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varenicline

Trade name: chantix

Small moleculeapproved

Approved

May 10, 2006

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. Varenicline is an alpha-4 beta-2 neuronal nicotinic acetylcholine receptor partial agonist. The drug shows high selectiviyty 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. Varenicline is sold under the trade name Chantix and Champix, it is indicated for use as an aid to smoking cessation treatment. — NCATS

Clinical trial activity

320 trials · 184 clinical orgs · 22 marketing orgs

Phase 1
42
Phase 2
126
Phase 3
66
Phase 4
90

Earliest trial started Feb 1, 2000 (NCT00150241)

Timeline

2000s

  1. Jan 1, 2000

    Pfizer — Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2003

    Pfizer — Earliest Phase 3 Sponsor(trial)

  3. May 10, 2006

    Pfizer — Earliest FDA Approval

  4. May 10, 2006

    Pfizer — NDA Organization

  5. Jan 1, 2007

    Pfizer — Earliest Phase 1 Sponsor(trial)

2010s

  1. May 15, 2012

    Apotex — Marketing Organization

  2. May 3, 2013

    Mylan — Marketing Organization

  3. Sep 10, 2013

    Teva — Marketing Organization

  4. Dec 15, 2016

    Watson Pharmaceuticals — Marketing Organization

  5. Dec 15, 2016

    Allergan PLC (2015) — Marketing Organization

2020s

  1. Aug 11, 2021

    Par Pharmaceuticals — Marketing Organization

  2. Aug 11, 2021

    Bristol-Myers Squibb — Marketing Organization

  3. Aug 11, 2021

    Endo Pharmaceuticals — Marketing Organization

  4. Oct 15, 2021

    Oyster Point Pharma, Inc. — Marketing Organization

  5. Oct 15, 2021

    Oyster Point Pharma, Inc. — NDA Secondary Org

  6. Jun 12, 2023

    Zydus Discovery DMCC — Marketing Organization

  7. Jul 25, 2023

    Medley Pharmaceutical Industry SA — Marketing Organization

  8. Aug 1, 2023

    Mankind Pharma — Marketing Organization

  9. Aug 23, 2023

    Alkem Labs Ltd — Marketing Organization

  10. Oct 23, 2023

    Hetero Labs Ltd — Marketing Organization

  11. Dec 4, 2023

    Lupin — Marketing Organization

  12. Mar 6, 2024

    Bionpharma Inc — Marketing Organization

  13. Mar 19, 2024

    Ajanta Pharma Ltd — Marketing Organization

  14. Jul 23, 2024

    Piramal — Marketing Organization

  15. Oct 1, 2024

    Dr. Reddy's Laboratories — Marketing Organization

  16. Oct 29, 2024

    Indoco Remedies — Marketing Organization

  17. Dec 9, 2024

    Macleods Pharmaceuticals, Ltd — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewMay 10, 2006

Chemistry & pharmacology

Loading structure…

SMILES

c1cnc2cc3c(cc2n1)C1CNCC3C1
Mol. weight
211.27 g/mol
Lipinski Ro5
Pass
Rule of 3
Yes
Chirality
Racemic Mixture
Inorganic
No
Polymer
No
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • champix
  • champix
  • champix
  • chantix
  • chantix
  • chantix
  • chantix
  • chantix
  • cp-526,555
  • cp-526,555
  • cp-526,555-18
  • cp-526555-18
  • cp-526555-18
  • oc-01
  • varencicline
  • varencline
  • vareniciline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline
  • varenicline tartrate
  • varenicline tartrate
  • varenicline tartrate
  • varenicline tartrate

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07099638Phase 2Jan 5, 2026Brown University, National Cancer Institute (NCI), Thomas Jefferson University, University of Oklahoma
NCT06966362Phase 4Dec 1, 2025Department of Veteran Affairs
NCT07171112Phase 2Nov 6, 2025Mayo Clinic
NCT07040566Phase 2Nov 4, 2025Medical University of South Carolina, National Cancer Institute (NCI), Yale University
NCT07145866Phase 4Oct 1, 2025Harvard University
NCT06883162Phase 3May 6, 2025Medical University of South Carolina, National Cancer Institute (NCI)
NCT06832085Phase 4Apr 30, 2025University of Ottawa
NCT06854406Phase 1Apr 1, 2025Mayo Clinic
NCT06798324Phase 4Mar 1, 2025Canadian Institutes of Health Research (CIHR), University of Toronto
NCT06679374Phase 2Feb 28, 2025National Institute of Neurological Disorders and Stroke (NINDS), University of Michigan
NCT06780215Phase 3Jan 16, 2025Huazhong University of Science and Technology
NCT06582888Early Phase 1 (Phase 1)Dec 15, 2024National Institute on Drug Abuse (NIDA), University of California, San Diego
NCT06688539Phase 4Dec 9, 2024Medical University of South Carolina, National Cancer Institute (NCI)
NCT06609369Phase 2Dec 1, 2024National Institute on Drug Abuse (NIDA), Yale University
NCT06474299Phase 4Sep 24, 2024National Cancer Institute (NCI), University of Wisconsin
NCT06006143N/ASep 1, 2024National Institute on Alcohol Abuse and Alcoholism (NIAAA), Yale University
NCT06218823Phase 4Mar 1, 2024National Cancer Institute (NCI), University of Wisconsin
NCT06027840Phase 1Dec 31, 2023National Cancer Institute (NCI), Yale University
NCT06029907Phase 4Dec 15, 2023Duke University
NCT05786547Phase 3Dec 15, 2023Harvard University, National Cancer Institute (NCI), University of Colorado, Denver
Showing 20 of 320 trials
Page 1 / 16

Organizations

Research & Development (184)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
PfizerFor profit803852000
National Institute on Drug Abuse (NIDA)Government54152005
National Cancer Institute (NCI)Government27152005
Yale UniversityAcademic/Hospital212142007
University of PennsylvaniaAcademic/Hospital191942006
Mayo ClinicAcademic/Hospital161552007
University of TorontoAcademic/Hospital161442007
Medical University of South CarolinaAcademic/Hospital13652007
National Institute on Alcohol Abuse and Alcoholism (NIAAA)Government13342007
National Institutes of Health (NIH)Government12042005
Duke UniversityAcademic/Hospital111152009
Department of Veteran AffairsGovernment10542007
Harvard UniversityAcademic/Hospital10742007
Oyster Point Pharma, Inc.For profit10742018
University of WisconsinAcademic/Hospital8812009
University of California, Los AngelesAcademic/Hospital7732008
Brown UniversityAcademic/Hospital6522007
University of Texas at HoustonAcademic/Hospital6632005
New York UniversityAcademic/Hospital5432007
University of KansasAcademic/Hospital5532008
184 organizations
Page 1 / 10

Marketing (26)

OrganizationOrg typeRelationshipDate
Ajanta Pharma LtdFor profitMKTGMar 19, 2024
Alkem Labs LtdFor profitMKTGAug 23, 2023
Allergan PLC (2015)For profitMKTGDec 15, 2016
ApotexFor profitMKTGMay 15, 2012
ApotexFor profitSYNJun 2, 2020
Bionpharma IncFor profitMKTGMar 6, 2024
Bristol-Myers SquibbFor profitMKTGAug 11, 2021
Dr. Reddy's LaboratoriesFor profitMKTGOct 1, 2024
Endo PharmaceuticalsFor profitMKTGAug 11, 2021
Hetero Labs LtdFor profitMKTGOct 23, 2023
Indoco RemediesFor profitMKTGOct 29, 2024
LupinFor profitMKTGDec 4, 2023
Macleods Pharmaceuticals, LtdFor profitMKTGDec 9, 2024
Mankind PharmaFor profitMKTGAug 1, 2023
Medley Pharmaceutical Industry SAFor profitMKTGJul 25, 2023
MylanFor profitMKTGMay 3, 2013
MylanFor profitSYNFeb 29, 2024
Oyster Point Pharma, Inc.For profitMKTGOct 15, 2021
Oyster Point Pharma, Inc.For profitNDA2Oct 15, 2021
Par PharmaceuticalsFor profitMKTGAug 11, 2021
PfizerFor profitNDAMay 10, 2006
PfizerFor profitSYNMay 10, 2006
PiramalFor profitMKTGJul 23, 2024
TevaFor profitMKTGSep 10, 2013
Watson PharmaceuticalsFor profitMKTGDec 15, 2016
Zydus Discovery DMCCFor profitMKTGJun 12, 2023