TMC278-TiDP38-C145: A Bioavailability Study in Healthy Adult Volunteers to Evaluate 3 Pediatric Formulations of TMC278 (a Solution, a Suspension, and Granules) Compared to an Adult Tablet Formulation

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details. Identifier: NCT00812292
Recruitment Status : Completed
First Posted : December 22, 2008
Last Update Posted : June 9, 2011
Information provided by:
Tibotec Pharmaceuticals, Ireland

Brief Summary:
The purpose of this study is to evaluate how much and how fast a single, oral, daily 25 mg dose of TMC278 is absorbed into the body when administered as a solution, suspension, granules, or a tablet. In addition, the effect of each formulation of TMC278 will be evaluated in patients in the fasted and fed states and the palatability (how the drug tastes) of each formulation will be assessed. Finally, the safety and tolerability of each formulation of TMC278 will be assessed throughout the study.

Condition or disease Intervention/treatment Phase
Pharmacokinetics Bioavailability HIV-1 Drug: TMC278 Phase 1

Detailed Description:
This is an open-label (both investigator and volunteer knows the name of the assigned study medication), randomized (study medication will be assigned by chance) cross-over study in healthy adults to compare the rate and the extent of absorption of TMC278 when administered as a single 25 mg dose of the 3 concept pediatric formulations (solution [10 mg/mL], suspension [5 mg/mL], granules [2.5 mg/g]), under fed and fasted conditions, to that when administered as the 25 mg TMC278 Phase III tablet formulation, under fed conditions, in healthy adults and to assess the effect of food on the bioavailability of TMC278 after a single 25 mg dose of the concept pediatric TMC278 formulations in healthy adults. The palatability of the 3 concept formulations will be assessed in a fasted state by use of a questionnaire and a visual analog scale. The short-term safety and tolerability of TMC278 following administration of 3 single oral doses of 25 mg, formulated as one of the concept pediatric formulations (under fed and fasted conditions) and as the Phase III tablet (under fed conditions), in healthy adults will be evaluated. TMC278 25 mg formulated as a solution, suspension, granules, or tablet will be administered orally (by mouth). Each volunteer will receive on the first day of one treatment session one TMC278 25 mg tablet. On the first day of the other sessions they receive a single dose of TMC278 25 mg formulated as a the solution, a suspension or granules.

Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 36 participants
Allocation: Randomized
Intervention Model: Crossover Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: A Phase I, Open-label, Randomized, Crossover Trial in Healthy Adults to Compare the Oral Bioavailability of TMC278 From Three Concept Pediatric Formulations (Solution, Suspension, Granules) With That From the Adult Phase III Tablet Formulation.
Study Start Date : January 2009
Actual Primary Completion Date : April 2009
Actual Study Completion Date : April 2009

Resource links provided by the National Library of Medicine

Drug Information available for: Rilpivirine

Primary Outcome Measures :
  1. For each treatment session, full pharmacokinetic profiles will be measured up to 168 hours post-dosing

Secondary Outcome Measures :
  1. Safety and tolerability will be monitored throughout the trial. Palatability of the 3 concept formulations will be assessed.

Information from the National Library of Medicine

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Ages Eligible for Study:   18 Years to 55 Years   (Adult)
Sexes Eligible for Study:   All
Accepts Healthy Volunteers:   Yes

Inclusion Criteria:

  • Non-smoking or smoking no more than 10 cigarettes, or 2 cigars, or 2 pipes per day for at least 3 months prior to selection
  • 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
  • Informed Consent Form signed voluntarily before the first trial-related activity
  • Able to comply with protocol requirements
  • Healthy on the basis of a medical evaluation that reveals the absence of any clinically relevant abnormality and includes a physical examination, medical history, electrocardiogram, vital signs, and the results of blood biochemistry and hematology tests and a urinalysis carried out at screening.

Exclusion Criteria:

  • A positive HIV-1 or -2 test at trial screening
  • Female, except if postmenopausal since more than two years, or post-hysterectomy or post-tubal ligation (without reversal operation)
  • One or more risk factors for QTc prolongation
  • Currently active gastrointestinal, cardiovascular, neurologic, psychiatric, metabolic, renal, hepatic, respiratory, inflammatory or infectious disease

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its identifier (NCT number): NCT00812292

Sponsors and Collaborators
Tibotec Pharmaceuticals, Ireland
Study Director: Tibotec Pharmaceuticals Clinical Trial Tibotec Pharmaceutical Limited

Additional Information: Identifier: NCT00812292     History of Changes
Other Study ID Numbers: CR012586
First Posted: December 22, 2008    Key Record Dates
Last Update Posted: June 9, 2011
Last Verified: April 2010

Keywords provided by Tibotec Pharmaceuticals, Ireland:
concept pediatric formulations of TMC278
HIV Infections

Additional relevant MeSH terms:
Reverse Transcriptase Inhibitors
Nucleic Acid Synthesis Inhibitors
Enzyme Inhibitors
Molecular Mechanisms of Pharmacological Action
Anti-Retroviral Agents
Antiviral Agents
Anti-Infective Agents
Anti-HIV Agents