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Phase 1 Clinical Investigation of 4'-(9-Acridinylamino)methanesulfon-m-anisidide (NSC 249992), a New Acridine Derivative¹

Department of Developmental Therapeutics, The University of Texas System Cancer Center, M. D. Anderson Hospital and Tumor Institute, Houston, Texas 77030

The compound 4'-(9-acridinylamino)methanesulfon-m-anisidide is a new acridine derivative that was evaluated in a Phase 1 clinical trial. The schedule of drug administration consisted of daily i.v. injection for 3 consecutive days, repeated at 3-week intervals. Twenty-six patients received a total of 63 courses of 4'-(9-acridinylamino)methanesulfon-m-anisidide in a dose range from 4 to 50 mg/sq m/day. Hematopoietic toxicity was dose limiting, but it was of short duration and rapidly reversible. Mild nausea and vomiting were observed in 16% of the courses, and a mild degree of phlebitis was observed in 10% of the courses. Responses were observed in two patients with adenocarcinoma of the lung and one each of melanoma and acute myeloblastic leukemia. Phase 2 studies of 4'-(9-acridinylamino)methanesulfon-m-anisidide are planned at a starting dose of 40 mg/sq m/day for 3 days in good-risk patients and at 25 to 30 mg/sq m/day for 3 days in poor-risk patients. Course of treatment would be repeated at 21-day intervals.

¹ Supported in part by Contract NO1-CM-43801 from the National Cancer Institute, NIH, USPHS, Bethesda, Md. 20014.

² To whom requests for reprints should be addressed.

Received 6/14/78. Accepted 8/ 7/78.