Trial Outcomes & Findings for Safety Tolerability & Pharmacokinetics of Co-administered Single Doses of OZ439 & Piperaquine to Healthy Subjects (NCT NCT01660022)

NCT ID: NCT01660022

Last Updated: 2015-01-21

Results Overview

OZ439 Maximum concentration level

• Recruitment status: COMPLETED
• Study phase: PHASE1
• Target enrollment: 59 participants
• Primary outcome timeframe: Up to 168 hours post-dose
• Results posted on: 2015-01-21

Participant Flow

Date of first enrolment: 11SEP2012 Date last volunteer completed: 07MAY2013 Phase 1 Clinical Research Unit

Participant milestones

Measure	Cohort 1 Sequence 1: OZ439 100mg Sequence 2: OZ439 100mg / PQP 160mg	Cohort 2 Sequence 1: OZ439 100mg Sequence 2: OZ439 100mg+PQP 480mg	Cohort 3 Sequence 1: OZ439 100mg Sequence 2: OZ439 100mg+PQP 1440mg	Cohort 4 Sequence 1: OZ439 300mg Sequence 2: OZ439 300mg+PQP 1440mg	Cohort 5 Sequence 1: OZ439 800mg Sequence 2: OZ439 800mg+PQP 1440mg	Placebo Cohorts 1, 2, 3, 4 and 5
First Sequence (7 Days) STARTED	8	8	8	8	7	20
First Sequence (7 Days) COMPLETED	8	7	8	7	6	16
First Sequence (7 Days) NOT COMPLETED	0	1	0	1	1	4
Second Sequence (42 Days) STARTED	8	7	8	7	6	16
Second Sequence (42 Days) COMPLETED	8	7	8	7	6	16
Second Sequence (42 Days) NOT COMPLETED	0	0	0	0	0	0

Reasons for withdrawal

Measure	Cohort 1 Sequence 1: OZ439 100mg Sequence 2: OZ439 100mg / PQP 160mg	Cohort 2 Sequence 1: OZ439 100mg Sequence 2: OZ439 100mg+PQP 480mg	Cohort 3 Sequence 1: OZ439 100mg Sequence 2: OZ439 100mg+PQP 1440mg	Cohort 4 Sequence 1: OZ439 300mg Sequence 2: OZ439 300mg+PQP 1440mg	Cohort 5 Sequence 1: OZ439 800mg Sequence 2: OZ439 800mg+PQP 1440mg	Placebo Cohorts 1, 2, 3, 4 and 5
First Sequence (7 Days) Withdrawal by Subject	0	1	0	1	0	0
First Sequence (7 Days) Adverse Event	0	0	0	0	1	3
First Sequence (7 Days) Protocol Violation	0	0	0	0	0	1

Baseline Characteristics

Safety Tolerability & Pharmacokinetics of Co-administered Single Doses of OZ439 & Piperaquine to Healthy Subjects

Baseline characteristics by cohort

Measure	Cohort 1 n=8 Participants Sequence 1: OZ439 100mg Sequence 2: OZ439 100 mg / PQP 160 mg	Cohort 2 n=7 Participants Sequence 1: OZ439 100mg Sequence 2: OZ439 100 mg / PQP 480 mg	Cohort 3 n=8 Participants Sequence 1: OZ439 100mg Sequence 2: OZ439 100 mg / PQP 1440 mg	Cohort 4 n=7 Participants Sequence 1: OZ439 300mg Sequence 2: OZ439 300 mg / PQP 1440 mg	Cohort 5 n=6 Participants Sequence 1: OZ439 800mg Sequence 2: OZ439 800 mg / PQP 1440 mg	Placebo n=20 Participants Cohorts 1, 2, 3, 4 and 5	Total n=56 Participants Total of all reporting groups
Age, Continuous	36.0 years STANDARD_DEVIATION 9.4 • n=5 Participants	41.7 years STANDARD_DEVIATION 7.1 • n=7 Participants	35.4 years STANDARD_DEVIATION 10 • n=5 Participants	32.1 years STANDARD_DEVIATION 8.4 • n=4 Participants	35.7 years STANDARD_DEVIATION 11.7 • n=21 Participants	37.3 years STANDARD_DEVIATION 10.3 • n=10 Participants	36.43 years STANDARD_DEVIATION 8.7 • n=115 Participants
Sex: Female, Male Female	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants	1 Participants n=10 Participants	1 Participants n=115 Participants
Sex: Female, Male Male	8 Participants n=5 Participants	7 Participants n=7 Participants	8 Participants n=5 Participants	7 Participants n=4 Participants	6 Participants n=21 Participants	19 Participants n=10 Participants	55 Participants n=115 Participants
Region of Enrollment Switzerland	8 participants n=5 Participants	7 participants n=7 Participants	8 participants n=5 Participants	7 participants n=4 Participants	6 participants n=21 Participants	20 participants n=10 Participants	56 participants n=115 Participants

PRIMARY outcome

Timeframe: Up to 168 hours post-dose

Population: All randomised subjects who fulfilled the study protocol requirements in terms of study drug intake and PK samplings, with no major deviations that could affect the PK results.

OZ439 Maximum concentration level

Outcome measures

Measure	Cohort 1 - OZ439 100mg n=8 Participants Cohort 1 - Sequence 1 OZ439 100mg	Cohort 1 - OZ439 100mg / PQP 160mg n=8 Participants Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	Cohort 2 - OZ439 100mg n=7 Participants Cohort 2 - Sequence 1 OZ439 100mg	Cohort 2 - OZ439 100mg / PQP 480mg n=7 Participants Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	Cohort 3 - OZ439 100mg n=8 Participants Cohort 3 - Sequence 1 OZ439 100mg	Cohort 3 - OZ439 100mg / PQP 1440mg n=8 Participants Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	Cohort 4 - OZ439 300mg n=7 Participants Cohort 4 - Sequence 1 OZ439 300mg	Cohort 4 - OZ439 300mg / PQP 1440mg n=7 Participants Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	Cohort 5 - OZ439 800mg n=5 Participants Cohort 5 - Sequence 1 OZ439 800mg	Cohort 5 - OZ439 800mg / PQP 1440mg n=5 Participants Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg
OZ439 Cmax	142 ng/mL Geometric Coefficient of Variation 39.2	139 ng/mL Geometric Coefficient of Variation 33.1	146 ng/mL Geometric Coefficient of Variation 43.2	198 ng/mL Geometric Coefficient of Variation 47.4	127 ng/mL Geometric Coefficient of Variation 22.9	199 ng/mL Geometric Coefficient of Variation 26.8	590 ng/mL Geometric Coefficient of Variation 31.5	778 ng/mL Geometric Coefficient of Variation 31.5	1500 ng/mL Geometric Coefficient of Variation 42.2	1650 ng/mL Geometric Coefficient of Variation 25.6

PRIMARY outcome

Timeframe: Up to 1008 hours post-dose (Day 43)

Population: All randomised subjects who fulfilled the study protocol requirements in terms of study drug intake and PK samplings, with no major deviations that could affect the PK results.

Piperaquine Maximum concentration level

Outcome measures

Measure	Cohort 1 - OZ439 100mg n=8 Participants Cohort 1 - Sequence 1 OZ439 100mg	Cohort 1 - OZ439 100mg / PQP 160mg n=7 Participants Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	Cohort 2 - OZ439 100mg n=8 Participants Cohort 2 - Sequence 1 OZ439 100mg	Cohort 2 - OZ439 100mg / PQP 480mg n=7 Participants Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	Cohort 3 - OZ439 100mg n=5 Participants Cohort 3 - Sequence 1 OZ439 100mg	Cohort 3 - OZ439 100mg / PQP 1440mg Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	Cohort 4 - OZ439 300mg Cohort 4 - Sequence 1 OZ439 300mg	Cohort 4 - OZ439 300mg / PQP 1440mg Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	Cohort 5 - OZ439 800mg Cohort 5 - Sequence 1 OZ439 800mg	Cohort 5 - OZ439 800mg / PQP 1440mg Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg
Piperaquine Cmax	8.59 ng/mL Geometric Coefficient of Variation 34.7	46.6 ng/mL Geometric Coefficient of Variation 44.3	393 ng/mL Geometric Coefficient of Variation 43.8	271 ng/mL Geometric Coefficient of Variation 30.9	356 ng/mL Geometric Coefficient of Variation 53.6	—	—	—	—	—

PRIMARY outcome

Timeframe: Up to 168 hours post-dose

Population: All randomised subjects who fulfilled the study protocol requirements in terms of study drug intake and PK samplings, with no major deviations that could affect the PK results.

Area under the plasma concentration versus time curve to 168 hours post-dose.

Outcome measures

Measure	Cohort 1 - OZ439 100mg n=8 Participants Cohort 1 - Sequence 1 OZ439 100mg	Cohort 1 - OZ439 100mg / PQP 160mg n=8 Participants Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	Cohort 2 - OZ439 100mg n=7 Participants Cohort 2 - Sequence 1 OZ439 100mg	Cohort 2 - OZ439 100mg / PQP 480mg n=7 Participants Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	Cohort 3 - OZ439 100mg n=8 Participants Cohort 3 - Sequence 1 OZ439 100mg	Cohort 3 - OZ439 100mg / PQP 1440mg n=8 Participants Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	Cohort 4 - OZ439 300mg n=7 Participants Cohort 4 - Sequence 1 OZ439 300mg	Cohort 4 - OZ439 300mg / PQP 1440mg n=7 Participants Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	Cohort 5 - OZ439 800mg n=5 Participants Cohort 5 - Sequence 1 OZ439 800mg	Cohort 5 - OZ439 800mg / PQP 1440mg n=5 Participants Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg
OZ439 AUC(0-168)	862 ng.h/mL Geometric Coefficient of Variation 33.9	920 ng.h/mL Geometric Coefficient of Variation 26.6	1130 ng.h/mL Geometric Coefficient of Variation 41.7	1390 ng.h/mL Geometric Coefficient of Variation 47.0	909 ng.h/mL Geometric Coefficient of Variation 21.4	1520 ng.h/mL Geometric Coefficient of Variation 26.1	5740 ng.h/mL Geometric Coefficient of Variation 29.9	7410 ng.h/mL Geometric Coefficient of Variation 30.3	15300 ng.h/mL Geometric Coefficient of Variation 47.6	18600 ng.h/mL Geometric Coefficient of Variation 36.8

PRIMARY outcome

Timeframe: Up to 168 hours post-dose

Population: All randomised subjects who fulfilled the study protocol requirements in terms of study drug intake and PK samplings, with no major deviations that could affect the PK results.

OZ439 Elimination half-life

Outcome measures

Measure	Cohort 1 - OZ439 100mg n=8 Participants Cohort 1 - Sequence 1 OZ439 100mg	Cohort 1 - OZ439 100mg / PQP 160mg n=8 Participants Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	Cohort 2 - OZ439 100mg n=7 Participants Cohort 2 - Sequence 1 OZ439 100mg	Cohort 2 - OZ439 100mg / PQP 480mg n=7 Participants Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	Cohort 3 - OZ439 100mg n=8 Participants Cohort 3 - Sequence 1 OZ439 100mg	Cohort 3 - OZ439 100mg / PQP 1440mg n=8 Participants Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	Cohort 4 - OZ439 300mg n=7 Participants Cohort 4 - Sequence 1 OZ439 300mg	Cohort 4 - OZ439 300mg / PQP 1440mg n=7 Participants Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	Cohort 5 - OZ439 800mg n=5 Participants Cohort 5 - Sequence 1 OZ439 800mg	Cohort 5 - OZ439 800mg / PQP 1440mg n=5 Participants Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg
OZ439 t1/2	NA hour Geometric Coefficient of Variation NA Insufficient data points for calculation	NA hour Geometric Coefficient of Variation NA Insufficient data points for calculation	NA hour Geometric Coefficient of Variation NA Insufficient data points for calculation	NA hour Geometric Coefficient of Variation NA Insufficient data points for calculation	NA hour Geometric Coefficient of Variation NA Insufficient data points for calculation	NA hour Geometric Coefficient of Variation NA Insufficient data points for calculation	90.6 hour Geometric Coefficient of Variation 19.4	112 hour Geometric Coefficient of Variation 45.2	65.4 hour Geometric Coefficient of Variation 23.2	135 hour Geometric Coefficient of Variation 53.2

PRIMARY outcome

Timeframe: Up to 1008 hours post-dose (Day 43)

Population: All randomised subjects who fulfilled the study protocol requirements in terms of study drug intake and PK samplings, with no major deviations that could affect the PK results.

Piperaquine area under the plasma concentration versus time curve to 168 hours post-dose

Outcome measures

Measure	Cohort 1 - OZ439 100mg n=8 Participants Cohort 1 - Sequence 1 OZ439 100mg	Cohort 1 - OZ439 100mg / PQP 160mg n=7 Participants Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	Cohort 2 - OZ439 100mg n=8 Participants Cohort 2 - Sequence 1 OZ439 100mg	Cohort 2 - OZ439 100mg / PQP 480mg n=7 Participants Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	Cohort 3 - OZ439 100mg n=5 Participants Cohort 3 - Sequence 1 OZ439 100mg	Cohort 3 - OZ439 100mg / PQP 1440mg Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	Cohort 4 - OZ439 300mg Cohort 4 - Sequence 1 OZ439 300mg	Cohort 4 - OZ439 300mg / PQP 1440mg Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	Cohort 5 - OZ439 800mg Cohort 5 - Sequence 1 OZ439 800mg	Cohort 5 - OZ439 800mg / PQP 1440mg Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg
Piperaquine AUC(0-168)	1340 ng.h/mL Geometric Coefficient of Variation NA Not Calculated. Insufficient data points for calculation.	3420 ng.h/mL Geometric Coefficient of Variation 22.8	17500 ng.h/mL Geometric Coefficient of Variation 25.7	17200 ng.h/mL Geometric Coefficient of Variation 12.8	13200 ng.h/mL Geometric Coefficient of Variation 53.8	—	—	—	—	—

PRIMARY outcome

Timeframe: Up to 1008 hours post-dose (Day 43)

Population: All randomised subjects who fulfilled the study protocol requirements in terms of study drug intake and PK samplings, with no major deviations that could affect the PK results.

Piperaquine Elimination half-life (t1/2).

Outcome measures

Measure	Cohort 1 - OZ439 100mg n=8 Participants Cohort 1 - Sequence 1 OZ439 100mg	Cohort 1 - OZ439 100mg / PQP 160mg n=7 Participants Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	Cohort 2 - OZ439 100mg n=8 Participants Cohort 2 - Sequence 1 OZ439 100mg	Cohort 2 - OZ439 100mg / PQP 480mg n=7 Participants Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	Cohort 3 - OZ439 100mg n=5 Participants Cohort 3 - Sequence 1 OZ439 100mg	Cohort 3 - OZ439 100mg / PQP 1440mg Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	Cohort 4 - OZ439 300mg Cohort 4 - Sequence 1 OZ439 300mg	Cohort 4 - OZ439 300mg / PQP 1440mg Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	Cohort 5 - OZ439 800mg Cohort 5 - Sequence 1 OZ439 800mg	Cohort 5 - OZ439 800mg / PQP 1440mg Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg
Piperaquine t1/2	294 hour Geometric Coefficient of Variation NA Not Calculated. Insufficient data points for calculation.	283 hour Geometric Coefficient of Variation 64.4	515 hour Geometric Coefficient of Variation 36.3	632 hour Geometric Coefficient of Variation 26.5	509 hour Geometric Coefficient of Variation 15.9	—	—	—	—	—

Adverse Events

OZ439 100mg

Serious events: 0 serious events

Other events: 3 other events

Deaths: 0 deaths

OZ439 300mg

Serious events: 0 serious events

Other events: 3 other events

Deaths: 0 deaths

OZ439 800mg

Serious events: 0 serious events

Other events: 2 other events

Deaths: 0 deaths

OZ439 100mg / PQP 160mg

Serious events: 0 serious events

Other events: 2 other events

Deaths: 0 deaths

OZ439 100mg / PQP 480mg

Serious events: 0 serious events

Other events: 0 other events

Deaths: 0 deaths

OZ439 100mg / PQP 1440mg

Serious events: 0 serious events

Other events: 1 other events

Deaths: 0 deaths

OZ439 300mg / PQP 1440mg

Serious events: 0 serious events

Other events: 3 other events

Deaths: 0 deaths

OZ439 800mg / PQP 1440mg

Serious events: 0 serious events

Other events: 1 other events

Deaths: 0 deaths

Placebo

Serious events: 1 serious events

Other events: 8 other events

Deaths: 0 deaths

Serious adverse events

Measure	OZ439 100mg n=24 participants at risk Cohorts 1, 2 and 3 OZ439 100mg	OZ439 300mg n=8 participants at risk Cohort 4 - Sequence 1 OZ439 300mg	OZ439 800mg n=7 participants at risk Cohort 5 - Sequence 1 OZ439 800mg	OZ439 100mg / PQP 160mg n=8 participants at risk Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	OZ439 100mg / PQP 480mg n=7 participants at risk Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	OZ439 100mg / PQP 1440mg n=8 participants at risk Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	OZ439 300mg / PQP 1440mg n=7 participants at risk Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	OZ439 800mg / PQP 1440mg n=6 participants at risk Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg	Placebo n=20 participants at risk Cohorts 1, 2, 3, 4 and 5
Blood and lymphatic system disorders Eosinophilia	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.

Other adverse events

Measure	OZ439 100mg n=24 participants at risk Cohorts 1, 2 and 3 OZ439 100mg	OZ439 300mg n=8 participants at risk Cohort 4 - Sequence 1 OZ439 300mg	OZ439 800mg n=7 participants at risk Cohort 5 - Sequence 1 OZ439 800mg	OZ439 100mg / PQP 160mg n=8 participants at risk Cohort 1 - Sequence 2 OZ439 100mg / PQP 160mg	OZ439 100mg / PQP 480mg n=7 participants at risk Cohort 2 - Sequence 2 OZ439 100mg / PQP 480mg	OZ439 100mg / PQP 1440mg n=8 participants at risk Cohort 3 - Sequence 2 OZ439 100mg / PQP 1440mg	OZ439 300mg / PQP 1440mg n=7 participants at risk Cohort 4 - Sequence 2 OZ439 300mg / PQP 1440mg	OZ439 800mg / PQP 1440mg n=6 participants at risk Cohort 5 - Sequence 2 OZ439 800mg / PQP 1440mg	Placebo n=20 participants at risk Cohorts 1, 2, 3, 4 and 5
Blood and lymphatic system disorders Eosinophilia	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 3 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Gastrointestinal disorders Abdominal Discomfort	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 3 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Gastrointestinal disorders Diarrhea	4.2% 1/24 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Gastrointestinal disorders Gastroenteritis Eosinophilic	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Gastrointestinal disorders Nausea	4.2% 1/24 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	12.5% 1/8 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	14.3% 1/7 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	14.3% 1/7 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	16.7% 1/6 • Number of events 2 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/20 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Gastrointestinal disorders Vomiting	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	16.7% 1/6 • Number of events 2 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/20 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
General disorders Malaise	4.2% 1/24 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	12.5% 1/8 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	16.7% 1/6 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/20 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Infections and infestations Nasopharyngitis	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	14.3% 1/7 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	12.5% 1/8 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	14.3% 1/7 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Investigations ALT Increased	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	10.0% 2/20 • Number of events 3 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Investigations AST Increased	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Investigations Blood Creatine Phosphokinase increased	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	25.0% 2/8 • Number of events 2 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	12.5% 1/8 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	14.3% 1/7 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	20.0% 4/20 • Number of events 5 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Metabolism and nutrition disorders Hypercalcaemia	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Metabolism and nutrition disorders Hyperkalaemia	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Musculoskeletal and connective tissue disorders Back Pain	4.2% 1/24 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/20 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.
Nervous system disorders Headache	0.00% 0/24 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/8 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/7 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	0.00% 0/6 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.	5.0% 1/20 • Number of events 1 • From informed consent signature up to final study visit. Safety variables: treatment-emergent adverse events (TEAEs), ECG results, vital signs, laboratory evaluations, in particular liver function tests.

Additional Information

Fiona Macintyre

Medicines for Malaria Venture

Phone: 0041 22 555 0319

Email: macintyref@mmv.org

Results disclosure agreements

• Principal investigator is a sponsor employee
• Publication restrictions are in place

Restriction type: GT60