Capecitabine

• Post Date:

  Aug 14,2015

• Expiry Date:

  Feb 10,2016

• Detailed Description:

  Cas No. :154361-50-9 Pharmaceutical Intermediates---Capecitabine:
  
  Capecitabine is an orally-administered chemotherapeutic agent used in the treatment of metastatic breast and colorectal cancers.Capecitabine is a prodrug,that is enzymatically converted to 5-fluorouracil in the tumor,where is inhibits DNA synthesis and slows growth of tumor tissue.The activation of capecitabine follows a pathway with three enzymatic steps and two intermediary metabolites.5'-deoxy-5-fluorocytidine(5'-DFCR)and 5'-deoxy-5-fluorouridine(5'-DFUR),to form 5-fluorouracil.
  Metastatic breast cancer in those resistant to both paclitaxel and an anthracycline-containing chemotherapy regimen or resistant to paclitaxel and for whom further anthracycline therapy is not indicated (e.g., those who have received cumulative doses of 400 mg/m2 of doxorubicin or doxorubicin equivalents).
  
  Capecitabine Pharmacological effects:
  Action/Kinetics: An oral prodrug of 5'-deoxy-5-fluorouridine (5'DFUR) that is converted to 5-fluorouracil (5-FU). 5-FU is metabolized to 5-fluoro-2-deoxyuridine monophosphate (FdUMP) and 5-fluorouridine triphosphate (FUTP) which cause cell injury in two ways. First, FdUMP and the folate cofactor, N5-10-methylenetetrahydrofolate, bind to thymidylate synthase to form a covalently bound ternary complex which inhibits the formation of thymidylate from uracil. Thymidylate is essential for the synthesis of DNA so a deficiency inhibits cell division. Secondly, nuclear transcriptional enzymes can mistakenly incorporate FUTP in place of uridine triphosphate during RNA synthesis; this interferes with RNA processing and protein synthesis. Readily absorbed from the GI tract. Peak blood levels, capecitabine: 1.5 hr; peak blood levels, 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.
  

• CAS Registry Number:

  154361-50-9

• Synonyms:

  ;5-Deoxy-5-fluoro-N-[(pentyloxy)carbonyl]cytidine;Pentyl [1-(3,4-dihydroxy-5-methyl-oxolan-2-yl)-5-fluoro-2-oxo-pyrimidin-4-yl]aminoformate;Xeloda;1-(5-deoxypentofuranosyl)-5-fluoro-4-{[(pentyloxy)carbonyl]amino}pyrimidin-2(1H)-one;R-340;Ro-09-1978;N4-[(pentyloxy)carbonyl]-5'-deoxy-5-fluorocytidine;

• Molecular Formula:

  C₉H₁₂FN₃O₄

• Molecular Weight:

  245.2077

• Molecular Structure:

  

• Company:

  Shandong Libaode Chemical Co., Ltd.     [ China ]        

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  +86-530-7612366,7613088

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