Although drugs such as the taxoids and vinorelbine have increased the optio
ns available for anthracycline-resistant metastatic breast cancer, new ther
apeutic options are needed, particularly for taxoid-refractory tumours. Inc
reasing emphasis is being placed on the development of oral agents, which m
any patients prefer provided efficacy is not compromised, particularly ii t
he oral agents are less toxic than current intravenous agents. Capecitabine
, a new, oral fluoropyrimidine, mimics continuous infusion 5-FU and is acti
vated preferentially at the tumour site. Phase II studies of capecitabine h
ave demonstrated encouraging response rates in patients with few further tr
eatment options (20% response with an additional 43% achieving stable disea
se in paclitaxel-refractory patients; 36% response with a further 23% achie
ving stable disease in anthracycline-refractory patients). In addition, a r
andomized, phase II trial demonstrated a response rate of 30% (95% CI: 19-4
3%) with capecitabine as first-line treatment for metastatic breast cancer,
compared with 16% (95% CI: 5-33%) in patients receiving low-dose CMF. Thes
e trials also showed that capecitabine has a favourable safety profile typi
cal of infused fluoropyrimidines. Both alopecia and myelosuppression were r
are. Capecitabine may therefore provide an effective, well-tolerated and co
nvenient alternative to intravenous cytotoxic agents, not only in taxoid-re
sistant patients, but also in anthracycline-resistant metastatic breast can
cer or as first-line therapy. Furthermore, the low incidence of myelosuppre
ssion makes capecitabine an attractive agent for incorporation into combina
tion regimens with agents such as epirubicin/doxorubicin, the taxoids and v
inorelbine. (C) 2001 Cancer Research Campaign.