biphenyl isoxazolidine

Biphenyl isoxazolidine is a novel small-molecule inhibitor of epithelial-restricted with serine box (ESX). It functions by reducing the levels of epidermal growth factor receptor (EGFR) and human epidermal growth factor receptor 2 (Her2). This action potentiates the antiproliferative efficacy of afatinib, an EGFR/Her2 tyrosine kinase inhibitor, particularly in head and neck squamous cell carcinoma (HNSCC). In preclinical studies, biphenyl isoxazolidine alone retarded in vivo tumorigenicity, and in combination with afatinib, it showed significantly superior results, leading to a 100% response rate and a 94% reduction in tumor volume in CAL27 cells.