Drug intelligence / Profile preview

UT-69

Development stage
Preclinical
Lead developer
University of Tennessee Research Foundation
Modality
Small Molecules
01

Overview

UT-69 is an experimental small-molecule selective androgen receptor degrader (SARD) that functions as a next-generation androgen receptor (AR) antagonist for the treatment of castration-resistant prostate cancer. It binds both the amino-terminal activation domain (AF-1) and the carboxy-terminal ligand-binding domain of the androgen receptor, antagonizing AR signaling and promoting degradation of both full-length AR and constitutively active splice variants such as AR-V7 at nanomolar concentrations. By degrading AR protein and inhibiting AR N–C terminal interaction, UT-69 suppresses AR transcriptional activity and downregulates AR target genes, including in enzalutamide-resistant models, positioning it as a potential therapeutic strategy to overcome resistance to current AR-targeted therapies.

02

Targets

AR-V7 (Androgen Receptor Variant 7)AR (Adrenergic receptors)

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