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临床试验/NCT02878096
NCT02878096已完成1 期

An Open-Label, 2-Part Sequential Dose Study Designed to Assess the Absolute Bioavailability, Mass Balance Recovery, Metabolite Profile and Metabolite Identification of [14C]-SK-1404 Administered to Healthy Male Subjects

Sanwa Kagaku Kenkyusho Co., Ltd.1 个研究点 分布在 1 个国家目标入组 6 人开始时间: 2016年7月最近更新:
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适应症
干预措施
相关药物

试验速览

阶段
1 期
状态
已完成
入组人数
6
试验地点
1
主要终点
Number and structural identification of known and unknown metabolites of SK-1404 in the plasma, urine and faeces samples
研究概览研究设计入排标准研究组 & 干预措施结局指标研究者研究点记录与标识符相似试验

研究概览

简要总结

The primary objectives of the study are:

  • To determine the absolute bioavailability of SK-1404
  • To assess the mass balance recovery after a single oral (PO) dose of carbon-14 (14C)-SK-1404
  • To provide plasma, urine and faecal samples for metabolite profiling and structural identification

The secondary objectives of the study are:

  • To determine the routes and rates of elimination of [14C]-SK-1404
  • To identify the chemical structure of each metabolite with an exposure (AUC) of more than 10% of circulating total radioactivity
  • To explore the intravenous (IV) pharmacokinetics (PK) of [14C]-SK-1404
  • To further explore the PO PK of SK-1404
  • To provide additional safety and tolerability information for SK-1404

详细描述

This is a single-centre, 2-part, open-label, non-randomised, sequential, single dose study in healthy male subjects. It is planned to enrol a single cohort of 6 healthy male subjects who will participate in Parts 1 and Part 2 of the study.

In Part 1, each subject will receive a single PO dose of SK-1404 followed by an IV microtracer dose of [14C]-SK-1404.

In Part 2, each subject will receive a single PO dose of [14C]-SK-1404.

研究设计

研究类型
Interventional
分配方式
Na
干预模型
Single Group
主要目的
Basic Science
盲法
None

入排标准

年龄范围
30 Years 至 65 Years（Adult, Older Adult）
性别
Male
接受健康志愿者
是

入选标准

  • •Healthy males
  • •Age 30 to 65 years of age
  • •Body mass index of 18.0 to 35.0 kg/m2 or, if outside the range, considered not clinically significant by the investigator
  • •Must be willing and able to communicate and participate in the whole study
  • •Must provide written informed consent
  • •Must have regular bowel movements (ie average stool production of ≥1 and ≤3 stools per day)
  • •Must agree to use an adequate method of contraception

排除标准

  • •Males with pregnant partners
  • •Participation in a clinical research study within the 3 months prior to IMP dose
  • •Subjects who are study site employees, or immediate family members of a study site or sponsor employee
  • •Subjects who have previously been enrolled in this study
  • •Subjects who have previously been dosed with SK-1404
  • •History of any drug or alcohol abuse in the past 2 years
  • •Regular alcohol consumption in males >21 units per week (1 unit = ½ pint beer, 25 mL of 40% spirit or a 125 mL glass of wine) in the past year
  • •Current smokers and those who have smoked within the last 12 months; this includes cigarettes, e-cigarettes and nicotine replacement products. A breath carbon monoxide reading of greater than 10 ppm at screening or admission
  • •Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeding 5 mSv in the last 12 months or 10 mSv in the last 5 years. No occupationally exposed worker, as defined in the Ionising Radiation Regulations 1999, shall participate in the study
  • •Subjects who have been enrolled in an ADME study in the last 12 months
  • •Subjects who do not have suitable veins for multiple venepunctures/cannulation as assessed by the investigator at screening
  • •Clinically significant abnormal biochemistry, haematology or urinalysis as judged by the investigator (laboratory parameters are listed in Appendix 1)
  • •Aspartate aminotransferase, alanine aminotransferase or alkaline phosphatase >1.5 × upper limit of normal confirmed by repeat testing
  • •Serum sodium below the lower limit of normal

研究组 & 干预措施

[14C]-SK-1404

Experimental

干预措施: [14C]-SK-1404 (Drug)

结局指标

主要结局

Number and structural identification of known and unknown metabolites of SK-1404 in the plasma, urine and faeces samples

时间窗: Predose to 168hr

Mass balance recovery of total radioactivity in urine, faeces and all excreta

时间窗: Predose to 168hr

Amount excreted (Ae), and Ae as a percentage of the administered dose (%Ae), cumulative recovery (Cum Ae) and cumulative recovery expressed as a percentage of the dose (Cum %Ae)

Absolute bioavailability (F) calculated with the AUC values of IV administration in Part 1 and PO administration in Part 2

时间窗: Predose to 96hr

次要结局

  • %Ae total radioactivity in plasma by metabolite profiling and structural identification to estimate the routes and rates of elimination of [14C]-SK-1404(Predose to 168hr)
  • Cum %Ae (total) for urine by metabolite profiling and structural identification to estimate the routes and rates of elimination of [14C]-SK-1404(Predose to 168hr)
  • Ae total radioactivity in plasma by metabolite profiling and structural identification to estimate the routes and rates of elimination of [14C]-SK-1404(Predose to 168hr)
  • Cum Ae (total) for urine by metabolite profiling and structural identification to estimate the routes and rates of elimination of [14C]-SK-1404(Predose to 168hr)
  • Cum Ae (total) for faeces by metabolite profiling and structural identification to estimate the routes and rates of elimination of [14C]-SK-1404(Predose to 168hr)
  • Cum %Ae (total) for faeces by metabolite profiling and structural identification to estimate the routes and rates of elimination of [14C]-SK-1404(Predose to 168hr)
  • The area under the concentration-time curve from dosing extrapolated to infinity (AUC(0-inf)) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The terminal elimination rate constant calculated from the slope of the apparent elimination phase (lambda-z) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The apparent total clearance (CL/F) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • Number and structural identification of unknown metabolites of SK-1404 with an AUC of more than 10% of circulating total radioactivity(Predose to 168hr)
  • The peak plasma concentration (Cmax) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The apparent terminal elimination half-life (T1/2) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The apparent volume of distribution (Vd) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The elapsed time from dosing at which the analyte was first quantifiable in a concentration vs time profile (Tlag) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The area under the concentration-time curve from dosing to the last measurable concentration (AUC(0-last)) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The area under the concentration-time curve from dosing extrapolated to infinity (AUC(0-inf)) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The apparent total clearance (CL/F) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The mean residence time (MRT) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The time from dosing at which Cmax was apparent (Tmax) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The percentage of AUC(0-inf) extrapolated beyond the last measured time point (AUC%extrap) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The apparent volume of distribution (Vss) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The mean residence time (MRT) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The elapsed time from dosing at which the analyte was first quantifiable in a concentration vs time profile (Tlag) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The area under the concentration-time curve from dosing to the last measurable concentration (AUC(0-last)) of SK-1404F and its active metabolites M-1, M-7 and M-9) after IV SK-1404(Predose to 96hr)
  • The time from dosing at which Cmax was apparent (Tmax) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The percentage of AUC(0-inf) extrapolated beyond the last measured time point (AUC%extrap) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The absolute bioavailability (F, PO vs IV from Part 1) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • To collect further information about the safety and tolerability of IMP(Predose to 168hr)
  • The peak plasma concentration (Cmax) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The apparent volume of distribution (Vd/F) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The terminal elimination rate constant calculated from the slope of the apparent elimination phase (lambda-z) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)
  • The apparent terminal elimination half-life (T1/2) of SK-1404F and its active metabolites M-1, M-7 and M-9) after PO SK-1404(Predose to 168hr)

研究者

申办方类型
Industry
责任方
Sponsor

研究点 (1)

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