The treatment of advanced colorectal cancer over the past 4 decades has req
uired the use of intravenous chemotherapy, most typically fluorouracil (5-F
U). The possibility of providing mt alternative to intravenous delivery whi
le at the same time improving the quality of life of patients who require f
luorouracil for advanced or adjuvant therapy has provided the stimulus for
the development of oral fluoropyrimidine drugs. Five oral fluoropyrimidine
drugs have recently entered clinical trials in the United States, These inc
lude capecitabine (Xeloda), UFT(uracil and tegafur) or UFT/leucovorin (Orze
l), eniluracil (ethynyluracil) S-1, and BOF A-2, At least two of these drug
s have demonstrated survival equivalent to the standard intravenous fluorou
racil and leucovorin regimens used to treat advanced colorectal cancer. Thi
s, together,with less severe toxicity and potential increased quality of li
fe, should lead to approval of one or more of these oral agents in the near
future. Based on both patient and physician acceptance of oral fluoropyrim
idines, other oral drugs from classes other than fluoropyrimidines will lik
ely be developed in the near future.