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ARV-027
- Development stage
- Preclinical
- Lead developer
- Arvinas
- 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
ARV-027 is an investigational, orally administered, peripherally restricted PROTAC (proteolysis-targeting chimera) protein degrader designed to selectively target and eliminate the toxic polyglutamine-expanded androgen receptor (polyQ-AR) in skeletal muscle. Developed by Arvinas, ARV-027 is being evaluated for the treatment of spinal-bulbar muscular atrophy (SBMA), also known as Kennedy's disease, a rare X-linked neuromuscular disorder. SBMA is caused by a CAG trinucleotide repeat expansion in the androgen receptor gene, which leads to protein misfolding, aggregation, and progressive degeneration of motor neurons and muscle tissue. ARV-027 utilizes the ubiquitin-proteasome system to degrade both cytosolic and nuclear polyQ-AR. Preclinical studies have shown that ARV-027 can reduce polyQ-AR levels in muscle and improve muscle strength and endurance in animal models. Arvinas plans to initiate Phase 1 clinical trials in 2026.
- Other names
- ARV-027-Arvinas-polyQ-AR-PROTAC-SBMAARV027-Arvinas-polyQ-AR-PROTAC-SBMAARV 027-Arvinas-polyQ-AR-PROTAC-SBMA
02
Targets
CRBN (Cereblon)AR (Adrenergic receptors)
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