Inhibition of EGFR has been used successfully to treat cancer patients.  However, drug resistance develops after a few weeks of treatment and this is one of the major problems associated with this target.  There are two possible mechanisms of resistance: the development of secondary mutations and over-activation of parallel pathways.  We have previously reported that co-targeting IGFR and EGFR kinases by dual inhibitors may offer a promising approach to anti-cancer therapy. A dual EGFR/IGF-1R inhibitor is expected not only to be beneficial in addressing the problems of resistance but may also provide unique opportunities for pharmacological intervention.  The SAR is described which led to the identification of a novel, small molecule dual EGFR/IGF-1R inhibitor with potent in vitro activity in cell-free and cell-based assays and potent in vivo efficacy.

Dual EGFR/ IGFR inhibitor: A novel approach to overcome resistance

245th National Meeting (2013)

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