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    DRUG:

    purinostat

    Company:
    Baoling Bio
    Drug class:
    HDAC1 inhibitor, HDAC2b inhibitor
    Related drugs:
    4ms
    A Phase IIa Clinical Study of Puesta Mesylate for Injection in Patients With T-Cell Lymphoma and Cutaneous T-Cell Lymphoma (clinicaltrials.gov)
    P2, N=50, Recruiting, Chengdu Zenitar Biomedical Technology Co., Ltd
    New P2 trial
    |
    purinostat
    4ms
    Puesta Mesylate Combined With Pomalidomide Capsules and Low-dose Dexamethasone in Patients With Relapsed or Refractory Multiple Myeloma (clinicaltrials.gov)
    P1/2, N=126, Not yet recruiting, Chengdu Zenitar Biomedical Technology Co., Ltd
    New P1/2 trial • Combination therapy
    |
    dexamethasone • pomalidomide • purinostat
    6ms
    A Clinical Study of Puesta Mesylate for Injection in Patients With Solid Tumors (clinicaltrials.gov)
    P1/2, N=120, Not yet recruiting, Chengdu Zenitar Biomedical Technology Co., Ltd
    New P1/2 trial
    |
    Tevimbra (tislelizumab-jsgr) • exemestane • purinostat
    almost2years
    In vitro pharmacodynamic studies of novel class Ⅰ and Ⅱb selective histone deacetylase inhibitor purinostat mesylate in the treatment of diffuse large B-cell lymphoma and its mechanism (PubMed, Zhonghua Xue Ye Xue Za Zhi)
    In addition, PM could downregulate the expression of oncogene marker proteins MYC, IKZF1, and IKZF3. PM has an efficient biological activity in vitro for diffuse large B-cell lymphoma, including double-hit lymphoma, and provides valuable experimental evidence for PM in clinical treatment.
    PK/PD data • Preclinical • Journal • IO biomarker • Epigenetic controller
    |
    BCL2 (B-cell CLL/lymphoma 2) • CCND1 (Cyclin D1) • CDK4 (Cyclin-dependent kinase 4) • IKZF1 (IKAROS Family Zinc Finger 1) • CDK6 (Cyclin-dependent kinase 6) • IKZF3 (IKAROS Family Zinc Finger 3) • CASP3 (Caspase 3) • CDK2 (Cyclin-dependent kinase 2) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    |
    MYC expression • CCND1 expression • CDK2 expression • CDK6 expression
    |
    purinostat
    2years
    HDAC I/IIb selective inhibitor Purinostat Mesylate combined with GLS1 inhibition effectively eliminates CML stem cells. (PubMed, Bioact Mater)
    The combination of PMF and glutaminase inhibitor BPTES synergistically eradicated LSCs by altering multiple key proteins and signaling pathways which are critical for LSC survival and self-renewal. Overall, our findings represent a new therapeutic strategy for eliminating LSCs by targeting HDAC I/IIb and glutaminolysis, which potentially provides a guidance for PMF clinical trials in the future for TKI resistance CML patients.
    Journal
    |
    ABL1 (ABL proto-oncogene 1) • BCR (BCR Activator Of RhoGEF And GTPase) • MYC (V-myc avian myelocytomatosis viral oncogene homolog) • CTNNB1 (Catenin (cadherin-associated protein), beta 1) • CD34 (CD34 molecule) • GLS1 (Glutaminase)
    |
    purinostat