Drug intelligence / Profile preview

GSK5471713

Development stage
Phase 2
Lead developer
GSK
Modality
PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
Administration
Oral
01

Overview

GSK5471713 is an investigational androgen receptor (AR) degrader being developed by GSK for the treatment of metastatic castration-resistant prostate cancer (mCRPC). As a targeted protein degrader, it is designed to facilitate the elimination of the AR protein, a primary driver of prostate cancer progression, potentially overcoming resistance mechanisms that limit the effectiveness of traditional androgen receptor pathway inhibitors (ARPI) and taxanes. The compound is currently being evaluated in an open-label Phase 1/2 first-in-human clinical trial (NCT07335198) as a monotherapy to assess its safety, tolerability, pharmacokinetics, and preliminary efficacy, including PSA50 response and objective response rates, in patients with heavily pre-treated advanced disease.

02

Targets

AR (Adrenergic receptors)

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