Trial Outcomes & Findings for A Study Investigating the Absolute Oral Bioavailability of Balovaptan After Single and Multiple Daily Oral Doses of Balovaptan in Healthy Volunteers (NCT NCT03764449)
NCT ID: NCT03764449
Last Updated: 2020-02-24
Results Overview
Absolute oral bioavailability of a single dose A of balovaptan.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
16 participants
Primary outcome timeframe
Day 1 of Period 1 (Period 1 is 14 days).
Results posted on
2020-02-24
Participant Flow
The study was conducted at 1 site in the Netherlands.
Participants in this study included healthy volunteers.
Participant milestones
| Measure |
Cohort 1
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|
|
Overall Study
STARTED
|
8
|
8
|
|
Overall Study
COMPLETED
|
8
|
8
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
Reasons for withdrawal
Withdrawal data not reported
Baseline Characteristics
A Study Investigating the Absolute Oral Bioavailability of Balovaptan After Single and Multiple Daily Oral Doses of Balovaptan in Healthy Volunteers
Baseline characteristics by cohort
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Total
n=16 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
41.4 Years
STANDARD_DEVIATION 16.18 • n=5 Participants
|
33.5 Years
STANDARD_DEVIATION 13.24 • n=7 Participants
|
37.4 Years
STANDARD_DEVIATION 14.85 • n=5 Participants
|
|
Sex: Female, Male
Female
|
2 Participants
n=5 Participants
|
2 Participants
n=7 Participants
|
4 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
6 Participants
n=5 Participants
|
6 Participants
n=7 Participants
|
12 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
0 Participants
n=5 Participants
|
2 Participants
n=7 Participants
|
2 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
8 Participants
n=5 Participants
|
6 Participants
n=7 Participants
|
14 Participants
n=5 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Asian
|
1 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Black or African American
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Race (NIH/OMB)
White
|
6 Participants
n=5 Participants
|
8 Participants
n=7 Participants
|
14 Participants
n=5 Participants
|
|
Race (NIH/OMB)
More than one race
|
1 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
1 Participants
n=5 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Absolute oral bioavailability of a single dose A of balovaptan.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Absolute Bioavailability of Oral Balovaptan at Dose Level A (Cohort 1)
|
100.6 Percentage
Geometric Coefficient of Variation 31.4
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Absolute oral bioavailability of a single dose B balovaptan.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Absolute Bioavailability of Oral Balovaptan at Dose Level B (Cohort 2)
|
108.2 Percentage
Geometric Coefficient of Variation 5.9
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 14 of Period 2 (Period 2 is 19 days).Population: PK analysis consisted of all receiving at least 1 dose balovaptan.Participants excluded from analysis, if significantly violated inclusion/exclusion criteria, deviated significantly from protocol, or if data unavailable/incomplete.There were 2 outliers;sensitivity analysis excluding those 2,resulted in similar bioavailability across all treatments.
Absolute oral bioavailability of balovaptan after once daily doses of Dose A and Dose B for 14 days.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Absolute Bioavailability of Oral Balovaptan at Dose A and Dose B
|
82.3 Percentage
Geometric Coefficient of Variation 72.4
|
103.1 Percentage
Geometric Coefficient of Variation 4.1
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Maximum Plasma Concentration (Cmax) of IV Balovaptan
Day 1 of Period 1
|
688 pg/mL
Geometric Coefficient of Variation 30.5
|
1601 pg/mL
Geometric Coefficient of Variation 28.2
|
—
|
—
|
|
Maximum Plasma Concentration (Cmax) of IV Balovaptan
Day 14 of Period 2
|
1591 pg/mL
Geometric Coefficient of Variation 115.8
|
1974 pg/mL
Geometric Coefficient of Variation 37.9
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Cmax of Oral Balovaptan
Day 1 of Period 1
|
36.9 ng/mL
Geometric Coefficient of Variation 36.8
|
443 ng/mL
Geometric Coefficient of Variation 15.2
|
—
|
—
|
|
Cmax of Oral Balovaptan
Day 14 of Period 2
|
108 ng/mL
Geometric Coefficient of Variation 20.4
|
643 ng/mL
Geometric Coefficient of Variation 25.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Cmax of M2 Metabolites
Day 1 of Period 1
|
3.87 ng/mL
Geometric Coefficient of Variation 62.1
|
23.6 ng/mL
Geometric Coefficient of Variation 38.1
|
—
|
—
|
|
Cmax of M2 Metabolites
Day 14 of Period 2
|
20.3 ng/mL
Geometric Coefficient of Variation 65.8
|
105 ng/mL
Geometric Coefficient of Variation 29.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Cmax of M3 Metabolites
Day 1 of Period 1
|
6.18 ng/mL
Geometric Coefficient of Variation 28.6
|
57.9 ng/mL
Geometric Coefficient of Variation 30.3
|
—
|
—
|
|
Cmax of M3 Metabolites
Day 14 of Period 2
|
57.2 ng/mL
Geometric Coefficient of Variation 18.8
|
260 ng/mL
Geometric Coefficient of Variation 26.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all partcipants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Time to Maximum Observed Plasma Concentration (Tmax) of IV Balovaptan
Day 1 of Period 1
|
0.25 Hour
Interval 0.1 to 0.25
|
0.25 Hour
Interval 0.25 to 0.25
|
—
|
—
|
|
Time to Maximum Observed Plasma Concentration (Tmax) of IV Balovaptan
Day 14 of Period 2
|
0.25 Hour
Interval 0.25 to 14.8
|
0.25 Hour
Interval 0.25 to 1.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Tmax of Oral Balovaptan
Day 1 of Period 1
|
1.23 Hour
Interval 0.5 to 1.35
|
1.00 Hour
Interval 1.0 to 1.33
|
—
|
—
|
|
Tmax of Oral Balovaptan
Day 14 of Period 2
|
1.28 Hour
Interval 0.5 to 1.75
|
1.11 Hour
Interval 0.5 to 1.75
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Tmax of M2 Metabolites
Day 1 of Period 1
|
24.0 Hour
Interval 24.0 to 48.0
|
24.0 Hour
Interval 16.0 to 24.1
|
—
|
—
|
|
Tmax of M2 Metabolites
Day 14 of Period 2
|
4.50 Hour
Interval 1.22 to 12.0
|
3.38 Hour
Interval 1.22 to 6.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Tmax of M3 Metabolites
Day 1 of Period 1
|
48.0 Hour
Interval 16.0 to 60.0
|
12.0 Hour
Interval 4.5 to 24.1
|
—
|
—
|
|
Tmax of M3 Metabolites
Day 14 of Period 2
|
2.13 Hour
Interval 1.0 to 4.5
|
1.88 Hour
Interval 1.22 to 4.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Apparent Terminal Half-Life (t1/2) of IV Balovaptan
Day 1 of Period 1
|
35.2 Hour
Geometric Coefficient of Variation 23.7
|
19.5 Hour
Geometric Coefficient of Variation 34.0
|
—
|
—
|
|
Apparent Terminal Half-Life (t1/2) of IV Balovaptan
Day 14 of Period 2
|
27.7 Hour
Geometric Coefficient of Variation 18.3
|
15.7 Hour
Geometric Coefficient of Variation 28.2
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
T1/2 of Oral Balovaptan
Day 1 of Period 1
|
38.8 Hour
Geometric Coefficient of Variation 25.9
|
29.1 Hour
Geometric Coefficient of Variation 28.7
|
—
|
—
|
|
T1/2 of Oral Balovaptan
Day 14 of Period 2
|
31.2 Hour
Geometric Coefficient of Variation 15.6
|
22.7 Hour
Geometric Coefficient of Variation 15.7
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
T1/2 of M2 Metabolites
Day 1 of Period 1
|
48.5 Hour
Geometric Coefficient of Variation 36.7
|
35.7 Hour
Geometric Coefficient of Variation 27.2
|
—
|
—
|
|
T1/2 of M2 Metabolites
Day 14 of Period 2
|
36.3 Hour
Geometric Coefficient of Variation 25.0
|
28.5 Hour
Geometric Coefficient of Variation 13.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
T1/2 of M3 Metabolites
Day 1 of Period 1
|
93.0 Hour
Geometric Coefficient of Variation 18.5
|
68.2 Hour
Geometric Coefficient of Variation 29.8
|
—
|
—
|
|
T1/2 of M3 Metabolites
Day 14 of Period 2
|
60.3 Hour
Geometric Coefficient of Variation 29.1
|
33.7 Hour
Geometric Coefficient of Variation 11.2
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days)Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Measurable Plasma Concentration Time Point (AUC0-last) of IV Balovaptan
|
8087 h*pg/mL
Geometric Coefficient of Variation 35.5
|
9372 h*pg/mL
Geometric Coefficient of Variation 19.3
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days)Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-last of Oral Balovaptan
|
937 h*ng/mL
Geometric Coefficient of Variation 25.6
|
5497 h*ng/mL
Geometric Coefficient of Variation 23.9
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days)Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-last of M2 Metabolites
|
297 h*ng/mL
Geometric Coefficient of Variation 72.0
|
1751 h*ng/mL
Geometric Coefficient of Variation 37.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days)Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-last of M3 Metabolites
|
754 h*ng/mL
Geometric Coefficient of Variation 24.3
|
3908 h*ng/mL
Geometric Coefficient of Variation 24.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of IV Balovaptan
Day 1 of Period 1
|
8929 h*pg/mL
Geometric Coefficient of Variation 34.0
|
9569 h*pg/mL
Geometric Coefficient of Variation 19.8
|
—
|
—
|
|
Area Under the Plasma Concentration-Time Curve From Time Zero Extrapolated to Infinity (AUC0-inf) of IV Balovaptan
Day 14 of Period 2
|
15492 h*pg/mL
Geometric Coefficient of Variation 71.5
|
10430 h*pg/mL
Geometric Coefficient of Variation 27.9
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-inf of Oral Balovaptan
|
1008 h*ng/mL
Geometric Coefficient of Variation 24.4
|
5550 h*ng/mL
Geometric Coefficient of Variation 23.9
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-inf of M2 Metabolites
|
520 h*ng/mL
Geometric Coefficient of Variation 55.1
|
1819 h*ng/mL
Geometric Coefficient of Variation 36.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-inf of M3 Metabolites
|
1122 h*ng/mL
Geometric Coefficient of Variation 14.8
|
4221 h*ng/mL
Geometric Coefficient of Variation 27.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Area Under the Plasma Concentration-Time Curve Over the Dosing Interval at Steady State (AUC0-24) of IV Balovaptan
Day 1 of Period 1
|
4400 h*pg/mL
Geometric Coefficient of Variation 42.8
|
6690 h*pg/mL
Geometric Coefficient of Variation 13.9
|
—
|
—
|
|
Area Under the Plasma Concentration-Time Curve Over the Dosing Interval at Steady State (AUC0-24) of IV Balovaptan
Day 14 of Period 2
|
9898 h*pg/mL
Geometric Coefficient of Variation 89.0
|
7908 h*pg/mL
Geometric Coefficient of Variation 19.4
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-24 of Oral Balovaptan
Day 1 of Period 1
|
458 h*ng/mL
Geometric Coefficient of Variation 22.3
|
3632 h*ng/mL
Geometric Coefficient of Variation 15.6
|
—
|
—
|
|
AUC0-24 of Oral Balovaptan
Day 14 of Period 2
|
1322 h*ng/mL
Geometric Coefficient of Variation 19.3
|
5505 h*ng/mL
Geometric Coefficient of Variation 30.7
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-24 of M2 Metabolites
Day 1 of Period 1
|
54.7 h*ng/mL
Geometric Coefficient of Variation 73.5
|
427 h*ng/mL
Geometric Coefficient of Variation 41.1
|
—
|
—
|
|
AUC0-24 of M2 Metabolites
Day 14 of Period 2
|
404 h*ng/mL
Geometric Coefficient of Variation 64.2
|
2087 h*ng/mL
Geometric Coefficient of Variation 32.1
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
AUC0-24 of M3 Metabolites
Day 1 of Period 1
|
106 h*ng/mL
Geometric Coefficient of Variation 40.5
|
1188 h*ng/mL
Geometric Coefficient of Variation 29.2
|
—
|
—
|
|
AUC0-24 of M3 Metabolites
Day 14 of Period 2
|
1102 h*ng/mL
Geometric Coefficient of Variation 17.4
|
4727 h*ng/mL
Geometric Coefficient of Variation 28.3
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Last Measurable Plasma Concentration (Clast) of IV Balovaptan
Day 1 of Period 1
|
13.6 pg/mL
Geometric Coefficient of Variation 49.7
|
6.62 pg/mL
Geometric Coefficient of Variation 29.8
|
—
|
—
|
|
Last Measurable Plasma Concentration (Clast) of IV Balovaptan
Day 14 of Period 2
|
12.5 pg/mL
Geometric Coefficient of Variation 45.5
|
6.92 pg/mL
Geometric Coefficient of Variation 22.6
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Clast of Oral Balovaptan
Day 1 of Period 1
|
1.22 ng/mL
Geometric Coefficient of Variation 13.4
|
1.22 ng/mL
Geometric Coefficient of Variation 10.6
|
—
|
—
|
|
Clast of Oral Balovaptan
Day 14 of Period 2
|
3.51 ng/mL
Geometric Coefficient of Variation 62.2
|
3.40 ng/mL
Geometric Coefficient of Variation 88.6
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Clast of M2 Metabolites
Day 1 of Period 1
|
1.24 ng/mL
Geometric Coefficient of Variation 10.4
|
1.25 ng/mL
Geometric Coefficient of Variation 15.6
|
—
|
—
|
|
Clast of M2 Metabolites
Day 14 of Period 2
|
3.19 ng/mL
Geometric Coefficient of Variation 51.2
|
9.95 ng/mL
Geometric Coefficient of Variation 58.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Clast of M3 Metabolites
Day 1 of Period 1
|
1.43 ng/mL
Geometric Coefficient of Variation 24.4
|
2.74 ng/mL
Geometric Coefficient of Variation 55.8
|
—
|
—
|
|
Clast of M3 Metabolites
Day 14 of Period 2
|
11.9 ng/mL
Geometric Coefficient of Variation 21.3
|
17.6 ng/mL
Geometric Coefficient of Variation 64.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Time of Last Measurable Plasma Concentration (Tlast) of IV Balovaptan
Day 1 of Period 1
|
106.75 Hour
Interval 106.75 to 106.82
|
100.75 Hour
Interval 58.75 to 106.75
|
—
|
—
|
|
Time of Last Measurable Plasma Concentration (Tlast) of IV Balovaptan
Day 14 of Period 2
|
106.75 Hour
Interval 106.75 to 106.77
|
82.75 Hour
Interval 58.75 to 106.75
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Tlast of Oral Balovaptan
Day 1 of Period 1
|
132.00 Hour
Interval 108.0 to 168.05
|
156.00 Hour
Interval 96.0 to 216.03
|
—
|
—
|
|
Tlast of Oral Balovaptan
Day 14 of Period 2
|
108.00 Hour
Interval 108.0 to 108.02
|
108.00 Hour
Interval 108.0 to 108.02
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Tlast of M2 Metabolites
Day 1 of Period 1
|
120.00 Hour
Interval 72.0 to 168.32
|
168.00 Hour
Interval 144.0 to 216.0
|
—
|
—
|
|
Tlast of M2 Metabolites
Day 14 of Period 1
|
108.00 Hour
Interval 108.0 to 108.02
|
108.00 Hour
Interval 108.0 to 108.02
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Tlast of M3 Metabolites
Day 1 of Period 1
|
216.00 Hour
Interval 192.0 to 216.05
|
216.00 Hour
Interval 192.0 to 216.03
|
—
|
—
|
|
Tlast of M3 Metabolites
Day 14 of Period 2
|
108.00 Hour
Interval 108.0 to 108.02
|
108.00 Hour
Interval 108.0 to 108.02
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Terminal Elimination Rate Constant (λz) of IV Balovaptan
Day 1 of Period 1
|
0.0197 /hour
Geometric Coefficient of Variation 23.7
|
0.0356 /hour
Geometric Coefficient of Variation 34.0
|
—
|
—
|
|
Terminal Elimination Rate Constant (λz) of IV Balovaptan
Day 14 of Period 2
|
0.0250 /hour
Geometric Coefficient of Variation 18.3
|
0.0442 /hour
Geometric Coefficient of Variation 28.2
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
λz of Oral Balovaptan
Day 1 of Period 1
|
0.0179 /h
Geometric Coefficient of Variation 25.9
|
0.0239 /h
Geometric Coefficient of Variation 28.7
|
—
|
—
|
|
λz of Oral Balovaptan
Day 14 of Period 2
|
0.0222 /h
Geometric Coefficient of Variation 15.6
|
0.0306 /h
Geometric Coefficient of Variation 15.7
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
λz of M2 Metabolites
Day 1 of Period 1
|
0.0143 /hour
Geometric Coefficient of Variation 36.7
|
0.0194 /hour
Geometric Coefficient of Variation 27.2
|
—
|
—
|
|
λz of M2 Metabolites
Day 14 of Period 2
|
0.0191 /hour
Geometric Coefficient of Variation 25.0
|
0.0244 /hour
Geometric Coefficient of Variation 13.5
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
λz of M3 Metabolites
Day 1 of Period 1
|
0.0075 /hour
Geometric Coefficient of Variation 18.5
|
0.0102 /hour
Geometric Coefficient of Variation 29.8
|
—
|
—
|
|
λz of M3 Metabolites
Day 14 of Period 2
|
0.0115 /hour
Geometric Coefficient of Variation 29.1
|
0.0206 /hour
Geometric Coefficient of Variation 11.2
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Total Body Clearance (CL) of IV Balovaptan
Day 1 of Period 1
|
9.98 L/h
Geometric Coefficient of Variation 34.1
|
9.75 L/h
Geometric Coefficient of Variation 20.4
|
—
|
—
|
|
Total Body Clearance (CL) of IV Balovaptan
Day 14 of Period 2
|
6.23 L/h
Geometric Coefficient of Variation 71.4
|
9.36 L/h
Geometric Coefficient of Variation 27.1
|
—
|
—
|
SECONDARY outcome
Timeframe: Day 1 of Period 1 (Period 1 is 14 days); Day 14 of Period 2 (Period 2 is 19 days).Population: The Pharmacokinetic (PK) analysis population consisted of all participants who received at least one dose of balovaptan. Participants were excluded from the PK analysis population if they significantly violated the inclusion or exclusion criteria, deviated significantly from the protocol, or if data were unavailable or incomplete.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Volume of Distribution (Vss) of IV Balovaptan
Day 1 of Period 1
|
396 Liter
Geometric Coefficient of Variation 53.1
|
197 Liter
Geometric Coefficient of Variation 21.9
|
—
|
—
|
|
Volume of Distribution (Vss) of IV Balovaptan
Day 14 of Period 2
|
166 Liter
Geometric Coefficient of Variation 95.4
|
154 Liter
Geometric Coefficient of Variation 15.3
|
—
|
—
|
SECONDARY outcome
Timeframe: Up to 35 days from screening (sceening is up to 28 days prior to admission to the clinical research unit).Population: The safety analysis population consisted of participants who received at least one dose of balovaptan.
Outcome measures
| Measure |
Cohort 1
n=8 Participants
Participants received the study drug at dose level A in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 1
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
Cohort 2, Period 2
n=8 Participants
Participants received the study drug at dose level B in 2 periods. There was a minimum of a 14-day wash out period between Day 1 of Period 1 and Day 1 of Period 2.
|
|---|---|---|---|---|
|
Percentage of Participants With Treatment-Emergent Adverse Events
|
50 Percentage
|
75 Percentage
|
63 Percentage
|
88 Percentage
|
Adverse Events
Cohort 1 Period 1
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Cohort 1, Period 2
Serious events: 0 serious events
Other events: 6 other events
Deaths: 0 deaths
Cohort 2, Period 1
Serious events: 0 serious events
Other events: 5 other events
Deaths: 0 deaths
Cohort 2, Period 2
Serious events: 0 serious events
Other events: 7 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
Cohort 1 Period 1
n=8 participants at risk
Balovaptan was administered at dose level A as a single oral dose. IV infusion of balovaptan was administered after the balovaptan oral dose.
|
Cohort 1, Period 2
n=8 participants at risk
Balovaptan was administered at dose level A as an oral dose once daily on Day 1 to Day 14. IV infusion of balovaptan was administered after the final oral dose of balovaptan.
|
Cohort 2, Period 1
n=8 participants at risk
Balovaptan was administered as a single oral dose at dose level B. IV infusion of balovaptan was administered after the balovaptan oral dose.
|
Cohort 2, Period 2
n=8 participants at risk
Balovaptan was administered at Dose level B as an oral dose once daily on Day 1 to Day 14. IV infusion of balovaptan was administered after the final oral dose of balovaptan.
|
|---|---|---|---|---|
|
General disorders
Fatigue
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
General disorders
Infusion site pain
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Ear and labyrinth disorders
Ear congestion
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Ear and labyrinth disorders
Tinnitus
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Gastrointestinal disorders
Abdominal distension
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Gastrointestinal disorders
Abdominal pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Gastrointestinal disorders
Abdominal pain upper
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Gastrointestinal disorders
Diarrhoea
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Gastrointestinal disorders
Flatulence
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Gastrointestinal disorders
Nausea
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
General disorders
Catheter site erythema
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
General disorders
Catheter site haematoma
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
General disorders
Catheter site pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
37.5%
3/8 • Number of events 4 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
General disorders
Catheter site swelling
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
25.0%
2/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Infections and infestations
Nasopharyngitis
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Injury, poisoning and procedural complications
Procedural pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Metabolism and nutrition disorders
Decreased appetite
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Arthralgia
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Bone pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Musculoskeletal chest pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
25.0%
2/8 • Number of events 3 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Musculoskeletal pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Musculoskeletal stiffness
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Myalgia
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
|
Musculoskeletal and connective tissue disorders
Pain in extremity
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Nervous system disorders
Dizziness
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Nervous system disorders
Dysgeusia
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Nervous system disorders
Headache
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
25.0%
2/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
25.0%
2/8 • Number of events 3 • Up to 21 days postdose (15 March 2019).
|
|
Psychiatric disorders
Insomnia
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
25.0%
2/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
|
Psychiatric disorders
Mood altered
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Psychiatric disorders
Nightmare
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Renal and urinary disorders
Pollakiuria
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Respiratory, thoracic and mediastinal disorders
Epistaxis
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
25.0%
2/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Respiratory, thoracic and mediastinal disorders
Oropharyngeal pain
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
|
Skin and subcutaneous tissue disorders
Dry skin
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Skin and subcutaneous tissue disorders
Pruritus
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
|
Vascular disorders
Haematoma
|
12.5%
1/8 • Number of events 1 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
0.00%
0/8 • Up to 21 days postdose (15 March 2019).
|
12.5%
1/8 • Number of events 2 • Up to 21 days postdose (15 March 2019).
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee The Study being conducted under this Agreement is part of the Overall Study. Investigator is free to publish in reputable journals or to present at professional conferences the results of the Study, but only after the first publication or presentation that involves the Overall Study. The Sponsor may request that Confidential Information be deleted and/or the publication be postponed in order to protect the Sponsor's intellectual property rights.
- Publication restrictions are in place
Restriction type: OTHER