Phase 1
Completed N=11
A Phase 1 Positron Emission Tomography Study to Measure Cholesterol 24S-Hydroxylase Target Occupancy of TAK-935
Epilepsy, Molecular Mechanisms of Pharmalogical Action, Protective Agents
Source: ClinicalTrials.gov NCT02497235 ↗
Enrolled (actual)
11
Serious AEs
0.0%
Results posted
Apr 2017
Primary outcomePrimary: Cholesterol 24S-Hydroxylase (CH24H) Brain Enzyme Occupancy as a Function of TAK-935 Plasma Concentration at 45 Minutes Post-TAK-935 Dose — NA; 98; NA percentage of occupancy
Summary
The purpose of this study is to determine the brain cholesterol 24S-hydroxylase (CH24H) enzyme occupancy of TAK-935 after single oral dose in healthy participants using the positron emission tomography (PET) ligand [18F]MNI-792 and PET imaging and to determine the relationship of occupancy to TAK-935 exposure.
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Cholesterol 24S-Hydroxylase (CH24H) Brain Enzyme Occupancy as a Function of TAK-935 Plasma Concentration at 45 Minutes Post-TAK-935 Dose |
NA; 98; NA | — |
| PRIMARY CH24H Brain Enzyme Occupancy as a Function of TAK-935 Plasma Concentration at 2 Hours Post-TAK-935 Dose |
70; 79; 96; 91; NA; 64 | — |
| PRIMARY CH24H Brain Enzyme Occupancy as a Function of TAK-935 Plasma Concentration at 10 Hours Post-TAK-935 Dose |
92; 87; NA | — |
| PRIMARY CH24H Brain Enzyme Occupancy as a Function of TAK-935 Plasma Concentration at 24 Hours Post-TAK-935 Dose |
22; 13; 79; 46; NA; 11 | — |
| SECONDARY Plasma Concentration of TAK-935 During Post-TAK-935 Dosing PET Scan Periods |
9.16; 11.3; 158; 56.2; 6.83; 3.79 | — |
| SECONDARY Percent Change From Baseline in the AUEC24 for Plasma 24S Hydroxycholesterol (24HC) |
-6.79; -14.82; -10.50; -12.41; -7.23; -13.38 | — |
Eligibility Criteria
Inclusion Criteria
- In the opinion of the investigator, is capable of understanding and complying with protocol requirements.
- Signs and dates a written, informed consent form and any required privacy authorization prior to the initiation of any study procedures including requesting that a participant fast for any laboratory evaluations.
- Is a healthy male or female and aged 19 to 55 years, inclusive, at the time of informed consent and first study medication dose.
- Weighs at least 45 kilogram (kg) and has a body mass index (BMI) from 18.0 to 30.0 kilogram per square meter (kg/m^2), inclusive at Screening.
- A female of non-bearing potential (example post-menopausal by history; or history of hysterectomy, bilateral salpingectomy, or oophorectomy).
Exclusion Criteria
- Have a known history or evidence of a clinically significant disorder (including neurologic and psychiatric), or disease that in the opinion of the study investigator would pose a risk to the participant safety or interfere with the study evaluation, procedures or completion.
- Contraindication to magnetic resonance imaging (MRI) based on the standard MRI radiography screening questionnaire.
- Had exposure to any radiation greater than (>) 15 millisievert (mSv)/year (example, occupational or radiation therapy) within the previous year prior to Baseline imaging.
- Has a known hypersensitivity to any component of the formulation of TAK-935 or related compounds, or to [18F]MNI-792 or to any of its components.
- Clinically significant abnormal findings on brain MRI scan or findings on brain MRI that may interfere with the interpretation of the PET imaging.
- Use of any over-the-counter, herbal, or prescription medications or supplements within 30 days prior to baseline imaging.
Data sourced from ClinicalTrials.gov (NCT02497235). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.