Drug intelligence / Profile preview

boronotyrosine

Development stage
Preclinical
Lead developer
TAE Life Sciences
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Intravenous
01

Overview

Boronotyrosine (BTS), also known as 3-borono-l-tyrosine, is a novel borylated amino acid analogue developed to enhance the efficacy of boron neutron capture therapy (BNCT), a binary cancer treatment that relies on the selective accumulation of ^10B in tumor cells followed by irradiation with neutrons. BTS demonstrates significantly improved characteristics over the historical BNCT drug 4-borono-l-phenylalanine (BPA), including up to four times greater cellular uptake and increased retention within tumor cells. Its uptake is mediated by the l-type amino acid transporter-1 (LAT1) but shows less sensitivity to competition from natural amino acids compared to BPA. BTS can be administered at higher doses, resulting in two-to-three times greater boron delivery in vivo, faster blood clearance, and superior tumor-to-blood ratios. These properties make it a promising candidate for improving modern BNCT interventions[1][2][3][5].

Other names
3-borono-l-tyrosine
02

Targets

SLC7A5 (Large neutral amino acid transporter small subunit 1)

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