Targeting melanoma with 211At/131I-methylene blue: preclinical and clinical experience

Hybridoma. 1999 Feb;18(1):77-82. doi: 10.1089/hyb.1999.18.77.


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.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Astatine
  • Drug Carriers
  • Humans
  • Iodine Radioisotopes / administration & dosage
  • Iodine Radioisotopes / therapeutic use*
  • Melanoma / diagnosis
  • Melanoma / radiotherapy*
  • Methylene Blue / therapeutic use*
  • Mice


  • Drug Carriers
  • Iodine Radioisotopes
  • Methylene Blue
  • Astatine