An Open-label Phase I Study to Assess Safety, Dosimetry and Biodistribution of the Radiotracer 18F-ML-10 in Healthy Volunteers
An open-label, non-randomized phase I clinical trial was performed to evaluate the safety of [18F]-ML-10. A single dose was injected intravenously to healthy volunteers (n=8), followed by continuous safety monitoring, repeated assessment of tracer biodistribution, and evaluation of tracer stability in vivo. Dosimetry calculations were performed to generate estimates of radiation doses to the various organs.
In addition, subjects were monitored at two follow-up visits, performed on days 3 and 7 after the administration.
All 8 subjects completed the study, with no deviations in any of the measured safety parameters throughout the study. All subjects felt well; no adverse events were reported, all vital signs were normal and no cardiovascular effects (ECG) were observed.
ML-10 manifested very high stability in vivo; with over 97.5% of the tracer being intact in the plasma at 150 minutes after administration. Biodistribution assessment revealed rapid distribution of [18F]-ML-10 in the extracellular space; no binding of the tracer to non-target tissues, including the brain; and rapid excretion of the tracer through the urine. All organs manifested low radiation doses, within the range for other PET tracers approved by the FDA for general marketing.
In addition, clear, specific uptake was demonstrated in the testes of all male subjects. It is known that 7% to 10% of sperm cells undergo apoptosis at any given time, as a natural "quality control" process to eliminate potentially defective sperm. This has been confirmed histologically in an animal model with fluorescent ML-10.