NCIt synonyms : 4-Amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-(hydroxymethyl)cyclopent-2-en-1-yl)pyrimidin-2(1H)-one; Fluorocyclopentenylcytosine; Cytidine Analog RX-3117;
NCIt definition : An orally available small molecule and nucleoside antimetabolite with potential antineoplastic
activity. Upon administration, roducitabine is taken up by cells through a carrier-mediated
transporter, phosphorylated by uridine cytidine kinase (UCK) and then further phosphorylated
to its diphosphate (RX-DP) and triphosphate forms (RX-TP). The triphosphate form is
incorporated into RNA and inhibits RNA synthesis. The diphosphate RX-DP is reduced
by ribonucleotide reductase (RR) to dRX-DP; its triphosphate form (dRX-TP) is incorporated
into DNA. In addition, roducitabine also inhibits DNA methyltransferase 1 (DNMT1).
This eventually leads to cell cycle arrest and the induction of apoptosis. UCK is
the rate-limiting enzyme in the pyrimidine-nucleotide salvage pathway.;