NCT04069221

Absolute BA and OZ439 PK Effect of Different OZ439 Dose Volumes and Cobicistat Co-administration Study

An Open-label, Two-part Study to Determine the Absolute Bioavailability (BA) of OZ439 Using Simultaneous Intravenous [14C]-OZ439 Microdose/800mg Oral Dosing and to Investigate the Pharmacokinetics (PK) of OZ439 Granules Administered as Single Doses Suspended in Different Volumes and When Co-administered With a Single Dose of Cobicistat, a Strong CYP3A4 Inhibitor, to Healthy Subjects in Fasted State

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 26 (actual)
• Sponsor: Medicines for Malaria Venture · Academic / Other
• Sex: All
• Age: 18 Years – 55 Years
• Healthy volunteers: Accepted

Summary

This study is an open-label, two-part study to determine the absolute bioavailability (BA) of OZ439 using simultaneous intravenous \[14C\]-OZ439 microdose/800mg oral dosing and to investigate the pharmacokinetics (PK) of OZ439 granules administered as single doses suspended in different volumes and when co-administered with a single dose of Cobicistat, a strong CYP3A4 inhibitor, to healthy subjects in fasted state.

Detailed description

Primary objectives of this study are: * to determine the absolute bioavailability of OZ439 following a single oral dose of OZ439 dispersion and a simultaneous single intravenous (iv) microdose (100 μg) infusion of \[14C\]-OZ439 under fasted conditions (Part 1) * To evaluate the effects of a single oral dose of cobicistat, a strong cytochrome P450 (CYP) 3A4 inhibitor, on the pharmacokinetic (PK) profile of a single oral dose of a dispersion of OZ439 simple granules under fasted conditions (Part 2) * To evaluate the PK of single doses of OZ439 granules when restricting the target dosing volumes to 64.5 or 100 mL (Parts 1 and 2) Secondary objectives are: * To assess the safety and tolerability of OZ439 when administered alone, and to assess the safety and tolerability of OZ439 and cobicistat when co-administered as single doses to healthy subjects (Parts 1 and 2) * To determine the PK parameters of OZ439 single iv microdose (100 μg) infusion of \[14C\]-OZ439 (Part 1) * To assess the effects of the total dosing volume and of dose to volume ratio on OZ439 PK under fasted conditions (Parts 1 and 2) * To determine the PK parameters and exposures of cobicistat (Part 2)

Conditions

• Malaria

Interventions

Type	Name	Description
DRUG	Single oral dose of 800 mg OZ439	Single oral dose of 800 mg OZ439
DRUG	Single oral dose of 400 mg OZ439	Single oral dose of 400 mg OZ439
DRUG	Single oral dose of cobicistat	Single oral dose of 150 mg cobicistat
DRUG	iv infusion of [14C]-OZ439	15-minute 10-mL iv infusion of 100 μg \[14C\]-OZ439

Timeline

• Start date: 2017-02-28
• Primary completion: 2017-05-30
• Completion: 2017-05-30
• First posted: 2019-08-28
• Last updated: 2019-11-26
• Results posted: 2019-11-26

Locations

1 site across 1 country: Netherlands