Authors:
H.-J. Machulla Universitätsklinikum Tübingen Sektion Radiopharmazie, PET-Zentrum Röntgenweg 15 72076 Tübingen Germany

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A. Blocher Universitätsklinikum Tübingen Sektion Radiopharmazie, PET-Zentrum Röntgenweg 15 72076 Tübingen Germany

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M. Kuntzsch Universitätsklinikum Tübingen Sektion Radiopharmazie, PET-Zentrum Röntgenweg 15 72076 Tübingen Germany

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M. Piert Universitätsklinikum Tübingen Abteilung für Allgemeine Chirurgie Röntgenweg 15 72076 Tübingen Germany

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R. Wei Universitätsklinikum Tübingen Sektion Radiopharmazie, PET-Zentrum Röntgenweg 15 72076 Tübingen Germany

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J.R. Grierson University of Washington Department of Radiology, Division of Nuclear Medicine Seattle WA 98195 USA

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Abstract  

[18F]FLT (3-deoxy-3-[18F]fluorothymidine) turned out to be a tracer particularly suitable for PET imaging of tumor proliferation because of lacking degradation in vivo. To facilitate clinical studies with [18F]FLT, we investigated two new easily accessible precursors, 2,3-anhydrothymidine (AThy) and 5-O-(4,4-dimethoxytriphenylmethyl)-2,3-anhydrothymidine (DMTThy), using a common approach for introducing the label with nucleophilic [18F]fluoride. Radiochemical yields were determined in dependence on substrate concentration, reaction time and temperature. In the case of AThy (10 mg), best FLT yields were 5.3%±1.2 (130 °C, 30 min). Labeling of DMTThy (10 mg) gave 14.3%±3.3 at 160 °C within 10 minutes. Starting with an aqueous solution of 20 GBq [18F]fluoride the new method allows to produce 1.3 GBq [18F]FLT within 90 minutes ready for intravenous injection. The new labeling procedures allow [18F]FLT synthesis without lengthy preparation of the precursor and with high reproducibility mandatory for clinical application.

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Journal of Radionalytical and Nuclear Chemistry
Language English
Size A4
Year of
Foundation
1968
Volumes
per Year
1
Issues
per Year
12
Founder Akadémiai Kiadó
Founder's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
Publisher Akadémiai Kiadó
Springer Nature Switzerland AG
Publisher's
Address
H-1117 Budapest, Hungary 1516 Budapest, PO Box 245.
CH-6330 Cham, Switzerland Gewerbestrasse 11.
Responsible
Publisher
Chief Executive Officer, Akadémiai Kiadó
ISSN 0236-5731 (Print)
ISSN 1588-2780 (Online)