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    DRUG:

    SLS009

    i
    Other names: SLS009, GFH009, GFH-009, GFH 009
    Company:
    GenFleet Therap, SELLAS Life Sciences
    Drug class:
    CDK9 inhibitor
    Related drugs:
    26d
    A Study of GFH009 in Combination With Zanubrutinib in Subjects With Relapsed or Refractory DLBCL (clinicaltrials.gov)
    P1/2, N=51, Recruiting, Zhejiang Genfleet Therapeutics Co., Ltd.
    New P1/2 trial • Combination therapy
    |
    Brukinsa (zanubrutinib) • SLS009
    3ms
    A Study of GFH009 Monotherapy in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (PTCL) (clinicaltrials.gov)
    P1/2, N=95, Recruiting, Zhejiang Genfleet Therapeutics Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    SLS009
    5ms
    The pharmacodynamic and mechanistic foundation for the antineoplastic effects of GFH009, a potent and highly selective CDK9 inhibitor for the treatment of hematologic malignancies. (PubMed, Oncotarget)
    Through rapid 'on-off' CDK9 inhibition, GFH009 exerts a proapoptotic effect on HHM preclinical models triggered by dynamic deprivation of crucial cell survival signals. Our results mechanistically establish CDK9 as a targetable vulnerability in assorted HHMs and, along with the previously shown superior class kinome selectivity of GFH009 vs other CDK9 inhibitors, strongly support the rationale for currently ongoing clinical studies with this agent in acute myeloid leukemia and other HHMs.
    PK/PD data • Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1)
    |
    MYC expression
    |
    SLS009
    10ms
    A Study of GFH009 Monotherapy in Patients With Relapsed or Refractory Peripheral T-cell Lymphoma (PTCL) (clinicaltrials.gov)
    P1/2, N=95, Not yet recruiting, Zhejiang Genfleet Therapeutics Co., Ltd.
    New P1/2 trial
    |
    SLS009
    over1year
    First in Human (FIH) Study of GFH009, a Highly Selective Cyclin-Dependent Kinase 9 (CDK9) Inhibitor, in Patients with Relapsed/Refractory (r/r) Hematologic Malignancies (ASH 2022)
    GFH009 as monotherapy is well tolerated at the tested doses and has shown clinical activity in patients with r/r lymphoma. The dose escalation in patients with AML and lymphoma is ongoing. Different dosing regimens are currently being explored for potentially better inhibition on the target.
    Clinical • P1 data
    |
    CDK9 (Cyclin Dependent Kinase 9)
    |
    Venclexta (venetoclax) • SLS009
    over1year
    In Vitro and In Vivo Studies Support GFH009, a Selective CDK9 Inhibitor, As a Potential Treatment for Hematologic Cancers (ASH 2022)
    The reference compound enitociclib (BAY 1251152) was used for experimental validation. Although several cytotoxic molecules that inhibit CDK9 are in the therapeutic pipeline, many show cross-reactivity to other CDK family members, leading to toxicity and tolerability issues. GFH009 is a potent and highly selective CDK9 inhibitor with the ability to reduce expression of downstream oncogenes required for rapid cellular division and protein expression through specific, short-lived inhibition of CDK9. We postulate that this mechanism drives GFH009's inhibition of cellular division, as tumor stabilization and shrinkage appear to be dose-dependent.
    Preclinical
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog) • MCL1 (Myeloid cell leukemia 1) • CASP3 (Caspase 3)
    |
    MYC expression • MCL1 expression
    |
    enitociclib (VIP152) • SLS009
    over1year
    AML-259 Pharmacokinetics and Bioequivalence of Two Formulations of GFH009 Maleate Injection in Sprague Dawley Rats. (PubMed, Clin Lymphoma Myeloma Leuk)
    The PK profiles of GFH009 were comparable following single IV administration of two formulations of GFH009 maleate injection in SD rats, which supported application of the pH 6.0 formulation in Phase I trials in patients with relapsed/refractory hematologic conditions, including AML and lymphoma.
    Clinical • PK/PD data • Preclinical • Journal
    |
    MCL1 (Myeloid cell leukemia 1) • CDK9 (Cyclin Dependent Kinase 9)
    |
    MYC expression • MCL1 expression
    |
    SLS009
    over1year
    Pharmacokinetics and Bioequivalence of Two Formulations of GFH009 Maleate Injection in Sprague Dawley Rats (SOHO 2022)
    The PK profi les of GFH009 were comparable following single IV administration of two formulations of GFH009 maleate injection in SD rats, which supported application of the pH 6.0 formulation in Phase I trials in patients with relapsed/refractory hematologic conditions, including AML and lymphoma.
    PK/PD data • Preclinical
    |
    MCL1 (Myeloid cell leukemia 1) • CDK9 (Cyclin Dependent Kinase 9)
    |
    MYC expression • MCL1 expression
    |
    SLS009