A Review on Anticancer Potential and Structure-Activity Relationships (SAR) of Novel EGFR/HER2 Inhibitors. (PubMed, Curr Top Med Chem)
EGFR/HER2 dual inhibitors, approved by the US FDA (Food and Drug Administration), include lapatinib, afatinib, neratinib, dacomitinib, etc., but these drugs lack selectivity, specificity, and undesirable adverse effects. The present manuscript focuses on the identification and development of therapeutic molecules that can inhibit the target proteins EGFR/HER2 and can further be used for the treatment of breast and lung malignancies. It also highlights the development of EGFR/HER2 dual inhibitors that belong to different structural classes like pyrimidine, quinazoline, pyridine, benzimidazole, and quinoline etc. Various parameters, such as Structure-Activity Relationships (SAR), clinical trials data, patent filed, and the molecular docking study of the most potent compounds provide a valuable asset for further designing and discovering new EGFR/HER2 dual inhibitors with potential therapeutic significances for cancer treatment.