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Journal of Nuclear Medicine

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Meeting ReportMolecular Targeting Probes - Radioactive and Nonradioactive

Optimization of 4-borono-2-[18F]fluoro-L-phenylalanine (FBPA) synthesis: PET tracer for boron neutron capture therapy (BNCT) for cancer treatment

Sadahiro Naka, Yasukazu Kanai, Hiroki Kato, Eku Shimosegawa and Jun Hatazawa
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1689;
Sadahiro Naka
1Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, Suita, Japan
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Yasukazu Kanai
2Molecular Imaging in Medicine, Osaka University Graduate School of Medicine, Suita, Japan
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Hiroki Kato
1Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, Suita, Japan
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Eku Shimosegawa
1Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, Suita, Japan
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Jun Hatazawa
1Nuclear Medicine and Tracer Kinetics, Osaka University Graduate School of Medicine, Suita, Japan
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Abstract

1689

Objectives Boron Neutron Capture Therapy (BNCT) is an anticancer treatment with alpha and Li particles produced by 10B(n, α)7Li reaction in tumors. In the BNCT, 10B-phenylalanine (BPA) is administered to deliver 10B to tumors. Before irradiation, it is very important to evaluate the amount of 10B in the tumor cells. For this purpose, PET with 4-Borono-2-[18F]fluoro-L-phenylalanine (FBPA) has been employed. In this study, we optimized the synthesis condition of [18F]FBPA with high specific radioactivity and enough radioactivity for clinical use.

Methods [18F]FBPA is synthesized by direct fluorination of BPA with [18F]CH3COOF converted from [18F]F2. We tested the concentration of carrier F2 gas (0.05 - 1.0%) and recovery gas flow rate of [18F]F2 (150 - 600 ml/min), with the deuteron irradiation at 10µA for 10 or 60 min. Then we synthesized [18F]FBPA under the optimized condition at 20µA for 150 min bombardment.

Results [18F]F2 radioactivity was approximately 300, 500 and 900 MBq with 0.05, 0.1 and 0.2% of carrier F2 gas respectively for 10 min bombardment. . By increasing F2 gas more than 0.2%, [18F]F2 radioactivity was not increased. The conversion rate to [18F]CH3COOF was approximately 35% with any concentration of F2 gas. By increasing F2 gas, specific radioactivity and recovery efficiency of [18F]FBPA became low. In the recovery gas flow rate, [18F]F2 radioactivity and the conversion rate to [18F]CH3COOF with gas flow rate of 150 ml/min were lower than that of 600 ml/min. Specific radioactivity and recovery efficiency of [18F]FBPA were not influenced by gas flow rate. The optimized method synthesized 740 MBq of [18F]FBPA at 20µA for 150 min bombardment.

Conclusions The concentration of carrier F2 gas of 0.2% and recovery gas flow rate of 600ml/min resulted in the highest [18F]FBPA production with high specific radioactivity. It became possible to test five patients per production

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Journal of Nuclear Medicine
Vol. 53, Issue supplement 1
May 2012
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Optimization of 4-borono-2-[18F]fluoro-L-phenylalanine (FBPA) synthesis: PET tracer for boron neutron capture therapy (BNCT) for cancer treatment
Sadahiro Naka, Yasukazu Kanai, Hiroki Kato, Eku Shimosegawa, Jun Hatazawa
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1689;

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Optimization of 4-borono-2-[18F]fluoro-L-phenylalanine (FBPA) synthesis: PET tracer for boron neutron capture therapy (BNCT) for cancer treatment
Sadahiro Naka, Yasukazu Kanai, Hiroki Kato, Eku Shimosegawa, Jun Hatazawa
Journal of Nuclear Medicine May 2012, 53 (supplement 1) 1689;
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