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fluoxymesterone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| androgens/anabolic steroids | 1210 | 76-43-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An anabolic steroid that has been used in the treatment of male HYPOGONADISM, delayed puberty in males, and in the treatment of breast neoplasms in women.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mg | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BA (Bioavailability) | 80 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 2.547 | Moderate | 0.72 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 4.102 | Moderate | 0.72 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 44.259 | 10^-6 cm/s | Moderate | 0.72 |
| dh-clint | Dog hepatocyte intrinsic clearance | 10.233 | uL/min/10^6 cells | Moderate | 0.72 |
| dppb | Dog plasma protein binding (% unbound) | 20.980 | % | Moderate | 0.72 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 34.060 | % | Moderate | 0.72 |
| herg | hERG pIC50 | 4.290 | pIC50 | Moderate | 0.72 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.589 | uL/min/10^6 cells | Moderate | 0.72 |
| hlm-clint | Human liver microsomal intrinsic clearance | 50.350 | uL/min/mg protein | Moderate | 0.72 |
| hppb | Human plasma protein binding (% unbound) | 16.570 | % | Moderate | 0.72 |
| kinase-safety-class | ACVR2B,CDK5,EIF2AK3,GRK2,PDK1,PDK2,PDK4,PRKDC | 8 | |||
| kinase-selectivity-class | EIF2AK3,GRK2,PDK2 | 3 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 17.783 | Moderate | 0.72 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 31.477 | Moderate | 0.72 | |
| mppb | Mouse plasma protein binding (% unbound) | 20.340 | Moderate | 0.72 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 25.645 | Moderate | 0.72 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 18.530 | % | Moderate | 0.72 |
| rh-clint | Rat hepatocyte intrinsic clearance | 37.844 | uL/min/10^6 cells | Moderate | 0.72 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 59.990 | % | Moderate | 0.72 |
| rppb | Rat plasma protein binding (% unbound) | 15.820 | % | Moderate | 0.72 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 477.529 | uM | Moderate | 0.72 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 15, 1956 | FDA |
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 |
|---|---|---|
| ATC | G03BA01 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ANDROGENS 3-oxoandrosten (4) derivatives |
| FDA CS | M0001109 | Androstanes |
| FDA MoA | N0000000146 | Androgen Receptor Agonists |
| MeSH PA | D006728 | Hormones |
| MeSH PA | D045930 | Anabolic Agents |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:36413 | anabolic agent |
| FDA EPC | N0000175824 | Androgen |
Related Drugs by ATC class:
G03BA 3-oxoandrosten (4) derivatives 2 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Deficiency of testosterone biosynthesis | indication | 38825009 | |
| Male hypogonadism | indication | 48723006 | |
| Congenital myotonia, autosomal dominant form | indication | 57938005 | |
| Undescended testicle | indication | 204878001 | DOID:11383 |
| Noonan's syndrome | indication | 205824006 | DOID:3490 |
| Delayed puberty | indication | 400003000 | |
| Klinefelter's syndrome, XXY | indication | 405769009 | |
| Hormone receptor positive malignant neoplasm of breast | indication | 417181009 | |
| LHRH Deficiency | indication | ||
| Primary Hypogonadism due to Bilateral Torsion | indication | ||
| Bilateral Anorchia | indication | ||
| Primary Hypogonadism due to Orchitis | indication | ||
| Anemia | off-label use | 271737000 | DOID:2355 |
| Hyperlipoproteinemia | contraindication | 3744001 | DOID:1168 |
| Hypocalcemia | contraindication | 5291005 | |
| Hypercholesterolemia | contraindication | 13644009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| 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 | |
| Dementia | contraindication | 52448006 | |
| Hepatic porphyria | contraindication | 55056006 | DOID:3133 |
| Systemic lupus erythematosus | contraindication | 55464009 | DOID:9074 |
| Thrombophlebitis | contraindication | 64156001 | DOID:3875 |
| Intermenstrual bleeding - irregular | contraindication | 64996003 | |
| Hypercalcemia | contraindication | 66931009 | DOID:12678 |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Heart failure | contraindication | 84114007 | DOID:6000 |
| 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 | |
| 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 | |
| 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 | 13.48 | 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 |
|---|---|---|---|---|---|---|---|---|---|
| Androgen receptor | Nuclear hormone receptor | AGONIST | Ki | 8.24 | CHEMBL | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4017725 | VUID |
| N0000146093 | NUI |
| D00327 | KEGG_DRUG |
| 4017725 | VANDF |
| C0016366 | UMLSCUI |
| CHEBI:5120 | CHEBI |
| CHEMBL1445 | ChEMBL_ID |
| DB01185 | DRUGBANK_ID |
| D005474 | MESH_DESCRIPTOR_UI |
| 6446 | PUBCHEM_CID |
| 2861 | IUPHAR_LIGAND_ID |
| 624 | INN_ID |
| 9JU12S4YFY | UNII |
| 4494 | RXNORM |
| 4747 | MMSL |
| 60 | MMSL |
| d00562 | MMSL |
| 001250 | NDDF |
| 126125005 | SNOMEDCT_US |
| 63470003 | SNOMEDCT_US |
| 9JU12S4YFY | INXIGHT DRUGS |
Pharmaceutical products:
None