- ICH GCP
- US Clinical Trials Registry
- Clinical Trial NCT03420469
Bupropion Stereoselective Disposition and CYP2D6-mediated Drug Interactions in Healthy Volunteers
December 19, 2019 updated by: Zeruesenay Desta, Indiana University
Primary objectives:
- To comprehensively characterize steady state stereoselective pharmacokinetics of bupropion and its primary and secondary metabolites in healthy volunteers
- To prospectively determine the time course (onset), extent and offset of CYP2D6 inhibition in relation to the pharmacokinetic profiles of bupropion and metabolites.
Study Overview
Status
Completed
Intervention / Treatment
Study Type
Interventional
Enrollment (Actual)
28
Phase
- Early Phase 1
Contacts and Locations
This section provides the contact details for those conducting the study, and information on where this study is being conducted.
Study Locations
-
-
Indiana
-
Indianapolis, Indiana, United States, 46202
- Indiana Clinical Research Center (ICRC)
-
-
Participation Criteria
Researchers look for people who fit a certain description, called eligibility criteria. Some examples of these criteria are a person's general health condition or prior treatments.
Eligibility Criteria
Ages Eligible for Study
18 years to 55 years (Adult)
Accepts Healthy Volunteers
Yes
Genders Eligible for Study
All
Description
Inclusion Criteria:
- Male and female (approximately 1:1) volunteers between the age of 18 and 55 years old and within 32% of your ideal body weight.
- Judged healthy without any significant medical condition as determined by and decided from a pre-enrollment screening session that include medical history, laboratory tests such as blood and urine tests, and an electrical tracing of the heart beat (electrocardiogram, EKG).
- Individuals who agree to refrain from taking any prescriptions medications, over-the-counter medications, and herbal, dietary, and alternative supplements that may interact with the metabolism of those study drugs at least 2 weeks prior to the start of the study and until study completion.
- Nonsmoker or individuals willing to refrain from smoking or use of tobacco or marijuana for at least two weeks prior to and until the completion of the study (the entire study lasts for approximately 32 days).
- Willing to commit the time requested for this study
Exclusion Criteria:
Subjects will be excluded from the study if they:
- Are underweight (weigh less than 52 kg or 114 lb) or overweight [body mass index (BMI) greater than 32].
- Have laboratory results that do not fall in a healthy range (e.g., blood hemoglobin less than 12.0 mg/dl).
- Have baseline EKG readings that are abnormal that could place the patient at the higher risk as decided by the study medical doctor (MD)
- Have history of intolerance, allergic reactions (e.g. rash) or other forms of hypersensitivities to any of the study medications (dextromethorphan and bupropion).
- Have current alcohol (more than 4 alcoholic drinks per day on a regular basis) or drug abuse.
- Have history or current gastrointestinal (digestive) disorders such as persistent diarrhea or malabsorption that would interfere with the absorption of orally administered drugs
- Have history or current seizures, hypertension and heart disease or any other cardiovascular disorders
- Have history or current psychiatric (mental or brain) disorders (e.g., feeling sad or unhappy, loss of interest in normal activities, worried) such as depression, anxiety, or suicidality or suicide attempts.
- Have significantly compromised liver and/or kidney functions.
- Have participated in a research study involving intensive blood sampling or have donated blood within the past two months
- Are unable or unwilling to stop taking other substances that may interfere with the metabolism of the study drugs (bupropion and dextromethorphan) two weeks prior to and during the entire study period, including prescription medications, over-the-counter medications, herbal or dietary supplements, and alternative medicines.
- Are employees or students under supervision of any of the study investigators.
- Cannot state a good understanding of this study including risks and requirements; are unable to follow the rules of this study.
- Cannot commit the time requested for this study.
Study Plan
This section provides details of the study plan, including how the study is designed and what the study is measuring.
How is the study designed?
Design Details
- Primary Purpose: Basic Science
- Allocation: Non-Randomized
- Interventional Model: Sequential Assignment
- Masking: None (Open Label)
Arms and Interventions
Participant Group / Arm |
Intervention / Treatment |
---|---|
Experimental: Baseline CYP2D6 activity
CYP2D6 activity will be determined using a single oral dose of dextromethorphan (30 mg PO) as a probe drug at baseline (control).
|
Phase 1: Baseline CYP2D6 activity, using dextromethorphan (30 mg single dose PO) as a probe drug Phase 2: Single dose bupropion pharmacokinetics and its effect on CYP2D6 activity (determined by dextromethorphan 30 mg single dose PO) Phase 3: Steady state disposition of bupropion and its interaction with CYP2D6 activity (30 mg single dose PO)
|
Experimental: CYP2D6 activity with single dose of bupropion
The effect of a single dose of bupropion (150 mg PO) on CYP2D6 activity will be determined using a single oral dose of dextromethorphan (30 mg PO) as a probe drug.
|
Phase 1: Baseline CYP2D6 activity, using dextromethorphan (30 mg single dose PO) as a probe drug Phase 2: Single dose bupropion pharmacokinetics and its effect on CYP2D6 activity (determined by dextromethorphan 30 mg single dose PO) Phase 3: Steady state disposition of bupropion and its interaction with CYP2D6 activity (30 mg single dose PO)
|
Experimental: CYP2D6 activity after treatment with bupropion to steady sate
CYP2D6 activity will be determined using a single oral dose of dextromethorphan (30 mg PO) as a probe drug after 14 days pretreatment with bupropion (150 mg twice daily PO).
|
Phase 1: Baseline CYP2D6 activity, using dextromethorphan (30 mg single dose PO) as a probe drug Phase 2: Single dose bupropion pharmacokinetics and its effect on CYP2D6 activity (determined by dextromethorphan 30 mg single dose PO) Phase 3: Steady state disposition of bupropion and its interaction with CYP2D6 activity (30 mg single dose PO)
|
What is the study measuring?
Primary Outcome Measures
Outcome Measure |
Measure Description |
Time Frame |
---|---|---|
Exposure
Time Frame: Through study completion, an average of 2 year
|
Area under the plasma concentration versus time curves (AUC0-inf) of bupropion and its metabolites as well as CYP2D6 activity measured by dextromethorphan to dextrorphan
|
Through study completion, an average of 2 year
|
Collaborators and Investigators
This is where you will find people and organizations involved with this study.
Sponsor
Collaborators
Study record dates
These dates track the progress of study record and summary results submissions to ClinicalTrials.gov. Study records and reported results are reviewed by the National Library of Medicine (NLM) to make sure they meet specific quality control standards before being posted on the public website.
Study Major Dates
Study Start (Actual)
June 5, 2018
Primary Completion (Actual)
May 1, 2019
Study Completion (Actual)
May 1, 2019
Study Registration Dates
First Submitted
January 26, 2018
First Submitted That Met QC Criteria
February 1, 2018
First Posted (Actual)
February 5, 2018
Study Record Updates
Last Update Posted (Actual)
December 23, 2019
Last Update Submitted That Met QC Criteria
December 19, 2019
Last Verified
December 1, 2019
More Information
Terms related to this study
Additional Relevant MeSH Terms
- Chemically-Induced Disorders
- Drug-Related Side Effects and Adverse Reactions
- Physiological Effects of Drugs
- Neurotransmitter Agents
- Molecular Mechanisms of Pharmacological Action
- Enzyme Inhibitors
- Psychotropic Drugs
- Neurotransmitter Uptake Inhibitors
- Membrane Transport Modulators
- Antidepressive Agents
- Dopamine Agents
- Cytochrome P-450 Enzyme Inhibitors
- Antidepressive Agents, Second-Generation
- Cytochrome P-450 CYP2D6 Inhibitors
- Dopamine Uptake Inhibitors
- Bupropion
Other Study ID Numbers
- 1R01GM121707-01A1 (U.S. NIH Grant/Contract)
Plan for Individual participant data (IPD)
Plan to Share Individual Participant Data (IPD)?
NO
Drug and device information, study documents
Studies a U.S. FDA-regulated drug product
Yes
Studies a U.S. FDA-regulated device product
No
product manufactured in and exported from the U.S.
No
This information was retrieved directly from the website clinicaltrials.gov without any changes. If you have any requests to change, remove or update your study details, please contact register@clinicaltrials.gov. As soon as a change is implemented on clinicaltrials.gov, this will be updated automatically on our website as well.
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