STUDIES ON ANTITUMOR DRUGS Ⅶ.THERAPEUTIC EFFECT OF p-BIS(2-CHLOROETHYL)AMINO-β-PHENYLALANINE ON ANIMAL TUMORS AND ITS TOXICITY

p-bis(2-chloroethyl)amino-β-phenylalanine(Ho-14) at the daily dosage of 10 mg/kg produced marked inhibitory action on spindle cell sarcoma, AK sarcoma,lymphatic leukemia,Ehrlich ascites carcinoma,mammary carcinoma in mice, and Walker carcinoma and Jensen sarcoma in rats. The acute and subacute LD₅₀(7 injections)levels after intraperitoneal injections of Ho-14 in mice were found to be 50.5 and 22.6 mg/kg respectively. Ho-14 was injected intravenously in rabbits for 15 days.At the dosage of 1 mg/kg it had no significant influence on the blood cell counts,hemoglobin content and urinalysis.When the dosage was raised to 5 mg/kg,the white cell counts decreased significantly and gradually re- covered 3 wceks after cessation of the drug.Under the influence of 10 mg/kg the leukocyte counts were also decreased and most of the rabbits died after 6—9 injections. Ho-14 was administered intragastrically at the dosages of 5 and 10 mg/kg every four days and the total doses attained 450 and 1260 mg,no remarkable change in the blood picture,EKG, blood pressure,urine and feces examinations was observed.