DGIdb - TERFENADINE Drug Record

TERFENADINE chembl:CHEMBL17157

Alternate Names:

ANTIHISTAMINE
TERFENOR FTE
TERFINAX 120
HISTAFEN 120
RMI-9918
TRILUDAN FTE
TERFENADINE
TERFINAX 60
TRILUDAN
SELDANE
HISTAFEN
TERFENOR
TERFEX
TRILUDAN®
TERFENADIN
TERFENADINA
TERFENADINUM
SELDANE®
TERFÉNADINE
(RS)-1-(4-TERT-BUTYLPHENYL)-4-{4-[HYDROXY(DIPHENYL)METHYL]PIPERIDIN-1-YL}-BUTAN-1-OL
drugbank:00342
chembl:CHEMBL17157
pubchem.compound:5405
chemidplus:50679-08-8
rxcui:42330

Drug Info:

Drug Class	anti-allergic agents
Year of Approval	1985
FDA Approval	1985
Drug Class	small molecule
Drug Indications	Anti-Allergic Agents

(3 More Sources)

Publications:

Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med
Perrin MJ et al., 2008, Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels., Mol Pharmacol
Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
Aronov AM, 2005, Predictive in silico modeling for hERG channel blockers., Drug Discov Today
Gessner et al., 2004, Molecular determinants for high-affinity block of human EAG potassium channels by antiarrhythmic agents., Mol. Pharmacol.
Testai et al., 2010, Effects of K openers on the QT prolongation induced by HERG-blocking drugs in guinea-pigs., J. Pharm. Pharmacol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Wood-Baker et al., 1995, A double-blind, placebo controlled study of the effect of the specific histamine H1-receptor antagonist, terfenadine, in chronic severe asthma., Br J Clin Pharmacol
Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.
Rafferty et al., 1987, Terfenadine (Seldane) is a potent and selective histamine H1 receptor antagonist in asthmatic airways., Am. Rev. Respir. Dis.
Kishimoto et al., 1997, Metabolism of epinastine, a histamine H1 receptor antagonist, in human liver microsomes in comparison with that of terfenadine., Res. Commun. Mol. Pathol. Pharmacol.
Phillips et al., 1989, The effect of histamine-H1 receptor antagonism with terfenadine on concentration-related AMP-induced bronchoconstriction in asthma., Clin. Exp. Allergy
Crampette et al., 1996, Inhibition of mediator and cytokine release from dispersed nasal polyp cells by terfenadine., Allergy
Gervasini et al., 2006, The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study., Br J Clin Pharmacol
Wang et al., 2001, Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein., Drug Metab. Dispos.
Kim et al., 1999, Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein., Pharm. Res.
Ohtani et al., 2003, Evaluation of the efficacy of antihistamines using human monocyte-derived dendritic cells stimulated with histamine., J. Am. Acad. Dermatol.
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Yang et al., 1995, Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers., Br. J. Pharmacol.
Crimi et al., 1990, Influence of antihistamine (astemizole) and anticholinergic drugs (ipratropium bromide) on bronchoconstriction induced by substance P., Ann Allergy
Amsellem et al., 1996, Antihistamines and production of granulocyte-macrophage colony-stimulating factor and interleukin-8 by human bronchial epithelial cells in vitro: evaluation of the effects of loratadine and cetirizine., Gen. Pharmacol.

TERFENADINE CD86

Interaction Score: 1.26

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
12894071

Sources:
NCI
TERFENADINE CYP2J2

Interaction Score: 0.88

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
15861034

Sources:
PharmGKB
TERFENADINE KCNA5

Interaction Score: 0.8

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
7670728

Sources:
NCI
TERFENADINE TAC1

Interaction Score: 0.4

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
1696438

Sources:
NCI
TERFENADINE HRH1

Interaction Score: 0.28

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7654486 8001268 2879489 9485522 11752352 2569356

Sources:
TdgClinicalTrial TEND
TERFENADINE CSF2

Interaction Score: 0.22

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8836342

Sources:
NCI
TERFENADINE CXCL8

Interaction Score: 0.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
8919641

Sources:
NCI
TERFENADINE KCNH2

Interaction Score: 0.12

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
14999113 18701618 16253929 15718164 15102940 20636881 11752352

Sources:
DTC PharmGKB
TERFENADINE ABCB1

Interaction Score: 0.09

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16842392 11454724 10213372

Sources:
NCI PharmGKB
TERFENADINE THPO

Interaction Score: 0.06

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TERFENADINE MTOR

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TERFENADINE HTT

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
TERFENADINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528

Sources:
PharmGKB
TERFENADINE GMNN

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

TERFENADINE Primary Drug Name

Drug Info:

Year of Approval 1985

Drug Class anti-allergic agents

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

Drug Info:

Drug Indications Anti-Allergic Agents

Drug Class small molecule

FDA Approval 1985

Publications:

NCI: ANTIHISTAMINE

Version: 14-September-2017

Alternate Names:

C29716 NCI drug code

Drug Info:

Publications:

Wang et al., 2001, Evaluation of the interaction of loratadine and desloratadine with P-glycoprotein., Drug Metab. Dispos.

Gervasini et al., 2006, The effect of CYP2J2, CYP3A4, CYP3A5 and the MDR1 polymorphisms and gender on the urinary excretion of the metabolites of the H-receptor antihistamine ebastine: a pilot study., Br J Clin Pharmacol

Amsellem et al., 1996, Antihistamines and production of granulocyte-macrophage colony-stimulating factor and interleukin-8 by human bronchial epithelial cells in vitro: evaluation of the effects of loratadine and cetirizine., Gen. Pharmacol.

NCI: TERFENADINE

Version: 14-September-2017

Alternate Names:

C29494 NCI drug code

Drug Info:

Publications:

Crampette et al., 1996, Inhibition of mediator and cytokine release from dispersed nasal polyp cells by terfenadine., Allergy

Kim et al., 1999, Interrelationship between substrates and inhibitors of human CYP3A and P-glycoprotein., Pharm. Res.

Yang et al., 1995, Mechanism of block of a human cardiac potassium channel by terfenadine racemate and enantiomers., Br. J. Pharmacol.

PharmGKB: terfenadine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics

Perrin MJ et al., 2008, Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels., Mol Pharmacol

Aronov AM, 2005, Predictive in silico modeling for hERG channel blockers., Drug Discov Today

DTC: TERFENADINE
- Version: 02-September-2020
Alternate Names:

CHEMBL17157 ChEMBL Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL17157
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	-

blocker (inhibitory)
inhibitor (inhibitory)

TERFENADINE Drug Record

TERFENADINE chembl:CHEMBL17157

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 12894071

Sources: NCI

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 15861034

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 7670728

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 1696438

Sources: NCI

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name -

PMIDs: 7654486 8001268 2879489 9485522 11752352 2569356

Sources: TdgClinicalTrial TEND

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8836342

Sources: NCI

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 8919641

Sources: NCI

Interaction Types & Directionality: blocker (inhibitory) inhibitor (inhibitory)

Interaction Info:

PMIDs: 14999113 18701618 16253929 15718164 15102940 20636881 11752352

Sources: DTC PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 16842392 11454724 10213372

Sources: NCI PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9187528

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

TEND: TERFENADINE

Alternate Names: TERFENADINE Primary Drug Name

Drug Info: Year of Approval 1985 Drug Class anti-allergic agents

Publications:

TdgClinicalTrial: TERFENADINE

Alternate Names:

Drug Info: Drug Indications Anti-Allergic Agents Drug Class small molecule FDA Approval 1985

Publications:

NCI: ANTIHISTAMINE

Alternate Names: C29716 NCI drug code

Drug Info:

NCI: TERFENADINE

Alternate Names: C29494 NCI drug code

Drug Info:

PharmGKB: terfenadine

Alternate Names:

Drug Info:

DTC: TERFENADINE

Alternate Names: CHEMBL17157 ChEMBL Drug ID

Interaction Types & Directionality:

n/a

PMIDs:
12894071

Sources:
NCI

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
15861034

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
7670728

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
1696438

Sources:
NCI

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

PMIDs:
7654486 8001268 2879489 9485522 11752352 2569356

Sources:
TdgClinicalTrial TEND

Interaction Types & Directionality:

n/a

PMIDs:
8836342

Sources:
NCI

Interaction Types & Directionality:

n/a

PMIDs:
8919641

Sources:
NCI

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

PMIDs:
14999113 18701618 16253929 15718164 15102940 20636881 11752352

Sources:
DTC PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
16842392 11454724 10213372

Sources:
NCI PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
9187528

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Alternate Names:

TERFENADINE Primary Drug Name

Drug Info:

Year of Approval 1985

Drug Class anti-allergic agents

Drug Info:

Drug Indications Anti-Allergic Agents

Drug Class small molecule

FDA Approval 1985

Alternate Names:

C29716 NCI drug code

Alternate Names:

C29494 NCI drug code

Alternate Names:

CHEMBL17157 ChEMBL Drug ID