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BMS-986470
- Development stage
- Phase 2
- Lead developer
- Bristol Myers Squibb
- Modality
- Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
- Administration
- Oral
01
Overview
BMS-986470 is an investigational oral small molecule developed by Bristol Myers Squibb for the treatment of sickle cell disease. It acts as a cereblon E3 ligase modulator (CELMoD) and functions as a targeted protein degrader, specifically designed to increase fetal hemoglobin (HbF) levels. The drug works by degrading two key transcriptional repressors, WIZ and ZBTB7A, which are involved in silencing fetal hemoglobin expression. By promoting the degradation of these proteins via the cereblon E3 ubiquitin ligase complex, BMS-986470 aims to boost HbF production in red blood cells—a therapeutic strategy for ameliorating symptoms of sickle cell disease. The compound is currently being evaluated in Phase 1/2 clinical trials for safety, pharmacokinetics, pharmacodynamics, and preliminary efficacy in both healthy volunteers and patients with sickle cell disease[1][3][4][6].
- Other names
- HbF-activating CELMoD
02
Targets
ZBTB7A (Zinc finger and BTB domain-containing protein 7A)CRBN (Cereblon)
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