Simplified and robust one-step radiosynthesis of [18 F]DCFPyL via direct radiofluorination and cartridge-based purification

Mark H Dornan; José-Mathieu Simard; Antoine Leblond; Daniel Juneau; Guila Delouya; Fred Saad; Cynthia Ménard; Jean N DaSilva

doi:10.1002/jlcr.3632

Simplified and robust one-step radiosynthesis of [¹⁸ F]DCFPyL via direct radiofluorination and cartridge-based purification

J Labelled Comp Radiopharm. 2018 May 2. doi: 10.1002/jlcr.3632. Online ahead of print.

Authors

Mark H Dornan^{1

2}, José-Mathieu Simard¹, Antoine Leblond^{1

2}, Daniel Juneau^{1

2}, Guila Delouya^{1

2}, Fred Saad^{1

3}, Cynthia Ménard^{1

2}, Jean N DaSilva^{1

2}

Affiliations

¹ Centre de Recherche du Centre Hospitalier de l'Université de Montréal, Montréal, Québec, Canada.
² Département de Radiologie, Radio-oncologie et Médecine Nucléaire, Université de Montréal, Montréal, Québec, Canada.
³ Département de Chirurgie, Service d'urologie, Centre Hospitalier de l'Université de Montréal, Montréal, Québec, Canada.

PMID: 29722070
DOI: 10.1002/jlcr.3632

Abstract

[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. Radiolabeling reaction optimization studies revealed an inverse correlation between the amount of precursor used and the radiochemical yield. 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 ± 0.23 Ci of [¹⁸ F]DCFPyL at EOS (n = 7) in high molar activity (37 933 ± 4158 mCi/μmol, 1403 ± 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% radiochemical yield, at EOS, n = 3).

Keywords: HPLC-free purification; PET imaging of prostate cancer; automated production; prostate-specific membrane antigen (PSMA) ligand; protection-free radiolabeling.