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

General Information of Drug (ID: DM2HN6Q)

Drug Name

Astemizole Drug Info

Synonyms

Alermizol; Astemina; Astemisan; Astemisol; Astemison; Astemizol; Astemizolum; Astesen; Emdar; Esmacen; Fustermizol; Hestazol; Hismanal; Histamen; Histaminos; Histazol; Hubermizol; Kelp; Laridal; Metodih; Metodik; Paralergin; Retolen; Rifedot; Rimbol; Romadin; Simprox; Urdrim; Wareezol; Waruzol; AlacanBrand of Astemizole; Alonga Brand of Astemizole; Astemizol Alonga; Astemizol [German]; Astemizol ratiopharm; Astemizole Alacan Brand; Astemizole Alonga Brand; Astemizole Byk Brand; Astemizole Diba Brand; Astemizole Elfar Brand; Astemizole Esteve Brand; Astemizole Fustery Brand; Astemizole ICN Brand; Astemizole Janssen Brand; Astemizole Lesvi Brand; Astemizole McNeil Brand; Astemizole Medinsa Brand; Astemizole Merck Brand; Astemizole Senosiain Brand; Astemizole Septa Brand; Astemizole Smaller Brand; Astemizole Urbion Brand; Astemizole Vita Brand; Astemizole ratiopharm Brand; Byk Brand of Astemizole; Diba Brand of Astemizole; Elfar Brand of Astemizole; Esteve Brand of Astemizole; Fustery Brand of Astemizole; ICN Brand of Astemizole; Janssen Brand of Astemizole; Lesvi Brand of Astemizole; McNeil Brand of Astemizole; Medinsa Brand of Astemizole; Merck Brand of Astemizole; Ratiopharm Brand of Astemizole; Reig Jofre Brand of Astemizole; Senosiain Brand of Astemizole; Septa Brand of Astemizole; Smaller Brand of Astemizole; Urbion Brand of Astemizole; Vita Brand of Astemizole; R 42512; [3H]Astemizole; Alonga, Astemizol; Astemizol [INN-Spanish]; Astemizolum [INN-Latin]; HISMANAL (TN); Hismanal (TN); MJD-30; Nono-Nastizol A; Novo-mastizol A; Ratiopharm, Astemizol; Astemizole [USAN:BAN:INN]; GNF-PF-2461; Astemizole (JAN/USP/INN); Hestazol, Kelp, Laridal, Retolen, Wareezol, HSBD 6799, BRN 4830190; 1-(p-Fluorobenzyl)-2-((1-(p-methoxyphenethyl)-4-piperidyl)amino)benzimidazole

Indication

Disease Entry	ICD 11	Status	REF
Allergic rhinitis	CA08.0	Withdrawn from market	[1]

Therapeutic Class

Antiallergic Agents

Cross-matching ID

PubChem CID: 2247
ChEBI ID: CHEBI:2896
CAS Number: CAS 68844-77-9
TTD Drug ID: DM2HN6Q
VARIDT Drug ID: DR00705
INTEDE Drug ID: DR0147

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	Withdrawn	[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	Phase 4	[4]
Cytochrome P450 2D6 (CYP2D6)	DECB0K3	CP2D6_HUMAN	Phase 4	[5]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Phase 4	[6]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_HUMAN	Phase 4	[6]
Cytochrome P450 2J2 (CYP2J2)	DERSX5P	CP2J2_HUMAN	Phase 4	[7]

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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 2J2 (CYP2J2)	DME	CYP2J2	7.706	6.315	4.621	7.65
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	10.08	7.207	5.403	9.211
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 rhinitis

ICD Disease Classification

CA08.0

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 2J2 (CYP2J2)	DME	CYP2J2	5.13E-02	2.48E-01	6.60E-01
Cytochrome P450 3A5 (CYP3A5)	DME	CYP3A5	9.57E-01	9.43E-03	1.29E-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: 2603).
2	Histamine H1 receptor induces cytosolic calcium increase and aquaporin translocation in human salivary gland cells. J Pharmacol Exp Ther. 2009 Aug;330(2):403-12.
3	Improving the prediction of the brain disposition for orally administered drugs using BDDCS. Adv Drug Deliv Rev. 2012 Jan;64(1):95-109.
4	Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448.
5	Involvement of multiple human cytochromes P450 in the liver microsomal metabolism of astemizole and a comparison with terfenadine. Br J Clin Pharmacol. 2001 Feb;51(2):133-42.
6	Drug Interactions Flockhart Table
7	Identifying a selective substrate and inhibitor pair for the evaluation of CYP2J2 activity. Drug Metab Dispos. 2012 May;40(5):943-51.