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

Phase 1

Completed

• Conditions: Schizophrenia
• Interventions: Drug: 20mg lurasidone; Drug: 40mg lurasidone; Drug: 80mg lurasidone; Drug: placebo

• Registration Number: NCT02174510
• Lead Sponsor: Sumitomo Pharma (Suzhou) Co., Ltd.

Brief Summary

To evaluate the pharmacokinetic (PK) characteristics of lurasidone after single oral administration of different doses in healthy Chinese subjects.

To evaluate the safety and tolerability of lurasidone after single oral administration of different doses in healthy Chinese subjects.

Detailed Description

Single administration, double-blinded, placebo-controlled (3 subjects in each group will take placebo) and 3 dose groups (20 mg, 40 mg and 80 mg). There are three groups which are 20mg lurasidone or placebo, 40mg lurasidone or placebo and 80mg lurasidone or placebo.

This study comprises a screening period (between signing of the informed consent form and Day -2), baseline period (Day -1), treatment period (Days 1-3) and ending of study examination period (Days 8-11 after the last sample collection for PK evaluation).

Study Timeline

• Study First Submitted: 2014-02-11
• Study Start: 2014-03
• Primary Completion: 2014-04
• Study Completion: 2014-04
• Study First Submitted QC: 2014-06-23
• Study First Posted: 2014-06-25
• Status Verified: 2018-05
• Results First Submitted: 2018-05-31
• Results First Submitted QC: 2019-01-09
• Last Update Submitted: 2019-01-09
• Results First Posted: 2019-01-11
• Last Update Posted: 2019-01-11

Recruitment & Eligibility

• Status: COMPLETED
• Sex: Male
• Target Recruitment: 37

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 written 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.
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 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 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
20mg lurasidone	20mg lurasidone	single oral lurasidone in 30 minutes after beginning of the over 350 kcal breakfast on day 1.The subjects will be follow up on day 8 to 11.
20mg lurasidone	placebo	single oral lurasidone in 30 minutes after beginning of the over 350 kcal breakfast on day 1.The subjects will be follow up on day 8 to 11.
40mg lurasidone	40mg lurasidone	single oral lurasidone in 30 minutes after beginning of the over 350 kcal breakfast on day 1.The subjects will be follow up on day 8 to 11.
40mg lurasidone	placebo	single oral lurasidone in 30 minutes after beginning of the over 350 kcal breakfast on day 1.The subjects will be follow up on day 8 to 11.
80mg lurasidone	80mg lurasidone	single oral lurasidone in 30 minutes after beginning of the over 350 kcal breakfast on day 1.The subjects will be follow up on day 8 to 11.
80mg lurasidone	placebo	single oral lurasidone in 30 minutes after beginning of the over 350 kcal breakfast on day 1.The subjects will be follow up on day 8 to 11.

Primary Outcome Measures

Name	Time	Method
Lurasidone Cmax	pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	Cmax：Maximum (peak) observed drug serum concentration.
Lurasidone AUC	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
Lurasidone Tmax	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
Lurasidone λZ	pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	λZ：Elimination rate constant
Lurasidone t1/2	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
Lurasidone MRT	pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	MRT：Mean residence time.
Lurasidone CL/F	pre-dose,0.5,1,1.5,2,3,4,6,8,12,24,36,48 hours post-dose	CL/F：Apparent total clearance.
Lurasidone VZ/F	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)

Trial Locations

Locations (1)

Xuhui Center Hospital; 🇨🇳 Shanghai, Shanghai, China