HealthyPhase 4NCT02401256
CYP2B6 Genetics and Drug Interactions in Healthy Volunteers
A Phase 4 study testing Efavirenz, Bupropion and Rosuvastatin in people with Healthy, run by Indiana University at 1 site in United States.
Trial summary
The CYP2B6 enzyme metabolizes a growing number of clinically important drugs such as the anti-HIV drug efavirenz, but its activity in the liver is highly variable, which may lead to failure of therapy or toxicity and unpredictable drug interactions. Genetic and several nongenetic factors affect the activity of CYP2B6. Read more about this study
- Who is it for?
- Ages 18 to 49 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy
- What is being tested?
- Efavirenz, Bupropion and Rosuvastatin
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 70 participants
- Where
- 1 siteUnited States
- Study dates
- Jul 2013to 31 May 2016
- Phase
- Phase 4
- Are there results?
- Yes, posted in the registrySummary in the doctors' view
Key requirements
Who can take part, as listed by the sponsor. Only the study team can confirm whether you are eligible, so take this list to your doctor.
- Ages 18 to 49 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- 18 to 49 years old healthy male and female participants within 32% of their ideal body weight
- Individuals who agree to refrain from taking any prescriptions medications, over-the-counter medications, hormonal agents, 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 one month prior to and until the completion of the study (the entire study lasts for approximately 38 days)
Who cannot join
- Are underweight (less than 114 lb) or overweight (BMI greater than 32)
- Have history or current alcohol or drug abuse (more than 4 alcoholic drinks per day on a regular basis)
- Have history of intolerance, allergic reactions (e.g. rash) or other forms of hypersensitivities to any of the study medications (efavirenz, montelukast, bupropion and rosuvastatin)
- Have history or current significant health conditions such as heart, liver, or kidney
- Have history or current psychiatric illness such as depression, anxiety, or nervousness that may be exacerbated by participation in study
- Have a history of suicidality including suicide attempts
Show all 21Show fewer
- Have history or current gastrointestinal disorders such as persistent diarrhea or malabsorption that would interfere with the absorption of orally administered drugs
- Have a serious infection within the last week before study enrollment
- Have a baseline EKG readings that is abnormal that could place the patient at the higher risk as decided by the study medical doctor (MD)
- Have donated blood within the past two months
- Have blood results that do not fall in a healthy range
- Are taking on regular basis substances that may interfere with the metabolism of study medications by the body, including prescription medications, over-the-counter, herbal or dietary supplements, alternative medications, or hormonal agents
- Are female with a positive pregnancy urine test obtained just prior to each study
- Are female breastfeeding
- Are child-bearing potential unable or unwilling to either practice abstinence or use two non-hormonal forms of birth control up until the study completion, which will take a total of 38 days
- Have a life style that places subjects at a higher risk for contracting HIV (e.g. drug abuse, excessive alcohol drinking, and having multiple sexual partners)
- Have a history or current HIV infection
- Have participation in a research study or use of an investigational drug in the last one month
- Are employed or are student under supervision of any of the investigators of this study
- 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
Trial locations and contacts
1 site in 1 country.
United States1 site
Indiana University School of Medicine
Indianapolis, Indiana, 46202
About this study
Official title: Influence of Autoinhibition/Autoinduction and CYP2B6 Genetic Variations on CYP2B6 Activity and Drug Interactions in Healthy Volunteers
The CYP2B6 enzyme metabolizes a growing number of clinically important drugs such as the anti-HIV drug efavirenz, but its activity in the liver is highly variable, which may lead to failure of therapy or toxicity and unpredictable drug interactions. Genetic and several nongenetic factors affect the activity of CYP2B6. The goal of this study is to determine the impact of simultaneous autoinhibition/autoinduction and CYP2B6 genetics on CYP2B6 activity, efavirenz exposure and efavirenz-mediated drug interactions. The pharmacokinetics and drug interactions will be determined on three occasions in a total of 60 healthy volunteers. The whole study will have 4 phases. A) Phase 1 (baseline control): using selective probe substrates, the baseline activities of CYP2B6 (bupropion), CYP2C8 (montelukast) and OATP1B1 (rosuvastatin) are determined. B) Phase 2 (inhibition): the metabolism and pharmacokinetics of a single 600 mg oral dose of efavirenz) and the activities of CYP2B6, CYP2C8 and OATP1B1 (inhibition) are determined. C) Phase 3 (treatment phase): After completing phase 2, subjects take 600 mg/day efavirenz at home for 17 days. C) Phase 4 (induction and inhibition): At the end of phase 3, steady state metabolism and pharmacokinetics of efavirenz and the activities of CYP2B6, CYP2C8 and OATP1B1 will be determined. Efavirenz serves as a model substrate, inhibitor and inducer of CYP2B6 (and other drug disposition proteins). Bupropion 4-hydroxylation is an alternative in vivo probe of CYP2B6 activity and will be studied here in addition to the metabolism and pharmacokinetics of efavirenz.
Read the detailed description
Schedule of assessment
PHASE 1 (CONTROL PHASE)
Phase 1 (day 1 to day 4): baseline (control) activities of CYP2B6, CYP2C8 and OATP1B1 will be measured using selective probe substrates. Eligible subjects will receive simultaneously a single 100 mg dose of bupropion (CYP2B6), a single 10 mg dose montelukast (CYP2C8) and a single 5 mg dose of rosuvastatin (OATP1B1) by mouth on empty stomach together at least 10 days before phase 2. Frequent plasma samples will be collected for 72 hours and urine for 48 hours after dosing. Safety assessment will be made for the first 24 hours. Phase 1 is completed after the last blood draw on day 4 (72 hours).
PHASE 2 (INHIBITION PHASE)
In phase 2 (days 11 to 16), the metabolism and pharmacokinetics of a single 600 mg oral dose efavirenz will be determined along with the activities of CYP2B6, CYP2C8 and OATP1B1. Subjects receive a single 600 mg oral dose of efavirenz and blood samples will be obtained at 30 min and 1 hour. Immediately after the 1 hour blood draw, the three probe drugs (10 mg montelukast, 100 mg bupropion, and 5 mg rosuvastatin) will be administered simultaneously. Frequent plasma samples will be collected for 120 hours and urine for 48 hours after efavirenz dosing. Safety assessment will be made for the first 24 hours. Phase 2 is completed after the last blood draw on day 16 (120 hours). Note: The additional time points (compared to phase 1) are needed because of the long elimination half-life of efavirenz.
PHASE 3 (EFAVIRENZ TREATMENT PHASE).
In phase 3 (days 16 to 32), subjects will take efavirenz (600 mg/day) every evening for 17 days (Note: Phase 3 starts when the subject takes the first dose that evening on Day 16). Prior to taking the evening dose, they will be requested to return to the Indiana Clinical Research Center on day 19, day 22, day 25, day 28 and day 31 for a brief outpatient visit to have vital signs checked, draw blood sample (~10 ml, approximately 2 teaspoonful), and to fill out the brief central nervous system (CNS) symptoms questionnaire. They will be reminded not to take the evening dose of efavirenz on these days until after their blood draw. Since efavirenz has a long half-life (~76 hours after single dose and ~50 at steady state), a total of 17 days of efavirenz treatment is required to achieve steady-state plasma concentrations of efavirenz and steady-state autoinduction of metabolism. Subjects will be instructed to take efavirenz at bed-time to minimize efavirenz-induced central nervous side effects. Minor rescheduling (±3 days) of the subject's fixed inpatient/outpatient visits will be allowed including adjusting the amount of study medication (up to 3 doses less or up to 3 doses more) to be given prior to the subject's 4th inpatient visit.
PHASE 4 (INHIBITION/INDUCTION PHASE)
In phase 4 (days 33 to 38), the steady-state metabolism and pharmacokinetics of efavirenz will be determined along the activities of CYP2B6, CYP2C8 and OATP1B1. The procedures described in phase 2 will be repeated. On day 38, an exit exam will be performed consisting of a repeat of a repeat of the screening laboratory tests including blood and urine tests. The study diary will be collected. Medication bottles with left over pills (if any) will be returned and pills remaining will be counted for compliance purposes. The total duration of the study will be 38 days.
- Conditions
- Healthy
- Being tested
- Efavirenz, Bupropion, Rosuvastatin, Montelukast
- Keywords
- Efavirenz, metabolism, pharmacokinetics changes
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
EfavirenzDrug
Also called Sustiva
The study has 4 phases:
Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control).
Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs.
Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days).
Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements.
BupropionDrug
Also called Wellbutrin
The study has 4 phases:
Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control).
Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs.
Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days).
Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements.
RosuvastatinDrug
Also called Crestor
The study has 4 phases:
Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control).
Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs.
Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days).
Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements.
MontelukastDrug
Also called Singulair
The study has 4 phases:
Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control).
Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs.
Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days).
Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements.
| Study group | Role | What they receive |
|---|---|---|
| CYP2B6 | Experimental | This is a fixed-order, open label prospective cohort study to determine: a) the contribution of CYP2B6 autoinhibition/autoinduction processes to variable CYP2B6 activity and efavirenz exposure; b) the impact of CYP2B6 genetic variants on these processes; and c) drug interactions that ensue.
Included drugs:
Efavirenz (600mg) - The volunteers will receive it in two of three inpatient visits and also during 17 days at home
Bupropion (100mg), Montelukast (10mg) and Rosuvastatin (5mg) - These drugs will be administrated on 3 occasions (at the begging each inpatient visit of Phase 1, 2 and 4). Receives: Drug: Efavirenz; Drug: Bupropion; Drug: Rosuvastatin; Drug: Montelukast |
What is being measured
The primary outcome is the main question the study is designed to answer.
Efavirenz AUC0-inf (Single Dose) and AUC0-24(Multiple Dose)
After the samples collection, blood from phase 2 and phase 4 were used to perform the quantification of Efavirenz in plasma. The composite of the efavirenz concentration (blood collection between 0 to 120 hrs) were used to calculate the area under the plasma concentration time curve (AUC0-inf for single dose and AUC0-24 for multiple dose) of efavirenz.
Measured: Single dose pharmacokinetics (PK) versus multiple doses (after 17 day pretreatment) PK (total 38 days for each subject)
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted27 Mar 2015 (estimated)
- Study startJul 2013
- Primary completionMay 2016
- Study completion31 May 2016
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Posted resultsParticipant flow, outcome measures and adverse events reported by the sponsor.
- Other trials for HealthyStudies of the same condition, open and under way.
- More trials run by Indiana UniversityThe sponsor's other registered studies.
- What the trial phases meanHow a treatment moves from first tests in people to approval.
More details
For doctors and researchers: how the study is designed, who runs it, and its registry IDs.
Study design
- Study type
- Interventional
- Phase
- Phase 4
- Primary purpose
- Treatment
- Allocation
- Not applicable
- Intervention model
- Single group
- Masking
- None (open label)
- Enrolment
- 70 participants (actual)
Sponsor and investigators
- Lead sponsor
- Indiana University
- Sponsor type
- University, hospital or other
- Collaborators
- National Institute of General Medical Sciences (NIGMS)
- Responsible party
- Principal investigator, Zeruesenay Desta, Indiana University
- Investigators
- Zeruesenay Desta, PhD, Principal investigator, +1 (317) 274-2823
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT02401256
- Sponsor's protocol ID
- 1205008739
- Other IDs
- 5R01GM078501
- Status last verified
- Sep 2017
- First submitted
- 26 Feb 2015
- Last updated
- 11 Oct 2017
- Results posted
- Yes, on ClinicalTrials.gov
- Data monitoring committee
- Yes
- Individual data sharing
- No
Study at a glance
From the registry record, last updated by the sponsor on 11 Oct 2017. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- Influence of Autoinhibition/Autoinduction and CYP2B6 Genetic Variations on CYP2B6 Activity and Drug Interactions in Healthy Volunteers
- ClinicalTrials.gov ID
- NCT02401256
- Acronym / sponsor ID
- 1205008739
- Conditions
- Healthy
- Keywords
- Efavirenz, metabolism, pharmacokinetics changes
- Phase
- Phase 4
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 70 participants (actual)
- Lead sponsor
- Indiana UniversityUniversity, hospital or other
- Collaborators
- National Institute of General Medical Sciences (NIGMS)
- Study start
- Jul 2013
- Primary completion
- May 2016 (actual)
- Study completion
- 31 May 2016 (actual)
- First posted
- 27 Mar 2015 (estimated)
- Results
- Posted 11 Oct 2017
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The CYP2B6 enzyme metabolizes a growing number of clinically important drugs such as the anti-HIV drug efavirenz, but its activity in the liver is highly variable, which may lead to failure of therapy or toxicity and unpredictable drug interactions. Genetic and several nongenetic factors affect the activity of CYP2B6. The goal of this study is to determine the impact of simultaneous autoinhibition/autoinduction and CYP2B6 genetics on CYP2B6 activity, efavirenz exposure and efavirenz-mediated drug interactions. The pharmacokinetics and drug interactions will be determined on three occasions in a total of 60 healthy volunteers. The whole study will have 4 phases. A) Phase 1 (baseline control): using selective probe substrates, the baseline activities of CYP2B6 (bupropion), CYP2C8 (montelukast) and OATP1B1 (rosuvastatin) are determined. B) Phase 2 (inhibition): the metabolism and pharmacokinetics of a single 600 mg oral dose of efavirenz) and the activities of CYP2B6, CYP2C8 and OATP1B1 (inhibition) are determined. C) Phase 3 (treatment phase): After completing phase 2, subjects take 600 mg/day efavirenz at home for 17 days. C) Phase 4 (induction and inhibition): At the end of phase 3, steady state metabolism and pharmacokinetics of efavirenz and the activities of CYP2B6, CYP2C8 and OATP1B1 will be determined. Efavirenz serves as a model substrate, inhibitor and inducer of CYP2B6 (and other drug disposition proteins). Bupropion 4-hydroxylation is an alternative in vivo probe of CYP2B6 activity and will be studied here in addition to the metabolism and pharmacokinetics of efavirenz.
Detailed description
Schedule of assessment
PHASE 1 (CONTROL PHASE)
Phase 1 (day 1 to day 4): baseline (control) activities of CYP2B6, CYP2C8 and OATP1B1 will be measured using selective probe substrates. Eligible subjects will receive simultaneously a single 100 mg dose of bupropion (CYP2B6), a single 10 mg dose montelukast (CYP2C8) and a single 5 mg dose of rosuvastatin (OATP1B1) by mouth on empty stomach together at least 10 days before phase 2. Frequent plasma samples will be collected for 72 hours and urine for 48 hours after dosing. Safety assessment will be made for the first 24 hours. Phase 1 is completed after the last blood draw on day 4 (72 hours).
PHASE 2 (INHIBITION PHASE)
In phase 2 (days 11 to 16), the metabolism and pharmacokinetics of a single 600 mg oral dose efavirenz will be determined along with the activities of CYP2B6, CYP2C8 and OATP1B1. Subjects receive a single 600 mg oral dose of efavirenz and blood samples will be obtained at 30 min and 1 hour. Immediately after the 1 hour blood draw, the three probe drugs (10 mg montelukast, 100 mg bupropion, and 5 mg rosuvastatin) will be administered simultaneously. Frequent plasma samples will be collected for 120 hours and urine for 48 hours after efavirenz dosing. Safety assessment will be made for the first 24 hours. Phase 2 is completed after the last blood draw on day 16 (120 hours). Note: The additional time points (compared to phase 1) are needed because of the long elimination half-life of efavirenz.
PHASE 3 (EFAVIRENZ TREATMENT PHASE).
In phase 3 (days 16 to 32), subjects will take efavirenz (600 mg/day) every evening for 17 days (Note: Phase 3 starts when the subject takes the first dose that evening on Day 16). Prior to taking the evening dose, they will be requested to return to the Indiana Clinical Research Center on day 19, day 22, day 25, day 28 and day 31 for a brief outpatient visit to have vital signs checked, draw blood sample (~10 ml, approximately 2 teaspoonful), and to fill out the brief central nervous system (CNS) symptoms questionnaire. They will be reminded not to take the evening dose of efavirenz on these days until after their blood draw. Since efavirenz has a long half-life (~76 hours after single dose and ~50 at steady state), a total of 17 days of efavirenz treatment is required to achieve steady-state plasma concentrations of efavirenz and steady-state autoinduction of metabolism. Subjects will be instructed to take efavirenz at bed-time to minimize efavirenz-induced central nervous side effects. Minor rescheduling (±3 days) of the subject's fixed inpatient/outpatient visits will be allowed including adjusting the amount of study medication (up to 3 doses less or up to 3 doses more) to be given prior to the subject's 4th inpatient visit.
PHASE 4 (INHIBITION/INDUCTION PHASE)
In phase 4 (days 33 to 38), the steady-state metabolism and pharmacokinetics of efavirenz will be determined along the activities of CYP2B6, CYP2C8 and OATP1B1. The procedures described in phase 2 will be repeated. On day 38, an exit exam will be performed consisting of a repeat of a repeat of the screening laboratory tests including blood and urine tests. The study diary will be collected. Medication bottles with left over pills (if any) will be returned and pills remaining will be counted for compliance purposes. The total duration of the study will be 38 days.
Study design
- Primary purpose
- Treatment
- Allocation
- Not applicable
- Intervention model
- Single group
- Masking
- None (open label)
- Number of arms
- 1
| Arm | Type | Receives |
|---|---|---|
| CYP2B6 | Experimental | Drug: Efavirenz, Drug: Bupropion, Drug: Rosuvastatin, Drug: MontelukastThis is a fixed-order, open label prospective cohort study to determine: a) the contribution of CYP2B6 autoinhibition/autoinduction processes to variable CYP2B6 activity and efavirenz exposure; b) the impact of CYP2B6 genetic variants on these processes; and c) drug interactions that ensue. Included drugs: Efavirenz (600mg) - The volunteers will receive it in two of three inpatient visits and also during 17 days at home Bupropion (100mg), Montelukast (10mg) and Rosuvastatin (5mg) - These drugs will be administrated on 3 occasions (at the begging each inpatient visit of Phase 1, 2 and 4). |
Who may qualify
- Ages
- 18 to 49 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (3 listed)
- 18 to 49 years old healthy male and female participants within 32% of their ideal body weight
- Individuals who agree to refrain from taking any prescriptions medications, over-the-counter medications, hormonal agents, 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 one month prior to and until the completion of the study (the entire study lasts for approximately 38 days)
Key exclusion criteria (21 listed)
- Are underweight (less than 114 lb) or overweight (BMI greater than 32)
- Have history or current alcohol or drug abuse (more than 4 alcoholic drinks per day on a regular basis)
- Have history of intolerance, allergic reactions (e.g. rash) or other forms of hypersensitivities to any of the study medications (efavirenz, montelukast, bupropion and rosuvastatin)
- Have history or current significant health conditions such as heart, liver, or kidney
- Have history or current psychiatric illness such as depression, anxiety, or nervousness that may be exacerbated by participation in study
Eligibility is decided by the study team after screening; this overview does not establish that a patient qualifies. Full inclusion and exclusion criteria.
Interventions
| Intervention | Type | Arms |
|---|---|---|
| EfavirenzAlso: SustivaThe study has 4 phases: Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control). Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs. Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days). Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements. | Drug | CYP2B6 |
| BupropionAlso: WellbutrinThe study has 4 phases: Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control). Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs. Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days). Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements. | Drug | CYP2B6 |
| RosuvastatinAlso: CrestorThe study has 4 phases: Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control). Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs. Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days). Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements. | Drug | CYP2B6 |
| MontelukastAlso: SingulairThe study has 4 phases: Phase 1 (control)-Subjects will receive simultaneously a single dose of bupropion 100 mg, montelukast 10 mg and rosuvastatin 5 mg (cocktail) by mouth (control). Phase 2 (inhibition)- a single 600 mg oral dose of efavirenz (blood draw at 30 min and 1 hour) will be administered with the cocktail drugs. Phase 3 (home treatment with efavirenz): Subjects will take efavirenz at home (600 mg/day for 17 days). Phase 4 (Induction) - is the same as phase 2. Blood samples (0 to 120 hrs) and urine voided over 48 hrs (Phases 1, 2 and 4) are collected. Blood draws will be made in phase 3 for trough concentration measurements. | Drug | CYP2B6 |
Primary outcome
Efavirenz AUC0-inf (Single Dose) and AUC0-24(Multiple Dose)
Time frame: Single dose pharmacokinetics (PK) versus multiple doses (after 17 day pretreatment) PK (total 38 days for each subject)
After the samples collection, blood from phase 2 and phase 4 were used to perform the quantification of Efavirenz in plasma. The composite of the efavirenz concentration (blood collection between 0 to 120 hrs) were used to calculate the area under the plasma concentration time curve (AUC0-inf for single dose and AUC0-24 for multiple dose) of efavirenz.
Results and safety
Loading the posted results from ClinicalTrials.gov…
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 11 Oct 2017.
- Posted resultsParticipant flow, baseline, all outcome measures and adverse events.
- Individual participant dataSharing planned: No
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Referral and contact
AzTrials does not enrol participants or take referrals. Contact the study team or a site listed below; they decide who can take part. This study is not recruiting at the moment.
Zeruesenay Desta, PhD principal investigator
+1 (317) 274-2823
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 4 study testing Efavirenz, Bupropion and Rosuvastatin in people with Healthy, run by Indiana University at 1 site in United States.
The full registered description is in the About this study section and the official record.
Who may be eligible to take part?
The sponsor lists 3 inclusion and 21 exclusion criteria. Eligibility is decided by the study team after screening, so read the full criteria and contact a listed site.
Is this clinical trial currently recruiting?
The record says: finished, as of the sponsor's last update on 11 Oct 2017. Status can change between updates, so confirm with the study contact before making plans.
Where is the study taking place?
The record lists 1 site in United States. Whether a site is taking part right now should be confirmed with that site. See every site.
What are the possible benefits and risks?
They depend on the study and the treatment, and no study can promise a benefit. The study team explains the known risks during informed consent, before anyone joins; the record itself does not list them.
What does this phase mean?
Phase 4 studies take place after a treatment is approved, to learn more about its long-term benefits and risks in everyday use.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
Yes. Results are posted in the registry (first posted 11 Oct 2017). A summary is in the For doctors view, and the full results are on ClinicalTrials.gov.
How can a doctor refer a patient or contact the research team?
The record lists no contact. The official record names the sponsor, who can be asked directly. AzTrials does not enrol participants or take referrals.
What does the primary outcome measure?
Efavirenz AUC0-inf (Single Dose) and AUC0-24(Multiple Dose) (time frame: Single dose pharmacokinetics (PK) versus multiple doses (after 17 day pretreatment) PK (total 38 days for each subject)). It is what the study was designed to measure, not a finding.
Where can I read the original study information?
Does a listing mean the treatment is approved or proven to work?
No. A listing means the study is registered. It does not show that the treatment is safe, works, or is approved by a regulator.
How often is this information updated?
AzTrials copies changed records from ClinicalTrials.gov every night and reloads the whole registry every week. The sponsor last updated this record on 11 Oct 2017; AzTrials last refreshed its copy on 7 Nov 2026.