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    DRUG:

    Jingzhuda (entinostat)

    i
    Other names: SNDX-275, MS-275, EDP-103, KHK-2375, MS 27-275, KHK2375, SND-275, SND 275, EOC-103
    Company:
    EOC Pharma, EddingPharm, Syndax Pharma
    Drug class:
    HDAC inhibitor, HDAC1 inhibitor, HDAC2 inhibitor, HDAC3 inhibitor
    Related drugs:
    2d
    Delactylation of the tumor suppressor ARHGDIB drives metastasis and chemoresistance in bladder cancer. (PubMed, Cell Rep)
    Entinostat, an inhibitor of class I HDAC, synergizes with cisplatin by preventing ARHGDIB delactylation. Collectively, our findings unveil a unique paradigm in which delactylation of tumor suppressors drives metastasis and chemoresistance. Targeting lactylation dynamics with HDAC inhibitors presents an avenue for intervention of bladder cancer.
    Journal
    |
    CHEK2 (Checkpoint kinase 2) • RAC1 (Rac Family Small GTPase 1) • HDAC2 (Histone deacetylase 2) • ARHGDIB (Rho GDP Dissociation Inhibitor Beta)
    |
    cisplatin • Jingzhuda (entinostat)
    6d
    ‌A Phase II, Two-Stage Study Evaluating the Efficacy of Entinostat in Combined with Fulvestrant in Locally Advanced or Metastatic Breast Cancer with Recurrence or Progression after CDK4/6 Inhibitor plus Endocrine Therapy (ChiCTR2500114131)
    P=N/A, N=50, Not yet recruiting, Sun Yat-sen University Cancer Center; Sun Yat-sen University Cancer Center
    New trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    HR positive • HER-2 negative
    |
    fulvestrant • Jingzhuda (entinostat)
    15d
    Single-Cell Regulatory Network Analysis Identifies Adjunctive Drug Candidates in Early Risankizumab-Treated Psoriasis. (PubMed, Curr Pharm Des)
    These findings offer preliminary clues for future risankizumab-based combination strategies in psoriasis.
    Journal
    |
    CD4 (CD4 Molecule) • S100A8 (S100 Calcium Binding Protein A8) • S100A9 (S100 Calcium Binding Protein A9) • ELF3 (E74 Like ETS Transcription Factor 3) • KRT14 (Keratin 14) • MAFB (MAF BZIP Transcription Factor B) • KRT6A (Keratin 6A) • NFIC (Nuclear Factor I C) • SREBF1 (Sterol Regulatory Element Binding Transcription Factor 1)
    |
    Jingzhuda (entinostat) • simvastatin
    18d
    Entinostat suppresses hepatocellular carcinoma metastasis by upregulating AZGP1 through histone acetylation. (PubMed, Biochem Pharmacol)
    In conclusion, our work elucidates a coherent epigenetic pathway wherein entinostat activates AZGP1 to inhibit HCC metastasis. These findings nominate AZGP1 as both a critical mediator and a potential biomarker for entinostat-based therapy in advanced HCC.
    Journal
    |
    TGFB1 (Transforming Growth Factor Beta 1) • AZGP1 (Alpha-2-Glycoprotein 1, Zinc-Binding)
    |
    Jingzhuda (entinostat)
    28d
    A Phase II Clinical Study Evaluating Entinostat With or Without Anlotinib + Fulvestrant for the Treatment of Hormone Receptor (HR) -Positive, Human Epidermal Growth Factor Receptor-2 (HER-2) -Negative Advanced Breast Cancer That Relapsed or Progressed After Endocrine Therapy (clinicaltrials.gov)
    P2, N=118, Recruiting, Zhejiang Cancer Hospital
    New P2 trial
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • PGR (Progesterone receptor)
    |
    ER positive • HR positive • HER-2 negative
    |
    Focus V (anlotinib) • fulvestrant • Jingzhuda (entinostat)
    29d
    Histone Deacetylase Inhibitor Entinostat Exerts Anti-NSCLC Effects Through the EGFR Signaling Pathway and MDM2-p53 Axis. (PubMed, Curr Pharm Biotechnol)
    Entinostat demonstrates strong anti-NSCLC activity by suppressing EGFR expression and downstream signaling, highlighting its potential as a therapeutic agent.
    Journal
    |
    STAT3 (Signal Transducer And Activator Of Transcription 3) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    |
    Zolinza (vorinostat) • Jingzhuda (entinostat)
    1m
    Targeting Class I Histone Deacetylases Triggers Antitumor Responses in Colorectal Cancer In Vitro and In Vivo. (PubMed, J Med Chem)
    The short-term in vitro effects of 5d were modulated by a compensatory upregulation of autophagy. However, in long-term, this protective mechanism becomes insufficient to sustain tumor survival, resulting in strong antitumor efficacy in vivo in the CAM assay for both compounds even outperforming entinostat.
    Preclinical • Journal
    |
    HDAC2 (Histone deacetylase 2) • HDAC1 (Histone Deacetylase 1) • CDKN1A (Cyclin-dependent kinase inhibitor 1A) • HDAC3 (Histone Deacetylase 3)
    |
    Jingzhuda (entinostat)
    1m
    Testing A New Anti-cancer Drug Combination, Entinostat and ZEN003694, for Advanced and Refractory Solid Tumors (clinicaltrials.gov)
    P1/2, N=49, Recruiting, National Cancer Institute (NCI) | N=30 --> 49
    Enrollment change
    |
    Jingzhuda (entinostat) • ZEN-3694
    1m
    A Phase I/II Study of Combination Immunotherapy for Advanced Cancers Including HPV-Associated Malignancies, Small Bowel, and Colon Cancers (clinicaltrials.gov)
    P1/2, N=55, Active, not recruiting, National Cancer Institute (NCI) | Trial primary completion date: Dec 2025 --> Nov 2026
    Trial primary completion date
    |
    PD-L1 (Programmed death ligand 1) • CD4 (CD4 Molecule)
    |
    PD-L1 negative
    |
    Jingzhuda (entinostat) • bintrafusp alfa (M7824) • PDS01ADC
    2ms
    Entinostat overcomes cisplatin resistance in bladder cancer by promoting H3K18la-mediated DHRS2 expression and nuclear translocation to suppress the AKR1C3-androgen axis. (PubMed, Drug Resist Updat)
    Furthermore, high DHRS2 predicts better survival specifically in male patients, indicating sex-specific androgen involvement. Overall, these findings elucidate the epigenetic mechanism underlying the cisplatin-sensitizing effect of Entinostat, and identifies the DHRS2-AKR1C3-androgen axis as a potential target, particularly for male patients.
    Journal
    |
    AKR1C3 (Aldo-Keto Reductase Family 1 Member C3) • DHRS2 (Dehydrogenase/Reductase 2)
    |
    cisplatin • Jingzhuda (entinostat)
    2ms
    Identification of 2 Ubiquitin-Proteasome System-Related Subtypes in Esophageal Squamous Cell Carcinoma for Prognostic and Immunotherapeutic Response Prediction. (PubMed, J Immunother)
    Selumetinib, entinostat, and erlotinib were identified as candidate drugs for cluster 2, whereas tozasertib, alpelisib, and cediranib showed higher suitability for cluster 1. Ten potential biomarkers, 13 transcription factors, and 2 miRNAs were characterized. This study elucidates the role of UPS in ESCC progression and provides a framework for personalized treatment strategies.
    Journal • IO biomarker
    |
    TP53 (Tumor protein P53) • CD8 (cluster of differentiation 8)
    |
    erlotinib • Koselugo (selumetinib) • Piqray (alpelisib) • Jingzhuda (entinostat) • Recentin (cediranib) • tozasertib (MK-0457)
    2ms
    Entinostat & Chemotherapy for Locally Advanced or Metastatic Bladder Cancer (clinicaltrials.gov)
    P1/2, N=29, Not yet recruiting, The Affiliated Nanjing Drum Tower Hospital of Nanjing University Medical School
    New P1/2 trial
    |
    cisplatin • Jingzhuda (entinostat)