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
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…