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

Stem definition	Drug id	CAS RN
leukotriene receptor antagonists	2855	107753-78-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: ICI-204219 ICI 204219 ICI 204,219 zafirlukast vanticon	a leukotriene D4 receptor antagonist Molecular weight: 575.68 Formula: C31H33N3O6S CLOGP: 7.09 LIPINSKI: 2 HAC: 9 HDO: 2 TPSA: 115.73 ALOGS: -5.78 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

ICI-204219
ICI 204219
ICI 204,219
zafirlukast
vanticon

a leukotriene D4 receptor antagonist

Molecular weight: 575.68
Formula: C31H33N3O6S
CLOGP: 7.09
LIPINSKI: 2
HAC: 9
HDO: 2
TPSA: 115.73
ALOGS: -5.78
ROTB: 8

Status: OFP

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

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

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Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.99 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Sept. 26, 1996	FDA	PAR PHARM INC

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
Asthma	73.80	19.27	50	2267	127511	63359194
Dyspnoea	25.95	19.27	67	2250	661246	62825459
Bronchospasm	21.10	19.27	11	2306	17269	63469436

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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
Asthma	70.45	32.19	27	602	42629	34913673
Eosinophilic granulomatosis with polyangiitis	35.37	32.19	8	621	1979	34954323

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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
Asthma	80.24	21.09	49	2209	135046	79607084
Dyspnoea	32.20	21.09	73	2185	856952	78885178
Eosinophilic granulomatosis with polyangiitis	31.30	21.09	9	2249	3651	79738479
Chest discomfort	23.55	21.09	24	2234	138020	79604110
Wheezing	23.10	21.09	22	2236	116642	79625488

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	R03DC01	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER SYSTEMIC DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES Leukotriene receptor antagonists
CHEBI has role	CHEBI:49159	leukotriene antagonists
CHEBI has role	CHEBI:65023	anti-asthmatic agents
FDA EPC	N0000175777	Leukotriene Receptor Antagonist
FDA MoA	N0000000083	Leukotriene Receptor Antagonists
FDA MoA	N0000185504	Cytochrome P450 2C9 Inhibitors
MeSH PA	D018927	Anti-Asthmatic Agents
MeSH PA	D006727	Hormone Antagonists
MeSH PA	D020024	Leukotriene Antagonists
MeSH PA	D019141	Respiratory System Agents

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

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Disease	Relation	SNOMED_ID	DOID
Asthma	indication	195967001	DOID:2841
Asthma management	indication	406162001
Suicidal thoughts	contraindication	6471006
Hallucinations	contraindication	7011001
Mood swings	contraindication	18963009
Cirrhosis of liver	contraindication	19943007	DOID:5082
Feeling agitated	contraindication	24199005
Depressive disorder	contraindication	35489007
Anxiety	contraindication	48694002
Dream disorder	contraindication	85418005

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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	3.84	acidic
pKa2	10.83	acidic

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
Cysteinyl leukotriene receptor 1	GPCR	Q9Y271	CLTR1_HUMAN	ANTAGONIST	Ki	9.50	CHEMBL	CHEMBL
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	6.11	DRUG MATRIX
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	5.65	DRUG MATRIX
Cytosolic phospholipase A2	Enzyme	P47712	PA24A_HUMAN		IC50	4.07	CHEMBL
Epidermal growth factor receptor	Kinase	P00533	EGFR_HUMAN		IC50	5.24	DRUG MATRIX
Peroxisome proliferator-activated receptor gamma	Nuclear hormone receptor	P37231	PPARG_HUMAN		EC50	5.61	CHEMBL
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	5.42	DRUG MATRIX
Mitogen-activated protein kinase 3	Kinase	P27361	MK03_HUMAN		IC50	5.36	DRUG MATRIX
Cysteinyl leukotriene receptor 2	GPCR	Q9NS75	CLTR2_HUMAN	ANTAGONIST	IC50	5.15	IUPHAR
Mitogen-activated protein kinase 14	Kinase	Q16539	MK14_HUMAN		IC50	6.45	DRUG MATRIX

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External reference:

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ID	Source
ZLK	PDB_CHEM_ID
006206	NDDF
108614003	SNOMEDCT_US
114970	RXNORM
178409	MMSL
3322	IUPHAR_LIGAND_ID
386880006	SNOMEDCT_US
4020987	VUID
4020987	VANDF
5701	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Accolate	HUMAN PRESCRIPTION DRUG LABEL	1	49884-589	TABLET, COATED	10 mg	ORAL	NDA	23 sections
Accolate	HUMAN PRESCRIPTION DRUG LABEL	1	49884-589	TABLET, COATED	10 mg	ORAL	NDA	23 sections
Accolate	HUMAN PRESCRIPTION DRUG LABEL	1	49884-590	TABLET, COATED	20 mg	ORAL	NDA	23 sections
Accolate	HUMAN PRESCRIPTION DRUG LABEL	1	49884-590	TABLET, COATED	20 mg	ORAL	NDA	23 sections
ACCOLATE	HUMAN PRESCRIPTION DRUG LABEL	1	53808-0203	TABLET, FILM COATED	20 mg	ORAL	NDA	22 sections
ACCOLATE	HUMAN PRESCRIPTION DRUG LABEL	1	64380-177	TABLET, FILM COATED	10 mg	ORAL	NDA	12 sections
ACCOLATE	HUMAN PRESCRIPTION DRUG LABEL	1	64380-178	TABLET, FILM COATED	20 mg	ORAL	NDA	12 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6646	TABLET, COATED	20 mg	ORAL	NDA	21 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	16571-654	TABLET	10 mg	ORAL	ANDA	23 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	16571-655	TABLET	20 mg	ORAL	ANDA	23 sections

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