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gridegalutamide
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- 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
**Gridegalutamide** is an oral, heterobifunctional androgen receptor ligand-directed degrader and competitive androgen receptor antagonist developed by Bristol Myers Squibb for prostate cancer. It recruits cereblon to drive ubiquitination and proteasomal degradation of wild-type and clinically relevant mutant androgen receptor while also competitively antagonizing residual androgen receptor signaling through the receptor ligand-binding domain. The asset is being evaluated in the phase 3 rechARge trial for metastatic castration-resistant prostate cancer and in a phase 2 neoadjuvant study with degarelix for high-risk localized prostate cancer before radical prostatectomy. ([pubchem.ncbi.nlm.nih.gov](https://pubchem.ncbi.nlm.nih.gov/compound/Gridegalutamide))
- Other names
- rechARge
02
Targets
AR (Adrenergic receptors)CRBN (Cereblon)
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