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TS-1

National Health Research Institutes, Taiwan · Phase 3 active Small molecule

TS-1 is an oral combination chemotherapy agent that inhibits thymidylate synthase and enhances fluorouracil activity against cancer cells.

TS-1 is an oral combination chemotherapy agent that inhibits thymidylate synthase and enhances fluorouracil activity against cancer cells. Used for Gastric cancer, Colorectal cancer, Non-small cell lung cancer.

At a glance

Generic nameTS-1
Also known asS-1, Tegafur-gimeracil-oteracil potassium
SponsorNational Health Research Institutes, Taiwan
Drug classAntimetabolite chemotherapy combination
TargetThymidylate synthase
ModalitySmall molecule
Therapeutic areaOncology
PhasePhase 3

Mechanism of action

TS-1 is a fixed-dose combination of tegafur (a prodrug of fluorouracil), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (a orotate phosphoribosyltransferase inhibitor). Gimeracil inhibits the degradation of fluorouracil, while oteracil reduces gastrointestinal toxicity by blocking its activation in the GI tract, allowing higher systemic exposure and improved efficacy.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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