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.
D000328:Adult; D000368:Aged; D000873:Anthracenes / Q000008:administration & dosage / Q000627:therapeutic use / Q000633:toxicity*; D000970:Antineoplastic Agents / Q000633:toxicity*; D004305:Dose-Response Relationship, Drug; D004334:Drug Administration Schedule; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009369:Neoplasms / Q000188:drug therapy*
D000873:Anthracenes; D000970:Antineoplastic Agents; C031404:bisantrene