Elacestrant

This drug entry is a stub and has not been fully annotated. It is scheduled to be annotated soon.

Identification

Generic Name
Elacestrant
DrugBank Accession Number
DB06374
Background

Not Available

Type
Small Molecule
Groups
Investigational
Structure
Thumb
Weight
Average: 458.646
Monoisotopic: 458.293328472
Chemical Formula
C30H38N2O2
Synonyms
  • Elacestrant
External IDs
  • ER-306323
  • RAD-1901
  • RAD1901

Pharmacology

Indication

Investigated for use/treatment in menopause and female hormonal deficiencies/abnormalities.

Pharmacology
Reduce drug development failure rates
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Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Not Available

Mechanism of action

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.

TargetActionsOrganism
UEstrogen receptor alphaNot AvailableHumans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Not Available

Metabolism
Not Available
Route of elimination

Not Available

Half-life

Not Available

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Not Available
Food Interactions
Not Available

Categories

Drug Categories
Classification
Not classified
Affected organisms
Not Available

Chemical Identifiers

UNII
FM6A2627A8
CAS number
722533-56-4
InChI Key
SIFNOOUKXBRGGB-AREMUKBSSA-N
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
IUPAC Name
(6R)-6-{2-[ethyl({4-[2-(ethylamino)ethyl]phenyl}methyl)amino]-4-methoxyphenyl}-5,6,7,8-tetrahydronaphthalen-2-ol
SMILES
CCNCCC1=CC=C(CN(CC)C2=C(C=CC(OC)=C2)[C@@H]2CCC3=CC(O)=CC=C3C2)C=C1

References

General References
Not Available
ChemSpider
57583807
BindingDB
349630
Wikipedia
Elacestrant

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
3Active Not RecruitingTreatmentBreast Cancer1
2CompletedTreatmentHot Flashes1
2TerminatedTreatmentHot Flashes / Vasomotor Symptoms Associated With Menopause1
1CompletedTreatmentAdvanced ER+, HER2-Negative Breast Cancer1
1CompletedTreatmentMetastatic Breast Cancer1
1, 2Not Yet RecruitingTreatmentBreast Cancer1
0RecruitingTreatmentBreast Cancer / Hormone Receptor Positive Breast Carcinoma1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
Not Available
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.00035 mg/mLALOGPS
logP6.54ALOGPS
logP6.23ChemAxon
logS-6.1ALOGPS
pKa (Strongest Acidic)10.58ChemAxon
pKa (Strongest Basic)9.96ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area44.73 Å2ChemAxon
Rotatable Bond Count10ChemAxon
Refractivity143.17 m3·mol-1ChemAxon
Polarizability55.16 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da

Drug created on March 19, 2008 16:28 / Updated on February 21, 2021 18:52