Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: New multimodal fluorinated and iodinated radiotracers

摘要

This study reports a series of 14 new iodinated and fluorinated compounds offering both early imaging (~(123)I, ~(124)I, ~(18)F) and systemic treatment (~(131)I) of melanoma potentialities. The biodistribution of each ~(125)I-labeled tracer was evaluated in a model of melanoma B16F0-bearing mice, using in vivo serial γ scintigraphic imaging. Among this series, [~(125)I]56 emerged as the most promising compound in terms of specific tumoral uptake and in vivo kinetic profile. To validate our multimodality concept, the radiosynthesis of [~(18)F]56 was then optimized and this radiotracer has been successfully investigated for in vivo PET imaging of melanoma in B16F0- and B16F10-bearing mouse model. The therapeutic efficacy of [~(131)I]56 was then evaluated in mice bearing subcutaneous B16F0 melanoma, and a significant slow down in tumoral growth was demonstrated. These data support further development of 56 for PET imaging (~(18)F, ~(124)I) and targeted radionuclide therapy (~(131)I) of melanoma using a single chemical structure.