BH-30643

BH-30643 is a novel, orally available, reversible, macrocyclic small molecule that acts as a mutant-selective OMNI-EGFR inhibitor. It is designed to potently inhibit a broad spectrum of activating and resistance mutations in the epidermal growth factor receptor (EGFR) kinase domain—including classical, atypical (uncommon/nonclassical), exon 20 insertions, and compound resistance mutations such as ex19del/T790M/C797S and L858R/T790M/C797S—as well as HER2 activating mutations. The drug demonstrates high potency against mutant EGFR and HER2 while sparing wild-type forms to reduce toxicity (notably skin rash). Its mechanism aims to address both primary oncogenic drivers in non-small cell lung cancer (NSCLC) and acquired resistance mechanisms following prior EGFR therapy. BH-30643 is currently being evaluated in the Phase 1/2 SOLARA clinical trial for patients with locally advanced or metastatic NSCLC harboring EGFR or HER2 mutations[1][2][3][5][7].

Other names

OMNI-EGFR inhibitor (investigational context)