S-1 for the treatment of gastrointestinal cancer

5-Fluorouracil (5-FU)-based regimens are used worldwide as the standard treatment in chemotherapy for gastric cancer. S-1 , a fourth-generation oral fluoropyrimidine that combines tegafur and two biochemical modulators: gimeracil and oteracil potassium, is now attracting considerable interest.

This review addresses the clinical evidence of S-1 in gastrointestinal malignancies, such as gastric, colorectal, pancreatic and biliary tract cancers. S-1 has demonstrated advantages over standard therapies, in both advanced and postoperative settings, in large Phase III studies. S-1 alone or S-1 plus cisplatin is recommended in the 2010 Gastric Cancer Treatment Guidelines, by the Japanese Gastric Cancer Association. Results from Phase III studies have demonstrated that S-1 in combination with chemotherapies, such as cisplatin in gastric cancer, and irinotecan and oxaliplatin in colorectal cancers, is non-inferior to conventional 5-FU-based standard regimens, with the benefit of convenience and reduced toxicity.

The excellent design of S-1 aimed to reduce toxicity by avoiding certain routes of degradation, and to enhance activity by reducing catabolism. This has provided not only a suitable alternative to 5-FU, but also higher efficacy.