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androstanolone 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| steroids, androgens | 3927 | 521-18-6 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
A potent androgenic metabolite of TESTOSTERONE. It is produced by the action of the enzyme 3-OXO-5-ALPHA-STEROID 4-DEHYDROGENASE.
|
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 3.756 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 3.112 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 35.563 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 88.308 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 3.290 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 4.140 | % | High | 1 |
| herg | hERG pIC50 | 4.798 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 59.566 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 52.602 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 2.600 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,BTK,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,NTRK2,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1 | 19 | |||
| kinase-selectivity-class | EIF2AK3,PDK2 | 2 | |||
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.199 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 195.434 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 2.250 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.445 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 2.580 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 288.403 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 9.560 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 3.980 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 9.977 | uM | High | 1 |
Approvals:
None
FDA Adverse Event Reporting System (Female)
None
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 |
|---|---|---|---|---|---|---|
| Polycythaemia | 87.63 | 71.86 | 10 | 4 | 2876 | 42618445 |
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 |
|---|---|---|---|---|---|---|
| Polycythaemia | 95.90 | 77.25 | 10 | 4 | 3265 | 110586020 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | A14AA01 | ALIMENTARY TRACT AND METABOLISM ANABOLIC AGENTS FOR SYSTEMIC USE ANABOLIC STEROIDS Androstan derivatives |
| ATC | G03BB02 | GENITO URINARY SYSTEM AND SEX HORMONES SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM ANDROGENS 5-androstanon (3) derivatives |
| MeSH PA | D000728 | Androgens |
| MeSH PA | D006728 | Hormones |
| CHEBI has role | CHEBI:50113 | androgene |
| CHEBI has role | CHEBI:75771 | Mus musculus metabolites |
| CHEBI has role | CHEBI:77746 | Homo sapiens metabolite |
| CHEBI has role | CHEBI:83056 | Daphnia magna metabolites |
Related Drugs by ATC class:
A14AA Androstan derivatives 8 drugs
G03BB 5-androstanon (3) derivatives 1 drug
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Anemia of chronic renal failure | indication | 49708008 | |
| Catabolic Process | indication | ||
| Turner syndrome | off-label use | 38804009 | DOID:3491 |
| Congenital hypoplastic anemia | off-label use | 88854002 | DOID:1339 |
| Hb SS disease | off-label use | 127040003 | DOID:10923 |
| Hypercholesterolemia | contraindication | 13644009 | |
| Myocardial infarction | contraindication | 22298006 | DOID:5844 |
| Obstruction of bile duct | contraindication | 30144000 | |
| Renal failure syndrome | contraindication | 42399005 | DOID:1074 |
| Body fluid retention | contraindication | 43498006 | |
| Humoral hypercalcemia of malignancy | contraindication | 47709007 | |
| Nephrotic syndrome | contraindication | 52254009 | DOID:1184 |
| Heart disease | contraindication | 56265001 | DOID:114 |
| Peliosis hepatis | contraindication | 58008004 | DOID:914 |
| Blood coagulation disorder | contraindication | 64779008 | DOID:1247 |
| Hypercalcemia | contraindication | 66931009 | DOID:12678 |
| Arteriosclerotic vascular disease | contraindication | 72092001 | |
| Diabetes mellitus | contraindication | 73211009 | DOID:9351 |
| Heart failure | contraindication | 84114007 | DOID:6000 |
| Kidney disease | contraindication | 90708001 | DOID:557 |
| Cholestatic hepatitis | contraindication | 95556007 | |
| Neoplasm of liver | contraindication | 126851005 | DOID:3571 |
| Neoplasm of prostate | contraindication | 126906006 | DOID:10283 |
| Hypoalphalipoproteinemia | contraindication | 190785000 | |
| Decompensated cardiac failure | contraindication | 195111005 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Benign prostatic hyperplasia | contraindication | 266569009 | |
| Edema | contraindication | 267038008 | |
| Pregnancy, function | contraindication | 289908002 | |
| Breastfeeding (mother) | contraindication | 413712001 | |
| Disorder of coronary artery | contraindication | 414024009 | |
| Breast Carcinoma in Males | contraindication |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
None
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 |
|---|---|---|---|---|---|---|---|---|---|
| Glucocorticoid receptor | Nuclear hormone receptor | IC50 | 6.27 | CHEMBL | |||||
| Mineralocorticoid receptor | Nuclear hormone receptor | IC50 | 6.44 | CHEMBL | |||||
| Androgen receptor | Nuclear hormone receptor | Ki | 9.70 | CHEMBL | |||||
| Aromatase | Enzyme | Ki | 6.66 | CHEMBL | |||||
| Corticosteroid-binding globulin | Secreted | Ki | 5.92 | CHEMBL | |||||
| Sex hormone-binding globulin | Secreted | Kd | 9.74 | CHEMBL | |||||
| Progesterone receptor | Nuclear hormone receptor | IC50 | 5.14 | CHEMBL | |||||
| Androgen receptor | Transcription factor | Ki | 9.57 | CHEMBL | |||||
| Progesterone receptor | Transcription factor | Ki | 6.79 | DRUG MATRIX | |||||
| Glucocorticoid receptor | Transcription factor | IC50 | 4.70 | CHEMBL | |||||
| Androgen receptor | Transcription factor | IC50 | 9 | CHEMBL | |||||
| Progesterone receptor | Transcription factor | IC50 | 6.36 | CHEMBL | |||||
| Mineralocorticoid receptor | Transcription factor | IC50 | 5.68 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| D07456 | KEGG_DRUG |
| C0038148 | UMLSCUI |
| CHEBI:16330 | CHEBI |
| CHEMBL27769 | ChEMBL_ID |
| DB02901 | DRUGBANK_ID |
| 238 | INN_ID |
| 08J2K08A3Y | UNII |
| 10635 | PUBCHEM_CID |
| 003255 | NDDF |
| 005232 | NDDF |
| 103042004 | SNOMEDCT_US |
| 56032002 | SNOMEDCT_US |
| D013196 | MESH_DESCRIPTOR_UI |
| DHT | PDB_CHEM_ID |
| 2856 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
None