Drug intelligence / Profile preview

gemcitabine + tegafur + uracil

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

Overview

Gemcitabine + tegafur + uracil is a combination chemotherapy regimen used primarily in the treatment of advanced cancers such as non-small cell lung cancer (NSCLC) and pancreatic cancer. Gemcitabine is a nucleoside analog that inhibits DNA synthesis by incorporating into DNA and causing chain termination, leading to apoptosis of rapidly dividing tumor cells. Tegafur is a prodrug that is metabolized to 5-fluorouracil (5-FU), which acts as an antimetabolite inhibiting thymidylate synthase and interfering with both DNA synthesis and RNA function. Uracil enhances the efficacy of tegafur by inhibiting dihydropyrimidine dehydrogenase, thereby increasing systemic exposure to 5-FU. This combination has demonstrated activity in patients who have failed previous platinum-based chemotherapy regimens for NSCLC and has also been studied in advanced pancreatic carcinoma[1][3][6][8].

Brand names
Uftoral
Other names
gemcitabine plus UFURgemcitabine plus UFTgemcitabine combined with uracil-tegafur
02

Targets

DNATS (Thymidylate synthase)DPYD (Dihydropyrimidine dehydrogenase)

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