When are third-generation endothelial growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) indicated for the treatment of non–small cell lung cancer (NSCLC)?

Updated: Jun 05, 2020
  • Author: Winston W Tan, MD, FACP; Chief Editor: Nagla Abdel Karim, MD, PhD  more...
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Answer

In many cases, tumors treated with agents directed against EGFR eventually develop resistance to the drugs. The EGFR T790M mutation is the most common mechanism of resistance to first-generation and second-generation EGFR TKIs. Several third-generation drugs have been developed to counteract this phenomenon, including rociletinib and osimertinib (now approved in the US). [187] A unique characteristic of rociletinib is its ability to bind to T790M but not to wild-type EGFR, thus causing milder adverse effects (eg, rash, diarrhea) in lung cancer.


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