PHARMACOLOGY AND TOXICOLOGY OF ALPHA-2'-DEOXYTHIOGUANOSINE IN CANCER-PATIENTS

  • 1 January 1979
    • journal article
    • research article
    • Vol. 63  (1) , 53-57
Abstract
.alpha.-2''-Deoxythioguanosine (.alpha.-TGdR) was administered as a single dose to 13 cancer patients in 18 experiments at dose levels of 150-1500 mg/m2 and as a daily dose to 22 patients in 42 experiments at dose levels of 100-4000 mg/m2 per day .times. 5 days. No significant toxicity was observed. Blood levels and rates of excretion were determined with radiosulfur-labeled .alpha.-TGdR. Approximately 80% of the dose was excreted in the urine in 24 h, initially as unchanged .alpha.-TGdR and increasingly as metabolites. Metabolites appear to be nucleosides and do not include 6-thioguanine, 6-thioxanthine, or 6-thiouric acid to any measurable extent. Small amounts of the .alpha.-TGdR in blood samples were bound to albumin and to rbc [red blood cell] membranes. Blood plasma levels of .alpha.-TGdR at the highest doses were in the range of 200-300 .mu.M, declining in 24 h to 67-124 .mu.M.

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