Drug intelligence / Profile preview

fruquintinib + sintilimab + chidamide

Development stage
Phase 2
Lead developer
Innovent Biologics
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

This drug refers to the experimental combination of three agents: **fruquintinib**, **sintilimab**, and **chidamide**. **Fruquintinib** is a highly selective small molecule inhibitor targeting vascular endothelial growth factor receptors (VEGFR) 1, 2, and 3, inhibiting angiogenesis in tumors. **Sintilimab** is a human anti–PD-1 monoclonal antibody that binds to the programmed cell death protein 1 (PD-1) receptor, blocking its interaction with PD-L1 and PD-L2, and thereby promoting T-cell mediated anti-tumor immunity. **Chidamide** is an oral, subtype-selective histone deacetylase (HDAC) inhibitor, acting predominantly on class I HDAC subtypes 1, 2, 3, and class IIb subtype 10, resulting in epigenetic modulation, increased acetylation of histones, altered gene expression, and induction of cell cycle arrest and apoptosis in tumor cells.

02

Targets

FGFR1 (Fibroblast growth factor receptor 1)HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)PDCD1 (Programmed cell death protein 1 receptor)RET (Rearranged during transfection receptor tyrosine kinase)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)KIT (c-KIT proto-oncogene receptor tyrosine kinase)

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