A Phase I Study to investigate the safety, tolerability \& pharmacokinetics of co-administered single doses of OZ439 and Piperaquine to healthy subjects.
Placebo-controlled, double-blind, five-cohort, 2-period (per cohort) dose-escalation study. For each subject, the study included a screening evaluation (within 21 days of the 1st dose), dosing on 2 separate occasions (Period 1 and Period 2) and a follow-up visit (6 weeks following the final dose). Within each cohort, subjects were randomised into two sequences to receive OZ439 in Period 1 and OZ439 plus piperaquine in Period 2 (sequence 1, 8 subjects) or OZ439-matching placebo in Period 1 and OZ439/piperaquine matching placebos in Period 2 (sequence 2, 4 subjects). Safety and tolerability were evaluated: Physical examination, ECG assessments including a full baseline matched profile of ECG tracings, vital signs, laboratory evaluations, in particular liver function tests and adverse events.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
BASIC_SCIENCE
Masking
QUADRUPLE
Enrollment
59
Cross Research S.A.
Mendrisio, Switzerland
OZ439 Cmax
OZ439 Maximum concentration level
Time frame: Up to 168 hours post-dose
Piperaquine Cmax
Piperaquine Maximum concentration level
Time frame: Up to 1008 hours post-dose (Day 43)
OZ439 AUC(0-168)
Area under the plasma concentration versus time curve to 168 hours post-dose.
Time frame: Up to 168 hours post-dose
OZ439 t1/2
OZ439 Elimination half-life
Time frame: Up to 168 hours post-dose
Piperaquine AUC(0-168)
Piperaquine area under the plasma concentration versus time curve to 168 hours post-dose
Time frame: Up to 1008 hours post-dose (Day 43)
Piperaquine t1/2
Piperaquine Elimination half-life (t1/2).
Time frame: Up to 1008 hours post-dose (Day 43)
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160 mg Piperaquine tablet
480 mg Piperaquine tablet
1440 mg Piperaquine tablet
800mg OZ439 oral suspension single dose