Varenicline

Generic Name: Varenicline

Brand Names: Champix, Chantix, Tyrvaya

Drug Type: Small Molecule

Chemical Formula: C_₁₃H_₁₃N_₃

CAS Number: 249296-44-4

Unique Ingredient Identifier: W6HS99O8ZO

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.

Indication: For use as an aid in smoking cessation.

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

Associated Conditions: Dry Eye Syndrome (DES)

Associated Therapies: Smoking, Cessation

Clinical Trials

Pharmacogenetics of Nicotine Addiction Treatment

Phase 3

Completed

Conditions: Nicotine Addiction

Interventions: Drug: Placebo
Drug: Transdermal Nicotine
Drug: Varenicline

First Posted Date: 2011-03-14

Last Posted Date: 2016-03-03

Lead Sponsor: University of Pennsylvania

Target Recruit Count: 1246

Registration Number: NCT01314001

Locations: 🇺🇸
University at Buffalo - State University of New York, Buffalo, New York, United States
🇺🇸
Center for Interdisciplinary Research on Nicotine Addiction, University of Pennsylvania, Philadelphia, Pennsylvania, United States
🇨🇦
Centre for Addiction and Mental Health, University of Toronto, Toronto, Ontario, Canada

and more 1 locations

Effect of Varenicline on Tobacco Addiction and on Abstinence-induced Cognitive Impairment

Phase 1

Withdrawn

Conditions: Drug Addiction

First Posted Date: 2011-03-07

Last Posted Date: 2017-10-06

Lead Sponsor: National Institute on Drug Abuse (NIDA)

Registration Number: NCT01309685

Influence of Varenicline on the Antiplatelet Action of Clopidogrel

Not Applicable

Conditions: Coronary Artery Disease

Interventions: Behavioral: Counseling and psychosocial support
Drug: Varenicline

First Posted Date: 2011-03-04

Last Posted Date: 2015-06-24

Lead Sponsor: General Hospital of Chinese Armed Police Forces

Target Recruit Count: 198

Registration Number: NCT01308671

Locations: 🇨🇳
General Hospital of Chinese People's Armed Police Forces, Beijing, China

Varenicline-Aided Cigarette Reduction in Smokers Not Ready to Quit

Not Applicable

Completed

Conditions: Tobacco Use Disorder

Interventions: Drug: Placebo pill
Drug: Varenicline

First Posted Date: 2011-03-04

Last Posted Date: 2017-07-17

Lead Sponsor: Rutgers, The State University of New Jersey

Target Recruit Count: 73

Registration Number: NCT01308736

Locations: 🇺🇸
Division of Addiction Psychiatry, New Brunswick, New Jersey, United States

Concurrent Bupropion / Varenicline for Smoking Cessation

Phase 3

Completed

Conditions: Nicotine Dependence

Interventions: Drug: Nicotine patches
Drug: Varenicline
Drug: Nicotine Inhaler
Drug: Bupropion

First Posted Date: 2011-02-25

Last Posted Date: 2014-08-06

Lead Sponsor: Duke University

Target Recruit Count: 702

Registration Number: NCT01303861

Locations: 🇺🇸
Duke Center for Nicotine and Smoking Cessation Research, Winston-Salem, North Carolina, United States

Varenicline Pregnancy Cohort Study

Completed

Conditions: Malformations

Interventions: Drug: varenicline
Behavioral: cigarette smoke from maternal smoking
Other: Non-Exposure

First Posted Date: 2011-02-07

Last Posted Date: 2023-07-24

Lead Sponsor: Pfizer

Target Recruit Count: 885185

Registration Number: NCT01290445

Varenicline in Drug Treatment

Phase 4

Completed

Conditions: Alcohol Abuse
Smoking Cessation

Interventions: Drug: placebo
Drug: varenicline

First Posted Date: 2011-01-31

Last Posted Date: 2015-02-05

Lead Sponsor: Centre for Addiction and Mental Health

Target Recruit Count: 33

Registration Number: NCT01286584

Locations: 🇨🇦
Centre for Addiction and Mental Health, Nicotine Dependence Clinic, Toronto, Ontario, Canada

A Multi-National Study To Assess How Effective And Safe The Smoking Cessation Medicine Varenicline Is In Smokers Who Have Already Tried Varenicline In The Past As A Prescription Medicine From Their Usual Healthcare Provider

Phase 4

Completed

Conditions: Smoking Cessation

Interventions: Drug: Placebo
Drug: Varenicline

First Posted Date: 2010-11-19

Last Posted Date: 2014-06-09

Lead Sponsor: Pfizer

Target Recruit Count: 498

Registration Number: NCT01244061

Locations: 🇺🇸
Ronald Reagan University of California Los Angeles Medical Center, Los Angeles, California, United States
🇦🇺
Royal Brisbane and Women's Hospital, Herston, Queensland, Australia
🇨🇦
Canadian Phase Onward Inc., Toronto, Ontario, Canada

and more 34 locations