Drug Details

General Information of the Drug (ID: DR0366)
Name
Belinostat
Synonyms
Belinostat; 414864-00-9; PXD101; Belinostat (PXD101); 866323-14-0; Beleodaq; PXD-101; (E)-N-hydroxy-3-(3-(N-phenylsulfamoyl)phenyl)acrylamide; NSC726630; N-HYDROXY-3-(3-PHENYLSULFAMOYLPHENYL)ACRYLAMIDE; PXD 101; UNII-F4H96P17NZ; PX-105684; N-HYDROXY-3-[3-[(PHENYLAMINO)SULFONYL]PHENYL]-2-PROPENAMIDE; 2-Propenamide, N-hydroxy-3-[3-[(phenylamino)sulfonyl]phenyl]-, (2E)-; F4H96P17NZ; (2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide; CHEBI:61076; PX 105684; (2E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]acrylamide; (E)-N-hydroxy-3-[3-(phenylsulfamoyl)phenyl]prop-2-enamide.; E-Belinostat; Belinostat [USAN:INN]; N-hydroxy-3-(3-(phenylsulfamoyl)phenyl)prop-2-enamide; PX105684; 2-Propenamide, N-hydroxy-3-(3-((phenylamino)sulfonyl)phenyl)-, (2E)-; Belinostat Ph3; Beleodaq (TN); PubChem22405; Belinostat - PXD101; Belinostat (USAN/INN); Belinostat (PXD101); N-Hydroxy-3-(3-phenylsulphamoylphenyl)acrylamide; cc-489; MLS006011091; CHEMBL408513; GTPL7496; BDBM25150; CHEBI:94531; AMY1792; DTXSID60194378; EX-A180; QCR-181; (E)-3-[3-(phenylsulfamoyl)phenyl]prop-2-enehydroxamic acid; BCPP000351; AOB87787; BCP01741; ZINC3818726; Belinostat,PXD101, PX105684; Belinostat/PXD101,PX105684/; ABP000140; MFCD08064035; NSC758774; s1085; AKOS025401741; BCP9000386; CCG-208758; DB05015; LS41098; NSC-726630; NSC-758774; SB16466; NCGC00263155-02; NCGC00263155-05; AC-25046; AS-17068; SMR004702879; AB0007889; SW219445-1; EC-000.2286; A25012; D08870; W-5363; J-523584; Q4882925; BRD-K17743125-001-01-9; N-Hydroxy-3-[(phenylamino)sulfonyl]-trans-cinnamamide; (E)-N-Hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide; 5OG
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Molecular Type
Small molecule
Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z] Phase 2 [1]
Structure
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2D MOL

3D MOL

ADMET Property
Clearance
The clearance of drug is 1240 mL/min
Half-life
The concentration or amount of drug in body reduced by one-half in 1.1 hours
Metabolism
The drug is metabolized via the hepatic UGT1A1
Unbound Fraction
The unbound fraction of drug in plasma is 0.06%
Vd
The volume of distribution (Vd) of drug is 409 +/- 76.7 L
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Formula
C15H14N2O4S
PubChem CID
6918638
Canonical SMILES
C1=CC=C(C=C1)NS(=O)(=O)C2=CC=CC(=C2)C=CC(=O)NO
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+
InChIKey
NCNRHFGMJRPRSK-MDZDMXLPSA-N
CAS Number
CAS 866323-14-0
ChEBI ID
CHEBI:61076
TTD Drug ID
D0XT6W
DrugBank ID
DB05015
Combinatorial Therapeutic Effect(s) Validated Clinically or Experimentally
    α. A List of Natural Product(s) Able to Enhance the Efficacy of This Drug
          Vincristine      Catharanthus roseus     Click to Show/Hide the Molecular Data of This NP
                 Achieving Therapeutic Synergy     Click to Show/Hide
                    Representative Experiment Reporting the Effect of This Combination [2]
                    Detail(s)  Combination Info  click to show the detail info of this combination
                    Molecule(s)
                    Regulation		 Up-regulation Expression BCL2L11  Molecule Info 
Pathway MAP
Down-regulation Expression MCL1  Molecule Info 
Pathway MAP
                    In-vitro Model SU-DHL-4 CVCL_0539 B-cell lymphoma Homo sapiens
DB CVCL_1168 B-cell lymphoma Homo sapiens
OCI-Ly19 CVCL_1878 B-cell lymphoma Homo sapiens
SU-DHL-8 CVCL_2207 B-cell lymphoma Homo sapiens
GM18564 CVCL_P179 Healthy Homo sapiens
                    Experimental
                    Result(s)		 Vincristine sensitizes DLBCL cells to the cytotoxic effects of belinostat.
Target and Pathway
Target(s) Histone deacetylase (HDAC)  Molecule Info  [3]
References
Reference 1 A Phase II trial of Belinostat (PXD101) in patients with relapsed or refractory peripheral or cutaneous T-cell lymphoma. Br J Haematol. 2015 Mar;168(6):811-9.
Reference 2 Belinostat and vincristine demonstrate mutually synergistic cytotoxicity associated with mitotic arrest and inhibition of polyploidy in a preclinical model of aggressive diffuse large B cell lymphoma. Cancer Biol Ther. 2016 Dec;17(12):1240-1252.
Reference 3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
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