DGIdb - ASTEMIZOLE Drug Record

ASTEMIZOLE chembl:CHEMBL296419

Alternate Names:

ASTEMIZOLE
GNF-PF-2461
R-43512
POLLON-EZE
HISMANAL
1-(P-FLUOROBENZYL)-2-{[1-(P-METHOXYPHENETHYL)-4-PIPERIDYL]AMINO}BENZIMIDAZOLE
1-(P-FLUOROBENZYL)-2-({1-[2-(P-METHOXYPHENYL)ETHYL]PIPERID-4-YL}AMINO)BENZIMIDAZOLE
rxcui:42328
pubchem.compound:2247
chemidplus:68844-77-9
drugbank:00637
chembl:CHEMBL296419

Drug Info:

Year of Approval	1988
Drug Class	anti-allergic agents
FDA Approval	1988
Drug Class	small molecule
Drug Indications	Anti-Allergic Agents

(2 More Sources)

Publications:

Zhou et al., 1999, Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole., J. Cardiovasc. Electrophysiol.
Taglialatela et al., 1999, Cardiac ion channels and antihistamines: possible mechanisms of cardiotoxicity., Clin. Exp. Allergy
Grzelewska-Rzymowska et al., 2001, [The effect of second generation histamine antagonists on the heart]., Pneumonol Alergol Pol
Chachin et al., 1999, Epinastine, a nonsedating histamine H1 receptor antagonist, has a negligible effect on HERG channel., Eur. J. Pharmacol.
Chiu et al., 2004, Validation of a [3H]astemizole binding assay in HEK293 cells expressing HERG K+ channels., J. Pharmacol. Sci.
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
Roden DM, 2004, Drug-induced prolongation of the QT interval., N Engl J Med
Gozalbes R et al., 2013, Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches., Bioorg Med Chem
Howarth et al., 1984, Astemizole, a potent histamine H1-receptor antagonist: effect in allergic rhinoconjunctivitis, on antigen and histamine induced skin weal responses and relationship to serum levels., Br J Clin Pharmacol
Krstenansky et al., 1987, Astemizole: a long-acting, nonsedating antihistamine., Drug Intell Clin Pharm
Llenas et al., 1999, Cardiotoxicity of histamine and the possible role of histamine in the arrhythmogenesis produced by certain antihistamines., Drug Saf
Salata et al., 1995, Cardiac electrophysiological actions of the histamine H1-receptor antagonists astemizole and terfenadine compared with chlorpheniramine and pyrilamine., Circ. Res.
Kaliner et al., Non-sedating antihistamines., Allergy Proc
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Richards et al., 1984, Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy., Drugs
Cavero et al., 1999, Preclinical in vitro cardiac electrophysiology: a method of predicting arrhythmogenic potential of antihistamines in humans?, Drug Saf
Kong X et al., 2014, Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2., J Med Chem
Lee SS et al., 2005, Identification and functional characterization of novel CYP2J2 variants: G312R variant causes loss of enzyme catalytic activity., Pharmacogenet Genomics
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

ASTEMIZOLE EED

Interaction Score: 9.51

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25369470

Sources:
DTC
ASTEMIZOLE CYP2J2

Interaction Score: 0.95

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
15861034

Sources:
PharmGKB
ASTEMIZOLE HPSE

Interaction Score: 0.73

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
23415087

Sources:
DTC
ASTEMIZOLE HRH1

Interaction Score: 0.42

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
6146346 2892659 10597866 8001268 3147222 11752352 6204835 10597865

Sources:
TdgClinicalTrial ChemblInteractions TEND
ASTEMIZOLE KCNH2

Interaction Score: 0.14

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10376921 10444235 11575008 10422790 15272206 18701618 16253929 15718164 14999113

Sources:
PharmGKB
ASTEMIZOLE PPARD

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ASTEMIZOLE ABCB1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
ASTEMIZOLE TP53

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ASTEMIZOLE IDH1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ASTEMIZOLE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528

Sources:
PharmGKB
ASTEMIZOLE GMNN

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ASTEMIZOLE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
ASTEMIZOLE AR

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

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

ASTEMIZOLE Primary Drug Name

Drug Info:

Drug Class anti-allergic agents

Year of Approval 1988

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

Drug Info:

Drug Indications Anti-Allergic Agents

Drug Class small molecule

FDA Approval 1988

Publications:

DTC: ASTEMIZOLE

Version: 02-September-2020

Alternate Names:

CHEMBL296419 ChEMBL Drug ID

Drug Info:

Publications:

Kong X et al., 2014, Astemizole arrests the proliferation of cancer cells by disrupting the EZH2-EED interaction of polycomb repressive complex 2., J Med Chem

Gozalbes R et al., 2013, Hit identification of novel heparanase inhibitors by structure- and ligand-based approaches., Bioorg Med Chem

PharmGKB: astemizole

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

Zhou et al., 1999, Block of HERG potassium channels by the antihistamine astemizole and its metabolites desmethylastemizole and norastemizole., J. Cardiovasc. Electrophysiol.

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

ChemblDrugs: chembl:CHEMBL296419
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL296419
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Novel drug target	Established target
Trial Name	-
Direct Interaction	yes

blocker (inhibitory)
inhibitor (inhibitory)

ASTEMIZOLE Drug Record

ASTEMIZOLE chembl:CHEMBL296419

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25369470

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 15861034

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 23415087

Sources: DTC

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Novel drug target Established target Trial Name - Direct Interaction yes

PMIDs: 6146346 2892659 10597866 8001268 3147222 11752352 6204835 10597865

Sources: TdgClinicalTrial ChemblInteractions TEND

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

Interaction Info:

PMIDs: 10376921 10444235 11575008 10422790 15272206 18701618 16253929 15718164 14999113

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: DTC

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: 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: 9187528

Sources: 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

TEND: ASTEMIZOLE

Alternate Names: ASTEMIZOLE Primary Drug Name

Drug Info: Drug Class anti-allergic agents Year of Approval 1988

Publications:

TdgClinicalTrial: ASTEMIZOLE

Alternate Names:

Drug Info: Drug Indications Anti-Allergic Agents Drug Class small molecule FDA Approval 1988

Publications:

DTC: ASTEMIZOLE

Alternate Names: CHEMBL296419 ChEMBL Drug ID

Drug Info:

PharmGKB: astemizole

Alternate Names:

Drug Info:

ChemblDrugs: chembl:CHEMBL296419

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL296419

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
25369470

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
15861034

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
23415087

Sources:
DTC

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Novel drug target Established target

Trial Name -

Direct Interaction yes

PMIDs:
6146346 2892659 10597866 8001268 3147222 11752352 6204835 10597865

Sources:
TdgClinicalTrial ChemblInteractions TEND

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

PMIDs:
10376921 10444235 11575008 10422790 15272206 18701618 16253929 15718164 14999113

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
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:
9187528

Sources:
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

Alternate Names:

ASTEMIZOLE Primary Drug Name

Drug Info:

Drug Class anti-allergic agents

Year of Approval 1988

Drug Info:

Drug Indications Anti-Allergic Agents

Drug Class small molecule

FDA Approval 1988

Alternate Names:

CHEMBL296419 ChEMBL Drug ID