IGF1R expression was demonstrated on human cancers and the possibility of therapeutically targeting cellular signaling mediated by the receptor suggested in 1987, and antitumor activity of an IGF1R-specific antibody was demonstrated only two years later in a human breast cancer xenograft mouse model by Arteaga and colleagues. In the 1990s and during the first half of the current decade, both epidemiological population-based studies, which showed a correlation between circulating IGF1 levels and cancer risk, and laboratory-based research performed by a number of investigators, which showed that IGFs can promote the growth of multiple types of cancer, provided validation for the relevance of IGF signaling in oncogenesis. Since 2000, a number of agents that target IGF1-IGF1R signaling have been shown to possess antitumor activity in preclinical studies and this research has led to the evaluation currently of more than 10 different drug candidates targeting IGF1 signaling in clinical trials. Initial results from this expanding clinical trial activity were reported in 2007, with the release of results from Phase I trials of IGF1R-antagonistic monoclonal antibodies, and the clinical development has now progressed to include several Phase II trials as well as the recent launch of a Phase III trial (the latter with the fully human monoclonal antibody CP-751,871 from Pfizer) for several of these antibodies.
Balachandran S, Dinsmore C J, Roychowdhury A, et al. Insulin-Like Growth Factor-1 Receptor Inhibitors: U.S. Patent Application 14/113,166[P]. 2012-4-19.