Production and Supply of α-Particle–Emitting Radionuclides for Targeted α-Therapy

Radchenko, Valery; Morgenstern, Alfred; Jalilian, Amir Reza; Ramogida, Caterina F.; Cutler, Cathy S.; Duchemin, Charlotte; Hoehr, Cornelia; Haddad, Ferrid; Bruchertseifer, Frank; Gausemel, H.; Yang, Hua; Osso, João Alberto; Washiyama, Kohshin; Czerwinski, Kenneth R.; Leufgen, Kirsten; Pruszyński, Marek; Valzdorf, Olga; Causey, Patrick; Schaffer, Paul; Perron, Randy; Maxim, Samsonov; Wilbur, D. Scott; Stora, T.; Li, Yawen

doi:10.2967/jnumed.120.261016

Cited by 81 publications

(60 citation statements)

References 62 publications

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“…germanium-68 and gallium-67, respectively [ 8 ]. The 90 Y currently available for radiolabelling is of high radionuclidic purity with no relevant amounts of accompanying nuclides [ 9 ]. Long-lived radioactive contaminants may require specific regulatory attention.…”

Section: Radionuclides and Radiopharmaceuticals Usedmentioning

confidence: 99%

Joint EANM, SNMMI and IAEA enabling guide: how to set up a theranostics centre

Herrmann

Giovanella

Santos

et al. 2022

Eur J Nucl Med Mol Imaging

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The theranostics concept using the same target for both imaging and therapy dates back to the middle of the last century, when radioactive iodine was first used to treat thyroid diseases. Since then, radioiodine has become broadly established clinically for diagnostic imaging and therapy of benign and malignant thyroid disease, worldwide. However, only since the approval of SSTR2-targeting theranostics following the NETTER-1 trial in neuroendocrine tumours and the positive outcome of the VISION trial has theranostics gained substantial attention beyond nuclear medicine. The roll-out of radioligand therapy for treating a high-incidence tumour such as prostate cancer requires the expansion of existing and the establishment of new theranostics centres. Despite wide global variation in the regulatory, financial and medical landscapes, this guide attempts to provide valuable information to enable interested stakeholders to safely initiate and operate theranostics centres. This enabling guide does not intend to answer all possible questions, but rather to serve as an overarching framework for multiple, more detailed future initiatives. It recognizes that there are regional differences in the specifics of regulation of radiation safety, but common elements of best practice valid globally.

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Section: Radionuclides and Radiopharmaceuticals Usedmentioning

confidence: 99%

Joint EANM, SNMMI and IAEA enabling guide: how to set up a theranostics centre

Herrmann

Giovanella

Santos

et al. 2022

Eur J Nucl Med Mol Imaging

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“…While radionuclides like 68 Ga, 18 F, or 177 Lu have become a sort of routine in the use of radiolabeled PSMA inhibitors, other radionuclides are gaining attention due to their specific properties [ 206 , 207 , 208 ]. For example, 225 Ac can play a pivotal role in targeted alpha therapy (TAT) of prostate cancer [ 48 , 51 , 78 , 209 , 210 , 211 , 212 , 213 , 214 , 215 ], but additional preclinical studies and prospective clinical trials need to be performed to secure its safety and efficacy [ 216 , 217 , 218 , 219 , 220 , 221 ].…”

Section: Potential Radionuclides For the Future Use Of Psma Inhibitorsmentioning

confidence: 99%

Radiolabeled PSMA Inhibitors

Neels

Kopka

Liolios

et al. 2021

Cancers

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PSMA has shown to be a promising target for diagnosis and therapy (theranostics) of prostate cancer. We have reviewed developments in the field of radio- and fluorescence-guided surgery and targeted photodynamic therapy as well as multitargeting PSMA inhibitors also addressing albumin, GRPr and integrin αvβ3. An overview of the regulatory status of PSMA-targeting radiopharmaceuticals in the USA and Europe is also provided. Technical and quality aspects of PSMA-targeting radiopharmaceuticals are described and new emerging radiolabeling strategies are discussed. Furthermore, insights are given into the production, application and potential of alternatives beyond the commonly used radionuclides for radiolabeling PSMA inhibitors. An additional refinement of radiopharmaceuticals is required in order to further improve dose-limiting factors, such as nephrotoxicity and salivary gland uptake during endoradiotherapy. The improvement of patient treatment achieved by the advantageous combination of radionuclide therapy with alternative therapies is also a special focus of this review.

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“…In the current TAT, 227 Th, 225 Ac, 213 Bi, 212 Bi and 149 Tb have become promising therapeutic radionuclides [144]. However, except for 227 Th, the use of HOPO-based bifunctional chelating agents in radiopharmaceuticals of 225 Ac, 213 Bi, 212 Bi and 149 Tb has not been reported.…”

Section: Summary and Future Prospectivementioning

confidence: 99%

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

Zhou¹,

Dong²,

Shen

2021

Molecules

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Hydroxypyridinones (HOPOs) have been used in the chelation therapy of iron and actinide metals. Their application in metal-based radiopharmaceuticals has also been increasing in recent years. This review article focuses on how multidentate HOPOs can be used in targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals. The general structure of radiometal-based targeted radiopharmaceuticals, a brief description of siderophores, the basic structure and properties of bidentate HOPO, some representative HOPO multidentate chelating agents, radiopharmaceuticals based on HOPO multidentate bifunctional chelators for gallium-68, thorium-227 and zirconium-89, as well as the future prospects of HOPO multidentate bifunctional chelators in other metal-based radiopharmaceuticals are described and discussed in turn. The HOPO metal-based radiopharmaceuticals that have shown good prospects in clinical and preclinical studies are gallium-68, thorium-227 and zirconium-89 radiopharmaceuticals. We expect HOPO multidentate bifunctional chelators to be a very promising platform for building novel targeted radiometal-based diagnostic and therapeutic radiopharmaceuticals.

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Production and Supply of α-Particle–Emitting Radionuclides for Targeted α-Therapy

Cited by 81 publications

References 62 publications

Joint EANM, SNMMI and IAEA enabling guide: how to set up a theranostics centre

Joint EANM, SNMMI and IAEA enabling guide: how to set up a theranostics centre

Radiolabeled PSMA Inhibitors

Hydroxypyridinones as a Very Promising Platform for Targeted Diagnostic and Therapeutic Radiopharmaceuticals

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