PSMA-GCK01: a generator-based 99mTc/188Re theranostic ligand for the prostate-specific membrane antigen
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 us...
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| Hauptverfasser: | , , , , , |
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| Dokumenttyp: | Article (Journal) |
| Sprache: | Englisch |
| Veröffentlicht: |
July 1, 2023
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| In: |
Journal of nuclear medicine
Year: 2023, Jahrgang: 64, Heft: 7, Pages: 1069-1075 |
| ISSN: | 2159-662X |
| DOI: | 10.2967/jnumed.122.264944 |
| Online-Zugang: | Verlag, kostenfrei, Volltext: https://doi.org/10.2967/jnumed.122.264944 Verlag, kostenfrei, Volltext: https://jnm.snmjournals.org/content/64/7/1069 
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| Verfasserangaben: | Jens Cardinale, Frederik L. Giesel, Christina Wensky, Hendrik G. Rathke, Uwe Haberkorn, and Clemens Kratochwil |
MARC
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| 245 | 1 | 0 | |a PSMA-GCK01: a generator-based 99mTc/188Re theranostic ligand for the prostate-specific membrane antigen |c Jens Cardinale, Frederik L. Giesel, Christina Wensky, Hendrik G. Rathke, Uwe Haberkorn, and Clemens Kratochwil |
| 246 | 3 | 3 | |a PSMA-GCK01: a generator-based 99m Tc/ 188 Re theranostic ligand for the prostate-specific membrane antigen |
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| 500 | |a Online veröffentlicht: 9. Februar 2023 | ||
| 500 | |a Published online Feb. 9, 2023 | ||
| 500 | |a Gesehen am 31.10.2023 | ||
| 520 | |a 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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