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CC2000199

Development stage
Preclinical
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

CC2000199 (also known as CC-199) is a potent and selective androgen receptor (AR) ligand-directed degrader (LDD) developed by Bristol Myers Squibb for the treatment of metastatic castration-resistant prostate cancer (mCRPC). It utilizes a dual mechanism of action, functioning both as a direct AR antagonist and as a heterobifunctional degrader that recruits the CRL4CRBN E3 ligase complex to induce the ubiquitination and subsequent proteasomal degradation of the receptor. CC2000199 is highly potent against both wildtype and mutant forms of AR, demonstrating superior activity compared to enzalutamide in preclinical models of advanced and therapy-resistant prostate cancer. It is described as a close analog of BMS-986365.

02

Targets

CRBN (Cereblon)AR (Adrenergic receptors)

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