Elacestrant

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Elacestrant
Elacestrant.svg
Clinical data
Synonyms RAD-1901, ER-306323
Routes of
administration
Oral
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
Chemical and physical data
Formula C30H38N2O2
Molar mass 458.63492 g/mol
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.[1][2][3][4][5] As of September 2016, it is in phase II clinical trials for vasomotor symptoms and breast cancer.[2][5] 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.[3] It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues.[4] 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,[3][4] and is orally bioavailable and does not require intramuscular injection.[3][4]

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