The aim was to review available literature on capecitabine-based chemoradiation regimens for the preoperative treatment of patients with locally advanced rectal cancer (LARC) and determine efficacy and safety data for capecitabine in this setting. Medical literature databases (Pubmed, Medline) and abstracts/posters presented at recent scientific congresses (ASCO, ASTRO, ESTRO and ECCO) were screened and critically analysed to identify relevant data. A number of phase I/II studies have demonstrated that capecitabine is effective and well tolerated in combination with preoperative radiotherapy in patients with LARC. Phase III studies are ongoing. Continuous oral administration of capecitabine (825 mg/m2 twice daily for 7 days/week) is an effective regimen and has similar tolerability to the less dose-intensive intermittent regimens of capecitabine given 5 days/week followed by 2 day's rest or 14 days followed by 7 day's rest as used in systemic chemotherapy for patients with colorectal or breast cancer. Capecitabine chemoradiation is associated with a relatively low rate of grade 3/4 adverse events. Capecitabine simplifies chemoradiation and provides a convenient treatment option for both patients and health care professionals. Combining capecitabine with cytotoxic agents such as oxaliplatin and irinotecan has the potential to further improve antitumour efficacy in patients receiving preoperative chemoradiation. Data from phase I/II single-agent and combination capecitabine chemoradiation studies provide a clear rationale for replacing infusional 5-FU with oral capecitabine as part of chemoradiation for patients with LARC.