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

Stem definition	Drug id	CAS RN
	1791	54-36-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: metyrapone mepyrapone methapyrapone methbipyranone methopirapone methopyrapone methopyrinine methopyrone metopiron metopirone metopyrone metroprione metyrapon	An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME. Molecular weight: 226.28 Formula: C14H14N2O CLOGP: 1.46 LIPINSKI: 0 HAC: 3 HDO: 0 TPSA: 42.85 ALOGS: -2.72 ROTB: 3 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

metyrapone
mepyrapone
methapyrapone
methbipyranone
methopirapone
methopyrapone
methopyrinine
methopyrone
metopiron
metopirone
metopyrone
metroprione
metyrapon

An inhibitor of the enzyme STEROID 11-BETA-MONOOXYGENASE. It is used as a test of the feedback hypothalamic-pituitary mechanism in the diagnosis of CUSHING SYNDROME.

Molecular weight: 226.28
Formula: C14H14N2O
CLOGP: 1.46
LIPINSKI: 0
HAC: 3
HDO: 0
TPSA: 42.85
ALOGS: -2.72
ROTB: 3

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Bocci G, Oprea TI, Benet LZ
S (Water solubility)	0.43 mg/mL	Bocci G, Oprea TI, Benet LZ

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Approvals:

Date	Agency	Company	Orphan
Dec. 4, 1961	FDA	HRA PHARMA

FDA Adverse Event Reporting System (Female)

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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
Premature delivery	77.71	46.26	23	601	30258	63458140
Cortisol increased	75.64	46.26	11	613	418	63487980
Cortisol free urine increased	61.38	46.26	7	617	34	63488364
Pneumocystis jirovecii pneumonia	57.44	46.26	16	608	16898	63471500
Adrenal insufficiency	56.53	46.26	16	608	17899	63470499
Blood corticotrophin decreased	46.47	46.26	7	617	338	63488060

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FDA Adverse Event Reporting System (Male)

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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
Pneumocystis jirovecii pneumonia	46.66	42.05	15	436	19695	34936785

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FDA Adverse Event Reporting System (Geriatric)

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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
Pneumocystis jirovecii pneumonia	96.74	41.72	29	929	32479	79710951
Adrenal insufficiency	78.65	41.72	24	934	28463	79714967
Cortisol free urine increased	77.22	41.72	9	949	43	79743387
Premature delivery	74.39	41.72	22	936	23445	79719985
Cortisol increased	63.37	41.72	10	948	535	79742895
Premature rupture of membranes	43.31	41.72	10	948	4059	79739371

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	V04CD01	VARIOUS DIAGNOSTIC AGENTS OTHER DIAGNOSTIC AGENTS Tests for pituitary function
CHEBI has role	CHEBI:33295	diagnostic aid
CHEBI has role	CHEBI:35221	antimetabolite
CHEBI has role	CHEBI:76798	cytochrome p450 XIB1 inhibitor
FDA EPC	N0000175928	Adrenal Steroid Synthesis Inhibitor
FDA MoA	N0000175921	Adrenal Steroid Synthesis Inhibitors
MeSH PA	D000963	Antimetabolites
MeSH PA	D004791	Enzyme Inhibitors
MeSH PA	D009676	Noxae

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

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Disease	Relation	SNOMED_ID
Diagnostic Test for Secondary Adrenocortical Insufficiency	indication
Hypercortisolism	off-label use	47270006
Primary adrenocortical insufficiency	contraindication	373662000

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	4.64	Basic
pKa2	1.71	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Cytochrome P450 11B1, mitochondrial	Enzyme	P15538	C11B1_HUMAN	INHIBITOR	IC50	7.84	CHEMBL	DRUG LABEL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6.10	DRUG MATRIX
Cytochrome P450 11B2, mitochondrial	Enzyme	P19099	C11B2_HUMAN		IC50	7.38	CHEMBL
Cytochrome P450 11B1	Enzyme		C11B1_BOVIN		Ki	6.24	CHEMBL
Cytochrome P450 11B1, mitochondrial	Enzyme		C11B1_RAT		IC50	5.34	CHEMBL

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External reference:

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ID	Source
MYT	PDB_CHEM_ID
002120	NDDF
10389	MMSL
1404	INN_ID
203002	RXNORM
395794007	SNOMEDCT_US
4018788	VUID
4018788	VANDF
4174	PUBCHEM_CID
5107	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Metopirone	HUMAN PRESCRIPTION DRUG LABEL	1	76336-455	CAPSULE, GELATIN COATED	250 mg	ORAL	NDA	32 sections
Metopirone	HUMAN PRESCRIPTION DRUG LABEL	1	76336-455	CAPSULE, GELATIN COATED	250 mg	ORAL	NDA	32 sections
Metopirone	HUMAN PRESCRIPTION DRUG LABEL	1	76336-455	CAPSULE, GELATIN COATED	250 mg	ORAL	NDA	32 sections

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