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aminoglutethimide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| 164 | 125-84-8 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 1 | g | O |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| BDDCS (Biopharmaceutical Drug Disposition Classification System) | 2 | Benet LZ, Broccatelli F, Oprea TI |
| MRTD (Maximum Recommended Therapeutic Daily Dose) | 71.89 µM/kg/day | Contrera JF, Matthews EJ, Kruhlak NL, Benz RD |
| BA (Bioavailability) | 95 % | Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| kinase-safety-class | ACVR2A,ACVR2B,ALK,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,ERBB2,FLT3,GRK2,GSK3B,IKBKB,ITK,JAK1,JAK2,MAP2K6,MAP3K21,MAP3K7,MAP4K1,MAPK10,MAPK7,MAPKAPK2,MARK4,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ULK1 | 49 | |||
| kinase-selectivity-class | AKT2,AURKA,AXL,EIF2AK3,GRK2,MAP2K6,MAP3K7,MAPK7,NTRK3,SIK2,STK33,TEK,TTK | 13 | |||
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 29, 1980 | FDA | NOVARTIS |
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 | L02BG01 | ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS ENDOCRINE THERAPY HORMONE ANTAGONISTS AND RELATED AGENTS Aromatase inhibitors |
| CHEBI has role | CHEBI:35610 | antineoplastic agent |
| CHEBI has role | CHEBI:35623 | anticonvulsant |
| CHEBI has role | CHEBI:37962 | adrenergic agent |
| CHEBI has role | CHEBI:50790 | EC 1.14.14.14 (aromatase) inhibitor |
| MeSH PA | D000970 | Antineoplastic Agents |
| MeSH PA | D004791 | Enzyme Inhibitors |
| MeSH PA | D004965 | Estrogen Antagonists |
| MeSH PA | D006727 | Hormone Antagonists |
| MeSH PA | D018931 | Antineoplastic Agents, Hormonal |
| MeSH PA | D047072 | Aromatase Inhibitors |
| MeSH PA | D065088 | Steroid Synthesis Inhibitors |
| FDA MoA | N0000175921 | Adrenal Steroid Synthesis Inhibitors |
| FDA EPC | N0000175928 | Adrenal Steroid Synthesis Inhibitor |
Related Drugs by ATC class:
L02BG Aromatase inhibitors 5 drugs
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Secondary malignant neoplasm of female breast | indication | 94297009 | |
| Hypochloremia | contraindication | 10399008 | |
| Hyperkalemia | contraindication | 14140009 | |
| Hyperbilirubinemia | contraindication | 14783006 | DOID:2741 |
| Infectious disease | contraindication | 40733004 | |
| Hypothyroidism | contraindication | 40930008 | DOID:1459 |
| Low blood pressure | contraindication | 45007003 | |
| Hyponatremia | contraindication | 89627008 | |
| Liver function tests abnormal | contraindication | 166603001 | |
| Disease of liver | contraindication | 235856003 | DOID:409 |
| Hypoglycemic disorder | contraindication | 237630007 | |
| Pregnancy, function | contraindication | 289908002 | |
| Surgical procedure | contraindication | 387713003 | |
| Traumatic injury | contraindication | 417746004 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.75 | acidic |
| pKa2 | 5.09 | Basic |
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 |
|---|---|---|---|---|---|---|---|---|---|
| Aromatase | Enzyme | INHIBITOR | IC50 | 5.11 | WOMBAT-PK | CHEMBL | |||
| Cholesterol side-chain cleavage enzyme, mitochondrial | Enzyme | INHIBITOR | CHEMBL | CHEMBL | |||||
| Thromboxane-A synthase | Enzyme | IC50 | 4.73 | CHEMBL | |||||
| Aromatase | Enzyme | EC50 | 6.59 | CHEMBL | |||||
| Cytochrome P450 11A1 | Enzyme | IC50 | 4.54 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| 4018784 | VUID |
| N0000147087 | NUI |
| D00574 | KEGG_DRUG |
| 152167 | RXNORM |
| C0002555 | UMLSCUI |
| CHEBI:2654 | CHEBI |
| CHEMBL488 | ChEMBL_ID |
| DB00357 | DRUGBANK_ID |
| D000616 | MESH_DESCRIPTOR_UI |
| 2145 | PUBCHEM_CID |
| 7054 | IUPHAR_LIGAND_ID |
| 837 | INN_ID |
| 0O54ZQ14I9 | UNII |
| 366 | MMSL |
| 4170 | MMSL |
| d00591 | MMSL |
| 4018784 | VANDF |
| 001625 | NDDF |
| 387257000 | SNOMEDCT_US |
| 47124006 | SNOMEDCT_US |
| 0O54ZQ14I9 | INXIGHT DRUGS |
Pharmaceutical products:
None