Drug intelligence / Profile preview

tegafur + uracil + mitomycin + tamoxifen

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

Overview

This is a combination regimen consisting of tegafur, uracil, mitomycin, and tamoxifen used primarily as postoperative adjuvant chemoendocrine therapy for breast cancer. Tegafur is a prodrug of 5-fluorouracil (5-FU), an antimetabolite that inhibits DNA synthesis in rapidly dividing cells. Uracil acts as a competitive inhibitor of dihydropyrimidine dehydrogenase (DPD), thereby increasing the bioavailability and efficacy of 5-FU derived from tegafur. Mitomycin is an alkylating agent that crosslinks DNA, leading to inhibition of DNA synthesis and function. Tamoxifen is a selective estrogen receptor modulator (SERM) that competitively inhibits estrogen binding to its receptor, blocking the growth-promoting effects of estrogen on breast cancer cells. This combination has been studied in patients with stage II, estrogen receptor-positive primary breast cancer as postoperative adjuvant therapy. Clinical trials have shown improved relapse-free survival rates when UFT (tegafur/uracil) plus tamoxifen are combined with mitomycin compared to regimens without UFT[1][2][3]. The regimen leverages both cytotoxic chemotherapy and hormonal blockade for enhanced efficacy.

Other names
UFT + mitomycin + tamoxifen
02

Targets

DPYD (Dihydropyrimidine dehydrogenase)ER (Estrogen receptor)DNATS (Thymidylate synthase)

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