Metabolism of borono-phenylalanine-fructose complex (BPA-fr) and borocaptate sodium (BSH) in cancer patients--results from EORTC trial 11001

J Pharm Biomed Anal. 2010 Jan 5;51(1):284-7. doi: 10.1016/j.jpba.2009.08.018. Epub 2009 Aug 22.

Abstract

Within the clinical trial EORTC 11001, patients were infused with (10)B-enriched borono-phenylalanine-fructose complex (BPA-fr), or borocaptate sodium (BSH) solutions, which are used as boron carriers for boron neutron capture therapy. Urine samples were periodically collected and analyzed by (10)B NMR spectroscopy. The results revealed time-dependent metabolic changes of the administered compounds. BPA-fr dissociated to the constituents BPA and fructose, and the borate group was partly cleaved from BPA. BSH was partly aggregated to a dimer form, BSSB. These observations were previously reported for cultured cells and animal models, and are confirmed here in human cancer patients.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Borohydrides / metabolism*
  • Borohydrides / urine
  • Boron Compounds / chemistry
  • Boron Compounds / metabolism*
  • Boron Compounds / urine
  • Boron Neutron Capture Therapy / methods*
  • Carcinoma, Squamous Cell / therapy
  • Clinical Trials as Topic
  • Fructose / chemistry
  • Head and Neck Neoplasms / therapy
  • Humans
  • Magnetic Resonance Spectroscopy / methods
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / chemistry
  • Phenylalanine / metabolism
  • Phenylalanine / urine
  • Sulfhydryl Compounds / metabolism*
  • Sulfhydryl Compounds / urine
  • Time Factors

Substances

  • Borohydrides
  • Boron Compounds
  • Sulfhydryl Compounds
  • mercaptoundecahydrododecaborate
  • Fructose
  • Phenylalanine
  • 4-boronophenylalanine