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ARID1B degrader
- Development stage
- Preclinical
- Lead developer
- Foghorn Therapeutics
- 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
Foghorn Therapeutics is developing a first-in-class selective ARID1B protein degrader for the treatment of cancers harboring ARID1A mutations. ARID1A is a frequently mutated subunit of the BAF (SWI/SNF) chromatin remodeling complex; its loss creates a specific synthetic lethal dependency on its paralog, ARID1B. This program utilizes bifunctional small molecule degraders (PROTACs) that recruit E3 ubiquitin ligases, such as VHL or Cereblon, to selectively target ARID1B for proteasomal degradation. The program is currently in preclinical development, with potential applications in a variety of ARID1A-deficient solid tumors, including endometrial, gastric, bladder, and non-small cell lung cancers. As of late 2025, the program is advancing toward in vivo proof of concept expected in 2026.
- Other names
- ARID1B protein degraderARID-1B protein degraderARID 1B protein degrader
02
Targets
ARID1B (AT-rich interactive domain-containing protein 1A)CRBN (Cereblon)VHL (Von Hippel–Lindau tumor suppressor protein)
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