A Study to Assess Bioavailability & Food Effect of Different Liquid and Capsule Formulations of TMC435.

Janssen (J&J Innovative Medicine)

Status and phase: Completed; Phase 1

Conditions: Healthy Volunteers

Treatments: Drug: TMC435 150 mg oral suspension (20 mg/mL); Drug: TMC435 150 mg capsule concept K; Drug: TMC435 150 mg capsule concept L; Drug: TMC435 150 mg capsule; Drug: TMC435 150 mg oral solution (10 mg/mL)

Study type: Interventional

Funder types: Industry

Identifiers

NCT01571570

TMC435HPC1002 (Other Identifier)

CR100787

Details and patient eligibility

About

The purpose of this study is to evaluate the relative bioavailability and the short-term safety and tolerability of TMC435 following administration of 3 single oral doses of 150 mg, given as different formulations in healthy adult participants. In addition, this study is to assess for the acceptability of the taste of both liquid formulations.

Full description

TMC435 is being investigated for the treatment of chronic hepatitis C infection. The current study 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) study designed to assess the relative bioavailability and food effect of 2 liquid formulations of TMC435, currently being developed for potential pediatric use, compared to the Phase III 150 mg capsule. Also new capsule concept formulations will be investigated in comparison with the Phase III 150 mg capsule. The study will be performed in healthy adult participants and is divided over 3 panels. Participants will be randomized within a panel. Each participant will receive 3 different treatments according to a classical 6-sequence, 3-period Williams design. In Panel 1 and Panel 2, a single oral dose of 150 mg TMC435 oral suspension respectively with other strength will be compared with the capsule used in Phase III. In Panel 3, two different capsule concept formulations will be compared with the capsule used in Phase III. In panels containing the liquids, formulations will be compared under fasted and fed conditions to investigate the food effect. In all treatments, the participants will receive medication on Day 1 of each treatment. There will be a washout period of at least 7 days between subsequent treatments. The main focus of the trial is the pharmacokinetic characteristics of all formulations (level-profile of TMC435 over time in the blood stream). This evaluation requires multiple blood samples from Day 1 till Day 4 in each treatment. Safety assessments (blood and urine tests, blood pressure, pulse, electrocardiogram, and physical examination) will follow a different schedule and will be evaluated from signing of the Informed Consent Form onwards until the last trial-related visit throughout the study.

Enrollment: 72 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Healthy volunteers should be healthy on the basis of physical examination, medical history, laboratory tests, 12-lead electrocardiogram and vital signs, performed at screening, have a body Mass Index (BMI, weight in kg divided by the square of height in meters) of 18.0 to 30.0 kg/m2, extremes included and be non-smoking for at least 3 months prior to screening.
• Women must be postmenopausal for at least 2 years and/or surgically sterile or not heterosexually active for duration of the trial.

Exclusion criteria

• All participants with known allergies, hypersensitivity or intolerance to TMC435 or any of the excipients.
• Use of concomitant medication, including over the counter products, herbal medication and dietary supplements, except for paracetamol (acetaminophen) or ibuprofen.
• Any condition that, in the opinion of the investigator, would compromise the study or well-being of the participant or prevent the subject from meeting or performing study requirements.
• History or suspicion of current use of alcohol, barbiturate, amphetamine, recreational or narcotic drug use, which in investigator's opinion would compromise participant's safety and/or compliance with the trial procedures.
• Participation in an investigational drug trial with TMC435.
• Infected with HIV or Hepatitic A, B or C.

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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72 participants in 9 patient groups

Treatment A

Experimental group

Description:

Panel 1: single oral dose of 150 mg TMC435 150 mg capsule, fed

Treatment:

Drug: TMC435 150 mg capsule

Treatment B

Experimental group

Description:

Panel 1: single oral dose of 150 mg TMC435 oral suspension (20 mg/mL), fasted

Treatment:

Drug: TMC435 150 mg oral suspension (20 mg/mL)

Treatment C

Experimental group

Description:

Panel 1: single oral dose of 150 mg TMC435 oral suspension (20 mg/mL), fed

Treatment:

Drug: TMC435 150 mg oral suspension (20 mg/mL)

Treatment D

Experimental group

Description:

Panel 2: single oral dose of 150 mg TMC435 150 mg capsule, fed

Treatment:

Drug: TMC435 150 mg capsule

Treatment E

Experimental group

Description:

Panel 2: single oral dose of 150 mg TMC435 oral solution (10 mg/mL), fasted

Treatment:

Drug: TMC435 150 mg oral solution (10 mg/mL)

Treatment F

Experimental group

Description:

Panel 2: single oral dose of 150 mg TMC435 oral solution (10 mg/mL), fed

Treatment:

Drug: TMC435 150 mg oral solution (10 mg/mL)

Treatment G

Experimental group

Description:

Panel 3: single oral dose of 150 mg TMC435 150 mg capsule, fed

Treatment:

Drug: TMC435 150 mg capsule

Treatment H

Experimental group

Description:

Panel 3: single oral dose of 150 mg TMC435 capsule concept K, fed

Treatment:

Drug: TMC435 150 mg capsule concept K

Treatment I

Experimental group

Description:

Panel 3: single oral dose of 150 mg TMC435 capsule concept L, fed

Treatment:

Drug: TMC435 150 mg capsule concept L