Oxaliplatin, a second-generation platinum analog, has evolved as one of the most important therapeutic agents in colorectal cancer (CRC) treatment. It has had a major impact on the management and outcome of this disease. AREAS COVERED: The pharmacokinetic and pharmacodynamic data of oxaliplatin are reviewed in this paper. It also discusses the current clinical data regarding the use of oxaliplatin in early colon cancer, locally advanced rectal cancer, and in the metastatic setting, with a particular reference to its combination with monoclonal antibodies, and strategies for prevention of cumulative toxicity. EXPERT OPINION: Oxaliplatin has proven beneficial in the treatment of CRC and can currently be regarded as one of the three most important chemotherapeutic drugs used in the treatment of both metastatic disease and adjuvant therapy in stage II/III after resection. With regards to a median overall survival of more than 20 months, and a median progression-free survival for first-line treatment of about 9 - 10 months, the majority of patients will receive all three compounds (oxaliplatin, fluoropyrimidines and irinotecan) during the course of their disease. At the moment there are no drugs in late clinical development which might be able to substitute oxaliplatin in its unique role in CRC.
