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Anti‐melanoma efficacy of internal radionuclide therapy in relation to melanin target distribution
Author(s) -
Bonnet M.,
Mishellany F.,
Papon J.,
Cayre A.,
PenaultLlorca F.,
Madelmont J. C.,
MiotNoirault E.,
Chezal J. M.,
Moins N.
Publication year - 2010
Publication title -
pigment cell and melanoma research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.618
H-Index - 105
eISSN - 1755-148X
pISSN - 1755-1471
DOI - 10.1111/j.1755-148x.2010.00716.x
Subject(s) - melanin , melanoma , in vivo , radiation therapy , distribution (mathematics) , microphthalmia associated transcription factor , medicine , targeted therapy , in vitro , cancer research , tyrosinase , pathology , dermatology , chemistry , biology , cancer , enzyme , biochemistry , microbiology and biotechnology , mathematical analysis , mathematics
Summary 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.