Drug intelligence / Profile preview

amcenestrant

Development stage
Phase 3
Lead developer
Sanofi
Modality
Small Molecules
Administration
Oral
01

Overview

Amcenestrant is an orally available, nonsteroidal selective estrogen receptor degrader (SERD), developed as a small molecule antineoplastic agent. It specifically targets and binds to the estrogen receptor (ER), inducing a conformational change that promotes ER degradation. This action blocks ER-mediated signaling pathways and inhibits the growth and survival of ER-expressing cancer cells. Amcenestrant was primarily investigated for the treatment of estrogen receptor-positive (ER+), human epidermal growth factor receptor 2-negative (HER2-) advanced or metastatic breast cancer. Clinical development included studies in both advanced/metastatic and early-stage breast cancer; however, all clinical trials were discontinued after interim analyses showed lack of efficacy compared to standard therapies[1][4][5][7].

Other names
amcenestrant5H-BENZOCYCLOHEPTENE-3-CARBOXYLIC ACID, 8-(2,4-DICHLOROPHENYL)-9-(4-(((3S)-1-(3-FLUOROPROPYL)-3-PYRROLIDINYL)OXY)PHENYL)-6,7-DIHYDRO-8-(2,4-DICHLOROPHENYL)-9-(4-(((3S)-1-(3-FLUOROPROPYL)PYRROLIDIN-3-YL)OXY)PHENYL)-6,7-DIHYDRO-5H-BENZO(7)ANNULENE-3-CARBOXYLIC ACID
02

Targets

ESR1 (ERα)

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