Capecitabine

Capecitabine is an oral fluoropyrimidine carbamate that is converted by thymidine phosphorylase (TP) into FU: because TP levels may be higher in tumour than in normal tissue, a specific therapeutic advantage was possible [27]. A substantial efficacy with an acceptable toxicity profile was documented in a phase II study [28].

A total of 1207 patients with previously untreated metastatic colorectal cancer were randomised to either oral capecitabine (1250 mg/m2 twice daily, days 1-14 every 21 days) or IV bolus FU-LV (Mayo regimen). Capecitabine demonstrated a statistically significant superior response rate compared with FU-LV (26 vs. 17%, p<0.0002). The median time to response, duration of response, time to progression and overall survival were equivalent in the two arms (median 12.9 vs. 12.8 months); an improved safety profile was observed and improved convenience compared with IV FU-LV as first-line treatment for metastatic colorectal cancer [29].

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