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A Study to Determine the Metabolism and Elimination of [14C]E7090 in Healthy Male Participants

Phase 1
Completed
Conditions
Healthy Volunteers
Interventions
Drug: [14C]E7090
Registration Number
NCT04493255
Lead Sponsor
Eisai Limited
Brief Summary

The primary objective of this study is to determine the pharmacokinetics (PK) and excretion of E7090 and its metabolites in healthy male participants. Also, to assess the safety and tolerability of a single dose of E7090 in healthy male participants.

Detailed Description

Not available

Recruitment & Eligibility

Status
COMPLETED
Sex
Male
Target Recruitment
8
Inclusion Criteria
  1. Non-smoking, healthy males, age greater than or equal to (>=) 35 years and less than or equal to (<=) 55 years old at the time of informed consent
  2. Body Mass Index (BMI) of >=18 to <=32 kilogram per square meter (kg/m^2) at Screening
  3. Provide written informed consent
  4. Willing and able to comply with all aspects of the protocol
  5. History of a minimum of 1 bowel movement per day
Exclusion Criteria
  1. Participant has participated in any clinical research study involving a radiolabeled investigational product within the 12 months prior to Day -1 (Baseline)

  2. Participant has previously completed or withdrawn from this study or any other study investigating E7090 or previously received E7090

  3. Participant has had exposure to significant diagnostic or therapeutic radiation (example: serial x-ray, computed tomography scan, barium meal) or has current employment in a job requiring radiation exposure monitoring within 12 months prior to Day -1

  4. Participant has the following ocular disorders:

    1. Any previous history or current evidence of corneal disorder
    2. Any previous history or current evidence of active macular disorder (example: age-related macular degeneration, central serous chorioretinal disease)
  5. Participants has a known history of clinically significant drug allergy at Screening or Baseline (Day -1)

  6. Participants has a known history of food allergies or significant seasonal or perennial allergy

  7. Participants is known to be human immunodeficiency virus positive at Screening

  8. Participants has active viral hepatitis (B or C) as demonstrated by positive serology at Screening

  9. Participant has a poor peripheral venous access, in the opinion of the investigator (or designee)

  10. Participant received blood products within 2 months prior to Day -1, or donation of blood within 3 months prior to Screening, donation of plasma within 2 weeks prior to Screening, or donation of platelets from 6 weeks prior to Screening

Study & Design

Study Type
INTERVENTIONAL
Study Design
SINGLE_GROUP
Arm && Interventions
GroupInterventionDescription
E7090[14C]E7090Participants will receive 100 microcurie (μCi) of \[14C\]E7090 as a single 35 milligram (mg), capsule, orally on Day 1.
Primary Outcome Measures
NameTimeMethod
feu: Percentage of Administered Radioactive Dose of [14C]E7090 Excreted in UrineUp to Day 57
feu+ef: Percentage of Administered Radioactive Dose excreted of [14C]E7090 in Combined Excreta (Urine and Feces)Up to Day 57
Cumulative feu: Cumulative Percentage of Administered Radioactive Dose of [14C]E7090 Excreted in Urine From 0 to tlast HoursUp to Day 57
Cumulative fef: Cumulative Percentage of Administered Radioactive Dose of [14C]E7090 Excreted in Feces From 0 to tlast HoursUp to Day 57
CL/F: Apparent Total Body Clearance for E7090Day 1: 0-672 hours post-dose
Vd/F: Apparent Volume of Distribution for E7090Day 1: 0-672 hours post-dose
fef: Percentage of Administered Radioactive Dose of [14C]E7090 Excreted in FecesUp to Day 57
AUC(0-t): Area Under the Concentration- time Curve From Time 0 to Time of Last Quantifiable Concentration for [14C]E7090, E7090 and its MetabolitesDay 1: 0-672 hours post-dose
AUCinf: Area Under the Plasma Concentration-time Curve From Time 0 to Infinity for [14C]E7090, E7090 and its MetabolitesDay 1: 0-672 hours post-dose
T1/2: Terminal Elimination Phase Half-life for [14C]E7090, E7090 and its MetabolitesDay 1: 0-672 hours post-dose
MPR AUC(0-inf): Metabolite to Parent Ratio For AUC(0-inf) of Metabolite to E7090, Corrected for Molecular WeightsDay 1: 0-672 hours post-dose
Cumulative feu+ef: Cumulative Percentage of Administered Radioactive Dose excreted of [14C]E7090 in Combined Excreta (Urine and Feces) From 0 to tlast HoursUp to Day 57
Cmax: Maximum Observed Plasma Concentration for [14C]E7090, E7090 and its MetabolitesDay 1: 0-672 hours post-dose
Tmax: Time to Reach the Maximum Plasma Concentration (Cmax) for [14C]E7090, E7090 and its MetabolitesDay 1: 0-672 hours post-dose
AUC(0-24h): Area Under the Plasma Concentration-time Curve From Time 0 to 24 Hours Postdose for [14C]E7090, E7090 and its MetabolitesDay 1: 0-24 hours post-dose
Secondary Outcome Measures
NameTimeMethod
Number of Participants With Clinically Significant Change From Baseline in Laboratory Parameters ValuesBaseline up to Day 29
Metabolic profile of E7090: Concentration of Metabolite of E7090 in Plasma, Urine, and FecesUp to Day 57

Blood, urine and feces samples will be collected and analyzed to estimate the concentration of metabolite of E7090 by Liquid Chromatography/ multiple-stage Mass Spectroscopy method.

Number of Participants With Treatment-emergent Adverse Events (TEAEs)Baseline up to Day 57
Number of Participants With Clinically Significant Change From Baseline in 12 Lead Electrocardiogram (ECG) FindingsBaseline up to Day 29
Number of Participants With Clinically Significant Change From Baseline in Vital Signs ValuesBaseline up to Day 29
Number of Participants With Any Suicidality Assessed Using Columbia-Suicide Severity Rating Scale (C-SSRS)Baseline up to Day 29

The C-SSRS is an interview-based rating scale to systematically assess any suicidality, any suicidal behavior, any suicidal ideation. Any suicidality: emergence of any suicidal ideation or suicidal behavior. Any suicidal behavior: when response is "yes" for any these questions- actual attempt to suicide, engaged in non-suicidal self-injurious behavior, interrupted attempt, aborted attempt, preparatory acts. Any suicidal ideation: when response is "yes" for any of these questions- wish to be dead, non-specific active suicidal thoughts, active suicidal ideation with methods without intent to act or some intent to act, without specific plan or with specific plan and intent to suicide. Number of participants with any suicidality will be reported for this outcome measure.

Number of Participants With Clinically Significant Change From Baseline in Ophthalmic ExaminationsBaseline up to Day 29

Ophthalmic examinations includes visual acuity, funduscopy, optical coherence tomography, and slit-lamp examination.

Number of Participants With Clinically Significant Change From Baseline in Physical ExaminationsBaseline up to Day 29

Trial Locations

Locations (1)

Covance Clinical Research Unit

🇬🇧

Leeds, United Kingdom

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