Capecitabine is an orally administered fluoropyrimidine carbamate used for the treatment of paclitaxel- or anthracycline-refractory breast cancer. Capecitabine is metabolised via a 3-step process to the active agent fluorouracil. The final step of this process occurs preferentially in malignant tissue. In patients with paclitaxel-refractory breast cancer receiving capecitabine (2510 mg/m2/day for 2 weeks of a 3-week cycle) the objective tumour response rate was 20%. Disease progression occurred in 34% of patients and 40% had stable disease. In this trial, the median duration of response was 241 days. Disease progression or death occurred in 83% of patients, and median time to progression was 93 days. Median survival time was 384 days. In previously untreated patients with breast cancer, the response rate was higher and time to disease progression was longer after oral capecitabine (2510 mg/m2/day for 2 weeks of a 3-week cycle) than after intravenous cyclophosphamide, methotrexate and fluorouracil therapy. In clinical trials, generally gastrointestinal or haematological adverse events were reported most frequently. Other commonly reported events included hand-and-foot syndrome, fatigue, hyperbilirubinaemia, dermatitis and anorexia.