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pazopanib + abexinostat
- Development stage
- Phase 3
- Lead developer
- Xynomic Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
A combination of **pazopanib**, a small molecule tyrosine kinase inhibitor of **VEGFR**, **PDGFR**, and **c-KIT**, with **abexinostat**, a small molecule **histone deacetylase (HDAC) inhibitor**. This regimen is being investigated for its capacity to enhance anti-tumor activity and reverse resistance to angiogenesis inhibitors in patients with advanced solid tumor malignancies, particularly *renal cell carcinoma (RCC)*. In clinical studies, this combination showed prolonged disease control and durable responses, even in patients previously refractory to VEGF inhibitors. **Pazopanib** inhibits the angiogenic signaling pathways, while **abexinostat** modulates gene expression via epigenetic regulation, downregulating hypoxia-inducible factor-1α (HIF-1α) and targeting HDAC2 to complement anti-angiogenic effects[1][2][5].
- Other names
- pazopanib + abexinostat
02
Targets
CSF1R (Macrophage colony-stimulating factor receptor)FGFR1 (Fibroblast growth factor receptor 1)FGFR3 (Fibroblast growth factor receptor 3)FLT3 (Fms related receptor tyrosine kinase 3)HDAC1 (Histone Deacetylase 1)HDAC10 (Histone Deacetylase 10)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC6 (Histone deacetylase 6)HDAC8 (Histone Deacetylase 8)ITK (Interleukin 2-inducible T-cell kinase)KIT (c-KIT proto-oncogene receptor tyrosine kinase)LCK (Proto-oncogene tyrosine-protein kinase Lck)PDGFRA (Platelet-derived growth factor receptor alpha)PDGFRB (Platelet-derived growth factor receptor beta)UGT1A1 (UDP-glucuronosyltransferase 1A1)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)HIF1A (Hypoxia-inducible factor 1-alpha)
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