Drug intelligence / Profile preview

chidamide + regorafenib

Development stage
Unknown
Lead developer
Akeso
Modality
Small Molecules
Administration
Oral
01

Overview

**Chidamide + regorafenib** is a combination of two small molecule antineoplastic agents under investigation for cancer therapy. **Chidamide** is a benzamide-based class I histone deacetylase (HDAC) inhibitor, which modulates gene expression and remodels the tumor microenvironment to reduce immunosuppressive cells and enhance T-cell activation[5][4]. **Regorafenib** is a multi-kinase inhibitor that primarily targets vascular endothelial growth factor receptors (VEGFR), among other tyrosine kinases, suppressing tumor growth and angiogenesis[2][5]. The combination is intended to synergistically enhance efficacy: chidamide’s epigenetic modulation may potentiate regorafenib’s anti-angiogenic and anti-tumor activities, while together they can heighten anti-tumor immune responses, as preclinical and early phase clinical data in hepatocellular carcinoma and colorectal cancer suggest improved objective response rate and overall survival[2][5][4].

02

Targets

HDAC11 (Histone Deacetylase 11)BRAF (B-Raf proto-oncogene, serine/threonine kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)VEGFR2 (Vascular endothelial growth factor receptor 2)FGFR1 (Fibroblast growth factor receptor 1)HDAC10 (Histone Deacetylase 10)HDAC1 (Histone Deacetylase 1)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))HDAC8 (Histone Deacetylase 8)VEGFR-1 (Vascular endothelial growth factor receptor 1)TEK (Tie2)VEGFR3 (Vascular endothelial growth factor receptor 3)RET (Rearranged during transfection receptor tyrosine kinase)

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