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 [...]
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Sep. 18, 2021
GNE-149: A Monovalent Degrader and Full Antagonist of Estrogen Receptor Alpha
GNE-149
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