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Pigment Cell Melanoma Res. 2010 Oct;23(5):e1-11. doi: 10.1111/j.1755-148X.2010.00716.x. Epub 2010 Apr 22.

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

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  • 1UMR 990 INSERM/UdA-Imagerie Moléculaire et Thérapie vectorisée, Clermont-Ferrand, France.


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 [(131)I]ICF01012 radiotherapy in vitro and in vivo in relation to melanogenesis using human melanoma models. [(125)I]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 [(131)I]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 (131)I-labelled iodoquinoxaline for effective treatment of melanoma.

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