thiarabine

Thiarabine is a next-generation deoxycytidine nucleoside analog and structural analog of cytarabine, developed as an antimetabolite with potent anticancer activity. It acts as a prodrug that requires intracellular phosphorylation by deoxycytidine kinase to its active triphosphate form (T-araCTP), which competes with cytidine for incorporation into DNA. This results in inhibition of DNA replication and RNA synthesis, leading to chain termination and decreased tumor cell proliferation. Thiarabine has demonstrated superior antitumor activity compared to gemcitabine, clofarabine, or cytarabine in preclinical models, particularly against solid tumors such as lung and pancreatic cancers. It is orally bioavailable (approximately 16%) and effective with once-daily dosing—features that distinguish it from cytarabine. In clinical trials, thiarabine showed some activity in heavily pretreated patients with hematologic malignancies and solid tumors but was associated with excessive fatigue[1][2][3][5][8].

Other names

thio-cytarabine4'-thioaracytidine1-beta-D-[4-thio-arabinofuranosyl]-cytosine