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词条 Belinostat
释义

  1. References

{{Infobox drug
| IUPAC_name = (2E)-N-Hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide
| image = Belinostat.svg
| alt =
| caption =
| tradename = Beleodaq
| Drugs.com = {{Drugs.com|parent|beleodaq}}
| MedlinePlus =
| pregnancy_AU =
| pregnancy_US = D
| pregnancy_category =
| legal_AU =
| legal_CA =
| legal_UK =
| legal_US = Rx-only
| legal_status =
| routes_of_administration = Intravenous (IV)
| bioavailability = 100% (IV)
| protein_bound = 92.9–95.8%[1]
| metabolism = UGT1A1
| onset =
| elimination_half-life =
| excretion = Urine
| CAS_number = 866323-14-0
| CAS_number_Ref = {{cascite|changed|??}}
| ATCvet =
| ATC_prefix = L01
| ATC_suffix = XX49
| PubChem = 6918638
| DrugBank =
| ChemSpiderID = 5293831
| ChemSpiderID_Ref = {{chemspidercite|correct|chemspider}}
| UNII = F4H96P17NZ
| UNII_Ref = {{fdacite|correct|FDA}}
| ChEMBL = 408513
| ChEMBL_Ref = {{ebicite|correct|EBI}}
| ChEBI = 61076
| ChEBI_Ref = {{ebicite|correct|EBI}}
| synonyms = PXD101
| KEGG = D08870
| C=15|H=14|N=2|O=4|S=1
| molecular_weight = 318.348 g/mol
| smiles = O=S(=O)(Nc1ccccc1)c2cc(\\C=C\\C(=O)NO)ccc2
| StdInChI_Ref = {{stdinchicite|correct|chemspider}}
| 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_Ref = {{stdinchicite|correct|chemspider}}
| 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.[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.[3] Final results in late 2009 of a phase II trial for T-cell lymphoma were encouraging.[4]

Belinostat has been granted orphan drug and fast track designation by the FDA,[5] and was approved in the US for the use against peripheral T-cell lymphoma on 3 July 2014.[6] It is not approved in Europe {{as of|2014|8|lc=on}}.[7]

The approved pharmaceutical formulation is given intravenously.[8]{{rp|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]{{rp|179 and 181}}

References

1. ^{{cite web|title=Beleodaq (belinostat) For Injection, For Intravenous Administration. Full Prescribing Information|url=http://www.beleodaq.com/downloads/Final_Beleodaq_PI.pdf|publisher=Spectrum Pharmaceuticals, Inc. Irvine, CA 92618|accessdate=21 November 2015}}
2. ^{{Cite journal |author1=Plumb JA |author2=Finn PW |author3=Williams RJ |display-authors=etal | title = Pharmacodynamic Response and Inhibition of Growth of Human Tumor Xenografts by the Novel Histone Deacetylase Inhibitor PXD101 | journal = Molecular Cancer Therapeutics | year = 2003 | volume = 2 | issue = 8 | pages = 721–728 | pmid = 12939461}}
3. ^{{cite news |url=http://www.biospace.com/news_story.aspx?NewsEntityId=75000 |title=CuraGen Corporation (CRGN) and TopoTarget A/S Announce Presentation of Belinostat Clinical Trial Results at AACR-NCI-EORTC International Conference |date=October 2007}}
4. ^{{citation |url=http://ash.confex.com/ash/2009/webprogram/Paper20945.html |title= Final Results of a Phase II Trial of Belinostat (PXD101) in Patients with Recurrent or Refractory Peripheral or Cutaneous T-Cell Lymphoma |date=December 2009}}
5. ^{{cite news |url=http://www.fiercebiotech.com/story/spectrum-adds-cancer-pipeline-350m-deal/2010-02-02#ixzz0fBunZz8B |title=Spectrum adds to cancer pipeline with $350M deal. |date=February 2010}}
6. ^{{cite news|url=http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm403929.htm|publisher=FDA|title=FDA approves Beleodaq to treat rare, aggressive form of non-Hodgkin lymphoma|date=3 July 2014}}
7. ^{{cite journal | author = H. Spreitzer | date = 4 August 2014 | title = Neue Wirkstoffe – Belinostat | journal = Österreichische Apothekerzeitung | issue = 16/2014 | pages = 27 | language = German }}
8. ^{{cite book |last1=Lexicomp |first1= (corporate author) |editor-last=Bragalone |editor-first=DL |edition=14th|title=Drug Information Handbook for Oncology|publisher=Wolters Kluwer |date=2016 |isbn=9781591953517 }}
{{Intracellular chemotherapeutic agents}}{{HDAC inhibitors}}{{antineoplastic-drug-stub}}

4 : Acrylamides|Histone deacetylase inhibitors|Sulfonamides|Hydroxamic acids

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