Phase I clinical investigation of 1,4-dihydroxy-5,8-bis (( (2-[(2-hydroxyethyl)amino]ethyl) amino))-9,10-anthracenedione dihydrochloride (NSC 301739), a new anthracenedione.
1,4-Dihydroxy-5,8-bis(( (2-[(2-hydroxyethyl)amino]ethyl)-amino))-9,10-anthracenedione dihydrochloride is a new anthracenedione derivative that was evaluated in a Phase I clinical trial. The schedule of administration consisted of a single i.v. injection, repeated at 4-week intervals. Twenty-five patients received a total of 41 courses of the drug in a dose range of 1.2 to 14 mg/sq m. Leukopenia and thrombocytopenia were dose limiting but were of short duration and rapidly reversible. Mild degrees of phlebitis were observed in 10% of courses, and a green discoloration of the urine was noted with doses of greater than or equal to 10 mg/sq m. One patient with adenocarcinoma of the lung experienced a partial response of his tumor secondary to the drug. Phase II studies of 1,4-dihydroxy-5,8-bis(( (2-[(2-hydroxyethyl)amino]ethyl)amino))-9,10-anthracenedione dihydrochloride are planned at a starting dose of 12 mg/sq m as a single dose repeated at 21- to 28-day intervals.
D000328:Adult; D000368:Aged; D000873:Anthracenes / Q000627:therapeutic use*; D000970:Antineoplastic Agents / Q000009:adverse effects; D004341:Drug Evaluation; D005260:Female; D006410:Hematopoiesis / Q000187:drug effects; D006801:Humans; D007364:Intercalating Agents / Q000627:therapeutic use*; D008297:Male; D008875:Middle Aged; D008942:Mitoxantrone
D000873:Anthracenes; D000970:Antineoplastic Agents; D007364:Intercalating Agents; D008942:Mitoxantrone