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BMS-986365

Development stage
Phase 3
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

BMS-986365 (also known as CC-94676) is an orally administered, selective, and highly potent androgen receptor (AR) degrader developed for the treatment of metastatic castration-resistant prostate cancer (mCRPC)[2][3][4]. It acts via a first-in-class dual mechanism as both an AR antagonist and a ligand-directed degrader, promoting AR degradation through cereblon E3 ligase-dependent proteolysis[2][3]. This dual action inhibits AR signaling and suppresses tumor growth in prostate cancer models[2][4]. Clinical studies have shown that BMS-986365 demonstrates anti-tumor activity in heavily pretreated mCRPC patients—including those with resistance to current androgen receptor pathway inhibitors—regardless of AR ligand binding domain mutation status[2][6]. The drug is currently being evaluated in phase 3 clinical trials for efficacy and safety compared to standard-of-care therapies such as abiraterone plus prednisone/prednisolone, enzalutamide, or docetaxel plus prednisone/prednisolone[1][7].

Other names
gridegalutamide
02

Targets

AR (Adrenergic receptors)

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