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| Stem definition | Drug id | CAS RN |
|---|---|---|
| antiestrogens or estrogen receptor modulators, clomifene and tamoxifen derivatives | 4749 | 128607-22-7 |
None
| Property | Value | Reference |
|---|---|---|
| fu (Fraction unbound in plasma) | 0 % | Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K |
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Feb. 26, 2013 | FDA | SHIONOGI INC | |
| Nov. 20, 2014 | EMA | Shionogi Limited |
| 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 | 310.13 | 36.75 | 87 | 1351 | 59401 | 90567608 |
| Labelled drug-drug interaction medication error | 193.10 | 36.75 | 45 | 1393 | 14537 | 90612472 |
| Vaginal discharge | 165.25 | 36.75 | 42 | 1396 | 19422 | 90607587 |
| Vaginal haemorrhage | 127.85 | 36.75 | 38 | 1400 | 31233 | 90595776 |
| No adverse event | 113.47 | 36.75 | 42 | 1396 | 67940 | 90559069 |
| Therapeutic response unexpected | 104.43 | 36.75 | 30 | 1408 | 21850 | 90605159 |
| Muscle spasms | 99.47 | 36.75 | 57 | 1381 | 251826 | 90375183 |
| Vulvovaginal burning sensation | 73.59 | 36.75 | 15 | 1423 | 2580 | 90624429 |
| Vulvovaginal discomfort | 67.18 | 36.75 | 14 | 1424 | 2683 | 90624326 |
| Inability to afford medication | 57.60 | 36.75 | 13 | 1425 | 3609 | 90623400 |
| Hyperhidrosis | 51.33 | 36.75 | 30 | 1408 | 136275 | 90490734 |
| Vulvovaginal pruritus | 51.04 | 36.75 | 12 | 1426 | 3981 | 90623028 |
| Off label use | 45.56 | 36.75 | 70 | 1368 | 1102182 | 89524827 |
| Labelled drug-disease interaction medication error | 38.96 | 36.75 | 6 | 1432 | 205 | 90626804 |
| Product prescribing error | 37.24 | 36.75 | 15 | 1423 | 30130 | 90596879 |
| Vulvovaginal pain | 36.94 | 36.75 | 9 | 1429 | 3465 | 90623544 |
None
| 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 | 240.47 | 41.91 | 65 | 967 | 65971 | 110522296 |
| Vaginal discharge | 121.11 | 41.91 | 29 | 1003 | 17879 | 110570388 |
| Labelled drug-drug interaction medication error | 111.64 | 41.91 | 30 | 1002 | 29272 | 110558995 |
| Vaginal haemorrhage | 101.79 | 41.91 | 27 | 1005 | 25047 | 110563220 |
| Muscle spasms | 86.86 | 41.91 | 45 | 987 | 278112 | 110310155 |
| Therapeutic response unexpected | 79.52 | 41.91 | 22 | 1010 | 23821 | 110564446 |
| Vulvovaginal discomfort | 64.96 | 41.91 | 12 | 1020 | 2112 | 110586155 |
| No adverse event | 55.11 | 41.91 | 22 | 1010 | 73817 | 110514450 |
| Vulvovaginal burning sensation | 52.57 | 41.91 | 10 | 1022 | 2059 | 110586208 |
None
| 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 agent |
| CHEBI has role | CHEBI:50739 | estrogen receptor modulator |
| CHEBI has role | CHEBI:67079 | anti-inflammatory agent |
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Dyspareunia | indication | 71315007 | |
| Atrophic vulva | indication | 248861000 | DOID:14275 |
None
None
None
| 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 | 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 |
None
| 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 | |||
| Estrogen receptor beta | Nuclear hormone receptor | ANTAGONIST | Ki | 6.39 | IUPHAR |
| ID | Source |
|---|---|
| D08958 | KEGG_DRUG |
| 4032347 | VANDF |
| CHEBI:73275 | CHEBI |
| CHEMBL2105395 | ChEMBL_ID |
| C119141 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7349 | IUPHAR_LIGAND_ID |
| DB04938 | DRUGBANK_ID |
| B0P231ILBK | UNII |
| 1370971 | RXNORM |
| 199207 | MMSL |
| 29311 | MMSL |
| d08070 | MMSL |
| 014918 | NDDF |
| 716223004 | SNOMEDCT_US |
| C1313616 | UMLSCUI |
| 7859 | INN_ID |
| 3036505 | PUBCHEM_CID |
| B0P231ILBK | INXIGHT DRUGS |
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Osphena | HUMAN PRESCRIPTION DRUG LABEL | 1 | 55494-580 | TABLET, FILM COATED | 60 mg | ORAL | NDA | 30 sections |