About: Elacestrant

An Entity of Type: chemical substance, from Named Graph: http://dbpedia.org, within Data Space: dbpedia.org:8891

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 and Takeda for the treatment estrogen receptor (ER)-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 ta

Property	Value
dbo:abstract	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 and Takeda for the treatment estrogen receptor (ER)-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. Menarini Group and Radius Health Announce Global License Agreement for the Development and Commercialization of Elacestrant. (en)
dbo:casNumber	722533-56-4
dbo:fdaUniiCode	FM6A2627A8
dbo:kegg	D11671
dbo:pubchem	23642301
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dbo:wikiPageExternalLink	http://www.radiuspharm.com/r-d/pipeline.html http://adisinsight.springer.com/drugs/800027755
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dbp:casNumber	722533 (xsd:integer)
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dbp:kegg	D11671 (en)
dbp:n	2 (xsd:integer)
dbp:o	2 (xsd:integer)
dbp:pubchem	23642301 (xsd:integer)
dbp:routesOfAdministration	dbr:Oral_administration
dbp:smiles	CCNCCC1=CC=CCNC2=CC3CCC4=CC=CCO (en)
dbp:stdinchi	1 (xsd:integer)
dbp:stdinchikey	SIFNOOUKXBRGGB-AREMUKBSSA-N (en)
dbp:synonyms	RAD-1901, ER-306323 (en)
dbp:unii	FM6A2627A8 (en)
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rdfs:comment	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 and Takeda for the treatment estrogen receptor (ER)-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 ta (en)
rdfs:label	Elacestrant (en)
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