Afatinib: emerging next-generation tyrosine kinase inhibitor for NSCLC

• DOI: 10.2147/ott.s23165
• Publication Date: 2013-03-05T03:00:19Z
• Authors: Mark Agulnik; Nelson; Ziehr; Johnson
• Keywords: Afatinib; T790M; EGFR Inhibitors; Osimertinib; Erlotinib Hydrochloride

The discovery of epidermal growth-factor receptor (EGFR)-activating mutations and the introduction oral EGFR tyrosine kinase inhibitors (EGFR-TKIs) have expanded treatment options for patients with non-small cell lung cancer. first two reversible EGFR-TKIs, erlotinib gefitinib, are approved use in first-line setting known EGFR-activating second- third-line settings all NSCLC patients. These first-generation EGFR-TKIs improve progression-free survival when compared to chemotherapy setting. However, nearly develop resistance EGFR-directed agents. There is a need further therapy disease progression after EGFR-TKIs. Afatinib an irreversible ErbB family blocker that inhibits EGFR, HER2, HER4. In vitro vivo, afatinib shown increased inhibition common as well T790M mutation gefitinib. Clinically, has been evaluated LUX-Lung series trials, improvement reported both first- second-/third-line chemotherapy. Further investigation needed determine precise role will play cancer mutations.