Clinical Trial of the Cytostatic Agent A-139 (2,5-Bis[1-Aziridinyl]-3,6-bis[2-methoxyethoxy]-p-benzoquinone)^* Free

2,5-Bis[1-Aziridinyl]-3,6-bis(2-methoxyethoxy)-p-benzoquinone was given to a total of 89 patients with far advanced cancer in an attempt to determine the best dose regimen for clinical use. Hemopoietic depression was severe at each of the dose levels used when the drug was given daily intravenously. For comparable total dose per unit time, the hemopoietic depression was less severe when the drug was given once weekly intravenously. Gastrointestinal toxicity was usually mild with both intravenous and oral routes of administration.

Significant antitumor effects occurred with both oral and parenteral administration and were seen in seven out of 68 patients with measurable tumor masses; these included two cases of ovarian carcinoma and one each of lymphoma and of mammary, bronchiolar, uterine, and colon adenocarcinoma.