S-1 + TAS-114

S-1 + TAS-114 is a combination therapy consisting of two oral small molecules used in oncology clinical trials. S-1 is an oral fluoropyrimidine derivative that combines tegafur (a prodrug of 5-fluorouracil), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (an orotate phosphoribosyltransferase inhibitor) to enhance the efficacy and reduce the gastrointestinal toxicity of 5-FU. TAS-114 is a first-in-class dual inhibitor targeting deoxyuridine triphosphatase (dUTPase) and dihydropyrimidine dehydrogenase (DPD). By inhibiting dUTPase, TAS-114 increases misincorporation of uracil and 5-FU into DNA, thereby enhancing the cytotoxic effect of fluoropyrimidines like those in S-1. The combination has been investigated primarily for advanced solid tumors including non-small cell lung cancer and gastric cancer after failure of standard therapies[2][3][6]. Clinical studies have shown modest antitumor activity with acceptable safety profiles but no significant improvement in progression-free survival compared to monotherapy[2][3].

Other names

TAS-114/S-1TAS-114 plus S-1TAS114 plus S-1TAS 114 plus S-1