Drug intelligence / Profile preview

chiauranib + chidamide

Development stage
Phase 2
Lead developer
Akeso
Modality
Small Molecules
Administration
Oral
01

Overview

Chiauranib + chidamide is an investigational oral combination therapy consisting of two small-molecule agents: chiauranib, a multi-targeted kinase inhibitor, and chidamide, a selective histone deacetylase inhibitor. Chiauranib targets and inhibits multiple kinases, including Aurora kinase B (AURKB), colony-stimulating factor 1 receptor (CSF-1R), vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR), and c-Kit receptor, thereby disrupting mitosis, angiogenesis, and inflammatory processes within tumors. Chidamide (also known as tucidinostat) selectively inhibits histone deacetylase subtypes (notably HDAC1, 2, 3, and 10), leading to epigenetic reprogramming, increased tumor cell apoptosis, cell cycle arrest, and modulation of the tumor microenvironment. Preclinical evidence and early clinical data show that the combination produces synergistic antitumor effects, enhancing efficacy over either agent alone, by both inhibiting key tumorigenic pathways and improving immune-mediated antitumor responses. The combination is under investigation for advanced or refractory solid tumors, with ongoing clinical trials examining its pharmacokinetics, efficacy, and safety in various cancer types[2][3].

02

Targets

AURKB (Aurora kinase B)CSF1R (Macrophage colony-stimulating factor receptor)HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC11 (Histone Deacetylase 11)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC8 (Histone Deacetylase 8)KIT (c-KIT proto-oncogene receptor tyrosine kinase)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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