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Preparation and Evaluation of [(18)F]AlF-NOTA-NOC for PET Imaging of Neuroendocrine Tumors: Comparison to [(68)Ga]Ga-DOTA/NOTA-NOC
Background: The somatostatin receptors 1–5 are overexpressed on neuroendocrine neoplasms and, as such, represent a favorable target for molecular imaging. This study investigates the potential of [(18)F]AlF-NOTA-[1-Nal(3)]-Octreotide and compares it in vivo to DOTA- and NOTA-[1-Nal(3)]-Octreotide ra...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9609173/ https://www.ncbi.nlm.nih.gov/pubmed/36296411 http://dx.doi.org/10.3390/molecules27206818 |
Sumario: | Background: The somatostatin receptors 1–5 are overexpressed on neuroendocrine neoplasms and, as such, represent a favorable target for molecular imaging. This study investigates the potential of [(18)F]AlF-NOTA-[1-Nal(3)]-Octreotide and compares it in vivo to DOTA- and NOTA-[1-Nal(3)]-Octreotide radiolabeled with gallium-68. Methods: DOTA- and NOTA-NOC were radiolabeled with gallium-68 and NOTA-NOC with [(18)F]AlF. Biodistributions of the three radioligands were evaluated in AR42J xenografted mice at 1 h p.i and for [(18)F]AlF at 3 h p.i. Preclinical PET/CT was applied to confirm the general uptake pattern. Results: Gallium-68 was incorporated into DOTA- and NOTA-NOC in yields and radiochemical purities greater than 96.5%. NOTA-NOC was radiolabeled with [(18)F]AlF in yields of 38 ± 8% and radiochemical purity above 99% after purification. The biodistribution in tumor-bearing mice showed a high uptake in tumors of 26.4 ± 10.8 %ID/g for [(68)Ga]Ga-DOTA-NOC and 25.7 ± 5.8 %ID/g for [(68)Ga]Ga-NOTA-NOC. Additionally, [(18)F]AlF-NOTA-NOC exhibited a tumor uptake of 37.3 ± 10.5 %ID/g for [(18)F]AlF-NOTA-NOC, which further increased to 42.1 ± 5.3 %ID/g at 3 h p.i. Conclusions: The high tumor uptake of all radioligands was observed. However, [(18)F]AlF-NOTA-NOC surpassed the other clinically well-established radiotracers in vivo, especially at 3 h p.i. The tumor-to-blood and -liver ratios increased significantly over three hours for [(18)F]AlF-NOTA-NOC, making it possible to detect liver metastases. Therefore, [(18)F]AlF demonstrates promise as a surrogate pseudo-radiometal to gallium-68. |
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