Acelarin (NUC-1031)

Acelarin, also known as NUC-1031, CPF-31; and GTPL7389, is a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine. Upon intravenous administration and cellular uptake, NUC-1031 is converted into the active metabolites difluorodeoxycytidine di- and triphosphate (dFdCDP, dFdCTP). dFdCDP inhibits ribonucleotide reductase, thereby decreasing the deoxynucleotide pool available for DNA replication; dFdCTP is incorporated into DNA, resulting in premature termination of DNA replication and eventually induction of apoptosis.