Clinical Application of 18F-AlF-NOTA-Octreotide PET/CT in Combination With 18F-FDG PET/CT for Imaging Neuroendocrine Neoplasms

Abstract

Objectives The study is to evaluate biodistribution, dosimetry, safety, and clinical usefulness of 18F-AlF-NOTA-octreotide (18F-OC) PET/CT in combination with 18F-FDG PET/CT for detection of neuroendocrine neoplasms (NENs). Methods The biodistribution, dosimetry, and safety of 18F-OC were evaluated in 3 healthy volunteers. Twenty-two NEN patients underwent PET/CT at 60 minutes after intravenous injection of 3.7 to 4.44 MBq (0.1–0.12 mCi) per kilogram of body weight of 18F-OC. This was followed by 18F-FDG PET/CT within a 2-week period. Results 18F-OC was well tolerated by all healthy volunteers and NEN patients. The calculated effective dose of 18F-OC was 0.023 ± 0.002 mSv/MBq. In NEN patients, we observed prominent 18F-OC tumor uptake and high tumor-to-background ratios. Tumor uptake of 18F-OC was greater than that of 18F-FDG, and this was particularly evident in G2 NENs (median SUVmax, 45.6 vs 4.3; P < 0.015). Tumor uptake of 18F-OC or 18F-FDG was significantly correlated with tumor differentiation (P < 0.05). Dual tracer PET/CT detected more lesions and also yielded information on the biological status of tumors. Conclusions The tracer 18F-OC exhibited favorable safety and dosimetry profiles. 18F-OC provided superior imaging of well-differentiated NENs and significantly higher tumor-to-background ratio compared with 18F-FDG. Combining 18F-FDG with 18F-OC PET/CT has the potential to improve NEN staging and management of patient treatment.

Radiolabelled Peptides for Positron Emission Tomography and Endoradiotherapy in Oncology

“…A set of alternative labelling strategies including the introduction of aluminium mono-[ 18 F]fluoride cations ([ 18 F]AlF 2+ ), labelling of SiFA by 19 F- 18 F isotopic exchange reactions (IEX), and 1-step 19 F- 18 F IEX on trifluoroborates such as trialkylammoniomethyl-BF 3 are currently being evaluated (for a review, see [138]). Initial clinical trials with 18 F-AlF-NOTA-octreotide [48] and 18 F-SiFAlin-TATE [139] most recently published indicate promising data. Further studies will demonstrate if these compounds might replace the established 68 Ga-labelled octreotide derivatives.…”

“…Critical might be the stability of the complexes. However, initial clinical data with RGD-peptides [46,47] and octreotide derivatives [48] demonstrated good delineation of the tumours with low activity in the bone (see also below).…”

[68Ga]Ga-DOTA-TOC: The First FDA-Approved 68Ga-Radiopharmaceutical for PET Imaging

“…Some of these tracers are currently in early clinical trials, e.g., [ 18 F]FET-βAG-TOCA [54], which shows promising imaging results, but its complicated production is a drawback. Another tracer, [ 18 F]AlF-NOTA-octreotide, which was first developed by Laverman et al [55] and shows promising imaging results [56,57], may overcome the problems of a complicated radiosynthesis. For this tracer, an automated two-step GMP-compliant synthesis was recently published [58].…”

The battle on time, money and precision: Da[18F] id vs. [68Ga]liath

“…This comparison confirmed a high in vitro binding affinity of [ 18 F]AIF-NOTA-octreotide towards SSTR2 [ 18 , 19 ]. In 2019, the first clinical experience with [ 18 F]AIF-NOTA-octreotide in 22 NET patients was reported showing that the tracer displays a favourable biodistribution and provides an excellent detection of tumoural lesions with a high tumour-to-background ratio; however, there was no comparison with a [ 68 Ga]-labelled SSA [ 20 ]. It took almost 10 years until an automated GMP compliant production of [ 18 F]AIF-NOTA-octreotide was published and a GMP grade precursor became commercially available [ 21 ].…”