gemcitabine monophosphate ProTide

NUC-1031 (Acelarin) is a phosphoramidate ProTide and a prodrug of the anticancer nucleoside analog gemcitabine. It is designed to overcome key resistance mechanisms associated with standard gemcitabine therapy by bypassing the need for nucleoside transporters (such as hENT1) and the rate-limiting activating enzyme deoxycytidine kinase (dCK). Once inside cancer cells, its protective phosphoramidate group is cleaved to release pre-activated gemcitabine monophosphate (dFdCMP), which is then rapidly converted into its active cytotoxic metabolite dFdCTP. dFdCTP incorporates into DNA, stalling the cell cycle and causing DNA damage. Additionally, NUC-1031 may bind to ribonucleotide reductase regulatory subunit M1, perturbing nucleotide pools. The drug has shown promise in clinical trials for advanced biliary tract cancer and ovarian cancer[1][2][3][5][6].

Brand names

Acelarin

Other names

NUC-1031NUC1031NUC 1031gemcitabine monophosphate ProTide