Drug intelligence / Profile preview

borofalan

Development stage
Phase 2
Lead developer
Stella Pharma
Modality
Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics, Small Molecules
Administration
Intravenous
01

Overview

Borofalan is a boronated derivative of phenylalanine enriched with the stable isotope boron‑10. It acts as a carrier for delivering boron to tumor cells and is used in Boron Neutron Capture Therapy (BNCT). Upon intravenous administration prior to neutron irradiation, it accumulates preferentially in tumor tissue via amino acid transporters such as LAT1. When exposed to thermal neutrons during BNCT, the ^{10}B isotope undergoes nuclear capture and fission reactions that release high-energy alpha particles and lithium nuclei locally within the tumor cell. This results in highly localized cytotoxicity with minimal damage to surrounding normal tissues. Borofalan has been developed primarily by Stella Pharma for use as an antitumor radiopharmaceutical agent and was first approved in Japan for unresectable or recurrent head and neck cancer[1][2][5][6].

Brand names
Steboronine
Other names
borofalan (10B)Boronophenylalanine B-104-(Borono-10B)-L-phenylalanineL-(p-(10B)Boronophenyl)alaninep-Boronophenylalanine (BPA)L-p-boronophenylalanineL-Phenylalanine 4-borono-L-Phenylalanine4-borono-L-Phenylalanine-4-borono-borofalanum (10B)BOROFALAN B-10 HYDROCHLORIDE
02

Targets

SLC7A5 (Large neutral amino acid transporter small subunit 1)

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