Drug intelligence / Profile preview

pazopanib + abexinostat

Development stage
Unknown
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

VEGFR2 (Vascular endothelial growth factor receptor 2)HDAC1 (Histone Deacetylase 1)UGT1A1 (UDP-glucuronosyltransferase 1A1)FLT3 (Fms related receptor tyrosine kinase 3)LCK (Proto-oncogene tyrosine-protein kinase Lck)KIT (c-KIT proto-oncogene receptor tyrosine kinase)ITK (Interleukin 2-inducible T-cell kinase)HDAC6 (Histone deacetylase 6)PDGFRB (Platelet-derived growth factor receptor beta)HDAC8 (Histone Deacetylase 8)FGFR1 (Fibroblast growth factor receptor 1)PDGFRA (Platelet-derived growth factor receptor alpha)CSF1R (Macrophage colony-stimulating factor receptor)HDAC10 (Histone Deacetylase 10)FGFR3 (Fibroblast growth factor receptor 3)VEGFR3 (Vascular endothelial growth factor receptor 3)VEGFR-1 (Vascular endothelial growth factor receptor 1)

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