oral selective ER degrader and antagonist
in Ph. IIb studies for ER+ breast cancer
from ligand-based design and opt.
J. Med. Chem., Sep. 29, 2020
AstraZeneca, Cambridge, UK / Waltham, MA
AZD9833 is a potent, orally available selective estrogen receptor degrader (SERD) and antagonist in development for breast cancer. The only approved SERD is the widely used fulvestrant, which is given by monthly intramuscular injection and may have submaximal antitumor activity. A safe, oral alternative has been highly sought after and the oncology community looks forward to clinical efficacy data from the AZD team.