Tezacitabine
Tezacitabine Uses, Dosage, Side Effects, Food Interaction and all others data.
A synthetic purine nucleoside analogue with potential antineoplastic activity.
Trade Name | Tezacitabine |
Generic | Tezacitabine |
Tezacitabine Other Names | Tezacitabine |
Type | |
Formula | C10H12FN3O4 |
Weight | Average: 257.2184 Monoisotopic: 257.081184092 |
Groups | Investigational |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Investigated for use/treatment in colorectal cancer, lung cancer, leukemia (unspecified), and gastric cancer.
How Tezacitabine works
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.
Innovators Monograph
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