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

Stem definition	Drug id	CAS RN
	164	125-84-8

Description:

Molecule

Description

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:

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

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 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|

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	P11511	CP19A_HUMAN	INHIBITOR	IC50	5.11		WOMBAT-PK	CHEMBL
Cholesterol side-chain cleavage enzyme, mitochondrial	Enzyme	P05108	CP11A_HUMAN	INHIBITOR				CHEMBL	CHEMBL
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	4.73		CHEMBL
Aromatase	Enzyme		CP19A_RAT		EC50	6.59		CHEMBL
Cytochrome P450 11A1	Enzyme		CP11A_BOVIN		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
387257000	SNOMEDCT_US
47124006	SNOMEDCT_US
4018784	VANDF
001625	NDDF

Pharmaceutical products:

None