Belinostat

Belinostat

Systematic (IUPAC) name
(2E)-N-Hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
Clinical data
Trade names	Beleodaq
AHFS/Drugs.com	entry
Pregnancy category	US: D (Evidence of risk)
Legal status	US: ℞-only
Routes of administration	Intravenous (IV)
Pharmacokinetic data
Bioavailability	100% (IV)
Protein binding	92.9–95.8%
Metabolism	UGT1A1
Excretion	Urine
Identifiers
CAS Number	866323-14-0 N
ATC code	L01XX49 (WHO)
PubChem	CID: 6918638
ChemSpider	5293831 Y
UNII	F4H96P17NZ Y
ChEBI	CHEBI:61076 Y
ChEMBL	CHEMBL408513 Y
Synonyms	PXD101
Chemical data
Formula	C15H14N2O4S
Molecular mass	318.348 g/mol
SMILES O=S(=O)(Nc1ccccc1)c2cc(\C=C\C(=O)NO)ccc2
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+ Y Key:NCNRHFGMJRPRSK-MDZDMXLPSA-N Y

Belinostat (trade name Beleodaq, previously known as PXD101) is a histone deacetylase inhibitor drug developed by TopoTarget for the treatment of hematological malignancies and solid tumors.

It was approved in July 2014 by the US FDA to treat peripheral T-cell lymphoma.

In 2007 preliminary results were released from the Phase II clinical trial of intravenous belinostat in combination with carboplatin and paclitaxel for relapsed ovarian cancer. Final results in late 2009 of a phase II trial for T-cell lymphoma were encouraging. Belinostat has been granted orphan drug and fast track designation by the FDA, and was approved in the US for the use against peripheral T-cell lymphoma on 3 July 2014. It is not approved in Europe as of August 2014.

The approved pharmaceutical formulation is given intravenously. Belinostat is primarily metabolized by UGT1A1; the initial dose should be reduced if the recipient is known to be homozygous for the UGT1A1*28 allele.