A Study to Determine the Metabolism and Elimination of [14C]E2027 in Healthy Male Participants
Study Details
Study Description
Brief Summary
The primary objective of the study is to achieve mass balance recovery of [14C]-radiolabel in urine and feces and to identify and quantify the main elimination pathways of E2027.
| Condition or Disease | Intervention/Treatment | Phase |
|---|---|---|
| Phase 1 |
Study Design
Arms and Interventions
| Arm | Intervention/Treatment |
|---|---|
| Experimental: E2027 Participants will receive approximately 130 microcurie (μCi) of [14C]E2027 as a single 50 milligram (mg) (free base), capsule, orally on Day 1. |
Drug: E2027
E2027 oral capsule.
|
Outcome Measures
Primary Outcome Measures
- Cumulative Percent of the Radiolabeled Dose of [14C]E2027 in Biological Matrices (Blood, Urine, Feces and Toilet Tissue) [Up to 56 days]
Blood, urine, feces and toilet tissue samples will be collected at specific time points and will be analyzed for the amount of radiolabeled [14C]E2027.
- Maximum Concentration (Cmax) of Radiolabeled [14C]E2027, Non-Radiolabeled E2027 and Metabolites in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Time to Reach Maximum (Peak) Concentration (Tmax) of Radiolabeled [14C]E2027, Non-Radiolabeled E2027 and Metabolites in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Area Under the Concentration-Time Curve From Time Zero to 24 hours (AUC(0-24h)) of Radiolabeled [14C]E2027, Non-Radiolabeled E2027 and Metabolites in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Area Under the Concentration-Time Curve From Time Zero to Time of Last Measurable Concentration (AUC(0-t)) of Radiolabeled [14C]E2027, Non-Radiolabeled E2027 and Metabolites in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Area Under the Concentration-Time Curve From Time Zero to Infinity (AUC(0-inf)) of Radiolabeled [14C]E2027, Non-Radiolabeled E2027 and Metabolites in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Terminal Elimination Half-life (t1/2) of Radiolabeled [14C]E2027, Non-Radiolabeled E2027 and Metabolites in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Apparent Total Body Clearance (CL/F) of E2027 in Biological Matrices [Pre-dose up to Day 56 post-dose]
- Apparent Volume of Distribution (Vd/F) of E2027 in Biological Matrices [Pre-dose up to Day 28 post-dose]
- Percent of AUC(0-inf) of Metabolite to E2027 in Biological Matrices [Pre-dose up to Day 28 post-dose]
Secondary Outcome Measures
- Number of Participants With Adverse Events (AEs) and Serious Adverse Events (SAEs) [Up to 56 days post-dose]
- Number of Participants With Clinically Significant Abnormal Laboratory Values [Up to 56 days post-dose]
- Number of Participants With Clinically Significant Abnormal Vital Sign Values [Up to 56 days post-dose]
- Number of Participants With Clinically Significant Abnormal Electrocardiogram (ECG) Findings [Up to 56 days post-dose]
- Number of Participants With Clinically Significant Abnormal Physical Examination Findings [Baseline, Up to 56 days post-dose]
Eligibility Criteria
Criteria
Inclusion Criteria:
Participants must meet all of the following criteria to be included in this study:
- Body Mass Index (BMI) of 18 to 30 kilogram per square meter (kg/m^2) at Screening
Exclusion Criteria
Participants who meet any of the following criteria will be excluded from this study:
-
Have participated in a [14C]-research study within the 6 months prior to Day -1
-
Exposure to clinically significant radiation (greater than [>] 100 millisieverts) within 12 months prior to Day -1
-
Clinically significant illness that required medical treatment within 8 weeks or a clinically significant infection that required medical treatment within 4 weeks before dosing
-
Any history of abdominal surgery that may affect pharmacokinetic profiles of study drug (example, hepatectomy, nephrectomy, digestive organ resection but not cholecystectomy nor appendectomy) at Screening or Baseline
-
Any other clinically abnormal symptom or organ impairment found by medical history, physical examinations, vital signs, ECG finding (including PR > 210 millisecond [msec], QRS > 110 msec), or laboratory test results that required medical treatment at Screening or Baseline
-
A prolonged QT/QTc interval (QTcF > 450 msec) as demonstrated by ECGs at Screening or Baseline
-
Systolic blood pressure > 130 millimetres of mercury (mmHg) or diastolic blood pressure > 85 mmHg at Screening or Baseline
-
Heart rate less than (<) 45 beats per minute (beats/min) or >100 beats/min at Screening or Baseline
-
Known history of clinically significant drug allergy at Screening or Baseline
-
Known history of food allergies or presently experiencing significant seasonal or perennial allergy at Screening or Baseline
-
Known to be human immunodeficiency virus (HIV) positive at Screening
-
Active viral hepatitis (A, B, or C) as demonstrated by positive serology at Screening
-
History of drug or alcohol dependency or abuse within the 2 years before Screening, or those who have a positive urine drug or alcohol test at Screening or Baseline
-
Use of tobacco or nicotine-containing products within 4 weeks before dosing
-
Currently enrolled in another clinical trial or used any investigational drug or device within 30 days (or 5 half-lives, whichever is longer) preceding informed consent
-
Engagement in strenuous exercise within 2 weeks before dosing (example, marathon runners, weight lifters)
-
Intake of caffeinated beverages or caffeinated food within 72 hours before dosing
-
Intake of nutritional supplements, juice, and herbal preparations or other foods or beverages that may affect the various drug metabolizing enzymes and transporters (example, alcohol, grapefruit, grapefruit juice, grapefruit-containing beverages, apple or orange juice, vegetables from the mustard green family [example, kale, broccoli, watercress, collard greens, kohlrabi, Brussels sprouts, mustard], and charbroiled meats) within 1 week before dosing
-
Intake of herbal preparations containing St. John's Wort within 4 weeks before dosing Intake of over-the-counter (OTC) medications within 14 days (or 5 half-lives, whichever is longer) before dosing unless the investigator and sponsor medical monitor consider that they do not compromise participant safety or study assessments
-
Use of any prescription drugs within 4 weeks before dosing
-
Use of illegal recreational drugs
-
Receipt of blood products within 4 weeks, or donation of blood within 8 weeks, or donation of plasma within 1 week of dosing
Contacts and Locations
Locations
| Site | City | State | Country | Postal Code | |
|---|---|---|---|---|---|
| 1 | Covance Clinical Research Unit Inc. | Madison | Wisconsin | United States | 53704 |
Sponsors and Collaborators
- Eisai Inc.
Investigators
None specified.Study Documents (Full-Text)
None provided.More Information
Publications
None provided.- E2027-A001-005