Therapy Detail

Therapy Name Entinostat
Therapy Description

Entinostat (MS-275) inhibits HDAC activity, with selectivity towards HDAC1, 2, and 3, which results in increased histone acetylation, and potentially leads to decreased tumor cell proliferation and tumor growth (PMID: 19724929, PMID: 17383217).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Entinostat HDAC inhibitor SNDX-275|MS 275 HDAC Inhibitor 34 Entinostat (MS-275) inhibits HDAC activity, with selectivity towards HDAC1, 2, and 3, which results in increased histone acetylation, and potentially leads to decreased tumor cell proliferation and tumor growth (PMID: 19724929, PMID: 17383217).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
Unknown unknown epithelioid sarcoma not applicable Entinostat Preclinical Actionable In a preclinical study, Entinostat inhibited growth and colony formation of epithelioid sarcoma cells in culture (PMID: 26396249). 26396249
FBXW7 inact mut Advanced Solid Tumor sensitive Entinostat Preclinical Actionable In a preclinical study, entinostat (MS-275) inhibited cancer cells from advanced solid tumors and hematological cells harboring FBXW7 inactivating mutations in culture (PMID: 23274910). 23274910
Unknown unknown Advanced Solid Tumor not applicable Entinostat Phase I Actionable In a Phase I trial, Entinostat treatment in patients with advanced solid tumors resulted in a partial response in 7% (2/27) of patients and stable disease in 26% (7/27) of patients, which ranged from 45 days to 10 months (PMID: 18579665). 18579665
FBXW7 inact mut hematologic cancer sensitive Entinostat Preclinical Actionable In a preclinical study, entinostat (MS-275) inhibited cancer cells from advanced solid tumors and hematological cells harboring FBXW7 inactivating mutations in culture (PMID: 23274910). 23274910
RB1 loss retinoblastoma sensitive Entinostat Preclinical - Cell line xenograft Actionable In a preclinical study, Entinostat (MS-275) inhibited growth of retinoblastoma cell lines in culture and inhibited tumor growth in a retinoblastoma cell line xenograft model (PMID: 18483379), which have been demonstrated to be deficient in RB1 (PMID: 23498719). 23498719 18483379
Clinical Trial Phase Therapies Title Recruitment Status
NCT03211988 Phase II Entinostat Entinostat Neuroendocrine (NE) Tumor Recruiting
NCT01928576 Phase II Nivolumab Entinostat Azacitidine Phase II Anti-PD1 Epigenetic Priming Study in NSCLC. Recruiting
NCT01038778 Phase Ib/II Entinostat Aldesleukin Entinostat in Combination With Aldesleukin in Treating Patients With Metastatic Kidney Cancer Active, not recruiting
NCT03361800 Entinostat Window of Opportunity Trial of Entinostat in Patients With Newly Diagnosed Stage I-IIIC,TNBC Recruiting
NCT02453620 Phase I Entinostat Nivolumab + Ipilimumab Entinostat, Nivolumab, and Ipilimumab in Treating Patients With Solid Tumors That Are Metastatic or Cannot Be Removed by Surgery or Locally Advanced or Metastatic HER2-Negative Breast Cancer Recruiting
NCT02897778 Phase I Entinostat Cardiac Safety Study of Entinostat in Men and Women With Advanced Solid Tumors Completed
NCT02780804 Phase I Entinostat Entinostat in Treating Pediatric Patients With Recurrent or Refractory Solid Tumors Recruiting
NCT02115282 Phase III Goserelin Entinostat Exemestane Exemestane With or Without Entinostat in Treating Postmenopausal Patients With Recurrent Hormone Receptor-Positive Breast Cancer That is Locally Advanced or Metastatic Active, not recruiting