Biodistribution, Radiation Dosimetry, and Clinical Application of a Melanin-Targeted PET Probe, F-P3BZA, in Patients.

-(2-(diethylamino)-ethyl)-F-5-fluoropicolinamide (F-P3BZA) is a radiotracer that demonstrates high binding selectivity and affinity in melanoma. The aim of the present study was to estimate the biodistribution and clinical radiation dosimetry of F-P3BZA in healthy volunteers and perform a preliminary clinical application for PET/CT imaging in melanoma patients. F-P3BZA was produced efficiently with a radiosynthesizer. Six healthy volunteers were injected with F-P3BZA (211.7 ± 15.4 MBq) followed by serial whole-body PET/CT scans and blood tests to assess biodistribution, pharmacokinetic, and radiation dosimetry at 10 min, 1 h, 2 h, and 4 h after injection. The vital signs of volunteers were recorded in regular intervals during the imaging sessions. The effective dose for each subject after the medical internal radiation dosimetry schema was calculated with OLINDA/EXM software. For the preliminary clinical application, 5 patients with suspected melanomas underwent F-P3BZA PET/CT imaging at 10 min and 1 h after injection. All patients also underwent F-FDG PET/CT scans on the third day to compare the potential diagnostic ability of F-P3BZA with F-FDG. The radiochemistry yield of F-P3BZA labeling was 12.3% ± 3.9%, and the purity of F-P3BZA after purification and formulation was higher than 99.5%. The highest uptake of F-P3BZA was in the liver with an SUV of 8.3 ± 1.0 at 10 min after injection. The resultant whole-body effective dose was 0.0193 mSv/MBq. F-P3BZA showed high uptake and suggested an ability for specific imaging of melanoma and its metastasis in patients. The average SUV of F-P3BZA and F-FDG in tumors was 19.7 ± 5.3 and 10.8 ± 2.7 at 60 min after injection. Our study suggests that F-P3BZA is safe and compatible for clinical use. The first-in-human clinical application to melanoma showed favorable delineated tumors in patients, demonstrating the potential of F-P3BZA for diagnostic PET imaging of melanoma.