|Other names||RAD-1901, ER-306323|
|Chemical and physical data|
|Molar mass||458.63492 g/mol g·mol−1|
|3D model (JSmol)|
Elacestrant (INN) (developmental code names RAD-1901, ER-306323) is a nonsteroidal 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. Elacestrant 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.
- Wardell, Suzanne E.; Nelson, Erik R.; Chao, Christina A.; Alley, Holly M.; McDonnell, Donald P. (1 October 2015). "Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader". Endocrine-Related Cancer. 22 (5): 713–724. doi:10.1530/ERC-15-0287. ISSN 1479-6821. PMC 4545300. PMID 26162914.
- Garner, Fiona; Shomali, Maysoun; Paquin, Dotty; Lyttle, C. Richard; Hattersley, Gary (October 2015). "RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models". Anti-Cancer Drugs. 26 (9): 948–956. doi:10.1097/CAD.0000000000000271. ISSN 0959-4973. PMC 4560273. PMID 26164151.
- Hattersley, Gary; Harris, Alan G.; Simon, James A.; Constantine, Ginger D. (2016). "Clinical investigation of RAD1901, a novel estrogen receptor ligand, for the treatment of postmenopausal vasomotor symptoms: a phase 2 randomized, placebo-controlled, double-blind, dose-ranging, proof-of-concept trial". Menopause. doi:10.1097/gme.0000000000000726. ISSN 1072-3714. PMID 27575546.
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