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PRT3789
- Development stage
- Phase 1
- Lead developer
- Prelude Therapeutics
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous
01
Overview
PRT3789 is a first-in-class, highly selective proteolysis-targeting chimera (PROTAC) designed to degrade SMARCA2 protein. It is being developed as an antineoplastic agent for the treatment of advanced or metastatic solid tumors harboring SMARCA4 mutations. The drug works by binding to both SMARCA2 and an E3 ubiquitin ligase, leading to targeted ubiquitination and subsequent proteasomal degradation of SMARCA2. This mechanism exploits synthetic lethality in cancers with loss-of-function mutations in the related gene SMARCA4, which are associated with poor prognosis and limited treatment options. Early clinical data show promising anti-tumor activity—particularly in non-small cell lung cancer (NSCLC) and esophageal cancer—with a favorable safety profile observed so far in Phase 1 trials[1][6][8][10].
- Other names
- SMARCA2 degrader PRT3789SMARCA-2 degrader PRT3789SMARCA 2 degrader PRT3789
02
Targets
SMARCA2 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily A member 2)
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