To Assess the Effect of the Special Condition on the Pharmacokinetics and Tolerability of the Esflurbiprofen Topical System (EFTS) in Healthy Volunteers.

NCT06870422 | Completed Phase 1 FDA Drug

• 2 other identifiers: TK-254RX-01042024-513059-33-00
• Study Type: interventional
• Target: 28
• Locations: 1 country
• Sites: 1

Brief Summary

This study is a single-center, open-label, single-dose trial performed in a randomized, four-way, change-over design in healthy volunteers. The primary purpose of this study is to evaluate the effect of moderate heat, occlusion, and moderate exercise on pharmacokinetics. The secondary purpose is to characterize the effect of special conditions on the bioavailability and to evaluate patch adhesion and safety of TK-254RX and a residual amount of the patch.

Conditions

Healthy

Outcome Measures

Primary Outcomes (4)

• Assessing the effect of each intervention by Area under the plasma concentration versus time curve over 24 hours (AUC0-24) of S-flurbiprofen

  assessment of the effect of heat, occlusion, and moderate exercise on Test by use of AUC0-24 of S flurbiprofen

  Day 1 to Day 2 for each period

• Assessing the effect of each intervention by peak plasma concentration (Cmax) of S-flurbiprofen

  assessment of the effect of heat, occlusion, and moderate exercise on Test determined by use of Cmax of S flurbiprofen

  Day 1 to Day 2 for each period

• Assessing the effect of each intervention by area under the plasma concentration versus time curve from patch application to last measurement time point with a concentration value above lower limit of quantitation (AUC0-tlast) of S-flurbiprofen

  assessment of the effect of heat, occlusion, and moderate exercise on Test determined by use of AUC0-tlast of S flurbiprofen

  Day 1 to Day 4 for each period

• Assessing the effect of each intervention by area under the plasma concentration versus time curve from patch application to infinity (AUC0-inf) of S-flurbiprofen

  assessment of the effect of heat, occlusion, and moderate exercise on Test determined by use of AUC0-inf of S flurbiprofen

  Day 1 to Day 4 for each period

Secondary Outcomes (15)

• Assessing the effect of each intervention by area under the curve over 24 hours (AUC0-24)

  Day 1 to Day 2 for each period

• Assessing the effect of each intervention by peak plasma concentration (Cmax)

  Day 1 to Day 2 for each period

• Assessing the effect of each intervention by area under the plasma concentration versus time curve from patch application to last time point with a concentration value above lower limit of quantitation (AUC0-tlast)

  Day 1 to Day 4 for each period

• Assessing the effect of each intervention by area under plasma concentration versus time curve from patch application to infinity (AUC0-inf)

  Day 1 to Day 4 for each period

• Assessing the effect of each intervention by percentage of area under the plasma concentration versus time curve extrapolated to infinity to area under the plasma concentration versus time curve from 0 hour to infinity (AUCexpol%)

  Day 1 to Day 4 for each period

Study Arms (4)

TK-254RX

EXPERIMENTAL

TK-254RX will be applied with no special condition

Drug: Esflurbiprofen Topical System

TK-254RX with heat

EXPERIMENTAL

TK-254RX will be applied with moderate heat

Drug: Esflurbiprofen Topical System

TK-254RX with occlusion

EXPERIMENTAL

TK-254RX will be applied with occlusion

Drug: Esflurbiprofen Topical System

TK-254RX with exercise

EXPERIMENTAL

TK-254RX will be applied with 3 moderate exercise sessions

Drug: Esflurbiprofen Topical System

Interventions

Esflurbiprofen Topical System DRUG

TK-254RX will be applied for one day

TK-254RX; TK-254RX with exercise; TK-254RX with heat; TK-254RX with occlusion

Eligibility Criteria

• Age: 18 Years - 64 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• age: 18 to 64 years (inclusive)
• body-mass index (BMI): ≧18.5 kg/m² and ≦ 30.0 kg/m²
• good state of health
• non-smoker or ex-smoker for at least 6 months
• written informed consent, after having been informed about benefits and potential risks of the clinical trial, as well as details of the insurance taken out to cover the subjects participating in the clinical trial

You may not qualify if:

• existing cardiac and/or haematological diseases or pathological findings, which might interfere with the safety or tolerability of the active ingredient
• existing or history of hypertension and/or heart failure
• existing hepatic and/or renal diseases or pathological findings, which might interfere with the safety or tolerability, and/or pharmacokinetics of the active ingredient
• existing gastrointestinal diseases or pathological findings, which might interfere with the safety and tolerability of the active ingredient
• history of gastrointestinal bleeding or perforation related to previous NSAID therapy
• active, or history of ulcerative colitis, Crohn's disease, peptic ulceration or gastrointestinal haemorrhage
• existing metabolic, endocrine and/or immunologic diseases or pathological findings, which might interfere with the safety or tolerability, and/or pharmacokinetics of the active ingredient
• diabetes mellitus
• hyperlipidaemia (LDL \> 4.16 mmol/l, HDL \< 0.91 mmol/l, triglycerides \> 2.28 mmol/l, cholesterol \> 6.24 mmol/l)
• history of relevant CNS and/or psychiatric disorders and/or currently treated CNS and/or psychiatric disorders
• presence or history of acute or chronic diseases of the skin (e.g., atopic dermatitis (eczema), neurodermatitis, contact allergy, psoriasis, vitiligo, melanoma, squamous cell carcinoma), any dermatological condition or skin sensitivity which might interfere with the safety, tolerability, absorption and/or pharmacokinetics of the active ingredient
• existing or history of bronchial asthma
• known allergic reactions (e.g., bronchospasm, rhinitis, angioedema, or urticaria) to the active ingredients used, to acetylsalicylic acid or other NSAIDs, or to constituents of the pharmaceutical preparations
• history of severe allergies or multiple drug allergies unless it is judged as not relevant for the clinical trial by the investigator
• systolic blood pressure \< 90 or \> 139 mmHg

Sponsors & Collaborators

• Teikoku Seiyaku Co., Ltd.: lead
• SocraTec R&D GmbH: collaborator
• SocraMetrics GmbH: collaborator
• HWI pharma services GmbH: collaborator

Study Sites (1)

SocraTec R&D GmbH Clinical Pharmacology Unit

Mainzerhofplatz, Erfurt, 99084, Germany

Location

Study Officials

• Kenichi Nishiyama

  Teikoku Seiyaku Co., Ltd.

  STUDY CHAIR

Study Design

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

Study Record Dates

• First Submitted: March 6, 2025
• First Posted: March 11, 2025
• Study Start: February 28, 2025
• Primary Completion: April 3, 2025
• Study Completion: April 14, 2025
• Last Updated: April 22, 2025

Record last verified: 2025-04

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)