monovalent degrader + full antagonist of ER_
orally efficacious in xenograft model
from ligand-based design of full antag.
ACS Med. Chem. Lett., May 29, 2020
Genentech, South San Francisco, CA
GNE-149
1 min read
GNE-149 is an efficient monovalent degrader and full antagonist of estrogen receptor alpha with significant oral bioavailability in higher species. The standard-of-care selective ER degrader (SERD) fulvestrant is not orally bioavailable and is believed to achieve incomplete target occupancy in humans. The full antagonist profile of GNE-149 is desirable to avoid the associated risk of further developing endometrial cancer in breast cancer patients.
Search By Structure
- eFT226 (zotatifin)
- JNJ-54717793
- DS-1971a
- BMS-986235/LAR-1219
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- [18F]LSN3316612
- RO7185876
- ONO-8430506
- “Compound 15”
- NLG802
- āCompound 6gā
- GSK232
- LEI401
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