TMC114-TiDP3-C176 - A Study in Healthy Volunteers Investigating the Bioequivalence Between Two Commercially Available 400-mg Tablets to One New 800-mg Tablet of Darunavir (DRV) in the Presence of Low-dose Ritonavir Under Fed and Fasted Conditions
Condition: Healthy
Study type: Interventional
Phase: Phase 1

Summary: 
      In this study participants will be given 800 mg darunavir, either as one 800-mg tablet
      formulation (G002), or as two commercially available 400-mg tablets formulation (F030), to
      evaluate the effect between both, in the presence of low-dose ritonavir under fasted and fed
      conditions.
    

Detailed description: 
      Darunavir (DRV, formerly known as TMC114) is an inhibitor of human immunodeficiency virus
      (HIV) protease. This study is designed to establish the bioequivalence of a commercially
      available 400-mg tablet formulation (F030) to one 800-mg tablet formulation of DRV (G002) in
      the presence of low-dose ritonavir under fasted and fed conditions. This 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), 2-panel, 2-way
      crossover study in healthy volunteers to assess the bioequivalence of DRV following
      administration of 2 tablet strengths (in the presence of low-dose ritonavir) under fasted and
      fed conditions. A total of 124 participants will participate in this study. Participants will
      be divided into 2 panels; 80 participants in Panel 1 (fasted) and 44 in Panel 2 (fed). In
      Panel 1, during 2 subsequent sessions, each participant will receive 2 treatments under
      fasted conditions, meaning Treatment A, a single oral 800-mg dose of DRV formulated as the
      400-mg commercially available tablet F030 and Treatment B, a single oral 800-mg dose of DRV
      formulated as the 800-mg tablet formulation G002. In Panel 2, the same design as Panel 1 will
      be followed but under fed conditions, and where the 2 treatments, respectively, will be
      called Treatments C and D. In both panels, participants will receive ritonavir 100 mg once a
      day on Days 1 to 5. Ritonavir will be administered under fed conditions in both panels except
      for the morning intake on Day 3 in Panel 2 where it will be administered under fasting
      conditions. A washout period of at least 7 days between subsequent treatments will be
      observed. Safety (blood and urine tests, blood pressure, pulse, electrocardiogram, and
      physical examination) and tolerability evaluations will be recorded at regular intervals
      throughout the trial. Panel 1 (fasted condition) and Panel 2 (fed condition): a single dose
      of 800 mg DRV on Day 3 and 100 mg ritonavir once daily from Day 1 to 5. DRV will be
      formulated as the commercially available 400-mg tablet formulation (F030) or as the
      investigational 800-mg tablet formulation (G002). Ritonavir will be used as the commercially
      available melt-extrusion tablet containing ritonavir eq. 100 mg.
    

Intervention name(s): Darunavir (DRV); ritonavir
Intervention type(s): Drug; Drug
Intervention description(s): 2x400-mg DRV tablet or 800-mg tablet; on Day 3
Intervention MeSH terms: Ritonavir; Darunavir
Allocation: Randomized
Intervention model: Crossover Assignment
Masking: None (Open Label)
Primary purpose: Treatment
Keywords: TMC114-C176; TMC114; DRV; HIV; Healthy volunteers