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AZD9496

Development stage: Phase 1
Lead developer: AstraZeneca
Modality: Small Molecules
Administration: Oral

Overview

AZD9496 is an orally available nonsteroidal small molecule that acts as a selective estrogen receptor degrader (SERD). It binds to the estrogen receptor alpha (ERα), induces a conformational change leading to degradation of the receptor and blocks ER-mediated signaling. This results in inhibition of growth and survival of ER-expressing cancer cells. Developed by AstraZeneca for the treatment of hormone receptor-positive breast cancer, it showed potent antagonist and degrader activity against ERα in preclinical models and early clinical trials. Clinical development reached phase I for advanced breast cancer but was discontinued[1][3][4][5][7].

Other names: (E)-3-(3,5-difluoro-4-((1R,3R)-2-(2-fluoro-2-methylpropyl)-3-methyl-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indol-1-yl)phenyl)acrylic acid

Targets

ESR1 (ERα)

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