Koukourakis Georgios V, Kouloulias Vassilios, Koukourakis Michael J, Zacharias Georgios A, Zabatis Haralabos, Kouvaris John
Attikon University Hospital of Athens, 2nd Radiology Department, Radiation Therapy Unit, Medical School of Athens, Greece.
Molecules. 2008 Aug 27;13(8):1897-922. doi: 10.3390/molecules13081897.
Capecitabine (Xeloda) was developed as a pro-drug of fluorouracil (FU), with the aim of improving tolerability and intratumor drug concentrations through its tumorspecific conversion to the active drug. The purpose of this paper is to review the available information on capecitabine, focusing on its clinical effectiveness against various carcinomas. Identification of all eligible English trails was made by searching the PubMed and Cochrane databases from 1980 to 2007. Search terms included capecitabine, Xeloda and cancer treatment. Nowadays, FDA has approved the use of capecitabine as a first line therapy in patients with metastatic colorectal cancer when single-agent fluoropyrimidine is preferred. The drug is also approved for use as a single agent in metastatic breast cancer patients who are resistant to both anthracycline and paclitaxel-based regimens or when further anthracycline treatment is contraindicated. It is also approved in combination with docetaxel after failure of prior anthracycline-based chemotherapy. In patients with prostate, pancreatic, renal cell and ovarian carcinomas, capecitabine as a single-agent or in combination with other drugs has also shown benefits. Improved tolerability and comparable efficacy, compared with the intravenous FU/LV combination, in addition to its oral administration, make capecitabine an attractive option for the treatment of several types of carcinomas.
卡培他滨(希罗达)是作为氟尿嘧啶(FU)的前体药物开发的,目的是通过其肿瘤特异性转化为活性药物来提高耐受性和肿瘤内药物浓度。本文的目的是回顾关于卡培他滨的现有信息,重点关注其对各种癌症的临床疗效。通过检索1980年至2007年的PubMed和Cochrane数据库来识别所有符合条件的英文试验。检索词包括卡培他滨、希罗达和癌症治疗。如今,美国食品药品监督管理局(FDA)已批准将卡培他滨用作转移性结直肠癌患者的一线治疗药物,前提是首选单药氟嘧啶。该药物也被批准用于对蒽环类和紫杉醇类方案均耐药或进一步使用蒽环类治疗禁忌的转移性乳腺癌患者的单药治疗。它还被批准在先前行基于蒽环类化疗失败后与多西他赛联合使用。在前列腺癌、胰腺癌、肾细胞癌和卵巢癌患者中,卡培他滨作为单药或与其他药物联合使用也显示出益处。与静脉注射FU/LV联合方案相比,卡培他滨耐受性更好且疗效相当,此外它还可口服,这使其成为治疗多种癌症的一个有吸引力的选择。