Drug intelligence / Profile preview

letrozole + tegafur + uracil

Development stage
Preclinical
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

This is a combination therapy consisting of letrozole, an aromatase inhibitor, and tegafur plus uracil (commonly known as UFT or UFUR), an oral fluoropyrimidine chemotherapy. Letrozole inhibits the enzyme aromatase, reducing estrogen synthesis and thereby suppressing the growth of hormone receptor-positive breast cancer cells. Tegafur is a prodrug that is converted in the liver to 5-fluorouracil (5-FU), which exerts cytotoxic effects by inhibiting thymidylate synthase and interfering with DNA synthesis in tumor cells. Uracil acts as a competitive inhibitor of dihydropyrimidine dehydrogenase (DPD), increasing systemic exposure to 5-FU by preventing its rapid degradation. The combination has been used in clinical practice for hormone receptor-positive breast cancer, particularly in Japan[3][4]. There are case reports and small studies supporting its use postoperatively for advanced breast carcinoma[3].

Other names
letrozole + UFTletrozole + UFUR
02

Targets

CYP19A1 (Aromatase)DPYD (Dihydropyrimidine dehydrogenase)TS (Thymidylate synthase)

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