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Capecitabine


Mechanism of action:

Capecitabine is a fluoropyrimidine carbamate prodrug that is converted in the body into the active metabolite 5-fluorouracil (5-FU). Because thymidine phosphorylase levels are often higher in tumor tissue than in normal tissue, the proportion of 5-FU generated within tumor tissue can be relatively increased. Subsequently, 5-FU is further converted into other active metabolites, such as FdUMP (5-fluoro-2'-deoxyuridine monophosphate), which inhibits thymidylate synthase and blocks dTMP synthesis; FUTP (5-fluorouridine triphosphate), which is incorporated into RNA and interferes with RNA function and protein synthesis; and FdUTP, which is incorporated into DNA, causing DNA abnormalities, blocking cancer cell division, and activating cell death-related pathways.

Reference(s):

1. Walko CM et al. (2005). Capecitabine: a review. Clin Ther. 


2. Wagstaff AJ et al. (2003). Capecitabine: a review of its pharmacology and therapeutic efficacy in the management of advanced breast cancer. Drugs. 


3. Koukourakis GV et al. (2008). Efficacy of the oral fluorouracil pro-drug capecitabine in cancer treatment: a review. Molecules.

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