prasterone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| androgens/anabolic steroids | 795 | 53-43-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A major C19 steroid produced by the ADRENAL CORTEX. It is also produced in small quantities in the TESTIS and the OVARY. Dehydroepiandrosterone (DHEA) can be converted to TESTOSTERONE; ANDROSTENEDIONE; ESTRADIOL; and ESTRONE. Most of DHEA is sulfated (DEHYDROEPIANDROSTERONE SULFATE) before secretion.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 6.50 | mg | V |
ADMET properties:
None
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| None | FDA |
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 |
|---|---|---|---|---|---|---|
| Butterfly rash | 132.78 | 20.40 | 28 | 3213 | 1745 | 63484036 |
| Periorbital oedema | 100.36 | 20.40 | 28 | 3213 | 5656 | 63480125 |
| Photosensitivity reaction | 80.95 | 20.40 | 30 | 3211 | 14964 | 63470817 |
| Off label use | 70.58 | 20.40 | 124 | 3117 | 674338 | 62811443 |
| Head discomfort | 69.34 | 20.40 | 26 | 3215 | 13389 | 63472392 |
| Swelling face | 58.98 | 20.40 | 38 | 3203 | 63437 | 63422344 |
| Tinnitus | 56.03 | 20.40 | 30 | 3211 | 35598 | 63450183 |
| Feeling hot | 51.40 | 20.40 | 32 | 3209 | 50322 | 63435459 |
| Application site discharge | 46.31 | 20.40 | 8 | 3233 | 169 | 63485612 |
| Cellulitis | 33.39 | 20.40 | 30 | 3211 | 81928 | 63403853 |
| Hypothalamic pituitary adrenal axis suppression | 32.90 | 20.40 | 6 | 3235 | 174 | 63485607 |
| Therapeutic response unexpected | 32.90 | 20.40 | 17 | 3224 | 18742 | 63467039 |
| Dehydroepiandrosterone increased | 26.65 | 20.40 | 3 | 3238 | 0 | 63485781 |
| Headache | 25.18 | 20.40 | 80 | 3161 | 633161 | 62852620 |
| Vaginal discharge | 24.18 | 20.40 | 11 | 3230 | 9187 | 63476594 |
| Granulomatous liver disease | 24.15 | 20.40 | 6 | 3235 | 772 | 63485009 |
FDA Adverse Event Reporting System (Male)
| 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 |
|---|---|---|---|---|---|---|
| Tendon calcification | 52.65 | 29.68 | 7 | 646 | 68 | 34956210 |
| Progesterone increased | 34.85 | 29.68 | 4 | 649 | 9 | 34956269 |
| Blood parathyroid hormone increased | 31.65 | 29.68 | 7 | 646 | 1507 | 34954771 |
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 |
|---|---|---|---|---|---|---|
| Butterfly rash | 144.80 | 21.88 | 28 | 2741 | 1668 | 79739951 |
| Periorbital oedema | 100.23 | 21.88 | 28 | 2741 | 8374 | 79733245 |
| Photosensitivity reaction | 78.51 | 21.88 | 29 | 2740 | 21098 | 79720521 |
| Head discomfort | 77.17 | 21.88 | 26 | 2743 | 14476 | 79727143 |
| Tinnitus | 66.81 | 21.88 | 32 | 2737 | 44301 | 79697318 |
| Swelling face | 57.77 | 21.88 | 34 | 2735 | 71178 | 79670441 |
| Feeling hot | 55.06 | 21.88 | 31 | 2738 | 59703 | 79681916 |
| Tendon calcification | 43.16 | 21.88 | 7 | 2762 | 149 | 79741470 |
| Cellulitis | 42.39 | 21.88 | 33 | 2736 | 109027 | 79632592 |
| Off label use | 39.88 | 21.88 | 93 | 2676 | 907122 | 78834497 |
| Headache | 29.68 | 21.88 | 68 | 2701 | 653704 | 79087915 |
| Application site discharge | 24.99 | 21.88 | 5 | 2764 | 354 | 79741265 |
| Dehydroepiandrosterone increased | 24.86 | 21.88 | 3 | 2766 | 5 | 79741614 |
| Granulomatous liver disease | 23.24 | 21.88 | 6 | 2763 | 1327 | 79740292 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A14AA07 | ALIMENTARY TRACT AND METABOLISM ANABOLIC AGENTS FOR SYSTEMIC USE ANABOLIC STEROIDS Androstan derivatives |
| ATC | G03EA03 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ANDROGENS AND FEMALE SEX HORMONES IN COMBINATION Androgens and estrogens |
| ATC | G03XX01 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM OTHER SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM Other sex hormones and modulators of the genital system |
| MeSH PA | D000276 | Adjuvants, Immunologic |
| MeSH PA | D007155 | Immunologic Factors |
| CHEBI has role | CHEBI:50113 | androgene |
| CHEBI has role | CHEBI:75771 | Mus musculus 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 |
|---|---|---|---|
| Systemic lupus erythematosus | indication | 55464009 | DOID:9074 |
| 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 |
|---|---|---|---|---|---|---|---|---|---|---|
| 6.5MG | INTRAROSA | MILLICENT | N208470 | Nov. 16, 2016 | RX | INSERT | VAGINAL | 8957054 | Jan. 8, 2030 | INTRAVAGINAL PRASTERONE (DEHYDROEPIANDROSTERONE) AT A DAILY DOSE OF 6.5MG FOR THE TREATMENT OF DYSPAREUNIA, A SYMPTOM OF VULVAR AND VAGINAL ATROPHY, DUE TO MENOPAUSE |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Corticosteroid-binding globulin | Secreted | Ki | 5 | CHEMBL | |||||
| Sex hormone-binding globulin | Secreted | Kd | 7.84 | CHEMBL | |||||
| Glucose-6-phosphate 1-dehydrogenase | Enzyme | Ki | 5.21 | CHEMBL | |||||
| Beta-glucuronidase | Enzyme | IC50 | 4.11 | CHEMBL | |||||
| Glucose-6-phosphate 1-dehydrogenase | Enzyme | Ki | 5.96 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4021360 | VUID |
| N0000148779 | NUI |
| D08409 | KEGG_DRUG |
| 1927689 | RXNORM |
| 4021360 | VANDF |
| 4036745 | VANDF |
| CHEBI:28689 | CHEBI |
| AND | PDB_CHEM_ID |
| CHEMBL90593 | ChEMBL_ID |
| 2370 | IUPHAR_LIGAND_ID |
| 2869 | INN_ID |
| DB01708 | DRUGBANK_ID |
| 459AG36T1B | UNII |
| 131731 | MMSL |
| 20676 | MMSL |
| 247058 | MMSL |
| 32118 | MMSL |
| 73034 | MMSL |
| d04425 | MMSL |
| 004609 | NDDF |
| 413963008 | SNOMEDCT_US |
| 78316004 | SNOMEDCT_US |
| C0011185 | UMLSCUI |
| D003687 | MESH_DESCRIPTOR_UI |
| 5881 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Intrarosa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 64011-601 | INSERT | 6.50 mg | VAGINAL | NDA | 17 sections |
| Intrarosa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72495-401 | INSERT | 6.50 mg | VAGINAL | NDA | 17 sections |
| Intrarosa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72495-401 | INSERT | 6.50 mg | VAGINAL | NDA | 17 sections |
| Intrarosa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72495-501 | INSERT | 6.50 mg | VAGINAL | NDA | 17 sections |
| Intrarosa | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72495-501 | INSERT | 6.50 mg | VAGINAL | NDA | 17 sections |
| Debaochun | HUMAN OTC DRUG LABEL | 7 | 82570-016 | POWDER | 10 g | TOPICAL | unapproved drug other | 8 sections |