Clinical trial NCT01383096
Conditions: Healthy Volunteers
Keywords: OZ439 Bioavailability Food Effect
Sponsor: Medicines for Malaria Venture
Start date: 2012-04-01; Completion date: 2012-08-01
Enrollment: 52 participants; Allocation: RANDOMIZED; Intervention model: CROSSOVER

Brief summary:
This study is designed to assess prototype formulations compared to the aqueous dispersion of Active Pharmaceutical Ingredient used in Phase I and Phase IIa studies to date. It is hoped that the bioavailability of OZ439 can be enhanced in the fasted state to be close to that observed when given after food. This will improve the utility of OZ439 in the field as well as decreasing the cost of treatment (by decreasing the dose of OZ439 required) which is very important for an antimalarial drug product destined for use in developing counties.

Detailed description:
This study was a single centre, open-label, pharmacokinetic, randomized cross-over study in healthy male volunteers and post-menopausal women. This study was conducted over three different cohorts as follows:

Cohort 1: Subjects received a single 800 mg (as free base) dose of five different treatment regimes (treatments A, B, C, D and E) on five occasions.

Cohort 2: Subjects received a single 800 mg (as free base) dose of four different treatment regimes (treatments F, G, H and I) on four occasions.

Cohort 3: Subjects received a single dose, 800mg (as free base) of prototype solution formulation 1 (treatment J) and 400mg (as free base) of prototype solution formulation 1 (treatment K) on two occasions. The treatments were administered under the fasted state.

Arms: arm 1: OZ439 800 mg (as free base) as powder in a bottle (PIB)for reconstitution in a suspension prior to administration. Administered 30 minutes after a standard fatty breakfast. arm 2: OZ439 800 mg (as free base) as a prototype solution formulation 1. Administered fasted. arm 3: OZ439 800 mg (as free base) as a prototype solution formulation 2. Administered fasted. arm 4: Best Prototype Solution - OZ439 400 mg as prototype solution formulation 1. Administered fasted. arm 5: OZ439 800 mg (as free base) as powder in a bottle (PIB) for reconstitution in a suspension prior to oral administration. Administered fasted. arm 6: OZ439 800 mg (as free base) as powder in a bottle (PIB) for reconstitution in a suspension prior to oral administration. Administered following 200 mL milk. arm 7: Best Prototype Solution - OZ439 800 mg (as free base) as prototype solution formulation 1. Administered fasted. arm 8: OZ439 800 mg (as free base) as a prototype solution formulation 1. Administered with milk. arm 9: OZ439 800 mg (as free base) as powder in a bottle (PIB) for reconstitution in a suspension prior to oral administration. Administered fasted. arm 10: OZ439 800 mg (as free base) as powder in a bottle (PIB) for reconstitution in a suspension prior to oral administration. Administered following 200 mL milk. arm 11: OZ439 800 mg (as free base) as a prototype solution formulation 2. Administered with milk.
Interventions: intervention 1: OZ439 mesylate 800mg Powder in Bottle for Oral Suspension intervention 2: OZ439 mesylate 400mg Prototype Solution Formula 1 intervention 3: OZ439 mesylate 800mg Prototype Solution Formula 1 intervention 4: OZ439 mesylate 800mg Prototype Solution Formula 2
Intervention descriptions: intervention 1: OZ439 800 mg (as free base) as powder in a bottle for reconstitution in a suspension prior to oral administration intervention 2: OZ439 400 mg (as free base) as a prototype solution formulation 1 intervention 3: OZ439 800 mg (as free base) as a prototype solution formulation 1 intervention 4: OZ439 800 mg (as free base) as a prototype solution formulation 2

Protocol documents: