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

Varenicline on Reward Responses and Cognition in Adolescent Smokers

Phase 1

Completed

Conditions: Tobacco Use Disorders

Interventions: Drug: Placebo
Drug: Varenicline

First Posted Date: 2012-06-20

Last Posted Date: 2014-02-03

Lead Sponsor: Yale University

Target Recruit Count: 16

Registration Number: NCT01624428

Locations: 🇺🇸
Substance Abuse Center, New Haven, Connecticut, United States

Tailored Tobacco Quitline for Rural Veterans

Phase 2

Completed

Conditions: Cigarette Smoking

Interventions: Drug: Nicotine replacement therapy - transdermal nicotine patch
Behavioral: Tailored behavioral intervention
Behavioral: Tobacco quit line referral
Drug: Nicotine replacement therapy - nicotine gum
Drug: Nicotine replacement therapy - nicotine lozenge
Drug: Bupropion Sustained Release
Drug: Varenicline
Drug: Combination pharmacotherapy - transdermal nicotine patch + nicotine gum
Drug: Combination pharmacotherapy - transdermal nicotine patch + nicotine lozenge
Drug: Combination pharmacotherapy - transdermal nicotine patch + bupropion
Behavioral: Alcohol use risk reduction
Behavioral: Behavioral activation for the treatment of depression
Behavioral: Behavioral management of post-cessation weight gain

First Posted Date: 2012-05-07

Last Posted Date: 2019-08-02

Lead Sponsor: Iowa City Veterans Affairs Medical Center

Target Recruit Count: 63

Registration Number: NCT01592695

Locations: 🇺🇸
Iowa City VA Health Care System, Iowa City, Iowa, United States

Varenicline as a Treatment for Methamphetamine Dependence

Phase 1

Completed

Conditions: Methamphetamine Dependence
Methamphetamine Abuse
Substance Abuse

Interventions: Drug: Placebo
Drug: Varenicline

First Posted Date: 2012-04-05

Last Posted Date: 2013-06-13

Lead Sponsor: Baylor College of Medicine

Target Recruit Count: 17

Registration Number: NCT01571167

Locations: 🇺🇸
Michael E. DeBakey Veterans Affairs Medical Center, Houston, Texas, United States

A Comparative Effectiveness & Long Term Health Study in Wisconsin Smokers

Phase 4

Completed

Conditions: Smoking
Nicotine Dependence
Smoking Cessation

Interventions: Drug: Nicotine Patch
Drug: Nicotine lozenge
Drug: Varenicline

First Posted Date: 2012-03-13

Last Posted Date: 2020-09-02

Lead Sponsor: University of Wisconsin, Madison

Target Recruit Count: 1086

Registration Number: NCT01553084

Locations: 🇺🇸
University of Wisconsin Center for Tobacco Research and Intervention, School of Medicine and Public Health, Milwaukee, Wisconsin, United States

Varenicline Treatment of Alcohol Dependence in Smokers

Phase 2

Completed

Conditions: Alcoholism
Alcohol Abuse
Smoking
Alcohol Drinking

Interventions: Drug: Varenicline

First Posted Date: 2012-03-13

Last Posted Date: 2020-03-06

Lead Sponsor: Yale University

Target Recruit Count: 131

Registration Number: NCT01553136

Locations: 🇺🇸
Connecticut Mental Health Center - Substance Abuse Treatment Unit, New Haven, Connecticut, United States
🇺🇸
Parallax Center, New York, New York, United States