Targeting EGFR T790M mutation in NSCLC: From biology to evaluation and treatment

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26 Citations (Scopus)

Abstract

The identification of EGFR mutations and their respectively tyrosine kinase inhibitors (TKIs), changed dramatically treatment and survival of patients with EGFR-positive lung cancer. Nowadays, different EGFR TKIs as afatinib, erlotinib and gefitinib are approved worldwide for the treatment of NSCLC harbouring EGFR mutations, in particular exon 19 deletions or exon 21 (Leu858Arg) substitution EGFR mutations. In first-line setting, when comparing with platinum-based chemotherapy, these target drugs improves progression-free survival, response rate and quality of life. Unfortunately, the development of different mechanism of resistance, limits the long term efficacy of these agents. The most clear mechanism of resistance is the development of EGFR Thr790Met mutation. Against this new target, different third-generation EGFR-mutant-selective TKIs, such as osimertinib, rociletinib and olmutinib, showed a great activity. In this review, we summarize the scientific evidences about biology, evaluation and treatment on NSCLC with EGFR T790M mutation.

Original languageEnglish
Pages (from-to)406-415
Number of pages10
JournalPharmacological Research
Volume117
DOIs
Publication statusPublished - Mar 1 2017

Fingerprint

Mutation
Protein-Tyrosine Kinases
Exons
Therapeutics
Platinum
Disease-Free Survival
Lung Neoplasms
Survival Rate
Quality of Life
Drug Therapy
Survival
Pharmaceutical Preparations

Keywords

  • EGFR
  • Liquid biopsy
  • NSCLC
  • Olmutinib
  • Osimertinib
  • Rociletinib
  • T790M

ASJC Scopus subject areas

  • Pharmacology

Cite this

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title = "Targeting EGFR T790M mutation in NSCLC: From biology to evaluation and treatment",
abstract = "The identification of EGFR mutations and their respectively tyrosine kinase inhibitors (TKIs), changed dramatically treatment and survival of patients with EGFR-positive lung cancer. Nowadays, different EGFR TKIs as afatinib, erlotinib and gefitinib are approved worldwide for the treatment of NSCLC harbouring EGFR mutations, in particular exon 19 deletions or exon 21 (Leu858Arg) substitution EGFR mutations. In first-line setting, when comparing with platinum-based chemotherapy, these target drugs improves progression-free survival, response rate and quality of life. Unfortunately, the development of different mechanism of resistance, limits the long term efficacy of these agents. The most clear mechanism of resistance is the development of EGFR Thr790Met mutation. Against this new target, different third-generation EGFR-mutant-selective TKIs, such as osimertinib, rociletinib and olmutinib, showed a great activity. In this review, we summarize the scientific evidences about biology, evaluation and treatment on NSCLC with EGFR T790M mutation.",
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author = "Antonio Passaro and Elena Guerini-Rocco and Alessia Pochesci and Davide Vacirca and Gianluca Spitaleri and Catania, {Chiara Matilde} and Alessandra Rappa and Massimo Barberis and {de Marinis}, Filippo",
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AU - Passaro, Antonio

AU - Guerini-Rocco, Elena

AU - Pochesci, Alessia

AU - Vacirca, Davide

AU - Spitaleri, Gianluca

AU - Catania, Chiara Matilde

AU - Rappa, Alessandra

AU - Barberis, Massimo

AU - de Marinis, Filippo

PY - 2017/3/1

Y1 - 2017/3/1

N2 - The identification of EGFR mutations and their respectively tyrosine kinase inhibitors (TKIs), changed dramatically treatment and survival of patients with EGFR-positive lung cancer. Nowadays, different EGFR TKIs as afatinib, erlotinib and gefitinib are approved worldwide for the treatment of NSCLC harbouring EGFR mutations, in particular exon 19 deletions or exon 21 (Leu858Arg) substitution EGFR mutations. In first-line setting, when comparing with platinum-based chemotherapy, these target drugs improves progression-free survival, response rate and quality of life. Unfortunately, the development of different mechanism of resistance, limits the long term efficacy of these agents. The most clear mechanism of resistance is the development of EGFR Thr790Met mutation. Against this new target, different third-generation EGFR-mutant-selective TKIs, such as osimertinib, rociletinib and olmutinib, showed a great activity. In this review, we summarize the scientific evidences about biology, evaluation and treatment on NSCLC with EGFR T790M mutation.

AB - The identification of EGFR mutations and their respectively tyrosine kinase inhibitors (TKIs), changed dramatically treatment and survival of patients with EGFR-positive lung cancer. Nowadays, different EGFR TKIs as afatinib, erlotinib and gefitinib are approved worldwide for the treatment of NSCLC harbouring EGFR mutations, in particular exon 19 deletions or exon 21 (Leu858Arg) substitution EGFR mutations. In first-line setting, when comparing with platinum-based chemotherapy, these target drugs improves progression-free survival, response rate and quality of life. Unfortunately, the development of different mechanism of resistance, limits the long term efficacy of these agents. The most clear mechanism of resistance is the development of EGFR Thr790Met mutation. Against this new target, different third-generation EGFR-mutant-selective TKIs, such as osimertinib, rociletinib and olmutinib, showed a great activity. In this review, we summarize the scientific evidences about biology, evaluation and treatment on NSCLC with EGFR T790M mutation.

KW - EGFR

KW - Liquid biopsy

KW - NSCLC

KW - Olmutinib

KW - Osimertinib

KW - Rociletinib

KW - T790M

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