PET Trial to Assess the Receptor Occupancy of Brexpiprazole in Adult Subjects With Schizophrenia

Inclusion Criteria

• A diagnosis of Schizophrenia.
• Ability to provide written informed consent.
• Ability to understand the protocol and meet the protocol requirements.
• Must be in good physical health determined by ECG and laboratory values, medical history and physical examinations.
• Has stable disease, defined as meeting all of the following criteria: A CGI-S score 2 times upper limit of normal
• ALT > 2 times upper limit of normal
• Creatinine >= 2 mg/dL
• Subjects with electrolytes outside of the normal range will not be enrolled in the trial without prior review and approval from the medical monitor.
• Subjects who have sitting (performed first) or supine blood pressure, after resting for >= 3 minutes, higher than 140/90 mmHg or lower than 100/50 mmHg. Upon standing from the supine position, subjects who have a fall in systolic blood pressure >= 20 mmHg or a fall in diastolic blood pressure >= 10 mm Hg after 1 to 3 minutes in the standing position. (Any repeated out-of-range values not deemed clinically significant need to be discussed with the medical monitor to determine eligibility.)
• Subjects who have a supine pulse rate, after resting for >= 3 minutes, outside the range of 40 to 90 bpm.
• Subjects with any ECG abnormality at Screening, prior to dosing, will be excluded, including but not limited to, a PR interval > 220 msec, QRS interval > 110 msec, QTc > 450 msec, QTcF > 450 msec, QTcB > 450 msec or the increase in QTcB is considered significant by the investigator, abnormal U waves, or other minor ST-T wave changes which are considered clinically significant.
• Prohibited concomitant medications/therapies used for the following time period prior to Day -1 and for the duration of the trial include:
• Antipsychotics
• Use of oral antipsychotics within 21 days prior to Day -1;
• Use of long-acting injectable antipsychotics within 6 months.
• Anxiolytics and Sleep Aids
• Regular use of benzodiazepines for 2 weeks (lorazepam [ 21 cigarettes per day). Other
• Prisoners or subjects who are compulsorily detained (involuntarily incarcerated) for treatment of either a psychiatric or physical (eg, infectious disease) illness must not be enrolled into this trial.
• Subjects with a history of allergy to more than one class of medications.
• Any subject who, in the opinion of the investigator, should not participate in the trial.
• A history of difficulty in donating blood.
• Exposure to any substances known to stimulate hepatic microsomal enzymes within 30 days prior to Screening through the end of the trial (eg, occupational exposure to pesticides, organic solvents).
• Additionally, subjects who meet the following imaging exclusion criteria will not be included in this trial:
• Subjects who suffer from claustrophobia.
• Subjects with MRI-incompatible implants and other contraindications for MRI, such as pacemaker, artificial joints, nonremovable body piercings, tattoos larger than 1 cm in diameter, metal fragments, claustrophobia, etc.
• Subjects who have received a diagnostic or therapeutic radiopharmaceutical within 7 days prior to participation in this trial.
• Participation in other research trials involving ionizing radiation within 1 year of the PET scans that would cause the subject to exceed the yearly dose limits for normal subjects.
• Subjects with history of IV drug use which would prevent venous access for PET tracer injection.
• Severe motor problems that prevent the subject from lying still for PET and MRI.
• Subjects who complain of chronic pain (eg, as the result of rheumatoid arthritis).