DGIdb - VARENICLINE Drug Record

VARENICLINE chembl:CHEMBL1396 Approved

Alternate Names:

CHANTIX
CP-526555
CP-526,555
VARENICLINE

Drug Info:

Drug Categories	quinoxalines
Drug Categories	physiological effects of drugs
Drug Categories	pharmacologic actions
Drug Categories	nicotinic agonists
Drug Categories	neurotransmitter agents
Drug Categories	nervous system
Drug Categories	molecular mechanisms of pharmacological action
Drug Categories	heterocyclic compounds, 2-ring
Drug Categories	heterocyclic compounds
Drug Categories	drugs used in nicotine dependence
Drug Categories	drugs used in addictive disorders
Drug Categories	cholinergic agonists
Drug Categories	cholinergic agents
Drug Categories	chemical actions and uses
Drug Categories	benzazepines
Drug Groups	investigational
Drug Groups	approved
Drug Type	small molecule
Drug Class	smoking-cessation agent
Year of Approval	2006
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	smoking-cessation agent
Drug Categories	smoking cessation agents
Drug Categories	partial cholinergic nicotinic agonists
Drug Categories	partial cholinergic nicotinic agonist
Drug Categories	oct2 substrates
Drug Categories	oct2 inhibitors
Drug Categories	miscellaneous autonomic drugs
Drug Categories	heterocyclic compounds, fused-ring
Drug Categories	drugs that are mainly renally excreted

(3 More Sources)

Publications:

Rollema et al., 2007, Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation., Trends Pharmacol. Sci.
Steensland et al., 2007, Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking., Proc. Natl. Acad. Sci. U.S.A.
McColl et al., 2008, Human abuse liability of the smoking cessation drug varenicline in smokers and nonsmokers., Clin. Pharmacol. Ther.
Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
Nakamura et al., 2007, Efficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokers., Clin Ther
Rocha Santos J et al., 2015, CHRNA4 rs1044396 is associated with smoking cessation in varenicline therapy., Front Genet
Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.
Niaura R et al., 2006, Varenicline., Nat Rev Drug Discov
Lerman C et al., 2015, Use of the nicotine metabolite ratio as a genetically informed biomarker of response to nicotine patch or varenicline for smoking cessation: a randomised, double-blind placebo-controlled trial., Lancet Respir Med

VARENICLINE CHRNA4

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Details of the Assay for Interaction <i>In vitro</i> affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine.

Publications:

Rollema et al., 2007, Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation., Trends Pharmacol. Sci.

Steensland et al., 2007, Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking., Proc. Natl. Acad. Sci. U.S.A.

McColl et al., 2008, Human abuse liability of the smoking cessation drug varenicline in smokers and nonsmokers., Clin. Pharmacol. Ther.

VARENICLINE CHRNA3

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Specific Action of the Ligand Agonist

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.
VARENICLINE CHRNB2

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Publications:

Niaura R et al., 2006, Varenicline., Nat Rev Drug Discov
VARENICLINE CHRNA7

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.
VARENICLINE CHRNA6

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.
VARENICLINE CHRNB4

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Publications:

VARENICLINE CYP2A6

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

Lerman C et al., 2015, Use of the nicotine metabolite ratio as a genetically informed biomarker of response to nicotine patch or varenicline for smoking cessation: a randomised, double-blind placebo-controlled trial., Lancet Respir Med

VARENICLINE HYKK

Interaction Types & Directionality:

n/a

Interaction Info:

Publications:

DrugBank: DB01273

Version: 5.1.7

Alternate Names:

VARENICLINE DrugBank Drug Name

249296-44-4 CAS Number

Apo-varenicline Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Niaura R et al., 2006, Varenicline., Nat Rev Drug Discov

Nakamura et al., 2007, Efficacy and tolerability of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, in a 12-week, randomized, placebo-controlled, dose-response study with 40-week follow-up for smoking cessation in Japanese smokers., Clin Ther

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

VARENICLINE Primary Drug Name

Drug Info:

Year of Approval 2006

Drug Class smoking-cessation agent

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

Drug Info:

Drug Indications smoking-cessation agent

Drug Class Small Molecule

FDA Approval approved

Publications:

PharmGKB: varenicline

Version: 18-August-2020

Alternate Names:

Drug Info:

Publications:

Rocha Santos J et al., 2015, CHRNA4 rs1044396 is associated with smoking cessation in varenicline therapy., Front Genet

Lerman C et al., 2015, Use of the nicotine metabolite ratio as a genetically informed biomarker of response to nicotine patch or varenicline for smoking cessation: a randomised, double-blind placebo-controlled trial., Lancet Respir Med

TTD: Varenicline
- Version: 2020.06.01
Alternate Names:

D0LM4A TTD Drug ID

Drug Info:

Publications:
GuideToPharmacologyInteractions: 178102109
- Version: 20-July-2020
Alternate Names:

VARENICLINE GuideToPharmacology Ligand Name

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1396
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:

Trial Name	varenicline, CP-526
Novel drug target	Established target
Details of the Assay for Interaction	<i>In vitro</i> affinity for recombinant human α4β2 receptors in membranes from transfected CHO-K1 cells, determined by displacement of [<sup>3</sup>H]-(−)-cytisine.

VARENICLINE	DrugBank Drug Name
249296-44-4	CAS Number
Apo-varenicline	Drug Brand

VARENICLINE Drug Record

VARENICLINE chembl:CHEMBL1396 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Types & Directionality: partial agonist (activating) agonist (activating)

Interaction Info: Trial Name varenicline, CP-526 Novel drug target Established target Specific Action of the Ligand Agonist

Publications: Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Interaction Types & Directionality: partial agonist (activating)

Interaction Info: Trial Name varenicline, CP-526 Novel drug target Established target

Publications: Niaura R et al., 2006, Varenicline., Nat Rev Drug Discov

Interaction Types & Directionality: agonist (activating)

Interaction Info: Trial Name varenicline, CP-526 Novel drug target Established target

Publications: Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Interaction Types & Directionality: partial agonist (activating)

Interaction Info:

Publications: Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Interaction Types & Directionality: n/a

Interaction Info: Trial Name varenicline, CP-526 Novel drug target Established target

Publications:

Interaction Types & Directionality: n/a

Interaction Info:

Publications: Lerman C et al., 2015, Use of the nicotine metabolite ratio as a genetically informed biomarker of response to nicotine patch or varenicline for smoking cessation: a randomised, double-blind placebo-controlled trial., Lancet Respir Med

Interaction Types & Directionality: n/a

Interaction Info:

Publications:

DrugBank: DB01273

Alternate Names: VARENICLINE DrugBank Drug Name 249296-44-4 CAS Number Apo-varenicline Drug Brand

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

TEND: VARENICLINE

Alternate Names: VARENICLINE Primary Drug Name

Drug Info: Year of Approval 2006 Drug Class smoking-cessation agent

Publications:

TdgClinicalTrial: VARENICLINE

Alternate Names:

Drug Info: Drug Indications smoking-cessation agent Drug Class Small Molecule FDA Approval approved

Publications:

PharmGKB: varenicline

Alternate Names:

Drug Info:

TTD: Varenicline

Alternate Names: D0LM4A TTD Drug ID

Drug Info:

Publications:

GuideToPharmacologyInteractions: 178102109

Alternate Names: VARENICLINE GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1396

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Specific Action of the Ligand Agonist

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Publications:

Niaura R et al., 2006, Varenicline., Nat Rev Drug Discov

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Interaction Types & Directionality:

partial agonist (activating)

Publications:

Mihalak et al., 2006, Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors., Mol. Pharmacol.

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

Interaction Types & Directionality:

n/a

Publications:

Lerman C et al., 2015, Use of the nicotine metabolite ratio as a genetically informed biomarker of response to nicotine patch or varenicline for smoking cessation: a randomised, double-blind placebo-controlled trial., Lancet Respir Med

Interaction Types & Directionality:

n/a

Alternate Names:

VARENICLINE DrugBank Drug Name

249296-44-4 CAS Number

Apo-varenicline Drug Brand

Drug Info:

Drug Type small molecule

Drug Groups approved

Drug Groups investigational

Alternate Names:

VARENICLINE Primary Drug Name

Drug Info:

Year of Approval 2006

Drug Class smoking-cessation agent

Drug Info:

Drug Indications smoking-cessation agent

Drug Class Small Molecule

FDA Approval approved

Alternate Names:

D0LM4A TTD Drug ID

Alternate Names:

VARENICLINE GuideToPharmacology Ligand Name