A Single and Multiple Dose Study of Dotinurad in Chinese Healthy Participants

NCT05278676 | Completed Phase 1

• 1 other identifier: FYU-981-J086-001
• Study Type: interventional
• Target: 26
• Locations: 1 country
• Sites: 1

Brief Summary

The primary purpose of this study is to evaluate the pharmacokinetics (PK) of dotinurad following single and multiple oral doses of dotinurad in Chinese healthy male and female participants.

Conditions

Healthy Volunteers

Outcome Measures

Primary Outcomes (23)

• Single-dose Part, Cmax: Maximum Observed Concentration for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, Tmax: Time at Which the Highest Drug Concentration Occurs for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, t1/2: Terminal Elimination Phase Half-life for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, AUC0-t: Area Under the Concentration-time Curve From Zero Time to Time of Last Quantifiable Concentration for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, AUC0-24h: Area Under the Concentration-time Curve From Zero Time to 24 hours for Dotinurad

  Day 1: 0-24 hours post dose

• Single-dose Part, AUC0-inf: Area Under the Concentration-time Curve From Zero Time Extrapolated to Infinite Time for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, CL/F: Apparent Total Clearance Following Oral Administration for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, Vz/F: Apparent Volume of Distribution at Terminal Phase for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, kel: Elimination Rate Constant for Dotinurad

  Day 1: 0-48 hours post dose

• Single-dose Part, MRT0-t: Mean Residence Time From Zero Time to Time of Last Quantifiable Concentration on Single Dose for Dotinurad

  Day 1: 0-48 hours post dose

• Multiple-dose Part, Css,max: Maximum Observed Concentration at Steady State for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, Css,min: Minimum Observed Concentration at Steady State for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, Css,av: Average Steady-state Concentration for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, tss,max: Time at Which the Highest Drug Concentration Occurs at Steady State for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, t1/2: Terminal Elimination Phase Half-life for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, AUC0-τ: Area Under the Concentration-time Curve Over the Dosing Interval on Multiple Dosing for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, CLss/F: Apparent Total Clearance Following Oral Administration at Steady State for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, Vz/F: Apparent Volume of Distribution at Terminal Phase for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, kel: Elimination Rate Constant for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, MRT: Mean Residence Time for Dotinurad

  Day 10: 0-72 hours post dose

• Multiple-dose Part, Rac(AUC0-24h): Accumulation Ratio for AUC(0-24h)

  Day 10: 0-24 hours post dose

• Multiple-dose Part, Rac(Cmax): Accumulation Ratio for Cmax

  Day 10: 0-72 hours post dose

• Multiple-dose Part, PTF: Peak-trough Fluctuation

  Day 10: 0-72 hours post dose

Study Arms (3)

Cohort A Single Dose: Dotinurad

EXPERIMENTAL

Participants will receive dotinurad 1 milligram (mg) (1\*1 mg tablet) as a single oral dose after 10-hour fasting on Day 1 in the morning.

Drug: Dotinurad

Cohort B Multiple Dose: Dotinurad

EXPERIMENTAL

Participants will receive dotinurad 4 mg (2\*2 mg tablets) as a single oral dose after 10-hour fasting on Day 1 in the morning. A washout period of 3 days will be maintained after single dose on Day 1 and then participants will receive dotinurad 4 mg (2\*2 mg tablets) after 10-hour fasting from Day 4 to Day 10 once daily in the morning.

Drug: Dotinurad

Cohort C Single Dose: Dotinurad

EXPERIMENTAL

Participants will receive dotinurad 10 mg (5\*2 mg tablets) as a single oral dose after 10-hour fasting on Day 1 in the morning.

Drug: Dotinurad

Interventions

Dotinurad DRUG

Dotinurad oral tablet.

Also known as: FYU-981

Cohort A Single Dose: Dotinurad; Cohort B Multiple Dose: Dotinurad; Cohort C Single Dose: Dotinurad

Eligibility Criteria

• Age: 18 Years - 45 Years
• Sex: all
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• Healthy Chinese participants living in China.
• Non-smoking, male or female, age greater than or equal to (\>=) 18 years and less than or equal to (\<=) 45 years old at the time of informed consent.
• Participants with serum uric acid level less than \>=5.5 milligrams per decilitre (mg/dL) at Screening (Cohort B only).

You may not qualify if:

• Females who are breastfeeding or pregnant at Screening or Baseline (as documented by a positive beta-human chorionic gonadotropin \[β-hCG\] or human chorionic gonadotropin \[hCG\] test). A separate baseline assessment of serum β-hCG (or hCG) or urine pregnancy test is required if a negative screening pregnancy test was obtained more than 72 hours before the first dose of study drug.
• Females of childbearing potential.
• Clinically significant illness that requires medical treatment within 8 weeks or a clinically significant infection that requires medical treatment within 4 weeks of dosing.
• Evidence of disease that may influence the outcome of the study within 4 weeks before dosing; example, psychiatric disorders and disorders of the gastrointestinal tract, liver, kidney, respiratory system, endocrine system, hematological system, neurological system, or cardiovascular system, or participants who have a congenital abnormality in metabolism.
• Any history of gastrointestinal surgery that may affect PK profiles of dotinurad, example, hepatectomy, nephrectomy, digestive organ resection at Screening.

Sponsors & Collaborators

• Eisai Co., Ltd.: lead

Study Sites (1)

Shanghai Xuhui District Central Hospital

Shanghai, China

Location

Related Publications (1)

• Liu Y, Chen Q, Sun H, Cai C, Kawamura K, Kokan R, Nomoto M. A Single- and Multiple-Dose Study to Characterize the Pharmacokinetics and Safety of Dotinurad in Healthy Chinese Adults. Clin Drug Investig. 2025 Dec;45(12):957-966. doi: 10.1007/s40261-025-01496-x. Epub 2025 Oct 19.

  PMID: 41111126 DERIVED

MeSH Terms

Interventions

dotinurad

Study Design

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

Study Record Dates

• First Submitted: February 18, 2022
• First Posted: March 14, 2022
• Study Start: July 1, 2022
• Primary Completion: December 13, 2022
• Study Completion: December 13, 2022
• Last Updated: September 14, 2023

Record last verified: 2023-02

Data Sharing

• IPD Sharing: Will share

Locations

CN (1)