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EGFR PROTAC (Hangzhou Polymed Biopharmaceuticals)
- Development stage
- Preclinical
- Lead developer
- Hangzhou Polymed Biopharmaceuticals
- Modality
- PROTACs (E3 ligase recruitment) → Targeted Protein Degraders (TPDs) → Small Molecules, Bivalent/Multivalent Binders → Multivalent & Scaffold-Based Small Molecules → Small Molecules
01
Overview
EGFR PROTAC (Hangzhou Polymed Biopharmaceuticals) is a small molecule proteolysis-targeting chimera (PROTAC) being developed for the treatment of non-small cell lung carcinoma (NSCLC). Developed by Hangzhou Polymed Biopharmaceuticals, the drug is designed to overcome resistance to third-generation EGFR inhibitors by inducing the degradation of EGFR proteins, including those with the C797S mutation (e.g., del19/Thr790Met/Cys797Ser and Leu858Arg/Thr790Met/Cys797Ser triple mutants). The molecule functions by recruiting the cereblon (CRBN) E3 ubiquitin ligase to the target EGFR protein, leading to its ubiquitination and subsequent degradation by the proteasome. As of early 2024, the program is in the IND-enabling stage with plans to be IND-ready in early 2025.
02
Targets
CRBN (Cereblon)Epidermal growth factor receptor (EGFR) Leu858Arg/Thr790Met/Cys797SerEGFR T790M (Epidermal growth factor receptor T790M mutant)Epidermal growth factor receptor (EGFR) with exon 19 deletion, Thr790Met, and Cys797Ser mutations
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