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Representative EGFR TKIs currently in use or development
| First generation (target WT EGFR) | Second generation (irreversible inhibitors of EGFR and HER2) | Third generation (EGFR mutant-specific, irreversible inhibitors) |
|---|---|---|
|
| ||
| Erlotinib* | Neratinib | Rociletinib (Clovis) |
| Gefitinib | Afatinib* | AZD9291 (AstraZeneca) |
| Icotinib | Dacomitinib | HM61713 (Hanmi) EGF816 (Novartis) ASP8273 (Astellas) |
FDA-approved in the US for treatment of lung cancer
