epertinib

Epertinib is a potent, orally active small molecule tyrosine kinase inhibitor that selectively and reversibly targets the epidermal growth factor receptor (EGFR/erbB1), human epidermal growth factor receptor 2 (HER2/erbB2), and human epidermal growth factor receptor 4 (HER4/erbB4). It inhibits these kinases by binding to their ATP-binding sites, thereby blocking downstream signaling pathways involved in tumor cell proliferation and survival. Epertinib has demonstrated antitumor activity in preclinical models and clinical trials, particularly in HER2-positive breast cancer—including cases with brain metastases—and other solid tumors. The drug was originally developed by Shionogi and has been licensed to EOC Pharma for development in China. Clinical studies have shown that epertinib is generally well-tolerated with manageable side effects such as diarrhea[1][3][5][6].

Other names

epertinib hydrochloride