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

Mobile Evidence-Based Smoking Cessation for Veterans Living With HIV (MESH)

Phase 4

Completed

Conditions: Smoking
Human Immunodeficiency Virus

Interventions: Drug: Bupropion
Drug: Varenicline
Behavioral: Cognitive Behavioral Therapy
Drug: Nicotine Replacement Therapy
Behavioral: Relapse Prevention Text Messaging

First Posted Date: 2019-10-23

Last Posted Date: 2023-07-27

Lead Sponsor: VA Office of Research and Development

Target Recruit Count: 12

Registration Number: NCT04135937

Locations: 🇺🇸
Durham VA Medical Center, Durham, NC, Durham, North Carolina, United States

Varenicline Light Smoking Pilot

Phase 4

Completed

Conditions: Smoking Cessation
Smoking Behaviors
Smoking

Interventions: Drug: Varenicline
Drug: Placebo oral tablet

First Posted Date: 2019-09-16

Last Posted Date: 2021-05-11

Lead Sponsor: Duke University

Target Recruit Count: 11

Registration Number: NCT04089982

Locations: 🇺🇸
Duke University, Durham, North Carolina, United States

Deep rTMS and Varenicline for Smoking Cessation

Not Applicable

Completed

Conditions: Tobacco Use Disorder
Smoking Cessation

Interventions: Device: Deep Repetitive Transcranial Magnetic Stimulation (Active)
Device: Deep Repetitive Transcranial Magnetic Stimulation (Sham)
Drug: Varenicline

First Posted Date: 2019-09-10

Last Posted Date: 2024-11-04

Lead Sponsor: Centre for Addiction and Mental Health

Target Recruit Count: 50

Registration Number: NCT04083144

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

A Clinical Study to Evaluate the Pharmacokinetics, Safety and Tolerability of HIP1502

Phase 1

Completed

Conditions: Healthy

Interventions: Drug: varenicline oxalate 1mg (HIP1502, T) - varenicline tartrate 1mg (HGP1604, R), TR
Drug: varenicline tartrate 1mg (HGP1604, R) - varenicline oxalate 1mg (HIP1502, T), RT

First Posted Date: 2019-07-12

Last Posted Date: 2019-07-12

Lead Sponsor: Korea University Anam Hospital

Target Recruit Count: 30

Registration Number: NCT04018378

Locations: 🇰🇷
Dept. of Clinical Pharmacology & Toxicology, Anam Hospital, Korea University College of Medicine, Seoul, Korea, Republic of

Varenicline Versus Cytisine for Smoking Cessation in Primary Care Setting

Phase 3

Completed

Conditions: Smoking Cessation

Interventions: Drug: Varenicline
Drug: Cytisine

First Posted Date: 2019-07-11

Last Posted Date: 2022-11-03

Lead Sponsor: University of Zagreb

Target Recruit Count: 352

Registration Number: NCT04015414

Locations: 🇭🇷
University of Zagreb School of Medicine, Zagreb, Croatia
🇸🇮
University of Ljubljana School of Medicine, Ljubljana, Slovenia

Novel Pharmacotherapy Approaches in Smokers With Serious Mental Illness

Phase 4

Completed

Conditions: Nicotine Dependence
Bipolar Disorder
Schizophrenia
Schizoaffective Disorder

Interventions: Drug: Varenicline

First Posted Date: 2019-07-08

Last Posted Date: 2023-06-22

Lead Sponsor: University of California, San Diego

Target Recruit Count: 39

Registration Number: NCT04011280

Locations: 🇺🇸
Pacific Treatment & Research Center at UCSD, La Jolla, California, United States

UH3 Varenicline for Cannabis Use Disorder

Phase 2

Completed

Conditions: Cannabis Use Disorder

Interventions: Drug: Placebo
Drug: Varenicline

First Posted Date: 2019-06-10

Last Posted Date: 2024-01-18

Lead Sponsor: Medical University of South Carolina

Target Recruit Count: 174

Registration Number: NCT03980561

Locations: 🇺🇸
Behavioral Health Services of Pickens County, Pickens, South Carolina, United States
🇺🇸
Medical University of South Carolina, Charleston, South Carolina, United States

Individualizing Pharmacotherapy for African American Smokers

Phase 3

Completed

Conditions: Smoking Cessation

Interventions: Drug: Nicotine patch
Drug: Varenicline Tartrate
Drug: Bupropion

First Posted Date: 2019-04-01

Last Posted Date: 2023-04-03

Lead Sponsor: University of Kansas Medical Center

Target Recruit Count: 392

Registration Number: NCT03897439

Locations: 🇺🇸
Swope Health Central, Kansas City, Missouri, United States

Using Non-invasive Brain Stimulation (tDCS) With Varenicline for Treating Tobacco Dependence

Not Applicable

Completed

Conditions: Tobacco Dependence
Smoking Cessation
Tobacco Smoking
Tobacco Use Disorder
Substance Use Disorders
Molecular Mechanisms of Pharmacological Action
Physiological Effects of Drugs