Institut de cancérologie, Hôpital privé Jean Mermoz, 55, avenue Jean Mermoz 69008 Lyon
The only oral molecules with demonstrated efficacy in colorectal cancer belong to the family of fluoropyrimidines. 5-fluorouracil (5FU), an antimetabolite antipyrimidine whose effects are modulated by folinic acid, has been the first cytotoxic drug used for the treatment of colorectal cancers, and still remains the pivotal molecule for all colorectal cancer stages, either alone or in combination with other chemotherapy targeted therapy drugs. Infusional administration of 5FU has replaced bolus administration, as it is more effective and less toxic. However, infusional administration requires the implantation of a central venous access, carrying a non-negligible rate of infectious or thrombotic complications. In addition, the need for infusion devices increases equipment and personnel costs and generates constraints that may affect patients’ quality of life. It thus appeared attractive to replace 5FU infusion by oral prodrugs (capecitabine, tegafur-uracil), since plasma and/or tumor concentrations in active metabolites were found to be broadly similar to those obtained from 5FU infusion. This pharmacokinetic equivalence, the results of available trials, and a better convenience and acceptability for patients allow considering oral fluoropyrimidines to be a valid alternative to intravenous 5FU for the treatment of colorectal cancer in the metastatic or adjuvant setting.