Syndax Pharma 
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  • ||||||||||  Farydak (panobinostat) / Novartis
    Journal, Epigenetic controller:  Class I and II Histone Deacetylase Inhibitor LBH589 Promotes Endocrine Differentiation in Bone Marrow Derived Human Mesenchymal Stem Cells and Suppresses Uncontrolled Proliferation. (Pubmed Central) -  Nov 29, 2021   
    The broad spectrum inhibitor of class I and class II histone deacetylases LBH589 upregulated the expression of these transcription factors in a significant way, whereas addition of selective class I histone deacetylase inhibitors MS-275 and MGCD0103 did not result in significant changes in gene expression.In conclusion, we deliver evidence that a combined class I and II histone deacetylase inhibition is able to modulate the transcripts of differentiation markers of mesenchymal stem cells. The treatment holds the capability to facilitate endocrine differentiation in future approaches to replace endocrine cells by stem cell therapy.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Journal:  HDAC1 deregulation promotes neuronal loss and deficit of motor function in stroke pathogenesis. (Pubmed Central) -  Nov 17, 2021   
    We also used MS-275 to inhibit HDAC1 function in rats exposed to ischemic insult...Additionally, HDAC1 inhibition deteriorated the behavioral outcomes of rats with ischemic insult. Overall, our findings demonstrate that HDAC1 participates in ischemic pathogenesis in the brain and possesses potential for use as a therapeutic target.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Journal, Tumor-specific neoantigens:  Entinostat induces antitumor immune responses through immune editing of tumor neoantigens. (Pubmed Central) -  Nov 10, 2021   
    Finally, combination treatment with anti-PD-1 and entinostat led to complete responses and conferred long-term immunologic memory. Our work defines a tumor cell-autonomous mechanism of action for entinostat and a strong preclinical rationale for the combined use of entinostat and PD-1 blockade in bladder cancer.
  • ||||||||||  VTP-50469 / Syndax Pharma
    The Menin-MLL1 Interaction Is a Molecular Dependency in NUP98-Rearranged AML (GWCC - Hall B5, Level 1) -  Nov 5, 2021 - Abstract #ASH2021ASH_3827;    
    Using mouse leukemia cell lines driven by NUP98-HOXA9 and NUP98-JARID1A fusion oncoproteins, we demonstrate that NUP98-fusion driven leukemia is sensitive to the Menin-MLL1 inhibitor VTP50469, with an IC50 similar to what we have previously reported for MLL -rearranged and NPM1c leukemia cells...Gene expression analysis revealed that Menin-MLL1 inhibition simultaneously suppresses a pro-leukemogenic gene expression program, including downregulation of the HOXA cluster, and upregulates tissue-specific markers of differentiation. These preclinical results suggest that Menin-MLL1 inhibition may represent a rational, targeted therapy for patients with NUP98 -rearranged leukemias.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Journal:  MS-275 (Entinostat) Promotes Radio-Sensitivity in PAX3-FOXO1 Rhabdomyosarcoma Cells. (Pubmed Central) -  Nov 4, 2021   
    MS-275 inhibited in vivo growth of RH30 cells and completely prevented the growth of RT-unresponsive RH30 xenografts when combined with radiation. Thus, MS-275 could be considered as a radio-sensitizing agent for the treatment of intrinsically radio-resistant PAX3-FOXO1 RMS.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Clinical, Journal, Checkpoint inhibition:  Epigenetic modifiers synergize with immune-checkpoint blockade to enhance long-lasting antitumor efficacy. (Pubmed Central) -  Oct 31, 2021   
    assess whether the HDAC inhibitor entinostat can enhance anti-PD-1 treatment in a bladder cancer model...In addition, the authors showed that HDAC inhibition augmented tumor neoantigen presentation, resulting in the immune editing of tumor antigens. This study highlights a mechanism by which epigenetic modifier agents can synergize with immune-checkpoint blockade for enhanced and long-lasting antitumor activity.
  • ||||||||||  bintrafusp alfa (M7824) / EMD Serono, Kadcyla (ado-trastuzumab emtansine) / Roche, Jingzhuda (entinostat) / EOC Pharma, EddingPharm
    Trial completion, Enrollment change, Trial completion date, Trial primary completion date, Metastases:  BN-Brachyury, Entinostat, Adotrastuzumab Emtansine and M7824 in Advanced Stage Breast Cancer (BrEAsT) (clinicaltrials.gov) -  Oct 27, 2021   
    P1b,  N=1, Completed, 
    This study highlights a mechanism by which epigenetic modifier agents can synergize with immune-checkpoint blockade for enhanced and long-lasting antitumor activity. Suspended --> Completed | N=65 --> 1 | Trial completion date: Jan 2024 --> Oct 2021 | Trial primary completion date: Jan 2024 --> Oct 2021
  • ||||||||||  paclitaxel / Generic mfg.
    Relieving immune suppressive pathways in breast cancer to improve outcomes (Stars at Night Ballroom 1&2) -  Oct 26, 2021 - Abstract #SABCS2021SABCS_1510;    
    Therapies targeting myeloid-mediated T cell suppression, in combination with PTX and αPD-1 mAb, results in tumor regression, but long-term T cell memory is limited. Durable long term anti-tumor T cell memory is instead achieved following addition of entinostat-induced epigenetic reprogramming.
  • ||||||||||  bintrafusp alfa (M7824) / EMD Serono, Kadcyla (ado-trastuzumab emtansine) / Roche, Jingzhuda (entinostat) / EOC Pharma, EddingPharm
    Trial suspension, Metastases:  BN-Brachyury, Entinostat, Adotrastuzumab Emtansine and M7824 in Advanced Stage Breast Cancer (BrEAsT) (clinicaltrials.gov) -  Oct 19, 2021   
    P1b,  N=65, Suspended, 
    Our findings demonstrate the therapeutic potential of birinapant to enhance the anti-tumor efficacy of gemcitabine in TNBC by targeting the IAP family of proteins. Recruiting --> Suspended
  • ||||||||||  mocetinostat (MGCD0103) / Mirati, Otsuka, Epidaza (chidamide) / Chipscreen, Meiji Seika, Eisai, HUYA Bioscience, entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Clinical, Journal:  Discovery of novel hit compounds as potential HDAC1 inhibitors: The case of ligand- and structure-based virtual screening. (Pubmed Central) -  Oct 13, 2021   
    The IFD and MD results cooperatively confirmed the interactions of the promising selected hits with critical residues within HDAC1 active site. In summary, the presented computational approach can provide a set of guidelines for the further development of improved benzamide-based derivatives targeting HDAC1 isoform.
  • ||||||||||  RGFP966 / BioMarin, entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma, quisinostat (JNJ 26481585) / J&J, ChemRar
    Journal:  CaMKII exacerbates heart failure progression by activating class I HDACs. (Pubmed Central) -  Oct 9, 2021   
    CaMKII activates class I HDACs in heart failure, which may be a central mechanism for heart failure progression. Selective class I HDACs inhibition may be a novel therapeutic avenue to alleviate CaMKII hyperactivity induced cardiac dysfunction.
  • ||||||||||  Jingzhuda (entinostat) / EOC Pharma, EddingPharm
    Trial completion, Trial completion date, Epigenetic controller:  Entinostat in Treating Pediatric Patients With Recurrent or Refractory Solid Tumors (clinicaltrials.gov) -  Oct 7, 2021   
    P1,  N=21, Completed, 
    Selective class I HDACs inhibition may be a novel therapeutic avenue to alleviate CaMKII hyperactivity induced cardiac dysfunction. Active, not recruiting --> Completed | Trial completion date: Aug 2022 --> Sep 2021
  • ||||||||||  Jingzhuda (entinostat) / EOC Pharma, EddingPharm
    Trial completion date, Trial primary completion date:  Entinostat Neuroendocrine (NE) Tumor (clinicaltrials.gov) -  Oct 7, 2021   
    P2,  N=40, Recruiting, 
    Active, not recruiting --> Completed | Trial completion date: Aug 2022 --> Sep 2021 Trial completion date: Aug 2021 --> Dec 2021 | Trial primary completion date: Aug 2019 --> Dec 2021
  • ||||||||||  Inlyta (axitinib) / Pfizer
    Journal, PD(L)-1 Biomarker, IO biomarker:  Axitinib and HDAC Inhibitors Interact to Kill Sarcoma Cells. (Pubmed Central) -  Oct 5, 2021   
    In vivo, axitinib and the HDAC inhibitor entinostat interacted to significantly reduce tumor growth. Collectively our findings support the exploration of axitinib and HDAC inhibitors being developed as a novel sarcoma therapy.
  • ||||||||||  Keytruda (pembrolizumab) / Merck (MSD), entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Clinical, P2 data, Clinical Trial,Phase II, Journal:  The PEMDAC phase 2 study of pembrolizumab and entinostat in patients with metastatic uveal melanoma. (Pubmed Central) -  Oct 3, 2021   
    P2
    In conclusion, HDAC inhibition and anti-PD1 immunotherapy results in durable responses in a subset of patients with metastatic UM.Trial registration ClinicalTrials.gov registration number: NCT02697630 (registered 3 March 2016). EudraCT registration number: 2016-002114-50.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma, saracatinib (AZD0530) / AstraZeneca
    Journal:  Prediction and identification of synergistic compound combinations against pancreatic cancer cells. (Pubmed Central) -  Sep 30, 2021   
    Examples of highly synergistic in vitro validated compound pairs include gemcitabine combined with Entinostat, thioridazine, loperamide, scriptaid and Saracatinib. Hence, the computational approach presented here was able to identify synergistic compound combinations against pancreatic cancer cells.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Preclinical, Journal:  Neuroprotective epi-drugs quench the inflammatory response and microglial/macrophage activation in a mouse model of permanent brain ischemia. (Pubmed Central) -  Sep 29, 2021   
    Our findings indicate that single treatment with MS-275 and resveratrol can reduce stroke-mediated brain injury and inflammation observed 2 days after the pMCAO and put the rational to test repeated administration of the drugs. The anti-inflammatory property of MS-275 and resveratrol combination can be ascribed to both primary direct inhibition of microglia/macrophage activation and secondary glial/macrophages inhibition mediated by neuroprotection.
  • ||||||||||  entinostat (SNDX-275) / Kyowa Kirin, Syndax Pharma
    Journal, Epigenetic controller:  Targeting foam cell formation in inflammatory brain diseases by the histone modifier MS-275. (Pubmed Central) -  Sep 26, 2021   
    The anti-inflammatory property of MS-275 and resveratrol combination can be ascribed to both primary direct inhibition of microglia/macrophage activation and secondary glial/macrophages inhibition mediated by neuroprotection. These findings identify class I-HDAC inhibition as a potential novel strategy to prevent disease promoting foam cell formation in CNS inflammation.
  • ||||||||||  doxorubicin hydrochloride / Generic mfg.
    Journal:  The protective effect of beta-hydroxybutyric acid on renal glomerular epithelial cells in adriamycin-induced injury. (Pubmed Central) -  Sep 21, 2021   
    In contrast, anacardic acid, a selective inhibitor of acetyltransferase, decreases the acetylation of nephrin, WT-1, and GSK3β and mitigates the podocyte protective effects of BHB. Taken together, BHB attenuates adriamycin-elicited glomerular epithelial cell injury, at least in part, by inhibiting the deacetylation of the key molecules implicated in glomerular injury.