VRN110755

VRN110755 is a brain-penetrant, next-generation, mutant-selective epidermal growth factor receptor (EGFR) inhibitor in clinical development for the treatment of non-small cell lung cancer (NSCLC) with EGFR mutations, especially those with resistance to first-line osimertinib and with brain metastases. It has shown potent in vitro and in vivo activity against common EGFR mutations (Del19, L858R), uncommon mutations, and resistance mutations including C797S. VRN110755 demonstrates selectivity for EGFR mutants over wild-type, has a long intracellular residence time, shows promising anti-tumor efficacy in both subcutaneous and intracranial models, and does not show the risk of hyperglycemia associated with IR/IGF1R inhibition. Clinical trials (Phase 1) investigating safety, pharmacokinetics, and early efficacy are ongoing or planned in Korea and Taiwan after voluntary withdrawal of a US IND. The drug is developed by Voronoi[1][2][3][5][7].