Working…
ClinicalTrials.gov
ClinicalTrials.gov Menu

Study to Evaluate D2 Receptor Occupancy Following Single Intravenous Administration of ATI-9242

The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Read our disclaimer for details.
 
ClinicalTrials.gov Identifier: NCT02824666
Recruitment Status : Completed
First Posted : July 7, 2016
Last Update Posted : July 17, 2017
Sponsor:
Information provided by (Responsible Party):
Braeburn Pharmaceuticals

Brief Summary:
This study involves evaluating the occupancy of ATI-9242 at steady state at three different dose levels on D2 receptors in the brain using [18F] Fallypride PET in up to three cohorts of subjects.

Condition or disease Intervention/treatment Phase
Schizophrenia Drug: ATI-9242 Radiation: [18F]Fallypride Imaging Phase 1

Detailed Description:
This study involves evaluating the occupancy of ATI-9242 at steady state at three different dose levels on D2 receptors in the brain using [18F]Fallypride PET in up to three cohorts of subjects. The first dose evaluated will be 0.5 mg/kg administered as an IV bolus injection. The second dose that will be evaluated will be 1.0 mg/kg as an IV bolus injection. The safety and occupancy after each dose level will be evaluated prior to moving to the next dose. On two separate days, subjects will undergo [18F]Fallypride PET imaging sessions. The plasma concentration of ATI-9242 will be obtained prior to and during the course of the imaging session to allow determination of the relationship between plasma concentration of ATI-9242 with in vivo D2 occupancy.

Layout table for study information
Study Type : Interventional  (Clinical Trial)
Actual Enrollment : 7 participants
Allocation: Non-Randomized
Intervention Model: Parallel Assignment
Masking: None (Open Label)
Primary Purpose: Treatment
Official Title: Phase 1, Open-Label Positron Emission Tomography (PET) Study to Evaluate D2 Receptor Occupancy Following Single Intravenous Administration of ATI-9242 in Adult Male Healthy Subjects
Actual Study Start Date : June 20, 2016
Actual Primary Completion Date : September 6, 2016
Actual Study Completion Date : November 8, 2016

Resource links provided by the National Library of Medicine


Arm Intervention/treatment
Experimental: 0.5 mg/kg
• Cohort 1: ATI-9242 - Single IV bolus dose of 0.5 mg/kg
Drug: ATI-9242

Formulated ATI-9242 will be administered as an IV bolus injection (2mg/mL of ATI-9242 in 40% solution of propylene glycol).

Two doses will be tested: single IV bolus injection of 0.5mg/kg and single IV bolus injection 1.0 mg/kg. In the event that a third cohort is needed the IV bolus injection would be 2.0 mg/kg


Radiation: [18F]Fallypride Imaging
Subjects will be injected with approximately 250 MBq or 6.75 mCi of [18F]Fallypride [5-6 mCi being the typical range of injected dose].

Experimental: ATI-9242 1.0 mg/kg
• Cohort 2: ATI-9242 - Single IV bolus dose of 1.0 mg/kg
Drug: ATI-9242

Formulated ATI-9242 will be administered as an IV bolus injection (2mg/mL of ATI-9242 in 40% solution of propylene glycol).

Two doses will be tested: single IV bolus injection of 0.5mg/kg and single IV bolus injection 1.0 mg/kg. In the event that a third cohort is needed the IV bolus injection would be 2.0 mg/kg


Radiation: [18F]Fallypride Imaging
Subjects will be injected with approximately 250 MBq or 6.75 mCi of [18F]Fallypride [5-6 mCi being the typical range of injected dose].




Primary Outcome Measures :
  1. Target receptor occupancy after single intravenous(IV) of ATI-9242 in 6 healthy adults using the D2 receptor ligand [18F]Fallypride and PET imaging. [ Time Frame: approximately 5 weeks ]
    Change from baseline in PET imaging at baseline of ATI-9242 and post-dose


Secondary Outcome Measures :
  1. Explore the relationship between ATI-9242 dose, plasma concentrations of ATI-9242 and target receptor occupancy in 6 subjects. [ Time Frame: approximately 5 weeks ]
    The relationship between plasma drug concentration/PK parameters of ATI-9242 and D2 occupancy will be explored.


Other Outcome Measures:
  1. Safety and tolerability of ATI-9242 following single IV dose in 6 healthy subjects via safety assessments . [ Time Frame: approximately 5 weeks ]
    incidence of adverse events (AEs), vital signs (blood pressure, pulse and oral temperature), physical examinations 12-lead ECG, CSSRS and clinical laboratory tests (hematology, clinical chemistry and urinalysis).



Information from the National Library of Medicine

Choosing to participate in a study is an important personal decision. Talk with your doctor and family members or friends about deciding to join a study. To learn more about this study, you or your doctor may contact the study research staff using the contacts provided below. For general information, Learn About Clinical Studies.


Layout table for eligibility information
Ages Eligible for Study:   18 Years to 50 Years   (Adult)
Sexes Eligible for Study:   Male
Accepts Healthy Volunteers:   Yes
Criteria

Inclusion Criteria:

  • Are males > 18 years of age and < 50 years of age.
  • BMI <30
  • Are in good health as determined by past medical history, physical examination, vital signs, electrocardiogram, and laboratory tests at screening.
  • Are able to communicate well with the investigator, to understand and comply with the requirements of the study, and understand and sign the written informed consent.
  • Provide informed consent for study procedures.
  • Male subjects and their partners of childbearing potential must commit to the use of two methods of contraception, one of which is a barrier method for male subjects and for 90 days after the end of the study.
  • Subjects must not donate sperm for the study duration and for 90 days after the end of the study.
  • Willing and able to cooperate with study procedures
  • A brain MRI within the past 120 days with no evidence of active or focal neurological disease that may interfere with the [18F]Fallypride PET data.

Exclusion Criteria:

  • Use of any prescription drugs, herbal supplements, within four (4) weeks prior to Baseline imaging, and/or over-the-counter (OTC) medication, dietary supplements (vitamins included) within two (2) weeks prior to Baseline imaging. If needed (i.e. an incidental and limited need), acetaminophen is acceptable, but must be documented as a concomitant medication/significant non-drug therapy.
  • Exposure to any investigational drug within the 4 weeks prior to screening visit.
  • Subjects with a history of exposure to any radiation >15 mSv/year (e.g., occupational or radiation therapy) over the past year.
  • Donation or loss of 400 ml or more of blood within eight (8) weeks prior to initial dosing, or longer if required by local regulation.
  • Have a history or presence of any significant cardiovascular, respiratory, hepatic, renal, gastrointestinal, endocrine, or neurological disorders which, in the opinion of the investigator, are capable of altering the absorption, metabolism, or elimination of drugs or posing a health risk to participate in the study.
  • Have clinically significant findings on laboratory evaluations in the opinion of the investigator.
  • Have clinically significant findings on ECG evaluation.
  • A positive Hepatitis B surface antigen (HBsAg), Hepatitis C antibody or HIV test result.
  • History of drug or alcohol abuse within the 12 months prior to screening, or evidence of such abuse as indicated by the laboratory assays conducted during the screening.
  • History of tobacco product use within 3 months prior to screening, to be verified by urine cotinine screening.
  • Implants such as implanted cardiac pacemakers or defibrillators, insulin pumps, cochlear implants, metallic ocular foreign body, implanted neural stimulators, CNS aneurysm clips and other medical implants that have not been certified for MRI.
  • Claustrophobia that would interfere with completion of MRI and/or SPECT procedures.
  • Inability to lie supine for 90 minutes at a time.

Information from the National Library of Medicine

To learn more about this study, you or your doctor may contact the study research staff using the contact information provided by the sponsor.

Please refer to this study by its ClinicalTrials.gov identifier (NCT number): NCT02824666


Locations
Layout table for location information
United States, Indiana
Indiana Clinical Research Center, IU Health University Hospital
Indianapolis, Indiana, United States, 46202
Sponsors and Collaborators
Braeburn Pharmaceuticals
Layout table for additonal information
Responsible Party: Braeburn Pharmaceuticals
ClinicalTrials.gov Identifier: NCT02824666    
Other Study ID Numbers: BB-ATI9242-001
First Posted: July 7, 2016    Key Record Dates
Last Update Posted: July 17, 2017
Last Verified: July 2017
Individual Participant Data (IPD) Sharing Statement:
Plan to Share IPD: No
Additional relevant MeSH terms:
Layout table for MeSH terms
Schizophrenia
Schizophrenia Spectrum and Other Psychotic Disorders
Mental Disorders
Fallypride
Dopamine D2 Receptor Antagonists
Dopamine Antagonists
Dopamine Agents
Neurotransmitter Agents
Molecular Mechanisms of Pharmacological Action
Physiological Effects of Drugs