Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C30H38N2O2 |
| Molecular Weight | 458.6349 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
[H][C@]1(CCC2=CC(O)=CC=C2C1)C3=C(C=C(OC)C=C3)N(CC)CC4=CC=C(CCNCC)C=C4
InChI
InChIKey=SIFNOOUKXBRGGB-AREMUKBSSA-N
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
| Molecular Formula | C30H38N2O2 |
| Molecular Weight | 458.6349 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
Elacestrant (ER-306323 or RAD 1901 [6R)-6-(2-(N-(4-(2-(ethylamino)ethyl)benzyl)-N-ethylamino)-4-methoxyphenyl)-5,6,7,8-tetrahydronaphthalen-2-ol dihydrochloride]) is a selective estrogen receptor (ER) degrader. Elacestrant induces the degradation of ER, inhibits ER-mediated signaling and growth of ER+ breast cancer cell lines in vitro and in vivo, and significantly inhibits tumor growth in breast cancer xenograft models. Elacestrant has the potential for use as a single agent or in combination with other therapies for the treatment of breast cancer. Elacestrant is being developed by Radius Health, for the treatment of estrogen receptor positive breast cancer.
Originator
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:42:51 UTC 2023
by
admin
on
Sat Dec 16 09:42:51 UTC 2023
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| Record UNII |
FM6A2627A8
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| Record Status |
Validated (UNII)
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| Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C1821
Created by
admin on Sat Dec 16 09:42:51 UTC 2023 , Edited by admin on Sat Dec 16 09:42:51 UTC 2023
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| Code System | Code | Type | Description | ||
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GH-120
Created by
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RAD-1901
Created by
admin on Sat Dec 16 09:42:51 UTC 2023 , Edited by admin on Sat Dec 16 09:42:51 UTC 2023
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PRIMARY | Study to Evaluate the Safety and Efficacy of RAD1901 in Postmenopausal Women With Moderate to Severe Vasomotor Symptoms | ||
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C120211
Created by
admin on Sat Dec 16 09:42:51 UTC 2023 , Edited by admin on Sat Dec 16 09:42:51 UTC 2023
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RAD-1901
Created by
admin on Sat Dec 16 09:42:51 UTC 2023 , Edited by admin on Sat Dec 16 09:42:51 UTC 2023
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PRIMARY | Description: RAD1901 is an orally available, selective estrogen receptor degrader (SERD) and selective estrogen receptor modulator (SERM), with potential antineoplastic and estrogen-like activities. Upon oral administration of higher doses of RAD1901, this agent acts as a SERD, which binds to the estrogen receptor (ER) and induces a conformational change that results in the degradation of the receptor. This may inhibit the growth and survival of ER-expressing cancer cells. At lower doses of this agent, RAD1901 acts as a SERM and has estrogen-like effects in certain tissues, which can both reduce hot flashes and protect against bone loss. In addition, RAD1901 is able to cross the blood-brain barrier (BBB). (last updated: 5/19/2016).Synonym: RAD1901, RAD-1901, RAD 1901, RAD1901 HCl salt. | ||
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CHEMBL3545015
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100000170507
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SUB184531
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722533-56-4
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DTXSID901045846
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FM6A2627A8
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DB06374
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FM6A2627A8
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23642301
Created by
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Elacestrant
Created by
admin on Sat Dec 16 09:42:51 UTC 2023 , Edited by admin on Sat Dec 16 09:42:51 UTC 2023
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10247
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admin on Sat Dec 16 09:42:51 UTC 2023 , Edited by admin on Sat Dec 16 09:42:51 UTC 2023
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| Related Record | Type | Details | ||
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TARGET->INHIBITOR, RECEPTOR DEGRADER |
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SALT/SOLVATE -> PARENT |
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| Related Record | Type | Details | ||
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ACTIVE MOIETY |
Class: Osteoporosis therapy, Small molecule, Tetra-hydro-naphthalene; Mechanism of Action: Selective estrogen receptor degraders, Selective estrogen receptor modulator; Highest Development Phases: Phase II for Vasomotor symptoms, Phase I for Breast cancer; Most Recent Events: 08 Feb 2016 Radius, in collaboration with Novartis, plan a clinical trial for RAD 1901 in combination with LEE 011 in the treatment of Breast cancer, 27 Jan 2016 Radius Health and Novartis enter into a clinical collaboration to evaluate combination regimens, RAD 1901 and ricociclib, for the treatment of Breast cancer, 01 Dec 2015 Phase-II clinical trials in Vasomotor symptoms in USA (PO) (NCT02653417)
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