Entinostat

Entinostat
IUPAC name

Pyridin-3-ylmethyl N-[[4-[(2-aminophenyl)carbamoyl]phenyl]methyl]carbamate
Other names

SNDX-275; MS-275
Identifiers
CAS number 209783-80-2 Y
PubChem 4261
KEGG D09338 Y
ChEMBL CHEMBL27759 N
Jmol-3D images Image 1
Properties
Molecular formula C21H20N4O3
Molar mass 376.4085
 N (verify) (what is: Y/N?)
Except where noted otherwise, data are given for materials in their standard state (at 25 °C, 100 kPa)
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

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].

References

  1. ^ Phase I trial of 5-azacitidine (5AC) and SNDX-275 in advanced lung cancer (NSCLC)
  2. ^ Novel Sulphonylpyrroles as Inhibitors of Hdac S Novel Sulphonylpyrroles
  3. ^ A Phase 2 Multi-Center Study of Entinostat (SNDX-275) in Patient With Relapsed or Refractory Hodgkin's Lymphoma
  4. ^ A Phase 2, Multicenter Study of the Effect of the Addition of SNDX-275 to Continued Aromatase Inhibitor (AI) Therapy in Postmenopausal Women With ER+ Breast Cancer Whose Disease is Progressing
  5. ^ A Phase 2 Exploratory Study of Erlotinib and SNDX-275 in Patients With Non-small Cell Lung Carcinoma Who Are Progressing on Erlotinib