Ibenzmethyzin was administered to 35 patients with neoplastic diseases. In 6 patients, daily, semiweekly, or weekly injections of 300 to 1,600 mg. per square meter were given. The adverse reactions were gastrointestinal and neurologic: nausea, vomiting, ataxia, confusion, and somnolence. When given in daily oral doses of 125 to 300 mg. per square meter, the drug caused nausea and vomiting and bone marrow depression. With oral administration, a dose of 125 mg. per square meter with interruption rather than downward modification to prevent bone marrow toxicity is recommended. Antitumor activity was seen in 5 of 10 patients with Hodgkin's disease and one with malignant melanoma. It is suggested that ibenzmethyzin metabolism or binding at the active site may be rate limiting.
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DeVita et al. (1966) studied this question.