belinostat   Click here for help

GtoPdb Ligand ID: 7496

Synonyms: Beleodaq® | PXD-101 | PXD101
Approved drug PDB Ligand
belinostat is an approved drug (FDA (2014))
Compound class: Synthetic organic
Comment: Belinostat is a pan-histone deacetylase (HDAC) inhibitor [1,3].
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 3
Rotatable bonds 6
Topological polar surface area 103.88
Molecular weight 318.07
XLogP 1.95
No. Lipinski's rules broken 0
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Canonical SMILES ONC(=O)C=Cc1cccc(c1)S(=O)(=O)Nc1ccccc1
Isomeric SMILES ONC(=O)/C=C/c1cccc(c1)S(=O)(=O)Nc1ccccc1
InChI InChI=1S/C15H14N2O4S/c18-15(16-19)10-9-12-5-4-8-14(11-12)22(20,21)17-13-6-2-1-3-7-13/h1-11,17,19H,(H,16,18)/b10-9+
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Summary of Clinical Use Click here for help
Belinostat was approved by the US FDA in 2014 for the treatment of patients with relapsed or refactory peripheral T-cell lymphoma (PTCL), a rare and fast-growing type of non-Hodgkin lymphoma (NHL). In the EU, belinostat has orphan designation to treat peripheral T-cell lymphoma (nodal, other extranodal and leukaemic / disseminated) and malignant thymoma.
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Belinostat is a hydroxamate-type HDAC inhibitor which induces apoptosis in vitro [2,4-6] thereby reducing tumour load. HDACs function as integral components of multi-protein complexes which are recruited to specific regions of the genome. These protein complexes control the expression and silencing (repression) of specific sets of genes which provides the basis for the reported phenotypes typical of malignant cancer cells. HDAC inhibition causes transcriptional de-repression of genes modulating growth inhibition, differentiation and apoptosis of cancer cells.
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