A Single Center, Single Dose, Open Label Phase 1 Study To Evaluate The Pharmacokinetics, Excretion, Mass Balance And Metabolism Of [14c]-Famitinib In Healthy Adult Male Subjects
试验速览
- 阶段
- 1 期
- 状态
- 进行中（未招募）
- 入组人数
- 6
- 试验地点
- 1
- 主要终点
- Mass balance recovery of total radioactivity in all excreta urine: CumAe and Cum%Ae
研究概览
简要总结
The purpose of this study is to evaluate the excretion balance, metabolic profile and the routes of excretion of famitinib in healthy adult male subjects.
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
- 18 Years 至 45 Years（Adult）
- 性别
- Male
- 接受健康志愿者
- 是
入选标准
- •Healthy adult male between the ages of 18 and 45 years;
- •Total body weight ≥ 50 kg, and the Body Mass Index (BMI) of 19 to 28 kg/m2;
- •Male subjects of childbearing potential and their partners have no birth or sperm donation plan and voluntarily take effective contraception during the course of clinical trial until 6 months after the drug administration;
- •An informed consent document signed and dated by the subject;
- •Normal bowel movements (1 to 2 times a day), no habitual constipation or diarrhea.
排除标准
- •No clinically relevant abnormalities identified by a detailed medical history, full physical examination, including blood pressure and pulse rate measurement, 12-lead ECG and clinical laboratory tests;
- •Positive results of hepatitis B surface antigen, hepatitis C antibody, HIV antibody or treponema pallidum antibody;
- •Have taken any clinical trial drug or participated in any clinical trial within 3 months before administration;
- •CYP3A4 inducers or inhibitors were taken within 28 days before administration;
- •Have taken any prescription or over-the-counter drugs, vitamin products, health care drugs, traditional Chinese medicines or food supplements within 14 days before administration;
- •Those who need to receive anticoagulant therapy such as warfarin or thrombin inhibitors and/or aspirin antiplatelet therapy within 1 month before administration and during the study period;
- •There are clinically significant bleeding symptoms or clear bleeding tendencies within 3 months before administration, such as gastrointestinal bleeding and peptic ulcers;
- •History of stroke or intracranial hemorrhage within 6 months before administration;
- •Have uncontrolled clinical symptoms or diseases of the heart, such as: (1) heart failure above NYHA2 (2) unstable angina (3) myocardial infarction within 1 year (4) clinically significant supraventricular or ventricular arrhythmias requiring treatment or intervention (5) screening period QTcF >450 ms (male);
- •Those who have undergone major surgery within 6 months before administration or that surgical incision has not completely healed; Major surgery includes, but is not limited to, any surgery that is at significant risk of bleeding, prolongs the period of general anesthesia, or has an incision biopsy or significant traumatic injury;
- •Abdominal fistula, gastrointestinal perforation or abdominal abscess occurred within 6 months before administration;
- •Hemorrhoids or perianal diseases accompanied by regular / hematochezia; Those with gastrointestinal abnormalities such as irritable bowel syndrome and inflammatory bowel disease, which may affect drug absorption as determined by investigator;
- •People with allergic constitution or allergic diseases, including those with severe drug allergies or history of drug allergies, and those who are known to be allergic to famitinib or excipients;
- •Have any history of clinical serious diseases or diseases or conditions that the researcher believes may affect the results of the trial, including but not limited to circulatory system, endocrine system, nervous system, digestive system, urinary system or blood, immune, psychiatric and metabolic disease history; Lifestyle Habits;
- •History of alcoholism with alcohol consumption over 14 units per week;; and can't abstain from smoking and alcohol during the study;
- •Heavy smoker or habitually use nicotine-containing products;
- •Have a history of drug abuse or have used soft drugs (such as: marijuana) within 3 months before administration or take drugs (such as cocaine, amphetamines, phencyclidine, etc.) within 1 year before administration; or positive urine drug abuse test during screening periods;
- •Habitual consumption of grapefruit juice or excessive tea, coffee and/or caffeinated beverages (more than 8 cups a day, 1 cup = 250 mL) and unable to quit during the study period;
- •Those who cannot tolerate venipuncture or with a history of needle-sickness and blood-sickness;
- •Workers who require long-term exposure to radioactive conditions; or those who have significant radiation exposure (≥ 2 chest/abdominal CT scans, or 3 other X-ray tests ≥) within 1 year prior to administration or who have participated in radiopharmaceutical labeling tests;
- •Blood donation no less than 400 mL or have blood transfusion within 3 months of dosing;
- •Subjects who, in the opinion of the Investigator should not participate in this study.
研究组 & 干预措施
Treatment group
干预措施: Famitinib (Drug)
结局指标
主要结局
Mass balance recovery of total radioactivity in all excreta urine: CumAe and Cum%Ae
时间窗: 0-336 hours
Amount and cumulative amount excreted and expressed as the percentage of the administered dose into the urine from time t1 to time t2
Mass balance recovery of total radioactivity in all excreta feces: CumAe and Cum%Ae
时间窗: 0-336 hours
Amount and cumulative amount excreted and expressed as the percentage of the administered dose into the feces from time t1 to time t2
Metabolic Profiling in Urine
时间窗: 0-336 hours
Metabolic profiling/identification and determination of relative abundance of famitinib and the metabolites of famitinib in urine if possible.
Total recovery of radioactivity in urine and feces as percentage of total radioactive dose administered
时间窗: 0-336 hours
To characterize the extent of excretion of total radioactivity in urine and feces following administration of famitinib
Metabolic Profiling in Blood
时间窗: 0 to 240 hours
Metabolic profiling/identification and determination of relative abundance of famitinib and the metabolites of famitinib in plasma if possible.
Plasma famitinib and SHR116637: Tmax
时间窗: 0-240 hours
Radioactivity Tmax
时间窗: 0-240 hours
Radioactivity Cmax
时间窗: 0-240 hours
Plasma famitinib and SHR116637: t1/2
时间窗: 0-240 hours
Radioactivity t1/2
时间窗: 0-240 hours
Metabolic Profiling in Feces
时间窗: 0-336 hours
Metabolic profiling/identification and determination of relative abundance of famitinib and the metabolites of famitinib in feces if possible.
Ratio of radioactivity of whole blood and plasma blood
时间窗: 0-72 hours
Radioactivity AUC
时间窗: 0-240 hours
Plasma famitinib and SHR116637: AUC
时间窗: 0-240 hours
Plasma famitinib and SHR116637: Cmax
时间窗: 0-240 hours
次要结局
- AEs and SAEs(0-14 days)