Transcatheter arterial embolization was performed in a group of rabbits bearing VX2 tumor in the liver by injecting gelatin sponge (GS) with or without an anticancer agent (ACA) or Lipiodol with or without ACA. The antitumor effects as evaluated by tumor size and histological examination revealed that GS with or without ACA was most effective, followed in order by Lipiodol-ACA, aqueous solution of ACA and Lipiodol alone. On the other hand, severe normal tissue damage (necrosis of the liver and gallbladder) with elevation of plasma GOT, GPT, and LDH levels was more commonly observed in GS with or without ACA. Pharmacological analysis of plasma and tissue revealed that the antitumor effect of Lipiodol-ACA was due to prolonged release of ACA in addition to the embolization effect of Lipiodol, while the chemotherapeutic role of ACA was of little importance in GS-ACA.