Belinostat

Belinostat
Clinical data
Trade names	Beleodaq
Other names	PXD101
AHFS/Drugs.com	beleodaq
Pregnancy; category	US: D (Evidence of risk) ;
Routes of; administration	Intravenous (IV)
ATC code	L01XX49 (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 ;
PubChem CID	6918638;
ChemSpider	5293831 ;
UNII	F4H96P17NZ;
KEGG	D08870;
ChEBI	CHEBI:61076 ;
ChEMBL	ChEMBL408513 ;
CompTox Dashboard (EPA)	DTXSID60194378 ;
Chemical and physical data
Formula	C15H14N2O4S
Molar mass	318.348 g/mol 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+ ; Key:NCNRHFGMJRPRSK-MDZDMXLPSA-N ;

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]

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.[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}

References

"Beleodaq (belinostat) For Injection, For Intravenous Administration. Full Prescribing Information" (PDF). Spectrum Pharmaceuticals, Inc. Irvine, CA 92618. Retrieved 21 November 2015.
Plumb JA; Finn PW; Williams RJ; et al. (2003). "Pharmacodynamic Response and Inhibition of Growth of Human Tumor Xenografts by the Novel Histone Deacetylase Inhibitor PXD101". Molecular Cancer Therapeutics. 2 (8): 721–728. PMID 12939461.
"FDA approves Beleodaq to treat rare, aggressive form of non-Hodgkin lymphoma". FDA. 3 July 2014.
"CuraGen Corporation (CRGN) and TopoTarget A/S Announce Presentation of Belinostat Clinical Trial Results at AACR-NCI-EORTC International Conference". October 2007. Archived from the original on 2011-07-16. Retrieved 2011-12-06.
Final Results of a Phase II Trial of Belinostat (PXD101) in Patients with Recurrent or Refractory Peripheral or Cutaneous T-Cell Lymphoma, December 2009
"Spectrum adds to cancer pipeline with $350M deal". February 2010.
H. Spreitzer (4 August 2014). "Neue Wirkstoffe – Belinostat". Österreichische Apothekerzeitung (in German) (16/2014): 27.
Lexicomp, (corporate author) (2016). Bragalone, DL (ed.). Drug Information Handbook for Oncology (14th ed.). Wolters Kluwer. ISBN 9781591953517.

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[1] "Beleodaq (belinostat) For Injection, For Intravenous Administration. Full Prescribing Information" (PDF). Spectrum Pharmaceuticals, Inc. Irvine, CA 92618. Retrieved 21 November 2015.

[2] Plumb JA; Finn PW; Williams RJ; et al. (2003). "Pharmacodynamic Response and Inhibition of Growth of Human Tumor Xenografts by the Novel Histone Deacetylase Inhibitor PXD101". Molecular Cancer Therapeutics. 2 (8): 721–728. PMID 12939461.

[FDA-2014-3] "FDA approves Beleodaq to treat rare, aggressive form of non-Hodgkin lymphoma". FDA. 3 July 2014.

[4] "CuraGen Corporation (CRGN) and TopoTarget A/S Announce Presentation of Belinostat Clinical Trial Results at AACR-NCI-EORTC International Conference". October 2007. Archived from the original on 2011-07-16. Retrieved 2011-12-06.

[5] Final Results of a Phase II Trial of Belinostat (PXD101) in Patients with Recurrent or Refractory Peripheral or Cutaneous T-Cell Lymphoma, December 2009

[6] "Spectrum adds to cancer pipeline with $350M deal". February 2010.

[Spreitzer-7] H. Spreitzer (4 August 2014). "Neue Wirkstoffe – Belinostat". Österreichische Apothekerzeitung (in German) (16/2014): 27.

[DIHO_2016_14-8] Lexicomp, (corporate author) (2016). Bragalone, DL (ed.). Drug Information Handbook for Oncology (14th ed.). Wolters Kluwer. ISBN 9781591953517.