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    DRUG CLASS:

    CK1α degrader

    Related drugs:
    2ms
    A Study of GLB-001 in Patients With Relapsed or Refractory Acute Myeloid Leukemia or Relapsed or Refractory Higher Risk Myelodysplastic Syndromes (clinicaltrials.gov)
    P1, N=48, Recruiting, GluBio Therapeutics Inc. | Trial primary completion date: Oct 2025 --> Jul 2026
    Trial primary completion date • First-in-human
    4ms
    Study to Evaluate Safety and Tolerability of CC-91633 (BMS-986397) in Participants With Relapsed or Refractory Acute Myeloid Leukemia or Relapsed or Refractory Higher-Risk Myelodysplastic Syndromes (clinicaltrials.gov)
    P1, N=56, Terminated, Celgene | N=180 --> 56 | Trial completion date: May 2027 --> Jul 2025 | Active, not recruiting --> Terminated | Trial primary completion date: May 2026 --> Jul 2025; Efficacy endpoint met; however, overall experimental dosing regimen is not considered optimal to support further clinical development in this patient population
    Enrollment change • Trial completion date • Trial termination • Trial primary completion date
    7ms
    Study to Evaluate Safety and Tolerability of CC-91633 (BMS-986397) in Participants With Relapsed or Refractory Acute Myeloid Leukemia or Relapsed or Refractory Higher-Risk Myelodysplastic Syndromes (clinicaltrials.gov)
    P1, N=180, Active, not recruiting, Celgene | Recruiting --> Active, not recruiting
    Enrollment closed
    1year
    Development of Oral, Potent, and Selective CK1α Degraders for AML Therapy. (PubMed, JACS Au)
    These findings indicate that phenotypic drug discovery campaigns, in combination with chemically distinct CRBN ligand libraries, can accelerate the development of therapeutically relevant MGDs. Furthermore, the development of dCK1α-1 and dCK1α-2 provides new therapeutic options for cancers with functional p53 signaling and offers valuable chemical tools for future investigations into the role of CK1α.
    Journal
    |
    CRBN (Cereblon)
    over1year
    Study to Evaluate Safety and Tolerability of CC-91633 (BMS-986397) in Participants With Relapsed or Refractory Acute Myeloid Leukemia or Relapsed or Refractory Higher-Risk Myelodysplastic Syndromes (clinicaltrials.gov)
    P1, N=180, Recruiting, Celgene | N=120 --> 180
    Enrollment change
    over1year
    GLB-001-02: A Study of GLB-001 in Patients With Myeloid Malignancies (clinicaltrials.gov)
    P1, N=108, Recruiting, Hangzhou GluBio Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    JAK2 (Janus kinase 2)
    over1year
    A Study of GLB-001 in Patients With Myeloid Malignancies (clinicaltrials.gov)
    P1, N=108, Not yet recruiting, Hangzhou GluBio Pharmaceutical Co., Ltd.
    New P1 trial
    |
    JAK2 (Janus kinase 2)
    almost2years
    Selective CK1α degraders exert antiproliferative activity against a broad range of human cancer cell lines. (PubMed, Nat Commun)
    In a panel of 115 cancer cell lines SJ3149 displays a broad antiproliferative activity profile, which shows statistically significant correlation with MDM2 inhibitor Nutlin-3a. These findings suggest potential utility of selective CK1α degraders for treatment of hematological cancers and solid tumors.
    Preclinical • Journal
    |
    IKZF1 (IKAROS Family Zinc Finger 1) • CRBN (Cereblon) • IKZF3 (IKAROS Family Zinc Finger 3) • DDB1 (Damage Specific DNA Binding Protein 1)
    |
    Nutlin-3
    over2years
    Dual IKZF2 and CK1α degrader targets acute myeloid leukemia cells. (PubMed, Cancer Cell)
    Target degradation by DEG-35 or a more soluble analog, DEG-77, delays leukemia progression in murine and human AML mouse models. Overall, we provide a strategy for multitargeted degradation of IKZF2 and CK1α to enhance efficacy against AML that may be expanded to additional targets and indications.
    Journal
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    CRBN (Cereblon) • IKZF2 (IKAROS family zinc finger 2)
    almost3years
    Discovery of potent and selective CK1α molecular degrader with a favorable safety profile for acute myeloid leukemia and solid tumors (AACR 2023)
    Also, we found that the combination treatment of PIN-A1 with agent X had a substantial effect on several solid tumors driven by enhancing the stability and activity of p53. In summary, these results suggest that a CK1α MGD with its favorable safety profile has a potential to become an effective treatment option for advanced AML and solid tumors.
    Clinical
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    CRBN (Cereblon)
    |
    TP53 mutation • TP53 wild-type
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    PIN-A1
    almost3years
    Developing PROTACs and molecular glues for pediatric leukemias (ACS-Sp 2023)
    The design of a Molecular Glue Library (MGL) containing over 5,000 small molecules, its screening against a large panel of cancer cell lines, and discovery of highly potent and selective GSPT1 and CK1a degraders will also be discussed. Extensive in vitro/vivo data will be disclosed to highlight lessons learned and discuss future opportunities for pediatric cancer research.
    Clinical
    |
    JAK2 (Janus kinase 2) • CRBN (Cereblon) • BRD4 (Bromodomain Containing 4) • GSPT1 (G1 To S Phase Transition 1)