A Study to Investigate the Safety, Tolerability and Pharm... | NCT00928083 | Trialant
NCT00928083
Sponsor
Medicines for Malaria Venture
Status
Completed
Last Update Posted
Jan 8, 2015Estimated
Enrollment
63Actual
Phase
Phase 1
Conditions
Malaria Falciparum
Malaria Vivax
Healthy Volunteers
Interventions
OZ439 50mg API capsules
OZ439 200mg API capsules
OZ439 400mg aqueous dispersion
OZ439 800mg aqueous dispersion
OZ439 100mg API capsules
OZ439 400mg API capsules
OZ439 1600mg aqueous dispersion
OZ439 800mg API capsules
OZ439 1200mg API capsules
Placebo
OZ439 200mg aqueous dispersion
Countries
United States
Protocol Section
Identification Module
NCT ID
NCT00928083
Obsolete or Duplicate NCT IDs
Not provided
Organization Study
MMV_OZ439_09_001
Secondary IDs
Not provided
Brief Title
A Study to Investigate the Safety, Tolerability and Pharmacokinetics of OZ439 in Healthy Male and Female Subjects
Official Title
A Phase I Study To Investigate The Safety, Tolerability And Pharmacokinetic Profile Of OZ439 In Healthy Male and Female Subjects
Acronym
Not provided
Organization
Medicines for Malaria VentureOTHER
Status Module
Record Verification Date
Jan 2015
Overall Recruitment Status or Expanded Access Status
Completed
Last Known Status
Not provided
Delayed Posting
Not provided
Why Stopped
Not provided
Expanded Access Info
No
Start Date
Apr 2009
Primary Completion Date
Oct 2009Actual
Completion Date
Dec 2009Actual
First Submitted Date
Jun 24, 2009
First Submission Date that Met QC Criteria
Jun 24, 2009
First Posted Date
Jun 25, 2009Estimated
Results Waived
Not provided
Results First Submitted Date
Nov 10, 2014
Results First Submitted that Met QC Criteria
Jan 7, 2015
Results First Posted Date
Jan 8, 2015Estimated
Certification/Extension (aka Delayed Results) First Submitted Date
Not provided
Certification/Extension First Submitted that Passed QC Review
Not provided
Certification/Extension First Posted Date
Not provided
Last Update Submitted Date
Jan 7, 2015
Last Update Posted Date
Jan 8, 2015Estimated
Sponsor/Collaborators Module
Responsible Party, by Official Title
Sponsor
Lead Sponsor
Medicines for Malaria VentureOTHER
Collaborators
Not provided
Oversight Module
Has Data Monitoring Committee (DMC)
No
Is FDA Regulated Drug
Not provided
Is FDA Regulated Device
Not provided
Is Unapproved Device
Not provided
Pediatric Postmarket Surveillance of a Device Product
Not provided
Product Exported from US
Not provided
FDAAA801 Violation
Not provided
Description Module
Brief Summary
OZ439 is a synthetic trioxolane that has potential value as a peroxide antimalarial agent.
This was a Phase I, single-centre, multi-component, double-blind, randomised, placebo-controlled study in healthy male and female subjects. The study was conducted in 3 parts:
Part A investigated the safety, tolerability and pharmacokinetics (PK) of single oral escalating doses of OZ439. Up to 6 dose levels will be investigated to estimate dose proportionality.
Part B, the effect of food on a single oral dose of OZ439 was investigated in a 2-way crossover design.
Part C investigated the safety, tolerability and PK profile of multiple oral doses of OZ439.
The starting oral dose was 50 mg and the maximum single dose to be administered did not exceed 1600 mg per subject. The maximum duration of dosing proposed was 3 days.
Detailed Description
Not provided
Conditions Module
Conditions
Malaria Falciparum
Malaria Vivax
Healthy Volunteers
Keywords
Phase I
Safety and tolerability
Pharmacokinetic
synthetic peroxide
trioxolane
treatment of erythrocytic stages of malaria
Design Module
Study Type
Interventional
Number of References to an Expanded Access Study
Not provided
Expanded Access Types
Not provided
Patient Registry
Not provided
Target Follow-Up Duration
Not provided
Phases
Phase 1
Interventional Study Design
Allocation
Biospecimen
No data available
No data is available for this block.
Enrollment
63Actual
Arms/Interventions Module
Arm Groups
Label
Type
Description
Intervention Names
Part A - 50 mg Single Dose
Experimental
OZ439 Single doses of 50mg (capsules)
Drug: OZ439 50mg API capsules
Part A - 100mg Single Dose
Experimental
OZ439 Single doses of 100mg (capsules)
Drug: OZ439 100mg API capsules
Part A - 200mg Single Dose
Experimental
OZ439 Single doses of 200mg (capsules)
Drug: OZ439 200mg API capsules
Part A - 400mg Single Dose
Experimental
OZ439 Single doses of 400mg (capsules)
Drug: OZ439 400mg API capsules
Part A - 400mg Single Dose + Food
Experimental
OZ439 Single doses of 400mg (capsules) administered with food.
Drug: OZ439 400mg API capsules
Part A - 400mg AD Single Dose
Experimental
OZ439 Single doses of 400mg (aqueous dispersion)
Interventions
Name
Type
Description
Arm Group Labels
Other Names
OZ439 50mg API capsules
Drug
Part A - 50 mg Single Dose
OZ439
OZ439 200mg API capsules
Outcomes Module
Primary Outcomes
Measure
Description
Time Frame
Adverse Events
Safety/Tolerability evaluation took into account the recorded AE profile, clinical laboratory safety tests, vital signs, 12 lead and continuous (Parts A and C) ECG monitoring, audiometry/Brainstem Auditory Evoked Potentials (BAEP) parameters (Parts A and C) including any additional tests required to evaluate any safety concerns.
From screening and at 10 (+/-2) days after last dose of study medication
Secondary Outcomes
Measure
Description
Time Frame
OZ439 AUC0-t
Area under the plasma concentration-time curve from zero to time t of the last measured concentration above the limit of quantification (AUC0-t).
Samples collected from Pre-dose up to 96h post dose
OZ439 AUC0-∝
Other Outcomes
Not provided
Eligibility Module
Eligibility Criteria
Inclusion Criteria:
Healthy male//female subjects between 18- 55 years of age (inclusive).
Body mass Index (BMI) between 18 - 30 kg/m2, inclusive; and a total body weight >60 kg (132 lbs).
Healthy as determined by pre-study medical history, PE, 12 Lead ECG.
Females of childbearing potential must use 1 of birth control methods throughout study and for 30 days after last dose of study drug:
Surgically sterile (bilateral tubal ligation, hysterectomy, bilateral oophorectomy) 6 months minimum prior to first dose of study drug.
Intrauterine device (IUD) in place for at least 3 months prior to first dose of study drug.
Barrier methods (condom or diaphragm) with spermicide starting at least 14 days prior to first dose of study drug through 30 days after last dose of study drug.
Surgical sterilization of the partner(s) (vasectomy with zero sperm count for 6 months minimum prior to the first dose of study drug).
Hormonal contraceptives starting at least 3 months prior to first dose of study drug. In addition, subjects must agree to use a barrier method (condom or diaphragm) with spermicide at least 14 days prior to first dose of study drug through 30 days after the last dose of study drug.
Post-menopausal women with amenorrhea for at least 1 year will be eligible confirmed by FSH.
Male subjects must agree to use double barrier method of contraception, from time of first dose of study drug through 90 days after last dose of study drug and must also agree to not donate sperm for 90 days after last dose of study drug. Clinical laboratory tests within the reference ranges.
Able/willing to give written informed consent.
Willing/to adhere to lifestyle guideline restrictions outlined in protocol.
Willing and able to be confined to Clinical Research Unit as required by the protocol.
Exclusion Criteria:
Evidence/history of clinically significant oncologic, pulmonary, hepatic, cardiovascular, hematologic, metabolic, neurological, immunologic, nephrologic, endocrine, psychiatric disease, current infection.
Evidence/history of clinically significant gastrointestinal (some exclusions exist) disease, current infection.
Any condition that affecting drug absorption, e.g., gastrectomy.
History of post-antibiotic colitis.
Breast feeding.
QTc greater than 450 msec for males and 470 msec for females as corrected by the Bazett formula.
History of drug or alcohol abuse within the past 2 years prior to Screening.
Tobacco users
Received investigational drug/ participated in another research study within 30 days of first dose of study drug in any part of study.
Use of prescription drugs within 14 days prior to the first dose of study drug in Period 1, or need for any antibiotic during study.
Received any non prescription meds, vitamins, herbal/dietary supplements within 7 days of administration of first dose of study drug in Period 1 (exceptions exist)
Consumed alcohol within 72 hours of Day -1 in any part of study, or have a positive alcohol screen at screening or each admission to Clinical Research Unit (CRU).
Consumed grapefruit juice or juices containing grapefruit or ate grapefruit within 7 days prior to first dose of study drug in any part of study.
Positive serum pregnancy test at the Screening Visit or on Day -1 prior to inclusion in any part of the study.
Positive test for HIV-1, HBsAg,HCV.
Positive urine drug screen at Screening or admission to CRU.
History of intolerance/ hypersensitivity to artemisinins.
Likelihood of requiring treatment during study period with drugs not permitted by protocol.
Subjects who have donated blood or experienced significant blood loss within 60 days of screening for study.
Subjects whose hemoglobin is <12.5 g/dL for males/ <11.5 g/dL for females.
Any concern by investigator regarding safe participation of the subject in study or for any other reason investigator considers subject inappropriate for participation in study.
Accepts Healthy Volunteers
Yes
Sex
All
Sex/Gender Based
Not provided
Sex/Gender Description
Not provided
Minimum Age
18 Years
Maximum Age
55 Years
Standard Ages
Adult
Study Population
Not provided
Sampling Method
Not provided
Contacts/Locations Module
Central Contacts
Not provided
Overall Officials
Name
Affiliation
Role
Joerg Moehrle, PhD
Medicines for Malaria Venture
Study Director
Maria Gutierrez, MD
Comprehensive Phase One Miramar, 3400 Enterprise Way, Miramar, FL 33025
Principal Investigator
Locations
Facility
Status
City
State
ZIP
Country
Contacts
Comprehensive Phase One Miramar; 3400 Enterprise Way
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
Drug: OZ439 800mg aqueous dispersion
Part B - 800mg AD Single Dose Fast
Experimental
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
Drug: OZ439 800mg aqueous dispersion
Part C - 200mg AD Multiple Dose
Experimental
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
Drug: OZ439 200mg aqueous dispersion
Part C - 400mg AD Multiple Dose
Experimental
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
Drug: OZ439 400mg aqueous dispersion
Part C - 800mg AD Multiple Dose
Experimental
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
Drug: OZ439 800mg aqueous dispersion
Part C - Placebo
Placebo Comparator
Placebo control for Multiple rising Part C
Drug: Placebo
Drug
Part A - 200mg Single Dose
OZ439
OZ439 400mg aqueous dispersion
Drug
Part A - 400mg AD Single Dose
Part C - 400mg AD Multiple Dose
OZ439 800mg aqueous dispersion
Drug
Part A - 800mg AD Single Dose
Part B - 800mg AD Single Dose Fast
Part B - 800mg AD Single Dose Fed
Part C - 800mg AD Multiple Dose
OZ439
OZ439 100mg API capsules
Drug
OZ439 100mg (2x50mg API capsules)
Part A - 100mg Single Dose
OZ439
OZ439 400mg API capsules
Drug
OZ439 400mg (2x200mg API capsules)
Part A - 400mg Single Dose
Part A - 400mg Single Dose + Food
OZ439
OZ439 1600mg aqueous dispersion
Drug
Part A - 1600mg AD Single Dose
OZ439
OZ439 800mg API capsules
Drug
OZ439 800mg (4x200 API capsules)
Part A - 800mg Single Dose
OZ439
OZ439 1200mg API capsules
Drug
OZ439 1200mg (6x200mg API capsules)
Part A - 1200mg Single Dose
OZ439
Placebo
Drug
Part A - Placebo
Part C - Placebo
OZ439 200mg aqueous dispersion
Drug
Part C - 200mg AD Multiple Dose
OZ439
Area under the plasma concentration-time curve from zero to infinity (AUC0-∝).
Samples collected from Pre-dose up to 96h post dose
OZ439 Cmax
Maximum observed plasma drug concentration (Cmax).
Samples collected from Pre-dose up to 96h post dose
OZ439 Tmax
Time to maximum observed plasma drug concentration of OZ439
Samples collected from Pre-dose up to 96h post dose
OZ439 t1/2
Apparent terminal half-life (t1/2)
Samples collected from Pre-dose up to 96h post dose
OZ439 Rac
Accumulation index is the ratio of drug exposure observed during a dosing interval at steady-state divided by drug exposure after a single first dose, as described by the following equations:
Accumulation index (Rac) = AUC0-(Day 3)/ AUC0-(Day 1)
Samples collected from Pre-dose up to 96h post dose
FG002
Part A - OZ439 Single Dose - Cohort 3
Oral Dispersion OZ439 50-1600 mg
FG003
Part B - Food Effect - Cohort 1
Food Effect - Cohort 1 800mg OZ439 Fasted then Fed
FG004
Part B - Food Effect - Cohort 2
Food Effect - Cohort 2 800mg OZ439 Fed then Fasted
FG005
Part C - 200mg OZ439 Multiple Dose
200mg OZ439 for 3 consecutive days
FG006
Part C - 400mg OZ439 Multiple Dose
OZ439 400mg for 3 consecutive days
FG007
Part C - 800mg OZ439 Multiple Dose
OZ439 800mg for 3 consecutive days
FG008
Part C - Placebo
Part C - Placebo
FG00010 subjects
FG0018 subjects
FG0028 subjects
FG0036 subjects
FG0047 subjects
FG0056 subjects
FG0066 subjects
FG0076 subjects
FG0086 subjects
COMPLETED
FG0006 subjects
FG0018 subjects
FG0028 subjects
FG0035 subjects
FG0046 subjects
FG0056 subjects
FG0066 subjects
FG0076 subjects
FG0086 subjects
NOT COMPLETED
FG0004 subjects
FG0010 subjects
FG0020 subjects
FG0031 subjects
FG0041 subjects
FG0050 subjects
FG0060 subjects
FG0070 subjects
FG0080 subjects
Type of Units Analyzed
Not provided
Arm/Group Information
ID
Title
Description
BG000
Part A - OZ439 Single Rising Dose
Included 3 Cohorts, where subjects in cohorts 1 and 2 were randomized to a treatment sequence, receiving doses of OZ439 on four occasions and placebo on one occasion, and subjects in Cohort 3 were administered increasing doses of the oral dispersion.
BG001
Part B - OZ439 Food Effect
Subjects were randomized to sequence groups, "fasted/fed or fed/fasted" while receiving a single dose of 800 mg OZ439.
BG002
Part C - OZ439 Multiple Rising Dose
Subjects were assigned to individual dose cohorts (200, 400 and 800 mg OZ439) and placebo.
BG003
Total
Total of all reporting groups
Denominators
Units
Counts
Participants
BG00026
BG00113
BG00224
BG00363
Baseline Measures
Title
Description
Population Description
Parameter Type
Dispersion Type
Unit of Measure
Calculate Percentage
Denominator Units Selected
Denominators
Classes
Age, Continuous
Mean
Standard Deviation
years
Title
Denominators
Categories
Title
Measurements
BG00035.6± 10.35
BG00133.7± 8.49
BG00240.1± 10.17
BG003
Sex: Female, Male
Count of Participants
Participants
Title
Denominators
Categories
Title
Measurements
Female
BG0005
BG0019
BG002
Region of Enrollment
Number
participants
Title
Denominators
Categories
United States
Title
Measurements
BG00026
BG00113
BG002
Type
Title
Description
Population Description
Reporting Status
Anticipated Posting Date
Parameter Type
Dispersion Type
Unit of Measure
Calculate Percentage
Time Frame
Units Analyzed
Denominator Units Selected
Arm/Group Information
Denominators
Classes
Analyses
Primary
Adverse Events
Safety/Tolerability evaluation took into account the recorded AE profile, clinical laboratory safety tests, vital signs, 12 lead and continuous (Parts A and C) ECG monitoring, audiometry/Brainstem Auditory Evoked Potentials (BAEP) parameters (Parts A and C) including any additional tests required to evaluate any safety concerns.
Posted
Number
participants
From screening and at 10 (+/-2) days after last dose of study medication
ID
Title
Description
OG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
OG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
OG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
OG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG004
Part A - 400mg Single Dose + Food
OZ439 Single doses of 400mg (capsules) administered with food.
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG005
Part A - 400mg AD Single Dose
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
OG006
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
OG007
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
OG008
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
OG009
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
OG010
Part A - Placebo
Placebo control for Single rising Part A
Placebo
OG011
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
OG012
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
OG013
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG014
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG015
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
OG016
Part C - Placebo
Placebo control for Multiple rising Part C
Placebo
Units
Counts
Participants
OG0008
OG0018
OG0028
OG003
Title
Denominators
Categories
Title
Measurements
OG0001
OG0010
OG0022
OG003
Secondary
OZ439 AUC0-t
Area under the plasma concentration-time curve from zero to time t of the last measured concentration above the limit of quantification (AUC0-t).
Pharmacokinetics Population
Posted
Geometric Mean
Geometric Coefficient of Variation
ng.h/ml
Samples collected from Pre-dose up to 96h post dose
ID
Title
Description
OG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
OG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
OG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
OG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG004
Secondary
OZ439 AUC0-∝
Area under the plasma concentration-time curve from zero to infinity (AUC0-∝).
Pharmacokinetics Population
Posted
Geometric Mean
Geometric Coefficient of Variation
ng.h/ml
Samples collected from Pre-dose up to 96h post dose
ID
Title
Description
OG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
OG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
OG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
OG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG004
Part A - 400mg AD Single Dose
Secondary
OZ439 Cmax
Maximum observed plasma drug concentration (Cmax).
Pharmacokinetics Population
Posted
Geometric Mean
Geometric Coefficient of Variation
ng/ml
Samples collected from Pre-dose up to 96h post dose
ID
Title
Description
OG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
OG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
OG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
OG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG004
Part A - 400mg AD Single Dose
Secondary
OZ439 Tmax
Time to maximum observed plasma drug concentration of OZ439
Pharmacokinetics Population
Posted
Median
Full Range
hours
Samples collected from Pre-dose up to 96h post dose
ID
Title
Description
OG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
OG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
OG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
OG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG004
Part A - 400mg AD Single Dose
Secondary
OZ439 t1/2
Apparent terminal half-life (t1/2)
Pharmacokinetics Population
Posted
Geometric Mean
Geometric Coefficient of Variation
hours
Samples collected from Pre-dose up to 96h post dose
ID
Title
Description
OG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
OG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
OG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
OG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
OG004
Part A - 400mg AD Single Dose
Secondary
OZ439 Rac
Accumulation index is the ratio of drug exposure observed during a dosing interval at steady-state divided by drug exposure after a single first dose, as described by the following equations:
Accumulation index (Rac) = AUC0-(Day 3)/ AUC0-(Day 1)
Pharmacokinetics Population received multiple dosing only. This PK parameter is not applicable in a single dose setting.
Posted
Geometric Mean
Geometric Coefficient of Variation
ratio
Samples collected from Pre-dose up to 96h post dose
ID
Title
Description
OG000
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG001
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG002
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
Units
Time Frame
Adverse event monitoring throughout the admission period.
Description
Not provided
All-Cause Mortality Comment
Not provided
Arm/Groups
ID
Title
Description
Deaths (Affected)
Deaths (At Risk)
Serious Events (Affected)
Serious Events (At Risk)
Other Events (Affected)
Other Events (At Risk)
EG000
Part A - 50 mg Single Dose
OZ439 Single doses of 50mg (capsules)
OZ439 50mg API capsules
0
8
1
8
EG001
Part A - 100mg Single Dose
OZ439 Single doses of 100mg (capsules)
OZ439 100mg API capsules: OZ439 100mg (2x50mg API capsules)
0
8
0
8
EG002
Part A - 200mg Single Dose
OZ439 Single doses of 200mg (capsules)
OZ439 200mg API capsules
0
8
2
8
EG003
Part A - 400mg Single Dose
OZ439 Single doses of 400mg (capsules)
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
0
7
0
7
EG004
Part A - 400mg Single Dose + Food
OZ439 Single doses of 400mg (capsules) administered with food.
OZ439 400mg API capsules: OZ439 400mg (2x200mg API capsules)
0
6
0
6
EG005
Part A - 400mg AD Single Dose
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
0
5
1
5
EG006
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
0
8
2
8
EG007
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
0
6
1
6
EG008
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
0
6
1
6
EG009
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
0
6
5
6
EG010
Part A - Placebo
Placebo control for Single rising Part A
Placebo
1
17
4
17
EG011
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
0
12
3
12
EG012
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
0
12
4
12
EG013
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
0
6
3
6
EG014
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
0
6
1
6
EG015
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
0
6
4
6
EG016
Part C - Placebo
Placebo control for Multiple rising Part C
Placebo
0
6
0
6
Serious Adverse Events
Term
Organ System
Source Vocabulary
Assessment Type
Notes
Statistical Information
Influenza
Respiratory, thoracic and mediastinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG0030 events0 affected7 at risk
EG004
Other Adverse Events
Term
Organ System
Source Vocabulary
Assessment Type
Notes
Statistical Information
Atrioventricular Block
Cardiac disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG0030 events0 affected7 at risk
EG0040 events0 affected6 at risk
EG0050 events0 affected5 at risk
EG0060 events0 affected8 at risk
EG0070 events0 affected6 at risk
EG0080 events0 affected6 at risk
EG0090 events0 affected6 at risk
EG0101 events1 affected17 at risk
EG0110 events0 affected12 at risk
EG0120 events0 affected12 at risk
EG0130 events0 affected6 at risk
EG0140 events0 affected6 at risk
EG0150 events0 affected6 at risk
EG0160 events0 affected6 at risk
Abdominal Disconfort
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Constipation
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Diarrhoea
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Dyspepsia
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Gastrointestinal Hypermotility
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Nausea
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Oropharyngeal Pain
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Throat Irritation
Gastrointestinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Sinusitis
Infections and infestations
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Oral Herpes
Infections and infestations
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Urinary Tract Infection
Infections and infestations
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Blood Creatine Phosphokinase Increased
Investigations
MedDRA (10.0)
Systematic Assessment
EG0001 events1 affected8 at risk
EG0010 events0 affected8 at risk
EG0021 events1 affected8 at risk
EG003
Blood Pressure Increased
Investigations
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Arthralgia
Musculoskeletal and connective tissue disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Back Pain
Musculoskeletal and connective tissue disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Flank Pain
Musculoskeletal and connective tissue disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Myalgia
Musculoskeletal and connective tissue disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Headache
Nervous system disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0021 events1 affected8 at risk
EG003
Paraesthesia
Nervous system disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Pelvic Pain
Renal and urinary disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Nasal Congestion
Respiratory, thoracic and mediastinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Throat Irritation
Respiratory, thoracic and mediastinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Upper Respiratory Tract Infection
Respiratory, thoracic and mediastinal disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Dizziness
Vascular disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Flushing
Vascular disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Syncope Vasovagal
Vascular disorders
MedDRA (10.0)
Systematic Assessment
EG0000 events0 affected8 at risk
EG0010 events0 affected8 at risk
EG0020 events0 affected8 at risk
EG003
Certain Agreements
Are all PI(s) employees of the sponsor?
No
Restriction Type
LTE60
Results Disclosure Restriction on PI(s)?
Yes
Other Details
Not provided
Point of Contact
Title
Organization
Phone
Extension
Email
Dr. Joerg Moehrle
Medicines for Malaria Venture
+41 22 555 0330
moehrlej@mmv.org
ID
Term
D016778
Malaria, Falciparum
D016780
Malaria, Vivax
Ancestor Terms
ID
Term
D008288
Malaria
D011528
Protozoan Infections
D010272
Parasitic Diseases
D007239
Infections
D000096724
Mosquito-Borne Diseases
D000079426
Vector Borne Diseases
Browse Leaves
Not provided
Browse Branches
Not provided
ID
Term
C558165
artefenomel
Ancestor Terms
Not provided
Browse Leaves
Not provided
Browse Branches
Not provided
36.5
± 9.67
9
BG00323
Male
BG00021
BG0014
BG00215
BG00340
24
BG00363
7
OG0046
OG0055
OG0068
OG0076
OG0086
OG0096
OG01017
OG01112
OG01212
OG0136
OG0146
OG0156
OG0166
0
OG0040
OG0051
OG0062
OG0071
OG0081
OG0095
OG0104
OG0113
OG0124
OG0133
OG0141
OG0154
OG0160
Part A - 400mg AD Single Dose
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
OG005
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
OG006
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
OG007
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
OG008
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
OG009
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
OG010
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
OG011
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG012
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG013
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
Units
Counts
Participants
OG0008
OG0018
OG0028
OG0037
OG0045
OG0058
OG0066
OG0076
OG0086
OG00912
OG01012
OG0116
OG0126
OG0136
Title
Denominators
Categories
Title
Measurements
OG000102± 133.7
OG001249± 145.4
OG002890± 89.1
OG0031130± 186.6
OG0045430± 72
OG0053010± 115.7
OG0069630± 56.9
OG0076530± 172.4
OG00817500± 70.1
OG00923100± 48.9
OG0107590± 64.7
OG0113060± 60.1
OG0127990± 57.5
OG01313700± 46.0
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
OG005
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
OG006
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
OG007
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
OG008
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
OG009
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
OG010
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
OG011
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG012
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG013
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
Units
Counts
Participants
OG0008
OG0018
OG0028
OG0037
OG0045
OG0058
OG0066
OG0076
OG0086
OG00912
OG01012
OG0116
OG0126
OG0136
Title
Denominators
Categories
Title
Measurements
OG000NA± NAInsufficient data points for calculation
OG001NA± NAInsufficient data points for calculation
OG002NA± NAInsufficient data points for calculation
OG003NA± NAInsufficient data points for calculation
OG0045540± 71.3
OG0054690± 43.5
OG0069790± 56.7
OG0079130± 136.8
OG00818400± 68
OG00923900± 49
OG0108080± 68.7
OG011NA± NAInsufficient data points for calculation
OG012NA± NAInsufficient data points for calculation
OG013NA± NAInsufficient data points for calculation
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
OG005
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
OG006
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
OG007
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
OG008
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
OG009
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
OG010
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
OG011
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG012
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG013
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
Units
Counts
Participants
OG0008
OG0018
OG0028
OG0037
OG0045
OG0058
OG0066
OG0076
OG0086
OG00912
OG01012
OG0116
OG0126
OG0136
Title
Denominators
Categories
Title
Measurements
OG00017.4± 84.7
OG00134.2± 173.5
OG002102± 82.9
OG003135± 164.9
OG004566± 53.9
OG005315± 121.8
OG006917± 35.6
OG007701± 154.7
OG0081340± 44.5
OG0092220± 52.6
OG010730± 61.1
OG011342± 52.5
OG012764± 46.6
OG0131390± 51.7
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
OG005
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
OG006
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
OG007
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
OG008
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
OG009
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
OG010
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
OG011
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG012
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG013
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 800mg aqueous dispersion
Units
Counts
Participants
OG0008
OG0018
OG0028
OG0037
OG0045
OG0058
OG0066
OG0076
OG0086
OG00912
OG01012
OG0116
OG0126
OG0136
Title
Denominators
Categories
Title
Measurements
OG0003(2 to 6)
OG0015(3 to 12)
OG0023.5(3 to 6)
OG0033(2 to 6)
OG0043(2 to 4)
OG0053(2 to 4)
OG0063(3 to 6)
OG0073(2 to 6)
OG0085(2 to 6)
OG0095(2 to 7)
OG0103(2 to 5)
OG0113(2 to 5)
OG0123(2 to 5)
OG0133(2 to 5)
OZ439 Single doses of 400mg (aqueous dispersion)
OZ439 400mg aqueous dispersion
OG005
Part A - 800mg Single Dose
OZ439 Single doses of 800mg (capsules)
OZ439 800mg API capsules: OZ439 800mg (4x200 API capsules)
OG006
Part A - 800mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 800mg aqueous dispersion
OG007
Part A - 1200mg Single Dose
OZ439 Single doses of 1200mg (capsules)
OZ439 1200mg API capsules: OZ439 1200mg (6x200mg API capsules)
OG008
Part A - 1600mg AD Single Dose
OZ439 Single doses of 800mg (aqueous dispersion)
OZ439 1600mg aqueous dispersion
OG009
Part B - 800mg AD Single Dose Fed
Single dose of OZ439 800mg aqueous dispersion administered under fed conditions
OZ439 800mg aqueous dispersion
OG010
Part B - 800mg AD Single Dose Fast
Single dose of OZ439 800mg aqueous dispersion administered under fast conditions
OZ439 800mg aqueous dispersion
OG011
Part C - 200mg AD Multiple Dose
200mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 200mg aqueous dispersion
OG012
Part C - 400mg AD Multiple Dose
400mg aqueous solution OZ439 or placebo once daily for 3 days fasted
OZ439 400mg aqueous dispersion
OG013
Part C - 800mg AD Multiple Dose
800mg aqueous solution OZ439 or placebo once daily for 3 days fasted