Drug intelligence / Profile preview

elacestrant

Development stage
Approved
Lead developer
Stemline Therapeutics
Modality
Molecular Glues → Targeted Protein Degraders (TPDs) → Small Molecules
Administration
Oral
01

Overview

Elacestrant is a non-steroidal small molecule oral selective estrogen receptor degrader (SERD) used to treat estrogen receptor (ER)-positive, human epidermal growth factor receptor 2 (HER2)-negative, ESR1-mutated advanced or metastatic breast cancer in adults who have experienced disease progression following at least one line of endocrine therapy. It works by binding to the estrogen receptor alpha (ERα), blocking its activity and promoting its degradation via the proteasomal pathway. This dual action inhibits estradiol-mediated cell proliferation and disrupts downstream signaling essential for tumor growth. Elacestrant was approved by the FDA in January 2023 and subsequently in the EU for this indication[3][4][6][8].

Brand names
Orserdu
Other names
elacestrantRAD1901RAD-1901RAD 1901Orserdu
02

Targets

ESR1 (ERα)

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