Trial Outcomes & Findings for Safety, Tolerability and PK of Multiple-ascending Doses of Emodepside (NCT NCT03383614)

NCT ID: NCT03383614

Last Updated: 2020-04-15

Results Overview

Death, serious adverse events (SAEs) and treatment-emergent adverse events (TEAEs).

Recruitment status

COMPLETED

Study phase

PHASE1

Target enrollment

24 participants

Primary outcome timeframe

up to 120 days

Results posted on

2020-04-15

Participant Flow

24 healthy subjects were randomized and received study drug or matching placebo.

Participant milestones

Participant milestones
Measure
Cohort 1: 5mg EMODEPSIDE OD
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
Overall Study
STARTED
6
6
6
6
Overall Study
COMPLETED
6
5
6
6
Overall Study
NOT COMPLETED
0
1
0
0

Reasons for withdrawal

Reasons for withdrawal
Measure
Cohort 1: 5mg EMODEPSIDE OD
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
Overall Study
Withdrawal by Subject
0
1
0
0

Baseline Characteristics

Includes only those subjects who drank alcohol-containing beverages.

Baseline characteristics by cohort

Baseline characteristics by cohort
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Total
n=24 Participants
Total of all reporting groups
Age, Categorical
<=18 years
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Age, Categorical
Between 18 and 65 years
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
24 Participants
n=24 Participants
Age, Categorical
>=65 years
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Age, Continuous
31.0 years
n=6 Participants
33.3 years
n=6 Participants
28.0 years
n=6 Participants
32.7 years
n=6 Participants
31.3 years
n=24 Participants
Sex: Female, Male
Female
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Sex: Female, Male
Male
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
24 Participants
n=24 Participants
Ethnicity (NIH/OMB)
Hispanic or Latino
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Ethnicity (NIH/OMB)
Not Hispanic or Latino
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
24 Participants
n=24 Participants
Ethnicity (NIH/OMB)
Unknown or Not Reported
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Race (NIH/OMB)
American Indian or Alaska Native
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Race (NIH/OMB)
Asian
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Race (NIH/OMB)
Black or African American
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Race (NIH/OMB)
White
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
6 Participants
n=6 Participants
24 Participants
n=24 Participants
Race (NIH/OMB)
More than one race
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Race (NIH/OMB)
Unknown or Not Reported
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=6 Participants
0 Participants
n=24 Participants
Region of Enrollment
United Kingdom
6 participants
n=6 Participants
6 participants
n=6 Participants
6 participants
n=6 Participants
6 participants
n=6 Participants
24 participants
n=24 Participants
Height
179.3 cm
STANDARD_DEVIATION 4.18 • n=6 Participants
179.7 cm
STANDARD_DEVIATION 4.59 • n=6 Participants
181.8 cm
STANDARD_DEVIATION 6.74 • n=6 Participants
182.7 cm
STANDARD_DEVIATION 8.80 • n=6 Participants
180.9 cm
STANDARD_DEVIATION 6.10 • n=24 Participants
Weight
72.18 kg
STANDARD_DEVIATION 6.204 • n=6 Participants
77.70 kg
STANDARD_DEVIATION 17.570 • n=6 Participants
75.23 kg
STANDARD_DEVIATION 9.520 • n=6 Participants
74.73 kg
STANDARD_DEVIATION 8.999 • n=6 Participants
74.96 kg
STANDARD_DEVIATION 10.807 • n=24 Participants
BMI
22.48 kg/m^2
STANDARD_DEVIATION 2.520 • n=6 Participants
23.88 kg/m^2
STANDARD_DEVIATION 4.392 • n=6 Participants
22.72 kg/m^2
STANDARD_DEVIATION 2.111 • n=6 Participants
22.33 kg/m^2
STANDARD_DEVIATION 0.882 • n=6 Participants
22.85 kg/m^2
STANDARD_DEVIATION 2.664 • n=24 Participants
Smokers
2 Participants
n=6 Participants
1 Participants
n=6 Participants
1 Participants
n=6 Participants
0 Participants
n=6 Participants
4 Participants
n=24 Participants
Weekly alcohol consumption (units)
8.3 units/week
STANDARD_DEVIATION 3.79 • n=3 Participants • Includes only those subjects who drank alcohol-containing beverages.
3.3 units/week
STANDARD_DEVIATION 2.31 • n=3 Participants • Includes only those subjects who drank alcohol-containing beverages.
7.0 units/week
STANDARD_DEVIATION 3.46 • n=4 Participants • Includes only those subjects who drank alcohol-containing beverages.
5.8 units/week
STANDARD_DEVIATION 2.17 • n=5 Participants • Includes only those subjects who drank alcohol-containing beverages.
6.1 units/week
STANDARD_DEVIATION 3.11 • n=15 Participants • Includes only those subjects who drank alcohol-containing beverages.
Xanthine
441.7 mL/day
STANDARD_DEVIATION 245.80 • n=6 Participants • Includes only those subjects who drank xanthine-containing beverages.
562.5 mL/day
STANDARD_DEVIATION 239.36 • n=4 Participants • Includes only those subjects who drank xanthine-containing beverages.
283.3 mL/day
STANDARD_DEVIATION 104.08 • n=3 Participants • Includes only those subjects who drank xanthine-containing beverages.
300.0 mL/day
STANDARD_DEVIATION 122.47 • n=6 Participants • Includes only those subjects who drank xanthine-containing beverages.
397.4 mL/day
STANDARD_DEVIATION 209.15 • n=19 Participants • Includes only those subjects who drank xanthine-containing beverages.

PRIMARY outcome

Timeframe: up to 120 days

Population: Adverse events were determined in the Safety population. Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days). AE=adverse event; OD=once daily; BID=twice daily.

Death, serious adverse events (SAEs) and treatment-emergent adverse events (TEAEs).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Adverse Events
AEs
5 Participants
6 Participants
6 Participants
4 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Adverse Events
TEAEs
5 Participants
6 Participants
6 Participants
4 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Adverse Events
Drug-related TEAEs
2 Participants
1 Participants
3 Participants
1 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Adverse Events
SAEs
1 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Adverse Events
Deaths
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Adverse Events
Withdrawals from the study owing to a TEAE
0 Participants
0 Participants
0 Participants
0 Participants

PRIMARY outcome

Timeframe: Up to 120 days

Population: Adverse events were determined in the Safety population. Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days). AE=adverse event; OD=once daily; BID=twice daily.

Number of subjects with a TEAE, by highest level of severity.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Adverse Event Severity
Mild
2 Participants
3 Participants
4 Participants
3 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Adverse Event Severity
Moderate
2 Participants
3 Participants
2 Participants
1 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Adverse Event Severity
Severe
1 Participants
0 Participants
0 Participants
0 Participants

PRIMARY outcome

Timeframe: up to 120 days

Population: Vital signs were measured pre-dose on Day -1, at regular time points until Follow-up (Day 30), and at each long-term follow-up visit. OD=once daily; BID=twice daily; HR=heart rate; BP=blood pressure.

Vital signs included heart rate, systolic and diastolic blood pressure and temperature.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Vital Signs Findings
Clinically significant change in HR
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Vital Signs Findings
Clinically significant change in systolic BP
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Vital Signs Findings
Clinically significant change in diastolic BP
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Vital Signs Findings
Clinically significant change in temperature
0 Participants
0 Participants
0 Participants
0 Participants

PRIMARY outcome

Timeframe: up to 30 days

Population: Twelve-lead ECG assessments were made predose on Day -1 and at regular timepoints until Follow-up (Day 30). ECG=electrocardiogram; OD=once daily; BID=twice daily; PR=PR interval.

The following variables were recorded in 12-lead ECGs: ventricular rate, PR interval, QRS interval, QTcB and QTcF interval.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With 12-lead Electrocardiogram Findings
Clinically significant changes in ventricular rate
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With 12-lead Electrocardiogram Findings
Clinically significant changes in PR interval
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With 12-lead Electrocardiogram Findings
Clinically significant changes in QRS interval
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With 12-lead Electrocardiogram Findings
Clinically significant changes in QTcB interval
0 Participants
0 Participants
0 Participants
0 Participants

PRIMARY outcome

Timeframe: up to 120 days

Population: Clinical laboratory parameters were measured pre-dose on Day -1, at regular time points until Follow-up (Day 30), and at each long-term follow-up visit. OD=once daily; BID=twice daily.

Clinical laboratory parameters included clinical chemistry, hematology, coagulation and urinalysis.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Clinical Laboratory Tests Findings
Clinically significant clinical chemistry changes
0 Participants
0 Participants
1 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Clinical Laboratory Tests Findings
Clinically significant hematology changes
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Clinical Laboratory Tests Findings
Clinically significant coagulation changes
0 Participants
0 Participants
0 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Clinical Laboratory Tests Findings
Clinically significant urinalysis changes
0 Participants
0 Participants
0 Participants
0 Participants

PRIMARY outcome

Timeframe: up to 10 days

Population: Ophthalmological assessments were performed at the second screening visit after all other eligibility criteria had been met and on Day 10. OD=once daily; BID=twice daily.

Ophthalmological examinations at Screening Visit 2 and Day 10 were done at a specialist eye hospital by a Consultant Ophthalmologist, or their assistant. Examinations included: ocular symptoms and history, autorefraction, best correct visual acuity, colour vision, Amsler grid, ocular alignment and motility, confrontation visual field, slit-lamp, measurement of intraocular pressure and an optical coherence tomography test.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Ophthalmology Assessment Findings
Clinically significant ocular symptoms
3 Participants
0 Participants
3 Participants
1 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Ophthalmology Assessment Findings
Clinically significant Amsler grid assessment
1 Participants
0 Participants
0 Participants
0 Participants

PRIMARY outcome

Timeframe: up to 120 days

Population: Physical and neurological examinations were measured pre-dose on Day -1, at regular time points until Follow-up (Day 30), and at each long-term follow-up visit. Results are reported for subjects experiencing abnormal result/AE, as opposed to individual events. OD=once daily; BID=twice daily.

Abnormal or clinically significant physical examination findings during the study or reported as an adverse event.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Physical Examination Findings
Abnormal physical examination
2 Participants
1 Participants
2 Participants
0 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Physical Examination Findings
Physical examination reported as an AE
2 Participants
1 Participants
1 Participants
0 Participants

PRIMARY outcome

Timeframe: up to 120 days

Population: Neurological examinations were measured pre-dose on Day -1, at regular time points until Follow-up (Day 30), and at each long-term follow-up visit. OD=once daily; BID=twice daily.

Abnormal or clinically significant neurological examination findings during the study or reported as an adverse event.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Neurological Examination Findings
Abnormal neurological examination
2 Participants
1 Participants
1 Participants
1 Participants
Safety and Tolerability of Emodepside After Multiple Doses as Measured by Number of Participants With Neurological Examination Findings
Neurological examination reported as an AE
1 Participants
1 Participants
1 Participants
1 Participants

SECONDARY outcome

Timeframe: From Day 1, pre-dose to Day 9, 24 hours post-dose

Population: OD=once daily; BID=twice daily.

Summary of geometric mean emodepside plasma pharmacokinetic concentration-time data (ng/mL) during the repeated dosing period (Days 0-9) in healthy men. Subjects in the 10 mg emodepside BID dosing group had twice-daily doses on Days 0-8 and a single dose on the morning of Day 9. Therefore, the Day 9, 24 h post-dose value was not comparable to the previous value in that dosing group.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 1, pre-dose
8.77 ng/mL
Geometric Coefficient of Variation 35.8
15.78 ng/mL
Geometric Coefficient of Variation 42.9
45.94 ng/mL
Geometric Coefficient of Variation 35.1
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 2, pre-dose
15.24 ng/mL
Geometric Coefficient of Variation 31.1
28.80 ng/mL
Geometric Coefficient of Variation 40.0
64.62 ng/mL
Geometric Coefficient of Variation 38.5
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 3, pre-dose
21.22 ng/mL
Geometric Coefficient of Variation 35.0
39.08 ng/mL
Geometric Coefficient of Variation 45.6
84.65 ng/mL
Geometric Coefficient of Variation 37.7
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 4, pre-dose
24.81 ng/mL
Geometric Coefficient of Variation 37.4
47.38 ng/mL
Geometric Coefficient of Variation 42.2
98.01 ng/mL
Geometric Coefficient of Variation 32.0
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 5, pre-dose
31.46 ng/mL
Geometric Coefficient of Variation 36.3
60.07 ng/mL
Geometric Coefficient of Variation 42.9
120.98 ng/mL
Geometric Coefficient of Variation 31.1
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 6, pre-dose
36.68 ng/mL
Geometric Coefficient of Variation 36.7
70.88 ng/mL
Geometric Coefficient of Variation 39.6
137.60 ng/mL
Geometric Coefficient of Variation 35.2
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 7, pre-dose
40.57 ng/mL
Geometric Coefficient of Variation 31.4
83.31 ng/mL
Geometric Coefficient of Variation 43.0
149.41 ng/mL
Geometric Coefficient of Variation 33.3
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 8, pre-dose
46.91 ng/mL
Geometric Coefficient of Variation 36.8
91.63 ng/mL
Geometric Coefficient of Variation 42.4
179.90 ng/mL
Geometric Coefficient of Variation 35.3
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 9, pre-dose
49.73 ng/mL
Geometric Coefficient of Variation 35.1
97.11 ng/mL
Geometric Coefficient of Variation 44.0
184.94 ng/mL
Geometric Coefficient of Variation 37.1
Geometric Mean Emodepside Plasma Pharmacokinetic Concentration-Time Data During the Repeated Dosing Period
Day 9, 24 hour post-dose
51.76 ng/mL
Geometric Coefficient of Variation 36.6
108.17 ng/mL
Geometric Coefficient of Variation 49.1
176.10 ng/mL
Geometric Coefficient of Variation 39.8

SECONDARY outcome

Timeframe: AUClast in plasma after the last dose (Day 9)

Population: OD=once daily; BID=twice daily.

Summary of AUClast of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120h (Day 14) after the morning dose. AUClast: the area under the concentration-time curve from time zero (pre-dose) to the time of last quantifiable concentration. PK=pharmacokinetic. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUClast of Emodepside in Plasma
19359 h*ng/mL
Geometric Coefficient of Variation 29.9
40655 h*ng/mL
Geometric Coefficient of Variation 43.5
59554 h*ng/mL
Geometric Coefficient of Variation 29.1

SECONDARY outcome

Timeframe: AUClast /D in plasma after the last dose (Day 9)

Population: OD=once daily; BID=twice daily.

Summary of AUClast/D of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120h (Day 14) after the morning dose. AUClast/D: the area under the concentration-time curve from time zero (pre-dose) to the time of last quantifiable concentration corrected for dose. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUClast/D of Emodepside in Plasma
3872 h*ng/mL/mg
Geometric Coefficient of Variation 29.9
4065 h*ng/mL/mg
Geometric Coefficient of Variation 43.5
5955 h*ng/mL/mg
Geometric Coefficient of Variation 29.1

SECONDARY outcome

Timeframe: AUClast,norm in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of AUClast,norm of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120h (Day 14) after the morning dose. AUClast,norm: the area under the concentration-time curve from time zero (pre-dose) to the time of last quantifiable concentration corrected by dose and body weight. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUClast,Norm of Emodepside in Plasma
53.9 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 33.1
52.9 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 69.5
79.1 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 40.6

SECONDARY outcome

Timeframe: AUC12 in plasma after the first (Day 0) and last (Day 9) dose

Population: BID=twice daily.

Summary of AUC12 of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120h (Day 14) after the morning dose. AUC12: the area under the concentration-time curve from time zero (pre-dose) to 12h. Note: AUC12 was calculated only in Cohort 3. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUC12 of Emodepside in Plasma
Day 0
742 h*ng/mL
Geometric Coefficient of Variation 29.4
The AUC12 of Emodepside in Plasma
Day 9
2810 h*ng/mL
Geometric Coefficient of Variation 35.0

SECONDARY outcome

Timeframe: AUC12/D in plasma after the first (Day 0) and last (Day 9) dose

Population: BID=twice daily.

Summary of AUC12/D of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120h (Day 14) after the morning dose. AUC12/D: the area under the concentration-time curve from time zero (pre-dose) to 12h, corrected for dose. Note: AUC12/D was collected only in Cohort 3. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUC12/D of Emodepside in Plasma
Day 0
74.2 h*ng/mL/mg
Geometric Coefficient of Variation 29.4
The AUC12/D of Emodepside in Plasma
Day 9
281 h*ng/mL/mg
Geometric Coefficient of Variation 35.0

SECONDARY outcome

Timeframe: AUC12,norm in plasma after the first (Day 0) and last (Day 9) dose

Population: BID=twice daily.

Summary of AUC12,norm of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. AUC12,norm: the area under the concentration-time curve from time zero (pre-dose) to 12 h corrected by dose and body weight. Note: AUC12,norm was calculated only in Cohort 3. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUC12,Norm of Emodepside in Plasma
Day 0
0.985 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 39.2
The AUC12,Norm of Emodepside in Plasma
Day 9
3.73 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 46.6

SECONDARY outcome

Timeframe: AUC24 in plasma after the first (Day 0) and last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of AUC24 of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. AUC24: the area under the concentration-time curve from time zero (pre-dose) to 24 h. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUC24 of Emodepside in Plasma
Day 0
574 h*ng/mL
Geometric Coefficient of Variation 19.7
1135 h*ng/mL
Geometric Coefficient of Variation 32.7
1428 h*ng/mL
Geometric Coefficient of Variation 26.5
The AUC24 of Emodepside in Plasma
Day 9
1689 h*ng/mL
Geometric Coefficient of Variation 31.3
3487 h*ng/mL
Geometric Coefficient of Variation 44.2
4897 h*ng/mL
Geometric Coefficient of Variation 35.8

SECONDARY outcome

Timeframe: AUC24/D in plasma after the first (Day 0) and last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of AUC24/D of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. AUC24/D: the area under the concentration-time curve from time zero (pre-dose) to 24h corrected for dose. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUC24/D of Emodepside in Plasma
Day 0
115 h*ng/mL/mg
Geometric Coefficient of Variation 19.7
113 h*ng/mL/mg
Geometric Coefficient of Variation 32.7
71.4 h*ng/mL/mg
Geometric Coefficient of Variation 26.5
The AUC24/D of Emodepside in Plasma
Day 9
338 h*ng/mL/mg
Geometric Coefficient of Variation 31.3
349 h*ng/mL/mg
Geometric Coefficient of Variation 44.2
490 h*ng/mL/mg
Geometric Coefficient of Variation 35.8

SECONDARY outcome

Timeframe: AUC24,norm in plasma at Day 0 and Day 9

Population: OD=once daily; BID=twice daily.

Summary of AUC24,norm of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120h (Day 14) after the morning dose. AUC24,norm: the area under the concentration-time curve from time zero (pre-dose) to 24h corrected by dose and body weight. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The AUC24,Norm of Emodepside in Plasma
Day 0
1.60 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 21.5
1.48 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 56.7
0.948 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 36.5
The AUC24,Norm of Emodepside in Plasma
Day 9
4.70 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 34.1
4.54 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 69.7
6.50 (h*ng/mL)/(mg*kg)
Geometric Coefficient of Variation 47.7

SECONDARY outcome

Timeframe: Cmax in plasma after the first (Day 0) and last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of Cmax of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. Cmax: the observed maximum plasma concentration measured in a subject after dosing identified by inspection of the drug concentration vs. time data. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Cmax of Emodepside in Plasma
Day 0
93.8 ng/mL
Geometric Coefficient of Variation 17.8
186 ng/mL
Geometric Coefficient of Variation 21.3
160 ng/mL
Geometric Coefficient of Variation 20.4
The Cmax of Emodepside in Plasma
Day 9
149 ng/mL
Geometric Coefficient of Variation 17.9
287 ng/mL
Geometric Coefficient of Variation 39.7
349 ng/mL
Geometric Coefficient of Variation 27.1

SECONDARY outcome

Timeframe: Cmax/D in plasma after the first (Day 0) and last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of Cmax/D of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. Cmax/D: the observed maximum plasma concentration measured in a subject after dosing identified by inspection of the drug concentration vs. time data, corrected for dose. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Cmax/D of Emodepside in Plasma
Day 0
18.8 ng/mL/mg
Geometric Coefficient of Variation 17.8
18.6 ng/mL/mg
Geometric Coefficient of Variation 21.3
16.0 ng/mL/mg
Geometric Coefficient of Variation 20.4
The Cmax/D of Emodepside in Plasma
Day 9
29.9 ng/mL/mg
Geometric Coefficient of Variation 17.9
28.7 ng/mL/mg
Geometric Coefficient of Variation 39.7
34.9 ng/mL/mg
Geometric Coefficient of Variation 27.1

SECONDARY outcome

Timeframe: Cmax,norm in plasma after the first (Day 0) and last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of Cmax,norm of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. Cmax,norm: the observed maximum plasma concentration measured in a subject after dosing identified by inspection of the drug concentration vs. time data, corrected for dose and body weight. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Cmax,Norm of Emodepside in Plasma
Day 0
0.261 (ng/mL)*(mg*kg)
Geometric Coefficient of Variation 18.4
0.242 (ng/mL)*(mg*kg)
Geometric Coefficient of Variation 42.8
0.212 (ng/mL)*(mg*kg)
Geometric Coefficient of Variation 28.7
The Cmax,Norm of Emodepside in Plasma
Day 9
0.416 (ng/mL)*(mg*kg)
Geometric Coefficient of Variation 20.6
0.374 (ng/mL)*(mg*kg)
Geometric Coefficient of Variation 65.4
0.464 (ng/mL)*(mg*kg)
Geometric Coefficient of Variation 38.2

SECONDARY outcome

Timeframe: Ctrough in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of Ctrough (log-transformed) of emodepside after last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. Ctrough: trough plasma concentration (measured concentration at the end of a dosing interval on Day 9 \[taken directly before next administration\]) obtained directly from the concentration-time data. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Ctrough of Emodepside in Plasma
49.7 ng/mL
Geometric Coefficient of Variation 36.8
97.1 ng/mL
Geometric Coefficient of Variation 50.8
185 ng/mL
Geometric Coefficient of Variation 39.5

SECONDARY outcome

Timeframe: tmax in plasma after the first (Day 0) and last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of tmax of emodepside after the first (Day 0) and last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. tmax: the time at which Cmax was apparent, identified by inspection of the drug concentration vs. time data.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Tmax of Emodepside in Plasma
Day 0
1.00 Hours
Interval 1.0 to 1.07
1.25 Hours
Interval 1.0 to 2.0
1.00 Hours
Interval 1.0 to 1.58
The Tmax of Emodepside in Plasma
Day 9
1.00 Hours
Interval 1.0 to 1.5
1.25 Hours
Interval 1.0 to 2.0
1.50 Hours
Interval 1.03 to 2.5

SECONDARY outcome

Timeframe: t1/2 in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of t1/2 of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. t1/2: terminal half-life. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The t1/2 of Emodepside in Plasma
419 Hours
Geometric Coefficient of Variation 42.6
450 Hours
Geometric Coefficient of Variation 30.6
508 Hours
Geometric Coefficient of Variation 56.9

SECONDARY outcome

Timeframe: t1/2,(0-24) in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of t1/2,(0-24) of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. t1/2,(0-24): half-life calculated from the terminal slope of the log concentration-time (0-24h) curve. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The t1/2,(0-24) of Emodepside in Plasma
26.9 Hours
Geometric Coefficient of Variation 52.4
18.4 Hours
Geometric Coefficient of Variation 30.0
33.2 Hours
Geometric Coefficient of Variation 55.0

SECONDARY outcome

Timeframe: λz in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of λz of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. λz: terminal rate constant. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The λz of Emodepside in Plasma
0.00166 1/h
Geometric Coefficient of Variation 42.6
0.00154 1/h
Geometric Coefficient of Variation 30.6
0.00137 1/h
Geometric Coefficient of Variation 56.9

SECONDARY outcome

Timeframe: CLss/F in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of CLss/F of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. CLss/F: apparent total clearance from plasma on Day 9. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The CLss/F of Emodepside in Plasma
2.96 L/h
Geometric Coefficient of Variation 31.3
2.87 L/h
Geometric Coefficient of Variation 44.2
3.56 L/h
Geometric Coefficient of Variation 35.0

SECONDARY outcome

Timeframe: Vz/F in plasma after the last (Day 9) dose

Population: OD=once daily; BID=twice daily.

Summary of Vz/F of emodepside after the last (Day 9) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 9 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12, 15, 24, 36 (Day 10), 48 (Day 11), 72 (Day 12), 96 (Day 13) and 120 h (Day 14) after the morning dose. Vz/F: apparent volume of distribution on Day 9. The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Vz/F of Emodepside in Plasma
1788 litre(s)
Geometric Coefficient of Variation 74.2
1861 litre(s)
Geometric Coefficient of Variation 68.5
2607 litre(s)
Geometric Coefficient of Variation 102.1

SECONDARY outcome

Timeframe: MRTlast in plasma after the first (Day 0) dose

Population: OD=once daily; BID=twice daily.

Summary of MRTlast of emodepside after the first (Day 0) dose for 10-day oral treatment courses in healthy men: PK parameter population. Data on Day 0 was collected at the following time points: pre-dose, 0.25, 0.5, 1, 1.5, 2, 2.5, 3, 4, 6, 8, 12 and 15 h after the morning dose. MRTlast: mean residence time from time zero (pre-dose) to the time of last quantifiable concentration (measurable up to 24h after dosing on Day 0). The geometric coefficient of variation is the between-subject coefficient of variation (%CVb).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The MRTlast of Emodepside in Plasma
7.28 Hours
Geometric Coefficient of Variation 10.7
7.00 Hours
Geometric Coefficient of Variation 11.0
10.8 Hours
Geometric Coefficient of Variation 2.8

SECONDARY outcome

Timeframe: Rac(AUC12) after 10 days' repeated doses of 10 mg emodepside (Day 9)

Population: BID=twice daily.

Summary of emodepside plasma Rac(AUC12) after 10 days' repeated doses of 10 mg emodepside (Day 9): PK parameter population. Rac(AUC12): accumulation ratio calculated from AUC12, where AUC12 is the area under the concentration-time curve from time zero (pre-dose) to 12h. Note: measure of dispersion is 'percentage coefficient of variation' (the between-subject coefficient of variation \[%CVb\]). Note: Rac(AUC12) was calculated only in Cohort 3.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Rac(AUC12) of Emodepside in Plasma
3.83 Ratio
Standard Deviation 15.5

SECONDARY outcome

Timeframe: Rac(AUC24) after 10 days' repeated doses of 10 mg emodepside (Day 9)

Population: OD=once daily; BID=twice daily.

Summary of emodepside plasma Rac(AUC24) after 10 days' repeated doses of 10 mg emodepside (Day 9): PK parameter population. Rac(AUC24): accumulation ratio calculated from AUC24, where AUC24 is the area under the concentration-time curve from time zero (pre-dose) to 24h. Note: measure of dispersion is 'percentage coefficient of variation' (the between-subject coefficient of variation \[%CVb\]).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Rac(AUC24) of Emodepside in Plasma
2.97 Ratio
Standard Deviation 16.1
3.09 Ratio
Standard Deviation 11.3
3.47 Ratio
Standard Deviation 17.1

SECONDARY outcome

Timeframe: Rac(Cmax) after 10 days' repeated doses of 10 mg emodepside (Day 9)

Population: OD=once daily; BID=twice daily.

Summary of emodepside plasma Rac(Cmax) after 10 days' repeated doses of 10 mg emodepside (Day 9): PK parameter population. Rac(Cmax): accumulation ratio calculated from Cmax, where Cmax is the observed maximum plasma concentration measured in a subject after dosing identified by inspection of the drug concentration vs. time data. Note: measure of dispersion is 'percentage coefficient of variation' (the between-subject coefficient of variation \[%CVb\]).

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
The Rac(Cmax) of Emodepside in Plasma
1.61 Ratio
Standard Deviation 16.5
1.58 Ratio
Standard Deviation 24.1
2.21 Ratio
Standard Deviation 17.4

SECONDARY outcome

Timeframe: Mean glucose at Day -1 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean glucose concentrations (mmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day -1.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Glucose Concentration at Day -1
-24 h
4.72 mmol/L
Standard Deviation 0.286
4.68 mmol/L
Standard Deviation 0.349
4.80 mmol/L
Standard Deviation 0.245
4.77 mmol/L
Standard Deviation 0.468
Mean Glucose Concentration at Day -1
-23 h
4.90 mmol/L
Standard Deviation 0.308
4.85 mmol/L
Standard Deviation 0.259
4.85 mmol/L
Standard Deviation 0.281
4.92 mmol/L
Standard Deviation 0.313
Mean Glucose Concentration at Day -1
-22 h
4.77 mmol/L
Standard Deviation 0.378
4.72 mmol/L
Standard Deviation 0.371
4.72 mmol/L
Standard Deviation 0.279
4.82 mmol/L
Standard Deviation 0.360
Mean Glucose Concentration at Day -1
-20 h
4.63 mmol/L
Standard Deviation 0.388
4.57 mmol/L
Standard Deviation 0.207
4.55 mmol/L
Standard Deviation 0.207
4.73 mmol/L
Standard Deviation 0.480
Mean Glucose Concentration at Day -1
-12 h
5.17 mmol/L
Standard Deviation 0.712
5.55 mmol/L
Standard Deviation 0.451
5.52 mmol/L
Standard Deviation 0.556
5.48 mmol/L
Standard Deviation 0.806

SECONDARY outcome

Timeframe: Mean glucose after repeated once or twice daily dosing for up to 10 days

Population: OD=once daily; BID=twice daily.

Mean glucose concentrations (mmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day 0. Baseline=predose on Day 0.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Glucose Concentration at Day 0
Predose (Baseline)
4.96 mmol/L
Standard Deviation 0.321
4.85 mmol/L
Standard Deviation 0.409
4.85 mmol/L
Standard Deviation 0.351
4.85 mmol/L
Standard Deviation 0.288
Mean Glucose Concentration at Day 0
1 h
5.07 mmol/L
Standard Deviation 0.367
5.57 mmol/L
Standard Deviation 0.816
5.42 mmol/L
Standard Deviation 0.445
4.78 mmol/L
Standard Deviation 0.214
Mean Glucose Concentration at Day 0
2 h
5.05 mmol/L
Standard Deviation 0.327
5.28 mmol/L
Standard Deviation 0.508
5.27 mmol/L
Standard Deviation 0.472
4.70 mmol/L
Standard Deviation 0.310
Mean Glucose Concentration at Day 0
4 h
4.73 mmol/L
Standard Deviation 0.378
4.75 mmol/L
Standard Deviation 0.274
4.82 mmol/L
Standard Deviation 0.279
4.70 mmol/L
Standard Deviation 0.276
Mean Glucose Concentration at Day 0
12 h
5.68 mmol/L
Standard Deviation 0.268
6.22 mmol/L
Standard Deviation 0.343
5.57 mmol/L
Standard Deviation 0.554
6.27 mmol/L
Standard Deviation 0.761
Mean Glucose Concentration at Day 0
24 h
5.07 mmol/L
Standard Deviation 0.314
4.88 mmol/L
Standard Deviation 0.264
4.87 mmol/L
Standard Deviation 0.273
4.97 mmol/L
Standard Deviation 0.288

SECONDARY outcome

Timeframe: Mean glucose at Day 9 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean glucose concentrations (mmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day 9.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Glucose Concentration at Day 9
Predose
4.52 mmol/L
Standard Deviation 0.306
4.95 mmol/L
Standard Deviation 0.362
4.97 mmol/L
Standard Deviation 0.314
4.67 mmol/L
Standard Deviation 0.234
Mean Glucose Concentration at Day 9
1 h
5.10 mmol/L
Standard Deviation 0.352
5.98 mmol/L
Standard Deviation 1.972
5.65 mmol/L
Standard Deviation 0.771
4.80 mmol/L
Standard Deviation 0.219
Mean Glucose Concentration at Day 9
2 h
5.03 mmol/L
Standard Deviation 0.250
5.72 mmol/L
Standard Deviation 1.543
5.57 mmol/L
Standard Deviation 0.761
4.74 mmol/L
Standard Deviation 0.329
Mean Glucose Concentration at Day 9
4 h
4.60 mmol/L
Standard Deviation 0.363
4.62 mmol/L
Standard Deviation 0.377
5.08 mmol/L
Standard Deviation 0.662
4.70 mmol/L
Standard Deviation 0.374
Mean Glucose Concentration at Day 9
12 h
5.58 mmol/L
Standard Deviation 0.319
6.00 mmol/L
Standard Deviation 0.745
7.03 mmol/L
Standard Deviation 1.111
6.02 mmol/L
Standard Deviation 0.615
Mean Glucose Concentration at Day 9
24 h
4.92 mmol/L
Standard Deviation 0.264
5.10 mmol/L
Standard Deviation 0.490
5.17 mmol/L
Standard Deviation 0.273
4.82 mmol/L
Standard Deviation 0.160
Mean Glucose Concentration at Day 9
48 h
5.02 mmol/L
Standard Deviation 0.194
5.07 mmol/L
Standard Deviation 0.532
5.10 mmol/L
Standard Deviation 0.390
4.90 mmol/L
Standard Deviation 0.379
Mean Glucose Concentration at Day 9
72 h
4.87 mmol/L
Standard Deviation 0.350
5.13 mmol/L
Standard Deviation 0.589
5.03 mmol/L
Standard Deviation 0.308
5.03 mmol/L
Standard Deviation 0.280
Mean Glucose Concentration at Day 9
96 h
4.80 mmol/L
Standard Deviation 0.276
5.10 mmol/L
Standard Deviation 0.540
4.85 mmol/L
Standard Deviation 0.315
4.87 mmol/L
Standard Deviation 0.320
Mean Glucose Concentration at Day 9
120 h
5.00 mmol/L
Standard Deviation 0.352
4.98 mmol/L
Standard Deviation 0.458
5.05 mmol/L
Standard Deviation 0.288
4.90 mmol/L
Standard Deviation 0.352

SECONDARY outcome

Timeframe: Mean glucose at Day 30 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean glucose concentrations (mmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day 30.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Glucose Concentration at Day 30
4.83 mmol/L
Standard Deviation 0.288
5.23 mmol/L
Standard Deviation 0.993
4.97 mmol/L
Standard Deviation 0.234
4.53 mmol/L
Standard Deviation 0.350

SECONDARY outcome

Timeframe: Mean insulin concentration at Day-1 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean insulin concentration (pmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day -1.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Insulin Concentration at Day -1
-24 h
29.0 pmol/L
Standard Deviation 8.60
25.8 pmol/L
Standard Deviation 8.11
33.2 pmol/L
Standard Deviation 17.90
32.3 pmol/L
Standard Deviation 12.31
Mean Insulin Concentration at Day -1
-23 h
25.8 pmol/L
Standard Deviation 3.87
26.2 pmol/L
Standard Deviation 7.73
28.0 pmol/L
Standard Deviation 11.33
26.5 pmol/L
Standard Deviation 8.92
Mean Insulin Concentration at Day -1
-22 h
24.0 pmol/L
Standard Deviation 6.69
25.7 pmol/L
Standard Deviation 8.91
28.3 pmol/L
Standard Deviation 14.50
33.0 pmol/L
Standard Deviation 5.73
Mean Insulin Concentration at Day -1
-20 h
22.7 pmol/L
Standard Deviation 6.02
22.7 pmol/L
Standard Deviation 7.97
24.3 pmol/L
Standard Deviation 9.18
24.5 pmol/L
Standard Deviation 12.76
Mean Insulin Concentration at Day -1
-12 h
129.5 pmol/L
Standard Deviation 54.14
157.0 pmol/L
Standard Deviation 81.51
204.7 pmol/L
Standard Deviation 78.37
136.5 pmol/L
Standard Deviation 64.30

SECONDARY outcome

Timeframe: Mean insulin concentration at Day 0 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean insulin concentration (pmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day 0. Baseline=predose on Day 0.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Insulin Concentration at Day 0
Predose (Baseline)
27.8 pmol/L
Standard Deviation 15.41
29.3 pmol/L
Standard Deviation 5.09
32.2 pmol/L
Standard Deviation 14.34
30.5 pmol/L
Standard Deviation 12.55
Mean Insulin Concentration at Day 0
1 h
25.0 pmol/L
Standard Deviation 3.79
23.2 pmol/L
Standard Deviation 10.85
29.2 pmol/L
Standard Deviation 14.86
33.0 pmol/L
Standard Deviation 9.10
Mean Insulin Concentration at Day 0
2 h
24.3 pmol/L
Standard Deviation 5.20
25.3 pmol/L
Standard Deviation 9.99
36.3 pmol/L
Standard Deviation 20.39
31.2 pmol/L
Standard Deviation 12.89
Mean Insulin Concentration at Day 0
4 h
21.7 pmol/L
Standard Deviation 5.01
21.7 pmol/L
Standard Deviation 5.39
27.7 pmol/L
Standard Deviation 11.69
20.2 pmol/L
Standard Deviation 6.85
Mean Insulin Concentration at Day 0
12 h
127.2 pmol/L
Standard Deviation 67.59
203.2 pmol/L
Standard Deviation 83.22
175.3 pmol/L
Standard Deviation 64.59
195.0 pmol/L
Standard Deviation 88.03
Mean Insulin Concentration at Day 0
24 h
36.7 pmol/L
Standard Deviation 15.49
41.2 pmol/L
Standard Deviation 14.51
30.3 pmol/L
Standard Deviation 11.43
35.2 pmol/L
Standard Deviation 16.59

SECONDARY outcome

Timeframe: Mean insulin concentration at Day 9 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean insulin concentration (pmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day 9.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Insulin Concentration at Day 9
Predose
31.5 pmol/L
Standard Deviation 8.62
32.7 pmol/L
Standard Deviation 15.02
29.2 pmol/L
Standard Deviation 10.19
31.3 pmol/L
Standard Deviation 9.83
Mean Insulin Concentration at Day 9
1 h
29.2 pmol/L
Standard Deviation 9.66
24.4 pmol/L
Standard Deviation 15.39
22.2 pmol/L
Standard Deviation 8.89
27.8 pmol/L
Standard Deviation 9.77
Mean Insulin Concentration at Day 9
2 h
27.7 pmol/L
Standard Deviation 4.84
31.2 pmol/L
Standard Deviation 10.53
30.2 pmol/L
Standard Deviation 13.91
29.8 pmol/L
Standard Deviation 10.26
Mean Insulin Concentration at Day 9
4 h
23.0 pmol/L
Standard Deviation 7.35
28.4 pmol/L
Standard Deviation 13.24
19.5 pmol/L
Standard Deviation 9.12
21.8 pmol/L
Standard Deviation 6.37
Mean Insulin Concentration at Day 9
12 h
147.2 pmol/L
Standard Deviation 77.58
143.0 pmol/L
Standard Deviation 113.7
215.8 pmol/L
Standard Deviation 128.1
215.7 pmol/L
Standard Deviation 151.8
Mean Insulin Concentration at Day 9
24 h
34.5 pmol/L
Standard Deviation 11.88
36.5 pmol/L
Standard Deviation 12.24
32.7 pmol/L
Standard Deviation 17.44
36.3 pmol/L
Standard Deviation 13.03
Mean Insulin Concentration at Day 9
48 h
36.2 pmol/L
Standard Deviation 5.60
44.8 pmol/L
Standard Deviation 17.89
36.3 pmol/L
Standard Deviation 13.59
38.2 pmol/L
Standard Deviation 19.17
Mean Insulin Concentration at Day 9
72 h
48.3 pmol/L
Standard Deviation 23.53
40.7 pmol/L
Standard Deviation 13.88
39.8 pmol/L
Standard Deviation 15.61
38.7 pmol/L
Standard Deviation 14.42
Mean Insulin Concentration at Day 9
96 h
37.8 pmol/L
Standard Deviation 10.42
39.3 pmol/L
Standard Deviation 12.31
37.2 pmol/L
Standard Deviation 17.66
30.0 pmol/L
Standard Deviation 11.63
Mean Insulin Concentration at Day 9
120 h
39.0 pmol/L
Standard Deviation 8.63
42.3 pmol/L
Standard Deviation 17.92
36.0 pmol/L
Standard Deviation 15.24
33.2 pmol/L
Standard Deviation 21.68

SECONDARY outcome

Timeframe: Mean insulin concentration at Day 30 after repeated once or twice daily dosing

Population: OD=once daily; BID=twice daily.

Mean insulin concentration (pmol/L) after repeated once or twice daily dosing with up to 10 mg emodepside or placebo at Day 30.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Insulin Concentration at Day 30
29.2 pmol/L
Standard Deviation 12.50
60.3 pmol/L
Standard Deviation 90.19
24.3 pmol/L
Standard Deviation 9.79
29.2 pmol/L
Standard Deviation 20.21

SECONDARY outcome

Timeframe: Mean serum glucose concentration at Day -2, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum glucose concentration at Day -2, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Glucose Concentration at Day -2
0 h (Baseline)
4.72 mmol/L
Standard Deviation 0.319
4.92 mmol/L
Standard Deviation 0.256
4.97 mmol/L
Standard Deviation 0.294
4.78 mmol/L
Standard Deviation 0.133
Mean Serum Glucose Concentration at Day -2
1 h
8.78 mmol/L
Standard Deviation 1.659
7.03 mmol/L
Standard Deviation 0.301
7.00 mmol/L
Standard Deviation 0.867
6.48 mmol/L
Standard Deviation 1.450
Mean Serum Glucose Concentration at Day -2
2 h
5.98 mmol/L
Standard Deviation 1.512
5.05 mmol/L
Standard Deviation 0.589
5.48 mmol/L
Standard Deviation 0.608
4.95 mmol/L
Standard Deviation 0.965
Mean Serum Glucose Concentration at Day -2
4 h
4.57 mmol/L
Standard Deviation 0.979
3.95 mmol/L
Standard Deviation 0.622
4.22 mmol/L
Standard Deviation 0.371
4.53 mmol/L
Standard Deviation 0.294

SECONDARY outcome

Timeframe: Mean serum glucose concentration at Day 1, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum glucose concentration at Day 1, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Glucose Concentration at Day 1
Predose (Baseline)
5.07 mmol/L
Standard Deviation 0.314
4.88 mmol/L
Standard Deviation 0.264
4.87 mmol/L
Standard Deviation 0.273
4.97 mmol/L
Standard Deviation 0.228
Mean Serum Glucose Concentration at Day 1
1 h
10.10 mmol/L
Standard Deviation 1.170
12.37 mmol/L
Standard Deviation 2.826
12.03 mmol/L
Standard Deviation 0.989
7.58 mmol/L
Standard Deviation 2.242
Mean Serum Glucose Concentration at Day 1
2 h
6.17 mmol/L
Standard Deviation 1.600
7.95 mmol/L
Standard Deviation 1.653
9.25 mmol/L
Standard Deviation 2.740
5.88 mmol/L
Standard Deviation 1.174
Mean Serum Glucose Concentration at Day 1
4 h
3.95 mmol/L
Standard Deviation 0.339
3.65 mmol/L
Standard Deviation 0.362
4.02 mmol/L
Standard Deviation 0.204
4.15 mmol/L
Standard Deviation 0.575

SECONDARY outcome

Timeframe: Mean serum glucose concentration at Day 8, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum glucose concentration at Day 8, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Glucose Concentration at Day 8
Predose (Baseline)
4.87 mmol/L
Standard Deviation 0.314
5.10 mmol/L
Standard Deviation 0.533
4.90 mmol/L
Standard Deviation 0.303
4.83 mmol/L
Standard Deviation 0.258
Mean Serum Glucose Concentration at Day 8
1 h
10.02 mmol/L
Standard Deviation 1.857
11.75 mmol/L
Standard Deviation 4.574
11.27 mmol/L
Standard Deviation 2.738
7.77 mmol/L
Standard Deviation 1.679
Mean Serum Glucose Concentration at Day 8
2 h
7.05 mmol/L
Standard Deviation 1.533
8.98 mmol/L
Standard Deviation 4.311
8.97 mmol/L
Standard Deviation 2.837
5.52 mmol/L
Standard Deviation 0.783
Mean Serum Glucose Concentration at Day 8
4 h
3.93 mmol/L
Standard Deviation 0.965
4.12 mmol/L
Standard Deviation 0.933
4.52 mmol/L
Standard Deviation 0.806
4.13 mmol/L
Standard Deviation 0.197

SECONDARY outcome

Timeframe: Mean serum glucose concentration at Day 120, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum glucose concentration at Day 120, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day. Note: At Day 120, serum glucose concentration was only measured in Cohort 3 (10 mg BID)

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Glucose Concentration at Day 120
0 h (Baseline)
4.93 mmol/L
Standard Deviation 0.294
Mean Serum Glucose Concentration at Day 120
1 h
8.12 mmol/L
Standard Deviation 2.542
Mean Serum Glucose Concentration at Day 120
2 h
6.08 mmol/L
Standard Deviation 0.540
Mean Serum Glucose Concentration at Day 120
4 h
4.26 mmol/L
Standard Deviation 0.305

SECONDARY outcome

Timeframe: Mean serum insulin concentration at Day -2, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum insulin concentration at Day -2, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Insulin Concentration at Day -2
0 h (Baseline)
24.5 pmol/L
Standard Deviation 13.81
25.7 pmol/L
Standard Deviation 8.55
27.0 pmol/L
Standard Deviation 14.00
29.0 pmol/L
Standard Deviation 14.68
Mean Serum Insulin Concentration at Day -2
1 h
334.8 pmol/L
Standard Deviation 207.66
305.3 pmol/L
Standard Deviation 65.59
306.7 pmol/L
Standard Deviation 180.00
338.3 pmol/L
Standard Deviation 189.61
Mean Serum Insulin Concentration at Day -2
2 h
174.7 pmol/L
Standard Deviation 206.08
103.7 pmol/L
Standard Deviation 32.38
136.0 pmol/L
Standard Deviation 70.52
186.8 pmol/L
Standard Deviation 83.55
Mean Serum Insulin Concentration at Day -2
4 h
44.3 pmol/L
Standard Deviation 72.56
17.2 pmol/L
Standard Deviation 6.11
20.8 pmol/L
Standard Deviation 7.44
21.8 pmol/L
Standard Deviation 9.33

SECONDARY outcome

Timeframe: Mean serum insulin concentration at Day 1, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum insulin concentration at Day 1, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Insulin Concentration at Day 1
Predose (Baseline)
36.7 pmol/L
Standard Deviation 15.49
41.2 pmol/L
Standard Deviation 14.51
30.3 pmol/L
Standard Deviation 11.43
35.2 pmol/L
Standard Deviation 16.59
Mean Serum Insulin Concentration at Day 1
1 h
312.2 pmol/L
Standard Deviation 153.67
288.8 pmol/L
Standard Deviation 171.44
332.2 pmol/L
Standard Deviation 228.84
606.7 pmol/L
Standard Deviation 157.35
Mean Serum Insulin Concentration at Day 1
2 h
268.5 pmol/L
Standard Deviation 107.14
377.3 pmol/L
Standard Deviation 224.73
336.2 pmol/L
Standard Deviation 165.71
238.0 pmol/L
Standard Deviation 165.06
Mean Serum Insulin Concentration at Day 1
4 h
28.8 pmol/L
Standard Deviation 22.35
30.8 pmol/L
Standard Deviation 12.35
35.7 pmol/L
Standard Deviation 4.59
33.8 pmol/L
Standard Deviation 19.56

SECONDARY outcome

Timeframe: Mean serum insulin concentration at Day 8, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum insulin concentration at Day 8, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Insulin Concentration at Day 8
Predose (Baseline)
32.5 pmol/L
Standard Deviation 9.85
39.3 pmol/L
Standard Deviation 22.59
34.5 pmol/L
Standard Deviation 15.83
33.8 pmol/L
Standard Deviation 12.94
Mean Serum Insulin Concentration at Day 8
1 h
302.5 pmol/L
Standard Deviation 145.61
286.8 pmol/L
Standard Deviation 179.53
225.3 pmol/L
Standard Deviation 148.93
690.5 pmol/L
Standard Deviation 342.10
Mean Serum Insulin Concentration at Day 8
2 h
337.0 pmol/L
Standard Deviation 110.23
225.7 pmol/L
Standard Deviation 101.02
229.8 pmol/L
Standard Deviation 79.00
238.3 pmol/L
Standard Deviation 92.34
Mean Serum Insulin Concentration at Day 8
4 h
63.0 pmol/L
Standard Deviation 86.69
63.3 pmol/L
Standard Deviation 83.32
36.8 pmol/L
Standard Deviation 21.17
21.7 pmol/L
Standard Deviation 19.97

SECONDARY outcome

Timeframe: Mean serum insulin concentration at Day 120, before and up to 4 hours after intake of a high-glucose solution

Population: OD=once daily; BID=twice daily.

Oral glucose tolerance test: mean serum insulin concentration at Day 120, before and up to 4 hours after intake of a high-glucose solution, in subjects receiving repeated doses of emodepside or placebo for 10 days (Days 0-9). Baseline=pre-glucose intake on each respective day. Note: At Day 120, serum glucose concentration was only measured in Cohort 3 (10 mg BID)

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
6 subjects with matching placebo (2 subjects per dose group)
Mean Serum Insulin Concentration at Day 120
0 h (Baseline)
28.0 pmol/L
Standard Deviation 13.74
Mean Serum Insulin Concentration at Day 120
1 h
417.8 pmol/L
Standard Deviation 379.72
Mean Serum Insulin Concentration at Day 120
2 h
152.8 pmol/L
Standard Deviation 114.92
Mean Serum Insulin Concentration at Day 120
4 h
18.8 pmol/L
Standard Deviation 11.39

OTHER_PRE_SPECIFIED outcome

Timeframe: Drug-related AEs were reported throughout the study

Population: OD=once daily; BID=twice daily.

Subjects presenting drug-related treatment-emergent adverse events listed by preferred term. Note: subjects with ≥1 adverse event are counted only once per preferred term.

Outcome measures

Outcome measures
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 Participants
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 Participants
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 Participants
6 subjects with matching placebo (2 subjects per dose group)
Drug-related Adverse Events
Visual impairment
2 Participants
1 Participants
3 Participants
1 Participants
Drug-related Adverse Events
Euphoric mood
1 Participants
1 Participants
0 Participants
0 Participants
Drug-related Adverse Events
Nervousness
1 Participants
0 Participants
0 Participants
0 Participants
Drug-related Adverse Events
Dizziness
1 Participants
0 Participants
0 Participants
0 Participants

Adverse Events

Cohort 1: 5mg EMODEPSIDE OD

Serious events: 1 serious events
Other events: 5 other events
Deaths: 0 deaths

Cohort 2: 10mg EMODEPSIDE OD

Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths

Cohort 3: 10mg EMODEPSIDE BID

Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths

Placebo Group

Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths

Serious adverse events

Serious adverse events
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 participants at risk
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 participants at risk
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 participants at risk
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 participants at risk
6 subjects with matching placebo (2 subjects per dose group)
Gastrointestinal disorders
Anal fistula
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Infections and infestations
Anal abscess
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).

Other adverse events

Other adverse events
Measure
Cohort 1: 5mg EMODEPSIDE OD
n=6 participants at risk
6 subjects with LSF emodepside 5mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 2: 10mg EMODEPSIDE OD
n=6 participants at risk
6 subjects with LSF emodepside 10mg, OD LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Cohort 3: 10mg EMODEPSIDE BID
n=6 participants at risk
6 subjects with LSF emodepside 10mg, BID LSF emodepside (BAY 44-4400) oral solution (1mg/mL)
Placebo Group
n=6 participants at risk
6 subjects with matching placebo (2 subjects per dose group)
Surgical and medical procedures
Sebaceous cyst excision
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Immune system disorders
Allergy to animal
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
General disorders
Fatigue
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
General disorders
Influenza like illness
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
General disorders
Malaise
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
General disorders
Medical device site erythema
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Psychiatric disorders
Euphoric mood
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Psychiatric disorders
Nervousness
16.7%
1/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Injury, poisoning and procedural complications
Skin laceration
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Investigations
Hepatic enzyme increased
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Investigations
Hepatitis E antibody positive
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Nervous system disorders
Headache
16.7%
1/6 • Number of events 3 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
33.3%
2/6 • Number of events 4 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Nervous system disorders
Dizziness
33.3%
2/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Eye disorders
Visual impairment
33.3%
2/6 • Number of events 3 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
50.0%
3/6 • Number of events 3 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Eye disorders
Vision blurred
16.7%
1/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Gastrointestinal disorders
Nausea
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
33.3%
2/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Gastrointestinal disorders
Abdominal pain
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Skin and subcutaneous tissue disorders
Acne
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Skin and subcutaneous tissue disorders
Dry skin
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Skin and subcutaneous tissue disorders
Rash
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Musculoskeletal and connective tissue disorders
Back pain
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Musculoskeletal and connective tissue disorders
Musculoskeletal chest pain
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Musculoskeletal and connective tissue disorders
Arthralgia
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Metabolism and nutrition disorders
Decreased appetite
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Infections and infestations
Nasopharyngitis
50.0%
3/6 • Number of events 3 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
50.0%
3/6 • Number of events 3 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Infections and infestations
Ear infection
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 2 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Infections and infestations
Tonsilitis
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
Infections and infestations
Urethritis
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
16.7%
1/6 • Number of events 1 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).
0.00%
0/6 • Adverse events were monitored from Screening (Day -28 and until Day -3) to Follow-up (up to Day 120 ±2 days).

Additional Information

Jean Yves Gillon

DNDi

Phone: +41.22.906.92.32

Results disclosure agreements

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