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

Phase 1

Completed

• Conditions: Schizophrenia
• Interventions: Drug: 40mg lurasidone; Drug: placebo

• Registration Number: NCT02174523
• Lead Sponsor: Sumitomo Pharma (Suzhou) Co., Ltd.

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.

Study Timeline

• Study First Submitted: 2014-02-11
• Study Start: 2014-04
• Primary Completion: 2014-04
• Study Completion: 2014-04
• Status Verified: 2014-06
• Study First Submitted QC: 2014-06-23
• Study First Posted: 2014-06-25
• Results First Submitted: 2018-05-31
• Results First Submitted QC: 2019-01-09
• Last Update Submitted: 2019-01-09
• Results First Posted: 2019-04-08
• Last Update Posted: 2019-04-08

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 14

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.

Study & Design

• Study Type: INTERVENTIONAL
• Study Design: PARALLEL

Arm && Interventions

Group	Intervention	Description
40mg lurasidone	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	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.

Primary Outcome Measures

Name	Time	Method
Lurasidone Cmax	Day8	Maximum (peak) observed drug serum concentration.
Lurasidone AUC 0-24	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 AUC 0-τ	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 AUC0-∞	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 Tmax	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 λz	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 t1/2	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 MRT	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 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

Trial Locations

Locations (1)

Xuhui Center Hospital; 🇨🇳 Shanghai, Shanghai, China