Fully automated synthesis and coupling of 18FFBEM to glutathione using the iPHASE FlexLab module

摘要

Site-specific radiolabelling of peptides or antibodies using 18FFBEM is often preferred over non-site-specific radiolabelling with 18FSFB because it does not affect the affinity of the antibody to its target. Unfortunately, the synthesis of 18FFBEM and its conjugation to thiol containing macromolecules requires some manual intervention, which leads to radiation exposure of the radiochemist. In this publication, we report on the complete automation of 18FFBEM production and its subsequent conjugation to glutathione using a slightly modified iPHASE FlexLab module. 18FFBEM was produced in 1.185?±?0.168?GBq (15–20; n?=?10; 0.75?±?0.106?GBq non-decay corrected) with a specific activity of 57?±?10?GBq/μmol. Radiochemical purity was 97?±?1 and the synthesis time including HPLC purification and reformulation was 70?min. After evaporation to dryness, 18FFBEM was conjugated to glutathione in PBS buffer pH?7.4 in quantitative yields. This fully automated method does not require any manual intervention and therefore reduces the radiation exposure to the operator.