Targeting melanoma with 211At/131I-methylene blue: preclinical and clinical experience.
The increasing incidence of melanoma and a lack of effective therapy have stimulated a search for new methods of early detection and treatment of the disease. Melanin synthesized in melanoma cells presents a unique target to which the treatment can be selectively addressed, provided the pigment is recognized by a suitable drug. Methylene blue possesses a high affinity for melanin and, therefore, accumulates preferentially in melanoma cells. Since not directly toxic to the tumor, methylene blue serves as a carrier for radioisotopes and, once taken up by melanoma cells, acts as a selectively localized source of radiation. Hence, radioderivatives of the compound can be used for diagnosis and therapy of disseminated melanoma. 131I-methylene blue in conjunction with gamma camera imaging has already proved in clinical studies to be a useful tool for the detection of early melanoma dissemination. 211At-methylene blue exceptional efficacy in treating melanoma and preventing its metastatic spread without damaging normal structures when administered systemically to human melanoma-bearing mice led to the approval of this alpha-particle emitting methylene blue derivative for the Phase I clinical trial.
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Department of Molecular Pathology, University College London Medical School, UK.
D000818:Animals; D001246:Astatine; D004337:Drug Carriers; D006801:Humans; D007457:Iodine Radioisotopes / Q000008:administration & dosage / Q000627:therapeutic use*; D008545:Melanoma / Q000175:diagnosis / Q000532:radiotherapy*; D008751:Methylene Blue / Q000627:therapeutic use*; D051379:Mice
D004337:Drug Carriers; D007457:Iodine Radioisotopes; D008751:Methylene Blue; D001246:Astatine