Routes of
administration Oral CAS Number 722533-56-4 ChemSpider 57583807 Molar mass 458.6349 g/mol | Synonyms RAD-1901, ER-306323 PubChem CID 23642301 UNII FM6A2627A8 Route Oral administration | |
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Elacestrant (INN) (developmental code names RAD-1901, ER-306323) is a non-steroidal combined selective estrogen receptor modulator (SERM) and selective estrogen receptor degrader (SERD) (described as a "SERM/SERD hybrid (SSH)") that was discovered by Eisai and is under development by Radius Health and Takeda for the treatment of menopausal vasomotor symptoms (hot flashes) and estrogen receptor (ER)-positive advanced breast cancer, as well as endometrial cancer and kidney cancer. As of September 2016, it is in phase II clinical trials for vasomotor symptoms and breast cancer. Elavestrant has dose-dependent, tissue-selective estrogenic and antiestrogenic activities, with biphasic weak partial agonist activity at the ER at low doses and antagonist activity at higher doses. It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues. Unlike the SERD fulvestrant, elacestrant is able to readily cross the blood-brain-barrier into the central nervous system, where it can target breast cancer metastases in the brain, and is orally bioavailable and does not require intramuscular injection.