Pharmacogenetics of Nicotine Addiction Treatment

NCT ID: NCT01314001

Last Updated: 2016-03-03

Study Results

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Basic Information

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Recruitment Status

COMPLETED

Clinical Phase

PHASE3

Total Enrollment

1246 participants

Study Classification

INTERVENTIONAL

Study Start Date

2010-12-31

Study Completion Date

2014-09-30

Brief Summary

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The purpose of this research program is to understand how a biomarker called the "nicotine metabolite ratio" (also referred to as NMR) may influence a smoker's ability to quit smoking.

Detailed Description

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Smoking is an enormous public health problem with a great need for research to improve treatment outcomes. Our prior data indicates that the cytochrome P450 2A6 (CYP2A6) enzyme is critical in the metabolic inactivation of nicotine, and also influences smoking behavior and response to therapies. With a vision toward translation of our research to practice, we have characterized a genetically-informed biomarker of CYP2A6 activity, specifically the nicotine metabolite ratio (NMR; 3'hydroxycotinine/cotinine), which reflects both CYP2A6 genetic variation and environmental influences on CYP2A6 activity. The NMR is measured non-invasively in smokers with established reliability, stability, analytic validity, and efficacy as a predictor of the ability to quit smoking and treatment response in multiple retrospective trials. Translation of these findings to clinical practice requires validation in a prospective clinical trial comparing alternative therapies for smoking cessation. Thus, the proposed trial is a prospective, stratified, placebo-controlled, multi-center clinical trial of alternative therapies for smoking cessation treatment in approximately 1,200 smokers. Randomization to placebo (PLA), transdermal nicotine (TN), or varenicline (VAR) will be stratified prospectively based on the nicotine metabolite ratio (NMR). Abstinence from smoking at the end of treatment will be the primary outcome. Quit rate at 6-month follow-up is a secondary outcome. To facilitate translation to practice, analysis of the cost-effectiveness of our proposed approach will also be completed. The proposed research provides the next critical step to validate a genetically-informed diagnostic tool, the NMR, which clinicians can use in the future to optimize treatment decisions for their patients who wish to quit smoking.

Conditions

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Nicotine Addiction

Study Design

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Allocation Method

RANDOMIZED

Intervention Model

PARALLEL

Primary Study Purpose

TREATMENT

Blinding Strategy

TRIPLE

Participants Caregivers Investigators

Study Groups

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Placebo (Slow Metabolizers)

Subjects in this arm are those identified as slow metabolizers of nicotine (based on their NMR) and will take placebo pills daily for twelve weeks \& wear a placebo patch daily for eleven weeks.

The placebo pill will look identical to the active varenicline tablets; however, they will not contain any active medication. Subjects will follow the same drug regimen as those in the active varenicline arm.

The placebo patch will look identical to the active transdermal nicotine patches; however, they do not contain actual nicotine. Subjects will follow the same regimen as those in the active transdermal nicotine arm.

All subjects in this arm will receive smoking cessation counseling during their sessions.

Group Type PLACEBO_COMPARATOR

Placebo

Intervention Type DRUG

Day 1-3: 0.5mg once daily orally Day 4-7: 0.5mg twice daily orally Day 8-84: 1.0mg twice daily orally

Week 1 - 6: 21mg placebo patch Week 7 - 8: 14mg placebo patch Week 9 - 11: 7mg placebo patch

Varenicline (Slow Metabolizers)

Subjects in this arm are those identified as slow metabolizers of nicotine (based on their NMR) and will take active varenicline pills daily for twelve weeks \& wear a placebo patch daily for eleven weeks.

When taking the active varenicline, subjects will follow the same treatment regimen per the manufacturer.

The placebo patch will look identical to the active transdermal nicotine patches; however, they do not contain actual nicotine. Subjects will follow the same regimen as those in the active transdermal nicotine arm.

All subjects in this arm will receive smoking cessation counseling during their sessions.

Group Type ACTIVE_COMPARATOR

Varenicline

Intervention Type DRUG

Day 1-3: 0.5mg once daily orally Day 4-7: 0.5mg twice daily orally Day 8-84: 1.0mg twice daily orally

Transdermal Nicotine (Slow Metabolizers)

Subjects in this arm are those identified as slow metabolizers of nicotine (based on their NMR) and will take placebo pills daily for twelve weeks \& will wear an active transdermal nicotine patch daily for eleven weeks.

The placebo pill will look identical to the active varenicline tablets; however, they will not contain any active medication. Subjects will follow the same drug regimen as those in the active varenicline arm.

When wearing the active transdermal nicotine, subjects will follow the same treatment regimen per the manufacturer.

All subjects in this arm will receive smoking cessation counseling during their sessions.

Group Type ACTIVE_COMPARATOR

Transdermal Nicotine

Intervention Type DRUG

Week 1-6: 21mg nicotine patch Week 7-8: 14mg nicotine patch Week 9-11: 7mg nicotine patch

Placebo (Normal Metabolizers)

Subjects in this arm are those identified as normal metabolizers of nicotine (based on their NMR) and will take placebo pills daily for twelve weeks \& wear a placebo patch daily for eleven weeks.

The placebo pill will look identical to the active varenicline tablets; however, they will not contain any active medication. Subjects will follow the same drug regimen as those in the active varenicline arm.

The placebo patch will look identical to the active transdermal nicotine patches; however, they do not contain actual nicotine. Subjects will follow the same regimen as those in the active transdermal nicotine arm.

All subjects in this arm will receive smoking cessation counseling during their sessions.

Group Type PLACEBO_COMPARATOR

Placebo

Intervention Type DRUG

Day 1-3: 0.5mg once daily orally Day 4-7: 0.5mg twice daily orally Day 8-84: 1.0mg twice daily orally

Week 1 - 6: 21mg placebo patch Week 7 - 8: 14mg placebo patch Week 9 - 11: 7mg placebo patch

Varenicline (Normal Metabolizers)

Subjects in this arm are those identified as normal metabolizers of nicotine (based on their NMR) and will take active varenicline pills daily for twelve weeks \& wear a placebo patch daily for eleven weeks.

When taking the active varenicline, subjects will follow the same treatment regimen per the manufacturer.

The placebo patch will look identical to the active transdermal nicotine patches; however, they do not contain actual nicotine. Subjects will follow the same regimen as those in the active transdermal nicotine arm.

All subjects in this arm will receive smoking cessation counseling during their sessions.

Group Type ACTIVE_COMPARATOR

Varenicline

Intervention Type DRUG

Day 1-3: 0.5mg once daily orally Day 4-7: 0.5mg twice daily orally Day 8-84: 1.0mg twice daily orally

Transdermal Nicotine (Normal Metabolizers)

Subjects in this arm are those identified as normal metabolizers of nicotine (based on their NMR) and will take placebo pills daily for twelve weeks \& will wear an active transdermal nicotine patch daily for eleven weeks.

The placebo pill will look identical to the active varenicline tablets; however, they will not contain any active medication. Subjects will follow the same drug regimen as those in the active varenicline arm.

When wearing the active transdermal nicotine, subjects will follow the same treatment regimen per the manufacturer.

All subjects in this arm will receive smoking cessation counseling during their sessions.

Group Type ACTIVE_COMPARATOR

Transdermal Nicotine

Intervention Type DRUG

Week 1-6: 21mg nicotine patch Week 7-8: 14mg nicotine patch Week 9-11: 7mg nicotine patch

Interventions

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Varenicline

Day 1-3: 0.5mg once daily orally Day 4-7: 0.5mg twice daily orally Day 8-84: 1.0mg twice daily orally

Intervention Type DRUG

Placebo

Day 1-3: 0.5mg once daily orally Day 4-7: 0.5mg twice daily orally Day 8-84: 1.0mg twice daily orally

Week 1 - 6: 21mg placebo patch Week 7 - 8: 14mg placebo patch Week 9 - 11: 7mg placebo patch

Intervention Type DRUG

Transdermal Nicotine

Week 1-6: 21mg nicotine patch Week 7-8: 14mg nicotine patch Week 9-11: 7mg nicotine patch

Intervention Type DRUG

Other Intervention Names

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Chantix Placebo pills Placebo patches Nicoderm CQ Nicotine Patch

Eligibility Criteria

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Inclusion Criteria

Eligible participants will be males and females

1. Between the ages of 18-65.
2. Smoke at least 10 cigarettes/day for the past 6 months.
3. Provide a baseline Carbon Monoxide (CO) reading greater than 10ppm at the Intake Session.
4. Are seeking smoking cessation treatment.
5. Plan to live in the area for the next 12 months.
6. Fluent English speaker.
7. Capable of giving written informed consent, which includes compliance with the requirements and restrictions listed in the combined consent and Health Insurance Portability and Accountability Act (HIPAA) form. All subjects must consent to use a medically accepted method of birth control (e.g., condoms and spermicide, oral contraceptive, Depo-Provera injection, contraceptive patch, tubal ligation) or abstain from sexual intercourse during the time they are taking study medication (pills and patches) and for at least one month after the medication period ends. All female subjects of child-bearing potential should not be pregnant for the duration of the study.

Exclusion Criteria

Smoking Behavior

1. Regular (daily) use of chewing tobacco, snuff or snus.
2. Current enrollment or plans to enroll in another smoking cessation or research program in the next 12 months.
3. Plan to use other nicotine substitutes or smoking cessation treatments in the next 12 months.
4. Provide a baseline CO reading less than or equal to 10ppm at the Intake Session.


1. History (within the last year) or currently receiving treatment for substance abuse (e.g., alcohol, opioids, cocaine, marijuana, or stimulants), excluding nicotine.
2. Current use of cocaine and/or methamphetamines (urine drug screen at the Intake Session).
3. Current alcohol consumption that exceeds greater than 25 standard drinks/week.
4. Current alcohol abuse or dependence.
5. Current non-alcoholic psychoactive substance abuse or dependence.


1. Women who are pregnant, planning a pregnancy, or lactating.
2. History of epilepsy or a seizure disorder.
3. Current medical problems for which transdermal nicotine is contraindicated including:

* Allergy to latex.
* History of kidney and/or liver disease, including transplant (self-report).
* Uncontrolled hypertension (determined as a Systolic Blood pressure (SBP) reading greater than 160 and/or a Diastolic Blood Pressure (DBP) greater than 100).
4. Serious or unstable disease within the past 6 months.
5. History (last 6 months) of abnormal heart rhythms, tachycardia and cardiovascular disease (stroke, angina, heart attack) may result in ineligibility. These conditions will be evaluated on a case by case basis by the Study Physician.
6. Inability to provide a blood sample to be used to assess nicotine metabolite ratio.


1. Current diagnosis of major depression. Persons with a history of major depression, if stable for 6 months or longer, are eligible, provided they are not excluded based on medications (below).
2. Any suicide risk score on MINI or self-reported suicide attempt on telephone screen.
3. Current or past hypomanic/manic episode.
4. History or current diagnosis of Post Traumatic Stress Disorder (PTSD).
5. History or current diagnosis of psychotic disorder, bipolar disorder, schizophrenia.


1. Current use or recent discontinuation (within the last 14-days) of:

* Smoking cessation medication (e.g. Zyban, Wellbutrin, Wellbutrin SR, Chantix); NOTE: Once participants are found eligible for the study, they are instructed to use the smoking cessation medication provided to them by the study staff. If a subject reports an isolated (non-daily) instance of using a non-study smoking cessation medication, the study physician and PI will evaluate the situation and determine if it is safe for the subject to continue participation.
* Anti-psychotic medications.
* Certain medications used to treat depression, including Wellbutrin, Monoamine Oxidase Inhibitors (MAOIs), and tricyclic antidepressants.
* Prescription stimulants (e.g. Provigil, Ritalin, Adderall).
2. Current use of:

* Nicotine replacement therapy (NRT); NOTE: Once participants are found eligible for the study, they are told they should only use the NRT provided to them by the study staff. If a subject reports an isolated (non-daily) instance of NRT use during the study, they may be permitted to continue.
* Tagamet (cimetidine).
* Heart medications such as digoxin, quinidine, nitroglycerin; use of these medications may result in ineligibility and will therefore be evaluated on a case-by-case basis by the Study Physician.
* Anti-coagulants (e.g., Coumadin, Warfarin).
3. Daily use of:

* Opiate-containing medications for chronic pain; if a participant reports taking an opiate-containing medication every day for the 14 days prior to the telephone screen and/or Intake Session, the participant will be ineligible.
* Rescue Inhalers (e.g. albuterol, proventil, ventolin, or maxair)

General Exclusion

1. Any medical condition, illness, disorder or concomitant medication that could compromise participant safety or treatment, as determined by the Principal Investigator and/or Study Physician.
2. Inability to provide informed consent or complete any of the study tasks as determined by the Principal Investigator and/or Study Physician.
Minimum Eligible Age

18 Years

Maximum Eligible Age

65 Years

Eligible Sex

ALL

Accepts Healthy Volunteers

No

Sponsors

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National Institute on Drug Abuse (NIDA)

NIH

Sponsor Role collaborator

University of Pennsylvania

OTHER

Sponsor Role lead

Responsible Party

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Responsibility Role SPONSOR

Principal Investigators

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Caryn Lerman, PhD

Role: PRINCIPAL_INVESTIGATOR

University of Pennsylvania

Rachel F Tyndale, PhD

Role: PRINCIPAL_INVESTIGATOR

University of Toronto

Locations

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University at Buffalo - State University of New York

Buffalo, New York, United States

Site Status

Center for Interdisciplinary Research on Nicotine Addiction, University of Pennsylvania

Philadelphia, Pennsylvania, United States

Site Status

MD Anderson Cancer Center, University of Texas

Houston, Texas, United States

Site Status

Centre for Addiction and Mental Health, University of Toronto

Toronto, Ontario, Canada

Site Status

Countries

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United States Canada

References

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Tonkin SS, Betts JM, Dowd AN, Mahoney MC, Cinciripini PM, Schnoll RA, George TP, Tyndale RF, Hawk LW Jr. Daily cigarette abstinence and smoking rate with varenicline: Relationships with treatment, craving, and affect during the first week of the quit attempt. Nicotine Tob Res. 2025 May 4:ntaf095. doi: 10.1093/ntr/ntaf095. Online ahead of print.

Reference Type DERIVED
PMID: 40358028 (View on PubMed)

Chenoweth MJ, Kim YJ, Nollen NL, Hawk LW Jr, Mahoney MC, Lerman C, Knight J, Tyndale RF. Genetic Prediction of Smoking Cessation Medication Side Effects: A Genome-Wide Investigation of Abnormal Dreams on Varenicline. Clin Pharmacol Ther. 2024 Jun;115(6):1277-1281. doi: 10.1002/cpt.3210. Epub 2024 Feb 19.

Reference Type DERIVED
PMID: 38369951 (View on PubMed)

Chenoweth MJ, Lerman C, Knight J, Tyndale RF. Influence of CYP2A6 Genetic Variation, Nicotine Dependence Severity, and Treatment on Smoking Cessation Success. Nicotine Tob Res. 2023 May 22;25(6):1207-1211. doi: 10.1093/ntr/ntac268.

Reference Type DERIVED
PMID: 36789481 (View on PubMed)

Tonkin SS, Colder C, Mahoney MC, Swan GE, Cinciripini P, Schnoll R, George TP, Tyndale RF, Hawk LW. Evaluating Treatment Mechanisms of Varenicline: Mediation by Affect and Craving. Nicotine Tob Res. 2022 Oct 26;24(11):1803-1810. doi: 10.1093/ntr/ntac138.

Reference Type DERIVED
PMID: 35639828 (View on PubMed)

Chenoweth MJ, Lerman C, Knight J, Tyndale RF. A Genome-Wide Association Study of Nausea Incidence in Varenicline-Treated Cigarette Smokers. Nicotine Tob Res. 2021 Aug 29;23(10):1805-1809. doi: 10.1093/ntr/ntab044.

Reference Type DERIVED
PMID: 33713409 (View on PubMed)

El-Boraie A, Chenoweth MJ, Pouget JG, Benowitz NL, Fukunaga K, Mushiroda T, Kubo M, Nollen NL, Sanderson Cox L, Lerman C, Knight J, Tyndale RF. Transferability of Ancestry-Specific and Cross-Ancestry CYP2A6 Activity Genetic Risk Scores in African and European Populations. Clin Pharmacol Ther. 2021 Oct;110(4):975-985. doi: 10.1002/cpt.2135. Epub 2021 Jan 1.

Reference Type DERIVED
PMID: 33300144 (View on PubMed)

Peng AR, Swardfager W, Benowitz NL, Ahluwalia JS, Lerman C, Nollen NL, Tyndale RF. Impact of early nausea on varenicline adherence and smoking cessation. Addiction. 2020 Jan;115(1):134-144. doi: 10.1111/add.14810. Epub 2019 Nov 5.

Reference Type DERIVED
PMID: 31502736 (View on PubMed)

Ashare RL, Thompson M, Leone F, Metzger D, Gross R, Mounzer K, Tyndale RF, Lerman C, Mahoney MC, Cinciripini P, George TP, Collman RG, Schnoll R. Differences in the rate of nicotine metabolism among smokers with and without HIV. AIDS. 2019 May 1;33(6):1083-1088. doi: 10.1097/QAD.0000000000002127.

Reference Type DERIVED
PMID: 30946162 (View on PubMed)

Robinson JD, Li L, Chen M, Lerman C, Tyndale RF, Schnoll RA, Hawk LW, George TP, Benowitz NL, Cinciripini PM. Evaluating the temporal relationships between withdrawal symptoms and smoking relapse. Psychol Addict Behav. 2019 Mar;33(2):105-116. doi: 10.1037/adb0000434. Epub 2019 Jan 7.

Reference Type DERIVED
PMID: 30614717 (View on PubMed)

Peng AR, Schnoll R, Hawk LW Jr, Cinciripini P, George TP, Lerman C, Tyndale RF. Predicting smoking abstinence with biological and self-report measures of adherence to varenicline: Impact on pharmacogenetic trial outcomes. Drug Alcohol Depend. 2018 Sep 1;190:72-81. doi: 10.1016/j.drugalcdep.2018.04.035. Epub 2018 Jun 26.

Reference Type DERIVED
PMID: 29986268 (View on PubMed)

Hamilton DA, Mahoney MC, Novalen M, Chenoweth MJ, Heitjan DF, Lerman C, Tyndale RF, Hawk LW Jr. Test-Retest Reliability and Stability of the Nicotine Metabolite Ratio Among Treatment-Seeking Smokers. Nicotine Tob Res. 2015 Dec;17(12):1505-9. doi: 10.1093/ntr/ntv031. Epub 2015 Mar 1.

Reference Type DERIVED
PMID: 25732567 (View on PubMed)

Lerman C, Schnoll RA, Hawk LW Jr, Cinciripini P, George TP, Wileyto EP, Swan GE, Benowitz NL, Heitjan DF, Tyndale RF; PGRN-PNAT Research Group. Use of the nicotine metabolite ratio as a genetically informed biomarker of response to nicotine patch or varenicline for smoking cessation: a randomised, double-blind placebo-controlled trial. Lancet Respir Med. 2015 Feb;3(2):131-138. doi: 10.1016/S2213-2600(14)70294-2. Epub 2015 Jan 12.

Reference Type DERIVED
PMID: 25588294 (View on PubMed)

Chenoweth MJ, Novalen M, Hawk LW Jr, Schnoll RA, George TP, Cinciripini PM, Lerman C, Tyndale RF. Known and novel sources of variability in the nicotine metabolite ratio in a large sample of treatment-seeking smokers. Cancer Epidemiol Biomarkers Prev. 2014 Sep;23(9):1773-82. doi: 10.1158/1055-9965.EPI-14-0427. Epub 2014 Jul 10.

Reference Type DERIVED
PMID: 25012994 (View on PubMed)

Other Identifiers

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U01DA020830

Identifier Type: NIH

Identifier Source: secondary_id

View Link

811722

Identifier Type: -

Identifier Source: org_study_id

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