A Single-center, Open-label, Single-dose Phase I Study to Investigate the Absorption, Metabolism and Excretion of [14C]D-0316 After a Single Oral 75mg/50µCi Dose in Healthy Chinese Male Subjects
概览
- 阶段
- 1 期
- 干预措施
- [14C]D-0316 suspension
- 疾病 / 适应症
- Advanced or Metastatic Non-small Cell Lung
- 发起方
- Betta Pharmaceuticals Co., Ltd.
- 入组人数
- 4
- 试验地点
- 1
- 主要终点
- Radioactivity concentration of each feces sample
- 最后更新
- 4年前
概览
简要总结
This is a single-center, open-label, single-dose phase I study to investigate the absorption, metabolism and excretion of [14C] D-0316 in healthy Chinese male subjects. The study will be conducted into two steps：Firstly, 2 subjects are enrolled in to participate in the pilot study to grope for the completion date of plasma, urine and feces sampling on the 3rd day post-dose and onwards. Then, the collection time of blood and excreta samples (urine and feces) from the subsequent 2-4 subjects will be adjusted according to the pilot study
详细描述
Subjects who had signed informed consent and meet inclusion criteria and no exclusion criteria are admitted to Phase I Clinical Unit two days prior to dosing (D-2). On the morning of Day 1 before dosing, subjects will be transferred to nuclear medical ward. And after an overnight fast of at least 10 h, subjects will receive a single oral dose of 75 mg (50 μCi) of \[14C\]D-0316 as an oral suspension. Then, after two days of the dosing, subjects will be transferred back to Phase I Clinical Unit ward and confined to this unit until blood or excreta sampling and safety monitoring at the designated time points or intervals are complete
研究者
入排标准
入选标准
- •healthy male volunteers between the ages of 18 to 50 years old；
- •Body weight \>=50 kg, Body mass index (body weight(kg)/hight2(m2)) between 19 and 26 kg/m2；
- •Normal physical findings, clinical laboratory values, vital signs and 12-lead ECG, or any abnormality that is non-clinically significant;
- •Male subjects of reproductive potential with partners will be instructed to, and must be willing to practice a highly effective method of birth control for the duration of the study and continuing 1 year after discontinuing treatment with the investigational product. Highly effective methods of birth control include using condom, contraceptive sponge, contraceptive gel, contraceptive film, intrauterine device, oral or injectable contraceptive pill, hypodermic implants or others；
- •Must understand, and voluntarily sign the informed consent, comply with the requirements of the study.
排除标准
- •History of or current clinically significant cardio, pulmonary, endocrine, metabolism, renal, hepatic, gastrointestinal, dermatology, infection, hematology, neurological, mental disease or disorder;
- •Positive test for HBsAg, HBeAg, anti-HCV, anti-HIV or syphilis antibody;
- •History of syncope / needle syncope and intolerable intravenous indwelling needle;
- •History of clinically significant disease or infection within 1 month before entering the study;
- •Abnormality in blood pressure, including hypertensive BP (SBP\>=140 mmHg, or DBP \>=90 mmHg), or hypotensive BP(SBP\<90 mmHg, or DBP \<=55 mmHg), Pulse rate\<55 bpm or \>100 bpm;
- •Long-QT syndrome or family history of it, or QTcB interval \> 450 ms; intraventricular blocks or left/right bundle branch block or QRS\>120ms; frequent ventricular ectopic beats (any 10s ECG ventricular premature beat \>= 1 in screening period); or abnormal resting heart rate (\> 100 bpm);
- •Received any drug within 14 days before taking the investigational drug, including any prescription drug, OTC drug, herbal drug or health care products, except for vitamins and paracetamol；
- •History of or current swallowing disorder, active gastrointestinal diseases, or other diseases that significantly affect absorption, distribution, metabolism and excretion of drugs;
- •Chronic constipation or diarrhea, irritable bowel syndrome, inflammatory bowel disease;
- •Hemorrhoids or perianal disease with regular/perianal bleeding;
研究组 & 干预措施
[14C]D-0316
To investigate the absorption properties, as well as to evaluate the mass balance and elucidate the pathways of biotransformation after a single oral dose (75mg, 50µCi) of \[14C\]D-0316 to healthy Chinese male subjects
干预措施: [14C]D-0316 suspension
结局指标
主要结局
Radioactivity concentration of each feces sample
时间窗: Day-1-Day85
Use liquid scintillation counter or accelerator mass spectrometry to evaluate radioactivity concentration of each feces（DPM/ml) sample
Radioactivity concentration of each plasma sample
时间窗: Day 1-Day85
Use liquid scintillation counter or accelerator mass spectrometry to evaluate radioactivity concentration of each plasma（DPM/ml) sample
Total recovery of radioactivity in urine and feces
时间窗: Day-1-Day85
Calculate the total radioactivity in urine and feces based on the radioactivity concentration of each sample
Radioactivity concentration of each urine samples
时间窗: Day-1-Day85
Use liquid scintillation counter or accelerator mass spectrometry to evaluate radioactivity concentration of each urine（DPM/ml) sample
Identification of metabolites in plasma, urine and fecal samples
时间窗: Day-1-Day85
LC-MS/MS was used to identify the main metabolites in plasma, urine and feces, and finally to provide the main biotransformation pathway of CM082 in human body
次要结局
- Pharmacokinetic parameters of unlabeled D-0316 and metabolite D-0865(Day-1-Day85)
- Number of participants with treatment-related adverse events as assessed by CTCAE v4.03(Day-14-Day85)