Drug intelligence / Profile preview

tamoxifen + tegafur-uracil

Development stage
Unknown
Lead developer
Taiho Pharmaceutical
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Oral
01

Overview

Tamoxifen + tegafur-uracil is an oral combination therapy used primarily in the treatment of estrogen receptor (ER)-positive early and advanced breast cancer. Tamoxifen is a selective estrogen receptor modulator (SERM) that acts as an antagonist of the estrogen receptor in breast tissue, thereby inhibiting tumor growth driven by estrogen signaling. Tegafur-uracil (UFT) is a fixed-dose combination of tegafur, a prodrug of 5-fluorouracil (5-FU), and uracil, which inhibits dihydropyrimidine dehydrogenase to increase 5-FU bioavailability. This combination provides cytotoxic antitumor activity by interfering with DNA synthesis in rapidly dividing cells. The regimen has demonstrated non-inferiority to standard cyclophosphamide-methotrexate-fluorouracil regimens for ER-positive node-positive early breast cancer and offers improved tolerability with fewer hematologic and gastrointestinal side effects compared to traditional chemotherapy[1][4]. It is widely used as adjuvant therapy in Japan.

Brand names
UftoralOrzel
Other names
tamoxifen + UFTtamoxifen + uracil-tegafur
02

Targets

ER (Estrogen receptor)TS (Thymidylate synthase)

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