Belinostat Explained

Iupac Name:(2E)-N-Hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
Tradename:Beleodaq
Pregnancy Us:D
Legal Us:Rx-only
Routes Of Administration:Intravenous (IV)
Bioavailability:100% (IV)
Protein Bound:92.9–95.8%[1]
Metabolism:UGT1A1
Excretion:Urine
Cas Number:866323-14-0
Atc Prefix:L01
Atc Suffix:XH04
Pubchem:6918638
Chemspiderid:5293831
Unii:F4H96P17NZ
Chembl:408513
Chebi:61076
Synonyms:PXD101
Kegg:D08870
C:15
H:14
N:2
O:4
S:1
Smiles:O=S(=O)(Nc1ccccc1)c2cc(\C=C\C(=O)NO)ccc2
Stdinchi: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+
Stdinchikey: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.

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.[3] 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,[4] and was approved in the US for the use against peripheral T-cell lymphoma on 3 July 2014.[5] It is not approved in Europe .[6]

The approved pharmaceutical formulation is given intravenously.[7] 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.[7]

Notes and References

  1. Web site: Beleodaq (belinostat) For Injection, For Intravenous Administration. Full Prescribing Information. Spectrum Pharmaceuticals, Inc. Irvine, CA 92618. 21 November 2015. 4 March 2016. https://web.archive.org/web/20160304070024/http://www.beleodaq.com/downloads/Final_Beleodaq_PI.pdf. dead.
  2. Plumb JA, Finn PW, Williams RJ, Bandara MJ, Romero MR, Watkins CJ, La Thangue NB, Brown R . 6 . Pharmacodynamic response and inhibition of growth of human tumor xenografts by the novel histone deacetylase inhibitor PXD101 . Molecular Cancer Therapeutics . 2 . 8 . 721–8 . August 2003 . 12939461 .
  3. News: CuraGen Corporation (CRGN) and TopoTarget A/S Announce Presentation of Belinostat Clinical Trial Results at AACR-NCI-EORTC International Conference . October 2007 . 2011-12-06 . https://web.archive.org/web/20110716091452/http://www.biospace.com/news_story.aspx?NewsEntityId=75000 . 2011-07-16 . dead .
  4. News: John . Carroll . vanc . Fierce Biotech . Spectrum adds to cancer pipeline with $350M deal. . 2 February 2010 .
  5. News: FDA approves Beleodaq to treat rare, aggressive form of non-Hodgkin lymphoma. FDA. 3 July 2014.
  6. Spreitzer H . 4 August 2014 . Neue Wirkstoffe – Belinostat . Österreichische Apothekerzeitung . 16/2014 . 27 . German .
  7. Book: Bragalone DL, ((American Pharmacists Association)), ((Lexi-Comp, Inc.)) . 14th . Drug Information Handbook for Oncology . Wolters Kluwer . 2016 . 9781591953517 .