Automated production of 2-18F-fluorobutyric acid and as a PET imaging agent for prostate cancer

DONG Weixuan; QIN Kaixin; HU Wenhao; SHEN Cong; NIU Chen; DUAN Xiaoyi

Abstract：Objective To investigate the automatic synthesis process of 2-18F-fluorobutyric acid(2-18F-FBA)and its C18 column purification method,so as to meet the production requirements of Good Manufacturing Practice of Medical Products(GMP),shorten the synthesis time and improve the yield.To evaluate the PET imaging of 2-18F-FBA in nude mice with prostate tumor.Methods Based on the GE TRACERlab FX-FN module,2-18F-FBA was automatically synthesized by'one-pot method'and'column hydrolysis method',respectively.Both schemes used methyl 2-bromobutyrate as a precursor,which was fluorinated,purified and hydrolyzed to obtain 2-18F-FBA.Micro-PET/CT was performed at different time points after tail vein injection of 2-18F-FBA in nude mice bearing prostate tumor,and the PMOD software was used to outline the region of interest and calculate the maximum standardized uptake value.Results The synthesis time of 2-18F-FBA by'one-pot method'and'column hydrolysis method'was 35 min and 27 min,respectively,and the uncorrected radiochemical yield was(34±5.2)%and(41±3.7)%.Micro-PET/CT showed significant radio-concentration at the tumor at 30 min after injection of 2-18F-FBA,and the tumor/muscle ratio was relatively high at 60 min.Both schemes were able to synthesize 2-18F-FBA,with the'column hydrolysis'method having a relatively shorter synthesis time and higher yield.Conclusion The 2-18F-FBA is clearly visualized in tumor of prostate tumor bearing nude mice with a high target/non-target ratio at 60 min.