卡培他滨的药理作用 卡培他滨的药品概况及适应症状

药品概况

  卡培他滨通用名称:卡培他滨

  英文名称:Capecitabine

  化学名:5'-脱氧-5-氟-N-[(戊氧基)羰基]胞啶

  商品名:希罗达

  分子式:C15H22O6N3F

  Cas No:154361-50-9

  分子量:359.35

  干燥失重:≤1.0% 

  含 量:大于99.0%

  有关物质:<0.5%

药理作用

  Classification: Antineoplastic, antimetabolite

  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.

适应症状

  希罗达适用于紫杉醇和包括有蒽环类抗生素化疗方案治疗无效的晚期原发性或转移性乳腺癌的进一步治疗。

  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).

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