Belinostat

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.^[2]

Belinostat

Clinical data
Trade names	Beleodaq
Other names	PXD101
AHFS/Drugs.com	beleodaq
Routes of administration	Intravenous (IV)
ATC code	L01XH04 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Bioavailability	100% (IV)
Protein binding	92.9–95.8%[1]
Metabolism	UGT1A1
Excretion	Urine
Identifiers
IUPAC name (2E)-N-Hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
CAS Number	866323-14-0 N
PubChem CID	6918638
ChemSpider	5293831 Y
UNII	F4H96P17NZ
KEGG	D08870
ChEBI	CHEBI:61076 Y
ChEMBL	ChEMBL408513 Y
CompTox Dashboard (EPA)	DTXSID60194378
Chemical and physical data
Formula	C15H14N2O4S
Molar mass	318.35 g·mol−1
3D model (JSmol)	Interactive image
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

It was approved in July 2014 by the US FDA to treat peripheral T-cell lymphoma.^[3]

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.^[4] Final results in late 2009 of a phase II trial for T-cell lymphoma were encouraging.^[5]Belinostat has been granted orphan drug and fast track designation by the FDA,^[6] and was approved in the US for the use against peripheral T-cell lymphoma on 3 July 2014.^[3] It is not approved in Europe as of August 2014^[update].^[7]

The approved pharmaceutical formulation is given intravenously.^[8]: 180 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.^{[8]: 179 and 181}