Phase I clinical evaluation of 9,10-anthracenedicarboxyaldehyde[bis(4,5-dihydro-1H-imidazol-2-yl)hydrazone]dihydrochloride (bisantrene).

9,10-Anthracenedicarboxyaldehyde[bis(4,5-dihydro-1H-imidazol-2-y1)-hydrazone ]dihydrochloride (bisantrene) is one of a series of anthracenedicarboxyaldehyde compounds that has significant antitumor activity similar to that of doxorubicin in experimental mouse tumor systems. A phase I clinical study was conducted using a weekly x 3 schedule. Twenty-six patients with a wide variety of advanced malignant solid tumors received a total of 39 courses of the drug at doses ranging from 40 to 180 mg/m2/week x 3. Leukopenia was the dose-limiting toxic effect. Other toxic effects included malaise, which was observed in 49% of the courses, nausea and vomiting in 36%, fever in 21%, and phlebitis in 21%. No responses were observed in this study. For phase II studies, using this schedule, a starting dose of 150 mg/m2/week x 3 repeated every 4-5 weeks is recommended. In patients who have received minimal or no therapy, the starting dose should be 180 mg/m2.