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

General Information of Drug (ID: DM4KLPT)

Drug Name

Terfenadine Drug Info

Synonyms

Aldaban; Allerplus; Cyater; Hisfedin; Rapidal; Seldane; Teldane; Teldanex; Terdin; Terfedura; Terfemundin; Terfen; Terfenadina; Terfenadinum; Terfenidine; Terfex; Ternadin; Triludan; Aliud Brand of Terfenadine; Balkis Saft Spezial; Bial Brand of Terfenadine; Cantabria Brand of Terfenadine; Ct Arzneimittel Brand of Terfenadine; Dolorgiet Brand of Terfenadine; Heumann Brand of Terfenadine; Hoechst Brand of Terfenadine; Merck dura Brand of Terfenadine; Mundipharma Brand of Terfenadine; Ratiopharm Brand of Terfenadine; Sigma Tau Brand of Terfenadine; Stadapharm Brand of Terfenadine; Terfenadin AL; Terfenadin Heumann; Terfenadin Stada; Terfenadin von ct; Wolff Brand of Terfenadine; MDL 9918; RMI 9918; RMI9918; T 9652; Ct-Arzneimittel Brand of Terfenadine; MDL-9918; RMI-9918; Seldane (TN); Sigma-Tau Brand of Terfenadine; Teldane (TN); Terfenadin-ratiopharm; Terfenadina [INN-Spanish]; Terfenadinum [INN-Latin]; Triludan (TN); Terfenadine (JAN/USAN/INN); Terfenadine [USAN:BAN:INN:JAN]; Alpha-(4-[1,1-Dimethylethyl]phenyl)-4-[hydroxydiphenylmethyl]-1-piperidinebutanol; Alpha-(p-tert-Butylphenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Alpha-[4-(1,1-Dimethylethyl)phenyl]-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperdinebutanol; Alpha-(4-(1,1-Dimethylethyl)phenyl)-4-(hydroxydiphenylmethyl)-1-piperidinebutanol; Alpha-(4-(1,1-dimethylethyl)phenyl)-4-(hydroxydiphenyl-methyl)-1-piperidine butanol; 1-(4-tert-Butylphenyl)-4-(4-(alpha-hydroxybenzhydryl)piperidino)-butan-1-ol; 1-(4-tert-butylphenyl)-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butan-1-ol; 1-(4-tert-butylphenyl)-4-[4-[hydroxy(diphenyl)methyl]piperidin-1-yl]butan-1-ol; 1-(p-tert-Butylphenyl)-4-(4'-(alpha-hydroxydiphenylmethyl)-1'-piperidyl)butanol; 1-[4-(1,1-dimethylethyl)phenyl]-4-{4-[hydroxy(diphenyl)methyl]piperidin-1-yl}butan-1-ol

Indication

Disease Entry	ICD 11	Status	REF
Allergy	4A80-4A85	Withdrawn from market	[1]

Therapeutic Class

Antihistamines

Cross-matching ID

PubChem CID: 5405
ChEBI ID: CHEBI:9453
CAS Number: CAS 50679-08-8
TTD Drug ID: DM4KLPT
VARIDT Drug ID: DR00755
INTEDE Drug ID: DR1558

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 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Phase 4	[6]
Cytochrome P450 3A5 (CYP3A5)	DEIBDNY	CP3A5_HUMAN	Phase 4	[7]
Cytochrome P450 3A7 (CYP3A7)	DERD86B	CP3A7_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 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 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

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

Allergy

ICD Disease Classification

4A80-4A85

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 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 2C9 (CYP2C9)	DME	CYP2C9	2.35E-01	2.78E-02	2.09E-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: 2608).
2	Small mouse cholangiocytes proliferate in response to H1 histamine receptor stimulation by activation of the IP3/CaMK I/CREB pathway. Am J Physiol Cell Physiol. 2008 Aug;295(2):C499-513.
3	Mammalian drug efflux transporters of the ATP binding cassette (ABC) family in multidrug resistance: A review of the past decade. Cancer Lett. 2016 Jan 1;370(1):153-64.
4	Mechanism-based inhibition of cytochrome P450 3A4 by therapeutic drugs. Clin Pharmacokinet. 2005;44(3):279-304.
5	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.
6	Effects of serum albumin and liver cytosol on CYP2C9- and CYP3A4-mediated drug metabolism. Drug Metab Pharmacokinet. 2002;17(6):522-31.
7	Drug Interactions Flockhart Table