Enozertinib (ORIC-114) is a potent, brain penetrant, orally bioavailable, irreversible inhibitor of exon 20 insertions in EGFR and HER2.
ORIC-114 is highly selective for the EGFR family of receptors, with excellent kinome selectivity compared to other reported exon 20 inhibitors, reducing the risk of off-target kinase liabilities.
ORIC-114 administration (3 mg/kg, once daily oral) induced robust tumor regressions with greater than 100% tumor growth inhibition in the absence of significant body weight loss in an EGFR exon 20 insertion H773_V774insNPH NSCLC PDX model.
