Iveson, PB;
Glaser, M;
Indrevoll, B;
Shales, J;
Mantzilas, D;
Omtvedt, L;
Luthra, SK;
... Grigg, J; + view all
(2019)
FASTlab Radiosynthesis of the ¹⁸F-labelled HER2-binding Affibody molecule [¹⁸F]GE-226.
Journal of Labelled Compounds and Radiopharmaceuticals
, 62
(14)
pp. 925-932.
10.1002/jlcr.3789.
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Abstract
An 18F‐labelled human epidermal growth factor receptor (HER2) receptor binding radiotracer is a potential tool to non‐invasively identify HER2 positive tumour lesions in subjects with recurrent metastatic breast cancer. Having explored the manual radiochemistry to conjugate the Affibody molecule ZHER2:2891 with [18F]4‐fluorobenzaldehyde, we have developed and optimised a full protocol for the automated GE FASTlab synthesiser. Our chemometric model predicted the best radiochemical purity for a short conjugation time (2.8 minutes), a low temperature (65°C), and a medium Affibody molecule precursor amount (5.5 mg). Under these optimised conditions, [18F]GE‐226 was produced after solid‐phase extraction purification with activity yield of 30% ± 7 (n = 18) and a radiochemical purity of 94% ± 2 (n = 18). The synthesis and purification was complete after 43 minutes and provided apparent molar activities of 12 to 30 GBq/μmol (n = 12) at the end of synthesis.
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