fosifloxuridine nafalbenamide

Fosifloxuridine nafalbenamide is a phosphoramidate-based small molecule prodrug of the monophosphate form of 5-fluoro-2'-deoxyuridine (FUdR), which is the active metabolite of fluorouracil (5-FU), an antimetabolite fluoropyrimidine analog. Upon administration, it is taken up by tumor cells where its phosphoramidate moiety is removed, converting it to its active form FUDR-MP. This active metabolite inhibits thymidylate synthase, leading to depletion of thymidine triphosphate and inhibition of DNA synthesis. Compared to 5-FU, this drug accumulates more efficiently in cancer cells due to increased lipophilicity and does not require nucleoside transporters or further phosphorylation for activation. It also avoids deactivation by dihydropyrimidine dehydrogenase and thymidine phosphorylase, resulting in a longer half-life and reduced toxicity. Fosifloxuridine nafalbenamide is being developed primarily as an anticancer agent for solid tumors including colorectal cancer, triple-negative breast cancer, and gastric cancer[1][2][3][4][5][7].

Other names

FUdR-MP prodrug5-fluoro-2'-deoxyuridine monophosphate prodrug