ospemifene 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives | 4749 | 128607-22-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
an estrogen agonist/antagonist with tissue selective effects, its biological actions are mediated through binding to estrogen receptors, this binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism)
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Nov. 20, 2014 | EMA | Shionogi Limited | |
| Feb. 26, 2013 | FDA | SHIONOGI INC |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hot flush | 291.95 | 39.22 | 87 | 1252 | 44082 | 50559703 |
| Vaginal discharge | 193.03 | 39.22 | 41 | 1298 | 5199 | 50598586 |
| Labelled drug-drug interaction medication error | 185.07 | 39.22 | 45 | 1294 | 10432 | 50593353 |
| No adverse event | 121.48 | 39.22 | 42 | 1297 | 33536 | 50570249 |
| Vaginal haemorrhage | 113.71 | 39.22 | 37 | 1302 | 24514 | 50579271 |
| Muscle spasms | 106.56 | 39.22 | 56 | 1283 | 125497 | 50478288 |
| Therapeutic response unexpected | 98.73 | 39.22 | 30 | 1309 | 15885 | 50587900 |
| Vulvovaginal burning sensation | 73.04 | 39.22 | 15 | 1324 | 1600 | 50602185 |
| Vulvovaginal discomfort | 63.94 | 39.22 | 14 | 1325 | 2027 | 50601758 |
| Off label use | 58.89 | 39.22 | 67 | 1272 | 474359 | 50129426 |
| Inability to afford medication | 56.40 | 39.22 | 12 | 1327 | 1518 | 50602267 |
| Vulvovaginal pruritus | 50.55 | 39.22 | 12 | 1327 | 2484 | 50601301 |
| Hyperhidrosis | 48.85 | 39.22 | 30 | 1309 | 89396 | 50514389 |
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Hot flush | 232.15 | 47.29 | 65 | 915 | 46170 | 64451582 |
| Vaginal discharge | 144.20 | 47.29 | 28 | 952 | 3969 | 64493783 |
| Labelled drug-drug interaction medication error | 105.62 | 47.29 | 30 | 950 | 22032 | 64475720 |
| Muscle spasms | 92.03 | 47.29 | 44 | 936 | 140979 | 64356773 |
| Vaginal haemorrhage | 91.18 | 47.29 | 26 | 954 | 19318 | 64478434 |
| Therapeutic response unexpected | 76.28 | 47.29 | 22 | 958 | 16979 | 64480773 |
| No adverse event | 65.04 | 47.29 | 22 | 958 | 28539 | 64469213 |
| Vulvovaginal discomfort | 62.86 | 47.29 | 12 | 968 | 1543 | 64496209 |
| Vulvovaginal burning sensation | 53.32 | 47.29 | 10 | 970 | 1169 | 64496583 |
| Off label use | 48.07 | 47.29 | 53 | 927 | 632753 | 63864999 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | G03XC05 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM Selective estrogen receptor modulators |
| FDA MoA | N0000000168 | Selective Estrogen Receptor Modulators |
| FDA EPC | N0000175826 | Estrogen Agonist/Antagonist |
| CHEBI has role | CHEBI:35610 | antineoplastic agents |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agents |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dyspareunia | indication | 71315007 |
🐶 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9566252 | Nov. 2, 2022 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8470890 | Feb. 13, 2024 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8470890 | Feb. 13, 2024 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8470890 | Feb. 13, 2024 | TREATMENT OF VAGINAL SYMPTOMS OF UROGENITAL ATROPHY BY ORALLY ADMINISTERING OSPEMIFENE WITH FOOD TO ENHANCE BIOAVAILABILITY OF OSPEMIFENE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8772353 | Feb. 13, 2024 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8772353 | Feb. 13, 2024 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8772353 | Feb. 13, 2024 | TREATMENT OF VAGINAL SYMPTOMS OF UROGENITAL ATROPHY BY ORALLY ADMINISTERING OSPEMIFENE WITH FOOD TO ENHANCE BIOAVAILABILITY OF OSPEMIFENE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9241915 | Feb. 13, 2024 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9241915 | Feb. 13, 2024 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9241915 | Feb. 13, 2024 | TREATMENT OF VAGINAL SYMPTOMS OF UROGENITAL ATROPHY BY ORALLY ADMINISTERING OSPEMIFENE WITH FOOD TO ENHANCE BIOAVAILABILITY OF OSPEMIFENE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9855224 | Feb. 13, 2024 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9855224 | Feb. 13, 2024 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 9855224 | Feb. 13, 2024 | TREATMENT OF VAGINAL SYMPTOMS OF UROGENITAL ATROPHY BY ORALLY ADMINISTERING OSPEMIFENE WITH FOOD TO ENHANCE BIOAVAILABILITY OF OSPEMIFENE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 6245819 | July 21, 2025 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 6245819 | July 21, 2025 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8236861 | Aug. 11, 2026 | TREATMENT OF DYSPAREUNIA ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8236861 | Aug. 11, 2026 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS AND PAIN WITH INTERCOURSE, SYMPTOMS OF VULVAR AND VAGINAL ATROPHY, ASSOCIATED WITH MENOPAUSE |
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | 8236861 | Aug. 11, 2026 | TREATMENT OF VAGINAL SYMPTOMS OF UROGENITAL ATROPHY BY ORALLY ADMINISTERING OSPEMIFENE WITH FOOD TO ENHANCE BIOAVAILABILITY OF OSPEMIFENE |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| 60MG | OSPHENA | DUCHESNAY | N203505 | Feb. 26, 2013 | RX | TABLET | ORAL | Jan. 25, 2022 | TREATMENT OF MODERATE TO SEVERE VAGINAL DRYNESS, A SYMPTOM OF VULVAR AND VAGINAL ATROPHY, DUE TO MENOPAUSE |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Estrogen receptor | Nuclear hormone receptor | MODULATOR | IC50 | 6.08 | WOMBAT-PK | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D08958 | KEGG_DRUG |
| 4032347 | VANDF |
| CHEBI:73275 | CHEBI |
| CHEMBL2105395 | ChEMBL_ID |
| C119141 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7349 | IUPHAR_LIGAND_ID |
| 7859 | INN_ID |
| DB04938 | DRUGBANK_ID |
| B0P231ILBK | UNII |
| 3036505 | PUBCHEM_CID |
| 1370971 | RXNORM |
| 199207 | MMSL |
| 29311 | MMSL |
| d08070 | MMSL |
| 014918 | NDDF |
| C1313616 | UMLSCUI |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Osphena | HUMAN PRESCRIPTION DRUG LABEL | 1 | 59630-580 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 29 sections |
| Osphena | HUMAN PRESCRIPTION DRUG LABEL | 1 | 75929-178 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 29 sections |