A Phase I Study to Evaluate Safety, Biodistribution, Radiation Dosimetry, and Pharmacokinetics of XTR004 in Healthy Chinese Volunteers
试验速览
- 阶段
- 1 期
- 状态
- 已完成
- 发起方
- 入组人数
- 10
- 试验地点
- 1
- 主要终点
- Changes in Laboratory tests
研究概览
简要总结
XTR004 is a 18F-labeled myocardial perfusion positron emission tomography tracer use to measure myocardial perfusion and myocardial blood flow. XTR004 binds to the myocytes and targets respiratory chain complex 1 in the mitochondria.This phase I study investigated the safety, biodistribution, radiation dosimetry and Pharmacokinetics of XTR004 in 10 healthy Chinese adults volunteers.
详细描述
XTR004 is a 18F-labeled myocardial perfusion PET tracer, the first one developed in China by Sinotau Pharmaceutical Group. XTR004 targets and binds to the mitochondrial complex I protein. XTR004 reflects myocardial function at a molecular level. In pre-clinical studies XTR004 demonstrated high myocardial first-pass extraction and prolonged retention, allowing for early or delayed imaging. XTR004 can be clinically used to measure myocardial perfusion and myocardial blood flow. This Phase I study will be open-labeled, nonrandomized, single center study. Enrolled 10 healthy Chinese adults who meet all of the inclusion and none of the exclusion criteria. Subjects will receive 6-8 mCi of XTR004 via IV injection. Safety and tolerability will be observed. Biodistribution, pharmacokinetics, and dosimetry will be investigated.
研究设计
- 研究类型
- Interventional
- 分配方式
- Na
- 干预模型
- Single Group
- 主要目的
- Diagnostic
- 盲法
- None
入排标准
- 年龄范围
- 18 Years 至 40 Years（Adult）
- 性别
- All
- 接受健康志愿者
- 是
入选标准
- •Chinese men and women are included age between 18-40 years
- •Normal vital signs and physical examination
- •No clinical abnormalities in ECG, EEG, and echocardiogram
- •No past history of cardiovascular, cerebrovascular, or gastrointestinal diseases
- •Normal or no clinical significance abnormalities in laboratory tests
- •No any other major or chronic illness
- •No presence of drug use
- •Females adopt effective medically approved contraceptive methods to prevent pregnancy for at least 6 months before the study and after the study
- •Voluntarily agree and signed written consent
排除标准
- •Previous history of cardiovascular diseases
- •A history of or physical or radiographic manifestations of any previous brain disease
- •Any previous major disease or unstable condition
- •Subjects who cannot complete XTR004 imaging as required
- •Positive HIV, hepatitis C or Treponema pallidum antibody and hepatitis B surface antigen detection
- •A history of coagulation or coagulation disorder
- •A history of liver or gastrointestinal disease or other conditions that interfere with drug absorption, distribution, excretion or metabolism as determined by the investigator
- •Previous history of cancer
- •High risk of drug allergic reaction
- •A history of alcohol or drug abuse/dependence
- •Exposure to significant occupational radiation (e.g >50 mvs/year) or exposure to radioactive substances for therapeutic or research purposes over the past 10 years
- •Scheduled surgery or other invasive interventions within one week before drug injection
- •Subjects use any drug or treatment that may interfere with the experimental data or cause serious side effects, as determined by the investigator
- •Pregnant or lactating women
- •Admitted to hospital due to illness during screening period Other conditions that investigators consider inappropriate to participate in a trial.
结局指标
主要结局
Changes in Laboratory tests
时间窗: up to 14 days post injection
Safety observation: Measurements of routine blood (g/L), routine urine (mg/dL), and blood troponin-I levels (ng/ml) after drug injection. To observe and report changes in routine blood, routine urine, and blood troponin-I levels compared to baseline values obtained before drug injection.
Physical examination of the major organ systems
时间窗: up to 14 days post injection
Safety observation: Observation of Cardiovascular system (blood pressure, pulse rate, and rhythm), Lungs (respiratory rate, chest expansion, and lung auscultation), Abdominal system (for any tenderness or organ enlargement), Nervous system ( cognitive testing, motor strength and control, including mental status), Musculoskeletal system, and Skin for any abnormalities, after drug injection. To report number of participants with changes in physical examination compared to baseline physical examination obtained before drug injection.
Monitoring of body temperature
时间窗: up to 14 days post injection
Safety observation: Vital sign monitoring of body temperature (degrees celsius ) after drug injection. To report changes in body temperature compared to baseline body temperature obtained before drug injection.
12-lead Electrocardiography
时间窗: up to 14 days post injection
Safety observation: Observation of ECG electrical activity pattern in the P-wave, PR interval, QRS wave complex, ST segment, and T-wave if associated with any abnormality after drug injection. To observe and report participants with ECG abnormality compared to baseline ECG obtained before drug injection.
Monitoring of respiratory rate
时间窗: up to 14 days post injection
Safety Observation: Vital sign monitoring of respiratory rate (breath per minute) after drug injection. To report changes in respiratory rate compared to baseline respiratory rate obtained before drug injection.
Monitoring of pulse rate
时间窗: up to 14 days post injection
Safety Observation: Vital sign monitoring of pulse rate (beats per minute) after drug injection. To report changes in pulse rate compared to baseline pulse rate obtained before drug injection.
Monitoring of Blood pressure
时间窗: up to 14 days post injection
Safety Observation: Vital sign monitoring of blood pressure (mmHg) after drug injection. To report changes in blood pressure compared to baseline blood pressure obtained before drug injection.
Incidence of adverse events
时间窗: up to 14 days post injection
Safety Observation: Number of participants with adverse events and severe adverse events after drug injection.
次要结局
- Urine radioactivity analysis(up to 7.25 hours)
- Biodistribution of XTR004 after a single dose IV injection. PET scan acquisition;(up to 4.5 hours)
- Plasma and blood radioactivity analysis(up to 7 hours)