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TS-1 + leucovorin + gemcitabine is a combination chemotherapy regimen used primarily in the treatment of advanced gastrointestinal cancers, such as pancreatic and colorectal cancer. TS-1 (also known as S-1) is an oral fluoropyrimidine anticancer drug composed of three components: tegafur (a prodrug of 5-fluorouracil), gimeracil (an inhibitor of dihydropyrimidine dehydrogenase to sustain 5-FU levels), and oteracil potassium (which reduces gastrointestinal toxicity)[2][4][7]. Leucovorin enhances the binding of 5-fluorouracil to thymidylate synthase, thereby increasing its antitumor activity[6]. Gemcitabine is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA strands during replication, leading to cell death. The combination leverages multiple mechanisms targeting DNA synthesis and repair pathways for synergistic cytotoxic effects against tumor cells.
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