Drug intelligence / Profile preview

cisplatin + oxaliplatin + tegafur

Development stage
Discontinued
Lead developer
Michigan State University
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Covalent Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Intravenous, Oral
01

Overview

This is a combination regimen consisting of three chemotherapeutic agents: - **Cisplatin** is a platinum-based compound that forms DNA crosslinks, leading to apoptosis in rapidly dividing cancer cells. - **Oxaliplatin** is another platinum-based agent, similar in mechanism to cisplatin but with a different toxicity profile and spectrum of activity. It also induces DNA crosslinking and inhibits DNA synthesis and transcription. - **Tegafur** is an oral prodrug of 5-fluorouracil (5-FU), which acts as an antimetabolite by inhibiting thymidylate synthase, thereby disrupting DNA synthesis in cancer cells. While combinations such as S-1 (tegafur/gimeracil/oteracil) plus either cisplatin or oxaliplatin are established regimens for advanced gastric cancer, there is no evidence from the provided sources or standard clinical practice supporting the use of all three agents—cisplatin, oxaliplatin, and tegafur—together in a single regimen. Typically, either cisplatin or oxaliplatin would be combined with tegafur-containing regimens for gastric or colorectal cancers[1][2][3][6][8][10]. The simultaneous use of both platinum agents with tegafur does not appear to be standard or supported by clinical trial data.

02

Targets

DNATS (Thymidylate synthase)

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