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]