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FASTlab Radiosynthesis of the 18 F‐labelled HER2‐binding Affibody molecule [ 18 F]GE‐226
Author(s) -
Iveson Peter B.,
Glaser Matthias,
Indrevoll Bard,
Shales Jonathan,
Mantzilas Dimitrios,
Omtvedt Lone,
Luthra Sajinder K.,
Hiscock Duncan,
Grigg Julian
Publication year - 2019
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.3789
Subject(s) - radiosynthesis , chemistry , conjugate , yield (engineering) , molecule , radiochemistry , molar ratio , extraction (chemistry) , nuclear chemistry , stereochemistry , chromatography , nuclear medicine , organic chemistry , positron emission tomography , catalysis , medicine , mathematical analysis , materials science , mathematics , metallurgy
Abstruct An 18 F‐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 Z HER2:2891 with [ 18 F]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, [ 18 F]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.