Oxaliplatin (trans-/-diaminocyclohexane oxalatoplatinum; L-OHP) is a new platinum derivative for the treatment of advanced colorectal cancer. Preclinical data have shown that oxaliplatin is active in a wide range of human and murine tumour cell lines, and has been found to be non-cross-resistant with cisplatin in various cisplatin-resistant cell lines and tumours. Oxaliplatin in combination with 5-fluorouracil (5-FU) leads to synergistic antiproliferative activity both in vivo and in vitro. Clinical data have shown that oxaliplatin is active and well tolerated both as monotherapy and in combination with 5-FU/folinic acid in first- or second-line treatment of patients with metastatic colorectal cancer. Oxaliplatin has a very good safety profile, and studies have confirmed that peripheral sensory neuropathy is related to the cumulative dose of oxaliplatin administered and that this neuropathy is generally reversible after discontinuation of treatment. High response rates and prolonged survival have been achieved in metastatic colorectal cancer patients, even after 5-FU failure.