elacestrant 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
estrogen antagonists, including estrogen receptor down-regulators 5710 722533-56-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • elacestrant
  • elacestrant dihydrochloride
  • orserdu
  • RAD1901
Elacestrant is an estrogen receptor antagonist that binds to estrogen receptor-alpha (ERalfa). In ER-positive (ER+) HER2-negative (HER2-) breast cancer cells, elacestrant inhibited 17beta-estradiol mediated cell proliferation at concentrations inducing degradation of ERalfa protein mediated through proteasomal pathway. Elacestrant demonstrated in vitro and in vivo antitumor activity including in ER+ HER2- breast cancer models resistant to fulvestrant and cyclin-dependent kinase 4/6 inhibitors and those harboring estrogen receptor 1 gene (ESR1) mutations.
  • Molecular weight: 458.65
  • Formula: C30H38N2O2
  • CLOGP:
  • LIPINSKI: 1
  • HAC: 4
  • HDO: 2
  • TPSA: 44.73
  • ALOGS:
  • ROTB: 10
  • Status: OFP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Jan. 27, 2023 FDA STEMLINE THERAPEUTICS INC

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
FDA MoA N0000000145 Estrogen Receptor Antagonists
FDA EPC N0000175582 Estrogen Receptor Antagonist
FDA MoA N0000185503 P-Glycoprotein Inhibitors
FDA MoA N0000190113 Breast Cancer Resistance Protein Inhibitors

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Estrogen receptor positive advanced or metastatic breast cancer indication 254837009 DOID:1612
HER2-negative advanced or metastatic breast cancer indication 254837009 DOID:1612
ESR1-mutated advanced or metastatic breast cancer indication 254837009 DOID:1612




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 345MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 8399520 Dec. 25, 2023 TREATMENT OF AN ER-POSITIVE BREAST CANCER
EQ 86MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 8399520 Dec. 25, 2023 TREATMENT OF AN ER-POSITIVE BREAST CANCER
EQ 345MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 7612114 Aug. 18, 2026 TREATMENT OF AN ER-POSITIVE BREAST CANCER
EQ 86MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 7612114 Aug. 18, 2026 TREATMENT OF AN ER-POSITIVE BREAST CANCER
EQ 345MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 10071066 Oct. 10, 2034 TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY
EQ 345MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 10420734 Oct. 10, 2034 TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY
EQ 86MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 10071066 Oct. 10, 2034 TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY
EQ 86MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 10420734 Oct. 10, 2034 TREATMENT OF AN ER-POSITIVE BREAST CANCER FOLLOWING AT LEAST ONE LINE OF ENDOCRINE THERAPY
EQ 345MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 10745343 Jan. 5, 2038 TREATMENT OF AN ER-POSITIVE BREAST CANCER
EQ 86MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL 10745343 Jan. 5, 2038 TREATMENT OF AN ER-POSITIVE BREAST CANCER

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 345MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL Jan. 27, 2028 NEW CHEMICAL ENTITY
EQ 86MG BASE ORSERDU STEMLINE THERAP N217639 Jan. 27, 2023 RX TABLET ORAL Jan. 27, 2028 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Estrogen receptor Nuclear hormone receptor ANTAGONIST IC50 7.32 DRUG LABEL DRUG LABEL
Estrogen receptor beta Nuclear hormone receptor ANTAGONIST IC50 6.06 DRUG LABEL

External reference:

IDSource
CHEMBL4297509 ChEMBL_ID
C000626176 MESH_SUPPLEMENTAL_RECORD_UI
C000626184 MESH_SUPPLEMENTAL_RECORD_UI
12339 IUPHAR_LIGAND_ID
DB06374 DRUGBANK_ID
019283 NDDF
019284 NDDF
4042013 VANDF
C4682404 UMLSCUI
I0V PDB_CHEM_ID
CHEMBL4594273 ChEMBL_ID
10247 INN_ID
23642301 PUBCHEM_CID
2628469 RXNORM
D11671 KEGG_DRUG
FM6A2627A8 UNII
364875 MMSL
41206 MMSL
d09981 MMSL

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ORSERDU HUMAN PRESCRIPTION DRUG LABEL 1 72187-0101 TABLET, FILM COATED 86 mg ORAL NDA 27 sections
ORSERDU HUMAN PRESCRIPTION DRUG LABEL 1 72187-0102 TABLET, FILM COATED 345 mg ORAL NDA 27 sections