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, broadly active mutation-selective EGFR inhibitor that targets both classical (exon 19 deletion and L858R) and uncommon EGFR mutations, including exon 20 insertion mutations as well as HER2 exon 20 insertion mutations. Furmonertinib is approved in China as an anticancer therapy for patients with NSCLC who have an EGFR T790M mutation, and more recently, as a first-line treatment in patients with NSCLC who have classical EGFR mutations. Furmonertinib is being developed in China by Allist Pharmaceuticals and in the rest of the world by ArriVent Biopharma.
ArriVent is studying furmonertinib globally in patients with NSCLC with EGFR mutations and HER2 Exon 20 insertion mutations.