A unique in vivo assessment of 4-[10B]borono-L-phenylalanine in tumour tissues for boron neutron capture therapy of malignant melanomas using positron emission tomography and 4-borono-2-[18F]fluoro-L-phenylalanine

Melanoma Res. 1992 Sep;2(3):171-9. doi: 10.1097/00008390-199209000-00005.

Abstract

A unique in vivo approach to assessing the concentrations of 4-[10B]borono-L-phenylalanine (L-BPA), a melanoma targeting compound for boron neutron capture therapy (BNCT), was investigated using L-BPA labelled with positron-emitting 18F (half-life = 110 min), i.e., 4-[10B]borono-2-[18F]fluoro-L-phenylalanine (L-[18F]FBPA). High melanoma uptake of L-[18F]FBPA was reduced slightly by competition with L-BPA in the two animal models of the murine B16 melanoma and the melanotic Greene's melanoma No. 179 in hamsters. In mice given L-[18F]FBPA and L-BPA, the concentrations of 10B in B16 estimated from 18F radioactivity were lower than those measured by inductively coupled plasma-atomic emission spectroscopy. Lower estimated values were dependent on the time after injection and on the loading dose of L-BPA. The estimated 10B concentrations for Green's melanomas were comparable to the measured values. Positron emission tomography (PET) using L-[18F]FBPA allowed Greene's melanomas to be clearly visualized. In conclusion, when L-[18F]FBPA is used as a probe for L-BPA in BNCT of malignant melanomas, the melanoma can be localized and the 10B concentrations in tissues can be assessed in vivo using 18F radioactivity by PET.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Boron Compounds / pharmacokinetics*
  • Boron Compounds / therapeutic use
  • Cricetinae
  • Fluorine Radioisotopes
  • Melanoma, Experimental / diagnostic imaging*
  • Melanoma, Experimental / radiotherapy
  • Mesocricetus
  • Mice
  • Mice, Inbred C57BL
  • Neoplasm Transplantation
  • Neutron Capture Therapy*
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / pharmacokinetics
  • Phenylalanine / therapeutic use
  • Tissue Distribution
  • Tomography, Emission-Computed

Substances

  • Boron Compounds
  • Fluorine Radioisotopes
  • 4-borono-2-fluorophenylalanine
  • Phenylalanine
  • 4-boronophenylalanine