Elacestrant
Elacestrant is a nonsteroidal combined selective estrogen receptor modulator and selective estrogen receptor degrader that was discovered by Eisai and is under development by Radius Health and Takeda for the treatment estrogen receptor -positive advanced 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.As of December 2019, it is in phase III trials for breast cancer. However, in December 2019 Radius Health announced plans to divest of oncology assets.
