Preclinical evaluation of melanocortin-1 receptor (MC1-R) specific 68Ga- and 44Sc-labeled DOTA-NAPamide in melanoma imaging

Nagy, Gábor; Dénes, Noémi; Kis, Anna; Szabó, Judit P.; Berényi, Ervin; Garai, Ildikó; Bai, Péter; Hajdu, István; Szikra, Dezső; Trencsényi, György

doi:10.1016/j.ejps.2017.06.026

Cited by 28 publications

(40 citation statements)

References 29 publications

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“…However, 52g Mn emits multiple high-energy g-rays, making work less favorable with 52g Mn than with some other radioisotopes (29). 52g Mn can be produced via the 52 Cr(p,x) 52g Mn reaction, but radioisotope contaminants, including the long-lived 54 Mn, can be produced via the 54 Cr(p,n) reaction when natural chromium targets are used (27)(28)(29). Several groups have studied cross sections of these reactions to attain the highest yields with the fewest impurities (30,31).…”

Section: Production Of 52 Mnmentioning

confidence: 99%

“…44g Sc was used to radiolabel DOTA-NAPamide for targeting of the melanocortin-1 receptor, with higher uptake in melanocortin-1 receptor-positive B16-F10 xenografts than in melanocortin-1 receptor-negative A375 xenografts (27). In another study, 44g Sc-DOTANOC was synthesized with high radiochemical yields and used for dynamic PET imaging, showing continuous uptake and high-quality images in AR42J tumor xenografts, encouraging the transition into clinical applications (24).…”

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confidence: 99%

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Production and Use of the First-Row Transition Metal PET Radionuclides^43,44Sc,⁵²Mn, and⁴⁵Ti

Chaple

Lapi

2018

J Nucl Med

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With the increasing focus on a more personalized approach to medicine using imaging techniques to select patients for targeted treatment or theranostic strategies, interest in the development of new radionuclides is expanding. Through the development of production and radiochemistry techniques, several new radiometals are being added to the toolbox of the nuclear imaging community. 43,44g,m Sc, 52g Mn, and 45 Ti are all emerging transition metal radionuclides and will be discussed in this short review. Each of these nuclides has unique imaging characteristics and shows promise for the development of new molecular imaging agents.

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Section: Production Of 52 Mnmentioning

confidence: 99%

mentioning

confidence: 99%

Production and Use of the First-Row Transition Metal PET Radionuclides^43,44Sc,⁵²Mn, and⁴⁵Ti

Chaple

Lapi

2018

J Nucl Med

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“…The peptide receptor melanocortin type 1 receptor (MC1R) has also been studied as a potential target for diagnostic imaging and therapy of melanoma and metastases, using mainly radiolabeled peptides. A set of relevant articles, including reviews, have appeared in the last years [93,94,95,96,97,98,99,100,101,102]. However, as far as the authors are aware, no relevant human clinical applications have emerged.…”

Section: Introductionmentioning

confidence: 99%

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

et al. 2018

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Precision medicine relies on individually tailored therapeutic intervention taking into account individual variability. It is strongly dependent on the availability of target-specific drugs and/or imaging agents that recognize molecular targets and patient-specific disease mechanisms. The most sensitive molecular imaging modalities, Single Photon Emission Computed Tomography (SPECT) and Positron Emission Tomography (PET), rely on the interaction between an imaging radioprobe and a target. Moreover, the use of target-specific molecular tools for both diagnostics and therapy, theranostic agents, represent an established methodology in nuclear medicine that is assuming an increasingly important role in precision medicine. The design of innovative imaging and/or theranostic agents is key for further accomplishments in the field. G-protein-coupled receptors (GPCRs), apart from being highly relevant drug targets, have also been largely exploited as molecular targets for non-invasive imaging and/or systemic radiotherapy of various diseases. Herein, we will discuss recent efforts towards the development of innovative imaging and/or theranostic agents targeting selected emergent GPCRs, namely the Frizzled receptor (FZD), Ghrelin receptor (GHSR-1a), G protein-coupled estrogen receptor (GPER), and Sphingosine-1-phosphate receptor (S1PR). The pharmacological and clinical relevance will be highlighted, giving particular attention to the studies on the synthesis and characterization of targeted molecular imaging agents, biological evaluation, and potential clinical applications in oncology and non-oncology diseases. Whenever relevant, supporting computational studies will be also discussed.

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“…To our knowledge, our study is the first proof of principle study that analyzes the labeling of HMPA polymers with scandium-44 and its in vivo distribution. Besides high in vitro stabilities, the good in vivo stability enables imaging of biological processes for up to 24 h. Further studies will focus on the comparison of different molecular weight polymers for enhanced EPR-mediated enrichment into tumors as well as receptor-mediated targeting to tumors as it was shown for [ 44 Sc]Sc-DOTA-NAPamide for melanoma imaging [ 51 ].…”

Section: Discussionmentioning

confidence: 99%

Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging

Eppard¹,

Fuente

Mohr

et al. 2018

EJNMMI Res

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BackgroundIn this work, the in vitro and in vivo stabilities and the pharmacology of HPMA-made homopolymers were studied by means of radiometal-labeled derivatives. Aiming to identify the fewer amount and the optimal DOTA-linker structure that provides quantitative labeling yields, diverse DOTA-linker systems were conjugated in different amounts to HPMA homopolymers to coordinate trivalent radiometals Me(III)* = gallium-68, scandium-44, and lutetium-177.ResultsShort linkers and as low as 1.6% DOTA were enough to obtain labeling yields > 90%. Alkoxy linkers generally exhibited lower labeling yields than alkane analogues despite of similar chain length and DOTA incorporation rate. High stability of the radiolabel in all examined solutions was observed for all conjugates. Labeling with scandium-44 allowed for in vivo PET imaging and ex vivo measurements of organ distribution for up to 24 h.ConclusionsThis study confirms the principle applicability of DOTA-HPMA conjugates for labeling with different trivalent metallic radionuclides allowing for diagnosis and therapy.Electronic supplementary materialThe online version of this article (10.1186/s13550-018-0372-x) contains supplementary material, which is available to authorized users.

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Preclinical evaluation of melanocortin-1 receptor (MC1-R) specific 68Ga- and 44Sc-labeled DOTA-NAPamide in melanoma imaging

Cited by 28 publications

References 29 publications

Production and Use of the First-Row Transition Metal PET Radionuclides^43,44Sc,⁵²Mn, and⁴⁵Ti

Production and Use of the First-Row Transition Metal PET Radionuclides^43,44Sc,⁵²Mn, and⁴⁵Ti

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging

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Preclinical evaluation of melanocortin-1 receptor (MC1-R) specific 68Ga- and 44Sc-labeled DOTA-NAPamide in melanoma imaging

Cited by 28 publications

References 29 publications

Production and Use of the First-Row Transition Metal PET Radionuclides43,44Sc,52Mn, and45Ti

Production and Use of the First-Row Transition Metal PET Radionuclides43,44Sc,52Mn, and45Ti

Less Exploited GPCRs in Precision Medicine: Targets for Molecular Imaging and Theranostics

Labeling of DOTA-conjugated HPMA-based polymers with trivalent metallic radionuclides for molecular imaging

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Product

Resources

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Production and Use of the First-Row Transition Metal PET Radionuclides^43,44Sc,⁵²Mn, and⁴⁵Ti

Production and Use of the First-Row Transition Metal PET Radionuclides^43,44Sc,⁵²Mn, and⁴⁵Ti