Preparation and Evaluation of [F]AlF-NOTA-NOC for PET Imaging of Neuroendocrine Tumors: Comparison to [Ga]Ga-DOTA/NOTA-NOC

Overview

Journal Molecules

Publisher MDPI

Specialty Biology

Date 2022 Oct 27

PMID 36296411

Authors

Johan Hygum Dam

Niels Langkjaer

Christina Baun

Birgitte Brinkmann Olsen

Aaraby Yoheswaran Nielsen

Helge Thisgaard

Affiliations

Soon will be listed here.

Abstract

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 [F]AlF-NOTA-[1-Nal]-Octreotide and compares it in vivo to DOTA- and NOTA-[1-Nal]-Octreotide radiolabeled with gallium-68.

Methods: DOTA- and NOTA-NOC were radiolabeled with gallium-68 and NOTA-NOC with [F]AlF. Biodistributions of the three radioligands were evaluated in AR42J xenografted mice at 1 h p.i and for [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 [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 [Ga]Ga-DOTA-NOC and 25.7 ± 5.8 %ID/g for [Ga]Ga-NOTA-NOC. Additionally, [F]AlF-NOTA-NOC exhibited a tumor uptake of 37.3 ± 10.5 %ID/g for [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, [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 [F]AlF-NOTA-NOC, making it possible to detect liver metastases. Therefore, [F]AlF demonstrates promise as a surrogate pseudo-radiometal to gallium-68.

Citing Articles

Evaluation of [F]AlF NOTA-5G, an Aluminum [F]fluoride Labeled Peptide Targeting the Cell Surface Receptor Integrin Alpha(v)beta(6) for PET Imaging.

Hausner S, Davis R, Ganguly T, Harris R, Sutcliffe J Mol Imaging Biol. 2025; .

PMID: 39979580 DOI: 10.1007/s11307-025-01989-3.

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