Drug intelligence / Profile preview

2'-f-ara-deoxyuridine

Development stage
Phase 1
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules, Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, DNA Intercalators/Alkylators → Nucleic Acid-Directed Small Molecules → Small Molecules
01

Overview

2'-f-ara-deoxyuridine (FAU) is a synthetic nucleoside analog structurally related to deoxyuridine. It acts as a prodrug that is phosphorylated and methylated within cells, ultimately being incorporated into DNA as FMAUMP. This incorporation leads to inhibition of DNA synthesis and cell growth. The drug’s activation depends on the catalytic activity of thymidylate synthase (TS), making it particularly effective in tumors with high TS activity that are resistant to traditional TS inhibitors. FAU has been studied as an antitumor agent and suicide prodrug for targeting cancer cells by exploiting their elevated TS levels[1][3]. Its mechanism allows selective toxicity toward certain tumor types while potentially enabling noninvasive imaging of tumor TS activity using radiolabeled derivatives[3].

Other names
2'-deoxy-2'-fluoro-arabinofuranosyl uridineFMAUMP (active metabolite)fluoroarabinofuranosyl uridine
02

Targets

TS (Thymidylate synthase)

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