molecules of the month


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

Structure of full antagonist and efficient degrader of ERα, 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.

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