Allosteric mutant-selective fourth-generation EGFR inhibitors as an efficient combination therapeutic in the treatment of non-small cell lung carcinoma

  • Drug Discov Today. 2021 Jun;26(6):1466-1472. doi: 10.1016/j.drudis.2021.02.005.
Surya Kant Tripathi  1 ,  Bijesh K Biswal  2
Affiliations
  • 1. Cancer Drug Resistance Laboratory, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India.
  • 2. Cancer Drug Resistance Laboratory, Department of Life Science, National Institute of Technology Rourkela, Odisha 769008, India. Electronic address: [email protected].
PMID: 33581322 DOI: 10.1016/j.drudis.2021.02.005
Abstract

Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR-TKIs) show most preferable treatment for non-small cell lung carcinoma (NSCLC) with EGFR activating mutations. Despite initial impressive response of first-, to third-generation EGFR-TKIs, these agents become ineffective because of rapid emergence of EGFR mutations (T790M or C797S) mediated resistance. Allosteric mutant-selective fourth-generation EGFR inhibitors appeared to be possible therapeutic option to overcome resistance. These EGFR inhibitors are less effective as a single agent but provide synergistic effect as a combinatorial drug with conventional chemo- or immunotherapeutic. Here, we aim to highlight the comprehensive overview on combined therapeutic efficacy of allosteric EGFR inhibitors for the treatment of EGFR mutant NSCLC.

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