Safety and Tolerability Comparison of Immediate and Controlled Release Formulations of Ecopipam

Ecopipam hydrochloride (HCl) is an investigational drug being studied for several possible
diseases. To date, all clinical studies have been done using the ecopipam immediate release
(IR) tablet. However, a controlled release (CR) capsule formulation of ecopipam has been
produced that may be able to improve its effectiveness and reduce its side effects. The main
purpose of this study is to evaluate the safety and tolerability of ecopipam CR capsules
when given as single oral dose in healthy volunteers. Another purpose of the study is to
measure how much CR and IR ecopipam gets into the blood stream, and how long the body takes
to get rid of them. Information about any side effects that may occur will be collected.

Inclusion Criteria:

1. Signed and dated, IRB-approved informed consent form before any protocol-specific
screening procedures

2. Non-smoking male subjects between the ages of 18 and 45 years (inclusive)

3. In good general health as determined by a thorough medical history and physical
examination, ECG, vital signs, and clinical laboratory evaluation

4. Willing and able to complete all study assessments and procedures

5. Body mass index (BMI) between 18 and 30 kg/m2 (inclusive) and a weight between 65 and
100 kg (inclusive)

6. QTcB interval (Bazett's correction factor) of the baseline ECG must be ≤ 450 ms at
screening

Exclusion Criteria:

1. Subjects with a history of suicide attempt or with past or current active suicidal
ideation

2. Subjects with a history of seizures or with head trauma leading to loss of
consciousness

3. Subjects with clinically significant neurologic, cardiovascular, hepatic, renal,
endocrinologic, pulmonary, hematological, psychiatric, or other medical illness that
would interfere with participation in this study

4. History of any primary malignancy, with the exception of basal cell or squamous cell
carcinomas of the skin or cervical carcinoma in situ or other malignancies curatively
treated and with no evidence of disease for at least 5 years

5. Supine blood pressure >140/90 mm/Hg or resting heart rate ≥100 bpm at the screening
visit

6. History of substance-related disorders (with the exception of caffeine-related and
nicotine-related disorders) or eating disorders as defined in the Diagnostic and
Statistical Manual of Mental Disorders (DSM-IV-TR) within 1 year of screening

7. History of smoking or the use of nicotine containing products within 3 months of
screening by self reporting

8. A positive alcohol Breathalyzer or urine drug screen for drugs of abuse at the
screening visit or at the beginning of the inpatient period

9. Treatment with an investigational drug within 30 days or 5 half-lives (whichever is
longer) prior to the beginning of the screening period

10. Treatment with any other prescription or non-prescription drugs (including vitamins,
herbal, and dietary supplements) within 7 days or 5 half-lives of the screening
visit, whichever is longer. Acetaminophen will be permitted for intermittent
treatment at doses of less than 2 grams/day

11. Subjects with a history of previous administration of ecopipam or of an allergic
reaction or hypersensitivity to any drug or to any component of the CR formulation

12. Blood collection or blood loss of greater than 500 mL within 56 days prior to
screening

13. Positive for human immunodeficiency virus (HIV) at screening

14. Positive for Hepatitis B surface antigen (HbsAg) or positive Hepatitis C virus (HCV)
antibody at screening

15. Any other condition and/or situation that causes the investigator to deem a subject
unsuitable for the study (e.g., due to expected study medication non-compliance,
inability to medically tolerate the study procedures, or a subject's unwillingness to
comply with study-related procedures)