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 Treatment for Smoking Cessation in Patients With Bipolar Disorder

Phase 4

Completed

Conditions: Smoking Cessation
Bipolar Disorder

Interventions: Drug: Placebo
Drug: Varenicline

First Posted Date: 2009-11-09

Last Posted Date: 2017-12-04

Lead Sponsor: K.N. Roy Chengappa

Target Recruit Count: 60

Registration Number: NCT01010204

Locations: 🇺🇸
Dubois Regional Medical Center, DuBois, Pennsylvania, United States
🇺🇸
Western Psychiatric Institute and Clinic, Pittsburgh, Pennsylvania, United States

Effect of Varenicline on Fixed-Dose Alcohol Administration in Participants With Alcohol Use Disorders

Phase 2

Completed

Conditions: Alcohol Reactivity

Interventions: Drug: placebo
Drug: varenicline

First Posted Date: 2009-10-23

Last Posted Date: 2018-02-19

Lead Sponsor: Yale University

Target Recruit Count: 44

Registration Number: NCT01000987

Locations: 🇺🇸
Yale Center for Clinical Investigation, Yale Human Behavioral Pharmacology Laboratory, New Haven, Connecticut, United States

Efficacy and Safety of NicVAX® Co-administered With Varenicline (Champix®)

Phase 2

Completed

Conditions: Smoking Behavior
Smoking Lapse Behavior
Smoking Relapse Behavior

Interventions: Biological: NicVAX vaccine
Biological: Placebo
Drug: Varenicline

First Posted Date: 2009-10-14

Last Posted Date: 2013-02-20

Lead Sponsor: Maastricht University Medical Center

Target Recruit Count: 558

Registration Number: NCT00995033

Locations: 🇳🇱
Maastricht University Medical Center, Maastricht, Limburg, Netherlands
🇳🇱
Slotervaart Hospital/ Smoking Cessation Clinic, Amsterdam, Noord-Holland, Netherlands

Study to Determine the Safety and Tolerability of Varenicline (Chantix®) in Treating Spinocerebellar Ataxia Type 3

Phase 2

Completed

Conditions: Spinocerebellar Ataxia Type 3

Interventions: Drug: varenicline
Drug: placebo

First Posted Date: 2009-10-09

Last Posted Date: 2012-06-18

Lead Sponsor: University of South Florida

Target Recruit Count: 20

Registration Number: NCT00992771

Locations: 🇺🇸
University of South Florida, Tampa, Florida, United States
🇺🇸
University of Florida, Gainesville, Florida, United States
🇺🇸
University of California - Los Angeles, Los Angeles, California, United States