In vivo evaluation of phosphorous-containing derivatives of dodecahydro-closo-dodecaborate for boron neutron capture therapy of gliomas and sarcomas

Anticancer Res. Mar-Apr 2001;21(2A):841-6.


The in vivo uptake of dodecahydro-closo-dodecaborate derivatives substituted with phosphate- and bisphosphonate groups was evaluated in two different experimental tumor model systems and compared to other boronated and non-boronated compounds. These phosphorous-containing boron clusters may have potential for use in boron neutron capture therapy, a chemoradiotherapeutic form of cancer treatment. Using the F98 rat glioma as a brain tumor model in syngeneic Fischer rats, there was selective tumor uptake of the phosphate derivative with 21.5 micrograms boron/g tumor versus 5.2 micrograms/g normal brain and a tumor:blood ratio of 2.7. However, this compound was toxic to test animals and lethal at relatively low doses. The uptake of the bisphosphonate by the murine K8 osteosarcoma was approximately 18 micrograms boron/g tumor with a T:Bl ratio of 7.6 and a tumor:bone ratio of 1.5. This compound was non toxic to the test animals. The results indicate that phosphate- and bisphosphonate derivatives of dodecahydro-closo-dodecaborate may have potential for BNCT of gliomas and osteosarcomas, respectively.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Animals
  • Bone Neoplasms / metabolism
  • Bone Neoplasms / radiotherapy*
  • Boron Compounds / chemistry
  • Boron Compounds / metabolism
  • Boron Compounds / therapeutic use*
  • Boron Neutron Capture Therapy / methods*
  • Brain Neoplasms / metabolism
  • Brain Neoplasms / radiotherapy*
  • Diphosphonates
  • Glioma / metabolism
  • Glioma / radiotherapy*
  • Mice
  • Mice, Inbred BALB C
  • Molecular Structure
  • Neoplasms, Experimental / radiotherapy
  • Osteosarcoma / metabolism
  • Osteosarcoma / radiotherapy*
  • Phosphates
  • Phosphorus Compounds / chemistry
  • Phosphorus Compounds / metabolism
  • Phosphorus Compounds / therapeutic use*
  • Rats
  • Rats, Inbred F344
  • Technetium Tc 99m Medronate
  • Tissue Distribution
  • Tumor Cells, Cultured


  • Boron Compounds
  • Diphosphonates
  • Phosphates
  • Phosphorus Compounds
  • Technetium Tc 99m Medronate