Relative Bioavailability of Three Oral Formulations Candidates of Rilpivirine for Potential Pediatric Use Compared to Oral Tablet

January 31, 2025 updated by: Janssen Sciences Ireland UC

A Phase 1, Open-label, Randomized, 2-panel, 4-way Crossover Study in Healthy Adult Subjects to Assess the Rilpivirine Relative Bioavailability Compared to the 25-mg Oral Tablet and the Food Effect Following Single Dose Administration of Oral Pediatric Formulation Candidates

The purpose of this study is to compare the rate and extent of absorption of rilpivirine in healthy adult participants following: 1) administration of a single dose of two different oral dispersible tablet formulation candidates and of an oral granules formulation with that following administration of a single dose of the 25-milligram (mg) oral tablet (EDURANT), after a standardized breakfast; 2) administration of a single dose of one selected oral formulation candidate (a dispersible tablet or granules) in different fed conditions (standardized breakfast or yoghurt) and in the fasted state and breakfast and 3) administration of a single dose of one selected oral formulation candidate (a dispersible tablet or granules) dispersed in water or in orange juice, in fed condition (standardized breakfast).

Study Overview

Status

Status

Indicates the current recruitment status or the expanded access status.
Completed

Conditions

Conditions

The disease, disorder, syndrome, illness, or injury that is being studied. On ClinicalTrials.gov, conditions may also include other health-related issues, such as lifespan, quality of life, and health risks.

Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.

Detailed Description

This is a Phase 1, open-label, randomized, 2-panel, 4-way crossover study in healthy adult participants to assess the relative bioavailability of rilpivirine following single dose administration of oral pediatric formulation candidates (two dispersible tablet formulations and one granules formulation), compared to the commercially available 25-mg tablet (EDURANT) and to assess the effect of food and different food constituents on the oral bioavailability of rilpivirine following single dose administration of one selected formulation candidate. The study will consist of 2 panels: Panel 1 and Panel 2. In each panel, participants will be randomized to receive treatment A, B, C, D and E, F, G, H, respectively. Pharmacokinetic parameters will be evaluated primarily. Safety will be monitored throughout the study.

Study Type

Study Type

Describes the nature of a clinical study. Study types include interventional studies (also called clinical trials), observational studies (including patient registries), and expanded access.
Interventional

Enrollment (Actual)

Enrollment

The number of participants in a clinical study. The "anticipated" enrollment is the target number of participants that the researchers need for the study.
32

Phase

Phase

The stage of a clinical trial studying a drug or biological product, based on definitions developed by the U.S. Food and Drug Administration (FDA). The phase is based on the study's objective, the number of participants, and other characteristics. There are five phases: Early Phase 1 (formerly listed as Phase 0), Phase 1, Phase 2, Phase 3, and Phase 4. Not Applicable is used to describe trials without FDA-defined phases, including trials of devices or behavioral interventions.
  • 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

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

Eligibility Criteria

The key requirements that people who want to participate in a clinical study must meet or the characteristics they must have. Eligibility criteria consist of both inclusion criteria (which are required for a person to participate in the study) and exclusion criteria (which prevent a person from participating). Types of eligibility criteria include whether a study accepts healthy volunteers, has age or age group requirements, or is limited by sex.

Ages Eligible for Study

18 years to 55 years (Adult)

Accepts Healthy Volunteers

Yes

Description

Inclusion Criteria:

  • Participants must be willing and able to adhere to the prohibitions and restrictions specified in the protocol and study procedures
  • Participant must be healthy on the basis of a medical evaluation that reveals the absence of any clinically significant abnormality and includes a physical examination, medical history, vital signs, electrocardiogram (ECG), and the results of blood biochemistry and hematology tests and a urinalysis performed at screening. If there are abnormalities, the participant may be included only if the Investigator judges the abnormalities or deviations from normal to be not clinically significant. This determination must be recorded in the participant's source documents and initialed by the Investigator
  • Female participant must be either postmenopausal(amenorrhea for at least 2 years and a serum follicle-stimulating hormone [FSH] level greater than or equal to (>) 40 international units per liter (IU/L) [to be confirmed at screening for all postmenopausal women]), OR permanently sterilized (eg, bilateral tubal occlusion [which includes tubal ligation procedures as consistent with local regulations], total hysterectomy, bilateral salpingectomy, bilateral oophorectomy) or otherwise incapable of becoming pregnant, and have a negative serum pregnancy test at screening
  • Male participants heterosexually active with a woman of childbearing potential must agree to use two effective contraceptive methods during the study and for at least 90 days after receiving the last dose of study drugs and male participants must agree not to donate sperm during the study and for at least 90 days after receiving the last dose of study drug
  • Participants must be non-smoking for at least 3 months prior to Screening

Exclusion Criteria:

  • Female participants who are breastfeeding at Screening
  • Participants with a history of any illness that, in the opinion of the Investigator, might confound the results of the study or pose an additional risk in administering study drug to the participants or that could prevent, limit or confound the protocol specified assessments. This may include, but is not limited to, renal dysfunction, significant cardiac, vascular, pulmonary, gastrointestinal (such as significant diarrhea, gastric stasis, or constipation that in the Investigator's opinion could influence drug absorption or bioavailability), endocrine, neurologic, hematologic, rheumatologic, psychiatric, neoplastic, or metabolic disturbances
  • Participants with current hepatitis B infection (confirmed by hepatitis B surface antigen [HBsAg]) or hepatitis C infection (confirmed by hepatitis C virus [HCV] antibody), or human immunodeficiency syndrome-1 (HIV-1 ) or HIV-2 infection
  • Participants with a history of drug or alcohol abuse according to Diagnostic and Statistical Manual of Mental Disorders (5th edition) (DSM-V) criteria within 5 years before screening or positive test result(s) for alcohol and/or drugs of abuse (including barbiturates, opiates, cocaine, amphetamines, methadone, benzodiazepines, methamphetamine, tetrahydrocannabinol, phencyclidine, and tricyclic antidepressants) at Screening
  • Participants with a history of clinically relevant skin disease such as, but not limited to, dermatitis, eczema, drug rash, psoriasis, food allergy, or urticaria

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: Treatment
  • Allocation: Randomized
  • Interventional Model: Crossover Assignment
  • Masking: None (Open Label)

Arms and Interventions

Participant Group / Arm

Participant Group / Arm

A group or subgroup of participants in a clinical trial that receives a specific intervention/treatment, or no intervention, according to the trial's protocol.
Intervention / Treatment

Intervention / Treatment

A process or action that is the focus of a clinical study. Interventions include drugs, medical devices, procedures, vaccines, and other products that are either investigational or already available. Interventions can also include noninvasive approaches, such as education or modifying diet and exercise.
Experimental: Panel 1: Group 1
Participants will receive Treatment A (25 milligram [mg] rilpivirine [RPV] formulated as the oral tablet under fed condition [standardized breakfast]) followed by Treatment D (25 mg RPV formulated as granules formulation G002 [10 g of 2.5 mg/g granules, dispersed in water] under fed [standardized breakfast]) followed by Treatment B (25 mg RPV formulated as dispersible tablet formulation G007 [10*2.5 mg tablets, dispersed in water] under fed condition) followed by Treatment C (25 mg RPV formulated as dispersible tablet formulation G009-01 [10*2.5 mg tablets, dispersed in water] under fed condition).
Drug: Rilpivirine Oral Tablet
Rilpivirine formulated as 25 mg oral tablet.
Other Names:
  • Edurant
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 1: Group 2
Participants will receive treatment B followed by treatment A then treatment C followed by treatment D.
Drug: Rilpivirine Oral Tablet
Rilpivirine formulated as 25 mg oral tablet.
Other Names:
  • Edurant
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 1: Group 3
Participants will receive treatment C followed by treatment B then treatment D followed by treatment A.
Drug: Rilpivirine Oral Tablet
Rilpivirine formulated as 25 mg oral tablet.
Other Names:
  • Edurant
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 1: Group 4
Participants will receive treatment D followed by treatment C then treatment A followed by treatment B.
Drug: Rilpivirine Oral Tablet
Rilpivirine formulated as 25 mg oral tablet.
Other Names:
  • Edurant
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 2: Group 1
Participants will receive Treatment E (25 mg RPV formulated as dispersible tablet formulation G007 or G009-01 or as granules formulation G002 [10*2.5 mg tablets or 10 g of 2.5 mg/g granules, dispersed in water] under fed [standardized breakfast] condition) followed by Treatment H (25 mg RPV formulated as dispersible tablet formulation G007 or G009-01 or as granules formulation G002 [10*2.5 mg tablets or 10 g of 2.5 mg/g granules, dispersed in water] under fed [yoghurt] condition) followed by Treatment F (25 mg RPV formulated as dispersible tablet formulation G007 or G009-01 or as granules formulation G002 [10*2.5 mg tablets or 10 g of 2.5 mg/g granules, dispersed in water] under fasted condition) followed by Treatment G (25 mg RPV formulated as dispersible tablet formulation G007 or G009-01 or as granules formulation G002 [10*2.5 mg tablets or 10 g of 2.5 mg/g granules, dispersed in water] under fed [standardized breakfast] condition).
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 2: Group 2
Participants will receive Treatment F followed by Treatment E then Treatment G followed by Treatment H.
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 2: Group 3
Participants will receive Treatment G followed by Treatment F then Treatment H followed by Treatment E.
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).
Experimental: Panel 2: Group 4
Participants will receive Treatment H followed by Treatment G then Treatment E followed by Treatment F.
Drug: Rilpivirine formulation G007
Rilpivirine G007 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G009-01
Rilpivirine G009-01 formulation as 10*2.5 mg tablets.
Drug: Rilpivirine formulation G002
Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.
Dietary supplement: Standardized Breakfast
It will consist of (or its equivalent) 4 slices of bread, 2 slices of ham and/or cheese, butter, fruit preserve and 1 or 2 cups (up to 480 milliliter [mL]) of decaffeinated coffee or decaffeinated tea with milk and/or sugar, if desired (containing approximately fat: 21 gram (gm), carbohydrates: 67 gm, proteins: 19 gm; calories 533 kilocalorie (kcal) [189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins]).

What is the study measuring?

Primary Outcome Measures

Primary Outcome Measures

In a clinical study's protocol, the planned outcome measure that is the most important for evaluating the effect of an intervention/treatment. Most clinical studies have one primary outcome measure, but some have more than one.
Outcome Measure
Measure Description
Time Frame
Maximum Observed Plasma Concentration (Cmax)
Time Frame: Up to Hour 168
The Cmax is the maximum observed plasma concentration.
Up to Hour 168
Area Under the Plasma Concentration-Time Curve From Time Zero to Last Quantifiable Time (AUC [0-last])
Time Frame: Up to Hour 168
The AUC (0-last) is the area under the plasma concentration-time curve from time zero to last quantifiable time.
Up to Hour 168
Area Under the Plasma Concentration-Time Curve From Time Zero to Infinite Time (AUC[0-infinity])
Time Frame: Up to Hour 168
The AUC (0-infinity) is the area under the plasma concentration-time curve from time zero to infinite time, calculated as the sum of AUC(last) and C(last)/lambda(z); wherein AUC(last) is area under the plasma concentration-time curve from time zero to last quantifiable time, C(last) is the last observed quantifiable concentration, and lambda(z) is elimination rate constant.
Up to Hour 168

Secondary Outcome Measures

Secondary Outcome Measures

In a clinical study's protocol, a planned outcome measure that is not as important as the primary outcome measure for evaluating the effect of an intervention but is still of interest. Most clinical studies have more than one secondary outcome measure.
Outcome Measure
Measure Description
Time Frame
Time to Reach Maximum Observed Plasma Concentration (Tmax)
Time Frame: Up to Hour 168
The Tmax is defined as time to reach maximum observed analyte concentration.
Up to Hour 168
Elimination Rate Constant (Lambda[z])
Time Frame: Up to Hour 168
Lambda(z) is first-order elimination rate constant associated with the terminal portion of the curve, determined as the negative slope of the terminal log-linear phase of the drug concentration-time curve.
Up to Hour 168
Elimination Half-Life (t1/2)
Time Frame: Up to Hour 168
The elimination half-life (t1/2) is the time measured for the plasma concentration to decrease by 1 half to its original concentration. It is associated with the terminal slope of the semi logarithmic drug concentration-time curve, and is calculated as 0.693/lambda(z).
Up to Hour 168
Number of Participants with Adverse Events
Time Frame: From signing of the informed consent form up to 30 days after last dose of study drug (Day 1)
An adverse event is any untoward medical event that occurs in a participant administered an investigational product, and it does not necessarily indicate only events with clear causal relationship with the relevant investigational product.
From signing of the informed consent form up to 30 days after last dose of study drug (Day 1)
Number of Participants with Taste Questionnaire Score
Time Frame: 15 minutes after study drug intake in each treatment period in both panels
The first part of the taste questionnaire rates sweetness, bitterness and flavour as well as overall acceptability in a 4-point scale (grading from worse to best). In the second part of the taste questionnaire the overall taste is assessed using a 5-point visual hedonic scale (categorical 5 point assessment).
15 minutes after study drug intake in each treatment period in both panels

Collaborators and Investigators

This is where you will find people and organizations involved with this study.

Sponsor

Sponsor

The organization or person who initiates the study and who has authority and control over the study.
Janssen Sciences Ireland UC

Investigators

Investigators

A researcher involved in a clinical study. Related terms include site principal investigator, site sub-investigator, study chair, study director, and study principal investigator.
  • Study Director: Janssen Sciences Ireland UC Clinical Trial, Janssen Sciences Ireland UC

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

Study Start

The actual date on which the first participant was enrolled in a clinical study. The "anticipated" study start date is the date that the researchers think will be the study start date.
October 1, 2015

Primary Completion (Actual)

Primary Completion

The date on which the last participant in a clinical study was examined or received an intervention to collect final data for the primary outcome measure. Whether the clinical study ended according to the protocol or was terminated does not affect this date. For clinical studies with more than one primary outcome measure with different completion dates, this term refers to the date on which data collection is completed for all the primary outcome measures. The "anticipated" primary completion date is the date that the researchers think will be the primary completion date for the study.
April 1, 2016

Study Completion (Actual)

Study Completion

The date on which the last participant in a clinical study was examined or received an intervention/treatment to collect final data for the primary outcome measures, secondary outcome measures, and adverse events (that is, the last participant's last visit). The "anticipated" study completion date is the date that the researchers think will be the study completion date.
April 1, 2016

Study Registration Dates

First Submitted

First Submitted

The date on which the study sponsor or investigator first submitted a study record to ClinicalTrials.gov. There is typically a delay of a few days between the first submitted date and the record's availability on ClinicalTrials.gov (the first posted date).
August 21, 2015

First Submitted That Met QC Criteria

First Submitted That Met QC Criteria

The date on which the study sponsor or investigator first submits a study record that is consistent with National Library of Medicine (NLM) quality control (QC) review criteria. The sponsor or investigator may need to revise and submit a study record one or more times before NLM's QC review criteria are met. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
September 25, 2015

First Posted (Estimated)

First Posted

The date on which the study record was first available on ClinicalTrials.gov after National Library of Medicine (NLM) quality control (QC) review has concluded. There is typically a delay of a few days between the date the study sponsor or investigator submitted the study record and the first posted date.
September 28, 2015

Study Record Updates

Last Update Posted (Actual)

Last Update Posted

The most recent date on which changes to a study record were made available on ClinicalTrials.gov. There may be a delay between when the changes were submitted to ClinicalTrials.gov by the study's sponsor or investigator (the last update submitted date) and the last update posted date.
March 25, 2025

Last Update Submitted That Met QC Criteria

Last Update Submitted That Met QC Criteria

The most recent date on which the study sponsor or investigator submitted changes to a study record that are consistent with National Library of Medicine (NLM) quality control (QC) review criteria. It is the responsibility of the sponsor or investigator to ensure that the study record is consistent with the NLM QC review criteria.
January 31, 2025

Last Verified

Last Verified

The most recent date on which the study sponsor or investigator confirmed the information about a clinical study on ClinicalTrials.gov as accurate and current. If a study with a recruitment status of recruiting; not yet recruiting; or active, not recruiting has not been confirmed within the past 2 years, the study's recruitment status is shown as unknown.
January 1, 2025

More Information

Terms related to this study

Keywords

Additional Relevant MeSH Terms

Other Study ID Numbers

Other Study ID Numbers

Identifiers or ID numbers other than the NCT number that are assigned to a clinical study by the study's sponsor, funders, or others. These numbers may include unique identifiers from other trial registries and National Institutes of Health grant numbers.
  • CR107783
  • TMC278IFD1008 (Other Identifier: Janssen Sciences Ireland UC)
  • 2015-002511-14 (EudraCT Number)

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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