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Entinostat for the treatment of breast cancer.

Abstract Breast cancer accounts for 29% of malignant tumors. It is an heterogenous disease covering a spectrum of different molecular subtypes. Epigenetic aberrations may affect gene expression through DNA and histone proteins modifications thus promoting tumor progression and resistance to anti- tumor treatment. Area covered: This article explores the potential role of entinostat in the treatment of breast cancer. The clinical trials evaluating entinostat are discussed, highlighting preclinical data and early-phase clinical studies results. The emerging activity of entinostat in several clinical settings is evaluated by focusing on endocrine-resistant, HER2 positive and triple-negative breast cancer with promising activity in boosting the immune-system. Expert opinion: Entinostat, a synthetic benzamide derivative class I histone deacetylases (HDACs) inhibitor, inhibits cell proliferation and promotes apoptosis in breast cancer. Several results from clinical trials demonstrate that the addition of an epigenetic therapy to antiestrogen therapy may be an effective approach to targeting resistance pathways in breast cancer, particularly in hormone-positive disease. Agents such as entinostat may have a role in immunogenic modulation. Genetic and pharmacological inhibition studies identified HDAC as a key determinant in the reversal of carcinoma immune escape. This offers the rationale for combining HDAC inhibitors with immunotherapy, including therapeutic cancer vaccines.
PMID
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Authors

Mayor MeshTerms
Keywords

HDAC

endocrine- resistance

entinostat

epigenetic

Journal Title expert opinion on investigational drugs
Publication Year Start




PMID- 28718331
OWN - NLM
STAT- MEDLINE
DA  - 20170718
DCOM- 20170807
LR  - 20170807
IS  - 1744-7658 (Electronic)
IS  - 1354-3784 (Linking)
VI  - 26
IP  - 8
DP  - 2017 Aug
TI  - Entinostat for the treatment of breast cancer.
PG  - 965-971
LID - 10.1080/13543784.2017.1353077 [doi]
AB  - INTRODUCTION: Breast cancer accounts for 29% of malignant tumors. It is an
      heterogenous disease covering a spectrum of different molecular subtypes.
      Epigenetic aberrations may affect gene expression through DNA and histone
      proteins modifications thus promoting tumor progression and resistance to anti-
      tumor treatment. Area covered: This article explores the potential role of
      entinostat in the treatment of breast cancer. The clinical trials evaluating
      entinostat are discussed, highlighting preclinical data and early-phase clinical 
      studies results. The emerging activity of entinostat in several clinical settings
      is evaluated by focusing on endocrine-resistant, HER2 positive and
      triple-negative breast cancer with promising activity in boosting the
      immune-system. Expert opinion: Entinostat, a synthetic benzamide derivative class
      I histone deacetylases (HDACs) inhibitor, inhibits cell proliferation and
      promotes apoptosis in breast cancer. Several results from clinical trials
      demonstrate that the addition of an epigenetic therapy to antiestrogen therapy
      may be an effective approach to targeting resistance pathways in breast cancer,
      particularly in hormone-positive disease. Agents such as entinostat may have a
      role in immunogenic modulation. Genetic and pharmacological inhibition studies
      identified HDAC as a key determinant in the reversal of carcinoma immune escape. 
      This offers the rationale for combining HDAC inhibitors with immunotherapy,
      including therapeutic cancer vaccines.
FAU - Trapani, Dario
AU  - Trapani D
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
FAU - Esposito, Angela
AU  - Esposito A
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
FAU - Criscitiello, Carmen
AU  - Criscitiello C
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
FAU - Mazzarella, Luca
AU  - Mazzarella L
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
FAU - Locatelli, Marzia
AU  - Locatelli M
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
FAU - Minchella, Ida
AU  - Minchella I
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
FAU - Minucci, Saverio
AU  - Minucci S
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
AD  - b Department of Oncology and Hematology , University of Milan , Milan , Italy.
FAU - Curigliano, Giuseppe
AU  - Curigliano G
AD  - a Division of Early Drug Development , European Institute of Oncology , Milan ,
      Italy.
LA  - eng
PT  - Journal Article
PT  - Review
DEP - 20170724
PL  - England
TA  - Expert Opin Investig Drugs
JT  - Expert opinion on investigational drugs
JID - 9434197
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Benzamides)
RN  - 0 (Histone Deacetylase Inhibitors)
RN  - 0 (Pyridines)
RN  - 1ZNY4FKK9H (entinostat)
SB  - IM
MH  - Animals
MH  - Antineoplastic Agents/*administration & dosage/pharmacology
MH  - Apoptosis/drug effects
MH  - Benzamides/*administration & dosage/pharmacology
MH  - Breast Neoplasms/*drug therapy/genetics/immunology
MH  - Cell Proliferation/drug effects
MH  - Epigenesis, Genetic
MH  - Female
MH  - Gene Expression Regulation, Neoplastic
MH  - Histone Deacetylase Inhibitors/administration & dosage/pharmacology
MH  - Humans
MH  - Immunotherapy/methods
MH  - Pyridines/*administration & dosage/pharmacology
OTO - NOTNLM
OT  - HDAC
OT  - endocrine- resistance
OT  - entinostat
OT  - epigenetic
EDAT- 2017/07/19 06:00
MHDA- 2017/08/08 06:00
CRDT- 2017/07/19 06:00
AID - 10.1080/13543784.2017.1353077 [doi]
PST - ppublish
SO  - Expert Opin Investig Drugs. 2017 Aug;26(8):965-971. doi:
      10.1080/13543784.2017.1353077. Epub 2017 Jul 24.