A Dose-escalation Study to Investigate Safety and Toleration of OZ439

Phase 1

Completed

Brief Summary: A randomised, placebo-controlled, dose-escalation study to investigate safety and toleration of OZ439 OD for 3 days to healthy male and female volunteers. The study aims:

* To determine the safety and tolerability of ascending doses of OZ439 OD for three days.

* To assess pharmacokinetic parameters of ascending doses of OZ439 given OD.

* To identify the maximum tolerated dose of OZ439 administered.

Detailed Description: This study will be conducted in a randomised, placebo-controlled dose-escalation design with OZ439 OD administered with full fat milk for three days to healthy male and female subjects between 18 to 55 years of age, using features of an adaptive study design. The study is expected to have three cohorts with a total of 36 healthy male and female subjects. An additional two cohorts may be used if required. The results of this study will inform the maximum tolerated exposure of OZ439 following OD dosing for three days in subjects who are not fasted.

Recruitment & Eligibility

Inclusion Criteria

Not provided

Exclusion Criteria

Not provided

Arm && Interventions

Group	Intervention	Description
OZ439 dose level 3	OZ439	Cohort 3 (12 subjects: 8 A, 4P). Subjects on active will receive X amount of OZ439 (dose level to be determined based on safety and tolerability of previous dose level) drinking solution once daily for 3 days
OZ439 Dose level 2	OZ439	• Cohort 2 (12 subjects: 8 A, 4P). Subjects on active will receive X amount of OZ439 (dose level to be determined based on safety and tolerability of previous dose level) drinking solution once daily for 3 days
OZ439 Dose level 1 (300mg)	OZ439	• Cohort 1 (12 subjects: 8 Active \[A\] and 4 on Placebo \[P\]) Active dose will consist of 300mg OZ439 drinking solution administered once daily for 3 days

Primary Outcome Measures

Name	Time	Method
OZ439 Cmax	Blood for analysis of OZ439 will be collected at the following times: pre-dose, 2, 4, 6, 8, 12, and 18 hours post-dose Day 1and Day 3, pre dose Day 2 and 4 hours post dose Day 2, and 24, 48, 72, 96 and 168 hours post 3rd dose and at follow up.	OZ439 maximum measured plasma concentration
OZ439 AUCτ	pre-dose, 2, 4, 6, 8, 12, and 18 hours post-dose Day 1and Day 3, pre dose Day 2 and 4 hours post dose Day 2, and 24, 48, 72, 96 and 168 hours post 3rd dose and at follow up.	OZ439 Area under the plasma concentration vs time curve from time zero to the time of the last quantifiable concentration t calculated using a log-linear trapezoidal method

Secondary Outcome Measures

Name	Time	Method
OZ439 Tmax	pre-dose, 2, 4, 6, 8, 12, and 18 hours post-dose Day 1and Day 3, pre dose Day 2 and 4 hours post dose Day 2, and 24, 48, 72, 96 and 168 hours post 3rd dose and at follow up.	Time to reach maximum measured OZ439 plasma concentration
OZ439 t½	pre-dose, 2, 4, 6, 8, 12, and 18 hours post-dose Day 1and Day 3, pre dose Day 2 and 4 hours post dose Day 2, and 24, 48, 72, 96 and 168 hours post 3rd dose and at follow up.	OZ439 estimated terminal phase half life