[A synthetic purine nucleoside analog with potential antineoplastic activity. Phosphorylated by cellular kinases, tezacitabine is converted into its active diphosphate and triphosphate metabolites. The diphosphate form binds to and irreversibly inhibits activity of ribonucleotide reductase (RNR), an enzyme overexpressed in many tumor types and is responsible for the conversion of ribonucleoside diphosphates to deoxyribonucleotides necessary for DNA synthesis. A shortage of deoxyribonuleotides inhibits DNA replication and induces apoptosis. The triphosphate form acts as a substrate for DNA polymerase, thereby further compromises DNA replication. In addition, tezacitabine is relatively resistant to metabolic deactivation by cytidine deaminase. ( NCI )]
UMLS (NCI) C0253087 - Nucleic Acid, Nucleoside, or Nucleotide
- Pharmacologic Substance