Abstract
The physiologic disposition of radioactive-labelled CCNU and MeCCNU was studied in patients receiving these drugs as part of their early clinical trial. CCNU was given orally in doses of 30–100 mg/m2 and MeCCNU in doses of 120–290 mg/m2. With both drugs, significant plasma levels of radioactivity were detected in as early as 10 min. with peak levels occurring at 1 to 6 hours. Plasma levels of isotope were prolonged, and the patterns of decline of radioactivity from plasma were similar for the same labelled moieties of CCNU and MeCCNU. Approximately 60% of the radioactivity given was excreted in the urine within 48 hours and of this more than 50% was excreted in the first 12 hours. Radioactivity was found in the cerebrospinal fluid of patients given both drugs, and, with CCNU, these levels paralleled concurrent plasma levels. The degradation of both drugs appears to be extremely rapid since the intact drug could not be detected in any plasma, CSF, or urine sample.
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