Fourth-Generation Allosteric EGFR Tyrosine Kinase Inhibitors to Combat the Drug Resistance Associated with Non-small Cell Lung Cancer (NSCLC)

Insights into fourth generation selective inhibitors of (C797S) EGFR mutation combating non-small cell lung cancer resistance: a critical review

“…According to reports, EAI001 (12) and EAI045 ( 13) are fourth-generation EGFR allosteric kinase inhibitors that have therapeutic effects despite the C797S mutation. 86 Due to their unique binding locations with the target, allosteric kinase inhibitors oen function as a potential complementary therapeutic method to ATP-competitive kinase inhibitors. It doesn't bind to Cys797 because its residue is outside the allosteric binding pocket 87,88 (Fig.…”

“…126 On the other hand, the fourth-generation EGFR TKIs that target the allosteric binding site can assist in overcoming "undruggable" resistance (C797S) with expected negligible side effects. 86 4. Cost-effectiveness of using EGFR-TKI in treatment for EGFR-mutated advanced NSCLC…”