DGIdb - PROPAFENONE Drug Record

PROPAFENONE chembl:CHEMBL631 Approved

Alternate Names:

GNF-PF-4594
PROPAFENONE
RYTHMOL
PROPAFENONUM
1-(2-(2-HYDROXY-3-(PROPYLAMINO)PROPOXY)PHENYL)-3-PHENYL-1-PROPANONE
2-(2'-HYDROXY-3'-PROPYLAMINOPROPOXY)-OMEGA-PHENYLPROPIOPHENONE
PROPAFENONA
ARYTHMOL®
RYTHMOL®
chembl:CHEMBL631
pubchem.compound:4932
drugbank:01182
rxcui:8754
chemidplus:54063-53-5

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antiarrythmic agent
Year of Approval	1989
Drug Class	anti-arrhythmia agents

(4 More Sources)

Publications:

Kroemer HK et al., 1989, Stereoselective disposition and pharmacologic activity of propafenone enantiomers., Circulation
Klein K et al., 2007, A natural variant of the heme-binding signature (R441C) resulting in complete loss of function of CYP2D6., Drug Metab Dispos
Toscano C et al., 2006, A silent mutation (2939G>A, exon 6; CYP2D6*59) leading to impaired expression and function of CYP2D6., Pharmacogenet Genomics
Chen B et al., 2003, Influence of CYP2D6*10B genotype on pharmacokinetics of propafenone enantiomers in Chinese subjects., Acta Pharmacol Sin
Cai WM et al., 2002, Effect of CYP2D6*10 genotype on propafenone pharmacodynamics in Chinese patients with ventricular arrhythmia., Acta Pharmacol Sin
Arias et al., 2003, Effects of propafenone and its main metabolite, 5-hydroxypropafenone, on HERG channels., Cardiovasc. Res.
Mergenthaler et al., 2001, Blocking effects of the antiarrhythmic drug propafenone on the HERG potassium channel., Naunyn Schmiedebergs Arch. Pharmacol.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Katchman AN et al., 2006, Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs., J Pharmacol Exp Ther
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Edrich T et al., 2005, State-dependent block of human cardiac hNav1.5 sodium channels by propafenone., J Membr Biol
McLeod AA et al., 1984, Demonstration of beta adrenoceptor blockade by propafenone hydrochloride: clinical pharmacologic, radioligand binding and adenylate cyclase activation studies., J Pharmacol Exp Ther
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

PROPAFENONE COP1

Interaction Score: 1.16

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
PROPAFENONE SCN5A

Interaction Score: 0.39

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name propafenone hydrochloride,Rythmol

Novel drug target Established target

PMIDs:
17016423 17139284 16463141

Sources:
TdgClinicalTrial TEND PharmGKB
PROPAFENONE KCNA5

Interaction Score: 0.31

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology
PROPAFENONE ADRB1

Interaction Score: 0.13

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
6141285

Sources:
GuideToPharmacology
PROPAFENONE KCNH2

Interaction Score: 0.12

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name propafenone hydrochloride,Rythmol

Novel drug target Established target

PMIDs:
12618228 11330342 11752352 16278312

Sources:
TdgClinicalTrial TEND PharmGKB
PROPAFENONE ADRB2

Interaction Score: 0.08

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
6141285

Sources:
GuideToPharmacology
PROPAFENONE CYP2D6

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
2713973 17460029 17001296 14653957 12421483

Sources:
PharmGKB FDA
PROPAFENONE MTOR

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROPAFENONE DRD1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
PROPAFENONE ABCB1

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB
PROPAFENONE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528

Sources:
PharmGKB

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

PROPAFENONE Primary Drug Name

Drug Info:

Drug Class anti-arrhythmia agents

Year of Approval 1989

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

Drug Info:

Drug Indications antiarrythmic agent

Drug Class Small Molecule

FDA Approval approved

Publications:

PharmGKB: propafenone

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Katchman AN et al., 2006, Comparative evaluation of HERG currents and QT intervals following challenge with suspected torsadogenic and nontorsadogenic drugs., J Pharmacol Exp Ther

Kroemer HK et al., 1989, Stereoselective disposition and pharmacologic activity of propafenone enantiomers., Circulation

Chen B et al., 2003, Influence of CYP2D6*10B genotype on pharmacokinetics of propafenone enantiomers in Chinese subjects., Acta Pharmacol Sin

GuideToPharmacology: 135650856
- Version: 29-September-2020
Alternate Names:

PROPAFENONE GuideToPharmacology Ligand Name

Drug Info:

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

CHEMBL631 ChEMBL Drug ID

Drug Info:

Publications:
TTD: Propafenone
- Version: 2020.06.01
Alternate Names:

D0J2KV TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL631
- Version: ChEMBL_27
Alternate Names:

Drug Info:

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

Drug Info:

Publications:

Trial Name	propafenone hydrochloride,Rythmol
Novel drug target	Established target

Direct Interaction?	False
Endogenous Drug?	False
Specific Action of the Ligand	None

Specific Action of the Ligand	Antagonist
Endogenous Drug?	False
Direct Interaction?	True

PROPAFENONE Drug Record

PROPAFENONE chembl:CHEMBL631 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name propafenone hydrochloride,Rythmol Novel drug target Established target

PMIDs: 17016423 17139284 16463141

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Direct Interaction? False Endogenous Drug? False Specific Action of the Ligand None

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? True

PMIDs: 6141285

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name propafenone hydrochloride,Rythmol Novel drug target Established target

PMIDs: 12618228 11330342 11752352 16278312

Sources: TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info: Specific Action of the Ligand Antagonist Endogenous Drug? False Direct Interaction? False

PMIDs: 6141285

Sources: GuideToPharmacology

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 2713973 17460029 17001296 14653957 12421483

Sources: PharmGKB FDA

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: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9187528

Sources: PharmGKB

TEND: PROPAFENONE

Alternate Names: PROPAFENONE Primary Drug Name

Drug Info: Drug Class anti-arrhythmia agents Year of Approval 1989

Publications:

TdgClinicalTrial: PROPAFENONE

Alternate Names:

Drug Info: Drug Indications antiarrythmic agent Drug Class Small Molecule FDA Approval approved

Publications:

PharmGKB: propafenone

Alternate Names:

Drug Info:

GuideToPharmacology: 135650856

Alternate Names: PROPAFENONE GuideToPharmacology Ligand Name

Drug Info:

Publications:

DTC: PROPAFENONE

Alternate Names: CHEMBL631 ChEMBL Drug ID

Drug Info:

Publications:

TTD: Propafenone

Alternate Names: D0J2KV TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL631

Alternate Names:

Drug Info:

Publications:

FDA: Propafenone

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name propafenone hydrochloride,Rythmol

Novel drug target Established target

PMIDs:
17016423 17139284 16463141

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand None

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? True

PMIDs:
6141285

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name propafenone hydrochloride,Rythmol

Novel drug target Established target

PMIDs:
12618228 11330342 11752352 16278312

Sources:
TdgClinicalTrial TEND PharmGKB

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
6141285

Sources:
GuideToPharmacology

Interaction Types & Directionality:

n/a

PMIDs:
2713973 17460029 17001296 14653957 12421483

Sources:
PharmGKB FDA

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:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9187528

Sources:
PharmGKB

Alternate Names:

PROPAFENONE Primary Drug Name

Drug Info:

Drug Class anti-arrhythmia agents

Year of Approval 1989

Drug Info:

Drug Indications antiarrythmic agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

PROPAFENONE GuideToPharmacology Ligand Name

Alternate Names:

CHEMBL631 ChEMBL Drug ID

Alternate Names:

D0J2KV TTD Drug ID