Due to the rapid development in cytotoxic agents and molecular target drugs, the response rate of advanced colorectal cancer patients has been elevated, and the overall survival has been prolonged. Some clinical trials even lead the median survival beyond 2 years. This article focused on the following issues: comparing single agent chemotherapy and combined chemotherapy, comparing different combined chemotherapy regimens, exploring the possibility of replacing 5-fluorouracil (5-FU) with capecitabine, introducing the stop-and-go conception, and analyzing the roles that molecular target agents, including Bevacizumab and Erbitux, have taken. The elucidation of above issues revealed that the efficacy of combined chemotherapy on advanced colorectal carcinoma is better than that of single agent therapy; both FOLFOX and FOLFIRI regimens are recommended as first-line chemotherapy, and can be crossed over as second-line chemotherapy; capecitabine can effectively replace 5-FU infusion while combined with oxaliplatin, but may not be a good option with irinotecan; available data support a stop-and-go strategy in metastasic colorectal Earcinoma if enough chemotherapy is given before stop; both Bevacizumab and Erbitux are active in improving the survival and response rate.