An Open-Label, Single-Dose Study to Determine the Metabolism and Elimination of [14C]E2027 in Healthy Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- Eisai Inc.
- 入组人数
- 8
- 试验地点
- 1
- 主要终点
- Cumulative Percent of the Radiolabeled Dose of [14C]E2027 in Biological Matrices (Blood, Urine, Feces and Toilet Tissue)
研究概览
简要总结
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.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Treatment
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •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
排除标准
- 未提供
研究组 & 干预措施
E2027
Participants will receive approximately 130 microcurie (μCi) of [14C]E2027 as a single 50 milligram (mg) (free base), capsule, orally on Day 1.
干预措施: E2027 (Drug)
结局指标
主要结局
Cumulative Percent of the Radiolabeled Dose of [14C]E2027 in Biological Matrices (Blood, Urine, Feces and Toilet Tissue)
时间窗: 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
时间窗: 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
时间窗: 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
时间窗: 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
时间窗: 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
时间窗: 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
时间窗: Pre-dose up to Day 56 post-dose
Apparent Total Body Clearance (CL/F) of E2027 in Biological Matrices
时间窗: Pre-dose up to Day 56 post-dose
Apparent Volume of Distribution (Vd/F) of E2027 in Biological Matrices
时间窗: Pre-dose up to Day 28 post-dose
Percent of AUC(0-inf) of Metabolite to E2027 in Biological Matrices
时间窗: Pre-dose up to Day 28 post-dose
次要结局
- 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 Physical Examination Findings(Baseline, 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)