Drug intelligence / Profile preview

3-deazauridine

Development stage
Discontinued
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous
01

Overview

3-deazauridine is a synthetic uridine analog that acts as an antimetabolite and biochemical modulator. Upon intracellular uptake, it is phosphorylated by uridine-cytidine kinase (UCK) to its active triphosphate metabolite, 3-deazauridine triphosphate (deaza-UTP). This metabolite competitively inhibits cytidine triphosphate (CTP) synthase (CTPS), the rate-limiting enzyme in the de novo synthesis of CTP from UTP. By depleting intracellular CTP pools, 3-deazauridine disrupts DNA and RNA synthesis, induces S-phase cell cycle arrest, and triggers apoptosis. It has been investigated primarily as an antineoplastic agent for the treatment of acute leukemia and advanced solid tumors, often in combination with other cytidine analogs (such as cytarabine or decitabine) to enhance their incorporation into nucleic acids.

Other names
3-DUDAUdeazauridine
02

Targets

CTPS1 (Cytidine triphosphate synthase 1)

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