First in Man Study of Safety, Tolerability and PK Profile of RBP-7000

Twelve subjects with stable schizophrenia will be enrolled. The expected duration of
participation is 88 days which includes at least a 2 days screening and an 85 day treatment
period (15 -day inpatient stay in the clinical unit and an additional 70-day outpatient
period, including the Day 85 end of study follow up or early termination visit. Visits will
occur approximately weekly during the outpatient period.

Neurological and clinical symptom assessments (Positive and Negative Syndrome Scale [PANSS],
Clinical Global Impressions-Schizophrenic Specific [CGI-SCH], Simpson-Angus Scale [SAS],
Barnes Akathisia Scale [BAS], and Columbia-Suicide Severity Rating Scale [C-SSRS]) will be
conducted at screening, on the day of admission to the clinical unit (Day -1), and at each
post-dose visit throughout the study including the follow-up visit. Scale results will be
reviewed by the Principal Investigator. The Abnormal Involuntary Movement Scale (AIMS) for
Tardive Dyskinesia will be performed at screening and at each post-dose visit throughout the
study including the end of study follow-up visit. CYP-2D6 genotyping will be conducted at
screening. Tolerability will be measured using SAS, which will be conducted as described
above.

Blood samples to assess the PK parameters will be taken from pre-dose until approximately 84
days post-dose.

End of study procedures will be conducted on follow-up Day 85 (84 days post-dose) or early
termination (ET) to assess any adverse events (AEs) that were ongoing at the last visit, any
new AEs that have developed, and for measurement of safety parameters.

Inclusion Criteria:

- Confirmed diagnosis of paranoid, residual, or undifferentiated schizophrenia in a
documented letter from the subject's psychiatrist or primary care provider.

- Clinically stable subjects (subjects whom the Principal Investigator (PI) established
by medical record or by history from the subject and at least one reliable informant
who resides with the subject, that the subject has been clinically stable for at
least 60 days without hospitalization) will be eligible to participate in the study.

- Subjects with a body mass index (BMI) of 18 to 33 kg/m2 inclusive and weighing at
least 49.9 kg are eligible for entry.

- Subjects who have given written informed consent.

Exclusion Criteria:

- Subjects taking any risperidone product in the last 60 days prior to study screening.

- Subjects with a history of cancer (excluding resected basal cell or squamous cell
carcinoma of the skin) unless they have been disease free for ≥ 5 years.

- Subjects with another active medical condition or organ disease that may either
compromise subject safety or interfere with the safety and/or outcome evaluation of
the study drug. This includes, but is not limited to the following abnormalities:
total bilirubin > 2.5 mg/dL (51 μmol/L), alanine aminotransferase (ALT) or aspartate
aminotransferase (AST) > 3 times the upper limit of normal (ULN) or clinically
significant serum creatinine > 2 x ULN, international normalized ratio (INR) ≥ 2.0.
Other excluded medical conditions including, but not limited to, history of heart
attack, brain injury, low blood pressure and clinically significant irregular
heartbeat.

- Subjects with known diagnosis of type 1 or 2 diabetes or subjects with an abnormal
Hemoglobin A1c (HbA1c) at screening.

- Subjects with clinically significant co-morbidities that could affect near-term
survival.

- Subjects treated with any investigational drug within 30 days beginning study
screening.

- Subjects with significant traumatic injury, major surgery or open biopsy within the
past 4 weeks.

- Subjects receiving opioid or opioid-containing analgesics.

- Subjects consuming > 1 alcoholic drink per day within the last 30 days (defined as
one ounce of 80 proof spirits, 12 ounces of beer, or 4 ounces of wine).

- Subjects with prior allergic reactions or sensitivities to any component of RBP-7000.

- Subjects with other concurrent uncontrolled illness that may interfere with his or
her ability to participate in the trial.

- Subjects with other known contraindications or sensitivity to risperidone or other
components of RBP-7000.

- Women with a positive pregnancy test at screening. Women of childbearing potential,
who are pregnant or lactating, seeking pregnancy, or failing to take adequate
contraceptive precautions, (e.g., an oral or injectable contraceptive, an approved
hormonal implant or topical patch, an intrauterine device, abstinence. Should a
female subject become sexually active, she must agree to use a double barrier method
or barrier plus spermicide). A woman of childbearing potential is defined as any
female who is less than 2 years post-menopausal or has not undergone a hysterectomy
or surgical sterilization, e.g. bilateral tubal ligation, bilateral ovariectomy
(oophorectomy).

- . Subjects with a positive urine drug screen for opiates, cocaine, amphetamines,
methadone, marijuana, barbiturates, benzodiazepines, methamphetamine, phencyclidine,
and tricyclic antidepressants unless the positive screen is determined to be
secondary to an allowable concomitant medication.

- Subjects with epilepsy or other seizure disorders, Parkinson's disease, or dementia.

- Subjects taking buproprion, chlorpheniramine, cimetidine, clomipramine, doxepin, or
quinidine.

- Subjects taking clozapine, phenothiazines, or haloperidol.

- Subjects taking serotonin reuptake inhibitors (e.g., fluoxetine, paroxetine) in the
30 days prior to beginning study screening.

- . Subjects taking medications, in addition to those listed above, which may be
expected to significantly interfere with the metabolism or excretion of risperidone
and/or 9-hydroxyrisperidone, that may be associated with a significant drug
interaction with risperidone, or may pose a significant risk to subjects'
participation in the study.

- Subjects who have been previously enrolled into the study.

- Subjects who are unable, in the opinion of the Principal Investigator, to comply
fully with the study requirements.