estetrol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| estrogens | 5450 | 15183-37-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
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.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| 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:
| Source | Code | Description |
|---|---|---|
| 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 | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent 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 strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 3MG;14.2MG | NEXTSTELLIS | MAYNE PHARMA | N214154 | April 15, 2021 | RX | TABLET | ORAL | April 15, 2026 | NEW CHEMICAL ENTITY |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA 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:
| ID | Source |
|---|---|
| D11513 | KEGG_DRUG |
| 2055649-81-3 | SECONDARY_CAS_RN |
| 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 |
| 018700 | NDDF |
| 1179488005 | SNOMEDCT_US |
| 1179489002 | SNOMEDCT_US |
| 1269193003 | SNOMEDCT_US |
| 4040424 | VANDF |
| 10439 | INN_ID |
| 2539031 | RXNORM |
| 345375 | MMSL |
| 39469 | MMSL |
| d09730 | MMSL |
| ENB39R14VF | UNII |
Pharmaceutical products:
None