abexinostat

Ligand id: 8366

Name: abexinostat

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 4
Hydrogen bond donors 3
Rotatable bonds 10
Topological polar surface area 104.04
Molecular weight 397.16
XLogP 2.33
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

No information available.
Summary of Clinical Use
Abexinostat is being assessed in Phase II clinical trials as a potential treatment for non-Hodgkin lymphoma or sarcoma (@ May 2015).
Mechanism Of Action and Pharmacodynamic Effects
HDAC inhibitors have shown clinical efficacy in AML, myelodysplastic syndrome and myeloproliferative neoplasms [3-4]. The HDAC inhibitor vorinostat was the first compound designed to inhibit HDACs to be approved for clinical use. HDAC inhibition increases acetylation of histone H3 and leads to downstream activation of the PI3K/Akt and MAPK/Ras signaling pathways and ultimately results in cell cycle arrest and apoptosis [2]. Mithraprabhu et al (2010) review the use of HDAC inhibitors in myeloproliferative neoplasms, and discuss the benefits of combination therapies with kinase inhibitors [3].