Entinostat

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Entinostat
Entinostat.png
Names
IUPAC name
Pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
Other names
SNDX-275; MS-275
Identifiers
209783-80-2 YesY
ChEMBL ChEMBL27759 N
ChemSpider 4111 N
Jmol-3D images Image
KEGG D09338 YesY
PubChem 4261
Properties
C21H20N4O3
Molar mass 376.4085
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
 N verify (what isYesY/N?)
Infobox references

Entinostat, also known as SNDX-275 and MS-275, is a benzamide histone deacetylase inhibitor undergoing clinical trials for treatment of various cancers.[1]

Entinostat inhibits class I HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, respectively.[2]

Clinical trials[edit]

There is an ongoing phase II trial studying the effect of entinostat on Hodgkin's lymphoma.[3] It is in other phase II trials for advanced breast cancer (in combination with aromatase inhibitors)[4] and for metastatic lung cancer (in combination with erlotinib).[5] As of September 2013, the Food and Drug Administration is working with the industry to design phase III clinical trials. They seek to evaluate the application of Entinostat for the reduction, or prevention of, treatment resistance to aromatase inhibitors in hormone receptor positive breast cancer.[6] Syndax pharmaceuticals currently holds the rights to Entinostat and recently received $26.6 million in funds to advance treatments of resistant cancers using epigenetic tools.[7]

References[edit]