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In boron neutron capture therapy ( BNCT ),  10 B‐4‐borono‐L‐phenylalanine ( BPA ) is commonly used as a  10 B carrier.  PET  using 4‐borono‐2‐ 18 F‐fluoro‐phenylalanine ( 18 F‐ FBPA PET ) has been performed to estimate boron concentration and predict the therapeutic effects of  BNCT ; however, the association between tumor uptake of  18 F‐ FBPA  and boron concentration in tumors remains unclear. The present study investigated the transport mechanism of  18 F‐ FBPA  and  BPA , and evaluated the utility of  18 F‐ FBPA PET  in predicting boron concentration in tumors. The transporter assay revealed that 2‐aminobicyclo‐(2.2.1)‐heptane‐2‐carboxylic acid, an inhibitor of the L‐type amino acid transporter, significantly inhibited  18 F‐ FBPA  and  14 C‐4‐borono‐L‐phenylalanine ( 14 C‐ BPA ) uptake in FaDu and  LN ‐229 human cancer cells.  18 F‐ FBPA  uptake strongly correlated with  14 C‐ BPA  uptake in 7 human tumor cell lines ( r  = .93;  P  < .01).  PET  experiments demonstrated that tumor uptake of  18 F‐ FBPA  was independent of the administration method, and uptake of  18 F‐ FBPA  by bolus injection correlated well with  BPA  uptake by continuous intravenous infusion. The results of this study revealed that evaluating tumor uptake of  18 F‐ FBPA  by  PET  was useful for estimating  10 B concentration in tumors.

Non‐invasive estimation of 10 B‐4‐borono‐L‐phenylalanine‐derived boron concentration in tumors by PET using 4‐borono‐2‐ 18 F‐fluoro‐phenylalanine