Drug intelligence / Profile preview

etoposide + leucovorin + uracil-ftorafur

Development stage
Unknown
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

This is an oral combination chemotherapy regimen consisting of three agents: - **Etoposide** is a semisynthetic derivative of podophyllotoxin that inhibits DNA synthesis by forming a complex with topoisomerase II and DNA, leading to double-stranded DNA breaks and cell death. It acts primarily in the G2 and S phases of the cell cycle. - **Leucovorin** (folinic acid) is used to enhance the efficacy of fluoropyrimidines like 5-fluorouracil or its prodrugs by stabilizing their binding to thymidylate synthase. - **Uracil-ftorafur (UFT)** is an oral combination of tegafur (a prodrug of 5-fluorouracil) and uracil in a fixed molar ratio. Tegafur is converted into 5-FU in vivo; uracil competitively inhibits dihydropyrimidine dehydrogenase, increasing 5-FU bioavailability. This regimen has been studied as an all-oral treatment for metastatic breast cancer[1], advanced gastric cancer[2][5], and as second/third-line therapy for other solid tumors[3]. The combination aims to provide effective cytotoxic activity with manageable toxicity profiles.

Other names
etoposide + leucovorin + UFTetoposide + leucovorin + uracil-tegafurUFT/leucovorin/etoposide
02

Targets

TS (Thymidylate synthase)TOP2A (DNA topoisomerase II)

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