^
    6d
    Targeting Cutaneous T-cell lymphoma in non-hodgkin lymphoma: What's new for investigational agents? (PubMed, Expert Opin Investig Drugs)
    Recent years have seen a shift away from chemotherapy with the approval of targeted therapies like mogamulizumab, brentuximab vedotin, and denileukin diftitox-cxdl. Though these novel agents have improved outcomes for patients with advanced-stage CTCL, most patients will continue to experience relapses. Emerging agents, including lacutamab, resminostat, and immune checkpoint inhibitors and biomarkers including CD5, CD70, and CD47/Sirpα represent the next frontier in maintaining durable remissions and improving quality of life (QoL) for these patients.
    Review • Journal • IO biomarker
    |
    CD70 (CD70 Molecule) • CD5 (CD5 Molecule) • SIRPA (Signal Regulatory Protein Alpha)
    |
    Adcetris (brentuximab vedotin) • Poteligeo (mogamulizumab-kpkc) • Ontak (denileukin diftitox) • Lymphir (denileukin diftitox-cxdl) • Kinselby (resminostat) • lacutamab (IPH4102)
    3ms
    Deacetylase-independent HDAC1 condensation defines temozolomide response in glioblastoma. (PubMed, Nat Chem Biol)
    Through phase-separation-based screening, we identified resminostat as an effective disruptor of HDAC1-CTCF condensates, thereby restoring temozolomide sensitivity in patient-derived xenograft models. Our findings introduce deacetylase-independent HDAC1 condensation as a distinct mechanism regulating temozolomide response, providing valuable insights into potential therapeutic strategies.
    Journal
    |
    HDAC1 (Histone Deacetylase 1)
    |
    temozolomide • Kinselby (resminostat)
    8ms
    Exploring DNA topoisomerase II alpha in adrenocortical carcinoma through multi-omics analysis: a potential biomarker and therapeutic target. (PubMed, Acta Biochim Biophys Sin (Shanghai))
    Potential inhibitors targeting TOP2A are discovered, and the therapeutic effects of resminostat and etoposide are confirmed via in vivo assays, suggesting new therapeutic strategies for ACC treatment. In conclusion, TOP2A serves as a crucial biomarker in ACC and is associated with adverse clinical outcomes and a diminished immune response. The identification of potential inhibitors against TOP2A opens new avenues for the development of targeted therapies for ACC patients.
    Journal • IO biomarker
    |
    CD8 (cluster of differentiation 8) • TOP2A (DNA topoisomerase 2-alpha)
    |
    etoposide IV • Kinselby (resminostat)
    over1year
    RESMAIN: Resminostat for Maintenance Treatment of Patients With Advanced Stage Mycosis Fungoides (MF) or Sézary Syndrome (SS) (clinicaltrials.gov)
    P2, N=201, Completed, 4SC AG | Active, not recruiting --> Completed
    Trial completion
    |
    Kinselby (resminostat)
    almost5years
    Histone deacetylase inhibitor resminostat in combination with sorafenib counteracts platelet-mediated pro-tumoral effects in hepatocellular carcinoma. (PubMed, Sci Rep)
    In addition, the drug combination decreased phosphorylated ERK level, indicating inhibition of the mitogenic signaling pathway MEK/ERK. Taken together, the resminostat plus sorafenib combination counteracts platelet-mediated cancer promoting effects in HCC cells.
    Journal • Combination therapy • Epigenetic controller
    |
    CD44 (CD44 Molecule)
    |
    CD44 expression
    |
    sorafenib • Kinselby (resminostat)
    5years
    Ruxolitinib with resminostat exert synergistic antitumor effects in Cutaneous T-cell Lymphoma. (PubMed, PLoS One)
    The JAKi/HDACi combination exhibited substantial anti-tumor effects in CTCL cell lines, and may represent a promising novel therapeutic modality for CTCL patients.
    Journal
    |
    JAK2 (Janus kinase 2) • JAK1 (Janus Kinase 1) • STAT3 (Signal Transducer And Activator Of Transcription 3)
    |
    Jakafi (ruxolitinib) • Kinselby (resminostat)
    over5years
    Resminostat, a histone deacetylase inhibitor, circumvents tolerance to EGFR inhibitors in EGFR-mutated lung cancer cells with BIM deletion polymorphism. (PubMed, J Med Invest)
    In comparison with PC-9 cells, PC-9 BIMi2- / - cells were less sensitive to apoptosis mediated by EGFR-TKIs such as gefitinib and osimertinib. Invest. 67 : 343-350, August, 2020.
    Journal
    |
    EGFR (Epidermal growth factor receptor)
    |
    EGFR mutation • BCL2L11 deletion
    |
    Tagrisso (osimertinib) • gefitinib • Kinselby (resminostat)