Data from AZD9496: An Oral Estrogen Receptor Inhibitor That Blocks the Growth of ER-Positive and <i>ESR1</i>-Mutant Breast Tumors in Preclinical Models
Abstract:<div>Abstract<p>Fulvestrant is an estrogen receptor (ER) antagonist administered to breast cancer patients by monthly intramuscular injection. Given its present limitations of dosing and route of administration, a more flexible orally available compound has been sought to pursue the potential benefits of this drug in patients with advanced metastatic disease. Here we report the identification and characterization of AZD9496, a nonsteroidal small-molecule inhibitor of ERα, which is a potent and sele… Show more
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