DGIdb - DOXEPIN Drug Record

DOXEPIN chembl:CHEMBL1628227 Approved

Alternate Names:

SINEQUAN
ZONALON
P-3693A
SINEPIN
DOXEPIN

Drug Info:

Drug Indications	hypnotic
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antimigraine agent
Drug Class	antidepressive agents, tricyclic
Year of Approval	1969
Drug Class	antipruritics

(3 More Sources)

Publications:

Stahl, 2008, Selective histamine H1 antagonism: novel hypnotic and pharmacologic actions challenge classical notions of antihistamines., CNS Spectr
Tatsumi et al., 1997, Pharmacological profile of antidepressants and related compounds at human monoamine transporters., Eur. J. Pharmacol.
de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem
Cusack et al., 1994, Binding of antidepressants to human brain receptors: focus on newer generation compounds., Psychopharmacology (Berl.)
Richelson et al., 1984, Antagonism by antidepressants of neurotransmitter receptors of normal human brain in vitro., J. Pharmacol. Exp. Ther.
Kano et al., 2004, Decreased histamine H1 receptor binding in the brain of depressed patients., Eur. J. Neurosci.
Claro et al., 1986, Phosphoinositide hydrolysis mediated by histamine H1-receptors in rat brain cortex., Eur. J. Pharmacol.
Figueiredo et al., 1990, Mechanism of action of doxepin in the treatment of chronic urticaria., Fundam Clin Pharmacol
Tashiro et al., 2004, Central effects of fexofenadine and cetirizine: measurement of psychomotor performance, subjective sleepiness, and brain histamine H1-receptor occupancy using 11C-doxepin positron emission tomography., J Clin Pharmacol
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Tran et al., 1981, [3H]doxepin interactions with histamine H1-receptors and other sites in guinea pig and rat brain homogenates., Eur. J. Pharmacol.
Singh et al., 2007, Novel therapeutic usage of low-dose doxepin hydrochloride., Expert Opin Investig Drugs
Ehlert et al., 1990, The interaction of amitriptyline, doxepin, imipramine and their N-methyl quaternary ammonium derivatives with subtypes of muscarinic receptors in brain and heart., J. Pharmacol. Exp. Ther.
Beil et al., 1988, Interaction of antidepressants and neuroleptics with histamine stimulated parietal cell adenylate cyclase and H+ secretion., Pharmacology
Maj et al., 1977, Doxepin as a blocker of central serotonin receptors., Pharmakopsychiatr Neuropsychopharmakol
Kirchheiner J et al., 2002, Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers., Pharmacogenetics
Duncan et al., 2007, Inhibition of the HERG potassium channel by the tricyclic antidepressant doxepin., Biochem. Pharmacol.
Hicks JK et al., 2013, Clinical Pharmacogenetics Implementation Consortium guideline for CYP2D6 and CYP2C19 genotypes and dosing of tricyclic antidepressants., Clin Pharmacol Ther

DOXEPIN HRH2

Interaction Score: 0.69

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Silenor (SO-101)

PMIDs:
2141000 2897127

Sources:
TdgClinicalTrial
DOXEPIN CHRM4

Interaction Score: 0.62

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
DOXEPIN HTR2B

Interaction Score: 0.61

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 309138

Sources:
TdgClinicalTrial
DOXEPIN HRH1

Interaction Score: 0.38

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
22007643 7855217 6086881 15255990 3011460 2141000 15286093 19179941 11752352 7238574 17685877

Sources:
DTC TdgClinicalTrial TTD
DOXEPIN SLC6A2

Interaction Score: 0.35

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name doxepin nasal solution,Dolorac

Novel drug target Established target

Trial Name Silenor (SO-101)

PMIDs:
19179941 9537821

Sources:
TdgClinicalTrial TEND
DOXEPIN CHRM5

Interaction Score: 0.34

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
DOXEPIN CHRM2

Interaction Score: 0.27

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
DOXEPIN SLC6A4

Interaction Score: 0.26

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name doxepin nasal solution,Dolorac

Novel drug target Established target

Trial Name Silenor (SO-101)

PMIDs:
19179941 9537821

Sources:
TdgClinicalTrial TEND
DOXEPIN HTR2C

Interaction Score: 0.21

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 309138

Sources:
TdgClinicalTrial
DOXEPIN CHRM1

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 19179941 2329499

Sources:
TdgClinicalTrial
DOXEPIN CHRM3

Interaction Score: 0.2

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial
DOXEPIN HTR2A

Interaction Score: 0.14

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 19179941 309138

Sources:
TdgClinicalTrial
DOXEPIN CYP2C19

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23486447 12360109

Sources:
PharmGKB FDA
DOXEPIN KCNH2

Interaction Score: 0.02

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
17560554

Sources:
PharmGKB
DOXEPIN CYP2C9

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12360109

Sources:
PharmGKB
DOXEPIN CYP1A2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
DOXEPIN CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
FDA
DOXEPIN CYP3A4

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

TEND: DOXEPIN
- Version: 01-August-2011
Alternate Names:

DOXEPIN Primary Drug Name

Drug Info:

Drug Class antipruritics

Year of Approval 1969

Drug Class antidepressive agents, tricyclic

Publications:
TdgClinicalTrial: DOXEPIN
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications antimigraine agent

Drug Class Small Molecule

FDA Approval approved

Publications:
DTC: DOXEPIN
- Version: 02-September-2020
Alternate Names:

CHEMBL1628227 ChEMBL Drug ID

Drug Info:

Publications:

de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem

PharmGKB: doxepin

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Kirchheiner J et al., 2002, Contributions of CYP2D6, CYP2C9 and CYP2C19 to the biotransformation of E- and Z-doxepin in healthy volunteers., Pharmacogenetics

Hicks JK et al., 2013, Clinical Pharmacogenetics Implementation Consortium guideline for CYP2D6 and CYP2C19 genotypes and dosing of tricyclic antidepressants., Clin Pharmacol Ther

TTD: Doxepin
- Version: 2020.06.01
Alternate Names:

D06FES TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1628227
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
FDA: Doxepin
- Version: 04-September-2020
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	Silenor (SO-101)

Trial Name	doxepin nasal solution,Dolorac
Novel drug target	Established target
Trial Name	Silenor (SO-101)

DOXEPIN Drug Record

DOXEPIN chembl:CHEMBL1628227 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name Silenor (SO-101)

PMIDs: 2141000 2897127

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 2141000 2329499

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 309138

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 22007643 7855217 6086881 15255990 3011460 2141000 15286093 19179941 11752352 7238574 17685877

Sources: DTC TdgClinicalTrial TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name doxepin nasal solution,Dolorac Novel drug target Established target Trial Name Silenor (SO-101)

PMIDs: 19179941 9537821

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 2141000 2329499

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 2141000 2329499

Sources: TdgClinicalTrial

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name doxepin nasal solution,Dolorac Novel drug target Established target Trial Name Silenor (SO-101)

PMIDs: 19179941 9537821

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 309138

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 2141000 19179941 2329499

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 2141000 2329499

Sources: TdgClinicalTrial

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Trial Name Silenor (SO-101) Novel drug target Established target

PMIDs: 7855217 19179941 309138

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23486447 12360109

Sources: PharmGKB FDA

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 17560554

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12360109

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: FDA

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

TEND: DOXEPIN

Alternate Names: DOXEPIN Primary Drug Name

Drug Info: Drug Class antipruritics Year of Approval 1969 Drug Class antidepressive agents, tricyclic

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name Silenor (SO-101)

PMIDs:
2141000 2897127

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 309138

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
22007643 7855217 6086881 15255990 3011460 2141000 15286093 19179941 11752352 7238574 17685877

Sources:
DTC TdgClinicalTrial TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name doxepin nasal solution,Dolorac

Novel drug target Established target

Trial Name Silenor (SO-101)

PMIDs:
19179941 9537821

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name doxepin nasal solution,Dolorac

Novel drug target Established target

Trial Name Silenor (SO-101)

PMIDs:
19179941 9537821

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 309138

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 19179941 2329499

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 2141000 2329499

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Trial Name Silenor (SO-101)

Novel drug target Established target

PMIDs:
7855217 19179941 309138

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
23486447 12360109

Sources:
PharmGKB FDA

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
17560554

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
12360109

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
FDA

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

DOXEPIN Primary Drug Name

Drug Info:

Drug Class antipruritics

Year of Approval 1969

Drug Class antidepressive agents, tricyclic

Drug Info:

Drug Indications antimigraine agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

CHEMBL1628227 ChEMBL Drug ID

Publications:

de Graaf C et al., 2011, Crystal structure-based virtual screening for fragment-like ligands of the human histamine H(1) receptor., J Med Chem

Alternate Names:

D06FES TTD Drug ID