The Pharmacokinetics, Tolerability and Safety of Brexpiprazole in Healthy Chinese Subjects

• Status: Completed
• Trial end date: 2020-05-18
• Target enrollment: 0
• Participant gender: All

Summary

This study is a single-center, open-label study evaluating the pharmacokinetics, tolerability and safety of single dose oral brexpiprazole tablets in healthy Chinese subjects. A total of 30 healthy adult subjects are to be enrolled into the study. Three dose groups will be set up, with about 10 subjects in each dose group. Subjects will enter 1 mg, 2 mg and 4 mg dose groups in sequence.

• Phase: Phase 1
• Accepts Healthy Volunteers?: Accepts Healthy Volunteers

Details

• Lead Sponsor: Otsuka Beijing Research Institute
• Treatments: Brexpiprazole

Criteria

Inclusion Criteria:

• 1. Sign the informed consent form

• 2.At the age of 18~45 years old (including upper and lower limits) when signing the informed consent form.

• 3.Body weight of not less than 50kg, BMI 19 ~ 24kg/m2 (including the upper and lower limits) [ body mass index (BMI) = body weight (kg) / height2 (m2)].

• 4.Subjects determined by the investigator to be healthy according to the medical history and the results of serological examination (HIV antibodies, HBsAg, HCV antibodies and syphilis antibodies), physical examination, vital signs (body temperature, blood pressure, heart rate), 12 lead ECG, laboratory tests (routine blood tests, blood biochemical tests, routine urine tests).

• 5.Subjects agree to take appropriate contraceptive measures during the trial and within 4 weeks after the dose.

Exclusion Criteria:

• 1. Participated in any interventional clinical trial within 12 weeks prior to enrollment.

• 2.Drug abuse in the past 2 years or a history of abuse

• 3.Drinking alcohol more than 2 unit per day (1 unit= 360 ml beer , or 45 ml 4.0% alcohol, or 150 ml liquor, or 50 ml wine ) 6 months before the screening, or subjects can not stop drinking during the hospitalization

• 4.Smoking urine test or drug abuse urine test at screening is positive.

• 5.Taking grapefruit, seville orange, coffee, alcohol or food containing these ingredients one week before taking the study drug.

• 6.Taking any other prescriptions or over-the-counter medications or Chinese herbal medicine or vitamin 14 days prior to taking the test medication

• 7.Use of any drug that inhibits or induces CYP2D6 and CYP3A4 metabolic enzymes 30 days prior to taking the study drug

• 8.At the discretion of the investigators, subjects' diet significantly deviates from normal intake of protein, carbohydrate and fat (e.g. vegetarians or absolute vegetarians).

• 9.Blood donation or equal blood loss (> 350 ml) within 12 weeks prior to medication.

• 10.Past or present allergy to any medication.

• 11.HbA1c ≥ 6.0% at screening.

• 12.Urinary pregnancy test (HCG) is positive at screening or female subjects who were in lactation.

• 13.Breath alcohol test positive.

• 14.Any positive result in HIV antibody, HBsAg, HCV antibody and syphilis serology test.

• 15.Heart rate <50 bpm or >100 bpm at resting state.

• 16.Blood pressure at resting satate in prone positon, sitting position or standing position > 140/90 mmHg, or < 90/60 mmHg.

• 17.Symptomatic hypotension or orthostatic hypotension (orthostatic hypotension is defined as standing blood pressure, systolic blood pressure (SBP) dropped ≥30 mmHg and/or diastolic blood pressure (DBP) decreased ≥20 mmHg after 3 minutes of resting pressure in the supine position or present symptoms).

• 18.Previous or current organic illness (including but not limited to cardiovascular, liver, kidney, nerve, digestive tract, respiratory tract, hematology, endocrine and immune diseases ).Other conditions determined by the investigator could bring risk to the subjects or interfere the result of the trial, including but not limited to drug absorption, distribution, metabolism or excretion.

• 19.Previous or current psychological abnormality, mental or neurological disorders or autonomic neuropathies that are considered potential by investigators to compromise or influence the subject's ability to participate in the trial.

• 20.Subjects with abnormal digestion and absorption function (e.g. alimentary canal excision history ).

• 21.Other subjects determined by the investigators not fit for the enrollment of the trial.