Elacestrant

Elacestrant is a non-steroidal small molecule and an estrogen receptor (ER) antagonist. In January 2023, it was approved by the FDA for the treatment of ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer. Elacestrant binds to estrogen receptor-alpha (ERα) and acts as a selective estrogen receptor degrader (SERD) thanks to its ability to block the transcriptional activity of the ER and promote its degradation. Other types of endocrine therapy, such as selective estrogen receptor modulators (SERMs) and aromatase inhibitors (AIs), may lead to drug resistance over time; therefore, the use of a SERD represents a therapeutic approach for the treatment of endocrine-resistant breast cancers. Unlike fulvestrant, another FDA-approved SERD, elacestrant is orally bioavailable.

Elacestrant is indicated for the treatment of postmenopausal women or adult men with ER-positive, HER2-negative, ESR1-mutated advanced or metastatic breast cancer with disease progression following at least one line of endocrine therapy.