Details of the Drug-Related molecule(s) Expression Atlas

General Information of Drug (ID: DMHNQOG)

Drug Name

Zafirlukast Drug Info

Synonyms

Accolate; Accoleit; Aeronix; Olmoran; Respix; Zafirst; AstraZeneca brand of zafirlukast; Menarini brand of zafirlukast; Novartis brand of zafirlukast; Zeneca brand of zafirkulast; Accolate (TN); Accoleit (TN); Vanticon (TN); Zafirlukast [USAN:BAN:INN]; Accolate, Accoleit, Vanticon, Zafirlukast; Zafirlukast (JAN/USAN/INN); Cyclopentyl N-[3-[[2-methoxy-4-[(2-methylphenyl)sulfonylcarbamoyl]phenyl]methyl]-1-methylindol-5-yl]carbamate; Cyclopentyl 3-(2-methoxy-4-((o-tolylsulfonyl)carbamoyl)benzyl)-1-methylindole-5-carbamate; Cyclopentyl 3-[2-methoxy-4-(2-methylphenylsulfonylcarbamoyl)benzyl]-1-methyl-1H-indol-5-ylcarbamate; Cyclopentyl [3-(2-methoxy-4-{[(2-methylphenyl)sulfonyl]carbamoyl}benzyl)-1-methyl-1H-indol-5-yl]carbamate; Cyclopentyl (1-methyl-3-{[2-(methyloxy)-4-({[(2-methylphenyl)sulfonyl]amino}carbonyl)phenyl]methyl}-1H-indol-5-yl)carbamate; Carbamic acid, (3-((2-methoxy-4-((((2-methylphenyl)sulfonyl)amino)carbonyl)phenyl)methyl)-1-methyl-1H-indol-5-yl)-, cyclopentyl ester; 4-(5-cyclopentyloxy-carbonylamino-1-methyl-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; 4-(5-cyclopentyloxycarbonylamino-1-methyl-1H-indol-3-ylmethyl)-3-methoxy-N-o-tolylsulfonylbenzamide; 4-(5-cyclopentyloxycarbonylamino-2-methylindol-3-yl-methyl)-3-methoxy-N-O-tolylsulfonylbenzamide

Indication

Disease Entry	ICD 11	Status	REF
Asthma	CA23	Approved	[1]

Therapeutic Class

Antiasthmatic Agents

Cross-matching ID

PubChem CID: 5717
ChEBI ID: CHEBI:10100
CAS Number: CAS 107753-78-6
TTD Drug ID: DMHNQOG
VARIDT Drug ID: DR00872
INTEDE Drug ID: DR1723
ACDINA Drug ID: D00737

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Leukotriene CysLT1 receptor (CYSLTR1)	TTGKOY9	CLTR1_HUMAN	Antagonist	[2]

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Drug-Metabolizing Enzyme (DME)

DME Name	DME ID	UniProt ID	Highest Status	REF
Cytochrome P450 3A4 (CYP3A4)	DE4LYSA	CP3A4_HUMAN	Approved	[3]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[4]
Cytochrome P450 2C8 (CYP2C8)	DES5XRU	CP2C8_HUMAN	Approved	[5]
Prostaglandin G/H synthase 1 (COX-1)	DE073H6	PGH1_HUMAN	Approved	[6]

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The Expression Level of Molecule(s) in Normal Tissue of Major ADME-Related Organs

Molecule	Molecule Type	Gene Name	Liver	Colon	Kidney	Small Intestine
Leukotriene CysLT1 receptor (CYSLTR1)	DTT	CYSLTR1	3.233	3.733	-0.152	3.797
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	9.791	3.744	3.413	1.609
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	11.76	5.931	6.164	9.423
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089
Prostaglandin G/H synthase 1 (COX-1)	DME	PTGS1	6.09	7.747	6.04	7.023

Molecule Expression Atlas in Normal Tissue of Major ADME-related organs

The Expression Level of Molecule(s) between Disease Section and Healthy Individual Tissue

ICD Disease Classification

12 Disease of the respiratory system

Disease Class

ICD-11: CA23 Asthma

The Studied Tissue

Nasal and bronchial airway

The Studied Disease

Asthma [ICD-11:CA23]

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Leukotriene CysLT1 receptor (CYSLTR1)	DTT	CYSLTR1	1.96E-02	0.24	0.43
Cytochrome P450 2C8 (CYP2C8)	DME	CYP2C8	2.93E-03	-2.19E-01	-4.49E-01
Cytochrome P450 2C9 (CYP2C9)	DME	CYP2C9	2.25E-03	-4.98E-01	-6.49E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	6.90E-01	2.35E-02	7.88E-02
Prostaglandin G/H synthase 1 (COX-1)	DME	PTGS1	5.11E-09	5.07E-01	9.56E-01

Molecular Expression Atlas between Disease Section and Healthy Individual Tissue

References

1	URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3322).
2	Inhibitory effects of zafirlukast on respiratory bursts of human neutrophils. Drugs Exp Clin Res. 2002;28(4):133-45.
3	Fluconazole but not the CYP3A4 inhibitor, itraconazole, increases zafirlukast plasma concentrations. Eur J Clin Pharmacol. 2012 May;68(5):681-8.
4	Potential of pranlukast and zafirlukast in the inhibition of human liver cytochrome P450 enzymes. Xenobiotica. 2004 May;34(5):429-38.
5	Pioglitazone is metabolised by CYP2C8 and CYP3A4 in vitro: potential for interactions with CYP2C8 inhibitors. Basic Clin Pharmacol Toxicol. 2006 Jul;99(1):44-51.
6	Substrates, inducers, inhibitors and structure-activity relationships of human Cytochrome P450 2C9 and implications in drug development. Curr Med Chem. 2009;16(27):3480-675.