Drug intelligence / Profile preview

entinostat + pembrolizumab

Development stage
Phase 2
Lead developer
Syndax Pharmaceuticals
Modality
Monoclonal Antibodies → Antibody-Based Therapeutics, Small Molecules
Administration
Oral, Intravenous
01

Overview

Entinostat + pembrolizumab is an investigational combination therapy consisting of two agents with distinct mechanisms of action. Entinostat is an oral class I selective histone deacetylase (HDAC) inhibitor that modulates epigenetic regulation and can reduce immunosuppressive cell types in the tumor microenvironment. Pembrolizumab (Keytruda) is a humanized monoclonal antibody targeting programmed death receptor-1 (PD-1), functioning as an immune checkpoint inhibitor to enhance anti-tumor immune responses. The combination has been studied in multiple cancer types—including non-small cell lung cancer (NSCLC), melanoma, uveal melanoma, myelodysplastic syndromes (MDS), acute myeloid leukemia (AML), Hodgkin lymphoma, and colorectal cancer—primarily in patients who are refractory or have progressed on prior therapies. Clinical trials have shown some durable responses in select subgroups but also notable toxicity and limited efficacy overall; ongoing research aims to identify populations most likely to benefit from this regimen[1][4][5][6][7][8].

Other names
entinostat and pembrolizumabentinostat plus pembrolizumab
02

Targets

HDAC1 (Histone Deacetylase 1)HDAC2 (Histone deacetylase 2)HDAC3 (Histone Deacetylase 3)PDCD1 (Programmed cell death protein 1 receptor)

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