A Phase I, Open-label Trial to Explore the Pharmacokinetics, Safety and Tolerability of TMC278 (Rilpivirine) 25 mg Once Daily Following a 2-week Period Receiving Efavirenz, in Healthy Male and Female Volunteers
Condition: HIV
Study type: Interventional
Phase: Phase 1

Summary: 
      The purpose of this study is to investigate the pharmacokinetics of TMC278 (rilpivirine) 25
      mg once daily following a preceding 2-week treatment period with efavirenz 600 mg once daily
      in healthy volunteers
    

Detailed description: 
      This is a Phase I, open-label (all people involved know the identity of the intervention),
      single center trial in healthy HIV negative volunteers to investigate the pharmacokinetics
      (how drugs are absorbed in the body, how they are distributed within the body, the rate at
      which a drug action begins, the duration of the effect, the chemical changes of the substance
      in the body, and the effects and routes of excretion of the metabolites) of the drug of
      rilpivirine (TMC278) 25 mg once daily (q.d.). An approximate total of 20 volunteers will be
      enrolled in this trial. All volunteers will receive 3 different treatments; o Treatment A:
      TMC278 25 mg q.d. administered for 14 days.; o Treatment B: efavirenz (EFV) 600 mg q.d.
      administered for 14 days.; o Treatment C: TMC278 25 mg q.d. administered for 28 days (4
      weeks).; All volunteers will start with Treatment A followed by Treatment B. Treatments A and
      B will be separated by a washout period of at least 14 days but no more than 21 days. At the
      end of Treatment B, volunteers will continue with Treatment C. There will be no washout
      period between Treatments B and C.; Full pharmacokinetic profiles of TMC278 will be
      determined up to 24 hours postdose on Days 1 and 14 of Treatment A (references), Day 1
      (immediately after cessation of EFV intake) of Treatment C (test), and on Days 14, 21, and 28
      (2, 3, and 4 weeks after cessation of EFV intake, respectively) of Treatment C. Trough (C0h)
      samples for determination of TMC278 plasma; concentrations will be collected regularly in
      between. Blood samples for determination of EFV plasma concentrations will be collected at
      regular time points during Treatment B and during Treatment C after cessation of EFV intake.;
      Serum samples for potential future testing of ex vivo antiviral activity will be collected
      and stored.; A pharmacogenomic blood sample for potential future CYP2B6 genotyping will be
      collected and stored from subjects who consent separately to the pharmacogenomic component of
      the trial.; Safety and tolerability will be evaluated throughout the trial. Rilpivirine
      (TMC278) 25mg once daily for 14 days, No Treatment 14-21 days, Efavirenz 600mg once daily for
      14 days, TMC278 25mg once daily for 28 days
    

Intervention name(s): TMC278; TMC278; Efavirenz
Intervention type(s): Drug; Drug; Drug
Intervention description(s): 25mg tablet once daily for 28 days; 25mg tablet once daily for 14 days; 600mg tablet once daily for 14 days
Intervention MeSH terms: Efavirenz; Rilpivirine
Intervention model: Single Group Assignment
Masking: None (Open Label)
Keywords: TMC278, rilpivirine, efavirenz, healthy volunteer