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] Menarini Group and Radius Health Announce Global License Agreement[4] for the Development and Commercialization of Elacestrant.

Elacestrant
Clinical data
Other namesRAD-1901, ER-306323
Routes of
administration		Oral
Identifiers
IUPAC name
  • (6R)-6-{2-[Ethyl({4-[2-(ethylamino)ethyl]phenyl}methyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
Chemical and physical data
FormulaC30H38N2O2
Molar mass458.646 g·mol−1
3D model (JSmol)
SMILES
  • CCNCCC1=CC=C(C=C1)CN(CC)C2=C(C=CC(=C2)OC)C3CCC4=C(C3)C=CC(=C4)O
InChI
  • InChI=1S/C30H38N2O2/c1-4-31-17-16-22-6-8-23(9-7-22)21-32(5-2)30-20-28(34-3)14-15-29(30)26-11-10-25-19-27(33)13-12-24(25)18-26/h6-9,12-15,19-20,26,31,33H,4-5,10-11,16-18,21H2,1-3H3/t26-/m1/s1
  • Key:SIFNOOUKXBRGGB-AREMUKBSSA-N

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). [5] Sep 24, 2020, Radius Health & Menarini Group Provide Elacestrant Update.[6] October 20, 2021, Menarini Group and Radius Health[7] announce positive phase 3 topline results[8] from the EMERALD trial evaluating elacestrant in breast cancer.

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. Inc, Radius Health (2020-07-23). "Menarini Group and Radius Health Announce Global License Agreement for the Development and Commercialization of Elacestrant". GlobeNewswire News Room. Retrieved 2021-10-20.
  5. "Radius Health Announces Third Quarter 2019 Results and Corporate Update". Radius Health, Inc. Retrieved 2020-01-03.
  6. "Radius Health & Menarini Group Provide Elacestrant Update". BioSpace. Retrieved 2021-10-20.
  7. "Menarini Group and Radius Health Announce Positive Phase 3 Topline Results from the EMERALD Trial Evaluating Elacestrant in Breast Cancer". finance.yahoo.com. Retrieved 2021-10-20.
  8. "Menarini Group and Radius Health (RDUS) Announce Positive Phase 3 Topline Results from the EMERALD Trial Evaluating Elacestrant in Breast Cancer". StreetInsider.com. Retrieved 2021-10-20.
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