Development of 18F-labeled picolinamide probes for PET imaging of malignant melanoma

摘要

Melanoma is an aggressive skin cancer with worldwide increasing incidence. Development of positron emission tomography (PET) probes for early detection of melanoma is critical for improving the survival rate of melanoma patients. In this research, ~(18)F-picolinamide-based PET probes were prepared by direct radiofluorination of the bromopicolinamide precursors using no-carrier-added ~(18)F-fluoride. The resulting probes, ~(18)F-1, ~(18)F-2 and ~(18)F-3, were then evaluated in vivo by small animal PET imaging and biodistribution studies in C57BL/6 mice bearing B16F10 murine melanoma tumors. Noninvasive small animal PET studies demonstrated excellent tumor imaging contrasts for all probes, while ~(18)F-2 showed higher tumor to muscle ratios than ~(18)F-1 and ~(18)F-3. Furthermore, ~(18)F-2 demonstrated good in vivo stability as evidenced by the low bone uptake in biodistribution studies. Collectively, these findings suggest ~(18)F-2 as a highly promising PET probe for translation into clinical detection of melanoma.