Pharmacology and toxicology of alpha-2'-deoxythioguanosine in cancer patients.

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/day X 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 hours, 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 erythrocyte membranes. Blood plasma levels of alpha-TGdR at the highest doses were in the range of 200--300 micrometer, declining in 24 hours to 67--124 micrometer.

• Authors: G A LePage, A Khaliq
• Journal: Cancer treatment reports (Cancer Treat Rep) Vol. 63 Issue 1 Pg. 53-7 (Jan 1979) ISSN: 0361-5960 [Print] United States
• PMID: 421233 (Publication Type: Journal Article)

Chemical References

• Antineoplastic Agents
• Thionucleosides
• alpha-2'-deoxythioguanosine
• Deoxyguanosine

Topics

• Antineoplastic Agents (adverse effects, metabolism, therapeutic use)
• Biotransformation
• Deoxyguanosine (adverse effects, metabolism, therapeutic use)
• Humans
• Kinetics
• Neoplasms (drug therapy, metabolism)
• Thionucleosides (adverse effects, metabolism, therapeutic use)