Entinostat (Not yet branded)

Other Medications

US Experimental EU Experimental ES Not available Oral 4 Clinical Trials
HDAC1 HDAC3

Description

Entinostat is a selective histone deacetylase (HDAC) inhibitor that has been evaluated in combination therapies for metastatic colorectal cancer, particularly in microsatellite stable (MSS) tumors. This epigenetic modifier is being tested alongside other agents like azacitidine and immunotherapy combinations to enhance treatment responses in advanced solid tumors. Entinostat represents a class of drugs that target chromatin remodeling to restore normal gene expression patterns in cancer cells.

Mechanism of Action

Entinostat selectively inhibits class I histone deacetylases, particularly HDAC1 and HDAC3, which leads to increased acetylation of histones and other proteins. This epigenetic modification results in chromatin relaxation and reactivation of tumor suppressor genes that have been silenced in cancer cells. The drug may also enhance immune recognition of tumors by upregulating antigen presentation and immune checkpoint molecules.

Molecular Targets

Side Effects

Fatigue Nausea Thrombocytopenia Neutropenia Anemia Decreased appetite Diarrhea Vomiting

Not all side effects are listed. Side effects vary by individual. Always consult your oncologist.

Clinical Trials

NCT04708470 Phase 1
Active, not recruiting
A Phase I/II Study of Combination Immunotherapy for Advanced Cancers Including HPV-Associated Malignancies, Small Bowel, and Colon Cancers
United States
NCT03215264 Phase 1
Archived
To Determine the Safety of Regorafenib, Hydroxychloroquine, and Entinostat Metastatic Colorectal Cancer
United States
NCT02437136 Phase 1
Archived
Ph1b/2 Dose-Escalation Study of Entinostat With Pembrolizumab in Non-small Cell Lung Cancer (NSCLC) With Expansion Cohorts in NSCLC, Melanoma, and Colorectal Cancer (CRC)
United States
NCT01105377 Phase 2
Archived
Azacitidine and Entinostat in Treating Patients With Metastatic Colorectal Cancer
United States