ,Cha 6 ,Leu 9 ,desArg 10 ]kallidin) contain unnatural amino acids to improve stability.…”

Section: B1r Imaging Agentsmentioning

confidence: 99%

A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors

Lau¹,

Rousseau²,

Kwon³

et al. 2020

Pharmaceuticals

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Kinins, bradykinin and kallidin are vasoactive peptides that signal through the bradykinin B1 and B2 receptors (B1R and B2R). B2R is constitutively expressed in healthy tissues and mediates responses such as vasodilation, fluid balance and retention, smooth muscle contraction, and algesia, while B1R is absent in normal tissues and is induced by tissue trauma or inflammation. B2R is activated by kinins, while B1R is activated by kinins that lack the C-terminal arginine residue. Perturbations of the kinin system have been implicated in inflammation, chronic pain, vasculopathy, neuropathy, obesity, diabetes, and cancer. In general, excess activation and signaling of the kinin system lead to a pro-inflammatory state. Depending on the disease context, agonism or antagonism of the bradykinin receptors have been considered as therapeutic options. In this review, we summarize molecular imaging agents targeting these G protein-coupled receptors, including optical and radioactive probes that have been used to interrogate B1R/B2R expression at the cellular and anatomical levels, respectively. Several of these preclinical agents, described herein, have the potential to guide therapeutic interventions for these receptors.

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“…[ 18 F]fluoro-deoxy-glucose ([ 18 F]FDG) is still predominant in PET imaging, but there is large interest in the development of further radionuclides to benefit from more favorable decay characteristics to match specific applications. In this regard, the availability, transport, dosimetry, and safety are critical aspects to be addressed [1][2][3][4][5].…”

Section: Introductionmentioning

confidence: 99%

Fifty Shades of Scandium: Comparative Study of PET Capabilities Using Sc-43 and Sc-44 with Respect to Conventional Clinical Radionuclides

et al. 2021

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Scandium-44 has been proposed as a valuable radionuclide for Positron Emission Tomography (PET). Recently, scandium-43 was introduced as a more favorable option, as it does not emit high-energy γ-radiation; however, its currently employed production method results in a mixture of scandium-43 and scandium-44. The interest in new radionuclides for diagnostic nuclear medicine critically depends on the option for image-based quantification. We aimed to evaluate and compare the quantitative capabilities of scandium-43/scandium-44 in a commercial PET/CT device with respect to more conventional clinical radionuclides (fluorine-18 and gallium-68). With this purpose, we characterized and compared quantitative PET data from a mixture of scandium-43/scandium-44 (~68% scandium-43), scandium-44, fluorine-18 and gallium-68, respectively. A NEMA image-quality phantom was filled with the different radionuclides using clinical-relevant lesion-to-background activity concentration ratios; images were acquired in a Siemens Biograph Vision PET/CT. Quantitative accuracy with scandium-43/scandium-44 in the phantom’s background was within 9%, which is in agreement with fluorine-18-based PET standards. Coefficient of variance (COV) was 6.32% and signal recovery in the lesions provided RCmax (recovery coefficient) values of 0.66, 0.90, 1.03, 1.04, 1.12 and 1.11 for lesions of 10-, 13-, 17-, 22-, 28- and 37-mm diameter, respectively. These results are in agreement with EARL reference values for fluorine-18 PET. The results in this work showed that accurate quantitative scandium-43/44 PET/CT is achievable in commercial devices. This may promote the future introduction of scandium-43/44-labelled radiopharmaceuticals into clinical use.

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A Step-by-Step Guide for the Novel Radiometal Production for Medical Applications: Case Studies with 68Ga, 44Sc, 177Lu and 161Tb

Cited by 40 publications

References 140 publications

Production of Mass-Separated Erbium-169 Towards the First Preclinical in vitro Investigations

Production of Mass-Separated Erbium-169 Towards the First Preclinical in vitro Investigations

A Systematic Review of Molecular Imaging Agents Targeting Bradykinin B1 and B2 Receptors

Fifty Shades of Scandium: Comparative Study of PET Capabilities Using Sc-43 and Sc-44 with Respect to Conventional Clinical Radionuclides

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