Phase I trial of 5-day continuous infusion aziridinylbenzoquinone (AZQ, diazaquone, NSC 182968).
AZQ was given to 14 patients with solid tumors in a phase I trial. Eight males and six females with a median Karnofsky performance status of 70% (range 40-90%) and a median age of 64 years (range 24-72) received 18 evaluable courses. All patients received prior chemotherapy and seven had prior irradiation. A continuous infusion for 5 consecutive days at doses of 4-8 mg/m2 per day was given every 3-4 weeks. Dose-limiting toxicity was myelosuppression, especially thrombocytopenia. No patient developed an infection while on this study. There was no evidence of cumulative toxicity in the three patients receiving two or more courses. Nonhematologic toxicity consisted only of mild nausea and vomiting in three patients and mild diarrhea in two patients. No patient experienced any mucosal, hepatic, renal, cardiac, or central nervous system toxicity. No objective antitumor responses were seen in the three patients with measurable disease who received two or more courses of AZQ. The recommended doses for phase II studies for continuous-infusion AZQ are 6 mg/m2/day X 5 repeated every 4 weeks.
D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000627:therapeutic use* / Q000633:toxicity; D001388:Aziridines / Q000627:therapeutic use* / Q000633:toxicity; D001389:Azirines / Q000627:therapeutic use*; D016227:Benzoquinones; D053138:Cyclohexenes; D004341:Drug Evaluation; D005260:Female; D006801:Humans; D008297:Male; D008875:Middle Aged; D009369:Neoplasms / Q000188:drug therapy*; D013921:Thrombocytopenia / Q000139:chemically induced
D000970:Antineoplastic Agents; D001388:Aziridines; D001389:Azirines; D016227:Benzoquinones; D053138:Cyclohexenes; C006052:2,5-bis(1-aziridinyl)-3,6-bis(2-methoxyethoxy)-4-benzoquinone