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[18F]BF3-BPA (also known as BR-02) is a next-generation PET imaging radiopharmaceutical developed as a companion diagnostic for Boron Neutron Capture Therapy (BNCT). It is a derivative of L-boronophenylalanine (BPA) that incorporates an organotrifluoroborate (BF3) moiety, allowing for rapid and efficient one-step radiolabeling via fluorine-18 (18F) isotope exchange. The compound acts as a phenylalanine mimic and is selectively internalized by tumor cells through the L-type amino acid transporter 1 (LAT1/SLC7A5), which is highly overexpressed in malignancies such as high-grade gliomas and head and neck cancers. By providing high-contrast PET visualization and precise quantification of boron accumulation in vivo, [18F]BF3-BPA facilitates accurate tumor-to-normal tissue ratio assessments and dosimetry planning for BNCT. This approach overcomes the significant synthesis complexity and low yields associated with traditional boron-targeting tracers like [18F]FBPA.
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