Because it is not possible to provide a complete coverage of all published papers dealing with IGF system, we have mainly focused on different strategies targeting IGF system in cancer and attempted to provide an overview on IGF system including IGF-1R, its inhibitors and potential limitations of IGF-1R, antibodies and tyrosine kinase inhibitors, IGFBP actions, and blocking IGF via IGFBP (which is better option than blocking IGF receptors) leading to development of novel cancer therapies. The gene discussed is IGF1R; the disease is cancer.