Study to investigate the effect of UGT1A1 inhibition by single and multiple oral doses of BI 201335 on the single and multiple oral dose pharmacokinetics of raltegravir and to investigate safety and tolerability.
Study Type
INTERVENTIONAL
Allocation
NA
Purpose
TREATMENT
Masking
NONE
Enrollment
24
Steady-state Cmax,ss (maximum measured concentration) of raltegravir and raltegravir glucuronide
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
Steady-state AUC0-12h,ss (Area under the concentration-time curve) of raltegravir and raltegravir glucuronide
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
C12h,ss of raltegravir and raltegravir glucuronide
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
Number of patients with abnormal findings in physical examination
Time frame: Baseline and within 7-14 days after last treatment
Number of patients with clinically significant changes in vital signs (blood pressure, pulse rate)
Time frame: Baseline and days 1, 5, 6, 7, 15 and within 7-14 days after last treatment
Number of patients with adverse events
Time frame: up to 7 - 14 days after last treatment
Number of patients with abnormal findings in 12-lead ECG (electrocardiogram)
Time frame: Baseline, days 1, 5, 6, 7, 15 and within 7-14 days after last treatment
Number of patients with abnormal changes in laboratory tests (hematology, clinical chemistry, urine analysis)
Time frame: Baseline, days 1, 2, 5, 6, 7, 8, 10, 12, 14, 15, 16 and within 7-14 days after last treatment
Assessment of tolerability by investigator on a 4-point scale
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Time frame: within 7-14 days after last treatment
Cmax,ss of BI 201335 ZW
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 7 and 15
C12h,ss of BI 201335 ZW
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 7 and 15
AUC0-12,ss of BI 201335 ZW
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 7 and 15
tmax,ss (Time from dosing to the maximum measured concentration) of BI 201335 ZW
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 7 and 15
CL/F0-12,ss (Total apparent clearance) of BI 201335 ZW
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 7 and 15
V/F0-12,ss (Apparent volume of distribution) of BI 201335 ZW
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 7 and 15
tmax,ss of raltegravir and raltegravir glucuronide
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
CL/F0-12,ss of raltegravir
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
V/F0-12,ss of raltegravir
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
t1/2 of raltegravir and raltegravir glucuronide
Time frame: Pre-dose and 0.5, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12 hours post-dose on day 5, 7 and 15
Ae (Amount of analyte eliminated in urine) of raltegravir and raltegravir glucuronide
Time frame: pre-dose and 0-4, 4-8, 8-12 hours post-dose on day 5, 7, 15
CLR (Renal clearance) of raltegravir and raltegravir glucuronide
Time frame: pre-dose and 0-4, 4-8, 8-12 hours post-dose on day 5, 7, 15
fe (Fraction of analyte eliminated in urine) of raltegravir and raltegravir glucuronide
Time frame: pre-dose and 0-4, 4-8, 8-12 hours post-dose on day 5, 7, 15