Analyst Outlook
Entinostat (Syndax Pharmaceuticals/Kyowa Hakko Kirin) may have an advantage over other pipeline
therapies in development for metastatic hormone receptor-positive (HR+)/human epidermal growth
factor receptor 2-negative (HER2-) breast cancer, because Phase II data have demonstrated that it
significantly improves overall survival (OS). If approved, entinostat will compete for relapsed
HR+/HER2- breast cancer patients with currently marketed therapies Faslodex (fulvestrant;
AstraZeneca) and Halaven (eribulin mesylate; Eisai), which have also demonstrated OS benefits in
Phase III trials.
Drug Overview
Entinostat is a class I selective histone deacetylase (HDAC) inhibitor. HDACs influence the expression
of genes involved in both the initiation of cancer and its progression through several pathways.
Specifically, class I HDACs play a role in cell survival and proliferation. Overexpression of class I HDACs
can lead to the repression of p53 and von Hippel–Lindau tumor suppressors, in addition to reductions
in the expression of the cyclin-dependent kinase (CDK) inhibitor p21. Histone deacetylation has also
been shown to cause resistance to endocrine therapies via the repression of the estrogen receptor (ER)
(Glozak and Seto, 2007; Ropero and Esteller, 2007; Sabnis et al., 2011).
TABLE OF CONTENTS
4 PRODUCT PROFILES
4 entinostat : Breast cancer: HR+/HER2-
LIST OF FIGURES
11 Figure 1: Entinostat for HR+/HER2- breast cancer – SWOT analysis
11 Figure 2: Datamonitor Healthcare’s drug assessment summary of entinostat in HR+/HER2-
breast cancer
12 Figure 3: Datamonitor Healthcare’s drug assessment summary of entinostat in HR+/HER2-
breast cancer
LIST OF TABLES
4 Table 1: Entinostat drug profile
7 Table 2: Entinostat Phase III trial in HR+/HER2- breast cancer
9 Table 3: Entinostat Phase II data in HR+/HER2- breast cancer