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| Verfasst von: | Cardinale, Jens [VerfasserIn]  |
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| | Giesel, Frederik L. [VerfasserIn] |
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| | Wensky, Christina [VerfasserIn] |
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| | Rathke, Hendrik [VerfasserIn] |
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| | Haberkorn, Uwe [VerfasserIn] |
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| | Kratochwil, Clemens [VerfasserIn] |
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| Titel: | PSMA-GCK01: a generator-based 99mTc/188Re theranostic ligand for the prostate-specific membrane antigen |
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| Verf.angabe: | Jens Cardinale, Frederik L. Giesel, Christina Wensky, Hendrik G. Rathke, Uwe Haberkorn, and Clemens Kratochwil |
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| E-Jahr: | 2023 |
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| Jahr: | July 1, 2023 |
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| Umfang: | 7 S. |
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| Fussnoten: | Im Titel ist "99m" und "188" jeweils hochgestellt ; Online veröffentlicht: 9. Februar 2023 ; Published online Feb. 9, 2023 ; Gesehen am 31.10.2023 |
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| Titel Quelle: | Enthalten in: Journal of nuclear medicine |
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| Ort Quelle: | New York, NY : Soc., 1964 |
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| Jahr Quelle: | 2023 |
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| Band/Heft Quelle: | 64(2023), 7 vom: Juli, Seite 1069-1075 |
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| ISSN Quelle: | 2159-662X |
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| | 1535-5667 |
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| Abstract: | Prostate-specific membrane antigen (PSMA) theranostics have been introduced with 68Ga and 177Lu, the most used radionuclides. However, 188Re is a well-known generator-based therapeutic nuclide that completes a theranostic tandem with 99mTc and may offer an interesting alternative to the currently used radionuclides. In the present work, we aimed at the development of a PSMA-targeted 99mTc/188Re theranostic tandem. Methods: The ligand HYNIC-iPSMA was chosen as the lead structure. Its HYNIC chelator has limitations for 188Re labeling and was replaced by mercaptoacetyltriserine to obtain PSMA-GCK01, a precursor for stable 99mTc and 188Re labeling. 99mTc-PSMA-GCK01 was used for in vitro evaluation of the ligand and comparison with 99mTc-EDDA/HYNIC-iPSMA. Planar imaging using 99mTc-PSMA-GCK01 and organ biodistribution with 188Re-PSMA-GCK01 were performed using LNCaP tumor-bearing mice. Finally, the theranostic tandem was applied for imaging and therapy in 3 prostate cancer patients in compassionate care. Results: Efficient radiolabeling of PSMA-GCK01 with both radionuclides was demonstrated. Cell-based assays with 99mTc-PSMA-GCK01 versus 99mTc-EDDA/HYNIC-iPSMA revealed comparable uptake characteristics. Planar imaging and organ distribution revealed good tumor uptake of both 99mTc-PSMA-GCK01 and 188Re-PSMA-GCK01 at 1 and 3 h after injection, with low uptake in nontarget organs. In patients, similar distribution patterns were observed for 99mTc-PSMA-GCK01 and 188Re-PSMA-GCK01 and in comparison with 177Lu-PSMA-617. Conclusion: The ligand PSMA-GCK01 labels stably with 99mTc and 188Re, both generator-based radionuclides, and thus provides access to on-demand labeling at reasonable costs. Preclinical evaluation of the compounds revealed favorable characteristics of the PSMA-targeted theranostic tandem. This result was confirmed by successful translation into first-in-humans application. |
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| DOI: | doi:10.2967/jnumed.122.264944 |
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| URL: | Bitte beachten Sie: Dies ist ein Bibliographieeintrag. Ein Volltextzugriff für Mitglieder der Universität besteht hier nur, falls für die entsprechende Zeitschrift/den entsprechenden Sammelband ein Abonnement besteht oder es sich um einen OpenAccess-Titel handelt.
kostenfrei: Volltext: https://doi.org/10.2967/jnumed.122.264944 |
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| | kostenfrei: Volltext: https://jnm.snmjournals.org/content/64/7/1069 |
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| | DOI: https://doi.org/10.2967/jnumed.122.264944 |
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| Datenträger: | Online-Ressource |
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| Sprache: | eng |
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| Sach-SW: | 188Re |
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| | 99mTc |
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| | PSMA |
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| | SPECT |
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| | theranostic |
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| K10plus-PPN: | 1868881784 |
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| Verknüpfungen: | → Zeitschrift |
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PSMA-GCK01: a generator-based 99mTc/188Re theranostic ligand for the prostate-specific membrane antigen / Cardinale, Jens [VerfasserIn]; July 1, 2023 (Online-Ressource)
