All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

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

Drug dosage:

Dose	Unit	Route
40	mg	O

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0 %	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

Approvals:

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

FDA Adverse Event Reporting System (Female)

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	70.92	18.41	45	2082	89292	50513705
Dyspnoea	23.84	18.41	63	2064	547545	50055452
Bronchospasm	21.21	18.41	11	2116	14843	50588154

FDA Adverse Event Reporting System (Male)

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	59.50	30.33	22	474	33827	29540204
Eosinophilic granulomatosis with polyangiitis	38.82	30.33	8	488	1378	29572653

FDA Adverse Event Reporting System (Geriatric)

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	70.76	22.58	41	1929	95184	64401578
Eosinophilic granulomatosis with polyangiitis	32.75	22.58	9	1961	2873	64493889
Dyspnoea	27.99	22.58	65	1905	718609	63778153

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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

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

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
Liver function tests abnormal	contraindication	166603001
Insomnia	contraindication	193462001
Disease of liver	contraindication	235856003	DOID:409
Breastfeeding (mother)	contraindication	413712001
Nervousness	contraindication
Tremors	contraindication

🐶 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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	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
Leukotriene B4 receptor 1	GPCR	Q15722	LT4R1_HUMAN		Ki	5.15		PDSP
Bifunctional epoxide hydrolase 2	Enzyme	P34913	HYES_HUMAN		IC50	5.70		CHEMBL
Mitogen-activated protein kinase 1	Kinase	P28482	MK01_HUMAN		IC50	6.27		DRUG MATRIX
Solute carrier family 22 member 2	Transporter	O15244	S22A2_HUMAN		IC50	5.01		CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	5.89		CHEMBL
Multidrug and toxin extrusion protein 2	Transporter	Q86VL8	S47A2_HUMAN		IC50	5.12		CHEMBL
Sodium/bile acid cotransporter	Transporter	Q14973	NTCP_HUMAN		IC50	5.19		CHEMBL
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		Ki	4.87		WOMBAT-PK
Prostaglandin E synthase	Enzyme	O14684	PTGES_HUMAN		IC50	4.74		CHEMBL
Cysteinyl leukotriene receptor 1	GPCR		CLTR1_CAVPO		Ki	9.52		CHEMBL

External reference:

ID	Source
4020987	VUID
N0000148457	NUI
D00411	KEGG_DRUG
4020987	VANDF
C0378466	UMLSCUI
CHEBI:10100	CHEBI
ZLK	PDB_CHEM_ID
CHEMBL603	ChEMBL_ID
DB00549	DRUGBANK_ID
C062735	MESH_SUPPLEMENTAL_RECORD_UI
3322	IUPHAR_LIGAND_ID
7244	INN_ID
XZ629S5L50	UNII
5717	PUBCHEM_CID
114970	RXNORM
178409	MMSL
5701	MMSL
d04053	MMSL
006206	NDDF
108614003	SNOMEDCT_US
386880006	SNOMEDCT_US

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	0904-6646	TABLET, COATED	20 mg	ORAL	NDA	21 sections
Zafirlukast	Human Prescription Drug Label	1	31722-007	TABLET, FILM COATED	10 mg	ORAL	ANDA	19 sections
Zafirlukast	Human Prescription Drug Label	1	31722-008	TABLET, FILM COATED	20 mg	ORAL	ANDA	19 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	49884-549	TABLET, COATED	10 mg	ORAL	NDA	21 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	49884-554	TABLET, COATED	20 mg	ORAL	NDA	21 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	53808-0203	TABLET, FILM COATED	20 mg	ORAL	NDA	22 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	55111-625	TABLET, FILM COATED	10 mg	ORAL	ANDA	22 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	55111-626	TABLET, FILM COATED	20 mg	ORAL	ANDA	22 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	63629-2102	TABLET, COATED	10 mg	ORAL	NDA	21 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	63629-2102	TABLET, COATED	10 mg	ORAL	NDA	21 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	68084-059	TABLET, FILM COATED	20 mg	ORAL	ANDA	22 sections
Zafirlukast	HUMAN PRESCRIPTION DRUG LABEL	1	68151-1977	TABLET, FILM COATED	20 mg	ORAL	ANDA	22 sections