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Capecitabine is a white to off-white crystalline powder, chemically described as 5'-deoxy-5-fluoro-N-[(pentyloxy)carbonyl]-cytidine, with a molecular formula of C₁₅H₂₂FN₃O₆ and a molecular weight of 359.35 g/mol[1][3][7]. It is a carbamate ester of cytidine and functions as a prodrug designed to be non-cytotoxic until it is metabolized in vivo[2][6][9]. Upon oral administration, capecitabine is absorbed and converted in the liver and tissues, particularly tumors, first by carboxylesterase to 5'-deoxy-5-fluorocytidine (5'-DFCR), then by cytidine deaminase to 5'-deoxy-5-fluorouridine (5'-DFUR), and finally by thymidine phosphorylase (preferentially in tumor tissue) to the active metabolite 5-fluorouracil (5-FU)[2][4][9][10]. 5-FU then exerts antitumor effects by inhibiting thymidylate synthase, thereby blocking DNA synthesis, as well as interfering with RNA and protein synthesis, leading to cell death[2][4][9]. Capecitabine is approved for the treatment of several cancers, including colorectal, breast, and gastric cancer, but it is not itself a molecular target—it is a chemotherapeutic agent designed to selectively deliver cytotoxic activity to tumor cells via enzymatic conversion[4][6][9].
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