INITIAL CLINICAL-STUDY WITH PYRAZOFURIN

  • 1 January 1977
    • journal article
    • research article
    • Vol. 61  (3) , 389-394
Abstract
Patients (25) with inoperable carcinoma and lymphoma were given pyrazofurin (PF) by i.v. bolus at a dose level ranging from 100-300 mg/m2 of estimated body surface area. Five patients with acute leukemia were given PF by infusion at doses ranging from 250 mg/m2 per 24 h to 1500 mg/m2 per 144 h. PF was well tolerated by most patients at doses of 100 mg/m2 given as an i.v. bolus weekly or 250 mg/m2 given every 2-3 wk. An infusion of 750 mg/m2 given over a period of 72-120 h to leukemic patients resulted in severe but reversible toxicity; 1500 mg/m2 of PF given over a 144 h period to 1 patient resulted in the development of severe mucocutaneous toxicity and leukopenia. The patient died of hemorrhagic pneumonitis. The major toxic effects observed were mucosal (oral pain, cheilosis, redness and oral and lip ulcers), cutaneous (erythema, erosion and bullae) and hematologic (anemia, leukopenia and thrombocytopenia). The mucosal manifestations appear to be the dose limiting toxic factors in most patients. Toxic reactions were more pronounced in patients who previously received radiotherapy. Dose limiting hematologic toxic reactions occurred in 4. After treatment with PF, 1 of the 4 patients with breast carcinoma had a partial response (> 50% regression) lasting 5 wk. Another patient with breast carcinoma improved for .apprx. 1 mo.