A Study to Determine the Relative Oral Bioavailability of Single Dose Administration of TMC207, Under Fed and Fasted Conditions in Healthy Participants

Tibotec Pharmaceutical

Status and phase: Completed; Phase 1

Conditions: Healthy

Treatments: Drug: Treatment A; Drug: Treatment C; Drug: Treatment B; Drug: Treatment D; Drug: Treatment E; Drug: Treatment F

Study type: Interventional

Funder types: Industry

Identifiers

NCT00946842

TMC207-TIDP13-C111 (Other Identifier)

CR007504

TMC207-C111 (Other Identifier)

Details and patient eligibility

About

The purpose of this study is to determine the relative oral bioavailability (the extent to which a medication or other substance becomes available to the body as compared with another form of medication or other substance) of TMC207 after single-dose oral administration of the Phase II clinical study tablet formulation, and a newly developed tablet formulations, under fed (with food) and fasted (without food) conditions.

Full description

This is a 2-panel (2 groups), open-label (all people know the identity of the intervention), randomized (the study medication is assigned by chance), 3- way crossover (method used to switch participants from one treatment arm to another in a clinical study) study. The study consists of 3 phases including, the screening phase (less than or equal to 21 days before administration of study medication), treatment phase (84 days), and the follow-up phase (up to 30 to 35 days after the last blood sample in the last treatment session is collected). Approximately 24 healthy participants will be allocated to one of two panels: Panel A (participants will receive study medication under fed condition); and Panel B (participants will receive study medication under fasted condition). Participants in Panel A will be randomly assigned to 1 of 6 treatment sequences (Treatment sequences ABC, ACB, BAC, BCA, CBA, and CAB) to receive the following 3 formulations of TMC207 with food: Treatments A: the Phase II tablet formulation; Treatment B: newly developed tablet formulation with fine particle size distribution; and Treatment C: newly developed tablet formulation with coarse particle size distribution. Participants in Panel B will be randomly assigned to 1 of 6 treatment sequences (Treatment sequences DEF, DFE, EDF, EFD, FDE, and FED) to receive the following 3 formulations of TMC207 without food: Treatments D: the Phase II tablet formulation; Treatment E: newly developed tablet formulation with fine particle size distribution; and Treatment F: newly developed tablet formulation with coarse particle size distribution. Subsequent treatments will be separated by a period of 4 weeks. The total duration of the study for each participant will be approximately 20 weeks. Safety evaluations will include assessment of adverse events, clinical laboratory tests, vital signs, electrocardiogram, physical examination, and alcohol urine medicine screen which will be monitored throughout the study.

Enrollment: 28 patients

Sex: All

Ages: 18 to 55 years old

Volunteers: Accepts Healthy Volunteers

Inclusion criteria

• Non-smoker or smokers with no more than 10 cigarettes or 2 cigars or 2 pipes per day for at least 3 months prior selection
• Normal weight as defined by a body mass index (weight in kilograms divided by the square of height in meters) of 18 to 30 kg/m2, extremes included
• Healthy on the basis of a medical evaluation that reveals the absence of any clinically relevant abnormality

Exclusion criteria

• Positive tests for Human Immunodeficiency Virus 1 (HIV type 1) or HIV 2; hepatitis A, hepatitis B, or hepatitis C infection; and urine drug tests at screening
• Female with no childbearing potential
• History or current use of alcohol, barbiturate, amphetamine, recreational or narcotic drug use
• Relevant medical history or presence of systemic disease (gastrointestinal, cardiovascular, neurologic, psychiatric, metabolic, renal, hepatic, respiratory, inflammatory, infectious disease), or significant skin disease
• History or presence of clinically significant electrocardiogram at screening
• Abnormal laboratory values at screening

Trial design

Primary purpose: Treatment

Allocation: Randomized

Interventional model: Crossover Assignment

Masking: None (Open label)

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28 participants in 12 patient groups

Panel A: Treatment Sequence ABC

Experimental group

Description:

Participants will receive the 3 treatments (Treatment A,B and C) in sequence ABC with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment B

Drug: Treatment A

Drug: Treatment C

Panel A: Treatment Sequence ACB

Experimental group

Description:

Participants will receive the 3 treatments (Treatment A,B and C) in sequence ACB with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment B

Drug: Treatment A

Drug: Treatment C

Panel A: Treatment Sequence BAC

Experimental group

Description:

Participants will receive the 3 treatments (Treatment A,B and C) in sequence BAC with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment B

Drug: Treatment A

Drug: Treatment C

Panel A: Treatment Sequence BCA

Experimental group

Description:

Participants will receive the 3 treatments (Treatment A,B and C) in sequence BCA with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment B

Drug: Treatment A

Drug: Treatment C

Panel A: Treatment Sequence CBA

Experimental group

Description:

Participants will receive the 3 treatments (Treatment A,B and C) in sequence CBA with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment B

Drug: Treatment A

Drug: Treatment C

Panel A: Treatment Sequence CAB

Experimental group

Description:

Participants will receive the 3 treatments (Treatment A,B and C) in sequence CAB with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment B

Drug: Treatment A

Drug: Treatment C

Panel B: Treatment Sequence DEF

Experimental group

Description:

Participants will receive the 3 treatments (Treatment D,E and F) in sequence DEF with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment F

Drug: Treatment E

Drug: Treatment D

Panel B: Treatment Sequence DFE

Experimental group

Description:

Participants will receive the 3 treatments (Treatment D,E and F) in sequence DFE with food and subsequent treatments will be separated by 4 weeks..

Treatment:

Drug: Treatment F

Drug: Treatment E

Drug: Treatment D

Panel B: Treatment Sequence EDF

Experimental group

Description:

Participants will receive the 3 treatments (Treatment D,E and F) in sequence EDF with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment F

Drug: Treatment E

Drug: Treatment D

Panel B: Treatment Sequence EFD

Experimental group

Description:

Participants will receive the 3 treatments (Treatment D,E and F) in sequence EFD with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment F

Drug: Treatment E

Drug: Treatment D

Panel B: Treatment Sequence FDE

Experimental group

Description:

Participants will receive the 3 treatments (Treatment D,E and F) in sequence FDE with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment F

Drug: Treatment E

Drug: Treatment D

Panel B: Treatment Sequence FED

Experimental group

Description:

Participants will receive the 3 treatments (Treatment D,E and F) in sequence FED with food and subsequent treatments will be separated by 4 weeks.

Treatment:

Drug: Treatment F

Drug: Treatment E

Drug: Treatment D