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An improved automated radiosynthesis of [F-18]FET-beta AG-TOCA

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Title: An improved automated radiosynthesis of [F-18]FET-beta AG-TOCA
Authors: Allott, L
Barnes, C
Brickute, D
Aboagye, EO
Item Type: Journal Article
Abstract: The fluorine-18 radiolabelled octreotide derivative [18F]FET-βAG-TOCA targeting somatostatin receptor type 2, has been evaluated clinically for positron emission tomography (PET) imaging of neuroendocrine tumours (NETs). We report an improved automated radiosynthesis of [18F]FET-βAG-TOCA with several advantages over the current automated GMP synthesis: 1) cartridge-based purification of 2-[18F]fluoroethylazide ([18F]FEA); 2) simple set-up for the radiolabelling on a single cassette; 3) HPLC purification using a biocompatible mobile phase. [18F]FET-βAG-TOCA was produced with a radiochemical yield of 16.7 ± 0.6% (non-decay corrected) and radiochemical purity ≥98%. The automated synthesis produced multi-patient doses (900 MBq) that were radiochemically stable (≥98%) over 4 hours. In addition, the automated procedure described can be used, with minimal adaptation, to radiolabel any alkyne-containing peptide with [18F]FEA using the GE FASTlab™ platform.
Issue Date: 1-Mar-2019
Date of Acceptance: 11-Dec-2018
URI: http://hdl.handle.net/10044/1/72963
DOI: https://dx.doi.org/10.1039/c8re00279g
ISSN: 2058-9883
Publisher: Royal Society of Chemistry
Start Page: 569
End Page: 574
Journal / Book Title: Reaction Chemistry and Engineering
Volume: 4
Issue: 3
Copyright Statement: © The Royal Society of Chemistry 2019.
Sponsor/Funder: Medical Research Council (MRC)
Medical Research Council (MRC)
Funder's Grant Number: MR/J007986/1
MR/N020782/1
Keywords: Science & Technology
Physical Sciences
Technology
Chemistry, Multidisciplinary
Engineering, Chemical
Chemistry
Engineering
PRECLINICAL EVALUATION
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Science & Technology
Physical Sciences
Technology
Chemistry, Multidisciplinary
Engineering, Chemical
Chemistry
Engineering
PRECLINICAL EVALUATION
CLICK
AZIDE
Publication Status: Published
Embargo Date: 2019-12-11
Online Publication Date: 2018-12-11
Appears in Collections:Division of Surgery
Division of Cancer



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