Pharmacokinetic Study of Lurasidone After Multiple Oral Administration in Healthy Human Subjects

Status

Completed

Phases

Phase 1

Study type

Interventional

Source

ClinicalTrials.gov

Registry ID

NCT02174523

Enrollment

Registered

2014-06-25

Start date

2014-04-30

Completion date

2014-04-30

Last updated

2019-04-08

For informational purposes only — not medical advice. Sourced from public registries and may not reflect the latest updates. Terms

Conditions

Schizophrenia

Keywords

pharmacokinetic, lurasidone, multiple dose

Brief summary

To evaluate the pharmacokinetic (PK) characteristics after multiple oral administration of 40 mg lurasidone in healthy Chinese subjects. To evaluate the safety and tolerance after multiple oral administration of 40 mg lurasidone in healthy Chinese subjects.

Detailed description

Single oral administration of 40 mg study drug lurasidone or placebo 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 or placebo, once daily between Day 4 and Day 8.

Interventions

DRUG40mg lurasidone

DRUGplacebo

Study design

Allocation

RANDOMIZED

Intervention model

PARALLEL

Primary purpose

OTHER

Masking

TRIPLE (Subject, Caregiver, Investigator)

Eligibility

Sex/Gender

MALE

Age

18 Years to 40 Years

Healthy volunteers

Yes

Inclusion criteria

1. After detailed explanations of study objectives, methods and procedures, anticipated efficacy, pharmacologic actions, risks and other relevant contents, subjects are aware of all relevant information related to this study and have signed the informed consent form voluntarily. 2. Male subjects are 18≤ age \<40 years of age when signing the informed consent. 3. Subjects with body weight of 50.0≤ and ≤80.0 kg and BMI (body mass index) of 19.0≤ and \<24.0 at screening examination. 4. Subjects are able to comply with all requirements during this study period, receive various physical and laboratory examinations per study protocol, and report subjective symptoms.

Exclusion criteria

1. Based on the examination results during screening period, various physical and laboratory examinations performed 1 day before medication (Day -1) and before administration of study drug on the medication day, there are certain medical concerns on subject's health status in principal investigator's or study supervising physician's opinions (certain treatment or medical observation are deemed necessary). 2. Subjects with past diabetic history. 3. Subjects has an HbA1c level of \>6.2% at screening. 4. Subjects with history of gastrointestinal operations (excluding appendectomy). 5. Because of subjects' past medical history of cardiovascular diseases, liver diseases, renal diseases, endocrine disorders, digestive diseases, hematologic diseases, respiratory diseases, mental illness, neurological disorders (especially epilepsy and other convulsive disorders) and other diseases, subjects are unsuitable to participate in this study in the principal investigator's or study supervising physician's opinions. 6. Subjects with past history of allergy to drugs. 7. Subjects have consumed grapefruit or food containing grapefruit ingredients between 7 days before medication (Day\_-7) and before administration of study drug on the medication day (Day 1). Subjects have consumed food containing hypericum perforatum L. ingredients between 14 days before medication (Day\_-14) and administration of study drug on the medication day (Day 1). 8. Subjects have taken any drugs (including over-the-counter drugs) between 7 days before medication (Day\_-7) and before administration of study drug on medication day. 9. Regular drinker (criteria are mean daily consumption ≥2 bottles of 640 mL beers or Chinese liquor≥150 mL). 10. Subjects are used to drink large amount (criteria are daily consumption\>1.8 L) of caffeine-containing beverages (e.g. coffee, black tea, green tea, coca cola or nutritional oral solution, etc). 11. Subjects have history of drug abuse or positive urine drug tests. 12. Subjects with positive immunologic test results. 13. Average amount of daily smoking\>20 cigarettes. 14. Subjects have taken other study drugs within 3 months (Day\_-90\ Day 1) before medication. 15. Subjects received lurasidone orally before. 16. Subjects have history of blood donations of 400 mL within 3 months (Day\_-90\ Day 1) before medication; 200 mL within 1 month (Day\_-30\ Day 1) before medication; or donation of blood components within 2 weeks (Day\_-14\ Day 1) before medication. 17. Subjects have consumed alcohol-containing food between 3 days before medication 3 (Day\_-3) and before administration of study drug on medication day. 18. Subjects can not tolerate venipuncture or have poor peripheral venous access. 19. Subjects are unwilling to abstain from vigorous exercise from Day\_-1 until discharge. 20. Other subjects who are unsuitable to participate in this study in principal investigator's or study supervising physician's opinions.

Design outcomes

Primary

Measure	Time frame	Description
Lurasidone Cmax	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	Maximum (peak) observed drug serum concentration.
Lurasidone AUC 0-24	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone AUC 0-τ	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone AUC0-∞	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone Tmax	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone λz	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone t1/2	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone MRT	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone CL/F	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
CLss/F	Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8	—
Lurasidone Vz/F	pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	—
Lurasidone Vzss/F	Day 8	—
Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,	Day 8/Day 1	—
Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 4 and Day 5	Pre-dose (-0.5h) of Day4 and Day5	—
Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 6 and Day 7	Pre-dose (-0.5h) of Day6 and Day7	—

Countries

China

Participant flow

Recruitment details

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）.

Participants by arm

Arm	Count
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.	10
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.	4
Total	14

Withdrawals & dropouts

Period	Reason	FG000	FG001
Overall Study	Withdrawal by Subject	1	0

Baseline characteristics

Characteristic	40mg Lurasidone	Placebo	Total
Age, Continuous	27.7 years STANDARD_DEVIATION 3.74	26.5 years STANDARD_DEVIATION 5.07	27.4 years STANDARD_DEVIATION 3.99
Sex: Female, Male Female	0 Participants	0 Participants	0 Participants
Sex: Female, Male Male	10 Participants	4 Participants	14 Participants

Adverse events

Event type	EG000 affected / at risk	EG001 affected / at risk
deaths Total, all-cause mortality	— / —	— / —
other Total, other adverse events	10 / 10	1 / 4
serious Total, serious adverse events	0 / 10	0 / 4

Outcome results

Primary

Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,

Time frame: Day 8/Day 1

Arm	Measure	Group	Value (MEAN)
40mg Lurasidone	Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,	Ratio of Cmax	0.94 Ratios
40mg Lurasidone	Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,	Ratio of AUC0-∞	1.74 Ratios
40mg Lurasidone	Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,	Ratio of AUC0-τ	1.25 Ratios
40mg Lurasidone	Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,	Ratio of Cτ	2.52 Ratios

Primary

CLss/F

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	CLss/F	211 L/h	Geometric Coefficient of Variation 27.9

Primary

Lurasidone AUC0-∞

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone AUC0-∞	314 ng･h/mL	Geometric Coefficient of Variation 26.6

Primary

Lurasidone AUC0-∞

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone AUC0-∞	179 ng･h/mL	Standard Deviation 29.9

Primary

Lurasidone AUC 0-24

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone AUC 0-24	190 ng･h/mL	Geometric Coefficient of Variation 27.9

Primary

Lurasidone AUC 0-24

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone AUC 0-24	152 ng･h/mL	Geometric Coefficient of Variation 33.2

Primary

Lurasidone AUC 0-τ

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone AUC 0-τ	234 ng･h/mL	Geometric Coefficient of Variation 27.4

Primary

Lurasidone AUC 0-τ

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone AUC 0-τ	166 ng･h/mL	Geometric Coefficient of Variation 32.4

Primary

Lurasidone CL/F

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone CL/F	223 L/h	Geometric Coefficient of Variation 29.9

Primary

Lurasidone Cmax

Maximum (peak) observed drug serum concentration.

Time frame: Day8

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone Cmax	48.5 ng/mL	Geometric Coefficient of Variation 49.4

Primary

Lurasidone Cmax

Maximum (peak) observed drug serum concentration.

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone Cmax	50.2 ng/mL	Geometric Coefficient of Variation 44.3

Primary

Lurasidone MRT

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone MRT	22.0 h	Geometric Coefficient of Variation 19

Primary

Lurasidone MRT

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone MRT	12.2 h	Geometric Coefficient of Variation 22.7

Primary

Lurasidone t1/2

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone t1/2	19.3 h	Geometric Coefficient of Variation 20.8

Primary

Lurasidone t1/2

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone t1/2	34.9 h	Geometric Coefficient of Variation 20.2

Primary

Lurasidone Tmax

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (MEDIAN)
40mg Lurasidone	Lurasidone Tmax	1.75 h

Primary

Lurasidone Tmax

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (MEDIAN)
40mg Lurasidone	Lurasidone Tmax	1.50 h

Primary

Lurasidone Vz/F

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone Vz/F	6198 L	Geometric Coefficient of Variation 47.9

Primary

Lurasidone Vzss/F

Time frame: Day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone Vzss/F	10618 L	Geometric Coefficient of Variation 38.6

Primary

Lurasidone λz

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

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone λz	0.0360 1/h	Geometric Coefficient of Variation 20.8

Primary

Lurasidone λz

Time frame: Day8 0.5hours pre-dose, 0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose in day 8

Population: All subjects with evaluable PK data were included in PK data analysis.

Arm	Measure	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	Lurasidone λz	0.0199 1/h	Geometric Coefficient of Variation 20.2

Primary

Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 4 and Day 5

Time frame: Pre-dose (-0.5h) of Day4 and Day5

Arm	Measure	Group	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	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
40mg Lurasidone	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

Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 6 and Day 7

Time frame: Pre-dose (-0.5h) of Day6 and Day7

Arm	Measure	Group	Value (GEOMETRIC_MEAN)	Dispersion
40mg Lurasidone	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
40mg Lurasidone	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

Source: ClinicalTrials.gov · Data processed: Mar 9, 2026

Pharmacokinetic Study of Lurasidone After Multiple Oral Administration in Healthy Human Subjects

Conditions

Keywords

Brief summary

Detailed description

Related papers

Interventions

Sponsors

Study design

Eligibility

Inclusion criteria

Exclusion criteria

Design outcomes

Primary

Countries

Participant flow

Recruitment details

Participants by arm

Withdrawals & dropouts

Baseline characteristics

Adverse events

Outcome results

Accumulation Ratios Lurasidone,Ratio of Cmax,Ratio of AUC0-∞,Ratio of AUC0-τ,

CLss/F

Lurasidone AUC0-∞

Lurasidone AUC0-∞

Lurasidone AUC 0-24

Lurasidone AUC 0-24

Lurasidone AUC 0-τ

Lurasidone AUC 0-τ

Lurasidone CL/F

Lurasidone Cmax

Lurasidone Cmax

Lurasidone MRT

Lurasidone MRT

Lurasidone t1/2

Lurasidone t1/2

Lurasidone Tmax

Lurasidone Tmax

Lurasidone Vz/F

Lurasidone Vzss/F

Lurasidone λz

Lurasidone λz

Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 4 and Day 5

Summary of Concentration (ng/mL) of Lurasidone - PK Population the Mean (SD) of Day 6 and Day 7