DGIdb - VARENICLINE Drug Record

VARENICLINE chembl:CHEMBL1396 Approved

Alternate Names:

CHANTIX
CP-526555
CP-526,555
VARENICLINE

Drug Info:

Drug Class	smoking-cessation agent
Year of Approval	2006
FDA Approval	approved
Drug Class	Small Molecule
Drug Indications	smoking-cessation agent

(2 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 HYKK

Interaction Score: 9.11

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
None found

Sources:
PharmGKB

VARENICLINE CHRNA4

Interaction Score: 2.22

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.

PMIDs:
17573127 17626178 18288085 11752352 17692720 25774163

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB

VARENICLINE CHRNA3

Interaction Score: 1.37

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

PMIDs:
16766716

Sources:
TdgClinicalTrial GuideToPharmacology
VARENICLINE CHRNB2

Interaction Score: 1.14

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
16883648

Sources:
TdgClinicalTrial
VARENICLINE CYP2A6

Interaction Score: 0.76

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
25588294

Sources:
PharmGKB
VARENICLINE CHRNB4

Interaction Score: 0.7

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial
VARENICLINE CHRNA7

Interaction Score: 0.62

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
16766716

Sources:
TdgClinicalTrial TEND

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:
GuideToPharmacology: 178102109
- Version: 29-September-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 Drug Record

VARENICLINE chembl:CHEMBL1396 Approved

Alternate Names:

Drug Info:

Publications:

VARENICLINE HYKK

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: None found

Sources: PharmGKB

VARENICLINE CHRNA4

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

PMIDs: 17573127 17626178 18288085 11752352 17692720 25774163

Sources: TdgClinicalTrial TEND GuideToPharmacology PharmGKB

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

PMIDs: 16766716

Sources: TdgClinicalTrial GuideToPharmacology

VARENICLINE CHRNB2

Interaction Types & Directionality: partial agonist (activating)

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

PMIDs: 16883648

Sources: TdgClinicalTrial

VARENICLINE CYP2A6

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 25588294

Sources: PharmGKB

VARENICLINE CHRNB4

Interaction Types & Directionality: n/a

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

PMIDs: None found

Sources: TdgClinicalTrial

VARENICLINE CHRNA7

Interaction Types & Directionality: agonist (activating)

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

PMIDs: 16766716

Sources: TdgClinicalTrial TEND

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:

GuideToPharmacology: 178102109

Alternate Names: VARENICLINE GuideToPharmacology Ligand Name

Drug Info:

Publications:

ChemblDrugs: chembl:CHEMBL1396

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality:

n/a

PMIDs:
None found

Sources:
PharmGKB

Interaction Types & Directionality:

partial agonist (activating)

agonist (activating)

PMIDs:
17573127 17626178 18288085 11752352 17692720 25774163

Sources:
TdgClinicalTrial TEND GuideToPharmacology PharmGKB

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

PMIDs:
16766716

Sources:
TdgClinicalTrial GuideToPharmacology

Interaction Types & Directionality:

partial agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
16883648

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

n/a

PMIDs:
25588294

Sources:
PharmGKB

Interaction Types & Directionality:

n/a

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
None found

Sources:
TdgClinicalTrial

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Trial Name varenicline, CP-526

Novel drug target Established target

PMIDs:
16766716

Sources:
TdgClinicalTrial TEND

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