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SMARCA2 Degrader Program
- Development stage
- Preclinical
- Lead developer
- Amphista Therapeutics
- Modality
- Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
Amphista Therapeutics is developing a series of small molecule Targeted Glue degraders designed to selectively target SMARCA2 for proteasomal degradation. Utilizing the proprietary Eclipsys platform, these molecules recruit the DCAF16 E3 ligase to induce the degradation of SMARCA2 with high selectivity over its close homolog SMARCA4. This program specifically focuses on treating lung cancer, particularly cases with central nervous system (CNS) metastasis, as the compounds have demonstrated significant CNS penetration in preclinical models. Preclinical data indicates these glues can achieve >95% degradation of SMARCA2 within four hours.
- Other names
- SMARCA2 Targeted GlueSMARCA-2 Targeted GlueSMARCA 2 Targeted GlueSMARCA2-DCAF16 Targeted GlueSMARCA-2-DCAF16 Targeted GlueSMARCA 2-DCAF16 Targeted Glue
02
Targets
DCAF16 (DDB1- and CUL4-associated factor 16)SMARCA2 (SWI/SNF related, matrix associated, actin dependent regulator of chromatin subfamily A member 2)
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