Oxaliplatin is a new cytotoxic drug, with a mechanism of action nearly similar to that of cisplatin. However, in vitro and in vivo studies showed an interesting activity in colorectal cancer. This article summarizes the main data available for patients with advanced colorectal cancer concerning phase I studies, pharmacokinetic, single agent phase II studies, combinations with 5-fluorouracil (5-FU), and tolerance. 10% response rate in second-line therapy, 20 to 25% in first-line, and 26 to 45% in combination with 5-FU in second-line have been reported. The limiting toxicity is a reversible sensitive neuropathy. Oxaliplatin combined with 5-FU should be considered as one of the best therapeutic options in second-line colorectal cancer patients. Further studies will indicate the role of oxaliplatin in less advanced disease, such as metastatic first-line or adjuvant therapy.