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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

Department of Medicine, Division of Oncology [D. D. V. H., E. P., C. A. C.] and School of Pharmacy [J. K.], University of Texas Health Science Center at San Antonio, and Audie Murphy VA Hospital, San Antonio, Texas 78284, and Medical Research Division, American Cyanamid Company, Lederle Laboratories, Pearl River, New York 10965 [E. M.]

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 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.

¹ To whom requests for reprints should be addressed, at Department of Medicine, Division of Oncology, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, Texas 78284.

Received 12/ 7/79. Accepted 2/ 1/80.

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