Pharmacokinetics of a new water-soluble nitrosourea derivative (ACNU) in human gliomas

The pharmacokinetics of a newly developed water-soluble nitrosourea derivative (ACNU) following a single intravenous injection was investigated in 11 patients with gliomas. A major portion of ACNU was excreted within 2 hours. The distribution rate was very fast, and the elimination rate tended to be slow. More than 50% of ACNU moves into the tissue compartment. ACNU tended to move into glioma tissue well. The ACNU level in glioma tissue was above 1.0 microgram/gm 30 to 60 minutes ater injections. ACNU was detected at a higher concentration in malignant gliomas than in benign gliomas. These results suggest that ACNU is taken up by tumor tissue relatively rapidly and eliminated slowly, which leads to effective manifestation of its antitumor activity.