An open-label, two-part study to determine the absolute bioavailability (BA) of OZ439 using simultaneous intravenous [14C] OZ439 microdose/800 mg 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 string CYP3A4 inhibitor, to healthy subjects in fasted state

An open-label, two-part study to determine the absolute bioavailability (BA) of OZ439 using simultaneous intravenous [14C] OZ439 microdose/800 mg 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 string CYP3A4 inhibitor, to healthy subjects in fasted state - Absolute BA PK of OZ439 volumes and cobicistat co-administration study

Status

Active, not recruiting

Phases

Unknown

Study type

Interventional

Source

NL-OMON

Registry ID

NL-OMON45245

Enrollment

Registered

2017-03-07

Start date

2017-02-27

Completion date

Unknown

Last updated

2024-02-28

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Malaria

Interventions

Part 1: The study will consist of 1 period during which you will receive OZ439 as an oral solution of 100 milliliters and 14C labeled OZ439 as an iv infusion of 10 milliliters and during 15 minutes.

malaria

OZ439

Eligibility

Age

18 Years to 64 Years

Inclusion criteria

Inclusion criteria: - the volunteer is willing to participate in this study - the volunteer isa healthy male or female - the female volunteers must be of non-childbearing potential (either surgically sterilized or postmenopausal) - the volunteer is between 18 and 55 years of age, inclusive - the volunteer has a BMI is between 18.0 and 30.0 kilograms/meter2 - the volunteer does not smoke or you smoke no more than 5 cigarettes per day (or comparable amount of cigars or pipe), and the volunteer is able to abstain from smoking from entry into the clinical research center and during his/herstay in the clinical research center - at the pre-study screening the volunteers state of health must satisfy the study entry requirements

Exclusion criteria

Exclusion criteria: Suffering from hepatitis B, hepatitis C, cancer or HIV/AIDS. In case of participation in another drug study within 90 days before the start of this study. Donation or loss of more than 100 mL of blood within 90 days prior to drug administration.

Design outcomes

Primary

Measure	Time frame
- 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)	—

Measure

Time frame

- 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

Measure	Time frame
- 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)	—

Measure

Time frame

- 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)

—

Countries

The Netherlands

Outcome results

None listed

Source: NL-OMON (via WHO ICTRP)