A Study to Determine the Metabolism and Elimination of [14C]E2027 in Healthy Male Participants

NCT04023877 | Completed Phase 1 FDA Drug

• 1 other identifier: E2027-A001-005
• Study Type: interventional
• Target: 8
• Locations: 1 country
• Sites: 1

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.

Conditions

Dementias With Lewy Bodies

Keywords

E2027; [14C]E2027; Dementia with Lewy bodies; Dementia

Outcome Measures

Primary Outcomes (10)

• Cumulative Percent of the Radiolabeled Dose of [14C]E2027 in Biological Matrices (Blood, Urine, Feces and Toilet Tissue)

  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.

  Up to 56 days

• 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 Outcomes (5)

• 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

Study Arms (1)

E2027

EXPERIMENTAL

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

Interventions

E2027 DRUG

E2027 oral capsule.

E2027

Eligibility Criteria

• Age: 18 Years - 55 Years
• Sex: male
• Healthy Volunteers: Yes
• Age Groups: Adult (18-64)

You may qualify if:

• 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

You may not qualify if:

• 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

Sponsors & Collaborators

• Eisai Inc.: lead

Study Sites (1)

Covance Clinical Research Unit Inc.

Madison, Wisconsin, 53704, United States

Location

MeSH Terms

Conditions

Lewy Body Disease; Dementia

Condition Hierarchy (Ancestors)

Parkinsonian Disorders; Basal Ganglia Diseases; Brain Diseases; Central Nervous System Diseases; Nervous System Diseases; Movement Disorders; Synucleinopathies; Neurodegenerative Diseases; Neurocognitive Disorders; Mental Disorders

Study Design

• Study Type: interventional
• Phase: phase 1
• Allocation: NA
• Masking: NONE
• Purpose: TREATMENT
• Intervention Model: SINGLE GROUP
• Sponsor Type: INDUSTRY
• Responsible Party: SPONSOR

Study Record Dates

• First Submitted: July 16, 2019
• First Posted: July 18, 2019
• Study Start: July 18, 2019
• Primary Completion: October 11, 2019
• Study Completion: October 11, 2019
• Last Updated: December 3, 2019

Record last verified: 2019-07

Data Sharing

• IPD Sharing: Will share

Locations

US (1)