tezacitabine

Tezacitabine is a synthetic nucleoside analogue structurally related to cytidine. It acts as an antimetabolite with potential antineoplastic activity. After phosphorylation by cellular kinases to its active diphosphate and triphosphate forms, tezacitabine exerts its effects through two main mechanisms: - The diphosphate form irreversibly inhibits ribonucleotide reductase (RNR), an enzyme essential for DNA synthesis in proliferating cells. - The triphosphate form serves as a substrate for DNA polymerase and disrupts DNA replication. Tezacitabine is relatively resistant to deactivation by cytidine deaminase. It has been investigated primarily for the treatment of various solid tumors including colorectal cancer, gastric cancer (including adenocarcinoma), esophageal carcinoma, non-small cell lung cancer, hematologic neoplasms and other advanced solid tumors[1][2][5][6][8]. Clinical studies have shown manageable toxicity profiles dominated by neutropenia.

Other names

2'-Deoxy-2'-(fluoromethylene)cytidine(E)-2'-deoxy-2'-(fluoromethylene)cytidineFmdc cpd