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Synthesis, Tissue Uptake, and Toxicity of a Nickel Tetracarboranylphenylporphyrin

  • Michiko Miura
  • Peggy L. Micca
  • Jason A. Donaldson
  • John C. Heinrichs
  • John A. Shelnutt
  • Gerald C. Finkel
  • Daniel N. Slatkin

Abstract

Porphyrins have been used for boron neutron capture therapy [BNCT] and photodynamic therapy [PDT] of experimental rodent tumors. PDT requires much less porphyrin than BNCT, typically 5 μg as compared to > 200 μg per gram body weight [gbw]. Toxicity is a major consideration in the use of boronated drugs for BNCT. At 265 μg/gbw, a boronated porphyrin, VCDP [1] (Figure 1) delivered 40 μg B/g to tumor tissue 4 days after the last of 12 intraperitoneal [ip] injections.1 There was transient hematologic and hepatic toxicity. If the VCDP dose rate was kept low (22 μg/gbw per ip injection; 12 injections over 4 days), lethality was under 10%. A tetraphenylporphyrin [2] containing four meta-nido-carborane cages was synthesized2 and when tested in mice found to be much more toxic than VCDP.

Keywords

Boron Concentration Boron Neutron Capture Therapy Diacetic Acid Boron Analysis Carborane Cage 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer Science+Business Media New York 1996

Authors and Affiliations

  • Michiko Miura
    • 1
  • Peggy L. Micca
    • 1
  • Jason A. Donaldson
    • 1
  • John C. Heinrichs
    • 1
  • John A. Shelnutt
    • 2
  • Gerald C. Finkel
    • 3
  • Daniel N. Slatkin
    • 1
  1. 1.Medical DepartmentBrookhaven National LaboratoryUptonUSA
  2. 2.Fuel Science DepartmentSandia National LaboratoryAlbuquerqueUSA
  3. 3.Thomas Jefferson UniversityPhiladelphiaUSA

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