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sunitinib + valproic acid
- Development stage
- Unknown
- Lead developer
- Thomas Jefferson University
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Sunitinib + valproic acid is a combination of two small-molecule drugs investigated primarily in oncology, including for the prevention of metastasis in uveal melanoma. Sunitinib is an oral, multi-targeted receptor tyrosine kinase (RTK) inhibitor that blocks signaling pathways involved in tumor growth and angiogenesis by inhibiting multiple RTKs such as platelet-derived growth factor receptors (PDGFRα/β), vascular endothelial growth factor receptors (VEGFR1/2/3), KIT, FLT3, CSF-1R, and RET. Valproic acid is an anticonvulsant with additional anti-proliferative effects; it increases GABAergic neurotransmission by inhibiting GABA transaminase and modulates gene expression through histone deacetylase inhibition. In cancer settings, valproic acid may alter gene expression to suppress tumor growth. The combination has been studied for its potential to prevent metastasis or recurrence in high-risk uveal melanoma patients[1][2][4].
- Other names
- sunitinib malateVPA
02
Targets
ABAT (4-aminobutyrate aminotransferase)NaV (Voltage-gated sodium channels)PDGFRA (Platelet-derived growth factor receptor alpha)KIT (c-KIT proto-oncogene receptor tyrosine kinase)CSF1R (Macrophage colony-stimulating factor receptor)PDGFRB (Platelet-derived growth factor receptor beta)HDAC (HDAC family)VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR-1 (Vascular endothelial growth factor receptor 1)VEGFR3 (Vascular endothelial growth factor receptor 3)CaV3 (Caveolin-3)FGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)
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