aminoglutethimide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
164 125-84-8

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • aminoglutetimide
  • cytadren
  • aminoglutethimide
  • DL-Aminoglutethimide
  • orimeten
An aromatase inhibitor that is used in the treatment of advanced BREAST CANCER.
  • Molecular weight: 232.28
  • Formula: C13H16N2O2
  • CLOGP: 0.77
  • LIPINSKI: 0
  • HAC: 4
  • HDO: 2
  • TPSA: 72.19
  • ALOGS: -2.80
  • ROTB: 2
  • Status: OFM
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1 g O

ADMET properties:

PropertyValueReference
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

Approvals:

DateAgencyCompanyOrphan
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:

SourceCodeDescription
ATC L02BG01 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ENDOCRINE THERAPY
HORMONE ANTAGONISTS AND RELATED AGENTS
Aromatase inhibitors
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:35623 anticonvulsants
CHEBI has role CHEBI:37962 adrenergic agents
CHEBI has role CHEBI:50790 aromatase inhibitors
MeSH PA D000970 Antineoplastic Agents
MeSH PA D018931 Antineoplastic Agents, Hormonal
MeSH PA D047072 Aromatase Inhibitors
MeSH PA D004791 Enzyme Inhibitors
MeSH PA D004965 Estrogen Antagonists
MeSH PA D006727 Hormone Antagonists
MeSH PA D065088 Steroid Synthesis Inhibitors
FDA MoA N0000175921 Adrenal Steroid Synthesis Inhibitors
FDA EPC N0000175928 Adrenal Steroid Synthesis Inhibitor

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
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 levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA 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:

IDSource
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
387257000 SNOMEDCT_US
47124006 SNOMEDCT_US
4018784 VANDF
001625 NDDF

Pharmaceutical products:

None