estradiol valerate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| estrogens | 1064 | 979-32-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
The 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 3 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 15, 1954 | FDA | PAR STERILE PRODUCTS |
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 |
|---|---|---|---|---|---|---|
| Ovarian hyperstimulation syndrome | 71.02 | 35.36 | 17 | 1517 | 3997 | 63483491 |
| Vestibular migraine | 64.78 | 35.36 | 10 | 1524 | 225 | 63487263 |
| Endometrial cancer | 53.65 | 35.36 | 13 | 1521 | 3212 | 63484276 |
| Ear congestion | 50.43 | 35.36 | 12 | 1522 | 2747 | 63484741 |
| Therapeutic response changed | 49.87 | 35.36 | 10 | 1524 | 1035 | 63486453 |
| Migraine | 39.97 | 35.36 | 27 | 1507 | 103319 | 63384169 |
| Bipolar disorder | 37.84 | 35.36 | 12 | 1522 | 7948 | 63479540 |
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 |
|---|---|---|---|---|---|---|
| Ovarian hyperstimulation syndrome | 77.98 | 36.82 | 17 | 1419 | 3554 | 79739398 |
| Ear congestion | 53.27 | 36.82 | 12 | 1424 | 2907 | 79740045 |
| Migraine | 40.40 | 36.82 | 23 | 1413 | 87470 | 79655482 |
| Vestibular migraine | 39.86 | 36.82 | 6 | 1430 | 154 | 79742798 |
| Thyroid disorder | 38.49 | 36.82 | 13 | 1423 | 14066 | 79728886 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA CS | M0447348 | Estradiol Congeners |
| FDA MoA | N0000000100 | Estrogen Receptor Agonists |
| MeSH PA | D004967 | Estrogens |
| MeSH PA | D006728 | Hormones |
| FDA EPC | N0000175825 | Estrogen |
| CHEBI has role | CHEBI:50114 | estrogens |
| CHEBI has role | CHEBI:62872 | quinoline oxidase inhibitors |
| CHEBI has role | CHEBI:75771 | Mus musculus metabolites |
| CHEBI has role | CHEBI:77746 | Homo sapiens metabolite |
| CHEBI has role | CHEBI:83056 | Daphnia magna metabolites |
| CHEBI has role | CHEBI:176497 | geroprotectors |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Contraception | indication | 13197004 | |
| Female hypogonadism syndrome | indication | 16041008 | |
| Primary ovarian failure | indication | 65846009 | |
| Menopausal flushing | indication | 198436008 | |
| Advanced Prostatic Carcinoma | indication | ||
| Metastatic Prostate Carcinoma | indication | ||
| Polycystic ovaries | off-label use | 69878008 | |
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Gynecomastia | contraindication | 4754008 | DOID:12698 |
| Hypocalcemia | contraindication | 5291005 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Diplopia | contraindication | 24982008 | |
| Retinal hemorrhage | contraindication | 28998008 | |
| Depressive disorder | contraindication | 35489007 | |
| Chloasma | contraindication | 36209000 | |
| Migraine | contraindication | 37796009 | DOID:6364 |
| Hypertensive disorder | contraindication | 38341003 | DOID:10763 |
| Disorder of gallbladder | contraindication | 39621005 | DOID:0060262 |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Body fluid retention | contraindication | 43498006 | |
| Thrombosis of retinal vein | contraindication | 46085004 | |
| Humoral hypercalcemia of malignancy | contraindication | 47709007 | |
| Chronic heart failure | contraindication | 48447003 | |
| Dementia | contraindication | 52448006 | |
| Hepatic porphyria | contraindication | 55056006 | DOID:3133 |
| Systemic lupus erythematosus | contraindication | 55464009 | DOID:9074 |
| Hyperlipidemia | contraindication | 55822004 | DOID:1168 |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
| Intermenstrual bleeding - irregular | contraindication | 64996003 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Sleep apnea | contraindication | 73430006 | DOID:0050847 |
| Epilepsy | contraindication | 84757009 | DOID:1826 |
| Breast lump | contraindication | 89164003 | |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Uterine leiomyoma | contraindication | 95315005 | DOID:13223 |
| Neoplasm of prostate | contraindication | 126906006 | DOID:10283 |
| Deep venous thrombosis | contraindication | 128053003 | |
| Seizure disorder | contraindication | 128613002 | |
| Endometriosis | contraindication | 129103003 | |
| Bed-ridden | contraindication | 160685001 | |
| Mammography abnormal | contraindication | 168750009 | |
| Asthma | contraindication | 195967001 | DOID:2841 |
| Cerebrovascular accident | contraindication | 230690007 | |
| Pulmonary thromboembolism | contraindication | 233935004 | |
| Thrombophilia | contraindication | 234467004 | DOID:2452 |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Endometrial carcinoma | contraindication | 254878006 | DOID:2871 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Edema | contraindication | 267038008 | |
| Chorea | contraindication | 271700006 | |
| Pregnancy, function | contraindication | 289908002 | |
| Hypertriglyceridemia | contraindication | 302870006 | |
| Functional visual loss | contraindication | 313165001 | |
| Malignant tumor of ovary | contraindication | 363443007 | DOID:2394 |
| Thromboembolic disorder | contraindication | 371039008 | |
| Cardiovascular event risk | contraindication | 395112001 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Chronic lung disease | contraindication | 413839001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Obesity | contraindication | 414916001 | DOID:9970 |
| Estrogen receptor positive tumor | contraindication | 416053008 | |
| Porphyria | contraindication | 418470004 | |
| Optic disc edema | contraindication | 423341008 | DOID:146 |
| Family history of malignant neoplasm of breast | contraindication | 429740004 | |
| Hypertensive urgency | contraindication | 443482000 | |
| Carcinoma of female breast | contraindication | 447782002 | |
| Smokes tobacco daily | contraindication | 449868002 | |
| Breast Carcinoma in Males | contraindication |
🐶 Veterinary Drug Use
| Species | Use | Relation |
|---|---|---|
| Cattle | To increase rate of weight gain | Indication |
| Cattle | To improve feed efficiency | Indication |
| Cattle | Synchronization of estrus/ovulation | Indication |
🐶 Veterinary products
| Product | Applicant | Ingredients |
|---|---|---|
| Syncro-Mate-B | Boehringer lngelheim Animal Health USA Inc. | 2 |
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 11.13 | acidic |
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 |
|---|---|---|---|---|---|---|---|---|---|---|
| N/A,2MG,3MG,N/A,N/A;3MG,2MG,2MG,1MG,N/A | NATAZIA | BAYER HLTHCARE | N022252 | May 6, 2010 | RX | TABLET | ORAL | 8071577 | May 13, 2026 | PREVENTION OF PREGNANCY |
| N/A,2MG,3MG,N/A,N/A;3MG,2MG,2MG,1MG,N/A | NATAZIA | BAYER HLTHCARE | N022252 | May 6, 2010 | RX | TABLET | ORAL | 8153616 | Jan. 30, 2028 | TREATMENT OF HEAVY MENSTRUAL BLEEDING IN WOMEN WITHOUT ORGANIC PATHOLOGY WHO CHOOSE TO USE AN ORAL CONTRACEPTIVE AS THEIR METHOD OF CONTRACEPTION |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Estrogen receptor | Nuclear hormone receptor | AGONIST | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017607 | VUID |
| N0000179123 | NUI |
| D01413 | KEGG_DRUG |
| 4017607 | VANDF |
| 4017609 | VANDF |
| 4021205 | VANDF |
| C0059623 | UMLSCUI |
| CHEBI:31561 | CHEBI |
| CHEBI:16469 | CHEBI |
| EST | PDB_CHEM_ID |
| CHEMBL1511 | ChEMBL_ID |
| DB13956 | DRUGBANK_ID |
| D004958 | MESH_DESCRIPTOR_UI |
| 13791 | PUBCHEM_CID |
| 7655 | IUPHAR_LIGAND_ID |
| 3921 | INN_ID |
| OKG364O896 | UNII |
| DB00783 | DRUGBANK_ID |
| 24395 | RXNORM |
| 4684 | MMSL |
| 4686 | MMSL |
| 6157 | MMSL |
| 6947 | MMSL |
| 73244 | MMSL |
| 756 | MMSL |
| 8602 | MMSL |
| d00537 | MMSL |
| 001265 | NDDF |
| 001269 | NDDF |
| 126172005 | SNOMEDCT_US |
| 12839006 | SNOMEDCT_US |
| 96350008 | SNOMEDCT_US |
| C0014912 | UMLSCUI |
| 406 | INN_ID |
| 5757 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Estradiol Valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9289 | INJECTION | 10 mg | INTRAMUSCULAR | ANDA | 15 sections |
| Estradiol Valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9289 | INJECTION | 10 mg | INTRAMUSCULAR | ANDA | 15 sections |
| Estradiol Valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9290 | INJECTION | 20 mg | INTRAMUSCULAR | ANDA | 15 sections |
| Estradiol Valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9290 | INJECTION | 20 mg | INTRAMUSCULAR | ANDA | 15 sections |
| Estradiol Valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9291 | INJECTION | 40 mg | INTRAMUSCULAR | ANDA | 15 sections |
| Estradiol Valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0143-9291 | INJECTION | 40 mg | INTRAMUSCULAR | ANDA | 15 sections |
| ESTRADIOL VALERATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-0420 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 26 sections |
| ESTRADIOL VALERATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-0420 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 26 sections |
| ESTRADIOL VALERATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-0440 | INJECTION, SOLUTION | 40 mg | INTRAMUSCULAR | ANDA | 26 sections |
| ESTRADIOL VALERATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0517-0440 | INJECTION, SOLUTION | 40 mg | INTRAMUSCULAR | ANDA | 26 sections |
| ESTRADIOL VALERATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0574-0870 | INJECTION, SOLUTION | 20 mg | INTRAMUSCULAR | ANDA | 26 sections |
| ESTRADIOL VALERATE | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0574-0872 | INJECTION, SOLUTION | 40 mg | INTRAMUSCULAR | ANDA | 26 sections |
| Delestrogen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-110 | INJECTION | 10 mg | INTRAMUSCULAR | NDA | 27 sections |
| Delestrogen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-111 | INJECTION | 20 mg | INTRAMUSCULAR | NDA | 27 sections |
| Delestrogen | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42023-112 | INJECTION | 40 mg | INTRAMUSCULAR | NDA | 27 sections |
| Estradiol valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70700-273 | INJECTION | 10 mg | INTRAMUSCULAR | ANDA | 27 sections |
| Estradiol valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70700-274 | INJECTION | 20 mg | INTRAMUSCULAR | ANDA | 27 sections |
| Estradiol valerate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70700-275 | INJECTION | 40 mg | INTRAMUSCULAR | ANDA | 27 sections |