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
Structure for Varenicline (DB01273)
- 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
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Symptomatic treatment of Dry eye syndrome (des) •••••••••••• ••••••••• ••••• - Associated Therapies
- Contraindications & Blackbox Warnings
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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.
Target Actions Organism ANeuronal acetylcholine receptor subunit alpha-4 partial agonistHumans UNeuronal acetylcholine receptor subunit alpha-7 agonistHumans UNeuronal acetylcholine receptor subunit alpha-3 partial agonistHumans UNeuronal acetylcholine receptor subunit alpha-6 partial agonistHumans UNeuronal acetylcholine receptor subunit beta-2 partial agonistHumans - 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
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Not Available
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Varenicline which could result in a higher serum level. Acebutolol The risk or severity of adverse effects can be increased when Acebutolol is combined with Varenicline. Aceclofenac Aceclofenac may decrease the excretion rate of Varenicline which could result in a higher serum level. Acemetacin Acemetacin may decrease the excretion rate of Varenicline which could result in a higher serum level. Acetaminophen Acetaminophen may decrease the excretion rate of Varenicline which could result in a higher serum level. - Food Interactions
- Avoid excessive or chronic alcohol consumption. Varenicline may increase the effects of alcohol; therefore, reduce consumption of alcohol when starting varenicline.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Varenicline tartrate 82269ASB48 375815-87-5 TWYFGYXQSYOKLK-CYUSMAIQSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-varenicline Tablet, film coated 1 mg/1 Oral Apotex Corp 2021-07-16 2024-07-31 US 
Apo-varenicline Tablet, film coated 0.5 mg/1 Oral Apotex Corp 2021-07-16 2025-03-31 US Champix Tablet, film coated 1 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU 
Champix Tablet, film coated 0.5 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU Champix Tablet, film coated 1.0 mg Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-varenicline Tablet 1 mg Oral Apotex Corporation 2018-05-02 Not applicable Canada 
Apo-varenicline Tablet 0.5 mg Oral Apotex Corporation 2018-05-02 Not applicable Canada Gd-varenicline Tablet 1 mg Oral Genmed A Division Of Pfizer Canada Ulc Not applicable Not applicable Canada Gd-varenicline Tablet 0.5 mg Oral Genmed A Division Of Pfizer Canada Ulc Not applicable Not applicable Canada PMS-varenicline Tablet 0.5 mg Oral Pharmascience Inc Not applicable Not applicable Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Apo-varenicline Varenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg) Kit; Tablet Oral Apotex Corporation 2018-06-12 Not applicable Canada Apo-varenicline Varenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg) Kit; Tablet Oral Apotex Corporation 2018-06-12 Not applicable Canada Champix Varenicline tartrate (0.5 mg) + Varenicline tartrate (1 mg) Kit; Tablet Oral Pfizer Canada Ulc 2007-10-02 Not applicable Canada CHAMPIX Varenicline (0.5 mg) + Varenicline (1 mg) Tablet, film coated Oral Pfizer Europe Ma Eeig 2014-07-08 Not applicable Italy 
CHAMPIX Varenicline (0.5 mg) + Varenicline (1 mg) Tablet, film coated Oral Pfizer Europe Ma Eeig 2014-07-08 Not applicable Italy - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Apo-varenicline Varenicline tartrate (0.5 mg/1) + Varenicline tartrate (1 mg/1) Kit; Tablet, film coated Oral Apotex Corp 2021-07-16 2023-01-23 US Apo-varenicline Varenicline tartrate (1 mg/1) Tablet, film coated Oral Apotex Corp 2021-07-16 2024-07-31 US Apo-varenicline Varenicline tartrate (0.5 mg/1) + Varenicline tartrate (1 mg/1) Kit; Tablet, film coated Oral Apotex Corp 2021-07-16 2023-01-23 US Apo-varenicline Varenicline tartrate (0.5 mg/1) Tablet, film coated Oral Apotex Corp 2021-07-16 2025-03-31 US
Categories
- ATC Codes
- S01XA28 — Varenicline
- S01XA — Other ophthalmologicals
- S01X — OTHER OPHTHALMOLOGICALS
- S01 — OPHTHALMOLOGICALS
- S — SENSORY ORGANS
- Drug Categories
- Benzazepines
- Cholinergic Agents
- Cholinergic Agonists
- Cholinergic Receptor Agonist
- Drugs that are Mainly Renally Excreted
- Drugs Used in Addictive Disorders
- Drugs Used in Nicotine Dependence
- Heterocyclic Compounds, Fused-Ring
- Miscellaneous Autonomic Drugs
- Nervous System
- Neurotransmitter Agents
- Nicotinic Agonists
- OCT2 Inhibitors
- OCT2 Substrates
- Ophthalmologicals
- Partial Cholinergic Nicotinic Agonist
- Partial Cholinergic Nicotinic Agonists
- Quinoxalines
- Sensory Organs
- Smoking Cessation Agents
- 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
- 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]
- 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]
- 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]
- 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]
- Kuehn BM: FDA speeds smoking cessation drug review. JAMA. 2006 Feb 8;295(6):614. [Article]
- FDA Approved Drug Products: TYRVAYA (varenicline) nasal spray [Link]
- External Links
- Human Metabolome Database
- HMDB0015398
- PubChem Compound
- 5310966
- PubChem Substance
- 46505502
- ChemSpider
- 148958
- BindingDB
- 50166908
- 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 Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Active Not Recruiting Health Services Research Smoking, Cessation / Smoking, Cigarette 1 4 Active Not Recruiting Treatment Cigarette Smokers / Tobacco Use Disorders 1 4 Active Not Recruiting Treatment Nicotine Dependence / Vaping 1 4 Active Not Recruiting Treatment Opioid Use Disorder (OUD) / Tobacco Use Disorders 1 4 Active Not Recruiting Treatment Tobacco Use Cessation 1
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
Form Route Strength Tablet Oral 0.5 mg Tablet Oral 1.0 MG Tablet Oral 1.000 mg Tablet, film coated Oral Tablet, coated Oral Tablet, coated Oral 0.5 mg Tablet, film coated Oral 0.5 mg Tablet, coated Oral Tablet, film coated Oral 1 mg Tablet, film coated Oral 1.0 MG Tablet, film coated Oral 1 mg/tablet Tablet, film coated Oral 0.5 mg Kit Oral Kit Oral 0.5 mg/1 Kit; tablet, film coated Oral Tablet, film coated Oral .5 mg/1 Tablet, film coated Oral 0.5 mg/1 Tablet, film coated Oral 1 mg/1 Tablet, film coated Oral 1.0 mg/1 Kit; tablet Oral Tablet Oral 1 mg Tablet Oral Spray Nasal 0.03 mg/0.05mL Tablet, film coated Oral 0.5 mg/561 Tablet, film coated Oral 1 mg/561 Tablet, film coated Oral 1.71 mg Tablet, coated Oral 1 mg - Prices
Unit description Cost Unit Chantix Continuing Month Pak 56 1 mg tablet Disp Pack 148.5USD disp Chantix Starting Month Pak 0.5 mg X 11, 1 mg X 42 Disp Pack 148.5USD disp Chantix 1 mg tablet 2.61USD tablet Chantix 0.5 mg tablet 2.56USD tablet Chantix 1 mg cont month pak 2.56USD each DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region CA2525874 No 2007-11-27 2024-05-07 Canada CA2316921 No 2004-12-07 2018-11-13 Canada US6410550 Yes 2002-06-25 2020-11-10 US US6890927 Yes 2005-05-10 2022-11-06 US US7265119 Yes 2007-09-04 2023-02-03 US US10456396 No 2019-10-29 2035-10-19 US US9597284 No 2017-03-21 2035-10-19 US US9532944 No 2017-01-03 2035-10-19 US US9504644 No 2016-11-29 2035-10-19 US US9504645 No 2016-11-29 2035-10-19 US US11224598 No 2015-10-19 2035-10-19 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source logP 0.9 Not Available - Predicted Properties
Property Value Source Water Solubility 0.0877 mg/mL ALOGPS logP 1.39 ALOGPS logP 1.01 Chemaxon logS -3.4 ALOGPS pKa (Strongest Basic) 9.73 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 37.81 Å2 Chemaxon Rotatable Bond Count 0 Chemaxon Refractivity 61.3 m3·mol-1 Chemaxon Polarizability 23.12 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9969 Blood Brain Barrier + 0.9908 Caco-2 permeable - 0.5233 P-glycoprotein substrate Substrate 0.5458 P-glycoprotein inhibitor I Non-inhibitor 0.7453 P-glycoprotein inhibitor II Non-inhibitor 0.9637 Renal organic cation transporter Inhibitor 0.5489 CYP450 2C9 substrate Non-substrate 0.8933 CYP450 2D6 substrate Non-substrate 0.6522 CYP450 3A4 substrate Non-substrate 0.7428 CYP450 1A2 substrate Non-inhibitor 0.507 CYP450 2C9 inhibitor Non-inhibitor 0.881 CYP450 2D6 inhibitor Inhibitor 0.6251 CYP450 2C19 inhibitor Non-inhibitor 0.8029 CYP450 3A4 inhibitor Non-inhibitor 0.6589 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.5453 Ames test Non AMES toxic 0.7128 Carcinogenicity Non-carcinogens 0.9592 Biodegradation Not ready biodegradable 0.9906 Rat acute toxicity 2.5914 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9382 hERG inhibition (predictor II) Inhibitor 0.5497
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0190000000-6a71a14a3d7d846e2bb5 Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-26a6da687803fbe379b7 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-03di-0190000000-27153010084484008811 Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-03di-0090000000-32dc73070779406a5db3 Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-001i-1900000000-e6055204d1a2b581af2e Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-001l-2900000000-7f435ebf2942f9a1d691 Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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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
- 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]
- 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]
- 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]
- 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]
- 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
- 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
- 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
- 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
- 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
- SubstrateInhibitor
- 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
- 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]
- 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 February 20, 2024 23:54