roducitabine

Roducitabine (also known as RX-3117 and fluorocyclopentenylcytosine) is an orally available small molecule cytidine analog with antimetabolite and antitumor activity. It is designed to overcome resistance to gemcitabine and other nucleoside analogs. Roducitabine acts as a prodrug that is taken up by cells via carrier-mediated transporters and phosphorylated by uridine-cytidine kinase 2 (UCK2), leading to its activation. The active triphosphate form can be incorporated into RNA, inhibiting RNA synthesis, while the diphosphate form can be reduced and incorporated into DNA, inhibiting DNA synthesis. Additionally, it inhibits DNA methyltransferase 1 (DNMT1), resulting in hypomethylation of DNA, cell cycle arrest, and induction of apoptosis in tumor cells. Roducitabine has demonstrated broad-spectrum anticancer activity in preclinical models—including efficacy against gemcitabine-resistant tumors—and is being investigated for use in pancreatic cancer, bladder cancer, and solid tumors[1][4][5][7].

Other names

roducitabinefluorocyclopentenylcytosine