Clinical Pharmacology Study of Oral Edaravone in Healthy Adult Subjects (Food Effect Study)

To evaluate the effect of food on the pharmacokinetics of oral edaravone in healthy adult subjects. In this study, we determined 5 different dietary conditions including 4 different meal contents and fasting condition.

Study Overview

• Status: Completed
• Conditions: Healthy Adult Subjects
• Intervention / Treatment: Drug: MT-1186

• Study Type: Interventional
• Enrollment (Actual): 16
• Phase: Phase 1

Contacts and Locations

Study Locations

• Japan
  • Tokyo, Japan
    • Investigational Site

Participation Criteria

Eligibility Criteria

• Ages Eligible for Study: 20 years to 45 years (Adult)
• Accepts Healthy Volunteers: Yes

Description

Inclusion Criteria:

• Subjects who meet all of the following criteria and who have the capability of giving informed consent will be included in the study.

  1. Healthy adult male or female volunteers
  2. Japanese
  3. Subjects aged between 20 and 45 years at the time of informed consent
  4. Subjects who have thoroughly understood the contents of the study and voluntarily provided written informed consent to participate in the study

Exclusion Criteria:

• Subjects who met any of the following exclusion criteria between screening and investigational product administration were excluded from the study:

  1. Subjects with a current or previous history of cardiac, hepatic, renal, gastrointestinal, respiratory, psychiatric/nervous, hematopoietic, or endocrine diseases, and those whom the investigator (or subinvestigator) deems unsuitable for the study
  2. History of drug or food allergies
  3. History of alcohol or drug abuse or dependence
  4. Body mass index (BMI) of < 18.0 or > 30.0, or a body weight of < 50 kg [BMI formula: body weight (kg)/height (m)2, rounded to one decimal place]
  5. Positive test for any of the following at screening: hepatitis B surface (HBs) antigen, serological test for syphilis, hepatitis C virus (HCV) antibody, or human immunodeficiency virus (HIV) antigen/antibody
  6. Any clinically significant 12-lead ECG abnormality or corrected QT interval (QTc) using Fridericia's formula (QTcF) interval ≥ 450 msec
  7. Blood donation or sampling with a total volume of ≥ 400 mL within 12 weeks, ≥ 200 mL within 4 weeks, or ≥ 800 mL within one year before providing informed consent
  8. Blood component donation or blood sampling within 2 weeks before providing informed consent
  9. Subjects who have undergone any surgery known to affect the gastrointestinal absorption of drugs (except for appendectomy and herniotomy)
  10. Female subjects who do not agree to use an effective method of contraception from screening or 2 weeks before the start of investigational product administration, whichever comes earlier, to 14 days after the completion (or discontinuation) of investigational product administration. Male subjects who do not agree to use an effective method of contraception from the start of investigational product administration to 14 days after the completion (or discontinuation) of investigational product administration
  11. Subjects who have previously received edaravone
  12. Subjects who have participated in another clinical study and received an investigational product within 12 weeks before providing informed consent
  13. Subjects who have used any drugs other than the single use of acetylsalicylic acid within 7 days before the initiation of investigational product administration
  14. Use of any nutritional supplement(s) within 7 days before the initiation of investigational product administration
  15. Use of alcohol or any products containing xanthin or caffeine within 24 hours before screening and visit on Day -1
  16. Use of grapefruit, grapefruit juice, or any processed food(s) containing these substances within 24 hours before screening and visit on Day -1
  17. Use of any tobacco or nicotine-containing product(s) within 24 hours before screening and visit on Day -1
  18. Female subjects who have a positive pregnancy test at screening and on Day -1, are pregnant or breast feeding, or plan to get pregnant during the study
  19. Subjects judged by the investigator (or subinvestigator) to be unsuitable for the study for any other reason

Study Plan

How is the study designed?

Design Details

• Primary Purpose: Basic Science
• Allocation: Randomized
• Interventional Model: Crossover Assignment
• Masking: None (Open Label)

Number of Arms

4

Arms and Interventions

Participant Group / Arm	Intervention / Treatment
Experimental: Group A; A single oral dose of MT-1186 with fasted condition in period 1, meal 1 condition in period 2, meal 2 condition in period 3, meal 3 condition in period 4, and meal 4 condition in period 5.	Drug: MT-1186; A crossover study in which Japanese healthy subjects receive a single dose of MT-1186 under several dosing condition on Day 1, 3, 5, 7 and 24 according to their treatment sequence.; Other Names: Edaravone
Experimental: Group B; A single oral dose of MT-1186 with meal 1 condition in period 1, meal 2 condition in period 2, meal 3 condition in period 3, fasted condition in period 4, and meal 4 condition in period 5.	Drug: MT-1186; A crossover study in which Japanese healthy subjects receive a single dose of MT-1186 under several dosing condition on Day 1, 3, 5, 7 and 24 according to their treatment sequence.; Other Names: Edaravone
Experimental: Group C; A single oral dose of MT-1186 with meal 2 condition in period 1, meal 3 condition in period 2, fasted condition in period 3, meal 1 condition in period 4, and meal 4 condition in period 5.	Drug: MT-1186; A crossover study in which Japanese healthy subjects receive a single dose of MT-1186 under several dosing condition on Day 1, 3, 5, 7 and 24 according to their treatment sequence.; Other Names: Edaravone
Experimental: Group D; A single oral dose of MT-1186 with meal 3 condition in period 1, fasted condition in period 2, meal 1 condition in period 3, meal 2 in period 4, and meal 4 condition in period 5.	Drug: MT-1186; A crossover study in which Japanese healthy subjects receive a single dose of MT-1186 under several dosing condition on Day 1, 3, 5, 7 and 24 according to their treatment sequence.; Other Names: Edaravone

What is the study measuring?

Primary Outcome Measures

Outcome Measure	Time Frame
Area Under the Concentration Versus Time Curve From Zero up to Infinity (AUC0-inf) of Edaravone	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Maximum Plasma Concentration (Cmax) of Edaravone	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
AUC0-inf of Sulfate Conjugate and Glucuronide Conjugate	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Cmax of Sulfate Conjugate and Glucuronide Conjugate	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Time to Reach Maximum Plasma Concentration (Tmax) of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Terminal Elimination Half-life (t1/2) of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Apparent Terminal Elimination Rate Constant (Kel) of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Mean Residence Time (MRT) of Unchanged Edaravone	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Apparent Total Clearance (CL/F) of Unchanged Edaravone	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Apparent Distribution Volume at Elimination Phase (Vz/F) of Unchanged Edaravone	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Apparent Distribution Volume at Steady State (Vss/F) of Unchanged Edaravone	Before administration, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 4, 6, 8, 10, 12, 24, 36 and 48 hours after administration
Cumulative Urinary Excretion Amount (Ae 0-24h) of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate	Day 1 to 9, Day 24 to 26
Urinary Excretion Ratio (Ae% 0-24h) of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate	Day 1 to 9, Day 24 to 26
Renal Clearance (CLr) of Unchanged Edaravone	Day 1 to 9, Day 24 to 26

Secondary Outcome Measures

Outcome Measure	Time Frame
Number of Participants With Adverse Events and Adverse Drug Reactions	Day 1 to Day 31

Collaborators and Investigators

• Sponsor: Tanabe Pharma Corporation
• Investigators: Study Director: General Manager, Tanabe Pharma Corporation

Publications and helpful links

General Publications

• Shimizu H, Nishimura Y, Shiide Y, Akimoto M, Matsuda H, Kato Y, Hirai M. Food Effect Study to Assess the Impact on Edaravone Pharmacokinetic Profiles in Healthy Participants. Clin Ther. 2022 Dec;44(12):1552-1565. doi: 10.1016/j.clinthera.2022.10.001. Epub 2022 Nov 12.

Study record dates

Study Major Dates

• Study Start (Actual): June 10, 2019
• Primary Completion (Actual): July 24, 2019
• Study Completion (Actual): July 24, 2019

Study Registration Dates

• First Submitted: April 19, 2022
• First Submitted That Met QC Criteria: April 19, 2022
• First Posted (Actual): April 22, 2022

Study Record Updates

• Last Update Posted (Actual): May 22, 2026
• Last Update Submitted That Met QC Criteria: May 21, 2026
• Last Verified: May 1, 2026

More Information

Terms related to this study

• Additional Relevant MeSH Terms: Heterocyclic Compounds, 1-Ring; Heterocyclic Compounds; Azoles; Pyrazoles; Antipyrine; Pyrazolones; Edaravone
• Other Study ID Numbers: MT-1186-J06

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: Yes
• Studies a U.S. FDA-regulated device product: No