Abstract
Although the radiosensitizer misonidazole is now being used widely in clinical trials, much more information is required concerning its metabolism and routes of excretion. This information will be useful in optimizing ways of using the drug in order to reduce peripheral neuropathy, which is its main dose-limiting toxicity, and in the design and development of new drugs structurally related to misonidazole. Flockhart et al. (1978) have investigated urinary excretion in man and shown that only 10–20% of the administered dose of misonidazole is excreted in the urine in the first 24 hours as unchanged drug, plus its o-demethylated metabolite (Ro–05 9963). Less than 1% is excreted as misonidazole glucuronide, while a study using 14C labelling showed that only 2% is excreted as amine derivative.
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