A Clinical Trial Evaluating the Safety and Tolerability, Biodistribution and Radiation Dosimetry, and Pharmacokinetics of Flotufolastat F-18 Injection in Healthy Chinese Adults

Flotufolastat F-18 Injection is a positron emission tomography (PET) imaging tracer that targets the extracellular domain of prostate-specific membrane antigen (PSMA). It is intended for the detection of prostate cancer (PCa) lesions.This Phase I study will be open-labeled, nonrandomized, single center study. Enrolled 6 healthy Chinese volunteers who meet all of the inclusion and none of the exclusion criteria. Subjects will receive 5.47~6.69mCi of Flotufolastat F-18 Injection via IV injection. Safety and tolerability will be observed. Biodistribution, pharmacokinetics, and dosimetry will be investigated.

Inclusion criteria

• Have the ability to understand the content of study and voluntarily sign the informed consent form.
• Healthy male or female, aged 18-60 (included).
• Body mass index (BMI) between 19 and 26 kg/m² (included).
• Vital signs, physical examination, 12-lead electrocardiogram (ECG), chest X-ray (posterior-anterior view), and abdominal ultrasound are normal, or any abnormalities that are diagnosed clinically insignificant.
• Clinical laboratory test results are within normal ranges or any abnormalities that are diagnosed clinically insignificant.
• Have the ability to communicate effectively with the investigator and comply with the study requirement to follow-up.
• Female subject shouldcontracept effectively during the study period and 6 months after the study completed (effective contraception includes sterilization, intrauterine hormonal devices, condoms, contraceptive pills/agents, abstinence, or partner vasectomy). Male subject should agree to use contraception during the study period and 6 months after the study completed.

Exclusion criteria

• Claustrophobia or inability to tolerate imaging examinations for any other reason.
• Have a history of epilepsy or seizures, excluding childhood febrile seizures.
• With chronic diseases, including but not limited to:

• cardiovascular, respiratory, gastrointestinal, urinary, hematological disease, neurological, endocrine, metabolic, or musculoskeletal diseases, or a history thereof.
• history of psychiatric disorders or currently significant psychiatric conditions
• Have a history of asthma or allergies.
• Have a history of malignant tumors.
• Present any condition that may interfere with the absorption or metabolism of the investigational drug, or that may affect study results, as determined by the investigator to be clinically significant.
• Underwent any surgical procedure within 3 months before administration or planned surgery during the study period.
• Accomplished the blood donation or significant blood loss (>400 mL) within 3 months before administration or during the screening period.
• Insufficient venous access (two distinct venous lines are required for investigational drug administration and PK sampling).
• Known allergy to the active ingredient or any excipients of the investigational product.
• Took any medications, including prescription, over-the-counter drugs, or herbal remedies, within 14 days before administration.
• Participated any other new drug's clinical trial within 4 weeks prior to the administration or within 5 half-lives of the investigating drug (whichever is longer).
• Radiopharmaceutical imaging or treatment within 7 days prior to screening or within 5 half-lives of the radiopharmaceutical (whichever is longer).
• Pregnant or breastfeeding women.
• Abnormal serological results (hepatitis B surface antigen, syphilis treponemal antibody, human immunodeficiency virus antibody, hepatitis C antibody) diagnosed clinically significant by the investigator.
• QTc intervalis longer than 450 milliseconds during the screening period.
• Major occupational exposure to ionizing radiation in the past 10 years (e.g., more than 50 mSv/year) or exposure to radioactive materials or ionizing radiation for therapeutic or research purposes.
• Any reason determined by the investigator that could not complet the study.