Drug intelligence / Profile preview

difluorodeoxyuridine

Development stage
Unknown
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules
Administration
Intravenous, Intra-arterial, Oral
01

Overview

Difluorodeoxyuridine (dFdU) is a nucleoside analog and the primary metabolite of the chemotherapeutic drug gemcitabine. It is transported into cells, where it is subsequently phosphorylated to its mono-, di-, and triphosphate forms. The triphosphate form, dFdUTP, is incorporated into DNA and RNA, leading to the inhibition of DNA synthesis, cell cycle arrest in the early S phase, and the induction of apoptosis in cancer cells. dFdU also exhibits a concentration- and schedule-dependent radiosensitizing effect in vitro and possesses anticancer and antitumor activities. While it is a biologically active compound with cytotoxic effects, it is primarily studied for research purposes and as a metabolite, rather than being marketed as a standalone therapeutic drug.

02

Targets

DNA polymerase familyDCK (Deoxycytidine kinase)SLC28A1 (Sodium/nucleoside cotransporter 1)RNAP (Bacterial dna-dependent RNA polymerase)DNA

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