Borofalan
chemical compound
Borofalan (also known as borofalan(10B)) is a boron-containing pharmaceutical compound used as a boron carrier in boron neutron capture therapy (BNCT) for the treatment of cancer. It is a boronic acid derivative of phenylalanine enriched with the isotope boron-10. Borofalan has been approved in Japan for the treatment of unresectable, locally advanced, or locally recurrent head and neck cancer.
Medical uses
Borofalan is used in BNCT for patients with recurrent or locally advanced head and neck cancer, including squamous-cell carcinoma and non-squamous-cell carcinoma. It is administered as an intravenous infusion over 2 hours, followed by neutron irradiation. In the open-label phase II clinical trial JHN002, borofalan was evaluated in combination with a cyclotron-based epithermal neutron source for recurrent or locally advanced head and neck cancer. Post-marketing surveillance in Japan conducted nationwide after approval confirmed the safety and efficacy of BNCT with borofalan in patients with locally advanced or recurrent head and neck cancer in a real-world setting.
Mechanism of action
Due to its structural similarity to phenylalanine, it is preferentially taken up by cancer cells via amino acid transporters. Borofalan then acts as a radiation sensitizer by delivering boron-10 to tumor cells, where it captures thermal neutrons during BNCT, leading to the production of high-energy alpha particles and lithium-7 nuclei that cause localized cell death.
History
Borofalan was developed by Stella Pharma Corporation.
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