HealthyPhase 1NCT01308658
TMC114-TiDP3-C176 - A Study in Healthy Volunteers Investigating the Bioequivalence Between Two Commercially Available 400-mg Tablets to One New 800-mg Tablet of Darunavir (DRV) in the Presence of Low-dose Ritonavir Under Fed and Fasted Conditions
A Phase 1 study testing Darunavir (DRV) and ritonavir in people with Healthy, run by Tibotec Pharmaceuticals, Ireland at 1 site in Germany.
Trial summary
In this study participants will be given 800 mg darunavir, either as one 800-mg tablet formulation (G002), or as two commercially available 400-mg tablets formulation (F030), to evaluate the effect between both, in the presence of low-dose ritonavir under fasted and fed conditions. Read more about this study
- Who is it for?
- Ages 18 to 55 yearsHealthy volunteers can take part
- Conditions the study is for
- Healthy
- What is being tested?
- Darunavir (DRV) and ritonavir
- Type of treatment
- Pill or oral medicine
- Could I receive a placebo?
- No, everyone receives an active treatment
- How many people
- 128 participants
- Where
- 1 siteGermany
- Study dates
- Jan 2011to May 2011
- 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 55 years
- All sexes
- Healthy volunteers accepted
- Adult
Who may be able to join
- Healthy based on a medical evaluation including medical history, physical examination, blood tests and electrocardiogram
- Body Mass Index of 18.0 to 30.0 kg/m² and non-smoker or smoking no more than 10 cigarettes, or 2 cigars, or 2 pipes per day for at least 3 months
- Women must be postmenopausal for at least 2 years or be surgically sterile or be not heterosexually active for the duration of the study or have a vasectomized partner
- Men must agree to use a highly effective method of birth control.
Who cannot join
- Infection with Hepatitis A, B, or C virus
- infection with HIV
- Women who are pregnant or breastfeeding
- History of, or any current medical condition which could impact the safety of the participant in the study
- Previously participated in a multiple-dose study with DRV.
Trial locations and contacts
1 site in 1 country.
About this study
Official title: A Phase I, Open-label, Randomized, 2-panel, 2-way Crossover Pivotal Bioequivalence Trial Between the Commercially Available 400-mg Tablet Formulation (F030) and the 800-mg Tablet Formulation of Darunavir (G002), in the Presence of Low-dose Ritonavir Under Fasted and Fed Conditions
In this study participants will be given 800 mg darunavir, either as one 800-mg tablet formulation (G002), or as two commercially available 400-mg tablets formulation (F030), to evaluate the effect between both, in the presence of low-dose ritonavir under fasted and fed conditions.
Read the detailed description
Darunavir (DRV, formerly known as TMC114) is an inhibitor of human immunodeficiency virus (HIV) protease. This study is designed to establish the bioequivalence of a commercially available 400-mg tablet formulation (F030) to one 800-mg tablet formulation of DRV (G002) in the presence of low-dose ritonavir under fasted and fed conditions. This is a Phase I, open-label (both participant and investigator know the name of the medication given at certain moment), randomized (study medication is assigned by chance), 2-panel, 2-way crossover study in healthy volunteers to assess the bioequivalence of DRV following administration of 2 tablet strengths (in the presence of low-dose ritonavir) under fasted and fed conditions. A total of 124 participants will participate in this study. Participants will be divided into 2 panels; 80 participants in Panel 1 (fasted) and 44 in Panel 2 (fed). In Panel 1, during 2 subsequent sessions, each participant will receive 2 treatments under fasted conditions, meaning Treatment A, a single oral 800-mg dose of DRV formulated as the 400-mg commercially available tablet F030 and Treatment B, a single oral 800-mg dose of DRV formulated as the 800-mg tablet formulation G002. In Panel 2, the same design as Panel 1 will be followed but under fed conditions, and where the 2 treatments, respectively, will be called Treatments C and D. In both panels, participants will receive ritonavir 100 mg once a day on Days 1 to 5. Ritonavir will be administered under fed conditions in both panels except for the morning intake on Day 3 in Panel 2 where it will be administered under fasting conditions. A washout period of at least 7 days between subsequent treatments will be observed. Safety (blood and urine tests, blood pressure, pulse, electrocardiogram, and physical examination) and tolerability evaluations will be recorded at regular intervals throughout the trial. Panel 1 (fasted condition) and Panel 2 (fed condition): a single dose of 800 mg DRV on Day 3 and 100 mg ritonavir once daily from Day 1 to 5. DRV will be formulated as the commercially available 400-mg tablet formulation (F030) or as the investigational 800-mg tablet formulation (G002). Ritonavir will be used as the commercially available melt-extrusion tablet containing ritonavir eq. 100 mg.
What participants receive
What participants receive. In a randomised study each person is assigned to one group by chance.
Darunavir (DRV)Drug
2x400-mg DRV tablet or 800-mg tablet
ritonavirDrug
on Day 3
| Study group | Role | What they receive |
|---|---|---|
| 001 | Experimental | Darunavir (DRV) 2x400-mg DRV tablet or 800-mg tablet on Day 3 Receives: Drug: Darunavir (DRV) |
| 002 | Experimental | ritonavir 100-mg once daily on Day 1 to Day 5 Receives: Drug: ritonavir |
What is being measured
The primary outcome is the main question the study is designed to answer.
Plasma concentrations of 100-mg ritonavir after a multiple oral dose on Days 1 to 5 in healthy volunteers in fed or fasted conditions
Measured: measured on Day 1 to Day 6
Plasma concentrations of Darunavir (DRV) after a single oral dose of 800-mg DRV on Day 3 in healthy volunteers in fed or fasted conditions
Measured: measured on Day 1
Plasma concentrations of DRV after a single oral dose of 800-mg DRV on Day 3 in healthy volunteers in fed or fasted conditions
Measured: measured on Day 3 to Day 6
Secondary outcomes (5)
Incidence of all adverse events by treatment group
Measured: Measured from Day 1 until end of trial
Blood tests
Measured: Measured from Day 1 until end of trial
Measurements of blood pressure
Measured: Measured from Day 1 until end of trial
Measurements of pulse
Measured: Measured from Day 1 until end of trial
Measurements of electrocardiograms
Measured: Measured from Day 1 until end of trial
Timeline
From the start of the study to its completion; the mark is today. Estimated dates are the sponsor’s plan.
- First posted4 Mar 2011 (estimated)
- Study startJan 2011
- Study completionMay 2011
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 HealthyStudies of the same condition, open and under way.
- 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
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Enrolment
- 128 participants (actual)
Sponsor and investigators
- Lead sponsor
- Tibotec Pharmaceuticals, Ireland
- Sponsor type
- Industry (pharma, biotech, devices)
- Responsible party
- Sponsor
- Investigators
- Tibotec Pharmaceuticals Clinical Trial, Study director, Tibotec Pharmaceutical Limited
IDs, dates and publications
- ClinicalTrials.gov ID
- NCT01308658
- Sponsor's protocol ID
- CR017776
- Other IDs
- TMC114-TiDP3-C176
- Status last verified
- Feb 2014
- First submitted
- 3 Feb 2011
- Last updated
- 6 Feb 2014
- Results posted
- No
Publications
Kakuda TN, Leopold L, Timmers M, Van De Casteele T, Hillewaert V, Tomaka FL, Hoetelmans RM. Bioavailability and bioequivalence of a darunavir 800-mg tablet formulation compared with the 400-mg tablet formulation. Int J Clin Pharmacol Ther. 2014 Sep;52(9):805-16. doi: 10.5414/cp202066.
PubMed 25109510
Study at a glance
From the registry record, last updated by the sponsor on 6 Feb 2014. Recruitment status is as the sponsor reported it: confirm with the study team.
- Official title
- A Phase I, Open-label, Randomized, 2-panel, 2-way Crossover Pivotal Bioequivalence Trial Between the Commercially Available 400-mg Tablet Formulation (F030) and the 800-mg Tablet Formulation of Darunavir (G002), in the Presence of Low-dose Ritonavir Under Fasted and Fed Conditions
- ClinicalTrials.gov ID
- NCT01308658
- Acronym / sponsor ID
- CR017776
- Conditions
- Healthy
- Keywords
- TMC114-C176, TMC114, DRV, HIV, Healthy volunteers
- Phase
- Phase 1
- Study type
- Interventional
- Recruitment status
- Completed
- Enrolment
- 128 participants (actual)
- Lead sponsor
- Tibotec Pharmaceuticals, IrelandIndustry (pharma, biotech, devices)
- Study start
- Jan 2011
- Study completion
- May 2011 (actual)
- First posted
- 4 Mar 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.
In this study participants will be given 800 mg darunavir, either as one 800-mg tablet formulation (G002), or as two commercially available 400-mg tablets formulation (F030), to evaluate the effect between both, in the presence of low-dose ritonavir under fasted and fed conditions.
Detailed description
Darunavir (DRV, formerly known as TMC114) is an inhibitor of human immunodeficiency virus (HIV) protease. This study is designed to establish the bioequivalence of a commercially available 400-mg tablet formulation (F030) to one 800-mg tablet formulation of DRV (G002) in the presence of low-dose ritonavir under fasted and fed conditions. This is a Phase I, open-label (both participant and investigator know the name of the medication given at certain moment), randomized (study medication is assigned by chance), 2-panel, 2-way crossover study in healthy volunteers to assess the bioequivalence of DRV following administration of 2 tablet strengths (in the presence of low-dose ritonavir) under fasted and fed conditions. A total of 124 participants will participate in this study. Participants will be divided into 2 panels; 80 participants in Panel 1 (fasted) and 44 in Panel 2 (fed). In Panel 1, during 2 subsequent sessions, each participant will receive 2 treatments under fasted conditions, meaning Treatment A, a single oral 800-mg dose of DRV formulated as the 400-mg commercially available tablet F030 and Treatment B, a single oral 800-mg dose of DRV formulated as the 800-mg tablet formulation G002. In Panel 2, the same design as Panel 1 will be followed but under fed conditions, and where the 2 treatments, respectively, will be called Treatments C and D. In both panels, participants will receive ritonavir 100 mg once a day on Days 1 to 5. Ritonavir will be administered under fed conditions in both panels except for the morning intake on Day 3 in Panel 2 where it will be administered under fasting conditions. A washout period of at least 7 days between subsequent treatments will be observed. Safety (blood and urine tests, blood pressure, pulse, electrocardiogram, and physical examination) and tolerability evaluations will be recorded at regular intervals throughout the trial. Panel 1 (fasted condition) and Panel 2 (fed condition): a single dose of 800 mg DRV on Day 3 and 100 mg ritonavir once daily from Day 1 to 5. DRV will be formulated as the commercially available 400-mg tablet formulation (F030) or as the investigational 800-mg tablet formulation (G002). Ritonavir will be used as the commercially available melt-extrusion tablet containing ritonavir eq. 100 mg.
Study design
- Primary purpose
- Treatment
- Allocation
- Randomised
- Intervention model
- Crossover
- Masking
- None (open label)
- Number of arms
- 2
| Arm | Type | Receives |
|---|---|---|
| 001 | Experimental | Drug: Darunavir (DRV)Darunavir (DRV) 2x400-mg DRV tablet or 800-mg tablet on Day 3 |
| 002 | Experimental | Drug: ritonavirritonavir 100-mg once daily on Day 1 to Day 5 |
Who may qualify
- Ages
- 18 to 55 years
- Sex
- All
- Healthy volunteers
- Accepted
- Age groups
- Adult
Key inclusion criteria (4 listed)
- Healthy based on a medical evaluation including medical history, physical examination, blood tests and electrocardiogram
- Body Mass Index of 18.0 to 30.0 kg/m² and non-smoker or smoking no more than 10 cigarettes, or 2 cigars, or 2 pipes per day for at least 3 months
- Women must be postmenopausal for at least 2 years or be surgically sterile or be not heterosexually active for the duration of the study or have a vasectomized partner
- Men must agree to use a highly effective method of birth control.
Key exclusion criteria (5 listed)
- Infection with Hepatitis A, B, or C virus
- infection with HIV
- Women who are pregnant or breastfeeding
- History of, or any current medical condition which could impact the safety of the participant in the study
- Previously participated in a multiple-dose study with DRV.
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 |
|---|---|---|
| Darunavir (DRV)2x400-mg DRV tablet or 800-mg tablet | Drug | 001 |
| ritonaviron Day 3 | Drug | 002 |
Primary outcome
Plasma concentrations of 100-mg ritonavir after a multiple oral dose on Days 1 to 5 in healthy volunteers in fed or fasted conditions
Time frame: measured on Day 1 to Day 6
Plasma concentrations of Darunavir (DRV) after a single oral dose of 800-mg DRV on Day 3 in healthy volunteers in fed or fasted conditions
Time frame: measured on Day 1
Plasma concentrations of DRV after a single oral dose of 800-mg DRV on Day 3 in healthy volunteers in fed or fasted conditions
Time frame: measured on Day 3 to Day 6
5 secondary outcomes
Incidence of all adverse events by treatment group
Time frame: Measured from Day 1 until end of trial
Blood tests
Time frame: Measured from Day 1 until end of trial
Measurements of blood pressure
Time frame: Measured from Day 1 until end of trial
Measurements of pulse
Time frame: Measured from Day 1 until end of trial
Measurements of electrocardiograms
Time frame: Measured from Day 1 until end of trial
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 6 Feb 2014.
- Derived from this study: PubMed 25109510Kakuda TN, Leopold L, Timmers M, Van De Casteele T, Hillewaert V, Tomaka FL, Hoetelmans RM. Bioavailability and bioequivalence of a darunavir 800-mg tablet formulation compared with the 400-mg tablet formulation. Int J Clin Pharmacol Ther. 2014 Sep;52(9):805-16. doi: 10.5414/cp202066.
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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.
Tibotec Pharmaceuticals Clinical Trial study director
Tibotec Pharmaceutical Limited
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 Darunavir (DRV) and ritonavir in people with Healthy, run by Tibotec Pharmaceuticals, Ireland at 1 site in Germany.
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 4 inclusion and 5 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 6 Feb 2014. 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 Germany. 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?
Plasma concentrations of 100-mg ritonavir after a multiple oral dose on Days 1 to 5 in healthy volunteers in fed or fasted conditions (time frame: measured on Day 1 to Day 6). The study lists 3 primary outcomes in all. 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 NCT01308658, 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 6 Feb 2014.