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Table 2 Different generations of EGFR TKIs

From: Management of acquired resistance to EGFR TKI–targeted therapy in advanced non-small cell lung cancer

Generation EGFR inhibition Drug Molecular Targetsa Adverse effect Status
1st-generation Reversible; Gefitinib EGFR del19, L858R Skin rash/acne, abnormal LFT FDA approved
competitive Erlotinib EGFR del19, L858R   FDA approved
2nd-generation Irreversible; covalent Afatinib EGFR del19, L858R, uncommon mutations, HER2, HER4 Diarrhea, paronychia. Skin rash FDA approved
  Dacomitinib EGFR del19, L858R, HER2, HER4 Diarrhea, skin rash/acne Phase III
  Neratinib EGFR G719X, HER2, HER4 Diarrhea, dyspnea, N/V Phase II
3rd-generation Irreversible; Osimertinib EGFR mutations and T790M Diarrhea, skin rash FDA approved
covalent Rociletinib EGFR T790M mutation, IGF-1R Hyperglycemia, QTc prolong Withdrawn
  Olmutinib EGFR T790M mutation Diarrhea, skin exfoliation, nausea Approved in South Korea
  ASP8273 EGFR L858R, del19, T790M, Diarrhea, N/V, thrombocytopenia Phase III Discontinued
  Nazartinib EGFR L858R, del19, T790M, Rash, diarrhea, pruritus Phase I/II
  Avitinib (AC0010) EGFR L858R, del19, T790M, Diarrhea, skin rash, abnormal LFT Phase I/II
  HS-10296 EGFR sensitive mutations (G719X, del19, L858R, L861Q) +/− T790M None reported Phase I/II
  PF-06747775 EGFR L858R, del19, T790M, None reported Phase I/II
  1. N/V nausea and/or vomiting, LFT liver function test, del19 deletion in exon19, EGFR epidermal growth factor receptor, FDA Food and Drug Administration
  2. aThe targets included FDA approved or associated targets