enozertinib

Enozertinib is a **brain-penetrant, orally bioavailable, irreversible small molecule inhibitor** designed to selectively target both **epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (HER2)**, with high potency against exon 20 insertion mutations. It demonstrates superior brain exposure and kinome selectivity in preclinical models compared to other clinical inhibitors for these targets. Enozertinib has shown strong anti-tumor activity in EGFR-driven intracranial lung cancer and HER2-positive breast cancer models. Its mechanism involves blocking EGFR and HER2 signaling, particularly in tumors harboring exon 20 insertion or atypical EGFR mutations. It is currently in Phase 1b clinical trials for patients with advanced solid tumors, including non-small cell lung cancer (NSCLC) with EGFR or HER2 exon 20 mutations, atypical EGFR mutations, and HER2 amplifications. The generic (INN) name "enozertinib" has been officially approved by WHO for ORIC-114[2][4][6][8][15].

Brand names

enozertinib

Other names

ORIC-114ORIC114ORIC 114