Exploratory Study Using Positron Emission Tomography With TS-121 and [11C]TASP0410699 in Healthy Adult Male Subjects

Study Overview
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Brief Summary
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The purpose of this study is to evaluate the binding of a novel tracer, [11C]TASP0410699, using Positron Emission Tomography (PET) scans with or without dosing of TS-121

Official Title
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A Phase 1 Receptor Occupancy Study Using Positron Emission Tomography to Investigate Novel Ligand [11C]TASP0410699 Alone and Following Single Oral Dose Administrations of TS-121 in Healthy Adult (Male) Subjects

Conditions
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Healthy

Intervention / Treatment
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* Drug: TS-121
* Drug: [11C]TASP0410699
* Radiation: Positron Emission Tomography (PET)


Participation Criteria
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Eligibility Criteria
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Inclusion Criteria: Healthy males 18 - 55 years of age (at time of initial informed consent) Body weight ≥ 50 kg Body Mass Index (BMI) 18 - 30 kg/m2 Male subjects with partners of childbearing potential must agree to use appropriate and effective measures of contraception for 90 days following drug administration Exclusion Criteria: Prescription, over-the-counter or herbal medications, supplements, within 14 days before the study. Clinically significant abnormal electrocardiogram, physical examination, or hematology, biochemistry, hormone, or urinalysis values at screening & baseline. Significant history &/or presence of hepatic, renal, cardiovascular, hemodynamic, pulmonary, gastrointestinal, hematological, CNS, immunologic, ophthalmologic, metabolic, endocrine, or oncological disease or condition within last 5 years. Current use of tobacco or tobacco-containing products, recent history of alcohol or drug abuse OR positive urine screen for alcohol or controlled substances at screening or baseline. History &/or current evidence of serologic positive results for hepatitis B or C, or HIV. Donation or acute loss of 450 milliliters or more of blood or plasma, within 60 days of the study. Any subject who has received treatment with a non-FDA approved drug within 30 days of study screening. Subjects who suffer from claustrophobia. Current, past, or anticipated exposure to radiation in the workplace or participation in other research studies involving ionizing radiation that would exceed the yearly dose limits for normal subjects.

Ages Eligible for Study
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Minimum Age: 18 Years
Maximum Age: 55 Years

Sexes Eligible for Study
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Male

Accepts Healthy Volunteers
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Accepts Healthy Volunteers

Study Plan
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How is the study designed?
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Design Details

Primary Purpose: Basic Science
Allocation: Non-Randomized
Intervention Model: Single Group Assignment
Masking: None (Open Label)


Arms and Interventions

| Participant Group/Arm | Intervention/Treatment |
| --- | --- |
| Experimental: PART 1 (Test/Retest)<br>Dosing with [11C]TASP0410699 for PET imaging without dosing of TS-121 | Drug: [11C]TASP0410699<br>* Intravenous radiotracer<br>Radiation: Positron Emission Tomography (PET)<br>* Imaging scanning procedure<br>|
| Experimental: PART 2 (PET Receptor Occupancy Study)<br>Dosing with [11C]TASP0410699 for PET imaging with dosing of TS-121 | Drug: TS-121<br>* Oral<br>Drug: [11C]TASP0410699<br>* Intravenous radiotracer<br>Radiation: Positron Emission Tomography (PET)<br>* Imaging scanning procedure<br>|

What is the study measuring?
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Primary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Positron emission tomography measure (receptor occupancy) |  | Day 1 through Day 3 | 

Secondary Outcome Measures

| Outcome Measure | Measure Description | Time Frame |
| --- | --- | --- |
| Pharmacokinetic parameters of TS-121 | Area under the plasma concentration (AUC) from time zero to time of last measurable concentration | Day 1 through Day 3 | 
| Pharmacokinetic parameters of TS-121 | Maximum concentration (Cmax) | Day 1 through Day 3 | 
| Pharmacokinetic parameters of TS-121 | Time to attain cmax (Tmax) | Day 1 through Day 3 | 
| Composite safety as assessed by clinical laboratory tests, 12-lead ECG, vital signs, adverse events and physical examinations |  | up to Day 11 | 

 Terms related to the study
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Keywords Provided by Centre Hospitalier Valida
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PET, Receptor Occupancy