PHASE-I CLINICAL-STUDY WITH 5'-DEOXY-5-FLUOROURIDINE, A NEW FLUOROPYRIMIDINE DERIVATIVE

  • 1 January 1982
    • journal article
    • research article
    • Vol. 66  (6) , 1307-1313
Abstract
5''-Deoxy-5-fluorouridine (DFUR) is a new fluoropyrimidine derivative with significant antineoplastic activity in animal systems. Compared to 5-FU [5-fluorouracil] or other fluoropyrimidines, DFUR has a more favorable therapeutic ratio in Sarcoma 180-bearing mice. DFUR was studied in this phase I trial with a daily .times. 5 bolus i.v. injection. A 2nd course was given .gtoreq. 3 wk after the 1st day of treatment. Doses were escalated from 300-5000 mg/m2/day in 30 patients. Dose-limiting factors were myelosuppression and stomatitis. Hematologic toxic effects were particularly marked on granulocytes. Thrombocytopenia was less frequently encountered. Stomatitis was severe at high doses of DFUR. Eleven patients had nausea or moderate vomiting. Drug-induced myocardial injury may exist, since ECG changes were recorded in 2 patients. After rapid i.v. injection, 4 patients felt hot in the face and pelvis. Other side effects were minimal. With this daily .times. 5 schedule of administration, the maximum tolerated dose of DFUR appeared to be 5000 mg/m2 per day. The dose recommended for further clinical use is 4000 mg/m2 per day .times. 5 for patients previously untreated with chemotherapy.

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