Phase 1
Completed N=42
Bioequivalence Study of Oral Suspension and Intravenous Formulation of Edaravone in Healthy Adult Subjects
Healthy Adult Subjects
Source: ClinicalTrials.gov NCT04493281 ↗
Enrolled (actual)
42
Serious AEs
0.0%
Results posted
Jan 2024
Primary outcomePrimary: Area Under the Plasma Concentration Versus Time Curve From Time Zero up to the Last Quantifiable Concentration Time-point (AUC0-t) of Unchanged Edaravone After Oral and Intravenous Administration — 1743; 1720 ng·h/mL
Summary
To evaluate the single-dose bioequivalence of oral suspension and intravenous (IV) formulation of edaravone in the fasting state in healthy adult subjects
Outcome Measures
| Outcome | Result | p-value |
|---|---|---|
| PRIMARY Area Under the Plasma Concentration Versus Time Curve From Time Zero up to the Last Quantifiable Concentration Time-point (AUC0-t) of Unchanged Edaravone After Oral and Intravenous Administration |
1743; 1720 | — |
| PRIMARY Area Under the Plasma Concentration Versus Time Curve From Time Zero up to Infinity With Extrapolation of the Terminal Phase (AUC0-inf) of Unchanged Edaravone After Oral and Intravenous Administration |
1762; 1736 | — |
| PRIMARY Maximum Plasma Concentration (Cmax) of Unchanged Edaravone After Oral and Intravenous Administration |
1656; 1253 | — |
| SECONDARY Time to Reach Maximum Plasma Concentration (Tmax) |
0.50; 1.00; 0.75; 1.08; 0.75; 1.08 | — |
| SECONDARY Area Under the Plasma Concentration Versus Time Curve From Time Zero up to 24 Hours (AUC0-24) |
1735; 1714; 19837; 14830; 3917; 2288 | — |
| SECONDARY Area Under the Plasma Concentration Versus Time Curve From Time Zero up to the Last Sampling Time-point (for All Time-points) (AUC0-all) |
1752; 1727; 20035; 15025; 3927; 2297 | — |
| SECONDARY Terminal Elimination Half-life (t1/2) |
9.75; 8.82; 5.77; 7.58; 3.75; 3.69 | — |
| SECONDARY Elimination Rate Constant From the Central Compartment (Kel) |
0.1194; 0.1156; 0.1295; 0.1010; 0.1909; 0.1924 | — |
| SECONDARY Mean Residence Time From Time Zero up to Infinity With Extrapolation of the Terminal Phase (MRT0-inf) of Unchanged Edaravone |
2.495; 2.333 | — |
| SECONDARY Total Clearance (CL) of Unchanged Edaravone After Intravenous Administration |
35.9 | — |
| SECONDARY Volume of Distribution During Terminal Phase (Vz) of Unchanged Edaravone After Intravenous Administration |
418 | — |
| SECONDARY Volume of Distribution at Steady State (Vss) of Unchanged Edaravone After Intravenous Administration |
63.1 | — |
| SECONDARY Apparent Total Clearance (CL/F) of Unchanged Edaravone After Oral Administration |
67.9 | — |
| SECONDARY Apparent Volume of Distribution During Terminal Phase (Vz/F) of Unchanged Edaravone After Oral Administration |
826 | — |
| SECONDARY Apparent Volume of Distribution at Steady State (Vss/F) of Unchanged Edaravone After Oral Administration |
164.0 | — |
| SECONDARY Cumulative Amount of Drug Excreted in Urine From Time Zero up to 48 Hours (Ae0-48) |
0.66; 0.52; 10.04; 7.06; 125.9; 94.3 | — |
| SECONDARY Cumulative Percentage of Drug Excreted in Urine From Time Zero up to 48 Hours (Ae0-48) |
0.629; 0.869; 6.58; 8.09; 59.8; 78.4 | — |
| SECONDARY Renal Clearance (CLr) of Unchanged Edaravone |
0.424; 0.311 | — |
| SECONDARY Bioavailability (F) of Unchanged Edaravone After Oral Administration |
57.3 | — |
| SECONDARY AUC0-t of Sulfate and Glucuronide Conjugates After Oral and Intravenous Administration |
20031; 15024; 3914; 2285 | — |
| SECONDARY AUC0-inf of Sulfate and Glucuronide Conjugates After Oral and Intravenous Administration |
20055; 15055; 3924; 2295 | — |
| SECONDARY Cmax of Sulfate and Glucuronide Conjugates After Oral and Intravenous Administration |
7291; 4843; 2237; 1012 | — |
| SECONDARY Number of Participants With Adverse Events and Adverse Drug Reactions |
1; 1; 0; 0 | — |
Eligibility Criteria
Inclusion Criteria
- Healthy adult male or female volunteers
- Japanese
- 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
- 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
- Subjects who have previously received edaravone
- Subjects who have participated in another clinical study and received an investigational product within 12 weeks before providing informed consent
Data sourced from ClinicalTrials.gov (NCT04493281). 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.