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

General Information of Drug (ID: DMPI98T)

Drug Name

Doxepin Drug Info

Synonyms

Zonalon; doxepin; Doxepine; Doxepinum [INN-Latin]; Doxepina [INN-Spanish]; Doxepin [USAN]; trans-doxepin; (e)-doxepin; 1668-19-5; Quitaxon; MF 10; UNII-851NLB57HQ; Sinequan; CCRIS 9176; HSDB 3069; Sinequan (TN); Cidoxepina; Cidoxepinum; 851NLB57HQ; 11-(3-(Dimethylamino)propylidene)-6H-dibenz(b,e)oxepine; 11-(3-Dimethylaminopropylidene)-6,11-dihydrodibenz(b,e)oxipin; 11-(3-Dimethylamino-propyliden)-6,11-dihydro-dibenz(b,e)oxipin; N,N-Dimethyldibenz(b,e)oxepin-delta(11(6H),gamma)-propylamine; Cidoxepin [INN]; Curatin; Adapin; Cidoxepin; Doxepina; Doxepinum; Triadapin; Doxepin Hydrochloride; MOLI001594; Adapine (TN); Aponal (TN); Cis-doxepin; Deptran (TN); Doxepin (INN); Doxepin, Hydrochloride; Sinquan (TN); Xepin (TN); Zonalon (TN); Doxepin (Z)-isomer; Cis-N-(3-(6H-Dibenz(b,e)oxepin-11-yliden)propyl)-N,N-dimethylamin; (3E)-3-(6H-benzo[c][1]benzoxepin-11-ylidene)-N,N-dimethylpropan-1-amine; (3E)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimethylpropan-1-amine; (3Z)-3-(6H-benzo[c][1]benzoxepin-11-ylidene)-N,N-di(methyl)propan-1-amine; (3Z)-3-(6H-benzo[c][1]benzoxepin-11-ylidene)-N,N-dimethylpropan-1-amine; (3Z)-3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimethylpropan-1-amine; (Z)-Doxepin; 3-(6H-benzo[c][1]benzoxepin-11-ylidene)-N,N-dimethylpropan-1-amine; 3-Dibenz[b,e]oxepin-11(6H)-ylidene-N,N-dimethyl-1-propanamine; 3-dibenzo[b,e]oxepin-11(6H)-ylidene-N,N-dimethylpropan-1-amine; [11C]doxepin

Indication

Disease Entry	ICD 11	Status	REF
Anxiety		Approved	[1]
Bipolar depression		Approved	[1]
Depression	6A70-6A7Z	Approved	[2]
Insomnia	7A00-7A0Z	Approved	[1]
Pruritus	EC90	Investigative	[1]

Therapeutic Class

Antidepressants

Cross-matching ID

PubChem CID: 667477
CAS Number: CAS 1668-19-5
TTD Drug ID: DMPI98T
VARIDT Drug ID: DR00542
INTEDE Drug ID: DR0544
ACDINA Drug ID: D00626

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	Inhibitor	[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	[5]
Cytochrome P450 2C9 (CYP2C9)	DE5IED8	CP2C9_HUMAN	Approved	[6]
Mephenytoin 4-hydroxylase (CYP2C19)	DEGTFWK	CP2CJ_HUMAN	Approved	[6]
Cytochrome P450 1A2 (CYP1A2)	DEJGDUW	CP1A2_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
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	10.036	5.779	6.508	6.481
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	7.867	5.142	5.52	7.08
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

Anxiety

ICD Disease Classification

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
Cytochrome P450 1A2 (CYP1A2)	DME	CYP1A2	8.46E-01	-6.63E-03	-4.49E-02
Mephenytoin 4-hydroxylase (CYP2C19)	DME	CYP2C19	9.62E-01	2.57E-02	1.10E-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	Doxepin FDA Label
2	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: 1225).
3	Novel therapeutic usage of low-dose doxepin hydrochloride. Expert Opin Investig Drugs. 2007 Aug;16(8):1295-305.
4	The N-demethylation of the doxepin isomers is mainly catalyzed by the polymorphic CYP2C19. Pharm Res. 2002 Jul;19(7):1034-7.
5	Doxepin inhibits CYP2D6 activity in vivo. Pol J Pharmacol. 2004 Jul-Aug;56(4):491-4.
6	Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers. Pharmacogenetics. 2002 Oct;12(7):571-80.