A Study of XTR004 Radiotracer in Healthy Volunteers

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.

Inclusion criteria

• 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

Exclusion criteria

• 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.