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Updated: Mar 5, 2026

Endobronchial Ultrasound-guided Intratumoral Injection of Cisplatin for the Treatment of Isolated Mediastinal Recurrence of Lung Cancer
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Entinostat: a promising treatment option for patients with advanced breast cancer

Roisin M Connolly1, Michelle A Rudek1, Richard Piekarz2

  • 1Sidney Kimmel Comprehensive Cancer Center, Johns Hopkins School of Medicine, Baltimore, MD, USA.

Future Oncology (London, England)
|March 23, 2017
PubMed

Insights

Entinostat, a histone deacetylase (HDAC) inhibitor, shows promise in advanced breast cancer treatment. Ongoing Phase III trials aim to confirm its survival benefits when combined with exemestane.

Area of Science:

  • Pharmacology
  • Oncology
  • Molecular Biology

Background:

  • Entinostat is a synthetic benzamide derivative and a potent, selective inhibitor of histone deacetylase (HDAC) class I and IV enzymes.
  • HDAC inhibition leads to histone hyperacetylation, transcriptional activation, and subsequent inhibition of cell proliferation, promoting terminal differentiation and apoptosis.

Purpose of the Study:

  • To provide an overview of entinostat's chemistry, pharmacokinetics, pharmacodynamics, and clinical data.
  • To focus on entinostat's potential in treating advanced breast cancer, particularly hormone-resistant types.

Main Methods:

  • Review of preclinical and clinical data for entinostat.
  • Overview of ongoing Phase III registration study (E2112, NCT02115282) in advanced breast cancer.

Main Results:

  • Entinostat has been evaluated in Phase I and II trials for advanced malignancies and is generally well tolerated.
  • Promising preclinical and clinical data exist for entinostat in hormone-resistant breast cancer.

Conclusions:

  • Entinostat is an orally available HDAC inhibitor with potential in advanced breast cancer.
  • Further confirmation of overall survival advantage is being investigated in a Phase III trial combining entinostat with exemestane.
Keywords:
breast cancerclinical trialsentinostatepigeneticshistone deacetylase inhibitor

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