Camizestrant (AZD9833) is an orally available and selective estrogen receptor (ER) antagonist with antineoplastic activity.
AZD9833 is demonstrated to be a highly potent selective estrogen receptor degraders (SERD) that shows a pharmacological profile comparable to fulvestrant in its ability to degrade ERα in both MCF-7 and CAMA-1 cell lines.[2]
A stringent control of lipophilicity ensures that AZD9833 has favorable physicochemical and preclinical pharmacokinetic properties for oral administration. AZD9833 is potent in vivo activity in mouse xenograft models.[2]
[1] Bernard Christophe Barlaam, et al. US20180111931A1. [2] James S Scott, et al. J Med Chem. 2020 Dec 10;63(23):14530-14559.