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UM-ERD-4001
- Development stage
- Preclinical
- Lead developer
- Proteovant 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
UM-ERD-4001 is a preclinical-stage, orally bioavailable proteolysis-targeting chimera (PROTAC) designed to degrade estrogen receptor alpha (ERα). Developed by the University of Michigan in collaboration with Proteovant Therapeutics, UM-ERD-4001 utilizes a cereblon (CRBN) E3 ligase ligand connected via an optimized linker to an estrogen receptor ligand. It achieves sub-nanomolar DC50 values for ER degradation and has demonstrated robust oral bioavailability and in vivo efficacy, effectively reducing both wild-type and mutated ERα proteins and inducing tumor regression in breast cancer models.
- Other names
- ERD-4001ERD4001ERD 4001
02
Targets
CRBN (Cereblon)ESR1 (ERα)
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