Clinical Trial: An Study to Investigate the Recovery, Excretion, and Pharmacokinetics of 14C-GSK1265744 Administered as a Single Oral Dose and a Study to Describe the Pharmacokinetics of a Supratherapeutic Dose of GSK1265744 in Healthy Adult Subjects

Study Status: Completed
Recruit Status: Completed
Study Type: Interventional

Official Title: An Open Label, Non-Randomized, Mass Balance Study to Investigate the Recovery, Excretion, and Pharmacokinetics of 14C-GSK1265744 Administered as a Single Oral Dose and a Placebo-Controlled, Randomized

Brief Summary: This will be a two-part study in healthy adults. Part A is a phase 1, non-randomized, open label, single-dose, single-centre mass balance study utilizing a radiolabeled dose to investigate the recovery, excretion, and pharmacokinetics of oral GSK1265744 in a cohort of 6 healthy adult male subjects. Subjects will undergo a pre-study screening visit within 30 days of the first dose and those who successfully pass pre-study assessments and meet eligibility criteria will be enrolled into the study to receive the equivalent of a 30 mg dose of GSK1265744 as an oral solution, containing approximately 70 microcuries (mcg Ci) [0.96 millisieverts (mSv)] of radioactivity under fasted conditions. Blood, urine and fecal samples will be collected for a maximum of 504 hours (21 days) following study drug administration. In Part B, approximately 10 healthy male and female subjects will be enrolled to evaluate the single-dose safety, tolerability and PK of supratherapeutic dose of GSK1265744 150 mg compared with placebo. Each subject will receive a single dose of GSK1265744 150 mg or placebo on Day 1 under fasting conditions in the morning. Blood, urine and fecal samples will be collected for 336 hours (14 days) following dosing.

Detailed Summary:
Sponsor: ViiV Healthcare

Current Primary Outcome:

  • Part A: Percent recovery of total radioactive [14C] GSK1265744 in urine and feces. [ Time Frame: Up to 21 days ]
    Measurement of total radioactivity present in individual samples (plasma, urine, and feces) collected for a minimum of 336 hours (14 days) post dose up to a maximum of 504 hours (21 days).
  • Part A: Composite of plasma GSK1265744 PK parameters to access total radioactivity in blood [ Time Frame: Pre-dose, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 288, 312 and 336 hours post dose. ]
    The PK parameters will include: Area under the concentration-time curve from time zero (pre-dose) to last time of quantifiable concentration within a profile [AUC (0-t)], Area under the concentration-time curve from time zero (predose) extrapolated to infinite time [AUC (0-infinity)], Maximum observed concentration (Cmax), Time of occurrence of Cmax (tmax), Terminal phase elimination rate constant (lambda z), apparent terminal phase half-life (t1/2), and oral clearance (CL/F) of plasma GSK1265744 and total radioactivity in plasma and blood following single dose.
  • Part B: Number of participants with the use of concurrent medication as a measure of safety and tolerability [ Time Frame: Up to 14 days ]
  • Part B: Absolute values and changes over time of hematology as a measure of safety and tolerability. [ Time Frame: Up to 14 days ]
  • Part B: Absolute values and changes over time of clinical chemistry as a measure of safety and tolerability. [ Time Frame: Up to 14 days ]
  • Part B: Absolute values and changes over time of ur

    Original Primary Outcome: Same as current

    Current Secondary Outcome:

    • Part A: Blood: Plasma ratio of total drug-related material (radioactivity) [ Time Frame: Up to 21 days ]
      The blood: plasma ratio of total radioactivity (Cb/Cp) will be calculated at each time point by Clinical Statistics at GSK.
    • Part A: Percent of total radioactivity associated with red blood cells [ Time Frame: Up to 21 days ]
      Percent of total radioactivity associated with red blood cells will be calculated based on radioactivity concentration in plasma and blood and hematocrit count.
    • Part A: Absolute values and changes over time of hematology as a measure of safety and tolerability. [ Time Frame: Up to 21 days ]
    • Part A: Absolute values and changes over time of clinical chemistry as a measure of safety and tolerability. [ Time Frame: Up to 21 days ]
    • Part A: Absolute values and changes over time of urinalysis as a measure of safety and tolerability. [ Time Frame: Up to 21 days ]
    • Part A: Absolute values and changes over time of vital signs as a measure of safety and tolerability. [ Time Frame: Up to 21 days ]
    • Part A: Absolute values and changes over time of ECG intervals and ECG rhythm as a measure of safety and tolerability. [ Time Frame: Up to 21 days ]
    • Part A: Number of participants with adverse events as a measure of safety and tolerability [ Time Frame: Up to 21 days ]


    Original Secondary Outcome: Same as current

    Information By: ViiV Healthcare

    Dates:
    Date Received: May 2, 2013
    Date Started: May 2013
    Date Completion:
    Last Updated: October 31, 2013
    Last Verified: October 2013