S-1 is a novel oral fluoropyrimidine derivative, widely used for treating gastric, pancreatic, lung, head, neck and breast carcinomas. It is designed to enhance the clinical utility of an oral fluoropyrimidine and is associated with low gastrointestinal toxicity. S-1 consists of three pharmacological agents (at a molar ratio of 1:0.4:1)-Tegafur (FT), a prodrug of 5-Fluorouracil (5-FU), 5-Chloro-2-4-Dihydroxypyridine (CDHP), which inhibits the activity of Dihydropyrimidine Dehydrogenase (DPD) and Oxonic Acid (Oxo), which reduces Gastrointestinal (GI) toxicity of 5-FU. The present article reviews the current development of clinical study of S-1. It is widely used for treating gastric, pancreatic, lung, head, neck, and breast carcinomas. FT is a prodrug that is converted by liver Cytochrome P4502A6 (CYP2A6) to 5-FU. 5-FU is then actively catabolized by liver into inactive metabolites. About 90% of FU is converted to inactive metabolites by enzyme DPD. Hence, remaining 10% would be responsible for anti-tumour activity. It owes its anti-tumour properties to the production of 5-FU, which is gradually converted from FT, following oral administration of S-1. Both CDHP and potassium Oxo act as bio-modulators to impart better anti-cancer effect of 5-FU and do not have any anti-tumour activity by themselves. CDHP inhibits DPD enzyme, that is responsible for inactivation of 5-FU and is 180 times more active than uracil in-vitro. Potassium Oxo, which is Orotate
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