Drug intelligence / Profile preview

TS-1 + leucovorin + gemcitabine

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

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.

Other names
TS-1 plus leucovorin plus gemcitabineTS1 plus leucovorin plus gemcitabineTS 1 plus leucovorin plus gemcitabineS-1 plus leucovorin plus gemcitabineS1 plus leucovorin plus gemcitabineS 1 plus leucovorin plus gemcitabine
02

Targets

DNA polymerase familyDPYD (Dihydropyrimidine dehydrogenase)RNR (Ribonucleotide reductase)TS (Thymidylate synthase)

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