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Radiochimica Acta

International Journal for chemical aspects of nuclear science and technology

Ed. by Qaim, Syed M.

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Simplified, automated synthesis of 3′[18F]fluoro-3′-deoxy-thymidine ([18F]FLT) and simple method for metabolite analysis in plasma

G. Reischl / Achim Blocher / Rongqing Wei / Walter Ehrlichmann / Matthias Kuntzsch / Christoph Solbach / Bernhard M. Dohmen / Hans-Jürgen Machulla

Citation Information: Radiochimica Acta. Volume 94, Issue 8/2006, Pages 447–451, ISSN (Print) 0033-8230, DOI: 10.1524/ract.2006.94.8.447, September 2009

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3′[18F]Fluoro-3′-deoxy-thymidine ([18F]FLT) (III) has been discussed to be a promising tracer for assessing tumor proliferation. In order to perform clinical studies for evaluating [18F]FLT a simplified labeling procedure was developed using 2,3′-anhydrothymidine with benzoyl as a protecting group in the 5′-position (I). In DMSO the labeling yield was 46% at 160 °C in 10 min. Hydrolysis was efficiently performed with 0.25% NaOH at room temperature within 10 min. The labeling procedure was transferred to a remote controlled synthesis module allowing the production of [18F]FLT in high activities. The overall radiochemical yield was 18.1 ± 5.4% (n = 55) with absolute yields of 9.2 ± 2.6 GBq of [18F]FLT at EOS ready for injection (60 min after EOB; irradiation parameters: 35 μA, 60 min) and specific activities of 100–220 GBq/μmol. A convenient cartridge method for metabolite analysis was developed and validated versus HPLC showing that after 90 min 69.0 ± 7.0% of the radioactivity in plasma (less than 20% of initial radioactivity) was unchanged [18F]FLT (26 patients with various tumors).

Keywords: [18F]FLT; PET; Tumor proliferation; Anhydrothymidine; Metabolite analysis

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