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

NCT02561936 | Completed Phase 1

• 3 other identifiers: CR107783TMC278IFD10082015-002511-14
• Study Type: interventional
• Target: 32
• Locations: 1 country
• Sites: 1

Brief Summary

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).

Conditions

Healthy

Keywords

Healthy; EUDRANT; Rilpivirine

Outcome Measures

Primary Outcomes (3)

• Maximum Observed Plasma Concentration (Cmax)

  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])

  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])

  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 Outcomes (5)

• Time to Reach Maximum Observed Plasma Concentration (Tmax)

  Up to Hour 168

• Elimination Rate Constant (Lambda[z])

  Up to Hour 168

• Elimination Half-Life (t1/2)

  Up to Hour 168

• Number of Participants with Adverse Events

  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

  15 minutes after study drug intake in each treatment period in both panels

Study Arms (8)

Panel 1: Group 1

EXPERIMENTAL

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; Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 1: Group 2

EXPERIMENTAL

Participants will receive treatment B followed by treatment A then treatment C followed by treatment D.

Drug: Rilpivirine Oral Tablet; Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 1: Group 3

EXPERIMENTAL

Participants will receive treatment C followed by treatment B then treatment D followed by treatment A.

Drug: Rilpivirine Oral Tablet; Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 1: Group 4

EXPERIMENTAL

Participants will receive treatment D followed by treatment C then treatment A followed by treatment B.

Drug: Rilpivirine Oral Tablet; Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 2: Group 1

EXPERIMENTAL

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; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 2: Group 2

EXPERIMENTAL

Participants will receive Treatment F followed by Treatment E then Treatment G followed by Treatment H.

Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 2: Group 3

EXPERIMENTAL

Participants will receive Treatment G followed by Treatment F then Treatment H followed by Treatment E.

Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Panel 2: Group 4

EXPERIMENTAL

Participants will receive Treatment H followed by Treatment G then Treatment E followed by Treatment F.

Drug: Rilpivirine formulation G007; Drug: Rilpivirine formulation G009-01; Drug: Rilpivirine formulation G002; Dietary Supplement: Standardized Breakfast

Interventions

Rilpivirine Oral Tablet DRUG

Rilpivirine formulated as 25 mg oral tablet.

Also known as: Edurant

Panel 1: Group 1; Panel 1: Group 2; Panel 1: Group 3; Panel 1: Group 4

Rilpivirine formulation G007 DRUG

Rilpivirine G007 formulation as 10\*2.5 mg tablets.

Panel 1: Group 1; Panel 1: Group 2; Panel 1: Group 3; Panel 1: Group 4; Panel 2: Group 1; Panel 2: Group 2; Panel 2: Group 3; Panel 2: Group 4

Rilpivirine formulation G009-01 DRUG

Rilpivirine G009-01 formulation as 10\*2.5 mg tablets.

Panel 1: Group 1; Panel 1: Group 2; Panel 1: Group 3; Panel 1: Group 4; Panel 2: Group 1; Panel 2: Group 2; Panel 2: Group 3; Panel 2: Group 4

Rilpivirine formulation G002 DRUG

Rilpivirine G002 formulation as 10 g of 2.5 milligram per gram (mg/gm) granules.

Panel 1: Group 1; Panel 1: Group 2; Panel 1: Group 3; Panel 1: Group 4; Panel 2: Group 1; Panel 2: Group 2; Panel 2: Group 3; Panel 2: Group 4

Standardized Breakfast DIETARY_SUPPLEMENT

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) \[189 kcal from fat, 268 kcal from carbohydrates, and 76 kcal from proteins\]).

Panel 1: Group 1; Panel 1: Group 2; Panel 1: Group 3; Panel 1: Group 4; Panel 2: Group 1; Panel 2: Group 2; Panel 2: Group 3; Panel 2: Group 4

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Janssen Sciences Ireland UC: lead

Study Sites (1)

Unknown Facility

Antwerp, Belgium

Location

MeSH Terms

Interventions

Rilpivirine

Intervention Hierarchy (Ancestors)

Nitriles; Organic Chemicals; Pyrimidines; Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds

Study Officials

• Janssen Sciences Ireland UC Clinical Trial

  Janssen Sciences Ireland UC

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: August 21, 2015
• First Posted: September 28, 2015
• Study Start: October 1, 2015
• Primary Completion: April 1, 2016
• Study Completion: April 1, 2016
• Last Updated: February 3, 2025

Record last verified: 2025-01

Locations

BE (1)