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

Stem definitionDrug idCAS RN
estrogens 5450 15183-37-6

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • estetrol
  • nextstellis
  • estetrol anhydrous
  • estetrol monohydrate
Estetrol is a synthetic analogue of a native estrogen present during pregnancy, that is selective for nuclear estrogen receptors ERalpha and ERbeta. It is used in combination with drospirenone, a spironolactone analogue with anti-mineralocorticoid and antiandrogenic activity, (nextstellis) as oral contraceptive.
  • Molecular weight: 304.39
  • Formula: C18H24O4
  • CLOGP: 2.62
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 4
  • TPSA: 80.92
  • ALOGS: -2.34
  • ROTB: 0

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
May 19, 2021 EMA Gedeon Richter Plc; Estetra SPRL
April 15, 2021 FDA MAYNE PHARMA

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
ATC G03AA18 GENITO URINARY SYSTEM AND SEX HORMONES
SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
HORMONAL CONTRACEPTIVES FOR SYSTEMIC USE
Progestogens and estrogens, fixed combinations
MeSH PA D003270 Contraceptive Agents
MeSH PA D012102 Reproductive Control Agents
FDA CS M0447348 Estradiol Congeners
FDA MoA N0000000100 Estrogen Receptor Agonists
FDA EPC N0000175825 Estrogen
CHEBI has role CHEBI:49325 oral contraceptives
CHEBI has role CHEBI:50114 estrogens
CHEBI has role CHEBI:63951 estrogen receptor agonists
CHEBI has role CHEBI:76967 human xenobiotic metabolites
CHEBI has role CHEBI:77746 Homo sapiens metabolite

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Prevent pregnancy indication 5935008
Hepatocellular carcinoma contraindication 25370001
Acute hepatitis contraindication 37871000
Hypertensive disorder contraindication 38341003 DOID:10763
Atrial fibrillation contraindication 49436004 DOID:0060224
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Cerebrovascular disease contraindication 62914000 DOID:6713
Blood coagulation disorder contraindication 64779008 DOID:1247
Diabetes mellitus contraindication 73211009 DOID:9351
Hepatocellular adenoma contraindication 78058005
Renal impairment contraindication 236423003
Carcinoma of breast contraindication 254838004 DOID:3459
Adrenal insufficiency contraindication 386584007 DOID:10493
Venous thromboembolic disease contraindication 429098002




🐶 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
3MG;14.2MG NEXTSTELLIS MAYNE PHARMA N214154 April 15, 2021 RX TABLET ORAL 7732430 March 2, 2025 USE BY FEMALES OF REPRODUCTIVE POTENTIAL TO PREVENT PREGNANCY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
3MG;14.2MG NEXTSTELLIS MAYNE PHARMA N214154 April 15, 2021 RX TABLET ORAL April 15, 2026 NEW CHEMICAL ENTITY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Estrogen receptor Nuclear hormone receptor MODULATOR Ki 8.31 SCIENTIFIC LITERATURE DRUG LABEL
Estrogen receptor beta Nuclear hormone receptor MODULATOR Ki 7.72 SCIENTIFIC LITERATURE DRUG LABEL

External reference:

IDSource
D11513 KEGG_DRUG
C0014899 UMLSCUI
CHEBI:142773 CHEBI
4OH PDB_CHEM_ID
CHEMBL1230314 ChEMBL_ID
27125 PUBCHEM_CID
DB12235 DRUGBANK_ID
D004953 MESH_DESCRIPTOR_UI
C000718213 MESH_SUPPLEMENTAL_RECORD_UI
11591 IUPHAR_LIGAND_ID
ENB39R14VF UNII
2539031 RXNORM
345375 MMSL
39469 MMSL
d09730 MMSL
1179488005 SNOMEDCT_US
1179489002 SNOMEDCT_US
4040424 VANDF
10439 INN_ID
018700 NDDF
2055649-81-3 SECONDARY_CAS_RN

Pharmaceutical products:

None