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

General Information of Drug (ID: DMKMWQG)

Drug Name

Olopatadine Drug Info

Synonyms

Allelock; Opatanol; Pataday; Patanase; Patanol; OLOPATADINE HCl; OLOPATADINE HYDROCHLORIDE; ALO4943A; HCl of KW 4679; KW 4679; O0361; AL-4943A; ALO-4943A; Allelock (TN); KW-4679; KW-4943A; Olopatadine [INN:BAN]; Pataday (TN); Patanase (TN); Patanol S (TN); {(11Z)-11-[3-(dimethylamino)propylidene]-6,11-dihydrodibenzo[b,e]oxepin-2-yl}acetic acid; 11-((Z)-3-(Dimethylamino)propylidene)-6,11-dihydrodibenz(b,e)oxepin-2-acetic acid; 11-((Z)-3-(Dimethylamino)propylidene)-6,11-dihydrodibenz(b,e)oxepin-2-acetic acid hydrochloride; 11-((Z)-3-(Dimethylamino)propylidene)-6,11-dihydrodibenz(b,e)oxepin-2-acetic acid, hydrochloride; 11-(3-(dimethylamino)propylidene)-6,11-dihydrodibenz(b,e)oxepin-2-acetic acid; 2-[(11Z)-11-[3-(dimethylamino)propylidene]-6H-benzo[c][1]benzoxepin-2-yl]acetic acid; 2-[(11Z)-11-[3-(dimethylamino)propylidene]-6H-benzo[c][1]benzoxepin-2-yl]acetic acid hydrochloride

Indication

Disease Entry	ICD 11	Status	REF
Allergic conjunctivitis	9A60.02	Approved	[1]
Allergic rhinitis	CA08.0	Approved	[2]
Seasonal allergic rhinitis	CA08.01	Approved	[2]
Ocular allergy	4A81	Phase 3	[1]

Therapeutic Class

Antiallergic Agents

Cross-matching ID

PubChem CID: 5281071
ChEBI ID: CHEBI:94593
CAS Number: CAS 113806-05-6
TTD Drug ID: DMKMWQG
VARIDT Drug ID: DR01357
INTEDE Drug ID: DR1192

Molecule(s) Related to This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Histamine H1 receptor (H1R)	TTTIBOJ	HRH1_HUMAN	Antagonist	[3]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[4]

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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	[5]
Dimethylaniline oxidase 3 (FMO3)	DEP76YL	FMO3_HUMAN	Approved	[]
Dimethylaniline oxidase 1 (FMO1)	DEJ73Q9	FMO1_HUMAN	Approved	[]

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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
Histamine H1 receptor (H1R)	DTT	HRH1	5.972	5.7	5.816	6.002
P-glycoprotein 1 (ABCB1)	DTP	P-GP	7.009	6.988	7.442	8.135
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	11.692	6.58	4.984	9.089

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

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

The Studied Disease

Allergic conjunctivitis

ICD Disease Classification

9A60.02

Molecule Name	Molecule Type	Gene Name	p-value	Fold-Change	Z-score
Histamine H1 receptor (H1R)	DTT	HRH1	6.74E-01	0.13	0.43
P-glycoprotein 1 (ABCB1)	DTP	P-GP	6.54E-01	1.95E-01	4.04E-01
Cytochrome P450 3A4 (CYP3A4)	DME	CYP3A4	1.76E-01	1.26E-01	8.27E-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: 7249).
2	Olopatadine FDA Label
3	Emerging drugs for ocular allergy. Expert Opin Emerg Drugs. 2005 Aug;10(3):505-20.
4	Human intestinal transporter database: QSAR modeling and virtual profiling of drug uptake, efflux and interactions. Pharm Res. 2013 Apr;30(4):996-1007.
5	Effects of olopatadine, a new antiallergic agent, on human liver microsomal cytochrome P450 activities. Drug Metab Dispos. 2002 Dec;30(12):1504-11.