The 3-step activation process of XELODA preferentially generates 5-fluorouracil (5-FU) through thymidine phosphorylase (TP) at the tumor site

  • TP is present in higher concentrations in some tumor tissue vs healthy tissue.
  • XELODA delivers increased concentration of 5-FU to colorectal tumor tissue.
Metabolic pathway of capecitabine to 5-FU
 

XELODA provides greater concentration of 5-FU in colorectal tumor tissue than in adjacent healthy tissue or plasma.1

 
Mean 5-FU colorectal concentration ratios
*Adapted from Schüller J, et al.1
 
Preclinical data: clinical significance unknown.
 

Prolonged cytotoxic presence

Cytotoxic activity in tumor tissue for 2 full weeks at a time.

Extended exposure
*20 mg/m2 leucovorin IV followed by 425 mg/m2 IV bolus 5-FU on days 1-5 every 28 days.
†CI = continuous infusion.
‡200 mg/m2 leucovorin IV followed by 400 mg/m2 bolus 5-FU and a 22-hour infusion of 600 mg/m2 5-FU on days 1 and 2 every 14 days.

XELODA-Established clinical activity to achieve your goals in Colorectal and metastatic Breast Cancer treatment


REFERENCES
1. Schüller J, Cassidy J, Dumont E, et al. Preferential activation of capecitabine in tumor following oral administration to colorectal cancer patients. Cancer Chemother Pharmacol. 2000;45:291-297.
2. Hoff PM, Ansari R, Batist G, et al. Comparison of oral capecitabine versus intravenous fluorouracil plus leucovorin as first-line treatment in 605 patients with metastatic colorectal cancer: results of a randomized phase III study. J Clin Oncol. 2001;19(8):2282-2292.
3. Andre T, Colin P, Louvet C, et al. Semimonthly versus monthly regimen of fluorouracil and leucovorin administered for 24 or 36 weeks as adjuvant therapy in stage II and III colon cancer: results of a randomized trial. J Clin Oncol. 2003;21(15):2896-2903.

 
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