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estradiol cypionate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| estrogens | 1059 | 313-06-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| S (Water solubility) | 0.01 mg/mL | Bocci G, Oprea TI, Benet LZ |
| BA (Bioavailability) | 5 % |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Aug. 15, 1979 | FDA | PHARMACIA AND UPJOHN |
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 |
|---|---|---|
| FDA CS | M0447348 | Estradiol Congeners |
| FDA MoA | N0000000100 | Estrogen Receptor Agonists |
| MeSH PA | D000080066 | Contraceptive Agents, Hormonal |
| MeSH PA | D003270 | Contraceptive Agents |
| MeSH PA | D003271 | Contraceptive Agents, Female |
| MeSH PA | D012102 | Reproductive Control Agents |
| MeSH PA | D004967 | Estrogens |
| MeSH PA | D006728 | Hormones |
| FDA EPC | N0000175825 | Estrogen |
| CHEBI has role | CHEBI:50114 | estrogen |
| CHEBI has role | CHEBI:77746 | human metabolite |
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 | ||
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Gynecomastia | contraindication | 4754008 | DOID:12698 |
| Hypocalcemia | contraindication | 5291005 | |
| Alcoholism | contraindication | 7200002 | |
| Weight gain finding | contraindication | 8943002 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Fibroadenosis of breast | contraindication | 23260002 | DOID:10352 |
| 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 |
| Anorexia nervosa | contraindication | 56882008 | DOID:8689 |
| Hepatic failure | contraindication | 59927004 | |
| Cerebrovascular disease | contraindication | 62914000 | DOID:6713 |
| Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
| Osteoporosis | contraindication | 64859006 | DOID:11476 |
| 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 | |
| Endometriosis | contraindication | 129103003 | |
| 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 | |
| Osteopenia | contraindication | 312894000 | |
| 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 | |
| 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
None
🐶 Veterinary products
None
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)
None
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 | EC50 | 10.74 | CHEMBL | CHEMBL | |||
| Glucocorticoid receptor | Nuclear hormone receptor | Ki | 4.72 | CHEMBL | |||||
| Sodium-dependent dopamine transporter | Transporter | Ki | 4.93 | CHEMBL | |||||
| Androgen receptor | Nuclear hormone receptor | IC50 | 7.72 | CHEMBL | |||||
| Estrogen receptor beta | Nuclear hormone receptor | EC50 | 11 | CHEMBL | |||||
| G-protein coupled estrogen receptor 1 | GPCR | Ki | 8.57 | CHEMBL | |||||
| Corticosteroid-binding globulin | Secreted | Ki | 5 | CHEMBL | |||||
| Steryl-sulfatase | Enzyme | IC50 | 4.08 | CHEMBL | |||||
| Sex hormone-binding globulin | Secreted | Kd | 8.83 | CHEMBL | |||||
| Steroid hormone receptor ERR1 | Nuclear hormone receptor | IC50 | 8.44 | CHEMBL | |||||
| Steroid hormone receptor ERR2 | Nuclear hormone receptor | IC50 | 8.49 | CHEMBL | |||||
| Cytochrome P450 1B1 | Enzyme | Ki | 5.72 | CHEMBL | |||||
| Sodium-dependent serotonin transporter | Transporter | Ki | 5.24 | CHEMBL | |||||
| Alpha-synuclein | Transporter | IC50 | 4.22 | CHEMBL | |||||
| Androgen receptor | Transcription factor | Ki | 6.63 | CHEMBL | |||||
| Arachidonate 15-lipoxygenase | Enzyme | IC50 | 4.95 | CHEMBL | |||||
| Progesterone receptor | Transcription factor | Ki | 5.37 | CHEMBL | |||||
| Estrogen receptor | Transcription factor | IC50 | 8.72 | CHEMBL | |||||
| Estrogen receptor beta | Transcription factor | IC50 | 8.77 | CHEMBL | |||||
| Estrogen receptor beta | Transcription factor | IC50 | 8.64 | CHEMBL | |||||
| Estrogen receptor | Transcription factor | IC50 | 8.66 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017608 | VUID |
| N0000179122 | NUI |
| D04063 | KEGG_DRUG |
| 4017608 | VANDF |
| 4017609 | VANDF |
| 4021205 | VANDF |
| C0059610 | UMLSCUI |
| CHEBI:34745 | CHEBI |
| EST | PDB_CHEM_ID |
| CHEMBL1200973 | ChEMBL_ID |
| DB13954 | DRUGBANK_ID |
| 9403 | PUBCHEM_CID |
| C007630 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7E1DV054LO | UNII |
| DB00783 | DRUGBANK_ID |
| 1000146 | RXNORM |
| 4253 | MMSL |
| 4684 | MMSL |
| 4685 | MMSL |
| 6157 | MMSL |
| 73244 | MMSL |
| 777 | MMSL |
| 8602 | MMSL |
| d00537 | MMSL |
| 001265 | NDDF |
| 001266 | NDDF |
| 109028003 | SNOMEDCT_US |
| 126172005 | SNOMEDCT_US |
| 12839006 | SNOMEDCT_US |
| C0014912 | UMLSCUI |
| 5757 | PUBCHEM_CID |
| 406 | INN_ID |
| D004958 | MESH_DESCRIPTOR_UI |
| CHEBI:16469 | CHEBI |
| 7E1DV054LO | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Depo-Estradiol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0009-0271 | INJECTION | 5 mg | INTRAMUSCULAR | ANDA | 26 sections |
| Depo-Estradiol | HUMAN PRESCRIPTION DRUG LABEL | 1 | 54868-1729 | INJECTION | 5 mg | INTRAMUSCULAR | ANDA | 26 sections |