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CDK4-targeted protein degrader
- Development stage
- Preclinical
- Lead developer
- Blueprint Medicines
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
This asset is a preclinical-stage targeted protein degrader (TPD) being developed by Blueprint Medicines. It is designed to selectively induce the degradation of Cyclin-dependent kinase 4 (CDK4), a key protein involved in cell cycle regulation that is frequently overactive in various cancers. By utilizing the cell's natural protein disposal system to eliminate CDK4, this therapeutic approach aims to provide more comprehensive inhibition of the signaling pathway compared to traditional small molecule inhibitors. The program is currently focused on the treatment of hormone receptor-positive (HR+), human epidermal growth factor receptor 2-negative (HER2-) breast cancer, where CDK4/6 inhibition is a standard of care but resistance remains a significant clinical challenge.
- Other names
- CDK4 degraderCDK-4 degraderCDK 4 degrader
02
Targets
CDK6 (Cyclin-dependent kinase 6)CRL4-CRBN (Cereblon-based E3 ubiquitin ligase complex)CDK4 (Cyclin-dependent kinase 4)
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