In this video, the wide-ranging aspects of the evolution of EGFR-TKIs were described, with a special focus on rociletinib. The influence of different oncogenic mutations on EGFR activity was also discussed. Resistance to the first (erlotinib, gefitinib)- and second (afatinib)-generation EGFR-TKIs provided the rationale behind the development of the third-generation inhibitors (rociletinib, osimertinib). On the basis of these data, a comparison of their efficacy on the different mutated EGFRs and the respective resistance mechanisms is further reported. Moreover, the evolution and results of the clinical trials of rociletinib (TIGER trials) are compared with the trials on osimertinib, another third-generation EGFR-TKI that now has been granted US Food and Drug Administration approval. The reasons behind the arrest in the further development of rociletinib are put in the perspective of future drug development.
This video has been published as supplemental file to the article:
Onco Targets Ther. 2016 Oct 6;9:6065-6074. eCollection 2016.
New developments in the management of non-small-cell lung cancer, focus on rociletinib: what went wrong?
Van Der Steen N, Caparello C, Rolfo C, Pauwels P, Peters GJ, Giovannetti E