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Issue 3, 2019
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An improved automated radiosynthesis of [18F]FET-βAG-TOCA

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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.

Graphical abstract: An improved automated radiosynthesis of [18F]FET-βAG-TOCA

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Supplementary files

Article information

29 Oct 2018
11 Dec 2018
First published
11 Dec 2018

React. Chem. Eng., 2019,4, 569-574
Article type

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

L. Allott, C. Barnes, D. Brickute and E. O. Aboagye, React. Chem. Eng., 2019, 4, 569
DOI: 10.1039/C8RE00279G

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