Drug intelligence / Profile preview

entinostat + sorafenib

Development stage: Phase 1
Lead developer: National Cancer Institute
Modality: Small Molecules
Administration: Oral

Overview

Entinostat + sorafenib is a combination therapy consisting of entinostat, a selective histone deacetylase (HDAC) inhibitor, and sorafenib, a multikinase inhibitor. This combination was developed based on preclinical data demonstrating cytotoxic synergy between the two agents. Entinostat selectively inhibits class I HDACs (particularly HDAC1, HDAC2, and HDAC3), which are involved in gene expression regulation, while sorafenib targets multiple kinases involved in tumor growth and angiogenesis, including VEGFR, PDGFR, and RAF kinases.

Targets

HDAC (HDAC family)FLT3 (Fms related receptor tyrosine kinase 3)PDGFRB (Platelet-derived growth factor receptor beta)RAF1 (c-Raf-1 (Y340D/Y341D))VEGFR2 (Vascular endothelial growth factor receptor 2)VEGFR4 (Vascular endothelial growth factor Receptor-3)

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