DGIdb - RANOLAZINE Drug Record

RANOLAZINE chembl:CHEMBL1404 Approved

Alternate Names:

CVT-303
RANEXA
RS-43285-003
RANOLAZINE
RANEXA®
N-(2,6-DIMETHYLPHENYL)-2-[4-[2-HYDROXY-3-(2-METHOXYPHENOXY)PROPYL]PIPERAZIN-1-YL]ACETAMIDE
RS-43285
drugbank:00243
pubchem.compound:56959
chembl:CHEMBL1404
rxcui:35829
chemidplus:95635-55-5

Drug Info:

FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	antiallergy agent
Year of Approval	2006
Drug Class	antianginal agents
Drug Categories	acetamides
Drug Categories	antianginal agents
Drug Categories	bsep/abcb11 substrates
Drug Categories	cytochrome p-450 cyp2d6 inhibitors (weak)
Drug Categories	cytochrome p-450 cyp2d6 substrates
Drug Categories	cytochrome p-450 cyp3a substrates
Drug Categories	cytochrome p-450 cyp3a4 inhibitors
Drug Categories	cytochrome p-450 cyp3a4 inhibitors (weak)
Drug Categories	cytochrome p-450 enzyme inhibitors
Drug Categories	cytochrome p-450 substrates
Drug Categories	drugs that are mainly renally excreted
Drug Categories	mate 1 inhibitors
Drug Categories	mate 2 inhibitors
Drug Categories	mate inhibitors
Drug Categories	moderate risk qtc-prolonging agents
Drug Categories	oct2 inhibitors
Drug Categories	p-glycoprotein inhibitors
Drug Categories	p-glycoprotein substrates
Drug Categories	qtc prolonging agents
Drug Categories	vasodilating agents

(3 More Sources)

Publications:

Rajamani et al., Block of tetrodotoxin-sensitive, Na(V)1.7 and tetrodotoxin-resistant, Na(V)1.8, Na+ channels by ranolazine., Channels (Austin)
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol
Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev
Hale et al., 2006, Ranolazine, an inhibitor of the late sodium channel current, reduces postischemic myocardial dysfunction in the rabbit., J. Cardiovasc. Pharmacol. Ther.
Neshatian L et al., 2015, Ranolazine inhibits voltage-gated mechanosensitive sodium channels in human colon circular smooth muscle cells., Am J Physiol Gastrointest Liver Physiol
Saad M et al., 2016, Ranolazine in Cardiac Arrhythmia., Clin Cardiol
Fredj S et al., 2006, Molecular basis of ranolazine block of LQT-3 mutant sodium channels: evidence for site of action., Br J Pharmacol
Peters CH et al., 2013, Effects of the antianginal drug, ranolazine, on the brain sodium channel Na(V)1.2 and its modulation by extracellular protons., Br J Pharmacol
Jerling M, 2006, Clinical pharmacokinetics of ranolazine., Clin Pharmacokinet
Rayner-Hartley E et al., 2016, Ranolazine: A Contemporary Review., J Am Heart Assoc
Virsolvy A et al., 2015, Antagonism of Nav channels and α1-adrenergic receptors contributes to vascular smooth muscle effects of ranolazine., Sci Rep
Zhao G et al., 2011, Antiadrenergic and hemodynamic effects of ranolazine in conscious dogs., J Cardiovasc Pharmacol
Létienne R et al., 2001, Evidence that ranolazine behaves as a weak beta1- and beta2-adrenoceptor antagonist in the rat [correction of cat] cardiovascular system., Naunyn Schmiedebergs Arch Pharmacol

RANOLAZINE KCNJ12

Interaction Score: 3.55

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26459200 26979079

Sources:
DrugBank
RANOLAZINE CACNA1C

Interaction Score: 0.41

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
26185330 26459200 16520744 23472826

Sources:
DrugBank
RANOLAZINE SCN5A

Interaction Score: 0.25

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name Ranexa

Novel drug target Established target

Mechanism of Interaction Sodium channel protein type V alpha subunit blocker

PMIDs:
17220471 19077543

Sources:
TEND TdgClinicalTrial ChemblInteractions
RANOLAZINE SCN1A

Interaction Score: 0.25

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

PMIDs:
16640453 26459200 26979079

Sources:
DrugBank
RANOLAZINE SCN9A

Interaction Score: 0.21

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Ranexa

Novel drug target Established target

PMIDs:
19077543 11752352

Sources:
TdgClinicalTrial
RANOLAZINE PLG

Interaction Score: 0.15

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
TTD
RANOLAZINE ADRB1

Interaction Score: 0.15

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
21633249 11330341 26979079

Sources:
DrugBank
RANOLAZINE ADRA1A

Interaction Score: 0.11

Interaction Types & Directionality:

antagonist (inhibitory)

Interaction Info:

PMIDs:
26655634 21633249 26979079

Sources:
DrugBank
RANOLAZINE SCN4A

Interaction Score: 0.07

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel protein type IV alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
RANOLAZINE ABCB1

Interaction Score: 0.04

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
24433361

Sources:
PharmGKB
RANOLAZINE CYP3A4

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
9187528

Sources:
PharmGKB
RANOLAZINE CYP2D6

Interaction Score: 0.01

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

DrugBank: DB00243

Version: 5.1.7

Alternate Names:

95635-55-5 CAS Number

Ranexa Drug Brand

CHEMBL1404 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Neshatian L et al., 2015, Ranolazine inhibits voltage-gated mechanosensitive sodium channels in human colon circular smooth muscle cells., Am J Physiol Gastrointest Liver Physiol

Saad M et al., 2016, Ranolazine in Cardiac Arrhythmia., Clin Cardiol

Fredj S et al., 2006, Molecular basis of ranolazine block of LQT-3 mutant sodium channels: evidence for site of action., Br J Pharmacol

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

Drug Info:

Drug Class antianginal agents

Year of Approval 2006

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

Drug Info:

Drug Indications antiallergy agent

Drug Class Small Molecule

FDA Approval approved

Publications:

PharmGKB: ranolazine

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol

Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

TTD: Ranolazine
- Version: 2020.06.01
Alternate Names:

D03HYQ TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1404
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1404
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Trial Name	Ranexa
Novel drug target	Established target
Mechanism of Interaction	Sodium channel protein type V alpha subunit blocker

Mechanism of Interaction	Sodium channel protein type IV alpha subunit blocker
Direct Interaction	yes

Drug Type	small molecule
Drug Groups	approved
Drug Groups	investigational

blocker (inhibitory)
inhibitor (inhibitory)

RANOLAZINE Drug Record

RANOLAZINE chembl:CHEMBL1404 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 26459200 26979079

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 26185330 26459200 16520744 23472826

Sources: DrugBank

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

Interaction Info: Trial Name Ranexa Novel drug target Established target Mechanism of Interaction Sodium channel protein type V alpha subunit blocker

PMIDs: 17220471 19077543

Sources: TEND TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info:

PMIDs: 16640453 26459200 26979079

Sources: DrugBank

Interaction Types & Directionality: inhibitor (inhibitory)

Interaction Info: Trial Name Ranexa Novel drug target Established target

PMIDs: 19077543 11752352

Sources: TdgClinicalTrial

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: TTD

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 21633249 11330341 26979079

Sources: DrugBank

Interaction Types & Directionality: antagonist (inhibitory)

Interaction Info:

PMIDs: 26655634 21633249 26979079

Sources: DrugBank

Interaction Types & Directionality: blocker (inhibitory)

Interaction Info: Mechanism of Interaction Sodium channel protein type IV alpha subunit blocker Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 24433361

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 9187528

Sources: PharmGKB

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

DrugBank: DB00243

Alternate Names: 95635-55-5 CAS Number Ranexa Drug Brand CHEMBL1404 ChEMBL ID

Drug Info: Drug Type small molecule Drug Groups approved Drug Groups investigational

TEND: RANOLAZINE

Alternate Names:

Drug Info: Drug Class antianginal agents Year of Approval 2006

Publications:

TdgClinicalTrial: RANOLAZINE

Alternate Names:

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

Publications:

PharmGKB: ranolazine

Alternate Names:

Drug Info:

Publications: Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

TTD: Ranolazine

Alternate Names: D03HYQ TTD Drug ID

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1404

Alternate Names:

Drug Info:

Publications:

ChemblInteractions: CHEMBL1404

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26459200 26979079

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
26185330 26459200 16520744 23472826

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

inhibitor (inhibitory)

Interaction Info:

Trial Name Ranexa

Novel drug target Established target

Mechanism of Interaction Sodium channel protein type V alpha subunit blocker

PMIDs:
17220471 19077543

Sources:
TEND TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

inhibitor (inhibitory)

PMIDs:
16640453 26459200 26979079

Sources:
DrugBank

Interaction Types & Directionality:

inhibitor (inhibitory)

Interaction Info:

Trial Name Ranexa

Novel drug target Established target

PMIDs:
19077543 11752352

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
TTD

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
21633249 11330341 26979079

Sources:
DrugBank

Interaction Types & Directionality:

antagonist (inhibitory)

PMIDs:
26655634 21633249 26979079

Sources:
DrugBank

Interaction Types & Directionality:

blocker (inhibitory)

Interaction Info:

Mechanism of Interaction Sodium channel protein type IV alpha subunit blocker

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
24433361

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
9187528

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Alternate Names:

95635-55-5 CAS Number

Ranexa Drug Brand

CHEMBL1404 ChEMBL ID

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Drug Info:

Drug Class antianginal agents

Year of Approval 2006

Drug Info:

Drug Indications antiallergy agent

Drug Class Small Molecule

FDA Approval approved

Publications:

Ehmann F et al., 2014, European Medicines Agency initiatives and perspectives on pharmacogenomics., Br J Clin Pharmacol

Rendic S et al., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors., Drug Metab Rev

Alternate Names:

D03HYQ TTD Drug ID