Mutational activation of the epidermal growth factor receptor (EGFR) is a common and early event in the development of non-small cell lung cancer (NSCLC) and confers oncogene dependency on the growth and proliferation of cancer cells. EGFR activating mutations are present in approximately 15% of NSCLC. Patients with NSCLC containing EGFR activating mutations are also particularly prone to the development of brain metastases, with 50% to 60% developing central nervous system (CNS) metastases over the course of their disease. Despite initial clinical response to currently approved EGFR inhibitors, patients with advanced EGFR mutated NSCLC inevitably acquire resistance mechanisms and progress at some point during treatment; therefore, there is the need for more effective, tolerable treatments.
Furmonertinib is an oral, highly brain-penetrant, irreversible pan-EGFR mutant inhibitor designed by our partners Allist Pharmaceuticals in Shanghai, China to selectively target EGFR activating mutations including atypical EGFR mutations such as EGFR Exon 20 insertions. Furmonertinib also targets HER2 Exon20 insertion mutations present in approximately 1.5% of NSCLC. In a Phase 3 double blind, placebo-controlled study in 1L EGFR mutant NSCLC conducted in China, furmonertinib has demonstrated superiority over the 1st generation EGFR inhibitor gefitinib. Furmonertinib is also being studied in China in EGFR Exon 20 insertion mutant NSCLC with encouraging preliminary activity.
Building on the clinical data collected in China by Allist, ArriVent is studying furmonertinib globally in patients with EGFR mutant and HER2 Exon 20 insertion mutant NSCLC.