Trial Outcomes & Findings for A Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Food-Effect of KQ-791 (NCT NCT02370043)
NCT ID: NCT02370043
Last Updated: 2019-11-26
Results Overview
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
19 participants
Primary outcome timeframe
Baseline to study completion (up to 11 weeks)
Results posted on
2019-11-26
Participant Flow
Sequence 60 mg/600 mg/Placebo subject discontinued after completion of 600 mg. Sequence Placebo/600 mg/1800 mg subject discontinued after completion of placebo.
Participant milestones
| Measure |
Sequence: 15 mg/Placebo/1200 mg/Placebo (Fed)
|
Sequence: 15 mg KQ791/195 mg/Placebo/195 mg (Fed)
|
Sequence: Placebo/195 mg/1200 mg/195 mg (Fed)
|
Sequence: 60 mg/Placebo/1800 mg
|
Sequence: 60 mg/600 mg/Placebo
|
Sequence: Placebo/600 mg/1800 mg
|
|---|---|---|---|---|---|---|
|
Overall Study
STARTED
|
3
|
3
|
3
|
3
|
3
|
4
|
|
Overall Study
COMPLETED
|
3
|
3
|
3
|
3
|
2
|
3
|
|
Overall Study
NOT COMPLETED
|
0
|
0
|
0
|
0
|
1
|
1
|
Reasons for withdrawal
| Measure |
Sequence: 15 mg/Placebo/1200 mg/Placebo (Fed)
|
Sequence: 15 mg KQ791/195 mg/Placebo/195 mg (Fed)
|
Sequence: Placebo/195 mg/1200 mg/195 mg (Fed)
|
Sequence: 60 mg/Placebo/1800 mg
|
Sequence: 60 mg/600 mg/Placebo
|
Sequence: Placebo/600 mg/1800 mg
|
|---|---|---|---|---|---|---|
|
Overall Study
Withdrawal by Subject
|
0
|
0
|
0
|
0
|
1
|
1
|
Baseline Characteristics
A Study to Evaluate the Safety, Tolerability, Pharmacokinetics and Food-Effect of KQ-791
Baseline characteristics by cohort
| Measure |
Overall Study
n=19 Participants
|
|---|---|
|
Age, Continuous
|
48.1 years
STANDARD_DEVIATION 8.8 • n=93 Participants
|
|
Sex: Female, Male
Female
|
2 Participants
n=93 Participants
|
|
Sex: Female, Male
Male
|
17 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Hispanic or Latino
|
6 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Not Hispanic or Latino
|
13 Participants
n=93 Participants
|
|
Ethnicity (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
American Indian or Alaska Native
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Asian
|
1 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Native Hawaiian or Other Pacific Islander
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Black or African American
|
1 Participants
n=93 Participants
|
|
Race (NIH/OMB)
White
|
17 Participants
n=93 Participants
|
|
Race (NIH/OMB)
More than one race
|
0 Participants
n=93 Participants
|
|
Race (NIH/OMB)
Unknown or Not Reported
|
0 Participants
n=93 Participants
|
|
Region of Enrollment
Canada
|
19 participants
n=93 Participants
|
PRIMARY outcome
Timeframe: Baseline to study completion (up to 11 weeks)Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
n=3 Participants
|
Placebo (Fasting)
n=17 Participants
|
|---|---|---|---|---|---|---|---|---|---|
|
Number of Participants With One or More Serious Adverse Events (SAEs) Considered by the Investigator to be Related to Study Drug
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
0 participants
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute AUC0-t.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Area Under the Plasma Concentration-Time Curve From Time Zero to the Last Non-Zero Concentration (AUC0-t)
|
2137673.75 h*ng/mL
Geometric Coefficient of Variation 34.74
|
34699.23 h*ng/mL
Geometric Coefficient of Variation 44.87
|
95223.95 h*ng/mL
Geometric Coefficient of Variation 32.54
|
358380.52 h*ng/mL
Geometric Coefficient of Variation 36.34
|
110566.98 h*ng/mL
Geometric Coefficient of Variation 17.39
|
721393.21 h*ng/mL
Geometric Coefficient of Variation 32.49
|
1207610.37 h*ng/mL
Geometric Coefficient of Variation 29.83
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, and 24 hours post-dosePopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute AUC0-24.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Area Under the Concentration-Time Curve From Time Zero to 24-hour Post-Dose (AUC0-24)
|
178100.82 h*ng/mL
Geometric Coefficient of Variation 44.64
|
3410.02 h*ng/mL
Geometric Coefficient of Variation 55.50
|
12251.48 h*ng/mL
Geometric Coefficient of Variation 25.11
|
33151.96 h*ng/mL
Geometric Coefficient of Variation 34.63
|
16718.65 h*ng/mL
Geometric Coefficient of Variation 17.76
|
60448.26 h*ng/mL
Geometric Coefficient of Variation 46.92
|
113891.92 h*ng/mL
Geometric Coefficient of Variation 24.54
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mg'Population: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute AUC0-inf.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=5 Participants
|
60 mg KQ-791 (Fasting)
n=3 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=2 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Area Under the Concentration-Time Curve From Time Zero to Infinity (AUC0-inf)
|
2176168.42 h*ng/mL
Geometric Coefficient of Variation 34.65
|
40581.44 h*ng/mL
Geometric Coefficient of Variation 51.90
|
128600.49 h*ng/mL
Geometric Coefficient of Variation 37.47
|
387934.16 h*ng/mL
Geometric Coefficient of Variation 31.98
|
120230.35 h*ng/mL
Geometric Coefficient of Variation 9.81
|
776014.78 h*ng/mL
Geometric Coefficient of Variation 37.64
|
1311488.40 h*ng/mL
Geometric Coefficient of Variation 29.23
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Cmax.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Maximum Observed Drug Concentration (Cmax)
|
9418.01 ng/mL
Geometric Coefficient of Variation 44.09
|
188.65 ng/mL
Geometric Coefficient of Variation 65.96
|
637.51 ng/mL
Geometric Coefficient of Variation 29.32
|
1857.08 ng/mL
Geometric Coefficient of Variation 45.29
|
923.51 ng/mL
Geometric Coefficient of Variation 20.32
|
3238.86 ng/mL
Geometric Coefficient of Variation 52.73
|
5828.97 ng/mL
Geometric Coefficient of Variation 32.07
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Residual Area.
calculated as 100\*(1- AUC0-t / AUC0-inf)
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=5 Participants
|
60 mg KQ-791 (Fasting)
n=3 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=2 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Residual Area
|
1.55 Percentage residual area under the AUC
Geometric Coefficient of Variation 47.64
|
4.59 Percentage residual area under the AUC
Geometric Coefficient of Variation 107.28
|
11.51 Percentage residual area under the AUC
Geometric Coefficient of Variation 45.28
|
3.58 Percentage residual area under the AUC
Geometric Coefficient of Variation 113.37
|
13.23 Percentage residual area under the AUC
Geometric Coefficient of Variation 50.26
|
4.25 Percentage residual area under the AUC
Geometric Coefficient of Variation 88.29
|
4.53 Percentage residual area under the AUC
Geometric Coefficient of Variation 84.07
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levelsPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Tmax.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Time to Observed Cmax (Tmax)
|
7.06 Hours
Interval 4.0 to 8.0
|
4 Hours
Interval 2.0 to 7.99
|
5 Hours
Interval 4.0 to 8.0
|
4 Hours
Interval 3.99 to 48.0
|
8 Hours
Interval 6.0 to 10.0
|
5.01 Hours
Interval 4.0 to 8.0
|
8 Hours
Interval 4.0 to 10.0
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute T1/2 el.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=5 Participants
|
60 mg KQ-791 (Fasting)
n=3 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=2 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Elimination Half-Life (T1/2 el)
|
215.58 Hours
Geometric Coefficient of Variation 12.61
|
200.67 Hours
Geometric Coefficient of Variation 16.89
|
196.45 Hours
Geometric Coefficient of Variation 17.67
|
214.42 Hours
Geometric Coefficient of Variation 28.77
|
76.86 Hours
Geometric Coefficient of Variation 22.80
|
219.71 Hours
Geometric Coefficient of Variation 7.83
|
197.77 Hours
Geometric Coefficient of Variation 24.28
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Kel.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=5 Participants
|
60 mg KQ-791 (Fasting)
n=3 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=2 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Elimination Rate Constant (Kel)
|
0.0032 Per hour
Geometric Coefficient of Variation 14.2298
|
0.0035 Per hour
Geometric Coefficient of Variation 18.9823
|
0.0035 Per hour
Geometric Coefficient of Variation 16.0482
|
0.0032 Per hour
Geometric Coefficient of Variation 32.1756
|
0.0090 Per hour
Geometric Coefficient of Variation 22.8030
|
0.0032 Per hour
Geometric Coefficient of Variation 7.9026
|
0.0035 Per hour
Geometric Coefficient of Variation 28.6322
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute CI/F.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=5 Participants
|
60 mg KQ-791 (Fasting)
n=3 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=2 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Apparent Body Clearance (Cl/F)
|
0.8271 Liters per hour (L/h)
Geometric Coefficient of Variation 40.4976
|
0.3696 Liters per hour (L/h)
Geometric Coefficient of Variation 48.4762
|
0.4666 Liters per hour (L/h)
Geometric Coefficient of Variation 43.0267
|
0.5027 Liters per hour (L/h)
Geometric Coefficient of Variation 32.8329
|
1.6219 Liters per hour (L/h)
Geometric Coefficient of Variation 9.8091
|
0.7732 Liters per hour (L/h)
Geometric Coefficient of Variation 47.0999
|
0.9150 Liters per hour (L/h)
Geometric Coefficient of Variation 37.9245
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Vd/F.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=5 Participants
|
60 mg KQ-791 (Fasting)
n=3 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=2 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Apparent Volume of Distribution (Vd/F)
|
257.25 Liters
Geometric Coefficient of Variation 29.61
|
107.01 Liters
Geometric Coefficient of Variation 34.95
|
132.23 Liters
Geometric Coefficient of Variation 32.37
|
155.49 Liters
Geometric Coefficient of Variation 27.72
|
179.83 Liters
Geometric Coefficient of Variation 13.14
|
245.08 Liters
Geometric Coefficient of Variation 46.56
|
261.06 Liters
Geometric Coefficient of Variation 18.01
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgPopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute AUC0-inf in Fed versus Fasting State.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
|
15 mg KQ-791 (Fasting)
n=2 Participants
|
60 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fed)
|
600 mg KQ-791 (Fasting)
|
1200 mg KQ-791 (Fasting)
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Area Under the Concentration-time Curve From Time Zero to Infinity (AUC0-inf) in Fed Versus Fasting State
|
—
|
0.32 h*ng/mL
Geometric Coefficient of Variation 15.17
|
—
|
—
|
—
|
—
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgOutcome measures
| Measure |
1800 mg Kq-791 (Fasting)
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fed)
|
600 mg KQ-791 (Fasting)
|
1200 mg KQ-791 (Fasting)
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Area Under the Concentration-time Curve From Time Zero to the Last Non-Zero Concentration (AUC0-t) in Fed Versus Fasting State
|
—
|
0.31 h*ng/mL
Geometric Coefficient of Variation 37.61
|
—
|
—
|
—
|
—
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levels, and on Day 28 for dose level 195 mg; on Days 14 and 28 for dose level 600 mg; and on Days 14, 28, and 56 for dose level 1800 mgOutcome measures
| Measure |
1800 mg Kq-791 (Fasting)
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fed)
|
600 mg KQ-791 (Fasting)
|
1200 mg KQ-791 (Fasting)
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Maximum Observed Drug Concentration (Cmax) in Fed Versus Fasting State
|
—
|
0.50 ng/mL
Geometric Coefficient of Variation 59.94
|
—
|
—
|
—
|
—
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Pre-dose and 0.5, 1, 2, 4, 6, 8,10, 24, 48, 96, and 144 hours post-dose, and on Day 10 for all dose levelsOutcome measures
| Measure |
1800 mg Kq-791 (Fasting)
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fasting)
|
195 mg KQ-791 (Fed)
|
600 mg KQ-791 (Fasting)
|
1200 mg KQ-791 (Fasting)
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Time to Maximum Drug Concentration (Tmax) in Fed Versus Fasting State
|
—
|
3 Hours
Interval -40.01 to 5.99
|
—
|
—
|
—
|
—
|
—
|
—
|
—
|
SECONDARY outcome
Timeframe: Four hour intervals up to 12 hours, and then 12-24 hours post dosePopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute the Amount of Drug Excreted in Urine.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=5 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Amount of Drug Excreted in Urine
|
3069.11 μg
Geometric Coefficient of Variation 37.08
|
37.72 μg
Geometric Coefficient of Variation 27.71
|
155.51 μg
Geometric Coefficient of Variation 15.81
|
381.35 μg
Geometric Coefficient of Variation 34.71
|
224.51 μg
Geometric Coefficient of Variation 31.25
|
739.07 μg
Geometric Coefficient of Variation 67.68
|
1796.43 μg
Geometric Coefficient of Variation 29.85
|
—
|
—
|
SECONDARY outcome
Timeframe: Four hour intervals up to 12 hours, and then 12-24 hours post dosePopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Ae0-t.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=5 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Cumulative Urinary Excretion From Time Zero to Time t (Ae0-t)
|
6680.04 μg
Geometric Coefficient of Variation 38.34
|
90.60 μg
Geometric Coefficient of Variation 37.17
|
350.68 μg
Geometric Coefficient of Variation 19.39
|
859.41 μg
Geometric Coefficient of Variation 39.32
|
421.70 μg
Geometric Coefficient of Variation 27.23
|
1893.11 μg
Geometric Coefficient of Variation 57.89
|
3793.47 μg
Geometric Coefficient of Variation 34.98
|
—
|
—
|
SECONDARY outcome
Timeframe: Four hour intervals up to 12 hours, and then 12-24 hours post dosePopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Rmax.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Maximum Rate of Urinary Excretion (Rmax)
|
377.72 μg/hour
Geometric Coefficient of Variation 38.11
|
5.13 μg/hour
Geometric Coefficient of Variation 44.88
|
21.09 μg/hour
Geometric Coefficient of Variation 29.33
|
49.05 μg/hour
Geometric Coefficient of Variation 39.75
|
25.53 μg/hour
Geometric Coefficient of Variation 29.88
|
123.11 μg/hour
Geometric Coefficient of Variation 48.42
|
206.83 μg/hour
Geometric Coefficient of Variation 33.25
|
—
|
—
|
SECONDARY outcome
Timeframe: Four hour intervals up to 12 hours, and then 12-24 hours post dosePopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute TRmax.
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=6 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Time of Rmax Urinary Excretion (TRmax)
|
5.96 Hours
Interval 5.89 to 9.94
|
5.93 Hours
Interval 5.91 to 5.94
|
5.93 Hours
Interval 5.9 to 9.91
|
5.91 Hours
Interval 5.87 to 9.9
|
9.88 Hours
Interval 5.85 to 9.91
|
5.88 Hours
Interval 5.86 to 5.9
|
9.90 Hours
Interval 5.84 to 9.96
|
—
|
—
|
SECONDARY outcome
Timeframe: Four hour intervals up to 12 hours, and then 12-24 hours post dosePopulation: All randomized participants who received at least 1 dose of KQ-791and had sufficient evaluable PK data to compute Clr.
Calculated by the following equation: Ae0-t/AUC0-24
Outcome measures
| Measure |
1800 mg Kq-791 (Fasting)
n=6 Participants
|
15 mg KQ-791 (Fasting)
n=6 Participants
|
60 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fasting)
n=6 Participants
|
195 mg KQ-791 (Fed)
n=6 Participants
|
600 mg KQ-791 (Fasting)
n=6 Participants
|
1200 mg KQ-791 (Fasting)
n=5 Participants
|
Placebo (Fed)
|
Placebo (Fasting)
|
|---|---|---|---|---|---|---|---|---|---|
|
Renal Clearance (Clr)
|
0.0375 Liters per hour
Geometric Coefficient of Variation 9.5596
|
0.0266 Liters per hour
Geometric Coefficient of Variation 31.5426
|
0.0286 Liters per hour
Geometric Coefficient of Variation 19.7181
|
0.0259 Liters per hour
Geometric Coefficient of Variation 19.7678
|
0.0252 Liters per hour
Geometric Coefficient of Variation 20.7044
|
0.0313 Liters per hour
Geometric Coefficient of Variation 17.2647
|
0.0333 Liters per hour
Geometric Coefficient of Variation 18.6140
|
—
|
—
|
Adverse Events
15 mg KQ-791 (Fasting)
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
60 mg KQ-791 (Fasting)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
195 mg KQ-791 (Fasting)
Serious events: 0 serious events
Other events: 3 other events
Deaths: 0 deaths
195 mg KQ-791 (Fed)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
600 mg KQ-791 (Fasting)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
1200 mg KQ-791 (Fasting)
Serious events: 0 serious events
Other events: 2 other events
Deaths: 0 deaths
1800 mg Kq-791 (Fasting)
Serious events: 0 serious events
Other events: 4 other events
Deaths: 0 deaths
Placebo (Fasting)
Serious events: 0 serious events
Other events: 8 other events
Deaths: 0 deaths
Placebo (Fed)
Serious events: 0 serious events
Other events: 1 other events
Deaths: 0 deaths
Serious adverse events
Adverse event data not reported
Other adverse events
| Measure |
15 mg KQ-791 (Fasting)
n=6 participants at risk
|
60 mg KQ-791 (Fasting)
n=6 participants at risk
|
195 mg KQ-791 (Fasting)
n=6 participants at risk
|
195 mg KQ-791 (Fed)
n=6 participants at risk
|
600 mg KQ-791 (Fasting)
n=6 participants at risk
|
1200 mg KQ-791 (Fasting)
n=6 participants at risk
|
1800 mg Kq-791 (Fasting)
n=6 participants at risk
|
Placebo (Fasting)
n=17 participants at risk
|
Placebo (Fed)
n=3 participants at risk
|
|---|---|---|---|---|---|---|---|---|---|
|
Gastrointestinal disorders
Diarrhoea
|
33.3%
2/6 • Number of events 2
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Constipation
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Faeces discolored
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
33.3%
2/6 • Number of events 2
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Abdominal discomfort
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Abdominal distension
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Abdominal pain
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Abnormal faeces
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Dyspepsia
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Gastrointestinal disorders
Gastresophageal reflux disease
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Nervous system disorders
Somnolence
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
33.3%
2/6 • Number of events 2
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
33.3%
1/3 • Number of events 1
Collected at each visit
|
|
Nervous system disorders
Headache
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Nervous system disorders
Presyncope
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 3
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Nervous system disorders
Dysgeusia
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Nervous system disorders
Syncope
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Investigations
Blood tryglycerides increased
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
33.3%
2/6 • Number of events 2
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
11.8%
2/17 • Number of events 2
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Nervous system disorders
Blood pressure increased
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Investigations
High density lipoprotein decreased
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Investigations
Heart Rate Increased
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Investigations
Protein urine
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Musculoskeletal and connective tissue disorders
Back Pain
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Musculoskeletal and connective tissue disorders
Arthralgia
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Musculoskeletal and connective tissue disorders
Neck Pain
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Infections and infestations
Nasopharyngitis
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Musculoskeletal and connective tissue disorders
Oral herpes
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Injury, poisoning and procedural complications
Laceration
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Injury, poisoning and procedural complications
Ligament sprain
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Injury, poisoning and procedural complications
Procedural dizziness
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
5.9%
1/17 • Number of events 1
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Eye disorders
Lacrimation increases
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
General disorders
Chills
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
|
Skin and subcutaneous tissue disorders
Rash
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
16.7%
1/6 • Number of events 1
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/6
Collected at each visit
|
0.00%
0/17
Collected at each visit
|
0.00%
0/3
Collected at each visit
|
Additional Information
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: OTHER