Targeting Disseminated Melanoma with Radiolabelled Methylene Blue: Comparative bio-distribution studies in man and animals

Authors

  • Eva M. Link Department of Molecular Pathology, University College London School of Medicine, Cleveland Street, London, UK
  • Durval C. Costa Institute of Nuclear Medicine, University College London School of Medicine, Mortimer Street, London, UK
  • Dominic Lui Institute of Nuclear Medicine, University College London School of Medicine, Mortimer Street, London, UK
  • Peter J. Ell Institute of Nuclear Medicine, University College London School of Medicine, Mortimer Street, London, UK
  • Philip J. Blower Department of Nuclear Medicine, Kent and Canterbury Hospital, Canterbury, UK
  • Margaret F. Spittle The Meyerstein Institute of Clinical Oncology, Middlesex Hospital of University College London Hospitals, London, UK

DOI:

https://doi.org/10.3109/02841869609101650

Abstract

Targeted radiotherapy for pigmented melanoma with 3, 7-(dimethylamino) phenazathionium chloride [methylene blue (MTB)] labelled with Astatine-211 (211At; α-particle emitter) proved to be very effective in animal model systems. Since the results justified an introduction of the treatment to the clinic, the aim of the bio-distribution studies using [123I]-MTB and [131I]-MTB in patients was to confirm selectiveness of radiolabeled MTB uptake in melanoma lesions. The investigations were carried out using planar and SPECT (single photon emission computed tomography) γ-cameras. A stable uptake of radioiodinated MTB was found in pigmented melanomas in man, with tumour/surrounding tissue and tumour/blood ratios amounting to 9 at 19 h after a single i.v. injection. A time-dependent kinetics of radioiodinated MTB distribution was similar to that observed in human melanoma-bearing athymic mice. Blood radioactivity decreased by about 90% during the first 2.5 min after i.v. injection of the compound (T1/2bioi=0.58 min). Its retention time in various organs was either the same or very similar to that characteristic of the blood. A rapid uptake of radioiodinated MTB in the liver and kidneys confirmed the importance of these organs in excreting the compound: 25-30% of the radioactivity administered was expelled with urine over the first 24 h after the injection. There was no obvious retention of radioiodinated MTB in the brain over the observation period and in the eyes for at least the first 14 h

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Published

1996-01-01

How to Cite

Link, E. M., Costa, D. C., Lui, D., Ell, P. J., Blower, P. J., & Spittle, M. F. (1996). Targeting Disseminated Melanoma with Radiolabelled Methylene Blue: Comparative bio-distribution studies in man and animals. Acta Oncologica, 35(3), 331–341. https://doi.org/10.3109/02841869609101650