How does NUC-1031 overcome the limitations of gemcitabine in cancer treatment?

Label:chem

Topic
Gemcitabine is a widely used chemotherapy agent but is associated with resistance and metabolic breakdown, limiting its efficacy. NUC-1031 is designed to address these limitations by being a pre-activated form of gemcitabine, protected by a phosphoramidate moiety.
Answer
NUC-1031 overcomes the limitations of gemcitabine by entering cancer cells independently of nucleoside transporters (hENT1 and hCNT1) and does not require activation by deoxycytidine kinase (dCK). Additionally, NUC-1031 is not subject to breakdown by cytidine deaminase (CDA), allowing it to produce higher concentrations of the active metabolite dFdCTP inside tumor cells. This results in prolonged DNA incorporation and sustained DNA damage, enhancing its anticancer activity.
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