Phase 1 clinical investigation of 4'- (9-acridinylamino) methanesulfon-m-anisidide (NSC 249992) , a new acridine derivative
Legha, S.S.; Gutterman, J.U.; Hall, S.W.; Benjamin, R.S.; Burgess, M.A.; Valdivieso, M.; Bodey, G.P.
Cancer Research 38(11 Part 1): 3712-3716
1978
ISSN/ISBN: 0008-5472 PMID: 279397 Document Number: 136032
The compound 4'-(9-acridinylamino)methanesulfon-m-anisidide is a new 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.