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gridegalutamide + rabeprazole

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

Overview

BMS-986365 + rabeprazole is a drug combination being evaluated in clinical pharmacology studies to understand the impact of gastric acid suppression on the pharmacokinetics of BMS-986365. BMS-986365 (gridegalutamide) is an investigational, orally bioavailable proteolysis-targeting chimera (PROTAC) that selectively targets the androgen receptor (AR) for ubiquitination and subsequent proteasomal degradation. It is being developed by Bristol Myers Squibb for the treatment of metastatic castration-resistant prostate cancer (mCRPC). Rabeprazole is a proton pump inhibitor (PPI) that suppresses gastric acid secretion by inhibiting the H+/K+-ATPase enzyme in gastric parietal cells. The combination is used in Phase 1 trials to determine if changes in stomach pH affect the absorption and bioavailability of gridegalutamide.

Other names: BMS-986365 + rabeprazole

Targets

ATP4A (Potassium–transporting ATPase alpha chain 1)CRBN (Cereblon)AR (Adrenergic receptors)

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