LOW-MOLECULAR WEIGHT IMMUNOSTIMULANT WITH POTENT ANTITUMOUR PROPERTIES

N-(2-cyanoethylenc)urea (BA 1) is a drug of low molecular weight which has outstanding immunostimulant properties in animals with antitumour activity superior to that of ifosfamide.

Intravenous administration to 214 rats with DS carcinosarcoma of BA 1 in doses of 150mg/kg (12% of the LDso ), resulted in a lethality of only 1.7% and a recovery rate of 40% after 20 days of treatment. In animals with induced hyperglycaemia the recovery rate rose to 80%. Under identical conditions, 150mg/kg (47% of th~ LD50 , the most effective dose) of ifosfamide produced a recovery rate of 25% and a lethality of 18%. In contrast to BA 1, ifosfamide, which is a derivative of cyclophosphamide shown to have the greatest potency against DS carcinosarcoma in rats, showed no increase in activity in hyperglycaemic rats.

Leucocyte counts during treatment with the 2 drugs showed a pronounced stimulation with BA I, and the known suppression in the post-therapeutic interval with ifosfamide as is normally found with standard antitumour agents. Similar studies in tumour-free rats after intravenous injection of BA I showed that the immunostimulant action occurred within the first few days, and suggested that the drug may have novel prophylactic potential.

Von Ardenne, M. and Reitnauer, P.G.: Arzneimittel-Forschung 25: 1369 (Sep 1975)