An Open-label Phase 1 Study to Evaluate Metabolism, Excretion, and Mass Balance of [¹⁴C]MK-5684 in Healthy Male Participants
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 入组人数
- 8
- 试验地点
- 1
- 主要终点
- Cumulative percentage of total radioactivity excreted in feces (Cumfef) after administration of single-dose [¹⁴C]Opevesostat
研究概览
简要总结
This is a study of opevesostat in healthy adult male participants. The purpose of this study is to understand the absorption, distribution, metabolism, and elimination of opevesostat in humans, as well as its pharmacokinetics (PK), metabolic profile, and safety and tolerability.
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
- 30 Years 至 55 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Is a healthy male according to the assessment of the investigator
- •Has a body mass index of 18.0 to 32.0 kg/m2
- •Has regular bowel movements (i.e., average stool production of ≥1 and ≤3 stools per day)
排除标准
- •Has the presence or history of clinically significant allergy requiring treatment
- •Has a history of adrenal insufficiency
- •Has veins not suitable for multiple venipunctures/cannulation
- •Has previously taken part in more than 3 radiolabeled drug studies in the last 12 months
- •Has donated blood or plasma within the previous 3 months or lost greater than 400 mL of blood
研究组 & 干预措施
[¹⁴C]Opevesostat
On Day 1, participants receive a single dose of [¹⁴C]opevesostat as an oral solution. Participants then receive single doses of 5.0 mg prednisone and 0.05 mg fludrocortisone tablets 4 hours later as hormone replacement therapy.
干预措施: Prednisone (Drug)
[¹⁴C]Opevesostat
On Day 1, participants receive a single dose of [¹⁴C]opevesostat as an oral solution. Participants then receive single doses of 5.0 mg prednisone and 0.05 mg fludrocortisone tablets 4 hours later as hormone replacement therapy.
干预措施: Fludrocortisone (Drug)
[¹⁴C]Opevesostat
On Day 1, participants receive a single dose of [¹⁴C]opevesostat as an oral solution. Participants then receive single doses of 5.0 mg prednisone and 0.05 mg fludrocortisone tablets 4 hours later as hormone replacement therapy.
干预措施: [¹⁴C]Opevesostat (Drug)
结局指标
主要结局
Cumulative percentage of total radioactivity excreted in feces (Cumfef) after administration of single-dose [¹⁴C]Opevesostat
时间窗: Predose and at designated time points (up to 8 days)
Fecal samples will be collected at pre-specified timepoints and used to determine Cumfef.
Plasma Opevesostat Pharmacokinetics: Area under the curve from time 0 to the time of last measurable concentration (AUC0-t)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-t of opevesostat.
Total Number of Metabolites in Feces that Represent at least 10% of the Dose of Radioactivity
时间窗: Predose and at designated time points (up to 8 days)
Fecal samples will be collected at pre-specified timepoints and used to determine the total number of metabolites that represent at least 10% of the dose of radioactivity. Metabolites will be determined using liquid scintillation and high-resolution mass spectrometry.
Cumulative percentage of total radioactivity excreted in urine (Cumfeu) after administration of single-dose [¹⁴C]Opevesostat
时间窗: Predose and at designated time points (up to 8 days)
Urine samples will be collected at pre-specified timepoints and used to determine CumFeu.
Plasma Opevesostat Pharmacokinetics: Area under the curve from time 0 to extrapolated infinity (AUC0-inf)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-inf of opevesostat.
Plasma Total Radioactivity Pharmacokinetics: Time of maximum observed concentration (Tmax)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine Tmax of total radioactivity.
Cumulative amount of total radioactivity excreted in urine (CumAeu) after administration of single-dose [¹⁴C]Opevesostat
时间窗: Predose and at designated time points (up to 8 days)
Urine samples will be collected at pre-specified timepoints and used to determine CumAeu.
Plasma Opevesostat Pharmacokinetics: Maximum observed concentration (Cmax)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine Cmax of opevesostat.
Plasma Opevesostat Pharmacokinetics: Terminal elimination half-life (t1/2)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine t1/2 of opevesostat.
Plasma Total Radioactivity Pharmacokinetics: Maximum observed concentration (Cmax)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine Cmax of total radioactivity.
Plasma Total Radioactivity Pharmacokinetics: Terminal elimination half-life (t1/2)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine t1/2 of total radioactivity.
Total Number of Metabolites in Plasma that Represent at least 10% of the Dose of Radioactivity
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine the total number of metabolites that represent at least 10% of the dose of radioactivity. Metabolites will be determined using liquid scintillation and high-resolution mass spectrometry.
Cumulative amount of total radioactivity excreted in feces (CumAef) after administration of single-dose [¹⁴C]Opevesostat
时间窗: Predose and at designated time points (up to 8 days)
Fecal samples will be collected at pre-specified timepoints and used to determine CumAef.
Plasma Opevesostat Pharmacokinetics: Time of maximum observed concentration (Tmax)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine Tmax of opevesostat.
Plasma Total Radioactivity Pharmacokinetics: Area under the curve from time 0 to the time of last measurable concentration (AUC0-t)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-t of total radioactivity.
Plasma Total Radioactivity Pharmacokinetics: Area under the curve from time 0 to extrapolated infinity (AUC0-inf)
时间窗: Predose and at designated time points (up to 8 days)
Plasma samples will be collected at pre-specified timepoints and used to determine AUC0-inf of total radioactivity.
Total Number of Metabolites in Urine that Represent at least 10% of the Dose of Radioactivity
时间窗: Predose and at designated time points (up to 8 days)
Urine samples will be collected at pre-specified timepoints and used to determine the total number of metabolites that represent at least 10% of the dose of radioactivity. Metabolites will be determined using liquid scintillation and high-resolution mass spectrometry.
次要结局
- Number of Participants with One or More Adverse Events (AEs)(Up to approximately 8 days)
- Number of Participants who Discontinue from the Study Due to an AE(Up to approximately 8 days)