Monovalent Degraders Focused on High Unmet Medical Needs
Programs
- Discovery
- Lead Optimization
- IND-Enabling
- Phase 1
Indication
SMARCA4-Deficient solid tumors
Rights
Wholly Owned
Overview
SMARCA2 and SMARCA4 are mutually exclusive components of the chromatin remodeling BAF complex, which regulates gene expression. Functional genomic screens in cancer cell lines have shown a synthetic lethal relationship between SMARCA2 and SMARCA4. SMARCA4 loss of function (LOF) mutations occur in 5-7% of all human cancers. SMARCA4-deficient cancer cells are highly dependent on SMARCA2 for survival. We have designed novel, selective, orally bioavailable monovalent direct degraders of SMARCA2 that utilize a tissue-restricted E3 ligase and demonstrate synthetic lethality in SMARCA4 LOF cancer cell lines.
Indication
ER+, Her2- Breast Cancer; CCNE1amp tumor types
Rights
Wholly Owned
Overview
Cyclin E regulates cell cycle progression by binding and activating CDK2. Amplification or overexpression of cyclin E is associated with poor survival in select solid tumors and as a resistance mechanism to CDK4/6 inhibitors in HR positive breast cancer patients. As a result, CDK2 is an attractive target for treating patients with tumors driven by CCNE1-amplification or overexpression. We have applied our knowledge of redirecting the E3 ligase substrate receptor cereblon to design potent, highly selective and orally bioavailable CDK2 molecular glue degraders.
Indication
Undisclosed
Rights
Wholly Owned
Overview
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