Drug intelligence / Profile preview

capecitabine + oxaliplatin + S-1

Development stage
Preclinical
Lead developer
Taiho Pharmaceutical
Modality
DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral, Intravenous
01

Overview

**Capecitabine** + oxaliplatin + S-1 is a combination chemotherapy regimen that includes three agents:\n- **Capecitabine** is an oral prodrug of 5-fluorouracil (5-FU), which inhibits thymidylate synthase, disrupting DNA synthesis in rapidly dividing cancer cells.\n- **Oxaliplatin** is a platinum-based chemotherapeutic that forms DNA crosslinks, inhibiting DNA replication and transcription.\n- **S-1** is an oral fluoropyrimidine derivative composed of tegafur (a prodrug of 5-FU), gimeracil (an inhibitor of dihydropyrimidine dehydrogenase to increase 5-FU bioavailability), and potassium oteracil (to reduce gastrointestinal toxicity).\nThis triple combination has been investigated for the treatment of advanced or metastatic gastric cancer and colorectal cancer. While both capecitabine plus oxaliplatin (CAPOX/XELOX) and S-1 plus oxaliplatin (SOX) are established regimens for these indications, the use of all three together as a single regimen is not standard but may be explored in clinical research settings. The mechanism involves inhibition of DNA synthesis and function through multiple pathways, enhancing antitumor efficacy.

02

Targets

DNATS (Thymidylate synthase)

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