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

A Phase 1, Single Center, Randomized (2-Sequence), Single Blind, 3-Period Study Comparing the Safety, Tolerability, and Pharmacokinetics of Ecopipam Controlled Release Capsules With Ecopipam HCl Immediate Release Tablets in Male Adult Volunteers

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.

Study Overview

• Status: Completed
• Conditions: Healthy
• Intervention / Treatment: Drug: Ecopipam immediate release form; Drug: 90 mg controlled release form; Drug: 180 mg controlled release form

Detailed Description

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.

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Contacts and Locations

Study Locations

• United States
  • Maryland
    • Baltimore, Maryland, United States, 21201
      • SNBL Clinical Pharmacology Center, Inc.

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 16 years to 43 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

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)

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: Single

Number of Arms

3

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Active Comparator: 100 mg immediate release form; This is the formulation currently in use	Drug: Ecopipam immediate release form; Tablet containing 100 mg of the immediate release form of ecopipam; Other Names: SCH 39166; PSYRX101
Experimental: 90 mg controlled release; This is the low dose of the controlled release form	Drug: 90 mg controlled release form; This is the 90 mg controlled release form; Other Names: SCH 39166; PSYRX101
Experimental: 180 mg controlled release form; This is the medium controlled release dose	Drug: 180 mg controlled release form; This is the 180 mg controlled release capsule; Other Names: SCH 39166; PSYRX101

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Safety	Physical examinations, adverse events, vital signs, clinical laboratory values, ECG and Columbia Suicide Severity Ratings scale	0-48 hours

Secondary Outcome Measures

Outcome Measure	Measure Description	Time Frame
Pharmacokinetics	Pharmacokinetic properties of CR and IR ecopipam following oral administration	0-48 hours

Collaborators and Investigators

• Sponsor: Emalex Biosciences Inc.
• Collaborators: Psyadon Pharma
• Investigators: Principal Investigator: Mohamed Al-Ibrahim, MB,ChB,FACP, SNBL Clinical Pharmacology Center, Inc.

Study record dates

Study Major Dates

• Study Start: August 1, 2011
• Primary Completion (Actual): February 1, 2012
• Study Completion (Actual): May 1, 2012

Study Registration Dates

• First Submitted: August 1, 2011
• First Submitted That Met QC Criteria: August 2, 2011
• First Posted (Estimated): August 3, 2011

Study Record Updates

• Last Update Posted (Estimated): April 19, 2024
• Last Update Submitted That Met QC Criteria: April 18, 2024
• Last Verified: May 1, 2013

More Information

Terms related to this study

• Keywords: safety; pharmacokinetics; formulation; controlled release
• Additional Relevant MeSH Terms: Physiological Effects of Drugs; Neurotransmitter Agents; Molecular Mechanisms of Pharmacological Action; Central Nervous System Depressants; Antipsychotic Agents; Tranquilizing Agents; Psychotropic Drugs; Dopamine Agents; Dopamine Antagonists; Ecopipam
• Other Study ID Numbers: PSY401