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

General Information of Drug (ID: DMX0K3Q)

Drug Name

Epinastine Drug Info

Synonyms

Epinastina; Epinastinum; Purivist; Epinastina [Spanish]; Epinastine [INN]; Epinastinum [Latin]; WAL 80; WAL 801; WAL 801CL; Elestat (TN); Epinastine (INN); Purivist (TN); Relestat (TN); WAL-80 Cl; (+-)-Epinastine; 3-Amino-9,13b-dihydro-1H-dibenz(c,f)imidazo(1,5-a)azepine; 3-amino-9,13b-dihydro-1H-benz(c,f)imidazo(1,5a)azepine; 9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine

Indication

Disease Entry	ICD 11	Status	REF
Allergic conjunctivitis	9A60.02	Approved	[1]

Therapeutic Class

Antihistamines

Cross-matching ID

PubChem CID: 3241
ChEBI ID: CHEBI:51032
CAS Number: CAS 80012-43-7
TTD Drug ID: DMX0K3Q
VARIDT Drug ID: DR01010
INTEDE Drug ID: DR0587

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	[2]

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Drug Transporter (DTP)

DTP Name	DTP ID	UniProt ID	Highest Status	REF
P-glycoprotein 1 (ABCB1)	DTUGYRD	MDR1_HUMAN	Approved	[3]

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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	[4]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Approved	[4]
Cytochrome P450 2B6 (CYP2B6)	DEPKLMQ	CP2B6_HUMAN	Approved	[4]

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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 2D6 (CYP2D6)	DME	CYP2D6	3.307	5.005	3.921	5.327
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 2B6 (CYP2B6)	DME	CYP2B6	4.32E-01	4.39E-02	4.30E-01
Cytochrome P450 2D6 (CYP2D6)	DME	CYP2D6	8.70E-01	2.98E-02	1.22E-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: 7176).
2	Influence of epinastine hydrochloride, an H1-receptor antagonist, on the function of mite allergen-pulsed murine bone marrow-derived dendritic cell... Mediators Inflamm. 2009;2009:738038.
3	Influx and efflux transport of H1-antagonist epinastine across the blood-brain barrier. Drug Metab Dispos. 2004 May;32(5):519-24.
4	Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine. Res Commun Mol Pathol Pharmacol. 1997 Dec;98(3):273-92.