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HRS-5350
- Development stage
- Unknown
- Lead developer
- Hengrui 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
HRS-5350 is an orally bioavailable proteolysis-targeting chimera (PROTAC) degrader developed by Jiangsu Hengrui Pharmaceuticals and co-developed by Bristol Myers Squibb (BMS) as part of a significant strategic partnership established in 2024. The drug is designed to target the androgen receptor (AR), a key driver in the progression of prostate cancer. As a PROTAC, HRS-5350 functions by recruiting an E3 ubiquitin ligase to the androgen receptor, facilitating its polyubiquitination and subsequent degradation by the 26S proteasome. This mechanism of action aims to achieve complete depletion of the target protein, potentially overcoming resistance mechanisms associated with traditional androgen receptor antagonists. It is currently being evaluated in early-stage clinical trials for the treatment of metastatic castration-resistant prostate cancer (mCRPC).
02
Targets
AR (Adrenergic receptors)CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)
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