Elacestrant

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 estrogen receptor (ER)-positive advanced breast cancer.[1] 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.[2] It shows agonistic activity on bone and antagonistic activity on breast and uterine tissues.[3] 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,[2][3] and is orally bioavailable and does not require intramuscular injection.[2][3]

Elacestrant
Clinical data
Other namesRAD-1901, ER-306323
Routes of
administration		Oral
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC30H38N2O2
Molar mass458.646 g·mol−1
3D model (JSmol)

Clinical Development

As of December 2019, it is in phase III trials for breast cancer.[1] However, in December 2019 Radius Health announced plans to divest of oncology assets (including elacestrant). [4]

See also

References
  1. Clinical trial number NCT03778931 for "Phase 3 Trial of Elacestrant vs. Standard of Care for the Treatment of Patients With ER+/HER2- Advanced Breast Cancer" at ClinicalTrials.gov
  2. Wardell SE, Nelson ER, Chao CA, Alley HM, McDonnell DP (October 2015). "Evaluation of the pharmacological activities of RAD1901, a selective estrogen receptor degrader". Endocrine-Related Cancer. 22 (5): 713–24. doi:10.1530/ERC-15-0287. PMC 4545300. PMID 26162914.
  3. Garner F, Shomali M, Paquin D, Lyttle CR, Hattersley G (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): 948–56. doi:10.1097/CAD.0000000000000271. PMC 4560273. PMID 26164151.
  4. "Radius Health Announces Third Quarter 2019 Results and Corporate Update". Radius Health, Inc. Retrieved 2020-01-03.
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