DGIdb - MIBEFRADIL Drug Record

MIBEFRADIL chembl:CHEMBL45816

Alternate Names:

POSICOR
MIBEFRADIL
POSICOR 100
POSICOR 50
POSICOR®
RO-405967-001
chemidplus:116644-53-2
drugbank:01388
pubchem.compound:60663
rxcui:83213
chembl:CHEMBL45816

Drug Info:

Drug Groups	investigational
Drug Categories	agents causing hyperkalemia
Drug Categories	antiarrhythmic agents
Drug Categories	bradycardia-causing agents
Drug Categories	calcium-regulating hormones and agents
Drug Categories	cytochrome p-450 cyp1a2 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a5 inhibitors
Drug Categories	cytochrome p-450 cyp3a5 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a7 inhibitors
Drug Categories	cytochrome p-450 cyp3a7 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 substrates
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	moderate risk qtc-prolonging agents
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	qtc prolonging agents
Drug Categories	vasodilating agents

(2 More Sources)

Publications:

Jiménez et al., 2000, Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels., Neuropharmacology
Mocanu et al., 1999, Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism., Cardiovasc Drugs Ther
Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology
Clozel et al., 1997, Discovery and main pharmacological properties of mibefradil (Ro 40-5967), the first selective T-type calcium channel blocker., J Hypertens Suppl
Massie, 1997, Mibefradil: a selective T-type calcium antagonist., Am. J. Cardiol.
McNulty et al., 2004, State-dependent mibefradil block of Na+ channels., Mol. Pharmacol.
Monteil et al., 2000, Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels., J. Biol. Chem.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Moosmang et al., 2006, Antihypertensive effects of the putative T-type calcium channel antagonist mibefradil are mediated by the L-type calcium channel Cav1.2., Circ. Res.
Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
Coste et al., 2007, Pharmacological dissection and distribution of NaN/Nav1.9, T-type Ca2+ currents, and mechanically activated cation currents in different populations of DRG neurons., J. Gen. Physiol.
Perez-Reyes, 2004, Paradoxical role of T-type calcium channels in coronary smooth muscle., Mol. Interv.
Cribbs et al., 1998, Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family., Circ. Res.
Brueggemann et al., 2005, Low voltage-activated calcium channels in vascular smooth muscle: T-type channels and AVP-stimulated calcium spiking., Am. J. Physiol. Heart Circ. Physiol.
Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

MIBEFRADIL ANO1

Interaction Score: 0.79

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CACNB3

Interaction Score: 0.79

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL CACNB4

Interaction Score: 0.79

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL CACNA1H

Interaction Score: 0.72

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
17190903 14993472 9670923 9481612 15498818 9375939 16899990 15562257

Sources:
TTD DrugBank GuideToPharmacology
MIBEFRADIL CACNA1G

Interaction Score: 0.68

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
9481612 10692398 11752352 9375939 16899990 15562257

Sources:
DrugBank GuideToPharmacology
MIBEFRADIL CACNB1

Interaction Score: 0.63

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL CATSPER2

Interaction Score: 0.59

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER1

Interaction Score: 0.59

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER3

Interaction Score: 0.59

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CATSPER4

Interaction Score: 0.59

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology
MIBEFRADIL CACNA1I

Interaction Score: 0.53

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
9481612 9375939 16899990 15562257

Sources:
DrugBank GuideToPharmacology
MIBEFRADIL CACNB2

Interaction Score: 0.5

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL CACNA1F

Interaction Score: 0.34

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL CACNA1D

Interaction Score: 0.28

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL CACNA1C

Interaction Score: 0.24

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
10665814 10372226 16306443 16899990

Sources:
DrugBank GuideToPharmacology
MIBEFRADIL CACNA1S

Interaction Score: 0.24

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank
MIBEFRADIL THPO

Interaction Score: 0.03

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL MTOR

Interaction Score: 0.02

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL MAPK1

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL KCNH2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
16253929

Sources:
PharmGKB
MIBEFRADIL ATXN2

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL ATAD5

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC
MIBEFRADIL CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
21447734

Sources:
DTC
MIBEFRADIL CYP2D6

Interaction Score: 0.0

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
DTC

DrugBank: DB01388

Version: 5.1.7

Alternate Names:

MIBEFRADIL DrugBank Drug Name

116644-53-2 CAS Number

Batenac Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups investigational

Drug Groups withdrawn

Publications:

Jiménez et al., 2000, Determinants of voltage-dependent inactivation affect Mibefradil block of calcium channels., Neuropharmacology

Mocanu et al., 1999, Mibefradil, a T-type and L-type calcium channel blocker, limits infarct size through a glibenclamide-sensitive mechanism., Cardiovasc Drugs Ther

Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology

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

CHEMBL45816 ChEMBL Drug ID

Drug Info:

Publications:

Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos
PharmGKB: mibefradil
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
TTD: Mibefradil
- Version: 2020.06.01
Alternate Names:

D0W8XT TTD Drug ID

Drug Info:

Publications:
GuideToPharmacology: 53801058
- Version: 29-September-2020
Alternate Names:

MIBEFRADIL GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL45816
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

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

Details of the Assay for Interaction	Patch clamp electrophysiology and kinetic rapid mixing fluometry.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

Details of the Assay for Interaction	Patch clamp electrophysiology, kinetic rapid mixing fluometry.
Specific Action of the Ligand	Inhibition
Endogenous Drug?	False

MIBEFRADIL	DrugBank Drug Name
116644-53-2	CAS Number
Batenac	Drug Brand

Drug Type	small molecule
Drug Groups	investigational
Drug Groups	withdrawn

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

blocker (inhibitory)
inhibitor (inhibitory)

MIBEFRADIL Drug Record

MIBEFRADIL chembl:CHEMBL45816

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

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

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

PMIDs: 17190903 14993472 9670923 9481612 15498818 9375939 16899990 15562257

Sources: TTD DrugBank GuideToPharmacology

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

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

PMIDs: 9481612 10692398 11752352 9375939 16899990 15562257

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

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

PMIDs: None found

Sources: GuideToPharmacology

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry. Specific Action of the Ligand Inhibition Endogenous Drug? False

PMIDs: None found

Sources: GuideToPharmacology

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

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

PMIDs: 9481612 9375939 16899990 15562257

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

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

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

PMIDs: 10665814 10372226 16306443 16899990

Sources: DrugBank GuideToPharmacology

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 10665814 10372226 16899990

Sources: DrugBank

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

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
17190903 14993472 9670923 9481612 15498818 9375939 16899990 15562257

Sources:
TTD DrugBank GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

PMIDs:
9481612 10692398 11752352 9375939 16899990 15562257

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology and kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Details of the Assay for Interaction Patch clamp electrophysiology, kinetic rapid mixing fluometry.

Specific Action of the Ligand Inhibition

Endogenous Drug? False

PMIDs:
None found

Sources:
GuideToPharmacology

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
9481612 9375939 16899990 15562257

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

PMIDs:
10665814 10372226 16306443 16899990

Sources:
DrugBank GuideToPharmacology

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
10665814 10372226 16899990

Sources:
DrugBank

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:
16253929

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:
21447734

Sources:
DTC

Interaction Types & Directionality:

n/a

PMIDs:
None found