Capecitabine CAS No. 154361-50-9

Classification: Antineoplastic,antimetabolite Action/Kinetics:An oral prodrug of 5'-deoxy-5-fluorouridine (5'DFUR) that is converted to5-fluorouracil (5-FU). 5-FU is metabolized to 5-fluoro-2-deoxyuridinemonophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) which cause cellinjury in two ways. First, FdUMP and the folate cofactor,N5-10-methylenetetrahydrofolate, bind to thymidylate synthase to form acovalently bound ternary complex which inhibits the formation of thymidylatefrom uracil. Thymidylate is essential for the synthesis of DNA so a deficiencyinhibits cell division. Secondly, nuclear transcriptional enzymes canmistakenly incorporate FUTP in place of uridine triphosphate during RNAsynthesis; this interferes with RNA processing and protein synthesis. Readilyabsorbed from the GI tract. Peak blood levels, capecitabine: 1.5 hr; peak bloodlevels, 5-FU: 2 hr. Food reduces the rate and extent of absorption. t1/2,capecitabine and 5-FU: 45 min. Metabolites excreted in the urine.

Application  

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Specification