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• W4665823 abstract "BS>Investigations were conducted on tritiated derivatives of 2-methyl-1, 4-naphthaquinol-bis-disodium phosphate (Synkavit, or Compound 1) for selective irradiation of tumors. This compound, investigated since 1946 as a therapeutic radiosensitizer, was found unexpectedly to concentrate to some extent selectively in the malignant cells of some human and animal tumors. Investigations with Compound 1 labeled with C/sup 14/ in the methyl group confirmed its uptake and retention in some human tumors, and Compound 1 was labeled with tritium in position 3 of the nucleus, but the product had too low a specific activity for clinical use. Studies were also done on the tritiated drug 2-methyl-5, 6,7- tritritio-1,4-naphthaquinol-bis-disodium phosphate, which has 3 firmly bound tritium atoms per molecule and a specific activity of 87.3 mu C/millimole with 1 mu C contained in 4.88 mg of compound. The tritium is introduced by reductive dehalogenation of the corresponding tribromo derivative, 2-methyl-5,6,7-trib romo- 1,4-naphthaquinol-bisdisodium phosphate using carrier-free tritium in the presence of a catalyst. It is referred to as TRA 119. A method of tritiation was devised which made it possible to obtain a compound containing approximately 1 atom of tritium per molecule with the tritium firmly bound. This compound is 2- methyl-6-tritio-1,4-naphthaquinol-bis-disodium phosphate, TRA 72. Itmore » was used in the treatment of 21 patients seriously ill with advanced, recurrent, radioresistart, or refractory malignant disease. Temporary improvement was observed in 5 and probably some improvement in a further 4 cases. Specific activity of biopsied specimens of tumor was almost invariably higher than that of bone marrow and of skeletal muscle, often by a factor of 3 and sometimes of 6 to 7. Similar therapeutic results were obtained with TRA 119, and no toxic effects were noted when single intravenous doses of 9.6 to 10.9 c of TRA 119 were administered. For most of the specimens of tumor taken 30 min after administration of THA 119, the specific activity was between 25 and 300 mu C/g of wet tissue. The results of the autoradiographic and related studies also provided evidence for selective concentration of TRA 119 in tumor cells in relation to normal cells in some cases of certain types of malignant disease. The estimated doses of radiation delivered by the tritium were consistent with the clinical findings that after intravenous injection of TRA 119, palliative effects may be produced in cases of highly radiosensitive conditions, such as testicular seminoma and Hodgkin's disease, and also in certain cases of slowly progressive recurrent adenocarcinoma of the gastrointestinal tract. (BBB)« less" @default.
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• W4665823 date "1963-08-01" @default.
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• W4665823 title "An Attempt to Develop a Radioactive Drug for Cancer Therapy" @default.
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• W4665823 doi "https://doi.org/10.1177/003591576305600808" @default.
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