Clinical Phase I Study of the Hypoxic Cell Radiosensitizer RO-07-0582, A 2-Nitroimidazole Derivative

Abstract

RO-07-0582 [1-(2-nitroimidazolyl)-3-methoxyisopropanol] toxicity studies were performed in 12 patients for a total of 16 assays. Single and multifraction dose schedules were used, and drug concentrations in solid tumor tissue, CSF and blood (at 14-24 h) were established. A severe peripheral neuropathy occurred in 1 patient on the multifraction regimen when the total dosage reached 24 g. Drug absorption and concentration in the blood do not significantly differ from that of metronidazole. Maximum blood levels were reached at from 2-4 h, and several days subsequent to administration stabilized to levels only slightly above control levels.