General
Preferred name
Elacestrant
Synonyms
RAD1901 dihydrochloride ()
RAD1901 ()
RAD-1901 ()
Elacestrant (dihydrochloride) ()
Elacestrant (RAD1901) Dihydrochloride ()
Elacestrant dihydrochloride ()
ELACESTRANT HYDROCHLORIDE ()
ER-306323 ()
Orserdu ()
RAD-1901 DIHYDROCHLORIDE ()
RAD1901 hydrochloride ()
Elacestrant (hydrochloride) ()
P&D ID
PD094617
CAS
722533-56-4
1349723-93-8
Tags
available
drug
Approved by
FDA
First approval
2023
Drug indication
Breast cancer
Hot flashes
breast neoplasm
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Elacestrant is an orally bioactive, selective, non-steroidal dual estrogen receptor degrader (SERD)/selective estrogen receptor modulator (SERM; with antagonist action) . It was developed primarily for antineoplastic potential (via its SERD action at high concentrations) . It has also demonstrated potential to treat the vasomotor symptoms of the menopause with estrogen-like effects detected at low concentrations (SERM activity), but the pharmacology in this setting is very complex . Elacestrant crosses the blood-brain barrier, so is predicted to provide efficacy against breast cancer metastases in the brain. (GtoPdb)
MOA RAD1901 is a novel selective estrogen receptor modulator(SERM). SERMs are small molecules that bind to and selectively modulate estrogen receptors. These molecules have the ability to stimulate or block estrogen's activity in different types of tissue, functioning as estrogen receptor agonists in some tissues and as estrogen receptor antagonists in others.; RAD1901 has potential to reduce vasomotor symptoms, along with a simultaneous bone-protective effect, without stimulating breast or uterine tissues. RAD1901 is distinctive from other SERMs in its unique biological profile, combined with its significant ability to penetrate the blood-brain barrier, which enables RAD1901 to function as an estrogen agonist within the central nervous system and thereby relieve hot flashes.;
DESCRIPTION Elacestrant (RAD1901) is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ER¦Á and ER¦Â, respectively. Elacestrant also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo[1][2].
PRICE 472
DESCRIPTION Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ER?? and ER??, respectively.Elacestrant ?is an orally available selective estrogen receptor degrader .
DESCRIPTION Elacestrant (RAD1901) dihydrochloride is an orally available and selective estrogen receptor degrader (SERD) with IC50s of 48 and 870 nM for ER¦Á and ER¦Â, respectively. Elacestrant dihydrochloride also can inhibit growth of ER+ breast cancer cell lines in vitro and in vivo[1][2].
PRICE 407
DESCRIPTION Elacestrant dihydrochloride (DA-DKRAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader with IC50s of 48 for ER?? and 870 nM for ER??, respectively.
DESCRIPTION Elacestrant (RAD1901) with IC50s of 48 and 870 nM for ERα and ERβ, respectively.Elacestrant  is an orally available selective estrogen receptor degrader . (TargetMol Bioactive Compound Library)
DESCRIPTION Elacestrant dihydrochloride (DA-DKRAD1901 dihydrochloride) is an orally available selective estrogen receptor degrader with IC50s of 48 for ERα and 870 nM for ERβ, respectively. (TargetMol Bioactive Compound Library)
Cell lines
1
Organisms
2
Compound Sets
14
Cayman Chemical Bioactives
37298
ChEMBL Approved Drugs
CHEMBL4297509
CHEMBL4594273
ChEMBL Drugs
CHEMBL4297509
CHEMBL4594273
Drug Repurposing Hub
DrugBank
DB06374
DrugBank Approved Drugs
DB06374
DrugCentral
5710
DrugCentral Approved Drugs
5710
DrugMAP
DM8RLJ5
Guide to Pharmacology
12339
MedChem Express Bioactive Compound Library
HY-19822
HY-19822A
ReFrame library
Selleckchem Bioactive Compound Library
elacestrant
TargetMol Bioactive Compound Library
T13674
T13675
External IDs
31
Properties
(calculated by RDKit )
Molecular Weight
458.29
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
2
Rotatable Bonds
10
Ring Count
4
Aromatic Ring Count
3
cLogP
5.85
TPSA
44.73
Fraction CSP3
0.4
Chiral centers
1.0
Largest ring
6.0
QED
0.37
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
ERα
ERβ
Estrogen Receptor/ERR
Estrogen/progestogen Receptor
MOA
estrogen receptor degrader
Pathway
Vitamin D Related/Nuclear Receptor
Endocrinology/Hormones
Source data