Chiauranib (Ibcasertib): A Comprehensive Monograph on a Novel Triple-Pathway Kinase Inhibitor

Executive Summary

Chiauranib, also known by its proposed International Nonproprietary Name (INN) Ibcasertib and developmental code CS-2164, is an orally administered, investigational small molecule antineoplastic agent representing a novel approach to cancer therapy.[1] It is a new chemical entity originally designed and developed by the Chinese biopharmaceutical firm Shenzhen Chipscreen Biosciences, which holds its global patent protection.[4] The core innovation of Chiauranib lies in its unique and synergistic triple-pathway mechanism of action, which is engineered to simultaneously attack three distinct hallmarks of cancer: tumor angiogenesis, unregulated cell mitosis, and the immunosuppressive tumor microenvironment.[4] This multi-pronged strategy distinguishes it from many single-target tyrosine kinase inhibitors (TKIs) and is intended to overcome the therapeutic limitations and resistance mechanisms often associated with more narrowly focused agents.[8]

At the molecular level, Chiauranib functions as a high-potency inhibitor of several key protein kinases. It demonstrates inhibitory concentrations in the half-maximal range () within the single-digit nanomolar scale against its primary targets.[9] These targets include: 1) angiogenesis-related kinases such as vascular endothelial growth factor receptors (VEGFRs) and platelet-derived growth factor receptors (PDGFRs); 2) the mitosis-related serine/threonine kinase Aurora B; and 3) the chronic inflammation-related kinase, colony-stimulating factor 1 receptor (CSF-1R).[1] Preclinical studies have underscored the high selectivity of Chiauranib, with minimal activity against a wide panel of off-target kinases and proteins, suggesting a potentially favorable safety profile.[9]