Hordenine not appropriate. More effective, better tolerated and more convenient chemotherapy is required for these patients. Moreover, a reported 84–89% of cancer patients would prefer oral to injected medications, given equivalent efficacy. Capecitabine is a novel oral fluorocytidine derivative discovered at the Nippon Roche Kamakura Laboratory (currently Chugai Pharmaceutical Co., Ltd. Kamakura Laboratory) that is designed to be converted to 5FU in steps to allow for selective delivery of high-dose 5FU to the target tumour while minimizing systemic exposure.
After oral administration, capecitabine is absorbed unchanged from the gastrointestinal Troxerutin tract and metabolized in the liver to 50-DFCR by carboxylesterase. The 50-DFCR is subsequently converted to 50-DFUR by cytidine deaminase, which is highly active primarily in the liver and tumour tissue. The 50-DFUR is then selectively converted in the tumour tissue to 5FU by thymidine phosphorylase, which is highly active in tumour tissue. Based on the findings of capecitabine monotherapy in metastatic colon and rectal cancer, a phase III clinical trial (X-ACT trial) was conducted to compare capecitabine to bolus 5FU/LV therapy (Mayo Clinic regimen) as adjuvant chemotherapy in resected stage purchase PF-562271 III colon cancer.
Twelves et al. reported that the capecitabine therapy in the study was at least equivalent to 5FU/LV therapy (Mayo Clinic regimen) in terms of the primary endpoint of 3-year disease-free survival (DFS) as well as overall survival (OS). In addition, capecitabine was associated with fewer gastrointestinal disturbances such as diarrhoea and stomatitis, indicating a superior safety profile. Capecitabine was approved in the US and Europe in order Phlorizin 2005 based on these results. Currently, the NCCN Guidelines include capecitabine monotherapy among the standard treatments for postoperative adjuvant chemotherapy in stage III colon cancer. Occasionally, the treatment must be suspended due to the development of the characteristic adverse reaction of hand–foot syndrome (HFS).
The treatment completion rate was 83.0% in the X-ACT trial, in which capecitabine was recognized as a standard postoperative adjuvant chemotherapy for colorectal cancer. Although capecitabine was approved in Japan based on the results of this trial, it has not yet been established to be a safe postoperative adjuvant therapy for colon cancer in Japanese patients. Accordingly, a feasibility study with an endpoint of the treatment completion rate of capecitabine in Japanese patients was planned. Patients who met any of the following criteria were excluded from participation in the study. Pregnant or lactating, or planning to become pregnant. History of hypersensitivity or severe adverse reaction to fluoropyrimidines. Past organ transplant. Serious concurrent disease [including muscular interstitial pneumonia, pulmonary fibrosis, intestinal paralysis, ileus, poorly controlled diabetes, liver cirrhosis or hepatitis (type B or C), poorly controlled hypertension, history of myocardial infarction or unstable angina within past 6 months]. Active multiple primary cancer (disease-free less than 5 years). Concurrent infectious disease.