Drug intelligence / Profile preview

leucovorin + oxaliplatin + docetaxel + S-1

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

Overview

This is a four-drug combination chemotherapy regimen consisting of leucovorin, oxaliplatin, docetaxel, and S-1. It is being investigated as perioperative chemotherapy for resectable and high-risk gastric cancer. Each component has a distinct mechanism of action: - Leucovorin (folinic acid) enhances the cytotoxic effect of fluoropyrimidines like S-1 by stabilizing the binding of fluorouracil to thymidylate synthase. - Oxaliplatin is a platinum-based agent that induces DNA crosslinking, leading to inhibition of DNA replication and transcription. - Docetaxel is a taxane that promotes microtubule assembly while inhibiting disassembly, resulting in cell cycle arrest and apoptosis. - S-1 is an oral fluoropyrimidine derivative combining tegafur (a prodrug of 5-fluorouracil), gimeracil (a dihydropyrimidine dehydrogenase inhibitor), and oteracil (to reduce gastrointestinal toxicity). The combination aims to improve pathological tumor response rates, curative resection rates, protocol completion rates, tolerability, and overall survival compared to standard regimens such as FLOT or SOX. Early-phase clinical trials have shown promising efficacy with manageable toxicity profiles in patients with advanced or high-risk gastric cancer[5][1].

Brand names
TS-1TS1TS 1TaxotereEloxatin
Other names
LOTS
02

Targets

TS (Thymidylate synthase)TUBB (Tubulin (alpha and beta subunits))DNA

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