Single photon emission computed tomography/positron emission tomography imaging and targeted radionuclide therapy of melanoma: new multimodal fluorinated and iodinated radiotracers.
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| Abstract |
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.
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| Authors | Aurélie Maisonial, Bertrand Kuhnast, Janine Papon, Raphaël Boisgard, Martine Bayle, Aurélien Vidal, Philippe Auzeloux, Latifa Rbah, Mathilde Bonnet-Duquennoy, Elisabeth Miot-Noirault, Marie-Josèphe Galmier, Michèle Borel, Serge Askienazy, Frédéric Dollé, Bertrand Tavitian, Jean-Claude Madelmont, Nicole Moins, Jean-Michel Chezal |
| Journal | Journal of medicinal chemistry (J Med Chem) Vol. 54 Issue 8 Pg. 2745-66 (Apr 28 2011) ISSN: 1520-4804 [Electronic] United States |
| PMID | 21417462 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't) |
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