The epidermal growth factor receptor (EGFR) family includes four structurally related receptor tyrosine
kinases, termed as HER1 (EGFR, erbB1), HER2 (erbB2), HER3 (erbB3), and HER4 (erbB4). Given its intimate role in
the development of several solid tumors, excessive HER signaling provides a unique opportunity for anticancer intervention.
Along with extensive pharmacological studies validating the therapeutic potential of targeting the EGFR family for
cancer therapy, kinase inhibitors of this family are continuously coming up and entering clinical studies. Herein, we review
the EGFR family small molecule kinase inhibitors which have been approved or progressed into clinical studies,
mainly focusing on their mechanisms of action, structure-activity relationships, binding modes, synthetic routes, and clinical