To Assess the Bioavailability of TK-254RX in Comparison with Oral Flurbiprofen Tablets and the Adhesion of TK-254RX in Healthy Subjects

NCT06823284 | Completed Phase 1 FDA Drug

• 2 other identifiers: TK-254RX-01022024-513058-31-00
• Study Type: interventional
• Target: 26
• Locations: 1 country
• Sites: 1

Brief Summary

This study is a single-center, open-label, multiple-dose trial performed in a 2-period, 2- sequence-cross-over design in healthy volunteers. The primary purpose of this study is to assess non-superiority of the bioavailability of TK-254RX compared with that of a marketed oral flurbiprofen-containing tablet formulation in healthy volunteers in a 2-period, 2- sequence-cross-over design and evaluate adhesion of TK-254RX. Secondary purpose is to assess safety of TK-254RX and residual amount of the patch.

Conditions

Healthy

Outcome Measures

Primary Outcomes (3)

• Area under the plasma concentration versus time curve over 24 hours of S-flurbiprofen for TK-254RX and tablet under steady-state conditions

  Day 5 to Day 6

• Peak Plasma Concentration of S-flurbiprofen for TK-254RX and tablet under steady-state conditions

  Day 5 to Day 6

• Characterization of patch adhesion

  Measuring patch adhesion area by percentage of visually by site staff with remaining patch adhered

  Day 1 to Day 6

Secondary Outcomes (34)

• Area under the plasma concentration versus time curve over 24 hours of S-flurbiprofen for TK-254RX on Day 1

  Day 1 to Day 2

• Peak Plasma Concentration of S-flurbiprofen for TK-254RX on Day 1

  Day 1 to Day 2

• Time to reach Peak Plasma Concentration of TK-254RX after the first two patches application on Day 1

  Day 1

• Time before first concentration value above the lower limit of quantitation of TK-254RX after the first two patches application on Day 1

  Day 1

• Trough concentration of TK-254RX

  24 hours, 48 hours, 72 hours, 96 hours, 120 hours after first TK-254RX application

Study Arms (2)

TK-254RX

EXPERIMENTAL

TK-254RX will be applied to left and right lower leg above ankle once daily over 5 consecutive days i.e. 10 patches will be applied totally.

Drug: Esflurbiprofen Topical System

Tablet (reference product)

EXPERIMENTAL

Tablets containing 100mg flurbiprofen will be administered three times daily (every 8 h) over 4 consecutive days i.e. 12 tablets will be administered totally.

Drug: Flurbiprofen tablet

Interventions

Esflurbiprofen Topical System DRUG

The total of two TK-254RX per day for 5 days (one patch applied to left and right lower leg above ankle)

TK-254RX

Flurbiprofen tablet DRUG

3 tablets per day for 4 days

Tablet (reference product)

Eligibility Criteria

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

You may qualify if:

• age: 18 years 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 3 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 triall

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, tolerability, absorption and/or pharmacokinetics 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
• fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency

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 14, Erfurt, 99084, Germany

Location

MeSH Terms

Interventions

Flurbiprofen

Intervention Hierarchy (Ancestors)

Propionates; Acids, Acyclic; Carboxylic Acids; Organic Chemicals; Biphenyl Compounds; Benzene Derivatives; Hydrocarbons, Aromatic; Hydrocarbons, Cyclic; Hydrocarbons

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: CROSSOVER
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: January 19, 2025
• First Posted: February 12, 2025
• Study Start: January 21, 2025
• Primary Completion: February 12, 2025
• Study Completion: February 24, 2025
• Last Updated: March 11, 2025

Record last verified: 2025-03

Data Sharing

• IPD Sharing: Will not share

Locations

DE (1)