ZZC4

ZZC4 is a novel, covalent purine-containing small molecule inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase. Currently in preclinical development, ZZC4 is designed to address acquired resistance to first-generation (gefitinib) and third-generation (osimertinib) EGFR tyrosine kinase inhibitors (TKIs) in non-small cell lung cancer (NSCLC). The compound exerts its anticancer effects by binding covalently to the EGFR kinase domain, thereby potently suppressing downstream signaling through the PI3K/Akt and MAPK pathways. This inhibition leads to cell cycle arrest and apoptosis, characterized by the upregulation of CDKN1B and the downregulation of CCNA2 and CHEK1. Preclinical studies have demonstrated that ZZC4 significantly inhibits the proliferation of lung, breast, and melanoma cell lines and exhibits robust anti-tumor efficacy in xenograft mouse models.

Other names

covalent purine-containing EGFR TKI