DZD1516

DZD1516 is an orally bioavailable, blood-brain barrier-penetrant, and highly selective small molecule inhibitor of the receptor tyrosine kinase human epidermal growth factor receptor 2 (HER2; also known as ErbB2). It is designed to selectively bind to and inhibit HER2 activity, thereby blocking downstream signaling pathways involved in tumor cell proliferation and survival. DZD1516 demonstrates potent antitumor activity in preclinical models, particularly against HER2-positive cancers with central nervous system involvement. The drug has shown good selectivity for HER2 over wild-type EGFR, minimizing off-target effects such as skin rash or diarrhea commonly associated with less selective inhibitors. Clinical studies have focused on patients with HER2-positive metastatic breast cancer who have relapsed after multiple prior treatments[1][3][4][5].

Other names

HER2 inhibitor DZD1516HER-2 inhibitor DZD1516HER 2 inhibitor DZD1516