High-yielding, automated production of 3′-deoxy-3′-[18F]fluorothymidine using a modified Bioscan Coincidence FDG reaction module

• Published in: Applied radiation and isotopes Vol. 97; pp. 47 - 51
• Main Authors: Cheung, Yiu-Yin, Nickels, Michael L., McKinley, Eliot T., Buck, Jason R., Manning, H. Charles
• Format: Journal Article
• Language: English
• Published: England Elsevier Ltd 01.03.2015
• Subjects: [18F]FLT; Animals; Automated radiosynthesis; Colorectal Neoplasms - diagnostic imaging; Dideoxynucleosides - chemical synthesis; Dideoxynucleosides - standards; HCT116 Cells; Heterografts; Humans; Mice; Mice, Nude; Positron emission tomography (PET); Positron-Emission Tomography - methods; Quality Control; Radiochemistry - instrumentation; Radiochemistry - methods; Radiopharmaceuticals - chemical synthesis; Radiopharmaceuticals - standards; Solid-phase extraction (SPE); Solid-phase extraction (SPE); Automated radiosynthesis; Positron emission tomography (PET); [18F]FLT; [F]FLT
• ISSN: 0969-8043; 1872-9800
• DOI: 10.1016/j.apradiso.2014.11.011

High-yielding, automated production of a PET tracer that reflects proliferation, 3′-deoxy-3′-[18F]fluorothymidine ([18F]FLT), is reported using a modified Bioscan Coincidence FDG reaction module. Production of [18F]FLT was implemented through: (1) modification of an original FDG manifold; (2) application of an alternate time sequence; and (3) altered solid-phase extraction (SPE) purification. Quality control testing, including standard radiochemical figures of merit and preclinical positron emission tomography (PET) imaging, was carried out. High decay-corrected yields of [18F]FLT (16–39%) were reproducibly obtained. The product exhibited very high specific activity (4586.9TBq/mmol; 123,969Ci/mmol) and radiochemical purity (>99%). Overall, the [18F]FLT produced in this manner was superior to typical productions that utilized a GE TRACERlab FXF-N reaction module. Additionally, purification with SPE cartridges, followed by manual elution, accelerated overall run time and resulted in a two-fold increase in [18F]FLT concentration. PET imaging showed the [18F]FLT produced by this method was highly suitable for non-invasive tumor imaging in mice. The Bioscan Coincidence GE FDG Reaction Module was readily adapted to reproducibly provide [18F]FLT in high yield, specific activity, and radiochemical purity. The approach was suitable to provide sufficient amounts of material for preclinical studies. [Display omitted] •Synthesis of [18F]FLT using a modified Bioscan Coincidence GE FDG reaction module.•Typical decay-corrected yields of 16–39% were obtained (n=12).•Very high specific activities and radiochemical purity.•High, preferential uptake of [18F]FLT uptake in human colon cancer xenografts.