In EGFRm advanced NSCLC
*Afatinib, erlotinib, and gefitinib
†Defined as gefitinib and erlotinib.
Acquired resistance affects patients who initially responded to first-generation† EGFR TKI therapy, then stopped responding. Acquired resistance occurs in most NSCLC patients treated with first-generation† EGFR TKIs.12
‡Studies published in the past 4 years (erlotinib, gefitinib). Primary manuscript, N≥50. Prospective tissue biopsy performed at disease progression. Primary endpoint = examining molecular mechanisms of acquired resistance; methodology reported.
Resistant Mechanisms to EGFR TKIs
Resistant Mechanisms to EGFR TKIs
Steric hindrance, which reduces receptor binding of reversible EGFR TKIs22
Increased binding affinity of EGFR for ATP, resulting in reduced TKI potency23
Obstáculo estérico, que reduz a ligação aos receptores de TKIs do EGFR reversíveis22
Afinidade de ligação aumentada do EGFR por ATP, resultando em potência reduzida do TKI23
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