Bioavailability of Intravenous Formulations of P-Boronophenylalanine in Dog and Rat
Boron neutron capture therapy (BNCT) is being developed as a treatment for malignant melanoma. P-boronophenyialanine (BPA) was initially proposed as a boron (B) delivery drug for BNCT of malignant melanoma because it was postulated that this B-containing amino acid, by mimicking a melanin precursor, would selectively accumulate in melanoma cells. BPA does seem to selectively accumulate in melanocytes, apparently as a result of uptake by an amino acid transport system1. For successful BNCT, tumor B concentrations of at least 20 ppm are thought to be necessary, but higher tumor B levels are desirable. Calculations2 indicate that for a given neutron exposure, each doubling of the tumor B concentration should increase tumor cell kill by a factor of about 10,000. Thus, even modest increases in the amount of B in tumor cells can dramatically improve the effectiveness of BNCT as a cancer treatment.
KeywordsMelanoma Cell Boron Neutron Capture Therapy Peak Serum Level Amino Acid Transport System Neutron Exposure
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