Clinical and clinical pharmacologic studies of aziridinylbenzoquinone.
Thirty patients were entered in a phase I trial of aziridinylbenzoquinone (AZQ). These patients were treated with a single iv dose of AZQ daily for 5 days at doses ranging from 0.5 mg/m2 to 10.0 mg/m2. The dose-limiting and only significant toxic effects were leukopenia and thrombocytopenia, which appeared with relative consistency at iv dosages of 4.0--4.5 mg/m2/day x 5 in patients with extensive prior treatment and 7.0 mg/m2/day x 5 in patients with little prior treatment. One patient with colon cancer achieved a partial response of 4+ months. No other evidence of antitumor activity was observed. Pharmacologic studies revealed that the drug disappeared from the plasma in a biphasic manner (alpha-half-life = 1.5 minutes, beta-half-life = 18 minutes). With our method of analysis by high-performance liquid chromatography, no metabolites were found in the serum.
D000328:Adult; D000368:Aged; D000970:Antineoplastic Agents / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use*; D001388:Aziridines / Q000009:adverse effects / Q000378:metabolism / Q000627:therapeutic use*; D001389:Azirines / Q000627:therapeutic use*; D016227:Benzoquinones; D053138:Cyclohexenes; D004341:Drug Evaluation; D005260:Female; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D007970:Leukopenia / Q000139:chemically induced; 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