Colorectal cancer represents one of the most common malignant diseases worldwide. Because of the expanding understanding of the biology of this disease entity, and the development/availability of a number novel antitumor agents, therapeutic options have considerably improved within the past few years. As for new drug development, therapeutic advances comprise the oral fluoropyrimidine prodrugs, specific thymidilate synthase inhibitors, irinotecan, oxaliplatin, and signal transduction inhibitors such as the anti-EGF-receptor monoclonal antibody Cetuximab. Compared to the area of conventional 5-fluorouracil therapy, much higher objective response rates and major improvements in overall survival can be achieved today, even in the case of disseminated disease. The aim of this review article is to provide the reader with an overview of presently available treatment options in the palliative, neoadjuvant and postoperative adjuvant setting in colon and rectal cancer, respectively. Furthermore, actual clinical-practice oriented and future perspectives in the management of this disease will be addressed.