Drug intelligence / Profile preview

L-leucovorin + Uftoral

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

Overview

L-leucovorin + Uftoral is a combination chemotherapy regimen used primarily for the treatment of colorectal cancer. The combination consists of L-leucovorin (the active enantiomer of leucovorin, also known as folinic acid) and Uftoral, a brand name for the oral fixed-dose combination of tegafur and uracil. Tegafur is a prodrug that is converted in the body to 5-fluorouracil (5-FU), an antimetabolite that inhibits DNA synthesis in rapidly dividing cells. Uracil acts by inhibiting dihydropyrimidine dehydrogenase, thereby increasing and prolonging 5-FU levels. L-leucovorin enhances the cytotoxic effect of 5-FU by stabilizing its binding to thymidylate synthase, further inhibiting DNA synthesis in tumor cells[2][4][6]. This regimen offers an oral alternative to intravenous 5-FU/leucovorin therapy.

Other names
tegafur + uracil + L-leucovorinUFT/LV
02

Targets

TS (Thymidylate synthase)DPYD (Dihydropyrimidine dehydrogenase)

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