Drug intelligence / Profile preview

leucovorin + oxaliplatin + tegafur

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

Overview

This is a combination chemotherapy regimen consisting of three agents: - **Leucovorin** (folinic acid), a reduced folate that enhances the cytotoxic effects of fluoropyrimidines and rescues normal cells from folate antagonist toxicity. - **Oxaliplatin**, a platinum-based chemotherapeutic that forms DNA crosslinks, inhibiting DNA replication and transcription, leading to cell death. - **Tegafur**, an oral prodrug of 5-fluorouracil (5-FU), which is converted in the body to 5-FU, an antimetabolite that inhibits thymidylate synthase and disrupts DNA synthesis. This combination is used primarily for the treatment of advanced or recurrent colorectal cancer. Leucovorin potentiates the effect of 5-FU derived from tegafur, while oxaliplatin adds synergistic cytotoxicity through its distinct mechanism. Tegafur provides continuous exposure to 5-FU with improved tolerability compared to intravenous administration[1][2][3].

02

Targets

DNATS (Thymidylate synthase)

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