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2. Highlight selection of radiochemistry and radiopharmacy developments by editorial board.

Author

DaSilva, Jean, Decristoforo, Clemens, Mach, Robert, Bormans, Guy, Carlucci, Giuseppe, Al-Qahtani, Mohammed, Duatti, Adriano, Gee, Antony, Szymanski, Wiktor, Rubow, Sietske, Hendrikx, Jeroen, Yang, Xing, Jia, Hongmei, Zhang, Junbo, Caravan, Peter, Yang, Hua, Zeevaart, Jan, Rodriquez, Miguel, Oliveira, Ralph, Zubillaga, Marcela, Sakr, Tamer, and Spreckelmeyer, Sarah

Subjects
Highlight articles, Nuclear medicine, Radiochemistry, Radiopharmaceutical sciences, Radiopharmacy, Trends in radiopharmaceutical sciences
Abstract

BACKGROUND: The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biannual highlight commentary to update the readership on trends in the field of radiopharmaceutical development. MAIN BODY: This selection of highlights provides commentary on 21 different topics selected by each coauthoring Editorial Board member addressing a variety of aspects ranging from novel radiochemistry to first-in-human application of novel radiopharmaceuticals. CONCLUSION: Trends in radiochemistry and radiopharmacy are highlighted. Hot topics cover the entire scope of EJNMMI Radiopharmacy and Chemistry, demonstrating the progress in the research field in many aspects.

Published
2023

3. Highlight selection of radiochemistry and radiopharmacy developments by editorial board.

Author

Toyohara, Jun, Al-Qahtani, Mohammed, Huang, Ya-Yao, Cazzola, Emiliano, Todde, Sergio, Furumoto, Shozo, Mikolajczak, Renata, Decristoforo, Clemens, Gillings, Nic, Yang, Min, Reilly, Raymond, Duatti, Adriano, Denkova, Antonia, Schirrmacher, Ralf, Carlucci, Giuseppe, Seimbille, Yann, Liu, Zhaofei, Ellis, Beverley, Cornelissen, Bart, Kopka, Klaus, and Bernardes, Emerson

Subjects
Highlight Articles, Nuclear Medicine, Radiochemistry, Radiopharmaceutical Sciences, Radiopharmacy, Trends in Radiopharmaceutical Sciences
Abstract

BACKGROUND: The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biannual highlight commentary to update the readership on trends in the field of radiopharmaceutical development. MAIN BODY: This commentary of highlights has resulted in 21 different topics selected by each coauthoring Editorial Board member addressing a variety of aspects ranging from novel radiochemistry to first in man application of novel radiopharmaceuticals. CONCLUSION: Trends in radiochemistry and radiopharmacy are highlighted demonstrating the progress in the research field in various topics including new PET-labelling methods, FAPI-tracers and imaging, and radionuclide therapy being the scope of EJNMMI Radiopharmacy and Chemistry.

Published
2022

5. Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Author

Jean DaSilva, Clemens Decristoforo, Robert H. Mach, Guy Bormans, Giuseppe Carlucci, Mohammed Al-Qahtani, Adriano Duatti, Antony D. Gee, Wiktor Szymanski, Sietske Rubow, Jeroen Hendrikx, Xing Yang, Hongmei Jia, Junbo Zhang, Peter Caravan, Hua Yang, Jan Rijn Zeevaart, Miguel Avila Rodriquez, Ralph Santos Oliveira, Marcela Zubillaga, Tamer Sakr, and Sarah Spreckelmeyer

Subjects
Highlight articles, Radiochemistry, Radiopharmacy, Radiopharmaceutical sciences, Nuclear medicine, Trends in radiopharmaceutical sciences, Medical physics. Medical radiology. Nuclear medicine, R895-920, Therapeutics. Pharmacology, RM1-950
Abstract

Abstract Background The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biannual highlight commentary to update the readership on trends in the field of radiopharmaceutical development. Main body This selection of highlights provides commentary on 21 different topics selected by each coauthoring Editorial Board member addressing a variety of aspects ranging from novel radiochemistry to first-in-human application of novel radiopharmaceuticals. Conclusion Trends in radiochemistry and radiopharmacy are highlighted. Hot topics cover the entire scope of EJNMMI Radiopharmacy and Chemistry, demonstrating the progress in the research field in many aspects.

Published
2023
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6. The DOTA macrocyclic cavity in metallic radiopharmaceuticals: Mythology or reality?

Author

Adriano Duatti

Subjects
DOTA, Macrocyclic cavity, Macrocyclic ligands, Macrocyclic effect, Metallic radiopharmaceuticals, Medical physics. Medical radiology. Nuclear medicine, R895-920, Therapeutics. Pharmacology, RM1-950
Abstract

Abstract Background The hypothetical concept of ‘macrocyclic cavity’ is largely employed as useful model to interpret the affinity of metal ions for the macrocyclic chelating ligand 2,2′,2′′,2′′′-(1,4,7,10-tetraazacyclododecane-1,4,7,10-tetrayl)tetraacetic acid (H4DOTA). It Is hypothesized that a close matching between the size of the macrocyclic cavity and that of the metallic ion is a key parameter to ensure the high-yield formation of stable coordination metal-DOTA complex. This approach has become popular in the design of radiopharmaceuticals containing radiometals and H4DOTA as chelating group. Results Based on X-ray structural data of metallic complexes formed by the ligand H4DOTA upon coordination with a variety of metals, an elementary argument based on Euclidean geometry is presented here that questions the existence of the hypothetical ‘macrocyclic cavity’ within the chelator macrocycle. The geometrical analysis was applied to the complex formed by a Ga3+ ion coordinated to H4DOTA as model compound. Conclusions Application of Euclidean geometry to calculate bond angles in the coordination complex of the ligand H4DOTA with the Ga+3 ion, supposed to incorporate a hypothetical ‘macrocyclic cavity’, revealed that this conceptual entity has no physical reality and, therefore, cannot be considered a meaningful description of a stable structural arrangement for metallic radiopharmaceuticals.

Published
2023
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7. Highlight selection of radiochemistry and radiopharmacy developments by editorial board.

Author

Aime, Silvio, Al-Qahtani, Mohammed, Behe, Martin, Bormans, Guy, Carlucci, Giuseppe, DaSilva, Jean, Decristoforo, Clemens, Duatti, Adriano, Elsinga, Philip, Kopka, Klaus, Li, Xiang-Guo, Liu, Zhibo, Mach, Robert, Middel, Oskar, Passchier, Jan, Patt, Marianne, Penuelas, Ivan, Rey, Ana, Scott, Peter, Todde, Sergio, Toyohara, Jun, Vugts, Danielle, and Yang, Zhi

Abstract

BACKGROUND: The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biyearly highlight commentary to update the readership on trends in the field of radiopharmaceutical development. RESULTS: This commentary of highlights has resulted in 23 different topics selected by each member of the Editorial Board addressing a variety of aspects ranging from novel radiochemistry to first in man application of novel radiopharmaceuticals. CONCLUSION: Trends in radiochemistry and radiopharmacy are highlighted demonstrating the progress in the research field being the scope of EJNMMI Radiopharmacy and Chemistry.

Published
2021

9. Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Author

Jun Toyohara, Mohammed Al-Qahtani, Ya-Yao Huang, Emiliano Cazzola, Sergio Todde, Shozo Furumoto, Renata Mikolajczak, Clemens Decristoforo, Nic Gillings, Min Yang, Raymond Reilly, Adriano Duatti, Antonia Denkova, Ralf Schirrmacher, Giuseppe Carlucci, Yann Seimbille, Zhaofei Liu, Beverley Ellis, Bart T. Cornelissen, Klaus Kopka, and Emerson Bernardes

Subjects
Highlight Articles, Radiochemistry, Radiopharmacy, Radiopharmaceutical Sciences, Nuclear Medicine, Trends in Radiopharmaceutical Sciences, Medical physics. Medical radiology. Nuclear medicine, R895-920, Therapeutics. Pharmacology, RM1-950
Abstract

Abstract Background The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biannual highlight commentary to update the readership on trends in the field of radiopharmaceutical development. Main Body This commentary of highlights has resulted in 21 different topics selected by each coauthoring Editorial Board member addressing a variety of aspects ranging from novel radiochemistry to first in man application of novel radiopharmaceuticals. Conclusion Trends in radiochemistry and radiopharmacy are highlighted demonstrating the progress in the research field in various topics including new PET-labelling methods, FAPI-tracers and imaging, and radionuclide therapy being the scope of EJNMMI Radiopharmacy and Chemistry.

Published
2022
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15. Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Author

Silvio Aime, Mohammed Al-Qahtani, Martin Behe, Guy Bormans, Giuseppe Carlucci, Jean N. DaSilva, Clemens Decristoforo, Adriano Duatti, Philip H. Elsinga, Klaus Kopka, Xiang-Guo Li, Zhibo Liu, Robert H. Mach, Oskar Middel, Jan Passchier, Marianne Patt, Ivan Penuelas, Ana Rey, Peter J. H. Scott, Sergio Todde, Jun Toyohara, Danielle Vugts, and Zhi Yang

Subjects
Medical physics. Medical radiology. Nuclear medicine, R895-920, Therapeutics. Pharmacology, RM1-950
Abstract

Abstract Background The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biyearly highlight commentary to update the readership on trends in the field of radiopharmaceutical development. Results This commentary of highlights has resulted in 23 different topics selected by each member of the Editorial Board addressing a variety of aspects ranging from novel radiochemistry to first in man application of novel radiopharmaceuticals. Conclusion Trends in radiochemistry and radiopharmacy are highlighted demonstrating the progress in the research field being the scope of EJNMMI Radiopharmacy and Chemistry.

Published
2021
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17. Fundamentals of Rhenium-188 Radiopharmaceutical Chemistry

Author

Janke Kleynhans, Adriano Duatti, and Cristina Bolzati

Subjects
rhenium, transition metal chemistry, ligand field theory, frontier orbitals, nuclear medicine, 188W/188Re generator, Organic chemistry, QD241-441
Abstract

The β− emitter, rhenium-188 (188Re), has long been recognized as an attractive candidate for targeted cancer radionuclide therapy (TRNT). This transition metal shares chemical similarities with its congener element technetium, whose nuclear isomer technetium-99m (99mTc) is the current workhorse of diagnostic nuclear medicine. The differences between these two elements have a significant impact on the radiolabelling methods and should always receive critical attention. This review aims to highlight what needs to be considered to design a successful radiopharmaceutical incorporating 118Re. Some of the most effective strategies for preparing therapeutic radiopharmaceuticals with 188Re are illustrated and rationalized using the concept of the inorganic functional group (core) and a simple ligand field theoretical model combined with a qualitative definition of frontiers orbitals. Of special interest are the Re(V) oxo and Re(V) nitrido functional groups. Suitable ligands for binding to these cores are discussed, successful clinical applications are summarized, and a prediction of viable future applications is presented. Rhenium-188 decays through the emission of a high energy beta particle (2.12 MeV max energy) and a half-life of 16.9 h. An ideal biological target would therefore be a high-capacity target site (transporters, potential gradients, tumour microenvironment) with less emphasis on saturable targets such as overexpressed receptors on smaller metastases.

Published
2023
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20. Research on Emerging Medical radionuclides from the X-sections (REMIX): The Accelerator-based Production of 47Sc, 149Tb, 152Tb, 155Tb and 161Tb

Author

Pupillo, G, primary, Anselmi-Tamburini, U, additional, Barbaro, F, additional, Bello, M, additional, Bortolussi, S, additional, Boschi, A, additional, Campostrini, M, additional, Canton, L, additional, Carante, M P, additional, Cazzola, E, additional, Cisternino, S, additional, Colombi, A, additional, Colucci, M, additional, Dominicis, L De, additional, Nardo, L De, additional, Duatti, A, additional, Fontana, A, additional, Gorgoni, G, additional, Groppi, F, additional, Haddad, F, additional, Manenti, S, additional, Martini, P, additional, Meléndez-Alafort, L, additional, Mou, L, additional, Nigron, E, additional, Rigato, V, additional, Sciacca, G, additional, and Esposito, J, additional

Published
2023
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21. Cyclotron production of 67Cu: A new measurement of the 68Zn(p,2p)67Cu, 68Zn(p,2n)67Ga and 68Zn(p,3n)66Ga nuclear cross sections

Author

Gaia Pupillo, Thomas Sounalet, Nathalie Michel, Férid Haddad, Liliana Mou, Luciano Canton, Andrea Fontana, Juan Esposito, and Adriano Duatti

Subjects
producción de isotopos, generadores de radisótopos, ciclotrones, secciones eficaces, cobre 6, Nuclear engineering. Atomic power, TK9001-9401, Medical physics. Medical radiology. Nuclear medicine, R895-920
Abstract

The cross sections of the 68Zn(p,2p)67Cu,68Zn(p,2n)67Ga and 68Zn(p,3n)66Ga reactions were measured at the ARRONAX facility by using the 70 MeV cyclotron, with particular attention to the production of the theranostic radionuclide 67Cu. Enriched 68Zn material was electroplated on silver backing and exposed to alow-intensity proton beam by using the stacked-foils target method. Since 67Cu and 67Ga radionuclides have similar half-lives and same γ-lines (they both decay to 67Zn), a radiochemical process aimed at Cu/Ga separation was mandatory to avoid interferences in γ-spectrometry measurements. A simple chemical procedure having a high separation efficiency (>99%)was developed and monitored during each foil processing, thanks to the tracer isotopes 61Cu and 66Ga.Nuclear cross sections were measured in the energy range 35-70 MeV by using reference reactions recommended by the International Atomic Energy Agency (IAEA) to monitor beam flux. In comparison with literature data a general good agreement on the trend of the nuclear reactions was noted, especially with latest measurements, but slightly lower values were obtained in case of 67Cu. Experimental results of the 68Zn(p,2p)67Cu,68Zn(p,2n)67Ga and 68Zn(p,3n)66Ga reactions were also compared with the theoretical values estimated by using the nuclear reaction code TALYS. The production yield of the theranostic radionuclide 67Cu was estimated considering the results obtained in this work.

Published
2019

23. IAEA Contribution to Nanosized Targeted Radiopharmaceuticals for Drug Delivery

Author

Amir R. Jalilian, Blanca Ocampo-García, Wanvimol Pasanphan, Tamer M. Sakr, Laura Melendez-Alafort, Mariano Grasselli, Ademar B. Lugao, Hassan Yousefnia, Clelia Dispenza, Siti Mohd Janib, Irfan U. Khan, Michał Maurin, Piotr Ulański, Say Chye Joachim Loo, Agnes Safrany, Joao A. Osso, Adriano Duatti, and Kattesh V. Katti

Subjects
nanoparticles, metallic, non-metallic, polymeric, radiopharmaceuticals, radioisotopes, Pharmacy and materia medica, RS1-441
Abstract

The rapidly growing interest in the application of nanoscience in the future design of radiopharmaceuticals and the development of nanosized radiopharmaceuticals in the late 2000′s, resulted in the creation of a Coordinated Research Project (CRP) by the International Atomic Energy Agency (IAEA) in 2014. This CRP entitled ‘Nanosized delivery systems for radiopharmaceuticals’ involved a team of expert scientist from various member states. This team of scientists worked on a number of cutting-edge areas of nanoscience with a focus on developing well-defined, highly effective and site-specific delivery systems of radiopharmaceuticals. Specifically, focus areas of various teams of scientists comprised of the development of nanoparticles (NPs) based on metals, polymers, and gels, and their conjugation/encapsulation or decoration with various tumor avid ligands such as peptides, folates, and small molecule phytochemicals. The research and development efforts also comprised of developing optimum radiolabeling methods of various nano vectors using diagnostic and therapeutic radionuclides including Tc-99m, Ga-68, Lu-177 and Au-198. Concerted efforts of teams of scientists within this CRP has resulted in the development of various protocols and guidelines on delivery systems of nanoradiopharmaceuticals, training of numerous graduate students/post-doctoral fellows and publications in peer reviewed journals while establishing numerous productive scientific networks in various participating member states. Some of the innovative nanoconstructs were chosen for further preclinical applications—all aimed at ultimate clinical translation for treating human cancer patients. This review article summarizes outcomes of this major international scientific endeavor.

Published
2022
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25. Highly Efficient Micro-Scale Liquid-Liquid In-Flow Extraction of 99mTc from Molybdenum

Author

Petra Martini, Licia Uccelli, Adriano Duatti, Lorenza Marvelli, Juan Esposito, and Alessandra Boschi

Subjects
microfluidics, liquid–liquid extraction, technetium-99m, in-flow chemistry, Organic chemistry, QD241-441
Abstract

The trend to achieve even more compact-sized systems is leading to the development of micro-scale reactors (lab-on-chip) in the field of radiochemical separation and radiopharmaceutical production. Technetium-99m extraction from both high and low specific activity molybdenum could be simply performed by MEK-driven solvent extraction if it were not for unpractical automation. The aim of this work is to develop a solvent extraction and separation process of technetium from molybdenum in a micro-scale in-flow chemistry regime with the aid of a capillary loop and a membrane-based separator, respectively. The developed system is able to extract and separate quantitatively and selectively (91.0 ± 1.8% decay corrected) the [99mTc]TcO4Na in about 20 min, by using a ZAIPUT separator device. In conclusion, we demonstrated for the first time in our knowledge the high efficiency of a MEK-based solvent extraction process of 99mTc from a molybdenum-based liquid phased in an in-flow micro-scale regime.

Published
2021
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26. Synthesis and Characterization of Manganese Dithiocarbamate Complexes: New Evidence of Dioxygen Activation

Author

Petra Martini, Alessandra Boschi, Lorenza Marvelli, Licia Uccelli, Stefano Carli, Giuseppe Cruciani, Erika Marzola, Anna Fantinati, Juan Esposito, and Adriano Duatti

Subjects
manganese complexes, diethyldithiocarbamate, manganese(III) complexes, dioxygen activator, Organic chemistry, QD241-441
Abstract

(1) Background: Metal dithiocarbamate compounds have long been the subject of research due to their ease of formation, excellent properties and potential applications. However, manganese complexes with dithiocarbamates, to our knowledge, have never been used for medical imaging applications. With the aim of developing a new class of mononuclear manganese(II)-based agents for molecular imaging applications, we performed a specific investigation into the synthesis of mononuclear bis-substituted Mn(II) complexes with dithiocarbamate ligands. (2) Methods: Synthesis in either open or inert atmosphere at different Mn(II) to diethyldithiocarbamate molar ratios were performed and the products characterized by IR, EA, ESI-MS and XRD analysis. (3) Results: We found that only under oxygen-free atmospheric conditions the Mn(II) complex MnL2, where L = diethyldithiocarbamate ligand, is obtained, which was further observed to react with dioxygen in the solid state to form the intermediate superoxo Mn(III) complex [MnL2(η2-O2)]. The existence of the superoxo complex was revealed by mass spectroscopy, and this species was interpreted as an intermediate step in the reaction that led the bis-substituted Mn(II) complex, MnL2, to transform into the tris-substituted Mn(III) complex, MnL3. A similar result was found with the ligand L’ (= bis(N-ethoxyethyl)dithiocarbamate). (4) Conclusions: We found that in open atmosphere and in aqueous solution, only manganese(III) diethyldithiocarbamate complexes can be prepared. We report here a new example of a small-molecule Mn(II) complex that efficiently activates dioxygen in the solid state through the formation of an intermediate superoxide adduct.

Published
2021
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29. Supplementary Data from Lactate Rewires Lipid Metabolism and Sustains a Metabolic–Epigenetic Axis in Prostate Cancer

Author

Ippolito, Luigi, primary, Comito, Giuseppina, primary, Parri, Matteo, primary, Iozzo, Marta, primary, Duatti, Assia, primary, Virgilio, Francesca, primary, Lorito, Nicla, primary, Bacci, Marina, primary, Pardella, Elisa, primary, Sandrini, Giada, primary, Bianchini, Francesca, primary, Damiano, Roberta, primary, Ferrone, Lavinia, primary, la Marca, Giancarlo, primary, Serni, Sergio, primary, Spatafora, Pietro, primary, Catapano, Carlo V., primary, Morandi, Andrea, primary, Giannoni, Elisa, primary, and Chiarugi, Paola, primary

Published
2023
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30. Data from Lactate Rewires Lipid Metabolism and Sustains a Metabolic–Epigenetic Axis in Prostate Cancer

Author

Ippolito, Luigi, primary, Comito, Giuseppina, primary, Parri, Matteo, primary, Iozzo, Marta, primary, Duatti, Assia, primary, Virgilio, Francesca, primary, Lorito, Nicla, primary, Bacci, Marina, primary, Pardella, Elisa, primary, Sandrini, Giada, primary, Bianchini, Francesca, primary, Damiano, Roberta, primary, Ferrone, Lavinia, primary, la Marca, Giancarlo, primary, Serni, Sergio, primary, Spatafora, Pietro, primary, Catapano, Carlo V., primary, Morandi, Andrea, primary, Giannoni, Elisa, primary, and Chiarugi, Paola, primary

Published
2023
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32. Data from Lactate Rewires Lipid Metabolism and Sustains a Metabolic–Epigenetic Axis in Prostate Cancer

Author

Paola Chiarugi, Elisa Giannoni, Andrea Morandi, Carlo V. Catapano, Pietro Spatafora, Sergio Serni, Giancarlo la Marca, Lavinia Ferrone, Roberta Damiano, Francesca Bianchini, Giada Sandrini, Elisa Pardella, Marina Bacci, Nicla Lorito, Francesca Virgilio, Assia Duatti, Marta Iozzo, Matteo Parri, Giuseppina Comito, and Luigi Ippolito

Abstract

Lactate is an abundant oncometabolite in the tumor environment. In prostate cancer, cancer-associated fibroblasts (CAF) are major contributors of secreted lactate, which can be taken up by cancer cells to sustain mitochondrial metabolism. However, how lactate impacts transcriptional regulation in tumors has yet to be fully elucidated. Here, we describe a mechanism by which CAF-secreted lactate is able to increase the expression of genes involved in lipid metabolism in prostate cancer cells. This regulation enhanced intracellular lipid accumulation in lipid droplets (LD) and provided acetyl moieties for histone acetylation, establishing a regulatory loop between metabolites and epigenetic modification. Inhibition of this loop by targeting the bromodomain and extraterminal protein family of histone acetylation readers suppressed the expression of perilipin 2 (PLIN2), a crucial component of LDs, disrupting lactate-dependent lipid metabolic rewiring. Inhibition of this CAF-induced metabolic–epigenetic regulatory loop in vivo reduced growth and metastasis of prostate cancer cells, demonstrating its translational relevance as a therapeutic target in prostate cancer. Clinically, PLIN2 expression was elevated in tumors with a higher Gleason grade and in castration-resistant prostate cancer compared with primary prostate cancer. Overall, these findings show that lactate has both a metabolic and an epigenetic role in promoting prostate cancer progression.Significance:This work shows that stromal-derived lactate induces accumulation of lipid droplets, stimulates epigenetic rewiring, and fosters metastatic potential in prostate cancer.

Published
2023

33. Supplementary Data from Lactate Rewires Lipid Metabolism and Sustains a Metabolic–Epigenetic Axis in Prostate Cancer

Author

Paola Chiarugi, Elisa Giannoni, Andrea Morandi, Carlo V. Catapano, Pietro Spatafora, Sergio Serni, Giancarlo la Marca, Lavinia Ferrone, Roberta Damiano, Francesca Bianchini, Giada Sandrini, Elisa Pardella, Marina Bacci, Nicla Lorito, Francesca Virgilio, Assia Duatti, Marta Iozzo, Matteo Parri, Giuseppina Comito, and Luigi Ippolito

Abstract

Supplementary Data from Lactate Rewires Lipid Metabolism and Sustains a Metabolic–Epigenetic Axis in Prostate Cancer

Published
2023

34. 1806: Transcriptome and tumor immune infiltrate in breast cancer treated with preoperative radiosurgery.

Author

Mangoni, Monica, Duatti, Assia, Caini, Saverio, Fiorito, Giovanni, Salvatore, Giulia, Anichini, Giulia, Sottili, Mariangela, Visani, Luca, Francolini, Giulio, Di Cataldo, Vanessa, Loi, Mauro, Becherini, Carlotta, Salvestrini, Viola, Bianchi, Simonetta, Masi, Laura, Doro, Raffaella, Nori, Jacopo, Orzalesi, Lorenzo, Bernini, Marco, and Greto, Daniela

Subjects
*CANCER invasiveness, *BREAST cancer, *RADIOSURGERY, *TRANSCRIPTOMES, *TUMORS
Published
2024
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36. Fundamentals of Rhenium-188 Radiopharmaceutical Chemistry

Author

CRISTINA BOLZATI, Adriano Duatti, and Janke Kleynhans

Subjects
Radioisotopes, theranostic, Organic Chemistry, Pharmaceutical Science, Technetium, 188W/188Re generator, Analytical Chemistry, ligand field theory, Rhenium, Chemistry (miscellaneous), frontier orbitals, targeted radionuclide therapy (TRNT), Drug Discovery, Molecular Medicine, transition metal chemistry, nuclear medicine, Physical and Theoretical Chemistry, Radiopharmaceuticals, perrhenate
Abstract

The β- emitter, rhenium-188 (188Re), has long been recognized as an attractive candidate for targeted cancer radionuclide therapy (TRNT). This transition metal shares chemical similarities with its congener element technetium, whose nuclear isomer technetium-99m (99mTc) is the current workhorse of diagnostic nuclear medicine. The differences between these two elements have a significant impact on the radiolabelling methods and should always receive critical attention. This review aims to highlight what needs to be considered to design a successful radiopharmaceutical incorporating 118Re. Some of the most effective strategies for preparing therapeutic radiopharmaceuticals with 188Re are illustrated and rationalized using the concept of the inorganic functional group (core) and a simple ligand field theoretical model combined with a qualitative definition of frontiers orbitals. Of special interest are the Re(V) oxo and Re(V) nitrido functional groups. Suitable ligands for binding to these cores are discussed, successful clinical applications are summarized, and a prediction of viable future applications is presented. Rhenium-188 decays through the emission of a high energy beta particle (2.12 MeV max energy) and a half-life of 16.9 h. An ideal biological target would therefore be a high-capacity target site (transporters, potential gradients, tumour microenvironment) with less emphasis on saturable targets such as overexpressed receptors on smaller metastases. ispartof: MOLECULES vol:28 issue:3 ispartof: location:Switzerland status: published

Published
2023

41. Cyclotron-production of manganese-52 for multi-modal imaging applications

Author

Boschi, Alessandra, primary, Martini, Petra, additional, Cazzola, Emiliano, additional, Cisternino, Sara, additional, Ghirardi, Teresa, additional, Duatti, Adriano, additional, Gorgoni, Giancarlo, additional, Marvelli, Lorenza, additional, Mou, Liliana, additional, Pupillo, Gaia, additional, Alvarez, Carlos Rossi, additional, Sciacca, Gabriele, additional, Amico, Jonathan, additional, Uccelli, Licia, additional, and Esposito, Juan, additional

Published
2022
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44. Highlight selection of radiochemistry and radiopharmacy developments by editorial board

Author

Aime, S, Al-Qahtani, M, Behe, M, Bormans, G, Carlucci, G, Dasilva, J, Decristoforo, C, Duatti, A, Elsinga, P, Kopka, K, Li, X, Liu, Z, Mach, R, Middel, O, Passchier, J, Patt, M, Penuelas, I, Rey, A, Scott, P, Todde, S, Toyohara, J, Vugts, D, Yang, Z, Aime S., Al-Qahtani M., Behe M., Bormans G., Carlucci G., DaSilva J. N., Decristoforo C., Duatti A., Elsinga P. H., Kopka K., Li X. -G., Liu Z., Mach R. H., Middel O., Passchier J., Patt M., Penuelas I., Rey A., Scott P. J. H., Todde S., Toyohara J., Vugts D., Yang Z., Aime, S, Al-Qahtani, M, Behe, M, Bormans, G, Carlucci, G, Dasilva, J, Decristoforo, C, Duatti, A, Elsinga, P, Kopka, K, Li, X, Liu, Z, Mach, R, Middel, O, Passchier, J, Patt, M, Penuelas, I, Rey, A, Scott, P, Todde, S, Toyohara, J, Vugts, D, Yang, Z, Aime S., Al-Qahtani M., Behe M., Bormans G., Carlucci G., DaSilva J. N., Decristoforo C., Duatti A., Elsinga P. H., Kopka K., Li X. -G., Liu Z., Mach R. H., Middel O., Passchier J., Patt M., Penuelas I., Rey A., Scott P. J. H., Todde S., Toyohara J., Vugts D., and Yang Z.

Abstract

Background: The Editorial Board of EJNMMI Radiopharmacy and Chemistry releases a biyearly highlight commentary to update the readership on trends in the field of radiopharmaceutical development. Results: This commentary of highlights has resulted in 23 different topics selected by each member of the Editorial Board addressing a variety of aspects ranging from novel radiochemistry to first in man application of novel radiopharmaceuticals. Conclusion: Trends in radiochemistry and radiopharmacy are highlighted demonstrating the progress in the research field being the scope of EJNMMI Radiopharmacy and Chemistry.

Published
2021

45. 18th European Symposium on Radiopharmacy and Radiopharmaceuticals: Salzburg, Austria. 7-10 April 2016

Author

Radchenko, V., Engle, J. W., Roy, C., Griswold, J., Nortier, M. F., Birnbaum, E. R., Brugh, M., Mirzadeh, S., John, K. D., Fassbender, M. E., Zhai, Chuangyan, Franssen, Gerben M., Petrik, Milos, Laverman, Peter, Decristoforo, Clemens, Samia, Ait-Mohand, Véronique, Dumulon-Perreault, Brigitte, Guérin, Summer, D., Kroess, A., Rangger, C., Haas, H., Laverman, P., Gerben, F., von Guggenberg, E., Decristoforo, C., Bolzati, Cristina, Salvarese, Nicola, Refosco, Fiorenzo, Meléndez-Alafort, Laura, Carpanese, Debora, Rosato, Antonio, Saviano, Michele, Del Gatto, Annarita, Comegna, Daniela, Zaccaro, Laura, Billaud, Emilie, Ahamed, Muneer, Cleeren, Frederik, Shahbazali, Elnaz, Noël, Tim, Hessel, Volker, Verbruggen, Alfons, Bormans, Guy, Cleeren, F., Lecina, J., Koole, M., Verbruggen, A., Bormans, G., Lugatoa, B., Stucchia, S., Turollaa, E. A., Giulianoa, L., Toddea, S., Ferraboschib, P., Klok, R. P., Mooijer, M. P. J., Hendrikse, N. H., Windhorst, A. D., Collet, C., Petry, N., Chrétien, F., Karcher, G., Pellegrini-Moïse, N., Lamandé-Langle, S., Pfaff, Sarah, Philippe, Cecile, Mitterhauser, Markus, Hacker, Marcus, Wadsak, Wolfgang, Guérard, François, Lee, Yong-Sok, Gouard, Sébastien, Baidoo, Kwamena, Alliot, Cyrille, Chérel, Michel, Brechbiel, Martin W., Gestin, Jean-François, Lam, K., Chan, C., Reilly, R. M., Paillas, Salomé, Marshall, John, Pouget, Jean-Pierre, Sosabowski, Jane, Briard, Emmanuelle, Auberson, Yves P., Reilly, John, Healy, Mark, Sykes, David, Paulus, Andreas, Lichtenbelt, Wouter van Marken, Mottaghy, Felix, Bauwens, Matthias, Baranski, Ann-Christin, Schäfer, Martin, Bauder-Wüst, Ulrike, Haberkorn, Uwe, Eder, Matthias, Kopka, Klaus, Chaussard, M., Hosten, B., Vignal, N., Tsoupko-Sitnikov, V., Hernio, N., Hontonnou, F., Merlet, P., Poyet, J. L., Sarda-Mantel, L., Rizzo-Padoin, N., Cardinale, J., Schäfer, M., Benešová, M., Bauder-Wüst, U., Seibert, O., Giesel, F., Haberkorn, U., Eder, M., Kopka, K., Nematallah, Mansour, Michel, Paquette, Samia, Ait-Mohand, Véronique, Dumulon-Perreault, Roger, Lecomte, Brigitte, Guérin, Fernandez-Maza, L., Rivera-Marrero, S., Capote, A. Prats, Parrado-Gallego, A., Fernandez-Gomez, I., Balcerzyk, M., Sablon-Carrazana, M., Perera-Pintado, A., Merceron-Martinez, D., Acosta-Medina, E., Rodriguez-Tanty, C., Attili, Bala, Ahamed, Muneer, Bormans, Guy, Philippe, C., Zeilinger, M., Scherer, T., Fürnsinn, C., Dumanic, M., Wadsak, W., Hacker, M., Mitterhauser, M., Janssen, B., Vugts, D. J., Molenaar, G.T. T., Funke, U., Kruijer, P. S., Dollé, F., Bormans, G., Lammertsma, A. A., Windhorst, A. D., Vermeulen, Koen, Ahamed, Muneer, Schnekenburger, Michael, Froeyen, Mathy, Olberg, Dag Erlend, Diederich, Marc, Bormansa, Guy, Raaphorst, R. M., Luurtsema, G., Lammertsma, A. A., Elsinga, P. H., Windhorst, A D., Rotteveel, Lonneke, Funke, Uta, ten Dijke, Peter, Bogaard, Harm Jan, Lammertsma, Adriaan A., Windhorst, Albert D., Song, Lei, Able, Sarah, Falzone, Nadia, Kersemans, Veerle, Vallis, Katherine, Carta, Davide, Salvarese, Nicola, Sihver, Wiebke, Gao, Feng, Pietzsch, Hans Jürgen, Biondi, Barbara, Ruzza, Paolo, Refosco, Fiorenzo, Bolzati, Cristina, Haubner, Roland, Finkensted, Armin, Stegmair, Armin, Rangger, Christine, Decristoforo, Clemens, Zoller, Heinz, Virgolini, Irene J., Pooters, Ivo, Lotz, Maartje, Wierts, Roel, Mottaghy, Felix, Bauwens, Matthias, Forsback, Sarita, Jörgen, Bergman, Riikka, Kivelä, Karageorgou, M., Radović, M., Tsoukalas, C., Antic, B., Gazouli, M., Paravatou-Petsotas, M., Xanthopouls, S., Calamiotou, M., Stamopoulos, D., Vranješ-Durić, S., Bouziotis, P., Lunev, A. S., Larenkov, A. A., Petrosova, K. A., Klementyeva, O. E., Kodina, G. E., Kvernenes, O. H., Adamsen, T. C. H., Martin, René, Weidlich, Sebastian, Zerges, Anna-Maria, Gameiro, Cristiana, Lazarova, Neva, Müllera, Marco, Luurtsema, Gert, de Vries, Michèl, Ghyoot, Michel, van der Woude, Gina, Zijlma, Rolf, Dierckx, Rudi, Boersma, Hendrikus H., Elsinga, Philip H., Lambrecht, Fatma Yurt, Er, Ozge, Ince, Mine, Avci, Cıgır Biray, Gunduz, Cumhur, Sarı, Fatma Aslihan, Ocakoglu, Kasim, Er, Ozge, Ersoz, Onur Alp, Lambrecht, Fatma Yurt, Ince, Mine, Kayabasi, Cagla, Gunduz, Cumhur, Kniess, Torsten, Meister, Sebastian, Fischer, Steffen, Steinbach, Jörg, Ashfaq, Rabia, Iqbal, Saeed, ullah Khan, Irfan, Iglesias-Jerez, R., Martín-Banderas, L., Perera-Pintado, A., Borrego-Dorado, I., Farinha-Antunes, Ines, Kwizera, Chantal, Lacivita, Enza, Lucente, Ermelinda, Niso, Mauro, De Giorgio, Paola, Perrone, Roberto, Colabufo, Nicola A., Elsinga, Philip H., Leopoldo, Marcello, Vaulina, V. V., Fedorova, O. S., Orlovskaja, V. V., Chen, С. L., Li, G. Y., Meng, F. C., Liu, R. S., Wang, H. E., Krasikova, R. N., Meléndez-Alafort, Laura, Abozeid, Mohamed, Ferro-Flores, Guillermina, Negri, Anna, Bello, Michele, Uzunov, Nikolay, Paiusco, Martha, Esposito, Juan, Rosato, Antonio, Meléndez-Alafort, Laura, Bolzati, Cristina, Ferro-Flores, Guillermina, Salvarese, Nicola, Carpanese, Debora, Abozeid, Mohamed, Rosato, Antonio, Uzunov, Nikolay, Palmieri, L., Verbrugghen, T., Glassner, M., Hoogenboom, R., Staelens, S., Wyffels, L., Orlovskaja, V. V., Kuznetsova, O. F., Fedorova, O. S., Maleev, V. I., Belokon, Yu. N., Geolchanyan, A., Saghyan, A. S., Mu, L., Schibli, R., Ametamey, S. M., Krasikova, R. N., Revunov, Evgeny, Malmquist, Jonas, Johnström, Peter, Van Valkenburgh, Juno, Steele, Dalton, Halldin, Christer, Schou, Magnus, Osati, Samira, Paquette, Michel, Beaudoin, Simon, Ali, Hasrat, Guerin, Brigitte, Leyton, Jeffrey V., van Lier, Johan E., Di Iorio, V, Iori, M., Donati, C., Lanzetta, V., Capponi, P. C., Rubagotti, S., Dreger, T., Kunkel, F., Asti, M., Zhai, Chuangyan, Rangger, Christine, Summer, Dominik, Haas, Hubertus, Decristoforo, Clemens, Kijprayoon, Suphansa, Ruangma, Ananya, Ngokpol, Suthatip, Tuamputsha, Samart, Filp, Ulrike, Pees, Anna, Taddei, Carlotta, Pekošak, Aleksandra, Gee, Antony D., Poot, Alex J., Windhorst, Albert D., Gunay, Mine Silindir, Ozer, A. Yekta, Erdogan, Suna, Baysal, Ipek, Guilloteau, Denis, Chalon, Sylvie, Galli, Filippo, Artico, Marco, Taurone, Samanta, Bianchi, Enrica, Weintraub, Bruce D., Skudlinski, Mariusz, Signore, Alberto, Lepareur, Nicolas, Noiret, Nicolas, Hindré, François, Lacœuille, Franck, Benoist, Eric, Garin, Etienne, Trejo-Ballado, F., Zamora-Romo, E., Manrique-Arias, J. C., Gama-Romero, H M, Contreras-Castañon, G., Tecuapetla-Chantes, R. G., Avila-Rodriguez, M. A., Kvaternik, H., Hausberger, D., Zink, C., Rumpf, B., Aigner, R. M., Kvaternik, H., Hausberger, D., Rumpf, B., Aigner, R. M., Janković, Drina, Lakić, Mladen, Savić, Aleksandar, Ristić, Slavica, Nikolić, Nadežda, Vukadinović, Aleksandar, Sabo, Tibor J., Vranješ-Đurić, Sanja, Vranješ-Đurić, S., Radović, M., Janković, D., Nikolić, N., Goya, G. F., Calatayud, P., Spasojević, V., Antić, B., Goblet, David, Gameiro, Cristiana, Lazarova, Neva, Gameiro, Cristiana, Oxley, Ian, Abrunhosa, Antero, Kramer, Vasko, Vosjan, Maria, Spaans, Arnold, Vats, Kusum, Satpati, Drishty, Sarma, Haladhar D., Banerjee, Sharmila, Wojdowska, W., Pawlak, D. W., Parus, L. J., Garnuszek, P., Mikołajczak, R., Pijarowska-Kruszyna, J., Jaron, A., Kachniarz, A., Malkowski, B., Garnuszek, P., Mikolajczak, R., Ilem-Ozdemir, Derya, Caglayan-Orumlu, Oya, Asikoglu, Makbule, Ilem-Ozdemir, Derya, Caglayan-Orumlu, Oya, Asikoglu, Makbule, Eveliina, Arponen, Semi, Helin, Timo, Saarinen, Simo, Vauhkala, Esa, Kokkomäki, Pertti, Lehikoinen, De Simone, Mariarosaria, Pascali, Giancarlo, Carzoli, Ludovica, Quaglierini, Mauro, Telleschi, Mauro, Salvadori, Piero A., Lam, Phoebe, Aistleitner, Martina, Eichinger, Reinhard, Artner, Christoph, Nakka, Surendra, MC, Hemantha Kumara, Al-Qahtani, Mohammed, Al-Qahtani, Mohammed, Al-Malki, Yousif, Mambilima, N., Rubow, S. M., Berroterán-Infante, N., Hacker, M., Mitterhauser, M., Wadsak, W., Funke, Uta, Cleeren, Frederik, Lecina, Joan, Gallardo, Rodrigo, Verbruggen, Alfons M., Bormans, Guy, Ramos-Membrive, Rocío, Brotons, Ana, Quincoces, Gemma, Inchaurraga, Laura, de Redín, Inés Luis, Morán, Verónica, García-García, Berta, Irache, Juan Manuel, Peñuelas, Iván, Trabelsi, M., Cooper, M. S., Abella, Alejandra, Fuente, Teodomiro, Montellano, Antonio Jesús, Martínez, Teresa, Rabadan, Ruben, Meseguer-Olmo, Luis, Lehtiniemi, P., Yim, C., Mikkola, K., Nuutila, P., Solin, O., von Guggenberg, E., Rangger, C., Mair, C., Balogh, L., Pöstényi, Z., Pawlak, D., Mikołajczak, R., Socan, A., Peitl, P. Kolenc, Krošelj, M., Rangger, C., Decristoforo, C., Collet, C., Remy, S., Didier, R., Vergote, T., Karcher, G., Véran, N., Pawlak, D., Maurin, M., Garnuszek, P., Karczmarczyk, U., Mikołajczak, R., Fredericia, Pil, Severin, Gregory, Groesser, Torsten, Köster, Ulli, Jensen, Mikael, Leonte, R., Puicea, F. D., Raicu, A., Min, E. A., Serban, R., Manda, G., Niculae, D., Zerna, Marion, Schieferstein, Hanno, Müller, Andre, Berndt, Mathias, Yim, Cheng-Bin, Mikkola, Kirsi, Nuutila, Pirjo, Solin, Olof, Seifert, D., Ráliš, J., Lebeda, O., Selivanova, Svetlana V., Senta, Helena, Lavallée, Éric, Caouette, Lyne, Turcotte, Éric, Lecomte, Roger, Kochovska, Marina Zdraveska, Ivanovska, Emilija Janjevik, Jokic, Vesna Spasic, Ackova, Darinka Gjorgieva, Smilkov, Katarina, Makreski, Petre, Stafilov, Trajče, Janevik-Ivanovska, Emilija, Alemu, Aschalew, Muchira, Joel Munene, Wanjeh, David Mwanza, Janevik-Ivanovska, Emilija, Janevik-Ivanovska, Emilija, Zdravev, Zoran, Bhonsle, Uday, Alberto, Osso Júnior João, Duatti, Adriano, Angelovska, Bistra, Stojanovska, Zdenka, Sarafinovska, Zorica Arsova, Bosnakovski, Darko, Gorgieva-Ackova, Darinka, Smilkov, Katarina, Drakalska, Elena, Venkatesh, Meera, Gulaboski, Rubin, Colin, Didier J., Inkster, James A. H., Germain, Stéphane, Seimbille, Yann, Atiq-ur-Rehman, and Cayero-Otero

Published
2016
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48. LARAMED: A Laboratory for Radioisotopes of Medical Interest

Author

Juan Esposito, Diego Bettoni, Alessandra Boschi, Michele Calderolla, Sara Cisternino, Giovanni Fiorentini, Giorgio Keppel, Petra Martini, Mario Maggiore, Liliana Mou, Micòl Pasquali, Lorenzo Pranovi, Gaia Pupillo, Carlos Rossi Alvarez, Lucia Sarchiapone, Gabriele Sciacca, Hanna Skliarova, Paolo Favaron, Augusto Lombardi, Piergiorgio Antonini, and Adriano Duatti

Subjects
Cyclotrons, medical radioisotopes, radiopharmaceuticals, targets, Organic chemistry, QD241-441
Abstract

The widespread availability of novel radioactive isotopes showing nuclear characteristics suitable for diagnostic and therapeutic applications in nuclear medicine (NM) has experienced a great development in the last years, particularly as a result of key advancements of cyclotron-based radioisotope production technologies. At Legnaro National Laboratories of the National Institute of Nuclear Physics (LNL-INFN), Italy, a 70-MeV high current cyclotron has been recently installed. This cyclotron will be dedicated not only to pursuing fundamental nuclear physics studies, but also to research related to other scientific fields with an emphasis on medical applications. LARAMED project was established a few years ago at LNL-INFN as a new research line aimed at exploiting the scientific power of nuclear physics for developing innovative applications to medicine. The goal of this program is to elect LNL as a worldwide recognized hub for the development of production methods of novel medical radionuclides, still unavailable for the scientific and clinical community. Although the research facility is yet to become fully operative, the LARAMED team has already started working on the cyclotron production of conventional medical radionuclides, such as Tc-99m, and on emerging radionuclides of high potential medical interest, such as Cu-67, Sc-47, and Mn-52.

Published
2018
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50. Review on 99mTc radiopharmaceuticals with emphasis on new advancements

Author

Adriano Duatti

Subjects
Cancer Research, medicine.diagnostic_test, Computer science, Rapid imaging, Nanotechnology, Receptor targeting, 030218 nuclear medicine & medical imaging, 03 medical and health sciences, 0302 clinical medicine, Positron emission tomography, 030220 oncology & carcinogenesis, High spatial resolution, medicine, Single Photon Emission Tomography, Molecular Medicine, Radiology, Nuclear Medicine and imaging, Membrane antigen
Abstract

Rapid imaging acquisition, high spatial resolution and sensitivity, powered by advancements in solid-state detector technology, are significantly changing the perspective of single photon emission tomography (SPECT). In particular, this evolutionary step is fueling a rediscovery of technetium-99m, a still unique radionuclide within the nuclear medicine scenario because of its ideal nuclear properties and easy preparation of its radiopharmaceuticals that does not require a costly infrastructure and complex procedures. Scope of this review is to show that the arsenal of technetium-99m radiopharmaceuticals is already equipped with imaging agents that may complement and integrate the role played by analogous tracers developed for positron emission tomography (PET). These include, in particular, somatostatin (SST) and prostate-specific membrane antigen (PSMA) receptor targeting agents, and a number of peptide-derived radiopharmaceuticals. Additionally, these recent technological developments, combined with new myocardial perfusion tracers having more favorable biodistribution and pharmacokinetic properties as compared to current commercial agents, may also reinvigorate the prevailing position still hold by technetium-99m radiopharmaceuticals in nuclear cardiology.

Published
2021

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