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Roche Holding AG

Drug Names(s): capecitabine, R340, RG340, Ro09-1978

Description: XELODA is a fluoropyrimidine carbamate with antineoplastic activity. XELODA is enzymatically converted to 5-fluorouracil (5-FU) in vivo. Capecitabine is readily absorbed from the gastrointestinal tract.

5-Fluorouracil exerts its cytotoxicity mainly following its conversion, by a two-step route, to 5-fluoro-uridine monophosphate (5-FUMP). 5-FUMP is further transformed to 5-FdUMP, an irreversible inhibitor of thymidylate synthase. This binding inhibits the formation of thymidylate from 2’-deoxyuridylate. Thymidylate is the necessary precursor of thymidine triphosphate, which is essential for the synthesis of DNA, so that a deficiency of this compound can inhibit cell division. Second, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate (UTP) during the synthesis of RNA. This metabolic error can interfere with RNA processing and protein synthesis.

Partners: Chugai Pharmaceutical Co., Ltd.

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