Phase 1 Completed N=78 Other

Clinical Pharmacology Study of Oral Edaravone in Healthy Adult Males (Drug Interaction Study and Preliminary Regimen-Finding Study)

Healthy Adult Subjects

Source: ClinicalTrials.gov NCT04481789 ↗

Enrolled (actual)

Serious AEs

0.0%

Results posted

Aug 2024

Primary outcomePrimary: Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of Rosuvastatin, Sildenafil and Furosemide. — 161; 165; 532; 482 ng*h/mL

Summary

* Cohort 1: To evaluate the drug interactions, safety, and tolerability of oral edaravone when coadministered with rosuvastatin, sildenafil or furosemide in healthy adult males * Cohort 2: To evaluate the pharmacokinetics, safety, and tolerability of oral edaravone in healthy Japanese and Caucasian adult males

Outcome Measures

Outcome	Result	p-value
PRIMARY Area Under the Concentration Versus Time Curve From Time Zero to Infinity (AUC0-inf) of Rosuvastatin, Sildenafil and Furosemide.	161; 165; 532; 482; 3861; 3906	—
PRIMARY Maximum Plasma Concentration (Cmax) of Rosuvastatin, Sildenafil and Furosemide.	11.3; 11.3; 232; 201; 1676; 1701	—
PRIMARY Tmax of Rosuvastatin, Sildenafil and Furosemide.	4.6; 5.1; 0.8; 0.9; 1.7; 1.8	—
PRIMARY T1/2 of Rosuvastatin, Sildenafil and Furosemide.	14.4; 12.1; 2.8; 3.5; 6.9; 5.8	—
PRIMARY AUC0-inf of Unchanged Edaravone.	1647; 1475; 1247	—
PRIMARY Cmax of Unchanged Edaravone.	1810; 1502; 1012	—
PRIMARY Tmax of Unchanged Edaravone.	0.4; 0.4; 0.67; 0.67; 0.53; 0.61	—
PRIMARY T1/2 of Unchanged Edaravone.	9.3; 16.2; 10.5; 10.7; 4.3; 4.4	—
PRIMARY AUC0-inf of Sulfate Conjugate.	26576; 30588	—
PRIMARY Cmax of Sulfate Conjugate.	8115; 8702	—
PRIMARY Tmax of Sulfate Conjugate.	0.76; 0.81	—
PRIMARY T1/2 of Sulfate Conjugate.	3.89; 4.20	—
PRIMARY AUC0-inf of Glucuronide Conjugate.	4817; 4953	—
PRIMARY Cmax of Glucuronide Conjugate.	2318; 2304	—
PRIMARY Tmax of Glucuronide Conjugate.	0.61; 0.57	—
PRIMARY T1/2 of Glucuronide Conjugate.	4.26; 4.35	—
PRIMARY AUC0-inf of Unchanged Edaravone.	1647; 1475; 1247	—
PRIMARY Cmax of Unchanged Edaravone.	1810; 1502; 1012	—
PRIMARY Tmax of Unchanged Edaravone.	0.4; 0.4; 0.67; 0.67; 0.53; 0.61	—
PRIMARY T1/2 of Unchanged Edaravone.	9.3; 16.2; 10.5; 10.7; 4.3; 4.4	—
PRIMARY AUCinf of Sulfate Conjugate and Glucuronide Conjugate.	24484; 22689; 23022; 4178; 4099; 3557	—
PRIMARY Cmax of Sulfate Conjugate and Glucuronide Conjugate.	8394; 7802; 8152; 2391; 2176; 1924	—
PRIMARY Tmax of Sulfate Conjugate and Glucuronide Conjugate.	0.67; 0.91; 0.72; 0.53; 0.76; 0.72	—
PRIMARY T1/2 of Sulfate Conjugate and Glucuronide Conjugate.	10.50; 7.53; 7.55; 4.26; 3.89; 3.88	—
PRIMARY T1/2 of Glucuronide Conjugate.	4.26; 4.35	—
PRIMARY Number of Participants With Adverse Events and Adverse Drug Reactions	0; 2; 0; 6; 3; 8	—
SECONDARY AUCinf of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate.	1647; 1423; 24484; 20098; 4178; 3795	—
SECONDARY Cmax of Unchanged Edaravone, Sulfate Conjugate and Glucuronide Conjugate.	1810; 1484; 8394; 6530; 2391; 2136	—
SECONDARY Tmax of Unchanged Edaravone.	0.4; 0.4; 0.67; 0.67; 0.53; 0.61	—
SECONDARY T1/2 of Unchanged Edaravone.	9.3; 16.2; 10.5; 10.7; 4.3; 4.4	—

Eligibility Criteria

Inclusion Criteria

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

Exclusion Criteria

Additional screening criteria check may apply for qualification:

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
Body mass index (BMI) of 30.0, or body weight of <50 kg (BMI formula: body weight [kg]/height [m]2, rounded to one decimal place)
Subjects who have undergone any surgery known to affect the gastrointestinal absorption of drugs
Subjects who do not agree to use an effective method of contraception from initiation of study drug administration to 14 days after completion (discontinuation) of study drug administration
Subjects who have previously received edaravone
Subjects who have participated in another clinical study and received a study drug within 12 weeks before providing informed consent
Use of any drug(s) other than the study drug or as-needed use of acetylsalicylic acid within 7 days before the initiation of study drug or victim drug administration
Use of any alcohol, xanthine, or caffeine-containing product(s) within 24 hours before screening and Day -1 visiting
Use of any supplement(s) within 7 days before the initiation of study drug or victim drug administration
Use of grapefruit, grapefruit juice, or any processed food(s) containing these substances during the following periods (Cohort 1: within 7 days before the initiation of victim drug administration, Cohort 2: within 24 hours before each Day -1 visiting)
Use of any tobacco or nicotine-containing product(s) (Cohort 1: within 12 weeks before the initiation of victim drug administration during the following periods, Cohort 2: within 24 hours before each Day -1 visiting)
Use of any health food(s) containing St John's Wort (Hypericum perforatum) within 2 weeks before the initiation of victim drug administration (only in Cohort 1)

View full record on ClinicalTrials.gov →

Data sourced from ClinicalTrials.gov (NCT04481789). Outcome figures and adverse-event rates are extracted automatically from the registry's posted results and are provided for clinician reference, not as a substitute for the primary publication. Informational only — not medical advice.