Drug intelligence / Profile preview

boronophenylalanine

Development stage
Phase 1
Lead developer
TAE Life Sciences
Modality
Small Molecules
Administration
Intravenous, Intra-arterial
01

Overview

Boronophenylalanine is a synthetic amino acid derivative in which a boron group is attached to the phenyl ring of phenylalanine. It acts as a boron carrier for use in Boron Neutron Capture Therapy (BNCT), an experimental form of radiotherapy primarily investigated for the treatment of malignant tumors such as glioblastoma multiforme and melanoma metastatic to the brain. The drug selectively accumulates in cancer cells via amino acid transporters, especially LAT1, which are overexpressed on many tumor types. Upon irradiation with low-energy neutrons, the boron atom undergoes nuclear capture and fission reactions that release high-energy alpha particles and lithium nuclei, causing localized cytotoxicity within cancer cells while sparing surrounding healthy tissue[1][3][5][7]. Boronophenylalanine is typically administered intravenously as a fructose complex (BPA-F) to improve solubility[7].

Brand names
Borofalan
Other names
p-boronophenylalanine4-borono-l-phenylalanineL-p-boronophenylalanineL-phenylalanine, 4-borono-(2S)-2-amino-3-(4-boronophenyl)propanoic acidpara-Boronophenylalanine
02

Targets

SLC7A5 (Large neutral amino acid transporter small subunit 1)

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