Trial Outcomes & Findings for A Pharmacokinetic Study of Lurasidone After Single Oral Administration in Healthy Subjects (NCT NCT02174510)

NCT ID: NCT02174510

Last Updated: 2019-01-11

Results Overview

Cmax：Maximum (peak) observed drug serum concentration.

• Recruitment status: COMPLETED
• Study phase: PHASE1
• Target enrollment: 37 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: 2019-01-11

Participant Flow

Total 72 subjects were screened at the clinical site after obtaining informed consent. The data of informed consent from the first subject was march 2014. A total of 37 subjects were enrolled into the study and were randomized to three test drug groups (8 to 20mg group, 8 to 40mg group, 12 to 80mg group), and 9 subjects received placebo.

Participant milestones

Measure	20mg Lurasidone 20mg lurasidone: single oral lurasidone.	40mg Lurasidone 40mg lurasidone: single oral lurasidone.	80mg Lurasidone 80mg lurasidone: single oral lurasidone.	Placebo Subjects administered placebo tablet at the same time with each lurasidone group.
Overall Study STARTED	8	8	12	9
Overall Study COMPLETED	8	8	12	9
Overall Study NOT COMPLETED	0	0	0	0

Reasons for withdrawal

Withdrawal data not reported

Baseline Characteristics

A Pharmacokinetic Study of Lurasidone After Single Oral Administration in Healthy Subjects

Baseline characteristics by cohort

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.	Placebo n=9 Participants Subjects administered placebo tablet at the same time with each lurasidone group.	Total n=37 Participants Total of all reporting groups
Age, Continuous	26.5 years STANDARD_DEVIATION 3.74 • n=5 Participants	25.4 years STANDARD_DEVIATION 3.07 • n=7 Participants	27.5 years STANDARD_DEVIATION 7.79 • n=5 Participants	28.4 years STANDARD_DEVIATION 4.72 • n=4 Participants	27.1 years STANDARD_DEVIATION 5.41 • n=21 Participants
Sex: Female, Male Female	0 Participants n=5 Participants	0 Participants n=7 Participants	0 Participants n=5 Participants	0 Participants n=4 Participants	0 Participants n=21 Participants
Sex: Female, Male Male	8 Participants n=5 Participants	8 Participants n=7 Participants	12 Participants n=5 Participants	9 Participants n=4 Participants	37 Participants n=21 Participants

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

Population: ALL 28 subjects who received lurasidone and have evaluable PK data.

Cmax：Maximum (peak) observed drug serum concentration.

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone Cmax	32.9 ng/ml Geometric Coefficient of Variation 35.4	50.9 ng/ml Geometric Coefficient of Variation 29.6	113 ng/ml Geometric Coefficient of Variation 39.5

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

AUC：Area under the serum concentration-time curve

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone AUC AUC0-t	97.9 ng･h/mL Geometric Coefficient of Variation 26.2	163 ng･h/mL Geometric Coefficient of Variation 26.5	353 ng･h/mL Geometric Coefficient of Variation 35.3
Lurasidone AUC AUC0-24	90.3 ng･h/mL Geometric Coefficient of Variation 26.3	151 ng･h/mL Geometric Coefficient of Variation 26.6	322 ng･h/mL Geometric Coefficient of Variation 34.8
Lurasidone AUC AUC0-∞	107 ng･h/mL Geometric Coefficient of Variation 26.3	174 ng･h/mL Geometric Coefficient of Variation 26.5	378 ng･h/mL Geometric Coefficient of Variation 35.6

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

Tmax：Time to maximum (peak) drug serum concentration

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone Tmax	2.00 h Interval 1.0 to 2.0	2.00 h Interval 1.5 to 3.0	1.50 h Interval 1.0 to 2.0

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

λZ：Elimination rate constant

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone λZ	0.0271 1/h Geometric Coefficient of Variation 26	0.0383 1/h Geometric Coefficient of Variation 32.9	0.0383 1/h Geometric Coefficient of Variation 17.4

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

t1/2 :Biological half life correlated with the elimination rate constant (kel) of semi-logarithmic concentration-time curve

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone t1/2	25.5 h Geometric Coefficient of Variation 26	18.1 h Geometric Coefficient of Variation 32.9	18.1 h Geometric Coefficient of Variation 17.4

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

MRT：Mean residence time.

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone MRT	13.2 h Geometric Coefficient of Variation 26.3	11.1 h Geometric Coefficient of Variation 21.5	11.7 h Geometric Coefficient of Variation 13.7

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

CL/F：Apparent total clearance.

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone CL/F	187 L/h Geometric Coefficient of Variation 26.3	231 L/h Geometric Coefficient of Variation 26.5	212 L/h Geometric Coefficient of Variation 35.6

PRIMARY outcome

Timeframe: pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose

VZ/F: Apparent volume of distribution at terminal phase (correlated with λz)

Outcome measures

Measure	20mg Lurasidone n=8 Participants 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 Participants 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 Participants 80mg lurasidone: single oral lurasidone.
Lurasidone VZ/F	6887 L Geometric Coefficient of Variation 36.3	6022 L Geometric Coefficient of Variation 41.8	5523 L Geometric Coefficient of Variation 39.0

Adverse Events

20mg Lurasidone

Serious events: 0 serious events

Other events: 5 other events

Deaths: 0 deaths

40mg Lurasidone

Serious events: 0 serious events

Other events: 7 other events

Deaths: 0 deaths

80mg Lurasidone

Serious events: 0 serious events

Other events: 12 other events

Deaths: 0 deaths

Placebo

Serious events: 0 serious events

Other events: 5 other events

Deaths: 0 deaths

Serious adverse events

Adverse event data not reported

Other adverse events

Measure	20mg Lurasidone n=8 participants at risk 20mg lurasidone: single oral lurasidone.	40mg Lurasidone n=8 participants at risk 40mg lurasidone: single oral lurasidone.	80mg Lurasidone n=12 participants at risk 80mg lurasidone: single oral lurasidone.	Placebo n=9 participants at risk Subjects administered placebo tablet at the same time with each lurasidone group.
Gastrointestinal disorders Nausea	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	16.7% 2/12 • Number of events 2 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/9 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.
General disorders Feeling hot	12.5% 1/8 • Number of events 1 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/12 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/9 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.
General disorders Irritability	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	12.5% 1/8 • Number of events 1 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/12 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/9 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.
Investigations Blood prolactin increased	12.5% 1/8 • Number of events 1 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	12.5% 1/8 • Number of events 1 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	83.3% 10/12 • Number of events 10 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	22.2% 2/9 • Number of events 2 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.
Investigations White blood cell count decreased	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	12.5% 1/8 • Number of events 1 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/12 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/9 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.
Nervous system disorders Somnolence	62.5% 5/8 • Number of events 5 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	75.0% 6/8 • Number of events 6 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	100.0% 12/12 • Number of events 12 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	33.3% 3/9 • Number of events 3 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.
Nervous system disorders Dizziness	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/8 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	25.0% 3/12 • Number of events 3 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.	0.00% 0/9 • From just after use of the study drug to the study-ending evaluation, up to 11 days. All 37 subjects who received lurasidone or placebo were included in the safety population.

Additional Information

Prof.Hu Chaoying

Shanghai Xuhui Central Hospital, Drug Clinical Trial Institution

Phone: 13816319160

Email: cyhu@shxh-centerlab.com

Results disclosure agreements

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

Restriction type: OTHER