Anti-melanoma efficacy of internal radionuclide therapy in relation to melanin target distribution.

Autor: Bonnet, M., Mishellany, F., Papon, J., Cayre, A., Penault-Llorca, F., Madelmont, J. C., Miot-Noirault, E., Chezal, J. M., Moins, N.
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Zdroj: Pigment Cell & Melanoma Research; Oct2010, Vol. 23 Issue 5, pe1-e11, 11p, 1 Color Photograph, 1 Black and White Photograph, 2 Diagrams, 1 Chart, 2 Graphs
Abstrakt: Targeted internal radionuclide therapy (TRT) could be an efficient, specific way to treat disseminated melanoma. Based on a previous pharmacomodulation study, we selected a quinoxaline-derived molecule (ICF01012) for its melanin specificity and kinetic properties suitable for TRT. Here, we determined the efficacy of [131I]ICF01012 radiotherapy in vitro and in vivo in relation to melanogenesis using human melanoma models. [125I]ICF01012 uptake was first assessed in relation to melanin content. We found that melanin distribution in different models was representative of pathology seen in human tumours: melanin content was high in the extracellular space of SKMel3 tumours, and accumulated primarily in melanophages in M4Beu tumours. Targeted [131I]ICF01012 radiotherapy had a strong anti-tumoural efficacy in pigmented versus unpigmented tumours, regardless of target distribution and content. This study supports the use of melanin targeting with 131I-labelled iodoquinoxaline for effective treatment of melanoma. [ABSTRACT FROM AUTHOR]
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