Elacestrant

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Elacestrant
Elacestrant.svg
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 mass458.63492 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.[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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References[edit]

  1. ^ http://www.who.int/medicines/publications/druginformation/LP_115.pdf
  2. ^ a b http://adisinsight.springer.com/drugs/800027755
  3. ^ a b c d 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.
  4. ^ a b c d 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.
  5. ^ a b 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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