Clinical Study on Histamine H3 Receptor Occupancy of TS-091 by PET Examination in Healthy Adult Subjects

Phase 1 Completed 12 enrolled Taisho Pharmaceutical Co., Ltd.

Non-randomizedSingle-groupOpen-labelTreatment

Summary

To evaluate the following items by PET examination in Japanese heathy adult male subjects who received single oral administration of TS-091 in an unblinded manner. 1. Relationship between plasma concentration and H3 receptor-occupancy of TS-091 2. Time course changes in H3 receptor-occupancy of TS-091

Timeline

Start: 2014-12-11
Primary completion: 2015-12-16
Completion: 2015-12-16

Publications

Kimura Y, Takahata K, Shimazaki T, Kitamura S, Seki C, Ikoma Y, Ichise M, Kawamura K, Yamada M, Zhang MR, Higuchi M, Nishino I, Suhara T. Pharmacokinetic and pharmacodynamic assessment of histamine H3 receptor occupancy by enerisant: a human PET study with a novel H3 binding ligand, [11C]TASP457. Eur J Nucl Med Mol Imaging. 2022 Mar;49(4):1127-1135. doi: 10.1007/s00259-021-05571-1. Epub 2021 Oct 15.

Drugs

Evaluation	Drug	Modality	Dose	Route
Subject	TS-091	Unknown	0.1 mg	Oral
Subject	TS-091	Unknown	0.2 mg	Oral
Subject	TS-091	Unknown	0.4 mg	Oral
Subject	TS-091	Unknown	1 mg	Oral
Subject	TS-091	Unknown	5 mg	Oral
Subject	TS-091	Unknown	12.5 mg	Oral
Subject	TS-091	Unknown	25 mg	Oral

Indications

No indication recorded.