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Third generation EGFR TKIs: current data and future directions.


ABSTRACT: Acquired T790 M mutation is the commonest cause of resistance for advanced non-small cell lung cancer (NSCLC) epidermal growth factor receptor (EGFR) mutant patients who had progressed after first line EGFR TKI (tyrosine kinase inhibitor). Several third generation EGFR TKIs which are EGFR mutant selective and wild-type (WT) sparing were developed to treat these patients with T790 M acquired resistant mutation. Osimertinib is one of the third generation EGFR TKIs and is currently the most advanced in clinical development. Unfortunately, despite good initial response, patients who was treated with third generation EGFR TKI would develop acquired resistance and several mechanisms had been identified and the commonest being C797S mutation at exon 20. Several novel treatment options were being developed for patients who had progressed on third generation EGFR TKI but they are still in the early phase of development. Osimertinib under FLAURA study had been shown to have better progression-free survival over first generation EGFR TKI in the first line setting and likely will become the new standard of care.

SUBMITTER: Tan CS 

PROVIDER: S-EPMC5817792 | biostudies-literature | 2018 Feb

REPOSITORIES: biostudies-literature

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Third generation EGFR TKIs: current data and future directions.

Tan Chee-Seng CS   Kumarakulasinghe Nesaretnam Barr NB   Huang Yi-Qing YQ   Ang Yvonne Li En YLE   Choo Joan Rou-En JR   Goh Boon-Cher BC   Soo Ross A RA  

Molecular cancer 20180219 1


Acquired T790 M mutation is the commonest cause of resistance for advanced non-small cell lung cancer (NSCLC) epidermal growth factor receptor (EGFR) mutant patients who had progressed after first line EGFR TKI (tyrosine kinase inhibitor). Several third generation EGFR TKIs which are EGFR mutant selective and wild-type (WT) sparing were developed to treat these patients with T790 M acquired resistant mutation. Osimertinib is one of the third generation EGFR TKIs and is currently the most advance  ...[more]

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