Capecitabine

Capecitabine is a prodrug of antitumor antimetabolite, metabolized to the active form 5-fluorouracil (5-FU) [F0151] by three enzymes located in the liver and in tumors. The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites, 5'-deoxy-5-fluorocytidine [D4342] and 5'-deoxy-5-fluorouridine (doxifluridine) [D3579], to form 5-FU. Capecitabine and its intermediary metabolites are not cytotoxic by themselves. The final step (doxifluridine to 5-FU) requires thymidine phosphorylase (dThdPase) that is significantly more active in tumor than normal tissue. This tumor-selective delivery of 5-FU ensured greater efficacy and a more favorable safety profile than with other fluoropyrimidines. For your reference, [D5787] is a synthetic precursor of capecitabine. (The product is for research purpose only.)