Identification

Summary

Varenicline is a partial agonist at nicotinic acetylcholine receptors used as an aid in smoking cessation.

Brand Names
Champix, Chantix, Tyrvaya
Generic Name
Varenicline
DrugBank Accession Number
DB01273
Background

Varenicline is a prescription medication used to treat smoking addiction. This medication is the first approved nicotinic receptor partial agonist. Specifically, varenicline is a partial agonist of the alpha4/beta2 subtype of the nicotinic acetylcholine receptor. In addition it acts on alpha3/beta4 and weakly on alpha3beta2 and alpha6-containing receptors. A full agonism was displayed on alpha7-receptors.

On March 9, 2015, the U.S. Food and Drug Administration warned that Varenicline, in the form of Pfizer Inc's quit-smoking drug, Chantix, has been associated with seizures and that some patients who drink while taking the drug may become aggressive or black out. Pfizer is conducting an additional safety study of the drug, results of which are expected in late 2015. The FDA said it is keeping the black box in place at least until the results of the trial are announced.

Type
Small Molecule
Groups
Approved, Investigational
Structure
Thumb
Weight
Average: 211.268
Monoisotopic: 211.110947431
Chemical Formula
C13H13N3
Synonyms
  • Vareniclina
  • Varenicline
  • Vareniclinum
External IDs
  • CP 526555
  • CP-526,555
  • CP-526555

Pharmacology

Indication

For use as an aid in smoking cessation.

Varenicline as a nasal spray is indicated for the symptomatic treatment of dry eye disease.6

Pharmacology
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Associated Conditions
Associated Therapies
Contraindications & Blackbox Warnings
Contraindications
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Pharmacodynamics

Varenicline is a partial nicotinic acetylcholine receptor agonist, designed to partially activate this system while displacing nicotine at its sites of action in the brain.

Mechanism of action

Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectivity for this receptor subclass, relative to other nicotinic receptors (>500-fold alpha-3 beta-4, >3500-fold alpha-7, >20,000-fold alpha-1 beta gamma delta) or non-nicotinic receptors and transporters (>2000-fold). The drug competitively inhibits the ability of nicotine to bind to and activate the alpha-4 beta-2 receptor. The drug exerts mild agonistic activity at this site, though at a level much lower than nicotine; it is presumed that this activation eases withdrawal symptoms.

TargetActionsOrganism
ANeuronal acetylcholine receptor subunit alpha-4
partial agonist
Humans
UNeuronal acetylcholine receptor subunit alpha-7
agonist
Humans
UNeuronal acetylcholine receptor subunit alpha-3
partial agonist
Humans
UNeuronal acetylcholine receptor subunit alpha-6
partial agonist
Humans
UNeuronal acetylcholine receptor subunit beta-2
partial agonist
Humans
Absorption

Not Available

Volume of distribution

Not Available

Protein binding

Less than 20%.

Metabolism

Metabolism is limited (<10%). Most of the active compound is excreted by the kidneys (81%). A minor amount of varenicline is glucuronidated, oxidated, N-formylated, as well as conjugated to form a hexose.

Route of elimination

Varenicline undergoes minimal metabolism, with 92% excreted unchanged in the urine. Renal elimination of varenicline is primarily through glomerular filtration along with active tubular secretion possibly via the organic cation transporter, OCT2.

Half-life

The elimination half-life of varenicline is approximately 24 hours

Clearance

Not Available

Adverse Effects
Adverseeffects
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Toxicity

Not Available

Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbacavirAbacavir may decrease the excretion rate of Varenicline which could result in a higher serum level.
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Varenicline.
AceclofenacAceclofenac may decrease the excretion rate of Varenicline which could result in a higher serum level.
AcemetacinAcemetacin may decrease the excretion rate of Varenicline which could result in a higher serum level.
AcetaminophenAcetaminophen may decrease the excretion rate of Varenicline which could result in a higher serum level.
AcetazolamideAcetazolamide may increase the excretion rate of Varenicline which could result in a lower serum level and potentially a reduction in efficacy.
Acetylsalicylic acidAcetylsalicylic acid may decrease the excretion rate of Varenicline which could result in a higher serum level.
AclidiniumVarenicline may decrease the excretion rate of Aclidinium which could result in a higher serum level.
AcrivastineVarenicline may decrease the excretion rate of Acrivastine which could result in a higher serum level.
AcyclovirAcyclovir may decrease the excretion rate of Varenicline which could result in a higher serum level.
Interactions
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Food Interactions
  • Avoid excessive or chronic alcohol consumption. Varenicline may increase the effects of alcohol; therefore, reduce consumption of alcohol when starting varenicline.

Products

Products2
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Product Ingredients
IngredientUNIICASInChI Key
Varenicline tartrate82269ASB48375815-87-5TWYFGYXQSYOKLK-CYUSMAIQSA-N
Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-vareniclineTablet, film coated0.5 mg/1OralApotex Corp2021-07-16Not applicableUS flag
Apo-vareniclineTablet, film coated1 mg/1OralApotex Corp2021-07-16Not applicableUS flag
ChampixTablet, film coated1 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated0.5 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated0.5 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated0.5 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated1.0 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated1.0 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated1 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
ChampixTablet, film coated1 mgOralPfizer Europe Ma Eeig2016-09-08Not applicableEU flag
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Apo-vareniclineTablet0.5 mgOralApotex Corporation2018-05-02Not applicableCanada flag
Apo-vareniclineTablet1 mgOralApotex Corporation2018-05-02Not applicableCanada flag
Gd-vareniclineTablet1 mgOralGenmed A Division Of Pfizer Canada UlcNot applicableNot applicableCanada flag
Gd-vareniclineTablet0.5 mgOralGenmed A Division Of Pfizer Canada UlcNot applicableNot applicableCanada flag
PMS-vareniclineTablet0.5 mgOralPharmascience IncNot applicableNot applicableCanada flag
PMS-vareniclineTablet1 mgOralPharmascience IncNot applicableNot applicableCanada flag
Teva-vareniclineTablet1 mgOralTEVA Canada Limited2019-04-23Not applicableCanada flag
Teva-vareniclineTablet0.5 mgOralTEVA Canada Limited2019-04-23Not applicableCanada flag
VareniclineTablet, film coated1 mg/1OralPar Pharmaceutical, Inc.2021-09-21Not applicableUS flag
VareniclineTablet, film coated0.5 mg/1OralPar Pharmaceutical, Inc.2021-09-21Not applicableUS flag
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Apo-vareniclineVarenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg)Kit; TabletOralApotex Corporation2018-06-12Not applicableCanada flag
Apo-vareniclineVarenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg)Kit; TabletOralApotex Corporation2018-06-12Not applicableCanada flag
ChampixVarenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg)Kit; TabletOralPfizer Canada Ulc2007-10-02Not applicableCanada flag
ChampixVarenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg)Kit; TabletOralPfizer Canada Ulc2007-10-02Not applicableCanada flag
CHAMPIX 0,5 MG 1 MG FILM KAPLI TABLET, 11 VE 14 ADETVarenicline (0.5 mg) + Varenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag
CHAMPIX 0,5 MG 1 MG FILM KAPLI TABLET, 11 VE 14 ADETVarenicline (0.5 mg) + Varenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag
CHAMPIX 0,5 MG 11 + 1 MG 42 FILM KAPLI TABLETVarenicline (0.5 mg) + Varenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag
CHAMPIX 0,5 MG 11 + 1 MG 42 FILM KAPLI TABLETVarenicline (0.5 mg) + Varenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag
CHAMPIX 0,5 MG 11 + 1 MG 98 FILM KAPLI TABLETVarenicline (0.5 mg) + Varenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag
CHAMPIX 0,5 MG 11 + 1 MG 98 FILM KAPLI TABLETVarenicline (0.5 mg) + Varenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing EndRegionImage
Apo-vareniclineVarenicline tartrate (1 mg/1)Tablet, film coatedOralApotex Corp2021-07-16Not applicableUS flag
Apo-vareniclineVarenicline tartrate (0.5 mg/1) + Varenicline tartrate (1 mg/1)Kit; TabletOralApotex Corp2021-07-16Not applicableUS flag
Apo-vareniclineVarenicline tartrate (0.5 mg/1)Tablet, film coatedOralApotex Corp2021-07-16Not applicableUS flag
Apo-vareniclineVarenicline tartrate (0.5 mg/1) + Varenicline tartrate (1 mg/1)Kit; TabletOralApotex Corp2021-07-16Not applicableUS flag
CHAMPIX 1 MG 56 FILM KAPLI TABLETVarenicline (1 mg)Tablet, coatedOralPFİZER PFE İLAÇLARI A.Ş.2020-08-14Not applicableTurkey flag

Categories

ATC Codes
N07BA03 — Varenicline
Drug Categories
Classification
Not classified
Affected organisms
  • Humans and other mammals

Chemical Identifiers

UNII
W6HS99O8ZO
CAS number
249296-44-4
InChI Key
JQSHBVHOMNKWFT-UHFFFAOYSA-N
InChI
InChI=1S/C13H13N3/c1-2-16-13-5-11-9-3-8(6-14-7-9)10(11)4-12(13)15-1/h1-2,4-5,8-9,14H,3,6-7H2
IUPAC Name
5,8,14-triazatetracyclo[10.3.1.0^{2,11}.0^{4,9}]hexadeca-2(11),3,5,7,9-pentaene
SMILES
C1C2CNCC1C1=C2C=C2N=CC=NC2=C1

References

Synthesis Reference

Vinod Kumar Kansal, Suhail Ahmad, Amit Gupta, "PROCESSES FOR THE PREPARATION OF VARENICLINE AND INTERMEDIATES THEREOF." U.S. Patent US20090318695, issued December 24, 2009.

US20090318695
General References
  1. Jorenby DE, Hays JT, Rigotti NA, Azoulay S, Watsky EJ, Williams KE, Billing CB, Gong J, Reeves KR: Efficacy of varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, vs placebo or sustained-release bupropion for smoking cessation: a randomized controlled trial. JAMA. 2006 Jul 5;296(1):56-63. [Article]
  2. Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [Article]
  3. Obach RS, Reed-Hagen AE, Krueger SS, Obach BJ, O'Connell TN, Zandi KS, Miller S, Coe JW: Metabolism and disposition of varenicline, a selective alpha4beta2 acetylcholine receptor partial agonist, in vivo and in vitro. Drug Metab Dispos. 2006 Jan;34(1):121-30. Epub 2005 Oct 12. [Article]
  4. Coe JW, Brooks PR, Vetelino MG, Wirtz MC, Arnold EP, Huang J, Sands SB, Davis TI, Lebel LA, Fox CB, Shrikhande A, Heym JH, Schaeffer E, Rollema H, Lu Y, Mansbach RS, Chambers LK, Rovetti CC, Schulz DW, Tingley FD 3rd, O'Neill BT: Varenicline: an alpha4beta2 nicotinic receptor partial agonist for smoking cessation. J Med Chem. 2005 May 19;48(10):3474-7. [Article]
  5. Kuehn BM: FDA speeds smoking cessation drug review. JAMA. 2006 Feb 8;295(6):614. [Article]
  6. FDA Approved Drug Products: TYRVAYA (varenicline) nasal spray [Link]
Human Metabolome Database
HMDB0015398
PubChem Compound
5310966
PubChem Substance
46505502
ChemSpider
148958
BindingDB
50166908
RxNav
591622
ChEBI
84500
ChEMBL
CHEMBL1396
ZINC
ZINC000001481833
Therapeutic Targets Database
DAP001535
PharmGKB
PA164781343
PDBe Ligand
QMR
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Varenicline
PDB Entries
4afg / 4aft / 5ain
FDA label
Download (334 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingPreventionSmoking, Cessation1
4Active Not RecruitingTreatmentCigarette Smokers / Tobacco Use Disorders1
4Active Not RecruitingTreatmentElectronic Cigarettes / Smoking, Cessation1
4Active Not RecruitingTreatmentSmoking, Cessation / Tobacco Dependence / Withdrawal Symptoms1
4Active Not RecruitingTreatmentTobacco Use Cessation1
4CompletedNot AvailableSmoking, Cessation2
4CompletedDiagnosticRecurrences / Smoking, Cessation / Substance Related Disorders1
4CompletedHealth Services ResearchSmoking, Cessation1
4CompletedOtherCraving / Schizophrenia / Smoking1
4CompletedPreventionCerebrovascular Diseases / Smoking, Cessation1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
  • Cardinal Health
  • Diversified Healthcare Services Inc.
  • Lake Erie Medical and Surgical Supply
  • Pfizer Inc.
  • Physicians Total Care Inc.
  • Rebel Distributors Corp.
  • US Pharmaceutical Group
Dosage Forms
FormRouteStrength
Kit; tabletOral
TabletOral0.5 mg
TabletOral1.0 MG
Tablet, film coatedOral
Tablet, film coatedOral0.5 MG
Tablet, film coatedOral1 mg
Tablet, film coatedOral1.0 MG
Tablet, coatedOral
Tablet, coatedOral0.5 mg
Tablet, film coatedOral
Tablet, coatedOral
Tablet, film coatedOral1 mg/tablet
Tablet, film coatedOral0.5 mg
KitOral
KitOral0.5 mg/1
Tablet, film coatedOral.5 mg/1
Tablet, film coatedOral0.5 mg/1
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral1.0 mg/1
TabletOral1 mg
TabletOral
SprayNasal0.03 mg/0.05mL
Tablet, film coatedOral1.71 mg
Tablet, coatedOral1 mg
Prices
Unit descriptionCostUnit
Chantix Continuing Month Pak 56 1 mg tablet Disp Pack148.5USD disp
Chantix Starting Month Pak 0.5 mg X 11, 1 mg X 42 Disp Pack148.5USD disp
Chantix 1 mg tablet2.61USD tablet
Chantix 0.5 mg tablet2.56USD tablet
Chantix 1 mg cont month pak2.56USD each
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
CA2525874No2007-11-272024-05-07Canada flag
CA2316921No2004-12-072018-11-13Canada flag
US6410550Yes2002-06-252020-11-10US flag
US6890927Yes2005-05-102022-11-06US flag
US7265119Yes2007-09-042023-02-03US flag

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP0.9Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0877 mg/mLALOGPS
logP1.39ALOGPS
logP1.01ChemAxon
logS-3.4ALOGPS
pKa (Strongest Basic)9.73ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count3ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area37.81 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity61.3 m3·mol-1ChemAxon
Polarizability23.12 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9969
Blood Brain Barrier+0.9908
Caco-2 permeable-0.5233
P-glycoprotein substrateSubstrate0.5458
P-glycoprotein inhibitor INon-inhibitor0.7453
P-glycoprotein inhibitor IINon-inhibitor0.9637
Renal organic cation transporterInhibitor0.5489
CYP450 2C9 substrateNon-substrate0.8933
CYP450 2D6 substrateNon-substrate0.6522
CYP450 3A4 substrateNon-substrate0.7428
CYP450 1A2 substrateNon-inhibitor0.507
CYP450 2C9 inhibitorNon-inhibitor0.881
CYP450 2D6 inhibitorInhibitor0.6251
CYP450 2C19 inhibitorNon-inhibitor0.8029
CYP450 3A4 inhibitorNon-inhibitor0.6589
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.5453
Ames testNon AMES toxic0.7128
CarcinogenicityNon-carcinogens0.9592
BiodegradationNot ready biodegradable0.9906
Rat acute toxicity2.5914 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9382
hERG inhibition (predictor II)Inhibitor0.5497
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
Not Available

Targets

Drugtargets2
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Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Partial agonist
General Function
Ligand-gated ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeabl...
Gene Name
CHRNA4
Uniprot ID
P43681
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-4
Molecular Weight
69956.47 Da
References
  1. Nakamura M, Oshima A, Fujimoto Y, Maruyama N, Ishibashi T, Reeves KR: 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. 2007 Jun;29(6):1040-56. [Article]
  2. McColl SL, Burstein AH, Reeves KR, Billing CB Jr, Stolar M, Sellers EM: Human abuse liability of the smoking cessation drug varenicline in smokers and nonsmokers. Clin Pharmacol Ther. 2008 Apr;83(4):607-14. doi: 10.1038/sj.clpt.6100510. Epub 2008 Feb 20. [Article]
  3. Rollema H, Coe JW, Chambers LK, Hurst RS, Stahl SM, Williams KE: Rationale, pharmacology and clinical efficacy of partial agonists of alpha4beta2 nACh receptors for smoking cessation. Trends Pharmacol Sci. 2007 Jul;28(7):316-25. Epub 2007 Jun 18. [Article]
  4. Steensland P, Simms JA, Holgate J, Richards JK, Bartlett SE: Varenicline, an alpha4beta2 nicotinic acetylcholine receptor partial agonist, selectively decreases ethanol consumption and seeking. Proc Natl Acad Sci U S A. 2007 Jul 24;104(30):12518-23. Epub 2007 Jul 11. [Article]
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Toxic substance binding
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The cha...
Gene Name
CHRNA7
Uniprot ID
P36544
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-7
Molecular Weight
56448.925 Da
References
  1. Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Ligand-gated ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name
CHRNA3
Uniprot ID
P32297
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-3
Molecular Weight
57479.54 Da
References
  1. Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Acetylcholine-activated cation-selective channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
Gene Name
CHRNA6
Uniprot ID
Q15825
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-6
Molecular Weight
56897.745 Da
References
  1. Mihalak KB, Carroll FI, Luetje CW: Varenicline is a partial agonist at alpha4beta2 and a full agonist at alpha7 neuronal nicotinic receptors. Mol Pharmacol. 2006 Sep;70(3):801-5. Epub 2006 Jun 9. [Article]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Partial agonist
General Function
Ligand-gated ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeabl...
Gene Name
CHRNB2
Uniprot ID
P17787
Uniprot Name
Neuronal acetylcholine receptor subunit beta-2
Molecular Weight
57018.575 Da
References
  1. Niaura R, Jones C, Kirkpatrick P: Varenicline. Nat Rev Drug Discov. 2006 Jul;5(7):537-8. [Article]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Curator comments
A study demonstrated that varenicline, excreted by the kidney predominantly without undergoing metabolism, serves as an OCT2 substrate in vitro, and, at a much higher concentration, as an OCT2 inhibitor.
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Feng B, Obach RS, Burstein AH, Clark DJ, de Morais SM, Faessel HM: Effect of human renal cationic transporter inhibition on the pharmacokinetics of varenicline, a new therapy for smoking cessation: an in vitro-in vivo study. Clin Pharmacol Ther. 2008 Apr;83(4):567-76. doi: 10.1038/sj.clpt.6100405. Epub 2007 Oct 31. [Article]
  2. Bergen AW, Javitz HS, Krasnow R, Michel M, Nishita D, Conti DV, Edlund CK, Kwok PY, McClure JB, Kim RB, Hall SM, Tyndale RF, Baker TB, Benowitz NL, Swan GE: Organic cation transporter variation and response to smoking cessation therapies. Nicotine Tob Res. 2014 Dec;16(12):1638-46. doi: 10.1093/ntr/ntu161. Epub 2014 Aug 20. [Article]

Drug created at May 16, 2007 20:24 / Updated at December 08, 2021 01:57