Introduction: EGFR is the receptor for epidermal growth factor (EGF) and belongs to the protein tyrosine kinase (PTK) receptor. It is closely related to the inhibition of tumor cell proliferation, invasion, and apoptosis. Overexpression or mutation activation of EGFR is involved in the development of many human malignancies, especially non-small cell lung cancer (NSCLC). At present, numerous small molecule tyrosine kinase inhibitors (TKIs) have been developed to target the ATP-binding region of EGFR, aiming to develop selective and effective inhibitors for the treatment of NSCLC against EGFR mutants.Areas covered: This review covers the latest progress in the patented EGFR inhibitors and the inhibition activity against NSCLC from 2014 to present.Expert opinion: EGFR is an important anti-tumor target, and small molecule inhibitors targeting EGFR have become important biologically active compounds for the treatment of cancer, especially against NSCLC. Among the recent patents available, great majority of them focus on selective inhibitors of EGFR mutants. Although great achievements have been made in the development of selective EGFR inhibitors, there is still an urgent need to discover new EGFR inhibitors which are safe, efficient, selective, and low-toxic to avoid the adverse pharmacokinetics caused by wild-type EGFR feature.
Keywords: Cancer; EGFR; EGFR-TKIs; NSCLC; resistance mutation.