Capecitabine, a new oral fluoropyrimidine for the treatment of colorectal cancer

✍ Scribed by Francesco Di Costanzo; Andrea Sdrobolini; Silvia Gasperoni

• Publisher: Elsevier Science
• Year: 2000
• Tongue: English
• Weight: 200 KB
• Volume: 35
• Category: Article
• ISSN: 1040-8428
• DOI: 10.1016/s1040-8428(00)00059-7

✦ Synopsis

Capecitabine (Xeloda) ® was developed as a tumour-selective fluoropyrimidine carbamate to achieve higher intratumoural 5-FU level and lower toxicity than 5-FU. Capecitabine passes unchanged through the gastrointestinal tract and is metabolised in the liver to 5%-deoxy-5-fluorocytidine (5%-DFCR). Here it is converted to doxifluridine (5%-DFUR) and finally, 5%-DFUR is metabolised by thymidine phosphorilase to 5-FU at the tumour site. Preclinical studies have demonstrated capecitabine's activity in both 5-FU-sensitive and 5-FU-resistant tumours. In a randomised phase II trial in advanced colorectal cancer the recommended dose and schedule of Capecitabine is 2.510 mg/m 2 /day (total dose divided into two equal morning and evening doses) given in an intermittent schedule (2 weeks on/1 week off). Phase III trials in patients with advanced colorectal cancer show a better response rate than the Mayo Clinic schedule, with no differences in terms of DR, PFS. Diarrhoea and hand-foot syndrome were the principal grade 3/4 toxicities noted, occurring in 10% and 16% of patients, respectively. The selectivity of this drug opens an important prospective in the treatment of colorectal cancer in advanced and adjuvant setting.