Safety, Tolerability & Pharmacokinetics (PK) of Co-administered Single Doses of OZ439 and Mefloquine (MQ) in Healthy Volunteers
Condition: Malaria
MeSH terms: Malaria
Intervention: OZ439 100mg; OZ439 400mg; MQ 250 mg, single dose; MQ 750mg, single dose; Placebo
Intervention description: OZ439 100mg oral suspension, single dose; OZ439 400mg oral suspension, single dose; Mefloquine 250 mg tablet, single dose; Mefloquine 750mg oral tablet, single dose
Intervention MeSH terms: Artefenomel
Phase: Phase 1
Study type: Interventional
Primary purpose: Treatment
Allocation: Randomized
Intervention model: Parallel Assignment
Masking: Triple (Participant, Investigator, Outcomes Assessor)
Enrollment: 25.0
Sex: All
Minimum age: 18 Years
Maximum age: 55 Years
Healthy volunteers: Accepts Healthy Volunteers
Keywords: Malaria; PK; OZ439; Mefloquine; Healthy Volunteers

Summary:

      OZ439 is a novel, synthetic trioxolane medicine which is related to artemisinin, but has the
      advantage of a longer elimination half-life so is being developed to be administered together
      with a potential partner drug e.g. mefloquine as a single dose cure for uncomplicated
      malaria. The study findings will be used to inform the dose and design of future studies. The
      aim of the study is to establish the safety, tolerability and pharmacokinetics of
      co-administered OZ439 and MQ at a range of doses up to the maximum tolerated dose, in healthy
      volunteers.
    

Eligibility criteria:

        Inclusion Criteria:

          -  Healthy male and non-childbearing potential female volunteers of between 18 and 55
             years of age

          -  Female volunteers must have a negative serum pregnancy test at screening

          -  Females must be of non-childbearing potential

          -  Male volunteers and their partner(s) must agree to use a double barrier method of
             contraception for at least 14 days prior to first dose of study drug through 90 days
             after the last dose.

          -  Body mass Index between 18 and 30kg/m2, inclusive; and a total body weight >50 kg

          -  Laboratory tests at screening within normal ranges or not clinically significant as
             judged by the Investigator.

        Exclusion Criteria:

          -  Received an investigational drug or participated in another research study within 30
             days of the first dose of study drug or at any time through the study

          -  Evidence of current or history of clinically significant oncologic, pulmonary,
             hepatic, cardiovascular, gastrointestinal, haematologic, metabolic, neurological,
             immunologic, nephrologic, endocrine, psychiatric disease, or clinically significant
             current infection.

          -  Any condition that could possibly affect drug absorption, such as gastrectomy,
             diarrhea and lactose intolerance

          -  Use of any medications, vitamins, herbal supplements, dietary supplements or
             vaccinations within 14 days of the first dose of study drug or at any time through the
             study, unless prior approval is granted. This includes any drugs that are substrates,
             inhibitors or inducers of CYP3A4. Intermittent use of acetaminophen at doses of up to
             2g/day is permitted

          -  History of drug or alcohol abuse within 2 years of Screening

          -  History of alcohol consumption within 24 hours of any study visit

          -  Tobacco users

          -  Consumption of fruit juices within 7 days prior to dosing

          -  Participation in unaccustomed strenuous exercise within 7 days prior to

          -  Positive urine drug screen

          -  Positive test for HIV-1, HBsAg or HCV

          -  Known hypersensitivity to MQ or artemisinins

          -  QTcF greater than 450msec