Tezacitabine

DB06433InvestigationalSmall molecule

A synthetic purine nucleoside analogue with potential antineoplastic activity.

Mechanism: Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. Tezacitabine diphosphate binds to and irreversibly inhibits the activity of the enzyme ribonucleotide reductase (RNR), which may result in the inhibition of DNA synthesis in tumor cells and tumor cell apoptosis. Tezacitabine triphosphate acts as a substrate for DNA polymerase, further compromising DNA replication. This agent is relatively resistant to metabolic deactivation by cytidine deaminase. RNR catalyzes the conversion of ribonucleoside 5'-diphosphates to deoxyribonucleoside 5'-diphosphates necessary for DNA synthesis and is overexpressed in many tumor types.
Curator reviewed
Primary indication: Investigated for use/treatment in colorectal cancer, lung cancer, leukemia (unspecified), and gastric cancer.Curator reviewed
Formula / weight: C₁₀H₁₂FN₃O₄ · 257.2184 g/mol (avg)
Code names: KW-2331 · MDL 101,731

Resolves to

Compound

Structure

InChIKeyGFFXZLZWLOBBLO-ASKVSEFXSA-NSMILESNC1=NC(=O)N(C=C1)[C@@H]1O[C@H](CO)[C@@H](O)\C1=C/F

Targets

What you can answer from here — as of August 29, 2026

2Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

39Drug interactionsStructured to mechanism, not free text

3Clinical trialsPhase, status and sponsor resolved per trial

3+ReferencesStructured and connected to the statements they support

Which drugs share a target with Tezacitabine, and which of those have an active Phase 3 trial?

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