Trial Outcomes & Findings for Pharmacokinetic Study of Lurasidone After Multiple Oral Administration in Healthy Human Subjects (NCT NCT02174523)
NCT ID: NCT02174523
Last Updated: 2019-04-08
Results Overview
Maximum (peak) observed drug serum concentration.
Recruitment status
COMPLETED
Study phase
PHASE1
Target enrollment
14 participants
Primary outcome timeframe
pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose
Results posted on
2019-04-08
Participant Flow
Total 27 subjects were screened at the clinical site after obtaining informed consent. A total 14 subjects were enrolled into the study and were randomized to lurasidone group (10) and placebo group (4). The data of informed consent from the first subject was 8th April 2014（and that from the last subject was 15th April 2014）.
Participant milestones
| Measure |
40mg Lurasidone
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
Placebo
Single oral administration of 40 mg study drug placebo after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg placebo, once daily between Day 4 and Day 8.
|
|---|---|---|
|
Overall Study
STARTED
|
10
|
4
|
|
Overall Study
COMPLETED
|
9
|
4
|
|
Overall Study
NOT COMPLETED
|
1
|
0
|
Reasons for withdrawal
| Measure |
40mg Lurasidone
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
Placebo
Single oral administration of 40 mg study drug placebo after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg placebo, once daily between Day 4 and Day 8.
|
|---|---|---|
|
Overall Study
Withdrawal by Subject
|
1
|
0
|
Baseline Characteristics
Pharmacokinetic Study of Lurasidone After Multiple Oral Administration in Healthy Human Subjects
Baseline characteristics by cohort
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
Placebo
n=4 Participants
Single oral administration of 40 mg study drug placebo after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg placebo, once daily between Day 4 and Day 8.
|
Total
n=14 Participants
Total of all reporting groups
|
|---|---|---|---|
|
Age, Continuous
|
27.7 years
STANDARD_DEVIATION 3.74 • n=5 Participants
|
26.5 years
STANDARD_DEVIATION 5.07 • n=7 Participants
|
27.4 years
STANDARD_DEVIATION 3.99 • n=5 Participants
|
|
Sex: Female, Male
Female
|
0 Participants
n=5 Participants
|
0 Participants
n=7 Participants
|
0 Participants
n=5 Participants
|
|
Sex: Female, Male
Male
|
10 Participants
n=5 Participants
|
4 Participants
n=7 Participants
|
14 Participants
n=5 Participants
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Maximum (peak) observed drug serum concentration.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone Cmax
|
50.2 ng/mL
Geometric Coefficient of Variation 44.3
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone AUC 0-24
|
152 ng･h/mL
Geometric Coefficient of Variation 33.2
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone AUC 0-τ
|
166 ng･h/mL
Geometric Coefficient of Variation 32.4
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone AUC0-∞
|
179 ng･h/mL
Standard Deviation 29.9
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone Tmax
|
1.50 h
Interval 1.0 to 4.0
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone λz
|
0.0360 1/h
Geometric Coefficient of Variation 20.8
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone t1/2
|
19.3 h
Geometric Coefficient of Variation 20.8
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone MRT
|
12.2 h
Geometric Coefficient of Variation 22.7
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone CL/F
|
223 L/h
Geometric Coefficient of Variation 29.9
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
CLss/F
|
211 L/h
Geometric Coefficient of Variation 27.9
|
PRIMARY outcome
Timeframe: pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dosePopulation: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone Vz/F
|
6198 L
Geometric Coefficient of Variation 47.9
|
PRIMARY outcome
Timeframe: Day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone Vzss/F
|
10618 L
Geometric Coefficient of Variation 38.6
|
PRIMARY outcome
Timeframe: Day 8/Day 1Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,
Ratio of Cmax
|
0.94 Ratios
Interval 0.75 to 1.18
|
|
Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,
Ratio of AUC0-∞
|
1.74 Ratios
Interval 1.59 to 1.9
|
|
Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,
Ratio of AUC0-τ
|
1.25 Ratios
Interval 1.14 to 1.36
|
|
Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,
Ratio of Cτ
|
2.52 Ratios
Interval 2.37 to 2.68
|
PRIMARY outcome
Timeframe: Pre-dose (-0.5h) of Day4 and Day5Outcome measures
| Measure |
40mg Lurasidone
n=10 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 4 and Day 5
Day4 Pre-dose (-0.5h)
|
0.277 ng/ml
Geometric Coefficient of Variation 31.5
|
|
Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 4 and Day 5
Day5Pre-dose (-0.5h)
|
1.15 ng/ml
Geometric Coefficient of Variation 28.7
|
PRIMARY outcome
Timeframe: Pre-dose (-0.5h) of Day6 and Day7Outcome measures
| Measure |
40mg Lurasidone
n=9 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 6 and Day 7
Day6 Pre-dose (-0.5h)
|
1.56 ng/ml
Geometric Coefficient of Variation 27.1
|
|
Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 6 and Day 7
Day7 Pre-dose (-0.5h)
|
2.00 ng/ml
Geometric Coefficient of Variation 27.3
|
PRIMARY outcome
Timeframe: Day8Maximum (peak) observed drug serum concentration.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone Cmax
|
48.5 ng/mL
Geometric Coefficient of Variation 49.4
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone AUC 0-24
|
190 ng･h/mL
Geometric Coefficient of Variation 27.9
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone AUC 0-τ
|
234 ng･h/mL
Geometric Coefficient of Variation 27.4
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone AUC0-∞
|
314 ng･h/mL
Geometric Coefficient of Variation 26.6
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone Tmax
|
1.75 h
Interval 1.0 to 4.0
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone λz
|
0.0199 1/h
Geometric Coefficient of Variation 20.2
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone t1/2
|
34.9 h
Geometric Coefficient of Variation 20.2
|
PRIMARY outcome
Timeframe: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8Population: All subjects with evaluable PK data were included in PK data analysis.
Outcome measures
| Measure |
40mg Lurasidone
n=8 Participants
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
|---|---|
|
Lurasidone MRT
|
22.0 h
Geometric Coefficient of Variation 19
|
Adverse Events
40mg Lurasidone
Serious events: 0 serious events
Other events: 10 other events
Deaths: 0 deaths
Placebo
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 |
40mg Lurasidone
n=10 participants at risk
Single oral administration of 40 mg study drug lurasidone after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg study drug lurasidone, once daily between Day 4 and Day 8.
|
Placebo
n=4 participants at risk
Single oral administration of 40 mg study drug placebo after the over 350 kcal breakfast on Day 1. Administration was suspended on Days 2 and 3. Continuous oral administration of 40 mg placebo, once daily between Day 4 and Day 8.
|
|---|---|---|
|
Gastrointestinal disorders
Diarrhoea
|
10.0%
1/10 • Number of events 1
|
0.00%
0/4
|
|
Gastrointestinal disorders
Dyspepsia
|
10.0%
1/10 • Number of events 1
|
0.00%
0/4
|
|
Gastrointestinal disorders
Nausea
|
10.0%
1/10 • Number of events 1
|
0.00%
0/4
|
|
Investigations
Blood prolactin increased
|
60.0%
6/10 • Number of events 6
|
25.0%
1/4 • Number of events 1
|
|
Investigations
Blood bilirubin increased
|
20.0%
2/10 • Number of events 2
|
0.00%
0/4
|
|
Nervous system disorders
Somnolence
|
100.0%
10/10 • Number of events 10
|
0.00%
0/4
|
|
Nervous system disorders
Dizziness
|
40.0%
4/10 • Number of events 4
|
25.0%
1/4 • Number of events 1
|
|
Psychiatric disorders
Restlessness
|
60.0%
6/10 • Number of events 6
|
0.00%
0/4
|
Additional Information
Dr.Hu Chaoying
Phase I Clinical Research Unit , Shanghai Xuihui Central Hospital
Phone: 021-54036058
Email: [email protected]
Results disclosure agreements
- Principal investigator is a sponsor employee
- Publication restrictions are in place
Restriction type: OTHER