FASTlab Radiosynthesis of the F-labelled HER2-binding Affibody molecule [ F]GE-226.

J Labelled Comp Radiopharm

Pharmaceutical Diagnostics, GE Healthcare, Chalfont St. Giles, Buckinghamshire, UK.

Published: December 2019

An 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 with [ 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, [ 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.

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http://dx.doi.org/10.1002/jlcr.3789DOI Listing

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