Pharmacokinetics of guanazole in man

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Abstract
Guanazole, 3,5‐diamino‐1,2,4‐triazole, synthesized nearly a century ago, has recently been shown to have antitumor properties. In patients with cancer, intravenous doses ranging from 3.5 to 10 gm per square meter of body surface area have been used. It was found that the 15 minute plasma level declines to one‐half in 1 to 2 hours. After 4 to 6 hours the plasma half‐life is 5 to 10 hours. The drug is eliminated almost quantitatively in the urine in 24 hours. No metabolites could be detected in the perfusate or bile of the isolated perfused rat liver preparation, suggesting that the drug itself rather than a metabolite is responsible for the antitumor activity.

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