Drug intelligence / Profile preview

UFT + cyclophosphamide + epirubicin + leucovorin

Development stage
Preclinical
Lead developer
Takeda
Modality
Small Molecules
Administration
Oral, Intravenous
01

Overview

This is a combination chemotherapy regimen consisting of UFT (tegafur/uracil), cyclophosphamide, epirubicin, and leucovorin. UFT is an oral formulation combining uracil (a competitive inhibitor of dihydropyrimidine dehydrogenase) and tegafur (a bioavailable 5-fluorouracil prodrug) in a 4:1 molar ratio. Tegafur is converted to the bioactive compound 5-FU by hepatic cytochrome P450 enzymes, while uracil competitively inhibits hepatic DPD, preventing immediate inactivation of 5-FU. Leucovorin (also known as folinic acid) is added to enhance the antitumor activity of 5-FU by increasing the available reduced folates, stabilizing the binding of FdUMP to thymidylate synthase, and ultimately inhibiting DNA synthesis. Cyclophosphamide is an alkylating agent, and epirubicin is an anthracycline antibiotic with antineoplastic properties.

02

Targets

TOP2A (DNA topoisomerase II)DNATS (Thymidylate synthase)

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