Phase I Clinical and Pharmacokinetic Study of 4’-(9-Acridinylamino)-methanesulfon-m-anisidide in Children with Cancer

Gaston Rivera, William E. Evans, Gary V. Dahl, Gary C. Yee, Charles B. Pratt

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Forty-one pediatric patients with advanced cancer (24 with acute leukemia and 17 with diverse solid tumors) received 74 courses of therapy with a new chemotherapeutic agent, 4’-(9-acridinylamino)methanesulfon-m-anisidide (AMSA; NSC 249992). Treatments were given by slow i.v. injection daily for five days every two to three weeks. In patients with leukemia: (A) dosages were escalated from 1.3 to 150 mg/sq m/day; (b) toxicity in the form of stomatitis, vomiting, and phlebitis occurred at dosage levels of 125 to 150 mg/sq m/day; and (c) oncolytic effects were observed in 13 of 24 patients. In patients with solid tumors: (A) dosages were escalated from 5 to 50 mg/sq m/day; (b) toxicity (stomatitis, myelosuppression, and phlebitis) occurred at the dosage level of 50 mg/sq m/day; and (c) no oncolytic responses were noted. Serum concentrations of total and free AMSA were assayed by a fluorescence technique and declined in a biphasic manner with free AMSA declining more rapidly than total AMSA. Dosages of >100 mg/sq m/day were required to maintain serum concentrations of total and free AMSA >0.2/im for the entire five-day schedule. The results suggest that maximum tolerated dosages of AMSA may differ in children with leukemia and solid tumors; however, hematopoietic toxicity could not be fully evaluated in the patients with leukemia. AMSA has clear antileukemic activity that warrants future Phase II trials.

Original languageEnglish (US)
Pages (from-to)4250-4253
Number of pages4
JournalCancer Research
Issue number11
StatePublished - Nov 1 1980


ASJC Scopus subject areas

  • Oncology
  • Cancer Research

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