drugset / Trial / NCT04202497
A Study With [18F]MNI-1054 to Determine Lysine -Specific Demethylase 1A (LSD1) Brain Enzyme Occupancy of TAK-418 After Single-Dose Oral Administration in Healthy Participants
NaSingle-groupOpen-labelOther
Summary
The purpose of this study is to determine brain LSD1 enzyme occupancy and the relationship of occupancy to TAK-418 dose and plasma exposure after single oral dosing of TAK-418 in healthy participants using \[18F\]MNI-1054 positron emission tomography (PET) imaging.
Timeline
- Start
- 2019-12-18
- Primary completion
- 2020-03-05
- Completion
- 2020-03-19
Outcome
Outcome not reported
Stopped: “Study was prematurely terminated because of administrative reasons.”
Publications
- Schwarz AJ, Sandiego CM, Constantinescu C, Takano A, McQuade P, Tauscher J, Daegele N, Marek K, Gunn RN, Madonia J, Russell DS. [18F]MNI-1054, a novel PET ligand for lysine-specific histone demethylase 1 A (LSD1): first-in human validation and enzyme occupancy of the LSD1 inhibitor TAK-418. EJNMMI Res. 2026 Jul 3. doi: 10.1186/s13550-026-01477-x. Online ahead of print.
- Matsuda S, Hattori Y, Kimura H. Drug discovery strategy for TAK-418, a specific inhibitor of LSD1 enzyme activity, as a novel therapy for autism. Adv Pharmacol. 2025;102:267-300. doi: 10.1016/bs.apha.2024.10.017. Epub 2024 Oct 29.
Drugs
| Evaluation | Drug | Modality | Dose | Route |
|---|---|---|---|---|
| Subject | TAK-418 | Small molecule | 1.5 mg | Oral |
| Subject | TAK-418 | Small molecule | 10 mg | Oral |
| Subject | TAK-418 | Small molecule | 30 mg | Oral |
| Subject | [18F]MNI-1054 | Diagnostic / imaging agent | 370 mbq | Intravenous |
Indications
No indication recorded.