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paclitaxel + tegafur + gimeracil + oteracil
- Development stage
- Unknown
- Lead developer
- Taiho Pharmaceutical
- Modality
- Nucleic Acid-Directed Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules
- Administration
- Intravenous, Oral
01
Overview
This drug is a combination chemotherapy regimen consisting of paclitaxel (a microtubule inhibitor) and S-1, an oral fluoropyrimidine derivative composed of tegafur (a prodrug of 5-fluorouracil), gimeracil (an inhibitor of dihydropyrimidine dehydrogenase to prolong 5-FU activity), and oteracil (which reduces gastrointestinal toxicity by inhibiting phosphorylation of 5-FU in the gut)[9][3]. Paclitaxel disrupts cell division by stabilizing microtubules, leading to apoptosis. Tegafur is converted into active 5-fluorouracil in the body; gimeracil increases its bioavailability; oteracil limits GI side effects[3][9]. This combination has been studied for advanced gastric cancer, biliary tract carcinoma, and other solid tumors. Clinical studies have shown antitumor activity with manageable safety profiles[2][6].
- Brand names
- TaxolTeysunoTS-1TS1TS 1
- Other names
- paclitaxel + S-1nab-paclitaxel + S-1paclitaxel + tegafur/gimeracil/oteracil potassium
02
Targets
TUBB (Tubulin (alpha and beta subunits))OPRT (Orotidine 5'-phosphate decarboxylase)DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)
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