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ARV-2001
- 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-2001 is a Proteolysis Targeting Chimera (PROTAC) developed by Arvinas, specifically designed to target and degrade the Tau protein. Tau protein aggregation is a key pathological feature of Alzheimer's disease and other neurodegenerative disorders known as tauopathies. ARV-2001 works by recruiting an E3 ubiquitin ligase to the Tau protein, facilitating its ubiquitination and subsequent degradation by the 26S proteasome. This mechanism aims to clear both soluble and insoluble forms of pathological Tau, potentially slowing or halting disease progression. The compound is designed for oral administration and is engineered to cross the blood-brain barrier to reach its target in the central nervous system.
- Other names
- Tau PROTAC
02
Targets
MAPT (Microtubule-associated protein tau)CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)
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