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

Autor: M, Bonnet, F, Mishellany, J, Papon, A, Cayre, F, Penault-Llorca, J C, Madelmont, E, Miot-Noirault, J M, Chezal, N, Moins
Rok vydání: 2010
Předmět:
Zdroj: Pigment cellmelanoma research. 23(5)
ISSN: 1755-148X
Popis: 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.
Databáze: OpenAIRE