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sorafenib + valproic acid
- Development stage
- Phase 1
- Lead developer
- Bayer Pharmaceuticals
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Sorafenib + valproic acid is a drug combination being investigated for the treatment of high-grade glioma, including glioblastoma. This combination works through complementary mechanisms of action. Sorafenib is a multikinase inhibitor that blocks enzymes needed for tumor cell growth. Valproic acid functions as a histone deacetylase (HDAC) inhibitor, which enhances sorafenib's activity. In clinical trials, this combination is often administered with sildenafil citrate, which blocks ABCB1 and ABCG2 drug efflux pumps, potentially increasing sorafenib concentration in the brain by preventing its efflux at the blood-brain barrier.[1][4]
02
Targets
HTR2A (Serotonin receptor 5-HT2A)BRAF V600EFGFR1 (Fibroblast growth factor receptor 1)FLT3 (Fms related receptor tyrosine kinase 3)HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)HDAC4HDAC5 (Histone deacetylase 5)HDAC7PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))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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