S-1 for the treatment of gastrointestinal cancer

Expert Opin Pharmacother. 2012 Sep;13(13):1943-59. doi: 10.1517/14656566.2012.709234. Epub 2012 Aug 4.


Introduction: 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.

Areas covered: 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.

Expert opinion: 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.

Publication types

  • Comparative Study
  • Review

MeSH terms

  • Animals
  • Antimetabolites, Antineoplastic / adverse effects
  • Antimetabolites, Antineoplastic / therapeutic use*
  • Antineoplastic Combined Chemotherapy Protocols / adverse effects
  • Antineoplastic Combined Chemotherapy Protocols / therapeutic use
  • Camptothecin / administration & dosage
  • Camptothecin / analogs & derivatives
  • Cisplatin / administration & dosage
  • Drug Combinations
  • Fluorouracil / therapeutic use
  • Gastrointestinal Neoplasms / drug therapy*
  • Gastrointestinal Neoplasms / pathology
  • Humans
  • Irinotecan
  • Organoplatinum Compounds / administration & dosage
  • Oxaliplatin
  • Oxonic Acid / adverse effects
  • Oxonic Acid / therapeutic use*
  • Practice Guidelines as Topic
  • Tegafur / adverse effects
  • Tegafur / therapeutic use*


  • Antimetabolites, Antineoplastic
  • Drug Combinations
  • Organoplatinum Compounds
  • Oxaliplatin
  • S 1 (combination)
  • Tegafur
  • Oxonic Acid
  • Irinotecan
  • Cisplatin
  • Fluorouracil
  • Camptothecin