NCT04804059已完成1 期
An Open Label, Single-Dose, Single-Period Study Designed to Assess the Mass Balance Recovery, Metabolite Profile and Metabolite Identification of [14C]-APX001 in Healthy Male Subjects After Oral and Intravenous Dosing
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
- 10
- 试验地点
- 1
- 主要终点
- Mass balance recovery as measured by mass unit equiv/g after a single oral or single intravenous (IV) dose of carbon-14 (14C)-labelled APX001 ([14C]-APX001).
研究概览
简要总结
This is a single-center, open-label, non-randomized, single dose study in healthy male subjects. It was planned to enroll 2 cohorts of 5 subjects (10 subjects in total), with the target of achieving data in 4 evaluable subjects per cohort. Five subjects were to receive a single oral dose of APX001 and not more than (NMT) 3.1 megabecquerel (MBq) (84.0 microcurie [μCi]) 14C in the fed state. Five subjects were to receive a single IV administration containing APX001 and NMT 3.4 MBq (93.0 μCi) 14C in the fed state.
研究设计
- 研究类型
- Interventional
- 分配方式
- Non Randomized
- 干预模型
- Parallel
- 主要目的
- Treatment
- 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
- •Aged 30 to 65 years of age
- •Body mass index (BMI) of 18.0 to 32.0 kg/m2 or, if outside the range, considered not clinically significant by the investigator
- •Good state of health (mentally and physically) as indicated by a comprehensive clinical assessment (detailed medical history and a complete physical examination)
- •Must have been willing and able to communicate and participate in the whole study
- •Must have had regular bowel movements (i.e. average stool production of ≥1 and
- •≤3 stools per day)
- •Must have provided written informed consent
- •Must have adhered to the contraception requirements defined in Section 9.4 of the protocol (Appendix 16.1.1)
排除标准
- •Subjects who had received any IMP in a clinical research study within the previous 3 months or a similar 14C radioactive clinical trial within the previous 12 months
- •Subjects who were study site employees, or immediate family members of a study site or sponsor employee
- •Subjects who had previously been enrolled in this study.
- •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, or a 25 mL shot of 40% spirit, 1.5 to 2 units = 125 mL glass of wine, depending on type)
- •Current smokers and those who had smoked within the last 12 months. A breath carbon monoxide (CO) reading of greater than 10 ppm at screening and admission
- •Current users of e-cigarettes and nicotine replacement products and those who had used these products within the last 12 months
- •Radiation exposure, including that from the present study, excluding background radiation but including diagnostic x-rays and other medical exposures, exceeded 5 millisieverts (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 2017, was to participate in the study
- •Subjects who did not have suitable veins for multiple venipunctures/cannulation as assessed by the investigator at screening
- •Clinically significant abnormality on electrocardiogram (ECG) as judged by the investigator
- •Clinically significant abnormal biochemistry, hematology or urinalysis at screening as judged by the investigator (laboratory parameters are listed in Appendix 1 of the protocol, Appendix 16.1.1)
- •Positive drugs of abuse test result (drugs of abuse tests are listed in Appendix 1 of the protocol, Appendix 16.1.1)
- •Positive hepatitis B surface antigen (HBsAg), hepatitis C virus antibody (HCV Ab) or human immunodeficiency virus (HIV) results
- •Evidence of renal impairment at screening, as indicated by an estimated creatinine clearance of <80 mL/min using the Cockcroft-Gault equation
- •History of clinically significant cardiovascular, renal, hepatic, chronic respiratory or gastrointestinal (GI) disease, neurological or psychiatric disorder, as judged by the investigator
- •Serious adverse reaction or serious hypersensitivity to any drug or the formulation excipients
- •Presence or history of clinically significant allergy requiring treatment, as judged by the investigator. Hayfever was allowed unless it was active
- •Donation or loss of greater than 400 mL of blood within the previous 3 months
- •Subjects who were taking, or had taken, any prescribed or over-the-counter drug (other than 4 g per day paracetamol) or herbal remedies in the 14 days before IMP administration (see Section 11.4 of the protocol, Appendix 16.1.1). Exceptions may have applied on a case by case basis, if considered not to interfere with the objectives of the study, as agreed by the PI and sponsor's medical monitor.
- •Failure to satisfy the investigator of fitness to participate for any other reason
研究组 & 干预措施
Cohort A
Experimental
[14C]-APX001 Oral Solution
干预措施: [14C]-APX001 Oral Solution (Drug)
Cohort B
Experimental
[14C]-APX001 Solution for Infusion
干预措施: [14C]-APX001 Solution for Infusion (Drug)
结局指标
主要结局
Mass balance recovery as measured by mass unit equiv/g after a single oral or single intravenous (IV) dose of carbon-14 (14C)-labelled APX001 ([14C]-APX001).
时间窗: 3 weeks
Profiling of metabolites of [14C]-APX001 in plasma and excreta.
时间窗: 3 weeks
Plasma, urine and feces samples from subjects dosed with \[14C\]-APX001 were analyzed using high resolution, accurate mass liquid chromatography tandem mass spectrometry (LC-MS/MS) with in-line fraction collection and off-line counting to obtain \[14C\]-radiochromatographic profiles and provide information on the nature of the radioactive components present, including chemical structure identification.
次要结局
- Elimination pathway of [14C]-APX001 following a single oral or single IV dose of [14C]-APX001.(3 weeks)
- Extent of distribution of total radioactivity into blood cells following a single oral or single IV dose of [14C]-APX001.(3 weeks)
研究者
研究点 (1)
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