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Selective Delivery of Boron by the Melanin Precursor Analogue p-Boronophenylalanine to Tumors Other than Melanoma ¹

Medical Department, Brookhaven National Laboratory, Upton, New York 11973; Mt. Sinai School of Medicine, New York, New York 10029; and Institute of Molecular Immunology, Center for Molecular Medicine and Immunology, University of Medicine and Dentistry of New Jersey, Newark, New Jersey 07103

The melanin precursor analogue p-boronophenylalanine (BPA) has been used to deliver ¹⁰B to melanoma tissue for boron neutron capture therapy. Uptake studies in tumor models other than melanoma now indicate that BPA is capable of delivering therapeutic amounts of boron to tumors other than melanoma. The KHJJ murine mammary tumor carried s.c. in BALB/c mice, the GS-9L rat glioma carried both s.c. and intracranially in F-344 rats, and the human U-87 MG glioma xenograft carried s.c. in nude mice have all shown significant accumulation of boron in tumor tissue following single p.o. (intragastric) doses of BPA. In the KHJJ mammary tumor, the L isomer of BPA was preferentially accumulated compared to the D isomer, indicative of a carrier-mediated transport process. Double-label, whole-body autoradiographic studies in a pigmented murine melanoma have shown that the boron distribution (from BPA) differs from the distribution of a tritiated melanin precursor (tyrosine). Boron accumulated only in the tumor; labeled tyrosine accumulated in tumor, liver, intestinal epithelium, bone marrow, and secretory glands. Toxicity studies in mice and rabbits indicate that, even at very high doses, BPA p.o. caused no adverse effect in tissues, on blood chemistry, or on differential leukocyte counts. These data indicate that BPA may be generally useful as a boron delivery agent for boron neutron capture therapy of tumors.

¹ This work was supported in part by Grants CA42446 (J. A. C.), DK10080 (J. D. G.), and CA43455 (I. F.) from the NIH and by Contract DE-AC02-76CH00016 with the United States Department of Energy. Accordingly the United States Government retains a nonexclusive, royalty-free license to publish or reproduce the published form of this contribution or allow others to do so for United States Government purposes.

² To whom requests for reprints should be addressed at Medical Department, Brookhaven National Laboratory, Upton, NY 11973.

Received 6/14/89. Revised 9/18/89. Accepted 10/ 2/89.

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