Belinostat

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Belinostat
Belinostat.svg
Clinical data
Trade namesBeleodaq
SynonymsPXD101
AHFS/Drugs.combeleodaq
Pregnancy
category
  • US: D (Evidence of risk)
Routes of
administration
Intravenous (IV)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability100% (IV)
Protein binding92.9–95.8%[1]
MetabolismUGT1A1
ExcretionUrine
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC15H14N2O4S
Molar mass318.348 g/mol
3D model (JSmol)

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[edit]

  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.
  3. ^ a b "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.
  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.
  7. ^ H. Spreitzer (4 August 2014). "Neue Wirkstoffe – Belinostat". Österreichische Apothekerzeitung (in German) (16/2014): 27.
  8. ^ a b Lexicomp, (corporate author) (2016). Bragalone, DL, ed. Drug Information Handbook for Oncology (14th ed.). Wolters Kluwer. ISBN 9781591953517.