In order to deliver a high concentration of anti-cancer drugs in tumor tissue, preoperative intra-arterial injection therapy using Etoposide (VP-16), Pirarubicin (THP-ADM) and Cisplatin (CDDP), was used for 22 patients with resectable advanced gastric cancer. The concentration of VP-16, Adriamycin (ADM) and platinum (Pt) were measured in cancer tissue, normal mucosa and lymphnodes without metastasis at the greater curvature, which were gathered operatively and in serum just before operation. Student's t test was performed with their data. The mean concentration of VP-16 was less than the detectable limit in all tissues and in serum. The mean concentration of ADM in cancer tissue was significantly higher than in normal gastric mucosa, in lymphnodes without metastasis, and in serum. The mean concentration of platinum in cancer tissue was higher than those in lymphnodes, normal mucosa, and serum, but no significant differences were noted among them. It was concluded that the intra-arterial injection of THP-ADM and CDDP was an effective method to maintain a high concentration of ADM and Pt in gastric cancer tissue. However, intra-arterial injection of VP-16 was not useful.