Drug intelligence / Profile preview

fluorouracil + leucovorin

Development stage
Phase 4
Lead developer
Pfizer
Modality
Small Molecules
Administration
Intravenous, Topical, Oral
01

Overview

Fluorouracil + leucovorin is a combination chemotherapy regimen primarily used in the treatment of colorectal cancer and other gastrointestinal malignancies. Fluorouracil (5-FU) is an antimetabolite that inhibits thymidylate synthase, thereby disrupting DNA synthesis and leading to cell death. Leucovorin (folinic acid) is a reduced form of folic acid that enhances the binding of 5-FU’s active metabolite (5-FdUMP) to thymidylate synthase, increasing the cytotoxic effect on cancer cells. This combination allows for greater efficacy than fluorouracil alone[1][2][3][4][6]. The regimen is widely used as first-line therapy for advanced or metastatic colorectal cancer.

Brand names
FU-LV
Other names
5-fluorouracil5-FUfolinic acidcalcium folinatecitrovorum factor
02

Targets

TS (Thymidylate synthase)DHFR (Dihydrofolate reductase)

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