Belinostat

Belinostat
Names
Trade namesBeleodaq
Other namesPXD101
IUPAC name
  • (2E)-N-Hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
Clinical data
Drug classHistone deacetylase inhibitor[1]
Main usesPeripheral T-cell lymphoma (PTCL)[1]
Side effectsNausea, tiredness, fever, low red blood cells[2]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • US: D (Evidence of risk)
    Routes of
    use    		Intravenous (IV)
    External links
    AHFS/Drugs.comMonograph
    Legal
    Legal status
    Pharmacokinetics
    Bioavailability100% (IV)
    Protein binding92.9–95.8%[3]
    MetabolismUGT1A1
    ExcretionUrine
    Chemical and physical data
    FormulaC15H14N2O4S
    Molar mass318.35 g·mol−1
    3D model (JSmol)
    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+ checkY
    • Key:NCNRHFGMJRPRSK-MDZDMXLPSA-N checkY

    Belinostat, sold under the brand name Beleodaq, is a medication used to treat peripheral T-cell lymphoma (PTCL).[1] It is used when other treatments have failed.[2] Regarding if it improves life expectancy is unclear as of 2020.[2] It is given by injection into a vein.[1]

    Common side effects include nausea, tiredness, fever, and low red blood cells.[2] Other side effects may include low platelets, low white blood cells, infection, liver problems, and tumor lysis syndrome.[2] Use in pregnancy may harm the baby.[2] It is a histone deacetylase inhibitor.[1]

    Belinostat was approved for medical use in the United States in 2014.[2] It was given an orphan designation in Europe in 2012.[4] In the United States a vial of 500 mg costs about 2,100 USD as of 2022.[5]

    Medical uses

    Dosage

    It is given at a dose of 1,000 mg/m2 once a day on days 1-5 out of a 21-day cycle.[2]

    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.[6]: 179 and 181 

    History

    Belinostat has been granted orphan drug and fast track designation by the FDA,[7] and was approved in the US for the use against peripheral T-cell lymphoma on 3 July 2014.[8]

    It is not approved in Europe as of August 2014.[9]

    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.[10] Final results in late 2009 of a phase II trial for T-cell lymphoma were encouraging.[11]

    References

    1. 1 2 3 4 5 "Belinostat Monograph for Professionals". Drugs.com. Retrieved 8 January 2022.
    2. 1 2 3 4 5 6 7 8 "DailyMed - BELEODAQ- belinostat injection, powder, lyophilized, for solution". dailymed.nlm.nih.gov. Archived from the original on 25 March 2021. Retrieved 8 January 2022.
    3. ↑ "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.
    4. ↑ "EU/3/12/1055: Orphan designation for the treatment of peripheral T-cell lymphoma (nodal, other extranodal and leukaemic/disseminated)". Archived from the original on 11 January 2022. Retrieved 8 January 2022.
    5. ↑ "Belinostat Prices, Coupons & Savings Tips - GoodRx". GoodRx. Retrieved 8 January 2022.
    6. ↑ Bragalone DL, American Pharmacists Association, Lexi-Comp, Inc. (2016). Drug Information Handbook for Oncology (14th ed.). Wolters Kluwer. ISBN 9781591953517.
    7. ↑ Carroll J (2 February 2010). "Spectrum adds to cancer pipeline with $350M deal". Fierce Biotech. Archived from the original on 2016-03-03. Retrieved 2021-05-25.
    8. ↑ "FDA approves Beleodaq to treat rare, aggressive form of non-Hodgkin lymphoma". FDA. 3 July 2014. Archived from the original on 18 January 2017. Retrieved 25 May 2021.
    9. ↑ Spreitzer H (4 August 2014). "Neue Wirkstoffe – Belinostat". Österreichische Apothekerzeitung (in German) (16/2014): 27.{{cite journal}}: CS1 maint: unrecognized language (link)
    10. ↑ "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.
    11. ↑ Final Results of a Phase II Trial of Belinostat (PXD101) in Patients with Recurrent or Refractory Peripheral or Cutaneous T-Cell Lymphoma, December 2009, archived from the original on 2011-07-26, retrieved 2021-05-25
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