Drug intelligence / Profile preview

UFT + leucovorin

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Small Molecules
Administration
Oral
01

Overview

UFT + leucovorin is an oral combination chemotherapy regimen used primarily for the treatment of colorectal cancer. The combination consists of UFT (a fixed-ratio mixture of tegafur and uracil) and leucovorin (folinic acid). Tegafur is a prodrug that is metabolized to 5-fluorouracil (5-FU), a cytotoxic antimetabolite that inhibits thymidylate synthase, thereby disrupting DNA synthesis in rapidly dividing tumor cells. Uracil acts as a competitive inhibitor of dihydropyrimidine dehydrogenase, the enzyme responsible for 5-FU degradation, resulting in increased and prolonged plasma concentrations of 5-FU. Leucovorin enhances the binding affinity of 5-FU to thymidylate synthase, further potentiating its antitumor effect. This all-oral regimen offers advantages over intravenous bolus or infusional 5-FU regimens in terms of convenience and toxicity profile. It has been studied as adjuvant therapy for stage II/III colorectal cancer and also evaluated in other cancers such as breast, gastric, lung, head and neck cancers[1][2][3].

Brand names
Orzel
Other names
tegafur-uracil + leucovorinuracil-tegafur plus leucovorinUFT/LVUFT/LV regimen
02

Targets

TS (Thymidylate synthase)

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