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 Categories	vasodilator agents
Drug Categories	therapeutic uses
Drug Categories	tetrahydronaphthalenes
Drug Categories	selective calcium channel blockers with mainly vascular effects
Drug Categories	polycyclic hydrocarbons, aromatic
Drug Categories	polycyclic compounds
Drug Categories	pharmacologic actions
Drug Categories	p-glycoprotein/abcb1 inhibitors
Drug Categories	organic chemicals
Drug Categories	naphthalenes
Drug Categories	molecular mechanisms of pharmacological action
Drug Categories	metabolic side effects of drugs and substances
Drug Categories	membrane transport modulators
Drug Categories	hydrocarbons, cyclic
Drug Categories	hydrocarbons, aromatic
Drug Categories	hydrocarbons
Drug Categories	heterocyclic compounds, 2-ring
Drug Categories	heterocyclic compounds
Drug Categories	enzyme inhibitors
Drug Categories	drug-related side effects and adverse reactions
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 cyp3a4 substrates
Drug Categories	cytochrome p-450 cyp3a inhibitors
Drug Categories	cytochrome p-450 cyp2d6 inhibitors
Drug Categories	cytochrome p-450 cyp1a2 inhibitors
Drug Categories	combined inhibitors of cyp3a4 and p-glycoprotein
Drug Categories	chemically-induced disorders
Drug Categories	chemical actions and uses
Drug Categories	cardiovascular system
Drug Categories	cardiovascular agents
Drug Categories	calcium channel blockers
Drug Categories	benzimidazoles
Drug Categories	antihypertensive agents
Drug Groups	withdrawn
Drug Type	small molecule
Drug Categories	vasodilating agents
Drug Categories	qtc prolonging agents
Drug Categories	p-glycoprotein substrates
Drug Categories	p-glycoprotein inhibitors
Drug Categories	moderate risk qtc-prolonging agents
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	cytochrome p-450 substrates
Drug Categories	cytochrome p-450 cyp3a7 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a7 inhibitors
Drug Categories	cytochrome p-450 cyp3a5 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a5 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (strength unknown)
Drug Categories	cytochrome p-450 cyp1a2 inhibitors (strength unknown)
Drug Categories	calcium-regulating hormones and agents
Drug Categories	bradycardia-causing agents
Drug Categories	antiarrhythmic agents
Drug Categories	agents causing hyperkalemia
Drug Groups	investigational

(2 More Sources)

Publications:

Lee et al., 2006, Actions of mibefradil, efonidipine and nifedipine block of recombinant T- and L-type Ca channels with distinct inhibitory mechanisms., Pharmacology
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
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
McNulty et al., 2004, State-dependent mibefradil block of Na+ channels., Mol. Pharmacol.
Massie, 1997, Mibefradil: a selective T-type calcium antagonist., Am. J. Cardiol.
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.
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.
Cribbs et al., 1998, Cloning and characterization of alpha1H from human heart, a member of the T-type Ca2+ channel gene family., Circ. Res.
Perez-Reyes, 2004, Paradoxical role of T-type calcium channels in coronary smooth muscle., Mol. Interv.
Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

MIBEFRADIL CATSPER4

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

Publications:
MIBEFRADIL CATSPER3

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
MIBEFRADIL ANO1

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Publications:
MIBEFRADIL CATSPER1

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Publications:
MIBEFRADIL CATSPER2

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

Publications:

MIBEFRADIL CACNB4

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

MIBEFRADIL CACNA1F

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

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

MIBEFRADIL CACNB3

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

MIBEFRADIL CACNA1I

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

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

McNulty et al., 2004, State-dependent mibefradil block of Na+ channels., Mol. Pharmacol.

MIBEFRADIL CACNA1G

Interaction Types & Directionality:

inhibitor (inhibitory)

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Publications:

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

Monteil et al., 2000, Molecular and functional properties of the human alpha(1G) subunit that forms T-type calcium channels., J. Biol. Chem.

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

MIBEFRADIL CACNA1C

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Publications:

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

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

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.

MIBEFRADIL CACNA1H

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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.

MIBEFRADIL CACNA1D

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

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

MIBEFRADIL CACNB1

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

MIBEFRADIL CACNB2

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

MIBEFRADIL CACNA1S

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Publications:

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

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

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

MIBEFRADIL KCNH2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm
MIBEFRADIL CYP3A4

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos
MIBEFRADIL MAPK1

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MIBEFRADIL THPO

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MIBEFRADIL ATAD5

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MIBEFRADIL ATXN2

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MIBEFRADIL MTOR

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:
MIBEFRADIL CYP2D6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

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:

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

McNulty et al., 2004, State-dependent mibefradil block of Na+ channels., Mol. Pharmacol.

Massie, 1997, Mibefradil: a selective T-type calcium antagonist., Am. J. Cardiol.

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
GuideToPharmacologyInteractions: 53801058
- Version: 20-July-2020
Alternate Names:

MIBEFRADIL GuideToPharmacology Ligand Name

Drug Info:

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

D0W8XT TTD Drug ID

Drug Info:

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

Drug Info:

Publications:

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

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

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

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

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

MIBEFRADIL Drug Record

MIBEFRADIL chembl:CHEMBL45816

Alternate Names:

Drug Info:

Publications:

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

Publications:

Interaction Types & Directionality: blocker (inhibitory)

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

Publications:

Interaction Types & Directionality: blocker (inhibitory)

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

Publications:

Interaction Types & Directionality: blocker (inhibitory)

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

Publications:

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

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

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

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

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

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

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

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

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

DrugBank: DB01388

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

DTC: MIBEFRADIL

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

Alternate Names:

Drug Info:

Publications: Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm

GuideToPharmacologyInteractions: 53801058

Alternate Names: MIBEFRADIL GuideToPharmacology Ligand Name

Drug Info:

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

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand None

Endogenous Drug? False

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Inhibition

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

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Direct Interaction? False

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

inhibitor (inhibitory)

blocker (inhibitory)

Interaction Info:

Specific Action of the Ligand Antagonist

Endogenous Drug? False

Direct Interaction? False

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Endogenous Drug? False

Specific Action of the Ligand Antagonist

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Types & Directionality:

n/a

Publications:

Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm

Interaction Types & Directionality:

n/a

Publications:

Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

Interaction Types & Directionality:

n/a

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

Alternate Names:

CHEMBL45816 ChEMBL Drug ID

Publications:

Foti RS et al., 2011, Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction., Drug Metab Dispos

Publications:

Fitzgerald PT et al., 2005, Drug-induced torsades de pointes: the evolving role of pharmacogenetics., Heart Rhythm

Alternate Names:

MIBEFRADIL GuideToPharmacology Ligand Name

Alternate Names:

D0W8XT TTD Drug ID