NCT02716987

Study to Determine D-amino Acid Oxidase Brain Enzyme Occupancy of TAK-831 After Single-dose Oral Administration

A Phase 1, Open-Label, Positron Emission Tomography Study in Healthy Subjects to Determine D-Amino Acid Oxidase Brain Enzyme Occupancy of TAK-831 After Single-Dose Oral Administration in Healthy Subjects

• Status: Completed
• Phase: Phase 1
• Study type: Interventional
• Enrollment: 20 (actual)
• Sponsor: Neurocrine Biosciences · Industry
• Sex: Male
• Age: 25 Years – 55 Years
• Healthy volunteers: Accepted

Summary

The purpose of this study is to determine the relationship between TAK-831 dose, plasma exposure, extent and duration of brain D-amino acid oxidase (DAO) enzyme occupancy following single oral dosing of TAK-831 in healthy participants.

Detailed description

The drug being tested in this study is called TAK-831. TAK-831 is a highly selective and potent inhibitor of DAO, a peroxisomal enzyme active towards neutral D-amino acids which potentially effects cerebellar dysfunction. This study will look at the relationship between TAK-831 plasma exposure and the extent and duration of brain DAO enzyme occupancy after single oral dosing of TAK-831 in healthy male participants using \[18F\]PGM299 radioactive tracer injection and PET imaging. The study will enroll up to 22 participants in two different sets. Up to 16 participants will be enrolled in Set A. Within that total, up to 5 dose levels of TAK-831 may be evaluated, with up to 6 participants per dose level, although typically, there will be 2 to 3 participants per dose level. All participants in Set A will also receive up to 3 doses of \[18F\]PGM299. Up to 6 participants will be enrolled in Set B. All participants in Set B will be assigned to single treatment group to receive 2 doses of \[18F\]PGM299. All participants in Set A will be asked to take single oral dose of TAK-831 suspension on Day 1. In Set A, each of the participant will receive a maximum of 3 PET scans with \[18F\]PGM299; 1 at baseline 2 following a single oral dose of TAK-831 on Days 1 and 2. In Set B, each of the participant will receive 2 PET scans with \[18F\]PGM299 on Days 1 and 10. Set B will be conducted after the confirmation of blockade of \[18F\]PGM299 binding by TAK-831 in 2 to 4 participants of Set A. This multi-center trial will be conducted in the United Kingdom. The overall time to participate in this study is 62 days. Participants in Set A will make 4 visits to the clinic, and participants in Set B will make 3 visits to the clinic and all will be contacted by telephone on Day 15 (Set A) and Day 12 (Set B) of treatment period for a follow-up assessment.

Conditions

• Healthy

Interventions

Type	Name	Description
DRUG	TAK-831	TAK-831 oral suspension.
DRUG	[18F]PGM299	\[18F\]PGM299 injection

Timeline

• Start date: 2016-03-21
• Primary completion: 2016-08-30
• Completion: 2016-08-30
• First posted: 2016-03-23
• Last updated: 2021-06-14
• Results posted: 2020-08-07

Locations

1 site across 1 country: United Kingdom