Clinical trial NCT05136391: A Phase I Study to Evaluate XTR003 in Healthy Chinese Volunteers
Official title: A Phase I Study to Evaluate the Safety, Biodistribution, Radiation Dosimetry, and Pharmacokinetics of XTR003 in Healthy Chinese Volunteers
Study type: INTERVENTIONAL
Overall status: COMPLETED
Phase: PHASE1
Conditions: Coronary Artery Disease (CAD)
Keywords: coronary artery disease; positron emission tomography (PET)
Lead sponsor: Sinotau Pharmaceutical Group
Sponsor class: INDUSTRY
First posted: 2021-11-29
Enrollment: 10
Sex: ALL
Minimum age (years): 18
Maximum age (years): 40
Standard ages: ADULT
Accepts healthy volunteers: yes
Allocation: NA
Intervention model: SINGLE_GROUP
Primary purpose: DIAGNOSTIC

Brief summary: 18F-FDG PET imaging is now considered the most effective method used in the clinical evaluation of viable myocardium. However, the need for fasting or glucose and insulin loading in the 18F-FDG PET protocol makes it unfavorable for a certain group of patients (i.e., insulin-resistance and diabetic patients). XTR003 is a fatty acid analog used for PET imaging, developed at the Beijing Anzhen Hospital affiliated to Sinotau Pharmaceutical Group. XTR003 is a promising fatty acid analog and perhaps have a potential clinical utility in the evaluation of viable myocardium. This phase I study investigated the safety, biodistribution, radiation dosimetry and Pharmacokinetics of XTR003 in 10 Chinese normal healthy volunteers both male and female between the ages of 18-40.

Detailed description: XTR003 is a PET imaging radiopharmaceutical agent used to trace myocardial fatty acid metabolism. XTR003 is a modified fatty acid that enters the myocytes and passes through mitochondrial membrane by the same process as the natural existing fatty acids and then undergoes partial β-oxidation before being trapped in the mitochondria. In preclinical study XTR003 showed high myocardial uptake and retention \[1\].

This is a phase I study, the study will be open-label, nonrandomised, single-arm, single-center clinical study. Subjects will receive single dose of XTR003.

Safety, biodistribution, radiation dosimetry and Pharmacokinetics was investigated.

Eligibility criteria: Inclusion Criteria:

1. Men and women aged between 18-40 years
2. Normal electrocardiogram and echocardiography
3. Normal vital signs and physical examination
4. No any major illness
5. No clinically significant abnormalities in laboratory tests
6. No clinically significant anomalies in 12-lead ECG
7. Females of child bearing possibility should adopt effective medically approved contraceptive methods to prevent pregnancy for at least 6 months before the study and after the study
8. Voluntarily signed written consent from all subjects

Exclusion Criteria:

1. Pregnancy or lactating woman
2. History of cardiovascular disease
3. History of any brain disease
4. History of coagulopathy
5. History of liver or gastrointestinal diseases or other factors that can interfere with drug absorption, distribution, excretion or metabolism
6. Past history of cancer
7. History of drug allergy
8. History of drug abuse or alcohol dependance
9. Any medications and treatments that may interfere with the test data or may cause serious side effects
10. Human immunodeficiency virus (HIV), hepatitis C or syphilis antibody test positive, hepatitis B surface antigen positive
11. Exposure to significant occupational radiation (e.g \>50 mvs/year) or exposure radioactive substances for therapeutic or research purposes over the past 10 years
12. Use of health products or medications (eg. coenzyme Q10, etc.) that have an effect on myocardial energy metabolism within 1 week
13. Hospital admission due to illness during the screening period

Primary outcomes:
measure: To evaluate the safety of healthy Chinese adults after a single dose of XTR003 intravenous injection. On Day1 of the study all subjects received a single dose 8.0-10 mCi of XTR003 intravenously.
timeFrame: 0 to 14 days post injection
Secondary outcomes:
measure: To investigate the biodistribution of XTR003
timeFrame: 0 to 5 hours
Other outcomes:
Locations:
city: Beijing
country: China
facility: Beijing Anzhen Hospital
state: Beijing
Study officials:
References:
citation: Shoup TM, Elmaleh DR, Bonab AA, Fischman AJ. Evaluation of trans-9-18F-fluoro-3,4-Methyleneheptadecanoic acid as a PET tracer for myocardial fatty acid imaging. J Nucl Med. 2005 Feb;46(2):297-304.