[18 F]DCFPyL is a clinical-stage PET radiotracer used to image prostate cancer. This report details the efficient production of [18 F]DCFPyL using single-step direct radiofluorination, without the use of carboxylic acid protecting groups. Radiolabelling reaction optimization studies revealed an inverse correlation between the amount of precursor used and the radiochemical yield (RCY). This simplified approach enabled automated preparation of [18 F]DCFPyL within 28 minutes using HPLC-purification (26% ± 6%, at EOS, n = 4), which was then scaled up for large-batch production to generate 1.46 Ci ± 0.23 Ci of [18 F]DCFPyL at EOS (n = 7) in high molar activity (37,933 mCi/μmol ± 4,158 mCi/μmol, 1403 GBq/μmol ± 153 GBq/μmol, at EOS, n = 7). Further, this work enabled the development of [18 F]DCFPyL production in 21 minutes using an easy cartridge-based purification (25% ± 9% RCY, at EOS, n = 3).
Journal of labelled compounds & radiopharmaceuticals. 2018 May 02 [Epub ahead of print]
Mark H Dornan, José-Mathieu Simard, Antoine Leblond, Daniel Juneau, Guila Delouya, Fred Saad, Cynthia Ménard, Jean N DaSilva
Radiochemistry and Cyclotron Laboratory, Centre de recherche du Centre hospitalier de l'Université de Montréal, Québec, Canada.