Belinostat

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Belinostat
Belinostat.svg
Names
Trade namesBeleodaq
Other namesPXD101
  • (2E)-N-Hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
Clinical data
Pregnancy
category
  • US: D (Evidence of risk)
Routes of
use
Intravenous (IV)
External links
AHFS/Drugs.combeleodaq
US NLMBelinostat
Legal
Legal status
Pharmacokinetics
Bioavailability100% (IV)
Protein binding92.9–95.8%[1]
MetabolismUGT1A1
ExcretionUrine
Chemical and physical data
FormulaC15H14N2O4S
Molar mass318.35 g·mol−1
3D model (JSmol)
  • O=S(=O)(Nc1ccccc1)c2cc(\C=C\C(=O)NO)ccc2
  • 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+ checkY
  • Key:NCNRHFGMJRPRSK-MDZDMXLPSA-N checkY

Belinostat, sold under the brand name Beleodaq, is a medication used to treat blood cancers and solid tumors.[2] It is used for peripheral T-cell lymphoma.[3] It is given by injection into a vein.[4]: 180 

It is a histone deacetylase inhibitor.

Belinostat was approved for medical use in the United States in 2014. It is not approved in Europe as of August 2014.[5]

Mechanism of action

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.[4]: 179 and 181 

History

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]

Research

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.[7] Final results in late 2009 of a phase II trial for T-cell lymphoma were encouraging.[8]

References

  1. "Beleodaq (belinostat) For Injection, For Intravenous Administration. Full Prescribing Information" (PDF). Spectrum Pharmaceuticals, Inc. Irvine, CA 92618. Archived from the original (PDF) on 4 March 2016. Retrieved 21 November 2015.
  2. Plumb JA, Finn PW, Williams RJ, Bandara MJ, Romero MR, Watkins CJ, et al. (August 2003). "Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101". Molecular Cancer Therapeutics. 2 (8): 721–8. PMID 12939461.
  3. 3.0 3.1 "FDA approves Beleodaq to treat rare, aggressive form of non-Hodgkin lymphoma". FDA. 3 July 2014.
  4. 4.0 4.1 Bragalone DL, American Pharmacists Association, Lexi-Comp, Inc. (2016). Drug Information Handbook for Oncology (14th ed.). Wolters Kluwer. ISBN 9781591953517.
  5. Spreitzer H (4 August 2014). "Neue Wirkstoffe – Belinostat". Österreichische Apothekerzeitung (in German) (16/2014): 27.CS1 maint: unrecognized language (link)
  6. Carroll J (2 February 2010). "Spectrum adds to cancer pipeline with $350M deal". Fierce Biotech.
  7. "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.
  8. Final Results of a Phase II Trial of Belinostat (PXD101) in Patients with Recurrent or Refractory Peripheral or Cutaneous T-Cell Lymphoma, December 2009

External links

Identifiers: