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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.
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| Label | Type | Description | Intervention Names |
|---|---|---|---|
| Single evaluation of H3 receptor occupancy | Experimental | Subjects received single-dose of 0.1, 0.2, 0.4, 1, 2.5, 25 mg TS-091 prior to an evaluation of H3 recepto occupancy |
|
| Multiple evaluations of H3 receptor occupancy | Experimental | Subjects received single-dose of 5, 12.5, 25 mg TS-091 prior to Multiple evaluations of H3 recepto occupancy |
|
| Name | Type | Description | Arm Group Labels | Other Names |
|---|---|---|---|---|
| TS-091 | Drug | Subjects received single-dose of 0.1, 0.2, 0.4, 1, 5, 12.5 and 25 mg of TS-091 (tablets or drug substance powder) |
|
| Measure | Description | Time Frame |
|---|---|---|
| H3 receptor occupancy | H3 receptor occupancy is calcurated at 2 hours after administration of TS-091. | 2 hours after administration of TS-091 |
| Changes in the H3 receptor occupancy | Changes in the H3 receptor occupancy is calcurated at 2, 6, and 26 hours after administration of TS-091 | 2, 6, and 26 hours after administration of TS-091 |
| Plasma concentration of unchanged TS-091 | Plasma concentration of unchanged TS-091 is calcurated at 2, 6, and 26 hours after administration of TS-091 | 2, 6, and 26 hours after administration of TS-091 |
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Inclusion Criteria:
Subjects who met all of the following criteria.
Exclusion Criteria:
Subjects who came under any of the following exclusion criteria.
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| Name | Affiliation | Role |
|---|---|---|
| Taisho Director | Taisho Pharmaceutical Co., Ltd. | Study Director |
| Facility | Status | City | State | ZIP | Country | Contacts |
|---|---|---|---|---|---|---|
| Taisho Pharmaceutical Co., Ltd selected site | Tokyo | Japan |
| PubMed Identifier | Type | Citation | Retractions |
|---|---|---|---|
| 34651222 | Derived | 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. |
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