An [^11C]T-773 Positron Emission Tomography (PET) Study to Determine Phosphodiesterase10A Occupancy by TAK-063

NCT02370602 | Completed Phase 1 Results

• 3 other identifiers: TAK-063_103U1111-1165-33622012-004576-18
• Study Type: interventional
• Target: 13
• Locations: 0 countries
• Sites: N/A

Brief Summary

The purpose of this study is to estimate phosphodiesterase 10A (PDE10A) occupancy in brain following a single dose of TAK-063.

Conditions

Healthy Volunteers

Keywords

Drug therapy

Outcome Measures

Primary Outcomes (1)

• Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 3 Hours Following a Single Dose of TAK-063

  Volume of tissue distribution (Vt) values will be estimated by several quantitative methods for each positron emission tomography (PET) scan. Based on the change in Vt before and after TAK-063 administration, PDE10A occupancy will be calculated. PET scan #2 in the Pilot Cohort and PET scan #1 in the Main Cohort will be used as a baseline for the occupancy calculation. Occupancy is reported for putamen only.

  3 hours post-dose

Secondary Outcomes (17)

• Phosphodiesterase 10A (PDE10A) Occupancy of Brain Regions With [^11C]T-773 at 23 Hours Following a Single Dose of TAK-063

  23 hours post-dose

• Percentage of Participants Who Experienced at Least 1 Treatment-Emergent Adverse Event

  First dose of study drug to 30 days after last dose of study drug (up to 46 days)

• Percentage of Participants With Markedly Abnormal Safety Laboratory Findings

  From Day 1 to Day 16

• Percentage of Participants With Markedly Abnormal Vital Sign Measurements

  From Day 1 to Day 16

• Percentage of Participants With Markedly Abnormal Criteria for Safety Electrocardiogram (ECG) Parameters

  From Day 1 to Day 16

Study Arms (2)

Pilot Cohort: [^11C]T-773 + TAK-063

EXPERIMENTAL

\[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenous (IV), once on Days 1 and 2 prior to PET scans and TAK-063 30 mg or 1000 mg, tablets, orally, once on Day 2 and after PET scan #2 and prior to PET scan #3 and \[\^11C\]T-773 IV after TAK-063 and prior to PET scan #3 on Day 2.

Drug: TAK-063; Drug: [^11C]T-773

Main Cohort: TAK-063 + [^11C]T-773

EXPERIMENTAL

TAK-063 3 to 100 mg, tablets, orally, once, on Day 1, and \[\^11C\]T-773 \<8 μg; 400MBq ± 10%, intravenously (IV), prior to PET scans, twice on Day 1 (before and after administration of TAK-063) and once on Day 2 .

Drug: TAK-063; Drug: [^11C]T-773

Interventions

TAK-063 DRUG

TAK-063 tablets

Main Cohort: TAK-063 + [^11C]T-773; Pilot Cohort: [^11C]T-773 + TAK-063

[^11C]T-773 DRUG

\[\^11C\]T-773 IV solution

Main Cohort: TAK-063 + [^11C]T-773; Pilot Cohort: [^11C]T-773 + TAK-063

Eligibility Criteria

• Age: 20 Years - 45 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Has never previously participated in a positron emission tomography (PET) study (lifetime).
• In the opinion of the investigator, the participant is capable of understanding and complying with protocol requirements.
• The participant, informed consent form and any required privacy authorization prior to the initiation of any study procedures.
• Is a healthy adult male, as determined by a physician based upon medical history and physical examination findings at Screening.
• Is aged 20 to 45 years, inclusive, at the time of informed consent.
• Weighs at least 50 kg and less than 100 kg and has a body mass index (BMI) between 18 and 32 kg/m\^2 inclusive at Screening.
• A male participant who is nonsterilized and sexually active with a female partner of childbearing potential agrees to use adequate contraception from signing of informed consent throughout the duration of the study and for 12 weeks after last dose.
• Has clinical laboratory evaluations (including clinical chemistry, hematology and complete urinalysis) within the reference range for the testing laboratory, unless the results are deemed not to be clinically significant (CS) by the investigator or sponsor at screening. Participants must have normal hemoglobin levels.
• Has a normal magnetic resonance imaging (MRI) scan or findings that are deemed not clinically significant at screening (the MRI scan may be performed on a day after other screening activities have been performed but before dosing).

You may not qualify if:

• Has received any investigational compound within 90 days prior to Screening.
• Has received TAK-063 in a previous clinical study or as a therapeutic agent.
• Is an immediate family member, study site employee, or in a dependant relationship with a study site employee who is involved in the conduct of this study (eg, spouse, parent, child, sibling) or may consent under duress.
• Has uncontrolled, clinically significant neurologic, cardiovascular, pulmonary, hepatic, renal, metabolic, gastrointestinal, urologic, immunologic, endocrine disease, or psychiatric disorder, or other abnormality, which may impact the ability of the participant to participate or potentially confound the study results.
• Has a known hypersensitivity to any component of the formulation of TAK-063 or \[\^11C\]T-773.
• Has a positive urine drug result for drugs of abuse or a positive breathalyzer test for alcohol at Screening or Day -1.
• Has a history of drug abuse (defined as any illicit drug use) or a history of alcohol abuse within 1 year prior to the screening visit or is unwilling to agree to abstain from alcohol until discharge from the Phase 1 unit and drugs throughout the study.
• Has taken any excluded medication, supplements, or food products listed in the Excluded Medications and Dietary Products table.
• Intends to donate sperm during the course of the study or within 12 weeks after last dose.
• Has evidence of current cardiovascular, central nervous system, hepatic, hematopoietic disease, renal dysfunction, metabolic or endocrine dysfunction, serious allergy, asthma hypoxemia, hypertension, seizures, or allergic skin rash. There is any finding in the participant's medical history, physical examination, or safety laboratory tests giving reasonable suspicion of a disease that would contraindicate taking TAK-063 or a similar drug in the same class, or that might interfere with the conduct of the study. This includes, but is not limited to, peptic ulcer disease, seizure disorders, and cardiac arrhythmias.
• The participant, in the opinion of the investigator, has current or recent (within 6 months) gastrointestinal disease that would be expected to influence the absorption of drugs (ie, a history of malabsorption, esophageal reflux, peptic ulcer disease, erosive esophagitis frequent \[more than once per week\] occurrence of heartburn, or any surgical intervention \[eg, cholecystectomy\]).
• Has a history of cancer, except basal cell carcinoma which has been in remission for at least 5 years prior to Day 1.
• Has a positive test result for hepatitis B surface antigen (HBsAg), hepatitis C antibody (HCV), human immunodeficiency virus (HIV) antibody/antigen, at Screening.
• Has used nicotine-containing products (including but not limited to cigarettes, pipes, cigars, chewing tobacco, nicotine patch or nicotine gum) within 28 days prior to Check-In Day -1.
• Has poor peripheral arterial/venous access or recent arm or wrist trauma.

Sponsors & Collaborators

• Takeda: lead

MeSH Terms

Interventions

1-(2-fluoro-4-(1H-pyrazol-1-yl)phenyl)-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one; T-773 compound

Results Point of Contact

• Title: Medical Director, Clinical Science
• Organization: Takeda (Note: This product was divested to Axsome in 2026)

clinicaltrialregistry@tpna.com

+1-877-825-3327

Study Officials

• Medical Director Clinical Science

  Takeda (Note: This product was divested to Axsome in 2026)

  STUDY DIRECTOR

Publication Agreements

• PI is Sponsor Employee: No
• Restriction Type: OTHER
• Restrictive Agreement: Yes

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: PARALLEL
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: February 18, 2015
• First Posted: February 25, 2015
• Study Start: October 1, 2013
• Primary Completion: February 1, 2014
• Study Completion: March 1, 2014
• Last Updated: May 8, 2026
• Results First Posted: March 20, 2015

Record last verified: 2026-04