Healthy Adult FemalesPhase 1NCT01330199
Pharmacokinetics of Tenofovir, Emtricitabine, Maraviroc, and Raltegravir in Cervical, Vaginal, and Rectal Tissues and Secretions
A Phase 1 study testing Pharmacokinetic Sampling in people with Healthy Adult Females, run by University of North Carolina, Chapel Hill at 1 site in United States.
Trial summary
The purpose of this study is to develop a predictive antiretroviral pharmacokinetic model of mucosal fluid and tissue distribution in genital tract fluid, rectal fluid and 3 mucosal tissues. Read more about this study
- Who is it for?
- Ages 18 to 49 years, women onlyHealthy volunteers can take part
- Conditions the study is for
- Healthy Adult Females
- What is being tested?
- Pharmacokinetic Sampling
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 49 participants
- Where
- 1 siteUnited States
- Study dates
- Feb 2012to Aug 2013
- Phase
- Phase 1
- Are there results?
- None posted in the registry
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
- Women only
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy pre-menopausal female subjects between the ages of 18 and 49 years, inclusive, with an intact gastrointestinal tract, uterus, and cervix. (Healthy is defined as no irregular menstrual cycles or clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests.)
- All subjects must have an estimated calculated creatinine clearance of at least 80 mL/min by the Cockcroft-Gault formula
- All subjects must have a negative serum pregnancy test at screening and negative urine pregnancy tests on days of sampling and should be using at least one of the following methods of contraception:
- Systemic hormonal contraceptive (oral, depot, transdermal or implant)
- IUD placed at least 1 month prior to study enrollment
- Bilateral tubal ligation (Sterilization)
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- Vasectomized male partner
- Condom + Spermicide
- Unless engaged in sexual activity with female only sex partners or abstinent for at least 3 months prior with no intention of becoming sexually active during the study period. Any history of recent or present concomitant male sex partners will be addressed and ruled out in the context of screening participants for eligibility for the protocol
- Female only partner
- Body Mass Index (BMI) of approximately 18 to 34 kg/m^2; and a total body weight > 45 kg (99 lbs).
- Evidence of a personally signed and dated informed consent document indicating that the subject has been informed of all pertinent aspects of the trial.
- Willing and able to comply with scheduled visits, treatment plan, laboratory tests, and other trial procedures.
- Subject must have a normal pap smear within 36 months of the screening visit, no procedures for abnormal cervical/vaginal pathology in the last six months, at least one prior gynecological visit as part of subject's routine medical history.
- Subject must be willing to abstain from sexual intercourse, douching, and all intravaginal and intrarectal products at least 72 hours prior to Day 1 until study completion.
- Subject must be HIV-1 and Hepatitis B surface antigen negative as documented on screening labs.
- Subject must not be actively involved in the conception process.
- Subject must be able to swallow pills and have no allergies to any component of the study products.
Who cannot join
- Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including documented drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
- Subjects with a history of hysterectomy
- Subjects who are pregnant, possibly pregnant, or lactating
- Subjects with a presence of vaginal discharge or genital bleeding at screening
- History of febrile illness within five days prior to first dose.
- Any condition possibly affecting drug absorption (eg, gastrectomy).
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- A positive urine drug screen.
- A positive result for HIV.
- Active Hepatitis B infection as determined by positive Hepatitis B surface antigen (HbsAg) or Hepatitis B core antibody (HBcAb) tests (in the absence of HBsAb).
- Active Hepatitis C infection as defined by anti-hepatitis C virus serology (determined by multi-antigen EIA) and detectable Hepatitis C viral RNA.
- A positive test for syphilis, gonorrhea, Chlamydia, or trichomonas at screening or symptomatic bacterial vaginosis.
- Any laboratory chemistry or hematology result Grade 2 or greater according to the DAIDS Laboratory Grading Tables.
- Treatment with an investigational drug within 4 months preceding the first dose of trial medication.
- History of regular alcohol consumption exceeding 14 drinks (1 drink = 5 ounces (150 mL) of wine or 12 ounces (360 mL) of beer or 1.5 ounces (45 mL) of spirits) per week.
- Participation in a clinical trial involving vaginal or rectal biopsies within 12 months preceding the first dose of trial medication.
- Use of prescription or nonprescription drugs, vitamins, and dietary supplements within 7 days or 5 half-lives (whichever is longer) prior to the first dose of trial medication. As an exception, systemic hormonal methods of contraception can be continued.
- Blood donation of approximately 1 pint (500 mL) within 56 days prior to dosing
- History of sensitivity to heparin or heparin-induced thrombocytopenia
- Any vaccination within 30 days of study entry
- Allergy to lidocaine or Mohl's solution
- Allergy to latex
- Abnormal pap smear in the past 12 months
- Any degree of ectopy or abnormality evident during the pelvic exam at screening
- Any condition which, in the opinion of the investigator, is likely to interfere with follow-up or ability to take the study medication appropriately.
- Unwilling or unable to comply with the following dietary restriction in regard to study drug administration:
- Subjects must abstain from all food and drink (except water) at least 4 hours prior to any safety laboratory evaluations
- Subjects must abstain from all food and drink (except water) at last 8 hours prior to the start of pharmacokinetic sample collections
- Subjects will not be allowed to eat or drink grapefruit containing products from 7 days prior to the first dose of trial medication until collection of the final pharmacokinetic blood sample. While confined, the total daily nutritional composition will be approximately 50% carbohydrate, 35% fat and 15% protein, and the daily caloric intake per subject should not exceed approximately 3200 kcal.
- Subjects will be required to consume only a clear liquids diet the night before the rectal biopsy procedure and until the procedure has been completed
Trial locations and contacts
1 site in 1 country.
United States1 site
UNC Hospitals CTRC
Chapel Hill, North Carolina, 27514
About this study
Official title: A Phase I Investigation of Single-Dose Pharmacokinetics of Tenofovir, Emtricitabine, Maraviroc, and Raltegravir in Cervical, Vaginal, and Rectal Tissues and Secretions
The purpose of this study is to develop a predictive antiretroviral pharmacokinetic model of mucosal fluid and tissue distribution in genital tract fluid, rectal fluid and 3 mucosal tissues. This will be accomplished by determining the pharmacokinetic disposition and dose proportionality of four antiretrovirals (tenofovir, emtricitabine, maraviroc, and raltegravir) in human rectal and cervicovaginal fluid and rectal, cervical, and vaginal tissue.
- Conditions
- Healthy Adult Females
- Being tested
- Pharmacokinetic Sampling
- Keywords
- Healthy, Female, Volunteer
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Pharmacokinetic SamplingOther
Blood plasma, Rectal, Cervical, and Vaginal Tissues and Secretions
| Study group | Role | What they receive |
|---|---|---|
| TDF 150mg + MVC 150mg | Experimental | Subjects will receive a single dose of tenofovir 150 mg and maraviroc 150 mg. Receives: Other: Pharmacokinetic Sampling |
| TDF 300mg + MVC 300mg | Experimental | Subjects will receive a single dose of tenofovir 300 mg and maraviroc 300 mg. Receives: Other: Pharmacokinetic Sampling |
| TDF 600mg +MVC 600mg | Experimental | Subjects will receive a single dose of tenofovir 600 mg and maraviroc 600 mg. Receives: Other: Pharmacokinetic Sampling |
| FTC 100mg + RAL 200mg | Experimental | Subjects will receive a single dose of emtricitabine 100 mg and raltegravir 200 mg. Receives: Other: Pharmacokinetic Sampling |
| FTC 200mg + RAL 400mg | Experimental | Subjects will receive a single dose of emtricitabine 200 mg and raltegravir 400 mg. Receives: Other: Pharmacokinetic Sampling |
| FTC 400mg + RAL 800mg | Experimental | Subjects will receive a single dose of emtricitabine 400 mg and raltegravir 800 mg. Receives: Other: Pharmacokinetic Sampling |
What is being measured
The primary outcome is the main question the study is designed to answer.
Dose Proportionality
To determine if antiretroviral mucosal fluid and tissue concentrations change proportionally with a change in antiretroviral dose.
Measured: 48 hours
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted6 Apr 2011 (estimated)
- Study startFeb 2012
- Primary completionAug 2013
- Study completionAug 2013
Resources
- Official record on ClinicalTrials.govThe registry entry this page is built from, with its full change history.
- Publications (1)Papers the sponsor has linked to this study.
- Other trials for Healthy Adult FemalesStudies of the same condition, open and under way.
- More trials run by University of North Carolina, Chapel HillThe 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 1
- Primary purpose
- Prevention
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Enrolment
- 49 participants (actual)
Sponsor and investigators
- Lead sponsor
- University of North Carolina, Chapel Hill
- Sponsor type
- University, hospital or other
- Responsible party
- Principal investigator, Angela Kashuba, PharmD, University of North Carolina, Chapel Hill
- Investigators
- Angela DM Kashuba, PharmD, Principal investigator, University of North Carolina, Chapel Hill
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT01330199
- Sponsor's protocol ID
- 10-1393
- Status last verified
- Sep 2013
- First submitted
- 17 Aug 2010
- Last updated
- 17 Sep 2013
- Results posted
- No
- Data monitoring committee
- Yes
Publications
Tompkins LAR, Khoei A, Kapeljushnik O, Dumond J, Kashuba ADM, Tropsha A, Hubal R, Cottrell ML. HIV Pharmacology Data Repository: Setting the New Information-Sharing Standard for Clinical and Preclinical Pharmacokinetic Studies. Clin Pharmacol Ther. 2025 Dec;118(6):1340-1349. doi: 10.1002/cpt.3699. Epub 2025 May 12.
PubMed 40354181
Study at a glance
From the registry record, last updated by the sponsor on 17 Sep 2013. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase I Investigation of Single-Dose Pharmacokinetics of Tenofovir, Emtricitabine, Maraviroc, and Raltegravir in Cervical, Vaginal, and Rectal Tissues and Secretions
- ClinicalTrials.gov ID
- NCT01330199
- Acronym / sponsor ID
- 10-1393
- Conditions
- Healthy Adult Females
- Keywords
- Healthy, Female, Volunteer
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 49 participants (actual)
- Lead sponsor
- University of North Carolina, Chapel HillUniversity, hospital or other
- Study start
- Feb 2012
- Primary completion
- Aug 2013 (actual)
- Study completion
- Aug 2013 (actual)
- First posted
- 6 Apr 2011 (estimated)
- Results
- Not posted in the source record
Clinical summary
The research question as the sponsor registered it. This describes what the study plans to test, not what it found.
The purpose of this study is to develop a predictive antiretroviral pharmacokinetic model of mucosal fluid and tissue distribution in genital tract fluid, rectal fluid and 3 mucosal tissues. This will be accomplished by determining the pharmacokinetic disposition and dose proportionality of four antiretrovirals (tenofovir, emtricitabine, maraviroc, and raltegravir) in human rectal and cervicovaginal fluid and rectal, cervical, and vaginal tissue.
Study design
- Primary purpose
- Prevention
- Allocation
- Non-randomised
- Intervention model
- Parallel groups
- Masking
- None (open label)
- Number of arms
- 6
| Arm | Type | Receives |
|---|---|---|
| TDF 150mg + MVC 150mg | Experimental | Other: Pharmacokinetic SamplingSubjects will receive a single dose of tenofovir 150 mg and maraviroc 150 mg. |
| TDF 300mg + MVC 300mg | Experimental | Other: Pharmacokinetic SamplingSubjects will receive a single dose of tenofovir 300 mg and maraviroc 300 mg. |
| TDF 600mg +MVC 600mg | Experimental | Other: Pharmacokinetic SamplingSubjects will receive a single dose of tenofovir 600 mg and maraviroc 600 mg. |
| FTC 100mg + RAL 200mg | Experimental | Other: Pharmacokinetic SamplingSubjects will receive a single dose of emtricitabine 100 mg and raltegravir 200 mg. |
| FTC 200mg + RAL 400mg | Experimental | Other: Pharmacokinetic SamplingSubjects will receive a single dose of emtricitabine 200 mg and raltegravir 400 mg. |
| FTC 400mg + RAL 800mg | Experimental | Other: Pharmacokinetic SamplingSubjects will receive a single dose of emtricitabine 400 mg and raltegravir 800 mg. |
Who may qualify
- Ages
- 18 to 49 years
- Sex
- Female only
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (18 listed)
- Healthy pre-menopausal female subjects between the ages of 18 and 49 years, inclusive, with an intact gastrointestinal tract, uterus, and cervix. (Healthy is defined as no irregular menstrual cycles or clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests.)
- All subjects must have an estimated calculated creatinine clearance of at least 80 mL/min by the Cockcroft-Gault formula
- All subjects must have a negative serum pregnancy test at screening and negative urine pregnancy tests on days of sampling and should be using at least one of the following methods of contraception:
- Systemic hormonal contraceptive (oral, depot, transdermal or implant)
- IUD placed at least 1 month prior to study enrollment
Key exclusion criteria (29 listed)
- Evidence or history of clinically significant hematological, renal, endocrine, pulmonary, gastrointestinal, cardiovascular, hepatic, psychiatric, neurologic, or allergic disease (including documented drug allergies, but excluding untreated, asymptomatic, seasonal allergies at time of dosing).
- Subjects with a history of hysterectomy
- Subjects who are pregnant, possibly pregnant, or lactating
- Subjects with a presence of vaginal discharge or genital bleeding at screening
- History of febrile illness within five days prior to first dose.
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 |
|---|---|---|
| Pharmacokinetic SamplingBlood plasma, Rectal, Cervical, and Vaginal Tissues and Secretions | Other | FTC 100mg + RAL 200mg, FTC 200mg + RAL 400mg, FTC 400mg + RAL 800mg, TDF 150mg + MVC 150mg, TDF 300mg + MVC 300mg, TDF 600mg +MVC 600mg |
Primary outcome
Dose Proportionality
Time frame: 48 hours
To determine if antiretroviral mucosal fluid and tissue concentrations change proportionally with a change in antiretroviral dose.
Results and safety
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
Research links
- Official record on ClinicalTrials.govLast updated by the sponsor 17 Sep 2013.
- Derived from this study: PubMed 40354181Tompkins LAR, Khoei A, Kapeljushnik O, Dumond J, Kashuba ADM, Tropsha A, Hubal R, Cottrell ML. HIV Pharmacology Data Repository: Setting the New Information-Sharing Standard for Clinical and Preclinical Pharmacokinetic Studies. Clin Pharmacol Ther. 2025 Dec;118(6):1340-1349. doi: 10.1002/cpt.3699. Epub 2025 May 12.
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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.
Angela DM Kashuba, PharmD principal investigator
University of North Carolina, Chapel Hill
1 site in 1 country: see every site and its status.
Questions about this trial
What is this clinical trial studying?
A Phase 1 study testing Pharmacokinetic Sampling in people with Healthy Adult Females, run by University of North Carolina, Chapel Hill 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 18 inclusion and 29 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 17 Sep 2013. 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 1 studies test a treatment in a small group of people for the first time or in a new way, mainly to check safety and find the right dose.
Not every study follows the same path, and some studies (observational studies, device studies) have no phase.
Are results available for this study?
The study is completed, but results are not available in the source record. That does not mean the treatment did or did not work.
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?
Dose Proportionality (time frame: 48 hours). It is what the study was designed to measure, not a finding.
Where can I read the original study information?
On the ClinicalTrials.gov record for NCT01330199, which also lists 1 linked publication.
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 17 Sep 2013.