The pharmacokinetics of p-Boronophenylalanine.fructose in human patients with glioma and metastatic melanoma.
OBJECTIVE
To study the biodistribution of p-Boronophenylalanine in patients undergoing surgery for intracranial tumors or metastatic melanoma.


METHODS
D,L-p-Boronophenylalanine was administered as boronophenylalanine.fructose in an intravenous bolus 1-4 h before the operation. Blood samples were collected for 24 h from the time of administration of the compound, and the blood boron elimination parameters were determined. For the glioma patients tumor samples were obtained and skin, dura, periosteum, and surrounding brain samples were collected whenever possible. For the metastatic melanoma patients tumor, fat, skin, and muscle were collected. Determination of the boron content was performed using inductively coupled plasma-atomic emission spectrometry. Twelve melanoma patients and six glioma patients participated in the study. The melanoma patients included four cases of cutaneous metastatic melanoma, six cases of metastatic melanoma to the lymph nodes and two cases of cerebral metastasis.


RESULTS
The results for the metastatic melanoma patients are encouraging with an average tumor:blood boron concentration ratio and standard deviation of about 4.4 +/- 3.2 and a maximum value of 10 for the cerebral metastasis. The glioma patients involved high grade glioma for which the tumor:blood ratio was 2.2 +/- 1.2.


CONCLUSIONS
The tumor:blood ratios for melanoma fulfil requirements for epithermal boron neutron capture therapy for cerebral melanoma metastases, whereas those for high grade glioma do not.
Mallesch
J L
JL
University of Sydney, NSW, Australia.
Moore
D E
DE
Allen
B J
BJ
McCarthy
W H
WH
Jones
R
R
Stening
W A
WA
D001895:Boron / Q000097:blood; D001896:Boron Compounds / Q000493:pharmacokinetics*; D016754:Boron Neutron Capture Therapy; D001932:Brain Neoplasms / Q000378:metabolism* / Q000532:radiotherapy; D005910:Glioma / Q000378:metabolism* / Q000532:radiotherapy; D006801:Humans; D008545:Melanoma / Q000378:metabolism* / Q000532:radiotherapy / Q000556:secondary; D010649:Phenylalanine / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D011838:Radiation-Sensitizing Agents / Q000493:pharmacokinetics*
D001896:Boron Compounds; D011838:Radiation-Sensitizing Agents; D010649:Phenylalanine; D001895:Boron; C033685:4-boronophenylalanine