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

NCT04631276 | Completed Phase 1

• 1 other identifier: TS091-1402
• Study Type: interventional
• Target: 12
• Locations: 1 country
• Sites: 1

Brief 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. 1.Relationship between plasma concentration and H3 receptor-occupancy of TS-091
2. 2.Time course changes in H3 receptor-occupancy of TS-091

Conditions

Healthy Subjects

Outcome Measures

Primary Outcomes (3)

• 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

Study Arms (2)

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

Drug: TS-091

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

Drug: TS-091

Interventions

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)

Multiple evaluations of H3 receptor occupancy; Single evaluation of H3 receptor occupancy

Eligibility Criteria

• Age: 20 Years - 39 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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.

You may not qualify if:

• 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.

Sponsors & Collaborators

• Taisho Pharmaceutical Co., Ltd.: lead

Study Sites (1)

Taisho Pharmaceutical Co., Ltd selected site

Tokyo, Japan

Location

Related Publications (1)

• 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.

  PMID: 34651222 DERIVED

Study Officials

• Taisho Director

  Taisho Pharmaceutical Co., Ltd.

  STUDY DIRECTOR

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NON RANDOMIZED
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: November 12, 2020
• First Posted: November 17, 2020
• Study Start: December 11, 2014
• Primary Completion: December 16, 2015
• Study Completion: December 16, 2015
• Last Updated: February 28, 2025

Record last verified: 2020-11

Data Sharing

• IPD Sharing: Will not share

Locations

JP (1)