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

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

Study Overview

• Status: Completed
• Conditions: Healthy Subjects
• Intervention / Treatment: Drug: TS-091

• Study Type: Interventional
• Enrollment (Actual): 12
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Tokyo, Japan
    • Taisho Pharmaceutical Co., Ltd selected site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 39 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

Subjects who met all of the following criteria.

• Age: between ≥20 years and <40 years at the time of providing written consent for participation in the study.
• Body mass index (BMI): ≥18.5 and <25.0 on the day of screening test.
• Subject who received a prior explanation on the study and was able to understand its content and capable of providing voluntary written consent for participation in the study.
• Other protocol defined inclusion criteria could apply-

Exclusion Criteria:

Subjects who came under any of the following exclusion criteria.

• Subjects who were considered to have some disease and not healthy by the investigator or subinvestigator according to his medical judgment based on the results of screening test
• Subjects with a drug or food allergy or a history thereof.
• Subjects with a significant allergic disposition (e.g. asthma requiring treatment) or a history thereof.
• Subjects with a history of heparin-induced thrombocytopenia.
• Other protocol defined exclusion criteria could apply

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Treatment
• Allocation: Non-Randomized
• Interventional Model: Single Group Assignment
• Masking: None (Open Label)

Number of Arms

2

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Single evaluation of H3 receptor occupancy; 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	Drug: TS-091; 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)
Experimental: Multiple evaluations of H3 receptor occupancy; Subjects received single-dose of 5, 12.5, 25 mg TS-091 prior to Multiple evaluations of H3 recepto occupancy	Drug: TS-091; 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)

What is the study measuring?

Primary Outcome Measures

Outcome Measure	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

Collaborators and Investigators

• Sponsor: Taisho Pharmaceutical Co., Ltd.
• Investigators: Study Director: Taisho Director, Taisho Pharmaceutical Co., Ltd.

Publications and helpful links

General 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.

Study record dates

Study Major Dates

• Study Start (Actual): December 11, 2014
• Primary Completion (Actual): December 16, 2015
• Study Completion (Actual): December 16, 2015

Study Registration Dates

• First Submitted: November 12, 2020
• First Submitted That Met QC Criteria: November 12, 2020
• First Posted (Actual): November 17, 2020

Study Record Updates

• Last Update Posted (Actual): March 25, 2025
• Last Update Submitted That Met QC Criteria: February 26, 2025
• Last Verified: November 1, 2020

More Information

Terms related to this study

• Other Study ID Numbers: TS091-1402

Plan for Individual participant data (IPD)

• Plan to Share Individual Participant Data (IPD)?: NO

Drug and device information, study documents

• Studies a U.S. FDA-regulated drug product: No
• Studies a U.S. FDA-regulated device product: No
• product manufactured in and exported from the U.S.: No