Drug intelligence / Profile preview

epirubicin + cisplatin + S-1

Development stage
Unknown
Lead developer
Pfizer
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

Epirubicin + cisplatin + S-1 is a combination chemotherapy regimen used primarily in the treatment of advanced or metastatic gastric cancer. This regimen combines three agents with distinct mechanisms of action: - Epirubicin is an anthracycline antibiotic that intercalates DNA, inhibiting topoisomerase II and leading to DNA strand breaks and apoptosis. - Cisplatin is a platinum-based compound that forms DNA crosslinks, disrupting DNA replication and transcription, ultimately causing cell death. - S-1 is an oral fluoropyrimidine derivative composed of tegafur (a prodrug of 5-fluorouracil), gimeracil (an inhibitor of dihydropyrimidine dehydrogenase to increase 5-FU bioavailability), and oteracil (to reduce gastrointestinal toxicity). It inhibits thymidylate synthase, impairing DNA synthesis. This combination aims to maximize antitumor efficacy by targeting cancer cells through multiple cytotoxic pathways. The regimen has been investigated as a first-line therapy for advanced gastric cancer, offering the convenience of oral administration for the fluoropyrimidine component compared to traditional intravenous 5-FU regimens.

02

Targets

DNATOP2A (DNA topoisomerase II)TS (Thymidylate synthase)

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