Drug intelligence / Profile preview

BTS(OMe)

Development stage
Preclinical
Modality
Small Molecules
Administration
Intravenous
01

Overview

BTS(OMe) is a **borylated tyrosine amino acid derivative** designed for use as a boron carrier in boron neutron capture therapy (BNCT) and proton boron fusion therapy (PBFT) for cancer treatment. It is a novel compound that incorporates a methoxy group into the borylated tyrosine structure, resulting in improved aqueous solubility relative to existing boron carriers such as boronophenylalanine (BPA), and may allow for higher dosing and enhanced delivery of boron to tumor cells. Its mechanism relies on **cellular uptake via the upregulated large neutral amino acid transporter 1 (LAT-1, SLC7A5)**, common in various human cancers. BTS(OMe) is synthesized from L-tyrosine using a series of protection, borylation, and methylation steps, and tested for uptake and selectivity in cell lines and tumor xenograft models. Its anticipated use is as a boron delivery agent for neutron or proton therapies in oncology, particularly where LAT-1 is upregulated[1].

02

Targets

SLC7A5 (Large neutral amino acid transporter small subunit 1)

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