Drug intelligence / Profile preview

PSMA-boron

Development stage
Preclinical
Lead developer
Shuttle Pharmaceuticals
Modality
Small Molecules, Antibody-Radionuclide Conjugates → Antibody Conjugates → Antibody-Based Therapeutics
Administration
Intravenous
01

Overview

PSMA-boron refers to a class of boron-containing ligands or inhibitors specifically designed to target the **prostate-specific membrane antigen (PSMA)** for selective delivery of boron to PSMA-expressing prostate cancer cells as part of **boron neutron capture therapy (BNCT)**. These are typically urea-based PSMA inhibitor scaffolds conjugated with boronic acid or carborane groups to achieve high affinity binding to PSMA and optimal boron delivery. BNCT requires efficient and selective delivery of boron atoms to tumor cells, which are then exposed to a neutron beam, inducing localized cytotoxic effects via nuclear capture and fission reactions. PSMA-boron agents have demonstrated nanomolar binding activity to PSMA, significant boron uptake in prostate cancer xenografts, and promising in vivo PET imaging and biodistribution results. These molecules are under preclinical development as theranostic agents for diagnosis and targeted therapy in metastatic castration-resistant prostate cancer.

Brand names
PSMA-boron
Other names
PSMA-boron
02

Targets

PSMA (Prostate-specific membrane antigen)

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